13 antacids and controllers upd

8/9/2019 13 Antacids and Controllers Upd

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AcidAcid--Related PathophysiologyRelated PathophysiologyThe stomach secretes:The stomach secretes:

Hydrochloric acid (HCl)Hydrochloric acid (HCl)

BicarbonateBicarbonatePepsinogenPepsinogen

Intrinsic factorIntrinsic factor

MucusMucus

ProstaglandinsProstaglandins


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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


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Cells of theG

astricG

landCells of theG

astricG

landParietalParietal

ChiefChief

MucoidMucoid


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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


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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)


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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


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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


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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


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Instructors may want to useInstructors may want to useEIC Image #123:EIC Image #123:

Parietal Cell Stimulation andParietal Cell Stimulation andSecretionSecretion


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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


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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.


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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.


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AntacidsAntacidsOTC formulations available as:OTC formulations available as:

Capsules and tabletsCapsules and tablets PowdersPowders

Chewable tabletsChewable tablets SuspensionsSuspensionsEffervescent granules and tabletsEffervescent granules and tablets


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AntacidsAntacidsAluminum saltsAluminum salts

Magnesium saltsMagnesium salts

Calcium saltsCalcium saltsSodium bicarbonateSodium bicarbonate

Used alone or in combinationUsed alone or in combination


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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)


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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)


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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


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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


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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.


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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.


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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


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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


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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


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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.


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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.


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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.


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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.


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Histamine Type 2 (HHistamine Type 2 (H22))

AntagonistsAntagonists


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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)


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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


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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


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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


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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.


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HH22 Antagonists: Drug Antagonists: Drug

InteractionsInteractionsSMOKING has been shown toSMOKING has been shown todecrease thedecrease theeffectiveness of Heffectiveness of H

22

blockersblockers


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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.


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Proton Pump InhibitorsProton Pump Inhibitors


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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.


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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..


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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)


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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


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Proton Pump Inhibitors: SideProton Pump Inhibitors: Side

EffectsEffects

Safe for shortSafe for short--term therapyterm therapy

Incidence low and uncommonIncidence low and uncommon


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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


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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.


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Other DrugsOther Drugs

sucralfate (Carafate)sucralfate (Carafate)

misoprostol (Cytotec)misoprostol (Cytotec)


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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)


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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


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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


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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


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THANK YOUTHANK YOU

WITHOUT FAITH , IT ISWITHOUT FAITH , IT IS

IMPOSSIBLE TO PLEASE GODIMPOSSIBLE TO PLEASE GOD

ROMEL Y. FELARCA,MD,DFM.

13 antacids and controllers upd

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