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OPIOIDS . Dr. Hisham Zein Alabdin. Plant origin. It is the dried extract of the poppy plant: Popover somniferum . Raw opium typically is composed of at least 10% morphine. Opioids. The term opioids are compounds that exert pharmacologic activity at opioids receptors.

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opioids

OPIOIDS

Dr. Hisham Zein Alabdin

plant origin
Plant origin
  • It is the dried extract of the poppy plant: Popover somniferum.
  • Raw opium typically is composed of at least 10% morphine.
opioids1
Opioids

The term opioids are compounds that exert pharmacologic activity at opioids receptors.

Opium derivatives:

  • Natural: morphine , codeine.
  • Semi- synthetic: heroin (Diacetyl morphine) , apomorphine.
  • Wholly synthetic: methadone, pethidine.
slide4
Uses
  • Medical: Analgesic,
  • Surgical.
  • Toxicological uses: in corrosive .

Contraindications:

  • Age: patient less than twelve (very sensitive respiratory center).
  • Head injury: it masks the pupil change, it leads to increased intracranial pressure by producing vasodilatation.
slide5

Acute abdomen: it masks the sign and symptom.

  • Bronchial asthma:(it cause bronchospasm).
  • Pregnancy and delivery: (crosses placental barrier)
  • Liver & kidney disease .
toxicokinetics
Toxicokinetics
  • Absorption: are well absorbed from GIT, IM, subcutaneous.
  • Metabolism: it takes place in the liver undergo hepatic conjugation with glucoronic acid .
  • Excretion: stomach is the main excretory organ (reexcetion).
clinical picture
Clinical picture

A-CNS

Are combination of stimulation and depression. There is transient euphoria followed by dysphoria .

Stimulant effects:

  • Chemoreceptor trigger zone nausea, vomiting
  • Vagus nucleus slow full pulse.
  • Third nerve nucleus pin point pupils.
slide8

Depressant effects:

  • on cerebral cortex:
  • Analgesia :by increasing pain tolerance and altering psychological response to pain.
  • Suppression of anxiety sedation.
  • Drowsiness, mood changes and mental cloudiness followed by sleep.
slide9

On the cough centre suppression of cough reflex.

  • On the respiratory centre slow, shallow (by reducing the sensitivity of respiratory centre to raised arterial CO2 tension) and apnea.
  • On the heat regulating centre hypothermia
slide10

On the cough centre suppression of the cough reflex e.g. codeine.

  • On respiratory centre slow, shallow respiration (by reducing the sensitivity of respiratory centre to raised arterial Co2 tension) and apnea.
  • On the heat regulating centre hypothermia
b cardiovascular effects
B) Cardiovascular effects:
  • Peripheral vasodilatations orthostatic hypotension and syncope due to release of histamine and central depression of vasomotor centre.
c gastrointestinal effects
C) Gastrointestinal effects

Mainly constipation due to:

1- Decreased gastrointestinal motility.

2- Decreased HCL secretion

3- Increased antral muscle tone and duodenal muscle tone.

4- Increased iliocecal valve and sphincter tone.

d biliary tract
D) Biliary tract:

Aggravates biliary colic by:

1- Constriction of sphincter of Oddi.

2- Increased biliary tract pressure.

3-Decreased biliary secretion.

e genito urinary tract
E) Genito- urinary tract:
  • Increased detrusor muscle tone and increased vesicle sphincter tone urgency and retention of urine, it is aggravated by increased secretion of ADH.

F) Skin:

Flushing, urticaria, and skin rash.

diagnosis
Diagnosis
  • By circumstantial evidence
  • History
  • Clinical examination:
  • CNS depression, miosis, hypothermia and respiratory depression.
differential diagnosis
Differential diagnosis
  • Other toxic coma (parathione).
  • Traumatic and pathological coma with miosis the most important is coma due to pontinehaemorrhage.
investigation
Investigation
  • TLC

It gives a positive result about 30 minutes after a single dose and remains +ve up to 36 hrs and up to 72 hrs after repeated doses.

treatment
Treatment
  • A B C
  • Prevent further absorption
  • Narcotic antagonists:
  • Pure narcotic antagonist: Naltrexone, Naloxone(Narcan).
  • Mixed narcotic agonist-antagonist: Not used
disadvantages of mixed agonist antagonist
Disadvantages of mixed agonist-antagonist
  • So they can produce synergism with opiates and aggravate respiratory depression.
  • In non opiate poisoning, they produce symptoms and signs like opiate toxic effects.
  • In addicts they produce severe withdrawal syndrome.
cause of death
Cause of death
  • Central asphyxia
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