Labetalol

Labetalol Brands

Brand Name	Manufacturer Name	Distributor	Drug Strength	Packaging	Formulation	Formulation Strength	Price
Lebatens	Bristol-Meyers Squibb	Phillips Pharmaceuticals Ltd.	100mg	30	Tablet	per tablet	KES 750

Labetalol More info

Hypertension: Oral: Initial: 100 mg twice daily, may increase as needed every 2-3 days by 100 mg twice daily (titration increments not to exceed 200 mg twice daily) until desired response is obtained; usual dose: 200-400 mg twice daily; may require up to 2.4 g/day.

I.V. bolus: Per the manufacturer: Initial: 20 mg I.V. push over 2 minutes; may administer 40-80 mg at 10-minute intervals, up to 300 mg total cumulative dose; as appropriate, follow with oral antihypertensive regimen

I.V. infusion (acute loading): Per the manufacturer: Initial: 2 mg/minute; titrate to response up to 300 mg total cumulative dose (eg, discontinue after 2.5 hours of 2 mg/minute); as appropriate, follow with oral antihypertensive regimen

Note: Although loading infusions are well described in the product labeling, the labeling is silent in specific clinical situations, such as in the patient who has an initial response to labetalol infusions but cannot be converted to an oral route for subsequent dosing. There is limited documentation of prolonged continuous infusions (ie, >300 mg/day). In rare clinical situations, higher continuous infusion doses up to 6 mg/minute have been used in the critical care setting (eg, aortic dissection) and up to 8 mg/minute (eg, hypertension with ongoing acute ischemic stroke). At these doses, it may be best to consider an alternative agent if the labetalol infusion is not meeting the goals of therapy. At the other extreme, continuous infusions at relatively low doses (0.03-0.1 mg/minute) have been used in some settings (following loading infusion in patients who are unable to be converted to oral regimens or in some cases as a continuation of outpatient oral regimens). These prolonged infusions should not be confused with loading infusions. Because of wide variation in the use of infusions, an awareness of institutional policies and practices is extremely important. Careful clarification of orders and specific infusion rates/units is required to avoid confusion. Due to the prolonged duration of action, careful monitoring should be extended for the duration of the infusion and for several hours after the infusion. Excessive administration may result in prolonged hypotension and/or bradycardia.

Arterial hypertension in acute ischemic stroke (unlabeled use [Adams, 2007; Jauch, 2010]): I.V.:

Patient otherwise eligible for reperfusion treatment (eg, alteplase): Blood pressure (BP): Systolic >185 mm Hg or diastolic >110 mm Hg: 10-20 mg over 1-2 minutes; may repeat once. If BP does not decline and remains >185/110 mm Hg, alteplase should not be administered.

Management of BP during and after reperfusion treatment (eg, alteplase): BP: Systolic ≥180 mm Hg or diastolic ≥105 mm Hg: 10 mg over 1-2 minutes; may repeat every 10-20 minutes (maximum dose: 300 mg) or 10 mg followed by an infusion of 2-8 mg/minute. If hypertension is refractory, consider other I.V. antihypertensives (eg, nitroprusside)

Note: Due to limited documentation of its use, labetalol should be initiated cautiously in pediatric patients with careful dosage adjustment and blood pressure monitoring.

Oral: Hypertension (unlabeled use): Initial: 1-3 mg/kg/day, in 2 divided doses; maximum: 10-12 mg/kg/day, up to 1200 mg/day

Pediatric hypertensive emergencies: Initial continuous infusions of 0.4-1 mg/kg/hour with a maximum of 3 mg/kg/hour have been used; administration requires the use of an infusion pump.

Oral: Initial dose: Refer to adult dosing. Usual maintenance: 100-200 mg twice daily

Not removed by hemo- or peritoneal dialysis; supplemental dose is not necessary.

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Bolus dose may be administered I.V. push at a rate of 10 mg/minute; may follow with continuous I.V. infusion

Stable in D5LR, D2.51/2NS, D51/4NS, D51/3NS, D5NS, D5W, LR, NS, Ringer's; most stable at pH of 2-4. Incompatible with sodium bicarbonate 5% and alkaline solutions.

Y-site administration: Compatible: Amikacin, aminophylline, amiodarone, ampicillin, butorphanol, calcium gluconate, cefazolin, ceftazidime, ceftizoxime, chloramphenicol, cimetidine, clindamycin, diltiazem, dobutamine, dopamine, enalaprilat, epinephrine, erythromycin lactobionate, esmolol, famotidine, fentanyl, gatifloxacin, gentamicin, hydromorphone, lidocaine, linezolid, lorazepam, magnesium sulfate, meperidine, metronidazole, midazolam, milrinone, morphine, nicardipine, nitroglycerin, norepinephrine, oxacillin, penicillin G potassium, piperacillin, potassium chloride, potassium phosphates, propofol, ranitidine, sodium acetate, sodium nitroprusside, tobramycin, trimethoprim/sulfamethoxazole, vancomycin, vecuronium. Incompatible: Amphotericin B cholesteryl sulfate complex, cefoperazone, ceftriaxone, nafcillin, thiopental, warfarin. Variable (consult detailed reference): Furosemide, heparin, insulin (regular).

Treatment of mild-to-severe hypertension; I.V. for severe hypertension (eg, hypertensive emergencies)

Pediatric hypertension; management of pre-eclampsia; severe hypertension in pregnancy; hypertension during acute ischemic stroke

Cardiovascular: Hypotension (1% to 5%), edema (≤2%), flushing (1%), ventricular arrhythmia (I.V. use; 1%)

<1% (Limited to important or life-threatening): Alopecia (reversible), anaphylactoid reaction, ANA positive, angioedema, bradycardia, bronchospasm, cholestatic jaundice, CHF, diabetes insipidus, heart block, hepatic necrosis, hepatitis, hypersensitivity, Peyronie's disease, psoriaform rash, Raynaud's syndrome, syncope, systemic lupus erythematosus, toxic myopathy, urinary retention, urticaria

Other adverse reactions noted with beta-adrenergic blocking agents include mental depression, catatonia, disorientation, short-term memory loss, emotional lability, clouded sensorium, intensification of pre-existing AV block, laryngospasm, respiratory distress, agranulocytosis, thrombocytopenic purpura, nonthrombocytopenic purpura, mesenteric artery thrombosis, and ischemic colitis.

Hypersensitivity to labetalol or any component of the formulation; severe bradycardia; heart block greater than first degree (except in patients with a functioning artificial pacemaker); cardiogenic shock; bronchial asthma; uncompensated cardiac failure; conditions associated with severe and prolonged hypotension

• Anaphylactic reactions: Use caution with history of severe anaphylaxis to allergens; patients taking beta-blockers may become more sensitive to repeated challenges. Treatment of anaphylaxis (eg, epinephrine) in patients taking beta-blockers may be ineffective or promote undesirable effects.

• Hepatic injury: Severe hepatic injury including some fatalities have also been rarely reported with use; periodically monitor LFTs with prolonged use.

• Hypotension/syncope: Symptomatic hypotension with or without syncope may occur with labetalol; close monitoring of patient is required especially with initial dosing and dosing increases; blood pressure must be lowered at a rate appropriate for the patient's clinical condition. Initiation with a low dose and gradual up-titration may help to decrease the occurrence of hypotension or syncope. Patients should be advised to avoid driving or other hazardous tasks during initiation of therapy due to the risk of syncope. Orthostatic hypotension may occur with I.V. administration; patient should remain supine during and for up to 3 hours after I.V. administration

• Bronchospastic disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring.

• Conduction abnormality: Consider pre-existing conditions such as sick sinus syndrome before initiating

• Diabetes: Use with caution in patients with diabetes mellitus; may potentiate hypoglycemia and/or mask signs and symptoms. May also reduce release of insulin in response to hyperglycemia; dosage of antidiabetic agents may need to be adjusted.

• Heart failure (HF): Use with extreme caution in patients with compensated heart failure and monitor for a worsening of the condition.

• Hepatic impairment: Use with caution in patients with hepatic impairment; bioavailability is increased due to decreased first-pass metabolism.

• Peripheral vascular disease (PVD): May precipitate or aggravate symptoms of arterial insufficiency in patients with PVD and Raynaud’s disease; use with caution and monitor for progression of arterial obstruction.

• Pheochromocytoma (untreated): If possible, obtain diagnostic tests for pheochromocytoma prior to use. Labetalol has been shown to be effective in lowering blood pressure and relieving symptoms in patients with pheochromocytoma. However, some patients have experienced paradoxical hypertensive responses; use with caution in patients with pheochromocytoma. Additional alpha-blockade may be required during use of labetalol.

• Psoriasis: Beta-blocker use has been associated with induction or exacerbation of psoriasis, but cause and effect have not been firmly established.

• Psychiatric disease: Use with caution in patients with a history of psychiatric illness; may cause or exacerbate CNS depression.

• Anesthetic agents: Use with caution in patients receiving anesthetic agents which decrease myocardial function.

• Calcium channel blockers: Use with caution in patients on concurrent verapamil or diltiazem; bradycardia or heart block can occur. Avoid concurrent I.V. use of both agents.

• Elderly: Elimination of labetalol is reduced in elderly patients; lower maintenance doses may be required.

• Abrupt withdrawal: Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia