Rimantadine - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Rimantadine is active against various strains of the influenza A virus (especially A2 type). Being a weak ground, rimantadine acts by increasing the pH of the endosome, which have a membrane of vacuoles that surround the viral particles after they penetrate the cell. The prevention of acidification in these vacuoles blocks the fusion of the viral envelope with the endosome membrane, thus preventing the transfer of the viral genetic material to the cytoplasm of the cell. Rimantadine also inhibits the release of viral particles from the cell, i.e. interrupts the transcription of the viral genome.

In humans, the appointment of rimantadine in a daily dose of 200 mg for 2-3 days before and 6-7 days after the onset of clinical manifestations of influenza A reduces the incidence, severity of symptoms and the degree of serological response. Some therapeutic effect can also be manifested if rimantadine appointed within 18 hours after the onset of the first symptoms of influenza.

Pharmacokinetics:After oral administration rimantadine almost completely absorbed in the intestine.
Absorption is slow. The connection with plasma proteins is about 40%. The volume of distribution: adults - 17-25 l / kg, children - 289 l / kg. Concentration in nasal secretion is 50% higher than plasma concentration. The maximum concentration of rimantadine in the blood plasma (Cmach) with the intake of 100 mg once a day - 181 ng / ml, 100 mg twice a day - 416 ng / ml.
Metabolised in the liver. The half-life (T1 / 2) is 24-36 h; is excreted by the kidneys 15% - unchanged, 20% - in the form of hydroxyl metabolites.
In chronic renal failure, T1 / 2 increases by 2 times. In individuals with kidney failure and in elderly people, it can accumulate in toxic concentrations if the dose is not corrected in proportion to the decrease in creatinine clearance (CC).

Indications:Influenza A (early treatment and prevention in children and adults).

Contraindications:Hypersensitivity to the drug, acute liver disease; acute and chronic kidney disease; thyrotoxicosis, pregnancy and lactation, children's age (up to 7 years).

Carefully:arterial hypertension, epilepsy, (including in the anamnesis), atherosclerosis of cerebral vessels, chronic renal failure, hepatic insufficiency.

Dosing and Administration:Adults and children over 14 years of age on 100 mg 2 times a day; Children from 7 to 10 years of age are prescribed 50 mg twice a day; 11-14 years - 50 mg 3 times a day. The maximum daily dose for children should not exceed 150 mg. Treatment of influenza A should begin within 24-48 hours after the onset of symptoms of the disease and continue for 5-7 days. The optimal duration is not set.
To prevent influenza in adults, 50 mg once a day for 10-15 days, depending on the focus of infection.
For treatment of influenza in chronic renal failure (CC less than 10 ml / min), severe hepatic insufficiency, elderly patients in nursing homes - 100 mg once a day.

Side effects:Rimantadine usually well tolerated. Sometimes it is observed:
From the gastrointestinal tract: pain in epigastrium, flatulence, dry mouth, anorexia, nausea, vomiting;
From the central nervous system: headache, dizziness, insomnia, neurological reactions, impaired concentration, drowsiness, anxiety, increased excitability, fatigue.
Other: Hyperbilirubinemia, allergic reactions (skin rash, itching, hives, etc.).

Overdose:Data on overdose are absent. There may be an increase in side effects. Treatment: symptomatic, in the case of the recent administration of the drug-gastric lavage.

Interaction:Pharmacodynamic: rimantadine reduces the effectiveness of antiepileptic drugs.
Pharmacokinetic: adsorbents, astringents and enveloping agents reduce the absorption of rimantadine.
Urinary alkalizing agents (acetazolamide, sodium hydrogen carbonate and others) enhance the effectiveness of rimantadine due to a decrease in its secretion by the kidneys.
Paracetamol and ascorbic acid reduce the maximum concentration rimantadine in blood plasma by 11%.
Cimetidine reduces the clearance of rimantadine by 18%.

Special instructions:With the use of rimantadine, an exacerbation of chronic comorbidity may occur. In elderly patients with hypertension, the risk of hemorrhagic stroke increases. With a history of epilepsy and ongoing anticonvulsant therapy with rimantadine, the risk of epileptic seizures increases. In such cases rimantadine apply at a dose of 0.1 g per day simultaneously with anticonvulsant therapy.
With influenza caused by virus B, rimantadine has an antitoxic effect.
Prophylactic reception is effective at contacts with the sick, with the spread of infection in closed collectives and at a high risk of the disease during the flu epidemic.
Perhaps the emergence of drug-resistant viruses.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Tablets of 50 mg.

Packaging:For 10, 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil. For 20 tablets in cans or bottles of lightproof glass.
To the bank, a bottle, 1,2 contour mesh packages together with the instruction for use are placed in a pack of cardboard.
Contoured cell packs, together with an equal number of instructions for use, are placed in a group package.

Storage conditions:In a dry place. Keep out of the reach of children.

Shelf life:5 years. Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-006419/08

Date of registration:08.08.2008

The owner of the registration certificate:EVROFARM, CJSC EVROFARM, CJSC Russia

Manufacturer: & nbsp

EVROFARM, CJSC Russia

Information update date: & nbsp22.09.2015

Illustrated instructions

Instructions

Rimantadine (Rimantadine)