Pharmacodynamics and pharmacokinetics
The active ingredient of the drug inhibits the activity of DNA polymerase herpes viruses , prevents the synthesis of viral DNA and inhibits replication processes.
After entering the body, valacyclovir is transformed into acyclovir and L-valine , then phosphorylation and acyclovir is converted into acyclovir triphosphate . The resulting compound is capable of inhibiting the DNA polymerase of a harmful agent (virus) through a competitive mechanism.
Phosphorylation usually occurs in two stages. In the first, the reaction is catalyzed by the enzyme thymidine kinase . The drug exhibits particular activity against Herpes simplex; it is less sensitive to Varicella zoster. The substance is excreted by the kidneys or feces; the half-life is approximately three hours.
Buy Valacyclovir Izvarino film-coated tablets 500 mg No. 10 in pharmacies
Valaciclovir Izvarino tab p.o. 500 mg No. 10
Pharmacological action Pharmaceutical group: antiviral agent. Pharmaceutical action: Nucleoside inhibitor of DNA polymerase of herpes viruses. Blocks viral DNA synthesis and viral replication. In the human body it is converted into acyclovir and L-valine; As a result of phosphorylation, active acyclovir triphosphate is formed from acyclovir, which competitively inhibits viral DNA polymerase. The first stage of phosphorylation occurs under the influence of a virus-specific enzyme (for Herpes simplex types 1 and 2, Varicella zoster is a viral thymidine kinase, which is found only in cells infected with the virus). More active against Herpes simplex than Varicella zoster. Pharmacokinetics: Absorption is high, quickly and almost completely converted into acyclovir and L-valine. The bioavailability of acyclovir when taking 1 g of valacyclovir is 54% (3-5 times higher than when taking acyclovir orally). After using valacyclovir at a dose of 1 g 4 times a day, the AUC is approximately equal to the AUC with intravenous administration of acyclovir at a dose of 5 mg every 8 hours. Cmax after a single dose of 1 g is 15-25 µmol/ml, TCmax is 1.6-2.1 hours; after 3 hours, unmetabolized valacyclovir is not detected in plasma. Protein binding of valacyclovir is 13-18%, acyclovir is 9-33%. Acyclovir is widely distributed in tissues and body fluids, including the brain, kidneys, lungs, liver, aqueous humor, tear fluid, intestines, muscles, spleen, uterus, vaginal mucosa and secretions, sperm, amniotic fluid, CSF (50% of the concentration in plasma), liquid of herpetic vesicles. The highest concentrations are created in the kidneys, liver and intestines. Penetrates through the placenta and into breast milk. T1/2 of valacyclovir - less than 30 minutes; acyclovir - 2.5-3.3 hours, for end-stage renal failure - 14 hours, in elderly patients (65-83 years old) - 3.3-3.7. Excreted by the kidneys (45.6%), mainly in the form of acyclovir and its metabolite 9-carboxymethoxymethylguanine, less than 1% - unchanged and with feces (47.12%) within 96 hours.
Indications In adults: herpes of the lips, genital herpes (primary and recurrent infection; long-term suppressive therapy of recurrent genital herpes in people with immunodeficiency, including HIV infection; reducing the risk of transmission of infection to a sexual partner), herpes zoster. In adults and children over 12 years of age: prevention of cytomegalovirus infection during organ transplantation.
Contraindications Hypersensitivity, HIV infection with a CD4+ lymphocyte count of less than 100/μl, childhood (up to 12 years for CMV, up to 18 years for other indications). Carefully. Liver/renal failure, old age, hypohydration, simultaneous use of nephrotoxic drugs, pregnancy, lactation, childhood.
Special instructions Elderly patients and persons with dehydration during the treatment period need to increase the volume of fluid consumed (risk of developing acute renal failure). When treating genital herpes, sexual contact should be avoided, because the drug does not protect against transmission of infection. Taking the drug in high doses for a long time in conditions accompanied by severe immunodeficiency (bone marrow transplantation, clinical forms of HIV infection, kidney transplantation) led to the development of thrombocytopenic purpura and hemolytic-uremic syndrome, including death. If side effects from the central nervous system occur (including agitation, hallucinations, confusion, delirium, convulsions and encephalopathy), the drug is discontinued.
Composition Valacyclovir 500 mg.
Directions for use and dosage : Orally, regardless of food intake. Adults, incl. with chronic renal failure and CC less than 50 ml/min/1.73 sq.m: for herpes of the lips (treatment begins when tingling, itching or burning appears) - 2 g every 12 hours, with CC 30-49 - 1 g every 12 hours, for CC 10-29 - 500 mg every 12 hours, for CC less than 10 - 500 mg once. Course of treatment - 1 day; for primary genital herpes (including for CC 30-49 ml/min/1.73 sq.m) - 1 g 2 times a day, for CC 10-29 - 1 g every 24 hours, for CC less than 10 - 500 mg every 24 hours. Course of treatment - 10 days; for recurrent genital herpes (including with CC 30-49 ml/min/1.73 sq.m.) - 500 mg 2 times a day, for CC less than 30 - 500 mg every 24 hours. Course of treatment - 3 days . Treatment begins at the first appearance of signs or symptoms of relapse; with long-term suppressive therapy of recurrent genital herpes in people with immunodeficiency, incl. HIV infection - 1 g per day (including with CC 30-49), with CC less than 30 - 500 mg every 24 hours, with the number of relapses less than 9 per year, use is possible (including with CC 30-49) - 500 mg per day, with CC less than 30 - 500 mg every 48 hours, in HIV-infected patients with a CD4+ cell count of more than 100/μl (including with CC 30-49) - 500 mg 2 times a day, with CC less than 30 - 500 mg every 24 hours; to reduce the risk of transmission of infection to a sexual partner, if the number of relapses is less than 9 per year, the sexual partner is prescribed 500 mg 1 time per day. for herpes zoster - 1 g every 8 hours for 7 days (treatment begins within 48 hours after the appearance of the rash), for CC 30-49 - 1 g every 12 hours, for CC 10-29 - 1 g every 24 hours, with CC less than 10 - 500 mg every 24 hours.
Adults and children over 12 years old, incl. with chronic renal failure and CC less than 75 ml/min/1.73 sq.m: prevention of CMV infection during organ transplantation - 2 g 4 times a day; with CC 50-75 - 1.5 g 4 times a day; with CC 25-50 - 1.5 g 3 times a day; with CC 10-25 - 1.5 g 2 times a day; with CC less than 10 and patients on hemodialysis - 1.5 g 1 time per day. The course of treatment is 90 days. The drug should be taken as soon as possible after transplantation. For patients on hemodialysis, the drug is administered after the hemodialysis procedure. T1/2 in such patients is 4 hours; During the 4-hour procedure, 30% of the drug is removed. With peritoneal dialysis, the drug is removed to a lesser extent, other pharmacokinetic parameters remain the same.
Side effects From the digestive system: nausea, abdominal pain, vomiting, diarrhea, increased activity of ALT, AST, alkaline phosphatase, hepatitis. From the nervous system: headache, dizziness, depression, aggressive behavior, agitation, ataxia, coma, confusion or depression of consciousness, dysarthria, encephalopathy, mania, psychosis, incl. auditory and visual hallucinations, convulsions, tremors. From the senses: visual impairment. From the urinary system: pain in the projection of the kidneys, acute renal failure. From the hematopoietic organs: neutropenia, thrombocytopenia, aplastic anemia, leukoclastic vasculitis, thrombotic thrombocytopenic purpura. From the skin: erythema multiforme, rash, photosensitivity, alopecia. Allergic reactions: angioedema, shortness of breath, itching, rash, urticaria, anaphylactic reactions. Laboratory indicators: decreased Hb, hypercreatininemia. Other: dysmenorrhea, arthralgia, nasopharyngitis, respiratory tract infections, facial swelling, increased blood pressure, tachycardia, fatigue; additionally in children - fever, dehydration, rhinorrhea.
Drug interactions Cimetidine and tubular secretion blockers reduce the effect (they reduce the rate, but not the completeness, of conversion to acyclovir). In persons with normal CC, no dosage adjustment is required. Nephrotoxic drugs (including cyclosporine, tacrolimus) increase the risk of developing nephrotoxicity.
Overdose Symptoms: possible deposition of acyclovir in the renal tubules, with the development of acute renal failure and anuria. Treatment: hemodialysis.
Conditions for dispensing from pharmacies
Dispensed with a doctor's prescription
Side effects
The drug has been well researched. As a result of laboratory studies and observations of patients with herpes zoster and herpes virus (including those with concomitant immunodeficiency ) taking valacyclovir , almost all possible adverse reactions were identified.
Possible:
- nausea, pain in the epigastric region, vomiting, anorexia and diarrhea , increased activity of liver enzymes, hepatitis ;
- impaired renal function, photosensitivity , shortness of breath, thrombocytopenia ;
- headaches, dizziness , hallucinations , depression , agitation , ataxia , psychosis , dysarthria , disturbances of consciousness and coma ;
- rash , itching , anaphylaxis , urticaria , Quincke's edema ;
- neutropenia , aplastic anemia , vasculitis , thrombocytopenia ;
- nasopharyngitis , facial swelling , tachycardia , increased blood pressure , increased fatigue;
- rhinorrhea , fever and dehydration .
Valacyclovir Velpharm film-coated tablets 500 mg 10 pcs. in St. Petersburg
According to the World Health Organization (WHO), side effects are classified according to their frequency as follows: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, < 1/100), rare (≥ 1/10000, < 1/1000), very rare (< 1/10000), frequency unknown (frequency cannot be determined based on available data).
Clinical trial data
Nervous system disorders
- Often: headache.
Gastrointestinal disorders
- Common: nausea.
Post-marketing data
Blood and lymphatic system disorders
- Very rare: leukopenia, thrombocytopenia. Basically, leukopenia was observed in patients with reduced immunity.
Immune system disorders
- Very rare: anaphylaxis.
Nervous system and mental disorders
- Rarely: dizziness, confusion, hallucinations, depression of consciousness.
- Very rare: agitation, tremor, ataxia, dysarthria, psychotic symptoms, convulsions, encephalopathy, coma. The symptoms listed above are mostly reversible and are usually observed in patients with impaired renal function or other predisposing conditions. In adult organ transplant patients receiving high doses (8 g per day) of valacyclovir for the prevention of CMV infection, neurological reactions develop more often than when taking lower doses.
Respiratory, thoracic and mediastinal disorders
- Uncommon: shortness of breath.
Gastrointestinal disorders
- Rarely: abdominal discomfort, vomiting, diarrhea.
Disorders of the liver and biliary tract
- Very rare: reversible abnormalities in liver function tests, which are sometimes regarded as manifestations of hepatitis.
Skin and subcutaneous tissue disorders
- Uncommon: rashes, including manifestations of photosensitivity.
- Rarely: itching.
- Very rare: urticaria, angioedema.
Renal and urinary tract disorders
- Uncommon: hematuria (often associated with other renal disorders).
- Rarely: renal dysfunction.
- Very rare: acute renal failure, renal colic. Renal colic may be associated with impaired renal function. Cases of precipitation of acyclovir crystals in the lumen of the renal tubules have been reported. It is necessary to maintain an adequate drinking regime during treatment.
Social circumstances
Cases of renal failure, microangiopathic hemolytic anemia and thrombocytopenia (sometimes in combination) have been observed in severely immunocompromised patients, especially adult patients with advanced HIV infection, receiving high doses of valacyclovir (8 g daily) for long periods of time. Similar complications were noted in patients with the same underlying and/or concomitant diseases, but not receiving valacyclovir.
Instructions for use of Valaciclovir (Method and dosage)
The drug is taken orally, regardless of food.
Valacyclovir tablets, instructions for use
For herpes zoster, a single dosage is 1000 mg (2 tablets), 3 times a day. The course of treatment is 7 days. The sooner the drug is started after the first symptoms of the disease appear, the more effective the treatment will be.
For herpes (including prophylactic use), the daily dosage is 1000 mg. It is recommended to divide into 2 doses, morning and evening, one tablet each. The duration of treatment is from 5 to 10 days (severe course of the disease).
If the patient has impaired renal function, the dose should be adjusted.
Valacyclovir tablet p/pl/o 500 mg N40 (Synthesis)
The drug Valacyclovir is taken regardless of food intake, the tablets should be washed down with water. Treatment of skin and mucous membrane infections caused by HSV, including newly diagnosed and recurrent genital herpes (Herpes genitalis), as well as labial herpes (Herpes labialis) Immunocompetent adults and adolescents aged 12 to 18 years. The recommended dose is 500 mg 2 times a day. In case of relapse, treatment should continue for 3 or 5 days. In the case of primary herpes, which can occur in a more severe form, treatment should begin as early as possible, and its duration should be increased from 5 to 10 days. In case of relapses of HSV, the most correct prescription of the drug Valaciclovir is considered to be in the prodromal period or immediately after the appearance of the first symptoms of the disease. The use of valacyclovir may prevent the development of lesions if it is given at the first signs and symptoms of relapse due to HSV. As an alternative treatment for labial herpes, the use of the drug Valacyclovir at a dose of 2000 mg 2 times a day for 1 day is effective. The second dose should be taken approximately 12 hours (but not earlier than 6 hours) after the first dose. When using this dosage regimen, the duration of treatment should not exceed 1 day, since exceeding the duration of this course of treatment does not lead to additional clinical benefit. Therapy should be started when the earliest symptoms of herpes labialis (ie, tingling, itching, burning) appear. Prevention (suppression) of recurrent infections of the skin and mucous membranes caused by HSV, including genital herpes, including in adults with immunodeficiency. Immunocompetent adults and adolescents aged 12 to 18 years. In immunocompetent patients, the recommended dose is 500 mg once daily. After 6-12 months of treatment, it is necessary to evaluate the effectiveness of therapy. Adults with immunodeficiency. In adult patients with immunodeficiency, the recommended dose is 500 mg 2 times a day. After 6-12 months of treatment, it is necessary to evaluate the effectiveness of therapy. Prevention of infections caused by HSV and diseases after solid organ transplantation. Adults and teenagers aged 12 to 18 years. The recommended dose is 2000 mg 4 times a day, prescribed as early as possible after transplantation. The dose should be reduced depending on creatinine clearance. The duration of treatment is usually 90 days, but in high-risk patients the course of treatment may be extended. Treatment of herpes zoster (Herpes zoster) and ophthalmic herpes zoster. Adults. The recommended dose is 1000 mg 3 times a day for 7 days. Special groups of patients. Children. The effectiveness of treatment with Valacyclovir in children has not been studied. Elderly patients. It is necessary to take into account the possible impairment of renal function in elderly patients, and the dose of Valaciclovir should be adjusted accordingly. It is necessary to maintain adequate water and electrolyte balance. Patients with impaired renal function. It is recommended to reduce the dose of Valaciclovir in patients with severe renal impairment (see dosage regimen in Table 2). In such patients, it is necessary to maintain adequate water and electrolyte balance. Dose adjustment of Valacyclovir for use in adults and adolescents aged 12 to 18 years with impaired renal function. Herpes zoster and ophthalmic herpes zoster in immunocompetent adults (treatment): at least 50 - 1000 mg 3 times a day, from 30 to 49 - 1000 mg 2 times a day, from 10 to 29 - 1000 mg 1 time a day, less than 10 - 500 mg 1 time per day. HSV (treatment). Immunocompetent adults and adolescents aged 12 to 18 years: at least 30-500 mg 2 times a day, less than 30-500 mg 1 time a day. Labial herpes in immunocompetent adults and adolescents aged 12 to 18 years (treatment): at least 50 - 2000 mg 2 times a day, from 30 to 49 - 1000 mg 2 times a day, from 10 to 29 - 500 mg 2 times per day, less than 10 - 500 mg 1 time per day. HSV (prevention (suppression)). Immunocompetent adults and adolescents aged 12 to 18 years: at least 30-500 mg once a day, less than 30-500 mg once every two days. Adults with immunodeficiency: at least 30-500 mg 2 times a day, less than 30-500 mg 1 time a day. Prevention of infections caused by CMV in adults and adolescents aged 12 to 18 years: at least 75 - 2000 mg 4 times a day, from 50 to 75 - 1500 mg 4 times a day, from 25 to 50 - 1500 mg 3 times per day, from 10 to 25 - 1500 mg 2 times a day, less than 10 or in patients on hemodialysis - 1500 mg 1 time per day. Additional information for indication: treatment of skin and mucous membrane infections caused by HSV, including newly diagnosed and recurrent genital herpes (Herpes genitalis), as well as labial herpes (Herpes labialis). There is no experience with the use of Valacyclovir in children with creatinine clearance values less than 50 ml/min/1.73 m2. Additional information for the indication: Prevention of CMV infections and morbidity after solid organ transplantation. Creatinine clearance should be determined frequently, especially during periods when renal function changes rapidly, such as immediately after transplantation or engraftment, and the dose of Valacyclovir is adjusted accordingly. with creatinine clearance indicators. Additional information for the indication: Treatment of herpes zoster and herpes zoster ophthalmicus Valacyclovir should be used after hemodialysis in patients undergoing intermittent hemodialysis. Patients with impaired liver function. Based on a study using a single dose of valaciclovir 1000 mg in adult patients with mild to moderate liver cirrhosis (with preserved synthetic liver function), no dose adjustment of valaciclovir is required. Pharmacokinetic data in adult patients with severe liver dysfunction (decompensated cirrhosis), impaired synthetic liver function and the presence of portacaval anastomoses also do not indicate the need for dose adjustment of Valacyclovir, however, clinical experience with these pathologies is limited. Information about doses greater than 4000 mg per day for patients with infections caused by HSV and CMV is listed in the section "Special Instructions."
Interaction
There were no clinically significant cases of interaction between tablets and other drugs.
However, the active substance is excreted from the body through the kidneys by tubular secretion . Any medications that are prescribed simultaneously with Valacyclovir will interfere with its normal elimination from the body. This primarily applies to Cimetidine and other drugs that block the mechanism of tubular secretion.
When combined with Mycophenolate , the concentration of acyclovir in the blood plasma increases.
When the drug is combined with Cyclosporine , Tacrolimus and drugs that interfere with the normal functioning of the kidneys, the load on these organs increases.
VALACICLOVIR
Pharmacokinetics
Absorption
After oral administration, valacyclovir is well absorbed from the gastrointestinal tract, quickly and almost completely converted to acyclovir and valine. This conversion is probably carried out by the liver enzyme valacyclovir hydrolase.
When taking valacyclovir in a dose of 1000 mg, the bioavailability of acyclovir is 54% and is not reduced by food intake. The pharmacokinetics of valacyclovir is not dose-dependent. The rate and extent of absorption decrease with increasing dose, resulting in a less proportionate increase in maximum plasma concentration (Cmax) compared to the therapeutic dose range and a decrease in bioavailability at doses above 500 mg.
Table 1. Results of assessing the pharmacokinetics of acyclovir when taking single doses of valacyclovir from 250 mg to 2000 mg in healthy volunteers with normal liver function
Pharmacokinetic parameters of acyclovir | 250 mg (N=15) | 500 mg (N=15) | 1000 mg (N=15) | 2000 mg (N=8) | |
Cmax | µmol/l | 9,78 ± 1,71 | 15,0 ±4,23 | 23,1 ±8,53 | 36,9 ± 6,36 |
µg/ml | 2,20 ± 0,38 | 3,37 ±0,95 | 5,20 ± 1,92 | 8,30 ± 1,43 | |
Tmax | hours (h) | 0,75 (0,75-1,5) | 1,0 (0,75-2,5) | 2,0 (0,75-3,0) | 2,0 (1,5-3,0) |
AUC | hµmol/l | 24,4 ± 3,65 | 49,3 ± 7,77 | 83,9 ±20,1 | 131 ±28,3 |
hµg/ml | 5,50 ±0,82 | 11,1 ± 1,75 | 18,9 ±4,51 | 29,5 ± 6,36 |
Cmax - maximum concentration in blood plasma;
Tmax is the time until the maximum concentration in the blood plasma is reached;
AUC is the area under the concentration-time pharmacokinetic curve. The Cmax and AUC values reflect the average standard deviation. Values for Tmax reflect the median value and range of values. The maximum concentration of valacyclovir in blood plasma is only 4% of the concentration of acyclovir, the median time to reach it ranges from 30 to 100 minutes after taking the drug. 3 hours after dosing, the concentration of valacyclovir reaches the level of quantitative determination or below.
Valacyclovir and acyclovir have similar pharmacokinetic parameters after single and multiple doses. VZV and HSV do not significantly alter the pharmacokinetics of valacyclovir and acyclovir after oral administration of valacyclovir.
Distribution
The degree of binding of valacyclovir to plasma proteins is very low (15%). The extent of penetration into the cerebrospinal fluid (CSF) is defined as the ratio of AUC in CSF to AUC in plasma and is about 25% for acyclovir and the metabolite 8-hydroxyacyclovir (8-OH-ACV); about 2.5% for the metabolite 9-(carboxymethoxy)methyl-guanine (CMMG).
Metabolism
After oral administration, valacyclovir is converted to acyclovir and L-valine through first-pass metabolism in the intestine and/or hepatic metabolism. Acyclovir is converted into small metabolites: CMMG under the influence of ethyl alcohol and aldehyde dehydrogenase; 8-OH-ACV under the influence of aldehyde oxidase. Approximately 88% of the total cumulative plasma exposure is due to acyclovir, 11% to CMMG, and 1% to 8-OH-ACV. Valacyclovir and acyclovir are not metabolized by isoenzymes of the cytochrome P450 system.
Removal
In patients with normal renal function, the half-life of acyclovir from the blood plasma after a single or multiple doses of valacyclovir is approximately 3 hours. Less than 1% of the administered dose of valacyclovir is excreted unchanged by the kidneys. Valaciclovir is excreted from the body by the kidneys mainly in the form of acyclovir (more than 80% of the dose taken) and the metabolite of acyclovir - CMMG.
Special patient groups
Patients with impaired renal function
The elimination of acyclovir correlates with renal function, and acyclovir exposure increases with the severity of renal failure. In patients with end-stage renal disease, the mean half-life of acyclovir following valacyclovir use is approximately 14 hours, compared with approximately 3 hours in those with normal renal function.
Exposure of acyclovir and its metabolites CMMG and 8-OH-ACV in plasma and CSF were assessed at steady state after multiple doses of valacyclovir in 6 patients with normal renal function (mean creatinine clearance 111 ml/min, range 91-144 ml/min), receiving 2000 mg every 6 hours, and 3 patients with severe renal impairment (mean creatinine clearance 26 ml/min, range 17-31 ml/min) receiving 1500 mg every 12 hours. In severe renal failure, compared with normal renal function, plasma and CSF concentrations of acyclovir, CMMG, and 8-OH-ACV were 2-, 4-, and 5-6-fold higher, respectively. There was no difference in the extent of acyclovir CSF penetration (defined as the ratio of CSF AUC to plasma AUC), CMMG, or 8-OH-ACV between the two populations with severe renal impairment and normal renal function.
Patients with liver dysfunction
Pharmacokinetic data show that in patients with hepatic impairment, the rate of conversion of valacyclovir to acyclovir is reduced, but not the extent of this conversion. The half-life of acyclovir is independent of liver function.
Pregnancy
A study of the pharmacokinetics of valacyclovir and acyclovir in late pregnancy found an increase in the daily AUC value at steady state when taking valacyclovir daily at a dose of 1000 mg per day, which was approximately 2 times higher than the AUC when taking oral acyclovir at a dose of 1200 mg per day.
HIV infection
In patients with HIV infection, the distribution and pharmacokinetic characteristics of acyclovir after oral administration of one or more doses of 1000 mg or 2000 mg of valacyclovir remain unchanged compared with healthy volunteers.
Organ transplantation
The maximum concentration of acyclovir in organ transplant patients receiving 2000 mg valacyclovir 4 times daily was comparable to or higher than the maximum concentration observed in healthy volunteers receiving the same dose. The established daily AUC values can be characterized as noticeably higher.
special instructions
If you have kidney problems, use the drug with caution. Possible development of acute renal failure , disorders of the central nervous system.
For elderly patients, no dose adjustment is required, but the amount of fluid consumed should be increased.
During treatment for genital herpes, you should refrain from sexual intercourse, as the drug does not protect you from transmitting the virus to your partner.
Caution should be exercised when treating patients with liver disease.
There is no clinical experience with the use of the drug for children under 12 years of age; therefore, the medicine is not prescribed to children.
If the patient has undergone a bone marrow or kidney transplant, a clinically pronounced form of HIV infection , and acute immunodeficiency , then taking the drug can lead to thrombocytopenic purpura , hemolytic-uremic syndrome and death.
hallucinations, convulsions, agitation, confusion and delirium are observed during treatment with the drug , the drug should be discontinued.
Valacyclovir
Inside. The drug Valacyclovir is taken regardless of food intake, the tablets should be washed down with water.
Treatment of herpes zoster
Adults
The recommended dose is 1000 mg 3 times a day for 7 days.
Treatment of infections caused by HIV
Adults
The recommended dose for treatment of an episode is 500 mg 2 times a day.
In the case of primary herpes, which can occur in a more severe form, treatment should begin as early as possible, and its duration can be increased from 5 to 10 days. In case of relapse, treatment should continue for 3 or 5 days. For recurrent HSV, it is ideal to prescribe valacyclovir in the prodromal period or immediately after the first symptoms of the disease appear.
As an alternative, valacyclovir 2 g twice daily is effective for the treatment of herpes labialis. The second dose should be taken approximately 12 hours (but not earlier than 6 hours) after the first dose. When using this dosage regimen, the duration of treatment should not exceed 1 day, since exceeding the duration of treatment does not lead to an additional clinical effect. Therapy should be started when the earliest symptoms of herpes labialis (ie, tingling, itching, burning) appear.
Prevention (suppression) of recurrent infections caused by HSV
Adults
In patients with preserved immunity, the recommended dose is 500 mg once daily.
In patients with immunodeficiency, the recommended dose is 500 mg 2 times a day.
Prevention of transmission of genital herpes to a healthy partner when taken as suppressive therapy in combination with safe sex
For infected immunocompetent individuals with relapses no more than 9 times a year, the recommended dose of valacyclovir is 500 mg once a day for a year or more every day.
There are no data on infection prevention in other patient populations.
Prevention of infections caused by cytomegalovirus (CMV) and diseases after solid organ transplantation
Adults and teenagers aged 12 years and older
The recommended dose is 2 g 4 times a day, prescribed as early as possible after transplantation.
The dose should be reduced depending on creatinine clearance.
The duration of treatment is 90 days, but in high-risk patients the course of treatment can be extended.
Special patient groups
Patients with impaired renal function
Treatment of herpes zoster and infections caused by HSV, prevention (suppression) of relapses of infection caused by HSV, prevention of transmission of genital herpes to a healthy partner.
It is recommended to reduce the dose of valacyclovir in patients with a significant decrease in renal function (see dosage for renal failure in the table). In such patients, it is necessary to maintain adequate water and electrolyte balance.
There is no experience with the use of valacyclovir in children with creatinine clearance values less than 50 ml/min/1.73 m2.
Indications | Creatinine clearance, ml/min | Valaciclovir dosage |
Herpes zoster | 15-30 | 1 g 2 times a day |
less than 15 | 1 g 5 times a day | |
Treatment of infection caused by HSV (but with a regimen of 500 mg 2 times a day) | less than 15 | 500 mg 1 time per day |
31-49 | 1 g twice in one day | |
Treatment of labial herpes (according to the regimen of 2 g 2 times during one day) | 15-30 | 500 mg twice in one day |
less than 15 | 500 mg once | |
Prevention (suppression) of recurrent infections caused by HSV: | ||
- patients with normal immunity | less than 15 | 250 mg 1 time per day |
- patients with reduced immunity | less than 15 | 500 mg 1 time per day |
– reducing the risk of transmission of genital herpes | less than 15 | 250 mg 1 time per day |
For patients on hemodialysis, it is recommended to use valacyclovir immediately after the end of the hemodialysis session at the same dose as in patients with creatinine clearance less than 15 ml/min.
Prevention of cytomegalovirus (CMV) infection after transplantation
The prescribing regimen for valacyclovir in patients with impaired renal function should be established in accordance with the table below.
Creatinine clearance, ml/min | Valacyclovir dose |
75 or more | 2 g 4 times a day |
from 50 to less than 75 | 1.5 g 4 times a day |
from 25 to less than 50 | 1.5 g 3 times a day |
from 10 to less than 25 | 1.5 g 2 times a day |
clearer 10 or dialysis* | 1.5 g 1 time per day |
* In patients undergoing hemodialysis, valacyclovir should be prescribed after the end of the hemodialysis session.
Creatinine clearance should be determined frequently, especially during periods when renal function changes rapidly, such as immediately after transplantation or engraftment, and the dose of valacyclovir is adjusted according to creatinine clearance.
Patients with liver dysfunction
In adult patients with mild or moderate hepatic impairment with preserved synthetic function, no dose adjustment of Valacyclovir is required.
Pharmacokinetic data in adult patients with severely impaired liver function (decompensated cirrhosis), with impaired synthetic liver function and the presence of portacaval anastomoses also do not indicate the need to adjust the dose of Valacyclovir, however, clinical experience with this pathology is limited.
Children under 12 years of age
There are no data on the use of valaciclovir in children.
Elderly patients
No dosage adjustment is required unless there is significant impairment of renal function. It is necessary to maintain adequate water and electrolyte balance.
Valacyclovir analogs
Level 4 ATC code matches:
Herperax
Vivorax
Vairova
Acyclostad
Geviran
Walcyte
Valavir
Ribavirin
Valtrex
Valvir
Rebetol
Cyclovir
Famciclovir Teva
Famvir
The closest analogues: Vayora, Valaciclovir Canon, Valaciclovir hydrochloride, Valogard, Valcicon, Virdel, Valavir, Valvir, Valtrex, Vacirex .
Which is better: Valaciclovir or Valtrex?
Valtrex is an imported analogue with the same active ingredient. In terms of effectiveness and frequency of adverse reactions, the drugs are identical. However, the cost of Valtrex is significantly higher than Valaciclovir.
Valacyclovir price
The price of Valaciclovir tablets in Russia is approximately 600 rubles for 10 pieces.
Together with tablets, as a rule, an ointment containing valacyclovir is used.
The price of Valacyclovir in Ukraine is slightly higher. You can buy the drug for 360 UAH (10 tablets).
- Online pharmacies in RussiaRussia
ZdravCity
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