Stimulants such as amphetamine can improve performance on difficult and boring tasks and are used by some students as a study and test-taking aid. This includes noradrenergic neurons in the locus coeruleus, dopaminergic neurons in the ventral tegmental area, histaminergic neurons in the tuberomammillary nucleus, and serotonergic neurons in the dorsal raphe nucleus. Amphetamine’s therapeutic mode of action in narcolepsy primarily involves increasing monoamine neurotransmitter activity in the ARAS. Lateral hypothalamic orexin neurons innervate every component of the ascending reticular activating system (ARAS), which includes noradrenergic, dopaminergic, histaminergic, and serotonergic nuclei that promote wakefulness. Patients with narcolepsy are diagnosed as either type 1 or type 2, with only the former presenting cataplexy symptoms.
Other Medical Problems
Amphetamine withdrawal symptoms can include anxiety, drug craving, depressed mood, fatigue, increased appetite, increased movement or decreased movement, lack of motivation, sleeplessness or sleepiness, and lucid dreams. One review noted that exercise may also prevent the development of a drug addiction by altering ΔFosB or c-Fos immunoreactivity in the striatum or other parts of the reward system. In particular, aerobic exercise decreases psychostimulant self-administration, reduces the reinstatement (i.e., relapse) of drug-seeking, and induces increased dopamine receptor D2 (DRD2) density in the striatum. A 2018 systematic review and network meta-analysis of 50 trials involving 12 different psychosocial interventions for amphetamine, methamphetamine, or cocaine addiction found that combination therapy with both contingency management and community reinforcement approach had the highest efficacy (i.e., abstinence rate) and acceptability (i.e., lowest dropout rate). A systematic review and meta-analysis from 2019 assessed the efficacy of 17 different pharmacotherapies used in randomized controlled trials (RCTs) for amphetamine and methamphetamine addiction; it found only low-strength evidence that methylphenidate might reduce amphetamine or methamphetamine self-administration. One review suggested that, based upon animal testing, pathological (addiction-inducing) psychostimulant use significantly reduces the level of intracellular magnesium throughout the brain.
Mixing amphetamines and other drugs
Do not take other medicines unless they have been discussed with your doctor. The results of some tests may be affected by this medicine. Your risk may be higher if you also take certain other medicines that affect serotonin levels in your body. These may be symptoms of a serious condition called serotonin syndrome. This medicine may cause Raynaud’s phenomenon, which is a problem with blood circulation in the fingers or toes. Do not drive or do anything else that could be dangerous until you or your child know how this medicine affects you.
Amphetamine, specifically the more dopaminergic dextrorotatory enantiomer (dextroamphetamine), is also used recreationally as a euphoriant and aphrodisiac, and like other amphetamines; is used as a club drug for its energetic and euphoric high. At therapeutic doses, the adverse effects of amphetamine do not impede athletic performance; however, at much higher doses, amphetamine can induce effects that severely impair performance, such as rapid muscle breakdown and elevated body temperature. Recreational doses are generally much larger than prescribed therapeutic doses and carry a far greater risk of serious side effects.sources 3 Addiction is a serious risk with heavy recreational amphetamine use, but is unlikely to occur from long-term medical use at therapeutic doses. At therapeutic doses, amphetamine causes emotional and cognitive effects such as euphoria, change in desire for sex, increased wakefulness, and improved cognitive control.
‡IP₃ binds to its receptors on the endoplasmic reticulum to release intracellular Ca²⁺ stores, and together with diacylglycerol activates conventional PKC isoforms. TAAR1 has been identified as a Amphetamine Drug Profile biomolecular target of amphetamine that initiates some of amphetamine’s kinase-dependent signaling cascades. Phosphorylation of DAT by either kinase induces transporter internalization (non-competitive reuptake inhibition), but PKC-mediated phosphorylation alone induces the reversal of dopamine transport through DAT (i.e., dopamine efflux). In parallel, amphetamine also increases intracellular cAMPTooltip cyclic adenosine monophosphate, which activates protein kinase A (PKA) and protein kinase C (PKC), whilst elevated intracellular Ca²⁺ activates PKC alone. As a consequence of DAT uptake, amphetamine produces competitive reuptake inhibition at the transporter. In humans, the only post-synaptic receptor at which amphetamine is known to bind is the 5-HT1A receptor, where it acts as an agonist with low micromolar affinity.
- The medication in each product is absorbed differently by the body, so one amphetamine product cannot be substituted for another product.If you are switching from one product to another, your doctor will prescribe a dose that is best for you.
- The pharmacokinetics of lisdexamfetamine are similar regardless of whether it is administered orally, intranasally, or intravenously.
- However, oral suspension and orally disintegrating tablet (ODT) dosage forms composed of the free base were introduced in 2015 and 2016, respectively.
- In organic chemistry, amphetamine is an excellent chiral ligand for the stereoselective synthesis of 1,1′-bi-2-naphthol.
- Conversely, an acidic pH means the drug is predominantly in a water-soluble cationic (salt) form, and less is absorbed.
- Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur.
Detection in body fluids
If you have been using this medicine for a long time and you think you may have become mentally or physically dependent on it, check with your doctor right away. Blood tests and blood pressure tests may be needed to check for unwanted effects. It is very important that your doctor check your or your child’s progress at regular visits to make sure the medicine is working properly. Ask your healthcare professional how you should dispose of any medicine you do not use. Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light.
Drug interactions
The adverse side effects of amphetamine are many and varied, and the amount of amphetamine used is the primary factor in determining the likelihood and severity of adverse effects. Evidence from human studies indicates that therapeutic amphetamine use does not cause developmental abnormalities in the fetus or newborns (i.e., it is not a human teratogen), but amphetamine abuse does pose risks to the fetus. These agencies also state that anyone with anorexia nervosa, bipolar disorder, depression, hypertension, liver or kidney problems, mania, psychosis, Raynaud’s phenomenon, seizures, thyroid problems, tics, or Tourette syndrome should monitor their symptoms while taking amphetamine. Food and Drug Administration (FDA),note 9 amphetamine is contraindicated in people with a history of drug abuse,note 10 cardiovascular disease, severe agitation, or severe anxiety.
Recreational use of amphetamine generally involves much larger doses, which have a greater risk of serious adverse drug effects than dosages used for therapeutic purposes. As amphetamines affect the way the brain processes dopamine naturally, cessation can cause uncomfortable withdrawal symptoms. Here we look at the types of amphetamines, their effects, potential for addiction, and treatment options.
You might be hesitant to use one because the word “amphetamine” can carry negative connotations. Your healthcare provider can tell you more about how long you should wait after taking your medication before it’s OK to drink alcohol. You shouldn’t drink alcohol too soon after taking an amphetamine. Make sure your healthcare provider knows about every medication, herbal remedy or supplement you take. They can also tell you which side effects need immediate care and which can wait for an appointment. Your healthcare provider or pharmacist can tell you more about possible or likely side effects.
Amphetamine prescription shortages
Dextroamphetamine, marketed under the brand names Dexedrine and Zenzedi, is the only enantiopure amphetamine product currently available. Of those, Evekeo (including Evekeo ODT) is the only product containing only racemic amphetamine (as amphetamine sulfate), and is therefore the only one whose active moiety can be accurately referred to simply as “amphetamine”. Several currently marketed amphetamine formulations contain both enantiomers, including those marketed under the brand names Adderall, Adderall XR, Mydayis,note 1 Adzenys ER, Adzenys XR-ODT, Dyanavel XR, Evekeo, and Evekeo ODT. As a result of the United Nations 1971 Convention on Psychotropic Substances, amphetamine became a schedule II controlled substance, as defined in the treaty, in all 183 state parties. Outside Europe, the illicit market for amphetamine is much smaller than the market for methamphetamine and MDMA. During 2012, approximately 5.9 metric tons of illicit amphetamine were seized within EU member states; the “street price” of illicit amphetamine within the EU ranged from €6–38 per gram during the same period.
Medical Professionals
An amphetamine overdose can lead to many different symptoms, but is rarely fatal with appropriate care. The few studies that have used equivalent (weight-adjusted) human therapeutic doses and oral administration show that these changes, if they occur, are relatively minor. Chronic use of amphetamine at excessive doses causes alterations in gene expression in the mesocorticolimbic projection, which arise through transcriptional and epigenetic mechanisms. Exercise therapy improves clinical treatment outcomes and may be used as an adjunct therapy with behavioral therapies for addiction.sources 10
The reinforcing and motivational salience-promoting effects of amphetamine are due mostly to enhanced dopaminergic activity in the mesolimbic pathway. A Cochrane review on treatment for amphetamine, dextroamphetamine, and methamphetamine psychosis states that about 5–15% of users fail to recover completely. An amphetamine overdose can result in a stimulant psychosis that may involve a variety of symptoms, such as delusions and paranoia. Tolerant individuals have been known to take as much as 5 grams of amphetamine in a day, which is roughly 100 times the maximum daily therapeutic dose.
- Evidence suggests that lisdexamfetamine’s treatment efficacy in BED is underpinned at least in part by a psychopathological overlap between BED and ADHD, with the latter conceptualized as a cognitive control disorder that also benefits from treatment with lisdexamfetamine.
- No information is available on the relationship of age to the effects of amphetamine tablets in geriatric patients.
- This medicine may cause slow growth and weight loss.
- In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do.
Dextroamphetamine also activates TAAR1 in peripheral organs along the gastrointestinal tract that are involved in the regulation of food intake and body weight. The pathophysiology of BED is not fully understood, but it is believed to involve dysfunctional dopaminergic reward circuitry along the cortico-striatal-thalamic-cortical loop. Stimulants like methylphenidate and amphetamine are effective in treating ADHD because they increase neurotransmitter activity in these systems. Another review indicated that, based upon the longest follow-up studies conducted to date, lifetime stimulant therapy that begins during childhood is continuously effective for controlling ADHD symptoms and reduces the risk of developing a substance use disorder as an adult. Randomized controlled trials of continuous stimulant therapy for the treatment of ADHD spanning 2 years have demonstrated treatment effectiveness and safety.
Amphetamine addiction is largely mediated through increased activation of dopamine receptors and co-localized NMDA receptorsnote 14 in the nucleus accumbens; magnesium ions inhibit NMDA receptors by blocking the receptor calcium channel. Consequently, ΔFosB is the most significant factor involved in both amphetamine addiction and amphetamine-induced sexual addictions, which are compulsive sexual behaviors that result from excessive sexual activity and amphetamine use. Similarly, accumbal G9a hyperexpression results in markedly increased histone 3 lysine residue 9 dimethylation (H3K9me2) and blocks the induction of ΔFosB-mediated neural and behavioral plasticity by chronic drug use,sources 12 which occurs via H3K9me2-mediated repression of transcription factors for ΔFosB and H3K9me2-mediated repression of various ΔFosB transcriptional targets (e.g., CDK5). Less common side effects include anxiety, change in libido, grandiosity, irritability, repetitive or obsessive behaviors, and restlessness;sources 9 these effects depend on the user’s personality and current mental state. However, amphetamine pharmaceuticals are contraindicated in individuals with preexisting cardiovascular disease.sources 8
Since the first preparation was reported in 1887, numerous synthetic routes to amphetamine have been developed. The class includes amphetamine itself, stimulants like methamphetamine, serotonergic empathogens like MDMA, and decongestants like ephedrine, among other subgroups. In organic chemistry, amphetamine is an excellent chiral ligand for the stereoselective synthesis of 1,1′-bi-2-naphthol.
You may take this medicine with or without food or liquid. It is best to take this medicine when you wake up in the morning. This medicine should come with a Medication Guide. If too much of this medicine is taken, it may become habit-forming (causing mental or physical dependence). Take this medicine exactly as directed by your doctor. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
This medication may be prescribed for other uses; ask your doctor or pharmacist for more information. Do not add the extended-release suspension (Adzenys® ER) to food or mix it with other liquids. It works by changing the amounts of certain natural substances in the brain. Selling or giving away amphetamine may harm others and is against the law. Do not sell, give away, or let anyone else take your medication. If you suddenly stop taking amphetamine after overusing it.
