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Physiology and Pharmacology > Lecture 3 > Flashcards

Lecture 3 Flashcards

1
Q

What is the difference between pharmacology and pharmacy?

A

Pharmacology: Study of mechanics by which drugs (biologically active compounds) affect the function of living systems.
Pharmacy: Study of formulation, dispensing and dosing

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2
Q

What are receptors?

A

Proteins which recognize and bind ‘chemical mediators/ messengers’

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3
Q

What are examples of chemical mediators?

A

hormones, neurotransmitters, antibodies

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4
Q

What is the main function of receptors?

A

regulation of cellular processes

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5
Q

What are the two types of cellular processes?

A
  1. hormone recognition and binding

2. intracellular signal generation

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6
Q

What are current proteins targeted by small molecule drugs?

A
  1. ST/Y kinases 22%
  2. GPCRs 15%
  3. Cation channels 5%
  4. Ser proteases (trypsin) 4%
  5. Protein phosphatases 4%
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7
Q

How much of drugs interfere with the function of receptors involved in chemical communication?

A

40%

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8
Q

What are subclasses of receptors classified by structure?

A
  1. carriers/transporters
  2. enzymes
  3. ion channels
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9
Q

How many types of receptors are there?

A

1000

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10
Q

What is an example of receptors that bind to different ligands?

A

Muscarinic ACh receptors

Ligands: ACh and nicotine

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11
Q

What is an example of an accessory protein that binds to enzymes?

A

ATP

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12
Q

What are drugs that bind to a receptor producing a response by mimicking the effect of chemical mediators?

A

Agonists

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13
Q

What are examples of agonists?

A

Morphine, pilocarpine

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14
Q

What is a poppy derived drug that interacts with pain-sensory neurons which mimics endorphins.

A

Morphine

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15
Q

What is a side-effect of morphine?

A

Addiction from constant stimulus

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16
Q

What does pilocarpine bind to?

A

Muscarinic ACh receptors in ANS

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17
Q

What is an antagonist?

A

Drugs that prevent the response of an agonist

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18
Q

What is an example of an antagonist?

A

atropine

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19
Q

What is atropine an antagonist to?

A

pilocarpine

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20
Q

What are examples of drugs which target ion channels?

A

Lignocaine, apamin, nifedipine ariloride

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21
Q

Where is lignocaine found in?

A

Strepsils

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22
Q

What is lignocaine?

A

Local anesthetic

23
Q

How does lignocaine work?

A

Binds to voltage gated sodium channels to stop their activity and prevent pain information inflammation, then pain nerve ending activation doesn’t reach CNS.

24
Q

Where is apamin found?

A

bees

25
Q

How does apamin work?

A

Blocks activity of voltage gated potassium channels so that pain nerve endings fire more AP

26
Q

What type of substance is nifidepine?

A

dihydropyridines

27
Q

What does nifidepine do?

A

Counteracts hypertension

28
Q

How does nifidepine work?

A

Blocks voltage gated calcium channels in smooth muscle lining arteries which reduces resistance to bring down hypertension

29
Q

Where does ariloride (an ENAC) work?

A

Kidneys

30
Q

What are examples of drugs which target enzymes?

A

acetylsalicylic acid, pargyline (and clorgyline), captopril

31
Q

Where is acetylsalicylic acid found?

A

aspirin

32
Q

Which enzymes does acetylsalicylic acid target to?

A

COX and MAO

33
Q

What does COX do?

A

Reduces pain associated with inflammation

34
Q

What does MAO do?

A

Breaks down noradrenaline, adrenaline

35
Q

What does Pargyline do?

A

Inhibits MAO against hypertension as a treatment against depression

36
Q

Where does pargyline affect?

A

CNS - unwanted side effects in CNS and PNS cannot be

37
Q

What is captopril?

A

ACE inhibitors

38
Q

What is captopril used for?

A

Treatment for hypertension

39
Q

How does captopril work?

A

Increases angiotensin by acting on an enzyme

40
Q

What are types of drugs that target transporters?

A
  1. some need ATP and some need solutes
  2. prevents action potential
  3. may be hijacked and transport is utilized to get into cells
41
Q

What are examples of drugs that target transporters?

A

fluoxetine (prozac), Digoxin

42
Q

What is fluoxetine (prozac)?

A

It is a widely prescribed antidepressant more specific to the CNS

43
Q

What transmitters does fluoxetine target?

A

5-HT, serotonin

44
Q

How does fluoxetine work?

A

It blocks transport of serotonin so that it builds up outside of neurons to ctivate receptors for happiness

45
Q

Where is digoxin found?

A

In foxgloves

46
Q

What transporter does digoxin target?

A

Na/K transporter (exchanger)

47
Q

How does digoxin work?

A
  1. Na in heart muscle builds up
  2. Ca builds up in heart
  3. Strength of contractility increases
  4. Prolongs action potential
48
Q

What is a receptor superfamily?

A

Receptors which have similar structural features

49
Q

How many receptor superfamilies are there?

A

4:
Ligand-gated ion channels (ionotropic receptors)
G-protein-coupled receptors (metabotropic receptors)
Kinase-linked receptors
Nuclear receptors

50
Q

Which receptor superfamilies are found on the cell surface?

A

All except nuclear receptors

51
Q

How many hydrophobic amino acid segments are there in transmembrane spanning receptor proteins?

A

20-25

52
Q

Many drugs act via the _ domain.

A

ligand binding

53
Q

Nuclear receptors are DNA-linked. What does this mean?

A

They regulate gene transcription and the ligand must be able to cross the plasma membrane

Physiology and Pharmacology (27 decks)

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