Generic
Amlodipine Besilate + Olmesartan Medoxomil
Pharmacology
Amlodipine is a dihydropyridine calcium channel blocker that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Amlodipine has a greater effect on vascular smooth muscle cells than on cardiac muscle cells. 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. Angiotensin II formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE), 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. Olmesartan Medoxomil blocks 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). In vitro binding studies indicate that Olmesartan Medoxomil is a reversible, competitive inhibitor of the AT1 receptor. Olmesartan Medoxomil does not inhibit ACE (kinase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin).
Dosage Administration
Substitute individually titrated components for patients on Amlodipine and Olmesartan Medoxomil. This combination may also be given with increased amounts of Amlodipine, Olmesartan Medoxomil, or both, as needed. Initial therapy: Initiate with 5/20 mg once daily for 1 to 2 weeks and titrate as needed up to a maximum of 10/40 mg once daily. Due to decreased clearance of Amlodipine among elderly patients the recommended starting dose of Amlodipine is 2.5 mg in patients 75 years. The lowest dose of the combination is 5/20 mg; therefore, initial therapy with this combination drug is not recommended in patients >75 years old.
Contraindications
Pregnancy Category D. Amlodipine and Olmesartan Medoxomil combination should not be used in 2nd and 3rd trimester because it can cause fetal death. When pregnancy is detected this combination should be discontinued as soon as possible. It is not known whether Olmesartan and Amlodipine are excreted in human milk. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Side Effects
Amlodipine and Olmesartan Medoxomil combination should be used with caution because there is a risk for- Hypotension in volume- or salt depleted patients. Vasodilation in patients with severe aortic stenosis. Increased frequency, duration or severity of angina or acute Ml in patients with severe obstructive coronary artery disease.
Pregnancy And Lactation
Pediatric use: The safety and effectiveness have not been established in pediatric patients. Geriatric use: No overall differences in safety or effectiveness were observed between subjects 65 years of age or older and younger subjects. Renal impairment: There are no studies in patients with renal impairment. Hepatic impairment: Initial therapy is not recommended in hepatically impaired patients.
Therapeutic
Pediatric use: The safety and effectiveness have not been established in pediatric patients. Geriatric use: No overall differences in safety or effectiveness were observed between subjects 65 years of age or older and younger subjects. Renal impairment: There are no studies in patients with renal impairment. Hepatic impairment: Initial therapy is not recommended in hepatically impaired patients.
Storage Conditions
There is no information on over dosage in humans.
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