Amitriptyline-nycomed coated pills 25mg N50
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Active ingredients
Amitriptyline
Release form
Pills
Composition
Amitriptyline hydrochloride (in terms of amitriptyline) 25 mg
Pharmacological effect
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 in 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 is apparently 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). The clear efficacy of amitriptyline in patients with bulimia in patients with and without depression is shown, and 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
Bioavailability of amitriptyline is 30-60%. Plasma protein binding 82-96%. Vd - 5-10 l / kg. Metabolized to form the active metabolite of nortriptyline. T1 / 2 - 31-46 hours. Excreted mainly by the kidneys.
Indications
Depression of any etiology. Especially effective in anxiety-depressive states, due to the severity of the sedative effect. It does not cause exacerbation of productive symptoms (delusions, hallucinations), unlike antidepressants with a stimulating effect. Neurogenic pain of a chronic nature. Mixed emotional and behavioral disorders, phobic disorders. Pediatric enuresis (with the exception of children with hypotonic bladder). Psychogenic anorexia, bulimic neurosis.
Contraindications
Heart failure in the stage of decompensation. Acute and recovery period of myocardial infarction. Disorders of cardiac muscle conduction. Severe arterial hypertension. Acute diseases of the liver and kidneys, with severe impairment of function. Blood diseases. Ulcer of the stomach and duodenum in the acute stage. Hypertrophy prostate gland. Bladder athenia. Pyloric stenosis, paralytic ileus of the intestine. Simultaneous treatment with MAO inhibitors (see Interaction). Pregnancy, thoracic vsk period rmlivaniya.Deti to 6 years (for oral administration), children up to 12 years (v / m and / in the introduction). Hypersensitivity to amitriptyline. Amitriptyline should be used with caution in patients suffering from alcoholism, people with asthma, manic-depressive psychosis (MDP) and epilepsy (see. Special instructions), the oppression of bone marrow hematopoiesis, hyperthyroidism, angina and heart failure, angle-closure glaucoma, ocular hypertension, schizophrenia (although when it is taken, there is usually no exacerbation of productive symptoms).
Precautionary measures
CNS and peripheral nervous system: drowsiness, asthenia, fainting, anxiety, disorientation, agitation, hallucinations (especially in elderly patients and in patients with Parkinson’s disease),anxiety, motor anxiety, manic state, hypomania, aggression, memory impairment, depersonalization, increased depression, decreased ability to concentrate, insomnia, nightmares, yawning, activation of symptoms of psychosis, headache, myoclonus, dysarthria, tremor (especially hands, head, tongue), peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus, ataxia, extrapyramidal syndrome, increased and increased epileptic seizures, changes in EEG. Since the cardiovascular system: orthostatic hypotension, tachycardia, conduction disturbances, dizziness, nonspecific changes on the ECG (ST interval or T wave), arrhythmia, blood pressure lability, violation of intraventricular conduction (expansion of the QRS complex, changes in the PQ interval, blockade of the bundle of the bundle of his ). On the part of the digestive system: nausea, heartburn, vomiting, gastralgia, increased or decreased appetite (increased or reduced body weight), stomatitis, change in taste, diarrhea, darkening of the tongue; rarely - liver dysfunction, cholestatic jaundice, hepatitis. On the part of the endocrine system: swelling of the testicles, gynecomastia, breast enlargement, galactorrhea, changes in libido, decreased potency, hypo- or hyperglycemia, hyponatremia (decreased production of vasopressin), inadequate secretion of ADH syndrome. On the part of the hematopoietic system: agranulocytosis, leukopenia, thrombocytopenia, purpura, eosinophilia.
Use during pregnancy and lactation
Amitriptyline should not be used during pregnancy, especially in the I and III trimesters, except in cases of extreme necessity. Adequate and strictly controlled clinical studies of the safety of the use of amitriptyline during pregnancy have not been conducted. Reception of amitriptyline should be gradually canceled, at least, 7 weeks prior to the expected childbirth in order to avoid development of a syndrome of cancellation at the newborn. In experimental studies, amitriptyline had a teratogenic effect. Contraindicated during lactation. It is excreted in breast milk and may cause drowsiness in infants.
Dosage and administration
Assign inside (during or after a meal). The initial daily dose for oral administration is 50-75 mg (25 mg in 2-3 doses), then the dose is gradually increased by 25-50 mg, to obtain the desired antidepressant effect. The optimal daily therapeutic dose is 150-200 mg (the maximum part of the dose is taken at night).In severe depressions resistant to therapy, the dose is increased to 300 mg or more, up to the maximum tolerated dose (the maximum dose for outpatients 150 mg / day). In these cases, treatment is advisable to start with intramuscular or intravenous administration of the drug, while applying a higher initial dose, accelerating the buildup of dosages under the control of the somatic condition. After obtaining a persistent anti-depressive effect after 2-4 weeks, the dose is gradually and slowly reduced to 50-100 mg / day and therapy is continued for at least 3 months. In the case of signs of depression with a decrease in dose, you must return to the previous dose. If the patient's condition does not improve within 3-4 weeks of treatment, then further therapy is inappropriate.
Side effects
Mainly associated with anticholinergic drug action paresis of accommodation. Blurred vision, increased intraocular pressure, dry mouth, constipation, intestinal obstruction, delayed urination, fever. All these phenomena usually disappear after adaptation to the drug or reduction of doses. For the CNS, headache, ataxia, fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, impaired concentration, nightmares, dysarthria, confusion, hallucinations, motor agitation, disorientation, tremor, paresthesias, peripheral neuropathy, changes in EEG. Rare extrapyramidal disorders, convulsions, anxiety. For the cardiovascular system, tachycardia, arrhythmia, conduction disturbance, labial pressure, expansion of the QRS complex on an ECG (violation of intraventricular conduction), heart failure symptoms, fainting. , stomatitis, taste disorders, darkening of the tongue, epigastric discomfort, gastralgia, increased activity of hepatic transaminases, rarely cholestatic jaundice, diarrhea. With endocrine th system increase the size of the mammary glands in men and women, galactorrhea, changes in the secretion of antidiuretic hormone (ADH), changes in libido, potency. Rare hypo-hyperglycemia, glycosuria, impaired glucose tolerance, testicular edema.Allergic reactions: skin rash, pruritus, photosensitization, angioedema, urticaria. Other agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura and other blood changes, hair loss, lymphadenopathy, weight gain during prolonged use, sweating, lesions With prolonged treatment, especially in high doses, with a sharp cessation of treatment, the development of withdrawal syndrome headache, nausea, vomiting, diarrhea, as well as irritability, sleep disturbance with vivid, unusual dreams, anxiety.
Overdose
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, hypotensive action, and respiratory depression is possible. With simultaneous use with drugs that have 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, it is possible to slow down the metabolism of amitriptyline, increase its concentration in the blood plasma and develop toxic effects.When applied simultaneously with ethanol, the effect of ethanol is enhanced, especially during the first few days of therapy.
Interaction with other drugs
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, hypotensive effect, respiratory depression is possible. With simultaneous use of drugs with anticholinergic activity, increased anticholinergic effects are possible. cardiovascular system and an increased risk of developing cardiac arrhythmias, tachycardia, severe hypertension In the case of simultaneous use with antipsychotics (neuroleptics), metabolism is mutually inhibited, while the threshold of convulsive readiness is reduced. simultaneous use with MAO inhibitors may develop a 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 the development of serotonin syndrome is described with simultaneous use with sertraline. With simultaneous use with sucralfate, absorption of amitriptyline decreases; 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, it is possible to slow down the metabolism of amitriptyline, increase its concentration in the 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.
special instructions
It is used with caution in CHD, arrhythmias, heart block, heart failure, myocardial infarction, arterial hypertension, stroke, chronic alcoholism, thyrotoxicosis, against the background of therapy with thyroid drugs. During therapy with amitriptyline, caution is required when abruptly moving to a vertical position from a prone or sitting position. With a sharp cessation of admission may develop withdrawal syndrome. Amitriptyline in doses of more than 150 mg / day reduces the threshold of convulsive readiness; The risk of developing epileptic seizures in susceptible patients, as well as other factors that increase the risk of developing convulsive syndrome (including brain damage of any etiology, simultaneous use of antipsychotic drugs, during the period of refusal from ethanol or drug withdrawal, have anticonvulsant activity). It should be borne in mind that suicidal attempts are possible in patients with depression. In combination with electroconvulsive therapy should be used only with careful medical supervision. In predisposed patients and elderly patients, it can provoke the development of medicinal psychoses, mainly at night (after discontinuation of the drug, they disappear within a few days). It can cause paralytic intestinal obstruction, mainly in patients with chronic constipation, the elderly or in patients forced to adhere to bed rest. Prior to general or local anesthesia, the anesthetist should be warned that the patient is taking amitriptyline. With prolonged use, an increase in the frequency of caries is observed. Possible increase in riboflavin. Amitriptyline can be used no earlier than 14 days after discontinuation of MAO inhibitors. It should not be used simultaneously with adrenergic and sympathomimetic, incl. with epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine, phenylpropanolamine. With caution used simultaneously with other drugs that have anticholinergic effects. While taking amitriptyline avoid alcohol. Impact on the ability to drive vehicles and control mechanisms: During the period of treatment should refrain from potentially hazardous activities that require increased attention and quick psychomotor reactions.