Chemistry of Adderall Amphetamines These

Chemistry of Adderall Amphetamines These compounds were first synthesized in 1887 by Lazar Edeleanu at the University of Berlin (Harrison 2007). He initially called them "phenylisopropylamine." These were among the first series of compounds purified two years earlier by Nagayoshi Nagai. They were related to the plant derivative ephedrine. The pharmacological use of amphetamine was not discovered until 1927 when Gordon Alles re-synthesized it. He was in a group in search for a substitute for ephedrine.

Amphetamine became known in the form of pharmaceutical Benzedrine then used by soldiers in several countries at war. It was prescribed to ward off fatigue and increase alertness. German soldiers took a lot of the derivative methamphetamine during World War II. In response to reported abuse of the drug, the FDA banned Benzedrine inhalers and limited the prescription of amphetamines in 1959. Its illegal use, however, persisted (Harrison).

Progenitor for ADHD The history of adderall is bound up with the development in the search for the treatment of Attention Deficiency Hyperactivity Disorder or ADHD. Dr. Charles Bradley was the first doctor to prescribe Benzedrine, a psychostimulant, to treat hyperactive children (Logan 2011 web p 1). That was in 1937 and his discovery was to be left unnoticed for the next 20 years. In the last three decades, ADHD became better known and gathered much interest. However, the disorder remained a mystery for a longer time.

In 1957, methylphenidate -- otherwise known as Ritalin -- was approved for the treatment of hyperactive children. ADHD was then regarded only as a "minimal brain dysfunction" until its name was changed into "hyperkinetic disorder" in the 1960s. Another drug, dextroamphetamine -- also known as Dexedrine -- was then introduced as treatment of the disorder (Logan). The American Psychiatric Association officially recognized ADHD in 1980 and included it in the third edition of the Diagnostic and Statistical Manual of Mental Disorders (Logan 2011 web p 1).

In 1996, an amphetamine, known as Obetrol, was renamed into Adderall upon obtaining FDA approval. It was previously used to treat obesity (Logan). The manufacturer of both Obetrol was Shire Pharmaceutical, a UK-based pharmaceutical company (Shire 2011). Improvements and Difficulties In 1992, Shire Pharmaceuticals (2011) entered into big ventures to strengthen its product lines and enhance its capabilities at creating products for specialty physicians. It runs two divisions to fulfill these ends. One division, the Specialty Pharmaceuticals Division and the Human Genetics Therapies Division, focuses on small-molecule medications for the treatment of ADHD.

Adderall consists of the salts dextroemphetamine saccahrate, dextroamphetamine sulfate, dl-amphetamine aspartate, and del-amphetamine sulfate. When the U.S. Congress passed the Controlled Substance Act in 1970, amphetamines were among those categories as Schedule II drugs (Geist 2007). Schedule II drugs are those with high potential for abuse that leads to severe psychological or physical dependence. Examples of these drugs are cocaine, opium and morphine. Four decades later today, various forms of amphetamines are prescribed every year to 1.5 million children for various conditions in the United States alone.

How amphetamines have been used calls for reforms in the approval and regulation of drugs by the FDA. Adderall sets the stage for those reforms (Geist). Chemical Process Amphetamine is a prescription stimulant consists of dextroamphetamine and l-amphetamine (Harrison 2007). It is believed to produce effects when it binds to monoamine transporters and raise extracellular levels of the biogenic amines dopamine, norepinephrine and serotonin. D-amphetamine is believed to act on the dopamiergic systems and the l-amphetamine on the norepinephrinergic systems.

Adderall is made up of the four salts dextroamphetamine saccharate, dextroamphetamine sulfate, amphetamine aspartate monohydrate and amphetatmine sulfate. These are in a racemic mixture of equal amounts of left-and-right-handed isomers (Harrison). Amphetamines are psycho-stimulant drugs, called phenethylamines, which stimulate psychological and physiological functions (Collier 2008). This happens when the drug increases the levels of dopamine and norepinephrine neurotransmitters in the brain. Amphetamines have proven medical benefits but are also highly potential for recreational abuse. They are quite addictive because of the euphoria they produce as one of their major side effects.

This occurs in the case of excessive recommended medical dosage (Collier). Both Adderall and Adderall RX contain the same combo and have identical composition, except that the XR is released at a different amount of time (Geist 2007). The inclusion of levoamphetamine provides quicker start and longer clinical effect in comparison with other drugs with only dextroamphetamine (Add Forums 2004, NCBI 2005). The human brain has been observed to have a preference for dextroamphetamine over levoamphetamine. The main reinforcing and behavioral and stimulant effect seems to be primarily in the mesolimbic dopaminergic pathway.

Amphetamine binds to dopamine transporter and blocks the transporter's ability to eliminate dopamine from the synaptic space. Amphetamine is also brought to the cell and leads to dopamine efflux (Geist, Add Forums, NCBI). The ingredients and proportions of Adderall instant release and Adderall XR are identical (NeuroChi 2001). Adderall XR is, however, delivered through the Microtrol system in order to assert the extended-release action. This delivery system consists of a capsule full of beads. Each bead contains part of the medication.

Half of all the beads are formulated to dissolve immediately and half are released four hours later. The mechanism brings the maximum plasma concentration to seven hours. Immediate-release Adderall reaches that concentration in three hours (NeuroChi). Amphetamine is also able to inhibit the enzymes monoamine oxidase A and B. when taken in high doses (Geist 2007). The first enzyme is responsible for the breakdown of dopamine, norepinephrine, and epinephrine. The second is responsible for the breakdown of dopamine more than the first enzyme is and of phenylethylamine.

Phenylethylamine asserts similar actions as amphetamine itself. It is believed to produce feels of lust, confidence, obsession and sexuality. Some earlier anti-depressants are, in fact, inhibitors of this enzyme. In summary, the effect of amphetamines is to increase neurotransmitter availability in the synapse. They do this by releasing more neurotransmitters and prolonging the availability in the synapse and slowing down their elimination (Geist).

Shire claims that the combination of the four salts in Adderall provides a smoother rise and fall of effects as compared with a single-salt formulation in that the four salts are metabolized at different rates (NeuroChi 2011). It says that the average body nation of dextroamphetamine is 10 hours in adults and 13 hours for levoamphetamine in the company's immediate release formulation. But little evidence supports the claims. A recent patent application for the drug was listed as for a rapid immediate release oral dosage form.

There was no claim for an increased or smooth drug delivery. Findings of a recent, double-blind placebo-controlled crossover study showed that the respondent children behaved similarly towards other immediate-release amphetamines. It found that the sustained-release dexamphetamine had longer action and was cheaper than Adderall. Dexamphetamine was less effective than Adderall in the first few hours. Nonetheless, no evidence was provided with certainty that the mixture provides smoother start and decline of effects (Neuro Chi).

Properties of Molecules Dextroamphetamine has a molecular weight of 368.49092 g/mol; molecular formula C18H28N204S; H-Bond Donor 4; H-Bond Acceptor 6; Rotatable Bond Count 4; Exact Mass of 368.176978; monoisotopic mass of 368.176978; topological polar surface area of 135; heavy atom count of 25; 166 complexity defined atom stereocenter count of 2; and.