Summery Info-DD Flashcards

(94 cards)

1
Q

Phase One Reactions

A

Oxidations
Hydrolysis
Reductions

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2
Q

Phase Two Reactions

A

Conjugations

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3
Q

Phase One Enzymes

A

CYP450
esterase-amidase
reductase

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4
Q

Phase Two Enzymes

A

Transferase

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5
Q

Gen Polymorph Phase 1 and 2

A

significant

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6
Q

Phase One Induce- Inhibit

A

Significant

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7
Q

Phase Two Induce-Inhibit

A

Possible- Less

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8
Q

FDA Regulates

A

Drugs to be sold to the public
Evaluate new drug safety
Prescription vs non

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9
Q

State regulates

A

who can prescribe drugs

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10
Q

Local regulates

A

drug use in their area

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11
Q

Schedule 1

A

no medical use
high abuse potential
high phys/psy dependance

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12
Q

Schedule 2

A

medical use
high abuse potential
high phy/psy dependence

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13
Q

Schedule 3`

A

Medical use
Moderate abuse potential
moderate/high dependence

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14
Q

Schedule 4

A

medical use
Low abuse
Low dependence

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15
Q

Schedule 5

A

medical use
limited abuse
lowest dependence

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16
Q

Phase One CT

A

is it safe?
Pharmacodynamics- metabolism, toxicity, response

~100 Healthy human

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17
Q

Phase Two CT

A

Does it work in patients?- compare placebo/existing treatment with new
Also safety and dose

200-300 Subjects

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18
Q

Phase Three CT

A

Does it work Double Blind-

a. Compare established therapies
b. Adverse rxn studies
c. FDA grants approval

1000-6000 people

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19
Q

Phase Four CT

A

Post market surveillance

a. Mortality/morbidity
b. Physicians must report adverse reactions

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20
Q

Animal Studies

A

Follows in vitro tests (synthesis and bio products)
Efficacy
Safety
Mechanism

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21
Q

Most rapid (sec to min) onse

A

Inhalational (volatile gas-aerosol), intravenous

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22
Q

Intermediate (5-15 min) onset

A

Sublingual, intramuscular, subcutaneous, buccal

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23
Q

Slower (15-30 min) onset

A

Oral - immediate release formulations

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24
Q

Slowest Onset (hours)

A

Transdermal, Oral - enteric-coated and sustained release formulations, IM and SC (depot forms)

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25
Vd 3-5 compartment
Highly bound to plasma proteins
26
Vd 12-15 compartment
Highly water soluble. enters the cell poorly
27
Vd 42 L compartment
drugs that freely enter cells
28
Over 50 Vd
often highly lipid soluble | Sequesters at spesific site ex: CNS, Fate, Protein
29
pH>pKa
A- and B predominate
30
pH
HA and BH+ predominate
31
Inducer/Inhibitor definition
Inducer: Increase CL (7-10 days) Inhibitor: Inhibit CL, inc drug levelsto possibly toxic
32
Cimetidine
Inhibitor
33
Phenytoin
Inducer
34
Erthromycin/clarithromycin
inhibitor
35
Azol Antifungal
Inhibitor
36
Carbamazepine
Inducer
37
Phase One saturablity
minimal
38
Phase Two saturablity
substantial
39
Rifampin
Inducer
40
Fluoxetine
Inhibitor
41
Grapefruit Juice
Inhibitor
42
Phenobarbital
Inducer
43
Ethanol
Inducer
44
St. Johns Wort
Inducer
45
HIV protease inhibitor
inhibitor
46
Tobacco Smoke
Inducer
47
Omeprazole
Inhibitor
48
Acetaminophen poison
N-acetylcysteine (Mucomyst)** antidote
49
Methanol, ethylene glycol poison
Ethanol, 4-methylpyrazole (Antizol)** antidote
50
Pregnancy risk A
no known risk to the fetus
51
Pregnancy risk B
no evidence for risk in humans
52
Pregnancy risk C
Risk cannot be ruled out (no studies or bad animal studies)
53
Pregnancy risk D
Positive risk, life threatening situations only | when use outweighs harm
54
Pregnancy risk X
DO NOT USE | risks outweigh any benefit
55
Chemical Antagonist
No receptor involved
56
Physiological Antagonist
Acts on a separate receptor
57
Allosteric binding
noncompetitive
58
Irreversible active site binding
non competitive
59
Reversible active site binding
competitive
60
bio-equivalent products are considered to be
therapeutic equivalent
61
Cmax
measures rate of absorption | Measure of bioequivalence
62
Tmax
measure rate of absorption | Measure of bioeq
63
AUC
measures extent of absorption
64
Controlled substance potentials
Medical usefulness Abuse potential Dependence risk
65
Colorado Controlled Substance Prescription requirements
requires a prescription for schedule V | and 2-4
66
Abbreviations to avoid | ~timing
qd qid qod
67
Abbreviations to avoid | ~Routes
``` ad as, al au od os, ol ou ```
68
Tight cellular junction compartments
BBB Gut Kidney REABSORPTION
69
Factors affecting membrane passage
Molecular size- plasma protein binding lipid solubility- oil water partion degree of ionization- affected by tissue pH concentration gradient- at site of admin
70
Passive diffusion through membrane
Lipid soluble drugs
71
Passive diffusion of water soluable drugs
aq channels
72
Routes affected by first pass metabolism
oral, rectal
73
Routes for systemic effect
``` oral rectal sub lingual/buccal intravenous IM sq Volitle inhalation Trandermal ```
74
Drug bioavailability
fraction of dose reaching blood
75
Rate of onset of drug effect
time to peak effect
76
Duration of drug action
time above MEC
77
Single dose equation
cp=DOSE/Vd
78
Endogenous/Phase2
substrate combines with pre-existing or metabolically inserted functional group (via Phase I reaction) on the drug
79
Time to see drug induction
7-10 days
80
Inhibition time frame
hours, dependent on the inhibited drug’s half-life
81
First order kinetics
Proportional clearance (fraction) Most drugs follow this patter Hepatic and renal
82
Zero order kinetics
Constant clearance
83
Time to eliminate a drug
4-5 half lives
84
Time to reach steady state
4-5 half lives
85
Inducers and inhibitors affect which metabolism?
Hepatic
86
Potency
concentration (EC50) or dose (ED50) required to produce 50% of the individual drug’s Emax
87
Emax
limit of dose-response relationship on response (y) axis most important determinant of clinical utility
88
antagonist definition
binds to the drug receptor but is unable to bring about the characteristic response rather, it blocks response
89
Competitive Antagonist graphical changes
EC50 increases (potency decreases) - Emax unchanged (surmountable)
90
non-Competitive Antagonist graphical changes
Minimal effect on EC50 - Emax is reduced (insurmountable)
91
Toxic doses of acetaminophen
N-acetylcysteine antidote Gastric lavage helps to prevent hepatic cell death
92
acetaminophen with ethenol
causes hepatic cell death
93
Methanol Poisoning toxin
formaldehyde formic acid treated with ethanol
94
Ethylene gycol toxin
oxalic acid treated with ethanol