A narcotic analgesic proposed for moderate to severe pain. It may be habituating. Ultracet is also prepared as a variable release capsules, marketed under the brand name ConZip. For example, a 150 mg capsule will contain 37.5 mg of the immediate release form and 112.5 mg of the extended release form.
Ultracet, a centrally-acting analgesic, exists as a racemic mixture of the trans isomer, with important differences in binding, activity, and metabolism associated with the two enantiomers. Although its mode of action is not completely understood, from animal tests, at least two complementary mechanisms appear applicable: binding of parent and M1 metabolite to μ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin. Opioid activity is due to both low affinity binding of the parent compound and higher affinity binding of the O-demethylated metabolite M1 to μ-opioid receptors. In animal models, M1 is up to 6 times more potent than ultracet in producing analgesia and 200 times more potent in μ-opioid binding. Opiate antagonist naloxone only partially antagonized ultracet-induced analgesia.
LD50=350mg/kg (orally in mice)
Strength: 325 Mg / 37.5 Mg
Pill Imprint: O M 650
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