Nabilone

What is Nabilone?

• Nabilone (Cesamet) is an orally active synthetic cannabinoid which, like other cannabinoids, has complex effects on the central nervous system (CNS) used to treat nausea and vomiting caused by cancer chemotherapy in people who have already taken other medications to treat this type of nausea and vomiting without good results.

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Nabilone

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What are the uses of this medicine?

• Nabilone (Cesamet) is used for the treatment of the nausea and vomiting associated with cancer chemotherapy in patients who have failed to respond adequately to conventional antiemetic treatments.

Limitations of use:

• Nabilone, which is controlled in Schedule II of the Controlled Substances Act. Schedule II substances have a high potential for abuse.
• Prescriptions for Cesamet should be limited to the amount necessary for a single cycle of chemotherapy (i.e., a few days).
• Cesamet capsules are not intended to be used on as needed basis or as a first antiemetic product prescribed for a patient.

How does this medicine work?

• Nabilone (Nab’ i lone) is a synthetic cannabinoid which is similar to the principal psychoactive constituent of the marijuana plant (Cannabis sativa).
• Nabilone is a partial agonist of the cannabinoid receptors which are found in the central nervous system (CB1 receptor), but also peripherally (largely CB2 receptors).
• Activation of CB receptors results in effects on appetite, mood, cognition, memory and perception.
• Nabilone therapy has been shown to decrease nausea and vomiting in patients undergoing cancer chemotherapy.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• who has a history of hypersensitivity to any cannabinoid.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• antidepressants, including amitriptyline (in Limbitrol), amoxapine, desipramine (Norpramin) and fluoxetine (Prozac)
• antihistamines
• amphetamines such as amphetamine (in Adderall), dextroamphetamine (Dexedrine, Dextrostat, in Adderall), and methamphetamine (Desoxyn)
• anticoagulants ('blood thinners') such as warfarin (Coumadin); atropine (Atropen, in Hycodan, in Lomotil, in Tussigon)
• codeine (in some cough syrups and pain relievers); barbiturates, including phenobarbital (Luminal) and secobarbital (Seconal, in Tuinal)
• buspirone (BuSpar)
• diazepam (Valium)
• digoxin (Lanoxicaps, Lanoxin)
• disulfiram (Antabuse)
• ipratropium (Atrovent)
• lithium (Eskalith, Lithobid)
• medications for anxiety, asthma, colds, irritable bowel disease, motion sickness, Parkinson's disease, seizures, ulcers, or urinary problems
• muscle relaxants
• naltrexone (Revia, Vivitrol)
• narcotic medications for pain
• propranolol (Inderal)
• scopolamine (Transderm-Scop)
• sedatives
• sleeping pills
• tranquilizers
• theophylline (TheoDur, Theochron, Theolair)

Is this medicine FDA approved?

• Nabilone was approved for use in the United States in 1985 and current indications are prevention of cancer chemotherapy associated nausea and vomiting.
• Nabilone is available as 1 mg capsules under the brand name Cesamet.

How should this medicine be used?

Recommended dosage:

• The usual adult dosage is 1 or 2 mg 2 times a day.
• On the day of chemotherapy, the initial dose should be given 1 to 3 hours before the chemotherapeutic agent is administered.
• To minimize side effects, it is recommended that the lower starting dose be used and that the dose be increased as necessary.
• A dose of 1 or 2 mg the night before may be useful.
• The maximum recommended daily dose is 6 mg given in divided doses 3 times a day.

Administration:

• Nabilone comes as a capsule to take by mouth. It is usually taken with or without food two to three times a day during a cycle of chemotherapy. Treatment with nabilone should begin 1 to 3 hours before the first dose of chemotherapy and may be continued for up to 48 hours after the end of the chemotherapy cycle. Take nabilone at around the same times every day.
• Your doctor will probably start you on a low dose of nabilone and may gradually increase your dose if needed.
• Nabilone helps control nausea and vomiting caused by cancer chemotherapy when taken as directed.
• Always take nabilone according to the schedule prescribed by your doctor even if you are not experiencing nausea or vomiting.
• Nabilone may be habit-forming.
• Do not take a larger dose, take it more often, or take it for a longer period of time than prescribed by your doctor.
• Call your doctor if you find that you want to take extra medication.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Cesamet capsule contains 1 mg of nabilone

This medicine is available in fallowing brand namesː

• Cesamet

What side effects can this medication cause?

The most common side effects of this medicine include:

• drowsiness, vertigo, dry mouth, euphoria (feeling “high”), ataxia, headache, and concentration difficulties

Additional side effects may include:

• Euphoria
• Sleep Disturbance
• Dysphoria
• Nausea
• Disorientation
• Depersonalization
• Drowsiness
• Depression
• Visual Disturbance
• Concentration Difficulties
• Hypotension
• Asthenia
• Anorexia
• Headache
• Sedation
• Increased Appetite

What special precautions should I follow?

• The effects of Cesamet 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.
• Cesamet has the potential to affect the CNS, which might manifest itself in dizziness, drowsiness, euphoria “high”, ataxia, anxiety, disorientation, depression, hallucinations and psychosis.
• Cesamet can cause tachycardia and orthostatic hypotension.
• Patients should remain under supervision of a responsible adult especially during initial use of Cesamet and during dose adjustments.
• Patients receiving treatment with Cesamet should be specifically warned not to drive, operate machinery, or engage in any hazardous activity while receiving Cesamet.
• Cesamet should not be taken with alcohol, sedatives, hypnotics, or other psychoactive substances because these substances can potentiate the central nervous system effects of nabilone.
• Since Cesamet can elevate supine and standing heart rates and cause postural hypotension, it should be used with caution in the elderly, and in patients with hypertension or heart disease.
• Cesamet should also be used with caution in patients with current or previous psychiatric disorders, (including manic depressive illness, depression, and schizophrenia) as the symptoms of these disease states may be unmasked by the use of cannabinoids.
• Cesamet should be used with caution in individuals receiving concomitant therapy with sedatives, hypnotics, or other psychoactive drugs because of the potential for additive or synergistic CNS effects.
• Cesamet should be used with caution in patients with a history of substance abuse, including alcohol abuse or dependence and marijuana use, since Cesamet contains a similar active compound to marijuana.
• Cesamet should be used with caution in pregnant patients, nursing mothers, or pediatric patients because it has not been studied in these patient populations.
• Nabilone is associated with a minimal rate of serum enzyme elevations during therapy and has not been linked to cases of clinically apparent liver injury with jaundice.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• psychiatric symptoms
• hypertension
• hypotension
• Tachycardia
• orthostatic hypotension
• hallucinations
• anxiety reactions
• respiratory depression
• coma

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• If psychotic episodes occur, the patient should be managed conservatively, if possible.
• For moderate psychotic episodes and anxiety reactions, verbal support and comforting may be sufficient.
• In more severe cases, antipsychotic drugs may be useful.
• Protect the patient’s airway and support ventilation and perfusion.
• Monitor and maintain, within acceptable limits, the patient’s vital signs, blood gases, serum electrolytes, as well as other laboratory values and physical assessments.
• Absorption of drugs from the gastrointestinal tract may be decreased by giving activated charcoal, which, in many cases, is more effective than [[]]emesis or lavage; consider charcoal instead of or in addition to gastric emptying.
• Repeated doses of charcoal over time may hasten elimination of some drugs that have been absorbed.
• Safeguard the patient’s airway when employing gastric emptying or charcoal.
• The use of forced diuresis, peritoneal dialysis, hemodialysis, charcoal hemoperfusion, or cholestyramine has not been reported.
• In the presence of normal renal function, most of a dose of nabilone is eliminated through the biliary system.
• Treatment for respiratory depression and comatose state consists in symptomatic and supportive therapy.
• Particular attention should be paid to the occurrence of hypothermia.
• If the patient becomes hypotensive, consider fluids, inotropes, and/or vasopressors.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies in pregnant women.
• Because animal studies cannot rule out the possibility of harm, Cesamet should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• Safety and effectiveness have not been established in patients younger than 18 years of age.
• Caution is recommended in prescribing Cesamet to children because of psychoactive effects.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• NABILONE

Inactive Ingredients:

• FD&C BLUE NO. 2
• FERRIC OXIDE RED
• GELATIN, UNSPECIFIED
• TITANIUM DIOXIDE

Who manufactures and distributes this medicine?

Distributed by:

• Bausch Health US, LLC
• Bridgewater, NJ USA

Manufactured by:

• Bausch Health Companies Inc.
• Laval, Quebec, Canada

• Cesamet is a trademark of Bausch Health Companies Inc. or its affiliates.

What should I know about storage and disposal of this medication?

• Store at controlled room temperature 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F).

Antidiarrheal agents

Antidiarrheal agents include bulk forming agents, hydroscopic agents, bile acid resins, bismuth, inhibitors of intestinal motility, non-absorbed antibiotics and hormones. Bulk forming agents include methylcellulose; hydroscopic agents include pectin and kaolin; bile acid resins are cholestyramine, colestipol and colesevalam; inhibitors of intestinal motility include opioids such as diphenoxylate and loperamide. Antibiotics include rifamycin and rifaximin which are non-absorbed and are used for travelers' diarrhea. Hormones with antidiarrheal activity include octretide and somatostatin. Most antidiarrheal agents are active locally in the small intestine and colon and are largely not absorbed. Some, however, have been implicated in rare causes of liver injury (senna, cascara, cholestyramine). Telotristat is a relatively new agent that inhibits the synthesis of serotonin and is used specifically for the diarrhea of carcinoid syndrome.

• Cholestyramine
• Colesevelam
• Colestipol
• Crofelemer
• Difenoxin
• Diphenoxylate
• Kaolin
• Loperamide
• Methylcellulose
• Octreotide
• Pectin
• Rifamycin
• Rifaximin
• Somatostatin
• Telotristat

Antiemetics are a diverse group of medications that act at different points in the pathways that regulate nausea and vomiting. These include antihistamines, anticholinergic agents, phenothiazines, serotonin type 3 receptor blockers, centrally acting benzamides, cannabinoid receptor agonists, substance P antagonists and miscellaneous.

Anticholinergic Agents

• Hyoscyamine, Methscopolamine, Scopolamine

Antihistamines

• Cyclizine, Dimenhydrinate, Hydroxyzine, Meclizine, and Promethazine

Cannabinoid Receptor Agonists

• Dronabinol, Nabilone, Tetrahydrocannabinol
• Phenothiazines [See Antipsychotic Agents]
• Chlorpromazine, Prochlorperazine

Serotonin 5-HT3 Receptor Antagonists

• Alosetron, Dolasetron, Granisetron, Ondansetron, Palonosetron

Substance P/Neurokinin 1 Receptor Antagonists

• Aprepitant, Fosaprepitant, Rolapitant

Miscellaneous

• Dexamethasone, Metoclopramide, Trimethobenzamide

Acid peptic disease/antiulcer agents that include antacids, the histamine type 2 receptor blockers (H2 blockers), and the proton pump inhibitors (PPIs). These agents are some of the most commonly taken medications and are very well tolerated, most being available both by prescription and over-the-counter. While many of these drugs are approved for use in duodenal and gastric ulcer disease, their major use is for acid reflux and indigestion.

Histamine H2 Receptor Antagonists (H2 Blockers) Cimetidine, Famotidine, Nizatidine, Ranitidine

Proton Pump Inhibitors

• Dexlansoprazole, Esomeprazole, Lansoprazole, Omeprazole, Pantoprazole, Rabeprazole

Cathartics, laxatives or agents for constipation include bulk forming agents, osmotic agents, stool wetting agents, nonspecific stimulants, prokinetic agents and agents that increase fluid secretion. Many of these therapies are not systemically absorbed and none are considered particularly hepatotoxic. Naldemedine and naloxegol are opioid antagonists and are used to treat the constipation associated with opioid use.

• Bisacodyl
• Cascara Sagrada
• Castor Oil
• Docusate
• Fiber, Bran
• Lactulose
• Magnesium Sulfate
• Methylcellulose
• Naldemedine (Opioid Antagonist)
• Naloxegol (Opioid Antagonist)
• Plecanatide (for Chronic Idiopathic Constipation)
• Prucalopride (for Chronic Idiopathic Constipation)
• Senna

Inflammatory bowel disease encompasses several disorders, most commonly ulcerative colitis and Crohn colitis. Agents can be classified as 5-aminosalicyclic acid (5-ASA) based agents, immunosuppressive drugs, antitumor necrosis factor agents, corticosteroids, antibiotics and miscellaneous.

5-Aminosalicyclic Acid (5-ASA) Derivatives

• Balsalazide, Mesalamine, Olsalazine, Sulfasalazine

Immunosuppressive Agents

• Azathioprine, Mercaptopurine, Methotrexate

Tumor Necrosis Factor Antagonists

• Adalimumab, Certolizumab, Golimumab, Infliximab

Miscellaneous

• Metronidazole, Natalizumab, Vedolizumab

Irritable Bowel Syndrome Agents Antimuscarinics/Antispasmodics [See Anticholinergic agents

• Dicyclomine, Glycopyrrolate, Hyoscyamine, Methscopolamine

Prokinetic Agents - See Serotonin 5-ht4 receptor agonists Alosetron, Cisapride, Domperidone, Linaclotide, Lubiprostone, Metoclopramide, Plecanatide, Prucalopride, Tegaserod

Other

• Eluxadoline

• Dailymed label info on Nabilone
• FDA Nabilone

Nabilone Resources
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