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The Life Raft Group - Ensuring that no one has to face GIST alone The Life Raft Group - Ensuring that no one has to face GIST alone
Hi, my name is Rachel. I'm 20 years old and from the U.K.
Hi, my name is Rachel. I'm 20 years old and from the U.K.
The Life Raft Group - Ensuring that no one has to face GIST alone
About GIST
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All About Gleevec (Glivec)

Long list of Inhibitors and Inducers of CYP3A4 and CYP2D6

Drugs that may alter Gleevec plasma concentrations

(Long List)

also see: www.drug-interactions.com

NOTE: CYP3A4 is the main enzyme that metabolizes Gleevec and therefore effects may be more pronounced that those related to CYP2D6

Drugs that
Induce CYP3A4
1


Drugs that
Inhibit CYP3A41


Reduce Gleevec levels

Increase Gleevec levels

  • May result in sub-therapeutic levels of Gleevec
  • May result in above normal levels of Gleevec
  • May be more of a concern for lower doses of Gleevec
  • May be more of a concern for higher doses of Gleevec
  • CYP3A4 inducers
  • CYP3A4 inhibitors

Carbamezepine
Dexamethasone
Ethosuximide
Glucocorticoids
Griseofulvin
Phenytoin
Primidone
Progesterone
Rifabutin
Rifampin
Nafcillin
Nelfinavir
Nevirapine
Oxcarbazepine
Phenobarbital
Phenylbutazone
Rofecoxib (mild)
St John's wort
Sulfadimidine
Sulfinpyrazone
Troglitazone
 

Aminodarone
Anastrozole
Azithromzcin
Cannabinoids
Cimetidine
Clarithromycin
Clotrimazole
Cyclosporine
Danazol
Delavirdine
Dexamethasone
Diethyldithiocarbamate
Diltiazem
Dirithyromycin
Disulfiram
Entacapone (high dose)
Erythromycin
Ethinyl estradiol
Fluconazole
Fluoxetine
Fluvoaxamine
Gestodene
Grapefruit juice
Indinavir
Isoniazid
Ketoconazole
Metronidazole
Mibefradil
Miconazole
Nefazodone
Nelfinavir
Nevirapine
Norfloxacin
Norfluoxetine
Omeprazole
Oxiconazole
Paroxetine (weak)
Propoxyphene
Quinidine
Quinine
Quinupristine and dalfopristin
Ranitidine
Ritonavir
Saquinavir
Sertindole
Sertraline
Troglitazone
Troleandomycin
Valproic acid

Drugs that
Induce CYP2D6
2


Drugs that
Inhibit CYP3A41


May Reduce Gleevec levels

May Increase Gleevec levels

  • May result in sub-therapeutic levels of Gleevec
  • May result in above normal levels of Gleevec
  • May be more of a concern for lower doses of Gleevec
  • May be more of a concern for higher doses of Gleevec
  • CYP2D6 inducers
  • CYP2D6 inhibitors

Dexamethasone
Rifampin
 

Amiodarone
Celecoxib
Chloroquine
Chlorpromazine
Cimetidine
Citalopram
Clomipramine
Codeine
Deiavirdine
Desipramine
Dextroprpoxyphene
Diltiazem
Doxorubicin
Entacapone (high dose)
Fluoxetine
Fluphenazine
Fluvaxamine
Haloperidol
Labetalol
Lobeline
Lomustine
Methadone
Mibefradil
Moclobemide
Nortuloxeline
Paroxetine
Perphenazine
Propafenone
Quinacrine
Quinidine
Ranitadine (ranitidine, Zantac)
Risperidone (weak)
Ritonavir
Serindole
Sertraline (weak)
Thioridazine
Valproic acid
Venlafaxine (weak)
Vinblastine
Vincristine
Vinorelbine
Yohimbine
 

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1. List of "medications to avoid (if possible)" given to phase II Gleevec/GIST patients.
2. www.drug-interactions.com

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