Antacids - StatPearls - NCBI Bookshelf https://www.ncbi.nlm.nih.
gov/books/NBK526049/
NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.
StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan-.
Antacids
Blake H. Salisbury; Jamie M. Terrell.
Author Information and Affiliations
Last Update: August 8, 2023.
Continuing Education Activity
Antacids are a group of drugs that have been on the market for many years. They were initially
first-line defense against peptic ulcer disease; however, the discovery of proton pump inhibitors
revolutionized the treatment of peptic ulcer disease. Currently, antacid use is restricted to relieve
mild intermittent gastroesophageal reflux disease (GERD) with associated heartburn. This
activity reviews the indications, contraindications, pharmaceutical action, adverse events, and
other key elements of antacid therapy in the clinical setting as relates to the essential points
needed by members of an interprofessional team managing the care of patients with heartburn
and mild GERD.
Objectives:
• Identify the mechanism of action antacids.
• Summarize the indications for antacid therapy, including relevant interactions with other
medications.
• Review the potential adverse events associated with the use of antacids.
• Outline the role of interprofessional coordination in guiding patient care and improving
outcomes when using antacid therapy.
Access free multiple choice questions on this topic.
Indications
Antacids are a group of drugs that have been on the market for many years. They were initially
first-line defense against peptic ulcer disease; however, the discovery of proton pump inhibitors
revolutionized the treatment of peptic ulcer disease. Currently, antacid use is restricted to
relieving mild intermittent gastroesophageal reflux disease (GERD) associated with heartburn.[1]
The estimated prevalence of heartburn at least once per week in North America ranges from 18%
to 28%, with 25% of adults reporting heartburn daily.[2][3][4][5]
Antacids are medications that do not require a prescription; in other words, they are self-
prescribed. Antacids are a combination of various compounds with various salts of calcium,
magnesium, and aluminum as active ingredients. The antacids act by neutralizing the acid in the
stomach and by inhibiting pepsin, which is a proteolytic enzyme. Each of these cationic salts has
a characteristic pharmacological property that determines its clinical use. Antacids have
therapeutic use for the following[6]:
• Heartburn symptoms in GERD
• Duodenal and gastric ulcers
• Stress gastritis
• Pancreatic insufficiency
• Non-ulcer dyspepsia
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• Diarrhea caused by bile-acid
• Biliary reflux
• Constipation
• Osteoporosis
• Urinary alkalinization
• Phosphate binding in chronic renal failure
Mechanism of Action
The antacids reduce the acid reaching the duodenum by neutralizing the acid present in the
stomach. The main therapeutic objectives are:
• Alleviating pain
• Relieving pylorospasms
• Avoid digestion and corrosion by acid chyme
The salts' mechanism of neutralization of acid varies, and each salt has a different mechanism
with the ultimate goal of acid neutralization.
Aluminum Hydroxide
The formulation of aluminum hydrochloride and water results in the neutralization of the acid in
the stomach. It is also known to inhibit pepsin activity.[7] Aluminum hydroxide is complexed
with a sulfated polysaccharide sucrose octasulfate to form sucralfate. This complex does not have
a significant buffering action against the acid or has no effect on the pepsin secretion, and does
not alter the gastric acid production in any way.[8][9] Nevertheless, it is known to heal chronic
ulcers and prevent acute mucosal damage induced chemically by reducing access to pepsin and
acid. Sucralfate, like its aluminum hydroxide component, is known to stimulate angiogenesis and
granulation tissue formation.[8]
Aluminum hydroxide is also useful in hyperphosphatemia due to its ability to bind phosphate in
the gastrointestinal (GI) tract and subsequently prevent the absorption of phosphate.[10]
Calcium Salts
Calcium salts neutralize gastric acidity, resulting in increased gastric and duodenal bulb pH; they
also inhibit pepsin's proteolytic activity if the pH is greater than 4 and increase lower esophageal
sphincter tone. The calcium released from calcium carbonate is known to increase peristalsis in
the esophagus, pushing the acid into the stomach and providing relief from heartburn symptoms.
The calcium salts also form combined insoluble compounds with dietary phosphate and prevent
the absorption of the latter.[11]
The acid-neutralizing mechanism of the antacids is well understood, as mentioned above. In
addition to this, other mechanisms add to the ulcer healing properties of this class of drugs. The
exact mechanism is still unclear, but it is believed to be a combination of[12][7]:
• Ability to promote angiogenesis
• Bind to bile acids
• Inhibit peptic activity
• Suppress Helicobacter pylori growth
Administration
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Antacids - StatPearls - NCBI Bookshelf https://www.ncbi.nlm.nih.gov/books/NBK526049/
The dose for antacids depends upon the patient's age, the purpose of administration
(neutralization of acid or off-label use), and the presence of other comorbidities like renal or
hepatic impairment. As all the forms of these medications are available in over-the-counter
formulations, the dosing recommendation varies by product/and or manufacturer.
Aluminum Hydroxide (Antacid)
• Oral: Usually taken daily after meals and at bedtime at a dose of 640 mg up to 5 to 6 times
a day with a maximum dose of 3,840 mg per 24 hours.
• Suspension The dose for suspension form is 320 mg/5 mL (473 mL). The suspension is to
be shaken before use and is to be followed by water.
Hyperphosphatemia
• Oral: Use is reserved for patients with serum phosphorus levels greater than 7 mg/dl. It is
to be taken with meals at a dose of 300 to 600 mg three times a day, with use limited to a
short period (4 weeks).[13]
Calcium Carbonate (Antacid)
It is used up to a maximum dose of 8000 mg per day (1 to 4 tablets daily) for up to two weeks for
symptomatic relief.
Hyperphosphatemia
The total dose is not to exceed 2000 mg per day.[13]
Pregnancy and Breastfeeding
Antacids containing aluminum salts are safe to be used in pregnant women as well as for women
during labor for aspiration prophylaxis. The information regarding the use of aluminum-
containing antacids in breastfeeding females has not been studied, but aluminum is known to be
endogenous to breast milk.[14][15] In the case of calcium-containing antacids, excessive use is to
be avoided in pregnant women as calcium crosses the placenta. The amount of calcium reaching
the fetus is dependent on the physiological changes in the mother. Maternal calcium intake also
affects the amount of calcium excreted in breast milk; the currently prevailing opinion is that the
use of calcium-containing antacids is safe during breastfeeding.[16]
Adverse Effects
Adverse effects are prominent in the infant and the elderly populations. The chronic use of
antacids in this population is not a recommendation due to safety concerns.
Aluminum Hydroxide
Aluminum use is associated with an increased risk of toxicity in individuals with renal failure and
infants. It presents as[17][18][19][20]:
• Osteopenia
• Microcytic anemia
• Neurotoxicity
• Osteomalacia
• Constipation
• Fecal impaction
• Nausea
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• Vomiting
• Abdominal cramps
• Hypomagnesemia
• Hypophosphatemia
Calcium Carbonate
The adverse reactions often seen with this group of antacids are[20][21]:
• Abdominal pain
• Anorexia
• Constipation
• Acid rebound
• Nausea
• Vomiting
• Flatulence
• Xerostomia
• Headache
• Hypercalcemia
• Hypophosphatemia
• Milk-alkali syndrome
Antacids can exhibit clinically significant interactions with other medication a patient may be
taking.[22] Some examples include:
• Using antacids concomitantly with acidic drugs (e.g., digoxin, chlorpromazine
isoniazid) can result in impaired absorption of these acidic drugs, reducing the blood
concentrations of the drugs and impairing their therapeutic effects.
• Concurrent antacid use with some drugs (e.g., pseudoephedrine, levodopa) can result
in increased absorption of the drugs, leading to potential toxicity or adverse events from
increased serum concentration of these drugs.
• Antacids containing magnesium trisilicate and magnesium hydroxide can bind to drugs like
tetracycline and fluoroquinolone antibiotics, impeding their absorption and therapeutic
effects.
• Sodium bicarbonate significantly affects urine acidity, which can alter the renal elimination
of some drugs by the kidney; sodium bicarbonate inhibits the excretion of basic drugs such
as amphetamines and quinidine while increasing the excretion of acidic drugs like aspirin.
Contraindications
The absolute contraindication is hypersensitivity to any component of the formulation. Also,
antacid agents require caution in patients with:
• Renal failure
• Heart failure
• Edema
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• Cirrhosis
• Low-sodium diets
• Uremia
• GI hemorrhages
• Hyperparathyroidism
• Renal calculus
• Achlorhydria
Monitoring
The average therapeutic dose of antacid is 10 to 15 mL (1 tablespoon or one package content) of
liquid or 1 to 2 tablets 3 to 4 times a day. Periodic monitoring of calcium and phosphorus plasma
concentrations is a suggested practice in patients on chronic therapy.
Toxicity
No information is available regarding toxicities caused by aluminum- and calcium-
containing antacids. However, antacids are to be used cautiously in the high-risk population
mentioned above.
Enhancing Healthcare Team Outcomes
Antacids are available as over-the-counter medications, meaning that patients do not require a
prescription to obtain them. These medications only provide symptomatic relief, which may mask
an underlying disorder, but lack of awareness in this regard may delay the diagnosis in health
conditions like GERD, peptic ulcer, gastric ulcer, and hiatal hernia. This situation results in the
improper use of these medications with little to no relief of symptoms. There is a need to educate
patients regarding the importance of a correct mode of administration, time of administration, and
dosage for the prompt and prolonged relief of symptoms. Although these medications do not
cause toxicities in high doses, it is imperative to understand their interaction with other
medicines, especially in patients engaged in polypharmacy.[23]
Nursing can verify drug use on intake and at each exam and report to the treating clinician.
Pharmacists will encounter patients in the retail pharmacy and can counsel and educate patients
on the advantages and pitfalls of antacid therapy and inform the patient's treating physician if
there are any issues (drug-drug interactions, for example). Even a medication as apparently
benign as OTC antacids can significantly affect patient health, and the interprofessional team
needs to work together and communicate to achieve positive outcomes. [Level 5]
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