Prelizer (Bisoprolol Fumarate): A Highly Selective Beta-1 Blocker

Prelizer contains Bisoprolol Fumarate, which is a highly selective β1​ blocker. It is indicated for the treatment of hypertension, angina, and moderate to severe heart failure. It is not recommended for the emergency treatment of hypertensive crises. It belongs to the therapeutic class of Anti-adrenergic agents (Beta blockers) / Beta-adrenoceptor blocking drugs.

How Prelizer Works (Pharmacology)

Bisoprolol Fumarate works by:

• Selective $\beta$$1$​ Adrenergic Receptor Blockade: It selectively blocks β1​ adrenergic receptors primarily located in the heart and vascular smooth muscle. This high selectivity means it has less effect on β2​ receptors found in the lungs and peripheral blood vessels.
• Reduced Heart Rate and Cardiac Output: By blocking β1​ receptors in the heart, it reduces heart rate and cardiac output.
• Decrease in Arterial Hypertension: The reduction in heart rate and cardiac output leads to a decrease in arterial blood pressure.
• No Adverse Effect on Lipid Metabolism: Unlike some non-β1​ selective β-blockers, Bisoprolol does not adversely affect lipid metabolism; it does not cause changes in cholesterol fractions, including cardioprotective HDL-cholesterol, in long-term therapy.
• Pharmacokinetic Properties: Bisoprolol is almost completely (>90%) absorbed from the GI tract, with an absolute bioavailability of 88%. Food intake does not affect absorption. It has a balanced elimination via renal excretion (50% unchanged) and hepatic metabolism (50% to inactive metabolites, also renally excreted). Its elimination half-life is 10-12 hours, supporting a single daily dose.

Key Indications & Benefits

Prelizer is indicated for the treatment of:

• Hypertension (mild to moderate).
• Angina.
• Moderate to severe heart failure.

Dosage & Administration

Prelizer is for oral administration. The dosage of Bisoprolol fumarate must be individualized. Always consult a registered physician for medication use.

Adults:

• Mild to Moderate Hypertension:
  • Usual starting dose: 5 mg once daily (alone or added to a diuretic).
  • If response is inadequate, dose may be increased to 10 mg, and then, if necessary, to 20 mg once daily.
  • An appropriate interval for dose titration is 2 weeks.
  • Increasing the dose beyond 20 mg once daily typically provides only a small additional benefit.

Children:

• Safety and effectiveness in children have not been established.

Patients With Renal or Hepatic Impairment:

• Initial daily dose: 5 mg, similar to other patients.
• Caution in dose titration: Due to the possibility of drug accumulation, caution must be used when increasing the dose.
• Dialysis: Bisoprolol fumarate is generally not dialyzable, so drug replacement is not necessary for patients undergoing dialysis.

Geriatrics (Elderly):

• Dose adjustment is not usually necessary, unless there is significant renal or hepatic dysfunction.

Important Considerations & Warnings

It is crucial to discuss your full medical history with your doctor before taking Prelizer.

Contraindications:

• Cardiogenic shock.
• Overt heart failure.
• Second or third-degree A-V block.
• Right ventricular failure secondary to pulmonary hypertension.
• Sinus bradycardia.

Side Effects:

• Common: Fatigue, dizziness, headache, gastrointestinal disturbances (nausea, vomiting, diarrhea, constipation, abdominal pain), cold or numb extremities (e.g., hands and feet), muscle weakness or cramps.
• Less Common/Serious: Slower than normal heart rate (bradycardia), breathing difficulties due to narrowing of airways (bronchospasm) in people with asthma or COPD.

Pregnancy & Lactation:

• Pregnancy: Bisoprolol fumarate was not teratogenic in rats (up to 375 times human dose) or rabbits (up to 31 times human dose), but showed fetotoxicity/embryolethality at high doses in animal studies. There are no adequate studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
• Lactation: Small amounts of bisoprolol fumarate (<2% of the dose) have been detected in the milk of lactating rats. It is not known whether this drug is excreted in human milk. If use of Bisoprolol fumarate is considered essential, mothers should stop nursing.

Precautions & Warnings:

• Impaired Renal or Hepatic Function: Use caution when adjusting the dose in patients with renal or hepatic impairment due to the possibility of accumulation.
• Anaphylactic Reactions: Patients with a history of severe anaphylactic reactions may be more reactive to repeated challenges while taking beta-blockers and may be unresponsive to usual doses of epinephrine used to treat allergic reactions.

Drug Interactions:

• Other $\beta$-blocking Agents: Prelizer should not be combined with other $\beta$-blocking agents.
• Catecholamine-Depleting Drugs (e.g., reserpine or guanethidine): Monitor closely, as the added β-adrenergic blocking action may produce excessive reduction of sympathetic activity.
• Centrally Active Antihypertensive Agents (e.g., clonidine): β-blockers may worsen rebound hypertension upon clonidine withdrawal. If co-administered, the β-blocker should be withdrawn several days before clonidine. If replacing clonidine, introduce β-blockers several days after clonidine cessation.
• Antiarrhythmic Agents (e.g., disopyramide) or Myocardial Depressants: Use with care, especially with inhibitors of A-V conduction.
• Calcium Channel Blockers (particularly verapamil and diltiazem classes): Combined use can lead to prolongation of S-A and A-V conduction, especially in patients with impaired ventricular function or conduction abnormalities. This may result in severe hypotension, bradycardia, and cardiac failure.

Overdose Effects

• Overdose information is not provided in detail, but given the pharmacology, symptoms would likely involve severe bradycardia, hypotension, and potentially cardiac failure.
• Treatment: Would be symptomatic and supportive.

Storage Conditions

Keep in a dry place away from light and heat. Keep out of the reach of children.