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CNS > 9. Drugs for Pain > Flashcards

9. Drugs for Pain Flashcards

1
Q

What is the difference between A and C pain fibres?

A

A is fast, sharp pain

C is slow, dull ache

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2
Q

What are the endogenous opioids?

A

Endorphins
Enkephalins
Dynorphins

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3
Q

What receptors do endorphins bind to?

A

Mu

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4
Q

What receptors do enkephalins bind to?

A

Delta and mu

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5
Q

What are the types of enkephalins?

A

Met-

Leu-

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6
Q

What receptors do dynorphins bind to?

A

Kappa

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7
Q

What are the types of dynorphins?

A

A and B

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8
Q

What kind of receptors are opioid receptors?

A

GPCRs

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9
Q

What is the MOA of opiates?

A

Bind to GPCR and inhibit adenylate cyclase to reduce cAMP> close Ca++ channels or open K+ channels> reduced NT release

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10
Q

What are the inhibitory neurotransmitters?

A

GABA (brain)

Glycine (peripheral)

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11
Q

What type of drug is morphine?

A

Strong opioid agonist

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12
Q

What are the effects of morphine?

A

Increase pain threshold without loss of consciousness

Euphoria at M or dysphoria at k

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13
Q

What are the adverse effects of opiates?

A

Respiratory depression, sedation
Pinpoint pupils in overdose
Nausea, vomiting, constipation
Tolerance, dependence

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14
Q

What is methadone used for?

A

Treatment of opiate addiction

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15
Q

What increases the efficacy of fentanyl compared to morphine?

A

Has a higher lipophilicity so it can cross the BBB much more rapidly

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16
Q

What non-analgesic effect does codeine have?

A

Antitussal

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17
Q

Name an analogue of codeine

A

Tramadol

18
Q

What is the active metabolite of tramadol?

What is its other effects?

A

Dematralodol

Inhibits reuptake of NA and serotonin

19
Q

What adverse effects are associated with tramadol?

A

Increased risk of seizures, serotonin syndrome and dependence

20
Q

Name 2 opioid antagonists

A

Naloxone

Naltrexone

21
Q

What are the functions of opioid antagonists?

A

Naloxone in overdoses

Naltrexone in withdrawal

22
Q

What kind of drug is buprenorphine?

A

Mixed agonist; also has antagonist properties

23
Q

Why is buprenorphine used?

A

In withdrawal it reduces high that other opiates would give

Less euphoria, sedation, milder withdrawal

24
Q

Which opiate properties is tolerance developed to?

A

Analgesia
Euphoria
Respiratory depression
Emesis

25
Q

What opiate properties is tolerance not developed to?

A

Pupillary constriction

Constipation

26
Q

What is neuropathic pain?

A

Due to nerve damage caused by toxins, infections, autoimmunity or tumours
Numbness along path of nerve, burning or heavy sensation
Anticonvulsants and antidepressants used to treat

27
Q

What is the MOA of anticonvulsants?

A

Inactivate Na+ channel to reduce neuronal excitability

Gapabentin acts on Ca++ channels

28
Q

Name 3 anticonvulsants that act on Na+ channels

A

Carbamazepine
Lamotrigine
Phenytoin

29
Q

What is the MOA of antidepressants?

A

Monoamine reuptake inhibitors

30
Q

Name 2 topical anaesthetics

A

Lidocaine

Benzocaine

31
Q

How do topical anaesthetics work?

A

Block Na+ preventing APs

32
Q

How is systemic toxicity from an injected anaesthetic avoided?

A

Co-administer a vasoconstrictor to avoid seeping into vessels
eg. adrenaline

33
Q

Name 2 general anaesthetics that target GABA channels

A

Barbituates and benzodiazepines

34
Q

What channel does ketamine block?

A

NMDA (glutamate)

35
Q

What is the limitation of halothane as an inhaled anaesthetic?

A

Must be given with oxygen

36
Q

What is the limitation of desflurane?

A

Rapidly excreted

37
Q

What channel does nitrous oxide block?

A

NMDA

38
Q

What used to be used to describe the efficacy of inhaled anaesthetics?

A

Blood: gas partition coefficient
Blood: brain partition coefficient

39
Q

What is now used to calculate the potency of inhaled anaesthetics?

A

Minimum alveolar concentration

40
Q

What is the minimum alveolar concentration?

A

Volume of anaesthetic in inspired air that provides analgesia to 50% of population

CNS (21 decks)

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