Essential Pharmacology & Autonomic and Neuromuscular Pharmacology Flashcards

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1
Q

Describe the basic functions of receptors.

A

Enable specificity, evoke an appropriate response.

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2
Q

What is the function of the G-protein receptor?

A

Regulate protein function

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3
Q

What is the largest class of receptor?

A

G-protein receptors

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4
Q

What is the secondary messenger commonly associated with the G-protein receptor?

A

cAMP - by the adenyl cyclase associated with the receptor or phospholipase C.

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5
Q

What is the function of G-protein receptors that are coupled to ion channels?

A

Evoke slow EPSPs or IPSPs.

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6
Q

What are the two main locations of receptors?

A

Transmembrane and intracellular.

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7
Q

Define agonist.

A

Mimic normal effect of the receptor.

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8
Q

Define antagonist.

A

Block normal action of receptor.

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9
Q

Describe the affinity and efficacy of agonists.

A

Full agonist = high affinity and high efficacy.

Partial agonist = high affinity and low efficacy.

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10
Q

Describe the affinity of antagonists.

A

High affinity and no efficacy.

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11
Q

Describe the relationship between the concentration of the agonist and the effect.

A

Increasing agonist con concentration, increases the response until drug binds and activates all receptors. The number of receptors are limited so the maximum saturated response will be reached.

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12
Q

Define affinity.

A

Does it bind receptor?

- Strength of chemical attraction between drug and receptor (lower EC50 = higher affinity)

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13
Q

How much of a drug would be required if it has higher affinity?

A

Less of the drug.

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14
Q

Where on the dose response curve would you find a curved for a drug with low affinity?

A

Shifted to the right (higher EC50).

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15
Q

Define efficacy.

A

Does it activate the receptor?

- how good the drug is at activating the receptor.

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16
Q

Where on the dose response curve would you find a curve for a drug with low efficacy?

A

Below the curve.

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17
Q

Compare efficacy in full and partial agonists.

A

Full agonist = High efficacy

Partial agonist = Low efficacy

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18
Q

Describe the process of transmembrane signalling (G-protein coupled receptors), giving two examples.

A
  1. Adenyl cyclase - produces cAMP and regulates PKA.

2. Phospholipase C - produces DAG and regulates PKC and IP3 that regulate calcium (secondary messenger)

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19
Q

List 5 transmembrane receptors.

A
  1. Enzyme-linked
  2. Ligand-gated ion channel
  3. G-protein coupled
  4. Voltage-gated
  5. Cytokine receptor
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20
Q

List three sources of intracellular calcium.

A
  1. Internal stores (via IP3 or Ca2+ stimulated release form endoplasmic reticulum)
  2. Outside cell (via voltage-gated or ligand-gated calcium channels)
  3. Via inhibition of calcium transport out of cell.
21
Q

What are the effects of calcium?

A
  1. Directly effect target protein (e.g PKC)
  2. Bind to calmodulin which activated target.
  3. Via some other binding protein e.g troponin.
22
Q

Where would you find the dose response curve for an agonist in presence of competitive antagonist.

A

Shifted to right (agonist less likely to bump into free receptors)

23
Q

What are the potential sites of action for drugs to modulate synaptic transmission in ANS?

A
  • Inhibit acetylcholine transport
  • block voltage-gated Ca2+ ion channels
  • block vessel fusion
  • block ACh activated channel
  • block non-depolarising nicotinic receptors
  • block depolarising nicotinic receptors
24
Q

How can postganglionic parasympathetic transmission be targeted?

A

Mimic (agonist) or block (antagonist) muscarinic receptors.

25
Q

How can postganglionic sympathetic transmission be targeted?

A
  1. Block enzymes that produce NA
  2. Block transporter or transmitter
  3. Introduce false transmitter
  4. Block alpha or beta receptors
  5. Sympathiometics (potentiate synapse)
26
Q

What is the function of indirect sympathomimetics?

A

Triggers release of noradrenaline.

27
Q

Give an example of an indirect sympathomimetic.

A

Amphetamine.

28
Q

Give an example of a sympathomimetic

A

Cocaine.

29
Q

What is the function of a sympathomimetic?

A

Act directly at the post-synaptic adrenergic receptor.

30
Q

Describe a clinical application of an a1 agonist.

A

Decongestant and dilate pupils.

31
Q

Describe a clinical application for an a2 agonist.

A

Hypertension

32
Q

Describe a clinical application for a B2 agonist.

A

Asthma.

33
Q

Give an example of a B2 agonist.

A

Salbutamol

34
Q

Describe a clinical application for a B1 antagonist.

A

Hypotension and angina.

35
Q

Give an example of a B1 antagonist.

A

Atenolol.

36
Q

Describe the mechanisms by which drugs modulate transmission at the NMJ.

A
  • Inhibit choline transport
  • Block voltage-gated calcium channels
  • Block vessel fusion
  • Use depolarising or non-depolarising nicotinic receptor blockers (e.g for paralysis during surgery)
37
Q

How can you make synapses function better at the NMJ?

A
  1. Prolong the AP (more calcium release)

2. Block acetylcholinesterase (stop breakdown of ACh)

38
Q

What are the consequences of modulating synaptic transmission in the ANS and NMJ?

A

Too many side-effects so next to no clinical applications. Drugs modulate both sympathetic, parasympathetic and NMJ transmission.

39
Q

What type of receptors does Acetylcholine bond to?

A

Cholinergic receptors.

40
Q

Give two examples of cholinergic receptors.

A
  1. Nicotinic

2. Muscarinic

41
Q

What cholinergic receptor is a g-protein receptor?

A

Muscarinic

42
Q

What cholinergic receptor is ionotropic?

A

Nicotinic

43
Q

How many sub-types does the muscarinic receptor have?

A

3 (M1, M2, M3)

44
Q

How many sub-types does the nicotinic receptor have?

A

2 (N1, N2)

45
Q

What type of receptors does Noradrenaline and adrenaline bind to?

A

Adrenergic

46
Q

What type of receptors are the adrenergic receptors?

A

G-protein receptors

47
Q

How many sub-types does the adrenergic receptor have?

A

5 (a1, a2, b1, b2, b3)

48
Q

What does the sympathetic and parasympathetic systems act on?

A

Smooth muscle, cardiac muscle, GI neutrons and glands.