🧬 Receptor activity
Mechanism of action
The pharmacologic actions of pemoline are qualitatively similar to those of the amphetamines and methylphenidate, and include CNS and respiratory stimulation and weak sympathomimetic activity. ... Limited animal experiments suggest that the CNS stimulatory action of pemoline may be mediated by brain dopamine. Pemoline may produce an increase in motor activity, mental alertness, diminished sense of fatigue, and mild euphoria. ... In usual therapeutic dosage, pemoline exhibits no substantial effects on the peripheral circulatory system.
Cylert (pemoline) has a pharmacological activity similar to that of other known central nervous system stimulants; however, it has minimal sympathomimetic effects. Although studies indicate that pemoline may act in animals through dopaminergic mechanisms, the exact mechanism and site of action of the drug in man is not known.
Pharmacodynamics
Pemoline belongs to the group of medicines called central nervous system (CNS) stimulants. It is used to treat attention deficit hyperactivity disorder (ADHD). Pemoline stimulates the brain, probably by affecting neurotransmitters, the chemicals in the brain that nerves use to communicate with each other.
Pharmacokinetics
Half-life
The serum half-life of pemoline is approximately 12 hours.
Following a single oral dose in healthy adults, the plasma or serum half-life of pemoline has ranged from about 9-14 hr. Following a single oral dose in children, the plasma elimination half-life exhibits considerable interindividual variation, ranging from about 2-12 hr (mean: 8.6 hr). Preliminary evidence suggests that the drug may exhibit nonlinar kinetics in children following multiple dosing, with the elimination half-life increasing substantially. ...
Absorption
Pemoline is rapidly absorbed from the gastrointestinal tract
Pemoline is excreted primarily by the kidneys with approximately 50% excreted unchanged and only minor fractions present as metabolites.
Pemoline is rapidly absorbed from the gastrointestinal tract. Approximately 50% is bound to plasma proteins. The serum half-life of pemoline is approximately 12 hours. Peak serum levels of the drug occur within 2 to 4 hours after ingestion of a single dose. Multiple dose studies in adults at several dose levels indicate that steady state is reached in approximately 2 to 3 days. In animals given radiolabeled pemoline, the drug was widely and uniformly distributed throughout the tissues, including the brain.
... Pemoline and its metabolites are excreted primarily in urine; only negligible amounts are excreted in feces. About 75% of an oral dose is excreted in urine within 24 hr; about 43% is excreted unchanged and about 22% is excreted as pemoline conjugates.
Pemoline is absorbed from the GI tract, and peak serum concentrations are achieved within 2-4 hours. Multiple-dose studies in adults indicate that serum concentrations plateau in about 3 days. In a study involving adults, the CNS stimulant effect of a single oral dose of pemoline was relatively long, reaching its peak within 4 hr and lasting at least 8 hr. However, when pemoline is administered to children in the treatment of attention deficit disorder, the drug has a gradual onset of action and therapeutic effects may not be apparent until 2 or 3 weeks of therapy.
Metabolism
Hepatic
Pemoline is metabolized by the liver. Metabolites of pemoline include pemoline conjugate, pemoline dione, mandelic acid, and unidentified polar compounds. Cylert is excreted primarily by the kidneys with approximately 50% excreted unchanged and only minor fractions present as metabolites.
Protein binding
Approximately 50% (bound to plasma proteins).
Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.