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Maprotiline ( Ludiomil )
Maprotiline hydrochloride Classification: Antidepressant, tetracyclic See Also: See also Antidepressants, Tricyclic. Action/Kinetics: A tetracyclic compound but has many similarities to the tricyclic drugs. Causes moderate anticholinergic, sedative, and orthostatic hypotensive effects. Effective plasma levels: 200-300 ng/mL. t1/2: Approximately 21-25 hr. Peak effect: 12 hr. Beneficial effects may not be observed for 2-3 weeks. Uses: Depressive illness, including depressive neuroses, manic-depressive illness, and major depressive disorder. Investigational: Relief of anxiety associated with depression. Additional Contraindications: Known or suspected seizure disorders. Special Concerns: Not recommended for clients under 18 years of age. Additional Side Effects: Overdosage may cause increased incidence of seizures. Drug Interactions: Anticholinergic drugs / Additive atropine-like side effects Diazepam / Additive effect on impairment of motor skills Ethanol / Additive effect on impairment of cognitive and motor skills Guanethidine / Maprotiline may block the effects of guanethidine Phenothiazines / Risk of seizures Thyroid hormones / Risk of CV toxicity How Supplied: Tablet: 25 mg, 50 mg, 75 mg Dosage Maprotiline (Ludiomil) is an antidepressant used to treat depression with or without anxiety. Maprotiline has been shown to exhibit an antidepressant action. It strongly inhibits the uptake of noradrenaline in the brain and peripheral tissues, though it is notable in its lack of inhibition of serotonergic uptake. Maprotiline also exerts a sedative effect on the anxiety component of depressive illness. Similar to other tricyclic antidepressants, maprotiline lowers the convulsive threshold. Following repeated daily doses of maprotiline, a plasma steady state concentration was reached in the second week, with the majority of subjects receiving daily doses of 150 mg attaining steady state blood levels between 100 and 400 ng/mL. Indications and Usage Ludiomil is used to treat depression, including the depressed phase of manic-depressive illness (bipolar disorder), psychotic depression (unipolar depression), and involutional melancholia. It might also be useful in selected patients suffering severe depressive neurosis. Maprotiline should not be given in conjunction with, or within 14 days of treatment with a MAO inhibitor. Combined therapy of this type could lead to the appearance of serious interactions such as hyperpyrexia, tremors, generalized clonic convulsions, delirium and possible death. Contraindicated in patients with a history of hypersensitivity to Maprotiline. Maprotiline is contraindicated during the acute recovery phase following myocardial infarction in the presence of acute congestive heart failure, and in patients with conduction defects. Should not be used in patients with known or suspected convulsive disorders. Maprotiline lowers the seizure threshold. Patients with narrow angle glaucoma should not be given maprotiline. Patients with urinary retention due to prostatic disease should not receive maprotiline. Maprotiline should be withdrawn in cases of acute poisoning with alcohol, hypnotics, analgesics or psychotropic drugs. Cardiovascular: Tricyclic and tetracyclic antidepressants, particularly in high doses, have been reported to produce arrhythmias. A few instances of unexpected death have been reported in patients with cardiovascular disorders. Myocardial infarction and stroke have also been reported with these drugs. Therefore, extreme caution should be used when maprotiline is given to elderly patients, or those with known cardiovascular disease including those with a history of myocardial infarction, arrhythmias and/or ischemic heart disease. Maprotiline should be used with caution in hyperthyroid patients and in those on thyroid medication because of the possibility of cardiovascular toxicity. Maprotiline should be used with caution in patients receiving guanethidine or similar sympatholytic antihypertensive agents (bethanidine, reserpine, alpha-methyldopa, clonidine) since it may block the effects of these drugs with subsequent loss of blood pressure control. Seizures: Seizures have been reported in patients without a known history of seizures who were treated with maprotiline at therapeutic dose levels. The risk of seizures may be increased when maprotiline is taken concomitantly with phenothiazines, when the dosage of benzodiazepines is rapidly tapered in patients receiving maprotiline, or when the recommended dosage of maprotiline is rapidly exceeded. The risk of seizures may be reduced by: initiating therapy at a low dosage; maintaining the initial dosage for 2 weeks before raising it gradually in small increments. Because of its anticholinergic properties, maprotiline should be used with caution in patients with a history of increased intraocular pressure or history of urinary retention, particularly in the presence of prostatic hypertrophy. Psychosis: An activation of psychosis has occasionally been observed in schizophrenic patients administered tricyclic antidepressant drugs and must be considered as a possibility when administering maprotiline. Hypomanic or manic episodes: in patients with cyclic disorders have been known to occur during treatment of a depressed phase with a tricyclic antidepressant. These 2 conditions, should they occur, may require a reduction in the dosage of maprotiline, discontinuation of the drug, and/or administration of an antipsychotic agent. Suicide: The possibility of suicide in seriously depressed patients is inherent in their illness and may persist until significant remission occurs. Therefore, patients must be carefully supervised during all phases of treatment with maprotiline and prescriptions should be written for the smallest amount consistent with good management. Cardiovascular: Particularly in patients with heart diseases, as well as in elderly subjects, cardiac function should be monitored and ECG examinations performed during long-term treatment with high doses. Regular measurements of the blood pressure are called for in patients susceptible to postural hypotension. Constipation: Tricyclic antidepressants may give rise to paralytic ileus, particularly in the elderly and in hospitalized patients. Therefore, since maprotiline has similar anticholinergic properties, appropriate measures should be taken if constipation occurs. Usage in Children: The drug is not recommended for use in children. Pregnancy and Withdrawl: Safe use of Maprotiline during pregnancy or lactation has not been established; therefore, its use in pregnancy, in nursing mothers or in women of childbearing potential requires that the benefits of treatment be weighed against the possible risks to mother and child. Interference with Cognitive or Motor Performance: Since Maprotiline may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks, such as operating an automobile or machinery, the patient should be cautioned accordingly. Prior to elective surgery: Little is known about the interaction between maprotiline and general anesthetics. Maprotiline should be discontinued for as long as clinically feasible. Drug Interactions Maprotiline should not be given in conjunction with, or within 14 days of treatment with a MAO inhibitor. Combined therapy of this type could lead to the appearance of serious interactions such as hyperpyrexia, tremors, generalized clonic convulsions, delirium and possible death. While taking maprotiline, responses to alcoholic beverages, barbiturates, and other CNS depressants may be exaggerated. Maprotiline may diminish or abolish the antihypertensive effects of adrenergic neuron blocking drugs, such as guanethidine, bethanidine, reserpine, clonidine and alpha-methyldopa. Therefore, patients requiring concomitant treatment for hypertension should be given antihypertensives of a different type (i.e., diuretics, vasodilators, or beta-blockers which do not undergo pronounced biotransformation). Maprotiline may potentiate the cardiovascular effects of indirect and directly acting sympathomimetic drugs such as noradrenaline, adrenaline, and methylphenidate. Maprotiline may also potentiate the effects of anticholinergic drugs (atropine, biperiden) and levodopa. Therefore, close supervision and careful adjustment of dosage is required when administering maprotiline with anticholinergic or sympathomimetic drugs because of the possibility of additive effects. Drugs that activate hepatic microsomal enzymes, such as barbiturates, phenytoin, oral contraceptives and carbamazepine, may accelerate the metabolism of maprotiline resulting in decreased antidepressant efficacy. If necessary, the dosage should be adapted accordingly. Concomitant treatment with maprotiline and major tranquilizers may result in increased plasma levels of maprotiline, a lowered convulsion threshold, and seizures. The combination of maprotiline and benzodiazepines may cause increased sedation. Concurrent use of parenteral magnesium sulfate and maprotiline may result in serious potentiation of CNS depressant effects. BEFORE USING THIS MEDICINE: INFORM YOUR DOCTOR OR PHARMACIST of all prescription and over-the-counter medicine that you are taking. This includes other medicines to treat depression. Inform your doctor of any other medical conditions including a recent heart attack, epilepsy, allergies, pregnancy, or breast-feeding. Adverse Reactions This medicine may cause blurred vision, especially during the first few weeks of treatment. Adverse reactions with maprotiline have been mild and transient, usually disappearing with continued treatment or following a reduction in the dosage. Check with your doctor as soon as possible if any of the following side effects occur: More common: Skin rash, redness, swelling, or itching. Less common: Constipation (severe); nausea or vomiting; shakiness or trembling; seizures (convulsions); unusual excitement; weight loss. Rare: Breast enlargement—in males and females; confusion (especially in the elderly); difficulty in urinating; fainting; hallucinations (seeing, hearing, or feeling things that are not there); inappropriate secretion of milk—in females; irregular heartbeat (pounding, racing, skipping); sore throat and fever; swelling of testicles; yellow eyes or skin. Other common side effects are: Blurred vision; decreased sexual ability; dizziness or lightheadedness (especially in the elderly); drowsiness; dryness of mouth; headache; increased or decreased sexual drive; tiredness or weakness; constipation (mild); diarrhea; heartburn; increased appetite and weight gain; increased sensitivity of skin to sunlight; increased sweating; trouble in sleeping; weight loss. Signs and Symptoms Symptoms of an overdose are convulsions (seizures); dizziness (severe); drowsiness (severe); fast or irregular heartbeat; fever; muscle stiffness or weakness (severe); restlessness or agitation; trouble in breathing; vomiting; and dilated pupils. Treatment If you or someone you know may have used more than the recommended dose of this medicine, contact your local poison control center or emergency room immediately. No specific antidote is known. Maintain adequate airway, empty stomach contents, and treat symptomatically. Cardiac arrhythmias and CNS involvement pose the greatest threat and may occur suddenly even when initial symptoms appear to be mild. Therefore, patients who may have ingested an overdosage of maprotiline, particularly children, should be hospitalized and kept under close surveillance. Several days to weeks may pass before you feel the full benefit of this medicine. Do not stop taking this medicine without checking with your doctor.
Additional Information:: Do not share this medicine with others for whom it was not prescribed. Do not use this medicine for other health conditions. Keep this medicine out of the reach of children. Patients should be kept under medical surveillance during treatment with maprotiline. The dosage of maprotiline should be individualized according to the requirements of each patient. Sometimes this medicine must be taken for up to 2 or 3 weeks before you begin to feel better. Adults: At first, 25 milligrams (mg) taken one to three times a day. Your doctor may increase your dose as needed. However, the dose is usually not more than 150 mg a day, unless you are in the hospital. Some hospitalized patients may need higher doses. (a higher initial dose of 100 mg daily in 2 or 3 divided doses may be indicated. The usual optimal dose in these patients is 150 mg daily, but some patients may require up to 225 mg in divided doses). When these higher doses are used, it is essential to exclude a history of convulsive disorders. Elderly and Debilitated Patients: In general, lower dosages are recommended for these patients, and doses should only be increased in gradual increments. Initially, 10 mg 3 times daily is suggested, with very gradual increments, depending on tolerance and response, up to 75 mg daily in divided doses. Children: This medicine is not recommended for use in children. Discontinuation: After you stop taking this medicine, your body will need time to adjust. This usually takes about 3 to 10 days. Continue to follow the precautions listed above during this period of time.
Tablets:: available in 25 mg, 50 mg, 75 mg.
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