Floxel: Full Drug Profile

Floxel - General Information

An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. [PubChem]

Pharmacology of Floxel

Floxel, a cyclic amine, is a synthetic antiviral drug and a derivate of adamantane, like a similar drug amantadine. Floxel 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. Floxel has little or no activity against influenza B virus. Floxel does not appear to interfere with the immunogenicity of inactivated influenza A vaccine.

Floxel for patients

Floxel 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.

Floxel Contraindications

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

Additional information about Floxel

Floxel 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. Floxel 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.

Generic Name

Rimantadine

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 Floxel

Tablet, film coated 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