Chemotherapy

Question 1

What are the targets of antibiotics?

Answer 1

Damaging cell wall, inhibitors of protein synthesis and inhibitors of RNA/DNA

Question 2

How do drugs damage the cell wall?

Answer 2

cell wall synthesis inhibitors or drugs that damage cell membranes

Question 3

How do drugs inhibit RNA?

Answer 3

inhibit RNA polymerase

Question 4

How do drugs inhibit protein synthesis?

Answer 4

ribosomal inhibitors

Question 5

How do drugs inhibit DNA?

Answer 5

inhibit purine synthesis, inflict DNA damage or inhibit DNA gyrase

Question 6

What type of drug are drugs that inhibit cell wall growth?

Answer 6

bacteriocidial

Question 7

What are the four steps of cell wall synthesis?

Answer 7

1. construction on peptidoglycan
2. transport pg to outer membrane
3. link pg end to end to form a row
4. joining of pg rows up

Question 8

What are the classes of drugs that inhibit cell wall synthesis?

Answer 8

beta-lactams, penicillins, cepthlaosporins, and carabanems

Question 9

How does penicillin inhibit cell wall synthesis?

Answer 9

Binds to transpeptidase binds to beta-lactam on penicillin and cannot form cross links and causes cell lysis

Question 10

Why are gram negative bacteria harder to treat than gram positive?

Answer 10

They have a thick layer of peptidoglycan to get the drugs through

Question 11

What property is needed by drugs to treat CNS?

Answer 11

lipophilic

Question 12

What are the mechanism of antiungal drugs?

Answer 12

damage cell wall or membrane- cell wall synthesis inhibitors or ergosterol inhibitors

Question 13

What is ergosterol?

Answer 13

found in cell membrane instead of cholesterol-disrupts cell membrane and cell lysis

Question 14

How do we target ergostrol?

Answer 14

target CYP450

Question 15

What are the class of drugs that inhibit CYP450 and a common brand name?

Answer 15

azoles, clotrimazole-Canasten

Question 16

What is the main concern of using azoles?

Answer 16

Drug interactions because of CYP450

Question 17

Why are we not worried about canasten and drug interactions?

Answer 17

Topical administered reactions so no interactions

Question 18

How do you target viruses>

Answer 18

Target life cycle

Question 19

What is the life cycle of HIV?

Answer 19

1. binding to CCR5 receptor
2. reverse transcriptase to transcribe DNA from RNA
3. integrase is then used to integrate HIV DNA into host genome
4. proteases chop up virsues to form mature virion

Question 20

What drug targets fusion?

Answer 20

Maraviroc-antagonist of CCR5, for last resort

Question 21

What classes of drugs targets reverse transcriptase?

Answer 21

nucleoside RTI
nucleotide RTI
Non-nucleoside RTI

Question 22

What are the nucleoside RTI?

Answer 22

emtricitabine

Question 23

What are the nucleotide RTI

Answer 23

tenofovir

Question 24

What are the non nucleoside RTI

Answer 24

Rilpirivine-first drug

Question 25

What is the drug that targets integrase?

Answer 25

Bictegravir

Question 26

What drug targets the reassembly/maturity step?

Answer 26

Darunavir

Question 27

Why don't we use protease inhibitors as much?

Answer 27

More toxic effects to humans-hyperglycemia, hyperlipidemia (aka cardiovascular disease)

Question 28

What are the common combinations of HAART?

Answer 28

nnRTI + nRTI (2) Integrase inhibitor + nRTI (2) PI + nRTI (2)

Question 29

What is the most common cause of resistance?

Answer 29

adherence

Question 30

What is meant by a 'booster' drug in HIV combos?

Answer 30

inhibitors of CYP450 to mediate elimination

Question 31

What are common boosters?

Answer 31

Cobicistat or ritonavir

Question 32

What are the common side effects of HIV drugs?

Answer 32

rash, GI

Question 33

What are the hallmarks of cancer cells?

Answer 33

invasion and metastases, uncontrolled proliferations, establishment of vascular supply and enhanced survival instinct

Question 34

What are the original cancer drugs and how do they work?

Answer 34

cytotoxic agents that target rapidly dividing cells-mitosis or DNA

Question 35

What drugs target mitosis and how do they work?

Answer 35

microtubule inhibitors-binds beta tubulin and prevents mitosis from occuring

Question 36

What are the side effects that come from cytotoxic drugs?

Answer 36

hair loss, anemia, immune loss, and GI issues

Question 37

What specific receptor are targeted by newer chemo drugs?

Answer 37

Tyrosine kinase

Question 38

What drug targets a receptor and what is the receptor?

Answer 38

osimertinib and targets epidermal growth factor receptor

Question 39

What is the drawback of targeting growth factor inhibitors?

Answer 39

shrink cancer but doesn't cure them, but just prolongs life

Question 40

How does stopping the establishment of vasculature help stop cancer?

Answer 40

Inhibit angiogenesis

Question 41

What is a type of drug inhibits angiogenesis and what does it inhibit?

Answer 41

Bevacizumab- vascular endothelial growth factor

Question 42

How does targeting the survival instinct help treat cancer?

Answer 42

block bh2 and bax which stops apoptosis through binding BH3

Question 43

What is an example of a drug that stops bh2?

Answer 43

Venetoclax

Question 44

What drugs target DNA repair?

Answer 44

PARP inhibitors poly(adp-ribose)-olaparib

Question 45

How do cancer cells evade immune system?

Answer 45

PD binds T cells and kills T cells

Question 46

What drug targets PD-1?

Answer 46

Pembrolizumab

Question 47

What are some common mechanism of resistance?

Answer 47

creating more enzyme, changing shape of enzyme, alter shape of ribosomal binding site, prevent entry of drug of cell or efflux pumps, or create enzyme to break down drugs

Question 48

What is a common enzyme that breaks down a common antibiotic?

Answer 48

beta-lactamase that attacks penicillin

Question 49

How do we target the penicillin resistance?

Answer 49

Pair drug with clavulanate and protect beta-lactam group

Question 50

What is the last resort antibiotic?

Answer 50

colistin

Question 51

What are the two future directions?

Answer 51

Disarming the bug-like targeting alpha hemolysin slowing resistance- target the proteins that Nanoparticless phage therapy

Question 52

How does phage therapy work?

Answer 52

Infect bacteria using phages to alter the part of the bacteria that helps aid in resistance (i.e. efflux pumps)