Prostacyclin

• ( Z) -5 - {( 3aR, 4R, 5R, 6aS )-5- hydroxy-4- [ (E, 3S )-3- hydroxyoct -1-enyl ] hexahydro -2H- cyclopenta [ b] furan-2- ylidene
• (5Z, 9α, 11α, 13E, 15S ) -6,9 -epoxy -11 ,15- dihydroxy- prosta -5 ,13- dien-1- acid

B01AC09

Prostaglandins

Template: Infobox chemical / molecular formula search available

Prostacyclin ( or synonymously prostaglandin I2, short PGI2 ) is one of the group of the series -2 prostaglandins, these are the inflammatory prostaglandins from arachidonic acid.

• 3.1 Therapeutic Application
• 3.2 Contraindications
• 3.3 interactions

Education

Prostacyclin is produced in endothelial cells by means of prostacyclin from prostaglandin PGH2 from arachidonic acid. Arachidonic acid is an essential omega -6 fatty acid and is found in many foods. Especially high is their share in lard (1700 mg per 100 g), pork liver (870 mg per 100 g), egg yolk (297 mg per 100 g), tuna (280 mg per 100 g) and liver sausage (230 mg per 100 g).

Effects

Prostacyclin ( PGI2 short ) binds to the (G- protein-coupled membrane receptor) IP receptor and deployed about different effects:

Inflammation

PGI2 is together with the Hauptprostaglandin PGE2, which is involved in the inflammatory process. It increases vascular permeability (which is the tissue swelling causes ) is involved in the development of redness (which by an increased blood flow comes about ) and increases the pain (which is caused by other inflammatory substances such as bradykinin or histamine ) by sensitized nociceptive nerve endings ( by lowering the activation threshold for tetrodotoxin-resistant sodium channels in sensory nerves ). IP receptors in sensory neurons increase the activity of adenylate cyclase and the phospholipase A and to modulate the activity of ion channels and neurotransmitter release by activation of protein kinase A and protein kinase C.

Cardiovascular System

Prostacyclin synthesis important for the normal balance of blood flow and thrombus formation

Prostacyclin is the most potent endogenous inhibitor of platelet aggregation

Prostacyclin causes reperfusion or improvement and suppression of blood circulation.

This medicine is a stable analogue of the endogenous prostacyclin ( prostaglandin I2 or PGI2 ). The stable prostacyclin analogue has been approved in the application of acute ischemic events because of peripheral atherosclerotic occlusions or diabetic angiopathy, as well as a therapy for pulmonary hypertension. Furthermore, it is in the treatment of scleroderma, Raynaud's syndrome and pulmonary arterial hypertension application. Endogenous prostacyclin is mainly formed in the vascular endothelium and smooth muscle. It has a vasodilative, anti-proliferative and cytoprotective effect. In Prostacyclin is the strongest endogenous inhibitor of platelet aggregation ( TAH ).

Platelet aggregation inhibition comes about through its inhibitory effect on platelets. Prostacyclin is eliminated renally to 70% and is metabolized predominantly hepatic.

Lungs

Again, it mainly increases the pulmonary vessels and prevents microthrombi. Further, it is a weak bronchodilator. The Prostacylinblutspiegel of patients rise under general anesthesia and mechanical ventilation on the 15-20 times the norm.

Pharmacology

Therapeutic Application

Therapeutically are prostacyclin and prostacyclin analogs for the treatment of Raynaud's Syndrome, Pulmonary Hypertension, used in off- label use of bone marrow edema and also the femoral head.

Contraindications

Exclusion criteria for treatment include pregnancy, treatment with warfarin or heparin, heart failure, myocardial infarction, or of previous unstable angina pectoris. When neuraxial anesthesia procedures ( spinal or epidural ) prostacyclin should be discontinued 30 minutes before, but can be given immediately after the procedure.

Interactions

Known side effects with the drug prostacyclin are, in particular because of the initially occurring vasodilatory hypotension, headache, flushing ( reddening), sweating and nausea, and cardiac side effects such as Ap symptoms to ECG changes. Furthermore, agitation, diarrhea, fever, paresthesias, myalgias, arrhythmia, extrasystoles, pulmonary embolism, and renal pain may occur. According side effects can also very common as bleeding such as Epistaxis ( nosebleeds ) or hemoptysis ( bloody sputum from the respiratory tract ), especially if, in addition, other blood-thinning medicines ( anticoagulants ) to be taken, occur. In patients who are concomitantly treated with other antiplatelet agents or anticoagulants ( agents that stop the blood from clotting), the risk of bleeding may be increased.