Pentazocine
Also called Talwin, Fortalgesic, Fortral, Sosigon
Part of the metabolic pathway of Pentazocine. See the timeline on the metabolic highway.
Dosage
Intramuscular
Intravenous
TripSit dose text
TripSit's factsheet also states its doses as text.
IM Light: 10-20mg Common: 20mg-30mg Strong: 30-60mg ( Do NOT Exceed 60mg) | IV Light: 5-10mg Common: 10-20mg Strong: 30mg (Do NOT Exceed 30mg) TS
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Duration
TripSit factsheet
Mixing
For best safety practice, don't mix this drug with other depressants.
Why: respiratory depression. PsychonautWiki says:
- “Respiratory depression (also known as hypoventilation) can be described as a reduced urge to breathe that can be fatal depending on its intensity.” (PsychonautWiki, Respiratory depression, revision 150612)
- “... otherwise safe dosages of these compounds can become fatal when combined with even small amounts of other classes of depressant. For example, benzodiazepines combined with opioids are an extremely common cause of fatal respiratory depression. It is therefore strongly discouraged to combine these depressants at any dosage range.” (PsychonautWiki, Respiratory depression, revision 150612)
- “The most common cause of substance-related deaths is the combination of depressants (such as opiates, benzodiazepines, or alcohol) with other depressants.” (PsychonautWiki, Responsible drug use, revision 168206)
- “This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration.” (PsychonautWiki, dangerous interactions table, "Depressants" row, revision 156847)
Quotes from PsychonautWiki, CC BY-SA 4.0.
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
TripSit combination chart
TripSit rates each pairing. Only pairings with a number carry a citation from TripSit. See the whole chart; TripSit's own notes are on combo.tripsit.me.
Risks and toxicity
TripSit factsheet
- Avoid
- All other CNS depressants[1] TS
- Warning
- When mixed with a barbituate in a syringe it will crystallize which can be fatal.[1] TS
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 male subcutaneous 175 +/- 36 mg/kg PC | Budavari, S. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Whitehouse Station, NJ: Merck and Co., Inc., 1996., p. 1225 (via HSDB record 3150) |
| LD50 Rat oral 1110 mg/kg PC | Lewis, R.J. Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold, 1996., p. 1275 (via HSDB record 3150) |
| LD50 Rat sc 61 mg/kg PC | Lewis, R.J. Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold, 1996., p. 1275 (via HSDB record 3150) |
| LD50 Rat iv 21 mg/kg PC | Lewis, R.J. Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold, 1996., p. 1275 (via HSDB record 3150) |
Testing
Effects
Overview
A synthetic opioid used as an analgesic. It is only used IM and IV in the medical field and has respiratory depressant effects. It is pregnancy category C and schedule IV in the US.[1] TS
Pentazocine, sold under the brand name Talwin among others, is an opioid analgesic medication used to treat moderate to severe pain. Pentazocine activates (agonizes) κ-opioid receptors (KOR) and μ-opioid receptors (MOR). It shares many of the side effects of other opioids like constipation, nausea, itching, drowsiness, and respiratory depression, but, unlike most other opioids, it fairly frequently causes hallucinations, nightmares, and delusions. It is also, unlike most other opioids, subject to a ceiling effect, which is when at a certain dose no more pain relief is obtained by increasing the dose any further.[2] WP
Chemically it is classed as a benzomorphan and it comes in two enantiomers. WP
It was patented in 1960 and approved for medical use in 1964. Usually, in its oral formulations, it is combined with naloxone so as to prevent people from crushing the tablets, dissolving them in saline and injecting them for a high (as orally administered naloxone produces no opioid-negating effects as it has no oral bioavailability, whereas intravenous or intramuscular administration does).[2]
History
History
Pentazocine was developed by the Sterling Drug Company, Sterling-Winthrop Research Institute, of Rensselaer, New York. The analgesic compound was first made at Sterling in 1958. U.S. testing was conducted between 1961 and 1967. It was approved by the Food and Drug Administration in June 1967 after being favorably reviewed following testing on 12,000 patients in the United States. By mid 1967 Pentazocine was already being sold in Mexico, England, and Argentina, under different trade names.[4] WP
Legal status
United states
Pentazocine was originally unclassified under the Controlled Substances Act in the United States. A petition was filed with the US Drug Enforcement Administration (DEA) on October 1, 1971, to shift it to Schedule III. The petition was filed by Joseph L. Fink III, a pharmacist and law student at Georgetown University Law Center as part of the course Lawyering in the Public Interest. That petition was accepted for review on November 10, 1971. The DEA published a Final Rule transferring it to Schedule IV on January 10, 1979, with an effective date of February 9, 1979. Pentazocine is still classified in Schedule IV under the Controlled Substances Act in the United States, even with the addition of naloxone. Some states classify it in Schedule II, such as Illinois and South Carolina (injectable form only), or Schedule III such as Kentucky.) Internationally, pentazocine is a Schedule III drug under the Convention on Psychotropic Substances, except in Canada where it is Schedule I under the federal Controlled Drugs and Substances Act. Pentazocine has a DEA ACSCN of 9720; being a Schedule IV substance, the DEA does not assign an annual manufacturing quota for pentazocine for the United States.[5–10] WP
Brand names
Pentazocine is sold under several brand names, such as Fortral, Sosegon, Talwin NX (with naloxone), Talwin, Talwin PX, Fortwin, and Talacen (with paracetamol). WP
Pharmacology
Pharmacology
Pentazocine has weak binding affinity for the μ-opioid receptor in humans at 117.8 nM (Morphine 1.168).[11] WP
Chemistry
User reports
Erowid erowid.org
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ListingsPop culture
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References
- Other information for dose duration onset warning and summary - Book - 2015 Jones and Bartlett Nurse's drug handbook fourteenth edition - page 929
- Other Martindale: The Complete Drug Reference. 9 January 2017
- Other Fischer J, Ganellin CR. Analogue-based Drug Discovery. 2006
- Other Pain-Killing Drug Approved By F.D.A., New York Times, June 27, 1967, pg. 41
- Other 36 Fed.Reg. 217. November 1971
- Other 44 Fed. Reg. 2169. 1979
- Other Illinois Controlled Substances Act
- Other South Carolina DHEC Controlled Substance Schedule
- Other Kentucky Scheduled Drug List
- Other List of psychotropic substances under international control. 2016
- Other Simon BT, Lizarraga I. Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones. 11 September 2024
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), TripSit factsheets, PubChem (public domain). Each value links to the exact revision it came from.