 |
|
|
Nadolol
|
|
| Systematic (IUPAC) name | |
| (2R,3S)5-[2-hydroxy-3-(tert-butylamino)-propoxy] tetralin-2,3-diol |
|
| Identifiers | |
| CAS number | |
| ATC code | C07 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C17H27NO4 |
| Mol. mass | 309. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 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 | |
| Routes | Oral |
Nadolol (Corgard) is a non-selective beta-blocker used in the treatment of high blood pressure, migraine headaches, and chest pain. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The kidneys are complicated organs that have numerous biological roles The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The United States of America —commonly referred to as the The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained The United States of America —commonly referred to as the In Pharmacology and Toxicology, a route Beta blockers (sometimes written as β-blocker) are a class of drugs used for various indications but particularly for the management of Cardiac arrhythmias Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated Migraine is a neurological Syndrome characterized by altered bodily experiences painful headaches and nausea Angina pectoris, commonly known as angina, is severe Chest pain due to Ischemia (a lack of blood and hence Oxygen supply of the heart
Contents |
Chemistry and pharmacokinetics
Nadolol is nonpolar and hydrophobic, with low lipid solubility. Lipids are broadly defined as any fat- Soluble ( lipophilic) naturally-occurring Molecule, such as fats oils waxes cholesterol sterols fat-soluble
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. The adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the Catecholamines Adrenergic receptors The heart is a muscular organ in all Vertebrates responsible for pumping Blood through the Blood vessels by repeated rhythmic Norepinephrine ( INN) (abbreviated norepi or NE) or noradrenaline ( BAN) (abbreviated NA or NAd) is a Measuring heart rate The Pulse rate (which in most people is identical to the heart rate can be measured at any point on the body where an Artery 's pulsation Blood pressure is also the title of a short story by Damon Runyan in Guys and Dolls and Other Stories It also blocks beta-2 adrenergic receptors which are located in bronchial smooth muscle, causing vasoconstriction. The bronchioles or bronchioli are the first Airway branches that no longer contain Cartilage. Smooth muscle is a type of non- Striated muscle, found within the Tunica media layer of large and small Arteries and Veins, the bladder Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels particularly the large Arteries, Arterioles By binding beta-2 receptors in the juxtaglomerular apparatus, nadolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. The juxtaglomerular apparatus is a microscopic structure in the Kidney, which regulates the function of each Nephron. Renin (pronounced "Ree-nin" or "Rē-nin" (ˈriːnɨn also known as Angiotensinogenase, is a circulating Enzyme that participates in the body's Angiotensin causes blood vessels to constrict and drives blood pressure up Aldosterone is a hormone that causes the tubules of the kidneys to retain sodium and water Nadolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively. Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels particularly the large Arteries, Arterioles
The drug impairs AV node conduction and decreases sinus rate. The atrioventricular node (abbreviated AV node) is an area of specialized tissue between the atria and the ventricles of the Heart, specifically The Sinoatrial node (abbreviated SA node or SAN, also called the sinus node) is the impulse generating (pacemaker tissue located in the Right atrium
Nadolol may also increase plasma triglycerides and decrease HDL-cholesterol levels. Blood plasma is the Liquid component of Blood, in which the Blood cells are suspended (more properly known as, TAG or triacylglyceride) is Glyceride in which the Glycerol is Esterified with three Fatty acids It is the High-density lipoproteins ( HDL) is one of the 5 major groups of Lipoproteins ( Chylomicrons, VLDL, IDL, LDL, HDL Cholesterol is a Lipid found in the Cell membranes and transported in the Blood plasma of all Animals It is an essential component of mammalian
Indications
Nadolol is indicated for treatment of moderate hypertension and chest pain. Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated Angina pectoris, commonly known as angina, is severe Chest pain due to Ischemia (a lack of blood and hence Oxygen supply of the heart In patients with severe hypertension, nadolol can also treat reflex tachycardia due to treatment with vasodilators. Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated 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 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. The Sympathetic Nervous System ( SNS) is a branch of the Autonomic nervous system along with the Enteric nervous system and Parasympathetic nervous g. patients with congestive heart failure or myocardial infarct) should avoid nadolol as it inhibits sympathetic function. Heart failure is a Cardiac condition that occurs when a problem with the structure or function of the Heart impairs its ability to supply Myocardial infarction ( MI or AMI for acute myocardial infarction) also known as a heart attack, occurs when the blood supply Nadolol is also contraindicated in patients with bradycardia (slow heart rate) because of its vasodilatory effects and tendency to cause bradycardia. Bradycardia, as applied to adult medicine is defined as a resting Heart rate of under 60 beats per minute though it is seldom symptomatic until the rate drops below 50 beat/min
Because of its beta-2 activity, nadolol causes pulmonary vasoconstriction and should be avoided in asthma patients in preference of a beta-1 blocker. Asthma is a chronic Condition involving the Respiratory system in which the airways occasionally constrict become inflamed, and are Beta blockers (sometimes written as β-blocker) are a class of drugs used for various indications but particularly for the management of Cardiac arrhythmias
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. Insulin is a Hormone with intensive effects on both metabolism and several other body systems (eg vascular compliance Hypoglycemia or hypoglycaemia is the medical term for a pathologic state produced by a lower than normal level of Glucose ( sugar) in the blood Diabetes mellitus (ˌdaɪəˈbiːtiːz or /ˌdaɪəˈbiːtəs/ /məˈlaɪtəs/ or /ˈmɛlətəs/ often referred to simply as diabetes ( Ancient Greek: grc In patients with insulin-dependent diabetes, a selective beta-1 blocker is preferred over non-selective blockers. Insulin is a Hormone with intensive effects on both metabolism and several other body systems (eg vascular compliance
Side effects
See also
External links
- Nadolol, from the University of Utah School of Medicine
References
^ Buice RG, Subramanian VS, Duchin KL, Uko-Nne S. Bradycardia, as applied to adult medicine is defined as a resting Heart rate of under 60 beats per minute though it is seldom symptomatic until the rate drops below 50 beat/min Bronchospasm is a sudden constriction of the muscles in the walls of the Bronchioles It is caused by the release ( Degranulation) of substances from Mast cells The renin-angiotensin system (RAS or the renin-angiotensin-aldosterone system (RAAS is a hormone system that regulates Blood pressure and water ( fluid Antihypertensives are a class of drugs that are used in Medicine and Pharmacology to treat Hypertension (high blood pressure Cardiology (from Greek grc καρδίᾱ kardiā, "heart" and grc -λογία -logia) is the branch of Internal medicine The University of Utah (referred to locally as ' The U' or ' the U of U') is a publicly funded Research university in Salt Lake (1996). "Bioequivalence of a highly variable drug: an experience with nadolol. ". Pharmaceutical Research 13 (7): 1109-15. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document.
Dictionary
nadolol
-noun
- A non-selective beta blocker used in the treatment of high blood pressure, migraine headaches, and chest pain.
Dapyx Software network: MP3 Explorer | Ebook Manager | Zenithic