What Is Pentobarbital Sodium Injection?
Pentobarbital sodium injection (Nembutal) is a sterile solution for intravenous or intramuscular injection. Each mL contains pentobarbital sodium 50 mg, in a vehicle of propylene glycol, 40%, alcohol, 10%, and water for injection, to volume. Nembutal can be used for procedural sedation or for use as a pre-anesthetic medication.
Pentobarbital, also known as pentobarbitone, is a short-acting barbiturate often used to carry out painless killings (euthanasia) since high doses of Pentobarbital causes death by respiratory arrest. In the United States, the drug has been used for executions of convicted criminals
Nembutal Sodium is a short-acting barbiturate, chemically designated as sodium 5-ethyl-5-(1-methylbutyl) barbiturate. The sodium salts of Nembutal, amobarbital, phenobarbital, and secobarbital are available as sterile parenteral solutions.
The pH is adjusted to approximately 9.5 with hydrochloric acid and/or sodium hydroxide.
Nembutal sodium salt occurs as a white, slightly bitter powder that is freely soluble in water and alcohol but practically insoluble in benzene and ether.
Pentobarbital sodium was usually prescribed for insomnia, it has been largely replaced by the benzodiazepines like Xanax Alprazolam and a lot more.
How Does Pentobarbital Work?
Pentobarbital sodium binds at a distinct binding site associated with a Cl- ionophore at the GABAA receptor, increasing the duration of time for which the Cl- ionophore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (GCA). The net result of Pentobarbital action is acute potentiation of inhibitory GABAergic tone.
Pentobarbital also acts through potent and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in profound suppression of glutamatergic neurotransmission.
Pentobarbital sodium is metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine, and less commonly, in the feces.
Approximately 25% to 50% percent of a dose of aprobarbital or phenobarbital is eliminated unchanged in the urine, whereas the number of other barbiturates excreted unchanged in the urine is negligible.
Symptoms of a Pentobarbital sodium overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.
What are Barbiturates?
Barbiturates are substituted pyrimidine derivatives in which the basic structure common to these drugs is barbituric acid, a substance that has no central nervous system activity. CNS activity is obtained by substituting alkyl, alkenyl, or aryl groups on the pyrimidine ring.
Barbiturates are nonselective central nervous system depressants which are primarily used as sedative-hypnotics and also anticonvulsants in sub hypnotic doses. Barbiturates and their sodium salts are subject to control under the Federal Controlled Substances Act.
The origin of barbiturates can be traced back to Germany in 1864. Ludwig von Baeyer, the founding father of the Bayer company, synthesized urea with malonic acid to create barbituric acid.
It was later transformed by Josef von Mering and Emil Fisher into the barbiturate compound we know today. The term ‘barbituric’ is said to have arisen from either Saint Barbara, being celebrated in the region at the time of the discovery, or to show his affection for a girl named Barbara.
Eventually, it found its way into veterinary medicine as an anesthetic drug that when overdosed, led to a swift and peaceful death. The term barbital was patented by Fisher in 1903.
Important Facts About Pentobarbital Sodium Injection.
Pentobarbital sodium was widely abused and known on the streets as “yellow jackets” due to their yellow capsule. The death of Marilyn Monroe in 1962 was ruled as probable suicide due to an overdose of Nembutal. Kenneth Halliwell’s death is also attributed to an overdose of Nembutal.
Phenobarbital sodium was used for over 25 years as prophylaxis in the treatment of febrile seizures. Although an effective treatment in preventing recurrent febrile seizures, it had no positive effect on patient outcome or risk of developing epilepsy.
NB: Pentobarbital in pill form is no longer available. Abbott Pharmaceuticals’ brand of pentobarbital, Nembutal, which was available in 50 and 100 mg yellow capsules, was discontinued in 1999.
A well-known manufacturer of Pentobarbital sodium called Lundbeck does not permit its sale to prisons or corrections departments to carry out the death penalty.
What Is Pentobarbital Sodium Used For?
Pentobarbital sodium nowadays is mostly used for Euthanasia and Executions. Pentobarbital sodium can cause death when used in high doses. It is used for euthanasia for humans as well as animals. It is also used by itself, or in combination with complementary agents such as phenytoin, in commercial animal euthanasia injectable solutions.
Pentobarbital has been used or considered as a substitute for other drugs traditionally used for capital punishment in the United States when they are in short supply. Such use, however, is illegal under Danish law, and when this was discovered, after public outcry in Danish media, Lundbeck, the owner of the drug, stopped selling it to US states that impose the death penalty.
How Is Pentobarbital Sodium Injection Supplied?
Nembutal Sodium Solution is available in the following sizes:
20-mL multiple-dose vial, 1 g per vial (NDC 67386-501-52); and 50-mL multiple-dose vial, 2.5 g per vial (NDC 67386-501-55).
Each mL contains:
Pentobarbital Sodium, a derivative of barbituric acid…………………50 mg
Propylene glycol………………………………………………………………..40% v/v
Water for Injection………………………………………………………………qs (pH adjusted to approximately 9.5 with hydrochloric acid and/or sodium hydroxide.)
Some Synonyms of Nembutal Sodium Include:
- 5-ethyl-5-(1-methylbutyl)barbituric acid
- 5-ethyl-5-(sec-pentyl)barbituric acid
How Nembutal Is Easily Ordered Online
Mexico used to dominate the market but now most Nembutal sodium is mostly bought over the internet from China. There are reports of internet scams and Lateline has spoken to several people who have lost hundreds of dollars trying to buy Nembutal online.
Chinese Nembutal comes in the form of a white powder, and Dr. Nitschke says people are uncertain about its quality. He said, “People obtain this white powder in envelopes from China and they’re concerned in a way that I never saw, the same concern with the South American product.
To combat concerns, He’s set up a mobile testing laboratory, and he says there is a long queue of people across Australia waiting to use it. He said Nembutal was easy to buy online and he was not fearful of any legal consequences.
Intramuscular Pentobarbital Dosage
* Drinkable Nembutal Pentobarbital mixed with sweeteners to avoid the bitterness of the liquid 330ml.
* Nembutal pentobarbital sodium ( Sterile solution) 6.5grams/100ml.
* Nembutal pentobarbital sodium ( oral solution) 10grams/100ml.
* Nembutal Pentobarbital sodium capsules ( 50mg & 100mg ).
* Nembutal Pentobarbital ( Sodium Salt ).
150 to 200mg IM. Use a reduced dosage in debilitated or geriatric patients.
Infants, Children, and Adolescents are required to take not more than 2 to 6 mg/kg/dose IM (Max: 100 mg/dose). If adequate sedation is not achieved 1 hour after administration, an additional 1 to 3 mg/kg/dose may be given.
Intravenous Nembutal Dosage For Adults.
100 mg IV is a common, initial dose for a 70-kg adult. Allow at least 1 minute to assess the full effect of dose. Additional doses may be given up to a total of 200 to 500 mg. Use a reduced dosage in debilitated or geriatric patients.
Oral capsules are no longer commercially available in the US. Although details regarding stability are not available, the parenteral solution has been mixed in a 3:1 ratio with cherry syrup and given orally.
In these pediatric studies, oral pentobarbital was better tolerated and as effective as the comparator (IV pentobarbital or chloral hydrate).