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Drug Summaries
Drug Summaries
Drug Summaries
Induction Agents
BAA
GA
l i sm
Propofol b o ↓SVR | ↓Contractility | ↓MAP | +/- ↑ HR
a
et
Weak acid M
lipid emulsion
Excretion
pKa 11 ↓CBF | ↓CMRO | ↓ICP | Excitation
IV Maintenance : 4-12mg/kg/hr
VD 4L/kg
Antiemetic
IV Sedation : 0.3-4mg/kg/hr Cl 30-60ml/kg/min
A A
GAB
pKa 7.6
25mg/ml Reduced Splanchnic/Renal bloodflow
VD 2.5L/kg
Cl 3ml/kg/min Porphyria
BAA
GA
s e Stable | +/- ↓MAP
e ra sm
Etomidate s t ol i
E ab
Weak base et Transient Apnoea | ↓VT with ↑RR
M
IV Induction: 0.3mg/kg Imidazole pH 8.1 ↓CBF | ↓CMRO | Epileptiform EEG
Excretion
DA
N M
sm
Ketamine bo
l i ↑HR | ↑C.O. | ↑CVP | ↑MAP
t a
e
Weak base M
Phencyclidine
↑RR | Bronchodilation
IV Induction: 1-2mg/kg
Derivative
pH 3.5-4.5
↑CBF | ↑CMRO | Emergence phenomena
Excretion
Summary Sheet:
Volatile Anaesthetics
MAC
O
↑ HR ↓ BP ↓ SVR ↓ Contractility
1.1 Potent
1.4
MAC
O
↓ BP ↓ SVR ↓ Contractility
2.0 2%
Potent
Flourides
Sevoflurane Oil:Gas ↑ RR ↓ VT Bronchodilation
Cheap
53 ↓ CMRO
Rapid
onset/offset
Blood:Gas
↓ Uterine tone Compounds
A-E
0.7
O
MAC
19 Minimally
↑ CBF ↓ CMRO
metabolised
Blood:Gas Carbon
↓ Uterine tone
Monoxide
Tec 6 Vapouriser
0.4
Minimum Alveolar Concentration: the concentration of inhalation anaesthetic at 1ATM & FiO2
100% at which 50% of subjects will fail to respond to a standard surgical stimulus.
↑ Unionised fraction μ1 Receptors
= Fast onset
Analgesia & Euphoria
Miosis
Duration of action
determined by:
Distribution
Summary Sheet: μ2 Receptors
↓ HR
Opioids
(e.g. Fentanyl short due to ↑ VD)
Respiratory Depression
Elimination
(e.g. Remifentanil short due to
rapid ester hydrolysis) ↓ Gut Motility
μ
Induction
analgesia
Fentanyl
pKa 8.4 Fast-acting
Norfentanyl
Unionised at pH 7.4: 9%
50mcg/ml
Short-
Excretion
VD 4L/kg acting
10mcg 1mg
Fent Morph Cl 13ml/kg/min
Renal failure
Terminal t½: 190mins PCAs
Alfentanil Induction
analgesia
pKa 6.5 Inactive
metabolites Ultrafast-
Unionised at pH 7.4: 90%
acting
500mcg/ml
Excretion
VD 0.4-1.0L/kg
100mcg 1mg Ultrashort-
Alf Morph Cl 6ml/kg/min
acting
Terminal t½: 100mins
μ IV Infusion
analgesia
Remifentanil AFOIs /
pKa 7.1 extubation
1mcg / Unionised at pH 7.4: 70% Esterase Ultrafast-
2mcg / VD 0.2-0.3L/kg Metabolism acting
10mcg 1mg 5mcg
Cl 30-40ml/kg/min
Remi Morph Shortest-
Terminal t½: 3-10mins acting
μ +κ
Phenanthrene
Morphine Intra/Post-op
analgesia
pKa 8.0
Conjugates
Unionised at pH 7.4: 23% Long acting
Excretion
10mg/ml
Aminosteroids
Suxamethonium
Benzylisoquinoliniums
Summary Sheet:
Neuromuscular Blockade
Monoquaternary Aminosteroids
50mg Duration: 20-35 mins 50% Fully
Dose: 0.6mg/kg Reversible
in 5ml Cl: 5ml/kg/min
RSI Dose : 1mg/kg
Elimination: Urine & Bile 50% Medium-
acting
S N
No histamine
Vecuronium Onset: 3-5 mins release
10mg VD 0.2L/kg
Fully
Dose: 0.08mg/kg or Duration: 20-35 mins 60% Reversible
20mg Cl: 5ml/kg/min
powder Medium-
Elimination: Urine & Bile 30% acting
S N
Bezylisoquinolinium
Atracurium Onset: 2 mins
VD 0.16L/kg Safe in Renal
& Liver Failure
Duration: 20-35 mins
Dose: 0.5mg/kg Medium-
10mg/ml
Cl: 5ml/kg/min
acting
Elimination: Esterases & Hoffman Degradation
N
↑ Gastric pressure ↓ HR
↑ LOS tone Short-acting
Irreversible ↑ IOP Myalgia
l o cks nary
B ater s
no qu eroid
Mo inost
Am
Sugammadex ↓ HR
γ-Cyclodextrin ring chelates Rocuronium
& Vecuronium to reverse even profound
Reversal dosing:- neuromuscular block. Prolonged PT & APTT
2ml of
Immediate: 16mg/kg 100 Onset: <3 mins
mg/ml Elimination t½: 2 hours (renal elimination) Reduces Progesterone
PTC of 1-2: 4-8mg/kg
exposure - missed pill rules
ToF 2 twitches: 2mg/kg
Arrhythmias
Flumazenil Competitive inhibitor of benzodiazepines
(& Zopiclone) at the GABAA binding sites.
Dyspnoea | Chest pain
Onset: 1-2 mins
100 mcg/ml
ACh H1
VESTIBULAR +
GI TRACT VOMITING CENTRE CEREBELLAR NUCLEI
ACh 5-HT3 H1
CHEMORECEPTOR
TRIGGER ZONE
D2 5-HT3 μ
-H T 3
5
Synthetic Carbazole
Ondansetron Blocks vagal afferents from GI tract
2mg/ml
H1
Piperazine derivative
Cyclizine Reduces sensitivity of vestibular apparatus
50mg/ml
D2
Phenothiazine neuroleptic
Prochlorperazine Central action at CTZ
12.5mg/ml
Dexamethasone Glucocorticoid
Unclear mechanism for antiemetic effects
Dose: 0.1mg/kg (4-8mg)
Summary Sheet:
Vasopressors
Ohm’s Law as Applied to CVS Optimising Perfusion & C.O.
MAP - CVP = HR × SV × SVRα 1
C.O.
SV
Preload A)erload HR β1
β1 Contractility Preload SV β1
Adrenoceptors
α1 Vasoconstriction
α2 Vasodilatation
SVR α1
β1 Inotropy & Chronotropy
α1
Various presentations - check concentration!
Metaraminol
Onset: 1-2 minutes
Duration: 20+mins (tapers)
Bolus Dose: 500-2000mcg
Direct & Indirect (↑NA release) sympathomimetic effects
IVI Dose: 15-100mg/hr
Predominant α1 activity, some β1 activity
Conc.: 500mcg/ml
↑SVR therefore ↑ BP (± ↓ HR)
+ β
α 1
Bronchoconstriction
h R
m AC
h R
mAC
?
Peak action: 3-4 minutes
Duration: 2-3 hours
Bolus Dose: 200mcg
Does not cross blood-brain barrier
Metabolised unknown
Onset Speed
inversely Duration of action
proportional to pKa directly proportional
(i.e. directly to protein-binding
proportional to
unionised fraction)
Summary Sheet:
Local Anaesthetics
Chemistry Mode of Action
Local anaesthetics are all weak bases.
Amide Local Anaesthetics have.a longer
half-life and are metabolised in the liver. B + H+ B H+
Ester Local Anaesthetics are rapidly
inactivated by plasma/liver esterases.
Na+
Extracellular
Toxicity
Intracellular
Paraesthesia | Light-headedness &
Dizziness | Visual/auditory
disturbances | Confusion |
Shivering | Twitching | Seizures B + H+ B H+
pKa: 8.1
Bupivicaine Unionised fraction at pH 7.4: 15% Levobupivicaine
Protein-binding: 95%
Max Dose: 2mg/kg Elimination t½: 160 mins Less motor block & vasodilatation
c ̅ Adrenaline: 2mg/kg More lipid-soluble than Lidocaine 97% Protein-bound
(so 8 × more potent) Lower risk of cardio toxicity
Plasma Composition Maintenance Fluids
Summary Sheet:
Next 2ml/kg =
Cl-: 95-105 mmol/L 10-20kg
IV Fluids
Ca2+: 2.2-2.6 mmol/L >20kg 1ml/kg =
Glucose: 3.5-5.5 mmol/L
Bicarbonate: 24-32 mmol/L Hourly requirements =
Transcellular
1%
7% 9%
Plasma 18% 18%
7%
25%
42%
Interstitial
25% ⅓ 100%
⅔ 82% 82%
67%
Intracellular
67% 48%
Extracellular Fluid
80% Interstitial 20% Plasma
Intracellular Interstitial Plasma
pH 7.4
308mOsm/L
pH 4.5 Crystalloids
pH 4.5 - 7.0 Na+ 140
pH 3.5-5.5 308mOsm/L K+ 5.0
4% 308mOsm/L
278mOsm/L Na+ 31 Cl- 98
5% Glucose Glucose + 0.9% NaCl Na+ 154 Plasmalyte
Gluc 278 0.18% Cl- 31 Acetate 27
Cl- 154
NaCl Gluc 222 Gluconate 23
Mg2+ 1.5