Antihypertensives
Tomáš Goněc 19.11.2012
Hypertension
 blood pressure >135/85 mmHg
 most common cardiovascular disease
 untreated = major risk of coronary artery
disease, heart failure, stroke, renal failure
 long-time untreated hypertension: left
ventricule hyperthropy, retinopathy, angina
pectoris, lung, liver, renal failure
Hypertension – drug therapy
 central and peripheral autonomic inervation
 blood vessel wall relaxation
 renine-angiotensine-aldosteron system
 diuretics
 other mechanism
α2-adrenergic and imidazoline receptor
agonists
Clonidine synthesis
Guanabenz synthesis
Guanfacine synthesis
Moxonidine synthesis
Rilmenidine synthesis
α1-adrenergic receptor antagonists
N
NO
O
NH2
N
N
O
O
N
NO
O
NH2
N
N
O
O
O
O
N
NO
O
NH2
N
N
O
Prazosin
Terazosin
Doxazosin
Prazosin synthesis
Doxazosin synthesis
β-blockers
 general structure:
O N
H
R1
OH
OH
N
H
R1
R2
R2
Aryloxypropanolamines
Arylethanolamines
β-blockers
 absolute configuration important
β-blockers – non selective
β-blockers - cardioselective
Mixed β + α antagonists
N
H
OH
O NH2
OH
O
OH
O
O
NH
Labetalol
Carvedilol
Labetalol synthesis
Ca2+blockers
Ca2+blockers
 Verapamil, diltiazem
 dihydropyridines
RAA system
ACE inhibitors – mechanism of action
 +
ACE inhibitors

ACE
inhibitors

Captopril synthesis
Enalapril synthesis
Angiotensin II inhibitors

Angiotensin II inhibitors
