CYP2D6 Ligands
Following is a table of selected substrates, inducers and inhibitors of CYP2D6. Where classes of agents are listed, there may be exceptions within the class.
Inhibitors of CYP2D6 can be classified by their potency, such as:
- Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values, or more than 80% decrease in clearance.
- Moderate inhibitor being one that causes at least a 2-fold increase in the plasma AUC values, or 50-80% decrease in clearance.
- Weak inhibitor being one that causes at least a 1.25-fold but less than 2-fold increase in the plasma AUC values, or 20-50% decrease in clearance.
Selected inducers, inhibitors and substrates of CYP2D6
Substrates
↑ = bioactivation by CYP2D6 |
Inhibitors |
Inducers |
- All tricyclic antidepressants, e.g.
- imipramine
- amitriptyline
- etc.
- Most SSRIs (antidepressant), e.g.
- fluoxetine
- paroxetine
- fluvoxamine
- venlafaxine (SNRI antidepressant)
- mianserin (tetracyclic antidepressant)
- opioids
- codeine ↑ into morphine
- tramadol ↑
- oxycodone
- hydrocodone ↑
- antipsychotics, e.g.
- haloperidol
- risperidone
- perphenazine
- thioridazine
- zuclopenthixol
- iloperidone
- aripiprazole
- chlorpromazine
- levomepromazine
- remoxipride
- minaprine (RIMA antidepressant)
- tamoxifen ↑ (SERM)
- beta-blockers
- metoprolol
- timolol
- alprenolol
- carvedilol
- bufuralol
- nebivolol
- propranolol
- debrisoquine (antihypertensive)
- Class I antiarrhythmics
- flecainide
- propafenone
- encainide
- mexiletine
- lidocaine
- sparteine
- ondansetron (antiemetic)
- donepezil (acetylcholinesterase inhibitor)
- phenformin (antidiabetic)
- tropisetron (5-HT3 receptor antagonist)
- amphetamine (in ADHD, narcolepsy)
- atomoxetine (in ADHD)
- chlorphenamine (antihistamine)
- dexfenfluramine (serotoninergic anorectic)
- dextromethorphan (antitussive) into psychoactive dextrorphan
- duloxetine (SNRI)
- metoclopramide (dopamine antagonist)
- Methoxyamphetamine
- perhexiline (antianginal agent)
- phenacetin (analgesic)
- promethazine (antihistamine antiemetic)
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strong:
- SSRIs
- bupropion (non-SSRI antidepressant)
- quinidine (class I antiarrhythmic agent)
- cinacalcet (calcimimetic)
- ritonavir (antiretroviral)
Moderate
- sertraline (SSRI)
- duloxetine (SNRI)
- terbinafine (antifungal)
weak:
- buprenorphine (in opioid addiction)
- amiodarone (antiarrhythmic)
- cimetidine (H2-receptor antagonist)
unspecified potency:
- antipsychotics
- haloperidol
- perphenazine
- thioridazine
- zuclopenthixol
- risperidone
- chlorpromazine
- bicalutamide
- hyperforin (St. Johns Wort)
- antihistamines (H1-receptor antagonists)
- Promethazine
- chlorphenamine
- diphenhydramine
- hydroxyzine
- tripelennamine
- some SSRI antidepressants
- clemastine (antihistamine and anticholinergic)
- celecoxib (NSAID)
- clomipramine (tricyclic antidepressant)
- cocaine (stimulant)
- doxorubicin (chemotherapeutic)
- metoclopramide (antiemetic, prokinetic)
- methadone (analgesic and anti-addictive)
- moclobemide (antidepressant)
- ranitidine (H2-receptor antagonist)
- doxepin (tricyclic antidepressant, anxiolytic)
- halofantrine (in malaria)
- levomepromazine (antipsychotic)
- mibefradil (calcium channel blocker)
- midodrine (α1 agonist)
- ticlopidine (antiplatelet)
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- dexamethasone (glucocorticoid)
- rifampicin (bactericidal)
strong:
- glutethimide (hypnotic sedative)
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