Vascor

Vascor Uses, Dosage, Side Effects, Food Interaction and all others data.

A long-acting, non selective, calcium channel blocker 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. It is no longer marketed in the United States, as it has been implicated in causing ventricular arrhythmias (ie. Torsade de pointes).

Vascor is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride.

Trade Name Vascor
Availability Discontinued
Generic Bepridil
Bepridil Other Names Bepadin, Bepridil
Related Drugs amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide, atenolol, diltiazem, nitroglycerin
Type
Formula C24H34N2O
Weight Average: 366.5396
Monoisotopic: 366.26711372
Protein binding

99%

Groups Approved, Withdrawn
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Vascor
Vascor

Uses

For the treatment of hypertension, and chronic stable angina (classic effort-associated angina).

How Vascor works

Vascor 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. Vascor 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. Vascor 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.

Toxicity

There has been one experience with overdosage in which a patient inadvertently took a single dose of 1600 mg of bepridil. The patient was observed for 72 hours in intensive care, but no significant adverse experiences were noted.

Food Interaction

  • Avoid alcohol. Alcohol can potentiate hypotension and dizziness when taken with this drug.
  • Take with food. Food reduces nausea.

[Moderate] MONITOR: Grapefruit juice may increase the plasma concentrations of orally administered drugs that are substrates of the CYP450 3A4 isoenzyme.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability).

In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands.

Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.

Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.

MANAGEMENT: Patients who regularly consume grapefruit or grapefruit juice should be monitored for adverse effects and altered plasma concentrations of drugs that undergo significant presystemic metabolism by CYP450 3A4.

Grapefruit and grapefruit juice should be avoided if an interaction is suspected.

Orange juice is not expected to interact with these drugs.

Vascor Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

Vascor multivitamins interaction

[Moderate] Calcium-containing products may decrease the effectiveness of calcium channel blockers by saturating calcium channels with calcium.

Calcium chloride has been used to manage acute severe verapamil toxicity.

Management consists of monitoring the effectiveness of calcium channel blocker therapy during coadministration with calcium products.

Elimination Route

Rapidly and completely absorbed after oral administration.

Half Life

24-50 hours

Innovators Monograph

You find simplified version here Vascor

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0002448
http://classyfire.wishartlab.com/tax_nodes/C0002279
http://classyfire.wishartlab.com/tax_nodes/C0000185
http://classyfire.wishartlab.com/tax_nodes/C0004204
http://classyfire.wishartlab.com/tax_nodes/C0003901
http://classyfire.wishartlab.com/tax_nodes/C0002673
http://classyfire.wishartlab.com/tax_nodes/C0000284
http://classyfire.wishartlab.com/tax_nodes/C0003899
http://classyfire.wishartlab.com/tax_nodes/C0003449
http://classyfire.wishartlab.com/tax_nodes/C0002239
http://classyfire.wishartlab.com/tax_nodes/C0001167
http://classyfire.wishartlab.com/tax_nodes/C0004139
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3061
http://www.hmdb.ca/metabolites/HMDB0015374
http://www.genome.jp/dbget-bin/www_bget?drug:D07520
http://www.genome.jp/dbget-bin/www_bget?cpd:C06847
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2351
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506353
https://www.chemspider.com/Chemical-Structure.2261.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=78577
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=1436
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=3061
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1008
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000525
http://www.pharmgkb.org/drug/PA164754755
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2337
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/BEP
http://www.rxlist.com/cgi/generic2/bepridil.htm
https://www.drugs.com/mtm/bepridil.html
https://en.wikipedia.org/wiki/Bepridil
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