No

Calcium Channel Blocker

Management of hypertension, alone or in combination with other antihypertensive agents

C

Hypersensitivity to nisoldipine, any component, or other dihydropyridine calcium channel blockers

Increased angina and/or myocardial infarction in patients with coronary artery disease. Use with caution in patients with hypotension, congestive heart failure, and hepatic impairment. Blood pressure lowering must be done at a rate appropriate for the patient's condition.

>10%:

Cardiovascular: Peripheral edema (dose-related 7% to 29%)

Central nervous system: Headache (22%)

1% to 10%:

Cardiovascular: Chest pain (2%), palpitations (3%), vasodilation (4%)

Central nervous system: Dizziness (3% to 10%)

Dermatologic: Rash (2%)

Gastrointestinal: Nausea (2%)

Respiratory: Pharyngitis (5%), sinusitis (3%), dyspnea (3%), cough (5%)

<1% (Limited to important or life-threatening symptoms): Cellulite, chills, facial edema, fever, flu syndrome, malaise, atria fibrillation, CVA, congestive heart failure, first-degree AV block, hypertension, angina, pulmonary edema, jugular venous distention, migraine, myocardial infarction, postural hypertension, ventricular extrasystoles, supraventricular tachycardia, syncope, systolic ejection murmur, T-wave abnormalities on EKG (flattening, inversion, nonspecific changes), venous insufficiency, abnormal liver function tests, anorexia, colitis, diarrhea, dry mouth, dyspepsia, dysphagia, flatulence, gastritis, gastrointestinal hemorrhage, gingival hyperplasia, glossitis, hepatomegaly, increased appetite, melena, mouth ulceration, diabetes mellitus, thyroiditis, anemia, ecchymoses, leukopenia, petechiae, gout, hypokalemia, increased serum creatine kinase, increased nonprotein nitrogen, weight gain, weight loss, arthralgia, arthritis, leg cramps, myalgia, myasthenia, myositis, tenosynovitis, abnormal dreams, abnormal thinking and confusion, amnesia, anxiety, ataxia, cerebral ischemia, decreased libido, depression, hypesthesia, hypertonia, insomnia, nervousness, paresthesia, somnolence, tremor, vertigo, asthma, dyspnea, end inspiratory wheeze and fine rales, epistaxis, increased cough, laryngitis, pharyngitis, pleural effusions, rhinitis, sinusitis, acne, alopecia, dry skin, exfoliative dermatitis, fungal dermatitis, herpes simplex, herpes zoster, maculopapular rash, pruritus, pustular rash, skin discoloration, skin ulcer, sweating, urticaria, abnormal vision, amblyopia, blepharitis, conjunctivitis, ear pain, glaucoma, itchy eyes, keratoconjunctivitis, otitis media, retinal detachment, tinnitus, watery eyes, taste disturbance, temporary unilateral loss of vision, vitreous floater, watery eyes, dysuria, hematuria, impotence, nocturia, urinary frequency, increased BUN and serum creatinine, vaginal hemorrhage, vaginitis, gynecomastia

Case report: Cholestatic jaundice

The primary cardiac symptoms of calcium blocker overdose include hypotension and bradycardia. The hypotension is caused by peripheral vasodilation, myocardial depression, and bradycardia. Bradycardia results from sinus bradycardia, second- or third-degree atrioventricular block, or sinus arrest with junctional rhythm. Intraventricular conduction is usually not affected so QRS duration is normal.

In a few reported cases, overdose with calcium channel blockers has been associated with hypotension and bradycardia, initially refractory to atropine but becoming more responsive to this agent when larger doses (approaching 1 g/hour for more than 24 hours) of calcium chloride was administered.

CYP3A3/4 enzyme substrate

Beta-blockers may have increased pharmacokinetic or pharmacodynamic interactions with nisoldipine.

Calcium may reduce the calcium channel blocker's effects, particularly hypotension.

Cimetidine reduced diltiazem's metabolism; consider an alternative H₂ antagonist.

Grapefruit juice increases the bioavailability of nisoldipine; monitor for altered nisoldipine effects.

Rifampin increases the metabolism of the calcium channel blocker; adjust the dose of the calcium channel blocker to maintain efficacy.

Tacrolimus's serum concentrations are increased by nifedipine; avoid the combination. Use another calcium channel blocker or monitor tacrolimus trough levels and renal function closely.

Phenytoin decreases nisoldipine to undetectable levels. Avoid use of any CYP3A4 inducer with nisoldipine.

As a dihydropyridine calcium channel blocker, structurally similar to nifedipine, nisoldipine impedes the movement of calcium ions into vascular smooth muscle and cardiac muscle. Dihydropyridines are potent vasodilators and are not as likely to suppress cardiac contractility and slow cardiac conduction as other calcium antagonists such as verapamil and diltiazem; nisoldipine is 5-10 times as potent a vasodilator as nifedipine.

Duration: >24 hours

Absorption: Well absorbed

Metabolism: Extensive presystemic metabolism in the intestinal wall and the liver; hepatically metabolized to inactive metabolites

Half-life: 7-12 hours

Bioavailability: 5%; T_max: 6-12 hours

Elimination: In the urine

Adults: Oral: Initial: 20 mg once daily, then increase by 10 mg/week (or longer intervals) to attain adequate control of blood pressure; doses >60 mg once daily are not recommended. A starting dose not exceeding 10 mg/day is recommended for the elderly and those with hepatic impairment.

Avoid grapefruit products before and after dosing

Nisoldipine alone or in combination with other agents is effective in the management of hypertension and angina. Nisoldipine should be avoided in patients with left ventricular systolic dysfunction because of negative inotropic effects.

May cause dizziness

None reported

No information available to require special precautions

Other drugs in this class can cause gingival hyperplasia, but there have been no reports for nisoldipine

Take as prescribed - swallow whole (do not crush or break). May be taken with food but avoid grapefruit products and high fat foods. Do not stop abruptly without consulting prescriber. You may experience headache (if unrelieved, consult prescriber), nausea or vomiting (frequent small meals may help), constipation (increased dietary bulk and fluids may help), depression (should resolve when drug is discontinued). May cause dizziness or drowsiness; use caution when driving or engaging in tasks that require alertness until response to drug is known. Promptly report any chest pain or swelling of hands or feet, respiratory distress, sudden weight gain, or unresolved constipation. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Administer at the same time each day to ensure minimal fluctuation of serum levels

Tablet, extended release: 10 mg, 20 mg, 30 mg, 40 mg