Dosing and uses of Sular (nisoldipine)
Adult dosage forms and strengths
tablet, extended-release (generic)
- 8.5mg
- 17mg
- 20mg
- 25.5mg
- 30mg
- 34mg
- 40mg
tablet, extended-release (Sular, new hydrogel ER formulation)
- 8.5mg
- 17mg
- 34mg
Hypertension
Hydrogel ER tablets (Sular's new formulation): 17 mg PO qDay initially; may increase slowly by at least 1-week intervals; not to exceed 34 mg PO qDay
Coat-core ER tablets (generic; old Sular formulation): 20 mg PO qDay initially; may increase slowly by at least 1-week intervals; not to exceed 60 mg/day
Hepatic Impairment
Hydrogel ER tablets (Sular's new formulation): Initial dose should not exceed 8.5 mg PO qDay; may increase slowly by at least 1-week intervals; not to exceed 34 mg PO qDay
Coat-core ER tablets (generic; old Sular formulation): Initial dose should not exceed 10 mg PO qDay; may increase slowly by at least 1-week intervals; not to exceed 30 mg PO qDay
Administration
Take on empty stomach; 1 hr before or 2 hr after meals
Swallow tablet whole; do not crush, divide, or chew
Pediatric dosage forms and strengths
Safety and efficacy not established
Geriatric dosage forms and strengths
Hydrogel ER tablets (Sular's new formulation): 8.5 mg PO qDay initially; may increase slowly by at least 1-week intervals; not to exceed 34 mg PO qDay
Coat-core ER tablets (generic; old Sular formulation): 10 mg PO qDay initially; may increase slowly by at least 1-week or longer intervals to minimum effective dose
Sular (nisoldipine) adverse (side) effects
>10%
Headache (22%)
Peripheral edema (22%)
1-10%
Dizziness (5%)
Palpitation (3%)
Vasodilation (4%)
Increased severity of angina (1.5%)
Nausea (2%)
Pharyngitis (5%)
Sinusitis (3%)
< 1%
Gingival hyperplasia
Colitis
Anemia
Alopecia
Anorexia
Anxiety
Ischemia
Diabetes mellitus
Dyspepsia
Dysphagia
Warnings
Contraindications
Hypersensitivity to nisoldipine or other calcium channel blockers
Cautions
Use caution in CHF, aortic stenosis, hypotension (initially or after dose increases), persistent progressive dermatologic reactions, exacerbation of angina (during initiation of treatment, after dose increased, beta blocker withdrawal), liver impairment
Reflex tachycardia resulting in angina and/or MI in patients with obstructive coronary disease reported
Peripheral edema may occur within 2-3 weeks of initiating therapy
Hypotension with or without syncope is possible (particularly with severe aortic stenosis)
Do not take with high fat meal or grapefruit products
Start at lower dose with liver/kidney dysfunction, elderly
Pregnancy and lactation
Pregnancy category: C
Lactation: not known if excreted in breast milk, use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Sular (nisoldipine)
Mechanism of action
Calcium channel blocker (dihydropyridine): inhibits transmembrane influx of extracellular Ca ions across membranes of myocardial cells and vascular smooth muscle cells, without changing serum calcium concentrations, resulting in inhibition of cardiac and vascular smooth muscle contraction, thereby dilating the main coronary and systemic arteries
Produces vasodilation and decreases peripheral resistance
Absorption
Bioavailability: 4-8%
Peak Plasma Time: 6-12 hr
Duration: 24 hr
Distribution
Protein Bound: 99%
Vd: 4-5 L/kg
Metabolism
Mainly metabolized in liver by CYP3A4
Metabolites: Hydroxylated isobutyl ester derivative (active, 10% potency of parent drug)
Elimination
Clearance: 1400-2200 L/hr
Excretion: Urine (60-80%); feces (6-12%)
Dialyzable: HD: No
