Pharmacology

Cannabinoids

Correct

Cannabinoids are endogenous, plant-derived and synthetic agents with pharmacological activity at the G-protein coupled cannabinoid receptors (CB1 and CB2).

Reasoning

Plant-derived cannabinoids are termed phytocannabinoids.

The phytocannabinoids are pre-cursor substances synthesised by the Cannabis sativa L. plant, including tetrahydrocannabinolic acid (THCA) and cannabidiolic acid (CBDA). Heating to temperatures above 100ºC causes decarboxylation (releasing CO2), converting the acids into their bioactive forms, delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD). THC and CBD interact with cannabinoid receptors (CB) within the human endocannabinoid system (ECS).

Incorrect

Cannabinoids are endogenous, plant-derived and synthetic agents with pharmacological activity at the G-protein coupled cannabinoid receptors (CB1 and CB2).

Reasoning

Plant-derived cannabinoids are termed phytocannabinoids.

The phytocannabinoids are pre-cursor substances synthesised by the Cannabis sativa L. plant, including tetrahydrocannabinolic acid (THCA) and cannabidiolic acid (CBDA). Heating to temperatures above 100ºC causes decarboxylation (releasing CO2), converting the acids into their bioactive forms, delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD). THC and CBD interact with cannabinoid receptors (CB) within the human endocannabinoid system (ECS).

Endocannabinoid System

Correct

The ECS contains cannabinoid receptors and is involved in a host of homeostatic and physiologic functions.

Reasoning

The human endocannabinoid system (ECS) contains cannabinoid receptors (CB) which are activated by naturally produced endocannabinoids.

The ECS plays a critical role in the nervous system and regulates multiple physiological processes, including the adjustment of the response to pain, appetite, digestion, sleep, mood, and memory.

The ECS also influences seizure thresholds, coordination, sensory integration (touch, balance, sense of space), and other processes such as the immune system and inflammation, heart function, fertility, bone physiology, the central stress response system, neural development, and eye pressure.

Incorrect

The ECS contains cannabinoid receptors and is involved in a host of homeostatic and physiologic functions.

Reasoning

The human endocannabinoid system (ECS) contains cannabinoid receptors (CB) which are activated by naturally produced endocannabinoids.

The ECS plays a critical role in the nervous system and regulates multiple physiological processes, including the adjustment of the response to pain, appetite, digestion, sleep, mood, and memory.

The ECS also influences seizure thresholds, coordination, sensory integration (touch, balance, sense of space), and other processes such as the immune system and inflammation, heart function, fertility, bone physiology, the central stress response system, neural development, and eye pressure.

Cannabinoid Receptors

Correct

The CB1 receptors are widely expressed in areas of the brain controlling pain, appetite, emotion and nausea.

Reasoning

Cannabinoid receptors (CB) belong to the superfamily of the G-protein-coupled receptors that mediate the pharmacological effects of phyto-cannabinoids, endocannabinoids, and synthetic cannabimimetic compounds.

The CB1 isoform is highly expressed in the central nervous system. It is thought to be the most widely expressed G-protein coupled receptor in the brain. Indeed, the CB1 receptors are concentrated in areas controlling pain, appetite, emotion and nausea, corresponding to the most prominent behavioural effects. CB1 receptors mediate most, if not all, of the psychoactive effects of THC and related compounds.

Incorrect

The CB1 receptors are widely expressed in areas of the brain controlling pain, appetite, emotion and nausea.

Reasoning

Cannabinoid receptors (CB) belong to the superfamily of the G-protein-coupled receptors that mediate the pharmacological effects of phyto-cannabinoids, endocannabinoids, and synthetic cannabimimetic compounds.

The CB1 isoform is highly expressed in the central nervous system. It is thought to be the most widely expressed G-protein coupled receptor in the brain. Indeed, the CB1 receptors are concentrated in areas controlling pain, appetite, emotion and nausea, corresponding to the most prominent behavioural effects. CB1 receptors mediate most, if not all, of the psychoactive effects of THC and related compounds.

THC

Correct

THC is psychoactive, is euphorigenic, and has intoxicating* effects at high doses.

Reasoning

THC is psychoactive, is euphorigenic, and has intoxicating* effects at high doses. Synthetic and semi-synthetic cannabinoids mimic the effects of THC. In the body, THC is converted to a potent psychoactive metabolite, 11-hydroxy-THC (11-OHTHC). THC activates both CB1 and CB2 receptors (as a partial agonist with high affinity), which in turn influences the activity of various physiological systems.

* WHO. ICD-10: Intoxication is a transient condition that follows the administration of a psychoactive substance and results in disturbances in the level of consciousness, cognition, perception, judgement, or behaviour, or other psycho-physiological functions and responses.

Incorrect

THC is psychoactive, is euphorigenic, and has intoxicating effects at high doses.

Reasoning

THC is psychoactive, is euphorigenic, and has intoxicating* effects at high doses. Synthetic and semi-synthetic cannabinoids mimic the effects of THC. In the body, THC is converted to a potent psychoactive metabolite, 11-hydroxy-THC (11-OHTHC). THC activates both CB1 and CB2 receptors (as a partial agonist with high affinity), which in turn influences the activity of various physiological systems.

* WHO. ICD-10: Intoxication is a transient condition that follows the administration of a psychoactive substance and results in disturbances in the level of consciousness, cognition, perception, judgement, or behaviour, or other psycho-physiological functions and responses.

CBD

Correct

CBD is psychoactive but does not have intoxicating effects.

Reasoning

CBD, by comparison to THC, has less affinity for the CB1 and CB2 receptors and works to partly block receptor activity (as a partial antagonist).

Incorrect

CBD is psychoactive but does not have intoxicating effects.

Reasoning

CBD, by comparison to THC, has less affinity for the CB1 and CB2 receptors and works to partly block receptor activity (as a partial antagonist).

Route of Administration

Correct

The two major administration routes are oromucosal and inhalation.

Reasoning

The pharmacokinetics of THC and CBD varies as a function of its route of administration. The management of the dose is critical to balance the desired therapeutic effects against the prevention of side effects.

There are two major administration routes:

• By inhalation – pulmonary absorption, and
• By mouth – oromucosal solutions, sprays and wafers with sublingual or buccal absorption, or ingested oral solutions and capsules with small intestine absorption.

Incorrect

The two major administration routes are oromucosal and inhalation.

Reasoning

The pharmacokinetics of THC and CBD varies as a function of its route of administration. The management of the dose is critical to balance the desired therapeutic effects against the prevention of side effects.

There are two major administration routes:

• By inhalation – pulmonary absorption, and
• By mouth – oromucosal solutions, sprays and wafers with sublingual or buccal absorption, or ingested oral solutions and capsules with small intestine absorption.