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Primary FRCA > Drug profiles > Flashcards

Drug profiles Flashcards

1
Q

Propofol

A
  • 2,6 diisopropylphenol
  • 1%/2%; lipid emulsion (soy bean oil, egg phosphatide), pH 7.0; 20/50/100ml vials
  • Weak acid pKa 11
  • Physically incompatible with atracurium
  • Used for induction/maintenance; sedation; status, N+V
  • Dose 1.5-3mg/kg bolus; 4-12mg/kg/hour maintenance
  • Dose[P] 2-7mg/kg
  • MOA: Potentiates GABA-A + glycine; may reduce Na channel opening times; D2 antagonist
  • CVS: ↓SVR ↓SV ↓CO (20%) ↓BP (15-25%) ↓HR ↑DCCV energy
  • RS: Apnoea (bolus), ↓VT ↑RR ↓reflexes ↓chemoreceptor response, bronchodilatation
  • CNS: Hypnosis (1ABCT) ↓CMRO2 ↓ICP/CBF, myoclonus, reduces length of seizures ↓IOP
  • GI: Antiemetic (D2 antagonism)
  • Toxicity: Lipaemia -> Propofol infusion syndrome (rhabdo/hepatic failure/acidosis/bradycardia)
  • Issues: Pain on injection; green urine/hair
  • D: 98% PPB; VD 4L/kg; rapid tissue distribution
  • M: Liver to inactive glucuronide (ok in failure); likely extrahepatic also
  • E: Renal (ok in failure); T1/2 1-5h (CS)
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2
Q

Thiopentone

A
  • Thiobarbiturate
  • Yellow powder sodium salt + 6% sodium carbonate under N2; 500mg vial; reconstituted to 25mg/ml with water pH 10.8 - stable for days
  • Weak acid pKa 7.6; v. lipid soluble
  • Displays tautomerism - water soluble enol form favoured in high pH
  • Used for induction; status and brain protection in ↑ICP
  • Dose: 3-7mg/kg bolus IV; 1g/22kg weight PR
  • MOA: Potentiates GABA-A + glycine; membrane stabilising effect (Na + K channels)
  • CVS: ↓CO (20%) ↓BP ↓SVR, may ↑HR
  • RS: Apnoea ↓VT ↓chemoreceptor response, laryngospasm/bronchoconstriction
  • CNS: Hypnosis (1ABCT), ↓CMRO2 ↓ICP/CBF ↓IOP
  • Renal: ↑ADH (+↓CO) -> ↓UO
  • Toxicity: Anaphylaxis 1:20000
  • Issues: Porphyria; extravasation
  • A: Absorbed PO/PR
  • D: 80% PPB; VD 2L/kg; rapid distribution; displaced by NSAIDs; free drug ↑↑in critically ill
  • M: Liver. Oxidised by CYP450 -> pentobarb and inactive metabolites; INDUCER; Zero-order kinetics with infusion
  • E: Urine, T1/2 4-22h (CS)
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3
Q

Etomidate

A
  • Carboxylated imidazole derivative
  • 2mg/ml, clear, colourless solution of enantiopure R(+)etomidate (10xeffect vs S(-)) with 35% propylene glycol, pH 8.1 or lipuro emulsion (faster onset)
  • Weak base, pKa 4.1
  • Used for induction; Rx of Cushing’s before surgery
  • Dose(A) 0.3mg/kg IV
  • MOA: Potentiation of GABA-A
  • CVS: Most cardiostable, mild ↓SVR but no effect on BP
  • RS: Apnoea with bolus, ↓RR + VT, cough, hiccup, laryngospasm reported
  • CNS: Hypnosis, involuntary movements, tremor, ↓CMRO2 ↓ICP/CBF ↓IOP
  • GI: PONV (40% if opiates also)
  • Endo: Inhibits 11β-hydroxylase and 17α-hydroxylase -> ↓cortisol ↓aldosterone for 24-48h
  • Haem: Antiplatelet effect -> ↑bleeding time
  • Toxicity: ↑mortality with infusions on ITU, anaesthetic doses ok unless risk of adrenal insufficiency
  • Issues: Pain on injection, thrombophlebitis, rare histamine release, porphyria
  • D: 75% PPB, VD 4L/kg, rapid distribution
  • M: Hepatic/plasma esterases to inactive metabolites
  • E: Renal (80%) + bile (20%); T1/2 1-4h (doubled in liver failure)
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4
Q

Ketamine

A
  • Phencyclidine derivative
  • Colourless solution 10/50/100mg/ml racemic ketamine hydrochloride pH approx 4.5. Also available as S(+)ketamine in 5/25mg/ml solutions. Both contain benzethonium chloride.
  • Weak base, pKa 7.5
  • Used for induction (esp. hypotension/asthma); pre-hospital anaesthesia; maintenance; acute analgesia in hospital setting; chronic pain; sole agent for short, painful procedures and treatment of refractory asthma
  • Dose (induct): 0.5-2mg/kg IV (over 60secs); 4-10mg/kg IM
  • Dose (maint): 0.6-3mg/kg/h (GA); 0.3-1.2mg/kg/h (sed)
  • Dose (sed): 0.2-0.75mg/kg IV; 2-4mg/kg IM
  • Onset/Dur: 30s IV; 2-8min IM / 5-10min IV; 10-20min IM
  • May also be given PO, PR, nasally, IT, Epid
  • MOA: Non-competitive NMDA antagonist; inhibits presynaptic glutamate release; weak interaction with MOP, KOP and DOP; ACh antagonist; inhibits monoamine reuptake (NA, D, 5-HT); Na channel inhibition (LA activity at high dose)
  • CVS: ↑HR ↑BP ↑CVP ↑CO (↑sympathetic drive), masks direct myocardial depressant effect (↓with S(+))
  • RS: ↑RR, reflexes preserved, bronchodilatation (R(-) > S(+))
  • CNS: Analgesia, dissociative anaesthesia, ↑ICP/CBF ↑CMRO2 ↑IOP, mydriasis/nystagmus/hypertonus, altered EEG (+BIS); emergence phenomena/hallucinations (↓with S(+) or BDZ)
  • GI: Hypersalivation, PONV
  • GU: Uterotonic, detrusor dysfunction in chronic abuse
  • Immune: Reduced WBC function in sepsis; suppresses inflammatory response
  • Issues: Pain on injection, drug of abuse
  • A: BA 20-25% (PO) 25-50% (nasal) 93% (IM)
  • D: 35% PPB, VD 3L/kg
  • M: Liver CYP450, norketamine (30% potent) -> glucuronidated
  • E: Renal. T1/2 2.5h
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5
Q

Nitrous Oxide

A
  • N2O
  • Produced by heating ammonium nitrate to 250degC; NH4NO3 -> N2O + H2O then purified
  • Stored in French Blue cylinders as liquid below critical temperature; 44bar at 15degC; filling ratio 0.75 temperate, 0.67 tropical.
  • Or as Entonox as 50:50 mix with O2 (O2 bubbled through N2O) which is a gas above pseudocritical temperature of -7degC (Poynting effect). Stored in French Blue with Blue/white shoulders at 137bar. Lamination below -7degC -> risk of hypoxic mix delivery
  • BP -88degC; CT 36.5degC; CP 72bar; B:G 0.47; O:G 1.4; MAC 105%
  • Used as adjuvant to GA; analgesia; refrigerant for cryosurgery
  • Dose: Typically 70% N2O in O2 for adjuvant to GA
  • Exhibits concentration and second gas effect due to 30x solubility vs N2
  • MOA: non-competitive NMDA antagonism; K2P enhancement -> hyperpolarisation; supraspinal opioid+GABA effect in PAG
  • CVS: ↓SV ↑SVR, BP stable but SV drops further in combination with opioid, or volatile/IV agents
  • RS: ↓VT ↑RR ↓MV, diffusion hypoxia (Fink effect)
  • CNS: Analgesia + anaesthesia (LOC >80%), MAC-sparing (additive), ↑ICP, neuromuscular problems with chronic use (confusion, paraesthesia, ataxia, weakness, spasticity), SCDC
  • GI: N&V/PONV
  • Haem: Oxidation of B12 -> megaloblastic anaemia + pancytopaenia with prolonged use
  • Safety: Max environmental exposure 100ppm (UK); Possible teratogen; Store Entonox on side; CI in PTX/ENT Sx/Prolonged ETT Sx
  • A: Freely diffuses across alv-cap membrane
  • M: Negligible metabolism
  • E: Lungs and skin
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6
Q

Isoflurane

A
  • Halogenated methyl ethyl ether
  • [draw]
  • MW 184; BP 48; SVP(20) 33kPa; B:G 1.4; O:G 98; MAC 1.15
  • Structural isomer of enflurane
  • MOA: Potentiation at GABAA + glycine; K2P enhancement; NMDA inhibition
  • CVS: ↓SVR ↓BP, HR unaffected ↓SV (dose related). Historic concern re ‘coronary steal’
  • RS: ↓VT ↓MV, reduced chemoreceptor response, ↓HPV, bronchodilatation, irritant
  • CNS: Hypnosis, ↓CMRO2 ↑CBF/ICP (dose related)
  • GI: PONV
  • GU: Uterine relaxant (esp >1.4 MAC)
  • Issues: MH trigger
  • A: Slow to equilibrate
  • M: 0.2% by liver -> TFAA and fluoride ions
  • E: Lung. Metabolites in urine
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7
Q

Sevoflurane

A
  • Polyfluorinated isopropyl methyl ether
  • [draw]
  • MW 200; BP 58; SVP(20) 23kPa; B:G 0.65; O:G 50; MAC 2.0
  • MOA: Potentiation at GABAA + glycine; K2P enhancement; NMDA inhibition
  • CVS: (dose related) ↓SVR ↓BP, can↓HR ↓SV, may prolong QT
  • RS: ↓VT ↑RR ↓MV, reduced chemoreceptor response, ↓HPV, non-irritant
  • CNS: Hypnosis, ↓CMRO2 ↑CBF/ICP (dose related)
  • GI: PONV
  • GU: Uterine relaxant (esp >1.4 MAC)
  • Issues: MH trigger; rapid emergence in children -> agitation; Down’s Syndrome -> bradycardia; Compounds A-E from reaction with soda lime (A = nephrotoxic but probably not at clinical concentrations)
  • A: Intermediate equilibration time (vs. iso + des)
  • M: 2-5% by liver CYP2E1 (induced by chronic EtOH) -> fluorides
  • E: Lung. Metabolites in urine
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8
Q

Desflurane

A
  • Fluorinated methyl ethyl ether
  • [draw]
  • MW 168; BP 23; SVP(20) 89kPa; B:G 0.4; O:G 26; MAC 6.0
  • MOA: Potentiation at GABAA + glycine; K2P enhancement; NMDA inhibition
  • CVS: (dose related) ↓SVR ↓BP, can↑HR ↓SV
  • RS: ↓VT ↑RR ↓MV, reduced chemoreceptor response, v irritant, not bronchodilator
  • CNS: Hypnosis, ↓CMRO2 ↑CBF/ICP (dose related), potentiation of NMB
  • GI: PONV
  • GU: Uterine relaxant (esp >1.4 MAC)
  • Issues: MH trigger; ++airway irritation in children; specific vaporiser
  • A: Fastest equilibration time (vs. iso + sevo)
  • M: 0.02% by liver -> TFAA
  • E: Lung. Trace metabolites in urine
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9
Q

Halothane

A
  • Halogenated alkane
  • [draw]
  • MW 197; B:G 2.3; O:G 224; MAC 0.75
  • MOA: Potentiation at GABAA + glycine; K2P enhancement; NMDA inhibition
  • CVS: (dose related) ↓SVR ↓BP, ↓HR ↓SV, myocardial sensitisation -> arrhythmia
  • RS: ↓VT ↓RR ↓MV, reduced chemoreceptor response, bronchodilatation, non-irritant
  • CNS: Hypnosis, ↓CMRO2 ↑↑CBF/ICP
  • GI: PONV, ↓motility, Halothane Hepatitis (hypoxic injury and autoimmune stimulation)
  • GU: ↓GFR, Uterine relaxant (esp >1.4 MAC)
  • Issues: MH trigger; Shivering post-op
  • A: Slowest equilibration time of volatiles
  • M: 20% by liver -> TFAA + halides
  • E: Lung. Metabolites in urine
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10
Q

Enflurane

A
  • Halogenated methyl ethyl ether
  • [draw]
  • MW 184; B:G 1.8; O:G 98; MAC 1.68
  • MOA: Potentiation at GABAA + glycine; K2P enhancement; NMDA inhibition
  • CVS: (dose related) ↓SVR ↓BP, ↓HR ↓SV, myocardial sensitisation -> arrhythmia
  • RS: ↓VT ↑RR ↓MV, reduced chemoreceptor response, bronchodilatation, irritant
  • CNS: Hypnosis, ↓CMRO2 ↑↑CBF/ICP, EPILEPTIFORM ACTIVITY, MUSCLE RELAXATION
  • GI: PONV
  • GU: Uterine relaxant (esp >1.4 MAC)
  • Issues: MH trigger; Shivering post-op
  • A: Slower onset than Iso
  • M: 2% by liver -> Fluorides
  • E: Lung, skin, sweat. Metabolites in urine
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11
Q

Suxamethonium

A
  • Succinylcholine (dicholine ester of succinic acid)
  • Two acetylcholine molecules joined at acetyl end
  • Depolarising neuromuscular blocker
  • Clear, colourless solution containing sux chloride; pH 4; 50mg/ml; 2ml ampoules; store at 4degC
  • Used for fast onset muscle relaxation eg. for RSI
  • Dose: 1-2mg/kg IV; up to 2.5mg/kg IM [TBW]
  • Onset/duration: 30s/3-5 mins
  • MOA: Competitive agonist at α-subunit of nAChR. Not degraded by AChE -> Prolonged depolarisation of skeletal muscle fibres preventing further action potentials. Also has an effect on prejunctional AChRs (incompletely characterised). Also weak agonist at mAChRs (hence SEs)
  • CVS: ↓HR and ↑BP, ventricular arrhythmias (esp. with repeated doses)
  • RS: Apnoea due to paralysis
  • NS: Fasciculations then Phase I (depolarising) NMB [prejunctional ↑ ACh release] (Sustained tetany, absence of post-tetanic facilitation, TOFR >0.7, potentiation by anticholinesterases [plasma cholinesterase also inhibited]), Phase II block with repeated administration [upregulation of Na/kATPase] (Poorly sustained tetany, post-tetanic facilitation, TOFR <0.3, reversal by anticholinesterases, tachyphylaxis), ↑IOP ↑ICP/CBF
  • GI: ↑Intragastric pressure with concomitant ↑LOS pressure
  • Issues: MH trigger; Anaphylaxis risk (11 per 100k); Sux apnoea; Myalgia (esp young, fit ambulant); Hyperkalaemia (esp burns in last 2y and neuromuscular disorders [extrajunctional AChRs release K+ into circulation])
  • D: Rapid redistribution and metabolism in plasma (20% reaches NMJ)
  • M: Plasma cholinesterase -> succinylmonocholine (weakly active) + choline; then to succinic acid and choline (inactive)
  • E: Urine, 5% unchanged. T1/2 3 mins
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12
Q

Atracurium

A
  • Benzylisoquinolinium non-depolarising muscle relaxant
  • Clear, colourless solution; 10mg/ml of atracurium besilate; 2.5/5/25ml ampoules; Stored at 4degC to avoid Hofmann degradation; pH 3.5
  • 4 chiral centres -> 10 stereoisomers! Available in mixed stereoisomer form (above) or as enantiopure cisatracurium 2mg/ml (dose 0.15mg/ml) - less histamine release; 80% Hofmann
  • Used as muscle relaxant for intubation/surgery
  • Dose: 0.5mg/kg (IBW)
  • Onset/duration: 1.5-2mins intubating conditions, maximal 3-5 mins / 15-35 mins
  • MOA: Competitive non-depolarising antagonism at α-subunit of nAChR; prejunctional block -> fade on TOF
  • CVS: Minimal ↓HR/SVR/BP (histamine related)
  • RS: Apnoea, Histamine -> bronchospasm (0.2%)
  • NS: Non-depolarising NMB (Tetanic fade, TOFR <0.3, Post-tetanic potentiation), no effect on IOP/ICP, Critical illness neuropathy with prolonged infusions
  • GI: Unaffected
  • Issues: Anaphylaxis (4 per 100k)
  • D: VD 0.15 L/kg
  • M: 2 pathways - Ester hydrolysis by non-specific esterases (60%) and Hofmann degradation (40%) both to laudanosine and other inactive metabolites (high laudanosine concs. cause seiures but not at clinical levels)
  • E: T1/2 20mins; independent of liver/renal Fn
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13
Q

Mivacurium

A

-Benzylisoquinolinium non-depolarising muscle relaxant
-Clear, colourless solution; 2mg/ml mivacurium hydrochloride; 5/10ml amps; Stored at RT; pH 4.5
-Mixture of three stereoisomers (trans-trans[58%]/cis-trans[36%]/cis-cis[6% - only 10% potent])
-Used as muscle relaxant for intubation/surgery, short duration
-Dose: 0.2mg/kg (IBW), give over 30s
-Onset/duration: 2-3mins intubating conditions / 20 mins
-MOA: Competitive non-depolarising antagonism at α-subunit of nAChR; prejunctional block -> fade on TOF
-CVS: Minimal ↑HR ↓SVR/BP (histamine related)
-RS: Apnoea, Histamine -> bronchospasm
-Skin: Histamine -> Rash/erythema
-Issues: Anaphylaxis (3 per 100k)
D: VD 0.25L/kg
M: Hydrolysis by plasma cholinesterases to inactive metabolites (except cis-cis) - effects prolonged by abnormal plasma cholinesterase (sux apnoea)
E: Urine and bile. Effects prolonged by hepatic/renal failure; T1/2 2 mins

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14
Q

Rocuronium

A
  • Aminosteroid non-depolarising muscle relaxant
  • Monoquaternary amine drug
  • Clear, colourless liquid; 10mg/ml Rocuronium Bromide; 5ml amps; stored at 4degC
  • Used for intubation/RSI/Surgical relaxation
  • Dose: 0.6mg/kg; 1mg/kg RSI [IBW]
  • Onset/duration: 2 mins (1min RSI) / 20-60mins
  • MOA: Competitive non-depolarising antagonism at α-subunit of nAChR; prejunctional block -> fade on TOF
  • CVS: ↑HR with high dose
  • RS: Apnoea
  • NS: Skeletal muscle relaxation
  • Issues: Pain on injection; Anaphylaxis (6 per 100k); Reversal with sugammadex
  • D: VD 0.2L/kg
  • M: Mainly unchanged, some hepatic deacetylation
  • E: Bile 60%, Urine 40%, effect prolonged in renal/hepatic dysfunction
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15
Q

Vecuronium

A
  • Aminosteroid non-depolarising muscle relaxant
  • Monoquaternary amine drug
  • White lyophilised powder in 10mg vial; reconstituted with 5ml water to 2mg/ml vecuronium bromide + sodium salts + mannitol; pH 4
  • Used for intubation/surgical conditions
  • Dose: 0.1mg/kg [IBW]
  • Onset/duration: 1.5-2mins / 45 mins
  • MOA: Competitive non-depolarising antagonism at α-subunit of nAChR; prejunctional block -> fade on TOF
  • CVS: Cardiostable
  • RS: Apnoea
  • NS: Skeletal muscle relaxation. Critical illness myopathy with prolonged administration
  • Issues: Possible ↑PT/APTT
  • D: VD 0.2L/kg
  • M: Hepatic deacetylation to active metabolites 3-, 17- and 3,17-dihydroxyvecuronium, only relevant in prolonged dosing
  • E: Bile 70%, Urine 30% (unchanged), T1/2 60 mins
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16
Q

Pancuronium

A
  • Aminosteroid non-depolarising muscle relaxant
  • Clear, colourless solution 2mg/ml pancuronium bromide; 2ml amps; stored at 4degC
  • Bis-quaternary amine drug
  • Used for intubation/surgical conditions; lethal injection in US; long-acting
  • Dose: 0.1mg/kg [IBW]
  • Onset/duration: 1.5-2mins / 90mins
  • MOA: Competitive non-depolarising antagonism at α-subunit of nAChR; prejunctional block -> fade on TOF
  • CVS: Vagolytic + blocks NA reuptake -> ↑HR ↑CO ↑BP
  • RS: Apnoea
  • NS: Prolonged muscle relaxation
  • Issues: Sweating/flushing
  • D: up to 40% PPB; VD 0.25L/kg
  • M: Hepatic -> 3-, 17- and 3,17-hydroxypancuronium (3- has 50% potency)
  • E: Bile 50%, Urine 50% (unchanged), T1/2 120mins, prolonged in hepatic and renal failure
17
Q

Neostigmine

A
  • Quaternary amine anticholinesterase
  • Medium duration of action (1-2h)
  • 15mg tablets or SFI 2.5mg/ml and combination with glyco (0.5mg/ml)
  • Used for reversal of non-depolarising NMB; Rx of myasthenia gravis and paralytic ileus
  • Dose: 0.05mg/kg for reversal (1ml dose for 50kg adult); 15-30mg 4 hourly in MG
  • Onset/duration(IV): Peak at 8-10mins / 1-2h
  • MOA: Reversible binding to esteratic site of AChE, carbamylates the enzyme, slowing hydrolysis -> reduces ACh breakdown -> ↑synaptic conc. -> competes with NMBs. Also inhibits plasma cholinesterase.
  • CVS: ↓HR ↓BP (muscarinic)
  • RS: Bronchoconstriction, ↑secretions
  • NS: Miosis, blurred vision, muscle spasm (low dose), neuromuscular blockade (high dose -> receptor flooding)
  • GI: ↑secretions + motility, N+V
  • Skin: Sweating
  • GU: Involuntary urination
  • Issues: Usually given with antimuscarinic
  • A: 1-2% BA PO
  • D: 10% PPB; VD <1L/kg
  • M: Plasma esterases to inactive alcohol, minor hepatic metabolism
  • E: Urine 60%, bile 40%, T1/2 60 mins
18
Q

Edrophonium

A
  • Quaternary amine anticholinesterase
  • Clear, colourless SFI, 10mg/ml
  • Used for reversal of NMB; diagnosis of myasthenia gravis (Tensilon test); differentiation of myasthenic and cholinergic crises
  • Dose: 0.6mg/kg (reversal) ; 2mg then 8mg for MG Dx; 2mg for test in crisis (atropine available)
  • Onset/duration: 1 min / 10 mins
  • MOA: Binds to both anionic and esteratic AChE sites, competitively inhibiting the enzyme’s activity on ACh -> ↑synaptic conc. -> competes with NMBs
  • CVS: ↓HR ↓BP (muscarinic)
  • RS: Bronchoconstriction, ↑secretions
  • NS: Miosis, blurred vision, muscle spasm (low dose), neuromuscular blockade (high dose -> receptor flooding)
  • GI: ↑secretions + motility, N+V
  • Skin: Sweating
  • GU: Involuntary urination
  • Issues: Usually given with antimuscarinic
  • D: VD 1L/kg
  • M: Some hepatic glucuronidation
  • E: Urine 60%, bile 40%, T1/2 110 mins
19
Q

Organophosphates

A
  • Class of compounds with varied characteristics
  • eg. malathion/parathion/TEPP (pesticides), Sarin (nerve agent), echothiophate (Glaucoma Rx)
  • Irreversible binding to AChE at esteratic site -> inactivation; also inhibit plasma cholinesterase
  • Highly lipid-soluble -> absorbed through skin
  • Cause muscle contraction/spasm -> apnoea, muscarinic SEs (autonomic instability, D+V, bronchoconstriction + secretions) and central excitation -> depression -> coma
  • Treatment is supportive, ↑↑dose atropine and AChE reactivator PRALIDOXIME/OBIDOXIME [hydrolyse phosphorylated enzyme]
20
Q

Sugammadex

A
  • Gamma cyclodextrin
  • Clear, colourless solution 100mg/ml; 2/5ml amps
  • Used to reverse Rocuronium and Vecuronium
  • Dose: 16mg/kg (intubating dose); 4mg/kg (deep block - post-tetanic count 1-2); 2mg/kg (moderate block - >1 twtich on TOF). Works in seconds
  • MOA: Ring structure is hydrophilic on outside and lipophilic on inside, encapsulates Roc/Vec within lipophilic centre, preventing drug effect and facilitating urinary excretion. Creates gradient drawing drug out of NMJ.
  • Issues: Significant anaphylaxis unlikely; reduces effectiveness of OCP (1 missed day) and parenteral hormonal contraceptives (alt. contraception for 1/52); Very rarely bradycardia
  • VD 12L; linear kinetics; not metabolised; renal excretion, T1/2 2.5h
21
Q

Atropine

A
  • Tertiary amine antimuscarinic
  • Named after Atropos - Greek fate
  • Naturally occurs eg. in Atropa belladonna (deadly nightshade)
  • Commercially synthetic - racemic mixture of D/L-hyoscyamine (only L active)
  • Clear, colourless solution 0.6mg/ml atropine sulfate; also 600mcg tablets for premed
  • Used for premed (secretions); Rx of bradycardia, muscarinic SEs, organophosphate poisoning and tetanus
  • Dose(A): 0.2-0.6mg IV
  • Dose(P): 20mcg/kg
  • MOA: Competitive antagonism at mAChR; some nAChR effect at high dose; crosses BBB
  • CVS: ↑HR, precipitates arrhythmias
  • RS: ↑RR, bronchodilatation, ↓ secretions
  • NS: Antiemetic, antiparkinsonian, central anticholinergic Sx (confusion, somnolence, hallucinations, agitation, amnesia, ataxia)
  • GI: ↓salivation ↓motility, antispasmodic ↓LOS tone
  • GU: Urinary retention
  • Issues: Pain on IM injection; ↓sweating + hyperpyrexia in children
  • A: Well absorbed, 20% BA PO
  • D: 50% PPB, VD 3L/kg; crosses placenta
  • M: Hepatic -> inactive metabolites
  • E: Urine, some unchanged, T1/2 2.5h
22
Q

Glycopyrronium

A
  • Synthetic quaternary amine antimuscarinic
  • Clear, colourless solution 0.2mg/ml; 3ml amps; also in combination with neostigmine (0.5mg glyco + 2.5mg neo/ml)
  • Used for premed (secretions); mitigation of anticholinesterase SEs; Rx of bradycardia, hyperhidrosis and symptom control at end of life
  • Dose(A): 0.2-0.4mg IV/IM
  • Dose(P): 4-10mcg/kg
  • Peak effect at 3 mins, 2-3h duration
  • MOA: Competitive antagonism at peripheral mAChR; does not cross BBB
  • CVS: ↑HR, less arrhythmogenic than atropine
  • RR: Significant bronchodilatation -> ↑deadspace
  • NS: Headache, drowsiness, weak LA activity
  • GI: ↓↓salivation (++vs atropine) ↓motility, antispasmodic ↓LOS tone
  • GU: Urinary retention
  • Issues: ↓sweating but no effect on temperature
  • A: 5% BA PO
  • D: VD 0.5L/kg, rapid redistribution
  • M: Minimal
  • E: Urine 85% + bile 15%, T1/2 1h
23
Q

Hyoscine

A
  • Tertiary amine antimuscarinic
  • Naturally occurring alkaloid
  • Clear, colourless solution as hydrobromide (0.4mg/ml) or butylbromide (20mg/ml); butylbromide available as tablet and hydrobromide as a patch (1mg/72h)
  • Racemic mixture, only L-hyoscine active
  • Used for premed (secretions); Rx of N+V/motion sickness; antispasmodic; palliative care
  • Dose: 5-10mcg/kg IV; 10-15mcg/kg IM; 20mg 6 hrly PO
  • MOA: Competitive antagonism at peripheral mAChR; butylbromide does not cross BBB; hydrobromide does cross BBB
  • CVS: Mild ↑HR IV
  • RS: ↑RR ↓↓secretions, bronchodilatation
  • NS: Mydriasis +++, Sedation, amnesia, antanalgesia, central anticholinergic syndrome (confusion, somnolence, hallucinations, agitation, amnesia, ataxia) [reduced with butylbromide]
  • GI: Antiemesis, ↓↓salivation, antispasmodic
  • GU: Urinary retention
  • Issues: ↓sweating
  • A: 10% BA PO
  • D: VD 2L/kg
  • M: Liver esterases -> inactive metabolites
  • E: Urine, T1/2 1h
24
Q

Morphine

A
  • Naturally occurring phenanthrene derivative
  • Strong opiate
  • Wide range of preparations and routes; tabs (SR/MR), syrup, suppos., SFI -clear, colourless 10/15/30mg/ml sulphate; pres-free
  • Weak base; pKa 8.0
  • Used for mod/sev pain; PCA; Premed; Palliative care and Rx of diarrhoea
  • Dose(A): 5-20mg 4hrly po; 25-30mg 4hrly pr; 0.05-0.1mg/kg IV; 0.1-0.2mg/kg sc/im; 0.2-1mg IT; 1-5mg Epi
  • Onset/duration: 10/30mins IV/IM / 3-4h duration
  • MOA: MOP + KOP agonism -> ↑K+ efflux -> hyperpol; ↓AC -> ↓cAMP; ↓VGCC activity; affects cortex, BG, PAG and SC (presynaptic primary afferents)
  • CVS: Histamine -> ↓SVR; OH; ↓HR (high dose)
  • RS: ↓RR ↓chemoreceptor response, antitussive, bronchoconstriction (high dose)
  • NS: Analgesia, sedation, euphoria, hallucinations, meiosis, rigidity + seizures (high dose), ↓MAC/BIS
  • GI: ↓motility -> constipation, ↓secretions, N+V, SoO spasm
  • GUS: ↑ureteric/bladder sphincter tone -> retention
  • Endo: ↑ADH -> ↓Na, ↓adrenal steroids
  • Skin: Itching, sweating
  • Issues: Controlled drug; Caution in liver / renal failure, hypopituitarism and chronic T2RF; Delayed ↓RR with IT/Epi; caution in children/neonates
  • A: BA 20-50% PO (FPM)
  • D: 40% PPB; VD 4L/kg (reduced in elderly -> ↑peakCp); xplacenta
  • M: Hepatic -> M-3- (70%, possible weak agonist), M-6-glucuronide (13x potency) and normorphine (inactive)
  • E: Urine 90%, Bile 10%; T1/2 2-4h
25
Q

Diamorphine

A
  • Synthetic morphine derivative - Diacetylmorphine
  • Strong opioid prodrug
  • Wide range of routes; 10mg tabs; white lyophilised powder diamorph hydrochloride for reconstitution with water/saline, range of strengths
  • Weak base pKa 7.6
  • Used for mod/sev pain; Premed; Palliative care; Dyspnoea associated with acute LVF
  • Dose(A): 5-10mg IV/IM; 0.1-1mg IT; 1-3mg Epi
  • Onset/duration: <10min / 90min
  • MOA: Prodrug -> 6-MAM and morphine are first active metabolites; MOP + (↓)KOP agonism -> ↑K+ efflux -> hyperpol; ↓AC -> ↓cAMP; ↓VGCC activity; affects cortex, BG, PAG and SC (presynaptic primary afferents)
  • CVS: Only with high dose. Histamine -> ↓SVR, OH, ↓HR
  • RS: ↓RR ↓chemoreceptor response, antitussive, bronchoconstriction (high dose)
  • NS: Analgesia, sedation, euphoria++, hallucinations, meiosis, rigidity + seizures (high dose), ↓MAC/BIS
  • GI: Less than morphine. ↓motility -> constipation, ↓secretions, N+V
  • GUS: ↑ureteric/bladder sphincter tone -> retention
  • Endo: ↓stress response to Sx
  • Skin: Itching, sweating
  • Issues: Controlled drug; Caution in chronic T2RF; No delayed ↓RR with IT/Epi
  • A: Low BA (FPM)
  • D: 40% PPB; VD 5L/kg; xplacenta
  • M: Plasma, RBC and tissue esterases -> 6-MAM + morphine. Then hepatic -> M-3- (70%, possible weak agonist), M-6-glucuronide (high potency) and normorphine (inactive)
  • E: Urine, 60% as morphine metabolites. Diamorph T1/2 3 mins
26
Q

Alfentanil

A
  • Synthetic phenylpiperidine derivative
  • Strong opioid
  • Clear, colourless solution alf hydrochloride; 0.5/5mg/ml
  • Weak base; pKa 6.5
  • Used for short acting analgesia; obtunding airway reflexes and sedation on ITU
  • Dose(A): 5-50mcg/kg bolus; 30-60mcg/kg/h IVI
  • Onset/duration: 90 sec / 5-10 mins; exhibits CSHT
  • MOA: Highly selective MOP agonist -> ↑K+ efflux -> hyperpol; ↓AC -> ↓cAMP; ↓VGCC activity; affects cortex, BG, PAG and SC (presynaptic primary afferents)
  • CVS: sympatholytic ↓HR -> ↓response to laryngoscopy, BP stable
  • RS: ↓RR, ↓chemoreceptor response, antitussive
  • NS: Analgesia, meiosis, minimal sedation, ↓IOP, ↓MAC/BIS
  • GI: ↓motility -> constipation, ↓secretions, N+V, SoO spasm
  • GUS: ↑ureteric/bladder sphincter tone -> retention
  • Endo: ↓stress response to Sx
  • Issues: Controlled drug; caution in liver/renal failure
  • D: 90% PPB; VD 0.6L/kg
  • M: Hepatic CYP3A4 -> noralfentanil (inactive), competition for 3A4 by midazolam -> ↓metabolism
  • E: Urine, T1/2 90 mins
27
Q

Fentanyl

A
  • Synthetic phenylpiperidine derivative
  • Strong opioid
  • Lozenges, patches (range of strengths); Clear, colourless solution fentanyl citrate; 50mcg/ml
  • Weak base; pKa 8.4
  • Used for mod/sev pain; PCA; chronic pain; palliative care; obtunding airway reflexes and sedation on ITU
  • Dose(A): 1-100mcg co-induction IV; 50-100mcg premed IV; 1mcg/kg bolus for pain; 10-30mcg IT; 25-100mcg Epi; 2-4mcg/kg/h IVI
  • Onset/duration: 2-5 min / 30mins - 6h (CSHT)
  • MOA: Highly selective MOP agonist -> ↑K+ efflux -> hyperpol; ↓AC -> ↓cAMP; ↓VGCC activity; affects cortex, BG, PAG and SC (presynaptic primary afferents)
  • CVS: sympatholytic ↓HR -> ↓response to laryngoscopy, BP stable
  • RS: ↓RR, ↓chemoreceptor response, antitussive, ‘wooden chest’ with high doses
  • NS: Analgesia, meiosis, minimal sedation, ↓MAC/BIS
  • GI: ↓motility -> constipation, ↓secretions, N+V
  • GUS: ↑ureteric/bladder sphincter tone -> retention
  • Endo: ↓stress response to Sx
  • Issues: Controlled drug; No delayed resp depression with IT
  • A: 33% BA PO
  • D: 90% PPB; VD 4L/kg
  • M: Hepatic CYP3A4 -> norfentanyl and further metabolites (inactive),
  • E: Urine 90%, Bile 10%; T1/2 3h+ (CSHT)
28
Q

Remifentanil

A
  • Synthetic phenylpiperidine derivative
  • Strong opioid
  • White lyophilised powder, containing glycine buffer, in 1/2/5mg vials for reconstitution with saline, typically to 50mcg/ml for infusion
  • Used for analgesia and induction of hypotension during GA; sedation on ITU and during awake airway procedures
  • Dose: 1mcg/kg slow bolus; 2-60mcg/kg/h IVI
  • Onset/duration: 2 mins / 5-10 mins, context-insensitive
  • MOA: Pure MOP agonist -> ↑K+ efflux -> hyperpol; ↓AC -> ↓cAMP; ↓VGCC activity; affects cortex, BG, PAG and SC (presynaptic primary afferents)
  • CVS: sympatholytic ↓HR/SV/BP (20%), ↓response to airway manipulation
  • RS: ↓RR, ↓chemoreceptor response, antitussive, ‘wooden chest’ with high doses
  • NS: Analgesia, meiosis, minimal sedation, ↓MAC/BIS
  • GI/GU: Reduced compared to morphine/fent
  • Endo: ↓stress response to Sx
  • Issues: Controlled drug; Profound ↓HR with rapid boluses
  • D: 70% PPB; VD 0.1L/kg
  • M: Plasma/tissue esterases -> inactive carboxylic acid derivatives
  • E: Urine; T1/2 90mins
29
Q

Pethidine

A
  • Synthetic phenylpiperidine derivative
  • Originally designed as an anticholinergic
  • Strong opioid
  • Tabs (50mg); clear, colourless solution for injection (10/50mg/ml)
  • Weak base, pKa 8.7
  • Used for labour analgesia; antispasmodic in colic; Rx of post-operative shivering
  • Dose: 50-150mg 4hrly PO; 25-100mg 4hrly IV/IM
  • MOA: MOP + KOP agonism -> ↑K+ efflux -> hyperpol; ↓AC -> ↓cAMP; ↓VGCC activity; affects cortex, BG, PAG and SC (presynaptic primary afferents); Anticholinergic effect; SSRI effect
  • CVS: ↑HR (anticholinergic), OH (opioid)
  • RS: ↓RR ↓VT ↓chemoreceptor response
  • NS: Analgesia, mydriasis (anticholinergic), euphoria+
  • GI: N+V, constipation (supposedly less than morphine)
  • GU: Urinary retention, uterotonic
  • Endo: ↑ADH -> ↓Na, ↓adrenal steroids
  • Issues: Crosses placenta -> fetal norpethidine accumulation (active metabolite + proconvulsant); Interaction with MAOIs -> hypertension, seizures, hyperpyrexia; caution in renal failure
  • A: 50% BA PO
  • D: 60% PPB; VD 4.5L/kg; xPlacenta
  • M: Hepatic demethylation -> norpethidine (50% potency, proconvulsant) -> pethidinic acid
  • E: Renal, T1/2 3h+

Primary FRCA (34 decks)

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