RIZATRIPTAN SULFATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	2C15H19N5.H2O.H2O4S
Molecular Weight	654.783
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.OS(O)(=O)=O.CN(C)CCC1=CNC2=C1C=C(CN3C=NC=N3)C=C2.CN(C)CCC4=CNC5=C4C=C(CN6C=NC=N6)C=C5

InChI

InChIKey=SMWLLNMVQNVPLD-UHFFFAOYSA-N

InChI=1S/2C15H19N5.H2O4S.H2O/c2*1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20;1-5(2,3)4;/h2*3-4,7-8,10-11,17H,5-6,9H2,1-2H3;(H2,1,2,3,4);1H2

HIDE SMILES / InChI

Molecular Formula	H2O4S
Molecular Weight	98.078
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C15H19N5
Molecular Weight	269.3449
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.drugbank.ca/drugs/DB00953 | https://www.drugs.com/pro/rizatriptan-orally-disintegrating-tablets.html | http://reference.medscape.com/drug/maxalt-maxalt-mlt-rizatriptan-343033 | https://www.ncbi.nlm.nih.gov/pubmed/9357514

Rizatriptan (trade name Maxalt) is a 5-HT1 receptor agonist of the triptan class of drugs developed by Merck & Co. for the treatment of migraine headaches. Rizatriptan (trade name Maxalt) is a 5-HT1 receptor agonist of the triptan class of drugs developed by Merck & Co. for the treatment of migraine headaches. Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors. Rizatriptan binds with high affinity to human cloned 5-HT1B/1D receptors. Rizatriptan benzoate presumably exerts its therapeutic effects in the treatment of a migraine headache by binding to 5-HT1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system. Rizatriptan is completely absorbed following oral administration. The mean oral absolute bioavailability of the rizatriptan benzoate tablet is about 45%, and mean peak plasma concentrations are reached in approximately 1-1.5 hours. The presence of a migraine headache did not appear to affect the absorption or pharmacokinetics of rizatriptan. Food has no significant effect on the bioavailability of rizatriptan but delays the time to reach peak concentration by an hour. The primary route of rizatriptan metabolism is via oxidative deamination by monoamine oxidase-A (MAO-A) to the indole acetic acid metabolite, which is not active at the 5-HT1B/1D receptor. N-mono-desmethyl-rizatriptan, a metabolite with activity similar to that of parent compound at the 5-HT1B/1D receptor, is formed to a minor degree. Plasma concentrations of N-mono-desmethyl-rizatriptan are approximately 14% of those of parent compound, and it is eliminated at a similar rate. Other minor metabolites, the N-oxide, the 6-hydroxy compound, and the sulfate conjugate of the 6-hydroxy metabolite are not active at the 5-HT1B/1D receptor.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Serotonin 1b (5-HT1b) receptor 45 Target ID: CHEMBL1898 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723	Agonist 2752	10.1 nM [Ki]
Serotonin 1d (5-HT1d) receptor 53 Target ID: CHEMBL1983 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723	Agonist 2752	3.0 nM [EC50]
Serotonin 1a (5-HT1a) receptor 177 Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723	Agonist 2752	140.0 nM [Ki]
Serotonin 2a (5-HT2a) receptor 237 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7752204	Agonist 2752	7.9 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Migraine with aura 11 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	Primary		Approved 8583	MAXALT Approved Use MAXALT is indicated for the acute treatment of migraine attacks with or without aura in adults. MAXALT is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see CONTRAINDICATIONS). Safety and effectiveness of MAXALT have not been established for cluster headache, which is present in an older, predominantly male population. Launch Date 1998
Migraine with aura 11 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	Primary		Approved 8583	MAXALT Approved Use MAXALT is indicated for the acute treatment of migraine attacks with or without aura in adults. MAXALT is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see CONTRAINDICATIONS). Safety and effectiveness of MAXALT have not been established for cluster headache, which is present in an older, predominantly male population. Launch Date 1998

C_max

Value	Dose	Analyte	Population
6.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
12.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
28.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
44.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
13.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
32.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
54 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
27.29 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16432269/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
16 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
33 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
72 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
127 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
19 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
42 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
97 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
161 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
68 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
84 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
69.88 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16432269/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
2.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
2.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
2.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10233200/	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:	RIZATRIPTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
10 mg single, oral Recommended Dose: 10 mg Route: oral Route: single Dose: 10 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23084593	unhealthy, 17 years Health Status: unhealthy Age Group: 17 years Sex: F Sources: https://pubmed.ncbi.nlm.nih.gov/23084593	Other AEs: Jaundice... Other AEs: Jaundice Sources: https://pubmed.ncbi.nlm.nih.gov/23084593
80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	unhealthy, 25 years Health Status: unhealthy Age Group: 25 years Sex: M Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	Other AEs: Syncope, Incontinence... Other AEs: Syncope (1 patient) Incontinence (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	unhealthy, 25-29 years Health Status: unhealthy Age Group: 25-29 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	Other AEs: Dizziness... Other AEs: Dizziness (2 patients) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	unhealthy, 29 years Health Status: unhealthy Age Group: 29 years Sex: F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	Other AEs: Vomiting, Bradycardia... Other AEs: Vomiting (1 patient) Bradycardia (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
10 mg 2 times / day multiple, oral Recommended Dose: 10 mg, 2 times / day Route: oral Route: multiple Dose: 10 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17112920	unhealthy, 43 years Health Status: unhealthy Age Group: 43 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/17112920	Disc. AE: Transient ischemic attack... AEs leading to discontinuation/dose reduction: Transient ischemic attack Sources: https://pubmed.ncbi.nlm.nih.gov/17112920

AEs

AE	Significance	Dose	Population
Jaundice		10 mg single, oral Recommended Dose: 10 mg Route: oral Route: single Dose: 10 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23084593	unhealthy, 17 years Health Status: unhealthy Age Group: 17 years Sex: F Sources: https://pubmed.ncbi.nlm.nih.gov/23084593
Incontinence	1 patient	80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	unhealthy, 25 years Health Status: unhealthy Age Group: 25 years Sex: M Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
Syncope	1 patient	80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	unhealthy, 25 years Health Status: unhealthy Age Group: 25 years Sex: M Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
Dizziness	2 patients	80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	unhealthy, 25-29 years Health Status: unhealthy Age Group: 25-29 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
Bradycardia	1 patient	80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	unhealthy, 29 years Health Status: unhealthy Age Group: 29 years Sex: F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
Vomiting	1 patient	80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf	unhealthy, 29 years Health Status: unhealthy Age Group: 29 years Sex: F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/20864lbl.pdf
Transient ischemic attack	Disc. AE	10 mg 2 times / day multiple, oral Recommended Dose: 10 mg, 2 times / day Route: oral Route: multiple Dose: 10 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17112920	unhealthy, 43 years Health Status: unhealthy Age Group: 43 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/17112920

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:48273	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:48273
ChemicalBook	CB3245026	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB3245026
eMolecules	902426	https://www.emolecules.com/cgi-bin/more?vid=902426
MolPort	MolPort-003-666-600	https://www.molport.com/shop/molecule-link/MolPort-003-666-600
ZINC	ZINC000000005895	http://zinc15.docking.org/substances/ZINC000000005895

PubMed

Title	Date	PubMed
Fast onset medications through thermally generated aerosols.	2004-05	14752061
Naratriptan for the treatment of acute migraine: meta-analysis of randomised controlled trials.	2004-02	14998068
Evaluating triptan usage.	2004-02	14756865
Neuronal expression and regulation of CGRP promoter activity following viral gene transfer into cultured trigeminal ganglia neurons.	2004-01-30	14715155
Productivity cost benefit to employers of treating migraine with rizatriptan: a specific worksite analysis and model.	2004-01	14724478
Defeating migraine pain with triptans: a race against the development of cutaneous allodynia.	2004-01	14705108
CNS effects of sumatriptan and rizatriptan.	2004-01	14687019
[It impairs quality of life and work time. Migraine therapy should not be left to the patients!].	2003-11-27	14725007
Meta-analysis of oral triptan therapy for migraine: number needed to treat and relative cost to achieve relief within 2 hours.	2003-11-14	14613361
Cost-effectiveness of almotriptan and rizatriptan in the treatment of acute migraine.	2003-11	14693315
Patient-reported benefits of rizatriptan compared with usual non-triptan therapy for migraine in a primary care setting.	2003-11	14686564
Triptans for treatment of acute pediatric migraine: a systematic literature review.	2003-11	14684238
An in vitro interethnic comparison of monoamine oxidase activities between Japanese and Caucasian livers using rizatriptan, a serotonin receptor 1B/1D agonist, as a model drug.	2003-11	14651728
Rizatriptan RPD for severe migraine in the emergency department--a multicenter study.	2003-10	14585450
Investigation of the effects of naratriptan, rizatriptan, and sumatriptan on jugular venous oxygen saturation in anesthetized pigs: implications for their mechanism of acute antimigraine action.	2003-10	12954804
Migraine: diagnosis and management.	2003-09-27	14511196
Almotriptan versus rizatriptan in patients with migraine in Spain.	2003-08-02	12890128
Migraine treatment patterns and patient satisfaction with prior therapy: a substudy of a multicenter trial of rizatriptan effectiveness.	2003-07	12946550
Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein.	2003-07	12814962
[Highly selective beginning. Associated symptoms and side effects in retrospect].	2003-05-26	14579499
Migraine headache recurrence: relationship to clinical, pharmacological, and pharmacokinetic properties of triptans.	2003-04	12656709
Safety profile of the triptans.	2003-03	12904112
Real-world experiences in migraine therapy with rizatriptan.	2003-03	12603640
[New therapeutic recommendations for severe migraine. High beginning dosage rather than slow dosage increase].	2003-01-30	12619220
Endothelium-dependent relaxant responses to selective 5-HT(1B/1D) receptor agonists in the isolated middle cerebral artery of the rat.	2003-01-22	14691338
Coprescription of triptans with potentially interacting medications: a cohort study involving 240,268 patients.	2003-01	12864757
Newer formulations of the triptans: advances in migraine management.	2003	14524731
Pharmacological approaches to migraine.	2003	12830928
Crossover comparison of efficacy and preference for rizatriptan 10 mg versus ergotamine/caffeine in migraine.	2003	12464714
[Satisfaction and recovery of normal activity with rizatriptan 10 mg. Results from the open, prospective, observational 4M study].	2002-12	12487957
[New onset headache. Which patients should be sent for CT imaging?].	2002-10-24	12534022
Further evaluation of rizatriptan in menstrual migraine: retrospective analysis of long-term data.	2002-10	12390621
Determinants of migraine-specific quality of life.	2002-10	12383065
Sum of Pain Intensity Differences (SPID) in migraine trials. A comment based on four rizatriptan trials.	2002-10	12383062
Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials.	2002-10	12383060
Comparison of rizatriptan and other triptans on stringent measures of efficacy.	2002-09-10	12229911
Comparison of rizatriptan and other triptans on stringent measures of efficacy.	2002-09-10	12221187
Rizatriptan 5mg is not efficacious for migraine in adolescents.	2002-09	12390657
Mechanisms of action of the 5-HT1B/1D receptor agonists.	2002-07	12117355
The effect of rizatriptan, ergotamine, and their combination on human peripheral arteries: a double-blind, placebo-controlled, crossover study in normal subjects.	2002-07	12100223
Gateways to Clinical Trials. June 2002.	2002-06	12168506
Rizatriptan combined with rofecoxib vs. rizatriptan for the acute treatment of migraine: an open label pilot study.	2002-05	12100094
[Treatment of migraine in patients with hypertension and ischemic heart disease].	2002-01-20	12122940
An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy.	2002	12434581
Impact of migraine symptoms on health care use and work loss in Canada in patients randomly assigned in a phase III clinical trial.	2002	12422253
Restoring migraine sufferers' ability to function normally: a comparison of rizatriptan and other triptans in randomized trials.	2002	12373035
Spotlight on rizatriptan in migraine.	2002	12269863
Comparative aspects of triptans in treating migraine.	2001	12739316
Rizatriptan: pharmacological differences from sumatriptan and clinical results.	2001	12463279
Sumatriptan: pharmacological basis and clinical results.	2001	12463276

Patents

Sample Use Guides

In Vivo Use Guide

5-10 mg PO at onset of symptoms; repeat dose after 2 hours if necessary; not to exceed 30 mg/24 hr

Route of Administration: Oral

In Vitro Use Guide

Rizatriptan intrinsic efficacy, expressed as percent of the maximal 5-HT response, was measured in cloned human 5-HT1D and 5-HT1B receptors stably expressed in CHO cells using agonist-induced [35S]GTPγS binding. In this assay, interaction of the agonist-occupied receptor with the G-protein results in dissociation of GDP from the G-protein R-subunit and the binding of a molecule of GTP. Under normal conditions the R-subunit dissociates from the âγ-subunits and, following modulation of its effector, intrinsic R-subunit GTPase hydrolyzes the GTP to GDP. Because [35S]GTPγS is resistant to this GTPase, it accumulates in the membrane and it can be measured by virtue of its radiolabel

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:12:10 GMT 2025` Edited by `admin` on `Mon Mar 31 18:12:10 GMT 2025`
Record UNII	13RRH2218G
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RIZATRIPTAN SULFATE

Official Name

English

RIZATRIPTAN HEMISULFATE HEMIHYDRATE

Preferred Name

English

RIZATRIPTAN SULPHATE

Common Name

English

RIZATRIPTAN SULFATE [USAN]

Common Name

English

MK-A462

Code

English

1H-INDOLE-3-ETHANAMINE, N,N-DIMETHYL-5-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-, SULFATE, HYDRATE (2:1:1)

Systematic Name

English

3-[2-(Dimethylamino)ethyl]-5-(1H-1,2,4-triazol-1-ylmethyl)indole sulfate (2:1), monohydrate

Common Name

English

RIZATRIPTAN SULFATE HYDRATE

Common Name

English

Rizatriptan sulfate [WHO-DD]

Common Name

English

1H-INDOLE-3-ETHANAMINE, N,N-DIMETHYL-5-(1H-1,2,4-TRIAZOL-1-YLMETHYL)-, SULFATE (2:1), MONOHYDRATE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C47794