Peringatan Keamanan

The oral LD₅₀ in rats is >100 mg/kg.^L50156

Cases of overdose have been reported. Frequently observed symptoms following overdose are dizziness, headache, flushing, nausea, jaw pain or back pain. Hypotension, vomiting, and diarrhea are possible. A specific antidote is not known. Interruption of the inhalation session, monitoring, and symptomatic measures are recommended.^L50146

Iloprost

DB01088

small molecule approved investigational

Deskripsi

Iloprost is an analog of prostacyclin (PGI2; epoprostenol), an endogenous prostanoid mainly produced in the vascular endothelium. It is more stable than prostacyclin, which is short-lived.^A263326 Iloprost consists of a mixture of the 4R and 4S diastereoisomers at a ratio of approximately 53:47.^L50146 It is a potent vasodilator with reported anti-thrombotic properties.^A263316 Iloprost is available as an inhaled solution and intravenous formulations. It is used to treat pulmonary arterial hypertension (PAH) ^L50146 and frostbites.^L50151

Struktur Molekul 2D

Berat 360.494

Wujud liquid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of iloprost is 20 to 30 minutes.[L50146]

Volume Distribusi Following intravenous infusion, the apparent steady-state volume of distribution was 0.7 to 0.8 L/kg in healthy subjects.[L50146]

Klirens (Clearance) Clearance in normal subjects was approximately 20 mL/min/kg.[L50146]

Absorpsi

Following inhalation of iloprost (5 mcg) patients with pulmonary hypertension have iloprost peak plasma levels of approximately 150 pg/mL. Iloprost was generally not detectable in plasma 30 minutes to one hour after inhalation. The absolute bioavailability of inhaled iloprost has not been determined.^L50146 When iloprost was administered via intravenous infusion at a rate of 2 ng/kg/min, steady-state plasma concentrations were 85 ng/L.^A263326

Metabolisme

In vitro studies reveal that cytochrome P450-dependent metabolism plays only a minor role in the biotransformation of iloprost. Iloprost is metabolized principally via ?-oxidation of the carboxyl side chain. The main metabolite is tetranor-iloprost, which was shown to be pharmacologically inactive in animal experiments.A263326, L50146 In rabbits, dinor-iloprost has also been identified as a drug metabolite.A263321, A263326

Rute Eliminasi

Unchanged iloprost and its metabolites are mainly excreted in urine.^L50146 About 70% of the drug and metabolites undergo renal excretion. Following the administration of intravenous infusion at the rate of 2 ng/kg/min and oral dose at 0.1 ug/kg, fecal excretion was 12% and 17%, respectively.^A263326

Interaksi Makanan

1 Data

1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Taking iloprost with anticoagulant/antiplatelet herbs may increase the risk of bleeding occurring as an adverse effect. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Interaksi Obat

521 Data

Duloxetine	The risk or severity of orthostatic hypotension and syncope can be increased when Iloprost is combined with Duloxetine.
Levodopa	The risk or severity of hypotension and orthostatic hypotension can be increased when Iloprost is combined with Levodopa.
Risperidone	Iloprost may increase the hypotensive activities of Risperidone.
Apixaban	Iloprost may increase the anticoagulant activities of Apixaban.
Obinutuzumab	The risk or severity of adverse effects can be increased when Iloprost is combined with Obinutuzumab.
Pentoxifylline	Iloprost may increase the hypotensive activities of Pentoxifylline.
Rivaroxaban	Iloprost may increase the anticoagulant activities of Rivaroxaban.
Urokinase	Iloprost may increase the anticoagulant activities of Urokinase.
Pentosan polysulfate	Iloprost may increase the anticoagulant activities of Pentosan polysulfate.
Aripiprazole	Aripiprazole may increase the hypotensive activities of Iloprost.
Aripiprazole lauroxil	Aripiprazole lauroxil may increase the hypotensive activities of Iloprost.
Nicorandil	Iloprost may increase the hypotensive activities of Nicorandil.
Valsartan	Iloprost may increase the hypotensive activities of Valsartan.
Ramipril	Iloprost may increase the hypotensive activities of Ramipril.
Esmolol	Iloprost may increase the hypotensive activities of Esmolol.
Betaxolol	Iloprost may increase the hypotensive activities of Betaxolol.
Reserpine	Iloprost may increase the hypotensive activities of Reserpine.
Remikiren	Iloprost may increase the hypotensive activities of Remikiren.
Torasemide	Iloprost may increase the hypotensive activities of Torasemide.
Bethanidine	Iloprost may increase the hypotensive activities of Bethanidine.
Guanadrel	Iloprost may increase the hypotensive activities of Guanadrel.
Metoprolol	Iloprost may increase the hypotensive activities of Metoprolol.
Isradipine	Iloprost may increase the hypotensive activities of Isradipine.
Olmesartan	Iloprost may increase the hypotensive activities of Olmesartan.
Chlorthalidone	Iloprost may increase the hypotensive activities of Chlorthalidone.
Nitroprusside	Iloprost may increase the hypotensive activities of Nitroprusside.
Atenolol	Iloprost may increase the hypotensive activities of Atenolol.
Diltiazem	Iloprost may increase the hypotensive activities of Diltiazem.
Minoxidil	Iloprost may increase the hypotensive activities of Minoxidil.
Timolol	Iloprost may increase the hypotensive activities of Timolol.
Treprostinil	Iloprost may increase the hypotensive activities of Treprostinil.
Amlodipine	Iloprost may increase the hypotensive activities of Amlodipine.
Nimodipine	Iloprost may increase the hypotensive activities of Nimodipine.
Nisoldipine	Iloprost may increase the hypotensive activities of Nisoldipine.
Bendroflumethiazide	Iloprost may increase the hypotensive activities of Bendroflumethiazide.
Prazosin	Iloprost may increase the hypotensive activities of Prazosin.
Fosinopril	Iloprost may increase the hypotensive activities of Fosinopril.
Trandolapril	Iloprost may increase the hypotensive activities of Trandolapril.
Metolazone	Iloprost may increase the hypotensive activities of Metolazone.
Lercanidipine	Iloprost may increase the hypotensive activities of Lercanidipine.
Benazepril	Iloprost may increase the hypotensive activities of Benazepril.
Bosentan	Iloprost may increase the hypotensive activities of Bosentan.
Propranolol	Iloprost may increase the hypotensive activities of Propranolol.
Clonidine	Iloprost may increase the hypotensive activities of Clonidine.
Enalapril	Iloprost may increase the hypotensive activities of Enalapril.
Doxazosin	Iloprost may increase the hypotensive activities of Doxazosin.
Labetalol	Iloprost may increase the hypotensive activities of Labetalol.
Cyclothiazide	Iloprost may increase the hypotensive activities of Cyclothiazide.
Bisoprolol	Iloprost may increase the hypotensive activities of Bisoprolol.
Candoxatril	Iloprost may increase the hypotensive activities of Candoxatril.
Nicardipine	Iloprost may increase the hypotensive activities of Nicardipine.
Guanabenz	Iloprost may increase the hypotensive activities of Guanabenz.
Mecamylamine	Iloprost may increase the hypotensive activities of Mecamylamine.
Losartan	Iloprost may increase the hypotensive activities of Losartan.
Moexipril	Iloprost may increase the hypotensive activities of Moexipril.
Phentolamine	Iloprost may increase the hypotensive activities of Phentolamine.
Eplerenone	Iloprost may increase the hypotensive activities of Eplerenone.
Lisinopril	Iloprost may increase the hypotensive activities of Lisinopril.
Nitroglycerin	Iloprost may increase the hypotensive activities of Nitroglycerin.
Metyrosine	Iloprost may increase the hypotensive activities of Metyrosine.
Hydroflumethiazide	Iloprost may increase the hypotensive activities of Hydroflumethiazide.
Cryptenamine	Iloprost may increase the hypotensive activities of Cryptenamine.
Perindopril	Iloprost may increase the hypotensive activities of Perindopril.
Candesartan cilexetil	Iloprost may increase the hypotensive activities of Candesartan cilexetil.
Tolazoline	Iloprost may increase the hypotensive activities of Tolazoline.
Fenoldopam	Iloprost may increase the hypotensive activities of Fenoldopam.
Indapamide	Iloprost may increase the hypotensive activities of Indapamide.
Tadalafil	Iloprost may increase the hypotensive activities of Tadalafil.
Alprenolol	Iloprost may increase the hypotensive activities of Alprenolol.
Eprosartan	Iloprost may increase the hypotensive activities of Eprosartan.
Chlorothiazide	Iloprost may increase the hypotensive activities of Chlorothiazide.
Quinapril	Iloprost may increase the hypotensive activities of Quinapril.
Omapatrilat	Iloprost may increase the hypotensive activities of Omapatrilat.
Phenoxybenzamine	Iloprost may increase the hypotensive activities of Phenoxybenzamine.
Pindolol	Iloprost may increase the hypotensive activities of Pindolol.
Telmisartan	Iloprost may increase the hypotensive activities of Telmisartan.
Methyldopa	Iloprost may increase the hypotensive activities of Methyldopa.
Hydrochlorothiazide	Iloprost may increase the hypotensive activities of Hydrochlorothiazide.
Guanfacine	Iloprost may increase the hypotensive activities of Guanfacine.
Trichlormethiazide	Iloprost may increase the hypotensive activities of Trichlormethiazide.
Felodipine	Iloprost may increase the hypotensive activities of Felodipine.
Irbesartan	Iloprost may increase the hypotensive activities of Irbesartan.
Nitrendipine	Iloprost may increase the hypotensive activities of Nitrendipine.
Deserpidine	Iloprost may increase the hypotensive activities of Deserpidine.
Pentolinium	Iloprost may increase the hypotensive activities of Pentolinium.
Trimethaphan	Iloprost may increase the hypotensive activities of Trimethaphan.
Diazoxide	Iloprost may increase the hypotensive activities of Diazoxide.
Carvedilol	Iloprost may increase the hypotensive activities of Carvedilol.
Bretylium	Iloprost may increase the hypotensive activities of Bretylium.
Terazosin	Iloprost may increase the hypotensive activities of Terazosin.
Guanethidine	Iloprost may increase the hypotensive activities of Guanethidine.
Rescinnamine	Iloprost may increase the hypotensive activities of Rescinnamine.
Acebutolol	Iloprost may increase the hypotensive activities of Acebutolol.
Captopril	Iloprost may increase the hypotensive activities of Captopril.
Nadolol	Iloprost may increase the hypotensive activities of Nadolol.
Bepridil	Iloprost may increase the hypotensive activities of Bepridil.
Hydralazine	Iloprost may increase the hypotensive activities of Hydralazine.
Bevantolol	Iloprost may increase the hypotensive activities of Bevantolol.
Practolol	Iloprost may increase the hypotensive activities of Practolol.
Polythiazide	Iloprost may increase the hypotensive activities of Polythiazide.

Target Protein

Prostacyclin receptor PTGIR

Prostaglandin E2 receptor EP2 subtype PTGER2

Prostaglandin E2 receptor EP1 subtype PTGER1

3',5'-cyclic-AMP phosphodiesterase 4A PDE4A

3',5'-cyclic-AMP phosphodiesterase 4B PDE4B

3',5'-cyclic-AMP phosphodiesterase 4C PDE4C

3',5'-cyclic-AMP phosphodiesterase 4D PDE4D

Tissue-type plasminogen activator PLAT

Prostaglandin D2 receptor 2 PTGDR2

Referensi & Sumber

Artikel (PubMed)

PMID: 14555558
Olschewski H, Rohde B, Behr J, Ewert R, Gessler T, Ghofrani HA, Schmehl T: Pharmacodynamics and pharmacokinetics of inhaled iloprost, aerosolized by three different devices, in severe pulmonary hypertension. Chest. 2003 Oct;124(4):1294-304. doi: 10.1378/chest.124.4.1294.
PMID: 22115402
John J, Palevsky H: Clinical pharmacology and efficacy of inhaled iloprost for the treatment of pulmonary arterial hypertension. Expert Rev Clin Pharmacol. 2011 Mar;4(2):197-205. doi: 10.1586/ecp.10.136.
PMID: 12388660
Schermuly RT, Schulz A, Ghofrani HA, Meidow A, Rose F, Roehl A, Weissmann N, Hildebrand M, Kurz J, Grimminger F, Walmrath D, Seeger W: Pharmacokinetics and metabolism of infused versus inhaled iloprost in isolated rabbit lungs. J Pharmacol Exp Ther. 2002 Nov;303(2):741-5. doi: 10.1124/jpet.303.2.741.
PMID: 1379160
Grant SM, Goa KL: Iloprost. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in peripheral vascular disease, myocardial ischaemia and extracorporeal circulation procedures. Drugs. 1992 Jun;43(6):889-924. doi: 10.2165/00003495-199243060-00008.
PMID: 35870081
Crooks S, Shaw BH, Andruchow JE, Lee CH, Walker I: Effectiveness of intravenous prostaglandin to reduce digital amputations from frostbite: an observational study. CJEM. 2022 Sep;24(6):622-629. doi: 10.1007/s43678-022-00342-9. Epub 2022 Jul 23.

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