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Basic Pharmacology > BP 2 - Drug receptor interactions > Flashcards

BP 2 - Drug receptor interactions Flashcards

1
Q

What are the common drug targets?

A

Receptors
Enzymes
Ion channels
Carrier molecules

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2
Q

What are the targets of drug action and medical use of benzodiazepenine?

A

GABA receptor

Anti-anxiety

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3
Q

What are the targets of drug action and medical use of penicillin?

A

Transpeptidase

Antibiotics

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4
Q

What are the targets of drug action and medical use of probenecid?

A

Organic ion transporter

Pronlong penicillin action

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5
Q

What is an agonist and antagonist receptors?

A
  1. Activate receptor

2. Block action against agonist

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6
Q

What is the function of enzymes at a drug target?

A

Inhibit/act as false substrate

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7
Q

What is the function of carriers at a drug target?

A

Block/ modulate opening/closing

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8
Q

What is the function of ion channels at a drug target?

A

Transported in place of endogenous substrate/ inhibit transport

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9
Q

What type of drug is benzodiazepine?

A

Anti-anxiety

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10
Q

How does benzodiazepine work on GABAA receptor?

A

Increase of charge when is goes through the channel, however BZ just working on the channel does nothing, but used with GABA it enhances its effect

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11
Q

What does NSAIDs stand for?

A

Non-steroidal anti-inflammatory drugs

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12
Q

Give 2 examples of NSAID.

A

Ibuprofen and aspirin

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13
Q

What is the effect of NSAID as a drug?

A

Inhibits cyclooxygenase, therefore arachidonic acid doesn’t convert into prostaglandins, in turn no inflammation, pain or fever

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14
Q

How does histamine act as an agonist?

A

Attaches to H1 receptor in smooth muscle and increasing local blood flow

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15
Q

How does terfenadine act as an antagonist?

A

Attaches to H1 receptor in smooth muscle to decrease local blood flow

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16
Q

What are receptor subtypes and how do they differ?

A

Similar structures but significant differences in their pharmacological responses

Subtypes show many diff cellular effects due to diff specificities what activates/ inhibits them and diff signal transduction mechanisms

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17
Q

Name 4 receptor types that respond to drugs?

A

Ligand gated ion channels
G-protein coupled receptors
Enzyme linked receptors
Intracellular receptors

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18
Q

What else are channel linked receptors called?

A

Ionotropic

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19
Q

What else are channel G-protein receptors called?

A

Metabotrophic

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20
Q

What types of ionotropic receptors are there?

A

Ligand gated
Voltage gated
ACh binding site

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21
Q

How do ligand gated receptors work?

A

Channel linked and need an agonist to open

E.g. nicotinic ACh receptor
ACh causes skeletal muscle to contract by opening channels

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22
Q

How do voltage gated receptors work?

A

Need change in electrical charge across the membrane to open/close

E.g. Na+ channels in N cell membranes
LA block these channels

23
Q

What molecules make up the ACh binding site?

A

2 alpha, beta, gamma and delta

24
Q

Nicotinic ACh receptor antagonists are used for what?

A

Muscle relaxants

25
Q

What are the G-coupled receptors of epinephrine and salbutamol?

A
  1. α/β adrenoceptors

2. ß2 adrenoceptors

26
Q

What are the 3 subunits of a G-coupled receptor? and which molecule produces its specificity?

A
  1. α, β, ɣ

2. α

27
Q

G protein stimulatory action?

A

Activates adenylyl cyclase and Ca2+ channels

28
Q

G protein inhibitory action?

A

Inhibits adenylyl cyclase and K+ channels

29
Q

G protein q action?

A

Activates phospholipase C

30
Q

List the Gs protein signal transduction mechanism

A
  • Hormone or NT binds to receptor
  • Occupied receptor changes shape and interacts with Gs protein
  • G protein releases GDP and binds GTP
  • Alpha subunit of protein dissociates and activates adenylyl cyclase
  • Adenylyl cyclase catalyses formation of cAMP
  • When no hormone/ drug the receptor reverts to its resting state
31
Q

Once α1 activated by Gq what function occurs?

A

Activates PLC

Vasoconstriction

32
Q

Once α2 activated by Gi what function occurs?

A

Inhibits adenylyl cyclase

Auto-inhibition of NT release

33
Q

Once ß1 activated by Gs what function occurs?

A

Stimulates adenylyl cyclase

Accelerated heart rate

34
Q

Once ß2 activated by Gs what function occurs?

A

Stimulates adenylyl cyclase

Bronchodilation

35
Q

What stimulates all subunit receptors?

A

NA and adrenaline

36
Q

What is a ß1 receptor antagonist?

A

Atenolol

37
Q

What is a ß2 receptor agonist?

A

Salbutamol

38
Q

What is a kinase linked receptor?

A
  • Large extracellular ligand binding domain connected to intracellular domain by single memb spanning helix
39
Q

What forms of kinase linked receptors are there?

A

o Receptor tyrosine kinase – i.e. Insulin
o Serine/threonine kinase
o Cytokine
o Guanylyl cyclase-linked

40
Q

How does a kinase linked receptor work?

A
  1. Ligand binding
  2. Dimerization
  3. Autophosphorylation
41
Q

Nuclear receptor examples.

A

o Estrogen receptor – estradiol

o Estrogen receptor – tamoxifen

42
Q

Describe the classes of nuclear receptors.

A

Class I - in cytoplasm, form homodimers, ligands are endocrine (steroids, hormones)
Class II - present in nucleus, form heterodimers, ligands are lipids (FA)

43
Q

What is a ß1 receptor antagonist?

A

Atenolol

44
Q

What is a ß2 receptor agonist?

A

Salbutamol

45
Q

What is a kinase linked receptor?

A
  • Large extracellular ligand binding domain connected to intracellular domain by single memb spanning helix
46
Q

What forms of kinase linked receptors are there?

A

o Receptor tyrosine kinase – i.e. Insulin
o Serine/threonine kinase
o Cytokine
o Guanylyl cyclase-linked

47
Q

How does a kinase linked receptor work?

A
  1. Ligand binding
  2. Dimerization
  3. Autophosphorylation
48
Q

Nuclear receptor examples.

A

o Estrogen receptor – estradiol

o Estrogen receptor – tamoxifen

49
Q

Describe the classes of nuclear receptors.

A

Class I - in cytoplasm, form homodimers, ligands are endocrine (steroids, hormones)
Class II - present in nucleus, form heterodimers, ligands are lipids (FA)

50
Q

What occurs when nuclear receptors bind to hormone response elements?

A

Starts gene transcription changes (+ve/-ve)

51
Q

List the mechanism of Class I nuclear receptor signal transduction.

A
  • Lipid-soluble drug diffuses across the cell memb
  • Drug binds to receptor – changing shape and now activated, moving to nucleus
  • Drug-receptor complex binds to chromatin, activating transcription of genes
  • mRNA is translated into proteins that result in a specific biologic response
52
Q

What is the function of some molecules having multiple receptors binding sites for drugs?

A

Binding at one site will alter binding at another site (positive or negative)

53
Q

What are 3 drug-receptor interactions?

A

Allosteric sites
Orthosteric sites
Effector regions

54
Q

What is are orthosteric and allosteric sites?

A

Orthosteric, which bind at the active site; and allosteric, which bind elsewhere on the protein surface, and allosterically change the conformation of the protein binding site.

Basic Pharmacology (7 decks)

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