Atenolol


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Emergency treatment of cardiac arrhythmias
Adult: 2.5 mg injected at a rate of 1 mg/minute, may repeat every 5 minutes if needed. Max: 10 mg. Alternatively, 0.15 mg/kg to be infused over 20 minutes. May repeat injection or infusion procedure every 12 hours as needed. Once control is achieved, maintain with oral doses of 50-100 mg daily.

Intravenous
Acute myocardial infarction
Adult: Within 12 hours of the onset of chest pain: Inject 5-10 mg slowly at a rate of 1 mg/minute, followed by an oral dose of 50 mg about 15 minutes later (if no adverse effects result from the injection). Alternatively, repeat IV dose of 5 mg 10 minutes after the initial dose followed by an oral dose of 50 mg 10 minutes after the last dose. A further oral dose of 50 mg may be given 12 hours after. Thereafter, maintain with 100 mg every 12 hours.

Oral
Hypertension
Adult: 50-100 mg once daily, titrate dose based on patient response.

Oral
Angina pectoris
Adult: 50-100 mg daily given as a single dose or in divided doses.
Renal Impairment
Intravenous:
CrCl (mL/min) Dosage
<15 10 mg once every 4 days
15-35 10 mg once every 2 days

Oral:
Patients on haemodialysis: 50 mg after each dialysis.
CrCl (mL/min) Dosage
<15 25 mg or 50 mg on alternate days
15-35  50 mg daily
Cách dùng
May be taken with or without food.
Chống chỉ định
Patients with bradycardia, cardiogenic shock, hypotension, metabolic acidosis, 2nd or 3rd degree heart block, severe peripheral arterial disease, sick sinus syndrome (without pacemaker), uncompensated cardiac failure, and untreated phaeochromocytoma.
Thận trọng
Patients with bronchospasm or reversible obstructive airways disease, diabetes mellitus, peripheral vascular disease, Raynaud’s disease, Prinzmetal’s angina, myasthenia gravis, psoriasis and thyroid diseases. Avoid abrupt withdrawal. Renal impairment. Elderly. Pregnancy and lactation.
Phản ứng phụ
Blood and lymphatic system disorders: Thrombocytopenia.
Cardiac disorders: Bradycardia.
Eye disorders: Dry eyes, visual disturbances.
Gastrointestinal disorders: Nausea, diarrhoea, dry mouth.
General disorders and administration site conditions: Fatigue.
Musculoskeletal and connective tissue disorders: Lupus-like syndrome.
Nervous system disorders: Dizziness, headache.
Psychiatric disorders: Hallucinations, depression, nightmare, psychoses.
Reproductive system and breast disorders: Impotence.
Skin and subcutaneous tissue disorders: Psoriasiform skin reactions, purpura, alopecia.
Vascular disorders: Postural hypotension, cold extremities, Raynaud’s phenomenon.
MonitoringParameters
Monitor blood pressure, heart rate, ECG, and serum glucose (in patients with diabetes mellitus).
Quá liều
Symptoms: Bradycardia, hypotension, bronchospasm, and acute cardiac failure; hypoglycaemia, impaired conduction, decreased cardiac contractility, heart block, shock, and cardiac arrest may also occur. Management: Initiate symptomatic and supportive treatment. Gastric lavage or activated charcoal may be used in acute atenolol overdose. IV atropine sulfate may be given for bradycardia and IV isoproterenol HCl for 2nd or 3rd degree AV block, a transvenous cardiac pacemaker may also be used. For severe hypotension, a vasopressor (e.g. dobutamine, norepinephrine) may be given. and for bronchospasm, a ß2-adrenergic agonist (e.g. isoproterenol, terbutaline). IV glucagon may also be useful if hypotension is refractory to vasopressors and IV glucose is used for hypoglycaemia. A cardiac glycoside, diuretic and oxygen should be used for cardiac failure. In severe cases, haemodialysis may be useful in enhancing elimination.
Tương tác
Additive effects with Ca channel blockers (e.g. verapamil, diltiazem) and catecholamine-depleting agents (e.g. reserpine). May increase atrioventricular conduction time with digitalis glycosides. May aggravate rebound hypertension following clonidine withdrawal. Class I anti-arrhythmic drugs (e.g. disopyramide) and amiodarone may potentiate effects on atrial-conduction time and induce negative inotropic effect. May increases hypoglycaemic effects of insulin and oral antidiabetic drugs. Decreased hypotensive effects with concomitant use of NSAIDs (e.g. ibuprofen, indometacin). May increases risk of hypotension and attenuates reflex tachycardia with anaesthetic drugs.
Lab Interference
May result to false-positive aldosterone/renin ratio (ARR).
Tác dụng
Description: Atenolol selectively and competitively blocks β1-adrenergic receptors but has little or no effect on β2-receptors except at high doses. It has negative inotropic effects without intrinsic sympathomimetic and membrane-stabilising activities.
Duration: Beta-blocking effect: Approx 12-24 hours. Antihypertensive effect: Approx 24 hours (oral).
Pharmacokinetics:
Absorption: Rapid and consistent but incompletely absorbed from the gastrointestinal tract (approx 50%). Time to peak plasma concentration: 2-4 hours (oral).
Distribution: Poorly penetrates tissues due to low lipid solubility, crosses placenta and present in breast milk. Plasma protein-binding: 6-16%.
Metabolism: Limited or no hepatic metabolism.
Excretion: Via urine (40% as unchanged drug); faeces (50%). Elimination half-life: Approx 6-7 hours.
Đặc tính

Chemical Structure Image
Atenolol

Source: National Center for Biotechnology Information. PubChem Database. Atenolol, CID=2249, https://pubchem.ncbi.nlm.nih.gov/compound/Atenolol (accessed on Jan. 21, 2020)

Bảo quản
Store below 25°C.
Phân loại MIMS
Phân loại ATC
C07AB03 - atenolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
References
Anon. Atenolol. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 12/02/2019.

Anon. Atenolol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 12/02/2019.

Atenolol Tablet (Zydus Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 12/02/2019.

Buckingham R (ed). Atenolol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/02/2019.

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