Amphetamine

Amphetamines are psychostimulants with high addiction potential. Learn more about amphetamines, including their long and short-term effects.

Amphetamine is a stimulant that was initially used as an over-the-counter drug for a wide variety of disorders including depression and nasal congestion.

The addictive properties of amphetamine were recognized and its use is now restricted as a prescription medication for disorders such as attention-deficit/hyperactivity disorder (ADHD) and narcolepsy. Because of its high addiction potential and relatively easy access, amphetamines are one of the most commonly abused drugs.

What Is Amphetamine?

Amphetamine is the common name for the chemical compound α-methylphenethylamine. The drug, methamphetamine, that shares similar chemical and biological properties with α-methylphenethylamine, is also referred to as an amphetamine. Amphetamines mimic the activation of the sympathetic nervous system, which is associated with increased arousal and fight-or-flight responses.

Amphetamines are psychostimulants that evoke an increase in the levels of catecholamines like norepinephrine and monoamines like dopamine and serotonin. This reaction is due to the increased production of these neurotransmitters as well as their reduced absorption or reuptake. The neurotransmitter dopamine is involved in motivated behaviors. Changes in the dopaminergic system are associated with addiction. The action of amphetamine on dopaminergic neurons contributes to the high addiction potential of this drug. Amphetamine use results in increased energy, euphoria, increased sensory awareness and focus.

What Is Amphetamine Used For?

Amphetamines are primarily used for the treatment of the symptoms of ADHD. Amphetamines used for pharmacological purposes are generally synthesized in the form of salts of amphetamines. ADHD is associated with a dysregulation of catecholamines like norepinephrine in the prefrontal cortex and the striatum that are involved in cognitive functioning and motivated behaviors.

Amphetamines are used to treat ADHD because of their ability to modulate the levels of norepinephrine and dopamine in the prefrontal cortex. Besides ADHD, amphetamines are also used for the treatment of narcolepsy, that is characterized by excessive sleepiness during the daytime. Amphetamines are also used recreationally to improve cognitive and athletic performance, to lose weight, to feel more energetic and for sleep postponement.

Administration and Dose

Amphetamines for therapeutic use were traditionally used in the form of immediate-release pellets that are administered twice a day. The onset of the therapeutic effects of such immediate release amphetamines requires about 30 minutes and the effects of the drug last for about five hours. Immediate-release amphetamines are approved by the FDA for the treatment of ADH at a dose of 2.5 mg per day for children between the ages of three and six. For school-aged children, a higher dose of 5 mg to 40 mg per day may be prescribed for ADHD treatment.

Recently, longer-lasting formulations that need to be administered only once a day were released. These delayed-release beads are enteric-coated and have a peak effect after four to seven hours after drug ingestion, with the effect of the drug lasting for about 12 hours. Such extended-release formulations of mixed salts like Adderall may be administered at a maximum dosage of 30 mg per day.  Medication may be initially prescribed at a lower dose and then gradually increased. The optimal dose for an individual depends upon the absorption of the drug that tends to vary from person to person. One must only take amphetamine medications as prescribed. Always consult with a medical professional before taking a new medication.

Types of Amphetamines

Amphetamine belongs to a family of stimulants that share similar chemical and biological properties, referred to as amphetamine-type substances. Besides amphetamine and methamphetamine, this family also includes other stimulant substances such as methylphenidate, methylenedioxymethamphetamine, ephedrine and pseudoephedrine.

Amphetamine exists in two chemically identical, or isomeric, forms that are mirror images of each other. These two forms (referred to as enantiomers) are non-superimposable and only differ in spatial configuration. The two mirror-image isomers are referred to as the dextro and levo forms of the compound. Amphetamine also exists in two such isomeric forms known as dextroamphetamine (d-amphetamine) and levoamphetamine (l-amphetamine).

Dextroamphetamine is the more potent form of the drug and is either used alone or in combination with levoamphetamine to prolong its effects.

Both amphetamines and amphetamine-type substances are used as prescription medications for ADHD and other health problems. Some of the common types of prescription amphetamines are:

Dextroamphetamine

Dextroamphetamine is the more potent of the two methylphenethylamine enantiomers and is sold under the brand name Dexedrine. It is generally prescribed for the treatment of ADHD.

Levoamphetamine

Levoamphetamine, or l-amphetamine, is also effective in the treatment of ADHD but its use has declined over the past few decades in favor of d-amphetamine. Levoamphetamine is used in combination with dextroamphetamine in the ratio of 1:3 to produce mixed salts/mixed enantiomers (MES) amphetamine.

Methamphetamine

Methamphetamine (Desoxyn) was approved by the FDA for the treatment of ADHD and obesity. It is a last-resort treatment for obesity and is only recommended for short-term use due to its high addiction potential. Methamphetamine is also a common drug of abuse and is known simply as meth, crystal meth or ice.

Adderall

Adderall is a 3:1 mixture of d-amphetamine and l-amphetamine and is commonly used for the treatment of ADHD in children and adults. Although d-amphetamine is three to five times more potent than l-amphetamine, the addition of the l-amphetamine enantiomer prolongs the effects of d-amphetamine.

Methylphenidate

Methylphenidate is sold under the brand names of Ritalin and Concerta, and is another commonly used stimulant for the treatment of ADHD. Methylphenidate is not an amphetamine but belongs to the amphetamine-type substance family. Ritalin has a similar mode of action and side effect profile as Adderall but it has a shorter half-life.

Lisdexamfetamine dimesylate

Lisdexamfetamine dimesylate is a relatively newer form of amphetamine. It consists of the amino acid lysine attached to d-amphetamine and is only active after oral ingestion. Lisdexamfetamine is considered to have a lower risk for abuse because of the delayed-release of the active form of the drug, d-amphetamine, in the circulation.

What Does Amphetamine Look Like?

Amphetamines in their pure form exist as white crystalline powder and are odorless and bitter. Amphetamines that are illicitly sold may take the form of powder, capsules, tablets or crystals. The appearance of amphetamines sold illicitly varies depending on the presence of impurities and the color may vary from white to brown with traces of green and pink.

Amphetamine Street Names

Amphetamines may also be used as a drug of abuse and are sold illicitly under different street names, such as:

• Biphematine
• Delcobase
• Desoxyn
• Obetrol
• Reds
• Black Beauties
• Crosses
• Hearts

Methamphetamine is sold under the names of:

•  Chalk
•  Crystal, meth or crystal meth
•  Glass
•  Ice
•  Speed
•  Tina

Amphetamine Side Effects

Amphetamine is a sympathomimetic drug that mimics the stimulation of the sympathetic nervous system. Consistent with this mode of action, amphetamine intake results in increased heart rate and blood pressure, hyperactivity, inhibition of hunger and gastrointestinal effects. Other short-term side effects associated with the use of amphetamines include effects on mood and behavior.

Short-Term Effects

Some of the common short-term effects of amphetamine include nervousness, insomnia, headaches, increased blood pressure and heart rate, and loss of appetite. Other symptoms may include increased anxiety, irritability, negative affect and worsening motor tics. Side effects due to the action of amphetamines on the digestive system may include vomiting, nausea and abdominal cramps. High doses of amphetamines can also induce symptoms of psychosis and agitation in some (but not all) healthy individuals, that are similar to schizophrenia. Such drug-induced psychosis often involves paranoid delusions, hallucinations, violent behavior and occasionally disorganized speech. High doses of amphetamines can lead to cardiotoxicities including arrhythmias and infarctions that can be fatal.

Long-Term Effects

When used at doses prescribed for the treatment of ADHD, the side effects of Adderall are not severe in most patients. The use of stimulants such as amphetamines and methylphenidate were shown to be effective and well-tolerated when taken over several years. However, whether long-term use affects cognitive abilities or other biological functions requires further investigation.

Long-term use of amphetamines can lead to drug dependence and addiction. Methamphetamine is a widely used illicit drug and most of the information on the long-term effects of amphetamine use is based on methamphetamine abuse. Long-term use of methamphetamine is associated with anxiety, depression, weight loss, dental problems and psychosis. Long-term methamphetamine use can also increase the risk of cardiac complications including arrhythmias and infarction. Long-term use of amphetamines can result in the neglect of social and occupational responsibilities and can cause irreparable damage to close relationships.

Abuse of prescription amphetamines or use of illicit amphetamines are also associated with neurotoxic effects. Chronic amphetamine abuse can cause neurotoxic effects that generally involve brain regions with the highest concentration of the dopamine neurons such as the striatum. This can also result in damage to serotonin neurons in the hippocampus, striatum and the frontal cortex. Amphetamine abuse is often comorbid with other psychological disorders, making it difficult to discriminate the impact of amphetamine abuse on cognitive function and behavior. However, studies suggest side effects include the impairment of memory, executive function and psychomotor functioning.

There has been a concern, however, regarding the use of stimulants such as amphetamine or methylphenidate in children with ADHD. Some of these concerns are related to ADHD being comorbid with substance use disorders and that treatment with amphetamines may increase the risk of addiction in such individuals. However, most studies do not support the association between treatment with amphetamines and substance use disorders, at least when treatment onset is in primary school. The onset of treatment in secondary school, however, increases the chances of developing an addiction. However, this may be due to the relationship between adolescence and drug abuse.

How Long Does Amphetamine Stay in Your System?

The time required by the body to remove a drug or metabolite is measured in terms of the elimination half-life, which is the time required to remove half of the total substance from the body. Amphetamines generally have a half-life between 9 to 14 hours but the amount of time amphetamines remain in the system varies depending on each person’s chemical makeup.

Amphetamines are metabolized by the liver and the metabolites are excreted through urine. Around 30% to 40% of the amphetamine may remain unmetabolized and pass directly through urine.

Testing for amphetamine use is often carried out for employment purposes, sports and to detect an overdose. Some testing methods include taking samples of:

• Blood – Amphetamines remain detectable in blood samples for between 24 and 48 hours
• Urine – Urine samples are the most common method for the detection of drug use. Amphetamines remain detectable in urine for between 1 and 3 days.
• Hair – Amphetamines may be detected in hair samples for up to 90 days, but this mode of detection is expensive and not as common as other testing methods
• Breast milk– Concentration of amphetamines in breast milk tends to be 2.8% to 7.5% higher than that found in blood plasma and may remain in breast milk for up to 24 hours

Is Amphetamine Addictive?

The doses of amphetamines used for the treatment of ADHD are not considered to be addictive, but amphetamines have a high addiction potential at higher doses. Prescription amphetamines should be taken in the prescribed fashion and at the prescribed doses. However, prescription amphetamines are often used by college students in an attempt to improve academic or athletic performance.

Frequent misuse of prescription amphetamines or the use of illicit amphetamines can lead to the development of drug dependence, making it difficult to carry out daily activities without the drug. Chronic use of amphetamines can lead to tolerance, with higher doses of the drug required to produce the desired effects. Discontinuing amphetamine use can lead to withdrawal symptoms involving depression, anxiety and intense cravings.

If you or a loved one struggle with amphetamine addiction, contact The Recovery Village Palm Beach at Baptist Health to speak with a representative about how addiction treatment can help. Take the first step toward a healthier future and call today.