Opioids in anesthesia

Opium derived from dried juice of poppy plant which contains over 20 plant alkaloids.including morphine and codiene.

NARCOTIC AGONISTS Site of Action

*Opioid receptors are predominantly located in the: 1-Brain stem (amygdala,corpus striatum,periaqueductal gray matter and medulla) 2-spinal cord (substantia gelatinosa). 3- GIT

They act on 3 types of receptors:

*

1. Mu receptors:analgesia,respiratory depression,euophoria,and physical dependence. 2.Kappa receptors:analgesia,sedation,respiratory depression,miosis. 3.Segma : dysphoria,hallucination,tachypnea,tachycar dia.

PHARMACOKINETICS
-Rapied distribution through the body following IV injection. -It is metabolised by the liver and the majority of the inactive metabolites are excreted unchanged in the urine.

PHARMACODYNAMICS CNS:
Opioids sedate through interfering with sensory perception of painful stimuli. **large doses produce unconsciousness but they are generally incapable of producing anesthesia and it can not guarantee total amnesia. It may produce nausia & emesis through stimulation of the chemoreceptor trigger zone.

RESPIRATORY
They result in dose related depression of respiratory rate and minute volume.but increase the tidal volume which will lead to a slow deep respiration.Reversed by Naloxone adminstration.

CVS
Opioids have litle myocardial depressant effect even when adminstrated in high doses. Supplementation with either N2O or Benzodiazepines my depress cardiac output. They decrease systemic vascular resistance either by decreasing sympathetic outflow or by releasing histamine ( as Morphine) which produces vasodilatation & decrease SVR. Synthetic opioids are less likely to release histamine. They lead to bradycardia by stimulation vagal nucleus in the brain stem.

GIT
*Narcotics slow GI mobility and may result in constipation or post operative ileus. **increases biliary tract tone which may lead to biliary colic eith patients with bile stones.

OTHERS
***Increases the bladder sphincters tone. And urine retention ***Anaphylactic reactions,bronchospasm,chest wall regidity and pruritis.

FENTANYL & MORPHINE

Fentanyl is the most commonly used during induction of anesthesia due to its rapied onset(highly lipid solubility)and predictable duration of action about 30 minutes **Morphine is used in the preioperative period to provide long lasting analgesia.and it should be adminstrated slowlyat a rate< 5 mg/min to avoid excessive histamine release.

Potency Ratio

Analgesic dose 10 mg

Low dose
0.05-0.2 mg/kg 0.5-3 mic g/kg

Morphine

Fentanyl

100

100 mcg

NARCOTIC ANTAGONISTS
NALOXONE: It competes at the mu,delta,kappa and sigma receptors. Peak effect 1-2 minutes. Duration of action 30-60 min. Indicated in perioperative surgical patientsnwith excessive sedation or respiratory sedationnsecondary to opioids.

 Given in small incremental doses. High doses of naloxone will result in sudden reversal of analgesiac effects leading to abrupt tachycardia,pulmonary edema,arrythmias and cardiac arrest.

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