Bisoprolol is indicated in the management of hypertension & in the treatment of angina. It may be used alone or in combination with other antihypertensive agents.
Beta-blocker; Antihypertensive
Bisoprolol Fumarate is the most selective ß1 blocker. It displays highest level of affinity for the ß1 receptor than any other beta-blocker available up to now. Selectively blocks ß1 adrenergic receptor in the heart and vascular smooth muscle and reduces heart rate and cardiac output resulting in decrease of arterial hypertension. Lipid metabolism can be adversely affected by ß-blockers, in patients with non-ß1 selective ß1-blocker, but Bisoprolol does not cause any change in the cholesterol fraction including the cardioprotective HDL-cholesterol, in long-term therapy.
The pharmacokinetic properties of Bisoprolol provide the prerequisite for a single daily dose and ensure an extremely low inter and intra-individual variability of the plasma concentration profiles. The high therapeutic reliability of Bisoprolol is based on these properties.
Absorption and bioavailability: Bisoprolol is almost completely (>90%) absorbed from the gastrointestinal tract. The high absorption rate and the small first-pass effect (<10%) lead to an absolute bioavailability of 88%. Concomitant food intake does not affect the absorption. Distribution: Bisoprolol is extensively distributed. The medium distribution volume is 3.51/kg.
Metabolism: Bisoprolol is metabolized via oxidative pathways with no subsequent conjugation. All metabolites, being very polar, are renally eliminated. The major metabolites in human plasma and urine were found to be without pharmacological activity. In vitro data from studies in human liver microsomes show that Bisoprolol is primarily metabolized via CYPSA4 (-95%) with CYP2D6 having only a minor role.
Elimination: The clearance of Bisoprolol is balanced between renal elimination of the unchanged molecule (-50%) and hepatic metabolism (-50%) to metabolites which are also renally excreted. The total clearance of Bisoprolol is approximately 15 I/h. Bisoprolol has an elimination half-life of 10-12 hours.
The dose of Bisoprolol must be individualized to the needs of the patient. The usual starting dose Bisoprolol 5 mg once daily. In some patients Bisoprolol 2.5 mg may be an appropriate starting dose. If the antihypertensive Effect of Bisoprolol 5 mg is inadequate, the dose may be increased to Bisoprolol 10 mg & then, if necessary, to 20 mg once daily.
Other β-blocking Agents: Bisoprolol Fumarate should not be combined with other β-blocking agents.
Catecholamine-Depleting Drugs: Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be monitored closely because the added β-adrenergic blocking action of bisoprolol fumarate may produce excessive reduction of sympathetic activity.
Centrally Active Antihypertensive Agents: β-blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the two drugs are coadministered, the β-blocker should be withdrawn several days before discontinuing clonidine. If replacing clonidine by β-blocker therapy, the introduction of β-blockers should be delayed for several days after clonidine administration has stopped (see also prescribing information for clonidine).
Antiarrhythmic Agents: Bisoprolol fumarate should be used with care when myocardial depressants or inhibitors of A-V conduction, such as certain calcium antagonists (particularly of the phenyl alkylamine (verapamil) and benzothiazepine (diltiazem) classes), or antiarrhythmic agents, such as disopyramide, are used concurrently.
Calcium Channel Blockers: Combined use of β-blockers and calcium channel blockers with negative inotropic effects can lead to prolongation of S-A and A-V conduction, particularly in patients with impaired ventricular function or conduction abnormalities. This may result in severe hypotension, bradycardia and cardiac failure.
Bisoprolol is contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, & marked sinus bradycardia. Impaired renal or hepatic function: Use caution in adjusting the dose of Bisoprolol in patients with renal or hepatic impairment. Risk of anaphylactic reaction: While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive torepeated challenge, accidental, diagnostic or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reaction.
Fatigue, dizziness, headache, disturbances of the gut such as nausea, vomiting, diarrhoea, constipation or abdominal pain, cold or numb extremities, e.g. hands & feet, muscle weakness or cramps, slower than normal heart beat (bradycardia), worsening of heart failure, sleep disturbance, depression, breathing difficulties due to a narrowing of the airways (bronchospasm) in people with asthma or COPD.
Pregnancy: Bisoprolol should not be used during pregnancy unless clearly necessary. If treatment with Bisoprolol is considered necessary, the uteroplacental blood flow & the foetal growth should be monitored. Lactation: It is not known whether this drug is excreted in human milk. Therefore, breast-feeding is not recommended during administration of Bisoprolol.
Keep in a dry place away from light and heat. Keep out of the reach of children.
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