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nadolol (Corgard)
Trademark: Corgard.
Indications:
- hypertension
- tachyarrhythmias
- thyrotoxicosis
- cardiac angina
- post myocardial infarction
- secondary prevention in patients with cardiovascular disease
- mitral valve prolapse
- long QT syndrome
- migraine prophylaxis
- tremor
Contraindications:
1) bronchial asthma or COPD
2) heart failure or cardiogenic shock
3) 2nd or 3rd degree AV block
4) severe sinus bradycardia
Dosage:
1) start: 40 mg PO QD
2) usual effective dose: 40-80 mg PO QD
3) maximum: 320 mg/day
4) taper over 1-2 weeks when discontinuing therapy
Tabs: 20, 40, 80, 120, 160 mg.
Dosage adjustment in renal failure:
creatinine clearance dosage
31-50 mL/min every 24-36 hours
10-30 mL/min every 24-48 hours
< 10 mL/min every 40-60 hours
Pharmacokinetics:
1) oral absorption averages 20-40%, no effect of food
2) protein-binding 30% [2]
3) therapeutic levels:
a) peak steady state concentration 55-62 ng/mL 2-4 hours after oral administration
b) trough level: 32 ng/mL
4) tissue distribution:
- aqueous humor concentration 1/2 of serum concentration
4) elimination 1/2life is 20-24 hours
5) NOT appreciably metabolized
6) eliminated unchanged in the urine & feces
7) antihypertensive effect may take a few days to several weeks
Adverse effects:
1) nausea
2) diarrhea
3) constipation
4) bradycardia
5) hypotension
6) paresthesias
7) dizziness
8) sedation
9) bronchospasm (0.1%)
10) carpal tunnel syndrome (rare)
11) hypoglycemia in type I diabetics:
a) may mask symptoms
b) may prolong hypoglycemia
12) dry eyes (0.1-0.5%)
13) papilledema (rare)
14) cough & nasal congestion (0.1-0.5%)
15) alopecia, rash, pruritus (0.1-0.5%)
Drug interactions:
1) alpha-1 adrenergic antagonists: orthostatic hypotension
2) amiodarone: symptomatic bradycardia & sinus arrest
3) sympathomimetics
4) lidocaine serum levels may increase by 20-30%
5) methacholine
6) methyldopa (paradoxical hypertensive response to stress)
7) NSAIDs may interfere with antihypertensive effect
6) phenothiazines may decrease metabolism of nadolol
Laboratory:
1) specimen: serum, plasma (EDTA, heparin)
2) methods: fluorometry, GC-MS, HPLC
Mechanism of action:
- lipid insoluble non-selective beta-adrenergic antagonist
Interactions
drug interactions
drug adverse effects (more general classes)
General
non-specific beta-adrenergic receptor antagonist (non-specific beta-blocker)
propanolamine
Properties
MISC-INFO: elimination route KIDNEY
1/2life 14-18 HOURS
20-24 HOURS
protein-binding 16-24%
30%
elimination by hemodialysis +
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- DrugDex Drug Evaluation
- Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed,
WB Saunders, Philadelpha 1995
- Deprecated Reference
Component-of
bendroflumethiazide/nadolol (Corzide)