Brands, Medical Use, Clinical Data
Drug Category
- Analgesics
- Narcotics
- Opiate Agonists
Dosage Forms
Brands / Synonyms
Adopol; Alidine; Anileridina [Inn-Spanish]; Anileridine [Ban:Inn]; Anileridinum [Inn-Latin]; Apidol; Apodol; Leritin; Leritine; Nipecotan; Phthalylsulfathiazole; Sulfathalidine
Indications
For treatment and management of pain (systemic) and for use as an anesthesia adjunct.
Pharmacology
Anileridine, a potent analgesic, is an analog of pethidine. Anileridine is useful for the relief of moderate to severe pain. It may also be used as an analgesic adjunct in general anesthesia in the same manner as meperidine to reduce the amount of anesthetic needed, to facilitate relaxation, and to reduce laryngospasm. In addition, anileridine exerts mild antihistaminic, spasmolytic and antitussive effects. Anileridine's main pharmacologic action is exerted on the CNS. Respiratory depression, when it occurs, is of shorter duration than that seen with morphine or meperidine when equipotent analgesic doses are used.
Mechanism of Action
Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Opioids such as anileridine close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Absorption
Anileridine is absorbed by all routes of administration.
Toxicity
Symptoms of overexposure include dizziness, perspiration, a feeling of warmth, dry mouth, visual difficulty, itching, euphoria, restlessness, nervousness and excitement have been reported.
Biotrnasformation / Drug Metabolism
Hepatic
Contraindications
Anileridine is contraindicated in the presence of respiratory depression.
It should not be used when respiratory failure is a possibility (head injury or brain tumor). In addition, the use of
anileridine is contraindicated when there is a known hypersensitivity to the drug or any of the nonmedicinal
ingredients of the preparations.
Drug Interactions
Caution should be observed when anileridine is coadministered with other
opioids, sedatives, phenothiazines, or anesthetics, as these agents may increase respiratory and circulatory
depression.
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