ISSN:
1432-1041
Keywords:
multifactorial antihypertensives
;
hybrid drugs
;
carvedilol
;
labetalol
;
ketanserin
;
urapidil
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
Summary Compounds with two or more different pharmacodynamic activities in a single molecule are designated as hybrid drugs. If several stereoisomers with different pharmacodynamic activities exist in one molecule, the term pseudo-hybrid drug is applied. In the treatment of hypertension, the use of hybrid drugs enables a considerable reduction in the number of tablets to be taken per day. Conversely, the dose of each individual component cannot be tritrated. Most hybrid drugs used in antihypertensive treatment are β-blockers with an additional vasodilator component, caused by different mechanisms such as α-adrenoceptor blockade, β2-adrenoceptor agonism, ACE inhibition or direct relaxation of vascular smooth muscle. Examples include labetalol (in fact, a mixture of four stereoisomers), carvedilol, celiprolol, dilevalol, tertatolol and BWA-575 C. A combination of β-receptor blockade and vasodilatation may be beneficial from a hemodynamic point of view. More recently it has been recognized that urapidil and ketanserin are hybrid drugs, each containing at least two pharmacodynamic activities in their molecules.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01409470
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