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All about: Irbesartan

Big Image Pronouncation: (ihr-beh-SAHR-tan)
Class: Angiotensin II receptor antagonist

Trade Names:
Avapro
- Tablets 75 mg
- Tablets 150 mg
- Tablets 300 mg

Mechanism of Action

Pharmacology

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.

Pharmacokinetics

Absorption

The mean absolute bioavailability is 60% to 80%. The T max is 1.5 to 2 h.

Distribution

90% is protein bound. The mean Vd is 53 to 93 L. Weakly crosses blood-brain barrier and placenta.

Metabolism

Less than 20% converted to metabolites, primarily via CYP2C9.

Elimination

Renal Cl 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.

Peak

4 h.

Duration

24 h.

Indications and Usage

Treatment of hypertension; nephropathy in type 2 diabetes.

Contraindications

Standard considerations.

Dosage and Administration

Hypertension
Adults

PO Start with 150 mg every day; then titrate to 300 mg every day as necessary.

Children (13 to 16 yr of age)

PO Start with 150 mg every day; then titrate patients requiring a further reduction in BP to 300 mg every day.

Children (6 to 12 yr of age)

PO Start with 75 mg every day; then titrate patients requiring a further reduction in BP to 150 mg every day.

Nephropathy in Type 2 Diabetes
Adults

PO Titrate dose to 300 mg every day.

Volume- and Salt-Depleted Patients

PO Start with 75 mg.

General Advice

Give prescribed dose with or without food.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F).

Drug Interactions

Lithium

Plasma concentrations my be increased by irbesartan, resulting in an increase in the pharmacologic and adverse effects of lithium.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Chest pain; tachycardia; edema.

CNS

Headache; anxiety/nervousness; dizziness.

GI

Diarrhea; dyspepsia/heartburn; abdominal pain; nausea/vomiting.

Respiratory

Upper respiratory tract infection; influenza; pharyngitis; rhinitis; sinus abnormality

Miscellaneous

Musculoskeletal pain/trauma; fatigue; UTI; rash.

Precautions

Warnings

Pregnancy

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. When pregnancy is detected, discontinue therapy as soon as possible.


Pregnancy

Category C (first trimester); Category D (second and third trimesters).

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 6 yr of age.

Renal Function

Use with caution in patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (eg, patients with severe CHF); use may be associated with oliguria, progressive azotemia, acute renal failure, and death.

Hypotension

Initiation of antihypertensive therapy may cause symptomatic hypotension in patients with intravascular volume or sodium-depletion.

Patient Information

  • Advise patient to take prescribed dose once daily, without regard to meals.
  • Advise patient to try to take each dose at about the same time each day.
  • Inform patient that drug controls, but does not cure, hypertension, and to continue taking drug as prescribed even when BP is not elevated.
  • Caution patient not to change the dose or stop taking unless advised by health care provider.
  • Instruct patient in BP and pulse measurement skills.
  • Advise patient to monitor and record BP and pulse at home and to inform health care provider should abnormal measurements be noted. Also advise patient to take record of BP and pulse to each follow-up visit.
  • Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
  • Instruct patient to lie or sit down if they experience dizziness or lightheadedness when standing.
  • Caution patient that inadequate fluid intake, excessive perspiration, diarrhea, or vomiting can lead to excessive fall in BP, resulting in lightheadedness or fainting.
  • Emphasize to hypertensive patient importance of other modalities on BP: weight control, regular exercise, smoking cessation, moderate intake of alcohol and salt.
  • Instruct patient to stop taking drug and immediately report any of these symptoms to health care provider: fainting; swelling of the face, lips, eyelids, or tongue.

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