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Opioid Autacoids

OPIOID

An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract. The receptors in these organ system mediate both the beneficial effects and the side effects of opioids.

.Classification  Opioid drugs include:  Full agonists  Partial agonists Pentazocin  Antagonists Naloxone Naltrexone Morphine Heroin Codeine Thebaine Etorphine Fentanyl Meperidine (Pethidine) Methadone Opioid peptides  Partial agonists can displace full agonists and produce antagonistic effects.

 .  Endogenous opioid peptides have been implicated in pain modulation. They can be released during stressful conditions such as pain or the anticipation of pain.Endogenous Opioid Peptides  Some regions in the brain contain peptides with opioid-like properties (endogenous opioid peptides).

The opioids act on neurons by:   Closing voltage-gated ca2+ channels on presynaptic nerve terminals and reducing transmitter release. Hyperpolarizing and inhibiting postsynaptic neurons by opening K+ channels. All are members of the G protein-coupled family.  .   Some opioids.Opioid Receptors  Three classes of opioid receptors ( µ. δ. can produce an agonist effect at one receptor subtype and an antagonist effect at another. κ) have been identified.

euphoria.d  Analgesia.Opioid Receptors Cont.  Opioid analgesic effects also include interaction with kappa and delta receptors. respiratory depression. All three major receptors are present in high concentrations in the dorsal horn of the spinal cord.  . and physical dependence result from actions at µ receptors.

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 Euphoria   Dysphoria  . Pleasant floating sensation with lessened anxiety and distress. An unpleasant state characterized by restlessness and malaise.Organ System Effects  Analgesia  Pain consists of both sensory and emotional components. Opioids reduce both aspects of the pain. may sometimes occur.

Organ System Effects Cont. . Combination of morphine with other central depressant drugs results in very deep sleep.d  Sedation  Drowsiness and clouding of mentation are frequent concomitants of opioid action.   Cough suppression.

Organ System Effects Cont. It is possible to partially overcome respiratory depression by stimulation of various sorts. in newborn infants (useful in obstetric). Meperidine produces less respiratory depression.d  Respiratory depression   The respiratory depression is dose-related. No tolerance develops for miosis.   Miosis   It is valuable in the diagnosis of opioid .

d  Gastrointestinal tract  Constipation Constriction of biliary smooth muscle.  Biliary tract   Renal    . especially in postoperative patients. which may result in biliary colic.Organ System Effects Cont. Increased sphincter tone may precipitate urinary retention. Ureteral colic by a renal calculus may be made worse by opioids. In this case (and biliary colic) the dose of opioid should be increased.

Stimulant drugs (amphetamine) enhance the analgesic actions of the opioids (useful in chronic pain).  . constant pain is relieved. Fixed interval administration (regular dose at regular time) is more effective than dosing on demand. Sharp.Clinical Use of Opioids  Paine relief    Severe. intermittent pain is not controlled.

Clinical Use of Opioids Cont.d  Acute pulmonary edema.  Cough suppression:  Obtained at doses lower than those needed for analgesia. The opioids used are: dextromethorphan & codeine In patients taking MAO inhibitors hyperpyrexic    . The effect is also produced by isomers of opioids that are devoid of analgesic and addiction effects.

Clinical Use of Opioids Cont. Not suitable treatment for all kinds of diarrhea. The usual dose is two tablets to start and then one tablet after each diarrheal stool.d  Anesthesia  In cardiovascular surgery where a primary goal is to minimize cardiovascular depression. Diarrhea from almost any cause can be controlled. is used in combination with atropine.  Diarrhea     . Diphenoxylate as an antidiarrheal drug.

Use during pregnancy. .Contraindications  Contraindications and cautions in therapy:  Use of pure agonists with weak partial agonists.   Use in patients with head injuries.

 Tolerance clinically appears after 2–3 weeks of frequent exposure.Tolerance  Tolerance begins with the first dose of an opioid. 60 mg of morphine causes respiratory arrest in a nontolerant person. 2000 mg of morphine may not produce respiratory depression. .    In addicts. The degree of tolerance may be up to 35 fold.

H.Farjoo .High Tolerance Analgesia Euphoria. dysphoria Mental clouding Respiratory depression Sedation Nausea & vomiting Cough suppression No Tolerance Miosis Constipation Convulsions Antidiuresis M.

Withdrawal or Abstinence Syndrome  Manifestations:        Rhinorrhea Lacrimation Yawning Chills Piloerection Hyperventilation Hyperthermia Mydriasis  Muscular aches  Vomiting  Diarrhea  Anxiety  Hostility  .

most of the effects have disappeared. Peak effects are seen at 36–48 hr. tolerance also disappears. It may last as long as 2 weeks. . Craving for opioid may persist for many months.  Methadone:     After the abstinence syndrome subsides. After the last dose.Withdrawal or Abstinence Syndrome Cont.d  Morphine or heroin:    Signs start within 6– 10 hr. Several days are required to reach the peak effects. but some may persist for months. By 5 days.

A depressed patient may recover after a single dose of naloxone and appear normal. Intravenous injection of naloxone reverses coma due to opioid overdose but not that due to other CNS depressants.Opioid Overdose   Injection of pure opioid antagonist drugs. Naloxone has a short duration of action (1–2 hours).   . but relapses into coma after 1–2 hours.

It induces seizures and is relatively contraindicated in patients with a history of epilepsy. so can be used with full agonists for chronic neuropathic pain.Tramadol  Tramadol is a strong analgesic which blocks serotonin reuptake.   . It is a weak µ receptor agonist.

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