Class: beta-Adrenergic Blocking Agents
VA Class: CV100
Chemical Name: 2-Hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]benzamide monohydrochloride
Molecular Formula: C19H24N2O3•HCl
CAS Number: 32780-64-6
Selective α1- and nonselective β-adrenergic blocking agent.1 2 3 4 5 6 7 8 9 19 21 22 23 32
Uses for Labetalol Hydrochloride
Management of hypertension, alone or in combination with other classes of antihypertensive agents.2 4 253 500
β-Blockers generally not preferred for initial management of hypertension, but may be considered in patients who have a compelling indication (e.g., prior MI, ischemic heart disease, heart failure) for their use or as add-on therapy in those who do not respond adequately to the preferred drug classes (ACE inhibitors, angiotensin II receptor antagonists, calcium-channel blockers, or thiazide diuretics).337 501 502 503 504 515 523 524 527 700
Black hypertensive patients generally tend to respond better to monotherapy with calcium-channel blockers or thiazide diuretics than to β-blockers.327 334 335 500 501 504 However, diminished response to β-blockers is largely eliminated when administered concomitantly with a thiazide diuretic.500
Recommended by ACOG and other experts as an appropriate drug of choice in pregnant women who require antihypertensive therapy.298 502 540
Severe Hypertension and Hypertensive Crisis
Used parenterally for immediate BP reduction in severe hypertension or hypertensive emergency;1 3 7 8 14 15 16 51 52 53 73 79 93 94 152 197 198 209 210 235 236 240 500 502 542 generally suitable for most hypertensive emergencies except when acute cardiac failure is present.239 500
One of several recommended parenteral agents for use in the hospital setting to urgently lower BP in severely hypertensive pregnant women, including those with preeclampsia†.298 338 500 540
Has been used alone in patients with pheochromocytoma to control hypertension and symptoms resulting from excessive β-receptor stimulation.51 85 181 182 183 184 However, some clinicians caution against use unless pretreatment with α-adrenergic blocking agents (e.g., IV phentolamine) has occurred.7 May be more effective when tumors predominantly secrete epinephrine rather than norepinephrine, and with sustained rather than paroxysmal hypertension.85 (See Pheochromocytoma under Cautions.)
Controlled Hypotension during Anesthesia
Treatment to produce controlled hypotension during anesthesia† to reduce bleeding resulting from surgical procedures.7 183 190 191 192 193 194 195
Chronic Stable Angina
Management of chronic stable angina pectoris†.7 17 18 127
β-Blockers are recommended as first-line anti-ischemic drugs in most patients with chronic stable angina; despite differences in cardioselectivity, intrinsic sympathomimetic activity, and other clinical factors, all β-blockers appear to be equally effective for this use.1101
Management of sympathetic overactivity syndrome associated with severe tetanus†.196 200 201 202
Labetalol Hydrochloride Dosage and Administration
If long-term therapy is discontinued, gradually reduce dosage over a period of 1–2 weeks.2 4 293 (See Abrupt Withdrawal of Therapy under Cautions.)
BP Monitoring and Treatment Goals
Carefully monitor BP during initial titration or subsequent upward adjustment in dosage.500 501 With continued oral dosing, BP can be measured approximately 12 hours after a dose to determine if further dosage titration is necessary.2 4 (See Absorption under Pharmacokinetics.)
Adjust oral dosage according to standing BP.2 4 293 Adjust gradually (e.g., every 2–4 weeks)203 over a period of 4–12 weeks9 75 76 203 to minimize or avoid adverse effects (e.g., nausea, dizziness) and improve patient tolerance.203
When available, use evidence-based dosing information (i.e., dosages shown in randomized controlled trials to reduce complications of hypertension) to determine target dosages; target dosages usually can be achieved within 2–4 weeks but may take up to several months.501
Goal is to achieve and maintain optimal control of BP; individualize specific target BP based on consideration of multiple factors, including patient age and comorbidities, and currently available evidence from clinical studies.500 501
Severe Hypertension and Hypertensive Crisis
Adjust dosage according to the severity of hypertension and the patient’s supine BP response and tolerance.1 3 500
Initial goal of IV therapy is to reduce mean arterial BP by no more than 25% within minutes to 1 hour, followed by further reduction if stable toward 160/100 to 110 mm Hg within the next 2–6 hours, avoiding excessive declines in pressure that could precipitate renal, cerebral, or coronary insufficiency.500 If this BP is well tolerated and the patient is clinically stable, further gradual reductions toward normal can be implemented in the next 24–48 hours.500
Patients with aortic dissection should have systolic pressure reduced to <100 mm Hg if tolerated.500
Administer orally,2 4 7 8 19 23 47 49 by direct IV injection, or by continuous IV infusion.1 3 7 19 23 51 52 53 73 79 93 94 210
Usually administered in 2 divided doses daily.2 4 If adverse effects (e.g., nausea, dizziness) occur and are intolerable (particularly with dosages ≥1.2 g daily), administration in 3 divided doses daily may improve patient tolerance and/or facilitate dosage titration.2 4
For solution and drug compatibility information, see Compatibility under Stability.
Administer by slow, direct IV injection or by slow, continuous IV infusion.1 3 7 19 23 51 52 53 73 79 93 94 210
Labetalol injection is intended for use in hospitalized patients.1
Patients must be kept in a supine position during and for 3 hours after IV administration since symptomatic orthostatic hypotension is likely to occur if patients are tilted upward or allowed to assume an upright position.1 3 (See Hypotension under Cautions.)
For IV infusion, dilute labetalol injection to an appropriate concentration in a compatible IV infusion solution (e.g., add 200 mg of the drug to 160 mL of 5% dextrose injection to provide a solution containing 1 mg/mL).1 3
Rate of Administration
Administer repeat doses by slow, direct IV injection over a 2-minute period at intervals of 10 minutes.1 3 53 73 79 94 298 500
Administer diluted solutions by slow, continuous IV infusion1 3 51 73 210 with a controlled-infusion device to facilitate a desired rate of infusion.1 3
Available as labetalol hydrochloride; dosage expressed in terms of the salt.
Initially, 1–3 mg/kg daily given in 2 divided doses.333 Increase dosage as necessary up to a maximum of 10–12 mg/kg or 1.2 g daily given in 2 divided doses.333
Rapid Reduction of BP†IV Injection
Children 1–17 years of age: 0.2–1 mg/kg up to maximum of 40 mg per dose by direct IV injection.333IV Infusion
Alternatively, 0.25–3 mg/kg per hour by continuous IV infusion.333
Initially, 100 mg twice daily, either alone or in combination with a diuretic.2 4 293
Adjust dosage in increments of 100 mg twice daily every 2 or 3 days until optimum BP response is achieved.2 4
For maintenance, manufacturers recommend a usual dosage of 200–400 mg twice daily.2 4 Manufacturers state that some adults with severe hypertension may require up to 1.2–2.4 g daily in 2 or 3 divided doses.2 4 a
Some experts recommend a usual range of 100–400 mg twice daily.500 Rationale for lower dosage range is that it may be preferable to add another drug rather than continue to increase dosage.332
If intolerable adverse effects occur, consider dosage reduction; if adverse effects worsen or fail to resolve, may need to discontinue and switch to another antihypertensive drug class.501
Adjustment of labetalol dosage may be necessary when diuretic is initiated in a patient already receiving labetalol; optimum maintenance dosage is usually lower.2 4
When transferring from other antihypertensive agents, start with usual initial labetalol dosage and gradually decrease dosage of the existing regimen.2 4
Severe Hypertension and Hypertensive Crisis
Initially, 20–80 mg by slow, direct IV injection.1 3 7 19 53 79 94 274 500
Higher initial doses (e.g., 1–2 mg/kg) have been administered,51 55 235 but the 20-mg dose is recommended to minimize adverse effects and the risks associated with too rapid reduction in BP.23 53 79
May give additional doses, usually 40–80 mg1 3 7 53 79 94 (range: 20–80 mg),19 73 79 274 500 at 10-minute intervals until the desired supine BP is achieved or up to a total cumulative dose of 300 mg.1 3 7 19 53 73 79 94 274 298
Alternatively, initial rate of 0.5–2 mg/minute by continuous IV infusion; adjust rate according to the BP response.1 3 7 19 52 73 210 274 500
The usual effective, cumulative dose is 50–200 mg; up to 300 mg may be required.1 3
Progressive, incremental IV infusion regimen† (i.e., infusing 20, 40, 80, and 160 mg/hour for 1 hour at each dose level, or until the desired BP is achieved) has been used, and may result in more gradual BP reduction, minimizing adverse effects compared with repeated IV injections of the drug.21 51 197 Controlled comparisons of various IV administration methods are not available.
Oral (following IV dosage)
Discontinue IV therapy and initiate oral labetalol therapy when the DBP begins to increase.1 3
Initially 200 mg, followed in 6–12 hours by an additional dose of 200 or 400 mg, depending on the BP response.1 3
If necessary, oral dosage may be increased in usual increments at 1-day intervals while the patient is hospitalized.1 3
Follow the usual oral dosage recommendations for subsequent outpatient dosage titration or maintenance dosing.1 3
Initially, 20 mg by slow, direct IV injection, followed by 40 mg IV 10 minutes later and then 80-mg doses at 10-minute intervals for 2 additional doses.500
Maximum 10–12 mg/kg or 1.2 g daily.333
Children 1–17 years of age: Maximum 40 mg per dose.333
Maximum titration increment of 200 mg twice daily.a
Severe Hypertension and Hypertensive Crisis
Maximum cumulative dose of 300 mg.1 3 7 19 53 73 79 94 274 298
Maximum cumulative dose of 220 mg.500
Dosage reduction may be necessary, but specific data are currently not available.7 39
No dosage adjustment required in patients with mild to moderate renal impairment.60 146 147 239 In patients with severe renal impairment (i.e., Clcr <10 mL/minute) undergoing dialysis, once-daily dosing may be adequate.241
Adjustment in initial dosage not required.a Maintenance dosage requirements are lower in most geriatric patients; 100–200 mg twice daily usually required.4 a 4
Cautions for Labetalol Hydrochloride
Obstructive airway disease (e.g., bronchial asthma).1 2 3 4 311
Overt cardiac failure.1 2 3 4 311
Heart block greater than first degree.1 2 3 4 311
Cardiogenic shock.1 2 3 4 311
Severe bradycardia.1 2 3 4 311
Other conditions associated with severe and prolonged hypotension.1 3 4 247
Known hypersensitivity to labetalol or any ingredient in the formulation.1 3 4 247
Rarely, jaundice, hepatitis, severe hepatocellular injury, and elevated liver function test results have occurred; usually reversible following discontinuance,1 2 3 4 247 248 however, hepatic necrosis and death have been reported.1 2 3 4 247 248 254 255 275 276
Discontinue immediately if jaundice or laboratory evidence of hepatic injury occurs.1 2 3 4 247 248
Perform liver function tests at the first signs or symptoms of liver dysfunction (e.g., pruritus, dark urine, persistent anorexia, jaundice, right upper quadrant tenderness, flu-like syndrome).1 2 3 4 247 248
Possible precipitation of heart failure.1 2 3 4 7 Use contraindicated in patients with overt heart failure;1 2 3 4 may use cautiously in patients with well-compensated heart failure (e.g., those controlled with cardiac glycosides and/or diuretics).1 2 3 4 Use with caution in patients with inadequate cardiac function.1 2 3 4 7
Adequate treatment (e.g., with a cardiac glycoside and/or diuretic) and close observation recommended if signs and symptoms of impending cardiac failure occur; if cardiac failure continues, discontinue therapy, gradually if possible.1 2 3 4
Abrupt Withdrawal of Therapy
Abrupt withdrawal may exacerbate angina symptoms or precipitate MI in patients with CAD.1 2 3 4 Avoid abrupt discontinuance.2 4 Gradually decrease dosage over a period of 1–2 weeks, particularly in patients with ischemic heart disease and monitor patients carefully.1 2 3 4 If exacerbation of angina occurs or acute coronary insufficiency develops, reinstitute therapy promptly, at least temporarily, and initiate appropriate measures for the management of unstable angina pectoris.1 2 3 4
Labetalol may be less likely than pure β-adrenergic blocking agents to produce adverse cardiovascular withdrawal reactions (e.g., angina, rebound hypertension) following abrupt withdrawal;9 74 75 76 77 78 164 angina pectoris has not been reported to date following discontinuance of labetalol.1 2 3 4
Possible inhibition of bronchodilation produced by endogenous catecholamines; use generally not recommended in patients with bronchospastic disease.2 4
May use oral labetalol with caution in patients with nonallergic bronchospasm (e.g., chronic bronchitis, emphysema) who do not respond to or cannot tolerate other hypotensive agents;2 4 use smallest effective dose to minimize inhibition of endogenous or exogenous β-adrenergic agonist activity.2 4
Do not use IV labetalol in patients with nonallergic bronchospasm at the usual therapeutic doses; has not been studied adequately.1 3
Use with caution in patients with pheochromocytoma;1 2 3 4 186 187 oral labetalol may induce paradoxical hypertensive crisis.7 186 187 203 Use not recommended unless pretreatment with α-adrenergic blocking agents (e.g., IV phentolamine) has occurred.7
Employ appropriate methods for determining urinary catecholamines if used in known or suspected pheochromocytoma.1 2 3 4 (See Specific Drugs and Laboratory Tests under Interactions.)
Diabetes and Hypoglycemia
Possible decreased signs and symptoms of hypoglycemia (e.g., tachycardia, BP changes),1 2 3 4 impaired glucose tolerance, delayed rate of recovery of blood glucose concentration following drug-induced hypoglycemia, altered hemodynamic response to hypoglycemia (possibly resulting in exaggerated hypertensive response), and impaired peripheral circulation.211 212
Use with caution in patients with diabetes mellitus;1 2 3 4 dosage adjustment of the hypoglycemic agent may be necessary.1 2 3 4
Severe, protracted hypotension and difficulty in restarting or maintaining a heart beat have occurred during surgery in some patients receiving β-adrenergic blocking agents;1 2 3 4 however, withdrawal of β-adrenergic blocking agent prior to major surgery is controversial.1 2 3 4
Effect of labetalol’s α-adrenergic activity in patients undergoing major surgery has not been evaluated,1 2 3 4 but several deaths have been reported with the use of the injection during surgery, including when used to control bleeding.1 3
Synergistic hypotensive response occurs with concomitant use of IV labetalol and halothane anesthesia.1 2 3 4 183 190 191 192 193 194 195 (See Specific Drugs and Laboratory Tests under Interactions.)
Severely Elevated BP
Use caution when reducing severely elevated BP.1 3
Use IV labetalol in hospitalized patients,1 3 and achieve the desired reduction over longest period of time compatible with the patient’s clinical status.1 3
Avoid rapid or excessive reductions in SBP or DBP.1 3
Serious adverse effects (e.g., cerebral infarction, optic nerve infarction, angina, and ischemic changes in the ECG)51 79 197 have been reported when severely elevated BP was reduced over several hours to up to 1 or 2 days with other hypotensive agents.311
Orthostatic hypotension associated with loss of consciousness reported occasionally following IV administration51 54 55 132 and rarely following oral administration.2 4 Symptomatic orthostatic hypotension is likely to occur if supine patients are tilted upward or allowed to assume the upright position within 3 hours following IV administration.1 3
If hypotension occurs, place the patient in Trendelenburg’s position, administer IV fluids, and/or temporarily discontinue administration of the drug.51 79 94 197
Patients should remain supine during and for up to 3 hours after IV administration.1 3 Establish patient’s ability to tolerate an upright position before any ambulation (e.g., use of toilet facilities) is permitted; advise patient on how to proceed gradually to become ambulatory and observe at the time of initial ambulation.1 3
Monitor laboratory parameters at regular intervals in patients receiving long-term oral therapy.2 4
Routine laboratory tests are usually not required before or after IV administration.1 3
In patients with concomitant illnesses (e.g., impaired renal function), perform appropriate tests to monitor these conditions.1 2 3 4
Possible Prescribing and Dispensing Errors
Ensure accuracy of prescription; similarity in spelling of labetalol hydrochloride and Lamictal (lamotrigine, an anticonvulsant agent) has resulted in dispensing errors.319 320 Errors may be associated with serious adverse events (e.g., status epilepticus, serious lamotrigine rash) in patients receiving the wrong drug.319 320
History of Anaphylactic Reactions
Possible increased reactivity to a variety of allergens;1 patients may be less responsive to usual doses of epinephrine used to treat anaphylactic reactions.1 3 4
Shares the toxic potentials of β-adrenergic and postsynaptic α1-adrenergic blocking agents;1 2 3 4 7 8 9 observe the usual precautions of these agents.1 2 3 4 7
Category C.1 2 3 4 247 248 a
Distributed into milk.1 2 3 4 6 7 64 68 69 Caution if used in nursing women.1 2 3 4
Safety and efficacy not fully established;1 2 3 4 247 248 however, some experts have recommended dosages for hypertension based on current limited clinical experience.333
Orthostatic symptoms (e.g., orthostatic hypotension, dizziness, lightheadedness) are more likely in geriatric individuals than in younger adults; caution geriatric patients about the possibility of such symptoms.4
A lower maintenance dosage may be required because of reduced elimination in geriatric patients.4 (See Geriatric Patients under Dosage and Administration.)
Use with caution; metabolism of the drug may be decreased.1 2 3 4 7 39 247 248 (See Special Populations under Pharmacokinetics.)
Elimination half-life may be increased in patients with severe renal impairment undergoing dialysis; once-daily dosing may be possible in these patients.241 (See Renal Impairment under Dosage and Administration.)
Common Adverse Effects
Symptomatic orthostatic hypotension,1 2 3 4 7 8 9 19 23 46 51 54 55 79 81 83 88 91 94 96 100 108 122 129 132 158 159 247 248 dizziness1 2 3 4 8 23 74 75 76 79 80 81 82 88 90 158 159 or lightheadedness,23 51 53 85 fatigue,1 2 3 4 23 75 76 78 87 159 nausea,1 2 3 4 7 8 19 23 51 53 74 75 76 78 79 80 81 82 83 87 90 93 94 158 159 247 248 dyspepsia.1 2 3 4 7 8 23 74 75 76 79 82 83 93 94 158 159 247 248
Interactions for Labetalol Hydrochloride
Specific Drugs and Laboratory Tests
Drug or Test
Labetalol may antagonize bronchodilating effects1 2 3 4
Greater than usual dosages of β-adrenergic agonist bronchodilators may be required1 2 3 4
Calcium-channel blocking agents (e.g., verapamil, diltiazem)
Possible additive therapeutic256 257 258 259 260 261 262 263 264 265 267 268 269 270 271 272 273 and adverse effects257 261 264 266 267 268 271 272 273
Use concomitantly with caution1 3 4 247 258 259 260 261 264 266 268 271 272 273 290 291
Absolute bioavailability of oral labetalol substantially increased, possibly via enhanced absorption or decreased first-pass hepatic metabolism 1 2 3 4 180 229
Carefully adjust labetalol dosage for optimal BP control with concomitant use1 2 3 4 229
Increased hypotensive effect 2 4 7 8 9 15 19 72 76 77 78 80 81 82 83 85 87 90 91 96 97 99 231 234
Usually used to therapeutic advantage; careful dosage adjustments recommended2 4 7 8 9 15 19 72 76 77 78 80 81 82 83 85 87 90 91 96 97 99 231 234
Glutethimide (no longer commercially available in the US)
Absolute bioavailability of oral labetalol decreased, possibly by increasing first-pass hepatic metabolism 229
Carefully adjust labetalol dosage for optimal BP control with concomitant use229
Synergistic hypotensive effect; 183 190 191 192 193 194 195 may result in large reduction in cardiac output and increase in central venous pressure1 2 3 4 183 190 191 192 193 194 195
Adjust halothane concentration to control the degree and duration of hypotension;183 190 191 192 193 194 195 to minimize the risk of excessive hypotension, inspired halothane concentrations of ≥3% should not be used1 2 3 4
Inform anesthesiologist if labetalol therapy is continued in a patient undergoing major surgery1 2 3 4
Mibefradil (no longer commercially available in the US)
Slowing or complete suppression of SA node activity, with slow ventricular rates290 291
Possible additive hypotensive effects1 2 3 4 and antagonism of the reflex tachycardia produced by nitroglycerin1 2 3 4
Possible increased incidence of tremor 1 2 3 4
Tests for urinary catecholamines
Labetalol metabolites in urine may result in false-positive elevations of urinary free216 and total217 catecholamines, metanephrine, normetanephrine, and 3-methoxy-4-hydroxymandelic acid (vanillylmandelic acid, VMA) measured by fluorometric or photometric methods1 2 3 4 216 217 218 248
When screening labetalol-treated patients suspected of having pheochromocytoma or when evaluating labetalol-treated patients with the tumor, use specific assay methods such as high-performance liquid chromatography (HPLC) with solid phase extraction1 2 3 4 218 248 252 to determine concentrations of catecholamines or their metabolites1 2 3 4 216 217 218 248
Labetalol Hydrochloride Pharmacokinetics
Rapidly and almost completely absorbed (i.e., 90–100%) from the GI tract following oral administration.2 4 5 6 7 8 10 34 58 59
Undergoes extensive first-pass metabolism in the liver and/or GI mucosa.2 4 5 6 7 8 10 23 33 34 35 37 41 58 Absolute bioavailability is about 25%.2 4 5 6 7 34 37
Following oral administration, hypotensive effect is generally apparent within 20 minutes to 2 hours,6 10 34 43 48 56 57 and maximal within 1–4 hours.2 4 5 6 7 34 43 48 56
Maximum, steady-state BP response with twice-daily dosing occurs within 1–3 days.2 4
Following slow, direct IV injection, hypotensive effect is apparent within 2–5 minutes,5 6 7 33 47 51 52 53 54 55 240 and usually maximal within 5–15 minutes.1 3 53 54 55 240
Dose dependent; about 8–12 or 12–24 hours after a single 200- or 300-mg dose, respectively.2 4 5 6 43 57
Following slow, direct IV injection, the hypotensive effect generally persists for about 2–4 hours,6 53 55 although a longer duration of effect (i.e., up to 24 hours) has been reported in some patients.6 33 53 55 240
Delays absorption,36 but increases absolute bioavailability.2 4 5 7 10 36 37
Relative bioavailability is increased in hepatic impairment.a 1 2 3 4 5 10 39
First-pass metabolism may be reduced and bioavailability substantially increased in geriatric patients.7 10 38
Following IV administration, rapidly and widely distributed into the extravascular space.5 7 10 33 34 35
In animals, highest concentrations in the lungs, liver, and kidneys;5 7 10 58 only minimal amounts cross the blood-brain barrier.1 2 3 4 5 7 10 58
Crosses the placenta;1 2 3 4 5 6 58 64 65 66 67 70 distributed into milk,1 2 3 4 5 6 7 64 68 69 principally as unbound labetalol.5
Plasma Protein Binding
Approximately 50%.1 2 3 4 5 7 10 58
In patients with impaired hepatic function, the apparent volume of distribution is decreased.39
Following oral administration, extensively metabolized in the liver and possibly in the GI mucosa principally by conjugation with glucuronic acid,1 2 3 4 5 7 10 58 principally to O-alkylglucuronide5 and smaller amounts of O-phenylglucuronide and N-glucuronide.5 10 58
Undergoes extensive first-pass metabolism in the liver and/or GI mucosa.2 4 5 6 7 8 10 23 33 34 35 37 41 58
Excreted in feces via biliary elimination (30% within 4 days) and in urine (55–60% within 24 hours), mainly as glucuronide conjugates.1 2 3 4 5 7 10 58 1 2 3 4 5 7 10 58
Less than 5% of a dose is excreted unchanged in urine.7 10 58
Biphasic5 7 10 33 35 43 58 59 or possibly triphasic;10 33 241 terminal half-life averages 2.5–8 hours.1 2 3 4 5 7 10 33 35 37 38 39 41 43 58 60 63 Manufacturers specify half-life of 5.5 or 6–8 hours following IV or oral administration, respectively.1 2 3 4
Elimination may be reduced and half-life may be slightly increased in geriatric individuals.4 7 10 38
Half-life apparently unchanged in individuals with renal1 2 3 4 5 10 60 71 239 or hepatic impairment,1 2 3 4 39 but may be increased in patients with severe renal impairment (i.e., Clcr <10 mL/minute) undergoing dialysis.241
Not appreciably removed (<1% of a dose) by hemodialysis203 204 241 242 or peritoneal dialysis.203 223 241 242
Well-closed containers20 at 2–30°C.2 4 5 6
Protect tablets in unit-dose packages from excessive moisture.2 4 5 6
2–30°C; protect from light and freezing.1 3 5 6
For information on systemic interactions resulting from concomitant use, see Interactions.
Dextrose 5% in Ringer’s injection
Dextrose 5% in Ringer’s injection, lactated
Dextrose 2.5% in sodium chloride 0.45%
Dextrose 5% in sodium chloride 0.2, 0.33, or 0.9%
Dextrose 5% in water
Polysal in dextrose 5%
Ringer’s injection, lactated
Sodium chloride 0.9%
Sodium bicarbonate 5%
Chloramphenicol sodium succinate
Hetastarch in lactated electrolyte injection (Hextend)
Hydroxyethyl starch 130/0.4 in sodium chloride 0.9%
Penicillin G potassium
Amphotericin B cholesteryl sulfate complex
Competitively blocks adrenergic stimulation of β-receptors within the myocardium (β1-receptors) and within bronchial and vascular smooth muscle (β2-receptors) and α1-receptors within vascular smooth muscle.1 2 3 4 7 8 9 21 22 23 24 28 29 30 32 44
Has some intrinsic β2-agonist activity in animals,1 2 3 4 7 30 62 221 222 but exerts little, if any, intrinsic β1-agonist activity;1 2 3 4 7 8 9 30 62 107 does not exhibit intrinsic α-adrenergic agonist activity.7 28 30
Unlike pure β-adrenergic blocking agents, produces a dose-dependent (at usual doses) decrease in systemic arterial BP and systemic vascular resistance without a substantial reduction in resting heart rate, cardiac output, or stroke volume, apparently because of its combined α- and β-adrenergic blocking activity.1 2 3 4 7 112 113 114
Effectively reduces BP in the standing or supine position, but because of the drug’s α1-adrenergic blocking activity, the effect on BP is position dependent; labetalol-induced decreases in BP are greater in the standing than in the supine position, and orthostatic hypotension can occur.1 2 3 4 7 8 9 112 113 114 115 116 117 118 119 120 121 122 123 124
Electrophysiologic effects of labetalol are variable and appear to be mediated via the drug’s myocardial β1-adrenergic blocking activity.1 2 3 4 7 111 219 220
May decrease conduction velocity through the AV node and increase the atrial effective refractory period (ERP), but the drug appears to have inconsistent effects on SA conduction time and the AV nodal refractory period;1 2 3 4 7 111 the decrease in AV nodal conduction velocity produced by labetalol is less than that produced by pure β-adrenergic blocking agents.7
Generally has little effect on sinus rate, intraventricular conduction, the His-Purkinje system, or duration of the QRS complex.1 2 3 4 7 111
Advice to Patients
Importance of taking medication exactly as prescribed.a
Importance of not interrupting or discontinuing therapy without consulting clinician; patients should temporarily limit their physical activity when discontinuing therapy.1 2 3 4
Importance of patients informing anesthesiologist or dentist about labetalol therapy before undergoing major surgery.1 2 3 4
Importance of immediately informing clinician at the first sign or symptom of impending cardiac failure or if any difficulty in breathing occurs.1 2 3 4
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1 2 3 4
Advise patients that transient scalp tingling may occur, usually during initiation of labetalol therapy.1 2 3 4
Caution geriatric patients about the possibility of orthostatic symptoms (orthostatic hypotension, dizziness, lightheadedness).4
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 2 3 4 247 248
Importance of informing patients of other important precautionary information. (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Labetalol Hydrochloride Tablets
Labetalol Hydrochloride Tablets
Labetalol Hydrochloride Tablets
Injection, for IV use
Labetalol Hydrochloride Injection
AHFS DI Essentials. © Copyright 2018, Selected Revisions October 30, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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