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penbutolol (Levatol)

 

Classes: Beta-Blockers, Nonselective

Dosing and uses of Levatol (penbutolol)

 

Adult dosage forms and strengths

tablet

  • 20mg

 

Arterial Hypertension

Initial 10mg PO qDay (full effect after 4-6weeks)

Maintenance dose: 10-40mg PO qDay (full effect after 2 weeks)

No more than 80mg PO qDay

May admininster alone or in combination with other antihypertensive agents

 

Additional Information

Less effective than thiazide diuretics in black and geriatric patients

Shown to decrease mortality in hypertension and post-myocardial infarction

 

Pediatric dosage forms and strengths

<18 years old: Safety and efficacy not established

 

Geriatric dosage forms and strengths

Initial 10mg PO qDay (full effect after 4-6weeks)

Maintenance dose: 10-40mg PO qDay (full effect after 2 weeks)

No more than 80mg PO qDay

May admininster alone or in combination with other antihypertensive agents

 

Levatol (penbutolol) adverse (side) effects

Frequency not defined

Aggravate CHF

Depression

Fatigue

Mask symptoms of hypoglycemia

May increase triglyceride levels

Decrease HDL (less than other beta blockers)

Bronchospasm

Decreased exercise tolerance

Raynaud's phenomenon

May increase insulin resistance

 

Warnings

Contraindications

Severe peripheral vascular disease, sinus bradycardia, 2°/3° heart block, cardiogenic shock, hypersensitivity, asthma/COPD, sick sinus syndrome without permanent pacemaker

 

Cautions

IDDM, CHF, hyperthyroidism, renal impairment, liver disease

Sudden discontinuation can exacerbate angina and lead to myocardial infarction

Increased risk of stroke after surgery, cerebrovascular insufficiency, peripheral vascular disease, anesthesia/surgery (myocardial depression), use in pheochromocytoma

Anesthesia/surgery (myocardial depression): chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery, however the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and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

 

Pregnancy and lactation

Pregnancy category: C

Lactation: unknown; use with caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Levatol (penbutolol)

Mechanism of action

Beta adrenergic receptor blocker; intrinsic sympathomimetic activity (lowers BP with little decrease in HR)

 

Pharmacokinetics

Half-Life: 5 hr

Peak Plasma: 2-3 hr

Duration: >20 hr

Peak effect: 1.3-3 hr

Protein bound: 80-98%

Metabolism: Liver (oxidation and conjugation)

Excretion: Urine