Drug information of Bisoprolol
Mechanism of effect
Bisoprolol fumarate is a beta1-selective (cardioselective) adrenoceptor blocking agent without significant membrane stabilizing activity or intrinsic sympathomimetic activity in its therapeutic dosage range. Cardioselectivity is not absolute, however, and at higher doses (greater than or equal to 20 mg) Bisoprolol fumarate also inhibits beta2-adrenoceptors, chiefly located in the bronchial and vascular musculature; to retain selectivity it is therefore important to use the lowest effective dose.
Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist.
Well absorbed. Bioavailability > 80%. Absorption is not affected by food. Binding to serum proteins is approximately 30%. Peak plasma concentrations occur within 2-4 hours. The first pass metabolism of Bisoprolol fumarate is about 20%Approximately 50% of the dose is metabolized primarily metabolized by CYP3A4 to inactive metabolites. Approximately 50% of the total orally administered dose is excreted unchanged in urine with the remainder appearing as inactive metabolites. Less than 2% of the dose is excreted in the feces. Half life: 9-12 hours; prolonged in the elderly and those with decreased renal function
Drug indications(hypertension (high blood pressure
Usual Adult Dose for Hypertension
Initial dose: 5 mg orally once a day
Dose Titration: If desired response is not achieved, may increase the dose to 10 mg, then 20 mg if necessary
Maximum dose: 20 mg per day
Drug contraindicationshypersensitivity to drug or its components. , sinus bradycardia , cardiogenic shock , overt cardiac failure , Second- or third-degree AV block
Side effectsnausea , Headache , insomnia , chest pain , dry mouth , dizziness , vomiting , fatigue , Bradycardia , vertigo , Depression , Diarrhea , Dyspnea , asthenia , Rhinitis , edema , Cough , sinusitis , Arthralgia , bronchospasm , pharyngitis , sweating , Vivid dreams
InteractionsDrospirenone , Neostigmine , formoterol , Atenolol , Aripiprazole , Amlodipine , Aminophiline , Amiodarone , Olanzapine , Yohimbine , Enzalutamide , Phentolamine Mesylate , Donepzil , Carvedilol , Ketoconazole , Clarithromycin , Clobazam , Clozapine , Clomipramine , Hydrochlorothiazide , Vardenafil , Valsartan , Verapamil , Voriconazole , Captopril , Nifedipine , Nilotinib , Nimodipine , Nicorandil , Hydralazine , Hydroxychloroquine , Metoprolol , Metolazone , Mefenamic acid , Meloxicam , Midodrine , Naphazoline , Losartan , Lovastatin , Levodopa/carbidopa , Lidocaine , Minoxidil , Mycophenolate mofetil , Fluoxetine , Fluconazole , Phenytoin , Furosemide , Galantamine , Gliclazide , Celexib , Sotalol , Citalopram , Sildenafil , Cyclosporine , Fluvoxamine , Dipyridamole , Diltiazem , Rituximab , Salbutamol , Salmeterol , Sertraline , Piroxicam , pimecrolimus , Tadalafil , Doxycycline , Duloxetine , Dihydroergotamine , Imipramine , Bupropion , Bortezomib , Bosentan , Paroxetine , Posaconazole , Enalapril , Octreotide acetate , Ibuprofen , Itraconazole , Isoniazid , Imatinib , ritodrine , Doxazosin , Dolasetron , Penbutolol , lipiodol , Telmisartan , Nebivolol , ProHance , Treprostinil , Oxtriphylline , Blonanserin , Florbetapir F18
1- In general, beta-blocking agents should be avoided in patients with overt congestive failure. However, in some patients with compensated cardiac failure it may be necessary to utilize them. In such a situation, they must be used cautiously.
2- Exacerbation of angina pectoris, and in some instances, myocardial infarction or ventricular arrhythmia, have been observed in patients with coronary artery disease following abrupt cessation of therapy with beta-blockers.
3- PATIENTS WITH BRONCHOSPASTIC DISEASE SHOULD, IN GENERAL, NOT RECEIVE BETA-BLOCKERS.
4- Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery; however, the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures.
5- Use caution in patients with renal or hepatic impairment
Points of recommendation
1-Patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents, should be cautioned that beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia, and Bisoprolol fumarate should be used with caution
2-If you need surgery, tell the surgeon ahead of time that you are using Bisoprolol You may need to stop using the medicine for a short time.
3- Take Bisoprolol at the same time each day