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Class: Dihydropyridines
VA Class: CV200
Chemical Name: 4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid methyl 1-methylethyl ester
Molecular Formula: C19H21N3O5
CAS Number: 75695-93-1
Brands: DynaCirc, DynaCirc CR


Calcium-channel blocking agent; dihydropyridine derivative.1 2 3 4 7

Uses for Isradipine


Management of hypertension (alone or in combination with other classes of antihypertensive agents).1 2 3 4 6 7 13 14 15 50 59 72

One of several preferred initial therapies in hypertensive patients with a high risk of developing CAD, including those with diabetes mellitus;72 in geriatric patients with isolated systolic hypertension;50 54 and in patients with coexisting angina.5 50

Can be used as monotherapy for initial management of uncomplicated hypertension; however, thiazide diuretics are preferred by JNC 7.72

Hypertensive Crises

Use of currently available conventional dosage form for acute management of hypertensive crises not established.4 5 50

Isradipine has been used for rapid reduction of BP in pediatric patients 1–17 years of age with hypertensive urgencies or emergencies.76

Isradipine Dosage and Administration


Oral Administration

Conventional Capsules

Administer orally twice daily without regard to meals.1 22

Extended-release Core Tablets

Administer orally once daily without regard to meals.22 59

Swallow extended-release core tablets intact; do not chew, divide, or crush.59


Pediatric Patients

Conventional Capsules

Initially, 0.15–0.2 mg/kg daily given in 3–4 divided doses.76 Increase dosage as necessary up to a maximum dosage of 0.8 mg/kg (up to 20 mg) daily.76

Extended-release Core Tablets

Initially, 0.15–0.2 mg/kg daily given once daily or in 2 divided doses.76 Increase dosage as necessary up to a maximum dosage of 0.8 mg/kg (up to 20 mg) daily.76

Hypertensive Urgencies or Emergencies
Rapid Reduction of BP
Oral Capsules, Extended-release Tablets, or Extemporaneous Suspension

Children and adolescents 1–17 years of age: 0.05–0.1 mg/kg per dose.76

Prepare extemporaneous isradipine suspension containing 1 mg/mL for those unable to swallow capsules or extended-release tablets.76 81 Open twenty-four 5-mg capsules and grind the contents to a fine powder with a mortar and pestle;76 levigate with a small amount of glycerin to form a paste.81 Add simple syrup in increasing amounts while mixing thoroughly; transfer the suspension to a graduated cylinder.81 Add any remaining drug in the mortar to the graduated container; the final volume of the suspension should be 120 mL.81 Transfer contents of the graduated cylinder into an appropriate size amber bottle.81 The isradipine suspension is stable for 35 days when refrigerated.81 Shake well before each use.81


Conventional Capsules

Initially, 1.25–2.5 mg twice daily 1 2 3 4 5 7 14 15 16 50 as monotherapy or when added to thiazide diuretic therapy.1 However, a dosage form suitable for administering 1.25-mg doses currently is not commercially available in the US.1 22

Full hypotensive effect may not be seen for 2–4 weeks.1 If BP control is inadequate after this period, increase dosage in increments of 5 mg daily at intervals of 2–4 weeks, up to a maximum of 20 mg daily, according to patient’s BP response.1 4 5 50 59

Dosages >10 mg daily usually do not result in further improvement in BP control and may increase risk of adverse effects.1 4 5 50 59 The JNC recommends a usual range of 2.5–10 mg daily.72

Extended-release Core Tablets

Initially, 5 mg once daily as monotherapy or when added to thiazide diuretic therapy.59

If necessary, increase dosage in increments of 5 mg daily at intervals of 2–4 weeks, up to a maximum of 20 mg daily, according to patient’s BP response.1 4 5 50 59

Dosages >10 mg daily usually do not result in further improvement in BP control and may increase risk of adverse effects.1 4 5 50 59 The JNC recommends a usual range of 2.5–10 mg daily.72

Prescribing Limits

Pediatric Patients


Conventional capsules: Maximum 0.8 mg/kg (up to 20 mg) daily.76

Extended-release core tablets: Maximum 0.8 mg/kg (up to 20 mg) daily.76



Conventional capsules: Maximum 20 mg daily.1 4 5 50 59

Extended-release core tablets: Maximum 20 mg daily.1 4 5 50 59

Special Populations

Hepatic Impairment

Some clinicians recommend dosage modification (i.e., reduced dosage) and careful titration,3 21 but the manufacturer recommends usual initial adult dosage.1 4 7 59

Renal Impairment

Dosage modification not necessary.1 4 7 59

Geriatric Patients

Initial dosage modification not necessary,1 3 4 5 7 16 20 59 but slower dosage escalation recommended;3 5 20 BP may be adequately controlled with relatively low dosages and once-daily dosing.2 3 16

Select dosage of isradipine extended-release core tablets with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.59

Cautions for Isradipine


  • Known hypersensitivity to isradipine or any ingredient in the formulation.1 59


General Precautions


Possible symptomatic hypotension.1 59 Carefully monitor BP, especially during therapy initiation or dosage increase.1


May precipitate or worsen heart failure.1 5 16 18 59 Use with caution and titrate dosage carefully, especially in those receiving concomitant β-adrenergic blocking agents.1 5 16 18 59


Frequency, duration, and severity of angina may rarely increase during therapy.3 14 18

Peripheral Edema

Possible mild to moderate peripheral edema associated with vasodilation of arterioles and other small blood vessels; appears to be dose related.59

GI Effects

Use extended-release core tablets with caution in patients with preexisting GI narrowing; obstruction may occur.59

Specific Populations


Category C.1 59


Not known whether isradipine is distributed into milk; discontinue nursing or the drug.1 59

Pediatric Use

Safety and efficacy remain to be fully established in children;1 22 59 however, some experts have recommended dosages for hypertension based on current limited clinical experience.76

Geriatric Use

Insufficient experience with use of isradipine extended-release core tablets in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults; select dosage with caution.59

Common Adverse Effects

Headache, dizziness, peripheral edema, palpitation, tachycardia, flushing, chest pain.1 2 3 4 5 10 11 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54

Interactions for Isradipine

Appears to be metabolized by CYP3A4.1 59

Specific Drugs





Increased peak plasma concentrations and AUC of isradipine1

Monitor carefully; reduction of isradipine dosage may be required1


Pharmacokinetic interaction unlikely1 59


Possible severe hypotension during fentanyl anesthesia with concomitant use of a β- blocker and a calcium channel blocker1 59

Increase volume of circulating fluids if hypotension occurs1 59


Pharmacokinetic interaction unlikely1 59


Pharmacokinetic interaction unlikely1 59


Decreased rate of absorption, increased AUC and peak plasma concentrations of propranolol observed with single doses; no substantial effect on either drug under steady-state conditions1 59


Increased isradipine metabolism and clearance; reduction of isradipine concentrations to below detectable levels1

Isradipine concentrations and therapeutic effects will be markedly reduced or abolished with concomitant use1


Pharmacokinetic or pharmacodynamic interaction unlikely

Isradipine Pharmacokinetics



90–95% absorbed following oral administration of conventional capsules, with peak plasma isradipine concentrations attained in about 1.5 hours.1

Bioavailability is approximately 15–24% due to first-pass metabolism.1 59


After a single dose, reduction in supine and standing BP occurs within 2–3 or about 2 hours after administration as conventional capsules 1 or extended-release core tablets, respectively.59


Effects persist for >12 or ≥24 hours after administration of conventional capsules or extended-release core tablets, respectively.1 59


Food decreases bioavailability of extended-release core tablets by up to 25%59 and decreases time to peak plasma concentration of conventional capsules by about 1 hour.1

Special Populations

In patients with hepatic impairment, the peak plasma concentration and AUC of conventional capsules are increased by 32 and 52%, respectively.1

In patients with mild renal impairment (Clcr 30–80 mL/min), the AUC of conventional capsules is increased by 45%; however, in patients with severe renal failure (Clcr <10 mL/min) who have been on hemodialysis, AUC is decreased by 20–50%.1

In geriatric patients, peak plasma isradipine concentration and AUC of conventional capsules are increased1 59 by 13 and 40%, respectively.1



It is not known whether isradipine is distributed into milk.1

Plasma Protein Binding




Completely metabolized in the liver, apparently by CYP3A4, to inactive metabolites.1 59

Elimination Route

Excreted in urine (60–65%) and feces (25–30%).1 59


Biphasic; initial half-life is 1.5–2 hours and terminal elimination half-life is approximately 8 hours.1 59




Conventional Capsules

Tight, light-resistant containers at 20–25°C.82

Extended-release Core Tablets

Tight containers at <30°C.59 Protect from moisture and humidity.59


  • Inhibits transmembrane influx of extracellular calcium ions across the membranes of myocardial cells and vascular smooth muscle cells, without changing serum calcium concentrations.1 59

  • Peripheral arterial vasodilator; acts directly on vascular smooth muscle causing reduction in peripheral vascular resistance (afterload) and BP.1 59

Advice to Patients

  • Importance of swallowing extended-release tablets whole; do not divide, chew, or crush.59

  • Advise patients that empty tablet shell of extended-release core tablets may be noticeable in stool.59

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1 59

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 59

  • Importance of informing patients of other important precautionary information.1 59 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name



Dosage Forms


Brand Names




2.5 mg*

Isradipine Capsules

5 mg*

Isradipine Capsules

Tablets, Extended-release core

5 mg

DynaCirc CR


10 mg

DynaCirc CR


Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

DynaCirc CR 10MG 24-hr Tablets (GLAXO SMITH KLINE): 30/$129.99 or 90/$369.96

DynaCirc CR 5MG 24-hr Tablets (GLAXO SMITH KLINE): 30/$83.99 or 90/$232.51

Isradipine 2.5MG Capsules (WATSON LABS): 60/$79.99 or 180/$211.97

AHFS DI Essentials. © Copyright, 2004-2016, Selected Revisions September 16, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.


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