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14 Cards in this Set

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acetylsalicylic acid (aspirin)
1.irreversibly acetylates serine residues on COX-1 & 2; prevents binding of arachidonate
2.weak acid; orally absorbed in stomach & small intestine
3.low dose—rapidly metabolized; ½-life 15 min. Undergoes enterohepatic circulation (sticks around longer despite low dose & short ½-life)
high dose—zero-order metabolism; ½-life 3-5 hrs. to 12-15 hrs.
4.binds to serum proteins; at high dose, less is bound
5.reversibility for platelets requires synthesis of new platelets (8-10 days); can’t produce more COX b/c no nucleus
6.anti-inflammatory & anti-nociceptive (interferes w/ kallikrein system); effective analgesic & anti-pyretic
7.high doses required for inflammatory disease (i.e. rheumatoid arthritis)
8.combos with aspirin are not more effective than aspirin alone (unless w/ opioid)
9.good anti-coagulant; prevents TIAs, unstable angina, coronary artery thrombosis w/ MI, thrombosis w/ coronary artery bypass surgery, may reduce incidence of colon cancer (anti-ox activity?)
10.preparations to ↓ GI irritation: buffering, enteric coating, misoprostol (PGE1 analog), omeprazole (proton-pump inhibitor)
11.dosage: <600 mg/4 h for analgesia & anti-pyretic effect; 3.2 – 4 g/d for anti-inflammatory effect
12.toxicities (dose-related): salicylism—nausea, vomiting, tinnitus, vertigo, ↓ hearing; higher doses cause respiratory alkalosis → metabolic acidosis, hyperthermia, vasomotor collapse, coma, renal & respiratory failure; treatment is symptomatic, use sodium bicarbonate to facilitate excretion
13.other adverse effects: hepatotoxicity, impaired renal function, asthma, Reyes syndrome
non-acetylated salicylates
(sodium salicylate; salicylsalicylate)
1.reversible but poor/ineffective inhibitors of COX
2.side effects less; no NSAID asthma or renal toxicity (valuable in specific pt.s)
3.good anti-inflammatories, poor analgesics
COX-1 & 2 non-selectives
-selection of agents depends on pt’s response/tolerance of side FX
-ibuprofen, diclofenac, etodolac, indomethacin, ketoprofen, naproxen, sulindac
Ibuprofen (OTC)
- non-selective
- 2400 mg/d: anti-inflammatory effectiveness of aspirin w/ less GI irritation
- low dose: effective analgesic but loses anti-inflammatory effect
- ½ life 2h, largely liver metabolized
- side FX: GI, rash, tinnitus, fluid retention, NSAID asthma, kidney failure, interstitial nephritis, hepatitis
- ½ life 1-2h, largely liver metabolized (renal dysfunction doesn’t impair clearance—good for pts w/ kidney damage
- ↑ serum aminotransferase seen (liver)
- non-selective
- ↑ affinity for COX-2, less GI irritation
- ½ life 4 – 6 hrs.
- non-selective
- very potent
- promotes closure of ductus arteriosus
- side FX: GI irritation, psychosis w/ hallucinations (indole derivative like 5-HT & LSD)
- non-selective
- inhibits COX-1, 2, and lipoxygenase
- ½-life 1 – 3 hrs. but available in slow-release prep. 1/d
- non-selective
- ½-life 12 hrs.; also available in slow-release prep.
- free fraction 40% higher in females than males
- usual side FX
- non-selective
- long-acting, sulfoxide prodrug
- helpful in familial intestinal polyposis
- can ↑ serum aminotransferases; associated w/ cholestatic liver damage
COX-2 selectives
- can’t be used in pts w/ gastric ulcers despite ↓ GI irritation!!!
- Celebrex, Vioxx, Bextra
Celecoxib (Celebrex)
- least potent COX-2 selective (less COX-2 selectivity)
- fewer GI side FX than non-selectives but no effect on platelet aggregation
- side FX: kidney damage, interferes w/ anti-hypertensive therapy & edema
- low dose aspirin + celecoxib = no cardiac complications but GI protection gone
Rofecoxib (Vioxx) & Valdecoxib (Bextra)
- more potent COX-2 selective
- side FX: heart complications, hypertension, edema
Acetaminophen (OTC)
- (must be converted to reactive metabolite & conjugated to glutathione for excretion)
- COX-1 & 2 inhibitor primarily in CNS; anti-pyretic & analgesic
- No anti-inflammatory or anti-coagulant effect, and no GI irritation
- Substitute for aspirin in children or when contraindicated
- Allergy occurs sometimes; pts sensitive to salicylates only rarely sensitive to acetaminophen
- side FX: liver toxicity (10-15 g) & death (20-25 g) w/ OD; glutathione (important anti-ox.) depleted in OD and hepatocytes suffer oxidant injury—enzymatic activity impaired
- Mucomyst (acetylcysteine): antidote; maintains glutathione by binding converted acetaminophen (reactive metabolite). Given up to 36 hrs. after OD, most effective at 8-10 hrs.