"IBUPROFEN" (injections): instructions for use, price in pharmacies, analogues

Compound

The tablets contain the active ingredient ibuprofen (200/400/500 mg) and excipients: potato starch, magnesium stearate, aerosil, vanillin, beeswax, food gelatin, azorubine dye, magnesium hydroxycarbonate, wheat flour, low molecular weight povidone, sucrose, dioxide titanium.
In the ointment and gel, the active substance is contained in a concentration of 50 mg/g, in the suspension - in a concentration of 20 mg/ml.

Auxiliary components of the gel: ethanol, propylene glycol, dimexide, carbomer 940, triethanolamine, neroli and lavender oil, methyl parahydroxybenzoate, purified water.

Auxiliary components of the ointment: dimethyl sulfoxide, macrogol 400 and 1500.

Ibuprofen in suppository form contains 60 mg of active substance and solid fat.

"IBUPROFEN" (injections): composition

• The active ingredient of the drug is ibuprofen. It is a chemical component made from propionic acid. It is a non-steroidal substance manufactured by the British in 1962. It took a long time to be finalized, and eventually, in the 1980s, the medicine was put into mass production. A decade later, Ibuprofen has cured a large number of people in the UK. In modern times, the component is used in all spheres of human life; it is used in medicine to treat anti-inflammatory diseases and fever. It is widely used by veterinarians;
• Sucrose, in everyday life this is cane sugar, is an additional substance, it is extracted from fruits and berries. In pharmaceuticals, sucrose is mainly needed as a preservative; mixtures, injections, and syrups are made from it;
• Talc is a secondary ingredient; in its raw form it is a white powder. This mineral, part of the silicate class, is in the subclass of layered silicates. For medical purposes it has been used as a disinfectant;
• Gum arabic is a substance that fades into the background when creating an injection. It is obtained from the resin of acacia sap. Effective for stomach problems;
• Other chemical substances of the drug are dyes, beeswax, carnauba wax.

Pharmacodynamics and pharmacokinetics

The effects of the drug are due to the suppression of Pg biosynthesis by inhibiting the COX enzyme.

Suppresses platelet . It has no effect on proteins that are involved in blood clotting. Slightly increases bleeding time.

When applied externally, the patient experiences a decrease in joint pain at rest and during movement; reducing morning stiffness, swelling and swelling of the joints, increasing flexibility and range of motion of the joints.

When taken orally, it is well (80%) absorbed into the gastrointestinal tract. Concomitant use with food slows down absorption, but does not affect its volume. TSmax - 2-4 hours.

The hypothermic effect develops 1 hour after administration. T1/2 - from 2 to 4 hours. Communication with plasma proteins is 90-99%.

It penetrates into the joint cavities slowly, lingers in the synovial tissue, where it accumulates in higher concentrations than in the plasma.

Achieving an anti-inflammatory effect requires from several days to 2 weeks of systematic use of the drug.

Biological activity is associated with the S-enantiomer.

After absorption, the pharmacologically inactive R-form (about 60%) is slowly transformed into the S-form. Metabolic products are excreted primarily by the kidneys and, partly, with bile. In its pure form, no more than 1% of ibuprofen is excreted.

The substance is not detected in breast milk. Complete removal occurs within 24 hours.

"IBUPROFEN" (injections): analogues

If a person has a personal intolerance to the ingredients of the original, is allergic, or has side effects, then he should urgently stop using the product and consult a doctor. He will prescribe you a similar medication with properties that are more suitable for you. Among all the substitutes, the following stand out:

Indications for use

Ibuprofen - what is it?

Ibuprofen is a non-narcotic analgesic that belongs to the NSAID group. Has pronounced anti-inflammatory activity.

These properties allow the drug to be used for heat and pain (mild and moderate intensity), polymyalgia rheumatica , and inflammatory and degenerative diseases of the musculoskeletal system.

Ibuprofen is included in the WHO list of essential medicines.

What is Ibuprofen tablets for?

Tablets are prescribed for:

• inflammatory diseases of the spine and joints ( ankylosing spondylitis , gouty and rheumatoid arthritis , osteoarthritis , etc.);
• moderate pain of various etiologies (the medicine helps with pain during menstruation, toothache, headache, migraine attack , myalgia , neuralgia , post-traumatic and postoperative pain, etc.);
• fever due to infectious or colds.

It should be remembered that tablets (like other dosage forms) are intended for symptomatic therapy, reducing pain intensity and relieving inflammation; the medicine has no effect on the progression of pathology.

Indications for use of gel and ointment

Gel and ointment with ibuprofen are effective for inflammatory and degenerative diseases of the musculoskeletal system:

• psoriatic , gouty and rheumatoid arthritis ;
• humeroscapular periarthritis;
• osteoarthritis;
• radicular syndrome in osteochondrosis ;
• ankylosing spondylitis;
• bursitis;
• sciatica;
• lumbago;
• radiculitis;
• myalgia;
• tendovaginitis;
• tendonitis;
• worsened gout;
• injuries in which the integrity of soft tissues is not compromised (rupture/sprain of ligaments, dislocation, bruise, post-traumatic swelling, etc.).

Indications for use of suppositories and syrup

Ibuprofen syrup and suppositories are dosage forms that were developed specifically for use in pediatric practice. They are prescribed to children for:

• reducing temperature during acute respiratory viral infections , childhood infections, influenza and other infectious and inflammatory diseases ;
• decrease in temperature during post-vaccination reactions;
• reducing the intensity of mild/moderate pain (the product can be used for toothache and headache, ear or throat pain, ligament damage, neuralgia, etc.).

Suppositories are intended for children 3-24 months, Ibuprofen syrup is used to treat children from 3 months to 12 years.

What is Ibuprofen used for injection?

Injections are used to treat congenital heart disease in premature newborns.

How does it affect the body?

In what cases is Ibuprofen prescribed? If a person experiences a strong body temperature, reaching 40 degrees Celsius, pain, ongoing inflammatory processes. All processes occur in arachidonic acid, an organic compound that is an omega 6 saturated acid. Metabolism occurs there - metabolism, where, during illness, cyclooxygenase - special enzymes - exhibit excessive activity. One of the functions of COX is the synthesis of prostaglandites, active substances that appear when there is a large load of fatty acids. Prostaglandites are causative agents of inflammatory processes, the goal of ibuprofen is to destroy them by eating proteins found in their deoxyribonucleic acid. After the prostaglandites lose a large amount of the necessary protein, they die and further progression of inflammation becomes impossible, as a result of which the fever and pain disappear. A positive quality of a medical product is considered to be its good effect on platelets; they do not stick together and do not form blood clots.

Contraindications

General contraindications:

• complete or partial combination of symptoms of the Fernand-Vidal triad (including a history);
• the presence of erosions and ulcers in the digestive canal;
• hemostasis disorders ;
• active gastric/intestinal bleeding ;
• severe liver failure;
• progressive kidney pathologies;
• renal failure in which Clcr does not exceed 30 ml/min;
• conditions after CABG ( coronary artery bypass grafting );
• chronic inflammatory processes in the intestines;
• confirmed hyperkalemia ;
• 3rd trimester of pregnancy;
• hypersensitivity.

In pediatrics, suspension and suppositories are used from 3 months, tablets - from 6 years of age.

Caution should be exercised when prescribing Ibuprofen for:

• liver cirrhosis , which is complicated by portal hypertension ;
• gastritis;
• colitis;
• enteritis;
• history of stomach/duodenal ulcer
• nephrotic syndrome;
• insufficiency of heart, kidney or liver function;
• IHD;
• arterial hypertension;
• cerebrovascular diseases;
• dys- or hyperlipidemia ;
• peripheral arterial diseases;
• the presence of Helicobacter pylori infection ;
• severe somatic pathologies;
• blood diseases of unknown etiology.

The drug is also prescribed with caution to persons suffering from alcoholism , long-term use of NSAIDs, taking oral corticosteroids, SSRIs, antiplatelet agents and anticoagulants, in the first 26-27 weeks of pregnancy, and lactating women.

Children under one year of age should be given the drug only on the recommendation of a pediatrician.

Side effects

The annotation for dosage forms for oral use and rectal suppositories lists the following side effects:

• NSAID gastropathy , dryness, irritation and/or ulceration of the oral mucosa, pain in the mouth, pancreatitis , aphthous stomatitis ;
• hepatitis;
• bronchospasm , shortness of breath ;
• noise/ringing in the ears, hearing loss;
• double vision or decreased clarity of visual images, irritation and dry eyes, toxic damage to the optic nerve , scotoma , swelling of the eyelids, swelling of the conjunctiva;
• nervousness, headache, anxiety, confusion, insomnia/drowsiness, dizziness, mental and motor agitation, hallucinations, depression, aseptic meningitis (rare and mainly in patients with autoimmune diseases );
• decreased contractility of the heart muscle, increased blood pressure, tachycardia ; acute renal failure, polyuria , nephrotic syndrome , allergic nephritis , cystitis ;
• hypersensitivity reactions;
• anemia , thrombocyto- and leukopenia , Werlhof's disease , agranulocytosis ;
• increased sweating.

The likelihood of visual impairment, development of gastric/intestinal bleeding and ulceration of the walls of the digestive canal increases with long-term use of high doses of Ibuprofen.

The drug affects laboratory parameters, namely:

• increases bleeding time;
• reduces serum glucose concentration, Clcr, hematocrit and hemoglobin ;
• increases the activity of liver transaminases;
• increases the concentration of creatinine in the blood serum.

Side effects when applied topically in gel/ointment form:

• tingling/burning sensation;
• skin hyperemia.

With long-term use of external therapy, the systemic effects inherent in all NSAIDs may develop.

"IBUPROFEN" (injections): reviews

The medical drug website will help us verify the effectiveness of the injection, where patients who have used the product leave their reviews. There we will look at the opinions of other users from the outside:

I am a busy person, I have absolutely no time to be distracted by headaches, back pain and fatigue. Sometimes it catches me at the most inopportune moment. If the pain happens in the evening, then I ask my wife to inject me with Ibuprofen, a few days of injections, and I’m as good as new!

I am an athlete, and I often have injuries, sometimes quite serious. Wear on joints during running and physical activity plays a role. I am not a rare visitor to my treating specialist. He prescribes me a dosage of injections, into muscles or veins, and I continue to play sports. Don’t be afraid to use this drug, it’s harmless, I’ve never had any symptoms.

Instructions for use of Ibuprofen (Method and dosage)

Ibuprofen tablets, instructions for use

The optimal dosage for children over 12 years of age and adults is 3-4 tablets of 200 mg. To achieve the desired effect, the dose can be increased to 1.2 g/day. (it should be divided into 3 doses).

When the required therapeutic effect is achieved, the daily dose should be reduced to 3-4 tablets of 200 mg per day.

The first dose is taken in the morning before meals, with a sufficient amount of liquid (this will allow the drug to be absorbed more quickly into the gastrointestinal tract). Later throughout the day, tablets are taken after meals.

The highest single dose is 400 mg (2 tablets of 200 mg), daily dose is 1.2 g (no more than 6 tablets of 200 mg within 24 hours). It is not recommended to take a repeat dose earlier than after 4 hours. Without medical advice, the drug should be taken for no more than 5 days in a row. Also, consultation with a specialist is necessary in cases where the tablets are used to treat a child under 12 years of age.

A child 6-12 years old can be given 1 tablet up to 4 times a day. A prerequisite is a weight of more than 20 kg. An interval of at least 6 hours should be maintained between tablet doses. The highest dose for this group of patients is 30 mg/kg/day.

There is no difference in how to take drugs from different manufacturers (for example, Ibuprofen-Belmed, Ibuprofen-Hemofarm or Ibuprofen-Darnitsa).

Instructions for candles

Suppositories are used rectally.

For pain and fever, the drug should be dosed based on the age and weight of the child. A single dose varies from 5 to 10 mg/kg. Frequency of applications - 3-4 rubles/day. The highest dose is 30 mg/kg/day.

The instructions for use for children indicate that patients weighing from 5.5 to 8 kg (3-9 months) should be administered 60 mg (1 suppository) every 6-8 hours, but no more than 3 suppositories per day. day. The highest dose for patients weighing from 8 to 12.5 kg (9-24 months) is 240 mg/day. (4 suppositories of 60 mg each).

To relieve fever, which is a consequence of immunization, in children under 12 months. 1 suppository of 60 mg should be administered and, if necessary, another 1 after 6 hours.

Ibuprofen suppositories can be used as an antipyretic for children for no more than 3 days. in a row, and as an analgesic - no more than 5 days. contract.

If fever persists after this time, consult a doctor.

Ibuprofen gel, instructions for use

Adults and children over 12 years of age should squeeze out a strip of gel 4-10 cm long and rub the drug with light movements until completely absorbed into the area of ​​pain projection.

The procedure can be repeated no earlier than 4 hours later. Ibuprofen is used no more than 4 times during the day. The dose depends on the extent of the painful area and varies from 50 to 125 mg.

For children 6-12 years old, a single dose is equal to the volume of a gel strip 2 to 4 cm long. The drug can be used no more than 3 times a day.

Treatment is continued for 2 to 3 weeks.

Ibuprofen ointment, instructions for use

The ointment is applied externally in the same way as the gel. The medicine is applied to the painful area 3 or 4 times a day. within 2-3 weeks. A single dose is equal to the volume of a gel strip 5 to 10 cm long.

How to take children's Ibuprofen (suspension)?

The suspension is given to children 3 times a day. at a dose of 5-10 mg/kg.

Children under one year of age can be given the drug only as prescribed by a pediatrician. The highest dose for infants is 10 ml/day. (2.5 ml 4 times/day).

Syrup for children from one to 12 years old is given 3 rubles per day. in a dose of 5 to 15 ml.

If pain and fever in a 3-6 month old child are a consequence of vaccination, 2 times a day should be given per 5-7.6 kg of body weight. 2.5 ml of suspension. After the first dose, the drug is repeated no earlier than 6 hours later.

Instructions for Ibuprofen solution for children

Ibuprofen injections are prescribed exclusively to premature infants with heart pathologies (in particular, with an unclosed ductus arteriosus).

Treatment is carried out in the intensive care unit and under the supervision of a neonatologist. Ibuprofen is administered intravenously 3 times at intervals of 24 hours. The dosage is selected depending on the child’s weight.

The first dose is 10, the second and third are 5 mg/kg.

The drug is infused slowly (over 15 minutes), preferably undiluted. If necessary, the injected volume is adjusted with 0.9% NaCl solution (or 5% glucose). The remaining unused solution is disposed of.

When determining the volume of injected solution, the total daily volume of prescribed fluid is taken into account.

If, after the child receives 1 or 2 doses, he develops overt oliguria or anuria , the next dose is administered only after restoration of normal diuresis .

If the botal duct is open 24 hours after the last dose or opens again, a repeat course is allowed, which also consists of 3 doses of the drug. If in this case it is not possible to achieve closure of the duct, the child may require surgical treatment.

ASA - acetylsalicylic acid

Gastrointestinal tract - gastrointestinal tract

IHD - coronary heart disease

LS - medicines

NSAIDs - non-steroidal anti-inflammatory drugs

COX - cyclooxygenase

PG - prostaglandin

TxA2 - thromboxane

It is difficult to imagine modern clinical practice without the use of various nonsteroidal anti-inflammatory drugs (NSAIDs). In Ancient Greece, more than 3.5 thousand years ago, Hippocrates used willow bark extract as an antipyretic and analgesic. Much later, in the 17th century, a substance was isolated from it, which was called salicylic acid (from the Latin salix - willow). At the end of the 19th century, the production of salicylic acid and acetylsalicylic acid (ASA) began in Germany. Currently, more than 20 different representatives of this group are known in clinical practice, differing in chemical structure, features of the mechanism of action, indications for use and tolerability.

Mechanism of action of NSAIDs.

NSAIDs inhibit the synthesis of prostaglandins (PGs), which are important physiological and pathological mediators.
PGs are involved in processes such as pain, inflammation, tumorigenesis, osteoporosis, regulation of body temperature (hyperthermia) and kidney function, etc. From arachidonic acid, with the participation of the enzyme cyclooxygenase (COX), PGH2 is formed, which is the precursor of PGs such as thromboxane (TxA2), prostacyclin, or PGI2, D2, E2 and F2 (see figure).

Figure 1. Mechanism of action of NSAIDs [2, 3]. Two main isoforms of COX are known: COX-1 and COX-2. The issue of isolating the third isoform, COX-3, as a variant of COX-1 under experimental conditions, remains unresolved [1]. The first isoform (COX-1) is synthesized constantly and works according to a universal mechanism, i.e. regardless of in which organ or tissue the synthesis occurs. The synthesis of the second isoform (COX-2) is stimulated by various inflammatory factors (lipopolysaccharides, interleukins, tumor necrosis factor α) in various cells of the human body, such as endothelium, osteoclasts, synoviocytes, monocytes and macrophages [2].

The main pharmacodynamic properties of NSAIDs - anti-inflammatory, antipyretic and analgesic effects - are achieved through inhibition of COX-1 and COX-2. It is the inhibition of COX-1 and COX-2 that causes the main adverse reactions associated with the use of NSAIDs. Prostaglandins PGE2 and PGI2, which are synthesized with the participation of COX-1 in the gastrointestinal tract (GIT), are cytoprotectors of the mucous membrane by reducing the secretion of hydrochloric acid by parietal cells of the stomach, improving blood flow and stimulating mucus production. In addition, with the participation of COX-1, TxA2 is synthesized in platelets, which have vasoconstrictive and proaggregant properties. NSAIDs, by blocking the synthesis of COX-1, can lead to damage to the mucous membrane of the stomach and intestines and disruption of platelet aggregation. Thus, NSAIDs increase the risk of developing severe gastrointestinal diseases such as inflammation, bleeding and penetration of the stomach or intestines. The risk of developing such complications is higher in older people and does not depend on the duration of drug use [4].

The classification of NSAIDs is presented in table. 1.

Among representatives of NSAIDs, there are differences in the chemical structure, features of action and the degree of inhibition of COX-1 and COX-2.
The selectivity of NSAIDs for COX isoforms is usually assessed by the ratio of the degree of inhibition of COX-1 to COX-2 (selectivity coefficient). Selective COX-2 inhibitors are those NSAIDs that have this coefficient of more than 5, highly selective inhibitors - if this coefficient is more than 50 (see Table 1)
. NSAIDs with high selectivity for COX-2 are called coxibs (from the English - cyclo-oxygenase, abbreviated version of COX).

Clinical pharmacology of ibuprofen.

One of the NSAIDs widely used in clinical practice is ibuprofen, which was synthesized by S. Adams and D. Nicholson in Great Britain in 1962. In the Russian Federation it is registered under the trade name Nurofen (original drug). It has pronounced anti-inflammatory, analgesic and antipyretic effects, which, combined with good tolerability, predictability of side effects and low risk of complications, has led to its widespread use in clinical practice.

According to the chemical structure, ibuprofen is a derivative of propionic acid; according to the mechanism of action, it is a non-selective inhibitor of COX-1 and COX-2, lipoxygenase involved in the synthesis of pro-inflammatory leukotrienes [6].

Ibuprofen is a racemic mixture of two optical left- and right-handed isomers, the S (+) and R (–) enantiomers. The clinical effectiveness of ibuprofen is mainly due to the action of the S (+) form, but the presence of the R (–) isomer explains some of the anti-inflammatory properties of ibuprofen [7].

Variety of dosage forms of ibuprofen.

Modern possibilities for the use of ibuprofen are associated with advances in the field of pathophysiology of diseases and the development of new dosage forms of this drug. Currently, ibuprofen is presented in a variety of dosage forms on the drug market.

Not only oral administration of ibuprofen is possible, but also its topical use in the form of a gel, rectal (in the form of suppositories) and parenteral (in the form of solutions for intravenous administration) (Table 2).

Modern technologies have made it possible to develop new dosage forms - capsules containing ibuprofen solution (Nurofen Ultracap) and ibuprofen derivatives - sodium dihydrate and lysinate. The advantages of the lysine salt of ibuprofen are the speed of dissolution of this compound, increased bioavailability and the speed of onset of maximum concentration in the blood plasma (Nurofen Express) [8-10].

In clinical practice, new dosage forms with modified release are also presented, i.e. with a mechanism and nature of release of the drug substance changed in relation to the usual form. Forms of ibuprofen are known as immediate release (IR) and sustained release (SR).

Pharmacokinetics of ibuprofen.

The main pharmacokinetic parameters of ibuprofen, in particular the concentration of enantiomers in plasma or the area under the pharmacokinetic curve, depend on the dosage form and dose of ibuprofen
(see Table 2)
.

When taken orally, ibuprofen is rapidly absorbed from the upper small intestine. The bioavailability of ibuprofen as a weak acid when taken orally averages 80%. Eating generally reduces the rate of absorption of ibuprofen, but certain foods and drinks (eg, Coca-Cola) have been shown to increase the rate of absorption. The time to reach the maximum concentration of ibuprofen isomers in plasma or serum averages 1-2 hours and depends on the dosage form of ibuprofen (see Table 2)

. Based on the rate of absorption, dosage forms of ibuprofen can be distributed in ascending order: ibuprofen tablets → ibuprofen suspension → ibuprofen solution. Rapid absorption of ibuprofen from liquid forms (suspension, solution) provides a faster analgesic and antipyretic effect.

After oral administration of 40-60% of the R (-) form, ibuprofen is metabolized in the intestines and liver into the S (+) form. Further biotransformation of ibuprofen takes place in 2 phases. I - phase of oxidative reactions is associated with a system of microsomal enzymes of cytochrome P-450 (2C9, 2C8 and 2C19), which ensure the formation of inactive carboxyl and phenolic compounds. Differences in genotypes of the P-450 2C9 system lead to differences in the metabolism of ibuprofen, an increase in the area under the pharmacokinetic curve and changes in hepatic clearance [7]. Phase II of ibuprofen metabolism includes the formation of inactive glucuronic and taurine compounds, which are subsequently excreted primarily through the kidneys. Impaired liver function due to liver cirrhosis leads to a slower inversion of the R (–) form of ibuprofen to the S form (+), as well as an increase in half-life to 3.4 hours. Impaired renal function also reduces the rate of elimination of ibuprofen metabolites.

Ibuprofen has a high degree of binding to plasma albumin (90-99%). In adults, ibuprofen, when taken orally and intravenously, has a short half-life of about 2 hours. Ibuprofen penetrates well into the synovial fluid of inflamed joints, which provides analgesic and anti-inflammatory effects. The antipyretic effect of ibuprofen is due to inhibition of PGE2 synthesis in the central nervous system. Ibuprofen is a lipophilic substance, but only its free (not bound to albumin) fraction penetrates the blood-brain barrier.

With topical application of ibuprofen, there is a slight decrease in the systemic bioavailability of the drug to 14-30% of that when taken orally [12], while after topical application, higher concentrations are observed in subcutaneous and soft tissues, including muscle [13]. A number of studies in patients of different categories have shown that the effectiveness of topical application of ibuprofen (5% gel) and ibuprofen (1200 mg/day) taken orally both for acute traumatic injuries of soft tissues and for chronic pain syndrome is the same, and the tolerability of topical forms is better [12, 14, 15].

The pharmacokinetic curve indicators for rectal use are comparable to the pharmacokinetic data for oral administration of the drug. Absorption during rectal administration of ibuprofen is characterized by a high degree of bioavailability and rapid onset of maximum plasma concentration. In addition, the peculiarities of the blood supply to the rectal area lead to the fact that only part of the drug is metabolized in the liver, which leads to an increase in the half-life.

Pharmacokinetics indicators do not differ significantly between men and women, and in different age groups. Pharmacokinetic parameters in children over 2 years of age and adolescents do not differ from those in adults. The only exceptions are children under 2 years of age, whose metabolism of ibuprofen is significantly lower than that of adults, which requires the correct dosage regimen of the drug depending on the child’s body weight. With increasing age, there is a slight increase in half-life, which reflects age-related changes in metabolism and clearance, however, in older people, the elimination of ibuprofen does not undergo significant changes.

Safety of ibuprofen.

The development of selective COX-2 inhibitors was aimed at overcoming the limitations of the use of NSAIDs due to the risk of developing adverse gastrointestinal reactions. However, during the introduction of coxibs into clinical practice, another safety problem arose with long-term use - an increased risk of developing cardiovascular thrombotic complications, myocardial infarction and stroke [16]. The increase in the risk of thrombotic complications in the presence of selective COX-2 inhibitors is based on an imbalance between thromboxane and prostacyclin, which regulate endothelial function and platelet aggregation. Selective coxibs, due to the selective blockade of COX-2, upset the balance between the levels of thromboxane and prostacyclin, which is the basis for the development of thrombotic complications [2]. However, the results of subsequent clinical observations showed that the use of non-selective NSAIDs also increases the risk of developing cardiovascular complications [17, 18]. Current international recommendations, based on the results of long-term clinical studies, limit the use of both coxibs and non-selective NSAIDs in patients with coronary heart disease (CHD), stroke, or at high risk of developing CHD [3, 5].

Another undesirable reaction due to long-term use of NSAIDs is impaired renal function, since both COX isoforms play a significant role in the regulation of kidney function. PGs regulate vascular tone and maintain normal blood flow, which is necessary to maintain normal kidney function. It is now known that inhibition of COX-1 leads to a decrease in glomerular filtration rate, and inhibition of COX-2 slows down sodium reabsorption in healthy volunteers and elderly people. According to a meta-analysis, selective COX-2 inhibitors increase the risk of developing renal failure and arrhythmia [2, 19].

Ibuprofen has an extensive evidence base for safety, due to which it is available over-the-counter (in dosages less than 1200 mg) in many countries around the world.

The safety of ibuprofen has been demonstrated in many large clinical studies. Of greatest interest is a multicenter randomized study conducted in 1999 in France with the participation of 8677 patients (PAIN study), the purpose of which was to compare the effectiveness and tolerability of over-the-counter analgesics: ASA, paracetamol and ibuprofen. It has been shown that ibuprofen (at a dose of less than 1200 mg) is tolerated as well as paracetamol, which was previously considered the standard of safety, and compared to ASA, it causes a significantly lower incidence of adverse reactions [20].

When comparing the frequency of adverse gastrointestinal reactions, it was noted that ibuprofen is characterized by high safety due to the presence of a low-active enantiomer R, which competes with the active form S for the active center of COX-1, which is responsible for the synthesis of PGs, which provide protection to the gastrointestinal mucosa. In addition, the short half-life of ibuprofen may also provide safety advantages for this drug.

Ibuprofen does not form toxic metabolites, its toxicity after accidental or intentional overdose is lower and it has a relatively higher therapeutic index (about 4 times higher than paracetamol). The development of Reye's syndrome (acute hepatic encephalopathy in children while taking ASA) is also uncharacteristic of ibuprofen [14, 21].

Clinical effectiveness of ibuprofen.

Ibuprofen is an effective analgesic for acute pain syndrome of various origins. At a dose of 400 mg, it has repeatedly proven its advantage over placebo in postoperative, toothache, sore throat, dysmenorrhea, tension headaches and migraines, soft tissue trauma, neuralgia and myalgia, as well as a number of other conditions accompanied by severe pain.

For headaches, ibuprofen as a first-line drug is included in the list of analgesics recommended by WHO, as well as the European Federation of Neurological Societies (EFNS) for the treatment of mild to moderate migraine attacks (class A) [22, 23]. The effectiveness of ibuprofen in the treatment of cephalgia has been proven in many placebo-controlled clinical trials, as well as several meta-analyses, including in children and adolescents [24-28].

At a dose of 200-400 mg, ibuprofen is the “gold standard” for the treatment of moderate pain in people with postoperative dental pain [29]. A meta-analysis demonstrated the high effectiveness of ibuprofen compared with placebo across 72 studies. Ibuprofen significantly reduced pain in all patients - by at least 50% for an average of 4.7 hours. Repeated analgesia was required in only 48% of patients taking ibuprofen at a dose of 200 mg, and in 42% - at a dose of 400 mg [30] . Another meta-analysis based on 33 studies found an advantage of ibuprofen (400 mg) in relieving pain after tooth extraction compared to paracetamol (1000 mg), as well as a combination of paracetamol (600-650 mg) and codeine (60 mg) [31].

The issue of choosing an effective and safe NSAID in pediatric practice is especially acute, due to the fact that fever and pain are leading in a number of diseases, including respiratory infections, which are most common in young children. Large multicenter randomized studies have shown that among all analgesic-antipyretic drugs, ibuprofen and paracetamol are the safest drugs. Thus, a meta-analysis combining 24 randomized and 12 observational studies from 1950 to 2008 did not show statistically significant differences in the incidence of adverse reactions of the gastrointestinal tract and kidneys, as well as in the effect on the course of bronchial asthma when taking ibuprofen, paracetamol and placebo [32]. The largest systematic review of data on the effectiveness and safety of ibuprofen compared with paracetamol in the treatment of fever and pain in children and adults was conducted in 2010. It included 85, including large randomized trials in the period 2008-2009. The authors concluded conclusion that ibuprofen is more effective than paracetamol in the treatment of fever and pain in all age groups with equal safety [33].

According to WHO recommendations, ibuprofen at a dose of 5-10 mg/kg, along with paracetamol, is the drug of choice as an antipyretic and analgesic (for mild to moderate pain) in children from 3 months. No other NSAIDs can be recommended for use in pediatric practice due to the lack of the necessary evidence base for their effectiveness and safety [34, 35].

Currently, ibuprofen is also the only drug listed by the WHO for the treatment of patent ductus arteriosus in newborns [36]. Potential new indications for the use of ibuprofen are being studied.

Cystic fibrosis.

Several clinical studies have demonstrated the effect of ibuprofen on slowing the progression of the pulmonary process (slowing the decline in forced expiratory volume in 1 second) in patients with cystic fibrosis with long-term use in various age groups [37-39]. The results obtained are likely due to a decrease in the influx of polymorphonuclear cells into the lungs and, consequently, the inflammatory process [40]. Despite the fact that large doses of ibuprofen were used, the risk of developing adverse gastrointestinal reactions remained low [37, 38].

Parkinson's disease.

It is believed that one of the key links in the pathogenesis of Parkinson's disease is neuroinflammation. Based on this assumption, several studies have been conducted to determine the role of NSAIDs in the development of the disease. A 2010 meta-analysis of 7 large epidemiological studies demonstrated a reduction in the risk of developing Parkinson's disease by 15% in the overall group of patients taking NSAIDs, and by 29 and 21%, respectively, with regular and long-term use of NSAIDs. The strongest neuroprotective effect was observed with ibuprofen, which was confirmed by a number of other studies [41–43].

Mammary cancer.

Currently, there is great interest in the positive effects of NSAIDs, primarily ASA and ibuprofen, on the risk of developing various types of cancer [44–46]. Based on the results of a meta-analysis (38 studies, n=2,788,715), conclusions were drawn about the possible oncoprotective effect of NSAIDs, primarily ibuprofen (relative risk 0.79 with a 95% confidence interval from 0.64 to 0.97) in relation to the development of breast cancer [ 47]. Another meta-analysis (26 studies, n=528,705) showed similar results [48]. Perhaps, after large placebo-controlled studies, the use of ibuprofen will be recommended as a preventive measure for cancer.

Thus, when prescribing therapy, it is important to choose a time-tested remedy. More than 40 years of experience with the use of ibuprofen in widespread clinical practice in almost 80 countries as an over-the-counter drug is a clear example of its effectiveness and safety [49].

Overdose

Overdose is accompanied by:

• abdominal pain;
• lethargy;
• nausea/vomiting;
• tinnitus;
• drowsiness;
• headache;
• depression;
• metabolic acidosis;
• coma;
• surge arrester;
• bradycardia;
• hypotension;
• atrial fibrillation;
• stopping breathing.

Treatment: gastric lavage (advisable within 1 hour after taking the drug), administration of enterosorbents, forced diuresis, abundant alkaline drinking, symptomatic therapy, the purpose of which is the correction of gastric and intestinal bleeding, blood pressure, blood pressure levels, etc.

Interaction

Drugs that induce microsomal oxidation increase the production of hydroxylated active metabolic products and thus increase the risk of developing serious hepatotoxic reactions. Drugs that inhibit microsomal oxidation, on the contrary, reduce it.

Ibuprofen reduces the sodium and diuretic activity of hydrochlorothiazide and Furosemide , the effectiveness of antihypertensive and uricosuric drugs (including ACE inhibitors and BMCC), and the antiplatelet and anti-inflammatory effects of ASA.

Potentiates the effect of antiplatelet agents, indirect anticoagulants, fibrinolytics, Insulin and oral forms of hypoglycemic drugs, ulcerogenic effect with bleeding of GCS and MCS.

Absorption of the drug is reduced in combination with cholestyramine and antacids. Caffeine enhances the analgesic effect . In combination with thrombolytics and anticoagulants, it increases the risk of bleeding.

Cefotetan , Cefoperazone , Cefamandole , Plicamycin and valproic acid prothrombin (clotting factor) deficiency

Myelotoxic drugs enhance the hematotoxicity of Ibuprofen. The drugs Au and Cyclosporine enhance the effect of the drug on the synthesis of Pg in the kidneys, resulting in increased nephrotoxicity. In turn, Ibuprofen increases the concentration of Cyclosporine in the blood plasma and its hepatotoxicity.

Drugs that block tubular secretion increase the concentration of ibuprofen in the blood plasma and reduce its excretion.

special instructions

In case of severe pathologies of the musculoskeletal system, it is advisable to combine external therapy with oral forms of NSAIDs.

During the period of use of Ibuprofen, it is necessary to monitor changes in renal/liver function and peripheral blood patterns.

If signs of NSAID gastropathy , the patient requires a blood test to determine the hematocrit number and Hb, a stool test for occult blood, and esophagogastroduodenoscopy. To prevent the development of gastropathy , Ibuprofen should be combined with PgE medications.

If it is necessary to determine 17-KS, the drug is discontinued 48 hours before the study.

Patients taking Ibuprofen should refrain from any activity that requires high concentration and speed of mental/motor reactions.

It should be remembered that this remedy should be used in the minimum effective dose and for the shortest possible course to reduce the likelihood of developing undesirable reactions from the digestive system.

Ibuprofen analogs

Level 4 ATC code matches:
Artrum

Brustan

Ketonal Duo

Nurofen Plus

Nurofen Express

Nurofen Forte

Nurofen Express Lady

Nurofen for children

Nurofen

Ibuprom

Advil

MIG 400

Has

Ketoprofen

Vimovo

Naproxen

Flexen

Nalgesin

Flamax

Novigan

Synonyms (analogs of Ibuprofen with the same active ingredient):

• Ibuprofen-Hemofarm
• Nurofen
• MIG 400
• Ibuprom
• Faspik
• Solpaflex
• Advil

Generic dosage forms for external therapy are the following drugs:

• Dolgit
• Ibalgin
• Nurofen
• Ibuprofen-Verte

Ibuprofen or Nurofen - which is better?

Nurofen is a medicine based on ibuprofen. That is, the drugs are generics. They are distinguished from each other by manufacturer, price and composition of auxiliary components.

Ibuprofen during pregnancy and lactation

Ibuprofen is the drug of choice for pain and fever during pregnancy, since during this period of time it is safer for the woman’s body than most other analgesics and antipyretics.

In the first 2 trimesters of pregnancy, it does not have a negative effect on the development of the fetus, does not provoke bleeding (unlike Aspirin ) and does not create a threat of miscarriage.

In the last trimester of pregnancy, taking Ibuprofen is contraindicated.

Firstly, the drug inhibits the contraction of the uterine muscles. Secondly, its use can cause closure of the ductus botellus and the development of pulmonary hypertension in a child. Thirdly, the medicine tends to block the hormones responsible for the birth process.

Ibuprofen during breastfeeding does not affect the quality and secretion of milk, therefore it can be used to treat nursing women.

"IBUPROFEN" (injections): instructions for use

Remember that you need to use the injection correctly, otherwise the chemical material will have an incorrect effect on the patient’s health and will worsen it. If the dosage is insufficient, nothing will happen, pain and inflammation will remain unchanged.

How to take it correctly?

1. The form in which the manufacturer produces the product is injection for internal use. The substance is prepared in ampoules, each containing 2 ml of injection. There are 5 ampoules in total in the package with instructions for use;
2. Algorithm of action - there are several ways to administer the drug. For both cases you will need a syringe and one injection ampoule;
3. There is only one way. Shake the syringe before injecting it. It must be injected into the muscle, next to the spine, into the shoulder blade if there is no fat layer there;
4. Method two. Shake the injection again before taking and inject into the syringe. It is advisable to perform this action by a doctor, because the substance must be injected into the epidural canal;
5. Injections are contraindicated for pregnant women, breastfeeding women and children under 12 years of age.

Reviews of Ibuprofen

It is probably impossible to find bad reviews about Ibuprofen in tablets, suppositories or syrup. The drug is considered to be an effective and fairly safe remedy.

Its advantages are:

• possibility of use for the treatment of pregnant women and children of any age;
• a large number of dosage forms (this allows you to correctly select the minimum effective dose);
• low price;
• quick effect.

As disadvantages, reviews usually mention the presence of contraindications and the risk of developing side effects characteristic of NSAIDs.

Reviews of doctors about the ointment/gel allow us to conclude that for postoperative and post-traumatic pain, as well as for pain caused by severe hypothermia, drugs containing NSAIDs are the most fast-acting and effective.

However, they should be used in short courses and not exceeding the dose recommended by the instructions.

Ibuprofen price, where to buy

The price of Ibuprofen in tablets is from 40 to 100 rubles. How much tablets cost depends on their quantity in the package and the manufacturer’s pricing policy. Syrup can be bought for 100 - 150 rubles. The price of Ibuprofen ointment is from 40 rubles, the price of Ibuprofen gel is from 70 rubles. Candles for children cost an average of 80 rubles (package No. 10).

The average cost of Ibuprofen tablets in Kharkov, Kyiv and other cities of Ukraine is about 30 UAH, suspensions are about 100 UAH, for ointment and gel the price varies from 30 to 50 UAH.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Ibuprofen-AKOS tab.
  p/o captivity. 400 mg 20 pcs Biosynthesis OJSC 62 rub. order
• Ibuprofen Welfarm tab. p/o captivity. 400 mg No. 20Velfarm LLC

  RUB 214 order

• Ibuprofen Susp. for internal approx. 100mg/5ml 100ml JSC Ecolab

  82 RUR order

• Ibuprofen Susp. d/reception internal. for children (from 3 months) without sugar 100 mg/5 ml fl. 100ml No. 1 strawberryPharmstandard-Leksredstva OJSC

  90 rub. order

• Ibuprofen capsules 200 mg 20 pcs. JSC Medisorb

  145 rub. order

Pharmacy Dialogue

• Ibuprofen Welfarm (tab.p.pl.vol. 400 mg No. 50) Welfarm LLC

  RUB 298 order

• Ibuprofen 5% gel tube 50gVertex

  92 rub. order

• Ibuprofen gel (tube 5% 50g)Ozone LLC

  79 RUR order

• Ibuprofen Welfarm (tab.p.pl/vol. 400 mg No. 10) Welfarm LLC

  111 rub. order

• Ibuprofen (susp. 100 mg/5 ml vial 100 ml (orange)) Synthesis OJSC

  96 RUR order

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Pharmacy24

• Ibuprofen-Darnitsa 200 mg No. 20 tablets PrAT" Pharmaceutical company "Darnitsa", Ukraine
  15 UAH. order
• Ibuprofen-Darnitsa 0.2 g No. 50 tablets PrAT” Pharmaceutical company “Darnitsa”, Ukraine

  28 UAH order

• Ibuprofen 200 mg N50 tablets PAT"Vitamin" Ukraine

  27 UAH order

• Ibuprofen 200 mg No. 50 tablets PrAT "Technolog", Uman, Cherkasy region, Ukraine

  22 UAH order

• Ibuprofen 200 mg No. 50 tablets PAT NEC "Borshchagivsky chemical and pharmaceutical plant", Kiev, Ukraine

  24 UAH order

PaniPharmacy

• Gel Ibuprogel for joints ibuprofen with bodyaga 75 ml Ukraine, Euro plus state of emergency

  32 UAH order

• IBUPROFEN tablets Ibuprofen-Darnitsa tablets 0.2g No. 50 Ukraine, Darnitsa ChAO

  28 UAH order

• Ibuprofen tablets Ibuprofen tablets. p/o 200 mg No. 50 Ukraine, Tekhnolog ChAO

  25 UAH order

• IBUPROFEN tablets Ibuprofen tablets. 0.2g No. 20 Ukraine, Darnitsa ChAO

  16 UAH order

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"IBUPROFEN" (injections): price

To assess the quality of a medicine, you need to choose the right pharmacy where the conditions for purchase will be the most favorable. Beware of various medical stalls of dubious content, as well as pharmacies where previously unsuccessful products were purchased. As an option for good pharmaceutical boutiques, we can offer:

• In Farmani it is possible to find an injection costing 100 rubles;
• Maksavit offers its customers a price of 90 rubles;
• For visitors to the State Pharmacy, the cost of injections varies from 80 to 110 rubles;
• ASNA has a price category of 105 rubles.