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Neurology > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

How do NSAIDs reduce pain

A

Act at the site of injury
They block the synthesis of prostaglandins which decreases nociceptor sensitisation in inflammation
Also decrease recruitment of leukocytes that cause inflammation

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2
Q

How do local anaesthetics work

A

They supress nerve conduction by blocking sodium channels

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3
Q

How do opioids work to reduce pain

A

Suppressing synaptic transmission of nociceptive signals
Block the first step in the dorsal horn of spinal cord
Can also work higher in CNS to activate inhibitory controls - in the PAG or the nucleus raphe magnus

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4
Q

How do tricyclics work to reduce pain

A

The decrease the reuptake of key substances such as adrenalin and 5HT

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5
Q

How do antiepileptics work to decrease pain

A

They target ion channel that become upregulated in nerve damage
Decreases release of NT from nociceptive neurons - less firing

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6
Q

Describe the ladder of analgesics

A

Paracetamol or NSAID at bottom - mild pain
Weak opioids such as co-codamol for moderate
Strong opioids - morphine for severe pain

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7
Q

What is the difference between opioids and opiates

A

Opiates are substances that are extracted from opium

Opioids refers to any agent that acts on opioid receptors

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8
Q

Describe supraspinal anti-nociception

A

The way the brain regulates pain
Regions involved in pain perception send signals to brainstem nuclei which can then send fibres to the spinal cord to modify the pain signals

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9
Q

Which brain regions are involved in pain and emotion perception

A

Cortex
Amygdala
Thalamus
Hypothalamus

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10
Q

What is the significance of the periaqueductal grey matter

A

Excitation of this area provides profound analgesia
Can be activated by endogenous opioids or morphine (and related drugs)
Once active it suppresses nociceptive transmission at the spinal cord

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11
Q

What type of receptors are opioid receptors

A

G-protein coupled

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12
Q

What are the major adverse effects of opioids

A 
Addictive potential 
Respiratory depression - worse when asleep 
Postural hypotension 
Nausea and vomiting 
Confusion, dysphoria, hallucinations
Dizziness 
Myoclonus 
Hyperalgesia if excessive use
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13
Q

What type of pain are opioids not good at treating

A

Neuropathic

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14
Q

How is morphine metabolised

A

Metabolised in the liver
Glucuronidation reaction produces an inactive product (M3G) and an active analgesic (M6G)
Excreted by the kidney

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15
Q

How can morphine be delivered

A

IV - acute setting

IM, SC or orally in general wards

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16
Q

Which administration route for morphine is best for chronic pain

A

Oral
Immediate as oramorph
or Sustained release

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17
Q

How long do sustained release morphines last

A

12-24hrs

High dose in tablet which is released slowly

18
Q

Describe the use of diamorphine

A

More lipophilic than morphine
Crosses the BBB rapidly when given IV
Only used for severe post-op pain
Heroin is in this class

19
Q

How is codeine used

A

For mild/moderate pain as it is a weaker opioid
Given orally
Has anti-diarrhoeal action

20
Q

How is codeine metabolised

A

In the liver
Converted to small amounts of morphine which gives the analgesia
Some people have variations in the enzymes that do this so codeine wont work as well

21
Q

What are the 2 main synthetic forms of codeine which are more potent

A

Oxycodone

Hydrocodone

22
Q

Describe the use of fentanyl

A

Extremely potent - 100x more than morphine
Given IV in some surgeries to act as analgesic in anaesthesia
Can be given as transdermal patch in chronic pain states

23
Q

Describe the use of pethidine

A

Used in acute pain, particularly labour
Rapid action when given IV, IM or SC
Short action so not good for chronic pain

24
Q

What drugs can not be used alongside pethidine

A

MAO inhibitors - anti-depressant and Parkinson drug

Will cause excitement, convulsions and hyperthermia

25
Q

Describe the use of buprenorphine

A

Partial agonist of opioid receptors
Used in chronic pain with syringe drivers
Slow onset but long duration

26
Q

Describe the use of tramadol

A

Significant analgesic action by potentiating descending pathways
Given orally
DONT give to epileptics

27
Q

Describe the use of methadone

A

Weaker agonist
Given orally
Long duration of action
Used for chronic cancer pain or heroin withdrawal

28
Q

How is naloxone used

A

It is a competitive agonist for opioid receptors
Used to reverse opioid toxicity
Given IV, IM or SC
Need to monitor dose and patient as toxicity can recur in longer acting preparations

29
Q

When may a newborn baby need naloxone

A

If they have respiratory depression due to opioid toxicity from mother taking pethidine as a painkiller in labour

30
Q

What is the risk with naloxone administration

A

Sudden withdrawal can make people agitated and violent

Particularly in addicts

31
Q

What drugs are antagonist of opioids

A

Naloxone
Naltrexone - oral and long half life
Alvimopan

32
Q

What actions do NSAIDs have

A

Analgesia
Antipyretic
Anti-inflammatory

33
Q

Give examples of NSAIDs

A

aspirin
ibuprofen
naproxen
diclofenac

34
Q

How do NSAIDs work (in general)

A

Inhibit synthesis of prostaglandins by inhibiting COX-1 and 2 enzymes

35
Q

Where are the COX enzymes active

A

COX-1 is active continuedly
COX-2 is induced at the site of inflammation by cytokines

Most therapy of NSAIDs is due to COX2 inhibition

36
Q

What are the adverse effects of NSAIDs

A

GI damage - as COX1 produces a protective prostaglandin

COX2 specific are prothrombotic so use is limited

37
Q

Which drugs are useful for neuropathic pain

A

Gabapentin and pregabalin - anti-epileptics
Amitriptyline - tricyclics
Carbamazepine

38
Q

When is gabapentin used

A

Migraine prophylaxis

39
Q

When is pregabalin used

A

Painful diabetic neuropathy

40
Q

How does carbamazepine work to reduce pain

A

Blocks voltage activated Na channels which become upregulated in damaged nerve cells

41
Q

When is carbamazepine used

A

First line to control pain intensity and frequency in trigeminal neuralgia

Neurology (18 decks)

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