The P-I-E-N-O Parkinsn's List Drug Database
pemoline / CylertTM
STIMULANT /
Anti ADD
Description: Pemoline is an oral central nervous system stimulant. This agent possesses pharmacologic actions that are similar to those of the amphetamines and methylphenidate; however, its sympathomimetic effects are minimal. Because of its long half-life, pemoline can be dosed once a day. Pemoline is indicated for use in attention-deficit hyperactivity disorder(ADHD). Pemoline was approved by the FDA in January 1975. It is classified as a schedule IV controlled substance.
Mechanism of Action: Pemoline exhibits pharmacological activity similar to that of the amphetamines and methylphenidate. The mechanisms by which pemoline alters mental and behavioral effects in children are not known. Animal studies suggest that the stimulatory effect is mediated through central dopaminergic mechanisms, possibly by blocking the reuptake mechanism present in dopaminergic neurons. The primary sites of activity appear to be in the cerebral cortex and the subcortical structures. Pemoline has weak sympathomimetic activity, with minor activity in the periphery. Pemoline can produce a decreased sense of fatigue, an increase in motor activity and mental alertness, mild euphoria, and brighter spirits. Pemoline also possesses some anorexigenic properties.
Pharmacokinetics: Pemoline is administered orally. Peak serum concentrations are achieved in 2-4 hours. The CNS-stimulant effects in adults are typically seen after 4 hours, with a duration of action of at least 8 hours. Following administration to children, however, therapeutic effects may not be observed for at least 2-3 weeks. The distribution of this drug is unknown. Plasma protein binding is not clinically significant.
At least 50% of a single dose is metabolized through hepatic and other pathways to pemoline dione, pemoline glucuronide, mandelic acid, and other unknown metabolites. Pemoline dione exhibits CNS stimulatory action that is less potent than the parent compound. The half-life of pemoline in adults is 9-14 hours; the half-life in children ranges from 2-12 hours. It has been suggested that pemoline exhibits nonlinear kinetics with multiple dosing in children, which would produce a significant prolongation of halflife. Approximately 75% of a dose is excreted renally over 24 hours, with 43% appearing as unchanged pemoline and the remainder as metabolites.
CONTRAINDICATIONS/PRECAUTIONS: Pemoline has caused hepatic disease including hepatitis, jaundice, and elevated liver enzymes. Fatalities have occurred, although a causal relationship to pemoline has not been established. Therefore, this drug is contraindicated in patients with hepatic disease. Liver-function tests should be performed before therapy and periodically during therapy with pemoline. If elevations in liver-function tests occur, the drug should be discontinued.
Pemoline should be used with caution in patients withTourette's syndrome or other motor tics disorders because attacks can be precipitated.
Caution should be exercised when administering pemoline to children with psychosis because behavior disturbance and thought disorders can be exacerbated.
Pemoline should be used with caution in patients with renal impairment because elimination of the drug can be altered.
Physical or psychological drug dependence could occur with pemoline in patients with a history of substance abuse because this phenomenon has occurred with similar psychostimulants.
DRUG INTERACTIONS: A reduction in seizure threshold has been reported following concomitant administration of pemoline with anticonvulsant agents. Dosage adjustments of anticonvulsants may be necessary during simultaneous use of these drugs.
The CNS stimulatory actions of pemoline can be potentiated by concurrent administration of this agent with other sympathomimetics. Patients receiving combination therapy should be closely observed for signs of nervousness, irritability, insomnia, convulsions, or arrhythmias.
ADVERSE REACTIONS: Pemoline has caused hepatic dysfunction including hepatitis, jaundice, and elevated hepatic enzymes (SGOT, SGPT, and serum LDH). Alterations in LFTs are usually observed after several months of treatment. Fatalities have occurred, although a causal relationship to pemoline has not been established. Patients with alterations in liver-function tests usually remain asymptomatic; however, liver-function tests should be performed before therapy and periodically during therapy with pemoline. Restoration to baseline levels usually occurs following discontinuation of the drug. If elevations in liver-function tests occur, pemoline should be discontinued.
The most frequently reported adverse reaction to pemoline is insomnia. This effect usually occurs during the period of initial treatment. Dosage reduction can eliminate or lessen the severity of this side effect. Other mild CNS reactions include headache, dizziness, mild mental depression, irritability, and drowsiness. More severe effects include extrapyramidal symptoms, such as dystonia, akathisia, and parkinsonism; precipitation of attacks of Tourette's syndrome; oculogyric crisis; seizures; and hallucinations.
Gastrointestinal effects include anorexia with weight loss, which is commonly seen during the initial stages of treatment. Weight gain usually resumes within 3-6 months with continued therapy. Nausea/vomiting and diarrhea also have been reported.
Growth inhibition has been observed in some children following long-term therapy with stimulants. Children requiring prolonged treatment with pemoline should be carefully monitored.
PATIENT INFORMATION:
What do pemoline tablets or chewable tablets do?
Pemoline (CylertTM ) is a stimulant that can increase or stimulate some aspect of brain activity. Pemoline helps improve attention in children who cannot concentrate or who are easily distracted. It helps to reduce restless or overactive behaviors. Federal law prohibits the transfer of pemoline to any person other than the patient for whom it was prescribed. Do not share this medicine with anyone else. Generic pemoline tablets and chewable tablets are not yet available.
What should my doctor, dentist, or pharmacist know before I take pemoline?
They need to know if you have any of these conditions:
How should I take this medicine?
Take pemoline tablets by mouth. Follow the directions on the prescription label. You can chew the chewable tablets or swallow them whole. Swallow the tablets with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed.
Special precautions for use in children:
This medicine is not for children under 6 years old.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
What other medicines can interact with pemoline?
Tell your doctor or pharmacist: about all other medicines you are taking, including non-prescription medicines; if you are a frequent user of drinks with caffeine or alcohol; if you smoke; or if you use illegal drugs. These may affect the way your medicine works. Check before stopping or starting any of your medicines.
What side effects may I notice from taking pemoline?
Serious side effects with pemoline include:
Call your doctor as soon as you can if you get any of these side effects.
Minor side effects with pemoline include:
Let your doctor know about these side effects if they do not go away or if they annoy you.
What do I need to watch for while I take pemoline?
The use of pemoline needs careful supervision. Visit your doctor for regular checks on your progress. It may be the third or fourth week after you start therapy before you see the full effect of pemoline. Your doctor may want you to stop taking pemoline after a while to see if there is still a need for you to take it. Do not stop taking except on your doctor's advice. Tell your doctor if you feel a need to take more tablets than prescribed, or to take them more often.
Pemoline may affect your concentration, hide signs of tiredness, or make you feel drowsy or dizzy. Until you know how pemoline affects you, do not drive, ride a bicycle, use machinery, or do anything that needs mental alertness.
Pemoline can interfere with your normal sleep pattern. Take your daily dose in the morning to prevent trouble sleeping at night.
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature below 30C (86F). Keep container tightly closed. Throw away any unused medicine after the expiration date.
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