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Trazodone


Category :

Antidepressant, antineuralgic. ( USP DI 2004)

Composition :

Each scored film coated tablet contains 50 mg of trazodone hydrochloride .

Chemistry :

Trazodone Hydrochloride is an antidepressant chemically unrelated to tricyclic , tetracyclic , or other known antidepressant agents.
Molecular weight: 408.3

Mechanism of Action :

Not completely established in humans Animal studies indicate that trazodone selectively inhibits serotonin re – uptake in the brain, causes beta – receptor subsensitivity , and induces significant changes in serotonin – receptor binding with only a slight effect on alpha – adrenergic receptors . Also , trazodone potentiates the behavioral changes in animals induced by 5 – hydroxytryptophan, a serotonin precursor. ( USP DI 2004 )

Absorption :

Well absorbed . When trazodone is taken with or shortly after ingestion of food , there may be an increase in the amount of drug absorbed , a decrease in maximum concentration and a lengthening of time to reach peak concentration .

Protein binding :

Very high ( 89 to 95% )

Biotransformation :

Hepatic : extensive , by hydroxylation .

Half – Life :

Biphasic More rapid, 3 to 6 hours : slower, 5 to 9 hours .

Onset of therapeutic action :

In clinical trials . Significant therapeutic results occurred after 2 weeks of therapy in 75% of the patients responsive to the medication . With some patients showing definite improvement after 1 week of therapy ; 25% of the responding patients required 2 to 4 weeks of therapy before noticeable improvement occurred. ( USP DI 2004 )

Time to peak concentration :

Fasting , 1 hour , with food, 2 hours .

Elimination :

Biliary -
20%
Renal –
75% , mostly as inactive metabolites .

Indications :

Depression , mental ( treatment ) - Trazodone is indicated in the treat ment of major depressive episodes with or without prominent anxiety . [ pain , Neurogenic ( treatment ) ]– Trazodone has been used to treat painful diabetic neuropathy and other types of chronic pain. ( USP DI 2004 )

Contraindications :

Trazodone is contraindicated in patients hypersensitive to trazodone.

Warnings :

Trazodone has been associated with the occurrence of priapism . In many of the cases reported , surgical intervention was required and in some of these cases, permanent impairment of erectile function or impotence resulted. Male patients with prolonged or inappropriate erections should immediately discontinue the drug and consult their physician.
  • Trazodone Hydrochloride is not recommended for use during the initial recovery phase of myocardial infarction .
  • Caution should be used when administering trazodone to patients with cardiac disease , and such patients should be closely monitored , since antidepressant drugs ( including trazodone ) have been associated with the occurrence of cardiac arrhythmias . Recent clinical studies in patients with pre – existing cardiac disease indicate that trazodone may be arrhythmogenic in some patients in that population.

Pregnancy :

Pregnancy category C. There are no adequate and well – controlled studies in pregnant women . Trazodone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers :

Trazodone and /or its metabolites have been found in the milk of lactating rats , suggesting that the drug may be secreted in human milk. Caution should be exercised when trazodone is administered to a nursing woman.

Precautions :

The possibility of suicide in seriously depressed patients is inherent in the illness and may persist until significant remission occurs. Therefore , prescriptions should be written for the smallest number of tablets consistent with good patient management .
Hypotension , including orthostatic hypotension and syncope , has been reported to occur in patients receiving trazodone. Concomitant administration of antihypertensive therapy with trazodone may require a reduction in the dose of the antihypertensive drug. Little is known about the interaction between trazodone and general anesthetics ; therefore, prior to elective surgery, trazodone should be discontinued for as long as clinically feasible .
As with all antidepressants, the use of trazodone should be based on the consideration of the physician that the expected benefits of therapy outweigh potential risk factors.
Pediatric Use :
Safety and effectiveness in children below the age of 18 have not been established .

Drug Interactions :

Increased serum digoxin or phenytoin levels have been reported to occur in patients receiving trazodone concurrently with either of those two drugs. It is not known whether interactions will occur between monoamine oxidase ( MAO ) inhibitors and trazodone .
Due to the absence of clinical experience, if MAO inhibitors are discontinued shortly before or are to be given concomitantly with trazodone , therapy should be initiated cautiously with gradual increase in dosage until optimum response is achieved . Concurrent administration with electroshock therapy should be avoided because of the absence of experience in this area. There have been reports of increased and decreased prothrombin time occurring in warfarinized patients who take trazodone .

Adverse Reactions :

Allergic reactions (skin condition edema ),Autonomic (blurred vision , constipation , dry mouth ) . Cardiovascular ( hypotension ) , CNS (confusion , dizziness, drowsiness, fatigue, headache , nervousness ) . Gastrontestinal ( bad taste in mouth , nausea/ vomiting ) . Musculoskeletal ( musculoskeletal aches ) . Neurological ( incoordination , tremor ) , Sexual function ( decreased libido ) .

Dosage and Administration :

Usual adult and adolescent dose : Antiepressant – initially 150 mg a day in divided doses, the dosage being increased by 50 mg per day at three – or four – day intervals , as needed and tolerated .
Usual adult prescribing limits : Outpatients : Up to 400 mg a day .
Inpatients : Up to 600 mg a day .
Usual geriatric dose : Antidepressant – initially 75 mg a day in divided doses , the dosage being increased gradually at three – or four – day intervals, as needed and tolerated .

Missed Dose :

Taking as soon as possible , not taking within 4 hours of next scheduled dose , not doubling doses .

Storage :

Store below 30° C in a dry place . Protect from light .

How Supplied :

Trazodone 50 mg is available as red , round , scored , film coated tablets in boxes of 100 . There are 10 blisters each contains 10 tablets in a box.

Refrences :

1 ) USP DI 2004
2 ) PDR 2005
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