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º¼Å¸¸¶À̽ÅÁ¡¾È¾× [Diclofenac sodium , Gentamicin Sulfate]
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[E22020101]
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(gentamicin sulfate opthalmic )
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| Mechanism of Action |
Diclofenac¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ The antiinflammatory effects of diclofenac are believed to be due to inhibition of both leukocyte migration and the enzyme cylooxygenase (COX-1 and COX-2), leading to the peripheral inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis is responsible for the analgesic effects of ketoprofen. Antipyretic effects may be due to action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat dissipation.
Gentamicin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Aminoglycosides like gentamicin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically gentamicin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes.
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| Pharmacology |
Diclofenac¿¡ ´ëÇÑ Pharmacology Á¤º¸ Diclofenac is an acetic acid nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Diclofenac is used to treat pain, dysmenorrhea, ocular inflammation, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and actinic keratosis
Gentamicin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Gentamicin is a broad spectrum aminoglycoside antibiotic. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses.
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| Metabolism |
Diclofenac¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C9 (CYP2C9)Cytochrome P450 2C19 (CYP2C19)Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2C8 (CYP2C8)Cytochrome P450 2D6 (CYP2D6)Glucuronosyltransferase
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| Protein Binding |
Diclofenac¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ More than 99%
Gentamicin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Low (between 0 and 30%)
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| Half-life |
Diclofenac¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2 hours
Gentamicin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3-3¨ö hours in infants one week to six months of age; this increases to 5¨ö hours in full-term and large premature infants less than one week old.
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| Absorption |
Diclofenac¿¡ ´ëÇÑ Absorption Á¤º¸ Completely absorbed from the gastrointestinal tract.
Gentamicin¿¡ ´ëÇÑ Absorption Á¤º¸ Injections lead to peak serum concentrations in 30-60 minutes. Topical gentamicin is readily absorbed from large burned, denuded, or granulating areas but not through intact skin. Absorption of gentamicin is faster and greater with the cream compared to the ointment. Gentamicin is absorbed in small quantities following topical application to the eye. Gentamicin is also absorbed in small amounts following topical application to the ear (especially if the eardrum is perforated or if tissue damage is present).
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| Pharmacokinetics |
Diclofenac sodiumÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ´Ü¹é°áÇÕ : 99%
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Gentamicin SulfateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- ºÐÆ÷ : ÅÂ¹Ý Åë°ú
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- ½Å»ý¾Æ : 0.4-0.6 L/kg
- ¼Ò¾Æ : 0.3-0.35 L/kg
- ¼ºÀÎ : 0.2-0.3 L/kg
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| Biotransformation |
Diclofenac¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
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| Toxicity |
Diclofenac¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include loss of consciousness, increased intracranial pressure, and aspiration pneumonitis. LD50=390mg/kg (orally in mice)
Gentamicin¿¡ ´ëÇÑ Toxicity Á¤º¸ Mouse, intravenous LD50: 52 mg/kg; rat, intravenous LD50: 96 mg/kg.
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| Drug Interactions |
Diclofenac¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alendronate Increased risk of gastric toxicityAnisindione The NSAID increases the anticoagulant effectCyclosporine Monitor for nephrotoxicityDicumarol The NSAID increases the anticoagulant effectWarfarin The NSAID increases the anticoagulant effectRifampin Decreased levels/effect of the NSAID
Gentamicin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Atracurium The agent increases the effect of muscle relaxantDoxacurium The agent increases the effect of muscle relaxantGallamine Triethiodide The agent increases the effect of muscle relaxantMetocurine The agent increases the effect of muscle relaxantMivacurium The agent increases the effect of muscle relaxantPancuronium The agent increases the effect of muscle relaxantPipecuronium The agent increases the effect of muscle relaxantRocuronium The agent increases the effect of muscle relaxantSuccinylcholine The agent increases the effect of muscle relaxantTubocurarine The agent increases the effect of muscle relaxantVecuronium The agent increases the effect of muscle relaxantBumetanide Increased ototoxicityEthacrynic acid Increased ototoxicityFurosemide Increased ototoxicityTorasemide Increased ototoxicityThalidomide Thalidomide increases the renal toxicity of the aminoglycosideCisplatin Increased risk of nephrotoxicityCefradine Increased risk of nephrotoxicityCephapirin Increased risk of nephrotoxicityCefamandole Increased risk of nephrotoxicityCefazolin Increased risk of nephrotoxicityCefonicid Increased risk of nephrotoxicityCefoperazone Increased risk of nephrotoxicityCeforanide Increased risk of nephrotoxicityCefotaxime Increased risk of nephrotoxicityCefotetan Increased risk of nephrotoxicityCefoxitin Increased risk of nephrotoxicityCeftazidime Increased risk of nephrotoxicityCeftizoxime Increased risk of nephrotoxicityCeftriaxone Increased risk of nephrotoxicityCefuroxime Increased risk of nephrotoxicityCephalothin Group Increased risk of nephrotoxicity
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Diclofenac¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2C9
NSAIDs:
**diclofenac**
ibuprofen
piroxicam
Oral Hypoglycemic Agents:
tolbutamide
glipizide
Angiotensin II Blockers:
NOT candesartan
irbesartan
losartan
NOT valsartan
celecoxib
fluvastatin naproxen
phenytoin
sulfamethoxazole
tamoxifen
tolbutamide
torsemide
warfarin
INHIBITORS
CYP 2C9
amiodarone
fluconazole
isoniazid
INDUCERS
CYP 2C9
rifampin
secobarbital
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| Food Interaction |
Diclofenac¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food to reduce irritation.Avoid alcohol.
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| Drug Target |
[Drug Target]
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| Description |
Diclofenac¿¡ ´ëÇÑ Description Á¤º¸ A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. [PubChem]
Gentamicin¿¡ ´ëÇÑ Description Á¤º¸ A complex of three different closely related aminoglycoside sulfates, Gentamicins C1, C2, and C1(subA), obtained from Micromonospora purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit protein synthesis (genetic translation). [PubChem]
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| Dosage Form |
Diclofenac¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Solution OphthalmicSolution TopicalSuppository RectalTablet OralTablet, coated OralTablet, extended release Oral
Gentamicin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Cream TopicalLiquid OphthalmicOintment OphthalmicOintment TopicalSolution Auricular (otic)Solution IntravenousSolution OphthalmicSolution / drops Auricular (otic)Solution / drops Ophthalmic
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| Drug Category |
Diclofenac¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Inflammatory Agents, Non-SteroidalCyclooxygenase InhibitorsNonsteroidal Antiinflammatory Agents (NSAIDs)
Gentamicin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Bacterial AgentsProtein Synthesis Inhibitors
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| Smiles String Canonical |
Diclofenac¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl
Gentamicin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNC(C)C1CCC(N)C(O1)OC1C(N)CC(N)C(OC2OCC(C)(O)C(NC)C2O)C1O
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| Smiles String Isomeric |
Diclofenac¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl
Gentamicin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN[C@H](C)[C@@H]1CC[C@@H](N)[C@@H](O1)O[C@H]1[C@H](N)C[C@H](N)[C@@H](O[C@@H]2OC[C@@](C)(O)[C@H](NC)[C@H]2O)[C@@H]1O
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| InChI Identifier |
Diclofenac¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C14H11Cl2NO2/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19/h1-7,17H,8H2,(H,18,19)/f/h18H
Gentamicin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C21H43N5O7/c1-9(25-3)13-6-5-10(22)19(31-13)32-16-11(23)7-12(24)17(14(16)27)33-20-15(28)18(26-4)21(2,29)8-30-20/h9-20,25-29H,5-8,22-24H2,1-4H3
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| Chemical IUPAC Name |
Diclofenac¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetic acid
Gentamicin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[4,6-diamino-3-[3-amino-6-(1-methylaminoethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-5-methyl-4-methylaminooxane-3,5-diol
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| Drug-Induced Toxicity Related Proteins |
DICLOFENAC ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP3A4 Drug:Diclofenac Toxicity:idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein:CYP2C9 Drug:Diclofenac Toxicity:idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] GENTAMICIN ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Phospholipase A Drug:gentamicin Toxicity:aminoglycoside toxicity. [¹Ù·Î°¡±â] Replated Protein:phospholipases C Drug:gentamicin Toxicity:aminoglycoside toxicity. [¹Ù·Î°¡±â] Replated Protein:Angiotensinase A Drug:gentamicin Toxicity:important consequences upon renal function and metabolism. [¹Ù·Î°¡±â] Replated Protein:Dipeptidylpeptidase IV Drug:gentamicin Toxicity:important consequences upon renal function and metabolism. [¹Ù·Î°¡±â] Replated Protein:Sodium/potassium-transporting ATPase Drug:Gentamicin Toxicity:necrosis. [¹Ù·Î°¡±â]
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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