Peringatan Keamanan

In neonatal patients given alprostadil intravenously, apnea, bradycardia, pyrexia, hypotension, and flushing may be signs of drug overdosage. In patients with apnea or bradycardia, discontinue the infusion, and provide appropriate medical treatment. Caution should be used in restarting the infusion. In patients with pyrexia or hypotension, reduce the infusion rate until these symptoms subside. Flushing is usually a result of incorrect intraarterial catheter placement, and the catheter should be repositioned.L45038

For patients given alprostadil intracavernosally for the treatment of erectile dysfunction, there is limited data on overdosage. Systemic reactions are uncommon with the intracavernous use of alprostadil, and hypotension occurrs in less than 1% of patients treated with this drug. A prolonged erection or priapism is the main symptom of an alprostadil overdose in this group of patients. Erections lasting more than 6 hours should be treated due to the potential for tissue hypoxia and possible necrosis. In the event of an intracavernous overdose, the patient is strongly encouraged to go to the nearest emergency room if his personal physician is not available. Supportive therapy according to the presence of other symptoms is recommended.L45028,L45033

The oral LD50 of alprostadil in mice and rats is 186 mg/kg and 228 mg/kg, respectively.L45043,L45073

Alprostadil

DB00770

small molecule approved investigational

Deskripsi

Alprostadil is a chemically-identical synthetic form of prostaglandin E1 (PGE1), a potent vasodilator produced endogenously. In 1996, the FDA approved the use of alprostadil, administered either with an intracavernosal injection or an intraurethral suppository, for the treatment of erectile dysfunction, and it is used in men for whom oral treatment is either contraindicated or ineffective. After administration, alprostadil promotes smooth muscle relaxation of the corpus cavernosal.A257068,A257088

Alprostadil is also used in neonatal patients with congenital heart defects that depend on a patent ductus for survival until corrective or palliative surgery can be performed. This drug causes vasodilation by directly affecting vascular and ductus arteriosus (DA) smooth muscle, preventing or reversing the functional closure of the DA that occurs shortly after birth. This results in increased pulmonary or systemic blood flow in infants.A34474,L45038,L45063

Struktur Molekul 2D

Berat 354.487
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In healthy adults and neonates given a single intravenous dose of alprostadil, half-life goes from 5 to 10 minutes.[L45063]
Volume Distribusi The volume of distribution of alprostadil has yet to be determined.[L45028]
Klirens (Clearance) In patients with erectile dysfunction given an intravenous infusion of alprostadil (20 ?g), the total body clearance was 115 L/min.[L45033]

Absorpsi

In patients with erectile dysfunction given 20 ?g of alprostadil intracavernously, the systemic plasma concentrations of prostaglandin E1 increased from a baseline of 0.8 pg/mL to a Cmax of 16.8 pg/mL (corrected for baseline). The tmax and AUC for this group of patients were 4.8 min and 173 pg?min/mL, respectively.L45033 In patients given 20 ?g of alprostadil intravenously, AUC was similar to the one detected in patients that received alprostadil intracavernously (174 pg?min/mL); however, they had a higher tmax (25.5 min) and a lower Cmax (7.09 pg/mL). Compared to the same dose given by a short-term intravenous infusion, the absolute bioavailability of alprostadil estimated from systemic exposure was about 98%.L45033

Metabolisme

Alprostadil is rapidly metabolized in the human body. Following intracavernous administration, alprostadil is metabolized in the corpus cavernosum, and a smaller portion is absorbed from the penis into systemic circulation.L45033 After intravenous or arterial administration, alprostadil is metabolized and distributed throughout the entire body except for the central nervous system.L45063 As much as 60-90% of the circulating alprostadil may be metabolized in the lungs through first-pass pulmonary elimination, in a process known as beta- and omega-oxidation.L45033 The enzymatic oxidation of the C15-hydroxy group of alprostadil leads to the formation of 15-keto-PGE1, while the reduction of the C13, 14-double bond produces 15-keto-PGE0, and 13,14-dihydro-PGE1 (PGE0). The 15-keto metabolites are inactive, but the PGE0 metabolite has a similar potency to alprostadil in isolated animal organs.L45033 The major metabolite of alprostadil is 15-keto-PGE0.A257068

Rute Eliminasi

Following the degradation of alprostadil by beta- and omega-oxidation, metabolites are excreted primarily by the kidney, and excretion is essentially complete within 24 hours after administration (92%).L45063 Approximately 88% and 12% of alprostadil metabolites are excreted through urine and feces, respectively, over 72 hours. Alprostadil and its metabolites are not retained in tissues, and unchanged alprostadil has not been detected in urine.L45033,L45063

Interaksi Obat

13 Data
Sildenafil The risk or severity of hypotension and priapism can be increased when Sildenafil is combined with Alprostadil.
Tadalafil The risk or severity of hypotension and priapism can be increased when Tadalafil is combined with Alprostadil.
Vardenafil The risk or severity of hypotension and priapism can be increased when Vardenafil is combined with Alprostadil.
Dipyridamole The risk or severity of hypotension and priapism can be increased when Dipyridamole is combined with Alprostadil.
Ibudilast The risk or severity of hypotension and priapism can be increased when Ibudilast is combined with Alprostadil.
Avanafil The risk or severity of hypotension and priapism can be increased when Avanafil is combined with Alprostadil.
Udenafil The risk or severity of hypotension and priapism can be increased when Udenafil is combined with Alprostadil.
Doxofylline The risk or severity of hypotension and priapism can be increased when Doxofylline is combined with Alprostadil.
Mirodenafil The risk or severity of hypotension and priapism can be increased when Mirodenafil is combined with Alprostadil.
Fostamatinib The risk or severity of hypotension and priapism can be increased when Fostamatinib is combined with Alprostadil.
Patent Blue The therapeutic efficacy of Alprostadil can be decreased when used in combination with Patent Blue.
Isosorbide mononitrate Alprostadil may increase the vasodilatory activities of Isosorbide mononitrate.
Iloprost Iloprost may increase the hypotensive activities of Alprostadil.

Target Protein

Thromboxane A2 receptor TBXA2R
Prostaglandin E2 receptor EP1 subtype PTGER1
Prostaglandin E2 receptor EP2 subtype PTGER2
Prostaglandin E2 receptor EP3 subtype PTGER3
Prostaglandin E2 receptor EP4 subtype PTGER4
Prostaglandin D2 receptor 2 PTGDR2

Referensi & Sumber

Synthesis reference: Rodríguez, A., et al. (1999), An Efficient Asymmetric Synthesis of Prostaglandin E1. Eur. J. Org. Chem., 1999: 2655-2662. https://doi.org/10.1002/(SICI)1099-0690(199910)1999:10<2655::AID-EJOC2655>3.0.CO;2-2
Artikel (PubMed)
  • PMID: 24369066
    Hanchanale V, Eardley I: Alprostadil for the treatment of impotence. Expert Opin Pharmacother. 2014 Feb;15(3):421-8. doi: 10.1517/14656566.2014.873789. Epub 2013 Dec 26.
  • PMID: 8785470
    Lea AP, Bryson HM, Balfour JA: Intracavernous alprostadil. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in erectile dysfunction. Drugs Aging. 1996 Jan;8(1):56-74. doi: 10.2165/00002512-199608010-00009.
  • PMID: 18473716
    Costabile RA, Mammen T, Hwang K: An overview and expert opinion on the use of alprostadil in the treatment of sexual dysfunction. Expert Opin Pharmacother. 2008 Jun;9(8):1421-9. doi: 10.1517/14656566.9.8.1421.
  • PMID: 6763200
    Heymann MA, Clyman RI: Evaluation of alprostadil (prostaglandin E1) in the management of congenital heart disease in infancy. Pharmacotherapy. 1982 May-Jun;2(3):148-55.
  • PMID: 17488147
    Degoute CS: Controlled hypotension: a guide to drug choice. Drugs. 2007;67(7):1053-76.

Contoh Produk & Brand

Produk: 42 • International brands: 38
Produk
  • Alprostadil
    Injection • 500 ug/1mL • Intravascular; Intravenous • US • Generic • Approved
  • Alprostadil
    Injection • 500 ug/1mL • Intravascular; Intravenous • US • Generic • Approved
  • Alprostadil
    Injection, solution, concentrate • 500 ug/1mL • Intravascular • US • Generic • Approved
  • Alprostadil
    Injection, solution, concentrate • 500 ug/1mL • Intravascular • US • Generic • Approved
  • Alprostadil Injection USP
    Solution • 500 mcg / mL • Intravascular • Canada • Approved
  • Alprostadil Injection, USP
    Liquid • 500 mcg / mL • Intra-arterial; Intravenous • Canada • Approved
  • Caverject
    Injection, powder, lyophilized, for solution • 5.4 ug/1mL • Intracavernous • US • Approved
  • Caverject
    Injection, powder, lyophilized, for solution • 10.5 ug/1mL • Intracavernous • US • Approved
Menampilkan 8 dari 42 produk.
International Brands
  • Alista
  • Alprostan — Zentiva
  • Alprostapint — Closter
  • Alprostar — Recordati
  • Alprostin — Pfizer
  • Alprox-TD
  • Altesil — Taiyo Pharmaceutical
  • Alyprost — Fuji Yakuhin
  • Apistandin — Fuji Yakuhin
  • Aplicav — Libbs

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