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Labetalol
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| Systematic (IUPAC) name | |
| 2-hydroxy-5-[1-hydroxy-2- (4-phenylbutan-2-ylamino)-ethyl]-benzamide |
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| Identifiers | |
| CAS number | |
| ATC code | C07 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C19H24N2O3 |
| Mol. mass | 328.406 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 90-100% |
| Protein binding | 50% |
| Metabolism | hepatic pass metabolism, |
| Half life | Tablet: 6-8 hours; IV: 5.5 hours |
| Excretion | Excreted in urine, not removed by hemodialysis |
| Therapeutic considerations | |
| Pregnancy cat. |
C |
| Legal status |
℞ Prescription only |
| Routes | oral iv |
Labetalol (Normodyne, Trandate, fixed combination with hydrochlorothiazide: Normozyde) is an alpha-1 and beta adrenergic blocker used to treat high blood pressure. It works by blocking these adrenergic receptors, which slows sinus heart rate, decreases peripheral vascular resistance. The alpha:beta antagonism of Labetalol is approximately 1:3.[1]
It has a particular indication in the treatment of pregnancy-induced hypertension.
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Administration
Labetalol 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 effects
Side effects may include:
- Drowsiness
- Fatigue
- Weakness
- Difficulty sleeping
- Diminished sexual function
- Scalp tingling which passes after time.
- A rare but potentially lethal side effect is respiratory distress.
Contraindications
Labetalol should not be used in patients that have asthma, congestive heart failure, any degree of heart blocks, slow heart rates or those in cardiogenic shock
References
- Hodgson, Barbara B., and Kizior, Robert J. Saunders Nursing Drug Handbook 2006. St. Louis, MO: Elsevier, Saunders, 2006. bledsoe "prehospital emergency pharmacology" upper Saddle River, New Jersey: Pearson 2005
- ^ D A Richards, J Tuckman, and B N Prichard (October 1976). "Assessment of alpha- and beta-adrenoceptor blocking actions of labetalol.". Br J Clin Pharmacol 3 (5): 849–855. PMID PMC1428931.
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Wikipedia content modification information:
- This page was last modified on 8 July 2008, at 02:31.
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