Acid Reducers :
H2 – Antagonist, Proton Pump Inhibitors and Antac
:Prepared by
Pharmacist: Hawraz Jawdat Jaafar
Email: Hawrazjawdat@[Link]
: H2 Receptor Antagonist
H2 antagonists, also called H2 blockers, are a class
of medications that block the action of histamine at
the histamine H2 receptors of the parietal cells in
the stomach. This decreases the production of stomach
.acid
H2 antagonists are a type of antihistamine, although in
common use the term "antihistamine" is often reserved
.for H1 antagonists. Like the H1 antagonists
H2 antagonists can be used in the treatment of dyspepsia,
but have been surpassed by the more effective proton
pump inhibitors. They are also used to treat peptic ulcer
. disease and gastroesophageal reflux disease ( GERD)
Note : H2 blockers are a different class of drugs to 'antihistamine drugs' which block
.H1 receptors in cells that are involved in allergy reactions
: H2 Receptor Blockers
Cimetidine ( Tagamet) -
Ranitidine ( Zantac) -
Famotidine (Pepcid , Pepcid AC) -
Nizatidine ( Axid) -
These products have been approved for the relief of
“heartburn associated with acid indigestion, and sour
stomach.” They should not be taken for longer than 2 weeks
.and are not recommended for children < 12 years of age
What conditions are they used to
?treat
To reduce acid reflux which may cause heartburn or -
inflammation of the gullet (esophagitis). These conditions are
.sometimes called gastro-esophageal reflux disease (GERD)
To treat ulcers in the stomach and in part of the gut (the -
.duodenum)
To help heal ulcers associated with anti-inflammatory -
medication called non-steroidal anti-inflammatory drugs
.(NSAIDs)
In other conditions where it is helpful to reduce acid in the - -
.stomach
: Also
Damage to the stomach and/or intestines due to stress or -
trauma
Hives -
Pancreatic problems -
Stomach or intestinal ulcers (sores) resulting from damage -
Mechanism of action of H2
: blockers
The H2 antagonists are competitive antagonists of histamine at parietal cell H2
. receptor
They suppress the normal secretion of acid by parietal cells and the meal –
. stimulated secretion of acid
They accomplish this by two mechanism : Histamine released by ECL
(enterochromaffin – like) cells in the stomach is blocked from binding on parietal
cell H2 receptor , which stimulate acid secretion : therefore other substances
that promote acid secretion ( such as gastrin and acetylcholine ) have a reduce
. effect on parietal cell when the H2 receptors are blocked
Some Side Effects of H2 Receptor
: Blockers
Some of the side effects that may occur with H2 receptor blockers
:include
constipation -
diarrhea -
difficulty sleeping -
dry mouth-
dry skin-
headaches-
ringing in the ears-
a runny nose-
trouble urinating-
Proton Pump Inhibitors
: ( PPI)
Proton pump inhibitors (PPIs) reduce the production of
acid by blocking the secretion in the wall of the stomach
that produces acid. Acid is necessary for the formation
of most ulcers in the esophagus, stomach, and
duodenum, and the reduction of acid with PPIs prevents
ulcers and allows any ulcers that exist in the esophagus,
.stomach, and duodenum to heal
? How do PPIs Work
Your stomach normally produces acid to help with the digestion of food
and to kill germs (bacteria). This acid is corrosive so your body
produces a natural mucous barrier which protects the lining of the
.stomach from being worn away (eroded)
In some people this barrier may have broken down allowing the acid to
damage the stomach, causing an ulcer. In others there may be a
problem with the muscular band at the top of the stomach (the
sphincter) that keeps the stomach tightly closed. This may allow the
acid to escape and irritate the gullet (esophagus). This is called 'acid
reflux' which can cause heartburn and/or inflammation of the gullet
.(esophagitis)
Available Proton Pump Inhibitors
:
Omeprazole - Generic Name Brand Name
dexlansopraz
Lanzoprazole - ole
Dexilant
Pantoprazole - esomeprazole Nexium
Esomeprazole - lansoprazole Prevacid
Rabeprazole - Prilosec,
omeprazole
Dexlansoprazole - Zegerid
pantoprazole Protonix
rabeprazole Aciphex
Proton pump inhibitors are approved for the treatment of frequent
heartburn in adults (≥ 18 years of age) with symptoms of heartburn 2 or
more days per week. These products are not intended for immediate relief
of heartburn, as they may take 1–4 days for full effect. They should not be
taken for more than 14 days or more often than every 4 months unless
directed by a physician. Omeprazole magnesium 20.6 mg is equivalent to
20 mg of omeprazole
(prescription strength).
: Medical uses of PPI
Dyspepsia-
Peptic Ulcer-
As part of Helicobacter Pylori eradication therapy-
Gastroesophageal reflux disease ( GERD)-
Barrett’s esophagus-
Eosinophilic esophagitis-
Mechanism of action of
: PPI
Proton pump inhibitors act by irreversibly blocking
the hydrogen/potassium adenosine triphosphates enzyme system
(the H+/K+ATPase, or, more commonly, the gastric proton pump) of the
gastric parietal cells.[41] The proton pump is the terminal stage in gastric
acid secretion, being directly responsible for secreting H+ ions into the
.gastric lumen, making it an ideal target for inhibiting acid secretion
Targeting the terminal step in acid production, as well as
the irreversible nature of the inhibition, results in a class of drugs that are
significantly more effective than H2 antagonists and reduce gastric acid
.secretion by up to 99%
Decreasing the acid in the stomach can aid the healing of duodenal ulcers
and reduce the pain from indigestion and heartburn. Stomach acids are
needed however to digest proteins, vitamin B12, calcium, and other
.nutrients. Too little stomach acid causes the condition hypochlorhydria
The PPIs are given in an inactive form, which is neutrally charged (lipophilic)
and readily crosses cell membranes into intracellular compartments (like
the parietal cell canaliculus) with acidic environments. In an acid
environment, the inactive drug is protonated and rearranges into its active
form. As described above, the active form will covalently and irreversibly
.bind to the gastric proton pump, deactivating it
Shortly Mechanism of
action
Block the last step in the secretion of gastric
acid by combining with hydrogen , potassium ,
and adenosine triphosphate in the parietal
. cells of the stomach
: Adverse Effects
Common adverse effects : Headache – nausea
– diarrhea – abdominal pain – fatigue –
. dizziness
Infrequent adverse effect include : itch – rash –
flatulence – constipation – anxiety – depression
.
: Antacid
Antacids are agents that neutralize the gastric acid and raise
the gastric pH, so are used to treat dyspepsia and are used as
symptomatic relief of peptic ulcer. Antacids in common use
salts of magnesium, aluminum and calcium. Some mixtures
contain sodium and should be used with caution in patients
who should avoid excess sodium intake. Alginates are
sometimes combined with antacids for use in
gastroesophageal reflux disease. Alginates float on top of the
gastric contents and act as a barrier between the acidic
contents of the stomach and the lower esophageal sphincter,
preventing erosion of the lower esophagus and therefore not
creating the pain experienced in gastroesophageal reflux
.disease
Possible side effects of
: antacids
Diarrhea
Constipation
Flatulence
Stomach cramps
Feeling sick or vomiting
Most antacids contain one or more of the
: following ingredients
Aluminum hydroxide -
Calcium carbonate -
Magnesium trisilicate -
Sodium Bicarbonate -
Bismuth subsalicylate -
GERD Treatments – Medications
?
Proton Pump Inhibitors : If you have GERD, the odds are you’ll be
prescribed one of these. This class of drugs -- which includes
Aciphex, Nexium, Prevacid, Prilosec, and Protonix -- is now the
standard GERD treatment. Not only do they help block the production
of acid in the stomach, they also protect the esophagus from damage
.and allow it to heal
H2 Blockers : These come as prescription and OTC medicines. They
include drugs like Axid, Pepcid, Tagamet, and Zantac and were once
the standard treatment for GERD. But they’re not used as often now.
.But H2 blockers just aren’t as powerful as the proton pump inhibitors
Antacids : The old standbys from your grandparents’ medicine
cabinet -- tablets like Tums and Rolaids and liquids like Maalox and
Mylanta -- can still play a role in controlling GERD. These heartburn
remedies aren’t suited for regular, long-term use. But their main
advantage is that they work quickly, unlike more powerful GERD
.medications
