Prescription Drug Information: Avapro
Avapro contains the active ingredient, Irbesartan, a non-peptide compound, which is classified as an angiotensin II receptor antagonist. Avapro is used for the treatment of high blood pressure, both as monotherapy and combination therapy. Irbesartan lowers blood pressure by dilating blood vessels. Avapro is also for the treatment of kidney disorders caused by type 2 diabetes. A prescription drug, manufactured and marketed by Bristol-Myers Squibb, Avapro is not yet available in generic form.
Doctors prescribe Avapro to treat high blood pressure. This medication is also used to slow the progression of diabetic nephropathy, or kidney damage, which occurs as a result of prolonged periods of high blood sugar in individuals with type 2 diabetes.
Avapro is an angiotensin II receptor blocker. As these receptors become blocked, the capability of angiotensin II becomes limited and it can no longer operate effectively in the body. Since this chemical causes blood vessels to become smaller, continued treatment with Avapro will help to keep blood vessels from narrowing. Blood pressure will lower over time, as will the risk for heart attack and stroke.
Indication/Usage: Avapro has been approved for the treatment of the following indications:
- Hypertension/High blood pressure: Avapro is indicated for the treatment of high blood pressure (hypertension) both for monotherapy and combination therapy.
- Type 2 diabetes associated nephropathy: Avapro is indicated in patients with type 2 diabetes, hypertension and microalbuminuria for the treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria.
- Avapro also delays the nephropathy progression in patients with type 2 diabetes and hypertension which is measured by the increased serum creatinine levels or end-stage renal disease (ESRD).
Dose, Dosage Fprms and Administration: Avapro is available in white to off-white, biconvex oval tablets in 75 mg, 150 mg and 300 mg strengths. It is generally started with a 150 mg daily dose in most hypertensive patients. The recommended dose for the treatment of high blood pressure is 75 mg to 300 mg once per day. For the treatment of diabetic nephropathy, Avapro is generally started with 300 mg daily. Avapro tablets should be stored at room temperature between 15 C to 30 C.
Mechanism of Action: Avapro contains Irbesartan which is an angiotensin 2 receptor antagonist. Angiotensin 2 (AT2) is a strong vasoconstrictor which is synthesized into the body from AT1 to AT2 conversion with the help of the angiotensin-converting enzyme (ACE, kininase II). Irbesartan blocks the vasoconstriction and aldosterone-secreting effects of AT2 by selectively and competitively binding to the AT1 receptors. This AT1 receptor blockade takes away the negative feedback mechanism of AT2 on renin secretion. This entire process results in suppressed AT2 levels at the receptor sites and thus, the vasoconstrictive effects of AT2 are suppressed, leading to vasodilatation and unhindered blood flow in blood vessels.
Irbesartan actually does not act on ACE receptors, renin receptors, and other ion channels involved in natural regulation of blood pressure.
Side-Effects and Safety Profile: Avapro may be associated with various serious side-effects which include: severe allergic reactions like hives, wheezing, dyspnea, swelling on face, lips, tongue, and throat; myocardial infarction, gout, arthritis, joint stiffness, heart failure, renal failure, unexplained muscle pain and tenderness along with fever and dark colored urine, faintness, angina pectoris, altered urination, mood changes, flushing, cardiac murmur, arrhythmia, cardio-respiratory arrest, cerebrovascular accident, hypertensive crisis, vision disturbance, tremor, etc.
Various moderately-serious side-effects possibly associated with Avapro include: confusion, skeletal muscle tissue breakdown, pruritus, swelling, weight gain, loss of appetite, heartburn, erythema, urticaria, sexual dysfunctions, altered libido, muscle cramps, sleep disturbance, prostate disorder, emotional disturbance, congestion, tracheobronchitis, etc.
Avapro is reported to be associated with various non-serious side-effects which include: drowsiness, increased thirst, nausea, diarrhea, constipation, flatulence, vomiting, upset stomach, tiredness, abdominal distention, numbness, etc.
Warning/Contraindications:
- It carries a warning of fetal toxicity; therefore, patients should immediately discontinue the use of Avapro if they become pregnant. Avapro can cause injury and death to the developing fetus.
- Avapro is contraindicated in patients with allergic reactions to Irbesartan.
- Hypotension: Avapro may cause hypotension in patients who are depleted in sodium or intravascular volume, such as patients on vigorous diuretics or on dialysis.
- Avapro should be used with caution in patients with renal disorders.
- Nursing women: Since it is not known whether Irbesartan is excreted via human milk or not, it should not be prescribed to nursing women as it may harm nursing infants.
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