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Nadolol



Nadolol
Systematic (IUPAC) name
(2R,3S)5-[2-hydroxy-3-(tert-butylamino)-propoxy]
tetralin-2,3-diol
Identifiers
CAS number 42200-33-9
ATC code C07AA12
PubChem 39147
DrugBank APRD00301
Chemical data
Formula C17H27NO4 
Mol. mass 309.401 g/mol
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

Nadolol (Corgard) is a non-selective beta-blocker used in the treatment of high blood pressure, migraine headaches, and chest pain.

Additional recommended knowledge

Contents

Chemistry and pharmacokinetics

Nadolol is nonpolar and hydrophobic, with low lipid solubility.

Mechanism of action

Nadol is a beta-specific sympatholytic which non-selectively blocks beta-1 adrenergic receptors which are mainly located in the heart, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate and blood pressure. It also blocks beta-2 adrenergic receptors which are located in bronchial smooth muscle, causing vasoconstriction. By binding beta-2 receptors in the juxtaglomerular apparatus, nadolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. Nadolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.

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. In patients with severe hypertension, nadolol can also treat reflex tachycardia due to treatment with vasodilators.

Off-Label Uses

A recent study found that, in certain adults with ADHD that had not responded to traditional therapies, or were unable to tolerate them, the addition of nadolol saw increase in attention and focusing capacities, along with a decrease in anxiety, impulsiveness, and somatic discomfort. [[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 vasoconstriction and should be avoided in asthma patients in preference of a beta-1 blocker.

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

Side effects

  • Bradycardia
  • Fatigue
  • Bronchospasms

See also

  • Renin-angiotensin system
  • Anti-hypertensive
  • Cardiology

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.

^ 


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Nadolol". A list of authors is available in Wikipedia.
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