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Cytochrome P450 : Alphabetical drug list C |
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C | ||
Drug | CYP interaction | Clinical consequences |
caffeine | CYP1A2 : low activity (neonates) | toxicity |
3A4 : metabolism | ? | |
Calcium channel blockers (dihydropyridine) | CYP3A4 : METABOLISM | less effective with high activity; low 3A4 activity delays clearance : hypotension [Clin Pharmacokinet 2000 Jan;38(1):41-57 ] |
CYP3A4 : INHIBIT | ? interactions | |
2D6, 2C9 (also inhibited: most notably by nicardipine) [Drug Metab Dispos 2000 Feb;28(2):125-30] | ? | |
cannabinoids (eg. cannabidiol), cannabis | 3A4 : metabolism AND inhibition | potential for interaction with eg. cyclosporine [Xenobiotica 1996 Mar;26(3):275-84] |
carbamazepine | CYP3A4 : INDUCES | hastens metabolism of
valproic acid, clonazepam,
ethosuximide, lamotrigine, topiramate, tiagabine and remacemide;
also tricyclic antidepressants, antipsychotics, steroid oral contraceptives, glucocorticoids, oral anticoagulants, cyclosporine, theophylline |
CYP3A4 : metabolism | toxicity with eg. macrolides,
stiripentol, remacemide, acetazolamide, macrolide antibiotics,
isoniazid, metronidazole, certain antidepressants, verapamil,
diltiazem, cimetidine, danazol and (dextro)propoxyphene;
rapid removal with phenytoin, phenobarbital, primidone [Clin Pharmacokinet 1996 Sep;31(3):198-214] | |
CYP2C9 : ? induces | ? less warfarin effect | |
carisoprodol | CYP2C19 : low activity | less effective (less formation of meprobamate) |
carvedilol (See also beta blockers) | 2D6 (some contribution from other CYPs e.g. 2C9, and non-oxidative elimination) | "possibly of little significance" [Drug Metab Dispos 1997 Aug;25(8):970-7], but low 2D6 may result in more alpha blockade |
celecoxib | 2C9 : metabolism [Clin Ther 1999 Jul;21(7):1131-57], [Clin Pharmacokinet 2000 Mar;38(3):225-42] | potential for interactions. |
2D6 : INHIBITS | ? warfarin - increased effect! | |
cerivastatin (See also HMG Co-A reductase inhibitors) | 3A4 : substrate | ?? significance (minor interaction with erythromycin) ; no interaction with nifedipine |
chlorpheniramine | 3A4 : metabolism | |
2D6 : inhibits (Ki 11 µM) | ||
chlorpromazine (See also Antipsychotics) | CYP2D6 : metabolism and inhibition
(? also 3A4 metabolism) | e.g. inhibition of codeine effect |
cimetidine | CYP1A2 : INHIBITS ( >> ranitidine) | ? |
CYP2D6 : INHIBITS (>>> ranitidine) | increases systemic effect of timolol opthalmic drops!
[J Clin Pharmacol 2000 Feb;40(2):193-9] | |
3A4 : INHIBITS (>>> ranitidine) (and metabolism ?) | ? | |
ciprofibrate | 3A4 | (see fibrates) |
ciprofloxacin | CYP1A2 : INHIBITS | ? |
3A4 : INHIBITS | (see also Quinolones) | |
cisapride | CYP3A4 METABOLISM | 3A4 inhibition gives polymorphic ventricular tachycardia eg with clarithromycin , nefazodone, diltiazem, saquinavir, grapefruit juice [Clin Pharmacol Ther 1999 Apr;65(4):395-401] |
citalopram (SSRI) | 2C19 : metabolism | ? |
3A4 : metabolism | ? | |
2D6 : metabolism (mild inhibition) | ? | |
clarithromycin | 3A4 : metabolism | levels may increase with ritonavir, omeprazole; low with rifampicin |
3A4 : INHIBITS | caution with cisapride, pimozide, midazolam, &c; carbamazepine, cyclosporine, theophylline, [see: Clin Pharmacokinet 1999 Nov;37(5):385-98 ??] | |
clemastine (1st generation antihistamine) | 2D6 : INHIBITS (Ki ~ 2 µM) | significant interaction feasible |
clindamycin | 3A4 : metabolism | ? |
clomipramine (see Tricyclics) | 1A2 : metabolism | ? |
2C19 : metabolism | ? | |
2D6 : metabolism also ? 3A4 metabolism | ? | |
2D6 : INHIBITS | e.g. decreased codeine action | |
clopidogrel | activated by CYP1A | Does NOT affect aminophyllin clearance [Semin Thromb Hemost 1999;25 Suppl 2:65-8] |
clozapine | CYP1A2 : METABOLISM
(? also 2D6) | lower levels with cigarette smoking, carbamazepine; raised with caffeine, erythromycin |
cocaine | 3A4 : metabolism | {norcocaine is oxidation product, responsible for hepatotoxicity} |
2d6 : INHIBITS (0.07 µmol) | Strong interaction potential | |
codeine : CYP2D6 activation to morphine is central to codeine's effects | CYP2D6 : low activity | inadequate analgesia;
fluoxetine could be used to treat codeine dependence ; gastrointestinal effect of codeine is also probably mediated by metabolite morphine |
CYP2D6: raised activity | excessive morphine production,
severe epigastric pain! [Ther Drug Monit 1997 Oct;19(5):543-4] | |
CYP3A4 : metabolism to norcodeine (N-demethylation) | ? (rifampicin attenuates codeine effect [J Pharmacol Exp Ther 1997 Apr;281(1):330-6] ) | |
cortisol : see hydrocortisone | ||
coumarin | 2A6 : metabolism (coumarin 7 hydroxylase) | ? |
cyclobenzaprine | CYP1A2 substrate | ? |
3A4 : substrate | ? | |
cyclophosphamide (prodrug, activated by 2B6) | CYP2B6 : metabolism | ? |
CYP2B6 : INDUCES | ? | |
cyclosporine (cyclosporin A)
{for a note on 'cyclosporine-sparing agents' see [Clin Pharmacokinet 1997 May;32(5):357-67] } | CYP3A4 : hi activity | less effective : transplant rejection. Potentially occurs with: rifampicin, sulfadimidine, phenobarbital, phenytoin, phenylbutazone, dexamethasone, sulfinpyrazone, and carbamazepine. |
CYP3A4 : low activity | toxicity (eg with nefazodone)
fluconazole increases cyA bioavailability
many other drugs eg clarithromycin,
quinolones,
glibenclamide,
ketoconazole,
amiodarone
Other potential drugs causing CYA toxicity include: triacetyloleandomycin, erythromycin, josamycin, midecamycin, miconazole, midazolam, nifedipine, diltiazem, verapamil, nicardipine, ergotamine, dihydroergotamine, glibenclamide, bromocriptine, ethinylestradiol, progesterone, cortisol, prednisone, prednisolone, methylprednisolone [Drug Metab Dispos 1990 Sep-Oct;18(5):595-606] | |
3A4 : INHIBITS | drug toxicity eg statins |
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Page author: jo@anaesthetist.com | Last update: 2000-6-22 |