Release form, composition and packaging
Pills
from white to white with a slightly yellowish tint, flat-cylindrical in shape, with a chamfer; Light marbling is allowed.
| 1 tab. | |
| amitriptyline hydrochloride | 11.32 mg, |
| which corresponds to the content of amitriptyline | 10 mg |
Excipients: microcrystalline cellulose - 40 mg, lactose monohydrate (milk sugar) - 40 mg, pregelatinized starch - 25.88 mg, colloidal silicon dioxide (Aerosil) - 400 mcg, talc - 1.2 mg, magnesium stearate - 1.2 mg.
10 pieces. — cellular contour packages (1) — cardboard packs. 10 pieces. — contour cell packaging (2) — cardboard packs. 10 pieces. — cellular contour packages (3) — cardboard packs. 10 pieces. — contour cell packaging (4) — cardboard packs. 10 pieces. — contour cell packaging (5) — cardboard packs. 100 pieces. — polymer jars (1) — cardboard packs.
Pills
from white to white with a slightly yellowish tint, flat-cylindrical in shape, with a chamfer and a notch; Light marbling is allowed.
| 1 tab. | |
| amitriptyline hydrochloride | 28.3 mg, |
| which corresponds to the content of amitriptyline | 25 mg |
Excipients: microcrystalline cellulose - 100 mg, lactose monohydrate (milk sugar) - 100 mg, pregelatinized starch - 64.7 mg, colloidal silicon dioxide (aerosil) - 1 mg, talc - 3 mg, magnesium stearate - 3 mg.
10 pieces. — cellular contour packages (1) — cardboard packs. 10 pieces. — contour cell packaging (2) — cardboard packs. 10 pieces. — cellular contour packages (3) — cardboard packs. 10 pieces. — contour cell packaging (4) — cardboard packs. 10 pieces. — contour cell packaging (5) — cardboard packs. 100 pieces. — polymer jars (1) — cardboard packs.
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Compound
Ludiomil is the trade name of the drug. Its active ingredient is the heterocyclic antidepressant mapro tilin . Maprotiline and ludiomil are essentially synonymous words. The dosage of maprotiline in the drug composition corresponds to that indicated on the packaging.
In addition to maprotiline, the composition includes excipients. The tablets contain the following components: lactose, starch, talc, stearate, polysorbate and compounds of inorganic substances. The infusion concentrate contains mannitol, methanesulfonate and water for injection. Excipients are contained in the drug in small quantities, therefore they do not affect the human body.
pharmachologic effect
Antidepressant (tricyclic antidepressant). It also has some analgesic (of central origin), antiserotonin effect, helps eliminate bedwetting and reduces appetite.
It has a strong peripheral and central anticholinergic effect due to its high affinity for m-cholinergic receptors; strong sedative effect associated with affinity for H1-histamine receptors and alpha-adrenergic blocking effect.
It has the properties of a class IA antiarrhythmic drug; like quinidine in therapeutic doses, it slows down ventricular conduction (in overdose it can cause severe intraventricular block).
The mechanism of antidepressant action is associated with an increase in the concentration of norepinephrine and/or serotonin in the central nervous system (CNS) (decreasing their reabsorption).
The accumulation of these neurotransmitters occurs as a result of inhibition of their reuptake by the membranes of presynaptic neurons. With long-term use, it reduces the functional activity of beta-adrenergic and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, and restores the balance of these systems, disturbed during depressive states. In anxiety-depressive conditions, it reduces anxiety, agitation and depressive symptoms.
The mechanism of antiulcer action is due to the ability to have a sedative and m-anticholinergic effect. Effectiveness for bedwetting appears to be due to anticholinergic activity leading to increased bladder distensibility, direct beta-adrenergic stimulation, alpha-adrenergic agonist activity leading to increased sphincter tone, and central blockade of serotonin uptake. It 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 an effect on endogenous opioid systems.
The mechanism of action in bulimia nervosa is unclear (may be similar to that in depression). A clear effect of the drug on bulimia has been shown in patients both without depression and in its presence, while a decrease in bulimia can be observed without a concomitant weakening of depression itself.
During general anesthesia, it reduces blood pressure and body temperature. Does not inhibit monoamine oxidase (MAO).
The antidepressant effect develops within 2-3 weeks after the start of use.
Reviews from patients about the action of "Amitriptyline-Grindeks"
Reviews about the drug are extremely mixed. Some patients are confident that they were able to maintain their performance and adequate perception of reality only thanks to Amitriptyline-Grindeks. Reviews from some patients, on the contrary, are sharply negative: many side effects, severe drowsiness, weakness, irritability and nervousness made life during treatment even worse than it was before taking it.
Unfortunately, many psychiatrist patients do not adhere to the rules of administration: they forget to take the drug on time, they allow the intake of alcoholic beverages during treatment. As a result of this frivolous approach, patients become disappointed in the effect of the drug. Meanwhile, “Amitriptyline-Grindeks” is a psychotropic drug, any deviations from the course of taking it are fraught with changes in the mental state and resistance of the nervous system to irritating factors.
Pharmacokinetics
Absorption is high.
The bioavailability of amitriptyline is 30-60%, its active metabolite nortriptyline is 46-70%. Time to reach Cmax after oral administration is 2.0-7.7 hours. Vd 5-10 l/kg. Effective therapeutic blood concentrations for amitriptyline are 50-250 ng/ml, for nortriptyline 50-150 ng/ml.
Cmax 0.04-0.16 µg/ml. Passes (including nortriptyline) through histohematic barriers, including the blood-brain barrier, placental barrier, and penetrates into breast milk. Communication with plasma proteins - 96%.
Metabolized in the liver with the participation of isoenzymes CYP2C19, CYP2D6, has a “first pass” effect (by demethylation, hydroxylation) with the formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites. T1/2 from blood plasma is 10-26 hours for amitriptyline and 18-44 hours for nortriptyline. Excreted by the kidneys (mainly in the form of metabolites) - 80% in 2 weeks, partially with bile.
Amitriptyline injections, tablets: instructions, price, reviews and side effects
Produced by Russian, Latvian and Japanese manufacturers.
You can buy an antidepressant at the following prices (the average cost in Russian pharmacies is indicated):
- tablets 50 pcs (produced under the name Amitriptyline Nycomed, made in Japan) – 60 rubles;
- tablets 50 pcs (made in Latvia, sold under the name Amitriptyline Grindeks) – 65 rubles;
- tablets 50 pcs (produced by the Moscow Endocrine Plant) - 22 rubles;
- tablets 50 pcs (manufacturer – Russian pharmaceutical company Ozone) – 50 rubles;
- ampoules 10 pcs (Russian production) – 45 rubles.
To purchase Amitriptyline (regardless of the release form and manufacturer), you must provide a prescription in Latin, written by a neurologist.
Indications
Depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, drug-induced, with organic brain damage).
As part of complex therapy, it is used for 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, post-traumatic neuropathy, diabetic or other peripheral neuropathy), headaches, migraines (prevention), gastric and duodenal ulcers.
Contraindications
Hypersensitivity, use in conjunction with MAO inhibitors and 2 weeks before treatment, myocardial infarction (acute and subacute periods), acute alcohol intoxication, acute intoxication with hypnotics, analgesics and psychoactive drugs, angle-closure glaucoma, severe AV and intraventricular conduction disorders (branch block His bundle, AV block II stage), lactation period, children under 6 years of age.
Due to the content of lactose monohydrate (milk sugar) in the tablets, the drug should not be taken by patients with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Carefully.
Amitriptyline should be used with caution in persons with alcoholism, bronchial asthma, schizophrenia (possible activation of psychosis), bipolar disorder, epilepsy, suppression of bone marrow hematopoiesis, diseases of the cardiovascular system (CVS) (angina pectoris, arrhythmia, heart block, chronic heart failure, myocardial infarction, arterial hypertension), intraocular hypertension, stroke, decreased motor function of the gastrointestinal tract (GIT) (risk of paralytic ileus), liver and/or renal failure, thyrotoxicosis, prostatic hyperplasia, urinary retention, hypotension bladder, during pregnancy (especially the first trimester), in old age.
Instructions for use
It is recommended that the therapeutic dosage be selected for each patient in a hospital setting. In this case, 50 mg of the active substance is initially prescribed three times a day. Gradually the concentration is increased. The average therapeutic dose is 100 mg three times a day. For elderly patients, the starting dose is 30 mg per day, which is gradually increased to 150 mg.
In outpatient settings, the concentrations of prescribed drugs are slightly lower. For patients treated at home, it is recommended to start with 25 mg of a single dose three times a day, gradually reaching the average therapeutic dosage.
The drug is administered by injection in severe cases when it is necessary to achieve a quick therapeutic effect. It is acceptable to administer from 1 to 6 ampoules of the drug.
All drugs containing maprotiline are dispensed without a doctor's prescription and are available for free sale in pharmacies.
Dosage
Administered orally, without chewing, immediately after meals (to reduce irritation of the gastric mucosa).
Adults
For adults with depression, the initial dose is 25-50 mg at night, then gradually the dose can be increased taking into account the effectiveness and tolerability of the drug to a maximum of 300 mg/day. in 3 doses (the largest part of the dose is taken at night). When a 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, the effectiveness and tolerability of the therapy and can range from several months to 1 year, and if necessary, more. In old age with mild disorders, as well as with bulimia nervosa, as part of complex therapy for mixed emotional disorders and behavioral disorders, psychosis with schizophrenia and alcohol withdrawal, a dose of 25-100 mg/day is prescribed. (at night), after achieving a therapeutic effect, switch to the minimum effective dose - 10-50 mg/day.
For the prevention of migraine, for chronic pain syndrome of a neurogenic nature (including prolonged headaches), as well as in the complex therapy of gastric and duodenal ulcers - from 10-12.5-25 to 100 mg/day. (the maximum dose is taken at night).
Children
For children as an antidepressant: from 6 to 12 years old - 10-30 mg/day. or 1-5 mg/kg/day. fractionally, in adolescence - up to 100 mg/day.
For nocturnal enuresis in children 6-10 years old - 10-20 mg/day. at night, 11-16 years - up to 50 mg/day.
Analogs
Structural analogues of Amitriptyline are:
- Amizol,
- Amirol,
- Saroten,
- Tryptisol,
- Elivel.
In addition, there are other antidepressant drugs. The group of tricyclic antidepressants also includes imipramine and clomipramine. However, of course, selecting the necessary remedy for depression is the prerogative of a psychotherapist, neurologist or neurologist, and self-medication here is inappropriate and even dangerous.
Taken orally immediately after meals (irritates the gastric mucosa), with a small amount of water
If it is impossible to prescribe Amitriptyline to the patient, the doctor may prescribe one of the following analogues:
- Saroten;
- Anafranil;
- Doxepin;
- Novo-Triptin;
- Melipramine.
It should be understood that each of the above drugs has its own side effects and contraindications that should be taken into account when using these drugs.
Side effects
Associated with the anticholinergic effect of the drug:
blurred vision, paralysis of accommodation, mydriasis, increased intraocular pressure (only in persons with a local anatomical predisposition - a narrow anterior chamber angle), tachycardia, dry mouth, confusion (delirium or hallucinations), constipation, paralytic ileus, difficulty urinating.
From the side of the central nervous system:
drowsiness, fainting, fatigue, irritability, anxiety, disorientation, hallucinations (especially in elderly patients and patients with Parkinson's disease), anxiety, psychomotor agitation, mania, hypomania, memory impairment, decreased ability to concentrate, insomnia, "nightmare" » dreams, asthenia; headache; dysarthria, tremor of small muscles, especially the arms, hands, head and tongue, peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus; ataxia, extrapyramidal syndrome, increased frequency and intensification of epileptic seizures; changes in the electroencephalogram (EEG).
From the SSS side:
tachycardia, palpitations, dizziness, orthostatic hypotension, nonspecific changes on the electrocardiogram (ECG) (S-T interval or T wave) in patients without heart disease; arrhythmia, blood pressure lability (decrease or increase in blood pressure), intraventricular conduction disturbances (widening of the QRS complex, changes in the PQ interval, bundle branch block).
From the gastrointestinal tract:
nausea, heartburn, gastralgia, hepatitis (including impaired liver function and cholestatic jaundice), vomiting, increased appetite and body weight or decreased appetite and body weight, stomatitis, changes in taste, diarrhea, darkening of the tongue.
From the endocrine system:
increase in size (swelling) of the testicles, gynecomastia; increase in the size of the mammary glands, galactorrhea; decreased or increased libido, decreased potency, hypo- or hyperglycemia, hyponatremia (decreased vasopressin production), syndrome of inappropriate secretion of antidiuretic hormone (ADH). Allergic reactions: skin rash, itching, photosensitivity, angioedema, urticaria.
Other:
hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, urinary retention, pollakiuria.
With long-term treatment, especially in high doses, if it is abruptly stopped, withdrawal syndrome may develop:
nausea, vomiting, diarrhea, headache, malaise, sleep disturbances, unusual dreams, unusual agitation; with gradual withdrawal after long-term treatment - irritability, motor restlessness, sleep disturbances, unusual dreams.
The connection with the drug has not been established:
lupus-like syndrome (migratory arthritis, the appearance of antinuclear antibodies and positive rheumatoid factor), liver dysfunction, ageusia.
Overdose
Symptoms.
From the side of the central nervous system:
drowsiness, stupor, coma, ataxia, hallucinations, anxiety, psychomotor agitation, decreased ability to concentrate, disorientation, confusion, dysarthria, hyperreflexia, muscle rigidity, choreoathetosis, epileptic syndrome.
From the SSS side:
decreased blood pressure, tachycardia, arrhythmia, intracardiac conduction disturbances, ECG changes (especially QRS) characteristic of intoxication with tricyclic antidepressants, shock, heart failure; in very rare cases - cardiac arrest.
Other:
respiratory depression, shortness of breath, cyanosis, vomiting, hyperthermia, mydriasis, increased sweating, oliguria or anuria.
Symptoms develop 4 hours after an overdose, reach a maximum after 24 hours and last 4-6 days. If an overdose is suspected, especially in children, the patient should be hospitalized.
Treatment:
for oral administration: gastric lavage, intake of activated charcoal; symptomatic and supportive therapy; for severe anticholinergic effects (lowering blood pressure, arrhythmia, coma, myoclonic epileptic seizures) - administration of cholinesterase inhibitors (the use of physostigmine is not recommended due to the increased risk of seizures); maintaining blood pressure and water-electrolyte balance. Monitoring of cardiovascular functions (including ECG) for 5 days (relapse may occur after 48 hours or later), anticonvulsant therapy, artificial pulmonary ventilation (ALV) and other resuscitation measures are indicated. Hemodialysis and forced diuresis are ineffective.
Drug interactions
When ethanol is used together with drugs that depress the central nervous system (including other antidepressants, barbiturates, benzadiazepines and general anesthetics), a significant increase in the depressant effect on the central nervous system, respiratory depression and hypotensive effect is possible. Increases sensitivity to drinks containing ethanol.
Increases the anticholinergic effect of drugs with anticholinergic activity (for example, phenothiazine derivatives, antiparkinsonian drugs, amantadine, atropine, biperiden, antihistamines), which increases the risk of side effects (from the central nervous system, vision, intestines and bladder). When used together with anticholinergic blockers, phenothiazine derivatives and benzodiazepines, there is a mutual enhancement of the sedative and central anticholinergic effects and an increased risk of epileptic seizures (lowering the threshold of convulsive activity); Phenothiazine derivatives may also increase the risk of neuroleptic malignant syndrome.
When used together with anticonvulsants, it is possible to enhance 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 used together with antihistamines, clonidine - increased inhibitory effect on the central nervous system; with atropine - increases the risk of paralytic intestinal obstruction; with drugs that cause extrapyramidal reactions - an increase in the severity and frequency of extrapyramidal effects.
With the simultaneous use of amitriptyline and indirect anticoagulants (coumarin or indadione derivatives), the anticoagulant activity of the latter may increase. Amitriptyline may enhance depression caused by glucocorticosteroids (GCS). Medicines used to treat thyrotoxicosis increase the risk of developing 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 dose reduction of 20-30% may be required), inducers of microsomal liver enzymes (barbiturates, carbamazepine, phenytoin, nicotine and oral contraceptives) reduce plasma concentrations and reduce the effectiveness of amitriptyline.
Combined use with disulfiram and other acetaldehydrogenase inhibitors provokes delirium.
Fluoxetine and fluvoxamine increase plasma concentrations of amitriptyline (a 50% reduction in amitriptyline dose may be required).
Estrogen-containing oral contraceptives and estrogens may increase the bioavailability of amitriptyline.
With the simultaneous use of amitriptyline with clonidine, guanethidine, betanidine, reserpine and methyldopa - a decrease in the hypotensive effect of the latter; with cocaine - the risk of developing cardiac arrhythmias.
Antiarrhythmic drugs (such as quinidine) increase the risk of developing rhythm disturbances (possibly slowing down the metabolism of amitriptyline).
Pimozide and probucol may increase cardiac arrhythmias, which is manifested by prolongation of the QT interval on the ECG.
It enhances the effect of epinephrine, norepinephrine, isoprenaline, ephedrine and phenylephrine on the cardiovascular system (including when these drugs are part of local anesthetics) and increases the risk of developing heart rhythm disturbances, tachycardia, and severe arterial hypertension.
When co-administered with alpha-adrenergic agonists for intranasal administration or for use in ophthalmology (with significant systemic absorption), the vasoconstrictor effect of the latter may be enhanced.
When taken together with thyroid hormones, there is a mutual enhancement of the therapeutic effect and toxic effects (including cardiac arrhythmias and a stimulating effect on the central nervous system).
M-anticholinergic drugs and antipsychotic drugs (neuroleptics) increase the risk of developing hyperpyrexia (especially in hot weather).
When co-administered with other hematotoxic drugs, increased hematotoxicity is possible.
Incompatible with MAO inhibitors (increased frequency of periods of hyperpyrexia, severe convulsions, hypertensive crises and patient death are possible).
special instructions
Before starting treatment, blood pressure monitoring is necessary (in patients with low or labile blood pressure, it may decrease even more); during the treatment period - 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, development of flu-like symptoms and sore throat), during long-term therapy - control of the functions of the cardiovascular system and liver. In the elderly and patients with cardiovascular diseases, monitoring of heart rate, blood pressure, and ECG is indicated. Clinically insignificant changes may appear on the ECG (smoothing of the T wave, depression of the ST segment, widening of the QRS complex).
Caution is required when suddenly moving to a vertical position from a “lying” or “sitting” position.
During the treatment period, the use of ethanol should be avoided.
Prescribed no earlier than 14 days after discontinuation of MAO inhibitors, starting with small doses.
If you suddenly stop taking it after long-term treatment, withdrawal syndrome may develop.
Amitriptyline in doses above 150 mg/day. reduces the threshold of convulsive activity (the risk of epileptic seizures in predisposed patients should be taken into account, as well as in the presence of other factors predisposing to the occurrence of convulsive syndrome, for example, brain damage of any etiology, simultaneous use of antipsychotic drugs (neuroleptics), during the period of abstinence from ethanol or withdrawal of medications with anticonvulsant properties, such as benzodiazepines). Severe depression is characterized by a risk of suicidal actions, which can persist until significant remission is achieved. In this regard, at the beginning of treatment, a combination with drugs from the group of benzodiazepines or antipsychotic drugs and constant medical supervision (entrust trusted persons with the storage and dispensing of drugs) may be indicated. In children, adolescents and young adults (under 24 years of age) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and behavior. Therefore, when prescribing amitriptyline or any other antidepressants in this category of patients, the risk of suicide should be weighed against the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, but it decreased slightly in people over 65 years of age. During treatment with antidepressants, all patients should be monitored for early detection of suicidal tendencies.
In patients with cyclic affective disorders during the depressive phase, manic or hypomanic states may develop during therapy (reducing the dose or discontinuing the drug and prescribing an antipsychotic drug is necessary). After relief of these conditions, if indicated, treatment in low doses can be resumed.
Due to possible cardiotoxic effects, caution is required when treating patients with thyrotoxicosis or patients receiving thyroid hormone preparations.
In combination with electroconvulsive therapy, it is prescribed only under the condition of careful medical supervision.
In predisposed patients and elderly patients, it can provoke the development of drug-induced psychoses, mainly at night (after discontinuation of the drug, they disappear within a few days).
May cause paralytic ileus, primarily in patients with chronic constipation, the elderly, or those forced to bed rest.
Before performing general or local anesthesia, the anesthesiologist should be warned that the patient is taking amitriptyline.
Due to the anticholinergic effect, there may be a decrease in tear production and a relative increase in the amount of mucus in the tear fluid, which can lead to damage to the corneal epithelium in patients using contact lenses.
With long-term use, an increase in the incidence of dental caries is observed. The need for riboflavin may be increased.
Animal reproduction studies have shown adverse effects on the fetus, and there are no adequate and well-controlled studies in pregnant women. In pregnant women, the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus.
Passes into breast milk and may cause drowsiness in nursing infants. To avoid the development of withdrawal syndrome in newborns (manifested by shortness of breath, drowsiness, intestinal colic, increased nervous excitability, increased or decreased blood pressure, tremor or spastic phenomena), amitriptyline is gradually discontinued at least 7 weeks before the expected birth.
Children are more sensitive to acute overdose, which should be considered dangerous and potentially fatal to 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.
Pregnancy and lactation
In pregnant women, the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus.
Passes into breast milk and may cause drowsiness in nursing infants. To avoid the development of withdrawal syndrome in newborns (manifested by shortness of breath, drowsiness, intestinal colic, increased nervous excitability, increased or decreased blood pressure, tremor or spastic phenomena), amitriptyline is gradually discontinued at least 7 weeks before the expected birth.
What is the drug?
The drug is produced in the form of dragees, tablets, capsules and solution for intramuscular or intravenous administration. It is sold in pharmacies only by prescription. You should start taking Amitriptyline tablets with a minimum dose and gradually increase it. Take them after eating food at a specific time of the day, with plenty of water. Amitriptyline injections are administered slowly, often changing the injection site. After 3 weeks, injections should be replaced with tablets. The rate of use of the drug is indicated below.
