Injection Of Pentazocine Research Articles

Diagnostic clinical features of pentazocine‐induced ulcers

Pentazocine was introduced in 1967 as a "non-narcotic, nonaddicting" analgesic. However, the abuse potential of this medication was soon recognized, and cutaneous and muscular complications of pentazocine abuse have been reported. Demographic and clinical data on 10 patients with pentazocine-induced ulcers attending the Dermatology Outpatient Department of the All India Institute of Medical Sciences (AIIMS), New Delhi, India between November 2000 and October 2002 have been compiled. Ten patients with pentazocine-induced ulcers were seen at AIIMS between November 2000 and October 2002, six of whom were female. The average age of these patients was 32 years. The duration of the complaints ranged from 10 days to 7 years (average 17.5 months). Nine of the 10 patients had past history of painful medical conditions for which they had received pentazocine injections. All the patients presented with deep ulcers and sinuses over the accessible sites. The margins of these ulcers were hyperpigmented and indurated. Six patients had scars along the superficial vein access sites. Three patients had puffy-hand syndrome, while two had muscle contractures. No underlying psychiatric disorders were found in any of these patients. Urine screening for pentazocine was positive in two patients. Antinuclear antibody (ANA), antineutrophil cytoplasmic antibody (ANCA) and antibody against DNA (antidsDNA) tests and screening for infections such as human immunodeficiency virus (HIV), hepatitis B virus (HBV) and hepatitis C virus (HCV) were negative in all patients. Pentazocine abuse can be suspected from cutaneous findings, even when the patient does not volunteer a history of self-medication. Recognition of the condition will prevent misdirected investigations and treatment. The patient should be encouraged to seek treatment for drug dependence.

Cross-Sensitization Between Phencyclidine and (−) But Not (+)Pentazocine

Repeated administration of psychomotor stimulants such as amphetamine and cocaine, and psychotomimetics such as phencyclidine, produce progressively enhanced behavioral effects, a phenomenon known as behavioral sensitization. Little is known about the effects of repeated treatment with sigma ligands on locomotor activity. The present research determined the psychomotor stimulant effects of the sigma ligand (+)pentazocine and its enantiomer; and investigated whether reciprocal cross-sensitization occurs between them and PCP-induced locomotor activity and ambulation. Adult female Sprague–Dawley rats were used. Total locomotor activity and ambulation were assessed with an automated photoelectric system. Acute (+) or (−)pentazocine given IP produced slight but insignificant locomotor stimulant effects. Repeated administration of (+)pentazocine failed to produce behavioral sensitization. However, four repeated injections of (−)pentazocine or PCP produced behavioral sensitization. (−)Pentazocine sensitized rats showed cross-sensitization to PCP-induced locomotion and ambulation. Furthermore, PCP sensitized rats showed cross-sensitization to (−)pentazocine-induced locomotion and ambulation. These findings suggest that (+) and (−)pentazocine act at different receptor sites. (−)Pentazocine is more similar to PCP in producing locomotor stimulant effects.

Focal myopathy induced by chronic intramuscular heroin injection

A patient developed focal fibrotic myopathy after many years of intramuscular heroin use. While such changes have been associated with chronic intramuscular injections of pentazocine and meperidine, a similar myopathy resulting from chronic intramuscular heroin has not been convincingly described.

Acute Myocardial Infarction Associated with Intravenous Injection of Pentazocine and Tripelennamine

This case report describes the evolution of an acute anteroseptal myocardial infarction in a 27-year-old man following intravenous injection of pentazocine and tripelennamine. Subsequent coronary angiography showed normal coronary arteries. Based on the known mechanism of action of these drugs, it is postulated that myocardial infarction resulted from coronary artery spasm secondary to excessive catecholamine stimulation.

Involvement of �-opioid receptors in the antitussive effects of pentazocine

The effect of pentazocine on the capsaicin-induced cough reflex in rats was investigated. Intraperitoneal injection of pentazocine, in doses from 1 to 10 mg/kg, significantly decreased the number of coughs in a dose-dependent manner. The antitussive effect of pentazocine (10 mg/kg, i.p.) was significantly reduced by prior injection of naloxone (0.3 mg/kg, i.p.), but it was unaffected by Mr-2266 BS (5 mg/kg, i.p.), an antagonist of kappa-opioid receptors. The antinociceptive potency of pentazocine (30 mg/kg, i.p.), as determined by the formalin test, was significantly reduced by pretreatment with Mr-2266 BS (5 mg/kg, i.p.), whereas naloxone (0.3 mg/kg, i.p.) had no significant effect on the antinociceptive effect of pentazocine. The antitussive effects of pentazocine (3 mg/kg) and morphine (0.1 mg/kg) were significantly enhanced in rats treated chronically with naloxone (5 mg/kg/day, 5 days), whereas the antitussive effect of U-50,488 H (1 mg/kg, i.p.), a selective kappa-opioid agonist, was not enhanced in these rats. By contrast, the antinociceptive effect of morphine (0.01 mg/kg, i.p.) was significantly enhanced in rats that had been pretreated chronically with naloxone. However, the antinociceptive effects induced by pentazocine (3 mg/kg, i.p.) and U-50,488 H (1 mg/kg, i.p.) were unchanged. These results suggest that pentazocine-induced antitussive effects in rats are mediated via stimulation of mu-opioid receptors.

Neurophysiologic and Histologic Changes Following Injection of Morphine , Meperidine and Pentazocine on Sciatic Nerve of Rabbits

Neurophysiologic and Histologic Changes Following Injection of Morphine , Meperidine and Pentazocine on Sciatic Nerve of Rabbits

Cyclosporine therapy for severe systemic sclerosis associated with the anti-Scl-70 autoantibody

delineated by Parks et a1.6 include (1) the tense, woody fibrosis; (2) irregularly shaped ulcers, some extending to expose muscle; (3) a halo of'hyperpigmentaion surrounding the ulcers; and (4) the apparent indifference of the patients toward the disfiguring process and their lack of expression of pain despite the degree of tissue destruction. Several reports have described the typical pentazocine abuser as middle-aged, college-educated, married, and associated with the health professions. Often there is a history of alcohol or drug abuse or psychiatric illness.Patients with a personal or family history of diabetes may also be at special risk for cutaneous complications' The exact mechanism by which injection of pentazocine induces cutaneous and muscle changes is unknown. There is histologic evidence of vascular thrombosis with dermal and epidermal infarction. Other authors'' postulate that precipitation of pentazocine in tissue incites an inflammatory response.

Discriminative stimulus effects of enkephalin analogs, EK-209 and EK-399, in rats

The discriminative stimulus effects of two enkephalin analogs, Tyr-D-Ala-Gly-MePhe-NHNHCOCH 2CH 3·AcOH (EK-209) and Tyr-D-Met(O)-Gly-EtPhe-NHNHCOCH 3·AcOH (EK-399), were assessed in a drug discrimination experiment with rats. The animals were trained to discriminate between the effect of morphine (3 mg/kg s.c.) and saline in a two-lever choice, water reinforced procudure. After the discrimination training had been completed, the animals were used in stimulus generalization tests. A test drug was administered subcutaneously before the test session, and the animals were allowed to select the morphine or saline lever. The animals completely generalized to the effect of codeine, fentanyl and EK-209, but did not generalize completely to the effect of ethylketocyclazocine. After receiving an injection of pentazocine, levallorphan, N-allylnormetazocine, or EK-399, the animals pressed the morphine lever, but did not generalize completely to the effects of these drugs. These results suggest that the discriminative stimulus effect of EK-209 is similar to that of morphine, whereas the effect of EK-399 may be different from that of morphine.

Blockade of dopamine D 1 receptors by SCH 23390 antagonizes discriminative stimulus effects of pentazocine

The purpose of this investigation was to test the hypothesis that the discriminative stimulus properties of pentazocine are mediated through an interaction with dopamine receptors. Rats were trained to discriminate s.c. injections of pentazocine (3.0 mg/kg) from vehicle in a two-choice discrete trial avoidance paradigm. SCH 23390 (0.003–0.056 mg/kg), a selective antagonist of dopamine D 1 receptors, inhibited the discriminative stimulus effects of pentazocine in a dose-dependent fashion, whilst the selective D 2 receptor antagonist sulpiride (20.0–80.0 mg/kg) did not antagonize them. It appears that the dopamine D 1 receptors play an important role in the discriminative stimulus effects of pentazocine.

Analgésie postopératoire : injection péridurale de phosphate sodique de dexaméthasone

Epidural administration of steroids has been suggested for the prevention of postoperative epidural fibrosis after lumbar lamino-arthrectomy. In order to assess the efficacy of this technique on pain occurring after such surgery, the demand of pentazocine during the first 24 postoperative hours was studied in 39 patients randomly assigned to two groups. Pain intensity was assessed by a five-point verbal scale (0 : none ; 1 : poor ; 2 : moderate ; 3 : severe ; 4 : very severe) at five intervals (0–4, 5–8, 9–12, 13–16 and 17–24 h). The patients in group T (n = 20) did not receive any steroid, whereas those in group C (n = 19) were given, just after the end of surgery, a single dose of dexamethasone (4 mg) via an epidural lumbar catheter previously inserted by the surgeon. In group T, 18 patients required one or several intramuscular injections of pentazocine, whereas only three patients of group C (p < 0.001) did so. Patients in group T expressed more severe pain (4 moderate, 12 severe, 3 unbearable) than those patients who had received steroids (1 moderate, 1 severe, 1 unbearable). As a consequence, they requested more pain killer (30 injections vs 8 injections, respectively ; p < 0.001) and sooner than patients of the steroid group (8 h vs 12 h ; p < 0.05). It was concluded that epidural administration of dexamethasone was helpful in preventing postoperative pain after lumbar lamino-arthrectomy.

Ganglioside composition of liver and kidney from rat after pentazocine treatment

1. 1. Female non-pregnant rats were intramuscularly injected with pentazocine for 3 months. Liver showed a statistically significant ( P < 0.05) increase in its ganglioside content after the pentazocine treatment; in addition, no changes were found in the kidney ganglioside content. 2. 2. We have also found changes in the ganglioside pattern of these rats after the pentazocine injection. The GM 1 and GD 1b liver content was decreased ( P < 0.05) in parallel with an increase ( P < 0.05) in GD 3 and GT 1b content; kidney showed a decrease ( P < 0.05) in GM 1, GD 1a and GD 1b content and an increase ( P < 0.05) in GM 4, GD 2, GT 1b and GQ content. 3. 3. Female pregnant rats were also injected with pentazocine from the first to the nineteenth day of the gestation period. The total ganglioside content of liver and kidneys from mothers and their newborns did not show statistically significant differences after the treatment. 4. 4. Mothers showed a decrease ( P < 0.05) in the GM 1 content of liver and an increase ( P < 0.05) in the GT 1b content of liver and GM 1, GD 3 and GD 1a content of kidney. Only the GM 3 content from kidney was increased ( P < 0.001). 5. 5. Newborns showed minor changes in their ganglioside pattern. GT 1b content from liver and GD 2 and GQ content from kidneys were decreased ( P < 0.05).

Effect of modern analgesic drugs (tramadol, pentazocine, and buprenorphine) on the bile duct sphincter in man.

Modern narcotic analgesic drugs, such as tramadol, pentazocine, and buprenorphine share similarities of molecular structure with morphine which is widely believed to cause spasm of the bile duct sphincter and so impede bile flow. This study assessed the effects of intravenously administered analgesics on bile duct sphincter motor activity measured by ERCP manometry. Ten minutes after pentazocine injection the duration of contractions and baseline pressure of the bile duct sphincter rose from 6.2 +/- 0.2 to 8.2 +/- 0.27 s and from 5.1 +/- 0.6 to 8.8 +/- 0.4 mmHg respectively. Tramadol, buprenorphine and saline showed no such effect. These data indicated that the effects of such drugs on bile duct sphincter function can be safely assessed by ERCP manometry and that pentazocine adversely affects the bile duct sphincter, whilst tramadol and buprenorphine do not. We consider therefore that pentazocine is not the premedication of first choice for endoscopic procedures involving the sphincter of Oddi and should also be avoided in patients with pancreatic and biliary disorders.

Comparison of the ability of opioid analgesics to increase endogenous opioid-like activity in the cerebrospinal fluid of rabbits

We have previously demonstrated that the acute administration of morphine increases the level of endogenous substances, which have antinociceptive activity, in cerebrospinal fluid (CSF). The present study was conducted to determine whether other opioid analgesics exert a similar effect. CSF was withdrawn from the cisterna magna of anesthetized rabbits before and after s.c. injections of meperidine, pentazocine, levorphanol and methadone, and was bioassayed for opioid-like activity in the mouse tail-flick and phenylquinone writhing tests. The opioid-like activity of CSF taken 60 min after meperidine (50 mg/kg) was significantly increased in both bioassays, and the CSF level of meperidine was insufficient to account for this effect. Pentazocine (25–75 mg/kg) also significantly increased opioid-like activity in rabbit CSF, but the effects of methadone (5–10 mg/kg) and levorphanol (20 mg/kg) were less marked. Dextrorphan (20 mg/kg), diazepam (10 mg/kg) and pentobarbital (20 mg/kg) administration did not significantly increase opioid-like activity in CSF. It is concluded that the antinociceptive action of some opioid analgesics in rabbits may be mediated in part by the release of endogenous antino-ciceptive substances.

Pharmacokinetic studies of the inhibition of glucuronization of pentazocine by salicylamide.

The serum concentrations of unchanged and glucuronized drug were determined after intravenous injection of pentazocine (PA) in rabbits. A compartment model isolating the liver from the central compartment was proposed to explain the observed time courses of the concentration, and the resulting convolution equation was M (t)=∫10D (t-θ) G (θ) dθ, where M (t) and D (t) are the serum concentrations of glucuronized PA and unchanged PA after intravenous injection, respectively. The weight function, G (t), which represents the response for a pulse input of glucuronized PA was estimated to be G (t)=0.00933 (e-0.00818t-e-0.223t) (min-1). The simultaneous intravenous administration of salicylamide (SAM) had no effect on the glucuronization of PA in serum. The serum concentration of glucuronized PA calculated by numerical convolution of G (t) and the published serum concentration of unchanged PA after oral administration represents that of glucuronide produced from the unchanged PA which escaped the first-pass effect. This calculated value was far below the published serum concentration of glucuronized PA after oral administration, and the difference represents the glucuronized PA produced by the first-pass effect. The area under the concentration-versus-time curve of glucuronized PA produced by the first-pass effect was 274 times larger than that of glucuronized PA produced from unchanged PA in the serum. Simultaneous oral administration of SAM only inhibits the first-pass effect.

Studies on the excitatory and inhibitory influence of intracerebroventricularly injected opioids on seizure thresholds in rats

The influence of centrally administered meperidine, normeperidine and pentazocine on the excitability of brain was studied by measuring the threshold for flurothyl-induced convulsions in rats. All three opioids are reported to lower seizure thresholds when given subcutaneously to rats in this test. Dose- and time-dependent changes in the seizure threshold occured after intracerebroventricular injection of pentazocine (10–160 μg), meperidine (25–150 μg) and normeperidine (50–150 μg). Rapid increases in the seizure threshold were associated with pentazocine and meperidine, whereas a slowly developing decrease in the threshold was caused by normeperidine. Naloxone (10 mg/kg, s.c.) antagonized the anticonvulsant effect of meperidine (but not that of pentazocine) and enhanced the proconvulsant effect of normeperidine. Thebaine (25–150 μg), which had no marked influence on the seizure threshold when given intracerebroventricularly, lowered the threshold after subcutaneous injection of 12.5 and 25 mg/kg. This effect was not altered by injection of naloxone. These results show that centrally administered opioids can act on excitatory or inhibitory systems that regulate seizure mechanisms in the rat brain. Furthermore both naloxone-sensitive and naloxone-insensitive components are involved. Meperidine, pentazocine and thebaine have different actions on the seizure threshold after intracerebroventricular, as opposed to subcutaneous, administration. This work has, therefore, identified the route of administration as a critical variable in the effect of opioids on the seizure threshold in rats.

Depression by morphine and levorphanol of activity in sympathetic nerve fibres in anaesthetized rats

In urethane-anesthetized rats, the effects of intravenous injections of morphine, levorphanol, dextrorphan, pentazocine and naloxone were studied on the activity in nerve fibres of the cervical sympathetic trunk, and on mean arterial blood pressure and heart rate. Impulse frequency in sympathetic nerve fibres was recorded with tungsten microelectrodes and proved to be more sensitive to drug action than blood pressure or heart rate. Morphine 1 and 2 mg/kg dose dependently reduced sympathetic impulse frequency, blood pressure and heart rate; morphine 0.5 mg/kg was ineffective. Levorphanol 1 and 2 mg/kg dose dependently reduced sympathetic impulse frequency and blood pressure but did not affect heart rate. Dextrorphan (the dextro-isomer of levorphanol) 2 and 4 mg/kg had no effect on the parameters tested. Pentazocine 3 and 6 mg/kg did not cause a consistent change in sympathetic impulse frequency, blood pressure and heart rate. Naloxone 0.2 mg/kg abolished the depressant effects of morphine and levorphanol and, when given alone, increased sympathetic impulse frequency. Naloxone 1 mg/kg increased blood pressure but did not affect heart rate. It is concluded that morphine can reduce blood pressure and heart rate by causing opiate-specific central sympathetic depression.

Myofibrosis and joint contractures caused by injections of pentazocine. A case report.

Myofibrosis and joint contractures caused by injections of pentazocine. A case report.

A comparison of the sites at which pentazocine and morphine act to produce analgesia

Sites in the brain stem at which microinjected morphine can produce analgesia have been investigated for sensitivity to microinjections of pentazocine, which has been proposed to act at receptors different to those mediating the effects of morphine. Microinjection of 10 mgg of pentazocine into the periaqueductal grey matter (PAG), the nucleus reticularis gigantocellularis (NRGC) and nucleus reticularis paragigantocellularis (NRPG) produced analgesia as determined by the tail flick response to noxious heat. Microinjection of pentazocine into nucleus raphe magnus (NRM) did not produce any discernible change in the nociceptive threshold measured with the tail flick test. Using the pain pressure test, analgesia was observed following microinjections of pentazocine into NRGC and NRPG, but not following microinjections into PAG or NRM. Morphine (3 and 5 gmg) microinjected into PAG, NRM, NRGC or NRPG produced analgesia as determined by both heat and pressure tests. The analgesia produced by injection of pentazocine into the NRGC or NRPG was comparable to the analgesia produced by microinjection of 3 g mg of morphine into these areas. The analgesia produced by injection of pentazocine into PAG was significantly less than that produced by 3 gmg of morphine injected into PAG. Pretreatment with naloxone did not affect the analgesia produced by microinjection of pentazocine into NRGC or NRPG, but did antagonize the analgesia produced by injection of pentazocine into PAG. Naloxone blocked the analgesic effects of microinjected morphine. Analgesia produced by systemically given pentazocine was significantly reduced following microinjection of naloxone into PAG or NRM but not into NRGC or NRPG. The present data provide further evidence that the effects of pentazocine, a gk agonist drug may be mediated by mechanisms different to those mediating the action of morphine, a gm agonist.

Foreign body granulomatosis. Clinical and immunologic findings.

We studied the clinical and immunologic features of 10 patients with foreign body granulomatosis associated with injection of pentazocine. Five had typical micronodules on chest radiographs, 9 had abnormal 67Ga lung images, and 9 had elevated serum angiotensin-converting enzyme levels. Pulmonary function tests showed significant decreases in diffusing capacity in 8 subjects, but were otherwise normal. Bronchoalveolar lavage fluid had significantly (p less than 0.02) increased total cell numbers (13.8 +/- 7.5 x 10(7) and significantly lower percentages of lymphocytes (2 +/- 1) and neutrophils (2 +/- 1) (p less than 0.02) when compared with that from control subjects. Peripheral blood lymphocytes were normal when expressed as percentages of total leukocytes or as percent T-lymphocytes. Monoclonal antibody determinations of T-lymphocyte subsets (helper and suppressor) were similar to those in control subjects (p = NS). Lymphocyte transformation responses to a variety of antigens and skin test reactivity were normal. Foreign body granulomatosis contrasts with other interstitial lung diseases in its bronchoalveolar lavage cellular profile and in the absence of altered peripheral immunologic indexes.

Depression of learned thermoregulatory behavior by central injection of opioids in cats

Third cerebral ventricular administration of morphine (20 μg), pentozocine (1 mg) or the synthetic opioid peptides d-Ala 2-Met-enkephalinamide (25 μg) and d-Ala 2- d-Leu 5 -enkephalin (10 μg) decreased heat-reinforcement activity and either reduced or did not increase heat-escape activity of cats trained to control thermal stimuli through behavior. If the behavioral changes had been coupled to the primary effects of these opioids on thermoregulation, one would have expected an inverse relationship between changes in heat-reinforcement and heat-excape activity. Motor incapacitation appeared not to have contributed to the reduction in responding except briefly after pentazocine injection. The opioids may have distracted the animals or otherwise reduced their reaction to thermal stimuli until body temperature increased to a potentially dangerous level.