Sular

nisoldipine

Sular, Syscor (UK)

Action

Suppresses calcium transport into vascular smooth muscle cells. This suppression inhibits vasoconstriction and dilates coronary arteries, improving myocardial oxygen uptake.

Availability

Tablets (extended-release): 8.5 mg, 17 mg, 22.5 mg, 34 mg

Indications and dosages

➣ Hypertension

Adults: Initially, 17 mg P.O. daily; may increase by 8.5 mg per week or longer intervals to attain adequate blood pressure control. Usual maintenance dosage is 17 to 34 mg daily.

Contraindications

• Hypersensitivity to drug or dihydropyridine calcium channel blockers

Precautions

Use cautiously in:

• heart failure and left ventricular dysfunction, hepatic impairment, renal disease, coronary artery disease, hypotension

• concurrent phenytoin use

• elderly patients

• pregnant or breastfeeding patients

• children (safety not established).

Administration

• Give with meals, but not with high-fat meals, grapefruit, or grapefruit juice.

• Don't crush or break extended-release tablets. Make sure patient swallows them whole.

• Know that drug may be given alone or with other antihypertensives.

Adverse reactions

CNS: headache, dizziness

CV: peripheral edema, chest pain, vasodilation, hypotension, palpitations

EENT: pharyngitis, sinusitis

GI: nausea

Skin: rash

Interactions

Drug-drug. Cimetidine: increased nisoldipine blood level

Phenytoin, other CYP3A4 inducers: decreased nisoldipine blood level and efficacy

Drug-food. Grapefruit juice: significantly increased drug blood level and effects

High-fat meal: decreased drug blood level

Drug-herbs. Ephedra (ma huang), yohimbine: antagonism of nimodipine effects

St. John's wort: decreased nimodipine blood level

Drug-behaviors. Alcohol use: increased hypotensive effects

Patient monitoring

• Check vital signs and ECG.

• Monitor fluid intake and output. Watch for peripheral edema.

Patient teaching

• Tell patient to swallow extended-release tablets whole and not to crush or break them.

• Advise patient to take with food, but not high-fat food. Recommend small, frequent meals.

• Instruct patient to avoid high-fat meals, alcohol, grapefruit, and grapefruit juice.

• Tell patient to immediately report irregular heart beat, shortness of breath, swelling, pronounced dizziness, rash, or chest pain.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, foods, herbs, and behaviors mentioned above.

nisoldipine

(nye-sole-di-peen) nisoldipine,

Sular

(trade name)

Classification

Therapeutic: antihypertensives
Pharmacologic: calcium channel blockers
Pregnancy Category: C

Indications

Management of hypertension.

Action

Inhibits the transport of calcium into vascular smooth muscle cells, resulting in inhibition of vasoconstriction and dilation of arterioles.

Therapeutic effects

Systemic vasodilation, resulting in decreased BP.

Pharmacokinetics

Absorption: Well absorbed (87%) following oral administration but rapidly and extensively metabolized in the gut wall, resulting in 5% bioavailability.Distribution: Unknown.Metabolism and Excretion: Highly metabolized CYP3A4 enzyme system.Half-life: 7–12 hr.

Time/action profile (antihypertensive effects)

ROUTEONSETPEAKDURATION
POunknown6–12 hr24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Cross-sensitivity with calcium channel blockers may occur;Concurrent phenytoin use.Use Cautiously in: HF/left ventricular dysfunction;Hepatic impairment (dose ↓ may be necessary);Coronary artery disease (may precipitate angina); Obstetric / Lactation / Pediatric: Safety not established; Geriatric: Dose ↓ may be necessary due to age-related ↓ in hepatic, renal or cardiac function.

Adverse Reactions/Side Effects

Central nervous system

  • headache (most frequent)
  • dizziness

Ear, Eye, Nose, Throat

  • pharyngitis
  • sinusitis

Cardiovascular

  • peripheral edema (most frequent)
  • chest pain
  • hypotension
  • palpitations

Gastrointestinal

  • nausea

Dermatologic

  • rash

Endocrinologic

  • gynecomastia

Interactions

Drug-Drug interaction

Additive hypotension may occur with other antihypertensives, acute ingestion of alcohol, or nitrates.Antihypertensive effects may be ↓ by concurrent use of NSAIDs.Phenytoin or other CYP3A4 inducers ↓ blood levels and effectiveness (avoid concurrent use).Grapefruit and grapefruit juice ↑ serum levels and effect.Blood levels are ↑ by concurrent ingestion of a high-fat meal and should be avoided.

Route/Dosage

Oral (Adults) Extended-release tablets—20 mg/day as a single dose initially; may be ↑ by 10 mg/day q 7 days, up to 60 mg/day (usual range 20–40 mg/day); Geomatrix extended-release tablets—17 mg/day as a single dose initially; may be ↑ by 8.5 mg/day q 7 days, up to 34 mg/day (usual range 8.5–34 mg/day).

Hepatic Impairment

Oral (Adults) Geomatrix extended-release tablets—Initial dose should not exceed 8.5 mg/day.

Availability (generic available)

Extended-release tablets: 20 mg, 30 mg, 40 mg Geomatrix extended-release tablets: 8.5 mg, 17 mg, 25.5 mg, 34 mg

Nursing implications

Nursing assessment

  • Monitor BP and pulse prior to therapy, during dose titration, and periodically throughout therapy. Monitor ECG periodically during prolonged therapy.
    • Monitor intake and output ratios and daily weight. Assess for signs of HF (peripheral edema, rales/crackles, dyspnea, weight gain, jugular venous distention).
  • Lab Test Considerations: Total serum calcium concentrations are not affected by calcium channel blockers.

Potential Nursing Diagnoses

Decreased cardiac output (Indications)

Implementation

  • Oral: Avoid administration within 1 hr of high-fat meals or grapefruit products.
    • Do not break, crush, or chew tablets.

Patient/Family Teaching

  • Advise patient to take medication exactly as directed, even if feeling well. If a dose is missed, take as soon as possible unless almost time for next dose; do not double dose. May need to be discontinued gradually.
    • Advise patient to avoid grapefruit or grapefruit juice during therapy.
    • Encourage patient to comply with other interventions for hypertension (weight reduction, low-sodium diet, smoking cessation, moderation of alcohol consumption, regular exercise, and stress management). Medication controls but does not cure hypertension.
    • Instruct patient and family in proper technique for monitoring BP. Advise patient to take BP weekly and to report significant changes to health care professional.
    • Caution patient to change positions slowly to minimize orthostatic hypotension.
    • May cause dizziness. Advise patient to avoid driving or other activities requiring alertness until response to the medication is known.
    • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to avoid concurrent use of alcohol or OTC medications and herbal products, especially cold preparations, without consulting health care professional.
    • Advise patient to notify health care professional if irregular heartbeat, dyspnea, swelling of hands and feet, pronounced dizziness, nausea, constipation, or hypotension occurs or if headache is severe or persistent.

Evaluation/Desired Outcomes

  • Decrease in BP.

Sular®

Nisoldipine, see there.