DESCRIPTION / DEFINITIONS: Concerta® is methylphenidate hydrochloride, a central nervous system (CNS) stimulant prescribed for the set of symptoms known as Attention Deficit Hyperactivity Disorder. It is prescribed to children from 6 years old through adults aged 65.
ABUSE: Concerta has a high potential for abuse. A black box warning – the most serious of cautions by the FDA – is included in the label information.
ADDICTION / DEPENDENCE: The FDA warns that abuse of and dependence on Concerta can be quite severe. See additional information and black box warning below.
SIDE EFFECTS: The FDA boxed warning cautions us about effects such as glaucoma, serious cardiovascular events, the potential for gastrointestinal blockages, and ‘frank psychotic episodes’. See more below.
WITHDRAWAL SYMPTOMS: Depression, disturbed sleep patterns, nightmares, and suicidal thoughts are among the potential symptoms experienced during withdrawal. See more below.
TREATMENT: Treatment is dependent upon how much Concerta you’ve been taking and for how long as well as how each individual reacts to the drug, and to withdrawal. See more information below.
The active ingredient in Concerta is methylphenidate, the same as Ritalin. However, the Concerta formulation is extended release, whereas Ritalin is available in both immediate release and extended. Concerta is used primarily to control the set of symptoms known as Attention Deficit Hyperactivity Disorder (ADHD).
Concerta, and similar drugs, is abused in several ways:
- As Concerta is a stimulant that can improve focus, concentration, alertness and energy, it is abused as a study drug.
- Concerta also suppresses appetite and so is used for weight loss.
- Also, because it activates the reward system in the brain – meaning that it increases the production of dopamine, a neurotransmitter – Concerta is also used to get high.
Concerta is chemically very similar to cocaine and amphetamine, and is therefore highly addictive.
Concerta labels bear the following black box warning:
WARNING: DRUG DEPENDENCE
Concerta® should be given cautiously to patients with a history of drug dependence or alcoholism. Chronic abusive use can lead to marked tolerance and psychological dependence with varying degrees of abnormal behavior. Frank psychotic episodes can occur, especially with parenteral (not taken by mouth and going through the digestive track) abuse. Careful supervision is required during withdrawal from abusive use since severe depression may occur. Withdrawal following chronic therapeutic use may unmask symptoms of the underlying disorder that may require follow-up.
HALF LIFE AND METABOLISM
The biological half life of a substance is the time it takes for a drug to lose half of its pharmacologic activity. This is significant because it affects how soon withdrawal symptoms may appear.
The half-life of methylphenidate in adults and adolescents following oral administration of CONCERTA was approximately 3.5 hours when tested.
Methylphenidate is metabolized primarily by de-esterification to α- phenyl-piperidine acetic acid (PPA or PPAA), which has little or no pharmacologic activity. In adults the metabolism of CONCERTA once daily as evaluated by metabolism to PPA is similar to that of methylphenidate three times a day. The metabolism of single and repeated once-daily doses of CONCERTA is similar.
The following side effects are taken from the Concerta label:
- abdominal discomfort
- abdominal pain
- accommodation disorder – the ability of the eye to change its focus from distant to near objects and vice versa
- affect lability – exaggerated changes in mood or emotions in quick succession
- alanine aminotransferase increased – liver enzymes that indicate Inflamed or injured liver cells
- asthenia – abnormal physical weakness or lack of energy
- blood pressure increased
- bruxism – teeth grinding, especially during sleep
- cardiac murmur
- confusional state
- decreased appetite
- depressed mood
- dry eye
- dry mouth
- dyspnea – difficult or labored breathing
- dyspepsia – indigestion
- erectile dysfunction
- feeling jittery
- heart palpitations
- heart rate increased
- hot flush
- hyperhidrosis – excessive sweating of the palms, soles, groin, face or head, and armpits. Generally an indication of an underlying health problem, or a side effect of drugs.
- hypervigilance – a state of increased alertness, often associated with PTSD, anxiety disorders, and schizophrenia.
- leucopenia – reduction in the number of white blood cells
- libido decreased
- macular rash – a rash with flat, red lesions about one centimeter in diameter
- mood altered
- mood swings
- muscle spasms
- muscle tightness
- nasopharyngitis – colds, or upper respiratory tract viral or bacterial infections
- opropharyngeal pain – pain when swallowing
- pain in the upper abdomen
- panic attack
- paresthesia – tingling or pricking (“pins and needles”), caused chiefly by pressure on or damage to peripheral nerves.
- psychomotor hyperactivity – feelings of extreme restlessness accompanied by muscle spasms, tremors, twitching, pacing, crossing and uncrossing the legs and other nervous activity.
- pyrexia – fever
- sleep disorder
- suicidal thoughts
- tension headache
- upper respiratory tract infection
- vision blurred
- weight loss
After Concerta was approved by the FDA and the drug was on the market, the following adverse reactions were also reported:
- acute hepatic failure – liver failure
- alopecia – hair loss
- anaphylactic reactions – a severe, potentially life-threatening allergic reaction which causes hives, itching, flushed or pale skin, low blood pressure, constriction of your airways and a swollen tongue or throat, which can cause wheezing and trouble breathing, a weak and rapid pulse, nausea, vomiting or diarrhea, dizziness or fainting
- angina pectoris
- arthralgia – pain in the joints
- auricular swelling – swelling related to the ear
- blood alkaline phosphatase increased – may indicate a problem with your liver or gallbladder. This could include hepatitis (liver inflammation), cirrhosis (liver scarring), liver cancer, gallstones, or a blockage in your bile ducts.
- blood bilirubin increased – a symptom of the red blood cells breaking down
- bradycardia – abnormally slow heart action
- bullous conditions
- chest discomfort
- chest pain
- diplopia – double vision
- drug effect decreased
- dyskinesia – impairment of voluntary movements resulting in fragmented or jerky motions (as in Parkinson’s disease)
- erythema – superficial reddening of the skin, usually in patches, as a result of injury or irritation causing dilatation of the blood capillaries.
- exfoliative conditions – redness and scaling of the skin that begins in patches and spreads
- extrasystoles – a heartbeat outside the normal rhythm
- grand mal convulsion
- hallucination auditory
- hallucination visual
- hepatocellular injury – a type of liver injury
- hyperpyrexia – fever above 106.7 degrees Fahrenheit
- hypersensitivity reactions such as angioedema
- libido changes
- logorrhea – excessive and often incoherent talkativeness or wordiness
- muscle twitching
- myalgia – pain in a muscle or group of muscles
- mydriasis – dilation of the pupil of the eye
- pancytopenia – deficiency of all three cellular components of the blood (red cells, white cells, and platelets
- platelet count decreased – platelets are colorless blood cells that help blood clot
- pruritus – itching
- Raynaud’s phenomenon
- rhabdomyolysis – destruction of certain types of muscles associated with various areas in the body, including skeletal muscle and heart muscle.
- serotonin syndrome in combination with serotonergic drugs – serotonin syndrome is a group of side effects that include high body temperature, agitation, increased reflexes, tremor, sweating, dilated pupils, and diarrhea, associated with serotonergic drugs. Serotonergic drugs are used to treat migraine headaches, depression and other difficulties with mood. The symptoms are experienced when these drugs are mixed with Ritalin.
- supraventricular tachycardia – an abnormally fast heart rhythm arising from improper electrical activity in the upper part of the heart.
- therapeutic response decreased
- thrombocytopenia – deficiency of platelets in the blood. This causes bleeding into the tissues, bruising, and slow blood clotting after injury.
- thrombocytopenic purpura – a bleeding disorder in which the immune system destroys platelets, which are necessary for normal blood clotting.
- urticarias – urticaria is a rash of round, red welts on the skin that itch intensely, sometimes with dangerous swelling, caused by an allergic reaction, typically to specific foods.
- visual impairment
- white blood cell count abnormal
Concerta withdrawal is often referred to as the “crash.” Withdrawal symptoms vary depending on the severity of addiction, what dosage the person has been taking, and for how long. Long-term use of Concerta and taking higher doses often result in more severe and longer-lasting withdrawal symptoms. It is best to quit taking Concerta under medical supervision.
According to the National Institute on Drug Abuse, common symptoms of Concerta withdrawal include:
- chronic and/or extreme fatigue
- disturbed sleep patterns
- increased appetite
- lowered heart rate
- moderate to severe depression
- suicidal thoughts
- vivid dreams
It’s important to consult with a medical professional before quitting Concerta. How long it will take to go through the withdrawal period, how severe it will be, and how long it will take for life to get back to normal depends on how long a person has been taking the drug and at what dosage, as well as how the individual reacts to the drug and going off it. The medical practitioner may suggest that the person wean off the drug, gradually decreasing the dosage as directed. But there are times when a doctor may suggest a medical detox facility.