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Isradipine

Pronunciation: iss-RAHD-ih-peen
Class: Calcium channel blocking agent

Trade Names

DynaCirc CR
- Tablets, controlled-release 5 mg
- Tablets, controlled-release 10 mg

Isradipine
- Capsules 2.5 mg
- Capsules 5 mg

Pharmacology

Reduces systemic vascular resistance and BP by inhibiting movement of calcium ions across cell membrane in systemic and coronary vascular smooth muscle and myocardium.

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Pharmacokinetics

Absorption

The bioavailability is 15% to 24%. The C max is approximately 1 ng/mL/mg (immediate release); 3 to 4 ng/mL (controlled release). The T max is 1.5 h (immediate release); 7 to 18 h (controlled release). Increased bioavailability up to 25% with food.

Distribution

95% is protein bound.

Metabolism

Completely metabolized by ring oxidation and ester cleavage primarily via CYP-450 3A4. Metabolites are inactive.

Elimination

The t 1/2 is approximately 8 h. 60% to 65% is excreted in the urine, 25% to 30 % in the feces.

Special Populations

Renal Function Impairment
Mild (CrCl 30 to 80 mL/min)

The AUC increases by 45%.

Severe (CrCl is less than 10 mL/min, hemodialysis)

The AUC decreases by 20 to 50%.

Hepatic Function Impairment

The C max increases by 32% and AUC increases by 52%.

Elderly

The AUC and C max increases.

Indications and Usage

Treatment of hypertension.

Contraindications

Standard considerations.

Dosage and Administration

Adults

PO 2.5 to 10 mg/day in 2 divided doses (max dose 20 mg/day).

Storage/Stability

Store in tightly closed container at room temperature. Protect from light.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Peripheral edema; flushing; palpitations; angina; tachycardia; hypotension; syncope; CHF; MI; atrial or ventricular fibrillation.

CNS

Dizziness; lightheadedness; headache; fatigue; lethargy; weakness; shakiness; psychiatric disturbances.

Dermatologic

Rash.

GI

Nausea; diarrhea; constipation; abdominal discomfort; cramps; dyspepsia; vomiting.

Genitourinary

Urinary frequency; micturition disorders; sexual difficulties.

Respiratory

Shortness of breath; dyspnea; wheezing.

Miscellaneous

Transient ischemic attack; stroke.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

CHF

Use with caution in patients with CHF.

Overdosage

Symptoms

Hypotension, dizziness, slurred speech, nausea, weakness, drowsiness, confusion.

Patient Information

  • Explain that dosage will be tapered slowly before stopping to avoid withdrawal symptoms. Warn patient that sudden discontinuation may cause serious chest pain.
  • Tell patient to brush and floss teeth regularly to minimize gum changes (eg, overgrowth of gums).
  • Instruct patient to report the following symptoms to health care provider: irregular heart beat, shortness of breath, swelling of hands or feet, pronounced dizziness, constipation, nausea, or hypotension.
  • Advise patient that drug may cause dizziness and to use caution while driving or performing other tasks requiring mental alertness.

Copyright © 2009 Wolters Kluwer Health.

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