1. Definition of drug. Pharmacodynamics: Structure-dependent and independent drug actions Flashcards

1
Q

Give the definition of ‘pharmacology’

A

Investigating the function-altering effect of several (exogenic and endogenic) substances in living entities.

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2
Q

Define pharmaceutical substances

A

If a substance can be used for treatment

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3
Q

Give the etymology of “Drug”

A

Drug” (“droog” → “dry”)

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4
Q

What are pharmacodynamics?

A

The process of the drug entering the body

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5
Q

What are pharmacokinetics?

A

The interaction of the body on the drug

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6
Q

Which mnemonic is used to represent the pathway of the drug (pharmacodynamics)

A

ADME

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7
Q

“Corpora non agunt nisi fixata”

A

“A drug will not work unless it is bound”

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8
Q

Most drugs achieve their therapeutic effects by…

A

Interacting selectively with target molecules

  • These play roles in physiologic or pathologic functioning
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9
Q

The selectivity of the drug binding may determine…

A

Adverse effects of a drug

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10
Q

Drug receptors are…

A

Macromolecules that, upon binding to a drug, mediate those biochemical and physiologic changes

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11
Q

Drugs binding to intracellular receptors

A

Highly lipophilic drugs that can easily pass through plasma membrane & also special barriers

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12
Q

Extracellular receptors

A

Surface protein receptors with extracellular domains linked to intracellular effector molecules

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13
Q

Which receptor types do drugs interact with?

A
  1. Ligand-gated ion channels
  2. G-protein coupled receptors
  3. Receptor-activated tyrosine kinases
  4. Intracellular nuclear receptors
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14
Q

Ligand-gated ion channels

A

Nicotinic ACh (nACh) receptors composed of 5 subunits

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15
Q

Give the area of the physiological function of nACh channels

A
  • Neuromuscular junction
  • Autonomic ganglia
  • CNS
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16
Q

Give the function of the nACh receptor

A
  1. ACh binds to both α-subunits
  2. Channels open
  3. Na+ passes down its conc. gradient into cell
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17
Q

Give the types of nACh receptors (ligand-gated ion channels) involved in pharmacology

A
  • Nm
  • N<span>G</span>
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18
Q

Nm receptor - Area of function

A

Motor endplate of neuromuscular junctions of somatic nerves & skeletal muscles

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19
Q

N<span>G</span> Receptor - Area of function

A

Autonomic ganglia in adrenal medulla & certail areas in the brain

20
Q

GABAA receptor-gated chloride ion channel

A
  • Orthosteric ⇔ Allosteric effect (propofol acts as both)
  • PAM = Positive allosteric modulator = Allosteric agonist
21
Q

G-protein coupled receptors

A

7-transmembrane receptors

22
Q

Give the types of G-protein coupled receptors

A
  • Gαs (Stimulatory)
  • I (Inhibitory)
  • Gq
23
Q

s receptors - Action of function

A
  1. GTP → GDP
  2. Interaction with adenylate cyclase
  3. Catalyses: ATP → cAMP
  4. cAMP activated PKA
  5. Phosphorylation & activation of effector proteins
  6. Drug effect is carried out
24
Q

List some Gαs receptors

A
  • H2
  • β1 Adrenoceptors
  • β2 Adrenoceptors
25
Q

H2 (Histamine) receptor function

A
  • ↑ gastric production
  • Vasodilation
  • Relaxes SM
26
Q

β1 adrenoceptors

A

(Excitatory)

  • ↑ Heart rate & contractility
  • ↑ Fat cell lipolysis
27
Q

β2 adrenoceptors

A

(Inhibitory)

  • Vasodilation
  • Intestinal SM relaxation
  • Bronchial SM relaxation
  • Uterine SM relaxation
28
Q

i receptors

A
  1. GDP→GTP
  2. Inhibition of Adenylate Cyclase
  3. ↓cAMP production
29
Q

Give an example of a Gαi receptor

A

α2 adrenoreceptors

30
Q

α2 ​adrenoreceptors - Function

A

Prejunctional inhibition of norepinephrine & other neurotransmitter release

31
Q

Gq receptors - Function

A
  1. ↑ Phospholipase activity
  2. Cleaves: Membrane phospholipid → DAG + IP
  3. DAG activated Protein Kinase C
  4. Phosphorylation & activation of cellular proteins
  5. IP releases Ca2+ from ER → cytoplasm
  6. Cellular processes activated
32
Q

List some Gq coupled receptors

A
  • α1 adrenoreceptors
  • H1 receptors
  • Serotonin receptors
33
Q

H1 receptor - function

A
  • ↑ Awakeness
  • ↑ Vasodilation
  • ↑ Permiability
34
Q

α1 adrenoreceptors - Function

A
  • Vasoconstriction
  • GI relaxation
  • Mydriasis
35
Q

Receptor-activated tyrosine kinases

A
  • Many growth-related signals
  • Liganded receptors autophosphorylate tyrosine
36
Q

Give an example of a receptor-activated tyrosine kinases

A

Insulin receptor substrate (IRS) → Insulin receptor

37
Q

JAK inhibitors - function

A

“Janus kinase inhibitors”

  • Inhibits JAK-1
    • Interleukins-4 /-13 /-31 (Allergy, inflammation, pruritus)
  • Used in atopic dermatitis
38
Q

Intracellular nuclear receptors (NR) - Function

A
  • Lipophylic ligands
  1. Binding ligand → structural changes in receptor
  2. Dissociation of chaperones → Receptor enters the nucleus
  3. Hetero-/homodimerisation of receptors & interaction with DNA
39
Q

Give examples of intracellular nuclear receptors

A
  • Ligand (pl. cortisol)
  • HSP90 (Heat shock protein)
  • CoA (Coactivator)
  • Pol II (RNA polymerase II)
40
Q

Identify receptor 1

A

Ligand-gated ion channel

41
Q

Identify receptor 2

A
42
Q

Identify receptor 3

A

Receptor-activated tyrosine kinases

43
Q

Identify receptor 4

A

Intracellular nuclear receptors

44
Q
A

Activation of conductance

45
Q
A
  1. G-protein activation
  2. Generation of second messenger
  3. Activation of cell signaling
46
Q
A
  1. Phosphorylation of tyrosines on key signalling molecules
  2. Activation of cell signalling
47
Q
A
  1. Transport to the nucleus
  2. Activation of transcription and translation