115-67-3CCC1(C)OC(=O)N(C)C1=OVQASKUSHBVDKGU-UHFFFAOYSA-NParamethadione can cause developmental toxicity according to state or federal government labeling requirements.
115-67-3DTXSID8023420CLEAR, COLORLESS LIQUID
Liquid
SLIGHTLY SOL IN WATER; FREELY SOL IN ALCOHOL, BENZENE, CHLOROFORM, ETHER
1.35e+02 g/L
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
101 to 102 °C at 11.3 mm Hg
101.5 °C
安全情報は参考情報です。供給元の安全データシート(SDS)、適用法令、専門家による評価に代わるものではありません。
Danger
H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]
P203, P261, P264, P264+P265, P271, P280, P302+P352, P304+P340, P305+P351+P338, P318, P319, P321, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)
The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.
Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).
Graca LM, Machado MH; Acta Med Port 8 (7-8): 441-9 (1995). Teratogenic effects of exogenous agents.
Brent RL, Beckman DA; Clin Obstet Gynecol 37 (3): 646-70 (1994). The contribution of environmental teratogens to embryonic and fetal loss.
Stevenson RE; Human Malformations and Related Anomalies (Oxford Monographs on Medical Genetics 27: 137-68 (1993). The environmental basis of human anomalies.
Schardein JL; Chemically Induced Birth Defects 2: 157-207 (1993). /A review of the/ anticonvulsants.
For more Special Reports (Complete) data for PARAMETHADIONE (7 total), please visit the HSDB record page.
N - Nervous system
QN - Nervous system
Paramethadione is an oxazolidinedione anticonvulsant similar to trimethadione that acts on the central nervous system (CNS) to reduce the number of absence seizures (often seen in epileptics). Absence seizures involve an interruption to consciousness where the person experiencing the seizure seems to become vacant and unresponsive for a short period of time (usually up to 30 seconds). Paramethadione acts on thalamic neurons in the thalamic reticular nucleus (which studies have shown to be associated with absence seizures, von Krosigk et al., 1993).
Dione anticonvulsants such as paramethadione reduce T-type calcium currents in thalamic neurons (including thalamic relay neurons). This inhibits corticothalamic transmission and raises the threshold for repetitive activity in the thalamus. This results in a dampening of the abnormal thalamocortical rhythmicity proposed to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram (EEG) during absence seizures.
Dione anticonvulsants reduce T-type calcium currents in thalamic neurons, including thalamic relay neurons. this raises the threshold for repetitive activity in the thalamus, and inhibits corticothalamic transmission. Thus, the abnormal thalamocortical rhythmicity, which is thought to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram (EEG) with absence seizures, is dampened. The maximal seizure pattern in patients undergoing electroconvulsive therapy is not modified. /Dione anticonvulsants/
12 to 24 hours (however the half-life for the active metabolite is not known)
Paramethadion - 12 to 24 hours; active metabolite - unknown.
Primarily hepatic (mainly via cytochrome P450 isozyme 2C9), paramethadione is completely demethylated to 5-ethyl-5-methyl-2,4-oxazolidinedione, the active metabolite.
現在のフィルター条件では反応記録がありません。
読み込み中…
CHEMBL1100CHEBI:7921Concurrent use of alcohol or CNS depression-producing medications with dione anticonvulsants may enhance CNS depression. /Dione anticonvulsants/
Concurrent use of tricyclic antidepressants; haloperidol; loxapine; maprotiline; molindone; monoamine oxidase (MAO) inhibitors, including furazolidone, procarbazine, and >10 mg/day selegiline; phenothiazines; pimozide; or thioxanthenes with dione anticonvulsants may lower the convulsive threshold, enhance CNS depression, and decrease the effects of the anticonvulsant medication. dosage adjustments may be necessary. /Dione anticonvulsants/
Concurrent use of phenacemide with dione anticonvulsants may result in additive toxicity. /Dione anticonvulsants/
Dione anticonvulsants such as paramethadione reduce T-type calcium currents in thalamic neurons (including thalamic relay neurons). This inhibits corticothalamic transmission and raises the threshold for repetitive activity in the thalamus. This results in a dampening of the abnormal thalamocortical rhythmicity proposed to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram (EEG) during absence seizures.
Symptoms of overdose include clumsiness or unsteadiness, coma, severe dizziness, severe drowsiness, severe nausea, and problems with vision. May cause a potentially dangerous rash that may develop into Stevens Johnson syndrome, an extremely rare but potentially fatal skin disease.
SEDATION MAY OCCUR WITH HIGH DOSES. UNCOMFORTABLE VISUAL ALTERATIONS, PARTICULARLY UNPLEASANT GLARE WHEN EMERGING INTO SUNLIGHT OR WELL-LIT ROOM... EDEMA & SEVERE PROTEIN-LOSING NEPHROPATHY MAY OCCUR... NEUTROPENIA OCCURS IN ABOUT 20% OF RECIPIENTS & OCCASIONALLY PANCYTOPENIA & FATAL APLASTIC ANEMIA HAVE BEEN REPORTED.
OTHER ADVERSE EFFECTS INCL HEPATITIS, SKIN REACTIONS (GENERALIZED ERYTHEMA, MACULOPAPULAR ERUPTIONS & EXFOLIATIVE DERMATITIS) &, RARELY, MILD GI DISTURBANCES.
Acute effects of overdose include ataxia (clumsiness or unsteadiness); coma - following massive overdose; severe dizziness; severe drowsiness; severe nausea; and visual disturbances.
The neuroactive drugs taken by pregnant women have two principal side effects: a teratogenic effect and a postnatal withdrawal effect. /The following characteristic syndromes are noted/: hydantoin-barbiturate syndrome, the trimethadione-paramethadione syndrome.
Treatment of overdose: To decrease absorption - immediate evacuation of stomach by induction of emesis, lavage, or both is recommended. To enhance elimination - alkalinization of urine is reported to enhance elimination of active metabolites. Monitoring - frequent monitoring of vital signs and close patient observation are required. Following recovery, a complete blood count and a careful evaluation of hepatic and renal function should be done. Supportive care - general supportive care is necessary in dione anticonvulsant overdose treatment. Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation. /Dione anticonvulsants/
Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).
PARAMETHADIONE IS COMPLETELY N-DEMETHYLATED TO 5-ETHYL-5-METHYL-OXAZOLIDINE-2,4-DIONE...
PARAMETHADIONE IS N-DEMETHYLATED BY HEPATIC MICROSOMAL ENZYMES TO ACTIVE METABOLITE THAT IS SLOWLY EXCRETED IN URINE...
PARAMETHADIONE IS N-DEMETHYLATED BY HEPATIC MICROSOMAL ENZYMES TO ACTIVE METABOLITE... METABOLITE ACCUMULATES DURING CHRONIC MEDICATION & IS PROBABLY RESPONSIBLE FOR MOST OF ANTICONVULSANT ACTIVITY OF PARENT DRUG...
Primarily hepatic (mainly via cytochrome P450 isozyme 2C9), paramethadione is completely demethylated to 5-ethyl-5-methyl-2,4-oxazolidinedione, the active metabolite. Half Life: 12 to 24 hours (however the half-life for the active metabolite is not known)
Rapid via the digestive tract.
PARAMETHADIONE IS COMPLETELY N-DEMETHYLATED TO 5-ETHYL-5-METHYL-OXAZOLIDINE-2,4-DIONE AND SLOWLY EXCRETED BY KIDNEYS.
MEDICATION (VET)
MEDICATION
Therap Cat: Anticonvulsant.
Used for the control of absence (petit mal) seizures that are refractory to treatment with other medications.
SPIELMAN, US PATENT 2,575,693 (1951 TO ABBOTT).
ETHYL ALPHA-HYDROXY-ALPHA-METHYLBUTYRATE & UREA...REFLUXED FOR 24 HR IN PRESENCE OF SODIUM METHOXIDE, RESULTING IN CONDENSATION CYCLIZATION WITH FORMATION OF SODIUM DERIV OF 5-ETHYL-5-METHYL-2,4-OXAZOLIDINEDIONE. AFTER DISTILLING OFF ALC, DIMETHYL SULFATE...ADDED TO EFFECT DESIRED N-METHYLATION.
使用Paramethadione is also used in minor forms of epilepsy.