pharmacodynamics Flashcards

1
Q

nitroglycerin

A
  • Eg nitroglycerin is taken
    § During an angina attack to relieve pain
    § Before activities that usually cause angina
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2
Q

metoprolol

A
  • Metoprolol must be taken regularly to reduce occurrence of angina episodes
    • Prophylactic administration
      • Typical for drugs used to treat chronic diseases
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3
Q

Potency

A
  • The dose required to produce and effect
    • A drug that produces its effects at lower doses is said to be more potent
      -
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4
Q

Effectiveness

A

A drug that produces a greater maximum level of effect is said to be more effective

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5
Q
  • Affinity
A
  • Tendency of a drug to bind to it’s target
    - Depends on the existence of
    § Complementary chemical forces of attraction and
    § Complementary 3D shapes between drug and target
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6
Q

fraction of target bound by drug

A

[drug]/[drug].Ka

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7
Q

Ka

A

concentration of the drug at which 50% of receptors are bound
□ A measure of affinity
□ Inverse relationship - low Ka means high affinity

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8
Q

Rt

A

total number of receptors

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9
Q

f

A

the efficiency of coupling between receptor activation and the end effect
○ Capacity of the activated receptor in creating an effect

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10
Q
  • Sigmoidal dose response curve
A

○ Plot of log[agonist] vs effect

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11
Q

EC50

A
  • Measures agonist potency

- Concentration of a drug required to produce 50% of its maximum response

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12
Q

EC50 depends on

A
○ Affinity 
		○ Efficacy 
		○ Cell dependant parameters
			§ Density of receptors 
			§ Efficiency of coupling
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13
Q

phenylephrine

A

nasal decongestant

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14
Q

salbutamol

A

an asthma reliever

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15
Q

Metoprolol binds

A
  • Competitive antagonist
    • Binds to B1 adrenocepttor and occupies the binding site of the receptor it inhibitts the binding of adrenaline to the receptor
    • Blocks the binding and actions of adrenaline
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16
Q

metoprolol causes

A
  • Blocks the binding and actions of adrenaline
    ○ Decreases chances of oxygen debt
    ○ Decreases frequencies of angine attacks
17
Q

metoprolol side effects

A
- At higher concentrations 
		○ Metorpolol binds to B2 
			§ May cause adverse side effects 
			§ May worsen symptoms in people with asmtha 
			§ By reducing bronchodilatation
18
Q
  • Labetolol
A

○ Has high affinity for alpha and beta adrenoceptors.

○ ADR selective antagonist

19
Q
  • Propanolol
A

○ Beta adrenoceptor selective antagonist