Product Name: Amitriptyline
Common Brand Names: Elavil; Endep; Tryptanol
Pharmaceutical Category: Antidepressants / Anti Anxiety
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There is an additional general information about this medication active ingredient amitriptyline:
Amitriptyline is an antidepressant tricyclic group of compounds derived dibenzocycloheptadiene.
The mechanism of antidepressant action is associated with an increased concentration of norepinephrine in the synapses and / or serotonin in the central nervous system depression due to reverse neuronal capture of these mediators. When anxiety and depressive states this medication reduces anxiety, agitation and depressive symptoms.
Also this drug has some analgesic effect, which is believed to be associated with changes in the concentrations of monoamines in the central nervous system, especially serotonin, and the influence on the endogenous opioid system.
It has distinct peripheral and central anticholinergic action, due to a high affinity for m-cholinergic receptors, a strong sedative effect connected with affinity for histamine H1-receptors and alpha-adrenoceptor blocking action.
Has antiulcer effect mechanism is due to the ability to block histamine H2-receptors in parietal cells of the stomach and provide a sedative and m-anticholinergic action (if gastric ulcer and duodenal ulcer reduces the pain and accelerate healing of ulcers).
Its efficiency in the bed-wetting is caused, apparently, anticholinergic activity, which leads to an increase in the ability of the bladder to stretch, direct beta-adrenergic stimulation, the activity of alpha-adrenergic agonists, accompanied by increased tone of the sphincter and the central blockade of serotonin reuptake.
The mechanism of therapeutic action for bulimia nervosa is not installed (possibly similar to that for depression). It shown a clear efficacy of amitriptyline in bulimia patients without depression, as well as in its presence, and the reduction of bulimia can be observed without a concomitant weakening of the most depressed.
With general anesthesia reduces blood pressure and body temperature. Amitriptyline does not inhibit MAO.
The antidepressant effect develops within 2-3 weeks after application.
The bioavailability of Amitriptyline is 30-60%. The plasma protein binding is 82-96%. Vd is 5-10 L / kg. This medicine is metabolized to the active metabolite nortriptyline. T1/2 is 31-46 hours. Amitriptyline excreted primarily by the kidneys.
Why is Amitriptyline prescribed?
Depression (especially with anxiety, agitation and sleep disorders, including childhood, endogenous, involutional, reactive, neurotic, drug, and organic brain damage, alcohol withdrawal), schizophrenic psychoses, mixed emotional disorders, behavioral disorders (activity and attention), nocturnal enuresis (except in patients with hypotonia of the bladder), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic pain, atypical facial pain, postherpetic neuralgia, posttraumatic neuropathy, diabetic neuropathy, peripheral neuropathy), prophylaxis of migraine, peptic ulcer and duodenal ulcer.
Dosage and administration
For oral administration the initial dose is 25-50 mg at night. Then, within 5-6 days the dose was increased to an individual 150-200 mg / day (most of the dose taken at night). If, during the second week of the improvement has not come, the daily dose increased to 300 mg. With the disappearance of symptoms of depression to reduce the dose of 50-100 mg / day and continue therapy for at least 3 months. In elderly patients with lung disorders the dose is 30-100 mg / day is usually 1 time / at night, after achieving the therapeutic effect switching to the minimum effective dose - 25-50 mg / day.
When nocturnal enuresis in children aged 6-10 years - 10-20 mg / overnight; at the age of 11-16 years - 25-50 mg / day.
For IM injections the initial dose is 50-100 mg / injection in 2-4 injections. If necessary, the dose can be gradually increased to 300 mg / day, in exceptional cases up to 400 mg / day.
Amitriptyline side effects, adverse reactions
CNS and peripheral nervous system: drowsiness, fatigue, fainting, anxiety, confusion, agitation, hallucinations (especially in elderly patients and patients with Parkinson's disease), anxiety, restlessness, mania, hypomania state, aggression, memory impairment, depersonalization, increased depression, decreased ability to concentrate, insomnia, nightmares, yawning, activation of psychosis symptoms, headache, myoclonus, dysarthria, tremor (especially of hands, head and tongue), peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus, ataxia, extrapyramidal syndrome, acceleration and intensification of epileptic seizures, EEG changes.
Cardiovascular system: orthostatic hypotension, tachycardia, conduction disturbances, dizziness, nonspecific ECG changes (ST interval or spike T), arrhythmias, blood pressure lability, impaired intraventricular conduction (widening complex QRS, change the interval PQ, block bundle-branch block).
Digestive system: nausea, heartburn, vomiting, gastralgia, increase or decrease in appetite (increase or decrease in body weight), disease, change in taste, diarrhea, darkening of the tongue, rarely - liver dysfunction, cholestatic jaundice, hepatitis.
Endocrine: testicular swelling, gynecomastia, breast enlargement, galactorrhea, changes in libido, reduced potency, hypo-or hyperglycemia, hyponatremia (decreased production of vasopressin), a syndrome of inappropriate secretion of ADH.
Hematopoietic system: agranulocytosis, leukopenia, thrombocytopenia, purpura, eosinophilia.
Allergic reactions: skin rash, itching, rash, photosensitivity, swelling of the face and tongue.
Effects due to the anticholinergic activity: dry mouth, tachycardia, accommodation disturbances, blurred vision, mydriasis, increased intraocular pressure (only those with a narrow anterior chamber angle), constipation, paralytic ileus, urinary retention, decreased sweating, confusion, delirium or hallucinations.
Other: Hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, pollakiuria, hypoproteinemia.
The acute period and early recovery period after myocardial infarction, acute alcohol intoxication, acute poisoning with soporific, analgesic and psychotropic drugs, angle-closure glaucoma, severe AV- and intraventricular conduction (bundle branch block feet, AV-block II degree), lactation, children under 6 years of age (for oral administration), children under 12 years (for IV and IM injections), simultaneous treatment with inhibitors and a period of 2 weeks prior to their use, increased sensitivity to Amitriptyline.
Using during pregnancy and breastfeeding
Amitriptyline should not be used during pregnancy, especially in the I and III trimester, except in cases of extreme necessity. Adequate and well controlled clinical studies on the safety of amitriptyline during pregnancy was not conducted.
This drug excreted in breast milk and may cause drowsiness in infants.
Taking of amitriptyline should be phased out, at least 7 weeks prior to delivery to avoid the development of withdrawal syndrome in the newborn.
In experimental studies this medicine exerted teratogenic effects.
Use Amitriptyline with caution in coronary artery disease, arrhythmias, heart block, heart failure, myocardial infarction, hypertension, stroke, chronic alcoholism, thyrotoxicosis, against the background of therapy with thyroid cancer.
The therapy amitriptyline it needed a caution when sharp transition in the vertical position of the "lying" or "sitting".
With a sharp stop taking may develop withdrawal symptoms.
Amitriptyline in doses of 150 mg / day lowers the threshold of convulsive readiness; it possible a risk of epileptic seizures in susceptible patients, as well as the presence of other factors that increase the risk of seizures (including with traumatic brain injury of any etiology, concomitant use of antipsychotic drugs in the period of refusal or withdrawal of alcohol, drugs with anticonvulsant activity).
It should be noted that patients with depression may attempt suicide.
In conjunction with electroconvulsive therapy it should only be used with careful medical supervision.
In predisposed patients and elderly patients may provoke the development of drug psychosis, mainly at night (after the withdrawal of the drug are within a few days).
Amitriptyline can cause paralytic ileus, mainly in patients with chronic constipation who are elderly or in patients who have to comply with bed rest.
Prior to the general or local anesthesia, the anesthesiologist it should be warned that patients taking amitriptyline.
With prolonged use, an increase the frequency of dental caries. May increase the need for riboflavin.
Amitriptyline may be taken no earlier than 14 days after discontinuation of MAO inhibitors.
The drug should not be used in combination with adrenergic and sympathomimetic, including with epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine, phenylpropanolamine.
Use Amitriptyline with caution in conjunction with other drugs, which have anticholinergic action.
While receiving amitriptyline to avoid drinking alcohol.
During the period of treatment you should refrain from potentially hazardous activities requiring increased attention and rapid psychomotor reactions.
Amitriptyline drug interactions
When this drug applied simultaneously with:
- drugs have a depressing effect on the central nervous system, it is possibly a significant increase in inhibitory action on the central nervous system, hypotensive effect, respiratory depression.
- drugs with anticholinergic activity may increase anticholinergic effects.
- it may be enhance the action of sympathomimetic funds for the cardiovascular system and increase the risk of cardiac arrhythmia, tachycardia, severe hypertension.
- antipsychotic drugs (neuroleptics) are relatively suppressed metabolism, with a reduction in the threshold of convulsive readiness.
- antihypertensive drugs (except clonidine, guanethidine and their derivatives) may increase the antihypertensive action and the risk of orthostatic hypotension.
- with MAO inhibitors may been developed a hypertensive crisis; with clonidine, guanethidine it may be decreased the hypotensive effect of clonidine or guanethidine; with barbiturates, carbamazepine it may be decreased the action of amitriptyline by increasing its metabolism.
- with sucralfate decreases absorption of amitriptyline; with fluvoxamine - increases the concentration of amitriptyline in blood plasma and the risk of toxic effects; with fluoxetine - increased concentration of amitriptyline in plasma and develop toxic reactions due to inhibition of isoenzyme CYP2D6 under the influence of fluoxetine; with quinidine - may slow metabolism of amitriptyline; with cimetidine - may slow metabolism of amitriptyline, increasing its concentration in blood plasma and the development of toxic effects.
While taking alcohol the action of ethanol increases, especially during the first few days of therapy.
There was described a case of serotonin syndrome with simultaneously use with sertraline.