opioid analgesic

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OPIOID ANALGESIC

Opioids natural or synthetic; produce morphine-like effects. They act by binding to specific opioid receptors in the CNS effects mimic the action of endogenous peptide neurotransmitters (e.g., leu- and met-enkephalins). They relieve severe pain - essential in treatment of major diseases, trauma, and surgery. Danger of the drug abuse. Although the opioids have a broad range of effects, their primary use is to relieve intense pain and the anxiety that accompanies it.Antagonists they can reverse actions of opioids, important clinically treatment of overdose. OPIOIDS (MORPHINE-LIKE) ANALGESICS AND ANTAGONISTS

History of OpioidsOpium is extracted from poppy seeds (Paper somniforum)Used for thousands of years to produce:EuphoriaAnalgesiaSedationRelief from diarrheaCough suppression

Terminologyopium is a Greek word meaning juice, or the exudate from the poppyopiate is a drug extracted from the exudate of the poppyopioid is a natural or synthetic drug that binds to opioid receptors producing agonist effects

Mechanism of ActionAction of endogenous and exogenous opioids at opioid receptors

Opioid ReceptorsMu and Kappa Receptor ActivationResponseMu-1Mu-2KappaAnalgesiaRespiratory DepressionEuphoriaDysphoriaDecrease GI motilityPhysical DependenceEffects of opioids

Opiods: dose-response relationship

comparison of the maximum efficacy and addiction/abuse liability of commonly used narcotic analgesics

MorphineThe opioids are classified in several ways:Therapeutic uses morphineDivision (in relation to the activity)

1. Strong agonists (e.g. morphine, meperidine=pethidine, methadone, fentanyl, sufentanil, alfentanil, remifentanil)2. Moderate agonists (e.g. propoxyphene, codein, oxycodone)3. Mixed agonist-antagonists (e.g. pentazocine, buprenorphine, nalbuphine, butorphanol)4. Other analgesics ( tramadol) 5. Antagonists (naloxone, naltrexone)

OPIOID ANALGESICS AND ANTAGONISTSSTRONG AGONISTSMODERATE/LOW AGONISTSMIXED AGONIST-ANTAGONISTS AND PARTIAL AGONISTSANTAGONISTSOTHER ANALGESICSAlfentanilFentanylMeperidineMethadone HeroinMorphineRemifentanilSufentanilCodeineOxycodonePropoxypheneBuprenorphineButorphanolNalbuphinePentazocineNaloxoneNaltrexoneTramadol(according to Lippincotts Pharmacology, 2006MorphineCNS effectsRespiratory depression and suppression of cough: reducing the responsiveness of the respiratory centers in the brain stem to blood levels of carbon dioxide and inhibiting directly the respiratory center. MorphineCNS effectsNausea and vomiting: stimulating the chemoreceptor trigger zone. In most cases, after therapeutic dose, subsequent doses of morphine do not produce vomiting. Miosis: pinpoint pupils are indicative of toxic dosage prior to asphyxia. It can be block with atropine.Morphine Cardiovascular effects:Orthostatic hypotention can occur due to vasomotor medullary depression and histamine release.Gastrointestinal effect:Reduces gastrointestinal motility, causing constipationDecreases biliary and pancreatic secretions.Constriction at the spincter of Oddi causes an increase in biliary pressure.Morphine Other systemic effects:Increases detrusor muscle tone in the urinary bladder, producing a feeling of urinary. Vesical sphincter tone is also increased, making voidingInhibits the cellular immunity and humoral immunity, which is significant in withdrawal syndrome and tolerant in chronic administration.Farmakokinetik Opioid

Adverse effectsContraindications and cautionsInteraksi ObatObat yang bekerja secara sentral seperti barbiturat, fenotiazin, penghambat MAO, antidepresan trisiklikefek sedatif dan depresi pernafasanFenotiazinefek menurunkan tek.darahAmphetamineanalgesia dari morphin dan mengurangi efek sedasi dan depresi pernafasanKeracunan Akut MorfinGejala : coma, miosis, eksterm dari pernafasan (hingga 2-4 tarikan nafas permenit), sianosis, suhu tubuh rendah, kehilangan tonus otot rangka. Tindakan : Pembebasan jalan nafas dan pemberian O2memberikan suatu antagonis morfin untuk menghilangkan kelumpuhan pernafasan (naloxone sbg antagonis kompetitif)Shock ditangani, mungkin perlu pemberian Ab untuk pencegahan pneumoniaMethadoneFentanylMeperidinePharmacokinetics: Meperidine is well absorbed from the gastrointestinal tract, and is useful when an orally administered However, meperidine is most often administered parenterallyThe drug has a duration of action of 2 to 4 hours, which is shorter than that of morphine Adverse effects: Large or repetitive doses of meperidine can cause anxiety, tremors, muscle twitches, and rarely, convulsions due to the accumulation of a toxic metabolite, normeperidine. Time to peak effect and duration of action of several opioids administered intravenously

CodeinePethidineTramadola centrally acting analgesic that binds to the -opioid receptor it weakly inhibits reuptake of norepinephrine and serotonin It is used to manage moderate to moderately severe painIts respiratory-depressant activity is less than that of morphineAdverse effects commonly observed in individuals treated with opioids

Opiate Withdrawal syndrome

Opioid AntagonistsOpioid AntagonistsClinical Use of Analgesic DrugsClinical Use of Analgesic DrugsClinical Use of Analgesic Drugs42

ALHAMDULILLAH.