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Pharmacology > Pain medications (NSAIDs etc) > Flashcards

Pain medications (NSAIDs etc) Flashcards

1
Q

NSAID indications

A

As needed for mild-moderate pain (e.g. dental, dysmenorrhoea)

Inflammation- MSK, RA, osteoarthritis, acute gout

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2
Q

NSAIDS MOA

A

Inhibits cyclo-oxygenase enzyme (COX) which inhibits the synthesis of prostaglandins from arachidonic acid

COX1 stimulates PGE synthesis (gastric mucosa, renal perfusion, inhibits clots)

COX-2: expressed in response to inflammatory stimuli. PGE which causes inflammation and pain

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3
Q

NSAIDs adverse reactions

A
  • GI toxicity
  • renal impairment
  • increased CVS event (MI/stroke)
  • hypersensitivity reactions

avoid in asthma, heart failure, liver failure, NSAID hypersensitivity, peptic ulcer disease, GI bleeding. meds such as anticoagulants, corticosteroids, aspirin

phospholipid -> aracodonic acid which gives
prostaglandin, thromboxane, leukotiene, PC

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4
Q

how are NSAID’s prescribed

A

taken orally (PO)
topical gels
suppositories
injectible preperations

regular treatment for at least 3 weeks is required.

acute pain: naproxen 250mg orally 6-8hrly as needed

ibuprofen 400mg

*if at risk of GI complications give PPI (lansaprozole 15mg daily)

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5
Q

types of NSAIDs

A

Ibuprofen
Naproxen
Etoricoxib

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6
Q

Paracetemol

A

first line analgesic for most forms of acute and phonic pain

antipyretic - can reduce fever and it’s associated symptoms (shivering)

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7
Q

MOA of paracetemol

A

poorly understod
weak inhibitor of COX- enzyme involved in prostaglandin metabolism

COX inhibition increases pain threshold and reduces PGE concentration

*weak anti inflammatory

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8
Q

paracetamol adverse effects

A

overdose- liver failure
metabolised by P45O enzyme into a toxic metabolite NAPQ (N-acetyl benzoquinonine? which is conjugated into glutathione. in a nOD this is saturated and NAPQI accumulates causing hepatocellular necrosis.

*treat with acetylcystine

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9
Q

paracetamol warnings

A

not indicated in liver toxicity, chronic excessive alcohol use, malnutrition, low body weight, severe hepatitisc imaprierment

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10
Q

important reactions of paracetemol

A

CYP inducers (phenytoin and carbamazepine) increase risk of NAPQI

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11
Q

how is paracetamol prescribed?

A

PO (orally)
IV infusion
rectal administration

0.5-1g every 4-6 hours
maximum of 4g daily

IV solution can be infused over 15 minutes or diluted in 0.9% saline chloride or 5% glucose solution before administation

regular/as required.

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12
Q

opioid examples

A

strong opioid:
morphine
oxycodone

weak opioid:
tramadol
codeine
dihydrocodeine

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13
Q

common indications for strong opioids

A

rapid relief of acute and severe pain including post-operative pain and pain associated with acute MI

relief of chronic pain (WHO ladder)

breathlessness (end of life care). breathlessness and anxiety in acute pulmonary oedema

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14
Q

strong opioids MOA

A

activation of opioid u receptors in the CNS (G couples receptors)reduces neuronal excitability and pain transmission

in the medulla, opioids blunt the response to hypoxia and hypercapnoea which reduces the rest drive and breathlessness.

reduces the sympathetic nervous system activity
(can reduce cardiac work and o2 demand)

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15
Q

adverse effect of opioids

A 
respiratory depression (reduces respiratory drive)
euphoria, detachement, neurological depression

activates the chemoreceptor trigger zone causing nausea and vomiting

pupillary constriction

large intestine - u receptor increases smooth muscle tone. reduces motility= constipation

skin= histamine= itching, urticaria, vasodilation, sweating

tolerance= dependence= withdrawal

important to consider age and GFR (do not give if GFR <50, give fentanyl insteaD)

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16
Q

strong opioid warning + reactions

A

! hepatic failure
! renal impairment
(opioids rely on the liver and kidneys for elimination)

! respiratory failure and reduced consciousness (sedation) . reverse with naloxone 400mg IV/subcut/IM
! biliary colic

do not give with other sedating drugs like antipsychotics, benzos, TCA’s

17
Q

how are opioids prescribed

A

acute severe pain in high dependency areas

IV rapid effect

2-10mg initiall tailored to age and GFR
IM or SC

30mg PO 2-4 hrly
10mg IV (divide oral by 3 for IV dose)

chronic
oramorph 5mg orally every 4 hours

breakthoruh analgesia
immediate release morphien at a dose of 1/6th of the Toal daily dose.

18
Q

features of opioid withdrawl

A 
opposite of the clinical effect
pain
breathlessness increase
anxiety
pupils dilate
skin is cool and dry with piloerection (cold turkey)
19
Q

MOA of weak opioids

A

codeine and dihydrocodine are very weak opioids in their unmodified form. when they are metabolised by the liver they produce a relatively small amount of morphine (from codeine) or hydromorphine (from dihydrocodeine) which are stronger agonsit of opioid mu receptors.

tramadol is a synthetic analogue of codeine

20
Q

tramadol MOA

A

synthetic analogue of codeine
moderate strength opioid
u receptor agonist
affects the serotonergic an adrenergic pathway where it is thought to act as a seretonin and noradrenaine reuptake inhibtor (SNRI)

21
Q

adverse effect of weak opioids

A

nausea, constipation, dizziness, drowsiness
neurological and respiratory depression

caution with resp dsease
renal impairment
hepatic imapriment
elderly
tramadol lowers seizure threshold
do not give with other sedsating drugs
22
Q

how are weak opioids perscribed?

A

PO. regular / as required.

codeine / dihydrocodeine 30mg orally 4hrly
tramadol 50mg orally 4hrly (400mg max/day)

+ laxative e.g. senna

co/codamol means 8/500 so 8mg of codeine and 500mg of paracetemol.
co-dydramol 10/500mg contians 10mg of codeine, 500mg of paracetemol.

23
Q

gabapentin and pregabalin indication (pain)

A

(focal epilepsy - not for absence or myoclonic seizures)

  1. first line for neuropathic pain including painful diabetic neuropathy. (trigeminal neuralgia= carbamezapine)
  2. GAD (pregabalin)
24
Q

gabapentin and pregabalin MOA

A

related to GABA (the major inhibitory neurotransmitter in the brain)

bind to pre-synaptic voltage sensitive calcium channels which inhibits hthe release of excitatory neurotransmittors thus reuslting in a reduction of neuronal excitabiltiy. (in brain and perpiheralnerves)

25
Q

gabapentin and pregabalin

  • side effects
  • warning
  • contraindications
A

side effects- drowsy, dizzy, ataxia
warning- renal impairment (eliminated via kidneys)
enhanced when combined with sedating drugs

26
Q

how are pregabalin/gabapentin perscribed?

A

start low dose and increase over days/weeks

27
Q

lidocaine indication

A

1st choice local anaesthetic (catheterisation, minor procedures like suturing)

antiarrhythmic drug (VT) (uncommon)

alternative to lidocaine is Bupivacaine (8-16hrs) (lidocaine lasts 2-4 hrs)

28
Q

lidocaine MOA

A

enters cells in it’s unchanged form then accepts a proton and becomes positively charged. once it’s inside the celll it blocks the voltage-gated SODIUM channels on the surface which prevents initiation and propogation of the action potentials in nerves and muscles.

in the heart it reduces duration of AP, slows conduction elocity and increases refractory period (Can terminate VT)

29
Q

lidocaine side effects, warning and important reactions

A

side effects- stinging sensation during local adminisration.

neuro- drowsy, restless, tremor, fits
little cvs toxicity but overdose can cause hypotension and arrythmias
reduced CO

if given into plasma (toxicity) CVS arrhythmias, asystole, PEA (pulseless electrical activity), low CO and low BP

if CNS- seizres LOC

reverse with intralipid antidote. lidocaine is lipid soluable (that’s how it gets into the cell) so when you give intralipid it causes the LA to ‘sink’ into it

30
Q

how is lidocaine prescribed?

A

minor procedure: 1% 10mg/mL of lidocaine hyrochloride
maximum dose is 200mg or 3mg/kg
for urinary catheterisation- gel with antiseptic agent such as chlorhexidine in pre-filled syringes (6-1mL)

31
Q

PCA

A

patient controled analgesia
bolus dose is 1mg
lockout period is 5 min (after each dose they can’t have another one for five mins)
background (never give this)

32
Q

fentanyl

A

only licenced in cancer pain
can give if not suitable for morphine (e.g if GFR <50)
does not work orally
same complicatoins as morphine

33
Q

epidural

A

rectus sheath
errectar spina for rib frcure?
canhit CSF (dural headache)
can damage nerve route
can cause bleeding (epidural haematoma), compression of spinal cord= neuropathic pain.
- epidural abscess (fever, malaise, neuropathic pain, 5-10 days after the event)

Pharmacology (14 decks)

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