Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Foundations 1 > Pharm > Flashcards

Pharm Flashcards

1
Q

Drug

A

Chemical capable of reacting w/ biological systems

Can be endogenous or foreign

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Toxin

A

Chemical that produces undesirable effects

Synthesized by plants, microorganisms, animals, insects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Poison

A

Chemical that produces undesirable effects

Synthetic or inorganic compound

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Pharmacodynamics

A

Drug’s effect on body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Pharmacokinetics

A

Body’s effect on drug

ADME

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Imantinib

A

Anti-cancer drug that interacts w/ BCR-Abl kinase A (rearrangement of 9 and 22 that causes tyrosine kinase to be always “on”, phosphorylates a target important in cell proliferation)
Inhibits phosphorylation of activation group
Not toxic to any other cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Ligand-gated transmembrane ion channel receptor

A

Activated by binding of ligand

Ex. Nicotinic receptor (ACh binds to 2 alpha subunits and opens Na+ gate)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Voltage-gated transmembrane ion channel receptor

A

Activated by change in transmembrane voltage gradient

Ex. tetrodotoxin in puffer fish inactivates fast Na+ channel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Second-messenger gated transmembrane ion channel receptor

A

Activated by binding of ligand to G protein-coupled receptor w/ cytosolic domain, which activates a second messenger
Ex. cAMP –> PKA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

G protein-coupled receptor

A

Ligand binds to receptor –> receptor changes conformation –> alpha subunit dissociates and diffuses to nearby effector
Ex. activation of adenylyl cyclase to form cAMP –> PKA and PLC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Transmembrane receptors w/ catalytic intracellular domain

A 
Receptor tyrosine kinases
Receptor tyrosine phosphatases
Receptor serine/threonine kinases
Non-receptor tyrosine kinases
Receptor guanylyl cyclases
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Cytoplasmic/nuclear receptor

A

Receptor AND/OR transcription factor

Ex. hormone receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Tachyphlaxis

A

Repeated administration of the same dose of a drug results in a reduced effect of the drug over time

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Desensitization

A

Decreased ability of a receptor to respond to stimulation by a drug or ligand

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Homologous desensitization

A

Decreased response at a single type of receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Heterologous desensitization

A

Decreased response at 2+ types of receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Inactivation

A

Loss of ability of a receptor to respond to stimulation by a drug or ligand

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Refractory

A

After a receptor is stimulated, a period of time is required before the next drug-receptor interaction can produce an effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Down-regulation

A

Repeated or persistent drug-receptor interaction results in removal of the receptor from sites where subsequent drug-receptor interactions could take place

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Receptor

A

Site on cell or organism that binds w/ endogenous substance or drug that initiates a chain of biochemical events that leads to a response
Number limits response to drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Inert binding sites

A

Proteins that bind and sequester drug and prevent it from performing its intended function
After withdrawn, the drug can come off and produce an effect
Ex. serum albumin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Agonist

A

Produces maximal response when receptors are fully occupied

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Partial agonist

A

Produces lower than maximal response at full receptor occupancy
Can act as antagonist if coupled w/ full agonist

24
Q

Antagonist

A

Prevents action of agonist (doesn’t do anything on its own)

Doesn’t change binding site

25
Q

Ligand

A

Molecule that binds to a receptor

26
Q

Drug-receptor interaction (equation)

A

[D][R]/[DR] = k2/k1 = Kd

27
Q

Low Kd

A

High affinity, very potent

Administered in small amounts

28
Q

High Kd

A

Low affinity, less potent

Administered in larger amounts

29
Q

Ligand-receptor binding curve (equation)

A

[DR]/[Rt] = [D]/(Kd + [D])

Plots as rectangular hyperbola

30
Q

Kd

A

Concentration of ligand at which half of the receptors are occupied

31
Q

Occupancy-response curve (equation)

A

E/Emax = [D]/(Ke + [D])
Maximal effect
Ke = value of DR that exhibits half-maximal response

32
Q

Drug potency

A

Concentration at which the drug elicits 50% of its maximal response (EC50)

33
Q

Drug efficacy

A

Maximal response produced by the drug (how strong the reaction is) (Emax)
State at which receptor-mediated signaling is maximal and any additional drug will produce no additional response
Comparatively, doesn’t depend on how much drug you give

34
Q

Effective Dose (ED50)

A

Dose at which50% of the population experiences a therapeutic effect

35
Q

Toxic Dose (TD50)

A

Dose at which 50% of the population experiences a toxic effect

36
Q

Lethal Dose (LD50)

A

Dose at which 50% of the population experiences a lethal effect

37
Q

Therapeutic Index

A

TI = TD50/ED50
High TI- large separation between effective dose and toxic dose, drug will be very effective w/o adverse effects
Low TI- small separation between effective dose and toxic dose, have to be careful!

38
Q

Margin of Safety

A

MS = LD1/ED99
Compares concentration of drug that is lethal to first 1% of population to concentration that is effective in 99% of population
Low MS- not safe, will cause some deaths, even at concentration that is therapeutic in most patients
High MS- safe, will affect most patients in therapeutic way w/o causing death

39
Q

Inverse agonist

A

Binds receptor in inactive state and reduces fraction of receptors in active state
Causes opposite effect of agonist

40
Q

Active site antagonist

A

Antagonist binds to same site as ligand

Can be reversible (competitive) or irreversible (noncompetitive)

41
Q

Allosteric site antagonist

A

Antagonist binds to different site than ligand
Can be reversible or irreversible (both noncompetitive)
A “ceiling” to the effect exists (once all sites are occupied, no further effect is observed)

42
Q

Chemical antagonist

A

Receptors are not involved
Activity is based on chemical interactions
Ex. Heparin (negatively charged) binds protamine (positively charged) to inactivate it

43
Q

Physiologic antagonist

A

Opposing pathways must be activated to produce antagonism

Ex. glucagon increases blood glucose, insulin decreases blood glucose

44
Q

Competitive antagonist effect on D-R curve

A

Reduces potency of agonist and increases Kd (curve shifts to right)
Does NOT affect efficacy

45
Q

Noncompetitive antagonist effect on D-R curve

A

Reduces efficacy of agonist and lowers response/decreases Emax (curve height decreased)
Does NOT change Kd or potency

46
Q

Spare receptors

A

Full response doesn’t require occupancy of all receptors
More receptors are present than are needed to produce Emax
System is more sensitive to drugs (b/c low concentration of drug occupies same number of receptors)

47
Q

Spare receptor effect on D-R curve

A

Lower concentration of drug gives half maximal effect (curve is shifted left wrt drug-receptor curve)

48
Q

Noncompetitive antagonist effect on D-R curve in presence of spare receptor

A

Antagonist destroys spare receptors (curve shifts to right)

Agonist action is reduced (curve shifts down)

49
Q

Hydroxyurea

A

Sickle cell anemia

Increases HbF

50
Q

Sulfonylurea

A

T2DM

Increases insulin release by permanently closing K+ channel in B-cells in pancreas

51
Q

Metformin

A

T2DM

Suppresses gluconeogenesis in liver

52
Q

SGLT2 inhibitors

A

T2DM

Decreases reabsorption/ncreases excretion of glucose in kidneys

53
Q

Pioglitazone

A

T2DM

Reduces insulin resistance/improves peripheral tissue sensitivity to insulin

54
Q

Acarbose/miglitol

A

T2DM

Impairs absorption of glucose in small intestine

55
Q

GLP-1 analogues

A

T2DM
Slow transit of nutrients through stomach (makes you feel full longer, decreases appetite)
Increases insulin
Ends in “tide”

56
Q

DPP-4 inhibitors

A

T2DM
Inhibits enzyme that breaks down GLP-1
Ends in “liptin”

57
Q

Insulin

A

Long-acting- basal insulin, lasts all day

Short-acting- bolus insulin, taken w/ meals

Foundations 1 (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions