메티프릴온 및 그 염류

DEA NFLIS-Drug Category -> Depressants and Tranquilizers

DEA Schedule III Controlled Substance -> Depressants

Pharmaceuticals -> Synthetic Cannabinoids or Psychoactive Compounds

1.2

0.78

CRYSTALS

NEARLY WHITE POWDER

SOL IN BENZENE, CHLOROFORM

VERY SOL IN ETHER

Partially sol in water (7%); freely sol in organic solvents such as alcohol

1.13e+01 g/L

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

Danger

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]

P261, P264, P264+P265, P270, P271, P272, P280, P301+P317, P302+P352, P304+P340, P305+P354+P338, P317, P319, P321, P330, P332+P317, P333+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 39 reports by companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

DEA schedule III controlled substance

2,4-Piperidinedione, 3,3-diethyl-5-methyl-: Does not have an individual approval but may be used under an appropriate group standard

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).

Schedules of controlled substances are established by section 202 of the Controlled Substances Act (21 U.S.C. 812). Schedule III includes methyprylon, DEA Code #2575; Drug class: Depressant.

Drugs; statement of required warning. The label of any drug listed as a "controlled substance" in schedule II, III, or IV of the Federal Controlled Substances Act shall, when dispensed to or for a patient, contain the following warning: "Caution: Federal law prohibits the transfer of this drug to any person other than the patient for whom it was prescribed." This statement is not required to appear on the label of a controlled substance for use in clinical investigations which are "blind".

Controlled substance in the USA - Schedule III.

Methyprylon binds at a distinct binding site associated with a Cl^- ionopore at the GABA_A receptor, increasing the duration of time for which the Cl^- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.

NEUTROPENIA & THROMBOCYTOPENIA OF UNPROVEN ORIGIN HAVE OCCURRED IN PERSONS TAKING METHYPRYLON.

UNTOWARD EFFECTS OF METHYPRYLON ARE NOT FREQUENT, BUT INCL "HANGOVER," NAUSEA, VOMITING, EPIGASTRIC DISTRESS, DIARRHEA, ESOPHAGITIS, HEADACHE, & RASH. IDIOSYNCRATIC EXCITEMENT OCCASIONALLY OCCURS.

HYPOTENSION, SHOCK, & PULMONARY EDEMA ARE MORE CONSPICUOUS FEATURES THAN IS RESPDEPRESSION. COMA MAY LAST UP TO 5 DAYS ... DEATH HAS OCCURRED WITH 6 G. HABITUATION, TOLERANCE, PHYSICAL DEPENDENCE, & ADDICTION CAN OCCUR.

May be habit forming.

For more Human Toxicity Excerpts (Complete) data for METHYPRYLON (6 total), please visit the HSDB record page.

Hemodialysis should be considered in cases of large ingestions that fail to respond to supportive care. Peritoneal dialysis in one patient recovered 80% of the unmetabolized drug. Hemoperfusion also increases clearance and reduces elimination half-life, but experience is too limited to draw conclusions. Forced diuresis is contraindicated because of the propensity of methyprylon to cause pulmonary edema.

Alert adult patients who ingest more than 800 mg of methylprylon and present within 4 hours of ingestion should be given ipecac. Patients asymptomatic after 4 hours require no decontamination. Obtunded patients who require lavage may benefit from the procedure up to 8 hours after ingestion because of decreased gastrointestinal mobility.

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).

Schedules of controlled substances are established by section 202 of the Controlled Substances Act (21 U.S.C. 812). Schedule III includes methyprylon, DEA Code #2575; Drug class: Depressant.

Drugs; statement of required warning. The label of any drug listed as a "controlled substance" in schedule II, III, or IV of the Federal Controlled Substances Act shall, when dispensed to or for a patient, contain the following warning: "Caution: Federal law prohibits the transfer of this drug to any person other than the patient for whom it was prescribed." This statement is not required to appear on the label of a controlled substance for use in clinical investigations which are "blind".

Controlled substance in the USA - Schedule III.

N - Nervous system

QN - Nervous system

Methyprylon, a piperidinedione CNS depressant, is close to barbituric acid in structure, but different enough to be called a "non-barbiturate" sedative-hynotic. Methyprylon is used for insomnia and daytime tension. Methyprylon depresses the activity of muscle tissues, the heart, and the respiratory system.

Methyprylon binds at a distinct binding site associated with a Cl^- ionopore at the GABA_A receptor, increasing the duration of time for which the Cl^- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.

INCREASED STEROID HYDROXYLATION IS PROBABLY ONE IMPORTANT MECHANISM OF ACTION OF SO-CALLED CATATOXIC STEROIDS. SUCH CMPD HAVE BEEN REPORTED TO PROTECT ANIMALS AGAINST ACUTE TOXIC EFFECTS OF EXTRAORDINARY VARIETY OF DRUGS ... METHYPRYLON.

METHYPRYLON STIMULATES HEPATIC MICROSOMAL ENZYME SYSTEM & DELTA-ALA SYNTHETASE ...

6-16 hours

PLASMA T1/2 IS 4 HR, BUT IT IS LONGER IN ACUTE INTOXICATION.

Plasma half-life is 6 to 16 hours. Onset of action within 45 minutes. Duration of action 5 to 8 hours.

Biologic half-life is not well defined, but varies between 4 and 16 hours, although a longer action has been observed in severely poisoned patients.

Hepatic. Methyprylon is almost completely metabolized.

FROM URINE OF HUMAN SUBJECTS ... TAKEN METHYPRYLON ... NEW METABOLITE HAS BEEN ... IDENTIFIED AS 2,4,6-TRIOXO-3,3-DIETHYL-5-METHYLPIPERIDINE. 2,4-DIOXO-3,3-DIETHYL-5-METHYLTETRAHYDROPYRIDINE, 2,4-DIOXO-3,3-DIETHYL-5-HYDROXYMETHYLTETRAHYDROPYRIDINE, & 4,6-DIOXO-5,5-DIETHYL-TETRAHYDRONICOTINIC ACID ... ESTABLISHED AS METABOLITES ...

While the metabolic degradation of methyprylon is known, it is not certain in which organ this takes place. Methyprylon is dehydrogenated to 5-methyl-pyrithyldione, then partially oxidized to hydroxy derivatives, and finally oxidized to 5-carboxy-pyrithyldione. The hydroxy derivatives are bound approximately 38% to human plasma proteins. Other less important metabolites may arise, but the metabolites are partly conjugated to glucuronide, with approximately 97% of the parent drug being metabolized. Intact methyprylon (3%) and its metabolites (60%) are recovered in the urine, while approximately 20% is found in the feces, demonstrating that enterohepatic circulation of the drug occurs.

Hepatic. Methyprylon is almost completely metabolized. Half Life: 6-16 hours

DRUG IS WELL ABSORBED FROM INTESTINE.

IT IS MORE WATER SOL THAN GLUTETHIMIDE, BUT IT IS NOT KNOWN WHETHER GI ABSORPTION IS CONSEQUENTLY LESS ERRATIC. ... ONLY 3% IS EXCRETED IN URINE UNCHANGED. ... ONLY 60% OF FREE METABOLITES & GLUCURONIDES IS RECOVERABLE FROM URINE.

THERAPEUTIC BLOOD CONCN PROBABLY DO NOT EXCEED 1.0 MG/100 ML. FOLLOWING SINGLE ORAL DOSE OF 650 MG IN ADULTS, MAX PLASMA CONCN OF APPROX 1.0 MG/100 ML IS REACHED AFTER 2 HR. IN FATAL CASES, BLOOD CONCN IN EXCESS OF 9.0 MG/100 ML HAVE BEEN REPORTED.

Methyprylon does not accumulate selectively in organ systems.

For more Absorption, Distribution and Excretion (Complete) data for METHYPRYLON (6 total), please visit the HSDB record page.

MEDICATION

For the treatment of insomnia.

3,3-DIETHYL-2,4(1H,3H)-PYRIDINEDIONE IS HYDROXYLATED @ 5-POSITION BY TREATMENT WITH FORMALDEHYDE IN PRESENCE OF ALKALINE CATALYST. RESULTING METHYLOL DERIV IS THEN SUBJECTED TO CATALYTIC HYDROGENATION WHEREUPON RING IS SATURATED & HYDROXYMETHYL GROUP IS DEOXYGENATED.