Cannabinoids against pain. Efficacy and strategies to reduce psychoactivity: a clinical perspective

Karst, Matthias; Wippermann, Sonja

doi:10.1517/13543780802691951

Cited by 24 publications

(8 citation statements)

References 93 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…In animal models, local administration of CB1 receptor agonists produced anti-nociceptive effects in both inflammatory and neuropathic conditions (Fox et al, 2001;Nackley et al, 2003;Richardson et al, 1998;Vera et al, 2012). Therefore, the activation of peripheral CB1 receptors (Karst and Wippermann, 2009) or the use of CB2 agonists, devoid of central effects, might be good alternatives for neuropathy management.…”

Section: Introductionmentioning

confidence: 99%

Characterization of cannabinoid-induced relief of neuropathic pain in a rat model of cisplatin-induced neuropathy

Vera

Cabezos

Martı́n

et al. 2013

Pharmacology Biochemistry and Behavior

View full text Add to dashboard Cite

Section: Introductionmentioning

confidence: 99%

Characterization of cannabinoid-induced relief of neuropathic pain in a rat model of cisplatin-induced neuropathy

Vera

Cabezos

Martı́n

et al. 2013

Pharmacology Biochemistry and Behavior

View full text Add to dashboard Cite

“…Plant‐derived cannabinoids, and in particular the two most abundant ones in Cannabis , Δ 9 ‐tetrahydrocannabinol (THC) and cannabidiol (CBD), are known to possess strong analgesic and anti‐inflammatory properties and their clinical use is now supported by several preclinical studies and clinical trials (see Mechoulam et al ., 2007; Karst and Wippermann, 2009; Rahn and Hohmann, 2009; for reviews). While most of the pharmacological effects of THC appear to be mediated selectively by cannabinoid CB 1 and CB 2 receptors, CBD is capable of interacting with several molecular targets involved in the control of pain.…”

Section: Introductionmentioning

confidence: 99%

Non‐psychoactive cannabinoids modulate the descending pathway of antinociception in anaesthetized rats through several mechanisms of action

Maione

Piscitelli²,

Gatta

et al. 2011

British J Pharmacology

144

110

View full text Add to dashboard Cite

BACKGROUND AND PURPOSETwo non-psychoactive cannabinoids, cannabidiol (CBD) and cannabichromene (CBC), are known to modulate in vitro the activity of proteins involved in nociceptive mechanisms, including transient receptor potential (TRP) channels of vanilloid type-1 (TRPV1) and of ankyrin type-1 (TRPA1), the equilibrative nucleoside transporter and proteins facilitating endocannabinoid inactivation. Here we have tested these two cannabinoids on the activity of the descending pathway of antinociception. EXPERIMENTAL APPROACHElectrical activity of ON and OFF neurons of the rostral ventromedial medulla in anaesthetized rats was recorded extracellularly and tail flick latencies to thermal stimuli were measured. CBD or CBC along with various antagonists were injected into the ventrolateral periaqueductal grey. KEY RESULTSCannabidiol and CBC dose-dependently reduced the ongoing activity of ON and OFF neurons in anaesthetized rats, whilst inducing antinociceptive responses in the tail flick-test. These effects were maximal with 3 nmol CBD and 6 nmol CBC, and were antagonized by selective antagonists of cannabinoid CB1 adenosine A1 and TRPA1, but not of TRPV1, receptors. Both CBC and CBD also significantly elevated endocannabinoid levels in the ventrolateral periaqueductal grey. A specific agonist at TRPA1 channels and a synthetic inhibitor of endocannabinoid cellular reuptake exerted effects similar to those of CBC and CBD. CONCLUSIONS AND IMPLICATIONSCBD and CBC stimulated descending pathways of antinociception and caused analgesia by interacting with several target proteins involved in nociceptive control. These compounds might represent useful therapeutic agents with multiple mechanisms of action. BJP

show abstract

“…Cannabinoids can induce analgesia but, the psychoactive side effects of centrally acting cannabinoids limits their use. This has sparked interest in a peripherally restricted class of cannabinoid receptors to treat pain of a peripheral nature (Karst and Wippermann, 2009). Given the positive effect of the cannabinoids on analgesia and its widespread distribution, this system may offer less risk of addiction, withdrawal, and overdose than opioid drugs if the appropriate cannabinoid-like compounds can be found with minimal side-effects.…”

Section: Research Directions Seeking Solutionsmentioning

confidence: 99%

“…Agonists of different receptor populations, each at an ineffective analgesic dose, can reduce off-target effects and become analgesic when co-administered. Such combinatorial drug therapies, for example those targeting the cannabinoid and opioid systems, may become promising analgesics (review; Karst and Wippermann, 2009). Another approach to increase pharmacological specificity is to target receptors/molecules expressed only in the nociceptive pathway.…”

Section: Research Directions Seeking Solutionsmentioning

confidence: 99%

Opioid pharmaceuticals and addiction: The issues, and research directions seeking solutions

Walwyn¹,

Miotto²,

Evans³

2010

Drug and Alcohol Dependence

View full text Add to dashboard Cite

There are few pharmaceuticals superior to opiates for the treatment of pain. However, with concerns of addiction, withdrawal and questionable efficacy for all types of pain, these compounds are far from a magical panacea for pain-relief. As it is unlikely that other classes of compounds will supersede the opioids in the very near future, it is important to both optimize current opioid therapies and curb the astounding diversion of opioids from their intended analgesic use to non-medical abuse. In optimizing opioid therapeutics it is necessary to enhance the clinical awareness of the benefits of treating pain and combine this with aggressive strategies to reduce diversion for non-medical use. At the heart of the issue of opioid misuse is the role of opioid systems in the reward circuitry, and the adaptive processes associated with repetitive opioid use that manifest during withdrawal. Emerging pharmacological insights of opioid receptors will be reviewed that provide future hope for developing opioid-based analgesics with reduced addictive properties and perhaps, reduced opponent processes. In addition, with the increased understanding of nociceptive circuitry and the molecules involved in transmitting pain, new therapeutic targets have become evident that may result in effective analgesics either alone or in combination with current opioid therapies.

show abstract

Cannabinoids against pain. Efficacy and strategies to reduce psychoactivity: a clinical perspective

Cited by 24 publications

References 93 publications

Characterization of cannabinoid-induced relief of neuropathic pain in a rat model of cisplatin-induced neuropathy

Characterization of cannabinoid-induced relief of neuropathic pain in a rat model of cisplatin-induced neuropathy

Non‐psychoactive cannabinoids modulate the descending pathway of antinociception in anaesthetized rats through several mechanisms of action

Opioid pharmaceuticals and addiction: The issues, and research directions seeking solutions

Contact Info

Product

Resources

About