Acyclovir, 1 piece, 0.25 g, lyophilisate for solution for infusion

From this article you will learn:

• what does Acyclovir help with?
• instructions for use of acyclovir (in children and adults),
• what analogues are there?
• tablets, ointment or cream acyclovir – price 2022.

Acyclovir is the first specific antiviral drug, which since 1981 has been widely used in the treatment of herpes simplex virus (types HSV-1, HSV-2), as well as herpes zoster and chickenpox. Type of virus HSV-1 - causes herpes on the lips, facial skin and oral mucosa. The HSV-2 virus type is predominantly genital herpes only, but in 10% of patients it can also cause both herpetic stomatitis and herpes labialis.

Acyclovir has a rather weak effect on other representatives of the herpevirus family (Epstein-Barr virus, cytomegalovirus). The drug is very well tolerated by children, even the youngest, and can also be used during pregnancy. Acyclovir cream or ointment is intended for external use and is available without a prescription, but Acyclovir tablets or vials for intravenous administration should be used only as prescribed by a doctor!

Acyclovir: photos of several release options

Composition and release form –

• cream for external use 5%,
• ointment for external use 5%,
• eye ointment 3%,
• Acyclovir tablets 200 and 400 mg,
• in bottles for preparing a solution (200 mg, 250 mg, 500 mg or 1 g).

Acyclovir analogues of the drug - the original drugs of acyclovir are drugs from the Zovirax line - from (Great Britain). All drugs containing acyclovir from other manufacturers are only generics, for example, Acyclovir-Akrikhin (Russia), Acyclovir-Sandoz (Switzerland), Acyclovir-Hexal (Germany), Acyclovir-Belupo (Croatia), as well as many others. And although manufacturers of generic drugs say that their drugs are no less effective, most doctors believe that generic drugs are still inferior to original drugs in terms of such criteria as effectiveness and safety. At the end of the article, you can also read about modern analogues of acyclovir - the antiviral drugs Famciclovir, Valacyclovir and Penciclovir.

Important: the original acyclovir under the Zovirax brand in tablets can be taken from 0 years of age. At the same time, the instructions for the Russian drug “Acyclovir-Akrikhin” indicate that children under 2 years of age are a contraindication. The same applies to the use of Acyclovir tablets during breastfeeding (Zovirax is allowed with caution, but for the Russian analogue this would be a contraindication).

Pharmacological action of the drug -

Acyclovir itself is not an active substance. Acyclovir acquires its antiviral activity only after it enters virus-infected cells, in which (under the influence of the enzyme “viral thymidine kinase”), acyclovir is converted first into acyclovir monophosphate, and then into acyclovir triphosphate. The latter is already an active component, which suppresses the reproduction of the herpes simplex virus - by incorporating acyclovir triphosphate into the viral DNA.

When will acyclovir be effective?

The use of acyclovir will give a pronounced effect only if several conditions are met. Firstly, if you started using the drug - during the prodromal period of the development of a herpetic infection (i.e. when there are no actual clinical manifestations yet, but there is already a burning, tingling or distension of tissue - in places where herpetic blisters will soon appear). Secondly, the effectiveness will be high even if therapy is started - within the first 12 hours from the moment the rash appears. By starting treatment this early, it is possible to reduce the duration of herpes symptoms by approximately 20 to 50%.

If the use of acyclovir begins from 12 to 72 hours (from the moment the rash appears), then its effectiveness will be very moderate. If more than 72 hours have passed and/or the herpetic blisters have already opened, acyclovir will not have a significant effect on the course of the disease at all. But when prescribing antiviral drugs (this applies to both creams and tablets), it is also important to take into account the potential risk of resistance of your herpes virus to acyclovir. All of the above is true for both tablets and Acyclovir ointment.

Important: with Acyclovir cream for the treatment of herpes on the skin or red border of the lips - everything is quite simple, and the main thing is to observe the correct timing of the start of therapy. But for acyclovir tablets for oral administration, it is also important to choose the correct dosage. Recent clinical studies (source) have shown the ineffectiveness of systemic therapy - using the basic standard dosage of acyclovir (200 mg 5 times a day, for 5 days). And below we will tell you what dosages are now recognized by the medical community as effective.

Resistance of the herpes virus to acyclovir -

In patients with good immunity, resistance to Acyclovir is rare - approximately 1 to 3% of cases. However, there is a clear relationship: the risk of developing resistance to acyclovir is directly proportional to the frequency and duration of its use. Resistance occurs especially often - 1) in immunocompromised patients who in the past regularly used drugs with acyclovir for treatment or prophylactic purposes, 2) in patients with HIV infection, 3) in patients with a history of bone marrow transplantation.

In the above groups, resistance can range from 7 to 27%, and according to some sources, even reach 30-36%. If any of the above applies to you, then you should not waste precious time taking acyclovir, choosing its stronger analogues. We are talking about antiviral tablet drugs based on Famciclovir or Valaciclovir. If we are talking about the form in the form of a cream (for external use), then it is better to use Fenistil-Pentsivir cream (contains penciclovir).

Injections for herpes: answers to patient questions

What are the best injections for herpes?

Currently, the most powerful antiviral drugs are Cycloferon, Allokin-Alpha, Alloferon.

What injections can you buy that completely kill herpes?

Today, no drugs have been found that can completely destroy the herpes virus.

However, there are drugs that can effectively suppress the symptoms of the virus and increase the protective functions of the immune system, reducing the risk of relapse of the disease.

Acyclovir ointment: instructions for use

Let's now figure out what Acyclovir ointment or cream helps with. This drug can only be used externally, and indications for its use:

• infections of the skin and mucous membranes caused by the herpes simplex virus (types HSV-1 and HSV-2), i.e. First of all, this is herpes on the lips and skin around the mouth, as well as as part of complex therapy for the treatment of genital herpes.

We have already said above that the key to the effectiveness of treatment with acyclovir is the earliest possible start of using the drug (24stoma.ru). For example, in the prodromal period (when the feeling of itching and bloating is just beginning to appear), or during the first 12 hours from the moment herpetic blisters erupt. If acyclovir ointment or cream is started to be used only after 48 hours or even after the herpetic blisters have opened, this will not reduce the duration of symptoms at all.

Application regimen - the effective concentration of acyclovir for the treatment of herpes of the lips and facial skin is 5%. It is very important to strictly follow the application regimen. For acyclovir ointment, the instructions for use state that the drug should be applied to the skin and red border of the lips 5-8 times a day (i.e., preferably every 2 hours while you are awake). The cream is applied in a thin layer to the areas of herpetic rashes and the adjacent skin - with careful massaging movements. The usual course of use is 5-6 days, but with severe clinical manifestations - up to 10 days.

How to choose ointment or cream with acyclovir –

Please note that acyclovir ointment and acyclovir cream differ in their properties. The ointment is absorbed much less well, which means the acyclovir contained in it will penetrate much worse into the skin cells affected by herpes, which reduces the effectiveness of the drug. The ointment is much cheaper to produce (than cream), and therefore 5% acyclovir ointment - the price starts from only 35 rubles.

The disadvantage of Acyclovir is also its rather poor penetration through the stratum corneum of the epidermis of the skin. To increase skin permeability to acyclovir, a number of manufacturers add propylene glycol to the composition. This component is added to the original acyclovir preparations - Zovirax cream and Zovirax Duo-Active cream, as well as to generics - Acyclovir-Belupo, Acyclovir-Sandoz and the Russian ointment Acyclovir-Acri.

If we compare the effectiveness of cream and ointment with the same 5% concentration of acyclovir, then the effectiveness of the cream will be higher. The cream tends to be absorbed faster, which means that acyclovir will better penetrate from the cream into the skin cells affected by the virus. Zovirax cream also contains dimethicone (silicone), which allows even cosmetics to be applied immediately after the cream is absorbed. On the other hand, Acyclovir-Acri 5% ointment will cost you only 40 rubles, and Zovirax cream will cost you 190 rubles. By the way, dimethicone is also included in the Acyclovir-Sandoz cream, which costs from 150 rubles.

Zovirax or Acyclovir: which is better? So, Zovirax cream is certainly better - when compared with Acyclovir Acri or similar drugs from other manufacturers. In addition to the classic Zovirax cream, which contains 5% acyclovir, propylene glycol and dimethicone, there is also Zovirax Duo-Active cream (it additionally contains 1% hydrocortisone). For example, if you start using this cream early in the prodromal period, due to hydrocortisone it can reduce the number and size of herpetic blisters that form, and sometimes even prevent their formation.

In our opinion, Zovirax Duo-Active cream is the best option for ointment or cream with acyclovir for herpes on the lips or facial skin. This cream has only 2 disadvantages - the price starts from 350 rubles (only 2 g per tube) and the age limit is up to 12 years. But, if we consider good herpes creams not only based on acyclovir, then Fenistil-Pentsivir (based on penciclovir) is also a very good cream. But the latter is currently temporarily unavailable in pharmacies - most likely due to the re-registration of the drug in Russia.

Acyclovir: injections for herpes

Injections for herpes are given intramuscularly.

This ensures rapid entry of the drug into the body and a higher therapeutic effect.

Virostatic agents containing a substance known as acyclovir are particularly effective.

These medications can be used as ointments, tablets, or intravenous injections.

Serious herpes infections must be treated with large doses of acyclovir, given regularly in parenteral form.

The most effective injections for herpes:

Acyclovir

Nucleoside analogue with selective action.

Acyclovir is an antiviral drug.

Slows down the growth and spread of the herpes virus, allowing the body to fight the infection.

Acyclovir cannot completely eliminate the herpes virus, but it can reduce the severity of the infection.

Acyclovir injection is used to treat severe illnesses caused by herpes viruses.

Including severe forms of genital herpes, encephalitis (brain swelling), Varicella–Zoster virus.

Injections against herpes with Acyclovir help prevent the formation of new rashes.

Minimizes the risk of complications due to the infectious process.

The drug accelerates the formation of crusts and reduces the severity of pain in patients with Herpes zoster (shingles/herpes).

Dosage and regimen of Acyclovir: one ampoule of the drug is diluted in 10 ml of 0.9% NaCl solution.

The medication is administered intravenously, slowly, over 60 minutes.

The product can also be administered dropwise, after diluting it in 100 ml of isotonic solution.

It is recommended to stop using Acyclovir if the following side effects develop:

• decreased urination, change in urine color
• the appearance of fever, chills, body aches, flu symptoms
• deterioration of the skin (redness, peeling, itching)
• development of jaundice (yellowing of the skin and mucous membranes of the eyes)
• swelling, tenderness, change in skin color at the injection site
• fatigue, deterioration of health, increased body temperature.

Less serious side effects may include:

• nausea, vomiting, diarrhea, stomach pain, loss of appetite
• muscle pain, numbness or tingling in the lower extremities
• loss of coordination
• drowsiness, loss of appetite
• headache, feeling dizzy

The development of an acute allergic reaction during the use of the drug is extremely rare.

Mainly due to incorrect dosing.

If any adverse reaction develops, even minor, it is recommended to consult a doctor and consult about the need to change the medication.

The drug is not prescribed if there is an allergic reaction to the active components of the medication.

And also in case of intolerance to the drug Valaciclovir.

Acyclovir does not prevent the spread of genital herpes.

Avoid sexual intercourse or use a latex condom to prevent spreading the virus and infecting your sexual partner.

Cycloferon injections for herpes

The use of the basic regimen of Cycloferon injections for herpes has an antiviral and immunostimulating effect.

The drug is a kind of inducer involved in the formation of endogenous interferon.

Interferon is a type of cytokine family originally identified as a factor that suppresses viral infection.

Additionally, the medication reduces the severity of the inflammatory reaction and has a slight antitumor effect.

Especially manifested in relation to papillomas/condylomas with HPV.

During the use of the drug, autoimmune reactions are suppressed.

The severity of pain and inflammation in the epidermis is reduced.

The drug reduces the severity of the symptomatic picture of viral pathology.

It starts the process of activating the immune system and has a bacteriostatic effect.

The effectiveness of the drug allows it to be prescribed for chlamydia infection.

When diagnosed with herpes, injections with Cycloferon are prescribed according to the following scheme: 1st day, 2nd, then on the 4th and 6th and 8th days.

After a two-day break, the injection is administered on days 11, 14 and 17, then on days 23, 26 and 29.

The drug is administered intramuscularly or intravenously, depending on the doctor’s recommendations.

The injection is given once a day.

Cycloferon has virtually no contraindications.

Not prescribed for liver cirrhosis and intolerance to the components of the drug.

The drug is not prescribed during pregnancy and lactation.

Has excellent compatibility with other medications.

Polyoxidonium injections for herpes

Polyoxidonium is a powerful immune stimulant.

Its use leads to a significant activation of the immune system's ability to respond to foreign antigens.

It “turns off” pathogenic microorganisms, soluble toxins, and other harmful microparticles.

The pharmacological action of the drug is represented by its following abilities:

• Polyoxidonium activates three subpopulations of phagocytes: the movement of resident macrophages, phagocytes of the blood supply and phagocytes of the reticuloendothelial tissue. This action is expressed in the activation of macrophage migration, their ability to capture and digest pathogenic microorganisms.
• The medication increases the efficiency of interaction between T and B lymphocytes in antibody production reactions as a response to pathogens.
• When stimulating the reactions of the immune system, Polyoxidonium does not disrupt the natural process of their inhibition.

Polyoxidonium is recommended for use as additional therapy for the following conditions:

• Diseases of viral, infectious and bacteriological etiology, including those occurring in a chronic form.
• Complications in the postoperative period, accompanied by purulent-septic lesions.
• The drug is prescribed to patients after undergoing a course of cancer therapy.
• Recommended as a prevention of toxic effects on the liver and kidneys when taking potent medications.
• To accelerate the regenerative capabilities of the body in case of fractures, sprains, burns.
• Prescribed to increase the effectiveness of treatment of pathologies of the musculoskeletal system and joint tissue.
• For acute infectious and inflammatory pathologies of the urogenital tract in men and women.
• As maintenance therapy in the presence of HIV infection or AIDS.

For children older than six months, the drug can be prescribed as the main method of treatment in the following cases:

• Diseases of a viral or infectious nature, occurring in acute as well as chronic forms.
• Pathologies of the allergic type, which are accompanied by the development of a number of complications: bronchial asthma, eczema, acute dermatitis.

Injections with the drug Polyoxidonium are prescribed to patients with ongoing herpes as a means of increasing the protective functions of the immune system.

However, it is worth remembering that this is just a drug that complements the main treatment.

Therefore, when treating a herpetic infection, an antiviral agent is prescribed.

Injections for herpes: Panavir

Panavir is a herbal preparation.

Contains an extract from the shoots of the plant Solanum tuberosum (potato, Solanaceae family).

Solanum tuberosum contains a hexose glycoside.

Glycosides are used by plants to protect against pathogenic microorganisms.

Hexose glycoside is used by the pharmaceutical industry for its pharmacological effects.

It reduces the inflammatory response by inhibiting histamine and provides an anticonvulsant and antiviral effect.

The action of Panavir is aimed at increasing nonspecific immunity and increasing the production of interferon by blood cells.

The drug is quite well tolerated.

Does not have a toxic effect on the liver and kidneys, does not affect the development of the embryo.

It was found that Panavir has minor anti-inflammatory and analgesic effects.

For herpes, injections with Panavir accelerate the body's regenerative capabilities.

This promotes the rapid formation of crusts and healing of herpetic eruptions.

Intravenous antiherpetic agents, such as Panavir, are intended for slow bolus administration.

The drug is not recommended to be mixed with other antiviral agents.

Adult patients with a herpetic infection are prescribed 5 ml of medication.

The drug is administered every 24 or 48 hours.

Depending on the patient’s condition and how acute the infectious process is.

If necessary, the course can be repeated after 4-6 weeks.

Allokin: injections for herpes

Allokin-Alpha is an antiviral drug with proven effectiveness against hepatitis B, C, herpes infection and HPV.

The main active ingredient of the drug is alloferon.

Alloferon is a peptide with 13 amino acids.

Isolated from bacteria-infected larvae of the moth fly Calliphora vicina.

The pharmaceutical value of the peptide has been well demonstrated by its ability to stimulate NK and interferon (IFN) cytotoxic activity in animal and human models.

In addition, the peptide proved to be an enhancer of antiviral and antitumor activity.

The antiviral and immunomodulatory effectiveness of alloferon has also been confirmed clinically.

In patients suffering from herpes simplex viruses (HSV) and human papillomavirus (HPV).

The drug is a low-toxic drug, well tolerated, and does not provoke the development of an allergic reaction.

Also, Allokin does not cause problems with the reproductive system.

Allokin injections showed good therapeutic results for the diagnosis of herpes zoster.

The medication is available in powder form for preparing a solution.

The product must be used immediately; it must not be stored in prepared form.

Allokin injections for herpes are usually used according to the following scheme: 1 ml of the drug is administered every 48 hours.

The total number of injections is no more than 3.

Injections with Allokin can be used against intimate zone herpes and HPV.

In case of an acute infectious process, the number of injections can be increased to 6.

The drug should be stored in the refrigerator, in powder form, for no more than two years from the date of production.

Acyclovir tablets: instructions for use

The instructions for use on Acyclovir tablets contain information that these are prescription drugs, i.e. They should be used in children and adults only as prescribed by a doctor. Let's look at the indications for use.

Indications for use –

• treatment of infections caused by the herpes simplex virus (herpes of the lips and facial skin, genital herpes),
• prevention of infections caused by the herpes simplex virus in patients with immunodeficiency,
• treatment of chickenpox (chickenpox),
• treatment of herpes zoster,
• prevention of cytomegalovirus infection (during bone marrow transplantation).

We have already said above that taking the drug will be effective if you start taking it - either in the prodromal period (i.e. when there are no actual herpetic vesicles yet, but there is already itching or burning), or in the first 12 hours from the moment of appearance rashes. Moderate effectiveness can be achieved with a later dose, but no later than 72 hours from the moment the rash appears. If the herpetic blisters have already opened, taking acyclovir will no longer reduce the severity of symptoms and will not speed up healing.

A very important question is the dosage of acyclovir when taken orally. Very often in the instructions you can find information that in children over 2 years of age and adults, the standard dosage is used to treat herpes - 200 mg 5 times a day, for 5 days. Clinical studies (source) show that this dosage regimen has no effect at all - neither on the duration of the disease, nor on the healing time of ulcerations that form at the site of opened herpetic vesicles.

Acyclovir tablets: instructions for use adults for herpetic lesions of the lips, facial skin and herpetic stomatitis in children over 2 years of age and adults - you need to take 400 mg 5 times a day, for 5 days (we explained above why this particular dosage). How to take acyclovir in children under 2 years of age and infants - the dosage is reduced by 2 times, i.e. An effective dosage regimen would be 200 mg 5 times a day for 5 days. If necessary and with the recommendation of a doctor, taking the drug can be extended up to 10 days.

Acyclovir for chickenpox -

For the treatment of chickenpox (chickenpox) in children and adults over 6 years of age, the dosage of acyclovir is 800 mg 5 times a day, and in children from 3 to 6 years old - 400 mg 5 times a day. Thus, the drug must be taken every 4 hours, except during night sleep. The duration of treatment is 7 days.

What drugs to choose -

Reviews for acyclovir tablets are more positive when using the original acyclovir from GlaxoSmithKline (UK). The drug is called Zovirax tablets 200 mg, and the cost of 1 package of 25 tablets will be about 260 rubles. Thus, taking into account the optimal single dosage of 400 mg, which is 2 tablets per dose, you will need 2 packages of the drug for a 5-day course of treatment. An alternative option is Acyclovir Akrikhin tablets of 200 or 400 mg (Russian production), which will cost from 70 rubles and from 200 rubles, respectively.

• Zovirax tablets instructions for use (view PDF)
• Acyclovir tablets instructions for use 200 mg (view PDF)
• Acyclovir tablets instructions 400 mg (view PDF)

Acyclovir lyophilisate d/ra d/inf 500 mg vial No. 1

Compound

Active substance
: acyclovir 0.25 g, 0.5 g, 1.0 g,
excipient
: sodium hydroxide.

Pharmacokinetics

Suction

In adults, the maximum steady-state concentrations (Cssmax) of acyclovir after a one-hour infusion at a dose of 2.5 mg/kg, 5 mg/kg, 10 mg/kg and 15 mg/kg were 22.7 μmol/L (5.1 μg/ml) , 43.6 µmol/L (9.8 µg/ml), 92 µmol/L (20.7 µg/ml) and 105 µmol/L (23.6 µg/ml), respectively. The minimum equilibrium concentrations of acyclovir in plasma (Cssmin) 7 hours after infusions were respectively 2.2 µmol/l (0.5 µg/ml), 3.1 µmol/l (0.7 µg/ml), 10.2 µmol /l (2.3 μg/ml) and 8.8 μmol/l (2.0 μg/ml). In children over 1 year of age, comparable Cssmax and Cssmin were observed when administered at a dose of 250 mg/m2 equivalent to 5 mg/kg (adult dose) and at a dose of 500 mg/m2 equivalent to 10 mg/kg (adult dose). In neonates (0 to 3 months) who received acyclovir infusions of 10 mg/kg over more than one hour every 8 hours, Cssmax was 61.2 µmol/L (13.8 µg/ml), and Cssmin - 10.1 µmol/l (2.3 µg/ml).

Distribution

The concentration of acyclovir in the cerebrospinal fluid is approximately 50% of its concentration in plasma.

Acyclovir binds to plasma proteins to a small extent (9-33%), so drug interactions due to displacement from plasma protein binding sites are unlikely.

Removal

In adults, after intravenous administration of acyclovir, the plasma half-life is about 2.9 hours. Most of the acyclovir is excreted unchanged by the kidneys. The renal clearance of acyclovir significantly exceeds the clearance of creatinine, which indicates that acyclovir is eliminated through not only glomerular filtration, but also tubular secretion. The main metabolite of acyclovir is 9-carboxymethoxymethylguanine, which accounts for about 10 - 15 %

from the administered dose of the drug. When acyclovir was administered 1 hour after taking 1 g of probenecid, the half-life of acyclovir and AUC (area under the concentration-time curve) increased by 18 and 40%, respectively.

Special patient groups

In elderly people, the clearance of acyclovir decreases with age in parallel with a decrease in creatinine clearance, but the half-life of acyclovir changes slightly.

In patients with chronic renal failure, the half-life of acyclovir averaged 19.5 hours; during hemodialysis, the average half-life of acyclovir was 5.7 hours, and plasma acyclovir concentrations decreased by approximately 60%.

Indications for use

— Primary and recurrent herpes of the mucous membranes and skin caused by HSV-1 and HSV-2 in people with immunodeficiency,

- initial manifestations of genital herpes in persons without immunodeficiency,

- encephalitis caused by the herpes simplex virus,

- infection caused by the herpes simplex virus in newborns,

- infection caused by the Varicella zoster virus in people with immunodeficiency.

Contraindications

Overdoses of the drug Acyclovir cause an increase in the concentration of serum creatinine, blood urea nitrogen and renal failure. Neurological symptoms include confusion, hallucinations, agitation, seizures and coma. Hemodialysis significantly enhances the removal of acyclovir from the blood, and is therefore indicated for an overdose of acyclovir.

Directions for use and doses

The drug is used only in a hospital setting.

Adults

In obese patients, dosages are recommended as in adults with normal body weight.

Treatment of infections caused by herpes simplex viruses (HSV, excluding herpes encephalitis) and varicella zoster virus (VZV)

Intravenous infusions at a dose of 5 mg/kg body weight every 8 hours.

Treatment and prevention of infections caused by HSV, VZV, and herpetic encephalitis in patients with immunodeficiency

Intravenous infusions at a dose of 10 mg/kg body weight every 8 hours with normal renal function.

Prevention of CMV infection during bone marrow transplantation

500 mg/m2 of body surface intravenously 3 times a day with an interval of 8 hours.

The duration of treatment is from 5 days before transplantation to 30 days after transplantation.

Special patient groups

Children

Doses of the drug

Acyclovir in children aged 3 months to 12 years is calculated depending on body surface area.

In newborns, doses are calculated depending on body weight. For infections caused by HSV, a dose of 10 mg/kg every 8 hours is recommended.

Treatment of infections caused by HSV (except herpetic encephalitis) and VZV

Intravenous infusions at a dose of 250 mg/m2 every 8 hours.

Treatment of herpetic encephalitis and VZV infections in children with immunodeficiency

Intravenous infusions at a dose of 500 mg/m2 every 8 hours with normal renal function.

Prevention of CMV infection in children over 2 years of age

Limited data suggest that children over 2 years of age who have undergone bone marrow transplantation may be given an adult dose of Acyclovir.

In children with reduced renal function, dose adjustment is required according to the degree of renal failure.

Elderly patients

In the elderly, the clearance of acyclovir in the body decreases in parallel with a decrease in creatinine clearance. In elderly patients with reduced creatinine clearance, a dose reduction should be considered.

Patients with kidney failure

Intravenous infusions of Acyclovir should be administered with caution in patients with renal failure. The following dose adjustment scheme has been proposed depending on the degree of decrease in creatinine clearance:

The course of treatment with Acyclovir in the form of intravenous infusion is usually 5 days, but may vary depending on the patient's condition and response to therapy. The duration of treatment for herpetic encephalitis and HSV infections in newborns is usually 10 days.

The duration of prophylactic use of the drug Acyclovir for intravenous infusion is determined by the duration of the period when there is a risk of infection.

Preparation of solution and method of administration

The recommended dose of Acyclovir should be administered as a slow intravenous infusion over 1 hour.

Use 10 ml of dilution solution (water for injection or sodium chloride solution for injection (0.9%)) to prepare a solution of the drug Acyclovir containing 25 mg of acyclovir in 1 ml of the resulting solution. The recommended volume of dilution solution must be added to the bottle with Acyclovir powder and shaken carefully until the contents of the bottle are completely dissolved.

After dilution, the Acyclovir drug solution can be administered as an intravenous infusion using a special infusion pump that regulates the rate of drug administration.

Another method of infusion administration is possible, when the prepared solution is diluted further to obtain an acyclovir concentration not exceeding 5 mg/ml (0.5%).

To do this, you need to add the prepared solution to the selected infusion solution, which is recommended below, and shake well until the solutions are completely mixed.

For children and newborns who need to administer minimal volumes of infusion, it is recommended to add 4 ml of the prepared solution of the drug Acyclovir (100 mg of acyclovir) to 20 ml of solvent.

For adults, it is recommended to use infusion solutions in 100 ml packs, even if this will give an acyclovir concentration significantly lower than 0.5%. Thus, one 100 ml infusion solution can be used for any dose of acyclovir between 250 mg and 500 mg (10 and 20 ml diluted solution). For doses between 500 and 1000 mg of acyclovir, another infusion solution of the same volume (100 ml) should be used.

Acyclovir is compatible with the following infusion solutions and, when diluted with them, remains stable for 12 hours at room temperature (15 to 25 C):

— Sodium chloride for intravenous infusion (0.45% and 0.9%),

— Sodium chloride (0.18%) and dextrose (4%) for intravenous infusion,

— Sodium chloride (0.45%) and dextrose (2.5%) for intravenous infusion,

- Hartmann's solution.

When preparing Acyclovir solution for infusion, as indicated above, the concentration of Acyclovir is no more than 0.5%.

Dissolution and dilution must be carried out completely under aseptic conditions immediately before administration of the drug. Unused solution is discarded. If the solution becomes cloudy or crystals fall out, it should be destroyed.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 C.

Keep out of the reach of children.

Best before date

3 years.

Do not use after the expiration date stated on the package.

special instructions

In case of renal failure, the dose of Acyclovir should be adjusted in accordance with its degree in order to prevent the accumulation of acyclovir in the body.

In patients receiving high doses of Acyclovir for herpetic encephalitis, it is necessary to monitor renal function, especially if it is initially impaired or there is dehydration.

The prepared solution of the drug Acyclovir has a pH of 11.0, so it cannot be used orally.

Description

A porous mass of white or white with a yellowish tint, compacted into a tablet.

Conditions for dispensing from pharmacies

On prescription

Dosage form

lyophilisate for the preparation of solution for infusion

Pharmacodynamics

Mechanism of action

Acyclovir is a synthetic purine nucleoside analogue that has the ability to inhibit in vitro

and
in vivo
human herpes viruses, including herpes simplex virus (HSV) types 1 and 2, varicella zoster virus (VZV), Epstein-Barr virus (EBV), and cytomegalovirus (CMV). In cell culture, acyclovir has the most pronounced antiviral activity against HSV-1, followed in descending order of activity by: HSV-2, VZV (Varicella zoster virus), EBV and CMV.

The effect of acyclovir on herpes viruses (HSV-1, HSV-2, VZV, EBV, CMV) is highly selective. Acyclovir is not a substrate for the thymidine kinase enzyme in uninfected cells, therefore acyclovir is of low toxicity to mammalian cells. Thymidine kinase of cells infected with HSV, VZV, EBV and CMV viruses converts acyclovir into acyclovir monophosphate, a nucleoside analogue, which is then sequentially converted into diphosphate and triphosphate under the action of cellular enzymes. The incorporation of acyclovir triphosphate into the viral DNA chain and subsequent chain termination block further replication of the viral DNA.

In patients with severe immunodeficiency, long-term or repeated courses of acyclovir therapy may lead to the emergence of resistant strains, so further treatment with acyclovir may be ineffective. The majority of isolated strains with reduced sensitivity to acyclovir had a relatively low content of viral thymidine kinase and a disorder in the structure of the viral thymidine kinase or DNA polymerase. Effect of acyclovir on herpes simplex virus (HSV) strains in vitro

can also lead to the formation of strains less sensitive to it.
A correlation has not been established between the sensitivity of herpes simplex virus (HSV) strains to acyclovir in vitro
and the clinical effectiveness of the drug.

Side effects

The adverse events presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. Frequency of occurrence is defined as follows: very often

(>.1/10),
often
(>.1/100 and <.1/10),
infrequently
(>.1/1000 and <.1/100
), rarely
(>.1/10000 and <.1/ 1000),
very rare
(<.1/10000, including isolated cases).

Frequency of occurrence of adverse events

From the blood and lymphatic system:

infrequently - a decrease in the content of blood cells (anemia, leukocytosis, neutropenia or neutrophilia, thrombocytopenia or thrombocytosis), rarely - lymphadenopathy, disseminated intravascular coagulation syndrome, hemolysis.

From the central nervous system:

rarely - headache, dizziness, drowsiness, agitation, confusion; very rarely - visual impairment, ataxia, dysarthria, mental disorders (including delirium), depression or psychosis, signs of encephalopathy (coma, confusion, hallucinations, convulsions, tremors). The above phenomena were usually observed in patients with impaired renal function and other predisposing factors and, as a rule, were reversible.

From the respiratory system:

very rarely - shortness of breath.

From the gastrointestinal tract: often -

loss of appetite, nausea, vomiting, infrequently - diarrhea, abdominal pain.

From the liver and biliary tract:

often - a reversible increase in the activity of liver transaminases, very rarely - a reversible increase in the concentration of bilirubin, jaundice, hepatitis.

From the kidneys and urinary tract:

often - increased concentrations of urea and creatinine in the blood, rarely - hematuria, hypercreatininemia (due to obstruction of the renal tubules), very rarely - impaired renal function, acute renal failure, pain in the projection of the kidneys. These complications depend on the maximum plasma concentration of the drug and the state of the patient’s water-electrolyte balance. To avoid such phenomena, it should be administered within 1 hour. Pain in the projection of the kidneys may be associated with impaired renal function. The fluid and electrolyte balance of patients should be maintained. Renal failure that develops during treatment with Acyclovir usually resolves quickly when patients are rehydrated and/or the dose of the drug is reduced or discontinued. Progression to acute renal failure occurs in extremely rare cases.

Local reactions:

often - phlebitis or inflammation at the injection site, peripheral edema, general weakness, very rarely - fever, local inflammatory reactions.

Anaphylactic reactions:

rarely - allergic skin reactions (itching, rash, urticaria), very rarely - Lyell's syndrome, exudative erythema multiforme, incl. Stevens-Johnson syndrome).

Use during pregnancy and breastfeeding

Acyclovir crosses the placental barrier and accumulates in breast milk. The use of the drug during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to take acyclovir during lactation, interruption of breastfeeding is required.

Interaction

When mixing solutions, it is necessary to take into account the alkaline reaction of acyclovir for intravenous administration (pH 11).

An enhanced effect is observed with the simultaneous administration of immunostimulants.

Tubular secretion blockers reduce the tubular secretion of intravenously administered acyclovir, which can lead to an increase in the concentration of acyclovir in the blood serum and cerebrospinal fluid (CSF), a slowdown in the elimination of acyclovir (increased half-life) from the blood and CSF, and increased toxic effects.

Other nephrotoxic drugs - increase the risk of nephrotoxicity from acyclovir.

Acyclovir is excreted unchanged through the kidneys by active tubular secretion. All drugs with a similar route of elimination may increase plasma concentrations of acyclovir. Thus, probenecid and cimetidine increase the AUC of acyclovir and reduce its renal clearance. However, no dose adjustment is required due to the wide range of therapeutic doses of acyclovir. In patients receiving Acyclovir, caution is required when prescribing drugs that compete for the elimination pathway due to the potential for increased plasma concentrations of one, both drugs, or their metabolites. The combined use of acyclovir and mycophenolate mofetil (an immunosuppressive drug) used in organ transplantation leads to an increase in the AUC for acyclovir and the inactive metabolite mycophenolate mofetil.

Overdose

Overdoses of the drug Acyclovir cause an increase in the concentration of serum creatinine, blood urea nitrogen and renal failure. Neurological symptoms include confusion, hallucinations, agitation, seizures and coma. Hemodialysis significantly enhances the removal of acyclovir from the blood, and is therefore indicated for an overdose of acyclovir.

Impact on the ability to drive vehicles and operate machinery

The drug Acyclovir is intended for use only in a hospital setting, therefore there is no data on the effect of the drug on the ability to drive a car and/or other mechanisms.

Acyclovir: price for 2022

The price of the drug acyclovir in 2022 has not increased compared to previous years, which is most likely due to high competition between manufacturers, as well as the appearance in pharmacies of a large number of more modern and effective analogues of acyclovir. The highest price is the original Acyclovir from GlaxoSmithKline (UK), sold under the Zovirax brand.

Ointment and cream Acyclovir 5% –

• Acyclovir-Acri ointment, 5 g – from 35 rubles,
• Acyclovir-Belupo cream, 5 g – from 70 rubles,
• Acyclovir-Sandoz cream, 5 g – from 150 rubles (2 g tube – from 75 rubles),
• Zovirax cream, 5 g – from 190 rub.
• Zovirax Duo-Active cream, 2 g – from 350 to 400 rubles.

Please note that all of the above products contain propylene glycol (to enhance the penetration of acyclovir into tissues). However, despite this, the ointment will in any case be inferior in effectiveness to the cream. The second point is that only Acyclovir-Sandoz cream and both Zovirax creams contain dimethicone, which will allow you to easily apply cosmetics over the absorbed cream.

Eye ointment Acyclovir 3% –

• Acyclovir-Sintez (Russia) – from 150 rubles,
• Acyclovir-Akos (Russia) – from 150 rubles,
• Zovirax 3% (UK) – from 240 rubles.

Acyclovir tablets: price

• Zovirax 200 mg (25 tablets) – from 250 rubles,
• Acyclovir Acri 200 mg (20 tablets) – from 70 rubles,
• Acyclovir Acri 400 mg (20 tablets) – from 220 rubles.

Ointment, cream, tablets Acyclovir: reviews

Acyclovir is one of the first antiviral drugs.
Of course, this is not the best antiherpetic drug, but in principle it works well in children, as well as in adults who have not received long-term regular treatment with acyclovir in the past (especially against the background of reduced immunity, since in this case one can expect the development of virus resistance herpes to acyclovir). In addition, for Acyclovir tablets, reviews will be good only if you start taking them early (the same applies to ointment and cream forms). Clinical studies have shown that the best treatment results are achieved when patients begin to use acyclovir, either in the prodromal period or in the first 12 hours from the onset of herpetic eruptions.

It makes sense to start using acyclovir cream or ointment only during the first 48 hours from the moment of illness, until the herpetic blisters burst (after this point, use will no longer speed up recovery). As for tablets with acyclovir, you can start using them no later than 72 hours, but you need to keep in mind that the later you start taking them by the end of this period, the less the result of treatment will be.

The main disadvantages of the drug Acyclovir are:

1) Low bioavailability of the drug - it is only 10 to 20% of the amount taken. In this regard, Acyclovir must be taken 5 times a day, which is not very convenient (this applies to both tablet forms and forms in the form of an ointment or cream). Valacyclovir and famciclovir have a bioavailability of 50 to 74%, which is why they usually need to be used only 2 times a day.

2) Poor penetration into the skin - products in the form of ointments or creams for external use have a significant drawback, which is that acyclovir does not penetrate very well through the most superficial layer of the skin (the stratum corneum of the epidermis). This certainly reduces the effectiveness of the drug. Some manufacturers, in order to increase the permeability of acyclovir, add propylene glycol to the ointment or cream.

3) Low tropism of acyclovir to the virus - acyclovir equally penetrates both healthy and cells infected with the herpes virus. If there is a “viral thymidine kinase” (enzyme) in the cell, acyclovir is activated and blocks the reproduction of the virus. However, the problem is that acyclovir has low tropism for viral thymidine kinase, so it may not find it in infected cells. Accordingly, in this case it simply does not convert into the active form of acyclovir-3-phosphate, which blocks the reproduction of the herpes virus.

4) Resistance to the drug - compared to all other modern antiviral drugs - resistance to the herpes virus most often occurs to acyclovir. According to statistics, in people with weakened immune systems, resistance occurs in 7-10% of cases, and in some groups of patients with immunodeficiency conditions it even reaches 27% or more of cases.

5) Intracellular half-life - acyclovir has a very short intracellular half-life (about 1 hour), which leads to a complete cessation of blocking viral replication - immediately after taking the drug. For example, the antiviral drug Penciclovir has a longer intracellular half-life (up to 20 hours), which ensures sufficient clinical antiviral effectiveness for up to 2 days after discontinuation of the drug.

Below you will find information about modern analogues of Acyclovir.

Acyclovir J

Treatment of infections caused by herpes simplex virus (HSV)

Acyclovir J should be administered as a slow intravenous infusion over 1 hour.

The course of treatment with Acyclovir J, lyophilisate for solution for infusion, is usually 5 days, but may vary depending on the patient's condition and response to therapy. The duration of treatment for herpetic encephalitis is usually 10 days.

The duration of treatment for herpes in newborns is usually 14 days in the case of infection of the skin and mucous membranes (eyes, mouth) and 21 days in the case of disseminated lesions or damage to the central nervous system.

Adults

For obese patients, calculating the dose of intravenous acyclovir based on actual body weight may result in higher plasma acyclovir concentrations. Therefore, the need to reduce the dose should be considered in obese patients, especially in elderly patients or with impaired renal function.

Patients with infection caused by HSV (except herpetic encephalitis) are prescribed Acyclovir J, a lyophilisate for the preparation of a solution for infusion, at a dose of 5 mg/kg body weight every 8 hours, provided there is no impairment of renal function.

Patients with herpetic encephalitis are prescribed the drug Acyclovir J, a lyophilisate for the preparation of a solution for infusion, at a dose of 10 mg/kg body weight every 8 hours, provided there is no impairment of renal function.

Children from 12 to 18 years old

In children aged 12 to 18 years, the drug Acyclovir J, lyophilisate for the preparation of solution for infusion, should be used in the dosage regimen indicated for adults.

Children from 3 months to 12 years

The dose calculation of Acyclovir J, lyophilisate for preparing a solution for infusion, in children aged 3 months to 12 years is carried out depending on the body surface area.

Children from 3 months to 12 years with an infection caused by HSV (except herpetic encephalitis) are prescribed the drug Acyclovir J, a lyophilisate for the preparation of a solution for infusion, at a dose of 250 mg/m2 of body surface every 8 hours, provided there is no impairment of renal function.

Children from 3 months to 12 years with herpetic encephalitis are prescribed the drug Acyclovir J, a lyophilisate for the preparation of a solution for infusion, at a dose of 500 mg/m2 of body surface every 8 hours, provided there is no impairment of renal function.

In children with reduced renal function, dose adjustment is required according to the degree of renal impairment.

Children from 29 days of life to 3 months

In children aged 29 days to 3 months, the drug Acyclovir J, lyophilisate for the preparation of solution for infusion, should be used in the dosage regimen indicated for newborns.

Newborns (children up to 28 days of life inclusive)

In newborns, doses are determined depending on body weight.

The recommended dose of the drug Acyclovir J, lyophilisate for the preparation of a solution for infusion, for newborns with herpes or suspected herpes is 20 mg/kg body weight every 8 hours for 21 days in the case of disseminated lesions and damage to the central nervous system or for 14 days in the case of disease , limited to damage to the skin and mucous membranes. For patients with reduced renal function, the prescribed dose should be adjusted according to the degree of renal impairment.

Elderly patients

The possibility of renal impairment in elderly patients must be taken into account, and doses should be adjusted according to the degree of renal impairment.

Adequate levels of body hydration should be maintained.

Patients with impaired renal function

Acyclovir J, a lyophilisate for solution for infusion, should be administered with caution to patients with reduced renal function.

Adequate levels of body hydration should be maintained.

Dose adjustment for patients with impaired renal function is based on creatinine clearance, which for adults and children over 12 years of age is presented in units of ml/min, for newborns, children from 29 days of life to 3 months, children from 3 months to 12 years - ml /min/1.73 m2.

Dose adjustment schemes:

Table 1. Dose adjustment scheme for the treatment of infections caused by HSV for children over 12 years of age and adults with impaired renal function

Table 2. Dose adjustment scheme for the treatment of infections caused by HSV in newborns, children from the 29th day of life to 3 months, children from 3 months to 12 years with impaired renal function

Prevention of herpes simplex virus (HSV) infections in immunocompromised patients

Acyclovir J should be administered as a slow intravenous infusion over 1 hour.

The duration of prophylactic use of the drug Acyclovir J, lyophilisate for the preparation of solution for infusion, is determined by the duration of the period of risk of infection.

Adults

For obese patients, calculating the dose of intravenous acyclovir based on actual body weight may result in higher plasma acyclovir concentrations. Therefore, the need to reduce the dose should be considered in obese patients, especially in elderly patients or with impaired renal function. Treatment regimens are the same as for the treatment of infections caused by HSV.

Children from 12 to 18 years old

In children aged 12 to 18 years, the drug Acyclovir J, lyophilisate for the preparation of solution for infusion, should be used in the dosage regimen indicated for adults.

Children from 3 months to 12 years

The dose calculation of Acyclovir J, lyophilisate for preparing a solution for infusion, in children aged 3 months to 12 years is carried out depending on the body surface area.

Treatment regimens are the same as for the treatment of infections caused by HSV.

In children from 3 months to 12 years with reduced renal function, dose adjustment is required according to the degree of renal impairment.

Elderly patients

It is necessary to take into account the likelihood of renal impairment in elderly patients, the dose of the drug should be adjusted in accordance with the degree of renal impairment.

Adequate levels of body hydration should be maintained.

Patients with impaired renal function

Acyclovir J, a lyophilisate for solution for infusion, should be administered with caution to patients with impaired renal function.

Adequate levels of body hydration should be maintained.

The dose for patients with impaired renal function should be adjusted according to Table 1 or 2.

Treatment of infections caused by the varicella zoster virus (VZV, Varicella zoster virus),

including chickenpox and herpes zoster

Acyclovir J should be administered as a slow intravenous infusion over 1 hour.

The course of treatment with Acyclovir J, lyophilisate for solution for infusion, is usually 5 days, but may vary depending on the patient's condition and response to therapy.

Adults

For obese patients, calculating the dose of intravenous acyclovir based on actual body weight may result in higher plasma acyclovir concentrations. Therefore, the need to reduce the dose should be considered in obese patients, especially in elderly patients or with impaired renal function.

Patients with VZV infections are prescribed Acyclovir J, a lyophilisate for solution for infusion, at a dose of 5 mg/kg body weight every 8 hours, provided there is no impairment of renal function.

Patients with immunodeficiency and infections caused by VZV are prescribed the drug Acyclovir J, a lyophilisate for the preparation of a solution for infusion, at a dose of 10 mg/kg body weight every 8 hours, provided there is no impairment of renal function.

Children from 12 to 18 years old

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children aged 12 to 18 years, the drug Acyclovir J, lyophilisate for the preparation of solution for infusion, should be used in the dosage regimen indicated for adults.

Children from 3 months to 12 years

The dose calculation of Acyclovir J, lyophilisate for preparing a solution for infusion, in children aged 3 months to 12 years is carried out depending on the body surface area.

Children from 3 months to 12 years with infection caused by VZV are prescribed the drug Acyclovir J, a lyophilisate for the preparation of a solution for infusion, at a dose of 250 mg/m2 of body surface every 8 hours, provided there is no impairment of renal function.

Children from 3 months to 12 years with immunodeficiency and infections caused by VZV are prescribed the drug Acyclovir J, a lyophilisate for the preparation of a solution for infusion, at a dose of 500 mg/m2 of body surface every 8 hours, provided there is no impairment of renal function.

Children from 3 months to 12 years with impaired renal function require dose adjustment in accordance with the degree of impaired renal function (see Table 2).

Elderly patients

The possibility of renal impairment in elderly patients must be taken into account, and the dose should be adjusted according to the degree of renal impairment.

Adequate levels of body hydration should be maintained.

Patients with impaired renal function

Acyclovir J, a lyophilisate for solution for infusion, should be administered with caution to patients with impaired renal function.

Adequate levels of body hydration should be maintained.

Doses in patients with impaired renal function should be adjusted according to Table 1 or 2.

Prevention of cytomegalovirus (CMV) infection in bone marrow transplant recipients

Acyclovir J should be administered as a slow intravenous infusion over 1 hour.

The duration of prophylactic use of the drug Acyclovir J, lyophilisate for the preparation of solution for infusion, is determined by the duration of the period of risk of infection.

Adults

For obese patients, calculating the dose of intravenous acyclovir based on actual body weight may result in higher plasma acyclovir concentrations. Therefore, the need to reduce the dose should be considered in obese patients, especially in elderly patients or with impaired renal function. For the prevention of CMV in bone marrow transplant recipients, the drug Acyclovir J, a lyophilisate for the preparation of a solution for infusion, is prescribed at a dose of 500 mg/m2 of body surface intravenously 3 times a day with an interval of 8 hours, provided there is no impairment of renal function. The duration of treatment is from 5 days before transplantation to 30 days after transplantation.

Children from 12 to 18 years old

In children aged 12 to 18 years, the drug Acyclovir J, lyophilisate for the preparation of solution for infusion, should be used in the dosage regimen indicated for adults.

Children from 3 months to 12 years

The dose calculation of Acyclovir J, lyophilisate for preparing a solution for infusion, in children aged 3 months to 12 years is carried out depending on the body surface area.

Limited data suggest that in children over 2 years of age who have undergone bone marrow transplantation, the dose indicated for adults can be used to prevent CMV infection.

In children from 3 months to 12 years with impaired renal function, dose adjustment is required in accordance with the degree of impaired renal function.

Elderly patients

The possibility of renal impairment in elderly patients must be taken into account, and the dose should be adjusted according to the degree of renal impairment.

Adequate levels of body hydration should be maintained.

Patients with impaired renal function

Acyclovir J, a lyophilisate for solution for infusion, should be administered with caution to patients with impaired renal function.

Adequate levels of body hydration should be maintained.

Doses in patients with impaired renal function should be calculated according to Table 3 for children from 12 years of age and adults and Table 4 for children from 3 months to 12 years.

Table 3. Dose adjustment scheme for the prevention of CMV infection for children over 12 years of age and adults with impaired renal function

Table 4. Dose adjustment scheme for the prevention of CMV infection for children from 3 months to 12 years with impaired renal function

Preparation of solution and method of administration

The recommended dose of Acyclovir J should be administered as a slow intravenous infusion over 1 hour.

To prepare a solution for infusion, the contents of the bottle with Acyclovir J are restored by adding water for injection or sodium chloride solution for injection (0.9%) to obtain a solution containing 25 mg of acyclovir in 1 ml.

The volume of infusion solution indicated in the table must be added to the bottle with the appropriate amount of lyophilisate of the drug Acyclovir J and shaken carefully until the contents of the bottle are completely dissolved.

After dilution, the solution of the drug Acyclovir J can be administered as an intravenous infusion using a special infusion pump that regulates the rate of administration.

As an alternative method of preparation, the reconstituted solution of Acyclovir J is further diluted to obtain an acyclovir concentration not exceeding 5 mg/ml (0.5%).

To do this, you need to add the reconstituted solution of the drug to the selected infusion solution (options for recommended infusion solutions are given below) and shake well until completely mixed.

For children and newborns who need to administer minimal volumes of infusions, it is recommended to add 4 ml of a reconstituted solution of Acyclovir J (100 mg of acyclovir) to 20 ml of infusion solution when diluting.

For adults, it is recommended to use infusion solutions in 100 ml packages, even if the concentration of acyclovir is significantly lower than 0.5%. Thus, one package of 100 ml infusion solution can be used for any dose of acyclovir from 250 mg to 500 mg (10 and 20 ml of reconstituted solution). For doses from 500 mg to 1000 mg of acyclovir, two packages of infusion solution of this volume (100 ml) must be used.

With the specified dilution method, Acyclovir J, lyophilisate for solution for infusion, is compatible with the following infusion solutions and remains stable for up to 12 hours at room temperature (15 to 25 °C):

- sodium chloride for intravenous infusion (0.45% and 0.9%);

- sodium chloride (0.18%) and dextrose (4%) for intravenous infusion;

- sodium chloride (0.45%) and dextrose (2.5%) for intravenous infusion;

- Hartmann's solution.

When preparing Acyclovir J solution for infusion according to the scheme indicated above, the concentration of acyclovir is no more than 0.5%.

When reconstituted as recommended, the pH of Acyclovir J solution for infusion is approximately 11.

Reconstitution and dilution must be carried out under completely aseptic conditions immediately before administration of the drug, since the drug does not contain antimicrobial preservatives. Unused solution is discarded.

Reconstituted and diluted solutions should not be frozen.

If the solution becomes cloudy or crystals appear before or during infusion, the solution should be discarded.

Contraindications to Acyclovir and features of its use -

The drug should not be taken if you are hypersensitive to acyclovir or valacyclovir. Do not use the intravenous route of administration of the drug during breastfeeding. The drug should also not be used in cases of severe renal impairment. Forms of the drug for external use (creams and ointments) cannot be used to treat the mucous membranes of the mouth, eyes, and vagina.

Acyclovir is not effective against influenza and ARVI, because it has no effect on these types of viruses at all. The drug is prescribed with great caution for dehydration and renal failure. When taking tablets, they should be washed down with a full glass of water (regardless of meals, since simultaneous food intake does not affect the absorption of the drug in the intestines). Acyclovir and alcohol: the compatibility of taking antibacterial and antiviral drugs with alcohol consumption reduces the effectiveness of treatment.

Important: taking acyclovir has nuances that are important for patients with gastrointestinal diseases. For diseases that occur with impaired absorption in the gastrointestinal tract, it is necessary to either increase the dosage of acyclovir, or (optimally) switch to intravenous administration of the drug.

Acyclovir during pregnancy and breastfeeding -

Acyclovir tablets during pregnancy can only be used as directed and under the supervision of a physician. The drug can be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus. But acyclovir ointment or cream during pregnancy (i.e. forms for external use) can be used without a doctor’s prescription.

When breastfeeding - there are no contraindications for using Acyclovir cream or ointment during lactation, i.e. You can use such drugs without a doctor’s recommendation. But with the exception of the drug Acyclovir Duo-Active, which in addition to acyclovir also contains 1% hydrocortisone (here it is advisable to obtain a doctor’s permission).

Acyclovir tablets can be used during breastfeeding, but only as prescribed by a doctor (and here you need to pay attention to some details). For example, according to the instructions, the original drug with acyclovir - Zovirax 200 mg tablets - can be used during breastfeeding, but the Russian tablets Acyclovir-Akrikhin cannot be used in nursing according to the instructions.

There are clinical studies that show that when a breastfeeding woman uses high dosages of tableted acyclovir, the dosage of acyclovir contained in breast milk will be only about 1% of the standard pediatric dosage taken for children (source). This is due to the fact that the baby receives acyclovir orally in breast milk, and acyclovir, in turn, has low bioavailability (only 10 to 20% of the total volume of the drug enters the blood from the intestines). In principle, this should prevent any negative side effects from occurring in breastfed babies, but you should still get a doctor's prescription.

Doses and method of administration

Dosage of the drug Acyclovir

Dosage

The dosage depends on the disease and the severity of its course.

• Hepatic infection of the skin and mucous membranes involves prescribing 200 mg of medication to children and adults 5 times a day at an interval of 4 hours, interrupted by sleep (8 hours). Duration of therapy – 5 days.
• When preventing influenza or ARVI, Acyclovir is prescribed 4 times a day, 200 mg every 6 hours.
• As a complex therapy for severe immunodeficiency, the drug is taken at a dose of 400 mg 5 times a day.
• Chickenpox in children and adults whose body weight exceeds 40 kg requires taking the medicine 800 mg 5 times a day. Children over 2 years of age with a body weight below 40 kg take the drug at a rate of 20 mg per kilogram of weight 4 times a day for 5 days.
• Treatment of herpes zoster involves taking Acyclovir for children over 6 years of age and adults, 800 mg every 6 hours for 5 days. Children from 2 to 6 years old take the medicine 400 mg 4 times a day, and children under 2 years old receive it 4 times a day 200 mg.

How to use Acyclovir

The method of use of Acyclovir depends on the form of release. The tablets are swallowed without chewing, regardless of food intake, with plenty of water. Apply the ointment and cream using a cotton swab to the affected areas in a thin layer 5 times a day (every 4 hours plus a night break). The lyophilisate (intravenously) must first be diluted to the desired concentration. Eye ointment is applied in a 1 cm strip behind the lower eyelid 5 times a day after 4 hours.

Acyclovir ointment

Acyclovir ointment and cream are intended for external use, and application to the surface of the mucous membranes (nasal and oral cavities) is not recommended, but not contraindicated. It is necessary to remember some rules for applying medications to the mucous membrane and consult a doctor!

Herpetic rashes in the oral cavity are localized on the palate, inner sides of the cheeks and lips. As for the nasal cavity, herpes sores appear both in the vestibule of the nose - the thin skin inside the nose - and on the mucous membrane, which is located 1.5-2 cm from the edge of the nostril. If herpes appears on the lip or on the eve of the nose, then the application technique is the same as for the rest of the face and body - on cleansed skin 5 times a day, every 4 hours, with a break at night.

As for the mucous membranes of the mouth and nose, due to the fact that drool and mucus interfere with the penetration of the drug and, at the same time, contribute to the spreading of the ointment over the mucous membrane, which reduces the effectiveness of the drug, the most correct decision would be to switch to the tablet form of Acyclovir. Also, do not forget that the mucous membrane is a very thin tissue, which means that the development of allergic reactions is stronger and more pronounced.

Acyclovir cream

If the ointment still needs to be applied, then clean the oral or nasal cavities before using Acyclovir. It is advisable to rinse them with saline solution or other rinsing or rinsing agent, and then blot the surface with a gauze pad or cotton ball. Then apply a small amount of cream or ointment pointwise. There may be a burning sensation and pain. If they pass, then apply the remaining cream or ointment. If the pain intensifies, then this is an allergic reaction, and the use of the product must be stopped. Remember that the cream and ointment will enter the esophagus through the oral cavity; in small quantities this is not dangerous, but it is better to use another form of Acyclovir.

Acyclovir - modern analogues of the drug

Below we will talk about several of the most common tablet analogues of acyclovir, the effectiveness of which is higher, and the resistance of the herpes virus to these drugs is lower. In addition, they have a very convenient dosage regimen. Please note that all tablet drugs discussed below are prescription drugs and should be used only as prescribed by a doctor.

Valacyclovir –

Valacyclovir is a precursor substance to acyclovir, i.e. this drug is converted into acyclovir after it enters the body. The most famous drug in the world based on valacyclovir is Valtrex (manufactured by GlaxoSmithKline, UK).

Valacyclovir and Acyclovir: what is the difference? It is the higher bioavailability of valacyclovir compared to acyclovir - 50% instead of only 10-20%. This allows, when taking valacyclovir tablets, to create a very high concentration of acyclovir in the tissues, which, when taking the conventional drug Acyclovir, can only be achieved when administered intravenously. In addition, the high bioavailability of valacyclovir also makes it possible to reduce the frequency of dosing to just 2 times a day.

Dosage regimen - clinical studies have shown that taking high dosages of the drug for 1 day was most effective for the treatment of herpes on the lips, facial skin, and herpetic stomatitis. The dosage regimen is 2000 mg 2 times a day, with an interval of 12 hours (1 day in total), but this regimen is effective if treatment begins no later than 12 hours from the onset of herpetic rashes, and also if you have satisfactory or good immunity.

If more than 12 hours have passed, or you have a weakened immune system, it would be optimal to use the standard treatment regimen: 500 mg 2 times a day for 3-5 days (for severe herpes infection - up to 10 days).

Valaciclovir: price 2022 cost of the original drug “Valtrex” (UK) – from 1350 rubles for 10 tablets. 500 mg each. The drug Valvir (Bulgaria) - costs from 750 rubles per pack of 10 tablets. 500 mg each. The price for Valacyclovir-Akos, produced in Russia, starts from 450 rubles (for a package of 10 tablets of 500 mg). When choosing a drug, keep in mind that if your herpes virus is resistant to acyclovir, taking valacyclovir will also be ineffective.

Famciclovir (Favirox, Famvir) –

Famciclovir is the most effective remedy for herpes, and is a tablet form of penciclovir (penciclovir is also contained in Fenistil-Pentsivir cream for the treatment of herpes on the lips and facial skin). The bioavailability of the drug is about 77%, and the tropism of penciclovir to the virus is at least 2 times higher than that of acyclovir. All this makes famciclovir one of the most effective drugs. Experts consider it even more effective - even compared to valacyclovir.

Dosage regimen - for herpes of the lips, facial skin and herpetic stomatitis, this drug can also be taken for only 1 day. The most effective dosage regimen is 750 mg 2 times a day, with an interval of 12 hours (1 day in total). However, a single dose of 1500 mg of the drug is possible, although clinical studies have shown a slightly worse result of such therapy (compared to the previous regimen). It should be noted that such short regimens will be effective only if taking the drug begins no later than 12 hours from the moment the herpetic rash appears, and also if you do not have a weakened immune system.

If more time has passed, or you have a weak immune system, in this case herpes of the lips, facial skin and herpetic stomatitis are best treated using the traditional full treatment regimen for 5 days. Standard regimen: 250 mg 2 times a day, for 5 days (for severe herpes infection - up to 7-10 days). But I would like to add that numerous clinical studies have revealed the weak effectiveness of this regimen - especially in patients with a poor immune system.

Studies have shown that the effectiveness of therapy increases significantly if famciclovir is prescribed in higher dosages. In patients with good immunity, it is better to use the regimen - 500 mg 2 times a day (for 5 days), and in patients with weakened immunity - 500 mg 3 times a day (for 7 days).

Important: once again we draw your attention to the fact that short one-day treatment regimens for herpetic infections work well - 1) only if you start taking medications no later than 12 hours from the moment the herpetic rash appears, 2) if you have a more or less normal immune system. In patients with poor immunity, short courses of therapy are ineffective, even if treatment is started early. And therefore, in patients with weak immunity, standard full treatment regimens should always be used - preferably famciclovir.

Fenistil-Pentsivir cream –

The drug Fenistil-Pentsivir is the same famciclovir, but not in tablets, but in the form of a cream. Intended for the treatment of herpes on the lips and facial skin in adults and children over 12 years of age. The peculiarity of this cream is that it will be effective even if you do not start using it immediately from the moment the herpetic rash appears (but after a longer time).

For Fenistil-Pentsivir the price will be from 430 rubles (per tube of 2 g). After use, the drug still remaining in the cells will continue to have an antiviral effect for another 2 days. The only drawback is the frequency of application - 8 times a day for 4 days (at 2 hour intervals during the daytime).

But there is an excellent effect, and almost complete absence of the risk of herpes virus resistance to this drug. In addition, the drug contains cetomacrogol and propylene glycol, which facilitate the penetration of penciclovir into infected skin cells. We hope that our article on the topic “Acyclovir - price, instructions for use” was useful to you!

Sources:

1. Higher medical education of the author of the article, 2. National Library of Medicine (USA), 3. The National Center for Biotechnology Information (NCBI, USA), 4. “Modern approaches to the treatment of herpes (HSV) infections in adults” (Khokhlova N.I.), 5. Composition of drugs taken from the official websites of manufacturers.

Acyclovir lyophilisate for the preparation of solution for infusion 0.25 g

Description:

International nonproprietary name

Acyclovir.
Acyclovir.

Pharmacotherapeutic group

Antiviral drugs for systemic use. Acyclovir.

Compound

1 vial (bottle) contains 250 mg, 500 mg or 1000 mg of acyclovir.

ATX code:

J05AB01.

pharmachologic effect

Pharmacodynamics

Acyclovir highly selectively inhibits the replication process of herpes simplex virus types 1 and 2, herpes zoster virus (Varicella zoster), and Epstein-Barr virus. Cytomegalovirus is less sensitive to the action of acyclovir.

The molecular biological mechanism of the antiviral activity of acyclovir is due to competitive interaction with viral thymidine kinase and sequential phosphorylation with the formation of mono-, di- and triphosphate. Acyclovir triphosphate is incorporated instead of deoxyguanosine into the DNA of the virus, inhibits the latter's DNA polymerase and suppresses the replication process.

Pharmacokinetics

In adults, after a 1-hour infusion of acyclovir at doses of 2.5 mg/kg, 5 mg/kg and 10 mg/kg, Css max is 5.1 μg/ml, 9.8 μg/ml and 20.7 μg/ml, respectively. After 7 hours, the Css min value is 0.5 μg/ml, 0.7 μg/ml and 2.3 μg/ml, respectively.

In newborns and infants under 3 months of age, when acyclovir is administered at a dose of 10 mg/kg over one hour at 8-hour intervals, Css max is 13.8 mcg/ml, Css min is 2.3 mcg/ml.

Acyclovir penetrates the blood-brain and placental barriers. The concentration of acyclovir in cerebrospinal fluid is 50% of its concentration in plasma. Found in breast milk. Slightly binds to plasma proteins (9-33%). The main metabolite of acyclovir is 9-carboxymethoxymethylguanine.

In adults, following intravenous administration of acyclovir, the plasma half-life is approximately 2.9 hours. Most of the drug is excreted by the kidneys unchanged and in the form of 9-carboxymethoxymethylguanine (10-15%). The renal clearance of acyclovir significantly exceeds the clearance of creatinine, indicating elimination of the drug by glomerular filtration and tubular secretion. In elderly patients, the half-life of acyclovir increases slightly.

In patients with chronic renal failure, the half-life of acyclovir is 19.5 hours, in the case of hemodialysis - 5.37 hours (while the plasma concentration decreases to 60% of the initial value).

In children under 3 months of age, when the drug is administered intravenously at a dose of 10 mg/kg over 1 hour 3 times a day, the half-life is 3.8 hours.

Indications for use

The drug is used for severe forms of infections of the skin and mucous membranes caused by herpes simplex viruses type 1 or 2 (including genital and rectal herpes); for the prevention of infections of the skin and mucous membranes caused by herpes simplex viruses type 1 or 2 in patients with impaired immune system; as part of complex therapy for patients with severe immunodeficiency, incl. with an advanced clinical picture of HIV infection (CD4+ cell count less than 200/mm3), and in patients who have undergone bone marrow transplantation; for infections caused by herpes zoster and chickenpox viruses; for the prevention of cytomegalovirus infection after bone marrow transplantation.

Directions for use and dosage regimen

For adults, for the treatment of infections caused by the Herpes Simplex virus types 1 and 2 with severe immunodeficiency, including after bone marrow transplantation, or impaired absorption from the intestine, it is prescribed intravenously at a dose of 5 mg/kg 3 times a day with an interval of 8 hours.

For infections caused by Herpes simplex types 1 and 2 (with the exception of herpetic meningoencephalitis), administer intravenously at a dose of 5 mg/kg 3 times a day with an interval of 8 hours.

For herpetic meningoencephalitis, a dose of 10 mg/kg is administered every 8 hours (provided that renal function is not impaired), treatment should begin as soon as possible after the onset of the disease.

To prevent infections caused by the Herpes Simplex virus types 1 and 2 in cases of severe immunodeficiency, including after bone marrow transplantation, or impaired absorption from the intestine, it is prescribed intravenously at a dose of 5 mg/kg 3 times a day with an interval of 8 hours.

For infections caused by Varicella zoster, administer intravenously at a dose of 5 mg/kg 3 times a day with an interval of 8 hours. For patients with immunodeficiency, the dose is increased to 10 mg/kg every 8 hours (provided that renal function is not impaired). Treatment should begin as soon as possible after the rash appears.

To prevent cytomegalovirus infection, the drug is administered intravenously at a dose of 500 mg/m2 3 times a day (every 8 hours), for 5 days before bone marrow transplantation and for 30 days after transplantation.

As part of complex therapy for severe immunodeficiency, adults are given a course of intravenous acyclovir therapy for 1 month, and then switch to oral acyclovir.

The maximum dose for adults is 30 mg/kg/day.

Children aged 3 months to 12 years are usually used at a dose equal to half the adult dose (250 mg/m2 3 times a day, every 8 hours).

For the treatment of infections caused by Herpes simplex types 1 and 2, as well as for the prevention of infections caused by the Herpes simplex virus types 1 and 2 in children with immunodeficiency, a dose of 250 mg/m2 is prescribed 3 times a day (every 8 hours).

For the treatment of chickenpox in children, use abt at a dose of 250 mg/m2 3 times a day (every 8 hours).

For the treatment of chickenpox in children with immunodeficiency and the treatment of herpetic meningoencephalitis, the recommended dose for intravenous administration is 500 mg/m2 3 times a day (every 8 hours), provided that renal function is not impaired.

For the prevention of cytomegalovirus infection in children aged 2 years and older, the same doses are recommended as for adults (500 mg/m2 3 times a day, every 8 hours, for 5 days before bone marrow transplantation and for 30 days after transplantation ).

Doses of the drug are determined in accordance with the values ​​of creatinine clearance: with a creatinine clearance of 25-50 ml/min, 5-10 mg/kg or 500 mg/m2 are prescribed 2 times a day (every 12 hours), with a creatinine clearance of 10-25 ml/min. min are prescribed at 5-10 mg/kg or 500 mg/m2 1 time per day, with creatinine clearance less than 10 ml/min, prescribed at 2.5-5 mg/kg or 250 mg/m2 1 time per day, subject to hemodialysis or continuous ambulatory peritoneal dialysis.

The duration of treatment depends on the patient's condition and response to therapy. The drug is administered intravenously, usually for 5 to 7 days. For herpetic meningoencephalitis, the duration of treatment is usually 10 days.

Rules for the preparation and administration of infusion solution for intravenous administration

For intravenous administration, the contents of 1 bottle containing 0.25 g are dissolved in 10 ml of sterile water for injection or in a sterile 0.9% sodium chloride solution. The solution can be injected slowly (over an hour) or used dropwise, for which the resulting solution (25 mg in 1 ml) is diluted with an additional 40 ml of solvent (the total volume of the resulting solution is 50 ml, 1 ml contains 5 mg).

For intravenous administration, the contents of 1 bottle containing 0.5 g are dissolved in 20 ml of sterile water for injection or in a sterile 0.9% sodium chloride solution. The solution can be injected slowly (over an hour) or used dropwise, for which the resulting solution (25 mg in 1 ml) is diluted with an additional 80 ml of solvent (the total volume of the resulting solution is 100 ml, 1 ml contains 5 mg).

For intravenous administration, the contents of 1 bottle containing 1.0 g are dissolved in 40 ml of sterile water for injection or in a sterile 0.9% sodium chloride solution. The solution can be injected slowly (over an hour) or used dropwise, for which the resulting solution (25 mg in 1 ml) is diluted in an additional 160 ml of solvent (the total volume of the resulting solution is 200 ml, 1 ml contains 5 mg).

It is necessary to achieve complete dissolution of the drug crystals. Freshly prepared solutions should be used.

For adults, when using acyclovir in doses up to 500 mg, the drug must be administered in a liquid volume of at least 100 ml. If it is necessary to administer the drug in high doses (from 500 mg to 1000 mg), the volume of injected fluid should be increased.

Intravenous administration is carried out slowly, drip-wise, over 1 hour, regardless of the dose of the drug. The drug can be administered using an injection pump with adjustable flow.

The solution prepared for intravenous administration should be stored at a temperature of 15-25°C for no more than 12 hours. In case of turbidity, crystallization during dilution, administration or storage, the use of the solution is excluded.

special instructions

During pregnancy and lactation, acyclovir is prescribed only for health reasons; Breastfeeding is stopped for the period of treatment.

In patients with immunodeficiency, viral resistance to acyclovir may occur, especially in the case of multiple repeated courses of treatment.

The drug is not prescribed to children with chickenpox if the disease is mild. The use of acyclovir in children with normal immunity for the prevention of recurrent infections caused by the Herpes simplex virus and for the treatment of infections caused by the herpes zoster virus is not recommended due to the lack of clinical data.

Administration of acyclovir intravenously for 1 month before bone marrow transplantation followed by oral administration of the drug leads to a decrease in mortality.

During the treatment period, adequate rehydration therapy should be carried out, especially in elderly patients and when using high doses of acyclovir. In elderly patients with renal failure, the drug should be prescribed in lower doses.

The drug does not affect the ability to drive vehicles and machinery.

Side effect

When using the drug, headaches, increased fatigue, increased levels of bilirubin, urea and creatinine in the blood serum, a transient increase in the activity of liver transaminases, edema, and lymphadenopathy are possible.

In isolated cases, neurological disorders, drowsiness, nausea, vomiting, diarrhea, and intestinal colic may occur. Possible allergic skin reactions (quickly disappear after discontinuation of the drug), urticaria, itching, fever, rarely - shortness of breath, angioedema, anaphylaxis, leukopenia, thrombocytopenia. In rare cases (usually with extravasation), local inflammation and phlebitis may occur at the injection site.

With a course of intravenous administration in high doses, renal failure may develop.

Side effects from the central nervous system are usually reversible and occur mainly when the drug is administered in high doses, as well as in patients with renal failure and AIDS.

Contraindications

Hypersensitivity to acyclovir or valacyclovir.

Release form

Lyophilized powder for the preparation of a solution for infusion of 250 mg in 20 ml bottles; 500 mg or 1000 mg in glass bottles with a capacity of 50 ml or 100 ml, respectively.