Granisetron

What is Granisetron?

• Granisetron (Kytril) is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist used to prevent nausea and vomiting caused by cancer chemotherapy and radiation therapy.

Granisetron structure

Granisetron 3D

Granisetron

What are the uses of this medicine?

Granisetron (Kytril) is used for the prevention of:

• Nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin.
• Nausea and vomiting associated with radiation, including total body irradiation and fractionated abdominal radiation.

• Sancuso (granisetron transdermal system) is a prescription medicine used to prevent nausea and vomiting in adults receiving anti-cancer (chemotherapy) treatment that causes moderate or severe vomiting.
• Sustol (granisetron extended-release injection) is used in combination with other antiemetics in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide (AC) combination chemotherapy regimens.

How does this medicine work?

• Granisetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist with little or no affinity for other serotonin receptors.
• Serotonin receptors of the 5-HT3 type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema.
• During chemotherapy that induces vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT3 receptors.
• This evokes vagal afferent discharge, inducing vomiting.
• Animal studies demonstrate that, in binding to 5-HT3 receptors, granisetron blocks serotonin stimulation and subsequent vomiting after emetogenic stimuli such as cisplatin.
• In the ferret animal model, a single granisetron injection prevented vomiting due to high-dose cisplatin or arrested vomiting within 5 to 30 seconds.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• known hypersensitivity to the drug or any of its components.

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:

• fentanyl (Abstral, Actiq, Duragesic, Fentora, Lazanda, Onsolis, Subsys)
• ketoconazole (Nizoral), lithium (Lithobid)
• 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)
• phenobarbital
• 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 patented in 1985 and approved for medical use in 1991.

How should this medicine be used?

Recommended dosage: In Emetogenic Chemotherapy:

• The recommended adult dosage of oral granisetron hydrochloride is 2 mg once daily or 1 mg twice daily.
• In the 2 mg once-daily regimen, two 1 mg tablets are given up to 1 hour before chemotherapy.
• In the 1 mg twice-daily regimen, the first 1 mg tablet is given up to 1 hour before chemotherapy, and the second tablet 12 hours after the first.

Use in the Elderly, Renal Failure Patients or Hepatically Impaired Patients:

• No dosage adjustment is recommended.

In Radiation (Either Total Body Irradiation or Fractionated Abdominal Radiation):

• The recommended adult dosage of oral granisetron hydrochloride is 2 mg once daily.
• Two 1 mg tablets are taken within 1 hour of radiation.

Use in the Elderly:

• No dosage adjustment is recommended.

Administration:

• Granisetron comes as a tablet to take by mouth.
• When taken to prevent nausea and vomiting caused by chemotherapy, granisetron is usually taken 1 hour before chemotherapy is begun.
• A second dose may be taken 12 hours after the first dose depending on the strength.
• When taken to prevent nausea and vomiting caused by radiation, granisetron is usually taken within 1 hour before treatment.

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

This medicine is available in fallowing doasage form:

• As Granisetron hydrochloride tablets

This medicine is available in fallowing brand namesː

• Kytril

What side effects can this medication cause?

The most common side effects of this medicine include: In Emetogenic Chemotherapy:

• Headache
• Constipation
• Asthenia
• Diarrhea
• Abdominal pain
• Dyspepsia

In Radiation:

• diarrhea
• asthenia
• constipation
• Headache

What special precautions should I follow?

• The development of serotonin syndrome has been reported with 5-HT3 receptor antagonists. If symptoms of serotonin syndrome occur, discontinue granisetron and initiate supportive treatment. Patients should be informed of the increased risk of serotonin syndrome, especially if granisetron is used concomitantly with other serotonergic drugs
• Granisetron is not a drug that stimulates gastric or intestinal peristalsis. The use of granisetron in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distention.
• QT prolongation has been reported with granisetron. Patients with cardiac disease, on cardio-toxic chemotherapy, with concomitant electrolyte abnormalities and/or on concomitant medications that prolong the QT interval are particularly at risk.
• It is not known whether granisetron is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when granisetron hydrochloride is administered to a nursing woman.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• headache

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 specific treatment for granisetron hydrochloride overdosage.
• In case of overdosage, symptomatic treatment should be given.

Can this medicine be used in pregnancy?

• Pregnancy Category B.
• 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 have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• granisetron hydrochloride

Inactive ingredients:

• hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, sodium starch glycolate, and titanium dioxide.

Who manufactures and distributes this medicine?

Manufactured by:

• NATCO PHARMA LIMITED
• Kothur,
• India.

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

• Store between 20º to 25ºC (68º and 77ºF).
• Keep container closed tightly.
• Protect from light.
• Retain in carton until time of use.

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 Granisetron
• FDA Granisetron

Granisetron Resources
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