Lafutidine, Second generation histamine H2 receptor antagonist
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Lafutidine is an H2 receptor antagonist effective against gastric and duodenal ulcers, launched in April 2000, available in 5 mg and 10 mg doses. It possesses gastroprotective properties by stimulating mucosal blood flow and increasing mucin biosynthesis, with a unique receptor-binding affinity stronger than other H2 antagonists. Adverse effects may include increased liver enzymes, hallucinations, and difficulty breathing, and it is primarily targeted at gastroenterologists for treating various gastric conditions.
Lafutidine, Second generation histamine H2 receptor antagonist
- 1. LAFUTIDINE 20 mg ATC - A02BA08 H2 receptor antagonist
- 2. Schedule 'H' drug warning : To be sold by retail on the prescription of a Registered Medical Practitioner only
- 3. Introduction The concept of H2 receptor antagonist BURIMAMIDE (Not In Clinical Use) Was Provided By :- Professor Sir James Black: Nobel laureate who designed the first modern drugs for high blood pressure (Propranolol) and peptic ulcers
- 4. ATC code Name A02BA01 CIMETIDINE A02BA02 RANITIDINE A02BA03 FAMOTIDINE A02BA04 NIZATIDINE A02BA05 NIPEROTIDINE A02BA06 ROXATIDINE A02BA07 RANITIDINE BISMUTH CITRATE A02BA08 LAFUTIDINE A02BA51 CIMETIDINE, COMBINATIONS A02BA53 FAMOTIDINE, COMBINATIONS H2 receptor antagonist
- 5. Launched in April 2000 in 5mg and 10mg dose Effective against gastric and duodenal ulcers. Brand PROTECADIN® Table By Taiho Pharmaceutical Co., Ltd. JAPAN LAFUTIDINE
- 6. Histamine H2 receptor antagonist
- 7. Lafutidine is a H2 (Histamine) receptor antagonist. Histamine is the most potent stimulus of acid secretion and acts as the common mediator. Pharmacology
- 12. Gastroprotective effect of lafutidine is independent of its acid antisecretory activity . Activates capsaicin-sensitive afferent neurons and stimulates the release of calcitonin gene-related peptide (CGRP), which inhibits acid secretion and stimulates mucosal blood flow . Increase in mucin biosynthesis via stimulation of nitric oxide production . Increasing the thickness of the surface mucus gel layer Maintaining gastric mucosal blood flow and bicarbonate response Gastroenterology Research and Practice Volume 2011 (2011), Article ID 640685, 8 pages http://dx.doi.org/10.1155/2011/640685
- 13. Mechanisms underlying stimulation of gastric HCO3- secretion induced by capsaicin and acid. Capsaicin stimulated HCO3- secretion in the stomach, essentially through capsaicin-sensitive afferent neurons via the activation of TRPV1, and this action was mediated with endogenous PGE2/EP1 receptors and NO. Mucosal acidification also increased HCO3- secretion through the activation of sensory neurons as well as endogenous PGs and NO; however, this action did not result from an interaction between H+ and the capsazepine-sensitive site of TRPV1, and depended on the PGI2/IP receptor. http://www.intechopen.com/books/capsaicin-sensitive-neural-afferentation-and-the-gastrointestinal-tract-from-bench-to- bedside/mechanism-of-capsaicin-stimulated-gastric-hco3-secretion-comparison-with-mucosal-acidification
- 14. Mechanisms of gastric cytoprotection induced by capsaicin and acid. Capsaicin affords gastric cytoprotection, essentially mediated by capsaicin- sensitive afferent neurons and dependent on endogenous PGs and NO, and this effect is attenuated by indomethacin, L- NAME, in addition to the TRPV1 antagonist capsazepine. The protective action of capsaicin is facilitated by endogenous PGs, mainly through PGI2/IP receptors, despite that capsaicin increased PGI2 but not PGE2 production in the stomach. Likewise, luminal acid by acting as a mild irritant shows gastroprotective action through activation of sensory neurons as well as endogenous PGs and NO, and the PG effect is mediated by PGE2/EP1 receptor. However, the activation of sensory neurons by acid does not result from the interaction with the capsazepine- sensitive site of TRPV1 and probably mediated by ASIC3. http://www.jpp.krakow.pl/journal/archive/02_14/articles/01_article.html
- 15. Constituent of gastric mucus http://cdn.intechopen.com/pdfs-wm/19866.pdf
- 16. Distribution of cells constituting the oxyntic gland. http://cdn.intechopen.com/pdfs-wm/19866.pdf
- 18. Gastric protection: which is stronger, aggressive factor or protective factor http://cdn.intechopen.com/pdfs-wm/19866.pdf
- 19. Structures and pharmacological activities of lafutidine and its analogs. Mucin biosynthetic activity was evaluated in an organ culture system of the rat stomach
- 20. Surface mucus gel layer of the human gastric mucosa from (A, B) lafutidine positive and (C, D) lafutidine negative groups stained with (A, C) HE and (B, D) GOTS-PCS. http://cdn.intechopen.com/pdfs-wm/19866.pdf
- 22. After oral administration, Lafutidine is rapidly absorbed in the GIT. The plasma protein binding capability of Lafutidine is 88%. The drug is predominantly metabolized via CYP2D6 and CYP3A4 enzymes. Lafutidine is mostly excreted in urine as drug metabolites and as unchanged drug, to some extent. peak plasma concentration of 265.15±49.84 ng/ml is achieved at 0.95±0.24 hours Half Life 1.92 ± 0.94 hours . Pharmacokinets of Lafutidine
- 23. Indication Gastric ulcers Duodenal ulcers Gastric mucosal lesions (erosion, hemorrhage, redness or edema) associated with acute gastritis Acute exacerbation of chronic gastritis.
- 24. DOSAGE & ADMINISTRATION For Gastric and duodenal ulcers (Adults): Consider administration of 10 mg of Lafutidine, twice daily, preferably after breakfast and at bedtime. For duodenal ulcers (Adults): Consider administration of 10 mg of Lafutidine, twice daily, preferably after breakfast and at bedtime. For Gastric mucosal lesions (Adults): Consider administration of 10 mg of Lafutidine, twice daily, preferably after breakfast and at bedtime. As Pre-anaesthetic medication (Adults): Consider administration of 10 mg of Lafutidine during night time before surgery, and 10 mg of Lafutidine, two hours prior to induction of anesthesia during surgery.
- 25. ADR SPECIAL PRECAUTION Adverse effects Protecadin OD may cause unwanted side effects such as: Increase in liver enzymes Hallucinations Constipation Sore throat Jaundice Loss of appetite Difficulty breathing or swallowing
- 26. STP
- 28. Targeting Gastric ulcers Gastro Esophageal Reflux Disease (GERD) Acute Duodenal Ulcer Gastric mucosal lesions Acute exacerbation of chronic gastritis
- 29. STUDY REFERENCES lafutidine increases plasma concentrations of CGRP and somatostatin in humans, which may result in inhibition of postprandial acid secretion and gastroprotective activity. http://www.ncbi.nlm.nih.gov/pubmed/16416222 lafutidine as an empiric treatment and superior efficacy for primary care practice patients with dyspepsia http://www.hindawi.com/journals/grp/2011/640685/ It has been shown to have mucosal protective action in the gastrointestinal tract, including the esophagus, stomach, small intestine, and large intestine http://www.wjgnet.com/2150-5349/full/v1/i5/112.htm
- 30. UNIQUE Has a receptor-binding affinity which is 2-80 times higher than other representative H2-receptor antagonists (e.g. famotidine, ranitidine, and cimetidine). Increase the gastric mucosal blood flow, gastric mucus secretion and to accelerate epithelial restitution. The gastroprotective effects and intestinal protective effects Lafutidine has been shown to significantly increase plasma somatostatin levels 0.3-2 h after a dose has been taken. Somatostatin inhibits gastric acid secretion http://www.wjgnet.com/2150-5349/full/v1/i5/112.htm
- 31. Market Size and Growth Rate Gastro & Hepato Market Size = 9938 Cr.* Growth Rate =14.2 %* Major Share as H2 Receptor Blocker :- Ranitidine (* MAT March 2015 Express Pharma)
- 32. RANITIDINE INJECTABLES = 43.666Crs.(MAT ~ 06/2014) RANITIDINE ORAL SOLIDS = 419.172 Crs.(MAT ~ 06/2014)
- 33. BRAND RANK Val. In Cr. ACILOC CI6 1 16.85 RANTAC UNQ 2 9.32 R-LOC ZYC 3 6.26 RANITIN TNT 4 5.37 HISTAC RBY 5 3.81 ZINETAC GSK 6 0.94 RANITIDINE MA& 7 0.25 RANLOC IN9 8 0.20 RANIPEP WOK 9 0.13 MONORIN AMB 10 0.09 (MAT ~ 06/2014) RANITIDINE INJECTABLES
- 34. RANIT IDINE ORAL SOLIDS 419.17 ACILOC CI6 1 129.40 RANTAC UNQ 2 78.96 HISTAC RBY 3 31.81 R-LOC ZYC 4 15.02 HISTAC EVT RBY 5 7.74 RANITIN TNT 6 4.64 MONORIN AMB 7 1.64 ZYNOL MRB 8 0.34 NICOTAC A1H 9 0.29 RANLOC IN9 10 0.09 BRAND RANK Val. In Cr. (MAT ~ 06/2014)
- 35. BRAND PLAN Plan as per Organizational Vision
- 36. Competitor
- 37. Competitor Brand Name Composition Company Packing LAFTID tab Lafutidine 5 mg ABBOTT 10 29.25 LAFUDAC tab Lafutidine 5 mg UNISEARCH 10 35 LAFUTAX tab Lafutidine 5 mg AJANTA PHARMA 10 40 LAFTID tab Lafutidine 10 mg ABBOTT 10 49.35 LAFUMAC Lafutidine 10 mg MACLEODS 10 50 LAFUKEM Lafutidine 10 mg ALKEM 10 53.08 LAFUDAC tab Lafutidine 10 mg UNISEARCH 10 65 LAFUTAX tab Lafutidine 10 mg AJANTA PHARMA 10 70 LAFAXID-10 tab Lafutidine 10 mg ZUVENTUS 10 77.45 LACILOC Lafutidine 10 mg CADILA 10 83.35 MRP Rs.
- 38. Brand Name Composition Company Packing LAFUMAC- DSR MACLEODS 10 79.9 LAFAXID-D ZUVENTUS 10 80 LAFUMAC- PLUS MACLEODS 10 95 LACILOC- D CAP. CADILA 10 101.5 LAFUDAC-D tab UNISEARCH 10 80 MRP Rs. Lafutidine 10 mg +Domperidone10mg (IR) + 20mg (SR) Lafutidine 10 mg +Domperidone30mg Lafutidine 10 mg + Rabiprazole20mg Lafutidine 10 mg +Domperidone30mg Lafutidine 5 mg, domperidone 10mg Combination
- 39. Marketing Strategy Communication strategy Distribution Strategy Pricing Strategy
- 41. Sales Force Management SFA/ SFE Efficiency Effectiveness Excellence