This interesting ppt is the continuation of the Pharmacology of Opioid analgesics I... This impressive ppt highlight the pharmacology, advantages and disadvantages of opioid analgesics other than morphine with illustrations....!!
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Pharmacology of Opioid analgesics II 2020
1. Dr. V. SATHYANARAYANAN M.B.B.S., M.D., ACME
PROFESSOR OF PHARMACOLOGY
SRM MCH & RC, KATTANKULATHUR, CHENNAI, INDIA
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*Morphine is the prototype of opioid analgesics
*It is Very useful in severe visceral pain, Though it has many
side effects
*It acts on opioid receptors
*Long term use cause tolerance and dependence
*Naloxone is the specific antidote for morphine poisoning
*Respiratory depression and hypotension has to be watched
for during morphine use
28. *
*Naturally occurring opium alkaloid
*Less potent than morphine ( 1/10th as analgesic)
*Depresses cough in subanalgesic doses
*Less constipating and respiratory depressant
*Less addiction liability
*Used as antitussive and in diarrhoea
*Combined with paracetamol for analgesia
41. *
* recently developed Synthetic codeine analogue
*Atypical opioid
*Weak opioid agonist
*Also blocks reuptake of serotonin, NA in the CNS additional
mechanism for pain relief
*Good oral bioavailability
*Generally well tolerated
*Cause sedation, dry mouth, nausea, mild respiratory depression
* may precipitate seizures
*Drug of dependence, but low abuse potential
*Avoided with MAO inhibitors, SSRIs ( serotonin syndrome )
*Used in mild to moderate acute and chronic pain
*Not for severe pain
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*Similar to tramadol
*Inhibition of NET is more marked than SERT
*Effective in moderately severe pain
*Less nausea and vomiting
*Risk of seizures and serotonin syndrome
*Useful alternate to tramadol
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*1/10th as potent as morphine
*Efficacy is equal to morphine
*More rapid onset of action & shorter duration of action
after I.M injection
*Does not effectively suppress cough
*Also has anticholinergic effects ( dry mouth, blurring of
vision)
*May produce negative inotropic effect
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*Similar to morphine
*Less constipation & urinary retention
*Dry mouth, blurred vision, tachycardia
*Serotonin syndrome
*Toxic doses sometimes produces CNS stimulation with
* tremors
*Restlessness
*Convulsions
*Because of norpethidine
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*Analgesic in visceral pain
*( preferred over morphine because of better
oral efficacy & less spasmogenic action )
*Obstetric analgesia ( less apnoea, no effect on
uterus )
*Preanaesthetic medication
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*Fentanyl and its congeners ( sufentanil,
alfentanil, remifentanil )
*Alphaprodine
*Diphenoxylate
*Loperamide
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*100 times more potent than morphine as analgesic and
respiratory depression
*Fast acting ( max effect within 5 minutes after I.V
Injection) but duration shorter (30-40 minutes )
*Mild effects on CVS
*Does not increase intracranial pressure
*Does not release histamine
*Available as transdermal patches ( act for 48 hours ) and
buccal preparation
*Commonly used opioid analgesic
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*In neuroleptanalgesia for short surgical procedures
*Postoperative analgesia, Obstetric analgesia ( epidural
fentanyl )
*Cancer/terminal illness pain
*Also used in chronic pain where opioid use is permissible
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*alfentanil, remifentanil are faster acting ( act
within a minute )
*Recovery is rapid
*Used for short surgical procedures
*Diphenoxylate , Loperamide used in
diarrhoeas
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*Synthetic opioid
*Mu receptor agonist
*Also blocks NMDA receptors
*Blocks monoaminergic receptor uptake transporters
*Has high oral:parenteral ratio ( 1:2 )
*90% plasma protein bound
*Gradually accumulates
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*Actions similar to morphine
*Effective analgesic
*Relieves even certain type of neuropathic pain,
cancer pain
*Longer duration of action ( t1/2 24-36 hours )
*Effective by many routes ( oral, rectal, SC, IV,
Spinal routes )
*Less abuse potential
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*Substitution therapy : in opioid dependence
*Methadone maintenance therapy in opioid addicts
*As an analgesic
*Caution --- may predispose to arrhythmias
*LAAM is a derivative of methadone with longer
duration of action than methadone
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*A congener of methadone
*Binds to opioid receptors with similar actions to morphine
*Less constipating
*Longer acting
*Good oral bioavailability
*Used in mild to moderate pain
*Several deaths have been reported ( rapid absorption
respiratory arrest, hypotension )
* has abuse potential
*Low efficacy
*BANNED IN INDIA, UK, EUROPE, USA ( CARDIOTOXICITY,
DELIRIUM, SEIZURES )
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*Related to pethidine
*Mild analgesic effects
*Low addiction potential
*Used orally in combination with NSAIDs
*EQUAGESIC – aspirin 325mg + ethoheptazine75mg
1tab tds
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*Analgesics of limited efficacy
*Equivalent to lower doses of morphine
*AGONIST-ANTAGONIST DRUGS
*Cause submaximal respiratory depression
*Less addicting
*Should not be administerd to patients who
receieved Mu opioid agonist May cause
withdrawal symptoms in addicts
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*Kappa receptor agonist, weak mu antagonist
*½ potent as morphine
*Cause primarily spinal analgesia
*Sedation, respiratory depression are less marked
*Increases BP and heart rate ( not suitable for MI )
*Less biliary spasm and constipation
*Less abuse liability
*Not a favoured analgesic now
*May be used for postoperative pain, moderately severe pain
in burns, trauma, fractures, cancer, etc
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*Analogue of naloxone
*Strong Kappa agonist with weak mu antagonist
*More potent analgesic than pentazocine
*Produces few dysphoric or psychotomimetic effects than
pentazocine
*Does not cause sympathetic stimulation, no cardiovascular effects (
safe in MI )
*Has a ceiling effect for analgesia and respiratory depression at
30mg IM
*Low abuse potential
*Useful in moderately severe pain, post operative pain
*10-20 mg IM
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*Synthetic thebaine congener
*Partial mu agonist
*25 times as potent as morphine
*Slow onset of action but long duration of analgesia
*Repeated use cause accumulation
*Less respiratory depression
*Lower tolerance and dependence
*Mild and late withdrawal symptoms
*Useful in Chronic painful conditions like that in terminal
cancer patients
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*For long-lasting painful conditions ( cancer pain )
*Premedication,
*post operative pain
*MI
*Treatment of morphine dependence ( alternative to
methadone )
*NOT SUITABLE FOR USE DURING LABOUR
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*Similar and more potent than pentazocine
*Causes tachycardia but does not increase BP
*Milder dysphoria
*1-2 mg IM/IV
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*Low doses good analgesic
*but no increased analgesia with increase in dose
*Causes dysphoria ( K agonist ) and respiratory
depression even in low doses
*Cannot be used as an analgesic
*High doses act as an antagonist and counters all
actions of opioids
*May be used in acute opioid poisoning
*Also used for the diagnosis of opioid addiction
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*Short acting agonist – antagonist with
anticholinergic actions
*Short duration of analgesia with less
respiratory depression
*Low incidence of confusion and abuse
*Suitable for obstetric analgesia
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*Pure antagonist
*For all 3 opioid receptors
*Normal people --- no actions
*Opium addicts – antagonises all actions of
morphine
*Blocks actions of endo.opioid peptides
*Dose – 0.4 mg IV
*Acts for 1-2 hours
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*Drug of choice for morphine overdosage
*To reverse neonatal asphyxia due to opioids
during labour
*Diagnosis of opioid dependence
*Hypotension during shock
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*More potent pure opioid antagonist
*Orally effective
*Longer duration of action ( 1-2 days)
*Used for opioid blockade therapy in post
addicts
*Used to prevent relapse of heavy drinking as it
Reduces alcohol craving
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*Several synthetic and semisynthetic opioids are
available
* some are more potent than morphine
*They afford several pharmacokinetic and
pharmacodynamic advantages over morphine
*The adverse effects also less with them
*Opioid antagonists are also useful therapeutically
*Short acting drugs are preferred for for acute pain
*Opioid rotation for chronic pain