A comprehensive overview of methylphenidate hydrochloride, commonly known by brand names like Ritalin and Concerta, which is used for treating Attention Deficit Hyperactivity Disorder (ADHD). It traces the history of Ritalin, starting with its synthesis by chemist Leandro Panizzon and its early use by his wife Marguerite.
Methylphenidate hydrochloride, with the brand names: Ritalin, Concerta, Delmosart, Equasym, Tranquilin, Xaggitin, Xenidate, and Medikinet,etc., is a stimulant used to treat Attention Deficit and Hyperactivity Disorder (ADHD). Slow- release tablets are taken 1x per day, standard release capsules or tablets may be taken 3x a day.
Ritalin was named after the wife of a chemist Leandro Panizzon, who synthesised methylphenidate at Cibas laboratories in Basel. He tested it on his wife Marguerite (nicknamed “Rita”). And she rapidly noticed the effects. Rita felt the most significant changes while playing tennis, as her game improved after taking the drug. The molecule acts quickly on the nervous system and improves concentration. A patent was filed, and methylphenidate was marketed to combat fatigue and confusion. 1
I shall use the brand name of Ritalin from hence forth, while referring to any forms of methylphenidate hydrochloride, prescribed for ADHD.
Ritalin is a benzylpiperidine and phenethylamine derivative which also shares part of its basic structure with catecholamines. Methylphenidate is a psychostimulant and increases the activity of the central nervous system through inhibition on reuptake of the neurotransmitters norepinephrine and dopamine.
Aggression (or hostility); alopecia; anxiety; appetite decreased; arrhythmias; arthralgia; asthenia; behaviour abnormal; cough; depression; diarrhoea; dizziness; drowsiness; dry mouth; feeling jittery; fever; gastrointestinal discomfort; growth retardation (in children); headaches; hyperhidrosis; hypertension; increased risk of infection; laryngeal pain; mood altered; movement disorders; muscle complaints; nausea; oropharyngeal pain; palpitations; paraesthesia; sexual dysfunction; skin reactions; sleep disorders; thirst; tic; toothache (in adults); vertigo; vision disorders; vomiting; weight decreased
Angioedema; chest discomfort; constipation; dry eye; dyspnoea; haematuria; hallucinations; hot flush; psychotic disorder; speech impairment; suicidal behaviours; tremor; urinary disorders
Anaemia; angina pectoris; cardiac arrest; cerebrovascular insufficiency; confusion; gynaecomastia; hepatic coma; hepatic disorders; hyperfocus; leucopenia; mydriasis; myocardial infarction; neuroleptic malignant syndrome; peripheral coldness; Raynaud's phenomenon; seizures; sudden cardiac death; thinking abnormal; thrombocytopenia
Delusions; drug dependence; hyperpyrexia; intracranial haemorrhage; pancytopenia; trismus (in adults); vasculitis. 3
The story of Ritalin begins with Dr. Charles Bradly, who on the eve of the Great Depression became a Medical Director at the Emma Pendleton Bradley Home for the treatment of children. The Home had been set up by his great uncle, George Bradly, who had made a fortune with Alexander Graham Bell and his telephone business. 4
The Home was filled with children from impoverished backgrounds who were subjected to 'treatments' such as pneumoencephalography5 (also referred to as an 'air study'), in which most of the cerebrospinal fluid (CSF) was drained from around the brain by means of a lumbar puncture and replaced with air, oxygen, or helium to allow the structure of the brain to show up more clearly on an X-ray image- (only it didn't). During the study, the child's body would be rotated into different positions in order to allow air to displace the CSF. The child would be strapped into an open backed chair which allowed the spinal needle to be inserted. The chair would be rotated upside down and then somersaulted into a face down position in a specific order to follow the air to different areas in the ventricles. The children suffered from headaches and severe vomiting from this procedure, which could last up to 2-3 months. More severe side effects included permanent brain damage and paralysis. Pneumoencephalography was only abandoned in the 1970s.
In the mid- thirties, American pharmaceutical company, Smith Kline and French (SKF, now GlaxoSmithKline) was scouting around for ways to increase revenue from its over- the counter nasal decongestant Benzedrine, active ingredient of which was amphetamine. They offered free supplies to any doctor willing to conduct research to expand their market. Benzedrine worked as a nasal decongestant because it constricted nasal mucus membranes. Bradley thought that perhaps it might help with the headaches in the CSF-drained children by constricting the brain membrane. He conducted a 3-week study in 1937 with 30 children and found that the drug did nothing to cure the headache, but the kids were better behaved: calmer, more focussed and performed much better at school. Bradly expanded his trial to 100 children in 1941 and the results were undeniable- children's behaviour improved as long as they were taking the drug, but as soon as they stopped, the behaviour reverted. It was not so much a cure as a very effective daily treatment.
SKF got the idea to market amphetamine to school kids to improve academic performance. Meanwhile reports begun to appear that people were becoming addicted to Benzedrine, and some even had psychotic episodes. The 'speed' addicts begun to pry open the nasal decongestants, and either eating or injecting the amphetamine. Hence, the idea of marketing amphetamine to school children was canned for a while. Luckily for SKF though, the Second World War broke out and the US Military begun to place large orders for amphetamine, since they discovered that it helps with combat fatigue and PTSD, removes fear and anxiety, and fills them with confidence. The US Military called them Bennies.
Amphetamine was not used again on children till 1950s, when the term 'hyperactivity' was first coined by the psychiatrists to label misbehaving kids.
Bradley's successor at The Home was Dr. Maurice Laufer, who begun to use the newly released Ritalin to treat hyperactive children. By 1960s Ritalin became a mainstream treatment for 'hyperactivity' in children. Currently, the Ritalin market is netting American pharmaceutical companies about $13b.
The latest version of the Diagnostic and Statistical Manual of Mental Disorders (DSM) is the DSM-5-TR, which was published in March 2022. In it, ADHD has been acknowledged as a neurodevelopmental disorder, even though it is admitted that 'discoveries that could confirm ADHD as a neurodevelopmental disorder have not yet materialised', and they admit, that 'no biological marker is diagnostic for ADHD'. 'Moreover, the DSM-5-TR includes a new and very interesting statement in the “Prevalence” section: “prevalence is higher in special populations such as foster children or correctional settings”'6 - perhaps it is worth looping back to the story of children in the Emma Pendleton Bradley Home- all from very low socio-economic and troubled backgrounds. I tend to agree with Koutsoklenis and Honkasilta: 'We conclude that DSM's latest edition does not escape the logical and scientific pitfalls of its predecessor. DSM-5-TR keeps the faith in the neo-Kraepelinian paradigm by explicitly and implicitly cultivating the essentialist medical scientific metaphor of disorder, creating the illusion that it represents scientific progress that validates ADHD as a neurodevelopmental disorder.'
Homeopathy is a good method to treat the underlying cause of the symptoms in children with the sc. ‘hyperactivity’ disorder. Read more in Judyth Reichenberg-Ullman and Robert Ullman’s book: Ritalin Free Kids: Safe and Effective Homeopathic Medicine for ADD and Other Behavioral and Learning Problems.