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
Starting from highest to lowest affinity for opioid receptors list morphine, buprenorphine and naloxone
Buprenorphine > naloxone > morphine
26
What are some contraindications of opioid treatment?
Hepatic failure, acute respiratory distress, comatose, head injuries, raised ICP
27
What examples of anxiolytics?
Diazepam, lorazepam, midazolam
28
What is the action of anxiolytics?
They increase GABA activity which is an inhibitory neurotransmitter
29
What drug classes are in the category of anti-emetics?
H1 antagonists, D2 antagonists, 5HT3 antagonists, muscarinic antagonists and neurokinin-1 antagonists
30
What is an example of a h1 antagonist anti-emetic?
Cyclizine
31
What are examples of d2 antagonist anti-emetic drugs?
Domperidone, metoclopramide
32
What is an example of a 5HT3 antagonist anti-emetic drug?
Ondansetron
33
What i an example of a muscarinic antagonist anti-emetic drug?
Hyoscine hydrobromide
34
What is an example of a neurokinin-1 antagonist anti-emetic drug?
Aprepitant
35
Which anti-emetic is first line for motion sickness?
Hyoscine hydrobromide
36
What anti-emetics are given in chemotherapy with high chance of emesis?
Ondansetron and aprepitant and metoclopramide for rescue
37
What are some side effects of metoclopramide?
Extra-pyramidal effects (dystonia, Parkinsonism) and galactorrhoea
38
What are some side effects of domperidone?
Galactorrhoea, sudden cardiac death
39
What are some examples of anti-psychotics?
Chlorpromazine, haloperidol
40
What is the primary action of anti-psychotics? What other agents can they act as?
Post synaptic D2 receptor antagonism, have anti-emetic effects
41
What is the purpose of high dose aspirin?
Analgesia
42
How does aspirin exert an analgesic effect?
Inhibits prostaglandin production
43
What are examples of opioid receptor agonists?
Buprenorphine, fentanyl, morphine, codeine, methadone, tramadol
44
What is given to a patient suffering paracetamol overdose?
Acetylcysteine
45
What drug is given in opioid overdoses because its an opioid receptor antagonist?
Naloxone
46
What are some anti-epileptic drugs which work by blocking sodium channels?
Carbamazepine, lamotrigine, phenytoin
47
What are side effects of carbamazepine?
Suicidal thoughts, joint pain and bone marrow failure
48
Why should you be careful adjusting doses of phenytoin?
Has zero order kinetics
49
What are side effects of phenytoin?
Bone marrow suppression, hypotension, arrhythmias
50
Which anti-epileptic is first line for generalised epilepsies?
Sodium valproate
51
What are the side effects of sodium valproate?
Liver failure, pancreatitis, lethargy
52
Which anti-epileptic is safe in pregnancy?
Levetiracetam
53
Is sodium valproate a CYP inducer or inhibitor?
Inhibitor
54
Are phenytoin, barbiturates and carbamazepine CYP inducers or inhibitors?
Inducers
55
How long will someone with epilepsy need to be seizure free for before they can reapply for their driving license?
1 year
56
Why is levodopa always given in combination with DOPA decarboxylase inhibitor?
Prevents conversion to dopamine in peripheral tissues: therefore less side effects and more L-dopa reaching the brain
57
What are some dopamine receptor agonists used in the treatment of Parkinson’s disease?
Rotigotine, ropinirole, apomorphine, amantadine
58
What drug class are rasagiline and selegiline which are used to treat Parkinson’s disease?
Monoamine oxidase type B inhibitors
59
What is an example of a COMT inhibitor?
Entacapone
60
What are some side-effects of dopamine receptor agonists?
Impulse control disorders, sedation, hallucination, confusion, nausea, hypotension