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LabetalolSystematic (IUPAC) name2-hydroxy-5-{1-hydroxy-2-ethyl}benzamideIdentifiersCAS number36894-69-6ATC codeC07AG01PubChem3869DrugBankAPRD01062Chemical dataFormulaC19H24N2O3 Mol. mass328.406 g/molPharmacokinetic dataBioavailability90-100%Protein binding50%Metabolismhepatic pass metabolism,Half lifeTablet: 6-8 hours; IV: 5.5 hoursExcretionExcreted in urine, not removed by hemodialysisTherapeutic considerationsPregnancy cat.COne of few drugs used for PIHLegal status℞ Prescription onlyRoutesoral ivLabetalol (Normodyne, Trandate, fixed combination with hydrochlorothiazide: Normozyde) is a mixed alpha/beta antagonistic drug used to treat high blood pressure.// ChemistryLabetalol has stereoisomers. It a racemic mixture of four isomers. Two of these isomers, the (S,S)- and (R,S)- forms are inactive. The third, the (S,R)-isomer, is a powerful α1 blocker. The fourth isomer, the (R,R)-isomer, is a mixed nonselective β blocker and selective β2 agonist.It works by blocking these adrenergic receptors, which decreases peripheral vascular resistance without significantly altering heart rate or cardiac output. The β:α antagonism of Labetalol is approximately 3:1. IndicationsIt has a particular indication in the treatment of pregnancy-induced hypertension which is commonly associated with pre-eclampsia. It is also used to treat chronic hypertension of pheochromocytoma and hypertensive crisis. AdministrationLabetalol is available in 100, 200, and 300 mg tablets and intravenously (only as Trandate) in 5 mg/ml solution. Adults taking tablets usually start with 100 mg two times a day, with a maximum of 2.4 g/day. In an emergency situation, this may be higher. IV doses are usually started at 20mg over 2 minutes. Additional doses of 40mg, then 80mg may be administered every ten minutes as needed. Additional 80mg doses can be given to a total maximum dose of 300 mg. Additionally, labetalol can be administered by IV infusion at a rate of 2mg/minute, with a maximum dose of 300mg. Side effectsSide effects may include:DrowsinessFatigueWeaknessDifficulty sleepingDiminished sexual functionScalp tingling which passes after time.A rare but potentially lethal side effect is respiratory distress. ContraindicationsLabetalol has relative contraindications for use in patients with asthma, congestive heart failure, any degree of heart block, bradycardia, or those in cardiogenic shock.
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