What Is Pemoline?

This product is a central nervous system stimulant, 20 times the caffeine in the excitatory effect, and is used to treat brain dysfunction, mild depressive disorder, and narcolepsy. However, many adverse reactions were gradually replaced by tricyclic and tetracyclic antidepressants. Oral LD50 was 500 mg / kg in rats.

Introduction to Pimoline compounds

Pimoline is a central stimulant. Pro is mostly used for the treatment of mild brain dysfunction; mild depression and narcolepsy; and treatment of hereditary allergic dermatitis. Central excitability is mild, and its intensity is between amphetamine and methylphenidate, which is about 5 times that of caffeine.

Pimoline Basic Information

Chinese name: Pimoline

Chinese alias: delphinium tamarind; 2-imino-5-phenyl-4-oxazolidinone; pecinoline pimaline phenisotoin

English name: pemoline

English alias: H310; Fio; la956; phenylisohydantoin; npl1; cs293; 2-Imino-5-phenyl-4-oxazolidinone; Hyton; 2-amino-5-phenyl-2-oxazolin-4-one; PIO; h3104; Pemoline ; 2-Amino-5-phenyl-4 (5H) -oxazolone; 2-amino-5-phenyl-4-oxazolinone; Yh 1;

Chemical structure:

As shown on the right

CAS number: 2153-34-3

Molecular formula: C ₉ H ₈ N ₂ O ₂

Molecular weight: 176.17200

Exact mass: 176.05900

PSA: 64.68000

LogP: 0.73510

Physical and chemical properties of pimoline

Density: 1.4g / cm ³

Melting point: 243ºC

Flash point: 143.4ºC

Appearance: white to off-white crystalline powder, odorless and tasteless.

Solubility: difficult to dissolve in water, ether, chloroform, acetone, benzene, dilute hydrochloric acid, soluble in absolute ethanol, propylene glycol, hot alcohol, easily soluble in alkaline solution and concentrated mineral acid. ^[1]

Pimolin related drug label information

Pharmacological effects of pimoline

This product is similar to methylphenidate hydrochloride and is a central stimulant; it can achieve the central excitatory effect by increasing the content of central norepinephrine. Its effect is mild and its intensity is between amphetamine and methylphenidate, which is about equivalent to caffeine 5 times; also has a weak sympathetic effect. It is a safe and effective medicine suitable for short-term treatment of children. Long action time, only need to be administered once a day. In addition, this product can increase the effect of levodopa in the treatment of Parkinson's disease. Studies have shown that when the norepinephrine content in urine is significantly increased to close to normal after treatment with this product, the clinical effect is significant; if there is no change or no significant increase in the norepinephrine content in urine after treatment, the clinical effect is poor . Therefore, it is thought that the treatment of mild brain dysfunction with pimoline seems to be related to the increase of central norepinephrine content and the lack of noradrenaline supplementation. It is used to treat minor brain dysfunction, with an effective rate of 94.2%. It is still being tested for the treatment of atopic dermatitis with an efficacy of 85%.

Pharmacokinetics of pimoline

The effect of oral administration of this product occurs for 20-30 minutes, T _{max is} 2 to 4 hours, t _{1/2 is} 12 hours, and the steady-state blood drug concentration can be reached after 2 to 3 days after repeated administration. It is mainly excreted by the kidney, and can be excreted in 75% in 24 hours, of which about 43% is in the original form.

Pimorin indication

Children's Minor Dysfunction Syndrome (MBD); Mild depression, narcolepsy, and menopausal anxiety; Fatigue and memory impairment caused by excessive mental work; Atopic dermatitis.

Pimolin dosage

Oral: 20-40mg, qd for adults; 20-40mg, qd for children, orally before breakfast. If it is not effective after 3 to 4 weeks, increase 10 mg / d every week until the symptoms are controlled. The maximum dose does not exceed 60 mg / d.

Pimolin adverse reactions and precautions

nystagmus and dyskinesia, occasionally headache, dizziness, rash, drowsiness, restlessness, irritability and mild depression. Some patients may suffer from insomnia, loss of appetite and weight loss within a few weeks of treatment, but most of them are transient, and can continue to disappear after continued medication or reduction. Liver function must be checked before and during treatment. Common insomnia occurs mostly in the early stage of treatment before the curative effect appears, and most of them are transient. To avoid insomnia, do not take it after lunch.

Contraindication

Epilepsy and liver and kidney dysfunction are disabled; children under 6 years, pregnant women and lactating women should be used with caution.

Pimoline Drug Evaluation

This product has been used for the treatment of MBD for many years. The domestic clinical observation and treatment effect is good, and the effective rate is 94.2%. The effect of treating atopic dermatitis is 85%. ^[2-4]