The Great Flupentixol And Its Application

Flupentixol: is an antipsychotic major tranquilizer, it's thioxanthene, and thus it's closely associated with the phenothiazine, its primary use is as a long-acting in action two or three weekly to people with schizophrenia who have poor compliance of medicine and suffer a frequent relapse of illness

-flupentixol: also referred to like the distinctive flupenthixol under brand names such as depixol and flannel, the standard master sedative for the thioxanthene class, was introduced in 1965 by Lund Buck, as well as a single drug preparation, which is also available as flupentixol/melitracen, a mixture medication that contains It contains both melioration (tricyclic antidepressant) and flupitenexol

_flupentixol isn't approved In use, however, it's approved in use in us, Australia, Russia, South Africa, and New Zeeland
Various information about flupentixol

1- Mechanism of the action:-

  • Flupentixol may be a thioxanthene antipsychotic neuroleptics, anxiolytic, antidepressant and mood-stabilizing drug.
  • The mechanism of action of Flupenthixol isn't completely understood. Flupenthixol may be a powerful antagonist of both D1 and D2 dopamine receptors and an alpha-receptor antagonist.
  •  Its antipsychotic activity is assumed to be associated with blocks postsynaptic dopamine receptors within the CNS.
  • Therefore, it increases the quantity of serotonin and noradrenaline that control mood and thinking, It’s structure closely associated with the phenothiazines.

2- Side effects and undesirable results:-

Undesirable effects
  • Cases of suicidal ideation and suicidal behaviors are reported during flupentixol therapy or early after treatment discontinuation.
  • The bulk of undesirable effects are dose-dependent. The frequency and severity are most pronounced within the early phase of treatment and decline during continued treatment.
  • Extrapyramidal reactions may occur, especially within the early phase of treatment.
  •  In most cases these side effects are often satisfactorily controlled by reduction of dosage and/or use of antipsychotic drugs.
  •  The routine prophylactic use of antiparkinsonian drugs isn't recommended. 
  • Antiparkinsonian drugs don't alleviate dyskinesia and should aggravate them.
  • Reduction in dosage or, if possible, discontinuation of flupentixol therapy is suggested. In persistent akathisia a benzodiazepine or propranolol could also be useful.

What are the possible side effects of Fluanxol?

Medicines and their possible side effects can affect individual people in several ways.
 the subsequent are a number of the side effects that are known to be related to flupentixol.
simply because a side effect is stated here doesn't suggest that each one people taking Fluanxol will experience that or any side effect.

  • Very common
  • Common
  • Uncommon

Affect quite (1 in 10 people):
  •  xerostomia.
  •  Sleepiness.
  • Feeling restless and unable to stay still (akathisia).

affect  1 in 10 and 1 in 100 people:

disturbances like blurred vision.
  •  Headache.
  •  Dizziness.
  •  Tremor.
  •  Problems concentrating.
  •  Feeling weak or tired.

affect  1 in 10 and 1 in 1000 people:

  • Feeling nervous or agitated.
  • Fast heartbeat or palpitations.
  • sleeping (insomnia).
  • Producing more saliva than Decreased appetite.
  • usual. Sweating. Itching.
  •  Difficulty passing urine.
  •  Disturbances of the gut like constipation, diarrhea, indigestion, vomiting.
  •  Reduced drive.
  •  Increased appetite and weight gain.
  •  Skin reactions like rashes or increased sensitivity to sunlight.
  •  Confusion.
  •  Speech problems

Abnormal involuntary body movements, eg affect fewer than 1 in 1000 people):
tremor, twitching,
rigidity (dyskinesias).
Sexual problems, like male erecticle dysfunction or problems with orgasm.
* Convulsions (fits or seizures).

RARE

  • Hyperprolactinemia.
  •  Sometimes this will cause symptoms like breast enlargement, production of milk and stopping of menstrual periods.
  • The decrease within the number of white blood cells or platelets within the blood (leucopenia or thrombocytopenia)
  • Unexplained bruising or bleeding, purple spots. pharyngitis.
  •  mouth ulcers or a heat (fever).
  •  Irregular heartbeats (arrhythmias).
  • Jaundice or liver problems observed yellowing skin and eye.
  •  grume during a vein (deep vein thrombosis) or within the lungs (pulmonary embolism) appeared as some symptoms : (stabbing pains and/or unusual redness or swelling in one leg, pain on breathing or coughing, expulsion blood or sudden breathlessness.)
  • High temperature combined with falling levels of consciousness, paleness, sweating, muscle stiffness and a quick heartbeat
  • (neuroleptic malignant syndrome). 
  • It requires stopping drugs and immediate medical treatment.

3- Contraindication,precaution: contraindicated in:

1- Hypersensitivity to flupentixol or other thioxanthenes (cross-sensitivity with phenothiazines may occur)
2_ CNS depression thanks to any cause, including comatose states, cortical brain damage (known or suspected), or circulatory collapse
3- Opiate, alcohol or barbiturate intoxication; Hepatic impairment, cerebrovascular insufficiency or severe cardiovascular pathology; Concurrent use of other drugs known to prolong QT interval; Pedi: Safety and effectiveness not established; not recommended. Use Cautiously
4- Brain tumors or ileus (may mask symptoms) Patients exposed to extreme heat
5- organophosphorus insecticides; Risk factors for/history of stroke; Any risk factors for QT prolongation including hypokalemia, hypomagnesemia, genetic predisposition, disorder history (including bradycardia), recent MI, HF or arrhythmias
6_ Known/suspected glaucoma; History of seizures (may ↓ seizure threshold); paralysis agitans (may worsen symptoms); Geri: Consider age-related ↓ in renal, cardiac and hepatic function; OB: Use as long as expected benefit outweighs potential risks to the infant; Lactation: Safe use not established; low levels in breast milk aren't expected to affect infant if therapeutic doses are used.

4-drug interaction:-

1. Flupentixol enhances the sedative response to alcohol and hence the consequences of barbiturates and other central nervous system depressants.
2. It should not be administered in high doses of hypnotics due to the possibility of strengthening.
3. Flupentixol should not be tilted in conjunction with guanethidine or similar compounds, since antipsychotic medications such as flupentixol may prevent the hypotensive effect of these compounds.
4. Many antipsychotic and tricyclic medications may prevent each other's metabolism interchangeably.
5. Concurrent use of metoclopramide increases the risk of extrapyramidal symptoms.
6. Flupentixol may antagonize the results of levodopa and dopamine agonists.
Simultaneous use of levodopa with Flupentixol may prevent the antiparkinson effects of levodopa because neoxanthin blocks the dopamine receptors inside the brain.
7. Antipsychotics

should be used in a long-acting depot (such as Fluanxol Depot) with caution along with other medications known to have pure suppression potentials, as they cannot be far from the body quickly in the conditions that this may require.
8. Medications are known to increase the QT interval joint administration of these drugs should be avoided.

Related chapters include:
- Class Ia and III arrhythmias eg: quinidine, amiodarone, sotalol

  • Some antipsychotics such as thioridazine.
  • Some macrolides such as erythromycin
  • Some quinolone antibiotics such as moxifloxacin

The above list is not exhaustive and other individual drugs known to significantly increase the QT period (such as lithium) should be avoided.
9. It is known that medications cause electrolyte disorders such as thiazide diuretics (hypokalemia) and medications to increase plasma concentration of flupentixol should be used with caution as they will increase the risk of prolonging QT and malignant arrhythmias.
10. amphetamines
Concomitant use with Flupentixol may inhibit the stimulating effects of the central nervous system of amphetamines due to the blockade of adrenergic alpha by thioxanthene; also, the antipsychotic effects of thioxanthene can be reduced by simply using it concurrently with amphetamines
11. Antacids or diarrhea antiperspirants
(Concurrent use may prevent Flupentixol oral absorption)
12. Bromocriptine
(Concomitant use with Flupentixol may increase prolactin concentrations in the blood and interfere with the effects of bromocriptine; adjusting the dose of bromocriptine may be necessary)
13. Drugs toxic to the ear, especially toxic ear antibiotics
(Concomitant use with Flupentixol may mask symptoms of auric toxicity such as tinnitus, dizziness or lightheadedness)
14. phenylephrine(Previous use of Flupentixol may reduce the pressure response to phenylephrine thanks to the action of alpha-adrenergic blocking of thioxanthene)
15. Kennedy(Concomitant use with Flupentixol may end with added heart effects

5- Uses: -

1- It has the properties of activating the central nervous system
2 - It is considered one of the factors that control irritable psychotic behavior, relieve severe psychotic states, reduces psychotic symptoms, and leads to a calming effect. But not in enthusiastic or obsessive patients.
3- It is used in schizophrenia.
Senile dementia transient psychosis after surgery, conditions such as schizophrenia and depression. This medicine is not recommended for use in patients but at the age of 18.
4- The main use of Flupentixol is a long-acting injection given once every two or three weeks for people with schizophrenia and those with poor compliance with medications and who suffer frequent relapses of the disease, although it is commonly given as a tablet. However, there is little evidence to support its use of this indicator.
Flupentixol is used in minimal doses as an antidepressant.
5- As an anti-depressant and mood stabilizer. It blocks the central monoamine receptors, especially the dopamine D1 and D2 receptors.
Therefore, it increases the number of Serotonin and Noradrenaline that controls mood and thinking and improves mood
6- These medications are often referred to as antipsychotics that indicate a tendency to present neurological side effects, but not all antipsychotics are likely to provide such effects.
 Many of these medications can also be effective against nausea, vomiting, and itching.

References:-

https://www.drugs.com/mmx/flupentixol.html
https://www.drugbank.ca/drugs/DB00875 (Drug Bank)
https://www.lundbeck.com/upload/ca/en/files/pdf/pm/Fluanxol PM EN 12Dec 2017.pdf
https://pubchem.ncbi.nlm.nih.gov/compound/5281881#section=Chemical-Disease-Co-Occurrences-in-Literature (PubChem)

Thank you and good luck