Lyudiomil is a tetracyclic antidepressant with a significant number of properties inherent in tricyclic antidepressants. It is characterized by a well-balanced spectrum of action, eliminates psychomotor inhibition, agitation and anxiety, improves mood.
Release form and composition
Drug forms of Lyudiomil:
- Tablets, coated (10 mg - 10 pcs. In blisters, 5 blisters in a cardboard box; 25 mg and 50 mg - 10 pcs. In blisters, 3 blisters in a cardboard box);
- Concentrate for preparation of solution for infusions (5 ml in ampoules, 10 ampoules in a carton box).
The active ingredient of the drug is maprotilina hydrochloride:
- In 1 tablet - 10, 25 or 50 mg;
- In 1 ml of concentrate - 5 mg.
Additional components of tablets 10 mg:
- Excipients: pregelatinized corn starch, talc, magnesium stearate, calcium phosphate, lactose monohydrate, stearic acid, silica colloidal anhydrous dioxide;
- Shell composition: titanium dioxide, talc, polysorbate 80, hypromellose, iron dye yellow oxide.
Excipients of tablets 25 and 50 mg: wheat starch, calcium phosphate, colloidal anhydrous silicon, lactose monohydrate, hydroxypropyl cellulose, titanium oxide, stearic acid, polysorbate 80, magnesium stearate, talc, iron yellow oxide, iron red oxide.
Concentrates of the concentrate: methanesulfonic acid, mannitol, water for injections.
Indications for use
- Somatogenic depression;
- Psychogenic, neurotic and reactive depression;
- Masked Depression;
- Depression of exhaustion;
- Endogenous and involutional depression;
- Menopausal (menopausal) depression;
- Other depressive mood disorders characterized by dysphoria, anxiety, or irritability; a state of apathy (especially in older people); complaints of somatic or psychosomatic nature in patients with depression and / or in the presence of anxiety.
Application Lyudiomila contraindicated in the following cases:
- Angle-closure glaucoma;
- Acute stage of myocardial infarction, intracardiac conduction disorders;
- Severe renal / hepatic function;
- Delayed urine flow (for example, due to prostate disease);
- Diseases accompanied by convulsive syndrome or low threshold of convulsive readiness (including brain damage of any origin, alcoholism);
- Acute alcohol poisoning, psychotropic or hypnotic drugs;
- The simultaneous use of monoamine oxidase inhibitors (MAO);
- Cross-hypersensitivity to tricyclic antidepressants;
- Hypersensitivity to the drug.
With caution, Lyudiomil is prescribed in such cases:
- Increased intraocular pressure in history;
- Diseases of the cardiovascular system;
- Simultaneous administration of thyroid hormone preparations;
- Elderly age.
Dosing and Administration
The doctor selects the dosing regimen for each patient individually, depending on the state and reaction to the drug. For example, the entire daily dose may be given in one dose by day, an evening dose may be increased, and the daily dose may be reduced at the same time.
The maximum permissible daily dose is 150 mg.
After a significant improvement in the condition, which is manifested by a decrease in the severity of symptoms, you can try to reduce the dose of Lyudiomil. However, in case of deterioration, the dose should be immediately raised to the initial level.
The goal of therapy is to achieve a therapeutic effect when taking the smallest effective dose. This is especially important in the treatment of adolescents and the elderly, because they are characterized by instability of the autonomic nervous system and a more pronounced reaction to maprotilin.
Tablets Lyudiomil should be taken orally, swallowing whole, squeezed water.
In case of depression of moderate and moderate severity (especially in outpatient patients), the drug is prescribed in 25 mg from 1 to 3 times a day or in a dose of 25-75 mg 1 time per day. The specific dose depends on the severity of symptoms and the effectiveness of Lyudiomil.
For severe depression (especially in patients in the hospital), the drug is used in 25 mg 3 times a day or at a dose of 75 mg 1 time per day. If necessary, gradually increase the daily dose to a maximum of 150 mg (in 1 or several doses).
From Lyudiomil concentrate, a solution is prepared which is administered as an intravenous infusion. The daily dose is 25-100 mg. When prescribing a dose of 25-50 mg, the contents of 1 or 2 ampoules (respectively) are diluted in 250 ml of glucose solution or isotonic sodium chloride solution and injected within 1.5-2 hours. At purpose of a dose of 75-150 mg contents of 3-6 ampoules dissolve in 500 ml of solvent, and enter within 2-3 hours. After a clear positive trend is noted (usually it takes 1-2 weeks), the patient is transferred to a tablet form of the drug.
With other depressed mood disorders, children and adolescents are prescribed 10 mg 3 times a day or 25 mg 1 time a day. If necessary, with each dose, the dose is slightly increased, up to the achievement of a dose of 25 mg 3 times a day or 75 mg 1 time a day.
It should be noted that the experience of using Lyudiomil in pediatrics is limited, therefore, the described dosing regimen for children should be considered as approximate recommendations. Adolescents, if necessary, the drug can be prescribed in a dose of a similar adult.
Prescribing lower doses is generally recommended for older people. The initial, as a rule, is 10 mg 3 times a day or 25 mg 1 time a day. If necessary, with each dose, the dose is slightly increased until a daily dose of 75 mg is reached (25 mg 3 times a day or 75 mg 1 time a day). The specific dose depends on the effectiveness of treatment and tolerability of maprotiline.
Patients should be under the supervision of a physician for the entire period of treatment.
The side effects given below develop at use as Lyudiomil, and tricyclic antidepressants in general:
- Central and peripheral nervous system. Mental status: often - feeling tired, sleepy; sometimes - sedation during the daytime, anxiety, anxiety, impaired memory and concentration, a feeling of tension, increased appetite, manic state, aggressiveness, hypomania, nightmares, sleep disturbances, insomnia, increased depression; rarely - nervousness, confusion, delirium, hallucinations (mainly in older people); in some cases - depersonalization, activation of symptoms of psychosis. Neurological status: often - small-scale tremor, headache, myoclonus, slight dizziness; sometimes - paresthesia (tingling, numbness), dysarthria, dizziness, muscle weakness; rarely - akathisia, ataxia, convulsions; in some cases - disorders of coordination of movements, dyskinesia, changes in the electroencephalogram;
- The digestive system: sometimes - abdominal discomfort, nausea, vomiting; rarely, elevated liver enzymes, diarrhea; in some cases - hepatitis (including jaundice);
- Endocrine system and metabolism: sometimes - impaired libido and potency, weight gain; in some cases - galactorrhea, an increase in the mammary glands, syndrome of inadequate secretion of antidiuretic hormone;
- Cardiovascular system: sometimes - orthostatic hypotension, palpitations, sinus tachycardia, clinically insignificant ECG changes (for example, changes in T wave or ST interval) in patients who do not have abnormalities of the heart; rarely - increased blood pressure, arrhythmias; in some cases - fainting, violations of intracardiac conduction (for example, blockade of the bundle of the bundle of His, expansion of the QRS complex, changes in the PQ interval);
- Hematopoietic system: in some cases - eosinophilia, agranulocytosis, thrombocytopenia, leukopenia;
- Respiratory system: in some cases - bronchospasm, allergic alveolitis, incl. with eosinophilia;
- Sense organs: in some cases - taste disturbances, tinnitus, nasal congestion;
- Dermatological reactions: sometimes - photosensitivity and allergic skin reactions (urticaria, rash), including those accompanied by fever; in some cases, cutaneous vasculitis, hair loss, edema (local or general), purpura, pruritus, erythema multiforme;
- Effects caused by anticholinergic activity: often - dry mouth; sometimes - disturbance of accommodation, blurred vision, hot flashes, impaired urination, sweating, constipation; in some cases - dental caries, stomatitis.
With abrupt withdrawal of the drug or a rapid dose reduction, the following symptoms are possible: abdominal pain, nausea, vomiting, diarrhea, irritability, headache, anxiety, insomnia, and increased depressive mood disorders or depression about which treatment was given. Usually described side effects are mild, are transient in nature and are their own. They are not always associated precisely with the concentration of Lyudiomil in plasma or with the dose of the drug. Often, some side effects are difficult to distinguish from symptoms associated with depression, such as sleep disturbances, general weakness, anxiety, agitation, dry mouth, and constipation.
In severe depressions, the risk of suicidal feelings, which may persist until the onset of remission, always increases. In rare cases, antidepressants may increase suicidal tendencies. For this reason, patients at all stages of treatment should be closely monitored.
There are reports of rare cases of seizures with the use of Lyudiomil in therapeutic doses in patients with a history of no evidence of convulsions. Sometimes there was a concomitant presence of predisposing factors, for example, the simultaneous use of drugs that reduce the threshold of convulsive readiness. The risk of seizures increases with a rapid increase in the dose of Lyudiomil, with abrupt cancellation of concomitantly used bezodiazepines or in the case of simultaneous use of phenothiazine derivatives. And although a clear causal relationship has not been identified, it is obvious that the likelihood of developing seizures can be reduced, subject to certain recommendations: start treatment with a small dose; increase the dose at least at 2-week intervals and small steps; for long-term maintenance therapy, prescribe the minimum effective dose; not to use at the same time drugs that reduce the threshold of convulsive readiness, and if the use of such funds is still necessary, change the dose with extreme caution; do not abruptly discontinuously apply benzodiazepines.
Lyudiomil can cause sinus tachycardia, arrhythmias, and slowing of intracardiac conduction. For this reason, the drug should be used with caution in the elderly and patients with diseases of the cardiovascular system (including ischemic heart disease, arrhythmias, myocardial infarction in history). These categories of patients, especially with long-term antidepressant therapy, should regularly monitor heart function, including an electrocardiogram. Patients prone to orthostatic hypotension should be regularly measured blood pressure.
If it is necessary to conduct electroconvulsive therapy for patients receiving Lyudiomil, especially careful monitoring is required.
The drug may affect the number of leukocytes in the peripheral blood. And although such cases are rare, it is necessary to monitor this indicator and be wary of such symptoms as sore throat and fever, especially in the first months of treatment and during long-term therapy.
Tricyclic antidepressants can contribute to the development of paralytic intestinal obstruction, especially in the elderly and inpatient patients. Therefore, in case of constipation should take appropriate measures.
With prolonged use of Lyudiomil, it is recommended to periodically monitor indicators of kidney and liver function, to conduct a dental examination.
Due to the anticholinergic action of tricyclic antidepressants, tearing may decrease and the amount of mucus in the composition of the tear fluid may increase relatively, resulting in possible corneal epithelium damage in patients who use contact lenses.
Before anesthesia (both general and local), the anesthesiologist should be warned about the reception of Lyudiomil.
Before prescribing the drug, the patient must be warned that possible disorders of the central nervous system, including blurred vision and drowsiness. If they develop, you should refrain from driving and working with potentially dangerous consequences. In addition, it is important to indicate that alcohol may exacerbate these side effects.
Lyudiomil should not be prescribed during treatment with MAO inhibitors and for 14 days after their withdrawal, because Such a combination is fraught with the development of pronounced drug interactions that can lead to tremor, hyperpyrexia, delirium, generalized clonic seizures, and even death. The same applies to cases where MAO inhibitors must be applied after the withdrawal of Lyudiomil.
Maprotiline hydrochloride can reduce or even completely block the hypotensive effect of drugs that affect the transfer of adrenergic arousal: reserpine, betanidin, clonidine, guanethidine, alphamethyldopa. If necessary, treatment for arterial hypertension during the period of using Lyudiomil should be prescribed drugs of a different type, for example, beta-blockers, vasodilators or diuretics, which are not subjected to severe biotransformation. At the same time, it is important to bear in mind that abrupt cancellation of Lyudiomil may lead to the development of severe arterial hypotension.
Maprotiline may enhance the cardiovascular effects of sympathomimetic drugs such as norepinephrine (norepinephrine), epinephrine (epinephrine), phenylephrine, ephedrine, and isoprenaline, even when they are part of local anesthetics (for example, used in dentistry) or nasal drops. In such situations, it is necessary to carefully monitor the patient (control of heart rate and blood pressure) and careful selection of doses of drugs.
Lyudiomil should not be administered concurrently with quinidine-type antiarrhythmic drugs.
Methylphenidate can increase plasma concentrations of tricyclic antidepressants and enhance their action.
Lyudiomil can potentiate the effect of drugs that have anticholinergic properties on the central nervous system, pupil, bladder and intestines (for example, biperiden, atropine, phenothiazines, antiparkinsonian and antihistamines).
Tranquilizers can increase the concentration of maprotilin in the blood plasma, reduce the threshold of convulsive readiness and lead to the development of seizures.
The combination of Lyudiomil with thioridazine can cause severe arrhythmias.
Drugs that activate microsomal liver enzymes (oral contraceptives, barbiturates and carbamazepine) can decrease the effectiveness of Peopleome. If necessary, the use of such a combination is necessary dose adjustment. In addition, there may be an increase in the concentration of carbamazepine or phenytoin in the serum and, as a consequence, an increase in the frequency of their side effects, therefore, it is also necessary to revise the doses of both drugs.
Beta-blockers, which are characterized by significant biotransformation (for example, propranolol), can increase the concentration of maprotiline in the blood plasma, therefore, its plasma concentration should be determined regularly and, if necessary, the dose should be adjusted.
Lyudiomil can enhance the anticoagulant effect of coumarin derivatives, so you need to carefully monitor the amount of prothrombin time and, if necessary, reduce the dose of anticoagulant.
Lyudiomil can potentiate the hypoglycemic effect of sulfonylurea and insulin derivatives, therefore, in patients with diabetes mellitus, it is necessary to regularly monitor the level of glucose in the blood.
Fluoxetine and fluvoxamine can significantly increase the level of maprotiline in the blood and lead to the development of corresponding side effects. And given the long half-life of fluvoxamine and fluoxetine, these side effects can persist for a long time.
Lyudiomil enhances the central nervous system depressing effect of alcohol, barbiturates and other drugs that have a similar effect.
With simultaneous use of maprotiline and benzodiazepines may increase the sedative effect.
It is known that cimetidine inhibits the metabolism of some tricyclic antidepressants, resulting in an increase in their concentration in the blood and an increase in the frequency of undesirable reactions (in particular, visual impairment and dry mouth). And although such an interaction was not reported in the case of the use of Lyudiomil, one cannot exclude the possibility that a reduction in its dose may be required.
Terms and conditions of storage
Keep out of reach of children at temperature up to 30 ° С.
Shelf life - 5 years.