Misc Flashcards
H1 antagonist
first gen -diphenhydrazine ->IV and oral second gen -cetirizine and loratadine ->only oral ->no anti muscurinic effects
MOA
- competitively antagonise H1
- > inhibit NO release and vasodilation
- > smooth muscle contraction and bronchospasm
- > decrease vascular permeability
- > improve AV nodal conduction
- anti muscurinic effect
- > sedation
- > anti motion sickness
SE
- sedation
- atropine like effects
- > dry mouth
- > constipation, urinary retention
ppi
Omeprazole
MOA:
-irreversible inhibitors of H/K antiporter on gastric parietal cells
Se:
- headache
- nausea/vomiting
- diarrhoea/constipation/flatulence
- abdominal pain,
- decreases absorption fe/ca/impairs absorption of drugs
possible associations with
- clostridium difficile infection
- community acquired pneumonia
- decreased serum vitamin B12 concentration (long-term)
- chronic kidney disease
- fracture (long-term use)/caution in osteoporosis
bismuth subsalicylate
MOA
-antisecretory and antimicrobial action
SE
- faeces grayish black
- black tongue
- cns sedation with confusion
H2 antagonist
ranitadine, cimitadine
MOA
- inhibit H2 receptor on gastric parietal cells
- > decrease acid secretion
SE
- tachyphylaxis
- rare
- > gynecomastia
- > impotence
- > B12 deficiency
- > confusion, hallucinations
- > inhibit CYP450
- > arrythymias
epinephrine
MOA
- α 1
- > vascoconstriction -> increase TPR
- > decrease mucosal edema in upper airway
- Beta1
- > inotropy and chronotropy
- Beta2
- > bronchodilation
- > decreased release of inflamm mediations from mast cells/basophils
SE
- fight/flight response
- > anxiety, dizziness
- > headache
- > tachycardia, palpitations
- > tremor
- serious effects
- > arrhythmias
- > angina/MI
- > pulmonary edema
- > hypertensive crisis
- > intracranial haemorrhage
morphine
MOA
- binds to mu receptor in CNS
- > G protein coupled
- > found on pre and post synaptic interneurons
- decreases perception and response to pain
- > dissociative
SE
- sedation
- resp depression
- > acts on mu receptors in resp centre of medulla
- > resp drive taken over by peripheral O2 receptors
- > don’t give 02 unless mechanically ventilated
- suppress cough reflex
- nausea and vomitting
- > stimulation of chemoreceptor trigger zone
- smooth muscle
- > longitudinal relax and circular constrict
- > constipation with cramping
- > urinary retention with urgency
- > exacerbate biliary colic
- > miosis
- histamine release
- > vasodilation
caution in renal failure as metabolite is highly active
post op opioid parenteral routes
parental opioid ROA
- bolus IV
- > moderate pain
- > avoids resp depression
- > doesn’t easily achieve steady state
- continuous infusion
- > for severe pain not managed by bolus
- > only in ventilated or ICU patients
- PCA
- > conscious, cooperative patient
- > decreases time to pain relief and risk of OD
- subcut
- > in palliative care
- > better than IM
- IM least prefered
- > variable absorption
- > lag time
- > painful
non opioid adjuncts post op
NSAIDs
- can reduce opioid use and side effects
- not routinely used in post op
- > renal dysfunction
- > cardiovascular and thrombotic effects in healthy people
- non selective
- > anti platelet and increased risk bleeding
- selective
- > no anti-platelet effect
- > less GI
- > same renal/cardiovascular/CVA risk
Paracetamol
- every 4-6 hours
- > max 4g/day
- IV and oral same efficacy
- moderate to severe (combined with opioids)
- > improves quality of analgesia and satisfaction
regional and local analgesia
- usually by infusion but can be PCA
- reduces systemic analgesia including opioids
oral opioids
morphine
-variable absorption makes titration difficult
oxycodene
- 1.5x oral morphine
- common
- risk of addiction
codeine
- 1/10th oral morphine
- approximately 10% of people
- > rapid metabolisers and toxicity
- > no analgesic effect (CYP2D6 gene)
tramadol
- 1/5th of oral morphine
- less typical side effects (including resp depression)
- less association with addiction and dependence
- serotonergic effects
- > nausea
- > sweating
- > dizziness
- > serotonin syndrome with other serotonergics
parenteral opioids
- morphine
- > peak in 20
- > half life = 3 hours
- > repeat dose 3-4hrs
- hydromorphone (semi-synthetic)
- potency 5x morphine
- peak within 10
- half life = 2hrs
- > repeat dose 3-4 hrs
- fentanyl (synthetic)
- > potency almost 100x morphine
- > peak within 5mins
- > half life 90mins
- > effective for rapid, less for ongoing
- sufefentanyl
- > potency 6x fentanyl
- > 2 mins onset, rapid half life
- > limited role in post op pain
- meperidine
- > has antimuscurinic effects
- > cannot use with PCA due accumulation of metabolite
- oxycodone
- > equivalent dose to morphine IV
- tramadol
- > 1/5th morphine IV
approach to pain
pain score 1-3 (mild)
- non pharm
- if not working, oral paracetamol
pain score 4-6 (moderate)
- step 1
- > and/or oral NSAID
- resistant and reduce quality of life
- > and/or oral opioid
- > codeine/tramadol/oxycodone
pain score 7-10 (severe)
- as for step 2 with increased dose
- or IV opioids
- > morphine
- > fentanyl
- > hydromorphone
- > oxycodone
in opioid addiction
- overall
- > early advice from pain specialist/addiction medicine specialist
- > contact managing doctor
- methadone
- > tolerance, dependence and withdrawal risk
- > PRN can be useful
- > consider local/regional analgesia
- naltrexone
- > reduced response to opioids
- > rebound hypersensitivity due to up-regulation
Octreotide
MOA
- somatostatin analogue
- inhibits serotonin release
- decrease portal venous flow
SE
- cardio
- > sinus Brady
- > HTN
- CNS
- > fatigue
- > headache
- > dizziness
- GI
- > abdo distress
- > abdo pain
- Endocrine
- > hypothyroid
- > hyperglycaemia
- muscular
- > back pain
- > arthragia/myalgia
magnesium sulfate
MOA
- unknown
- > may block glutamate receptors or cerebral vasodilation
SE
- flushing
- nausea/vomiting
- headache
- dizziness
Adverse effects
- hypermagnesaemia
- > loss of deep tendon reflexes
- > respiratory depression
- > CNS depression
- > hypotension/bradycardia/cardiac arrest
Precautions
- nifidepine
- > increases effects and respiratory depression
- renal dysfunction
- > hypermagnesaemia (monitor magnesium levels)
- before administering
- > assess deep tendon reflexes
- > determine resp rate
- during administration
- > monitor BP/HR/RR/O2 and urine output
- > use calcium gluconate if toxic
Magpie trial -Setting ->over 10,000 participants ->multicenter across dozens of countries -Eligibility ->hypertensive with proteinuria ->uncertainty for mag sulfate treatment -Outcomes ->eclampsia ->fetal/neonatal death -Eclampsia results ->risk ratio (compared to placebo) for severe or non severe = approx 0.40 ->risk reduction greater <34 compared to >34 ->NNT for severe = approx 60/ non severe = approx 100 -Baby results ->no reduction (very small increase in death)