Pharmacological properties of the drug Maprotiline
Tetracyclic antidepressant, non-selective inhibitor of neuronal monoamine reuptake. Improves mood, reduces feelings of fear and excitement, eliminates psychomotor retardation and somatic disorders in depression. The therapeutic effect of maprotiline, especially the anxiolytic effect and normalization of sleep, is noted within a few days from the start of treatment. After oral administration, it is completely absorbed from the digestive tract. 88% of maprotiline binds to plasma proteins. The half-life is about 43 hours.
Comparison of the characteristics of the drugs "Fermatron", "Sinokrom" and "Noltrex"
| Sinokrom | Fermatron | Noltrex | |
| Molecular mass | 1.6 million Yes | up to 1 million Yes | more than 10 million Yes |
| Compound | 1% sodium hyaluronate solution | 1% or 1.5% sodium hyaluronate solution | 4.5% solution of artificial biopolymer |
| Number of injections per course | 3-5 | 3-4 | 1-3 |
| After what number of injections does improvement occur? | after the third | after the third | after the first |
| Number of injections for severe osteoarthritis | 5 | 5 | 2-4 |
| Duration of effect for moderate to moderate severity of osteoarthritis | up to 6 months | up to 6 months | 6-24 months |
| Rate of elimination from the body | average | average | slow |
| Potential to cause allergies | Yes | Yes | No |
| Indications | moderate to moderate osteoarthritis | moderate to moderate osteoarthritis | osteoarthritis of any severity |
| Local phenomena after administration (redness, pain) | periodically | periodically | very rarely |
| Duration of side effects | 1-3 days | a few days | 12-24 hours |
| Manufacturer | Kroma Pharma GmbH (Austria) | Hyaltech Ltd (UK) | "Bioform" (Russia) |
| Shelf life | 3 years | 3 years | 3 years |
Use of the drug Maprotiline
Orally for depression (mainly in outpatient treatment), 25 mg is prescribed 1-3 times a day or 25-75 mg once (preferably in the evening), depending on the severity of symptoms and therapeutic effectiveness. For severe depression (preferably in a hospital setting) - 25 mg 3 times a day or 75 mg once (preferably in the evening). If necessary, the daily dose can be increased to 150 mg (once or in several doses). For newly diagnosed severe depression or when oral administration is insufficiently effective, it is administered intravenously at a dose of 25–100 mg/day. If it is necessary to administer a higher dose, an infusion of 75–150 mg is performed over 2–3 hours. After achieving a therapeutic effect (usually within the first 2 weeks of treatment), the patient is transferred to oral maprotiline.
Publications in the media
(Maprotilinum) INN
Synonyms. Ludiomil.
Composition and release form. Maprotiline dragees 0.01, 0.025 and 0.05g; 1.25% Solution in ampoules of 2 ml (25 mg).
Indications. Various forms of depression, including reactive, neurotic, cyclothymic, involutional, accompanied by fear and irritability.
Pharmachologic effect. Maprotiline in its pharmacological properties is close to tricyclic antidepressants. The drug blocks the reuptake of monoamines, but unlike other antidepressants in this group, it strongly inhibits the reuptake of norepinephrine by presynaptic nerve endings, which leads to increased pressor action of norepinephrine and adrenaline. The anticholinergic, adrenolytic and antihistamine activity of maprotiline is moderate; MAO does not cause oppression. The antidepressant effect of maprotiline is accompanied by anxiolytic and moderate sedative effects.
Pharmacokinetics. Maprotiline is slowly but completely absorbed from the gastrointestinal tract into the blood. Peak plasma concentration after taking 0.05 g of the drug is reached after 8 hours. Equilibrium concentration of the drug is achieved at 2 weeks of treatment with repeated doses. Plasma protein binding is 88-89%. Metabolized in the liver; T1/2 averages 43 hours. About 70% of a single dose of the drug is excreted in the urine - 50% in the form of metabolites, 20% unchanged; About 30% of the drug is excreted in feces (in the form of metabolites and unchanged).
Side effects. Headache, dizziness, dysarthria, paresthesia, general weakness, lethargy, drowsiness, dry mouth; skin rash, urticaria; constipation, urinary retention, disturbance of accommodation; leukopenia, agranulocytosis.
Contraindications. Hypersensitivity to the drug; epilepsy; myocardial conduction disorders, recent myocardial infarction; angle-closure glaucoma; prostate adenoma.
Adverse reactions when interacting with other drugs. With the simultaneous use of maprotiline with guanethidine and betadine, the hypotensive effect of the latter is reduced. The drug enhances the sedative effect of reserpine and methyldopa. When maprotiline is taken together with sympathomimetic drugs, the effect on the cardiovascular system of the latter increases. Maprotiline, when administered concomitantly with drugs that depress the central nervous system (barbiturates, antipsychotics, benzodiazepines), potentiates the inhibitory effect on the central nervous system of these drugs. Maprotiline enhances the anticholinergic properties of drugs from the atropine group. Barbiturates and carbamazepine, which stimulate microsomal liver enzymes, reduce the antidepressant effect of maprotiline. Maprotiline may increase serum concentrations of phenytoin (diphenine) and increase its side effects. When taking maprotiline simultaneously with tranquilizers, the concentration of maprotiline in the blood serum may increase, the seizure threshold may decrease, and convulsions may occur.
Information for the patient. For adults, maprotiline is usually prescribed 0.025 g 1-3 times a day, or the daily dose of the drug is taken in one dose after meals, swallowing the tablets whole, without chewing and drinking plenty of water. If necessary, the dose can be increased. Driving vehicles and drinking alcoholic beverages are not recommended during treatment with the drug. With long-term use of maprotiline, cases of caries have been observed. After therapy with MAO inhibitors, a break of 14 days should be taken before starting maprotiline therapy and vice versa. Missed dose: Take the missed dose as soon as possible; if there is no time left before taking the next dose of the drug, then do not take it at all; do not take double doses.
Special instructions for the use of Maprotiline
Maprotiline should be used with caution in patients with impaired liver or kidney function, urinary disorders and increased intraocular pressure. With long-term use of high doses, monitoring of ECG and other functional indicators of the heart is necessary, especially in patients with diseases of the cardiovascular system and in elderly patients. In persons with a tendency to orthostatic hypotension, blood pressure should be regularly monitored. During treatment, you should refrain from drinking alcohol, as well as from driving vehicles and performing other work that requires a quick psychomotor reaction. Parenterally used only in a hospital setting. During pregnancy, maprotiline is used only in cases of extreme necessity and in the absence of alternative treatment. Maprotiline during a course of use is determined in breast milk in a concentration exceeding the concentration in the blood plasma of a breastfeeding woman.
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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Maprotiline, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.
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Drug interactions Maprotiline
Cannot be used simultaneously with MAO inhibitors; the interval between their administration should be at least 2 weeks. Maprotiline may reduce or completely eliminate the antihypertensive effect of antiadrenergic agents (eg, guanethidine). Maprotiline may potentiate the cardiovascular effects of epinephrine or norepinephrine, as well as the activity of CNS depressants and anticholinergic drugs.
List of pharmacies where you can buy Maprotiline:
- Moscow
- Saint Petersburg
Molecular weight of drugs: why you need to know about it
Molecular weight is information that manufacturers of many synovial fluid endoprostheses deliberately keep silent. Instead, various marketing information about hyaluronic acid injections is presented, often not supported by facts.
Let's look at the problem from a scientific point of view. High molecular weight drugs have multiple intermolecular cross-links. In order for the endoprosthesis to dissolve in the joint, they must be neutralized - the molecules gradually disintegrate and are eliminated from the body. The higher the molecular weight of the drug, the longer the period of molecular breakdown, which means the drug will remain inside the joint longer . In analogues with low molecular weight (including Fermatron, Sinokrom), this process occurs very quickly, so the person is forced to go for the procedure again and again.
The main task of liquid endoprostheses, be it Fermatron or Noltrex, is to stay in the joint capsule for as long as possible, cover damaged cartilage and prevent their friction. The longer they remain in the joint, the longer a person diagnosed with osteoarthritis will not experience pain during movement. This period does not directly depend on the name of the drug or on the dosage of hyaluronic acid, and not even on the country of origin: only the molecular weight matters.
Preparations based on hyaluronic acid “Fermatron” and “Sinokrom” have a molecular weight of 1 and 1.6 million Da, respectively. The molecular weight of Noltrex is more than 10 million Yes, that is, the synthetic synovial fluid substitute is absorbed and excreted from the body almost 10 times longer! This explains its longer effect - up to two years, as well as quick results - after the first injection.
Noltrex is the only drug on the market with a high molecular weight (more than 10 million Da)
