Pharmacokinetic Table

A

acetylcysteine

n/a

2-6 h

deacetylation

0.3

aciclovir

0.2

3 h

renal

0.8

alendronic acid

0.006

1 h

renal

0.5

30 minutes before first food of the day.

Antacids and calcium ↓ absorption.

Deposits in bone for ten years.

allopurinol

(oxypurinol)

0.8

1 h

(24 h)

xanthine oxidase

(renal)

0

(0.8)

Increases 6-mercaptopurine and azathioprine toxicity.

alprazolam

0.9

6-16 h

CYP3A

0.2

amiodarone

(desethylamiodarone)

0.4

55 d

(62 d)

CYP3A, 1A2

0

(0)

Inhibits 2C8/9.

TDM.

amitriptyline

(nortriptyline)

0.5

15 h

(30 h)

CYP2D6

0

(0)

amlodipine

0.7

40 h

CYP3A

0

amoxicillin

0.9

2 h

renal

0.9

amoxicillin+

clavulanic acid

0.9/0.5

2 h

1 h

renal

0.9

0.5

amphotericin

0.05

15 d

unknown

0.1

aspirin

0.8

0.3 h

esterases and glucuronidation (enzyme unknown)

0

(salicylic acid)

(2h)

glucuronidation (enzyme unknown) and renal

(0.2)

Renal excretion depends on urine pH; and contributes to more elimination in overdose. In overdose, half life increases up to 13 hours.

(acetyl)

unknown

unknown

unknown (likely = 0)

Acetyl binds irreversibly to platelets, contributing to COX inhibition.

atenolol

0.6

6 h

renal

0.9

atorvastatin

(ortho-hydroxy atorvastatin)

0.1

14 h

(18 h)

CYP3A, Pgp, OATP1B1

(CYP3A)

0

(0)

Subject to CYP3A and Pgp inhibition.

Duration of action more than 24 hours.

atropine

1

4 h

hepatic oxidation

0.3

azathioprine

(6-mercaptopurine)

0.6

4 h

(1 h)

TPMT

0

(0.1)

Allopurinol ↑ conc. (of 6TGN)

TDM.

azithromycin

0.4

60 h

substantial biliary excretion

0.1

↑ warfarin effect.

B

baclofen

1

4 h

deamination

0.8

beclometasone

(beclomet. monoprop.)

n/a

0.5 h

(3 h)

esterases

0.1

(0.1)

bendroflumethiazide

(bendrofluazide)

1

6 h

renal (metabolism unknown)

0.3

↑ lithium conc.

Affects sodium, potassium, magnesium, calcium.

benzylpenicillin

n/a

1 h

hydrolysis

0.9

bezafibrate

1

2 h

CYP3A

0.4

Modified-release tablets have longer duration of action. Do not crush or chew modified-release dose form.

bisoprolol

0.9

10 h

renal

0.5

budesonide

0.1

2 h

CYP3A

0

bupropion

(hydroxybupropion)

0.5

21 h

(21 h)

CYP2B6

0

Inhibits CYP2D6.

buspirone

0.04

3 h

CYP3A

0

C

calcitriol

1

15 h

hydroxylation

0.1

candesartan (prodrug)

0.4

9 h

CYP2C8/9 (10%)

0.6

captopril

0.7

2 h

renal

0.5

carbamazepine

0.9

15 h

CYP3A

0

Induces CYPs.

TDM.

carvedilol

0.3

7 h

CYP2D6

0.1

cefaclor

0.9

0.7 h

renal

0.7

cefazolin

n/a

2 h

renal

0.9

cefalexin

0.9

1 h

renal

0.9

cefepime

n/a

2 h

renal

0.8

cefotaxime

n/a

1 h

renal

0.7

ceftazidime

n/a

2 h

renal

0.9

ceftriaxone

n/a

8 h

50% renal and 50% biliary excretion

0.5

cefuroxime

0.4

2 h

renal

0.9

celecoxib

0.4

11 h

CYP2C8/9

(> 70%)

0

Ensure euvolaemic. Hypovolaemia increases risk of renal impairment.

cetirizine

0.8

7–11 h

dealkylation

0.7

chlorpromazine

0.3

30 h

CYP2D6

0

ciclosporin

0.5

12 h

CYP3A

0

Inhibits CYP and OATP.

TDM.

cilazapril (prodrug)

(cilazaprilat)

0.6

n/a

(45 h)

n/a

(renal)

n/a

(0.9)

ciprofloxacin

0.7

4 h

renal

0.5

Inhibits CYP1A2 and 3A.

Antacids, milk, and enteral feeds ↓ absorption.

citalopram

0.8

35 h

CYP3A, CYP2C19

0.1

clarithromycin

0.5

4 h

CYP3A

0.2

Inhibits CYP3A and Pgp.

clindamycin

0.9

3 h

CYP3A

0.1

clomipramine

0.5

25 h

CYP2D6, 1A2

0

clonazepam

0.8

30 h

CYP3A

0

clonidine

1

13 h

renal

0.6

clopidogrel

(prodrug)

0.5

8 h

CYP2C19

0.1

2C19 inhibitors ↓ efficacy.

clozapine

0.6

12 h

CYP1A2

0.1

TDM. Smoking induces 1A2 and ↓ clozapine conc.

codeine

(morphine)

(m-6-glucuronide)

0.5

3 h

(3 h)

(5 h)

CYP2D6 (major)

0.1

(0.1)

(0.9)

CYP2D6 inhibitors ↓ morphine conc.

colchicine

0.3

0.2 h

deacetylation

0.3

(cole)calciferol

(calcitriol)

0.8

14 d

(15h)

hydroxylation

(hydroxylation)

0

(0.1)

Colestyramine ↓ absorption.

colestyramine

0

n/a

not absorbed - excreted in stool

0

↓ absorption of some drugs e.g. warfarin and fat soluble vitamins.

cyclizine

0.5

24 h

demethylation

0

D

dabigatran etexilate

(prodrug)

(dabigatran)

0.07

0.5 h

(15 h)

esterases

(glucuronidation)

0

(0.8)

TDM

dantrolene

0.8

9 h

unknown

0

dexamethasone

0.8

4 h

CYP3A

0

diazepam

(desmethyldiazepam)

(oxazepam)

0.9

30 h

(50 h)

(4-24 h)

CYP3A, 2C19

(hydroxylation)

(glucuronidation)

0

(0)

(0.1)

diclofenac

0.6

2 h

UGT3B7

0

Ensure euvolaemic, hypovolaemia increases risk of renal impairment.

Modified-release tablets have longer duration of action. Do not crush or chew modified-release dose form.

digoxin

0.7

36 h

renal

0.8

TDM

dihydrocodeine

0.2

4 h

glucuronidation

0.3

diltiazem

0.4

4 h

CYP3A

0

Inhibits CYP3A and Pgp.

Modified-release capsules have longer duration of action. Do not crush or chew modified-release dose form.

dipyridamole

0.5

11 h

unknown

0

domperidone

0.2

14 h

CYP3A

0.1

doxazosin

0.7

12 h

CYP3A

0.1

doxycycline

1

16 h

renal; metabolism unknown

0.4

Chelation with multivalent cations, e.g. iron and calcium.

Take with food.

dulaglutide

n/a

5 d

protein catabolism

0

Delays gastric emptying.

E

empagliflozin

0.6

12 h

glucuronidation and renal

0.5

No dose reduction in chronic kidney disease.

enalapril (prodrug)

(enalaprilat)

0.6

n/a

(36 h)

n/a

(renal)

n/a

(0.9)

enoxaparin

n/a

5 h

renal; and hepatic metabolism (desulfation, depolymerisation)

0.7

erythromycin

0.4

2 h

CYP3A

0

Inhibits CYP3A.

ethambutol

0.8

3 h

renal; and metabolised (dicarboxylic acid derivative and an aldehyde intermediate)

0.8

ethinylestradiol

0.5

12 h

CYP3A

0

ethosuximide

1

55 h

CYP3A

0.2

ezetimibe

(ezetimibe glucuronide)

unknown

25 h

(17 h)

glucuronidation

0

F

famotidine

0.4

3 h

renal

0.7

↓ absorption of azole antifungals

felodipine

0.2

3 h

CYP3A

0

Modified-release tablets have longer duration of action (~24 hours). Do not crush or chew modified-release dose form.

fentanyl

0.7 nasal

4 h

CYP3A

0.1

flecainide

1

14 h

CYP2D6

0.3

TDM

flucloxacillin

0.9

1 h

renal

0.7

fluconazole

0.9

30 h

renal

0.8

Inhibits CYP3A, 2C8/9, 2C19.

flumazenil

n/a

1 h

liver

0.1

fluoxetine

(norfluoxetine)

0.9

4 d

(15 d)

CYP2D6

0.1

(0.1)

Inhibits CYP2D6 and 2C19.

flutamide

(N-hydroxyflutamide)

0.9

8 h

(8 h)

CYP1A2

0.1

(0.1)

fluticasone

n/a

2-5 h

CYP3A

0.1

formoterol

n/a

10 h

glucuronidation

0.2

furosemide (frusemide)

0.5

1 h

renal

0.8

↓ cation conc. except lithium which ↑.

G

gabapentin

0.6

6 h

renal

0.8

ganciclovir

0.08

4 h

renal

0.8

gentamicin

n/a

3 h

renal

0.9

TDM.

glibenclamide

0.9

12 h

CYP2C9

Usually stopped when insulin started.

gliclazide

0.9

10 h

CYP2C9

0

Usually stopped when insulin started.

glipizide

1

3 h

CYP2C9

0.1

Usually stopped when insulin started.

glyceryl trinitrate

0.4

subling

0.5 h

hydrolysis, glucuronidation

0.1

H

haloperidol

0.7

20 h

CYP3A, 2D6

0

heparin

-

2 h

reticulo-endothelial system

0

hydrocortisone

1

2 h

CYP3A

0

hyoscine-N-butylbromide

0.01

5 h

renal; metabolism unknown

0.5

I

ibuprofen

0.9

2 h

CYP2C8/9

0

Ensure euvolaemic. Hypovolaemia increases risk of renal impairment.

↓ dose if co-prescribed with strong CYP2C9 inhibitors (e.g. voriconazole and fluconazole, which double ibuprofen conc.)

Modified-release tablets have longer duration of action. Do not crush or chew modified-release dose form.

imipenem+cilastatin

n/a

1 h

renal

0.7

insulin

n/a

6 minutes

insulin degrading enzyme (liver and kidneys)

0

Different insulins have different subcutaneous absorption times that determine duration of effect.

Medicine (brand)

Tmax

Duration of action

insulin glargine

(Lantus)

no peak

24 hours

insulin aspart

(Novorapid)

1 hour

4 hours

insulin lispro

(Humalog)

1 hour

1 hour

isophane insulin

(Protaphane)

2–8 hours

16 hours

human neutral insulin

(Actrapid, Humulin R)

1–4 hours

8 hours

insulin glulisine (Apidra)

1 hour

4 hours

indometacin

1

6 h

CYP2C9 (50%), UGT1A9 (30%)

0.1

Ensure euvolaemic, Hypovolaemia increases risk of renal impairment

iron polymaltose

n/a

6 h

unknown

trace

isoniazid

0.9

1–4 h

acetylation

0.05–0.3

isosorbide mononitrate

0.9

5 h

glucuronidation, dinitration

0

Modified-release tablets have longer duration of action. Do not crush or chew modified-release dose form.

isotretinoin

(4-oxo-isotretinoin)

0.2

21 h

(21 h)

CYPs

0

(unknown)

itraconazole

0.6

35 h

CYP3A

0

Take capsules with food.

Inhibits CYP3A.

TDM.

K

ketoconazole

0.8

8 h

CYP3A

0

Inhibits CYP3A, 2C8/9, 2C19, 1A2 and Pgp.

L

labetalol

0.3

3 h

glucuronidation

0

lamivudine

0.9

6 h

renal, sulphoxation

0.8

lamotrigine

1

24 h

glucuronidation

0.1

TDM.

levetiracetam

1

8 h

renal, hydrolysis (24%)

0.7

levodopa

+benserazide

0.4/0.7

1 h

dopa decarboxylase

0

lidocaine

n/a

2 h

CYP3A, 2D6

0.1

lisinopril

0.3

12–30 h

renal

0.9

lithium

1

22 h

renal

1

NSAIDs, ACEIs, and thiazides ↑ conc.

TDM.

loperamide

0.01

11 h

CYP3A

0.1

loratadine

n/a

12 h

CYP3A

0

lorazepam

0.9

15 h

glucuronidation

0

losartan

(active metabolite)

0.4

2 h

(6 h)

CYP2C8/9

0.1

(0.4)

M

6-mercaptopurine

0.1

1 h

TMPT

0.1

Allopurinol ↑ conc. (of 6TGN).

meropenem

n/a

1 h

renal, hydrolysis

0.7

mesalazine (5ASA)

0.3

1 h

acetylation

0

metformin

0.5

5 h

renal

0.9

TDM (for GFR < 30 mL/min)

methadone

0.8

15–55 h

CYP3A

0.15

methotrexate

0.9–0.2

8 h

renal, intracellular metabolism to polyglutamates

0.9–0.5

Co-prescribe folate.

Weekly dose (not daily).

F, half life, and fe vary with dose.

methylphenidate

0.2

3 h

de-esterification

0

methylprednisolone

0.8

3 h

CYP3A

0

metoclopramide

0.7

5 h

CYP2D6

0.2

metoprolol

0.4

4 h

CYP2D6

0.1

Modified-release tablets have longer duration of action. Do not crush or chew modified-release dose form.

metronidazole

1

8 h

oxidation, glucuronidation

0.1

midazolam

0.5

2 h

CYP3A

0

mirtazapine

0.5

30 h

unknown

0

moclobemide

1

2 h

CYP2C19

0

Inhibits CYP2D6.

morphine

(m-6-glucuronide)

0.3

3 h

(5 h)

glucuronidation

(renal)

0

(0.9)

Modified-release tablets have longer duration of action. Do not crush or chew modified-release dose form.

mycophenolate

(mycophenolic acid)

0.9

0.03 h

(16 h)

esterases to mycophenolic acid then glucuronidated

0

(0)

TDM.

N

nadolol

0.3

20 h

renal

0.8

naloxone

n/a

1 h

glucuronidation

0

naproxen

1

14 h

CYP2C8/9

0.1

Ensure euvolaemic, hypovolaemia increases risk of renal impairment.

Modified-release tablets have longer duration of action. Do not crush or chew modified-release dose form.

nefopam

0.6

4 h

unknown

0

nicorandil

0.9

1 h

dinitration, oxidation

0

nicotinic acid

(niacin)

0.9

1 h

renal, metabolism unknown

0.4

nifedipine

0.5

2 h

CYP3A

0

Do not crush or chew modified-release dose form. Different formulations have different durations of action and dose frequency.

nimodipine

0.1

8 h

CYP3A

0

nitrofurantoin

0.9

1 h

reduction

0.5

Modified-release capsules have longer duration of action. Do not crush or chew the modified-release dose form.

norfloxacin

0.5

4 h

renal, conjugation

0.3

Antacids ↓ absorption.

nortriptyline

0.6

30 h

CYP2D6

0

O

olanzapine

0.6

33 h

CYP1A2

0

omeprazole

0.5

1 h

CYP2C19 (80%)

0

Inhibits 2C19.

Do not crush or chew the modified-release dose form.

ondansetron

0.6

4 h

CYP2D6

0

oseltamivir (prodrug)

(oseltamivir carboxylate)

0.8

n/a

(2 h)

n/a

(renal, OAT1)

n/a

(0.9)

Oseltamivir carboxylate apparent half life 8 hours.

oxazepam

1

4–25 h

glucuronidation

0.1

oxybutynin

0.03

2 h

CYP3A

0

oxycodone

0.7

3 h

CYP2D6

0.2

Do not crush or chew the modified-release dose form.

P

pantoprazole

0.8

1 h

CYP2C19

0

Do not crush or chew the modified-release dose form.

paracetamol

0.8

2 h

glucuronidation (60%), sulphation (30%), CYP2E1 (< 10%)

0

Inducers increase hepatotoxic potential.

parecoxib

(valdecoxib)

n/a

0.5 h

(8 h)

hydrolysis

glucuronidation, CYP2C9,

CYP3A4

0

(0)

Ensure euvolaemic. Hypovolaemia increases risk of renal impairment.

paroxetine

0.5

20 h

CYP2D6

0

CYP2D6 inhibitor.

perhexiline

0.9

15 h

CYP2D6

0

TDM.

perindopril (prodrug)

(perindoprilat)

0.9

n/a

(30 h)

n/a

(renal)

n/a

(0.9)

pethidine

(norpethidine)

0.5

4 h

(25 h)

CYP2D6

(renal)

0.2

(0.9)

Norpethidine is CNS toxic, and accumulates in renal failure.

phenobarbital

1

3–4 d

metabolism unknown

0.1–0.25

Strong CYP inducer.

phenoxymethylpenicillin

0.4

0.5 h

renal

0.9

phenytoin

0.9

n/a

CYP2C8/9

0

Saturable elimination.

Induces several drug-metabolising enzymes.

TDM.

pioglitazone

(MIV metabolite)

(MIII metabolite)

0.9

6 h

(24 h)

(12 h)

CYP2C8/9

CYP2C8/9

CYP3A4/5

0

(0.1)

(0.1)

Duration of action more than 24 hours due to active metabolites.

piperacillin

+tazobactam

n/a

1 h

renal

0.8/0.6

pravastatin

0.2

2 h

acid isomerisation

0.1

prednisone

(prednisolone)

0.1

(0.8)

0.5 h

(3 h)

CYP3A

0

prochlorperazine

0.1

8–20 h

unknown

0

promethazine

0.3

10 h

CYP2D6

0

propranolol

0.3

4 h

CYP2D6

0

protamine

n/a

10 min 

(variable)

complexes with heparin

0

Q

quetiapine

0.09

6 h

CYP3A

0.1

quinapril (prodrug)

(quinaprilat)

0.5

n/a

(2 h)

n/a

(renal)

n/a

(0.9)

R

rifampicin

0.9

3 h

glucuronidation, deacetylation

0

Induces several CYP enzymes and Pgp.

risperidone

(9-OH risperidone)

0.7

3 h

(24 h)

CYP2D6,

3A (minor)

0

rivaroxaban

0.9

7 h

CYP3A4, Pgp, renal

0.4

Subject to CYP3A and Pgp inhibition and induction. TDM

rosuvastatin

0.2

19 h

biliary, OATP1B1

0.1

roxithromycin

0.8

12 h

CYP3A

0.1

S

salbutamol

n/a

4 h

conjugation

0

selegiline

(amphetamine,

methamphetamine, desmethylselegiline)

0.1

3 h

(14 h)

(12 h)

(5 h)

CYP2C19

0.1

simvastatin

(beta-hydroxyacid simvastatin)

0.05

2 h

(4 h)

esterases

(CYP3A, Pgp, OATP1B1)

0

(0)

Subject to CYP3A and Pgp inhibition (including grapefruit).

sodium valproate

1

12 h

0.05 glucuronidation (30–50%), oxidation (40%)

0

Inhibits several CYP enzymes.

solifenacin

0.9

52 h

CYP3A4

0.1

sotalol

0.9

12 h

renal

0.9

spironolactone

(active metabolites)

0.7

1 h

(15 h)

multiple metabolic pathways

0.1

(0.1)

Take with food.

↑ digoxin conc.

sulphasalazine

0.05

8 h

bacteria

0

sumatriptan

0.1

2 h

oxidation

0.2

T

tacrolimus

0.3

10 h

CYP3A

0

TDM

Food decreases bioavailability, so dose consistently with or without food.

tamoxifen

(active metabolite)

1

7 d

(12 d)

CYP2D6

(CYP3A, 2C8/9)

0

tamsulosin

1

12 h

CYP3A4, CYP2D6

0.1

teicoplanin

n/a

90–150 h

renal

1

temazepam

1

9 h

glucuronidation

0

tenoxicam

1

72 h

CYP2C8/9

0

Ensure euvolaemic, hypovolaemia increases risk of renal impairment.

terbinafine

0.4

22–26 h

CYP3A, 1A 2C8/9

0

Inhibits 2D6.

theophylline

1

8 h

CYP1A2

0.1

TDM

ticagrelor

(active metabolite)

0.4

7 h

(9 h)

CYP3A

(CYP3A)

0

(0)

tobramycin

n/a

3 h

renal

0.9

TDM

tramadol

(active metabolite)

0.7

6 h

(8 h)

CYP2D6

(renal)

0.2

(0.9)

tranexamic acid

0.7

2 h

renal

0.9

triazolam

0.4

3 h

CYP3A

0

trifluoperazine

n/a

7–18 h

glucuronidation

0.1

Inhibits Pgp.

trimethoprim

1

10 h

renal

0.7

trimethoprim

+sulfamethoxazole

0.8

9 h

12 h

CYP2C8/9 acetylated

0.3

0.7

V

valganciclovir

(ganciclovir)

0.6

4 h

(4 h)

renal, hydrolysed

0.8

(0.8)

vancomycin

n/a

6 h

renal

0.9

TDM.

varenicline

1

24 h

renal

0.9

venlafaxine

(O-desmethylvenlafaxine.)

0.1–0.5

5 h

(11 h)

CYP2D6

(2D6, 2C19)

0.1

(0.1)

verapamil

0.2

2–5 h

CYP3A

0

CYP3A and Pgp inhibitor.

Modified-release tablets have longer duration of action. Do not crush or chew modified-release dose form.

vildagliptin

0.8

2 h

hydrolysis

0.2

voriconazole

1

6 h

CYP3A

0

IV vehicle of voriconazole injection accumulates in renal impairment and has caused vacuolation in rats.

Inhibits 3A and 2C8/9.

TDM.

W

warfarin

1

36 h

CYP2C8/9

0

Z

zopiclone

0.8

5 h

plasma decarboxylation

0.1