- Recent hypertension guidelines recommend that diuretics, calcium channel blockers (CCBs), angiotensin receptor blockers (ARBs) and ACE inhibitors are all appropriate initial antihypertensive therapies for most people.
- In general, the ARBs are effective in lowering blood pressure and generally they are well tolerated.
- Each ARB is important in treatment of hypertension yet due to its pharmacokinetics and pharmacodynamics properties, some ARB are shown to be beneficial for certain population.
Pharmacokinetics Characteristics of ARB
|
ARB
|
Hypertension
|
Heart Failure
|
Diabetic Neuropathy
|
Prevention of Stroke
|
CVS Risk Reduction
|
Following Myocardial Infarction
|
|
Candesartan
|
X
|
X
|
||||
|
Losartan
|
X
|
X
|
X
|
X
|
||
|
Irbesartan
|
X
|
X
|
||||
|
Telmisartan
|
X
|
X
|
||||
|
Valsartan
|
X
|
X
|
X
|
Choice of ARB in Clinical Condition of
Concern
|
Clinical Condition of Concern
|
Frist ARB of Choice
|
ARB with potentially Beneficial Effects
|
ARB to Avoid/Potentially Negative Effects
|
|
Cardiovascular
prevention
|
Telmisartan
|
Losartan
|
|
|
Heart
failure
|
Valsartan
Candesartan
Losartan
|
||
|
Myocardial
infarction
|
Valsartan
|
Telmisartan
|
|
|
Stroke
|
Losartan
|
Telmisartan
Candesartan
Eprosartan
|
|
|
Atrial
fibrillation
|
Telmisartan
|
Losartan
Candesartan
Valsartan
|
|
|
Diabetes
mellitus
|
Telmisartan
Valsartan
|
Telmisartan
Valsartan
|
Olmesartan
|
|
Diabetic
nephropathy
|
Losartan
Irbesartan
|
Telmisartan
Valsartan
Candesartan
|
Olmesartan
|
|
Metabolic
syndrome
|
Telmisartan
|
Valsartan
|
|
|
Hyperuricemia
|
Losartan
|
Irbesartan
|
Candesartan
|
|
Erectile
dysfunction
|
Valsartan
Losartan
Irbesartan
|
||
|
Cognitive
decline
|
Candesartan
Irbesartan
Losartan
Valsartan
Eprosartan
Telmisartan
|
Irbesartan
- It is well absorbed, does not require biotransformation to an active metabolite to exert its antihypertensive activity.
- While both losartan and irbesartan are registered for the treatment of late stage diabetic nephropathy, irbesartan is also registered for early stage diabetic nephropathy in the EU.
Losartan
- It has shown benefit in controlling hypertension, decreasing proteinuria, slowing the progression of type 2 diabetic nephropathy, and decreasing the risk of stroke in certain populations.
- Reduce proximal tubular reabsorption of uric acid leading to increased uric acid excretion and decreased serum uric acid concentrations.
- Losartan exerts an antiplatelet action by blockade of thromboxane A2 (TxA2) receptors.
Telmisartan
- long-lasting antihypertensive effects of telmisartan compared with other ARBs are likely due to this agent having the longest plasma elimination half-life of approximately 24 hours
- These unique characteristics of telmisartan manifest in a number of clinical advantages, such as long-lasting BP control and CV protection - consequently telmisartan has been identified as a gold-standard treatment and has been recommended as a preferred ARB treatment option
Valsartan
- Shown to improve insulin sensitivity in obese hypertensive patients.
- Cause significant improvement in NYHA class, ejection fraction and HF signs and symptoms in HF patients
Availability
in HKGU :
- Tab Irbesartan 150mg & 300 mg, Tab Losartan 50 mg & 100 mg, Tab Telmisartan 40 mg & 80 mg, Tab Valsartan 80 mg & 160 mg
References
:
- Abraham, H. M. A., White, C. M., & White, W. B. (2015). The comparative efficacy and safety of the angiotensin receptor blockers in the management of hypertension and other cardiovascular diseases. Drug Safety, 38(1), 33–54. http://doi.org/10.1007/s40264-014-0239-7
- Adams, M. A., & Trudeau, L. (2000). Irbesartan: review of pharmacology and comparative properties. The Canadian Journal of Clinical Pharmacology = Journal Canadien de Pharmacologie Clinique, 7(1), 22–31. Retrieved from http://www.ncbi.nlm.nih.gov/pubmed/10822210
- Bramlage, P., Durand-Zaleski, I., Desai, N., Pirk, O., & Hacker, C. (2009). The value of irbesartan in the management of hypertension. Expert Opinion on Pharmacotherapy, 10(11), 1817–31. http://doi.org/10.1517/14656560903103820
- Dézsi, C. A. (2016). The Different Therapeutic Choices with ARBs. Which One to Give? When? Why? American Journal of Cardiovascular Drugs, 16(4), 255–266. http://doi.org/10.1007/s40256-016-0165-4
- Mallat, S. G., Egan, B., Zhao, Y., Axon, R., Ezzati, M., Oza, S., … Palatini, P. (2012). What is a preferred angiotensin II receptor blocker-based combination therapy for blood pressure control in hypertensive patients with diabetic and non-diabetic renal impairment? Cardiovascular Diabetology, 11(1), 32. http://doi.org/10.1186/1475-2840-11-32
- Munger, M. A. (2011). Use of Angiotensin receptor blockers in cardiovascular protection: current evidence and future directions. P & T : A Peer-Reviewed Journal for Formulary Management, 36(1), 22–40. Retrieved from http://www.ncbi.nlm.nih.gov/pubmed/21386934
- //www.ncbi.nlm.nih.gov/pubmed/21386934
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