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Medical Biochemistry > Drugs > Flashcards

Drugs Flashcards

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USMLE® Step 1 flashcards
1
Q

Azidohymidine (AZT)

A

Anti-viral nucleoside analogue
Viral reverse transcriptase inhibitor
Terminates process due to lack of 3’ OH
used for HIV treatment

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2
Q

Didanosine (ddI)

A

Anti-viral nucleoside analogue
Viral reverse transcriptase inhibitor
Terminates process due to lack of 3’ OH
High affinity for prokaryotic cells

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3
Q

Acyclovir

A

Anti-viral nucleoside analogue
Viral reverse transcriptase inhibitor
Terminates process due to lack of 3’ OH
Is first phosphorylated by viral kinase and is only activated in infected cells

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4
Q

Tenofovir

A

Anti-viral nucleotide base analogue

Gets incorporated into newly formed HIV DNA and terminates synthesis

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5
Q

Cytosine arabinoside (Cytarabine)

A

AraC has a 3’ OH group to act as an acceptor for further chain elongation. However the OH gp at posn., 2 prevents polymerase adding the next dNTP due to stereo restraints causing chain termination.

Used for acute myeloid leukaemia.

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6
Q

Adenosine arabinoside (Vidarabine)

A

Planar configuration of arabinoside prevents DNA elongation despite 3’ OH being present.

Used for acute lymphoblastic leukaemia and herpes simplex infections

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7
Q

5-azacytidine, 5-aza-2’-deoxycytidine (Decitabine)

A

Under methylate DNA and inhibit DNA methyltransferase enzymes
Methylation of cytosine shuts down transcription
p15 tumor suppressor session

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8
Q

Ciproflaxin

A

inhibits DNA gyrase (topoisomerase II in eukaryotes) so DNA can’t unwind and replication is stopped

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9
Q

Actinomycin D

A

Inhibitor of replication
Intercalates between G-C bases
Prevent formation of regions of ss DNA
inhibits RNA transcription (prevents strand separation

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10
Q

Rifampin

A

Antibiotic from Streptomyces
Inhibits initiation of transcription
Blocks formation of first phosphodiester bond by binding to prokaryote RNA polymerase - doesn’t affect eukaryotic RNA polymerase
Used for TB treatment

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11
Q

Camptothecin

A

Inhibitor of eukaryotic replication
Inhibits topoisomerase I activity resulting in DNA breakage

Anti cancer drug

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12
Q

Etopside

A

inhibits activity of topoisomerase II

Anti-cancer drug

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13
Q

Alpha-amantin from Death Cap Mushroom

A

Inhibitor of RNA polymerase II

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14
Q

Tetracycline

A

Blocks elongation
Interacts with 30S sub unity of complete 70s ribosome
Prevent incoming aminoacyl-tRNA to access A site

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15
Q

Chloramphenicol

A

Inhibits prokaryotic elongation

Not used in developed countries - may inhibit mitochondrial ribosomes

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16
Q

Erythromycin

A

Macrolide structure
Binds to 50S subunit in complete ribosome
Blocks elongation by preventing ribosome movement relative to mRNA
Blocks ribosome translocation

17
Q

Puromycin

A

structural analog to a portion of aminoacyl-tRNA
toxic to both prokaryotes and eukaryotes - not clnically useful
blocks elongation and causes peptide to fall out of ribosome P-site and causes premature translation termination

18
Q

Cyclohexamide

A

simple organic molecule that inhibits elongation in eukaryotes - similar to choloramphenicol
extremely toxic to eukaryotes
widely used in laboratories

19
Q

Streptomycin

A

Aminoglycoside

Binds to 30s ribosomal subunit
Distorts structure
Prevents assembly of complete ribosome and initiation

20
Q

Acetazolamide

A

interferes with bicarbonate reabsorption into kidneys which reacidifies blood and alkalises urine

21
Q

Aspirin

A

Acetylates a serene in channel of active site
Irreversibly inhibits cyclooxygenase (COX)
COX-1 (constitutive, physiologic functions)
COX-2 (inducible, pain, fever, inflammation)

22
Q

DFP (do-isopropyl fluorophosphate)

A

Nerve gas poison, similar action as sarin
Irreversible inhibitor of acetylcholinesterase –> normally cleaves neurotransmitter acetylcholine in postsynaptic neuromuscular junction
Binds covalently to serene in active site
Leads to blurred vision, bronchoconstriction, seizures, respiratory arrest, and death

23
Q

Statin drugs

A

HMG co-A reductase - catalyses synthesis step of cholesterol

24
Q

Allopurinol

A

Drug is used as a substrate for xanthine oxidase and modified to an irreversible inhibitor

Medical Biochemistry (4 decks)

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