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Nisoldipine

Pronunciation

(nye SOL di peen)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet Extended Release 24 Hour, Oral:

Sular: 8.5 mg

Sular: 17 mg [contains tartrazine (fd&c yellow #5)]

Sular: 34 mg

Generic: 8.5 mg, 17 mg, 20 mg, 25.5 mg, 30 mg, 34 mg, 40 mg

Brand Names: U.S.

  • Sular

Pharmacologic Category

  • Antihypertensive
  • Calcium Channel Blocker
  • Calcium Channel Blocker, Dihydropyridine

Pharmacology

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.

Absorption

Well absorbed. Peak concentrations significantly increased with high-lipid meals; however, AUC is reduced.

Metabolism

Extensively hepatic; 1 active metabolite (10% of activity of parent); first-pass effect

Excretion

Urine (60% to 80% as inactive metabolites); feces

Time to Peak

4-14 hours

Duration of Action

>24 hours

Half-Life Elimination

9-18 hours

Protein Binding

>99%

Special Populations: Renal Function Impairment

Dosage adjustments are not needed in patients with mild to moderate renal function impairment.

Special Populations: Hepatic Function Impairment

Liver cirrhosis: Increased plasma concentrations. Use lower starting and maintenance doses.

Special Populations: Elderly

Higher nisoldipine plasma concentrations (Cmax and AUC) have been found in elderly.

Use: Labeled Indications

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

The 2014 guideline for the management of high blood pressure in adults (JNC 8) recommends initiation of pharmacologic treatment to lower blood pressure for the following patients (JNC 8 [James, 2013]):

• Patients ≥60 years of age with systolic blood pressure (SBP) ≥150 mm Hg or diastolic blood pressure (DBP) ≥90 mm Hg. Goal of therapy is SBP <150 mm Hg and DBP <90 mm Hg.

• Patients <60 years of age with SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

• Patients ≥18 years of age with diabetes with SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

• Patients ≥18 years of age with chronic kidney disease (CKD) with SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

In patients with chronic kidney disease (CKD), regardless of race or diabetes status, the use of an ACE inhibitor (ACEI) or angiotensin receptor blocker (ARB) as initial therapy is recommended to improve kidney outcomes. In the general nonblack population (without CKD) including those with diabetes, initial antihypertensive treatment should consist of a thiazide-type diuretic, calcium channel blocker, ACEI, or ARB. In the general black population (without CKD) including those with diabetes, initial antihypertensive treatment should consist of a thiazide-type diuretic or a calcium channel blocker instead of an ACEI or ARB.

Contraindications

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

Dosing: Adult

Hypertension: Oral:

Sular (Geomatrix delivery system): Oral: Initial: 17 mg once daily, then increase by 8.5 mg/week (or longer intervals) to attain adequate control of blood pressure

Usual dose range: 17-34 mg once daily; doses >34 mg once daily are not recommended

Nisoldipine extended-release tablet (original formulation): Initial: 20 mg once daily, then increase by 10 mg/week (or longer intervals) to attain adequate control of blood pressure

Usual dose range: 20-40 mg once daily; doses >60 mg once daily are not recommended

Conversion from nisoldipine extended-release (original formulation) to Sular Geomatrix delivery system:

Nisoldipine Extended Release Dosing Equivalency

Original Extended Release Formulation

Sular Extended Release (Geomatrix delivery system)

10 mg

8.5 mg

20 mg

17 mg

30 mg

25.5 mg

40 mg

34 mg

Table has been converted to the following text.

Nisoldipine Extended Release Dosing Equivalency

Original extended release formulation dose 10 mg equals

Sular Geomatrix dose 8.5 mg

Original extended release formulation dose 20 mg equals

Sular Geomatrix dose 17 mg

Original extended release formulation dose 30 mg equals

Sular Geomatrix dose 25.5 mg

Original extended release formulation dose 40 mg equals

Sular Geomatrix dose 34 mg

Dosing: Geriatric

Hypertension: Oral:

Sular (Geomatrix delivery system): Initial dose: 8.5 mg once daily; increase by 8.5 mg/week (or longer intervals) to attain adequate blood pressure control

Nisoldipine extended-release (original formulation): Initial dose: 10 mg once daily; increase by 10 mg/week (or longer intervals) to attain adequate blood pressure control.

Conversion from nisoldipine extended-release (original formulation) to Sular Geomatrix delivery system: Refer to adult dosing.

Dosing: Renal Impairment

Mild to moderate impairment: No dosage adjustment necessary .

Severe impairment: No dosage adjustment provided in manufacturer's labeling.

Dosing: Hepatic Impairment

Sular (Geomatrix delivery system): An initial dose exceeding 8.5 mg once daily is not recommended for patients with hepatic impairment.

Nisoldipine extended-release (original formulation): An initial dose exceeding 10 mg once daily is not recommended for patients with hepatic impairment.

Administration

Administer at the same time each day to ensure minimal fluctuation of serum levels. Avoid high-fat diet. Administer on an empty stomach (1 hour before or 2 hours after a meal). Swallow whole; do not crush, break, split, or chew.

Dietary Considerations

Take on an empty stomach (1 hour before or 2 hours after a meal). Avoid grapefruit juice before and after dosing. Avoid grapefuit juice; avoid high-fat diet.

Storage

Store at controlled room temperature of 20°C to 25°C (68°F to 77°F). Protect from light; protect from moisture.

Drug Interactions

Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Alpha1-Blockers: May enhance the hypotensive effect of Calcium Channel Blockers. Monitor therapy

Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. Consider therapy modification

Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Monitor therapy

Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Atosiban: Calcium Channel Blockers may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. Monitor therapy

Barbiturates: May increase the metabolism of Calcium Channel Blockers. Management: Monitor for decreased therapeutic effects of calcium channel blockers with concomitant barbiturate therapy. Calcium channel blocker dose adjustments may be necessary. Nimodipine Canadian labeling contraindicates concomitant use with phenobarbital. Monitor therapy

Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Calcium Channel Blockers (Nondihydropyridine): Calcium Channel Blockers (Dihydropyridine) may enhance the hypotensive effect of Calcium Channel Blockers (Nondihydropyridine). Calcium Channel Blockers (Nondihydropyridine) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). Monitor therapy

Calcium Salts: May diminish the therapeutic effect of Calcium Channel Blockers. Monitor therapy

Cimetidine: May increase the serum concentration of Calcium Channel Blockers. Management: Consider alternatives to cimetidine. If no suitable alternative exists, monitor for increased effects of calcium channel blockers following cimetidine initiation/dose increase, and decreased effects following cimetidine discontinuation/dose decrease. Consider therapy modification

Clopidogrel: Calcium Channel Blockers may diminish the therapeutic effect of Clopidogrel. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CycloSPORINE (Systemic): May decrease the metabolism of Calcium Channel Blockers (Dihydropyridine). Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Nisoldipine. Avoid combination

CYP3A4 Inducers (Strong): May decrease the serum concentration of Nisoldipine. Avoid combination

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Nisoldipine. Avoid combination

Dapoxetine: May enhance the orthostatic hypotensive effect of Calcium Channel Blockers. Monitor therapy

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Monitor therapy

Fluconazole: May increase the serum concentration of Calcium Channel Blockers. Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Grapefruit Juice: May increase the serum concentration of Nisoldipine. Avoid combination

Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Herbs (Hypotensive Properties): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Levodopa: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa. Monitor therapy

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Macrolide Antibiotics: May decrease the metabolism of Calcium Channel Blockers. Management: Consider using a noninteracting macrolide. Felodipine Canadian labeling specifically recommends avoiding its use in combination with clarithromycin. Exceptions: Azithromycin (Systemic); Fidaxomicin; Roxithromycin; Spiramycin. Consider therapy modification

Magnesium Salts: Calcium Channel Blockers may enhance the adverse/toxic effect of Magnesium Salts. Magnesium Salts may enhance the hypotensive effect of Calcium Channel Blockers. Monitor therapy

Melatonin: May diminish the antihypertensive effect of Calcium Channel Blockers (Dihydropyridine). Monitor therapy

Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Neuromuscular-Blocking Agents (Nondepolarizing): Calcium Channel Blockers may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). Monitor therapy

Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nitroprusside: Calcium Channel Blockers may enhance the hypotensive effect of Nitroprusside. Monitor therapy

Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Consider therapy modification

Osimertinib: May increase the serum concentration of CYP3A4 Substrates. Osimertinib may decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Tacrolimus (Systemic): Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of Tacrolimus (Systemic). Monitor therapy

TiZANidine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of TiZANidine. Management: Avoid these combinations when possible. If combined use cannot be avoided, initiate tizanidine at an adult dose of 2 mg and increase in 2-4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Consider therapy modification

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Yohimbine: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Adverse Reactions

>10%:

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

Central nervous system: Headache (22%)

1% to 10%:

Cardiovascular: Vasodilation (4%), palpitation (3%), angina exacerbation (2%), chest pain (2%)

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

Dermatologic: Rash (2%)

Gastrointestinal: Nausea (2%)

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

<1% (Limited to important or life-threatening): Alopecia, amblyopia, amnesia, anemia, anorexia, anxiety, appetite increased, arthralgia, arthritis, asthma, ataxia, atrial fibrillation, blepharitis, BUN increased, bruising, cellulitis, cerebral ischemia, colitis, conjunctivitis, creatinine increased, creatine kinase increased, CVA, depression, diabetes mellitus, diaphoresis, diarrhea, dreams abnormal, dyspepsia, dysphagia, dyspnea, dysuria, end inspiratory wheeze, epistaxis, exfoliative dermatitis, facial edema, fever, first-degree AV block, flu-like syndrome, gastritis, gastrointestinal hemorrhage, gingival hyperplasia, glaucoma, glossitis, gout, gynecomastia, heart failure (decompensated), hematuria, hepatomegaly, herpes simplex, herpes zoster; hypersensitivity reaction (eg, angioedema, shortness of breath, tachycardia, chest tightness, hypotension, and rash); hyper-/hypotension, hypertonia, hypoesthesia, hypokalemia, insomnia, jugular venous distention, keratoconjunctivitis, leukopenia, libido decreased, liver function tests abnormal, maculopapular rash, malaise, melena, migraine, mouth ulceration, myalgia, myasthenia, MI, myositis, nocturia, nonprotein nitrogen increased, orthostatic hypotension, paresthesia, petechiae, photosensitivity, pleural effusion, pruritus, pustular rash, rales, retinal detachment, skin discoloration, skin ulcer, somnolence, supraventricular tachycardia, syncope, systolic ejection murmur, taste disturbance, temporary unilateral loss of vision, tenosynovitis, thyroiditis, tremor; T-wave abnormalities on ECG (flattening, inversion, nonspecific changes); urinary frequency, urticaria, vaginal hemorrhage, venous insufficiency, ventricular extrasystoles, vertigo, vitreous floater, weight gain/loss, xerostomia

Warnings/Precautions

Concerns related to adverse effects:

• Angina/MI: Increased angina and/or MI has occurred with initiation or dosage titration of dihydropyridine calcium channel blockers. Reflex tachycardia may occur resulting in angina and/or MI in patients with obstructive coronary disease, especially in the absence of concurrent beta-blockade.

• Hypotension/syncope: Symptomatic hypotension with or without syncope can rarely occur; blood pressure must be lowered at a rate appropriate for the patient's clinical condition. Monitor closely during initial dosing and with dosage adjustment.

• Peripheral edema: The most common side effect is peripheral edema; occurs within 2-3 weeks of starting therapy.

Disease-related concerns:

• Aortic stenosis: Use with caution in patients with severe aortic stenosis.

• Heart failure (HF): The ACCF/AHA heart failure guidelines recommend to avoid use in patients with heart failure due to lack of benefit and/or worse outcomes with calcium channel blockers in general (Yancy, 2013]).

• Hepatic impairment: Use with caution in patients with severe hepatic impairment; lower starting dose required.

• Hypertrophic cardiomyopathy (HCM) with outflow tract obstruction: Use with caution in patients with HCM and outflow tract obstruction since reduction in afterload may worsen symptoms associated with this condition.

Dosage form specific issues:

• Tartrazine: Some dosage forms contain tartrazine, which may cause allergic reactions in certain individuals (eg, aspirin hypersensitivity).

Special populations:

• Elderly: Use with caution in patients >65 years of age; lower starting dose recommended.

Monitoring Parameters

Blood pressure, heart rate

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies when using doses that were not maternally toxic. Untreated chronic maternal hypertension is associated with adverse events in the fetus, infant, and mother. If treatment for hypertension during pregnancy is needed, other agents are preferred (ACOG, 2013).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience pharyngitis or headache. Have patient report immediately to prescriber severe dizziness, passing out, shortness of breath, excessive weight gain, swelling of arms or legs, or angina (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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