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|Rimantadine Hydrochloride

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Rimantadine Hydrochloride

Pronouncation: (rih-MAN-tuh-deen HIGH-droe-KLOR-ide)
Class: Antiviral agent

Trade Names:
Flumadine
- Syrup 50 mg/5 mL
- Tablets 100 mg

Mechanism of Action

Pharmacology

Inhibits viral replication cycle in various strains of influenza A virus.

Pharmacokinetics

Absorption

Well absorbed. C _max is 74 ng/mL (single dose). T _max is 6 hr (single dose).

Distribution

Protein binding is 40%, mainly albumin.

Metabolism

Extensively metabolized in the liver to 3 hydroxylated metabolites.

Elimination

Eliminated in the urine (less than 25% as unchanged drug). T _½ is 25.4 hr (single dose) and 32 hr (elderly older than 70 yr).

Special Populations

Renal Function Impairment

Apparent clearance for Ccr 31 to 50 mL/min was 37% lower; apparent clearance for Ccr 11 to 30 mL/min was 16% lower and plasma metabolite concentrations were higher; apparent clearance for Ccr 0 to 10 mL/min was 40% lower with a 1.6-fold increase in elimination half-life.

Elderly

In patients older than 70 years of age, the average AUC, peak concentrations, and elimination half-life at steady state were 20% to 30% higher.

Severe hepatic insufficiency

AUC was about 3–fold larger, elimination half-life was about 2-fold longer, and the apparent clearance was 50% lower.

Indications and Usage

Adults

Prophylaxis and treatment of infection caused by various strains of influenza A virus.

Children

Prophylaxis against influenza A virus.

Contraindications

Hypersensitivity to drugs of adamantine class including rimantadine and amantadine.

Dosage and Administration

Prophylaxis and Treatment
Adults

PO 100 mg bid.

Elderly Nursing Home Patients, Hepatic and Renal Impairment (Ccr less than 10 mL/min)

Reduce to 100 mg/day.

Prophylaxis
Children 10 yr or older

PO 100 mg bid.

Children younger than 10 yr

PO 5 mg/kg/day (max, 150 mg/dose).

Storage/Stability

Store at controlled room temperature (59° to 86°F).

Drug Interactions

Acetaminophen, aspirin

Decreased peak serum concentration of rimantadine.

Cimetidine

Increased serum concentration caused by decreased clearance.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Insomnia; dizziness; headache; nervousness; asthenia; impaired concentration.

EENT

Eye pain.

GI

Nausea; vomiting; anorexia; dry mouth; abdominal pain.

Precautions

Pregnancy

Category C .

Lactation

Undetermined. Do not administer to nursing mothers.

Children

Safety and efficacy for prophylaxis not established in children younger than 1 yr.

Elderly

CNS symptoms may occur more frequently.

Seizures

Increased incidence of seizures in patients with seizure history and who receive amantadine.

Overdosage

Symptoms

Agitation, cardiac arrhythmias, hallucinations, death.

Patient Information

Tell patient with history of seizures to discontinue drug and notify health care provider if seizure activity develops.
Instruct patient to report insomnia, dizziness, headache, nervousness, asthenia, impaired concentration, nausea, vomiting, anorexia, persistent diarrhea, dry mouth, abdominal pain, dyspnea, cough, palpitations, or syncope.
Caution patient to avoid driving or operating hazardous equipment if dizziness or confusion develops.
Advise patient to take drug several hours before going to bed if insomnia develops.
Advise female patients to contact health care provider if pregnant, planning on becoming pregnant, or breastfeeding.

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