Term
| What are the receptors that PGs and PCs bind, and what are their function? |
|
Definition
Relaxant: Gs>^cAMP
Contractile: Gq>^CA
Inhibiting: Gi>decreased cAMP |
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Term
| What are the receptors bound by leukotrienes, and what are their functions? |
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Definition
B-LT1: Gi>chemotactic response
B-LT2: Gq>neutrophil secretion
CysLT1: airway sm muscle (bronchoconstriction) & vasc endothel (^ cell adhesion molecules) |
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Term
| How do PGs protect the gastric mucosa? |
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Definition
| They stimulate mucus production, increase blood flow, and inhibit acid secretion |
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Term
| What are the effects of LTs? |
|
Definition
decreased myocardial contractility
decreased coronary blood flow
attract neutrophils to GI tract
bronchoconstriction of airways, ^ microvasc perm and plasma exudate, mucus secretion |
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Term
|
Definition
intiate/stimulate labor
protect gastric mucosa
activate sm muscle
induce contraction of longitudinal muscles
relax resp smooth musces (airway dilation) |
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Term
|
Definition
| they go to periph sensory neurons & central sites within the SC and brain > activate prostanoid receptors |
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Term
| What is the MOA of acetylsalicyclic acid, and what is it used for? |
|
Definition
irrev inhibits COX by acetylating serine residue in active site
analgesic
antipyretic
prevent heart attack
stroke
TIA
angina
anti-inflamm at high (325-600mg) doses
long term @ low doses: lower incidence of colon cancer |
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Term
| What is the MOA of Celebrex and what is it used for? |
|
Definition
COX 2 specific inhibitor
used for chronic inflamm states (RA, osteopathies) and gastroprotection |
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Term
|
Definition
5-LO inhibitor
used for long term asthma control |
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Term
|
Definition
CysLT1 receptor antagonists
used for long term asthma control |
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Term
|
Definition
synthetic PGE2 (gel, suppository, or controlled release formulation)
used for induction of labor (uterine contractions and softens cervic) or pregnancy termination |
|
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Term
|
Definition
synthetic PGE1
used for ulcer treatment, but not recommended in US due to AEs; used in Europe |
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Term
|
Definition
PGF2a derivative
used for glaucoma (decreases intraocular pressure by decreasing aqueous humor production) |
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Term
|
Definition
prostacyclin
vasodilator used for pulmonary hypertension |
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Term
|
Definition
PGF2 analogue
used for abortion in the 2nd trimester, or post-partum hemorrhage |
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Term
| What are the 2 types of adaptive pain? |
|
Definition
| nocioceptive and inflammatory |
|
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Term
| What are the 2 types of maladaptive pain? |
|
Definition
neuropathic: damage to PNS or CNS
functional: abn responsiveness or fxn of the nervous system |
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Term
| What are the properties of NSAIDs? |
|
Definition
analgesic: blocks PGE2 production, which normally sensitizes nerve endings to chemical mediators at inflamm site
anti-inflamm: decreases PG production so prevents vasodilation and PCV permeability
antipyretic: reduces fever due to increased PG levels in hypothal thermoregulatory areas |
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Term
| What are the pharmacokinetics of aspirin? |
|
Definition
a weak acid that is readily absorbed from the stomach or SI
it is widely distributed in all tissues
it is bound to plasma proteins and can displace other drugs (^ toxicity)
acetylates albumin
deacylated in liver and plasma
pH dependent urinary excretion |
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Term
| What are the AEs of aspirin? |
|
Definition
GI upset (bleeding, ulceration, perforation)
hypersensitivity-like reactions
viral illnesses can lead to Reye's syndrome
salicyclism (sweating, vomiting, epigastric pain, tinnitus, blurred vision)
acid base imbalance
anticoag
renal failure
gout |
|
|
Term
| Ibuprofen (motrin, advil, naproxen) |
|
Definition
equal to aspirin in pain relief but lower frequency of GI irritation
anti-inflamm: 2400mg/day
lower doses: analgesic
cross allergy w/aspirin
used for: RA, OA, patent ductus arteriosus |
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Term
|
Definition
very potent COX inhib (significant GI toxicity)
used for mod-severe arthritic pain, gouty arthritis, ankylosing spondylitis, OA of the hip, PDA |
|
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Term
| What 2 NSAIDs are used for Patent Ductus Arteriosus? |
|
Definition
| ibuprofen and indomethacin |
|
|
Term
|
Definition
the only NSAID administered IM
used for mod-severe pain (analgesic potency equal to moderate dose of morphine), NOT used as anti-inflamm
AE: GI upset, renal effects, risk of bleeding (do not use before surgery) |
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Term
| What drug has the analgesic potency similar to a moderate dose of morphine, and how is it administered? |
|
Definition
|
|
Term
|
Definition
selective COX2 inhibitor (does not cause GI damage)
used for OA, RA, management of acute pain in adults, treatment of primary dysmenorrhea, management of FAP (reduces number of polyps)
AE: cardiovascular disease |
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Term
|
Definition
| COX2 inhibitors removed from the market due to significant increase in MIs and sudden death |
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Term
|
Definition
COX III inhibitor???
analgesic, antipyretic, NOT anti-inflamm
AE: metab by ctyP450, large doses deplete glutathione which normally reactis w/metabolite to prevent its toxicity |
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