Sulprostone

• (5Z, 11α, 13E, 15R ) - 11,15 -dihydroxy -9 -oxo -16 -phenoxy -17 ,18,19,20 - tetranorprosta -5 ,13- dienoic acid methane sulfonamide
• CP- 34089
• SHB -286
• ZK- 57671

Colorless to brownish liquid

Liquid

Soluble in DMSO

Risk

12 mg · kg -1 ( LD50, rat, ip)

Template: Infobox chemical / molecular formula search available

Sulprostone is a synthetic derivative of prostaglandin E2, which leads to a contraction of smooth muscles of the uterus, cervix uteri, but the extended. It is used as a drug for preparing an instrumental removal of the uterus ( abortion, treatment of a subdued abortion ) or for the treatment of atonic uterine bleeding, when the administration of oxytocin and surgical measures are not sufficient to stop the bleeding.

Sulprostone relatively often leads to nausea and vomiting, and in rare cases, serious complications such as pulmonary edema or cardiac arrhythmias can occur and even cardiac arrest. Spasm of the coronary arteries with subsequent heart attacks are also possible, though rare.

Sulprostone is administered intravenously as continuously as possible. The dose should not exceed the dose of 500 micrograms / hour. The days Höch amount is a total of 1500 g / 24 h

For postpartum atonic uterine bleeding if applied initially 100 micrograms / hour, up to 500 micrograms / h after the start of the therapeutic effect of reducing the amount of intravenously administered to the maintenance dose of 100 micrograms / h, taking into account the maximum daily amount.

The medication shall not be used in patients over 35 years or with pre-existing coronary artery disease. It must not be administered simultaneously with oxytocin.

Pharmacokinetics of the prostaglandin E2 derivative sulprostone

Pharmacokinetic must distinguish the distribution phase ( distribution) of the drug in the organism from that of Verstoffwechselns (metabolism ) and elimination ( excretion and secretion).

• Distribution: The binding of sulprostone to plasma proteins is 20-30 %.

After intravenous administration, the apparent volume of distribution ( Vss) is approximately 1100 l A peak plasma level of 0.3 nmol / l ( = 140 ng / l ) of a ten-hour infusion at an infusion rate of 100 g / h is achieved in the end. Thereafter, the drug concentration decreases quickly, and is two hours later under the detection limit.

• Metabolism

Sulprostone is extensively metabolized in the liver tissue, so converted. One of the minor metabolites, the free acid of sulprostone, binds to the prostaglandin. Participation of cytochrome P450 -dependent enzymes in the metabolism of sulprostone there are no adequate studies.

• Elimination

Sulprostone is excreted exclusively in the form of metabolites. About 85 % of the dose is excreted via the kidneys, and the rest in the bile fluid. About 75 % of the administered substance is excreted within 6 hours ( initial half-life of less than 2 hours). The terminal half -life is about 20 hours.

Finished medicinal product

Nalador (D, CH)

1 ampoule containing, for example, 0.5 g of the 500 micrograms sulprostone.