Felodipine ER (felodipine)
OTHER BRAND NAMES
Calcium channel blocker (CCB) (dihydropyridine)
Treatment of HTN, alone or concomitantly with other antihypertensive agents, to lower BP.
Initial: 5mg qd
Titrate: May decrease to 2.5mg qd or increase to 10mg qd at intervals of not <2 weeks, depending on the patient's response
Range: 2.5-10mg qd
Initial: 2.5mg qd
Initial: 2.5mg qd
Take regularly either w/o food or w/ a light meal
Swallow whole; do not crush or chew
Tab, Extended-Release: 2.5mg, 5mg, 10mg
May occasionally precipitate significant hypotension and, rarely, syncope. May lead to reflex tachycardia, which may precipitate angina pectoris. Caution with heart failure (HF) or compromised ventricular function, particularly in combination with a β-blocker. Closely monitor BP during dose adjustment in patients with hepatic impairment and in elderly. Peripheral edema reported. Caution in elderly.
Peripheral edema, headache, asthenia, dyspepsia, dizziness, upper respiratory infection, flushing.
CYP3A4 inhibitors (eg, ketoconazole, erythromycin, grapefruit juice, cimetidine) may increase plasma levels by several-fold. Decreased levels with long-term anticonvulsant therapy (eg, phenytoin, carbamazepine, phenobarbital); consider alternative antihypertensive therapy. May increase metoprolol and tacrolimus levels; monitor tacrolimus blood concentration and adjust tacrolimus dose if needed.
PREGNANCY AND LACTATION
Category C, not for use in nursing.
MECHANISM OF ACTION
Calcium channel blocker (dihydropyridine); reversibly competes with nitrendipine and/or other calcium channel blockers for dihydropyridine binding sites and blocks voltage-dependent Ca2+ currents in vascular smooth muscle.
Absorption: Almost complete. Systemic bioavailability (20%); Cmax=23nmol/L (20mg); Tmax=2.5-5 hrs. Distribution: Vd=10L/kg; plasma protein binding (>99%). Metabolism: Extensive 1st-pass. Elimination: Urine (70%), feces (10%); T1/2=11-16 hrs (immediate-release).
Assess for hypersensitivity to the drug, HF, compromised ventricular function, hepatic impairment, pregnancy/nursing status, and possible drug interactions.
Monitor for syncope, angina pectoris, peripheral edema, and other adverse reactions. Monitor BP.
Inform that mild gingival hyperplasia (gum swelling) has been reported and that good dental hygiene decreases its incidence and severity.
20-25°C (68-77°F). Protect from light.
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