Lisdexamfetamine


Generic Medicine Info
Indications and Dosage
Oral
Attention deficit hyperactivity disorder
Adult: Initially, 30 mg once daily in the morning, may be increased in increments of 10 mg or 20 mg at approx weekly intervals if necessary. Max: 70 mg daily. If symptoms do not improve after 1 month with an appropriate dosage adjustment, discontinue treatment. Individualise dosage according to patient response and needs to therapy. Use the lowest effective dose.
Child: ≥6 years Same as adult dose.
Elderly: Initiate at the lower end of the dosing range.

Oral
Binge eating disorder
Adult: Moderate to severe cases: Initially, 30 mg once daily in the morning, may be titrated in increments of 20 mg at approx weekly intervals to reach the target dose range of 50-70 mg daily. Max: 70 mg daily. If binge eating does not improve, discontinue treatment.
Elderly: Initiate at the lower end of the dosing range.
Renal Impairment
ESRD (GFR <15 mL/min/1.73 m2): Max: 30 mg daily. Severe (GFR 15-<30 mL/min/1.73 m2): Max: 50 mg daily.
Administration
May be taken with or without food. Take in the morning. Cap may be taken whole, or the cap opened & the entire contents dissolved in a glass of water & drunk immediately. The dose of a single cap should not be divided.
Contraindications
Moderate to severe hypertension, symptomatic CV disease, structural cardiac abnormalities, serious heart arrhythmia, cardiomyopathy, coronary artery disease, other serious heart problem; advanced arteriosclerosis, hyperthyroidism or thyrotoxicosis, agitated states, glaucoma. Lactation. Concomitant use with or within 14 days of discontinuing MAOIs (including linezolid and IV methylene blue).
Special Precautions
Patient with CV disease (e.g. pre-existing hypertension, recent MI, heart failure, ventricular arrhythmia, QTc interval prolongation), electrolyte disturbances, pre-existing bipolar disorder or psychosis, seizure disorder, Tourette's syndrome, other tic syndromes, history of drug or alcohol abuse. Not indicated or recommended for weight loss. Avoid abrupt withdrawal. Severe renal impairment, including ESRD. Children and elderly. Pregnancy.
Adverse Reactions
Significant: Cardiomyopathy, QTc interval prolongation, increased blood pressure and heart rate; sudden death (patient with pre-exisiting structural cardiac abnormalities or other serious heart problems); hypersensitivity reactions, including anaphylaxis, angioedema, Stevens-Johnson syndrome; induction of mixed/manic episodes, emergence or exacerbation of psychotic symptoms (e.g. hallucination, delusion), aggression and hostility (particularly in children and adolescents), motor and phonic tic exacerbation, worsened Tourette's syndrome, decreased seizure threshold, increased risk of drug abuse and dependence; withdrawal symptoms; weight loss, growth and appetite suppression (particularly in children), urticaria, visual disturbances (e.g. blurred vision, accommodation difficulties), peripheral vasculopathy, including Raynaud’s phenomenon. Rarely, digital ulceration or soft tissue breakdown.
Cardiac disorders: Tachycardia, palpitation, chest pain.
Gastrointestinal disorders: Dry mouth, nausea, vomiting, diarrhoea, upper abdominal pain, constipation.
General disorders and administration site conditions: Fatigue, feeling jittery, irritability, pyrexia.
Metabolism and nutrition disorders: Decreased appetite.
Nervous system disorders: Headache, dizziness, tremor, restlessness, drowsiness.
Psychiatric disorders: Insomnia, agitation, anxiety, bruxism, depression, affect lability, psychomotor hyperactivity.
Reproductive system and breast disorders: Erectile dysfunction, decreased libido.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Hyperhidrosis, rash.
Potentially Fatal: Serious CV events including MI and stroke.
Patient Counseling Information
This drug may cause dizziness, drowsiness, or visual disturbances such as blurred vision; if affected, do not drive or operate machinery.
Monitoring Parameters
Perform complete assessment for the presence of cardiac disease including a physical exam and family history of sudden unexplained/cardiac death and ventricular arrhythmia before treatment initiation; if findings suggest such disease, further evaluate CV status (e.g. ECG, echocardiogram). Assess for the potential of misuse, abuse, or diversion, and those at risk for bipolar disorder or mania development prior to starting treatment. Conduct prompt cardiac evaluation in patients who develop symptoms of cardiac disease (e.g. exertional chest pain, unexplained syncope) during therapy. Monitor blood pressure and heart rate at baseline, after dose increases, and periodically thereafter; weight in adults; growth rate (e.g. height, weight), appetite in children. Assess for signs of worsening of psychiatric disorder during dose adjustments or visits and at least every 6 months thereafter, behavioural or sleep changes, peripheral vasculopathy (e.g. digital changes), and misuse, abuse, or addiction throughout therapy.
Overdosage
Symptoms: Tremor, restlessness, rapid respiration, hyperreflexia, confusion, panic states, aggression, hallucination, hyperpyrexia, rhabdomyolysis, fatigue and depression following the CNS stimulation, CV effects (e.g. hypertension or hypotension, arrhythmias, circulatory collapse), gastrointestinal symptoms (e.g. nausea, vomiting, diarrhoea, abdominal cramps), convulsions and coma. Management: Symptomatic treatment. Perform gastric lavage; administer activated charcoal or a cathartic and induce sedation. Consider urine acidification to enhance excretion (may increase risk of acute renal failure if with myoglobinuria). Administer IV phentolamine for acute severe hypertension.
Drug Interactions
Urine alkalinising agents (e.g. acetazolamide) may increase the plasma levels and action of amfetamines. Blood levels and efficacy of amfetamines may be decreased by urine acidifiers (e.g. Na acid phosphate, ammonium chloride, ascorbic acid, methenamine salts). May potentiate the effects of narcotic analgesics. Central stimulant effects of amfetamines may be inhibited by haloperidol and chlorpromazine. Lithium carbonate may block the anorectic and stimulatory effects of amfetamines. May enhance the CV effects of tricyclic or sympathomimetic agents (e.g. desipramine, protriptyline).
Potentially Fatal: Increased risk of serotonin syndrome and hypertensive crisis with MAOIs. Increased risk of serotonin syndrome with SSRIs, serotonin norepinephrine reuptake inhibitors (SNRIs), triptans, TCAs, fentanyl, lithium, tramadol, tryptophan, and buspirone.
Food Interaction
Increased risk of serotonin syndrome with St. John's wort.
Lab Interference
May interfere with the determination of urinary steroids. May significantly increase plasma corticosteroid levels.
Action
Description: Lisdexamfetamine, a prodrug of dexamfetamine (also known as dextroamphetamine), is a non-catecholamine sympathomimetic amine with CNS stimulating action. Its mechanism of action is unknown; however, it is thought to inhibit norepinephrine and dopamine reuptake into the presynaptic neuron and increase the release of these monoamines in the extraneuronal space.
Duration: 8-14 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: Lisdexamfetamine: Approx 1 hour (cap); 1 hour (chewable tab, at fasted state). Dexamfetamine: 3.8 hours (cap, at fasted state); 4.7 hours (cap, after a high-fat meal); 3.9-4.4 hours (chewable tab, at fasted state); 4.9 hours hour (chewable tab, after a high-fat meal).
Distribution: Crosses the placenta (as dexamfetamine) and enters breastmilk.
Metabolism: Metabolised mainly in the blood via the hydrolytic activity of the RBCs to form dexamfetamine (active metabolite) and l-lysine.
Excretion: Via urine (96%; 42% as amfetamine-related compounds, 25% as hippuric acid, 2% as unchanged drug); faeces (0.3%). Elimination half-life: <1 hour (lisdexamfetamine); 10-13 hours (dexamfetamine).
Chemical Structure

Chemical Structure Image
Lisdexamfetamine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 11597698, Lisdexamfetamine. https://pubchem.ncbi.nlm.nih.gov/compound/Lisdexamfetamine. Accessed Sept. 24, 2021.

Storage
Store between 15-30°C. Protect from light.
MIMS Class
Other CNS Drugs & Agents for ADHD
ATC Classification
N06BA12 - lisdexamfetamine ; Belongs to the class of centrally-acting sympathomimetics. Used as CNS stimulant.
References
Anon. Lisdexamfetamine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 01/07/2021.

Anon. Lisdexamfetamine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/07/2021.

Buckingham R (ed). Lisdexamfetamine Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/07/2021.

Elvanse Adult 30 mg Hard Capsules (Shire Pharmaceutical Contracts Limited). MHRA. https://products.mhra.gov.uk. Accessed 01/07/2021.

Joint Formulary Committee. Lisdexamfetamine Mesilate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/07/2021.

Vyvanse Capsule and Chewable Tablet (Takeda Pharmaceuticals America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/07/2021.

Vyvanse Capsules (Takeda Pharmaceuticals [Hong Kong] Ltd). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 01/07/2021.

Disclaimer: This information is independently developed by MIMS based on Lisdexamfetamine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 MIMS. All rights reserved. Powered by MIMS.com
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