Propranolol (capsule)

Propranolol (capsule)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alonso Alvarado, M.D. [2]

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Overview

Propranolol (capsule) is a beta-adrenergic blocker that is FDA approved for the {{{indicationType}}} of hypertension, angina pectoris, migraine, hypertrophic subaortic stenosis. Common adverse reactions include dermatitis, pruritus, diarrhea, dizziness, sleep disorder, fatigue.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Hypertension

The usual initial dosage is 80 mg propranolol once daily, whether used alone or added to a diuretic. The dosage may be increased to 120 mg once daily or higher until adequate blood pressure control is achieved. The usual maintenance dosage is 120 to 160 mg once daily. In some instances a dosage of 640 mg may be required. The time needed for full hypertensive response to a given dosage is variable and may range from a few days to several weeks.

Angina Pectoris

Starting with 80 mg propranolol once daily, dosage should be gradually increased at three- to seven-day intervals until optimal response is obtained. Although individual patients may respond at any dosage level, the average optimal dosage appears to be 160 mg once daily. In angina pectoris, the value and safety of dosage exceeding 320 mg per day have not been established.

If treatment is to be discontinued, reduce dosage gradually over a period of a few weeks.

Migraine

The initial oral dose is 80 mg propranolol once daily. The usual effective dose range is 160 to 240 mg once daily. The dosage may be increased gradually to achieve optimal migraine prophylaxis. If a satisfactory response is not obtained within four to six weeks after reaching the maximal dose, propranolol therapy should be discontinued. It may be advisable to withdraw the drug gradually over a period of several weeks depending on the patient's age, comorbidity, and dose of propranolol.

Hypertrophic Subaortic Stenosis

The usual dosage is 80 to 160 mg propranolol once daily.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Thyroid Storm

• Developed by: American Thyroid Association and American Association of Clinical Endocrinologists

• Class of Recommendation: 1 (high recommendation)

• Strength of Evidence: + (poor quality of evidence)

• Dosing Information/Recommendation

• 10–40 mg.

Non–Guideline-Supported Use

Anxiety

Congestive Heart Failure

• Dosing Information

• Initial dose of 10 mg/day followed by 10-mg increments until a dose of 30 mg q8h.

Gastrointestinal Hemorrhage

Percutaneous Coronary Intervention

• Dosing Information

• 15 μg/kg injected through the catheter directly to the coronary artery.

Portal Hypertention

• Dosing Information

• 40–120 mg/day.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Propranolol (capsule) FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Propranolol in pediatric patients.

Non–Guideline-Supported Use

Congestive Heart Failure

• Dosing Information

• 1,6 mg/kg/day

Tetralogy of Fallot

• Dosing Information

• (Dosage)

Portal Hypertension

Neonatal Thyroid Storm

Contraindications

• Cardiogenic shock
• Sinus bradycardia
• Second-degree AV block
• Third-degree AV block
• Bronchial asthma
• Hypersensitivity

Warnings

Angina Pectoris

There have been reports of exacerbation of angina and, in some cases, myocardial infarction, following abrupt discontinuance of propranolol therapy. Therefore, when discontinuance of propranolol is planned, the dosage should be gradually reduced over at least a few weeks, and the patient should be cautioned against interruption or cessation of therapy without the physician's advice. If propranolol therapy is interrupted and exacerbation of angina occurs, it usually is advisable to reinstitute propranolol therapy and take other measures appropriate for the management of unstable angina pectoris. Since coronary artery disease may be unrecognized, it may be prudent to follow the above advice in patients considered at risk of having occult atherosclerotic coronary disease who are given propranolol for other indications.

Hypersensitivity and Skin Reactions

Hypersensitivity reactions, including anaphylactic/anaphylactoid reactions, have been associated with the administration of propranolol

Cutaneous reactions, including Stevens-Johnson Syndrome, toxic epidermal necrolysis, exfoliative dermatitis, erythema multiforme, and urticaria, have been reported with use of propranolol.

Cardiac Failure

Sympathetic stimulation may be a vital component supporting circulatory function in patients with congestive heart failure, and its inhibition by beta blockade may precipitate more severe failure. Although beta blockers should be avoided in overt congestive heart failure, some have been shown to be highly beneficial when used with close follow-up in patients with a history of failure who are well compensated and are receiving diuretics as needed. Beta-blockers agents do not abolish the inotropic action of digitalis on heart muscle.

In Patients without a History of heart failure, continued use of beta blockers can, in some cases, lead to cardiac failure.

Nonallergic Bronchospasm (e.g., Chronic Bronchitis, Emphysema)

In general, patients with bronchospastic lung disease should not receive beta-blockers. Propranolol should be administered with caution in this setting since it may provoke a bronchial asthmatic attack by blocking bronchodilation produced by endogenous and exogenous catecholamine stimulation of beta-receptors.

Major Surgery

Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery, however the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures.

Diabetes and Hypoglycemia

Beta-adrenergic blockade may prevent the appearance of certain premonitory signs and symptoms (pulse rate and pressure changes) of acute hypoglycemia, especially in labile insulin-dependent diabetics. In these patients, it may be more difficult to adjust the dosage of insulin.

Propranolol therapy, particularly when given to infants and children, diabetic or not, has been associated with hypoglycemia especially during fasting as in preparation for surgery. Hypoglycemia has been reported in patients taking propranolol after prolonged physical exertion and in patients with renal insufficiency.

Thyrotoxicosis

Beta-blockade may mask certain clinical signs of hyperthyroidism. Therefore, abrupt withdrawal of propranolol may be followed by an exacerbation of symptoms of hyperthyroidism, including thyroid storm. Propranolol may change thyroid-function tests, increasing T4 and reverse T3, and decreasing T3.

Wolff-Parkinson-White Syndrome

Beta-blockade in patients with Wolff-Parkinson-White syndrome and tachycardia has been associated with severe bradycardia requiring treatment with a pacemaker. In one case, this result was reported after an initial dose of 5 mg propranolol.

Adverse Reactions

Clinical Trials Experience

Cardiovascular

• Bradycardia
• Congestive heart failure
• Intensification of AV block
• Hypotension
• Paresthesia of hands
• Thrombocytopenic purpura
• Arterial insufficiency, usually of the Raynaud type.

Central Nervous System

• Light-headedness
• Mental depression: Manifested by insomnia, lassitude, weakness, fatigue
• Catatonia
• Visual disturbances
• Hallucinations
• Vivid dreams
• An acute reversible syndrome characterized by disorientation for time and place, short-term memory loss, emotional lability, slightly clouded sensorium, and decreased performance on neuropsychometrics.
• For immediate release formulations, fatigue, lethargy, and vivid dreams appear dose related.

Gastrointestinal

• Nausea
• Vomiting
• Epigastric distress
• Abdominal cramping
• Diarrhea
• Constipation
• Mesenteric arterial thrombosis
• Ischemic colitis

Allergic

• Hypersensitivity reactions, including anaphylactic/anaphylactoid reactions
• Pharyngitis
• Agranulocytosis
• Erythematous rash
• Fever combined with aching and sore throat
• Laryngospasm
• Respiratory distress

Respiratory

• Bronchospasm

Hematologic

• Agranulocytosis
• Nonthrombocytopenic purpura and thrombocytopenic purpura.

Autoimmune

• Systemic lupus erythematosus (SLE).

Skin and mucous membranes

• Stevens-Johnson Syndrome
• Toxic epidermal necrolysis
• Dry eyes
• Exfoliative dermatitis
• Erythema multiforme
• Urticaria
• Alopecia
• SLE-like reactions,
• Psoriasisiform rashes.
• Oculomucocutaneous syndrome involving the skin, serous membranes, and conjunctivae reported for a beta-blocker (practolol) have not been associated with propranolol.

Genitourinary

• Male impotence
• Peyronie's disease

Postmarketing Experience

There is limited information regarding Propranolol (capsule) Postmarketing Experience in the drug label.

Drug Interactions

All drug interaction studies were conducted with propranolol. There are no data on drug interactions with Inderal LA capsules.

Interactions with Substrates, Inhibitors or Inducers of Cytochrome P-450 Enzymes

Because propranolol's metabolism involves multiple pathways in the Cytochrome P-450 system (CYP2D6, 1A2, 2C19), co-administration with drugs that are metabolized by, or affect the activity (induction or inhibition) of one or more of these pathways may lead to clinically relevant drug interactions (see Drug Interactions under PRECAUTIONS).

• Substrates or Inhibitors of CYP2D6: Blood levels and/or toxicity of propranolol may be increased by co-administration with substrates or inhibitors of CYP2D6, such as amiodarone, cimetidine, delavudin, fluoxetine, paroxetine, quinidine, and ritonavir. No interactions were observed with either ranitidine or lansoprazole.

• Substrates or Inhibitors of CYP1A2: Blood levels and/or toxicity of propranolol may be increased by co-administration with substrates or inhibitors of CYP1A2, such as imipramine, cimetidine, ciprofloxacin, fluvoxamine, isoniazid, ritonavir, theophylline, zileuton, zolmitriptan, and rizatriptan.

• Substrates or Inhibitors of CYP2C19: Blood levels and/or toxicity of propranolol may be increased by co-administration with substrates or inhibitors of CYP2C19, such as fluconazole, cimetidine, fluoxetine, fluvoxamine, tenioposide, and tolbutamide. No interaction was observed with omeprazole.

• Inducers of Hepatic Drug Metabolism: Blood levels of propranolol may be decreased by co-administration with inducers such as rifampin, ethanol, phenytoin, and phenobarbital. Cigarette smoking also induces hepatic metabolism and has been shown to increase up to 77% the clearance of propranolol, resulting in decreased plasma concentrations.

Cardiovascular Drugs

Antiarrhythmics

• The AUC of propafenone is increased by more than 200% by co-administration of propranolol.
• The metabolism of propranolol is reduced by co-administration of quinidine, leading to a two to three fold increased blood concentration and greater degrees of clinical beta-blockade.
• The metabolism of lidocaine is inhibited by co-administration of propranolol, resulting in a 25% increase in lidocaine concentrations.

Calcium Channel Blockers

• The mean Cmax and AUC of propranolol are increased respectively, by 50% and 30% by co-administration of nisoldipine and by 80% and 47%, by co-administration of nicardipine.
• The mean Cmax and AUC of nifedipine are increased by 64% and 79%, respectively, by co-administration of propranolol.
• Propranolol does not affect the pharmacokinetics of verapamil and norverapamil. Verapamil does not affect the pharmacokinetics of propranolol.

Non-Cardiovascular Drugs

Migraine Drugs

• Administration of zolmitriptan or rizatriptan with propranolol resulted in increased concentrations of zolmitriptan (AUC increased by 56% and Cmax by 37%) or rizatriptan (the AUC and Cmax were increased by 67% and 75%, respectively).

Theophylline

• Co-administration of theophylline with propranolol decreases theophylline oral clearance by 30% to 52%.

Benzodiazepines

• Propranolol can inhibit the metabolism of diazepam, resulting in increased concentrations of diazepam and its metabolites. Diazepam does not alter the pharmacokinetics of propranolol.
• The pharmacokinetics of oxazepam, triazolam, lorazepam, and alprazolam are not affected by co-administration of propranolol.

Neuroleptic Drugs

• Co-administration of long-acting propranolol at doses greater than or equal to 160 mg/day resulted in increased thioridazine plasma concentrations ranging from 55% to 369% and increased thioridazine metabolite (mesoridazine) concentrations ranging from 33% to 209%.
• Co-administration of chlorpromazine with propranolol resulted in a 70% increase in propranolol plasma level.

Anti-Ulcer Drugs

• Co-administration of propranolol with cimetidine, a non-specific CYP450 inhibitor, increased propranolol AUC and Cmax by 46% and 35%, respectively. Co-administration with aluminum hydroxide gel (1200 mg) may result in a decrease in propranolol concentrations.
• Co-administration of metoclopramide with the long-acting propranolol did not have a significant effect on propranolol's pharmacokinetics.

Lipid Lowering Drugs

• Co-administration of cholestyramine or colestipol with propranolol resulted in up to 50% decrease in propranolol concentrations.
• Co-administration of propranolol with lovastatin or pravastatin, decreased 18% to 23% the AUC of both, but did not alter their pharmacodynamics. Propranolol did not have an effect on the pharmacokinetics of fluvastatin.

Warfarin

• Concomitant administration of propranolol and warfarin has been shown to increase warfarin bioavailability and increase prothrombin time.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): (Description)
Pregnancy Category (AUS): (Description)

Labor and Delivery

(Description)

Nursing Mothers

(Description)

Pediatric Use

(Description)

Geriatic Use

(Description)

Gender

(Description)

Race

(Description)

Renal Impairment

(Description)

Hepatic Impairment

(Description)

Females of Reproductive Potential and Males

(Description)

Immunocompromised Patients

(Description)

Others

(Description)

Administration and Monitoring

Administration

(Oral/Intravenous/etc)

Monitoring

Condition 1

(Description regarding monitoring, from Warnings section)

Condition 2

(Description regarding monitoring, from Warnings section)

Condition 3

(Description regarding monitoring, from Warnings section)

IV Compatibility

Solution

Compatible

• Solution 1
• Solution 2
• Solution 3

Not Tested

• Solution 1
• Solution 2
• Solution 3

Variable

• Solution 1
• Solution 2
• Solution 3

Incompatible

• Solution 1
• Solution 2
• Solution 3

Y-Site

Compatible

• Solution 1
• Solution 2
• Solution 3

Not Tested

• Solution 1
• Solution 2
• Solution 3

Variable

• Solution 1
• Solution 2
• Solution 3

Incompatible

• Solution 1
• Solution 2
• Solution 3

Admixture

Compatible

• Solution 1
• Solution 2
• Solution 3

Not Tested

• Solution 1
• Solution 2
• Solution 3

Variable

• Solution 1
• Solution 2
• Solution 3

Incompatible

• Solution 1
• Solution 2
• Solution 3

Syringe

Compatible

• Solution 1
• Solution 2
• Solution 3

Not Tested

• Solution 1
• Solution 2
• Solution 3

Variable

• Solution 1
• Solution 2
• Solution 3

Incompatible

• Solution 1
• Solution 2
• Solution 3

TPN/TNA

Compatible

• Solution 1
• Solution 2
• Solution 3

Not Tested

• Solution 1
• Solution 2
• Solution 3

Variable

• Solution 1
• Solution 2
• Solution 3

Incompatible

• Solution 1
• Solution 2
• Solution 3

Overdosage

Acute Overdose

Signs and Symptoms

(Description)

Management

(Description)

Chronic Overdose

Signs and Symptoms

(Description)

Management

(Description)

Pharmacology

Propranolol (capsule)
Systematic (IUPAC) name
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Identifiers
CAS number	?
ATC code	?
PubChem	?
Chemical data
Formula	?
Mol. mass	?
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
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Mechanism of Action

(Description)

Structure

(Description with picture)

Pharmacodynamics

(Description)

Pharmacokinetics

(Description)

Nonclinical Toxicology

(Description)

Clinical Studies

Condition 1

(Description)

Condition 2

(Description)

Condition 3

(Description)

How Supplied

(Description)

Storage

There is limited information regarding Propranolol (capsule) Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

(Patient Counseling Information)

Precautions with Alcohol

Alcohol-Propranolol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Propranolol (capsule) Brand Names in the drug label.

Look-Alike Drug Names

• (Paired Confused Name 1a) — (Paired Confused Name 1b)
• (Paired Confused Name 2a) — (Paired Confused Name 2b)
• (Paired Confused Name 3a) — (Paired Confused Name 3b)

Drug Shortage Status

Drug Shortage

Price

References

The contents of this FDA label are provided by the National Library of Medicine.