Flupentixol is an antipsychotic neuroleptic drug. It is a thioxanthene, and therefore closely related to the phenothiazines. Its primary use is as a long-acting injection given two or three weeks to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness. It is a D1 and D2 receptor antagonist.
Mechanism of Action of flupentixol
Flupenthixol is a thioxanthene antipsychotic. The mechanism of action of Flupenthixol is not completely understood. Flupenthixol is a powerful antagonist of both D1 and D2 dopamine receptors and an alpha-adrenergic receptor antagonist. Its antipsychotic activity is thought to be related to blocks postsynaptic dopamine receptors in the CNS.
Indications of flupentixol
- Different types of anxiety,
- Depression & apathy
- Psychogenic depression,
- Depressive neuroses,
- Masked depression,
- Psychosomatic affections accompanied by anxiety and apathy,
- Menopausal depressions,
- Dysphoria
- Depression in alcoholics and drug addicts.
- Depressive illness
- Anxiety or bipolar illness. Its second component, melitracen acts against bipolar illnesses.
- Psychogenic depression
- Menopausal depression, where nothing else works
- Long lasting myogenic headache
- Resistant migraines
- Certain gastrointestinal disturbances which have a neurological component.
Contra-Indications of Flupentixol
- Concomitant use with the large dose of hypnotics
- Geriatric patients with confusion or agitation
- Hypersensitivity to this drug
- Patients with central nervous system depression
- Patients with dementia
- Patients with liver damage, cerebrovascular or renal insufficiency, and severe cardiovascular disorders
- Presence of alcohol, barbiturate, or opiate intoxication
- Psychoneurotic patients
- Severely agitated psychotic patients
Dosage of Flupentixol
Psychoses
- As decanoate: Initially, 20 mg (1 ml of a 2% oily solution) is given as test dose. After at least 7 days and depending on the response, subsequent doses of 20-40 mg may be given at intervals of 2-4 wk.
- Usual maintenance dose: 50 mg every 4 wk to 300 mg every 2 wk. Up to 400 mg wkly may be used in severe or resistant cases.
- Initial dose: ¼ or ½ of the usual initial dose.
Depression with or without anxiety
- Initially, 1 mg daily increased after 1 wk to 2 mg daily and then to a max of 3 mg daily, last dose should be given not later than 4 p.m.
- Doses >2 mg should be given in 2 divided doses. Discontinue treatment if there is no improvement within 1 wk of using the max dose.
- Initially, 0.5 mg daily increased after 1 wk to 1 mg daily with the last dose given not later than 4 p.m. Max: 2 mg daily in 2 divided doses.
Depression with psychoses
- Initially, 3-9 mg bid, adjusted according to response. Max: 18 mg daily.
- Initial dose: ¼ or ½ of the usual initial dose.
Side Effects of Flupentixol
The most common
- Weakness
- Drowsiness
- Anxiety
- Insomnia
- Dry mouth.
- Difficulty in breathing
- A headache
- Weight gain
- Nausea
- Upset stomach
- Decreased appetite
- Diarrhea
More common
- Sweating
- Blurred vision
- Dizziness.
- slower heart rate
- change in sex drive or performance
- diarrhea
- dry eyes
- hair loss
- nausea
- weakness or tiredness
Common
- Cough producing mucus
- difficulty with breathing
- tightness in the chest
- Abdominal or stomach pain and tenderness
- blistering, peeling, or loosening of the skin
- Anxiety
- dry mouth
- irritability
- shaking
- sleepiness or unusual drowsiness
- trouble sleeping
- unusual dreams blood in the urine
- Decreased appetite
Drug Interactions of Flupentixol
Flupenthixol may interact with following drugs, supplements & may change the efficacy of drugs
- antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- antiseizure medications (e.g., clobazam, phenobarbital, phenytoin, valproic acid, zonisamide)
- aripiprazole
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- baclofen
- barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- domperidone
- famotidine
- gabapentin
- ipratropium
- ketotifen
- levodopa
- macrolide antibiotics (e.g., azithromycin, clarithromycin, erythromycin)
- magnesium sulfate
- methylphenidate
- mirtazapine
- monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, rasagiline, selegiline, tranylcypromine)
- muscle relaxants (e.g., cyclobenzaprine, methocarbamol, orphenadrine)
- orphenadrine
- quinolone antibiotics (e.g., levofloxacin, norfloxacin, moxifloxacin)
- selective serotonin reuptake inhibitors (SSRIs; e.g., paroxetine, fluoxetine, citalopram)
- serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
- sotalol
- tapentadol
- thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, )
- thioridazine
- tolterodine
- tramadol
- trimethoprim
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- “triptan” migraine medications (e.g., eletriptan, sumatriptan)
- tryptophan
- tyrosine kinase inhibitors (e.g., dasatinib, imatinib, nilotinib, sunitinib)
- vardenafil
Pregnancy & Lactation of Flupentixol
FDA Pregnancy category C
Pregnancy
This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. Newborn babies who have been exposed to this medication in the last 3 months of pregnancy have experienced withdrawal symptoms after birth.
Lactation
This medication passes into breast milk. If you breastfeeding-feeding mother and are taking flupenthixol, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.
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