The document discusses various classes of opioid analgesics, including their classifications, mechanisms of action, pharmacologic effects, and therapeutic uses. It highlights key opioids such as morphine, codeine, fentanyl, and methadone, along with partial agonists like buprenorphine and pentazocine, and antagonists including naloxone and naltrexone. Additionally, it briefly mentions other centrally acting analgesics like tapentadol and tramadol for pain management.

1. PRESENTED BY- AMEENA MEHABOOB

2. OPIOID
•Morphine type
NON-OPIOID
•Aspirin type

3. OPIOID ANALGESICS

4. CLASSIFICATION

5. • Most analgesic effects
• ADR- euphoria, sedation, dependence, resp depressionᵘ receptors
• Analgesia
• Proconvulsantᵟ receptors
• Analgesia at spinal level
• Sedation, dysphoria, hallucinationsᵏ receptors
• Not true opioid receptors
• Site of action for psychomimetic drugsσ receptors
OPIOID RECEPTORS

7. 1. MORPHINE

8. MECHANISM OF ACTION

9. PHARMACOLOGIC ACTIONS
Analgesia
Euphoria, sedation, hypnosis
Respiratory depression
Depression of cough reflex
Miosis
Emesis
Excitatory effects
CNS EFFECTS

10. • Hypotension
CVS
• Gastric motility-decreased
• Decreases intestinal secretions
GIT
• Decrease renal blood flow
• Antidiuretic effect
Renal function
• Inhibit release of GnRH
• Decrease blood levels of FSH, LH, ACTH
Neuroendocrine
effects

11. PHARMACOKINETICS
• Orally- absorption slow
• 1st pass metabolism
• Bioavailability- 20-40%
• SC, onset of action- 15-20 min
• Peak effect- 1 hr
• T1/2- 3-5hr
• Duration of action- 3-5hr

12. DOSE
Oral
• 10-50mg
SC/IM injection
• 10-15mg
IV
• 2-6mg

13. ADR
Nausea
Vomiting
Dizziness
Drowsiness, Sedation
Mental clouding
Constipation
Respiratory depression
Urinary retention

14. CODEINE
•Naturally occuring opioid
•Weak analgesic compared to
morphine
Analgesic
Anti tussive
Anti diarrhoeal
Therapeutic uses

15. FENTANYL
•Synthetic opioid
•100 fold analgesic potency of morphine
•Used in anesthesia

16. SUFENTANIL, ALFENTANIL,
RAMIFENTANIL
•Synthetic opioid analgesic
•Related to Fentanyl
•Used during surgical procedures requiring anesthesia

17. METHADONE
•Synthetic opioid
•Less euphoria
•Longer duration of action
Similar to morphine
Anti tussive
PHARMACOLOGICAL ACTIONS

18. PARTIAL AGONISTS AND MIXED
AGONIST-ANTAGONISTS
1. BUPRENORPHINE
• Opioid detoxification
• Less severe withdrawal
symptoms
• Treatment of opioid
dependence

19. 2. PENTAZOCINE
•Relieve moderate pain
•Less euphoria compared to morphine
•High doses-
•Hallucination, nightmares, dysphoria, tachycardia

20. 3. NALBUPHINE, BUTORPHANOL
•Limited use in chronic pain
•Butophanol- severe headaches- nasal, abuse

21. ANTAGONISTS
A) NALOXONE
•Reverse coma, respiratory depression of opioid overdose
•Within 30 sec of IV administration, resp depression and coma are
reversed
•Competitive antagonist
•T1/2- 30-81min

22. B) NALTREXONE
•Longer duration of action than Naloxone
•Single oral dose blocks effect of heroin for upto 24 hrs
•Used in combination with Clonidine for opioid detoxification
•Can lead to hepatotoxicity

23. OTHER ANALGESICS
1. TAPENTADOL
•Centrally acting analgesic
•Manage moderate to severe pain
•Immediate release and extended release formulations

24. 2. TRAMADOL
Centrally acting analgesic
Moderate to moderately severe pain