Ribavirin
Ribavirin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Ribavirin
ATX code: J05AB04
Active ingredient: ribavirin (ribavirin)
Producer: Ozon, LLC (Russia), Pranafarm (Russia), Valenta Pharmaceuticals, OJSC (Russia), Kanonpharma production, CJSC (Russia), Severnaya zvezda, CJSC (Russia), Pharmproject, AO (Russia), VERTEX, CJSC (Russia))
Description and photo update: 2019-20-08
Prices in pharmacies: from 106 rubles.
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Ribavirin is a drug with a pronounced antiviral effect, a broad spectrum of activity against various DNA and RNA viruses; synthetic analogue of nucleosides.
Release form and composition
- Tablets: flat-cylindrical with a chamfer and a line, from white to yellowish-white (10 or 20 pcs. In blister strip packs, 1, 2, 5, 10, 14, 20, 28, 50 or 100 contour packs in a cardboard box; 100 or 200 pcs. in polymer cans, 1, 2, 4, 10, 20, 30, 50 cans in a cardboard box; 50 pcs. in polymer cans, 1,2, 5, 10, 20, 30 or 50 cans in a cardboard box; for hospitals - from 1000 to 50,000 tablets per pack);
- Capsules: No. 0, cream-colored cap and body; content - powder or mixture of granules and powder from white to yellowish-white; compaction of the contents in the form of a capsule is permissible, when pressed, the formation disintegrates (5 or 6 pcs. in blisters, 1-10, 20, 40, 60, 80, 100, 800 blisters in a cardboard box; 10 pcs. in polymer containers, 1, 5, 10, 20 containers in a cardboard box; 10 pcs. In blisters, 2, 3, 4, 5, 6, 7, 9, 10, 20, 40, 60, 80, 100 or 800 blisters in a cardboard box; 10 pcs. in bottles, 1, 5, 10 or 20 bottles in a cardboard box; 12, 18, 20, 30, 36, 40, 45, 50, 60, 100, 120, 140, 180, 200 pcs. in polymeric containers, 1, 5, 10 or 20 containers in a cardboard box).
Composition of 1 tablet:
- Active ingredient: ribavirin - 200 mg;
- Auxiliary components: potato starch, microcrystalline cellulose, calcium stearate, povidone.
Composition of 1 capsule:
- Active ingredient: ribavirin - 200 mg;
- Auxiliary components: potato starch, microcrystalline cellulose, colloidal silicon dioxide, lactose monohydrate (milk sugar), magnesium stearate;
- Capsule body and cap: iron dye yellow oxide, titanium dioxide, gelatin - up to 100%.
Pharmacological properties
Pharmacodynamics
After oral administration, ribavirin easily penetrates into cells affected by the virus, and is rapidly phosphorylated by intracellular adenosine kinase into ribavirin tri-, di- and monophosphate - metabolites that have a pronounced antiviral effect (especially ribavirin triphosphate).
The mechanism of action of the drug is not fully established, but it is known for sure that it inhibits IMP dehydrogenase (inosine monophosphate dehydrogenase), as a result of which the level of intracellular guanosine triphosphate (GTP) is significantly reduced, which is accompanied by inhibition of the synthesis of viral RNA and virus-specific proteins. Ribavirin inhibits the replication of new viruses, thereby reducing viral load. The drug selectively inhibits RNA synthesis, that is, it does not suppress it in normally functioning cells.
Ribavirin is effective against many RNA and DNA viruses. The most sensitive to its action are DNA viruses virus of Marek's illness, Simplex herpes virus and poks-virus, RNA viruses RNA tumoral viruses, reoviruses, paramyxovirus (Nucasl's illness, epidemic parotitis, parainfluenza), influenza A and B.
DNA viruses Varicella Zoster, cow smallpox and pseudorabies, RNA viruses of Semlicy Forest, rhinovirus and enteroviruses are insensitive to the action of the drug.
Ribavirin is active against the hepatitis C virus, but its mechanism of action is not fully understood. Presumably, ribavirin triphosphate, which accumulates during phosphorylation, competitively inhibits the formation of guanosine triphosphate, thereby reducing the synthesis of viral RNA. It is also believed that the mechanism of action of ribavirin and alpha interferon against hepatitis C virus is due to increased phosphorylation of ribavirin by interferon.
Pharmacokinetics
After oral administration, ribavirin is rapidly absorbed from the gastrointestinal tract. Its bioavailability is> 45%. The substance is distributed in plasma, erythrocytes and secretions of the respiratory tract mucosa. The metabolite ribavirin triphosphate accumulates in large quantities in erythrocytes, reaches a plateau by the 4th day of taking the drug and persists for several weeks.
The volume of distribution is approximately 647–802 liters. The half-life is 3.7 hours. It binds slightly to plasma proteins.
When the drug is taken in a course, ribavirin in large quantities accumulates in the plasma. The ratio of indicators of its bioavailability (area under the curve "concentration - time", or AUC) with repeated and single doses is 6. With prolonged use of the drug, more than 67% of the concentration can be found in the cerebrospinal fluid.
The maximum plasma concentration (C max) reaches within 1–1.5 hours. The time to reach the therapeutic plasma concentration depends on the value of the minute blood volume.
The average value of the maximum plasma concentration is ~ 5 μmol / L at the end of the first week of taking the drug at a dose of 200 mg every 8 hours, ~ 11 μmol / L at the end of the first week of taking the drug at a dose of 400 mg every 8 hours.
Ribavirin is metabolized in the liver by phosphorylation to form active metabolites of ribavirin di-, mono- and triphosphate, which are then metabolized to 1,2,4-triazole carboxamide (amide hydrolysis to tricarboxylic acid and deribosylation to form a triazole carboxylic metabolite).
The drug is slowly excreted from the body. After a single dose of 200 mg of ribavirin, the half-life (T ½) from plasma is 1-2 hours, from erythrocytes - up to 40 days. After the end of the course of therapy T ½ - approximately 300 hours.
Ribavirin and its metabolites are excreted mainly in the urine, with feces - about 10%. For the first day, about 7% is excreted unchanged, about 10% in two days.
In patients with renal failure, due to a decrease in true clearance, C max and AUC increase. In hepatic insufficiency (classes A, B and C according to the Child-Pugh classification), the pharmacokinetic parameters of ribavirin do not change.
In the case of taking the drug with food containing fats, the C max and AUC of ribavirin increase by 70%.
Indications for use
According to the instructions, Ribavirin is indicated for use in chronic hepatitis C (CHC) in the following cases:
- Combined therapy with peginterferon alfa-2b or interferon alfa-2b in patients who have not previously been treated with these drugs;
- Exacerbation of the disease due to a course of monotherapy with peginterferon alfa-2b or interferon alfa-2b;
- Patient immunity to monotherapy with peginterferon alfa-2b or interferon alfa-2b.
Contraindications
Absolute:
- Severe depression with suicidal intentions;
- Chronic heart failure (CHF) IIb-III degree;
- Myocardial infarction;
- Severe anemia;
- Renal failure with creatinine clearance (CC) less than 50 ml / min;
- Severe liver failure;
- Autoimmune diseases (including autoimmune hepatitis);
- Decompensated liver cirrhosis;
- Diseases of the thyroid gland that do not respond to treatment;
- Pregnancy and breastfeeding period;
- Children and youth up to 18 years old;
- Hypersensitivity.
Relative (Ribavirin should be taken with caution):
- Decompensated diabetes mellitus, incl. accompanied by attacks of ketoacidosis;
- Chronic obstructive pulmonary disease (COPD);
- Pulmonary embolism;
- CHF I-IIa degree;
- Diseases of the thyroid gland, including thyrotoxicosis;
- Blood clotting disorders, myelodepression, thrombophlebitis, hemoglobinopathy (including thalassemia and sickle cell anemia);
- Depression, suicidal tendencies (history data inclusive);
- HIV infection (increased risk of lactic acidosis in the presence of combined highly active antiretroviral therapy);
- Reproductive age in women, because pregnancy is undesirable;
- Elderly age.
Instructions for the use of Ribavirin: method and dosage
Ribavirin tablets and capsules are taken orally, washed down with water, without chewing, at the same time with meals.
Recommended dosage regimen: 800-1200 mg per day, divided into 2 doses (morning and evening), in combination with interferon alfa-2b - 3 million IU subcutaneously 3 times a week or peginterferon alfa 2b - 1.5 μg / kg subcutaneously once a week.
The daily dose of ribavirin in combination with interferon alfa-2b, depending on the patient's body weight:
- <75 kg - 1000 mg (400 mg in the morning and 600 mg in the evening);
- ≥75 kg - 1200 mg (600 mg in the morning and 600 mg in the evening).
The daily dose of ribavirin in combination with peginterferon alfa-2b, depending on the patient's body weight:
- <65 kg - 800 mg (400 mg in the morning and 400 mg in the evening);
- 65-85 kg - 1000 mg (400 mg in the morning and 600 mg in the evening);
- ≥85 kg - 1200 mg (600 mg in the morning and 600 mg in the evening).
The duration of the course of therapy in various categories of patients:
- Previously untreated - 24 weeks or more;
- With hepatitis C virus genotype 1 - 48 weeks;
- Unresponsive to monotherapy with peginterferon alfa-2b or interferon alfa-2b, as well as in case of relapse - from six months to a year, depending on the clinical course of the disease and the response to treatment.
Side effects
- Nervous system: dizziness, headache, malaise, general weakness, insomnia, depression, asthenia, anxiety, irritability, emotional lability, nervousness, aggressive behavior, agitation, confusion; rarely - suicidal tendencies, tremors, increased smooth muscle tone, paresthesia, hypesthesia, hyperesthesia, fainting;
- Cardiovascular system: increase or decrease in blood pressure, bradycardia, palpitations, tachycardia, cardiac arrest;
- Hematopoietic organs: leukopenia, hemolytic anemia, thrombocytopenia, neutropenia, granulocytopenia; extremely rare - aplastic anemia;
- Respiratory system: pharyngitis, shortness of breath, cough, bronchitis, sinusitis, rhinitis, otitis media;
- Digestive system: perverted taste, decreased appetite, dry mouth, nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, pancreatitis, stomatitis, bleeding from the gums, glossitis, hyperbilirubinemia;
- Sensory organs: damage to the lacrimal gland, visual impairment, conjunctivitis, tinnitus, hearing impairment / loss;
- Musculoskeletal system: myalgia, arthralgia;
- Genitourinary system: menorrhagia, dysmenorrhea, amenorrhea, decreased libido, prostatitis;
- Skin and subcutaneous fat: "hot flashes";
- Hypersensitivity reactions: skin rash, urticaria, erythema, angioedema, bronchospasm, hyperthermia, anaphylaxis, erythema multiforme, photosensitivity, Lyell's syndrome, Stevens-Johnson syndrome;
- Other reactions: alopecia, hair loss, hair loss, dry skin, hypothyroidism, sweating, thirst, chest pain, mycoses, viral infections (including herpes), flu-like syndrome, lymphadenopathy.
Overdose
In case of an overdose, the severity of side effects may increase. You should stop taking Ribavirin and carry out symptomatic therapy.
special instructions
It is required to take into account the teratogenicity of ribavirin: men and women of reproductive age during the period of drug therapy and for 7 months after the end of treatment must use effective methods of contraception.
It is recommended to carry out the following laboratory tests before starting therapy, at 2 and 4 weeks, and then regularly the following laboratory tests: clinical blood test with counting the number of platelets and leukocyte formula, determination of liver function tests, electrolytes, creatinine concentration.
Acute manifestation of hypersensitivity reactions (angioedema, urticaria, bronchospasm, anaphylaxis) requires immediate discontinuation of the drug. At the same time, transient rashes cannot serve as a basis for interrupting therapy.
The maximum decrease in the hemoglobin content in the blood during therapy with ribavirin is mainly observed after 4-8 weeks from the beginning of the course. If the hemoglobin value is <110 g / l, the dose of ribavirin should be temporarily reduced by 400 mg per day; hemoglobin <100 g / l - the dose should be reduced to 50% of the original; hemoglobin ≤85 g / l, and ribavirin intolerance persists after dose adjustment - the drug should be discontinued.
Before starting treatment for hepatitis C, an assessment is made of the need for histological confirmation of the diagnosis (therapy for genotype 2 or 3 virus does not require a preliminary liver biopsy).
During therapy with ribavirin, patients experiencing drowsiness, fatigue, disorientation are advised to refrain from engaging in potentially hazardous activities that require a high speed of psychomotor reactions and increased concentration of attention, including from driving.
Application during pregnancy and lactation
During pregnancy and lactation, this antiviral agent is contraindicated.
Pediatric use
Ribavirin is contraindicated for use in children and adolescents (up to 18 years).
With impaired renal function
It is forbidden to prescribe the drug to patients with concomitant renal failure if creatinine clearance is less than 50 ml / min.
For violations of liver function
The drug is prohibited for use in patients with severe hepatic impairment, autoimmune hepatitis, decompensated liver cirrhosis.
Use in the elderly
Elderly patients should be careful during treatment.
Drug interactions
- Substances / preparations containing ions of aluminum and magnesium salts, simethicone - reduce the bioavailability of ribavirin, reducing the AUC by 14%, but this decrease is clinically insignificant;
- Interferon alfa-2b or peginterferon alfa-2b - have a synergistic effect;
- Zidovudine and / or stavudine - their phosphorylation decreases, this can lead to HIV viremia, and also require a change in the therapy regimen;
- Phosphorylated metabolites of purine nucleosides (including didanosine, abacavir) - ribavirin increases their concentration, as a result of which the risk of developing lactic acidosis increases;
- Cytochrome P 450 - does not affect the enzymatic activity of the liver;
- Foods high in fat - increases the bioavailability of ribavirin (C max and AUC increase by 70%).
Analogs
Analogues of Ribavirin are: Rebetol, Trivorin, Arviron, Ribavin, Virazol, Ribavirin-LIPINT, Ribavirin-FPO, Ribapeg, Vero-Ribavirin, Devirs, Ribamidil, Ribavirin Meduna.
Terms and conditions of storage
Store in a dry, dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Shelf life:
- Tablets - 4 years;
- Capsules - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ribavirin
In general, the reviews about Ribavirin are positive. Patients note its high antiviral effect against the hepatitis C virus.
There are some opinions that as monotherapy Ribavirin is ineffective, and in order to obtain a therapeutic effect, it is necessary to undergo combined treatment with interferon.
Many patients complain of the development of various side effects, mostly they were moderately expressed, and therefore did not require discontinuation of the drug.
The price of Ribavirin in pharmacies
Depending on the manufacturer of the drug, prices for Ribavirin can vary over a wide range. The cost of 200 mg capsules ranges from 119–286 rubles for 30 pcs. and 150-300 rubles - for 60 pcs. You can buy 200 mg tablets for about 145–279 rubles for a pack of 20 pcs., For 450–650 rubles for a pack of 60 pcs.
Ribavirin: prices in online pharmacies
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Drug name Price Pharmacy |
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Ribavirin 200 mg tablets 20 pcs. 106 RUB Buy |
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Ribavirin Canon 200 mg tablets 30 pcs. 139 RUB Buy |
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Ribavirin 200 mg capsule 30 pcs. RUB 350 Buy |
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Ribavirin caps. 200 mg 60 pcs. 582 r Buy |
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Ribavirin 200 mg capsule 60 pcs. 632 RUB Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
