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OPIOIDS.pptx
- 1.
- 2. OPIOIDS drugs with depressantaction on the CNS, which cause: • analgesia • calming anxiety • sedation • euphoria
- 3. OPIOIDS • Opioids arenatural or synthetic compounds that produce morphine-like effects. • The term “opiate” is reserved for drugs, such as morphine and codeine, obtained from the juice of the opium poppy. • All drugs in this category act by binding to specific opioid receptors in the CNS to produce effects that mimic the action of endogenous peptide neurotransmitters (for example, endorphins, enkephalins, and dynorphins). • Although the opioids have a broad range of effects, their primary use is to relieve intense pain, whether that pain is from surgery or a result of injury or disease such as cancer
- 4. Types of opioids •endogenous opioids • exogenous opioids - extracted from opium or produced by synthesis
- 6. ENDOGENOUS OPIOIDS Role =neuromodulators • enkephalin • B- endorphin • dynorphins • NOCICEPTIN
- 7. ENDOGENOUS OPIOIDS Role =neuromodulators • Distribution: - central - CNS - peripheral – intestine 1. ENKEPHALINE = pentapeptide: It acts on miu and delta receptors ENDORPHINE = polypeptide Precursors = pro-opiomelanocortin (POMC) POMC => endorphins, ACTH It acts on miu and delta receptors
- 8. ENDOGENOUS OPIOIDS 3. DINORFINE= polypeptides • Acts on Kappa receptors 4. NOCICEPTINS = polypeptides • They have an ALGEZIC effect
- 9. Types of opioidreceptors
- 10. The mechanism ofaction of opioid receptors • Opioid receptors • Gi protein-coupled receptors 1. inhibits adenyl cyclase => decreases the intracellular concentration of cAMP 2. open K + => hyperpolarization 3. close Ca2 channels + voltage dependent => prevent the release of mediators
- 11. µ (miu) κ (kappa) δ (delta) Supraspinal analgesia Sedation /Euphoria miosis Respiratory depression Addiction Constipation Hypothermia Spinal analgesia Sedation / Dysphoria miosis Favors the action of µ and κ
- 12. Classification of opioids 1.Agonists (encephalomimetics) 2. Agonists k - antagonists µ 3. Antagonists
- 13. OPIOUS AGONISTS STRONG AGONISTS •Alfentanil ALFENTA • Fentanyl ACTIQ, DURAGESIC, FENTORA • Heroin • Hydrocodone various • Hydromorphone DILAUDID • Meperidine DEMEROL • Methadone DOLOPHINE • Morphine ROXANOL, CONTIN, ORAMORPH, • KADIAN, AVINZA • Oxycodone OXYCONTIN • Oxymorphone OPANA • Remifentanil ULTIVA • Sufentanil SUFENTA • Tapentadol NUCYNTA MODERATE/LOW AGONISTS • Codeine MIXED AGONIST-ANTAGONISTS AND PARTIAL AGONISTS • Buprenorphine BUPRENEX, SUBUTEX • Butorphanol STADOL • Nalbuphine NUBAIN • Pentazocine TALWIN
- 14. Morphine PHARMACOLOGICAL EFFECTS • CNSeffects • Digestive effects • Genitourinary effects • Cardiovascular effects • Lung effects • Effects on the eye • Effects on thermoregulation • Neurohormonal effects • Tolerance and dependence
- 15. Morphine 1. Effects onthe CNS a. Intense analgesia • increases the threshold of painful perception • decreases reactions to pain: screaming, fear • changes the perception of pain - detachment from pain • - duration of analgesia = 4 - 6 hours • - place of action: central, bone marrow, peripheral (can be administered for example in a joint and causes local analgesia) b. Respiratory depression • - is installed in parallel with analgesia • - occurs by decreasing the sensitivity of the respiratory centers to CO2 c. Depression of the cough center d. Behavioral change • - euphoria, sedation, well-being e. Vomiting - causes vomiting at low doses
- 16. Morphine 2. Digestive effects •1. decreases digestive peristalsis • 2. decreases digestive secretions →→constipation →antidiarrheal effect 3. spasm of the bile ducts and sphincter of Odi => in colic is associated with antispasmodics
- 17. Morphine 3. Effects atthe genitourinary level • - increases the contraction of the ureters => in renal colic is associated with antispasmodics • - increases the tonus of the bladder detrusor • - increases the tonus of sphincter of the bladder →difficult urination
- 18. Morphine 4. Cardiovascular effects a.vasodilation -arterial and venous => indication in acute pulmonary edema -cerebral vessels => increases CSF pressure => contraindicated in brain trauma - cutaneous => congestion, sweating b. depress circulatory => orthostatic hypotension
- 19. Morphine 5. Effects onthe lungs • - bronchospasm - by the release of histamine 6. Eye effects – miosis 7. Effects on thermoregulation – depression 8. Neurohormonal effects - decreases the secretion of ACTH, FSH, LH - increases the secretion of prolactin. 9. Tolerance and dependence
- 20. Indications 1. Analgesia -when thereis no response to other painkillers - in cancer pre and postoperative 2. Acute pulmonary edema 3. Colic - associated with antispasmodics 4. Diarrhea - loperamide IS better 5.Cough - better codeine or dextromethorphan
- 21. Contraindications and sideeffects • addiction => contraindicated abusive administration • respiratory depression => contraindicated in patients with respiratory failure • Sedation • vomiting • hypotension • increase in intracranial pressure => contraindicated in head trauma • constipation • urinary retention => contraindicated in patients with prostate adenoma • contraindicated in labor in administration iv => newborn asphyxia • contraindicated in allergies - because it causes the release of histamine
- 22. Heroin • - isa synthetic opiate produced by acetylation of morphine • - it is more fat soluble than morphine => it crosses the blood-brain barrier better => it transforms into morphine • - has a potency 2-3x higher than morphine (10 mg morphine = 5 mg herion) • - duration of action approx. 2 hours (½ of morphine duration of action) • - is not used in therapy • - used by drug addicts
- 23. Meperidine( Mialgin) • -synthetic opioid (first) Pharmacological effects : • analgesia 10 times lower than morphine (10 mg morphine = 100 mg meperidine) • shorter duration of action - 2-4 hours • sedation / euphoria - more pronounced than morphine • respiratory depression - less than or equal to morphine • mydriasis not miosis like morphine • - atropine-like effect Indications • - Just like morphine • - not for coughs and diarrhea
- 24. Methadone • - syntheticopioid with oral administration Pharmacological effects • Analgesia similar to morphine after parenteral administration, but much higher after oral administration because it is better absorbed • long duration of action (3 - 5 HOURS) Indications : 1. detoxification cure - as a substitute for morphine because it causes in abstinence syndrome slower onset and milder than morphine due to long T / 2 (35 hours vs. 2-3 hours morphine) 2. analgesic - orally - in chronic pain - 5-15 mg - sc. - 5-10mg
- 25. . Fentanyl • -acts predominantly on miu receptors Pharmacological effects: Analgesia 100 times higher than morphine immediate action after adm. iv and short - ½ hour Parasympathomimetic effects => bradycardia Indications - dissociative anesthesia together with droperidol - treatment of neoplastic pain - transdermal devices (72 hours)
- 26. MIXED AGONIST- ANTAGONISTS AND PARTIALAGONISTS Buprenorphine Butorphanol Nalbuphine Pentazocine
- 27. Pentazocine • an agoniston κ receptors and is a weak antagonist at µ and δ receptors. Pharmacological effects: • analgesic action lower than morphine • low risk of addiction (may cause withdrawal syndrome in morphine addicts) • depresses the breath less than morphine • sedative • ATTENTION: at high doses - dysphoria, hallucinations (by kappa stimulation) Indications - acute and chronic pain
- 28. OPIOUS ANTAGONISTS Naloxone Use: • Acuteopioid poisoning • Respiratory depression caused by opioids Naltrexone Indications : Treatment of drug addicts after detoxification