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PMCOL 200 Final > Drugs II > Flashcards

Drugs II Flashcards

1
Q

Warfarin

A

Inhibits Vitamin K epoxide reductase
Preventing the formation of clotting factors

Increases INR

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2
Q

Vitamin K

A

Is reduced from Vitamin K (KO) to Reduced Vitamin K (KH2) and is converted to prothrombin (clotting factor)

The greater amount of Vit K the weaker the effects of warfarin

Decreasing clotting time

Decrease INR

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3
Q

Xanax

A

Benzodiazepines

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4
Q

Valium

A

Benzodiazepines

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5
Q

Benzodiazepines

A

Positive allosteric modulator of GABA A

Causing sedation and unconsciousness

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6
Q

Barbiturates

A

Positive allosteric modulator or agonist of GABA A

Causing sedation and unconsciousness

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7
Q

Alcohols

A

Positive allosteric modulator of GABA A

Causing sedation and unconsciousness

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8
Q

Ambien

A

Zolpidem
Positive allosteric modulator of GABA A

Causing sedation and unconsciousness

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9
Q

Monoamine Oxidase

A

Breaks down 5-HT

Inhibitors would lead to an increase in 5-HT

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10
Q

Tricyclic Antidepressants

A

Reuptake inhibitors

Would leave more 5-HT in the synapse

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11
Q

Methamphetamine

A

Promotes serotonin release

Often by causing uptake pumps/transporters to work in reverse
Increase 5-HT

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12
Q

MDMA

A

Promotes serotonin release

Often by causing uptake pumps/transporters to work in reverse
Increase 5-HT

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13
Q

5-HTP

A

Precursor of 5-HT

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14
Q

L-tryptophan

A

Precursor of 5-HT

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15
Q

Lidocaine

A

Blocks Na+

When taken with epinephrin its effects are more localized for a longer time due to constriction of blood vessels

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16
Q

Epinephrine

A

Constricts blood vessels

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17
Q

CYP3A4

A

Most common for biotransformation of drug

Changing expression can alter pharmacodynamics
More CYP3A4 = Less drug activity = L
Less CYP3A4 = Increase drug activity

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18
Q

Rifampicin

A

CYP3A4 Inducer

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19
Q

Phenytoin*

A

CYP3A4 Inducer

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20
Q

Carbamazepine*

A

CYP3A4 Inducer

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21
Q

Glucocorticoids*

A

CYP3A4 Inducer

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22
Q

Grapefruit Juice

A

CYP3A4 Inhibitor

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23
Q

Erythromycin*

A

CYP3A4 Inhibitor

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24
Q

Ciprofloxacin*

A

CYP3A4 Inhibitor

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25
Q

Components of peptidoglycan

A

Glycan strands alternating
N-Acetylglucosamine
N-Acetylmuramic acid

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26
Q

Glycotransferase

A

GT
Assembles chains of glycan into peptidoglycan chains

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27
Q

Transpeptidase

A

PT/Penicillin Binding Protein
Cross-links chains of peptidoglycan

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28
Q

Penicillin

A

Cell Wall Inhibitor, bacteriocidal

Inhibit DD-transpeptidase enzyme / penicillin-binding protein

Works only on gram positive

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29
Q

Cephalosporin

A

Cell Wall Inhibitor, bacteriocidal

Inhibit DD-transpeptidase enzyme / penicillin-binding protein

Works only on gram-positive and gram-negative
More effective on gram-positive

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30
Q

Beta-lactamases

A

Inhibits beta-lactam rings of certain penicillins and cephalosporins

Found in most gram-negative and staphylococci
Confers resistance

31
Q

Clavulanic Acid

A

Beta-lactamase inhibitor

Protects penicillins and cephalosporins that can be potentially hydrolyzed

32
Q

Vanomyocin

A

Cell Wall Inhibitor
Not a beta-lactam ring
Inhibits peptidoglycan cross-linking

Produced by Actinobacteria and Amycolatopsis orientalis

33
Q

PABA

A

Para-aminobenzoic acid

Is converted by dihydropteroate synthase into dihydrofolic acid

34
Q

Dihydrofolic acid

A

Is converted by Dihydrofolate reductase into tetrahydrofolic acid

35
Q

Tetrahydrofolic acid

A

Is converted into purines (Nucleic acids) which are used to synthesize DNA

36
Q

Sulfonamides

A

Competes with PABA for Dihydropteroate synthase

Interferes with PABA metabolic pathway preventing DNA synthesis

37
Q

Trimethoprim

A

Competes with Dihydrofolic acid for Dihydrofolate reducatase

Interferes with PABA metabolic pathway preventing DNA synthesis

38
Q

70S ribosomal complex

A

Bacteria Ribosomal Subunits
30S and 50S

39
Q

80S ribosomal complex

A

Euk Ribosomal subunits
40S and 60S

40
Q

Chloramphenicol

A

Binds to 50S subunit

Prevents transpeptidation (movement of amino acid onto growing chain)

41
Q

Tetracycline

A

Binds to 30S subunit

Prevents binding of tRNA to to the ribosome

42
Q

Macrolides

A

Binds to 50S subunit

Prevents transpeptidation (movement of amino acid onto growing chain)

43
Q

Aminoglycosides

A

Binds to 30S subunit

Blocks initiation of complex
Causes misreadings of mRNA template, wrong proteins are created
Inhibits translocation

44
Q

Poxvirus

A

DNA Virus

Contain their own DNA-dependent RNA polymerase
Can perform DNA –> mRNA in the cytoplasm

Need DNA-dependent DNA polymerase from host to replicate (in the nucleus)

45
Q

Influenza Virus

A

RNA Virus

Contain their own RNA dependent RNA polymerase (Humans don’t make mRNA from RNA, only make from DNA)
Transcribed in the nucleus

46
Q

HIV Virus

A

Retrovirus

Contains RNA-dependent DNA polymerase
This viral DNA is then integrated and transcribed into mRNA by the host cell
mRNA is translated into proteins by the host cell

47
Q

Acyclovir

A

Anti-Herpes

Fake nucleoside analog
Lacks hydroxyl group, causing DNA chain termination

Must be phosphorylated to acyclovir-triphosphate

48
Q

Thymidine Kinase

A

Herpes Virus
Performs first phosphorylation on acyclovir

Has high affinity for acyclovir

49
Q

HIV / Infects what?

A

CD4+ T-Cells

Body loses cell-mediated immunity and becomes susceptible to infections (AIDS)

50
Q

HAART

A

Highly Active Antiretroviral Therapy

Drug combinations to slow HIV

51
Q

Maraviroc

A

Entry Inhibitor
CCR5 receptor antagonist

Binds to CCR5 receptor and prevents HIV from binding to CD4 receptors using their gp120 proteins

52
Q

NRTI

A

Nucleotide Reverse Transcriptase Inhibitors

Small molecules that mimic host nucleosides
Lack 3’ hydroxyl group causing chain termination

53
Q

Raltegravir

A

Integrase Strand Transfer Inhibitor (INSTs)

Prevents the action of integrase that causes the injection of the viral genome into the cell

54
Q

Protease Inhibitor

A

Aspartate proteases cleave precursor proteins to form the final mature virion core

Protease inhibitors prevent formation of the mature HIV

Used with NRTI

55
Q

Amantadine

A

Prevents Influenza A

Blocks H+ from entering M2, prevents acidification and activation of viral transcription

56
Q

Zanamivir

A

Prevents Influenza A and B

Inhibits neuroaminidases from cleaving sialic acid residues from viral proteins, prevents the release of virus from host

57
Q

p53

A

Tumour suppressor protein that regulates cell cycle

Inhibits cell division
Initaite apoptosis following irreversible DNA damage
DNA repair proteins (BRCA)

58
Q

BRCA

A

DNA repair proteins

59
Q

Proto-oncogenes

A

Normal genes involved in cell growth, proliferation, or inhibition of apoptosis

60
Q

Oncogene

A

Mutation in a proto-oncogene that increases expression and proliferation

61
Q

BCR-ABL

A

Philadelphia chromosome

ABL1 gene chromosome 9
Tyrosine kinase activity, controls cell division

BCR gene chromosome 22
Very strong promoter

62
Q

5-Fluorouracil

A

5-FU
Pyrimidine Analogue
Effects only in its active metabolite form Fdump

Competes with normal pyrimidine for thymidylate synthase (TS)
TS converts dUMP to dTMP

63
Q

6-mercaptopurine

A

Inhibits purine nucleotide synthesis and metabolism by inhibiting PRPP amidotransferase (Phsophoribibosyl pyrophosphate amidotransferase)

PRPP used to convert Ribose into IMP
IMP is the rate-limiting factor

64
Q

Cisplatin

A

Alkylating Agent
Platinum analogue
Causes inter-strand crosslinks that inhibit DNA synthesis and function

N7 atom of guanine is susceptible
G1 and S phase cancer cells are most susceptible

65
Q

Methotrexate

A

Anti-Folate
Folic Acid analogue
Binds with high affinity to the active catalytic site of dihydrofolate reductase

Interferes with FH4 metabolism, folic acid is not properly converted by enzyme reduction to FH4 cofactors

Effective during S phase when cancer cells are proliferating rapidly

66
Q

Vinca Alkaloids

A

Periwinkle Plant

Inhibit tubulin polymerization
Disrupts microtubule assembly in miotic spindle apparatus (M phase)

67
Q

Taxanes

A

Pacific yew tree

Promote microtubule assembly through high-affinity binding
Inhibits microtubule depolymerization (M phase)

68
Q

Paclitaxel

A

Taxane

Inhibits microtubule depolymerization

69
Q

Camptothecins

A

Campthotheca acuminate tree

Bind and stabilize DNA-topoisomerase I complex, it now can not move down the strand

Inhibits re-ligation, accumulation of single-stranded breaks in DNA causing apoptosis
(Does not affect initial cleavage)

S-phase specific can only occur when DNA synthesis is ongoing

70
Q

Anthracycline

A

Product of Streptomyces
Most widely used cancer drug

Inhibit topoisomerases
Generate free radicals (DNA mutagenesis), mutated cell can not divide
High affinity binding to DNA
Bind cellular membrane to alter fluidity and ion transport

71
Q

Imatinib

A

Tyrosine Kinase Inhibitors

Inhibits the tyrosine kinase domain of the BCR-ABL oncoprotein

Treats leukemia

72
Q

Cetuximab

A

Epidermal Growth Factor Receptor (EGFR) Inhibitor

Inhibit the EGFR signal that is overly expressed in cancer cell and is what is causing cell growth, metastasis

73
Q

Tamoxifen

A

Selective estrogen receptor antagonists

Blocks binding of estrogen to estrogen-sensitive cancer cells in breast tissue

Estrogen promotes cell division by changing gene activity to produce more signals for cell division

PMCOL 200 Final (5 decks)

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