Iloprost

360.49

360.49

DTXSID2041046

B01AC11|B - Blood and blood forming organs

2918199090

77.76000

2.94

colorless oil

1.2±0.1 g/cm3

115.7ºC

539.2±50.0 °C at 760 mmHg

294.0±26.6 °C

1.629

Very slightly soluble

Desiccate at -20°C

|Danger|H301 (98.48%): Toxic if swallowed [Danger Acute toxicity, oral]|P201, P202, P261, P264, P270, P271, P280, P281, P301+P310, P302+P352, P304+P340, P308+P313, P311, P312, P321, P322, P330, P361, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 66 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Overdoses can lead to hypotension, headache, flushing, nausea, vomiting, and diarrhea.

60%

Used for the treatment of pulmonary arterial hypertension.|FDA Label|Treatment of patients with primary pulmonary hypertension, classified as New York Heart Association functional class III, to improve exercise capacity and symptoms.

Iloprost is a synthetic analogue of prostacyclin PGI2 that dilates systemic and pulmonary arterial vascular beds. It was shown to affect platelet aggregation, but whether this effect contributes to its vasodilatory action has not been elucidated. There are two diastereoisomers of iloprost and the 4S isomer is reported to exhibit a higher potency in dilating blood vessels compared to the 4R isomer.

Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)|Drugs or agents which antagonize or impair any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. (See all compounds classified as Platelet Aggregation Inhibitors.)

Rapidly absorbed with bioavailability of 63%|0.7 to 0.8 L/kg|20 mL/min/kg [Normal subjects]

Primarily hepatic. Iloprost is metabolized principally via beta-oxidation of the carboxyl side chain.

20-30 minutes

Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, such as carbaprostacyclin. Iloprost binds with equal affinity to human prostacyclin (Prostanoid IP) and prostaglandin EP1 receptors. Iloprost constricts the ilium and fundus circular smooth muscle as strongly as prostaglandin E2 (PGE2) itself. Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets. In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time. All of these properties help to antagonize the pathological changes that take place in the small pulmonary arteries of patients with pulmonary hypertension.

Ciloprost

Human drugs -> Ventavis -> EMA Drug Category|Antithrombotic agents -> Human pharmacotherapeutic group|Human drugs -> Rare disease (orphan)|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals