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Dexamethasone
Systematic (IUPAC) name
(8S,9R,10S,11S,13S,14S,16R,17R)- 9-Fluoro-11,17-dihydroxy-17- (2-hydroxyacetyl)-10,13,16-trimethyl- 6,7,8,11,12,14,15,16- octahydrocyclopenta[a]phenanthren- 3-one
Identifiers
CAS number 50-02-2
ATC code A01AC02 C05AA09, D07AB19, H02AB02, R01AD03, S01BA01, S02BA06, S03BA01
PubChem 5743
DrugBank APRD00674
Chemical data
Formula C22H29FO5 
Mol. mass 392. 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 ATC code A01 is a division of the Anatomical Therapeutic Chemical Classification System and part of the A Alimentary tract and metabolism section A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. 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 Fluorine, fluorum meaning "to flow" is the Chemical element with the symbol F and Atomic number 9 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 464 g/mol
Pharmacokinetic data
Bioavailability 80-90%
Protein binding 70%
Metabolism hepatic
Half life 36-54 hours
Excretion renal
Therapeutic considerations
Pregnancy cat.

C(US)
Legal status

℞ Prescription only
Routes Oral, IV, IM, SC and IO

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid hormones. 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 liver is a vital organ in the human body and is present in Vertebrates and some other animals 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 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 In Pharmacology and Toxicology, a route Intravenous therapy or IV therapy is the giving of Liquid substances directly into a Vein. Intramuscular injection is the injection of a substance directly into a Muscle. An injection is an infusion method of putting Liquid into the Body, usually with a hollow needle and a Syringe which is pierced through Intraosseous infusion is the process of injection directly into the Marrow of the bone A steroid is a Terpenoid Lipid characterized by a Carbon skeleton with four fused rings generally arranged in a 6-6-6-5 fashion Hormones (from Greek ὁρμή - "impetus" are chemicals released by cells that affect cells in other parts of the body It acts as an anti-inflammatory and immunosuppressant. Anti-inflammatory refers to the property of a substance or treatment that reduces Inflammation. For a list of immunosuppressive drugs see the Transplant rejection page. Its potency is about 20-30 times that of hydrocortisone and 4-5 times of prednisone. Cortisol is a Corticosteroid Hormone produced by the Adrenal gland (in the Zona fasciculata of the Adrenal cortex) Prednisone is a synthetic Corticosteroid drug that is usually taken orally but can be delivered by Intramuscular injection and can be used for a great number

Contents

Therapeutic use

Anti-inflammatory

Dexamethasone is used to treat many inflammatory and autoimmune conditions, e. Inflammation ( Latin, inflamatio, to set on fire is the complex biological response of vascular tissues to harmful stimuli such as Pathogens Autoimmune diseases arise from an overactive Immune response of the body against substances and tissues normally present in the body g. , rheumatoid arthritis. Rheumatoid arthritis ( RA) is a chronic systemic autoimmune disorder that causes the Immune system to attack the Joints, where

It is also given in small amounts (usually 5-6 tablets) before and/or after some forms of dental surgery, such as the extraction of the wisdom teeth, an operation which often leaves the patient with puffy, swollen cheeks. Dental surgery is any of a number of Medical procedures which involve artificially modifying the Dentition.

It is injected into the heel when treating plantar fasciitis, sometimes in conjunction with triamcinolone acetonide. Plantar fasciitis is a painful inflammatory condition of the Foot caused by excessive wear to the Plantar fascia that supports the Arch Triamcinolone acetonide is a more potent type of Triamcinolone, being about 8 times as effective as Prednisone.

It is useful to counteract allergic shock, if given in high doses. It is present in certain eye drops and as a nasal spray (trade name Dexacort). Eye drops are saline -containing Drops used as a vector to administer medication in the Eye. Nasal sprays, or nasal mists, are used for the nasal delivery of a drug or drugs generally to alleviate cold or Allergy symptoms such as Nasal congestion

Dexamethasone is used in transvenous screw-in cardiac pacing leads to minimize the inflammatory response of the myocardium. The steroid is released into the myocardium as soon as the screw is extended and can play a significant role in minimizing the acute pacing threshold due to the reduction of inflammatory response. The typical quantity present in a lead tip is less than 1. 0 mg.

Oncologic uses

In oncology, it is given to cancer patients undergoing chemotherapy, to counteract certain side-effects of their antitumor treatment. Cancer (medical term Malignant Neoplasm) is a class of Diseases in which a group of cells display uncontrolled Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer. An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted negative consequences Dexamethasone can augment the antiemetic effect of 5-HT3 receptor antagonists like ondansetron. An anti-emetic is a drug that is effective against Vomiting and Nausea. The 5-HT3 antagonists are a class of Medications which act as Receptor antagonists at the 5-hydroxytryptamine-3 receptor (5-HT3 receptor Ondansetron ( INN) (ɒnˈdænsɛtrɒn or Zofran is a Serotonin 5-HT3 receptor antagonist used mainly as an Antiemetic to Dexamethasone is also used in certain hematological malignancies, especially in the treatment of multiple myeloma, in which dexamethasone is given alone or together with thalidomide (thal-dex) or a combination of Adriamycin (doxorubicin) and vincristine (VAD). Hematological malignancies are the types of Cancer that affect Blood, Bone marrow, and Lymph nodes As the three are intimately connected through Multiple myeloma (also known as MM, myeloma, plasma cell myeloma, or as Kahler's disease after Otto Kahler) is a type of Thalidomide is a Sedative - Hypnotic, and Multiple myeloma Medication. Doxorubicin ( INN,; trade name Adriamycin; also known as hydroxydaunorubicin) is a drug used in cancer Chemotherapy. Vincristine (brand name Oncovin also known as leurocristine, is a vinca Alkaloid from the Madagascar periwinkle ( Catharanthus roseus, In brain tumours (primary or metastatic), dexamethasone is used to counteract the development of edema, which could eventually compress other brain structures. A brain tumor is any intracranial Tumor created by abnormal and uncontrolled cell division, normally either in the Brain itself ( Neurons Oedema (or Edema in American English formerly known as dropsy or hydropsy, is the increase of Interstitial fluid in any organ &mdash swelling Dexamethasone is also given in cord compression where a tumor is compressing the spinal cord. Spinal cord compression develops when the Spinal cord is compressed by bone fragments from a vertebral fracture a Tumor, Abscess, ruptured Intervertebral

Endocrine

Dexamethasone can be used in the context of congenital adrenal hyperplasia, to prevent virilisation of a female fetus. Congenital adrenal hyperplasia ( CAH) refers to any of several Autosomal Recessive Diseases resulting from Mutations In biology and medicine virilization refers to the biological development of Sex differences, changes which make a Male body different from a Female body If one or both parents are carriers of mutations to the CYP21A gene, the mother may start dexamethasone treatment within 7 weeks of conception. Controversy over the beginning of pregnancy usually occurs in the context of the Abortion debate At the 12th week, a chorionic villus sample will determine whether the fetus is male (in which case the dexamethasone is stopped) or female. Chorionic villus sampling (CVS is a form of Prenatal diagnosis to determine chromosomal or Genetic disorders in the Fetus. Subsequent DNA analysis can then reveal whether the female fetus is a carrier of the mutation, in which case dexamethasone treatment must continue until birth. The side-effects for the mother can be severe and the long-term impact on the child is not clear.

Obstetrics

Dexamethasone may be given to women at risk of delivering prematurely in order to promote maturation of the fetus' lungs. In living organisms a respiratory system functions to allow Gas exchange. This has been associated with low birth weight, although not with increased rates of neonatal death. Birth weight is the weight of a baby at its birth. It has direct links with the Gestational age at which the child was born and can be estimated [1]

High altitude illnesses

Dexamethasone is used in the treatment of high altitude cerebral edema as well as pulmonary edema. High altitude cerebral edema (or HACE) is a severe (frequently fatal form of Altitude sickness. It is commonly carried on mountain climbing expeditions to help climbers deal with altitude sickness. [2]

Diagnostic use

Dexamethasone is also used in a diagnostic context, namely in its property to suppress the natural pituitary-adrenal axis. The hypothalamic-pituitary-adrenal axis ( HPA or HTPA axis) also known as the Limbic -hypothalamic-pituitary-adrenal axis (LHPA axis is a complex set of direct influences Patients presenting with clinical signs of glucocorticoid excess (Cushing's syndrome) are generally diagnosed by a 24-hour urine collection for cortisol or by a dexamethasone suppression test. The dexamethasone suppression test is designed to diagnose and differentiate among the various types of Cushing's syndrome and other hypercortisol states During the latter, the response of the body to a high dose of glucocorticoids is monitored. Various forms are performed. In the most common form, a patient takes a nighttime dose of either 1 or 4 mg of dexamethasone, and the serum cortisol levels are measured in the morning. If the levels are relatively high (over 5 µg/dl or 150 nmol/l), then the test is positive and the patient has an autonomous source of either cortisol or ACTH, indicating Cushing's syndrome where the tumor does not have a feedback mechanism. Cortisol is a Corticosteroid Hormone produced by the Adrenal gland (in the Zona fasciculata of the Adrenal cortex) Adrenocorticotropic hormone ( ACTH or corticotropin) is a Polypeptide Hormone produced and secreted by the Pituitary gland If ACTH levels are lowered by at least 50%, this would indicate Cushing's Disease, since the pituitary adenoma has a feedback mechanism that has been reset to a higher level of cortisol. Pituitary adenomas are Tumors that occur in the Pituitary gland, and account for about 10% of intracranial neoplasms. Longer versions rely on urine collections on oral dexamethasone over various days.

Veterinary use

Combined with marbofloxacin and clotrimazole, dexamethasone is available under the name Aurizon , CAS number 115550-35-1, and used to treat difficult ear infections, especially in dogs. Marbofloxacin is a potent Antibiotic of the Fluoroquinolone group Clotrimazole is an Antifungal medication commonly used in the treatment of fungal infections of both humans and animals such as vaginal yeast infections and CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to It can also be combined with Trichlormethiazide to treat horses with swelling of distal limbs and general bruising. Trichlormethiazide ( INN, currently being sold under the brand names of Achletin, Diu-Hydrin and Triflumen) is a Diuretic with properties In fields of Anatomy, anatomical terms of location are descriptive terms to help identify relative positions or directions within a species [3]

Contraindications

Some of these contraindications are relative:

Side effects

If dexamethasone is given orally or by injection (parenteral) over a period of more than a few days, side-effects common to systemic glucocorticoids may occur. In Medicine, a contraindication (pronounced as contra-indication is a condition or factor that increases the Risks involved in using a particular drug, Ulceration may refer to Ulcer, healing wound that develops on the skin Fear Factory, an American heavy metal band formerly known as Ulceration Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated Diabetes mellitus (ˌdaɪəˈbiːtiːz or /ˌdaɪəˈbiːtəs/ /məˈlaɪtəs/ or /ˈmɛlətəs/ often referred to simply as diabetes ( Ancient Greek: grc Tuberculosis (abbreviated as TB for tubercle bacillus or T u' b' erculosis Bacillus --> is a common Glaucoma is a group of diseases of the Optic nerve involving loss of retinal ganglion cells in a characteristic pattern of optic neuropathy. Osteoporosis is a Disease of Bone that leads to an increased risk of fracture. These may include:

Other side-effects have been noted, and should cause concern if they are more than mild.

The short time treatment for allergic reaction, shock, and diagnostic purposes usually does not cause serious side effects.

Interactions

Other interactions (with certain antibiotics, estrogens, ephedrine, digoxin) are known.

Dosage

Sports doping

In 2005, Polish cross country skier Justyna Kowalczyk was disqualified from the Under 23 (U23) OPA (Alpine nations) Intercontinential Competition in Germany and issued a 2-year suspension for her doping offenses on dexamethasone. Year 2005 ( MMV) was a Common year starting on Saturday (link displays full calendar of the Gregorian calendar. Poland (Polska officially the Republic of Poland Cross-country skiing (also known as XC skiing) is a Winter sport popular in many countries with large snowfields primarily Northern Europe, Justyna Kowalczyk ( (born January 19, 1983 in Limanowa) is a Polish Cross country skier who has been competing since 2000 Germany, officially the Federal Republic of Germany ( ˈbʊndəsʁepuˌbliːk ˈdɔʏtʃlant is a Country in Central Europe. [4] This was eventually reduced to one year during 2005 and later rescinded by the Court of Arbitration for Sport in December 2005. The Court of Arbitration for Sport ( CAS; Tribunal Arbitral du Sport or TAS in French) is an international arbitration body set up to settle disputes [5] She would later earn a bronze in the women's 30 km freestyle mass start at the 2006 Winter Olympics in Turin. The 2006 Winter Olympics, officially known as the XX Olympic Winter Games, were a Winter Multi-sport event which was celebrated in

References

  1. ^ Bloom SL, Sheffield JS, McIntire DD, Leveno KJ (2001). "Antenatal dexamethasone and decreased birth weight". Obstet Gynecol 97 (4): 485–90. doi:10.1016/S0029-7844(00)01206-0. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 11275014.  
  2. ^ COMMENTS AND RESPONSES Reducing the Incidence of High-Altitude Pulmonary Edema Annals of Internal Medicine PDF
  3. ^ Trichlormethiazide and Dexamethasone for veterinary use. Wedgewood Pharmacy. Retrieved on 2008-01-23. 2008 ( MMVIII) is the current year in accordance with the Gregorian calendar, a Leap year that started on Tuesday of the Common Events 393 - Roman Emperor Theodosius I proclaims his nine year old son Honorius co-emperor
  4. ^ June 13, 2005 FIS Doping Control statement on Kowalcyzk (Digitized version). - Accessed July 30, 2006
  5. ^ December 14, 2005 FIS Newsflash on her overturned suspension (Digitized version). - Accessed July 30, 2006

External links

Events 1419 - First Defenestration of Prague. 1502 - Christopher Columbus lands at Guanaja in the Bay Islands off Year 2006 ( MMVI) was a Common year starting on Sunday of the Gregorian calendar.

Dictionary

dexamethasone

-noun

  1. (biochemistry) A synthetic member of the glucocorticoid class of steroid hormones, having the chemical formula C22H29FO5, or a derivative thereof
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