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

Composition:Each tablet contains rimantadine hydrochloride as active ingredient -50 mg.
Excipients: sugar milk (lactose), potato starch, talc, calcium stearate.

Description:White tablets are flat-cylindrical with a bevel.

Pharmacotherapeutic group:An antiviral agent.

ATX: & nbsp

J.05.A.C Cyclic amines

J.05.A.C.02 Rimantadine

Pharmacodynamics:Antiviral agent, adamantane derivative; effective against strains of the influenza A virus, Herpes simplex type I and II viruses, tick-borne encephalitis viruses (Central European and Russian spring-summer from the group of arboviruses of the family Flaviviridae). Has antitoxic and immunomodulating effect. The polymeric structure provides a long circulation of rimantadine in the body, which makes it possible to apply it not only with curative, but also with a preventive purpose. Being a weak base, it increases the pH of the endosome, which have a membrane of vacuoles and surrounding virus particles after they penetrate the cell. The prevention of acidification in these vacuoles blocks the fusion of the viral envelope with the endosome membrane, thereby preventing it. transfer of 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. Prophylactic administration of rimantadine in a daily dose of 200 mg reduces the risk of flu, and reduces the symptoms of influenza and serological response.A certain therapeutic effect may also be manifested when it is administered within the first 18 hours after the development of the first symptoms of influenza.

Pharmacokinetics:After oral administration, it is almost completely absorbed in the intestine. Absorption is slow. The time to reach the maximum concentration (TCmax) is 1-4 hours. The connection with plasma proteins is about 40%. The volume of distribution: adults - 17-25 l / kg, children - 289 liters. Concentration in nasal secretion is 50% higher than plasma concentration. The maximum concentration (Сmах) 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 period (T1 / 2) in adults 20-44 years is 25-30 hours, in elderly patients (71-79 years) and in patients with chronic hepatic insufficiency - about 32 hours, in children 4-8 years - 13-38 h; more than 90% is excreted by the kidneys within 72 hours, mainly in the form of metabolites, 15% - unchanged. In chronic renal failure (CRF), T1 / 2 increases by 2 times. Persons with renal insufficiency and elderly people may accumulate in toxic concentrations if the dose is not adjusted in proportion to the decrease in creatinine clearance (QC). Hemodialysis has an insignificant effect on the clearance of rimantadine.

Indications:Early treatment and prevention of influenza A in adults and children older than 7 years.

Contraindications:- Hypersensitivity to rimantadine;
- 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:Inside (after eating), washed down with water, according to the following scheme:
Adults are prescribed on the first day of the disease for 100 mg of Zraza; in the second and third days can be 100 mg 2 times; the fourth day, 100 mg once. On the first day of the disease, the drug can be used once in a dose of 300 mg.
Children from 7 to 10 years are prescribed 50 mg twice a day; 11-14 years 50 mg 3 times a day.
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.
For the prevention of 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 (KK 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 there are:
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 (rash, itching, hives, etc.).

Interaction:Pharmacodynamic: rimantadine reduces the effectiveness of antiepileptic drugs.
Pharmacokinetic: adsorbents, astringents and enveloping agents reduce the absorption of rimantadine.
Urinary acidifying agents (ammonium chloride, ascorbic acid, etc.) reduce the effectiveness of rimantadine, due to a faster release of the latter kidneys.
Urinary alkalizing agents (diacarb, sodium hydrogen carbonate and others) intensify the action of rimantadine, due to the decrease in its excretion by the kidneys.
Paracetamol and acetylsalicylic acid decrease the Cmax of rimantadine by 11 and 10%, respectively.
Cimetidine reduces the clearance of rimantadine by 18%.

Special instructions:In comparison with amantadine has a higher clinical efficacy and less toxic.
Perhaps the emergence of drug-resistant viruses.
With influenza caused by virus B, rimantadine has an antitoxic effect.
With the use of rimantadine, an exacerbation of chronic comorbidity may occur. In elderly patients with hypertension, the risk of developing a 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. Prophylactic reception is effective at contacts with the sick (taking the drug is necessary at least for 10 days after contact), with the spread of infection in closed groups and at a high risk of disease during the flu epidemic.

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,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets of 50 mg.

Packaging:For 10, 15, 20 or 30 tablets in a contour cell package.
For 1 or 2 contour mesh packages along with the instruction for use are placed in a pack of cardboard.

Storage conditions:List B. In a dry, the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.

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

Terms of leave from pharmacies:Without recipe

Registration number:P N001555 / 01

Date of registration:14.08.2008

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp22.09.2015

Illustrated instructions

Instructions

Rimantadine Aktitab (Rimantadine Actitab)