Nefopam


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular
Acute pain, Postoperative pain
Adult: Usual dose: 20 mg, repeated 6 hourly if needed. Max: 120 mg daily. Patient must lie down during and for 15-20 minutes after administration.

Intravenous
Acute pain, Postoperative pain
Adult: Usual dose: 20 mg via slow IV bolus infusion over at least 15 minutes, repeated 4 hourly if needed. Max: 120 mg daily. Patient must lie down during and for 15-20 minutes after administration.

Oral
Moderate acute pain, Moderate chronic pain
Adult: For the relief of pain including postoperative, dental, musculoskeletal, acute traumatic and cancer pain: Initially, 60 mg tid. Usual dose: 30-90 mg tid, adjusted according to patient response.
Elderly: Initially, 30 mg tid.
Child: ≥12 years Same as adult dose.
Suy thận
PO:
ESRD: Dose reduction may be necessary.
Cách dùng
May be taken with or without food. May be taken w/ meals if GI discomfort occurs.
Hướng dẫn pha thuốc
IV infusion: May be diluted in 0.9% NaCl solution or 5% dextrose in water.
Chống chỉ định
History of convulsive disorders. IM/IV: Urinary retention linked to urinary or prostate disorders, angle-closure glaucoma. Oral: Concomitant use with MAOIs.
Thận trọng
Patient with angle-closure glaucoma, urinary retention, benign prostatic hyperplasia, CV disease or history of ischaemic heart disease. Patient concomitantly taking TCA. Not recommended for the treatment of MI. Renal and hepatic impairment. Children and elderly. Pregnancy and lactation. IM/IV: Not indicated for the treatment of chronic pain; not advisable for use in the elderly.
Tác dụng không mong muốn
Significant: Anticholinergic effects (e.g. blurred vision, xerostomia, constipation, urinary retention), sympathomimetic effects (e.g. tachycardia, exacerbation of angina); drug dependence and abuse. Rarely, transient pink discolouration of urine.
Cardiac disorders: Palpitations.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain.
Immune system disorders: Angioedema, allergic reactions.
Nervous system disorders: Dizziness, drowsiness, headache, paraesthesia, tremor, convulsion, lightheadedness.
Psychiatric disorders: Insomnia, nervousness, confusion, hallucination.
Skin and subcutaneous tissue disorders: Diaphoresis.
Vascular disorders: Hypotension, syncope.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and drowsiness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor renal and hepatic function; signs of anticholinergic effects (e.g. nausea, sweating) particularly within approx 15 minutes of administration (IM/IV).
Quá liều
Symptoms: Tachycardia with hyperdynamic circulation; agitation, hallucinations, convulsions, and coma. Management: Supportive and symptomatic treatment. Perform gastric lavage, or induce vomiting or diuresis. May administer activated charcoal to prevent absorption. May give diazepam for convulsions and hallucinations, and β-adrenergic blockers for CV complications.
Tương tác
May cause serotonin toxicity (including serotonin syndrome) with TCAs and SSRIs. May result in additive adverse effects with other anticholinergic or sympathomimetic agents.
Potentially Fatal: May increase the risk of serotonin toxicity (including serotonin syndrome) with MAOIs.
Tương tác với thức ăn
Alcohol may increase the CNS depressant effects of nefopam.
Ảnh hưởng đến kết quả xét nghiệm
May cause false-positive result with urinary screening test for opioids and benzodiazepines.
Tác dụng
Description:
Mechanism of Action: Nefopam is a potent, centrally-acting, non-opioid analgesic with anticholinergic and sympathomimetic actions. Its exact mechanism is unclear; however, in vitro studies suggest that it inhibits the reuptake of norepinephrine, serotonin and dopamine.
Onset: Rapid.
Pharmacokinetics:
Absorption: Absorbed from the gastrointestinal tract. Bioavailability: 40% (oral). Time to peak plasma concentration: Approx 1-3 hours (oral); 0.5-1 hour (IM).
Distribution: Enters breast milk. Plasma protein binding: Approx 73%.
Metabolism: Extensively metabolised in the liver to form desmethylnefopam, nefopam N-oxide, and N-glucuronide.
Excretion: Mainly via urine (87%, <5% as unchanged drug); faeces (approx 8%). Elimination half-life: Approx 4 hours.
Đặc tính

Chemical Structure Image
Nefopam

Source: National Center for Biotechnology Information. PubChem Database. Nefopam, CID=4450, https://pubchem.ncbi.nlm.nih.gov/compound/Nefopam (accessed on Jan. 22, 2020)

Bảo quản
Tab: Store below 25°C. Solution for inj: Store below 30°C.
Phân loại MIMS
Thuốc giảm đau (không opioid) & hạ sốt
Phân loại ATC
N02BG06 - nefopam ; Belongs to the class of other analgesics and antipyretics.
Tài liệu tham khảo
Acupan 20 mg/2 mL, Solution for Injection (DKSH Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 03/05/2021.

Anon. Nefopam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/05/2021.

Buckingham R (ed). Nefopam Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/05/2021.

iNova Pharmaceuticals (New Zealand) Limited. Acupan 30 mg Tablets data sheet 10 July 2018. Medsafe. http://www.medsafe.govt.nz. Accessed 03/05/2021.

Joint Formulary Committee. Nefopam Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/05/2021.

Nefopam Hydrochloride 30 mg Film-Coated Tablets (Key Pharmaceuticals Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 03/05/2021.

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