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z F1: Pharmacology > Exam 1 > Flashcards

Exam 1 Flashcards

1
Q

What is drug discovery

A

Early sources of drugs
-Natural products derived from plants

Based on observation of medicinal properties (discover)

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2
Q

What is drug invention

A

Modern approach is a process (inventive)
Chemical synthesis, experimentation and optimization

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3
Q

What is rational drug design

A

Starting from a known molecule and optimizing it through synthsis to improve its potency, selectivity, stability

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4
Q

What is screening

A

Random process
-identify a target
-develop a screen that identify active compound
-test large library of compounds to get a hit
-modify hits to get a lead molecule

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5
Q

What are screening library approach refined through

A

Combinatorial chemistry
Increased chemical diversity of compound libraries
High-throughput screening (well plate test)
Virtual screening (big chemical databases)

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6
Q

Small vs large molecules

A

In the past many were small, but now recombinant DNA technology permitted development of large molecules

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7
Q

Targets of drug action critical questions to ask

A

-can one find a drug that will have the desired effect against its target
-does modulation of the target protein affect the course of disease
-does this project make sense economically

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8
Q

What are druggable targets

A

Does it have known binding sites
-Do other small ligands interact with target
-What type of molecules interact (smaller are ideal)

Are binding sites extracellular or intracellular
-Extracellular are better because they don’t have to go through membranes

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9
Q

Valid drug target

A

Is the target critical for disease process (or normal function)
-What happens if the target is disrupted
-Redundancy of biological systems
-Adaption to presence of drugs

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10
Q

Economically viable targets

A

Biotech start-ups and university spin-offs
-Funded by small investors or grants
Big Pharma (large companies)
-Well funded, lots of resources
Private foundations and non-profits
-Special interests
Federal Agencies (NIH, FDA)
-Help support university and small business efforts
-Support rare diseases (ophans)

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11
Q

Preclinical Research

A

Medicinal Chemistry
-synthesis of novel compounds
Pharmacology
-Measure affinity, selectivity, activity
-Pharmacokinetic properties (ADME)
Pharmaceutics
-Pharmaceutical properties (stability, solubility, formulation)
Toxicology
-safety

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12
Q

Preclinical safety data required

A

Acute toxicity studies
-several doses
-at least two species (one non-rodent)
Chronic tox studies
-period related to extent of proposed human use
-two species (one non-rodent)
Genotoxicity, cardiotoxicity, respiratory safety, other systems
-In vitro
-In vito

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13
Q

What is in the investigational new drug application (IND)

A

Chemistry, manufacturing (API)
Pharmacological, pharmokinetics, tox data
Human study rational
Protocol plan

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14
Q

How long does the FDA have to approve the IND application

A

30 days
If no contact before then trails can start

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15
Q

Role of US food and drug administration

A

Responsible for protecting public health by assuring safety, efficiency, and security of drugs

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16
Q

What were some setbacks of the pure food and drug act

A

No restrictions on what was in the medications
Needed to implement tox testing
Resulted in NDA (new drug application)

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17
Q

Food drug and cosmetic act
Kefauver-Harris amendments

A

Ads that have side effects listed

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18
Q

What is an IRB (institutional review board)

A

It is a board at a university to approve trials
they review protocols, address privacy concerns, requires informed consent to participate in clinical trials

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19
Q

What do phase 1 and 2 do in clinical trials

A

Phase I: 10-100 healthy volunteers, emphasis on safety
Phase 2: 50 -500 people with disease, focus on efficacy

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20
Q

What are phase 3 and 4 in clinical trials

A

Phase 3: 200 - 2,000 patients, full drug approval
Phase 4: 10,000+ patients

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21
Q

What are the seven ethical principles for conducting clinical trails

A

social and clinical value
scientific validity
fair selection of subjects
informed consent
favorable risk-benefit ratio
independent review
respect for potential and enrolled subjects

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22
Q

What is the importance of hypothesis testing for clinical trials

A

identify primary endpoint for assessing outcomes
surrogate endpoints
biomarkers

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23
Q

What is the importance of sample size for clinical trials

A

small size for initial studies of safety
large size for studies of efficacy

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24
Q

What is the belmont report outlines ethical framework for studies with human subjects

A

respect for persons
beneficence
justice

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25
Q

What are biomarkers

A

a characteristic that is measured as an indication of a physiological process or pathological state

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26
Q

What is type for biomarkers

A

target
mechanism
outcome

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27
Q

What is linkage to efficacy or outcome for biomarkers

A

low - no consistent linage
medium - some information
high - reproducibility demonstrated

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28
Q

Why is it important for biomarkers to have predefined criteria and qualification of biomarkers

A

predefined criteria: similar to considerations about primary clinical endpoints
qualification of biomarkers: assay or measure reliably established and reflects outcome or safety

29
Q

What does ADME stand for in pharmacokinetics

A

Absorption
Distribution
Metabolism
Elimination

30
Q

What properties determine the nature of drug action of pharmacodynamics

A

Binding and activity at therapeutic target
Toxicity (bind and activity at other targets)

31
Q

What is pharmacokinetics

A

the study of biochemcial and physiological effects of drugs and their mechanism of action

32
Q

What are drug targets

A

Cell surface
Intracellular
Nucleus
DNA
Protein

33
Q

What are chemical messengers

A

Cell to cell communication
-Hormones (distal)
-Neurotransmitters (local)
Modulate activity at receptor represents important target for therapeutic intervention

34
Q

How are receptors named

A

For endogenous compound

35
Q

Cholinergic receptors are activated by acetylcholine

A

Muscarinic - GPCR
Nicotinic - ligand gated

36
Q

Called ________ receptors when endogenous compound is unknown

A

orphan

37
Q

Agonists

A

Activates receptors
-produces physiological responses (full vs partial)
-Endogenous compounds are agonists (acetylcholine)
-Synthetic compounds or natural products may be agonists

38
Q

Antagonists

A

Inhibit physiological responses produced by agonists
-shift agonist dose response to right in parallel manner

39
Q

Inverse agonists

A

Produce opposite effect of agonist
-may inhibit agonist response

40
Q

Allosteric Ligand

A

modify agonist activity
bind to site outside agonist binding site (orthosteric site)

41
Q

Orthosteric site vs Allosteric site

A

Orthosteric: site for endogenous ligand, competitive inhibitor, highly conserved amino acid residue

Allosteric: modulate binding to orthosteric site, may activate or inhibit receptors, less highly conserved

42
Q

Drug affinity and intrinstic activity related to chemical structure

A

-small changes in structure may lead to large changes in pharmacological properties
-stereoselectivity
-pharmacophore (functional groups, chem properties)

43
Q

How has drugs interaction with receptors been enhanced by several recent developments

A

-Molecular modeling of drug molecules combined with structure activity relationship studies
-Site-directed mutagenesis
-Structural data for receptors

44
Q

G protein coupled receptors

A

-Mediate slow onset, long duration responses
-Target for many best-selling drugs

45
Q

What does Gi, Gs, Gq, G(olf), Gt do

A

Gi: inhibits adenylyl cyclase
Gs: stimulates adenylyl cyclase
Gq: stimulates phospholopase C
G(olf): olfactory G protein mediates olfactory sensation
Gt: transducen mediates sensitivity to light

46
Q

What do odd and even muscarinic receptors do

A

odd: activate Gq (promote phosphoinositide metabolism)
even: activate Gi/o (inhibit adenylyl cylase, decrease cAMP)

47
Q

What do ligand-gated channels do

A

regulate ion flow in response to extracellular signals
can be excitatory or inhibitory depending on ion flow

48
Q

What do nicotinic receptors do

A

mediate fast-onset, short duration responses to acetylcholine

49
Q

What are GABA receptors

A

predominant inhibitory receptor in the CNS

50
Q

How long are patents good for

A

20 years about date filed
(5 years on market)

51
Q

Generic vs brand name

A

generic: assigned by USAN council
brand: assigned by manufacturer

52
Q

Tyrosine kinases and growth hormones activate ________ signals that alter cellular function

A

intracellular

53
Q

Nuclear receptors regulate gene ________ and __________ of proteins

A

transcription and translation

54
Q

What is quantification

A

interaction between drugs and receptors
*important for understanding relationship between dose and response of drug

55
Q

What are dose-response curves

A

Permit a measure of receptor binding or activity as a function of drug concentration

56
Q

What is KD and EC50

A

KD: affinity
EC50: potency

57
Q

What is B(max) and S(max)

A

B(max): binding
S(max): activity

58
Q

What is the difference between linear and log plots

A

linear is closer together and can not see the curve while log you can

59
Q

Stats for mean values are converted to what

A

convert to log units then calculate mean then convert back

60
Q

When KD is low it indicates ______ affinity

A

high affinity
(low concentrations are needed to occupy half the receptors)

61
Q

What are competitive antagonists

A

Indicated when agonist and antagonist compete for same binding site on receptor
-shift to right

62
Q

What are irreversible antagonists

A

Antagonist dissociates slowly from receptor
*agonist can not overcome presence of antagonist
-shift to right

63
Q

Increasing concentrations of ______ cannot fully overcome the effects of allosteric inhibitors

A

agonsists

63
Q

Endogenous ligands bind to what sites

A

orthosteric sites

64
Q

Orthosteric binding sites are more highly conserved than _________ sites

A

allosteric

65
Q

Allosteric ligands can enhance or inhibit activity of ________

A

agonists

66
Q

Allosteric ligands can directly activate or inhibit ________

A

receptors

67
Q

Positive allosteric modulators (PAMs) can enhance agonist potency (PAM __) or agonist efficacy (PAM __)

A

potency: X
efficacy: Y

z F1: Pharmacology (4 decks)

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