Download Chemistry of antacids

Chia Jia Yan
Lee Dang Ni
Lim Chai Ying
Lim Ren Hann
U062203H
U051984H
U062410N
U062774H
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Introduction
Types of antacids
Usage and treatment
Mode of action & reaction
Side effects
Combination Drugs
Conclusion
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Stomach contains gastric acid of pH of 2 to 3.
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Gastric acid contains HCl, KCl and NaCl.
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Excess acid can cause pH to fall below 2 which
can cause problems such as abdominal pain and
heartburn etc.
Gastric juice activates pepsin, an enzyme that
carries out proteolysis – break down proteins by
breaking bonds that links amino acids
Parietal cell produce gastric acid using
proton pump H+/K+ ATPase, an
enzyme.
Epithelial cells
As a proton pump, it transport 1 H+ in
exchange of 1 K+ from stomach against
concentration gradient with ATP
providing the energy.
Picture taken from My Optum Health.
http://www.myoptumhealth.com/portal/DiseasesandConditions/item/Gastroesophageal+reflux+disease+and
+hea?section=2 (accessed on 8 April 2009)
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Alkaline salt or buffer substances
used to neutralize stomach acid
and bring its pH back to 2 to 3
Treat indigestion or relieve any
discomfort caused by acidity of
stomach acid
Reduces acid concentration
within the lumen of the
esophagus which increase the
intra-esophageal pH and decrease
pepsin activity
In forms of tablet, liquid suspension , lonzenges, chewing
gum, dissolving tablet
Liquid relief symptoms faster
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Active ingredient: Basic metal salt
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Cations used are highlighted in Red
Anions used: OH-, O2-, CO32-, HCO3-, HPO3-, Trisilicate (Mg), amino
acetate (Al)
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Commonly used: Al(OH)3, MgOH, CaCO3
By mixing and matching cations and anions, combining
different types of antacids, unique attributes, properties and
potency of antacids are created.
Either Mixture or Complex antacids
Other common ingredient:
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Simethicone – relieve gas by breaking down bubbles
Alginic acid – foaming agent that floats on top of
stomach content
Calcium Carbonate
Magnesium Salts
Aluminium Salts
(usually hydroxide)
 Alka-mints tablets
 Childrens’ Mylanta
Tablet
 Chooz Gum
 Alcalak
 Titralac
 Milk of Magnesia
 Maalox
 Philips Tablets
 Mylanta
 Philips Oral Suspension  ALternaGEL
 Most potent antacid
ingredient; acts rapidly
with more prolonged
action than sodium
bicarbonate
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 Most stable form of
Can use hydroxide,
aluminium salts under
phosphate & trisilicate
normal conditions
(common in Singapore)
Calcium Carbonate
 Fast acting and long
lasting effect
 Good when patient
suffers from calcium
deficiency
Magnesium Salts
Aluminium Salts
(usually hydroxide)
 Less potent that Ca
 May be dehydrated to
 hydroxide has the
form powder that readily
highest potency
dissolves in acids
 Slow acting
 Mild and slow acting
 Magnesium antacids are
antacid, last longer
generally NOT
 Insoluble in water and
absorbed. Any small
forms a suspension/gel
amounts are cleared
that coats and protects the
renally
stomach lining
 Most appropriate if
patient suffers from renal
failure
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Antacids needs to be in hydrated form for better
neutralizing effect
Aluminium Antacids
 Aluminium based antacids preferred for kidney failure
patient as it can be used to remove excess phosphate ions
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Other usage:
Magnesium used as a laxative for constipated patient
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Strength of an antacid to neutralize acid in the stomach is determined
using the antacid’s neutralizing capacity (ANC)
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ANC is expressed as milliequivalents (mEq) of the amount of 1N HCl
that can be neutralized
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FDA: all antacids must have a neutralizing capacity of at least 5 mEq
per dose.
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The commonly used antacids are ranked in this order with respect to
ANC, from strongest to weakest
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CaCO3 > NaHCO3 > Mg(OH)2 > Al(OH)3
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CaCO3 + 2 HCl  CaCl2 + H2O + CO2
1g will neutralize 20mEq of acid
CaCl2 + CO32-  CaCO3 + Cl- (higher pH in intestine)
Some unchange calcium is absorbed by the gut, which
can raise the pH of the blood causing alkalosis – can
affect proteins
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Magnesium oxides, hydroxides and carbonates are poorly
soluble, only Chloride are soluble.
Mg(OH)2 + 2HCl  MgCl2 + 2H2O
1 g can neutralize 2.7 mEq of acid
MgCl + HCO3-  MgCO3 +
Although non-absorbable, 5% - 10% of Mg enter systemic
circulation which then rapidly removed by kidney
Al(OH)3 + 3HCl  AlCl3 + 3H2O Al(H2O)63+
1 g can neutralize 0.4 – 1.8 mEq of acid
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Solubility of Al increases as pH decrease
Complex antacids can be used.
E.g. Magaldrate [Mg(OH)Al2(OH)10]4-.2H2O
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Causes constipation
Relaxation of the gastrointestinal smooth muscle
delay in stomach emptying
constipation
Form insoluble complex of aluminum phosphate (AlPO4),
which is excreted in the feces. May lead to lowered serum
phosphate concentrations and phosphorus mobilization
from the bone. If phosphate depletion is already present,
osteomalacia, osteoporosis, and fracture may result
BUT it reduce phosphates in the urine and prevent
formation of phosphatic (struvite) urinary stones
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Causes diarrhea:
1. Mg2+ draw water from the surrounding body tissues into
the intestinal tract by osmosis.
2. Higher quantity of water in the intestinal tract softens and
increases the volume of feces, stimulating nerves in the
intestines.
3. Mg2+ also play a role in releasing the peptide hormone
cholecystokinin, causing accumulation of water and
electrolytes in the intestine and triggering intestinal
motility.
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Magnesium salts may cause central nervous depression in
the presence of renal insufficiency
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Causes hypermagnesaemia in patients with severe renal
function impairment
BUT Magnesium hydroxide inhibits the precipitation of
calcium oxalate and calcium phosphate, thus preventing the
formation of calcium stones
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Release of CO2 cause belching, nausea, abdominal
distention, and flatulence.
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Calcium may induce rebound acid secretion.
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Calcium stone (kidney stone) can be formed.
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Excess Ca2+ cause hypercalcemia. Not a problem in normal
patients. But 3 - 4 g of CaCO3 per day can be problematic in
patients with uremia.
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Antacids may affect drugs by altering gastric and urinary
pH, (e.g., thyroid hormones)
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Al3+ and Mg2+ antacids are notable for their propensity to
chelate other drugs present in the GI tract, forming
insoluble complexes that pass through the GI tract without
absorption
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Most interactions can be avoided by taking antacids 2 hours
before or after ingestion of other drugs
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Require large neutralizing capacity
single dose (156 meq) antacid 1 hr after meal  neutralize
gastric acid for 2 hr
2nd dose 3 hr after eating  maintains effect for > 4 hr
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Tablet antacids generally weaker  large number
required
Very inconvenient to adminster
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Simethicone
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Anti-flatulence drug to ease discomfort
Breaking down gas bubbles in stomach by lowering
the surface tension
Alginates
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React with saliva to form a viscous raft of nonirritating material that floats atop stomach contents.
When reflux occurs, refluxate consists of nonirritant
materials
Cannot be used with simethicone!
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H2-Blockers
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Inhibit gastric acid secretion
Proton Pump Inhibitors – Omeprezole
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Best for short-term and long term treatment of
GERD
But take long to take effect (approx 1-4 days)
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Pictures:
http://www.specialtyminerals.com/specialtyapplications/specialty-markets-forminerals/pharmaceuticals/antacids/
NiDDK Image Library,
http://www.catalog.niddk.nih.gov/imagelibrary/det
ail.cfm?id=124