Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Labetalol hydrochloride is the prototype drug of a new class of antihypertensive agents that competitively and peripherally blocks both beta- and alpha-adrenergic receptors. It possesses approximately one fourth of the beta-blocking activity of propranolol hydrochloride and one half of the alpha-blocking activity of phentolamine. In humans, the effective beta- to alpha-blocking activity is approximately 7:1. It has been used successfully in oral form to treat patients with mild, moderate, and severe hypertension and in intravenous form to manage hypertensive emergencies. Prominent side effects include orthostatic hypotension and gastrointestinal disturbances. Overall, the drug appears to offer several advantages over pure beta-blocking drugs in some patients and should expand the armamentarium of the practicing physician in the management of the difficult hypertensive patient.
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PMID:Labetalol. Current research and therapeutic status. 633 50

Labetalol hydrochloride (LBT), 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl) amino] ethyl]-benzamide, a non-selective alpha, beta-adrenoceptor antagonist is used in the treatment of hypertension. It shows variable bioavailability ranging from 10-80% which may be attributed to its minimum solubility in pH range 6 to 10, the pH conditions prevailing at the major site of absorption i.e. small intestine. Also due to its half life of 3 to 6 hrs it is administered twice daily. In the present work non-effervescent sustained release gastroretentive floating tablets of labetalol hydrochloride have been developed using various grades of HPMC and Poloxamer M127 as wetting agent. The tablets were evaluated for in vitro drug release, floating time, floating lag time, swelling studies etc. The tablets formulated with HPMC K4M CR and HPMC K15M CR along with Poloxamer showed negligible floating lag time with a total floating time over 12 hrs with complete release. Formulation was optimized using Stat-Ease Design Expert 7.1 software. Optimized batch was evaluated for the effect of change of osmolarity and pH on drug release, floating and swelling behaviour.
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PMID:Formulation and evaluation of a gastroretentive dosage form of labetalol hydrochloride. 2036 5