Selamat

Datang
Peserta
Lokakarya

Paulus Kurnia
Bagian Farmakologi FKUH
UNIVERSITAS HASANUDDIN

ANATOMI SALURAN
CERNA

MEKANISME SEKRESI
ASAM LAMBUNG

HISTOLOGI LAMBUNG

Faktor Faktor FaktorDefensif FaktorAgresif Agresif Defensif .

Nitric oxide .Merokok .Ulcus Pepticum Ketidakseimbangan antara faktor AGRESIF & DEFENSIF Faktor Defensif Faktor Agresif -Mukus .H Pylori -Aliran darah .OAINS -Prostaglandin .Asam lambung -Bicarbonate .

H2-Receptor Antagonists (Ranitidin) 3.Kelompok Obat Ulcus Pepticum 1. Antibiotics (Triple combination) . PGE1 Analogs (Misoprostol) 6. Proton Pump Inhibitors (Omeprazole) 4. M1 Blocker (Pirenzipine) 5. Cytoprotectans ( Sucralfate) 7. Antasida 2.

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1. Antasida Sodium bicarbonate CaCO3 Al3+ hydroxides Mg2+ hydroxide Mg Trisilicate .

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mual.acid rebound. Antasida • Diberikan oral 1-3 jam setelah makan / sebelum makan • Preparat Mg+2 meningkatkan motilitas usus (laksatif) – ES : Diare • Preparat Al+3 merelaksasi otot polos usus – ES : Konstipasi • Preparat Ca+2 menghasilkan gas CO2 – ES : perut kembung. konstipasi . flatulence.

enchephalopathy.Efek Samping Toksisitas Aluminum yang berhub. myopathy Hypercalcemia Phosphate retention Calcium precipitation in the kidney Mengganggu absorpsi beberapa obat Take 2 hrs before or after other drugs . dengan Peny.Ginjal Osteoporosis.

2.H2RAs Menghambat secara kompetitif dan reversibel terhadap reseptor H2 yang terdapat pada membran sel parietal basolateral lambung Kurang potent dibandingkan PPIs tetapi tetap menekan asam lambung 70% dalam waktu 24 Jam .

400 mg) H2-blocker I yg tersedia Menghambat enzim P450 => Interaksi obat Ranitidine (150 .As H2 receptor blockers Cimetidine (200 . 40 mg ) . 300 mg) ≠ Enzim P450 => Efek smping minimal Nizatidine (300 mg) Famotidine ( 20 .

Farmakokineti kdiabsorpsi Cepat : setelah pemberian Konsentrasi serum mencapai puncak 1-3 jam Level Terapeutik dipertahankan sampai 12 jam Ikatan protein plasmanya hanya 20 % Dimetabolisme di hati 10% s/d 35 % Obat dan metabolitx diekskresikan oleh ginjal (**kurangi dosis pada gangguan faal ginjal) .

delirium in the elderly Associated with thrombocytopenia Cimetidine anti-androgen effects .Efek Samping H2RAs All less than 3% Diarrhea Headache Drowsiness Fatigue Muscular pain Constipation Much less common Confusion.

absorpsi baik. mencapai peredaran darah dan bisa sampai ke sel parietal. • Obat ini diberikan dalam bentuk kapsul yang dilapisi gelatin. 3. . untuk mencegah pemecahan oleh asam lambung. sehingga bisa mencapai usus halus. memblokade 98% sekresi asam pada berbagai bentuk ulkus dan sindroma zollinger-Ellison hipersekresi.PPIs • Penekan sekresi asam lambung yang paling poten • Efek penekan asam bekerja 24-48 Jam • Penghambat pompa proton Irreversibel.

PPIs • Penghambat secara ireversibel H+/K+ATPase dengan tujuan : – Blok sekresi asam lambung – Menurunkan konsentrasi Pepsin – Meningkatkan pH gastric • Sekresi asam hanya bisa tercapai bila pompa proton baru ada • Steady-state inhibition (affecting 70% of pumps) bisa sampai 2 – 5 hari .

masuk ke sirkulasi sistemik.Farmakologi PPI Obat bekerja ketika pH dibawah 4  setelah diabsorpsi.kmdn akan berdifusi ke sel parietal lambung Biovailabilitas menurun dengan makanan Sangat efektif bekerja setelah puasa lama ketika sejumlah pompa proton aktif (mis : ketika seblum sarapan) .

30 mg(1x1) Omeprazole 10 mg. Sediaan PPI yg Ada saat ini Esomeprazole 20.40mg (1x1) Lansoprazole 15.40 mg (1x1)  Rabeprazole 10. 20 mg (1x1) . 20 mg (1x1) Pantoprazole 20.

Metabolisme PPI Cepat diserap Ikatan protein kuat Dimetabolisme dihati oleh sitokrom P450 (CYP2C19 and CYP3A4) Sisa metabolites sulfat diekskresikan lewat feces dan urin Penyakit hati mengurangi clearance dari lansoprazole( kurangi dosis ) .

• Menghambat reseptor kolinergik muskarinik selektif di reseptor M1 di lambung • Bisa menghambat produksi asam basal 40 – 50 % •Afinitas sgt rendah pd reseptor di otot jantung& otot polos •Dosis 50 mg (2x1) •Sediaan 25 mg/tab •Jarang digunakan sekarang .

PGE1 Analogs ( Misoprostol) PGE2.5.1 and PGI2 Disintesis mukosa lambung Acid-reducing effects Bind to EP3 receptors on parietal cells Decrease acid production Efek sitoprotective Stimulation of mucin and bicarbonate Increase mucosal blood flow Contrast with NSAIDS which diminish prostaglan formation by inhibition of cycloxygenase and lea ulcer formation .

Farmakokinetik  Cepat diserap Efek terapeutik mencapai puncak dalam waktu 60-90 minutes Bertahan hanya sampai 3 jam (qid dose required) .

Samping : Diarrhea ± abdominal cramps as high as 30% Begins within 2 weeks and often resolves spontaneously in 1 week Can exacerbate inflammatory bowel disease Contraindicated during pregnancy trimester 1 (uterotrofik) .

Nsaid induced) .Dosis :  Misoprostol 200 microgram (4x1)  Terutama sebagai profilakasis tukak peptik pada pasien beresiko tinggi (lansia.

6. adsorbs pepsin Binds bile acids Not absorbed => essentially free of side effects .Cytoprotectans (Sucralfate) Sulfated polysaccharide Acid activated (pH ‹ 4) Administered on an empty stomach 1 hr before meals Stimulates local prostaglandin synthesis.

Indikasi dan Dosis  Tukak lambung dan duodenum  1 gr 4x sehari 1 jam sebelum makan .

fluroquinolone antibiotics) . digoxin. cimetidine. Efek Samping Constipation (2 %) Avoid in renal failure May impair absorption of other drugs (inhibit absorption phenytoin. ketoconazole.

Antibiotic for Peptic Ulcer Antibiotic ulcer therapy: Combinations must be used: -Bismuth – disrupts cell wall of H. or due to intolerance by the patient Standard treatment regimen for peptic ulcer: PPI + Clarithromycin 500 mg + Amoxicilln 500 mg . 7. pylori -Clarithromycin – inhibits protein synthesis -Amoxicillin – disrupts cell wall -Tetracyclin – inhibits protein synthesis -Metronidazole – used often due to bacterial resistance to amoxicillin and tetracyclin.

Terima Kasih .

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anticholinergics. not a disease Disorder of movement through the colon and/or rectum Can be caused by many diseases or drugs(opium.clonidine ) .antacid.Constipation Abnormally infrequent and difficult passage of feces through the lower GI tract Symptom.

Laxatives: Mechanism Bulk forming of Action High fiber Absorbs water to increase bulk Distends bowel to initiate reflex bowel activity Examples: psyllium (plantago) methylcellulose Calsium polycarbophil Agar(hydrophilic colloid) .

Laxatives: Mechanism Emollient of Action Stool softeners and lubricants Promote more water and fat in the stools Lubricate the fecal material and intestinal walls Examples:  Dioktilnatrium sulfosuksinat  Parafin cair  Minyak zaitun .

Laxatives: Mechanism Stimulant cathartics of Action Increases peristalsis via intestinal nerve stimulation Examples: minyak jarak sena cascara bisacodyl fenolftalein .

Laxatives: Side Effects  Bulk forming Impaction Fluid overload  Emollient Skin rashes • Decreased absorption of vitamin  Stimulant Nutrient malabsorption Skin rashes Gastric irritation Rectal irritation .

Antidiarrheals .

Causes of Diarrhea Acute Diarrhea Chronic Diarrhea Bacterial Tumors Viral Diabetes Drug induced Hyperthyroidism Nutritional/Alergy Irritable bowel Protozoal syndrome Food Intoxication Psychogenic .

thereby allowing fluid absorption from the intestinal contents Examples:  Anticholinergics  Protectants/adsorbents  Opiate-related agents  Probiotics  Antibiotics .Antidiarrheals Drugs that decrease peristalsis.

butilbromida  Propantheline bromida  Scopolamin metil .Antidiarrheals Anticholinergics are used to treat tenemus and vomiting Examples:  Atropine  Ekst Belladona  Hiosin N .bromida Side effects include dry mucous membranes. tachycardia. urine retention. and constipation .

Antidiarrheals Protectants/adsorbents coat inflamed intestinal mucosa with a protective layer (protectants) or bind bacteria and/or digestive enzymes and/or toxins to protect intestinal mucosa from damaging effects (adsorbents) Examples:  Bismuth subsalicylate (bismuth + aspirin-like product)  Kaolin/pectin  Attapulgite  simethicone Side effects include constipation .

Antidiarrheals Opiate-related agents control diarrhea. urine retention. and constipation SP: < 2years. bloat. lactation . pregnancy. ileus. or absorption (µ & δ receptors) Examples:  Diphenoxylate  Loperamide Side effects include CNS depression. intestinal secretion (δ receptors).  MOA : effects on intestinal motility (µ receptors).

Bio GI.Antidiarrheals Probiotics seed the GI tract with beneficial bacteria. Lacbon . use is based on the theory that some forms of diarrhea are caused by disruption of the normal bacterial flora of the GI tract Must be refrigerated to maintain the viability of the bacteria Examples:  Plain yogurt with active cultures  Variety of trade-name products Eg : L-Bio.

Antibiotic A theory regarding the development of diarrhea is that anaerobic bacteria may increase due to disruption of normal GI flora One way to treat this is to use an antibiotic effective against anaerobic bacteria Metronidazole is an example of an antibiotic used to treat diarrhea. .

GIT Regulator  Antagonist dopamine:(cholinergic effect) -metoclopramide -domperidone  Cholinomimetic indirect: cisapride .

Antibiotic Quinolone Chloramphenicol Tetracycline Cotrimoxazole Metronidazole .

Antiviral Lamivudine Adefovir dipivoxil Telbivudine Interferon/pegylated interferon .

semua : dbn. PF : KU baik. datang dengan keluhan nyeri ulu hati yang hilang timbul sejak 5 hari yg lalu.kasus 1. kadang sendawa. Seorang wanita. Juga disertai rasa mual. karyawati. kec adanya nyeri tekan epigastrium. belum menikah. Bila saudara memilik terapi empirik. obat apa saja yang akan saudara berikan?tuliskan resepx1 .. Keluhan tersebut dirasakan baik pada waktu perut kosong maupun setelah makan. 26 tahun. kembung dan nanfsu makan berkurang.