Bisoprolol; Uses, Dosage, Side Effects, Interactions, Pregnancy

Bisoprolol Fumarate is the fumarate salt of a synthetic phenoxy-2-propanol-derived cardioselective beta-1 adrenergic receptor antagonist with antihypertensive and potential cardioprotective activities. Devoid of intrinsic sympathomimetic activity, bisoprolol selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, decreasing cardiac contractility and rate, reducing cardiac output, and lowering blood pressure. In addition, this agent may exhibit antihypertensive activity through the inhibition of renin secretion by juxtaglomerular epithelioid (JGE) cells in the kidney, thus inhibiting activation of the renin-angiotensin system (RAS). Bisoprolol has been shown to be cardioprotective in animal models.

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Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. Bisoprolol is structurally similar to metoprolol, acebutolol and atenolol in that it has two substituents in the para position of the benzene ring. The β1-selectivity of these agents is thought to be due in part to the large substituents in the para position. At lower doses (less than 20 mg daily), bisoprolol selectively blocks cardiac β1-adrenergic receptors with little activity against β2-adrenergic receptors of the lungs and vascular smooth muscle.

Mechanism of Action of Bisoprolol

Bisoprolol selectively blocks catecholamine stimulation of β1-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. At higher doses (e.g. 20 mg and greater) bisoprolol may competitively block β2-adrenergic receptors in bronchial and vascular smooth muscle causing bronchospasm and vasodilation.Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. Activation of β1-receptors (located mainly in the heart) by epinephrine increases heart rate and the blood pressure causing the heart to consume more oxygen. β1-adrenergic blocking agents such as bisopolol lower the heart rate and blood pressure and may be used to reduce workload on the heart and hence oxygen demands. They are routinely prescribed in patients with ischemic heart disease. In addition, β1-selective blockers prevent the release of renin, a hormone produced by the kidneys causes constriction of blood vessels. Bisoprolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane-stabilizing activity.

Indications of Bisoprolol

• Angina pectoris
• High blood pressure (Hypertension)
• Migraines
• Nonvalvular atrial fibrillation
• Acute hemodynamically stable myocardial infarction
• Atrial fibrillation
• Supraventricular Tachycardia
• Mitral valve prolapse
• Angina pectoris prophylaxis
• Benign essential tremor
• Heart attack
• Heart failure
• Left ventricular dysfunction
• Migraine prevention
• Supraventricular arrhythmias
• Chronic, stable Angina pectoris
• Perioperative arrhythmia
• Supraventricular tachycardia
• Heart failure
• Mitral valve prolapse
• Angina pectoris prophylaxis
• Premature ventricular depolarizations
• For management of heart failure, angina pectoris, and mild to moderate hypertension and for secondary prevention of myocardial infarction (MI).

Contra Indications of Bisoprolol

• Complete Heart Block
• Second Degree Atrioventricular Heart Block
• Sinus Bradycardia
• Occasional Numbness
• Prickling or Tingling of Fingers and Toes
• Asthma
• Severe Chronic Obstructed Lung Disease
• Severe Renal Impairment
• Psoriasis
• Blood Circulation Failure due to Serious Heart Condition
• Abnormal Liver Function Tests
• Pregnancy
• Anaphylactic Shock due to Allergy Shots
• Acutely Decompensated HF Requiring Parenteral Inotropic Therapy

Dosage of Bisoprolol

Strengths: 1.25mg; 2.5mg; 5 mg; 7.5mg ;10 mg

• 1.25mg bisoprolol once daily for one week
• 2.5mg bisoprolol once daily for one week
• 3.75mg bisoprolol once daily for one week
• 5mg bisoprolol once daily for four weeks
• 7.5mg bisoprolol once daily for four weeks
• 10mg bisoprolol once daily for maintenance (on-going) therapy.

The maximum recommended daily dose is 10mg bisoprolol.

 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

Side Effects of Bisoprolol

The most common

• Dry cough
• Depression
• Dizziness and light-headedness due to low blood pressure
• Fatigue, especially in the early stages
• Mouth dryness in the early stages
• The most commonrn (a burning feeling in the chest, behind the breastbone or gullet)
• Abdominal or stomach pain
• Constipation
• High blood pressure
• Nausea ,vomiting,
• painful or swollen gums
• numbness or heavy feeling in the jaw
• dull, aching pain in the hip, groin, or thigh
• stomach pain,
• headache,
• reversible hair loss or thinning, and
• fever.

Common

• chills or fever
• headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in chest
• excessive sweating
• sudden drowsiness or need to sleep
• coughing up blood
• liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
• decreased amount of urine

Rare

• Anxiety
• change in vision
• chest pain or tightness
• confusion
• cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• hallucinations
• headache
• irritability
• lightheadedness
• cold and clammy skin
• fast and shallow breathing
• swelling of your feet, legs, or hands purple spot on your skin caused by internal bleeding
• fast or abnormal heart rate or palpitations
• loss of appetite
• lower back, side, or stomach pain
• mental depression
• muscle pain or cramps

Drug Interaction of Bisoprolol

Bisoprolol may interact with following drugs, supplements, & may change the efficacy of drugs

• aminophylline
• asthma medications (e.g., theophylline)
• diabetes medications (e.g., glyburide)
• calcium channel blocker medicines (e.g., diltiazem, nifedipine, verapamil)
• diltiazem
• medications for abnormal heart rhythms (e.g., disopyramide)
• nitroglycerin
• nonsteroidal anti-inflammatory medications (NSAIDs; e.g., indomethacin, naproxen)
• oral diabetes medications (e.g., metformin, pioglitazone)
• pentoxifylline
• monoamine oxidase (MAO) inhibitors (e.g., phenelzine, selegiline, )
• other beta-blockers (e.g., propranolol, metoprolol)
• oxtriphylline
• verapamil

Pregnancy & Lactation of Bisoprolol

 FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if bisoprolol passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.

References

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