Versant-XR

Versant-XR

felodipine

Manufacturer:

LR Imperial

Distributor:

United Lab

Marketer:

Westmont
Full Prescribing Info
Contents
Felodipine.
Action
Pharmacology: Felodipine is a vascular-selective dihydropyridine calcium channel blocker that produces a sustained 24-hour reduction in systolic and diastolic pressure in patients with all degrees of primary hypertension with no direct effect on cardiac contractility and conduction. It lowers arterial blood pressure by decreasing systemic vascular resistance.
Felodipine improves coronary blood flow and myocardial oxygen supply by dilating the epicardial arteries and arterioles. These properties together with the resulting decrease in left ventricular afterload and myocardial oxygen demand due to reduction in systemic blood pressure makes felodipine an effective anti-anginal and anti-ischemic agent.
Felodipine increases stroke volume and cardiac output that may be sustained during long term therapy in patients with heart failure.
Felodipine is as effective in diabetic patients as in non-diabetic patients, causing no significant change in glycemic control in type 1 or type 2 diabetic patients. Felodipine appears to have no clinically significant effects on blood levels of lipids or glucose.
Felodipine appears to be suitable for use in patients with concomitant renal dysfunction. It has diuretic and natriuretic effect due to reduced tubular reabsorption of filtered sodium but does not affect daily potassium excretion. Glomerular filtration rate and creatinine clearance appear unaffected by felodipine, while renal vascular resistance is decreased, and renal blood flow is either unchanged or marginally increased.
Felodipine does not affect urinary albumin excretion.
In addition to its antihypertensive action, felodipine therapy is associated with significant regression of left ventricular hypertrophy.
Pharmacokinetics: Bioavailability: Felodipine extended-release tablets contain felodipine in a matrix which forms a gel on contact with gastrointestinal fluid. It is then gradually eroded releasing felodipine slowly at a constant rate. This results in an even plasma felodipine concentration versus time curve, without the pronounced peak seen with conventional formulations and, therefore, allows once-daily administrations.
Following administration of felodipine a reduction in blood pressure generally occurs within 2 to 5 hours. During chronic administration, substantial blood pressure control lasts for 24 hours, with trough reduction in diastolic blood pressure approximately 40-50% of peak reductions. The antihypertensive effect is dose dependent and correlates with the plasma concentration. Felodipine is greater than 99% bound to plasma proteins.
Felodipine is virtually completely metabolized, initially by the formation of the pyridine analog by the hepatic microsomal cytochrome P-450 system. At least 10 metabolites are formed by several subsequent pathways, mainly via oxidation. All metabolites are hemodynamically inactive and excreted in both free and conjugated forms: within 72 hours of a radiolabelled dose, 60-70% of radioactivity is recovered in urine and 10% in feces. Felodipine is a high-clearance drug with an average blood clearance of 1200 mL/min. The apparent mean terminal elimination half-life increases and mean total blood clearance decreases with age. However, while disease states or increasing age may cause an increase in plasma felodipine concentrations, the clinical impact is considered minor when compared with the normal interindividual variation in plasma felodipine concentrations.
Therapeutic Efficacy: In patients with mild to moderate hypertension, felodipine monotherapy is at least as effective in reducing blood pressure as usual therapeutic dosages of diuretics (hydrochlorothiazide alone or in combination with amiloride), β-blockers (metoprolol or atenolol), ACE inhibitors (captopril or enalapril) and other calcium channel blockers (nifedipine, nitrendipine or diltiazem). Statistically significant differences were sometimes found, almost invariably in favor of felodipine. In some studies, felodipine was effectively combined with other agents, including controlled-release metoprolol and enalapril, in patients with mild to moderate hypertension.
In more severe forms of essential hypertension inadequately controlled by a β-blocker and/or diuretic therapy, placebo-controlled trials indicate that felodipine 5 to 20 mg once-daily as 'add-on' therapy produces an additional reduction in blood pressure. In this situation 'add-on' therapy with felodipine was significantly more effective than usual dosages of sustained-release nifedipine or nitrendipine.
Indications/Uses
For the treatment of mild to moderate hypertension, either alone or with other antihypertensive agents.
Dosage/Direction for Use
Usual Initial Adult Dose: Orally, 5 mg once daily.
Adjust dosage according to patient's response with the usual dosage range being 2.5-10 mg once-daily.
Geriatric Dosing (especially for patients > 65 years old): Orally, 2.5 mg once daily.
Patients with Impaired Liver Function: Orally, 2.5 mg once daily.
Felodipine tablets should be taken without food or with a light meal.
Felodipine tablets should be swallowed whole and not crushed or chewed, since it may cause mild gingival hyperplasia (gum swelling).
Or as prescribed by the physician.
Special Precautions
Felodipine, like other calcium channel blockers, may occasionally precipitate significant hypotension, and rarely, syncope. It may lead to reflex tachycardia which in susceptible individuals, may result to angina pectoris.
Adverse Reactions
As with other dihydropyridine calcium channel blockers, the most common undesirable effects of felodipine 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, visual disturbances, and mental depression have also occurred. A paradoxical increase in ischemic chest pain may occur at the start of treatment and in a few patients excessive fall in blood pressure has led to cerebral or myocardial ischemia 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.
MIMS Class
ATC Classification
C08CA02 - felodipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
Presentation/Packing
Tab 5 mg x 100's.
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