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Cannabis and cannabinoids: pharmacology and rationale for clinical use.

Abstract

It is now known that there are at least two types of cannabinoid receptors. These are CB1 receptors, present mainly on central and peripheral neurones, and CB2 receptors, present mainly on immune cells. Endogenous cannabinoid receptor agonists ('endocannabinoids') have also been identified. The discovery of this 'endogenous cannabinoid system' has led to the development of selective CB1 and CB2 receptor ligands and fueled renewed interest in the clinical potential of cannabinoids. Two cannabinoid CB1 receptor agonists are already used clinically, as antiemetics or as appetite stimulants. These are D 9 - tetrahydrocannabinol (THC) and nabilone. Other possible uses for CB1 receptor agonists include the suppression of muscle spasm/spasticity associated with multiple sclerosis or spinal cord injury, the relief of chronic pain and the management of glaucoma and bronchial asthma. CB1 receptor antagonists may also have clinical applications, e. g. as appetite suppressants and in the management of schizophrenia or disorders of cognition and memory. So too may CB2 receptor ligands and drugs that activate cannabinoid receptors indirectly by augmenting endocannabinoid levels at cannabinoid receptors. When taken orally, THC seems to undergo variable absorption and to have a narrow 'therapeutic window' (dose range in which it is effective without producing significant unwanted effects). This makes it difficult to predict an oral dose that will be both effective and tolerable to a patient and indicates a need for better cannabinoid formulations and modes of administration. For the therapeutic potential of cannabis or CB1 receptor agonists to be fully exploited, it will be important to establish objectively and conclusively (a) whether these agents have efficacy against selected symptoms that is of clinical significance and, if so, whether the benefits outweigh the risks, (b) whether cannabis has therapeutic advantages over individual cannabinoids, (c) whether there is a need for additional drug treatments to manage any of the disorders against which cannabinoids are effective, and (d) whether it will be possible to develop drugs that have reduced psychotropic activity and yet retain the ability to act through CB1 receptors to produce their sought-after effects.

Authors+Show Affiliations

Institute of Biomedical Sciences, Aberdeen, Scotland. rgp@aberdeen.ac.uk

Source

Forschende Komplementarmedizin 6 Suppl 3: 1999 Oct pg 12-5

MeSH

Antiemetics
Appetite Stimulants
Cannabinoid Receptor Modulators
Cannabinoids
Cannabis
Dronabinol
Humans
Phytotherapy
Receptors, Cannabinoid
Receptors, Drug

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

10575283

Citation

Pertwee, R G.. "Cannabis and Cannabinoids: Pharmacology and Rationale for Clinical Use." Forschende Komplementarmedizin, vol. 6 Suppl 3, 1999, pp. 12-5.
Pertwee RG. Cannabis and cannabinoids: pharmacology and rationale for clinical use. Forsch Komplementarmed. 1999;6 Suppl 3:12-5.
Pertwee, R. G. (1999). Cannabis and cannabinoids: pharmacology and rationale for clinical use. Forschende Komplementarmedizin, 6 Suppl 3, pp. 12-5.
Pertwee RG. Cannabis and Cannabinoids: Pharmacology and Rationale for Clinical Use. Forsch Komplementarmed. 1999;6 Suppl 3:12-5. PubMed PMID: 10575283.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Cannabis and cannabinoids: pharmacology and rationale for clinical use. A1 - Pertwee,R G, PY - 1999/11/27/pubmed PY - 1999/11/27/medline PY - 1999/11/27/entrez SP - 12 EP - 5 JF - Forschende Komplementarmedizin JO - Forsch Komplementarmed VL - 6 Suppl 3 N2 - It is now known that there are at least two types of cannabinoid receptors. These are CB1 receptors, present mainly on central and peripheral neurones, and CB2 receptors, present mainly on immune cells. Endogenous cannabinoid receptor agonists ('endocannabinoids') have also been identified. The discovery of this 'endogenous cannabinoid system' has led to the development of selective CB1 and CB2 receptor ligands and fueled renewed interest in the clinical potential of cannabinoids. Two cannabinoid CB1 receptor agonists are already used clinically, as antiemetics or as appetite stimulants. These are D 9 - tetrahydrocannabinol (THC) and nabilone. Other possible uses for CB1 receptor agonists include the suppression of muscle spasm/spasticity associated with multiple sclerosis or spinal cord injury, the relief of chronic pain and the management of glaucoma and bronchial asthma. CB1 receptor antagonists may also have clinical applications, e. g. as appetite suppressants and in the management of schizophrenia or disorders of cognition and memory. So too may CB2 receptor ligands and drugs that activate cannabinoid receptors indirectly by augmenting endocannabinoid levels at cannabinoid receptors. When taken orally, THC seems to undergo variable absorption and to have a narrow 'therapeutic window' (dose range in which it is effective without producing significant unwanted effects). This makes it difficult to predict an oral dose that will be both effective and tolerable to a patient and indicates a need for better cannabinoid formulations and modes of administration. For the therapeutic potential of cannabis or CB1 receptor agonists to be fully exploited, it will be important to establish objectively and conclusively (a) whether these agents have efficacy against selected symptoms that is of clinical significance and, if so, whether the benefits outweigh the risks, (b) whether cannabis has therapeutic advantages over individual cannabinoids, (c) whether there is a need for additional drug treatments to manage any of the disorders against which cannabinoids are effective, and (d) whether it will be possible to develop drugs that have reduced psychotropic activity and yet retain the ability to act through CB1 receptors to produce their sought-after effects. SN - 1021-7096 UR - https://www.unboundmedicine.com/medline/citation/10575283/Cannabis_and_cannabinoids:_pharmacology_and_rationale_for_clinical_use_ L2 - https://medlineplus.gov/herbalmedicine.html DB - PRIME DP - Unbound Medicine ER -