Celiprolol Hydrochloride

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Generic Name of Celiprolol Hydrochloride - Learn More

Celiprolol Hydrochloride

Celiprolol Hydrochloride Precaution - What You Need to Know

- Special Populations: Celiprolol, a beta-blocker with additional vasodilatory properties, should be used cautiously in pregnant women. It is classified as a pregnancy category C drug, meaning potential risks to the fetus cannot be ruled out, and it should only be used if the potential benefits outweigh the risks. It is not known whether Celiprolol is excreted in human breast milk, so breastfeeding should be approached with caution. In elderly patients, lower doses may be needed, and they should be monitored for side effects, particularly bradycardia or hypotension.
- Monitoring Parameters: Patients should have their heart rate, blood pressure, and electrocardiogram (ECG) monitored regularly during treatment, especially in the initial stages or during dose escalation. Kidney and liver function should be checked, particularly in patients with pre-existing conditions, as Celiprolol is metabolized in the liver and excreted through the kidneys.
- Misuse or Dependency: Celiprolol has no known risk of misuse or dependency, as it does not produce addictive effects. However, sudden discontinuation should be avoided, as it may precipitate withdrawal symptoms, particularly exacerbations of angina or hypertension. Gradual tapering of the dose is recommended if the drug needs to be discontinued.

Celiprolol Hydrochloride Indication - Uses and Benefits

- Primary Indications: Celiprolol is primarily used for the management of:
- Hypertension (High Blood Pressure): Celiprolol is used to lower blood pressure by blocking beta-adrenergic receptors and promoting vasodilation, making it effective in managing both systolic and diastolic blood pressure.
- Chronic Stable Angina: It is used to prevent angina attacks by reducing myocardial oxygen demand and improving blood flow.
- Off-Label Uses: Celiprolol is occasionally used in the treatment of certain arrhythmias, particularly those related to atrial fibrillation, due to its beta-blocking effects.
- Evidence-Based Context: Celiprolol is considered a second-line option for hypertension, particularly in patients who may benefit from its additional vasodilatory effects. Unlike other beta-blockers, it does not exacerbate symptoms of peripheral vascular disease due to its vasodilatory properties.

Celiprolol Hydrochloride Contraindications - Important Warnings

- Exclusion Criteria: Celiprolol should be avoided in patients with:
- Severe Bradycardia: Celiprolol can further slow the heart rate, potentially leading to severe bradycardia, which could result in hemodynamic instability.
- Heart Block (Second- or Third-Degree): Since Celiprolol has beta-blocking properties, it may worsen heart block by inhibiting the conduction of electrical impulses within the heart.
- Hypotension: Patients with significantly low blood pressure should not use Celiprolol, as it can exacerbate hypotension.
- Asthma and Chronic Obstructive Pulmonary Disease (COPD): Although Celiprolol is a selective beta-1 blocker, at higher doses, it may still affect beta-2 receptors in the lungs, potentially worsening respiratory conditions such as asthma and COPD.
- Severe Renal or Hepatic Impairment: Celiprolol is contraindicated in patients with severe renal or hepatic dysfunction due to the potential accumulation of the drug and its metabolites.
- Rationale: These contraindications are based on Celiprolol’s effects on heart rate, blood pressure, and respiratory function, which could be exacerbated in patients with certain pre-existing conditions.

Celiprolol Hydrochloride Side Effects - What to Expect

- Common Side Effects:
- Fatigue: As with most beta-blockers, Celiprolol may cause fatigue or lethargy, particularly during the initial phases of treatment.
- Dizziness or Lightheadedness: Especially when standing up quickly (orthostatic hypotension), dizziness can occur due to the blood pressure-lowering effects of the drug.
- Nausea and Diarrhea: Gastrointestinal discomfort, such as nausea or diarrhea, is possible but generally mild.
- Bradycardia: A slowing of the heart rate is a typical side effect, particularly at higher doses or in those with preexisting bradycardia.
- Serious Side Effects:
- Heart Block: In patients with preexisting conduction issues or those who are sensitive to beta-blockers, Celiprolol may exacerbate heart block, which can be life-threatening.
- Severe Hypotension: Excessive lowering of blood pressure could lead to dizziness, fainting, or shock in extreme cases.
- Respiratory Symptoms: While Celiprolol is selective for beta-1 receptors, high doses can still affect beta-2 receptors and may worsen symptoms of asthma or chronic obstructive pulmonary disease (COPD), such as wheezing or shortness of breath.
- Liver Enzyme Elevation: Rarely, Celiprolol can lead to liver enzyme elevation or hepatic dysfunction, especially in patients with preexisting liver conditions.
- Mitigation and Monitoring: Regular monitoring of heart rate, blood pressure, and liver function is essential, particularly when starting or adjusting the dose. Patients with asthma or COPD should be carefully monitored for any respiratory worsening. If serious side effects like heart block, significant bradycardia, or hypotension occur, the drug should be discontinued immediately.

Celiprolol Hydrochloride Pregnancy Category ID - Safety Information

2

Celiprolol Hydrochloride Mode of Action - How It Works

- Mechanism: Celiprolol is a selective beta-1 adrenergic blocker with additional vasodilatory properties. It works by binding to beta-1 receptors in the heart, which reduces the heart rate and the force of contraction, ultimately lowering cardiac output and blood pressure. The drug also has partial agonist activity at beta-2 receptors, which causes peripheral vasodilation, helping to reduce vascular resistance. This dual action of beta-blockade and vasodilation helps to manage hypertension and prevent angina by lowering the heart’s oxygen demand and improving blood flow.
- Pharmacodynamics and Pharmacokinetics: Celiprolol is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1-2 hours. It has a relatively long half-life (approximately 6-8 hours), which allows for twice-daily dosing. The drug undergoes extensive metabolism in the liver and is excreted mainly in the urine. Its effects on both beta-1 receptors and vasodilation provide an advantage in treating conditions like hypertension and chronic angina, where both heart rate control and vascular tone are important.
- Distinctive Action: Unlike traditional beta-blockers, Celiprolol’s partial agonist activity at beta-2 receptors helps it avoid some of the negative effects typically seen with non-selective beta-blockers, such as worsening peripheral vascular disease or exacerbating symptoms of asthma.

Celiprolol Hydrochloride Drug Interactions - What to Avoid

- Drug-Drug Interactions:
- Calcium Channel Blockers: Co-administration with calcium channel blockers (especially those with negative chronotropic effects like verapamil or diltiazem) can lead to severe bradycardia, hypotension, or heart block.
- Other Beta-Blockers: Using Celiprolol in combination with other beta-blockers increases the risk of bradycardia and hypotension. This combination should be avoided unless necessary and closely monitored.
- Antiarrhythmic Drugs: Antiarrhythmic agents like amiodarone or digoxin can have additive effects with Celiprolol, potentially causing bradycardia or worsening heart block.
- NSAIDs (Non-Steroidal Anti-Inflammatory Drugs): Chronic use of NSAIDs may reduce the antihypertensive efficacy of Celiprolol by inhibiting renal prostaglandin synthesis, which can impair the vasodilatory effect of the drug.
- Insulin or Oral Hypoglycemics: Beta-blockers, including Celiprolol, can mask the symptoms of hypoglycemia (such as tachycardia), making it harder to recognize low blood sugar levels in diabetic patients.
- Food and Alcohol Interactions: While food does not significantly impact the absorption of Celiprolol, alcohol can enhance its blood pressure-lowering effects, leading to an increased risk of hypotension. It is advised to limit alcohol consumption when taking Celiprolol.
- Clinical Recommendations: Monitoring of heart rate and blood pressure is essential when Celiprolol is used in combination with other blood pressure-lowering agents or antiarrhythmics. Patients taking both Celiprolol and diabetes medications should be monitored for hypoglycemia, and those using NSAIDs should have their blood pressure and kidney function monitored regularly.

Celiprolol Hydrochloride Pregnancy Category Note - Key Information

Pregnancy Category B in (1st trimester), D in 2nd & 3rd trimesters.

Celiprolol Hydrochloride Adult Dose - Recommended Dosage

- Standard Dosage:
- For Hypertension: The typical starting dose is 200 mg once daily. Depending on the patient’s response, the dose may be increased up to 400 mg per day.
- For Angina: The usual dose is 200-400 mg daily, divided into two doses.
- Dose Adjustment: For patients with renal or hepatic impairment, a lower starting dose may be necessary, and careful monitoring is required.
- Maximum Dosage: The maximum recommended daily dose is 400 mg, though doses above this should only be prescribed under close supervision due to the risk of side effects.

Celiprolol Hydrochloride Child Dose - Dosage for Children

- Pediatric Use: Celiprolol is not commonly prescribed for children and its safety and efficacy in pediatric populations have not been well established. It is generally not recommended for use in children under 18 years unless advised by a specialist.
- Pediatric Considerations: If prescribed, the dosing would be tailored based on body weight, and close monitoring for side effects, particularly cardiovascular issues, would be essential.

Celiprolol Hydrochloride Renal Dose - Dosage for Kidney Conditions

- Renal Impairment: Celiprolol is contraindicated in patients with severe renal impairment (creatinine clearance <30 mL/min) because it is excreted via the kidneys. In patients with mild to moderate renal impairment, the drug should be used cautiously, with potential dose reduction and frequent monitoring of renal function.
- Monitoring Recommendations: Renal function should be monitored regularly during therapy, and adjustments to the dose may be required based on creatinine clearance.