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Lansoprazole

(British Approved Name, US Adopted Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

LansoprazoleSynonyms: A-65006; AG-1749; Lansopratsoli; Lansoprazol; Lansoprazolum
BAN: Lansoprazole
USAN: Lansoprazole
INN: Lansoprazole [rINN (en)]
INN: Lansoprazol [rINN (es)]
INN: Lansoprazole [rINN (fr)]
INN: Lansoprazolum [rINN (la)]
INN: Ланзопразол [rINN (ru)]
Chemical name: 2-({3-Methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl)methyl} sulphinylbenzimidazole
Molecular formula: C16H14F3N3O2S =369.4
CAS: 103577-45-3
ATC code: A02BC03
Read code: y01JU

Pharmacopoeias. In Europe and US.

European Pharmacopoeia, 6th ed. (Lansoprazole). A white or brownish powder. Practically insoluble in water soluble in anhydrous alcohol very slightly soluble in acetonitrile. It exhibits polymorphism. Store in airtight containers. Protect from light.

The United States Pharmacopeia 31, 2008(Lansoprazole). A white to brownish-white powder. Practically insoluble in water freely soluble in dimethylforma-mide. Store in airtight containers at a temperature not exceeding 40°. Protect from light.

Adverse Effects and Precautions

As for Omeprazole.

Effects on the blood

For a report of thrombocytopenia with lansoprazole, see under Omeprazole.

Effects on the endocrine system

For cases of gynaecomastia associated with lansoprazole.

Effects on the gastrointestinal tract

Glossitis (associated in some cases with black tongue or stomatitis) has been reported in a few patients taking lansoprazole as part of a triple therapy regimen for Helicobacter pylori elimination in peptic ulcer disease. Discoloured tongue has been reported in a patient taking lansoprazole alone.

An increase in gastritis occurred in patients infected with Helicobacter pylori when given long-term lansoprazole therapy. For further discussion of the link between Helicobacter pylori, gastritis, and proton pump inhibitor use, see Gastrointestinal Tumours.

For a suggestion that the incidence of diarrhoea may be greater with lansoprazole than omeprazole see Incidence of Adverse Effects. Cases of microscopic colitis have been reported with use of lansoprazole. UK licensed product information states that stopping therapy should be considered in the case of severe and/or persistent diarrhoea.

Effects on the musculoskeletal system

For reference to a case of eosinophilia and myalgia related to lansoprazole therapy.

Effects on the skin

For mention of skin reactions to lansoprazole.

Interactions

As for Omeprazole. Antacids and sucralfate may reduce the bioavailability of lansoprazole, and should not be taken within 1 hour of a dose of lansoprazole.

For reference to a lack of effect of lansoprazole on diazepam, see Gastrointestinal Drugs, and for a clinically insignificant effect on theophylline clearance. For reference to glossitis occurring when lansoprazole was used with some antibacterials, see Effects on the Gastrointestinal Tract, above.

Pharmacokinetics

Lansoprazole is rapidly absorbed after oral doses, with peak plasma concentrations achieved after about 1.5 to 2 hours. Bioavailability is reported to be 80% or more even with the first dose, although the drug must be given in an enteric-coated form since lansoprazole is unstable at acid pH. Food slows the absorption of lansoprazole and reduces the bioavailability by about 50%.

It is extensively metabolised in the liver, primarily by cytochrome P450 isoenzyme CYP2C19 to form 5-hydroxyl-lansoprazole and by CYP3A4 to form lansoprazole sulfone. Metabolites are excreted mainly in faeces via the bile only about 15 to 30% of a dose is excreted in urine. The plasma elimination half-life is around 1 to 2 hours but the duration of action is much longer. Lansoprazole is about 97% bound to plasma protein. Clearance is decreased in elderly patients, and in hepatic impairment.

Metabolism

As for omeprazole, the cytochrome P450 isoenzyme CYP2C19 (S-mephenytoin hydroxylase) is involved in the hydroxylation of lansoprazole, and individuals who are deficient in this enzyme are poor metabolisers of lansoprazole. There is some suggestion that the effect of this genetic polymorphism on lansoprazole may be less than the effect on omeprazole.

Uses and Administration

Lansoprazole is a proton pump inhibitor with actions and uses similar to those of omeprazole. It is used in the treatment of peptic ulcer disease and in other conditions where inhibition of gastric acid secretion may be beneficial.

Lansoprazole is usually given orally as capsules, dis-persible tablets, or suspension containing enteric-coated granules. Once daily regimens are taken before food in the morning. An intravenous formulation is also available.

For the relief of acid-related dyspepsia intermittent courses of lansoprazole may be given in doses of 15 or 30 mg once daily, for 2 to 4 weeks. In the treatment of gastro-oesophageal reflux disease the dose is 15 to 30 mg once daily for 4 to 8 weeks thereafter maintenance therapy can be continued with 15 or 30 mg once daily according to response. In patients unable to take oral therapy, lansoprazole may be given by intravenous infusion for the treatment of erosive oesophagitis for up to 7 days a dose of 30 mg over 30 minutes daily is recommended. Lansoprazole is given for the treatment of peptic ulcer disease in the UK in doses of 30 mg once daily. Treatment is continued for 2 to 4 weeks for duodenal and 4 to 8 weeks for gastric ulcer. In the USA, a dose of 15 mg daily for 4 weeks is recommended for duodenal ulcer, and 30 mg once daily is given for up to 8 weeks for gastric ulceration.

When appropriate, 15 mg daily may be used as maintenance therapy for the prevention of relapse of duodenal ulcer. Lansoprazole may be combined with antibacterials in one-week triple therapy regimens for the eradication of Helicobacter pylori. Effective regimens include lansoprazole 30 mg twice daily combined with clarithromycin 500 mg twice daily and amoxicillin 1 g twice daily, or combined with clarithromycin 250 mg twice daily and metronidazole 400 mg twice daily lansoprazole with amoxicillin and metronidazole has also been used. In patients with NSAID-associated ulceration a dose of 30 mg daily for 4 to 8 weeks is recommended 15 to 30 mg daily may be used as prophylaxis for patients who require continued NSAID treatment. In the treatment of pathological hypersecretory states such as the Zollinger-Ellison syndrome the initial dose is 60 mg once daily, adjusted as required. Doses of up to 90 mg twice daily have been used. Daily doses greater than 120 mg should be given in divided doses.

In the USA, children aged from 1 to 11 years may be given lansoprazole for the short-term treatment of erosive oesophagitis and symptomatic gastro-oesophageal reflux disease. Children weighing 30 kg or less should be given 15 mg once daily, and those weighing more than 30 kg are given 30 mg once daily, for up to 12 weeks. Doses of up to 30 mg twice daily have been used. In children aged from 12 to 17 years, lansoprazole 30 mg once daily for up to 8 weeks may be used for erosive oesophagitis, and 15 mg once daily for up to 8 weeks may be used for symptomatic gastro-oesophageal reflux disease. Although not licensed for children in the UK, the BNFC recommends comparable oral daily doses of 0.5 to 1 mg/kg in children up to 30 kg in weight, and 15 or 30 mg once daily in those over 30 kg.

Doses of lansoprazole may need to be reduced in patients with hepatic impairment (see below).

Administration

Lansoprazole capsules should be swallowed whole and not crushed or chewed. Lansoprazole dispersible tablets should be placed on the tongue and allowed to disintegrate and the resultant granules swallowed alternatively, the tablets may be swallowed whole with a glass of water. The tablets should not be crushed or chewed. The tablets may also be dispersed in a small amount of water and given via an oral syringe, or via a nasogastric tube.

Lansoprazole granulesfor oral suspension should be reconstituted in a little water and swallowed immediately. Where the suspension formulation is not available, the contents of the capsules (enteric-coated granules) can be sprinkled on a small amount of soft food (such as yogurt or apple sauce) or mixed with a little fruit juice and swallowed. For administration via a nasogastric tube, the contents of a capsule may be mixed with 40 mL of apple juice additional apple juice may be used to flush the tube.

Administration in hepatic impairment

Exposure to lansoprazole is increased in patients with hepatic impairment. Licensed product information recommends that patients with moderate to severe liver disease should be kept under supervision, and that the daily dose should be reduced by 50%.

Preparations

The United States Pharmacopeia 31, 2008: Lansoprazole Delayed-Release Capsules.

Proprietary Preparations

Argentina: Isatecf Lanzopral Mesactol Ogasto

Australia: Zoton

Austria: Agopton Lansobene

Belgium: Dakar

Brazil: Anzoprol Lanogastro Lanz Lanzol Lanzopept Neozol Ogastro Prazol

Canada: Prevacid

Chile: Fudermex Gastride Lanzopral Ogasto Unival

Czech Republic: Lansone Lansoprol Lanzul

Denmark: Lanzo

Finland: Lanzo Zolt

France: Lanzor Ogast Ogastoro

Germany: Agopton Lanzor

Greece: Elcodil Lanciprol Lanso Laprazol

Hong Kong: Takepron

Hungary: Lansacid Lansogen Lansone Lansoptol Levant Protonexa Refluxon

India: Chexid Lancus Lanzol

Indonesia: Compraz Digest Gastrolan Inhipraz Lancid Lapraz Laproton Lasgan Laz Loprezol Nufaprazol Prazotec Prolanz Prosogan Protica Pysolan Solans Sopralan Ulceran

Ireland: Lanziop Lanzol Razolager Zomel Zoton Zotrole

Israel: Lanton Zoton

Italy: Lansox Limpidex Zoton

Japan: Prevacid Takepron

Malaysia: Prevacid

Mexico: Bonzol llsatec Imidex Keval Lafin Lanodizol Mavilan Mediprim Ogastro Olan Palatrin Pranix Safemar Uldapril Ulpax

Norway: Lanzo

New Zealand: Solox Zoton

Philippines: Lanzohex Prevacid Fylison

Poland: LansoLek Lanzostad Lanzul

Portugal: Alexin Dispepci Gastrex Gastrolanzo Gastroliber Lansox Lanzogastro Lapol Lizul Monolitum Ogasto Pampe Pepzol Ulcertec

Russia: Acrilans Epicur Helicol Lanzap

South Africa: Adco-Roznal Lancap Lansoloc Lanzor

Singapore: Prevacid

Spain: Bamalite Estomil Eudiges Lanzol Monolitum Opiren Pro Ulco Protoner

Sweden: Lanzo

Switzerland: Agopton

Thailand: Prevacid

Turkey: Aprazol Degastrol Helicol Lansazol Lansoprol Lansor Lanzedin Ogastro Opagis Vogast Zoprol

UAE: Lanfast

United Kingdom: Zoton

USA: Prevacid

Venezuela: Biolanz Gastrazol Lansovax Lanzapf Lanzol Lanzopral Ogastro

Multi-ingredient

Argentina: Helikar

Brazil: Anzopac H-Bacter Helicopac Helikar Lansodom Lansoprid Fylorikit Pyloripac Fyloritrat

Canada: Hp-Pac

Finland: Helipak A Helipak K Helipak T

India: Okalan D Pylokit

Mexico: Pylopac

Turkey: Helipak

UK- Heliclear HeliMet

USA: Prevpac

Used as on adjunct in:

USA: Prevacid NapraPAC

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