1. P H R M A C O L O G Y - NOTE 9 - Opioid Analgesics (Nacrotic analgesic)
OPIOID ANALGESICS DRUGS
pure Agonist patial Agonist Atagonist
Morphine Nalorphine Pentazocainel Naloxone
Methagone
Codeine
Pholocodeine
Dextropropoxyphene
• Mu
Classes of Opioid Rs •Kappa
•Delta
Diphenoxylate
•CNS
Loperamide
place of Opioid R •Periphral tiissues
Noscapine •agonist if it is combined
partial Agonist with pure agonist.
(mixed agonist-antagonist) •antagonist if it is combined
Fentanyl with antagonist.
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2. P H R M A C O L O G Y - NOTE 9 - Opioid Analgesics (Nacrotic analgesic)
DRUG PHARMACOKINETIC USES ACTION SIDE EFFECT
Morphine Administration Strong analgesic for chronic pain (cancer). On CNS. Dysphoria.
All taken by orally. MI ACTION MECHNISM Respiratory depression.
Sustained release formulation. Add with inhaler GA to produce analgesia. 1 Analgesia Nausea & vomiting.
Morphine is given by I.V. Manegment for dyspnea. 2 Euphoria prominent with pain intra-cranial pressure.
Methadone o 75% of it, become inactive Strong analgesic for chronic pain (cancer). 3 Dysphoria Constipation.
Meperidine after absorption Strong analgesic for chronic pain (cancer). 4 Resp. sensitivity of RC to CO2 Urinary retention.
Analgesic for labor pain. 5 Nausea stimulation of CTZ Allergy:
Distribution
Add with inhaler GA to produce analgesia. Vomiting Itching.
They are well distributed.
Pure Agonists
Codeine Moderate analgesic for chronic pain (cancer) 6 Miosis agonize R on III c.n. Bronchospasm.
It is lipid soluble.
7 Antitussive depress the CC Tranceal rigidity(back
They cross BBB & placenta. Cough suppression.
pain)
hydrocodeine Moderate analgesic for chronic pain (cancer 8 BP & VD Depress VMC
Metabolism
Pholocodeine Cough suppression On CVS. ( in large iv dose)
By microsomal system
Dextropropoxyphen BP depress VMC VD
The metabolites are active.
Noscapine Heroin (diacetylmorphine) Morphine. direct VD effect
Diphenoxylate Codeine (Methylomorphine) Morphine. Treatment of diarrhea. release of histamine VD
Loperamide The metabolite are conjugated. On GIT.
Fentanyl Add with inhaler GA to produce analgesia. 1 Constipa- sphincter tone
Elimination tion s.m. motility
Mainly by kidney. 2 intra- spasm of bile duct
USES COTRA-INDICATION billary P spasm sphincter of oddi Treatment of addication
1) Analgesic for acute & chronic sever pain. 1) Head injury. On UT. Clonidine.
a. Acute pain (MI , post-operative) Miosis. 1 spasm of ureters Control withdrawal
b. Chronic pain (cancer) Resp. 2 Constriction of U sphincter symptom.
c. Labor pain 2) Biliary & renal colic(ex Meperidine) 3 micturation reflex
2) Cough suppression. Tolerance & Dependence. Methadone
3) Respiratory diseases.
3) Treatment of diarrhea. effect with repeated administration
(asthma & COPD)
4) Mangment of dyspnea. 1 Analgesic Rapid tolerance
5) Analgesic with GA 4) Acute abdomen pain.
Interfere with proper 2 Resp. Slow tolerance
a. Add with inhaler GA
diagnosis. 3 Miosis NOT develop
Acute MORPHINE poisoning 5) Pregnancy & labor (ex Meperidine) 4 constipation
Manifestation: Treatment Addict fetus. 5 convulsion
Coma / pin point pupil 1) Artificial respiration. Neonatal asphyxia. 6 Cross tolerance occur different agonist
Hypoventilation & hypoxia 2) Stomach wash. Addcation.
6) Liver diseases
Hypotension 3) Repeated I.V. Physical D Sudden withdrawal lead to
Deficient metabolism
Hypothermia Naloxone Psycho. D withdrawal syndrome
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3. P H R M A C O L O G Y - NOTE 9 - Opioid Analgesics (Nacrotic analgesic)
DRUG PHARMACOKINETIC USES ACTION SIDE EFFECT
Pentazocine Agonist on Kappa R. Analgesia. Dysphoria.
Partial agonist on Mu R. Psychomimetic effect.
Cause weak RC. Anxiety.
Mild dependency. Nightmares.
Partial Agonists
Mild withdrawal manifestations. Hallucination.
Withdrawal manifest.
with morphine addict.
Buprenorphine Maintainance drug for opioid dependent Psychomimetic effect.
patient. Anxiety.
Nightmares.
Nalorphine Hallucination.
Withdrawal manifest.
with morphine addict
Naloxone Acute opiod poisoing Reverse sever respiratory depression.
Antagonist
Pure
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