| A |
| Drug |
CYP interaction |
Clinical consequences |
| aceclofenac
| 2C9 : METABOLISM
| ?
|
| acetaminophen : see paracetamol
|
| alfentanil
| CYP3A4 : metabolism
| eg. fluconazole inhibits clearance 55%
[Anesth Analg 1998 Jul;87(1):190-4]
See also [Anesthesiology 1997 Jul;87(1):36-50] -
rifampicin and troleandromycin strongly inhibit metabolism.
|
| alprazolam (See also Benzodiazepines)
| CYP3A4 : metabolism
| ? expect interactions eg. ritonavir, nefazodone, some SSRIs,
itraconazole,
troleandromycin
excessive sedation with 3A4 inhibitors
|
| alprenolol (see also beta blockers)
| 2D6 : metabolism
| potential for impaired effect / toxicity (2D6 overactivity /
lack)
|
| aminoglutethimide
| CYP11,
CYP19,
CYP21 : inhibits
| potent 'adrenal suppression'.
|
| aminophyllin (see theophylline)
|
| amiodarone
| CYP2C9 : INHIBITS
| 'clinically significant';
IC50 25µmol
Interaction with warfarin may be 2 months later!
[Clin Pharmacokinet 1996 Jun;30(6):416-44]
|
| 1A2: inhibits (weakly)
| ?
|
| 2D6: INHIBITS
| increased flecainide levels
|
| 3A4 : INHIBITS
| lignocaine clearance inhibited,
cyclosporine toxicity
|
| 3A4 : metabolism
| ?
|
| amitriptyline : See also tricyclics
| 1A2 : metabolism
| ?
|
| 2C19 : metabolism (most important)
| SSRIs increase levels!
|
| 3A4 : metabolism (next most important) [J Clin Pharmacol 1998 Feb;38(2):112-21]
| ?
|
| 2C9 : metabolism
| ?
|
| 2D6 : metabolism
| {? also inhibits}
|
| amlodipine
| 3A4 : inhibits (? metabolism)
| ? 'minor effect' on cyclosporine [Clin Nephrol 1997 Nov;48(5):336;
Hypertension 1994 Sep;24(3):297-300]
|
| 1A1 : inhibits
| ?
|
| 2B6 : inhibits
| ?
|
| amphetamine incl. methylenedioxymetamphetamine = MDMA = 'ecstasy';
methamphetamine is probably similar
| 2D6 : metabolism
| serious reaction with HIV protease inhibitors
[Arch Intern Med 1999 Oct 11;159(18):2221-4]
|
| amprenavir
| 3A4 : metabolism
| interaction with 3A4 inhibitors eg ritonavir
|
| 3A4 : INHIBITS (Ki 0.5µM)
| probably significant
|
| anastrozole
| CYP19,
also may inhibit 1A2, 2C8, 2C9, 3A4
| ?
|
| Angiotensin II receptor blockers : See losartan, valsartan, irbesartan
| 2C9
|
|
| Antidepressants :
See individual agents.
Metabolism varies
and is complex, but in general:
| CYP2D6 : low activity
| toxicity
|
| CYP2D6: hi activity
| ineffective
|
Antihistamines (non-sedating, some)
terfenadine, & especially astemizole [see Br J Clin Pharmacol 1999 Mar;47(3):307-13 ]
fexofenadine appears 'safe', as do cetirizine,
azelastine, loratadine;[Clin Ther 1999 Feb;21(2):281-95],
mizolastine [Clin Exp Allergy 1999 Mar;29 Suppl 1:15-24]
(? not ebastine: experimentally prolongs QT)
| CYP3A4 : low activity
| fatal arrhythmias
|
Antipsychotics (see also individual drugs)
2D6 inhibition : perphenazine > thioridazine > chlorpromazine
> haloperidol > fluphenazine > > risperidone > clozapine >
cis-thiothixine.
| CYP2D6 : INHIBITS
|
|
| aprindine (class I antiarrhythmic)
| 1A2 : mild inhibition
| ?
|
| 2D6 : metabolism and INHIBITION
| significant inhibition [Br J Clin Pharmacol 1993 Apr;35(4):426-30]
|
| artemisinin
| CYP2B6 : metabolism (main)
| ?
|
| 3A4 : metabolism (minor)
| (? interaction with azole antifungals, calcium channel blockers)
|
| CYP2C19 : INDUCES
|
probably clinically relevant
|
| astemizole
| CYP3A4 : METABOLISM
| low activity = fatal arrhythmias with eg. ketoconazole, erythromycin,
cimetidine
{Blocks IKr}
|
| 3A4 : inhibits (IC50 21 µM)
| ?
|
| atorvastatin (See also HMG Co-A reductase inhibitors)
| 3A4 : metabolism
| interaction with eg troglitazone
|
azelastine (anti-histamine)
(main metabolite: desmethylazelastine)
| CYP2D6 : metabolism
| ?
|
| CYP3A4 : metabolism
| ? (azelastine appears NOT to induce arrhythmias)
|
| 2D6 : inhibits (Ki 1.2 µM)
| ?
|
| Azole antifungals
| CYP2C9
| INHIBIT
|
| CYP3A4
| INHIBIT
|