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Pentazocine is a synthetically prepared prototypical mixed agonist–antagonist narcotic (opioid analgesic) drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain. Pentazocine is sold under several brand names, such as Fortral, Sosegon, Talwin NX (with the μ-antagonist naloxone, will cause withdrawal in opioid dependent persons on injection), Talwin, Talwin PX (without naloxone), Fortwin (Lactate injectable form) and Talacen (with acetaminophen). This compound may exist as one of two enantiomers, named (+)-pentazocine and (-)-pentazocine. (-)-pentazocine is a κ-opioid receptor agonist, while (+)-pentazocine is not, instead displaying a ten-fold greater affinity for the σ receptor. Talwin PX is the main pentazocine pharmaceutical in Canada, where laws and regulations prohibit the addition of naloxone to the formulation for non-therapeutic purposes.^{[citation needed]} Related drugs include phenazocine, dezocine, cyclazocine and several chemicals used in research on the central nervous system.

Therapeutic uses[edit]

Pentazocine is used to treat moderate to severe pain.

Administration[edit]

Pentazocine is administered by subcutaneous (rarely), intramuscular, and intravenous injection as the lactate.^[1] It is also available in 50 mg tablets with naloxone added.^[2] and also used in analgesic

Adverse effects[edit]

Side effects are similar to those of morphine, but pentazocine may be more likely to cause hallucinations and other psychotomimetic effects; cardiovascular effects make it unsuitable for use in myocardial infarction. Unlike morphine, its respiratory depressant action is subject to a "ceiling" effect. 30 milligrams of pentazocine has the same pain relieving capacity as 10 milligrams of morphine.^[1]

Tissue damage at injection sites[edit]

Severe injection site necrosis and sepsis has occurred (sometime requiring amputation of limb) with multiple injection of pentazocine lactate. In addition, animal studies have demonstrated that Pentazocine is tolerated less well subcutaneously than intramuscularly.^[1]

Illicit use[edit]

In the 1970s, recreational drug users discovered that combining pentazocine with tripelennamine (a first-generation ethylenediamine antihistamine most commonly dispensed under the brand names Pelamine and Pyribenzamine) produced a euphoric sensation. Since tripelennamine tablets are typically blue in color and brand-name Pentazocine is known as Talwin (hence "Ts"), the pentazocine/tripelennamine combination acquired the slang name Ts and blues. After health-care professionals and drug-enforcement officials became aware of this scenario, the mu-opioid-antagonist naloxone was added to oral preparations containing pentazocine to prevent injection misuse,^[2] and the reported incidence of its misuse has declined precipitously since.

Legal status[edit]

Pentazocine was originally classified in Schedule V under the Controlled Substances Act but a petition was filed with the D.E.A. on October 1, 1971, to shift it to Schedule III. The petition was filed by Joseph L. Fink III, a pharmacist and law student at Georgetown University Law Center as part of the course Lawyering in the Public Interest. That petition was accepted for review on November 10, 1971^[3] D.E.A. published a Final Rule transferring it to schedule IV on January 10, 1979, with an effective date of February 9, 1979^[4] This is understood to be the first instance of a successful petition to reclassify a substance under the relatively recently-enacted Controlled Substances Act. Pentazocine is still classified in Schedule IV under the Controlled Substances Act in the United States, even with the addition of Naloxone. although some states classify it in Schedule III. Internationally, pentazocine is a Schedule III drug under the Convention on Psychotropic Substances.^[5]

History[edit]

Pentazocine was developed by the Sterling Drug Company, Sterling-Winthrop Research Institute, of Rensselaer, New York. It was approved by the Food and Drug Administration in June 1967 after being favorably reviewed following testing on 12,000 patients in the United States. The analgesic compound was first made at Sterling in 1958. U.S. testing was conducted between 1961 - 1967. By mid 1967 Pentazocine was already being sold in Mexico, England, and Argentina, under different trade names.^[6]

References[edit]

^ ^a ^b ^c "TALWIN (pentazocine lactate) injection, solution". DailyMed. National Institute of Health. Retrieved 2011-12-10.
^ ^a ^b "Pentazocine and Naloxone tablets". DailyMed. National Institute of Health. Retrieved 2011-12-10.
^ 36 Fed.Reg. 217
^ 44 Fed. Reg. 2169
^ "List of psychotropic substances under international control". Green List - Annex to the annual statistical report on psychotropic substances (form P) (23rd ed.). International Narcotics Control Board. August 2003.
^ Pain-Killing Drug Approved By F.D.A., New York Times, June 27, 1967, pg. 41.

External links[edit]

Eurekalert report on PNAS article

UpToDate Contents

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English Journal

The calcium-sensitive Sigma-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases.

Sánchez-Blázquez P1, Rodríguez-Muñoz M1, Herrero-Labrador R1, Burgueño J2, Zamanillo D2, Garzón J1.
The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP).Int J Neuropsychopharmacol.2014 Dec;17(12):1943-55. doi: 10.1017/S1461145714000029. Epub 2014 Jan 31.
Through the cannabinoid receptor 1 (CB1), the endocannabinoid system plays a physiological role in maintaining the activity of glutamate N-methyl-d-aspartate (NMDA) receptor within harmless limits. The influence of cannabinoids must be proportional to the stimulus in order to prevent NMDAR overactiv
PMID 24485144

Type of opioids injected: Does it matter? A multicentric cross-sectional study of people who inject drugs.

Ambekar A1, Rao R, Mishra AK, Agrawal A.
Drug and alcohol review.Drug Alcohol Rev.2014 Oct 10. doi: 10.1111/dar.12208. [Epub ahead of print]
INTRODUCTION AND AIMS: Injecting pharmaceutical opioids for non-medical purposes is a major concern globally. Though pharmaceutical opioids injection is reported in India, the exact proportion of people who inject drugs (PWID) using pharmaceutical opioids is unknown. The objectives of this study wer
PMID 25302827

Sigma-1 Receptor Stimulation Protects Retinal Ganglion Cells from Ischemia-Like Insult through the Activation of Extracellular-Signal-Regulated Kinases1/2.

Mueller BH 2nd1, Park Y2, Ma HY3, Dibas A2, Ellis DZ4, Clark AF5, Yorio T6.
Experimental eye research.Exp Eye Res.2014 Oct 8. pii: S0014-4835(14)00271-1. doi: 10.1016/j.exer.2014.10.007. [Epub ahead of print]
Sigma-1 receptor (σ-1) activation and mitogen-activated protein kinases (MAPKs) have been shown to protect retinal ganglion cells (RGCs) from cell death. The purpose of this study was to determine if σ-1 receptor stimulation with pentazocine could promote neuroprotection under conditions of an isc
PMID 25305575

Related Pictures

talwin Nx prescription drug /side effects ; pentazocine lactate; talwin › Medications › Talwin nx TALWIN 30 MG/ML VIAL Talwin Nx: Oral tablet oblong, green, imprinted with 395 50 0 .5 Talwin Nx: Oral tablet (0.5-50mg) talwin drug

★リンクテーブル★

リンク元

「ペンタゾシン」

Pentazocine
Systematic (IUPAC) name
	(2RS,6RS,11RS)-6,11-dimethyl-3-(3-methylbut-2-en-1-yl)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-8-ol; or; 2-dimethylallyl-5,9-dimethyl-2'-hydroxybenzomorphan
Clinical data
Pregnancy cat.	C/D (U.S.)
Legal status	Controlled (S8) (AU) Schedule IV (U.S.); III international
Routes	Oral, IV, IM
Pharmacokinetic data
Bioavailability	~20% orally
Metabolism	Hepatic
Half-life	2 to 3 hours
Excretion	Renal
Identifiers
CAS number	359-83-1
ATC code	N02AD01
PubChem	CID 441278
IUPHAR ligand	1606
DrugBank	DB00652
ChemSpider	390041
UNII	RP4A60D26L
KEGG	D00498
ChEMBL	CHEMBL560
Chemical data
Formula	C19H27NO
Mol. mass	285.424 g/mol
	SMILES Oc1ccc3c(c1)[C@]2([C@H]([C@H](N(CC2)C\C=C(/C)C)C3)C)C;
	InChI InChI=1S/C19H27NO/c1-13(2)7-9-20-10-8-19(4)14(3)18(20)11-15-5-6-16(21)12-17(15)19/h5-7,12,14,18,21H,8-11H2,1-4H3/t14-,18+,19+/m0/s1 ; Key:VOKSWYLNZZRQPF-GDIGMMSISA-N ;
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　　[★]

英: pentazocine
ラ: pentazocinum
化: 塩酸ペンタゾシン pentazocine hydrochloride
商: ソセゴン Sosegon(アステラス)、ペンタジン Pentagin(第一三共)、ペルタゾン、Talwin
関: 全身麻酔薬、拮抗性麻酔薬

全身麻酔薬

拮抗性麻酔薬

作用機序

μ受容体に対する部分作動薬、κ受容体の全てに対する作動薬であり、κ受容体を通じて麻酔作用を示す。

利点

胆道閉塞性疾患にも慎重に使用できる(ブプレノルフィンは慎重投与だがペンタゾシンの大量投与は慎重) μ2受容体がOddi筋収縮に関わるとされている。

[mono-1] "TALWIN (pentazocine lactate) injection, solution". DailyMed. National Institute of Health. Retrieved 2011-12-10.

[monotabsnalox-2] "Pentazocine and Naloxone tablets". DailyMed. National Institute of Health. Retrieved 2011-12-10.

[3] 36 Fed.Reg. 217

[4] 44 Fed. Reg. 2169

[5] "List of psychotropic substances under international control". Green List - Annex to the annual statistical report on psychotropic substances (form P) (23rd ed.). International Narcotics Control Board. August 2003.

[talwin-6] Pain-Killing Drug Approved By F.D.A., New York Times, June 27, 1967, pg. 41.

匿名

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案内

案内

Talwin