Dolasetron

What is Dolasetron?

• Dolasetron (Anzemet) is a selective serotonin 5-HT3 receptor antagonists used an antinauseant and antiemetic agent.

Dolasetron

Dolasetron 3D

What are the uses of this medicine?

• Dolasetron (Anzemet) Tablets are indicated for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy, including initial and repeat courses in adults and children 2 years and older.

Dolasetron (Anzemet) Injection is indicated for:

• the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including high dose cisplatin;
• the prevention of postoperative nausea and vomiting.
• the treatment of postoperative nausea and/or vomiting.

How does this medicine work?

• Dolasetron mesylate and its active metabolite, hydrodolasetron, are selective serotonin 5-HT3 receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors.
• The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema.
• It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine, and that the released serotonin then activates 5-HT3 receptors located on vagal efferents to initiate the vomiting reflex.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• known to have hypersensitivity to the drug.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• cimetidine
• Diuretics ('water pills')
• fentanyl (Abstral, Actiq, Duragesic, Fentora, Lazanda, Onsolis, Subsys)
• lithium (Lithobid)
• medications to control blood pressure
• medications for irregular heart beat such as atenolol (Tenormin, in Tenoretic)
• flecainide , quinidine (in Nuedexta), and verapamil (Calan, Covera-HS, Verelan, in Tarka)
• medications to treat migraines such as almotriptan (Axert), eletriptan (Relpax), frovatriptan (Frova), naratriptan (Amerge), rizatriptan (Maxalt), sumatriptan (Imitrex), and zolmitriptan (Zomig)
• methylene blue
• mirtazapine (Remeron)
• monoamine oxidase (MAO) inhibitors including isocarboxazid (Marplan), linezolid (Zyvox), phenelzine (Nardil), selegiline (Eldepryl, Emsam, Zelapar), and tranylcypromine (Parnate)
• rifampin (Rifadin, Rimactane, in Rifamate, in Rifater)
• selective serotonin reuptake inhibitors (SSRIs) such as citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem, in Symbyax), fluvoxamine (Luvox), paroxetine (Brisdelle, Paxil, Pexeva), and sertraline (Zoloft)
• tramadol (Conzip, Ultram, in Ultracet)

Is this medicine FDA approved?

• It was first approved in 1997 and is available as tablets of 50 and 100 mg and as a solution for injection in single or multidose vials (20 mg/mL) under the brand name Anzemet.

How should this medicine be used?

Recommended dosage:

Anzemet Tablets: In Adults:

• The recommended oral dosage of Anzemet (dolasetron mesylate) is 100 mg given within one hour before chemotherapy.

In Pediatric Patients:

• The recommended oral dosage in pediatric patients 2 to 16 years of age is 1.8 mg/kg given within one hour before chemotherapy, up to a maximum of 100 mg.

Anzemet Injection:

For Prevention of Cancer Chemotherapy-Induced Nausea and Vomiting:

In Adults:

• The recommended intravenous dosage of Anzemet Injection from clinical trial results is 1.8 mg/kg given as a single dose approximately 30 minutes before chemotherapy.
• Alternatively, for most patients, a fixed dose of 100 mg can be administered over 30 seconds.

In Pediatric Patients:

• The recommended intravenous dosage in pediatric patients 2 to 16 years of age is 1.8 mg/kg given as a single dose approximately 30 minutes before chemotherapy, up to a maximum of 100 mg.

For Prevention or Treatment of Postoperative Nausea and/or Vomiting:

In Adults:

• The recommended intravenous dosage of Anzemet Injection is 12.5 mg given as a single dose approximately 15 minutes before the cessation of anesthesia (prevention) or as soon as nausea or vomiting presents (treatment).

In Pediatric Patients:

• The recommended intravenous dosage in pediatric patients 2 to 16 years of age is 0.35 mg/kg, with a maximum dose of 12.5 mg, given as a single dose approximately 15 minutes before the cessation of anesthesia or as soon as nausea or vomiting presents.

Administration:

• Dolasetron injection comes as a solution to be injected intravenously by a healthcare provider in a hospital or clinic.
• It is usually given as a single injection just before the end of surgery or as soon as nausea or vomiting occurs.
• Dolasetron injection may be mixed in apple or apple-grape juice for children to take by mouth.
• It usually is given within 2 hours before surgery.
• This mixture may be kept at room temperature but must be used within 2 hours after mixing.
• Dolasetron comes as a tablet to take by mouth.
• It is usually taken within 1 hour before chemotherapy.
• For children unable to swallow the tablet, a specially prepared dolasetron liquid dose may be mixed in apple or apple-grape juice to take by mouth. This mixture may be kept at room temperature, but must be used within 2 hours after mixing.

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

This medicine is available in fallowing doasage form:

• As a solution to be injected intravenously
• As a tablet

This medicine is available in fallowing brand namesː

• Anzemet

What side effects can this medication cause?

The most common side effects of this medicine in Chemotherapy-Induced Nausea and Vomiting Studies may include:

• Headache
• Fatigue
• Diarrhea
• Bradycardia
• Dizziness
• Pain
• Tachycardia
• Dyspepsia
• Chills/Shivering

The most common side effects of this medicine in Postoperative Nausea and Vomiting Studies may include:

• Headache
• Dizziness
• Drowsiness
• Pain
• Urinary Retention

What special precautions should I follow?

• Patients should be informed that Anzemet may cause serious cardiac arrhythmias such as QT prolongation or heart block. Patients should be instructed to tell their health care provider right away if they perceive a change in their heart rate, if they feel lightheaded, or if they have a syncopal episode.
• Anzemet should be avoided in these patients, since they may be more at risk for cardiac arrhythmias such as QT prolongation and Torsade de Pointes.
• Advise patients of the possibility of serotonin syndrome with concomitant use of Anzemet and another serotonergic agent such as medications to treat depression and migraines. Advise patients to seek immediate medical attention if the following symptoms occur: changes in mental status, autonomic instability, neuromuscular symptoms with or without gastrointestinal symptoms.
• It is not known whether dolasetron mesylate is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Anzemet Tablets are administered to a nursing woman.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• tremors
• depression
• convulsions
• second-degree or higher AV conduction block

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.
• There is no known specific antidote for dolasetron mesylate, and patients with suspected overdose should be managed with supportive therapy.
• It is not known if dolasetron mesylate is removed by hemodialysis or peritoneal dialysis.

Can this medicine be used in pregnancy?

• There are, however, no adequate and well-controlled studies in pregnant women.
• Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients under 2 years of age have not been established.

What are the active and inactive ingredients in this medicine?

Anzemet Tablet:

• Active ingredient:
• dolasetron mesylate (as the monohydrate)

• Inactive ingredients:
• croscarmellose sodium, hypromellose, lactose, magnesium stearate, polyethylene glycol, polysorbate 80, pregelatinized starch, synthetic red iron oxide, and titanium dioxide.

Anzemet Injection:

• Active ingredient:
• dolasetron mesylate

• Inactive ingredients:
• mannitol
• acetate buffer in water for injection

Who manufactures and distributes this medicine?

Anzemet Tablet:

Manufactured for and Distributed by:

• Validus Pharmaceuticals LLC
• Parsippany, NJ

Anzemet Injection:

Mfd. for:

• sanofi-aventis U.S. LLC
• Bridgewater, NJ
• Origin Italy

Mfd by:

• Hospira, Inc.
• McPherson, KS USA

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

Anzemet Tablet:

• Store at 68° to 77°F (20° to 25°C).
• Protect from light.

Anzemet Injection:

• Store at 68° to 77°F (20° to 25°C).
• Protect from light.

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 Dolasetron
• FDA Dolasetron

Dolasetron Resources
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