Bupranolol

C07AA19

220-222 ° C ( hydrochloride racemate)

• 45 mg · kg -1 ( LD50, mouse, i.v.)
• 39.3 mg · kg -1 ( LD50, mouse, iv, hydrochloride)
• 329 mg · kg -1 ( LD50, Mouse, oral, hydrochloride)
• 15.3 mg · kg -1 ( LD50, rat, iv, hydrochloride)
• 518 mg · kg -1 ( LD50, Rat, oral, hydrochloride)

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Bupranolol (trade name: Betadrenol ) is a nonselective beta-blockers without intrinsic activity (ISA ), but with strong membrane stabilizing effect. Its effectiveness is similar to that of Propranolol.

Stereochemistry

Bupranolol is a chiral compound containing an asymmetrically substituted carbon atom. Therefore, the compound is usually present as a 1:1 mixture (racemate ) of two mirror-image molecules ( enantiomers ), which may differ in physiological effects and the rotation value. As the drug is used as the racemate.

By a suitable synthetic strategies (see also: enantiomerically pure drug synthesis ) or separation process ( resolution ) can be selectively isolate the individual stereoisomers.

Dosage

Like other beta-blockers bupranolol is used to treat high blood pressure and tachycardia. The initial dose is 50 mg twice daily. This can be increased to up to 100 mg four times daily. Bupranolol eye drops ( 0.05-0.5 % ) can be used for the treatment of glaucoma.

Pharmacology

Bupranolol is rapidly and almost completely from the gut. About 90 % of the amount taken subject to first-pass effect. Bupranolol has a plasma half -life of 2 to 4 hours, and rarely achieved in therapeutic dosage levels above 1 g / L in plasma. The major metabolite of Bupranonols is Carboxybupranolol (4- chloro-3- [3 - (1,1- dimethylethylamino )-2 -hydroxy- propoxy ] benzoylsäure ), which is excreted to 88% within 24 hours via the kidneys.

Contraindications and interactions

Contraindications and interactions are essentially the same as in non-selective beta-blockers, propranolol and other.