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Therapeutic Classification: antihypertensives

Pharmacologic Classification: calcium channel blockers

• Hypertension (as monotherapy or in combination with other antihypertensive agents).

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

• Systemic vasodilation, resulting in ↓ BP.

Absorption: Well absorbed (87%) following oral administration but rapidly and extensively metabolized in the gut wall, resulting in 5% bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 isoenzyme.

Half-life: 7–12 hr.

(antihypertensive effects)

Contraindicated in:

• Hypersensitivity
• Cross-sensitivity with calcium channel blockers may occur
• Lactation: Lactation.

Use Cautiously in:

• HF/left ventricular dysfunction
• Hepatic impairment (dose ↓ may be necessary)
• Coronary artery disease (may precipitate angina)
• OB: Safety not established in pregnancy
• Pedi: Safety and effectiveness not established in children
• Geri: Dose ↓ may be necessary due to age-related ↓ in hepatic, renal or cardiac function.

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

Derm: rash.

EENT: pharyngitis, sinusitis.

Endo: gynecomastia.

GI: nausea.

Neuro: headache, dizziness.

Drug-Drug:

• 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.

Drug-Food:

• Grapefruit and grapefruit juice↑ serum levels and effect.
• Blood levels are ↑ by concurrent ingestion of a high-fat meal and should be avoided.

• PO (Adults): Extended-release tablets: 20 mg/day as a single dose initially; may be ↑ by 10 mg/day every 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 every 7 days, up to 34 mg/day (usual range 8.5–34 mg/day).

(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;

• Monitor BP and HR 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).

• Total serum calcium concentrations are not affected by calcium channel blockers.

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

• Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes. 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.
  • 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 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, 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.
  • 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.
  • Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding.

• Decrease in BP.

Sular