Details
Stereochemistry | RACEMIC |
Molecular Formula | C9H8N2O2 |
Molecular Weight | 176.172 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC(=O)C(O1)C2=CC=CC=C2
InChI
InChIKey=NRNCYVBFPDDJNE-UHFFFAOYSA-N
InChI=1S/C9H8N2O2/c10-9-11-8(12)7(13-9)6-4-2-1-3-5-6/h1-5,7H,(H2,10,11,12)
Molecular Formula | C9H8N2O2 |
Molecular Weight | 176.172 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
Pemoline is a central nervous system stimulant. Pemoline is structurally dissimilar to the amphetamines and methylphenidate. Pemoline is generally considered dopaminergic, but its precise method of action hasn't yet been definitively determined. The interaction of pemoline with other drugs has not been studied in humans. The following are adverse reactions in decreasing order of severity within each category associated with pemoline: hepatic dysfunction, aplastic anemia, convulsive seizures, hallucinations, insomnia, anorexia and weight loss.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: map04728 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | CYLERT Approved UseCYLERT (pemoline) is indicated in Attention Deficit Hyperactivity Disorder (ADHD). Because of its association with life threatening hepatic failure, CYLERT should not ordinarily be considered as first line therapy for ADHD. Launch Date1.60012796E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.76 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/4017397/ |
2 mg/kg single, oral dose: 2 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
PEMOLINE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
46.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/4017397/ |
2 mg/kg single, oral dose: 2 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
PEMOLINE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7.28 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/4017397/ |
2 mg/kg single, oral dose: 2 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
PEMOLINE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
150 mg 1 times / day steady, oral Highest studied dose Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: |
unhealthy n = 11 Health Status: unhealthy Condition: human immunodeficiency virus disease Sex: M+F Population Size: 11 Sources: |
|
37.5 mg 1 times / day steady, oral (starting) Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: steady Dose: 37.5 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorder Sources: |
Other AEs: Hepatic failure... Other AEs: Hepatic failure (grade 5) Sources: |
96 mg 1 times / day steady, oral (mean) Dose: 96 mg, 1 times / day Route: oral Route: steady Dose: 96 mg, 1 times / day Sources: |
unhealthy n = 45 Health Status: unhealthy Condition: human immunodeficiency virus disease Sex: M+F Population Size: 45 Sources: |
Disc. AE: Neuropathic pain... AEs leading to discontinuation/dose reduction: Neuropathic pain (1 patient) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hepatic failure | grade 5 | 37.5 mg 1 times / day steady, oral (starting) Recommended Dose: 37.5 mg, 1 times / day Route: oral Route: steady Dose: 37.5 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorder Sources: |
Neuropathic pain | 1 patient Disc. AE |
96 mg 1 times / day steady, oral (mean) Dose: 96 mg, 1 times / day Route: oral Route: steady Dose: 96 mg, 1 times / day Sources: |
unhealthy n = 45 Health Status: unhealthy Condition: human immunodeficiency virus disease Sex: M+F Population Size: 45 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Gilles de la Tourette's disorder associated with pemoline. | 1980 Dec |
|
Pemoline abuse. | 1985 Aug 16 |
|
Evidence of lack of abuse or dependence following pemoline treatment: results of a retrospective survey. | 1986 Jun |
|
Case study: adverse response to clonidine. | 1997 Apr |
|
Pemoline therapy resulting in liver transplantation. | 1998 Apr |
|
Exacerbation of autoimmune hepatitis: another hepatotoxic effect of pemoline therapy. | 1998 Jan |
|
Four cases of severe hepatotoxicity associated with pemoline: possible autoimmune pathogenesis. | 1998 May |
|
Severe hypotension in a patient receiving pemoline during general anesthesia. | 2000 Nov |
|
Blood pressure changes associated with medication treatment of adults with attention-deficit/hyperactivity disorder. | 2005 Feb |
|
A surveillance method for the early identification of idiosyncratic adverse drug reactions. | 2008 |
|
Individual differences in vulnerability for self-injurious behavior: studies using an animal model. | 2011 Feb 2 |
Substance Class |
Chemical
Created
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admin
on
Edited
Sat Dec 16 16:44:43 UTC 2023
by
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Sat Dec 16 16:44:43 UTC 2023
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Record UNII |
7GAQ2332NK
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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LIVERTOX |
750
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WHO-VATC |
QN06BA05
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DEA NO. |
1530
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WHO-ATC |
N06BA05
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NCI_THESAURUS |
C47795
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Code System | Code | Type | Description | ||
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SUB09657MIG
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DTXSID3023427
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m8458
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C47655
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D010389
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2933-45-1
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2152-34-3
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DB01230
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7966
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3148
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1054
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101053-01-4
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PEMOLINE
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100000082496
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CHEMBL1177
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2075
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4723
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7953
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169499
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25159
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218-438-8
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7GAQ2332NK
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