Pharmaceutical compound DroxidopaClinical dataTrade namesNorthera, DopsOther names3,4-Dihydroxyphenylserine; 3,4-threo-DOPS; L-threo-Dihydroxyphenylserine; L-DOPS; L-threo-DOPS; Threo-DOPS; β,3-Dihydroxytyrosine; (–)-threo-3-(3,4-Dihydroxyphenyl)-L-serine; SM-5688AHFS/Drugs.comMonographMedlinePlusa614025License data US DailyMed: Droxidopa Routes ofadministrationBy mouthATC codeC01CA27 (WHO) Legal statusLegal status US: ℞-only In general: ℞ (Prescription only) Pharmacokinetic dataBioailability90%MetabolismLiverMetabolitesNorepinephrineElimination half-life1.5 hoursExcretionKidneyIdentifiers IUPAC name (2S,3R)-2-Amino-3-(3,4-dihydroxyphenyl)-3-hydroxypropanoic acid CAS Number23651-95-8 YPubChem CID92974DrugBankDB06262ChemSpider83927UNIIJ7A92W69L7KEGGD01277ChEBICHEBI:31524ChEMBLChEMBL2103827CompTox Dashboard (EPA)DTXSID6046422 ECHA InfoCard100.215.254 Chemical and physical dataFormulaC9H11NO5Molar mass213.189 g·mol−13D model (JSmol)Interactive image SMILES N[C@H](C(=O)O)[C@H](O)c1ccc(O)c(O)c1 InChI InChI=1S/C9H11NO5/c10-7(9(14)15)8(13)4-1-2-5(11)6(12)3-4/h1-3,7-8,11-13H,10H2,(H,14,15)/t7-,8+/m0/s1Key:QXWYKJLNLSIPIN-JGVFFNPUSA-Na (verify)
Droxidopa, also known as L-threo-dihydroxyphenylserine (L-DOPS) and sold under the brand names Northera and Dops among others, is sympathomimetic medication which is used in the treatment of hypotension (low blood pressure) and for other indications.[1][2] It is taken by mouth.[1]
Side effects of droxidopa include headache, dizziness, nausea, and hypertension, among others.[1] Droxidopa is a synthetic amino acid precursor which acts as a prodrug to the neurotransmitter norepinephrine (noradrenaline).[3] Hence, it acts as a non-selective agonist of the α- and β-adrenergic receptors. Unlike norepinephrine, but similarly to levodopa (L-DOPA), droxidopa is capable of crossing the protective blood–brain barrier (BBB).[3]
Droxidopa was first described by 1971.[4][5] It was approved for use in Japan in 1989[6] and was introduced in the United States in 2014.[1][7]
Medical uses[edit]Droxidopa is approved for use in the treatment of orthostatic hypotension, intradialytic hypotension (IDH; hemodialysis-induced hypotension), dizziness, and amyloid polyneuropathy.[2] For hypotension, it is specifically used in the treatment of neurogenic orthostatic hypotension (NOH) in dopamine β-hydroxylase deficiency,[6] as well as NOH associated with multiple system atrophy (MSA),[8] familial amyloid polyneuropathy (FAP), and pure autonomic failure (PAF).[9] The drug is also used off-label in the treatment of freezing of gait in Parkinson's disease.[citation needed]
Side effects[edit]With over 20 years on the market, droxidopa has proven to he few side effects of which most are mild. The most common side effects reported in clinical trials include headache, dizziness, nausea, hypertension and fatigue.[10][11][12]
Pharmacology[edit]Droxidopa is a prodrug of norepinephrine used to increase the concentrations of these neurotransmitters in the body and brain.[3] It is metabolized by aromatic L-amino acid decarboxylase (AAAD), also known as DOPA decarboxylase (DDC). Patients with NOH he depleted levels of norepinephrine which leads to decreased blood pressure or hypotension upon orthostatic challenge.[13] Droxidopa works by increasing the levels of norepinephrine in the peripheral nervous system (PNS), thus enabling the body to maintain blood flow upon and while standing.[13]
Droxidopa can also cross the blood–brain barrier (BBB) where it is converted to norepinephrine from within the brain.[3] Increased levels of norepinephrine in the central nervous system (CNS) may be beneficial to patients in a wide range of indications. Droxidopa can be coupled with a peripheral aromatic L-amino acid decarboxylase inhibitor (AAADI) or DOPA decarboxylase inhibitor (DDC) such as carbidopa (Lodosyn) to increase central norepinephrine concentrations while minimizing increases of peripheral levels.[citation needed]
Chemistry[edit]Droxidopa, also known as (–)-threo-3-(3,4-dihydroxyphenyl)-L-serine (L-DOPS), is a substituted phenethylamine and is chemically analogous to levodopa (L-3,4-dihydroxyphenylalanine; L-DOPA). Whereas levodopa functions as a precursor and prodrug to dopamine, droxidopa is a precursor and prodrug of norepinephrine.[citation needed]
History[edit]Droxidopa was first described in the scientific literature by 1971.[4][5]
Droxidopa was developed by Sumitomo Pharmaceuticals for the treatment of hypotension, including NOH,[6] and NOH associated with various disorders such as MSA, FAP, and PD, as well as IDH. The drug has been used in Japan and some surrounding Asian areas for these indications since 1989.[6]
Following a merger with Dainippon Pharmaceuticals in 2006, Dainippon Sumitomo Pharma licensed droxidopa to Chelsea Therapeutics to develop and market it worldwide except in Japan, Korea, China, and Taiwan. In February 2014, the United States Food and Drug Administration approved droxidopa for the treatment of symptomatic neurogenic orthostatic hypotension.[7]
Clinical trials[edit]A systematic review and meta-analysis conducted on clinical trials comparing the clinical use of droxidopa and midodrine he found that midodrine was more likely to cause supine hypertension than droxidopa in patients with NOH. Midodrine was also found to be slightly more effective at raising blood pressure but not statistically significantly.[14]
Chelsea Therapeutics obtained orphan drug status (ODS) for droxidopa in the US for NOH, and that of which associated with PD, PAF, and MSA. In 2014, Chelsea Therapeutics was acquired by Lundbeck along with the rights to droxidopa which was launched in the US in Sept 2014.[15]
Society and culture[edit] Names[edit]Droxidopa is the generic name of the drug and its INNTooltip International Nonproprietary Name and JANTooltip Japanese Accepted Name.[16] Brand names of droxidopa include Dops and Northera.[16][1]
Research[edit]Droxidopa alone and in combination with carbidopa has been studied in the treatment of attention deficit hyperactivity disorder (ADHD).[17][18] Droxidopa was under development for the treatment of ADHD, chronic fatigue syndrome, and fibromyalgia, but development for these indications was discontinued.[2]
References[edit] ^ a b c d e "Northera (droxidopa) capsules - Prescribing Information" (PDF). Food and Drug Administration. February 10, 2017. ^ a b c "Sumitomo Pharma/Lundbeck". AdisInsight. 2023-11-05. Retrieved 2024-09-01. ^ a b c d Goldstein DS (2006). "L-Dihydroxyphenylserine (L-DOPS): a norepinephrine prodrug". Cardiovascular Drug Reviews. 24 (3–4): 189–203. doi:10.1111/j.1527-3466.2006.00189.x. PMID 17214596. ^ a b Robson RD (June 1971). "Modification of the cardiovascular effects of L-dopa in anesthetized dogs by inhibitors of enzymes involved in catecholamine metabolism". Circ Res. 28 (6): 662–670. doi:10.1161/01.res.28.6.662. PMID 4325846. ^ a b Redmond DE, Olander R, Maas JW (November 1975). "Cardiovascular effects of D,L-threo-dihydroxyphenylserine in cats". Toxicol Appl Pharmacol. 34 (2): 301–308. Bibcode:1975ToxAP..34..301R. doi:10.1016/0041-008x(75)90035-6. PMID 1209627. ^ a b c d Mathias CJ (March 2008). "L-dihydroxyphenylserine (Droxidopa) in the treatment of orthostatic hypotension: the European experience". Clinical Autonomic Research. 18 (Supplement 1): 25–29. doi:10.1007/s10286-007-1005-z. PMID 18368304. S2CID 29861644. ^ a b "FDA grants accelerated approval to NORTHERA (droxidopa) for patients with symptomatic NOH". news-medical.net. February 18, 2014. ^ Calandra-Buonaura G, Doria A, Lopane G, et al. (February 2016). "Pharmacodynamics of a low subacute levodopa dose helps distinguish between multiple system atrophy with predominant Parkinsonism and Parkinson's disease". Journal of Neurology. 263 (2): 250–256. doi:10.1007/s00415-015-7961-7. PMID 26566913. S2CID 189866517. ^ Palma JA, Kaufmann H (February 2020). "Management of Orthostatic Hypotension". Continuum. 26 (1): 154–177. doi:10.1212/CON.0000000000000816. PMC 7339914. PMID 31996627. ^ Kaufmann H, Freeman R, Biaggioni I, Low P, Pedder S, Hewitt LA, et al. (July 2014). "Droxidopa for neurogenic orthostatic hypotension: a randomized, placebo-controlled, phase 3 trial". Neurology. 83 (4): 328–35. doi:10.1212/WNL.0000000000000615. PMC 4115605. PMID 24944260. ^ Hauser RA, Isaacson S, Lisk JP, Hewitt LA, Rowse G (April 2015). "Droxidopa for the short-term treatment of symptomatic neurogenic orthostatic hypotension in Parkinson's disease (nOH306B)". Movement Disorders. 30 (5): 646–54. doi:10.1002/mds.26086. PMID 25487613. S2CID 2828467. ^ "Highlights of prescribing information for Northera (droxidopa)" (PDF). Food and Drug Administration. 2014. ^ a b Robertson D (March 2008). "The pathophysiology and diagnosis of orthostatic hypotension". Clinical Autonomic Research. 18 (Supplement 1): 2–7. doi:10.1007/s10286-007-1004-0. PMID 18368300. S2CID 15693501. ^ Chen JJ, Han Y, Tang J, Portillo I, Hauser RA, Dashtipour K (December 2018). "Standing and Supine Blood Pressure Outcomes Associated With Droxidopa and Midodrine in Patients With Neurogenic Orthostatic Hypotension: A Bayesian Meta-analysis and Mixed Treatment Comparison of Randomized Trials". The Annals of Pharmacotherapy. 52 (12): 1182–1194. doi:10.1177/1060028018786954. PMID 29972032. S2CID 49674644. ^ "Lundbeck Announces Availability of NORTHERATM (droxidopa) Capsules in the U.S. for Symptomatic Neurogenic Orthostatic Hypotension" (PDF). Lundbeck NA Ltd. Archived from the original (PDF) on 2018-09-20. Retrieved 2015-11-02. ^ a b Schweizerischer Apotheker-Verein (2004). Index Nominum: International Drug Directory. Medpharm Scientific Publishers. p. 434. ISBN 978-3-88763-101-7. Retrieved 1 September 2024. ^ Buoli M, Serati M, Cahn W (2016). "Alternative pharmacological strategies for adult ADHD treatment: a systematic review". Expert Rev Neurother. 16 (2): 131–44. doi:10.1586/14737175.2016.1135735. PMID 26693882. S2CID 33004517. ^ Adler LA, Gorny SW (January 2019). "Pilot Study of Droxidopa With Carbidopa in Adults With ADHD". J Atten Disord. 23 (2): 189–198. doi:10.1177/1087054715580393. PMID 25907673. S2CID 20990991. External links[edit] "Droxidopa". Drug Information Portal. U.S. National Library of Medicine. Archived from the original on January 23, 2017. vteCardiac stimulants excluding cardiac glycosides (C01C)Adrenergic anddopaminergic agentsAdrenergic agonistsα Denopamine Metaraminol Methoxamine Midodrine Norfenefrine Oxedrine Phenylephrine β Arbutamine Dobutamine Isoprenaline Prenalterol mixed Amezinium metilsulfate Droxidopa Epinephrine # Etilefrine Norepinephrine Dopamine agonists Fenoldopam Both Docarpamine Dopamine # Dopexamine Ibopamine Octopamine Unknown/ungrouped Cafedrine Dimetofrine Gepefrine Mephentermine Theodrenaline Phosphodiesterase inhibitors (PDE3I) Amrinone Bucladesine Enoximone Milrinone Vesnarinone Other cardiac stimulants Angiotensinamide Levosimendan Omecamtiv mecarbil Pimobendan Xamoterol #WHO-EM ‡Withdrawn from market Clinical trials: †Phase III §Never to phase III vteStimulantsAdamantanes Adapromine Amantadine Bromantane Memantine Rimantadine Adenosine antagonists 8-Chlorotheophylline 8-Cyclopentyltheophylline 8-Phenyltheophylline Aminophylline Caffeine 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Amidephrine 2-Amino-1,2-dihydronaphthalene 2-Aminoindane 5-(2-Aminopropyl)indole 2-Aminotetralin Acridorex Amphetamine (Dextroamphetamine, Levoamphetamine) Amphetaminil Arbutamine β-Methylphenethylamine β-Phenylmethamphetamine Benfluorex Benzphetamine BDB BOH 3-Benzhydrylmorpholine BPAP Camfetamine Cathine Chlorphentermine Cilobamine Cinnamedrine Clenbuterol Clobenzorex Cloforex Clortermine Cypenamine D-Deprenyl Denopamine Dimethoxyamphetamine Dimethylamphetamine Dobutamine DOPA (Dextrodopa, Levodopa) Dopamine Dopexamine Droxidopa EBDB Ephedrine Epinephrine Epinine Etafedrine Ethylnorepinephrine Etilamfetamine Etilefrine Famprofazone Fencamfamin Fencamine Fenethylline Fenfluramine (Dexfenfluramine, Levofenfluramine) Fenproporex Feprosidnine Fludorex Formetorex Furfenorex Gepefrine Hexapradol HMMA Hordenine 4-Hydroxyamphetamine 5-Iodo-2-aminoindane Ibopamine Indanylamphetamine Iofetamine Isoetarine Isoprenaline L-Deprenyl (Selegiline) Lefetamine Lisdexamfetamine Lophophine MBDB MDA 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Altropane (IACFT) Brasofensine CFT (WIN 35,428) β-CIT (RTI-55) Cocaethylene Cocaine Dichloropane (RTI-111) Difluoropine FE-β-CPPIT FP-β-CPPIT Ioflupane (123I) Norcocaine PIT PTT RTI-31 RTI-32 RTI-51 RTI-112 RTI-113 RTI-120 RTI-121 (IPCIT) RTI-126 RTI-150 RTI-177 RTI-229 RTI-336 RTI-354 RTI-371 RTI-386 Salicylmethylecgonine Tesofensine Troparil (β-CPT, WIN 35,065-2) Tropoxane WF-23 WF-33 Tryptamines 4-HO-αMT 4-Methyl-αET 4-Methyl-αMT 5-Chloro-αMT 5-Fluoro-αMT 5-MeO-αET 5-MeO-αMT 5-MeO-DIPT 6-Fluoro-αMT 7-Methyl-αET αET αMT Others 2-MDP 3,3-Diphenylcyclobutanamine Amfonelic acid Amineptine Amiphenazole Atipamezole Atomoxetine Bemegride Benzydamine BTQ BTS 74,398 Centanafadine Ciclazindol Clofenciclan Cropropamide Crotetamide D-161 Desipramine Diclofensine Dimethocaine Efaroxan Etamivan Fenisorex Fenpentadiol Gamfexine Gilutensin GSK1360707F GYKI-52895 Hexacyclonate Idazoxan Indanorex Indatraline JNJ-7925476 Lazabemide Leptacline Lomevactone LR-5182 Mazindol Meclofenoxate Medifoxamine Mefexamide Methamnetamine Methastyridone Methiopropamine Naphthylaminopropane Nefopam Nikethamide Nomifensine O-2172 Oxaprotiline PNU-99,194 PRC200-SS Rasagiline Rauwolscine Rubidium chloride Setazindol Tametraline Tandamine Thiopropamine Thiothinone Trazium UH-232 Yohimbine ATC code: N06B vteAdrenergic receptor modulatorsα1Agonists 6-FNE Amidephrine Buspirone Cirazoline Corbadrine Deoxyepinephrine (epinine, N-methyldopamine) Desglymidodrine Dexisometheptene Dipivefrine Dopamine Droxidopa (L-DOPS) Epinephrine Etilefrine Etilevodopa Ethylnorepinephrine Ibopamine Indanidine Isometheptene L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Melevodopa Metaraminol Methoxamine Methyldopa Midodrine Naphazoline Norepinephrine Octopamine Oxymetazoline Phenylephrine Phenylpropanolamine Synephrine Tetryzoline Tiamenidine XP21279 Xylometazoline Antagonists Abanoquil Ajmalicine Alfuzosin Anisodamine Anisodine Atiprosin Atypical antipsychotics (e.g., brexpiprazole, clozapine, olanzapine, quetiapine, risperidone) Benoxathian Beta blockers (e.g., adimolol, amosulalol, arotinolol, carvedilol, eugenodilol, labetalol) Buflomedil Bunazosin Corynanthine Dapiprazole Domesticine Doxazosin Ergolines (e.g., acetergamine, ergotamine, dihydroergotamine, lisuride, nicergoline, terguride) Etoperidone Fenspiride Hydroxyzine Indoramin Ketanserin L-765,314 mCPP Mepiprazole Metazosin Monatepil Moxisylyte Naftopidil Nantenine Neldazosin Niaprazine Niguldipine Pardoprunox Pelanserin Perlapine Phendioxan Phenoxybenzamine Phentolamine Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione) Piperoxan Prazosin Quinazosin Quinidine Silodosin Spegatrine Spiperone Talipexole Tamsulosin Terazosin Tiodazosin Tolazoline Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin) Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine) Trimazosin Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine) Urapidil WB-4101 Zolertine α2Agonists (R)-3-Nitrobiphenyline 4-NEMD 6-FNE Amitraz Apraclonidine Brimonidine CHF-1024 Clonidine Corbadrine Deoxyepinephrine (epinine, N-methyldopamine) Detomidine Dexmedetomidine Dihydroergotamine Dipivefrine Dopamine Droxidopa (L-DOPS) Etilevodopa Ergotamine Epinephrine Etilefrine Ethylnorepinephrine Guanabenz Guanfacine Guanoxabenz L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Ibopamine Lofexidine Medetomidine Melevodopa Methyldopa Mivazerol Moxonidine Naphazoline Nolomirole Norepinephrine Oxymetazoline Phenylpropanolamine Piperoxan PS75 Rezatomidine Rilmenidine Romifidine Talipexole Tasipimidine Tetryzoline Tiamenidine Tizanidine Tolonidine Urapidil Vatinoxan XP21279 Xylazine Xylometazoline Antagonists 1-PP Adimolol Amesergide Aptazapine Atipamezole Atypical antipsychotics (e.g., asenapine, brexpiprazole, clozapine, lurasidone, olanzapine, paliperidone, quetiapine, risperidone, zotepine) Azapirones (e.g., buspirone, gepirone, ipsapirone, tandospirone) BRL-44408 Buflomedil Cirazoline Efaroxan Esmirtazapine Fenmetozole Fluparoxan Idazoxan Ketanserin Lisuride mCPP Mianserin Mirtazapine NAN-190 Pardoprunox Phentolamine Phenoxybenzamine Piperoxan Piribedil Rauwolscine Rotigotine Setiptiline Spegatrine Spiroxatrine Sunepitron Terguride Tolazoline Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine) Yohimbine βAgonists Abediterol Alifedrine Amibegron Arbutamine Arformoterol Arotinolol BAAM Bambuterol Befunolol Bitolterol Broxaterol Buphenine Butopamine Carbuterol Carmoterol Cimaterol Clenbuterol Colterol Corbadrine Denopamine Deoxyepinephrine (epinine, N-methyldopamine) Dipivefrine Dobutamine Dopamine Dopexamine Droxidopa (L-DOPS) Epinephrine Etafedrine Etilefrine Etilevodopa Ethylnorepinephrine Eugenodilol Fenoterol Formoterol Hexoprenaline Higenamine Ibopamine Indacaterol Isoetarine Isoprenaline Isoxsuprine L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Levosalbutamol Lubabegron Mabuterol Melevodopa Methoxyphenamine Methyldopa Mirabegron Norepinephrine Orciprenaline Oxyfedrine PF-610355 Phenylpropanolamine Pirbuterol Prenalterol Ractopamine Procaterol Reproterol Rimiterol Ritodrine Salbutamol Salmeterol Solabegron Terbutaline Tretoquinol Tulobuterol Vibegron Vilanterol Xamoterol XP21279 Zilpaterol Zinterol Antagonists Acebutolol Adaprolol Adimolol Afurolol Alprenolol Alprenoxime Amosulalol Ancarolol Arnolol Arotinolol Atenolol Befunolol Betaxolol Bevantolol Bisoprolol Bopindolol Bornaprolol Brefonalol Bucindolol Bucumolol Bufetolol Bufuralol Bunitrolol Bunolol Bupranolol Butaxamine Butidrine Butofilolol Capsinolol Carazolol Carpindolol Carteolol Carvedilol Celiprolol Cetamolol Cicloprolol Cinamolol Cloranolol Cyanopindolol Dalbraminol Dexpropranolol Diacetolol Dichloroisoprenaline Dihydroalprenolol Dilevalol Diprafenone Draquinolol Ecastolol Epanolol Ericolol Ersentilide Esatenolol Esprolol Eugenodilol Exaprolol Falintolol Flestolol Flusoxolol Hydroxycarteolol Hydroxytertatolol ICI-118,551 Idropranolol Indenolol Indopanolol Iodocyanopindolol Iprocrolol Isoxaprolol Isamoltane Labetalol Landiolol Levobetaxolol Levobunolol Levomoprolol Medroxalol Mepindolol Metipranolol Metoprolol Moprolol Nadolol Nadoxolol Nebivolol Nifenalol Nipradilol Oxprenolol Pacrinolol Pafenolol Pamatolol Pargolol Penbutolol Pindolol Practolol Primidolol Procinolol Pronethalol Propafenone Propranolol Ridazolol Ronactolol Soquinolol Sotalol Spirendolol SR 59230A Sulfinalol Talinolol Tazolol Tertatolol Tienoxolol Tilisolol Timolol Tiprenolol Tolamolol Toliprolol Xibenolol Xipranolol See also: Receptor/signaling modulators Dopaminergics Serotonergics Monoamine reuptake inhibitors Monoamine releasing agents Monoamine metabolism modulators Monoamine neurotoxins vteXenobiotic-sensing receptor modulatorsCARTooltip Constitutive androstane receptor Agonists: 6,7-Dimethylesculetin Amiodarone Artemisinin Benfuracarb Carbamazepine Carvedilol Chlorpromazine Chrysin CITCO Clotrimazole Cyclophosphamide Cypermethrin DHEA (prasterone) Efirenz Ellagic acid Griseofulvin Methoxychlor Mifepristone Nefazodone Nevirapine Nicardipine Octicizer Permethrin Phenobarbital Phenytoin Pregnanedione (5β-dihydroprogesterone) Reserpine TCPOBOP Telmisartan Tolnaftate Troglitazone Valproic acid Antagonists: 3,17β-Estradiol 3α-Androstanol 3α-Androstenol 3β-Androstanol 17-Androstanol AITC Ethinylestradiol Meclizine Nigramide J Okadaic acid PK-11195 S-07662 T-0901317 PXRTooltip Pregnane X receptor Agonists: 17α-Hydroxypregnenolone 17α-Hydroxyprogesterone Δ4-Androstenedione Δ5-Androstenediol Δ5-Androstenedione AA-861 Allopregnanediol Allopregnanedione (5α-dihydroprogesterone) Allopregnanolone (brexanolone) Alpha-Lipoic acid Ambrisentan AMI-193 Amlodipine besylate Antimycotics Artemisinin Aurothioglucose Bile acids Bithionol Bosentan Bumecaine Cafestol Cephaloridine Cephradine Chlorpromazine Ciglitazone Clindamycin Clofenvinfos Chloroxine Clotrimazole Colforsin Corticosterone Cyclophosphamide Cyproterone acetate Demecolcine Dexamethasone DHEA (prasterone) DHEA-S (prasterone sulfate) Dibunate sodium Diclazuril Dicloxacillin Dimercaprol Dinaline Docetaxel Docusate calcium Dodecylbenzenesulfonic acid Dronabinol Droxidopa Eburnamonine Ecopipam Enzacamene Epothilone B Erythromycin Famprofazone Febantel Felodipine Fenbendazole Fentanyl Flucloxacillin Fluorometholone Griseofulvin Guggulsterone Haloprogin Hetacillin potassium Hyperforin Hypericum perforatum (St John's wort) Indinir sulfate Lasalocid sodium Levothyroxine Linolenic acid: α-Linolenic acid and γ-Linolenic acid LOE-908 Loratadine Lovastatin Meclizine Metacycline Methylprednisolone Metyrapone Mevastatin Mifepristone Nafcillin Nicardipine Nicotine Nifedipine Nilvadipine Nisoldipine Norelgestromin Omeprazole Orlistat Oxatomide Paclitaxel Phenobarbital Piperine Plicamycin Prednisolone Pregnanediol Pregnanedione (5β-dihydroprogesterone) Pregnanolone Pregnenolone Pregnenolone 16α-carbonitrile Proadifen Progesterone Quingestrone Reserpine Reverse triiodothyronine Rifampicin Rifaximin Rimexolone Riodipine Ritonir Simvastatin Sirolimus Spironolactone Spiroxatrine SR-12813 Suberoylanilide Sulfisoxazole Suramin Tacrolimus Tenylidone Terconazole Testosterone isocaproate Tetracycline Thiamylal sodium Thiothixene Thonzonium bromide Tianeptine Troglitazone Troleandomycin Tropanyl 3,5-dimethulbenzoate Zafirlukast Zeranol Antagonists: Ketoconazole Sesamin See also Receptor/signaling modulators Portal: Medicine