Thông tin thuốc gốc
Chỉ định và Liều dùng
Treatment and prophylaxis of postoperative nausea and vomiting
Adult: 12.5 mg once daily as IV push over 30 seconds or via infusion over 15 min; given as soon as nausea or vomiting present (treatment) or approx 15 min before cessation of anaesthesia (prophylaxis).

Nausea and vomiting associated with cancer chemotherapy
Adult: 100 or 200 mg once daily w/in 1 hr before chemotherapy. Duration of treatment: 4-7 consecutive days/chemotherapy cycle.

Prophylaxis of postoperative nausea and vomiting
Adult: 50 mg at the induction of anaesthesia, or 100 mg w/in 2 hr before surgery.
Hướng dẫn pha thuốc
IV infusion: Dilute in 50 ml of a compatible soln (i.e. NaCl 0.9%, dextrose 5%, Lactated Ringer’s soln, dextrose 5% and Lactated Ringer’s soln, dextrose 5% and NaCl 0.45%, and mannitol 10% inj).
Tương kỵ
Incompatible w/ aciclovir, alemtuzumab, aminocaproic acid, aminophylline, amphotericin B, ampicillin Na, carmustine, cefazolin Na, chloramphenicol Na succinate, clindamycin phosphate, dexamethasone, K phosphate, thiopentone Na, 5-fluorouracil, heparin Na, methylprednisolone succinate, Na bicarbonate, pantoprazole, trimethoprim w/ sulfamethoxazole.
Chống chỉ định
Complete heart block (w/o pacemaker), congenital QT syndrome.
Thận trọng
Patient w/ history of abnormal heart rhythms, structural heart disease, sick sinus syndrome, AF w/ slow ventricular response, myocardial ischemia, electrolyte abnormalities (i.e. hypokalaemia, hypomagnesemia). IV admin is not intended for prophylaxis of chemotherapy-associated nausea and vomiting. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: PR, QRS, and QT prolongation.
Nervous: Dizziness, headache, drowsiness, fatigue, syncope, flushing, paraesthesia, tremor, ataxia, twitching, agitation, anxiety, sleep disorder, depersonalization, confusion, abnormal dreaming.
CV: Bradycardia, HTN, orthostatic hypotension, tachycardia, peripheral oedema and ischaemia, phlebitis.
GI: Diarrhoea, dyspepsia, flatulence, taste disturbance, constipation, abdominal pain, anorexia, pancreatitis.
Resp: Bronchospasm, dyspnea, epistaxis.
Genitourinary: Oliguria, dysuria, polyuria, acute renal failure, urinary retention, hematuria.
Haematologic: Anemia, hematoma, thrombocytopenia, prolonged partial thromboplastin time (PTT) and prothrombin time.
Musculoskeletal: Myalgia, arthralgia.
Ophthalmologic: Abnormal vision, photophobia.
Otic: Tinnitus.
Dermatologic: Pruritus, urticaria, increased sweating, rash.
Others: Chills, fever, pain, pain at inj site.
Potentially Fatal: Serotonin syndrome. Rarely, cardiac arrest, 2nd or 3rd degree AV block, serious ventricular arrhythmia (e.g. torsade de pointes).
IV/Parenteral/PO: B
Chỉ số theo dõi
Monitor ECG, serum K and Mg concentration.
Quá liều
Symptoms: Severe hypotension, dizziness; PR, QRS, and QT prolongation. Management: Symptomatic and supportive treatment. Monitor cardiac function.
Tương tác
Increased risk of QT prolongation w/ other QT prolonging agents (e.g. pimozide, ziprasideone) and drugs known to cause electrolyte imbalance (e.g. diuretics). Decreased blood levels and therapeutic effects w/ rifampicin. Increased blood levels and effects w/ atenolol and cimetidine. Increased risk of conduction abnormalities when concurrently used w/ antiarrhythmic agents (e.g. verapamil, flecainide, quinidine).
Tác dụng
Description: Dolasetron, a selective serotonin (5-HT3) receptor antagonist, has antiemetic actions similar to ondansetron. It blocks serotonin both peripherally at the GI tract (main site of action) and centrally at the chemoreceptor trigger zone.
Absorption: Rapid and completely absorbed (oral). Bioavalability: Approx 75%. Time to peak plasma concentration: Hydrodolasetron: Approx 1 hr (oral); 0.6 hr (IV).
Distribution: Widely distributed in the body. Volume of distribution: 5-7.9 L/kg. Plasma protein binding: 69-77%.
Metabolism: Rapidly metabolised hepatically via reduction by carbonyl reductase to hydrodolasetron (active metabolite); further metabolised by CYP2D6, CYP3A, and flavin monooxygenase enzymes.
Excretion: Via urine (approx 67%); faeces (approx 33%). Elimination half-life: Dolasetron: ≤10 min (IV); hydrodolasetron: 8.1 hr (oral); 7.3 hr (IV).
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Dolasetronum, CID=3033818, (accessed on Jan. 21, 2020)

Bảo quản
Store between 20-25°C. Protect from light.
Phân loại MIMS
Thuốc chống nôn / Trị liệu chăm sóc nâng đỡ
Phân loại ATC
A04AA04 - dolasetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
Tài liệu tham khảo
Anon. Dolasetron. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 27/02/2017.

Anzemet Injection (Sanofi-Aventis U.S. LLC). DailyMed. Source: U.S. National Library of Medicine. Accessed 27/02/2017.

Anzemet Tablet, Film Coated (Validus Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. Accessed 27/02/2017.

Buckingham R (ed). Dolasetron Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. . Accessed 27/02/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Dolasetron Mesylate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). Accessed 27/02/2017.

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