Labetalol Injection (labetalol hydrochloride)
OTHER BRAND NAMES
Trandate Injection (Discontinued)
Alpha1 blocker/nonselective beta blocker
Control of BP in severe HTN.
Repeated IV Inj:
Initial: 20mg slow IV inj over 2 min; measure supine BP immediately before and at 5 and 10 min after inj to evaluate response
Titrate: May give additional 40mg or 80mg inj at 10-min intervals until desired supine BP is achieved or a total of 300mg has been injected
Slow Continuous Infusion:
Titrate: May adjust infusion rate according to BP response
Effective Dose: 50-200mg
When a satisfactory response is obtained, d/c and start oral labetalol
Initiation of Dosing w/ Labetalol Tab:
Begin when supine diastolic BP has begun to rise
Initial: 200mg, followed by an additional 200mg or 400mg 6-12 hrs later, depending on BP response
Inpatient Titration: 200mg bid (400mg/day), 400mg bid (800mg/day), 800mg bid (1600mg/day), then 1200mg bid (2400mg/day)
If needed, total daily dose may be given in 3 divided doses
While in hospital, may increase dose of tabs at 1-day intervals
Administer in supine position
Ringers inj; lactated Ringers inj;D5 and Ringers inj; 5% lactated Ringers and D5 inj;
D5 inj; 0.9% NaCl inj; D5 and 0.2% NaCl; 2.5% Dextrose and 0.45% NaCl inj; D5 and 0.9% NaCl inj;
D5 and 0.33% NaCl inj
5% Sodium bicarbonate inj
Care should be taken when administering alkaline drugs, including furosemide, in combination w/ labetalol
Inj: 5mg/mL [20mL, 40mL]
Bronchial asthma, overt cardiac failure, >1st-degree heart block, cardiogenic shock, severe bradycardia, other conditions associated with severe and prolonged hypotension, and history of obstructive airway disease.
For IV use in hospitalized patients. Severe hepatocellular injury (rare) reported. Caution with hepatic impairment. Perform appropriate lab testing at the 1st symptom/sign of liver dysfunction. D/C and do not restart if with lab evidence of liver injury or jaundice. May precipitate more severe failure in patients with congestive heart failure (CHF); avoid with overt CHF and caution with history of well-compensated heart failure (HF). May lead to cardiac failure in patients without a history of HF; digitalize and/or treat with a diuretic at the 1st sign/symptom of HF and observe carefully; d/c (gradually, if possible) if cardiac failure continues. Exacerbation of angina and, in some cases, myocardial infarction reported after abrupt discontinuation. If angina markedly worsens or acute coronary insufficiency develops, reinstitute therapy promptly, at least temporarily, and take other appropriate measures for the management of unstable angina. Avoid in patients with nonallergic bronchospastic disease. Caution with pheochromocytoma; paradoxical hypertensive responses reported. May prevent appearance of premonitory signs/symptoms of acute hypoglycemia (eg, tachycardia). Chronically administered therapy should not be routinely withdrawn prior to major surgery. Several deaths have occurred during surgery (including when used in cases to control bleeding). Caution when reducing severely elevated BP; cerebral infarction, optic nerve infarction, angina, and ECG ischemic changes reported with other agents. Avoid rapid/excessive falls in BP; achieve desired BP lowering over as long a period of time as is compatible with patient status. Symptomatic postural hypotension may occur if patients are tilted or allowed to assume upright position within 3 hrs of administration; establish patient's ability to tolerate an upright position before permitting any ambulation. Intraoperative floppy iris syndrome (IFIS) observed during cataract surgery. Avoid in patients with low cardiac indices and elevated systemic vascular resistance. Hypotension or bradycardia reported with administration of up to 3g/day as an infusion for up to 2-3 days. Patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge and may be unresponsive to usual doses of epinephrine. Lab test interactions may occur.
Symptomatic postural hypotension, dizziness, N/V, somnolence/yawning, increased sweating, tingling of scalp/skin, transient BUN/SrCr increase.
Tremors reported with oral labetalol in combination with TCAs. May blunt the bronchodilator effect of β-agonists in patients with bronchospasm; doses greater than the normal antiasthmatic dose may be required. Cimetidine may increase bioavailability of oral labetalol; caution in establishing required dose for BP control in patients with conditions that enhance absorption or alter hepatic metabolism. Synergistic effect with halothane; do not use ≥3% halothane during controlled hypotensive anesthesia. Additional antihypertensive effects with nitroglycerin. Caution with calcium antagonists of the verapamil type. May need to adjust dose of antidiabetic drugs.
PREGNANCY AND LACTATION
Category C, caution in nursing.
MECHANISM OF ACTION
α1-blocker/nonselective β-blocker; produces dose-related falls in BP without reflex tachycardia and significant reduction in HR.
Distribution: Plasma protein binding (50%); found in breast milk; crosses placenta. Metabolism: Conjugation to glucuronide metabolites. Elimination: Urine (55-60%, unchanged or conjugates), feces; T1/2=5.5 hrs.
Assess for hypersensitivity to the drug, bronchospastic disease, heart block, severe bradycardia, cardiogenic shock, overt cardiac failure, diabetes mellitus, pheochromocytoma, ischemic heart disease, hepatic/renal impairment, any other conditions where treatment is contraindicated or cautioned, pregnancy/nursing status, and possible drug interactions. Obtain baseline BP.
Monitor BP. Monitor LFTs periodically. In patients with concomitant illnesses (eg, renal impairment), monitor these conditions. Monitor for signs/symptoms of HF, postural hypotension, exacerbation of ischemic heart disease following abrupt withdrawal, hypersensitivity reactions, IFIS during cataract surgery, and other adverse reactions. Monitor patient when discontinuing therapy.
Instruct to remain supine during and immediately following (for up to 3 hrs) inj; advise on how to proceed gradually to become ambulatory. Instruct to consult physician at any sign/symptom of impending HF or hepatic dysfunction. Instruct on appropriate directions for titration of dosage when started on labetalol tabs following adequate BP control with labetalol inj. Inform that transient scalp tingling may occur when treatment with tabs is initiated. Instruct patients being treated with labetalol tabs not to interrupt or d/c therapy without physician's advice. Advise to limit physical activity when discontinuing therapy.
2-30°C (36-86°F). Protect from light and freezing.
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