Names and pronunciation
(lor-a′ze-pam) Ativan
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Drug reference
(lor-a′ze-pam) Ativan
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Func. class.: Sedative, hypnotic; antianxiety
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Chem. class.: Benzodiazepine, short acting Controlled Substance Schedule IV
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Do not confuse: LORazepam/ALPRAZolam/clonazePAM
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ACTION: Potentiates the actions of GABA, especially in the limbic system and the reticular formation
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USES: Anxiety, irritability with psy- chiatric or organic disorders, preop- L eratively; insomnia; adjunct for endo- scopic procedures, status epilepticus, insomnia
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Unlabeled uses: Antiemetic before che- motherapy, rectal use, alcohol with- drawal, seizure prophylaxis, agitation, insomnia, sedation maintenance
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CONTRAINDICATIONS: Preg- nancy, breastfeeding, hypersensitivity to benzodiazepines, benzyl alcohol; closed-angle glaucoma, psychosis, history of drug abuse, COPD, sleep apnea Precautions: Children <12 yr, geriatric patients, debilitated patients, renal/ hepatic disease, addiction, suicidal ide- ation, abrupt discontinuation
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Black Box Warning: Coadministration with other CNS depressants, abrupt dis- continuation, substance abuse Black Box Warning: Increase: LORaze- pam effects—CNS depressants, opioids, alcohol, disulfiram Increase: delirium, sedation—cloZAPine Increase: LORazepam effect of probene- cid, valproate reduce dose by 50% Decrease: LORazepam effects—oral contraceptives; change dose as needed Drug/Herb Increase: CNS depression—chamomile, kava, valerian Drug/Lab Test Increase: AST, ALT Black Box Warning: Coadministration with other CNS depressants (especially opioids) should be avoided; if used to- gether, use lower dose • Renal/hepatic/blood status if receiving high-dose therapy • Physical dependency, withdrawal symptoms: headache, nausea, vomiting, muscle pain, weakness, tremors, sei zures; after long-term, excessive use • Beers: avoid in older adults; may in- crease cognitive impairment, delirium • Pregnancy/breastfeeding: use only if L clearly needed; neonatal withdrawal syn drome may occur; do not breastfeed un less benefits outweigh risk; excreted in breast milk Black Box Warning: To avoid alcohol, other psychotropic medications, opioids unless directed by prescriber; to notify prescriber immediately of trouble breathing, dizziness, coma, or if no response • Not to discontinue medication abruptly after long-term use, taper • To rise slowly because fainting may occur, especially among geriatric pa- tients • That drowsiness may worsen at begin- ning of treatment • To report suicidal ideation • Pregnancy/breastfeeding: not to use in pregnancy or breastfeeding; to use contraception while using this product
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SIDE EFFECTS CNS: Dizziness, drowsiness, confusion, headache, anxiety, tremors, stimulation, fatigue, depression, insomnia, hallucina- tions, weakness, unsteadiness CV: Orthostatic hypotension, ECG changes, tachycardia, hypotension, apnea, cardiac arrest (IV, rapid) EENT: Blurred vision, tinnitus, mydriasis GI: Constipation, dry mouth, nausea, vomiting, anorexia, diarrhea INTEG: Rash, dermatitis, itching MISC: Acidosis
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INTERACTIONS
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TREATMENT OF OVERDOSE: Lavage, VS, supportive care, flumazenil HIGH ALERT
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DOSAGE AND ROUTES Anxiety • Adult/adolescent ≥12 yr: PO 2-3 mg/ day in divided doses, max 10 mg/day • Geriatric: PO 1-2 mg/day in divided doses or 0.5-1 mg at bedtime • Child <11 yr (unlabeled): PO 0.025- 0.05 mg/kg/dose (max q4hr) Preoperatively for sedation • Adult: IM 50 mcg/kg 2 hr before sur- gery; IV 44 mcg/kg 15-20 min before sur- gery, max 2 mg 15-20 min before surgery • Child ≥12 yr: IV 0.05 mg/kg, max 4 mg Status epilepticus • Adult: IM/IV 4 mg, may repeat after 10-15 min • Neonate: IV 0.05 mg/kg • Child: IV 0.1 mg/kg up to 4 mg/dose; RECT(unlabeled) 0.05-0.1 mg × 2; wait 7 min before giving 2nd dose Insomnia • Adult: PO 2-4 mg at bedtime; only minimally effective after 2 wk continuous therapy • Geriatric: PO 0.5-1 mg initially Sedation in mechanically ventilated patients (unlabeled) • Adult/adolescent: INTERMITTENT IV 0.044 mg/kg q2-4hr, prn, max 4-mg single dose • Adult/adolescent: IV INFUSION 0.5-8 mg/hr, titrate, use loading dose of 2-4 mg Alcohol withdrawal (unlabeled) • Adult: PO 2 mg q6hr × 4 doses, then 1 mg q6hr for 8 doses
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Available forms: Tabs 0.5, 1, 2 mg; inj 2, 4 mg/mL; oral sol 2 mg/mL
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Administer: PO route • With food or milk for GI symptoms; crushed if patient is unable to swallow medication whole • Sugarless gum, hard candy, frequent sips of water for dry mouth • Give largest dose before bedtime if giv- ing in divided doses • Oral solution: use calibrated dropper; add to food/drink; consume immediately IM route • Deep into large muscle mass • Use this route when IV is not feasible Direct IV route • Prepare immediately before use; short stability time • IV after diluting in equal vol sterile water, 5% dextrose, or 0.9% NaCl for inj; give through Y-tube or 3-way stop- cock; give at ≤2 mg/1 min; do not give rapidly • To reduce amount of benzyl alcohol to a neonate, dilute with preservative-free sterile water injection (0.4 mg/mL) for IV use Y-site compatibilities: Acetaminophen, acyclovir, albumin, allopurinol, amifos- tine, amikacin, amoxicillin, amoxicillin/ clavulanate, amphotericin B cholesteryl, amsacrine, atenolol, atracurium, bivaliru- din, bleomycin, bumetanide, butorphanol, calcium chloride/gluconate, CARBOplatin, ceFAZolin, cefepime, cefotaxime, cefo- TEtan, cefOXitin, cefTAZidime, ceftizox- ime, ceftobiprole, cefTRIAXone, cefurox- ime, chloramphenicol, chlorproMAZINE, cimetidine, ciprofloxacin, cisatracurium, CISplatin, cladribine, clindamycin, cloNI- Dine, cyclophosphamide, cycloSPORINE, cytarabine, DACTINomycin, DAPTOmycin, dexamethasone, dexmedetomidine, diltia- zem, DOBUTamine, DOCEtaxel, DOPa- mine, doripenem, DOXOrubicin, DOXO- rubicin liposomal, droperidol, enalaprilat, ePHEDrine, EPINEPHrine, epirubicin, eptifibatide, erythromycin, esmolol, etomidate, famotidine, fenoldopam, fen- taNYL, filgrastim, fluconazole, fludarabine, fosphenytoin, furosemide, ganciclovir, gatifloxacin, gemcitabine, gentamicin, gly- copyrrolate, granisetron, haloperidol, heparin, hydrocortisone, HYDROmor- phone, hydrOXYzine, ifosfamide, inamri- none, insulin (regular), irinotecan, iso- proterenol, ketorolac, labetalol, lidocaine, linezolid, magnesium sulfate, mannitol, mechlorethamine, melphalan, merope- nem, metaraminol, methadone, metho- trexate, methyldopate, methylPREDNISo- lone, metoclopramide, metoprolol, metroNIDAZOLE, micafungin, midazolam, milrinone, minocycline, mitoXANtrone, morphine, mycophenolate, nafcillin, nalbu- phine, naloxone, nesiritide, niCARdipine, nitroglycerin, nitroprusside, norepineph- rine, octreotide, oxaliplatin, oxytocin, PACLitaxel, palonosetron, pamidronate, pancuronium, PEMEtrexed, pentamidine, PENTobarbital, PHENobarbital, piperacil- lin, piperacillin-tazobactam, polymyxin B, potassium chloride, propofol, ranitidine, remifentanil, tacrolimus, teniposide, the- ophylline, thiotepa, ticarcillin, ticarcillin- clavulanate, tigecycline, tirofiban, tobra- mycin, TPN, trastuzumab, trimethobenzamide, trimethoprim-sulfa- methoxazole, vancomycin, vasopressin, vecuronium, verapamil, vinCRIStine, vinorelbine, voriconazole, zidovudine
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Assess: • Anxiety: decrease in anxiety; mental status: mood, sensorium, affect, sleeping pattern, drowsiness, dizziness, suicidal tendencies
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Evaluate: • Therapeutic response: decreased anxi- ety, restlessness, insomnia
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That product may be taken with food • Not to take more than prescribed amount; may be habit forming • To avoid OTC preparations (cough, cold, hay fever) unless approved by prescriber • To avoid driving, activities that require alertness since drowsiness may occur
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PHARMACOKINETICS Metabolized by liver; excreted by kid- neys; crosses placenta, excreted in breast milk; half-life 42 hr (neonates), 10.5 hr (older child), 12 hr (adult), 91% pro- tein bound PO: Onset 1 hr, peak 2 hr, duration 12-24 hr IM: Onset 15-30 min, peak 1-11⁄2 hr, duration 6-8 hr IV: Onset 5 min, peak 1-11⁄2 hr, duration 6-8 hr
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• Adult/adolescent ≥12 yr: PO 2-3 mg/ day in divided doses, max 10 mg/day
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• Adult: IM 50 mcg/kg 2 hr before sur- gery; IV 44 mcg/kg 15-20 min before sur- gery, max 2 mg 15-20 min before surgery
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• Adult: IM/IV 4 mg, may repeat after 10-15 min
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• Adult: PO 2-4 mg at bedtime; only minimally effective after 2 wk continuous therapy
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• Adult/adolescent: INTERMITTENT IV 0.044 mg/kg q2-4hr, prn, max 4-mg single dose
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• Adult/adolescent: IV INFUSION 0.5-8 mg/hr, titrate, use loading dose of 2-4 mg Alcohol withdrawal (unlabeled)
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• Adult: PO 2 mg q6hr × 4 doses, then 1 mg q6hr for 8 doses
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