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Clinical Medicine > Fundamentals of Pharm > Flashcards

Fundamentals of Pharm Flashcards

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
Q

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 _
A

eliminated via the glomerulus

bypasses the glomerulus and goes through tubular secretion

passively reabsorbed back to blood or bound to a plasma protein

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26
Q

Formula of volume distribution

A

Vd = Ab/C

Ab = total amt of drug in body
C = concentration of drug in blood

27
Q

A low Vd indicates _
A high Vd indicates _

A

drug is retained in vascular compartment

drug is absorbed into tissues

28
Q

definition of volume distribution

A

measure of apparent space in the body available to contain the drug

tells us where drugs are spending their time

29
Q

Bioavailability definition

A

fraction of administered dose of a drug that reaches the systemic circulation in an active form

30
Q

formula for bioavailability

A

F = amount absorbed /dose

“area under the curve”
IV has 100% bioavailability

31
Q

pH of stomach is _ to _
Absorbs pka of _ to _

A

1-2
3-3.5

32
Q

pka is the level where

A

50% is ionized and 50 is not

33
Q

pH of small intestine is _ to _
absorbs pka of _ to _

A

4-8
6.3-6.5

34
Q

weak base pka is _

then you go up _ and down _

A

8.2

2,3 (6.2,7.2etc)

35
Q

weak acid pka is _

then you go up _ and down _

A

3.8

2,3 (1.8,2.8 etc)

36
Q

4 determining factors of distribution

A

blood flow (liver is highly perfused, more oxygen, adipose poorly perfused)

specific tissue barriers (BBB)

tissue binding (adipose/bone)

plasma protein binding (albumin)

37
Q

we want drug to be in _ and _ form

A

fat soluble, non-ionized, liquid form

(water soluble dissociate into ions)

38
Q

Drug saftey and efficacy laws (3)

A

pure food/drug act (labeling)
food drug and cosmetic act (efficacy)
- durham humphry (prescribe)
- kefauver harris (animals then humans)
orphan drug act (incentives)

39
Q

drug abuse and prevention laws (2)

A

harrison narcotics act (tax stamps)
controlled substance act (class via schedule)

40
Q

pure food and drug act

A

labeling of ingredients

41
Q

food drug and cosmetic act concentrated on _

subtypes:
- durham and humphrey amendment
- kefauver harris amendment

A

efficacy

OTC vs prescription, some must be prescribed

saftey/efficacy on animals then humans

42
Q

orphan drug act

A

incentives/tax benefits to research tx of rare disease

43
Q

harrison narcotic act

A

controlled narcotics via use of tax stamps on legal drug products but didnt make them illegal

44
Q

controlled substance act

A

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
Q

how long is step 1: disocovery and chracterization
what is goal

A

2-10 years
screening tests to determine biological activity

46
Q

how long is step 2: preclinical trials

A

3-6 years
toxicity to animals
- harmful to organs
- mechanism of action
- pharmokinetics
- therapeutic effects
- toxicty

47
Q

how long is step 4: clinical trials

A

6-7 yrs
phase 1: healthy humans
Phase 2: sick humans
phase 3: large scale efficacy w/ placebos

48
Q

list steps of drug development

A

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
Q

4 factors that effect drug saftey/efficacy

A

age, disease, prenancy, lactation

50
Q

4 adverse events that may lead to a black box warning

A

excessive pharmacologic activity
idiosyncratic rxns (not known to pharm property)
organ toxicity like cardiomyopathy
drug hypersensitivity

51
Q

what drug application is most potent

A

transdermal due to lipid solubility for kin penetration

52
Q

NANC

A

nitric oxide actng as post synaptic ganglion nt - can be retrograde to feed pre synaptic ganglion

drives glutamate to stimulate

53
Q

Adrenergic receptors are _ receptors
Pertain to the _ system

Alpha receptors respond to
Beta receptors respond to

A

GPCR
sympathetic/ANS

NE has higher affinity
EPI has equal affinity

EPI has equal affinity (more effective)

note alpha 2 is inhibibtory

54
Q

Nicotinic receptors are _
Pertain to the _ system(s)

A

ligand gated ion channels
somatic Ach, all pregangs

55
Q

Nm

A

Nicotinic
opening of Na/K channels for depolarization
skeletal muscle and neuromuscular end plates

56
Q

Nn

A

Nicotinic
opening of Na/K channels and depolarization
post ganglionic neurons

57
Q

Muscarinic receptors are

A

GPCR
on all all postgangs except somatic

58
Q

What kind of G stimulation is the following

M1
M2
M3

A

Gq stimulation of sympathetic post gangs

Gi inhibition, k channel opening, smooth muscle/myocardium

Gq stimulation of endocrine gland, smooth muscle, endothelium

59
Q

rate limiting enzyme of NE synthesis

how do you make epi

A

tyrosine hydroxylase

add ch2 to ne

60
Q

enzyme that loads pre-ne onto vesicles

A

VMAT

61
Q

degrader of NE

A

MAO/COMT

62
Q

rate limiting enzyme of Ach synthesis

A

acetyl choline acetyltransferase adds choline + acetyl coA together

63
Q

enzyme that loads pre-ach onto vesicles

A

VAT

64
Q

degrader of ach

A

acetylcholineesterase

Clinical Medicine (3 decks)

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