Names and pronunciation
(la-bet′a-lole) Trandate
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Drug reference
(la-bet′a-lole) Trandate
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Func. class.: Antihypertensive, antianginal
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Chem. class.: α-1/β-Blocker
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Do not confuse: labetalol/Lamictal/lamotrigine
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ACTION: Produces decreases in B/P without reflex tachycardia or significant reduction in heart rate through mixture of α-blocking, β-blocking effects; ele- vated plasma renins are reduced
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USES: Mild to moderate hypertension; treatment of severe hypertension (IV)
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CONTRAINDICATIONS: Hyper- sensitivity to β-blockers, cardiogenic shock, heart block (2nd or 3rd degree), sinus bradycardia, HF, bronchial asthma Precautions: Pregnancy, breastfeeding, geriatric patients, major surgery, diabe- tes mellitus, thyroid/renal/hepatic dis- ease, COPD, well-compensated heart failure, nonallergic bronchospasm, peripheral vascular disease
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Black Box Warning: Abrupt discontinu- ation Black Box Warning: Abrupt discontinu- ation: product should be tapered to pre- vent adverse reactions • Baselines of renal/hepatic studies be- fore therapy begins • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; use caution in breastfeeding Black Box Warning: Not to discontinue product abruptly; to taper over 2 wk; may cause precipitate angina • Not to use OTC products containing α-adrenergic stimulants (nasal decon- gestants, OTC cold preparations) unless directed by prescriber • To report bradycardia, dizziness, confu sion, depression, fever, difficulty breathing, cold extremities, confusion, rash, sore throat • To take pulse at home; advise when to notify prescriber • May mask symptoms of hypoglycemia; monitor blood glucose closely in diabetes • To avoid alcohol, smoking, increased sodium intake • Hypertension: To comply with weight control, dietary adjustments, modified exercise program • To carry emergency ID to identify product, allergies • To avoid hazardous activities if dizzi- ness is present • To avoid hot baths, showers • To report symptoms of HF: difficulty breathing, especially on exertion or when lying down; night cough; swelling of ex tremities • To advise providers of use before surgery • To avoid driving or other hazardous activities until response is known; dizzi- ness, drowsiness, may occur
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SIDE EFFECTS CNS: Dizziness, mental changes, drowsi- ness, fatigue, headache, depression, anxi- ety, nightmares, paresthesias, lethargy CV: Orthostatic hypotension, bradycar- dia, HF, chest pain, ventricular dysrhyth mias EENT: Visual changes; double vision; dry, burning eyes; floppy iris syndrome; nasal congestion ENDO: Hyperkalemia GI: Nausea, vomiting, diarrhea, dyspep- sia, taste distortion, hepatotoxicity GU: Impotence, dysuria, ejaculatory failure INTEG: Rash, urticaria, pruritus, fever L RESP: Bronchospasm, dyspnea, wheezing
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INTERACTIONS • Do not use within 2 wk of MAOIs Increase: myocardial depression— hydantoins, general anesthetics, verap amil, class I antidysrhythmics Increase: tremor—tricyclic antidepressants Increase: hypotension—diuretics, other antihypertensives, cimetidine, nitroglyc- erin, alcohol, nitrates Decrease: effects of—sympathomimet- ics, lidocaine, theophylline, β-blockers, bronchodilators, xanthines Decrease: antihypertensive effect—NSAIDs, salicylates Increase or decrease: effects of—anti- diabetics; monitor blood glucose Drug/Herb Increase: antihypertensive effect— hawthorn Decrease: antihypertensive effect—ephe- dra (ma huang) Drug/Lab Test Increase: ANA titer, blood glucose, alk phos, LDH, AST, ALT, uric acid False increase: urinary catecholamines
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TREATMENT OF OVERDOSE: Lavage, IV glucagon or atropine for brady- cardia, theophylline (nebulizer) for bron- chospasm; digoxin, O2, diuretic for cardiac failure; hemodialysis useful for removal/ hypotension; administer vasopressor, car- diac monitor (hypertensive urgency)
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DOSAGE AND ROUTES Hypertension • Adult: PO Outpatient 100 mg bid; may be given with diuretic; may increase to 200 mg bid after 2 days; may increase q1-3days; max 2400 mg/day in divided doses; Inpa- tient 200 mg then 200-400 mg in 6-12 hr, depends on response; may increase by 200 mg bid at 1-day intervals • Child/adolescent (unlabeled): PO 1-3 mg/kg/day, titrate to max 10-12 mg/kg/ day based on B/P, max 12 mg/kg/day, max 1200 mg/day; IV 0.2-1 mg/kg over 2 min; IV INFUSION 0.25-3 mg/kg/hr, max 3 mg/kg/hr Hypertensive crisis • Adult: IV Intermittent 20 mg over 2 min; may repeat 20-80 mg over 2 min q10min, max 300 mg; IV Cont INFU- SION after loading dose give 1-2 mg/min until desired response or max 300 mg
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Available forms: Tabs 100, 200, 300 mg; inj 5 mg/mL, 20-, 40-mL vials
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Administer: PO route • PO before meals, or with meals; tab may be crushed or swallowed whole; give with meals to increase absorption • Take pulse before use; if <50 bpm, hold dose, notify prescriber • Take apical pulse before use; if <50 bpm, withhold; notify prescriber • When discontinuing IV and starting PO, begin PO when B/P rises; start at 200 mg, then 200-400 mg in 6-12 hr; adjust as needed • Do not discontinue before surgery or abruptly • Store in dry area at room temperature; do not freeze Direct IV route • Give undiluted (5 mg/mL) over 2 min Continuous IV INFUSION route • Give at a rate of 2 mg/min after diluting in LR, D5W, D5 in 0.2%, 0.9%, 0.33% NaCl, Ringer’s inj; infusion is titrated to patient response; 200 mg of product/160 mL sol = 1 mg/mL; 300 mg of product/240 mL sol = 1 mg/mL; 200 mg of product/250 mL sol = 2 mg/3 mL; use infusion pump • Keep patient recumbent during and for 3 hr after administration; monitor VS q5- 15min Y-site compatibilities: Alemtuzumab, alfen- tanil, amikacin, aminocaproic acid, aminophylline, amiodarone, anidulafungin, argatroban, arsenic trioxide, ascorbic acid injection, atracurium, atropine, azithromy- cin, aztreonam, benztropine, bivalirudin, bleomycin, bretylium, bumetanide, buprenorphine, butorphanol, calcium chloride/gluconate, CARBOplatin, carmus- tine, caspofungin, ceFAZolin, cefotaxime, cefoTEtan, cefOXitin, ceftaroline, cefTAZi- dime, ceftizoxime, chlorproMAZINE, cimetidine, CISplatin, cloNIDine, cyanoco- balamin, cyclophosphamide, cycloSPO- RINE, cytarabine, DACTINomycin, DAPTO- mycin, DAUNOrubicin liposome, dexmedetomidine, dexrazoxane, digoxin, diltiazem, diphenhydrAMINE, DOBUTa- mine, DOCEtaxel, dolasetron, DOPamine, doripenem, doxacurium, DOXOrubicin, DOXOrubicin liposomal, doxycycline, enal- aprilat, ePHEDrine, EPINEPHrine, epirubi- cin, epoetin alfa, eptifibatide, ertapenem, erythromycin lactobionate, esmolol, etopo- side, etoposide phosphate, famotidine, fenoldopam, fentaNYL, fluconazole, fluda- rabine, fluorouracil, folic acid, gallium, ganciclovir, gatifloxacin, gemcitabine, gen- tamicin, glycopyrrolate, granisetron, HYDROmorphone, hydroxyzine, IDArubi- cin, ifosfamide, imipenem-cilastatin, inamrinone, irinotecan, isoproterenol, lac- tated Ringer’s injection, lepirudin, leucovo- rin, levofloxacin, lidocaine, linezolid injec- tion, LORazepam, magnesium sulfate, mannitol, mechlorethamine, meperidine, metaraminol, methyldopate, methylPRED- NISolone, metoclopramide, metoprolol, metroNIDAZOLE, midazolam, milrinone, minocycline, mitoXANtrone, morphine, moxifloxacin, multiple vitamins injection, mycophenolate, nalbuphine, naloxone, netilmicin, niCARdipine, nitroglycerin, nitroprusside, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxyto- cin, palonosetron, pamidronate, pan- curonium, papaverine, PEMEtrexed, pent- amidine, pentazocine, PENTobarbital, PHENobarbital, phentolamine, phenyleph- rine, phytonadione, polymyxin B, potas- sium acetate/chloride/phosphates, procain- amide, prochlorperazine, promethazine, propofol, propranolol, protamine, pyridox- ine, quiNIDine, quinupristin-dalfopristin, ranitidine, Ringer’s injection, rocuronium, sodium acetate/bicarbonate, succinylcho- line, SUFentanil, tacrolimus, telavancin, teniposide, theophylline, thiamine, thiotepa, ticarcillin-clavulanate, tigecycline, tirofiban, tobramycin, tolazo- line, urokinase, vancomycin, vasopressin, vecuronium, verapamil, vinBLAStine, vin- CRIStine, vinorelbine, voriconazole, zole- dronic acid
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Assess: • Hypertension: monitor B/P before starting treatment, periodically thereafter; note pulse, rate, rhythm, quality; apical/ radial pulse before administration; notify prescriber of any significant changes, watch for orthostatic hypotension • HF: I&O, weight daily; fluid overload: weight gain, jugular venous distention, edema, crackles in lungs; report weight gain >5 lb
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Evaluate: • Therapeutic response: decreased B/P after 1-2 wk
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CLINICAL CONSIDERATIONS
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Patient and caregiver information:
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PHARMACOKINETICS Half-life 2.5-8 hr, metabolized by liver (metabolites inactive), excreted in urine, crosses placenta, excreted in breast milk, protein binding 50% PO: Onset 30 min, peak 1-4 hr, duration 8-24 hr IV: Onset 2-5 min, peak 5-15 min, dura- tion 2-4 hr
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• Child/adolescent (unlabeled): PO 1-3 mg/kg/day, titrate to max 10-12 mg/kg/ day based on B/P, max 12 mg/kg/day, max 1200 mg/day; IV 0.2-1 mg/kg over 2 min; IV INFUSION 0.25-3 mg/kg/hr, max 3 mg/kg/hr Hypertensive crisis
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