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Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q
  1. Membrane potential change opens the channel
  2. Inactivation occurs after
  3. Channel returns to closed state
A
  • voltage-gated ion channels
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2
Q
  1. Binding to receptor
  2. Transient increase in permeability to a particular ion
  3. Negative membrane potential
    - influx of Na+
    - depolarization of cell
    - possible AP
A
  • ligand gated ion channel
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3
Q

Nicotinic ACh, GABA type A and glutamate

A
  • ligand gated ion channel examples
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4
Q
  1. Inhibition of adenylate cyclase (AC)
  2. decrease of cAMP in cell
  3. Increase in K+ efflux
  4. Decrease in Ca+ influx
A
  • Gi/Go protein coupled receptors
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5
Q

Muscarinic ACh (M2), Alpha-2 adrenoceptors, serotonin receptors: 5-HT1

A
  • Gi/Go protein coupled receptors examples
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6
Q
  1. Activation of phospholipase C
  2. Increase in InsP3 and Ca2+
  3. Conversion of PIP2 into DAG
  4. Increase in protein kinase C
A
  • Gq protein coupled receptors
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7
Q

Muscarinic ACh (M1, M3), Alpha-1 adrenoceptors, serotonin receptors: 5-HT2, Histamine H1

A
  • Gq protein coupled receptors examples
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8
Q
  1. Activation of adenylate cyclase

2. Increase of cAMP in the cell

A
  • Gs protein coupled receptors
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9
Q
  1. Ligand binds receptor
  2. Protein phosphorylation occurs
  3. Gene transcription
  4. Protein synthesis
  5. Cellular effects
A
  • Kinase-linked receptors
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10
Q

Insulin, growth factor and cytokine receptors

A
  • kinase linked receptors
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11
Q
  1. Ligand enters the nucleus
  2. Gene transcription
  3. Protein synthesis
  4. Cellular effects
A
  • nuclear receptors
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12
Q

Steroids receptors (oestrogen receptor)

A
  • nuclear receptors
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13
Q

Two most important things for drug-receptor interaction

A
  1. A close fit between the drug and receptor is essential

2. Strong binding forces

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14
Q

Binding forces

A
  • Covalent > ionic > hydrogen > van der waals > hydrophobic
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15
Q

Excellent receptor fit and elicits a therapeutic response

A
  • agonist
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16
Q

Strength of binding between drug and receptor

A
  • affinity
17
Q

Weak binding forces means

A
  • short interaction with the receptor

and vice versa with strong binding forces

18
Q

Measured by the dissociation constant Ko (50% occupancy)

A
  • affinity
19
Q

Tendency to activate the receptor and the strength of response after binding to the receptor

A
  • efficacy
20
Q

Drugs with a high ______ usually have a high affinity and occupy a significant proportion of receptors EVEN at LOW concentrations

A
  • potency
21
Q

Measured for example as EC50 (concentration that leads to 50% of the maximum effect)

A
  • drug potency

- > more to the left on the graph

22
Q

Agonists

A
  • lead to a response
23
Q

Antagonists

A
  • lead to no response
24
Q

Activation is governed by ____

A
  • efficacy
25
Q

Occupation is governed by ____

A
  • affinity
26
Q

Antagonist binds with the active site of the enzyme molecule and prevents the binding of a substrate molecule (no product molecules generated)

A
  • competitive antagonist
27
Q

Antagonist binds with the inhibitor site of enzyme molecule. Molecule may still bind with the enzyme molecule, but the reaction is hindered.

A
  • non-competitive antagonist
28
Q

When an antagonist is added there is a parallel shift to the right, an increase in the EC50(potency) and no change in maximum effect (efficacy)

A
  • competitive inhibition

- > can overcome antagonist by increasing dose of agonist

29
Q

When an antagonist is added there is a decreased maximum response (efficacy) and no change in EC50(potency)

A
  • non-competitive inhibition

- > can NOT overcome antagonist by increasing dose of agonist

30
Q

Acts on receptors that always lead to a response and lowers the constitutive level of receptor activation

A
  • inverse agonists
31
Q

Prolonged use of an agonist leads to? Prolonged use of an antagonist leads to?

A
  • receptor down-regulation

- receptor up-regulation

Pharmacology (9 decks)

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