Details of the Drug

General Information of Drug (ID: DM92AH3)

• Drug Name: Cyproheptadine
• Synonyms: Ciproheptadina; Ciprovit; Cypoheptadine; Cyproheptadiene; Cyproheptadinum; Dihexazin; Dronactin; Eiproheptadine; Periactin; Periactine; Periactinol; Viternum; Cyproheptadine Hcl; MK 141; Ciproheptadina [INN-Spanish]; Ciprovit (TN); Cyproheptadine (INN); Cyproheptadine [INN:BAN]; Cyproheptadinum [INN-Latin]; Dibenzosuberonone/Cyproheptadine; Periactin (TN); 1-Methyl-4-(5-dibenzo(a,e)cycloheptatrienylidene)piperidine; 1-Methyl-4-(5H-dibenzo(a,d)cycloheptenylidene)piperidine; 4-(5-Dibenzo(a,d)cyclohepten-5-ylidine)-1-methylpiperidine; 4-(5H-Dibenzo(a,d)cyclohepten-5-ylidene)-1-methylpiperidene; 4-(5H-Dibenzo(a,d)cyclohepten-5-ylidene)-1-methylpiperidine; 4-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-1-methylpiperidine; 4-(5H-dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine; 5-(1-Methylpiperidylidene-4)-5H-dibenzo(a,d)cyclopheptene

Indication

Disease Entry	ICD 11	Status	REF
Rhinitis	FA20	Approved	[1]

• Therapeutic Class: Antihistamines
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 287.4
  Topological Polar Surface Area (xlogp); 4.7
  Rotatable Bond Count (rotbonds); 0
  Hydrogen Bond Donor Count (hbonddonor); 0
  Hydrogen Bond Acceptor Count (hbondacc); 1
• ADMET Property:
  Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 209 mcgh/L [2]
  Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 30.0 mcg/L [2]
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
  Elimination: Approximately 2-20% of the radioactivity from an orally administered radio-labeled dose of cyproheptadine is excreted in the feces, of which approximately 34% is unchanged parent drug (less than 5.7% of the total dose) [4]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.73969 micromolar/kg/day [5]
  Water Solubility: The ability of drug to dissolve in water is measured as 3.636 mg/mL [3]
• Chemical Identifiers:
  Formula: C21H21N
  IUPAC Name: 1-methyl-4-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,9,11,13-heptaenylidene)piperidine
  Canonical SMILES: CN1CCC(=C2C3=CC=CC=C3C=CC4=CC=CC=C42)CC1
  InChI: InChI=1S/C21H21N/c1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21/h2-11H,12-15H2,1H3
  InChIKey: JJCFRYNCJDLXIK-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 2913
  ChEBI ID: CHEBI:4046
  CAS Number: 129-03-3
  DrugBank ID: DB00434
  TTD ID: D00TLN
  VARIDT ID: DR00776
  INTEDE ID: DR0395
  ACDINA ID: D00160

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]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Substrate	[8]
UDP-glucuronosyltransferase 1A3 (UGT1A3)	DEF2WXN	UD13_HUMAN	Substrate	[9]

Molecular Expression Atlas of This Drug

• The Studied Disease: Rhinitis
• ICD Disease Classification: FA20

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
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	4.53E-01	4.14E-02	1.83E-01

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Cyproheptadine (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Scopolamine	DMOM8AL	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Scopolamine.	Addictive disorder [6C50-6C5Z]	[36]
Mepyramine	DMB4SFH	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Mepyramine.	Allergic/hypersensitivity disorder [4A80-4A8Z]	[37]
Phenyltoloxamine	DMKAEQW	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Phenyltoloxamine.	Allergic/hypersensitivity disorder [4A80-4A8Z]	[37]
Tripelennamine	DMZBU15	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Tripelennamine.	Allergic/hypersensitivity disorder [4A80-4A8Z]	[36]
Memantine	DMD9WSC	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Memantine.	Alzheimer disease [8A20]	[36]
Galantamine	DMEO794	Moderate	Antagonize the effect of Cyproheptadine when combined with Galantamine.	Alzheimer disease [8A20]	[38]
Rivastigmine	DMG629M	Moderate	Antagonize the effect of Cyproheptadine when combined with Rivastigmine.	Alzheimer disease [8A20]	[38]
Donepezil	DMIYG7Z	Moderate	Antagonize the effect of Cyproheptadine when combined with Donepezil.	Alzheimer disease [8A20]	[38]
Hydroxyzine	DMF8Y74	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Hydroxyzine.	Anxiety disorder [6B00-6B0Z]	[36]
Desipramine	DMT2FDC	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Desipramine.	Attention deficit hyperactivity disorder [6A05]	[36]
Linezolid	DMGFPU2	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Linezolid.	Bacterial infection [1A00-1C4Z]	[39]
Cariprazine	DMJYDVK	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Cariprazine.	Bipolar disorder [6A60]	[36]
Loperamide	DMOJZQ9	Moderate	Additive antimotility effects by the combination of Cyproheptadine and Loperamide.	Bowel habit change [ME05]	[40]
Acetylcholine	DMDF79Z	Moderate	Antagonize the effect of Cyproheptadine when combined with Acetylcholine.	Cataract [9B10]	[41]
Umeclidinium	DM4E8O9	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Umeclidinium.	Chronic obstructive pulmonary disease [CA22]	[42]
Tiotropium	DMFDC0Q	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Tiotropium.	Chronic obstructive pulmonary disease [CA22]	[42]
Revefenacin	DMMP5SI	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Revefenacin.	Chronic obstructive pulmonary disease [CA22]	[42]
Olopatadine	DMKMWQG	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Olopatadine.	Conjunctiva disorder [9A60]	[43]
Ethanol	DMDRQZU	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Ethanol.	Cystitis [GC00]	[43]
Trimipramine	DM1SC8M	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Trimipramine.	Depression [6A70-6A7Z]	[36]
Cyclobenzaprine	DM1YBRM	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Cyclobenzaprine.	Depression [6A70-6A7Z]	[36]
Imipramine	DM2NUH3	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Imipramine.	Depression [6A70-6A7Z]	[36]
Nortriptyline	DM4KDYJ	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Nortriptyline.	Depression [6A70-6A7Z]	[36]
Isocarboxazid	DMAF1NB	Moderate	Antagonize the effect of Cyproheptadine when combined with Isocarboxazid.	Depression [6A70-6A7Z]	[44]
Tranylcypromine	DMGB5RE	Moderate	Antagonize the effect of Cyproheptadine when combined with Tranylcypromine.	Depression [6A70-6A7Z]	[44]
OPC-34712	DMHG57U	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and OPC-34712.	Depression [6A70-6A7Z]	[36]
Phenelzine	DMHIDUE	Moderate	Antagonize the effect of Cyproheptadine when combined with Phenelzine.	Depression [6A70-6A7Z]	[44]
Clomipramine	DMINRKW	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Clomipramine.	Depression [6A70-6A7Z]	[36]
Amoxapine	DMKITQE	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Amoxapine.	Depression [6A70-6A7Z]	[36]
Doxepin	DMPI98T	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Doxepin.	Depression [6A70-6A7Z]	[37]
Maprotiline	DMPWB7T	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Maprotiline.	Depression [6A70-6A7Z]	[36]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Esketamine.	Depression [6A70-6A7Z]	[45]
Mepenzolate	DM8YU2F	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Mepenzolate.	Digestive system disease [DE2Z]	[36]
Oxybutynine	DMJPBAX	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Oxybutynine.	Discovery agent [N.A.]	[36]
Meclizine	DMS7T13	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Meclizine.	Dizziness and giddiness [MB48]	[36]
Zonisamide	DM0DTF7	Major	Increased risk of hyperpyrexia by the combination of Cyproheptadine and Zonisamide.	Epilepsy/seizure [8A61-8A6Z]	[46]
Diphenhydramine	DMKQTBA	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Diphenhydramine.	Episodic vestibular syndrome [AB31]	[36]
Solifenacin	DMG592Q	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Solifenacin.	Functional bladder disorder [GC50]	[36]
Tolterodine	DMSHPW8	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Tolterodine.	Functional bladder disorder [GC50]	[36]
Darifenacin	DMWXLYZ	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Darifenacin.	Functional bladder disorder [GC50]	[36]
Propantheline	DM2EN6G	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Propantheline.	Gastric ulcer [DA60]	[36]
Isoflurophate	DMBSK7X	Moderate	Antagonize the effect of Cyproheptadine when combined with Isoflurophate.	Glaucoma [9C61]	[41]
Brimonidine	DMQLT4N	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Brimonidine.	Glaucoma [9C61]	[47]
Pilocarpine	DMV9ADG	Moderate	Antagonize the effect of Cyproheptadine when combined with Pilocarpine.	Glaucoma [9C61]	[41]
Procarbazine	DMIK367	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Procarbazine.	Hodgkin lymphoma [2B30]	[39]
Belladonna	DM2RBWK	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Belladonna.	Infectious gastroenteritis/colitis [1A40]	[36]
Amantadine	DMS3YE9	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Amantadine.	Influenza [1E30-1E32]	[48]
Propiomazine	DMKY8V1	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Propiomazine.	Insomnia [7A00-7A0Z]	[36]
ITI-007	DMUQ1DO	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and ITI-007.	Insomnia [7A00-7A0Z]	[36]
Clidinium	DMUMQZ0	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Clidinium.	Irritable bowel syndrome [DD91]	[36]
Dicyclomine	DMZSDGX	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Dicyclomine.	Irritable bowel syndrome [DD91]	[36]
Physostigmine	DM2N0TO	Moderate	Antagonize the effect of Cyproheptadine when combined with Physostigmine.	Lips/oral mucosa miscellaneous disorder [DA02]	[38]
Porfimer Sodium	DM7ZWNY	Moderate	Increased risk of photosensitivity reactions by the combination of Cyproheptadine and Porfimer Sodium.	Lung cancer [2C25]	[49]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[50]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Lasmiditan.	Migraine [8A80]	[51]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Flibanserin.	Mood disorder [6A60-6E23]	[52]
Thalidomide	DM70BU5	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Thalidomide.	Multiple myeloma [2A83]	[53]
Phenindamine	DMDTC7R	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Phenindamine.	Nasopharyngitis [CA00]	[36]
Dimenhydrinate	DM264B3	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Dimenhydrinate.	Nausea/vomiting [MD90]	[36]
Promethazine	DM6I5GR	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Promethazine.	Nausea/vomiting [MD90]	[36]
Cyclizine	DM9G7BS	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Cyclizine.	Nausea/vomiting [MD90]	[36]
Apraclonidine	DMO4PVE	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Apraclonidine.	Optic nerve disorder [9C40]	[47]
Dextropropoxyphene	DM23HCX	Major	Additive CNS depression effects by the combination of Cyproheptadine and Dextropropoxyphene.	Pain [MG30-MG3Z]	[54]
Flavoxate	DMKV4NL	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Flavoxate.	Pain [MG30-MG3Z]	[36]
Biperiden	DME78OA	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Biperiden.	Parkinsonism [8A00]	[36]
Orphenadrine	DMW542E	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Orphenadrine.	Parkinsonism [8A00]	[36]
Methylscopolamine	DM5VWOB	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Methylscopolamine.	Peptic ulcer [DA61]	[36]
Levomepromazine	DMIKFEL	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Levomepromazine.	Psychotic disorder [6A20-6A25]	[36]
Fluphenazine	DMIT8LX	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Fluphenazine.	Psychotic disorder [6A20-6A25]	[36]
Triflupromazine	DMKFQJP	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Triflupromazine.	Psychotic disorder [6A20-6A25]	[36]
Quetiapine	DM1N62C	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Quetiapine.	Schizophrenia [6A20]	[36]
Mesoridazine	DM2ZGAN	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Mesoridazine.	Schizophrenia [6A20]	[36]
Thioridazine	DM35M8J	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Thioridazine.	Schizophrenia [6A20]	[36]
Aripiprazole	DM3NUMH	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Aripiprazole.	Schizophrenia [6A20]	[36]
Iloperidone	DM6AUFY	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Iloperidone.	Schizophrenia [6A20]	[36]
Paliperidone	DM7NPJS	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Paliperidone.	Schizophrenia [6A20]	[36]
Haloperidol	DM96SE0	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Haloperidol.	Schizophrenia [6A20]	[36]
Perphenazine	DMA4MRX	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Perphenazine.	Schizophrenia [6A20]	[36]
Molindone	DMAH70G	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Molindone.	Schizophrenia [6A20]	[36]
Chlorpromazine	DMBGZI3	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Chlorpromazine.	Schizophrenia [6A20]	[36]
Thiothixene	DMDINC4	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Thiothixene.	Schizophrenia [6A20]	[36]
Trifluoperazine	DMKBYWI	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Trifluoperazine.	Schizophrenia [6A20]	[36]
Risperidone	DMN6DXL	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Risperidone.	Schizophrenia [6A20]	[36]
Asenapine	DMSQZE2	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Asenapine.	Schizophrenia [6A20]	[36]
Pimozide	DMW83TP	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Pimozide.	Schizophrenia [6A20]	[36]
Tizanidine	DMR2IQ4	Moderate	Additive CNS depression effects by the combination of Cyproheptadine and Tizanidine.	Tonus and reflex abnormality [MB47]	[55]
Atropine	DMEN6X7	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Atropine.	Unspecific substance harmful effect [NE6Z]	[36]
Methdilazine	DMAUHQX	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Methdilazine.	Vasomotor/allergic rhinitis [CA08]	[36]
Carbinoxamine	DMCT31R	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Carbinoxamine.	Vasomotor/allergic rhinitis [CA08]	[36]
Trimeprazine	DMEMV9D	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[37]
Brompheniramine	DMFOVSD	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Brompheniramine.	Vasomotor/allergic rhinitis [CA08]	[36]
Acrivastine	DMTIGA0	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Acrivastine.	Vasomotor/allergic rhinitis [CA08]	[36]
Azatadine	DMZ80SB	Moderate	Additive anticholinergic effects by the combination of Cyproheptadine and Azatadine.	Vasomotor/allergic rhinitis [CA08]	[36]

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

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Cyproheptadine Hydrochloride 4mg tablet	4mg	Tablet	Oral
Cyproheptadine 4 mg tablet	4 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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