Rimantadine Actitab, pills 50mg 20pcs

Composition

Active ingredient: rimantadine hydrochloride 50 mg

Pharmacological action

Pharmaceutical group:

antiviral agent.

Pharmaceutical action:  

Rimantadine Actitab is an antiviral agent derived from adamantane; it is effective against strains of influenza A virus, Herpes simplex viruses type I and II, and tick-borne encephalitis viruses (Central European and Russian spring-summer arboviruses family). Flaviviridae).

It has antitoxic and immunomodulatory effects. The polymer structure ensures long-term circulation of rimantadine in the body, which allows it to be used not only for therapeutic, but also for preventive purposes.

Being a weak base, it increases the pH of endosomes that have a membrane of vacuoles and surround viral particles after they enter 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 to the cell cytoplasm. Rimantadine also inhibits the release of viral particles from the cell, i. e. interrupts the transcription of the viral genome.

Prophylactic use of rimantadine in a daily dose of 200 mg reduces the risk of flu, as well as reduces the severity of flu symptoms and serological response. Some therapeutic effect may also occur when it is prescribed in the first 18 hours after the first flu symptoms develop.

Pharmacokinetics:

 After oral use, it is almost completely absorbed in the intestines. Absorption is slow. The time to reach the maximum concentration (TCmax) is 1-4 hours. Binding to plasma proteins is about 40%. Volume of distribution: adults-17-25 l / kg, children-289 l. The concentration in the nasal secretions is 50% higher than the plasma one.

The maximum concentration (Cmax) when taking 100 mg once a day is 181 ng / ml,100 mg twice a day is 416 ng / ml. It is metabolized in the liver. Half-life (T1 / 2) in adults 20-44 years – 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 hours; more than 90% is excreted by the kidneys within 72 hours, mainly in the form of metabolites,15% – unchanged.

In chronic kidney failure (CRF), T1/2 increases 2-fold. In patients with renal insufficiency and in the elderly, toxic concentrations may accumulate if the dose is not adjusted in proportion to the decrease in creatinine clearance (CC). Hemodialysis has little effect on rimantadine clearance.

Indications

Early treatment and prevention of influenza A in adults and children over 7 years of age.

Contraindications

-Hypersensitivity to rimantadine. – Acute liver diseases; – Acute and chronic kidney diseases;- Thyrotoxicosis;- Pregnancy and lactation;- Children’s age (up to 7 years);

With caution:

Arterial hypertension, epilepsy (including in the anamnesis), cerebral vascular atherosclerosis, chronic renal failure, liver failure.

Side effects

From the digestive system:  epigastric pain, flatulence, increased bilirubin levels in the blood, dry mouth, anorexia, nausea, vomiting, gastralgia.

From the central nervous system:  headache, insomnia, nervousness, dizziness, impaired concentration, drowsiness, anxiety, increased excitability, fatigue.

Other services:  allergic reactions.

Interaction

When used concomitantly, rimantadine reduces the effectiveness of antiepileptic drugs.

Adsorbents, binders and enveloping agents reduce the absorption of rimantadine.

Drugs that acidify the urine (ammonium chloride, ascorbic acid), reduce the effectiveness of rimantadine (due to increased excretion by the kidneys).

Urine alkalinizing agents (acetazolamide, sodium bicarbonate) increase its effectiveness (reduced renal excretion).

Paracetamol and acetylsalicylic acid reduce the Cmax of rimantadine by 11%.

Cimetidine reduces the clearance of rimantadine by 18%.

How to take, course of use and dosage

Inside (after eating), washed down with water, according to the following scheme:

Adults are prescribed 100 mg 3 times on the first day of the disease; 100 mg 2 times on the second and third days; 100 mg once on the fourth day. On the first day of the disease, it is possible to use the drug once in a dose of 300 mg.

Children from 7 to 10 years old are prescribed 50 mg 2 times a day; 11-14 years old 50 mg 3 times a day. Treatment for influenza A should begin within 24-48 hours after the onset of symptoms and continue for 5-7 days. The optimal duration is not set.

For the prevention of influenza in adults,50 mg is prescribed 1 time a day for 10-15 days, depending on the source of infection.

For the treatment of influenza in CRF (creatinine clearance less than 10 ml / min), severe hepatic insufficiency, elderly patients in nursing homes-100 mg 1 time per day.

Special instructions

In comparison with amantadine, it has a higher clinical efficacy and is less toxic.

Viruses that are resistant to the drug may appear.

In influenza caused by the B virus, rimantadine has an antitoxic effect.

When using rimantadine, it is possible to exacerbate chronic concomitant diseases. Elderly patients with arterial hypertension have an increased risk of developing a hemorrhagic stroke. If there is a history of epilepsy and ongoing anticonvulsant therapy with rimantadine, the risk of developing an epileptic seizure increases. In such cases, rimantadine is used at a dose of 0.1 g per day simultaneously with anticonvulsant therapy.

Preventive treatment is effective in cases of contact with sick people (taking the drug is necessary for at least 10 days after contact), when the infection spreads in closed groups and when there is a high risk of developing the disease during an influenza epidemic.

During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Active ingredient

Rimantadine

Dosage form

Tablets

Indications

Flu, SARS, Tick-borne encephalitis, Flu prevention