Flupenthixol

Registered South African indications:

• Schizophrenia
• Depression

Contraindications

Injection

• Hypersensitivity to the active ingredient or any of its excipients
• Extremely excitable and overactive patients
• Acute barbiturate, alcohol and opiate poisoning
• Pregnancy

Tablet

• Hypersensitivity to the active ingredient or any of its excipients
• Not recommended for severe depression requiring electro-convulsive therapy (ECT) and/or hospitalisation. In states of excitement or overactivity, including mania
• Pre-existing CNS depression or coma, bone marrow suppression or phaechromocytoma
• Severe alcohol, barbiturate and opiate intoxications
• Pregnancy
• Lactation
• Not recommended for children

Cautions

• Hypersensitivity to thioxanthenes or other antipsychotics
• Breastfeeding (inj)
• Renal impairment 
• Hepatic impairment 
• Elderly 
• Arrhythmias
• QT prolongation
• Cardiovascular disease
• Recent myocardial infarction
• Decompensated cardiac failure
• Risk factors for venous thromboembolism
• Parkinson's disease
• Seizure disorders
• Severe respiratory disease
• Glaucoma
• Prostatic hypertrophy
• Hypothyroidism
• Hyperthyroidism
• Myasthenia gravis
• Pheochromocytoma  
• Abrupt withdrawal
• Suicidal ideation
• Diabetes mellitus
• Blood dycrasias
• Risk factors for cerebrovascular accident
• Dementia
• Organic brain syndrome
• Mental retardation
• Alcohol abuse
• Opioid abuse
• Galactose intolerance
• Lapp lactase deficiency  
• Glucose-galactose malabsorption  

Forms avail. in SA and covered in this monograph: inj, tab

Schizophrenia
- Especially those who are unreliable in taking the medication prescribed for them. Features of the illness most likely to benefit are apathy, inertia, withdrawnness, anxiety, anergy, hallucinations and paranoid delusions

• IM: Usual doses: 20-60mg (1-3ml) at intervals of 2-4 weeks, depending on response

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Certain patients may need larger doses, on need them at shorter intervals

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Administer by deep intramuscular injection in the gluteal region

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Depression - mild to moderate
- Short term symptomatic treatment of depression of mild to moderate severity (with or without anxiety)

• Oral (tab): Initial: 1mg, dly as a single morning dose; If inadequate clinical response: Increase to 2mg, dly after 1 week; Max: 3mg/24hrs

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Daily dosage of more than 2mg, should be in divided doses up to a max. of 3mg

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In view of the activating properties of flupenthixol, it is advisable to give the last dose of the day no later than 4pm. Patients often respond to flupenthixol within 2-3 days. If no effect has been observed within one week at max. dosage the drug should be withdrawn

Injection

• No information available

Tablet

• Contraindicated

Pregnancy

• Contraindicated

Breastfeeding

Injection

• Caution; no information available

Tablet

• Contraindicated

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended 

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Insomnia
• Depression
• Nervousness
• Agitation
• Confusion
• Suicidal ideation 
• Suicidal behaviour
• Somnolence
• Akathisia 
• Hyperkinesia
• Hypokinesia
• Tremor
• Dystonia
• Dizziness
• Headache
• Disturbance in attention
• Tardive dyskinesia
• Parkinsonism
• Speech disorder
• Seizures 
• Neuroleptic malignant syndrome
• Fatigue
• Neonatal drug withdrawal syndrome 

Cardiovascular Disorders

• Tachycardia
• Palpitations
• Prolonged QT interval
• Hypotension
• Venous thromboemoblism

Respiratory Disorders

• Dyspnoea 

Gastrointestinal Disorders

• Dry mouth
• Salivary hypersecretion
• Constipation
• Dyspepsia
• Diarrhoea
• Abdominal pain
• Nausea and vomiting
• Flatulence

Hepatobiliary Disorders

• Abnorma hepatic function tests
• Jaundice

Genitourinary Disorders

• Micturition disorder
• Urinary retention
• Ejaculation failure
• Erectile dysfunction

Endocrine and Metabolic Disorders

• Hyperprolactinaemia
• Increased appetite
• Increased weight 
• Decreased appetite
• Hyperglycaemia
• Impaired glucose tolerance
• Hot flushes
• Decreased libido
• Gynaecomastia 
• Galactorrhoea
• Amenorrhoea

Musculoskeletal Disorders

• Myalgia
• Muscle rigidity

Skin and Subcutaneous Tissue Disorders

• Hyperhidrosis
• Pruritus
• Rash
• Photosensitivity reaction
• Dermatitis
• Injection site reaction

Immune, Blood and Lymphatic System Disorders

• Thrombocytopenia
• Neutropenia
• Leukopenia
• Agranulocytosis
• Hypersensitivity
• Anaphylactic reaction

Sensory Disorders

• Accommodation disorder
• Vision abnormal
• Oculogyration

• Central nervous system depressants
• General anaesthetics 
• Anticoagulants 
• Neuromuscular blocking agents
• Anticholinergics
• Metoclopramide
• Piperazine 
• Antiparkinson agents
• Lithium 
• Sibutramine 
• Quinidine
• Corticosteroids 
• Digoxin
• Vasodilator antihypertensives
• Methyldopa
• Qt prolongation agents 
• Thiazide diuretics 
• Sympathomimetic agents
• Guanethidine
• Alpha blockers
• Beta blockers 
• Levodopa
• Anticonvulsants
• Tricyclic antidepressants

None routine. Specific cases may require

• Hepatic function
• Full blood count
• Lipid profile
• Blood glucose

Flupenthixol is a thioxanthene antipsychotic. It is an antagonist of D1 and D2 dopamine receptors and an alpha-adrenergic receptor antagonist. Its antipsychotic activity is thought to be related to its blockade of postsynaptic dopamine receptors in the central nervous system.

Tablet 0.5mg 

• Fluanxol (H.Lundbeck) originator

Tablet 1mg 

• Fluanxol (H.Lundbeck) originator

Injection (per 1ml) 20mg

• Fluanxol Depot (H.Lundbeck) originator