Flupentixol


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular
Psychoses, Schizophrenia
Adult: For patients stabilised on oral treatment: As flupentixol decanoate inj: In patients who have not received prior depot antipsychotics: Initially, 20 mg is given as a test dose. After at least 1 week according to patient response, may be followed by 20-40 mg every 2-4 weeks via deep IM inj. Other patients may be adequately maintained on 20-40 mg every 2-4 weeks. Usual dose: Between 50 mg every 4 weeks and 300 mg every 2 weeks. Max: 400 mg weekly. Dose and dosing interval must be individualised and adjusted based on individual symptoms and response. Max inj volume recommendations may vary depending on the concentration used (refer to detailed product guideline).
Elderly: As flupentixol decanoate inj: Initial dose may require to be reduced to 1/4 or 1/2 of the usual starting dose.

Oral
Depression
Adult: Cases with or without anxiety: As 0.5 or 1 mg flupentixol dihydrochloride tab: Initially, 1 mg daily as a single dose in the morning. After 1 week, dosage may be increased to 2 mg daily given in 2 divided doses according to patient response. Max: 3 mg daily. Withdraw treatment if no effect has been observed within 1 week of taking the max dose.
Elderly: As 0.5 or 1 mg flupentixol dihydrochloride tab: Initially, 0.5 mg daily as a single dose in the morning. After 1 week, dosage may be increased to 1 mg once daily according to patient response. Max: 1.5 mg daily given in 2 divided doses.

Oral
Psychoses, Schizophrenia
Adult: As 3 mg flupentixol dihydrochloride tab: 3-9 mg bid, adjusted according to patient response. Max: 18 mg daily.
Elderly: As 3 mg flupentixol dihydrochloride tab: Initial dose may require to be reduced to 1/4 or 1/2 of the usual starting dose.
Nhóm bệnh nhân đặc biệt
Oral/IM:
For Schizophrenia; Psychoses:

Debilitated patients: As 3 mg flupentixol dihydrochloride tab/as flupentixol decanoate inj: Initial dose may require to be reduced to 1/4 or 1/2 of the usual starting dose.
Cách dùng
May be taken with or without food.
Chống chỉ định
Circulatory collapse, depressed level of consciousness due to any cause (e.g. alcohol intoxication, opiates, barbiturates), coma; severe depression requiring electroconvulsive therapy or hospitalisation, and states of excitement or overactivity, including mania (for 0.5 or 1 mg tab used in depression). Not recommended for use in excitable or agitated patients.
Thận trọng
Patient with CV disease (e.g. QT prolongation), significant bradycardia, recent MI, decompensated heart failure, arrhythmias, hypovolaemia, hypokalaemia, hypomagnesaemia, severe respiratory disease, epilepsy or conditions predisposing to epilepsy (e.g. alcohol withdrawal, brain damage, head trauma), organic brain syndrome, Parkinson’s disease, narrow-angle glaucoma, prostatic hypertrophy, hypothyroidism, hyperthyroidism, diabetes, myasthenia gravis, phaeochromocytoma, decreased gastrointestinal motility, paralytic ileus, urinary retention, visual problems; prolactin-dependent tumours; history of suicide-related events; risk factors for venous thromboembolism (VTE); history of or risk factors for cerebrovascular accident; at risk of aspiration pneumonia (e.g. Alzheimer’s disease). Patient undergoing surgery; subjected to dehydration or strenuous exercise; exposed to extreme heat. Not approved for the treatment of elderly with dementia-related psychosis. Concomitant use with other antipsychotics. Avoid abrupt withdrawal. Debilitated patients. Elderly. Renal and hepatic impairment. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Extrapyramidal symptoms (e.g. akathisia, dystonia, tardive dyskinesia), QT prolongation, VTE, cerebrovascular events, anticholinergic effects (e.g. xerostomia, blurred vision, constipation, urinary retention), blood dyscrasias (e.g. agranulocytosis, neutropenia, leucopenia, thrombocytopenia), diabetic ketoacidosis, oesophageal dysmotility and aspiration, falls, orthostatic hypotension, impaired core body temperature regulation, increased prolactin levels; withdrawal symptoms. Rarely, lens opacity.
Cardiac disorders: Palpitation, tachycardia.
Eye disorders: Abnormal vision, accommodation disorder.
Gastrointestinal disorders: Nausea, vomiting, dyspepsia, diarrhoea, sialorrhoea.
General disorders and administration site conditions: Fatigue, asthenia.
Investigations: Increased weight.
Metabolism and nutrition disorders: Increased appetite.
Musculoskeletal and connective tissue disorders: Myalgia.
Nervous system disorders: Dizziness, drowsiness, headache, hyper- or hypokinesia, tremor.
Psychiatric disorders: Depression, insomnia, nervousness, agitation, disturbance in attention.
Renal and urinary disorders: Micturition disorder.
Reproductive system and breast disorders: Decreased libido.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Hyperhidrosis, pruritus.
Potentially Fatal: Suicidal thoughts or attempts, arrhythmias, neuroleptic malignant syndrome.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, drowsiness, or blurred vision; if affected, do not drive or operate machinery.
Chỉ số theo dõi
Correct electrolyte abnormalities prior to initiation of treatment. Monitor ECG, blood pressure, body weight; CBC, electrolytes, LFTs, fasting plasma glucose level/HbA1c and lipid panel as clinically indicated. Check for clinical worsening, suicidal thoughts, or unusual changes in behaviour; involuntary movements or parkinsonian signs, tardive dyskinesia; signs and symptoms of neuroleptic malignant syndrome (e.g. mental status changes, fever, muscle rigidity). Perform ocular examination yearly in patients >40 years.
Quá liều
Symptoms: Somnolence, hypotension, shock, extrapyramidal symptoms, hyper- or hypothermia, convulsions, and coma. Management: Symptomatic and supportive treatment, particularly the CV and respiratory systems. May consider administration of activated charcoal or perform gastric lavage. May give anticholinergic agents used in Parkinson’s disease for extrapyramidal symptoms; benzodiazepines for excitement, agitation or convulsions; norepinephrine in IV saline drip for shock.
Tương tác
May potentiate the effects of other CNS depressants, barbiturates, general anaesthetics, and anticoagulants. May increase risk of QT interval prolongation with class Ia and III antiarrhythmics (e.g. quinidine, sotalol), erythromycin, moxifloxacin, cisapride, thioridazine, and thiazide diuretics. May prolong the action of neuromuscular blocking agents. May potentiate the anticholinergic effects of atropine. May increase risk of extrapyramidal effects with metoclopramide and piperazine. May enhance the hypotensive effects of hydralazine, doxazosin, and methyldopa. May reverse the antihypertensive effects of guanethidine. Increased risk of neurotoxicity with lithium and sibutramine. Efficacy of adrenergic agents, levodopa and anticonvulsants may be impaired. May inhibit the metabolism of TCAs; antagonise the effects of epinephrine and sympathomimetics. Insulin and glucose responses may be modified by flupentixol.
Tương tác với thức ăn
Enhanced CNS depressant effect with alcohol.
Tác dụng
Description: Flupentixol, a thioxanthene derivative antipsychotic agent, inhibits the postsynaptic dopamine receptors in the CNS which results in the blockage of dopamine-mediated effects.
Synonym: flupenthixol.
Onset: 24-72 hours after inj (IM depot).
Duration: 2-4 weeks (IM depot).
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract. Slowly absorbed from the site of IM inj. Bioavailability: Approx 40-55% (oral). Time to peak plasma concentration: 3-8 hours (oral); 4-7 days (IM depot).
Distribution: Widely distributed in the body. Crosses the blood-brain barrier and placenta; enters breast milk. Volume of distribution: Approx 14.1 L/kg. Plasma protein binding: Approx 99%.
Metabolism: Extensively metabolised in the liver via sulfoxidation, side-chain N-dealkylation, and glucuronic acid conjugation into inactive metabolites; undergoes first-pass metabolism in the gut wall.
Excretion: Via faeces and urine as metabolites. Elimination half-life: Approx 35 hours (oral); approx 3 weeks (IM depot).
Đặc tính

Chemical Structure Image
Flupentixol

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5281881, Flupentixol. https://pubchem.ncbi.nlm.nih.gov/compound/cis-Flupentixol. Accessed Dec. 21, 2020.

Bảo quản
Tab: Store below 30°C. IM inj: Store between 15-25°C. Protect from light.
Phân loại MIMS
Thuốc chống trầm cảm / Thuốc chống loạn thần
Phân loại ATC
N05AF01 - flupentixol ; Belongs to the class of thioxanthene derivatives antipsychotics.
Tài liệu tham khảo
Anon. Flupentixol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/10/2020.

Buckingham R (ed). Flupentixol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/10/2020.

Depixol 3 mg Film-Coated Tablets (Lundbeck Limited). MHRA. https://products.mhra.gov.uk. Accessed 04/12/2020.

Depixol Conc. 100 mg/mL Solution for Injection (Lundbeck Limited). MHRA. https://products.mhra.gov.uk/. Accessed 06/10/2020.

Fluanxol 0.5 and 1 mg Film-Coated Tablets (Lundbeck Limited). MHRA. https://products.mhra.gov.uk. Accessed 06/10/2020.

Fluanxol 0.5 mg Film-Coated Tablets (Lundbeck Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 06/10/2020.

Healthcare Logistics. Fluanxol Depot 20 mg/mL and Fluanxol Concentrated Depot 100 mg/mL Solution for Injection data sheet 05 December 2018. Medsafe. http://www.medsafe.govt.nz/. Accessed 06/10/2020.

Joint Formulary Committee. Flupentixol Decanoate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/10/2020.

Joint Formulary Committee. Flupentixol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/12/2020.

Psytixol 100 mg/mL Injection (Generics [UK] Ltd t/a Mylan). MHRA. https://products.mhra.gov.uk/. Accessed 06/10/2020.

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