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Propranolol

Class: beta-Adrenergic Blocking Agents
VA Class: CV100
CAS Number: 318-98-9
Brands: Inderal LA, Innopran XL

Medically reviewed by Drugs.com. Last updated on Feb 15, 2021.

Introduction

Nonselective β-adrenergic blocking agent (β-blocker).

Uses for Propranolol

Hypertension

Management of hypertension, alone or in combination with other antihypertensive agents. Not indicated for the treatment of hypertensive emergencies.

β-Blockers generally not preferred for first-line therapy of hypertension according to current evidence-based hypertension guidelines, 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). Propranolol is one of several β-blockers (including bisoprolol, carvedilol, metoprolol succinate, metoprolol tartrate, nadolol, and timolol) recommended by a 2017 ACC/AHA multidisciplinary hypertension guideline as first-line therapy for hypertension in patients with stable ischemic heart disease/angina.

Individualize choice of therapy; consider patient characteristics (e.g., age, ethnicity/race, comorbidities, cardiovascular risk) as well as drug-related factors (e.g., ease of administration, availability, adverse effects, cost).

The 2017 ACC/AHA hypertension guideline classifies BP in adults into 4 categories: normal, elevated, stage 1 hypertension, and stage 2 hypertension. (See Table 1.)

Source: Whelton PK, Carey RM, Aronow WS et al. 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA guideline for the prevention, detection, evaluation, and management of high blood pressure in adults: a report of the American College of Cardiology/American Heart Association Task Force on Clinical Practice Guidelines. Hypertension. 2018;71:e13-115.

Individuals with SBP and DBP in 2 different categories (e.g., elevated SBP and normal DBP) should be designated as being in the higher BP category (i.e., elevated BP).

Table 1. ACC/AHA BP Classification in Adults1200

Category

SBP (mm Hg)

DBP (mm Hg)

Normal

<120

and

<80

Elevated

120–129

and

<80

Hypertension, Stage 1

130–139

or

80–89

Hypertension, Stage 2

≥140

or

≥90

The goal of hypertension management and prevention is to achieve and maintain optimal control of BP. However, the BP thresholds used to define hypertension, the optimum BP threshold at which to initiate antihypertensive drug therapy, and the ideal target BP values remain controversial.

The 2017 ACC/AHA hypertension guideline generally recommends a target BP goal (i.e., BP to achieve with drug therapy and/or nonpharmacologic intervention) <130/80 mm Hg in all adults regardless of comorbidities or level of atherosclerotic cardiovascular disease (ASCVD) risk. In addition, an SBP goal of <130 mm Hg generally is recommended for noninstitutionalized ambulatory patients ≥65 years of age with an average SBP of ≥130 mm Hg. These BP goals are based upon clinical studies demonstrating continuing reduction of cardiovascular risk at progressively lower levels of SBP.

Other hypertension guidelines generally have based target BP goals on age and comorbidities. Guidelines such as those issued by the JNC 8 expert panel generally have targeted a BP goal of <140/90 mm Hg regardless of cardiovascular risk and have used higher BP thresholds and target BPs in elderly patients compared with those recommended by the 2017 ACC/AHA hypertension guideline.

Some clinicians continue to support previous target BPs recommended by JNC 8 due to concerns about the lack of generalizability of data from some clinical trials (e.g., SPRINT study) used to support the 2017 ACC/AHA hypertension guideline and potential harms (e.g., adverse drug effects, costs of therapy) versus benefits of BP lowering in patients at lower risk of cardiovascular disease.

Consider potential benefits of hypertension management and drug cost, adverse effects, and risks associated with the use of multiple antihypertensive drugs when deciding a patient's BP treatment goal.

For decisions regarding when to initiate drug therapy (BP threshold), the 2017 ACC/AHA hypertension guideline incorporates underlying cardiovascular risk factors. ASCVD risk assessment is recommended by ACC/AHA for all adults with hypertension.

ACC/AHA currently recommend initiation of antihypertensive drug therapy in addition to lifestyle/behavioral modifications at an SBP ≥140 mm Hg or DBP ≥90 mm Hg in adults who have no history of cardiovascular disease (i.e., primary prevention) and a low ASCVD risk (10-year risk <10%).

For secondary prevention in adults with known cardiovascular disease or for primary prevention in those at higher risk for ASCVD (10-year risk ≥10%), ACC/AHA recommend initiation of antihypertensive drug therapy at a BP of ≥130/80 mm Hg.

Adults with hypertension and diabetes mellitus, chronic kidney disease (CKD), or age ≥65 years are assumed to be at high risk for cardiovascular disease; ACC/AHA state that such patients should have antihypertensive drug therapy initiated at a BP ≥130/80 mm Hg. Individualize drug therapy in patients with hypertension and underlying cardiovascular or other risk factors.

In stage 1 hypertension, experts state that it is reasonable to initiate drug therapy using the stepped-care approach in which one drug is initiated and titrated and other drugs are added sequentially to achieve the target BP. Initiation of antihypertensive therapy with 2 first-line agents from different pharmacologic classes recommended in adults with stage 2 hypertension and average BP >20/10 mm Hg above BP goal.

Black hypertensive patients generally tend to respond better to monotherapy with calcium-channel blockers or thiazide diuretics than to β-blockers. However, diminished response to β-blockers is largely eliminated when administered concomitantly with a thiazide diuretic.

Chronic Stable Angina

Long-term management of chronic stable angina pectoris.

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.

Supraventricular Arrhythmias

Treatment of supraventricular tachycardia (SVT) (e.g., atrial flutter, junctional tachycardia, focal atrial tachycardia, paroxysmal supraventricular tachycardia [PSVT]).

Vagal maneuvers and/or IV adenosine are considered first-line interventions for acute treatment of SVT when clinically indicated; if such measures are ineffective or not feasible, may consider an IV β-blocker. Oral β-blockers may be used for ongoing management. Although evidence of efficacy is limited, experts state that overall safety of β-blockers warrants use.

Used to slow ventricular rate in patients with atrial fibrillation or flutter when ventricular rate cannot be controlled by standard measures.

Ventricular Arrhythmias

Generally less effective in the management of ventricular arrhythmias than supraventricular arrhythmias, but may be considered when cardioversion or other drugs not effective.

May be used in the treatment of persistent premature ventricular complexes.

β-Blockers have been used in patients with cardiac arrest precipitated by ventricular fibrillation or pulseless VT; however, routine administration after cardiac arrest is potentially harmful and not recommended.

β-Blockers may be useful in the management of certain forms of polymorphic VT (e.g., associated with acute ischemia).

Tachyarrhythmias Associated with Cardiac Glycoside Intoxication or Catecholamine Excess

Management of supraventricular or ventricular tachyarrhythmias associated with cardiac glycoside toxicity when AV block is not present.

Management of resistant tachyarrhythmias associated with catecholamine excess during anesthesia; use with extreme caution and constant ECG and central venous pressure monitoring. More effective and less hazardous therapy, such as lessening the depth of anesthesia or improving ventilation, is preferred.

Hypertrophic Subaortic Stenosis

Management of exertional or other stress-induced angina, vertigo, syncope, and palpitation in patients with hypertrophic subaortic stenosis; clinical improvement may be temporary.

Pheochromocytoma

Management of symptoms resulting from excessive β-receptor stimulation in patients with inoperable or metastatic pheochromocytoma, as an adjunct to α-adrenergic blocking agents. Initiate therapy with an α-adrenergic blocking agent prior to treatment of pheochromocytoma. (See Pheochromocytoma under Cautions.)

Management of tachycardia prior to or during surgery in patients with pheochromocytoma, as an adjunct to α-adrenergic blocking agents. Initiate therapy with an α-adrenergic blocking agent prior to treatment of pheochromocytoma. (See Pheochromocytoma under Cautions.)

Thyrotoxicosis

Short-term (2–4 weeks) adjunctive therapy of tachycardia and supraventricular arrhythmias in patients with thyrotoxicosis when these symptoms are distressful or hazardous, or when immediate therapy is necessary.

Vascular Headache

Prophylaxis of common migraine headache; not recommended for the treatment of a migraine attack that has already started.

MI

Secondary prevention following acute MI to reduce the risk of cardiovascular mortality.

Administration within 5–21 days following MI associated with reductions in overall and cardiovascular mortality.

Experts recommend β-blocker therapy in all patients with left ventricular systolic dysfunction and prior MI; a β-blocker with proven mortality benefit (bisoprolol, carvedilol, or metoprolol succinate) is preferred. Although benefits of long-term β-blockade in patients with normal left ventricular function are less well established, experts recommend continued β-blocker therapy for at least 3 years in such patients.

Essential Tremor

Management of essential (familial, hereditary) tremor.

Not indicated for tremor associated with Parkinsonism.

Propranolol Dosage and Administration

General

BP Monitoring and Treatment Goals

  • Monitor BP regularly (i.e., monthly) during therapy and adjust dosage of the antihypertensive drug until BP controlled.

  • If unacceptable adverse effects occur, discontinue drug and initiate another antihypertensive agent from a different pharmacologic class.

  • If adequate BP response not achieved with a single antihypertensive agent, either increase dosage of single drug or add a second drug with demonstrated benefit and preferably a complementary mechanism of action (e.g., ACE inhibitor, angiotensin II receptor antagonist, calcium-channel blocker, thiazide diuretic). Many patients will require ≥2 drugs from different pharmacologic classes to achieve BP goal; if goal BP still not achieved, add a third drug.

Administration

Administer orally or IV.

Individualize dosage according to patient response.

Oral Administration

Administer conventional tablets in divided doses before meals and at bedtime.

Administer extended-release capsules once daily.

Extended-release capsules produce lower blood concentrations than conventional tablets; do not substitute on a mg-for-mg basis. Consider dosage retitration when switching from conventional tablets to extended-release capsules, especially to maintain effectiveness at the end of the dosing interval.

Dilute oral concentrate solution with water, juice, or carbonated beverages or mix with semisolid foods (e.g., applesauce, puddings) just prior to administration.

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Monitor ECG and central venous pressure carefully during IV administration.

Replace IV therapy with oral therapy as soon as possible.

Rate of Administration

Administer by slow IV injection at a rate not >1 mg/minute.

Dosage

Available as propranolol hydrochloride; dosage expressed in terms of the salt.

If long-term therapy is to be discontinued, reduce dosage gradually over a period of about 2 weeks. (See Abrupt Withdrawal of Therapy under Cautions.)

Pediatric Patients

Hypertension
Oral

Some experts have recommended an initial dosage of 1–2 mg/kg daily given in 2 or 3 divided doses as an immediate-release formulation. Increase dosage as necessary up to a maximum dosage of 4 mg/kg (up to 640 mg) daily given in 2 or 3 divided doses.

Extended-release formulation may be administered once daily.

Cardiac Arrhythmias
Oral

Initially, 1.5–2 mg/kg daily; titrate upward as necessary to 16 mg/kg daily in 4 divided doses to control the arrhythmia.

Dosages >4 mg/kg daily may be necessary for the management of supraventricular tachyarrhythmias.

IV

10–20 mcg/kg infused over 10 minutes has been recommended.

Thyrotoxicosis
Treatment of Tachyarrhythmias in Neonates with Thyrotoxicosis
Oral

2 mg/kg daily in 2–4 divided doses has been used. Higher dosages occasionally may be needed.

Adults

Hypertension
Propranolol Therapy
Oral

Conventional tablets or oral solution: Initially, 40 mg twice daily, either alone or in combination with a diuretic. Manufacturers state usual effective dosage is 120–240 mg daily. Some experts state usual dosage range is 80–160 mg daily, given in 2 divided doses. If satisfactory BP response is not maintained throughout the day, larger doses or administration in 3 divided doses daily may be required.

Extended-release capsules: Initially, 80 mg once daily, either alone or in combination with a diuretic. Manufacturers state usual effective dosage is 120–160 mg once daily. Some experts state usual dosage range is 80–160 mg once daily. However, manufacturer of Innopran XL states that dosages >120 mg once daily do not provide additional hypotensive effects.

Full hypotensive effect usually evident within 2–3 weeks, but timing is variable.

Propranolol/Hydrochlorothiazide Fixed-combination Therapy
Oral

Administer in 2 divided doses daily (up to 160 mg of propranolol hydrochloride and 50 mg of hydrochlorothiazide total daily dosage).

Combination preparation is inappropriate with propranolol hydrochloride dosages >160 mg daily due to excessive dosage of the thiazide component. May gradually add another antihypertensive agent when necessary using half of the usual initial dosage to avoid an excessive decrease in BP.

Initial use of fixed-combination preparations is not recommended; adjust by administering each drug separately, then use the fixed combination if the optimum maintenance dosage corresponds to the drug dosages in the combination preparation.

Chronic Stable Angina
Oral

Conventional tablets or oral solution: Usual dosage is 80–320 mg daily in 2–4 divided doses. Dosages exceeding 320 mg daily have been recommended when there is only a partial response to usual dosage.

Extended-release capsules: Initially, 80 mg daily. Gradually increase dosage at 3- to 7-day intervals as needed to control symptoms. Optimum response usually occurs at 160 mg daily, but there is wide variation in response.

Periodically reevaluate chronic therapy for angina to determine need for dosage adjustment or continued therapy.

Cardiac Arrhythmias
Oral

Conventional tablets or oral solution: usually 10–30 mg 3 or 4 times daily.

Life-threatening Arrhythmias or Those Occurring during Anesthesia
IV

1–3 mg by slow IV injection. If necessary, repeat dose after 2 minutes. May administer additional doses at intervals of ≥4 hours until desired response is obtained.

SVT (e.g., Atrial Flutter, Junctional Tachycardia, PSVT, Atrial Tachycardia)
IV

Some experts recommend initial dose of 1 mg over 1 minute; may repeat at 2-minute intervals up to 3 doses.

Oral

Usual maintenance dosage: 40–160 mg daily in single (with long-acting preparations) or divided doses.

Atrial Fibrillation
IV

Experts recommend initial dose of 1 mg over 1 minute; may repeat at 2-minute intervals up to 3 doses.

Oral

Usual maintenance dosage: 40–160 mg daily in divided doses.

Hypertrophic Subaortic Stenosis
Oral

Conventional tablets or oral solution: 20–40 mg 3 or 4 times daily.

Extended-release capsules: 80–160 mg once daily.

Pheochromocytoma
Prior to Surgery
Oral

Conventional tablets or oral solution: 60 mg daily in divided doses (in conjunction with an α-adrenergic blocking agent) for 3 days prior to surgery. (See Pheochromocytoma under Cautions.)

Adjunctive Treatment for Inoperable Pheochromocytoma.
Oral

30 mg daily in divided doses (in conjunction with an α-adrenergic blocker). (See Pheochromocytoma under Cautions.)

Vascular Headache
Prevention of Common Migraine
Oral

Conventional tablets or oral solution: initially, 80 mg daily in divided doses.

Extended-release capsules: 80 mg once daily.

Gradually increase dosage to achieve optimum response; usual effective dosage is 80–240 mg daily.

Discontinue if response is inadequate after 4–6 weeks; gradual withdrawal over several weeks may be advisable.

MI
Mortality Reduction after Acute MI
Oral

Conventional tablets or oral solution: 180–240 mg daily in divided doses; in the study demonstrating mortality benefit with propranolol, the drug was initiated 5–21 days after infarction. Higher dosage may be necessary for patients with coexisting conditions (e.g., angina, hypertension).

Administered in 3–4 divided doses daily in clinical studies, but twice-daily dosing also may be adequate.

Optimal duration of therapy for secondary prevention remains to be clearly established. Experts generally recommend long-term therapy in post-MI patients with left ventricular systolic dysfunction, and at least 3 years of therapy in those with normal left ventricular function.

Essential Tremor
Routine Therapy
Oral

Conventional tablets: Initially, 40 mg twice daily.

Response is variable and dosage must be individualized; optimal suppression of tremor usually occurs with 120–320 mg daily in 3 divided doses.

Complete suppression of tremor rarely is achieved; dosages exceeding 320 mg daily may not provide substantial added benefit but are associated with an increased risk of adverse effects.

Extended-release capsules: Usual dosages administered once daily each morning appear to be at least as effective as equivalent dosages of conventional tablets administered in divided doses daily.

Intermittent Therapy
Oral

Conventional tablets: 80–120 mg as a single dose 1–3 hours before planned activity or anticipated stress associated with tremor.

Prescribing Limits

Pediatric Patients

Hypertension
Oral

Some experts have recommended a maximum dosage of 4 mg/kg (up to 640 mg) daily.

Adults

Chronic Stable Angina
Oral

320 mg daily; some clinicians recommend higher dosage if there is only a partial response to usual dosage.

MI
Oral

240 mg daily.

Essential Tremor
Oral

320 mg daily; higher dosages do not provide substantial added benefit and are associated with an increased risk of adverse effects.

Special Populations

Hepatic Impairment

Use with caution.

Renal Impairment

Dosage adjustments not required. Use with caution.

Geriatric Patients

Use caution in dosage selection; initiate therapy at low end of dosage range.

Cautions for Propranolol

Contraindications

  • Sinus bradycardia.

  • Heart block greater than first degree.

  • Cardiogenic shock.

  • CHF (unless secondary to a tachyarrhythmia treatable with propranolol). (See Heart Failure under Cautions.)

  • Raynaud’s syndrome.

  • Malignant hypertension.

  • Bronchial asthma. (See Bronchospastic Disease under Cautions.)

  • Concomitant thioridazine therapy. (See Specific Drugs under Interactions.)

Warnings/Precautions

Warnings

Heart Failure

Possible precipitation of heart failure.

Avoid use in patients with overt heart failure; may use cautiously in patients with inadequate myocardial function and, if necessary, in patients with well-compensated heart failure (e.g., those controlled with heart glycosides and/or diuretics). Adequate treatment (e.g., with a cardiac glycoside and/or diuretic) and close observation recommended if signs or symptoms of impending heart failure occur; if heart failure continues, discontinue therapy, gradually if possible.

Possible decreased exercise tolerance in patients with left ventricular dysfunction.

Abrupt Withdrawal of Therapy

Abrupt withdrawal of propranolol is not recommended as it may exacerbate angina symptoms or precipitate MI in patients with CAD. Gradually decrease dosage over about 2 weeks and monitor patients carefully. 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.

Bronchospastic Disease

Possible inhibition of bronchodilation produced by endogenous catecholamines. Possible increased airway resistance and bronchospasm, particularly in patients with a history of asthma.

Use with caution in patients with a history of nonallergic bronchospasm (e.g., chronic bronchitis, emphysema). Use not recommended in patients with bronchial asthma. (See Contraindications under Cautions.)

Major Surgery

Possible increased risks associated with general anesthesia (e.g., severe hypotension, difficulty restarting or maintaining heart beat) due to decreased ability of the heart to respond to reflex β-adrenergic stimuli. Use with extreme caution for management of arrhythmias occurring during anesthesia with myocardial depressant anesthetics.

Diabetes and Hypoglycemia

Possible decreased signs and symptoms of hypoglycemia (e.g., tachycardia, palpitation, BP changes, tremor). Possible hypoglycemia, especially in those undergoing dialysis, prolonged fasting, or severe exercise regimens.

Use with caution in patients with diabetes mellitus.

Thyrotoxicosis

Signs of hyperthyroidism may be masked. Possible thyroid storm if therapy is abruptly withdrawn; carefully monitor patients having or suspected of developing thyrotoxicosis. Possible altered thyroid function test results.

Bradycardia

Possible bradycardia, occasionally severe and accompanied by hypotension, syncope, shock, or angina. Severe bradycardia requiring a demand pacemaker has occurred in patients with Wolff-Parkinson-White syndrome. Treat severe bradycardia with IM or IV atropine sulfate. If response is inadequate, consider cautious administration of IV isoproterenol.

Possible depressed SA node automaticity; use with caution in patients with sinus node dysfunction.

AV Block

Possible intensification of AV block, AV dissociation, AV conduction delays, complete heart block, or cardiac arrest, especially in patients with preexisting heart block caused by digitalis or other factors.

Pheochromocytoma

To prevent severe hypertension, institute α-adrenergic blocking agent therapy prior to the use of propranolol and continue during propranolol therapy.

General Precautions

History of Anaphylactic Reactions

Possible increased reactivity to a variety of allergens; patients may be unresponsive to usual doses of epinephrine used to treat anaphylactic reactions.

Ocular Effects

May reduce IOP; may interfere with glaucoma screening tests. IOP may increase upon drug withdrawal.

Myasthenia Gravis

Myasthenic condition (e.g., ptosis, weakness of limbs, and double vision) reported rarely with propranolol; use may be contraindicated in patients with myasthenia gravis.

Other Precautions

Shares the toxic potentials of β-blockers; observe usual precautions of these agents.

When used in fixed combination with hydrochlorothiazide, consider the cautions, precautions, and contraindications associated with thiazide diuretics.

Specific Populations

Pregnancy

Category C.

Lactation

Distributed into milk. Use with caution.

Pediatric Use

Efficacy and adverse effect profiles in children generally similar to such profiles in adults. Bioavailability may be increased in children with Down’s syndrome. Safety and efficacy of extended-release capsules, oral solution, and injection not established in children.

Geriatric Use

Insufficient evidence in patients ≥65 years of age to determine whether geriatric patients respond differently than younger patients. Select dosage with caution, usually initiating therapy at the low end of the dosage range because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.

Hepatic Impairment

Use with caution; assess hepatic function prior to and periodically during prolonged therapy.

Renal Impairment

Use with caution; assess renal function prior to and periodically during prolonged therapy.

Common Adverse Effects

Bradycardia, nausea, vomiting, diarrhea, epigastric distress, abdominal cramping, constipation, flatulence.

Interactions for Propranolol

Specific Drugs

Drug

Interaction

Comments

Antipsychotic agents (e.g., phenothiazines)

Possible additive hypotensive effect, especially with large doses of phenothiazines

Chlorpromazine

Possible decreased propranolol clearance

Thioridazine

Possible decreased thioridazine metabolism.

Possible increased risk of serious, potentially fatal cardiac arrhythmias (e.g., torsades de pointes)

Concomitant use contraindicated

Haloperidol

Possible hypotension and cardiac arrest

Fluoxetine

Possible decreased propranolol metabolism; complete heart block reported

Caution recommended with concomitant use and in those with impaired cardiac conduction

Sympathomimetic agents

Possible antagonism of β-adrenergic stimulating effects; very large doses of isoproterenol may be needed to overcome β-adrenergic blocking effects

Administer epinephrine with caution; decreased pulse rate with first- and second-degree heart block may occur

Drugs with anticholinergic effects

Possible antagonism of cardiac β-adrenergic blocking effects

Diuretics

Possible increased hypotensive effect

Careful dosage adjustments recommended

Reserpine

Possible additive effects

Antiarrhythmic drugs (lidocaine, phenytoin, procainamide, quinidine, verapamil)

Possible additive or antagonistic cardiac effects and additive toxic effects

Verapamil

Serious adverse reactions reported rarely with concomitant IV verapamil, especially in patients with severe cardiomyopathy, CHF, or recent MI

Other cardiovascular drugs (e.g., cardiac glycosides, nondihydropyridine calcium-channel blocking agents)

Possible additive negative effects on SA or AV nodal conduction

Neuromuscular blocking agents

Possible increased effects of neuromuscular blocking agents

Administer with caution to patients receiving or recovering from the effects of neuromuscular blocking agents

Antidiabetic agents

Possible altered antidiabetic response

Close monitoring recommended

Ergot alkaloids

Possible additive peripheral vasoconstriction

Use concomitantly with caution

Cimetidine

Possible decreased propranolol clearance

Monitor for signs and symptoms of increased β-adrenergic blocking activity

Antacids

Possible decreased propranolol absorption

Need to avoid concomitant use or stagger dosing of an aluminum hydroxide antacid has not been fully elucidated; consider increasing propranolol dosage if interaction suspected

Levodopa

Possible decreased hypotensive and positive inotropic effects of levodopa

NSAIAs

Possible decreased hypotensive effects of propranolol

Theophylline

Possible decreased theophylline clearance.

Possible decreased theophylline-induced bronchodilation

Propranolol Pharmacokinetics

Absorption

Bioavailability

Oral absorption almost complete.

Bioavailabilities of conventional tablet and oral solution reportedly equivalent in adults.

Oral bioavailability may be increased in children with Down’s syndrome.

Onset

Conventional oral tablets: peak effect in 1–1.5 hours.

Plasma Concentrations

100–150 ng/mL with considerable interpatient variation; 100 ng/mL generally represents high degree of β-blockade.

Distribution

Extent

Widely distributed into body tissues, including lungs, liver, kidneys, and heart. Portion of orally administered dose immediately bound by liver.

Crosses blood-brain barrier.

Crosses placenta and is distributed into milk.

Plasma Protein Binding

>90% over a wide range of blood concentrations.

Elimination

Metabolism

Almost completely metabolized in the liver.

Elimination Route

Excreted principally in urine; at least 8 metabolites have been identified.

1–4% of an oral or IV dose of the drug appears in feces as unchanged drug and metabolites.

Half-life

IV: 10 minutes (initial phase), 2.3 hours (terminal phase).

Conventional oral tablets: about 4 hours.

3.4–6 hours with chronic administration of usual therapeutic doses; 2–3 hours after single dose.

Extended-release capsules: apparent half-life about 10 hours.

Special Populations

In patients with severely impaired renal function, a compensatory increase in fecal excretion of propranolol occurs. Propranolol apparently not substantially removed by hemodialysis.

Stability

Storage

Oral

Capsules

Tight, light-resistant containers at 20–25°C; protect from moisture, freezing or excessive heat.

Tablets

10, 60, and 80 mg: Tight containers at 20–25°C.

20 and 40 mg: Tight, light-resistant containers at 20–25°C.

Tablets (Propranolol Hydrochloride and Hydrochlorothiazide)

Tight containers at about 25°C; protect from moisture, freezing or excessive heat.

Solution and Solution Concentrate

Tight, light-resistant containers at 20–25°C.

Maximum stability at pH 3, rapidly decomposes at alkaline pH.

Decomposition in aqueous solution is accompanied by lowered pH and discoloration.

Parenteral

Injection

20–25°C; Protect from freezing or excessive heat.

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution CompatibilityHID

Compatible

Dextrose 5% in sodium chloride 0.45 or 0.9%

Dextrose 5% in water

Ringer’s injection, lactated

Sodium chloride 0.45 or 0.9%

Drug Compatibility
Admixture CompatibilityHID

Compatible

Dobutamine HCl

Verapamil HCl

Y-Site CompatibilityHID

Compatible

Alteplase

Fenoldopam mesylate

Heparin sodium

Hydrocortisone sodium succinate

Linezolid

Meperidine HCl

Milrinone lactate

Morphine sulfate

Nesiritide

Potassium chloride

Propofol

Tacrolimus

Tirofiban HCl

Incompatible

Amphotericin B cholesteryl sulfate complex

Actions

  • Inhibits response to adrenergic stimuli by competitively blocking β-adrenergic receptors within the myocardium and within bronchial and vascular smooth muscle; no intrinsic sympathomimetic activity.

  • Decreases resting and exercise-stimulated heart rate, myocardial contractility, and cardiac output; increases systolic ejection time and cardiac volume; decreases conduction velocity through the sinoatrial (SA) and atrioventricular (AV) nodes; and decreases myocardial automaticity.

  • Initially increases peripheral resistance; however, peripheral resistance decreases with chronic administration.

  • Decreases renal blood flow, glomerular filtration rate, and hepatic blood flow.

  • Membrane-stabilizing effect on the heart occurs at high dosages.

  • Reduces BP by decreasing cardiac output, decreasing sympathetic outflow from the CNS, and/or by suppressing renin release.

  • Reduces the frequency of anginal attacks and increases exercise tolerance by decreasing myocardial oxygen consumption and coronary blood flow. May reduce myocardial oxygen requirements.

  • Exact mechanism of antimigraine effect not known. β-Adrenergic receptors present in pial vessels of brain. Some evidence suggests propranolol may prevent migraines through diminishing central catecholaminergic hyperactivity, possibly by inhibiting norepinephrine release, reducing neuronal activity and excitability, exerting membrane-stabilizing effects, and inhibiting nitric oxide production.

  • Increases airway resistance (especially in asthmatic patients), inhibits glycogenolysis in the skeletal and cardiac muscles, blocks the release of free fatty acids and insulin, increases the number of circulating eosinophils, and increases uterine activity.

Advice to Patients

  • Importance of taking medication exactly as prescribed.

  • Importance of not interrupting or discontinuing therapy without consulting clinician; importance of temporarily limiting physical activity when discontinuing therapy.

  • Importance of immediately informing clinician at the first sign or symptom of impending cardiac failure or if any difficulty in breathing occurs.

  • Importance of patient informing anesthesiologist or dentist about propranolol therapy before undergoing major surgery.

  • Importance of informing patients that propranolol may interfere with glaucoma screening test.

  • Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

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

Propranolol Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules, extended-release

60 mg

Inderal LA

Ani Pharms

80 mg

Inderal LA

Ani Pharms

Innopran XL

Ani Pharms

120 mg

Inderal LA

Ani Pharms

Innopran XL

Ani Pharms

160 mg

Inderal LA

Ani Pharms

Solution

20 mg/5 mL*

Propranolol Hydrochloride Solution

40 mg/5 mL*

Propranolol Hydrochloride Solution

Tablets

10 mg*

Propranolol Hydrochloride Tablets

20 mg*

Propranolol Hydrochloride Tablets

40 mg*

Propranolol Hydrochloride Tablets

60 mg*

Propranolol Hydrochloride Tablets

80 mg*

Propranolol Hydrochloride Tablets

Parenteral

Injection

1 mg/mL*

Propranolol Hydrochloride Injection

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Propranolol Hydrochloride and Hydrochlorothiazide

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

40 mg Propranolol Hydrochloride and Hydrochlorothiazide 25 mg*

Propranolol Hydrochloride and hydroCHLOROthiazide Tablets

80 mg Propranolol Hydrochloride and Hydrochlorothiazide 25 mg*

Propranolol Hydrochloride and hydroCHLOROthiazide Tablets

AHFS DI Essentials™. © Copyright 2021, Selected Revisions February 25, 2019. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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