Irbesartan
Pronunciation: (ihr-beh-SAHR-tan)Class: Angiotensin II receptor antagonist
Trade Names:
Avapro
- Tablets 75 mg
- Tablets 150 mg
- Tablets 300 mg
Pharmacology
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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
HypertensionAdults
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 DiabetesAdults
PO Titrate dose to 300 mg every day.
Volume- and Salt-Depleted PatientsPO 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
LithiumPlasma 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
WarningsPregnancyWhen 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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irbesartan - Includes detailed dosage instructions.
Compare Irbesartan with other medications for the treatment of:
High Blood Pressure, Diabetic Kidney Disease
