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Opioid Analgesics & Antagonists(PHARMACOLOGY) - Coggle Diagram
Opioid Analgesics & Antagonists(PHARMACOLOGY)
1.Strong agonists
Pharmacokinetics
Hepatic metabolism
duration: 1-4h ,(methadone 4-6 h)
Toxicities
Respiratory depression, constipation, addiction liability
Clinical uses
Severe pain, anesthesia (adjunctive),dependence maintenance (methadone)
Mechanism of Action
Strong δ agonists variable S and κ agonists
Drugs
Fentanyl
hydromorphone
meperidine
morphine
methadone
oxymorphone
3.Mixed agonist-antagonist
Buprenorphine
Clinical uses
Moderate-to-severe pain dependence maintenance, reduces craving for alcohol (buprenorphine)
Pharmacokinetics
Buprenorphine(long duration)Nalbuphine (parenteral only)
Mechanism of Action
Partial µ agonist and
κ antagonist
Toxicities
Like strong agonists but can antagonize their
effects
Nalbuphine
Clinical uses
-
Pharmacokinetics
-
Mechanism of Action
κ agonist and µ antagonist
Toxicities
-
4.Antagonists
Clinical uses
Opioid overdose
dependence maintenance
(naltrexone)
Pharmacokinetics
Duration: naloxone 2 h naltrexone and
nalmefene 10h
Mechanism of Action
Antagonists at all opioid
receptors
Toxicities
Rapid antagonism of all opioid actions
Drugs
Antagonists
Naloxone
naltrexone
nalmefene
5.Antitussives
Codeine,dextromethorphan
Toxicities
Reduce cough reflex toxic in overdose
Pharmacokinetics
Duration: 0.5-1h
Clinical uses
Acute debilitating cough
Mechanism of Action
Mechanism uncertain Weak agonist inhibits norepinephrine and
5-HT transporters
Tramadol
Mechanism of Action
Weak agonist, blocks serotonin reuptake
Clinical uses
Moderate pain
adjunctive to opioids in
chronic pain states
Pharmacokinetics
Duration: 4 - 6h
Toxicities
Toxic in overdose
(seizures)
2.Partial agonists
Clinical uses
Mild-to-moderate pain;
cough (codeine) analgesic combinations with NSAIDs and
acetaminophen
Pharmacokinetics
Genetic variations in
metabolism
Mechanism of Action
As above, but lower affinity
Toxicities
As above, but weaker.
Drugs
Codeine
hydrocodone