Rimantadine is an antiviral agent, a derivative of adamantane; it is active against various strains of influenza A virus (especially type A2).
Being a weak base, rimantadine acts by increasing pH of endosomes – membrane vacuoles that surround viral particles after their penetration into the cell. Preventing acidification in these vacuoles blocks the fusion of the viral envelope with the endosome membrane, thus preventing the transfer of viral genetic material into the cell cytoplasm. Rimantadine also inhibits the exit of viral particles from the cell, i.e. it interrupts transcription of the viral genome.
Pharmacokinetics
After oral administration rimantadine is almost completely absorbed in the intestine. Absorption is slow. Binding with plasma proteins is about 40%. Volume of distribution: adults – 17-25 l/kg, children – 289 l/kg. Concentration in nasal secretion is 50% higher than in plasma.
Maximum concentration (Cmax) of active substance in plasma after a single dose of 100 mg once daily is reached after 6 hours and is 181 ng/ml, after 100 mg twice daily – 416 ng/ml. It is metabolized in the liver.
Half-life period is 24-36 hours (T1/2); 75-85% of dose is excreted by kidneys mainly as metabolites, 15% – unchanged. In chronic renal failure the half-life is increased by 2 times. In patients with renal insufficiency and elderly persons can accumulate in toxic concentrations if the dose is not corrected in proportion to the decrease in creatinine clearance (CC).
Indications
Active ingredient
Composition
How to take, the dosage
Interaction
Special Instructions
Contraindications
Side effects
Overdose
Symptoms: agitation, hallucinations, arrhythmia. In some cases, if the recommended dose is exceeded: tearfulness of the eyes and pain in the eyes, increased urination, fever, constipation, sweating, inflammation of the oral mucosa, dry skin.
Treatment: gastric lavage, symptomatic therapy. When poisoning it is necessary to maintain vital functions. Rimantadine is partially excreted by hemodialysis.
Pregnancy use
Similarities
Weight | 0.013 kg |
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Shelf life | 5 years. |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 ° C. |
Manufacturer | Update PFC AO, Russia |
Medication form | pills |
Brand | Update PFC AO |
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