Ролитетрациклин

Описание

Rolitetracycline was synthesized in 1958. Bristol-Myers Laboratories prepared it from tetracycline by introducing a pyrrolidinylmethyl moiety. This antibiotic is very soluble in water and more stable than tetracycline under acidic conditions. Rolitetracycline is used by intravenous injection, and its nitrate is used by both intravenous and intramuscular injections for therapy of the same infections as those treated by tetracycline.

Использование

Rolitetracycline is a tetracycline antibiotic that may be given intravenously or intramuscularly in serious bacterial infections when oral administration is not practicable.

Определение

ChEBI: A derivative of tetracycline in which the amide function is substituted with a pyrrolidinomethyl group.

Общее описание

Rolitetracycline, N-(pyrrolidinomethyl)tetracycline(Syntetrin), was introduced for use by intramuscular or intravenousinjection. This derivative is made by condensingtetracycline with pyrrolidine and formaldehyde in the presenceof tert-butyl alcohol. It is very soluble in water (1 g dissolvesin about 1 mL) and provides a means of injecting theantibiotic in a small volume of solution. It has been recommendedfor cases when the oral dosage forms are not suitable,but it is no longer widely used.

Фармацевтические приложения

2-N-pyrrolidinomethyl-tetracycline. A semisynthetic derivative of tetracycline supplied as the nitrate sesquihydrate for parenteral use.
It is not absorbed from the gastrointestinal tract. It is highly soluble and therefore can be administered parenterally. Peak plasma concentrations of 4–6 mg/L occur at 0.5–1 h after 350 mg intravenously. The plasma elimination half-life is 5–8 h. About 50% of the dose is excreted in the urine, producing high concentrations.
Intravenous administration is occasionally accompanied by abnormal taste, shivering and rigors, hot flushes, facial reddening, dizziness and, rarely, circulatory collapse. Symptoms of myasthenia gravis have occasionally been exacerbated.