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Nsaid: Pharmakokinetics Pharmakodynamics CU AE CI DI Salicylic Acid

This document summarizes the pharmacokinetics, pharmacodynamics, clinical uses, adverse effects, and drug interactions of various non-steroidal anti-inflammatory drugs (NSAIDs). It describes the metabolism, protein binding, mechanisms of action, dosing, and indications for aspirin, celecoxib, meloxicam, diclofenac, diflusinal, flurbiprofen, ibuprofen, indomethacin, ketoprofen, ketolorac, nabumetone, and naproxen. It also lists common adverse effects and contraindications for each drug as well as important drug-drug interaction information.

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0% found this document useful (0 votes)
66 views2 pages

Nsaid: Pharmakokinetics Pharmakodynamics CU AE CI DI Salicylic Acid

This document summarizes the pharmacokinetics, pharmacodynamics, clinical uses, adverse effects, and drug interactions of various non-steroidal anti-inflammatory drugs (NSAIDs). It describes the metabolism, protein binding, mechanisms of action, dosing, and indications for aspirin, celecoxib, meloxicam, diclofenac, diflusinal, flurbiprofen, ibuprofen, indomethacin, ketoprofen, ketolorac, nabumetone, and naproxen. It also lists common adverse effects and contraindications for each drug as well as important drug-drug interaction information.

Uploaded by

jessmasaki
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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NSAID

PHARMAKOKINETICS PHARMAKODYNAMICS
CU AE CI DI
Metabol PB MOA Dose
SALICYLIC ACID
Aspirin Rapidly Salicylate Irreversible  HD: uricosuric ↓incidence of ischemic attack  Respi rate & depth ↓  Hemophilia  ↓conc: indomethacin,
hidrolyzed: acetic nonlinier inhibiton of  Kronic LD: Unstable angina  Alkalosis respi  krn PCO2  Tx preeclampsia naproxen, ketoprofen,
acid & salicylate bound to platelet COX: lower colon Ca Coronary artery thrombosis w ↓ – eclampsia fenoprofen
albumin anti platelet incidence myocardial infarction  Nephrotoxicity  Fever caused by  Antagonis of
efek last 8-10  <1000mg   Thrombosis after bypass grafting  Periferal vessel dilate viral inf in spironolactone-induced
days analgetic & Oral formulation  IBD , ulcerative  Pendrhn GIT children  reye natriuresis  antagonis
antipiretik colitis  Insulin like effect ↑sensi syndrome aldosteron
Least toxic  3-4g  Rectal enema  mild – moderate reseptor insulin  Blockade active transpor
antilinflamasi ulcerative colitis, procitis,  Ototoxic penicilin dr CSF k drh
Eliminasi: proctosigmoidistis
alkalinisasi  Rectal supository  active UC
 RA & ankylosing spondylitis
 Keratolytic action  fungal dkk
 Liniments
 <efektif for ankylosing spondytilytis
NONACETYLATED SALICYLATE
Celecoxib CYP2C9  COX2 selective  Asthma  Sulfonamide derivat  may   Warfarin  CYP2C9
Meloxicam inhibitor w/ bleeding tendency cause rash metabolism
 Inhibit vasc w/ renal dysfunction (close  AE GI ↓
endothelium supervision  No impact on platelet
prostacycline aggregation
synthesis  not  Renal toxicity (krn COX2 aktif
offer Cardio d ginjal)
protective effect  MELO: Fewer than
piroxicam, diclofenac,
naproxen
NON SELECTIVE COX INHIBITOR
Diclofenac  More liver func  IM adm  + misoprotol : GIU, diare
abnorm  + omeprazole: U bleeding, renal
ADR
 Opthalmic  Post op. Ophtalmic inflamm
prep
 Topical  Solar keratosis
 Oral mouth wash
Diflusinal  Not metab to salic  RA: 500-1000  Cancer pain w bone metastase
acid/ salicylate  Pain control in dental surgery
 Enterohepatic  RA
cycle
 Capacity limited
metabolism
 Renal klirens
flurbiprofen  Extensive hepatic  Topical  Intraoperative miosis inhibition
metabolism opthalmic
 IV  Minor preoperative analgesia

 Lozenge  Sore throat


Ibuprofen  Less fluid  PO<2400  Analgesic  Rare agranulocytosis &  Nasal polyp  Aspirin antagonizes
retention than  2400  Anti inflamm anemia aplastik  Angiodema irreversible plt induced
indomethacin  PO/IV  Closing PDA  Bronchospastic by Aspirin
 Least toxic reactivity to Decrease total anti
aspirin inflam effect
Indomethacin  Potent non  Opthalmic  Conjunctival inflamm, traumatic  Accelerated PDA
selective COX prep corneal abration reduce pain  Pancreatitits
inhibition  Oral rinse  Gingival inflam  Dizzines
 Inhibit: PLA & C  Epidural inj  Post laminectomy sy  Confusion
 Reduce netruphil  Depression
migration  Hallucination
 Decrease T & B  Great toxicity
cell proliferation
ketoprofen  (-) COX & LOX  GIT  (+)probenecid: elevates
 CNS ketiprofen level &
prolong HL
Ketolorac  IM  Systemic use analgesic. Not anti
inflam
 IV  Replace morphine in post op pain
 Oral  Reduce opioid dose
 Ophtalmic  Limited use (GI, renal SE)
prep
Nabumetone  HL: >24 hrs  Pseudophorphyria  Renal impairment
 Enterohepatic  Photosensitivity  doubling HL
cycle (-)
Naproxen  SR, oral susp,  Rheumatologic  alergic pneumonitis
topical,  leukocytoclastic
opthalmic sol  vasculitis
 OTC  GIT Bleedingibuprofen  ps.phorphyria
Piroxicam  HD: (-) PMN  Rheumatic  Peptic ulcer bleeding (9,5
migration & times other NSAID)
limfosit
function.
↓oxygen
radical prod
Sulindac  Enterohepatic  RD  Thrombositopenia
cycle  Agranulocytosis
 DOA 12-16 jam  Nephrotic sy
 Aminotransferase> 
cholestatic liver damage 
stop!

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