Drug information of Bepridil

Bepridil


Bepridil is in a class of drugs called calcium channel blockers. Bepridil relaxes (widens) your blood vessels (veins and arteries), which makes it easier for your heart to pump and reduces its workload.

Bepridil is used to treat hypertension (high blood pressure) and to treat angina (chest pain).

Mechanism of effect

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   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.

Pharmacokinetics

Absorption:

Rapidly and completely absorbed after oral administration.

Protein binding:

99%

Metabolism:

Hepatic.

Half life:

24-50 hours

 

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.

Drug indications

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

Dosage

Usual Adult Dose for Angina Pectoris Prophylaxis

Initial dose: 200 mg orally once a day.
Maintenance dose: 300-400 mg orally once a day.

Side effects

If you experience any of the following serious side effects, stop taking bepridil and call your doctor immediately or seek emergency medical treatment:

  • an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives);
  • unusually fast or slow heartbeat;
  • fainting or severe dizziness;
  • chest pain;
  • abnormal behavior or psychosis;
  • yellowing of your skin or eyes (jaundice); or
  • swelling of your legs or ankles.

Other, less serious side effects may be more likely to occur. Continue to take bepridil and talk to your doctor if you experience

  • unusual fatigue or tiredness;
  • nausea, upset stomach, diarrhea, or constipation;
  • headache;
  • nervousness or mild dizziness;
  • insomnia; or
  • tremor (shaking).

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

Interactions

Histrelin , saquinavir , Palonosetron , vandetanib , Goserelin , Vasopressin , Halofantrine , Grepafloxacin , cobicistat , Terfenadine , Abarelix , Asenapine , Alfuzosin , Amisulpride , Perflutren , Betrixaban , Apalutamide , Pitolisant , Amitriptyline , Amiodarone , Epirubicin , Adenosine , Erythromycin , Ofloxacin , levomethadyl acetate , ozanimod , lefamulin , lofexidine , macimorelin , selpercatinib , norfloxacin , Eliglustat , Romidepsin , conivaptan , bosutinib , Pasireotide , Siponimod , Lomefloxacin , gilteritinib , glasdegib , Ceritinib , Nilutamide , Crizotinib , Edoxaban , Telavancin , Deutetrabenazine , Entrectinib , Cabozantinib , Foscarnet , lenvatinib , encorafenib , midostaurin , Triclabendazole , ivosidenib , Paliperidone , Pazopanib , ezogabine , Iloperidone , Pimavanserin , Degarelix , Arsenic trioxide , Efavirenz , Telaprevir , Gatifloxacin , Trimeprazine , Triflupromazine , Idarubicin , Anagrelide , Fosphenytoin , Promazine , probucol , Abiraterone , Panobinostat , Ribociclib , Dofetilide , Ibutilide , Eribulin , Inotuzumab‎ , Chloroquine , sparfloxacin , Mesoridazine , Procainamide , Polyethylene glycol , Mefloquine , boceprevir , Droperidol , Halothane , vemurafenib , Osimertinib , Quinine , Fosamprenavir , Ivabradine , Mifepristone , Dolasetron , Liposomal Amphotericin-B , Telithromycin , mitotane , Mirtazapine , primaquine , Apomorphine , valbenazine , Amprenavir , Ziprasidone , propoxyphene , protriptyline , ISOPROTERENOL , dronedarone , ritonavir , Toremifene , Tamoxifen , Metaproterenol , Prochlorperazine , Quinidine , Amoxapine , Clofazimine , Rifabutin , Ranolazine , Pentamidine , Quetiapine , lithium , Enzalutamide , Flecainide , Bicalutamide , ritodrine , Leuprolide acetate , escitalopram , Clarithromycin , Chlorpromazine , Colchicine , Clozapine , Clomipramine , Solifenacin , Hydroxychloroquine , Vardenafil , Venlafaxine , Voriconazole , Carbamazepine , Ketoconazole , Maprotiline , Methadone , Moxifloxacin , Nortriptyline , Nilotinib , Haloperidol , Fluoxetine , Fluconazole , Fingolimod , Granisetron , Lapatinib , Levofloxacin , Sevoflurane , Ciprofloxacin , Citalopram , Cisapride , Flutamide , Fluphenazine , Doxorubicin , Disopyramide , Sunitinib , Sertraline , Sotalol , Sorafenib , Tizanidine , Thioridazine , Gemifloxacin , Daunorubicin , Desipramine , Doxepin , Trazodone , Tramadol , Terbutaline , Trifluoperazine , Triptorelin , Trimipramine , Propafenone , Promethazine , Posaconazole , Pimozide , Tacrolimus , Tetrabenazine , Oxaliplatin , Ondansetron , Oxytocin , Itraconazole , Imipramine , Papaverine , bedaquiline , Dasatinib , Vernakalant , Venetoclax , Remoxipride , Fidaxomicin
 

Alerts

Before taking this medication, tell your doctor if you have

  • kidney disease;
  • liver disease; or
  • another disease of the heart or blood vessels, such as sick sinus syndrome, irregular heartbeats, heart failure, low blood pressure, or coronary artery disease.

You may not be able to take bepridil, or you may require a lower dose or special monitoring during treatment if you have any of the conditions listed above.

Bepridil passes into breast milk and may harm a nursing infant. Do not take bepridil without first talking to your doctor if you are breast-feeding a baby.

Points of recommendation

Take bepridil exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

Do not stop taking this medication unless your doctor approves. If you stop taking your medication, your condition could become much worse.

Follow any diet or exercise recommendations for your condition.

Store bepridil at room temperature away from moisture and heat.

Symptoms of a bepridil overdose include dizziness, weakness, chest pain, shortness of breath, fainting, unusually fast or slow heartbeat, coma, slurred speech, and confusion.

Use alcohol cautiously. Alcohol may further lower blood pressure and increase drowsiness and dizziness while you are taking bepridil.

Follow any recommendations your doctor makes about diet or exercise.

Pregnancy level

C

Bepridil has been assigned to pregnancy category C by the FDA. Animal studies revealed decreased litter size in rats. There are no controlled data in human pregnancy. Bepridil should only be given during pregnancy when benefit outweighs risk.

Bepridil is known to cross the human placenta, but experience in human pregnancy has not been reported.

Breast feeding warning

Bepridil is excreted into human milk. The milk to serum bepridil concentration ratio is about 1:3. There are no reports of the use of bepridil during human lactation. The manufacturer recommends that due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Drug forms

Vascor

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