This drug is considered as a potent drug with a long-half life that can be used once daily. Bisoprolol is generally well tolerated due to its β1-adrenergic receptor selectivity . It is a useful alternative to non-selective β-blocker drugs in the treatment of hypertension ( Carvedilol and Labetalol).
This drug can be used alone or in combination with other drugs to treat hypertension.Bisoprolol can be useful in patients with chronic obstructive pulmonary disease (COPD) due to its receptor selectivity.
Indications:
Bisoprolol is indicated for the treatment of
●Lowers high blood pressure helps prevent strokes, heart attacks, and kidney problems
●Treatment of Hypertension
●Treatment of stable chronic angina
Pharmacology
Mechanism of action:
Bisoprolol is a potent highly beta1-selective-adrenoceptor blocking agent, lacking intrinsic sympathomimetic. It only shows low affinity to the beta2-receptor of the smooth muscles of bronchi and vessels as well as to the beta2-receptors which is concerned with metabolic regulation. Its beta1-selectivity extends beyond the therapeutic dose range.
Though the mechanism of action of bisoprolol has not been fully elucidated in hypertension. Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. When β1-receptors are activated by adrenergic neurotransmitters such as epinephrine, both the blood pressure and heart rate increase, which leads to greater cardiovascular work, which increases the demand for oxygen. Bisoprolol reduce the output of renin in the kidneys, which normally increases blood pressure. some central nervous system effects of bisoprolol may include diminishing sympathetic nervous system output from the brain, decreasing blood pressure and heart rate.
Pharmacodynamics:
Bisoprolol decreases heart rate, chronotropy, decreases contractility (inotropy), and reduces blood pressure.The results of various clinical studies indicate that bisoprolol reduces cardiovascular mortality and all-cause mortality in patients with heart failure and decreased cardiac ejection fraction.
Pharmacokinetics:
Absorption: Bisoprolol is absorbed completely from the gastrointestinal tract. Together with the very small first pass effect in the liver, this results in a high bioavailability of approx90%. The plasma protein binding of bisoprolol is about 30 %. The distribution volume is 3.5 l/kg. The total clearance is approx. 15 l/h.
Bioavailability of bisoprolol is about 90% due to the minimal first pass effects.Absorption is unaffected by food intake. Peak plasma concentrations of bisoprolol are attained within 2-4 hours and steady-state concentrations are achieved within 5 days of administration.
Distribution: The volume of distribution of bisoprolol is 3.5 L/kg.The mean volume of distribution was found to be 230 L/kg in heart failure patientsThe plasma elimination half-life (10-12 hours) provides 24 hours efficacy following a once daily dosage.
About 50% of a single bisoprolol dose is metabolized mainly by the enzyme CYP3A4 to inactive metabolites.16
Elimination: Bisoprolol is excreted from the body by two routes. 50% is metabolised by the liver to inactive metabolites which are then excreted by the kidneys. The remaining 50% is excreted by the kidneys .The elimination takes place in the kidneys and the liver to the same extent. Bisoprolol is eliminated equally by both renal and hepatic pathways. About 50% of an oral dose is excreted unchanged in the urine with the remainder of the dose excreted as inactive bisoprolol metabolites. Under 2% of the ingested dose is found to be excreted in the feces.
Contraindications:
Bisoprolol is contra-indicated in patients with:
● hypersensitivity to the active substance
● acute heart failure
● cardiogenic shock
● Second or third degree AV
● sick sinus syndrome
● symptomatic bradycardia
● symptomatic hypotension
● severe bronchial asthma or severe chronic obstructive pulmonary disease
Side Effects:
● slower heart rate
● diarrhea
● weakness, tiredness
● dizziness,anxiety
● changes in sex drive or performance
● nausea
● dry or burning eyes
● cold or flu symptoms
● swelling in any part of your body
● Allergic reactions
● Changes to your heart rate.
● Heart problems.
● Sweating, Tremors
● Vomiting
Special Warning & Precaution:
Special Warnings: Applies only to chronic heart failure
Applies only to hypertension or angina pectoris
There is no therapeutic experience of bisoprolol treatment in heart failure in patients with the following diseases:
- insulin dependent diabetes mellitus (type I)
- severely impaired renal function
- congenital heart disease
- myocardial infarction within 3 months
Pregnant: Bisoprolol is having some pharmacological effects that may cause harmful effects on pregnancy and to newborn.
Bisoprolol is not recommended during pregnancy unless clearly necessary