Halothane , sold under the brandname Fluothane among others, is a general anesthetic . It can be used to start or maintain anaesthesia . One of its benefits is that it does not increase the production of saliva which can be particularly useful in those who are difficult to intubate . It is used by inhalation .[2]
Side effects include an irregular heartbeat , decreased effort to breathe (respiratory depression), and liver problems . It should not be used in people with porphyria or a history of malignant hyperthermia either in themselves or their family members.[2] It is unclear whether use during pregnancy is harmful to the baby, and it is not generally recommended for use during a cesarean section .[3]
Halothane was discovered in 1955.[4] It is on the World Health Organization's List of Essential Medicines , the most effective and safe medicines needed in a health system .[5] As of 2014 the wholesale cost in the developing world is about 22 to 52 USD for a 250 ml bottle.[6] Its use in developed countries has been mostly replaced by newer agents such as sevoflurane .[7] It is no longer commercially available in the United States.[3]
Medical uses [ edit ]
Packaging of ICI Fluothane (their trade name for halothane)
It is a potent anesthetic with a MAC of 0.74%. Its blood/gas partition coefficient of 2.4 makes it an agent with moderate induction and recovery time. It is not a good analgesic and its muscle relaxation effect is moderate.[8]
Side effects [ edit ]
In rare cases, repeated exposure to halothane in adults was noted to result in severe liver injury. This occurred in about one in 10,000 exposures. The resulting syndrome was referred to as halothane hepatitis , and is thought to result from the metabolism of halothane to trifluoroacetic acid via oxidative reactions in the liver. About 20% of inhaled halothane is metabolized by the liver and these products are excreted in the urine. The hepatitis syndrome had a mortality rate of 30% to 70%. Concern for hepatitis resulted in a dramatic reduction in the use of halothane for adults and it was replaced in the 1980s by enflurane and isoflurane . By 2005, the most common volatile anesthetics used were isoflurane , sevoflurane , and desflurane . Since the risk of halothane hepatitis in children was substantially lower than in adults, halothane continued to be used in pediatrics in the 1990s as it was especially useful for inhalation induction of anaesthesia . However, by 2000, sevoflurane, excellent for inhalation induction, had largely replaced the use of halothane in children.
Halothane sensitises the heart to catecholamines, so it is liable to cause cardiac arrhythmias, occasionally fatal, particularly if hypercapnia has been allowed to develop. This seems to be especially problematic in dental anaesthesia.
Like all the potent inhalational anaesthetic agents, it is a potent trigger for malignant hyperthermia . Similarly, in common with the other potent inhalational agents, it relaxes uterine smooth muscle and this may increase blood loss during delivery or termination of pregnancy.
Occupational safety [ edit ]
People can be exposed to halothane in the workplace by breathing it in as waste anaesthetic gas, skin contact, eye contact, or swallowing it. The National Institute for Occupational Safety and Health (NIOSH) has set a recommended exposure limit (REL) of 2 ppm (16.2 mg/m3 ) over 60 minutes.[9]
Pharmacology [ edit ]
Halothane activates GABAA and glycine receptors .[10] [11] It also acts as an NMDA receptor antagonist ,[11] inhibits nACh and voltage-gated sodium channels ,[10] [12] and activates 5-HT3 and twin-pore K+ channels .[10] [13] It does not affect the AMPA or kainate receptors .[11]
Chemical and physical properties [ edit ]
Chemically, halothane is an alkyl halide (not an ether like many other anesthetics).[14] The structure has one stereocenter, so (R )- and (S )-optical isomers occur.
Synthesis [ edit ]
The commercial synthesis of halothane starts from trichloroethylene , which is reacted with hydrogen fluoride in the presence of antimony trichloride at 130 °C to form 2-chloro-1,1,1-trifluoroethane. This is then reacted with bromine at 450 °C to produce halothane.[15]
Related substances [ edit ]
Attempts to find anesthetics with less metabolism led to halogenated ethers such as enflurane and isoflurane. The incidence of hepatic reactions with these agents is lower. The exact degree of hepatotoxic potential of enflurane is debated, although it is minimally metabolized. Isoflurane is essentially not metabolized and reports of associated liver injury are quite rare. Small amounts of trifluoroacetic acid can be formed from both halothane and isoflurane metabolism and possibly accounts for cross sensitization of patients between these agents.
The main advantage of the more modern agents is lower blood solubility, resulting in faster induction of and recovery from anaesthesia.
History [ edit ]
Halothane was first synthesized by C. W. Suckling of Imperial Chemical Industries in 1951 in Widnes and was first used clinically by M. Johnstone in Manchester in 1956. It became popular as a nonflammable general anesthetic replacing other volatile anesthetics such as trichloroethylene , diethyl ether and cyclopropane . In many parts of the world it has been largely replaced by newer agents since the 1980s but is still widely used in developing countries and in veterinary surgery because of its lower cost.
A meter for measuring halothane. This was used to measure the amount of halothane a flow of inspired gas during anesthesia.
Halothane was given to many millions of adult and pediatric patients worldwide from its introduction in 1956 through the 1980s.[16] Its properties include cardiac depression at high levels, cardiac sensitization to catecholamines such as norepinephrine , and potent bronchial relaxation. Its lack of airway irritation made it a common inhalation induction agent in pediatric anesthesia. Due to its cardiac depressive effect, it was contraindicated in patients with cardiac failure. Halothane was also contraindicated in patients susceptible to cardiac arrhythmias , or in situations related to high catecholamine levels such as pheochromocytoma .
Availability [ edit ]
It is available as a volatile liquid, at 30, 50, 200, and 250 ml per container[17] but in many developed nations is not available having been displaced by newer agents.
It is the only inhalational anesthetic containing bromine . It is colorless and pleasant-smelling, but unstable in light. It is packaged in dark-colored bottles and contains 0.01% thymol as a stabilizing agent.
References [ edit ]
^ DrugBank: DB01159 (Halothane)
^ a b WHO Model Formulary 2008 (PDF) . World Health Organization. 2009. pp. 17–18. ISBN 9789241547659 . Retrieved 8 December 2016 .
^ a b "Halothane - FDA prescribing information, side effects and uses" . www.drugs.com . June 2005. Retrieved 13 December 2016 .
^ Walker, S. R. (2012). Trends and Changes in Drug Research and Development . Springer Science & Business Media. p. 109. ISBN 9789400926592 .
^ "WHO Model List of EssentialMedicines" (PDF) . World Health Organization . October 2013. Retrieved 22 April 2014 .
^ "Halothane" . International Drug Price Indicator Guide . Retrieved 13 August 2015 .
^ Yentis, Steven M.; Hirsch, Nicholas P.; Ip, James (2013). Anaesthesia and Intensive Care A-Z: An Encyclopedia of Principles and Practice (5 ed.). Elsevier Health Sciences. p. 264. ISBN 9780702053757 .
^ "Halothane" .
^ "CDC - NIOSH Pocket Guide to Chemical Hazards - Halothane" . www.cdc.gov . Retrieved 2015-11-03 .
^ a b c Hugh C. Hemmings; Philip M. Hopkins (2006). Foundations of Anesthesia: Basic Sciences for Clinical Practice . Elsevier Health Sciences. pp. 292–. ISBN 0-323-03707-0 .
^ a b c Paul Barash; Bruce F. Cullen; Robert K. Stoelting; Michael Cahalan; Christine M. Stock; Rafael Ortega (7 February 2013). Clinical Anesthesia, 7e: Print + Ebook with Multimedia . Lippincott Williams & Wilkins. pp. 116–. ISBN 978-1-4698-3027-8 .
^ Jürgen Schüttler; Helmut Schwilden (8 January 2008). Modern Anesthetics . Springer Science & Business Media. pp. 70–. ISBN 978-3-540-74806-9 .
^ Norman G. Bowery (19 June 2006). Allosteric Receptor Modulation in Drug Targeting . CRC Press. pp. 143–. ISBN 978-1-4200-1618-5 .
^ "DrugBank: Halothane (DB01159)" . 17 December 2010.
^ Suckling et al.,"PROCESS FOR THE PREPARATION OF 1,1,1-TRIFLUORO-2-BROMO-2-CHLOROETHANE" , US patent 2921098 , granted January 1960 , assigned to Imperial Chemical Industries
^ Niedermeyer, Ernst; Silva, F. H. Lopes da (2005). Electroencephalography: Basic Principles, Clinical Applications, and Related Fields . Lippincott Williams & Wilkins. p. 1156. ISBN 978-0-7817-5126-1 .
^ National formulary of India, 4th Ed. New Delhi, India, Indian Pharmacopoeia commission; 2011: 411
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LY-233,053
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Ro8-4304
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PAMs: Alcohols (e.g., brometone , chlorobutanol (chloretone) , ethanol , tert -butanol (2M2P) , tribromoethanol , trichloroethanol , trifluoroethanol )
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RU-5135
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Trihexyphenidyl
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WIN-2299
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Nicotinic agonists : 5-HIAA
A-84,543
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A-867,744
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SB-206553
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TC-1698
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WAY-317,538
XY-4083
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Atypical antipsychotics (e.g., aripiprazole , asenapine , clozapine , lurasidone , quetiapine , ziprasidone )
Azapirones (e.g., buspirone , eptapirone , gepirone , perospirone , tandospirone )
Bay R 1531
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BMY-14802
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Dimemebfe
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F-11461
F-12826
F-13714
F-14679
F-15063
F-15599
Flesinoxan
Flibanserin
Flumexadol
Lesopitron
LY-293284
LY-301317
mCPP
MKC-242
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Piclozotan
Rauwolscine
Repinotan
Roxindole
RU-24969
S-14506
S-14671
S-15535
Sarizotan
Serotonin (5-HT)
SSR-181507
Sunepitron
Tryptamines (e.g., 5-CT , 5-MeO-DMT , 5-MT , bufotenin , DMT , indorenate , N-Me-5-HT , psilocin , psilocybin )
TGBA01AD
U-92016A
Urapidil
Vilazodone
Xaliproden
Yohimbine
Antagonists: Atypical antipsychotics (e.g., iloperidone , risperidone , sertindole )
AV965
Beta blockers (e.g., alprenolol , cyanopindolol , iodocyanopindolol , oxprenolol , pindobind , pindolol , propranolol , tertatolol )
BMY-7378
CSP-2503
Dotarizine
Ergolines (e.g., metergoline )
Flopropione
GR-46611
Isamoltane
Lecozotan
Mefway
Metitepine (methiothepin)
MIN-117 (WF-516)
MPPF
NAN-190
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S-15535
SB-649915
SDZ 216-525
Spiperone
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Spiroxatrine
UH-301
WAY-100135
WAY-100635
Xylamidine
5-HT1B
Agonists: CGS-12066A
CP-93129
CP-94253
CP-122,288
CP-135807
Eltoprazine
Ergolines (e.g., bromocriptine , dihydroergotamine , ergotamine , methylergometrine (methylergonovine) , methysergide , pergolide )
mCPP
RU-24969
Serotonin (5-HT)
Triptans (e.g., avitriptan , donitriptan , eletriptan , sumatriptan , zolmitriptan )
TFMPP
Tryptamines (e.g., 5-BT , 5-CT , 5-MT , DMT )
Vortioxetine
5-HT1D
Agonists: CP-122,288
CP-135807
CP-286601
Ergolines (e.g., bromocriptine , cabergoline , dihydroergotamine , ergotamine , LSD , methysergide )
GR-46611
L-694247
L-772405
mCPP
PNU-109291
PNU-142633
Serotonin (5-HT)
TGBA01AD
Triptans (e.g., almotriptan , avitriptan , donitriptan , eletriptan , frovatriptan , naratriptan , rizatriptan , sumatriptan , zolmitriptan )
Tryptamines (e.g., 5-BT , 5-CT , 5-Et-DMT , 5-MT , 5-(nonyloxy)tryptamine , DMT )
5-HT1E
5-HT1F
5-HT2A
Agonists: 25H/NB series (e.g., 25I-NBF , 25I-NBMD , 25I-NBOH , 25I-NBOMe , 25B-NBOMe , 25C-NBOMe , 25TFM-NBOMe , 2CBCB-NBOMe , 25CN-NBOH , 2CBFly-NBOMe )
2Cs (e.g., 2C-B , 2C-E , 2C-I , 2C-T-2 , 2C-T-7 , 2C-T-21 )
2C-B-FLY
2CB-Ind
5-Methoxytryptamines (5-MeO-DET , 5-MeO-DiPT , 5-MeO-DMT , 5-MeO-DPT , 5-MT )
α-Alkyltryptamines (e.g., 5-Cl-αMT , 5-Fl-αMT , 5-MeO-αET , 5-MeO-αMT , α-Me-5-HT , αET , αMT )
AL-34662
AL-37350A
Bromo-DragonFLY
Dimemebfe
DMBMPP
DOx (e.g., DOB , DOC , DOI , DOM )
Efavirenz
Ergolines (e.g., 1P-LSD , ALD-52 , bromocriptine , cabergoline , ergine (LSA) , ergotamine , lisuride , LA-SS-Az , LSB , LSD , LSD-Pip , LSH , LSP , methylergometrine (methylergonovine) , pergolide )
Flumexadol
Jimscaline
Lorcaserin
MDxx (e.g., MDA , MDMA , MDOH , MMDA )
O-4310
Oxaflozane
PHA-57378
PNU-22394
PNU-181731
RH-34
Phenethylamines (e.g., lophophine , mescaline )
Piperazines (e.g., BZP , mCPP , quipazine , TFMPP )
Serotonin (5-HT)
TCB-2
TFMFly
Tryptamines (e.g., 5-BT , 5-CT , bufotenin , DET , DiPT , DMT , DPT , psilocin , psilocybin , tryptamine )
Antagonists: 5-I-R91150
5-MeO-NBpBrT
AC-90179
Adatanserin
Altanserin
AMDA
APD-215
Atypical antipsychotics (e.g., amperozide , aripiprazole , asenapine , blonanserin , carpipramine , clocapramine , clorotepine , clozapine , fluperlapine , gevotroline , iloperidone , melperone , mosapramine , ocaperidone , olanzapine , paliperidone , quetiapine , risperidone , sertindole , zicronapine , ziprasidone , zotepine )
Cinanserin
CSP-2503
Cyproheptadine
Deramciclane
Dotarizine
Eplivanserin
Ergolines (e.g., amesergide , LY-53857 , LY-215840 , mesulergine , metergoline , methysergide , sergolexole )
Etoperidone
Fananserin
Flibanserin
Glemanserin
Irindalone
Ketanserin
KML-010
Lubazodone
LY-393558
Medifoxamine
Mepiprazole
Metitepine (methiothepin)
MIN-101
Naftidrofuryl
Nantenine
Nefazodone
Pelanserin
Phenoxybenzamine
Pimavanserin
Pirenperone
Pizotifen
Pruvanserin
Rauwolscine
Ritanserin
S-14671
Sarpogrelate
Setoperone
Spiperone
Spiramide
SR-46349B
TGBA01AD
Teniloxazine
Temanogrel
Tetracyclic antidepressants (e.g., amoxapine , aptazapine , esmirtazapine , maprotiline , mianserin , mirtazapine )
Trazodone
Tricyclic antidepressants (e.g., amitriptyline )
Typical antipsychotics (e.g., chlorpromazine , fluphenazine , haloperidol , loxapine , perphenazine , pimozide , pipamperone , prochlorperazine , thioridazine , thiothixene , trifluoperazine )
Volinanserin
Xylamidine
Yohimbine
5-HT2B
Agonists: 4-Methylaminorex
Aminorex
Amphetamines (eg., chlorphentermine , cloforex , dexfenfluramine , fenfluramine , levofenfluramine , norfenfluramine )
BW-723C86
DOx (e.g., DOB , DOC , DOI , DOM )
Ergolines (e.g., cabergoline , dihydroergocryptine , dihydroergotamine , ergotamine , methylergometrine (methylergonovine) , methysergide , pergolide )
MDxx (e.g., MDA , MDMA , MDOH , MMDA )
Piperazines (e.g., mCPP )
PNU-22394
Ro60-0175
Serotonin (5-HT)
Tryptamines (e.g., 5-BT , 5-CT , 5-MT , α-Me-5-HT , bufotenin , DET , DiPT , DMT , DPT , psilocin , psilocybin , tryptamine )
5-HT2C
Agonists: 2Cs (e.g., 2C-B , 2C-E , 2C-I , 2C-T-2 , 2C-T-7 , 2C-T-21 )
5-Methoxytryptamines (5-MeO-DET , 5-MeO-DiPT , 5-MeO-DMT , 5-MeO-DPT , 5-MT )
α-Alkyltryptamines (e.g., 5-Cl-αMT , 5-Fl-αMT , 5-MeO-αET , 5-MeO-αMT , α-Me-5-HT , αET , αMT )
A-372159
AL-38022A
Alstonine
CP-809101
Dimemebfe
DOx (e.g., DOB , DOC , DOI , DOM )
Ergolines (e.g., ALD-52 , cabergoline , dihydroergotamine , ergine (LSA) , ergotamine , lisuride , LA-SS-Az , LSB , LSD , LSD-Pip , LSH , LSP , pergolide )
Flumexadol
Lorcaserin
MDxx (e.g., MDA , MDMA , MDOH , MMDA )
MK-212
Org 12962
Org 37684
Oxaflozane
PHA-57378
Phenethylamines (e.g., lophophine , mescaline )
Piperazines (e.g., aripiprazole , BZP , mCPP , quipazine , TFMPP )
PNU-22394
PNU-181731
Ro60-0175
Ro60-0213
Serotonin (5-HT)
Tryptamines (e.g., 5-BT , 5-CT , bufotenin , DET , DiPT , DMT , DPT , psilocin , psilocybin , tryptamine )
Vabicaserin
WAY-629
WAY-161503
YM-348
Antagonists: Adatanserin
Agomelatine
Atypical antipsychotics (e.g., asenapine , clorotepine , clozapine , fluperlapine , iloperidone , melperone , olanzapine , paliperidone , quetiapine , risperidone , sertindole , ziprasidone , zotepine )
Captodiame
CEPC
Cinanserin
Cyproheptadine
Deramciclane
Dotarizine
Eltoprazine
Ergolines (e.g., amesergide , bromocriptine , LY-53857 , LY-215840 , mesulergine , metergoline , methysergide , sergolexole )
Etoperidone
Fluoxetine
FR-260010
Irindalone
Ketanserin
Ketotifen
Latrepirdine (dimebolin)
Medifoxamine
Metitepine (methiothepin)
Nefazodone
Pirenperone
Pizotifen
Propranolol
Ritanserin
RS-102221
S-14671
SB-200646
SB-206553
SB-221284
SB-228357
SB-242084
SB-243213
SDZ SER-082
Tedatioxetine
Tetracyclic antidepressants (e.g., amoxapine , aptazapine , esmirtazapine , maprotiline , mianserin , mirtazapine )
TIK-301
Trazodone
Tricyclic antidepressants (e.g., amitriptyline , nortriptyline )
Typical antipsychotics (e.g., chlorpromazine , loxapine , pimozide , pipamperone , thioridazine )
Xylamidine
5-HT3
Agonists: Alcohols (e.g., butanol , ethanol , trichloroethanol )
m-CPBG
Phenylbiguanide
Piperazines (e.g., BZP , mCPP , quipazine )
RS-56812
Serotonin (5-HT)
SR-57227
SR-57227A
Tryptamines (e.g., 2-Me-5-HT , 5-CT , bufotenidine (5-HTQ) )
Volatiles/gases (e.g., halothane , isoflurane , toluene , trichloroethane )
YM-31636
Antagonists: Alosetron
AS-8112
Atypical antipsychotics (e.g., clozapine , olanzapine , quetiapine )
Azasetron
Batanopride
Bemesetron (MDL-72222)
Cilansetron
CSP-2503
Dazopride
Dolasetron
Galanolactone
Granisetron
ICS-205930
Lerisetron
Memantine
Ondansetron
Palonosetron
Ramosetron
Renzapride
Ricasetron
Tedatioxetine
Tetracyclic antidepressants (e.g., amoxapine , mianserin , mirtazapine )
Thujone
Tropanserin
Tropisetron
Typical antipsychotics (e.g., loxapine )
Volatiles/gases (e.g., nitrous oxide , sevoflurane , xenon )
Vortioxetine
Zacopride
Zatosetron
5-HT4
5-HT5A
5-HT6
Agonists: Ergolines (e.g., dihydroergocryptine , dihydroergotamine , ergotamine , lisuride , LSD , mesulergine , metergoline , methysergide )
Serotonin (5-HT)
Tryptamines (e.g., 2-Me-5-HT , 5-BT , 5-CT , 5-MT , Bufotenin , E-6801 , E-6837 , EMD-386088 , EMDT , LY-586713 , N-Me-5-HT , tryptamine )
WAY-181187
WAY-208466
Antagonists: ABT-354
Atypical antipsychotics (e.g., aripiprazole , asenapine , clorotepine , clozapine , fluperlapine , iloperidone , olanzapine , tiospirone )
AVN-101
AVN-211
AVN-322
AVN-397
BGC20-760
BVT-5182
BVT-74316
Cerlapirdine
EGIS-12233
GW-742457
Idalopirdine
Ketanserin
Latrepirdine (dimebolin)
Metitepine (methiothepin)
MS-245
PRX-07034
Ritanserin
Ro04-6790
Ro 63-0563
SB-258585
SB-271046
SB-357134
SB-399885
SB-742457
Tetracyclic antidepressants (e.g., amoxapine , mianserin )
Tricyclic antidepressants (e.g., amitriptyline , clomipramine , doxepin , nortriptyline )
Typical antipsychotics (e.g., chlorpromazine , loxapine )
5-HT7
Antagonists: Atypical antipsychotics (e.g., amisulpride , aripiprazole , asenapine , clorotepine , clozapine , fluperlapine , olanzapine , risperidone , sertindole , tiospirone , ziprasidone , zotepine )
Butaclamol
DR-4485
EGIS-12233
Ergolines (e.g., 2-Br-LSD (BOL-148) , amesergide , bromocriptine , cabergoline , dihydroergotamine , ergotamine , LY-53857 , LY-215840 , mesulergine , metergoline , methysergide , sergolexole )
JNJ-18038683
Ketanserin
LY-215840
Metitepine (methiothepin)
Ritanserin
SB-258719
SB-258741
SB-269970
SB-656104
SB-656104A
SB-691673
SLV-313
SLV-314
Spiperone
SSR-181507
Tetracyclic antidepressants (e.g., amoxapine , maprotiline , mianserin , mirtazapine )
Tricyclic antidepressants (e.g., amitriptyline , clomipramine , imipramine )
Typical antipsychotics (e.g., acetophenazine , chlorpromazine , chlorprothixene , fluphenazine , loxapine , pimozide )
Vortioxetine