Drug List 4: Eicosanoids & Leukotrienes Flashcards
prostaglandin E1 (PGE1)
Class: endogenous eicosanoid
mech: EP R agonist
Indication: erectile dysfunction, maintain patent ductus arteriosus
effect: vasodilation, inhibit platelet aggregation
SE: apnea, bradycardia, hypotension, hypercapnia
prostaglandin D2 (PGD2)
class: Endogenous eicosanoid
mech: DP1 & DP2/CRTH2 R agonist
Ind: –
effect: vasodilation, plasma exudation, chemotaxis, inflammation, bronchoconstriction, sleep
SE: –
prostaglandin E2 (PGE2)
class: endogenous eicosanoid
mech: EP R agonist
Ind: facilitate labor/induce abortion, (*better than PG-F)
effects: inhibit ADH & natriuresis; vasodilate, inflammation
SE: fever, GI cramps, diarrhea
prostaglandin I2 (PGI2) * aka: prostacyclin
class: endogenous eicosanoid
mech: IP R agonist
Ind: primary pulm. HTN, heparin substitute
Effects: vasodilation, inhibit platelet aggregation
SE: flushing, headache, hypotension, nausea, diarrhea
prostaglandin F2a (PGf2a)
class: endogenous eicosanoid
mech: FP R agonist
Ind: facilitate labor/induce abortion (2nd choice drug)
Effects: non-vascular sm. muscle contraction (uterus), vasoconstriction
SE: bronchoconstriction, nausea, vomiting, diarrhea
carboprost
class: synthetic PGF analog
mech: FP R agonist (mimics PG-F, but longer lasting)
Ind: postpartum hemorrhage, induce abortion
Effects: oxytocic
SE: vomiting, diarrhea, bronchoconstriction
thromboxane A2 (TXA2)
class: endogenous eicosanoid
mech: TP R agonist
ind: – (not a Tx)
effects: vasoconstriction, bronchoconstriction, stimulate platelet aggregation
Leukotriene B (LTB4)
class: endogenous eicosanoid
mech: LT R agonist
Ind: — (not a Tx)
effects: chemotaxis & recruitment of inflammatory cells
cysteinyl leukotrienes (LTs C/D/E)
class: endogenous eicosanoid
mech: cysLT R agonist, activates PLC
Ind: – (not a Tx)
effects: bronchoconstriction, increase capillary permeability
iloprost
Class: synthetic prostaglandin
mech: mimcs PGI (IP R agonist)
Ind: pulmonary HTN
effects: vasodilation, inhibits platelet aggregation
SE: flushing, headache, hypotension, nausea, vomiting
misoprostol
class: synthetic prostaglandin
mech: mimics PGE2 (EP R agonist)
Ind: prevent ulcers, induce abortion
Effects: increase gastric cytoprotection, oxytocic
SE: fever, GI cramps, diarrhea
latanoprost
class: synthetic prostaglandin Mech: mimics PGF2a (FP R agonist) Ind: ocular HTN, glaucoma effects: reduce IOP SE: pigmentation, irritation/inflammation, eyelash growth
bimatoprost
class: synthetic prostaglandin Mech: mimics PGF2a (FP R agonist) Ind: ocular HTN, glaucoma Effects: reduce IOP SE: pigmentation, irritation/inflammation, eyelash growth
NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)
class: NSAID
mech: inhibit COX
Ind: inflammation, pain, fever
Effects: decrease inflammation, pain, & fever
SE: may cause ulcers, fluid retention –> weight gain & arterial HTN, increase risk of CV thrombotic events
Aspirin (ASA)
class: PG synthesis inhibitor
mech: COX1/2 inhibitor
Ind: heart attack prophylaxis (only baby size), decrease risk thrombosis, reduce inflammation
Effects: decrease inflammation, decrease pain
SE: Reye’s syndrome, + others (like NSAIDs)
ibuprofen
Class: PG synthesis inhibitor
Mech: COX1/2 inhibitor
Ind: inflammation, fever, pain
Effects: decrease Sx (inflamm, pain, fever)
SE: ulcers, weight gain (H2O retention), arterial HTN, increased risk CV thrombotic events
celecoxib
Class: PG synthesis inhibitor ("Coxib") mech: COX2 inhibitor, ~selective! Ind: inflamm, pain, fever Effects: decrease inflamm & pain SE: allergic rxn if sensitive to sulfonamides, NSAID SEs
acetominophen
class: weak PG inhibitor Mech: COX3 inhibitor (not useful for humans) Ind: inflammation, fever/pain Effects: decrease inflamm, pain, fever SE: liver toxicity risk if EtOH abuse
glucocorticoids
class: –
mech: steroid anti-inflamm. agent
Ind: inflammation (only)
effects: many.
SE: many.
Zilueton
Class: leukotriene synthesis inhibitor, aka: anti-leutoktriene agent
mech: blocks 5-LOX
Ind: asthma prophylaxis
Effects: decrease bronchoconstriction (from asthma)
SE: possible liver toxicity
zafirlukast
Class: leukotriene antagonist/anti-leukotriene agent
Mech: blocks CYSLT-1 R
Ind: asthma prophylaxis
Effects: decrease bronchocostriction (from asthma)
SE: –
lubiprostone
class: synthetic prostaglandin analogue
Mech: CIC-2 (chloride channel agonist)
Ind: idiopathic constipation, IBS w/ constipation
Effects: increase chloride efflux & fluid secretion into GI lumen, soften stools
SE: nausea, diarrhea