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Key Clinical Message: When self‐administration with counterfeit or mislabeled medicine is suspected, comprehensive laboratory analysis should be preferred over immunoassay screening to avoid false negative results. Carisoprodol, which was formerly a popular muscle relaxant drug in many countries, has reappeared on illegal drug markets, and may cause an itching, purple‐colored rash, even after a single dose. [ABSTRACT FROM AUTHOR]

Key Clinical Message When self‐administration with counterfeit or mislabeled medicine is suspected, comprehensive laboratory analysis should be preferred over immunoassay screening to avoid false negative results. Carisoprodol, which was formerly a popular muscle relaxant drug in many countries, has reappeared on illegal drug markets, and may cause an itching, purple‐colored rash, even after a single dose.

Introduction: Studying polysubstance use is a public health recommendation. In the United Arab Emirates, more than 80% of adults with opioid use disorder (OUD) use 2 or more nonopioid substances. This secondary analysis contrasts the characteristics of polysubstance users (OUD + ≥1 nonopioid) with OUD, explores the correlates and predictors of nonfatal overdose, and examines the impact of polysubstance use on OUD treatment outcomes using buprenorphine (BUP). Methods: This analysis uses data from a 16-week outpatient randomized controlled trial of 141 adults with OUD allocated to BUP + incentivized adherence and abstinence monitoring (n = 70) and BUP in usual care (control, n = 71). Outcomes were nonfatal overdose events over the preceding 12 months, positive drug screens, and treatment retention. Participant characteristics were contrasted, and bivariate statistical tests were conducted for simple associations followed by logistic regression. Results: Polysubstance use was reported by 117 participants (82.9%), the majority of whom used pregabalin 72.1% (n = 75). Compared with OUD, polysubstance users observed higher arrests (median, 1.0 [interquartile range, 0.0–3.0] vs 0.5 [interquartile range, 0.0–2.0]; P = 0.04]) and nonfatal overdose events (n = 33 [31.8%] vs 2 [10.8%], P = 0.003). Carisoprodol and injecting drug use independently predicted nonfatal overdose (adjusted odds ratio, 4.519 [95% confidence interval, 1.81–11.22] and 2.74 [95% confidence interval, 1.15–6.51], respectively). No significant difference was observed in opioid use and retention in treatment outcomes between groups. Conclusion: Carisoprodol and injecting drug use increase the likelihood of nonfatal overdose in adults with OUD. Polysubstance use does not impact response to BUP treatment compared with OUD. [ABSTRACT FROM AUTHOR]

This study evaluated the early drug prescription patterns as predictors of final workers compensation claim costs and closure based on an updated analysis on a large cohort. The result would provide claim management with tools to estimate final claims outcomes in the first 3- or 6-months post-injury. Objective: The aim of the study is to determine the associations of workers' compensation claim costs and return to work with drugs prescribed for early symptom management. Methods: Claims filed from 1998 to 2007 were followed for 10 years from the injury date. Drugs analyzed included gabapentin, pregabalin, antipsychotics, antidepressants, sedatives, benzodiazepines, carisoprodol, and opioids, controlling for initial reserve, sex, age, physical therapy, attorney involvement, and surgery. Results: Gabapentin, antipsychotics, antidepressants, and sedatives used in the first 3 months after injury were significantly associated with higher claim cost (≥$100,000). All opioid morphine equivalent doses greater than or equal to 5 mg/d for the first 6 months was significantly associated with higher cost (≥$100,000) and not being released to work at end of third year after injury with dose-response relationships. Conclusions: Prescription patterns in the first 3 months or first 6 months of workers' compensation claim development may be used as predictors of claim outcomes. [ABSTRACT FROM AUTHOR]

PURPOSE: To evaluate the role of muscle-relaxants as risk factors for the development of central serous chorioretinopathy (CSC) - the second most common retinopathy in our settings; despite multiple risk factors seen in our patients, 21% were initially labelled as idiopathic. MATERIALS AND METHODS: Retrospective case-control study at a tertiary hospital in the United Arab Emirates, where we reviewed the medical records of 273 patients with CSC examined between 2010 and 2019 for use of muscle-relaxants including tolperisone/eperisone, carisoprodol and gabapentin/pregabalin within a year of onset/recurrence of the disease. Intake of drugs with known association with CSC (including corticosteroids/sympathomimetics) was also recorded. Two hundred eighty-six subjects with adverse events seen at the same institute during the same study period served as controls. Odds ratios, Chi-Square tests and multivariate logistic regression were carried out to determine any associations with the muscle-relaxants and other pharmacological confounders - corticosteroids/sympathomimetics. RESULTS: Muscle relaxants may increase the risk of CSC as evident on multivariate regression analysis (OR: 2.55; confidence interval [CI]: 1.208-5.413); the significance was retained on removing the 6 subjects who had corticosteroids/sympathomimetics (OR: 2.30; CI: 1.073–4.939). Univariate analysis yielded an OR of 2.52 for muscle relaxants (CI: 1.2149–5.2276), 2.96 for eperisone/tolperisone (CI: 1.3531–6.5038), and 6.26 for eperisone as an individual agent (CI: 1.8146–21.6252). CONCLUSION: We found muscle relaxants to be associated factors of CSC regardless of inclusion of corticosteroids/sympathomimetics (P < 0.05). Among individual classes of muscle relaxants in this study, only eperisone/tolperisone posed a significant risk (P < 0.05). The vascular smooth muscle relaxation could be the possible mechanism that affects the choroidal blood flow and indirectly predisposes to CSC.

PURPOSE: To evaluate the role of muscle-relaxants as risk factors for the development of central serous chorioretinopathy (CSC) - the second most common retinopathy in our settings; despite multiple risk factors seen in our patients, 21% were initially labelled as idiopathic. MATERIALS AND METHODS: Retrospective case-control study at a tertiary hospital in the United Arab Emirates, where we reviewed the medical records of 273 patients with CSC examined between 2010 and 2019 for use of muscle-relaxants including tolperisone/eperisone, carisoprodol and gabapentin/pregabalin within a year of onset/recurrence of the disease. Intake of drugs with known association with CSC (including corticosteroids/sympathomimetics) was also recorded. Two hundred eighty-six subjects with adverse events seen at the same institute during the same study period served as controls. Odds ratios, Chi-Square tests and multivariate logistic regression were carried out to determine any associations with the muscle-relaxants and other pharmacological confounders - corticosteroids/sympathomimetics. RESULTS: Muscle relaxants may increase the risk of CSC as evident on multivariate regression analysis (OR: 2.55; confidence interval [CI]: 1.208-5.413); the significance was retained on removing the 6 subjects who had corticosteroids/sympathomimetics (OR: 2.30; CI: 1.073-4.939). Univariate analysis yielded an OR of 2.52 for muscle relaxants (CI: 1.2149-5.2276), 2.96 for eperisone/tolperisone (CI: 1.3531-6.5038), and 6.26 for eperisone as an individual agent (CI: 1.8146-21.6252). CONCLUSION: We found muscle relaxants to be associated factors of CSC regardless of inclusion of corticosteroids/sympathomimetics (P < 0.05). Among individual classes of muscle relaxants in this study, only eperisone/tolperisone posed a significant risk (P < 0.05). The vascular smooth muscle relaxation could be the possible mechanism that affects the choroidal blood flow and indirectly predisposes to CSC. [ABSTRACT FROM AUTHOR]

Objective To examine the prevalence and duration of skeletal muscle relaxant (SMR) treatment among commercially insured adults in the United States. Methods We used the MarketScan Research Database to identify a cohort of adults 18 to 64 years who had ≥2-year continuous enrollment between 2005 and 2018. We estimated the prevalence of SMR treatment using a repeated cross-sectional design and derived treatment duration using the Kaplan-Meier method. Analyses were stratified by age group, sex, geographic region, individual SMR agent, and musculoskeletal disorder. Results 48.7 million individuals were included. Treatment prevalence ranged from 61.5 to 68.3 per 1,000. About one-third of users did not have a preceding musculoskeletal disorder diagnosis. Cyclobenzaprine was the dominant agent accounting for >50% of prescriptions. The considerable growth in the use of baclofen, tizanidine, and methocarbamol paralleled with a decline in carisoprodol and metaxalone use. The prevalence was highest in the South while lowest in the Northeast. The median treatment duration was 14 days with 4.0%, 1.9%, and 1.0% of individuals using SMRs for more than 90, 180, and 365 days, respectively. Compared with cyclobenzaprine, patients initiating baclofen, tizanidine, and carisoprodol had longer treatment duration. Conclusions SMRs are widely used in the United States. Their use slightly increased in recent years, but trends varied among individual agents, patient groups, and geographic regions. Despite limited evidence to support efficacy, a sizable number of U.S. adults used SMRs for long-term and off-label conditions. Further study is needed to understand determinants of treatment as well as outcomes associated with such use. [ABSTRACT FROM AUTHOR]

Background: Carisoprodol (Somadril®) is a centrally acting skeletal muscle relaxant that is commonly used to treat serious musculoskeletal disorders. Carisoprodol's mechanism of action is unknown and it is often attributed to its active metabolite, meprobamate. Objective: This study aimed to detect histopathological and immunohistochemical changes in the tissues of the splenic pregnant rats treated orally with Carisoprodol (Soma). Method: Thirty pregnant female albino rats were randomly categorized into three groups. The first group was a negative control and administered oral doses of distilled water. The other two groups were administered oral doses of carisoprodol in the distilled water equivalent to 10.8 mg and 21.6 mg/100g body weight/day respectively for 15 days from the 6th day to the 20th day of gestation. Results: Histological and immunohistochemical studies have been performed on the tissue of the spleen to detect histopathological and immunohistochemical changes. Compared to untreated (negative control) and pregnant rats treated with carisoprodol, the treated rats showed numerous histopathological and immunochemical changes. Conclusion: Treatment of pregnant rats with carisoprodol has induced many atrophic changes in the tissue of the spleen in pregnant rats, so the use of this drug during pregnancy should be under strict protection. [ABSTRACT FROM AUTHOR]

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The incidence of melanoma is one of the fastest growing of all tumor types in the United States and the number of cases worldwide has doubled in the past 30 years. Melanoma, which arises from melanocytes, is an extremely aggressive tumor that invades the vascular and lymphatic systems to establish tumors elsewhere in the body. Melanoma is a particularly resilient cancer and systemic therapy approaches have achieved minimal success against metastatic melanoma resulting in only a few FDA-approved treatments with limited benefit. Leading treatments offer minimal efficacy with response rates generally under 15% in the long term with no clear effect on melanoma-related mortality. Even the recent success of the specific BRAF mutant inhibitor vemurafenib has been tempered somewhat since acquired resistance is rapidly observed. Thus, understanding the mechanism(s) of melanoma carcinogenesis is paramount to combating this deadly disease. Not only for the treatment of melanoma but, ultimately, for prevention. In this report, we will summarize our work to date regarding the characterization of ultraviolet radiation (UVR)-mediated melanomagenesis and highlight several promising avenues of ongoing research. © 2014 Elsevier B.V. All rights reserved.

Background: skeletal muscle relaxants contain a diverse mix of agents with different buildings and tools for achievement. These agents are classified as antispasmodics or antispasmodic agents, one of them is the drug carisoprodol. Objective: the current study aimed to investigate the possible effect of somadril compound on the skeletal muscle fibres and skin of fetuses maternally treated with carisoprodol.Material and methods: 30 pregnant female rats were categorized into 3 groups equal in number ten for each group, the first one (Control group ) ten pregnant female rats were administrated oral doses of distilled water; rats of the second group (S1) were administrated oral doses of carisoprodol in distilled water equivalent to 10.8 mg / 100 g body weight/ day and rats of the third group (S2) were administrated oral dose of carisoprodol in the distilled water equivalent to 21.6 mg /100g body weight/day. Rats of S1 and S2 were administrated oral dose of carisoprodol for 15 days from the 6 th day to the 20th day of gestation. Many histological, histochemical and immunohistochemical studied were done to detect the alterations in the fetal skeletal muscles and skin. Results: fetal skin and skeletal muscle tissues of both treated groups showed many changes compared to the control group. Conclusion: treatment of the pregnant rats with carisoprodol led to numerous pathological changes in the fetal skin and skeletal muscle fibres. [ABSTRACT FROM AUTHOR]

The aim of this study to explore the spectroscopic behavior of carisoprodol in terms of simulated spectra (IR and Raman). The intramolecular H-bond of the molecule has been inspected from the Atoms in a Molecule (AIM) approach which infers that there exists partial covalent H-bond in nature. The protein-ligand binding activity of the drug molecule has been analyzed theoretically from the molecular docking approach with the predicted targets in terms of binding energy and conventional H-bond with residue. The molecular docking analysis of the title molecule explores that the binding energy with the protein acetylcholinesterase is more than the protein epoxide hydrolase1. The nonlinear optical (NLO) behavior of the title molecule has been scrutinized which motivates that the potent use of the molecule as NLO material. BIBECHANA 18 (1) (2021) 48-57

Carisoprodol has been widely used as a muscle relaxant agent. In Indonesia, carisoprodol is well-known as carnophene/zenith. Many retailers sell this drug illegally, especially to sex workers to make them feel more relaxed. Due to high incidence of carisoprodol abuse, Drug Enforcement Administration (DEA) categorized it into Schedule IV. Knowledge about pharmacokinetic and pharmacodynamic of carisoprodol are essential to be understood for proper diagnosis and management. Until now, there are only a few case reports about carisoprodol intoxication and no guideline has been published. This article aims to provide an overview about carisoprodol intoxication, starting from the mechanism of action to its management. In the body, carisoprodol is metabolized to meprobamate by CYP2C19 liver enzyme. Diagnosis of carisoprodol intoxication is challenging because carisoprodol and meprobamate have opposite effect. Gastric lavage, administration of flumazenil and bemegride may be effective for acute intoxication case. [ABSTRACT FROM AUTHOR]

Background: In January 2012, the Drug Enforcement Agency (DEA) classified carisoprodol as a Schedule IV controlled substance at the US federal level. We aimed to examine the effect of this policy on the use of carisoprodol in a commercially-insured population.Methods: This interrupted time series study included individuals with musculoskeletal disorders in the IBM MarketScan Commercial Database between December 2009 and February 2014. We used comparative segmented linear regression to assess changes in the proportions of patients who filled/newly filled carisoprodol each month.Results: A total of 13.3 million patients were included. 29 states with no scheduling prior to the DEA classification had lower baseline prevalence of carisoprodol use compared to 17 states that had scheduled carisoprodol individually before 2010 (11.0 vs. 21.1 patients with fills per 1000 patients). The federal scheduling was associated with an immediate decline (-1.12 per 1000 patients, p < 0.01) and decreasing trend in prevalence (-0.07 per 1000 patients per month, p = 0.02). This effect was not modified by existing state-level scheduling status. During the first, second, third, and fourth 6-month periods after federal scheduling, the relative difference between observed and predicted prevalence was 7.8%, 10.5%, 13.4%, and 19.8%. Similar patterns were observed for carisoprodol initiation. Overall, declining use was more pronounced among younger age groups and patients with injury.Conclusions: Schedule IV controlled substance classification at the federal level was associated with a moderate reduction in the dispensing of carisoprodol regardless of whether scheduling was already present at the state level. [ABSTRACT FROM AUTHOR]

The aim of study was to determine factor of drug abuse of PCC (paracetamol, caffein, carisoprodol) in Kendari City, 2017. This study was an analytical research with cross sectional study approach. The population in this study were all drug users recorded in the Health Agency of Southeast Sulawesi in 2017 which were 90 people, while the sample in this study was the entire population which was using exhaustive sampling technique. The results of this study with 95% confidence level showed RP = 1.481 with CI range = 1.037-2,115. The value of RP> 1, means that respondents with introverted personality were 1.5 times more likely to abuse PCC drugs than those with extroverted personality. RP value = 3.500 with range CI = 1,529-8,012. RP value> 1, meaning high curiosity respondents were 3.5 times more likely to abuse PCC drugs than those with low curiosity. RP value = 0.103 with range CI = 0,041-0,260. The value of RP <1, meaning that respondents with high economic conditions were 0.1 times greater risk of abuse of PCC drugs than those with low economic conditions. The range of LL values RP (0.041) to UL RP (0.260) includes a value <1, then the risk was protective or not significant. And the value of RP = 1.305 with the range CI = 0.857-1.985. The value of RP> 1, means that respondents whose family environment was at risk 1.3 times more likely to abuse PCC drugs than the poor family environment. Advice To the government authorities to increase supervision and enforcement of the law against the circulation of drugs so the affordability of these drugs cannot be easily obtained by everyone. [ABSTRACT FROM AUTHOR]

The polymorphism in carisoprodol was analyzed, and a metastable polymorph, B, was detected for the first time whose melting enthalpy was estimated, and which showed a monotropic relationship with the most stable polymorph, A. A third crystalline form was sometimes observed in small quantities, with a melting temperature very close to that of B. Polymorph A melted at T fus  = 95 °C ( ΔH fus  = 38 kJ mol −1 ); on the other hand carisoprodol showed a strong glass forming ability with a glass transition temperature T g  = −8 °C, meaning that it can exist as a metastable liquid at room temperature; furthermore, it crystallizes isothermally at room temperature over long periods, and exhibits cold crystallization at about 60 °C when heated on slow ramps. The molecular mobility of the amorphous solid state of carisoprodol was characterized by its steepness (or fragility) index, m , and by the activation energy at T g , E a (T g ) , determined from the heating rate dependence of the temperature location of the DSC glass transition signature as well as from the features of the TSDC peak of the glass transition. Finally, the dynamic fragility measured for carisoprodol and for a wide range of other drugs and small molecule glass-forming liquids, was compared with the thermodynamic fragility as defined by Wang and Angell. The comparison showed a reasonable agreement, and it was found that the most probable value of the reduced glass transition temperature is 0.73, somewhat different from that corresponding to the “2/3 rule”. [ABSTRACT FROM AUTHOR]