Lisdexamfetamine

Lisdexamfetamine
ATC Code N06BA12
Formula C15H25N3O
Molar Mass (g·mol−1) 263,38
Physical State solid
CAS Number 608137-32-2
PUB Number 21954928
Drugbank ID DB01255

Basics

Lisdexamfetamine is a central nervous system (CNS) stimulant used to treat attention deficit hyperactivity disorder (ADHD) in adults and children over 6 years of age and moderate to severe eating disorders.

Use and indications

Lisdexamfetamine is most commonly used to treat ADHD in children between 6 and 18 years of age. However, if well tolerated and indicated, use beyond this age is possible. In some countries, lisdexamfetamine is only indicated if previous therapy with the active ingredient methylphenidate (Ritalin, Medikinet, etc.) has not been effective. In many countries, however, it can also be used as a "first-line therapeutic". In addition, it can be used to treat so-called binge-eating disorder, an eating disorder. This involves reducing the number of binge eating episodes in affected patients.

The active ingredient is administered in the form of raked capsules and is available in doses of 30 mg, 50 mg, and 70 mg. The dosage depends on the patient's weight. Lisdexamfetamine can also be given in the form of chewable tablets.

History

Lisdexamfetamine was first approved for medical use in the United States in 2007. It was developed and patented by Takeda Pharmaceutical.

Pharmacology

Pharmacodynamics and mechanism of action

Lisdexamfetamine is a prodrug of d-amphetamine. Amphetamines are non-catecholamine sympathomimetic amines with CNS stimulant properties. The effects of this substance are primarily due to the release of the neurotransmitters dopamine and norepinephrine from their storage vesicles in presynaptic nerve endings. These two transmitters contribute to effects such as alertness, increased concentration, and effort and motivation.

Pharmacokinetics

After oral administration, lisdexamfetamine is rapidly absorbed from the gastrointestinal tract. Lisdexamfetamine is hydrolyzed in the blood to D-amphetamine, as well as to the amino acid L-lysine. D-amphetamine is degraded via the liver, primarily by the enzyme CYP2D6. More than 90% of the given dose is excreted in the urine. The mean plasma elimination half-life of dextroamphetamine after oral administration was approximately 12 hours.

Drug Interactions

  • Drugs that acidify the urine, such as ascorbic acid, increase urinary excretion of dextroamphetamine and thus shorten the half-life of dextroamphetamine in the body, attenuating its effect.
  • Drugs that alkalinize the urine, such as sodium bicarbonate, decrease the urinary excretion of dextroamphetamine and thus increase the half-life of dextroamphetamine in the body, thereby increasing the effect.
  • Potent CYP2D6 inhibitors, such as paroxetine, fluoxetine, bupropion, and duloxetine, may inhibit the metabolism of dextroamphetamine, thereby increasing exposure to the drug. Concomitant use of lisdexamfetamine with CYP2D6 inhibitors may increase the risk of serotonin syndrome.
  • Concomitant use of MAOIs and central nervous system stimulants such as lisdexamfetamine may lead to hypertensive crisis.

Toxicity

Contraindications

This agent is contraindicated if:

  • there is an allergy to the active substance
  • if MAO inhibitors have been taken in the last 14 days before taking this drug
  • if there are thyroid problems
  • if there is a history of heart problems, such as heart attack, arrhythmia, or congenital heart defect
  • if there is particularly high blood pressure (severe hypertension)
  • if there is increased intraocular pressure (glaucoma)

Side effects

Serious side effects that should be reported to a doctor immediately if they occur:

  • irregular heartbeat (palpitations),
  • chest pain
  • seeing, feeling, or hearing things that are not really there (hallucinations),
  • feeling of unusual excitement, excessive activity, or disinhibition (mania),
  • allergic reaction (hypersensitivity),
  • shortness of breath or swelling of the legs (signs of heart muscle disease).
  • severe allergic reaction characterized by severe drop in blood pressure, difficulty breathing, and hives/itching(anaphylactic reaction),
  • seeing or feeling or hearing things that are not really there, paranoia, delusions (psychotic episodes),
  • seizures (convulsions),
  • abnormal heart rhythm, life-threatening irregular heart rhythm (visible on electrocardiogram). See section 2, Warnings and Precautions,
  • Yellowing of the whites of the eyes
  • Skin swelling (angioedema) or severe skin rash manifested as severe blistering of the skin and mucous membranes (Stevens-Johnson syndrome).

Other possible side effects:

  • decreased appetite,
  • weight loss,
  • sleep disturbances,
  • dry mouth,
  • abdominal pain,
  • headache,
  • feeling agitated, run down or "hippy", anxiety, depression, aggressiveness, irritability, or mood swings,
  • unusual sleepiness, fatigue, or restlessness,
  • Inability to get or maintain an erection or changes in sex drive,
  • dizziness,
  • uncontrolled twitching or jerky movements, tremors, or unusually vigorous activity,
  • fast or irregular heartbeat (tachycardia),
  • difficulty breathing,
  • nausea, vomiting, or diarrhea
  • constipation
  • Increased temperature(fever) or excessive sweating,
  • skin rash,
  • teeth grinding
  • hardly interruptible and often rapid speech,
  • dejection, anxiety, sad or depressed mood
  • excessively elevated or excited mood (euphoria),
  • compulsive excessive working of the skin,
  • uncontrolled twitching or erratic movements of the body,
  • itching, rash or red, itchy welts
  • blurred vision
  • excessive dilatation of the pupils
  • poor blood circulation with resulting numbness and whitening of the toes and fingers(Raynaud's syndrome)
  • high blood pressure
  • metallic taste in the mouth
  • brief loss of consciousness

Pregnancy and breastfeeding

This medicine should be used during pregnancy only as specifically instructed by a doctor. Do not breastfeed while taking Elvanse.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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