COMPLETE INTRODUTIONS OF OPIOIDS, MODE OF ACTONS,PHARMACOOGY,CLINICAL USES AND SIDE EFFECTS.

1. OPIOIDS
DEFINITION
CLASSIFICATION(MODE
OF ACTIONS)
PHARMACOLOGY
CLINICAL USES
SIDE EFECTS
IMPORTANT POINTS

2.  DEFINITION-Opioids are the class of drugs which is naturally
found in opium poppy(paper somniferum) plant and that work in
brain to produce variety of effects , Including the pain relief with
many of these drugs.
 CLASSIFICATION
A. Chemical classification
Two types of alkaloids contains in opium poppy capsule
1.Phenanthrene derivatives- Morphine ,codeine and thebaine(NA)
2.Benzoisoquinoline derivatives- Papaverine(NA),Noscapine(NA)
NA*-NONANALGESIC

3. B. On basis of source
1. Natural- Morphine, codeine( mor co natural ki samjo).
2. Semisynthetic-Di acetyl morphine(heroine),pholcodeine.
(DAM sexy heroine phoolo co semi synthetic bolti h)
3. Synthetics-Pethidine (meperidine) ,fentanyl , methadone,
Taramadol, Dextrophophoxyphene.
 Mode of action
1. Morphine-It acts as a mu and kappa agonist of opioids
recepter.

4. 2.Codeine-It’s partial agonist of mu opioids receptor and having very
low affinity towards opioids receptor.
3.Heroin(Di acetyl morphine)-It is agonist of mu ,kappa and delta
opioid receptors and heroin is three times more potent then
morphine. Also known as Diamorphine.
4.Pethidine(Meperidine)-It is mu opioid receptor agonist.
5.Fentanyl- It is mu opioid receptor agonist.
6.Tarmadol-Affinity toward mu is low , while kappa and delta receptor
affinity is very low of Tarmadol.

5.  PHARMACOLOGY
1.Morphine-Pharmacology
CNS- sedation, analgesic, euphoric, cough center suppuration,
Respiratory center depration
CVS- Bradycardia, vesodialatio,
GIT- Decrees the GIT mobility(constipation),decrees the GIT fluid
secretion.
Others- Miosis(pupil constriction) , Hyperglycemia,Anticholinergic
Action.
Morphine is metabolized by liver glucuronide congugation.

6. 2.CODEINE- It is more selective cough center suppressant and
use in Diarrhea .
IMPORTANT NOTES-Morphine is the only opioid which is agonist
of mu, kappa and delta.
 Morphine withdrawal syndrome cure by Methadone.
 Human Lethal does of morphine is 250mg and Antidote o
morphine is Naloxone.
 Morphine is not use in head injury due to its effect on CTZ and
increase intracranial pressure.
 Fantanyl+Dolpridol provides nuroleptic analgesia.

7. ENDOGENOUS OPIOID PEPTIDES
• These components having morphine like action and they
isolated from mammalian brain, pituitary, spinal cord and GIT.
• Same like morphine there action is blocked by naloxone.
• Mainly are in three types
1.Endorphins-Primerly it is mu agonist but also have delta
actions.(mu>delta>>kappa)
2.Enkephalins- Equal action on mu and delta
receptor.(mu=delta>kappa)
3.Dynorphine- More selective towards kappa receptor then
mu.(kappa>>mu=delta)

8. CLINICAL USES
 Analgesic
 Pre-anesthetic
 Diarrhea
 Cough suppressants
 Vomiting inducer
 Sedative
 Balanced anesthesia and surgical analgesia
 Cardiac asthma (Acute left ventricular failure)

9. SIDE EFFECTS OF OPIOIDS
 Dependency
 Withdrawal syndrome of morphine
 Allergy
 Idiosyncrasy
 Acute morphine poisoning