Hubungan Struktur-aktivitas

Antihistamin H2
Siti Rahmah KR
CIMEDITIN

RANITIDIN

FAMOTIDIN

NIZATIDIN
Histamin merupakan amine aktif yang ditemukan di jaringan,
mempunyai efek fisiologis dan patologis yang kompleks,
bekerja pada reseptor tertentu, dan biasanya dilepas secara
Iokal.
Mekanisme pelepasan histamin, dapat melalui dua cara :
1. Secara imunologik, dimana sel mast dan basofil
disensitisasi oleh Ig E, Ialu menempel pada membran sel.
Ketika terpapar antigen, histamin mengalami degranulasi
sehingga muncul gejala alergi (reaksi hipersensitif tipe I)
2. Secara mekanik dan kimia, dimana terjadi trauma meknik
dan trauma kimia sehingga merangsan kerja sel mast
Histamin berikatan dengan reseptor spesifik di
membran sel :
H1 : Otot polos, endotel, otak
H2 : Mukosa gaster, otot jantung, sel mast, otak
H3 : Presinap otak-dan plexus myentericus
H4 : Eosinofil, neutrofil, CD4 Tcell
ANTIHISTAMIN H2
CIMETIDIN
Cimetidine is used to inhibit stomach acid
production and is used in the treatment of
heartburn and peptic ulcers,
RANITIDIN
• Ranitidine, is a medication that decreases stomach acid
production. It is commonly used in treatment of peptic ulcer
disease, gastroesophageal reflux disease, and Zollinger-Ellison
syndrome. lt can be taken by mouth , by injection into a muscle,
or into a vein.[2]
• It is generally safe in pregnancy. Ranitidine is an H2histamine
receptor antagonist that works by blocking histamine and thus
decreasing the amount of acid released by cells of the stomach
FAMOTIDIN
• Famotidine, merupakan antagonis reseptor H2 histamin yang bekerja
menghambat produksi asam Iambung. Famotidin digunakan untuk mengobati
pepetic ulcer dan penyakit GERD.
Medical use:
• Relief of heartburn, acid indigestion, and sour stomach
• Treatment for gastric and duodenal ulcers
• Treatment for pathologic gastrointestinal hypersecretory conditions such as
Zollinger-ElIison syndrome and multiple endocrine adenomas
• Treatment for gastroesophageal reflux disease (GERD)
• Treatment for esophagitis
• Part of a multidrug regimen for Helicobacter pylori eradication, although
omeprazole may be somewhat more effective. [4][5][6][7][8][9]
• Prevention of NSAlD-induced peptic ulcers. [10][11]
• Given to surgery patients before operations to reduce the risk of aspiration
pneumonitis.
• 10 mg and 20 mg tablets
NIZATIDIN
• Nizatidine is a histamine H2receptor
antagonist that inhibits stomach acid
production, and is commonly used in the
treatment of peptic ulcer disease and
gastroesophageal reflux disease.