Nadolol

Nadolol
Nadolol
Systematic (IUPAC) name
(2R,3S)-5-{[(2R)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-1,2,3,4-tetrahydronaphthalene-2,3-diol
Clinical data
Trade names Corgard
AHFS/Drugs.com monograph
MedlinePlus a682666
Pregnancy cat. C(US)
Legal status POM (UK) ℞-only (US)
Routes Oral
Pharmacokinetic data
Protein binding 30%
Metabolism Nil
Half-life 14-24 hours
Excretion Renal and fecal (unchanged)
Identifiers
CAS number 42200-33-9 YesY
ATC code C07AA12
PubChem CID 39147
IUPHAR ligand 554
DrugBank APRD00301
ChemSpider 35815 YesY
UNII FEN504330V YesY
KEGG D00432 YesY
ChEMBL CHEMBL649 YesY
Chemical data
Formula C17H27NO4 
Mol. mass 309.401 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

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.

Pharmacology

Main article: Beta-blocker

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 leads 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 has U.S. Food and Drug Administration approved indications for the treatment of hypertension and for the long-term treatment of angina pectoris.[1]

Off-label uses

Nadolol is used for the prevention of migraine headaches for which there is good documentation.[2]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.[3])

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

  1. ^ Drug Facts And Comparisons. 2011 Edition. Wolters Kluwer Health, 77 Westport Plaza, Suite 450, St. Louis, Missouri. (4)775.
  2. ^ Drug Facts And Comparisons. 2011 Edition. Wolters Kluwer Health, 77 Westport Plaza, Suite 450, St. Louis, Missouri. (4)775
  3. ^ http://ajrcmb.atsjournals.org/cgi/content/full/38/3/249

^ 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. PMID 8842054.  ^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

v · d · eSympatholytic (and closely related) antihypertensives (C02)
Sympatholytics
(antagonize α-adrenergic
vasoconstriction)
Central
Adrenergic release inhibitors
Bethanidine • Bretylium • Debrisoquine • Guanadrel • Guanazodine • Guanethidine • Guanoclor • Guanoxan • Guanazodine • Guanoxabenz • Guanoxan
Mecamylamine • Pentolinium • Trimethaphan
Peripheral
Indirect
Tyrosine hydroxylase inhibitor
Direct
Non-selective α blocker
Other antagonists
dual (Bosentan) • selective (Ambrisentan, Sitaxentan)

M: VAS

anat(a:h/u/t/a/l,v:h/u/t/a/l)/phys/devp/cell/prot

noco/syva/cong/lyvd/tumr, sysi/epon, injr

proc, drug(C2s+n/3/4/5/7/8/9)

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Look at other dictionaries:

  • Nadolol — Nombre (IUPAC) sistemático (2R,3S) 5 {[(2R) 3 (tert butilamino) 2 hidroxipropil]oxi} 1,2,3,4 tetrahidronaftalene 2,3 diol …   Wikipedia Español

  • nadolol — Agente bloqueante betaadrenérgico utilizado en el tratamiento a largo plazo de la angina de pecho y la hipertensión. Diccionario Mosby Medicina, Enfermería y Ciencias de la Salud, Ediciones Hancourt, S.A. 1999 …   Diccionario médico

  • Nadolol — Strukturformel Gemisch von vier Stereoisomeren Allgemeines Freiname …   Deutsch Wikipedia

  • Nadolol — НАДОЛОЛ ( Nаdolol )*. 2,3 цис 1,2,3,4 Тетрагидро 5 [2 окси 3(трет бутиламино)]пропокси 2,3 нафталиндиол. Синонимы: Коргард, Аnabet, Веtаdоl, Соrgаrd, Nаdiс, Sоlgol. b Адреноблокатор неизбирательного действия (блокирует b 1 и b 2 адренорецепторы) …   Словарь медицинских препаратов

  • nadolol — noun A non selective beta blocker used in the treatment of high blood pressure, migraine headaches, and chest pain …   Wiktionary

  • nadolol — A β adrenergic blocking agent with actions similar to those of propranolol. * * * na·do·lol nā dō .lȯl, .lōl n a beta blocker C17H27NO4 used in the treatment of hypertension and angina pectoris * * * n. a beta blocker used in the treatment of… …   Medical dictionary

  • nadolol — n. a beta blocker used mainly in the treatment of angina pectoris and arrhythmias and to prevent migraine attacks. It is administered by mouth; side effects include decreased heart rate, dizziness, and low blood pressure. Trade names: Corgard …   The new mediacal dictionary

  • nadolol — noun a beta adrenergic blocking agent (trade name Corgard) that is used to treat hypertension and angina • Syn: ↑Corgard • Usage Domain: ↑trade name (for: ↑Corgard) • Hypernyms: ↑beta blocker, ↑ …   Useful english dictionary

  • Beta blocker — Beta blockers Drug class Skeletal formula of propranolol, the first clinically successful beta blocker ATC code C07 …   Wikipedia

  • Bêta-bloquant — Pour les articles homonymes, voir Bêta (homonymie). Un bêta bloquant ou β bloquant est un médicament utilisé en cardiologie qui bloque l action des médiateurs du système adrénergique tels l adrénaline. Les bêta bloquants prennent la place de ces… …   Wikipédia en Français

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