Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14.13.97), a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. The Human Genome Organisation (HUGO is an organization involved in the Human Genome Project, a project about mapping the human genome HomoloGene, a tool of the National Center for Biotechnology Information (NCBI is a system for automated detection of homologs (similarity attributable to descent This article is about the Enzyme Commission codes For the European Commission system for coding chemicals see EC-No. The Entrez Global Query Cross-Database Search System is a powerful Federated search engine or Web portal that allows users to search many discrete Health sciences Ensembl is a joint scientific project between the European Bioinformatics Institute and the Wellcome Trust Sanger Institute, which was launched in 1999 in response to the imminent UniProt is the uni versal prot ein resource a central repository of Protein data created by combining Swiss-Prot, TrEMBL PubMed is a free search engine for accessing the MEDLINE database of citations and abstracts of biomedical research articles This article is about the Enzyme Commission codes For the European Commission system for coding chemicals see EC-No. Cytochrome P450 (abbreviated CYP, P450, infrequently CYP450) is a very large and diverse superfamily of Hemoproteins found in all Domains A xenobiotic is a Chemical which is found in an Organism but which is not normally produced or expected to be present in it CYP3A4 is involved in the oxidation of the largest range of substrates of all the CYPs. Cytochrome P450 (abbreviated CYP, P450, infrequently CYP450) is a very large and diverse superfamily of Hemoproteins found in all Domains CYP3A4 is also, correspondingly, present in the largest quantity of all the CYPs in the liver. The liver is a vital organ in the human body and is present in Vertebrates and some other animals
Fetuses do not express CYP3A4 in their liver/tissues; but rather CYP3A7, which acts on a similar range of substrates. A fetus (or foetus or fœtus) is a developing Mammal or other Viviparous Vertebrate, after the Embryonic stage and CYP3A7 is a member of the Cytochrome P450 family It serves in fetuses a role similar to the role CYP3A4 serves in adults CYP3A7 is gradually replaced by CYP3A4 in the developing neonate.
Distribution
Although CYP3A4 is predominantly found in the liver, it is also present in other organs and tissues of the body where it may play an important role in metabolism. CYP3A4 in the intestine plays an important role in the metabolism of certain drugs. Often this allows prodrugs to be activated and absorbed - as in the case of the histamine H1-receptor antagonist terfenadine. A prodrug is a pharmacological substance ( drug) that is administered in an inactive (or significantly less active form A histamine antagonist is an agent which serves to inhibit the release or action of Histamine. Terfenadine is an Antihistamine formerly used for the treatment of allergic conditions
Recently CYP3A4 has also been identified in the brain, however its role in the CNS is still unknown. [1]
Variability
While over 28 single nucleotide polymorphisms (SNPs) have been identified in the CYP3A4 gene, it has been found that this does not translate into significant interindividual variability in vivo. A single nucleotide polymorphism ( SNP, pronounced snip) is a DNA sequence variation occurring when a single Nucleotide - A, T It can be supposed that this may be due to the induction of CYP3A4 on exposure to substrates.
Variability in CYP3A4 function can be determined noninvasively by the erythromycin breath test (ERMBT). The erythromycin breath test (ERMBT is a method used to measure Metabolism (oxidation and elimination from the system by a part of the Cytochrome P450 system The ERMBT estimates in vivo CYP3A4 activity by measuring the radiolabelled carbon dioxide exhaled after an intravenous dose of (14C-N-methyl)-erythromycin. In vivo ( Latin: within the living means that which takes place inside an organism. Carbon dioxide ( Chemical formula:) is a Chemical compound composed of two Oxygen Atoms covalently bonded to a single Intravenous therapy or IV therapy is the giving of Liquid substances directly into a Vein. Erythromycin is a Macrolide Antibiotic that has an antimicrobial spectrum similar to or slightly wider than that of Penicillin, and is often used for people [2]
Induction
CYP3A4 is induced by a wide variety of ligands. Enzyme inhibitors are Molecules that bind to Enzymes and decrease their activity. In Chemistry, a ligand is either an Atom, Ion, or Molecule (see also Functional group) that bonds to a central metal generally These ligands bind to the Pregnane X Receptor (PXR). In the field of Molecular biology, the pregnane X receptor ( PXR) also known as NR1I2 (nuclear receptor subfamily 1 group I member 2 is a nuclear The activated PXR complex forms a heterodimer with the Retinoid X Receptor (RXR) which binds to the XREM region of the CYP3A4 gene. The retinoid X receptor ( RXR) is a type of Nuclear receptor which is activated by 9-cis retinoic acid. XREM is a regulatory region of the CYP3A4 gene, and binding causes a cooperative interaction with proximal promoter regions of the gene, resulting in increased transcription and expression of CYP3A4.
CYP3A4 ligands
Selected inducers, inhibitors and substrates of CYP3A4[3]| Substrates | Inhibitors | Inducers |
|---|
| Often mentioned: [4] Other: - protease inhibitors
- Mirtazapine (NaSSA)
- nefazodone (5-HT2A receptor antagonist)
- pimozide (antipsychotic)
- reboxetine (antidepressant)
- zopiclone (hypnotic)
- non-nucleoside reverse transcriptase inhibitors
- alfentanil (analgesic)
- budesonide (glucocorticoid)
- donepezil (acetylcholinesterase inhibitor)
- esomeprazole (proton pump inhibitor)
- omeprazole (proton pump inhibitor)
- finasteride (antiandrogen)
- glibenclamide (antidiabetic)
- cisapride (5-HT4 receptor agonist)
- terfenadine (H1-receptor antagonist)
- toremifene (SERM)
- barbiturates
- carbamazepine (anticonvulsant, mood stabilizing)
- codeine (analgesic, antitussive, antidiarrheal)
- dextromethorphan (antitussive)
- digoxin (Antiarrhythmic)
- ergot alkaloids (circulation, neurotransmission)
- estradiol (sex hormone)
- fentanyl (analgesic)
- ivabradine (in angina pectoris)
- levonorgestrel (hormonal contraceptive)
- lidocaine (local anesthetic, antiarrhythmic)
- methadone (analgesic, anti-addictive)
- mifepristone (abortifacient)
- montelukast (leukotriene receptor antagonist)
- ondansetron (5-HT3 antagonist)
- paracetamol (analgesic, antipyretic)
- quinidine (class I antiarrhythmic)
- quinine (antipyretic, anti-smallpox, analgesic)
- testosterone (androgen)
- theophylline (stimulant)
- valproate (anticonvulsant, mood-stabilizing)
- warfarin (anticoagulant)
- tetrahydrocannabinol (psychoactive)
- Antipsychotics
- Aripiprazole
- Risperidone
- Ziprasidone
| Strong: [5] unspecified: | Often mentioned: [4] Other: |
References
- ^ Robertson G, Field J, Goodwin B, Bierach S, Tran M, Lehnert A, Liddle C (2003). Calcium channel blockers are a class of drugs and natural substances with effects on many excitable cells of the body like the muscle of the Heart, smooth muscles Diltiazem is a member of the group of drugs known as Benzothiazepines which are a class of Calcium channel blockers used in the treatment of Hypertension Nifedipine (brand name Adalat, Nifedical, and Procardia) is a Dihydropyridine Calcium channel blocker. Felodipine is a Calcium channel blocker (calcium antagonist a drug used to control Hypertension (high blood pressure Verapamil (brand names Isoptin, Verelan, Calan, Bosoptin, Covera-HS) is an L-type Calcium channel blocker. An immunosuppressant is a substance that performs Immunosuppression of the Immune system. Ciclosporin (ˌsaɪkləˈspɔrən cyclosporine ( USAN) or cyclosporin (former BAN) is an Immunosuppressant drug widely Tacrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after allogenic Organ transplant to reduce the Sirolimus ( INN) is a relatively new immunosuppressant drug used to prevent rejection in organ transplantation, and is especially useful in Kidney Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer. Cyclophosphamide (the generic name for Cytoxan Neosar Revimmune also known as cytophosphane is a Nitrogen mustard alkylating agent, from the oxazophorines group Docetaxel is a clinically well established anti-mitotic Chemotherapy Doxorubicin ( INN,; trade name Adriamycin; also known as hydroxydaunorubicin) is a drug used in cancer Chemotherapy. Etoposide phosphate (brand names Eposin, Etopophos, Vepesid, VP-16) is an inhibitor of the Enzyme Topoisomerase II. Ifosfamide (pronounced eyefos'famide (also marketed as Mitoxana and Ifex) is a Nitrogen mustard alkylating agent used in Paclitaxel is a Mitotic inhibitor used in Cancer Chemotherapy. Tamoxifen is an orally active Selective estrogen receptor modulator (SERM that is used in the treatment of Breast cancer and is currently the world's largest Teniposide ( Vumon, VM-26) is a chemotherapeutic Medication mainly used in the treatment of childhood Acute lymphocytic leukemia. Vinblastine is an anti-mitotic drug used to treat certain kinds of Cancer, including Hodgkin's lymphoma, non-small cell Lung cancer Vindesine is an anti-mitotic Vinca alkaloid used in Chemotherapy. Gefitinib ( INN) (gɛˈfɪtɨnɪb (originally coded ZD1839 is a drug used in the treatment of certain types of Cancer. The benzodiazepines (pronounced, often abbreviated to "benzos") are a class of Psychoactive drugs with varying Hypnotic Flunitrazepam (ˌfluːnaɪˈtræzəpæm is a highly potent Hypnotic drug with powerful Sedative, Anxiolytic, Amnestic, and Skeletal Midazolam (marketed under brand names Dormicum, Flormidal, Versed, Hypnovel and Dormonid, pronounced mɪˈdæzəlæm Alprazolam, also known under the trade names Xanax and Niravam, is a short-acting drug of the Benzodiazepine class used to treat moderate Triazolam (marketed under brand names Halcion, Novodorm, Songar) is a Benzodiazepine derivative drug Clonazepam (marketed by Roche under the trade-names Klonopin in the United States and Rivotril, Ravotril or Rivatril in Europe South An antifungal drug is Medication used to treat fungal Infections such as Athlete's foot, Ringworm, Candidiasis (thrush Ketoconazole is a synthetic Antifungal drug used to prevent and treat skin and fungal infections especially in immunocompromised patients such as those Itraconazole (marketed as Sporanox by Janssen Pharmaceutica) invented in 1984 is a Triazole Antifungal agent that is prescribed to patients Clotrimazole is an Antifungal medication commonly used in the treatment of fungal infections of both humans and animals such as vaginal yeast infections and Tricyclic antidepressants (abbreviation TCAs) are a class of Antidepressant drugs first used in the 1950s Amitriptyline (or Amitryptyline) hydrochloride (sold as Elavil Tryptanol Endep Elatrol Tryptizol Trepiline Laroxyl Saroten is a Tricyclic antidepressant Imipramine (sold as Antideprin, Deprenil, Deprimin, Deprinol, Depsonil, Dynaprin, Eupramin, Imipramil Clomipramine (brand-name Anafranil) is a Tricyclic antidepressant. The macrolides are a group of drugs (typically Antibiotics) whose activity stems from the presence of a macrolide ring, a large macrocyclic Erythromycin is a Macrolide Antibiotic that has an antimicrobial spectrum similar to or slightly wider than that of Penicillin, and is often used for people Clarithromycin is a Macrolide Antibiotic used to treat Pharyngitis, Tonsillitis, acute maxillary Sinusitis, acute bacterial exacerbation Selective serotonin reuptake inhibitors ( SSRIs) are a class of Antidepressants used in the treatment of depression, Anxiety disorders Citalopram is an Antidepressant drug used to treat major depression associated with Mood disorders It is also used on occasion in the treatment The statins (or HMG-CoA reductase inhibitors) form a class of hypolipidemic drugs used to lower Cholesterol levels in people with or at risk of Cardiovascular Atorvastatin ( INN) (əˌtɔrvəˈstætən (marketed under the name Lipitor, Lipidra Aztor Torvatin Sortis Torvast Torvacard Totalip Tulip Xarator Lovastatin is a member of the drug class of Statins used for lowering Cholesterol ( Hypolipidemic agent) in those with Hypercholesterolemia and Simvastatin ( INN) (ˈsɪmvəstætɨn (marketed under the trade names Zocor, Simvastatin Simlup Simcard and others is a hypolipidemic drug belonging A phosphodiesterase type 5 inhibitor, often shortened to PDE5 inhibitor, is a drug used to block the degradative action of Phosphodiesterase type 5 on Sildenafil citrate, sold as Viagra, Revatio and under various other trade names is a drug used to treat Erectile dysfunction (male impotence Buspirone (brand-names Ansial, Ansiced, Anxiron, Axoren, Bespar, BuSpar, Buspimen, Buspinol, An anxiolytic is a drug prescribed for the treatment of Symptoms of Anxiety. Haloperidol is a Typical antipsychotic. It is in the Butyrophenone class of Antipsychotic medications and has pharmacological effects similar Antipsychotics are a group of Psychoactive drugs commonly but not exclusively used to treat Psychosis, which is typified by Schizophrenia. Venlafaxine (Effexor Efexor is an Antidepressant of the Serotonin-norepinephrine reuptake inhibitor (SNRI class first introduced by Wyeth in 1993 Serotonin-norepinephrine reuptake inhibitors (SNRIs are a class of Antidepressant used in the treatment of major depression and other mood disorders Amiodarone is an Antiarrhythmic agent (medication used for irregular heart beat used for various types of tachyarrhythmias (fast forms of irregular heart beat both ventricular Antiarrhythmic agents are a group of Pharmaceuticals that are used to suppress fast rhythms of the Heart ( Cardiac arrhythmias) such as Atrial fibrillation Ethinylestradiol, also ethinyl estradiol (EE is a Derivative of Estradiol. Hormonal contraception refers to Birth control methods that act on the hormonal system A kinin is any of various structurally related Polypeptides, such as Bradykinin and Kallikrein. Smooth muscle is a type of non- Striated muscle, found within the Tunica media layer of large and small Arteries and Veins, the bladder For natural protease inhibitors please see Protease inhibitor (biology Protease inhibitors (PIs are a class of Medications used Indinavir (IDV trade name Crixivan, manufactured by Merck) is a protease inhibitor used as a component of highly active antiretroviral therapy Ritonavir, with trade name Norvir Saquinavir is an Antiretroviral drug used in HIV therapy It falls in the protease inhibitor class Nelfinavir ( Viracept) is an Antiretroviral drug used in the treatment of the Human immunodeficiency virus (HIV Mirtazapine is an Antidepressant introduced by Organon International in 1994 used for the treatment of moderate to severe depression. Noradrenergic and selective serotonergic antidepressants (abbreviated NaSSAs) are a relatively new class of Antidepressants They are thought to work by blocking presynaptic Nefazodone hydrochloride (trade name Serzone, Nefadar) is an Antidepressant drug marketed by Bristol-Myers Squibb. The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor which belongs to the Serotonin receptor family and is a G protein coupled receptor Pimozide (sold as Orap) is an Antipsychotic drug. It was discovered at Janssen Pharmaceutica in 1963. Antipsychotics are a group of Psychoactive drugs commonly but not exclusively used to treat Psychosis, which is typified by Schizophrenia. Reboxetine is an Antidepressant drug used in the treatment of Clinical depression, Panic disorder and ADD/ADHD, developed by Pharmacia (now An antidepressant is a Psychiatric medication used for alleviating major depression or Dysthymia ('milder' depression Zopiclone (pronunciation perhaps ˈzɒpɪkloʊn sold as Imovane and Zimovane in Europe and Canada and as the Eszopiclone analogue Lunesta For the state of mind see Hypnosis. Hypnotic drugs induce Sleep (which differentiates them from the Sedative Reverse transcriptase inhibitors (RTIs are a class of Antiretroviral drug used to treat HIV infection Tumors, and Cancer. Nevirapine, also marketed under the trade name Viramune ( Boehringer Ingelheim) is a non-nucleoside Reverse transcriptase inhibitor (NNRTI used to treat Alfentanil (trade name Alfenta) is a potent but short-acting synthetic Opioid Analgesic drug, used for Anaesthesia in Surgery Budesonide is a Glucocorticoid Steroid for the treatment of Asthma, non-infectious Rhinitis (including Hay fever and other allergies Glucocorticoids (GC are a class of Steroid hormones characterised by an ability to bind with the glucocorticoid receptor ( GR) and trigger similar effects Donepezil (also used incorrectly as Donezepil marketed under the trade name Aricept ( Eisai) ( Pfizer) is a centrally acting reversible Acetylcholinesterase An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the Cholinesterase enzyme from breaking down Acetylcholine Proton pump inhibitors (or "PPI"s are a group of drugs whose main action is pronounced and long-lasting reduction of Gastric acid production Omeprazole ( INN) (oʊˈmɛprəzoʊl is a Proton pump inhibitor used in the treatment of Dyspepsia, peptic ulcer disease (PUD Gastroesophageal Proton pump inhibitors (or "PPI"s are a group of drugs whose main action is pronounced and long-lasting reduction of Gastric acid production Finasteride (marketed as Proscar, Propecia, Fincar, Finpecia, Finax, Finast, Finara, Finalo, An antiandrogen, or androgen antagonist, is any of a group of Hormone Receptor antagonist compounds that are capable of preventing or inhibiting the biologic Glibenclamide ( INN) also known as glyburide ( USAN) is an Anti-diabetic drug in a class of medications known as Sulfonylureas used Anti-diabetic drugs treat Diabetes mellitus by lowering Glucose levels in the blood Cisapride is a Parasympathomimetic which acts as a Serotonin 5-HT4 receptor Agonist. 5-hydroxytryptamine (serotonin receptor 4, also known as HTR4, is a human Gene. An agonist is a term used to describe a type of ligand or drug that binds and alters the activity of a receptor. Terfenadine is an Antihistamine formerly used for the treatment of allergic conditions An H1 antagonist is a Histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by Histamine Toremifene citrate is an oral Selective estrogen receptor modulator (SERM which helps oppose the actions of Estrogen in the body Selective Estrogen Receptor Modulators ( SERMs) are a class of Medication that acts on the Estrogen receptor. Barbiturates are drugs that act as central nervous system Depressants and by virtue of this they produce a wide spectrum of effects from mild Sedation Phenobarbital ( INN) or phenobarbitone (former BAN) is a Barbiturate, first marketed as Luminal by Friedr Carbamazepine ("CBZ" is an Anticonvulsant and mood stabilizing drug used primarily in the treatment of Epilepsy and Bipolar disorder The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic This article refers to the medication For other uses see Stabilizer. Codeine ( INN) or methylmorphine is an Opiate used for its Analgesic, antitussive and antidiarrheal properties A cough medicine is a medicinal drug used to treat Coughing and related conditions An anti-diarrheal drug is any Medication which provides symptomatic relief for diarrhea. Dextromethorphan ( DXM or DM) is an Antitussive (cough suppressant drug found in many over-the-counter cold and Cough medicines A cough medicine is a medicinal drug used to treat Coughing and related conditions Digoxin ( INN) (dɨˈdʒɒksɨn also known as Digitalis, is a purified Cardiac glycoside extracted from the Foxglove plant Digitalis Antiarrhythmic agents are a group of Pharmaceuticals that are used to suppress fast rhythms of the Heart ( Cardiac arrhythmias) such as Atrial fibrillation Ergot is the common name of a Fungus in the Genus Claviceps that is parasitic on certain grains and grasses Neurotransmission (latin transmissio = passage crossing from transmitto = send let through also called synaptic transmission, is an electrical movement Estradiol (17β-estradiol (also oestradiol) is a Sex hormone. Sex steroids, also known as gonadal steroids, are Steroid hormones that interact with Vertebrate Androgen or Estrogen receptors Fentanyl is one of the most powerful Opioid Analgesics with a potency approximately 81 times that of Morphine. Ivabradine ( INN) (ɪˈvæbrədin is a novel Medication used for the symptomatic management of stable Angina pectoris. Angina pectoris, commonly known as angina, is severe Chest pain due to Ischemia (a lack of blood and hence Oxygen supply of the heart Levonorgestrel (or' l - Norgestrel or D - Norgestrel) is a synthetic progestogen used as Hormonal contraception refers to Birth control methods that act on the hormonal system Lidocaine ( INN) (ˈlaɪdoʊkeɪn or lignocaine (former BAN) (/ˈlɪgnoʊkeɪn/ is a common Local anesthetic and antiarrhythmic drug A local anesthetic is a drug that causes reversible Local anesthesia and a loss of Nociception. Antiarrhythmic agents are a group of Pharmaceuticals that are used to suppress fast rhythms of the Heart ( Cardiac arrhythmias) such as Atrial fibrillation Methadone ( Dolophine Amidone Methadose Physeptone Heptadon and many others is a synthetic Opioid, used medically as an Analgesic, Antitussive Drug addiction is widely considered a pathological state. The disorder of addiction involves the progression of acute Drug use to the development of drug-seeking Mifepristone is a synthetic Steroid compound used as a pharmaceutical. An abortifacient is a substance that induces Abortion. Abortifacients for Animals that have mated undesirably are known as Mismating shots Montelukast (trade name Singulair) is a Leukotriene receptor antagonist (LTRA used for the maintenance treatment of Asthma and to relieve symptoms of seasonal A leukotriene antagonist is a Hormone antagonist acting upon Leukotrienes It has been demonstrated that leukotrienes are implicated in Bronchoconstriction Ondansetron ( INN) (ɒnˈdænsɛtrɒn or Zofran is a Serotonin 5-HT3 receptor antagonist used mainly as an Antiemetic to The 5-HT3 antagonists are a class of Medications which act as Receptor antagonists at the 5-hydroxytryptamine-3 receptor (5-HT3 receptor Paracetamol ( INN) (ˌpærəˈsiːtəmɒl -ˈsɛtə- or acetaminophen ( USAN) is a widely-used Analgesic and Antipyretic Medication Antipyretics are Drugs that reduce body temperature in situations such as Fever. Quinidine is a Pharmaceutical agent that acts as a Class I antiarrhythmic agent in the Heart. Antiarrhythmic agents are a group of Pharmaceuticals that are used to suppress fast rhythms of the Heart ( Cardiac arrhythmias) such as Atrial fibrillation Quinine (ˈkwaɪnaɪn kwɪˈniːn ˈkwiːniːn is a natural white Crystalline Alkaloid having Antipyretic (fever-reducing antimalarial, Antipyretics are Drugs that reduce body temperature in situations such as Fever. Smallpox is an Infectious disease unique to humans caused by either of two virus variants named Variola major and Variola minor. Testosterone is a Steroid hormone from the Androgen group In mammals testosterone is primarily secreted in the testes of males and the Ovaries Androgen is the generic term for any natural or synthetic compound usually a Steroid Hormone, that stimulates or controls the development and maintenance of masculine Theophylline, also known as dimethylxanthine, is a Methylxanthine drug used in therapy for Respiratory diseases such as COPD or Asthma Stimulant drugs are Drugs that temporarily increase alertness and awareness Valproic acid ( VPA) is a Chemical compound that has found clinical use as an Anticonvulsant and mood-stabilizing drug, primarily in The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic This article refers to the medication For other uses see Stabilizer. Warfarin (also known under the brand names Coumadin, Jantoven, Marevan, and Waran) is an Anticoagulant. An anticoagulant is a substance that prevents coagulation; that is it stops Blood from clotting A psychoactive drug or psychotropic substance is a Chemical substance that acts primarily upon the Central nervous system where it alters Brain Antipsychotics are a group of Psychoactive drugs commonly but not exclusively used to treat Psychosis, which is typified by Schizophrenia. Aripiprazole (ay-ree-PIP-ray-zole (sold as Abilify) was approved by the Food and Drug Administration (FDA on November 15, 2002 for the Risperidone (pronounced Ris-PER-ǐ-dōn and sold under the trade name Risperdal in the Netherlands, United States, Canada, the Ziprasidone (marketed as Geodon, Zeldox) was the fifth Atypical antipsychotic to gain FDA approval (February 2001 Fluconazole ( INN) (fluːˈkɒnəzoʊl is a Triazole Antifungal drug used in the treatment and prevention of superficial and systemic fungal infections An antifungal drug is Medication used to treat fungal Infections such as Athlete's foot, Ringworm, Candidiasis (thrush Ritonavir, with trade name Norvir For natural protease inhibitors please see Protease inhibitor (biology Protease inhibitors (PIs are a class of Medications used The macrolides are a group of drugs (typically Antibiotics) whose activity stems from the presence of a macrolide ring, a large macrocyclic Erythromycin is a Macrolide Antibiotic that has an antimicrobial spectrum similar to or slightly wider than that of Penicillin, and is often used for people Telithromycin is the first Ketolide Antibiotic to enter clinical use Clarithromycin is a Macrolide Antibiotic used to treat Pharyngitis, Tonsillitis, acute maxillary Sinusitis, acute bacterial exacerbation An antifungal drug is Medication used to treat fungal Infections such as Athlete's foot, Ringworm, Candidiasis (thrush Ketoconazole is a synthetic Antifungal drug used to prevent and treat skin and fungal infections especially in immunocompromised patients such as those Itraconazole (marketed as Sporanox by Janssen Pharmaceutica) invented in 1984 is a Triazole Antifungal agent that is prescribed to patients Nefazodone hydrochloride (trade name Serzone, Nefadar) is an Antidepressant drug marketed by Bristol-Myers Squibb. The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor which belongs to the Serotonin receptor family and is a G protein coupled receptor Bergamottin is a natural Furanocoumarin found principally in Grapefruit juice. The grapefruit is a subtropical Citrus Tree grown for its Fruit which was originally named the "forbidden fruit " of Barbados Quercetin is a Flavonoid and to be more specific a flavonol. It is the Aglycone form of a number of other flavonoid Glycosides, such as Amiodarone is an Antiarrhythmic agent (medication used for irregular heart beat used for various types of tachyarrhythmias (fast forms of irregular heart beat both ventricular Antiarrhythmic agents are a group of Pharmaceuticals that are used to suppress fast rhythms of the Heart ( Cardiac arrhythmias) such as Atrial fibrillation Aprepitant is a chemical compound that belongs to a class of drugs called Substance P antagonists (SPA In Neuroscience, Substance P is a Neuropeptide: a short-chain Polypeptide that functions as a Neurotransmitter and as a Neuromodulator Neurokinin NK1 antagonists are a novel class of medications that possesses unique Antidepressant, Anxiolytic, and Antiemetic properties Cimetidine ( INN) (sɨˈmɛtɨdiːn/ /saɪ- is a histamine H2-receptor antagonist that inhibits the production of acid in the Stomach. The H2-receptor antagonists (H2RA often shortened to H2 antagonist) are a class of drugs used to block the action of Histamine In modern usage an antibiotic is a Chemotherapeutic agent with activity against Microorganisms such as Bacteria, fungi or Protozoa Ciclosporin (ˌsaɪkləˈspɔrən cyclosporine ( USAN) or cyclosporin (former BAN) is an Immunosuppressant drug widely An immunosuppressant is a substance that performs Immunosuppression of the Immune system. Diltiazem is a member of the group of drugs known as Benzothiazepines which are a class of Calcium channel blockers used in the treatment of Hypertension Calcium channel blockers are a class of drugs and natural substances with effects on many excitable cells of the body like the muscle of the Heart, smooth muscles Imatinib is a drug used to treat certain types of Cancer. It is currently marketed by Novartis as Gleevec ( USA) or Glivec Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer. Echinacea, commonly called Purple Coneflower, is a genus of nine species of Herbaceous plants in the family Asteraceae. Immunostimulators are substances (drugs and nutrients that stimulate the Immune system by inducing activation or increasing activity of any of its components Enoxacin (trade names Enroxil, Penetrex) is an oral broad-spectrum Fluoroquinolone Antibacterial agent used in the treatment of Urinary Antiseptics (from Greek αντί - anti, '"against" + σηπτικός - septikos, "putrefactive" are antimicrobial Ergotamine is an Ergopeptine and part of the Ergot family of Alkaloids it is structurally and biochemically closely related to Ergoline. Migraine is a neurological Syndrome characterized by altered bodily experiences painful headaches and nausea Metronidazole ( INN) (mɛtrəˈnaɪdəzoʊl is a Nitroimidazole anti-infective medication used mainly in the treatment of infections caused by susceptible Antiseptics (from Greek αντί - anti, '"against" + σηπτικός - septikos, "putrefactive" are antimicrobial Mifepristone is a synthetic Steroid compound used as a pharmaceutical. An abortifacient is a substance that induces Abortion. Abortifacients for Animals that have mated undesirably are known as Mismating shots Reverse transcriptase inhibitors (RTIs are a class of Antiretroviral drug used to treat HIV infection Tumors, and Cancer. Efavirenz (brand names Sustiva and Stocrin) is a Non-nucleoside reverse transcriptase inhibitor (NNRTI and is used as part of highly active antiretroviral Nevirapine, also marketed under the trade name Viramune ( Boehringer Ingelheim) is a non-nucleoside Reverse transcriptase inhibitor (NNRTI used to treat Gestodene is a Progestogen Hormonal contraceptive. Products containing gestoden include Meliane which contains 20 mcg of Ethinylestradiol and 75 mcg Hormonal contraception refers to Birth control methods that act on the hormonal system Mibefradil ( Posicor) is a drug for the treatment of Hypertension and chronic Angina pectoris. Angina pectoris, commonly known as angina, is severe Chest pain due to Ischemia (a lack of blood and hence Oxygen supply of the heart For natural protease inhibitors please see Protease inhibitor (biology Protease inhibitors (PIs are a class of Medications used Saquinavir is an Antiretroviral drug used in HIV therapy It falls in the protease inhibitor class Indinavir (IDV trade name Crixivan, manufactured by Merck) is a protease inhibitor used as a component of highly active antiretroviral therapy Selective serotonin reuptake inhibitors ( SSRIs) are a class of Antidepressants used in the treatment of depression, Anxiety disorders ||-||-|}The carambola is a species of Tree native to Indonesia, India and Sri Lanka and is popular throughout Southeast Asia, Piperine is the Alkaloid responsible for the Pungency of Black pepper and Long pepper, along with Chavicine (an Isomer Verapamil (brand names Isoptin, Verelan, Calan, Bosoptin, Covera-HS) is an L-type Calcium channel blocker. Calcium channel blockers are a class of drugs and natural substances with effects on many excitable cells of the body like the muscle of the Heart, smooth muscles Barbiturates are drugs that act as central nervous system Depressants and by virtue of this they produce a wide spectrum of effects from mild Sedation Phenobarbital ( INN) or phenobarbitone (former BAN) is a Barbiturate, first marketed as Luminal by Friedr Carbamazepine ("CBZ" is an Anticonvulsant and mood stabilizing drug used primarily in the treatment of Epilepsy and Bipolar disorder The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic This article refers to the medication For other uses see Stabilizer. Hyperforin is one of the principal constituents identified in St John's wort. St John's wort (pronounced) used alone refers to the species Hypericum perforatum, also known as Tipton's Weed or Klamath weed, but with qualifiers is Reverse transcriptase inhibitors (RTIs are a class of Antiretroviral drug used to treat HIV infection Tumors, and Cancer. Efavirenz (brand names Sustiva and Stocrin) is a Non-nucleoside reverse transcriptase inhibitor (NNRTI and is used as part of highly active antiretroviral Nevirapine, also marketed under the trade name Viramune ( Boehringer Ingelheim) is a non-nucleoside Reverse transcriptase inhibitor (NNRTI used to treat Etravirine (formerly known as TMC-125 brand name Intelence is a Drug used for the treatment of HIV. Phenytoin sodium is a commonly used Antiepileptic. Phenytoin acts to dampen the unwanted runaway brain activity seen in seizure by reducing electrical conductance among brain The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic Rifampicin ( INN) (rɪˈfæmpəsɪn or rifampin ( USAN) is a Bactericidal Antibiotic drug of the Rifamycin group A bactericide or bacteriocide is a substance that kills bacteria and preferably nothing else Modafinil ( Provigil) is a stimulant-like drug manufactured by Cephalon, and is approved by the FDA for the treatment of Narcolepsy Dexamethasone is a potent synthetic member of the glucocorticoid class of Steroid Hormones It acts as an Anti-inflammatory and immunosuppressant Anti-inflammatory refers to the property of a substance or treatment that reduces Inflammation. An immunosuppressant is a substance that performs Immunosuppression of the Immune system. Felbamate (marketed under the brand name Felbatol by MedPointe) is an Anticonvulsant drug used in the treatment of Epilepsy. The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic Glucocorticoids (GC are a class of Steroid hormones characterised by an ability to bind with the glucocorticoid receptor ( GR) and trigger similar effects Blood sugar, used in a physiological context is a misnomer and misleading Immunosuppression involves an act that reduces the activation or Efficacy of the Immune system. Griseofulvin (also known as Grisovin is an Antifungal drug. It is used both in animals and in humans to treat Ringworm infections of the skin and nails An antifungal drug is Medication used to treat fungal Infections such as Athlete's foot, Ringworm, Candidiasis (thrush Pioglitazone is a prescription drug of the class Thiazolidinedione with hypoglycemic (antihyperglycemic antidiabetic action Hypoglycemia or hypoglycaemia is the medical term for a pathologic state produced by a lower than normal level of Glucose ( sugar) in the blood Primidone is an Anticonvulsant of the Pyrimidinedione class whose active Metabolites Phenobarbital (major and phenylethylmalonamide (PEMA (minor The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic Topiramate (brand name Topamax) is an Anticonvulsant drug produced by Ortho-McNeil Neurologics and Noramco Inc The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic Troglitazone (Rezulin Resulin or Romozin is an Anti-diabetic and Antiinflammatory drug and a member of the drug class of the Thiazolidinediones Hypoglycemia or hypoglycaemia is the medical term for a pathologic state produced by a lower than normal level of Glucose ( sugar) in the blood Rifabutin is a Bactericidal Antibiotic drug primarily used in the treatment of Tuberculosis. Tuberculosis (abbreviated as TB for tubercle bacillus or T u' b' erculosis Bacillus --> is a common Cafestol is a Diterpene Molecule present in Coffee. A typical bean of Coffea arabica "Transgenic mouse models of human CYP3A4 gene regulation". Mol Pharmacol 64 (1): 42-50. doi:10.1124/mol.64.1.42. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 12815159.
- ^ Watkins P (1994). "Noninvasive tests of CYP3A enzymes". Pharmacogenetics 4 (4): 171-84. doi:10.1097/00008571-199408000-00001. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 7987401.
- ^ Where classes of agents are listed, there may be exceptions within the class
- ^ a b Mentioned both in the reference named FASS and were previously mentioned in Wikipedia. Further contributions may follow other systems
- ^ [http://www.fass.se/LIF/produktfakta/fakta_lakare_artikel.jsp?articleID=18352 Swedish environmental classification of pharmaceuticals] Facts for prescribers (Fakta för förskrivare)
- ^ a b Non-nucleoside reverse transcriptase inhibitors have been shown to both induce and inhibit CYP3A4.
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