Pentazocine

doi:10.1016/0376-8716(85)90064-X

Drug and Alcohol Dependence

Volume 14, Issues 3–4, February 1985, Pages 313-323

https://doi.org/10.1016/0376-8716(85)90064-X Get rights and content

Abstract

Published clinical studies and extensive experience has shown that pentazocine, the first of the practical agonist/antagonist analgesics, is a potent analgesic with wide application in clinical medicine. It has been shown to have a spectrum of pharmacological activity which has qualitative differences from pure opiate agonists and these have important implications in clinical medicine.

Pentazocine can provide analgesia as great as the opiates including morphine and meperidine, but does not have the same effect on mood. It is, therefore, less effective than the opiates in those situations where an anxiolytic effect is desired. Conversely, it produces less CNS depression in particular with regard to respiratory depression and nausea and vomiting. It also does not have the same potential for producing hypotension.

The parenteral administration of pentazocine produces rapid strong analgesia which is of less duration than with morphine or meperidine. The oral administration of pentazocine is less predictable with regard to response but in appropriate patients it is capable of providing a similar degree of analgesia to that achieved with parenteral pentazocine.

The dependence liability of pentazocine is substantially less than that with the opiates, and where abuse of parenteral pentazocine alone has taken place, it has usually been in medical and paramedical personnel seeking a support for inadequate personalities. Though physical and psychic dependence to parenteral pentazocine is undoubtedly possible, its incidence is extremely low with regard to the extent of the therapeutic use of pentazocine.

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Cited by (29)

Comparative study of dezocine, pentazocine and tapentadol on antinociception and physical dependence
2021, Life Sciences
Citation Excerpt :
To enhance analgesic activity, dezocine, a bridged aminotetralin analog chemically modified from pentazocine, was developed in 1970s and was approved for the treatment of postoperative pain in 1990 although withdrawal from the US market since 2000 [12,23,24]. However, pentazocine and particularly dezocine (occupied more than 45% of China's opioid analgesics market) have been widely used in China to treat moderate to postoperative pain, probably due to better tolerability than conventional opioids regarding gastrointestinal tract effects, respiratory depression, analgesic tolerance and physical dependence [12,25–29]. In addition, dezocine and pentazocine attenuated morphine-induced dependence-related withdrawal and conditioned place preference and morphine analgesic tolerance [30,31].
Dezocine and pentazocine, widely prescribed in China for postoperative pain, were initially considered as mixed agonist/antagonist targeting μ-opioid receptors (MORs) and κ-opioid receptors (KORs). However, dezocine has been revealed to alleviate chronic neuropathic pain through MOR activation and norepinephrine reuptake inhibition (NRI). This study investigated dezocine- and pentazocine-induced antinociception and physical dependence development, compared to the typical MOR-NRI opioid tapentadol.
Calcium mobilization assay was conducted to assess the potency of the drugs while hot-plate test was performed to compare the antinociception. Physical dependence development was compared with morphine.
Treatment with dezocine, pentazocine and tapentadol stimulated calcium mobilization in HEK293 cells stably expressed MORs but not KORs, whereas dezocine and pentazocine inhibited KOR activities. Subcutaneously injected dezocine-, tapentadol- and pentazocine-induced antinociception dose-dependently, in hot-plate test. Intrathecally injected MOR antagonist CTAP, norepinephrine depletor 6-OHDA and α₂-adrenoceptor (α₂-AR) antagonist yohimbine partially antagonized dezocine, pentazocine and tapentadol antinociception. Whereas specific KOR antagonist GNTI did not alter their antinociception, the putative inverse KOR agonist nor-BNI reduced dezocine and pentazocine antinociception. Moreover, combined CTAP and 6-OHDA or yohimbine blocked dezocine and tapentadol antinociception but displayed the same partial inhibition on pentazocine antinociception as CTAP alone. Furthermore, compared to morphine and pentazocine, long-term treatment with dezocine and tapentadol produced much less physical dependence-related withdrawal signs, which were restored by spinal 6-OHDA or yohimbine treatment.
Our findings illustrated that dezocine and tapentadol, but not pentazocine, exert remarkable antinociception in nociceptive pain with less abuse liability via dual mechanisms of MOR activation and NRI.
A comprehensive review of partial opioid agonists for the treatment of chronic pain
2020, Best Practice and Research: Clinical Anaesthesiology
Citation Excerpt :
While there has not been sufficient data showing intranasal butorphanol's effects on chronic pain, it should be noted that given its μ-antogonism butorphanol is very useful in preventing and aborting the dry cough associated with μ-agonist opioid use [81]. Pentazocine, another of the mixed partial agonists, was discovered in 1962 and is not a commonly used medication today [82]. It weakly partially agonizes the μ-receptor while fully agonizing the κ-receptor, a unique combination not seen in other drugs [82,83].
Chronic pain is a common condition that is being increasingly recognized, diagnosed, and treated in a variety of settings. Opioids can be used to treat chronic pain but at the cost of adverse effects and risk of dependence. Recently, there has been a movement to improve analgesic care in the setting of the opioid epidemic and the overprescribing of opioids, causing over-accessibility, dependence, and large numbers of overdose deaths. Opioid-specific receptors, including the μ, δ, κ, and opioid receptor like-1 (ORL-1) receptors, are each 7-transmembrane spanning proteins, which affect the G-protein and β-arrestin cascades. Each opioid class can act differently on the receptors, resulting in full, partial, or antagonizing effects. This comprehensive review looks at different agents in major classes, nonselective and mixed/partial agonists/antagonists, including the nonselective partial agonists, levorphanol and tramadol. Mixed partial agonists/antagonists include buprenorphine, pentazocine, nalbuphine, and butorphanol. Oliceridine is the only current selective partial agonist that agonizes specific pathways to promote analgesic effects and discourage adverse effects.
Prescription Opioids: An Overview
2020, Fighting the Opioid Epidemic: The Role of Providers and the Clinical Laboratory in Understanding Who is Vulnerable
Over 100 million Americans suffer from chronic pain. Therefore, proper pain management is essential for well-being of these patients. Morphine and codeine are natural alkaloids present in opium. In addition to morphine and codeine, many semisynthetic opiates such as oxycodone, oxymorphone, nalbuphine, naloxone, naltrexone, and buprenorphine are synthesized from thebaine, a naturally occurring alkaloid present in opium. In addition, synthetic opioids, such as fentanyl, alfentanil, sufentanil, remifentanil, meperidine, methadone, levorphanol, pentazocine tramadol, and tapentadol, are routinely used in pain management patients. Unlike semisynthetic opioids that have structural similarity with morphine, synthetic opioid are not structurally related to morphine, but similar to morphine, synthetic opioids also interact with opioid receptors for their pharmacological action. In order to combat opioid misuse and abuse, pharmaceutic companies more recently have introduced abuse-deterrent formulations of opioids. Various approaches, such as physical/chemical barrier, formulating with opioid receptor antagonists such as naloxone or naltrexone, using an aversion agent to deter abuse, prodrug formulation, or subcutaneous delivery of opioid, have been utilized to marker abuse-deterrent opioid formulations.
Pentazocine use among people who inject drugs in India
2015, Asian Journal of Psychiatry
Citation Excerpt :
In India, however, the data are scarce and available reports suggest that the parenteral form is procured and used by the people who use drugs (Bhalla et al., 2006; Grover et al., 2005). Pharmacological studies worldwide have suggested the subjective effects of Pentazocine to be mildly euphoric or even dysphoric at times (Goldstein, 1985; Preston and Bigelow, 1993; Walker et al., 2001; Zacny et al., 1998). Considering its lesser potential to produce euphoric effect and the likelihood to induce dysphoric effects, the phenomena of its use needs further evaluation.
Data regarding prevalence of Pentazocine use is sparse and intervention strategies aimed at it are meager. In view of the fact that Pentazocine has significant abuse potential contrary to what was earlier thought, along with the actuality that people who use injectable Pentazocine are at risk of various complications as HIV, this domain needs more attention. This review examines the extent of the problem of Pentazocine use with consequent effects on the overall health of the people. It is based on nationally representative large scale survey(s) and other reliable documented data on Pentazocine abuse. Possible strategies and future lines of actions have been delineated. Data suggests Pentazocine use from 0.1% to 21.8% in different parts of the country. Various reports have also linked it with unique health complications. Its use has been reported mostly among subjects seeking treatment, with recent reports suggesting increasing use at street level. The strategies to document the extent of injection drug use applied in most cases might not be adequate. There is a need for further research and monitoring to document the burden of the problem. Indirect methods to estimate the extent of problem may need to be implemented and regulatory mechanisms for prescription drug use may need to be strengthened.
High-dose pentazocine antagonizes the antinociception induced by high-dose morphine
2015, Life Sciences
Citation Excerpt :
In clinical trials, pentazocine has been shown to relieve moderate to severe pain [17]. It is characterized by strong analgesia potency and fewer adverse effects, including respiratory depression, nausea, hypotension and addiction potential, than morphine [11]. However, pentazocine often demonstrates an upper limit to the analgesic effects in clinical trials and animal experiments.
To investigate the effects of high doses of pentazocine on antinociception induced by a high dose of morphine and the role of the kappa-opioid receptors (KORs) in these effects in mice.
Sixty-six C57BL/6J mice were pretreated with a KOR antagonist, nor-binaltorphimine (nor-BNI) (10 mg·kg^− 1), or a normal saline placebo. All the mice received a subcutaneous injection of morphine (10 mg·kg^− 1) 120 min later and different doses of pentazocine (3, 10, 30, 56, 100 mg·kg^− 1) or a normal saline placebo. A tail pressure test, hot plate test and tail flick test were performed before and at 30, 60, 90 and 120 min after the injection of morphine.
The tail pressure test, hot plate test and tail flick test showed that pentazocine at doses of 10 to 100 mg·kg^− 1, but not at 3 mg·kg^− 1, had significant antagonizing effects on the antinociception induced by high-dose morphine to mechanical and thermal pain, and nor-BNI did not affect antinociception in combination with pentazocine at 10 to 100 mg·kg^− 1 and morphine at 10 mg·kg^− 1.
High-doses of pentazocine antagonize the antinociception induced by a high-dose of morphine in a dose-dependent manner, and this antagonistic effect is not associated with the activation of KORs.
Gender Differences in Analgesia for Endodontic Pain
2008, Journal of Endodontics
The purpose of this prospective clinical trial was to investigate the analgesic efficacy of three oral medication groups on postoperative endodontic pain in male and female dental patients, with an emphasis on analgesic differences between the sexes. Forty-three patients were administered ibuprofen 600 mg, placebo, or pentazocine 50 mg/0.5 mg naloxone in a randomized, double-blinded manner. Beginning immediately after endodontic treatment, patients took the assigned medication every 6 hours for 24 hours and recorded their degree of discomfort on a 100-mm visual analog scale. Statistical analysis of the data showed that ibuprofen 600 mg provided statistically significantly greater analgesia than placebo at 6 and 12 hours (P = 0.0014 and 0.0024), and pentazocine/naloxone provided statistically significantly greater analgesia than placebo at 12 hours (P = 0.0084). Sex-dependent differences were noted within the pentazocine/naloxone group, which showed significantly greater analgesia in females compared with males (P = 0.007).

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Review of individual compoundPentazocine

Abstract

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Review of individual compound
Pentazocine