Amitriptyline - instructions for use, reviews, analogs and formulations (tablets and pills 10 mg and 25 mg, injections in ampoules) of a drug for the treatment of depression and psychosis in adults, children and pregnancy. Combination with alcohol
In this article, you can read the instructions for using the drug Amitriptyline. There are reviews of visitors to the site - consumers of this medication, as well as the opinions of doctors of specialists on the use of Amitriptyline in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Amitriptyline in the presence of existing structural analogues.Use to treat depression, psychosis and schizophrenia in adults, children, as well as in pregnancy and lactation. Combination of the drug with alcohol.
Amitriptyline antidepressant (tricyclic antidepressant). It also has some analgesic (central genesis), antiserotonin action, helps to eliminate night incontinence and reduces appetite.
Has a strong peripheral and central anticholinergic action due to high affinity for m-holinoretseptoram; a strong sedative effect associated with affinity for H1-histamine receptors, and an alpha-adrenergic blocking action.
Has the properties of antiarrhythmic drug class IA, like quinidine in therapeutic doses, slows down the ventricular conduction (in case of an overdose it can cause severe intraventricular blockade).
The mechanism of antidepressant action is associated with an increase in the concentration of noradrenaline and / or serotonin in the central nervous system (CNS) (a decrease in their reverse absorption).
Accumulation of these neurotransmitters occurs as a result of inhibition of their inverse capture by the membranes of presynaptic neurons.With prolonged use reduces the functional activity of beta-adrenergic and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, disturbed in depressive states. With anxiety-depressive states reduces anxiety, agitation and depressive manifestations.
The mechanism of antiulcer action is due to the ability to exert sedative and m-anticholinergic action. Efficacy at night urinary incontinence is apparently due to anticholinergic activity leading to increased bladder capacity for stretching, direct beta adrenergic stimulation, alpha-adrenergic agonist activity accompanied by increased sphincter tone, and central blockade of serotonin uptake. Has a central analgesic effect, which is believed to be associated with changes in the concentration of monoamines in the central nervous system, especially serotonin, and influence on endogenous opioid systems.
The mechanism of action for bulimia nervosa is unclear (it may be similar to that in depression).It shows a distinct effect of the drug with bulimia in patients with both depression and its presence, while a decrease in bulimia can be noted without the concomitant weakening of depression itself.
When general anesthesia reduces blood pressure and body temperature. Does not inhibit monoamine oxidase (MAO).
Antidepressant effect develops within 2-3 weeks after the beginning of application.
Pharmacokinetics
Absorption is high. Passes (including nortriptyline - amitriptyline metabolite) through the histohematetic barriers, including the blood-brain barrier, placental barrier, penetrates into breast milk. It is excreted by the kidneys (mainly in the form of metabolites) - 80% in 2 weeks, in part with bile.
Indications
- depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, drug, with organic brain lesions);
- as part of complex therapy used in mixed emotional disorders, psychoses in schizophrenia, alcohol withdrawal, behavioral disorders (activity and attention), nocturnal enuresis (except for patients with bladder hypotension), bulimia nervosa,chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical pain in the face, postherpetic neuralgia, posttraumatic neuropathy, diabetic or other peripheral neuropathy), headache, migraine (prophylaxis), gastric ulcer and 12-finger guts.
Forms of release
Tablets 10 mg and 25 mg.
Dragee 25 mg.
Solution for intravenous and intramuscular injection (injections in ampoules for injection).
Instructions for use and dosage
Assign inside, not liquid, immediately after meals (to reduce irritation of the gastric mucosa).
Adults
Adults with depression, the initial dose - 25-50 mg per night, then gradually the dose can be increased taking into account the effectiveness and tolerability of the drug to a maximum of 300 mg per day in 3 divided doses (most of the dose is taken at night). When the therapeutic effect is achieved, the dose can be gradually reduced to the minimum effective depending on the patient's condition. The duration of the course of treatment is determined by the patient's condition, effectiveness and tolerability of the therapy and can range from several months to 1 year, and, if necessary, more.In old age, when light violations, as well as nervous bulimia, in combined therapy with mixed emotional disorders and behavioral disorders, psychoses, schizophrenia and alcohol withdrawal administered in a dose of 25-100 mg daily (at night), after moving the therapeutic effect at minimal effective doses - 10-50 mg per day.
For the prevention of migraine, chronic pain syndrome, neurogenic character (including long headaches), as well as in the treatment of gastric ulcer and duodenum 12 - from 10-12.5-25 to 100 mg per day (maximum dose portion taken at night).
Children
Babies as an antidepressant: 6 to 12 years - 10-30 mg per day, or 1-5 mg / kg per day fractional, a teenager - to 100 mg per day.
When nocturnal enuresis in children 6-10 years - 10-20 mg per day at night, 11-16 years - up to 50 mg per day.
Side effect
- blurred vision;
- mydriasis;
- increased intraocular pressure (only in individuals with a local anatomical predisposition - a narrow angle of the anterior chamber);
- drowsiness;
- fainting;
- fatigue;
- irritability;
- anxiety;
- disorientation;
- hallucinations (especially in elderly patients and patients with Parkinson's disease);
- anxiety;
- mania;
- memory impairment;
- decreased ability to concentrate;
- insomnia;
- "nightmarish" dreams;
- asthenia;
- headache;
- ataxia;
- increase and intensification of epileptic seizures;
- changes on the electroencephalogram (EEG);
- tachycardia;
- a feeling of palpitations;
- dizziness;
- orthostatic hypotension;
- arrhythmia;
- lability of blood pressure (decrease or increase in blood pressure);
- dry mouth;
- constipation;
- nausea, vomiting;
- heartburn;
- gastralgia;
- increased appetite and body weight or decreased appetite and body weight;
- stomatitis;
- change in taste;
- diarrhea;
- darkening of the tongue;
- an increase in the size (swelling) of the testicles;
- gynecomastia;
- increase in the size of the mammary glands;
- galactorrhea;
- decreased or increased libido;
- decreased potency;
- skin rash;
- itching;
- photosensitization;
- angioedema;
- hives;
- hair loss;
- noise in ears;
- edema;
- hyperpyrexia;
- enlarged lymph nodes;
- retention of urine.
Contraindications
- hypersensitivity;
- application 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 hypnotics, analgesics and psychoactive drugs;
- angle-closure glaucoma;
- severe disturbances of AV and intraventricular conduction (blockade of the bundle of the bundle, AV blockade of 2 items);
- lactation period;
- children's age till 6 years;
- intolerance to galactose;
- deficiency of lactase;
- glucose-galactose malabsorption.
Application in pregnancy and lactation
In pregnant women, the drug should be used only if the intended benefit to the mother exceeds the potential risk to the fetus.
Penetrates into breast milk and can cause drowsiness in infants. To avoid the development of the "cancellation" syndrome in newborns (manifested by shortness of breath, drowsiness, intestinal colic, increased nervous excitability, increase or decrease in blood pressure, tremor, or spastic phenomena), amitriptyline is gradually withdrawn at least 7 weeks before the expected delivery.
Use in children
Contraindicated in children under 6 years.
In children, adolescents and young people (under 24 years) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, with the appointment of amitriptyline or any other.antidepressants in this category of patients, it is necessary to correlate the risk of suicide and the benefit from their use
special instructions
Before the start of treatment, it is necessary to control blood pressure (in patients with low or labile blood pressure it can decrease even more); in the period of treatment - control of peripheral blood (in some cases, agranulocytosis may develop, and therefore it is recommended to monitor the blood picture, especially with an increase in body temperature, the development of influenza-like symptoms and sore throats), with prolonged therapy - control of the functions of the CCC and liver. In the elderly and patients with SSS diseases, control of heart rate, blood pressure, and ECG is shown. On the ECG, there may be clinically insignificant changes (T wave smoothing, S-T segment depression, QRS complex expansion).
Care must be taken when jumping to a vertical position from the "lying" or "sitting" position.
During the treatment should be excluded from the use of ethanol.
Assign no earlier than 14 days after the abolition of MAO inhibitors, starting with small doses.
With a sudden discontinuation after long-term treatment, the syndrome of "withdrawal" may develop.
Amitriptyline in doses above 150 mg per day reduces the threshold of convulsive activity (it should take into account the risk of epileptic attacks in predisposed patients, as well as in the presence of other predisposing factors to the emergence of convulsive syndrome, for example, brain damage of any etiology, simultaneous use of antipsychotic drugs (neuroleptics ), during the period of rejection of ethanol or withdrawal of drugs with anticonvulsant properties, for example, benzodiazepines). Depression is characterized by the risk of suicidal actions, which can persist until a significant remission is achieved. In this regard, at the beginning of treatment, a combination with drugs from the benzodiazepine group or neuroleptic drugs and continuous medical monitoring (entrusting trusted persons with storage and dispensing of medicines) may be indicated. In children, adolescents and young people (under 24 years) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, with the appointment of amitriptyline or any other.antidepressants in this category of patients should be related to the risk of suicide and the benefits of their use. In short-term studies in people over 24 years of age, the risk of suicide did not increase, but in people older than 65 years, it declined slightly. During treatment with antidepressants, all patients should be monitored for early detection of suicidal tendencies.
In patients with cyclical affective disorders in the period of the depressive phase, manic or hypomanic conditions may develop on the background of therapy (dose reduction or drug withdrawal and antipsychotic drug administration are necessary). After the relief of these conditions, if there are indications, treatment at low doses can be resumed.
Due to possible cardiotoxic effects, care must be taken when treating patients with thyrotoxicosis or patients receiving thyroid hormone preparations.
In combination with electroconvulsive therapy is prescribed only under the condition of careful medical supervision.
At predisposed patients and patients of advanced age can provoke development of medicinal psychoses,mainly at night (after the drug is withdrawn for several days).
May cause paralytic intestinal obstruction, mainly in patients with chronic constipation, the elderly or in patients who are obliged to comply with bed rest.
Before conducting general or local anesthesia, an anesthesiologist should be warned that the patient is taking amitriptyline.
Due to the anticholinergic effect, tearing can be reduced and the relative amount of mucus in the tear fluid can be increased, which can damage the epithelium of the cornea in patients using contact lenses.
With prolonged use, there is an increase in the frequency of tooth decay. The need for riboflavin may be increased.
The study of reproduction on animals has revealed an unfavorable effect on the fetus, and adequate and strictly controlled studies in pregnant women have not been conducted. In pregnant women, the drug should be used only if the intended benefit to the mother exceeds the potential risk to the fetus.
Penetrates into breast milk and can cause drowsiness in infants. To avoid the development of the "cancellation" syndrome in newborns (manifested by shortness of breath, drowsiness, intestinal colic, increased nervous excitability, increase or decrease in blood pressure, tremor, or spastic phenomena), amitriptyline is gradually withdrawn at least 7 weeks before the expected delivery.
Children are more sensitive to acute overdose, which should be considered dangerous and potentially fatal for them.
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Drug Interactions
With the joint use of ethanol (alcohol) and drugs, depressing the central nervous system (including other antidepressants, barbiturates, benzadiazepines and general anesthetics), a significant increase in the inhibitory effect on the central nervous system, respiratory depression and hypotensive effect. Increases the sensitivity to beverages containing ethanol (alcohol).
Increases anticholinergic drugs with anticholinergic activity (e.g., phenothiazine derivatives, antiparkinsonian drugs, amantadine, atropine, biperiden, antihistaminic drugs), which increases the risk of side effects (CNS, vision, and bladder intestine). When combined with the use holinoblokatorami, derivatives of phenothiazine and benzodiazepine - mutual enhancement of sedation and central anticholinergic effects and increase the risk of seizures (seizure threshold reduction); derivatives of phenothiazine, in addition, may increase the risk of neuroleptic malignant syndrome.
When combined with anticonvulsant drugs, it is possible to increase the inhibitory effect on the central nervous system, reduce the threshold of convulsive activity (when used in high doses), and reduce the effectiveness of the latter.
When combined with antihistamine drugs, clonidine - increased oppressive effect on the central nervous system; with atropine - increases the risk of paralytic intestinal obstruction; with medicines,causing extrapyramidal reactions - an increase in the severity and frequency of extrapyramidal effects.
With the simultaneous use of amitriptyline and indirect anticoagulants (coumarin derivatives or indadion), an increase in anticoagulant activity of the latter is possible. Amitriptyline may increase depression caused by glucocorticosteroids (GCS). Drugs for the treatment of thyrotoxicosis increase the risk of agranulocytosis. Reduces the effectiveness of phenytoin and alpha-blockers.
Inhibitors of microsomal oxidation (cimetidine) prolong T1 / 2, increase the risk of developing toxic effects of amitriptyline (a 20-30% dose reduction may be required), inducers of microsomal liver enzymes (barbiturates, carbamazepine, phenytoin, nicotine and oral contraceptives) reduce plasma concentration and reduce the effectiveness of amitriptyline.
Joint use with Disulfiram and other inhibitors of acetaldehyde genase provokes delirium.
Fluoxetine and fluvoxamine increase the concentration of amitriptyline in plasma (a decrease in the dose of amitriptyline by 50% may be required).
Estrogen-containing oral contraceptive medications and estrogens can increase the bioavailability of amitriptyline.
With the simultaneous use of amitriptyline with clonidine, guanethidine, betanidine, reserpine and methyldopa - reducing the hypotensive effect of the latter; with cocaine - the risk of arrhythmia of the heart.
Antiarrhythmic drugs (such as quinidine) increase the risk of developing rhythm disturbances (possibly slowing the metabolism of amitriptyline).
Pimozide and probucol may increase cardiac arrhythmias, which is manifested in the prolongation of the Q-T interval on the ECG.
Strengthens the effect on the CCC of epinephrine, norepinephrine, isoprenaline, Ephedrine and phenylephrine (including when these drugs are part of local anesthetics) and increases the risk of heart rhythm disturbances, tachycardia, severe arterial hypertension.
When co-administered with alpha-adrenomimetics for intranasal administration or for use in ophthalmology (with significant systemic absorption), the vasoconstrictor effect of the latter may be enhanced.
With a joint admission with thyroid hormones - a mutual enhancement of the therapeutic effect and toxic effects (include cardiac arrhythmias and a stimulating effect on the central nervous system).
M-holinoblokatory and antipsychotic drugs (neuroleptics) increase the risk of hyperpyrexia (especially in hot weather).
When co-administered with other hematotoxic drugs, it is possible to increase hematotoxicity.
Incompatible with MAO inhibitors (there may be an increase in the frequency of periods of hyperpyrexia, severe seizures, hypertensive crises and death of the patient).
Analogs of the drug Amitriptyline
Structural analogs for the active substance:
- Amizole;
- Amirol;
- Amitriptyline Lechiva;
- Amitriptyline Nycomed;
- Amitriptyline-AKOS;
- Amitriptyline-Grindeks;
- Amitriptyline-LENS;
- Amitriptyline-Ferein;
- Amitriptyline hydrochloride;
- Apo-Amitriptyline;
- Vero-Amitriptyline;
- Saroten retard;
- Triptysole;
- Elivel.
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