Details of the Drug

General Information of Drug (ID: DMDJMA3)

Drug Name

Rizatriptan

Synonyms

Risatriptan; Rizatriptanum; Rizatriptan benzoat; MK 462 free base; Maxalt (TN); Rizaliv (TN); Rizalt (TN); Rizatriptan (INN); Rizatriptan [INN:BAN]; N,N-Dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indole-3-ethanamine; N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine; N,N-Dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine; N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]-ethanamine; N,N-dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine

Indication

Disease Entry	ICD 11	Status	REF
Migraine	8A80	Approved	[1]
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Therapeutic Class

Antiinflammatory Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

269.34

Logarithm of the Partition Coefficient (xlogp)

1.7

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Half-life: The concentration or amount of drug in body reduced by one-half in 2 - 3 hours [2]
Metabolism: The drug is metabolized via the monoamine oxidase A isoenzyme (MAO-A) to an inactive indole acetic acid metabolite []
Vd: The volume of distribution (Vd) of drug is 140 L in male and 110 L in female []

Chemical Identifiers

Formula: C15H19N5
IUPAC Name: N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine
Canonical SMILES: CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3
InChI: InChI=1S/C15H19N5/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3
InChIKey: ULFRLSNUDGIQQP-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 5078
ChEBI ID: CHEBI:48273
CAS Number: 144034-80-0
DrugBank ID: DB00953
TTD ID: D0S9MU
VARIDT ID: DR01281
ACDINA ID: D00603

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 1D receptor (HTR1D)	TT6MSOK	5HT1D_HUMAN	Agonist	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Organic cation transporter 1 (SLC22A1)	DTT79CX	S22A1_HUMAN	Substrate	[4]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3 (GNB3)	OTA6HYBA	GBB3_HUMAN	Drug Response	[5]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Methylene blue	DMJAPE7	Major	Decreased metabolism of Rizatriptan caused by Methylene blue mediated inhibition of non-CYP450 enzyme.	Acquired methaemoglobinaemia [3A93]	[6]
Oliceridine	DM6MDCF	Moderate	Additive serotonergic effects by the combination of Rizatriptan and Oliceridine.	Acute pain [MG31]	[7]
Desipramine	DMT2FDC	Major	Additive serotonergic effects by the combination of Rizatriptan and Desipramine.	Attention deficit hyperactivity disorder [6A05]	[8]
Droxidopa	DM5YF4M	Moderate	Additive hypertensive effects by the combination of Rizatriptan and Droxidopa.	Autonomic nervous system disorder [8D87]	[9]
Dihydrocodeine	DMB0FWL	Moderate	Additive serotonergic effects by the combination of Rizatriptan and Dihydrocodeine.	Chronic pain [MG30]	[7]
Levomilnacipran	DMV26S8	Major	Additive serotonergic effects by the combination of Rizatriptan and Levomilnacipran.	Chronic pain [MG30]	[8]
Sertraline	DM0FB1J	Major	Additive serotonergic effects by the combination of Rizatriptan and Sertraline.	Depression [6A70-6A7Z]	[8]
Vilazodone	DM4LECQ	Major	Additive serotonergic effects by the combination of Rizatriptan and Vilazodone.	Depression [6A70-6A7Z]	[8]
Nefazodone	DM4ZS8M	Major	Additive serotonergic effects by the combination of Rizatriptan and Nefazodone.	Depression [6A70-6A7Z]	[8]
Vortioxetine	DM6F1PU	Major	Additive serotonergic effects by the combination of Rizatriptan and Vortioxetine.	Depression [6A70-6A7Z]	[8]
Isocarboxazid	DMAF1NB	Major	Decreased metabolism of Rizatriptan caused by Isocarboxazid mediated inhibition of non-CYP450 enzyme.	Depression [6A70-6A7Z]	[6]
Milnacipran	DMBFE74	Major	Additive serotonergic effects by the combination of Rizatriptan and Milnacipran.	Depression [6A70-6A7Z]	[8]
Escitalopram	DMFK9HG	Major	Additive serotonergic effects by the combination of Rizatriptan and Escitalopram.	Depression [6A70-6A7Z]	[8]
Desvenlafaxine	DMHD4PE	Major	Additive serotonergic effects by the combination of Rizatriptan and Desvenlafaxine.	Depression [6A70-6A7Z]	[8]
5-hydroxy-L-tryptophan	DMDWZGJ	Major	Additive serotonergic effects by the combination of Rizatriptan and 5-hydroxy-L-tryptophan.	Discovery agent [N.A.]	[10]
Procarbazine	DMIK367	Major	Decreased metabolism of Rizatriptan caused by Procarbazine mediated inhibition of non-CYP450 enzyme.	Hodgkin lymphoma [2B30]	[6]
Ozanimod	DMT6AM2	Moderate	Additive serotonergic effects by the combination of Rizatriptan and Ozanimod.	Multiple sclerosis [8A40]	[11]
Sibutramine	DMFJTDI	Major	Additive serotonergic effects by the combination of Rizatriptan and Sibutramine.	Obesity [5B80-5B81]	[6]
Lorcaserin	DMG6OYJ	Major	Additive serotonergic effects by the combination of Rizatriptan and Lorcaserin.	Obesity [5B80-5B81]	[12]
Dexfenfluramine	DMJ7YDS	Major	Additive serotonergic effects by the combination of Rizatriptan and Dexfenfluramine.	Obesity [5B80-5B81]	[8]
Levomethadyl Acetate	DM06HG5	Moderate	Additive serotonergic effects by the combination of Rizatriptan and Levomethadyl Acetate.	Opioid use disorder [6C43]	[7]
Oxymorphone	DM65AGJ	Moderate	Additive serotonergic effects by the combination of Rizatriptan and Oxymorphone.	Pain [MG30-MG3Z]	[7]
Dezocine	DMJDB0Y	Moderate	Additive serotonergic effects by the combination of Rizatriptan and Dezocine.	Pain [MG30-MG3Z]	[7]
Hydrocodone	DMQ2JO5	Moderate	Additive serotonergic effects by the combination of Rizatriptan and Hydrocodone.	Pain [MG30-MG3Z]	[7]
Pitolisant	DM8RFNJ	Moderate	Decreased metabolism of Rizatriptan caused by Pitolisant mediated inhibition of CYP450 enzyme.	Somnolence [MG42]	[13]
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⏷ Show the Full List of 25 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
Acesulfame	E00341	36573	Flavoring agent
Aminoethanoic acid	E00025	750	Buffering agent; Disintegrant; Lyophilization aid
Aspartame	E00402	134601	Flavoring agent
Isopropyl alcohol	E00070	3776	Antimicrobial preservative; Solvent
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Menthol	E00050	1254	Flavoring agent
Sodium stearyl fumarate	E00545	23665634	lubricant
Sucralose	E00370	71485	Flavoring agent
Calcium hydrogenphosphate	E00294	24441	Diluent
Calcium silicate	E00533	21910000	Adsorbent; Anticaking agent; Diluent; Opacifying agent
Carmellose sodium	E00625	Not Available	Disintegrant
Crospovidone	E00626	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
Hexahydric alcohol	E00083	5780	Diluent; Flavoring agent; Humectant; Plasticizing agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Monosodium citrate	E00550	23666341	Acidulant; Antimicrobial preservative; Buffering agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium chloride	E00077	5234	Diluent; Tonicity agent
Xylitol	E00136	6912	Coating agent; Diluent; Emollient; Flavoring agent; Humectant
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⏷ Show the Full List of 20 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Rizatriptan 10 mg tablet	10 mg	Disintegrating Oral Tablet	Oral
Rizatriptan 5 mg tablet	5 mg	Disintegrating Oral Tablet	Oral
Rizatriptan 10 mg tablet	10 mg	Oral Tablet	Oral
Rizatriptan 5 mg tablet	5 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	Clinical pipeline report, company report or official report of Intelgenx.
2	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
3	An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.
4	OCT1 mediates hepatic uptake of sumatriptan and loss-of-function OCT1 polymorphisms affect sumatriptan pharmacokinetics. Clin Pharmacol Ther. 2016 Jun;99(6):633-41.
5	G protein beta3 polymorphism and triptan response in cluster headache. Clin Pharmacol Ther. 2007 Oct;82(4):396-401. doi: 10.1038/sj.clpt.6100159. Epub 2007 Mar 14.
6	Chan BSH, Graudins A, Whyte IM, Dawson AH, Braitberg G, Duggin GG "Serotonin syndrome resulting from drug interactions." Med J Aust 169 (1998): 523-5. [PMID: 9861909]
7	Vizcaychipi MP, Walker S, Palazzo M "Serotonin syndrome triggered by tramadol." Br J Anaesth 99 (2007): 919. [PMID: 18006535]
8	Achamallah NS "Visual hallucinations after combining fluoxetine and dextromethorphan ." Am J Psychiatry 149 (1992): 1406. [PMID: 1530079]
9	Product Information. Northera (droxidopa). Chelsea Therapeutics Inc, Charlotte, NC.
10	Ciraulo DA, Shader RI "Fluoxetine drug-drug interactions: I. Antidepressants and antipsychotics." J Clin Psychopharmacol 10 (1990): 48-50. [PMID: 1968472]
11	Alvine G, Black DW, Tsuang D "Case of delirium secondary to phenelzine/L-tryptophan combination." J Clin Psychiatry 51 (1990): 311. [PMID: 2365671]
12	Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ.
13	Cerner Multum, Inc. "UK Summary of Product Characteristics.".