Labetalol 5mg/ml Inj, 20ml
It is used to treat high blood pressure.
Drug Class
Antihypertensive
Pharmacologic Class
Alpha-1 and Non-selective Beta-Adrenergic Blocker
Pregnancy Category
C
FDA Approved
Aug 1984
DEA Schedule
Not Controlled
Overview
What is this medicine?
Labetalol injection is a medicine given into a vein to quickly lower very high blood pressure. It works by relaxing blood vessels and slowing down the heart rate.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Adhere to the dosage instructions carefully. This medication is administered intravenously over a specified period.
Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist for guidance on proper storage procedures.
Missing a Dose
If you miss a dose, contact your doctor for advice on the best course of action to take.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Adhere to the dosage instructions carefully. This medication is administered intravenously over a specified period.
Storing and Disposing of Your Medication
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist for guidance on proper storage procedures.
Missing a Dose
If you miss a dose, contact your doctor for advice on the best course of action to take.
Lifestyle & Tips
- Remain in a lying or sitting position for a period after receiving the injection to prevent dizziness or fainting.
- Report any unusual symptoms immediately to your healthcare provider.
- Avoid sudden changes in position (e.g., standing up quickly) once mobile, as this can cause dizziness.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Hypertensive Emergency: Initial 20 mg IV bolus, then 40-80 mg every 10 minutes, or continuous infusion 0.5-2 mg/min. Max total dose 300 mg.
Dose Range:
20 - 300 mg
Condition-Specific Dosing:
Hypertensive Emergency:
Initial 20 mg IV bolus, then 40-80 mg every 10 minutes, or continuous infusion 0.5-2 mg/min. Max total dose 300 mg.
Pediatric Dosing
Neonatal:
Not established
Infant:
Hypertensive Emergency: Initial 0.2-1 mg/kg IV (max 20 mg), then 0.25-1 mg/kg/dose every 10-15 min (max 3 mg/kg total or 300 mg). Continuous infusion 0.25-3 mg/kg/hr.
Child:
Hypertensive Emergency: Initial 0.2-1 mg/kg IV (max 20 mg), then 0.25-1 mg/kg/dose every 10-15 min (max 3 mg/kg total or 300 mg). Continuous infusion 0.25-3 mg/kg/hr.
Adolescent:
Hypertensive Emergency: Initial 0.2-1 mg/kg IV (max 20 mg), then 0.25-1 mg/kg/dose every 10-15 min (max 3 mg/kg total or 300 mg). Continuous infusion 0.25-3 mg/kg/hr.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment needed, use with caution.
Moderate:
No specific dose adjustment needed, use with caution.
Severe:
No specific dose adjustment needed, use with caution due to potential for accumulation of metabolites.
Dialysis:
Labetalol is not significantly removed by hemodialysis. No specific supplemental dose needed, but monitor response.
Hepatic Impairment:
Mild:
Use with caution.
Moderate:
Use with caution, reduced metabolism may occur. Consider lower doses.
Severe:
Use with caution, reduced metabolism may occur. Consider lower doses.
Pharmacology
Mechanism of Action
Labetalol is a non-selective beta-adrenergic receptor blocker (beta1 and beta2) and a selective alpha1-adrenergic receptor blocker. It reduces peripheral vascular resistance through alpha1-blockade and reduces heart rate and myocardial contractility through beta-blockade, leading to a reduction in blood pressure.
Pharmacokinetics
Absorption:
Bioavailability:
100% (IV)
Tmax:
Not applicable (IV)
FoodEffect:
Not applicable (IV)
Distribution:
Vd:
3.2-16.3 L/kg
ProteinBinding:
Approximately 50%
CnssPenetration:
Limited
Elimination:
HalfLife:
5.5-8 hours (IV)
Clearance:
1.1-1.7 L/min
ExcretionRoute:
Primarily renal (55-60% as metabolites, <5% unchanged), some biliary/fecal.
Unchanged:
<5%
Pharmacodynamics
OnsetOfAction:
2-5 minutes (IV)
PeakEffect:
5-15 minutes (IV)
DurationOfAction:
2-4 hours (IV)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe dizziness or fainting
Slow heartbeat
Abnormal burning, numbness, or tingling sensations
Erectile dysfunction
Heart failure or worsening of existing heart failure, characterized by:
+ Shortness of breath
+ Sudden weight gain
+ Irregular heartbeat
+ New or worsening swelling in the arms or legs
Liver problems, which may be indicated by:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellowing of the skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:
Dizziness
Fatigue
Weakness
Upset stomach
Tingling sensation on the scalp
* Stuffy nose
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe dizziness or fainting
Slow heartbeat
Abnormal burning, numbness, or tingling sensations
Erectile dysfunction
Heart failure or worsening of existing heart failure, characterized by:
+ Shortness of breath
+ Sudden weight gain
+ Irregular heartbeat
+ New or worsening swelling in the arms or legs
Liver problems, which may be indicated by:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellowing of the skin or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:
Dizziness
Fatigue
Weakness
Upset stomach
Tingling sensation on the scalp
* Stuffy nose
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe dizziness or lightheadedness
- Fainting
- Very slow heartbeat
- Difficulty breathing or wheezing
- Swelling in hands or feet
- Chest pain
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have low blood pressure.
If you have any of the following health conditions:
+ Respiratory problems, such as asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block or heart failure (a weakened heart)
+ Shock caused by heart problems
+ A slow heartbeat
If you are currently taking diltiazem or verapamil.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications (including prescription and over-the-counter drugs, natural products, and vitamins) and health problems with your doctor and pharmacist. Before starting, stopping, or changing the dose of any medication, consult with your doctor to confirm that it is safe to do so in conjunction with this medication.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have low blood pressure.
If you have any of the following health conditions:
+ Respiratory problems, such as asthma or chronic obstructive pulmonary disease (COPD)
+ Heart block or heart failure (a weakened heart)
+ Shock caused by heart problems
+ A slow heartbeat
If you are currently taking diltiazem or verapamil.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications (including prescription and over-the-counter drugs, natural products, and vitamins) and health problems with your doctor and pharmacist. Before starting, stopping, or changing the dose of any medication, consult with your doctor to confirm that it is safe to do so in conjunction with this medication.
Precautions & Cautions
Important Information About Your Medication
It is crucial that you inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This will help ensure that you receive the best possible care.
Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other activities that require you to be alert. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying down position, and be careful when climbing stairs.
Monitoring Your Condition
Follow your doctor's instructions for checking your blood pressure and heart rate. Additionally, have your blood work and other laboratory tests done as directed by your doctor. This medication may affect the results of certain lab tests, so be sure to inform all of your healthcare providers and laboratory personnel that you are taking this medication.
Managing Low Blood Sugar
This medication may mask some symptoms of low blood sugar, such as a rapid heartbeat, which can increase the risk of severe or prolonged low blood sugar. This is particularly concerning for individuals with diabetes, children, and those who are fasting, undergoing surgery, or experiencing nausea and vomiting. If you have questions or concerns, discuss them with your doctor. If you have diabetes, it is essential to monitor your blood sugar levels closely.
Stopping the Medication
Do not stop taking this medication abruptly, as this can lead to worsening chest pain or even a heart attack, especially if you have certain types of heart disease. To avoid these side effects, your doctor will instruct you on how to gradually stop taking the medication. If you experience new or worsening chest pain or other heart problems, contact your doctor immediately.
Allergic Reactions
If you have a history of severe allergic reactions, consult with your doctor about the potential risks of anaphylaxis. If you use epinephrine to treat severe allergic reactions, discuss this with your doctor, as the medication may affect the efficacy of epinephrine.
Surgery and Eye Procedures
Inform your doctor if you are scheduled to undergo cataract surgery or other eye procedures.
Interactions with Other Medications
Before taking over-the-counter (OTC) medications that may increase blood pressure, such as cough and cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, or certain natural products, consult with your doctor.
Special Considerations for Older Adults
If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects.
Pregnancy and Breastfeeding
If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
It is crucial that you inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This will help ensure that you receive the best possible care.
Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other activities that require you to be alert. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying down position, and be careful when climbing stairs.
Monitoring Your Condition
Follow your doctor's instructions for checking your blood pressure and heart rate. Additionally, have your blood work and other laboratory tests done as directed by your doctor. This medication may affect the results of certain lab tests, so be sure to inform all of your healthcare providers and laboratory personnel that you are taking this medication.
Managing Low Blood Sugar
This medication may mask some symptoms of low blood sugar, such as a rapid heartbeat, which can increase the risk of severe or prolonged low blood sugar. This is particularly concerning for individuals with diabetes, children, and those who are fasting, undergoing surgery, or experiencing nausea and vomiting. If you have questions or concerns, discuss them with your doctor. If you have diabetes, it is essential to monitor your blood sugar levels closely.
Stopping the Medication
Do not stop taking this medication abruptly, as this can lead to worsening chest pain or even a heart attack, especially if you have certain types of heart disease. To avoid these side effects, your doctor will instruct you on how to gradually stop taking the medication. If you experience new or worsening chest pain or other heart problems, contact your doctor immediately.
Allergic Reactions
If you have a history of severe allergic reactions, consult with your doctor about the potential risks of anaphylaxis. If you use epinephrine to treat severe allergic reactions, discuss this with your doctor, as the medication may affect the efficacy of epinephrine.
Surgery and Eye Procedures
Inform your doctor if you are scheduled to undergo cataract surgery or other eye procedures.
Interactions with Other Medications
Before taking over-the-counter (OTC) medications that may increase blood pressure, such as cough and cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, or certain natural products, consult with your doctor.
Special Considerations for Older Adults
If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects.
Pregnancy and Breastfeeding
If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
Overdose Information
Overdose Symptoms:
- Severe hypotension (low blood pressure)
- Bradycardia (slow heart rate)
- Heart block
- Cardiogenic shock
- Bronchospasm
- Seizures
What to Do:
Seek immediate medical attention. Management is supportive and symptomatic. May include IV fluids, atropine for bradycardia, glucagon for severe beta-blocker toxicity, vasopressors for hypotension, and bronchodilators for bronchospasm. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Contraindicated Interactions
- Bronchial asthma
- Overt cardiac failure
- Greater than first-degree heart block
- Cardiogenic shock
- Severe bradycardia
Major Interactions
- Calcium channel blockers (e.g., verapamil, diltiazem): Risk of severe bradycardia, heart block, or cardiac arrest.
- General anesthetics (e.g., halothane, isoflurane): Additive hypotensive effects.
- Cimetidine: Increases labetalol bioavailability and plasma levels.
- Tricyclic antidepressants: May increase incidence of tremor.
- Other beta-blockers: Additive effects, increased risk of bradycardia and hypotension.
Moderate Interactions
- NSAIDs (e.g., ibuprofen, indomethacin): May reduce antihypertensive effect.
- Alpha-blockers (e.g., prazosin): Additive hypotensive effects.
- Phosphodiesterase-5 inhibitors (e.g., sildenafil): Additive hypotensive effects.
- Insulin and oral hypoglycemics: May mask symptoms of hypoglycemia (tachycardia).
Minor Interactions
- Not many specific minor interactions are clinically significant.
Monitoring
Baseline Monitoring
Blood Pressure (BP)
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to administration
Heart Rate (HR)
Rationale: To establish baseline and monitor for bradycardia.
Timing: Prior to administration
Electrocardiogram (ECG)
Rationale: To assess for pre-existing heart block or arrhythmias.
Timing: Prior to administration
Renal Function (BUN, Creatinine)
Rationale: To assess kidney function, as metabolites are renally excreted.
Timing: Prior to administration
Liver Function Tests (ALT, AST)
Rationale: To assess liver function, as labetalol is primarily metabolized in the liver.
Timing: Prior to administration
Routine Monitoring
Blood Pressure (BP)
Frequency: Continuously during infusion, then every 5-15 minutes until stable, then every 1-4 hours.
Target: Individualized based on clinical condition (e.g., MAP reduction by 10-25% in first hour for hypertensive emergency).
Action Threshold: Hypotension (e.g., SBP <90 mmHg or significant drop from baseline), or inadequate BP control.
Heart Rate (HR)
Frequency: Continuously during infusion, then every 5-15 minutes until stable, then every 1-4 hours.
Target: Typically >50-60 bpm, individualized.
Action Threshold: Bradycardia (<50 bpm or symptomatic bradycardia).
Fluid Balance
Frequency: Daily or as clinically indicated.
Target: Not applicable
Action Threshold: Signs of fluid overload or dehydration.
Symptom Monitoring
- Dizziness
- Lightheadedness
- Fatigue
- Shortness of breath
- Wheezing
- Chest pain
- Peripheral edema
- Nausea
- Vomiting
- Scalp tingling
Special Patient Groups
Pregnancy
Category C. Labetalol is often used for hypertension in pregnancy, including preeclampsia and eclampsia. Use only if the potential benefit justifies the potential risk to the fetus. Neonates exposed to labetalol in utero should be monitored for signs of bradycardia, hypoglycemia, and respiratory depression.
Trimester-Specific Risks:
First Trimester:
Limited data, but generally considered safer than some other antihypertensives. Risk of fetal growth restriction has been reported.
Second Trimester:
Commonly used for hypertension in this trimester. Monitor fetal growth.
Third Trimester:
Commonly used for hypertension in this trimester. Monitor neonate for bradycardia, hypoglycemia, and respiratory depression after birth.
Lactation
L3 (Moderately Safe). Labetalol is excreted into breast milk in small amounts. Generally considered compatible with breastfeeding, but monitor the infant for signs of bradycardia, hypotension, and hypoglycemia.
Infant Risk:
Low risk, but monitor for bradycardia, hypotension, and hypoglycemia.
Pediatric Use
Used for hypertensive emergencies in pediatric patients. Dosing is weight-based and requires careful titration and monitoring. Safety and efficacy in neonates have not been established.
Geriatric Use
Use with caution in elderly patients, starting with lower doses, due to increased likelihood of decreased hepatic, renal, or cardiac function, and concomitant disease or other drug therapy. Monitor closely for adverse effects, especially hypotension and bradycardia.
Clinical Information
Clinical Pearls
- IV Labetalol is a first-line agent for hypertensive emergencies, especially when heart rate control is also desired.
- Avoid in patients with bronchial asthma, overt cardiac failure, or severe bradycardia due to its beta-blocking effects.
- Can cause orthostatic hypotension, particularly with initial doses or rapid titration; patients should remain supine during and immediately after administration.
- Paradoxical pressor response (hypertension) can occur if given with epinephrine due to unopposed alpha-adrenergic stimulation.
- Scalp tingling is a common, benign side effect that usually resolves with continued therapy.
Alternative Therapies
- Nicardipine (IV)
- Clevidipine (IV)
- Esmolol (IV)
- Hydralazine (IV)
- Sodium Nitroprusside (IV)
- Fenoldopam (IV)
Cost & Coverage
Average Cost:
Varies widely, typically low for generic IV formulation. per 20ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure safe and effective treatment, never share your medication with others or take someone else's medication.
Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Properly dispose of unused or expired medications by checking with your pharmacist for guidance on the best disposal method. Unless instructed to do so, avoid flushing medications down the toilet or pouring them down the drain, as this can harm the environment. Many communities have drug take-back programs that provide a safe and responsible way to dispose of unwanted medications.
Some medications may come with an additional patient information leaflet, which can be obtained by consulting with your pharmacist. If you have any questions or concerns about your medication, it is crucial to discuss them with your doctor, nurse, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken, as this will help healthcare professionals provide the most effective treatment.
Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Properly dispose of unused or expired medications by checking with your pharmacist for guidance on the best disposal method. Unless instructed to do so, avoid flushing medications down the toilet or pouring them down the drain, as this can harm the environment. Many communities have drug take-back programs that provide a safe and responsible way to dispose of unwanted medications.
Some medications may come with an additional patient information leaflet, which can be obtained by consulting with your pharmacist. If you have any questions or concerns about your medication, it is crucial to discuss them with your doctor, nurse, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken, as this will help healthcare professionals provide the most effective treatment.