Usage
- Bisoprolol + S-Amlodipine is prescribed for the treatment of hypertension (high blood pressure).
- Pharmacological Classification: Antihypertensive (combination of beta-blocker and calcium channel blocker).
- Mechanism of Action: This combination therapy targets two different mechanisms to control blood pressure. S-Amlodipine, a calcium channel blocker, relaxes blood vessels by inhibiting calcium ion influx across cell membranes. This reduces peripheral vascular resistance, thus lowering blood pressure. Bisoprolol, a beta-1 adrenergic receptor blocker, decreases heart rate and cardiac output, further contributing to blood pressure reduction. The combined action results in synergistic blood pressure control.
Alternate Names
- Bi-Amlodipine
- Bisoprolol/Amlodipine
- Bi Samlo
- Bisobis AM
How It Works
- Pharmacodynamics: S-Amlodipine causes vasodilation, reducing peripheral resistance and blood pressure. Bisoprolol reduces heart rate and myocardial contractility, which lowers cardiac output and blood pressure.
- Pharmacokinetics: Both drugs are absorbed orally. S-Amlodipine undergoes extensive hepatic metabolism, primarily by CYP3A4. Bisoprolol is partially metabolized by the liver and partially excreted unchanged in the urine.
- Mode of Action: S-Amlodipine blocks L-type calcium channels in vascular smooth muscle, leading to vasodilation. Bisoprolol selectively blocks beta-1 adrenergic receptors in the heart, inhibiting the sympathetic nervous system’s effects on heart rate and contractility.
- Elimination Pathways: S-Amlodipine is primarily eliminated through hepatic metabolism, with metabolites excreted in urine and feces. Bisoprolol is eliminated via both hepatic metabolism and renal excretion.
Dosage
Standard Dosage
Adults:
- Initial dose: Bisoprolol 2.5 mg and S-Amlodipine 2.5 mg once daily or Bisoprolol 5 mg and S-Amlodipine 5 mg once daily.
- The dosage may be increased to 10 mg of Bisoprolol and/or 10 mg of S-Amlodipine based on individual patient response and tolerance.
- Maximum dose: Bisoprolol 20 mg and S-Amlodipine 10 mg once daily.
Children:
- Not generally recommended for children under 12 years of age due to lack of established safety and efficacy data.
Special Cases:
- Elderly Patients: Start with a lower dose (e.g., Bisoprolol 2.5 mg and S-Amlodipine 2.5 mg) and titrate cautiously based on response and tolerability.
- Patients with Renal Impairment: For creatinine clearance less than 40 mL/min, start with a lower dose of Bisoprolol (2.5 mg) and titrate cautiously. S-Amlodipine dosage adjustments are usually not necessary.
- Patients with Hepatic Dysfunction: Start with a lower dose of both Bisoprolol (2.5 mg) and S-Amlodipine (2.5 mg) and titrate cautiously.
- Patients with Comorbid Conditions: Careful monitoring is necessary for patients with diabetes, thyroid disease, asthma, or other relevant medical conditions.
Clinical Use Cases
- The combination is typically not used in specific clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. It is primarily intended for chronic hypertension management.
Dosage Adjustments
- Adjust dosage based on individual patient response, tolerability, renal or hepatic function, and the presence of other medical conditions.
- In patients with renal or hepatic impairment, start with lower doses and titrate cautiously.
- Monitor closely for side effects and efficacy.
Side Effects
Common Side Effects
- Headache
- Dizziness
- Fatigue
- Nausea
- Peripheral edema (swelling, especially in the ankles and feet)
- Bradycardia (slow heart rate)
- Flushing
Rare but Serious Side Effects
- Severe hypotension (low blood pressure)
- Worsening heart failure
- Liver dysfunction
- Angioedema (swelling of the face, lips, tongue, or throat)
Long-Term Effects
- Long-term side effects are generally similar to the common side effects, and can include persistent peripheral edema, fatigue, and dizziness. Regular monitoring for cardiovascular events is crucial.
Adverse Drug Reactions (ADR)
- Severe hypotension
- Bradycardia with atrioventricular block
- Angioedema
Contraindications
- Severe bradycardia
- Second- or third-degree atrioventricular block (without a pacemaker)
- Sick sinus syndrome
- Cardiogenic shock
- Severe heart failure
- Hypersensitivity to bisoprolol, amlodipine, or any component of the formulation
Drug Interactions
- Other antihypertensive medications (additive hypotensive effects)
- Calcium channel blockers (increased risk of hypotension and bradycardia)
- Beta-blockers (additive bradycardia and negative inotropic effects)
- Digoxin (increased risk of bradycardia)
- Insulin or oral hypoglycemic agents (may mask symptoms of hypoglycemia)
- Grapefruit juice (may increase S-Amlodipine levels)
- CYP3A4 inhibitors (e.g., some antifungals, antibiotics) may increase S-Amlodipine levels
- CYP3A4 inducers (e.g., rifampin, St. John’s wort) may decrease S-Amlodipine levels
Pregnancy and Breastfeeding
- Pregnancy: Use with caution. Bisoprolol may cross the placenta and potentially affect fetal growth. S-Amlodipine’s safety during pregnancy is not well-established. Consult a doctor before use.
- Breastfeeding: Both drugs are excreted in breast milk. Monitor infants for potential adverse effects like bradycardia and hypotension. Use with caution; consult a doctor before use.
Drug Profile Summary
- Mechanism of Action: S-Amlodipine: Calcium channel blocker (vasodilation); Bisoprolol: Beta-1 blocker (decreased heart rate and cardiac output).
- Side Effects: Headache, dizziness, fatigue, nausea, peripheral edema, bradycardia.
- Contraindications: Severe bradycardia, heart block, sick sinus syndrome, cardiogenic shock, severe heart failure, hypersensitivity.
- Drug Interactions: Other antihypertensives, calcium channel blockers, beta-blockers, digoxin, insulin/oral hypoglycemics, grapefruit juice, CYP3A4 inhibitors/inducers.
- Pregnancy & Breastfeeding: Use with caution; consult a doctor. Monitor for adverse effects in infants.
- Dosage: See detailed dosage section above.
- Monitoring Parameters: Blood pressure, heart rate, signs of heart failure, liver function tests, renal function tests, and electrolyte levels.
Popular Combinations
While Bisoprolol + S-Amlodipine is itself a combination, it may be further combined with other antihypertensives like thiazide diuretics (e.g., hydrochlorothiazide) or ACE inhibitors (e.g., lisinopril) if blood pressure control is inadequate. The rationale for combining with a thiazide diuretic or an ACE inhibitor is to achieve synergistic blood pressure lowering by targeting different mechanisms involved in blood pressure regulation.
Precautions
- General Precautions: Pre-screening for allergies, heart conditions (e.g., bradycardia, heart block), liver or kidney dysfunction is essential. Monitor blood pressure, heart rate, and electrolyte levels regularly.
- Specific Populations:
- Pregnant Women: Use with caution only if the benefit outweighs the risk. Consult a doctor.
- Breastfeeding Mothers: Use with caution. Monitor infant for adverse effects. Consult a doctor.
- Children & Elderly: Not recommended for children under 12. Start with lower doses in elderly patients.
- Lifestyle Considerations: Limit alcohol intake, as it may enhance hypotensive effects. Avoid grapefruit juice. Advise patients about potential dizziness and the need for caution when driving or operating machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Bisoprolol + S-Amlodipine?
A: The initial recommended dose for adults is typically Bisoprolol 2.5 or 5 mg and S-Amlodipine 2.5 or 5 mg once daily. This can be increased up to a maximum of Bisoprolol 20 mg and S-Amlodipine 10 mg per day as needed for blood pressure control. Dose adjustments are necessary for patients with renal or hepatic dysfunction and elderly patients.
Q2: What are the common side effects of Bisoprolol + S-Amlodipine?
A: Common side effects include headache, dizziness, fatigue, nausea, peripheral edema, and bradycardia.
Q3: How does this combination medication work to lower blood pressure?
A: It works by combining two different mechanisms. S-Amlodipine relaxes and widens blood vessels, while Bisoprolol reduces heart rate and cardiac output. This combined action leads to a greater decrease in blood pressure than either drug alone.
Q4: Can Bisoprolol + S-Amlodipine be used during pregnancy or breastfeeding?
A: It should be used with caution during pregnancy and breastfeeding. Consult a doctor for advice, as both medications can cross the placenta and are present in breast milk.
Q5: Are there any specific contraindications for using this medication?
A: Yes. It is contraindicated in individuals with severe bradycardia, second- or third-degree heart block (without a pacemaker), sick sinus syndrome, cardiogenic shock, severe heart failure, and hypersensitivity to either drug.
Q6: What are the potential drug interactions with Bisoprolol + S-Amlodipine?
A: Potential drug interactions exist with other antihypertensive medications, calcium channel blockers, beta-blockers, digoxin, and CYP3A4 inhibitors or inducers. It’s important to inform your doctor about all other medications, supplements, and herbal products you are taking.
Q7: How should I monitor a patient taking this medication?
A: Monitor blood pressure, heart rate, signs and symptoms of heart failure (e.g., shortness of breath, edema), and renal and hepatic function. Electrolyte monitoring may also be necessary.
Q8: What should I do if a patient misses a dose?
A: If a dose is missed, instruct the patient to take it as soon as remembered unless it’s almost time for the next dose. Do not double the dose.
Q9: Can this medicine be stopped abruptly?
A: No. Bisoprolol, in particular, should not be stopped abruptly. The dosage should be gradually tapered under medical supervision to avoid potential rebound hypertension or other adverse cardiovascular events.
Q10: What are the signs of an overdose?
A: Signs of overdose can include severe hypotension, bradycardia, dizziness, and fainting. Seek immediate medical attention if overdose is suspected.
