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Antipsychotic

Prochlorperazine

Also called Compazine, Stemzine, Buccastem, Stemetil, Phenotil, Prochlorpromazine, Chlormeprazine, Chlorperazine

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Part of the metabolic pathway of Prochlorperazine. See the timeline on the metabolic highway.

Enzymes that break it down: CYP2D6 and CYP3A4. Wikipedia’s drug infobox says: “Mainly Liver (CYP2D6 and/or CYP3A4)” (revision 1373298496).

Common dose · Oral5–20 mg PW
Onset30–45 minutes PW
Total4–8 hours PW

Dosage

Oral

SourceThresholdLightCommonStrongHeavy
PsychonautWiki2 mg PW2.5–5 mg PW5–20 mg PW20–40 mg PW–
What dose are you on? (self-reported, unverified)
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Duration

Route · sourceOnsetCome-upPeakOffsetTotalAfter-effects
Oral · PsychonautWiki30–45 minutes PW–––4–8 hours PW–

Mixing

Acute combinations: what happens when these are taken close together. Entries backed by a medical journal or agency are listed first.

Backed by medical journals

Awaiting sourcePeer-reviewed reports on acute combinations, from PubMed and the journals the harm reduction sites cite.

Risks and toxicity

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.[10][11] PW

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). PW

Lethal dosage

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. PW

It is strongly recommended that one use harm reduction practices when using this drug. PW

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. PW

Median lethal dose (LD50) in animals

Quoted from PubChem's Non-Human Toxicity Values, which come from the Hazardous Substances Data Bank (HSDB). PubChem describes them as: “Quantitative non-human toxicity values (e.g., lethal dose) for this compound. The data shown here are mostly for lab animals (e.g., rat, mouse, guinea pig, and rabbit).” and defines the “LD50 (median lethal dose, the estimated amount of a chemical expected to kill 50% of test animals in a single dose)”. PC

LD50 (as the source gives it)Reference
LD50 Rat oral 1800 mg/kg PCLewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 3054 (via HSDB record 3171)
LD50 Mouse oral 400 mg/kg PCLewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 3054 (via HSDB record 3171)
LD50 Mouse ip 120 mg/kg PCLewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 3054 (via HSDB record 3171)
LD50 Mouse sc 400 mg/kg PCLewis, R.J. Sr. (ed) Sax's Dangerous Properties of Industrial Materials. 11th Edition. Wiley-Interscience, Wiley & Sons, Inc. Hoboken, NJ. 2004., p. 3054 (via HSDB record 3171)

Testing

Awaiting sourceReagent reactions and test kit guidance from a harm reduction testing service.

Effects

Awaiting sourceSubjective and physical effects from PsychonautWiki or TripSit.

Overview

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.[1] PW

Prochlorperazine, formerly sold under the brand name Compazine among others, is a medication used to treat nausea, migraines, schizophrenia, psychosis and anxiety. It is a less preferred medication for anxiety. It may be taken by mouth, rectally, injection into a vein, or injection into a muscle.[2–6] WP

Common side effects include sleepiness, blurry vision, low blood pressure, and dizziness. Serious side effects may include movement disorders including tardive dyskinesia and neuroleptic malignant syndrome. Use in pregnancy and breastfeeding is generally not recommended. It is a typical antipsychotic which is believed to work by reducing the action of dopamine in the brain.[3][7] WP

Prochlorperazine was approved for medical use in the United States in 1956. It is available as a generic medication. In 2020, it was the 355th most commonly prescribed medication in the United States, with more than 600 thousand prescriptions.[3][4][8][9] WP

History

Awaiting sourceHistory and culture from Wikipedia or PsychonautWiki, with their citations.

Pharmacology

Pharmacology

Prochlorperazine is thought to exert its antipsychotic effects by blocking dopamine receptors.[21] WP

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. Hyperprolactinemia is a side effect of dopamine antagonists as blockade of D₂ receptors within the tuberoinfundibular pathway results in increased plasma levels of prolactin due to increased secretion by lactotrophs in the anterior pituitary. WP

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

Receptor binding · Wikipedia

Prochlorperazine

col1col2col3col4
5-HT1A5,888Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
5-HT2A7.24Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
5-HT2C123Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
5-HT₃1349Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
5-HT₆148Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
5-HT₇6,760Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
α₁24Human[18] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
α₂1700Human[18] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
M₁776Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
M₂1413Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
D₁251Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
D₂2.24Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
D₃1.82Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
D₄5.37Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
H₁6.03Human[19] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
H₃17,378Human[19] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
H₄17783Human[19] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
DAT589Human[17] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.
NET600Rat[20] WP⚠ This row of the source table has a different number of cells than its headings, so columns may not line up.

Chemistry

Formula
C20H24ClN3S PC
CAS number
58-38-8 PC
Molar mass (g/mol)
373.9 PC
IUPAC name (computed by PubChem)
2-chloro-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine PC
SMILES
CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl PC
InChIKey
WIKYUJGCLQQFNW-UHFFFAOYSA-N PC
PubChem CID
4917

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Pop culture

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References

  1. Other Husseini, A; Gianakos, D (February 2006). "The 15-Minute Visit". Patient Care 40: 9–10
  2. Other Side Effects of Compazine (Prochlorperazine), Warnings, Uses
  3. Other Prochlorperazine Monograph for Professionals
  4. Other British national formulary: BNF 76. 2018
  5. Journal / agency Orr SL, Friedman BW, Christie S, Minen MT, Bamford C, Kelley NE, Tepper D. Management of Adults With Acute Migraine in the Emergency Department: The American Headache Society Evidence Assessment of Parenteral Pharmacotherapies. Headache. June 2016. doi:10.1111/head.12835 · PMID 27300483
  6. Journal / agency Din L, Preuss CV. StatPearls [Internet]. March 2022. PMID 30725768
  7. Other Prochlorperazine Use During Pregnancy
  8. Other The Top 300 of 2020
  9. Other Prochlorperazine - Drug Usage Statistics
  10. Other Brown, T. M., Stoudemire, A. Psychiatric Side Effects of Prescription and Over-the-counter Medications: Recognition and Management. 1998
  11. Other http://www.drugs.com/sfx/procot-side-effects.html
  12. Other 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) #l:Buccastem M use guide, last revised in January 2016..pdf
  13. Other Buccastem M - Summary of Product Characteristics (SPC) - (eMC). 16 February 2016
  14. Other Medicines information
  15. Other Prochlorperazine international brands
  16. Other Compazine (Prochlorperazine) Patient Information: Side Effects and Drug Images at RxList
  17. Journal / agency Silvestre JS, Prous J. Research on adverse drug events. I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes. Methods and Findings in Experimental and Clinical Pharmacology. June 2005. doi:10.1358/mf.2005.27.5.908643 · PMID 16082416
  18. Journal / agency Richelson E, Nelson A. Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. European Journal of Pharmacology. August 1984. doi:10.1016/0014-2999(84)90478-3 · PMID 6149136
  19. Journal / agency Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R. Interactions of recombinant human histamine H₁R, H₂R, H₃R, and H₄R receptors with 34 antidepressants and antipsychotics. Naunyn-Schmiedeberg's Archives of Pharmacology. February 2012. doi:10.1007/s00210-011-0704-0 · PMID 22033803
  20. Journal / agency Richelson E, Pfenning M. Blockade by antidepressants and related compounds of biogenic amine uptake into rat brain synaptosomes: most antidepressants selectively block norepinephrine uptake. European Journal of Pharmacology. September 1984. doi:10.1016/0014-2999(84)90403-5 · PMID 6499924
  21. Other Ebadi MS. Desk Reference of Clinical Pharmacology. 2007

Text and values on this page are quoted from PsychonautWiki (CC BY-SA 4.0), Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.