|Summary sheet: Prochlorperazine|
|Common names||Compazine, Stemzine, Buccastem, Stemetil, Phenotil|
|Systematic name||2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]- 10H-phenothiazine|
|Routes of Administration|
Prochlorperazine (Compazine, Stemzine, Buccastem M, Stemetil, Phenotil) is a dopaminergic D2 receptor antagonist that belongs to the phenothiazine class of antipsychotic agents that are used for the treatment of nausea and vertigo. It is also a highly potent typical antipsychotic and is 10–20× more potent than chlorpromazine. It is also used to treat migraine headaches.
Prochlorperazine is a piperazine derivative of the phenothiazine class of organic compounds. Prochlorperazine contains a thiazine ring, a six-member ring which includes one nitrogen and one sulfur atom. The thiazine ring is fused to two benzene rings, creating a tricyclic phenothiazine. Prochlorperazine contains a chlorine atom bound to R2 of the phenothiazine group.
Additionally, there is a three carbon propyl chain bound at R10 to the nitrogen atom of the structure. The propyl chain is bound at its terminal carbon to a piperazine ring at R1. Piperazine is a six-membered saturated ring with two nitrogen atoms at positions 1 and 4. The piperazine ring of prochlorperazine is also substituted at R4 with a methyl group. Prochlorperazine is found in pills as a maleate. It is analogous to chlorpromazine, another antipsychotic phenothiazine.
Prochlorperazine is analogous to chlorpromazine; both of these agents antagonize dopaminergic D2 receptors in various pathways of the central nervous system. This D2 blockade results in antipsychotic, antiemetic and other effects.
Disclaimer: The effects listed below are cited from the subjective effect index, which is based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be treated with a healthy degree of skepticism. It is worth noting that these effects will rarely (if ever) occur all at once, although higher doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- The general head space of prochlorperazine is often described as one of sleepiness, emptiness, apathy, stupor and catatonia. The specific cognitive effects can be broken down into several components which progressively intensify proportional to dosage. These are described below and generally include:
Toxicity and harm potential
Nervous system side effects have been associated with the use of prochlorperazine. Extrapyramidal side effects such as acute dystonic reactions, pseudoparkinsonism (not to be confused with Parkinson's disease), or akathisia can affect 2% of patients at low doses, whereas higher doses may affect as many as 40% of patients.
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, or irregular heart rhythms (arrhythmias).
The lethal dosage of this compound is unknown. Symptoms of overdose, however, may include agitation, coma, confusion, difficulty breathing, fainting, irregular heartbeat, loss of consciousness, muscle spasms, uncontrolled muscle movements, restlessness, seizures, severe constipation, stomach pain, severe drowsiness, dizziness, tremors, or trouble urinating.
It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
As with other antipsychotics, dependence can be present with long-term use and is both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage.
- Australia: The substance is Schedule 3, meaning it is available with the advice of a pharmacist without a prescription.
- United Kingdom: The drug is available over the counter as a pharmacy medicine and as a prescription medication. The OTC brand is Buccastem M, a buccal delivery system of prochlorperazine for motion sickness or nausea.
- United States: Prochlorperazine is available only through prescription.
- Husseini, A; Gianakos, D (February 2006). "The 15-Minute Visit". Patient Care 40: 9–10.
- Manuchair S. Ebadi, Desk reference of clinical pharmacology. 2007
- Psychiatric Side Effects of Prescription and Over-the-counter Medications | http://books.google.com.au/books?id=K7kevbILCuQC&source=gbs_navlinks_s
- Package leaflet: Information for the user. Buccastem® M Buccal Tablets (PROCHLORPERAZINE MALEATE 3 MG, EQUIVALENT TO 1.85 MG PROCHLORPERAZINE BASE) Alliance Pharmaceuticals, LTD. (2016) Buccastem M use guide, last revised in January 2016.