Tiopentale – Wikipedia

The tiopentale It is a drug -likeing drug of the CNS, belonging to the class of barbiturates, used for general anesthesia. It is also used in the induction of the artificial coma and in veterinary medicine.

It is the Tiobarbitural derivative of the Potobarbital: the oxygen atom is replaced with a sulfur atom.

The Tipopental was reported in the list of essential drugs of the World Health Organization, but was supplanted by the propofol, better tolerated. ^{[2] [3]} Despite this, Tipopental is still listed as an acceptable alternative to propofol, depending on local availability and the cost of drugs. ^[3]

In the United States it was used, together with the pancuronium and chloride of potassium, to practice lethal injection to death condemned; ^[4] This mixture of drugs is also used, in some countries, in human euthanasia.

The Tipopental as a sodium salt is known by the name of Pentothal , above all thanks to cinema and television, for having been used, to sub -anesthetic dosages, as a serum of truth: for example, they make great use of it in their imaginary adventures Diabolik and agent 47 and is also used by Hannibal Lecter in the film Hannibal Lecter: the origins of evil and in the series Human Target .

The Tipopental was discovered in the early 1930s by Ernest H. Volwiler and Donalee L. Tabern, who worked for the Abbott workshops.

It was used for the first time in humans on March 8, 1934, by Dr. Ralph M. Waters. Three months later, Dr. John S. Lundy began a clinical experimentation at the Mayo Clinic at the request of Abbott. ^[5]

Abbott continued to produce the drug until 2004.

The US producer Hospira stopped manufacturing the drug and the EU has forbidden the export of the drug for the death penalty.

The Tiiopental quickly and easily crosses the hematencephalic barrier because it is a lipophilic molecule.

The half -life of the elimination phase after a single intravenous dose is between three and eight hours. The distribution and metabolism of the Tiopental (as for the other barbiturates) is influenced above all by its liposolubility (distribution coefficient), by the protein bond and the degree of ionization.

Like all liposoluble anesthetic drugs, its short duration of action is due to redistribution from central circulation to muscles and adipose tissue. His distribution coefficient (about 10) leads him to settle in the adipose tissue.

Once redistributed, the free fraction in the blood is metabolized in the liver.

The Tipopental is metabolized in Potobarbital acid, ^[6] 5-Ethil-5- (1′-meteil-3′-hydroxybutil) -2 -iotabarbiturico and 5-ethil-5- (1′-meteil-3′- acid carboxypropil) -2-9thibarbituine. ^[7]

The Tipopental belongs to the class of barbiturate drugs, which are non -selective compounds that bind to a surface of ionic channels, including the Gaba channel _A , the Nachr receptor, the 5ht3r channel, the Glyr channel and others. The Gaba receptor _A It is an inhibitory channel that decreases neuronal activity; The barbiturates favor the inhibitory action of the GABA receptor _A. While some barbiturates favor the opening of the GABA receptors _A , these compounds block ionic channels. Nachr’s neuronal channels are blocked both of the Tipopental Sodium and Potobarbital. ^[8]

Repeated intravenous doses involve prolonged anesthesia, as the adipose tissue works as a reserve. The adipose tissue accumulates in concentrations from 6 to 12 times higher than plasma and releases the medicine slowly with consequent prolonged anesthesia.

Anesthesia [ change | Modifica Wikitesto ]

The Tipopental is an ultra short barbiturate action that has been used under general anesthesia. Its use has been replaced with that of the propofol. After the intravenous injection, the drug quickly reaches the brain and causes loss of consciousness within 30-45 seconds.

Tipopental is not used to maintain anesthesia in surgical procedures because, in infusion, it shows a zero -order elimination pharmacokinetics, therefore it requires a long period before re -acquired consciousness. Anesthetics are preferred in the form of gas, which are quickly eliminated, in order to allow a rapid return of consciousness. ^[9]

Tipopental is used in veterinary medicine to induce anesthesia in animals.

The Tiopental was used to induce pharmacological coma. ^[ten] Today it has been replaced by drugs such as propofol, because their effects mitigate more quickly. It can be used in patients with an increase in intracranial pressure, due to trauma or surgery. Barbiturates reduce neuronal activity, reducing brain metabolism and oxygen consumption, decrease the intracranial vascular response to carbon dioxide (CO2), which in turn decreases intracranial pressure. Patients with high intracranial pressure caused by head injury can benefit from the use of barbiturates. ^{[11] [twelfth] [13]}

Euthanasia [ change | Modifica Wikitesto ]

The Tiopental is administered intravenously in euthanasia. Both in Belgium and in the Netherlands, where active euthanasia is allowed by the law, the standard protocol recommends the Tiopental as an ideal agent for inducing the coma, followed by the bromide of pancuronio to paralyze the muscles and stop breathing. ^[14]

Intravenous administration is the fastest and most reliable way to achieve euthanasia, because death comes more quickly. The coma is induced by the intravenous administration of 20 mg/kg of Tiopental (Nesdonal) in a small volume of physiological solution. Therefore, a triple dose of a non -depolarizing neuromuscular blocker drug is administered, such as the bromide of Pancuronio (Pavulon) or the vecuronium bromide (Norcuron). The Miorilassant must be administered intravenously to ensure optimal bioavailability. ^[14]

In February 2022 a medical commission indicated, for the first time in Italy, the Tipopental as a drug appropriate to the “assisted suicide”. ^[15]

Lethal injection [ change | Modifica Wikitesto ]

The Tipopental is used, together with the bromide of Pancuronio and the chloride of potassium, to perform the lethal injection in the United States. A high dose is administered to ensure rapid loss of consciousness. The use of Tipopental in the executions was contested after the publication of a study in the scientific journal The Lancet , where it was reported that the autopsies of the executed prisoners had shown a level of tiopental in the bloodstream not sufficient to cause unconsciousness.

On December 8, 2009, Ohio became the first state to use a single dose of tedium sodium for capital executions, following the bankruptcy in the use of the three -drug cocktail during an execution. ^[16] Washington has become the second state of the United States to use single -dose sodium injections for executions. On September 10, 2010 the execution of Cal Coburn Brown was the first in the state to use a single -dose injection. His death was pronounced approximately a minute and a half after the intravenous administration of five grams of drug.

In December 2010, the United Kingdom introduced a ban on Topental’s export. ^{[17] [18]} The restrictions were based on the “Regulation on torture of the European Union (including the granting of licenses for drugs used in lethal injections)”. ^[19] Since 21 December 2011, the European Union has extended commercial restrictions to prevent the export of certain medicines, stating that “the Union does not approve the capital penalty and works for its universal abolition”. ^[20]

Serum of truth [ change | Modifica Wikitesto ]

Tipopental is used in some countries as a serum of truth, because it causes the loss of inhibition typical of barbiturates. ^[21] Drugs tend to make subjects talkative and cooperative in interrogations; However, the reliability of the confessions made under Typeter is very questionable. ^[22]

Psychiatry [ change | Modifica Wikitesto ]

The Tipopental was used to desensitize patients with phobias. ^[23] A psychiatrist who worked with Tipopental is the Dutch professor Jan Bastiaans, who used this drug to help relieve trauma in the surviving victims of the Holocaust. ^[24]

As with almost all anesthetic drugs, the Tipopental causes cardiovascular and respiratory depression with consequent hypotension, apnea and airways obstruction. For these reasons, the drug is administered under medical supervision. The side effects include headache, agitation, drowsiness and nausea. Postumes due to side effects can last up to 36 hours.

The Tipopental must be used with caution in the case of liver diseases, Addison’s disease, mixedama, serious heart disease, severe hypotension, serious respiratory or porphyra disorders. ^{[25] [26]}

The administration of pentossyphillin and tiopental causes death from acute pulmonary edema in the rats, due to the increased pulmonary vascular permeability. ^[27]

• Pentotal . are TRECCANI.IT – encyclopedia online , Institute of the Italian Encyclopedia.
• Pentotal , in Dictionary of Medicine , Institute of the Italian Encyclopedia, 2010.
• Tiopentale . are Vocabulary Treccani , Institute of the Italian Encyclopedia.
• Sodium tiopental . are sape.it , De Agostini.
• ( IN ) Sodium Pentothal . are British encyclopedia Encyclopaedia Britannica, Inc.