Pharmacologic and clinical assessment of kratom: An update

2019 ◽  
Vol 76 (23) ◽  
pp. 1915-1925 ◽  
Author(s):  
C Michael White

Abstract Purpose This article presents updated information on kratom (Mitragyna speciosa), a natural opioid with stimulant properties that is currently sold in the United States without a prescription. Summary Kratom exerts opioid and alpha-2 agonistic effects, as well as anti-inflammatory and mild stimulant effects. Respiratory depression has not been commonly reported, but kratom does cause a host of adverse effects. While kratom may have a role in patients who are in chronic pain or dependent on opioid painkillers or heroin, this needs to be established in clinical trials. Kratom may have drug interactions as both a cytochrome P-450 system substrate and inhibitor. Kratom does not appear in normal drug screens and, especially when ingested with other substances of abuse, may not be recognized as an agent of harm. There are numerous cases of death in kratom users, but many involved polypharmaceutical ingestions. There are assessments where people have been unable to stop using kratom therapy and withdrawal signs/symptoms occurred in patients or their newborn babies after kratom cessation. Both banning and failure to ban kratom places people at risk; a middle-ground alternative, placing it behind the pharmacy counter, might be useful. Conclusion Kratom has a unique pharmacologic profile that might offer advantages over other opioids, but its high abuse liability, potential for drug interactions and adverse events, and inadequate research into the balance of benefits to harm are concerning. There is mounting information on the adverse events associated with kratom use and potential treatments that can be useful to clinicians.

2018 ◽  
Author(s):  
Jon-Patrick Allem ◽  
Likhit Dharmapuri ◽  
Adam M Leventhal ◽  
Jennifer B Unger ◽  
Tess Boley Cruz

BACKGROUND Hookah (or tobacco waterpipe) use has recently become prevalent in the United States. The contexts and experiences associated with hookah use are unclear, yet such information is abundant via publicly available hookah users’ social media postings. OBJECTIVE In this study, we utilized Twitter data to characterize Twitter users’ recent experiences with hookah. METHODS Twitter posts containing the term “hookah” were obtained from April 1, 2017 to 29 March, 2018. Text classifiers were used to identify clusters of topics that tended to co-occur in posts (n=176,706). RESULTS The most prevalent topic cluster was Person Tagging (use of @username to tag another Twitter account in a post) at 21.58% (38,137/176,706) followed by Promotional or Social Events (eg, mentions of ladies’ nights, parties, etc) at 20.20% (35,701/176,706) and Appeal or Abuse Liability (eg, craving, enjoying hookah) at 18.12% (32,013/176,706). Additional topics included Hookah Use Behavior (eg, mentions of taking a “hit” of hookah) at 11.67% (20,603/176,706), Polysubstance Use (eg, hookah use along with other substances) at 10.95% (19,353/176,706), Buying or Selling (eg, buy, order, purchase, sell) at 9.37% (16,552/176,706), and Flavors (eg, mint, cinnamon, watermelon) at 1.66% (2927/176,706). The topic Dislike of Hookah (eg, hate, quit, dislike) was rare at 0.59% (1043/176,706). CONCLUSIONS Social events, appeal or abuse liability, flavors, and polysubstance use were the common contexts and experiences associated with Twitter discussions about hookah in 2017-2018. Considered in concert with traditional data sources about hookah, these results suggest that social events, appeal or abuse liability, flavors, and polysubstance use warrant consideration as targets in future surveillance, policy making, and interventions addressing hookah.


2012 ◽  
Vol 2 (6) ◽  
pp. 144-151
Author(s):  
Aaron Crawford ◽  
Tiffany-Jade Kreys

The prevalence of obesity in the United States (U.S.) is currently at 34%. This article will review two of the newer weight loss agents: lorcaserin and phentermine/topiramate. Mechanism of action, dosing, adverse events, and drug interactions will be discussed.


2020 ◽  
Vol 21 (6) ◽  
pp. 427-435 ◽  
Author(s):  
Cheng Cui ◽  
Siqi Tu ◽  
Valerie Sia Jie En ◽  
Xiaobei Li ◽  
Xueting Yao ◽  
...  

Background: As the number of severe acute respiratory syndrome coronavirus 2 (SARS-COV-2) infected people is greatly increasing worldwide, the international medical situation becomes very serious. Potential therapeutic drugs, vaccine and stem cell replacement methods are emerging, so it is urgent to find specific therapeutic drugs and the best treatment regimens. After the publications on hydroxychloroquine (HCQ) with anti- SARS-COV-2 activity in vitro, a small, non-randomized, open-label clinical trial showed that HCQ treatment was significantly associated with reduced viral load in patients with coronavirus disease-19 (COVID-19). Meanwhile, a large prophylaxis study of HCQ sulfate for COVID-19 has been initiated in the United States. HCQ offered a promising efficacy in the treatment of COVID-19, but the optimal administration is still being explored. Methods: We used the keyword "hydroxychloroquine" to conduct a literature search in PubMed to collect relevant literature on the mechanism of action of HCQ, its clinical efficacy and safety, pharmacokinetic characteristics, precautions for clinical use and drug interactions to extract and organize information. Results: This paper reviews the mechanism, clinical efficacy and safety, pharmacokinetic characteristics, exposureresponse relationship and precautions and drug interactions of HCQ, and summarizes dosage recommendations for HCQ sulfate. Conclusion: It has been proved that HCQ, which has an established safety profile, is effective against SARS-CoV-2 with sufficient pre-clinical rationale and evidence. Data from high-quality clinical trials are urgently needed worldwide.


2021 ◽  
Vol 14 (5) ◽  
pp. 472
Author(s):  
Tyler C. Beck ◽  
Kyle R. Beck ◽  
Jordan Morningstar ◽  
Menny M. Benjamin ◽  
Russell A. Norris

Roughly 2.8% of annual hospitalizations are a result of adverse drug interactions in the United States, representing more than 245,000 hospitalizations. Drug–drug interactions commonly arise from major cytochrome P450 (CYP) inhibition. Various approaches are routinely employed in order to reduce the incidence of adverse interactions, such as altering drug dosing schemes and/or minimizing the number of drugs prescribed; however, often, a reduction in the number of medications cannot be achieved without impacting therapeutic outcomes. Nearly 80% of drugs fail in development due to pharmacokinetic issues, outlining the importance of examining cytochrome interactions during preclinical drug design. In this review, we examined the physiochemical and structural properties of small molecule inhibitors of CYPs 3A4, 2D6, 2C19, 2C9, and 1A2. Although CYP inhibitors tend to have distinct physiochemical properties and structural features, these descriptors alone are insufficient to predict major cytochrome inhibition probability and affinity. Machine learning based in silico approaches may be employed as a more robust and accurate way of predicting CYP inhibition. These various approaches are highlighted in the review.


2021 ◽  
Vol 12 ◽  
pp. 204209862095927
Author(s):  
Wei C. Yuet ◽  
Didi Ebert ◽  
Michael Jann

Neurocognitive adverse events have been observed with the widespread use of 3-hydroxy-3-methylglutaryl-CoA reductase inhibitors or “statins,” which reduce low-density lipoprotein cholesterol (LDL-C) levels and subsequently cardiovascular risk. The United States Food and Drug Association directed manufacturers of proprotein convertase subtilisin-kexin type 9 (PCSK9) inhibitors to monitor for neurocognitive adverse events due to their potent effects on LDL-C reduction, which is a proposed mechanism for neuronal cell dysfunction. Other proposed mechanisms for PCSK9 inhibitor-associated neurocognitive adverse events include N-methyl-d-aspartate receptor modulation, dysregulation of lipid and glucose metabolism, and patient-specific risk factors for cognitive impairment. The purpose of this narrative review article is to describe the proposed mechanisms, incidence of neurocognitive adverse events from phase II and III trials for PCSK9 inhibitors, neurocognitive assessments utilized in clinical trials, and clinical implications. Given the increasing prevalence of PCSK9 inhibitor use and the neurocognitive adverse events observed with prior lipid-lowering therapies, clinicians should be aware of the risks associated with PCSK9 inhibitors, especially when therapy is indicated for patients at high risk for cardiovascular events. Overall, the incidence of PCSK9 inhibitor-associated neurocognitive appears to be uncommon. However, additional prospective studies evaluating cognitive impairment may be beneficial to determine the long-term safety of these agents.


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