Indications of Arbitel 40 mg
Arbitel 40 mg is indicated in-Hypertension: Treatment of essential hypertension in adults.Cardiovascular prevention: Reduction of cardiovascular morbidity in adults with:
Atherothrombotic cardiovascular disease (history of coronary heart disease, stroke, or peripheral arterial disease) or
Type 2 diabetes mellitus with documented target organ damage.
Angiotensin-ll receptor blocker
Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Arbitel 40 mg blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis.There is also an AT2 receptor found in many tissues, but AT2 is not known to be associated with cardiovascular homeostasis. Arbitel 40 mg has a much greater affinity ( > 3,000 fold) for the AT1 receptor than for the AT2 receptor.Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because Arbitel 40 mg does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Arbitel 40 mg does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of Arbitel 40 mg on blood pressure.
Dosage of Arbitel 40 mg
Dosage must be individualized. The usual starting dose of Arbitel 40 mg tablets is 40 mg once a day. Blood pressure response is dose-related over the range of 20 to 80 mg. Most of the antihypertensive effect is apparent within 2 weeks and maximal reduction is generally attained after 4 weeks. When additional blood pressure reduction beyond that achieved with 80 mg Arbitel 40 mg is required, may switch to the combination. No initial dosage adjustment is necessary for elderly patients or patients with renal impairment, including those on hemodialysis. Patients on dialysis may develop orthostatic hypotension; their blood pressure should be closely monitored. Arbitel 40 mg tablets may be administered with other antihypertensive agents. Arbitel 40 mg tablets may be administered with or without food. Initial therapy with Arbitel 40 mg is not recommended in patients ≥75 years old or with hepatic impairment.
Administration of Arbitel 40 mg
Arbitel 40 mg tablets may be administered with other antihypertensive agents with or without food.
Interaction of Arbitel 40 mg
NSAIDS: Increased risk of renal impairment and loss of antihypertensive effect.
Co-administration with aliskiren with Arbitel 40 mg: in patients with diabetes should be avoided.
Known hypersensitivity to this product or any of its components.
Side Effects of Arbitel 40 mg
In hypertensive patients: The most common side effects of Arbitel 40 mg tablets include sinus pain and congestion (sinusitis), back pain, diarrhea etc. For patients of cardiovascular risk reduction: The most common side effects of Arbitel 40 mg tablets in CV risk reduction include intermittent claudication and skin ulcer.
Pregnancy & Lactation
Arbitel 40 mg has been assigned to pregnancy categories C (use during first trimester) by the FDA. When pregnancy is detected or expected, Arbitel 40 mg should be discontinued as soon as possible. The use of drugs that act directly on the RAA system during the second and third trimesters has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure and death. There are no data on the excretion of Arbitel 40 mg into human milk, due to the potential for serious adverse effects in the nursing infant, a decision should be made to discontinue nursing or discontinue the drug.
Precautions & Warnings
Avoid fetal or neonatal exposure.
Monitor carefully in patients with impaired hepatic or renal function.
Avoid concomitant use of an ACE inhibitor and angiotensin receptor blocker.
Overdose Effects of Arbitel 40 mg
The most likely manifestation of overdosage with Arbitel 40 mg tablets would be hypotension, dizziness and tachycardia; bradycardia, increase in serum creatinine and acute renal failure could occur from parasympathetic (vagal) stimulation.
Do not store above 30°C. Protect from light and high humidity. Keep out of the reach of children.
Use In Special Populations
Renal Impairment: Severe impairment or on haemodialysis: Initially, 20 mg once daily.Hepatic Impairment: Mild to moderate: Max: 40 mg once daily. Severe: Contraindicated.
Angiotensin-ll receptor blocker
Mode Of Action
Arbitel 40 mg blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis. Arbitel 40 mg has much greater affinity (>3,000 fold) for the AT1 receptor than for the AT2 receptor. Because Arbitel 40 mg does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Arbitel 40 mg does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
Pregnancy Category C (first trimester) and D (second and third trimester). Because of the potential for adverse effects on the nursing infant, decide whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric use: The safety and effectiveness of Arbitel 40 mg in pediatric patients have not been established.Geriatric use: No overall differences in effectiveness and safety were observed in these patients compared to younger patients.Hepatic impairment: Monitor carefully and up titrate slowly in patients with biliary obstructive disorders or hepatic insufficiency.