Attention Deficit Hyperactivity Disorder (ADHD) ADHD treatments for hyperactive children
Ritalin and other medications or pharmaceutical drugs used for ADHD

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Pharmaceutical Treatments for ADHD - Medications for Attention-Deficit/Hyperactivity Disorder


Overview:

Psychostimulants constitute the major pharmacological treatment of ADHD. Theoretically, these stimulants cause more blood flow to areas of the frontal lobe that are important for attention.

Many clinicians treating ADHD believe that greater harm--emotionally and socially--occurs to untreated ADHD patients than could possibly come from the side effects of the medications. Not everyone agrees, however, and many parents are concerned about the side effects of medications. Nor does medication work for every child. Nevertheless, the usefulness of psychostimulants in the treatment of ADHD has been established and is the standard of care in mainstream medicine.

There are many styles for the use of medication in ADHD. Some clinicians increase the medicine's dose until the desired effect is achieved or too many undesirable side effects, such as jitteriness, stomach aches or headaches occur and do not subside after several weeks. Some clinicians use other medications to treat the side effects of the psychostimulants, an approach that becomes even more problematic for parents already concerned about the consequences or long-term effects of medication use. For example, Zantac or Pepto-Bismo can be used to help patients who experience stomach ache from using psychostimulants.

If psychostimulants are not effective or sufficiently effective, the second line therapy consists of anti-depressants, such as imipramine, desipramine, nortriptyline, bupropion, or venlafaxine. Clonidine is a third-line medication. Another approach when none of these three classes of medications work, is to combine classes and give multiple drugs.

If the first psychostimulant medication does not help, Thomas Phelan, Ph.D., suggests that all patients try a second or even a third stimulant. Individuals may respond quite differently to each one. For instance, he might start with Ritalin, noting the best result the patient achieves and at what dose. He then has the patient try dexedrine or Adderall or Cylert , again observing the best result at what dose. After this, he and the patient jointly decide which medicine at what dose is best for long-term usage. He believes that patients may be "treated" for ADHD, but without comparisons among medications, the patients will not know which one works best.

Dr. Phelan emphasizes that patients need a clinician who is aware of what changes medicines can bring about in a patient's ability to function and who knows that ADHD is not a disorder in which one medicine or one dosing schedule suits all. Patients need to watch for changes in functioning when on medicine. Sometimes another person in the patient's life needs to note these changes.

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First-line therapy: Psychostimulants:

Psychostimulants are controlled substances that calm persons with ADHD rather than stimulate them. While we know that ADHD affected persons have neurochemical correlates these have not been accurately determined. However, it has been asserted that the dopamine and norepinephrine circuits are affected in ADHD.

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  • Methylphenidate HCL (Ritalin) and sustained-release preparations (Ritalin-SR, Concerta, Metadate CD):
Ritalin is said to affect as much as a 70% improvement in those affected with ADHD. Ritalin is supposed to induce hyperperfusion [increase blood supply] to the frontal lobes of the brain. Of all the ADHD medications, Ritalin is the most inconsistently absorbed. Some adults and children absorb as much as 80-90% of the medication, whereas others only absorb 30-40% of a medication dose.

Methylphenidate is derived from the same family as cocaine and increases blood flow to the basal ganglia and decreases flow to frontal and motoric regions. The basal ganglia are involved in the control of movement. Parkinson's disease, for example, is caused by a degeneration of certain neurons located in the mid-brain that send axons to parts of the basal ganglia. Cerebral studies in persons with ADHD have shown cerebral hypoperfusion in the frontal lobe and decreased blood flow to the caudate nucleus. The amygdala, considered by some anatomists to be part of the basal ganglia, is located within the temporal lobe near its rostral tip. The side effects of Methylphenidate include facial tics and a delay in the onset of action.

Some important facts to remember about Ritalin & Methylphenidate:
  1. Its onset of action is rapid: 20-30 minutes.
  2. It has the shortest duration of action of 2-4 hours. Many children only benefit for 3 hours from medication.
  3. There may be a significant "rebound" when the medication wears off, constituted by over-agitation and/or anxiety.

Summary Drug Monograph:


(Provided courtesy of and copyright by: RxList - The Internet Drug Index)

Clinical Pharmacology:

The mode of action of Methylphenidate hydrochloride in man is not completely understood, but methylphenidate presumably activates the brain stem arousal system and cortex to produce its stimulant effect.

There is neither specific evidence which clearly establishes the mechanism whereby methylphenidate produces its mental and behavioral effects in children, nor conclusive evidence regarding how these effects relate to the condition of the central nervous system.

Methylphenidate hydrochloride in extended-release tablets is more slowly but as extensively absorbed as in the regular tablets. Bioavailability of the MD Pharmaceutical Inc. methylphenidate hydrochloride extended-release tablet was compared to a sustained release reference product and an immediate-release product. The extent of absorption for the three products was similar, and the rate of absorption of the two sustained-release products was not statistically different.

Dosage and Aministration:

Children (6 years and over):

Methylphenidate hydrochloride should be initiated in small doses, with gradual weekly increments. Daily dosage above 60 mg is not recommended.

If improvement is not observed after appropriate dosage adjustment over a one-month period, the drug should be discontinued.

Tablets: Start with 5 mg twice daily (before breakfast and lunch) with gradual increments of 5 to 10 mg weekly.

Extended-Release Tablets: Methylphenidale hydrochloride extended-release tablets have a duration of action of approximately 8 hours. Therefore, the extended-release tablets may be used in place of the immediate-release tablets when the 8-hour dosage of methylphenidate hydrochloride extended-release tablets corresponds to the titrated 8-hour dosage of the immediate-release tablets. Methylphenidate hydrochloride extended-release tablets must be swallowed whole and never crushed or chewed.

If paradoxical aggravation of symptoms or other adverse effects occur, reduce dosage, or, if necessary, discontinue the drug.

Methylphenidate should be periodically discontinued to assess the child's condition. Improvement may be sustained when the drug is either temporarily or permanently discontinued.

Drug treatment should not and need not be indefinite and usually may be discontinued after puberty.

Warnings:

Methylphenidate should not be used in children under six years, since safety and efficacy in this age group have not been established.

Sufficient data on safety and efficacy of long-term use of methylphenidate hydrochloride in children are not yet available. Although a causal relationship has not been established, suppression of growth ( i.e., weight gain, and/or height) has been reported with the long-term use of stimulants in children. Therefore, patients requiring long-term therapy should be carefully monitored. Methylphenidate should not be used for severe depression of either exogenous or endogenous origin. Clinical experience suggests that in psychotic children, administration of methylphenidate may exacerbate symptoms of behavior disturbance and thought disorder.

Methylphenidals should not be used for the prevention or treatment of normal fatigue states. There is some clinical evidence that methylphenidate may lower the convulsive threshold in patients with prior history of seizures, with prior EEG abnormalities in absence of seizures, a.d. very rarely, in absence of history of seizures and no prior EEG evidence of seizures. Safe concomitant use of anticonvulsants and methylphenidate has not been established. In the presence of seizures, the drug should be discontinued. Use cautiously in patients with hypertension. Blood pressure should be monitored at appropriate intervals in all patients taking methylphenidate, especially those with hypertension.

Symptoms of visual disturbances have been encountered in rare cases. Difficulties with accommodation and blurring of vision have been reported.

Drug Interactions:

Methylphenidate may decrease the hypotensive effect of guanethidine. Use cautiously with pressor agents and MAO inhibitors. Human pharmacologic studies have shown that methylphenidate may inhibit the metabolism of coumarin anticoagulants, anticonvulsants (phenobarbital, phenytoin, primidone), phenylbutazone, and tricyclic anti-depressants (imipramine, clomipramnine, desipramine). Downward dosage adjustments of these drugs may be required when given concomitantly with methylphenidate.

Precautions:

Patients with an element of agitation may react adversely; discontinue therapy if necessary. Periodic C.C. differential, and platelet counts are advised during prolonged therapy.

Drug treatment is not indicated in all cases of this behavioral syndrome and should be considered only in light of the complete history and evaluation of the child. The decision to prescribe methylphenidate should depend on the physician's assessment of the chronicity and severity of the child's symptoms and their appropriateness for his/her age. Prescription should not depend solely on the presence of one or more of the behavioral characteristics.

When these symptoms are associated with acute stress reactions, treatment with methylphenidate is usually not indicated.

Long-term effects of methylphenidate in children have not been well established.

Adverse Reactions:

Nervousness and insomnia are the most common adverse reactions but are usually controlled by reducing dosage and omitting the drug in the afternoon or evening.

Other reactions indude hypersensitivity (including skin rash, urticaria, fever, arthralgia, exfoliative dermatitis, erythema multiforme with histopathological findings of necrotizing vasculitis, and thrombocytopenic purpura); anorexia; nausea; dizziness; palpitations; headache; dyskinesia; drowsiness; blood pressure and pulse changes, both up and down; tachycardia; angina; cardiac arrhythmia; abdominal pain; weight loss during prolonged therapy. There have been rare reports of Tourette's syndrome.

Toxic psychosis has been reported. Although a definite causal relationship has not been established, the following have been reported in patients taking this drug: instances of abnormal liver function, ranging from transaminase elevation to hepatic coma; isolated cases of cerebral arteritis and/or occlusion; leukopenia and/or anemia; transient depressed mood; a few instances of scalp hair loss.

In children, loss of appetite, abdominal pain, weight loss during prolonged therapy,insomnia, and tachycardia may occur more frequently; however, any of the other adverse reactions listed above may also occur.

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  • Adderall:
Adderall is made by Richwood Pharmaceuticals, and was previously known as 'Obetral'. The dosage of Adderall is roughly equivalent to a comparable dose of Dexedrine. Adderall tablets consist of equal amounts of Amphetamine and Dextroamphetamine, with both short and long-acting preparations. The therapeutic effect is apparently more subtle and smooth than other preparations and the length of action is 6-9 hours.

Important points to note when prescribing or taking Adderall:
  1. It provides therapeutic cover for a full school or working day.
  2. Adderall has been used for 'impulse-control.'
  3. Adderall has a distinct anorexic effect and therefore management of diet, especially in children, is essential.
  4. Because Adderall has a slow onset of action and a sloped drop-off of action, anxiety induced at the onset of action and rebound at drop-off is reduced over other stimulants

Summary Drug Monograph:


(Provided courtesy of and copyright by: RxList - The Internet Drug Index)

Clinical Pharmacology:

Amphetamines are non-catecholamine sympathomimetic amines with CNS stimulant activity. Peripheral actions include elevation of systolic and diastolic blood pressures and weak bronchodilator and respiratory stimulant action.

There is neither specific evidence which clearly establishes the mechanism whereby amphetamine produces mental and behavioral effects in children, nor conclusive evidence regarding how these effects relate to the condition of the central nervous system.

Dosage and Aministration:

Regard less of indication, amphetamines should be administered at the lowest effective dosage and dosage should be individually adjusted. Late evening doses should be avoided because of the resulting insomnia.

Attention Deficit Disorder with Hyperactivity; Not recommended for children under 3 years of age. In children from 3 to 5 years of age, start with 2.5 mg daily; daily dosage may be raised in increments of 2.5 mg at weekly intervals until oplimal response is obtained.

In children 6 years of age and older, start with 5 mg once or twice daily; daily dosage may be raised in increments of 5 mg at weekly intervals until optimal response is obtained. Only in rare cases will it be necessary to exceed a total of 40 mg per day. Give first dose on awakening; additional doses (1 or 2) at intervals of 4 to 6 hours

Where possible, drug administration should be interrupted occasionally to determine if there is a recurrence of behavioral symptoms sufficient to require continued therapy.

Warnings:

Clinical experience suggests that in psychotic children, administration of amphetamine may exacerbate symptoms of behavior disturbance and thought disorder. Data are inadequate to determine whether chronic administration of amphetamine may be associated with growth inhibition; therefore, growth should be monitored during treatment.

Drug Interactions:

Acidifying agents - Gastrointestinal acidifying agents (guanethidine,reserpine, glutamic acid HCl,ascorbic acid, fruit juices, etc.) lower absorption of amphetamines.

Urinary acidifying agents -(ammonium chloride, sodium acid phosphate, etc.) Increase the concentration of the ionized species of the amphetamine.

Primary excretion - Both Groups of agents lower blood levels and efficacy of amphetamines.

Adrenergic blockers - Adrenergic blockers are inhibited by amphetamines.

Alkalinizing agents -Gastrointestinal alkalinizing agents (sodium bicarbonate, etc.)increase absorption of amphetamines. Urinary alkalinizing agents (acetazolamide, some thiazides) increase the concentration of the non-ionized species of the amphetamine molecule, thereby decreasing urinary excretion. Both groups of agents increase blood levels and therefore potentate the actions of amphetamines.

Antidepressants, tricyclic - Amphetamines may enhance the activity of tricyclic or sympathomimetic agents; d-amphetamine with desipramine or protriptyline and possibly other tricyclics cause striking and sustained increases in the concentration of d-amphetamine in the brain; cardiovascular effects can be potentiated.

MAO inhibitors - M.O. antidepressants, as well as a metabolite of furazolidone, slow amphetamine metabolism. This slowing potentiates amphetamines, increasing their effect on the release of norepinephrine and other monoamines from adrenergic nerve endings, this can cause headaches and other signs of hypertensive crisis. A variety of neurological toxic effects and malignant hyperpyrexia can occur, sometimes with fatal results.

Antihistamines - Amphetamines may counteract the sedative effect of antihistamines.

Antihypertensives - Amphetamines may antagonize the hypotensive effects of antihypertensives.

Chlorpromazine - Chlorpromazine blocks dopamine and norepinephrine receptors, thus inhibiting the central stimulant effects of amphetamines, and can be used to treat amphetamine poisoning.

Ethosuximide - Amphetamines may delay intestinal absorption of ethosuximide.

Haloperidol - Haloperidol blocks dopamine receptors, thus inhibiting the central stimulant effects of amphetamines.

Lithium carbonate - The anorectic and stimulatory effects of amphetamines may be inhibited by lithium carbonate.

Meperidine - Amphetamines pone the analgesic effect of meperidine.

Methenamine therapy - Urinary excretion of amphetamines is increased, and efficacy is reduced, by acidifying agents used in methenamine therapy.

Norepinephrine - Amphetamines enhance the adrenergic effect of norepinephrine.

Phenobarbital - Amphetamines may delay intestinal absorption of phenobarbital; co-administration of phenobarbital may produce a synergistic anticonvulsant action.

Phenytoin - Amphetamines may delay intestinal absorption of phenytoin; co-administration of phenytoin may produce a synergistic anticonvulsant action.

Propoxyphene - In cases of propoxyphene overdose, amphetamine CNS stimulation is potentiated and fatal convulsions can occur.

Veratrum alkaloids - Amphetamines inhibit the hypotensive effect of veratrum alkaloids.

Precautions:

Caution is to be exercised in prescribing amphetamines for patients with even mild hypertension.

The least amount feasible should be prescribed or dispensed at one time in order to minimize the possibility of over dosage.

Amphetamines may impair the ability of the patient to engage in potentially hazardous activities s.c. as operating machinery or vehicles; the patient should therefore be cautioned accordingly.

Adverse Reactions:

Cardiovascular: Palpitations, tachycardia, elevation of blood pressure There have been isolated reports of cardiomyopathy associated with chronic amphetamine use.

Central Nervous System: Psychotic episodes at recommended doses (rare), overstimulation, restlessness. dizziness, insomnia, euphoria. dyskinesia, dysphoria, tremor, headache, exacerbation of motor and phonictics and Tourette's syndrome.

Gastrointestinal: Dryness of the mouth, unpleasant taste, diarrhea, constipation, other gastrointestinal disturbances. Anorexia and weight loss may occur as undesirable effects when amphetamines are used for other than the anorectic effect.

Allergic: Urticaria.

Endocrine: Impotence. Changes in libido.

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  • Dextroamphetamine saccharate/Dextroamphetamine sulfate (Dexedrine):

Dexedrine is one of the better known stimulant medications and is second only to Ritalin in the treatment of ADHD. The generic equivalent of Dexedrine is Dextroamphetamine Sulfate. Because the PDR continues to list Dexedrine under "Diet Control" medications, some insurance companies will not cover Dexedrine for the treatment of ADHD.

Important things to bear in mind when prescribing or taking Dexedrine:
  1. The onset of action is 30 minutes, slower than Ritalin.
  2. The coverage provided by Dexedrine is 3 1/2 to 4 1/2 hours; about an hour longer than Ritalin, especially with adult administration.
  3. Dexedrine purportedly has a "smoother" onset of action and "drop-off" than Ritalin. It is usually almost completely absorbed and therefore one does not usually see the variation in onset of action that one sees with the use of Ritalin.
  4. Dexedrine 5mg is about equivalent to 10mg of Ritalin. In other words it is about twice as potent as Ritalin.
  5. Ingestion of Vitamin C and Dexedrine simultaneously, e.g., taking medication with orange juice, may significantly reduce Dexedrine absorption.
  6. Because Dexedrine in the SR form is long acting, it is very useful for Middle and High school students who forget to take their second or third dose. Dexedrine, however, has the potential side effect of reduced appetite.

Summary Drug Monograph:


(Provided courtesy of and copyright by: RxList - The Internet Drug Index)

Clinical Pharmacology:

Amphetamines are non-catecholamine, sympathomimetic amines with CNS stimulant activity. Peripheral actions include elevations of systolic and diastolic blood pressures and weak bronchodilator and respiratory stimulant action.

There is neither specific evidence which clearly establishes the mechanism whereby amphetamines produce mental and behavioral effects in children, nor conclusive evidence regarding how these effects relate to the condition of the central nervous system.

Dexedrine (dextroamphetamine sulfate) Spansule capsules are formulated to release the active drug substance in vivo in a more gradual fashion than the standard formulation, as demonstrated by blood levels. The formulation has not been shown superior in effectiveness over the same dosage of the standard, noncontrolled-release formulations given in divided doses.

Dosage and Aministration:

Attention Deficit Disorder with Hyperactivity :

Not recommended for pediatric patients under 3 years of age.

In pediatric patients from 3 to 5 years of age, start with 2.5 mg daily, by tablet daily dosage may be raised in increments of 2.5 mg at weekly intervals until optimal response is obtained.

In pediatric patients 6 years of age and older, start with 5 mg once or twice daily, daily dosage may be raised in increments of 5 mg at weekly intervals until optimal response is obtained. Only in rare cases will it be necessary to exceed a total of 40 mg per day.

Spansule capsules may be used for once-a-day dosage wherever appropriate. With tablets, give first dose on awakening additional doses (1 or 2) at intervals of 4 to 6 hours.

Where possible drug administration should be interrupted occasionally to determine if there is a recurrence of behavioral symptoms sufficient to require continued therapy.

Warnings:

Amphetamines have a high potential for abuse. Admimistration of Amphetamines for prolonged periods of time may lead to drug dependence and should be avoided. Particular attention should be paid to patients obtaining Amphetamines for nontherapeutic use or distribution to others.

Contraindications:

Advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension, hyperthyroidism, known hypersensitivity or idiosyncrasy to the sympathomimetic amines, glaucoma.

Agitated states.

Patients with a history of drug abuse.

During or within 14 days following the administration of monoamine oxidase inhibitors (hypertensive crises may result).

Drug Interactions:

Acidifying Agents: Gastrointestinal acidifying agents (guanethidine, reserpine, glutamic acid HCl, ascorbic acid, fruit juices, etc.) lower absorption of amphetamines, Urinary acidifying agents (ammonium chloride, sodium acid phosphate, etc.) increase the concentration of the ionized species of the amphetamine molecule, thereby increasing urinary excretion. Both groups of agents lower blood levels and efficacy of amphetamines.

Adrenergic Blockers: Adrenergic blockers are inhibited by amphetamines.

Alkalinizing Agents: Gastrointestinal alkalinizing agents (sodium bicarbonate, etc.) increase absorption of amphetamines. Urinary alkalinizing agents (acetazolamide, some thiazides) increase the concentration of the non-ionized species of the amphetamine molecule, thereby decreasing urinary excretion. Both groups by agents increase blood levels and therefore potentiate the action of amphetamines.

Antidepressants tricyclic: Amphetamines may enhance the activity of tricyclic or sympathometic agents; d-amphetamine with desipramine or protriptyline and possibly other tricyclics cause striking and sustained increases in the concentration of d-amphetamine in the brain; cardiovascular effects can be potentiated.

MAO Inhibitors: MAOI antidepressants, as well as a metabolite of furazolidone, slow amphetamine metabolism. This slowing potentiates amphetamines, increasing their effect on the release of norepinephrine and other monoamines from adrenergic nerve endings; this can cause headaches and other signs of hypertensive crisis. A variety of neurological toxic effects and malignant hyperpyrexia can occur, sometimes with fatal results.

Antihistamines:Amphetamines may counteract the sedative effect of antihistamines.

Antihypertensives: Amphetamines may antagonize the hypotensive effects of antihypertensives.

Chlorpromazine: Chlorpromazine blocks dopamine and norepinephrine reuptake, thus inhibiting the central stimulant effects of amphetamines, and can be used to treat amphetamine poisoning.

Ethosuximide: Amphetamines may delay intestinal absorption of ethosuximide.

Haloperidol: Haloperidol blocks dopamine and norepinephrins reuptake, thus inhibiting the central stimulant effects of amphetamines.

Lithium Carbonate: The stimulatory effects of amphetamines may be inhibited by lithium carbonate.

Meperidine: Amphetamines potentiate the analgesic effect of meperidine.

Methenamine Therapy: Urinary excretion of amphetamines is increased, and efficacy is reduced, by acidifying agents used in methenamine therapy.

Norepinephrine: Amphetamines enhance the adrenergic effect of norepinephrine.

Phenobarbital: Amphetamines may delay administration of phenobarbital and may produce an intestinal absorption of phenobarbital; coadministration of phenobarbital may produce a co-synergistic anticonvulsant action.

Phenytoin: Amphetamines may delay intestinal absorption of phenytoin; co-administration of phenytoin may produce a synergistic anticonvulsant action.

Propoxyphene: In cases of propoxyphene overdosage, amphetamine CNS stimulation is potentiated and fatal convulsions can occur.

Veratrum Alkaloids: Amphetamines inhibit the hypotensive effect of veratrum alkaloids.

Precautions:

Long-term effects of amphetamines in pediatric patients have not been well established.

Amphetamines are not recommended for use in pediatric patients under 3 years of age with Attention Deficit Disorder with Hyperactivity. Clinical experience suggests that in psychotic children, administration of amphetamines may exacerbate symptoms of behavior disturbance and thought disorder.

Amphetamines have been reported to exacerbate motor and phonic tics and Tourette's syndrome. Therefore, clinical evaluation for tics and Tourette's syndrome in children and their families should precede use of stimulant medications.

Data are inadequate to determine whether chronic administration of amphetamines may be associated with growth inhibition; therefore growth should be monitored during treatment.

Drug treatment is not indicated in all cases of Attention Deficit Disorder with Hyperactivity and should be considered only in light of the complete history and evaluation of the child. The decision to prescribe amphetamines should depend on the physician's assessment of the chronicity and severity of the child's symptoms and their appropriateness for his/her age. Prescription should not depend solely on the presence of one or more of the behavioral characteristics.

When these symptoms are associated with acute stress reactions treatment with amphetamines is usually not indicated.

Adverse Reactions:

Cardiovascular: Palpitations, tachycardia, elevation of blood pressure. There have been isolated reports of cardiomyopathy associated with chronic amphetamine use.

Central Nervous System: Psychotic episodes at recommended doses (rare), overstimulation, restlessness, dizziness, insomnia, euphoria, dyskinesia, dysphoria, tremor, headache, exacerbation of motor and phonic tics and Tourette's syndrome.

Gastrointestinal: Dryness of the mouth, unpleasant taste, diarrhea, constipation, other gastrointestinal disturbances. Anorexia and weight loss may occur as undesirable effects.

Allergic: Urticaria.

Endocrine: Impotence, changes in libido.

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  • Methamphetamine HCL (Desoxyn):

Desoxyn is rarely used in the treatment of ADHD. There is no generic available. Desoxyn is made by Abbott and the dosage is comparable to Dexedrine. However, Desoxyn is about 2-3 times more expensive than Dexedrine.

Important points to remember when prescribing or taking Desoxyn:
  1. Desoxyn is apparently effective for the Inattentive form of ADHD.
  2. Onset of action is 20-30 minutes, lasting 3 to 4 hours where the drop-off in effect is more similar to Dexedrine than Ritalin.
  3. Desoxyn is contraindicated in patients with glaucoma.

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  • Pemoline (Cylert) for ADHD:
Cylert ranks third in sales for the treatment of ADHD. Cylert is manufactured by Abbott; no generic is available.

Unlike other stimulant medications Cylert has an onset of action of about an hour and must be taken for 1-2 weeks before improvement occurs. It is recommended that the dosage of this medication be increased in increments of 18.75mg every 2-3 days over several weeks. Cylert is more expensive than Ritalin or Dexedrine.

Important points about Cylert:

  1. Liver enzyme changes have occasionally been noted on patients taking Cylert. Baseline liver enzymes are recommended with follow ups at 3-6 months.
  2. Persons using alcohol are at higher risk with this medication. Patients with either liver or kidney compromise should not take this medication.
  3. SSRI's affect the use of Cylert due to their effects on the liver P450 isoenzymes.
  4. Cylert is a useful alternative for patients with cardiovascular disease as it has no effect on this system.
  5. Cylert may cause insomnia, appetite suppression, and tics.

Summary Drug Monograph:


(Provided courtesy of and copyright by: RxList - The Internet Drug Index)

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% excretedunchanged 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.

Dosage and Aministration:

Cylert (pemoline) is administered as a single oral dose each morning. The recommended starting dose is 37.5 mg/day. This daily dose should be gradually increased by 18.75 mg at one week intervals until the desired clinical response is obtained. The effective daily dose for most patients will range from 56.25 to 75 mg. The maximum recommended daily dose of pemoline is 112.5 mg.

Clinical improvement with Cylert is gradual. Using the recommended schedule of dosage titration, significant benefit may not be evident until the third or fourth week of drug administration.

Where possible, drug administration should be interrupted occasionally to determine if there is a recurrence of behavioral symptoms sufficient to require continued therapy. ufficient to require continued therapy.

Warnings:

Because of its association with life threatening hepatic failure, Cylert should not ordinarily be considered as first line drug therapy for ADHD.

Since Cylerts's marketing in 1975, 13 cases of acute hepatic failure have been reported to the FDA. While the absolute number of reported cases is not large. the rate of reporting ranges from 4 to 17 times the rate expected in the general population. This estimate may be conservative because of under reporting and because the long latency between initiation of Cylert treatment and the occurrence of hepatic failure may limit recognition of the association. If only a portion of actual cases were recognized and reported, the risk could be substantially higher.

Of the 13 cases reported as of May 1996, 11 resulted in death or liver transplantation, usually within four weeks of the onset of signs and symptoms of liver failure. The ear-liest onset of hepatic abnormalities occurred six months after initiation of Cylert. Although some reports described dark urine and nonspecific prodromal symptoms (e.g., anorexia, malaise, and gastrointestinal symp-toms), in other reports it was not clear if any prodromal symptoms preceded the onset of jaundice. It is also not clear if the recom-mended baseline and periodic liver function testing are predictive of these instances of acute liver failure. Cylert should be dis-continued if clinically significant hepatic dysfunction is observed during its use.

Drug Interactions:

The interaction of Cylert (pemoline) with other drugs has not been studied in humans. Patients who are receiving Cylert concurrently with other drugs, especially drugs with CNS activity, should be monitored carefully.

Decreased seizure threshold has been reported in patients receiving Cylert concomitantly with antiepileptic medications.

Precautions:

Clinical experience suggests that in psychotic children administration of Cylert may exacerbate symptoms of behavior disturbance and thought disorder.

Cylert should be administered with caution to patients with significantly impaired renal function.

Since Cylert's market introduction. there have been reports of elevated liver enzymes associated with its use. Many of these patients had this increase detected several months after starting Cylert. Most patients were asymptomatic, with the increase in liver enzymes returning to normal after Cylert was discontinued. Liver function tests should be performed prior to and periodically during therapy with Cylert. Treatment with Ctlert should be initiated only in individual without liver disease and with normal baseline liver function tests.

The relationship, if any, between reversible elevations in liver function tests and the occurrence of life threatening hepatic failure in patients on long-term therapy with Cylert is not known. Liver function testing may not predict the onset of acute liver failure. Nonetheless, Cylert should be discontinued if clinically significant liver function test abnormalities are revealed at any time during therapy with this drug

Adverse Reactions:

The following are adverse reactions in decreasing order of severity within each category associated with Cylert:

Hepatic: There have been reports of hepatic dysfunction, ranging from asymptomatic reversible increases in liver enzymes to hepatitis, jaundice and life- threatening hepatic failure, in patients taking Cylert.

Hematopoietic: There have been isolated reports of aplastic anemia.

Central Nervous System: The following CNS effects have been reported with the use of Cylert: convulsive seizures: literature reports indicate that Cylert may precipitate attacks of Gilles de la Tourette syndrome; hallucinations; dyskinetic movements of the tongue, lips, face and extremities: abnorrnal oculomotor function including nystagmus and oculogyric crisis; mild depression; dizziness; increased irritability; headache; and drowsiness.

Insomnia is the most frequently reported side effect of Cylert, it usually occurs early in therapy prior to an optimum therapeutic response. In the majority of cases it is transient in nature or responds to a reduction in dosage.

Gastrointestinal: Anorexia and weight loss may occur during the first weeks of therapy. In the majority of cases it is transient in nature; weight gain usually resumes within three to six months.

Nausea and stomach ache have also been reported.

Miscellaneous: Suppression of growth has been reported with the long- term use of stimulants in children. Skin rash has been reported with Cylert.

Mild adverse reactions appearing early during the course of treatment with Cylert often remit with continuing therapy. If adverse reactions are of a significant or protracted nature, dosage should be reduced or the drug discontinued.

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Second-line Therapy - When Stimulants Cannot Be Used:

  • Antidepressant Medications and ADHD:

Anti-depressant medication is often prescribed for persons with ADHD who cannot tolerate or show no signs of improvement on stimulants, or for those who have mood sequealae. Dosage levels, while there are guidelines, are essentially determined on a case to case basis. Because ADHD persons are often poor self observers it may be helpful to enlist a person with whom the ADHD person is close in order to note any improvement or deterioration in behavior following medication changes.

It should be strongly emphasized that treatment of ADHD with anti-depressants does not necessarily imply that the patient is depressed. Antidepressants are often used to enhance the control of the patient's symptoms, rather than as treatment of primary depression.

Some clinician feel that the SSRI's have superior benefits, especially with children, for the mooded aspects of ADHD because they cause less side-effects than older generation anti-depressants such as the tricyclics (Imipramine, Nortriptyline, Amitryptyline, Desipramine). Desipramine has become less prescribed due to some unexplained sudden deaths which appeared to be related to heart conduction patterns.

Zoloft, Paxil, and Prozac, are the three most widely prescribed SSRI medications. Bupropion HCL (Wellbutrin) can also be a good second-line treatment. Links for drug monographs for antidepressant medications used for ADHD can be found at the end of this section.

In order to assess the effectiveness of medication any therapy it is important to ask whether an improvement has been noted in the following signs:

  • Inattentiveness and academic underachievement
  • Fidgeting and hyperactivity
  • Behavioral or verbal impulsivity (interrupting others, blurting out, acting before thinking)
  • Difficulty falling asleep at night
  • Trouble waking up (not getting out of bed) in the morning
  • Excessive irritability with-out cause and/or easy frustration
  • Bedwetting or primary nocturnal enuresis
  • Dyslexia with spatial or verbal reversals
  • Episodic explosiveness, emotional outbursts, or temper tantrums
  • Unexplained and persistent emotional negativity

If your medication does not help with any or all of these symptoms then either an increased dosage is required or a change, elimination or addition of a medication may be necessary.

Summary Drug Monographs -
Selected Antidepressant Medications Used for ADHD:


(Provided courtesy of and copyright by: RxList - The Internet Drug Index)

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  • The Use of Busiprone (BuSpar) in Treating ADHD:

Busiprone (BuSpar) is a relatively new anti-anxiety medication which shows some promise in treating ADHD when psychostimulant medications are not effective or their side effects cannot be tolerated. It can also "potentiate" benefits of the serotonergic antidepressants. The side-effects of Busoprone are often better tolerated than those of other medications used for ADHD. It should always be remembered, that for reasons still not fully understood, every individual responds differently and uniquely to a specific medication. The effective administration of a specific medication for any psycho-neurological condition will still - and most likely will for quite some time - remain an art, rather than a science.

For adults with ADHD, it has been noted that women with ADHD often report especially severe PMS, and their spouses and children may be very troubled by their exceptional irritability and impatience during this time of the month. Medications such as BuSpar are often extremely effective in relieving PMS symptoms.

RELATED STUDIES:

Transdermal Patch Formulation of Anti-Anxiety Medication Holds Promise For Treating Hyperactive Children

C. Keith Conners, Ph.D.,
Professor of Medical Psychology
Duke University Medical Center

Administration through a skin patch developed by Sano Corporation of a widely used anti-anxiety medication may provide a safe and effective treatment alternative for children with attention deficit hyperactivity disorder (ADHD), according to the results of a pilot study presented at a National Institute of Mental Health conference by Duke University researchers.

The drug buspirone (BuSpar) was administered to a group of 32 children with ADHD using a new transdermal (through the skin) delivery technology. The transdermal buspirone patch is not yet commercially available and will require completion of current trials as well as the necessary FDA review and approvals.

Following the eight-week, open-label study, 70-80% of patients treated were rated by parents and teachers as "much improved or very much improved," according to study-leader C. Keith Conners, Ph.D., Professor of Medical Psychology at Duke University Medical Center. "The treatment was well liked by parents and well tolerated by the patients in the study - important considerations in evaluating prospective therapies for ADHD," said Dr. Conners.

He noted that the results of transdermal buspirone evaluated in the phase II trial suggest that the therapy may offer several benefits for treatment of ADHD in children. Unlike oral medications that must be taken repeatedly at home and school, the transdermal patch is applied once each morning, relieving children and their caregivers of the daily responsibility and stigma of pill-taking.

Oral medications are frequently metabolized in the liver. In the drugs currently used to treat hyperactivity and attention deficit disorder this so-called "first-pass metabolism" releases active drug components erratically, creating fluctuations which increase the risk of inconsistent control of symptoms.

"The main difference is that oral drugs' side effects are associated with their peak level in thebloodstream, which is higher than their therapeutic level," Dr. Conners noted. "If you can reduce these peak levels, you can avoid a lot of adverse effects." He said that this may help account for the tolerability of the transdermal buspirone noted in the study.

The study looked at boys and girls aged 8-12 years who were physically healthy and had been diagnosed with ADHD. Two eight-child groups wore low- dose skin patches measuring either 2.5 cm2 or 5 cm2. Two high-dose groups of eight children began the treatment period with skin patches measuring 10 cm2 or 20 cm2. Patches were replaced daily. The high-dose skin patches were increased in size every 10 days.

According to Dr. Conners, the study demonstrated a relationship between dose and effect. That is, the two high-dose groups showed improvement in terms of clinical global impairment ratings by parents and teachers, while the low-dose groups showed less improvement. He characterized the side effect profile as mild and well tolerated.

The adverse effects reported were mild or moderate in severity and included insomnia (15.6%), reaction at the site of the patch (12.5%), headache (9.4%), and increased activity level (9.4%). There was one severe headache. The next steps in evaluating the therapy will be the analysis of placebo- controlled efficacy studies currently underway.

For a complete drug monograph of Busiprone HCL (BuSpar), please click here.

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  • Clonidine (Catapres), Another Alternative to Stimulants for Treating ADHD:

Clonidine (Catapres), another alternative to stimulants for treating ADHD, has been receiving widespread anectdotal support from parents with ADHD children, and is now considered a reasonable and increasingly popular pharmaecuetical treatment for ADHD. It seems to work best in decreasing hyperactivity, but does not always improve distractibility (as stimulants do). Some physicians have found benefits in using this medication with children who have ADHD and conduct problems.

Clonidine can be useful in alleviating the hyperactivity and fidgetiness of ADHD, without having any clear affect on the attentional part. It is often used in conjunction with methylphenidate, which helps the learning and attentiveness. Methylphenidate in higher doses, ie, those necessary to control the hyperactivity in some kids, will begin to have a negative effect on learning. Thus the combination, which enables specific treatment of attention with one drug and activity with another. Clonidine may be used with Group One or Two medications to increase their effectiveness.

Warnings: Only 10 children total have been studied in double blind placebo controlled clonidine trials. Possible sudden death may be related to clonidine/stimulant combination.

Robert Renichel and Charles Popper have a review, in the Journal of Child and Adolescent Psychopharmacology, of cases of sudden death in children taking the combination of clonidine and methylphenidate. This came in response to a July, 1995, National Public Radio news piece about three deaths in children being treated with the combination. Their conclusion was that none of the fatalities support the conclusion that the combination played any role in the children's deaths.

The most common presenting symptom of clonidine poisoning in children is lethargy. Other toxic effects include bradycardia; early transient hypertension followed by hypotension; respiratory depression and apnea; miosis; and hypothermia.

Among the 285 clonidine toxicity cases among children reported to the Kentucky poison center since 1990, 55% involved the child's own medication; 106 cases were the result of therapeutic error, usually a double dose. A common scenario was for one parent to dose their child and then the second parent to unknowingly give the child a second dose, he said. Ninety-nine children were 1-3 years old, the most common age range for accidental poisonings; 81 children were 7-10 years old, most of whom took their own medication in excess.

For a complete drug monograph of Clonidine HCL (Catapres), please click here.

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Other Medications For Selected Symptoms Of ADHD & Accompanying Disorders:

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Mood Stabilizers (for ADHD with Mood and Behavior Problems) :

Lithium, Carbemazepine (Tegretol), and Valproic Acid (Depakote) have been used when mood disorders co-exist with ADHD. One frequently sees bipolar patients with supposed comorbid ADHD or diagnosed solely with ADDH. This is becoming increasingly common in adults as well as kids thanks to the popularity of the ADHD diagnosis. The problem is that just about all bipolar patients have a disorder of attention. To differentiate between the two, it is sometimes helpful to look for symptoms that are seen in bipolar disorders but not usually in ADHD, for example:

  • racing thoughts
  • not needing to sleep or hypersomnia
  • changes in energy parallel to the above
  • tangential thinking
  • overspending, overcommitting
  • grandiosity
  • grandiose thrill seeking (eg, jumping off of high places)
  • psychosis.

When ADHD and Bipolar Disorder are comorbid, starting treatment with a stimulant in these patients will often exacerbate the hyperactivity, flatten affect, and greatly decrease appetite. Some doctors start instead with either clonidine or guanfacine plus one of the following mood stabilizers: lithium, carbamazepine, valproic acid, or lamotrigine.

Once the patient is stable on therapeutic doses, a stimulant can be added if ADHD symptoms remain; if necessary, an antidepressant is sometimes added as well.

The boundary between persistent hypomania and ADHD is unclear. The usual practice is to treat such cases with stimulants before puberty and with mood-stabilizing agents in adulthood.

Summary Drug Monographs -
Selected Medications Mentioned in this Section:


(Provided courtesy of and copyright by: RxList - The Internet Drug Index)

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Innovative Pharmacological Agents for Attention-Deficit/Hyperactivty Disorder:

 

  • Dimephosphonum:
Professor Vadim G. Malyshev, Head of the Department of Pathology, Ulyanovsk State University, Russia, is studying the biological properties of new phosphorous-containing drugs, synthesized at the Kazan State Institute of Organic and Physical Chemistry. He reports that one of these agents, Dimephosphonum, produces a normalizing effect on the functioning of the nervous system, mechanisms of blood circulation control, the tonicity of vessels, and on the acid-base state in acidosis of different aetiology and membrane functions of tissues.

When locally applied, he reports that dimephosphonum exhibits an antiseptic, antiphlogistic, and antiallergenic effect, increasing the protective barrier of the skin and the mucous membrane functions, thus contributing to the healing of wounds.

Dimephosphonum produced a normalizing effect on

  1. Brain functioning in stroke due to:

    1. Vertebral and carotid artery lesions (initial manifestations, transient ischemic attacks, ischemic and haemorrhagic insults, post insult complications, discirculatory encephalopathy, myelopathy and radiculopathy)

    2. Arterial hypertension

    3. Vasomotor dystonia


  2. In neurosurgical trauma in the course of cranial and spinal operations;

  3. In craniocerebral injuries (concussion and contusion of brain);

  4. In Meniere's syndrome and disease.

  5. In vegetative dysfunction.

Malyshev reports that dimephosphonum is more effective than sermionum and pyracetam in correction of cerebral vessel reactivity. For more information email him at cik@pop.ul.ru, or write him at 2-21 pr Sozidately, Ulyanovsk 432059, Russia. Telephone and fax numbers are 7 (8422) 217.992.

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Points About the Outcome of Any Therapy:

In monitoring treatments for ADHD, measurable improvements include attention span, concentration, memory, mood, task completion, motor coordination. Behaviors that may decrease include daydreaming, hyperactivity, immature behavior, anger, defiance, oppositional behavior, and impulsivity.

In order to assess the effectiveness of any therapy for ADHD it is important to ask whether an improvement has been noted in the following signs:

  • Inattentiveness and academic underachievement
  • Fidgeting and hyperactivity
  • Behavioral or verbal impulsivity (interrupting others, blurting out, acting before thinking)
  • Difficulty falling asleep at night
  • Trouble waking up (not getting out of bed) in the morning
  • Excessive irritability with-out cause and/or easy frustration
  • Bedwetting or primary nocturnal enuresis
  • Dyslexia with spatial or verbal reversals
  • Episodic explosiveness, emotional outbursts, or temper tantrums
  • Unexplained and persistent emotional negativity

If your medication does not help with any or all of these symptoms then either an increased dosage is required or a change, elimination or addition of a medication may be necessary.

For decades, medications have been used to treat the symptoms of ADHD (Attention Deficit Hyperactivity Disorder). For many people, these medicines dramatically reduce their hyperactivity and improve their ability to focus, work, and learn. The medications may also improve physical coordination, such as handwriting and ability in sports. Recent research by the National Institute of Mental Health (NIMH) suggests that these medicines may also help children with an accompanying conduct disorder to control their impulsive, destructive behaviors.

Unfortunately, when people see such immediate improvement, they often think medication is all that's needed. But these medicines don't cure the disorder, they only temporarily control the symptoms. Although the drugs help people pay better attention and complete their work, they can't increase knowledge or improve academic skills. The drugs alone can't help people feel better about themselves or cope with problems. These require other kinds of treatment and support.

For lasting improvement, numerous clinicians recommend that medications should be used along with treatments that aid in these other areas. There are no quick cures. Many experts believe that the most significant, long-lasting gains appear when medication is combined with behavioral therapy, emotional counseling, and practical support. Some studies suggest that the combination of medicine and therapy may be more effective than drugs alone. NIMH is conducting a large study to check this.

Use Of Stimulant Drugs

Stimulant drugs, such as Ritalin, Cylert, and Dexedrine, when used with medical supervision, are usually considered quite safe. Although they can be addictive to teenagers and adults if misused, these medications are not addictive in children.

Sometimes, a child's ADHD symptoms seem to worsen, leading parents to wonder why. They can be assured that a drug that helps rarely stops working. However, they should work with the doctor to check that the child is getting the right dosage. They also need to know that new or exaggerated behaviors may also crop up when a child is under stress. The challenges that all children face, like changing schools or entering puberty, may be even more stressful for a child with ADHD.

Some doctors recommend that children be taken off a medication now and then to see if the child still needs it. They recommend temporarily stopping the drug during school breaks and summer vacations, when focused attention and calm behavior are usually not as crucial. These "drug holidays" work well if the child can still participate at camp or other activities without medication.

Children on medications should have regular checkups. Parents should also talk regularly with the child's teachers and doctor about how the child is doing. This is especially important when a medication is first started, re-started, or when the dosage is changed.

The Medication Debate

As useful as these drugs are, Ritalin and the other stimulants have sparked a great deal of controversy. Most doctors feel the potential side effects should be carefully weighed against the benefits before prescribing the drugs. While on these medications, some children may lose weight, have less appetite, and temporarily grow more slowly. Others may have problems falling asleep. Some doctors believe that stimulants may also make the symptoms of Tourette's syndrome worse, although recent research suggests this may not be true. Other doctors say if they carefully watch the child's height, weight, and overall development, the benefits of medication far outweigh the potential side effects. Side effects that do occur can often be handled by reducing the dosage.

It's natural for parents to be concerned about whether taking a medicine is in their child's best interests. Parents need to be clear about the benefits and potential risks of using these drugs.

Another debate is whether Ritalin and other stimulant drugs are prescribed unnecessarily for too many children. Remember that many things, including anxiety, depression, allergies, seizures, or problems with the home or school environment can make children seem overactive, impulsive, or inattentive. Critics argue that many children who do not have a true attention disorder are medicated as a way to control their disruptive behaviors.

Medication & Self-Esteem

When a child's schoolwork and behavior improve soon after starting medication, the child, parents, and teachers tend to applaud the drug for causing the sudden change. But these changes are actually the child's own strengths and natural abilities coming out from behind a cloud. Giving credit to the medication can make the child feel incompetent. The medication only makes these changes possible. The child must supply the effort and ability. To help children feel good about themselves, parents and teachers need to praise the child, not the drug.

It's also important to help children and teenagers feel comfortable about a medication they must take every day. They may feel that because they take medicine they are different from their classmates or that there's something seriously wrong with them. Parents and teachers can help children view the medication in a positive way.

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