PED2001

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What fills the gaps in the membrane of cells
protein matrix
1 of 84
What are benzylpenicilin and insulin inactivated by
gastric acid
2 of 84
what ensures consistency of rate delivered in transdermal patches
drug in excess
3 of 84
what is an advantage of IV administration
avoids first pass metabolism
4 of 84
What is inhalation mostly used for
respiratory problems
5 of 84
how do spacers help inhalation of respiratory drugs
reduce velocity of particles
6 of 84
what is liposome encapsulation used for
gradual release
7 of 84
what makes a drug bioequivalent
comparable bioavailability and similar peak conc times
8 of 84
what causes the bioinequvalence toxicity of phenytoin
switch from calcium phosphate to lactose
9 of 84
how do local anaesthetics prevent drug being carried away
contain adrenaline to cause vasoconstriction
10 of 84
Why do ADCs have a more effective mode of action
directed toward certain receptor
11 of 84
pro drugs minimise side effects by doing what
only activated in site of interest
12 of 84
What is Vd
hypothetical volume of liquid in which the drug is disseminated
13 of 84
what happens when class I and class II drugs administered together
displacement of class I, so conc of class I free drug high
14 of 84
Which CYP does grapefruit juice inhibit
CYP3A4
15 of 84
where does CYP xenobiotic metabolism occur
ER
16 of 84
Where does CYP steroid, fatty acid and vitamin oxidation occur
ER
17 of 84
Where does CYP steroid biosynthesis occur
mitochondria
18 of 84
what is the iron atom coordinated to
4 nitrogens and cysteine
19 of 84
what is in the 6th coordination position
water
20 of 84
name one thing needed for CYP metabolism
NADPH-cytochrome P450 reductase
21 of 84
name another thing needed for CYP metabolism
phosphatidylcholine
22 of 84
Which flavoproteins are needed for NADPH-cytochrome P450 reductase
FAD and FMN
23 of 84
name an inducer of CYPs
PAH
24 of 84
what are the main substrates of CYP2D6
cardiovascular agents
25 of 84
What is true about CYP2D6
have basic nitrogen and hydrophobic region
26 of 84
what is CYP2D6 induced by
nothing
27 of 84
What are the main substrates of CYP2C9
NSAIDs
28 of 84
What is true of CYP2C9
have strong hydrogen bond potential
29 of 84
What is true of CYP3A4
large binding site to accommodate large molecules
30 of 84
What is CYP2C9 inducible by
barbiturates
31 of 84
What prosthetic group do FMOs have
FAD
32 of 84
what are the requirements of FMOs
NADPH and O2
33 of 84
What is true of prostaglandin H-synthase
has COX activity
34 of 84
What are MAOs dependant on
FAD
35 of 84
MAOs main substrate
neurotransmitters
36 of 84
Oxidoreductases dependant on
NADP in oxidising direction, NADPH in reducing direction
37 of 84
What does alcohol dehydrogenase do
convert alcohols to carbonyls
38 of 84
What is a co factor of alcohol dehydrogenase
NAD+
39 of 84
What does NADPH quinone oxidoreducatse do
directly reduces quinones to hydroquinones
40 of 84
hCE1 prefers what
small alcohol group, large acetyl group
41 of 84
what does hCE2 prefer
large alcohol group, small acetyl group
42 of 84
What is glucuronidation carried out by
UDP-GTs
43 of 84
what is the co-factor in glucuronidation
UDP-glucuronic acid
44 of 84
when is a drug excreted in the bile
when its MW is >400
45 of 84
what are UDP-GTs induced by
phenobarbitone and PAHs
46 of 84
What is the main liver sulphotransferase isoform
SULT1A1
47 of 84
what is a side effect of sulfation
activation of carcinogens
48 of 84
Where does amino acid conjugation take place
mitochondria
49 of 84
What is the initial AA conjugation reaction carried out by
CoA ligases
50 of 84
In AA conjugation reactions, what group is targeted
carboxyl group
51 of 84
Acetyltransferases donate what
acetyl groups
52 of 84
What are the main human isoforms in the liver
NAT1, NAT2
53 of 84
How does glutathione bond
nucleophilic cysteine thiol group
54 of 84
What toxic metabolite is produced from paracetamol metabolism
NAPQI
55 of 84
Which methyltransferase targets catechol and phenol
O-methyltransferases
56 of 84
Which methyltransferase targets histamine and nicotinamide
N-methyltransferases
57 of 84
Which methyltransferase targets thiopurine and thiol
S-methyltransferases
58 of 84
What is the cofactor for methyltransferases
SAM
59 of 84
Type I isoform specific inhibitors do what to inhibit CYP function
Push Fe3 into high spin state
60 of 84
Type II isoform specific inhibitors do what to inhibit CYP function
Replace 6th protein ligand
61 of 84
What does competitive inhibition mean
blocks interaction
62 of 84
What is mixed inhibition
interacts with haem group
63 of 84
What is a suicide substrate
Irreversibly binds to enzyme to stop substrate binding
64 of 84
Example of suicide substrate for CYP3A4
troleandomycin
65 of 84
What causes an ultra-rapid metaboliser
extra copies of CYP2D6 gene
66 of 84
What does the CYP2D6*4 mutation cause
change in splice site
67 of 84
Which acetylator is mutated in slow acetylators
NAT2
68 of 84
Why are liver S9 fractions used in experiments
more representative
69 of 84
If CLr<fu x GFR, what is happening
renal reabsorption
70 of 84
If CLr>fu x GFR, what is happening
filtered and cleared by active tubular secretion
71 of 84
What is a standard measurement of renal function
creatine clearance
72 of 84
What is a factor with GFR in old age
decreases, lower dose needed
73 of 84
what is the name of the process where the free drug is reabsorbed and cycle repeated
enterohepatic circulation
74 of 84
How do SLC-encoded facilitative proteins transport drugs
flow downhill with gradient
75 of 84
How do SLC-encoded secondary active proteins transport drugs
coupled with co-substrate
76 of 84
What membrane do OATP proteins transport drugs across
sinusoidal membrane into liver
77 of 84
What is special about the drug substrates transported by OATP proteins
generally protein bound
78 of 84
Where is the OAT4 protein located
apical membrane facing urine
79 of 84
Where is the OCT1 protein located
sinusoidal face of liver
80 of 84
What is a substrate of OCT1
metformin, cisplatin
81 of 84
Along with metformin and cisplatin, what is the other substrate of OCT2
cimetidine
82 of 84
What is not a substrate of PEPT1/2
statins
83 of 84
What do MATE transporters contribute to
excretion of cations
84 of 84

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Card 2

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What are benzylpenicilin and insulin inactivated by

Back

gastric acid

Card 3

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what ensures consistency of rate delivered in transdermal patches

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Card 4

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what is an advantage of IV administration

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Card 5

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What is inhalation mostly used for

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