Bepridil; Uses, Dosage, Side Effects, Interactions, Pregnancy

Bepridil; Uses, Dosage, Side Effects, Interactions, Pregnancy

Bepridil is a long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist.

Bepridil Hydrochloride is the hydrochloride salt form of bepridil, a calcium antagonist and class IV anti-arrhythmic agent. Bepridil hydrochloride blocks calcium entry through membranous calcium channels of coronary and peripheral vascular smooth muscle, thereby dilating coronary arteries and peripheral arterioles. This increases oxygen delivery and reduces oxygen requirements. This drug is used to treat chronic stable and variant angina pectoris.

Mechanism of action of Bepridil

Bepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes in vitro, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works.

Indications of Bepridil

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

Contra-Indications of Bepridil

  • Extreme loss of body water
  • The high amount of potassium in the blood
  • Renal artery stenosis
  • Liver problems
  • Blockage of a bile duct
  • Kidney disease with the reduction in kidney function
  • Pregnancy
  • Second and third trimester of pregnancy
  • Biliary obstructive disorders.
  • Severe hepatic impairment.
  • Hypersensitivity to the active substance or to any of the excipients

Hypersensitivity, history of serious ventricular or atrial arrhythmias, uncompensated cardiac insufficiency, congenital QT interval prolongation.

Dosage of Bepridil

Strengths: 200 mg ,300mg , 400 mg

Angina pectoris

  • Initially, 200 mg/day.
  • If necessary, increase to 300 mg/day after 10 days.
  • Max dose: 400 mg once daily.

Side Effects of Bepridil

The most common

Common

You Might Also Like   Cefepime; Uses, Dosage, Side Effects, Interactions

Rare

Drug Interactions of Bepridil

Bepridil may interact with following drugs, supplyments, & may change the efficacy of drugs

Pregnancy & Lactation of Bepridil

FDA Pregnancy Category C

Pregnancy

Reproductive studies (fertility and peri-postnatal) have been conducted in rats. Reduced litter size at birth and decreased pup survival during lactation was observed at maternaldosages 37 times (on a mg/kg basis) the maximum daily recommended therapeutic dosage.In teratology studies, no effects were observed in rats or rabbits at these same dosages.

Lactation

Bepridil is excreted in human milk. Bepridil concentration in human milk is estimated to reach about one third the concentration in serum. Because of the potential for serious adverse reactions in nursing infants from  bepridil a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.The safety and effectiveness of bepridil in children have not been established.

You Might Also Like   Abortion Pill Mifepristone - Indications, Contraindication

References

  1. Bepridil

About the author

Translate »