Irbesartan; Uses, Dosage, Side Effects, Interactions, Pregnancy

Irbesartan, Irbesartan; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun
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Irbesartan is a nonpeptide angiotensin II antagonist with antihypertensive activity. Irbesartan selectively and competitively blocks the binding of angiotensin II to the angiotensin I receptor. Angiotensin II stimulates aldosterone synthesis and secretion by adrenal cortex, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle.
Irbesartan is an angiotensin II receptor blocker used alone or in combination with other agents in the therapy of hypertension and diabetic nephropathy. Irbesartan is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury.

Irbesartan is an angiotensin receptor blocker (ARB) used mainly for the treatment of hypertension. It competes with angiotensin II for binding at the AT1 receptor subtype. Unlike ACE inhibitors, ARBs do not have the adverse effect of dry cough. The use of ARBs is pending revision due to findings from several clinical trials suggesting that this class of drugs may be associated with a small increased risk of cancer.

Mechanism of Action of Irbesartan

Irbesartan is a nonpeptide tetrazole derivative and an angiotensin II antagonist that selectively blocks the binding of angiotensin II to the AT1 receptor. In the renin-angiotensin system, angiotensin I is converted by angiotensin-converting enzyme (ACE) to form angiotensin II. Angiotensin II stimulates the adrenal cortex to synthesize and secrete aldosterone, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle. Irbesartan, by blocking the binding of angiotensin II to the AT1 receptor, promotes vasodilation and decreases the effects of aldosterone. The negative feedback regulation of angiotensin II on renin secretion is also inhibited, but the resulting rise in plasma renin concentrations and consequent rise in angiotensin II plasma concentrations do not counteract the blood pressure–lowering effect that occurs. The action of ARBs is different from ACE inhibitors, which block the conversion of angiotensin I to angiotensin II, meaning that the production of angiotensin II is not completely inhibited, as the hormone can be formed via other enzymes. Also, unlike ACE inhibitors, irbesartan and other ARBs do not interfere with response to bradykinins and substance P, which allows for the absence of adverse effects that are present in ACE inhibitors (eg. dry cough).

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Indications of Irbesartan

Therapeutic Indications of Irbesartan

  • Irbesartan is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
  • Irbesartan is indicated for the treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria (>300 mg/day) in patients with type 2 diabetes and hypertension.
  • In this population,  Irbesartan reduces the rate of progression of nephropathy as measured by the occurrence of doubling of serum creatinine or end-stage renal disease (need for dialysis or renal transplantation).
  • Angiotensin II receptor antagonists including irbesartan have been used in the management of congestive heart failure.
  • Treatment of essential hypertension.
  • Treatment of renal disease in patients with hypertension and type 2 diabetes mellitus as part of an antihypertensive medicinal product regimen (see section 5.1).
  • Treatment of essential hypertension.
  • Treatment of renal disease in patients with hypertension and type 2 diabetes mellitus as part of an antihypertensive medicinal product regimen.
  • Irbesartan is an angiotensin II receptor antagonist indicated for the treatment of hypertension. It may be used either alone or in combination with other antihypertensive agents (ie, thiazide diuretics, beta-adrenergic blocking agents, and long-acting calcium-channel blocking agents).
  • Irbesartan is also indicated for the treatment of renal disease in patients with hypertension and type 2 diabetes mellitus. Irbesartan is available in the following formulations: 75, 100, 150, or 300 mg unscored or film-coated tablets for oral administration.
  • The usual recommended initial and maintenance dose is 150mg once daily, with or without food. However, initiation of therapy with 75 mg could be considered, particularly in haemodialysed patients and in the elderly over 75 years. In patients insufficiently controlled with 150 mg once daily, the dose of irbesartan can be increased to 300 mg, or other antihypertensive agents can be added.
  • In hypertensive type 2 diabetic patients, therapy should be initiated at 150 mg of irbesartan once daily and titrated up to 300 mg once daily as the preferred maintenance dose for treatment of renal disease.
  • Treatment of essential hypertension – Treatment of renal disease in patients with hypertension and type 2 diabetes mellitus as part of an antihypertensive medicinal product regimen
  • Irbesartan is indicated in adults for the treatment of essential hypertension.
  • It is also indicated for the treatment of renal disease in adult patients with hypertension and type 2 diabetes mellitus as part of an antihypertensive medicinal product regimen.
  • Irbesartan  is indicated in adults for the treatment of essential hypertension.It is also indicated for the treatment of renal disease in adult patients with hypertension and type 2 diabetes mellitus as part of an antihypertensive medicinal product regimen.
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Contra Indications of Irbesartan

  • Low amount of sodium in the blood
  • High amount of potassium in the blood
  • Decreased Neutrophils a Type of White Blood Cell
  • Renal Artery Stenosis
  • Abnormally low blood pressure
  • Liver problems
  • Severe renal impairment
  • Pregnancy
  • Decreased Blood Volume

Dosage of Irbesartan

Strengths

Tablet : 75mg ,150mg  ,300mg

Hypertension

150 mg/day PO initially; may be increased to 300 mg/day PO

Hypovolemia: 75 mg/day PO initially

Nephropathy in Type 2 Diabetes

75-300 mg/day PO

Side Effects of Irbesartan

The most common 

Common

Rare

Drug Interactions of Irbesartan

Irbesartan may interact with following drugs, supplements, & may change the efficacy of drugs

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Pregnancy & Lactation of Irbesartan

Pregnancy

This drug has a black box warning. This is the most serious warning from the Food and Drug Administration (FDA). A black box warning alerts doctors and patients about drug effects that may be dangerous. Don’t take this drug if you’re pregnant or plan to become pregnant. Irbesartan can harm or end your pregnancy. If you get pregnant while taking this drug, tell your doctor right away.

Lactation

Because no information is available regarding the use of irbesartan breastfeeding-feeding, Irbesartan Milpharm is not recommended and alternative treatments with better established safety profiles during breast-feeding are preferable, especially while nursing a newborn or preterm infant. It is unknown whether irbesartan or its metabolites are excreted in human milk. Available pharmacodynamic/toxicological data in rats have shown excretion of irbesartan or its metabolites in milk

Irbesartan had no effect upon the fertility of treated rats and their offspring up to the dose levels inducing the first signs of parental toxicity.

References

Irbesartan, Irbesartan; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun

Irbesartan, Irbesartan; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun

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