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Fundamentals of Pharm Flashcards

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1
Q

Kd - Affinity

A

strength of reversible interaction between a drug and its receptor

Kd = concentration that occupies 50% of receptors (lower the Kd, higher the affinity)

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2
Q

ED50 - Potency

A

Concentration of drug required to produce a specific effect

ED50= dose that produces 50% max effect

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3
Q

Efficacy

A

How much drug do you need to reach max effect (at or close to 100%)

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4
Q

Effect of competitive antagonists on potency/efficacy

A

Potency: shifts to right/decreases
Efficacy: stays the same

(can be overcome with more agonst)

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5
Q

Effect of non-competitve antagonists on efficacy

A

Efficacy/Emax decreases

(cannot be overcome by adding more agonist bc receptor is not available anymore)

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6
Q

Physiological antagonism

A

two agonists bind different receptors and their responses oppose each other

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7
Q

Chemical antagonism

A

direct interaction with the agonist instead of the receptor

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8
Q

Partial agonist Emax

A

will never reach Emax

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9
Q

With spare receptors you are able to elicit a max response without _ occupancy of all receptors

This is done by using _ to compensate loss up to a certain point.

A

agonist
antagonist

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10
Q

Assumptions of dose-response relationship:
- Intensity of a response is directly proportional to ___
- One drog molecule binds to ___
- Amt of drug binding to a receptor is __ compared to the total amount of the available drug
- binding is _ and _ duration
- binding of one receptor _ affect another

A

Number of occupied receptors
one receptor
small
reversible, short
does not

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11
Q

ED50 = _effect
TD50= _ effect
LD50 = _ effect

A

50% therapeutic effect
50% toxic effect
50% lethal on animals

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12
Q

Formula for therapeutic index

A

TI = TD50/ED50 (toxic/therapeutic)

(therapeutic window is space between therapeutic and toxic that is the range that elicits desired response

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13
Q

what is the difference between cytokine receptors and receptors like tyrosine kinase

A

enzymatic activity is not built into the receptor

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14
Q

beta adrenergic amines, histamine, seratonin, and hormones require _ protein

A

Gs

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15
Q

Gs –> _ AC and _ cAMP
Gi –> _ AC and _ cAMP in turn opening cardiac K channels and _ HR

A

increase, increase
decrease, decrease, decreasing

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16
Q

alpha-2 adrenergic amines, ach, opioids, and seratonin require _ protein

A

Gi (M2 of muscarinic ach)

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17
Q

Gq –> _ PLC, _ IP3, _ DAG in turn _ cytosolic calcium

A

increase, increase, increase
increasing

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18
Q

Ach, serotonin, and many other reeceptors require _ protein

A

Gq (M1/3 of muscarinic ach)

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19
Q

rank these in speed:

nuclear receptors
g protein coupled receptors
ligand gated ion channels
kinase linked receptors

A

ligand gated - milliseconds due to voltage only
G-proteins - seconds due to second messengers
Kinase linked/nuclear receptors - hours due to gene transcription alterations and protein synthesis

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20
Q

Formula for loading dose

A

LD = Css x Vd

(note Vd = total/blood)
Css= target concentration

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21
Q

formula for maintenance dose

A

MD = Css x T/F

T = time interval
F = bioavailability
bioavailability = amount that reaches circulation/dose

this is steady state bc amount of drug given = its elimination, administer at constant time intervals like every 4 hrs

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22
Q

Elimination definition
Clearance definition

A

AMOUNT of chemical that is removed by metabolism per unit time - mg

VOLUME of body fluid from which the chemical is removed by metabolism - mL (relates to creatinine clearance)

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23
Q

Formula for elimination

A

K = CL/C

K = rate of elimination
C = concentration
CL = clearance = K/C

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24
Q

Formula for clearance

A

CL = K/C

K = rate of elimination
C = concentration
CL = clearance = K/C

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25
In relation to the glomerulus: - if renal clearance = creatinine clearance then the drug __ - if renal clearance > creatinine clearance then the drug _ - if renal clearance < creatinine clearance then the drug _
eliminated via the glomerulus bypasses the glomerulus and goes through tubular secretion passively reabsorbed back to blood or bound to a plasma protein
26
Formula of volume distribution
Vd = Ab/C Ab = total amt of drug in body C = concentration of drug in blood
27
A low Vd indicates _ A high Vd indicates _
drug is retained in vascular compartment drug is absorbed into tissues
28
definition of volume distribution
measure of apparent space in the body available to contain the drug tells us where drugs are spending their time
29
Bioavailability definition
fraction of administered dose of a drug that reaches the systemic circulation in an active form
30
formula for bioavailability
F = amount absorbed /dose "area under the curve" IV has 100% bioavailability
31
pH of stomach is _ to _ Absorbs pka of _ to _
1-2 3-3.5
32
pka is the level where
50% is ionized and 50 is not
33
pH of small intestine is _ to _ absorbs pka of _ to _
4-8 6.3-6.5
34
weak base pka is _ then you go up _ and down _
8.2 2,3 (6.2,7.2etc)
35
weak acid pka is _ then you go up _ and down _
3.8 2,3 (1.8,2.8 etc)
36
4 determining factors of distribution
blood flow (liver is highly perfused, more oxygen, adipose poorly perfused) specific tissue barriers (BBB) tissue binding (adipose/bone) plasma protein binding (albumin)
37
we want drug to be in _ and _ form
fat soluble, non-ionized, liquid form (water soluble dissociate into ions)
38
Drug saftey and efficacy laws (3)
pure food/drug act (labeling) food drug and cosmetic act (efficacy) - durham humphry (prescribe) - kefauver harris (animals then humans) orphan drug act (incentives)
39
drug abuse and prevention laws (2)
harrison narcotics act (tax stamps) controlled substance act (class via schedule)
40
pure food and drug act
labeling of ingredients
41
food drug and cosmetic act concentrated on _ subtypes: - durham and humphrey amendment - kefauver harris amendment
efficacy OTC vs prescription, some must be prescribed saftey/efficacy on animals then humans
42
orphan drug act
incentives/tax benefits to research tx of rare disease
43
harrison narcotic act
controlled narcotics via use of tax stamps on legal drug products but didnt make them illegal
44
controlled substance act
classified drugs with abuse potential into 5 schedules - all providers must register w/ DEA risk of abuse and risk for someone to become dependent schedule 1 - not cucrently accepted into tx (marijuana, heroin) 2: currently accepted w/ severe restriction (morphine) 3-5:accepted
45
how long is step 1: disocovery and chracterization what is goal
2-10 years screening tests to determine biological activity
46
how long is step 2: preclinical trials
3-6 years toxicity to animals - harmful to organs - mechanism of action - pharmokinetics - therapeutic effects - toxicty
47
how long is step 4: clinical trials
6-7 yrs phase 1: healthy humans Phase 2: sick humans phase 3: large scale efficacy w/ placebos
48
list steps of drug development
1-discovery/characterization 2-preclinical studies 3- IND app (investigational new drug app) 4- clinical trials 5- submission of NDA (new drug app) 6- approval of NDA 7- post-maketing survaillance via FAERS
49
4 factors that effect drug saftey/efficacy
age, disease, prenancy, lactation
50
4 adverse events that may lead to a black box warning
excessive pharmacologic activity idiosyncratic rxns (not known to pharm property) organ toxicity like cardiomyopathy drug hypersensitivity
51
what drug application is most potent
transdermal due to lipid solubility for kin penetration
52
NANC
nitric oxide actng as post synaptic ganglion nt - can be retrograde to feed pre synaptic ganglion drives glutamate to stimulate
53
Adrenergic receptors are _ receptors Pertain to the _ system Alpha receptors respond to Beta receptors respond to
GPCR sympathetic/ANS NE has higher affinity EPI has equal affinity EPI has equal affinity (more effective) note alpha 2 is inhibibtory
54
Nicotinic receptors are _ Pertain to the _ system(s)
ligand gated ion channels somatic Ach, all pregangs
55
Nm
Nicotinic opening of Na/K channels for depolarization skeletal muscle and neuromuscular end plates
56
Nn
Nicotinic opening of Na/K channels and depolarization post ganglionic neurons
57
Muscarinic receptors are
GPCR on all all postgangs except somatic
58
What kind of G stimulation is the following M1 M2 M3
Gq stimulation of sympathetic post gangs Gi inhibition, k channel opening, smooth muscle/myocardium Gq stimulation of endocrine gland, smooth muscle, endothelium
59
rate limiting enzyme of NE synthesis how do you make epi
tyrosine hydroxylase add ch2 to ne
60
enzyme that loads pre-ne onto vesicles
VMAT
61
degrader of NE
MAO/COMT
62
rate limiting enzyme of Ach synthesis
acetyl choline acetyltransferase adds choline + acetyl coA together
63
enzyme that loads pre-ach onto vesicles
VAT
64
degrader of ach
acetylcholineesterase

Clinical Medicine (3 decks)

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