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Medical Biochemistry > Drugs > Flashcards

Drugs Flashcards

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USMLE® Step 1 flashcards
1
Q

AZT (azidothymidine)

A
  • nucleoside analogue of thymidine
  • anti-viral
  • no free 3’ OH group = chain termination
  • has high affinity for reverse transcriptase
  • Treatment for HIV
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2
Q

Didanosine (ddl)

A
  • nucleoside analogue of adenosine
  • no free 3’ OH group = chain termination
  • high affinity for reverse transcriptase
  • Treatment for HIV
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3
Q

Acyclovir

A
  • 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
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4
Q

Tenofovir

A
  • nucleotide analogue of adenosine monophosphate
  • open chain instead of pentose sugar ring
  • no free 3’ OH group = chain termination
  • treatment for HIV infections
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5
Q

Cytosine arabinoside (araC) aka cytarabine

A
  • 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]
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6
Q

Adenosine Arabinoside (araA) aka vidarabine

A
  • 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
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7
Q

Decitabine

A
  • 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
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8
Q

azacytidine

A
  • 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
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9
Q

Ciprofloxacin (Quinolone type)

A
  • 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
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10
Q

Camptothecin

A
  • anti-cancer drug
  • binds to and inhibits topoisomerase I = DNA breakage
  • inhibits replication
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11
Q

Etoposide

A
  • anti-cancer drug
  • inhibits the activity of topoisomerase II (DNA gyrase) = DNA breakage
  • inhibits replication
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12
Q

Actinomycin D (Dactinomycin)

A
  • binds between G-C bases
  • inhibits replication by prevent ssDNA and inhibiting RNA transcription
  • anti-cancer drug, not normally used as an antibiotic
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13
Q

Rifampin

A
  • 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
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14
Q

Amanita Phalloides

A

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

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15
Q

Novobiocin

A
  • inihibits topoisomerase II (DNA gyrase)

- positive supercoils are not unwound

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16
Q 
What do Rotenone
piericidine A (bacterial antibiotic)
barbiturate amytal
do?
A

Inhibit NADH dehydrogenase in Complex I

17
Q 
What do CO
Azide
Hydrogen Sulphide (H2S)
Cyanide (CN-)
do?
A

Inhibit cytochrome oxidase (Complex IV)

18
Q

what does Antimycin A (antibiotic) do?

A

Inhibits cytochrome b of cytochrome reductase (Complex III)

19
Q

what does Oligomycin (Streptomyces antibiotic) do?

A

Inhibits ATP synthase (Complex V)

20
Q

what do ETC inhibitors do?

A

decrease ATP synthesis, decrease ETC and oxygen consumption

21
Q

what does Atractyloside
Bongkrekic Acid
do?

A

Inhibits ADP/ATP transport; inhibits function of nucleotide translocase

22
Q 
what do DNP (dinitrophenol)
ASA (aspirin)
Thermogenin
Ionophores
do?
A

Destroy the protein gradient

23
Q

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

A

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

24
Q

what do uncouplers do?

A

decrease ATP synthesis, increase ETC, increase oxygen consumption

25
Q

what do uncouplers and ionophores do?

A

allow for dissipation of the proton gradient

26
Q

Streptomycin

A

Family of antibiotics with aminoglycoside structure

Prevents assembly of ribosome by binding to 30S subunit

27
Q

Tetracycline

A

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
Q

Erythromycin (clindamycin)

A

Family of antibiotics and has macrolide structure

Binds to the 50S subunit of the complete 70S ribosome of bacteria and blocks ribosome translocation

29
Q

Chloramphenicol

A

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
Q

Cycloheximide

A 
Inhibits peptidyl transferase activity
May inhibit mitochondrial translation
Toxic to eukaryotes
Prokaryotes and mitochondria not affected
Important experimental tool (cheap)
31
Q

Puromycin

A

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

32
Q

Diphtheria toxin

A

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

Medical Biochemistry (17 decks)

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