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Premidterm biochem > Premidterm Drugs > Flashcards

Premidterm Drugs Flashcards

0
Q

Didanosine (ddl)

A

Dideoxy A nucleoside
Host kinases
HIV rt inhibitor
Not used alone

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1
Q

Azidothymidine (AZT)

A

Aka Zidovudine

Deoxythymidine ( nucleoside) analog

Host kinases

Rt inhibitor (HIV)

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2
Q

Acyclovir

A

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

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3
Q

Tenoflir

A

dAMP analog (nucleotide)
HIV rt inhibitor
Host kinases

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4
Q

Cytarabine

A

Cytosine arabinoside (araC)

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

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5
Q

Vidarabine

A

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

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6
Q

Decitabine

A

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
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7
Q

5-azacytidine

A

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

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8
Q

Ciprofloxain

A

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

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9
Q

Actinomycin D

A

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

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10
Q

Camptothecin

A

Eukaryotic topoisomerase I inhibitor.
Anti-cancer
DNA breaks

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11
Q

Epotoside

A

Eukaryotic Topoisomerase II inhibitor

Anti cancer

Affects actively dividing cells

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12
Q

Rifamycin/Rifampin

A

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

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13
Q

Alpha-amanitin

A

From death cap mushroom

Binds and inhibits RNA Pol II

GI symptoms followed by kidney and liver failure

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14
Q

Streptomycin

A

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

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15
Q

Tetracycline

A

Blocks aminoacyl-tRNA from entering A site of ribosome.

Binds 30S of complete ribosome.

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16
Q

Doxycycline

A

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

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17
Q

Doxorubicin

A

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

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18
Q

Erythromycin

A

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

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19
Q

Chloramphenicol

A

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

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20
Q

Cyclohexamide

A

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

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21
Q

Puromycin

A

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
Q

Lysergic acid diethylamide

A

LSD

Affects serotonin receptors.

23
Q

Gamma-aminobutyric acdi

A

GABA
Neurotransmitter
Decarboxylation of glutamate

24
Q

Histamine

A

Decarboxylation of histidine

25
Q

Serotonin

A

Hydroxylation, followed by decarboxylation of tryptophan.

26
Q

Carecholamines

A

Dopamine, norepinephrine, epinephrine.

All made from tyrosine

27
Q

Dopamine

A

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

Catecholamine
Used to make (not)epinephrine

28
Q

Acetalzolamide

A

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
Q

Aspirin

A

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
Q

Allopurinol

A

Suicide inhibitor of xanthine oxidase.

31
Q

Diisopropylflourophosphate

A

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

32
Q

Statins

A

Competitive inhibition if HMG-CoA reductase

33
Q

Caffeine and Theophylline

A

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

34
Q

Cholera Toxin

A

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

35
Q

E. Coli toxin

A

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

36
Q

Pertussis toxin

A

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

Diarrhea

37
Q

Nitroglycerin/Nitroprusside

A

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
Q

Malonate

A

Inhibits succinate dehydrogenase

44
Q

Fluoroacetate

A

Inhibits aconitase

45
Q

Rotenone

A

Complex I/ NADH dehydrogenase inhibitor

46
Q

Piericidin A

A

Complex I/ NADH dehydrogenase inhibitor

47
Q

Amytal

A

A barbituate

Complex I/ NADH dehydrogenase inhibitor

48
Q

Antimycin A

A

Complex III/Cytochrome reductase inhibitor

49
Q

CO

A

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

50
Q

Azide

A

complex IV/cytochrome oxidase inhibitor

51
Q

H2S

A

complex IV/cytochrome oxidase inhibitor

52
Q

Cyanide

A

complex IV/cytochrome oxidase inhibitor

53
Q

Oligomycin

A

(F1F0) ATP synthase inhibitor

54
Q

Atractyloside

A

Inhibits adenine nucleotide transporter

Inter membrane space side
Effect similar to oligomycin

55
Q

Bongkrekic acid

A

Inhibits adenine nucleotide transporter

Matrix side

Effect similar to oligomycin

56
Q

Dinitrophenol

A

Etc uncoupler

Dnp

57
Q

Gramicidin

A

Ionophore/etc uncoupler/makes channel

58
Q

Valinomycin

A

Ionophore

Typically K+, can uncouple, carries across membrane

Premidterm biochem (5 decks)

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