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Amitriptyline

Amitriptyline
Amitriptyline belongs to the group of antidepressants, has a sedative effect, improves mood, and helps to eliminate bedwetting.

Brand: Amitriptyline

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: December 2023
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Amitriptyline 100 mg
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Amitriptyline 50 mg
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90 pills - 50 mg $43.25 $0.48 $8.55 Add to cart
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Amitriptyline 25 mg
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Product description

Pharmacological action of Amitriptyline

Buy Amitriptyline in Canada

An antidepressant from the group of tricyclic compounds, a derivative of dibenzocycloheptadine.

The mechanism of antidepressant action is associated with an increase in the concentration of norepinephrine in the synapses and / or serotonin in the central nervous system due to inhibition of the reverse neuronal uptake of these mediators. With prolonged use, it reduces the functional activity of β-adrenergic receptors and serotonin receptors of the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, disturbed in depressive conditions. In anxiety-depressive states, it reduces anxiety, agitation and depressive manifestations.

It also has some analgesic effect, which is believed to be associated with changes in the concentration of monoamines in the central nervous system, especially serotonin, and the effect on the endogenous opioid systems.

Treating depression with amitriptyline

It has a pronounced peripheral and central anticholinergic effect due to a high affinity for m-cholinergic receptors; a strong sedative effect associated with an affinity for histamine H1receptors, and an alpha-adrenergic blocking effect.

It has an anti-effect, the mechanism of which is due to the ability to block histamine H2ulcer-receptors in the parietal cells of the stomach, as well as to have a sedative and m-anticholinergic effect (in case of gastric ulcer and duodenal ulcer, it reduces pain syndrome, promotes the acceleration of ulcer healing).

Efficacy in bed-wetting is apparently due to anticholinergic activity, leading to an increase in the ability of the bladder to stretch, direct β-adrenergic stimulation, the activity of α-adrenergic receptor agonists, accompanied by an increase in sphincter tone and central blockade of serotonin uptake.

The mechanism of therapeutic action in bulimia nervosa has not been established (possibly similar to that in depression). A distinct efficacy of amitriptyline has been shown for bulimia in patients with and without depression, while a decrease in bulimia can be observed without a concomitant weakening of depression itself.

During general anesthesia, it lowers blood pressure and body temperature. Does not inhibit MAO.

The antidepressant effect develops within 2-3 weeks after the start of use.

Pharmacokinetics

Bioavailability of amitriptyline is 30-60%. Plasma protein binding 82-96%. Vd - 5-10 l / kg. It is metabolized to form the active metabolite of nortriptyline.

T1/2 - 31-46 hours. It is excreted mainly by the kidneys.

Indications of the active substances of the drug Amitriptyline

Depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, medicinal, with organic brain lesions, alcohol withdrawal), schizophrenic psychoses, mixed emotional disorders , behavioral disorders (activity and attention), nocturnal enuresis (with the exception of patients with hypotension of the bladder), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic pain, atypical pain in the face, postherpetic neuralgia, post-traumatic neuropathy , diabetic neuropathy, peripheral neuropathy), prevention of migraine, gastric ulcer and duodenal ulcer.

Dosage regimen of Amitriptyline

Packaging of Amitriptyline tablets

For oral administration, the initial dose is 25-50 mg at night. Then, within 5-6 days, the dose is individually increased to 150-200 mg / day (most of the dose is taken at night). If during the second week there is no improvement, the daily dose is increased to 300 mg. When signs of depression disappear, the dose is reduced to 50-100 mg / day and therapy is continued for at least 3 months. In elderly patients with mild disorders, the dose is 30-100 mg / day, usually 1 time / day at night, after reaching the therapeutic effect, they switch to the minimum effective dose - 25-50 mg / day.

With nocturnal enuresis in children aged 6-10 years - 10-20 mg / day at night, at the age of 11-16 years - 25-50 mg / day.

In / m - the initial dose is 50-100 mg / day in 2-4 injections. If necessary, the dose can be gradually increased to 300 mg / day, in exceptional cases - up to 400 mg / day.


Contraindications for use

Acute period and early recovery period after myocardial infarction, acute alcohol intoxication, acute intoxication with hypnotics, analgesic and psychotropic drugs, angle-closure glaucoma, severe violations of AV and intraventricular conduction (bundle branch block, AV block of II degree) lactation period, children under 6 years of age (for oral administration), children under 12 years of age (for intramuscular and intravenous administration), simultaneous treatment with MAO inhibitors and a period of 2 weeks before their use, hypersensitivity to amitriptyline.

Use during pregnancy and lactation

Amitriptyline should not be used during pregnancy, especially in the first and third trimesters, except in cases of extreme necessity. There have been no adequate and strictly controlled clinical studies of the safety of amitriptyline during pregnancy.

Amitriptyline should be withdrawn gradually, at least 7 weeks before the expected birth, in order to avoid the development of withdrawal syndrome in the newborn.

In experimental studies, amitriptyline has a teratogenic effect.

Contraindicated during lactation. It is excreted in breast milk and may cause drowsiness in infants.

Application for violations of liver function

Use with caution in case of violations of liver function.

Application for impaired renal function

Use with caution in impaired renal function.

Use in children

Contraindication: children under 6 years of age (for oral administration), children under 12 years of age (for intramuscular and intravenous administration).

Use in elderly patients

In elderly patients, it can provoke the development of drug psychoses, mainly at night (after discontinuation of the drug, they disappear within a few days), and also cause paralytic intestinal obstruction.

Special instructions

Use with caution in ischemic heart disease, arrhythmias, heart block, heart failure, myocardial infarction, arterial hypertension, stroke, chronic alcoholism, thyrotoxicosis, against the background of therapy with thyroid gland drugs, with impaired liver and / or kidney function.

Against the background of therapy with amitriptyline, caution is necessary with a sharp transition to an upright position from a lying or sitting position.

With a sharp cessation of admission, withdrawal syndrome may develop.

Amitriptyline in doses over 150 mg / day lowers the seizure threshold; the risk of developing epileptic seizures in predisposed patients should be taken into account, as well as in the presence of other factors that increase the risk of developing convulsive syndrome (including with brain damage of any etiology, the simultaneous use of antipsychotic drugs, during the period of refusal of ethanol or drug withdrawal, having anticonvulsant activity).

It should be borne in mind that suicidal attempts are possible in patients with depression.

In combination with electroconvulsive therapy, it should be used only with close medical supervision.

In predisposed patients and elderly patients, it can provoke the development of drug psychoses, mainly at night (after discontinuation of the drug, they disappear within a few days).

May cause paralytic intestinal obstruction, mainly in patients with chronic constipation, the elderly, or in patients who have to comply with bed rest.

Before performing general or local anesthesia, the anesthesiologist should be warned that the patient is taking amitriptyline.

With prolonged use, there is an increase in the frequency of caries. The need for riboflavin may increase.

Amitriptyline can be used no earlier than 14 days after the withdrawal of MAO inhibitors.

Should not be used simultaneously with adrenergic and sympathomimetics, incl. with epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine, phenylpropanolamine.

Use with caution in conjunction with other drugs that have anticholinergic effects.

Avoid drinking alcohol while taking amitriptyline.

Influence on the ability to drive vehicles and mechanisms

During the period of treatment, one should refrain from potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Drug interactions

With simultaneous use with drugs that have a depressing effect on the central nervous system, a significant increase in the inhibitory effect on the central nervous system, hypotensive effect, respiratory depression is possible.

With simultaneous use with drugs with anticholinergic activity, anticholinergic effects may increase.

With simultaneous use, it is possible to increase the effect of sympathomimetic agents on the cardiovascular system and increase the risk of developing cardiac arrhythmias, tachycardia, and severe arterial hypertension.

When used simultaneously with antipsychotics (neuroleptics), metabolism is mutually inhibited, while the threshold of convulsive readiness decreases.

With simultaneous use with antihypertensive drugs (with the exception of clonidine, guanethidine and their derivatives), an increase in the antihypertensive effect and the risk of orthostatic hypotension is possible.

With simultaneous use with MAO inhibitors, the development of a hypertensive crisis is possible; with clonidine, guanethidine - it is possible to reduce the hypotensive effect of clonidine or guanethidine; with barbiturates, carbamazepine - a decrease in the action of amitriptyline due to an increase in its metabolism is possible.

A case of the development of serotonin syndrome with simultaneous use with sertraline is described.

With simultaneous use with sucralfate, the absorption of amitriptyline decreases; with fluvoxamine - the concentration of amitriptyline in the blood plasma and the risk of developing toxic effects increase; with fluoxetine - the concentration of amitriptyline in the blood plasma increases and toxic reactions develop due to inhibition of the CYP2D6 isoenzyme under the influence of fluoxetine; with quinidine - it is possible to slow down the metabolism of amitriptyline; with cimetidine - it is possible to slow down the metabolism of amitriptyline, increase its concentration in blood plasma and develop toxic effects.

When used simultaneously with ethanol, the effect of ethanol is enhanced, especially during the first few days of therapy.


Side effect

From the nervous system: drowsiness, asthenia, fainting, anxiety, disorientation, agitation, hallucinations (especially in elderly patients and in patients with Parkinson's disease), anxiety, motor restlessness, mania, hypomania, aggressiveness, memory impairment , depersonalization, increased depression, decreased ability to concentrate, insomnia, nightmares, yawning, activation of psychosis symptoms, headache, myoclonus, dysarthria, tremor (especially of the hands, head, tongue), peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus, ataxia, extrapyramidal syndrome, increased frequency and intensification of epileptic seizures, changes in the EEG.

From the side of the cardiovascular system: orthostatic hypotension, tachycardia, conduction disturbances, dizziness, nonspecific ECG changes (ST interval or T wave), arrhythmia, blood pressure lability, disturbance of intraventricular conduction (expansion of the QRS complex, changes in the PQ interval, bundle branch blockade ).

From the digestive system: nausea, heartburn, vomiting, gastralgia, increased or decreased appetite (increased or decreased body weight), stomatitis, taste changes, diarrhea, darkening of the tongue; rarely - liver dysfunction, cholestatic jaundice, hepatitis.

From the endocrine system: testicular edema, gynecomastia, breast enlargement, galactorrhea, changes in libido, decreased potency, hypo- or hyperglycemia, hyponatremia (decreased vasopressin production), syndrome of inadequate secretion of ADH.

From the hematopoietic system: agranulocytosis, leukopenia, thrombocytopenia, purpura, eosinophilia.

Allergic reactions: skin rash, pruritus, urticaria, photosensitivity, swelling of the face and tongue.

Effects due to anticholinergic activity: dry mouth, tachycardia, accommodation disturbances, blurred vision, mydriasis, increased intraocular pressure (only in people with a narrow angle of the anterior chamber of the eye), constipation, paralytic obstruction, urinary retention, decreased sweating, confusion, delirium or hallucinations.

Others: hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, pollakiuria, hypoproteinemia.