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Friday, August 19, 2016

ARB Comparison

  • 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 
 
  Currently approved indication of ARB in the US and EU. 
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 : 
  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. //www.ncbi.nlm.nih.gov/pubmed/21386934

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