Indications and Usage
Protriptyline hydrochloride tablets are indicated for the treatment of symptoms of mental depression in patients who are under close medical supervision. Its activating properties make it particularly suitable for withdrawn and anergic patients.
Dosage and Administration
Dosage should be initiated at a low level and increased gradually, noting carefully the clinical response and any evidence of intolerance.
Usual Adult Dosage
Fifteen to 40 mg a day divided into 3 or 4 doses. If necessary, dosage may be increased to 60 mg a day. Dosages above this amount are not recommended. Increases should be made in the morning dose.
Adolescent and Elderly Patients
In general, lower dosages are recommended for these patients. Five mg 3 times a day may be given initially, and increased gradually if necessary. In elderly patients, the cardiovascular system must be monitored closely if the daily dose exceeds 20 mg.
When satisfactory improvement has been reached, dosage should be reduced to the smallest amount that will maintain relief of symptoms.
Minor adverse reactions require reduction in dosage. Major adverse reactions or evidence of hypersensitivity require prompt discontinuation of the drug.
The safety and effectiveness of protriptyline in pediatric patients have not been established.
Contraindications
Protriptyline hydrochloride tablets are contraindicated in patients who have shown prior hypersensitivity to it.
It should not be given concomitantly with a monoamine oxidase inhibiting compound. Hyperpyretic crises, severe convulsions, and deaths have occurred in patients receiving tricyclic antidepressant and monoamine oxidase inhibiting drugs simultaneously. When it is desired to substitute protriptyline for a monoamine oxidase inhibitor, a minimum of 14 days should be allowed to elapse after the latter is discontinued. Protriptyline should then be initiated cautiously with gradual increase in dosage until optimum response is achieved.
Protriptyline is contraindicated in patients taking cisapride because of the possibility of adverse cardiac interactions including prolongation of the QT interval, cardiac arrhythmias and conduction system disturbances.
This drug should not be used during the acute recovery phase following myocardial infarction.
Adverse Reactions
To report SUSPECTED ADVERSE REACTIONS, contact Epic Pharma, LLC at 1-888-374-2791, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Within each category the following adverse reactions are listed in order of decreasing severity. Included in the listing are a few adverse reactions which have not been reported with this specific drug. However, the pharmacological similarities among the tricyclic antidepressant drugs require that each of the reactions be considered when protriptyline is administered. Protriptyline is more likely to aggravate agitation and anxiety and produce cardiovascular reactions such as tachycardia and hypotension.
Cardiovascular:
Myocardial infarction; stroke; heart block; arrhythmias; hypotension, particularly orthostatic hypotension; hypertension; tachycardia; palpitation.
Psychiatric:
Confusional states (especially in the elderly) with hallucinations, disorientation, delusions, anxiety, restlessness, agitation; hypomania; exacerbation of psychosis; insomnia, panic, and nightmares.
Neurological:
Seizures; incoordination; ataxia; tremors; peripheral neuropathy; numbness, tingling, and paresthesias of extremities; extrapyramidal symptoms; drowsiness; dizziness; weakness and fatigue; headache; syndrome of inappropriate ADH (antidiuretic hormone) secretion; tinnitus; alteration in EEG patterns.
Anticholinergic
Paralytic ileus; hyperpyrexia; urinary retention, delayed micturition, dilatation of the urinary tract; constipation; blurred vision, disturbance of accommodation, increased intraocular pressure, mydriasis; dry mouth and rarely associated sublingual adenitis.
Allergic
Drug fever; petechiae, skin rash, urticaria, itching, photosensitization (avoid excessive exposure to sunlight); edema (general, or of face and tongue).
Hematologic:
Agranulocytosis; bone marrow depression; leukopenia; thrombocytopenia; purpura; eosinophilia.
Gastrointestinal:
Nausea and vomiting; anorexia; epigastric distress; diarrhea; peculiar taste; stomatitis; abdominal cramps; black tongue.
Endocrine:
Impotence, increased or decreased libido; gynecomastia in the male; breast enlargement and galactorrhea in the female; testicular swelling; elevation or depression of blood sugar levels.
Other:
Jaundice (simulating obstructive); altered liver function; parotid swelling; alopecia; flushing; weight gain or loss; urinary frequency, nocturia; perspiration.
Withdrawal Symptoms:
Though not indicative of addiction, abrupt cessation of treatment after prolonged therapy may produce nausea, headache, and malaise.
Drug Interactions
When protriptyline is given with anticholinergic agents or sympathomimetic drugs, including epinephrine combined with local anesthetics, close supervision and careful adjustment of dosages are required.
Hyperpyrexia has been reported when tricyclic antidepressants are administered with anticholinergic agents or with neuroleptic drugs, particularly during hot weather.
Cimetidine is reported to reduce hepatic metabolism of certain tricyclic antidepressants, thereby delaying elimination and increasing steady-state concentrations of these drugs. Clinically significant effects have been reported with the tricyclic antidepressants when used concomitantly with cimetidine. Increases in plasma levels of tricyclic antidepressants, and in the frequency and severity of side-effects, particularly anticholinergic, have been reported when cimetidine was added to the drug regimen. Discontinuation of cimetidine in well-controlled patients receiving tricyclic antidepressants and cimetidine may decrease the plasma levels and efficacy of the antidepressants.
Tricyclic antidepressants may enhance the seizure risk in patients taking ULTRAM (tramadol hydrochloride).
Protriptyline may enhance the response to alcohol and the effects of barbiturates and other CNS depressants.
Overdosage
Deaths may occur from overdosage with this class of drugs. Multiple drug ingestion (including alcohol) is common in deliberate tricyclic antidepressant overdose. As management of overdose is complex and changing, it is recommended that the physician contact a poison control center for current information on treatment. Signs and symptoms of toxicity develop rapidly after tricyclic antidepressant overdose, therefore, hospital monitoring is required as soon as possible.
Description
Protriptyline HCl is N-methyl-5H dibenzo[a,d]-cycloheptene-5-propanamine hydrochloride. Its molecular formula is C19H21N•HCl and its structural formula is:
Protriptyline HCl, a dibenzocycloheptene derivative, has a molecular weight of 299.84. It is a white to yellowish powder that is freely soluble in water and soluble in dilute HCl. Protriptyline HCl is supplied as 5 mg or 10 mg film-coated tablets. Inactive ingredients are microcrystalline cellulose, pregelatinized starch, lactose monohydrate, dibasic calcium phosphate, sodium starch glycolate, magnesium stearate, hypromellose, triacetin, polysorbate, titanium dioxide and FD & C yellow 6 aluminum lake. The 10 mg tablet also contains polyethylene glycol and polysorbate 80.
structural formulaClinical Pharmacology
Protriptyline hydrochloride is an antidepressant agent. The mechanism of its antidepressant action in man is not known. It is not a monoamine oxidase inhibitor, and it does not act primarily by stimulation of the central nervous system.
Protriptyline has been found in some studies to have a more rapid onset of action than imipramine or amitriptyline. The initial clinical effect may occur within one week. Sedative and tranquilizing properties are lacking. The rate of excretion is slow.
How Supplied / Storage and Handling
Protriptyline Hydrochloride Tablets USP, 5 mg are dark orange, round biconvex, film coated tablets, de-bossed “Є96” on one side, and plain on the other side, available in bottles of 30 (NDC: 42806-096-30), in bottles of 100 (NDC: 42806-096-01) and in bottles of 1000 (NDC: 42806-096-10).
Protriptyline Hydrochloride Tablets USP, 10 mg are light orange, round biconvex, film coated tablets, de-bossed “Є97” on one side, and plain on the other side, available in bottles of 30 (NDC: 42806-097-30), in bottles of 100 (NDC: 42806-097-01) and in bottles of 1000 (NDC: 42806-097-10).
Dispense in a tight container as defined in the USP.
Store at 20°-25°C (68°-77°F) [See USP Controlled Room Temperature].
Patient Counseling Information
Prescribers or other health professionals should inform patients, their families and their caregivers about the benefits and risks associated with treatment with protriptyline hydrochloride and should counsel them in its appropriate use. A patient Medication Guide about “Antidepressant Medicines, Depression and other Serious Mental Illness, and Suicidal Thoughts or Actions” is available for protriptyline hydrochloride. The prescriber or health professional should instruct patients, their families, and their caregivers to read the Medication Guide and should assist them in understanding its contents. Patients should be given the opportunity to discuss the contents of the Medication Guide and to obtain answers to any questions they may have. The complete text of the Medication Guide is reprinted at the end of this document.
Patients should be advised of the following issues and asked to alert their prescriber if these occur while taking protriptyline hydrochloride.
Patients should be advised that taking protriptyline hydrochloride tablets can cause mild pupillary dilation, which in susceptible individuals, can lead to an episode of angle-closure glaucoma. Pre-existing glaucoma is almost always open-angle glaucoma because angle-closure glaucoma, when diagnosed, can be treated definitively with iridectomy. Open angle glaucoma is not a risk factor for angle closure glaucoma. Patients may wish to be examined to determine whether they are susceptible to angle closure, and have a prophylactic procedure (e.g., iridectomy), if they are susceptible.