Amantadine analogs synonyms. Medicinal reference book geotar

  • The date: 04.07.2020

Amantadines are presented as two salts - sulfate and hydrochloride. The pharmaceutical industry produces amantadine sulfate - PK-Merz, which has been successfully used in the treatment of ischemic stroke, as shown by numerous studies. Amantadine sulfate and hydrochloride are very similar in pharmacodynamics, but differ in pharmacokinetics: amantadine sulfate provides the most stable plasma concentration in the brain, is better tolerated by the patient, causes fewer side effects (insomnia, hallucinations, edema, confusion, etc.).

Efficacy of amantadine sulfate in the treatment of ischemic stroke

PK-Merz is considered the only amantadine that has an infusion form of release, and this makes it simply indispensable for the prevention, as well as the treatment of complications that occur against the backdrop of the main anti-Parkinsonian therapy. As a drug that has a neuroprotective mechanism of action, amantadine sulfate is effective in long-term therapy of acute cerebrovascular accidents, as well as in the rehabilitation period.

Numerous analyzes have been conducted to provide evidence of the effectiveness of this drug in the treatment of stroke. The main goal of the analyzes was to determine whether the data on the clinical efficacy of PK-Merz are sufficient to distinguish it from other amantadines and other drugs with neuroprotective properties in the treatment of stroke. If amantadine sulfate is prescribed in the early stages of a stroke, then its use can prevent pathophysiological changes and also improve the outcome of the condition.

Pilot study by S.A. Rumyantseva and her co-authors in 39 patients with severe stroke (19 of them used the drug) noted the expediency of including this drug in the therapy program, and as early as possible after the onset of a vascular accident. Amantadine sulfate was used in the first three hours of the disease in the form of an infusion solution (dose 1000 ml (400 mg) per day intravenously for 5 days from the moment the patient was admitted to the hospital). The results showed that there was a decrease in the severity of the condition of patients according to the SAPS scale. Decrease from 14.8 to 6.7 points in the study group by the eighth day of illness (in comparison, from 14.9 to 8.8 points). The dynamics of neurological deficit on a certain scale was more pronounced in patients treated with PK-Merz, and convincingly it continued to decrease by the 120th day.

Thus, the clinical efficacy of glutamate receptors (amantadine sulfate) in the treatment of brain damage of vascular origin was confirmed in a large number of patients who received this drug in the course of conducting controlled studies using control drugs or placebo. Clinical results using amantadine were better or as good as those obtained in the control groups, and also superior to the results obtained in the placebo groups.

The inclusion of this drug in the complex in the treatment of acute cerebral insufficiency simultaneously with bioflavonoids, cytoprotectors and choline donators will reduce mortality, reduce the number of complications, and improve the prognosis in patients with acute cerebrovascular insufficiency.

Contraindications to the use of the drug

Contraindications for the use of amantadine sulfate are as follows:

  • severe congestive heart failure;
  • myocarditis; cardiomyopathy;
  • hypokalemia;
  • hypomagnesemia;
  • AV blockade of the I2nd and 3rd degree;
  • elongation of a special defined interval of more than 420 ms;
  • bradycardia (heart rate less than 55 beats per minute).
  • ventricular arrhythmia;
  • severe renal failure;
  • simultaneous reception with means that lengthen the special interval;
  • childhood;
  • pregnancy;
  • breastfeeding period;
  • phenylketonuria.

Amantadine INN

International name: Amantadine

Dosage form: solution for infusion, tablets, coated tablets

Chemical Name:

1 - aminoadamantane glucuroid (tricyclodecane - 1 - amine hydrochloride) or tricyclodecane - 1 - amine (and as glucuronide, hydrochloride or sulfate)

Pharmachologic effect:

Antiparkinsonian and antiviral agent, tricyclic symmetrical adamantamine. It blocks glutamate NMDA receptors (including in the substantia nigra), thereby reducing the excessive stimulating effect of cortical glutamate neurons on the neostriatum, which develops against the background of insufficient dopamine release. By reducing the flow of ionized Ca2+ into neurons, it reduces the possibility of their destruction. To a greater extent affects stiffness (rigidity and bradykinesia). Reduces the penetration of influenza A virus into cells (different degrees of in vitro activity against other viruses have been noted).

Pharmacokinetics:

After oral administration, it is well absorbed in the gastrointestinal tract. TCmax - 5 h; T1 / 2 amantadine sulfate - 12-13 hours, amantadine hydrochloride - 30 hours. Excreted by the kidneys unchanged.

Indications:

Parkinson's disease, parkinsonism syndrome; neuralgia in shingles caused by Varicella zoster. Influenza A (prevention, including in combination with vaccination and treatment).

Contraindications:

Hypersensitivity, liver failure, chronic renal failure, psychosis (history), thyrotoxicosis, epilepsy, angle-closure glaucoma, prostatic hyperplasia, arterial hypotension, CHF II-III stage, state of excitation, predelirium, delirious psychosis, pregnancy (I trimester), lactation period , simultaneous administration of triamterene / hydrochlorothiazide. C with caution. Orthostatic arterial hypotension, allergic dermatitis, pregnancy (II-III trimesters), old age, alcoholism, mental disorders (including history).

Dosing regimen:

Inside, after meals, with Parkinson's disease, the initial dose is 100 mg / day with an interval of 6 hours (the last dose before dinner) for 3 days, from 4 to 7 days - 200 mg / day, for 2 weeks - 300 mg / day days, from 3 weeks, depending on the patient's condition - 300-400 mg / day. The maximum dose is 600 mg / day. 200 mg is administered intravenously 1-3 times a day for 3 hours, the infusion rate is 55 drops / min. The duration of infusion therapy is 5-7 days. In case of impaired renal function, the dose is reduced and the intervals between doses are increased; at a glomerular filtration rate of 80-60 ml / min - 100 mg every 12 hours, 60-50 ml / min - 200 and 100 mg alternately every second day, 30-20 ml / min - 200 mg 2 times a week, 20-10 ml / min - 100 mg 3 times a week, less than 10 ml / min - 200 mg 1 time per week and 100 mg every other week. With neuralgia associated with Varicella zoster - in / in 1-2 infusions per day for 14-17 days. In elderly patients, reduced doses are used. For the prevention and treatment of influenza - orally 200 mg / day for 10 days. Children - 4.4-8.8 mg / kg / day, but not more than 150 mg / day.

Side effects:

From the nervous system: motor or mental agitation, convulsions, headache, dizziness, irritability, insomnia, tremor, mental disorders accompanied by visual hallucinations. From the CCC: the development or aggravation of heart failure, tachycardia, orthostatic hypotension, arrhythmogenic effect. From the digestive system: dry mouth, nausea, loss of appetite, dyspepsia. From the urinary system: acute urinary retention in patients with prostatic hyperplasia, polyuria, nocturia. Others: dermatosis, the appearance of a bluish coloration of the skin of the upper and lower extremities, decreased visual acuity.

Special instructions:

Information about the effectiveness in the treatment of extrapyramidal disorders during treatment with antipsychotic drugs (drug parkinsonism) is contradictory. Therapy should not be stopped suddenly, because. a sharp exacerbation of the disease is possible. During therapy, patients suffering from CHF or peripheral circulatory disorders require constant medical supervision. The use of ethanol while taking the drug is contraindicated. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Interaction:

Drugs that stimulate the central nervous system (including psychostimulants), ethanol increase the risk of side effects. Compatible with central anticholinergics and other antiparkinsonian drugs.

Recipe (international)

Rp.: Amantadini 0.1

D. No. 30 in tab.

S.: 1 tablet 3 times a day

Recipe (Russia)

Prescription form - 107-1 / y

pharmachologic effect

Antiparkinsonian and antiviral agent, tricyclic symmetric adamantanamine.

It blocks glutamate NMDA receptors and thereby reduces the excessive stimulating effect of cortical glutamate neurons on the neostriatum, which develops against the background of dopamine deficiency. Amantadine inhibits the NMDA receptors of the substantia nigra neurons, reduces the supply of Ca2+ to them, which reduces the possibility of destruction of these neurons. To a greater extent affects stiffness (rigidity and bradykinesia).

Inhibits the penetration of the influenza A virus into the cell.

Mode of application

For adults:

Inside, after meals, with Parkinson's disease, the initial dose is 100 mg / day with an interval of 6 hours (the last dose before dinner) for 3 days, from 4 to 7 days - 200 mg / day, for 2 weeks - 300 mg / day days, from 3 weeks, depending on the patient's condition - 300-400 mg / day. The maximum dose is 600 mg / day.

200 mg is administered intravenously 1-3 times a day for 3 hours, the infusion rate is 55 drops / min. The duration of infusion therapy is 5-7 days.
In case of impaired renal function, the dose is reduced and the intervals between doses are increased; at a glomerular filtration rate of 80-60 ml / min - 100 mg every 12 hours, 60-50 ml / min - 200 and 100 mg alternately every second day, 30-20 ml / min - 200 mg 2 times a week, 20-10 ml / min - 100 mg 3 times a week, less than 10 ml / min - 200 mg 1 time per week and 100 mg every other week.

With neuralgia associated with Varicella zoster - in / in 1-2 infusions per day for 14-17 days. In elderly patients, reduced doses are used.

For the prevention and treatment of influenza - orally 200 mg / day for 10 days.


For kids: Children - 4.4-8.8 mg / kg / day, but not more than 150 mg / day.

Indications

tablets
Parkinson's Syndrome: Treatment for symptoms of Parkinson's disease such as rigidity, tremors, hypokinesia and akinesia.
Extrapyramidal side effects of neuroleptics and other drugs: early dyskinesia, akathisia and parkinsonism.

Solution
Intensive care and initial treatment of an akinetic crisis with a sharp exacerbation of the symptoms of parkinsonism.
Increasing the ability to focus attention (vigilance) in post-coma states of various etiologies in a hospital setting.

Contraindications

Liver failure in history;
The presence of psychosis;
Chronic renal failure;
With thyrotoxicosis;
In the presence of epilepsy;
Do not use the drug in ophthalmic pathology, in particular in angle-closure glaucoma;
With prostatic hyperplasia, the drug is also not used;
A history of high blood pressure is also a contraindication;
Chronic heart failure in history;
You can not use this tool in an excited state;
With predelirium, as well as with delirious psychosis, Amantadine is contraindicated;
Do not prescribe the drug during pregnancy, especially in its first trimester;
The period of lactation is also considered a contraindication;
With hypersensitivity to Amantadine. In addition to the listed conditions, contraindication is the simultaneous use with drugs such as triamterene and hydrochlorothiazide.

Side effects

From the nervous system and sensory organs: dizziness, insomnia, anxiety, irritability, decreased visual acuity, agitation, tremor, convulsions, visual hallucinations.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): development or aggravation of heart failure, tachycardia, orthostatic hypotension.

From the digestive tract: anorexia, nausea, dry mouth, dyspepsia.

Others: urinary retention in patients with prostatic hyperplasia, polyuria, nocturia, peripheral edema, dermatosis, the appearance of a bluish coloration of the skin of the upper and lower extremities.

Release form

Coated tablets.
Tablets.
Substance-powder.
Solution for intravenous drip infusions (infusions).

ATTENTION!

The information on the page you are viewing was created for informational purposes only and does not promote self-treatment in any way. The resource is intended to familiarize healthcare professionals with additional information about certain medicines, thereby increasing their level of professionalism. The use of the drug "" without fail provides for a consultation with a specialist, as well as his recommendations on the method of application and dosage of the medicine you have chosen.

Amantadine hydrochloride is a tricyclic amine that is minimally metabolized and excreted in the urine (with elevated creatinine levels in patients, the dose should be reduced). In the gastrointestinal tract, amantadine is well absorbed. The maximum level in the blood occurs after 1-4 hours, the half-life is 15 hours in healthy patients, but may vary depending on age (14.7 in young people, 28.9 in older people).

At the beginning of use, the mechanism of action of the drug was not fully known. Numerous clinical and neurochemical studies have shown that amantadine has a presynaptic/postsynaptic effect and blocks NMDA receptors.

By acting on presynaptic membranes, the drug enhances the release of catecholamine stores of intact dopamine terminals, increases the level of extravesicular intraneuronal dopamine in patients previously treated with drugs such as reserpine and tetrabenzine that block the presynaptic membrane, and also inhibits the reuptake of dopamine by presynaptic terminals.

Postsynaptically, amantadine activates dopamine receptors and fixes them in a highly sensitive configuration (like agonists). During the experiment, the drug showed direct dopaminagonistic and anticholinergic effects, in particular, stimulation of motor activity was observed, a decrease in rigidity in catecholamine-depleted animals.

According to recent data, the main mechanism of action of amantadine lies in its ability to block glutamate, namely, NMDA receptors. It is known that prolonged activation of glutamate receptors in the striatum, seahorse, and other brain structures leads to long-term potentiation. However, as a result of excessive stimulation of glutamate receptors, a pathological process of glutamate excitotoxicity develops, which underlies the pathogenesis of many neurodegenerative diseases of the brain, including progressive degeneration of dopaminergic neurons in PD and GABA-ergicity of spiny neurons in Guntington's disease.

Normally, NMDA receptors are blocked by Mg 2+. Prolonged stimulation with glutamate leads to the release of Mg 2+ from the channel, which allows the flow of Ca 2+ to enter cells in an uncontrolled large amount, which leads to oxidative stress, degradation of proteins, membranes, and cell apoptosis. Amantadine has been found to block NMDA receptors, similar to Mg 2+. The drug enters the open NMDA receptor, attaches its blocking side deep into the receptor channel and stays there for a long time.

Amantadine, by blocking NMDA receptors, causes the closure of their channels for Ca2 + ions.

A number of studies have shown the neuroprotective effect of amantadine in PD and parkinsonism.

The antiglutamatergic action of amantadine by blocking NMDA receptors has sharpened the theoretical and clinical interest in the drug.

Side effect

The side effects of amantadine are mostly minor and do not lead to treatment limitation.

Most often, livedo reticularis, swelling of the legs, dry mouth, difficulty concentrating, hallucinations are observed.

All complications from taking the drug disappear after its withdrawal and do not lead to irreversible changes.

So, taking into account all of the above, we can draw the following conclusions.

  1. Amantadine is an effective drug for the treatment of PD.
  2. The therapeutic effect of the drug is observed 24 hours after the start of administration.
  3. Amantadine is recommended for use as a monotherapy in the initial stages of the disease, as well as a pathogenetic therapy for more severe stages of the disease, especially in patients with levodopa-induced dyskinesias.
  4. Amantadine is well tolerated with few side effects.
  5. The drug has an activating effect on the hippocampus, subcortical structures and is recommended for patients with bradyphrenia and cognitive impairment.
  6. The mechanism of action of amantadine allows it to be prescribed for fasting and presynaptic parkinsonism caused by various factors (toxic, infectious, traumatic, degenerative).

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> > Amantadine: instructions for use and prices

active substance: amantadine sulfate

1 tablet contains amantadine sulfate 100 mg

Excipients: lactose, microcrystalline cellulose, potato starch, gelatin, povidone, croscarmellose sodium, talc, colloidal silicon dioxide, magnesium stearate, Opadry II White (polyethylene glycol, polyvinyl alcohol, talc, titanium dioxide (E 171)).

Dosage form

Film-coated tablets.

Pharmacological group

Antiparkinsonian drugs. dopaminergic agents.

ATC code N04B B01.

Indications

  • Parkinson's disease, parkinsonism of various etiologies;
  • neuralgia with herpes zoster (Herpes zoster);
  • prevention and treatment of influenza A.

Contraindications

Hypersensitivity to amantadine or to any component of the drug epilepsy and other convulsive seizures; severe renal failure peptic ulcer.

Dosage and administration

Tablets are taken orally after meals, with a small amount of liquid, preferably in the morning and / or afternoon. Due to the possible activating effect on the central nervous system (CNS), the last dose is recommended to be taken no later than the sixteenth hour.

Parkinson's disease. Dosing regimen is individual. The recommended initial dose is 100 mg (1 tablet) Amantine 1 time per day for the first 7 days, followed by an increase in dose to 100 mg 2 times a day. The dose should be increased gradually at weekly intervals until an effective therapeutic dose is reached, which should be taken in 2 divided doses. Doses above 200 mg per day may provide additional therapeutic benefit but may also increase toxicity. The maximum daily dose is 400 mg.

Elderly patients (over 65 years of age) are recommended to prescribe the minimum effective dose due to the trend towards a decrease in renal clearance and a subsequent increase in the level of amantadine in the blood plasma.

In some cases, continuous treatment with amantadine for several months may reduce the effectiveness. Efficacy can be improved by discontinuing amantadine for 3-4 weeks. During this time period, concomitant antiparkinsonian therapy should be continued or treatment with a low dose of levodopa should be started if clinically necessary.

Amantine is usually prescribed in combination with other antiparkinsonian drugs. In this case, the dose of Amantine is selected individually.

Treatment with Amantine should be stopped gradually, for example at ½ dose at weekly intervals. Abrupt discontinuation of treatment may worsen the course of parkinsonism, to the point of an akinetic crisis. In case of increased side effects, the dose of Amantine should be reduced more quickly. In patients receiving high doses of anticholinergics or levodopa, the start of treatment with Amantine should be delayed by 15 days.

For the treatment of influenza A appoint 100 mg every 12:00, patients over the age of 65 - no more than 100 mg per day.

For treatment, the drug is used no later than 18-24 hours after the onset of the first symptoms of influenza, the duration of treatment is 5 days.

To prevent influenza A Amantine is used at 100 mg per day for 2-4 weeks.

For the treatment of neuralgia in herpes zoster (Herpes zoster) appoint 100 mg twice a day for 14 days. Therapy should begin as soon as possible after diagnosis. In case of persistent postherpetic pain, treatment may be continued for the next 14 days.

Dosage for patients with impaired renal function.

In patients with impaired renal function, the dose of amantadine should be reduced by reducing the total daily dose or increasing the interval between doses of the drug, depending on creatinine clearance, as shown in the table:

QC, ml / min

Dosage of the drug, mg

Amantine is contraindicated

100 mg every second to third day

100 mg daily

Adverse reactions

Adverse reactions to amantadine are often mild and transient. As a rule, they appear within 2-4 days from the start of treatment and quickly disappear after stopping the drug.

From the blood and lymphatic system: leukopenia.

From the nervous system: anxiety, dizziness, headache, drowsiness, insomnia, weakness, agitation, fever, ataxia, slurred speech, impaired concentration, irritability, depression, myalgia, paresthesia, confusion, disorientation, psychosis, tremor, convulsions , dyskinesia, stupor, suicidal thoughts and intentions, neuroleptic malignant syndrome, delirium, hypomania and mania, hallucinations, nightmares. Paranoid exogenous psychoses, which are accompanied by visual hallucinations, are more often observed when used together with anticholinergic drugs and in patients prone to mental disorders.

From the side of the organs of vision: corneal lesion (punctate subepithelial opacification, which may be associated with superficial punctate keratitis), corneal epithelial edema, decreased visual acuity, oculogyric crises, mydriasis.

From the side of the cardiovascular system: orthostatic hypotension, cardiac arrhythmia, tachycardia, QT prolongation, peripheral edema, heart failure , "marble skin" (appearance of a reticulate bluish tint to the skin), sometimes associated with swelling of the ankle joint. May occur after taking high doses of the drug or use for a long period.

From the digestive tract: nausea, dry mouth, anorexia, vomiting, constipation, diarrhea, reversible increase in liver enzymes.

From the skin and subcutaneous tissue: skin rashes, itching, increased sweating, photosensitivity, eczematous dermatitis.

From the genitourinary system: urinary retention in patients with prostatic hyperplasia, urinary incontinence, changes in libido.

Other: hypersensitivity reactions with intolerance to any component of the drug.

Overdose

An overdose of amantadine can be fatal.

Symptoms. A significant place in the overdose of amantadine is occupied by the symptoms of acute psychosis and neuromuscular disorders. Hyperreflexia, restlessness, convulsions, extrapyramidal phenomena, torsion spasms, dilated pupils, dysphagia, confusion, disorientation, delirium, visual hallucinations, myoclonus, nausea, vomiting, dry mouth, hyperventilation, pulmonary edema, respiratory failure, respiratory distress syndrome , hypertension, cardiac arrhythmia, tachycardia, angina attacks, cardiac arrest.

Possible impaired renal function, including an increase in urea nitrogen and a decrease in creatinine clearance, urinary retention.

Treatment. There is no specific antidote. To prevent absorption of the drug, it is necessary to induce vomiting or gastric lavage (if the patient is conscious), take activated charcoal; ensure the maintenance of vital body functions, adequate hydration. For rapid excretion of the drug, an acidic urine reaction is provided. With the help of hemodialysis, a small amount of the drug is excreted. Careful monitoring of blood pressure, heart rate, ECG, respiratory function, body temperature is recommended for the timely detection of the development of hypotension and cardiac arrhythmia and, if necessary, their treatment. To reduce the severity of symptoms from the central nervous system, adults are recommended to prescribe physostigmine at a dose of 1 mg, if necessary, repeatedly, but not more than 2 mg per hour. With urinary retention - it is necessary to carry out catheterization of the bladder.

Use during pregnancy and lactation

Amantine is contraindicated during pregnancy and women planning a pregnancy. The drug is contraindicated during lactation, as it passes into breast milk. If necessary, the use of the drug breast-feeding should be discontinued.

Children

Experience with the drug in children is not enough.

Application features

Special care must be taken when using the drug in patients with:

  • psychoses;
  • agitation or confusion;
  • dysfunction of the liver and kidneys;
  • heart failure
  • thyrotoxicosis;
  • prostatic hyperplasia;
  • recurrent eczema;
  • when used simultaneously with drugs that affect the central nervous system (see section "Interaction with other drugs and other types of interactions").

The drug should be used with caution in patients with cardiovascular diseases, including rhythm and conduction disorders, electrolyte imbalance.

Amantine treatment should not be stopped suddenly, as this can lead to worsening of Parkinson's disease, the appearance of symptoms characteristic of neuroleptic malignant syndrome, as well as the development of cognitive impairment, such as: catatonia, confusion, disorientation, worsening mental state, delirium.

You should not abruptly stop taking Amantine in patients who are simultaneously using antipsychotics, due to the possible risk of developing neuroleptic malignant syndrome or neuroleptic-induced catatonia.

Suicidal attempts and suicidal thoughts have been reported in patients treated with amantadine. In order to prevent the occurrence of suicidal thoughts and intentions, the drug must be prescribed in the minimum effective doses.

In some patients, with prolonged use of the drug, peripheral edema may occur. This should be taken into account in persons with chronic heart failure.

The drug should not be used in patients with angle-closure glaucoma.

The drug contains lactose, so patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use Amantine.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms.

The drug can reduce concentration and response speed, cause dizziness, decreased visual acuity, so patients should be warned about the potential danger when driving or working with mechanisms.

Interaction with other medicinal products and other forms of interaction

A combination of amantadine with anticholinergics and other antiparkinsonian drugs is possible. In combination with other antiparkinsonian drugs, a mutual enhancement of the therapeutic effect is observed. However, concomitant use of amantadine and anticholinergics or levodopa may increase confusion, hallucinations, nightmares, gastrointestinal disturbances, or other atropine-like side effects. Psychotic disorders may occur in patients receiving amantadine and levodopa.

Avoid concomitant use with memantine.

In rare cases, worsening of psychotic symptoms may occur in patients who simultaneously use amantadine and neuroleptics.

The simultaneous use of amantadine and drugs or substances that act on the central nervous system (including alcohol-containing drugs) can increase the toxic effect on it. In such cases, careful monitoring of the patient is recommended. During treatment with amantadine, you should not drink alcoholic beverages.

The concomitant use of diuretics such as triamterene/hydrochlorothiazide and Amantine may reduce the excretion of amantadine from blood plasma, leading to toxic plasma concentrations of the latter.

The concomitant use of diuretics and Amantine should be avoided.

The simultaneous use of Amantin and drugs that prolong the QT interval is contraindicated.

Pharmacological properties

Pharmacodynamics. Antiparkinsonian, antiviral agent. Tricyclic symmetrical adamantamine. It blocks glutamate NMDA receptors, reducing the excessive stimulating effect of cortical glutamate neurons on the neostriatum, which develops against the background of insufficient release of dopamine and thereby reducing the manifestations of parkinsonism. Significantly affects stiffness (rigidity and bradykinesia). Eliminates extrapyramidal side effects of neuroleptics and other drugs: early dyskinesia, akathisia and parkinsonism. In addition, amantadine also has some anticholinergic activity.

The antiviral effect is associated with the ability of amantadine to block the penetration of influenza A virus into cells.

Mechanism of action of Amantine in treatment herpes zoster not fully defined.

Pharmacokinetics. After oral administration, amantadine is well absorbed in the digestive tract. The maximum plasma concentration is reached 4:00 after taking a single dose (100 mg) and is 0.15 µg/ml. When taking the drug at a dose of 200 mg / day, the state of equilibrium concentration is reached after 4-7 days. The conditional volume of distribution is 4.2 ± 1.9 l / kg and depends on age, in the elderly - 6 l / kg.

The half-life is 10-30 hours (average 15 hours) and largely depends on the age of the patient. In elderly male patients (62-72 years), the elimination half-life is 30 hours. In patients with renal insufficiency, the terminal half-life can be significantly prolonged (up to 68 ± 10:00).

Amantadine binds to plasma proteins by 67% ( in vitro) about 33% is found in plasma in unbound form. Penetrates through the blood-brain barrier, placental barrier, into breast milk. It is excreted in the urine almost unchanged (90% of a single dose), a small amount is excreted in the feces.

The dialysis capacity of amantadine is low, approximately 5% per dialysis.

Basic physical and chemical properties

round, bevelled, scored, white film-coated tablets.

Best before date. 3 years.

Storage conditions

Keep out of the reach of children in the original packaging at a temperature not exceeding 25 ° C.

Package.

10 tablets in a blister, 3 or 6 blisters in a cardboard box.