Lecture 1,2

Question 1

Define pharmacology

Answer 1

investigatiing the function altering effect of several substances in living entiities

Question 2

What is a pharmaceutical substance?

Answer 2

when a substance can be used for treatment

Question 3

what does drug mean?

Answer 3

dry

dried out substance of plants

Question 4

Define pharmacodynamics

Answer 4

Drugs affect on the body

Question 5

Define pharmacokinetics

Answer 5

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

Question 6

What is the principle of ADME?

Answer 6

• 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

Question 7

What are some non-specific physical interaction drugs?

Give example for each of them:

Answer 7

Osmotic diuretics - mannitol

antacids - magnesium hydroxide

laxatives - magnesium sulfate

chelators - EDTA, deferoxamine

Question 8

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

Answer 8

With receptors

and

Without receptors

Question 9

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

Answer 9

Inhibition of enzymes: NSAIDs, ACE inhibitor, AChE inhibitors

DNA damage: anticancer drugs

Transporters: proton-pump inhibtors, diuretics

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

Question 10

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

Answer 10

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

Question 11

Name the four groups of receptors

Answer 11

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

Question 12

How does ligand gated ion channels operate?

Answer 12

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

Question 13

give an example of an ligand gated ion channel

Answer 13

nikotinic acetylcholine receptor

Question 14

where can you find nicotinic acetylcholine receptor?

Answer 14

• neuromuscular junction
• autonomic ganglia
• CNS

Question 15

What does it mean that a drug is orthosteric?

Answer 15

binds to the natural binding site of the receptor

Question 16

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

Answer 16

it will bind next to the binding site, enhance it

Question 17

is propofol allosteric or orthosteric?

Answer 17

both

Question 18

What is PAM an acronym for?

Answer 18

Positive Allosteric Modulator (allosteric agonist)

Question 19

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

Answer 19

Crosses 7 times

Transmembrane

Question 20

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

Answer 20

Ga_s- coupled receptor: stimulatory

Ga_I - coupled receptors: inhibitory

G_q - coupled receptors

Question 21

Give an example for an Ga_s - coupled receptor

Answer 21

-Beta-adrenoceptor

Ligand is adrenaline - Leads to phosphorylation

Question 22

Where can the Ga_s-coupled receptors be found?

Answer 22

• Cardiac muscle cells
• Vascular smooth muscle cells

Question 23

Give some examples of Ga_i-coupled receptors

Answer 23

• M2 Cholinergic receptors
• A₂ receptors

Question 24

Give some examples of G_q coupled receptors

Answer 24

A1- receptor

H1 receptors

Serotonin receptors

Question 25

What happens when serotonin binds to a serotonin receptor?

Answer 25

GDP -\> GTP PLC activated PIP2 -\> IP3 + DAG = Ca2+ and PKC is activated

Question 26

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

Answer 26

- Serotonin binds - Tyrosin is phosphorylated - AKT is activated (phosphokinase b) - multiple cellular effects

Question 27

What happpens when cytokines binds to the cytrokine receptor

Answer 27

JAK causes phosphorylation STAT binds STAT: activated, goes inside the cell nucleus and stimulate DNA gene transcription Protein synthesis: inflammation, allergy

Question 28

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

Answer 28

inhibit redominately JAK-1 (kinase) (JAK1 produce: IL-2, IL-4, IL-6. IL13 (allergy, inflammation) IL-31 (itching)) Drug: Oclacitinib

Question 29

Give some examples of drugs that use intracellular nuclear receptors

Answer 29

Ligand - cortisol HEat shock protein CoA RNA polymerase II

Question 30

What is a ligand

Answer 30

a substrate that binds to the receptor - drug

Question 31

what bonds are formed between the ligand and the receptor? and what are their characterisitcs

Answer 31

Van der waals, hydrogen and ionic - they are usually reversible they cause altered confirmation leading to an effect difference in the affinity

Question 32

Is there some lignads that bind irreverisble? what bond?

Answer 32

covalent bond omenprazol - proton pump long lasting action needs to be given once a day

Question 33

What does a continous dose-response curve show?

Answer 33

the affect of a drug in an animal over time if dose is increased the curve must be watched to see effect

Question 34

What is EC50?

Answer 34

half maximum effective conencentration

Question 35

What is meant by efficacy

Answer 35

the strength of the effect

Question 36

what is meant by potency?

Answer 36

how fast a drug reacts in the animal

Question 37

1. Which drug is the most potent? 2. Which drug has least efficacy?

Answer 37

1. fentanyl is most potent (100x more than morphine) 2. butorphenol

Question 38

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

Answer 38

Drug in a population - about 100 dogs

Question 39

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

Answer 39

Effective dose toxic dose lethal dose

Question 40

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

Answer 40

the slope of the graph is also important

Question 41

What is the therapeutic index and what does it mean?

Answer 41

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

Question 42

Range these drugs in their order of beeing safest ethanol digoxin morphine remifentanyl atropine

Answer 42

from safest to unsafest remifentanyl morphine ethanol digoxin atropine

Question 43

What is the therapeutic window?

Answer 43

where the drug acts and is safe between minimum toxic concentration and minimum effective concentration

Question 44

What is an full agonist?

Answer 44

a drug that has high affinity to receptor high efficancy induces maximum response binds to the receptor and will activate it

Question 45

what is an full antagonist?

Answer 45

Drug that will bind to an receptor and keep the respons from happening no efficacy receptor will not be activated

Question 46

what is a partial agonist?

Answer 46

drug that will induce a sub-maximal response it has hig affinity it has low efficacy will bind to and partially activate the receptor

Question 47

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

Answer 47

Full agonist - fentanyl, morphine Full antagonist - naloxone Partial agonist - buprenorphine

Question 48

What is an inverse agonist

Answer 48

a drug that causes the reverse action, such as antihistamine

Question 49

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

Answer 49

A) full agonist B) partial agonist C) partial agonist

Question 50

Fill in the graph

Answer 50

Question 51

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

Answer 51

unchanged

Question 52

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

Answer 52

decreases

Question 53

What is meant by pharmacodynamic tolerance?

Answer 53

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

Question 54

what is pharmacokinetic tolerance?

Answer 54

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