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Active ingredient: Rimantadine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Antiviral Agents
  • Nucleic Acid Synthesis Inhibitors

Dosage Forms

  • Available as 100 mg film-coated tablets and as syrup for oral administration.

Brands / Synonyms

Flumadine; Levofloxacin hydrochloride; Rimantadine HCL

Indications

For the prophylaxis and treatment of illness caused by various strains of influenza A virus in adults.

Pharmacology

Rimantadine, a cyclic amine, is a synthetic antiviral drug and a derivate of adamantane, like a similar drug amantadine. Rimantadine is inhibitory to the in vitro replication of influenza A virus isolates from each of the three antigenic subtypes (H1N1, H2H2 and H3N2) that have been isolated from man. Rimantadine has little or no activity against influenza B virus. Rimantadine does not appear to interfere with the immunogenicity of inactivated influenza A vaccine.

Mechanism of Action

The mechanism of action of rimantadine is not fully understood. Rimantadine appears to exert its inhibitory effect early in the viral replicative cycle, possibly inhibiting the uncoating of the virus. Genetic studies suggest that a virus protein specified by the virion M2 gene plays an important role in the susceptibility of influenza A virus to inhibition by rimantadine.

Absorption

Well absorbed, with the tablet and syrup formulations being equally absorbed after oral administration.

Toxicity

Oral LD50 in rats is 640 mg/kg. Overdoses of a related rug, amantadine, have been reported with adverse reactions consisting of agitation, hallucinations, cardiac arrhythmia and death.

Biotrnasformation / Drug Metabolism

Following oral administration, rimantadine is extensively metabolized in the liver with less than 25% of the dose excreted in the urine as unchanged drug. Glucuronidation and hydroxylation are the major metabolic pathways.

Contraindications

Rimantadine HCl is contraindicated in patients with known hypersensitivity to drugs of the adamantine class, including rimantadine and amantadine.

Drug Interactions

Cimetidine: The effects of chronic cimetidine use on the metabolism of rimantadine are not known. When a single 100 mg dose of rimantadine HCl was administered one hour after the initiation of Cimetidine (300 mg four times a day), the apparent total rimantadine clearance of this single dose in normal healthy adults was reduced by 18% (compared to the apparent total rimantadine clearance in the same subjects in the absence of cimetidine).

Acetaminophen: Rimantadine HCl, 100 mg, was given twice daily for 13 days to 12 healthy volunteers. On day 11, acetaminophen (650 mg four times daily) was started and continued for 8 days. The pharmacokinetics of rimantadine were assessed on days 11 and 13. Coadministration with acetaminophen reduced the peak concentration and AUC values for rimantadine by approximately 11%.

Aspirin: Rimantadine HCl, 100 mg, was given twice daily fro 13 days to 12 healthy volunteers. On day 11, aspirin (650 mg, four times daily) was started and continued for 8 days. The pharmacokinetics of rimantadine were assessed on days 11 and 13. Peak plasma concentrations and AUC of rimantadine were reduced approximately 10% in the presence of aspirin.

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