Includes OPIOID drugs - Codeine, Pholcodine, Ethylmorphine, Heroin, Pethidine, Fentanyl, Remifentanil, Methadone, Dextropropoxyphyne, Tramadol, Tapentadol and Buprenorphine

1. OTHER OPIOIDS
- RASHMI RITHUSHA.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
• Have codeine like properties
• Used mainly as antitussives
• Less constipating

5. 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

6. THIS IS WHAT HAPPENS
WHEN YOU TAKE HEROIN

7. 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?

8. REMIFENTANIL
Faster acting congener of
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 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

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 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 ?

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