Besanta

BESANTA 150 MG TABLET: Each tablet contains Irbesartan 150 mg.
BESANTA 300 MG TABLET: Each tablet contains Irbesartan 300 mg .

Pharmacology: Pharmacodynamics: Irbesartan is an anti-hypertensive drug, classified as Angiotensin II type 1 (AT 1) receptor antagonist. Angiotensin II is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system. Its effects are vasoconstriction, stimulations of synthesis and release of aldosterone and re-absorption of sodium there are important component in the pathophysiology of hypertension. Angiotensin II receptor antagonist block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II at the AT₁ receptor in many tissues; for such, vascular smooth muscle and adrenal gland. Irbesartan does not inhibit ACE, the drug does not interfere with response to bradykinins and substance P.
Pharmacokinetics: The bioavailability of Irbesartan is 60-80% after the oral administration; food has no effect in the absorption. The peak plasma concentration of the drug is within 1.5-2 hours and 90% bind to plasma protein. Less than 20% of the drug is converted to inactive metabolites via CYP2C9. The half-life of the drug is 11-15 hours and the the steady concentration is within 3 days after the first dose. The drug is excreted 20% in urine and 80% in feces; while, less than 2% of the dose is excreted in the urine as unchanged form. Irbesartan is not removed by hemodialysis.

Use for the treatment of hypertension.
For the treatment of diabetic nephropathy in patients with type 2 diabetes mellitus and hypertension.

Irbesartan can be used alone or with other anti-hypertensive agents. Irbesartan can be administering with or without food. The condition of intravascular volume depletion or sodium depletion should be corrected before the administration of the drug.
For the treatment of hypertension: Dosage in adults: The recommended initial and maintenance dose is 150 mg once daily.
In case of uncontrolled hypertension with 150 mg once daily, the dose can be titrated up to 300 mg once daily or adding low dose diuretic; for such, hydrochlorothiazide, as it has been shown to have an additive effect.
The use in elderly aged more than 75 years old, patients undergoing hemodialysis and patients with volume and sodium depletion, the initial dose is 75 mg once daily. Patients not adequately treated by the maximum dose of 300 mg once daily are unlikely to derive additional benefit from a higher dose or twice-daily dosing.
Diabetic nephropathy: Therapy should be initiated at 150 mg once daily and titrated up to 300 mg daily as the preferred maintenance dose for treatment of renal disease. It can be used along with other diuretics, such as, hydrochlorothiazide.
Dosage in elderly: In patients aged more than 75 years old, the initial dose is 75 mg once daily. Dosage adjustment in elderly is not always necessary.
Dosage in children: Safety and efficacy profile of Irbesartan have not been established in children.
Dosage in renal impairment: No dosage adjustment is needed in patients with impaired renal function. An initial dose of 75 mg should be considered in volume depleted and undergoing hemodialysis patients.
Dosage in hepatic impairment: No dosage adjustment is needed in mild and moderate hepatic function impairment. However, the reports and studies on the used of the drug in severe hepatic function impairment have not been established.

Symptoms: Hypotension, dizziness, tachycardia, bradycardia.
Treatment: There is no antidote for Irbesartan toxicities, therefore, gastric lavage and administration activated charcoal should be implemented. The patients should be closely monitored on cardiovascular system and respiratory function and other supportive treatment should be instituted. Irbesartan is not removed by hemodialysis.

Irbesartan is contraindicated in patients with hypersensitivity to this drug and its components and history of hypersensitivity to Angiotensin II type 1 (AT₁) receptor antagonist. Do not use the drug in pregnant women in second and third semester; and also in nursing mother.

1. Do not use the drug during pregnancy.
2. Consult the physician if the symptoms of nausea and vomiting occurred.
3. If the face, tongue and lips edema or dyspnea occurred, discontinue the drug and consult physician.
4. The drug can caused renal failure; therefore it should be used with caution.
5. The drug may increase potassium level, therefore, it should not be used in patients who received potassium supplement or who recently used potassium sparing diuretics.

In patients with intravascular volume depletion; for such, patients who treated with diuretics, restriction of sodium intake, diarrhea or vomiting, hypotension may occur. Correct these conditions prior to administration under close medical care and dose reduction.
As a consequence of inhibiting the renin-angiotensin-aldosterone system, Irbesartan may lead to renal artery stenosis resulting in severe hypotension and renal insufficiency.
When the drug is used in patients with impaired renal function and kidney transplantation, a frequent monitoring of potassium and creatinine level is recommended.
The drug is not recommended to use in patients with primary aldosteronism due to the renin-angiotensin-aldosterone effect.
As the renin-angiotensin-aldosterone effect, Irbesartan may increase serum potassium level, especially in renal impairment or heart failure. Close monitoring of serum potassium in patients at risk is advised.
The drug should be used with caution in patients with aortic, mitral valve stenosis and obstructive hypertrophic cardiomyopathy.
Angiotensin antagonists are apparently less effective in lowering blood pressure in black people than in non-blacks, possibly because of low renin states in this population.

Use in pregnancy: Do not use the drug during pregnancy. Stop taking Irbesartan immediately when detected pregnancy.
Use in lactation: It is not known whether the drug is excreted in human breast milk or not, therefore the drug should be avoid during breast feeding.

Adverse reactions which may occur during the use of the drug are: CNS: dizziness, headache, insomnia, fatigue, anxiety, depression, tremor, loss of sensation.
CVS: tachycardia, flushing, hypertension, angina pectoris.
Gastrointestinal tract: diarrhea, anorexia, heartburn, vomiting, abdominal pain, taste perversion, constipation, flatulence, mouth ulcer.
Musculoskeletal: joint and muscle pain, joint injury.
Respiratory tract: upper respiratory tract infection, cough, sinusitis, pharyngitis, rhinitis, influenza-like symptoms, bronchitis.
Dermatology: rash, urticaria, skin inflammation.
Others: malaise, increase creatinine kinase, increase potassium level, hepatitis, jaundice, renal failure, chest pain, angioedema, urinary tract infection, tinnitus, decrease libido, edema, cramp, heart failure.

Irbesartan can be used along with other anti-hypertensive agents; for such, β-blockers, calcium channel blocker and thiazide diuretic, for synergistic effect. However, the treatment of high dose diuretic may result in volume depletion and a risk of hypotension and therefore it should be used with caution.
The use of Irbesartan with potassium-sparing diuretic; such as, spironolactone, triamterene, amiloride potassium supplements may increase serum potassium level. Therefore avoid coadministration of these agents.
Coadministration of Irbesartan and lithium will increase lithium concentration resulting in toxicities. Therefore, this combination is not recommended. If the therapy is necessary, a close monitoring of lithium level is advised.
Administration of Irbesartan simultaneously with NSAIDs may reduce anti-hypertensive efficacy and worsen renal function, including acute renal failure. Moreover, it will increase serum potassium level, especially, in patients with history of renal function impairment.

Store below 30°C.

Angiotensin II Antagonists

C09CA04 - irbesartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.

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