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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 of RIZATRIPTAN

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
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

1998
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

1998
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
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
1999 Mar 5
Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy.
2000 Dec
New abortive agents for the treatment of migraine.
2001
The anti-migraine 5-HT(1B/1D) agonist rizatriptan inhibits neurogenic dural vasodilation in anaesthetized guinea-pigs.
2001 Aug
A systematic review of the use of triptans in acute migraine.
2001 Feb
Influence of beta-adrenoceptor antagonists on the pharmacokinetics of rizatriptan, a 5-HT1B/1D agonist: differential effects of propranolol, nadolol and metoprolol.
2001 Jul
Establishing a standard of speed for assessing the efficacy of the serotonin(1B/1D) agonists (triptans).
2001 Jul
Acute treatment of migraine and the role of triptans.
2001 Mar
Meta-analysis of rizatriptan efficacy in randomized controlled clinical trials.
2001 Mar
Cluster headache without autonomic symptoms?
2001 Nov
Clinical features of withdrawal headache following overuse of triptans and other headache drugs.
2001 Nov 13
Triptans in the treatment of basilar migraine and migraine with prolonged aura.
2001 Nov-Dec
Triptans are all different.
2001 Sep
Restoring migraine sufferers' ability to function normally: a comparison of rizatriptan and other triptans in randomized trials.
2002
Spotlight on rizatriptan in migraine.
2002
Migraine: diagnosis, management, and new treatment options.
2002 Feb
Molecular cloning and expression of the porcine trigeminal ganglion cDNA encoding a 5-ht(1F) receptor.
2002 Feb 1
Treatment of migraine with rizatriptan: when to take the medication.
2002 Jan
Pharmacological treatments for acute migraine: quantitative systematic review.
2002 Jun
CNS effects of sumatriptan and rizatriptan in healthy female volunteers.
2002 May
[Controlling migraine with highly effective triptanes. Lowers rate of drug use].
2002 May 6
Crossover comparison of efficacy and preference for rizatriptan 10 mg versus ergotamine/caffeine in migraine.
2003
[New therapeutic recommendations for severe migraine. High beginning dosage rather than slow dosage increase].
2003 Jan 30
Meta-analysis of oral triptan therapy for migraine: number needed to treat and relative cost to achieve relief within 2 hours.
2003 Jan-Feb
Migraine treatment patterns and patient satisfaction with prior therapy: a substudy of a multicenter trial of rizatriptan effectiveness.
2003 Jul
[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
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 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
  • 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 [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
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
NCI_THESAURUS C47794
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
NDF-RT N0000175764
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
WHO-ATC N02CC04
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
NDF-RT N0000175763
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
WHO-VATC QN02CC04
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
LIVERTOX 857
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
Code System Code Type Description
SMS_ID
100000080246
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
NCI_THESAURUS
C61930
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
MERCK INDEX
m9640
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY Merck Index
FDA UNII
51086HBW8G
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
DRUG CENTRAL
2393
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
DAILYMED
51086HBW8G
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
EVMPD
SUB10346MIG
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
LACTMED
Rizatriptan
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
MESH
C093622
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
WIKIPEDIA
Rizatriptan
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
ChEMBL
CHEMBL905
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
PUBCHEM
5078
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
DRUG BANK
DB00953
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
EPA CompTox
DTXSID2023565
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
CHEBI
48273
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
RXCUI
88014
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY RxNorm
IUPHAR
51
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
CAS
144034-80-0
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
PRIMARY
INN
7474
Created by admin on Fri Dec 15 15:53:26 GMT 2023 , Edited by admin on Fri Dec 15 15:53:26 GMT 2023
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
SOLVATE->ANHYDROUS
Related Record Type Details
METABOLITE -> PARENT
URINE
METABOLITE -> PARENT
after oral (10-mg)
URINE
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
IMPURITY -> PARENT
IMPURITY -> PARENT
IMPURITY -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION