Ethchlorvynol
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Also known as placidyl, ethchlorvnolTS
Sedative Hypnotic medication made in the 50's. It was used for short term help for insomnia (No longer than two weeks)TS
Oral
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| — | 100–200 mg | 200–500 mg | 500–750 mg | —+ |
| Onset | 15–45 minutes |
|---|---|
| Total | 6–9 hours |
| After-effects | 1–6 hours |
🧬 Receptor activityDC
Mechanism of actionPH
Although the exact mechanism of action is unknown, ethchlorvynol appears to depress the central nervous system in a manner similar to that of barbiturates. Barbiturates bind at a distinct binding sites 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.
MOST OF MODERN SEDATIVE-HYPNOTIC AGENTS ARE GENERAL DEPRESSANTS. THEY DEPRESS WIDE RANGE OF CELLULAR FUNCTIONS IN MANY VITAL ORGAN SYSTEMS. /HYPNOTICS & SEDATIVES/
The mechanism of action of the drug is not known. In doses used for hypnosis, ethchlorvynol produces cerebral depression and quiet, deep sleep. Higher doses may lead to general anesthesia and concurrent depression of respiratory and vasomotor centers; death may result from respiratory failure, hypotension, or complications of prolonged coma. The effect of ethchlorvynol or rapid eye movement (REM) or other stages of sleep has not yet been established. In experimental animals, ethchlorvynol exhibits anticonvulsant and muscle relaxant activity.
Intravenous injection of ethchlorvynol (ECV) leads to hypoxemia and a permeability pulmonary edema. Whether the hypoxemia is directly attributable to the pulmonary edema or caused by release of mediators has not been explored. Three groups of dogs were studied: (1) ethchlorvynol, (2) indomethacin--ethchlorvynol, and (3) ketanserin--ethchlorvynol. In group 1, 25 to 30 mg/kg of ethchlorvynol caused a significant fall in PaO2 at 4 min (92 +/- 12.6 to 77 +/- 21 mm Hg, p <0.05), which persisted throughout the experiment. The P(A-a)O2 gradient widened significantly at 3 min (22 +/- 11 to 31 +/- 16.8 mm Hg, p <0.05) and remained abnormal for the remainder of the experiment. There was no significant fall in PaO2 in groups 2 and 3. Lung tissue water to dry weight ratio increased significantly in all groups at 60 min. Lung tissue water to dry weight ratios were normal at 10 min after ethchlorvynol injection in additional groups. It was concluded that ethchlorvynol causes hypoxemia, which is mediated by cyclooxygenase products and 5-hydroxytryptamine. This hypoxemia can be prevented by the administration of drugs that block these products.
PharmacodynamicsPH
Ethchlorvynol is a sedative drug and schedule IV (USA) controlled substance. It produces cerebral depression, however the exact mechanism of action is not known.
Pharmacokinetics
Half-lifePH
Plasma half-life is approximately 10 to 20 hours, terminal half-life is 21-100 hours.
AFTER EQUILIBRIUM FOLLOWING HYPNOTIC DOSES, BLOOD LEVEL FALLS RAPIDLY, WITH AVG T/2 OF 5.6 HR.
... HALF-LIFE FOR ... DISTRIBUTION ... 5 TO 6 HR ... HALF-LIFE FOR ... ELIMINATION /IS/ 70 HR /HUMAN/
Plasma half-life is approximately 10 to 20 hours.
100 hr (overdose) /From table/
A 33 year old obese, hypothyroid, white male with several medical problems was admitted to University Hospital in September 1984 for treatment of drug intoxication. Admitting medications included ethchlorvynol in addition to other central nervous system depressants. Initial serum concn were reported at 70 ug/ml in this somnolent yet totally conscious adult. Established therapeutic concn are 2-8 ug/ml, with toxic exceeding 20 ug/ml. A tolerance phenomenon seemed evident. Serum ethchlorvynol concn were monitored daily during early hospitalization and continued to be substantially greater than reported toxic concn. Kinetic values were as follows: total body clearance 9.92 ml/min, volume of distribution 68.0 liters, and half-life 78 hr. These values are unique in that they were calculated from a patient who had not suffered an acute overdose, thereby differing markedly from previously published values. The influence of hypothyroidism and hyperlipidemia on these markedly different values appears to be significant. Ethchlorvynol should probably be added to the list of drugs influenced by thyroid disease.
AbsorptionPH
Rapidly absorbed from gastrointestinal tract.
... SLOW DISAPPEARANCE OF DRUG WAS SHOWN TO BE DUE LARGELY TO EXTENSIVE TISSUE DISTRIBUTION.
AFTER ORAL INGESTION OF 1 G OF ETHCHLORVYNOL, SYMPTOMS OF CNS DEPRESSION OCCUR WITHIN 15-30 MIN. VOL OF DISTRIBUTION IS GREATER THAN VOL OF TOTAL BODY WATER. IN ACUTELY INTOXICATED PATIENT ... CONCN IN CSF REACHES 50% OF THAT IN PLASMA.
DRUG IS MAINLY /METABOLIZED BY THE/ LIVER, BUT APPROX 10% OF USUAL DOSE IS EXCRETED INT URINE.
RAPIDLY ABSORBED FROM GI TRACT ... ORAL ADMIN OF 200 MG, 500 MG & 750 MG ... PRODUCED PEAK PLASMA LEVELS OF 0.9 TO 2.5 MCG/ML, 4.2 TO 6.5 MCG/ML & 8 MCG/ML, RESPECTIVELY, WITHIN 1 TO 2 HR ... /HUMAN/
For more Absorption, Distribution and Excretion (Complete) data for ETHCHLORVYNOL (17 total), please visit the HSDB record page.
MetabolismPH
About 90% of a dose is metabolized in the liver. Some ethchlorvynol may also be metabolized in the kidneys. Ethchlorvynol and metabolites undergo extensive enterohepatic recirculation.
About 90% of a dose is metabolized in the liver. Some ethchlovynol may also be metabolized in the kidneys.
Although the metabolic fate of ethchlorvynol has not been fully elucidated, there is evidence that the drug is extensively metabolized, probably in the liver. There is also some evidence that the kidneys may play an essential role in metabolism of the drug.
Metabolism in liver originally was assumed to be negligible, but this has been somewhate disproved since it was later found that ethchlorvynol is readily metabolized in liver. Although metabolites have not yet been identified, it would appear that glucuronide conjugation occurs as well as hydroxylation with reduction of unsaturated bonds in the chemical structure.
Approximately 90% of the drug will undergo biotransformation, probably in the liver, since ethchlorvynol is concentrated in bile to three times as much as in serum.
About 90% of a dose is metabolized in the liver. Some ethchlorvynol may also be metabolized in the kidneys. Ethchlorvynol and metabolites undergo extensive enterohepatic recirculation.
Half Life: Plasma half-life is approximately 10 to 20 hours, terminal half-life is 21-100 hours.
Protein bindingPH
35-50%
Plan a dose of Ethchlorvynol
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Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.