Above slides consist of detailed description about opioid. This includes agonist , antagonist , side effects, toxicity of opioid.

1. SUBMITTED BY :-
ATHISAM (1421723)
JAGDEEP (1421726)
SHIVANI (1421734)
SUBMITTED TO :-
MR. RANDHIR SINGH
DAHIYA
M.M. COLLEGE OF
PHARMACY , MULLANA

2. • Opioids are substances that act on opioid
receptors to produce morphine like effects.
Medicinally they are primarilly used for pain
relief, including anesthesia.
• Opioid are derived from opium poppy plant
Papaver somniferum.

3. Analgesic:- drug that selectively relieves the pain at CNS or
peripherally.
Types:-
Somatic pain:- originate from skin.
Cause :- inflammation, it is sharp and defined.
Visceral pain:- pain arising from viscera (dull aching type)
Cause:- spasm, ischemia, inflammation
difficult to pin point the site of pain.

5. 1. Mu subtypes µ1,µ2
location :- thalamus, grey matter, area postrema, dorsal horn.
Effect :- µ1 analgesia , euphoria, sedation,
µ2-> respiratory depression, constipation.
2.Kappa(k):-k1,k2,k3
location:-cerebral cortex,hipocampus,striatum,mid brain,dorsal horn
effects:-analgesia,respiratory depression,sedation,miosis,constipation
3.Delta(δ)
location:-myentric plexus,trigeminal nucleus
effect:-analgesia,respiratory depression

6. AGONIST
Alfantanil,fentanyl,heroin,hydrocodone,methadone,morp
hine.
moderate/low agonist :-codeine
mixed agonist -antagonist:-
buprenorphine,butorphanol,pentazocine
Antagonist :naloxone, neltraxone,nalmephene.

7.  All opioid receptors are g protein coupled receptor.
 Opening of potassium channel (hyperpolarisation)
 Inhibit the opening of calcium channel.
 Decrease release of neurotransmitter GABA,NA,5-HT
 Decrease transmission of pain impulse.

9.  Potent analgesic action on kappa receptor in the spinal cord and
a weak opoid antagonist activity at mu receptor.
 It does not cause euphoria
 It causes less respiratory depression
 ADVERSE REACTIONS sedation ,sweating, hallucinations

10.  It is a competitive antagonist at mu and exerts agonistic
action on kappa receptor.
 It is 20 times as potent as pentazocine
 ADVERSE REACTIONS sedation, necrosis vomiting

11. • Naloxone
• Naltrezone
• Nalbuphene
• Levallorphan
• Alvimopan

12. NALOXONE

13. • Acute opioid intoxication is characterized by euphoria and
drowsiness .mast cell effects(flushing ,itching)are common
particularly with morphine

14. The patient who has taken an overdose of an opioid usually is
stuporous.
Respiratory rate will be low the patient may be apniec and cyanosis
may be present
BP may fall
Pupil dilates due to hypoxia
Urine formation is decompressed
Skeletal muscle or flaccid.

15.  Examination of urine and gastric
contents for drugs may aid in diagnosis.

16. The first step is to establish a patient airway and
ventile the patient
Naloxone is the treatment of choice
The safest approach is to dilute the standard naloxone
dose (0.4 mg) and slowly administered it IV monitoring
arousal and respiratory function.

17. ACUTE
EFFECTS
CHRONIC
EFFECTS

18. • Effect on hypothalamus
• Miosis
• Convulsions
• Respiration
• Cough
• Nausea and vomiting

19. TOLERANCE :- marked tolerance can develop with the exception of miosis
and constipation .Tolerance to opioids defined as a loss of effect,
The mechanism of tolerance may involve receptor uncoupling . antagonist
of glutamate NMDA receptor.
E.G:- ketamine as well as delta receptor antagonist reported to block
opioid tolerance
DEPENDENCE :- .
Physical dependence is revealed on abrupt discontinuence as an abstinence
syndrome include rhinorrhea, lacrimation, chills, muscle aches, diarrhoea,
anxiety

20. • Infants and elderly are more susceptible to respiratory
depressant.
• It is dangerous in patients with respiratory insufficiency ;
sudden death may occur
• Opioids with low histamine releasing potential (fentanyl) should
be used in asthma patients.
• Morphine is contraindicated in patients with head injury.