OTHER OPIOIDS
- RASHMI RITHUSHA.V
MBBS student
SRMMCH&RC
CODEINE
• Natural opioid, methyl-morphine
• Demethylation by CYP2D6 →Morphine
• Potency -1/10th of morphine -analgesic property,
• Potency -1/3rd of morphine -cough suppression
• Less efficacious and partial agonist at µ opioid receptor
• Oral route
• Uses: cough, diarrohea
• Side effect: constipation
• Abuse liability is low
PHOLCODINE &
ETHYLMORPHINE
• Have codeine like properties
• Used mainly as antitussives
• Less constipating
HEROIN
• Diacetylmorphine →6 mono-acetylmorphine
→morphine
• 3 times more potent than morphine
• More lipid soluble →enters brain easily
• Highly euphoriant on iv injection and addictive
• Used in illicit drug trafficking as its highly
potent
• Sedative, emetic and hypotensive actions –less
prominent
• Banned in most countries except UK
THIS IS WHAT HAPPENS
WHEN YOU TAKE HEROIN
PETHIDINE (MEPERIDINE)
• Synthesized as an Atropine substitute
• µ opioid receptor agonist
• Actions blocked by naloxone
• Metabolism – meperinidic acid and norpethidine
To compare with morphine on the following aspects:
1.Potency 5.Spasmogenic action
2.Efficacy 6.Tachycardia due to antimuscarinic action
3.Onset of action 7.Absorption
4.Cough 8.Atropinic side effects
Serotonin syndrome?
REMIFENTANIL
Faster acting congener of
fentanyl and used
exclusively in anaesthesia
METHADONE
• Synthetic opioid
• Full µ receptor agonist
• Actions similar to morphine
• High oral : parenteral activity (1:2)
• Firm binding to tissue proteins
• Plasma protein binding is 90%
• Metabolized in liver by demethylation and cyclization
• Withdrawal syndrome?
• Substitution therapy for opioid dependence
• Lower abuse potential
DEXTROPROPOXYPHENE
• Weak synthetic opioid, related chemically to methadone
• Lacks antitussive property
• Previously included in the OTC Analgesic combination
• Overdose –delirium & seizures
• Repeated dosing –cardiotoxicity & fatal
• Banned in India
BUPRENORPHINE
• Drug Class: Opioid Analgesics; Partial Agonist at µ And antagonist at K
Brand name: Buprenex
• Buprenorphine is indicated for the management of pain severe enough to
require an opioid analgesic and for which alternate treatments are
inadequate.
• Limitations of Use : Risks of addiction and abuse, inadequate analgesia
• Dosage: age, pregnancy, lactation, severity of pain, any respiratory illness,
renal and hepatic impairment
• Side effects: Sedation, headache, dizziness, Constricted pupils, adrenal
insufficiency
• Neonatal opioid withdrawal syndrome?
• Contraindication: Respiratory depression, git obstruction
• Buprenorphine –Naloxone?
QUIZ
• I am an opioid used commonly as a cough suppressant.😷 Who am I?
• I was once an OTC drug, but banned now.😞 Who am I?
• I am an opioid often used illicitly.🤭 Who am I?
• Mention drugs causing serotonin syndrome.😨
• I am an opioid used commonly as an anesthetic. Remember me?🤭
• Name the synthetic opioid used in treating opioid dependence.😶
• Buprenorphine-naloxone ?
SUMMARY
• CODEINE & PHOLCODINE –Cough
• HEROIN –illicit drug trafficking
• FENTANYL & REMIFENTANIL –Anaesthesia
• METHADONE –Opioid dependence
• DEXTROPROPOXYPHYNE –Banned
• PETHIDINE , TRAMADOL & TAPENTADOL –
Serotonin Syndrome
• BUPRENORPHINE-NALOXONE- treats opioid
addiction
Other opioids pharmacology

Other opioids pharmacology

  • 1.
    OTHER OPIOIDS - RASHMIRITHUSHA.V MBBS student SRMMCH&RC
  • 3.
    CODEINE • Natural opioid,methyl-morphine • Demethylation by CYP2D6 →Morphine • Potency -1/10th of morphine -analgesic property, • Potency -1/3rd of morphine -cough suppression • Less efficacious and partial agonist at µ opioid receptor • Oral route • Uses: cough, diarrohea • Side effect: constipation • Abuse liability is low
  • 4.
    PHOLCODINE & ETHYLMORPHINE • Havecodeine like properties • Used mainly as antitussives • Less constipating
  • 5.
    HEROIN • Diacetylmorphine →6mono-acetylmorphine →morphine • 3 times more potent than morphine • More lipid soluble →enters brain easily • Highly euphoriant on iv injection and addictive • Used in illicit drug trafficking as its highly potent • Sedative, emetic and hypotensive actions –less prominent • Banned in most countries except UK
  • 6.
    THIS IS WHATHAPPENS WHEN YOU TAKE HEROIN
  • 7.
    PETHIDINE (MEPERIDINE) • Synthesizedas an Atropine substitute • µ opioid receptor agonist • Actions blocked by naloxone • Metabolism – meperinidic acid and norpethidine To compare with morphine on the following aspects: 1.Potency 5.Spasmogenic action 2.Efficacy 6.Tachycardia due to antimuscarinic action 3.Onset of action 7.Absorption 4.Cough 8.Atropinic side effects Serotonin syndrome?
  • 8.
    REMIFENTANIL Faster acting congenerof fentanyl and used exclusively in anaesthesia
  • 9.
    METHADONE • Synthetic opioid •Full µ receptor agonist • Actions similar to morphine • High oral : parenteral activity (1:2) • Firm binding to tissue proteins • Plasma protein binding is 90% • Metabolized in liver by demethylation and cyclization • Withdrawal syndrome? • Substitution therapy for opioid dependence • Lower abuse potential
  • 11.
    DEXTROPROPOXYPHENE • Weak syntheticopioid, related chemically to methadone • Lacks antitussive property • Previously included in the OTC Analgesic combination • Overdose –delirium & seizures • Repeated dosing –cardiotoxicity & fatal • Banned in India
  • 14.
    BUPRENORPHINE • Drug Class:Opioid Analgesics; Partial Agonist at µ And antagonist at K Brand name: Buprenex • Buprenorphine is indicated for the management of pain severe enough to require an opioid analgesic and for which alternate treatments are inadequate. • Limitations of Use : Risks of addiction and abuse, inadequate analgesia • Dosage: age, pregnancy, lactation, severity of pain, any respiratory illness, renal and hepatic impairment • Side effects: Sedation, headache, dizziness, Constricted pupils, adrenal insufficiency • Neonatal opioid withdrawal syndrome? • Contraindication: Respiratory depression, git obstruction • Buprenorphine –Naloxone?
  • 15.
    QUIZ • I aman opioid used commonly as a cough suppressant.😷 Who am I? • I was once an OTC drug, but banned now.😞 Who am I? • I am an opioid often used illicitly.🤭 Who am I? • Mention drugs causing serotonin syndrome.😨 • I am an opioid used commonly as an anesthetic. Remember me?🤭 • Name the synthetic opioid used in treating opioid dependence.😶 • Buprenorphine-naloxone ?
  • 16.
    SUMMARY • CODEINE &PHOLCODINE –Cough • HEROIN –illicit drug trafficking • FENTANYL & REMIFENTANIL –Anaesthesia • METHADONE –Opioid dependence • DEXTROPROPOXYPHYNE –Banned • PETHIDINE , TRAMADOL & TAPENTADOL – Serotonin Syndrome • BUPRENORPHINE-NALOXONE- treats opioid addiction