Fun 1 Flashcards

0
Q

Epoprostenol

A

PGI2
Treat primary pulmonary hypertension (vasodilator; platelet inhibitor)
Increases cAMP –> decreased calcium
Continuous IV infusion

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1
Q

Alprostadil

A

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

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2
Q

Treprostinil

A

PGI2
Treat primary pulmonary hypertension (vasodilator; platelet inhibitor)
Subcutaneous administration (longer half-life than epoprostenol)

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3
Q

Latanoprost

A

PGF2a
Treat open-angle glaucoma (increase outflow of aqueous humor)
Topical administration (drops once daily)
Increases melanization of iris and lashes

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4
Q

Misoprostol

A

PGE1
1) Minimize GI bleeding and ulceration
Only oral PG preparation
2) Expel blastocyst in pregnant women

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5
Q

Carboprost

A

PGFa2
IM injection
Produce uterine contractions to induce abortion and limit postpartum hemmorhage
Higher risk of inducing arrythmia than dinoprostone

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6
Q

Dinoprostone

A

PGE2
Vaginal suppository
Induce uterine contractions
Prepare cervix for dilationy

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7
Q

Zafirlukast

A

Leukotriene receptor antagonist
Treat asthma and airway inflammation
Effective after three days
Maximal effects may take weeks to months

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8
Q

Montelukast

A

Leukotriene receptor antagonist
Treat asthma and airway inflammation
Maximal effects may take weeks to months

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9
Q

Zileuton

A

5-lipoxygenase inhibitor
Treat asthma
Administered four times daily

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10
Q

Aspirin

A

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

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11
Q

Acetaminophen

A

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)

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12
Q

Acetylcysteine

A

Substitutes for glutathione in liver

Treats acetaminophen toxicity

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13
Q

Indomethacin

A

NSAID
Non-selective competitive COX inhibitor
Use now restricted to acute gout treatment

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14
Q

Ibuprofen

A

NSAID

Low bleeding incidence

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15
Q

Naproxen

A

NSAID

Slightly higher bleeding risk than ibuprofen

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16
Q

Diclofenac sodium

A

NSAID

Accumulates in synovial fluid - arthritis treatment

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17
Q

Ketorolac

A

NSAID

IM injection

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18
Q

Celecoxib

A

NSAID
Selective COX-2 antagonist
Increased risk of thrombosis and MI (Loss of PGI2 but normal TXA2)

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19
Q

Piroxicam

A

NSAID

Decreases PMN migration and lymphocyte activation

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20
Q

Methotrexate

A

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

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21
Q

Glucocorticoids

A

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

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22
Q

Infliximab

A

DMARD
TNFa antibody
Reduces plasma TNFa level
IV injection every 1-3 months

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23
Q

Adalimumab

A

DMARD

TNFa antibody

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24
Q

Etanercept

A

DMARD
Fusion protein of TNFa receptor and IgG Fc i.e. floating receptor
SC injection twice a week

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25
Q

Abatcept

A

DMARD
CTLA4 antibody
Blocks T cell co-stimulatory signal of CD28-CD86 (specifically blocks CD86 on APC from binding to CD28 on T cell)

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26
Q

Rituximab

A

DMARD
CD20 antibody
Blocks B cell co-stimulatory pathway

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27
Q

Anakinra

A

DMARD

IL-1 receptor antagonist

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28
Q

Rilonacept

A

DMARD

Soluble IL-1 receptor

29
Q

Leflunomide

A

DMARD
Reduces rUMP levels in lymphocytes (blocks cell cycle)
Not commonly used

30
Q

Azathioprine

A
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
31
Q

Hydroxychloroquine

A
DMARD/Anti-malarial
Unknown MOA
Requires 6 months to show effect
No bone marrow suppression
Not commonly used
32
Q

Sulfasalazine

A

DMARD
Unknown MOA
Can cause hypersensitivity to sulfas

33
Q

Ondansetron

A

Anti-migraine/Anti-emetic

Control acute migraine symptoms

34
Q

Sumatriptan

A
Anti-migraine
5HT1 agonist (vasoconstriction of cerebral vessels)
Acute treatment (use as soon as possible after migraine onset)
35
Q

Zolmitriptan

A

Anti-migraine
5HT1 agonist
Acute treatment

36
Q

Ergotamine

A

Anti-migraine
5HT1 agonist (less selective than triptans; largely replaced)
Acute treatment

37
Q

Propranolol

A

Beta-blocker (may act through 5HT2 receptor)

Migraine prophalaxis

38
Q

Amitriptyline

A

Anti-depressant

Migraine prophalaxis

39
Q

Verapamil

A

Calcium channel blocker

Migraine prophalaxis

40
Q

Topiramate

A

Anti-seizure
Migraine prophalaxis
Increases GABA (inhibitory) channel activity; Inhibits glutamate (excitatory)

41
Q

Methysergide

A

5HT agonist

Migraine prophalaxis

42
Q

Colchine

A

Anti-gout
Decreases neutrophil migration (Disrupts microtubules)
Low doses can be used as prophylactic

43
Q

Prednisone

A

Glucocorticoid
Anti-gout (anti-inflammatory)
Acute treatment

44
Q

Probenecid

A

Anti-gout
Decreases reabsorption of urate
Should be given with lots of water and IV isotonic sodium bicarbonate (prevent precipitation of urate crystals)

45
Q

Sulfinpyrazone

A

Anti-gout
Blocks resorption of urate
Should be given with lots of water and IV isotonic sodium bicarbonate (prevent precipitation of urate crystals)

46
Q

Allopurinol

A
Anti-gout
Chronic treatment
Prevents urate formation
Metabolite inhibits xanthine oxidase
Interacts with azathioprine (decreases metabolism)
47
Q

Febuxostat

A
Anti-gout
Chronic treatment
Decreases urate formation
Non-purine inhibitor of xanthine oxidase
Better tolerated than allopurinol
Interacts with azathioprine
48
Q

Rasburicase

A

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

49
Q

Cyclosporine

A

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

50
Q

Tacrolimus

A

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

51
Q

Sirolimus

A
Inhibits TOR protein kinase
Blocks T-cell proliferation
Oral
Liver metabolism
Prophylaxis for acute renal transplant rejection (in combo with cyclosporine and glucocorticoids)
52
Q

Mycophenolate Mofetil

A

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)

53
Q

Daclizumab

A

Anti-IL-2 receptor
Acts on activated, not resting T cells
Prophylaxis of acute organ rejection

54
Q

Enfuvirtide

A

Fusion inhibitor

Binds to gp41 (prevents hairpin)

55
Q

Zidovudine

A

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)

56
Q

Lamivudine

A

NRTI

Also used for Hep B

57
Q

Emtricitabine

A

NRTI

58
Q

Tenofovir

A

NRTI
First nucleoTide RTI
Also used for Hep B

59
Q

Nevirapine

A

nNRTI (do not require activation; not incorporated into DNA)
Prevents maternal transmission
Can cause life-threatening skin rashes

60
Q

Efavirenz

A

nNRTI

Long half life (50 hours)

61
Q

Raltegravir

A

Integrase inhibitor

62
Q

Saquinavir

A
Protease inhibitor
Can crystallize (avoid by drinking lots of water)
63
Q

Ritonavir

A

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

64
Q

Acyclovir

A

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

65
Q

Valacyclovir

A

Anti-HSV and varicella-zoster

Higher absorption than acyclovir; rapidly converted to acyclovir

66
Q

Ganciclovir

A

Anti-CMV
IV administration for CMV retinitis in AIDS patients
Can cause myelosuppresion

67
Q

Foscarnet

A

Anti-CMV
Used when resistance for ganciclovir exists
Does not need activation
Lots of side effects (renal dysfunction, severe hypocalcemia, and chromosomal damage)

68
Q

Zanamivir

A

Anti-influenza

Inhibits viral neuraminidase (Prevents release of virus from host cell)

69
Q

Oseltamivir

A

Anti-influenza

Inhibits viral neuraminidase (Prevents release of virus from host cell)

70
Q

Interferon alpha (pegylated)

A

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

71
Q

Ribavirin

A

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