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Prochlorperazine
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| Systematic (IUPAC) name | |
| 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]- 10H-phenothiazine |
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| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C20H24ClN3S |
| Mol. mass | 373.943 g/mol |
| Pharmacokinetic data | |
| Bioavailability | not exactly known, but substantial |
| Protein binding | 91–99% |
| Metabolism | Mainly hepatic (CYP2D6 and/or CYP3A4) |
| Half life | 4-8 hours, differs with the mode of application |
| Excretion | Biliary, (colored) inactive metabolites in urine |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral, buccal, rectal, IM |
Prochlorperazine (marketed under the names Compazine, Buccastem, Stemetil and Phenotil) is a drug that belongs to the phenothiazine class of antipsychotic agents that are used for the treatment of nausea and vertigo. It is also a typical antipsychotic drug and a highly potent neuroleptic, 10 to 20 times more potent than chlorpromazine.
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Indications
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
- As an antiemetic, particularly for nausea and vomiting caused by cancer treatment, radiation and in the pre- and postoperative setting
- Quite recently, in the UK prochlorperazine maleate has been made available as Buccastem M in buccal form as an over-the-counter treatment for migraine. 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.
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
- Further information: Typical antipsychotic
Due to the short duration of treatment it is usually well tolerated. It shares in general all side effects of chlorpromazine, 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.
If treating psychotic conditions on a long-term basis, the high incidence of early and late (tardive dyskinesia) 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.
External links
- Prochlorperazine medlineplus.org article
- AZ-001 (Staccato(TM) prochlorperazine) Press release pertaining to phase IIb clinical trial of inhaled prochlorperazine for migraine headache
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Wikipedia content modification information:
- This page was last modified on 3 October 2008, at 10:46.
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