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1st Line Agents for GERD - Coggle Diagram
1st Line Agents for GERD
Omeprazole
PK/PD/PGx:
PK: bioavailability is 30-40% (absorption affected by food) Vd is 0.34-0.37 L/kg. Extensive first pass metabolism via CYP2C19. Renally excreted. No significant PD interactions. Onset of action takes ~1 hour. PGx testing not recommended
MOA
Irreversibly inhibits the H+,K+ATPase to suppress both basal stimulated gastric acid secretion to reduce irritation/damage in the stomach that is symptomatic of acid-peptic diseases like GERD
ADR's
:
Common (>10%) - respiratory system disorder
(1-10%) - skin rash, abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting, dizziness, headache, asthenia, back pain, cough, upper respiratory infection
Dosing Regimen
: 10mg PO QD; can increase to 20mg PO QD for 4-8 weeks if necessary. Discontinue once asymptomatic for 8 weeks.
Monitoring
Susceptibility testing is recommended in patients who fail H.pylori-eradication regimen; magnesium levels, s/s of cutaneous lupus erythematosus or systemic lupus erythematosus; C.difficile associated diarrhea; bone loss fractures
Duration
: trial up to 8 weeks for GERD, other indications may prescribe for longer
Warnings, Precautions, Contraindications
Contraindications: concomitant use of rilpivirine containing products; hypersensitivity to any component of the product or to substituted benzimidazoles
Warnings: bone loss and fractures, Vitamin B12 deficiency, CDAD, hypomagnesemia
Interactions
Omeprazole is a major CYP2C19 substrate and a minor 3A4/2C9 substrate so has interactions with inhibitors of these enzymes. Omeprazole increases gastric pH which causes a decreased in the bioavailability of acids and increase the bioavailability of bases.
Special pops
: avoid in elderly due to increased risk of osteoporosis fractures, hepatic impairment requires dose adjustment, use lowest possible dose in Asians
Education/counseling
: counsel pt to report diarrhea that does not improve, warn patients to report symptoms of hypomagnesemia, Swallow whole or sprinkle contents on a teaspoon of soft food and swallow mixture immediately (Do not store or chew)
SDOH
: Cheapest among all PPI and is on the Walmart's $4 list
Lansoprazole
PK/PD/PG
x: PGx testing not yet used/recommended. PK: >80% bioavailability (decreased when administered directly after eating) Vd is 0.61-0.9 L/kg in children and ~16L in adults. Metabolized mainly by CYP2C19/CYP3A4. Mainly excreted in feces. Does not have significant PD interactions. Onset of action takes 24+ hours
MOA
: irreversibly inhibits the H+/K+/ATPase pump in parietal cells of the stomach to prevent acidification of the stomach
ADR's
: common: GI upset, headache; severe/rare: CDAD, fractures, SJS/TEN, SLE
Dosing Regimen
: 15 mg daily for up to 8 weeks; other indications (ulcers, GI bleed) may allow for dosing up to 30 mg daily for up to 12 weeks
Monitoring
: baseline CBC, LFT's, BMP, CMP; monitor electrolytes and for serious ADR's periodically
Duration
: trial for up to 8 wks for GERD; may be longer for other indications
Warnings, Precautions
: CDAD, SLE, SJS/TEN, fractures, renal dysfunction, or electrolyte imbalances could occur. Dose-adjust with severe hepatic impairment.
Contraindications
: hypersensitivity to PPI's; concomitant use with rilpivirine.
Interactions
: lansoprazole is major CYP2C19 substrate, minor 2C9/3A4 substrate so has interactions with inhibitors of these enzymes. By increasing intragastric pH, lansoprazole can decrease bioavailability of weak acids and increase bioavailability of weak bases. Do not use lansoprazole with other meds that could increase fracture risk.
Special Pops
: avoid chronic use in geriatric patients due to osteoporosis/fracture risk. Considered safe (although 2nd line to nonpharm treatment) in pregnancy/lactation. Avoid use in pediatrics < 12 months of age.
Education/Counseling
: Take ~30 min before 1st meal of the day. Counsel on possible side effects. Tell patient to tell prescriber/pharmacist if taking this med so can watch out for drug interactions.
SDOH
: may be more expensive than other PPI's as an Rx medication (not on Walmart's $4 or $15 list) but can be bought generic OTC at Walmart for $14.97 per 42 caps