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Pharmacology > 26 Analgesic drugs > Flashcards

26 Analgesic drugs Flashcards

1
Q

26.01 OPIOID DRUGS

Opioid agonists: morphine, diamorphine (heroin), buprenorphine, codeine, oxycodone - actions

A

analgesia
sedation
euphoria/reduced anxiety
physical/psychological dependence
cough suppression and respiratory depression
inhibition of gut motility

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2
Q

26.01 OPIOID DRUGS

Opioid agonists: morphine, diamorphine (heroin), buprenorphine, codeine, oxycodone - MOA

A

activates µ opioid receptors in the brain and spinal cord to inhibit pain transmission and modify the central perception of pain
activation of κ receptors may exert an additional effect on pain transmission in the spinal cord
may inhibit the activation of sensory nerve endings
opioid receptors are G protein–coupled receptors, which inhibit adenylate cyclase activity, open K+ channels and inhibit the opening of Ca2+ channels in nerve endings

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3
Q

26.01 OPIOID DRUGS

Opioid agonists: morphine, diamorphine (heroin), buprenorphine, codeine, oxycodone - abs/distrib/elim

A

given orally or by SC/IM injection
glucuronic acid conjugation in the liver
half-lives: morphine 3-4h, buprenorphine 12h
the actions of diamorphine and codeine are due, at least in part, to metabolism to morphine

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4
Q

26.01 OPIOID DRUGS

Opioid agonists: morphine, diamorphine (heroin), buprenorphine, codeine, oxycodone - clinical use

A

moderate to severe chronic and postoperative pain (codeine for mild pain)
epidural anaesthesia
neuropathic pain
treatment of painful cough
diarrhoea

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5
Q

26.01 OPIOID DRUGS

Opioid agonists: morphine, diamorphine (heroin), buprenorphine, codeine, oxycodone - adverse effects

A

hypotension
constipation, nausea, vomiting, drowsiness, dizziness tolerance, dependence and withdrawal effects
larger doses - coma with respiratory depression

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6
Q

26.01 OPIOID DRUGS

Opioid agonists: morphine, diamorphine (heroin), buprenorphine, codeine, oxycodone - special notes

A

naloxone is an opioid receptor antagonist at µ, δ and κ receptors and given in opioid overdoses
can cause withdrawal symptoms in opioid addicts

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7
Q

26.02 OPIOID DRUGS

Synthetic analogues: pethidine, fentanyl, remifentanil, sufentanil - actions

A

analgesia
euphoria
physical/psychological dependence
respiratory depression
inhibition of gut motility
(antimuscarinic effects of pethidine cause tachycardia)

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8
Q

26.02 OPIOID DRUGS

Synthetic analogues: pethidine, fentanyl, remifentanil, sufentanil - MOA

A

activates µ opioid receptors in the brain and spinal cord to inhibit pain transmission
activation of κ receptors may exert an additional effect on pain transmission in the spinal cord
may inhibit the activation of sensory nerve endings

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9
Q

26.02 OPIOID DRUGS

Synthetic analogues: pethidine, fentanyl, remifentanil, sufentanil - abs/distrib/elim

A

given orally or IM
pethidine is subject to hydrolysis and P450 oxidation, half-life 3-5h
fentanyl is also available as a transdermal patch for long-term effects
remifentanil has a very short half-life (0.1h)

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10
Q

26.02 OPIOID DRUGS

Synthetic analogues: pethidine, fentanyl, remifentanil, sufentanil - clinical use

A

moderate to severe pain
pethidine does not reduce uterine contractions so favoured for labour pain
remifentanil and sufentanil are given IV for surgical analgesia

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11
Q

26.02 OPIOID DRUGS

Synthetic analogues: pethidine, fentanyl, remifentanil, sufentanil - adverse effects

A

constipation (less than morphine), nausea, vomiting, drowsiness, dizziness, tolerance, dependence and withdrawal effects
larger doses - coma with respiratory depression

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12
Q

26.03 OPIOID DRUGS

Long-acting µ opioid receptor agonist: methadone - actions

A

analgesia
euphoria
physical/psychological dependence
respiratory depression
inhibition of gut motility

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13
Q

26.03 OPIOID DRUGS

Long-acting µ opioid receptor agonist: methadone - MOA

A

activates µ opioid receptors in the brain and spinal cord to inhibit pain transmission and modify the central perception of pain
may inhibit the activation of sensory nerve endings

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14
Q

26.03 OPIOID DRUGS

Long-acting µ opioid receptor agonist: methadone - abs/distrib/elim

A

oral absorption
long duration of action
P450 metabolism in liver
half-life 15-40h

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15
Q

26.03 OPIOID DRUGS

Long-acting µ opioid receptor agonist: methadone - clinical use

A

analgesia
maintenance of opioid addicts and assistance in withdrawal program

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16
Q

26.03 OPIOID DRUGS

Long-acting µ opioid receptor agonist: methadone - adverse effects

A

constipation, nausea, vomiting, drowsiness, dizziness
tolerance, dependence and withdrawal effects
larger doses - coma with respiratory depression and possible cardiac dysrhythmia

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17
Q

26.04 OPIOID DRUGS

Atypical narcotic analgesic: tramadol, tapentadol - actions

A

analgesia

18
Q

26.04 OPIOID DRUGS

Atypical narcotic analgesic: tramadol, tapentadol - MOA

A

weak agonist action at µ opioid receptors
main action: inhibits 5-HT and NA reuptake into nerve endings, so potentiates monoamine neurotransmission
analgesic action is inhibited by 5-HT3 receptor antagonists

19
Q

26.04 OPIOID DRUGS

Atypical narcotic analgesic: tramadol, tapentadol - abs/distrib/elim

A

given orally
subject to hepatic demethylation and conjugation
tramadol half-life 6h

20
Q

26.04 OPIOID DRUGS

Atypical narcotic analgesic: tramadol, tapentadol - clinical use

A

moderate/moderately severe pain
used postoperatively
neuropathic pain

21
Q

26.04 OPIOID DRUGS

Atypical narcotic analgesic: tramadol, tapentadol - adverse effects

A

dizziness, nausea and vomiting
respiratory depression, constipation and addiction (but less than with morphine)
convulsions

22
Q

26.05 DRUGS USED FOR NEUROPATHIC PAIN

Tricyclic antidepressants: amitriptyline, nortriptyline, desipramine - actions

A

reduction of neuropathic pain

23
Q

26.05 DRUGS USED FOR NEUROPATHIC PAIN

Tricyclic antidepressants: amitriptyline, nortriptyline, desipramine - MOA

A

analgesic action of antidepressants is mainly due to inhibition of the opening of neuronal voltage-gated Na+ channels (Nav 1.7 subtype), rather than to inhibition of monoamine reuptake
Na+ channel block reduces pain transmission from site of nerve injury

24
Q

26.05 DRUGS USED FOR NEUROPATHIC PAIN

Tricyclic antidepressants: amitriptyline, nortriptyline, desipramine - abs/distrib/elim

A

given orally
hepatic P450 metabolism (nortriptyline is a metabolite of amitriptyline)
amitriptyline half-life 12-24h

25
Q

26.05 DRUGS USED FOR NEUROPATHIC PAIN

Tricyclic antidepressants: amitriptyline, nortriptyline, desipramine - clinical use

A

postherpetic neuralgia, diabetic peripheral neuropathy, neuropathic cancer pain
pain treatment typically requires lower doses than depression treatment

26
Q

26.05 DRUGS USED FOR NEUROPATHIC PAIN

Tricyclic antidepressants: amitriptyline, nortriptyline, desipramine - adverse effects

A

sedation (antihistamine action, less with nortriptyline)
blurred vision, dry mouth, constipation, urinary retention (antimuscarinic action)
postural hypotension (α1-adrenoceptor antagonism)
overdose potentially fatal due to cardiac dysrhythmia, severe hypotension, seizure and CNS depression

27
Q

26.06 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: gabapentin, pregabalin - actions

A

reduction of neuropathic pain

28
Q

26.06 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: gabapentin, pregabalin - MOA

A

effectiveness in neuropathic pain is due to binding to the α2-δ-1 and α2-δ-2 subunits of voltage-activated Ca2+ channels (P/Q or N-type) to block Ca2+ entry and exocytosis of transmitter (glutamate) from pain nerve endings

29
Q

26.06 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: gabapentin, pregabalin - abs/distrib/elim

A

given orally
excreted unchanged
gabapentin half-life 6h

30
Q

26.06 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: gabapentin, pregabalin - clinical use

A

postherpetic and trigeminal neuralgia
pregabalin is also used for painful diabetic peripheral neuropathy

31
Q

26.06 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: gabapentin, pregabalin - adverse effects

A

sedation, dizziness and unsteadiness

32
Q

26.07 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: carbamazepine - actions

A

reduction of neuropathic pain

33
Q

26.07 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: carbamazepine - MOA

A

inhibits the opening of neuronal voltage-gated Na+ channels to reduce nociceptive transmission from site of nerve injury

34
Q

26.07 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: carbamazepine - abs/distrib/elim

A

given orally
active P450 metabolite

35
Q

26.07 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: carbamazepine - clinical use

A

second- or third-line treatment of neuropathic pain
main uses: trigeminal neuralgia, diabetic neuropathy

36
Q

26.07 DRUGS USED FOR NEUROPATHIC PAIN

Antiepileptic drugs: carbamazepine - adverse effects

A

drowsiness, headache, mental disorientation, motor disturbances
rare, but serious, adverse effects are liver damage, agranulocytosis and aplastic anaemia
serious dermatological reaction in genetically susceptible patients
strong inducer of cytochrome P450 enzymes, leading to many drug interactions

37
Q

26.08 OTHER ANALGESIC DRUGS

NSAIDs

A

ibuprofen, naproxen - COX inhibitors
mild to moderate pain due to inflammatory disease, surgery, dysmenorrhoea, headache
paracetamol - resembles NSAIDs and is effective as an analgesic, but lacks anti-inflammatory activity

38
Q

26.08 OTHER ANALGESIC DRUGS

Triptans

A

sumatriptan, zolmitriptan, eletriptan - antimigraine
triptans are agonists at 5-HT1B and 5-HT1D receptors

39
Q

26.08 OTHER ANALGESIC DRUGS

Dopamine receptor agonists

A

ropinirole, pramipexole, rotigotine - used to treat restless leg syndrome, which can be painful

40
Q

26.08 OTHER ANALGESIC DRUGS

Cannabinoids

A

nabilone, dronabinol - both synthetic cannabinoids
nabiximols - natural cannabinoids
strongest evidence for therapeutic benefit is for central neuropathic pain in multiple sclerosis

Pharmacology (34 decks)

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