I I I I I
➢ Antacids: weak bases that react with hydrochloric acid to form salt & water.
I I I I I I I I I I I I
o Used in the treatment of Hyperacidity, GERD, PUD, hyperphosphatemia, and calcium deficiency
I I I I I I I I I I I
o Contain combinations of
I I
▪ metallic Ication I(aluminum, Icalcium, Imagnesium, Iand Isodium)
▪ and Ibasic Ianion I(hydroxide, Ibicarbonate, Icarbonate, Icitrate, Iand Itrisilicate)
➢ Pharmacodynamics, IPharmacokinetics, IPharmacotherapeutics
o Neutralize IGastric IAcidity I(causes I^pH Iof Ithe Istomach Iand Iduodenal Ibulb)
o Inhibit Iproteolytic Iactivity Iof Ipepsin
o Increase Ilower Iesophageal Isphincter Itone
o Acid-neutralizing Icapacity IANC Ivaries Ibetween Iproducts Iexpressed Iin ImEqs
o If Iingested Iin Ia Ifasting Istate, Iantacids Ireduce Iacidity Ifor Iapproximately I20 Ito I40 Iminutes
o If Itaken I1 Ihr Iafter Ia Imeal, Iacidity Iis Ireduced Ifor I2 Ito I3 Ihrs
o A Isecond Idose Itaken Iafter Ia Imeal Imaintains Ireduced Iacidity Ifor Imore Ithan I4 Ihrs Iafter Ithe Imeal
o The Iaction Iof Iantacids Ioccurs Ilocally Iin Ithe IGI Itract Iwith Iminimal Iabsorption, Iminimal Imetabolism
o ALL Iantacids Iare Icontraindicated Iin Ithe Ipresence Iof Isevere Iabdominal Ipain Iof Iunknown Icause, Iespecially Iif
Iaccompanied Iby Ifever
-HIGH ISODIUM Icontent: Ipts Iw/ IHTN, ICHF, Imarked Irenal Ifailure, Ior Ion Ilow-sodium Idiets Ineed Ito Iuse Ilow Isodium
Ipreparation
-Concurrent Iadministration Iwith Ienteric-coated Idrugs, Idestroys Ithe Icoating= Ialters Iabsorption, I^ Ithe Irisk Ifor
Iadverse Ieffects
-Administrations Ishould Ibe Iseparated Iby Iat Ileast I2 Ihours Ito Idecrease Idrug/drug Iinteractions
1. Calcium Ibased Iantacids: ITUMS, ICaltrate, ICalcarb
• Prescribed Ito Itreat Icalcium Ideficient Istates, Ii.e. Ichronic Irenal Ifailure, Ipost-menopause, Iand Iosteoporosis
• Used Ito Ibind Iphosphates Iin ICRF
• Require IVitamin ID Ifor Iabsorption Ifrom Ithe IGI Itract
• Excreted Imainly Iin Ifeces, I20% Iin Iurine
• ADR: IContraindicated Iin Ithe Ipresence Iof Ihypercalcemia Iand Irenal Icalculi
• Can Icause Iconstipation- Iincrease Ibulk, Ifluids Iand Imobility, Istool Isoftener
• Administered I30min- I1hr Ion Iempty Istomach Ior I3hr Iafter Imeals
• Should Inot Ibe Iadministered Iwith Ifood Icontaining Ilarge Iamounts Iof Ioxalic Iacid I(spinach, Irhubarb), Ior
Iphytic Iacid I(bran, Icereals), Ithey Idecrease Ithe Iabsorption Iof Icalcium
• Taking Iw/ Ifoods Icontaining Iphosphorus I(milk, Idairy) Ican Ilead Ito Imilk-alkali Isyndrome I(N/V, Iconfusion,
Iheadache).
• Taking Iwith Iacidic Ifruit Ijuice Iimprove Iabsorption
2. Aluminum Ibased: IAlternaGEL, IAmphojel, IMylanta
• Inhibit Ismooth Imuscle Icontraction Iand Islow Igastric Iemptying
• Used Ito Ibind Iphosphates Iin ICRF
Aluminum Iis Inot Ieasily
removed Iby Idialysis • Not Iabsorbable Iwith Iroutine Iuse
Ib/cIit Iis Ibound Ito • Aluminum Iconcentrated Iin Ithe ICNS
Ialbumin I& Itransferrin
I= Ido Inot Icross Idialysis • Bind Iwith Iphosphate Iand Iexcreted Iin Ifeces
Imembrane
• Prolonged Iuse Iin Ipatients Iwith Irenal Ifailure Imay Iresult Iin Idialysis Iosteomalacia
o Aluminum Ideposits Iin Ibone Iand Iosteomalacia Ioccurs
• Elevated Ialuminum Itissue Ilevels Icontribute Ito Ithe Idevelopment Iof Idialysis Iencephalopathy
• Used Ito Itreat Ihyperphosphatemia Iin Ipts Iw/ Irenal Ifailure I& Iphosphate Irenal Istone Iprevention
• Can Icause Iconstipation- Iincrease Ibulk, Ifluids Iand Imobility, Istool Isoftener
3. Magnesium Ibased: IMilk Iof Imag, IMaalox, IMylanta
, • Can Ibe Iused Ito Itreat Imagnesium Ideficiencies Ifrom Imalnutrition, Ialcoholism, Ior Imag-depleting Idrugs
The Imalfunctioning • Contraindicated Iin Ipatients Iwith Irenal Ifailure I& Iused Iwith Icaution Iin Ipts Iwith Irenal Iinsufficiency
Ikidney Icannot
Iexcrete • Not Iabsorbable Iwith Iroutine Iuse
Imagnesium=
• Excreted Iin Ithe Iurine
Ihypermagnesemia
• Contraindicated Iin Ipatients Iwith Irenal Ifailure, Iuse Iwith Icaution Ifor Ipatients Iwith Iany Idegree Iof Irenal
Iinsufficiency
o Malfunctioning Ikidney Iis Iunable Ito Iexcrete Imagnesium Iand Ihypermagnesemia Imay Iresult
• Can Icause Idiarrhea- Iincrease Ifiber Iintake I (Alkalosis Imay Ioccur Iin Irenal Iimpairment)
Clinical IUse Iand IDosing
,➢ Rational Idrug Iselection
o ANC, Isodium Icontent, Iand Icost
o Combination Iproducts Iwith Ialuminum Ihydroxide Iand Imagnesium Ihydroxide Ihave Ithe Ihighest IANC I(use Iis
Imoderate Ito Isevere Idisease
➢ Monitoring
o Serum Iphosphate, Ipotassium, Iand Icalcium Iduring Ichronic Iuse
o These Idrugs Imay Icause Iincreased Iserum Icalcium Iand Idecreased Iserum Iphosphate
o Chronic Imagnesium Ihydroxide Iuse Imay Icause Ielevated IMg Ilevels Iin Ipatients Iwith Irenal Ifailure Ior Ithe Ielderly
Iwith Idecreased Irenal Ifunction
➢ Patient Ieducation
o Take Ias Iprescribed, Iespecially Irelated Ito Imealtimes
o Take I1-3 Ihrs Iafter Imeals Iand Iat Ibedtime
o Chewable Itablets Ichew Ithoroughly Iand Idrink Ihalf Ia Iglass Iof Iwater
o Shake Isuspensions Ibefore Iadministration
o Many Idrug Iinteractions, Iseparate Idoses Iby I2 Ihours Iapart
o Calcium Ibased Iantacids Ishould Inot Ibe Iadminister Iwith Ifood Icontaining Ilarge Iamounts Iof Ioxalic Iacid I(spinach,
Irhubarb) Ior Iphytic Iacid I(brans, Icereals) Idecrease Iabsorption
o Avoid Itaking Iwith Ifood Icontaining Iphosphorus I(milk, Idairy Iproducts) Ican Icause Imilk-alkali Isyndrome I(NV,
Iconfusion, IHA)
o Consult Iprovider: Ibefore Itaking Iantacids Ifor Imore Ithan I2 Iweeks Iif Ia Iproblem Irecurs, Iif Irelief Iis Inot Iobtained,
Ior Iif Isymptoms Iof IGI Ibleeding I(black, Itarry Istools, Icoffee Iground Iemesis
o Aluminum Iand Icalcium Iantacids Imay Icause Iconstipation: Iincrease Ibulk, Iincrease Ifluid Iintake, Iand Imore
Imobility, Istool Isoftened
o Magnesium Iantacids Imay Icause Idiarrhea, Iincrease Ifiber
o Avoid Ismoking, Iavoid Iflat Ilying Ibody Iposition Iwhile Isleeping, Ifoods Ithat Iirritate Ithe Igastric Imucosa I(spicy
Ifoods), Ior Istimulate Iacid Iproduction I(alcohol) Iand Ifoods Ithat Idecrease Ilower Iesophageal Isphincter Itone
I(caffeine, Ichocolate, Ifatty Ifoods)
, ➢ Antidiarrheals:
• Diarrhea Ithat Ilasts Ifor Iless Ithan I2 Iweeks Iis Iconsidered Iacute; Iif Iit Ilasts Imore Ithan I2 Iweeks, Iit Iis Iconsidered Ichronic.
• Pharmacodynamics, IPharmacokinetics
• Three Imain Iclasses Iabsorbent Ipreparations I(kaolin Iand Ipectin I(Kapectolin) Iand Ibismuth Isubsalicylate I(Pepto-
IBismol, IKaopectate ILiquid), Iopiates I(diphenoxylate Iwith Iatropine I(Lomotil), Idiphenoxin Iwith Iatropine I(Motofen),
Iand Iloperamide I(Imodium)) Iand Ianticholinergics I(IBD)
• Contraindications: IDrugs Ithat Idecrease Igastric Imotility Ior Idelay Iintestinal Itransit Itime Ihave Iinduced Itoxic
Imegacolon, Iespecially Iin Ithose Iwith Iinflammatory Ibowel Idisease
• All Iantidiarrheals I(except ICrofelemer) Irequire Icautious Iuse Iin Iolder Iadults Iand Iwhen Ithere Iis Ir/f Iimpaction
• Older Iadults Iare Iespecially Isensitive Ito Idiphenoxylate Ior Idifenoxin Ir/t Iatropine Iand Ianticholinergic Iproperties
• Not Irecommended Ifor Ichildren Iunder I12, Inone Iof Ithe Iantidiarrheals Iare Isafe Ifor Ichildren Iunder I2 Iyears Iold
• Antidiarrheals Iare Icontraindicated Iin Ithe ITx Iof Idiarrhea Iin Imost Ichildren
• Standard Iof Icare: Ioral Irehydration Itherapy
• ADRS IRebound Iconstipation Iis Ithe Imain Iadverse Ieffect
-Kaolin-pectin I(kapectolin): IAcute Idiarrhea
• Kaolin Iis Ia Iclay-like Ipowder Ithat Iattracts Iand Iholds Ionto Ibacteria
• Pectin Ithickens Ithe Istool Iby Iabsorbing Imoisture
• Used Ito Itreat Isimple Idiarrhea
• Act Ilocally Iin Ithe Ibowel, Inot Isystemically Iabsorbed
• Pregnancy ICategory IB
-Bismuth Isubsalicylate I(Pepto Ibismol): IAcute Idiarrhea, Itravelers’ Idiarrhea
▪ Antisecretory Iand Iantimicrobial Ieffects
▪ Also Iused Ias Ipart Iof Ia Imultidrug Iregimen Ifor IH. Ipylori
▪ Undergoes Ichemical Idissociation Iin IGI, Isalicylate Imoiety Iis Iabsorbed
▪ Salicylate Iis Imetabolized Iin Ithe Iliver Iand Imore Ithan I90% Iis Iexcreted Iin Iurine
▪ Contraindicated Iin Ichildren Ior Iteenagers Iduring Ior Iafter Irecovery Ifrom Ichickenpox Ior Iflu-like Iillness
▪ Contraindicated Ifor Ipatients Iwith IASA Ihypersensitivity
▪ For Ibismuth Isubsalicylate, Iadditional Ireactions Ithat Iall Ipatients Ishould Ibe Iwarned Iabout Iare Igray/black
Istools Iand Iblack Itongue, Ithe Iresults Iof Ithe Ibismuth. IPatients Ishould Ibe Itold Ito Iexpect Ithis Ireaction Iand
Ithat Iit Idoes Inot Iindicate IGI Ibleeding.
▪ Bismuth Isubsalicylate Imay Ipotentiate Ithe Irisk Ifor Itoxicity Iif Itaken Iw/ Iaspirin
▪ R/f Ihypoglycemia Iin Ilarge Idoses Iwith Iinsulin Ior Ioral Ihypoglycemics
-Crofelemer I(fulyzaq): ISymptomatic Irelief Iof Inoninfectious Idiarrhea Iin Iadult Ipts Iw/ IHIV/AIDS Ion Iantiretroviral Itherapy
▪ Botanical Iblocking Ichloride Isecretion Ifrom Ithe Iepithelial Icells Iin Ithe Iintestinal Ilumen, Idecreasing Iwater Iloss
Iand Inormalizing Ithe Iflow Iof Ichloride Iand Iwater Iin Ithe Iintestinal Itract
▪ Minimal Iabsorption Iafter IPO Iadministration
▪ Metabolism Iand Iexcretion Iare Inot Iknown
▪ In Iclinical Itrials Imore Ilikely Ito Ihave IURI, Ibronchitis, Iand Icough Ithan Iplacebo Igroup
▪ Adverse IGI Ieffects Iflatulence, Iincreased Ibilirubin, Iand Inausea
-diphenoxylate Iw/atropine I(Lomotil): IAcute Idiarrhea
▪ Constipating Imeperidine Icongener, Ilacks Ianalgesic Iactivity
▪ At Ihigh Idoses Ican Iproduce Ieuphoria Iand Iphysical Idependence
▪ Anticholinergics Iare Iuseful Ionly Iwith Iinflammatory Ibowel Idisease
▪ Well Iabsorbed Ifrom IGI Itract