Drug information of Dolasetron

Dolasetron

Drug group:

Dolasetron blocks the actions of chemicals in the body that can trigger nausea and vomiting.

Dolasetron oral (taken by mouth) is used to prevent nausea and vomiting that may be caused by medicine to treat cancer (chemotherapy).

Mechanism of effect

Dolasetron is a selective serotonin receptor (5-HT3) antagonist which blocks serotonin both peripherally (primary site of action) and centrally at the chemoreceptor trigger zone

Pharmacokinetics

Absorption

Oral: Rapid and complete

Distribution

Hydrodolasetron: Children: 5.9 to 7.4 L/kg; Adults: 5.8 L/kg

Metabolism

Hepatic; rapid reduction by carbonyl reductase to hydrodolasetron (active metabolite); further metabolized by CYP2D6, CYP3A, and flavin monooxygenase

Excretion

Urine ~67% (dolasetron: <1% excreted unchanged in urine; hydrodolasetron: 53% to 61% of the total dose); Feces ~33%

Time to Peak

Hydrodolasetron: IV: 0.6 hours; Oral: ~1 hour

Half-Life Elimination

Dolasetron: IV: ≤10 minutes

Hydrodolasetron:

Oral: Children: 5.5 hours; Adolescents: 6.4 hours; Adults: 8.1 hours

IV: Children: 4.8 hours; Adults: 7.3 hours

Severe renal impairment: 11 hours

Severe hepatic impairment: 11 hours

Protein Binding

Hydrodolasetron: 69% to 77% (~50% bound to alpha1-acid glycoprotein)

Drug indications

: Labeled Indications

Chemotherapy-associated nausea and vomiting (oral): Prevention of nausea and vomiting associated with initial and repeat course of moderately emetogenic cancer chemotherapy in adults and children ≥2 years

Postoperative nausea and vomiting (injection): Prevention and treatment of postoperative nausea and vomiting (PONV) in adults and children ≥2 years

Dosage

Usual Adult Dose for Nausea/Vomiting - Postoperative

Recommended dose: 12.5 mg IV approximately 15 minutes before the cessation of anesthesia or as soon as nausea and vomiting presents

Comments:
-The recommended dose should not be exceeded. If a prophylactic dose fails, avoid initiating another dose as rescue therapy.
-This drug should be given as a single dose, and may be given as an IV infusion over at least 30 seconds or diluted and infused over 15 minutes.

Uses:
-For the prevention of postoperative nausea and vomiting
-For the treatment of postoperative nausea and/or vomiting

Usual Pediatric Dose for Nausea/Vomiting - Postoperative

2 to 16 years:
-Recommended dose: 0.35 mg/kg IV approximately 15 minutes before the cessation of anesthesia or as soon as nausea and vomiting presents
-Maximum dose: 12.5 mg
-Alternative dose: 1.2 mg/kg (of the IV injection solution) given orally within 2 hours before surgery, up to a maximum dose of 100 mg

Comments:
-The injection solution may be mixed with apple or apple-grape juice and administered orally; the mixed product may be kept up to 2 hours at room temperature before use.
-This drug should be given as a single dose, and may be given as an IV infusion over at least 30 seconds or diluted and infused over 15 minutes.

Uses:
-For the prevention of postoperative nausea and vomiting
-For the treatment of postoperative nausea and/or vomiting

Usual Pediatric Dose for Nausea/Vomiting - Chemotherapy Induced

2 to 16 years:
-Recommended dose: 1.8 mg/kg orally within 1 hour before chemotherapy
-Maximum dose: 100 mg

Comment:
-The recommended dose should not be exceeded.

Use:
-For the prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy

Drug contraindications

 

Side effects

Side effects requiring immediate medical attention

Along with its needed effects, dolasetron may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking dolasetron:

More common

  • Chest pain or discomfort
  • lightheadedness, dizziness, or fainting
  • slow or irregular heartbeat
  • unusual tiredness or weakness

Less common

  • Chills
  • decrease in the amount of urine
  • fast, pounding, or irregular heartbeat or pulse
  • fever

Rare

  • Agitation
  • black, tarry stools
  • bleeding gums
  • bloating or swelling of the face, arms, hands, lower legs, or feet
  • blood in the urine or stools
  • blurred vision
  • burning while urinating
  • changes in skin color
  • confusion
  • cough
  • delirium
  • depression
  • diarrhea
  • difficult or labored breathing
  • difficult or painful urination
  • difficulty with swallowing
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • feeling of warmth
  • feeling uncoordinated
  • frequent urination
  • hallucinations
  • headache
  • hives or welts, itching, or skin rash
  • increased volume of pale, dilute urine
  • irritability
  • lethargy
  • muscle twitching
  • nausea
  • noisy breathing
  • numbness and tingling of the face, fingers, or toes
  • pain in the arms, legs, or lower back, especially pain in the calves or heels upon exertion
  • pain, tenderness, or swelling of the foot or leg
  • pale skin
  • pale, bluish-colored, or cold hands or feet
  • pinpoint red or purple spots on the skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • rapid weight gain
  • red skin
  • rigid muscles
  • seizures
  • sweating
  • swelling of the face, ankles, or hands
  • tightness in the chest
  • tingling of the hands or feet
  • tremor
  • troubled breathing with exertion
  • unusual bleeding or bruising
  • unusual weight gain or loss
  • vomiting
  • weak or absent pulses in the legs

Side effects not requiring immediate medical attention

Some side effects of dolasetron may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects.

Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common

  • Belching
  • heartburn
  • indigestion
  • pain
  • stomach discomfort, upset, or pain

Rare

  • Abnormal dreams
  • bad, unusual, or unpleasant (after) taste
  • bloating
  • bloody nose
  • change in taste
  • changes in vision
  • continuing ringing or buzzing or other unexplained noise in the ears
  • darkened urine
  • difficulty having a bowel movement (stool)
  • difficulty seeing at night
  • difficulty with moving
  • feeling of constant movement of self or surroundings
  • feeling of unreality
  • hearing loss
  • increased sensitivity of the eyes to sunlight
  • increased sweating
  • joint pain
  • loss of appetite
  • muscle aching or cramping
  • muscle pain or stiffness
  • pain or burning sensation at the injection site
  • pains in the stomach, side, or abdomen, possibly radiating to the back
  • redness of the face, neck, arms, and occasionally, upper chest
  • sensation of spinning
  • sense of detachment from self or body
  • shakiness and unsteady walk
  • shakiness in the legs, arms, hands, or feet
  • swollen joints
  • unsteadiness, trembling, or other problems with muscle control or coordination
  • weight loss
  • yellow eyes or skin

Interactions

Amlodipine/Atorvastatine , Busulfan , Sibutramine , Tapentadol , Almotriptan , Apomorphine , Atenolol , Atomoxetine , Amlodipine , Amitriptyline , Amiodarone , Epirubicin , lacosamide , Benzthiazide , hydroflumethiazide , levamlodipine , osilodrostat , selpercatinib , ozogamicin , st. john's wort , vortioxetine , digitoxin , levomethadyl acetate , ozanimod , lefamulin , lofexidine , macimorelin , methotrimeprazine , 5-hydroxytryptophan , rilpivirine , Romidepsin , bosutinib , Methyclothiazide , Pasireotide , Siponimod , Rucaparib , Lomefloxacin , Ceritinib , Nilutamide , norfloxacin , Crizotinib , Telavancin , Deutetrabenazine , Entrectinib , Cabozantinib , Levomilnacipran , Foscarnet , lenvatinib , encorafenib , midostaurin , Triclabendazole , ivosidenib , ezogabine , Nadolol , Isradipine , Iloperidone , Pimavanserin , Degarelix , Trimeprazine , Triflupromazine , Amisulpride , Paliperidone , Pazopanib , Bendroflumethiazide , Esmolol , Gatifloxacin , Carteolol , Nebivolol , Nicardipine , Nisoldipine , Torsemide , probucol , Abiraterone , Felodipine , Penbutolol , Efavirenz , Eribulin , Inotuzumab‎ , Idarubicin , Goserelin , Anagrelide , Bumetanide , Procainamide , Polyethylene glycol , Mefloquine , Panobinostat , Ribociclib , Ibutilide , Halothane , vemurafenib , Osimertinib , Quinine , Chloroquine , Mesoridazine , Mifepristone , Pindolol , Telithromycin , Sufentanil , Alfentanil , Droperidol , primaquine , valbenazine , Arsenic , Tryptophan , Vilazodone , Ivabradine , Frovatriptan , Fenfluramine , dronedarone , saquinavir , eletriptan , Mirtazapine , protriptyline , meperidine , Nefazodone , ISOPROTERENOL , Pentazocine , Naratriptan , isocarboxazid , Remifentanil , methylene blue , Ziprasidone , Histrelin , propoxyphene , Tamoxifen , Metaproterenol , Prochlorperazine , Quinidine , Acebutolol , Amoxapine , Quetiapine , lithium , Buprenorphine , Chlorothiazide , Phenelzine , Toremifene , Atazanavir , Ranolazine , Linezolid , astemizole , ethacrynic acid , Pentamidine , Zolmitriptan , ritodrine , Leuprolide acetate , escitalopram , Clofazimine , fentanyl , Clomipramine , Solifenacin , Enzalutamide , Flecainide , Bicalutamide , Bisoprolol , Voriconazole , Carvedilol , Ketoconazole , Clarithromycin , Chlorpromazine , Clozapine , Haloperidol , Hydroxychloroquine , Hydrochlorothiazide , Vardenafil , Verapamil , Venlafaxine , Moxifloxacin , Mitoxantrone , Nortriptyline , Nifedipine , Nilotinib , Nimodipine , Lapatinib , Levofloxacin , Maprotiline , Methadone , Metoprolol , Metolazone , Fluconazole , Furazolidone , Furosemide , Fingolimod , Granisetron , Labetalol , Citalopram , Cisapride , Flutamide , Fluphenazine , Fluvoxamine , Fluoxetine , Sunitinib , Sertraline , Sotalol , Sorafenib , Sevoflurane , Ciprofloxacin , Doxorubicin , Disopyramide , Digoxin , Diltiazem , Rizatriptan , Risperidone , Thioridazine , Gemifloxacin , Daunorubicin , Desipramine , Duloxetine , Doxepin , Terbutaline , Trifluoperazine , Triptorelin , Trimipramine , Tizanidine , Timolol , Pimozide , Tacrolimus , Tetrabenazine , Trazodone , Tramadol , Tranylcypromine , perphenazine , Propafenone , Propranolol , Promethazine , Procarbazine , Posaconazole , Imipramine , Betaxolol , Bupropion , Buspirone , Papaverine , Paroxetine , Adenosine , Erythromycin , Ofloxacin , Oxaliplatin , Ondansetron , Oxytocin , Palonosetron , vandetanib , sparfloxacin , Indapamide , Dofetilide , Promazine , Vasopressin , Chlorthalidone , Arsenic trioxide , Desvenlafaxine , Milnacipran , Halofantrine , Grepafloxacin , Mibefradil , Dexfenfluramine , Terfenadine , Abarelix , Asenapine , Alfuzosin , Perflutren , Apalutamide , Pitolisant , Clevidipine , gilteritinib , glasdegib , Bepridil , bedaquiline , Dasatinib , Gemtuzumab , lasmiditan , vemurafenib , Halaven
fostemsavir  , polyethylene glycol 3350 with electrolytes ,trichlormethiazide

Alerts

You should not take dolasetron if you are allergic to it.

To make sure you can safely take dolasetron, tell your doctor if you have any of these other conditions:

  • kidney disease;
  • a serious heart condition such as "sick sinus syndrome";
  • a heart rhythm disorder such as slow heartbeats, or atrial fibrillation (fast, irregular heart rhythm);
  • personal or family history of long QT syndrome;
  • congestive heart failure; or
  • an electrolyte imbalance (such as low levels of potassium or magnesium in your blood).

Points of recommendation

It is not known whether dolasetron will harm an unborn baby. Tell your doctor if you are pregnant.

It is not known whether dolasetron passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Dolasetron should not be given to a child younger than 2 years old.

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Dolasetron is usually taken 1 hour before chemotherapy. Follow your doctor's instructions.

Store at room temperature away from moisture, heat, and light.

Tell your doctor if you forget to take your dose within 1 hour before chemotherapy. Do not take extra medicine to make up the missed dose.

Pregnancy level

B

Animal studies have failed to reveal evidence of teratogenicity or impaired fertility. There are no controlled data in human pregnancy.

Use is recommended only if clearly needed and the benefit outweighs the risk.

AU TGA pregnancy category: B1
US FDA pregnancy category: B

Breast feeding warning

AU: Use is not recommended.
US: Caution is recommended.

Excreted into human milk: Unknown
Excreted into animal milk: Unknown

Comments: The effects in the nursing infant are unknown.

When animal models were given the oral formulation of this drug, survival, growth, and development of pups were not affected.

Related drugs

Palonosetron , tropisetron

Drug forms

Anzemet

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