Penbutolol Brand Name– Levatol
What is Penbutolol
Penbutolol is a nonselective beta-blocker and is available as an oral formulation indicated for hypertension.
Due to its high lipid solubility, penbutolol undergoes extensive hepatic metabolism and has a higher potential for inducing CNS side effects relative to less lipid-soluble beta-blockers.
Penbutolol has low intrinsic sympathomimetic activity (ISA) and lacks membrane-stabilizing activity (MSA). The beta blocking potency of penbutolol is approximately 4 times that of propranolol.
The 2007 AHA guidelines for the management of hypertension state beta-blockers should not be used as first-line therapy for the treatment of hypertension, as several comparative clinical trials have shown beta blockers to be inferior to ACE inhibitors, angiotensin-receptor blockers, or calcium channel blockers for preventing both stroke and coronary artery disease complications. These guidelines do, however, recommend the use of beta-blockers for the treatment of hypertension in patients with angina, prior myocardial infarction, or heart failure.
Penbutolol was approved by the FDA in 1987.
Indications
- angina
- hypertension
Side Effects
- agranulocytosis
- alopecia
- amnesia
- asthenia
- AV block
- bradycardia
- bronchospasm
- chest pain (unspecified)
- colitis
- confusion
- cough
- depression
- diabetes mellitus
- diaphoresis
- diarrhea
- dizziness
- dyspepsia
- dyspnea
- emotional lability
- erythema
- fatigue
- headache
- heart failure
- hyperglycemia
- hypertension
- hypoglycemia
- hypotension
- impotence (erectile dysfunction)
- insomnia
- laryngospasm
- nausea
- palpitations
- purpura
- rash
- sinus tachycardia
- throat irritation
- thrombosis
- thrombotic thrombocytopenic purpura (TTP)
- tremor
- withdrawal
Limb pain was reported in 2.4% of penbutolol-treated patients compared to 1.4% of placebo-treated patients in controlled clinical trials of penbutolol.
Monitoring Parameters
- blood pressure
- heart rate
- serum creatinine/BUN
Contraindications
- abrupt discontinuation
- acute bronchospasm
- asthma
- AV block
- bradycardia
- breast-feeding
- bronchitis
- cardiogenic shock
- cerebrovascular disease
- children
- chronic obstructive pulmonary disease (COPD)
- depression
- diabetes mellitus
- driving or operating machinery
- emphysema
- geriatric
- heart failure
- hepatic disease
- hyperthyroidism
- hypoglycemia
- hypotension
- myasthenia gravis
- peripheral vascular disease
- pheochromocytoma
- pregnancy
- psoriasis
- pulmonary disease
- pulmonary edema
- Raynaud’s phenomenon
- renal disease
- renal failure
- renal impairment
- sick sinus syndrome
- surgery
- thyroid disease
- thyrotoxicosis
- vasospastic angina
- ventricular dysfunction
Interactions
- Acetaminophen; Aspirin, ASA; Caffeine
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