anti histamin ( dra. yanti )
DESCRIPTION
antihistaminTRANSCRIPT
![Page 1: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/1.jpg)
AUTAKOIDHISTAMIN, ANTIHISTAMIN &
SEROTONIN
Dra. Yanti Mariana
![Page 2: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/2.jpg)
AUTAKOID
1. Amine : histamin serotonin
2. Polipeptide : angiotensin bradikinin / kinin
3. Lipid : Prostaglandin
![Page 3: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/3.jpg)
AUTAKOIDANTIHISTAMIN, ANTISEROTONIN
Autakoidhistamin prostaglandinserotonin angiotensinogenkinin – bradikinin slow reacting
subtance A (SRS-A)
![Page 4: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/4.jpg)
HISTAMIN ENDOGEN
Kadar tinggi = kulit, mukosa usus, paruSumber, sintesa = HISTIDIN
HISTIDIN Histidin dekarboksilase
HISTAMINGudang utama = sel mast
sel basofil
![Page 5: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/5.jpg)
PERANAN HISTAMIN ENDOGEN
Pada keadaan alergi / hipersensitivitasReaksi antigen – antibodi dilepaskan =
- Histamin- Autakoid lain =
- kinin- SRS-A / Slow Reacting
Substance A
![Page 6: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/6.jpg)
ALERGEN : a.1 = obat racun
Gejala alergi :urtikariaasma bronkialreaksi anafilaksisangioneurotik udemudem laring
![Page 7: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/7.jpg)
ANTIHISTAMINKompetitif menghambat interaksi histamin dengan
reseptor histamin = H1, H2
A. Antihistamin penghambat reseptor H1 (AH1) = antihistamin, antialergi
B. Antihistamin penghambat reseptor H2 (AH2) sejak 1972menghambat sekresi asam lambung akibat histamin
![Page 8: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/8.jpg)
ANTIHISTAMIN PENGHAMBAT RESEPTOR H1 (AH1)
KIMIA : AR1 H X - - CH2 - - CH2 - - N AR2 H
FARMAKOLOGIAntagonisme terhadap histamin
- otot polos : usus, bronkus, pembuluh darah- reaksi anafilaksis dan alergi = beberapa refrakterudem, eritem, pruritus, rasa gatal : dipengaruhi sangat baik. hipotensi = kurang dipengaruhi bronkokonstriksi = sangat sedikit dipengaruhi (oleh leukotrien)
Untuk darurat : EPINEPRIN
![Page 9: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/9.jpg)
KEL. EKSOKRIN
SalivaKel. eksokrin lainCairan lambung : tak dapat dilawan
Susunan Saraf Pusatmerangsang / menghambat
untuk : mual, muntah mabuk perjalanan (‘motion sickness’)
misalnya : oleh etanolaminAnastesi lokal : prometazin
pirilamin
“ atropin like”
![Page 10: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/10.jpg)
Antikolinergik :seperti atropin mulut kering, kesukaran miksi, impotensi
Kardiovaskuler :dosis terapi efek tak berarti
Efek samping :jarang serious, kadang-kadang hilang bila obat diteruskan
![Page 11: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/11.jpg)
FARMAKOKINETIKOral, enteral
Oral : mula kerja 15 - 30 menit efek maksimal : 1-2 jam lama kerja : 4-6 jam
(klorsiklizin : 8-12 jam)
Biotransformasi : hati, paru, ginjal
Ekskresi : urin
![Page 12: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/12.jpg)
INTOKSIKASIINDIKASI :
Pencegahan dan pengobatan alergi (sifat paliatif)- baik untuk : urtikaria akutpolinosis, Hay fever- asma bronkial ringan . . . . profilaksis- untuk reaksi anafilaktik : sebagai tambahan- angioneurotik udem (dengan udem laring sebagai tambahan)
![Page 13: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/13.jpg)
ANTIHISTAMIN1. Gol. Amino alkil eter = Etanolamine
* difenhidramin : utk. motion sicknessG.I.T. < - sering parenteral- insidens ngantuk tinggiKarbinoksaminKlemastinDimenhidrinat : M.S.
2. Gol. EtilenediaminTripelenamin G.I.T. : >Pirilamin
![Page 14: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/14.jpg)
ANTIHISTAMIN3. Gol. Alkilamin
* Klorfeniramin : sering pada prep. batuk, ngantuk < Bromfeniramin
4. Gol. Fenotiazin Metdilazin Prometazin : efek sedasi jelas, M.S.
5. Lain-lain :* Siproheptadin : cold-urticaria Azatadin
![Page 15: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/15.jpg)
ANTIHISTAMIN6. “Nonsedatif”
TerfenadinAstemizolLoratadin
7. PiperazineSiklisin (Cyclizine)Meklisin (Meclizine)
![Page 16: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/16.jpg)
INTENSITAS EFEK BEBERAPA ANTIHISTAMIN
Gol. Anti- Sedatif Anti- Anti- Sal.histamin k’nergik emetik
cerna
1. Etanolamin + sd 2+ + sd 3+ 3+ 2+ sd 3+ +
2. Etilendiamin + sd 2+ + sd 2+ (-) - 3+
3. Alkilamin 2+ sd 3+ + sd 2+ 2+ - +
4. Piperazin 2+ sd 3+ + sd 3+ + 3+ +
5. Fenotiazin + sd 3+ 3+ 3+ 4+ -
![Page 17: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/17.jpg)
PENGGUNAAN KLINIK ANTIHISTAMIN
1. Reaksi & alergi
2. “Motion-sickness” dan gangguan
vestibuler
3. Nausea dan vomitus pada kehamilan
4. Penyakit parkinson
![Page 18: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/18.jpg)
ANTI ALERGI LAIN• KETOTIFEN
Antihistamin kuatProfilaksis asma bronkial- menghambat penglepasan histamin- oral -- 12 bulan
Efek samping :- pernah dilaporkan me BB nafsu makan- kombinasi dg antidiabetik oral me jumlah
trombosit (reversibel)- alergi
![Page 19: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/19.jpg)
ANTI ALERGI LAIN• CROMOLYN SODIUM / Na. KROMOLIN
- Menghambat Release* histamin* lain autakoid a.l. leukotriene- Pencegahan asma bronkial- Iritasi lokal, hipersensitif- Inhalasi- Indikasi lain : rinitis alergika atopik pada mata (obat tetes)
![Page 20: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/20.jpg)
Efek Samping :Seperti antihistamin :
- ngantuk- atropin-like
BB anak : mulut kering
KETANSERINJuga mempunyai reseptor adrenergik
histamindopamin
Antihipertensi
![Page 21: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/21.jpg)
ANTAGONIST RESEPTOR HISTAMIN H2
SimetidinRanitidin>< gastrin, asetilkolinAntagonis bersaing ---- reversibel
Absorpsi, nasib ekskresi :- sedikit dipengaruhi makanan, antasid- puncak : 1 - 2 jam- ranitidin : efektif untuk 8-12 jam
derivat imidazol
![Page 22: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/22.jpg)
Penggunaan :
Hipersekresi asam lambung- ulkus duodeni 35 - 90 %- zollinger Ellison syndrome (gastrin >>)- ulkus lambung 50-75 %
![Page 23: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/23.jpg)
Efek samping :
Simetidin : anti androgen - hilangnya libido, impoten, ginekomastia
IV / oral kronik : prolaktin Menghambat enzim oxidase : mempengaruhi metabolisme obat lain : warfarin, fenitoinGangguan SSP terutama pada usia lanjut
(Ranitidin lebih ringan)Trombositopenia, granulositopeniaHepatotoksik, nefrotoksikKreatinin
![Page 24: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/24.jpg)
Simetidin, ranitidin : IV cepat - bradikardia, kardiotiksik
G.I.T.C.N.S.Insuf. vaskulerFibrosis inflamasi
Fibrosis retroperitonealFibrosis endocardialFibrosis paru-paru
Kerusakan katup jantung
![Page 25: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/25.jpg)
SIPROHEPTADIN• Struktur mirip fenotiazin• Juga antagonis H. (Antihistamin)
Kegunaan :Seperti Antihistamin :
- alergi kulit (pruritus)- cold urticaria
Sebagai anti serotonin- postgastrectomy dumping syndrome- diare pada karsinoid
![Page 26: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/26.jpg)
SEROTONIN(5. HIDROKSI TRIPTAMIN)Sel enterokromafin (90 %)TrombositCNS - Neurotransmitter
Triptofanhidroksilasi 5 Hidroksi Triptofandekarboksilasi 5 Hidroksi TriptaminMAO 5 Hidroksi Indole Acetic Acid(5.HIAA)
![Page 27: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/27.jpg)
TUMOR KARSINOIDEFEK FARMAKOLOGIK
C.V : TD Triphasic- Otot polos GIT
Bronkus
- Syaraf, GGL, Medula adrenal
- Trombosit > Hipotalamus
stimulasi
![Page 28: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/28.jpg)
NORMAL KARSINOID 2 % 60 % Triptofan
Serotonin
0,1 - 0,3 mcg/ml 0,5 - 2,7 mcg/ml
2 - 10 mg / 24 jam 25 mg - 1 gr / 24 jam
![Page 29: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/29.jpg)
ANTAGONIST SEROTONINa.l.Der. Lysergic acid, alkaloid ergot, klorpromasinYang digunakan : Metisergid
Siproheptadin Ketanserin
METISERGID >< VASOKONSTRIKSI- der. lysergic acid, mirip metil-ergonovin- profilaktik migrain dan sakit kepala vaskular- “rebound headache”- karsinoid- postgastrectomy dumping syndrome
![Page 30: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/30.jpg)
SINTESA DAN METABOLISME ANGIOTENSIN
AngiotensinogenRenin
Angiotensin IConverting-ensyme
Angiotensin II = AngiotensinAminopeptidase
Angiotensin II = AngiotensinAngiotensinase
Peptida
![Page 31: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/31.jpg)
ANTAGONIS SISTEM RENIN ANGIOTENSIN
1. Menghambat sekresi reninClonidinePropranololMetildopa
2. Inhibitor reninN-acetylpepstatin
3. Inhibitor “converting enzyme”TeprotideCaptopril
4. Antagonist angiotensinSaralasin
![Page 32: Anti Histamin ( Dra. Yanti )](https://reader030.vdocuments.net/reader030/viewer/2022033008/5695d35e1a28ab9b029db256/html5/thumbnails/32.jpg)