Instructions for use of rimantadine tablets for adults and children. Remantadine - instructions for use Appointment during pregnancy and lactation

Active ingredient: 50 mg rimantadine.

Pharmacodynamics. Remantadine is effective against various strains of the A virus (especially A type 2). Active against viruses (Central European and Russian spring-summer), which belong to the group of arboviruses of the Flaviviridae family. The main mechanism of antiviral action is inhibition of the early stage of specific reproduction after the penetration of the virus into the cell and before the initial transcription of RNA. The pharmacological efficacy of the drug is ensured by inhibiting the reproduction of the virus in the initial stage of the infectious process. Remantadine has an antitoxic effect in influenza caused by virus B. It is not effective in others.

Pharmacokinetics. Remantadine is well, but slowly absorbed from the gastrointestinal tract. Most of the drug is extensively metabolized. The plasma half-life is 24-36 hours. Excreted in the urine: less than 15% of the dose - unchanged, about 20% - in the form of hydroxyl metabolites. With the half-life increases approximately 2 times.

Early treatment in both adults and children over 7 years of age; prevention of influenza during epidemics in adults; prevention of tick-borne encephalitis of viral etiology.

As remedy with influenza, rimantadine is prescribed according to the following scheme. Adults: on the 1st day - 100 mg 3 times / day; on the 2nd and 3rd days - 100 mg 2 times / day; on the 4th and 5th days - 100 mg 1 time / day. On the 1st day of the disease, it is possible to prescribe the drug at a dose of 150 mg 2 times / day or 300 mg per 1 dose. Children aged 7 to 10 years - 50 mg 2 times / day; 11-14 years - 50 mg 3 times / day; course of treatment - 5 days.

For the prevention of influenza, the drug is prescribed 50 mg 1 time / day for 10-15 days.

For the prevention of tick-borne encephalitis of viral etiology, adults are prescribed 100 mg of rimantadine 2 times / day with a 12-hour interval for 3 days. In some cases, according to the doctor's prescription - 5 days. Prevention with rimantadine begins immediately after a tick bite, but no later than 48 hours! Risk groups (persons living or staying in a forest overgrown area) are allowed to prevent tick-borne encephalitis for up to 15 days.

Remantadine is taken orally after meals with water.

When treating patients with kidney failure dose reduction is necessary.

Precautionary measures. When using rimantadine, an exacerbation of chronic concomitant diseases is possible. In elderly patients with arterial hypertension increased risk of development. In patients with indications of a history of epilepsy and anticonvulsant therapy during treatment with rimantadine, the risk of developing an epileptic seizure increases. In such cases, it is recommended to prescribe rimantadine at a dose of up to 100 mg / day simultaneously with anticonvulsants.

Active substance: rimantadine hydrochloride 50 mg.

Excipients: lactose monohydrate (milk sugar) - 74 mg, potato starch - 24.35 mg, calcium stearate - 1.5 mg, talc - 0.15 mg.

Tablets of white color of a ploskotsilindrichesky form with a facet.

Pharmacodynamics.

Antiviral agent, adamantane derivative; effective against various strains of virus A, Herpes simplex type I and II viruses, viruses (Central European and Russian spring-summer from the group of arboviruses of the Flaviviridae family). It has antitoxic and immunomodulatory effects.

Sufficiently slow metabolism (T1 / 2 usually more than a day) causes a long-term circulation of rimantadine in the body, which allows it to be used not only for therapeutic, but also for prophylactic purposes. Suppresses early stage specific reproduction (after the penetration of the virus into the cell and before the initial transcription of RNA); induces the production of alpha and gamma interferons, increases the functional activity of lymphocytes - natural killers (NK cells), T- and B-lymphocytes.

Being weak base, increases the pH of endosomes that have a membrane of vacuoles and surrounding viral particles after they enter the cell. Prevention of acidification in these vacuoles blocks the fusion of the viral envelope with the endosome membrane, thus preventing transfer of viral genetic material into the cytoplasm of the cell. Rimantadine also inhibits the release of viral particles from the cell, that is, it interrupts the transcription of the viral genome.

Prophylactic administration of rimantadine in daily dose 200 mg reduces the risk of influenza, and also reduces the severity of influenza symptoms and serological reactions. Some therapeutic effect may also appear when it is administered in 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 (tablets and syrup provide equally good absorption). Absorption is slow. TCmax - 1-4 hours. Communication with plasma proteins - about 40%. Volume of distribution: adults - 17-25 l / kg, children - 289 l. The concentration in the nasal secretion is 50% higher than the plasma concentration. The value of Cmax when taking 100 mg 1 time per day - 181 ng / ml, 100 mg 2 times a day - 416 ng / ml.

Metabolized in the liver. Half-life in adults 20-44 years old - 25-30 hours, in elderly patients (71-79 years old) and in patients with chronic liver failure - about 32 hours, in children 4-8 years old - 13-38 hours; more than 90% is excreted by the kidneys within 72 hours, mainly in the form of metabolites, 15% - unchanged.

When the half-life increases by 2 times. In persons with renal insufficiency and in the elderly, it can accumulate in toxic concentrations if the dose is not adjusted in proportion to the decrease in CC. has little effect on the clearance of rimantadine.

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

Inside after eating, drinking water.

Prevention: adults are prescribed 50 mg once a day for up to 30 days.

Children over 7 years old - 50 mg 1 time per day for up to 15 days.

Influenza treatment should begin within 24-48 hours after the onset of symptoms of the disease.

Adults on the first day are prescribed 100 mg 3 times a day; on the second and third day, 100 mg 2 times a day; on the fourth and fifth day, 100 mg 1 time per day. On the first day of the disease, it is possible to use the drug once at a dose of 300 mg. Children aged 7 to 10 years are prescribed 50 mg 2 times a day; from 11 to 14 years old - 50 mg 3 times a day. Over 14 years old - doses for adults. Accepted within 5 days.

For the treatment and prevention of influenza in chronic renal failure (creatinine clearance less than 10 ml / min), severe liver failure, elderly patients in nursing homes - 100 mg 1 time per day.

Carefully:
Epilepsy (including history), .

Pregnancy and lactation:
Contraindicated in pregnancy and during breastfeeding.

When using rimantadine, exacerbation of chronic concomitant diseases is possible. In elderly patients with arterial hypertension, the risk of developing is increased.

With indications of a history of epilepsy and conductive anticonvulsant therapy against the background of the use of rimantadine, the risk of developing an epileptic seizure increases. In such cases, rimantadine is used at a dose of 100 mg per day simultaneously with anticonvulsant therapy.

Prophylactic administration is effective in contact with sick people, with the spread of infection in closed groups, and with a high risk of illness during an influenza epidemic.

The emergence of drug-resistant viruses is possible.

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

Allergic reactions:, itching,.

From the side of the central nervous system: decreased ability to concentrate, insomnia, nervousness, anxiety, excessive fatigue, drowsiness, irritability.

From the side digestive system: dryness of the oral mucosa, hyperbilirubinemia.

Paracetamol and acetylsalicylic acid reduce the maximum concentration of rimantadine by 11% and 10%, respectively. Cimetidine reduces the clearance of rimantadine by 18%.

Rimantadine reduces the effectiveness of antiepileptic drugs.

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

Urine alkalizing agents (acetazolamide, sodium bicarbonate, etc.) increase the concentration of rimantadine due to a decrease in its excretion by the kidneys.

Hypersensitivity to rimantadine, drug components, acute, acute and chronic, thyrotoxicosis, lactase deficiency, lactose intolerance, lactose/isomaltose malabsorption syndrome, childhood(up to 7 years).

In case of poisoning, it is necessary to maintain vital functions. If symptoms from the central nervous system occur - effectively intravenous administration physostigmine adults 1-2 mg, children 0.5 mg with repetition if necessary, but not more than 2 mg / hour.

Rimantadine is an antiviral agent.

Release form and composition

Dosage form - tablets: round, white or almost white, with a bevel, there may be a risk (10, 20 or 30 pieces in blister packs, in a carton pack 1, 2, 3, 4, 5, 6, 8 or 10 packs, 10, 20, 30, 40, 50, 60, 70, 80, 90 or 100 pieces in polymer cans, in a carton pack 1 can, packaging for hospitals - in a carton 200, 400, 500, 600, 800, 1000 blisters).

Composition of 1 tablet:

• active substance: rimantadine hydrochloride - 50 mg;
• excipients (may differ slightly from different manufacturers): calcium stearate, lactose monohydrate, talc, potato starch.

Pharmacological properties

Pharmacodynamics

Rimantadine is an antiviral agent derived from adamantane. Effective against various strains of the influenza A virus (especially A2).

Thanks to the polymer structure, long-term circulation of rimantadine in the body is ensured, so the drug is used not only for the treatment, but also for the prevention of influenza.

Rimantadine inhibits the early stage of specific reproduction of the virus (after its entry into the cell and before the initial transcription of RNA).

Rimantadine is a weak base. Its action is due to the ability to increase the pH of endosomes, which have a vacuole membrane and surround viral particles after they enter the cell. Thus, the substance of the drug prevents acidification in these vacuoles, which blocks the fusion of the viral envelope with the endosomal membrane and, as a result, interrupts the transcription of the viral genome, i.e., prevents the transfer of viral genetic material into the cytoplasm of the cell.

When taking rimantadine at a daily dose of 200 mg for 2–3 days before and within 6–7 days after development clinical symptoms influenza A reduces the incidence, severity of symptoms and the degree of serological reactions. Some therapeutic effect of the drug is possible if it is taken within the next 18 hours after the onset of the first signs of influenza.

Pharmacokinetics

After oral administration, rimantadine is slowly but almost completely absorbed from the intestine. It is approximately 40% bound to plasma proteins. Its volume of distribution is 17-25 l/kg in adults, 289 l/kg in children.

In the nasal secretion, the concentration of the drug is 50% higher than in the blood plasma. Maximum plasma concentrations: 181 ng / ml - when taking a daily dose of 100 mg, 416 ng / ml - when taking a daily dose of 200 mg.

It is metabolized in the liver. It is excreted by the kidneys mainly in the form of metabolites (75-85%), partially - unchanged (15%). The elimination half-life is 24-36 hours, but increases by 2 times in patients with concomitant chronic renal failure.

In renal insufficiency and in elderly patients, accumulation of rimantadine in toxic concentrations is possible if the dose is not adjusted in proportion to the decrease in creatinine clearance.

Indications for use

According to the instructions, Rimantadine is used for the early treatment and prevention of influenza A in children from 7 years of age and adults.

Prophylactic administration is recommended after contact with a sick person (it is recommended to take it for at least 10 days), in case of spread of infection in closed groups, and also if there is a high risk of morbidity during an influenza epidemic.

Contraindications

• sharp and chronic diseases kidneys;
• acute liver disease;
• thyrotoxicosis;
• glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
• children's age up to 7 years;
• the period of pregnancy and breastfeeding;
• the presence of hypersensitivity to any component of the drug.

With caution, an antiviral agent must be used for diseases gastrointestinal tract, liver failure, arterial hypertension, cerebral atherosclerosis, epilepsy (including history), as well as in old age.

Instructions for use Rimantadine: method and dosage

Rimantadine tablets are taken orally, after meals, with water.

• adults: 50 mg once a day for up to 30 days;
• children from 7 years: 50 mg once a day for up to 15 days.

The duration of admission is determined by the epidemiological situation.

With influenza, Rimantadine should be started within the first 24-48 hours after the onset of the first symptoms of the disease.

Scheme of prescribing the drug to adults and adolescents from 14 years of age by day:

• 1st day - 100 mg 3 times a day or 300 mg once;
• 2nd day - 100 mg 2 times a day;
• 3rd day - 100 mg 2 times a day;
• 4th day - 100 mg 1 time per day;
• 5th day - 100 mg 1 time per day.

Children from 7 years of age medicinal purposes doses are determined depending on age:

• 7-10 years - 50 mg 2 times a day;
• 10-14 years - 50 mg 3 times a day.

The duration of treatment is also 5 days.

Elderly patients and patients with concomitant chronic renal / hepatic insufficiency, as well as persons suffering from epilepsy, for the treatment of influenza, Rimantadine is prescribed 100 mg once a day.

Side effects

• from the side respiratory system: shortness of breath, cough, bronchospasm;
• from the nervous system: movement disorders, fatigue, headache, insomnia, impaired concentration, confusion, depressed mood, irritability, hyperkinesia, drowsiness, hallucinations, dizziness, tremor, euphoria, convulsions;
• from the gastrointestinal tract: dryness of the oral mucosa, loss of appetite, nausea, diarrhea, abdominal pain, vomiting, dyspepsia;
• from the side of cardio-vascular system: loss of consciousness, impaired cerebral circulation, arterial hypertension, heart block (cardiac arrhythmias), tachycardia, palpitations, heart failure;
• on the part of the senses: loss or change in smell, tinnitus;
• other: fatigue, rash.

Overdose

Symptoms: arrhythmia, hallucinations, agitation. Dry skin, eye pain, watery eyes, inflammation of the mucous membrane are also possible. oral cavity, sweating, constipation, increased urination, fever.

The first measure in case of overdose is gastric lavage. Further treatment is symptomatic, aimed, among other things, at maintaining the vital functions of the body. In the case of the development of negative symptoms from the nervous system, intravenous administration of physostigmine (1.2 mg for adults and 0.5 mg for children) is indicated, if necessary, the drug is administered repeatedly (no more than 2 mg / h). Rimantadine can be partially removed by hemodialysis.

special instructions

It is advisable to take the drug for the prevention of influenza after contact with a sick family member. However, it is less effective for prophylactic use in a family in which patients with influenza took rimantadine in preventive purposes, which is probably associated with the transmission of viruses resistant to its action.

In influenza caused by virus B, Rimantadine has antitoxic activity.

During the period of antiviral treatment, exacerbation of existing chronic diseases is possible. In older people with arterial hypertension increased risk of developing hemorrhagic stroke. Patients with a history of epilepsy and anticonvulsant therapy are at an increased risk of seizures. In such cases, Rimantadine is prescribed in a daily dose of 100 mg simultaneously with anticonvulsant therapy.

Consideration should be given to the possibility of emergence of viruses resistant to the drug.

Influence on the ability to drive vehicles and complex mechanisms

Due to the risk of developing side effects from the central nervous system, the entire period of taking the drug, care must be taken when performing potentially hazardous types of work that require heightened attention and reaction rates (including driving vehicles).

Use during pregnancy and lactation

Rimantadine tablets are contraindicated during the entire period of pregnancy and lactation.

Application in childhood

This dosage form the drug is not intended for the treatment of children under the age of 7 years.

For impaired renal function

The presence of acute and chronic kidney disease is a contraindication to the use of Rimantadine.

In renal failure, the dose is reduced in proportion to the level of creatinine clearance.

For impaired liver function

At acute diseases liver administration of the drug is prohibited. In hepatic insufficiency, the drug should be used with caution.

Use in the elderly

Elderly patients during treatment should be under close medical supervision. Dose reduction required.

drug interaction

Rimantadine reduces the effect of antiepileptic drugs.

The influence of other drugs on the action of rimantadine:

• adsorbents, enveloping and astringent agents reduce absorption;
• cimetidine reduces clearance by 18%;
• acetylsalicylic acid and paracetamol reduce the maximum concentration (by 10 and 11%, respectively);
• urine acidifying agents (including ammonium chloride, sodium bicarbonate, diacarb, acetazolamide, ascorbic acid) increase excretion by the kidneys and, as a result, reduce the effect.

Analogues

The analogues of Rimantadine are: Orvirem, Remantadin, Rimantadin Avexima, Rimantadin Aktitab.

Terms and conditions of storage

Store in a dry, dark place, out of the reach of children, at temperatures up to 25 °C.

Shelf life - 3 or 5 years (depending on the manufacturer).