Premidterm Drugs Flashcards

(54 cards)

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
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