lansoprazole (Prevacid)
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Introduction
Tradename: Prevacid.
Indications
- short-term treatment of gastric & duodenal ulcers
- prevention of stress ulceration
- GERD, pyrosis
- erosive esophagitis
- Helicobacter pylori infection
- prevention of upper GI bleed due to hypersecretory conditions
Dosage
* IV given over 30 minutes; requires filter[5]
Tabs: 15 mg & 30 mg.
Suspension: (oral) 15 & 30 mg packets.[4];
Injection: IV form available in 30 mg vials[5]
Pharmacokinetics
- oral bioavailability is about 80%
- drug undergoes extensive 1st pass metabolism to primarily inactive metabolites
- metabolized by cyt P450 2C19 & 3A4
- elimination 1/2life < 2 hours
- duration of action > 24 hours, related to prolonged binding of the drug to the parietal cell
- when discontinued, secretory action returns in 3-5 days
elimination via liver
Adverse effects
Drug interactions
- drugs that require an acidic gastric pH for absorption
- sucralfate & H2 blockers
- no benefit to using in combination
- may inhibit protonation & activation of proton pump inhibitors
- any drug which inhibits cyt P450 2C19 or 3A4 can increase lansoprazole levels
- any drug which induces cyt P450 3A4 can diminish lansoprazole levels
- lansoprazole induces cyt P450 1A2
- may diminihs levels of drugs metabolized by cyt P450 1A2
- drug interaction(s) of levothyroxine with proton pump inhibitors
- drug interaction(s) of palbociclib with proton pump inhibitors
- drug interaction(s) of methotrexate with proton pump inhibitors
- drug interaction(s) of bisphosphonates with proton pump inhibitors
- drug interaction(s) of aspirin with proton pump inhibitors
- drug interaction(s) of antiplatelet agents with proton pump inhibitors
- drug interaction(s) of clopidogrel with proton pump inhibitors
- drug interaction(s) of ginko biloba with proton pump inhibitors
Mechanism of action
- suppression of gastric acid secretion by inhibiting H+/K+ ATPase (proton pump)
- proton pump inhibitors need protonation by parietal cells to be active
- inhibition of intrinsic factor secretion ???
- interacts with sulfhydryl groups proton pump
- inactive at neutral pH
More general terms
Additional terms
- cytochrome p450 1A2 (cytochrome P3-450, phenacetin deethylase, cytochrome p450-4, CYP1A2)
- cytochrome P450 2C19 (cytochrome P450 2C17, cytochrome P450 11A, mephenytoin 4-hydroxylase, cytochrome P450 254C, CYP2C19)
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 4.0 4.1 Prescriber's Letter 8(12):69 2001
- ↑ 5.0 5.1 5.2 Prescriber's Letter 11(8): 2004 New Drug: Prevacid I.V. (Lansoprazole) Injection Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=200806&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Deprecated Reference