Methylphenidate Hydrochloride｜化工社

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HCID 9280作成日：2026年10月27日

Methylphenidate Hydrochloride

https://huagongshe.com/ja/chemical/9280

Methylphenidate Hydrochloride の分子構造式

識別子と物理属性

CAS No.	298-59-9
分子式	C14H20ClNO2
平均分子量	269.77 g/mol
単同位体質量	269.1182566 g/mol
SMILES	COC(=O)C(c1ccccc1)C1CCCCN1.Cl
InChIKey	JUMYIBMBTDDLNG-UHFFFAOYSA-N
PubChem CID	9280
ChEMBL	CHEMBL1722
EC No.	206-065-3
DTXSID	DTXSID8020886

化学・物理的性質

極性表面積	38.3
水素結合供与体数	2
水素結合受容体数	3
回転可能結合数	4
重原子数	18
形式電荷	0
複雑度	249
溶解度	greater than or equal to 100 mg/mL at 68 °F (NTP, 1992)
融点	435 to 439 °F (NTP, 1992)
Physical Description	Methylphenidate hydrochloride is an odorless white crystalline powder. Metallic taste. Solutions are acid to litmus. Absence of general acid/base catalysis. (NTP, 1992)
Collision Cross Section	152.9 Å² [M+H]+ [CCS Type: TWMethod: calibrated with polyalanine and drug standards]

安全性と法規制

GHS 分類	DangerH302 (98.4%): Harmful if swallowed [Warning Acute toxicity, oral]H317 (12.5%): May cause an allergic skin reaction [Warning Sensitization, Skin]H334 (67.2%): May cause allergy or asthma symptoms or breathing difficulties if inhaled [Danger Sensitization, respiratory]H336 (14.1%): May cause drowsiness or dizziness [Warning Specific target organ toxicity, single exposureNarcotic effects]P233, P260, P261, P264, P270, P271, P272, P280, P284, P301+P317, P302+P352, P304+P340, P319, P321, P330, P333+P317, P342+P316, P362+P364, P403, P403+P233, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 64 reports by companies from 9 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. For more detailed information, please visit ECHA C&L website.
規制情報	Methylphenidate hydrochloride: Does not have an individual approval but may be used under an appropriate group standard
その他の安全情報	IMAP assessments - 2-Piperidineacetic acid, .alpha.-phenyl-, methyl ester, hydrochloride: Environment tier I assessmentIMAP assessments - 2-Piperidineacetic acid, .alpha.-phenyl-, methyl ester, hydrochloride: Human health tier I assessment
輸送ラベル（DOT）	Poison
火災危険	Flash point data for this chemical are not availablehowever, it is probably combustible. (NTP, 1992)
健康有害性	SYMPTOMS: Symptoms of exposure to this chemical may include nausea, vomiting, nervousness, insomnia, dizziness, headache, blood pressure and pulse changes, anorexia, palpitations, dyskinesia, drowsiness, tachycardia, angina, cardiac arrhythmia, abdominal pain and weight loss. It may also cause hypersensitivity, including skin rash, urticaria, fever, arthralgia, exfoliative dermatitis, erythema multiforme with histopathological findings of necrotizing vasculitis and thrombocytopenia purpura. Exposure to this compound may cause multiple small retinal emboli and a rise in ocular pressure in glaucomatous patients. Other symptoms include difficulties with accommodation and blurring of vision, Tourette`s syndrome, toxic psychosis, leukopenia, anemia, scalp hair loss, agitation, tremors, hyperreflexia, muscle twitching, convulsions which may be followed by coma, euphoria, confusion, hallucinations, delirium, sweating, flushing, hyperpyrexia, hypertension, mydriasis and dryness of mucous membranes. It also causes dryness of the mouth, constipation or diarrhea, difficulty in micturition, restlessness, changes in libido, talkativeness, disorientation, aggressive behavior, fatigue, mental depression which may be followed by convulsions and coma, aplastic anemia, acute conjunctivitis, pancytopenia, hypotension, angioneuroti edema, paranoid psychosis, lethargy, sleepiness and akathisia.

応急処置

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. IMMEDIATELY transport the victim after flushing eyes to a hospital even if no symptoms (such as redness or irritation) develop.SKIN: IMMEDIATELY flood affected skin with water while removing and isolating all contaminated clothing. Gently wash all affected skin areas thoroughly with soap and water. If symptoms such as redness or irritation develop, IMMEDIATELY call a physician and be prepared to transport the victim to a hospital for treatment.INHALATION: IMMEDIATELY leave the contaminated areatake deep breaths of fresh air. If symptoms (such as wheezing, coughing, shortness of breath, or burning in the mouth, throat, or chest) develop, call a physician and be prepared to transport the victim to a hospital. Provide proper respiratory protection to rescuers entering an unknown atmosphere. Whenever possible, Self-Contained Breathing Apparatus (SCBA) should be usedif not available, use a level of protection greater than or equal to that advised under Protective Clothing.INGESTION: DO NOT INDUCE VOMITING. If the victim is conscious and not convulsing, give 1 or 2 glasses of water to dilute the chemical and IMMEDIATELY call a hospital or poison control center. Be prepared to transport the victim to a hospital if advised by a physician. If the victim is convulsing or unconscious, do not give anything by mouth, ensure that the victim's airway is open and lay the victim on his/her side with the head lower than the body. DO NOT INDUCE VOMITING. IMMEDIATELY transport the victim to a hospital. (NTP, 1992)

非火災時の漏出対応

SMALL SPILLS AND LEAKAGE: If you spill this chemical, you should dampen the solid spill material with water, then transfer the dampened material to a suitable container. Use absorbent paper dampened with water to pick up any remaining material. Seal your contaminated clothing and the absorbent paper in a vapor-tight plastic bag for eventual disposal. Wash all contaminated surfaces with a soap and water solution. Do not reenter the contaminated area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned.STORAGE PRECAUTIONS: You should protect this material from exposure to light, and store it at ambient temperatures. This compound is a Schedule II DEA Controlled Substance and is to be stored according to State and Federal Regulations. Refer to Code of Federal Regulations Title 21 Part 1300 to End. (NTP, 1992)

Isolation and Evacuation

Excerpt from ERG Guide 151 [Substances - Toxic (Non-Combustible)]:IMMEDIATE PRECAUTIONARY MEASURE: Isolate spill or leak area in all directions for at least 50 meters (150 feet) for liquids and at least 25 meters (75 feet) for solids.SPILL: Increase the immediate precautionary measure distance, in the downwind direction, as necessary.FIRE: If tank, rail tank car or highway tank is involved in a fire, ISOLATE for 800 meters (1/2 mile) in all directionsalso, consider initial evacuation for 800 meters (1/2 mile) in all directions. (ERG, 2024)

Personal Protective Equipment (PPE)	RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with an organic vapor/acid gas cartridge (specific for organic vapors, HCl, acid gas and SO2) with a dust/mist filter. (NTP, 1992)

Treatment

Treatment consists of appropriate supportive measures. The patient must be protected against self-injury and against external stimuli that would aggravate overstimulation already present. Gastric contents may be evacuated by gastric lavage. In the presence of severe intoxication, use a carefully titrated dosage of a short-acting barbiturate before performing gastric lavage. Other measures to detoxify the gut include administration of activated charcoal and a cathartic. Intensive care must be provided to maintain adequate circulation and respiratory exchangeexternal cooling procedures may be required for hyperpyrexia. (L1712)

健康影響	Using large amounts of these drugs can result in a condition known as amphetamine psychosis -- which can result in auditory, visual and tactile hallucinations, intense paranoia, irrational thoughts and beliefs, delusions, and mental confusion.

暴露経路

Oral. Readily absorbed in a biphasic manner when orally administered (tablets) to children diagnosed with ADHD and to healthy adults. In children and adults males, after administration of a single oral dose of Ritalin LA and Ritalin given in two doses 4 hours apart, peak plasma concentration is reached approximately 2 hours for the first phase and 5-6 hours for the second phase. The absolute oral bioavailability of methylphenidate in children was 22&#1778% for d-methylphenidate and 5&#1773% for l-methylphenidate. These low values suggest that methylphenidate is highly metabolized presystemically.

毒性の概要	Methylphenidate blocks dopamine uptake in central adrenergic neurons by blocking dopamine transport or carrier proteins. Methylphenidate acts at the brain stem arousal system and the cerebral cortex and causes increased sympathomimetic activity in the central nervous system. Alteration of serotonergic pathways via changes in dopamine transport may result.

Signs and Symptoms	Symptoms of overdose include vomiting, agitation, tremors, hyperreflexia, muscle twitching, convulsions (may be followed by coma), euphoria, confusion, hallucinations, delirium, sweating, flushing, headache, hyperpyrexia, tachycardia, palpitations, cardiac arrhythmias, hypertension, mydriasis, and dryness of mucous membranes.

Carcinogen Classification	Methylphenidate HydrochlorideTR-439: Toxicology and Carcinogenesis Studies of Methylphenidate Hydrochloride (CASRN 298-59-9) in F344/N Rats and B6C3F1 Mice (Feed Studies) (1995 )06/22/93No EvidenceSome Evidence

Effects During Pregnancy and Lactation

◉ Summary of Use during LactationIn dosages prescribed for medical indications, limited evidence indicates that methylphenidate levels in milk are very low and not detectable in infant serum. If methylphenidate is required by the mother, it is not a reason to discontinue breastfeeding. It is possible that large dosages of methylphenidate might interfere with milk production, especially in women whose lactation is not well established.◉ Effects in Breastfed InfantsSeven of 8 infants, whose mothers were taking either dextroamphetamine (average dosage 25 mg daily) or methylphenidate (average dosage 52 mg daily) were clinically evaluated. The infants had no drug-related adverse reactions and were developing normally for their ages which averaged 4.4 months.One 6.4-month-old infant was mostly breastfed by a mother who had been taking methylphenidate 40 mg twice daily 5 days/week for 5.5 weeks. The mother reported that the infant was sleeping, eating and gaining weight normally. This patient might have been one of those in the report above by the same authors.An infant was being breastfed (extent not stated) by a mother who began taking sertraline 50 mg daily and methylphenidate after 5 weeks postpartum. The dosage began at 10 mg daily with an immediate-release product and gradually increased to 72 mg daily of an extended-release product. At 14 weeks of age, the infant was developing normally with no feeding difficulties. Examinations at 6 months and 1 year of age found no developmental problems in the child.A nursing mother was taking extended-release methylphenidate (Concerta) 36 mg daily and duloxetine 90 mg daily for ADHD, generalized anxiety disorder, borderline personality disorder, and depression. She partially (amount not stated) breastfed her infant for about 1 month. At 6 months of age, the infant’s development was considered to be normal, except for recurrent pneumonia caused by congenital pulmonary airway malformation.A woman with narcolepsy discontinued methylphenidate during pregnancy, but continued sertraline 100 mg and a prenatal vitamin daily during pregnancy and postpartum. She expressed breastmilk for bottle feeding and her infant was fed breastmilk exclusively until 6 months of age, and was weaned at 7 months. When her infant was 13 weeks old, she resumed methylphenidate 10 mg three times daily. The infant met all growth milestones through 6 months of age.A woman who was taking extended-release bupropion 300 mg daily for depression was diagnosed with attention deficit/hyperactivity disorder. She started on immediate-release methylphenidate 5 mg daily which was increased to 5 mg twice daily by 2 months postpartum. At 3 months postpartum, she transitioned to an osmotically controlled-release formulation of methylphenidate oral tablet, beginning at 18 mg daily, which was subsequently increased to 27 mg daily at 4 months and then to 36 mg daily at 6 months postpartum. Her exclusively breastfed infant maintained normal growth and developmental milestones during the first 6.75 months of life.◉ Effects on Lactation and BreastmilkMethylphenidate reduces serum prolactin, but no studies have been located as of the revision date on the effect of methylphenidate on milk production. The maternal prolactin level in a mother with established lactation may not affect her ability to breastfeed.A 15-year-old girl had been receiving methylphenidate 54 mg daily in an osmotic release tablet (OROS) for 2 years. Sertraline was started for depression at 50 mg daily and increased to 100 mg daily along with haloperidol 0.5 mg daily. After 12 weeks of therapy, inattentiveness at school and headaches prompted a change from the OROS product to a modified-release methylphenidate product (brand not specified) at 30 mg daily, then increasing to 50 mg daily. Three days after the increase in dosage, the girl had spontaneous milk flow from both breasts and subsequently had an elevated serum prolactin of 67.7 mcg/L. Methylphenidate and haloperidol were discontinued, but sertraline was continued. One week later, galactorrhea resolved completely. Fifteen days after drug discontinuation, the girl’s prolactin level was in the normal range at 19.4 mcg/L.