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Diclofenac / M02AA15
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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.
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
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
Absorption
Diclofenac¿¡ ´ëÇÑ Absorption Á¤º¸ Completely absorbed from the gastrointestinal tract.
Pharmacokinetics
Diclofenac diethylammoniumÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
´Ü¹é°áÇÕ : 99%
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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)
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
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
Food Interaction
Diclofenac¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food to reduce irritation.Avoid alcohol.
Drug Target
[Drug Target]
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]
Dosage Form
Diclofenac¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Solution OphthalmicSolution TopicalSuppository RectalTablet OralTablet, coated OralTablet, extended release Oral
Drug Category
Diclofenac¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Inflammatory Agents, Non-SteroidalCyclooxygenase InhibitorsNonsteroidal Antiinflammatory Agents (NSAIDs)
Smiles String Canonical
Diclofenac¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl
Smiles String Isomeric
Diclofenac¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl
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
Chemical IUPAC Name
Diclofenac¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetic acid
Drug-Induced Toxicity Related Proteins
DICLOFENAC ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸Replated Protein :CYP3A4Drug :Diclofenac Toxicity :idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein :CYP2C9Drug :Diclofenac Toxicity :idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â]
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