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Physician’s Resource The physician’s psychoactive medication resource guide 25% of your patients taking an antidepressant will have weight gain and the weight gain is directly caused by the antidepressant.
Ritalin (Methylphenidate) Ritalin Truth. What is Ritalin? What are the Ritalin side effects? How to taper off Ritalin. Ritalin,  the new street drug. Ritalin. Ritalin has become the street drug of choice with high school and  college students. Why Ritalin? Is Ritalin Really speed? Is Ritalin addictive? Does Ritalin enlarge  the heart?  Ritalin (Methylphenidate)   Warnings Precautions Adverse Effects Overdose CNS Stimulant The mode of action 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 CNS.  Methylphenidate is rapidly and extensively absorbed from the tablets following oral  administration; however, owing to extensive first-pass metabolism, bioavailability is low (approx.  30%) and large individual differences exist (11 to 52%).  In one study, the administration of methylphenidate with food accelerated absorption, but had no  effect on the amount absorbed.  Peak plasma concentrations of 10.8 and 7.8 ng/mL were observed, on average, 2 hours after  administration of 0.30 mg/kg in children and adults, respectively. However, peak plasma  concentrations showed marked variability between subjects. Both the area under the plasma  concentration curve (AUC), and the peak plasma concentrations (C(max)) showed dose-  proportionality. Methylphenidate is eliminated from the plasma with a mean half-life of 2.4 hours in children and  2.1 hours in adults. The apparent mean systemic clearance is 10.2 and 10.5 L/hr/kg in children  and adults, respectively for a 0.3 mg/kg dose. These data indicate that the pharmacokinetic  behavior of methylphenidate in hyperactive children is similar to that in normal adults. The  apparent distribution volume of methylphenidate in children was approximately 20 L/kg, with  substantial variability (11 to 33 L/kg).  Following oral administration of methylphenidate, 78 to 97% of the dose is excreted in the urine  and 1 to 3% in the feces in the form of metabolites within 48 to 96 hours. The main urinary  metabolite is ritalinic acid (alpha-phenyl-2-piperidine acetic acid, PPAA); unchanged  methylphenidate is excreted in the urine in small quantities (<1%). Peak PPAA plasma  concentrations occurred at approximately the same time as peak methylphenidate  concentrations, however, levels were several-fold greater than those of the unchanged drug.  The half-life of PPAA was approximately twice that of methylphenidate.  In blood, methylphenidate and its metabolites are distributed between plasma (57%) and  erythrocytes (43%). Methylphenidate and its metabolites exhibit low plasma protein binding  (approx. 15%).  Methylphenidate in the extended-release tablets is more slowly but as extensively absorbed as  in the regular tablets. Relative bioavailability of the Ritalin SR tablet, compared to the Ritalin  tablet, measured by the urinary excretion of the methylphenidate major metabolite (PPAA), was  105% (49 to 168%) in children and 101% (85% to 152%) in adults. The time to peak rate in  children was 4.7 hours (1.3 to 8.2 hours) for the extended-release tablets and 1.9 hours (0.3 to  4.4 hours) for the regular tablets. The elimination half-life and the cumulative urinary excretion of  PPAA are not significantly different between the two dosage forms. An average of 67% of the  extended-release tablet dose was excreted in children as compared to 86% in adults. Warnings Methylphenidate should not be used in children under 6 years of age, since safety and efficacy  
in this age group have not been established. 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. In addition, the use of "Drug Holidays" is recommended, that is, withholding the drug on weekends and during school holidays in as much as the clinical situation permits. 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. Methylphenidate 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 and, very rarely, in patients with no prior EEG evidence nor history 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. Pregnancy: Adequate animal reproduction studies to establish safe use of methylphenidate during pregnancy have not been conducted. Therefore, until more information is available, the use of methylphenidate in pregnancy is not recommended. Lactation: It is not known whether the active substance of methylphenidate and/or its metabolites pass into breast milk. For safety reasons, mothers taking methylphenidate should refrain from breast feeding their infants. Drug Dependence: Methylphenidate should be given cautiously to emotionally unstable patients, such as those with a history of drug dependence or alcoholism, because such patients may increase dosage on their own initiative. Chronically abusive use can lead to marked tolerance and psychic dependence with varying degrees of abnormal behavior. Frank psychotic episodes can occur, especially with parenteral abuse. Careful supervision is required during drug withdrawal, since severe depression as well as the effects of chronic overactivity can be unmasked. Long-term follow-up may be required because of the patient's basic personality disturbances. Available clinical data indicate that treatment with methylphenidate during childhood and/or adolescence does not seem to result in increased predisposition for addiction. Precautions Patients with an element of agitation may react adversely; discontinue therapy if necessary. Periodic CBC, differential, and platelet counts are advised during prolonged therapy. Drug treatment is not indicated in all cases of Attention Deficit Hyperactivity Disorders 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. Occupational Hazards: Because methylphenidate may affect performance, patients should be cautioned against engaging in hazardous activities such as operation of automobiles or dangerous machinery. 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, diphenylhydantoin, primidone), phenylbutazone and tricyclic antidepressants (imipramine, desipramine). Downward dosage adjustments of these drugs may be required when given concomitantly with methylphenidate. Adverse Effects Nervousness and insomnia are the most common adverse reactions reported with methylphenidate but are usually controlled by reducing dosage and omitting the drug in the afternoon or evening. Decreased appetite is also common but usually transient. Central and Peripheral Nervous System: Dizziness, drowsiness, headache, and dyskinesia may occur. Isolated cases of the following have been reported: hyperactivity, convulsions, muscle cramps, choreo-athetoid movements, tics, or exacerbation of pre-existing tics, Tourette's syndrome, and psychotic episodes including hallucinations which subsided when methylphenidate was discontinued. Psychic dependence in emotionally unstable persons has occurred rarely with chronic treatment. Although a definite causal relationship has not been established, isolated cases of transient depressed mood have been reported. Symptoms of visual disturbances have been encountered in rare cases. Difficulties with accommodation and blurring of vision have been reported. Gastrointestinal: Nausea and abdominal pain may occur at the start of treatment and may be alleviated if taken with food. Cardiovascular: Palpitations, blood pressure and pulse changes (both up and down), tachycardia, angina and cardiac arrhythmias. Skin and/or Hypersensitivity: Rash, pruritus, urticaria, fever, arthralgia, and alopecia. Isolated cases of exfoliative dermatitis, erythema multiforme with histopathological findings of necrotizing vasculitis, and thrombocytopenic purpura. Hematologic: Isolated cases of leukopenia, thrombocytopenia and anemia. Other: Weight loss during prolonged therapy. 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. Minor retardation of growth may also occur during prolonged therapy in children (see Warnings). Overdose Symptoms: Signs and symptoms of acute overdosage, resulting principally from CNS overstimulation and from excessive sympathomimetic effects, may include the following: vomiting, agitation, tremors, hyperreflexia, muscle twitching, convulsions (may be followed by coma), euphoria, confusion, hallucinations, delirium, sweating, flushing, headache, hyperpyrexia, tachycardia, palpitations, cardiac arrhythmias, hypertension, mydriasis and dryness of mucous membranes. Treatment: Appropriate supportive measures. The patient must be protected against self-injury and against external stimuli that would aggravate overstimulation already present. If signs and symptoms are not too severe and the patient is conscious, gastric contents may be evacuated by induction of emesis or gastric lavage. In the presence of severe intoxication, use a carefully titrated dosage of short-acting barbiturate before performing gastric lavage. Intensive care must be provided to maintain adequate circulation and respiratory exchange; external cooling procedures may be required for hyperpyrexia. Efficacy of peritoneal dialysis or extracorporeal hemodialysis for methylphenidate overdosage has not been established. Dosage Dosage should be individualized according to the needs and responses of the patient. Children (6 years and over): Ritalin tablets: Should be initiated in small doses, (e.g. 5 to 10 mg 3 times daily) with weekly increments of 5 to 10 mg in the daily dosage. Dosage should be individualized on the basis of factors such as age, body weight and individual response. Timing of drug administration should be aimed to coincide with periods of greatest academic, behavioral and social difficulties for the patient. Daily dosage above 60 mg is not recommended. If improvement is not observed after appropriate dosage adjustments over a 1 month period, the drug should be discontinued. Ritalin SR (extended-release) tablets: Ritalin SR tablets have a duration of action of approximately 8 hours. Therefore, they may be used in place of Ritalin tablets when the 8 hour dosage of Ritalin SR corresponds to the titrated 8 hour dosage of Ritalin. Ritalin SR tablets must be swallowed whole and never be crushed or chewed. If paradoxical aggravation of symptoms or other adverse effects occur, reduce dosage, or if necessary, discontinue the drug. Ritalin 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. Adults: Ritalin tablets: Administer in divided doses 2 or 3 times daily, preferably 30 to 40 minutes before meals. Average daily dosage is 20 to 30 mg. Some patients may require 40 to 60 mg daily. In others, 10 to 15 mg daily will be adequate. Patients who are unable to sleep if medication is taken late in the day, should take the last dose before 6 p.m. Ritalin SR (extended-release) tablets: SR tablets have a duration of action of approximately 8 hours. Therefore, they may be used in place of Ritalin tablets when the 8 hour dosage of Ritalin SR corresponds to the titrated 8 hour dosage of Ritalin. Ritalin SR tablets must be swallowed whole and never be crushed or chewed. Supplied Ritalin: Each pale blue, round, scored tablet, imprinted CIBA on one side and AB on the other, contains: Methylphenidate HCl 10 mg. Energy: 1.88 kJ (0.45 kcal). Each light yellow, round, scored tablet, imprinted CIBA on one side and PN on the other, contains: Methylphenidate HCl 20 mg. Energy: 2.4 kJ (0.58 kcal). Both strengths contain lactose. Alcohol-free, bisulfite-free, gluten-free, parabens-free, sodium-free and tartrazine-free. Bottles of 100 and 500. Protect from heat and humidity. Ritalin SR: Each white, round, coated extended-release tablet, imprinted CIBA on one side and 16 on the other, contains: Methylphenidate HCl 20 mg. Energy: 1.55 kJ (0.37 kcal). Also contains lactose. Alcohol-free, bisulfite-free, gluten-free, parabens-free, sodium-free and tartrazine- free free. Bottles of 100.