Hyoscine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Gastrointestinal tract spasm, Genitourinary spasm
Adult: As hyoscine butylbromide: 20 mg 4 times daily.
Child: As hyoscine butylbromide: 6-11 years 10 mg tid; ≥12 years Same as adult dose.

Oral
Prophylaxis of motion sickness
Adult: As hyoscine hydrobromide: Initially, 0.15-0.3 mg 20-30 minutes before a journey, repeat 6 hourly if needed, up to max 3 doses in 24 hours. Max: 0.9 mg daily.
Child: As hyoscine hydrobromide: 3-4 years Initially, 0.075 mg, repeated once if needed. Max: 0.15 mg daily; >4-10 years 0.075-0.15 mg, repeat 6 hourly if needed. Max: 0.45 mg daily; >10 years 0.15-0.30 mg, repeat 6 hourly if needed. Max: 0.9 mg daily. All doses should be given 20-30 minutes before a journey.

Oral
IBS (irritable bowel syndrome)
Adult: As hyoscine butylbromide: Initially, 10 mg tid, may increase up to 20 mg 4 times daily if needed.
Child: As hyoscine butylbromide: 6-11 years 10 mg tid; ≥12 years Same as adult dose.

Parenteral
Motion sickness, Nausea and vomiting, Vertigo
Adult: As hyoscine hydrobromide: 0.2 mg as a single dose via IM or SC inj (may also be given via IV inj if required).
Child: As hyoscine hydrobromide: 0.006 mg/kg as a single dose via IM or SC inj.

Parenteral
Gastrointestinal tract spasm, Genitourinary spasm
Adult: As hyoscine butylbromide: 20 mg via slow IV or IM inj, may be repeated after 30 minutes if needed. Max: 100 mg daily.

Parenteral
Preoperative medication
Adult: As hyoscine hydrobromide: 0.2-0.6 mg given via IV, IM, or SC inj, 30-60 minutes prior to induction of anaesthesia.
Child: As hyoscine hydrobromide: 0.015 mg/kg given via IM or SC inj, 30-60 minutes prior to induction of anaesthesia.

Transdermal
Prophylaxis of motion sickness
Adult: As hyoscine hydrobromide patch containing 1.5 mg: Apply 1 patch behind the ear, 4-6 hours before a journey or in the evening before journey.
Child: >10 years Same as adult dose.

Transdermal
Postoperative nausea and vomiting
Adult: As hyoscine hydrobromide patch containing 1.5 mg: Apply 1 patch behind the ear on the evening before the surgery or 1 hour before caesarean section. Discard 24 hours after the surgery.
Child: >10 years Same as adult dose.
Chống chỉ định
Myasthenia gravis, narrow-angle glaucoma, tachycardia, megacolon; hypersensitivity.
Thận trọng
Patient with angina, cardiac failure, (including those who are undergoing cardiac surgery), coronary artery disease, hypertension, open angle glaucoma, pyrexia, thyrotoxicosis; pyloric, intestinal or urinary bladder neck obstruction, paralytic ileus, gastrointestinal tract stenoic lesions, prostatic hypertrophy, urinary retention; history of seizure or psychosis. Renal or hepatic impairment. Children. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Tachyarrhythmias, hypotension, increased intra-ocular pressure, drowsiness, confusional states, visual hallucinations, blurred vision, eye pain, idiosyncratic reactions (e.g. agitation, delusion, acute toxic psychosis), epileptic seizures.
Nervous system disorders: Dizziness, headache, equilibrium disturbance, excitement, ataxia, hallucinations, behavioural abnormalities, acute toxic psychosis, agitation, confusion, paranoia, rambling speech, fatigue, migraine, irritability, amnesia, restlessness, sedation.
Cardiac disorders: Bradycardia.
Gastrointestinal disorders: Nausea, vomiting, hypersalivation, diarrhoea, dry mouth, abdominal cramps, constipation, oesophageal ulceration.
General disorders and administration site conditions: Hyperpyrexia.
Eye disorders: Mydriasis, cycloplegia, eye pruritus.
Musculoskeletal: Muscle weakness.
Renal and urinary disorders: Urinary retention, dysuria.
Skin and subcutaneous tissue disorders: Flushing, sweating, dry skin, rash, erythema, pruritus, skin burns, contact dermatitis (transdermal).
Potentially Fatal: Anaphylaxis, shock.
Parenteral/PO/Transdermal: C
Thông tin tư vấn bệnh nhân
This drug may cause drowsiness, disorientation, confusion, or blurred vision, if affected, do not drive or operate machinery. Remove transdermal hyoscine before medical scan.
Chỉ số theo dõi
Monitor heart rate, urinary output, body temperature, and intraocular pressure.
Quá liều
Symptoms: CNS stimulation, tachycardia, arrhythmia, urinary retention, coma, respiratory depression. Management: Symptomatic and supportive treatment. Empty stomach immediately via gastric lavage or induced emesis. Short acting benzodiazepines or barbiturate may be given to control CNS stimulation.
Tương tác
May decrease the absorption of oral medicines due to decreased gastric motility and delayed gastric emptying. The sedative effect of hyoscine may be enhanced by other CNS depressants. Other drugs with anticholinergic properties (e.g. amantadine, antihistamines) may enhance the effects of hyoscine.
Tương tác với thức ăn
The sedative effect of hyoscine may be enhanced by alcohol.
Ảnh hưởng đến kết quả xét nghiệm
Interferes with gastric secretion test.
Tác dụng
Description:
Mechanism of Action: Hyoscine is a tertiary amine antimuscarinic agent. It blocks the action of acetylcholine in the smooth muscles of the gastrointestinal, biliary and urinary tracts, in secretory glands and in the CNS, thus exhibiting spasmolytic actions on smooth muscles and inhibit secretions. It also blocks transmission of cholinergic impulses from the vestibular nuclei to the CNS, thus preventing motion-induced nausea and vomiting.
Onset: Inhibition of saliva: Within 30-60 minutes (IM, oral); Amnesia: Within 10 minutes (IV); Antiemesis: Within 15-30 minutes (IM), approx 4 hours (transdermal).
Duration: Antiemesis: Up to 72 hours. (transdermal), approx 4 hours (IM); Inhibition of saliva: Up to 4-6 hours (IM, oral); Amnesia: ≥2 hours (IV); Mydriasis: Up to 8 hours (IM).
Pharmacokinetics:
Absorption: Tertiary salts: Readily absorbed from the gastrointestinal tract. Quaternary salts: Poorly absorbed. Bioavailability: 8% (oral). Time to peak plasma concentration: Within 24 hours (transdermal); As hydrobromide: Approx 20 minutes (IM), 15 minutes (SC); As butylbromide: Approx 2 hours (oral).
Distribution: Tertiary salts: Crosses blood-brain barrier and the placenta, enters breast milk. Volume of distribution: As butylbromide: 128 L. Plasma protein binding: As butybromide: Approx 4%, to albumin.
Metabolism: Metabolised in the liver mainly via conjugation.
Excretion: As hydrobromide: Mainly via urine (<10% as unchanged drug and some metabolites). As butylbromide: IV: Via urine (42-61% as unchanged drug) and faeces (28-37%). Elimination half-life: Hyoscine base 9.5 hours; As butylbromide: Approx 5-11 hours; As hydrobromide: Approx 1-4 hours.
Đặc tính

Chemical Structure Image
Hyoscine

Source: National Center for Biotechnology Information. PubChem Database. (-)-Scopolamine, CID=3000322, https://pubchem.ncbi.nlm.nih.gov/compound/Scopine-_-_-tropate (accessed on Jan. 23, 2020)

Bảo quản
Store between 15-30°C. Protect from light.
Phân loại MIMS
Thuốc chống co thắt
Phân loại ATC
A04AD01 - scopolamine ; Belongs to the class of other antiemetics.
Tài liệu tham khảo
Anon. Scopolamine (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/07/2017.

Anon. Scopolamine, Scopolamine Hydrobromide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 10/07/2017.

Buckingham R (ed). Hyoscine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/07/2017.

Joint Formulary Committee. Hyoscine Butylbromide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/07/2017.

Joint Formulary Committee. Hyoscine Hydrobromide (Scopolamine Hydrobromide). British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/07/2017.

Transderm Scop Patch, Extended Release (Baxter Healthcare Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/07/2017.

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