MEDICINAL CHEMISTRY
MEDICINAL CHEMISTRY
MEDICINAL CHEMISTRY
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Ramipril Altace ( Hoechst-Marion) 2.5 – 20 1or 2 12 –24<br />
Trandolapril Mavik (Knoll) 1 - 4 1 24<br />
4. Angiotensin- II Antagonist<br />
Candesartan cilexetil Atacand (Astra) 8 – 32 1 or 2 24<br />
Irbesartan Avapro (Sanobil) 75 – 300 1 24<br />
Losartan Cozaar (Merk) 25 – 100 1 or 2 12 –24<br />
Telmisartan Micardis (Boehringer) 40 - 80 1 24<br />
Valsartan Diovan (Novartis) 80 - 320 1 24<br />
Calcium Channel Antagonist<br />
(i) Dihydro pyridines<br />
Amlodipine Norvasc (Pfizer) 2.5 – 10 1 24<br />
Felodipine Plendil (Astra) 2.5 – 10 1 24<br />
Isradipine DynaCirc ( Novartis)<br />
DynaCirc CR<br />
(Novartis)<br />
Nifedipine Procardia XL (Pfizer)<br />
Adalat CC (Bayer)<br />
5 – 20<br />
5 – 20<br />
2<br />
1<br />
3 - 6<br />
24<br />
30 –90 1 24<br />
Nicardipine Generic 60 –120 2 12<br />
Nisoldipine Sular ( Zeneca) 20 - 60 1 12 –24<br />
(ii) Non –Dihydropyridines<br />
(a) Phenylalkyl amine<br />
Verapamil Calan SR(Searle)<br />
Covera HS (Searle)<br />
Isoptin SR ( Knoll)<br />
Verelan (lederle)<br />
(b) Benzothiazepines<br />
Diltiazem Cardizem SR (Hoechst)<br />
Cardizem CR (Hoechst)<br />
Dilacor XR<br />
( Watson)<br />
Tiazac (Forest)<br />
120 –480<br />
180 – 480<br />
120 – 480<br />
120 - 480<br />
120- 360<br />
120 –360<br />
120 – 540<br />
120 - 540<br />
1<br />
1(at bed time)<br />
1 or 2<br />
1<br />
ACE = Angiotensin Converting Enzyme. IR = Immediate release, SR = Sustained release, CR = Control<br />
release, LA = Long acting, XR = Extra release (Oparil, 2000; Negrea, 2001).<br />
Classification of Antihypertensives agents and their Chemistry<br />
Antihypertensives are those agents which are used to reduce high blood pressure.<br />
(A) Adrenoceptor Blocking Agents:<br />
1) α - Adrenergic Antagonist<br />
a) Piperazinylquinazoline derivatives e.g. Prazosin, Terazosin<br />
b) Imidazoline derivatives e.g. Tolazoline, Phentolamine<br />
2) β - adrenoceptor antagonists e.g. Propranolol, Atenolol, Metoprolol<br />
3) α, β - adrenoceptor antagonists e.g. Labetalol<br />
4) Centrally Acting Agents e.g. Methyldopa, Clonidine, Guanabenz, Guanfacine<br />
5) Agents Depleting Neurotransmitter Stores e.g. Reserpine, Guanethidine,<br />
Guandrel Sulfate<br />
6) Gaglionic Blocking Agents e.g. Pentolinium, Trimethaphan, Mecamylamine HCl<br />
2<br />
1<br />
1<br />
1<br />
24<br />
24<br />
12-24<br />
24<br />
12<br />
24<br />
24<br />
24
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