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ontents move to sidebar hide top 1 uses toggle uses subsection 1 1 anesthesia 1 2 medically induced coma 1 3 euthanasia 1 4 lethal injection 1 5 truth serum 1 6 psychiatry 2 mechanism of action 3 controversies 4 metabolism 5 dosage 6 contraindications 7 history 8 references 9 external links toggle the table of contents sodium thiopental 38 languages العربية تۆرکجه বাংলা català čeština cymraeg deutsch esperanto español euskara فارسی suomi français ghanaian pidgin magyar bahasa indonesia italiano 日本語 한국어 latviešu nederlands norsk bokmål ଓଡ଼ିଆ polski português română русский srpskohrvatski српскохрватски සිංහල simple english српски srpski svenska türkçe twi українська اردو tiếng việt 中文 edit links article talk english read edit view history tools tools move to sidebar hide actions read edit view history general what links here related changes upload file permanent link page information cite this page get shortened url switch to legacy parser print export download as pdf printable version in other projects wikimedia commons wikidata item appearance move to sidebar hide from wikipedia the free encyclopedia barbiturate general anesthetic not to be confused with pentobarbital or phenobarbital sodium pentathol and c11 h17 n2 o2 s na redirect here for the song by anthrax see sound of white noise pharmaceutical compound sodium thiopental skeletal structure of sodium thiopental 3d representation of a sodium thiopental molecule clinical data trade names pentothal others other names truth serum thiopentone thiopental ahfs drugs com monograph pregnancy category au d routes of administration intravenous by mouth rectal drug class barbiturate atc code n01af03 who n05ca19 who legal status legal status au s4 prescription only br class b1 psychoactive drugs 1 ca schedule iv uk class b us schedule iii 2 pharmacokinetic data protein binding 80 metabolism liver metabolites pentobarbital others onset of action 30 45 seconds elimination half life 5 5 3 26 hours 4 duration of action 5 10 minutes identifiers iupac name sodium 5 ethyl 5 pentan 2 yl 2 sulfanylidene 1 3 diazinane 4 6 dione cas number 71 73 8 76 75 5 pubchem cid 3000714 drugbank db00599 chemspider 2272257 unii 49y44qzl70 kegg d00714 chebi chebi 9561 chembl chembl738 comptox dashboard epa dtxsid1021744 echa infocard 100 000 694 chemical and physical data formula c 11 h 17 n 2 na o 2 s molar mass 264 32 g mol 1 3d model jsmol interactive image chirality racemic mixture smiles na o c1nc s n c o c1 c c ccc cc inchi inchi 1s c11h18n2o2s na c1 4 6 7 3 11 5 2 8 14 12 10 16 13 9 11 15 h7h 4 6h2 1 3h3 h2 12 13 14 15 16 q 1 p 1 key awlilqarpmwuha uhfffaoysa m pentothal vintage package sodium thiopental also known as thiopental sodium or thiopentone and sold under the brand name pentothal is a rapid onset short acting barbiturate general anesthetic it is the thiobarbiturate analog of pentobarbital and an analog of thiobarbital sodium thiopental is a therapeutic alternative on the world health organization s list of essential medicines 5 it was the first of three drugs administered during most lethal injections in the united states until the us division of hospira objected and stopped manufacturing the drug for this purpose in 2011 and the european union additionally banned the export of the drug for this purpose 6 although thiopental abuse carries a dependency risk its recreational use is rare 7 sodium thiopental is well known in popular culture especially under the name sodium pentothal as a truth serum although its efficacy in this role is questioned 8 9 uses edit anesthesia edit sodium thiopental is an ultra short acting barbiturate and has been used commonly in the induction phase of general anesthesia its use has been largely replaced with that of propofol but may retain some popularity as an induction agent for rapid sequence induction and intubation such as in obstetrics 10 following intravenous injection the drug rapidly reaches the brain and causes unconsciousness within 30 45 seconds at one minute the drug attains a peak concentration of about 60 of the total dose in the brain thereafter the drug distributes to the rest of the body and in about 5 10 minutes the concentration in the brain is low enough that consciousness returns a normal dose of sodium thiopental usually 4 6 mg kg given to a pregnant person for operative delivery caesarean section rapidly makes them unconscious but the baby in their uterus remains conscious however larger or repeated doses can depress the baby s consciousness 11 sodium thiopental is not used to maintain anesthesia in surgical procedures because in infusion it displays zero order elimination pharmacokinetics leading to a long period before consciousness is regained instead anesthesia is usually maintained with an inhaled anesthetic gas agent inhaled anesthetics are eliminated relatively quickly so stopping the inhaled anesthetic allows rapid return of consciousness sodium thiopental would have to be given in large amounts to maintain unconsciousness during anaesthesia due to its rapid redistribution throughout the body as it has a high volume of distribution since its half life of 5 5 to 26 hours is quite long consciousness would take a long time to return 4 in veterinary medicine sodium thiopental is used to induce anesthesia in animals since it is redistributed to fat certain lean breeds of dogs such as sighthounds have prolonged recoveries from sodium thiopental due to their lack of body fat conversely obese animals recover rapidly but it takes much longer for the drug to be entirely removed metabolized from their bodies sodium thiopental is always administered intravenously as it can be fairly irritating to tissue and is a vesicant severe tissue necrosis and sloughing can occur if it is injected incorrectly into the tissue around a vein 12 medically induced coma edit in addition to anesthesia induction sodium thiopental was historically used to induce medical comas 13 it has now been superseded by drugs such as propofol because their effects wear off more quickly than thiopental patients with brain swelling causing elevation of intracranial pressure either secondary to trauma or following surgery may benefit from this drug sodium thiopental and the barbiturate class of drugs decrease neuronal activity thereby decreasing cerebral metabolic rate of oxygen consumption cmro 2 thus decreasing the cerebrovascular response to carbon dioxide which in turn decreases intracranial pressure patients with refractory elevated intracranial pressure rich due to traumatic brain injury tbi may have improved long term outcome when barbiturate coma is added to their neurointensive care treatment 14 reportedly thiopental has been shown to be superior to pentobarbital in reducing intracranial pressure 15 this phenomenon is also called an inverse steal or robin hood effect as cerebral perfusion to all parts of the brain is reduced due to the decreased cerebrovascular response to carbon dioxide allowing optimal perfusion to ischaemic areas of the brain which have higher metabolic demands since vessels supplying ischaemic areas of the brain would already be maximally dilated because of the metabolic demand 16 euthanasia edit sodium thiopental is used intravenously for the purposes of euthanasia in both belgium and the netherlands where active euthanasia is allowed by law the standard protocol recommends sodium thiopental as the ideal agent to induce coma followed by pancuronium bromide to paralyze muscles and stop breathing 17 intravenous administration is the most reliable and rapid way to accomplish euthanasia death is quick a coma is first induced by intravenous administration of 20 mg kg thiopental sodium nesdonal in a small volume 10 ml physiological saline then a triple dose of a non depolarizing neuromuscular blocking drug is given such as 20 mg pancuronium bromide pavulon or 20 mg vecuronium bromide norcuron the paralytic should be given intravenously to ensure optimal bioavailability but pancuronium bromide may be administered intramuscularly at an increased dosage level of 40 mg 17 lethal injection edit further information lethal injection along with pancuronium bromide and potassium chloride thiopental is used in 34 us states to execute prisoners by lethal injection a large dose is given to ensure rapid loss of consciousness although death usually occurs within ten minutes of the beginning of the injection process some have been known to take longer 18 in december 2009 ohio became the first state in the us to use a single dose of sodium thiopental for an execution following the failed use of the standard three drug cocktail during a prior execution due to inability to locate suitable veins kenneth biros was executed using the single drug method 19 washington became the second state in the us to use the single dose sodium thiopental injections for executions in september 2010 the execution of cal coburn brown was the first in the state to use a single dose single drug injection his death was pronounced approximately one and a half minutes after the intravenous administration of five grams of the drug 20 after its use for the execution of jeffrey landrigan in the us the united kingdom introduced a ban on the export of sodium thiopental in december 2010 21 after it was established that no european supplies to the us were being used for any other purpose 22 the restrictions were based on the european union torture regulation including licensing of drugs used in execution by lethal injection 23 from 21 december 2011 the eu extended trade restrictions to prevent the export of certain medicinal products for capital punishment stating that the union disapproves of capital punishment in all circumstances and works towards its universal abolition 24 truth serum edit further information truth serum thiopental is still used in some places as a truth serum to weaken the resolve of a subject and make the individual more compliant to pressure 25 barbiturates decrease both higher cortical brain function and inhibition it is thought that because lying is a more involved process than telling the truth suppression of the higher cortical functions may lead to the uncovering of the truth the drug tends to make subjects verbose and cooperative with interrogators however the reliability of confessions made under thiopental is questionable 26 psychiatry edit psychiatrists have used thiopental to desensitize patients with phobias 27 and to facilitate the recall of painful repressed memories 28 one psychiatrist who worked with thiopental is jan bastiaans who used this procedure to help relieve trauma in surviving victims of the holocaust 29 another notable psychiatrist using thiopental for the first time in the 1960s in psychoanalytic therapy setting in a somewhat similar way to psycholytic psychotherapy was the hungarian australian psychiatrist imre zádor 30 he administered thiopental to psychotherapy patients to reduce transferential resistance in cases of anorexia nervosa as well as to resolve unconscious blockages in other cases mechanism of action edit main article barbiturate sodium thiopental is a member of the barbiturate class of drugs which are relatively non selective compounds that bind to an entire superfamily of ligand gated ion channels of which the gaba a receptor channel is one of several representatives this superfamily of ion channels includes the neuronal nicotinic acetylcholine receptor nachr the 5 ht3 receptor the glycine receptor and others surprisingly while gaba a receptor currents are increased by barbiturates and other general anesthetics ligand gated ion channels that are predominantly permeable for cationic ions are blocked by these compounds for example neuronal nachr are blocked by clinically relevant anesthetic concentrations of both sodium thiopental and pentobarbital 31 such findings implicate non gabaergic ligand gated ion channels e g the neuronal nachr in mediating some of the side effects of barbiturates 32 the gaba a receptor is an inhibitory channel that decreases neuronal activity and barbiturates enhance the inhibitory action of the gaba a receptor 33 controversies edit following a shortage that led a court to delay an execution in california a company spokesman for hospira the sole american manufacturer of the drug objected to the use of thiopental in lethal injection hospira manufactures this product because it improves or saves lives and the company markets it solely for use as indicated on the product labeling the drug is not indicated for capital punishment and hospira does not support its use in this procedure 34 on january 21 2011 the company announced that it would stop production of sodium thiopental from its plant in italy because it could not provide italian authorities with guarantees that exported doses would not be used in executions according to a company spokesperson italy was the only viable place where it could produce the drug leaving the us without a supplier 35 in october 2015 the us food and drug administration fda confiscated an overseas shipment of thiopental destined for the states of arizona and texas the fda said in a statement courts have concluded that sodium thiopental for the injection in humans is an unapproved drug and may not be imported into the country 36 metabolism edit thiopental rapidly and easily crosses the blood brain barrier as it is a lipophilic molecule as with all lipid soluble anaesthetic drugs the short duration of action of sodium thiopental is due almost entirely to its redistribution away from central circulation into muscle and fatty tissue due to its very high lipid water partition coefficient approximately 10 leading to sequestration in fatty tissue once redistributed the free fraction in the blood is metabolized in the liver by zero order kinetics sodium thiopental is mainly metabolized to pentobarbital 37 5 ethyl 5 1 methyl 3 hydroxybutyl 2 thiobarbituric acid and 5 ethyl 5 1 methyl 3 carboxypropyl 2 thiobarbituric acid 38 dosage edit the usual dose range for induction of anesthesia using thiopental is from 3 to 6 mg kg however there are many factors that can alter this premedication with sedatives such as benzodiazepines or clonidine will reduce requirements due to drug synergy as do specific disease states and other patient factors among patient factors are age sex and lean body mass 39 specific disease conditions that can alter the dose requirements of thiopentone and for that matter any other intravenous anaesthetic are hypovolemia burns azotemia liver failure hypoproteinemia etc 40 contraindications edit thiopental should be used with caution in cases of liver disease addison s disease myxedema severe heart disease severe hypotension a severe breathing disorder or a family history of porphyria 41 42 co administration of pentoxifylline and thiopental causes death by acute pulmonary edema in rats this pulmonary edema was not mediated by cardiac failure or by pulmonary hypertensio...
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