Search references for CYP3A4. Phrases containing CYP3A4
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Enzyme that metabolizes substances by oxidation
(abbreviated CYP3A4) (EC 1.14.14.56) is an important enzyme in the body, mainly found in the liver and the intestine. In humans is encoded by CYP3A4 gene. It
CYP3A4
Medication
substrate for CYP3A4 and hence interacts with CYP3A4 inhibitors and inducers. In addition to being a CYP3A4 substrate, tavapadon is a CYP3A4 inducer and
Tavapadon
Antibiotic
pancytopenia, and organ failure. CYP3A4 is an enzyme that metabolizes many drugs in the liver. Some drugs can inhibit CYP3A4, which means they reduce its
Azithromycin
Medication
Oveporexton is primarily metabolized by the cytochrome P450 enzyme CYP3A4. As such, CYP3A4 inhibitors and inducers can alter oveporexton exposure and hence
Oveporexton
Drug interactions with grapefruit juice
inhibit key drug metabolizing enzymes, such as cytochrome P450 3A4 (CYP3A4). CYP3A4 is a metabolizing enzyme for almost 50% of drugs, and is found in the
Grapefruit–drug_interactions
Medication used to treat insomnia
impairment. Concomitant use of daridorexant with strong CYP3A4 inhibitors and moderate to strong CYP3A4 inducers is not recommended and should be avoided due
Daridorexant
Chemical compound
dehydrogenase (CYP3A4). 6β-hydroxycortisol is used as a biomarker of 6β-hydroxysteroid dehydrogenase (CYP3A4) activity. Drugs that induce CYP3A4 may accelerate
6β-Hydroxycortisol
Antidepressant medication
enzymes, including CYP3A4, CYP2D6, and CYP1A2. Its active metabolite meta-chlorophenylpiperazine (mCPP) is known to be formed by CYP3A4 and metabolized by
Trazodone
Combination drug
serious drug interactions due to strong CYP3A4 inhibition by ergotamine. Ergotamine is a vasoconstrictive CYP3A4 substrate. Bellergal was widely used during
Bellergal
Major active metabolite of ketamine
is the major active metabolite of ketamine, which is formed mainly by CYP3A4. Similarly to ketamine, norketamine acts as a noncompetitive NMDA receptor
Norketamine
Pharmaceutical compound
benzodioxolylbutanamine (BDB) in humans. It is metabolised by the enzymes CYP2D6 and CYP3A4. Substituted α-ethylphenethylamine α-Methyldopamine Meyer MR, Peters FT
Α-Ethyldopamine
Cholesterol-lowering medication
rarely with other CYP3A4 inhibitors, such as amiodarone and aprepitant. Often, bosentan, fosphenytoin, and phenytoin, which are CYP3A4 inducers, can decrease
Atorvastatin
Citrus fruit
inhibit the CYP3A4 enzyme (among others from the cytochrome P450 enzyme family responsible for metabolizing 90% of drugs). The action of the CYP3A4 enzyme
Grapefruit
Medication to treat gastroesophageal reflux disease and other conditions
possible because omeprazole is an inhibitor of the enzymes CYP2C19 and CYP3A4. Clopidogrel is an inactive prodrug that partially depends on CYP2C19 for
Omeprazole
Class of natural products
results. US FDA-approved: Azithromycin – unique; does not extensively inhibit CYP3A4 Clarithromycin Dirithromycin – discontinued but was US FDA approved Erythromycin
Macrolide
American physician and pharmacologist
characterised an inducible form of cytochrome P450 in human liver, later designated CYP3A4, an enzyme now understood to be involved in the metabolism of a large proportion
Paul_B._Watkins
Cough suppressant and dissociative drug
metabolizers. Dextromethorphan is also metabolized by CYP3A4. N-demethylation is primarily accomplished by CYP3A4, contributing to at least 90% of the MEM formed
Dextromethorphan
Antihypertensive drug of the calcium channel blocker class
cells. The substance is metabolised by the liver enzyme CYP3A4. In a study, the strong CYP3A4 inhibitor ketoconazole increased the maximal blood plasma
Lercanidipine
Anticoagulant drug
recommend administering rivaroxaban with drugs known to be strong combined CYP3A4/P-glycoprotein inhibitors because this results in significantly higher plasma
Rivaroxaban
Type of corticosteroid medication
Budesonide is mainly metabolized in the liver by the enzyme CYP3A4. Drugs that are CYP3A4 inhibitors such as ketoconazole, clarithromycin, ritonavir,
Budesonide
Enzyme involved in drug metabolism
expressed as a 52.5-kD protein, whereas CYP3A4 migrates as a 52.0-kD protein. The human CYP3A subfamily, CYP3A4, CYP3A5, CYP3A7 and CYP3A43, is one of
CYP3A5
Chemical compound
agonist of the human pregnane X receptor ligand-binding domain and to induce CYP3A4 expression in vitro. Shukla SJ, Sakamuru S, Huang R, Moeller TA, Shinn P
Metacycline
Dissociative anesthetic and anti-depressant
body, ketamine undergoes extensive metabolism. It is biotransformed by CYP3A4 and CYP2B6 isoenzymes into norketamine, which, in turn, is converted by
Ketamine
Medication against high blood pressure
inhibitors, by nature of inhibiting the enzyme that metabolizes amlodipine, CYP3A4, are one such class of drugs. Others include the calcium-channel blocker
Amlodipine
Chemical compound
cytochrome P450 enzyme CYP3A4. Thus the potential exists for adverse drug interactions with other drugs that induce or inhibit CYP3A4. Specifically, the concomitant
Eplerenone
Antiretroviral medication
is a highly potent inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme. By inhibiting CYP3A4, ritonavir prevents the metabolic breakdown of co-administered
Ritonavir
Opioid drug used in pain relief
oxycodone. Hydrocodone is metabolized by the cytochrome P450 enzymes CYP2D6 and CYP3A4, and inhibitors and inducers of these enzymes can modify hydrocodone exposure
Hydrocodone
Chemical compound
N-phenethylnormorphine. with its formation from morphine catalyzed by the liver enzymes CYP3A4 and CYP2C8. Normorphine is a controlled substance listed under the Single
Normorphine
Anxiolytic medication
schizophrenia. Tofisopam has been shown to act as an inhibitor of the liver enzyme CYP3A4, and some researches suspect that this could cause dangerous drug interactions
Tofisopam
Chemical compound
levomethorphan, and has been shown to produce local anesthetic effects. It is the CYP3A4 metabolite of the aforementioned drugs, and is itself metabolized by the
3-Methoxymorphinan
Medication used to treat insomnia
strong CYP3A4 inhibitors is not recommended due to potential for increased suvorexant exposure while concomitant use of suvorexant with strong CYP3A4 inducers
Suvorexant
Chemical compound
and is partially metabolized by CYP3A4 and CYP1A2. Dose adjustments may be necessary if people are treated with CYP3A4 and CYP1A2 inhibitors and medications
Cinacalcet
ISOZYMES". "The Life Raft Group: Long List of Inhibitors and Inducers of CYP3A4 and CYP2D6". "DRUGBANK Online: Cytochrome P-450 Enzyme Inhibitors". "MEDICATIONS
List of cytochrome P450 modulators
List_of_cytochrome_P450_modulators
Short-acting barbiturate
Pentobarbital is a short-acting barbiturate typically used as a sedative, a preanesthetic, and to control convulsions in emergencies. It can also be used
Pentobarbital
Glucocorticoid medication
Fluticasone propionate is broken down by CYP3A4 (cytochrome P450 3A4), and has been shown to interact with strong CYP3A4 inhibitors such as ritonavir and ketoconazole
Fluticasone_propionate
Non-opioid analgesic drug
studies comparing suzetrigine with high-dose opioids. Suzetrigine exhibits CYP3A4-mediated drug interactions and there is limited long-term data regarding
Suzetrigine
Chemical compound
P-glycoprotein (P-gp) and CYP3A4. Hence P-gp and CYP3A4 inhibitors may increase plasma levels of bosutinib. Likewise CYP3A4 inducers may reduce plasma
Bosutinib
Benzodiazepine
alleviating anxiety at one week follow-up. Mexazolam is metabolised via the CYP3A4 pathway. HMG-CoA reductase inhibitors including simvastatin, simvastatin
Mexazolam
Chemical compound
cimetidine inhibits the breakdown of the sulfoxide by interfering with CYP3A4. The half-life of the sulfoxide metabolite thus increases from 7.4 hours
Albendazole
Calcium channel blocker medication
infarction, and hepatotoxicity. Because of its inhibition of hepatic cytochromes CYP3A4, CYP2C9 and CYP2D6, there are a number of drug interactions. Some of the
Diltiazem
Chemical compound
the liver by the cytochrome P450 enzyme CYP3A4. When administered concomitantly with drugs that inhibit CYP3A4, such as ketoconazole, the metabolism of
Solifenacin
Chemical compound
Cilostazol is metabolized by CYP3A4 and CYP2C19, two isoenzymes of the cytochrome P450 system. Drugs that inhibit CYP3A4, such as itraconazole, erythromycin
Cilostazol
Toxic plant alkaloid
metabolism. The results indicate that aconitine was mainly metabolized by CYP3A4, 3A5 and 2D6. CYP2C8 and 2C9 had a minor role to the aconitine metabolism
Aconitine
Medication for migraine headache acute treatment
mouth. Ubrogepant is contraindicated for co-administration with strong CYP3A4 inhibitors. Ubrogepant, also known as MK-1602, was discovered by scientists
Ubrogepant
Vasodilating drug
system, particularly CYP3A4. The potential exists for adverse drug interactions with other drugs which inhibit or induce CYP3A4, including HIV protease
PDE5_inhibitor
Active metabolite of Δ9-THC
metabolized inside the body by cytochrome P450 enzymes such as CYP2C9 and CYP3A4 into 11-hydroxy-THC and then further metabolized by dehydrogenase[which
11-Hydroxy-THC
Compound that activates dopamine receptors
metabolized by CYP3A4 enzyme concentration rises with the use of CYP3A4 inhibitors. For example, in one study bromocriptine was given with a CYP3A4 inhibitor
Dopamine_agonist
Antiarrhythmic medication
predominantly by CYP3A4 enzymes predominantly in the liver and GI tract. This means that it is likely to interact with drugs that inhibit CYP3A4, such as erythromycin
Dofetilide
Human gene
cytochrome P450 superfamily of genes. The CYP3A cluster consists of four genes: CYP3A4, CYP3A5, CYP3A7, and CYP3A43. The region also contains four pseudogenes:
CYP3A
Coronary medication
other adverse effects. Ticagrelor is a weak CYP3A4 inhibitor and can increase the plasma concentration of CYP3A4 substrates Current evidence suggests that
Ticagrelor
Medication for chronic obstructive pulmonary disease
Fluticasone furoate is metabolized by cytochrome P450 3A4 (CYP3A4). Medications that are inhibitors of CYP3A4 (e.g. ketoconazole) may decrease fluticasone's metabolism
Fluticasone furoate/umeclidinium bromide/vilanterol
Fluticasone_furoate/umeclidinium_bromide/vilanterol
Atypical antipsychotic medicine
cytochrome P450 3A4 isoenzyme (CYP3A4), with some minor metabolism by CYP2D6. Cariprazine does not induce the production of CYP3A4 or CYP1A2 in the liver, and
Cariprazine
Blood pressure medication
about 33%. Metabolism is primarily by cytochrome P450 isoenzymes CYP2C9 and CYP3A4. Peak plasma concentrations of losartan and EXP3174 occur about one hour
Losartan
Investigational selective androgen receptor modulator
CYP3A4 and the UDP-glucuronosyltransferase (UGT) enzymes UGT1A1 and UGT2B7. It shows very minimal metabolism by cytochrome P50 enzymes, with CYP3A4 merely
Enobosarm
Antiarrhythmic medication
warfarin depend on metabolism of warfarin by both cytochromes CYP2C9 and CYP3A4, coadministation leads to rise in international normalized ratio (INR)—the
Amiodarone
Chemical compound
CYP3A4 inhibitors may increase levels of apalutamide or its major active metabolite N-desmethylapalutamide, while mild to moderate CYP2C8 or CYP3A4 inhibitors
Apalutamide
Protein-coding gene in the species Homo sapiens
in size and shares 87% of its sequence with CYP3A4. It carries out a similar role in fetuses that CYP3A4 serves in adults. The gene location is 7q22.1
CYP3A7
Medication used to treat anxiety disorders
cocaine. Buspirone has been shown in vitro to be metabolized by the enzyme CYP3A4. This finding is consistent with the in vivo interactions observed between
Buspirone
Triazolobenzodiazepine
by CYP2B6, CYP2C19, and CYP3A4. 4-hydroxy bromazolam, as well as α-hydroxy bromazolam, were formed by CYP2B6, CYP2C19, CYP3A4, and CYP3A5. Additionally
Bromazolam
Peripheral D2 receptor antagonist
exclusively metabolized by CYP3A4/5, though minor contributions by CYP1A2, CYP2D6, and CYP2C8 have been reported. CYP3A4 is the major enzyme involved
Domperidone
Chemical compound
Amentoflavone can interact with many medications by being a potent inhibitor of CYP3A4 and CYP2C9, which are enzymes responsible for the metabolism of some drugs
Amentoflavone
Beta-1 selective adrenenergic blocker medication used to treat cardiovascular diseases
Bioavailability >90% Protein binding 30% Metabolism 50% liver, CYP2D6, CYP3A4 Elimination half-life 10–12 hours Excretion Kidney, fecal (<2%) Identifiers
Bisoprolol
Antidepressant medication
inhibitors or inducers of the cytochrome P450 isoenzymes CYP1A2, CYP2D6, or CYP3A4 can result in altered concentrations of mirtazapine, as these are the main
Mirtazapine
Chemical compound
Naringin inhibits some drug-metabolizing cytochrome P450 enzymes, including CYP3A4 and CYP1A2, which may result in drug-drug interactions. Ingestion of naringin
Naringin
Chemical compound
limited use because they are metabolized by CYP3A4 may become viable medications when taken with a CYP3A4 inhibitor because the dose required to achieve
Bergamottin
Species of plant
Silybum marianum is a species of thistle. It has various common names including milk thistle, blessed milkthistle, Marian thistle, Mary thistle, Saint
Silybum_marianum
Antihistamine medication
retention, dry mouth, blurred vision). Substances that act as inhibitors of the CYP3A4 enzyme such as ketoconazole, erythromycin, cimetidine, and furanocoumarin
Loratadine
Chemical compound
CYP7B1 (steroid 7α-hydroxylase) in tissues such as the prostate gland and by CYP3A4 in the liver. The major metabolic pathway of DHEA outside the liver is via
7α-Hydroxy-DHEA
Class of compounds
CYP3A4 enzyme, so concurrent use is not recommended as it may increase the plasma levels of the Alpha-1 blockers which are metabolised by the CYP3A4 enzyme
Alpha-1_blocker
Antidepressant pharmacology hypotheses
(strong) CYP3A4 (weak–moderate) Fluvoxamine 53% 18 25 100–200 3–8 hr 80% Urine (85%) CYP2D6 CYP1A2 CYP3A4 CYP2C9 CYP1A2 (strong) CYP2C9 (moderate) CYP3A4 (weak)
Pharmacology of antidepressants
Pharmacology_of_antidepressants
Substance derived from opium
duration of effect are longer than morphine. It is metabolized in the liver by CYP3A4 enzymes to the compound norfentanyl. Heroin, the common name for diacetylmorphine
Opiate
Chemical compound
Rufinamide is an anticonvulsant medication. It is used in combination with other medication and therapy to treat Lennox–Gastaut syndrome and various other
Rufinamide
Chemical compound
Pioglitazone, sold under the brand name Actos among others, is an anti-diabetic medication used to treat type 2 diabetes. It may be used with metformin
Pioglitazone
Medication of the calcium channel blocker type
3A4, so substances that inhibit or activate CYP3A4 can strongly effect how much felodipine is present. CYP3A4 inhibitors, which increase the amount of felodipine
Felodipine
Steroid medication
of the liver enzyme CYP3A4 speed up metabolization of triamcinolone and can therefore reduce its effectiveness. Conversely, CYP3A4 inhibitors, such as
Triamcinolone
Lysergamide
CA: Schedule VI US: ℞-only Pharmacokinetic data Metabolism Liver (partly CYP3A4) Elimination half-life 2-phase (10 min; 2 hrs) Excretion Bile duct Identifiers
Ergonovine
Chemical compound, antibiotic
Norfloxacin, sold under the brand name Noroxin among others, is an antibiotic that belongs to the class of fluoroquinolone antibiotics. It is used to treat
Norfloxacin
Opioid medication
to inhibition of CYP3A4 and CYP2D6. Rifampicin greatly reduces plasma concentrations of oxycodone due to strong induction of CYP3A4. There is also a case
Oxycodone
Antibiotic medication
clarithromycin is excreted in human milk. Clarithromycin inhibits a liver enzyme, CYP3A4, involved in the metabolism of many other commonly prescribed drugs. Taking
Clarithromycin
Biopharmaceutical drug
and during pregnancy. Substances that strongly inhibit the liver enzyme CYP3A4, such as ketoconazole, itraconazole, or clarithromycin, increase upadacitinib
Upadacitinib
Chemical compound
function. Abiraterone acetate is a CYP3A4 substrate and hence should not be administered concurrently with strong CYP3A4 inhibitors such as ketoconazole
Abiraterone_acetate
Pharmaceutical drug
the P-gp substrate digoxin by 70%. Strong inducers of the liver enzyme CYP3A4 decrease the area under the curve of rolapitant and its active metabolite
Rolapitant
Quaternary ammonium cation
diarrhea as common issues. Berberine is known to inhibit the activity of CYP3A4, an enzyme important to drug metabolism and clearance of endogenous substances
Berberine
Chemical compound
formed from hydrocodone in the liver via N-demethylation predominantly by CYP3A4. Unlike hydromorphone, a minor metabolite of hydrocodone, norhydrocodone
Norhydrocodone
Medication for overactive bladder
amide hydrolysis, and minimal oxidative metabolism in vivo by CYP2D6 and CYP3A4. Some involvement of butylcholinesterase Elimination half-life 50 hours
Mirabegron
Chemical compound
inhibitor of CYP3A4, aprepitant can increase plasma concentrations of co-administered medicinal products that are metabolized through CYP3A4. Specific interaction
Aprepitant
Chemical compound
OATP1B3. It is partly degraded by the liver enzymes CYP2B6, CYP2C8 and CYP3A4. Substances that are transported or inactivated by these proteins, or interfere
Velpatasvir
Chemical compound
formed from oxycodone in the liver via N-demethylation predominantly by CYP3A4. Noroxycodone binds to and activates the μ-opioid receptor (MOR) similarly
Noroxycodone
Anticonvulsant medication
oxcarbazepine and licarbazepine are CYP3A4 and CYP3A5 inducers and thus have the potential to decrease the plasma concentration of CYP3A4 and CYP3A5 substrates, including
Oxcarbazepine
Chemical compound
increased concentrations of drugs that are metabolized by the liver enzymes CYP3A4 and CYP2C9, because miconazole inhibits these enzymes. Such interactions
Miconazole
Opioid treatment
inhibitors of the liver enzyme CYP3A4, such as ketoconazole, moderately increase buprenorphine concentrations; CYP3A4 inducers can theoretically decrease
Buprenorphine/naloxone
Class of drugs to lower cholesterol
bergamottin and dihydroxybergamottin) inhibit the cytochrome P450 enzyme CYP3A4, which is involved in the metabolism of most statins (however, it is a major
Statin
Antihypertensive drug of the calcium channel blocker class
enzyme CYP3A4. Consequently, CYP3A4 inducers such as rifampicin or carbamazepine could reduce the effectiveness of nisoldipine, while CYP3A4 inhibitors
Nisoldipine
Chemical compound
carbamazepine (in descending order of inhibition) due to their effects on the CYP3A4 enzyme. Zonisamide is not known to inhibit cytochrome P450 enzymes when
Zonisamide
Kinase inhibitor for treatment of non-small-cell lung cancer
the liver enzymes CYP3A4/5 if it can be avoided, as serious cases of liver toxicity have been observed under combination with the CYP3A4/5 inducer rifampicin
Lorlatinib
Benzodiazepine medication
including CYP3A4. Erythromycin, clarithromycin, ritonavir, itraconazole, ketoconazole, nefazodone, cimetidine, and grapefruit juice are inhibitors of CYP3A4 and
Clonazepam
COX-2 selective NSAID medication
Protein binding 92% Metabolism Liver, CYP extensively involved (mainly CYP3A4) Elimination half-life 22 hours Excretion Kidney (70%) and fecal (20%) Identifiers
Etoricoxib
Antihistamine medication
High Protein binding 91–92% Metabolism Minimal (less than 14%, primarily CYP3A4) Elimination half-life 8 to 9 hours Excretion Urine: 85% Feces: 12.9% Identifiers
Levocetirizine
Phenomenon of drug metabolism
and thus the bioavailability of the drug. Cytochromes P450, especially CYP3A4, play a crucial role in first-pass metabolism, affecting the bioavailability
First_pass_effect
NRI antidepressant drug
reliance on CYP3A4, reboxetine O-desethylation is markedly inhibited by papaverine and ketoconazole. It weakly inhibits CYP2D6 and CYP3A4. Reboxetine
Reboxetine
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CYP3A4
CYP3A4
CYP3A4
CYP3A4
CYP3A4
CYP3A4
CYP3A4
CYP3A4
CYP3A4
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