Canterbury DHB

Context

Pharmacokinetic Table

This table has key pharmacokinetic data for commonly prescribed medicines.

The data are for an "average healthy adult".

Consider the prescribed dose form and route of administration as these may impact drug bioavailability and clearance.

See the prescribing guidelines for how to adapt these data to patient characteristics.

A B C D E F G H I K L M N O P Q R S T V W Z

Medicine

(active metabolite)

F

NOTE

Half life

Elimination

NOTE

fe

NOTE

Additional Points

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

Take 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

(cilazaprilat)

0.6

1–2 h

(36–50 h)

esterases

(renal)

0

(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

0.3

12 h

CYP1A2

(> 50%)

0.1

TDM

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)

Dose individualisation – see Hospital HealthPathways.

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

2 h

(36 h)

esterases

(renal)

0.2

(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

TDM.

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

 

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

(perindoprilat)

0.9

 

2 h

30 h

esterases

(renal)

0.1

(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.

pholcodine

unknown

32–43 h

renal, metabolism unknown

0.3

 

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

(quinaprilat)

0.5

1 h

(2 h)

esterases  

(renal)

0.1

(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

 

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

 

F = The fraction bioavailable following oral administration.

fe = The fraction excreted unchanged in the urine.

Conc = Concentration in plasma.

d = days

h = hours

min = minutes

Information about this Canterbury DHB document (102199):

Document Owner:

Not assigned (see Who's Who)

Last Updated:

September 2020

Next Review Due:

September 2022

Keywords:

Note: Only the electronic version is controlled. Once printed, this is no longer a controlled document.

Topic Code: 102199