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Pronunciation |
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(pen
BYOO toe
lole) |
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U.S. Brand
Names |
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Levatol® |
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Generic
Available |
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No |
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Synonyms |
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Penbutolol Sulfate |
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Pharmacological Index |
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Beta Blocker (with Intrinsic Sympathomimetic Activity) |
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Use |
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Treatment of mild to moderate arterial hypertension |
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Pregnancy Risk
Factor |
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C (per manufacturer); D (in 2nd and 3rd trimester, per expert
analysis) |
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Contraindications |
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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) |
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Warnings/Precautions |
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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. |
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Adverse
Reactions |
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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 |
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Overdosage/Toxicology |
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Enhancement of elimination: Charcoal hemoperfusion can be used to lower serum
levels. Treatment is symptom directed and supportive. |
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Drug
Interactions |
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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. |
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Mechanism of
Action |
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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 |
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Pharmacodynamics/Kinetics |
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Absorption: Well absorbed, ~100%
Half-life: 5 hours |
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Usual Dosage |
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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 |
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Cardiovascular
Considerations |
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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.
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Mental Health: Effects
on Mental Status |
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May cause dizziness or depression; may rarely cause insomnia, confusion, or
nightmares |
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Mental Health:
Effects on Psychiatric
Treatment |
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Concurrent use with phenothiazines may potentiate hypotensive effects of
penbutolol |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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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. |
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Nursing
Implications |
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Advise against abrupt withdrawal
Monitor orthostatic blood pressures, apical and peripheral pulse and mental
status changes (ie, confusion, depression) |
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Dosage Forms |
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Tablet, as sulfate: 20 mg |
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