Nervous System Pharmacology 💊 Flashcards

1
Q

What type of pain is transmitted via myelinated Ad fibres?

A

Sharp, well-localised pain

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2
Q

What type of pain is transmitted via non-myelinated C fibres?

A

Dull, diffuse, burning pain

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3
Q

What are the actions of stimulating opioid receptors?

A

Hyperpolarisation by potassium efflux, inhibit transmitter release, inhibit adenylyl cyclise so reduce cAMP production

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4
Q

What are some side effects of morphine?

A

Respiratory depression, nausea and vomiting, constipation

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5
Q

What structure in the nervous system help modulate pain peripherally and centrally?

A

Peripherally- substantia gelatinosa

Centrally- peri aqueductal grey

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6
Q

What are some endogenous opioids?

A

Enkephalins, endorphins, dynorphins

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7
Q

What type of receptors are opioid receptors?

A

G-protein coupled receptors

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8
Q

What are two common mechanisms of opioid tolerance?

A

1- phosphorylation and uncoupling, 2- cAMP production

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9
Q

What is morphine’s bioavailability like orally?

A

Poor

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10
Q

Can morphine easily cross the blood-brain barrier?

A

No it struggles to cross BBB

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11
Q

What are the metabolites of morphine formed from glucoronidation in the liver, which exerts therapeutic effect?

A

M6G- exerts therapeutic effect

M3G

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12
Q

How is morphine excreted?

A

Renally

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13
Q

How does fentanyl’s bioavailability compare to morphine’s?

A

Fentanyls is much higher

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14
Q

Can fentanyl cross the blood-brain barrier?

A

Yes- high level of CNS crossing

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15
Q

How is fentanyl metabolised and excreted?

A

Hepatic metabolism via CYP3A4

Excreted renally

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16
Q

How does codeine get broken down?

A

Codeine gets broken down into morphine via CYP2D6 enzyme

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17
Q

Why would you not give codeine to children under 12?

A

Risk of respiratory distress which is worse in children

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18
Q

How is buprenorphine metabolised and excreted?

A

Hepatic metabolism via CYP3A4

Biliary excretion

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19
Q

How does buprenorphine’s affinity for opioid receptors compare to that of morphine’s?

A

Buprenorphine has much higher affinity

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20
Q

What are some side effects of buprenorphine?

A

Respiratory depression, low BP, dizziness, nausea

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21
Q

What is an example of a mixed agonist-antagonist (partial agonist) of opioid receptor?

A

Buprenorphine

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22
Q

What is an example of an opioid receptor antagonist?

A

Naloxone

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23
Q

What is naloxone’s bioavailability like orally?

A

Very low

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24
Q

What is the duration of action of naloxone?

A

30-60mins

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25
Q

Starting from highest to lowest affinity for opioid receptors list morphine, buprenorphine and naloxone

A

Buprenorphine > naloxone > morphine

26
Q

What are some contraindications of opioid treatment?

A

Hepatic failure, acute respiratory distress, comatose, head injuries, raised ICP

27
Q

What examples of anxiolytics?

A

Diazepam, lorazepam, midazolam

28
Q

What is the action of anxiolytics?

A

They increase GABA activity which is an inhibitory neurotransmitter

29
Q

What drug classes are in the category of anti-emetics?

A

H1 antagonists, D2 antagonists, 5HT3 antagonists, muscarinic antagonists and neurokinin-1 antagonists

30
Q

What is an example of a h1 antagonist anti-emetic?

A

Cyclizine

31
Q

What are examples of d2 antagonist anti-emetic drugs?

A

Domperidone, metoclopramide

32
Q

What is an example of a 5HT3 antagonist anti-emetic drug?

A

Ondansetron

33
Q

What i an example of a muscarinic antagonist anti-emetic drug?

A

Hyoscine hydrobromide

34
Q

What is an example of a neurokinin-1 antagonist anti-emetic drug?

A

Aprepitant

35
Q

Which anti-emetic is first line for motion sickness?

A

Hyoscine hydrobromide

36
Q

What anti-emetics are given in chemotherapy with high chance of emesis?

A

Ondansetron and aprepitant and metoclopramide for rescue

37
Q

What are some side effects of metoclopramide?

A

Extra-pyramidal effects (dystonia, Parkinsonism) and galactorrhoea

38
Q

What are some side effects of domperidone?

A

Galactorrhoea, sudden cardiac death

39
Q

What are some examples of anti-psychotics?

A

Chlorpromazine, haloperidol

40
Q

What is the primary action of anti-psychotics? What other agents can they act as?

A

Post synaptic D2 receptor antagonism, have anti-emetic effects

41
Q

What is the purpose of high dose aspirin?

A

Analgesia

42
Q

How does aspirin exert an analgesic effect?

A

Inhibits prostaglandin production

43
Q

What are examples of opioid receptor agonists?

A

Buprenorphine, fentanyl, morphine, codeine, methadone, tramadol

44
Q

What is given to a patient suffering paracetamol overdose?

A

Acetylcysteine

45
Q

What drug is given in opioid overdoses because its an opioid receptor antagonist?

A

Naloxone

46
Q

What are some anti-epileptic drugs which work by blocking sodium channels?

A

Carbamazepine, lamotrigine, phenytoin

47
Q

What are side effects of carbamazepine?

A

Suicidal thoughts, joint pain and bone marrow failure

48
Q

Why should you be careful adjusting doses of phenytoin?

A

Has zero order kinetics

49
Q

What are side effects of phenytoin?

A

Bone marrow suppression, hypotension, arrhythmias

50
Q

Which anti-epileptic is first line for generalised epilepsies?

A

Sodium valproate

51
Q

What are the side effects of sodium valproate?

A

Liver failure, pancreatitis, lethargy

52
Q

Which anti-epileptic is safe in pregnancy?

A

Levetiracetam

53
Q

Is sodium valproate a CYP inducer or inhibitor?

A

Inhibitor

54
Q

Are phenytoin, barbiturates and carbamazepine CYP inducers or inhibitors?

A

Inducers

55
Q

How long will someone with epilepsy need to be seizure free for before they can reapply for their driving license?

A

1 year

56
Q

Why is levodopa always given in combination with DOPA decarboxylase inhibitor?

A

Prevents conversion to dopamine in peripheral tissues: therefore less side effects and more L-dopa reaching the brain

57
Q

What are some dopamine receptor agonists used in the treatment of Parkinson’s disease?

A

Rotigotine, ropinirole, apomorphine, amantadine

58
Q

What drug class are rasagiline and selegiline which are used to treat Parkinson’s disease?

A

Monoamine oxidase type B inhibitors

59
Q

What is an example of a COMT inhibitor?

A

Entacapone

60
Q

What are some side-effects of dopamine receptor agonists?

A

Impulse control disorders, sedation, hallucination, confusion, nausea, hypotension