Irbesartan

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Irbesartan.jpg

[edit] MECHANISM OF ACTION

Irbesartan is a member of a family of drugs called angiotensin receptor blockers (ARBs).

Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium.

Irbesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland.

[edit] INDICATIONS

  • Treatment of hypertension
  • To reduce the rate of progression of nephropathy in type 2 diabetes patients with an elevated serum creatinine and proteinuria (≥300 mg/day)

[edit] DOSAGE

  • Hypertension: The recommended initial dose is 150 mg once daily, with or without food. Patients requiring further reduction in blood pressure should be titrated to 300 mg once daily. A low dose of a diuretic (hydrochlorothiazide) may be added, if blood pressure is not controlled by Irbesartan alone.
  • Nephropathy in type 2 diabetes: 300 mg once daily with or without food

[edit] DOSAGE FORMS AND STRENGTHS

Tablets: 75 mg, 150 mg, 300 mg.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity (e.g., anaphylaxis or angioedema) to Irbesartan
  • Pregnancy; Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus
  • Do not co-administer Aliskiren with Irbesartan in patients with diabetes

[edit] PRECAUTIONS

[edit] INTERACTIONS

  • Lithium clearance may be reduced. Serum lithium levels should be monitored carefully.
  • [[NSAIDS]]: Caution is advised if non steroidal antiinflammatory drugs NSAIDs are prescribed with angiotensin II receptor antagonists, including Irbesartan. (Concomitant use of NSAIDS may result in decreased angiotensin II receptor antagonists effectiveness). In some patients with compromised renal function who are being treated with NSAIDS, the co-administration of angiotensin II receptor antagonists may result in further deterioration of renal function. Cases of acute renal failure, usually reversible, have also been reported.
  • Do not co-administer aliskiren with Irbesartan in patients with diabetes
  • Drugs that inhibit the renin-angiotensin system, including Irbesartan, can cause hyperkaliemia. Potassium-sparing diuretics and potassium supplements may have an additive effect on potassium retention, resulting in hyperkalemia.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category D (US). Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus, thus Irbesartan should not be used during pregnancy or in women planning to become pregnant and is not advisable to use in breast-feeding mothers. If pregnancy is detected during therapy, Irbesartan should be discontinued as soon as possible.
  • Nursing Mothers: Choose to discontinue nursing or drug

[edit] SIDE EFFECTS

Possible adverse effects include: headache , dizziness (vertigo), fatigue, nausea/vomiting, hyperkalemia (especially in patients with high blood pressure, type 2 diabetes with kidney impairment), increases in plasma creatine kinase, musculoskeletal pain, orthostatic hypotension,


Rare cases of allergic skin reactions (rash, urticaria), as well as localised swelling of the face, lips and/or tongue have been reported

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)