Introduction: Opioid dependence is recorded as the most common drug of abuse in Malaysia. Currently, the preferred substitution therapy for most Government treatment centres is methadone used as substitution therapy for opioid dependence. There are, however patients who may benefit from being on the combined buprenorphine-naloxone formulation as substitution therapy instead. We discuss six cases of opioid dependence of varied backgrounds that were treated with buprenorphinenaloxone therapy and their outcomes. Discussion: All of the reported patients improved after the induction of buprenorphine- naloxone. Two of the cases highlighted the transfer of patients on methadone to buprenorphine-naloxone due to the adverse effect and interactions of methadone with other medications. During the transfer there were no major adverse reactions noted, and patients were safely able to continue with the maintenance therapy of buprenorphine- naloxone. Conclusion: Buprenorphine-naloxone is a safe and effective drug substitution therapy for opioid dependence. It has fewer interactions with other medications, and has similar efficacy to methadone. Being a partial agonist, it has a less sedating effect making patients more functional.
Buprenorphine, Naloxone Drug Combination

Biological Evolution ; Morphinans ; Papaver ; Plant Proteins ; genetics

Since the first use of epidural morphine in man, a number of other opiates have been studied including fentanyl, pethidine, methadone, diamorphine and buprenorphine. Among them buprenorphine is a relatively new synthetic opiate that is known to be highly lipophilic and to have an affmity for the opiate receptor approximately twice that of morphin:, It is produced in a preservative free solution, and would seem a logical choice for epidural analgesia. But there was no data on the adequate dose for the. postoperative pain control after lower abdominal surgery. Current study was designed to investigate the efficacy of three doses of epidural buprenorphine for postoperative pain control with the checking the pain score. Fifty seven female patients undergoing elective lower abdominal surgery were randomly assigncd to receive epidural buprenorphine as a rate of 0.3 (group A, initial dose 0.15 mg + maintenance dose O.l5 mg), 0.45 (group B, 0.15 mg + 0.3 mg), or 0.6 mg (group C, 0.3 mg + 0.3 mg) utilizing the Two-Day TI4l Infusor during the two days after cessation of operation. Authors compared the efficacy of three doses with checking the pain scale (Facial expression pain scale, Prince Henry pain scale) at 6, 12, 24, and 48 hour postoperatively. Side-effects were recorded. There were no significant difference among three groups with respects to mean age. Analgesic effects for patients receiving 0.6 mg (group C) were superior to those of group A but were not significantly different from analgesic effects of group B except 6 hour postoperatively. Side-effects (nausea and vomiting) of group C were significantly more than group B. The dose of epidural buprenorphine in Group B (initial dose 0.15 mg+maintenance dose 0 3 mg) may be recommended for postoperative analgesia following lower abdominal surgery.
Analgesia ; Analgesia, Epidural ; Buprenorphine* ; Female ; Fentanyl ; Heroin ; Humans ; Infusion Pumps ; Logic ; Meperidine ; Methadone ; Morphine ; Pain, Postoperative* ; Receptors, Opioid

The paper reports the establishment of a liquid chromatography-tandem mass spectrometry (LC-MS/MS) for simultaneous analysis of 11 opiates in hair samples, and the study of presence of opiates in the hair of active heroin addicts. About 20 mg of decontaminated and pulverized hair sample was hydrolyzed with buffer solution for 30 min, in the presence of morphine-d3 and acetylmorphine-d6 used as internal standards, and then extracted with the mixture of dichlormethane and isopropanol, separated by the Allure PFP propyl column with a mobile phase consisting of acetonitrile and 20 mmol L(-1) ammonium acetate buffer, and then analyzed by LC-MS/MS. Multiple reaction monitoring (MRM) mode was used to analyze 11 opiates. Eleven opiates showed a fairly good linearity over the corresponding range (r > 0.996 0). The detection limits were less than 0.05 ng mg(-1). The recoveries were between 47.2% and 110%, and the deviations of intra- and inter-day precision were less than 14%. Heroin, acetylmorphine, morphine, codeine, acetylcodeine and hydrocodone were detected in hair samples of 21 herion addicts. The developed method shows high sensitivity and selectivity, and is suitable for the simultaneous analysis of 11 opiates in hair samples and identify legal and illegal use of opiates.
Analgesics, Opioid ; analysis ; Chromatography, Liquid ; methods ; Codeine ; analogs & derivatives ; analysis ; Hair ; chemistry ; Heroin ; analysis ; Humans ; Hydrocodone ; analysis ; Limit of Detection ; Morphine ; analysis ; Morphine Derivatives ; analysis ; Sensitivity and Specificity ; Substance Abuse Detection ; methods ; Tandem Mass Spectrometry ; methods

BACKGROUND: Spinal opioid administration is an excellent option to separate the desirable analgesic effects of opioids from their expected dose-limiting side effects to improve postoperative analgesia. Therefore, physicians must better identify either specific opioids or adequate doses and routes of administration that result in a mainly spinal site of action rather than a cerebral analgesic one. METHODS: The purpose of this topical review is to describe current available clinical evidence to determine what opioids reach high enough concentrations to produce spinally selective analgesia when given by epidural or intrathecal routes and also to make recommendations regarding their rational and safety use for the best management of postoperative pain. To this end, a search of Medline/Embase was conducted to identify all articles published up to December 2013 on this topic. RESULTS: Recent advances in spinal opioid bioavailability, based on both animals and humans trials support the theory that spinal opioid bioavailability is inversely proportional to the drug lipid solubility, which is higher in hydrophilic opioids like morphine, diamorphine and hydromorphone than lipophilic ones like alfentanil, fentanyl and sufentanil. CONCLUSIONS: Results obtained from meta-analyses of RTCs is considered to be the 'highest' level and support their use. However, it's a fact that meta-analyses based on studies about treatment of postoperative pain should explore clinical surgery heterogeneity to improve patient's outcome. This observation forces physicians to use of a specific procedure surgical-based practical guideline. A vigilance protocol is also needed to achieve a good postoperative analgesia in terms of efficacy and security.
Alfentanil ; Analgesia ; Analgesics, Opioid ; Animals ; Biological Availability ; Fentanyl ; Heroin ; Humans ; Hydromorphone ; Morphine ; Pain, Postoperative* ; Population Characteristics ; Solubility ; Sufentanil

Renal artery pseudoaneurysm after blunt renal trauma is an uncommon complication of delayed hemorrhage, and diagnostic difficulties are experienced due to its rarity. Delayed hemorrhage after renal trauma is a lifethreatening complication. Angiography is considered the gold standard to diagnose a traumatic renal artery pseudoaneurysm. We report here a case of delayed bleeding from a renal artery pseudoaneurysm that was diagnosed at 17 days after the injury and that was managed successfully with selective renal artery embolization without medical complication.
Aneurysm, False ; Angiography ; Hemorrhage ; Kidney ; Morphinans ; Renal Artery

Animals ; Brain ; drug effects ; metabolism ; Male ; Mice ; Mice, Inbred Strains ; Morphinans ; pharmacology ; Morphine Dependence ; metabolism ; Nitric Oxide Synthase Type I ; metabolism

AIMTo reinvestigate the chemical constituents of the ethanolic extract of Meconopsis quintuplinervia Regel which is a traditional Tibetan medicine used for treatments of hepatitis, tuberculosis etc..

METHODSThe compounds were enriched by column chromatography techniques over silica gel, macro porous resin and Sephadex LH-20 absorbents, and finally purified by reverse phase preparative HPLC methods with isocratic mobile phase systems of methanol-H2O-acetic acid (500:500:1) and acetonitrile-H2O-acetic acid (200:800:1). Structural determination of the pure compounds were based on extensive analyses of modern spectroscopic methods including IR, MS, HRMS, 1D- and 2D-NMR spectra.

RESULTSThree alkaloids were obtained and their structures were elucidated as norsanguinarine (I), O-methylflavinantine (II) and 6-methoxy-17-methyl-2, 3-[methylenebis (oxy)]-morphin-5-en-7-one (III).

CONCLUSIONNorsanguinarine (I) was isolated from genus Meconopsis for the first time, and 6-methoxy-17-methyl-2,3-[methylenebis(oxy)]-morphin-5-en-7-one (III) is a new alkaloid named as meconoquintupline.

Alkaloids ; chemistry ; isolation & purification ; Medicine, Tibetan Traditional ; Molecular Conformation ; Molecular Structure ; Morphinans ; chemistry ; isolation & purification ; Morphine Derivatives ; chemistry ; isolation & purification ; Papaveraceae ; chemistry ; Plants, Medicinal ; chemistry

OBJECTIVE: Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was developed for the determination of opiates in biological samples according to the emerging problem in drugs abuse. METHODS: Opiates such as heroin, 6-acetylmorphine, morphine, codeine, acetylcodeine, hydrocodone and hydromorphone were isolated from human blood, urine, oral fluid and hair using a simple extraction and consequently analyzed using LC-MS/MS. The method was evaluated by real cases. RESULTS: The mobile phase give the optimum separation for opiates. The detection limit of morphine in urine with dilution and liquid-liquid extraction and in hair is 10ng/mL, 0.01 ng/mL and 0.01 ng/mg, respectively. CONCLUSION The method is simple and rapid, offering superior sensitivity and selectivity for opiates. The target compounds comprising hydrocodone and hydromorphone enlarge the applied area.
Chromatography, Liquid ; Codeine/analysis* ; Forensic Medicine/methods* ; Hair/chemistry* ; Humans ; Hydrocodone/analysis* ; Hydromorphone/analysis* ; Morphine/analysis* ; Narcotics/analysis* ; Reproducibility of Results ; Saliva/chemistry* ; Substance Abuse Detection/methods* ; Tandem Mass Spectrometry

OBJECTIVETo evaluate the effects of Caulis Sinomenii and sinomenine on conditioned place preference (CPP) induced by morphine and brain histamine level in mice.

METHODSSixty mice were randomized into 6 equal groups and morphine (Mor) was injected subcutaneously (9 mg/kg) for 6 consecutive days to induce CPP using a shuttle box. Since the 4th day of training, the mice in 5 of the groups were treated for 3 consecutive days with Caulis Sinomenii (10 g/kg), sinomenine (60 mg/kg), diphenhydramine (30 mg/kg), CP48/80 (5 mg/kg) and L-histidine (750 mg/kg) in addition to morphine (9 mg/kg) treatment, respectively, leaving the other group with exclusive morphine treatment. Another 10 mice received saline injection to serve as saline control group. The content of histamine (HA) in the mouse brain was measured by fluorospectrophotometry.

RESULTSIn morphine group, the mice showed significantly extended stay in morphine-paired compartment whose HA content in the brain was markedly increased (P<0.01). Treatment with Caulis Sinomenii and sinomenine resulted in significantly reduced time of stay in morphine-paired compartment and brain HA level (P<0.01).

CONCLUSIONCPP induced by morphine in mice is associated with increased HA level in the brain. Caulis Sinomenii and sinomenine can suppress the acquisition of place preference induced by morphine and modulate HA level in the central nervous system in morphine-dependent mice.

Animals ; Arginine ; pharmacology ; Brain ; drug effects ; metabolism ; Conditioning, Operant ; drug effects ; physiology ; Diphenhydramine ; pharmacology ; Histamine ; metabolism ; Male ; Mice ; Morphinans ; pharmacology ; Morphine ; toxicity ; Morphine Dependence ; etiology ; physiopathology ; Motor Activity ; drug effects ; Random Allocation ; Sinomenium ; chemistry