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
Etanercept
DMARD Fusion protein of TNFa receptor and IgG Fc i.e. floating receptor SC injection twice a week
25
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)
26
Rituximab
DMARD CD20 antibody Blocks B cell co-stimulatory pathway
27
Anakinra
DMARD | IL-1 receptor antagonist
28
Rilonacept
DMARD | Soluble IL-1 receptor
29
Leflunomide
DMARD Reduces rUMP levels in lymphocytes (blocks cell cycle) Not commonly used
30
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 ```
31
Hydroxychloroquine
``` DMARD/Anti-malarial Unknown MOA Requires 6 months to show effect No bone marrow suppression Not commonly used ```
32
Sulfasalazine
DMARD Unknown MOA Can cause hypersensitivity to sulfas
33
Ondansetron
Anti-migraine/Anti-emetic | Control acute migraine symptoms
34
Sumatriptan
``` Anti-migraine 5HT1 agonist (vasoconstriction of cerebral vessels) Acute treatment (use as soon as possible after migraine onset) ```
35
Zolmitriptan
Anti-migraine 5HT1 agonist Acute treatment
36
Ergotamine
Anti-migraine 5HT1 agonist (less selective than triptans; largely replaced) Acute treatment
37
Propranolol
Beta-blocker (may act through 5HT2 receptor) | Migraine prophalaxis
38
Amitriptyline
Anti-depressant | Migraine prophalaxis
39
Verapamil
Calcium channel blocker | Migraine prophalaxis
40
Topiramate
Anti-seizure Migraine prophalaxis Increases GABA (inhibitory) channel activity; Inhibits glutamate (excitatory)
41
Methysergide
5HT agonist | Migraine prophalaxis
42
Colchine
Anti-gout Decreases neutrophil migration (Disrupts microtubules) Low doses can be used as prophylactic
43
Prednisone
Glucocorticoid Anti-gout (anti-inflammatory) Acute treatment
44
Probenecid
Anti-gout Decreases reabsorption of urate Should be given with lots of water and IV isotonic sodium bicarbonate (prevent precipitation of urate crystals)
45
Sulfinpyrazone
Anti-gout Blocks resorption of urate Should be given with lots of water and IV isotonic sodium bicarbonate (prevent precipitation of urate crystals)
46
Allopurinol
``` Anti-gout Chronic treatment Prevents urate formation Metabolite inhibits xanthine oxidase Interacts with azathioprine (decreases metabolism) ```
47
Febuxostat
``` Anti-gout Chronic treatment Decreases urate formation Non-purine inhibitor of xanthine oxidase Better tolerated than allopurinol Interacts with azathioprine ```
48
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
49
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
50
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
51
Sirolimus
``` Inhibits TOR protein kinase Blocks T-cell proliferation Oral Liver metabolism Prophylaxis for acute renal transplant rejection (in combo with cyclosporine and glucocorticoids) ```
52
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)
53
Daclizumab
Anti-IL-2 receptor Acts on activated, not resting T cells Prophylaxis of acute organ rejection
54
Enfuvirtide
Fusion inhibitor | Binds to gp41 (prevents hairpin)
55
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)
56
Lamivudine
NRTI | Also used for Hep B
57
Emtricitabine
NRTI
58
Tenofovir
NRTI First nucleoTide RTI Also used for Hep B
59
Nevirapine
nNRTI (do not require activation; not incorporated into DNA) Prevents maternal transmission Can cause life-threatening skin rashes
60
Efavirenz
nNRTI | Long half life (50 hours)
61
Raltegravir
Integrase inhibitor
62
Saquinavir
``` Protease inhibitor Can crystallize (avoid by drinking lots of water) ```
63
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
64
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
65
Valacyclovir
Anti-HSV and varicella-zoster | Higher absorption than acyclovir; rapidly converted to acyclovir
66
Ganciclovir
Anti-CMV IV administration for CMV retinitis in AIDS patients Can cause myelosuppresion
67
Foscarnet
Anti-CMV Used when resistance for ganciclovir exists Does not need activation Lots of side effects (renal dysfunction, severe hypocalcemia, and chromosomal damage)
68
Zanamivir
Anti-influenza | Inhibits viral neuraminidase (Prevents release of virus from host cell)
69
Oseltamivir
Anti-influenza | Inhibits viral neuraminidase (Prevents release of virus from host cell)
70
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
71
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