Therapeutic strategiesThe treatment of patients with inflammation involves twoprimarygoals:1. The relief of pain2. The slowing or -in theory-arrest of thetissue-damaging processTherapeutic drugs1. Nonsteroidal anti-inflammatory drugs(NSAIDs)2.Glucocorticoids3.Disease-modifying anti-rheumatic drugsSlow-acting antirheumatic drugs(SAARDS)
Therapeutic strategies The treatment of patients with inflammation involves two primary goals: 1. The relief of pain 2. The slowing or –in theory-arrest of the tissue-damaging process. Therapeutic drugs 1. Nonsteroidal anti-inflammatory drugs(NSAIDs) 2. Glucocorticoids 3. Disease-modifying anti-rheumatic drugs Slow-acting antirheumatic drugs(SAARDS)
Nonsteroidal anti-inflammatorydrugsChemistry andpharmacokineticsAll but one of the NSAIDs are weak organic acidsMostofthesedrugs arewell absorbedMost of the NSAIDs are highly protein-boundMost of the NSAIDs are highly metabolized in theliverRenal excretion is the most important route for finalelimination,，nearly all undergoenterohepaticcirculation
Nonsteroidal anti-inflammatory drugs Chemistry and pharmacokinetics All but one of the NSAIDs are weak organic acids Most of these drugs are well absorbed Most of the NSAIDs are highly protein-bound Most of the NSAIDs are highly metabolized in the liver Renal excretion is the most important route for final elimination, nearly all undergo enterohepatic circulation
Nonsteroidal anti-inflammatory drugs1.NSAIDSdiflunlsal,aspirin,diclogenac,etodolac,fenamates, fenoprofen, flurblprofen, Ibuprofen,indomethacin,ketoprofen,methylsalicylate,nabumetone,naproxin,oxaprazin,phenylbutazone, piroxicam, sulindac,tolmetin2.COX-2 INHIBITORScelecoxib3.NON-NARCOTIC ANALGESICSacetaminophenphenacetin
Nonsteroidal anti-inflammatory drugs 1.NSAIDS aspirin, diflunlsal, diclogenac, etodolac, fenamates, fenoprofen, flurblprofen, lbuprofen, indomethacin, ketoprofen, methylsalicylate, nabumetone, naproxin, oxaprazin, phenylbutazone, piroxicam, sulindac, tolmetin 2. COX-2 INHIBITORS celecoxib 3.NON-NARCOTIC ANALGESICS acetaminophen phenacetin
Nonsteroidal anti-inflammatorydrugsChemistry andpharmacokineticsAll but one of the NSAIDs are weak organic acidsMostofthesedrugs arewell absorbedMost of the NSAIDs are highly protein-boundMost of the NSAIDs are highly metabolized in theliverRenal excretion is the most important route for finalelimination,，nearly all undergoenterohepaticcirculation
Nonsteroidal anti-inflammatory drugs Chemistry and pharmacokinetics All but one of the NSAIDs are weak organic acids Most of these drugs are well absorbed Most of the NSAIDs are highly protein-bound Most of the NSAIDs are highly metabolized in the liver Renal excretion is the most important route for final elimination, nearly all undergo enterohepatic circulation
Mechanism of actionAlltheNSAIDS areInhibition of the enzVme COXAnd resulting inhibition of prostaglandin synthesisInhibition of COX can occur by several mechanism.1. Irreversible inhibition: aspirin2. Competitive inhibition: ibuprofen3. Reversible, non-competitive inhibition: paracetamol
Mechanism of action All the NSAIDS are Inhibition of the enzyme COX, And resulting inhibition of prostaglandin synthesis. Inhibition of COX can occur by several mechanism: 1. Irreversible inhibition: aspirin 2. Competitive inhibition: ibuprofen 3. Reversible, non-competitive inhibition: paracetamol