Pain Pharma

Question 1

Name an example of a local anaesthetic.

Answer 1

Lignocane.

Question 2

Explain the use-dependant block of Na+ channels with local anaesthetics.

Answer 2

Use-dependant blocking of Na+ channels means that there is a better blocking of Na+ channels when neurotransmission is increased. More frequent opening of Na+ channels= better blocking of Na+ channels with local anaesthetics.

Question 3

List some ADRs if local anaesthetics get into systemic circulation.

Answer 3

Decreased neurotransmission, bradycardia and arrhythmia’s.

Question 4

What opioid analgesic(s) are considered to be full agonists?

Answer 4

Morphine and oxycodone.

Question 5

What opioid analgesic(s) is considered to be a partial agonist?

Answer 5

Buprenorphine.

Question 6

Opioid analgesics are agonists at what receptors.

Answer 6

Mu receptors, and they are GPCR coupled to a Gi protein.

Question 7

List the 3 main mechanisms of anti-epileptics.

Answer 7

1. Use-dependant block of Na+ channels.
2. Enhancement of GABA mediated synaptic inhibition/direct agonist to GABA receptors= decreased metabolism of GABA and increased GABA activity.
3. Inhibition of T-type Ca2+ channels= decrease in neurotransmission.