Drug monograph

ชื่อยาทั่วไป (Generic Name): Omeprazole Lansozprazole

ชื่อการค้า (Trade name) LOSEC® PREVACID FDT ®
รูปแบบ/ ความแรง/ ขนาด Omeprazole 20 mg enteric coat capsule Lansozprazole 30 mg orodispersible tablet
บรรจุ (Dosage form/
Strength):
กลุ่มยา (Classification): Ulcer-healing drugs and drugs used in variceal bleeding; บัญชียา นอกบัญชียา
หลัก ก
ข้อบ่งใช้ (Approved -Eradication of Helicobacter pylori associated with peptic ulcer -Eradication of Helicobacter pylori associated with peptic
Indication): disease ulcer disease
-Acid-related dyspepsia -Acid-related dyspepsia
-Gastro-oesophageal reflux disease -Gastro-oesophageal reflux disease
-Prophylaxis of NSAID-induced ulcers -Benign gastric ulcer
-NSAID-associated ulceration -Prophylaxis of NSAID-induced ulcers
-Reflux oesophagitis -Erosive oesophagitis
-Duodenal ulcer -NSAID-associated ulceration
-Zollinger-Ellison syndrome -Reflux oesophagitis
-Duodenal ulcer
-Zollinger-Ellison syndrome
กลไกการออกฤทธิ์ ยับยั้งการทำงานของ H+/K+ ATPase ซึ่งทำหน้าที่เกี่ยวกับการหลังกรดเกลือในกระเพาะอาหาร โดยทำหน้าที่นำ H+ ออกจากเซลล์ pariental
(Mechanism of action): cell ออกสู่โพรงกระเพาะอาหารโดยแลกเปลี่ยนกับ K+ เอนไซม์ H+/K+ ATPase เป็นขั้นตอนการทำงานสุดท้ายของการหลั่งกรด โดยยาในกลุ่ม
PPIเป็น prodrug จะออกฤทธิ์ในสภาวะที่เป็นกรด โดยจะเปลี่ยนเป็น sulphenamind ซึ่งเป็นสารที่จับกับ sulfhydryl (SH) group ของ H+/K+
ATPase จึงยับยั้งเอนไซม์นอี้ ย่างถาวร (irreversible)ทำให้ยับยั้งการหลั่งกรด
ข้อควรระวัง/ ข้อห้ามใช้
(Precaution/
Contraindication):
อาการไม่พึงประสงค์จากการใช้
ยา (Adverse Drug
Reaction):
ขนาดและวิธีการบริหารยา
(Dosage and
Administration):
Concomitant use with nelfinavir or rilpivirine. Patients with known severe hypersensitivity to any
component of the formulation
Hypomagnesaemia, vitamin B12 deficiency, fundic gland Clostridium difficile-associated diarrhoea, gastrointestinal
polyps (long-term use); cutaneous lupus erythematosus, infections (e.g. Salmonella, Campylobacter), cutaneous
subacute cutaneous lupus erythematosus (SCLE), SLE; lupus erythematosus (CLE), subacute CLE, SLE, severe
osteoporosis-related fractures of the hip, wrist or spine (long-cutaneous adverse reactions (e.g. acute generalised
term use or high doses); Clostridium difficile-associated exanthematous pustulosis, drug reaction with eosinophilia
diarrhoea (CDAD), gastrointestinal infections (e.g. Salmonella, and systemic symptoms, Stevens-Johnson syndrome,
Campylobacter). toxic epidermal necrolysis); osteoporosis-related bone
fractures of the hip, spine, or wrist (long-term use or high
doses); fundic gland polyps (prolonged use), acute
tubulointerstitial nephritis, vitamin B12 deficiency (long-
term use).
Eradication of Helicobacter pylori associated with peptic Eradication of Helicobacter pylori associated with
ulcer disease: As triple therapy: 20 mg bid for 7 or 10 days in peptic ulcer disease: As triple therapy: 30 mg bid for 7-
combination with clarithromycin and with either amoxicillin or 14 days in combination with clarithromycin and with
metronidazole (or tinidazole). Alternatively, 40 mg once daily either amoxicillin or metronidazole. As dual therapy: 30
for 1 week in combination with amoxicillin and metronidazole mg tid for 14 days in combination with amoxicillin.
(or tinidazole). As dual therapy: 40 mg once daily for 14 days Acid-related dyspepsia: 15-30 mg once daily for 2-4
in combination with clarithromycin. weeks
Acid-related dyspepsia: 10 mg or 20 mg daily for 2-4 weeks. Gastro-oesophageal reflux disease: 15 mg or 30 mg
Gastro-oesophageal reflux disease: 10-20 mg once daily once daily for 4 weeks
Prophylaxis of NSAID-induced ulcers: 20 mg once daily. Benign gastric ulcer: 30 mg once daily for 4-8 weeks.
 Gastric ulcer: 20 mg once daily for 4-8 weeks, may increase to
40 mg once daily if needed. Maintenance therapy (prevention
of ulcer relapse): 20 mg once daily, may increase to 40 mg
once daily if needed.
NSAID-associated ulceration: 20 mg once daily for 4 weeks
Reflux oesophagitis: Treatment: 20 mg once daily for 4-8
weeks. Severe cases: 40 mg once daily for 8 weeks.
Maintenance therapy (after healing of oesophagitis): 10 mg
once daily, may be increased to 20-40 mg once daily if
needed.
Duodenal ulcer: 20 mg once daily for 2-4 weeks, may
increase to 40 mg once daily if needed. Maintenance therapy
(prevention of ulcer relapse): 10-20 mg once daily, may
increase to 40 mg once daily if needed.
Zollinger-Ellison syndrome:Initially, 60 mg daily, adjust
according to response. Usual dose: 20-120 mg daily. Daily
doses of >80 mg should be given in 2 divided doses.
เภสัชจลนศาสตร์
(Pharmacokinetics):
การดูดซึม(absorption): Rapid but variably absorbed from the gastrointestinal tract.
Bioavailability: Approx 30-40%. Time to peak plasma
concentration: 0.5-3.5 hours.
Onset: Antisecretory: Approx 1 hour.
Prophylaxis of NSAID-induced ulcers: 15-30 mg once
daily.
Erosive oesophagitis: For short-term treatment: 30 mg
once daily for up to 8 weeks. Maintenance therapy
following healing of cases (to reduce recurrence): 15 mg
once daily.
NSAID-associated ulceration: 30 mg once daily for 4-8
weeks.
Reflux oesophagitis: Treatment: 30 mg once daily for 4-8
weeks. Prophylaxis: 15 mg once daily, may be increased
up to 30 mg once daily if necessary.
Duodenal ulcer: 30 mg once daily for 2-4 weeks.
Alternatively, 15 mg once daily for 4 weeks. Maintenance
therapy (prevention of ulcer relapse): 15 mg once daily
Zollinger-Ellison syndrome: Initially, 60 mg once daily,
may be adjusted according to response. Doses of up to
90 mg bid have been used. Daily doses of >120 mg
should be given in 2 divided doses.
Rapidly absorbed from the gastrointestinal tract. Food
delays absorption and reduces bioavailability by approx
50-70%. Bioavailability: >80%. Time to peak plasma
concentration: Approx 1.5-2 hours.
 Duration: Up to 72 hours. Onset: Gastric acid suppression: 1-3 hours.
Duration: Gastric acid suppression: >24 hours.
การกระจายยา (Distribution): Enters breast milk. Plasma protein binding: Approx 95%. Volume of distribution: 15.7 ± 1.9 L. Plasma protein
binding: 97%.
การเปลี่ยนแปลงยา Metabolised in the liver primarily by CYP2C19 isoenzyme into Extensively metabolised in the liver primarily by CYP2C19
(Biotransformation or hydroxyomeprazole, and to a lesser extent by CYP3A4 into isoenzyme to inactive 5-hydroxyl-lansoprazole, and by
metabolism): omeprazole sulfone. CYP3A4 isoenzyme to inactive lansoprazole sulfone.
การกำจัดยาออกจากร่างกาย Mainly via urine (approx 77% as metabolites, small amount as Mainly via faeces (67%); urine (33%; 14-25% as
(Elimination): unchanged drug); faeces. Elimination half-life: 0.5-1 hour. metabolites, <1% as unchanged drug). Elimination half-
life: Approx 1-2 hours.
การเกิดอันตรกิริยาระหว่างยา – May decrease the plasma concentrations of nelfinavir, Does not have clinically significant interactions with other
(Drug interaction) rilpivirine, and atazanavir. drugs
– Increased risk of hypomagnesaemia with diuretics.
– May increase the plasma concentrations of saquinavir,
tacrolimus, methotrexate, citalopram. May significantly
decrease the absorption of itraconazole, ketoconazole,
posaconazole and erlotinib.
– May decrease metabolism of diazepam, phenytoin and
cilostazol.
– May reduce the antiplatelet effect of clopidogrel; avoid
concomitant use. May increase the bioavailability of
digoxin.
– Increased INR and prothrombin time with warfarin.
 – Concomitant use with CYP2C19 or CYP3A4 inhibitors (e.g.
clarithromycin, voriconazole) may increase the plasma
concentrations of omeprazole. Concomitant use with
CYP2C19 or CYP3A4 inducers (e.g. rifampicin) may decrease
the plasma concentrations of omeprazole.
Pregnancy Category : pregnancy category C pregnancy category B
ราคา 0.62 บาท/เม็ด 37.53 บาท/เม็ด