Angiotensin receptors: their pharmacological aspects and side effects
defined G q -mediated calcium and protein kinase C signaling pathways as well as
intracellular signaling cascade till to the nucleus. These different pathways are
responsible for the regulation of gene transcription and the expression of proteins
which control the growth responses and proliferation of cell in Angiotensin-
II target tissues. Some of the later consequences of AT 1 receptor activation are
counteracted by the structurally dissimilar AT 2 receptor, which antagonizes the
effects of AT 1 -mediated growth responses in several cell types, in particular
endothelial cells, cardiomyocytes, and ovarian granulosa cells. This account of the
AT 1 receptor will address its gene expression, ligand binding, activation and signal
transduction pathways, and physiological roles in the regulation of the activity and
growth of its major target cells in cardiovascular, neuronal, and endocrine tissues.
Angiotensin-II receptor blockers are the new class of drugs which classified
under antihypertensive agents drugs .ARBs mode of action is different from other
Angiotensin converting enzyme (ACE) inhibitors. ACE also works on Renin
Angiotensin System. Because of binding to the receptor site, ARBs produces the
complete inhibition of Angiotensin-II action. A lot of ARB drugs are available in
the market. which are approved by Food and DrugAdministration for the treatment
of hypertension, for the use either alone or in combination with other drugs (SPI,
2002; Olin, 2002). The different drugs available in the market are condensartan,
eprosartan, irbesartan, losartan, olmesartan, telmisartan and valsartan.
Those drugs which are used for the lowering blood pressure can cause some side
effects like dizziness, headache, cold flu and others. Kidney failure, liver failure
and some allergic reactions like swelling around the mouth and throat are also
shows by these drugs but rarely. (Rodgers and Patterson, 2001).
Different Angiotensin-II receptor blocker shows same mode of action but all of
them has different efficacy and pharmacokinetic profile with low side effects.ACE
inhibitors affect the bradykinin level of body but ARBs do not affect bradykinin
level but they are contraindicated in pregnancy.
Pharmacology of Angiotensin Receptor Blocker
Pharmacology of ARBs depends on the Rennin Angiotensin Systen (RAS). In
RAS renin converts the angiotensinogen to an inactive decapeptide Angiotensin-I
(Dzau et al. , 1993; Urata et al. , 1990; Linz et al. , 1995). Then After angiotensin-I
is converted to angiotensin-II by Angiotensin converting enzyme. Angiotensin-II
is the main end product of this cycle. Different type of pathogenesis reactions
like essential Hypertension, reno-vascular hypertension, congestive heart failure
and renal disease associated with albuminuria are produced by angiotensin-II.
Because of ACE inhibitors, when rennin angiotensin system blocks its shows few
side effects also like cough, and angioedema (Burnier and Brunner, 2000; Bumier,
2001; Rodgers and Patterson, 2001).
International Journal of Bioinformatics and Biological Sciences : v.2 n.3&4. Dec. 2014
147