NSAIDs Flashcards
COX-1
Enzyme that produce prostaglandins that are important for general housekeeping function of gastric protection and hemostasis
COX-2
Inducible form of the enzyme
Prostaglandins that mediate pain, inflammation, fever and carcinogenesis
Key mediator of both peripheral and central pain sensitization
PG-E2
Effect of PG
Increase release of Sub. P and glutamate (1ON)
Increase sensitivity of 2ON
Decrease NT from descending pain modulating pathways
NSAID general MoA
Competitive inhibitor of COX
Duration of NSAID relates directly to
Metabolism of the drug
Hyperalgesia
Exaggerated pain response to normally painful stimulus
Allodynia
Painful response to a typically non-painful stimulus
Areas where COX-2 is constitutively expressed
Kidney
Bone
Brain
Reproductive organ
Side effect of NSAIDs
Platelet dysfunction
GI ulceration
Risk of nephrotoxicity
Hypertension
Contraindications of NSAIDs and COX-2 selective inhibitor
Hypersensitivity
Triad of Asthma, aspirin and nasal polyposis
Contraindications for COX-2 inhibitors
Allergy to sulfonamides
NSAID with no/little anti inflammatory and anti platelets effect
Paracetamol
MoA of Paracetamol
Inhibition of central COX-3 in CNS
Modulation of descending inhibitory serotonergic pathway
Act on opioid and NMDA receptor
Effect of Salicylates on Respiration
Increase O2 consumption
Increase CO2 production
Increase respiration
MDD of Paracetamol
4gm
DOA of Paracetamol
2 hours
Dosage of Paracetamol
0.5-1 gm/4-6 hrs
Dosage of Salicylate
0.5-1 gm/4-6 hrs
DOA of Salicylates
15-20 min
MDD of Salicylates
3gm
Effect of Salicylates on CVS
Cardioprotective effect <100mg
Salt and water retention»_space; increased CO
Contraindications of Salicylates against bleeding time
Hypoprothrombinemia
Severe hepatic damage
Vit K deficiency
Haemophilia
Contraindications of Salicylates in third trimester because
Prolonged gestation
Complicated deliveries
Premature closure of ductus arteriosus
Excretion of Salicylates
Free salicylates 10%
Metabolites 90%
Urine pH dependecy of Salicylates excretion
Alkaline urine - 30%
Acidic urine - 2%
Toxicity of Salicylates
Hearing impairment
Blurred vision
Light-headedness
Use of Ketrolac
Short-term pain management
Immediate postop period
Ketorolac (Vs Morphine)
Less dosage
Similar onset to morphine
Longer DOA
Use of Ketorolac
Patient at high risk for postoperative respiratory depression or emesis
Pre-admission of Ketorolac
Hypovolemia should be corrected
Effect of Ketorolac on CNS
Minimal effect
Does not cross BBB to significant degree
Side effect of Ketorolac
Inhibit platelet aggregation
Prolong bleeding
Long term use may lead to renal toxicity
Contraindication of Ketorolac
Aspirin or NSAID allergy
Triad (AAP)
Most commonly used NSAID in Europe
Diclofenac
DOA of Diclofenac
8hrs
Property of Diclofenac
Preferentially COX-2 inhibitor
High first pass effect
Accumulate in synovial fluid
Use of Diclofenac
Long-term symptomatic treatment of RA and OA
Short-term treatment of acute musculoskeletal pain, post-op pain, dysmenorrhea
Cataract Extraction
Side effect of Diclofenac
Modest, reversible elevation of hepatic transaminase
Property of Indomethacin
More potent inhibitor of COX than aspirin
Central and peripheral anti-inflammatory action
Excellent oral bioavailability
Use of Indomethacin
Acute gouty arthritis
RA
OA
Closure of PDA
Side effect of Indomethacin
Diarrhea
PUD
Acute pancreatitis
Hepatitis
Which NSAID has inhibitory effect on leukocyte function
Ibuprofen
