Brainscape's Knowledge GenomeTM

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


See full index

Year 2 sem 1 > Dynamics > Flashcards

Dynamics Flashcards

1
Q

What are the 2 methods that a drug can take to induce an effect on the target cell

A

Receptor or non-receptor mechanisms

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

What are the 4 non-receptor based mechanisms

A

Physicochemical, interaction with small ions or molecules, incorporation of drug into macromolecules, enzyme inhibition

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

What are some physicochemical mechanisms

A

Osmotic diuretics
Osmotic cathartics
Neutralisation
Decreasing membrane excitability
Detergent effects

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

What are some drug interactions with other molecules or ions

A

EDTA binds to Pb2+ to increase excretion
Penicillamine binds Cu2+ for excretion
PAL chelates arsenic, gold, bismuth, and mercury

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

What are examples of drugs incorporated into macromolecules and their effects

A

Antimetabolites: 5-bromouracil replaces thymine in DNA synth resulting in chromosomal breakages for anti-cancerous effects
5-flourouracil replaces uracil in RNA synthesis making faulty proteins

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

What are examples of enzyme inhibition

A

COX inhibitors like NSAIDs
Cholinesterase inhibitors like neostigmine
Decarboxylase inhibitors like carbidopa
Bacterial dihydrofolate reductase inhibitor like trimethoprim

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

How could receptor count affect drug activity when using different concentrations

A

At high enough concentrations, all the receptors will be occupied and no increase in drug conc will affect activity

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

What are some characteristics that determine receptor-drug compatibility?

A

Drug size, shape, and charge

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

What are the requirements for drug and receptor binding

A

Both should be close enough
R should be complimentary to D
Binding should be reversible

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

The type of interaction produced by drug and receptor depends on:

A

Chemical structure of d and r
Sites of drug loss like plasma albumin
Intermolecular binding forces

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

What are the attractive forces between drug and receptor

A

Van der waals: weakest but most common
H bonds: reversible and stronger than van der waals
Ionic bond: reversible
Covalent: rarest and is irreversible (strongest)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What are the factors that a receptor based drug response depends on

A

Affinity of drug to receptor
Efficacy of drug

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

T/F: the receptor count is what determines whether a drug concentration is toxic or not

A

True (for drugs that bind to receptors)

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

What are the 4 major receptor families?

A

GPCR
Ligand-gated ion channels
Enzyme linked receptor
Intracellular receptors

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

How are ion channels opened or closed

A

Using ligand binding

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

What happens when Acetylcholine binds to nicotinic receptors?

A

Sodium ion influx into cell (can be used to induce muscle contraction)

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

What are some molecules that use GPCR?

A

Some hormones
Peptides
Neurotransmitters (adrenergic and cholinergic)

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

How do enzyme-linked receptors function?

A

Ligand binds to extracellular domain, resulting in activation or inhibition of a related cytosolic enzyme usually via phosphorylation.

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

How do intracellular receptors work?

A

A lipid soluble ligand diffuses into the cell and interacts with a receptor

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

Give an example for intracellular receptors

A

Steroids form a complex with the intracellular receptor and migrate into the nucleus, binding to dna sequences and regulating their expression

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

What are some common 2ndary messengers?

A

cAMP
cGMP
IP3
DAG
Ca2+

22
Q

What is the shape of a dose-response curve?

A

Logarithmic

23
Q

What is the shape of a graph of response vs log dose?

A

Sigmoid

24
Q

What is ED50

A

The concentration of drug that results in therapeutic effects in 50% of people

25
Q

What is LD50?

A

The dose that results in the death of 50% of users. It is usually approximated

26
Q

What is Vmax in pharmacodynamics?

A

Max response, efficacy, or intrinsic activity.

27
Q

What is the therapeutic index?

A

LD50/ED50 larger is better

28
Q

What is potency?

A

When comparing 2 drugs with the same effects, it is the ratio of dose of drug 1 vs drug 2 to produce the same effect

29
Q

The ability of a drug to form a stable complex with the receptor is called:

A

Affinity

30
Q

What is the margin of safety and what is the minimum required value?

A

LD0.1/ED99.9 the value should be greater than 1

31
Q

What is the protective index?

A

Best measure of safety
ED50 producing side effects/ED50 producing desired effect

32
Q

What is a full agonist?

A

A drug that interacts with a receptor and produces a maximum response (strong agonists produce full effect while occupying less receptors)

33
Q

A drug that has reduced efficacy but maximum potency and high affinity is:

A

Partial agonist

34
Q

What is an agonist-antagonistic agonist?

A

A drug with agonistic and antagonistic activities

35
Q

A drug that produces an effect opposite to the agonist

A

Inverse agonist

36
Q

Why are inverse agonists used?

A

Some receptors produce an effect without a ligand (constitutive activity). Inv agonists block that activity.
Can be used to treat hyperthyroidism and precocious puberty

37
Q

Define:
Addition
Synergism
Potentiation

A

Addition: 2 drugs producing sane response, the net response is the sum of the response of each drug
Synergism: same as addition but the response is greater than the sum of both
Potentiation: one drug giving no effect coupled with a drug with an effect results in an amplified effect of the 2nd drug

38
Q

What are spare receptors?

A

Some full agonists can elicit full response without utilising all receptors, the extra receptors are called spare receptors.

39
Q

What are some effectors that give spare receptors?

A

Insulin, epinephrine, norepinephrine

40
Q

What is up-regulation and down-regulation

A

Up regulation is the increase of receptor number while the opposite happens in down regulation. The less the receptors the more drug you need for max effect

41
Q

What is tachyphylaxis?

A

Abnormal desensitization to a drug quickly

42
Q

What are the types of antagonism?

A

Physiological (ANS)
Neutralisation (forming inactive complex)
Pharmacological

43
Q

What is surmountable antagonism?

A

Competitive inhibition and is reversible

44
Q

What happens to ed50, affinity, and potency of an agonist when taken with a competitive antagonist?

A

ED50 inc
Affinity decreases
Potency is relative
Vmax same
Dose response curves are shifted to the right

45
Q

What are the types of unsurmountable antagonism?

A

Noncompetitve
Uncompetitive
Irreversible

46
Q

What is a competitive irreversible antagonist?

A

The antagonist binds irreversibly

47
Q

What is an uncompetitive inhibitor

A

One that binds to enzyme substrate complex lowering Km and Vmax

48
Q

What is a non-competitive inhibitor?

A

One that binds to enzyme-substrate complex or an allosteric site, lowering Vmax only

49
Q

What happens when irreversible antagonists bind to enzymes?

A

The dose-response curve shifts down

50
Q

What is an antidote?

A

Drug that binds another drug thereby inactivating it

Year 2 sem 1 (17 decks)

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