ILOPROST

Absorption

Rapidly absorbed with bioavailability of 63%

Toxicity

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

Description

Iloprost is a stable epoprostenol derivative which acts as an inhibitor of platelet aggregation and is recommended for the treatment of peripheral vascular diseases. The compound was shown to be a potent agonist at PGE₂-sensitive and prostacyclin-sensitive receptors in animal studies. Iloprost is administered by IV infusion and has been reported to have beneficial effects in Buerger's and Raynaud's diseases as well as peripheral artery occlusive disease.

Chemical properties

Colourless Oil

Chemical properties

Quinone exists as a large, yellow, monoclinic prism with an irritating odor. Quinone is extensively used in the dye, textile, chemical, tanning, and cosmetic industries. In chemical synthesis for hydroquinone and other chemicals, quinone is used as an intermediate. It is also used in the manufacturing industries and chemical laboratories associated with protein fi ber, photographic fi lm, hydrogen peroxide, and gelatin making.

Originator

Schering AG (Germany)

The Uses of ILOPROST

A synthetic analogue of Prostacyclin (PGI2) used to treat pulmonary arterial hypertension (PAH), scleroderma, Raynaud's phenomenon and ischemia. It acts through elevation of cAMP by binding to the prostacyclin receptor (IP receptor). Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets with an ED50 of about 13 nM. In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time.

The Uses of ILOPROST

A synthetic analogue of Prostacyclin (PGI2) used to treat pulmonary arterial hypertension (PAH), scleroderma, Raynaud''s phenomenon and ischemia. It acts through elevation of cAMP by binding to the prostacyclin receptor (IP receptor). Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets with an ED50 of about 13 nM. In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time.

Indications

Used for the treatment of pulmonary arterial hypertension.

Background

Iloprost is a synthetic analogue of prostacyclin PGI2 that dilates systemic and pulmonary arterial vascular beds. It is used to treat pulmonary arterial hypertension (PAH).

What are the applications of Application

Iloprost is a second generation structural analog of prostacyclin (PGI)

Definition

ChEBI: A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R /stereo>)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension.

brand name

Ventavis (Schering);Iiomedin.

Health Hazard

Exposures to quinine vapor are highly irritating to the eyes and may be followed by corneal opacities, structural changes in the cornea, and loss of vision. Solid quinone may produce discoloration, severe irritation, swelling, and form papules and vesicles.

Biological Activity

Prostacyclin (PGI 2 ) analog that binds with high affinity to IP, EP 1 and EP 3 receptors (K i values are 11, 11, 56, 284, 619, 1035, 1870 and 6487 nM for IP, EP 1 , EP 3 , EP 4 , FP, DP, EP 2 and TP receptors respectively). Inhibits platelet aggregation induced by collagen, thrombin and ADP (IC 50 values are 0.24, 0.71 and 1.07 nM respectively).

Biochem/physiol Actions

Iloprost is used to treat children with PH (pulmonary hypertension) after the surgery to clear CHD (congenital heart disease). In transplant patients, this prostacyclin analogue is used to inhibit renal dysfunction. Iloprost performs various functions like vasodilatation and cytoprotection. It has higher stability than prostacyclin.

Pharmacokinetics

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.

Metabolism

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