Nabilone
Drug Info:
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Nabilone
Brand names: Cesamet™
- Drug Forms:
- Nabilone capsules (below)
- Nabilone Oral capsule
- Espa�ol:
- Nabilón, Cápsula oral
Nabilone capsules
What are Nabilone capsules?
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:• a history of drug or alcohol abuse
• dizziness or fainting spells on standing
• heart disease, including angina or irregular heart rate
• high or low blood pressure
• kidney disease
• liver disease
• mental health problems (schizophrenia, mania, depression)
• an unusual reaction to Nabilone, marijuana, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should this medicine be used?
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
What if I miss a dose?
What drug(s) may interact with Nabilone?
• caffeine
• cocaine
• disulfiram
• dronabinol, THC
• medicines for colds and breathing difficulties
• ritonavir
• theophylline
Because nabilone can cause drowsiness, other medicines that also cause drowsiness may increase this effect. Some medicines that cause drowsiness are:
• alcohol-containing medicines or alcoholic drinks
• barbiturates such as phenobarbital
• certain antihistamines used in cold medicines
• certain medicines used to treat nausea/vomiting
• muscle relaxants
• medicines for anxiety or sleeping problems
• some medicines for pain such as codeine, morphine, nalbuphine, propoxyphene, and tramadol
• some medications for mental health disorders (depression, mania, psychosis, schizophrenia)
• some medications for Parkinson's disease
Ask your prescriber or health care professional about other medicines that may increase the effect of nabilone.
Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking Nabilone?
Do not smoke marijuana while you are taking this medicine. Nabilone is similar to one of the active substances found in marijuana. You are at increased risk of serious heart and/or nervous system side effects if these drugs are used together.
What side effects may I notice from receiving Nabilone?
Side effects that you should report to your prescriber or health care professional as soon as possible:• changes in blood pressure (lower or higher than usual)
• chest pain or shortness of breath
• facial redness or swelling
• fast or irregular heartbeat (palpitations)
• fainting spells, lightheadedness
• hallucinations (seeing or hearing things that are not really there)
• panic reactions
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• anxiety or nervousness
• changes in vision
• confusion
• drowsiness or dizziness
• dry mouth
• headache
• impaired coordination
• increased or decreased appetite
• irritability
• loss of memory
• mood changes (especially improved mood or euphoria)
• nausea/vomiting
• weakness
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from moisture. Keep container tightly closed. Throw away any unused medicine after the expiration date.
Last updated: 5/30/2006 1:55:00 PM
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford A-Z of Medicinal Drugs:
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nabilone
A synthetic derivative of cannabis that is used to prevent or treat the nausea and vomiting caused by cytotoxic drug treatment for cancer. It is used in patients who have not responded to other antiemetics, but treatment needs to be carefully supervised, since some people can experience disorientation and mood changes as side effects (see below). Nabilone is available as capsules on prescription only.
Side effects:
include drowsiness, vertigo, euphoria, shaky movements, dry mouth, visual disturbances, difficulty in concentrating, sleep disturbances, confusion, disorientation, hallucinations, psychosis, depression, lack of coordination, tremor, a fast heart rate, and loss of appetite. Mood changes and other mental side effects may persist for up to three days after stopping the treatment.
Precautions:
nabilone should not be taken by people with severe liver disease or by women who are breastfeeding. It should be used with caution in people with a history of psychiatric disorders, in the elderly, and in pregnant women. Nabilone may affect driving ability, and its sedative effects are increased by alcohol.
Interactions with other drugs:
Anxiolytics and hypnotics: enhance the sedative effects of nabilone.
| Nystaform-HC, Nystaform, Nuvelle Continuous | |
| nabumetone, nadolol, nafarelin |
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(năb'ə-lōn')
n.
n.
A synthetic cannabinoid used in the treatment of nausea and vomiting associated with cancer chemotherapy.
Wikipedia on Answers.com:
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Nabilone
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|---|---|
| Systematic (IUPAC) name | |
| (6aR,10aR)-rel-1-hydroxy-6,6-dimethyl-3-(2-methyloctan-2-yl)- | |
| Clinical data | |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a607048 |
| Pregnancy cat. | C (US) |
| Legal status | Schedule II (US) |
| Routes | Oral form (PO)- capsule |
| Pharmacokinetic data | |
| Bioavailability | 20% after first-pass by the liver |
| Protein binding | similar to THC (+/-97%) |
| Half-life | 2 hours, with metabolites around 35 hours. |
| Identifiers | |
| CAS number | 51022-71-0  |
| ATC code | A04AD11 |
| PubChem | CID 5284592 |
| DrugBank | DB00486 |
| ChemSpider | 4447641 |
| UNII | 2N4O9L084N |
| KEGG | D05099 |
| ChEMBL | CHEMBL947 |
| Chemical data | |
| Formula | C24H36O3 |
| Mol. mass | 372.541 g/mol |
| SMILES | eMolecules & PubChem |
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Nabilone 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 chemical compound of cannabis (THC). Chemically, nabilone is similar to the active ingredient found in naturally occurring Cannabis sativa L. [1]
In Canada, the United States, the United Kingdom and Mexico, nabilone is marketed as Cesamet. It was approved in 1985 by the U.S. Food and Drug Administration (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 demonstrated various benefits for conditions such as fibromyalgia[2] and multiple sclerosis.[3]
Nabilone is a racemic mixture consisting of the (S,S) and the (R,R) isomers ("trans").
Clinical trials
The main settings that have seen published clinical trials of nabilone include movement disorders such as Parkinson's syndrome, chronic pain, dystonia and spasticity neurological disorders, fibromyalgia, multiple sclerosis, and the nausea of cancer chemotherapy. Nabilone is also effective in the treatment of inflammatory bowel disease, especially ulcerative colitis. Medical marijuana patients report that nabilone is more similar in effect to CBD than THC, indicating that it has more of a therapeutic effect on the body than a "high" effect on the mind.
A study comparing nabilone with metoclopramide, conducted before the development of modern 5-HT3 antagonist anti-emetics such as ondansetron, revealed that patients taking cisplatin chemotherapy preferred metoclopramide, while patients taking carboplatin chemotherapy preferred nabilone to control nausea and vomiting. [4] Another study compared nabilone alone to nabilone with dexamethasone. The study found that the combination worked better than the single medication. [5] An older study revealed that nabilone was more effective than prochlorperazine in controlling nausea, though in this study, only 9% of nabilone patients had complete resolution of symptoms. [6] A follow-up to this study revealed similar findings. [7]
One study compared the efficacy and tolerability of nabilone with that of dihydrocodeine in the treatment of neuropathic pain.[8] The authors found that nabilone was not as effective as dihydrocodeine in controlling pain, and caused a higher incidence of minor adverse drug reactions than did dihydrocodeine. One critic of the study has suggested that nabilone might be best suited for the treatment of patients suffering from central and spasticity-related pain, for which there is stronger evidence for the benefits of cannabinoid therapy; however, these patients made up only a small fraction of the study's population, and the study was not designed to identify subgroups which might have responded more favorably to treatment than others.[9]
A clinical trial performed in Canada reviewed the use of nabilone to treat nightmares in individuals suffering from post-traumatic stress syndrome[10]. The study found that nighttime administration of nabilone reduced the frequency and/or intensity of nightmares in 34 out of 47 (72%) of patients, with 28 reporting complete cessation of nightmares[10]. This study is limited to the extent that there was no placebo control, but warrants future investigation into the use of cannabinoid therapy in the treatment of post-traumatic stress syndrome and other disorders involving recurrent nightmares. As endocannabinoids play a significant role in regulating long-term depression, perhaps downregulating the CB1 system can help remove the highly potentiated, hippocampal/amydygalia memories of the fear. At the very least, CB1 agonists make one less likely to remember a dream, or even make REM sleep happen without significant involvement of the limbic system.
References
- ^ "How to use Cesamet". Artek LLC. 2008. http://patientsville.com/labels/cesamet_label.htm.
- ^ Skrabek RQ, Galimova L, Ethans K, Perry D (2008). "Nabilone for the treatment of pain in fibromyalgia". J Pain 9 (2): 164–73. doi:10.1016/j.jpain.2007.09.002. PMID 17974490.
- ^ Wissel J, Haydn T, Müller J, Brenneis C, Berger T, Poewe W, Schelosky LD. (2006). "Low dose treatment with the synthetic cannabinoid Nabilone significantly reduces spasticity-related pain : a double-blind placebo-controlled cross-over trial". J Neurol. 253 (10): 1337–41. doi:10.1007/s00415-006-0218-8. PMID 16988792.
- ^ Cunningham D, Bradley C, Forrest G, Hutcheon A, Adams L, Sneddon M, Harding M, Kerr D, Soukop M, Kaye S (1988). "A randomized trial of oral nabilone and prochlorperazine compared to intravenous metoclopramide and dexamethasone in the treatment of nausea and vomiting induced by chemotherapy regimens containing cisplatin or cisplatin analogues". Eur J Cancer Clin Oncol 24 (4): 685–9. doi:10.1016/0277-5379(88)90300-8. PMID 2838294.
- ^ Niiranen A, Mattson K (1987). "Antiemetic efficacy of nabilone and dexamethasone: a randomized study of patients with lung cancer receiving chemotherapy". Am J Clin Oncol 10 (4): 325–9. doi:10.1097/00000421-198708000-00014. PMID 3039831.
- ^ Herman T, Einhorn L, Jones S, Nagy C, Chester A, Dean J, Furnas B, Williams S, Leigh S, Dorr R, Moon T (1979). "Superiority of nabilone over prochlorperazine as an antiemetic in patients receiving cancer chemotherapy". N Engl J Med 300 (23): 1295–7. doi:10.1056/NEJM197906073002302. PMID 375088.
- ^ Einhorn L, Nagy C, Furnas B, Williams S (1981). "Nabilone: an effective antiemetic in patients receiving cancer chemotherapy". J Clin Pharmacol 21 (8–9 Suppl): 64S–69S. PMID 6271844.
- ^ Frank B, Serpell MG, Hughes J, Matthews JN, Kapur D. "Comparison of analgesic effects and patient tolerability of nabilone and dihydrocodeine for chronic neuropathic pain: randomised, crossover, double blind study." British Medical Journal. 2008 Jan 8. [Epub ahead of print]. PMID 18182416. doi:10.1136/bmj.39429.619653.80
- ^ Cohen SP. "Cannabinoids for chronic pain." British Medical Journal. 2008 Jan 8. [Epub ahead of print]. PMID 18182415. doi:10.1136/bmj.39434.444583.80
- ^ a b Fraser, GA (2009). "The Use of a Synthetic Cannabinoid in the Management of Treatment-Resistant Nightmares in Posttraumatic Stress Disorder (PTSD)". CNS Neurosci Ther 15 (1): 84–88. doi:10.1111/j.1755-5949.2008.00071.x. PMID 19228182.
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