Methyprylon
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3 sources
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Also known as noludarTS
Sedative of the pipeidinedone family. Was used for treating insomnia, yet is rarely used today due to substances with fewer side effects, such as benzodiazepines.TS
Oral
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| — | 150–200 mg | 200–300 mg | — | —+ |
| Total | 6–12 hours |
|---|---|
| After-effects | 1–16 hours |
🧬 Receptor activityDC
Mechanism of actionPH
Methyprylon binds at a distinct binding site associated with a Cl<sup>-</sup> ionopore at the GABA<sub>A</sub> receptor, increasing the duration of time for which the Cl<sup>-</sup> 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 ...
PharmacodynamicsPH
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.
Pharmacokinetics
Half-lifePH
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.
AbsorptionPH
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.
MetabolismPH
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
Protein bindingPH
60%
Plan a dose of Methyprylon
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Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.