General Information of Drug (ID: DM5URA2)

Drug Name
Chlorpheniramine
Synonyms
Allergican; Allergisan; Antagonate; Chloropheniramine; Chlorophenylpyridamin; Chlorophenylpyridamine; Chloropiril; Chloroprophenpyridamine; Chlorphenamine; Chlorphenaminum; Chlorpheniraminum; Chlorprophenpyridamine; Clofeniramina; Clorfenamina; Clorfeniramina; Cloropiril; Haynon; Hayon; Histadur; ISOCLOR; Kloromin; Phenetron; PiriIton; Piriton; Polaronil; Telachlor; Teldrin; Chlorphenamine [INN]; Clorfeniramina [Italian]; Pediacare Allergy Formula; [3H]Chlorpheniramine; Aller-Chlor; Chlo-amine; Chlor-Pro; Chlor-Trimeton Repetabs; Chlor-trimeton; Chlorphenamine (INN); Chlorphenaminum [INN-Latin]; Clofeniramina (TN); Clorfenamina [INN-Spanish]; Comakin (TN); Gen-Allerate; Novo-Pheniram; Piriton (TN); Chlor-Trimeton (TN); Chlor-Tripolon (TN); CHLORPHENIRAMINE (SEE ALSO: CHLORPHENIRAMINE MALEATE (CAS113-92-8)); Gamma-(4-Chlorophenyl)-gamma-(2-pyridyl)propyldimethylamine; Gamma-(4-Chlorophenyl)-N,N-dimethyl-2-pyridinepropanamine; 1-(p-Chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpropylamine; 1-(p-Chlorophenyl)-1-(2-pyridyl)-3-dimethylaminopropane; 2-(p-Chloro-alpha-(2-(dimethylamino)ethyl)benzyl)pyridine; 3-(4-chlorophenyl)-N,N-dimethyl-3-(pyridin-2-yl)propan-1-amine; 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine; 3-(p-Chlorophenyl)-3-(2-pyridyl)-N,N-dimethylpropylamine; 4-Chloropheniramine
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Approved [1], [2]
Therapeutic Class
Antiallergic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 274.79
Topological Polar Surface Area (xlogp) 3.4
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Clearance
The drug present in the plasma can be removed from the body at the rate of 2.5 mL/min/kg [4]
Elimination
10% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 22 hours [4]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.48399 micromolar/kg/day [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.7% [4]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 3.3 L/kg [4]
Chemical Identifiers
Formula
C16H19ClN2
IUPAC Name
3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine
Canonical SMILES
CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2
InChI
InChI=1S/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3
InChIKey
SOYKEARSMXGVTM-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
2725
ChEBI ID
CHEBI:52010
CAS Number
113-92-8
DrugBank ID
DB01114
TTD ID
D0B7NG
VARIDT ID
DR00595
INTEDE ID
DR0304
ACDINA ID
D00123

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Antagonist [6], [7], [8]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Substrate [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [10]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [11]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [10]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [10]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Allergic rhinitis
ICD Disease Classification CA08.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Histamine H1 receptor (H1R) DTT HRH1 6.74E-01 0.13 0.43
Multidrug resistance-associated protein 1 (ABCC1) DTP MRP1 3.67E-01 -1.78E-01 -9.02E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.57E-01 9.43E-03 1.29E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 8.70E-01 2.98E-02 1.22E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.76E-01 1.26E-01 8.27E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Chlorpheniramine
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Trimeprazine DMEMV9D Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [59]
Acrivastine DMTIGA0 Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Acrivastine. Vasomotor/allergic rhinitis [CA08] [60]
Coadministration of a Drug Treating the Disease Different from Chlorpheniramine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Phenyltoloxamine DMKAEQW Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Phenyltoloxamine. Allergic/hypersensitivity disorder [4A80-4A8Z] [59]
Desipramine DMT2FDC Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Desipramine. Attention deficit hyperactivity disorder [6A05] [60]
Cariprazine DMJYDVK Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Cariprazine. Bipolar disorder [6A60] [60]
Acetylcholine DMDF79Z Moderate Antagonize the effect of Chlorpheniramine when combined with Acetylcholine. Cataract [9B10] [61]
Umeclidinium DM4E8O9 Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Umeclidinium. Chronic obstructive pulmonary disease [CA22] [62]
Tiotropium DMFDC0Q Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Tiotropium. Chronic obstructive pulmonary disease [CA22] [62]
Revefenacin DMMP5SI Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Revefenacin. Chronic obstructive pulmonary disease [CA22] [62]
Isocarboxazid DMAF1NB Moderate Additive CNS depression effects by the combination of Chlorpheniramine and Isocarboxazid. Depression [6A70-6A7Z] [63]
OPC-34712 DMHG57U Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and OPC-34712. Depression [6A70-6A7Z] [60]
Clomipramine DMINRKW Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Clomipramine. Depression [6A70-6A7Z] [60]
Doxepin DMPI98T Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Doxepin. Depression [6A70-6A7Z] [59]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Chlorpheniramine and Esketamine. Depression [6A70-6A7Z] [64]
Mepenzolate DM8YU2F Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Mepenzolate. Digestive system disease [DE2Z] [60]
Solifenacin DMG592Q Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Solifenacin. Functional bladder disorder [GC50] [60]
Mirabegron DMS1GYT Moderate Decreased metabolism of Chlorpheniramine caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [65]
Procarbazine DMIK367 Moderate Additive CNS depression effects by the combination of Chlorpheniramine and Procarbazine. Hodgkin lymphoma [2B30] [63]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Chlorpheniramine caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [66]
Givosiran DM5PFIJ Moderate Decreased metabolism of Chlorpheniramine caused by Givosiran mediated inhibition of CYP450 enzyme. Inborn porphyrin/heme metabolism error [5C58] [67]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Chlorpheniramine caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [68]
ITI-007 DMUQ1DO Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and ITI-007. Insomnia [7A00-7A0Z] [60]
Dacomitinib DMOH8VY Moderate Decreased metabolism of Chlorpheniramine caused by Dacomitinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [69]
Vemurafenib DM62UG5 Moderate Decreased metabolism of Chlorpheniramine caused by Vemurafenib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [70]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Chlorpheniramine and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [71]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Chlorpheniramine and Lasmiditan. Migraine [8A80] [72]
Flibanserin DM70DTN Moderate Additive CNS depression effects by the combination of Chlorpheniramine and Flibanserin. Mood disorder [6A60-6E23] [73]
Panobinostat DM58WKG Moderate Decreased metabolism of Chlorpheniramine caused by Panobinostat mediated inhibition of CYP450 enzyme. Multiple myeloma [2A83] [74]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Chlorpheniramine caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [75]
Nilotinib DM7HXWT Moderate Decreased metabolism of Chlorpheniramine caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [76]
Rolapitant DM8XP26 Moderate Decreased metabolism of Chlorpheniramine caused by Rolapitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [77]
Cyclizine DM9G7BS Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Cyclizine. Nausea/vomiting [MD90] [60]
Bupropion DM5PCS7 Moderate Decreased metabolism of Chlorpheniramine caused by Bupropion mediated inhibition of CYP450 enzyme. Nicotine use disorder [6C4A] [78]
Lorcaserin DMG6OYJ Moderate Decreased metabolism of Chlorpheniramine caused by Lorcaserin mediated inhibition of CYP450 enzyme. Obesity [5B80-5B81] [79]
Methylscopolamine DM5VWOB Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Methylscopolamine. Peptic ulcer [DA61] [60]
ABIRATERONE DM8V75C Moderate Decreased metabolism of Chlorpheniramine caused by ABIRATERONE mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [80]
Levomepromazine DMIKFEL Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Levomepromazine. Psychotic disorder [6A20-6A25] [60]
Quetiapine DM1N62C Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Quetiapine. Schizophrenia [6A20] [60]
Aripiprazole DM3NUMH Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Aripiprazole. Schizophrenia [6A20] [60]
Iloperidone DM6AUFY Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Iloperidone. Schizophrenia [6A20] [60]
Paliperidone DM7NPJS Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Paliperidone. Schizophrenia [6A20] [60]
Molindone DMAH70G Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Molindone. Schizophrenia [6A20] [60]
Thiothixene DMDINC4 Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Thiothixene. Schizophrenia [6A20] [60]
Asenapine DMSQZE2 Moderate Additive anticholinergic effects by the combination of Chlorpheniramine and Asenapine. Schizophrenia [6A20] [60]
⏷ Show the Full List of 42 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Allura red AC dye E00338 33258 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Hydrazine yellow E00409 164825 Colorant
methylparaben E00149 7456 Antimicrobial preservative
Oleic acid E00421 445639 Emulsifying agent; Penetration agent; Solubilizing agent
Quinoline yellow WS E00309 24671 Colorant
Sodium benzoate E00432 517055 Antimicrobial preservative; lubricant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Calcium hydrogenphosphate E00294 24441 Diluent
Calcium sulfate anhydrous E00303 24497 Desiccant; Diluent
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Ethanethiol E00116 6343 Flavoring agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Rosin E00470 5280656 Binding agent; Film/membrane-forming agent
Saccharose E00091 5988 Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triethyl citrate E00128 6506 Plasticizing agent; Solvent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
⏷ Show the Full List of 27 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Chlorpheniramine 12 mg tablet 12 mg 12 HR Extended Release Oral Tablet Oral
Chlorpheniramine 4 mg tablet 4 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6976).
2 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070797.
3 BDDCS applied to over 900 drugs
4 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
6 Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
7 Combined histamine H1 and H3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion. Am J Rhinol. 1999 Sep-Oct;13(5):391-9.
8 Inhibition by histamine H1 receptor antagonists of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes. Eur J Pharmacol. 1994 Jan 1;266(1):99-102.
9 Carrier mediated transport of chlorpheniramine and chlorcyclizine across bovine olfactory mucosa: implications on nose-to-brain transport. J Pharm Sci. 2005 Mar;94(3):613-24.
10 Drug Interactions Flockhart Table
11 The roles of CYP2D6 and stereoselectivity in the clinical pharmacokinetics of chlorpheniramine. Br J Clin Pharmacol. 2002 May;53(5):519-25.
12 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
13 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
14 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
15 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
16 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
17 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
18 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
19 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
20 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
21 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
22 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
23 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
24 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
25 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
26 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
27 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
28 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
29 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
30 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
31 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
32 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
33 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
34 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
35 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
36 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
37 The role of cytochrome P450 3A (CYP3A) isoform(s) in oxidative metabolism of testosterone and benzphetamine in human adult and fetal liver. J Steroid Biochem Mol Biol. 1993 Jan;44(1):61-7.
38 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
39 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
40 The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
41 The role of bioreductive activation of doxorubicin in cytotoxic activity against leukaemia HL60-sensitive cell line and its multidrug-resistant sublines. Br J Cancer. 2005 Jul 11;93(1):89-97.
42 Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32.
43 Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1). Biochem Pharmacol. 2004 Apr 15;67(8):1541-8.
44 Hammerhead ribozyme against gamma-glutamylcysteine synthetase sensitizes human colonic cancer cells to cisplatin by down-regulating both the glutathione synthesis and the expression of multidrug resistance proteins. Cancer Gene Ther. 2001 Oct;8(10):803-14.
45 Multidrug resistance-associated protein-1 functional activity in Calu-3 cells. J Pharmacol Exp Ther. 2001 Sep;298(3):1199-205.
46 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
47 ATP-Dependent efflux of CPT-11 and SN-38 by the multidrug resistance protein (MRP) and its inhibition by PAK-104P. Mol Pharmacol. 1999 May;55(5):921-8.
48 Structural determinants of substrate specificity differences between human multidrug resistance protein (MRP) 1 (ABCC1) and MRP3 (ABCC3). Drug Metab Dispos. 2008 Dec;36(12):2571-81.
49 Evaluation of transport of common antiepileptic drugs by human multidrug resistance-associated proteins (MRP1, 2 and 5) that are overexpressed in pharmacoresistant epilepsy. Neuropharmacology. 2010 Jun;58(7):1019-32.
50 Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83.
51 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
52 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
53 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
54 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
55 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
56 Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
57 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
58 Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
59 Kulik AV, Wilbur R "Delirium and stereotypy from anticholinergic antiparkinson drugs." Prog Neuropsychopharmacol Biol Psychiatry 6 (1982): 75-82. [PMID: 7202232]
60 Cohen MA, Alfonso CA, Mosquera M. Development of urinary retention during treatment with clozapine and meclizine [published correction appears in Am J Psychiatry 1994 Jun;151(6):952]. Am J Psychiatry. 1994;151(4):619-620. [PMID: 8147469]
61 Multum Information Services, Inc. Expert Review Panel.
62 Cole JM, Sheehan AH, Jordan JK "Concomitant use of ipratropium and tiotropium in chronic obstructive plmonary disease." Ann Pharmacother 46 (2012): 1717-21. [PMID: 23170031]
63 Canadian Pharmacists Association.
64 Cerner Multum, Inc. "Australian Product Information.".
65 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
66 Product Information. Stribild (cobicistat/elvitegravir/emtricitabine/tenofov). Gilead Sciences, Foster City, CA.
67 Product Information. Givlaari (givosiran). Alnylam Pharmaceuticals, Cambridge, MA.
68 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
69 Product Information. Vizimpro (dacomitinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
70 Product Information. Zelboraf (vemurafenib). Genentech, South San Francisco, CA.
71 Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
72 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
73 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
74 Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
75 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
76 Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ.
77 Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
78 Dufresne RL, Weber SS, Becker RE "Bupropion hydrochloride." Drug Intell Clin Pharm 18 (1984): 957-64. [PMID: 6439541]
79 Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ.
80 Product Information. Zytiga (abiraterone). Centocor Inc, Malvern, PA.