Maprotiline

Category :

Antidepressant

Composition :

Each tablet contains 25 or 75 mg of maprotiline hydrochloride .

Chemistry :

Maprotiline hydrochloride is a tetracyclic antidepressant.

Mechanism of Action :

Maprotiline is thought to increase the synaptic concentration of norepinephrine in the central nervous system ( CNS ) by blocking its re-uptake by the presynaptic neuronal membrane .
No effect on serotonin re-uptake has been observed Recent research has suggested that after long-term treatment with antidepressants , changes in post synaptic beta-adrenergic receptor sensitivity and enhancement of response to alpha-adrenergic and serotonergic stimulation may contribute to the mechanism of antidepressant action . ( USP DI 2005 )

Pharmacokinetics :

The mean time to peak is 12 hours . The half-life of elimination averages 43 hours.

Indications :

Maprotiline is indicated for the treatment of depressive illness in patients with major depressive disorder , dysthymic disorder , or bipolar disorder , depressed type .
Maprotiline is also indicated for the management of anxiety associated with mental depression maprotiline is used to treat some types of chronic pain . ( USP DI 2005 )

Contraindications:

Except under special circumstances , maprotiline should not be used when the following medical problems exist :

• Myocardial infarction , during the acute recovery period .
• Seizure disorders , including epilepsy , or history of seizures .
• Risk – benefit should be considered when the following medical . Problems exist : Alcoholism , Asthma, Blood disorders , Glaucoma , angle-closure , Increased intraocular pressure , urinary retention , Bipolar disorder , Cardiovascular , Gastrointestinal , Hepatic function impairment , Hyperthyroidism , myocardial infarction , Prostatic hypertrophy , Schizophernia , Sensitivity to maprotiline or tricyclic antidepressants . ( USP DI 2005 )

Pregnancy :

Adequate and well-controlled studies in humans have not been done . FDA Pregnancy category B .

Nursing mothers :

Maprotiline is distributed into breast milk in the same concentration as in blood . ( USP DI 2005 )

Precautions :

Regular visits to physician to check progress during therapy .

• Avoiding the use of alcohol or ther CNS depressants during maprotiline therapy .
• Possible drowsiness,caution when driving , using machines , or doing
• other things requiring alertness .
• Possible dizziness or lightheadedness, caution when getting up suddenly from a lying or sitting position .
• Possible dryness of mouth , using sugarless gum or candy , ice or saliva substitute for relief , checking with physician or dentist if dry mouth continues for more than 2 weeks .
• Caution if any kind of surgery , dental treatment , or emergency treatment is required .
• Checking with physician before discontinuing medication , gradual dosage reduction may be needed . ( USP DI 2005 )

Drug Interactions :

The following drug interactions have been selected on the basis of their potential clinical significance – not necessarily inclusive : Alcohol , other CNS depression – producing medications , Anticholinergics or other medications with anticholinergic activity , Antihistamines , Anticonvulsants , tricyclic Antidepressants , Bupropion , Trazodone , Cimetidine , Monoamine oxidase inhibitors , including furazolidone , procarbazine and selegiline , Naphazoline ( ophthalmic ) , phenylephrine ( nasal or ophthalmic ) , Thyroid hormones . ( USP DI 2005 )

Adverse Effects :

Although not all of the following side effects have been attributed specifically to maprotiline , apotential exists for their occurrence as with the tricyclic antidepressants .
The following side/adverse effects have been selected on the basis of their potential clinical significance-not necessarily inclusive : Skin rash , redness, swelling , itching , constipation , severe , nausea or vomiting , seizures , shakiness , unusual excitement , weight loss .( USP DI 2005 )

Overdose :

The following effects have been selected on the basis of their potential clinical significance – not necessarily inclusive : Coma , convulsions , dizziness , severe , drowsiness , severe , fast or irregular heartbeat , fever , muscle ftiffness or weakness , severe , restlessness or agitation , trouble in breathing , vomiting .
Note :
Risk of seizures , respiratory complications , and cardiotoxicity is greater with maprotiline than with tricyclic antidepressants , and duration of comatose state and QRS complex is longer . ( USP DI 2005 )

Dosage and Administration :

Usual adult and adolescent does : Antidepressant – Initially 25 to 75 mg a day in divided doses , for at least two weeks, the dosage being adjusted gradually by 25 mg a day as needed and tolerated .
Note :
The effective maintenance dose is usually about 150 mg a day , often given once a day at bedtime . ( USP DI 2005 )

Usual adult prescribing limits :

Outpatients ; up to 150 mg a day , tlospitalized patients : up to 225 mg a day usual pediatric dose : children up to 18 years of age , safety and efficacy have not been established . ( USP DI 2005 )

Usual geriatric dose :

Initial : 25 mg a day .
Maintenance : 50 to 75 mg a day .
Storage : Store below 40°C , preferably between 15 and 30°C store in a well – closed container . ( USP DI 2005 )

How supplied :

Maprotiline 75 mg is available as red , oral scored , film-coated tablets in boxes of 100 . There are 10 blisters , each contains 10 tablets in a box . Maprotiline 25 mg is available as pink , oval , scored , film – coated tablets in boxes of 100 . There are 10 blisters , each contains 10 tablets in a box . ( USP DI 2005 )