Rimantadine is an antiviral agent, a derivative of adamantane; it is active against various strains of influenza A virus (especially type A2).
Being a weak base, rimantadine acts by increasing pH of endosomes – membrane vacuoles that surround viral particles after their penetration into the cell. Preventing acidification in these vacuoles blocks the fusion of the viral envelope with the endosome membrane, thus preventing the transfer of viral genetic material into the cell cytoplasm. Rimantadine also inhibits the exit of viral particles from the cell, i.e. it interrupts transcription of the viral genome.
Pharmacokinetics
After oral administration rimantadine is almost completely absorbed in the intestine. Absorption is slow. Binding with plasma proteins is about 40%. Volume of distribution: adults – 17-25 l/kg, children – 289 l/kg. Concentration in nasal secretion is 50% higher than in plasma.
Maximum concentration (Cmax) of active substance in plasma after a single dose of 100 mg once daily is reached after 6 hours and is 181 ng/ml, after 100 mg twice daily – 416 ng/ml. It is metabolized in the liver.
Half-life period is 24-36 hours (T1/2); 75-85% of dose is excreted by kidneys mainly as metabolites, 15% – unchanged. In chronic renal failure the half-life is increased by 2 times. In patients with renal insufficiency and elderly persons can accumulate in toxic concentrations if the dose is not corrected in proportion to the decrease in creatinine clearance (CC).
Indications
Early treatment and prevention of influenza A in adults and children over 7 years old.
Active ingredient
Rimantadine
Composition
Active ingredient:
Rimantadine hydrochloride – 50,0 mg
Excipients:
lactose monohydrate – 74,5 mg
potato starch – 24,0 mg
magnesium stearate – 1,5 mg.
How to take, the dosage
Rimantadine is taken orally (after meals) with water.
Treatment of influenza should be started within 24-48 hours after the onset of symptoms.
Administration in adults:
– On the first day of the disease – 100 mg 3 times a day;
– On the second and third days of the disease – 100 mg 2 times a day;
– On the fourth and fifth days of the disease – 100 mg once a day.
On the first day of the therapy it is possible to use the preparation once in a dose of 300 mg.
The course of treatment is 5 days.
Administration in children:
– in the age of 7 to 10 years – 50 mg twice a day;
– in the age of 10-14 years – 50 mg 3 times a day;
– over 14 years – doses for adults.
The course of treatment is 5 days.
Influenza prevention:
– adults 50 mg once a day for 30 days, depending on the epidemiological situation.
– in children over 7 years – 50 mg once a day for 15 days, depending on the epidemiological situation.
Interaction
Rimantadine reduces the effectiveness of antiepileptic drugs. Adsorbents, astringents and coagulants decrease absorption of rimantadine. Urine alkalizing agents (acetazolamide, sodium bicarbonate and others) increase the effectiveness of rimantadine due to reduction of its excretion by the kidneys. Paracetamol and ascorbic acid decrease maximum concentration of rimantadine in blood plasma by 11%. Cimetidine decreases clearance of rimantadine by 18 %.
If you use the above mentioned or other drugs (including over-the-counter drugs), consult your doctor before using rimantadine.
Special Instructions
Prophylactic administration is effective in case of contact with ill people, when the infection spreads in closed groups and at high risk of influenza epidemics.
During the use of Rimantadine exacerbation of chronic comorbidities is possible. In elderly patients with arterial hypertension the risk of hemorrhagic stroke increases. In case of indications in the anamnesis of epilepsy and anticonvulsant therapy, during using Rimantadine, the risk of seizure increases. In such cases, Rimantadine is used in dose of 100 mg/day simultaneously with anticonvulsant therapy.
In case of influenza caused by B virus, rimantadine has antitoxic effect.
Effect on ability to drive vehicles, mechanisms
Rimantadine does not affect the ability to drive a vehicle, but persons who experience dizziness, headache or other side effects from the central nervous system should be careful.
Contraindications
Hypersensitivity to rimantadine or any other component of the drug. Acute liver disease, acute and chronic kidney disease, thyrotoxicosis, lactase deficiency, lactose intolerance, glucose-galactose malabsorption, pregnancy, breast-feeding, children under 7 years of age.
With caution
Arterial hypertension, epilepsy (including anamnesis), cerebral atherosclerosis, liver failure, elderly patients, diseases of the gastrointestinal tract.
Side effects
Cardiovascular system: tachycardia, heart failure, heart block (heart rhythm disorders), palpitations, arterial hypertension, disorders of cerebral circulation, loss of consciousness.
Nervous system disorders: insomnia, dizziness, headache, irritability, fatigue, concentration disorders, movement disorders, drowsiness, depressed mood, euphoria, hyperkinesia, tremors, hallucinations, confusion, seizures.
Senses: tinnitus, change or loss of sense of smell.
Respiratory system: shortness of breath, bronchospasm, cough.
Gastrointestinal tract: nausea, vomiting, loss of appetite, dry mouth, abdominal pain, diarrhea, dyspepsia.
Skin and subcutaneous tissue: rash.
Other: fatigue.
If you have side effects mentioned in the instructions or they are aggravated, or if you notice any other side effects not specified in the instructions, inform your doctor.
Overdose
Symptoms: agitation, hallucinations, arrhythmia. In some cases, if the recommended dose is exceeded: tearfulness of the eyes and pain in the eyes, increased urination, fever, constipation, sweating, inflammation of the oral mucosa, dry skin.
Treatment: gastric lavage, symptomatic therapy. When poisoning it is necessary to maintain vital functions. Rimantadine is partially excreted by hemodialysis.
Pregnancy use
The use of the drug Rimantadine is contraindicated in pregnancy and during breastfeeding.
Similarities
Orvirem, Rimantadine, Rimantadine Kids
Weight | 0.013 kg |
---|---|
Shelf life | 5 years. |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 ° C. |
Manufacturer | Update PFC AO, Russia |
Medication form | pills |
Brand | Update PFC AO |
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