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Encyclopedia > Pethidine
Pethidine
Systematic (IUPAC) name
Ethyl-1-methyl-4-phenylpiperidine-4-carboxylate
Identifiers
CAS number 57-42-1
ATC code N02AB02
PubChem 4058
DrugBank APRD00074
Chemical data
Formula C15H21NO2 
Mol. mass 247.33
Pharmacokinetic data
Bioavailability variable
Protein binding 65-75%
Metabolism Liver
Half life 3-5 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C(AU) C(US) Image File history File links Circle-question-red. ... Image File history File links Size of this preview: 747 × 600 pixel Image in higher resolution (1100 × 883 pixel, file size: 20 KB, MIME type: image/png) File links The following pages on the English Wikipedia link to this file (pages on other projects are not listed): Pethidine ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... This article does not cite its references or sources. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, Symbol, Number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated MM) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... seadonkey rules =P ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ present in vertebrates and some other animals. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... Kidneys viewed from behind with spine removed The kidneys are bean-shaped excretory organs in vertebrates. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... Anthem Advance Australia Fair Royal anthem: God Save the Queen Capital Canberra Largest city Sydney Official languages English (de facto 1) Government Federal constitutional monarchy and parliamentary democracy  -  Queen Elizabeth II  -  Governor-General Michael Jeffery  -  Prime Minister John Howard Independence from the United Kingdom   -  Constitution 1 January 1901   -  Statute of... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from...

Legal status

Controlled (S8)(AU) Class A(UK) Schedule II(US) The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... The Standard for the Uniform Scheduling of Drugs and Poisons, abbreviated SUSDP, is a document used in the regulation of drugs and poisons in Australia. ... Anthem Advance Australia Fair Royal anthem: God Save the Queen Capital Canberra Largest city Sydney Official languages English (de facto 1) Government Federal constitutional monarchy and parliamentary democracy  -  Queen Elizabeth II  -  Governor-General Michael Jeffery  -  Prime Minister John Howard Independence from the United Kingdom   -  Constitution 1 January 1901   -  Statute of... The Misuse of Drugs Act 1971 is an Act of Parliament, by which the United Kingdom aims to control the possession and supply of numerous drugs and drug-like substances, as listed under the Act, and to enable international co-operation against illegal drug trafficking. ... The Controlled Substances Act (CSA) was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970. ... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from...

Routes oral, IV, IM

Pethidine (INN) or meperidine (USAN) (also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil®; Alodan®; Centralgin®; Demerol®; Dispadol®; Dolantin®; Dolargan® (in Poland);[1] Dolestine®; Dolosal®; Dolsin®; Mefedina®) is a fast-acting opioid analgesic drug. In the United States, it is more commonly known as meperidine or by its brand name Demerol.[2] In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... Intramuscular injection is an injection of a substance directly into a muscle. ... An International Nonproprietary Name (INN) is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization. ... There have been a number of attempts to coin an alternative to American as an adjective (a demonym) for United States nationals. ... An opioid is a chemical substance that has a morphine-like action in the body. ... This article or section does not adequately cite its references or sources. ...


Pethidine is indicated for the treatment of moderate to severe pain, and is delivered as its hydrochloride salt in tablets, as a syrup, or by intramuscular or intravenous injection. For much of the 20th century, pethidine was the opioid of choice for many physicians; in 1983 60% of doctors prescribed it for acute pain and 22% for chronic severe pain.[3] Compared to morphine, pethidine was supposed to be safer and carry less risk of addiction, and to be superior in treating the pain associated with biliary spasm or renal colic due to its putative antispasmodic effects. In fact, pethidine is no more effective than morphine at treating biliary or renal pain, and its low potency, short duration of action, and unique toxicity (i.e. seizures, delirium, other neuropsychological effects) relative to other available opioid analgesics have seen it fall out of favor in recent years, for all but a very few, very specific indications.[4] Several countries, including Australia, have put severe limits on its use or curtailed it outright.[5] Nevertheless, some physicians continue to use it as a first-line strong opioid. Hurting redirects here. ... In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (mostly amines). ... Intramuscular injection is an injection of a substance directly into a muscle. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... This article or section does not adequately cite its references or sources. ... Renal colic is a type of pain commonly caused by kidney stones. ...

Contents

Pharmacodynamics/Mechanism of Action

Main article: Opioid

Pethidine's efficacy as an analgesic was discovered fortuitously; it was synthesized in 1939 as an antimuscarinic agent.[6] Pethidine exerts its analgesic effects by the same mechanism as morphine, by acting as an agonist at the μ-opioid receptor. In addition to its strong opiodergic and anticholinergic effects, it has local anesthetic activity related to its interactions with sodium ion channels. Pethidine's apparent in vitro efficacy as an "antispasmodic" is due to its local anesthetic effects. It does not, contrary to popular belief, have antispasmodic effects in vivo.[7] Pethidine also has stimulant effects mediated by its inhibition of the dopamine transporter (DAT) and norepinephrine transporter (NAT). Because of its DAT inhibitory action, pethidine will substitute for cocaine in animals trained to discriminate cocaine from saline.[8] Several analogues of pethidine have been synthesized that are potent inhibitors of the reuptake of the monoamine neurotransmitters dopamine and norepinephrine via DAT and NAT.[9][10] It has also been associated with cases of serotonin syndrome, suggesting some interaction with serotonergic neurons, but the relationship has not been definitively demonstrated.[5][6][8][10] It is more lipid-soluble than morphine, resulting in a faster onset of action. Its duration of clinical effect is 120-150 minutes. Despite producing analgesia for 2-3 hours at most, pethidine is typically administered at 4-6 hour intervals, so that the patient spends at least an hour (and up to four hours) between doses without any analgesia, resulting in much unnecessary pain and suffering. In addition, pethidine has been shown to be less effective than morphine or hydromorphone at easing severe pain, or pain associated with movement or coughing.[6][8][10] Like other opioid drugs, pethidine has the potential to cause physical dependence or addiction. In fact, pethidine may be more addictive than other opioids because of its exceptionally rapid onset of action and associated "rush", and additional activity as a monoamine transporter inhibitor, which results in cocaine-like stimulant effects in addition to its typical opioid effects.[11] When compared with morphine, hydromorphone, and placebo, pethidine was consistently associated with more euphoria, difficulty concentrating, confusion, and impaired psychomotor and cognitive performance when administered to healthy volunteers.[12] The especially severe side effects unique to pethidine among opioids — serotonin syndrome, seizures, delirium, dysphoria, tremor — are primarily or entirely due to the action of its metabolite, norpethidine.[6][10] An opioid is a chemical substance that has a morphine-like action in the body. ... An anticholinergic agent is a member of a class of pharmaceutical compounds which serve to reduce the effects mediated by acetylcholine in the central nervous system and peripheral nervous system. ... This article does not adequately cite its references or sources. ... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... To meet Wikipedias quality standards, this article may require cleanup. ... A local anesthetic is a drug that reversibly inhibits the propagation of signals along nerves. ... Sodium channels (also known as voltage-gated sodium channels) are integral membrane proteins that are localized in and conduct sodium ions (Na+) through a cells plasma membrane. ... Wiktionary has a definition of: In vitro In vitro (Latin: within glass) means within a test tube, or, more generally, outside a living organism or cell. ... An antispasmodic is a drug that suppresses smooth muscle contraction, especially in tubular organs. ... In vivo (Latin for (with)in the living). ... Dopamine is a phenethylamine naturally produced by the human body. ... The dopamine transporter or DAT is a monoamine transporter that is specific for clearing the neurotransmitter dopamine out of the synaptic cleft and into a glial cell or the presynaptic neuron. ... Norepinephrine (INN) or noradrenaline (BAN) is a catecholamine and a phenethylamine with chemical formula C8H11NO3. ... The norepinephrine transporter or NET is a monoamine transporter that transports the neurotransmitter norepinephrine from the synapse back to its vesicles for storage until later use. ... Monoamine neurotransmitters are neurotransmitters and neuromodulators that contain one amino group that is connected to an aromatic ring by a two-carbon chain (-CH2-CH2-). All monoamines are derived from aromatic amino acids like phenylalanine, tyrosine, histidine, tryptophan, and the thyroid hormones by the action of aromatic amino acid decarboxylase... Norepinephrine (INN) or noradrenaline (BAN) is a catecholamine and a phenethylamine with chemical formula C8H11NO3. ... Serotonin syndrome is a rare, but potentially life-threatening adverse drug reaction that results from intentional self-poisoning, therapeutic drug use, or inadvertent interactions between drugs. ... Serotonin (5-hydroxytryptamine, or 5-HT) is a monoamine neurotransmitter synthesized in serotonergic neurons in the central nervous system (CNS) and enterochromaffin cells in the gastrointestinal tract of animals including humans. ... Hydromorphone is a drug developed in Germany in the 1920s and introduced to the mass market beginning in 1926. ... Physical dependence describes increased tolerance of a drug combined with a physical need of the drug to function. ... Addiction is a chronic or recurrent condition proposed to be precipitated by one or more of the following: genetic, biological/pharmacological and social factors. ...


Pharmacokinetics

Pethidine is quickly hydrolysed in the liver to pethidinic acid and is also demethylated to norpethidine, which has half the analgesic activity of pethidine but a longer elimination half-life (8-12 hours[13]); accumulating with regular administration, or in renal failure. Norpethidine is toxic and has convulsant and hallucinogenic effects. The toxic effects mediated by the metabolites cannot be countered with opioid receptor antagonists such as naloxone or naltrexone and are probably primarily due to norpethidine's anticholinergic activity; its pharmacology has not been thoroughly explored. The neurotoxicity of pethidine's metabolites is a unique feature of pethidine compared to other opioids. Pethidine's metabolites are further conjugated with glucuronic acid and excreted into the urine. Image File history File links No higher resolution available. ... Antagonists In medicine and biology, a receptor antagonist is a ligand that inhibits the function of an agonist and inverse agonist for a specific receptor. ... Naloxone is a drug used to counter the effects of opioid overdose, for example heroin and morphine overdose. ... Naltrexone is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. ... An anticholinergic agent is a member of a class of pharmaceutical compounds which serve to reduce the effects mediated by acetylcholine in the central nervous system and peripheral nervous system. ... The α-D form of glucuronic acid. ...


Interactions

Pethidine has serious interactions that can be dangerous with MAOIs (e.g. furazolidone, isocarboxazid, linezolid, moclobemide, phenelzine, procarbazine, selegiline, tranylcypromine, naltrexone, ritonavir, and sibutramine). Such patients may suffer agitation, delirium, headache, convulsions, and/or hyperthermia. Fatal interactions have been reported. It is thought to be caused by an increase in cerebral serotonin concentrations. It is possible that Pethidine can also interact with a number of other medications, including muscle relaxants, some antidepressants, benzodiazepines, and alcohol. Monoamine oxidase inhibitors (MAOIs) are a class of antidepressant drugs prescribed for the treatment of depression. ... This article or section does not cite its references or sources. ... A recent form of antidepressant medication - Prozac Serotonin-norepinephrine reuptake inhibitor, Venlafaxine An antidepressant, in the most common usage, is a medication taken to alleviate clinical depression or dysthymia (milder depression). ... Alprazolam 2mg tablets The benzodiazepines (pronounced , or benzos for short) are a class of psychoactive drugs considered as minor tranquilizers with varying hypnotic, sedative, anxiolytic, anticonvulsant, muscle relaxant and amnesic properties, which are brought on by slowing down the central nervous system. ... Functional group of an alcohol molecule. ...


Pethidine is also relatively contraindicated for use when a patient is suffering from liver, or kidney disease, has a history of seizures or epilepsy, has an enlarged prostate or urinary retention problems, or suffers from hyperthyroidism, asthma, or Addison's disease. The liver is an organ present in vertebrates and some other animals. ... It has been suggested that Renal anomalies and Renal plasma threshold be merged into this article or section. ... The term disease refers to an abnormal condition of an organism that impairs function. ... The prostate is a compound tubuloalveolar exocrine gland of the male mammalian reproductive system. ... Hyperthyroidism (or overactive thyroid gland) is the clinical syndrome caused by an excess of circulating free thyroxine (T4) or free triiodothyronine (T3), or both. ... Addisons disease (also known as chronic adrenal insufficiency, or hypocortisolism) is a rare endocrine disorder which results in the body not producing sufficient amounts of certain adrenal hormones. ...


Adverse effects

Main article: Opioid An opioid is a chemical substance that has a morphine-like action in the body. ...


In addition to the adverse effects common to all opioids, such as constipation, dry mouth, lightheadedness, twitchiness, muscular twitches, and nausea, the repeated administration of pethidine can lead to neurotoxic effects. Adverse effect, in medicine, is an abnormal, harmful, undesired and/or unintended side-effect, although not necessarily unexpected, which is obtained as the result of a therapy or other medical intervention, such as drug/chemotherapy, physical therapy, surgery, medical procedure, use of a medical device, etc. ... Constipation or irregularity, is a condition of the digestive system where a person (or animal) experiences hard feces that are difficult to egest; it may be extremely painful, and in severe cases (fecal impaction) lead to symptoms of bowel obstruction. ... For the Beck song, see Nausea (song). ...


References

  1. ^ Lekopedia - Dolargan. jestemchory.pl. Retrieved on 2006-08-01.
  2. ^ Demerol RxList. Retrieved 19 Jun. 2006.
  3. ^ Kaiko, Robert F.; Kathleen M. Foley, Patricia Y. Grabinski, George Heidrich, Ada G. Rogers, Charles E. Inturrisi, Marcus M. Reidenberg (February 1983). "Central Nervous System Excitatory Effects of Meperidine in Cancer Patients". Annals of Neurology 13 (2): 180-185. ISSN: 0364-5134. 
  4. ^ Donna Wong (2002-03-15). Notes on Meperidine. Wong on Web Papers. Elsevier. Retrieved on 2007-04-13.
  5. ^ a b Davis, Sharon (August 2004). [www.clininfo.health.nsw.gov.au/nswtag/publications/posstats/Pethidinefinal.pdf Use of pethidine for pain management in the emergency department: a position statement of the NSW Therapeutic Advisory Group] (PDF). New South Wales Therapeutic Advisory Group. Retrieved on 2007-01-17.
  6. ^ a b c d Latta, Kenneth S.; Brian Ginsberg, Robert L. Barkin (January/February 2002). "Meperidine: A Critical Review". American Journal of Therapeutics 9 (1): 53-68. ISSN: 1075-2765. 
  7. ^ Wagner, Larry E., II; Michael Eaton, Salas S. Sabnis, Kevin J. Gingrich (November 1999). "Meperidine and Lidocaine Block of Recombinant Voltage-Dependent Na+ Channels: Evidence that Meperidine is a Local Anesthetic". Anesthesiology 91 (5): 1481-1490. ISSN: 0003-3022. 
  8. ^ a b c Izenwasser, Sari; Amy Hauck Newman, Brian M. Cox, Jonathan L. Katz (January/February 1996). "The cocaine-like behavioral effects of meperidine are mediated by activity at the dopamine transporter". European Journal of Pharmacology 297 (1-2): 9-17. DOI:10.1016/0014-2999(95)00696-6. ISSN: 0014-2999. 
  9. ^ Lomenzo, Stacey A.; Jill B. Rhoden, Sari Izzenwasser, Dean Wade, Theresa Kopajtic, Jonathan L. Katz, Mark L. Trudell (2005-03-05). "Synthesis and Biological Evaluation of Meperdine Analogs at Monoamine Transporters". Journal of Medicinal Chemistry 48 (5): 1336-1343. ISSN: 0022-2623. 
  10. ^ a b c d (June 2006) "Demerol: Is It the Best Analgesic?". Pennsylvania Patient Safety Reporting Service Patient Safety Advisory 3 (2). Retrieved on 2007-01-16. 
  11. ^ In Brief. NPS Radar. National Prescribing Service (December 2005). Retrieved on 2007-01-17.
  12. ^ Walker, Diana J.; James P. Zacny (June 1999). "Subjective, Psychomotor, and Physiological Effects of Cumulative Doses of Opioid µ Agonists in Healthy Volunteers". The Journal of Pharmacology and Experimental Therapeutics 289 (3): 1454-1464. 
  13. ^ Norpethedine half-life. 2002. Australian prescriber[1]

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External links

  • Links to external chemical sources

  Results from FactBites:
 
Pethidine - definition of Pethidine in Encyclopedia (372 words)
Because pethidine has the potential to be both physically and psychologically habituating, it is important that it be used in only the doses prescribed, and that withdrawal from the drug be supervised by a physician to ensure there are no adverse reactions.
Pethidine is quickly hydrolysed in the liver to pethidinic acid and also demethylated to norpethidine, which is more toxic than pethidine, due to its convulsant and hallucinogenic effects.
Pethidine is also contraindicated for use when a patient is suffering from gallbladder, liver, or kidney disease, has a history of seizures or epilepsy, has an enlarged prostate or urinary retention problems, or suffers from hyperthyroidism, asthma, or Addison's disease.
  More results at FactBites »

 
 

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