International Journal for Environmental Rehabilitation and Conservation

ISSN: 0975 — 6272

XI (SP2): 114 — 119 www.essence-journal.com Review Article

A review on pharmacology and therapeutic uses of

Saraswat Renu1, Chatterji Nupur1 and Saraswat Devesh2 1Department of Chemistry, Meerut college, Meerut, India 2Department of chemistry, Eicher School, Faridabad, India Corresponding Author: [email protected]; [email protected]

A R T I C L E I N F O Received: 20 July 2020 | Accepted: 15 August 2020 | Published Online: 30 September 2020 EOI: 10.11208/essence.20.11.SP2.136 Article is an Open Access Publication. This work is licensed under Attribution-Non Commercial 4.0 International (https://creativecommons.org/licenses/by/4.0/)

©The Authors (2020). Publishing Rights @ MANU—ICMANU and ESSENCE—IJERC.

A B S T R A C T Antacids have been used since the last more than hundred years for the symptomatic relief by raising the pH of the stomach and without hampering the gastric condition of the body namely killing of bacteria. bicarbonate, hydroxide, hydroxide besides ranitidine and the prazoles react with the HCL present in the stomach and have become the ready choice of physicians to treat all kinds of gastric disorders. This study sheds a light on the pharmacokinetics of various antacids, their advantages, disadvantages and the chemical conditions which they help to subside. Present paper specifically focuses on the study of clinical uses and side effects of long run use of antacids

K E Y W O R D S Antacids | Gastric pH | GERD | Ulcer

C I T A T I O N Saraswat, Renu; Chatterji, Nupur and Saraswat, Devesh (2020): A review on pharmacology and therapeutic uses of Antacids. ESSENCE Int. J. Env. Rehab. Conserv. XI (SP2): 114 — 119. https://eoi.citefactor.org/10.11208/essence.20.11.SP2.136

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Introduction antacids. They are usually the hydroxides of Drugs: The term drug is derived from the aluminium, magnesium, or sodium french word "DROGUE" which means bicarbonate which are alkaline in nature and herbs. Natural products extracted from counteract the acid in the stomach to make plants, fungi, algae, sponges, animals and the pH more neutral. The normal gastric pH worms have been used for the treatment of range of the stomach is 1.5 to 3.5. diseases since time immemorial.A drug is a Antacids were used in the treatment of natural or synthetic substance which when gastric problems since a long time. They give administered affects the functioning and relief from the condition of hyperacidity and structure of a living body. These drugs can other gastrointestinal problems by neutrlizing be used for the diagnosis ,treatment or the gastric acid and thereby increasing the prevention of a disease and at the same time pH of gastric contents, balancing acid-base relieving of the discomfort. . As a number of ratio, lowering the pepsin activity and raising herbs are being used since ancient times for bicarbonate and prostaglandin secretion. The the treatment of various ailments therefore antacids quickly relieve occasional heartburn compounds and herbs for treatment of which happens to be the major symptom of various diseases are known as drugs in gastroesophageal reflux disease (GERD). modern age also. They do not kill bacteria or inhibit other Drugs are the chemical compounds which actions of body and hence are distinct from are either synthesized in the laboratory or of the reducing drugs. plant animal or marine origin and intends to Gastroesophageal reflux (GERD) is a normal bring change in normal physiological physiological process short duration, often function of the body. Medicinal or remain asymptomatic, and limited to the therapeutic drugs are the substances or distal part of esophagus. According to the preparations which are used in the treatment American College of Gastroenterology of diseases. Thus in short we can say that all GERD is defined as the “mucosal damage medicines are essentially drugs but all drugs that produce chronic symptoms by the are not medicines. abnormal presence of gastric juices in the Monitoring of therapeutic drugs is a branch esophagus produced by hyperacidity”. of clinical chemistry and clinical Types of Antacids pharmacology that deals with the Drugs are classified mainly into two measurement of concentration in categories on the basis of digestive the blood. Drugs are basically chemicals absorption which affect the course of conditions, 1. Absorbable diseases, syndrome or pathology to benefit  Sodium carbonate (baking soda) the health of an individual.  (magnesia) Antacids and their medical uses  Magnesium carbonates A common class of medicines that neutilize  Calcium carbonates the acid presnt in the stomach, heartburn,  Bourget mixture (sodium bicarbonates, indigestion and upset stomach are termed as sulphate, phosphate) 115

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 Rennie mixture (calcium carbonates,  magnesium carbonates)  Aluminum-magnesium combination  Tums mixture (calcium carbonates,  Aluminum-magnesium combination with magnesium oxide). other Active ingredients (anesthetics, antiflatulents, alginates, etc.) Table 1 2. Non-absorbable

 Aluminum phosphate  Aluminum hydroxide  Magnesium silicate S. No. Advantages disadvantages Clinical conditions 1. Calcium Potent and rapidly GI distress Heartburn Acid indigestion carbonate acting Nausea/vomiting Upset stomach Hypercalcemia Hypo- phosphatemia, milk-alkali syndrome

2 Magnesium Slow but prolonged Low solubility and Dyspepsia Heart burn trisilicate action laxative (at reactivity, Absorbed Hyperacidity larger doses) systemically (problem in renal compromised function patients) 3 Magnesium GI distress, Electrolyte Hyperacidity and peptic ulcer carbonate imbalances Hypotension dyspepsia heartburn GERD Neuromuscular blockade Constipation hypotension 4 Magnesium Reacts with HCl Low water solubility, no Constipation, digitalis toxicity hydroxide Promptly and is an systemic alkalosis (mg is Gastric acidity efficacious antacid, low poorly absorbed from gut) Hypomagnesaemia Peptic ulcer systemic absorption Pre-eclampsia, Magaldrate 5 Magaldrate Good oral antacid with Constipation Gastritis Hyperacidity Reflux prompt and sustained Intestinal pain neutralizing action 6 Aluminium Raises the pH of the Efficient, low systemic Chronic diarrhea, hyper hydroxide gastric juice, Adsorbs absorption, Decreases parathyroidism pepsin phosphate via Hyperphosphatemia (in renal kidney failure), nephrolithiasis, peptic ulcer, reflux esophagitis, stress ulcers 7 Sodium Most rapidly acting Metabolic alkalosis with Heartburn Alkalinisation of bicarbonate antacid urine alkalinisation, Intake urine Acidosis of large doses Table 1: Important Antacids and their features

Conventional antacids offer less combination of simethicone and loperamide symptomatic relief from gastric problems (Imodium Advanced) and is effective in and therefore their use has been declined relieving abdominal bloating however, it has with the availability of more efficacious anti- not been studied in nondiarrhoea-associated acid secretory (H2 blockers and flatulence. PPIs). Pharmacokinetics An important type of antacid usually given Absorbable antacids are rapidly dissolving after the administration of Anaesthesia or to substances that immediately react with reduce post operational acidity is a hydrochloric acid in the stomach forming 116

ESSENCE—IJERC | Saraswat et. al., (2020) | XI (SP2): 114 — 119 carbon dioxide and water. Carbon dioxide units in the GERD pathogenesis. In case causes gastric distention which provokes of erosive GERD antacids are given as a gastroesophageal reflux and stimulates co-drug to the PPIs main course. gastric secretion enhancement. 2. Acute gastritis: In this case antacids are used in addition to proton pump Most of the antacids used are non adsorbable inhibitor therapy, H2-blockers in the but Sodium carbonate acts differently as it is treatment of acute gastritis especially absorbed into the blood affecting the with severe pain and dyspeptic organisms pH in whole. Patients with syndromes. They play an important role absolute renal failure excrete the excess of in the prevention and/or treatment of bicarbonate rapidly while some of this acid reflux. The presence of bile acids bicarbonate is accumulated causing systemic and lysolecithin(responsible for fat alkalosis in cases of patients with breakage)poses a hinderance in their parafunction of the kidneys. Most antacids action. used in medical practice are non-absorbable, 3. Chronic Gastritis / Gastroduodenitis: without systemic pharmacokinetics. To prevent recurrences, antacids are Indications and Principles of Сlinical Use either used alone or in combination with Clinical chemistry is the branch of chemistry antisecretory agents. These drugs that deals in the therapeutic management of supposed to be of choice for preventing drugs and specializes in the measurement of and treating eflux gastritis, where the the concentration of medicines in the blood main disturbing factor are found to be .High security Antacid are supposed to be bile acids and lysolecithin. the drugs of choice for the self treatment 4. Gastropathy caused by nonsteroidal because of the quick symptomatic effect, anti-inflammatory drugs (NSAIDs - pleasant organoleptic properties and, gastropathy): In order to prevent convenient presentation (suspensions, duodenopathies and gastropathies chewable tablets). Therapeutic indications of affected by the administration of antacids for the treatment of acid related nonsteroidal antiinflammatory drugs disorders of proven effectiveness belongs to (NSAIDs) antacids can either be taken the class H2 antagonists, proton pump alone or can be taken in addition to inhibitors and eradication therapy of antisecretary drugs. infection Helicobacter pylori 5. Gastric and duodenal ulcer: Here In this case antacids are mainly used for 1. Gastroesophageal reflux disease severe pain treatment during the (GERD): The main function of antacids screening phase and within first day of in this disorder is to neutralize PPIs administration before the acid hydrochloric acid, absorb bile acids, production blockade (after 1-3 days). inactivate pepsin, , stimulate the 6. For dyspeptic syndromes and pains: synthesis of bicarbonates and raise the For the healthy people with discomfort tone of the lower esophageal sphincter or dyspeptic symptoms (heartburn, thereby affecting on the majority of 117

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belching, meteorism) and epigastric pain drugs in the blood which ultimately antacids are recommended .Non- results in lowering the effects of the absorbable antacids are used as the drugs. essential drug to relieve heartburn in  Antacids taken with drugs such as pregnancy, which occurs in pseudoephedrine (Sudafed, Semprex D, approximately (50-80 %). Clarinex-D 12hr, Clarinex-D 24hr, 7. Prevention of (stress) Ulcers: Antacids Deconsal, Entex PSE, Claritin D, and are used in the intensive care units to more), and levodopa (Dopar), increase prevent so-called (stress) ulcers (in absorption of the drugs and this may patients after a major operation, with result in adverse events or toxicity due to craniocerebral traumas - Cushing's increased concentration of the drugs in ulcers or with severe burns – Curling's the blood levels. ulcers, etc.).  Antacids that consists of magnesium hydroxide [Mg(OH) ] and magnesium Side effects of long term use of antacids 2 trisilicate when taken with some other  Antacids may cause hyperacidity and medications (like ) will bind milk-alkali syndrome which depends on to the drugs, and reduce their absorption its dose. and effects.

 Antacids that contain aluminum  (Na2CO3) has a very hydroxide [Al (OH)3 ]may cause strong effect on the acidity of the urine, hypophosphatemia ,aluminum- and this can affect the elimination intoxication, constipation and (excretion) of some drugs by the kidney. osteomalacia. Thus the presence of sodium bicarbonate  Antacids that contain magnesium are inhibits the excretion of some basic found to have a laxative effect that may drugs like quinidine (Quinidex, cause diarrhea. Patients with renal failure Quinidine Sulfate Quinidine Gluconate, are unable to eliminate magnesium from Quinidine Injection) and amphetamines, the body with urine thus leading to and thereby results in the increases of increased magnesium levels in the blood. excretion of some acidic drugs like  Sodium containing antacids are harmful aspirin. for the patients on sodium restricted diet Conclusion while calcium containing antacids may cause kidney stone formatiom.. Antacids have gained considerable confidence for the treatment of gastric With which drugs do antacids interact? disorders due to the prolonged relief and  When antacids are taken with acidic quick action with the administration of low drugs (e.g digoxin [Digitek] , [isoniazid] doses. Anaesthetic antacid which are mainly ,phenytoin [Dilantin], chlorpromazine a combination of aluminium and magnesium [Thorazine], ), they cause the absorption hydroxides with an Anaesthetic (oxethazine) of the acidic drugs to be decreased, is recently becoming a choice for the which reduces the concentrations of the 118

ESSENCE—IJERC | Saraswat et. al., (2020) | XI (SP2): 114 — 119 treatment of GERD ,ulcers and other Maton, P. N., Burton, M. E. (1999): Antacids conditions relating to acidity .These Revised: A Review of their clinical anaesthetic antacids remain non iodised in pharmacology and recommended hyper acidic conditions causing numbness of therapeutic use. Drugs, 855-70. the duodenum thus reducing the pain besides Pontes, J. F., Richards, D. J. and Sartoretto, neutralizing acids normally. J. N. (1975): Double-blind The therapeutic efficacy of this group of comparison of an oxethazaine-antacid antacids in the light of low dosage ,side combination (Oxaine M) against the effects and the faster and long duration of the antacid alone (Aludrox) in the relief of symptoms is better and needs to be treatment of duodenal ulcer pain. looked further into Curr Ther Res Clin Exp, 18:315-23.

References Uenishi, K. (2010): Fractional absorption of active absorbable algal calcium Badillo, R. (2014): Diagnosis and treatment (AAACa) and of gastroesophageal reflux disease / measured by a dual stable-isotope R. Badillo, D. Francis World J method / K. Uenishi, H. Ishida, Y. Gastrointest Pharmacol Ther. 5(3): Fujii [et al.] Nutrients, 2 (7): 752- 105-112. 761. Belousov Yu, B. (2010): Clinical Veber, V. (2009): Clinical Pharmacology / Pharmacology and Pharmacotherapy V. Veber. Medicine, 448. / Y. Belousov. – M.: Medical News Agency, 884. Zhang, Y. F. (2014): Effects of an Al (3+)- and Mg(2+)-containing antacid, Chiba, N. and Fennerty, M. B. (2010): ferrous sulfate, and calcium Gastroesophageal reflux disease. carbonate on the absorption of Evidence-based gastroenterology & nemonoxacin in healthy Chinese hepatology. Third edition. Editor: volunteers / Y.F. Zhang, X.J. Dai, T. John W.D. McDonald, Andrew K. Wang [et al.] Acta Pharmacol Sin, Burroughs, Brian G. Feagan, M. 35(12): 1586-1592. Brian Fennerty,19.

Hanauer, S. B., DuPont, H. L., Cooper, K. M. and Laudadio, C. (2007): Randomized, double-blind, placebo- controlled clinical trial of loperamide plus simethicone versus loperamide alone and simethicone alone in the treatment of acute diarrhea with gas- related abdominal discomfort. Curr. Med Res Opin.23:1033-43.

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