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Flashcards in Premidterm Drugs Deck (54):
0

Azidothymidine (AZT)

Aka Zidovudine

Deoxythymidine ( nucleoside) analog

Host kinases

Rt inhibitor (HIV)

1

Didanosine (ddl)

Dideoxy A nucleoside
Host kinases
HIV rt inhibitor
Not used alone

2

Acyclovir

Deoxyguanosine nucleoside analog
1st Pi from herpes thymidine kinase
Others from host kinases
Viral DNA pol inhibitor (30x affinity for viral pol)

3

Tenoflir

dAMP analog (nucleotide)
HIV rt inhibitor
Host kinases

4

Cytarabine

Cytosine arabinoside (araC)

Cytosine ribonucleoside analog
Human DNA pol inhibitor (sterics)
Anti cancer (acute myeloid leukemia and other leukemias and lymphomas)

5

Vidarabine

Adenosine arabinoside
Adenosine ribonucleoside analog
DNA pol inhibitor (sterics)
Anti cancer and herpes simplex

6

Decitabine

5-aza-2'-deoxycytidine (nucleoside)

When incorporated into DNA causes hypomethylation (inhibits DNA methylates)

Anti cancer (acute myeloid leukemia and myelodysplastic syndrome)
Turn on P15 tumor suppressor

7

5-azacytidine

Ribonucleoside
(inhibits DNA methylase)

Anti cancer
Can be metabolized and incorporated into DNA causes hypomethylation
More likely to get into and fuck up rRNA and tRNA

Turn on P15 tumor suppressor

8

Ciprofloxain

DNA Gyrase inhibitor (prokaryotic topo II)
Antibiotic of Quinolone family
UTIs, respiratory infection, anthrax

9

Actinomycin D

Intercalates between adjacent GC pairs and stabilizes double helix and thus inhibits DNA replication and transcription

10

Camptothecin

Eukaryotic topoisomerase I inhibitor.
Anti-cancer
DNA breaks

11

Epotoside

Eukaryotic Topoisomerase II inhibitor

Anti cancer

Affects actively dividing cells

12

Rifamycin/Rifampin

Binds prokaryote RNA Polymerase and prevents formation of first phosphodiester bond (inhibits initiation)
Tuberculosis
No effect on eukaryotes

13

Alpha-amanitin

From death cap mushroom

Binds and inhibits RNA Pol II

GI symptoms followed by kidney and liver failure

14

Streptomycin

Binds 30S and prevents assembly of 70S ribosome.
Aminoglycoside
Antibiotic

15

Tetracycline

Blocks aminoacyl-tRNA from entering A site of ribosome.
Binds 30S of complete ribosome.

16

Doxycycline

Related to tetracycline. Blocks A site. Binds 30S of complete ribosome.

17

Doxorubicin

Related to tetracycline. Blocks A site. Binds 30S of complete ribosome.

18

Erythromycin

Binds 50S subunit of complete ribosome.
Prevents translocation. Prevents initiation and translocation.
Macrolide

19

Chloramphenicol

Inhibits prokaryotic peptidyl transferase activity (elongation). Not widely used in developed word. May inhibit mitochondrial ribosomes.

20

Cyclohexamide

Inhibits peptidyl transferase activity (elongation). Similar mechanism to chloramphenicol. Toxic to eukaryotes. Used in labs.

21

Puromycin

Aminoacyl-tRNA analog. Enters A site. Reacts with polypeptide chain. Chain terminating (blocks elongation). Is/was used in labs. Toxic to euks and proks.

22

Lysergic acid diethylamide

LSD

Affects serotonin receptors.

23

Gamma-aminobutyric acdi

GABA
Neurotransmitter
Decarboxylation of glutamate

24

Histamine

Decarboxylation of histidine

25

Serotonin

Hydroxylation, followed by decarboxylation of tryptophan.

26

Carecholamines

Dopamine, norepinephrine, epinephrine.

All made from tyrosine

27

Dopamine

Tyrosine + -OH -> L-DOPA (dishy stocky-phenylalanine) -> dopamine + CO2

Catecholamine
Used to make (not)epinephrine

28

Acetalzolamide

Carbonic anhydrase inhibitor

Inhibits carbonic anhydrase in kidneys. Prevents reabsorption of HCO3-. Causes metabolic acidosis. Can be used to treat alkylosis (hasten acclimatization esp with altitude sickness)

29

Aspirin

Irreversibly inhibits cyclooxygenase (COX1/2) by acetlyating ser residue in active site (inhibits thrombin and in thrombocytes, prostacyclin in epithelial cells). Low dose for clotting, high dose for pain. Also is an ETC decoupler.

30

Allopurinol

Suicide inhibitor of xanthine oxidase.

31

Diisopropylflourophosphate

DFP
Irreversibly inhibits acetlycholinesterase
Blurred vision, bronchi constriction, seizures, respiratory arrest, death

32

Statins

Competitive inhibition if HMG-CoA reductase

33

Caffeine and Theophylline

Inhibit cyclic nucleotide phosphodiesterase (more cAMP around->more PKA)

34

Cholera Toxin

ADP-riboslyates Gs->inhibits GTPase->Gs is continuously active->andnyl Cyclase is constitutively active->PKA->turns on CFTR
Diarrhea

35

E. Coli toxin

ADP-riboslyates Gs->inhibits GTPase->Gs is continuously active->andnyl Cyclase is constitutively active->PKA->turns on CFTR
Diarrhea

36

Pertussis toxin

ADP-riboslyates Gi->Gs is continuously inactive->andnyl Cyclase is constitutively active->PKA->turns on CFTR

Diarrhea

37

Nitroglycerin/Nitroprusside

Metabolized to NO. NO activates soluble guanylate cyclase activating PKG leading to vasodilation. NO (radical) also reacts with superoxide to give peroxynitrate which is bacteriocidal

43

Malonate

Inhibits succinate dehydrogenase

44

Fluoroacetate

Inhibits aconitase

45

Rotenone

Complex I/ NADH dehydrogenase inhibitor

46

Piericidin A

Complex I/ NADH dehydrogenase inhibitor

47

Amytal

A barbituate

Complex I/ NADH dehydrogenase inhibitor

48

Antimycin A

Complex III/Cytochrome reductase inhibitor

49

CO

Binds heme in Hb, myoglobin, and complex IV/cytochrome oxidase

50

Azide

complex IV/cytochrome oxidase inhibitor

51

H2S

complex IV/cytochrome oxidase inhibitor

52

Cyanide

complex IV/cytochrome oxidase inhibitor

53

Oligomycin

(F1F0) ATP synthase inhibitor

54

Atractyloside

Inhibits adenine nucleotide transporter

Inter membrane space side
Effect similar to oligomycin

55

Bongkrekic acid

Inhibits adenine nucleotide transporter

Matrix side

Effect similar to oligomycin

56

Dinitrophenol

Etc uncoupler

Dnp

57

Gramicidin

Ionophore/etc uncoupler/makes channel

58

Valinomycin

Ionophore
Typically K+, can uncouple, carries across membrane