Prab at 19:53, 8 September 2023

2023-09-08T19:53:38Z

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== '''What is Dolasetron?'''==

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

[[File:Dolasetron.svg|thumb|Dolasetron]]

[[File:Dolasetron 3D.png|thumb|Dolasetron 3D]]

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== '''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 antagonist'''s 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 [[Postremal chamber|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 inhibitors|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|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, CTCAE|Torsade de Pointes]].
* Advise patients of the possibility of [[serotonin syndrome]] with concomitant use of Anzemet and another [[Serotonergic|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 block|AV conduction block]]

Management of overdosage:
* {{overdose}}
* 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, Inc.|Validus Pharmaceuticals LLC]]
* Parsippany, NJ

'''Anzemet Injection:'''

Mfd. for:
* [[Sanofi-aventis|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.
{{gastrointestinal agents}}
{{coststubd}}
{{5-HT3 antagonists}}
{{Serotonergics}}
[[Category:Antiemetics]]
[[Category:5-HT3 antagonists]]
[[Category:Prodrugs]]
[[Category:Indoles]]
[[Category:Carboxylate esters]]
[[Category:Ketones]]
[[Category:Nitrogen heterocycles]]

Dolasetron - Revision history

Prab at 19:53, 8 September 2023