Chemical formula: C₁₄H₁₉NO₂ Molecular mass: 233.306 g/mol PubChem compound: 4158
Methylphenidate interacts in the following cases:
Caution is advised in patients being treated with methylphenidate with any other medicinal product that can also elevate blood pressure.
It is not known how methylphenidate may effect plasma concentrations of concomitantly administered medicinal products. Therefore, caution is recommended at combining methylphenidate with other medicinal products, especially those with a narrow therapeutic window.
Serotonin syndrome has been reported following coadministration of methylphenidate with serotonergic medicinal products. If concomitant use of methylphenidate with a serotonergic medicinal product is warranted, prompt recognition of the symptoms of serotonin syndrome is important. These symptoms may include mental-status changes (e.g. agitation, hallucinations, coma), autonomic instability (e.g. tachycardia, labile blood pressure, hyperthermia), neuromuscular abnormalities (e.g. hyperreflexia, incoordination, rigidity), and/or gastrointestinal symptoms (e.g. nausea, vomiting, diarrhoea). Methylphenidate must be discontinued as soon as possible if serotonin syndrome is suspected.
Serious, adverse events, including sudden death, have been reported in concomitant use of methylphenidate and clonidine. The long-term safety of using methylphenidate in combination with clonidine or other centrally acting alpha-2 agonists has not been systematically evaluated.
Alcohol may exacerbate the adverse CNS effect of psychoactive medicinal products, including methylphenidate. It is therefore advisable for patients to abstain from alcohol during treatment.
There are reports indicating that methylphenidate may inhibit the metabolism of coumarin anticoagulants, anticonvulsants (e.g., phenobarbital, phenytoin, primidone), and some antidepressants (tricyclics and selective serotonin reuptake inhibitors). When starting or stopping treatment with methylphenidate, it may be necessary to adjust the dose of these medicinal products already being taken and establish plasma concentrations of the active substance (or for coumarin, coagulation times).
Methylphenidate may decrease the effectiveness of medicinal products used to treat hypertension.
There is a risk of sudden blood pressure and heart rate increase during surgery. If surgery is planned, methylphenidate treatment should not be used on the day of surgery.
Caution is recommended when administering methylphenidate with dopaminergic medicinal products, including antipsychotics. Because a predominant action of methylphenidate is to increase extracellular dopamine levels, methylphenidate may be associated with pharmacodynamic interactions when co-administered with direct and indirect dopamine agonists (including DOPA and tricyclic antidepressants) or with dopamine antagonists including antipsychotics.
Methylphenidate should be used with caution in patients with epilepsy.
Category B3.
Data from a cohort study of in total approximately 3,400 pregnancies exposed in the first trimester do not suggest an increased risk of overall birth defects. There was a small increased occurrence of cardiac malformations (pooled adjusted relative risk, 1.3; 95% CI, 1.0-1.6) corresponding to 3 additional infants born with congenital cardiac malformations for every 1000 women who receive methylphenidate during the first trimester of pregnancy, compared with non-exposed pregnancies.Cases of neonatal cardiorespiratory toxicity, specifically foetal tachycardia and respiratory distress have been reported in spontaneous case reports.
Studies in animals have shown evidence of reproductive toxicity at maternally toxic doses.
Methylphenidate is not recommended for use during pregnancy unless a clinical decision is made that postponing treatment may pose a greater risk to the pregnancy.
Methylphenidate is excreted in human milk.
Based on reports of breast milk sampling from five mothers, methylphenidate concentrations in human milk resulted in infant doses of 0.16% to 0.7% of the maternal weight-adjusted dose, and a milk to maternal plasma ratio ranging between 1.1 and 2.7. There is one case report of an infant who experienced an unspecified decrease in weight during the period of exposure but recovered and gained weight after the mother discontinued treatment with methylphenidate. A risk to the suckling child cannot be excluded.
A decision must be made whether to discontinue breast-feeding or to discontinue/abstain from methylphenidate therapy taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman.
No human data on the effect of methylphenidate on fertility are available. There were no relevant effects observed in the non-clinical studies.
Methylphenidate can cause dizziness, drowsiness and visual disturbances including difficulties with accommodation, diplopia and blurred vision. It may have a moderate influence on the ability to drive and use machines. Patients should be warned of these possible effects and advised that if affected, they should avoid potentially hazardous activities such as driving or operating machinery.
The table below shows all adverse reactions observed during clinical trials of children, adolescents, and adults and postmarket spontaneous reports with methylphenidate prolonged-release tablet and those, which have been reported with other methylphenidate hydrochloride formulations. If the adverse reactions with methylphenidate prolonged-release tablet and the methylphenidate formulation frequencies were different, the highest frequency of both databases was used.
Frequency estimate: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10,000 to <1/1000), very rare (<1/10,000), not known (cannot be estimated from the available data).
| System Organ Class | Adverse Reaction | |||||
|---|---|---|---|---|---|---|
| Frequency | ||||||
| Very common | Common | Uncommon | Rare | Very rare | Not known | |
| Infections and infestations | Nasopharyngitis, Upper respiratory tract infection#, Sinusitis# | |||||
| Blood and lymphatic system disorders | Anaemia†, Leucopenia†, Thrombocytopenia, Thrombocytopenic purpura | Pancytopenia | ||||
| Immune system disorders | Hypersensitivity reactions such as Angioneurotic oedema, Anaphylactic reactions, Auricular swelling, Bullous conditions, Exfoliative conditions, Urticarias, Pruritus, Rashes, and Eruptions | |||||
| Metabolism and nutritional disorders | Anorexia, Decreased appetite†, Moderately reduced weight and height gain during prolonged use in children | |||||
| Psychiatric disorders | Insomnia, Nervousness | Affect lability, Aggression, Agitation, Anxiety†, Depression#, Irritability, Abnormal behaviour, Mood swings, Tics, Initial insomnia#, Depressed mood#, Libido decreased#, Tension#,Bruxism&, Panic attack# | Psychotic disorders, Auditory, visual and tactile hallucination, Anger, Suicidal ideation, Mood altered, Restlessness†, Tearfulness, Worsening of pre-existing tics of Tourette’s syndrome, Logorrhoea, Hypervigilance, Sleep disorder | Mania†, Disorientation, Libido disorder, Confusional state† | Suicidal attempt† (including completed suicide), Transient depressed mood, Abnormal thinking, Apathy†, Repetitive behaviours, Over-focussing | Delusions†, Thought disturbances, dependence, Cases of abuse and dependence have been described, more often with immediate release formulations |
| Nervous system disorders | Headache | Dizziness, Dyskinesia, Psychomotor hyperactivity, Somnolence, Paresthaesia#, Tension headache# Sedation, | Tremor†, Lethargy# | Convulsion, Choreoathetoid movements, Reversible ischaemic neurological deficit, Neuroleptic malignant syndrome (NMS; Reports were poorly documented and in most cases, patients were also receiving other medicinal products, so the role of methylphenidate is unclear). | Cerebrovascular disorders†† (including vasculitis, cerebral haemorrhages, cerebrovascular accidents, cerebral arteritis, cerebral occlusion), Grand mal convulsion, Migraine†, Dysphemia | |
| Eye disorders | Accommodation disorder# | Blurred vision† Dry eye# | Difficulties in visual accommodation, Visual impairment, Diplopia | Mydriasis | ||
| Ear and labyrinth disorders | Vertigo# | |||||
| Cardiac disorders | Arrhythmia, Tachycardia, Palpitations | Chest pain | Angina pectoris | Cardiac arrest; Myocardial infarction | Supraventricular tachycardia, Bradycardia, Ventricular extrasystoles†, Extrasystoles† | |
| Vascular disorders | Hypertension | Hot flush# | Cerebral arteritis and/or occlusion, Peripheral coldness†, Raynaud’s phenomenon | |||
| Respiratory, thoracic and mediastinal disorders | Cough, Oropharyngeal pain | Dyspnoea† | ||||
| Gastrointestinal disorders | Abdominal pain upper, Diarrhoea, Nausea†, Abdominal discomfort, Vomiting, Dry mouth† Dyspepsia# | Constipation† | ||||
| Hepatobiliary disorders | Alanine aminotransferase increased# | Hepatic enzyme increased | Abnormal liver function, including acute hepatic failure and hepatic coma, Blood alkaline phosphatase increased, Blood bilirubin increased† | |||
| Skin and subcutaneous tissue disorders | Alopecia, Pruritis, Rash, Urticaria, Hyperhidrosis† | Angioneurotic oedema, Bullous conditions, Exfoliative conditions | Macular rash; Erythema | Erythema multiforme, Exfoliative dermatitis, Fixed drug eruption | ||
| Musculoskeletal and connective tissue disorders | Arthralgia, Muscle tightness#, Muscle spasms# | Myalgia†, Muscle twitching | Muscle cramps | Trismus& | ||
| Renal and urinary disorders | Haematuria, Pollakiuria | Incontinence | ||||
| Reproductive system and breast disorders | Erectile dysfunction# | Gynaecomastia | Priapism, Erection increased and Prolonged erection | |||
| General disorders and administration site conditions | Pyrexia, Growth retardation during prolonged use in children, Fatigue†, Irritability#, Feeling jittery#, Asthenia#, Thirst# | Chest pain | Sudden cardiac death | Chest discomfort†, Hyperpyrexia | ||
| Investigations | Changes in blood pressure and heart rate (usually an increase), Weight decreased | Cardiac murmur | Platelet count decreased, White blood cell count abnormal | |||
# Frequency derived from adult clinical trials and not on data from trials in children and adolescents; may also be relevant for children and adolescents.
† Adverse drug reaction from clinical trials in adult patients that were reported with a higher frequency than in children and adolescents.
& Based on the frequency calculated in adult ADHD studies (no cases were reported in the paediatric studies).
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