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Prochlorperazine

 

 
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Prochlorperazine
 
 
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Prochlorperazine (marketed under the names Compazine, Stemzine, Buccastem, Stemetil and Phenotil) is a drug that belongs to the phenothiazine
Phenothiazine

Phenothiazine is the organic compound with the formula S2NH. This yellow tricyclic compound is soluble in acetic acid, benzene, and ether....
 class of antipsychotic agents that are used for the treatment of nausea
Nausea

Nausea is the sensation of unease and discomfort in the stomach with an urge to vomit....
 and vertigo
Vertigo (medical)

Vertigo is a specific type of dizziness, a major symptom of a balance disorder. It is the sensation of spinning or swaying while the body is actually stationary with respect to the surroundings....
. It is also a typical antipsychotic
Typical antipsychotic

Typical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis , and are generally being replaced by atypical antipsychotic drugs....
 drug and a highly potent neuroleptic, 10 to 20 times more potent than chlorpromazine
Chlorpromazine

Chlorpromazine is a phenothiazine antipsychotic, and the oldest in the antipsychotic family of drugs. It is a typical antipsychotic. It is principally used in the treatment of schizophrenia, though it has also been used to treat severe manic episodes in people with bipolar disorder....
.

etil suppresses activity in the trigger zones of the vomiting center by paralyzing the gastrointestinal tract which governs the vomiting reflex, which can exacerbate dismotility.






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Prochlorperazine (marketed under the names Compazine, Stemzine, Buccastem, Stemetil and Phenotil) is a drug that belongs to the phenothiazine
Phenothiazine

Phenothiazine is the organic compound with the formula S2NH. This yellow tricyclic compound is soluble in acetic acid, benzene, and ether....
 class of antipsychotic agents that are used for the treatment of nausea
Nausea

Nausea is the sensation of unease and discomfort in the stomach with an urge to vomit....
 and vertigo
Vertigo (medical)

Vertigo is a specific type of dizziness, a major symptom of a balance disorder. It is the sensation of spinning or swaying while the body is actually stationary with respect to the surroundings....
. It is also a typical antipsychotic
Typical antipsychotic

Typical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis , and are generally being replaced by atypical antipsychotic drugs....
 drug and a highly potent neuroleptic, 10 to 20 times more potent than chlorpromazine
Chlorpromazine

Chlorpromazine is a phenothiazine antipsychotic, and the oldest in the antipsychotic family of drugs. It is a typical antipsychotic. It is principally used in the treatment of schizophrenia, though it has also been used to treat severe manic episodes in people with bipolar disorder....
.

Indications

Stemetil suppresses activity in the trigger zones of the vomiting center by paralyzing the gastrointestinal tract which governs the vomiting reflex, which can exacerbate dismotility. It works by affecting the chemical balance in the brain. The antiemetic action of Stemetil may mask the signs and symptoms of drug overdosage from other drugs and may obscure the diagnosis and treatment of other conditions. Gastrointestinal tract disruption may deprive the brain of essential nutrients for key metabolic pathways.

Stemetil (Procholorperazine) is a phenothiazine drug. Most drugs in this category are used as anti-psychotics(neuroleptics). Neuroleptic means "nerve seizing," and describes the semi-paralyzing effect these drugs have on the brain and nervous system. Stemetil® is no longer being manufactured for sale in Canada.

It is now relatively seldom used for the treatment of psychosis
Psychosis

Psychosis , with adjective psychotic, literally means abnormal condition of the mind, and is a generic psychiatry term for a mental state often described as involving a "loss of contact with reality"....
 and the manic
Manic

Manic is a List of Belgrade neighborhoods of Belgrade, the capital of Serbia. It is located in the municipality of Barajevo.Manic developed on the eastern slopes of the Kosmaj mountain....
 phase of bipolar disorder
Bipolar disorder

Bipolar disorder is a Classification of mental disorders that describes a category of mood disorders, or mood swings, defined by the presence of one or more episodes of abnormally elevated mood clinically referred to as mania or, if milder, hypomania....
. It has a prominent antiemetic/antivertiginoic activity and is most often used for the (short-time) treatment of nausea and vomiting and vertigo
Vertigo (medical)

Vertigo is a specific type of dizziness, a major symptom of a balance disorder. It is the sensation of spinning or swaying while the body is actually stationary with respect to the surroundings....
 as follows:

  1. To alleviate the symptoms of vertigo
  2. As an antiemetic
    Antiemetic

    An antiemetic is a medication that is effective against vomiting and nausea. Anti-emetics are typically used to treat motion sickness and the Adverse effect of opioid analgesics, general anaesthetics and chemotherapy directed against cancer....
    , particularly for nausea and vomiting caused by cancer treatment, radiation
    Radiation

    In physics, radiation describes any process in which energy emitted by one body travels through a medium or through space, ultimately to be absorbed by another body....
     and in the pre- and postoperative setting
    Postoperative nausea and vomiting

    Postoperative nausea and vomiting is an unpleasant complication affecting about a third of the 10% of the population undergoing general anaesthesia each year....
  3. Quite recently, in the UK prochlorperazine maleate has been made available as Buccastem M in buccal
    Buccal

    Buccal can refer to:* The adjective form of cheek* The buccal index* The buccal smear* The "buccal artery", also known as the Buccinator artery...
     form as an over-the-counter treatment for migraine. In this indication it blocks the chemoreceptor trigger zone
    Chemoreceptor trigger zone

    The Chemoreceptor trigger zone is an area of the brain which receives inputs from blood-borne drugs or hormones, and communicates with the Vomiting center, to initiate vomiting....
     (CTZ) in the brain, which is responsible for causing severe nausea and vomiting. Its OTC use is strictly restricted to a maximum of 2 days, because of the potentially severe side effect
    Adverse drug reaction

    An adverse drug reaction or adverse drug event is an expression that describes the unwanted, negative consequences associated with the use of given medications....
    s of prochlorperazine, which mandate supervision by a health care provider.
  4. In the UK prochlorperazine maleate has been prescribed to alleviate the symptoms of labyrinthitis
    Labyrinthitis

    Labyrinthitis is a balance disorder. It is an inflammatory process affecting the Labyrinth s that house the vestibular system of the inner ear....
    , which include not only nausea and vertigo, but spatial and temporal 'jerking' and distortion.


Formulations and pharmacokinetics

Prochlorperazine is available as an oral liquid, tablets, and suppositories, as well as in an injectable form.

Following intramuscular injection the antiemetic action is evident within 5 to 10 minutes and lasts for 3 to 4 hours. Rapid action is also noted after buccal treatment. With oral dosing the start of action is delayed but the duration somewhat longer (approximately 6 hours).

There is an inhaled form of prochlorperazine under development by Alexza Pharmaceuticals, currently in Phase II clinical trials.

Side effects

Due to the short duration of treatment it is usually well tolerated. It shares in general all side effects of chlorpromazine
Chlorpromazine

Chlorpromazine is a phenothiazine antipsychotic, and the oldest in the antipsychotic family of drugs. It is a typical antipsychotic. It is principally used in the treatment of schizophrenia, though it has also been used to treat severe manic episodes in people with bipolar disorder....
, but these are seen less frequently so and are less disturbing to the patient, particularly as most patients with the aforementioned conditions are hospitalized. In the treatment of nausea/emesis it might be given together with an antiparkinsonian drug to prevent extrapyramidal side effects of prochlorperazine.

Some individuals are inherently allergic to this medicine. This medicine is known to produce seizures and seizure-like symptoms in individuals who might not have had prior seizures. In such cases, contact health-care facilities for immediate attention. Long-term delays might lead to long-term effects. In extreme cases,as with any tonic clonic seizures, it has been known to produce permanent damage to the lower jaw and the jaw joint due to extended seizure symptoms. A common, over-the-counter remedy for side-effects is Diphenhydramine
Diphenhydramine

Diphenhydramine hydrochloride , trade name Benadryl as produced by McNeil Laboratories a division of J&J, or Dimedrol outside the U.S....
.

If treating psychotic conditions on a long-term basis, the high incidence of early and late (tardive dyskinesia
Tardive dyskinesia

Tardive dyskinesia is a variety of Dyskinesia manifesting as a side effect of long-term or high-dose use of dopamine antagonists, usually antipsychotics....
) extrapyramidal side effects should be considered carefully. Prochlorperazine has in the long-term treatment approximately the same incidence and severity of extrapyramidal side effects as haloperidol
Haloperidol

Haloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacology similar to the phenothiazines....
.

External links

  • medlineplus.org article
  • Press release pertaining to phase IIb clinical trial of inhaled prochlorperazine for migraine headache