pharmacopeia

Mechanism of action

Sourced from openFDA

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.

M2 Protein

Indications

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  • Rimantadine hydrochloride tablet is indicated for the prophylaxis and treatment of illness caused by various strains of influenza A virus in adults (17 years and older). Rimantadine hydrochloride tablet is indicated for prophylaxis against influenza A virus in children (1 year to 16 years of age).ICD-10: J11.1

Contraindications

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  • Rimantadine hydrochloride tablet is contraindicated in patients with known hypersensitivity to drugs of the adamantane class, including rimantadine and amantadine.contraindicated

Dosage & administration

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For Prophylaxis in Adults and Children Adults (17 years and older) The recommended adult dose of rimantadine hydrochloride is 100 mg twice a day. Study durations ranged from 11 days to 6 weeks in adult and elderly patients. In patients with severe hepatic dysfunction, severe renal impairment (CrCl 5 to 29 mL/min) or renal failure (CrCl ≤ 10 mL/min) and in elderly nursing home patients, a dose reduction to 100 mg daily is recommended. Because of the potential for accumulation of rimantadine metabolites during multiple dosing, patients with hepatic or renal impairment should be monitored for adverse effects. Children (1 year to 16 years of age) Study duration ranged from 5 weeks to 6 weeks in pediatric subjects. In children 1 year to 9 years of age, rimantadine hydrochloride should be administered once a day, at a dose of 5 mg/kg but not exceeding 150 mg. For children 10 years of age or older, use the adult dose. (see Directions for Compounding of an Oral Suspension from Rimantadine Hydrochloride Tablets to prepare an oral suspension for administration to children and patients with difficulty swallowing tablets). Children (Birth to 11 months) The safety and efficacy of rimantadine hydrochloride for prophylaxis of influenza in pediatric patients younger than 1 year of age have not been established. For Treatment in Adults Adults (17 years and older) The recommended adult dose of rimantadine hydrochloride is 100 mg twice a day for 7 days.

Adverse reactions

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In 1,027 patients treated with rimantadine hydrochloride in controlled clinical trials at the recommended dose of 200 mg daily, the most frequently reported adverse events involved the gastrointestinal and nervous systems. Incidence >1%: Adverse events reported most frequently (1 % to 3%) at the recommended dose in controlled clinical trials are shown in the table below. Rimantadine (n=1,027) Control (n=986) Nervous System Insomnia 2.1% 0.9% Dizziness 1.9% 1.1% Headache 1.4% 1.3% Nervousness 1.3% 0.6% Fatigue 1.0% 0.9% Gastrointestinal System Nausea 2.8% 1.6% Vomiting 1.7% 0.6% Anorexia 1.6% 0.8% Dry mouth 1.5% 0.6% Abdominal Pain 1.4% 0.8% Body as a Whole Asthenia 1.4% 0.5% Less frequent adverse events (0.3 to 1%) at the recommended dose in controlled clinical trials were: Gastrointestinal System: diarrhea, dyspepsia; Nervous System: impairment of concentration, ataxia, somnolence, agitation, depression; Skin and Appendages: rash; Hearing and Vestibular: tinnitus; Respiratory: dyspnea. Additional adverse events (less than 0.3%) reported at recommended doses in controlled clinical trials were: Nervous System: gait abnormality, euphoria, hyperkinesia, tremor, hallucination, confusion, convulsions; Respiratory: bronchospasm, cough; Cardiovascular: pallor, palpitation, hypertension, cerebrovascular disorder, cardiac failure, pedal edema, heart block, tachycardia, syncope; Reproduction: non-puerperal lactation; Special Senses: taste loss/change, parosmia.

Use in specific populations

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Pregnancy Teratogenic Effects : There are no adequate and well-controlled studies in pregnant women. Rimantadine is reported to cross the placenta in mice. Rimantadine has been shown to be embryotoxic in rats when given at a dose of 200 mg/kg/d (11 times the MRHD based on mg/m 2 ). At this dose the embryotoxic effect consisted of increased fetal resorption in rats; this dose also produced a variety of maternal effects including ataxia, tremors, convulsions and significantly reduced weight gain. No embryotoxicity was observed when rabbits were given doses up to 50 mg/kg/d (approximately 0.1 times the MRHD based on AUC), but evidence of a developmental abnormality in the form of a change in the ratio of fetuses with 12 or 13 ribs were noted. This ratio is normally about 50:50 in a litter but was 80:20 after rimantadine treatment. However, in a repeat embryofetal toxicity study in rabbits at doses up to 50 mg/kg/d (approximately 0.1 times the MRHD based on AUC), this abnormality was not observed. Nonteratogenic Effects: Rimantadine was administered to pregnant rats in a peri- and postnatal reproduction toxicity study at doses of 30 mg/kg/d, 60 mg/kg/d and 120 mg/kg/d (1.7, 3.4 and 6.8 times the MRHD based on mg/m 2 ).

Pharmacokinetics

Sourced from openFDA
Metabolism
Although the pharmacokinetic profile of rimantadine hydrochloride has been described, no pharmacodynamic data establishing a correlation between plasma concentration and its antiviral effect are available. Rimantadine hydrochloride is absorbed after oral administration.

Overdosage

Sourced from openFDA

As with any overdose, supportive therapy should be administered as indicated. Overdoses of a related drug, amantadine, have been reported with adverse reactions consisting of agitation, hallucinations, cardiac arrhythmia and death. The administration of intravenous physostigmine (a cholinergic agent) at doses of 1 to 2 mg in adults (Ref. 7) and 0.5 mg in children (Ref. 8) repeated as needed as long as the dose did not exceed 2 mg/hour has been reported anecdotally to be beneficial in patients with central nervous system effects from overdoses of amantadine.

Approval history

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  • Aug 30, 2002ANDAANDA076132Impax Labs

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
26 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective415%
  2. 2Malaise312%
  3. 3Convulsion27.7%
  4. 4Drug Resistance27.7%
  5. 5Febrile Neutropenia27.7%
  6. 6Hyperhidrosis27.7%
  7. 7Hyperkalaemia27.7%
  8. 8Myocardial Infarction27.7%
  9. 9Pneumocystis Jiroveci Pneumonia27.7%
  10. 10Pneumonia27.7%
  11. 11Staphylococcal Bacteraemia27.7%
  12. 12Abdominal Discomfort13.8%
  13. 13Abdominal Distension13.8%
  14. 14Abdominal Pain13.8%
  15. 15Abortion Spontaneous13.8%

Literature

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Recent PubMed references pinned to Rimantadine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 4 most recently updated of 4 ClinicalTrials.gov registrations naming Rimantadine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Rimantadine work?
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.
What is Rimantadine used for?
According to FDA labeling, Rimantadine carries indications including: Rimantadine hydrochloride tablet is indicated for the prophylaxis and treatment of illness caused by various strains of influenza A virus in adults (17 years and older). Rimantadine hydrochloride tablet is indicated for prophylaxis against influenza A virus in children (1 year to 16 years of age).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Rimantadine?
Rimantadine is classified as Cyclic amines, Influenza A M2 Protein Inhibitor, Ion Channel Interactions, M2 Protein Inhibitors, Cellular Synthetic Activity Alteration.
What are the brand names for Rimantadine?
Rimantadine is marketed under brand names including Flumadine.
What are the contraindications for Rimantadine?
Rimantadine labeling lists contraindications including: Rimantadine hydrochloride tablet is contraindicated in patients with known hypersensitivity to drugs of the adamantane class, including rimantadine and amantadine.. Always consult the full prescribing information and a clinician.
Note. Data for rimantadine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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