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(dexamethasone opthalmic )
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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.
Tobramycin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Tobramycin binds irreversibly to one of two aminoglycoside binding sites on the 30 S ribosomal subunit, inhibiting bacterial protein synthesis. Tobramycin may also destabilize bacterial memebrane by binding to 16 S 16 S r-RNA. An active transport mechanism for aminoglycoside uptake is necessary in the bacteria in order to attain a significant intracellular concentration of tobramycin.
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| 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.
Tobramycin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Tobramycin, an aminoglycoside antibiotic obtained from cultures of Streptomyces tenebrarius, is used in combination with other antibiotics to treat urinary tract infections, gynecologic infections, peritonitis, endocarditis, pneumonia, bacteremia and sepsis, respiratory infections including those associated with cystic fibrosis, osteomyelitis, and diabetic foot and other soft-tissue infections.
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| Metabolism |
Dexamethasone¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
Tobramycin¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Dexamethasone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 70%
Tobramycin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Dexamethasone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 36-54 hours
Tobramycin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Not Available
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| Absorption |
Dexamethasone¿¡ ´ëÇÑ Absorption Á¤º¸ 80-90%
Tobramycin¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
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| Biotransformation |
Dexamethasone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
Tobramycin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available
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| 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.
Tobramycin¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=441mg/kg (s.c. in mice)
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| 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
Tobramycin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Dexamethasone¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food to reduce irritation.Avoid taking with grapefruit juice.
Tobramycin¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Dexamethasone¿¡ ´ëÇÑ Description Á¤º¸ An anti-inflammatory 9-fluoro-glucocorticoid. [PubChem]
Tobramycin¿¡ ´ëÇÑ Description Á¤º¸ An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the pseudomonas species. It is a 10% component of the antibiotic complex, nebramycin, produced by the same species. [PubChem]
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| Drug Category |
Dexamethasone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic AgentsAnti-inflammatory AgentsAntiemeticsAntineoplastic Agents, HormonalGlucocorticoids
Tobramycin¿¡ ´ëÇÑ Drug_Category Á¤º¸ AminoglycosidesAnti-Bacterial Agents
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| 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
Tobramycin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NCC1OC(OC2C(N)CC(N)C(OC3OC(CO)C(O)C(N)C3O)C2O)C(N)CC1O
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| 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
Tobramycin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ NC[C@H]1O[C@H](O[C@@H]2[C@@H](N)C[C@@H](N)[C@H](O[C@H]3O[C@H](CO)[C@@H](O)[C@H](N)[C@H]3O)[C@H]2O)[C@H](N)C[C@@H]1O
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| 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
Tobramycin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H37N5O9/c19-3-9-8(25)2-7(22)17(29-9)31-15-5(20)1-6(21)16(14(15)28)32-18-13(27)11(23)12(26)10(4-24)30-18/h5-18,24-28H,1-4,19-23H2/t5-,6+,7+,8-,9+,10+,11-,12+,13+,14-,15+,16-,17+,18+/m0/s1
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| 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
Tobramycin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-amino-2-[4,6-diamino-3-[3-amino-6-(aminomethyl)-5-hydroxyoxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-6-(hydroxymethyl)oxane-3,5-diol
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| 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 3 Drug:dexamethasone Toxicity:apoptosis. [¹Ù·Î°¡±â] Replated Protein:Heme oxygenase 1 Drug:dexamethasone Toxicity:oxidative injury. [¹Ù·Î°¡±â] Replated Protein:Alkaline phosphatase Drug: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:Gastrin 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: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 kinase Drug:dexamethasone Toxicity:Dex-induced apoptosis. [¹Ù·Î°¡±â] Replated Protein:Cadherin-4 Drug:dexamethasone Toxicity:osteoblast differentiation. [¹Ù·Î°¡±â] Replated Protein:Glucose transporter 4 Drug:dexamethasone Toxicity:cushing's syndrome. [¹Ù·Î°¡±â] Replated Protein:Nuclear factor NF-kappa-B Drug:dexamethasone Toxicity:pulmonary inflammation. [¹Ù·Î°¡±â] Replated Protein:Signal transducer and activator of transcription 3 Drug: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 polypeptide Drug:dexamethasone Toxicity:marked stimulatory effect. [¹Ù·Î°¡±â] TOBRAMYCIN ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Lysozyme Drug:tobramycin Toxicity:nephrotoxicity. [¹Ù·Î°¡±â] Replated Protein:phospholipases C Drug:tobramycin Toxicity:aminoglycoside toxicity. [¹Ù·Î°¡±â] Replated Protein:Phospholipase A Drug:tobramycin Toxicity:aminoglycoside toxicity. [¹Ù·Î°¡±â] Replated Protein:Lactate dehydrogenase Drug:tobramycin Toxicity:nephrotoxicity. [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[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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