Protriptyline Hydrochloride

Pronunciation: proe-TRIP-ti-leen HYE-droe-KLOR-ide
Class: Tricyclic compound

Trade Names

Vivactil
- Tablets 5 mg
- Tablets 10 mg

Pharmacology

Inhibits reuptake of norepinephrine and serotonin in CNS.

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Pharmacokinetics

Absorption

Well absorbed from GI tract and rapidly sequestered into tissues. T _max is 8 to 12 h. Steady state is 14 to 19 days.

Distribution

Widely distributed into tissues, including CNS. Penetrates into the brain rapidly. Small amounts are found in breast milk. Protein binding is 90% in plasma and tissues. Vd is 22 L/kg.

Metabolism

Metabolized in the liver by demethylation of secondary amine moiety.

Elimination

In the urine (small amounts unchanged). The t _½ is 67 to 89 h.

Onset

2 to 3 wk (antidepressant effect).

Indications and Usage

Relief of symptoms of mental depression in patients who are under close medical supervision.

Unlabeled Uses

Obstructive sleep apnea; panic disorder.

Contraindications

Hypersensitivity to tricyclic antidepressants; generally not to be given in combination with an MAOI or within 14 days of treatment with MAOIs; during acute recovery phase of MI; coadministration with cisapride.

Dosage and Administration

PO 15 to 60 mg/day in divided doses. The maintenance dose may be given as a single dose.

PO Initial dosage is 5 mg 3 times daily. Increase slowly if needed (max, 20 mg/day).

General Advice

• Administer without regard to meals; administer with food if GI upset occurs.

Storage/Stability

Store at 68° to 77°F in tightly closed, light-resistant container.

Drug Interactions

Risk of hyperpyrexia may be increased, especially during hot weather.

Increased protriptyline blood levels and effects.

Contraindicated in patients receiving tricyclic antidepressants.

Hypertensive crisis.

Additive depressant effects.

Protriptyline plasma levels may be elevated, increasing the risk of adverse reactions.

Inhibition of hypotensive action by guanethidine.

Death, hyperexcitability, hyperthermia, and seizures may occur.

Increased pressor response.

Decreased pressor response.

Risk of seizures may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Arrhythmias, CHF, ECG changes, heart block, hypertension, MI, orthostatic hypotension, palpitations, stroke, tachycardia.

CNS

Agitation, anxiety, ataxia, confusion, delusions, disorientation, dizziness, drowsiness, emotional lability, exacerbation of psychosis, extrapyramidal symptoms, fatigue, hallucinations, headache, incoordination, increased and decreased libido, insomnia, mania, nervousness, nightmares, numbness, panic, paresthesia, peripheral neuropathy, restlessness, seizures, stinging, tremors, weakness.

Dermatologic

Acne, alopecia, dry skin, flushing, itching, perspiration, petechiae, photosensitivity reaction, pruritus, rash, urticaria.

EENT

Blurred vision, increased IOP, mydriasis, peculiar taste, tinnitus.

GI

Abdominal cramps, anorexia, black tongue, constipation, diarrhea, dry mouth, flatulence, GI distress, nausea, paralytic ileus, peculiar taste, stomatitis, vomiting.

Genitourinary

Amenorrhea, breast enlargement and galactorrhea in women, dilatation of the urinary tract, dysmenorrhea, gynecomastia in men, impotence, nocturia, sexual dysfunction, testicular swelling, urinary frequency, urinary retention and hesitancy.

Hematologic

Bone marrow depression (including agranulocytosis), eosinophilia, leukopenia, purpura, thrombocytopenia.

Hepatic

Altered LFTs, jaundice.

Metabolic-Nutritional

Edema, elevation or depression of blood glucose, SIADH, weight gain or loss.

Respiratory

Cough, laryngitis, pharyngitis, rhinitis, sinusitis.

Miscellaneous

Drug fever, hyperpyrexia, parotid swelling.

Precautions

Pregnancy

Undetermined.

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Special Risk Patients

Use with caution in patients with history of seizures, urinary retention, urethral or ureteral spasm, angle-closure glaucoma or increased IOP, CV disorders, hyperthyroidism or those receiving thyroid medication, hepatic or renal function impairment, or schizophrenia or paranoia.

Anticholinergic effects

Additive with other medications with anticholinergic effects.

Schizophrenia

Psychotic symptoms may be aggravated.

Suicide

Observe adults and children treated with antidepressants for clinical worsening, suicidality, and unusual changes in behavior. Prescribe the smallest quantity consistent with good patient management to reduce the risk of overdose.

Tachycardia/Postural hypotension

May occur more frequently with protriptyline.

Overdosage

Symptoms

Cardiac arrhythmias, CNS stimulation (eg, agitation, delirium, irritability) followed by depression (eg, drowsiness to coma), hyperpyrexia followed by hypothermia, hypertension followed by hypotension, seizures.

Patient Information

• Advise patient to read the Medication Guide before using product the first time and with each refill.
• Explain that therapeutic effect of drug may be seen within 2 to 5 days, but full effectiveness of drug may not occur for 2 to 3 wk.
• Tell patient that dosage will be tapered slowly before stopping to prevent withdrawal symptoms.
• Warn patient to monitor food intake; weight gain can occur because of increased appetite.
• Instruct patient to report the following symptoms to health care provider: mental status changes (especially increase in depression or panic); urinary retention and extrapyramidal symptoms (frequently noted in elderly patients), such as rigidity or fine hand tremors; or visual disturbances.
• Advise patient and caregiver to be alert for abnormal changes in mood or thinking. The following symptoms should be reported immediately to the health care provider: agitation, anxiety, hostility or aggression, impulsivity, irritability, panic attacks, suicidal thoughts and behavior.
• Advise patient to take sips of water frequently, to suck on ice chips or sugarless hard candy, or chew sugarless gum to relieve dry mouth.
• Caution patient to avoid sudden position changes to avoid dizziness.
• Instruct patient to avoid alcoholic beverages or other CNS depressants while taking this medicine.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing other activities requiring mental alertness.
• Caution patient to avoid exposure to sunlight and to use sunscreen or wear protective clothing to avoid photosensitivity reaction.

Copyright © 2009 Wolters Kluwer Health.