Isradipine (isradipine)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Isradipine is a 1,4-dihydropyridine-derivative calcium-channel blocking agent (calcium-channel blocker).
Isradipine is a 1,4-dihydropyridine-derivative calcium-channel blocking agent that is structurally related to felodipine and nifedipine. Isradipine has pharmacologic actions similar to those of other dihydropyridine calcium-channel blocking agents (e.g., felodipine, nifedipine). The principal physiologic action of isradipine is to inhibit the transmembrane influx of extracellular calcium ions across the membranes of myocardial cells and vascular smooth muscle cells.
Isradipine is a peripheral arterial vasodilator; the drug acts directly on vascular smooth muscle, causing reductions in peripheral vascular resistance (afterload) and blood pressure. The effects of isradipine are more selective to vascular smooth muscle than cardiac muscle.
Following oral administration, 90-95% of isradipine is absorbed; peak plasma concentrations are attained in about 1.5 hours. The low oral bioavailability of isradipine (approximately 15-24%) is due to extensive first-pass metabolism. When the drug is administered with food, time to peak plasma concentration is increased by about 1 hour; however, no effect on AUC is observed.
After a single dose, a reduction in supine and standing blood pressure occurs within 2-3 hours; during chronic administration of twice daily dosing, over 50% of the peak blood pressure effect remains at trough prior to the next dose. Isradipine plasma protein binding is 95%; the drug crosses the placenta, but it is not known whether it is distributed into human milk. Isradipine is completely metabolized in the liver to inactive metabolites; approximately 60-65% is excreted in urine and 25-30% in feces.
Isradipine elimination is biphasic; the initial half-life is 1.5-2 hours and terminal elimination half-life is approximately 8 hours. Peak plasma concentration and AUC are increased by 32 and 52%, respectively, in patients with hepatic impairment. In patients with mild renal impairment (creatinine clearance 30-80 mL/minute), AUC is increased by 45%; however, in patients with severe renal failure (creatinine clearance <10 mL/minute) who have been on hemodialysis, AUC is decreased by 20-50%.
Isradipine peak plasma concentration and AUC are increased by 13 and 40%, respectively, in geriatric patients.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Isradipine belongs to a class of drugs known as calcium channel blockers.
It works by relaxing blood vessels so blood can flow more easily.
Generic name: isradipine
Pronunciation: (is-RAD-i-peen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Isradipine
Indications
The following indications are listed for Isradipine:
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.
Dosing
No dosing information is available for this tab.
Isradipine is administered orally. Administration of isradipine conventional capsules with food decreases the rate (e.g., delaying peak plasma concentrations by about 1 hour) but not extent of absorption.
Store capsules at 20-25degreesC in a tight, light-resistant container.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to isradipine or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects reported in patients treated with isradipine include headache, dizziness, peripheral edema, palpitations, fatigue, flushing, and chest pain.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Although safety and efficacy remain to be fully established in children younger than 18 years of age, some experts have recommended pediatric dosages for hypertension based on clinical experience.
There are no adequate and controlled studies to date with isradipine in pregnant women. When administered to a small number of women being treated for hypertension in pregnancy, isradipine was found to cross the placenta; however, the drug concentration in fetal plasma was considerably lower compared to maternal levels at delivery.
Isradipine should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.
Isradipine has produced maternotoxicity (reduced maternal weight gain) and reductions in birthweight and pup survival during reproductive studies in rats given an oral isradipine dosage of 20 and 60 mg/kg daily (50 and 150 times the maximum recommended human dosage, respectively) during the perinatal and postnatal period. In studies in pregnant rats receiving isradipine during organogenesis, dosages of 60 mg/kg daily impaired maternal weight gain but had no lasting effect on dams or offspring. The drug has produced maternotoxicity (reduced maternal weight gain) and increased fetal resorption during reproductive studies in rabbits given oral isradipine dosages of 3-10 mg/kg daily (7.5-25 times the maximum recommended human dosage).
It is not known whether isradipine is distributed in human milk. Because of the potential for serious adverse reactions to isradipine in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Isradipine peak plasma concentrations and bioavailability are increased in geriatric patients, however, the manufacturer states that therapy with the drug can be initiated with the usual initial adult dosage in such patients.
In geriatric patients, clearance of isradipine is decreased, resulting in 13 and 40% increases in peak plasma concentrations and AUC, respectively. The manufacturer states that therapy with the drug can be initiated with the usual initial adult dosage in such patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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