Final Exam Drugs

Question 1

Prednisone

Answer 1

Inactive prodrug
Metabolized into prednisolone
Effective oral or intravenous drug
Not very effective topically
Glucocorticoid effects (anti-inflammatory, catabolic effects, etc.)

Question 2

Prednisolone

Answer 2

Active form of prednisone
Effective topical drug
Glucocorticoid effects (anti-inflammatory, immunosuppressive, etc.)

Question 3

Hydrocortisone

Answer 3

Glucocorticoid effects (anti-inflammatory, catabolic effects, etc.)
Used to treat Addison’s disease

Question 4

Cyclosporine

Answer 4

Calcineurin inhibitor
Suppresses IL-2 gene transcription and T cell proliferation/maturation
Binds to Calcineurin as cyclosporine:cyclophilin complex

Question 5

Tacrolimus

Answer 5

Calcineurin inhibitor
Suppresses IL-2 gene transcription and T cell proliferation/maturation
Binds to Calcineurin as tacrolimus:FKBP complex

Question 6

Rapamycin

Answer 6

AKA sirolimus
Proliferation signal inhibitor
Binds to mTOR as FKBP:sirolimus complex
Inhibits mTOR and prevents T cell growth/proliferation

Question 7

Cyclophosphoamide

Answer 7

Alkylating agent (cytotoxic)
Leads to cross linking of neighbouring bases
Interferes with DNA replication in rapidly dividing cells

Question 8

Azathioprine

Answer 8

Cytotoxic agent
Prodrug (metabolized to 6-mercaptopurine)
Fraudulent nucleotide
Inhibits nucleotide synthesis in rapidly dividing cells

Question 9

Alemtuzumab

Answer 9

Humanized IgG1 antibody
Recognizes CD52 receptor on many immune cells
IgG1 Fc domain is recognized by phagocytic immune cells
Leads to T and B cell death by lysis or phagocytosis

Question 10

Basiliximab

Answer 10

Chimeric mouse-human IgG1 antibody
Binds to CD25 (part of IL-2 receptor) and blocks IL-2 signalling
Inhibits proliferation/activation of T cells

Question 11

Levothyroxine

Answer 11

Synthetic thyroxine (T4)
Used for hormone replacement
Treats hypothyroidism

Question 12

Methimazole

Answer 12

Thioamide
Prevents iodination and coupling steps of thyroxine synthesis (inhibits thyroperoxidase)
Used to treat hyperthyroidism

Question 13

Denosumab

Answer 13

Treats osteoporosis
Monoclonal antibody directed against RANKL
Sane mechanism as endogenous osteoprotegerin
Binds RANKL and inhibits bone resorption by osteoclasts

Question 14

Alendronate

Answer 14

Treats osteoporosis
Most commonly prescribed bisphosphonate
High affinity for calcium ions (accumulates in bones)
Inhibits osteoclast resorption of bone through unknown mechanism
Speculated association with glucocorticoids

Question 15

Teriperatide

Answer 15

Treats osteoporosis
Fully active PTH fragment (amino acids 1-34)
Stimulates osteoblasts over osteoclasts using selective dose timing

Question 16

Raloxifene

Answer 16

Estrogen mimetic
Treats osteoporosis in older females

Question 17

Calcitriol

Answer 17

Active metabolite of vitamin D3
Used to treat hypocalcemia caused by a vitamin D deficiency or hypoparathyroidism
Increases calcium ion concentrations by affecting kidneys, bones and gut

Question 18

Warfarin

Answer 18

Anti-coagulant
Inhibits vitamin K epoxidase reductase
Reduces blood clots and raises INR
Inhibited by vitamin K
Metabolized by CYP3A4

Question 19

Penicillin

Answer 19

First antibiotic developed in 1928 by Alexander Fleming
Produced by fungus Penicillium notatum
Beta-lactam that inhibits DD-transpeptidase and bacterial cell wall assembly
Bacteriocidal antibiotic
Only effective against gram positive bacteria

Question 20

Cephalosporins

Answer 20

Produced by fungus Acremonium
Beta-lactam that inhibits DD-transpeptidase and bacterial cell wall assembly
Bacteriocidal antibiotic
Effective against gram positive and gram negative bacteria

Question 21

Calvulanic Acid

Answer 21

Beta-lactamase inhibitor
Given with a beta-lactam to protect it from hydrolysis

Question 22

Vancomycin

Answer 22

Not a beta lactam
Produced by actinobacteria (Amycolatopsis orientalis)
Inhibits peptide cross linking and cell wall assembly

Question 23

Sulfonamides

Answer 23

Competitive antagonist for PABA
Prevents conversion of PABA into dihydrofolic acid
Given in conjunction with trimethoprim

Question 24

Trimethoprim

Answer 24

Competitive antagonist for dihydrofolic acid
Prevents conversion dihydrofolic acid into tetrahydrofolic acid
Given in conjunction with a sulfonamide

Question 25

Chloramphenicol

Answer 25

Binds to 50S subunit of bacterial ribosome Blocks transpeptidation

Question 26

Macrolides

Answer 26

Binds to 50S subunit of bacterial ribosome Blocks transpeptidation

Question 27

Tetracyclines

Answer 27

Binds to 30S subunit of bacterial ribosome Prevents binding of incoming tRNA

Question 28

Aminoglycosides

Answer 28

Binds to 30S subunit of bacterial ribosome Blocks the initiation complex Causes misreading of mRNA Blocks translocation

Question 29

Acyclovir

Answer 29

Nucleoside analog Used as a chain terminator Has to be phosphorylated High affinity for thymidine kinase from Herpes virus

Question 30

Maraviroc

Answer 30

HIV entry inhibitor CCR5 receptor antagonist Interferes with HIV binding to T cells

Question 31

Raltegravir

Answer 31

HIV integrase strand transfer inhibitor Blocks integration of viral genome into host DNA

Question 32

Amantadine

Answer 32

Prophylactive against influenza A Blocks acidification of viral core via M2 channels Inhibits initiation of viral transcription and uncoating

Question 33

Zanamavir

Answer 33

Neuroaminidase inhibitor Prevents cleavage of sialic acid residues from viral proteins Blocks virus from detaching and spreading

Question 34

5-fluorouracil

Answer 34

Pyramiding analogue Anti-cancer drug Converted into FdUMP (active form) Inhibits thymidylate synthase Effective against cells in S phase

Question 35

6-mercaptopurine

Answer 35

Purine analogue Anti-cancer drug Inhibits phosphoribosyl pyrophosphate amidotransferase (PRPP amidotransferase) Effective against cells in S phase

Question 36

Cisplatin

Answer 36

Platinum analogue Alkylating agent Anti-cancer drug Causes inter-strand crosslinks between guanine residues Effective in late G1 and S phase

Question 37

Methotrexate

Answer 37

Folic acid analogue Anti-cancer drug Binds to dihydrofolate reductase Interferes with pyrimidine synthesis Effective during S phase

Question 38

Vinca Alkyloids

Answer 38

Derived from periwinkle plant Anti-cancer drug Inhibit microtubule polymerization Effective during M phase

Question 39

Paclitaxel

Answer 39

Taxane Anti-cancer drug Inhibits microtubule depolymerization Effective during M phase

Question 40

Camptothecins

Answer 40

Anti-cancer drug Inhibit ligation of DNA topoisomerase 1 S phase specific drug

Question 41

Anthracyclines

Answer 41

Doxorubicin Anti-cancer drug Inhibit topoisomerases Generate free radicals (DNA mutagenesis) High binding affinity to DNA Alter fluidity and transport across cell membrane

Question 42

Imantinib

Answer 42

Treatment for leukemia Inhibits tyrosine kinase domain of BCR-ABL1

Question 43

Cetuximab

Answer 43

Anti-cancer drug Monoclonal antibody directed against extracellular portion of EGFR Prevent proliferation signalling

Question 44

Tamoxifen

Answer 44

Treatment for breast cancer Antagonist at estrogen receptor Blocks estrogen binding to estrogen sensitive cancer cells in breast tissue