Names and pronunciation
(im-ip′ra-meen) Impril , Novo-Pramine , Toframil
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Drug reference
(im-ip′ra-meen) Impril , Novo-Pramine , Toframil
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Func. class.: Antidepressant, tricyclic
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Chem. class.: Dibenzazepine, tertiary amine
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Do not confuse: imipramine/desipramine
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ACTION: Blocks reuptake of norepi- nephrine, serotonin into nerve endings, thereby increasing action of norepineph- rine, serotonin in nerve cells
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USES: Major depression, enuresis
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Unlabeled uses: Bulimia, neuropathic pain, panic disorder, ADHD, stress/urge incontinence, social phobia
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CONTRAINDICATIONS: Preg- nancy, hypersensitivity to this product or carBAMazepine; acute MI, MAOI therapy Precautions: Breastfeeding, geriatric patients, suicidal patients, severe depression, increased intraocular pressure, closed-angle glaucoma, uri- nary retention, cardiac/hepatic disease, hyperthyroidism, electroshock therapy, elective surgery, seizure disorders, prostatic hypertrophy, MI, AV block, bundle branch block, ileus, QT prolon- gation, hypersensitivity to tricyclics
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Black Box Warning: Children; suicidal ideation Black Box Warning: Depression: mood, behavior, sleep, lability; mental status, suicidal tendencies especially in children, young adults; increase in psychiatric symp- toms, panic, monitor weekly × 1 mo, then q3 wk, give limited amount of medication • CV: B/P (lying, standing), pulse; if systolic B/P drops 20 mm Hg, hold prod- uct, notify prescriber, monitor HR, rhythm, take ECG baseline in those with CV disease • Blood studies: CBC, leukocytes, differ- ential, cardiac enzymes, serum imipra- mine levels (125-250 ng/mL) if patient is receiving long-term therapy • Hepatic studies: AST, ALT, bilirubin • Weight weekly; appetite may increase with product • QT prolongation: monitor ECG for flat tening of T wave, bundle branch block, AV block, dysrhythmias in cardiac patients • EPS primarily in geriatric patients: ri- gidity, dystonia, akathisia I • Urinary retention, constipation; constipa- tion is more likely to occur in children, ge- riatric patients; increase fluids, bulk in diet • Withdrawal symptoms: headache, nausea, vomiting, muscle pain, weakness, diarrhea, insomnia, restlessness; not usu al unless product is discontinued abruptly • Serotonin syndrome, hypertensive ep- isodes, orthostatic hypotension: identify drug interactions before use of product • Alcohol consumption; if alcohol is consumed, hold dose until morning • Assistance with ambulation during beginning therapy because drowsiness, dizziness, orthostatic hypotension may occur • Safety measures, primarily for geriatric patients • Beers: avoid in older adults; highly anticholinergic, high risk of delirium, orthostatic hypotension Black Box Warning: To report suicidal thoughts, behaviors immediately; more common in children, young adults • Pregnancy/breastfeeding: Identify if pregnancy is planned or suspected or if breastfeeding
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SIDE EFFECTS CNS: Dizziness, drowsiness, confusion, seizures, headache, anxiety, insomnia, sui cidal ideation, paresthesia CV: Orthostatic hypotension, ECG changes, tachycardia, dysrhythmias EENT: Blurred vision, mydriasis, tinnitus ENDO: Hyperglycemia, hypo/hyperthy- roidism, SIADH GI: Diarrhea, dry mouth, nausea, vomit- ing, paralytic ileus, increased appetite, taste change GU: Retention, decreased libido HEMA: Agranulocytosis, thrombocytope nia, eosinophilia, leukopenia INTEG: Rash, urticaria, pruritus, photosensitivity
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INTERACTIONS • Increase: Hyperpyretic crisis, seizures, hypertensive episode: MAOIs, cloNIDine • Increase: serotonin syndrome, neuro leptic malignant syndrome—SSRIs, SN RIs, serotonin-receptor agonists, bupro pion, cyclobenzapine, trazadone, tramadil, tricyclics; avoid concurrent use, linezolid, methylene blue IV Increase: QT interval—class IA/III anti dysrhythmics, tricyclics, gatifloxacin, levoFLOXacin, moxifloxacin, ziprasidone Increase: effects of direct-acting sym pathomimetics (EPINEPHrine), alcohol, barbiturates, benzodiazepines, CNS depressants Decrease: effects of guanethidine, cloNI- Dine, indirect-acting sympathomimetics (ePHEDrine) Drug/Herb Increase: serotonin syndrome—SAM-e, St. John’s wort Increase: sedation—chamomile, kava, valerian Drug/Lab Test Increase: serum bilirubin, alk phos, blood glucose, LFTs Mental status: mood, sensorium, affect, suicidal tendencies especially in chil- dren, young adults; increase in psychiatric symptoms: depression, panic, monitor weekly × 1 mo, then 3 wk give limited amount of product
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TREATMENT OF OVERDOSE: ECG monitoring; lavage if recently ingested; sodium bicarbonate (cardiac effects); administer anticonvulsant, antidysrrthmics
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DOSAGE AND ROUTES Depression • Adult: PO 75-100 mg/day in divided doses, may increase by 25-50 mg to 200 mg/day (outpatients), 300 mg/day (inpatients); may give daily dose at bedtime • Adolescent/geriatric: PO 30-40 mg at bedtime, may increase to 100 mg/ day in divided doses • Child ≥6 yr (unlabeled): PO 1.5 mg/ kg/day in divided doses, max 2.5 mg/ kg/day Enuresis • Adolescents: PO 25 mg daily, 1 hr prior to bedtime, max 75 mg/day • Child 6-12 yr: PO 25 mg daily 1 hr prior to bedtime; max 50 mg/day
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Available forms: Tabs 10, 25, 50, 75 mg; caps 75, 100, 125, 150 mg
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Administer: PO route • Improvement may take 1-2 wk (sleep, energy); 1-4 wk (improved mood) 6-12 wk (optimal mood) • Not to break, crush, or chew caps • With food or milk for GI symptoms • Dosage at bedtime if oversedation oc- curs during day; may take entire dose at bedtime; geriatric patients may not toler- ate once-daily dosing • Sugarless gum, hard candy, or fre- quent sips of water for dry mouth • Do not discontinue abruptly, taper 50% × 3 days, another 50% × 3 days, then stop • Store in tight container at room tem- perature; do not freeze
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Assess:
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Evaluate: • Therapeutic response: decreased de- pression, enuresis
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That full therapeutic effects may take 2-3 wk • That product may be dispensed in small amounts because of suicide poten- tial, especially at beginning of therapy • To use caution when driving, perform- ing other activities requiring alertness because of drowsiness, dizziness, blurred vision • To report urinary retention immediately • To avoid alcohol, other CNS depres- sants during treatment • Not to discontinue medication abruptly after long-term use; may cause nausea, headache, malaise • To wear sunscreen or large hat be- cause photosensitivity occurs • To rise slowly, orthostatic hypotension may occur
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PHARMACOKINETICS Metabolized to desipramine in liver by CYP2D6; excreted in urine, breast milk, feces; crosses placenta; half-life 8-16 hr, protein binding 90%-95%
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• Adult: PO 75-100 mg/day in divided doses, may increase by 25-50 mg to 200 mg/day (outpatients), 300 mg/day (inpatients); may give daily dose at bedtime
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