8/9/2019 13 Antacids and Controllers Upd
1/63
8/9/2019 13 Antacids and Controllers Upd
2/63
AcidAcid--Related PathophysiologyRelated PathophysiologyThe stomach secretes:The stomach secretes:
Hydrochloric acid (HCl)Hydrochloric acid (HCl)
BicarbonateBicarbonatePepsinogenPepsinogen
Intrinsic factorIntrinsic factor
MucusMucus
ProstaglandinsProstaglandins
8/9/2019 13 Antacids and Controllers Upd
3/63
Glands of the Stomach
Glands of the Stomach
CardiacCardiac
PyloricPyloric
Gastric*Gastric*
*The gastric glands are the largest in*The gastric glands are the largest innumbernumber
8/9/2019 13 Antacids and Controllers Upd
4/63
Cells of theG
astricG
landCells of theG
astricG
landParietalParietal
ChiefChief
MucoidMucoid
8/9/2019 13 Antacids and Controllers Upd
5/63
Cells of theG
astricG
landCells of theG
astricG
landParietal CellsParietal Cells
Produce and secrete HClProduce and secrete HCl
Primary site of action for many acidPrimary site of action for many acid--controller drugscontroller drugs
8/9/2019 13 Antacids and Controllers Upd
6/63
Cells of theG
astricG
landCells of theG
astricG
landChief CellsChief Cells
Secrete pepsinogen, a proenzymeSecrete pepsinogen, a proenzyme
Pepsinogen becomes PEPSIN whenPepsinogen becomes PEPSIN whenactivated by exposure to acidactivated by exposure to acid
Pepsin breaks down proteins (proteolytic)Pepsin breaks down proteins (proteolytic)
8/9/2019 13 Antacids and Controllers Upd
7/63
Cells of theG
astricG
landCells of theG
astricG
landMucoid CellsMucoid Cells
MucusMucus--secreting cells (surface epithelialsecreting cells (surface epithelialcells)cells)
Provide a protective mucous coatProvide a protective mucous coat
Protects against selfProtects against self--digestion by HCldigestion by HCl
8/9/2019 13 Antacids and Controllers Upd
8/63
Hydrochloric Acid
Hydrochloric Acid
Secreted by the parietal cellsSecreted by the parietal cells
Maintains stomach at a pH of 1 to 4Maintains stomach at a pH of 1 to 4
Secretion stimulated by:Secretion stimulated by:Large, fatty mealsLarge, fatty meals
Excessive amounts of alcoholExcessive amounts of alcohol
Emotional stressEmotional stress
8/9/2019 13 Antacids and Controllers Upd
9/63
8/9/2019 13 Antacids and Controllers Upd
10/63
8/9/2019 13 Antacids and Controllers Upd
11/63
8/9/2019 13 Antacids and Controllers Upd
12/63
AcidAcid--Related DiseasesRelated DiseasesCaused by imbalance of the threeCaused by imbalance of the threecells of the gastric gland and theircells of the gastric gland and their
secretionssecretionsMost common:Most common: HyperacidityHyperacidity
Most harmful:Most harmful: Peptic ulcer diseasePeptic ulcer disease(PUD)(PUD)
Lay terms for overproduction of HClLay terms for overproduction of HClby the parietal cells: indigestion,by the parietal cells: indigestion,sour stomach, heartburn, acidsour stomach, heartburn, acid
stomachstomach
8/9/2019 13 Antacids and Controllers Upd
13/63
Instructors may want to useInstructors may want to useEIC Image #123:EIC Image #123:
Parietal Cell Stimulation andParietal Cell Stimulation andSecretionSecretion
8/9/2019 13 Antacids and Controllers Upd
14/63
8/9/2019 13 Antacids and Controllers Upd
15/63
Antacids: Mechanism of ActionAntacids: Mechanism of ActionPromote the gastric mucosal defensePromote the gastric mucosal defense
mechanismsmechanisms
Secretion of:Secretion of:Mucus: Protective barrier against HClMucus: Protective barrier against HCl
Bicarbonate: Helps buffer acidicBicarbonate: Helps buffer acidicproperties of HClproperties of HCl
Prostaglandins: Prevent activation ofProstaglandins: Prevent activation ofproton pumpproton pump
8/9/2019 13 Antacids and Controllers Upd
16/63
Antacids: Mechanism of ActionAntacids: Mechanism of ActionAntacids DO NOT prevent theAntacids DO NOT prevent theoverproduction of acid.overproduction of acid.
Antacids DO neutralize the acid onceAntacids DO neutralize the acid onceits inits in the stomach.the stomach.
8/9/2019 13 Antacids and Controllers Upd
17/63
Antacids: Drug Effects Antacids: Drug EffectsReduction of pain associated withReduction of pain associated with
acidacid--related disordersrelated disorders
Raising gastric pH from 1.3 to 1.6
Raising gastric pH from 1.3 to 1.6neutralizes 50% of the gastric acid.neutralizes 50% of the gastric acid.
Raising gastric pH 1 point (1.3 to 2.3)Raising gastric pH 1 point (1.3 to 2.3)neutralizesneutralizes 90% of the gastric acid.90% of the gastric acid.
8/9/2019 13 Antacids and Controllers Upd
18/63
AntacidsAntacidsOTC formulations available as:OTC formulations available as:
Capsules and tabletsCapsules and tablets PowdersPowders
Chewable tabletsChewable tablets SuspensionsSuspensionsEffervescent granules and tabletsEffervescent granules and tablets
8/9/2019 13 Antacids and Controllers Upd
19/63
AntacidsAntacidsAluminum saltsAluminum salts
Magnesium saltsMagnesium salts
Calcium saltsCalcium saltsSodium bicarbonateSodium bicarbonate
Used alone or in combinationUsed alone or in combination
8/9/2019 13 Antacids and Controllers Upd
20/63
AntacidsAntacidsAluminum SaltsAluminum Salts
Forms: carbonate, hydroxide, phosphateForms: carbonate, hydroxide, phosphate
Have constipating effectsHave constipating effectsOften used with magnesium to counteractOften used with magnesium to counteractconstipationconstipation
Example: aluminum carbonate (Basaljel)Example: aluminum carbonate (Basaljel)
8/9/2019 13 Antacids and Controllers Upd
21/63
AntacidsAntacidsMagnesium SaltsMagnesium Salts
Forms: carbonate, hydroxide, oxide,Forms: carbonate, hydroxide, oxide,trisilicatetrisilicate
Commonly cause a laxative effectCommonly cause a laxative effect
Usually used with other agents toUsually used with other agents tocounteract this effectcounteract this effect
Dangerous when used with renal failureDangerous when used with renal failure
the failing kidney cannot excrete extrathe failing kidney cannot excrete extramagnesium, resulting in accumulationmagnesium, resulting in accumulation
Examples: magnesium hydroxide (MOM);Examples: magnesium hydroxide (MOM);combination products such as Maalox,combination products such as Maalox,
Mylanta (aluminum and magnesium)Mylanta (aluminum and magnesium)
8/9/2019 13 Antacids and Controllers Upd
22/63
AntacidsAntacidsCalcium SaltsCalcium Salts
Forms: many, but carbonate is mostForms: many, but carbonate is mostcommoncommon
May cause constipationMay cause constipation
Their use may result in kidney stonesTheir use may result in kidney stones
Long duration of acid action may causeLong duration of acid action may cause
increased gastric acid secretionincreased gastric acid secretion(hyperacidity rebound)(hyperacidity rebound)
Often advertised as an extra source ofOften advertised as an extra source ofdietary calciumdietary calcium
Exam le: Tums calcium carbonateExam le: Tums calcium carbonate
8/9/2019 13 Antacids and Controllers Upd
23/63
AntacidsAntacidsSodium BicarbonateSodium Bicarbonate
Highly solubleHighly soluble
Quick onset, but short durationQuick onset, but short durationMay cause metabolic alkalosisMay cause metabolic alkalosis
Sodium content may cause problems inSodium content may cause problems inpatients with CHF, hypertension, or renalpatients with CHF, hypertension, or renal
insufficiencyinsufficiency
8/9/2019 13 Antacids and Controllers Upd
24/63
Antacids and AntiflatulentsAntacids and AntiflatulentsAntiflatulents: used to relieve theAntiflatulents: used to relieve thepainful symptoms associated withpainful symptoms associated withgasgas
Several agents are used to bind orSeveral agents are used to bind oralter intestinal gas, and are oftenalter intestinal gas, and are oftenadded to antacid combinationadded to antacid combination
products.products.
8/9/2019 13 Antacids and Controllers Upd
25/63
Antacids and AntiflatulentsAntacids and AntiflatulentsOTC AntiflatulentsOTC Antiflatulents
activated charcoalactivated charcoal
simethiconesimethiconeAlters elasticity of mucusAlters elasticity of mucus--coatedcoated
bubbles, causing them to break.bubbles, causing them to break.
Used often, but there are limited data toUsed often, but there are limited data to
support effectiveness.support effectiveness.
8/9/2019 13 Antacids and Controllers Upd
26/63
Antacids: Side EffectsAntacids: Side EffectsMinimal, and depend on the compoundMinimal, and depend on the compound
usedused
Aluminum and calciumAluminum and calciumConstipationConstipation
MagnesiumMagnesium
DiarrheaDiarrhea
Calcium carbonateCalcium carbonate
Produces gas and belching; oftenProduces gas and belching; oftencombinedcombined with simethiconewith simethicone
8/9/2019 13 Antacids and Controllers Upd
27/63
Antacids: Drug InteractionsAntacids: Drug Interactions
ChelationChelation
Chemical binding, or inactivation, ofChemical binding, or inactivation, ofanother druganother drug
Chemical inactivationChemical inactivation
Produces insoluble complexesProduces insoluble complexes
Result: reduced drug absorptionResult: reduced drug absorption
8/9/2019 13 Antacids and Controllers Upd
28/63
Antacids: Drug InteractionsAntacids: Drug Interactions
Increased stomach pHIncreased stomach pH
Increased absorption of basic drugsIncreased absorption of basic drugs
Decreased absorption of acidic drugsDecreased absorption of acidic drugsIncreased urinary pHIncreased urinary pH
Increased excretion of acidic drugsIncreased excretion of acidic drugs
Decreased excretion of basic drugsDecreased excretion of basic drugs
8/9/2019 13 Antacids and Controllers Upd
29/63
Antacids: Nursing ImplicationsAntacids: Nursing Implications
Assess for allergies and preexistingAssess for allergies and preexistingconditions that may restrict the useconditions that may restrict the useof antacids, such as:of antacids, such as:
Fluid imbalancesFluid imbalances RenalRenaldiseasedisease CHFCHF
PregnancyPregnancy GI obstructionGI obstruction
Patients with CHF or hypertensionPatients with CHF or hypertensionshould use lowshould use low--sodium antacids suchsodium antacids suchas Riopan, Maalox, or Mylanta II.as Riopan, Maalox, or Mylanta II.
8/9/2019 13 Antacids and Controllers Upd
30/63
Antacids: Nursing ImplicationsAntacids: Nursing Implications
Use with caution with otherUse with caution with othermedications due to the many drugmedications due to the many druginteractions.interactions.
Most medications should be given 1Most medications should be given 1to 2 hours after giving an antacid.to 2 hours after giving an antacid.
Antacids may cause prematureAntacids may cause premature
dissolving of entericdissolving of enteric--coatedcoatedmedications, resulting in stomachmedications, resulting in stomachupset.upset.
8/9/2019 13 Antacids and Controllers Upd
31/63
Antacids: Nursing ImplicationsAntacids: Nursing Implications
Be sure that chewable tablets areBe sure that chewable tablets arechewed thoroughly, and liquid formschewed thoroughly, and liquid formsare shaken well before giving.are shaken well before giving.
Administer with at least 8 ounces ofAdminister with at least 8 ounces ofwater to enhance absorption (exceptwater to enhance absorption (exceptfor the rapid dissolve forms).for the rapid dissolve forms).
Caffeine, alcohol, harsh spices, andCaffeine, alcohol, harsh spices, andblack pepper may aggravate theblack pepper may aggravate theunderlying GI condition.underlying GI condition.
8/9/2019 13 Antacids and Controllers Upd
32/63
Antacids: Nursing ImplicationsAntacids: Nursing Implications
Monitor for side effects:Monitor for side effects:
Nausea, vomiting, abdominal pain,Nausea, vomiting, abdominal pain,diarrheadiarrhea
With calciumWith calcium--containing products:containing products:constipation, acid reboundconstipation, acid rebound
Monitor for therapeutic response:Monitor for therapeutic response:
Notify heath care provider if symptomsNotify heath care provider if symptomsare not relieved.are not relieved.
8/9/2019 13 Antacids and Controllers Upd
33/63
8/9/2019 13 Antacids and Controllers Upd
34/63
Histamine Type 2 (HHistamine Type 2 (H22))
AntagonistsAntagonists
8/9/2019 13 Antacids and Controllers Upd
35/63
HH22AntagonistsAntagonistsReduce acid secretionReduce acid secretion
All available OTCAll available OTC
Most popular drugs for treatment ofMost popular drugs for treatment ofacidacid--related disordersrelated disorders
cimetidine (Tagamet)cimetidine (Tagamet)
famotidine (Pepcid)famotidine (Pepcid)
nizatidine (Axid)nizatidine (Axid) ranitidine (Zantac)ranitidine (Zantac)
8/9/2019 13 Antacids and Controllers Upd
36/63
HH22Antagonists:Antagonists:
Mechanism of ActionMechanism of Action
Block histamine (HBlock histamine (H22) at the) at thereceptors of acidreceptors of acid--producingproducingparietal cellsparietal cells
Production of hydrogen ions isProduction of hydrogen ions isreduced, resulting in decreasedreduced, resulting in decreased
production of HClproduction of HCl
8/9/2019 13 Antacids and Controllers Upd
37/63
8/9/2019 13 Antacids and Controllers Upd
38/63
8/9/2019 13 Antacids and Controllers Upd
39/63
8/9/2019 13 Antacids and Controllers Upd
40/63
HH22 Antagonists: Therapeutic Antagonists: Therapeutic
UsesUses
Shown to be effective for:Shown to be effective for:
Gastric ulcerGastric ulcer Gastroesophageal refluxGastroesophageal refluxdisease (GERD)disease (GERD)
Upper GIUpper GI Duodenal ulcer (with orDuodenal ulcer (with orbleedingbleeding without H. pylori)without H. pylori)
May be effective for:May be effective for:
Stress ulcersStress ulcers Peptic esophagitisPeptic esophagitisPrevention and management of allergicPrevention and management of allergic
conditions, when used with Hconditions, when used with H11 blockersblockers
8/9/2019 13 Antacids and Controllers Upd
41/63
HH22 Antagonists: Side Effects Antagonists: Side EffectsOverall, less than 3% incidence ofOverall, less than 3% incidence ofside effectsside effects
Cimetidine may induce impotenceCimetidine may induce impotenceand gynecomastiaand gynecomastia
8/9/2019 13 Antacids and Controllers Upd
42/63
HH22 Antagonists: Drug Antagonists: Drug
InteractionsInteractionsCimetidineCimetidine
Binds with PBinds with P--450 microsomal oxidase450 microsomal oxidasesystem in the liver, resulting in inhibitedsystem in the liver, resulting in inhibited
oxidation of many drugs and increasedoxidation of many drugs and increaseddrug levelsdrug levels
All HAll H22 antagonists may inhibit theantagonists may inhibit theabsorption of drugs that require anabsorption of drugs that require anacidic GI environment for absorption.acidic GI environment for absorption.
8/9/2019 13 Antacids and Controllers Upd
43/63
HH22 Antagonists: Drug Antagonists: Drug
InteractionsInteractionsSMOKING has been shown toSMOKING has been shown todecrease thedecrease theeffectiveness of Heffectiveness of H
22
blockersblockers
8/9/2019 13 Antacids and Controllers Upd
44/63
HH22Antagonists: NursingAntagonists: Nursing
ImplicationsImplicationsAssess for allergies and impairedAssess for allergies and impairedrenal or liver function.renal or liver function.
Use with caution in patients who areUse with caution in patients who areconfused, disoriented, or elderly.confused, disoriented, or elderly.
Take 1 hour before or after antacids.Take 1 hour before or after antacids.
Ranitidine may be givenRanitidine may be givenintravenously; follow administrationintravenously; follow administrationguidelines.guidelines.
8/9/2019 13 Antacids and Controllers Upd
45/63
Proton Pump InhibitorsProton Pump Inhibitors
8/9/2019 13 Antacids and Controllers Upd
46/63
8/9/2019 13 Antacids and Controllers Upd
47/63
Proton Pump InhibitorsProton Pump Inhibitors
The parietal cells release positiveThe parietal cells release positivehydrogen ions (protons) during HClhydrogen ions (protons) during HClproduction.production.
This process is called the protonThis process is called the protonpump.pump.
HH22 blockers and antihistamines doblockers and antihistamines do
not stop the action of this pump.not stop the action of this pump.
8/9/2019 13 Antacids and Controllers Upd
48/63
Proton Pump Inhibitors:Proton Pump Inhibitors:
Mechanism of ActionMechanism of ActionIrreversibly bind to H+/K+Irreversibly bind to H+/K+ ATPaseATPase
enzyme.enzyme.
This bond prevents the movement of hydrogenThis bond prevents the movement of hydrogenions from the parietal cell into the stomach.ions from the parietal cell into the stomach.
Result:Result: AchlorhydriaAchlorhydriaALL gastric acidALL gastric acidsecretionsecretionis blocked.is blocked.
In order to return to normal acid secretion,In order to return to normal acid secretion,the parietal cell must synthesize new H+/K+the parietal cell must synthesize new H+/K+ATPaseATPase..
8/9/2019 13 Antacids and Controllers Upd
49/63
8/9/2019 13 Antacids and Controllers Upd
50/63
8/9/2019 13 Antacids and Controllers Upd
51/63
Proton Pump Inhibitors: DrugProton Pump Inhibitors: Drug
EffectEffect
Total inhibition of gastric acidTotal inhibition of gastric acidsecretionsecretionlansoprazole (Prevacid)lansoprazole (Prevacid) omeprazoleomeprazole
(Prilosec)(Prilosec)
rabeprazole (Aciphex)rabeprazole (Aciphex)pantoprazolepantoprazole(Protonix)(Protonix)
esomeprazole (Nexium)esomeprazole (Nexium)
8/9/2019 13 Antacids and Controllers Upd
52/63
Proton Pump Inhibitors:Proton Pump Inhibitors:
Therapeutic UsesTherapeutic Uses
GERD maintenance therapyGERD maintenance therapy
Erosive esophagitisErosive esophagitis
ShortShort--term treatment of activeterm treatment of activeduodenal and benign gastric ulcersduodenal and benign gastric ulcers
ZollingerZollinger--Ellison syndromeEllison syndrome
T
reatment of H. pyloriT
reatment of H. pylori--induced ulcersinduced ulcers
8/9/2019 13 Antacids and Controllers Upd
53/63
Proton Pump Inhibitors: SideProton Pump Inhibitors: Side
EffectsEffects
Safe for shortSafe for short--term therapyterm therapy
Incidence low and uncommonIncidence low and uncommon
8/9/2019 13 Antacids and Controllers Upd
54/63
Proton Pump Inhibitors:Proton Pump Inhibitors:
Nursing ImplicationsNursing Implications
Assess for allergies and history of liverAssess for allergies and history of liverdiseasedisease
PantoprazolePantoprazole is the only proton pumpis the only proton pumpinhibitor available forinhibitor available for parenteralparenteraladministration, and can be used foradministration, and can be used forpatients who are unable to take oralpatients who are unable to take oral
medicationsmedicationsMay increase serum levels of diazepam,May increase serum levels of diazepam,phenytoinphenytoin, and cause increased chance, and cause increased chancefor bleeding withfor bleeding with warfarinwarfarin
8/9/2019 13 Antacids and Controllers Upd
55/63
Proton Pump Inhibitors:Proton Pump Inhibitors:
Nursing ImplicationsNursing Implications
Instruct the patient takingInstruct the patient takingomeprazole:omeprazole:
It should be taken before meals.It should be taken before meals.
The capsule should be swallowed whole,The capsule should be swallowed whole,not crushed, opened or chewed.not crushed, opened or chewed.
It may be given with antacids.It may be given with antacids.
Emphasize that the treatment will beEmphasize that the treatment will beshortshort--term.term.
8/9/2019 13 Antacids and Controllers Upd
56/63
Other DrugsOther Drugs
sucralfate (Carafate)sucralfate (Carafate)
misoprostol (Cytotec)misoprostol (Cytotec)
8/9/2019 13 Antacids and Controllers Upd
57/63
Sucralfate (Carafate)Sucralfate (Carafate)
Cytoprotective agentCytoprotective agent
Used for stress ulcers, erosions, PUDUsed for stress ulcers, erosions, PUD
Attracted to and binds to the base ofAttracted to and binds to the base ofulcers and erosions, forming aulcers and erosions, forming aprotective barrier over these areasprotective barrier over these areas
Protects these areas from pepsin,Protects these areas from pepsin,which normally breaks down proteinswhich normally breaks down proteins(making ulcers worse)(making ulcers worse)
8/9/2019 13 Antacids and Controllers Upd
58/63
Sucralfate (Carafate)Sucralfate (Carafate)
Little absorption from the gutLittle absorption from the gut
May cause constipation, nausea, andMay cause constipation, nausea, anddry mouthdry mouth
May impair absorption of otherMay impair absorption of otherdrugs, especially tetracyclinedrugs, especially tetracycline
Binds with phosphate; may be usedBinds with phosphate; may be usedin chronic renal failure to reducein chronic renal failure to reducephosphate levelsphosphate levels
Do not administer with otherDo not administer with othermedicationsmedications
8/9/2019 13 Antacids and Controllers Upd
59/63
misoprostol (Cytotec)misoprostol (Cytotec)
Synthetic prostaglandin analogueSynthetic prostaglandin analogue
Prostaglandins have cytoprotectiveProstaglandins have cytoprotective
activity:activity:Protect gastric mucosa from injury byProtect gastric mucosa from injury byenhancing local production of mucus orenhancing local production of mucus orbicarbonatebicarbonate
Promote local cell regenerationPromote local cell regenerationHelp to maintain mucosal blood flowHelp to maintain mucosal blood flow
8/9/2019 13 Antacids and Controllers Upd
60/63
8/9/2019 13 Antacids and Controllers Upd
61/63
8/9/2019 13 Antacids and Controllers Upd
62/63
misoprostol (Cytotec)misoprostol (Cytotec)
Used for prevention of NSAIDUsed for prevention of NSAID--induced gastric ulcersinduced gastric ulcers
Doses that are therapeutic enough toDoses that are therapeutic enough totreat duodenal ulcers often producetreat duodenal ulcers often produceabdominal cramps, diarrheaabdominal cramps, diarrhea
8/9/2019 13 Antacids and Controllers Upd
63/63
THANK YOUTHANK YOU
WITHOUT FAITH , IT ISWITHOUT FAITH , IT IS
IMPOSSIBLE TO PLEASE GODIMPOSSIBLE TO PLEASE GOD
ROMEL Y. FELARCA,MD,DFM.