Term
| Aspirin (acetyl-salicylic acid) pharmokinetics |
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Definition
orally ingested--rapidly absorbed in part of the stomach, but mainly from the uper small intestine
-t1/2 in plasma is 15 minutes
-highly plasma protein bound |
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Term
| Aspirin Mechanism of action |
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Definition
| irreversibly and non-selectively inhibits fatty acid cyclo-genases--stop PGG2 (precursor to PG's, PGI2 and Thromboxanes) |
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Term
| Aspirin other possible mechanism |
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Definition
acetylation of COX-2 leading to increased production of lipoxins
-NFK-beta activation and production of other eicosanoids |
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Term
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Definition
-Anti-pyretic action: reduces body temp in febrile states. Inhibits synthesis and release of PG's in the CNS
-Analgesia: effective against low to moderate pain. Inhibits peripheral synthesis and release of PG's in inflammation and averts the sensitization of pain receptors to mechanical stimulation or other mediators
-Anti-inflammatory action: inhibits PG synthesis, and thus decreases inflammation
-uncouples oxidative phosphorylation |
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Term
| Aspirin FDA labeled indications |
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Definition
| Cerebrovascular accident (prophylaxis), fever, generalized aches and pains, headache, migraine, myocardial infarction, myocardial infarction prophylaxis, osteoarthritis, pain, rheumatoid arthritis |
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Term
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Definition
-gastric irritant, can cause ulceration (inhibits synthesis of PGE2 and PGI2, cytoprotective of gastric mucosa)
-increased bleeding time by inhibiting platelet aggregation (inhibition of fatty acid cyclo-oxygenase)
-prolongation of gestation (inhibition of cyclo-oxygenase) |
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Term
| Hypersensitivity to aspirin |
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Definition
| a non-immunological, anaphylactoid response |
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Term
| Hypersensitivity to aspririn signs and symptoms |
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Definition
-vasomotor rhinitis
-angioneurotic edema
-urticaria
-bronchial asthma
-nasal polyposis |
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Term
| explanation for aspririn hypersensitivity response |
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Definition
| inhbits fatty acid cyclo-oxygenase, thus shifts the released arachidonic acid towars the leukotriene pathway. The LT's responsible for anaphylactoid response |
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Term
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Definition
| decreased teh 1st pass metabolism of ethanol |
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Term
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Definition
| mild, chronic salicylate intoxication; usually occures after large repeated doses of aspirin |
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Term
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Definition
| headache, dizziness, tinnitus, hearing difficulty, dimness of vision, nausea and vomiting, disturbance in acid-base balance, hemorrhagic phenomena |
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Term
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Definition
acute poisoning-accidental or deliberate
-reye's syndrome in kids
-end-stage renal failure associations
-renal toxicity of NSAID's |
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Term
| Indomethacin (INDOCIN) mechanism of action |
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Definition
| one of the most potent inhibitors of fatty acid cyclo-oxygenase thus inhibiting prostaglandin, thromboxane and prostacyclin synthesis |
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Term
| Indomethacin pharm properties |
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Definition
-more potent than aspirin, although show no superiority over aspirin
-analgesic
-antipyretic
-anti-inflammatory |
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Term
| Indomethacin FDA labaled indications |
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Definition
| ankylosing spondylitis, gouty arthritis, osteoarthritis, pain (acute shoulder), patent ductus arteriousus, rheumatoid arthritis |
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Term
| indomethacin toxicity and adverse effects |
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Definition
-GI complaints
-hypersensitivity--usually shows cross-reactivity with aspirin
-CNS effects--headache, vertigo, somnolence |
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Term
| indomthecin therapuetic uses |
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Definition
-rheumatoid arthritis
Barter's syndrome
patent ductus arteriousus
-prevent spontaneous abortion |
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Term
| Proprionic acid derivatives |
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Definition
-usually better tolerated than aspirin, indomethacin and the pyranzolones
-inhibit cyclo-oxygenase
-can produce aspirin like hypersensitivity |
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Term
| Ibuprofen (Motrin, Brufen) fda labeled indications |
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Definition
-fever
-headache
-migraine
-osteoarthritis
-pain
-primary dysmenorrhea (pain during menses)
-rheumatoid arthritis |
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Term
| Naproxen (Naprosyn, others) indications |
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Definition
-ankylosing spondylitis (spine arthritis)
-brusitis
-fever
gout, acute
Headache, osteoarthritis, pain, primary dysmenorrhea, rheum arth, tendinitis |
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Term
| Ketorlac tromethamine (Toradol) pharmacokinetics |
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Definition
-intramuscular injection
-99% plasma protein bound
-some transpiacental transfer, may inhibit platelet aggregation in infants when used for labor
-clearance reduced in elderly and those with renal disease, lower dosages must be used |
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Term
| Ketorlac tromethamine (toradol) indications |
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Definition
-extraction of cataract
-pain, short term
-pain in eye--refractive keratoplasty
-seasonal allergic conjuctivitis |
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Term
| ketorolac tromethamine properties |
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Definition
used for short term management of post op moderate to severe pain
-shown to be superior to morphine and meperidine
-may be used with opiates
-lacks repiratory depresent effects of narcotic analgesics
-limit duration of use because of renal failure |
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Term
| Celecoxib (celebrex) mechanism and pharmokinetics |
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Definition
-selective Cox II inhibitor
-absorption decreased by food
-effective t1/2 = 11 hours
-high plasma protein binding
-metabolized by CYP 2C9 |
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Term
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Definition
| -ankylosing spondylitis, familial multiple polyposis syndrome, juvenile rhem arth, osteo arth, acute pain, primary dysmenorrhea, rhem arth |
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Term
| celecobix adverse effects |
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Definition
some dyspepsia
-increase incidence of cardiovascular disease |
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Term
| acetaminophen (tylenol, tempra) pharmacokinetics |
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Definition
-rapidly and completely absored from teh GI tract after oral admin
-t1/2 = 3 to 4 hours |
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Term
| acetameniphan pharm actions |
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Definition
-analgesic
-anti-pyretic
-weak anti-inflammatory--in therapeutic doses it prob has no anti inflam action |
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Term
| acetameniphan indications |
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Definition
dysmenorrhea
fever
headache
pain, mild to moderate |
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Term
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Definition
-tolerated well in recommended doses
-hepatic necrosis--also associated with alcohol abuse
-renal tubular necrosis
-methemoglobinemia
-hemolytic anemia
-increased risk of end stage renal disease
-treatment of toxicity--use acetylcysteine (mucomyst) to bind hepatotoxic metabolite |
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