Sulbutiamine

Pharmacology of sulbutiamine

Pharmacological action - stimulates metabolism in the central nervous system, anti-asthenic. It regulates metabolic processes in the CNS. It can be accumulated in the cells of reticular formations, hippocampus and the dentate gyrus, and in cells of the Purkinje fibers and glomeruli of the granular layer of the cerebellar cortex (according to immunofluorescence examination).

Placebo-controlled clinical trials using psychometric tests and rating scales have shown high efficacy in the symptomatic treatment of functional asthenia. It is rapidly absorbed from the gastrointestinal tract, C max is achieved through 1-2 h after reception. It easily passes through blood-brain barrier; the ability to penetrate into breast milk has not been studied. T1/2 — about 5 hours. The drug is excreted by the kidneys. Experiments on animals have shown the absence of the teratogenic effect. According to the results of clinical studies, it has no effect on the development of the fetus, but sufficient clinical data is not available.

 

History

The creation of sulbutiamine is associated with the research of thiamine in Japan. The lack of thiamine in the nervous system causes the disease known as beriberi. Until the 20th century, the disease was mostly found only in Japan and in other Asian territories due to the large use of plain rice as the main food. The connection of beriberi with the diet was first noticed by a military surgeon Kanehiro Takaki. Further studies led to the discovery of thiamine, it was isolated in 1926 and synthesized in 1936. A committee for studying the vitamin in Japan has led to new research of the properties of thiamine and its derivatives.
The first derivative of thiamine is called allithiamine. It was derived from garlic in 1951. Allithiamine is produced from allyl disulfide. After the discovering of allithiamine, several special derivatives were got, supposing that they would have better pharmacokinetic features than thiamine had. Due to the positively charged component, a molecule of thiamine cannot diffuse through the plasma membrane. Sulbutiamine has much greater oral bioavailability due to its ability to smoothly dissolve in fats. It is not obvious when sulbutiamine has been first created, but first notions about the substance itself are dated back to 1973.

Synthetic ingredient, which has almost the same structure as thiamine, is rapidly absorbed from the gastrointestinal tract and easily permeates through GEB. Unlike thiamine, it can be accumulated in the cells of reticular formations, hippocampus and the dentate gyrus, and in cells of the Purkinje fibers and glomeruli of the granular layer of the cerebellar cortex (according to immunofluorescence examination).

 

 

Adverse effects

CNS: tremor, headache, mild agitation, malaise, dyspepsia.
AR: possible skin manifestations.

 

Drug contraindications

Hypersensitivity to sulbutiamine. It is not recommended to prescribe in case of pregnancy and lactation, to children. There are possible allergic reactions, agitation (to the elderly).


Overdose

Symptoms. There may be excited state with symptoms of euphoria and tremor of the limbs.
Treatment. Symptoms disappear quickly and do not require special treatment.


Interaction with other medications

No data on drug interactions.


Application in case of pregnancy and breastfeeding

It is not recommended to take during pregnancy (there is not enough clinical experience) and during breastfeeding (there is no data on the penetration of breast milk).


Precautions

During the course of the therapy you should observe caution while driving vehicles and occupation of potentially hazardous activities that require high concentration and psychomotor speed reactions.


Applications


The drug is prescribed in case of asthenic condition in hypo - and avitaminosis, long-term diseases, after surgical interventions.


Drug contraindications

Hypersensitivity, children's age. Restrictions are applied in case of pregnancy, breast-feeding.


Side effects

Allergic reactions, agitation (to the elderly).
Overdose symptoms: excited state (euphoria, tremor of the extremities). Treatment: symptoms of overdose pass quickly and do not require special treatment.


Method of application and dose


It is taken inside, 400-600 mg/day, the duration of the course is prescribed individually. Special instructions do not affect the ability to focus and speed psychomotor reactions.

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Dr. Carpentier previously provided internationally acclaimed NaProTECHNOLOGY services to couples throughout New England for 25 years. He was one of the first family physicians trained in NaProTECHNOLOGY and was honored with the international award for Outstanding Medical Consultant in Natural Family Planning and the Diocese of Worcester’s Mother Teresa Prolife Award.

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