Drugs II Flashcards
(73 cards)
1
Q
Warfarin
A
Inhibits Vitamin K epoxide reductase
Preventing the formation of clotting factors
Increases INR
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
3
Q
Xanax
A
Benzodiazepines
4
Q
Valium
A
Benzodiazepines
5
Q
Benzodiazepines
A
Positive allosteric modulator of GABA A
Causing sedation and unconsciousness
6
Q
Barbiturates
A
Positive allosteric modulator or agonist of GABA A
Causing sedation and unconsciousness
7
Q
Alcohols
A
Positive allosteric modulator of GABA A
Causing sedation and unconsciousness
8
Q
Ambien
A
Zolpidem
Positive allosteric modulator of GABA A
Causing sedation and unconsciousness
9
Q
Monoamine Oxidase
A
Breaks down 5-HT
Inhibitors would lead to an increase in 5-HT
10
Q
Tricyclic Antidepressants
A
Reuptake inhibitors
Would leave more 5-HT in the synapse
11
Q
Methamphetamine
A
Promotes serotonin release
Often by causing uptake pumps/transporters to work in reverse
Increase 5-HT
12
Q
MDMA
A
Promotes serotonin release
Often by causing uptake pumps/transporters to work in reverse
Increase 5-HT
13
Q
5-HTP
A
Precursor of 5-HT
14
Q
L-tryptophan
A
Precursor of 5-HT
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
16
Q
Epinephrine
A
Constricts blood vessels
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
18
Q
Rifampicin
A
CYP3A4 Inducer
19
Q
Phenytoin*
A
CYP3A4 Inducer
20
Q
Carbamazepine*
A
CYP3A4 Inducer
21
Q
Glucocorticoids*
A
CYP3A4 Inducer
22
Q
Grapefruit Juice
A
CYP3A4 Inhibitor
23
Q
Erythromycin*
A
CYP3A4 Inhibitor
24
Q
Ciprofloxacin*
A
CYP3A4 Inhibitor
25
Components of peptidoglycan
Glycan strands alternating
N-Acetylglucosamine
N-Acetylmuramic acid
26
Glycotransferase
GT
Assembles chains of glycan into peptidoglycan chains
27
Transpeptidase
PT/Penicillin Binding Protein
Cross-links chains of peptidoglycan
28
Penicillin
Cell Wall Inhibitor, bacteriocidal
Inhibit DD-transpeptidase enzyme / penicillin-binding protein
Works only on gram positive
29
Cephalosporin
Cell Wall Inhibitor, bacteriocidal
Inhibit DD-transpeptidase enzyme / penicillin-binding protein
Works only on gram-positive and gram-negative
More effective on gram-positive
30
Beta-lactamases
Inhibits beta-lactam rings of certain penicillins and cephalosporins
Found in most gram-negative and staphylococci
Confers resistance
31
Clavulanic Acid
Beta-lactamase inhibitor
Protects penicillins and cephalosporins that can be potentially hydrolyzed
32
Vanomyocin
Cell Wall Inhibitor
Not a beta-lactam ring
Inhibits peptidoglycan cross-linking
Produced by Actinobacteria and Amycolatopsis orientalis
33
PABA
Para-aminobenzoic acid
Is converted by dihydropteroate synthase into dihydrofolic acid
34
Dihydrofolic acid
Is converted by Dihydrofolate reductase into tetrahydrofolic acid
35
Tetrahydrofolic acid
Is converted into purines (Nucleic acids) which are used to synthesize DNA
36
Sulfonamides
Competes with PABA for Dihydropteroate synthase
Interferes with PABA metabolic pathway preventing DNA synthesis
37
Trimethoprim
Competes with Dihydrofolic acid for Dihydrofolate reducatase
Interferes with PABA metabolic pathway preventing DNA synthesis
38
70S ribosomal complex
Bacteria Ribosomal Subunits
30S and 50S
39
80S ribosomal complex
Euk Ribosomal subunits
40S and 60S
40
Chloramphenicol
Binds to 50S subunit
Prevents transpeptidation (movement of amino acid onto growing chain)
41
Tetracycline
Binds to 30S subunit
Prevents binding of tRNA to to the ribosome
42
Macrolides
Binds to 50S subunit
Prevents transpeptidation (movement of amino acid onto growing chain)
43
Aminoglycosides
Binds to 30S subunit
Blocks initiation of complex
Causes misreadings of mRNA template, wrong proteins are created
Inhibits translocation
44
Poxvirus
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
Influenza Virus
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
HIV Virus
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
Acyclovir
Anti-Herpes
Fake nucleoside analog
Lacks hydroxyl group, causing DNA chain termination
Must be phosphorylated to acyclovir-triphosphate
48
Thymidine Kinase
Herpes Virus
Performs first phosphorylation on acyclovir
Has high affinity for acyclovir
49
HIV / Infects what?
CD4+ T-Cells
Body loses cell-mediated immunity and becomes susceptible to infections (AIDS)
50
HAART
Highly Active Antiretroviral Therapy
Drug combinations to slow HIV
51
Maraviroc
Entry Inhibitor
CCR5 receptor antagonist
Binds to CCR5 receptor and prevents HIV from binding to CD4 receptors using their gp120 proteins
52
NRTI
Nucleotide Reverse Transcriptase Inhibitors
Small molecules that mimic host nucleosides
Lack 3' hydroxyl group causing chain termination
53
Raltegravir
Integrase Strand Transfer Inhibitor (INSTs)
Prevents the action of integrase that causes the injection of the viral genome into the cell
54
Protease Inhibitor
Aspartate proteases cleave precursor proteins to form the final mature virion core
Protease inhibitors prevent formation of the mature HIV
Used with NRTI
55
Amantadine
Prevents Influenza A
Blocks H+ from entering M2, prevents acidification and activation of viral transcription
56
Zanamivir
Prevents Influenza A and B
Inhibits neuroaminidases from cleaving sialic acid residues from viral proteins, prevents the release of virus from host
57
p53
Tumour suppressor protein that regulates cell cycle
Inhibits cell division
Initaite apoptosis following irreversible DNA damage
DNA repair proteins (BRCA)
58
BRCA
DNA repair proteins
59
Proto-oncogenes
Normal genes involved in cell growth, proliferation, or inhibition of apoptosis
60
Oncogene
Mutation in a proto-oncogene that increases expression and proliferation
61
BCR-ABL
Philadelphia chromosome
ABL1 gene chromosome 9
Tyrosine kinase activity, controls cell division
BCR gene chromosome 22
Very strong promoter
62
5-Fluorouracil
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
6-mercaptopurine
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
Cisplatin
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
Methotrexate
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
Vinca Alkaloids
Periwinkle Plant
Inhibit tubulin polymerization
Disrupts microtubule assembly in miotic spindle apparatus (M phase)
67
Taxanes
Pacific yew tree
Promote microtubule assembly through high-affinity binding
Inhibits microtubule depolymerization (M phase)
68
Paclitaxel
Taxane
Inhibits microtubule depolymerization
69
Camptothecins
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
Anthracycline
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
Imatinib
Tyrosine Kinase Inhibitors
Inhibits the tyrosine kinase domain of the BCR-ABL oncoprotein
Treats leukemia
72
Cetuximab
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
Tamoxifen
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
