Drugs Exam 1 Flashcards
methylene blue
a dye that is reduced to leucomethylene blue, which then reduces the ferric iron back to ferrous iron to treat methemoglobinemia
anti-inflammatory steroids
inhibit phospholipase A2 to prevent formation of prostaglandins aka eicosanoids by COX.
allopurinol
a purine analog used to treat gout (excess uric acid). Purines are carbolized to uric acid (low water solubility), but allopurinol is converted to alloxanthine (AX) by xanthine oxidase (XO). AX competitively inhibits XO, decreasing uric acid and increasing xanthine and hypoxanthine, the mixture of these 3 is more soluble.
ciprofloxacin
bacterial topoisomerase II inhibitor
nalidixic acid
bacterial topoisomerase II inhibitor
etoposide
human topoisomerase II inhibitor
doxorubicin
human topoisomerase II inhibitor
cytochalasin B and D
fungal toxin that binds to + end of actin filament to block elongation and causing degradation.
Phallotoxin (phalloidin)
binds to actin filaments to prevent dissociation into G actin, stabilizes AF; can be used with fluorescent conjugates to label F-actin
Cofilin
binds to actin filaments to increase dissociation from - end and stays bound to ADP-actin monomers, preventing reassembly
profilin
can stimulate actin exchange of ADP to ATP, so can allow repolymerization
Colchicine
bind and inhibit MT polymerization and disrupt MT spindle; stops cell in metaphase
colcemid
bind and inhibit MT polymerization and disrupt MT spindle; stops cell in metaphase
nocodazole
bind and inhibit MT polymerization and disrupt MT spindle; stops cell in metaphase
vincristine
bind to tubulins and inhibit rapidly dividing cells (chemotherapy)
vanblastin
bind to tubulins and inhibit rapidly dividing cells (chemotherapy)
Paclitaxel/Taxol
stabilizes MT’s and arrests mitosis (chemotherapy)
albuterol
relaxes smooth muscle to treat asthma and prevent premature labor
Oxytosin
stimulates smooth muscle contraction to induce labor.
statins
competitively target HMG-CoA reductase to decrease cholesterol synthesis
competitive inhibition
(changes Km, but not Vmax; increasing amount of substrate in constant concentration of inhibitor overcomes effects)
sulfanilamide
blocks prokaryotic nucleic acid synthesis through competitive inhibition of dihydropteroate synthetase
methotrexate
competitively blocks eukaryotic nucleic acid synthesis through dihydrofolate reductase
Captopril
competitively inhibits ACE to treat hypertension
Coumadin
mimics vitamin K to competitively inhibit γ-glutamyl-carbocylase reaction in the hepatic synthesis of coagulation factors; blood thinner.
cyanide and sulfide
suicide inhibitors of the ETC
organophosphates
suicide inhibitors (like serine nerve gas inhibiting acetylcholinesterase)
aspirin
suicide inhibitor for COX; through inactivation of PGH synthase by addition of an acyl group to Ser 530 in active site? Irreversibly interferes with prostaglandin synthesis
5-bromouracil
Base analog that is incorporated into DNA and causes mutations
N-methyl-N-nitrosoguanidine (MNNG)
Alkylating agent (attaches alkyl group)
nitrous acid
Deaminating agent removes amino group: Deamination of A results in hypoxanthine, G results in xanthine, and C results in deoxyuracil
ethidium bromide
intercalating agents insert between stacked bases to cause frameshift mutations
proflavin
intercalating agents insert between stacked bases to cause frameshift mutations
Rifampicin
specifically inhibits RNA initiation in prokaryotes by binding to beta subunit of bacterial RNA pol; does not inhabit eukaryotic RNA pol
α-amanitin
toxic mushroom poison from the “death cap” mushroom that binds very tightly to eukaryotic RNA pol II and prevent formation of mRNA through elongation; no effect on bacterial RNA pol
Actinomycin D
binds to dsDNA at deoxyguanosine residues through intercalating into the helix. Specifically inhibits RNA synthesis, but not replication or protein synthesis; works by inhibiting the formation of a transcription bubble, thereby inhibiting RNA elongation. This is not specific for prokaryotes or eukaryotes
Streptomycin
Causes misreading of the genetic code.
(Prokaryotes) Interferes with initiation by binding to the small subunit and preventing assemebly of the small and large subunits
Tetracycline
Inhibits binding of aminoacyl-tRNA to the A-site: Prokaryotic antibiotic
Choramphenicol
Inhibits peptidyl transferase activity on ribosomes: Prokaryotic antibiotic
Erythromycin
Binds to the 50S subunit and inhibits translocation: Prokaryotic antibiotic
Puromycin
Resembles aminoacyl-tRNA and binds to A-site. Causes premature release of polypeptide chain. (Prokaryotic & eukaryotic)
Cycloheximide
Inhibits translocation during elongation: eukaryotic
Diphtheria toxin
Inhibits eEF-2 and prevents translocation: eukaryotic
Ricin
Inactivates 60S subunit of ribosome: eukaryotic
Pertussis toxin
Causes pertussis aka whooping cough. Toxin is endocytosed and ribosylates the αi subunit (inhibitory subunit) resulting in the protein being locked in the GDP bound state, resulting in increased cAMP
