Penghambat fosfodiesterase tipe 5

Struktur kimia sildenafil (Viagra), contoh penghambat fosfodiesterase tipe 5

Penghambat fosfodiesterase tipe 5 atau disingkat menjadi penghambat PDE5 (Bahasa Inggris: phosphodiesterase type 5 inhibitor, disingkat PDE5 Inhibitor) adalah jenis obat yang sering kali digunakan untuk memicu ereksi pada penis, sehingga sering kali digunakan untuk menangani disfungsi ereksi. Salah satu contoh obat penghambat PDE5 adalah sildenafil atau viagra. Obat penghambat PDE5 juga digunakan untuk penyakit hipertensi paru dan juga bermanfaat untuk menangani penyakit jantung.[1]

Contoh

Tadalafil STADA Pharma - T20 - 20 mg

Kisah penghambat PDE5 bermula dari karya dokter dan ahli fisiologi Britania Raya Henry Hyde Salter yang pada tahun 1886 menyadari bahwa gejala asmanya mereda setelah minum secangkir kopi kental. Kini diketahui bahwa hal tersebut disebabkan oleh sifat bronkodilator kafein, penghambat PDE5 yang tidak selektif, meskipun lemah.[2] Pada tahun 1986, ilmuwan Pfizer di Sandwich, Britania Raya, memulai pekerjaan praklinis untuk mengembangkan penghambat PDE5 (yang kemudian dikenal sebagai sildenafil sitrat) untuk pengobatan angina.

Sildenafil, tadalafil, vardenafil, dan avanafil merupakan agen utama yang dipasarkan secara global, meskipun mirodenafil, udenafil, gisadenafil, yonkenafil (tunodafil), dan lodenafil tersedia di beberapa negara.[1] Agen lain dengan sifat penghambatan PDE5 yang lemah meliputi fenspirida, MBCQ, zaprinast, dan ikariin.[3]

Meskipun semua penghambat PDE5 memiliki mekanisme kerja yang sama, setiap agen memiliki farmakokinetika dan farmakodinamika yang berbeda yang memengaruhi seberapa cepat kerjanya, berapa lama efeknya bertahan, dan efek sampingnya. Khususnya, meskipun semua penghambat PDE5 secara khusus menghambat PDE5, tingkat penghambatan fosfodiesterase lainnya juga memengaruhi profil efek sampingnya. Misalnya, sildenafil juga menghambat PDE6 yang terdapat di retina mata; reaksi ini dianggap bertanggung jawab atas perubahan penglihatan sementara yang dialami beberapa pasien yang menggunakan sildenafil. Demikian pula tadalafil juga menghambat PDE11 yang terdapat di prostat, meskipun belum ada efek pada kesuburan yang dilaporkan. Meskipun agen yang lebih selektif untuk PDE5 sedang dalam tahap pengembangan, uji coba ini telah ditangguhkan, kemungkinan karena pasar telah jenuh dengan diperkenalkannya agen dengan manfaat kardiovaskular yang luas, seperti penghambat SGLT2 dan antagonis reseptor endotel.[1]

Meskipun demikian, penghambat PDE5 yang telah dipasarkan untuk disfungsi ereksi dan hipertensi arteri paru sedang menjalani penelitian dalam beberapa kondisi seperti hipertensi resisten, infark miokard, gagal jantung, klaudikasio intermiten, sindrom Raynaud, gagal ginjal kronis, dan diabetes melitus karena pemahaman kita yang lebih baik tentang sifat fisiologisnya yang luas.[1]

Referensi

  1. ^ a b c d Tzoumas N, Farrah TE, Dhaun N, Webb DJ (November 2019). "Established and emerging therapeutic uses of phosphodiesterase type 5 inhibitors in cardiovascular disease". British Journal of Pharmacology. doi:10.1111/bph.14920. PMID 31721165. 
  2. ^ Boswell-Smith V, Spina D, Page CP (January 2006). "Phosphodiesterase inhibitors". British Journal of Pharmacology. 147 Suppl 1 (S1): S252–7. doi:10.1038/sj.bjp.0706495. PMC 1760738 alt=Dapat diakses gratis. PMID 16402111. 
  3. ^ Dell'Agli M, Galli GV, Dal Cero E, Belluti F, Matera R, Zironi E, et al. (September 2008). "Potent inhibition of human phosphodiesterase-5 by icariin derivatives". Journal of Natural Products. 71 (9): 1513–7. doi:10.1021/np800049y alt=Dapat diakses gratis. PMID 18778098. 

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