DOCSLIB.ORG

Effects of Antacids and Food on Absorption of Famotidine

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Effects of Antacids and Food on Absorption of Famotidine Br. J. clin. Pharmac. (1987), 24, 551-553 Effects of antacids and food on absorption of famotidine J. H. LIN, A. N. CHREMOS, S. M. KANOVSKY, S. SCHWARTZ, K. C. YEH & J. KANN Merck Sharp and Dohme Research Laboratories, West Point, PA 19486 and Biodecision Laboratories, Inc. Pittsburgh, PA 15213, USA The effect of a high potency antacid and food on the bioavailability of famotidine was studied in 17 healthy volunteers in an open randomized three-way cross-over trial. After an overnight fast, famotidine was administered to each subject as follows: 40 mg famotidine orally alone; 40 mg orally with antacid; and 40 mg orally with a standard breakfast. Co- administration of the antacid caused a small but significant reduction in the maximum plasma concentration (Cmax) of famotidine from 81.1 ± 54.2 to 60.8 ± 21.6 ng ml-' (P < 0.05) and a small decrease in the area under plasma concentration-time curve [AUC] from 443.3 ± 249.2 to 355.0 ± 125.1 ng ml-1 h (P > 0.05). However, there was only a minimal effect of food on these parameters; the Cmax and [AUC] were 81.6 ± 29.6 ng ml-' and 434.8 ± 145.9 ng ml-' h, respectively. Keywords famotidine antacids food absorption Introduction Famotidine (3-(((2-((aminoiminomethyl)amino)- The purpose of the present study was to in- 4-thiazolyl)methyl)-thio)-N(aminosulphonyl)- vestigate the effects of a high potency antacid propanimidamide) is a new histamine H2- and food on the bioavailability and disposition of receptor antagonist. It has been reported to be famotidine. more potent than ranitidine and cimetidine in inhibiting gastric acid secretion (Pendleton et al., 1983). Renal excretion plays a substantial Methods role in the elimination of famotidine from the body. Earlier studies from our laboratory have Seventeen volunteers of either sex were each shown that the renal clearance of famotidine in studied on three occasions at least 1 week apart. man and rats was about three times the glomerular All subjects were in good health as judged by filtration rate, suggesting that famotidine might appropriate laboratory tests and clinical examin- be secreted by an active secretary mechanism ation. (Lin et al., 1987). After an overnight fast, they received the In the treatment of peptic ulcer disease ant- treatment of famotidine on three different acids are sometimes prescribed or self-admin- occasions separated by at least 1 week, famoti- istered concurrently with histamine H2-receptor dine alone (Treatment A), famotidine plus antagonists. Gugler et al. (1981) reported that Mylanta II (Treatment B) and famotidine plus a cimetidine absorption was reduced by co-admin- standard breakfast (Treatment C). The assign- istration with antacids. The absorption of raniti- ment of treatment sequences was randomized. dine has also been reported to be diminished by Famotidine was given in one 40 mg tablet. The antacids (Mihaly et al.,.1982). It was therefore of selected antacid (10 ml Mylanta II) is of high importance to investigate the effect of antacids potency and composed of 800 mg each aluminum on the bioavailability of famotidine. and magnesium hydroxide plus 60 mg simethicone Correspondence: Dr Jiunn H. Lin, Drug Metabolism, WP42-2, Merck Sharp and Dohme Research Laboratories West Point, PA 19486, USA 551 552 J. H. Lin et al. with an antacid neutralizing capacity of50.8 meq (1973) wherein the variability in renal excretion acid/10 ml of the liquid preparation. The stan- is considered. dard breakfast consisted of 4 ounces of orange Statistical analysis was performed by Fisher's juice, one bowl of Special Kg cereal, 130 ml low least significant difference test based on an fat milk and one fruit danish with one pat of analysis of variance which blocked only on sub- margarine. When famotidine was administered ject before testing treatment effects (Snedecor concurrently with Mylanta II, the antacid was & Cochran, 1974). P < 0.05 was considered to taken first and immediately followed by famoti- be significant. dine with 150 ml of water. In the study of food effect, the breakfast was eaten first and im- Results mediately followed by famotidine with 150 ml of water. When famotidine was administered alone, Co-administration with antacids caused a small it was also taken with 150 ml of water. but significant reduction in the maximum plasma Heparinized blood was collected at 0, 0.5, 1, concentration (Cm.1) for famotidine and a small 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24 and 48 h after decrease in the area under plasma concentration- drug administration. Urine was collected as per time curve (AUC) (Table 1). The time to reach the following schedule: -1 to 0 (pre-drug); 0-2, the peak concentration (tm.a) was somewhat 2-4, 4-6, 6-8, 8-12, 12-24, 24-36, and 36-48 h shorter in the presence of antacids. There was no post treatment. Plasma was immediately separ- significant effect of food on these parameters, as ated by centrifugation. Volunteers were in- shown by the similar values obtained for these structed to empty their bladder at the end of parameters after food compared with the fasting each collection period. The plasma and urine state (Table 1). The total amount excreted as stored at -20° C until assay. The concentrations unchanged famotidine was slightly reduced in of famotidine in plasma and urine were deter- the antacids study, whereas the urinary recovery mined by h.p.l.c. (Vincek et al., 1985). of unchanged drug tended to be higher with The renal clearance of famotidine was calcu- breakfast (Table 1). lated as the amount of unchanged famotidine The values for the renal clearance are practi- excreted in the urine over the period of time cally identical following all three treatments, (0-12 h) divided by area under plasma concen- suggesting that neither the antacid nor the food tration-time curve (AUC) over the same time has an effect on the renal excretion of famotidine. period. The ratio of bioavailability (relative bio- The mean bioavailability ratios of famotidine availability) of famotidine with co-administration with antacid, and with food to that of famotidine of antacids or food to that of famotidine alone alone were 0.90 and 1.14, respectively, suggest- was calculated by the method of Kwan & Till ing that antacids sli,ghtly reduced the extent of Table 1 Area under plasma concentration-time curve (AUC), renal clearance, and maximum plasma concentrations (Cm.in) of famotidine and the time (tQmU) at which they were observed following treatment A, B, and C in healthy volunteers (n= 17) TreatmentA Treatment B" Treatment CC Cma, 81.1 60.8d 81.6 (ng ml-1) ±54.2 +21.6 ±29.6 tmax 2.62 2.24 2.44 (h) ±1.13 ±0.79 ±0.63 AUC (0-cc) 443.3 355.0 434.8 (ng ml-' h) ±249.2 +125.1 ±145.9 Renal clearance 25.8 27.9 28.5 (1h-1) ±10.5 ±125.1 ±145.9 Urinary recovery of 9.87 8.79 11.1 unchanged drug ±4.29 ±2.82 ±3.0 (mg) a Treatment A = famotidine 40 mg tablet. b Treatment B = famotidine 40 mg tablet and Mylanta II. c Treatment C = famotidine 40 mg tablet and standard breakfast. d Significantly different from Treatment A, P < 0.05. Short report 553 absorption offamotidine, while food had slightly the percentage of administered basic drugs that enhanced absorption. are dissolved when they pass into the small in- testine and hence increase their absorption. This may explain why there is a small increase in the Discussion absorption of famotidine when the drug was given with a standard breakfast. Antacids have been shown to decrease the bio- The unchanged values for renal clearance of availability of cimetidine (Gugler et al., 1981) famotidine after the three different treatments and ranitidine (Mihaly etal., 1982) to about 35% indicated that the renal excretion of famotidine in healthy volunteers. A similar effect, but to a was not affected by antacids or food. These smaller degree, was observed when an antacid results suggested that the observed reductions in was co-administered with famotidine. This was Cm. and AUC of famotidine after co-admin- shown by the reduced AUC and the comparable istration of antacids are due to the interaction reduction in the urinary recovery of unchanged between famotidine and antacids in the gastro- famotidine (Table 1). intestinal lumen, rather than the alterations in By raising the pH in the gastrointestinal tract, the elimination processes. antacids may decrease the solubility of bases, In conclusion, co-administration of the ant- such as famotidine, ranitidine and cimetidine. acids caused a small but significant decrease in Antacids may also absorb or chelate drug the Cm.x, and a small decrease in the AUC and molecules to form insoluble complexes and may the extent of absorption offamotidine, while the also indirectly affect the gastric emptying time. standard breakfast had an opposite effect. These Nevertheless, the exact mechanism ofthe reduc- effects are considered minor. Since famotidine is tion in the absorption of famotidine observed in a potent H2-receptor antagonist, the 10-15% this study is unclear. change in bioavailability is unlikely to be clinically Ingested food tends to delay stomach-emptying. relevant. Prolonged retention in the stomach may increase References Gugler, R., Brand, M. & Somogyi, A. (1981). Impaired on MK-208 (YM-11170), a new slowly dissoluable cimetidine absorption due to antacids and meto- H2-receptor antagonist. Arch. int. Pharmacodyn. clopramide. Eur. J. clin. Pharmac., 20, 225-228. Ther., 266, 4-16. Kwan, K. C. & Till, A. E. (1973). Novel method for Snedecor, M. & Cochran, G. (1974).
Load more

Recommended publications
  • Medicines That Affect Fluid Balance in the Body
    the bulk of stools by getting them to retain liquid, which encourages the Medicines that affect fluid bowels to push them out. balance in the body Osmotic laxatives e.g. Lactulose, Macrogol - these soften stools by increasing the amount of water released into the bowels, making them easier to pass. Older people are at higher risk of dehydration due to body changes in the ageing process. The risk of dehydration can be increased further when Stimulant laxatives e.g. Senna, Bisacodyl - these stimulate the bowels elderly patients are prescribed medicines for chronic conditions due to old speeding up bowel movements and so less water is absorbed from the age. stool as it passes through the bowels. Some medicines can affect fluid balance in the body and this may result in more water being lost through the kidneys as urine. Stool softener laxatives e.g. Docusate - These can cause more water to The medicines that can increase risk of dehydration are be reabsorbed from the bowel, making the stools softer. listed below. ANTACIDS Antacids are also known to cause dehydration because of the moisture DIURETICS they require when being absorbed by your body. Drinking plenty of water Diuretics are sometimes called 'water tablets' because they can cause you can reduce the dry mouth, stomach cramps and dry skin that is sometimes to pass more urine than usual. They work on the kidneys by increasing the associated with antacids. amount of salt and water that comes out through the urine. Diuretics are often prescribed for heart failure patients and sometimes for patients with The major side effect of antacids containing magnesium is diarrhoea and high blood pressure.
    [Show full text]
  • Mast Cell Tumor (Canine)
    MAST CELL TUMOR (CANINE) What is a mast cell tumor? A mast cell tumor is a cancer of a specific type of inflammatory cell, usually in the skin. Mast cell tumors may originate from other areas such as the gastrointestinal tract, spleen, liver, or mouth, but they are far more com- monly found on the skin. What are the symptoms of a mast cell tumor? Mast cell tumors on the skin can be red, hairless, and itchy. They can also feel soft or firm, and look like many other types of masses. Because they release histamine, they can grow and shrink periodically. How do you diagnose a mast cell tumor? A fine needle aspirate of the mass is performed and evaluated under a microscope for cytology. Cytology de- termines the type of tumor, however further diagnostics such as a biopsy (histopathology) are needed to further categorize or grade a mast cell tumor. What is the behavior of this type of tumor? Mast cell tumors are graded 1, 2, or 3 based on microscopic analysis of a biopsy specimen. Grade 1 tumors typically behave like benign tumors and have a low potential to spread (metastasize). Grade 3 tumors are aggressive and have a high potential to metastasize to the lymph nodes and possibly the liver, spleen, or bone marrow. Grade 2 tumors may behave either like a Grade 1 or 3 tumor. A newer grading system will determine whether a mast cell tumor is low grade or high grade. Many pathologists will use both systems to help provide as much information as possible.
    [Show full text]
  • 1.1 Antacids and Other Drugs for Dyspepsia 1.1.1 Aluminium
    1. Drugs acting on the Gastrointestinal System 1.1 Antacids and other drugs for dyspepsia 1.1.1 Aluminium- and magnesium- containing Aluminium hydroxide antacids Co-magaldrox (Mucogel®) Magnesium trisilicate 1.1.2 Antacid preparations containing simeticone Asilone® (for use in accordance with the Palliative Care Pain and Symptom Control Guidelines) 1.1.3 Other drugs for dyspepsia and gastro- Algicon® (second-line alginate) oesophageal disease Gaviscon Advance® liquid (first-line alginate) Gaviscon Infant® (Neonatal Unit only) 1.2 Antispasmodics and other drugs altering gut motility Alverine (Gastroenterology only) Dicycloverine Domperidone Hyoscine-n-butyl bromide Mebeverine Metoclopramide Peppermint oil 1.3 Ulcer-healing drugs 1.3.1 H2-receptor antagonists Cimetidine Ranitidine 1.3.3 Chelates and complexes Sucralfate 1.3.5 Proton pump inhibitors - Omeprazole capsules (first line PPI - Losec MUPS are non-formulary) see Salford PPI Strategy and Guidelines Lansoprazole orodispersible tablet (FasTab®) (for patients unable to swallow tablets) Rabeprazole (Gastroenterologists and Gastroenterology Surgeons only) 1.4 Acute diarrhoea 1.4.1 Adsorbents & bulk-forming Kaolin mixture 1.4.2 Antimotility drugs Codeine phosphate Loperamide 1.5 Chronic bowel disorders Colifoam® (hydrocortisone) Infliximab (in accordance with NICE guidance) - Follow restricted high cost drug procedure when prescribing infliximab Mesalazine Predenema® Predfoam® Predsol® Sulfasalazine Clipper® (Beclometasone dipropionate) (consultant gastroenterologist only) Budesonide Rectal
    [Show full text]
  • Acid-Reducing Medications: Interactions with Harvoni and Epclusa
    November 2016 | www.hepatitis.va.gov Acid-Reducing Medications: Interactions with Harvoni® and Epclusa® Sofosbuvir/Velpatasvir = Epclusa® Ledipasvir/Sofosbuvir = Harvoni® • Acid-reducing medications can decrease the effectiveness of Harvoni® and Epclusa® and could prevent successful cure. • Let your provider know if you are taking any acid-reducing medications—either prescribed to you or purchased over the counter. Types of Acid-Reducing What to Do if What to Do if Medications Taking Epclusa® Taking Harvoni® Antacids Separate taking the antacid and Separate taking the antacid and Epclusa® by 4 hours Harvoni® by 4 hours Combinations of aluminum, magnesium, and calcium. Brand names include: Alka-Seltzer® Maalox® Mylanta® Rolaids® TUMS® H2 Blockers Do not take more than the Do not take more than the recommended doses recommended doses Cimetidine (Tagamet®) Famotidine (Pepcid®) May take together with Epclusa® May take together with Harvoni® Nizatidine (Axid®) or 12 hours apart or 12 hours apart Ranitidine (Zantac®) Proton Pump Inhibitors (PPI) It is best to avoid PPIs during treat- It is best to avoid PPIs during ment with Epclusa®. If there are no treatment with Harvoni®. If there Esomeprazole (Nexium®) alternatives, follow these instructions: are no alternatives, follow these Lansoprazole (Prevacid®) instructions: Omeprazole (Prilosec®) Take Epclusa® with food Pantoprazole (Protonix®) Take the proton pump inhibitor 4 Take Harvoni® and the proton Rabeprazole (Aciphex®) hours after taking Epclusa® pump inhibitor at the same time in the morning after fasting overnight Do not take the proton pump (on an empty stomach) inhibitor at the same time as Epclusa® Do not take proton pump Do not take proton pump inhibitors inhibitors at more than the at more than the recommended dose recommended dose U.S.
    [Show full text]
  • Risks of Proton Pump Inhibitors for Gastroesophageal Reflux Disease and a Diet Alternative
    Journal of Nutritional Health & Food Engineering Literature Review Open Access Risks of proton pump inhibitors for gastroesophageal reflux disease and a diet alternative Abstract Volume 10 Issue 1 - 2020 Gastroesophageal reflux disease (GERD) is one of the most common digestive conditions Mark Stengler NMD treated by gastroenterologists. The most commonly prescribed drugs for GERD are proton Stengler Center for Integrative Medicine, USA pump inhibitors (PPIs) that reduce stomach acid. While these medications are effective for relieving GERD symptoms, their long-term use is associated with several side effects Correspondence: Mark Stengler NMD, Stengler Center for and chronic diseases. Several publications have questioned the long-term safety of PPIs. Integrative Medicine, 324 Encinitas Blvd. Moreover, recent studies have demonstrated that the Mediterranean Diet may be more Encinitas, CA 92024 1-760-274-2377, effective than PPIs for people suffering from GERD. Email Keywords: GERD, mediterranean diet, proton pump inhibitors, PPI, acid reflux, LES, Received: April 14, 2020 | Published: April 28, 2020 lower esophageal sphincter, omeprazole, prilosec Introduction Proton pump inhibitors to treat GERD Gastroesophageal reflux disease (GERD) is one of the most common The most commonly prescribed drugs for GERD are proton digestive conditions treated by gastroenterologists and primary care pump inhibitors (PPIs).2 PPIs currently available on prescription in doctors. Typical symptoms include heartburn, regurgitation, and the USA are: dexlansoprazole
    [Show full text]
  • Treating Heartburn and GERD
    ® Treating heartburn and GERD eartburn is a feeling of burning pain in the pit of your stomach or your lower chest. It comes from acid backing up from your stomach into your throat. You Hmay have seen ads for heartburn drugs, such as Nexium, Prilosec, or Prevacid. These drugs are called PPIs (proton pump inhibitors). They keep the stomach from making too much acid. They have been shown to heal irritation of the tube between the throat and the stomach (the esophagus). In most cases, you don’t need a PPI for heartburn. You can get relief from a less powerful drug. And when you do need a PPI, you should take the lowest dose for as short a time as possible. Here’s why: You may not need a PPI. PPIs have risks. More than half of the people who take PPIs If you need a PPI, taking a low dose for less probably do not need them. Simple heartburn than a year is probably safe. PPIs are expensive can be treated with antacids or other drugs, plus and have been linked to higher risk of some diet and lifestyle changes. problems. Talk with your doctor before taking You may only have heartburn every now and them for longer than two weeks. Be sure you then—such as after a big, spicy meal. This may have a good reason to take the PPI, and take it be uncomfortable, but it is not serious. You can for the shortest time possible. usually get relief from an antacid, like Rolaids or Tums, or an H2 blocker, such as Pepcid AC or Zantac.
    [Show full text]
  • Anaesthetic Antacids: a Review of Its Pharmacological Properties and Therapeutic Efficacy
    International Journal of Research in Medical Sciences Parakh RK et al. Int J Res Med Sci. 2018 Feb;6(2):383-393 www.msjonline.org pISSN 2320-6071 | eISSN 2320-6012 DOI: http://dx.doi.org/10.18203/2320-6012.ijrms20180005 Review Article Anaesthetic antacids: a review of its pharmacological properties and therapeutic efficacy Rajendra Kumar Parakh*, Neelakanth S. Patil Department of Medicine, SDM College of Medical Sciences and Hospital, Sattur, Dharwad, Karnataka, India Received: 13 December 2017 Accepted: 27 December 2017 *Correspondence: Dr. Rajendra Kumar Parakh, E-mail: [email protected] Copyright: © the author(s), publisher and licensee Medip Academy. This is an open-access article distributed under the terms of the Creative Commons Attribution Non-Commercial License, which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. ABSTRACT Anaesthetic antacids, combination of antacids (Aluminium hydroxide, Magnesium hydroxide) with an anaesthetic (oxethazaine), is becoming a choice of physicians and is re-emerging across all types of GI disorders (esophagitis, peptic ulcer, duodenal ulcer, heartburn, gastritis, functional dyspepsia), despite the discovery of potent and efficacious acid suppressants like H2 receptor blockers and proton pump inhibitors (PPIs). The reason being that anaesthetic antacids increase the gastric pH and provide relief from pain for a longer period of duration at considerably a lower dosage. Furthermore, it significantly increases the duration between the time of medication and the peak pH as compared to antacid alone. Oxethazaine, an anaesthetic component, produces a reversible loss of sensation and provides a prompt and prolonged relief of pain, thereby broadening the therapeutic spectrum of antacids.
    [Show full text]
  • Antacid Drug Use and Risk of Esophageal and Gastric Adenocarcinomas in Los Angeles County
    526 Antacid Drug Use and Risk of Esophageal and Gastric Adenocarcinomas in Los Angeles County Lei Duan,1 Anna H. Wu,2 Jane Sullivan-Halley,1 and Leslie Bernstein1,2 1City of Hope National Medical Center, Duarte, California and 2Department of Preventive Medicine, Keck School of Medicine, University of Southern California/Norris Comprehensive Cancer Center, Los Angeles, California Abstract Objectives: Concern has been expressed that antacid among persons with no UGI disorder than among drugs increase the risk of esophageal and gastric those with an UGI disorder (homogeneity of trends adenocarcinomas. P = 0.07). Regular use of nonprescription acid Methods: This population-based case-control study neutralizing agents was not associated with risk of recruited patients with incident esophageal adeno- adenocarcinomas of the gastric cardia or distal carcinoma (n = 220), gastric cardiac adenocarcinoma stomach. Regular use of prescription acid suppressive (n = 277), or distal gastric adenocarcinoma (n = 441) drugs was not associated with risk for any of these diagnosed between 1992 and 1997, and 1,356 control cancers. participants in Los Angeles County. Unconditional Conclusion: We found risk of esophageal adenocarci- polychotomous multivariable logistic regression anal- noma was greater among long-term nonprescription yses were done to evaluate the association between acid neutralizing drugs in participants without physi- antacid drug use and these cancers. cian-diagnosed UGI conditions than among those with Results: Among participants who took nonprescription these conditions; this may represent self medication for acid neutralizing agents for >3 years, the odds ratio for undiagnosed precursor conditions or it may be that esophageal adenocarcinoma was 6.32 compared with nonprescription acid neutralizing drugs, taken without P never users (95% confidence interval, 3.14-12.69; trend limitation on amount used when symptoms are most < 0.01).
    [Show full text]
  • Magnesium/Aluminum Antacids
    Magnesium/Aluminum Antacids (mag-nee-zee-um / ah-loo-mih-num) Category: Oral Antacid; Laxative (Anti-Constipation) Other Names for this Medication: Maalox®, Mylanta® Common Dosage Forms: Veterinary: None. Human: aluminum hydroxide 200 mg and magnesium hydroxide 200 mg per 5 mL oral suspension; various forms of tablets, chewable tablets, and aerosol foam suspensions. This information sheet does not contain all available information for this medication. It is to help answer commonly asked questions and help you give the medication safely and eff ectively to your animal. If you have other questions or need more information about this medication, contact your veterinarian or pharmacist. This drug SHOULD NOT be used in patients: Key Information XXThat are allergic to it. X Used to lower stomach acidity and treat stomach upset. XXThat have severe kidney disease. X Generally well tolerated; constipation or diarrhea can This drug should be used in patients: occur. WITH CAUTION XXWith electrolyte- (salt-) restricted diets, as some of these X Magnesium/aluminum antacids are available over-the- products can have significant amounts of sodium or potassium. counter (without a prescription). Do not give antacids (or any other over-the-counter medications) to your animal XXWith gastric outlet obstruction (inability of the stomach to without first talking with your veterinarian. empty). If your pet has any of these conditions, talk to your veterinarian about the potential risks versus benefits. How is this medication useful? Magnesium hydroxide with aluminum salts can lower stomach What are the side eff ects of this medication? acidity to treat a variety of conditions. The FDA (U.S.
    [Show full text]
  • "Antacids" from the WHO Model List of Essential Medicines Submitted by Abdol Majid Cheraghali ; Pharm.D.; Ph.D
    18th Expert Committee on the Selection and Use of Essential Medicines Application for the removal of "Antacids" from the WHO Model List of Essential Medicines Submitted by Abdol Majid Cheraghali ; Pharm.D.; Ph.D. Professor of Pharmacology Faculty of Medicine University of Baqiytallah Medical Science University Tehran- Iran Fax: (9821) 88601580 [email protected] Summary statement of the proposal for deletion Antacids are oral medicines to relieve heartburn, sour stomach, or acid indigestion. They work by neutralizing excess stomach acid. They mainly consist of aluminum, calcium or magnesium salts. Some antacids, such as aluminum carbonate and aluminum hydroxide, may be prescribed with a low-phosphate diet to treat hyperphosphatemia and/or to prevent the formation of some kinds of kidney stones. These medicines are widely available without a prescription. Long term use of these formulations may cause or exacerbate renal insufficiency (especially in patients with renal insufficiency) and metabolic alkalosis. Despite lack of systematic data on efficacy of these medicines, they have been used for decades in management of dyspepsia and the gastroesophageal reflux disease (GERD). However, currently most up to date clinical guidelines recommend use of proton-pump inhibitor (PPI) medicines or histamine H 2 receptor antagonists for suppression of gastric acid secretion to control symptoms and prevent complications of dyspepsia and GERD. With widespread availability and demonstrated efficacy and safety of PPIs and histamine H 2 receptor antagonists these medicines (especially PPIs) are the recommended first line antisecretary therapy in dyspepsia. Today antacids have no place in current and updated clinical guidelines for management of dyspepsia with or without H.
    [Show full text]
  • Zetia® (Ezetimibe) Tablets
    25751841T REV 03 ZETIA® (EZETIMIBE) TABLETS DESCRIPTION ZETIA (ezetimibe) is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. The chemical name of ezetimibe is 1-(4-fluorophenyl)- 3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone. The empirical formula is C24H21F2NO3. Its molecular weight is 409.4 and its structural formula is: OH OH S R S N F F O Ezetimibe is a white, crystalline powder that is freely to very soluble in ethanol, methanol, and acetone and practically insoluble in water. Ezetimibe has a melting point of about 163°C and is stable at ambient temperature. ZETIA is available as a tablet for oral administration containing 10 mg of ezetimibe and the following inactive ingredients: croscarmellose sodium NF, lactose monohydrate NF, magnesium stearate NF, microcrystalline cellulose NF, povidone USP, and sodium lauryl sulfate NF. CLINICAL PHARMACOLOGY Background Clinical studies have demonstrated that elevated levels of total cholesterol (total-C), low density lipoprotein cholesterol (LDL-C) and apolipoprotein B (Apo B), the major protein constituent of LDL, promote human atherosclerosis. In addition, decreased levels of high density lipoprotein cholesterol (HDL-C) are associated with the development of atherosclerosis. Epidemiologic studies have established that cardiovascular morbidity and mortality vary directly with the level of total-C and LDL-C and inversely with the level of HDL-C. Like LDL, cholesterol-enriched triglyceride-rich lipoproteins, including very-low- density lipoproteins (VLDL), intermediate-density lipoproteins (IDL), and remnants, can also promote atherosclerosis. The independent effect of raising HDL-C or lowering triglycerides (TG) on the risk of coronary and cardiovascular morbidity and mortality has not been determined.
    [Show full text]
  • Prevention and Treatment of Oral Mucositis in Cancer Patients
    Volume 2, Issue 3, 1998 ISSN 1329 - 1874 BestPractice Evidence Based Practice Information Sheets for Health Professionals Prevention And Treatment Of Oral Mucositis In Cancer Patients Introduction This Practice Information Sheet Levels of Evidence Oral mucositis, also called Covers The Following Concepts All studies were categorised according to the strength of the evidence based on the following stomatitis, is a common, debilitating classification system. complication of cancer chemo- therapy and radiotherapy, occurring 1. Quality Of Research Level I Evidence obtained from a systematic in about 40% of patients. It results review of all relevant randomised from the systemic effects of controlled trials. Level II cytotoxic chemotherapy agents Evidence obtained from at least one and from the local effects of 2. Treatment Options properly designed randomised radiation to the oral mucosa. Oral controlled trial. Level III.1 mucositis is inflammation of the Evidence obtained from well mucosa of the mouth which ranges designed controlled trials without 3. What Is Effective randomisation. from redness to severe ulceration. Level III.2 Symptoms of mucositis vary from Evidence obtained from well designed cohort or case control pain and discomfort to an inability analytic studies preferably from more to tolerate food or fluids. Mucositis 4. Recommendations - than one centre or research group. may also limit the patient’s ability Level III.3 Oral Care Protocol Evidence obtained from multiple time to tolerate either chemotherapy or series with or without the radiotherapy. Mucositis may be so intervention. Dramatic results in uncontrolled experiments. severe as to delay treatment and Level IV so limit the effectiveness of cancer Opinion of respected authorities, therapy.
    [Show full text]