Amantadine - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

Midantan

pills inwards

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Neomidantan

capsules inwards

Olainfarm, AO Latvia

PC-Merz

pills inwards

Merz Pharma GmbH & Co. KG. KGaA Germany

PC-Merz

solution d / infusion

Merz Pharma GmbH & Co. KG. KGaA Germany

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

ONLS

АТХ:

N.04.B.B.01 Amantadine

Pharmacodynamics:

Amantadine has a moderate anti-Parkinsonian effect.

Strengthens the release of dopamine from intact neurons into the synaptic cleft and disrupts the reverse neuronal capture of dopamine. An increase in the concentration of dopamine in the central nervous system leads to a decrease in the severity of symptoms of Parkinson's disease. Interaction of amantadine with NMDA-receptors of cholinergic neurons of basal nuclei. Amantadine, blocking these receptors, interferes with the stimulating effect of glutamate on cholinergic neurons. This leads to the inhibition of cholinergic transmission in the neostriatum. Has some anticholinergic activity. Neuroprotective effect of amantadine in relation to dopaminergic neurons of a black substance is also possible.This is associated with the blockade of NMDA receptors localized on these neurons and a decrease in the intake of calcium ions into nerve cells that prevent their destruction.

Amantadine has an antiviral effect. There is a blockage of the rupture of the envelope of the influenza A virus and the release of its nucleic acid into the epithelial cells of the respiratory system; inhibition of the early replicative phase of the virus that penetrated the cell. Amantadine blocks M2-proton channels and, preventing the acidification of the internal environment of the virion, disrupts the process of dissociation of ribonucleoproteins from the protein matrix and the release of the viral genome. Thus, the drug acts at an early stage of virus reproduction and is therefore more effective for the prevention of influenza A or at an early stage of the disease. There is evidence of their possible effect at a later stage associated with a change in the conformation of hemagglutinin.

Pharmacokinetics:Absorption is high, complete. Penetrates through blood-brain barrier and the placenta, into breast milk. Tissue concentrations (especially in the lungs) are higher than plasma concentrations. The connection with plasma proteins is 67%. Virtually not metabolized. Half-life - 11-15 hours (in the elderly 24-29 hours). The onset of antidiskinetic activity is at 48 h. Elimination in unchanged form by the kidneys exceeds 90%.

Indications:

Parkinson's disease;

Parkinsonism (rigidity and akinetic forms);

Postencephalic syndrome;

Symptomatic Parkinsonism (with carbon monoxide poisoning and cerebral atherosclerosis);

Extrapyramidal disorders caused by the administration of neuroleptics or other drugs;

Neuralgia with shingles, caused by the virus Varicella zoster;

Loss of consciousness due to traumatic brain injury;

Slow exit from anesthesia;

Residual effects after stereotactic operations;

Prevention and treatment of influenza (influenza A virus), including in combination with vaccination.

ICD-10

VI.G20-G26.G20 Parkinson's disease

VI.G20-G26.G21 Secondary Parkinsonism

I.B00-B09.B02.2 Shingles with other complications from the nervous system

X.J10-J18.J10 Influenza caused by an identified influenza virus

Contraindications:

Hypersensitivity, hepatic and / or renal insufficiency, psychoses (in the anamnesis), a condition of exaltation, predelly, delirious psychosis, epilepsy.

Thyrotoxicosis, zakratougolnaya glaucoma, prostatic hyperplasia, heart failure II-III stage, arterial hypotension.

Pregnancy (I trimester), breast-feeding; simultaneous administration of triamterene and hydrochlorothiazide.

Carefully:Orthostatic arterial hypotension, allergic dermatitis, pregnancy (II-III trimester), elderly age, alcoholism, mental disorders (including history).

Pregnancy and lactation:

The action category for the fetus by the FDA is C. Passes through the placenta. Controlled studies are not conducted. Embryotoxicity and teratogenicity are proven in human studies (tetralogy of Fallot in an infant whose mother took the drug at a dose of 100 mg orally for 7 days at the 6-7th week of pregnancy; single ventricle, pulmonary atresia with 100 mg amantadine daily during the first 2 weeks of pregnancy) and animal experiments. Applied only if the benefit exceeds the potential risk to the fetus.

Penetrates into breast milk. Action on newborns and children of the first year of life has not been studied. Do not apply!

Dosing and Administration:Inside, after eating. Adults: the initial dose is 100 mg per day, if necessary, after 1 week, an increase in the dose to 200 mg per day is possible; the maximum daily dose is 400 mg.In connection with the possible activating effect on the central nervous system, the last dose is recommended to be taken no later than 16 hours. In case of impaired renal function and in elderly patients, the dose reduces and increases the interval between doses. Usually amantadine prescribe in combination with other antiparkinsonian means. Intravenously: 200 mg 1-3 times a day for 3 hours (infusion rate 50-60 drops per minute).

For the prevention and treatment of influenza appoint 200 mg per day for at least 10 days.

Side effects:

From the nervous system and sense organs: headaches, dizziness, depression, anxiety, irritability, insomnia, decreased visual acuity, sleep disorders, motor and mental arousal, tremor, convulsions, visual hallucinations.

From the side of the cardiovascular system: development or aggravation of heart failure, tachycardia, arrhythmogenic effect, orthostatic hypotension.

On the part of the digestive system: anorexia, nausea, dry mouth, indigestion.

From the genitourinary system: retention of urine in patients with prostatic hyperplasia, polyuria, nocturia, peripheral edema.

Dermatological reactions: dermatosis, the appearance of bluish coloration of the skin of the upper and lower extremities.

Overdose:

Symptoms: agitation, aggression, confusion, convulsions, impaired renal function, pulmonary edema, arrhythmia (including malignant tachyarrhythmia), hypertension, hyperthermia.

Treatment is symptomatic: intravenous injection of physostigmine (elimination of central effects). Hemodialysis is not effective. Acidification of urine helps the faster removal of amantadine. The minimum lethal dose is 1 g.

Interaction:

Alcohol - dizziness, confusion, orthostatic hypotension.

Anti-Parkinsonics: increased side effects.

Thiazide diuretics: development of toxic effects of amantadine (ataxia, excitation, hallucinations), probably due to a decrease in its renal clearance.

Stimulators of the central nervous system: excessive stimulation of the central nervous system - nervousness, irritability, insomnia, convulsions and cardiac arrhythmias.

Quinine, quinidine, trimethoprim and sulfamethoxazole: a disorder of renal clearance of amantadine, an increase in its plasma concentration, a decrease in excretion in the urine.

Holin blockers and other drugs,possessing anticholinergic activity: potentiation of anticholinergic effects (confusion, hallucinations, nightmares, intestinal peristalsis).

Special instructions:

When Parkinson's disease is used in combination with levodopa, benzohexol. In terms of effectiveness, it is comparable with biperidenum, triexyphenidyl in extrapyramidal disorders caused by neuroleptics, in patients with schizophrenia. For the prevention and treatment of influenza A, it is comparable in effectiveness to rimantadine, but causes more side effects.

Influence on the ability to drive vehicles and control mechanisms: during the period of treatment should not engage in activities that require high concentration of attention and rapid psychomotor reactions.

Avoid abrupt discontinuation of the drug.

Instructions

Amantadine (Amantadinum)