Sedation drugs fact sheet

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Sedation Drugs
Propofol
Thiopentone
Etomidate
Ketamine
no analgesia
MOA: potentiates GABA; anti-emetic; amnesia;
; decr ICP (but cerebral protective
effects offset by hypotension); anti-convulsant
Onset: 9-20 seconds
Offset: 3-9 mins; rapid redistribution
Dose: Induction: 1-2mg/kg
Procedural sedation: 0.5 – 1mg/kg over 1-5mins  0.5mg/kg boluses (initial dose 2mg/kg in children;
decr dose if >65yrs)
Infusion: 1.5-3mg/kg/hr
SE: MARKED decr BP during induction via decr PVR and venoD, myocardial dep; SBP drop >20 in 15%;
transient and fluid responsive); Marked –ive inotropic effects
Apnoea (ventilation required in 1.5% when used for sedation; intubation in 0.02%; resp complication
rates similar to midaz; resp dep seen in 50% ASA I and II, 61% ASA 4 and 5; apnoea in up to 22%;
transient hypoxia in 6-44%); prolonged in muscular dystrophies and myotonias
Prolonged  incr serum lipid levels, muscle movements, hypotonus, tremors
Pain on injection
Severe acidosis in children, with prolonged neurological sequelae on withdrawal
Myoclonic jerks / hypertonicity – rare
Propofol-related infusion syndrome: unexplained decr HR, lipidaemia, fatty liver, AGMA; rare; in
high dose prolonged infusions
CI: egg allergy
no analgesia
MOA: short acting barbiturate; amnesia;
; anti-convulsant
Indication: HI, seizures – decr cerebral metabolic rate, decr raised ICP due to intubation, anti-convulsant
Onset: 30-40secs
Offset: 10-30mins; mostly due to redistribution
Dose: induction – 3-5mg/kg (decrease to 2mg/kg if hypoV, elderly, decr LOC)
CI: multi-trauma, LV dysfunction; porphyria (causes widespread demyelination)
SE: hypotension; Apnoea; Cardiac arrhythmias; Emergence delirium; Phlebitis; Trismus; decr cerebral blood
flow
no analgesia
MOA: non-barbiturate hypnotic drug; acts at GABAa;
; no alteration to sympathetic
response to intubation
Indication: For induction in pt with limited CV reserve with minimal CV and resp depression – good in
elderly; HR unchanged; incidence of apnoea low; closed HI, decr cerebral O2 consumption and ICP
Onset: 5-15secs; Rapid LOC and mod fast recovery; slower recovery than propofol
Offset: 5-10mins; short due to redistribution from brain to highly perfused tissues
Dose: 0.1 – 0.3mg/kg  boluses 0.05mg/kg
SE: Pain on injection; myoclonic activity (20%); post-op N+V; similar resp depression to propofol
Infusion: seizures; may cause adrenocortical suppression
Prolonged infusion in critically ill  hypotension, electrolyte imbalance, oligura (due to adrenal
suppression)
analgesia
MOA: Produces dissociative anaesthetic state with catatonia, amnesia,
, maybe LOC;
Blockade of effects of glutamate at NMDA receptor; preservation of airway reflexes and respiration;
bronchorelaxant
Indication: Can be used as adjunct to volative agent instead of opioid to decr resp depression; good for
elderly and shocked pt due to CV support; anaphylaxis, hypotension, procedural sedation (children, in field),
severe pain
Onset: 30-40secs IV; 3-8min IM; mod onset and recovery
Offset: 5-10min IV; 10-30min IM
Dose: Induction: 1.5-2mg/kg IV  additional doses of 0.5-1mg/kg to prolong sedation
Procedural sedation: 0.5-1mg/kg IV / 2-4mg/kg IM / 5-10mg/kg PO
Analgesia: 5mg IV Q5minly  2-10mg/hr infusion
SE: Dose-related CV STIMULATION  incr HR, BP, CO (peak at 2-4mins, return to normal over 10-20mins)
by stimulating central SNS and inhibiting reuptake of NE, risk of MI in elderly
Marked incr cerebral blood flow, O2 consumption and ICp (significance minor in HI)
Decr RR, salivation, bronchorrhoea; laryngospasm rare (1-2.5% in children); transient resp depression
for 1-2mins if rapid IV administration; Resp adverse events more common if: IV; dose >2.5mg/kg IV;
total dose >5mg/kg IV; <2yrs age
Post-op disorientation, sensory and perceptual illusions, vivid dreams – decr by benzos
Vomiting 8%; purposeless movements; ataxia during recovery; dysphoric reactions and emergence
phenomena;; incr sympathetic tone
CI: HI, URTI, LRTI, procedures of post pharynx, CF, <3/12, incr ICP, glaucoma, globe penetration, HTN, CCF,
arterial aneurysm, porphyria, thyrotoxicosis, IHD
Midazolam
Fentanyl
Remifentanyl
no analgesia
MOA: benzo; incr GABAa binding; anxiolytic, sedative, amnesia;
; less hypotension
than propofol/thio
Onset: 2 mins IV; 15min IM/PR/PO
Offset: 30-90mins
Dose: 0.05-0.1mg/kg IV in young children
0.025-0.05mg/kg in older children and adults; ie. 2mg stat  1mg increments to 10mg max
for anxiolysis for PS in children: 0.5-0.75mg/kg PO, 0.3-0.5mg/kg IN
SE: erotic hallucinations at high dose, hypoT, resp dep, paradoxical agitation (1-15% when used PO/IN)
Pros: less phlebitis, hypoT than diazepam; less hypotension than propofol / thio
Cons: more expensive and longer recovery time than diazepam
no amnesia, no anxiolysis
MOA: opiate;
; for PSA, combine with sedative agent
Indication: hypoV (less hypotensive than thio/propofol/morphine as no histamine release, good in trauma);
pain (eg. fractures, burns); good in renal failure
Onset: <1 min
Peak: 2-5min
Offset: 30-60min; tissue uptake and redistribution responsible for termination of effect
Dose: Induction: 2-10mcg/kg
Analgesia/PSA: 1-2mcg/kg
SE: chest wall rigidity (>5mcg/kg, not reversible with naloxone); hypotension (when BP maintained by
sympathetic tone); bradycardia; resp depression (outlasts analgesia); N+V; facial pruritis
Cons: more expensive than morphine
MOA: semi-synthetic opioid; may provide satisfactory intubating conditions with propofol, without
paralysis; no amnesia, no anxiolysis
Indication: hypoV, pain
Onset: 30-180secs
Offset: 3-10mins (ultra-short acting)
Metabolism: tissue and blood esterases
Dose: 0.5mcg/kg; no dose modification in organ failures
SE: muscle rigidity, resp depression
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