Last reviewed by Miljan Krcobic on August 18th, 2018.
What is Focalin?
Focalin is the name of a drug product which contains dexmethylphenidate hydrochloride as an active ingredient. Focalin is the brand name of the drug while the pharmacologically active ingredient which is present in the formulation is dexmethyphenidate hydrochloride. It acts on the central nervous system and stimulates it. The drug is used primarily for the treatment of attention deficit hyperactive disorder (ADHD).
Focalin is a drug which is available on the prescription of a registered medical practitioner. It stimulates the central nervous system therefore it belongs to the class of central nervous system stimulants.
It normally works by altering the levels of neurotransmitters in the brain which primarily includes norepinephrine and dopamine and the drug usually acts by increasing the levels of these chemicals. The drug may also be used by patients of narcolepsy for alleviating the symptoms.
Chemistry ad identification of Focalin
Focalin is a drug which consists of dexmethylphenidate hydrochloride as an active ingredient. This pharmacologically active ingredient is responsible for the beneficial effects of the drug. Each tablet consists of dexmethylphenidate hydrochloride which is taken orally.
Focalin’s active ingredient dexmethylphenidate hydrochloride IUPAC name, molecular structure, weight, formula and drug class
IUPAC name: methyl (2R)-2-phenyl-2-[(2R)-piperidin-2-yl]acetate;hydrochloride
Molecular formula: C14H20ClNO2
Molecular weight: 269.769 g/mol
Drug class: This compound belongs to the class of organic compounds known as aralkylamines. These are alkylamines in which the alkyl group is substituted at one carbon atom by an aromatic hydrocarbyl group.
Focalin which consists of dexmethylphenidate hydrochloride is an enantiomer of the racemic mixture of methylphenidate hydrochloride. This racemic mixture is a 50/50 mixture of two enantiomers namely d-threo and l-threo enantiomerof which Focalin is a d-threoenantiomer.
The drug acts as a stimulant of the central nervous system and is available as tablet dosage form in 3 strengths. Each tablet consists of dexmethylphenidate hydrochloride 2.5, 5 or 10 mg which is taken orally. This CNS stimulant is chemically described asmethyl α- phenyl-2-piperidineacetate hydrochloride, (R,R’)-(+)- having a molecular weight of 269.77 g/mol.
The colour of dexmethylphenidate hydrochloride is white to off-white and is in powder form. It forms acidic solutions. It is only slightly soluble in organic solvents like chloroform and acetone while it is freely soluble in water and alcohols like methanol. Focalin is a combination of pharmacologically active ingredients as well as pharmaceutical excipients. These excipients are inert and pharmacologically inactive in nature.
What are the active and inactive ingredients of Focalin?
Focalin is a mixture of pharmacologically active and inactive ingredients. The active ingredient is dexmethylphenidate hydrochloride which possesses the pharmacological activity while the inactive ingredients include pregelatinized starch, lactose monohydrate, sodium starch glycolate, microcrystalline cellulose, magnesium stearate, and dyes including FD&C Blue No.1 #5516 aluminium lake (present in 2.5 mg tablets), D&C Yellow lake #10 (present in 5 mg tablets) while the 10 mg tablets do not contain any dye.
What is the mechanism of action of Focalin?
The active ingredient in the drug is dexmethylphenidate hydrochloride which is a synthetic amine having sympathomimetic properties and also stimulates the central nervous system. It increases the release of neurotransmitters particularly norepinephrine and dopamine in the brain and also prevents their uptake.
This leads to an increase in the motor activity resulting in excitement, euphoria, mental alertness and suppression of appetite. Therefore, the drug is primarily used in attention deficit hyperactive disorder while it may also be used for the treatment of fatigue and other nervous system effects resulting from chemotherapy.
How should Focalin be taken?
- Focalin is a prescription drug and should be taken as prescribed by the doctor. The doctor may need to adjust the dose according to the condition of the patient.
- The tablets are usually taken 2 times a day such that the total daily dose should not exceed 20 mg for immediate release tablets and should not exceed 40 mg for extended release dosage form.
- The doses should be taken with an interval of at least 4 hours.
- The patients who are new to the drug or those receiving other CNS stimulants should be given 5 mg per day. Dose may be adjusted on weekly basis and can be increased to a maximum of 20 mg per day.
- The drug can be taken with or without food.
- It is not recommended to take a dose at night as the drug causes insomnia.
- The medication may result in blurred vision and may also alter the thinking process so caution must be taken if the patient needs to drive or do some work requiring alertness.
- The doctor may stop the drug for short intervals to check the progress of the condition of the patient suffering from ADHD.
- If the drug causes adverse events in patients or if the symptoms are aggravated then dose should be adjusted but if this adjustment does not prove to be beneficial then the use of the drug should be discontinued.
What if a dose of Focalin is missed?
In case a person forgets to take the drug and a dose is missed, the patient is advised to take the dose as soon as he remembers it. It is not advisable to take the dose late in the day as the drug may cause insomnia so it might be difficult to sleep.
In such cases, it is advisable to skip the dose and patient should continue with the prescribed dosing schedule. Moreover, doubling of the dose at a single time to make up for the missed dose is not recommended.
Description of dosage form and available strengths
Focalin is supplied as D shaped tablets. The tablets are 18 mm in size. The tablets have a “D” impression on the upper surface while the strength of the tablet is on the lower surface. The tablets are taken orally and are supplied in bottles of 100 tablets. Focalin is available on 3 different dosage strengths.
- 5 mg tablets – blue
- 5 mg tablets – yellow
- 10 mg tablets – white
What are the indications of Focalin?
The primary indication in which Focalin is prescribed is attention deficit hyperactive disorder. It is also included in the total treatment programme for patients with ADHD along with other physiological, educational and social measures which are taken for the treatment of patients with this disorder.
Pharmacokinetics of Focalin
Absorption and distribution:
Upon oral administration of Focalin, dexmethylphenidate hydrochloride is readily absorbed from the gastrointestinal tract. The drug undergoes extensive first pass metabolism due to which the mean absolute bioavailability is 22 to 25%. When the drug is administered orally to patients with ADHD, plasma concentrations of dexmethylphenidate increase rapidly and reach to a maximum concentration within 60 to 90 minutes.
Since the pharmacokinetics of the drug are not altered followed by single or twice daily dosing, this indicates that the drug does not accumulate significantly in children with ADHD.When the drug is administered to children in single doses of 2.5 mg, 5 mg or 10 mg in the form of capsules, Cmaxand AUC0-inf of the drug were proportional to the dose.
Although the drug can be taken with or without food, a meal which is rich in fat might slow the absorption of the drug but does not affect the extent of absorption and even the peak concentration of the drug. There are also variations in the absorption patterns between men and women as AUC is higher in women as compared to men. When compared with children, AUC is lower as compared to adults.
It is not exactly known whether the drug enters breast milk or crosses placenta but upon oral administration the plasma concentrations show an exponential decline in children.
Metabolism and excretion:
The drug is metabolized in the liver by a process called de-esterification. This process metabolizes dexmethylphenidate to d-α-phenyl-piperidine acetic acid which is also known as d-ritalinic acid. This metabolite does not possess any pharmacological activity. Upon the oral administration of the radiolabelled methylphenidate, 90% of the radioactivity was recovered in urine.
Therefore, the drug is eliminated primarily in urine in the form of ritalinic acid. This metabolite of the drug is responsible for 80% of the dose as the drug is not excreted unchanged in urine but in the form of the metabolite. The drug neither induces nor inhibits the cytochrome P450 isozymes in the liver. The mean plasma elimination half-life of the drug is 2 to 3 hours in children while 2 to 4.5 hours in adults.
Side effects of Focalin
The drug may cause common to serious side effects. Many of these effects may be eliminated by the discontinuation of the drug. Following are some of the serious side effects which might need immediate medical attention, caused by Focalin:
- chest pain
- shortness of breath
- extreme fatigue
- fast, pounding or irregular heartbeat
- changes in vision
- slow or difficult speech
- dizziness or fainting
- aggressive behaviours
- weakness or numbness in the arm or leg
- having suspicion for others
- hallucinations or believing false things
- mood changes
- swelling of the face, tongue, lips, throat, or eyes
- rash, hives, or itching
- purples blotches under the skin
- joint pain
- blistering or peeling skin
- painful and frequent erections
- having erections for more than 4 hours
- numbness, pain, or sensitivity of temperature in the fingers and toes
- changes in skin colour in the fingers and the toes
Common side effects caused by Focalin include:
- weight loss and loss of appetite
- pain in the stomach, nausea, and heartburn
- dry mouth
- difficulty to fall asleep and even difficulty in staying asleep
- nervousness or jitteriness
It is advisable to tell the doctor if any of the side effects persist for longer periods or even aggravate during the treatment.
What are certain conditions in which Focalin is contraindicated?
The use of Focalin is contraindicated in the following conditions:
- Agitation: the drug is contraindicated in patients who have anxiety, tension and agitation as it may worsen the symptoms.
- Hypersensitivity to methyphenidate: those individuals who are allergic to methyphenidate or any of the components of the drug including the inactive ingredients must not be given the drug. It is the duty of the doctor to ask the patients for their allergies to prevent any serious hypersensitivity reactions which include angioedema or anaphylactic reactions.
- Glaucoma: the drug is contraindicated in this case.
- Tics: those patients who are diagnosed with Tourette’s syndrome or have a family history of the syndrome or even those patients having motor tics are contraindicated to use the drug.
What are the drugs which are contraindicated with Focalin?
The use of Focalin is contraindicated with the following drugs:
- Monoamine oxidase inhibitors: patients who are currently using monoamine oxidase inhibitors or those who had used them in the preceding 14 days are contraindicated to use the drug since this may lead to hypertensive crisis.
Focalin during pregnancy and breast-feeding
Those women who are planning to start a family soon or those who are pregnant should consult their doctor before starting the drug. The drug is included in the US FDA pregnancy category C and should only be recommended if the benefits of the drug outweigh the potential risks associated with the use of the drug.
Animal studies have shown that the drug affects the developing fetus while the studies on humans are not adequate therefore the drug should be used with caution.
Those women who are breastfeeding their young ones must use the drug with caution. Although, there is not enough evidence to support that the drug is excreted into breast milk in humans but animal data suggests that it is excreted in breast milk. If given in large doses, the drug might interfere with milk production therefore the drug should be used with caution and after consultation with the health care provider by nursing mothers.
Focalin in geriatrics and pediatrics
The use of the drug in children less than 6 years of age has not been well established in term of the safety and efficacy of the drug. However, those children who have with cardiac abnormalities or heart problems should not be given the drug as deaths have been reported in case of using the drug in normal doses by those patients.
In case of older patients, the drug should be used with caution and at such doses that the condition of the patient does not get worse. Since geriatric patients are already suffering from heart problems or are more susceptible to cardiac abnormalities therefore the patient must consult with the health care provider before using the drug.
What drugs can interact with Focalin?
Focalin is CNS stimulant, therefore, a number of drugs can interact with it. You should always consult with your doctor if you are using Focalin with other drugs because a number of drugs can have life threatening interactions when used concomitantly with Focalin. Some of the major interactions that have occurred with Focalin are mentioned below.
- bupropion: bupropion has a tendency to cause seizures and when used concomitantly with medications such as dexmethylphenidate, it increases the risk. Elderly patients are at an increased risk as well as those having a history of seizures, undergoing drug or alcohol withdrawal, or those having a condition that affects the central nervous system such as brain tumor or head trauma.
Examples of drugs containing bupropion: Budeprion, Contrave, Forvivo XL, etc.
- selegiline: the concomitant use of selegiline and dexmethyphenidate is not recommended. Using the two drugs are used together can increase the blood pressure to a dangerously high level and even death can occur.The patient may experience symptoms of excessively high blood pressure when treated with selegiline which includes severe headache, blurred vision, confusion, seizures, chest pain, nausea, numbness, speech difficulties, fever, sweating, lightheadedness, and even fainting. Before prescribing Focalin, the doctor should check if the patient has been using selegiline and should prescribe the drug only if selegiline has not been used by the patient for atleast 2 weeks otherwise these life-threatening events can occur.
Examples of drugs containing selegiline: Atapryl, Selgene, Zelapar, etc.
- safinamide: if safinamide and dexmethylphenidate are used concomitantly then this may lead to increased cardiovascular events such as high blood pressure and increased heart rate. The blood pressure might increase to such a level which may require medical attention. Those patients who have a history of high blood pressure, irregular heart rhythm, or any other heart diseases should always consult the doctor before using these medications.
Examples of drugs containing safinamide: Xadago, etc.
- tramadol:one of the most unwanted effects of tramadol is its tendency to cause seizures and if it is used in combination with drugs that cause seizures so it may aggravate the symptoms. Since dexmethylphenidate also has the tendency to cause seizures therefore both the drugs should not be used concomitantly as it may increase the risk of having seizures. The elderly patients or those who have a history of seizures or a condition like brain tumor or head trauma affecting the central nervous system are at an increased risk of having seizures.
Examples of drugs containing tramadol: Tramahexal, Tramedo, Zydol, etc.
- citalopram: when dexmethylphenidate and citalopram are used concomitantly, this leads to increased blood levels and subsequently the effects of citalopram.The increased level of citalopram in blood can lead to confusion, hallucination, seizure, increased heart rate, fever, sweating, shivering, blurred vision, muscle cramps, tremors, muscle spasm or stiffness along with a serious condition called serotonin syndrome. The patient should seek immediate medical attention if he eperiences any of these symptoms when using the drugs.
- guanfacine: if the patient has to use this drug, he should tell the doctor if he is currently using dexmethyphenidate since both of the drugs can interact with each other. If both the drugs are used concomitantly then this can affect the rhythm of the heart. If the patient experiences symptoms such as irregular heartbeat, chest tightness, blurred vision or nausea then he should contact the doctor and seek medical help.
Examples of drugs containing guanfacine: Intuniv etc.
What happens if I overdose Focalin?
If the drug is overdosed, this may lead to symptoms which include restlessness, tremor, muscle twitches, confusion, hallucinations, depression, tiredness, nausea, vomiting, diarrhea, stomach pain, uneven heartbeats, panic, muscle pain or weakness, urine becomes dark coloured, euphoria, flushing, sweating, palpitations, tachycardia, cardiac arrhythmias, mydriasis, feeling light-headed, fainting, seizures (convulsions), or coma. Rhabdomyolysis may also occur.
These symptoms require prompt and immediate treatment. This can be treated by using appropriate supportive measures along with gastric lavage of the stomach contents so that the drug which is not absorbed can be removed. The airways should be protected and the seizures should be controlled while doing gastric lavage. Activated charcoal can also be used along with other necessary measures as may be required for the detoxification of the gut.
Focalin abuse and dependence
Focalin is a drug which is included in the Schedule II under the Controlled Substances Act. This states that the drug has a high potential for abuse and can cause severe physical or physiological dependence. Focalin has potential for abuse and is used largely by abused by drug addicts. Abuse of the drug can cause over dosage and leads to life threatening symptoms which can eventually cause death if not given prompt treatment.
Many addicts become dependent on the drug since it has the potential to cause physical and physiological dependence. This dependence can be distinguished as the person experiences withdrawal symptoms upon sudden discontinuation of the drug or if the dose of the drug is decreased from a higher strength to a lower strength.
What precautions are needed with Focalin?
You should always talk to your doctor or pharmacist if you have any allergies and particularly if you are allergic to this drug or methylphenidate. This will also help him to identify if you are allergic to any excipient which is present in the preparation.
You should also discuss your medical history with your doctor or pharmacist especially history of having high blood pressure, blood circulation problems, glaucoma, heart problems including heart failure, previous heart attack, problems with heart structure, having any family history of heart problems like cardiac death or irregular heartbeat, mental or mood conditions such as anxiety, tension, agitation, if u have any personal or family history of any mental or mood disorder such as bipolar disorder, depression. psychosis, if u have any personal or family history of uncontrolled muscle movements like motor tics or Tourette’s syndrome, hyperthyroidism or seizure disorder.
If you use alcohol or marijuana along with this drug so this can make you dizzy. In such cases, driving, using heavy machinery or doing activities requiring mental alertness should be avoided. If such work needs to be done then alcoholic beverages and marijuana should be avoided.
This drug can affect a child’s growth rate, weight and final adult height if it is used for a long time. In order to reduce this risk, the doctor may advise the patient to stop using the rug from time to time and you should regularly check your child’s weight and height and inform you doctor or pharmacist accordingly.
The side effects associated with the drug occur more frequently in older adults including trouble sleeping, weight loss or chest pain. This drug should only be used in pregnancy if the benefits outweigh the risks and if the doctor or the pharmacist so recommends.
What are warnings associated with the use of Focalin?
This drug can cause serious and life threatening cardiovascular events. Those children and adolescents who are suffering from serious heart problems or having structural cardiac abnormalities, when treated with the drug have had sudden deaths. Therefore, the drug should not be used in children or adolescents having serious structural cardiac abnormalities, cardiomyopathy, or serious heart rhythm problems.
In adults, the incidence of sudden deaths, stroke and myocardial infarction has also been reported when using Focalin for the treatment of ADHD. Therefore, Focalin should be used in adults suffering from coronary artery disease, heart rhythm abnormalities or other heart problems.
Focalin also causes an increase in the blood pressure and heart rate hence it should be used with caution in patients whose medical condition might get worse due to increase in the blood pressure or heart rate.
Those patients who are suffering from psychotic disorder should not use the drug as it may exacerbate the symptoms of behaviour disturbance. Also, those patients who are suffering from bipolar disorder can experience a mixed/manic episode if treated with Focalin for ADHD. In such instances care must be taken. Focalin can induce aggressive behaviour or hostility in children when treated with the drug for ADHD.
The drug should not be given to patients suffering from seizures as it may exacerbate the condition. This drug also has the tendency to cause painful and prolonged erections in both paediatric and adult patients. Therefore, it should be used with caution and if such event occurs then the patient should seek immediate medical attention. Patients using the drug also experience blurring of vision and difficulties with accommodation.
How to store Focalin?
Focalin should be stored in a safe place at a temperature of 59°F to 86°F (15°C to 30°C). such temperature is necessary otherwise it may lose its effectiveness and lead to deterioration of the drug. Since it is a controlled drug hence it should be kept at a place where it is inaccessible for the children.
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