Labetalol

Indications
 Oral
Hypertension
Adult: As hydrochloride: Initially, 100 mg bid; increase gradually according to patient's response to 200-400 mg bid. Max dose: 2.4 g daily in 2-4 divided doses.
Elderly: Initially, 50 mg bid.
Intravenous
Emergency treatment of hypertension
Adult: As hydrochloride: 50 mg injected slowly for at least 1 min; repeat at 5-min intervals as necessary, up to 200 mg. Monitor BP and the patient should remain supine during and 3 hr after the procedure. Alternatively, 2 mg/min infusion at concentrations of 1 mg/ml or 2 mg/3 ml of a suitable diluent.
Intravenous
Hypertension in pregnancy
Adult: As hydrochloride: Start infusion at a rate of 20 mg/hr, then doubled every 30 min until a favourable response is achieved or a dose of 160 mg/hr is reached.
Intravenous
Hypertension after myocardial infarction
Adult: As hydrochloride: Start 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.
Intravenous
Hypotensive anaesthesia
Adult: As hydrochloride: Initially, 10-20 mg; increase at 5-10 mg increments if satisfactory hypotension is not achieved after 5 minutes. Administer higher initial doses if halothane anaesthesia is not used.
Contraindications
 2nd and 3rd degree heart block, cardiogenic shock, obstructive airway disease e.g. bronchial asthma, uncompensated heart failure, severe bradycardia, sick sinus syndrome, Prinzmetal's angina, severe peripheral arterial disease.
Warnings / Precautions
 Phaeochromocytoma, compensated heart failure, nonallergic bronchospasm. Avoid abrupt withdrawal. DM. Hepatic impairment. Perform LFTs. Elderly. Pregnancy and lactation.
Adverse Reactions
 Orthostatic hypotension, dizziness, fatigue, vertigo, paraesthesia, headache, nasal stuffiness, dyspnoea, diarrhoea, abdominal pain, sexual dysfunction, dyspepsia, nausea, vomiting, scalp tingling, rash, increased transaminases, nightmares, worsening of intermittent claudication.
Potentially Fatal: Hepatic injury.
Drug Interactions
 Increased bioavailability with cimetidine. Decreased bioavailability with glutethimide. Increased incidence of tremors with TCAs. Additive hypotensive effect with nitroglycerin.
Potentially Fatal: Increased risk of bradycardia with drugs that slows AV conduction. Synergistic hypotensive effect with halothane.
See Below for More labetalol Drug Interactions
Lab Interactions
 False-positive results in fluorimetric analysis of urinary catecholamines.
Mechanism of Actions
 Labetalol competitively inhibits the adrenergic stimulation of β-receptors within the myocardium, bronchial and vascular smooth muscle, and α1-receptors within vascular smooth muscle. It also has some intrinsic β2-agonist and membrane-stabilising activity.
Absorption: Absorbed readily from the GIT (oral); peak plasma concentrations after 1-2 hr. Bioavailability increased by food.
Distribution: Protein-binding: 50%. Crosses the blood-brain barrier, placenta and enters breast milk.
Metabolism: Extensive first-pass metabolism.
Excretion: Via urine (as metabolites and traces of unchanged drug); also via faeces. Elimination half-life: 8 hr (steady state), 5.5 hr (IV infusion).
Administration
 Should be taken with food. (Take immediately after meals.)
Storage Conditions
 Intravenous: Store at 2-30°C (36-86°F). Oral: Store at 2-30°C (36-86°F).
ATC Classification
 C07AG01 - labetalol ; Belongs to the class of alpha and beta blocking agents. Used in the treatment of cardiovascular diseases.
Storage
 Intravenous: Store at 2-30°C (36-86°F). Oral: Store at 2-30°C (36-86°F).
Available As
  • Labetalol 100 mg
  • Labetalol Hcl 100 mg
  • Labetalol 200 mg
  • Labetalol 5 mg
  • Labetalol 50 mg

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