Product Overview
Structure
Active ingredient:
Rimantadine hydrochloride - 50.0 mg
Excipients:
lactose monohydrate - 74.5 mg
potato starch - 24.0 mg
magnesium stearate - 1.5 mg
Rimantadine hydrochloride - 50.0 mg
Excipients:
lactose monohydrate - 74.5 mg
potato starch - 24.0 mg
magnesium stearate - 1.5 mg
pharmachologic effect
Rimantadine is an antiviral agent derived from adamantane; active against various strains of influenza A virus (especially type A2).
Being a weak base, rimantadine acts by increasing the pH of endosomes, which have a vacuole membrane that surrounds the viral particles after they enter the cell. Prevention of acidification in these vacuoles blocks the fusion of the viral envelope with the endosome membrane, thereby preventing the transmission 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.
Pharmacokinetics
After oral administration, rimantadine is almost completely absorbed in the intestine. Absorption is slow. Communication with plasma proteins is about 40%. Distribution volume: adults - 17-25 l / kg, children - 289 l / kg. The concentration in nasal secretion is 50% higher than in plasma.
The maximum concentration (Cmax) of the active substance in blood plasma after a single dose of 100 mg once a day is reached after 6 hours and is 181 ng / ml, at 100 mg twice a day - 416 ng / ml. Metabolized in the liver.
The elimination half-life is 24-36 hours (T1 / 2); 75-85% of the dose taken is excreted by the kidneys mainly in the form of metabolites, 15% - unchanged. In chronic renal failure, the elimination half-life increases by 2 times. In persons with renal failure and in elderly people, it can accumulate in toxic concentrations if the dose is not corrected in proportion to a decrease in creatinine clearance (CC).
Being a weak base, rimantadine acts by increasing the pH of endosomes, which have a vacuole membrane that surrounds the viral particles after they enter the cell. Prevention of acidification in these vacuoles blocks the fusion of the viral envelope with the endosome membrane, thereby preventing the transmission 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.
Pharmacokinetics
After oral administration, rimantadine is almost completely absorbed in the intestine. Absorption is slow. Communication with plasma proteins is about 40%. Distribution volume: adults - 17-25 l / kg, children - 289 l / kg. The concentration in nasal secretion is 50% higher than in plasma.
The maximum concentration (Cmax) of the active substance in blood plasma after a single dose of 100 mg once a day is reached after 6 hours and is 181 ng / ml, at 100 mg twice a day - 416 ng / ml. Metabolized in the liver.
The elimination half-life is 24-36 hours (T1 / 2); 75-85% of the dose taken is excreted by the kidneys mainly in the form of metabolites, 15% - unchanged. In chronic renal failure, the elimination half-life increases by 2 times. In persons with renal failure and in elderly people, it can accumulate in toxic concentrations if the dose is not corrected in proportion to a decrease in creatinine clearance (CC).
Indications
Early treatment and prevention of influenza A in adults and children older than 7 years.
Pregnancy and lactation
The use of the drug Rimantadine is contraindicated in pregnancy and during breastfeeding.
Contraindications
Hypersensitivity to rimantadine or any other component of the drug. Acute liver diseases, acute and chronic kidney diseases, thyrotoxicosis, lactase deficiency, lactose intolerance, glucose-galactose malabsorption, pregnancy, breast-feeding, children under 7 years of age.
Precautions
Arterial hypertension, epilepsy (including a history of), cerebral arteriosclerosis, liver failure, elderly patients, diseases of the gastrointestinal tract.
Precautions
Arterial hypertension, epilepsy (including a history of), cerebral arteriosclerosis, liver failure, elderly patients, diseases of the gastrointestinal tract.
Side effects
From the cardiovascular system: tachycardia, heart failure, heart block (disturbance of the heart rhythm), palpitations, arterial hypertension, cerebrovascular accident, loss of consciousness.
From the side of the nervous system: insomnia, dizziness, headache, irritability, fatigue, impaired attention, movement disorders, drowsiness, depressed mood, euphoria, hyperkinesia, tremor, hallucinations, confusion, convulsions.
From the sensory organs: tinnitus, change or loss of smell.
From the respiratory system: shortness of breath, bronchospasm, cough.
From the gastrointestinal tract: nausea, vomiting, loss of appetite, dry oral mucosa, abdominal pain, diarrhea, dyspepsia.
On the part of the skin and subcutaneous tissue: rash.
Other: fatigue.
If you have side effects indicated in the instructions or are aggravated, or you notice any other side effects not listed in the instructions, notify the doctor.
From the side of the nervous system: insomnia, dizziness, headache, irritability, fatigue, impaired attention, movement disorders, drowsiness, depressed mood, euphoria, hyperkinesia, tremor, hallucinations, confusion, convulsions.
From the sensory organs: tinnitus, change or loss of smell.
From the respiratory system: shortness of breath, bronchospasm, cough.
From the gastrointestinal tract: nausea, vomiting, loss of appetite, dry oral mucosa, abdominal pain, diarrhea, dyspepsia.
On the part of the skin and subcutaneous tissue: rash.
Other: fatigue.
If you have side effects indicated in the instructions or are aggravated, or you notice any other side effects not listed in the instructions, notify the doctor.
Interaction
Rimantadine reduces the effectiveness of antiepileptic drugs. Adsorbents, astringents and enveloping agents reduce the absorption of rimantadine. Urine-alkalizing agents (acetazolamide, sodium bicarbonate and others) enhance the effectiveness of rimantadine due to a decrease in its excretion by the kidneys. Paracetamol and ascorbic acid reduce the maximum concentration of rimantadine in blood plasma by 11%. Cimetidine reduces the clearance of rimantadine by 18%.
If you are using the above or other medications (including over-the-counter), consult your doctor before using rimantadine.
If you are using the above or other medications (including over-the-counter), consult your doctor before using rimantadine.
How to take, course of administration and dosage
Rimantadine is taken orally (after eating), washed down with water.
Flu treatment should be started within 24-48 hours after the onset of symptoms of the disease.
Adult use:
- on the first day of the disease - 100 mg 3 times a day;
- on the second and third day of the disease - 100 mg 2 times a day;
- on the fourth and fifth day of the disease - 100 mg once a day.
On the first day of therapy, it is possible to use the drug once in a dose of 300 mg.
The course of treatment is 5 days.
Use in children:
- aged 7 to 10 years - 50 mg 2 times a day;
- at the age of 10-14 years - 50 mg 3 times a day;
- over 14 years old - doses for adults.
The course of treatment is 5 days.
Influenza prophylaxis:
- for adults, 50 mg once a day for 30 days, depending on the epidemiological situation.
- in children older than 7 years, 50 mg 1 time per day for 15 days, depending on the epidemiological situation.
Flu treatment should be started within 24-48 hours after the onset of symptoms of the disease.
Adult use:
- on the first day of the disease - 100 mg 3 times a day;
- on the second and third day of the disease - 100 mg 2 times a day;
- on the fourth and fifth day of the disease - 100 mg once a day.
On the first day of therapy, it is possible to use the drug once in a dose of 300 mg.
The course of treatment is 5 days.
Use in children:
- aged 7 to 10 years - 50 mg 2 times a day;
- at the age of 10-14 years - 50 mg 3 times a day;
- over 14 years old - doses for adults.
The course of treatment is 5 days.
Influenza prophylaxis:
- for adults, 50 mg once a day for 30 days, depending on the epidemiological situation.
- in children older than 7 years, 50 mg 1 time per day for 15 days, depending on the epidemiological situation.
Overdose
Symptoms: agitation, hallucinations, arrhythmia. In some cases, when the recommended dose is exceeded, tearing of the eyes and eye pain, increased urination, fever, constipation, sweating, inflammation of the oral mucosa, and dry skin are observed.
Treatment: gastric lavage, symptomatic therapy. In case of poisoning, it is necessary to maintain vital functions. Rimantadine is partially excreted during hemodialysis.
Special instructions
Perhaps the emergence of drug-resistant viruses.
Prophylactic is effective in contact with patients with the spread of infection in closed groups and at high risk of the disease during an influenza epidemic.
When using the drug Rimantadine, an exacerbation of chronic concomitant diseases is possible. In elderly patients with arterial hypertension, the risk of hemorrhagic stroke is increased. When there is a history of epilepsy and ongoing anticonvulsant therapy, the risk of a seizure increases with the use of rimantadine. In such cases, the drug Rimantadine is used at a dose of 100 mg / day simultaneously with anticonvulsant therapy.
In influenza caused by virus B, rimantadine has an antitoxic effect.
Impact on the ability to drive vehicles, mechanisms
Rimantadine does not affect the ability to drive a vehicle, but caution should be exercised for persons who experience dizziness, headache, or other side effects from the central nervous system.
Prophylactic is effective in contact with patients with the spread of infection in closed groups and at high risk of the disease during an influenza epidemic.
When using the drug Rimantadine, an exacerbation of chronic concomitant diseases is possible. In elderly patients with arterial hypertension, the risk of hemorrhagic stroke is increased. When there is a history of epilepsy and ongoing anticonvulsant therapy, the risk of a seizure increases with the use of rimantadine. In such cases, the drug Rimantadine is used at a dose of 100 mg / day simultaneously with anticonvulsant therapy.
In influenza caused by virus B, rimantadine has an antitoxic effect.
Impact on the ability to drive vehicles, mechanisms
Rimantadine does not affect the ability to drive a vehicle, but caution should be exercised for persons who experience dizziness, headache, or other side effects from the central nervous system.
Storage conditions
In a dry, dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
Shelf life
5 years.
