Meperidine is commonly underprescribed in terms of dose and interval. Meperidine is metabolized to normeperidine, a compound capable of inducing seizures at high concentrations. Meperidine is not recommended for the treatment of chronic pain because of the risk of seizures with repetitive dosing and its short duration of action. Meperidine is often used as a rescue medication for treatment of Migraine, meaning used for controlling severe Migraine when a Migraineur dose not respond to abortive treatments or the Migraineur cannot use effective abortive regimes when they are contraindicated. Meperidine is available in both oral and parenteral forms and was approved by the FDA and marketed in 1942.
Meperidine is primarily a kappa-opiate receptor agonist and also has local anesthetic effects.
Meperidine has more affinity for the kappa-receptor than morphine. Opiates do not alter the pain threshold of afferent nerve endings to noxious stimuli, nor do they affect the conductance of impulses along peripheral nerves. There is no ceiling effect of analgesia for opiates. The emotional response to pain is also altered. Binding of GTP leads to a release of the G-protein subunit, which acts on the effector system.