Thông tin thuốc gốc
Chỉ định và Liều dùng
Emergency treatment of hypertension
Adult: 20 mg injected slowly for at least 2 min, followed by 40-80 mg dose every 10 min, if necessary up to 300 mg. Patient should remain supine during and 3 hr after the procedure.

Hypotensive anaesthesia
Adult: Initially, 10-20 mg, increase at 5-10 mg increments if satisfactory hypotension is not achieved after 5 min. Administer higher initial doses if halothane anaesth is not used.

Hypertension after myocardial infarction
Adult: Initiate infusion at a rate of 15 mg/hr, then increase gradually until a favourable response is obtained or a dose of 120 mg/hr is reached.

Hypertension in pregnancy
Adult: Start infusion at a rate of 20 mg/hr, doubled every 30 min until a satisfactory response is achieved or a dose of 160 mg/hr is reached.

Adult: Initially, 100 mg bid, may increase gradually according to patients response to 200-400 mg bid. Max: 2.4 g/day in 2-4 divided doses.
Elderly: Initially, 50-100 mg bid. Maintenance: 100-200 mg bid.
Cách dùng
Should be taken with food. Take immediately after meals.
Tương kỵ
Na bicarbonate 5% and alkaline solutions.
Chống chỉ định
Obstructive airway disease (e.g. bronchial asthma), 2nd and 3rd degree heart block, cardiogenic shock, conditions w/ severe or prolonged hypotension, uncompensated heart failure, severe bradycardia.
Thận trọng
Patients w/ phaeochromocytoma, inadequate cardiac function and well-compensated heart failure, DM, nonallergic bronchospasm. Patients undergoing major surgery involving general anaesth. May mask symptoms of hypoglycaemia. Avoid abrupt withdrawal as it may exacerbate angina. Hepatic impairment. Elderly, pregnancy and lactation.
Phản ứng phụ
Intraoperative floppy iris syndrome, orthostatic hypotension, bradycardia, syncope, paraesthesia, dizziness, dyspnoea, fatigue, vertigo, headache, nasal stuffiness, diarrhoea, abdominal pain, male sexual dysfunction, dyspepsia, nausea, vomiting, flatulence, constipation, taste disturbances, scalp tingling, tremor, muscle weakness, urinary retention, hepatitis, jaundice, rash, increased transaminases, nightmares, claudication.
Potentially Fatal: Hepatic injury.
IV/Parenteral/PO: C
Monitor LFT periodically and BP.
Quá liều
Symptoms: Hypotension, bradycardia, cardiac failure, bronchospasm. Management: Symptomatic and supportive treatment. Admin activated charcoal after emesis or gastric lavage. Atropine or epinephrine may be given for bradycardia. For severe hypotension, a vasopressor (e.g. dopamine, norepinephrine) may be administered and for heart failure, a cardiac glycoside and diuretic. Glucagon may be beneficial for the management of myocardial depression and hypotension. A β2-adrenergic agonist and/or a theophylline derivative may be used for bronchospasm. Diazepam may be used for seizures.
Tương tác
Synergistic hypotensive effect w/ halothane. Increased absolute bioavailability w/ cimetidine. Decreased absolute bioavailability w/ glutethimide. Additive hypotensive effect w/ nitroglycerin. Increased incidence of tremor w/ TCAs. Increased risk of bradycardia and heart block w/ Ca channel blocker (e.g. verapamil, diltiazem).
Lab Interference
False-positive results in fluorometric or photometric analysis of urinary catecholamines.
Tác dụng
Description: Labetalol competitively inhibits the adrenergic stimulation of β-receptors w/in the myocardium, bronchial and vascular smooth muscle, and α1-receptors w/in vascular smooth muscle. It also has some intrinsic β2-agonist and membrane-stabilising activity.
Onset: 20 min to 2 hr (oral); 2-5 min (IV).
Duration: Dose dependent: 8-12 hr (oral); 2-18 hr (IV).
Absorption: Absorbed readily from the GI tract. Bioavailability increased by food. Time to peak plasma concentration: Approx 1-2 hr (oral); 5-15 min (IV).
Distribution: Crosses the placenta, enters breast milk. Volume of distribution: 3-16 L/kg. Plasma protein binding: Approx 50%.
Metabolism: Extensive first-pass metabolism primarily via glucuronide conjugation.
Excretion: Via urine (55-60% as glucuronide conjugates; <5% as unchanged drug). Elimination half-life: Approx 6-8 hr (oral); approx 5.5 hr (IV).
Bảo quản
Store between 2-30°C.
Phân loại MIMS
Anon. Labetalol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 26/11/2013.

Buckingham R (ed). Labetalol Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 26/11/2013.

Joint Formulary Committee. Labetalol Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. Accessed 26/11/2013.

Labetalol HCl Tab, Film-Coated (Par Pharmaceutical Companies, Inc). DailyMed. Source: U.S. National Library of Medicine. Accessed 26/11/2013.

Labetalol Injection (Sagent Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. Accessed 26/11/2013.

McEvoy GK, Snow EK, Miller J et al (eds). Labetalol Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). Accessed 26/11/2013.

Trandate Tablets and Injection. U.S. FDA. Accessed 26/11/2013.

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