Celiprol (Tablets) Instructions for Use

ATC Code

C07AB08 (Celiprolol)

Active Substance

Celiprolol (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Beta₁-adrenoblocker

Pharmacotherapeutic Group

Selective beta1-adrenergic blocker with ISA

Pharmacological Action

A selective beta1-adrenergic blocker with intrinsic sympathomimetic activity. It does not possess membrane-stabilizing activity. It exerts antihypertensive and antianginal effects.

Pharmacokinetics

The absorption of celiprolol is dose-dependent and increases with higher doses. The bioavailability after oral administration of a 100 mg dose is 30%, and of a 400 mg dose is 70%. Concurrent food intake reduces the bioavailability level of celiprolol (with long-term use, the same bioavailability level is observed both when taken 1 hour before meals and 2 hours after).

C_max in blood plasma is reached after 2-3 hours. With continuous use, C_ss is achieved after 2-3 days. It is minimally metabolized (1-2%) in the liver (this distinguishes it from lipophilic substances, which are significantly metabolized during the first pass through the liver), and the active metabolites formed in this process possess cardioselective action.

It is excreted by the kidneys and with bile in approximately equal amounts.

Indications

Arterial hypertension, treatment of coronary artery disease, prevention of angina attacks.

ICD codes

Dosage Regimen

Administer orally as tablets. The dosage regimen must be individualized based on the clinical indication and patient response.

For arterial hypertension and angina pectoris, initiate therapy with 200 mg taken once daily. If the clinical response is inadequate after 2-3 weeks, increase the dose to 400 mg once daily.

The maximum recommended daily dose is 600 mg. This higher dose should be reserved for patients with severe hypertension not controlled by 400 mg and should be administered as a single daily dose.

Take the tablet with a glass of water. For consistent bioavailability, administer at least 1 hour before or 2 hours after a meal.

In patients with renal impairment, adjust the dose. Initiate treatment with a reduced dose of 100 mg once daily. Monitor renal function and clinical response before considering any dose escalation.

Do not abruptly discontinue therapy, particularly in patients with coronary artery disease. To prevent rebound hypertension or exacerbation of angina, gradually reduce the dose over 1-2 weeks under medical supervision.

Adverse Reactions

From the nervous system: fatigue, headache, dizziness, sleep disorders, tremor may occur; in isolated cases with high doses – depression.

Dermatological reactions: skin itching, exacerbation of psoriasis, appearance of psoriasiform exanthemas.

From the digestive system: nausea, diarrhea, constipation.

From the organ of vision: decreased tear fluid production.

From the endocrine system: rarely – worsening of the condition in patients with diabetes mellitus, hypoglycemia in patients with labile blood glucose levels, decreased potency.

From the cardiovascular system: cold extremities; in isolated cases with high doses – AV block, arterial hypotension, heart failure.

From the respiratory system: bronchospasm is possible in patients with severe respiratory diseases.

Other: muscle weakness, chills.

Contraindications

Hypersensitivity to celiprolol; AV block II and III degree, sinoatrial block, sick sinus syndrome, severe bradycardia, acute heart failure, cardiogenic shock, severe arterial hypotension, chronic heart failure in the stage of decompensation, severe ischemic diseases of the peripheral vessels of the lower extremities (accompanied by pain at rest and trophic disorders), untreated pheochromocytoma, metabolic acidosis, bronchial asthma.

Use in Pregnancy and Lactation

Use during pregnancy and lactation (breastfeeding) is possible only for strict indications, when the intended therapeutic benefit for the mother outweighs the potential risk to the fetus or child.

Use in Renal Impairment

In patients with impaired renal function, it is necessary to reduce the dose to 100 mg once daily.

Special Precautions

Use with caution in hyperthyroidism, myasthenia, depression.

In pheochromocytoma, use is possible only against the background of therapy with alpha-adrenergic blockers.

Discontinuation of treatment should be gradual, reducing the dose over 1-2 weeks, especially in patients with coronary artery disease.

Use with caution in patients using contact lenses, as Celiprolol may reduce tear fluid production.

During the use of celiprolol, a positive result in a doping test is possible.

Effect on the ability to drive vehicles and operate machinery

During the use of celiprolol, the ability to perform work requiring concentration and high speed of psychomotor reactions may be impaired.

Drug Interactions

With simultaneous use of celiprolol with calcium channel blockers, an enhancement of the antihypertensive effect is possible (control of blood pressure and other hemodynamic parameters is required).

With simultaneous use with nifedipine, the development of a negative inotropic effect with manifestations of heart failure and pronounced arterial hypotension is possible; with verapamil – arrhythmia, arterial hypotension, bradycardia are possible. Intravenous administration of verapamil during the use of celiprolol is contraindicated.

If surgical intervention is necessary during the use of celiprolol, the possibility of a negative inotropic effect when using anesthetic agents should be considered.

With simultaneous use with methyldopa, reserpine, guanfacine, a significant decrease in heart rate is possible.

The interval between taking MAO inhibitors and celiprolol should be at least 14 days; simultaneous use is not recommended due to the risk of a significant increase in the hypotensive effect.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.