RIZATRIPTAN

Details

Stereochemistry	ACHIRAL
Molecular Formula	C15H19N5
Molecular Weight	269.3449
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)CCC1=CNC2=CC=C(CN3C=NC=N3)C=C12

InChI

InChIKey=ULFRLSNUDGIQQP-UHFFFAOYSA-N

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

HIDE SMILES / InChI

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

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 46 Target ID: CHEMBL1898 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723	Agonist 2678	10.1 nM [Ki]
Serotonin 1d (5-HT1d) receptor 52 Target ID: CHEMBL1983 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723	Agonist 2678	3.0 nM [EC50]
Serotonin 1a (5-HT1a) receptor 172 Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9986723	Agonist 2678	140.0 nM [Ki]
Serotonin 2a (5-HT2a) receptor 231 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7752204	Agonist 2678	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 8429	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 8429	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
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
6.2 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
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
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
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
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
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
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
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

AUC

Value	Dose	Analyte	Population
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
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
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
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
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
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
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
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
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
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
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

T_1/2

Value	Dose	Analyte	Population
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
2.1 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
2.4 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
2.2 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
2.2 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/	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
2.9 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/	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/	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
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

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 n = 1 Health Status: unhealthy Age Group: 17 years Sex: F Population Size: 1 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 n = 2 Health Status: unhealthy Age Group: 25 years Sex: M Population Size: 2 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 n = 2 Health Status: unhealthy Age Group: 25-29 years Sex: M+F Population Size: 2 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 n = 2 Health Status: unhealthy Age Group: 29 years Sex: F Population Size: 2 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 Co-administed with:: tacrolimus(8.5 mg/day; oral) Sources: https://pubmed.ncbi.nlm.nih.gov/17112920	unhealthy, 43 years n = 1 Health Status: unhealthy Age Group: 43 years Sex: M Population Size: 1 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 n = 1 Health Status: unhealthy Age Group: 17 years Sex: F Population Size: 1 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 n = 2 Health Status: unhealthy Age Group: 25 years Sex: M Population Size: 2 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 n = 2 Health Status: unhealthy Age Group: 25 years Sex: M Population Size: 2 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 n = 2 Health Status: unhealthy Age Group: 25-29 years Sex: M+F Population Size: 2 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 n = 2 Health Status: unhealthy Age Group: 29 years Sex: F Population Size: 2 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 n = 2 Health Status: unhealthy Age Group: 29 years Sex: F Population Size: 2 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 Co-administed with:: tacrolimus(8.5 mg/day; oral) Sources: https://pubmed.ncbi.nlm.nih.gov/17112920	unhealthy, 43 years n = 1 Health Status: unhealthy Age Group: 43 years Sex: M Population Size: 1 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
MolPort	MolPort-003-666-600	https://www.molport.com/shop/molecule-link/MolPort-003-666-600
ZINC	ZINC000000005895	http://zinc15.docking.org/substances/ZINC000000005895
eMolecules	902426	https://www.emolecules.com/cgi-bin/more?vid=902426

PubMed

Title	Date	PubMed
Comparative aspects of triptans in treating migraine.	2001	12739316
Acute treatment of migraine and the role of triptans.	2001 Mar	11898508
Evidence-based migraine therapy.	2001 Nov	11903292
Cluster headache without autonomic symptoms?	2001 Nov	11903290
Triptans in the treatment of basilar migraine and migraine with prolonged aura.	2001 Nov-Dec	11903526
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
Rizatriptan: an update of its use in the management of migraine.	2002	12093318
Gateways to Clinical Trials.	2002 Apr	12087878
[Satisfaction and recovery of normal activity with rizatriptan 10 mg. Results from the open, prospective, observational 4M study].	2002 Dec	12487957
Comparison of triptan tablet consumption per attack: a prospective study of migraineurs in Spain.	2002 Feb	12005301
Migraine: diagnosis, management, and new treatment options.	2002 Feb	11859906
Molecular cloning and expression of the porcine trigeminal ganglion cDNA encoding a 5-ht(1F) receptor.	2002 Feb 1	11834243
Rizatriptan 5 mg for the acute treatment of migraine in adolescents: a randomized, double-blind, placebo-controlled study.	2002 Jan	12005275
Treatment of migraine with rizatriptan: when to take the medication.	2002 Jan	12005270
Tripstar: a comprehensive patient-based approach to compare triptans.	2002 Jan	11966860
The effect of rizatriptan, ergotamine, and their combination on human peripheral arteries: a double-blind, placebo-controlled, crossover study in normal subjects.	2002 Jul	12100223
Gateways to Clinical Trials. June 2002.	2002 Jun	12168506
Pharmacological treatments for acute migraine: quantitative systematic review.	2002 Jun	12044621
Rizatriptan combined with rofecoxib vs. rizatriptan for the acute treatment of migraine: an open label pilot study.	2002 May	12100094
CNS effects of sumatriptan and rizatriptan in healthy female volunteers.	2002 May	12100089
[Controlling migraine with highly effective triptanes. Lowers rate of drug use].	2002 May 6	12070871
[Good ruler for assessing effectiveness. Pain free with only one tablet].	2002 May 6	12070853
[New meta-analysis of triptanes. Concrete help, so the choice doesn't become overwhelming].	2002 May 6	12070852
Sum of Pain Intensity Differences (SPID) in migraine trials. A comment based on four rizatriptan trials.	2002 Oct	12383062
Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials.	2002 Oct	12383060
[New onset headache. Which patients should be sent for CT imaging?].	2002 Oct 24	12534022
Comparison of rizatriptan and other triptans on stringent measures of efficacy.	2002 Sep 10	12229911
Comparison of rizatriptan and other triptans on stringent measures of efficacy.	2002 Sep 10	12221187
Pharmacological approaches to migraine.	2003	12830928
Crossover comparison of efficacy and preference for rizatriptan 10 mg versus ergotamine/caffeine in migraine.	2003	12464714
Migraine headache recurrence: relationship to clinical, pharmacological, and pharmacokinetic properties of triptans.	2003 Apr	12656709
[New therapeutic recommendations for severe migraine. High beginning dosage rather than slow dosage increase].	2003 Jan 30	12619220
Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein.	2003 Jul	12814962
Safety profile of the triptans.	2003 Mar	12904112
Real-world experiences in migraine therapy with rizatriptan.	2003 Mar	12603640
[Highly selective beginning. Associated symptoms and side effects in retrospect].	2003 May 26	14579499
Cost-effectiveness of almotriptan and rizatriptan in the treatment of acute migraine.	2003 Nov	14693315
Patient-reported benefits of rizatriptan compared with usual non-triptan therapy for migraine in a primary care setting.	2003 Nov	14686564
Triptans for treatment of acute pediatric migraine: a systematic literature review.	2003 Nov	14684238
[It impairs quality of life and work time. Migraine therapy should not be left to the patients!].	2003 Nov 27	14725007
Endothelium-dependent relaxant responses to selective 5-HT(1B/1D) receptor agonists in the isolated middle cerebral artery of the rat.	2003 Nov-Dec	14691338
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 Oct	12954804
Naratriptan for the treatment of acute migraine: meta-analysis of randomised controlled trials.	2004 Feb	14998068
Evaluating triptan usage.	2004 Feb	14756865
Productivity cost benefit to employers of treating migraine with rizatriptan: a specific worksite analysis and model.	2004 Jan	14724478
Defeating migraine pain with triptans: a race against the development of cutaneous allodynia.	2004 Jan	14705108
CNS effects of sumatriptan and rizatriptan.	2004 Jan	14687019
Neuronal expression and regulation of CGRP promoter activity following viral gene transfer into cultured trigeminal ganglia neurons.	2004 Jan 30	14715155
Fast onset medications through thermally generated aerosols.	2004 May	14752061

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 `Fri Dec 15 15:53:26 GMT 2023` Edited by `admin` on `Fri Dec 15 15:53:26 GMT 2023`
Record UNII	51086HBW8G
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RIZATRIPTAN

Official Name

English

RIZATRIPTAN [MI]

Common Name

English

MK-462 FREE BASE

Code

English

Rizatriptan [WHO-DD]

Common Name

English

rizatriptan [INN]

Common Name

English

L-705126

Code

English

RIZATRIPTAN [VANDF]

Common Name

English

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

Systematic Name

English

Classification Tree Code System Code

NDF-RT

N0000175765