Amphetamine Aspartate

For the treatment of ADHD in adults, the typical starting dose of mixed amphetamine salts (containing Amphetamine Aspartate) is 5 mg once or twice daily. Your healthcare provider may increase the daily dose by 5 mg at weekly intervals until the optimal therapeutic response is achieved. The maximum recommended dose for most adults is 40 mg per day, although some clinical situations may require higher doses under strict supervision. For Narcolepsy, the usual dose range is 5 mg to 60 mg per day, divided into multiple doses depending on the patient's sleep patterns and response.

• Children (ages 3 to 5): For ADHD, the starting dose is usually 2.5 mg daily. The dose may be increased in increments of 2.5 mg weekly.
• Children (ages 6 and older): The starting dose is typically 5 mg once or twice daily. Increments of 5 mg per week are common until the desired effect is reached.
• Narcolepsy: Amphetamine is rarely used for narcolepsy in children under 6. For those 6-12, the starting dose is 5 mg daily, increasing by 5 mg weekly. For those 12 and older, the starting dose is 10 mg daily.

Renal Impairment

In patients with severe renal impairment (GFR 15 to <30 mL/min/1.73 m²), the maximum dose should not exceed 20 mg per day for extended-release formulations. In patients with end-stage renal disease (ESRD), the use of Amphetamine Aspartate is generally not recommended as the drug is not efficiently cleared by dialysis.

Hepatic Impairment

While the liver is the primary site of metabolism, there are no specific quantitative guidelines for dose adjustments in hepatic impairment. However, healthcare providers usually exercise caution and may start at the lower end of the dosing spectrum due to the potential for reduced metabolic clearance.

Elderly Patients

Clinical studies for Amphetamine Aspartate did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function.

Amphetamine Aspartate should be taken exactly as prescribed. For immediate-release forms, the first dose is typically taken upon awakening, with subsequent doses spaced 4 to 6 hours apart. Extended-release capsules should be taken once daily in the morning. Taking this medication late in the day may result in significant insomnia (difficulty sleeping).

Extended-release capsules should generally be swallowed whole. However, for patients who cannot swallow capsules, some brands allow the capsule to be opened and the beads sprinkled onto a tablespoon of applesauce. The mixture must be consumed immediately without chewing the beads, as crushing or chewing destroys the extended-release mechanism and can lead to a dangerous "dose dump" of the medication.

If you miss a dose, take it as soon as you remember. However, if it is already late afternoon or evening, skip the missed dose and return to your regular schedule the next morning. Do not take a double dose to make up for a missed one, as this increases the risk of cardiovascular side effects and insomnia.

An overdose of Amphetamine Aspartate can be life-threatening. Signs of acute overdose include restlessness, tremor, rapid breathing (tachypnea), confusion, aggression, hallucinations, panic states, hyperpyrexia (extremely high fever), and rhabdomyolysis (muscle breakdown). Cardiovascular effects may include arrhythmias, hypertension or hypotension, and circulatory collapse. Gastrointestinal symptoms include nausea, vomiting, diarrhea, and abdominal cramps.

In the event of a suspected overdose, contact emergency services or a poison control center immediately. Treatment usually involves supportive care, administration of activated charcoal, and medications to manage blood pressure and seizures.

> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose or stop the medication without medical guidance, as sudden discontinuation can lead to severe withdrawal symptoms.

Most patients taking Amphetamine Aspartate will experience some level of side effects, particularly during the initial titration phase. Common effects include:

• Anorexia (Loss of Appetite): This is one of the most frequent side effects, often leading to weight loss. It is most pronounced during the middle of the day.
• Xerostomia (Dry Mouth): A decrease in saliva production can cause discomfort and increase the risk of dental cavities over time.
• Insomnia: Difficulty falling asleep or staying asleep, especially if the medication is taken too late in the day.
• Abdominal Pain: Often described as stomach cramps or nausea, which may improve if the medication is taken with a small amount of food.
• Tachycardia (Rapid Heart Rate): A noticeable increase in heart rate or palpitations.

• Emotional Lability: Irritability, mood swings, or a "rebound effect" where ADHD symptoms worsen as the medication wears off.
• Dizziness and Headache: These often subside as the body acclimates to the stimulant.
• Diarrhea or Constipation: Disruptions in gastrointestinal motility.
• Libido Changes: Changes in sexual drive or erectile dysfunction.

• Raynaud’s Phenomenon: Reduced blood flow to the fingers and toes, causing them to feel cold, numb, or change color (blue or white).
• Alopecia: Temporary thinning of the hair.
• Visual Disturbances: Blurred vision or difficulty with accommodation (focusing).

> Warning: Stop taking Amphetamine Aspartate and call your doctor immediately if you experience any of these serious symptoms.

• Cardiovascular Events: Chest pain, shortness of breath, or fainting. Stimulants can cause sudden death in patients with pre-existing heart defects or serious heart problems.
• Psychiatric Symptoms: New or worsening psychosis (hearing voices, believing things that are not true) or mania (extreme agitation and racing thoughts), even in patients with no prior history of these conditions.
• Anaphylaxis: Severe allergic reactions including swelling of the face, lips, or tongue, and difficulty breathing.
• Seizures: A lowering of the seizure threshold, particularly in patients with a history of epilepsy.
• Priapism: Painful and prolonged erections (lasting more than 4 hours), which require immediate surgical intervention to prevent permanent tissue damage.

Prolonged use of Amphetamine Aspartate may lead to several long-term considerations:

• Growth Suppression: In pediatric patients, stimulants have been associated with a temporary slowing in growth rate (both height and weight). Most children eventually reach their predicted adult height, but monitoring is essential.
• Tolerance and Dependence: Over time, the body may require higher doses to achieve the same effect. Physical and psychological dependence can develop, making it difficult to stop the medication.
• Cardiovascular Strain: Chronic elevation of blood pressure and heart rate may increase the long-term risk of cardiovascular disease.

Amphetamine Aspartate carries a prominent FDA Black Box Warning regarding its high potential for abuse and administration for prolonged periods may lead to drug dependence. Particular attention should be paid to the possibility of subjects obtaining amphetamines for non-therapeutic use or distribution to others. Furthermore, misuse of amphetamines may cause sudden death and serious cardiovascular adverse events.

Report any unusual symptoms or persistent side effects to your healthcare provider to ensure your treatment plan remains safe and effective.

Amphetamine Aspartate is a powerful stimulant that must be used with extreme caution. It is not suitable for everyone, and a comprehensive cardiovascular and psychiatric screening is mandatory before the first dose. Patients must be monitored regularly for changes in blood pressure, heart rate, and mental status.

Abuse and Dependence: Amphetamines have a high potential for abuse. Use of amphetamines for prolonged periods of time may lead to drug dependence and must be avoided. Misuse of amphetamine may cause sudden death and serious cardiovascular adverse events.

• Cardiovascular Risks: Stimulants cause an increase in blood pressure (average 2-4 mmHg) and heart rate (average 3-6 bpm). While these increases may be minor for many, they can be life-threatening for individuals with underlying heart defects, cardiomyopathy, or serious heart rhythm abnormalities.
• Psychiatric Risks: Stimulant medications may exacerbate symptoms of behavior disturbance and thought disorder in patients with a pre-existing psychotic condition. There is also a risk of inducing a mixed/manic episode in patients with bipolar disorder.
• Vascular Issues: Peripheral vasculopathy, including Raynaud’s phenomenon, has been reported. Patients should be monitored for digital changes (fingers/toes) such as numbness or color changes.
• Serotonin Syndrome: When used in combination with other serotonergic drugs (like SSRIs or SNRIs), there is a risk of Serotonin Syndrome, a potentially fatal condition characterized by mental status changes, autonomic instability, and neuromuscular hyperactivity.

Healthcare providers will typically require the following monitoring:

• Cardiovascular Screening: Baseline EKG (electrocardiogram) may be recommended if a family history of heart disease exists.
• Vital Signs: Regular checks of blood pressure and pulse at every office visit.
• Growth Tracking: In children, height and weight should be plotted on growth charts at least twice a year.
• Psychiatric Evaluation: Assessment for new-onset suicidal ideation, aggression, or hallucinations.

Amphetamine Aspartate may impair the ability of the patient to engage in potentially hazardous activities such as operating machinery or vehicles. While it often improves focus, the potential for dizziness or "crashing" as the medication wears off can affect reaction times. Use caution until you know how the medication affects you.

Alcohol should be strictly avoided. Alcohol can alter the way the body releases and absorbs Amphetamine Aspartate, particularly extended-release versions, leading to unpredictable blood levels. Furthermore, stimulants can mask the sedative effects of alcohol, increasing the risk of alcohol poisoning or risky behavior.

Do not stop taking Amphetamine Aspartate abruptly after long-term use. Sudden discontinuation can lead to "amphetamine crash," characterized by extreme fatigue, depression, and sleep disturbances. Your doctor will provide a tapering schedule to gradually reduce the dose.

> Important: Discuss all your medical conditions, especially any history of heart problems or mental health issues, with your healthcare provider before starting Amphetamine Aspartate.

• MAO Inhibitors (MAOIs): Amphetamine Aspartate must not be used during or within 14 days following the administration of monoamine oxidase inhibitors (e.g., phenelzine, selegiline). This combination can trigger a hypertensive crisis—a sudden, severe increase in blood pressure that can lead to stroke or organ damage.

• Serotonergic Drugs: Combining amphetamines with SSRIs (e.g., fluoxetine), SNRIs (e.g., venlafaxine), or triptans increases the risk of Serotonin Syndrome. This occurs because amphetamine has mild serotonergic activity which can be additive.
• CYP2D6 Inhibitors: Drugs that inhibit the CYP2D6 enzyme (e.g., paroxetine, quinidine) can slow the metabolism of amphetamine, leading to toxic levels in the blood.
• Alkalinizing Agents: Sodium bicarbonate (baking soda) or certain antacids increase the absorption of amphetamine and reduce its excretion, significantly increasing its effects.

• Antihypertensives: Amphetamines may antagonize (work against) the effects of blood pressure medications, requiring dosage adjustments of the antihypertensive agent.
• Anticonvulsants: Amphetamines may delay the absorption of certain seizure medications like ethosuximide.
• Tricyclic Antidepressants: May enhance the cardiovascular effects of amphetamines, leading to significant increases in heart rate.

• Acidic Foods and Juices: Fruit juices (like orange or grapefruit juice) and foods high in Vitamin C (ascorbic acid) can act as urinary acidifying agents. This increases the rate at which the kidneys flush amphetamine out of the system, potentially reducing the drug's effectiveness.
• Caffeine: Excessive caffeine intake can worsen the stimulant side effects of Amphetamine Aspartate, leading to jitteriness, anxiety, and severe insomnia.

• St. John’s Wort: May increase the risk of Serotonin Syndrome.
• Melatonin: While often used to counter stimulant-induced insomnia, it should be used cautiously as it may affect the morning-after alertness.
• Vitamin C Supplements: High doses (1000mg+) can reduce the blood levels of amphetamine by increasing renal excretion.

Amphetamines can cause a significant elevation in plasma corticosteroid levels, with the greatest increase occurring in the evening. They may also interfere with urinary steroid determinations. If you are undergoing a drug screen, Amphetamine Aspartate will result in a positive test for amphetamines; always provide your prescription documentation to the testing laboratory.

> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, as well as any changes in your diet.

Amphetamine Aspartate must NEVER be used in patients with the following conditions:

• Advanced Arteriosclerosis: Hardening of the arteries, as the stimulant effects can lead to vascular rupture or heart attack.
• Symptomatic Cardiovascular Disease: Any active heart condition where increased heart rate or blood pressure poses an immediate threat.
• Moderate to Severe Hypertension: Uncontrolled high blood pressure.
• Hyperthyroidism: Excessive thyroid hormone already overstimulates the metabolism; adding a CNS stimulant can lead to a thyroid storm.
• Glaucoma: Amphetamines can increase intraocular pressure (pressure inside the eye), worsening the condition.
• Agitated States: Patients who are currently in a state of extreme agitation or anxiety.
• History of Drug Abuse: Due to the high potential for addiction and relapse.
• MAOI Use: Within the last 14 days.

Conditions requiring careful risk-benefit analysis include:

• Tics or Tourette’s Syndrome: Stimulants may exacerbate motor or vocal tics in some patients.
• Seizure Disorders: May lower the threshold for having a seizure.
• Bipolar Disorder: Risk of inducing mania.

Patients who have shown a hypersensitivity or allergic reaction to other sympathomimetic amines (such as pseudoephedrine or methylphenidate) should use Amphetamine Aspartate with extreme caution, as cross-sensitivity is possible. Symptoms of an allergic reaction include rash, hives, or swelling.

> Important: Your healthcare provider will evaluate your complete medical history before prescribing Amphetamine Aspartate to ensure it is safe for your specific health profile.

Amphetamine Aspartate is classified under the former FDA Pregnancy Category C. Data on its use in pregnant women are limited. However, studies suggest that infants born to mothers dependent on amphetamines have an increased risk of premature delivery and low birth weight. There is also a risk of withdrawal symptoms (neonatal abstinence syndrome) in the newborn, characterized by agitation and extreme drowsiness. Amphetamine Aspartate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Amphetamines are excreted in human milk. Because of the potential for serious adverse reactions in nursing infants (such as tachycardia, irritability, and poor weight gain), mothers taking Amphetamine Aspartate are advised to avoid breastfeeding. Consult with a pediatrician about safe infant feeding alternatives.

Amphetamine Aspartate is FDA-approved for the treatment of ADHD in children as young as 3 years old. However, it is not recommended for children under 3. The primary concern in pediatric use is the suppression of growth. Clinical data suggests that children on long-term stimulant therapy may experience a temporary slowing in height and weight gain. Healthcare providers must monitor growth parameters closely and may suggest "medication holidays" (stopping the drug during summer breaks) to allow for catch-up growth.

Elderly patients (65+) are at a higher risk for cardiovascular side effects and may have reduced renal function, which can lead to drug accumulation. Stimulants can also worsen pre-existing sleep disturbances or agitation in older adults. Lower starting doses and frequent monitoring are mandatory for this population.

Since the kidneys are responsible for the excretion of amphetamine, any reduction in GFR (Glomerular Filtration Rate) will result in higher drug levels. For patients with a GFR between 15 and 30, the dose of extended-release forms should be capped at 20 mg. It is not recommended for those with a GFR below 15.

While specific dose adjustments are not codified, the liver's role in the oxidative metabolism of amphetamine means that patients with severe cirrhosis or hepatitis may experience prolonged drug effects. Monitoring for toxicity is essential.

> Important: Special populations require individualized medical assessment and frequent follow-up to ensure safety and efficacy.

Amphetamine Aspartate is a potent inducer of monoamine release. Its primary molecular target is the Trace Amine-Associated Receptor 1 (TAAR1), a G protein-coupled receptor located in the presynaptic terminal. Upon binding, it triggers the phosphorylation of the Dopamine Transporter (DAT), causing it to function in reverse. Simultaneously, it enters the neuron via DAT and inhibits the Vesicular Monoamine Transporter 2 (VMAT2), which normally packages dopamine into vesicles. This causes a massive efflux of dopamine and norepinephrine into the synapse, enhancing signal transmission in the reward and attention centers of the brain.

The pharmacodynamic effects of Amphetamine Aspartate include increased alertness, decreased fatigue, and improved mood. There is a clear dose-response relationship, where higher doses lead to greater neurotransmitter release but also a higher risk of side effects like hypertension. Tolerance to the euphoric and appetite-suppressant effects often develops within weeks, whereas the therapeutic effects for ADHD tend to remain stable over longer periods.

| Parameter | Value |

|---|---|

| Bioavailability | 75% - 80% |

| Protein Binding | ~20% |

| Half-life | 9 - 14 hours (Adults) |

| Tmax | 3 hours (IR), 7 hours (ER) |

| Metabolism | Hepatic (CYP2D6) |

| Excretion | Renal (pH dependent) |

Amphetamine Aspartate (C13H19NO4) is the aspartic acid salt of the racemic mixture of d-amphetamine and l-amphetamine. It has a molecular weight of approximately 269.3 g/mol. It appears as a white, odorless crystalline powder that is soluble in water. The aspartate salt is used specifically to modulate the solubility and release characteristics of the amphetamine molecule within a multi-salt matrix.

Amphetamine Aspartate belongs to the CNS Stimulant class, specifically the Amphetamine sub-class. Related medications include Dextroamphetamine Sulfate, Amphetamine Sulfate, and Lisdexamfetamine (Vyvanse).