Nebivolol


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Hypertension
Adult: Initially, 5 mg once daily. May increase dose at intervals of 2 wk if needed. Max: 40 mg once daily.
Elderly: >65 yr Initially, 2.5 mg once daily increased to 5 mg once daily if required.

Oral
Heart failure
Adult: Initially, 1.25 mg once daily. May double dose every 1-2 wk if tolerated. Max: 10 mg once daily.
Renal Impairment
Hypertension: Initially, 2.5 mg once daily. Maintenance: Increase to 5 mg daily if required.
Cách dùng
May be taken with or without food.
Chống chỉ định
Sick sinus syndrome, 2nd or 3rd degree heart block (w/o pacemaker), decompensated cardiac failure, severe bradycardia, cardiogenic shock, untreated phaeochromocytoma, metabolic acidosis, severe peripheral circulatory disturbances, history of bronchospasm and bronchial asthma. Hepatic impairment.
Thận trọng
Patients w/ inadequate cardiac function, well-compensated heart failure, myasthenia gravis. Patients undergoing major surgery involving general anaesth. May mask signs and symptoms of hypoglycaemia and hyperthyroidism. Abrupt withdrawal may exacerbate angina symptoms and/or precipitate MI and ventricular arrhythmias in patients w/ coronary artery disease. Pregnancy and lactation.
Phản ứng phụ
Headache, paraesthesia, fatigue, asthenia, dizziness, diarrhoea, nausea, constipation, abdominal pain, insomnia, chest pain, bradycardia, dyspnoea, rash, and peripheral oedema, hypercholesterolaemia, hyperuricaemia, increased BUN, decreased HDL levels.
Monitoring Parameters
Monitor ECG, BP and blood glucose in diabetic patients.
Quá liều
Symptoms: Bradycardia, hypotension, cardiac failure, dizziness, fatigue, hypoglycaemia, vomiting, bronchospasm, heart block. Management: Symptomatic and supportive treatment. IV atropine may be given for bradycardia, if it persists, admin IV isoproterenol cautiously. For hypotension, admin IV fluids and vasopressors. IV glucagon may also be useful. A β2-agonist and/or aminophylline for bronchospasm. Admin IV glucose for hypoglycaemia and an IV cardiac glycoside and diuretic may be used for CHF.
Tương tác
Increased plasma concentrations w/ potent CYP2D6 inhibitors (e.g. paroxetine, fluoxetine, propafenone, thioridazine, quinidine). Concomitant use w/ antiarrhythmic drugs (e.g. amiodarone, disopyramide) or nondihydropyridine Ca channel blockers (e.g. diltiazem, verapamil) may cause conduction disturbance. Additive negative effects on AV conduction and heart rate w/ other β-adrenergic blocking agents or digoxin. Concurrent admin w/ catecholamine-depleting agents (e.g. reserpine) may result in additive hypotension or bradycardia. Abrupt withdrawal of clonidine may increase risk of rebound HTN.
Tác dụng
Description: Nebivolol exhibits high selectivity for β1-adrenergic receptors and has vasodilating activity due to a direct action on the endothelium, involving nitric oxide release. It lacks intrinsic sympathomimetic and membrane-stabilising activity.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: 1.5-4 hr.
Distribution: Volume of distribution: 8-12 L/kg. Plasma protein binding: Approx 98% (mainly to albumin).
Metabolism: Undergoes extensive hepatic metabolism via glucuronidation and via alicyclic and aromatic hydroxylation, N-dealkylation by CYP2D6 isoenzyme.
Excretion: Via urine and faeces (as metabolites). Elimination half-life: Approx 10 hr (nebivolol); approx 24 hr (hydroxy metabolites).
Bảo quản
Store between 20-25°C. Protect from light.
Phân loại MIMS
References
Anon. Nebivolol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com.

Buckingham R (ed). Nebivolol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com.

Bystolic Tablet (Cardinal Health). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/.

Bystolic Tablet (Cardinal Health). U.S. FDA. https://www.fda.gov/.

McEvoy GK, Snow EK, Miller J et al (eds). Nebivolol. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com.

Wickersham RM. Nebivolol HCl. Facts and Comparisons [online]. St. Louis, MO. Wolters Kluwer Clinical Drug Information, Inc. https://www.wolterskluwercdi.com/facts-comparisons-online/.

Thông báo miễn trừ trách nhiệm: Thông tin này được MIMS biên soạn một cách độc lập dựa trên thông tin của Nebivolol từ nhiều nguồn tài liệu tham khảo và được cung cấp chỉ cho mục đích tham khảo. Việc sử dụng điều trị và thông tin kê toa có thể khác nhau giữa các quốc gia. Vui lòng tham khảo thông tin sản phẩm trong MIMS để biết thông tin kê toa cụ thể đã qua phê duyệt ở quốc gia đó. Mặc dù đã rất nỗ lực để đảm bảo nội dung được chính xác nhưng MIMS sẽ không chịu trách nhiệm hoặc nghĩa vụ pháp lý cho bất kỳ yêu cầu bồi thường hay thiệt hại nào phát sinh do việc sử dụng hoặc sử dụng sai các thông tin ở đây, về nội dung thông tin hoặc về sự thiếu sót thông tin, hoặc về thông tin khác. © 2021 MIMS. Bản quyền thuộc về MIMS. Phát triển bởi MIMS.com
  • Mibelet
  • Nebibio
  • Nebicard
  • Nevol 5
  • Nodon
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in