Names and pronunciation
(tray′zoe-done) Desyrel
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Drug reference
(tray′zoe-done) Desyrel
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Func. class.: Antidepressant— miscellaneous
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Chem. class.: Triazolopyridine
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Do not confuse: traZODone/traMADol
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ACTION: Selectively inhibits serotonin uptake by brain; potentiates behavorial changes
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USES: Major depressive disorder (unipolar)
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Unlabeled uses: Aggressive or agitated T behavior associated with dementia, insomnia
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CONTRAINDICATIONS: Hyper- sensitivity to tricyclics Precautions: Pregnancy, suicidal patients, severe depression, increased intraocular pressure, closed-angle glau- coma, urinary retention, cardiac/hepatic disease, hyperthyroidism, electroshock therapy, elective surgery, bleeding, abrupt discontinuation, bipolar disorder, breastfeeding, dehydration, hyponatre- mia, hypovolemia, recovery phase of MI, seizure disorders, prostatic hypertrophy, family history of long QT
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Black Box Warning: Suicidal ideation in children/adolescents Black Box Warning: Mental status changes: mood, sensorium, affect, sui- cidal tendencies, increase in psychiatric symptoms, depression, panic; observe for suicidal behaviors in children/adoles- cents, not approved for children; if wors- ening depression occurs, product may need to be tapered as rapidly as possible, without abrupt discontinuation • Urinary retention, constipation; consti- pation most likely in children • Alcohol consumption; hold dose until morning • Serotonin syndrome, neuroleptic malignant syndrome: increased heart rate, shivering, sweating, dilated pupils, tremors, high B/P, hyperthermia, headache, confusion; if these occur, stop product, ad minister serotonin antagonist if needed • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; no well-con trolled studies; cautious use in breast feeding, excreted in breast milk Black Box Warning: That suicidal thoughts/behaviors may occur (adolescents/ children); to notify health care professional if there is an increase in depression, agitation • To notify prescriber if pregnancy is planned or suspected; to avoid breast feeding • To rise slowly to prevent dizziness
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SIDE EFFECTS CNS: Dizziness, drowsiness, confusion, headache, anxiety, tremors, stimulation, weakness, insomnia, nightmares, EPS (geriatric patients), increase in psychiat- ric symptoms, suicide in children/ adolescents CV: Orthostatic hypotension, ECG changes, tachycardia, hypertension, palpitations EENT: Blurred vision, tinnitus, mydriasis GI: Diarrhea, dry mouth, nausea, vomit- ing, paralytic ileus, increased appetite, cramps, epigastric distress, jaundice, hepatitis, stomatitis, constipation GU: Urinary retention, acute renal fail ure, priapism HEMA: Agranulocytosis, thrombocytope nia, eosinophilia, leukopenia INTEG: Rash, urticaria, sweating, pruri- tus, photosensitivity
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INTERACTIONS Hyperpyretic crisis, seizures, hyper- tensive episode: MAOIs; do not use within 14 days of traZODone Increase: toxicity, serotonin syndrome— FLUoxetine, nefazodone, other SSRIs, SNRIs, linezolid; methylene blue (IV) Increase: effects of direct-acting sympa- thomimetics (EPINEPHrine), alcohol, barbiturates, benzodiazepines, CNS depressants, digoxin, phenytoin, carBA- Mazepine, traMADol Increase: effects of traZODone—CYP3A4, 2D6 inhibitors (phenothiazines, protease inhibitors, azole antifungals) Increase or decrease: effects of warfarin Increase: QT prolongation—tricyclics Decrease: effects of guanethidine, cloNI- Dine, indirect-acting sympathomimetics (ePHEDrine) Drug/Herb Increase: serotonin syndrome—SAM-e, St. John’s wort Increase: CNS depression—hops, kava, lavender, valerian Drug/Lab Test Increase: LFTs Decrease: HB
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TREATMENT OF OVERDOSE: ECG monitoring; administer anticonvulsant, atropine for bradycardia
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DOSAGE AND ROUTES Depression • Adult: PO 150 mg/day in divided doses, may increase by 50 mg/day q3- 4days, max 400 mg/day (outpatient), 600 mg/day (inpatient); EXT REL 150 mg in PM, may increase gradually by 75 mg/day q3days, max 375 mg/ day • Child 6-18 yr (unlabeled): PO 1.5-2 mg/kg/day in divided doses, may in- crease q3-4days up to 6 mg/kg/day or 400 mg/day, whichever is less • Geriatric: PO 25-50 mg at bedtime, increase by 25-50 mg q3-7days to de- sired dose, usually 75-150 mg/day
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Available forms: Tabs 50, 100, 150, 300 mg; ext rel tabs 150, 300 mg
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Administer: • Increased fluids, bulk in diet if consti- pation occurs, especially in geriatric patients • With food, milk for GI symptoms • Dosage at bedtime for oversedation during day; may take entire dose at bed- time; geriatric patients may not tolerate daily dosing • Avoid use of CNS depressants • Do not crush, break, chew ext rel product • Store in tight, light-resistant container at room temperature
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Assess: • CV status: B/P lying, standing; pulse q4hr; if systolic B/P drops 20 mm Hg, hold product, notify prescriber; take vital signs q4hr in patients with CV disease • Blood studies: CBC, leukocytes, differ- ential • Hepatic studies: AST, ALT, bilirubin • Weight weekly; appetite may increase with product • ECG for flattening of T wave, bundle branch block, AV block, dysrhythmias in cardiac patients • EPS, primarily in geriatric patients: rigidity, dystonia, akathisia
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Evaluate: • Therapeutic response: decreased de- pression
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That therapeutic effects may take 2-3 wk; to take ext rel product before bed- time; not to crush, chew ext rel prod- uct • To use caution when driving, performing other activities requiring alertness because of drowsiness, dizziness, blurred vision • To avoid alcohol ingestion • Not to discontinue medication quickly after long-term use; may cause nausea, headache, malaise • To report urinary retention, priapism >4 hr immediately • To wear sunscreen or large hat be- cause photosensitivity occurs
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PHARMACOKINETICS Peak 1 hr without food, 2 hr with food; metabolized by liver (CYP3A4); excreted by kidneys, in feces; half-life 4.4-7.5 hr
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• Child 6-18 yr (unlabeled): PO 1.5-2 mg/kg/day in divided doses, may in- crease q3-4days up to 6 mg/kg/day or 400 mg/day, whichever is less
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