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drugs / psychostimulants / based on methylphenidates

Psychostimulants based on methylphenidates

Caution​

Methylphenidates should be prescribed with caution in people with emotional instability,

especially in those with a history of drug or alcohol abuse, because these tend to increase the dose

medication on their own.

 

Abuse of the drug for a long time can lead to pronounced habituation and psychological dependence accompanied by behavioral abnormalities of varying degrees.

Overt psychotic episodes may occur, particularly with excessive parenteral (medication given by injection) use.

 

Close monitoring is essential during withdrawal, as withdrawal of the drug may cause major depression to reappear. After long-term treatment, withdrawal may result in the onset of previously masked symptoms of an underlying disorder that may require follow-up.

 

There have been reports of sudden death, stroke, and myocardial infarction in adults taking stimulants at usual doses for the treatment of ADHD and of sudden death in children and adolescents with structural heart abnormalities or other serious heart problems.

Directions ​

  • Attention deficit disorder with or without hyperactivity (ADHD)

  • Adjunctive therapy for narcolepsy (Ritalin)

Contraindications ​

  • Anxiety, tension or restlessness

  • Thyrotoxicosis (hyperthyroidism)

  • Advanced stage arteriosclerosis

  • Glaucoma

  • Hypersensitivity to methylphenidate, to any excipient used in the product or to any component of the container

  • Motor tics, or a family history or  a diagnosis of Tourette syndrome  (vocal tics)

  • During treatment with monoamine oxidase inhibitors (MAOIs), as well as for a minimum of 14 days following discontinuation of monoamine oxidase inhibitor therapy

  • Pre-existing cardiovascular disorder, including moderate to severe hypertension, angina, obliterating arterial disease, heart failure, congenital heart disease of significant hemodynamic significance, cardiomyopathy, myocardial infarction, life-threatening arrhythmia, and calcium channel dysregulation disorders.

  • Pregnancy: Methylphenidates should not be given to pregnant women unless the potential benefits outweigh the risks to the fetus.

  • Breast- feeding: Methylphenidates pass into breast milk, so breast-feeding is not recommended.

  • Children: It is not recommended to use amphetamines for the treatment of attention deficit disorder with or without hyperactivity in children under 6 years of age.

Drugs interactions​

Antihypertensives

Methylphenidates may decrease the effect of antihypertensives.

 

Drugs that raise blood pressure

These products should be used with caution in people being treated with agents that increase blood pressure. Because of the risk of hypertensive crisis they would involve, their use  is contraindicated in persons receiving monoamine oxidase inhibitors (MAOIs) or who have received them within the  14 previous days.

 

Anesthetics

During anesthesia with a halogenated agent, the blood pressure and heart rate of the person receiving methylphenidates may increase suddenly. Methylphenidate may also lessen the sedative effect of general anesthetics. If we plan  to perform surgery under anesthesia, the treatment must be suspended on the day of the operation.

 

Central alpha-2 receptor agonists

(eg, clonidine [Catapres], a blood pressure medication)

Serious adverse effects, including sudden death, have been reported during concurrent use of Ritalin and clonidine (Catapres). However, it was not possible to establish a causal link due to a lack of data.

 

Drugs acting on the dopaminergic system

Levodopa and tricyclic antidepressants or dopamine antagonists (antipsychotics, such as haloperidol). Concomitant administration of methylphenidates and antipsychotics is not recommended because  that these products have opposite modes of action.

 

Coumarin anticoagulants (warfarin), anticonvulsants (phenobarbital, phenytoin, primidone) and certain antidepressants (tricyclics and selective serotonin reuptake inhibitors)

Doses of these drugs may need to be reduced when co-administered with methylphenidate. When starting or stopping concomitant treatment with methylphenidate, it may be necessary to adjust the dosage and to monitor plasma concentrations of these drugs (or, in the case of coumarin, clotting times).

 

Alcohol

Alcohol may exacerbate the adverse effects of psychoactive agents on the central nervous system (CNS). People should therefore be advised not to consume alcohol during treatment.

Side effects​

They depend on the dosage and duration of treatment, the metabolism of the individual and the context in which he lives.

 

Frequent

 

Head

  • Sore throat

  • Runny nose

  • Dry mouth

  • Headache

  • Dizziness

  • Toothache

  • Hair loss

  • Cough

  • Fever

 

Heart

  • Change in blood pressure  (usually an increase)

  • Abnormal heart rhythm

  • Palpitations

 

Abdomen

  • Nausea

  • Upset stomach (Stomach upset can be reduced by taking Ritalin with food)

  • Vomiting

 

Members

  • Tremors

  • Skin rash

  • Itching

  • Urticaria

  • Dyskinesia (involuntary muscle jerks and jerks)

  • Joint pain

 

Others

  • Decreased appetite

  • Nervousness

  • Difficulty falling asleep, sleep disturbances

  • Excessive emotional distress, emotional arousal

  • Excessive sweating

  • Weightloss

  • Hustle

Infrequent or rare

 

  • Slowing of growth (height and weight) during long-term treatment of the child

  • Blurred sight, blurred vision

  • Low red blood cell count (anaemia), low platelet count (thrombocytopenia), low white blood cell count (leukopenia)

  • depressed mood

  • Vocalizations and involuntary movements (syndrome  by Gilles de la Tourette)

  • Abnormal functioning of the liver, which may include hepatic coma

  • Muscle cramps

  • Tics

  • Abnormal thoughts or hallucinations

  • Allergy

Therapeutic effects ​

  • improves behavior by decreasing restlessness and promoting the ability to concentrate

  • helps increase attention and reduce impulsiveness and hyperactivity

  • helps relieve unwelcome bouts of sleep during the day

Monitoring and medical supervision​

Before treatment:

  • Check blood pressure (high pressure), possibilities of heart trouble.

  • Check for hyperthyroidism.

  • Perform an eye exam.

  • Check for the presence of motor tics and vocal tics.

  • Check for a history of Raynaud's phenomenon (tingling, numbness, discoloration of cold fingers and toes).

  • Indicate if you are taking MAOIs.

  • Indicate if you are taking other ADHD medications.

  • Indicate allergies.

  • Indicate the presence of epilepsy.

  • Indicate a family history of sudden death or death related to cardiac disorders.

  • Indicate if you have abused drugs, alcohol or medication.

 

During treatment:

  • Check growth and weight regularly.

  • Check blood pressure and heart rate.

  • Call your doctor right away if you/your child have any signs of heart problems such as: rapid heartbeat, palpitations, chest pain, shortness of breath, difficulty breathing or fainting during treatment.

  • Indicate the onset of mental health problems.  

All people :

- Appearance or aggravation of behavioral or     thought.

- Appearance or aggravation of a “bipolar disorder”.

- Appearance or worsening of “aggressive or hostile behavior”.

Children and adolescents :

Appearance of psychotic symptoms (eg, hearing voices, believing things that are not true or suspicious) or appearance of “manic symptoms”.

Withdrawal symptoms

Psychotropic drugs act in the brain just as they do in the rest of the body; and as we have seen, each person reacts differently. It's the same with weaning; the person's metabolism, the type of drug, the dose as well as the duration of the intake and its half-life, explain that the withdrawal effects are varied. We have listed the potential and main withdrawal symptoms of each class of psychotropic drugs. This list is incomplete, as not all withdrawal effects are listed; moreover, knowledge is rapidly evolving in this area. A person may have no withdrawal symptoms or experience one, a few, or even many. The medication reduction journey is specific to each person, just as each process is unique. For example, a person can take the same medicine twice at the same dose and the effects will be different. Gradual reduction, like removing 10  % of dose per week/month, reduces the frequency or intensity of withdrawal symptoms and the incidence of rapid relapses. It is very important to undertake this process with the collaboration of your doctor. The pharmacist also plays a key role and can provide guidance to monitor withdrawal effects for each drug. Most people who will have withdrawal symptoms will tolerate them without problems for the short duration of these symptoms.

 

Common and frequent withdrawal symptoms for all classes: anxiety, nervousness, restlessness, sleep problems, greater need to rest, sleep, irritability, fatigue.

Withdrawal symptoms for psychostimulants :

Withdrawal symptoms appear a few days after the dose is reduced. In the process of progressive reduction according to the method of 10  %, the last step can be particularly difficult. It can be lengthened or split to reduce withdrawal symptoms.

Main psychological withdrawal symptoms:

  • Depressive syndrome

  • Hyperactivity

  • Return of original issues

  • suicidal tendencies

  • Irritability

  • Anxiety with agitation

  • Anger and aggression

 

Main physical withdrawal symptoms:

  • Lack of attention and concentration

  • Social withdrawal

  • Excessive need to sleep

  • Excessive need to eat

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