Rimantadine HCL
Rimantadine HCL - General Information
An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. [PubChem]
Pharmacology of Rimantadine HCL
Rimantadine HCL, a cyclic amine, is a synthetic antiviral drug and a derivate of adamantane, like a similar drug amantadine. Rimantadine HCL 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 HCL has little or no activity against influenza B virus. Rimantadine HCL does not appear to interfere with the immunogenicity of inactivated influenza A vaccine.
Rimantadine HCL for patients
Rimantadine HCL 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.
Rimantadine HCL Contraindications
Rimantadine HCl is contraindicated in patients with known hypersensitivity to drugs of the adamantine class, including rimantadine and amantadine.
Additional information about Rimantadine HCL
Rimantadine HCL Indication: For the prophylaxis and treatment of illness caused by various strains of influenza A virus in adults.
Mechanism Of Action: The mechanism of action of rimantadine is not fully understood. Rimantadine HCL 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Rimantadine
Synonyms: Not Available
Drug Category: Antiviral Agents; Nucleic Acid Synthesis Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Rimantadine: Flumadine; Levofloxacin hydrochloride; Rimantadine HCL;
Absorption: Well absorbed, with the tablet and syrup formulations being equally absorbed after oral administration.
Toxicity (Overdose): 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.
Protein Binding: Approximately 40% over typical plasma concentrations.
Biotransformation: 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.
Half Life: 25 to 30 hours in young adults (22 to 44 years old). Approximately 32 hours in elderly (71 to 79 years old) and in patients with chronic liver disease. Approximately 13 to 38 hours in children (4 to 8 years old).
Dosage Forms of Rimantadine HCL: Tablet, film coated Oral
Syrup Oral
Chemical IUPAC Name: 1-(1-adamantyl)ethanamine
Chemical Formula: C12H21N
Rimantadine on Wikipedia: https://en.wikipedia.org/wiki/Rimantadine
Organisms Affected: Human Influenza A Virus