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Nadolol
Systematic (IUPAC) name
(2R,3S)-5-{[(2R)-3-( tert-butylamino)-2-hydroxypropyl]oxy}-1,2,3,4-tetrahydronaphthalene-2,3-diol
Identifiers
CAS number 42200-33-9
ATC code C07AA12
PubChem 39147
DrugBank APRD00301
Chemical data
Formula C 17H27NO4  
Mol. mass 309.401 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Protein binding 30%
Metabolism Nil
Half life 14-24 hours
Excretion Renal and fecal (unchanged)
Therapeutic considerations
Pregnancy cat. C(US)
Legal status POM (UK) -only (US)
Routes Oral
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Nadolol (Corgard, Anabet, Solgol, Corzide, Alti-Nadolol, Apo-Nadol, Novo-Nadolol) is a non-selective beta blocker used in the treatment of high blood pressure, migraine headaches, and chest pain.

Contents

Chemistry

Nadolol is polar and hydrophilic, with low lipid solubility.

Pharmcology

Nadolol is a non-selective beta blocker; that is, it non-selectively blocks both beta-1 and beta-2 receptors. It has a preference for beta-1 receptors, which are predominantly located in the heart, thereby inhibiting the effects of catecholamines and causing a decrease in heart rate and blood pressure. Its inhibition of beta-2 receptors, which are mainly located in the bronchial smooth muscle of the airways, leads to airway constriction similar to that seen in asthma. Inhibition of beta-1 receptors in the juxtaglomerular apparatus of the kidney inhibits the renin-angiotensin system, causing a decrease in vasoconstriction and a decrease in water retention. Nadolol's inhibition of beta-1 receptors in the heart and kidney lead to its effects on lowering blood pressure.

The drug impairs AV node conduction and decreases sinus rate.

Nadolol may also increase plasma triglycerides and decrease HDL-cholesterol levels.

Indications

Nadolol is indicated for treatment of moderate hypertension and chest pain and supraventricular tachycardia. In patients with severe hypertension, nadolol can also treat reflex tachycardia due to treatment with vasodilators. Nadolol and other non-selective beta-blockers are used in the prevention of rebleeding in the setting of bleeding secondary to portal hypertension.

Off-Label Uses

A case report study from Harvard Medical School, published in 1991, described three adult patients with ADHD unsuccessfully treated with traditional psychostimulant (amphetamine) therapy due to lack of effectiveness or intolerance of the psychostimulant. Nadolol was then added to the psychostimulant therapy and the combination of medications resulted in improved attention and focus with decreased medication side effects. This suggested the combination of nadolol and the psychostimulant might be effective for treatment-resistant adults with ADHD.[1]

Contraindications

Patients whose heart rate is largely mediated by the sympathetic nervous system (e.g. patients with congestive heart failure or myocardial infarct) should avoid nadolol as it inhibits sympathetic function. Nadolol is also contraindicated in patients with bradycardia (slow heart rate) because of its vasodilatory effects and tendency to cause bradycardia.

Because of its beta-2 activity, nadolol causes pulmonary bronchoconstriction and should be avoided in asthma patients in preference of a beta-1 blocker. (There may be new evidence indicating that long-term non-selective beta-blocker use may actually prove to be beneficial in mild asthma. [Hanania])

As nadolol, like other beta-2 blockers, inhibits the synthesis and release of glucose in response to hypoglycemia, it slows patients' recovery from acute hypoglycemic episodes and should be avoided in patients getting treatment for their diabetes mellitus. In patients with insulin-dependent diabetes, a selective beta-1 blocker is preferred over non-selective blockers.

Side Effects

See also

References

^  Buice RG, Subramanian VS, Duchin KL, Uko-Nne S. (1996). "Bioequivalence of a highly variable drug: an experience with nadolol". Pharmaceutical Research 13 (7): 1109–15. doi:10.1023/A:1016031313065.   ^N. Hanania, S. Singh, R. El-Wali, et al. The safety and effects of the beta-blocker, nadolol, in mild asthma: An open-label pilot study Pulmonary Pharmacology & Therapeutics, Volume 21, Issue 1, Pages 134-141

External links

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