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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/06/28 19:59:26」(JST)
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Not to be confused with Profadol.
| Systematic (IUPAC) name | |
|---|---|
| 2,6-diisopropylphenol | |
| Clinical data | |
| Pregnancy cat. | B (U.S.), C (Au) |
| Legal status | Prescription Only (S4) (AU) ℞-only (U.S.) |
| Routes | Intravenous |
| Pharmacokinetic data | |
| Bioavailability | NA |
| Protein binding | 95 to 99% |
| Metabolism | Hepatic glucuronidation |
| Half-life | 30 to 60 min |
| Excretion | Hepatic |
| Identifiers | |
| CAS number | 2078-54-8 Y |
| ATC code | N01AX10 |
| PubChem | CID 4943 |
| DrugBank | DB00818 |
| ChemSpider | 4774 Y |
| UNII | YI7VU623SF Y |
| KEGG | D00549 Y |
| ChEBI | CHEBI:44915 Y |
| ChEMBL | CHEMBL526 Y |
| Chemical data | |
| Formula | C12H18O |
| Mol. mass | 178.271 g/mol |
|
SMILES
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InChI
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| Y (what is this?) (verify) | |
Propofol (INN, marketed as Diprivan by AstraZeneca) is a short-acting, intravenously administered hypnotic/amnestic agent. Its uses include the induction and maintenance of general anesthesia, sedation for mechanically ventilated adults, and procedural sedation. Propofol is also commonly used in veterinary medicine. Propofol is approved for use in more than 50 countries, and generic versions are available.
Chemically, propofol is unrelated to barbiturates and has largely replaced sodium thiopental (Pentothal) for induction of anesthesia because recovery from propofol is more rapid and "clear" when compared with thiopental. Propofol is not considered an analgesic, so opioids such as fentanyl may be combined with propofol to alleviate pain.[1] Propofol has been referred to as milk of amnesia (a play on words of milk of magnesia), because of the milk-like appearance of its intravenous preparation.[2] It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a health system.[3]
Contents
- 1 Medical uses
- 2 Other uses
- 2.1 Executions
- 2.2 Recreational use
- 3 Adverse effects
- 3.1 Propofol infusion syndrome
- 4 Contraindications and interactions
- 5 Chemistry
- 6 Mechanism of action
- 7 Pharmacokinetics
- 8 Supply issues
- 9 Recent developments
- 10 References
- 11 External links
Medical uses
Propofol is used for induction of anesthesia, having largely replaced sodium thiopental for this indication.[1] Propofol can also be administered as part of an anaesthesia maintenance technique called TIVA (Total Intravenous Anaesthesia) using computer controlled infusion pumps in a process called target controlled infusion or TCI. Propofol is also used to sedate individuals who are receiving mechanical ventilation who are not undergoing surgery, such as patients in the intensive care unit. In critically ill patients, propofol has been found to be superior to lorazepam both in effectiveness as well as overall cost.[4] Propofol is also used for procedural sedation, for example during endoscopic procedures. Its use in these settings results in a faster recovery compared to midazolam.[5] Due to its fast induction and recovery time, propofol is also widely used for sedation of infants and children undergoing MRI.[6]
In combination with remifentanil, propofol is used for anesthesia of patient undergoing electroconvulsive therapy.[7]
Other uses
Executions
The Missouri Supreme Court decided to allow the use of propofol to execute prisoners condemned to death. However, the first execution by administration of a lethal dose of propofol was halted on 11 October 2013 by governor Jay Nixon following threats from the European Union to limit the drug's export if it were used for that purpose.[8][9]
Recreational use
There are reports of self-administration of propofol for recreational purposes.[10][11] Short-term effects include mild euphoria, hallucinations, and disinhibition.[12][13] Long-term use has been reported to result in addiction.[14][15] Such use of the drug has been described amongst medical staff, such as anesthetists who have access to the drug.[14] Recreational use is reported to be more common among anesthetists on rotations with short rest periods, as recreational users report rousing to a well-rested state.[16] Recreational use of the drug is relatively rare due to its potency and the level of monitoring required to take it safely. Propofol has not been scheduled by the US Drug Enforcement Administration.[16][17] The steep dose-response curve of the drug makes potential misuse very dangerous without proper monitoring, and at least three deaths from self-administration have been recorded.[18][19]
Attention to the risks of off-label use of propofol increased in August 2009 due to the Los Angeles County coroner's conclusion that pop icon Michael Jackson died from a mixture of propofol and the benzodiazepine drugs lorazepam on top of diazepam ingested earlier.[20][21][22][23] According to a 22 July 2009 search warrant affidavit unsealed by the district court of Harris County, Texas, Jackson's personal physician, Conrad Murray, administered 25 milligrams of propofol diluted with lidocaine shortly before Jackson's death.[21][22][24]
Adverse effects
One of propofol's most frequent side effects is pain on injection, especially in smaller veins. This pain arises from activation of the pain receptor, TRPA1,[25] found on sensory nerves and can be mitigated by pretreatment with lidocaine.[26]Empirically, less pain is experienced when infused at a slower rate, in a large vein (Anitcubital Fossa). Patients show great variability in their response to propofol, at times showing profound sedation with small doses.
Additional side effects include low blood pressure related to vasodilation, transient apnea following induction doses, and cerebrovascular effects. Propofol has more pronounced hemodynamic effects relative to many intravenous anesthetic agents.[27] Reports of blood pressure drops as much as 30% or more are thought to be at least partially due to inhibition of sympathetic nerve activity.[28] This effect is related to dose and rate of propofol administration. It may also be potentiated by opioid analgesics.[29] Propofol can also cause decreased systemic vascular resistance, myocardial blood flow, and oxygen consumption, possibly through direct vasodilation.[30]
As a respiratory depressant, propofol frequently produces apnea. The persistence of apnea can depend on factors such as premedication, dose administered and rate of administration, and may sometimes persist for longer than 60 seconds.[31] Possibly as the result of depression of the central inspiratory drive, propofol may produce significant decreases in respiratory rate, minute volume, tidal volume, mean inspiratory flow rate and functional residual capacity.[27]
Diminishing cerebral blood flow, cerebral metabolic oxygen consumption and intracranial pressure are also characteristic of propofol administration.[32] In addition, propofol may decrease intraocular pressure by as much as 30 to 50% in patients with normal intraocular pressure.[33]
A more serious but rare side effect is dystonia.[34] Mild myoclonic movements are common, as with other intravenous hypnotic agents. Propofol appears to be safe for use in porphyria, and has not been known to trigger malignant hyperpyrexia.
Propofol has reportedly induced priapism in some individuals.[35][36]
Propofol administration to achieve the recommended level of sedation suppresses the REM sleep stage and further worsens the poor sleep quality of these patients.[37]
It has been reported that the euphoria caused by propofol is unlike that caused by other sedation agents, "I even remember my first experience using propofol: a young woman who was emerging from a MAC anesthesia[38] looked at me as though I were a masked Brad Pitt and told me that she felt simply wonderful." —C.F. Ward, M.D.[39]
Propofol infusion syndrome
Main article: Propofol infusion syndrome
Another recently described rare, but serious, side effect is propofol infusion syndrome. This potentially lethal metabolic derangement has been reported in critically ill patients after a prolonged infusion of high-dose substance in combination with catecholamines and/or corticosteroids.[40]
Contraindications and interactions
The respiratory effects of propofol are potentiated by other respiratory depressants, including benzodiazepines.[41] As with any other general anesthetic agent, propofol should be administered only where appropriately trained staff and facilities for monitoring are available, as well as proper airway management, a supply of supplemental oxygen, artificial ventilation and cardiovascular resuscitation.[42]
Chemistry
20-mL ampoule of 1% propofol emulsion, as sold in Australia by Sandoz
Propofol was originally developed in the UK by Imperial Chemical Industries as ICI 35868. Clinical trials followed in 1977, using a form solubilised in cremophor EL. However, due to anaphylactic reactions to cremophor, this formulation was withdrawn from the market and subsequently reformulated as an emulsion of a soya oil/propofol mixture in water. The emulsified formulation was relaunched in 1986 by ICI (now AstraZeneca) under the brand name Diprivan (abbreviated version of diisopropyl intravenous anesthetic)[citation needed]. The currently available preparation is 1% propofol, 10% soybean oil, and 1.2% purified egg phospholipid as an emulsifier, with 2.25% of glycerol as a tonicity-adjusting agent, and sodium hydroxide to adjust the pH. Diprivan contains EDTA, a common chelation agent, that also acts alone (bacteriostatically against some bacteria) and synergistically with some other antimicrobial agents. Newer generic formulations contain sodium metabisulfite or benzyl alcohol as antimicrobial agents. Propofol emulsion is a highly opaque white fluid due to the scattering of light from the tiny (~150 nm) oil droplets that it contains.
A water-soluble prodrug form, fospropofol, has recently been developed and tested with positive results. Fospropofol is rapidly broken down by the enzyme alkaline phosphatase to form propofol. Marketed as Lusedra, this new formulation may not produce the pain at injection site that often occurs with the traditional form of the drug. The US Food and Drug Administration approved the product in 2008.[43]
Mechanism of action
Propofol has been proposed to have several mechanisms of action,[44][45][46] both through potentiation of GABAA receptor activity, thereby slowing the channel-closing time,[47][48][49] and also acting as a sodium channel blocker.[50][51] Recent research has also suggested that the endocannabinoid system may contribute significantly to propofol's anesthetic action and to its unique properties.[52] EEG research upon those undergoing general anesthesia with propofol finds that it causes a prominent reduction in the brain's information integration capacity at gamma wave band frequencies.[53]
Researchers at Washington University School of Medicine in St. Louis and Imperial College London have identified the site where propofol binds to GABAA receptors in the brain.[54]
Pharmacokinetics
Propofol is highly protein-bound in vivo and is metabolised by conjugation in the liver.[55] The half life of elimination of propofol has been estimated at between 2 and 24 hours. However, its duration of clinical effect is much shorter, because propofol is rapidly distributed into peripheral tissues. When used for IV sedation, a single dose of propofol typically wears off within minutes. Propofol is versatile; the drug can be given for short or prolonged sedation as well as for general anesthesia. Its use is not associated with nausea as is often seen with opioid medications. These characteristics of rapid onset and recovery along with its amnestic effects[56] have led to its widespread use for sedation and anesthesia.
Supply issues
On 4 June 2010, Teva Pharmaceutical Industries Ltd., an Israel-based pharmaceutical firm and a major supplier of the drug, announced that the firm would no longer manufacture it. This aggravates an already existing shortage, caused by manufacturing difficulties at Teva and Hospira. A Teva spokesperson attributed the halt to ongoing process difficulties, and a number of pending lawsuits related to the drug.[57] In Switzerland, various preparations of the drug are supplied by Fresenius-Kabi, a German company.
Recent developments
By incorporation of an azobenzene unit, a photoswitchable version of propofol (AP2) was developed in 2012 that allows for optical control of GABAA receptors with light.[58] In 2013, a propofol binding site on mammalian GABAA receptors has been identified by photolabeling using a Diazirine derivative.[59] Additionally, it was shown that the hyaluronan polymer present in the synovia can be protected from free-radical depolymerization by propofol.[60]
References
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- ^ Euliano TY, Gravenstein JS (2004). "A brief pharmacology related to anesthesia". Essential anesthesia: from science to practice. Cambridge, UK: Cambridge University Press. p. 173. ISBN 0-521-53600-6. Retrieved 2 June 2009.
- ^ "WHO Model List of EssentialMedicines". World Health Organization. October 2013. p. 6. Retrieved 22 April 2014.
- ^ Cox, CE.; Reed, SD.; Govert, JA.; Rodgers, JE.; Campbell-Bright, S.; Kress, JP.; Carson, SS. (March 2008). "Economic evaluation of propofol and lorazepam for critically ill patients undergoing mechanical ventilation.". Crit Care Med 36 (3): 706–14. doi:10.1097/CCM.0B013E3181544248. PMC 2763279. PMID 18176312.
- ^ McQuaid, KR.; Laine, L. (May 2008). "A systematic review and meta-analysis of randomized, controlled trials of moderate sedation for routine endoscopic procedures.". Gastrointest Endosc 67 (6): 910–23. doi:10.1016/j.gie.2007.12.046. PMID 18440381.
- ^ Machata, AM; Willschke, H; Kabon, B; Kettner, SC; Marhofer, P (August 2008). "Propofol-based sedation regimen for infants and children undergoing ambulatory magnetic resonance imaging.". British journal of anaesthesia 101 (2): 239–43. doi:10.1093/bja/aen153. PMID 18534971. Cite uses deprecated parameters (help)
- ^ Ulusoy H H (February 2014). "Sevoflurane/remifentanil versus propofol/remifentanil for electroconvulsive therapy: comparison of seizure duration and haemodynamic responses.". J Int Med Res 42 (1): 111–119. doi:10.1177/0300060513509036. PMID 24398757.
- ^ Death Row Improvises, Lacking Lethal Mix, By RICK LYMAN, New York Times, 18 August 2013
- ^ After EU threats, Missouri halts execution by Propofol injection Al Jazeera America October 12th 2013
- ^ Riezzo I, Centini F, Neri M, Rossi G, Spanoudaki E, Turillazzi E, Fineschi V (2009). "Brugada-like EKG pattern and myocardial effects in a chronic propofol abuser". Clin Toxicol (Phila) 47 (4): 358–63. doi:10.1080/15563650902887842. PMID 19514884.
- ^ Belluck, Pam (6 August 2009). "With High-Profile Death, Focus on High-Risk Drug". New York Times. Retrieved 7 August 2009.
- ^ In Sweetman SC (Ed.). Martindale: The Complete Drug Reference 2005. 34th Edn London pp. 1305–7
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- ^ a b Roussin A, Montastruc JL, Lapeyre-Mestre M (21 October 2007). "Pharmacological and clinical evidences on the potential for abuse and dependence of propofol: a review of the literature". Fundamental and Clinical Pharmacology 21 (5): 459–66. doi:10.1111/j.1472-8206.2007.00497.x. PMID 17868199.
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- ^ DEA may limit drug eyed in Jackson case. Associated Press. 15 July 2009.
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- ^ Kranioti EF, Mavroforou A, Mylonakis P, Michalodimitrakis M. (22 March 2007). "Lethal self administration of propofol (Diprivan): A case report and review of the literature". Forensic Science International 167 (1): 56–8. doi:10.1016/j.forsciint.2005.12.027. PMID 16431058.
- ^ Moore, Solomon (28 August 2009). "Jackson’s Death Ruled a Homicide". New York Times.
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- ^ "Propofol Drug Information, Professional". m drugs.com. Retrieved 2 January 2007.
- ^ a b Sebel PS, Lowden JD (1989). Propofol: a new intravenous anesthetic. Anesthesiology; 71(2):260-77.
- ^ Robinson B, Ebert T, O'Brien T, et al. Mechanisms whereby propofol mediates peripheral vasodilation in humans (1997). Anesthesiology; 86:64-72.
- ^ New awakening in anaesthesia—at a price. Lancet 1987; 8548: 1469-70.
- ^ Larijani G, Gratz I, Afshar M, et al. Clinical pharmacology of propofol: an intravenous anesthetic agent [published erratum appears in DICP 1990 Jan; 24: 102]. DICP 1989; 23: 743-9.
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- ^ Bailey J, Mora C, Shafer S. Pharmacokinetics of propofol in adult patients undergoing coronary revascularization. Anesthesiology 1996; 84: 1288-97.
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- ^ Schramm BM, Orser BA (2002). Dystonic reaction to propofol attenuated by benztropine (Cogentin). Anesth Analg, 94, 1237–40.
- ^ Vesta, Kimi; Shaunta' Martina, Ellen Kozlowski (25 April 2009). "Propofol-Induced Priapism, a Case Confirmed with Rechallenge". The Annals of Pharmacotherapy 40 (5): 980–982. doi:10.1345/aph.1G555. PMID 16638914. Cite uses deprecated parameters (help);
|accessdate=requires|url=(help) - ^ Fuentes, Ennio; Silvia Garcia, Manuel Garrido, Cristina Lorenzo, Jose Iglesias, Juan Sola (July 2009). "Successful treatment of propofol-induced priapism with distal glans to corporal cavernosal shunt". Urology 74 (1): 113–115. doi:10.1016/j.urology.2008.12.066. PMID 19371930. Cite uses deprecated parameters (help);
|accessdate=requires|url=(help) - ^ "Effects of propofol on sleep quality in mechanically ventilated critically ill patients: a physiological study - Eumorfia Kondili, Christina Alexopoulou, Nectaria Xirouchaki, Dimitris Georgopoulos". http://icmjournal.esicm.org/. Retrieved 2 October 2012.
- ^ MAC anesthesia: Monitored anesthesia care
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- ^ Doheny, Kathleen; Louise Chang, Hector Vila Jr (24 August 2009). "Propofol Linked to Michael Jackson's Death". WebMD. Retrieved 26 August 2009. Cite uses deprecated parameters (help)
- ^ "AstraZeneca - United States Home Page". .astrazeneca-us.com. Retrieved 8 June 2013.
- ^ "Drugs@FDA: FDA Approved Drug Products". Accessdata.fda.gov. Retrieved 8 June 2013.
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- ^ Kotani Y, Shimazawa M, Yoshimura S, Iwama T, Hara H. The experimental and clinical pharmacology of propofol, an anesthetic agent with neuroprotective properties. CNS Neuroscience and Therapeutics. 2008 Summer;14(2):95–106. doi:10.1111/j.1527-3458.2008.00043.x PMID 18482023
- ^ Vanlersberghe C, Camu F. Propofol. Handbook of Experimental Pharmacology. 2008;(182):227-52. doi:10.1007/978-3-540-74806-9_11 PMID 18175094
- ^ Trapani G, Latrofa A, Franco M, Altomare C, Sanna E, Usala M, Biggio G, Liso G. Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors. Journal of Medicinal Chemistry. 21 May 1998;41(11):1846–54. doi:10.1021/jm970681h PMID 9599235
- ^ Krasowski MD, Jenkins A, Flood P, Kung AY, Hopfinger AJ, Harrison NL (April 2001). "General anesthetic potencies of a series of propofol analogs correlate with potency for potentiation of gamma-aminobutyric acid (GABA) current at the GABA(A) receptor but not with lipid solubility". J. Pharmacol. Exp. Ther. 297 (1): 338–51. PMID 11259561.
- ^ Krasowski MD, Hong X, Hopfinger AJ, Harrison NL. 4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor. Journal of Medicinal Chemistry. 18 July 2002;45(15):3210–21. doi:10.1021/jm010461a PMID 12109905
- ^ Haeseler G, Leuwer M (March 2003). "High-affinity block of voltage-operated rat IIA neuronal sodium channels by 2,6 di-tert-butylphenol, a propofol analogue". Eur J Anaesthesiol 20 (3): 220–4. doi:10.1017/s0265021503000371. PMID 12650493.
- ^ Haeseler G, Karst M, Foadi N, Gudehus S, Roeder A, Hecker H, Dengler R, Leuwer M. High-affinity blockade of voltage-operated skeletal muscle and neuronal sodium channels by halogenated propofol analogues. British Journal of Pharmacology. 2008 Sep;155(2):265-75. doi:10.1038/bjp.2008.255 PMID 18574460
- ^ Fowler CJ (February 2004). "Possible involvement of the endocannabinoid system in the actions of three clinically used drugs". Trends Pharmacol. Sci. 25 (2): 59–61. doi:10.1016/j.tips.2003.12.001.
- ^ Lee U, Mashour GA, Kim S, Noh GJ, Choi BM. (2009). Propofol induction reduces the capacity for neural information integration: implications for the mechanism of consciousness and general anesthesia. Conscious Cogn. 18(1):56–64. PMID 19054696 doi:10.1016/j.concog.2008.10.005
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- ^ Veselis RA, Reinsel RA, Feshchenko VA, Wroński M (October 1997). "The comparative amnestic effects of midazolam, propofol, thiopental, and fentanyl at equisedative concentrations". Anesthesiology 87 (4): 749–64. doi:10.1097/00000542-199710000-00007. PMID 9357875.
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- ^ Stein M, et al. (September 2012). "Azo-Propofols: Photochromic Potentiators of GABAA Receptors". Angewandte Chemie International Edition 51 (42): 15000–4. doi:10.1002/anie.201205475. PMID 22968919.
- ^ Yip G, Z.-W Chen, Edge C J, Smith E H, Dickinson R, Hohenester, E, Townsend R R, Fuchs K, Sieghart W, Evers A S, Franks N P (September 2013). "A propofol binding site on mammalian GABAAreceptors identified by photolabeling". Nature Chemical Biology. doi:10.1038/nchembio.1340.
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External links
- Diprivan web site run by AstraZeneca
- Detailed pharmaceutical information
- U.S. National Library of Medicine: Drug Information Portal – Propofol
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UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
- 1. Airway management for induction of general anesthesia
- 2. 成人における処置時の鎮静 procedural sedation in adults
- 3. Anesthesia for emergent eye surgery
- 4. Anesthesia for endovascular aortic repair
- 5. 小児に対する手術室外での鎮静処置に使用する薬剤 pharmacologic agents for pediatric procedural sedation outside of the operating room
English Journal
- Use of propofol as an anesthetic and its efficacy on some hematological values of ornamental fish Carassius auratus.
- Gholipourkanani H, Ahadizadeh S.SourceDepartment of fisheries and natural resource, agriculture faculty, Gonbad Kavous University, Gonbad Kavous, Iran.
- SpringerPlus.Springerplus.2013 Dec;2(1):76. Epub 2013 Mar 4.
- The aim of this study was to determine the level of anesthesia attained in Carassius auratus using a propofol bath administration and using values of haematological profile of blood and examinations, to assess the effects of the fish exposure to that anaesthetic. Acute toxicity values of propofol fo
- PMID 23539492
- Circumstantial and toxicological features of deaths from self-administered intravenous anesthetic/narcotic agents.
- Hayashi T, Buschmann C, Riesselmann B, Roscher S, Tsokos M.SourceInstitute of Legal Medicine and Forensic Sciences, University Medical Centre Charité, University of Berlin, Turmstr. 21, Building N, 10559, Berlin, Germany, takahito@m2.kufm.kagoshima-u.ac.jp.
- Forensic science, medicine, and pathology.Forensic Sci Med Pathol.2013 Jun;9(2):138-44. doi: 10.1007/s12024-012-9374-6. Epub 2012 Aug 28.
- For a better understanding of circumstantial and toxicological findings of fatalities resulting from self-administration of intravenous anesthetic/narcotic agents, medico-legal autopsy files of the State Institute of Legal and Social Medicine Berlin from 1998 to 2011 were reviewed retrospectively. O
- PMID 22926775
- The influence of propofol, remifentanil and lidocaine on the tone of human bronchial smooth muscle.
- Rogliani P, Calzetta L, Rendina EA, Massullo D, Dauri M, Rinaldi B, Capuano A, Matera MG.SourceDepartment of System Medicine, University of Rome "Tor Vergata", Rome, Italy.
- Pulmonary pharmacology & therapeutics.Pulm Pharmacol Ther.2013 Jun;26(3):325-31. doi: 10.1016/j.pupt.2013.01.002. Epub 2013 Jan 16.
- BACKGROUND: Bronchoscopy is generally a safe procedure, but the induction of anaesthesia can induce bronchospasm. Consequently we investigated the influence of propofol, remifentanil and lidocaine on the tone of the human bronchial smooth muscle.MATERIALS AND METHODS: The influence of propofol, remi
- PMID 23333814
Japanese Journal
- 症例 ディプリバンによる,冠動脈攣縮を伴った致死的アナフィラキシーショックの1例
- 内科 106(2), 371-374, 2010-08
- NAID 40017231942
- プロポフォールTCI投与による静脈内鎮静法導入時のリドカインによる血管痛軽減効果 : 0.5%, 1%および2%リドカインの比較
- 歯科薬物療法 28(2), 88-94, 2009-08-01
- NAID 10026406882
- プロポフォール(ディプリバン^【○!R】)
- 北海道歯学雑誌 18(1), 56-57, 1997-06-15
- NAID 10016277528
Related Links
- Learn about the prescription medication Diprivan (Propofol), drug uses, dosage, side effects, drug interactions, warnings, reviews and patient labeling. ... Strict aseptic technique must always be maintained during handling. Diprivan ...
- Diprivan - description, side Effects of Diprivan, dosage (Diprivan), proper use of Diprivan. Drugs review. ... The large contribution of distribution (about 50%) to the fall of propofol plasma levels following brief infusions means that after ...
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| 関連記事 | 「diprivan」 |
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特徴
構造
作用機序
薬理作用
- 鎮痛：× → 麻酔性鎮痛薬などと組み合わせて用いる。
- 意識消失：○
- 筋弛緩：△
- 反射抑制：○
効能又は効果
- 1%ディプリバン注
- 全身麻酔の導入及び維持
- 集中治療における人工呼吸中の鎮静
動態
- 1%ディプリバン注
- 1. 半減期は
- 日本人健康成人男子6例に1.0、2.0及び2.5mg/kgを単回静脈内ボーラス投与したとき、プロポフォールの体内動態は3-コンパートメントモデルに適合し、全血中濃度は3相性に減衰した。各相の半減期は2.6分(t1/2α)、51.0分(t1/2β)及び365分(t1/2γ)であった。中央コンパートメントにおける分布容積及び定常状態時の分布容積はそれぞれ26L及び317Lであった。全身クリアランス(CLTB)値は1.62L/分であった。1～2.5mg/kgの用量範囲で、血漿中薬物濃度－時間曲線下面積(AUC0-∞)が用量に比例して増加することが示された。また、薬物動態パラメータに明らかな性差はみられなかった（外国人の成績）。
- 2. 代謝及び排泄
- 成人患者8例に平均2.6mg/kgを単回静脈内ボーラス投与した場合、投与後24時間までにプロポフォール及び1,4キノール体のグルクロン酸抱合体ならびに1,4キノール体の硫酸抱合体として投与量の68.3%が尿中に排泄された。
- 3. 蛋白結合率6)
- 外国人患者にプロポフォールを2.5mg/kg用量で単回静脈内ボーラス投与したとき、投与後10及び120分後の蛋白結合率は約97～99%であった。
適応
注意
- 妊婦、授乳婦 → 母乳に移行する。ただし、その量は微々たるものらしい。しかし、できるだけ回避。
禁忌
- 1%ディプリバン注
- 1. 本剤又は本剤の成分に対し過敏症の既往歴のある患者
- 2. 妊産婦（「妊婦、産婦、授乳婦等への投与」の項参照）
- 3. 小児（集中治療における人工呼吸中の鎮静）
副作用
- 注射時の痛み、呼吸抑制、無呼吸、低血圧(麻酔導入時に起こる低血圧はバルビツレートに比べて高頻度に起こる)
- 徐脈-アシドーシス(プロポフォール注入症候群)：稀であるが致命的。
参考
- 1%ディプリバン注
「diprivan」
- 同
- Diprivan
- 関
- Propofol