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Flashcards in Drugs Deck (32):
1

AZT (azidothymidine)

-nucleoside analogue of thymidine
-anti-viral
-no free 3' OH group = chain termination
-has high affinity for reverse transcriptase
-Treatment for HIV

2

Didanosine (ddl)

-nucleoside analogue of adenosine
-no free 3' OH group = chain termination
-high affinity for reverse transcriptase
-Treatment for HIV

3

Acyclovir

-nucleoside analogue of guanosine
-has an open chains instead of a closed pentose sugar ring
-no free 3' OH group
-viral thymidine kinase = 1st phosphorylation
-Treatment for herpes = only attacks infected cells and does not touch healthy cells because it can only be phosphorylated by viral thymidine kinase which is only in infected cells

4

Tenofovir

-nucleotide analogue of adenosine monophosphate
-open chain instead of pentose sugar ring
-no free 3' OH group = chain termination
-treatment for HIV infections

5

Cytosine arabinoside (araC) aka cytarabine

-nucleoside analogue of cytosine - anti-cancer
-has 3'OH group, but there is a 2' OH group too = steric hinderance!
-chain termination
-treatment for leukemia [myeloid + lymphoma]

6

Adenosine Arabinoside (araA) aka vidarabine

-nucleoside analogue of adenosine - anti-caner
-has 3'OH group, but there is a 2' OH group too = steric hinderance!
-chain termination
-treatment for anti-neoplastic agent, relapsed childhood acute lymphoblastic leukemia and herpes simplex infections

7

Decitabine

-nucleoside analogue of cytidine - hypomethylation agent
-removes a methyl group
-prevent DNA methyltransferase enzymes from methylating cytosine - remember because DNA methylation is an important mechanism of gene regulation euk.
-important for transcriptional regulation
-use as a anti-methylator to counteract cancer cells

8

azacytidine

-nucleoside analogue of cytidine - hypomethylation agent
-removes a methyl group
-prevent DNA methyltransferase enzymes from methylating cytosine - remember because DNA methylation is an important mechanism of gene regulation euk.
-important for transcriptional regulation
-use as a anti-methylator to counteract cancer cells

9

Ciprofloxacin (Quinolone type)

-inhibits topoisomerase II (bacterial DNA gyrase)
-positive supercoils are not unwound
-treatment of respiratory and urinary tract infections and can also be used to treat anthrax

10

Camptothecin

-anti-cancer drug
-binds to and inhibits topoisomerase I = DNA breakage
-inhibits replication

11

Etoposide

-anti-cancer drug
-inhibits the activity of topoisomerase II (DNA gyrase) = DNA breakage
-inhibits replication

12

Actinomycin D (Dactinomycin)

-binds between G-C bases
-inhibits replication by prevent ssDNA and inhibiting RNA transcription
-anti-cancer drug, not normally used as an antibiotic

13

Rifampin

-Antibiotic
-from a strain of streptomycin
-inhibits transcription initiation by blocking the formation of the 1st phosphodiester bond
-RNA polymerase is not affected
-treatment for tuberculosis

14

Amanita Phalloides

-produces alpha amanitin which inhibits RNA polymerase II (mRNA)

15

Novobiocin

-inihibits topoisomerase II (DNA gyrase)
- positive supercoils are not unwound

16

What do Rotenone
piericidine A (bacterial antibiotic)
barbiturate amytal
do?

Inhibit NADH dehydrogenase in Complex I

17

What do CO
Azide
Hydrogen Sulphide (H2S)
Cyanide (CN-)
do?

Inhibit cytochrome oxidase (Complex IV)

18

what does Antimycin A (antibiotic) do?

Inhibits cytochrome b of cytochrome reductase (Complex III)

19

what does Oligomycin (Streptomyces antibiotic) do?

Inhibits ATP synthase (Complex V)

20

what do ETC inhibitors do?

decrease ATP synthesis, decrease ETC and oxygen consumption

21

what does Atractyloside
Bongkrekic Acid
do?

Inhibits ADP/ATP transport; inhibits function of nucleotide translocase

22

what do DNP (dinitrophenol)
ASA (aspirin)
Thermogenin
Ionophores
do?

Destroy the protein gradient

23

what do Ionophores
• Gramicidin = channel formers
• Valinomycin = mobile carrier
do?

Make inner mitochondrial membrane permeable to compounds that can’t usually cross (small molecules now can get through)

24

what do uncouplers do?

decrease ATP synthesis, increase ETC, increase oxygen consumption

25

what do uncouplers and ionophores do?

allow for dissipation of the proton gradient

26

Streptomycin

Family of antibiotics with aminoglycoside structure
Prevents assembly of ribosome by binding to 30S subunit

27

Tetracycline

Family of antibiotics with four (tetra) ring (cyclic) structure
Blocks elongation by binding to 30S subunit and blocking the access of the aminoacyl-tRNA access to the A-site on the mRNA-ribosomal complex

28

Erythromycin (clindamycin)

Family of antibiotics and has macrolide structure
Binds to the 50S subunit of the complete 70S ribosome of bacteria and blocks ribosome translocation

29

Chloramphenicol

nhibits peptidyl transferase activity
May inhibit mitochondrial translation
Not broadly used because potential to develop decrease WBC
Important in some cases – some meningitis conditions

30

Cycloheximide

Inhibits peptidyl transferase activity
May inhibit mitochondrial translation
Toxic to eukaryotes
Prokaryotes and mitochondria not affected
Important experimental tool (cheap)

31

Puromycin

Analog of aminoacyl-tRNA
Toxic to both prokaryotes and eukaryotes translation
It’s a chain terminator in protein synthesis

32

Diphtheria toxin

C. diphtheria + bacterial virus
Causes diphtheria – lethal disease of respiratory tract
The A fragment of the toxin catalyzes the ADP-ribosylation of EF-2 = inhibiting translocation in eukaryotes