📌 COMPOSITION

Each F/C tablet contains: Bisoprolol fumarate 2.5 mg, 5 mg or 10 mg.

📌 DESCRIPTION

Conolol (Bisoprolol) is a cardio‑selective beta‑1 adrenergic blocking agent used to treat high blood pressure. It is considered a potent drug with a long half‑life that can be used once daily to reduce the need for multiple doses of antihypertensive drugs. Conolol decreases heart rate, decreases contractility and need for oxygen, and hence dilates blood vessels, leading to reduced blood pressure. Conolol also reduces the output of renin in the kidneys, which normally increases blood pressure. Due to its receptor selectivity (low affinity to beta‑2 receptors of the smooth muscles of the bronchi), it can be useful in patients with chronic obstructive pulmonary disease (COPD).

📌 INDICATIONS

• Treatment of hypertension.
• Treatment of stable chronic angina.
• Treatment of stable chronic heart failure in addition to other drugs such as ACE inhibitors, diuretics and cardiac glycosides.

📌 DOSAGE & ADMINISTRATION

The tablet should be taken in the morning before, after or with breakfast.

Treatment of hypertension and stable chronic angina:

• The usual starting dose is 5 mg once daily. If necessary and after being closely monitored, the dose may be increased to 10 mg once daily. The maximum daily recommended dose is 20 mg.
• Patients with severe renal impairment (Cr.Cl < 20 ml/min) or severe liver impairment: the dose should not exceed 10 mg once daily.
• In elderly patients, it is recommended to start with the lowest possible dose.

Treatment of stable chronic heart failure:

The treatment should not be initiated unless the patient has not had any heart failure during the past 6 weeks and the basic therapy has not changed for the past 2 weeks.

• The dose starts with 1.25 mg once daily (in the morning) for 1 week, then, if well tolerated, increased to 2.5 mg once daily for 1 week, then 3.75 mg once daily for 1 week, then 5 mg once daily for 4 weeks, then 7.5 mg once daily for 4 weeks, then 10 mg once daily.
• The maximum recommended dose is 10 mg once daily.
• After initiation of treatment with 1.25 mg, the vital signs of the patient should be observed over a period of 4 hours.
• Patients with severe renal and hepatic impairment: the up‑titration should be made with additional caution.
• If deterioration of heart failure intolerance occurs during titration, gradual reduction of the dose is recommended, or in the presence of compelling reasons for immediate discontinuation, the treatment should be stopped gradually.

📌 RESTRICTIONS ON USE

Contraindications

• Must not be used in patients with acute heart failure or during deterioration of heart failure requiring IV therapy.
• It is contraindicated in patients with cardiogenic shock, sinoatrial block, symptomatic bradycardia, symptomatic hypotension, second or third degree AV block, and sick sinus syndrome (bradycardia and tachycardia).
• Must not be used in severe bronchial asthma, severe chronic obstructive pulmonary disease, severe forms of peripheral arterial occlusive disease or Raynaud's syndrome (a syndrome affecting the blood vessels).
• Must be avoided in patients with untreated phaeochromocytoma and metabolic acidosis.
• It is contraindicated when there is hypersensitivity to bisoprolol.

Precautions

• Must be used with caution by patients with diabetes mellitus or those undergoing strict fasting, because it masks the signs and symptoms of hypoglycaemia; it also masks the signs of thyrotoxicosis.
• Must be used with caution in patients with first‑degree AV block, Prinzmetal's angina, peripheral arterial occlusive disease, and psoriasis.
• In bronchial asthma or other chronic obstructive pulmonary disease, concomitant bronchodilator therapy is recommended.
• Conolol may increase sensitivity to allergens and the severity of anaphylactic reactions.
• Conolol's withdrawal should be done gradually before surgery and completed about 48 hours prior to anaesthesia.
• Conolol must not be used until after alpha‑receptor blockade in patients with phaeochromocytoma.
• Abrupt withdrawal of clonidine, especially if Conolol was discontinued prior to the withdrawal, leads to an increased risk of rebound hypertension.
• Patients should avoid contact lenses because Conolol leads to a reduction of lacrimal fluid secretion.
• Conolol should not be stopped abruptly. The dosage should be diminished gradually.

Use in Pregnancy and Lactation

Conolol is not recommended during pregnancy unless its benefits outweigh the risks, and is contraindicated during lactation.

Effects on the ability to drive vehicles or use machines

The ability to drive vehicles and operate machines may vary from person to person, so this must be taken into consideration, especially at the start of treatment and when changing therapy.

📌 DRUG INTERACTIONS

Concomitant use of Conolol with the following drugs is not recommended:

• Centrally acting antihypertensive drugs (such as methyldopa and clonidine) may reduce heart rate and cardiac output and may lead to vasodilation.
• Calcium antagonists (such as verapamil and diltiazem) and class I anti‑arrhythmic agents may reduce the contractility of heart muscle and delay AV impulse conduction.

Concomitant use of Conolol with the following drugs should be taken with caution:

• Calcium antagonists (such as amlodipine) may increase the risk of hypotension.
• Class III antiarrhythmic drugs such as amiodarone, and parasympathomimetic medicines, because they may increase the inhibitory effect on AV impulse conduction.
• Topical beta blockers such as eye drops for glaucoma treatment.
• Insulin or oral antihyperglycaemics lead to potentiating their effect.
• Anaesthetic agents may lead to hypotension.
• Cardiac glycosides (digitalis) lead to a reduction in heart rate.
• NSAIDs may reduce the effect of bisoprolol.
• Beta sympathomimetics such as isoprenaline and dobutamine lead to a reduction of the effect of both drugs.
• Sympathomimetics that activate both beta and alpha receptors (adrenaline and noradrenaline) lead to an increase in blood pressure.
• Antihypertensive drugs and other drugs (such as tricyclic antidepressants, barbiturates, phenothiazines) and MAOIs (except MAO-B inhibitors) may increase the risk of hypotension.
• Mefloquine increases the risk of bradycardia.

📌 ADVERSE EFFECTS

Conolol is mostly well tolerated.

Common and very common adverse effects: Dizziness, headache and fatigue (temporary side effects that appear for the first to the second week after the start of treatment and apply to hypertensive and angina pectoris patients), bradycardia in patients with chronic heart failure, worsening of pre‑existing heart failure, feeling of coldness and numbness of extremities, arthralgia, insomnia, nausea, vomiting, diarrhoea, cough, pharyngitis, rhinitis, sinusitis, peripheral oedema.

Uncommon adverse effects: Asthenia, orthostatic hypotension, bronchospasms in patients with bronchial asthma or a history of obstructive airway disease, AV‑conduction disturbances, sleep disorders, muscle cramps and weakness.

Rare adverse effects: Hypersensitivity reactions such as itching, flush, rash, potency disorders, and very rarely alopecia, conjunctivitis.

📌 OVERDOSAGE

The most frequent signs are bradycardia, markedly dropped blood pressure, bronchospasm, acute heart failure, AV block and hypoglycaemia. Patients should be taken to the nearest health centre so they can be monitored closely and treated by the physician.

Treatment of overdose: Supportive and symptomatic treatment, such as giving the patient intravenous atropine or isoprenaline cautiously in case of bradycardia; and IV diuretics, inotropic agents and vasodilating agents in case of acute worsening of heart failure. If there is bronchospasm, the patient should be given bronchodilator therapy. If hypotension is manifested, the patient should be given IV fluids and vasopressors.

📌 STORAGE INSTRUCTIONS

Store below 30°C in a dry place.

📌 PHARMACEUTICAL FORMS

• Conolol 2.5 mg tablets: pack of different sizes.
• Conolol 5 mg tablets: pack of different sizes.
• Conolol 10 mg tablets: pack of different sizes.