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a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/11/07 23:21:53」(JST)

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Remifentanil (marketed by GlaxoSmithKline and Abbott as Ultiva) is a potent ultra short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is used for sedation as well as combined with other medications for use in general anesthesia. The use of remifentanil has made possible the use of high-dose opioid and low-dose hypnotic anesthesia, due to synergism between remifentanil and various hypnotic drugs and volatile anesthetics.

Administration[edit]

It is administered in the form remifentanil hydrochloride and in adults is given as an intravenous infusion in doses ranging from 0.1 microgram per kilogram per minute to 0.5 (µg/kg)/min. Children may require higher infusion rates (up to 1.0 (µg/kg)/min).^[1] Doses listed in the package insert from its manufacturer are much higher than those used in actual clinical practice. The clinically useful infusion rates are 0.025-0.1 (µg/kg)/min for sedation (rates adjusted to age of patient, severity of their illness and invasiveness of surgical procedure). Small amounts of other sedative medications are usually co-administered with remifentanil to produce sedation. Clinically useful infusion rates in general anesthesia vary but are usually 0.1-1 µg/kg/min[1].

Remifentanil can be administered as part of an anaesthesia technique called TIVA (Total Intravenous Anaesthesia) using computer controlled infusion pumps in a process called target controlled infusion or TCI. A target plasma concentration is entered as ng/ml into the pump, which calculates its infusion rate according to patient factors like age and weight. Induction levels of 4 ng/ml are commonly used, but it generally varies between 3-8 ng/ml. For certain surgical procedures that produce particularly strong stimuli a level of up to 15 ng/ml might be needed. The relatively short context-sensitive half-life of Remifentanil allows the desired blood plasma level to be achieved quickly and also for the same reason recovery occurs quickly.

Metabolism[edit]

Unlike other synthetic opioids which are hepatically metabolised, remifentanil has an ester linkage which undergoes rapid hydrolysis by non-specific tissue and plasma esterases. This means that accumulation does not occur with remifentanil and its context-sensitive half-life remains at 4 minutes after a 4 hour infusion.

Remifentanil is metabolized to a compound (remifentanil acid) which has 1/4600th the potency of the parent compound.^[2]

Owing to its quick metabolism and short effects remifentanil has opened up new possibilities in anesthesia. When remifentanil is used together with a hypnotic (i.e. one that produces sleep) it can be used in relative high doses. This is because remifentanil will be rapidly eliminated from the blood plasma on termination of the remifentanil infusion, hence the effects of the drug will quickly dissipate even after very long infusions. Owing to synergism between remifentanil and hypnotic drugs (such as propofol) the dose of the hypnotic can be substantially reduced.^[3] This leads often to more haemodynamic stability during surgery and a quicker post-operative recovery time.

Side-effects[edit]

Remifentanil is a specific μ-receptor agonist.^[3] Hence, it causes a reduction in sympathetic nervous system tone, respiratory depression and analgesia. The drug's effects include a dose-dependent decrease in heart rate and arterial pressure and respiratory rate and tidal volume. Muscle rigidity is sometimes noted.

The most common side effects reported by patients receiving this medication are a sense of extreme "dizziness" (often short lived, a common side effect of other fast-acting synthetic phenylpiperidine narcotics such as fentanyl and alfentanil) and intense itching (pruritus), often around the face. These side effects are often controlled by either altering the administered dose (decreasing or in some cases, increasing the dose) or by administering other sedatives that allow the patient to tolerate or lose awareness of the side effect.

Because pruritus is due to excessive serum histamine levels, antihistamines such as diphenhydramine (Benadryl) are often co-administered. This is done with care, however, as excessive sedation may occur.

Nausea can occur as a side effect of remifentanil, however, it is usually transient in nature due to the drug's short half-life which rapidly removes it from the patient's circulation once the infusion is terminated.

Potency[edit]

Remifentanil is approximately twice as potent as fentanyl, and 100-200 times as potent as morphine.

Circumventing Naltrexone[edit]

Remifentanil has been used with some success to circumvent naltrexone in patients who are in need of pain management.

Regulation[edit]

In Hong Kong, Remifentanil is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. It can only be used legally by health professionals and for university research purposes. The substance can be given by pharmacists under a prescription. Anyone who supplies the substance without prescription can be fined $10000 (HKD). The penalty for trafficking or manufacturing the substance is a $5,000,000 (HKD) fine and life imprisonment. Possession of the substance for consumption without license from the Department of Health is illegal with a $1,000,000 (HKD) fine and/or 7 years of jail time.

Regulation in the US is as a schedule II narcotic.

References[edit]

^ Weale NK, Rogers CA, Cooper R, Nolan J, Wolf AR (February 2004). "Effect of remifentanil infusion rate on stress response to the pre-bypass phase of paediatric cardiac surgery". Br J Anaesth 92 (2): 187–94. doi:10.1093/bja/aeh038. PMID 14722167.
^ Hoke JF, Cunningham F, James MK, Muir KT, Hoffman WE (April 1997). "Comparative pharmacokinetics and pharmacodynamics of remifentanil, its principle metabolite (GR90291) and alfentanil in dogs". J. Pharmacol. Exp. Ther. 281 (1): 226–32. PMID 9103501.
^ ^a ^b Patel SS, Spencer CM (Sep 1996). "Remifentanil". Drugs 52 (3): 417–27. doi:10.2165/00003495-199652030-00009. PMID 8875131.

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1. 周術期に成人に静脈内投与するオピオイド鎮痛薬 perioperative uses of intravenous opioids in adults
2. 眼の緊急手術に対する麻酔 anesthesia for emergent eye surgery
3. 麻酔における迅速気管導入・挿管法（RSII） rapid sequence induction and intubation rsii for anesthesia
4. 危篤状態の成人患者における疼痛管理 pain control in the critically ill adult patient
5. 全身麻酔：維持と覚醒 general anesthesia maintenance and emergence

English Journal

Intranasally Administered Adjunctive Dexmedetomidine Reduces Perioperative Anesthetic Requirements in General Anesthesia.

Wu X1, Hang LH2, Wang H2, Shao DH2, Xu YG1, Cui W1, Chen Z3.
Yonsei medical journal.Yonsei Med J.2016 Jul;57(4):998-1005. doi: 10.3349/ymj.2016.57.4.998.
PURPOSE: Intranasal dexmedetomidine is an effective sedative for premedication and is regularly used to reduce preoperative tension and anxiety in children. This study aimed to assess the effect of intranasally adjunctive dexmedetomidine on perioperative sedative and analgesic requirements in adults
PMID 27189297

Comparison of Dexmedetomidine and Remifentanil on Airway Reflex and Hemodynamic Changes during Recovery after Craniotomy.

Kim H1, Min KT2,3, Lee JR2,3, Ha SH2, Lee WK2, Seo JH2, Choi SH2,4.
Yonsei medical journal.Yonsei Med J.2016 Jul;57(4):980-6. doi: 10.3349/ymj.2016.57.4.980.
PURPOSE: During emergence from anesthesia for a craniotomy, maintenance of hemodynamic stability and prompt evaluation of neurological status is mandatory. The aim of this prospective, randomized, double-blind study was to compare the effects of dexmedetomidine and remifentanil on airway reflex and
PMID 27189295

Inhaled Remifentanil in Rodents.

Bevans T1, Deering-Rice C, Stockmann C, Light A, Reilly C, Sakata DJ.
Anesthesia and analgesia.Anesth Analg.2016 Jun;122(6):1831-8. doi: 10.1213/ANE.0000000000001228.
BACKGROUND: Remifentanil is an injectable opioid that is metabolized rapidly at a constant rate by plasma esterases. This supports its use as an analgesic for short-term, but painful, procedures in a wide range of patients. The aim of this study was to explore the feasibility and safety of administe
PMID 26974021

Japanese Journal

目の前で起こった不整脈への対応 : 頻拍症に対するβブロッカーの使用

日本臨床麻酔学会誌 = The Journal of Japan Society for Clinical Anesthesia 30(5), 779-784, 2010-09-15
NAID 10026629783

アルチバ^【○!R】(レミフェンタニル塩酸塩)静注用2mg・5mgの薬理学的特徴および臨床試験成績

日本薬理学雑誌 : FOLIA PHARMACOLOGICA JAPONICA 130(4), 321-329, 2007-10-01
NAID 10020167614

NEW DRUGS レミフェンタニル塩酸塩

クリニカルプラクティス 26(7), 568-570, 2007-07
NAID 40015553451

「レミフェンタニル」

Remifentanil
Systematic (IUPAC) name
	methyl 1-(3-methoxy-3-oxopropyl)-4-(N-phenylpropanamido)piperidine-4-carboxylate
Clinical data
AHFS/Drugs.com	monograph
Pregnancy cat.	?
Legal status	Controlled (S8) (AU) Class A (UK) Schedule II (US)
Routes	Intravenous
Pharmacokinetic data
Bioavailability	Not applicable (intravenous administration)
Protein binding	70% (bound to plasma proteins)
Metabolism	cleaved by non-specific plasma and tissue esterases
Half-life	1-20 minutes
Identifiers
CAS number	132875-61-7
ATC code	N01AH06
PubChem	CID 60815
DrugBank	DB00899
ChemSpider	54803
UNII	P10582JYYK
KEGG	D08473 Ramelteon
ChEBI	CHEBI:8802
ChEMBL	CHEMBL1005
Synonyms	methyl 1-(2-methoxycarbonylethyl)-4-(phenyl-propanoyl-amino)-piperidine-4-carboxylate
Chemical data
Formula	C20H28N2O5
Mol. mass	376.447 g/mol
	SMILES O=C(OC)C2(N(c1ccccc1)C(=O)CC)CCN(CCC(=O)OC)CC2;
	InChI InChI=1S/C20H28N2O5/c1-4-17(23)22(16-8-6-5-7-9-16)20(19(25)27-3)11-14-21(15-12-20)13-10-18(24)26-2/h5-9H,4,10-15H2,1-3H3 ; Key:ZTVQQQVZCWLTDF-UHFFFAOYSA-N ;
Physical data
Melt. point	5 °C (41 °F)
(what is this?) (verify);

　　[★]

英: remifentanil
化: 塩酸レミフェンタニル remifentanil hydrochloride
商: アルチバ
関: 麻薬、麻酔薬、オピオイド、オピオイド受容体

合成麻薬

フェニルピペリジン構造(フェンタニル、アルフェンタニル、スフェンタニル、レミフェンタニル)

選択的μ受容体アゴニスト
脳内への移行が速やかなため、作用発現までの時間が短く、消失も早い。
投与中中止後、速やかに血中濃度が低下し、術後呼吸抑制の心配が少ない(SAN.55)
血中および組織内の非特異的エステラーゼによって加水分解されるため(腎・肝機能に非依存的)、蓄積性がなく、肝・腎機能障害を有している患者にも有効。

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[1] Weale NK, Rogers CA, Cooper R, Nolan J, Wolf AR (February 2004). "Effect of remifentanil infusion rate on stress response to the pre-bypass phase of paediatric cardiac surgery". Br J Anaesth 92 (2): 187–94. doi:10.1093/bja/aeh038. PMID 14722167.

[2] Hoke JF, Cunningham F, James MK, Muir KT, Hoffman WE (April 1997). "Comparative pharmacokinetics and pharmacodynamics of remifentanil, its principle metabolite (GR90291) and alfentanil in dogs". J. Pharmacol. Exp. Ther. 281 (1): 226–32. PMID 9103501.

[Patel-3] Patel SS, Spencer CM (Sep 1996). "Remifentanil". Drugs 52 (3): 417–27. doi:10.2165/00003495-199652030-00009. PMID 8875131.

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案内

案内

remifentanil hydrochloride