3. Pharmacology
 3.10. Pharmacology tables

Inhalational

Inhalational anaesthetics (compiled from notes)
Blood:gas Oil:gas MAC MAC awake MW Boiling point Vapour pressure
Halothane 2.54 224 0.75% 0.55 MAC 197 50.2C 244 mmHg
Enflurane 1.90 1.63% 184 56.5C 172 mmHg
Isoflurane 1.46 98 1.17% 0.38 MAC 184 48.5C 240 mmHg
Desflurane 0.42 19 6.60% 0.34 MAC 168 22.8C 669 mmHg
Sevoflurane 0.69 47 1.80% 0.34 MAC 200 58.5C 170 mmHg
N2O 0.46 1.4 104% 0.64 MAC 44 -88.5C gas
Xenon 0.115 71% 131 -108C gas
Comment

Hal = most potent

N2O = least

Des = highest

Sev = lowest

IV anaesthetic agents

IV anaesthetic agents (compiled from notes)
Vd PB Clearance Elimination halflife

CSHT

(8 hrs)

pK Acid/base pH Dose
Propofol 3.5 - 4.5 L/kg 98% 30 - 60 mL/kg/min 0.5 - 1 hours <40min 11 Acid

7 - 8.5 (Diprivan)

4.5 - 6.4 (Generic)

1 - 2.5 mg/kg
Thiopentone 2.5 L/kg 80% 3.4 mL/kg/min 11.6 hours 3 hours 7.6 Acid 10.5 3 - 5 mg/kg
Methohexitone 2.2 L/kg 10.9 mL/kg/min 3.9 hours higher than 7.6 Acid
Ketamine 2.5 - 3.5 L/kg 20-50% 16 - 18 mL/kg/min 2 - 3 hours 7.5 3.5 - 5.5 1 - 2 mg/kg IV
Etomidate 2.2 - 4.5 L/kg 76% 10 - 20 mL/kg/min 2 - 5 hours 4.2 Base

6.9 (Propylene glycol)

8.1 (

0.2 - 0.4 mg/kg
Midazolam 1 - 1.5 L/kg 96 - 98% 6 - 8 mL/kg/min 1 - 4 hours 6.15 3.5 0.1 - 0.2 mg/kg

NB:

  • Ketamine dose
    * 1 - 2 mg/kg IV for induction
    * 4 - 8 mg/kg IM for induction
    * 0.2 - 0.5 mg/kg IV for analgesia

Local anaesthetics

Local anaesthetics (compiled from notes)
Potency pK

Nonionised

fraction

at pH 7.4

Lipid solubility Relative lipid solubility Protein-binding Vd (L) Speed of metabolism
(1 is fastest)
Onset Duration Elimination T1/2 Clearance Comment
Ester LA
Procaine 1 8.9

3%

0.6 6% 65 L 2 Slow 45 - 60 min 9 min  
Chloroprocaine 4 8.7 5% 35 L 1 Rapid 30 - 35 min 7 min Rapid onset despite high pK, due to the high concentration used (3%)

Amethocaine

16 8.5 7% 80 76% 3 Slow 60 - 180 min

High potency, slow metabolism

Used topically on eyes

Benzocaine 3.5 Very low pK, almost entirely non-ionised at physiological pH
Cocaine ?8.5
Amide LA
Lignocaine 1 7.9 25% 2.9 1 70% 91 L 2 Rapid 60 - 120 min 1.6 hours 9 mL/kg/min
Etidocaine 4 7.7 33% 141 39 94% 133 L 3 Slow 240 - 480 min 2.6 hours

Prilocaine

1 7.9 24% 0.9 55% 191 L 1 Slow 60 - 120 min 1.6 hours
Pipecoloxylidide
Mepivacaine 1 7.6 39% 0.8 77% 84 L 2 Slow 90 - 180 min 1.9 hours
Bupivacaine 4 8.1 17% 27.5 10 95% 73 L 3 Slow 240 - 480 min 3.5 hours 7 mL/kg/min
Levobupivacaine 4 8.1 17% >97% 55 L Slow 240 - 480 min 2.6 hours
Ropivacaine 4 8.1 17% 2.9 94% 59 L 3 Slow 240 - 480 min 1.8 hours 11 mL/kg/min

  • Relative lipid solubility is based on relative heptane:buffer partition coefficient

Opioid agonists

Opioids

Potency

(IV, appr)

Vd PB

Lipid

solubility 

pKa % non-ionised HER Clearance T1/2

CSHT

(4hr)

Equ'n time
Morphine 1 3-5 L/kg 35% 1 7.9 23% 0.6-0.8 15 - 30 mL/kg/min 1.7 - 3.3 hr
Pethidine 0.1 3-5 L/kg 70% 32 8.5 7% 0.5-0.7 8 - 18 mL/kg/min 3 - 5 hr
Fentanyl 100 3-5 L/kg 84% 955 8.4 8.5% 0.8-1.0 10 - 20 mL/kg/min 3.1 - 6.6 hr 260 min 6.8 min
Sufentanil 1000 2.5-3 L/kg 93% 1727 8.0 20% 0.7-0.9 10 - 15 mL/kg/min 2.2 - 4.6 hr 30 min 6.2 min
Alfentanil 10 0.4-1.0 L/kg 92% 129 6.5 89% 0.3-0.5 4 - 9 mL/kg/min 1.4 - 1.5 hr 60 min 1.4 min
Remifentanil 2000 0.2-0.3 L/kg 80% 7.3 58% 30 - 40 mL/kg/min 0.17 - 0.33 hr 4 min 1.1 min
Tramadol 2-3 L/kg 20% 9.41 6 - 9 mL/kg/min

5 - 7 hr

6 - 8 hr (M1)

NB:

  • Potency table is a very rough estimation
  • Fentanyl is 75-125 times as potent as morphine
  • Sufentanil is about 10 times as potent as fentanyl
  • Alfentanil is about 1/10 as potent as fentanil
  • Remifentanil is 15-20 times as potent as fentanyl

=====

Still need to do tables for

  • NMBD
  • Anticholinesterase
  • Anticholinergics
  • Benzodiazepine (Diazepam, Midazolam, lorazepam, Flumazenil)



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