Isradipine; Mechanism, Uses, Contraindications, Dosage, Side effects

Isradipine; Mechanism, Uses, Contraindications, Dosage, Side effects

Isradipine is a second generation calcium channel blocker that is used to treat hypertension. Isradipine is associated with a low rate of serum enzyme elevations during therapy but has not been linked convincingly to instances of clinically apparent liver injury.

Isradipine is a dihydropyridine calcium channel blockers with antihypertensive and vasodilator activities. Isradipine blocks the calcium entry through the calcium ion channels of coronary and peripheral vascular smooth muscle, thereby dilating coronary arteries and peripheral arterioles. This increases oxygen delivery due to an increased blood flow and reduces oxygen requirements due to a decrease in total peripheral resistance.

Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. It is structurally related to felodipine, nifedipine, and nimodipine and is the most potent calcium-channel blocking agent of the DHP class. Isradipine binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and arterial smooth muscle cells.

Mechanism of action of Isradipine

Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. CCBs target L-type calcium channels, the major channel in muscle cells that mediates contraction. Similar to other DHP CCBs, isradipine binds directly to inactive calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells. Alternative splicing of the alpha-1 subunit of the channel gives isradipine additional arterial selectivity. At therapeutic sub-toxic concentrations, isradipine has little effect on cardiac myocytes and conduction cells.

Indications of Isradipine

You Might Also Like   Midazolam; Uses, Dosage, Side Effects, Interactions, Pregnancy

Contra-Indications of Isradipine

  • Porphyria
  • An acute syndrome of the heart
  • Severe narrowing of the aortic heart valve
  • Severe heart failure
  • Abnormally low blood pressure
  • Kidney disease with a reduction in kidney function
  • Fluid Retention in the Legs, arms or hands
  • Blood Circulation Failure due to Serious Heart Condition
  • Chronic idiopathic constipation
  • Stomach or intestine blockage
  • Narrowing of the intestines
  • Decreased motility function of stomach or intestines
  • Heart attack
  • Allergies to Calcium Channel Blockers
  • Calcium Channel Blocking Agents-Dihydropyridines

Dosage of Isradipine

Strengths: 2.5 mg; 5 mg; 10 mg

Hypertension

Initial dose

  • Immediate-release capsules: 2.5 mg orally twice a day
  • Controlled-release tablets: 5 mg orally once a day
  • Maintenance dose: The dose may be adjusted as needed and tolerated in increments of 5 mg at 2 to 4-week intervals.

Side Effects of Isradipine

The most common 

More common

You Might Also Like   Ubiquinone - Uses, Dosage, Side Effects, Interactions

Rare

Drug Interactions of Isradipine

Isradipine  may interact with following drugs, supplements, & may change the efficacy of the drug

Pregnancy Category of Isradipine

FDA Pregnancy Category C

Pregnancy

This medication should not be taken by women who are or may become pregnant, as isradipine may cause harm to the developing baby if it is taken by the mother during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

You Might Also Like   Diclofenamide - Uses, Dosage, Side Effects, Interaction

Lactation

This medication should not be taken by women who are breastfeeding. The safety and effectiveness of using this medication have not been established for children.

References

  1. https://pubchem.ncbi.nlm.nih.gov

Isradipine

About the author

Translate »