Hypercor 2.5

Bisoprolol fumarate.

Each film-coated tablet contains Bisoprolol fumarate 2.5 mg.

Pharmacology: Pharmacodynamics: Bisoprolol is a β₁-selective adrenergic blocking agent which does not exhibit the intrinsic sympathomimetic activity or the membrane stabilizing activity. According to in vitro studies at low dosages, Bisoprolol selectively inhibits response to adrenergic stimuli by competitively blocking cardiac β₁-adrenergic receptors, while having little effect on the β₂-adrenergic receptors of bronchial and vascular smooth muscle but at high doses (e.g., 20 mg or higher), the selectivity of Bisoprolol on β₁-adrenergic receptors usually diminishes, and the drug will competitively inhibit both β₁ and β₂-adrenergic receptors.
Pharmacokinetics: Absorption: Bisoprolol is almost completely absorbed from the gastrointestinal tract and undergoes only minimal first-pass metabolism resulting in an oral bioavailability of about 90%. Peak plasma concentrations occur 2 to 4 hours after oral doses.
Distribution: Bisoprolol is about 30% bound to plasma proteins.
Metabolism: Bisoprolol is moderately lipid soluble. It is metabolised in the liver.
Excretion: Bisoprolol has a plasma elimination half-life of 10 to 12 hours and is excreted in urine, about 50% as unchanged drug and 50% as metabolites.

Use alone or in combination with other classes of antihypertensive agents in the management of hypertension.

Recommended Dose: Hypertension: The usual initial dosage of bisoprolol fumarate is 2.5-5 mg once daily. In patients whose blood pressure is not controlled adequately with the initial bisoprolol fumarate dosage, dosage can be increased gradually as tolerated, generally at intervals of at least 2 weeks, up to a maximum of 20 mg once daily.
Dosage in Hepatic and Renal Impairment: The initial dose of bisoprolol fumarate for hypertension should be 2.5 mg once daily and the dose should be increased cautiously in patients with severe hepatic impairment or renal impairment (creatinine clearance less than 40 mL/minute).
In patients with severe renal impairment (creatinine clearance < 20 mL/min) and in patients with severe hepatic impairment a daily dose of 10 mg bisoprolol fumarate must not be exceeded.
Discontinuation of treatment: Do not stop treatment abruptly or change the recommended dose without talking to the doctor first since this might lead to a transitory worsening of heart condition. Especially in patients with ischaemic heart disease, treatment must not be discontinued suddenly. If discontinuation is necessary, the daily dose is gradually decreased.
Mode of Administration: Bisoprolol fumarate is administered orally. GI absorption of the drug does not appear to be affected by food.

Overdose and Treatment: Many cases of β-blocker overdosage are uneventful, but some patients develop severe and occasionally fatal cardiovascular depression. Effects can include bradycardia, cardiac conduction block, hypotension, heart failure, and cardiogenic shock or convulsions, coma, respiratory depression, and bronchoconstriction can also occur, although infrequently. In overdosage, use of activated charcoal or gastric lavage should be considered if the patient presents within 1 hour of ingestion. Mild hypotension may respond to intravenous fluids. If hypotension continues, glucagon should be given or sympathomimetics may be used as an alternative or given with glucagon via intravenous route.

Do not use Bisoprolol in patients with these following symptoms: 1. Uncontrolled heart failure or acutely decompensated heart failure requiring IV inotropic therapy.
2. Cardiogenic shock.
3. Second or third-degree AV block.
4. Sinus bradycardia.
5. Severe peripheral arterial disease.
6. Hypotension.
7. Patients with bronchospasm or asthma or those with a history of obstructive airways disease.
8. Patients with phaeochromocytoma without α blockers therapy given as well.
9. Metabolic acidosis.

Use cautiously in patients with diabetes because it can mask prominent hypoglycemic symptoms.
Use with caution in patients with first-degree AV block.
β-blockers without α₁-adrenergic receptor blocking activity should be avoided in patients with Prinzmetal's angina.
Bisoprolol can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease and Raynaud disease. Use with caution and monitor for progression of arterial obstruction.
Patients with psoriasis or those with a history of psoriasis should be cautious with the use of Bisoprolol since it may induce or exacerbate psoriasis.
Use with caution in patients with history of severe anaphylaxis because such patients may become more sensitive to repeated challenges. Treatment of anaphylaxis in patients taking Bisoprolol may be ineffective or promote undesirable effects.
Use with caution in patients with hyperthyroidism because it may mask signs of hyperthyroidism (e.g., tachycardia). Abrupt withdrawal may precipitate thyroid storm.

Exposure to β-blockers during pregnancy may increase the risk for adverse events in the neonate. If maternal use of Bisoprolol is needed, fetal growth should be monitored during pregnancy and the newborn should be monitored for 48 hours after delivery for bradycardia, hypoglycemia, and respiratory depression. Chronic maternal hypertension is also associated with adverse events in the fetus/infant. Untreated chronic hypertension may also increase the risks of adverse maternal outcomes. When treatment of chronic hypertension in pregnancy is indicated, agents other than Bisoprolol are preferred. It is not known if Bisoprolol is present in breast milk thus Bisoprolol should be used with caution in a lactating female or use of β-blockers other than Bisoprolol may be preferred.

Cardiovascular: Cardiac arrhythmia, cardiac failure, chest pain, claudication, cold extremities, edema, flushing, hypersensitivity angiitis, hypotension, orthostatic hypotension, palpitations.
Central nervous system: Anxiety, depression, dizziness, drowsiness, fatigue, headache, hyperesthesia, hypoesthesia, insomnia, lack of concentration, malaise, memory impairment, paresthesia, restlessness, sensation of eye pressure, twitching, vertigo, vivid dream.
Dermatologic: Acne vulgaris, alopecia, diaphoresis, eczema, pruritus, skin irritation, skin rash.
Endocrine & metabolic: Decreased libido, gout, increased serum glucose, increased serum phosphate, increased serum potassium, increased serum triglycerides, increased uric acid, weight gain.
Gastrointestinal: Abdominal pain, constipation, diarrhea, dysgeusia, dyspepsia, epigastric pain, gastric pain, gastritis, nausea, peptic ulcer, vomiting, xerostomia.
Genitourinary: Cystitis, impotence.
Hematologic & oncologic: Decreased white blood cell count, positive ANA titers, purpuric rash, thrombocytopenia.
Hepatic: Increased serum alanine aminotransferase, increased serum aspartate aminotransferase.
Neuromuscular & skeletal: Back pain, muscle cramps, myalgia, neck pain, tremor.
Ophthalmic: Abnormal lacrimation, eye pain, visual disturbance.
Otic: Otalgia, tinnitus.
Renal: Increased blood urea nitrogen, increased serum creatinine, polyuria, renal colic.
Respiratory: Asthma, bronchitis, bronchospasm, cough, dyspnea, dyspnea on exertion, pharyngitis, rhinitis, sinusitis, upper respiratory tract infection.
Rare but important or life-threatening: Angioedema, arthralgia, asthenia, auditory impairment, bradycardia, dermatitis, exfoliative dermatitis, Peyronie disease, psoriasis, sleep disturbance, syncope, unsteadiness.

Avoid concomitant use with Bisoprolol: Bromperidol, Fexinidazole, Floctafenine, Rivastigmine.
Increased Effect/Toxicity: Bisoprolol may increase the levels/effects of α₁ Blockers, α₂ Agonists, Amifostine, Antipsychotic Agents (Phenothiazines), Antipsychotic Agents (Second Generation [Atypical]), Bradycardia-Causing Agents, Bromperidol, Bupivacaine, Cardiac Glycosides, Ceritinib, Cholinergic Agonists, Disopyramide, Duloxetine, Ergot Derivatives, Fexinidazole, Fingolimod, Grass Pollen Allergen Extract (5 Grass Extract), Hypotension-Associated Agents, Insulins, Ivabradine, Lacosamide, Levodopa-Containing Products, Lidocaine (Systemic/Topical), Mepivacaine, Methacholine, Nitroprusside, Pholcodine, Siponimod, Sulfonylureas.
The levels/effects of Bisoprolol may be increased by Acetylcholinesterase Inhibitors, Alfuzosin, α₂ Agonists, Aminoquinolines (Antimalarial), Amiodarone, Antipsychotic Agents (Phenothiazines), Barbiturates, Benperidol, Brigatinib, Brimonidine (Topical), Calcium Channel Blockers (Nondihydropyridine), Diazoxide, Dipyridamole, Disopyramide, Dronedarone, Floctafenine, Herbs (Hypotensive Properties), Lormetazepam, Methoxyflurane, Midodrine, Molsidomine, Naftopidil, Nicergoline, Nicorandil, Nifedipine, Obinutuzumab, Opioids (Anilidopiperidine), Pentoxifylline, Phosphodiesterase 5 Inhibitors, Propafenone, Prostacyclin Analogues, Quinagolide, Regorafenib, Reserpine, Rivastigmine, Ruxolitinib, Terlipressin, Tofacitinib.
Decreased Effect: Bisoprolol may decrease the levels/effect of β₂ Agonists, Epinephrine (Nasal/Oral/Inhalation/Racemic/Systemic), Theophylline Derivatives.
The levels/effects of Bisoprolol may be decreased by Amphetamines, Barbiturates, Bosentan, Brigatinib, Bromperidol, CYP3A4 Inducers (Moderate/Strong), Dabrafenib, Deferasirox, Dexmethylphenidate, Enzalutamide, Erdafitinib, Herbs (Hypertensive Properties), Ivosidenib, Lorlatinib, Methylphenidate, Mitotane, NSAIDs, Rifamycin Derivatives, Sarilumab, Siltuximab, Tocilizumab, Yohimbine.

Store below 30°C and protect from light.

Beta-Blockers

C07AB07 - bisoprolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.

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