Pharmacology Department

1. Pharmacology Department,
Faculty Of Pharmacy,
Helwan University.
Designed By,
Ahmed Kamal Abdel Aziz

2. Content:
 Trade Names.
 Drug Description.
 Dosage Forms.
 Pharmacodynamic (Pharmacological Mechanisms).
 Pharmacokinetics.
 Indications And Usage.
 Drug-drug Interactions .
 Drug-food Interactions.
 Side Effects.
 Overdose.
 Contraindications.
 Storage.

3. Trade Names:
Avalide®
 Avapro®
 Aprovel ®
 Karvea ®

4. Dosage Forms:
 Tablets 75 mg
 Tablets 150 mg
 Tablets 300 mg

5. Market-share
 Percentages of patients receiving various irbesartan (± HCT)
dosages at study entry (n = 72 479). HCT = hydrochlorothiazide

6. Pharmacological Mechanisms
(Pharmacodynamic):
 Antagonizes the effect of angiotensin II
(vasoconstriction and aldosterone secretion)
by blocking the angiotensin II (AT1 receptor) in vascular smooth
muscle and the adrenal gland, producing decreased BP

8. Combination with diuretic
 Irbesartan is also available in a combination
formulation with a low dose thiazide diuretic,
invariably hydrochlorothiazide, to achieve an
additive antihypertensive effect.
Hydrochlorothiazide
Irbesartan/hydrochlorothiazide combination preparations are
marketed under similar trade names to irbesartan preparations,
including
Irda, CoIrda, CoAprovel, Karvezide, Avalide and
Avapro HCT.

9. Pharmacokinetics:
 Absorption:
The mean absolute bioavailability is:
60% to 80%.
The T max is 1.5 to 2 h.
Food does not affect the bioavailability of irbesartan.

10. Pharmacokinetics,
(continue)
 Distribution:
90% is protein bound.
Weakly crosses blood-brain barrier and
placenta.

11. Pharmacokinetics,
(continue)
 Metabolism:
Less than 20% converted to metabolites, primarily via CYP2C9.
 Elimination:
Renal clearances is 3 to 3.5 mL/min.
The mean t ½ is 11 to 15 h.
Approximately, 20% is eliminated in the
urine and 80% in the feces.

12. Indications and Usage
 Treatment of hypertension.
Maximum antihypertensive effects are attained
within 2 to 4 weeks after a change in dose.

13. Drug-Drug interactions :
 No significant drug-drug pharmacokinetic (or
pharmacodynamic) interactions have been found in
interaction studies with :
 Hydrochlorothiazide, a diuretic and antihypertensive drug.
 Digoxin, cardiotonic steroid .
 Warfarin, anticoagulant.
 Nifedipine, a calcium channel blocker .
 Lithium :
However,
Plasma concentrations my be increased by irbesartan,
resulting in an increase in the pharmacologic and adverse
effects of lithium

15. Drug-Food interactions:
 The chances of an interaction with Avapro are low.
Avalide may be administered with or without food.

16. Side Effects:
 Several potential side
effects may develop with the
use of Avapro.
 Side effects that were most
commonly reported include :
diarrhea,
heartburn,
dizziness,
and fatigue.

17. OVERDOSE
No data are available in regard to
over dosage in humans.
 However, daily doses of 900 mg for
8 weeks were well-tolerated.
 The most likely manifestations of
over dosage are expected to be :
hypotension and tachycardia;
bradycardia might also occur from overdose.
Irbesartan is not removed by hemodialysis.

18. Contraindications:
 Avapro® (irbesartan) is contraindicated in
patients who are hypersensitive to any component
of this product.
However,
Because of the hydrochlorothiazide component,
this product is contraindicated in patients with :
 Anuria ,
 Hypersensitivity to other sulfonamide-derived
drugs.

19. WARNING:
USE IN PREGNANCY
When pregnancy is detected, discontinue AVALIDE as soon as
possible.
When used in pregnancy during the second and third trimesters,
drugs that act directly on the renin-angiotensin system can
cause injury and even death to the developing fetus.

20. Storage
 Store at 25°C (77°F);
 excursions permitted to 15°C - 30°C (59°F - 86°F)

21. http://www.medicineonline.com/drugs/A/2137/AV
References APRO-irbesartan-Tablets.html
^ Lewis EJ, Hunsicker LG, Clarke WR, Berl T, Pohl MA, Lewis JB, Ritz E,
Atkins RC, Rohde R, Raz I; Collaborative Study Group. (2001).
"Renoprotective effect of the angiotensin-receptor antagonist irbesartan in
patients with nephropathy due to type 2 diabetes". N Engl J Med 345 (12):
851–60. doi:10.1056/NEJMoa011303. PMID 11565517.
^ Rossi S, editor. Australian Medicines Handbook 2006. Adelaide:
Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3
^ Massie BM, Carson PE, McMurray JJ, Komajda M, McKelvie R, Zile MR,
Anderson S, Donovan M, Iverson E, Staiger C, Ptaszynska A (December
2008). "Irbesartan in patients with heart failure and preserved ejection
fraction". N. Engl. J. Med. 359 (23): 2456–67. doi:10.1056/NEJMoa0805450.
PMID 19001508.

22. Team,
Students from No. 3011-3020
 Ahmed Salah Mohamed 2011
 Ahmed Adel Ibrahim 2012
 Ahmed Abdel Aziz El-beltagi 2013
 Ahmed Abdel Mohsen 2014
 Ahmed Alaa El-dien Ahmed 2015
 Ahmed Fathi Abdel Samee’a 2016
 Ahmed Fawzy Selim 2017
 Ahmed Karim El-dien Zaki 2018
 Ahmed Kamal Abdel Aziz 2019
 Ahmed Maher Ismael 2020