3. Pharmacodynamics Flashcards

1
Q

Receptor activators (2)

A

Adrenaline, morphine

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2
Q

Enzyme inhibitor

A

aspirin

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3
Q

Enzyme false substrate

A

methyldopa

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4
Q

Receptor blocker

A

tubocurarine

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5
Q

Ion channel blockers

A

Local anaesthetics

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6
Q

Ion channel modulators (2)

A

Diazepam, general anaesthetics

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7
Q

Neurotransmitter uptake blocker

A

Prozac

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8
Q

What are the 4 different types of receptors?

A
  1. Ligand gated ion channels (ionotropic)
  2. G protein coupled receptors (metabotropic)
  3. Kinase-linked.
  4. Nuclear - linked to gene transcription.
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9
Q

How can responses be measured experimentally? (5 ways)

A
  1. Production of second messenger
  2. Muscle contraction.
  3. Electrophysiology.
  4. Inhibition of transmitter release.
  5. Changes in heart rate
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10
Q

What is affinity?

A

how well a ligand binds to a receptor

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11
Q

What is efficacy?

A

Measure of the response of the binding

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12
Q

Potency =

A

Efficacy + affinity

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13
Q

What are 4 things that cause desensitisation?

A
  1. Change to receptors (phosphorylation)
  2. loss of receptors (internalisation)
  3. Exhaustion of mediators
  4. Physiological adaptation - homeostatic response
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14
Q

Which clinical agonists (2) used to increase heart rate and force of contraction?

A

Adrenaline and dopamine

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15
Q

Which clinical agonist is used for asthma?

A

Salbutamol

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16
Q

Which clinical agonist is used for nasal congestion?

A

oxymetalazine

17
Q

Which clinical agonist is used as an analgesic for severe pain?

A

morphine

18
Q

Why might partial agonists be used?

A

reduce overactivity but not block basal activity

19
Q

Example of partial agonist?

A

Buprenorphine. Less abuse liability and dysphoria.

20
Q

What are 4 examples of competitive receptor antagonists?

A

Naloxone - opiate overdose
Beta blockers - anxiety/hypertension
Tubocurarine - muscle relaxant
Chlorpromazine - schizophrenia