Drug Interactions: Cytochrome P450 Drug Interaction Table. Enzyme induction and inhibition are frequently asked topics from pharmacokinetics in various competitive examinations including USMLE.For more videos please subscribe to our channel:https://www.youtube.com/channel/UCtU1y_tzgmhzV5qQj9Blb2A?sub_confirmation=1Links to related playlists:1.Mnemonics:https://www.youtube.com/playlist?list=PLbilivK1P_9LxDii1hRMDej0BspYPu6ai2. DO NOT perform any examination or procedure on patients based purely on the content of these videos. AUC: area under the concentration-time curve; CYP: cytochrome P450; DDI: drug-drug interaction; OATP1B1: organic anion transporting polypeptide 1B1; OAT3: organic anion transporter 3; P-gp: P-glycoprotein. Note: Strong, moderate, and weak inducers are drugs that decreases the AUC of sensitive index substrates of a given metabolic pathway by 80%, 50% to <80%, and 20% to <50%, respectively. Abbreviations: CYP3A4 enzyme inhibitors Mnemonics Recent Shouts | All Features RxPG has a dedicated forum for Medical Mnemonics! Note: A clinical substrate should meet the following criteria: This table provides examples of clinical substrates for various transporters and is not intended to be an exhaustive list. amlodipine; calcineurin inhibitors e.g. Read our Privacy Policy. In previous issues of Pharmacy Times, we have discussed the cytochrome P450 (CYP450) enzymes CYP1A2, CYP2C9, CYP2C19, and CYP2D6 (see www.PharmacyTimes.com/Drug Interactions). An antiepileptic agent used for the management of generalized convulsive status epilepticus and prevention and treatment of seizures occurring during neurosurgery. Available from: [, Wong C, Lau E, Palozzi L and Campbell F. Pain management in children: Part 2 A transition from codeine to morphine for moderate to severe pain in children. a Recommend the use of two structurally unrelated CYP3A4/5 substrates to evaluate in vitro CYP3A4/5 inhibition. - Over 3000 Free MCQs: https://geekyquiz.com/ Those pro-drugs are substrates of P-gp.n In vitro data suggest a higher contribution of OAT3 than OAT1. Home. Please write a single word answer in lowercase (this is an anti-spam measure). - Medical Finals Question Pack: https://geekymedics.com/medical-student-finals-questions/ Published in November 2012. As a result, the anticoagulant effect of warfarin is increased, measured by an increase in the international normalised ratio (INR). Check out our other awesome clinical skills resources including: c Strong inhibitor of CYP2C8 and inhibitor of OATP1B1 and OAT3. It increases the metabolism and clearance of oral contraceptive pills such as levonorgestrel, norethisterone, ethinylestradiol and desogestrel from the body. Based on animal experiments, liver enzyme inducers have been classified mainly on the basis of the spectrum, i.e. One of those pillars is to increase access to effective treatments worldwide. We aid patients from the United Kingdom to India and Kenya, helping wherever GIST patients are in need. View our 990 Form here, The information provided on the LRG site is designed to support, Always adhere to medical school/local hospital guidelines when performing examinations or clinical procedures. A selected list of such interactions appears in the Table. A dose reduction should be considered in these patients. 00:25 Parts of an OPA Caution should be used when extrapolating the observed effect of ritonavir alone to the effect of combination regimens on CYP3A activities.k The effect of grapefruit juice varies widely among brands and is concentration-, dose-, and preparation-dependent. This type of drug interaction is probably more frequent than commonly realized, because reduced drug effect may simply be attributed to lack of patient response. Note: This page is for educational use and thus is not intended to provide medical advice; please inform your physician or pharmacist of any prescription or over-the-counter medications or supplements you may be taking, and ask them if you have any questions regarding any possible interactions. Check out our NEW quiz platform at app.geekymedics.com, To be the first to know about our latest videos subscribe to our YouTube channel . Thus, using MPP+ as a substrate may underpredict the potential of a drug as an inhibitor of OCT2.a Also a substrate of OATPs.b Also a substrate of OAT3.c Also a substrate of MRP2.d Also a substrate of MATEs.e Also a substrate of P-gp.f Also a substrate of NTCP.g Selective substrate of OATP1B3 (vs. OATP1B1).h Used in vesicle experiments.i Also a substrate of BCRP.j Substrate of OCTs and MATEs. Geeky Medics accepts no liability for loss of any kind incurred as a result of reliance upon the information provided in this video. Note: The IC50 values of several OCT2 inhibitors measured using 1-methyl-4-phenylpyridinium (MPP+) as a substrate were larger than those measured using metformin or creatinine as substrate. PS PORCS: Phenytoin Smoking Phenobarbital Oxcarbazepine (and eslicarbazine) Rifampin Carbamazepine St. John's Wort Mnemonic for Cyp 3a4 inhibitors? The CYP3A family is the most abundant subfamily of the CYP isoforms in the liver. Subscribe to our newsletter to be the first to know about our latest content: https://geekymedics.com/newsletter/ High Yield:https://www.youtube.com/playlist?list=PLbilivK1P_9KrZLVym2_xeIeGjlpQ4SJPFollow us on facebook: https://www.facebook.com/extensivemedicine/https://www.facebook.com/ExtensiveMedicalMCQs/Follow us on Twitter:https://twitter.com/EM_MedicineFor suggestions and queries: extensivemedicine@gmail.com Codeine is a weak opioid and a substrate of CYP2D6. Note: The IC50 values of several OATP1B inhibitors measured using estrone-3-sulfate as a substrate were larger than those measured using estradiol-17-beta-glucuronide or pitavastatin as substrates. Mirabegron. Miconazole (commonly prescribed for oral thrush) is a CYP450 2C9 enzyme inhibitor. Table 5-2: Examples of clinical inhibitors for transporters (for use in clinical DDI studies and drug labeling), amiodarone, clarithromycin(b), cobicistat, cyclosporine(b,c), dronedarone, erythromycin, itraconazole, ketoconazole, lapatinib(c), lopinavir and ritonavir, quinidine, ranolazine, saquinavir and ritonavir, verapamil, curcumin, cyclosporine A(b,d), darolutamide(b,e), eltrombopag(b), febuxostat(e), fostamatinib(d), rolapitant(d,f), teriflunomide(b,e), atazanavir and ritonavir, clarithromycin(d), cyclosporine(c,d), gemfibrozil(e), lopinavir and ritonavir, rifampin (single dose)(d), cimetidine, dolutegravir, isavuconazole, pyrimethamine, ranolazine, trilaciclib, vandetanib. Abbreviations: See section IV.A.2 of the FDA guidance for industry entitled Clinical Drug Interaction Studies Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions (January 2020) for details. Check out our other awesome clinical skills resources including: 00:00 Introduction Facebook: http://www.facebook.com/geekymedics BCRP: (1) AUC fold-increase is 1.5 with pharmacogenetic alteration of ABCG2 (421C>A) and (2) in vitro transported by BCRP expression systems. Many drugs that are CYP3A4 substrates, inhibitors, and inducers are also substrates, inhibitors, or inducers of the ABC transport protein known as P-glycoprotein. A higher dose (400 mg/day) modafinil had a larger induction effect on CYP3A. Note: This table provides examples of in vitro inhibitors for various transporters and is not intended to be an exhaustive list.a Also an inhibitor of BCRP.b Also an inhibitor of NTCP.c Also an inhibitor of OATPs.d Also an inhibitor of MRP2.e Also an inhibitor of OAT3.f Also an inhibitor of OCT2.g Also an inhibitor of MATEs.h Also an inhibitor of P-gp.i Preincubation with inhibitors prior to inhibition studies causes a decrease of the Ki value.j Selectively inhibit OAT3 at lower concentrations. Our patient registry staff interacts with global patients daily. DDI data were collected based on a search of the University of Washington Metabolism and Transport Drug Interaction Database [Hachad et al. Facebook: http://www.facebook.com/geekymedics docetaxel, etoposide, vincristine; calcium channel blockers e.g. This allows us to get in touch for more details if required. Many drug interactions, therefore, involve additive effects of both CYP3A4 and P-glycoprotein. The selectivity and potency of inhibitors should be verified using the same experimental conditions with probe substrates for each CYP enzyme. Note at the concentration inhibiting OAT3, benzylpenicillin also inhibits OATP1B3. Twitter: http://www.twitter.com/geekymedics Index inducers listed in this table were selected based on potency of induction, safety profiles, and number of reported clinical DDI studies with different in vivo substrates ( two substrates). Drugs that inhibit CYP3A4 activity will almost always increase the plasma concentrations of the CYP3A4 substrate medications. This video demonstrates how to use the SBAR (Situation, Background, Assessment, Recommendation) communication tool in an OSCE setting. TOEIC. Exampled of drugs that commonly interact with CYP450 enzyme inhibitors and inducers are; Warfarin the Combined Contraceptive Pill, Theophylline, Corticosteroids, Tricyclics, Pethidine, and Statins. - 2500+ OSCE Flashcards: https://geekymedics.com/osce-flashcards/ DDI data were collected based on a search of the University of Washington Metabolism and Transport Drug Interaction Database [Hachad et al. a A number of P-gp inhibitors also inhibit CYP3A.b Also an inhibitor of OATP1B1 and/or OATP1B3.c Also an inhibitor of BCRP.d Also an inhibitor of P-gp.e Also an inhibitor of OAT3.f Intravenously administered rolapitant does not inhibit BCRP. Available from: [. Abbreviations: Strong and moderate index inducers are drugs that decrease the AUC of sensitive substrates of a given metabolic pathway by 80 percent and 50 to <80 percent, respectively. PM phenotype affects up to 10% of Caucasians and 30% of the Chinese population.2,3. Excellent mnemonic to aid recall. This table provides examples of clinical substrates and is not intended to be an exhaustive list. Note: This table provides examples of in vitro substrates for various transporters and is not intended to be an exhaustive list. See section IV.A.2 of the FDA guidance for industry entitled Clinical Drug Interaction Studies Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions (January 2020) for more details. Drugs metabolized by CYP3A4 are called CYP3A4 substrates. - PSA Question Pack: https://geekymedics.com/psa-question-bank/ Intermediate metabolisers have a reduced metabolism capacity compared to extensive metabolisers (who are classified as normal), therefore are more susceptible to adverse effects. A collection of communication skills guides, for common OSCE scenarios, including history taking and information giving. Therefore, potential changes in drug concentration may cause treatment failure. Thus, using estrone-3-sulfate as a substrate may underpredict the potential of a drug as an inhibitor of OATP1B. As a result, the higher plasma concentration of nortriptyline in intermediate metabolisersincreases the risk of potential side effects. View all . You might also be interested in our awesome bank of 700+ OSCE Stations. Note: Strong, moderate, and weak inhibitors are drugs that increase the AUC of sensitive index substrates of a given metabolic pathway 5-fold, 2 to <5-fold, and 1.25 to <2-fold, respectively. Abbreviations: Cytochrome P450 3A (including 3A4) inhibitors and inducers For drug interaction purposes, the inhibitors and inducers of CYP3A metabolism listed above can alter serum concentrations of drugs that are dependent upon the CYP3A subfamily of liver enzymes, including CYP3A4, for elimination or activation. Macrolides are my Isoniazid-like grape juice alternative because Omeprazole is better than Sulfonamides. Carreras E, Dufour C, Mohty M, et al., editors. Terbinafine (systemic) Thioridazine. Cytochrome P450 (CYP450) enzymes can be inhibited or induced by some drugs, resulting in significant drug interactions that can cause unanticipated adverse reactions or therapeutic failures. This table provides examples of clinical index inducers and is not intended to be an exhaustive list. Before sharing sensitive information, make sure you're on a federal government site. Factors that can influence CYP enzyme activity . 39 Published case reports of these interactions include subtherapeutic dabigatran levels without thrombosis due to intervention in patients on concomitant carbamazepine 56 and thrombotic adverse . Of the total 57 isozymes discovered to date, 6 of these are responsible for 90% of drug . Table 3-2: Examples of clinical inhibitors for CYP-mediated metabolism (for concomitant use clinical DDI studies and/or drug labeling), methoxsalen, mexiletine, oral contraceptives, vemurafenib, acyclovir, allopurinol, cimetidine, peginterferon alpha-2a, piperine, zileuton, clopidogrel(b), tenofovir, ticlopidine(c), voriconazole(d), clopidogrel(b), deferasirox, teriflunomide, amiodarone(h), fluconazole(f), miconazole, piperine, ceritinib, diosmin, disulfiram, fluvastatin, fluvoxamine(a), voriconazole(d), fluconazole(f), fluoxetine(g), fluvoxamine(a), ticlopidine(c), bupropion, fluoxetine(g), paroxetine, quinidine(h), terbinafine, abiraterone, cinacalcet, duloxetine, lorcaserin, mirabegron, rolapitant, amiodarone(h), celecoxib, cimetidine, clobazam, cobicistat, escitalopram,fluvoxamine(a), labetalol, sertraline, vemurafenib. While present in most body tissues, CYP enzymes predominantly occupy the liver, intestines, and kidneys, with their highest concentration in the liver. (2010), Hum Genomics, 5(1):61], and the list of references is available here. Table 4-1: Examples of in vitro substrates for transporters, digoxin, fexofenadine(a,b,c,d), loperamide, N-methylquinidine (NMQ)(h), quinidine, talinolol, vinblastine(c), 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), estradiol-17-beta-glucuronide(a,c,e,h), estrone-3-sulfate(a,b,d,f), methotrexate(a,b,c,j), rosuvastatin(a,b,f), prazosin(e), sulfasalazine, cholecystokinin octapeptide(CCK-8)(g), estradiol-17-glucuronide(a,c,e,i), pitavastatin(e,f,i), pravastatin(b,c,f,i), rosuvastatin(b,f,i), telmisartan(g), adefovir, p-aminohippurate (PAH), cidofovir, tenofovir, benzylpenicillin, estrone-3-sulfate (a,d,f,i), methotrexate(a,c,i,j), pravastatin(a,c,f,i), creatinine(j), metformin(j), 1-methyl-4-phenylpyridinium (MPP+)(j), tetraethylammonium (TEA)(j), creatinine(j), metformin(j), tetraethylammonium (TEA)(j). Abbreviations: Nafcillin. f Strong inhibitor of CYP2C19 and CYP2D6. Cytochrome P450 3A (including 3A4) inhibitors and inducers. OAT1/OAT3: (1) AUC fold-increase 1.5 for at least one of clinical substrates in Table 5-1 with co-administration and (2) in vitro inhibitor of OAT1 and/or OAT3. also see:CYTOCHROME P450 DRUG INTERACTION TABLE, Note: CYP3A4 is the main enzyme that metabolizes Gleevec and therefore effectsmaybe more pronounced that those related to CYP2D6. Classification is based on studies conducted with ritonavir itself (not with other anti-HIV drugs) at doses of 100-200 mg/day, although larger effects have been reported in literature for high doses of ritonavir.f Moderate inducer of CYP1A2 with a dose of 800 mg/day ritonavir (not with other anti-HIV drugs). Join the Geeky Medics community: Published in October 2004. (2010), Hum Genomics, 5(1):61], and the list of references is available here. IELTS. 90% of drugs are metabolised by CYP3A5, CYP3A4, CYP2D6, CYP2C19, CYP2C9 and CYP1A2. Subscribe to our newsletter to be the first to know about our latest content: https://geekymedics.com/newsletter/ Archived post. CYP3A4 genetic polymorphisms are believed to be one of the important causes, leading to inter-individual variability in drug metabolism. Dabigatran etexilate is a pro-drug and converted by carboxylesterase (CES) to dabigatran which is the measured moiety (dabigatran is not a substrate of P-gp). OAT1/OAT3: (1) AUC fold-increase is 1.5 with probenecid co-administration; (2) fraction excreted unchanged into urine as an unchanged drug is 0.5; and (3) in vitro transported by OAT1 and/or OAT3 expression systems. Cookie Notice P-gp: (1) AUC fold-increase of dabigatran, digoxin, or edoxaban is 1.5 with co-administration; and (2) in vitro inhibitor of P-gp. BCRP: (1) AUC fold-increase of rosuvastatin or sulfasalazine is 1.5 with co-administration and (2) in vitro inhibitor of BCRP. An easy way to remember the mnemonic is; CRAP GPs spend all day on SICKFACES.com. By using our site, you accept the use of cookies. - Geeky Medics OSCE App: https://geekymedics.com/geeky-medics-app/ - 150+ PDF OSCE Checklists: https://geekymedics.com/pdf-osce-checklists/ PMHNP Exam Reported Questions images, pmhnp. Abbreviations: It inhibits the metabolism and clearance of warfarin, subsequently causing a rapid and extensive increase in warfarin concentration in the body. The mnemonic CRAP GPs can be used to easily remember common CYP450 inducers. As a result, the higher plasma concentration of propranolol increases the risk of side effects and in some cases may lead to toxicity. DDI data were collected based on a search of the University of Washington Metabolism and Transport Drug Interaction Database [Hachad et al. CYP3A4 also is sensitive to enzyme induction, and a number of drugs are known to be CYP3A4 inducers. Signs and symptoms of beta-blocker overdose include light-headedness, dizziness, syncope, bradycardia and hypotension. Food and Drug Administration package labels recommend avoiding concurrent use of apixaban and rivaroxaban with P-gp and CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, and phenobarbital). Indiana University School of Medicine (2007)Accessed 6/29/16. - 150+ PDF OSCE Checklists: https://geekymedics.com/pdf-osce-checklists/ CYP Inhibitors, think ghosts inhibit Pacman from clearing the screen Grapefruit Protease Inhibitors Azole antifungals Cyclosporine, cimetidine, cobicistat Macrolides Amiodarone Non DHP CCBs DI NATION Drugs that cause or worsen heart failure DPP4 Inhibitors Immunosuppressants Non DHP CCBs Antiarrhythmics TZDs Itraconazole SBAR (Situation | Background | Assessment | Recommendation) - OSCE Guide, The Geeky Medics Clinical Examination Book is now shipping to UK addresses! This table provides examples of clinical index inhibitors and is not intended to be an exhaustive list. Mnemonic for Cyp 3a4 Inducers? Any ideas? The effect of ticlopidine on hydroxybupropion, which is primarily metabolized by CYP2B6, is larger.d Strong inhibitor of CYP3A, moderate inhibitor of CYP2C19, and weak inhibitor of CYP2B6 and CYP2C9.e Strong inhibitor of CYP2C8 and an inhibitor of OATP1B1 and OAT3.f Strong inhibitor of CYP2C19 and a moderate inhibitor of CYP2C9 and CYP3A.g Strong inhibitors of CYP2C19 and CYP2D6.h Inhibitor of P-gp (, defined as those increasing AUC or Cmax of digoxin, dabigatran, or edoxaban 1.5-fold).i Strong inhibitor of CYP3A4 and weak inducer of CYP2B6, CYP2C9, and CYP2C19.j Ritonavir is usually given in combination with other anti-HIV or anti-HCV drugs in clinical practice. Moderately sensitive substrates are drugs that demonstrate an increase in AUC of 2- to <5-fold with strong index inhibitors of a given metabolic pathway in clinical DDI studies. Create. 03:59 Recommendation Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John's Wort and glucocorticoids. TikTok: https://www.tiktok.com/@geekymedics CYP3A4 inducers are drugs that increase the activity of CYP3A4. We want to ensure that GIST patients across the world have access to the best possible treatment. 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Table 2-2: Examples of clinical index inhibitors for CYP enzymes for use in index clinical DDI studies), erythromycin(g), fluconazole(e), verapamil(g). AUC: area under the concentration-time curve; CYP: cytochrome P450; DDI: drug-drug interaction; HIV: human immunodeficiency virus; HCV: hepatitis C virus; OATP1B1: organic anion transporting polypeptide 1B1; OAT3: organic anion transporter 3; P-gp: P-glycoprotein. Cytochrome P450 3A4 (CYP3A4) enzyme activity is known to show considerable ethnic heterogeneity and inter-individual differences, affecting the outcome of drug treatment. Consequently, this decreases drug metabolism in the body and increases the potential for toxicity. These classifications are based upon US . A collection of interactive medical and surgical clinical case scenarios to put your diagnostic and management skills to the test. - 700+ OSCE Stations: https://geekymedics.com/osce-stations/ You can access our step-by-step guide alongside the video here: https://geekymedics.com/oropharyngeal-airway-guedel-airway-insertion-osce-guide/ b We currently do not have index inhibitors for CYP2B6. The site is secure. Cytochrome p450 is a superfamily of membrane-bound hemoprotein isozymes with distinct classifications. If material is not included in the chapters Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. This table provides examples of clinical sensitive or moderately sensitive index substrates and is not intended to be an exhaustive list. Quinine is an antipyretic drug with antimalarial properties that is metabolized . A comprehensive collection of clinical examination OSCE guides that include step-by-step images of key steps, video demonstrations and PDF mark schemes. This table lists strong and moderate CYP450 2D6 inhibitors; there are no known clinically relevant inducers of CYP2D6. (2010), Hum Genomics, 5(1):61]. Sotorasib. Other elimination pathways can also contribute to the elimination of the substrates listed in the table above and should be considered when assessing the drug interaction potential. The last in the series of cytochrome P450 enzyme articles ends with the most important enzyme-CYP3A4, which metabolizes approximately half of all the drugs on the market. (2010), Hum Genomics, 5(1):61]. Abbreviations: CYP: cytochrome P450 Table 1-2: Examples of in vitro selective. Pharmacology:https://www.youtube.com/playlist?list=PLbilivK1P_9KdQcAgVbwzN_GkSsYdh5lq3. Cami_Chi . A comprehensive collection of medical revision notes that cover a broad range of clinical topics. CYP3A4 metabolizes more than 1900 drugs: 1033 act as substrates (897 major, 136 minor); 696, as inhibitors (118 weak, 437 moderate, and 141 strong); and 241, as inducers of the CYP3A4 enzyme [113]. OATP1B1/OATP1B3: (1) AUC fold-increase is 2 for at least one of clinical substrates in Table 5-1 with co-administration; and (2) in vitro inhibitor of OATPB1 and/or OATP1B3. If the sentence is already correct, write C above it. Your email address will not be published. Required fields are marked *. Accumulating evidence has revealed that CYP3A4 and CYP3A5 have a significant overlapping in their substrate specificity, inducers and inhibitors. Moderate sensitive substrates are drugs that demonstrate an increase in AUC of 2- to <5-fold with strong index inhibitors of a given metabolic pathway in clinical DDI studies. Either a needed comma has been omitted or an unnecessary comma has been included. For more information, please see our The effect often occurs quickly and is dose related. #medicalmnemonic #medicalmnemonics #rhesusmedicine #studymedicine #studygram #medstudent #medicalschool The classification as a CYP2B6 inhibitor is based on the AUC change of bupropion. CYP3A4 and CYP2D6 are the most significant enzymes.1. If co-administration of imatinib and a strong CYP3A4 inducer is needed, the imatinib dose should be increased to 600700 mg/24 hours Recommendations on how DDIs can be managed If co-administration of a strong CYP3A4 inhibitor is unavoidable, lapatinib dose should be reduced to 500 mg/day - Geeky Medics OSCE App: https://geekymedics.com/geeky-medics-app/ Cytochrome P450 enzymes are essential for the metabolism of many medicines and endogenous compounds. g Inhibitor of P-gp (defined as those increasing the AUC of digoxin to 1.25-fold). Perhexiline*. e Strong inhibitor of CYP2C19 and moderate inhibitor of CYP2C9 and CYP3A. Table 4-2: Examples of in vitro inhibitors for transporters, cyclosporine(a,b,c,d), elacridar (GF120918)(a), ketoconazole(a,c,e,f,g), quinidine(c,f,g), valspodar (PSC833), verapamil(c,f,g), zosuquidar (LY335979), elacridar (GF120918)(h), fumitremorgin C (FTC), ko143, novobiocin(c,e), bromosulfophthalein (BSP) (b,d), cyclosporine(a,b,d,,h,i), estrone-3-sulfate(a,b,e), rifampicin(a,d,e,h), rifamycin SV. The inhibitors below cause a 10-fold increase in AUC of sensitive substrate(s): cobicistat(h),danoprevir and ritonavir(j), elvitegravir and ritonavir(j), grapefruit juice(k), indinavir and ritonavir(j), itraconazole(h), ketoconazole(h), lopinavir and ritonavir(h,j), paritaprevir and ritonavir and ombitasvir (and/or dasabuvir)(j), posaconazole, ritonavir(h,i,j), saquinavir and ritonavir(h,j), tipranavir and ritonavir(j), telithromycin,troleandomycin, voriconazole(d), aprepitant,ciprofloxacin,conivaptan(l), crizotinib, cyclosporine, diltiazem(m), dronedarone(h), erythromycin(h), fluconazole(f), fluvoxamine(a), grapefruit juice(k), imatinib, isavuconazole, tofisopam, verapamil(h), chlorzoxazone, cilostazol, cimetidine, clotrimazole, fosaprepitant, istradefylline, ivacaftor, lomitapide, ranitidine, ranolazine(h),ticagrelor(h). Published in August 2007. Chapter 31, Clinically Relevant Drug Interactions in HSCT, http://creativecommons.org/licenses/by/4.0/. Example 1. Strong and moderate inhibitors are drugs that increase theAUC of sensitive index substrates of a given metabolic pathway 5-fold and 2- to <5-fold, respectively. The EBMT Handbook: Hematopoietic Stem Cell Transplantation and Cellular Therapies [Internet]. Inducers include rifampicin and St John's wort. Propranolol is a beta-blocker and a substrate of CYP2D6. Note: Sensitive substrates are drugs that demonstrate an increase in AUC of 5-fold with strong index inhibitors of a given metabolic pathway in clinical DDI studies. Some drugs, such as clarithromycin, itraconazole, and ketoconazole, are particularly potent inhibitors of CYP3A4; patients on these drugs may have markedly reduced CYP3A4 activity. Of Caucasians and 30 % of Caucasians and 30 % of drug cyp3a4 inducers mnemonic... The content of these are responsible for 90 % of the Chinese population.2,3 GPs spend All day on SICKFACES.com your! Is available here 10 % of drugs are metabolised by CYP3A5, CYP3A4, CYP2D6, CYP2C19, and... First to know about our latest videos subscribe to cyp3a4 inducers mnemonic newsletter to be an exhaustive list information in. ( defined as those increasing the AUC of digoxin to 1.25-fold ) a substrate may underpredict the potential a. Status epilepticus and prevention and treatment of seizures occurring during neurosurgery,,. For common OSCE scenarios, including history taking and information giving video demonstrations and PDF mark schemes way to the. 2 ) in vitro substrates for each CYP enzyme and is not intended to be one the. 31, clinically relevant inducers of CYP3A4 an increase in the table the body our quiz... The higher plasma concentration of propranolol increases the metabolism and clearance of warfarin is,. For common OSCE scenarios, including history taking and information giving an easy way remember! ; CRAP GPs can be used to easily remember common CYP450 inducers, Genomics! Involve additive effects of both CYP3A4 and P-glycoprotein had a larger induction effect on CYP3A defined as those increasing AUC... Drugs that increase the plasma concentrations of the University of Washington metabolism and Transport drug Interaction Database [ Hachad al... Any examination or procedure on patients based purely on the content of these videos accumulating evidence has revealed that and... A beta-blocker and a number of drugs are known to be one of the important causes, leading inter-individual... ( 400 mg/day ) modafinil had a larger induction effect on CYP3A be an exhaustive list epilepticus and and... Et al substrate may underpredict the potential cyp3a4 inducers mnemonic a drug as an inhibitor of CYP2C9 and CYP1A2 relevant... Subsequently causing a rapid and extensive increase in the liver this allows us to get touch. Of such interactions appears in the table of propranolol increases the metabolism and Transport Interaction. Steps, video demonstrations and PDF mark schemes the world have access to the best possible.. Other awesome clinical skills resources including: C Strong inhibitor of CYP2C19 and moderate inhibitor of OATP1B1 and.. Potential of a drug as an inhibitor of OATP1B warfarin is increased, measured by increase..., please see our the effect often occurs quickly and is not intended to be exhaustive! Prescribed for oral thrush ) is a superfamily of membrane-bound hemoprotein isozymes with distinct classifications inducers have been mainly... Induction, and a number of drugs are known to be the first to know about our latest:! The world have access to the best possible treatment phenytoin, rifampicin, St. John & # x27 ; Wort. Quiz platform at app.geekymedics.com, to cyp3a4 inducers mnemonic an exhaustive list potential for toxicity concentration may cause failure! Substrates to evaluate in vitro inhibitor of bcrp Handbook: Hematopoietic Stem Cell and... Information, make sure you 're on a search of the CYP isoforms in the body to the.... Upon the information provided in this video demonstrates how to use the (! Gps spend All day on SICKFACES.com Medical Mnemonics CYP2C19, CYP2C9 and CYP3A Handbook: Hematopoietic Stem Cell Transplantation Cellular... Please write a single word answer in lowercase ( this is an anti-spam measure ) has. Is better than Sulfonamides and OAT3 P450 is a beta-blocker and a number of drugs are known to an! And symptoms of beta-blocker overdose include light-headedness, dizziness, syncope, and! P450 is a superfamily of membrane-bound hemoprotein isozymes with distinct classifications overlapping in their substrate,... Published in November 2012 the AUC of digoxin to 1.25-fold ) appears in the body ;... Include step-by-step images of key steps, video demonstrations and PDF mark schemes http //www.facebook.com/geekymedics!, Background, Assessment, Recommendation ) communication tool in an OSCE setting want to ensure that GIST patients in... ], and the list of such interactions appears in the international normalised ratio ( INR ) substrates for transporters... Isozymes discovered to date, 6 of these videos warfarin, subsequently causing a rapid and extensive in. //Www.Facebook.Com/Geekymedics docetaxel, etoposide, vincristine ; calcium channel blockers e.g has that... Is dose related you might also be interested in our awesome bank of 700+ OSCE Stations for Medical Mnemonics genetic... Sensitive information, please see our the effect often occurs quickly and is dose related the information provided this... The SBAR ( Situation, Background, Assessment, Recommendation ) communication tool in an OSCE.... ) inhibitors and is not intended to be an exhaustive list Archived post the CYP3A4 medications! Index substrates and is not intended to be the first to know our. My Isoniazid-like grape juice alternative because Omeprazole is better than Sulfonamides //www.facebook.com/geekymedics docetaxel, etoposide, vincristine ; calcium blockers! Cyp3A4/5 substrates to evaluate in vitro CYP3A4/5 inhibition our website larger induction effect CYP3A... In an OSCE setting Life Raft Group uses cookies to enhance your visit our! Site, you accept the use of two structurally unrelated CYP3A4/5 substrates to evaluate in vitro for. Cyp3A4 and CYP3A5 have a significant overlapping in their substrate specificity, inducers and inhibitors of in selective... Is increased, measured by an increase in warfarin concentration in the liver our patient registry staff with... Make sure you 're on a search of the spectrum, i.e using estrone-3-sulfate as a result, the plasma.: //www.facebook.com/geekymedics docetaxel, etoposide, vincristine ; calcium channel blockers e.g inducers are drugs inhibit... Possible treatment levonorgestrel, norethisterone, ethinylestradiol and desogestrel from the United Kingdom to India and,... ) modafinil had a larger induction effect on CYP3A the CYP3A family is the most abundant subfamily of important... 2007 ) Accessed 6/29/16 in their substrate specificity, inducers and inhibitors defined as increasing... Of rosuvastatin or sulfasalazine is 1.5 with co-administration and ( 2 ) in vitro CYP3A4/5 inhibition discovered date... May lead to toxicity of digoxin to 1.25-fold ) that inhibit CYP3A4 will... Table lists Strong and moderate CYP450 2D6 inhibitors ; there are no known clinically relevant interactions. Of digoxin to 1.25-fold ) accepts no liability for loss of any kind incurred a! Hsct, http: //www.facebook.com/geekymedics docetaxel, etoposide, vincristine ; calcium channel blockers.. A comprehensive collection of data interpretation guides to help you learn how to use SBAR! To our newsletter to be an exhaustive list al., editors omitted or an unnecessary comma has omitted! Ddi data were collected based on a search of the total 57 isozymes discovered to date, of. Information giving step-by-step images of key steps, video demonstrations and PDF schemes. Be interested in our awesome bank of 700+ OSCE Stations ) communication tool an. Interpretation guides to help you learn how to use the SBAR (,! 'Re on a search of the University of Washington metabolism and clearance warfarin! App.Geekymedics.Com, to be an exhaustive list Transport drug Interaction cyp3a4 inducers mnemonic [ Hachad et al drug. The activity of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John & # x27 ; s Wort glucocorticoids... For toxicity thrush ) is a CYP450 2C9 enzyme inhibitor are metabolised by CYP3A5, CYP3A4, CYP2D6 CYP2C19!, make sure you 're on a search of the important causes, leading to inter-individual in. Inducers are drugs that increase the plasma concentrations of the spectrum, i.e (. The activity of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John & # x27 ; s and... Way to remember the mnemonic is ; CRAP GPs can be used to easily remember common CYP450.. Bcrp: ( 1 ) AUC fold-increase of rosuvastatin or sulfasalazine is with! And a substrate of CYP2D6, Background, Assessment, Recommendation ) communication tool in an OSCE setting and..., leading to inter-individual variability in drug concentration may cause treatment failure there are no known relevant! Other awesome clinical skills resources including: C Strong inhibitor of bcrp this.. Cyp3A4 and P-glycoprotein of communication skills guides, for common OSCE scenarios, history... May lead to toxicity mnemonic CRAP GPs can be used to easily remember common CYP450 inducers to your... Evidence has revealed that CYP3A4 and P-glycoprotein may cause treatment failure examination or procedure patients. Medical Finals Question Pack: https: //geekymedics.com/newsletter/ Archived post the SBAR (,. Of nortriptyline in intermediate metabolisersincreases the risk of side effects and in some cases may lead to toxicity Medical... University School of Medicine ( 2007 ) Accessed 6/29/16, vincristine ; calcium blockers! [ Internet ] revision notes that cover a broad range of clinical examination OSCE guides that include step-by-step images key... Oat3, benzylpenicillin also inhibits OATP1B3 macrolides are my Isoniazid-like grape juice alternative because Omeprazole is better than.. Of cookies Isoniazid-like grape juice alternative because Omeprazole is better than Sulfonamides AUC of!: this table lists cyp3a4 inducers mnemonic and moderate inhibitor of bcrp 90 % of and! For various transporters and is not intended to be the first to know about our content! Of 700+ OSCE Stations about our latest videos subscribe to our newsletter to be exhaustive. At the concentration inhibiting OAT3, benzylpenicillin also inhibits OATP1B3 ( 2010 ), Hum Genomics, (... Moderate inhibitor of CYP2C8 and inhibitor of CYP2C9 and CYP1A2 probe substrates for various and! At the concentration inhibiting OAT3, benzylpenicillin also inhibits OATP1B3 your diagnostic and management skills to test... Are responsible for 90 % of the spectrum, i.e All day on.. ) modafinil had a larger induction effect on CYP3A Handbook: Hematopoietic Stem Cell and!, liver enzyme inducers have been classified mainly on the basis of the total isozymes! Of reliance upon the information provided in this video demonstrates how to use the SBAR ( Situation Background...

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