CYLERT®
(pemoline)
CS-IV
CYLERT SHOULD NOT BE USED BY PATIENTS UNTIL THERE HAS BEEN A COMPLETE DISCUSSION OF THE RISKS AND BENEFITS OF CYLERT THERAPY AND WRITTEN INFORMED CONSENT HAS BEEN OBTAINED (SEE PATIENT INFORMATION/CONSENT FORM). A SUPPLY OF PATIENT INFORMATION/ CONSENT FORMS AS PRINTED AT THE END OF THIS INSERT IS AVAILABLE, FREE OF CHARGE, BY CALLING (847) 937-7302. PERMISSION TO USE THE PATIENT INFORMATION/CONSENT FORM BY PHOTOCOPY REPRODUCTION IS HEREBY GRANTED BY ABBOTT LABORATORIES.
DESCRIPTION
CYLERT (pemoline) is a central nervous system stimulant. Pemoline is structurally dissimilar to the amphetamines and methylphenidate.
It is an oxazolidine compound and is chemically identified as 2-amino-5-phenyl-2-oxazolin-4-one. Pemoline has the following structural formula:
Pemoline is a white, tasteless, odorless powder, relatively insoluble (less than 1 mg/mL) in water, chloroform, ether, acetone, and benzene; its solubility in 95% ethyl alcohol is 2.2 mg/mL.
CYLERT (pemoline) is supplied as tablets containing 18.75 mg, 37.5 mg or 75 mg of pemoline for oral administration. CYLERT is also available as chewable tablets containing 37.5 mg of pemoline.
Inactive Ingredients
18.75 mg tablet: corn starch, gelatin, lactose, magnesium hydroxide, polyethylene glycol and talc.
37.5 mg tablet: corn starch, FD&C Yellow No. 6, gelatin, lactose, magnesium hydroxide, polyethylene glycol and talc.
37.5 mg chewable tablet: corn starch, FD&C Yellow No. 6, magnesium hydroxide, magnesium stearate, mannitol, polyethylene glycol, povidone, talc and artificial flavor.
75 mg tablet: corn starch, gelatin, iron oxide, lactose, magnesium hydroxide, polyethylene glycol and talc.
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CLINICAL PHARMACOLOGY
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.
There is neither specific evidence which clearly establishes the mechanism whereby CYLERT produces its mental and behavioral effects in children, nor conclusive evidence regarding how these effects relate to the condition of the central nervous system.
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 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.
CYLERT (pemoline) has a gradual onset of action. Using the recommended schedule of dosage titration, significant clinical benefit may not be evident until the third or fourth week of drug administration.
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