Antacids in management of Acid-peptic Disorders
Transcript of Antacids in management of Acid-peptic Disorders
Antacids in managementof Acid-peptic Disorders
Magaldrate 400 mg + Simethicone 20 mg Suspension
For a prompt and quick relief in acid
peptic disorders
Introduction
Acid peptic disorders (APD) are the result of distinctive, but overlapping pathogenic mechanisms leading to either excessive acid secretion or diminished mucosal defense. It usually includes two conditions: Gastroesophageal Reflux Disease (GERD) and peptic ulcer disease (PUD). An epidemiology study in 30,216 patients (41.7±12.7 years; 66% males) reported a prevalence of 7.8% for PUD
1in India. The prevalence of GERD in India is likely to be between 8% and 19% in general population. Antacids are commonly used world over as Over the Counter (OTC) or prescribed medications. They were the mainstay of treatment for acid-peptic disorders until the advent of H receptor antagonist and proton pump inhibitors. Antacids are basic substances that reduce gastric acidity by neutralizing hydrochloric acid. Therapeutic efficacy depends on the metallic ion with which the base is combined. The metallic ion is usually aluminium, magnesium or sodium and hydroxide is the most common base, but trisillicate, carbonate and bicarbonate are also used. They have been used in the treatment for acid-peptic disorders such as peptic ulcers, gastritis, Gastro-
2oesophageal reflux disease (GERD) and functional dyspepsia. Antacids provide relief of heartburn within 5 minutes, but their effect 3
is very short (30 to 60 minutes). Antacids are fast and effective at relieving reflux symptoms.
Magaldrate and Simethicone Suspension
Magaldrate Ÿ Magaldrate is hydroxymagnesium aluminate. It contains the equivalent of 28-39% magnesium oxide and 17-25% aluminum
oxide.Ÿ It reacts with acid in stages; the hydroxymagnesium ion is relatively rapidly converted to magnesium ion and the aluminate to
hydrated aluminium hydroxide and then to aluminium salts.2,4
Ÿ It is a good antacid with prompt and sustained neutralizing action.
Simethicone Ÿ Simethicone is an orally administered antifoaming agent, used to
reduce gas from the digestive tract in patients complaining of recurrent flatulence.
Ÿ It is a mixture of dimethicone (polydimethylsiloxane) and hydrated silica gel (silicon dioxide).
Ÿ Simethicone is pharmacologically inert and is therefore considered relatively safe.
Ÿ It acts by decreasing the surface tension of gas bubbles, thus facilitating their coalescence and expulsion as flatus or belching. It also prevents the formation and accumulation of mucus-enclosed pockets of gas in digestive tract. Simethicone also facilitates the passage of gas through bowel lumen and allows patients to excrete a greater volume of gas at one time, thereby reducing the number of flatus events.
Ÿ It is used as an effective adjunct therapy in conditions where excessive gas is aggravating the symptoms in conditions such as
Table 1. Recommendations of the Roman Society of Neurogastroenterology concerning the use of antacids in GERD-2016
Statement Expertsagreement
Level ofevidence
Grade ofevidence
Grade ofrecommendation
Antacids are slightly superior over placebo in treating heartburn
Antacids may be used to rapidly relief uncontrolled GERD symptoms
Antacids may be used as over-the counter drugs, to treat mild or infrequent reflux symptoms, especially in NERD patients who choose to self-medicate
Antacids (calcium or magnesium-containing antacids) can be used in pregnant women with GERD symptoms.
In pregnant women, there is no clear difference in the rate of side effects between antacids and placebo.
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Antacids in management of Acid-peptic Disorders
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Figure 1. O'Brien sum score of normalized symptom changes from baseline (± S.E.M.) after 2, 4 and 8 weeks of treatment.
References 1.Rai RR, Gangadhar A, Mayabhate MM. Clinical profiling of patients with Acid Peptic Disorders (APD) in India: a cross-sectional survey of clinicians. Int J Basic Clin Pharmacol 2017;6:194-202. Md. Jakaria, Zaman R, Parvez M et al. Comparative Study among the Different Formulation of Antacid Tablets by Using Acid-Base 2.Neutralization Reaction. Global Journal of Pharmacology. 2015; 9(3): 278-281. Surdea-Blaga T, Băncilă I, Dobru D et al. Mucosal Protective Compounds in the 3.Treatment of Gastroesophageal Reflux Disease. A Position Paper Based on Evidence of the Romanian Society of Neurogastroenterology. J Gastrointestin Liver Dis. 2 0 1 6 ; 2 5 ( 4 ) : 5 3 7 - 5 4 6 . D r u g s f o r P e p t i c U l c e r a n d G a s t r o e s o p h a g e a l R e fl u x D i s e a s e . A c c e s s e d f r o m w e b s i t e4 . http://202.74.245.22:8080/xmlui/bitstream/handle/123456789/930/Chapter%2046-%2050.pdf?sequence=12 as on 08.04.2019. 5.Parakh RK and Patil NS. Anaesthetic antacids: a review of its pharmacological properties and therapeutic efficacy. Int J Res Med Sci. 2018 ;6(2):383-393. Holtmann G, Gschossmann J, Mayr P et al. A 6.randomized placebo-controlled trial of simethicone and cisapride for the treatment of patients with functional dyspepsia. Aliment Pharmacol Ther. 2002;16(9):1641-1648.
5dyspepsia, peptic ulcer, post-operative gaseous distention and irritable colon.
Ÿ A study comparing the efficacy of simethicone (105 mg t.d.s.) with placebo (t.d.s.) and the prokinetic cisapride (10 mg t.d.s.) in 185 patients with functional dyspepsia showed that Simethicone was significantly better than cisapride after 2 weeks (p = 0.0007; Figure 1), but the differences were not statistically significant after 4 and 8 weeks. Patients treated with simethicone judged the efficacy of their treatment as very good in 46% of cases, compared to 15% and 16% receiving cisapride and placebo, respectively.
Dried Aluminium Hydroxide + Magnesium Hydroxide + Simethicone Suspension
Aluminium Hydroxide Ÿ Aluminium hydroxide is the one of the most commonly in antacid formulations more often in combination with magnesium
hydroxide and used rarely alone as a single substance.Ÿ Aluminium hydroxide is found to be absorbed, in only relatively small amounts, into the digestive tract. Ÿ The onset of action of aluminium hydroxides ranges from 5-10 minutes and its action lasts for about 100 minutes. Ÿ Aluminium hydroxide inhibits pepsin activity by increasing pH and through adsorption and exerts cytoprotective effects
1through increases in bicarbonate ion and prostaglandins.
Magnesium HydroxideŸ Magnesium hydroxide suspension neutralizes gastric acid by reacting with hydrochloric acid in the stomach to form
magnesium chloride and water. Ÿ It decreases the direct acid irritant effect and increases the pH in the stomach leading to inactivation of pepsin. Ÿ Magnesium hydroxide enhances the integrity of the mucosal barrier of the stomach as well as improving the tone of both the
1gastric and esophageal sphincters.
Antacid combinations – How are they beneficial?A combination of two or more antacids is frequently used. These may be superior to any single agent on the following accounts:
(a) Fast (Magnesium hydroxide) and slow ( A l u m i n i u m h y d r o x i d e ) a c t i n g components yield prompt as well as sustained effect.
(b) Magnesium salts are laxative, while aluminium salts are constipating: combination may annul each other's action and bowel movement may be least affected.
(c) Gastric emptying is least affected; while aluminium salts tend to delay it, mag./cal. salts tend to hasten it.
(d) Dose of individual components is reduced; systemic toxicity (dependent on fractional
2absorption) is minimized.
Simethicone Ÿ Simethicone is an orally administered
antifoaming agent, used to reduce gas from the digestive tract in patients complaining of recurrent flatulence.
Figure 1. Reflux treatment guidelines for over-the-counter medications.
Alarm SymptomsŸ DysphagiaŸ Frequent vomitingŸ GI bleedingŸ Weight loss
Typical symptomsŸ HeartburnŸ Regurgitation
Non-alarm symptomsŸ AsthmaŸ Chronic coughŸ Chronic hoarsenessŸ Nausea and vomitingŸ Unexplained chest pain
Refer for urgent diagnostic evaluation
In pregnancy prefer calcium/magnesium containing antacids
Lifestyle and dietary modifications (LDM)
Recurrent/intermittent symptoms
OTC antacids* as required Relief
Recurrent symptoms
OTC antacids/H RAs2
Recurrent symptoms
Relief
Seek medical advice
Refer for diagnostic evaluation
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Ÿ Simethicone is pharmacologically inert and is therefore considered relatively safe.Ÿ Simethicone prevents the formation and accumulation of mucus-enclosed pockets of gas in digestive tract. It is used as an
effective adjunct therapy in conditions where excessive gas is aggravating the symptoms in conditions such as dyspepsia, peptic 1
ulcer, post-operative gaseous distention and irritable colon.
Safety in pregnancy Ÿ About 30-50% of women required only antacids to ease their heartburn of pregnancy. Ÿ Magnesium, aluminium, or calcium containing antacids have been reported to have no teratogenic risk, and also magnesium
and aluminium hydroxide containing antacids were reported safe during lactation. Ÿ A European consensus conference has recommended Ca/Mg-based antacids for pregnant women because of their safety
1,3-5 profile.
References 1.Parakh RK and Patil NS. Anaesthetic antacids: a review of its pharmacological properties and therapeutic efficacy. Int J Res Med Sci. 2018 ;6(2):383-393. Drugs for Peptic Ulcer and Gastroesophageal Reflux Disease. Accessed from website http://202.74.245.22:8080/xmlui/bitstream/handle/1234562.789/930/Chapter%2046-%2050.pdf?sequence=12 as on 08.04.2019. Black RA, Hill DA. Over-the-counter medications in pregnancy. Am Fam 3.Physician. 2003;67(12):2517-2524. Tytgat GN, Heading RC, Muller-Lissner S et al. Contemporary understanding and management of reflux and 4.constipation in the general population and pregnancy: a consensus meeting. Aliment Pharmacol Ther. 2003;18:291-101. Thorpe PG, Gilboa SM, 5.Hernandez-Diaz S, et al. Medications in the first trimester of pregnancy: most common exposures and critical gaps in understanding fetal risk. Pharmacoepidemiol Drug Saf. 2013;22(9):1013-1018.
61/C, 6th Main Road, 4th Phase, 7th BlockB.S.K 3rd Stage, Bangalore - 560085.
2019
Indications:
Ÿ Heart burn symptoms in Gastroesophageal reflux disease (GERD)
Ÿ Acid indigestion
Ÿ Sour Stomach
Ÿ Gastric and Duodenal ulcer
Ÿ Flatulence and abdominal distension bloating
Dosage in Adults:
Ÿ 1-2 teaspoonfuls daily or as advised by the Physician
Indications:
Ÿ Peptic ulcers
Ÿ Non-ulcer dyspepsia
Ÿ Functional dyspepsia
Ÿ Stress gastritis
Ÿ Heart burn symptoms in Gastroesophageal reflux disease (GERD)
Ÿ Flatulence and abdominal distension bloating
Ÿ Biliary reflux
Dosage in Adults:
1-2 teaspoonfuls daily or as advised by the Physician
Magaldrate 400 mg + Simethicone 20 mg Suspension
Also available
Dried Aluminium Hydroxide 200mg+Magnesium Hydroxide 200mg+Simethicone 25mg Suspension (MINT Flavour)