Pharmacotherapeutic group: Antiviral drug.
ATX code: J05AC02
Pharmacological properties:
Pharmacodynamics
Rimantadine is an antiviral agent, an adamantane derivative; active against various shiampas of influenza A virus (especially type A2).
A weak base, the drug Rimantadine acts by increasing the pH of endosomes, which have a membrane of vacuoles that surround viral particles after their penetration into the cell. Preventing acidification in these vacuoles blocks the fusion of the viral membrane with the endosome membrane, thus preventing the transfer of viral genetic material into the cell cytoplasm. The drug Rimantadine also inhibits exit of viral particles from the cell, i.e. it interrupts transcription of the viral genome.
Pharmacokinetics
After oral administration, the drug Rimantadine is almost completely absorbed in the intestine.
Absorption is slow. Binding to plasma proteins is about 40%. Distribution volume: adults – 17-25 l/kg, children – 289 l/kg. Concentration in nasal secretion is 50% higher than plasma concentration. Maximal concentration of preparation Rimantadine in plasma (Сmax) when administered by 100 mg once daily – 181 ng/ml, by 100 mg twice daily – 416 ng/ml.
Metabolized in liver. Half-life period (T1/2) – 24-36 hours; excreted by kidneys – 15% unchanged, 75-85% – as metabolites.
The T1/2 in chronic renal insufficiency is increased twice. In patients with renal insufficiency and elderly patients it may accumulate in toxic concentrations if the dose is not corrected in proportion to the decrease of creatinine clearance.
Indications
Early treatment and prevention of influenza A in adults and children over 7 years old.
Active ingredient
Rimantadine
Composition
Active substance: rimantadine hydrochloride – 50.0 mg. Excipients: lactose monohydrate – 74.50 mg, potato starch – 22.57 mg, talc – 1.50 mg, calcium stearate – 1.43 mg.
How to take, the dosage
Orally (after meals) with water. Flu treatment should be started within 24-48 hours after the onset of symptoms. Adults on the first day, 100 mg 3 times a day; on the second and third days, 100 mg 2 times a day; on the fourth and fifth days, 100 mg once a day. On the first day of therapy it is possible to use the drug once in a dose of 300 mg. The course of treatment is 5 days. For children aged 7 to 10 years, 50 mg 2 times a day; 10 to 14 years – 50 mg 3 times a day; over 14 years – doses for adults. The course of treatment is 5 days. For flu prophylaxis: in adults, 50 mg once a day for up to 30 days; in children over 7 years of age, 50 mg once a day for up to 15 days, depending on the epidemiological situation. If after treatment there is no improvement or if symptoms worsen or new symptoms appear, consult a physician. Use the drug only according to the indications, the route of administration and the dosage indicated in the instructions. You should consult a doctor if symptoms worsen or do not improve after 2-3 days of treatment.
Interaction
When used concomitantly, rimantadine reduces the effectiveness of antiepileptic drugs.
Adsorbents, astringents and coating agents decrease absorption of rimantadine.
Means that acidify the urine (ammonium chloride, ascorbic acid) reduce the effectiveness of rimantadine (due to its increased excretion by the kidneys).
The agents that alkalize the urine (acetazolamide, sodium bicarbonate) increase its effectiveness (decrease its excretion by the kidneys).
Paracetamol and acetylsalicylic acid decrease Cmax of rimantadine by 11%.
Cimetidine decreases clearance of rimantadine by 18%.
Special Instructions
With caution use rimantadine in arterial hypertension, epilepsy (including anamnesis), atherosclerosis of cerebral vessels.
When using rimantadine an exacerbation of chronic comorbidities is possible. In elderly patients with arterial hypertension the risk of hemorrhagic stroke increases. In case of indications in the anamnesis of epilepsy and anticonvulsant therapy, during rimantadine use, the risk of epileptic seizure increases. In these cases, rimantadine is used in dose up to 100 mg/day concomitantly with anticonvulsant therapy.
In influenza caused by B virus, rimantadine has antitoxic effect.
The prophylactic administration is effective in contacts with ill people, in the spread of infection in closed groups and at high risk of the disease during the influenza epidemic. It is possible that viruses resistant to the drug may develop.
Contraindications
- acute liver disease,
- acute and chronic kidney disease,
- thyrotoxicosis,
- high sensitivity to rimantadine,
- pregnancy and lactation,
- children under 7 years of age,
- in lactase deficiency, lactose intolerance, lactose/isomaltose malabsorption syndrome (because the drug contains lactose.
- With caution: in arterial hypertension, atherosclerosis of cerebral vessels, hepatic failure, epilepsy, diseases of the gastrointestinal tract.
Side effects
Digestive system disorders: epigastric pain, flatulence, increased bilirubin level in blood, dry mouth, anorexia, nausea, vomiting, gastralgia.
CNS disorders: headache, insomnia, nervousness, dizziness, concentration disorders, drowsiness, anxiety, increased excitability, fatigue.
Others: allergic reactions.
Overdose
Symptoms: agitation, hallucinations, arrhythmia.
Treatment: gastric lavage, symptomatic therapy: measures to maintain vital functions. Rimantadine is partially excreted by hemodialysis.
Similarities
Remantadine, Orvirem, Rimantadine, Rimantadine Kids
Weight | 0.013 kg |
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Shelf life | 2 years. Do not use after the expiration date stated on the package. |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 ° C. Keep out of reach of children. |
Manufacturer | Pharmstandard-Leksredstva, Russia |
Medication form | pills |
Brand | Pharmstandard-Leksredstva |
Other forms…
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