Drugs Exam 1 Flashcards

1
Q

methylene blue

A

a dye that is reduced to leucomethylene blue, which then reduces the ferric iron back to ferrous iron to treat methemoglobinemia

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2
Q

anti-inflammatory steroids

A

inhibit phospholipase A2 to prevent formation of prostaglandins aka eicosanoids by COX.

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3
Q

allopurinol

A

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.

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4
Q

ciprofloxacin

A

bacterial topoisomerase II inhibitor

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5
Q

nalidixic acid

A

bacterial topoisomerase II inhibitor

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6
Q

etoposide

A

human topoisomerase II inhibitor

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7
Q

doxorubicin

A

human topoisomerase II inhibitor

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8
Q

cytochalasin B and D

A

fungal toxin that binds to + end of actin filament to block elongation and causing degradation.

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9
Q

Phallotoxin (phalloidin)

A

binds to actin filaments to prevent dissociation into G actin, stabilizes AF; can be used with fluorescent conjugates to label F-actin

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10
Q

Cofilin

A

binds to actin filaments to increase dissociation from - end and stays bound to ADP-actin monomers, preventing reassembly

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11
Q

profilin

A

can stimulate actin exchange of ADP to ATP, so can allow repolymerization

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12
Q

Colchicine

A

bind and inhibit MT polymerization and disrupt MT spindle; stops cell in metaphase

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13
Q

colcemid

A

bind and inhibit MT polymerization and disrupt MT spindle; stops cell in metaphase

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14
Q

nocodazole

A

bind and inhibit MT polymerization and disrupt MT spindle; stops cell in metaphase

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15
Q

vincristine

A

bind to tubulins and inhibit rapidly dividing cells (chemotherapy)

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16
Q

vanblastin

A

bind to tubulins and inhibit rapidly dividing cells (chemotherapy)

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17
Q

Paclitaxel/Taxol

A

stabilizes MT’s and arrests mitosis (chemotherapy)

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18
Q

albuterol

A

relaxes smooth muscle to treat asthma and prevent premature labor

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19
Q

Oxytosin

A

stimulates smooth muscle contraction to induce labor.

20
Q

statins

A

competitively target HMG-CoA reductase to decrease cholesterol synthesis

21
Q

competitive inhibition

A

(changes Km, but not Vmax; increasing amount of substrate in constant concentration of inhibitor overcomes effects)

22
Q

sulfanilamide

A

blocks prokaryotic nucleic acid synthesis through competitive inhibition of dihydropteroate synthetase

23
Q

methotrexate

A

competitively blocks eukaryotic nucleic acid synthesis through dihydrofolate reductase

24
Q

Captopril

A

competitively inhibits ACE to treat hypertension

25
Q

Coumadin

A

mimics vitamin K to competitively inhibit γ-glutamyl-carbocylase reaction in the hepatic synthesis of coagulation factors; blood thinner.

26
Q

cyanide and sulfide

A

suicide inhibitors of the ETC

27
Q

organophosphates

A

suicide inhibitors (like serine nerve gas inhibiting acetylcholinesterase)

28
Q

aspirin

A

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

29
Q

5-bromouracil

A

Base analog that is incorporated into DNA and causes mutations

30
Q

N-methyl-N-nitrosoguanidine (MNNG)

A

Alkylating agent (attaches alkyl group)

31
Q

nitrous acid

A

Deaminating agent removes amino group: Deamination of A results in hypoxanthine, G results in xanthine, and C results in deoxyuracil

32
Q

ethidium bromide

A

intercalating agents insert between stacked bases to cause frameshift mutations

33
Q

proflavin

A

intercalating agents insert between stacked bases to cause frameshift mutations

34
Q

Rifampicin

A

specifically inhibits RNA initiation in prokaryotes by binding to beta subunit of bacterial RNA pol; does not inhabit eukaryotic RNA pol

35
Q

α-amanitin

A

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

36
Q

Actinomycin D

A

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

37
Q

Streptomycin

A

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

38
Q

Tetracycline

A

Inhibits binding of aminoacyl-tRNA to the A-site: Prokaryotic antibiotic

39
Q

Choramphenicol

A

Inhibits peptidyl transferase activity on ribosomes: Prokaryotic antibiotic

40
Q

Erythromycin

A

Binds to the 50S subunit and inhibits translocation: Prokaryotic antibiotic

41
Q

Puromycin

A

Resembles aminoacyl-tRNA and binds to A-site. Causes premature release of polypeptide chain. (Prokaryotic & eukaryotic)

42
Q

Cycloheximide

A

Inhibits translocation during elongation: eukaryotic

43
Q

Diphtheria toxin

A

Inhibits eEF-2 and prevents translocation: eukaryotic

44
Q

Ricin

A

Inactivates 60S subunit of ribosome: eukaryotic

45
Q

Pertussis toxin

A

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