Pharmacological action

Amitriptyline is used as the antidepressant, anxiolytic, sedative and anti dysuric drug. It inhibits the neuronal uptake of the norepinephrine, dopamine and serotonin in the central nervous system (CNS). It also blocks m-cholinergic receptors.In case of long-term use of Amitriptyline this drug is able to reduce the functional activity of the beta-adrenergic and serotonin receptors in the brain and restore the balance of these systems, impaired in patients with depressive states. In patients with anxiety-depressive states it reduces anxiety, agitation and depressive symptoms. The antidepressant effect of the drug is observed during the second or third week of the Amitriptyline treatment. In case when the patient suddenly stops taking Amitriptyline after the long-term use of the drug, the withdrawal syndrome is possible.

Pharmacokinetics: Amitriptyline is produced in the form of white odorless crystalline powder soluble in water. It is well absorbed from the gastrointestinal tract. The bioavailability of the drug (depending on the routes of administration is 30-60%, and the bioavailability of its metabolite (nortriptyline) is 46-70%. C_max in the blood is reached in 2,0-7,7 hours after the Amitriptyline btc administration. Therapeutic blood concentrations of Amitriptyline are 50-250 ng / ml, and therapeutic blood concentrations of nortriptyline are 50-150 ng / ml. T 1/2 is 10-26 hours for Amitriptyline, and 18-44 hours for nortriptyline. The biotransformation of Amitriptyline (demethylation, hydroxylation, N-oxidation) takes place in the liver. As the result of biotransformation the active metabolites (nortriptyline, 10-hydroxy-amitriptyline) and inactive metabolites are produced. Amitriptyline is excreted by the kidneys (mostly in the form of metabolites) during several days after the drug administration.

Indications for use: Amitriptyline is prescribed in case of endogenous, involutional, reactive, neurotic or medicamentous depressions or in case of depressions caused by the organic brain damage. It is also effective in case of depressive syndrome, schizophrenic psychosis, anxiety-depressive states of various origins, mixed emotional disturbances, behavioral disorders, psychogenic anorexia, nocturnal enuresis or severe pains of neurogenic nature.

Contraindications: Being the most widely used TCA, Amitriptyline has the range of contraindications. It is not recommended for use in patients having hypersensitivity to this drug, as well as in patients with glaucoma, epilepsy, prostatic hyperplasia, bladder atony, pseudoileus, pyloristenosis, myocardial infarction in past history and in patients who used MAO inhibitors during two weeks before the start of the Amitriptyline bitcoin treatment. It is also shouldn't be prescribed in any case to the pregnant women or to the nursing mothers, as well as to the children aged less than 6 years old.

Side effects: While Amitriptyline treatment some side effects can be observed. Due to the blockade of peripheral M-cholinergic it can be dry mouth, urinary retention, constipation, blurred vision or the accommodation disturbance, and desudation. As for the buy Amitriptyline btc effect on the cardiovascular system, the tachycardia, orthostatic hypotension, pressure rise, asequence and ECG changes can be observed. As for the CNS, Amitriptyline administration can cause drowsiness, dizziness or tremor. Allergic reactions, such as rash are also possible.

Interaction with other drugs: Amitriptyline is incompatible with MAO inhibitors. It also potentiates the effect of compounds, which are CNS depressants (sedatives, hypnotics and alcohol inclusive), sympathomimetics and antiparkinsonian drugs, and weakens the effect of antihypertensive and anticonvulsant medications. The inducers of microsomal oxidation (such as barbiturates or carbamazepine) are able to reduce the concentration of Amitriptyline in the blood plasma, and cimetidine, on the contrary, increases the concentration of the drug in the plasma of the blood.

Precautionary measures: If Amitriptyline is prescribed to the elderly people or children, the reduced doses of the drug are highly recommended. Amitriptyline shouldn't be taken by the suicidal patients or manic patients. In patients with CHD, cardiac arrhythmia or heart failures it should be prescribed and taken with great care. While following the buy Amitriptyline bitcoin treatment, the alcohol drinking should be avoided. Take into your consideration the fact that Amitriptyline affects the quick reaction capability and focus. In case you follow Amitriptyline treatment, try to avoid the activities where the attention and quick reaction are highly needed. Amitriptyline is prescribed by the doctor and cannot be used without doctor's recommendations.

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