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20160155
20161230
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Dexamethasone ¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do
Mechanism of Action
Dexamethasone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Dexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic receptors. This results in a modification of transcription and, hence, protein synthesis in order to achieve inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The antiinflammatory actions of dexamethasone are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
Pharmacology
Dexamethasone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Dexamethasone and its derivatives, dexamethasone sodium phosphate and dexamethasone acetate, are synthetic glucocorticoids. Used for its antiinflammatory or immunosuppressive properties and ability to penetrate the CNS, dexamethasone is used alone to manage cerebral edema and with tobramycin to treat corticosteroid-responsive inflammatory ocular conditions.
Metabolism
Dexamethasone¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
Protein Binding
Dexamethasone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 70%
Half-life
Dexamethasone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 36-54 hours
Absorption
Dexamethasone¿¡ ´ëÇÑ Absorption Á¤º¸ 80-90%
Pharmacokinetics
Dexamethasone palmitateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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Biotransformation
Dexamethasone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
Toxicity
Dexamethasone¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, rat LD50 : >3 gm/kg. Signs of overdose include retinal toxicity, glaucoma, subcapsular cataract, gastrointestinal bleeding, pancreatitis, aseptic bone necrosis, osteoporosis, myopathies, obesity, edemas, hypertension, proteinuria, diabetes, sleep disturbances, psychiatric syndromes, delayed wound healing, atrophy and fragility of the skin, ecchymosis, and pseudotumor cerebri.
Drug Interactions
Dexamethasone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Ambenonium The corticosteroid decreases the effect of anticholinesterasesAminoglutethimide Aminogluthetimide decreases the effect of dexamethasoneAmobarbital The barbiturate decreases the effect of the corticosteroidAnisindione The corticosteroid alters the anticoagulant effectAprepitant Aprepitant increases the effect and toxicity of dexamethasoneAprobarbital The barbiturate decreases the effect of the corticosteroidAspirin The corticosteroid decreases the effect of salicylatesButabarbital The barbiturate decreases the effect of the corticosteroidButalbital The barbiturate decreases the effect of the corticosteroidButethal The barbiturate decreases the effect of the corticosteroidDicumarol The corticosteroid alters the anticoagulant effectDihydroquinidine barbiturate The barbiturate decreases the effect of the corticosteroidEdrophonium The corticosteroid decreases the effect of anticholinesterasesEthotoin The enzyme inducer decreases the effect of the corticosteroidFosphenytoin The enzyme inducer decreases the effect of the corticosteroidHeptabarbital The barbiturate decreases the effect of the corticosteroidHexobarbital The barbiturate decreases the effect of the corticosteroidImatinib Decreases levels of imatinibMephenytoin The enzyme inducer decreases the effect of the corticosteroidMethohexital The barbiturate decreases the effect of the corticosteroidMethylphenobarbital The barbiturate decreases the effect of the corticosteroidMidodrine Increased arterial pressureNeostigmine The corticosteroid decreases the effect of anticholinesterasesPentobarbital The barbiturate decreases the effect of the corticosteroidPhenobarbital The barbiturate decreases the effect of the corticosteroidPhenytoin The enzyme inducer decreases the effect of the corticosteroidPrimidone The barbiturate decreases the effect of the corticosteroidPyridostigmine The corticosteroid decreases the effect of anticholinesterasesQuinidine barbiturate The barbiturate decreases the effect of the corticosteroidRifampin The enzyme inducer decreases the effect of the corticosteroidSecobarbital The barbiturate decreases the effect of the corticosteroidSunitinib Possible decrease in sunitinib levelsTalbutal The barbiturate decreases the effect of the corticosteroidWarfarin The corticosteroid alters the anticoagulant effectBismuth The corticosteroid decreases the effect of salicylatesAcenocoumarol The corticosteroid alters the anticoagulant effectSalicylate-magnesium The corticosteroid decreases the effect of salicylatesSalsalate The corticosteroid decreases the effect of salicylates
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Food Interaction
Dexamethasone¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food to reduce irritation.Avoid taking with grapefruit juice.
Drug Target
[Drug Target]
Description
Dexamethasone¿¡ ´ëÇÑ Description Á¤º¸ An anti-inflammatory 9-fluoro-glucocorticoid. [PubChem]
Dosage Form
Dexamethasone¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Elixir OralLiquid IntramuscularLiquid IntravenousLiquid OralOintment OphthalmicSolution IntravenousSolution OphthalmicSolution / drops OphthalmicTablet Oral
Drug Category
Dexamethasone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic AgentsAnti-inflammatory AgentsAntiemeticsAntineoplastic Agents, HormonalGlucocorticoids
Smiles String Canonical
Dexamethasone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1CC2C3CCC4=CC(=O)C=CC4(C)C3(F)C(O)CC2(C)C1(O)C(=O)CO
Smiles String Isomeric
Dexamethasone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)CO
InChI Identifier
Dexamethasone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C22H29FO5/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,23)17(26)10-20(16,3)22(12,28)18(27)11-24/h6-7,9,12,15-17,24,26,28H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,17+,19+,20+,21+,22+/m1/s1
Chemical IUPAC Name
Dexamethasone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (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
Drug-Induced Toxicity Related Proteins
DEXAMETHASONE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein :Brain-cadherin (BR-cadherin)Drug :dexamethasone Toxicity :osteoblast differentiation. [¹Ù·Î°¡±â] Replated Protein :Glucocorticoid-induced leucine zipper (GILZ)Drug :dexamethasone Toxicity :apoptosis. [¹Ù·Î°¡±â] Replated Protein :Signal transducer and activator of transcription 3Drug :dexamethasone Toxicity :apoptosis. [¹Ù·Î°¡±â] Replated Protein :Heme oxygenase 1Drug :dexamethasone Toxicity :oxidative injury. [¹Ù·Î°¡±â] Replated Protein :Alkaline phosphataseDrug :dexamethasone Toxicity :osteoblast differentiation. [¹Ù·Î°¡±â] Replated Protein :Interleukin-6 Drug :dexamethasone Toxicity :apoptosis. [¹Ù·Î°¡±â] Replated Protein :Ornithine decarboxylase Drug :dexamethasone Toxicity :pathogenesis of peptic ulcers. [¹Ù·Î°¡±â] Replated Protein :Aromatic-L-amino-acid decarboxylase Drug :dexamethasone Toxicity :pathogenesis of peptic ulcers. [¹Ù·Î°¡±â] Replated Protein :Interleukin-4 Drug :dexamethasone Toxicity :dexamethasone-induced differentiation of mouse myeloid leukemia cells. [¹Ù·Î°¡±â] Replated Protein :GastrinDrug :dexamethasone Toxicity :pathogenesis of peptic ulcers. [¹Ù·Î°¡±â] Replated Protein :Interleukin-4 Drug :dexamethasone Toxicity :dexamethasone-induced differentiation of mouse myeloid leukemia cells. [¹Ù·Î°¡±â] Replated Protein :Cadherin-11 Drug :dexamethasone Toxicity :osteoblast differentiation. [¹Ù·Î°¡±â] Replated Protein :Haptoglobin Drug :dexamethasone Toxicity :hepatic lipidosis(fatty liver). [¹Ù·Î°¡±â] Replated Protein :Interferon alpha-7 Drug :dexamethasone Toxicity :apoptosis. [¹Ù·Î°¡±â] Replated Protein :C-jun-amino-terminal kinase-interacting protein Drug :dexamethasone Toxicity :apoptosis of multiple myeloma cells. [¹Ù·Î°¡±â] Replated Protein :Mitogen-activated protein kinaseDrug :dexamethasone Toxicity :Dex-induced apoptosis. [¹Ù·Î°¡±â] Replated Protein :Cadherin-4 Drug :dexamethasone Toxicity :osteoblast differentiation. [¹Ù·Î°¡±â] Replated Protein :Glucose transporter 4Drug :dexamethasone Toxicity :cushing's syndrome. [¹Ù·Î°¡±â] Replated Protein :Nuclear factor NF-kappa-BDrug :dexamethasone Toxicity :pulmonary inflammation. [¹Ù·Î°¡±â] Replated Protein :Signal transducer and activator of transcription 3Drug :dexamethasone Toxicity :oxidative injury such as endotoxins and heme. [¹Ù·Î°¡±â] Replated Protein :Thrombomodulin Drug :dexamethasone Toxicity :deep venous thrombosis (DVT). [¹Ù·Î°¡±â] Replated Protein :Islet amyloid polypeptideDrug :dexamethasone Toxicity :marked stimulatory effect. [¹Ù·Î°¡±â]
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The database contains the following fields:
The generic name of each chemical
For module A10 (liver enzyme composite module):
Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method)
Number of endpoints at which each compound is marginally active (M)
Number of endpoints at which each compound is active (A)
For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively):
Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method)
Number of ADR reports for each compound, given as <4 or ¡Ã4
Reporting Index value for each compound, except where no shipping units were available (NSU)
Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period.
DEXAMETHASONE PALMITATE [GGT Increase] [Composite Activity] (Score) NA (Marginal) 0 (Active) 0 [Alkaline Phosphatase Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA [SGOT Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA [SGPT Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA [LDH Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA [GGT Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA
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