Desyrel (Trazodone HCl)



Trazodone HCl


Action And Clinical Pharmacology: Trazodone is a psychoactive compound with sedative and antidepressant properties. Its mechanism of action in humans is not clear.

Trazodone is well absorbed after oral administration with peak plasma levels obtained within 0.5 to 2 hours after ingestion. Absorption is somewhat delayed and enhanced by food. The mean plasma elimination half-life is 4.4 hours for the period from 3 to 10 hours after dosing, and 7 to 8 hours for the period from 10 to 34 hours. The drug is extensively metabolized with 3 or 4 major metabolites having been identified in man. Approximately 60 to 70% of C14-labelled trazodone was found to be excreted in the urine within 2 days and 9 to 29% in feces over 60 to 100 hours. Trazodone is 89 to 95% protein bound in vitro at concentrations attained with therapeutic doses.

Indications And Clinical Uses: For the symptomatic relief of depressive illness.

Contra-Indications: Known hypersensitivity to trazodone.

Manufacturers’ Warnings In Clinical States: Trazodone has been associated with the occurrence of priapism. In approximately 33% of the cases reported, surgical intervention was required and, in a portion 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. If the condition persists for more than 24 hours, it would be advisable for the treating physician to consult a urologist or appropriate specialist in order to decide on a management approach. Recent clinical studies in patients with pre-existing cardiac disease indicate that trazodone may be arrhythmogenic in some patients in that population. Arrhythmias identified include isolated PVCs, ventricular couplets, and in 2 patients short episodes (3 to 4 beats) of ventricular tachycardia. There have also been several post-marketing reports of arrhythmias in trazodone-treated patients who have pre-existing cardiac disease and in some patients who did not have pre-existing cardiac disease. Until the results of prospective studies are available, patients with pre-existing cardiac disease should be closely monitored, particularly for cardiac arrhythmias. Trazodone is not recommended for use during the initial recovery phase of myocardial infarction.

Precautions: The possibility of suicide in depressed patients remains during treatment and until significant remission occurs. Therefore, the number of tablets prescribed at any one time should take into account this possibility, and patients with suicide ideation should never have access to large quantities of trazodone.

Episodes of grand mal seizures have been reported in a small number of patients. The majority of these patients were already receiving anticonvulsant therapy for a previously diagnosed seizure disorder.

Occupational Hazards: Since trazodone may impair the mental and/or physical abilities required for performance of potentially hazardous tasks, such as operating an automobile or machinery, the patient should be cautioned not to engage in such activities while impaired.

Drug Interactions: Trazodone may enhance the response to alcohol and the effects of barbiturates and other CNS depressants and patients should be cautioned accordingly.

Increased serum digoxin and phenytoin levels have been reported to occur in patients receiving trazodone concurrently with either of those 2 drugs. 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.

Because it is not known whether an interaction will occur between trazodone and MAO inhibitors, administration of trazodone should be initiated very cautiously with gradual increase in dosage as required, if an MAO inhibitor is given concomitantly or has been discontinued shortly before medication with trazodone is instituted.

Trazodone may cause hypotension including orthostatic hypotension and syncope; caution is required if it is given to patients receiving antihypertensive drugs and an adjustment in the dose of the antihypertensive medication may be required.

Because of the absence of experience, concurrent administration of electro-shock therapy should be avoided.

Pregnancy and Lactation: Since the safety and use of trazodone in pregnant women has not been established, it should not be used in women of childbearing potential unless, in the opinion of the physician, the expected benefits justify the potential risk to the fetus. Since trazodone and/or its metabolites have been detected in the milk of lactating animals, it should not be administered to nursing mothers unless the potential benefits justify the possible risks to the child.

Children: The safety and effectiveness of trazodone in children below the age of 18 have not been established.

Laboratory Tests: It is recommended that white blood cell and differential counts should be performed in patients who develop sore throat, fever, or other signs of infection or blood dyscrasia and trazodone should be discontinued if the white blood cell or absolute neutrophil count falls below normal.

Hyperprolactinemia and Breast Tumors: There is sufficient experimental evidence to conclude that chronic administration of those psychotropic drugs, such as trazodone, which increase prolactin secretion has the potential to induce mammary neoplasms in rodents under appropriate conditions. Tissue culture experiments indicate that approximately 33% of human breast cancers are prolactin dependent in vitro, a factor of potential importance if the prescription of these drugs is contemplated in a patient with a previously detected breast cancer. Although disturbances such as galactorrhea, amenorrhea, gynecomastia and impotence have been reported, the clinical significance of elevated serum prolactin levels or increased secretion and turnover are unknown for most patients. Neither clinical studies nor epidemiological studies conducted to date, however, have shown an association between administration of these drugs and mammary tumorigenesis: available evidence is considered too limited to be conclusive at this time.

Adverse Reactions: The most common adverse reactions encountered are drowsiness, nausea/vomiting, headache and dry mouth. Adverse reactions reported include the following: Behavioral: drowsiness, fatigue, lethargy, retardation, lightheadedness, dizziness, difficulty in concentration, confusion, impaired memory, disorientation, excitement, agitation, anxiety, tension, nervousness, restlessness, insomnia, nightmares, anger, hostility and, rarely, hypomania, visual distortions, hallucinations, delusions and paranoia.

Neurologic: tremor, headache, ataxia, akathisia, muscle stiffness, slurred speech, retarded speech, vertigo, tinnitus, tingling of extremities, paresthesia, weakness, grand mal seizures (see Precautions), and, rarely impaired speech, muscle twitching, numbness, dystonia and involuntary movements.

Autonomic: dry mouth, blurred vision, diplopia, miosis, nasal congestion, constipation, sweating, urinary retention, increased urinary frequency and incontinence.

Cardiovascular: orthostatic hypotension, hypertension, tachycardia, palpitations, shortness of breath, apnea, syncope, arrhythmias, prolonged P-R interval, atrial fibrillation, bradycardia, ventricular ectopic activity (including ventricular tachycardia), myocardial infarction and cardiac arrest.

Gastrointestinal: nausea, vomiting, diarrhea, gastrointestinal discomfort, anorexia, increased appetite.

Endocrine: priapism (see Warnings), decrease and, more rarely, increase in libido, weight gain and loss, and rarely, menstrual irregularities, retrograde ejaculation and inhibition of ejaculation.

Allergic or Toxic: skin rash, itching, edema, and, rarely, hemolytic anemia, methemoglobinemia, liver enzyme alterations, obstructive jaundice, leukocytoblastic vasculitis, purpuric maculopapular eruptions, photosensitivity and fever.

Miscellaneous: aching joints and muscles, peculiar taste, hypersalivation, chest pain, hematuria, red, tired and itchy eyes.

Symptoms And Treatment Of Overdose: Symptoms: Overdosage of trazodone may cause an increase in incidence or severity of any of the reported adverse reactions, e.g. hypotension and excessive sedation. In one known suicide attempt, the patient presented with symptoms of drowsiness and weakness 3 hours after ingesting 7.5 g (12.5 times the maximum daily dose) of trazodone. Recovery was uneventful. Death by deliberate or accidental overdosage has not been reported.

Treatment: There is no specific antidote for trazodone. Management of overdosage should, therefore, be symptomatic and supportive. Any patient suspected of having taken an overdosage should be admitted to hospital as soon as possible and the stomach emptied by gastric lavage. Forced diuresis may be useful in facilitating elimination of the drug.

Dosage And Administration: Dosage should be initiated at a low level and increased gradually noting carefully the clinical response and any evidence of intolerance. It should be kept in mind that there may be a lag in the therapeutic response. Increasing the dosage rapidly does not normally shorten this latent period and may increase the incidence of side effects.

Usual Adult Dosage: The recommended initial dose is 150 to 200 mg daily, in 2 or 3 divided doses. Trazodone should be taken shortly after a meal or light snack in order to reduce the incidence of adverse reactions. The initial dose may be increased according to tolerance and response by increments of 50 mg, usually up to 300 mg daily in divided doses. In some patients, doses up to 400 mg daily and rarely up to 600 mg daily in hospitalized patients, may be required. Occurrence of drowsiness may require the administration of a major portion of the daily dose at bedtime or a reduction of dosage. Once an adequate response has been achieved, the dosage may be gradually reduced, with adjustment depending on therapeutic response. During prolonged maintenance therapy the dosage should be kept at the lowest effective level.

Geriatrics: If used in the elderly, doses not exceeding one-half the recommended adult dosage should be used, with adjustments made depending on tolerance and response.

Because safety and effectiveness in children have not been established trazodone is not recommended in the pediatric age group.

Availability And Storage: Desyrel: 50 mg: Each orange, round, scored tablet contains: trazodone hydrochloride 50 mg. Nonmedicinal ingredients: cornstarch, dibasic calcium phosphate, FD&C yellow No. 6 aluminum lake, lactose, magnesium stearate, microcrystalline cellulose, povidone and sodium starch glycolate. May or may not contain castor oil and ethylcellulose. Bottles of 100 and 250.

100 mg: Each white, round, film-sealed, scored tablet contains: trazodone hydrochloride 100 mg. Nonmedicinal ingredients: cornstarch, dibasic calcium phosphate, lactose, magnesium stearate, microcrystalline cellulose, povidone and sodium starch glycolate. May or may not contain castor oil and ethylcellulose. Bottles of 100.

Desyrel Dividose: Each orange rectangular-shaped, trisected and bisected tablet contains: trazodone hydrochloride 150 mg. Nonmedicinal ingredients: FD&C yellow No. 6 aluminum lake, magnesium stearate, microcrystalline cellulose, pregelatinized starch and stearic acid. Each tablet can be broken accurately to provide any of the following dosages: 50 mg (1/3 of a tablet), 75 mg (1/2 of a tablet), 100 mg (2/3 of a tablet), 150 mg (entire tablet). To break a Dividose tablet accurately and easily, hold the tablet between your thumbs and index fingers, close to the appropriate score (groove). Then with the tablet score facing you, apply pressure and snap the tablet segments apart. Bottles of 100. (Shown in Product Recognition Section)

DESYREL® DESYREL® DIVIDOSE Bristol Trazodone HCl Antidepressant

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