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Pharmacology C.N.S 58070d26

Mechanism of action of methadone is

A
Opioid receptor agonist
B
Opioid receptor partial agonist
C
Opioid receptor antagonist
D
Opioid receptor inverse agonist
High-Yield Explanation
Ans. is 'a' i.e., Opioid receptor agonist Methadone* Methadone is opioid receptor agonist.* Most important feature is high oral: parenteral activity ratio (1:2) and firm binding to tissue protein.* It relieves cancer and neuropathic pain not responding to morphine.* Abuse potential is less than morphine.* It also blocks NMDA receptors and uptake of monoamines.* It is the drug of choice for substitution therapy of opioid dependence.* 1 mg of methadone can be substituted for 4 mg of morphine.* Methadone is less hypnotic than morphine (sedative action is less intense).

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