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Misc (Seconal) Secobarbital Bioavailability

Cface

Bluelighter
Joined
Jan 2, 2008
Messages
802
Did some searching, can't find much info on secobarbital BA with various ROAs (oral, intranasal, IM, IV, rectal).

Any info?
 

amapola

Bluelight Crew
Joined
Mar 23, 2010
Messages
4,795
Location
The Great White North
Oral and rectal would both be high with IV obviously better and IM similar with a longer duration of onset.

Try http://toxnet.nlm.nih.gov

edit:
Okay I was curious and did a search on it.
http://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@[email protected]+76-73-3
Barbiturates are weak acids that are absorbed and rapidly distributed to all tissues and fluids, with high concentrations in the brain, liver, and kidneys. Lipid solubility of the barbiturates is the dominant factor in their distribution within the body. The more lipid soluble the barbiturate, the more rapidly it penetrates all tissues of the body. Barbiturates are bound to plasma and tissue proteins to a varying degree, with the degree of binding increasing directly as a function of lipid solubility. Phenobarbital has the lowest lipid solubility, lowest plasma binding, lowest brain protein binding, the longest delay in onset of activity, and the longest duration of action. At the opposite extreme is secobarbital, which has the highest lipid solubility, highest plasma protein binding, highest brain protein binding, the shortest delay in onset of activity, and the shortest duration of action.

Approximately 30-45% of the drug is bound to plasma proteins.

Secobarbital is metabolized by the liver via penultimate oxidation of the 1-methylbutyl substituent to form 5-allyl-5(3'-hydroxy-1'-methylbutyl)barbituric acid (hydroxysecobarbital), the major metabolite. Oxidation of the allyl substituent may also occur to form 5-[2',3'-dihydroxypropyl-5-(1'-methylbutyl)]barbituric acid (secodiol). These inactive metabolites are excreted in urine unchanged or as glucuronide conjugates. Hydroxysecobarbital may also be further oxidized to a ketone or a carboxylic acid. The allyl substituent at C 5 may be removed, and small quantities of the resulting 5-(1'-methylbutyl)barbituric acid metabolite have been found in urine.

Approximately 90% of an oral dose of secobarbital is absorbed from the GI tract within 2 hours after ingestion, and peak plasma concentrations are reached within 2-4 hours. Virtually all of the drug is absorbed following rectal administration.

Barbiturates are absorbed in varying degrees following oral, rectal, or im administration. The sodium salts are more rapidly absorbed by all routes of administration than are the acids. The rate of oral absorption is increased when the sodium salt is ingested as a dilute solution or taken on an empty stomach. Alcohol also enhances the rate of absorption, possibly by increasing blood flow through the gastric mucosa. /Barbiturates General Statement/

The plasma half-life for secobarbital sodium in adults ranges between 15 to 40 hours, with a mean of 28 hours.
 
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