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. Author manuscript; available in PMC: 2012 Jul 1.
Published in final edited form as: Expert Opin Drug Metab Toxicol. 2011 Apr 8;7(7):803–816. doi: 10.1517/17425255.2011.574127

Table 1.

Pharmacological interventions involved in critical ill patients and their pharmacokinetic characteristics

ANALGESICS/SEDATIVE Half life Protein binding Hepatic extraction ratio to blood flow CYP3A CYP2C9/19 CYP2D6 Renal elimination Transporter/OTHERS
Fentanyl 2.5–6.5mins 80–85% High
Propofol 30–60mins 95–99% High CYP2B/UGT
Alfentanil 1.5–2 hrs 92% Low
Midazolam 1.8–6.4hrs 95% Low/Intermediate
Morphine 2–3hrs 30–40% High UGT
MUSCLE RELAXANT
Vecuronium 51–80mins 30% Low PGP
Pancuronium 1.5–2.7hrs 77–91% Low √ +Bile
ANTI-ARRYTHMICS
Lidocaine 1.5–2hrs 61–80% High CYP1A2
Amiodarone 15–142 days 33–65% Low Bile
Digoxin 38–48hrs 25% Low PGP
Procainamide 2.5–4.5hrs 15–20% Intermediate
Bretylium 7–8hrs N/A N/A √ only
ANTI-HYPERTENSIVE
Verapamil 2.8–7.4hrs 90% Intermediate PGP
Enalapril 11hrs N/A Intermediate OATP/MRP2
Metoprolol 3–7hrs 15% Intermediate/high
Propranolol 4–5hrs 88% High
Atenolol 6–7hrs 6–16% Low
Valsartan 6hrs 95% N/A √+Bile OATP/MRP2
Pravastatin 77hrs 50% Intermediate/high OATP1B1/OATP2B1
RESUSCITATION/INCREASE HEART RATE
Epinephrine 2mins N/A N/A MAO/COMT
Dopamine 9mins N/A N/A MAO/COMT
ANTI-CONVULSANT
Phenytoin 6–24hrs 90% Intermediate √+Bile UGT
Phenobarbital 2–7 days 20–45% N/A CYP2C19/UGT
Carbamazepine 25–65hrs 76% Low PGP/UGT
MISCELLANEOUS
Warfarin 30–60hrs 99.5% Low √ (S−,R−) CYP1A2(R−)
Mannitol 100mins N/A N/A √ only
Gentamicin 2 hrs 0–10% N/A
Rifampin 1.5–5hrs 90–95% N/A Esterases
Ranitidine 2–3hrs 15% N/A PGP
Famotidine 8–12hrs 10–28% N/A
Corticosteriods Varies varies N/A
Magnesium Sulfate N/A NA N/A √ only

Abbreviations: N/A: Not available; mins: Minutes; hrs: Hours; PGP: P-glycoprotein; UGT: UDP-galactose transporter; MAO: monoamine oxydase; COMT: catechol-O-methyltransferase; OATP: organic anion transporter; MRP2: Multidrug resistance protein 2.