Name | Iloprost |
Synonyms | Ilopros ILOPROST Iloprost Ciloprost CILOPROST Iloprost (for research only) 6,9ALPHA-METHYLENE-11ALPHA,15S-DIHYDROXY-16-METHYL-PROSTA-5E,13E-DIEN-18-YN-1-OIC ACID (5E)-5-[(3aS,5R,6aS)-5-hydroxy-4-[(1E,3S)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl]hexahydropentalen-2(1H)-ylidene]pentanoic acid (5Z)-5-[(3aS,5R,6aS)-5-hydroxy-4-[(1E,3R)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl]hexahydropentalen-2(1H)-ylidene]pentanoic acid |
CAS | 73873-87-7 78919-13-8 |
InChI | InChI=1/C22H32O4/c1-3-4-7-15(2)20(23)11-10-18-19-13-16(8-5-6-9-22(25)26)12-17(19)14-21(18)24/h8,10-11,15,17-21,23-24H,5-7,9,12-14H2,1-2H3,(H,25,26)/b11-10+,16-8+/t15?,17-,18?,19-,20+,21+/m0/s1 |
Molecular Formula | C22H32O4 |
Molar Mass | 360.49 |
Density | 1.21g/cm3 |
Boling Point | 539.2°C at 760 mmHg |
Flash Point | 294°C |
Solubility | Chloroform (Slightly), Methanol (Slightly) |
Vapor Presure | 7.06E-14mmHg at 25°C |
Appearance | Solid |
Color | Colourless to Pale Yellow Oil to |
Storage Condition | Amber Vial, -20°C Freezer, Under inert atmosphere |
Stability | Light Sensitive |
Refractive Index | 1.629 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.774 ml | 13.87 ml | 27.74 ml |
5 mM | 0.555 ml | 2.774 ml | 5.548 ml |
10 mM | 0.277 ml | 1.387 ml | 2.774 ml |
5 mM | 0.055 ml | 0.277 ml | 0.555 ml |
usage and dosage | adult: each inhalation should start from 2.5 micrograms (the dose provided by the mouthholder in the inhalation device). According to the needs and tolerability of different patients, iloprost should be inhaled 6-9 times a day. Depending on the dose of the drug required for the mouthpart and nebulizer, each inhalation time should be approximately 5-10 minutes. Course of treatment: long-term treatment. use of atomizer: the median aerodynamic diameter (MMAD) or median diameter (MMD) of the droplet is 3-4 m; The output dose of the mouthpiece is: 2.5 or 5 ug of iloprost each time; The atomization time of iloprost with a dose of 2.5 or 5 ug is about 4-10 minutes (in order to avoid systemic side effects, the output of iloprost within 4 minutes shall not exceed 5 ug). In order to minimize accidental exposure, it is recommended to use an atomizer equipped with a filter or inhalation trigger device when inhaling iloprost, and to maintain good ventilation in the room. Inhale the prepared solution with appropriate equipment (nebulizer). |
pharmacological effects | pulmonary hypertension is mainly characterized by increased pulmonary vascular resistance, and its pathogenesis includes vasoconstriction, vascular remodeling and thrombosis. Iloprost can stimulate adenylate cyclase, increase the concentration of cAMP in smooth muscle cells, and then dilate blood vessels. In addition, studies have shown that prostacyclin antagonizes the production and secretion of endothelin, inhibits platelet aggregation, and inhibits cell migration and proliferation. Regardless of intravenous or inhalation treatment of pulmonary hypertension, it is important to avoid uneven drug distribution leading to imbalance of ventilatory blood flow ratio and aggravating hypoxemia. The anatomical characteristics of the alveoli-capillaries determine that the drug can work through inhalation. Iloprost inhaler is a selective pulmonary vasodilator. Because the pre-capillary resistance blood vessel is surrounded by the alveoli, the local concentration of the alveoli after inhalation Higher, it directly acts on the sphincter and smooth muscle cells of the pre-capillary resistance blood vessel through diffusion, so it has a targeted therapeutic effect that other pathways cannot match. |