Cesamet - General Information
Cesamet is a synthetic cannabinoid with therapeutic use as an antiemetic and as an adjunct analgesic for neuropathic pain. It is a synthetic cannabinoid, which mimics the main ingredient of marijuana (THC) but it has more predictable side effects and causes no or minimal euphoria. Cesamet is not derived from the cannabis plant as is dronabinol.
In Canada, the United States, the United Kingdom and Mexico, nabilone is marketed as Cesamet. It was approved in 1985 by the United States FDA for treatment of chemotherapy-induced nausea and vomiting that has not responded to conventional antiemetics. Though it was approved by the FDA in 1985, the drug only began marketing in the United States in 2006. It is also approved for use in treatment of anorexia and weight loss in patients with AIDS.
Although it doesn't have the official indication (except in Mexico), nabilone is widely used as an adjunct therapy for chronic pain management. Numerous trials and case studies have demonstrate various benefits for condition such as fibromyalgia and multiple scerosis.
Cesamet is a racemate consisting of the (S,S) and the (R,R) isomers ("trans").
Pharmacology of Cesamet
Cesamet is a cannabinoid with therapeutic uses. It is an analog of dronabinol (also known as tetrahydrocannabinol or THC), the psychoactive ingredient in cannabis. It is reserved for use in individuals who do not respond to the more commonly used anti-emetics. This is mainly because cannabinoids have potential adverse effects similar to that of cannabis and may cause changes in mood and behaviour.
Cesamet for patients
Nabilone may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks such as operating machinery or driving a car; therefore the patient should be advised accordingly. The effects of Nabilone may persist for a variable and unpredictable period of time following its oral administration. Adverse psychiatric reactions can persist for 48 to 72 hours following cessation of treatment.
Nabilone is an abusable substance, capable of producing subjective side-effects, such as euphoria or "high", at therapeutic doses. Prescriptions should be limited to the amount necessary for a single cycle of chemotherapy (ie., a few days). The physical dependence capability of Nabilone is unknown. Patients who participated in clinical trials, up to 5 days duration, showed no withdrawal symptoms on cessation of dosing.
Nabilone should be administered with caution to patients who are taking other psychoactive drugs or CNS depressants, including alcohol, barbiturates and narcotic analgesics, or to those with a history of psychiatric disorder (including manic-depressive illness and schizophrenia). Nabilone has been shown to have an additive CNS depressant effect when given with either diazepam, secobarbitone sodium, alcohol or codeine.
Nabilone is contra-indicated in patients with a known allergy to cannabinoid agents and when the nausea and vomiting arises from any cause other than cancer chemotherapy.
Additional information about Cesamet
Cesamet Indication: Used for the control of nausea and vomiting, caused by chemotherapeutic agents used in the treatment of cancer, in patients who have failed to respond adequately to conventional antiemetic treatments.
Mechanism Of Action: The mode of action of nabilone has been studied in cats and dogs. Although its anti-emetic action is not yet fully understood, it is apparent that there are a number of points in the control systems of the body at which Cesamet could block the emetic mechanism. It is likely that nabilone exerts its actions via binding to the cannabinoid receptors.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Nabilone
Synonyms: Not Available
Drug Category: Anti-anxiety Agents; Antiemetics
Drug Type: Small Molecule; Approved; Investigational
Absorption: Rapidly absorbed from the gastrointestinal tract following oral administration.
Toxicity (Overdose): Symptoms of overdose include difficulty in breathing, hallucinations, mental changes (severe), nervousness or anxiety (severe). Monkeys treated with Nabilone at doses as high as 2mg/kg/day for a year experienced no significant adverse events. This result contrasts with the finding in a planned 1-year dog study that was prematurely terminated because of deaths associated with convulsions in dogs receiving as little as 0.5mg/kg/day. The earliest deaths, however, occurred at 56 days in dogs receiving 2mg/kg/day. The unusual vulnerability of the dog is not understood; it is hypothesised, however, that the explanation lies in the fact that the dog differs markedly from other species (including humans) in its metabolism of Nabilone.
Protein Binding: Not Available
Biotransformation: Hepatic. Two metabolic pathways have been suggested. The major pathway probably involves the direct oxidation of Nabilone to produce hydroxylic and carboxylic analogues. These compounds are thought to account for the remaining plasma radioactivity when carbinol metabolites have been extracted.
Half Life: 2 hours, with metabolites around 35 hours.
Dosage Forms of Cesamet: Capsule Oral
Chemical IUPAC Name: (6aR,10aR)-1-hydroxy-6,6-dimethyl-3-(2-methyloctan-2-yl)-7,8,10,10a-tetrahydro-6aH-benzo[c]chromen-9-one
Chemical Formula: C24H36O3
Nabilone on Wikipedia: https://en.wikipedia.org/wiki/Nabilone
Organisms Affected: Humans and other mammals