Drugs

Question 0

Epoprostenol

Answer 0

• PGI2 that vasodilates and inhibits platelet aggregation through GPCRs that increase cAMP
• used in primary pulmonary hypertension
• continuous IV infusion

Question 1

Alprostadil

Answer 1

• PGE1 used to maintain patency of ductus arteriosis in congenital heart defects until surgery
• alleviates ED - topical option available, especially useful in patients taking nitrates that can’t take Viagra
• administered by IV infusion

Question 2

Treprostinil

Answer 2

Newer version of epoprostenol that has longer half life and can be given subcutaneously

Question 3

Latanoprost

Answer 3

• PGF2alpha that increases uveoscleral outflow of aqueous humor
• used in glaucoma
• topical - drops applied once daily
• synergistic effect with beta blockers that decrease synthesis of aqueous humor

Question 4

Misoprostol

Answer 4

• PGE minimizes risk of GI bleeding and ulceration in high risk patients taking NSAIDs
• used to expel blastocyst - do NOT use in pregnant women until inducing labor
• tablet - only oral pg preparation

Question 5

Carboprost

Answer 5

• PGF2alpha used to produce uterine contractions to induce absorption and control postpartum hemorrhage
• higher incidence of arrhythmias than dinoprostone
• intramuscular injection

Question 6

Dinoprostone

Answer 6

• PGE2 - also used to produce uterine contractions to induce abortions and control postpartum hemorrhage
• vaginal suppository - used more than carboprost because less risk of arrhythmia
• also used to prepare cervix for dilation

Question 7

Zafirlukast

Answer 7

• leukotriene receptor antagonist
• for asthma and airway inflammation
• twice daily oral admin
• effective after 3 days but maximal effect may take weeks to months

Question 8

Montelukast

Answer 8

• leukotriene receptor antagonist used for asthma
• approved for children more than 1 year old and adults
• maximal effects may take weeks to months

Question 9

Zileuton

Answer 9

• selective inhibitor of 5-lipoxygenase that blocks leukotriene formation
• approved for asthma but can be used in RA or ulcerative colitis
• administered four times daily
• effective in about two hours

Question 10

Indomethacin

Answer 10

Drug for gout
Non selective cox inhibitor
Older drug used to close patent ductus arteriosus (now use ibuprofen)

Question 11

Propionic acids

Answer 11

NSAIDs - also as analgesics and antipyretics
Ibuprofen
Naproxen

Question 12

Diclofenac sodium

Answer 12

Drug for RA that concentrates in synovial fluid

NSAID

Question 13

Ketorolac

Answer 13

P.o or I.m for postoperative pain

NSAID

Question 14

Cox2 specific agents

Answer 14

Fewer bleeding side effects, risk of thrombosis leading to MI and stroke
Celecoxib
Piroxicam - decreases PMN migration and lymphocyte activation - once a day admin

Question 15

Methotrexate

Answer 15

Therapy for RA
Immunosuppressant
Slows progression of disease
Nausea and mucosal ulcers are common side effects

Question 16

Glucocorticoids

Answer 16

Drug for RA
Prednisone
Blocks production of cytokines, induction of cox2 and production of arachidonic acid
Acutely effective but long term side effects
Prednisone Also used to treat gout

Question 17

Anti TNFalpha agents

Answer 17

Drugs for RA
Infliximab - monoclonal antibody to it
Adalimumab - monoclonal antibody
Etanercept - fusion protein of TNFalpha receptor ligand binding domain with IgG Fc

Question 18

Abatacept

Answer 18

Interrupts T cell co-stimulatory signal through CD28-CD80/CD86 pathway
Drug for RA because T cells mediate RA

Question 19

Rituximab

Answer 19

Anti cd20 monoclonal antibody

Drug for RA

Question 20

Anti IL-1beta drugs

Answer 20

Anakinra - IL 1 receptor antagonist
Rilonacept - soluble IL 1 receptor
Drugs for RA

Question 21

Leflunomide

Answer 21

Reduces rUMP in lymphocytes leading to block of cell cycle progression
Drug for RA

Question 22

Azathioprine

Answer 22

Nucleic acid synthesis inhibitor

Drug for RA

Question 23

Hydroxychloroquine

Answer 23

Drug for RA

Anti inflammatory but doesn’t slow disease progression

Question 24

Sulfasalazine

Answer 24

Drug for RA

Question 25

Colchicine

Answer 25

Drug for gout | Decreases neutrophil migration into joint by disrupting micro tubules

Question 26

Uricosuric agents

Answer 26

Increase excretion of urate by decreasing reabsorption from tubular fluid - used in gout Probenecid - prolongs penicillin by decreasing tubular secretion Sulfinpyrazone Should not be used in conjunction with salicylates

Question 27

Drugs to lower uric acid formation

Answer 27

Allopurinol - Inhibits xanthine oxidase to reduce formation of uric acid Drugs for gout Febuxostat - does the same thing but better tolerated Both have severe drug interaction with azathioprine

Question 28

Rasburicase

Answer 28

Prevents renal failure and reduces need for transfusions in patients with tumor lysis syndrome Drug for gout Antibodies will develop and limit use

Question 29

Prednisone

Answer 29

Prophylactically used before transplant | Used in graft vs host disease

Question 30

Calcineurin inhibitors

Answer 30

Cyclosporine, oral and IV Tacrolimus - 100x more potent, only oral Both hydrophobic - bind to cyclophilins in cytoplasm - inhibition of calcineurin prevents dephosphorylation of NFAT which prevents formation of IL2 Don't affect humoral response Any inducer or inhibitor of c. P450 is a drug interaction Possible risk of nephrotoxicity Used in organ transplantation, RA, and dermatology

Question 31

Sirolimus

Answer 31

Anti-proliferative drug Inhibits mTOR to block T cell response to cytokines and proliferation Oral, metabolized by c.p450 No renal toxicity Used in renal transplant and usually in combo with cyclosporine

Question 32

Mycophenolate mofetil

Answer 32

Anti-proliferative drug Converted to mycophenolic acid by plasma esterases Inhibits IMP dehydrogenase to block de novo purine synthesis - specifically targets lymphocytes Oral, limited drug interactions GI and hematologic toxicity Prophylaxis in transplant rejection

Question 33

Azathioprine (as immunosuppressant)

Answer 33

Anti proliferative drug Converted to 6-Mercaptopurine - inhibits production of purine nucleotides and blocks DNA synthesis Oral admin Combined with cyclosporine and prednisone for suppression of organ rejection High incidence of complications so only used when other drugs don't work

Question 34

Daclizumab

Answer 34

Anti IL2 receptor antibody Binds receptor on activated but not resting T cells Used to prevent organ rejection