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
Rilonacept
DMARD
Soluble IL-1 receptor
Leflunomide
DMARD
Reduces rUMP levels in lymphocytes (blocks cell cycle)
Not commonly used
Azathioprine
Prodrug converted to 6-mercaptopurinol Prevents purine synthesis --> Nucleic acid synthesis inhibitor Organ transplant (with cyclosporine and glucocorticoids) DMARD (not common; must be non-pregnant) Oral Bimodal metabolism Interacts with allopurinol High incidence of infection/malignancy
Hydroxychloroquine
DMARD/Anti-malarial Unknown MOA Requires 6 months to show effect No bone marrow suppression Not commonly used
Sulfasalazine
DMARD
Unknown MOA
Can cause hypersensitivity to sulfas
Ondansetron
Anti-migraine/Anti-emetic
Control acute migraine symptoms
Sumatriptan
Anti-migraine 5HT1 agonist (vasoconstriction of cerebral vessels) Acute treatment (use as soon as possible after migraine onset)
Zolmitriptan
Anti-migraine
5HT1 agonist
Acute treatment
Ergotamine
Anti-migraine
5HT1 agonist (less selective than triptans; largely replaced)
Acute treatment
Propranolol
Beta-blocker (may act through 5HT2 receptor)
Migraine prophalaxis
Amitriptyline
Anti-depressant
Migraine prophalaxis
Verapamil
Calcium channel blocker
Migraine prophalaxis
Topiramate
Anti-seizure
Migraine prophalaxis
Increases GABA (inhibitory) channel activity; Inhibits glutamate (excitatory)
Methysergide
5HT agonist
Migraine prophalaxis
Colchine
Anti-gout
Decreases neutrophil migration (Disrupts microtubules)
Low doses can be used as prophylactic
Prednisone
Glucocorticoid
Anti-gout (anti-inflammatory)
Acute treatment
Probenecid
Anti-gout
Decreases reabsorption of urate
Should be given with lots of water and IV isotonic sodium bicarbonate (prevent precipitation of urate crystals)
Sulfinpyrazone
Anti-gout
Blocks resorption of urate
Should be given with lots of water and IV isotonic sodium bicarbonate (prevent precipitation of urate crystals)
Allopurinol
Anti-gout Chronic treatment Prevents urate formation Metabolite inhibits xanthine oxidase Interacts with azathioprine (decreases metabolism)
Febuxostat
Anti-gout Chronic treatment Decreases urate formation Non-purine inhibitor of xanthine oxidase Better tolerated than allopurinol Interacts with azathioprine
Rasburicase
Urate metabolism
Urate oxidase enzyme from aspergillus (metabolizes urate into more soluble metabolite)
Used in patients undergoing chemotherapy and tumor lysis
Antibodies will form because it is a foreign protein
Cyclosporine
Calcineurin inhibitor
Blocks IL-2 expression (prevents dephosphorylation of NF-AT)
Oral and IV
Liver metabolism
Renal toxicity, hypertension, neurological effects and increased risk of infection/malignancy
Used for organ transplants, severe RA and dermatology
Tacrolimus
Calcineurin inhibitor
Blocks IL-2 expression (prevents dephosphorylation of NF-AT)
Oral
Liver metabolism
Renal toxicity, hypertension, neurological effects and increased risk of infection/malignancy
Used for organ transplants, severe RA and dermatology
Sirolimus
Inhibits TOR protein kinase Blocks T-cell proliferation Oral Liver metabolism Prophylaxis for acute renal transplant rejection (in combo with cyclosporine and glucocorticoids)
Mycophenolate Mofetil
Inhibits IMP dehydrogenase (blocks de novo DNA synthesis)
Selectively suppresses lymphocyte proliferation
Prevents leukocyte recruitment (loss of GTP prevents glycosylation of cell adhesion molecules)
Oral; high F
GI/hematologic toxicity; increased infection
Prophylaxis for transplant rejection (with cyclosporine and glucocorticoids)
Daclizumab
Anti-IL-2 receptor
Acts on activated, not resting T cells
Prophylaxis of acute organ rejection
Enfuvirtide
Fusion inhibitor
Binds to gp41 (prevents hairpin)
Zidovudine
Prototype NRTI
Prodrug activated and incorporated into nascent DNA (no 3’ OH, preventing chain elongation)
Suicide inhibitor
Oral
Liver metabolism; kidney excretion
Myelosuppression (blocks mitochondrial DNA pol.)
Avoid probenecid and drugs affecting liver metabolism (increases blood concentration)
Lamivudine
NRTI
Also used for Hep B
Emtricitabine
NRTI
Tenofovir
NRTI
First nucleoTide RTI
Also used for Hep B
Nevirapine
nNRTI (do not require activation; not incorporated into DNA)
Prevents maternal transmission
Can cause life-threatening skin rashes
Efavirenz
nNRTI
Long half life (50 hours)
Raltegravir
Integrase inhibitor
Saquinavir
Protease inhibitor Can crystallize (avoid by drinking lots of water)
Ritonavir
Protease inhibitor
Many drug-drug interactions (inhibits and induces P450 enzymes)
Boosts other protease inhibitors (blocks CYP3A4 - degrades protease inhibitors)
Causes HIV lipodystrophy, spontaneous bleeding in hemophiliacs
Acyclovir
Anti-HSV and varicella-zoster
Prodrug activated by viral thymidine kinase (highly specific)
Inhibits viral DNA pol. and causes chain termination
Resistance in immunocompromised patients
Oral; IV for severe cases
Rarely can cause renal dysfunction and encephalopathy
Renal clearance
Valacyclovir
Anti-HSV and varicella-zoster
Higher absorption than acyclovir; rapidly converted to acyclovir
Ganciclovir
Anti-CMV
IV administration for CMV retinitis in AIDS patients
Can cause myelosuppresion
Foscarnet
Anti-CMV
Used when resistance for ganciclovir exists
Does not need activation
Lots of side effects (renal dysfunction, severe hypocalcemia, and chromosomal damage)
Zanamivir
Anti-influenza
Inhibits viral neuraminidase (Prevents release of virus from host cell)
Oseltamivir
Anti-influenza
Inhibits viral neuraminidase (Prevents release of virus from host cell)
Interferon alpha (pegylated)
Anti-Hepatitis B and C
Induces anti-viral pathways
SC or IM administration
Cleared by liver and kidney (pegylation increases half-life tenfold)
Side effects: acute flu-like symptoms, neurotoxicity and myelosuppression
Administered with ribavirin and/or protease inhibitor for Hep C
Ribavirin
Anti-Hepatitis C
Prodrug affects nucleotide metabolism when activated
Aerosol for RSV; oral for Hep C (in combination with interferon alpha)
Teratogen - avoid in pregnant adults
