Not in clinical use in the United States

Piritramide is a synthetic opioid that has been used for more than 30 years in parts of Europe as the analgesic of choice for the management of postoperative pain.

• Piritramide was discovered at Janssen Pharmaceutica in 1960 and is currently manufactured and distributed within continental Europe and some other places by Janssen-Cilag. Piritramide is not available in all countries. It is marketed under the brand name Dipidolor in Germany, Lithuania, Slovenia, Austria.
• Piritramide is most commonly prescribed IM or IV for postoperative analgesia.
• It is used successfully for patient-controlled analgesia in adults 14 and more recently in children.
• Piritramide has potency 0.65 to 0.75 times that of morphine.
• Upon administration, piritramide binds to and activates mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opioids and producing analgesic relief.
• The most common side effect of piritramide appears to be a dose-related incidence of sedation. It is reported in many studies, but rarely accurately quantified.

  Diaphoresis, urinary retention, flushing, focal myopathy and thrombophlebitis have all been reported.

• Piritramide is a strong opioid and therefore is regulated much the same as morphine in all known jurisdictions.
• It was never introduced in the United States and is therefore a Schedule I/Narcotic controlled substance.

Piritramide:
https://drugs.ncats.io/drug/4RP92LYZ2F

Definition:
A diphenylpropylamine and opioid receptor agonist, with analgesic activity. Upon administration, piritramide binds to and activates mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opioids and producing analgesic relief.

Piritramide:
https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C119750

Piritramide is a synthetic opioid analgesic with a potency 0.65 to 0.75 times that of morphine.

Piritramide is commonly used for the treatment of postoperative pain.

• Piritramide is a strong opioid and therefore is regulated much the same as morphine in all known jurisdictions. It is listed under international treaties and other laws such as the German Betabungsmittelgesetz, the Austrian Suchtgiftmittelgesetz, the Opium Laws of various other European countries, Canadian controlled substances act, UK Misuse of Drugs Act of 1971, and equivalents elsewhere.
• Piritramide is also known as pirinitramide.

  Its closest chemical relatives amongst well-known drugs are diphenoxylate (Lomotil) and bezitramide (Burgodin).

• Piritramide is available in tablets and ampoules of sterile solution for injection by all routes, and is used in Patient Controlled Analgesia units.
• A common starting dose is 15 mg IV, equivalent to 10 mg of morphine hydrochloride.
• Piritramide is most often used in post-operative situations and emergency departments
• Some of its properties would seem to lend it well to chronic pain control as well.
• It is one of the longer-lasting opioids and has a plasma half-life of 3 to 12 hours.
• Belongs to the class of organic compounds known as diphenylacetonitriles.

Piritramide tends to cause less respiratory depression than morphine and can take a while to have full effect especially if taken by mouth.

Metabocard for Piritramide:
https://hmdb.ca/metabolites/HMDB0041990

Breastfeeding:

Summary of Use During Lactation:
Piritramide is not approved for marketing in the United States by the U.S. Food and Drug Administration, but is available in other countries. Limited data indicate that the amounts of piritamide in colostrum is very low after use of intravenous piritamide by patient-controlled analgesia.

In general, maternal use of oral narcotics during breastfeeding can cause infant drowsiness, central nervous system depression and even death.

Newborn infants seem to be particularly sensitive to the effects of even small dosages of narcotic analgesics. Once the mother's milk comes in, it is best to provide pain control with a nonnarcotic analgesic and limit maternal intake of meperidine to a few days at a low dosage with close infant monitoring.

If the baby shows signs of increased sleepiness (more than usual), difficulty breastfeeding, breathing difficulties, or limpness, a physician should be contacted immediately.

Piritramide Drug Levels and Effects:
https://www.ncbi.nlm.nih.gov/books/NBK500902/

Synonyms:

• Piritramide
• Dipidolor
• ipiritramide
• Pirdolan
• Piridolan
• irinitramide

Piritramide:
https://drugcentral.org/drugcard/3478

Opioid Pain Killer:
It belongs to a group of medicines called opioid analgesics (strong painkillers). Piritramide [MAH] is used to relieve severe and strongest pain

Piritramide [MAH] 7.5 mg/ml solution for injection Leaflet (PDF 6 pages):
https://mri.cts-mrp.eu/human/downloads/DE_H_2753_001_FinalPL.pdf

Piritramide stability in solutions and mixtures (PDF 2 pages):
https://www.stabilis.org/Monographie.pdf.php?Molecule=Piritramide

Onset:
Peak Response: Pain, intramuscular: 10 to 60 minutes.

• One investigator observed maximal analgesia at 1 to 2 hours with the same doses (10 to 20 mg)

Duration:
Single Dose: Pain, intramuscular: 6 hours.

• A shorter duration (4 hours) has also been reported

Piritramide:
http://www.jodrugs.com/products/39905-piritramide.aspx

Piritramide:
https://www.reddit.com/r/ObscureDrugs/comments/hhda3z/piritramide/

Abstract:
Background: Piritramide is a synthetic opioid used for postoperative analgesia in several European countries. The authors present a mixed-effects model of its population pharmacokinetics in patients undergoing surgery.

Population pharmacokinetics of piritramide in surgical patients:
https://www.opioids.com/piritramide/index.html

Abstract:
I.V. patient-controlled analgesia (PCA) has become a well recognized and widely accepted technique for providing postoperative pain relief. Indeed, in numerous studies itwas shown clearly that PCA allows optimum individual titration of analgesia and enhances patient satisfaction with postoperative pain management. However, sedation and nausea are still the most frequent side effects during PCA with opioids. Theoretically, reducing the opioid dose could reduce side effects, but may also lead to insufficient pain relief. There is cumulating evidence that the efficacy ofPCA is at least partly related to non-pharmacological and psychological factors such as coping, anxiety, emotional distress and self-control. We hypothesized that a PCA regimen with a small bolus dose and a short lockout time would enable the patient to titrate analgesic effect more effectively against side effects.Therefore, we have examined, in a prospective, randomized,double-blind study, the relative efficacy, patient satisfaction and side effects of i.v. PCA with a low (0.75 mg) bolus dose of piritramide compared with our routinely prescribedbolus dose (1.5 mg)

(1999) Influence of bolus size on efficacy of postoperative patient-controlled analgesia with Piritramide (PDF 4 pages):
https://core.ac.uk/download/pdf/34476986.pdf

Not in clinical use in the United States

• A synthetic opioid analgesic (narcotic painkiller)
• Developed and patented in Belgium, at Janssen, in 1960
• Marketed in certain European countries including: Austria, Belgium, Czech Republic, Germany and the Netherlands.
• It comes in free form
• About 3/4 as potent as morphine
• Given parenterally (by injection) for the treatment of severe pain.
• Nausea, vomiting, respiratory depression and constipation are believed to be less frequent with piritramide than with morphine
• It produces more rapid-onset analgesia (pain relief) when compared to morphine and pethidine.
• Onset of effects is as little as 1 - 2 minutes (intravenous)