Overview
DESCRIPTION SULAR ® (nisoldipine) is an extended release tablet dosage form of the dihydropyridine calcium channel blocker nisoldipine. Nisoldipine is 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, methyl 2-methylpropyl ester, C 20 H 24 N 2 O 6 , and has the structural formula: Nisoldipine is a yellow crystalline substance, practically insoluble in water but soluble...
Mechanism of Action
CLINICAL PHARMACOLOGY Mechanism of Action Nisoldipine is a member of the dihydropyridine class of calcium channel antagonists (calcium ion antagonists or slow channel blockers) that inhibit the transmembrane influx of calcium into vascular smooth muscle and cardiac muscle. It reversibly competes with other dihydropyridines for binding to the calcium channel. Because the contractile process of vascular smooth muscle is dependent upon the movement of extracellular calcium into the muscle through specific ion channels, inhibition of the calcium channel results in dilation of the arterioles. In vitro studies show that the effects of nisoldipine on contractile processes are selective, with greater potency on vascular smooth muscle than on cardiac muscle.
Indications
- INDICATIONS AND USAGE SULAR is indicated for the treatment of hypertension. It may be used alone or in combination with other anti-hypertensive agents.
Common Doses
- 17 mg
- 8.5 mg
- 34 mg
Dosage
DOSAGE AND ADMINISTRATION The dosage of SULAR must be adjusted to each patient's needs. Therapy usually should be initiated with 17 mg orally once daily, then increased by 8.5 mg per week or longer intervals, to attain adequate control of blood pressure. Usual maintenance dosage is 17 to 34 mg once daily. Blood pressure response increases over the 8.5 - 34 mg daily dose range but adverse event rates also increase. Doses beyond 34 mg once daily are not recommended. SULAR has been used safely with diuretics, ACE inhibitors, and beta-blocking agents.
Contraindications
- CONTRAINDICATIONS SULAR is contraindicated in patients with known hypersensitivity to dihydropyridine calcium channel blockers.
Side Effects
- ADVERSE EXPERIENCES More than 6000 patients world-wide have received nisoldipine in clinical trials for the treatment of hypertension, either as the immediate release or the SULAR extended release formulation. Of about 1,500 patients who received SULAR in hypertension studies, about 55% were exposed for at least 2 months and about one third were exposed for over 6 months, the great majority at doses equivalent to 17 mg and above. SULAR is generally well-tolerated. In the U.S. clinical trials of SULAR in hypertension, 10.
Interactions
- Drug Interactions A 30 to 45% increase in AUC and C max of nisoldipine was observed with concomitant administration of cimetidine 400 mg twice daily. Ranitidine 150 mg twice daily did not interact significantly with nisoldipine (AUC was decreased by 15 - 20%). No pharmacodynamic effects of either histamine H 2 receptor antagonist were observed. CYP3A4 inhibitors and inducers : SULAR is substrate of CYP3A4 and coadministration of SULAR with any known inducer or inhibitor of CYP3A4 should be avoided in general.