footslogging away Nabilone Class: Antiemetics, Miscellaneous VA Class: GA605 Chemical Name: ( )-trans-3-(1,1-dimethylheptyl)-6,6a,7,8,10,10a-hexahydro-1-hydroxy-6-6-dimethyl-9H-dibenzo[b,d]pyran-9-one Molecular Formula: C 24 H 36 O 3 CAS Number: 51022-71-0 Brands: Cesamet Overview Side Effects Dosage Professional Interactions More Pregnancy Warnings User Reviews Support Group Q & A Introduction Antiemetic; a synthetic cannabinoid. 1 2 6 15 Uses for Nabilone Cancer Chemotherapy-induced Nausea and Vomiting Prevention of nausea and vomiting associated with cancer chemotherapy in patients who have failed to respond adequately to conventional antiemetic therapy. 1 2 3 4 5 8 10 11 15 ASCO does not consider cannabinoids (e.g., nabilone, dronabinol) appropriate first-line antiemetics for any group of patients receiving chemotherapy of high emetic risk and states that these drugs should be reserved for patients unable to tolerate or refractory to first-line agents (i.e., a type 3 serotonin [5-HT 3 ] receptor antagonist [e.g., dolasetron, granisetron, ondansetron, palonosetron] with dexamethasone and aprepitant). 11 14 Slideshow Juvenile Arthritis: The Big Disease In A Little Body Nabilone Dosage and Administration Administration Oral Administration Administer orally without regard to meals. 1 2 5 Has been administered IV; however, a parenteral preparation is not commercially available in the US. 1 2 6 Dosage Adults Cancer Chemotherapy-induced Nausea and Vomiting Oral Usual dose: 1 or 2 mg twice daily; administer initial dose 1 3 hours before chemotherapy. 1 2 May be administered 2 or 3 times daily during the entire chemotherapy cycle and for 48 hours after the last dose of chemotherapy in each cycle. 1 2 Initiate with the lower dosage (i.e., 1 mg twice daily) to minimize adverse effects, then increase dosage as necessary up to a maximum of 2 mg 3 times daily. 1 2 May administer a dose of 1 or 2 mg the night prior to chemotherapy. 1 2 Prescribing Limits Adults Cancer Chemotherapy-induced Nausea and Vomiting Oral Maximum: 2 mg 3 times daily. 1 2 Special Populations Hepatic Impairment No specific dosage recommendations at this time. 1 Renal Impairment No specific dosage recommendations at this time. 1 Geriatric Patients Select dosage with caution, usually initiating at the lower end of the recommended dosage range because of possible age-related decreases in hepatic, renal, and/or cardiac function; concomitant diseases and drug therapy; and possible increased sensitivity to adverse effects. 1 (See Geriatric Use under Cautions.) Cautions for Nabilone Contraindications Hypersensitivity to any cannabinoid. 1 2 Warnings/Precautions Warnings Effects of nabilone may persist for a variable and unpredictable period of time following oral administration. 1 2 3 5 12 CNS Effects CNS effects, including dizziness, drowsiness or sedation, euphoria (i.e., high ), ataxia, anxiety, disorientation, depression, hallucinations, and psychosis, reported. 1 2 4 5 6 7 8 12 Adverse psychiatric reactions can persist for 48 72 hours following discontinuance of nabilone. 1 2 5 12 Individual response and tolerance may vary; a responsible adult should supervise patients, particularly during initial therapy and during dosage adjustments. 1 2 Cardiovascular Effects May cause tachycardia and orthostatic hypotension. 1 2 3 4 5 6 8 12 Elevations in supine and standing heart rates also reported. 1 2 3 4 5 6 8 12 Individual response and tolerance may vary; a responsible adult should supervise patients, particularly during initial therapy and during dosage adjustments. 1 2 Carefully evaluate the potential risks and benefits of the drug; use with caution in geriatric patients and in patients with hypertension and/or cardiovascular disease. 1 2 4 12 (See Geriatric Use under Cautions.) General Precautions Psychiatric Disorders Use with caution in patients with current or history of psychiatric disorders (e.g., bipolar disorder, depression, schizophrenia); cannabinoid use may unmask the symptoms of these diseases. 1 2 Abuse Potential Marijuana contains an active compound similar to nabilone. 1 2 Use nabilone with caution in patients with history of substance abuse, including alcohol abuse or dependence and marijuana use. 1 2 Increased risk of substance abuse in patients with personal or family history of substance abuse or mental illness. 1 2 Monitor patients receiving nabilone for signs of excessive use, abuse, and misuse. 1 8 12 High potential for abuse. 1 2 Limit prescriptions to quantity necessary for a single cycle of chemotherapy (i.e., a few days); 1 2 not intended for use on an as-needed basis or as the initial prescribed antiemetic therapy. 1 2 15 Specific Populations Pregnancy Category C. 1 2 Lactation Not known whether nabilone is distributed into milk. 1 2 Avoid use in nursing women. 1 2 Pediatric Use Safety and effectiveness not established. 1 2 Caution is advised because of psychoactive effects. 1 2 Geriatric Use Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults. 1 2 Use with caution because of increased sensitivity to psychoactive effects and risk of elevated supine and standing heart rates and postural hypotension. 1 2 12 Hepatic Impairment Not studied in patients with hepatic impairment. 1 2 Renal Impairment Not studied in patients with renal impairment. 1 2 Common Adverse Effects Adverse effects may be similar to those of marijuana (cannabis) and other cannabinoids. 1 2 12 13 Drowsiness, vertigo, dry mouth, ataxia, euphoria (i.e., feeling high ), dysphoria, sleep disturbances, headache. 1 2 4 5 6 7 8 12 13 Interactions for Nabilone Nabilone is a synthetic cannabinoid; interactions reported with Cannabis sativa L (marijuana) also may occur with nabilone. 1 2 Extensively metabolized by multiple CYP isoenzymes. 1 2 Does not substantially inhibit CYP isoenzymes 1A2, 2A6, 2C19, 2D6, and 3A4; weak inhibitor of 2E1 and 3A4 isoenzymes and a moderate inhibitor of 2C8 and 2C9 isoenzymes. 1 2 Drugs Metabolized by Hepatic Microsomal Enzymes Inhibitors or inducers of CYP isoenzymes: possible altered nabilone metabolism. 1 2 Pharmacokinetic interaction with drugs metabolized by CYP isoenzymes unlikely because very low plasma nabilone concentrations are achieved with clinical use. 1 2 Protein-bound Drugs Possible displacement of other protein-bound drugs. 1 2 Monitor patients and adjust dosages as necessary. 1 2 Specific Drugs Drug Interaction Comments Alcohol Possible additive drowsiness and CNS depression; increase in the positive subjective mood effects reported with smoked marijuana 1 2 Avoid alcohol during therapy 1 2 Anticholinergic agents (e.g., antihistamines, atropine, scopolamine) Possible additive or super-additive anticholinergic effects (e.g., tachycardia, drowsiness) 1 2 Antidepressants, tricyclic (e.g., amitriptyline, amoxapine, desipramine) Possible additive tachycardia, hypertension, or drowsiness 1 2 Antipyrine Possible decreased antipyrine clearance 1 2 CNS depressants (e.g., antihistamines, barbiturates, benzodiazepines, buspirone, hypnotics, lithium, muscle relaxants, sedatives) Possible additive drowsiness and CNS depression 1 2 Possible decreased barbiturate clearance 1 2 Administer with caution 1 2 Disulfiram Reversible hypomanic reaction reported in a disulfiram-treated patient who smoked marijuana 1 2 Fluoxetine Hypomanic reaction reported in a fluoxetine-treated patient after smoking marijuana; symptoms resolved within 4 days 1 2 Naltrexone Possible enhanced effects of oral delta-9-tetrahydrocannabinol observed during opiate receptor blockade 1 2 Opiate agonists (e.g., meperidine, methadone, propoxyphene, tramadol) Possible additive drowsiness and CNS depression; possible cross-tolerance and potentiation of other pharmacologic effects 1 2 Sympathomimetic agents (e.g., amphetamines, cocaine) Possible additive hypertension, tachycardia, or cardiotoxicity 1 2 Theophylline Increased theophylline metabolism reported with marijuana smoking; similar to that reported following tobacco smoking 1 2 Nabilone Pharmacokinetics Absorption Bioavailability Appears to be completely absorbed from the GI tract after oral administration, with peak plasma concentrations achieved within 2 hours. 1 Food Food does not appear to significantly affect the rate or extent of absorption. 1 Distribution Extent Volume of distribution: Approximately 12.5 L/kg. 1 Elimination Metabolism Extensively metabolized, including metabolism via multiple CYP isoenzymes, to several metabolites; relative pharmacologic activities of the metabolites and the parent drug not established. 1 2 Elimination Route Following IV administration, nabilone and its metabolites are eliminated principally in feces (approximately 67%) and to a lesser extent in urine (approximately 22%) within 7 days. 1 2 Following oral administration, about 60% of nabilone and its metabolites were recovered in feces and about 24% in urine. 1 2 The principal excretory pathway appears to be the biliary system. 1 2 No substantial accumulation of nabilone observed after chronic oral administration, but metabolites may accumulate at concentrations in excess of the parent drug with repeated administration. 1 2 Half-life Approximately 2 hours. 1 Plasma half-life of total radioactivity (identified and unidentified metabolites) is approximately 35 hours. 1 Stability Storage Oral Capsules 25 C (may be exposed to 15 30 C). 1 Actions Exerts complex effects on CNS. 1 2 6 12 15 Antiemetic effect may be caused by interaction with the cannabinoid receptor system, including the cannabinoid 1 (CB 1 ) receptors in the central and peripheral nervous system. 1 2 12 15 Binds to cannabinoid 2 (CB 2 ) receptors in the spleen and other peripheral tissues, which may play a role in the immunosuppressive effects of cannabinoids. 2 12 15 Like other cannabinoids, may possess analgesic, antispasmodic, and muscle relaxant activity; however, further evaluation is necessary. 2 10 15 Advice to Patients Risk of additive or synergistic CNS depression during concurrent use with alcohol or other CNS depressants, including benzodiazepines and barbiturates. 1 2 Importance of avoiding alcohol and other CNS depressants during nabilone therapy. 1 2 Importance of avoiding driving, operating machinery, or performing hazardous tasks during nabilone therapy. 1 2 Importance of informing patients about possible changes in mood and other adverse behavioral effects of nabilone to avoid panic if such manifestations occur. 1 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as concomitant illnesses. 1 Importance of informing patients that they should remain under the supervision of a responsible adult during therapy. 1 2 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 1 Importance of informing patients of other important precautionary information. 1 2 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Subject to control under the Federal Controlled Substances Act of 1970 as a schedule II (C-II) drug. 1 2 Nabilone Routes Dosage Forms Strengths Brand Names Manufacturer Oral Capsules 1 mg Cesamet (C-II; with povidone) Valeant AHFS DI Essentials. Copyright 2017, Selected Revisions September 1, 2007. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. Valeant Pharmaceuticals International. Cesamet (nabilone) capsules prescribing information. Costa Mesa, CA; 2006 Jul. 2. Valeant Pharmaceuticals North America. Cesamet (nabilone) capsules, 1 mg: innovations in omnineuromodulation formulary dossier. Costa Mesa, CA; 2006 Jun 21. 3. Tramer MR, Carroll D, Campbell FA et al. Cannabinoids for control of chemotherapy induced nausea and vomiting: quantitative systematic review. Br Med J . 2001; 323:1-8. 4. Einhorn LH, Nagy C, Furnas B et al. Nabilone: an effective antiemetic in patients receiving cancer chemotherapy. J Clin Pharmacol . 1981; 21:64-9S. 5. Herman TS, Einhorn LH, Jones SE et al. Superiority of nabilone over prochlorperazine as an antiemetic in patients receiving cancer chemotherapy. N Engl J Med . 1979; 300:1295-7. [PubMed 375088] 6. Lemberger L, Rowe H. Clinical pharmacology of nabilone, a cannabinol derivative. Clin Pharmacol Ther . 1975; 18:720-6. [PubMed 1204278] 7. Talbott JA, Teague JW. Marijuana psychosis: acute toxic psychosis associated with the use of Cannabis derivatives. JAMA . 1969; 210:299-302. [PubMed 5394365] 8. Ahmedzai S, Carlyle DL, Calder IT et al. Anti-emetic efficacy and toxicity of nabilone, a synthetic cannabinoid, in lung cancer chemotherapy. Br J Cancer . 1983; 48:657-63. [PubMed 6315040] 9. Williamson EM, Evans FJ. Cannabinoids in clinical practice. Drugs . 2000; 60:1303-14. [PubMed 11152013] 10. Croxford JL. Therapeutic potential of cannabinoids in CNS disease. CNS Drugs . 2003; 17:179-202. [PubMed 12617697] 11. Kris MG, Hesketh PJ, Somerfield MR et al. American Society of Clinical Oncology guideline for antiemetics in oncology: update 2006. J Clin Oncol . 2006; 24:1-16. [PubMed 16330665] 12. Ashton CH. Adverse effects of cannabis and cannabinoids. Br J Anaesthesia . 1999; 83:637-49. 13. Herman TS, Jones SE, Dean J et al. Nabilone: a potent antiemetic cannabinol with minimal euphoria. Biomedicine . 1977; 27:331-4. [PubMed 606307] 14. Gralla RJ, Osoba D, Kris MG et al. Recommendations for the use of antiemetics: evidence-based, clinical practice guidelines. J Clin Oncol . 1999; 17:2971-94. [PubMed 10561376] 15. Ben Amar M. Cannabinoids in medicine: a review of their therapeutic potential. J Ethnopharmacol . 2006; 105:1-25. [PubMed 16540272] Next Interactions Print this page Add to My Med List More about nabilone Side Effects During Pregnancy Dosage Information Drug Interactions Support Group En Español 8 Reviews Add your own review/rating Drug class: miscellaneous antiemetics Consumer resources Nabilone Nabilone (Advanced Reading) Professional resources Nabilone (Wolters Kluwer) Other brands: Cesamet Related treatment guides Fibromyalgia Nausea/Vomiting, Chemotherapy Induced} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out 2 CSA Schedule High potential for abuse Approval History Drug history at FDA Drug Class Miscellaneous antiemetics Related Drugs Nausea / Vomiting, Chemotherapy Induced lorazepam , ondansetron , Zofran , Ativan , dexamethasone , metoclopramide , Reglan , Decadron , Marinol , dronabinol , Zofran ODT , Emend , Aloxi , granisetron , Varubi , palonosetron , Kytril , aprepitant , Akynzeo , fosaprepitant , Dexasone , Sancuso , More... Nabilone Rating 8 User Reviews 7.4 /10 8 User Reviews 7.4 Rate it!} } seems to be
fulfillment Nabilone practice
EmoticonEmoticon