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Novel psychoactive substances and inhalants
Published in Ilana B. Crome, Richard Williams, Roger Bloor, Xenofon Sgouros, Substance Misuse and Young People, 2019
The psychoactive chemical found in Salvia is salvinorin A, which is one of the most potent naturally occurring hallucinogens. It is absorbed rapidly from the buccal mucosa and crosses the blood-brain barrier where it is rapidly metabolised into an inactive form. This aspect of its pharmacokinetics results in Salvia’s very rapid but short-lived action in terms of hallucinatory experiences (Yan and Roth, 2004).
Phytochemicals: Some Basics
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
Other well-known pharmacologically active terpenes are: beta-carotene, the common terpene that is the precursor to vitamin A; valerenic acid, a component of valerian root extract thought to be partially responsible for its sedative effects; gossypol, the extract of cotton seed that has been investigated as a male contraceptive pill; and paclitaxel (perhaps better known as Taxol), the large and complex anticancer terpene from the yew tree. The medically important heart drug digoxin and the ginsenosides from the revered ginseng plant are modified terpenes, i.e., terpene glycosides. The hallucinogenic drug, salvinorin A, extracted from the leaves of Salvia divinorum, is a bicyclic diterpenoid.
Licit and illicit drugs
Published in Jason Payne-James, Richard Jones, Simpson's Forensic Medicine, 2019
Jason Payne-James, Richard Jones
The effects produced by salvinorin A are qualitatively different than those produced by the other hallucinogens such as LSD or mescaline, and the mechanism of action is not understood. It is known that κ-opioid receptors also play a key role in the human stress response. Because κ stimulation tends to neutralise the effects of μ1 stimulation, some feel the presence of the κ receptor may diminish the possibility of drug overdose. There is also evidence that stimulation of κ receptors in some way protects the neuron from damage; in particular, damage produced by hypoxia/ischaemia is minimised in the presence of κ receptor agonists but, again, the mechanisms involved remain totally unknown.
Adverse pharmacokinetic interactions between illicit substances and clinical drugs
Published in Drug Metabolism Reviews, 2020
Kodye L. Abbott, Patrick C. Flannery, Kristina S. Gill, Dawn M. Boothe, Muralikrishnan Dhanasekaran, Sridhar Mani, Satyanarayana R. Pondugula
Salvia divinorum, is a sage species used as an entheogen (Tsujikawa et al. 2009; Serra et al. 2015). Salvia can be smoked, chewed, or brewed as a tea (NIDA 2019). Salvinorin A, the active ingredient of salvia, acts as a selective κ-opioid receptor agonist resulting in its dissociative and psychoactive properties (Kuhn et al. 2008; Cruz et al. 2017). Salvinorin A is metabolized by CYP2D6, CYP1A1, CYP2C18, CYP2E1 and UGT2B7 (Teksin et al. 2009) (Table 3). Salvinorin A may also be metabolized by blood esterases (Schmidt et al. 2005). Salvinorin A was noted to be a substrate of P-gp (Teksin et al. 2009; Butelman et al. 2012) (Table 3). Currently, there are no reports whether salvia can modulate drug-metabolizing enzymes and drug-transporters, or whether it can cause adverse interactions when taken with clinical drugs.
How can we develop better antispasmodics for irritable bowel syndrome?
Published in Expert Opinion on Drug Discovery, 2019
Sheyda Ranjbar, Seyed Afshin Seyednejad, Shekoufeh Nikfar, Roja Rahimi, Mohammad Abdollahi
Plant-derived molecules were also effective in alleviating symptoms of animal IBS-D models. Patchouli alcohol (PA), a sesquiterpene extracted from Pogostemon cablin, alleviated IBS-D symptoms in a rat model by inhibition of spontaneous contraction of longitudinal SMCs in a concentration-dependent manner. It was suggested that the cholinergic, nitrergic and K+ channel pathways are involved in its activity [73]. Oral administration of dichloromethane (DCM) extracts of Calea zacatechichi, a Mexican plant, exhibited antidiarrheal effect on mouse IBS model. The extract restricted GI hypermotility while exerting analgesic effects as well. Furthermore, no psychoactive component of C.zacatechichi was found in DCM extract, substantiating its safety profile [74]. Salvinorin A is a derivative from another Mexican plant, Salvia divinorum. Motility-inhibitory effects of PR-38, a novel analogue of Salvinorin was investigated in vitro and in vivo. PR-38 was found to dramatically inhibit colonic motility and pain in mouse IBS model, with suggested mechanism of interaction with opioid and cannabinoid pathways. Again, it was observed that PR-38 is free of the CNS side effects associated with Salvinorin A, suggesting its safety profile [75]. Berberine is a widely investigated alkaloid mainly isolated from Berberis vulgaris and has demonstrated beneficial effects against IBS-D symptoms like diarrhea and pain possibly through the involvement of mu and delta opioid receptors [76]. In a clinical study, berberine was well tolerated and successfully managed the IBS-D symptoms and improved the patients’ QOL [77].
Antinociceptive and anxiolytic-like effects of a neo-clerodane diterpene from Salvia semiatrata aerial parts
Published in Pharmaceutical Biology, 2020
Nancy Ortiz-Mendoza, Lizeth M. Zavala-Ocampo, Martha J. Martínez-Gordillo, María Eva González-Trujano, Francisco A. Basurto Peña, Iván J. Bazany-Rodríguez, José Alberto Rivera Chávez, Alejandro Dorazco-González, Eva Aguirre-Hernández
Although there are several studies reporting the antinociceptive effects of different extracts and species of Salvia, there is not enough research on the main responsible active metabolites. In the case of neo-clerodane terpenes, there is also scarce information about its potential to relieve pain. An exception is S. divinorum, which is well known because of the presence of salvinorin A, a neo-clerodane terpene widely studied for its depressant activity on the CNS (Casselman et al. 2014). The dose-dependent antinociceptive effects of salvinorin A have been explored using the tail-flick and the hot plate tests (Tlacomulco-Flores et al. 2020), formalin (Guida et al. 2012) and writhing tests (McCurdy et al. 2006) in mice. In the present study, it should be noted that 1 tested at 10 mg/kg, p.o. produced a dose-dependent antinociceptive effect that remained until the end of the experiment (30 min) in the writhing test in mice (Figure 5(A)). Our data agree to that reported for tilifolidione (1–100 mg/kg, p.o.), a clerodane diterpene isolated from Salvia tiliifolia Vahl, which produced a dose-dependent antinociceptive effect in the writhing and formalin tests in mice (González-Chávez et al. 2018). Whereas, amarisolide (1, 5 and 10 mg/kg, i.p.), a neo-clerodane isolated from the aerial parts of S. circinata, produced significant but non-dose-dependent antinociceptive effects in the writhing test in mice (Moreno-Pérez et al. 2019). These data together reinforce the participation of neo-clerodane diterpenes as responsible for the depressant CNS activity of sage and their potential as alternative for pain treatment.