DESIPRAMINE HYDROCHLORIDE

DESIPRAMINE HYDROCHLORIDE
(dess-ip'ra-meen)
Norpramin, Pertofrane
Classifications: psychotherapeutic; tricyclic antidepressant;
Therapeutic:tricyclic antidepressant
Prototype: Imipramine
Pregnancy Category: C

Availability

10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg tablets

Action

Desipramine is a tricyclic antidepressant (TCA) and the active metabolite of imipramine. Antidepressant activity appears to be related to blocking reuptake of norepinephrine and serotonin in the CNS, thus increasing their levels. A more recent theory of antidepressant action of the drug is thought to be a restoration of the balance of monoamine output.

Therapeutic Effect

In common with other TCAs, it has antidepressant activity.

Uses

Endogenous depression and various depression syndromes.

Unlabeled Uses

Attention deficit disorder in children >6 y and adolescents; to prevent depression in cocaine withdrawal.

Contraindications

Hypersensitivity to tricyclic compounds; recent MI, QT prolongation, cardiac arrhythmias, AV block, bundle branch block; concurrent use of MAOI therapy; suicidal ideation; pregnancy (category C), lactation. Safe use in children <6 y is not established.

Cautious Use

Urinary retention, prostatic hypertrophy; narrow-angle glaucoma; epilepsy; alcoholism; adolescents, older adults; bipolar disease; thyroid; cardiovascular, renal, and hepatic disease; suicidal tendency; ECT; elective surgery.

Route & Dosage

Antidepressant
Adult: PO 75–100 mg/d at bedtime or in divided doses, may gradually increase to 150–300 mg/d (use lower doses in older adult patients)
Adolescent: PO 25–50 mg/d (max: 100 mg/d) in divided doses
Child (6–12 y): PO 1–3 mg/kg/d in divided doses (max: 5 mg/kg/d)

Administration

Oral

Give drug with or immediately after food to reduce possibility of gastric irritation.
Give maintenance dose at bedtime to minimize daytime sedation.
Store drug in tightly closed container at 15°–30° C (59°–86° F) unless otherwise specified.

Adverse Effects (≥1%)

Body as a Whole: Hypersensitivity (rash, urticaria, photosensitivity). CNS: Drowsiness, dizziness, weakness, fatigue, headache, insomnia, confusional states, depressive reaction, paresthesias, ataxia. CV: Postural hypotension, hypotension, palpitation, tachycardia, ECG changes, flushing, heart block. Special Senses: Tinnitus, parotid swelling; blurred vision, disturbances in accommodation, mydriasis, increased IOP. GI: Dry mouth, constipation, bad taste, diarrhea, nausea. Urogenital: Urinary retention, frequency, delayed micturition, nocturia; impaired sexual function, galactorrhea. Hematologic: Bone marrow depression and agranulocytosis (rare). Other: Sweating, craving for sweets, weight gain or loss, SIADH secretion, hyperpyrexia, eosinophilic pneumonia.

Interactions

Drug: May somewhat decrease response to antihypertensives; cns depressants, alcohol, hypnotics, barbiturates, sedatives potentiate CNS depression; may increase hypoprothombinemic effect of oral anticoagulants; ethchlorvynol may cause transient delirium; levodopa, sympathomimetics (e.g., epinephrine, norepinephrine) pose possibility of sympathetic hyperactivity with hypertension and hyperpyrexia; mao inhibitors pose possibility of severe reactions, toxic psychosis, cardiovascular instability; methylphenidate increases plasma TCA levels; thyroid agents may increase possibility of arrhythmias; cimetidine may increase plasma TCA levels. Herbal: Ginkgo may decrease seizure threshold; St. John's wort may cause serotonin syndrome.

Pharmacokinetics

Absorption: Rapidly absorbed from GI tract and injection sites. Peak: 4–6 h. Distribution: Crosses placenta. Metabolism: In liver. Elimination: Primarily in urine. Half-Life: 7–60 h.

Nursing Implications

Assessment & Drug Effects

Monitor children and adolescents for signs of suicidal ideation.
Monitor for therapeutic effectiveness: Usually not realized until after at least 2 wk of therapy.
Monitor BP and pulse rate during early phase of therapy, particularly in older adult, debilitated, or cardiovascular patients. If BP rises or falls more than 20 mm Hg or if there is a sudden increase in pulse rate or change in rhythm, withhold drug and inform physician.
Note: Drowsiness, dizziness, and orthostatic hypotension are signs of impending toxicity in patient on long-term, high dosage therapy. Prolonged QT or QRS intervals indicate possible toxicity. Report to physician.
Observe patient with history of glaucoma. Report symptoms that may signal acute attack: Severe headache, eye pain, dilated pupils, halos of light, nausea, vomiting.
Monitor bowel elimination pattern and I&O ratio. Severe constipation and urinary retention are potential problems of TCA therapy.
Note: Norpramin tablets may contain tartrazine, which can cause allergic-type reactions including bronchial asthma in susceptible individuals. Such individuals are frequently also sensitive to aspirin.

Patient & Family Education

Make all position changes slowly and in stages, particularly from recumbent to standing position.
Do not drive or engage in other potentially hazardous activities until reaction to drug is known.
Take medication exactly as prescribed; do not change dose or dose intervals.
Note: Patients who receive high doses for prolonged periods may experience withdrawal symptoms including headache, nausea, musculoskeletal pain, and weakness if drug is discontinued abruptly.
Do not take OTC drugs unless physician has approved their use.
Stop, or at least limit, smoking because it may increase the metabolism of desipramine, thereby diminishing its therapeutic action.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

(25)