Prochlorperazine
Encyclopedia
Prochlorperazine is a dopamine (D2) receptor antagonist that belongs to the phenothiazine
class of antipsychotic agents that are used for the antiemetic
treatment of nausea
and vertigo
. It is also a highly-potent typical antipsychotic
, 10-20x more potent than chlorpromazine
. It is also used to treat migraine headaches. Intravenous administration can be used to treat status migrainosus
.
It is now relatively seldom used for the treatment of psychosis
and the manic
phase of bipolar disorder
. It has a prominent antiemetic
/antivertiginoic activity and is most often used for the (short-time) treatment of nausea and vomiting and vertigo
as follows:
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).
It is available in Egypt under the brand name Emedrotec buccal adhesive tablets by Eva pharma.
There is an inhaled form of prochlorperazine under development by Alexza Pharmaceuticals, currently in Phase II clinical trials.
Symptoms of a reaction include dyskinesia (unusual, uncontrollable body or face movements, including abnormal movements of the tongue, also known as dystonia
), seizures and seizure-like symptoms in individuals who have never had a seizure before.
Long-term delay of medical treatment can lead to long-term effects. In extreme cases, it has been known to produce permanent damage to the lower jaw and the jaw joint due to extended seizure symptoms.
Prochlorperazine can also cause a life-threatening condition called neuroleptic malignant syndrome
(NMS). Some symptoms of NMS include: A high fever, stiff muscles, confusion, irregular pulse or blood pressure, a fast heart rate (tachycardia), sweating, irregular heart rhythms (arrhythmias).
VA and FDA research shows injection site reaction.
Phenothiazine
Phenothiazine is an organic compound that occurs in various antipsychotic and antihistaminic drugs. It has the formula S2NH. This yellow tricyclic compound is soluble in acetic acid, benzene, and ether. The compound is related to the thiazine-class of heterocyclic compounds...
class of antipsychotic agents that are used for the antiemetic
Antiemetic
An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer....
treatment of nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
and vertigo
Vertigo (medical)
Vertigo is a type of dizziness, where there is a feeling of motion when one is stationary. The symptoms are due to a dysfunction of the vestibular system in the inner ear...
. It is also a highly-potent typical antipsychotic
Typical antipsychotic
Typical antipsychotics are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis...
, 10-20x more potent than chlorpromazine
Chlorpromazine
Chlorpromazine is a typical antipsychotic...
. It is also used to treat migraine headaches. Intravenous administration can be used to treat status migrainosus
Status migrainosus
Status migrainosus is a debilitating migraine headache lasting for more than 72 hours....
.
Indications
Prochlorperazine 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 as an anti-psychotic, but it is still available for treatment of nausea, etc.It is now relatively seldom used for the treatment of psychosis
Psychosis
Psychosis means abnormal condition of the mind, and is a generic psychiatric term for a mental state often described as involving a "loss of contact with reality"...
and the manic
Mania
Mania, the presence of which is a criterion for certain psychiatric diagnoses, is a state of abnormally elevated or irritable mood, arousal, and/ or energy levels. In a sense, it is the opposite of depression...
phase of bipolar disorder
Bipolar disorder
Bipolar disorder or bipolar affective disorder, historically known as manic–depressive disorder, is a psychiatric diagnosis that describes a category of mood disorders defined by the presence of one or more episodes of abnormally elevated energy levels, cognition, and mood with or without one or...
. It has a prominent antiemetic
Antiemetic
An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer....
/antivertiginoic activity and is most often used for the (short-time) treatment of nausea and vomiting and vertigo
Vertigo
Vertigo is a form of dizziness.Vertigo may also refer to:* Vertigo , a 1958 film by Alfred Hitchcock**Vertigo , its soundtrack** Vertigo effect, or Dolly zoom, a special effect in film, named after the movie...
as follows:
- To alleviate the symptoms of vertigoVertigoVertigo is a form of dizziness.Vertigo may also refer to:* Vertigo , a 1958 film by Alfred Hitchcock**Vertigo , its soundtrack** Vertigo effect, or Dolly zoom, a special effect in film, named after the movie...
- As an antiemeticAntiemeticAn antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer....
, particularly for nausea and vomiting caused by chemotherapyChemotherapyChemotherapy is the treatment of cancer with an antineoplastic drug or with a combination of such drugs into a standardized treatment regimen....
, radiation therapyRadiation therapyRadiation therapy , radiation oncology, or radiotherapy , sometimes abbreviated to XRT or DXT, is the medical use of ionizing radiation, generally as part of cancer treatment to control malignant cells.Radiation therapy is commonly applied to the cancerous tumor because of its ability to control...
and in the pre- and postoperative settingPostoperative nausea and vomitingPostoperative nausea and vomiting is an unpleasant complication affecting about a third of the 10% of the population undergoing general anaesthesia each year. This equates to about two million people in the United Kingdom annually.-Impact:... - In the UK, prochlorperazine maleate is available as Buccastem M in buccalBuccalBuccal may refer to:* Mouth, a body cavity** Specifically the cheek* Buccal artery...
form as an over-the-counter treatment for migraine. In this indication it blocks the chemoreceptor trigger zoneChemoreceptor trigger zoneThe chemoreceptor trigger zone , is an area of the medulla that receives inputs from blood-borne drugs or hormones, and communicates with the vomiting center, to initiate vomiting. The CTZ is close to the area postrema on the floor of the fourth ventricle and is outside of the blood-brain barrier...
(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 effectAdverse drug reactionAn adverse drug reaction is an expression that describes harm associated with the use of given medications at a normal dosage. ADRs may occur following a single dose or prolonged administration of a drug or result from the combination of two or more drugs...
s of prochlorperazine, which mandate supervision by a health care provider. - In the UK prochlorperazine maleate has been prescribed to alleviate the symptoms of labyrinthitisLabyrinthitisLabyrinthitis is an inflammation of the inner ear, and a form of unilateral vestibular dysfunction. It derives its name from the labyrinths that house the vestibular system . Labyrinthitis can cause balance disorders....
, which include not only nausea and vertigo, but spatial and temporal 'jerking' and distortion
Pharmacology
Prochlorperazine is thought to exert its antipsychotic effects by blocking dopamine receptors.Formulations and pharmacokinetics
Prochlorperazine is available as an oral liquid, tablets, cream for trans dermal(compounding pharmacy), 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).
It is available in Egypt under the brand name Emedrotec buccal adhesive tablets by Eva pharma.
There is an inhaled form of prochlorperazine under development by Alexza Pharmaceuticals, currently in Phase II clinical trials.
Side effects
Hypersensitivities to prochlorperazine can occur and there is cross-reactivity with other drugs in the phenothiazine class.Symptoms of a reaction include dyskinesia (unusual, uncontrollable body or face movements, including abnormal movements of the tongue, also known as dystonia
Dystonia
Dystonia is a neurological movement disorder, in which sustained muscle contractions cause twisting and repetitive movements or abnormal postures. The disorder may be hereditary or caused by other factors such as birth-related or other physical trauma, infection, poisoning or reaction to...
), seizures and seizure-like symptoms in individuals who have never had a seizure before.
Long-term delay of medical treatment can lead to long-term effects. In extreme cases, it has been known to produce permanent damage to the lower jaw and the jaw joint due to extended seizure symptoms.
Prochlorperazine can also cause a life-threatening condition called neuroleptic malignant syndrome
Neuroleptic malignant syndrome
Neuroleptic malignant syndrome is a life- threatening neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs...
(NMS). Some symptoms of NMS include: A high fever, stiff muscles, confusion, irregular pulse or blood pressure, a fast heart rate (tachycardia), sweating, irregular heart rhythms (arrhythmias).
VA and FDA research shows injection site reaction.
Chemistry
Prochlorpherazine (2-chloro-10-[3-(4-methyl-1-piperazinyl) propyl]-phenothiazine) is prepared by the alkylation of 2-chlorophenothiazine using 4-methyl-1-piperazinyl)propyl-3-chloride in the presence of sodamide, or alkylation of 2-chloro-10-[(3-chloropropyl)]phenothiazine using 1-methylpiperazine.- R.J. Horclois, (1959).
- R.J. Horclois, (1957).
- R.J. Horclois, (1955).
- R.J. Horclois, (1959).
External links
- Prochlorperazine. MedlinePlus. U.S. National Library of MedicineUnited States National Library of MedicineThe United States National Library of Medicine , operated by the United States federal government, is the world's largest medical library. Located in Bethesda, Maryland, the NLM is a division of the National Institutes of Health...
. National Institutes of HealthNational Institutes of HealthThe National Institutes of Health are an agency of the United States Department of Health and Human Services and are the primary agency of the United States government responsible for biomedical and health-related research. Its science and engineering counterpart is the National Science Foundation...
. - AZ-001 (Staccato prochlorperazine) Press release pertaining to phase IIb clinical trial of inhaled prochlorperazine for migraine headache
- Prochlorperazine edisylate Injection prescribing information Drugs.com
- Prochlorperazine. Hazardous Substances Data BankHazardous Substances Data BankThe Hazardous Substances Data Bank is a toxicology database on the U.S. National Library of Medicine's Toxicology Data Network . It focuses on the toxicology of potentially hazardous chemicals, and includes information on human exposure, industrial hygiene, emergency handling procedures,...
(HSDB). U.S. National Library of MedicineUnited States National Library of MedicineThe United States National Library of Medicine , operated by the United States federal government, is the world's largest medical library. Located in Bethesda, Maryland, the NLM is a division of the National Institutes of Health...
. National Institutes of HealthNational Institutes of HealthThe National Institutes of Health are an agency of the United States Department of Health and Human Services and are the primary agency of the United States government responsible for biomedical and health-related research. Its science and engineering counterpart is the National Science Foundation...
.