ARBLOC CCB Amlodipine Besilate / Losartan Potassium 5mg / 50mg Film-Coated Tablet 1's
RXDRUG-DRP-5685-01-1pc
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Used in the treatment of mild to moderate hypertension in case of inadequate control with monotherapy.
Dosage/Direction for Use
Usual initial dose is one (1) tablet daily. Increased if necessary to two (2) tablets daily or as prescribed by the physician.
Similar doses are given in the treatment of stable angina and Prinzmetal's angina or as prescribed by the physician.
Similar doses are given in the treatment of stable angina and Prinzmetal's angina or as prescribed by the physician.
Overdosage
Amlodipine overdosage can cause excessive peripheral vasodilation with marked hypotension and possibly a reflex tachycardia. If overdosage occurs, initiate active cardiac and respiratory monitoring. Frequent blood pressure measurements are essential. Should hypotension occur, provide cardiovascular support including elevation of the extremities and the judicious administration of fluids. If hypotension remains unresponsive to these conservative measures, consider administration of vasopressors (such as phenylephrine) with attention to circulating volume and urine output. As amlodipine is highly protein bound, hemodialysis is not likely to be of benefit.
Losartan manifestation of overdosage would be hypotension and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If sympathomimetic hypotension should occur, supportive treatment should be instituted. Neither losartan nor its metabolite can be removed by hemodialysis.
Losartan manifestation of overdosage would be hypotension and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If sympathomimetic hypotension should occur, supportive treatment should be instituted. Neither losartan nor its metabolite can be removed by hemodialysis.
Administration
May be taken with or without food.
Contraindications
5 mg/100 mg FC tab: Amlodipine (as besilate) and Losartan potassium: Patients with hypersensitivity reaction to any components of this product.
Warnings
5 mg/50 mg FC tab: Hypersensitivity to any component of this product.
Special Precautions
Amlodipine should be used with caution in patients with hypotension, in patients whose cardiac reserve is poor, and in those with heart failure has been noted. It should not be used in cardiogenic shock, in patients who have recently suffered a myocardial infarction, or in acute unstable angina. It should not be used to treat an angina attack in chronic stable angina. In patients with severe aortic stenosis it may increase the risk of developing heart failure. Sudden withdrawal might be associated with an exacerbation of angina. The dose may need to be reduced in patients with hepatic impairment. It should be discontinued in patients who experience ischaemic pain following its administration.
Losartan is contraindicated in pregnancy and should be used with care, if at all, during breast feeding. It should be used with caution in patients with renal artery stenosis. Reduced doses may be required in patients with renal impairment and should be considered in patients with hepatic impairment. Patients with volume depletion (for example those who have received high-dose diuretic therapy) may experience hypotension, which may be minimized by initiating treatment with a low dose of Losartan. Since hyperkalaemia may occur, serum potassium concentrations should be monitored, especially in the elderly and patients with renal impairment, and the concomitant use of potassium-sparing diuretics should be generally be avoided.
Losartan is contraindicated in pregnancy and should be used with care, if at all, during breast feeding. It should be used with caution in patients with renal artery stenosis. Reduced doses may be required in patients with renal impairment and should be considered in patients with hepatic impairment. Patients with volume depletion (for example those who have received high-dose diuretic therapy) may experience hypotension, which may be minimized by initiating treatment with a low dose of Losartan. Since hyperkalaemia may occur, serum potassium concentrations should be monitored, especially in the elderly and patients with renal impairment, and the concomitant use of potassium-sparing diuretics should be generally be avoided.
Use In Pregnancy & Lactation
Amlodipine: There are no adequate and well-controlled studies in pregnant women. Amlodipine should be used during pregnancy only if the potential benefit justifies the risk to the fetus. It is not known whether Amlodipine is excreted in human milk. In the absence of this information, it is recommended that nursing be discontinued.
Losartan: Drugs that act directly on the renin-angiotensin system can cause fetal and neonatal morbidity and death when administered to pregnant women. When pregnancy is detected, Losartan potassium should be discontinued, as soon as possible. It is not known whether Losartan potassium is excreted in human milk. It is recommended that nursing be discontinued.
Losartan: Drugs that act directly on the renin-angiotensin system can cause fetal and neonatal morbidity and death when administered to pregnant women. When pregnancy is detected, Losartan potassium should be discontinued, as soon as possible. It is not known whether Losartan potassium is excreted in human milk. It is recommended that nursing be discontinued.
Adverse Reactions
Adverse effects of Losartan have been reported to be usually mild and transient, and include dizziness, headache, and dose-related orthostatic hypotension. Hypotension may occur particularly in patients with volume depletion (for example those who have received high-dose diuretics). Impaired renal function and, rarely, rash, angioedema, and raised liver enzyme values may occur. Hyperkalaemia, myalgia and arthralgia have been reported. Losartan appears less likely than ACE inhibitors to cause cough. Other adverse effects that have been reported with angiotensin II receptor antagonists include respiratory-tract disorders, back pain, gastrointestinal disturbances, fatigue, and neutropenia.
The most common adverse effects of amlodipine are associated with its vasodilator action and often diminish on continued therapy. They include dizziness, flushing, headache, hypotension, peripheral edema, tachycardia and palpitations. Nausea and other gastrointestinal disturbances, increased micturition frequency, lethargy, eye pain, and mental depression have also occurred. A paradoxical increase in ischaemic chest pain may occur at the start of treatment and in few patients excessive fall in blood pressure has led to cerebral or myocardial ischaemia or transient blindness. There have been reports of rashes (including erythema multiforme), fever, and abnormalities in liver function, including cholestasis, due to hypersensitivity reactions. Gingival hyperplasia, myalgia, tremor and impotence have been reported.
Overdose may be associated with bradycardia and hypotension; hyperglycemia, metabolic acidosis, and coma may also occur.
The most common adverse effects of amlodipine are associated with its vasodilator action and often diminish on continued therapy. They include dizziness, flushing, headache, hypotension, peripheral edema, tachycardia and palpitations. Nausea and other gastrointestinal disturbances, increased micturition frequency, lethargy, eye pain, and mental depression have also occurred. A paradoxical increase in ischaemic chest pain may occur at the start of treatment and in few patients excessive fall in blood pressure has led to cerebral or myocardial ischaemia or transient blindness. There have been reports of rashes (including erythema multiforme), fever, and abnormalities in liver function, including cholestasis, due to hypersensitivity reactions. Gingival hyperplasia, myalgia, tremor and impotence have been reported.
Overdose may be associated with bradycardia and hypotension; hyperglycemia, metabolic acidosis, and coma may also occur.
Drug Interactions
Amlodipine: Amlodipine may enhance the antihypertensive effects of other antihypertensive drugs such as beta blockers although the combination is generally well tolerated. Enhanced antihypertensive effects may also be seen if used with drugs such as aldesleukin and antipsychotics that can cause hypotension. Amlodipine may modify insulin and glucose responses and therefore diabetic patients may need to adjust their antidiabetic treatment when receiving amlodipine. Amlodipine is extensively metabolized in the liver by the cytochrome P450 isoenzyme CYP3A4, and interactions may occur with other drugs, such as quinidine, sharing the same metabolic pathway, and with enzyme inducers, such as carbamazepine, phenytoin, and rifampicin, and enzyme inhibitors, such as cimetidine, erythromycin, and HIV-protease inhibitors.
Losartan: The antihypertensive effects of losartan may be potentiated by drugs or other agents that lower blood pressure. An additive hyperkalemic effect is possible with potassium supplements, potassium-sparing diuretics, or other drugs that can cause hyperkalemia; losartan and potassium-sparing diuretics should not generally be given together. NSAIDs should be used with caution in patients taking losartan as the risk of renal impairment may be increased, particularly in those who are inadequately hydrated; use of NSAIDs may also attenuate the hypotensive effect of losartan. Losartan and some other angiotensin II receptor antagonists are metabolized by cytochrome P450 isoenzymes and interactions may occur with drugs that affect these enzymes.
Losartan: The antihypertensive effects of losartan may be potentiated by drugs or other agents that lower blood pressure. An additive hyperkalemic effect is possible with potassium supplements, potassium-sparing diuretics, or other drugs that can cause hyperkalemia; losartan and potassium-sparing diuretics should not generally be given together. NSAIDs should be used with caution in patients taking losartan as the risk of renal impairment may be increased, particularly in those who are inadequately hydrated; use of NSAIDs may also attenuate the hypotensive effect of losartan. Losartan and some other angiotensin II receptor antagonists are metabolized by cytochrome P450 isoenzymes and interactions may occur with drugs that affect these enzymes.
Storage
Store at temperatures not exceeding 30°C.
Action
Pharmacology: Pharmacodynamics: Mechanism of Action: Amlodipine is a dihydropyridine calcium channel blocker (CCB) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Serum calcium concentration is not affected by Amlodipine. Within the physiologic pH range, Amlodipine is an ionized compound (pKa=8.6), and its kinetic interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect.
Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
Losartan potassium is an angiotensin II receptor (Type AT1) antagonist. Angiotensin II [formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)], is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland).
Pharmacokinetics: Amlodipine is well absorbed following oral administration with peak blood concentrations occurring after 6 to 12 hours. The bioavailability is about 60 to 65%. Amlodipine is reported to be about 97.5% bound to plasma proteins. It has a prolonged terminal elimination half-life of 35 to 50 hours and steady-state plasma concentrations are not achieved until after 7 to 8 days of administration. Amlodipine is extensively metabolized in the liver; metabolites are mostly excreted in urine together with less than 10% of dose as unchanged drug.
Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
Losartan potassium is an angiotensin II receptor (Type AT1) antagonist. Angiotensin II [formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)], is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland).
Pharmacokinetics: Amlodipine is well absorbed following oral administration with peak blood concentrations occurring after 6 to 12 hours. The bioavailability is about 60 to 65%. Amlodipine is reported to be about 97.5% bound to plasma proteins. It has a prolonged terminal elimination half-life of 35 to 50 hours and steady-state plasma concentrations are not achieved until after 7 to 8 days of administration. Amlodipine is extensively metabolized in the liver; metabolites are mostly excreted in urine together with less than 10% of dose as unchanged drug.
MedsGo Class
Angiotensin II Antagonists / Calcium Antagonists
Features
Brand
Arbloc CCB
Full Details
Dosage Strength
5 mg / 50 mg
Drug Ingredients
- Amlodipine
- Losartan Potassium
Drug Packaging
Film-Coated Tablet 1's
Generic Name
Losartan Potassium / Amlodipine Besilate
Dosage Form
Film-Coated Tablet
Registration Number
DRP-5685-01
Drug Classification
Prescription Drug (RX)
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