Amitriptyline

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Available since: 2019-09-19

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Clinical Pharmacology

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

The mechanism of the antidepressant effect is associated with an increase in the concentration of norepinephrine in the synapses and / or serotonin in the CNS due to the inhibition of the reverse neuronal uptake of these mediators. With prolonged use 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 states. In anxiety and 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 concentrations of monoamines in the central nervous system, especially serotonin, and the effect on endogenous opioid systems.

It has a pronounced peripheral and central anticholinergic effect due to its high affinity for m-cholinergic receptors; strong sedative effect associated with affinity for histamine H1 receptors, and alpha-adreno-blocking action.

It has an anti-ulcer effect, the mechanism of which is due to its ability to block histamine H2 receptors in the parietal cells of the stomach, as well as to have a sedative and m-holinoblokiruyuschee effect (with gastric ulcer and duodenal ulcer reduces pain, accelerates ulcer healing).

The efficacy of nocturnal urinary incontinence appears to be due to anticholinergic activity leading to an increase in bladder's ability to stretch, direct β-adrenergic stimulation, activity of α-adrenoreceptor 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 depression). A clear efficacy of amitriptyline in patients with bulimia in patients with and without depression is shown, while a decrease in bulimia can be observed without a concomitant weakening of the depression itself.

When conducting general anesthesia, lowers blood pressure and body temperature. Does not inhibit MAO.

Antidepressant effect develops within 2-3 weeks after the start of the application.

Pharmacokinetics. The bioavailability of amitriptyline with various routes of administration is 30-60%, its active metabolite nortriptyline is 46-70%. The time to reach the maximum concentration (Tmax) after ingestion 2.0-, 7.7 hours. The volume of distribution is 5-10 l / kg.

Effective therapeutic blood concentrations of amitriptyline - 50-250 ng / ml, for nortriptyline (its active metabolite) 50-150 ng / ml. The maximum plasma concentration (Сmax) is 0.04-0.16 mcg / ml.

Passes through histohematogenous barriers, including the blood-brain barrier (including nortriptyline). The concentrations of amitriptyline in tissues are higher than in plasma. Communication with plasma proteins 92-96%. It is metabolized in the liver (by demethylation, hydroxylation) with the formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites.

The plasma half-life is from 10 to 28 hours for amitriptyline and from 16 to 80 hours for nortriptyline. Excreted by the kidneys - 80%, partly with bile. Complete clearance within 7-14 days. Amitriptyline crosses the placental barrier, is secreted into breast milk in concentrations similar to plasma.

Indications

Depression (especially with anxiety, agitation, and sleep disorders, including children, endogenous, involutional, reactive, neurotic, drug, with organic brain lesions, alcohol withdrawal), schizophrenic psychosis, mixed emotional disorders, behavioral disorders (activity and attention), nocturnal enuresis (with the exception of patients with bladder hypotension), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical pains in the region and persons, postherpetic neuralgia, post-traumatic neuropathy, diabetic or other peripheral neuropathy), headache, migraine (prophylaxis), gastric ulcer and duodenal ulcer.

Composition

Active ingredient: 10 mg or 25 mg amitriptyline.

Excipients: lactose monohydrate, povidone, silicon dioxide, magnesium stearate, corn starch.

Shell 10 mg: Opadry II Blue 85 F 20753 dye, carnauba wax.

Shell 25 mg: Opadry II Yellow dye 85 F 22450, carnauba wax.

Amitriptyline is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Amitriptyline Grindex	Grindex	Latvia	pills
Amitriptyline	Takeda GmbH	Japan	pills
Amitriptyline			ampoules
Amitriptyline	Ozon	Russia	pills
Amitriptyline	Alsi Pharma	Russia	pills

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Dosage and Administration

Orally, without chewing, immediately after eating (to reduce irritation of the gastric mucosa).

The initial dose for adults is 25-50 mg at night, then the dose is increased over 5-6 days to 150-200 mg / day in 3 divided doses (the maximum part of the dose is taken at night). If there is no improvement within 2 weeks, the daily dose is increased to 300 mg.

With the disappearance of signs of depression, the dose is reduced to 50-100 mg / day and continue therapy for at least 3 months.

In old age, in case of lung disorders, it is prescribed in a dose of 30-100 mg / day (overnight), after reaching a therapeutic effect, they switch to the minimum effective dose - 25-50 mg / day. IM or / in (injected slowly) at a dose of 20-40 mg 4 times a day, gradually replacing by ingestion. The duration of treatment is not more than 6-8 months.

With nocturnal enuresis in children 6-10 years old - 10-20 mg / day for the night, 11-16 years old - 25-50 mg / day.

Children as an antidepressant: from 6 to 12 years old - 10-30 mg or 1-5 mg / kg / day fractionally, in adolescence - 10 mg 3 times a day (if necessary up to 100 mg / day).

For the prevention of migraine, with chronic pain of a neurogenic nature (including long headaches) - from 12.5-25 to 100 mg / day (the maximum part of the dose is taken at night).

Adverse reactions

Caused by the blockade of peripheral m-cholinergic receptors: dry mouth, urinary retention, constipation, intestinal obstruction, blurred vision, accommodation paresis, increased intraocular pressure, increased sweating.

Nervous system and sensory organs: headache, dizziness, ataxia, fatigue, weakness, irritability, drowsiness, insomnia, nightmarish dreams, motor agitation, tremor, paresthesia, peripheral neuropathy, EEG changes, impaired concentration, dysarthria, confusion consciousness, hallucinations, tinnitus.

Since the cardiovascular system: tachycardia, orthostatic hypotension, arrhythmia, blood pressure lability, expansion of the QRS complex on the ECG (violation of intraventricular conduction), symptoms of heart failure, fainting, changes in the blood picture, including agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura.

On the part of the gastrointestinal tract organs: nausea, vomiting, heartburn, anorexia, epigastric discomfort, gastralgia, increased activity of hepatic transaminases, stomatitis, taste disturbance, darkening of the tongue.

On the part of metabolism: galactorrhea, change in secretion of ADH; rarely, hypo- or hyperglycemia, impaired glucose tolerance.

On the part of the urogenital system: changes in libido, potency, swelling of the testicles, glycosuria, pollakiuria.

Allergic reactions: skin rash, itching, angioedema, urticaria.

Other: increase in the size of the mammary glands in women and men, hair loss, swollen lymph nodes, photosensitivity, weight gain (with prolonged use), withdrawal syndrome: headache, nausea, vomiting, diarrhea, irritability, sleep disturbance with bright, unusual dreams , increased excitability (after long-term treatment, especially in high doses, with a sharp cessation of the drug).

Contraindications

Hypersensitivity, use in conjunction with MAO inhibitors and 2 weeks before the start of treatment, myocardial infarction (acute and subacute periods), acute alcohol intoxication, acute intoxication with hypnotic, analgesic and psychoactive drugs, angle-closure glaucoma, severe AV and intragastric disorder, severe AV and intragastric pain, intraocular pressure, psychoactive drugs His, AV blockade of Art. II), lactation period, children's age (up to 6 years - oral forms, up to 12 years with a / m and / in the introduction).

With caution. Chronic alcoholism, bronchial asthma, manic depression , hepatic and / or renal failure, thyrotoxicosis, prostatic hyperplasia, urinary retention, bladder hypotension, schizophrenia (activation of psychosis is possible), epilepsy, without armpit (especially I trimester), old age.

Drug interactions

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

With simultaneous use with drugs with anticholinergic activity, it is possible to enhance the anticholinergic effects.

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

With simultaneous use with antipsychotics (neuroleptics), metabolism is mutually inhibited, with a decrease in the convulsive readiness threshold.

With simultaneous use with antihypertensive agents (with the exception of clonidine, guanethidine and their derivatives), it is possible to enhance the antihypertensive effect and the risk of orthostatic hypotension.

With simultaneous use with MAO inhibitors may develop hypertensive crisis; with clonidine, guanethidine - reduction of the hypotensive effect of clonidine or guanethidine is possible; with barbiturates, carbamazepine - possibly reducing the action of amitriptyline due to an increase in its metabolism.

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

With simultaneous use with sucralfate, the absorption of amitriptyline is reduced; with fluvoxamine - increases the concentration of amitriptyline in the blood plasma and the risk of developing toxic effects; with fluoxetine - the concentration of amitriptyline in the blood plasma increases and toxic reactions develop due to the inhibition of the CYP2D6 isoenzyme under the influence of fluoxetine; with quinidine - possibly slowing the metabolism of amitriptyline; with cimetidine - possibly slowing the metabolism of amitriptyline, increasing its concentration in the blood plasma and the development of toxic effects.

With simultaneous use with ethanol, the effect of ethanol is enhanced, especially during the first few days of therapy.

Special instructions

Simultaneous use with MAO inhibitors can be fatal.

A break in treatment between taking MAO inhibitors and amitriptyline (and other tricyclic antidepressants) should be at least 14 days.

Amitriptyline at a dose of more than 150 mg / day reduces the threshold of seizure activity, and therefore increases the risk of seizures in patients with a history of seizures.

At the time of treatment it is prohibited to drive vehicles, maintain machinery and other types of work that require increased attention.

Treatment of elderly patients should be carefully monitored, using minimal doses of the drug, increasing them gradually.

The transition from the depressive phase of manic-depressive psychosis to the manic stage is possible.

If the patient’s condition does not improve within 3–4 weeks, further therapy is not appropriate.

Overdosage

Symptoms: drowsiness, disorientation, confusion, dilated pupils, fever (dyspnea), shortness of breath, dysarthria, agitation, hallucinations, seizures, muscle stiffness, stupor, coma, vomiting, arrhythmia, hypotension, heart failure, respiratory depression.

Treatment: cessation of therapy, gastric lavage, fluid infusion, intramuscular or intravenous injection of physostigmine 1–3 mg every 0.5–2 h (children start physostigmine with a dose of 0.5 mg, then repeat the dose with a 5-minute interval to determine the minimum effective dose, but not more than 2 mg).

Physostigmine should be used only for coma, respiratory depression and other serious disorders; symptomatic therapy, maintaining blood pressure and water-electrolyte balance.

The monitoring of cardiovascular activity (ECG) for 5 days is shown, because relapse may occur after 48 hours and later.