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66 Cards in this Set
- Front
- Back
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Pathways of synthesis
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study P. 171+
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Prostaglandin PGE1/PGE2
Fxns |
relax vascular smooth muscle of kidney and periph
stim gastric mucosal secretion inhibit parietal cells contract uterine SM PAIN - bradykinin and Hist |
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Prostaglandin PGF2a
Fxns |
vasoconstrictor
strong uterine contraction regulates aqueous humor |
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Prostacyclin PGI2
Fxns |
vasodilaor - venous and arterial side
inhib. platelet aggregation PAIN |
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Thromboxane A2
fxns |
potent vasoconscrictor
platelet release |
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Leukotrienes
LTB4 fxn |
chemotaxis of inflam mediators
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Leukotrienes
LTC,D,E 4 |
bronchoconstrictors
asthma! involved in RA and inflam bowel disease (IBD) |
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PGE1/2
Newborns |
maintains ductus arteriosus
newborns have a decline in production PGE1 can temp maintain ductus can be continuously infused b.c metab rapidly |
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PGE1/2
Penis |
induction of erection
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PGF2a
Abortion IM - 15-methyl carboprost tromethane |
makes strong uterine contractions - leads to abortions 69%
methyl makes longer duration control postpartum hemorrhage |
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PGE2
Dinoprostone Abortions |
uterine contractions
cervical ripening/dilitation can be used with carboprost, mifepristone, and methotrexate |
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PGE2
Dinoprostone Birth |
stim. myometrial contractions
cervial ripening before induction of labor by oxytocin or alternative to |
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PGE1
Ulcers |
protects stomach and GI from ulcers
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Epoprostenol
Iloprost (nasal) |
PGI2 analogues
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Epoprostenol
Iloprost PGE Uses |
vasodilators!
Raynaud's and cold digital ischemia pul. HTn MI, cerebral ischemia |
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Latanoprost
PGF2a |
reduce intraocular P
inc. outflow of aqueous humor by activating FP receptors |
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PGI2
Iloprost Epoprostenol Dialysis |
replacement for heparin b.c heparin can cause systemic side E b.c of long half life
also, platelet inhib (heparin is not) |
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COX1 features
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constitutive enz, BV, stomach, kidney, GFR
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COX2 features
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inflame by cytokines, H2Oand Na homeostasis
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PAIN Induction and cytokines
PGE2/PGI2 |
sensitize pain receptors and processing
C and Ad fibers in periph in dorsal root - GABA inhib pain; PG dec. GABA; inhib. the inhibitor; inc pain central hyperalgesia - PGs produce allodynia - inc perception of pain (flu) |
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Fever
Mech |
pyrogens induce IL1 from neutrophils
In hypo, IL1 causes PGE2 syn, inc body temp COX2 inhib modulates temp |
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Imflamme
Mech |
NSAIDs don't effect HETEs or leukotrienes
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PGE1 Analogues
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Prostin
Alprostadil Misoprostol |
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Salicyates
Aspirin (ASA) Acetylsalicylic Acid Features |
analgesia - good
antipyresis - high doses can cause fever Inc O2 consumption respiration - contributes to acid base balance in poisioning |
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Salicyates
Aspirin (ASA) Mech |
Irr covalent acetylation of serine on COX 1 and 2
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Salicyates
Aspirin (ASA) Absorption, Distribution |
ab in upper SI
ditribute to most fluids crosses BBB and placenta 90% bound to plasma proteins |
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Salicyates
Aspirin (ASA) Metab/excretion |
rapidly de-acetylation in stomach and plasma
in liver make salcyluric acid half like 15h excreted in kidney by 1st and 0 order |
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Salicyates
Aspirin (ASA) Side E |
GI ulcer - pill causes irritation; causes dec. mucus prod.
hepatotoxicity/nephrotoxicity reye's syndrome - viral infection in young prolong bleeding time |
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Salicyates
Aspirin (ASA) Toxic Effects |
dose dependant
tinnitus, hypervent and resp alkalosis fever, dehydration, metabolic acidosis shock/resp failure. |
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Salicyates
Aspirin (ASA) Contraindications |
bldding disorders
acute bronchospasm, asthma head trauma active peptic ulcer NSAID hypersensitivity agranulocytosis |
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Acetic Acids
Drugs 4 |
Indomethacin
Etodolac ketorolac diclofenac |
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Acetic Acids
Indomethacin Features |
inhibit COX; 40X greater than aspirin
rapidly absorbed, plasma proteins eliminated in urine, bile, feces |
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Acetic Acids
Indomethacin Mech |
inhibt COX 1 and 2
INTERFERES with active site non-covalent, competitive inhib of AA binding platelets can recover |
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Acetic Acids
Indomethacin Interactions |
prodenecid - elevates amt of idomethacin
furosemide - antag indometh thiazide diuretics - effects dec by indometh |
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Acetic Acids
Indomethacin Toxic |
GI ulcers
CNS - headache, dizziness, confusion nutropenia intol. in long term use more than aspirin |
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Acetic Acids
Indomethacin Uses |
acute gout (aspirin better)
acute flare up in RA drug of choice - ankylosing spondylosis |
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Acetic Acids
Sulindac |
half as potent as indometh
produg; converted in liver |
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Acetic Acids
Etodolac |
some COX2 specificity
plasma proteins no interference with warfarin 7 hr half life once a day dosing |
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Acetic Acids
Ketorolac |
only NSAID with IV administration
COX1 specific - stopped after 5 days b.c after then 80% adverse effects |
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Acetic Acids
Diclofenac |
most commonly used NSAID in europe
some cox2 specificity; antiinflammatory agent |
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Propionic acids
Ibuprofen Features |
better tolerated
RA and for analgesia least amt side E |
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Propionic acids
Ibuprofen Mech |
non covalent inhib of cox 1 and 2; same efficacy as aspirin
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Propionic acids
Ibuprofen Pharmaco |
2-4 hr half life
99% bound, rapid excretion in urine |
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Propionic acids
Naproxen Features |
acid or Na salt so absorbed rapidly
half life 15 h |
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Fenamates
meclofenamic acid |
noncovalent inhib of cox 1 and 2
metab in liver; elimin in urine used if hypersensitive to others |
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Oxicams
Piroxicam |
enterohepatic circulation
some toxic effects |
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COX2 Inhibitors
Celecoxib Pharmaco |
oral absorption
97% plasma bound extensive distribution metab by P450 in liver |
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COX2 Inhibitors
Celecoxib Use/Mech |
competitive inhib of COX2 10X to cox1
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COX2 Inhibitors
Celecoxib Benefits |
reduced gastroduodenal erosion
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COX2 Inhibitors
Celecoxib Use |
analgesic
antipyretic antiinflammatory OA, RA, ulcers |
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COX2 Inhibitors
Celecoxib contraindications |
asthma
hepatic/renal insufficiency late in preggers |
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COX2 Inhibitors
Celecoxib Interactions |
cidofovir - antiviral; inc. toxicities
fluconazole ace inhib - NSAIDs reduce activity Li - interfere with secretion |
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COX2 Inhibitors
Celecoxib Side E |
Death
edema, headache upper resp tract infection stomach pain, nausea HTN due to thromboxane leads to effects |
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COX2 Inhibitors
Rofecoxib (Vioxx) |
OA and dysmenorrhea
withdrawn from market by Merck |
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Non-opiate Analgesic
Acetaminophen Tylenol Use |
analgesic
antipyretic little antiinflammatory activity |
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Non-opiate Analgesic
Acetaminophen Tylenol Pharmaco |
oral admin, slightly bound to pp
2-3 hr half life |
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Non-opiate Analgesic
Acetaminophen Tylenol Mech |
inhib of prostaglandin syn; more effective in CNS
inhib of COX |
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Non-opiate Analgesic
Acetaminophen Tylenol Indications |
ASA poorly tolerated
blood abnormality peptic ulcer history |
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Non-opiate Analgesic
Acetaminophen Tylenol Benefits |
reduce risk of ulcers
fewer renal side E does not diminish platelet aggregation can be used in preggers |
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Non-opiate Analgesic
Acetaminophen Tylenol Toxicity |
renal - long term low dose
hepatic necrosis WITH ETOH GSH saturated; NAPB builds up; Mercaptopuric Acid normal metabolite |
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Lipoxygenase Pathway
Zileuton Mech |
inhib 5-lipoxygenase
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Lipoxygenase Pathway
Zileuton Use |
persistent asthma
esp if sensitive to aspirin |
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Lipoxygenase Pathway
Zileuton Features |
orally
inhib P450 enz, dec. metab of other drugs (terfenadine theophilline) |
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Lipoxygenase Pathway
Montekulast Mech |
antag to LTD4 receptors
orally |
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Lipoxygenase Pathway
Montekulast Use |
presistent asthma
alternate to inhaled glucocorticoids headaches and elevated hepatic enz side E |
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SUMMARY OF MECH
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END OF LECUTRE P 190-4
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