Fun 1 Flashcards
Epoprostenol
PGI2
Treat primary pulmonary hypertension (vasodilator; platelet inhibitor)
Increases cAMP –> decreased calcium
Continuous IV infusion
Alprostadil
PGE1
1) Maintain patency of ductus arteriosus in congenital heart defects
IV infusion
2) Alleviate ED
Intracavernous injection
Used for patients on nitrates who cannot use Viagra
Treprostinil
PGI2
Treat primary pulmonary hypertension (vasodilator; platelet inhibitor)
Subcutaneous administration (longer half-life than epoprostenol)
Latanoprost
PGF2a
Treat open-angle glaucoma (increase outflow of aqueous humor)
Topical administration (drops once daily)
Increases melanization of iris and lashes
Misoprostol
PGE1
1) Minimize GI bleeding and ulceration
Only oral PG preparation
2) Expel blastocyst in pregnant women
Carboprost
PGFa2
IM injection
Produce uterine contractions to induce abortion and limit postpartum hemmorhage
Higher risk of inducing arrythmia than dinoprostone
Dinoprostone
PGE2
Vaginal suppository
Induce uterine contractions
Prepare cervix for dilationy
Zafirlukast
Leukotriene receptor antagonist
Treat asthma and airway inflammation
Effective after three days
Maximal effects may take weeks to months
Montelukast
Leukotriene receptor antagonist
Treat asthma and airway inflammation
Maximal effects may take weeks to months
Zileuton
5-lipoxygenase inhibitor
Treat asthma
Administered four times daily
Aspirin
Irreversible COX inhibitor
Zero-order kinetics
NSAID prototype
Toxicity treated with sodium bicarbonate (alkalosis reduces absorption)
Risk of GI bleeding
Avoid in patients on anti-coagulants or with clotting disorders
Avoid use in viral infections
Avoid use in CHF/hypovolemic patients
Intolerance can result (Excess shunting to LT synthesis)
Small increase in blood pressure
ASA specifically competes with urate secretion
Acetaminophen
MOA not well understood; Weak COX inhibitor
Not anti-inflammatory or anti-platelet
Liver toxicity - creates toxic oxene metabolite (normally inactivated by glutathione)
Alcohol induces P450 enzyme that creates toxic metabolite
Treat with acetylcysteine (substitutes for glutathione)
Acetylcysteine
Substitutes for glutathione in liver
Treats acetaminophen toxicity
Indomethacin
NSAID
Non-selective competitive COX inhibitor
Use now restricted to acute gout treatment
Ibuprofen
NSAID
Low bleeding incidence
Naproxen
NSAID
Slightly higher bleeding risk than ibuprofen
Diclofenac sodium
NSAID
Accumulates in synovial fluid - arthritis treatment
Ketorolac
NSAID
IM injection
Celecoxib
NSAID
Selective COX-2 antagonist
Increased risk of thrombosis and MI (Loss of PGI2 but normal TXA2)
Piroxicam
NSAID
Decreases PMN migration and lymphocyte activation
Methotrexate
DMARD
First line of RA teratment
AICAR inhibition (AICAR accumulation increases AMP leading to adenosine formation decreasing inflammation)
Avoid in pregnancy (reduces folate, affecting DNA synthesis)
Used before misoprostol to induce abortion
Glucocorticoids
1) DMARD
Blocks arachidonic acid metabolism and production of cytokines
Effective for acute attacks
2) Immunosuppressant for organ transplantation
Decrease expression of pro-inflammatory (IkB) and increase expression of anti-inflammatory (GRE)
Long-term side effects
Infliximab
DMARD
TNFa antibody
Reduces plasma TNFa level
IV injection every 1-3 months
Adalimumab
DMARD
TNFa antibody
Etanercept
DMARD
Fusion protein of TNFa receptor and IgG Fc i.e. floating receptor
SC injection twice a week
Abatcept
DMARD
CTLA4 antibody
Blocks T cell co-stimulatory signal of CD28-CD86 (specifically blocks CD86 on APC from binding to CD28 on T cell)
Rituximab
DMARD
CD20 antibody
Blocks B cell co-stimulatory pathway
Anakinra
DMARD
IL-1 receptor antagonist