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Details

Stereochemistry ACHIRAL
Molecular Formula C15H19N5
Molecular Weight 269.3454
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RIZATRIPTAN

SMILES

CN(C)CCc1c[nH]c2ccc(cc12)Cn3cncn3

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 269.3454
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
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.

Originator

Curator's Comment:: # Merck Sharp and Dohme Ltd.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
10.1 nM [Ki]
3.0 nM [EC50]
140.0 nM [Ki]
7.9 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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

8.9907842E11
Primary
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

8.9907842E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
44.8 ng/mL
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
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
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
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
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
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
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
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
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

AUC

ValueDoseCo-administeredAnalytePopulation
127 ng × h/mL
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
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
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
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
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
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
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
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
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
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
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.4 h
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
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
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
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
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
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
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
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
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
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

Doses

DosePopulationAdverse events​
10 mg single, oral
Recommended
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 17 years
n = 1
Health Status: unhealthy
Age Group: 17 years
Sex: F
Population Size: 1
Sources:
Other AEs: Jaundice...
Other AEs:
Jaundice
Sources:
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 25 years
n = 2
Health Status: unhealthy
Age Group: 25 years
Sex: M
Population Size: 2
Sources:
Other AEs: Syncope, Incontinence...
Other AEs:
Syncope (1 patient)
Incontinence (1 patient)
Sources:
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 25-29 years
n = 2
Health Status: unhealthy
Age Group: 25-29 years
Sex: M+F
Population Size: 2
Sources:
Other AEs: Dizziness...
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 29 years
n = 2
Health Status: unhealthy
Age Group: 29 years
Sex: F
Population Size: 2
Sources:
Other AEs: Vomiting, Bradycardia...
Other AEs:
Vomiting (1 patient)
Bradycardia (1 patient)
Sources:
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:
unhealthy, 43 years
n = 1
Health Status: unhealthy
Age Group: 43 years
Sex: M
Population Size: 1
Sources:
Disc. AE: Transient ischemic attack...
AEs leading to
discontinuation/dose reduction:
Transient ischemic attack
Sources:
AEs

AEs

AESignificanceDosePopulation
Jaundice
10 mg single, oral
Recommended
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 17 years
n = 1
Health Status: unhealthy
Age Group: 17 years
Sex: F
Population Size: 1
Sources:
Incontinence 1 patient
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 25 years
n = 2
Health Status: unhealthy
Age Group: 25 years
Sex: M
Population Size: 2
Sources:
Syncope 1 patient
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 25 years
n = 2
Health Status: unhealthy
Age Group: 25 years
Sex: M
Population Size: 2
Sources:
Dizziness 2 patients
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 25-29 years
n = 2
Health Status: unhealthy
Age Group: 25-29 years
Sex: M+F
Population Size: 2
Sources:
Bradycardia 1 patient
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 29 years
n = 2
Health Status: unhealthy
Age Group: 29 years
Sex: F
Population Size: 2
Sources:
Vomiting 1 patient
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 29 years
n = 2
Health Status: unhealthy
Age Group: 29 years
Sex: F
Population Size: 2
Sources:
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:
unhealthy, 43 years
n = 1
Health Status: unhealthy
Age Group: 43 years
Sex: M
Population Size: 1
Sources:
PubMed

PubMed

TitleDatePubMed
Comparative aspects of triptans in treating migraine.
2001
Sumatriptan: pharmacological basis and clinical results.
2001
Acute treatment of migraine and the role of triptans.
2001 Mar
Evidence-based migraine therapy.
2001 Nov
Cluster headache without autonomic symptoms?
2001 Nov
Triptans in the treatment of basilar migraine and migraine with prolonged aura.
2001 Nov-Dec
An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy.
2002
Restoring migraine sufferers' ability to function normally: a comparison of rizatriptan and other triptans in randomized trials.
2002
Gateways to Clinical Trials.
2002 Apr
[Satisfaction and recovery of normal activity with rizatriptan 10 mg. Results from the open, prospective, observational 4M study].
2002 Dec
Treatment of migraine with rizatriptan: when to take the medication.
2002 Jan
Tripstar: a comprehensive patient-based approach to compare triptans.
2002 Jan
[Treatment of migraine in patients with hypertension and ischemic heart disease].
2002 Jan 20
Mechanisms of action of the 5-HT1B/1D receptor agonists.
2002 Jul
The effect of rizatriptan, ergotamine, and their combination on human peripheral arteries: a double-blind, placebo-controlled, crossover study in normal subjects.
2002 Jul
Gateways to Clinical Trials. June 2002.
2002 Jun
Pharmacological treatments for acute migraine: quantitative systematic review.
2002 Jun
Rizatriptan combined with rofecoxib vs. rizatriptan for the acute treatment of migraine: an open label pilot study.
2002 May
[Good ruler for assessing effectiveness. Pain free with only one tablet].
2002 May 6
[New meta-analysis of triptanes. Concrete help, so the choice doesn't become overwhelming].
2002 May 6
Further evaluation of rizatriptan in menstrual migraine: retrospective analysis of long-term data.
2002 Oct
Determinants of migraine-specific quality of life.
2002 Oct
Sum of Pain Intensity Differences (SPID) in migraine trials. A comment based on four rizatriptan trials.
2002 Oct
Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials.
2002 Oct
[New onset headache. Which patients should be sent for CT imaging?].
2002 Oct 24
Comparison of rizatriptan and other triptans on stringent measures of efficacy.
2002 Sep 10
Comparison of rizatriptan and other triptans on stringent measures of efficacy.
2002 Sep 10
Newer formulations of the triptans: advances in migraine management.
2003
Pharmacological approaches to migraine.
2003
Migraine headache recurrence: relationship to clinical, pharmacological, and pharmacokinetic properties of triptans.
2003 Apr
[New therapeutic recommendations for severe migraine. High beginning dosage rather than slow dosage increase].
2003 Jan 30
Migraine treatment patterns and patient satisfaction with prior therapy: a substudy of a multicenter trial of rizatriptan effectiveness.
2003 Jul
Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein.
2003 Jul
Almotriptan versus rizatriptan in patients with migraine in Spain.
2003 Jul-Aug
Real-world experiences in migraine therapy with rizatriptan.
2003 Mar
Cost-effectiveness of almotriptan and rizatriptan in the treatment of acute migraine.
2003 Nov
Patient-reported benefits of rizatriptan compared with usual non-triptan therapy for migraine in a primary care setting.
2003 Nov
Triptans for treatment of acute pediatric migraine: a systematic literature review.
2003 Nov
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 Nov
[It impairs quality of life and work time. Migraine therapy should not be left to the patients!].
2003 Nov 27
Endothelium-dependent relaxant responses to selective 5-HT(1B/1D) receptor agonists in the isolated middle cerebral artery of the rat.
2003 Nov-Dec
Rizatriptan RPD for severe migraine in the emergency department--a multicenter study.
2003 Oct
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
Naratriptan for the treatment of acute migraine: meta-analysis of randomised controlled trials.
2004 Feb
Evaluating triptan usage.
2004 Feb
Productivity cost benefit to employers of treating migraine with rizatriptan: a specific worksite analysis and model.
2004 Jan
Defeating migraine pain with triptans: a race against the development of cutaneous allodynia.
2004 Jan
CNS effects of sumatriptan and rizatriptan.
2004 Jan
Neuronal expression and regulation of CGRP promoter activity following viral gene transfer into cultured trigeminal ganglia neurons.
2004 Jan 30
Fast onset medications through thermally generated aerosols.
2004 May
Patents

Sample Use Guides

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 Sat Jun 26 02:22:58 UTC 2021
Edited
by admin
on Sat Jun 26 02:22:58 UTC 2021
Record UNII
51086HBW8G
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RIZATRIPTAN
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
RIZATRIPTAN [MI]
Common Name English
MK-462 FREE BASE
Code English
RIZATRIPTAN [INN]
Common Name English
L-705126
Code English
RIZATRIPTAN [VANDF]
Common Name English
RIZATRIPTAN [WHO-DD]
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
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
NCI_THESAURUS C47794
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
NDF-RT N0000175764
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
WHO-ATC N02CC04
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
NDF-RT N0000175763
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
WHO-VATC QN02CC04
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
LIVERTOX 857
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C61930
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
MERCK INDEX
M9640
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY Merck Index
FDA UNII
51086HBW8G
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
DRUG CENTRAL
2393
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
EVMPD
SUB10346MIG
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
LACTMED
Rizatriptan
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
MESH
C093622
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
WIKIPEDIA
Rizatriptan
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
ChEMBL
CHEMBL905
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
PUBCHEM
5078
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
DRUG BANK
DB00953
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
EPA CompTox
144034-80-0
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
RXCUI
88014
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY RxNorm
IUPHAR
51
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
CAS
144034-80-0
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
INN
7474
Created by admin on Sat Jun 26 02:22:59 UTC 2021 , Edited by admin on Sat Jun 26 02:22:59 UTC 2021
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
Approximately 26 and 14% of i.v. and oral rizatriptan doses, respectively, were excreted in urine as intact parent drug
URINE
SALT/SOLVATE -> PARENT
TARGET -> AGONIST
SALT/SOLVATE -> PARENT
TARGET -> AGONIST
Related Record Type Details
METABOLITE -> PARENT
URINE
METABOLITE -> PARENT
The mono N-desmethyl metabolite has intrinsic potency that is about 3-fold lower. Its contribution to in vivo efficacy is probably very low or negligible, since circulating concentrations are about one-tenth those of the parent drug
METABOLITE -> PARENT
after i.v. (3-mg)
URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION