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Pharma midterm 1 > Lecture 1,2 > Flashcards

Lecture 1,2 Flashcards

1
Q

Define pharmacology

A

investigatiing the function altering effect of several substances in living entiities

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2
Q

What is a pharmaceutical substance?

A

when a substance can be used for treatment

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3
Q

what does drug mean?

A

dry

dried out substance of plants

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4
Q

Define pharmacodynamics

A

Drugs affect on the body

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5
Q

Define pharmacokinetics

A

how the body acts on the drug, the behaviour and the movement

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6
Q

What is the principle of ADME?

A
  • Absorption
    • how it gets into the body
  • Distribution
    • where it goes
    • transporters
  • metabolism
    • how it is broken down
    • liver
  • excretion
    • how it leaves the body
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7
Q

What are some non-specific physical interaction drugs?

Give example for each of them:

A

Osmotic diuretics - mannitol

antacids - magnesium hydroxide

laxatives - magnesium sulfate

chelators - EDTA, deferoxamine

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8
Q

Some drugs have biochemical interaction, these are proteins, what groups do we divide them into?

A

With receptors

and

Without receptors

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9
Q

What are the the task of drugs that are without receptors?

A

Inhibition of enzymes: NSAIDs, ACE inhibitor, AChE inhibitors

DNA damage: anticancer drugs

Transporters: proton-pump inhibtors, diuretics

Ion channels: local anasthetics (lidocain, Na+ channel)

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10
Q

What are the task of drugs that are working with receptors?

A

they act on signaling mechanisms as acceptors - will bind to something

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11
Q

Name the four groups of receptors

A
  1. Ligand-gated ion channels
  2. G protein-coupled receptors
  3. Receptor-activated tyrosine kinases
  4. Intracellular nuclear receptors
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12
Q

How does ligand gated ion channels operate?

A

the ligand will bind to the receptor and there will be an influx. ex Na+ and there will be an effect

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13
Q

give an example of an ligand gated ion channel

A

nikotinic acetylcholine receptor

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14
Q

where can you find nicotinic acetylcholine receptor?

A
  • neuromuscular junction
  • autonomic ganglia
  • CNS
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15
Q

What does it mean that a drug is orthosteric?

A

binds to the natural binding site of the receptor

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16
Q

what does it mean that a drug has an allosteric effect?

A

it will bind next to the binding site, enhance it

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17
Q

is propofol allosteric or orthosteric?

A

both

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18
Q

What is PAM an acronym for?

A

Positive Allosteric Modulator (allosteric agonist)

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19
Q

How many times does a G-coupled receptor cross the membrane, and what is the correct term for corssing the membrane?

A

Crosses 7 times

Transmembrane

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20
Q

What are the three types of G protein-coupled receptors?

A

Gas- coupled receptor: stimulatory

GaI - coupled receptors: inhibitory

Gq - coupled receptors

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21
Q

Give an example for an Gas - coupled receptor

A

-Beta-adrenoceptor

Ligand is adrenaline - Leads to phosphorylation

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22
Q

Where can the Gas-coupled receptors be found?

A
  • Cardiac muscle cells
  • Vascular smooth muscle cells
23
Q

Give some examples of Gai-coupled receptors

A
  • M2 Cholinergic receptors
  • A2 receptors
24
Q

Give some examples of Gq coupled receptors

A

A1- receptor

H1 receptors

Serotonin receptors

25
Q

What happens when serotonin binds to a serotonin receptor?

A

GDP -> GTP

PLC activated

PIP2 -> IP3 + DAG

=

Ca2+ and PKC is activated

26
Q

What happens when insulin binds to the insulin receptor (kinase activity)

A
  • Serotonin binds
  • Tyrosin is phosphorylated
  • AKT is activated (phosphokinase b)
  • multiple cellular effects
27
Q

What happpens when cytokines binds to the cytrokine receptor

A

JAK causes phosphorylation

STAT binds

STAT: activated, goes inside the cell nucleus and stimulate DNA gene transcription

Protein synthesis: inflammation, allergy

28
Q

What does JAK inhibitors primarly inhibit and give an example of a veterinary drug

A

inhibit redominately JAK-1 (kinase)

(JAK1 produce: IL-2, IL-4, IL-6. IL13
(allergy, inflammation) IL-31 (itching))

Drug: Oclacitinib

29
Q

Give some examples of drugs that use intracellular nuclear receptors

A

Ligand - cortisol

HEat shock protein

CoA

RNA polymerase II

30
Q

What is a ligand

A

a substrate that binds to the receptor - drug

31
Q

what bonds are formed between the ligand and the receptor?

and what are their characterisitcs

A

Van der waals, hydrogen and ionic

  • they are usually reversible

they cause altered confirmation leading to an effect

difference in the affinity

32
Q

Is there some lignads that bind irreverisble? what bond?

A

covalent bond

omenprazol - proton pump

long lasting action

needs to be given once a day

33
Q

What does a continous dose-response curve show?

A

the affect of a drug in an animal over time

if dose is increased the curve must be watched to see effect

34
Q

What is EC50?

A

half maximum effective conencentration

35
Q

What is meant by efficacy

A

the strength of the effect

36
Q

what is meant by potency?

A

how fast a drug reacts in the animal

37
Q
  1. Which drug is the most potent?
  2. Which drug has least efficacy?
A
  1. fentanyl is most potent (100x more than morphine)
  2. butorphenol
38
Q

What does a quantal dose-response curve give information about?

A

Drug in a population

  • about 100 dogs
39
Q

Which parameters does a quantal dose-response curve give us?

A

Effective dose

toxic dose

lethal dose

40
Q

When reading a graph giving therapeutic definitions what elese but efficancy and potency is important to look for?

A

the slope of the graph is also important

41
Q

What is the therapeutic index and what does it mean?

A

LD50/ED50

It is a comparison of the amount of a therapeutic agent that causes the therapeutic effect to the amount that causes toxicity.

larger therapeutic index means the drug is safer

42
Q

Range these drugs in their order of beeing safest

ethanol

digoxin

morphine

remifentanyl

atropine

A

from safest to unsafest

remifentanyl

morphine

ethanol

digoxin

atropine

43
Q

What is the therapeutic window?

A

where the drug acts and is safe

between minimum toxic concentration and minimum effective concentration

44
Q

What is an full agonist?

A

a drug that has high affinity to receptor

high efficancy

induces maximum response

binds to the receptor and will activate it

45
Q

what is an full antagonist?

A

Drug that will bind to an receptor and keep the respons from happening

no efficacy

receptor will not be activated

46
Q

what is a partial agonist?

A

drug that will induce a sub-maximal response

it has hig affinity

it has low efficacy

will bind to and partially activate the receptor

47
Q

give example of a full agonist, full antagonist and partial agonist

A

Full agonist - fentanyl, morphine

Full antagonist - naloxone

Partial agonist - buprenorphine

48
Q

What is an inverse agonist

A

a drug that causes the reverse action, such as antihistamine

49
Q

What type of drug is A, B and C (agonist)

A

A) full agonist

B) partial agonist

C) partial agonist

50
Q

Fill in the graph

A
51
Q

What happens to the maximum efficcacy in presence of a competitive antagonist?

A

unchanged

52
Q

what happens to the agonist potency in prescens of a competitive antagonist`?

A

decreases

53
Q

What is meant by pharmacodynamic tolerance?

A
  • Desensitization
  • Agonist that continously binds to the receptor will cause inactivation, sequestration or down-regulation
54
Q

what is pharmacokinetic tolerance?

A

induction of CYP450 enzymes

PL.phenobarbital, ethanol

often a consequence of the drug being an inducer or inhibitor of a specific metabolic enzyme or transporter system, resulting in a time-dependent decrease in presentation of the active moiety to the receptor biophase

Pharma midterm 1 (14 decks)

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