Propiram
Encyclopedia
Propiram is a partial mu opioid
receptor agonist and weak mu antagonist analgesic
from the ampromide family of drugs. It was invented in 1963 in the United Kingdom by Bayer but was not widely marketed, although it saw some limited clinical use, especially in dentistry. A report in the reference Drug Facts & Comparisons, 56th (2002) Edition reports that research about the drug has increased in the past few years, having reached the (albeit restricted) Stage III clinical trial process in the United States and Canada. Propiram is currently a Schedule I/Narcotic controlled substance in the United States. It has been almost exclusively used as the fumarate salt, which has a free base conversion ratio of 0.70.
Propiram exhibits weak opioid antagonist activity on the mu receptor -- quite a bit weaker than its agonist effects -- and the effect on kappa and delta opioid, sigma receptors, or the NMDA
system are not well understood. Other drugs of the partial mu-opioid agonist/antagonist type include meptazinol
, buprenorphine
, butorphanol
, phenazocine
, nalbuphine
, pentazocine
, dezocine
and its relatives.
With about 10 per cent of the analgesic potency of morphine
with 50 mg being equivalent to more than 60 mg of codeine or 50 mg of pentazocine in many patients, propiram is an effective analgesic comparable to other drugs such as these as well as pethidine
, with a normal dose of around 50-100mg and a duration of action of 3 to 6 hours. It is more potent and effective than codeine, and longer lasting and with a faster onset of action compared to pethidine. Side effects include sedation
, dizziness
, nausea
and vomiting
. Propiram has been available in oral, rectal, and injectable formulations, with bioavailability above 97 per cent after oral administration. Many related compounds are known, although only propiram was ever commercialised.
Opioid
An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
receptor agonist and weak mu antagonist analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
from the ampromide family of drugs. It was invented in 1963 in the United Kingdom by Bayer but was not widely marketed, although it saw some limited clinical use, especially in dentistry. A report in the reference Drug Facts & Comparisons, 56th (2002) Edition reports that research about the drug has increased in the past few years, having reached the (albeit restricted) Stage III clinical trial process in the United States and Canada. Propiram is currently a Schedule I/Narcotic controlled substance in the United States. It has been almost exclusively used as the fumarate salt, which has a free base conversion ratio of 0.70.
Propiram exhibits weak opioid antagonist activity on the mu receptor -- quite a bit weaker than its agonist effects -- and the effect on kappa and delta opioid, sigma receptors, or the NMDA
NMDA
N-Methyl-D-aspartic acid or N-Methyl-D-aspartate is an amino acid derivative which acts as a specific agonist at the NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor...
system are not well understood. Other drugs of the partial mu-opioid agonist/antagonist type include meptazinol
Meptazinol
Meptazinol is an opioid analgesic for use with moderate to severe pain, most commonly used to treat pain in obstetrics . A partial µ-opioid receptor agonist, its mixed agonist/antagonist activity affords it a lower risk of dependence and abuse than full µ agonists like morphine...
, buprenorphine
Buprenorphine
Buprenorphine is a semi-synthetic opioid that is used...
, butorphanol
Butorphanol
Butorphanol is a morphinan-type synthetic opioid analgesic developed by Bristol-Myers. Brand name Stadol was recently discontinued by the manufacturer. It is now only available in its generic formulations, manufactured by Novex, Mylan, Apotex and Ben Venue Laboratories. Butorphanol is most...
, phenazocine
Phenazocine
Phenazocine is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects....
, nalbuphine
Nalbuphine
Nalbuphine is a semi-synthetic opioid used commercially as an analgesic under a variety of trade names, including Nubain. It is noteworthy in part for the fact that at low dosages, it is found much more effective by women than by men, and may even increase pain in men, leading to its...
, pentazocine
Pentazocine
Pentazocine is a synthetically prepared prototypical mixed agonist-antagonist narcotic drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain...
, dezocine
Dezocine
Dezocine was developed by American Home Products and is an opioid analgesic related to pentazocine, with a similar profile of effects that include analgesic action and euphoria at low doses, but produces dysphoria and hallucinations at high doses, most likely due to action at κ-opioid...
and its relatives.
With about 10 per cent of the analgesic potency of morphine
Morphine
Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...
with 50 mg being equivalent to more than 60 mg of codeine or 50 mg of pentazocine in many patients, propiram is an effective analgesic comparable to other drugs such as these as well as pethidine
Pethidine
Pethidine or meperidine Pethidine (INN) or meperidine (USAN) Pethidine (INN) or meperidine (USAN) (commonly referred to as Demerol but also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil; Alodan; Centralgin; Dispadol; Dolantin; Mialgin (in Indonesia); Petidin Dolargan (in Poland);...
, with a normal dose of around 50-100mg and a duration of action of 3 to 6 hours. It is more potent and effective than codeine, and longer lasting and with a faster onset of action compared to pethidine. Side effects include sedation
Sedation
Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure...
, dizziness
Dizziness
Dizziness refers to an impairment in spatial perception and stability. The term is somewhat imprecise. It can be used to mean vertigo, presyncope, disequilibrium, or a non-specific feeling such as giddiness or foolishness....
, nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
and vomiting
Vomiting
Vomiting is the forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose...
. Propiram has been available in oral, rectal, and injectable formulations, with bioavailability above 97 per cent after oral administration. Many related compounds are known, although only propiram was ever commercialised.