Opioids
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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.


Opioids

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.


Opioids

  • 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.


Opioids

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.


Opioids

  • 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


Opioids

  • 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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