Prochlorperazine (marketed under the names Compazine, Stemzine, Buccastem, Stemetil and Phenotil) is a drug 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 to 20 times more potent than chlorpromazine. [edit] Indications Prochlorperazine is a phenothiazine drug. Most drugs in this category are used as anti-psychotics (neuroleptics).[1] 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 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: - To alleviate the symptoms of Vertigo[2]
- As an antiemetic, particularly for nausea and vomiting caused by chemotherapy, radiation therapy and in the pre- and postoperative setting[3]
- In the UK, prochlorperazine maleate is available as Buccastem M in buccal form as an over-the-counter treatment for migraine.[4] In this indication it blocks the chemoreceptor trigger zone (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 effects of prochlorperazine, which mandate supervision by a health care provider.
- In the UK prochlorperazine maleate has been prescribed to alleviate the symptoms of labyrinthitis, which include not only nausea and vertigo, but spatial and temporal 'jerking' and distortion[5]
[edit] 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[when?] in Phase II clinical trials.[6] [edit] Side effects Many individuals are inherently allergic to this medicine. Prochlorperazine can cause tardive dyskinesia, a condition involving unusual, uncontrollable body or face movements (including abnormal movements of the tongue). The condition can become permanent even if prochlorperazine is stopped. 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). This medicine is a direct blood reactant and can cause severe circulatory damage when used as an i.v. push drug in emergency rooms. [edit] References - ^ Casey JF, Lasky JJ, Klett CJ, Hollister LE (August 1960). "Treatment of schizophrenic reactions with phenothiazine derivatives. A comparative study of chlorpromazine, triflupromazine, mepazine, prochlorperazine, perphenazine, and phenobarbital". American Journal of Psychiatry 117: 97–105. DOI 10.1176/appi.ajp.117.2.97. PMID 13808146.
- ^ Benson AJ (June 1969). "Effect of diphenidol and prochlorperazine on semicircular canal function in man". Aerospace Medicine 40 (6): 589–95. PMID 4891872.
- ^ Gralla RJ, Osoba D, Kris MG, et al. (September 1999). "Recommendations for the use of antiemetics: evidence-based, clinical practice guidelines". Journal of Clinical Oncology 17 (9): 2971–94. PMID 10561376. http://jco.ascopubs.org/cgi/content/full/17/9/2971. Retrieved 2009-06-21.
- ^ Siow HC, Young WB, Silberstein SD (April 2005). "Neuroleptics in headache". Headache 45 (4): 358–71. doi:10.1111/j.1526-4610.2005.05074.x. PMID 15836574.
- ^ Coatesworth AP (November 2000). "Assessment and treatment of dizziness". Journal of Neurology, Neurosurgery, and Psychiatry 69 (5): 706. DOI 10.1136/jnnp.69.5.706. PMID 11184241.
- ^ Alexza Pharmaceuticals (2009-06-15). "[www.prnewswire.com/news-releases/alexza-announces-agreement-to-acquire-symphony-allegro-including-all-rights-to-az-004-az-104-and-az-002-62125847.html Alexza Announces Agreement to Acquire Symphony Allegro, Including All Rights to AZ-004, AZ-104 and AZ-002]". Press release. www.prnewswire.com/news-releases/alexza-announces-agreement-to-acquire-symphony-allegro-including-all-rights-to-az-004-az-104-and-az-002-62125847.html. Retrieved 2009-11-29.
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