6.2 Opioid & Non-Opioids

OPIOID & NON-OPIOIDS
Ilo
• Classification of pain and analgesics
• Members of opioid analgesics
• Mechanism of action
• Therapeutic Uses
• Precautions with Morphine Therapy

Classification
• Analgesic drugs; used to relief pain sensation are therapeutically
classified into:
A.Opioid Analgesics (narcotic analgesics).
This type of analgesics are used in pain with severe intensity
and visceral or internal origin.

B. Non-narcotic Analgesics (NSAIDS).
This type of analgesics are used in pain with mild to

moderate intensity and with somatic origin.
Therapeutic Uses
(1) Relief of Pain

The main therapeutic use of morphine is to relieve severe pain as that
encountered in acute myocardial infarction, acute pericarditis, bone
fractures, burns, pulmonary embolism, pleural effusion, spontaneous
pneumothorax and terminal stage of malignancy and is preferred over
aspirin like analgesics.
•For relief of sudden agonizing pain, morphine is usually given I.V.
where it produces immediate relief and minimizes shock.
** Excessive use of morphine to reduce postoperative pain should
be avoided as it may produce respiratory depression, urinary
retention and constipation; it may mask the signs of recovery and
prevent the early recognition of complications.
•In biliary colic morphine exacerbates rather than relieving pain due
to spasm of sphincter of Oddi and increases intrabiliary pressure.
•Atropine partially relieves morphine induced biliary spasm but
opioid antagonists (e.g. Naloxone) prevent or relieve it.
(2) In Preanesthetic Medication and as supplement during general
anesthesia with inhalational or I.V. agents. In high doses opioids are used
as primary anesthetic agents , most commonly , in cardiovascular and high
risk surgeries to minimize cardiovascular depression.
• In such cases, mechanical respiratory assistance must be provided.
(3) Cardiac Asthma with Pulmonary Edema
• Morphine is valuable in the treatment of acute left ventricular failure.

The dyspnea is dramatically relieved in response to intravenous
morphine. The mechanism underlying this relief is not clear but may be
due to reduced fear and apprehension and decreased respiratory and
cardiac effort.
Opioid analgesics
• The term opiate refers to morphine like properties.
Examples:
• Morphine. Meperidine (pethidine).
• Fentanyl. Methadone.
• Levorphanol
• Nalbuphine . Buprenorphine.
Sy.
Pentazosin
To stop action of morphine
Fentanyl partial agonists

Levorphanol
Opioid analgesics
Strong agonists (i.e, those with the highest analgesic efficacy, full
agonists) include morphine, methadone, meperidine (pethidine),
fentanyl, levorphanol, and heroin. Drugs with mixed agonist-
antagonist actions (eg, buprenorphine) may antagonize the analgesic
actions of full agonists and should not be used concomitantly.
Codeine, hydrocodone, and oxycodone are partial agonists with mild
to moderate analgesic efficacy. They are commonly available in
combinations with acetaminophen and nonsteroidal anti-inflammatory
drugs (NSAIDs). Propoxyphene, a very weak agonist drug, is also
available combined with acetaminophen.
Mechanism of action
• Opioids act on stereospecific binding sites or receptors in CNS (high
concentrations in the Limbic system) and other tissues all over the body.
Different contribution for final response:
1. ( mu ) include two types
μ1 : supraspinal analgesia (descending inhibitory pain)
μ2: spinal analgesia (dorsal horn), respiratory depression, sedation,
euphoria, miosis and decreased GIT-motility.
2. ĸ ( kappa ):
responsible for spinal analgesia,
dysphoria, hallucinations
3. δ ( delta ) :
• they may produce analgesia at both spinal and supraspinal levels.
After prolonged use, tolerance of previous dose with decreased
response is produced due to down regulation& desensitization of
opioid receptors thus dose needs to be increased.
If stopped suddenly will produce withdrawal effects (diarrhea,
anxiety, nervesnous, agitation, pain, insomnia, dysphoria,
tachycardia, headache)
• Naloxone t1/2 =1hr, Morphine t1/2= 4hrs
• May need more than one vial of naloxone depending on respiratory
assessment of the patient after one hour.
• Naloxone is not used with addicts as it will precipitate withdrawal
syndromes
• Naloxone is preserved in case of emergency cases of acute toxicity of
morphine overdose.
• Methadone has the greatest bioavailability of the drugs used orally, and
its effects are more prolonged. Tolerance and physical dependence
develop, and dissipate, more slowly with methadone than
with morphine. These properties underlie the use of methadone for
detoxification and maintenance programs (fewer withdrawal signs on
abrupt discontinuance than morphine).
Precautions with Morphine Therapy
1) The use of morphine in asthmatic patients is hazardous as it depresses
the respiratory center and cough reflex, releases histamine
(2) When morphine is administered to the mother during labor, it crosses

the placental barrier and the newborn infant may exhibit manifestations
of respiratory depression "asphyxia neonatorum”.
(3) Patients with diminished respiratory reserve as in emphysema,

kyphoscoliosis, severe obesity and chronic cor-pulmonale, morphine
should be given with caution because such patients are already on
hypoxia which they compensate for by an increased respiratory rate.
(4) ‘’ Cardiac Asthma with acute Pulmonary Edema
• Morphine is valuable in the treatment of acute left ventricular
heart failure.
• The dyspnea is dramatically relieved in response to intravenous
morphine.
• The mechanism underlying this relief may be due to:
reduced fear and apprehension (analgesia; sensory and emotional)
and decreased respiratory centers in brain and decrease tachypnea
(5) Morphine also produces miosis and mental clouding
(6) In acute abdomen cases, pain is a chief diagnostic symptom and

its total abolition may interfere with the diagnosis. Morphine should
not be given until the diagnosis is made.
(7) An ordinary dose of morphine given to myxedematous patients
may cause coma for about 3 days.
Patients with myxedema ( low Basal Metabolic Rate ) are more
sensitive to morphine while hyperthyroid individuals seem more
tolerant.
(8) Patients with reduced blood volume are more susceptible to the
hypotensive effect of morphine and therefore should be used with
caution in any type of hemorrhage.
(9) Patients with severe hepatic and/or renal dysfunction are not able
to tolerate morphine. Cumulative toxicity can occur due to
inadequate metabolism and /or excretion of morphine.
Thank You
Any Questions?

6.2 Opioid & Non-Opioids

Uploaded by

Copyright:

Available Formats

6.2 Opioid & Non-Opioids

Uploaded by

Document Information

Original Description:

Original Title

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

6.2 Opioid & Non-Opioids

Uploaded by

Copyright:

Available Formats

OPIOID & NON-OPIOIDS

• Members of opioid analgesics

• Precautions with Morphine Therapy

and visceral or internal origin.

This type of analgesics are used in pain with mild to

(1) Relief of Pain

• In such cases, mechanical respiratory assistance must be provided.

(3) Cardiac Asthma with Pulmonary Edema

• Morphine is valuable in the treatment of acute left ventricular failure.

• Morphine. Meperidine (pethidine).

Fentanyl partial agonists

(2) When morphine is administered to the mother during labor, it crosses

(3) Patients with diminished respiratory reserve as in emphysema,

and decreased respiratory centers in brain and decrease tachypnea

(5) Morphine also produces miosis and mental clouding

(6) In acute abdomen cases, pain is a chief diagnostic symptom and

You might also like