Premidterm Drugs Flashcards
Didanosine (ddl)
Dideoxy A nucleoside
Host kinases
HIV rt inhibitor
Not used alone
Azidothymidine (AZT)
Aka Zidovudine
Deoxythymidine ( nucleoside) analog
Host kinases
Rt inhibitor (HIV)
Acyclovir
Deoxyguanosine nucleoside analog
1st Pi from herpes thymidine kinase
Others from host kinases
Viral DNA pol inhibitor (30x affinity for viral pol)
Tenoflir
dAMP analog (nucleotide)
HIV rt inhibitor
Host kinases
Cytarabine
Cytosine arabinoside (araC)
Cytosine ribonucleoside analog
Human DNA pol inhibitor (sterics)
Anti cancer (acute myeloid leukemia and other leukemias and lymphomas)
Vidarabine
Adenosine arabinoside
Adenosine ribonucleoside analog
DNA pol inhibitor (sterics)
Anti cancer and herpes simplex
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
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
Ciprofloxain
DNA Gyrase inhibitor (prokaryotic topo II)
Antibiotic of Quinolone family
UTIs, respiratory infection, anthrax
Actinomycin D
Intercalates between adjacent GC pairs and stabilizes double helix and thus inhibits DNA replication and transcription
Camptothecin
Eukaryotic topoisomerase I inhibitor.
Anti-cancer
DNA breaks
Epotoside
Eukaryotic Topoisomerase II inhibitor
Anti cancer
Affects actively dividing cells
Rifamycin/Rifampin
Binds prokaryote RNA Polymerase and prevents formation of first phosphodiester bond (inhibits initiation)
Tuberculosis
No effect on eukaryotes
Alpha-amanitin
From death cap mushroom
Binds and inhibits RNA Pol II
GI symptoms followed by kidney and liver failure
Streptomycin
Binds 30S and prevents assembly of 70S ribosome.
Aminoglycoside
Antibiotic
Tetracycline
Blocks aminoacyl-tRNA from entering A site of ribosome.
Binds 30S of complete ribosome.
Doxycycline
Related to tetracycline. Blocks A site. Binds 30S of complete ribosome.
Doxorubicin
Related to tetracycline. Blocks A site. Binds 30S of complete ribosome.
Erythromycin
Binds 50S subunit of complete ribosome.
Prevents translocation. Prevents initiation and translocation.
Macrolide
Chloramphenicol
Inhibits prokaryotic peptidyl transferase activity (elongation). Not widely used in developed word. May inhibit mitochondrial ribosomes.
Cyclohexamide
Inhibits peptidyl transferase activity (elongation). Similar mechanism to chloramphenicol. Toxic to eukaryotes. Used in labs.
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.
Lysergic acid diethylamide
LSD
Affects serotonin receptors.
Gamma-aminobutyric acdi
GABA
Neurotransmitter
Decarboxylation of glutamate
Histamine
Decarboxylation of histidine
Serotonin
Hydroxylation, followed by decarboxylation of tryptophan.
Carecholamines
Dopamine, norepinephrine, epinephrine.
All made from tyrosine
Dopamine
Tyrosine + -OH -> L-DOPA (dishy stocky-phenylalanine) -> dopamine + CO2
Catecholamine
Used to make (not)epinephrine
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)
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.
Allopurinol
Suicide inhibitor of xanthine oxidase.
Diisopropylflourophosphate
DFP
Irreversibly inhibits acetlycholinesterase
Blurred vision, bronchi constriction, seizures, respiratory arrest, death
Statins
Competitive inhibition if HMG-CoA reductase
Caffeine and Theophylline
Inhibit cyclic nucleotide phosphodiesterase (more cAMP around->more PKA)
Cholera Toxin
ADP-riboslyates Gs->inhibits GTPase->Gs is continuously active->andnyl Cyclase is constitutively active->PKA->turns on CFTR
Diarrhea
E. Coli toxin
ADP-riboslyates Gs->inhibits GTPase->Gs is continuously active->andnyl Cyclase is constitutively active->PKA->turns on CFTR
Diarrhea
Pertussis toxin
ADP-riboslyates Gi->Gs is continuously inactive->andnyl Cyclase is constitutively active->PKA->turns on CFTR
Diarrhea
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
Malonate
Inhibits succinate dehydrogenase
Fluoroacetate
Inhibits aconitase
Rotenone
Complex I/ NADH dehydrogenase inhibitor
Piericidin A
Complex I/ NADH dehydrogenase inhibitor
Amytal
A barbituate
Complex I/ NADH dehydrogenase inhibitor
Antimycin A
Complex III/Cytochrome reductase inhibitor
CO
Binds heme in Hb, myoglobin, and complex IV/cytochrome oxidase
Azide
complex IV/cytochrome oxidase inhibitor
H2S
complex IV/cytochrome oxidase inhibitor
Cyanide
complex IV/cytochrome oxidase inhibitor
Oligomycin
(F1F0) ATP synthase inhibitor
Atractyloside
Inhibits adenine nucleotide transporter
Inter membrane space side
Effect similar to oligomycin
Bongkrekic acid
Inhibits adenine nucleotide transporter
Matrix side
Effect similar to oligomycin
Dinitrophenol
Etc uncoupler
Dnp
Gramicidin
Ionophore/etc uncoupler/makes channel
Valinomycin
Ionophore
Typically K+, can uncouple, carries across membrane
