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Look Up > Drugs > Penbutolol
Penbutolol
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Cardiovascular Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms

Pronunciation
(pen BYOO toe lole)

U.S. Brand Names
Levatol®

Generic Available

No


Synonyms
Penbutolol Sulfate

Pharmacological Index

Beta Blocker (with Intrinsic Sympathomimetic Activity)


Use

Treatment of mild to moderate arterial hypertension


Pregnancy Risk Factor

C (per manufacturer); D (in 2nd and 3rd trimester, per expert analysis)


Contraindications

Hypersensitivity to penbutolol; uncompensated congestive heart failure; cardiogenic shock; bradycardia or heart block (except in patients with a functioning artificial pacemaker); sinus node dysfunction; asthma; bronchospastic disease; COPD; pulmonary edema; pregnancy (2nd and 3rd trimester)


Warnings/Precautions

Avoid abrupt discontinuation in patients with a history of CAD; slowly wean while monitoring for signs and symptoms of ischemia. Use caution with concurrent use of beta-blockers and either verapamil or diltiazem; bradycardia or heart block can occur. Use caution in patients with PVD (can aggravate arterial insufficiency). Use cautiously in diabetics because it can mask prominent hypoglycemic symptoms. Can mask signs of thyrotoxicosis. Can cause fetal harm when administered in pregnancy. Use cautiously in the renally impaired (dosage adjustment required). Use care with anesthetic agents which decrease myocardial function. Beta-blockers with intrinsic sympathomimetic activity (including penbutolol) do not appear to be of benefit in congestive heart failure.


Adverse Reactions

1% to 10%:

Cardiovascular: Congestive heart failure, arrhythmia

Central nervous system: Mental depression, headache, dizziness, fatigue

Gastrointestinal: Nausea, diarrhea, dyspepsia

Neuromuscular & skeletal: Arthralgia

<1% (Limited to important or life-threatening symptoms): Bradycardia, mesenteric arterial thrombosis, A-V block, persistent bradycardia, hypotension, edema, Raynaud's phenomena, cold extremities, insomnia, lethargy, nightmares, confusion, purpura, hypoglycemia, ischemic colitis, thrombocytopenia, bronchospasm, cough


Overdosage/Toxicology

Enhancement of elimination: Charcoal hemoperfusion can be used to lower serum levels. Treatment is symptom directed and supportive.


Drug Interactions

Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.

Albuterol (and other beta2 agonists): Effects may be blunted by nonspecific beta-blockers.

Clonidine: Hypertensive crisis after or during withdrawal of either agent.

Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.

Epinephrine (including local anesthetics with epinephrine): Penbutolol may cause hypertension.

Glucagon: Penbutolol may blunt the hyperglycemic action.

Insulin and oral hypoglycemics: May mask symptoms of hypoglycemia.

NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.

Penbutolol masks the tachycardia that usually accompanies insulin-induced hypoglycemia.

Salicylates may reduce the antihypertensive effects of beta-blockers.

Sulfonylureas: beta-blockers may alter response to hypoglycemic agents.

Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.


Mechanism of Action

Blocks both beta1- and beta2-receptors and has mild intrinsic sympathomimetic activity; has negative inotropic and chronotropic effects and can significantly slow A-V nodal conduction


Pharmacodynamics/Kinetics

Absorption: Well absorbed, ~100%

Half-life: 5 hours


Usual Dosage

Adults: Oral: Initial: 20 mg once daily, full effect of a 20 or 40 mg dose is seen by the end of a 2-week period, doses of 40-80 mg have been tolerated but have shown little additional antihypertensive effects


Cardiovascular Considerations

This drug possesses intrinsic sympathomimetic activity. While beta-blockers with intrinsic sympathomimetic activity induce fewer side effects, the cardiovascular benefits when used in patients with hypertension or heart failure are less clear than for beta-blockers without intrinsic sympathomimetic activity.

Surgery: Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction.

Angina: Beta-blockers are effective in the treatment of angina as monotherapy or when combined with nitrates and/or calcium channel blockers. In patients with severe intractable angina requiring negative cardiac chronotropic medications, pacemaker placement has been carried out to maintain heart rate in the setting of large doses of beta-blockers and/or calcium channel blockers. Beta-blockers are ineffective in the treatment of pure vasospastic (Prinzmetal) angina.

Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.


Mental Health: Effects on Mental Status

May cause dizziness or depression; may rarely cause insomnia, confusion, or nightmares


Mental Health: Effects on Psychiatric Treatment

Concurrent use with phenothiazines may potentiate hypotensive effects of penbutolol


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Take exactly as directed. Do not increase, decrease, or adjust dosage without consulting prescriber. Take pulse daily, prior to medication and follow prescriber's instruction about holding medication. Do not take with antacids. Do not use alcohol or OTC medications (eg, cold remedies) without consulting prescriber. If diabetic, monitor serum sugars closely (may alter glucose tolerance or mask signs of hypoglycemia). May cause fatigue, dizziness, or postural hypotension; use caution when changing position from lying or sitting to standing, when driving, or when climbing stairs until response to medication is known. May cause alteration in sexual performance (reversible). Report unresolved swelling of extremities, difficulty breathing or new cough, unresolved fatigue, unusual weight gain, unresolved constipation, or unusual muscle weakness. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.


Nursing Implications

Advise against abrupt withdrawal

Monitor orthostatic blood pressures, apical and peripheral pulse and mental status changes (ie, confusion, depression)


Dosage Forms

Tablet, as sulfate: 20 mg


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