Drug Monograph

Famotidine

Pepcid (Rx); Pepcid AC, Zantac 360 (OTC)
H2-Receptor Antagonist·Oral & Injectable
Pharmacokinetic Profile
Half-Life
2.5–3.5 h
Metabolism
Minimal hepatic; weak CYP1A2 inhibitor; 65–70% excreted unchanged in urine
Protein Binding
15–22%
Tmax
2–4 h (oral)
Vd
1.0–1.3 L/kg
Clinical Information
Drug Class
H2-Receptor Antagonist
Available Doses
Rx: 20 mg, 40 mg tablets; oral suspension; injection. OTC: 10 mg, 20 mg
Route
Oral, IV
Renal Adjustment
Yes — CrCl <60 mL/min (see dosing)
Hepatic Adjustment
None required
Pregnancy
Insufficient human data; no adverse effects in animal studies at 243× MRHD
Lactation
Limited data; no effects on breastfed infant; weigh benefits vs risks
Schedule
Rx (20 mg, 40 mg) and OTC (10 mg, 20 mg)
Generic Available
Yes
Rx

Indications

IndicationApproved PopulationTherapy TypeStatus
Active duodenal ulcerAdults and paediatric patients ≥40 kgMonotherapyFDA Approved
Active gastric ulcerAdults and paediatric patients ≥40 kgMonotherapyFDA Approved
Symptomatic nonerosive GERDAdults and paediatric patients ≥40 kgMonotherapyFDA Approved
Erosive esophagitis due to GERD (diagnosed by biopsy)Adults and paediatric patients ≥40 kgMonotherapyFDA Approved
Pathological hypersecretory conditions (e.g., Zollinger-Ellison syndrome, multiple endocrine neoplasias)Adults onlyMonotherapyFDA Approved
Reduction of the risk of duodenal ulcer recurrenceAdults onlyMonotherapyFDA Approved

Famotidine is a competitive inhibitor of histamine H2-receptors on parietal cells. It reduces both basal and stimulated gastric acid secretion by blocking histamine binding. The 20 mg and 40 mg tablet formulations are not recommended in paediatric patients weighing less than 40 kg because the lowest available tablet strength exceeds the recommended dose for these patients; another famotidine formulation (e.g., oral suspension) should be used instead.

Off-Label Uses

Stress ulcer prophylaxis — Evidence quality: Moderate. Famotidine is used in critically ill patients for stress-related mucosal injury prevention, although PPIs have become more commonly used in this setting.

Refractory chronic urticaria — Evidence quality: Moderate. H2-receptor antagonists including famotidine are used as adjunctive therapy with H1-antihistamines for chronic urticaria that does not respond to H1-blockers alone.

Dose

Dosing

Adult and Paediatric (≥40 kg) Dosing — Normal Renal Function

IndicationRecommended DoseDurationNotes
Active duodenal ulcer40 mg once daily or 20 mg twice dailyUp to 8 weeksMost patients heal within 4 weeks; if not healed, continue 2–4 additional weeks
Active gastric ulcer40 mg once dailyUp to 8 weeks
Symptomatic nonerosive GERD20 mg twice dailyUp to 6 weeks
Erosive esophagitis due to GERD20 mg twice daily or 40 mg twice dailyUp to 12 weeksBoth regimens effective per clinical trials
Pathological hypersecretory conditions (adults only)20 mg every 6 hoursAs clinically indicatedAdjust to individual patient needs; maximum 160 mg every 6 hours
DU recurrence risk reduction (adults only)20 mg once daily1 yearLonger durations not studied

Renal Impairment Dosing

IndicationCrCl 30–60 mL/minCrCl <30 mL/min
Active DU20 mg QD or 40 mg QOD20 mg QOD
Alt: 10 mg QD (use alternate formulation)
Active GU20 mg QD or 40 mg QOD20 mg QOD
Alt: 10 mg QD (use alternate formulation)
Symptomatic nonerosive GERD20 mg QD20 mg QOD
Alt: 10 mg QD (use alternate formulation)
Erosive esophagitis (from 20 mg BID regimen)20 mg QD20 mg QOD
Alt: 10 mg QD (use alternate formulation)
Erosive esophagitis (from 40 mg BID regimen)40 mg QD20 mg QD
Pathological hypersecretory conditionsAvoid useAvoid use
DU recurrence risk reduction20 mg QOD10 mg QOD
Use alternate formulation for 10 mg dose
Clinical Pearl: Administration

Take once daily before bedtime or twice daily in the morning and before bedtime. May be taken with or without food, and may be given concurrently with antacids. The antisecretory effect lasts approximately 10–12 hours. No hepatic dose adjustment is required — liver cirrhosis does not significantly affect famotidine disposition unless severe renal insufficiency coexists.

PK

Pharmacology

Mechanism of Action

Famotidine is a competitive inhibitor of histamine H2-receptors on gastric parietal cells. By blocking the action of histamine at these receptors, famotidine inhibits both basal and stimulated gastric acid secretion, reducing both the acid concentration and volume of gastric secretion. Changes in pepsin secretion are proportional to volume output. Unlike proton pump inhibitors, which irreversibly block the H+/K+-ATPase proton pump, famotidine acts upstream by blocking one of the three stimulatory pathways (histamine, acetylcholine, and gastrin) that converge on the parietal cell. This results in a less complete but faster-onset acid suppression compared to PPIs, with clinical effects evident within 1 hour of oral administration.

ADME Profile

ParameterValueClinical Implication
AbsorptionOral bioavailability 40–50% (incomplete absorption); Tmax 2–4 h; onset of antisecretory action within 1 h; dose-independent absorption (5–40 mg range); food does not significantly affect bioavailability; potent antacids may reduce absorption by 20–30%Can be taken with or without food; faster onset than PPIs; can co-administer with antacids per PI (despite modest absorption reduction)
DistributionProtein binding 15–22% (low); Vd 1.0–1.3 L/kgLow protein binding means famotidine is readily removed by haemodialysis; moderate tissue distribution
MetabolismMinimal first-pass hepatic metabolism; weak CYP1A2 inhibitor; minimal interference with hepatic cytochrome P450 system; no clinically significant effects on CYP2D6, CYP3A4, or other CYP isoformsVery low drug interaction potential compared to cimetidine; no hepatic dose adjustment required; liver cirrhosis does not alter disposition unless severe renal impairment coexists
Eliminationt½ 2.5–3.5 h; 65–70% excreted unchanged in urine; renal clearance ~15 L/h (exceeds GFR, indicating tubular secretion); eliminated by haemodialysis; t½ can exceed 20 h in severe renal impairment (CrCl <10 mL/min); antisecretory effect duration ~10–12 hPredominantly renal elimination necessitates dose reduction in moderate-severe renal impairment; CNS adverse reactions and QT prolongation risk increase with renal impairment due to drug accumulation
SE

Side Effects

In clinical trials of approximately 2,500 patients (1,442 treated with famotidine), the overall adverse reaction incidence in the famotidine 40 mg at bedtime group was similar to placebo. The population ranged from 17 to 91 years of age.

≥1%Common (Reported in ≥1% of Famotidine-Treated Patients)
Adverse EffectFrequencyClinical Note
Headache≥1%Most commonly reported; incidence similar to placebo
Dizziness≥1%Incidence similar to placebo
Constipation≥1%Incidence similar to placebo
Diarrhoea≥1%Listed in highlights; incidence similar to placebo
<1%Uncommon (Reported in <1% of Famotidine-Treated Patients)
SystemAdverse Effects
Body as a WholeFever, asthenia, fatigue
CardiovascularPalpitations
GastrointestinalElevated liver enzymes, vomiting, nausea, abdominal discomfort, anorexia, dry mouth
HaematologicThrombocytopenia
HypersensitivityOrbital oedema, rash, conjunctival injection, bronchospasm
MusculoskeletalMusculoskeletal pain, arthralgia
Nervous System / PsychiatricSeizure, hallucinations, depression, anxiety, decreased libido, insomnia, somnolence
SkinPruritus, dry skin, flushing
Special SensesTinnitus, taste disorder
OtherImpotence
SeriousSerious Post-Marketing Adverse Reactions
Adverse EffectSystemRequired Action
Arrhythmia, AV block, prolonged QT intervalCardiovascularECG monitoring; higher risk in renal impairment if dose/interval not adjusted
Cholestatic jaundice, hepatitisGastrointestinalMonitor LFTs; discontinue if hepatotoxicity suspected
Agranulocytosis, pancytopenia, leukopeniaHaematologicCBC monitoring; discontinue if blood dyscrasia occurs
Anaphylaxis, angioedema, facial oedema, urticariaHypersensitivityImmediate discontinuation; emergency care
Rhabdomyolysis, muscle crampsMusculoskeletalCheck CK; discontinue if rhabdomyolysis confirmed
Confusion, agitation, paresthesiaNervous SystemReduce dose or discontinue; higher risk in elderly and renal impairment
Interstitial pneumoniaRespiratoryDiscontinue; pulmonary workup
Toxic epidermal necrolysis / Stevens-Johnson syndromeSkinImmediate discontinuation; emergency care
CNS Adverse Reactions — FDA Warning

Confusion, delirium, hallucinations, disorientation, agitation, seizures, and lethargy have been reported in elderly patients and patients with moderate and severe renal impairment. Famotidine blood levels are higher in these patients. Use the lowest effective dose and monitor renal function.

Int

Drug Interactions

Famotidine has a much lower drug interaction potential than cimetidine. Unlike cimetidine, famotidine does not significantly inhibit hepatic cytochrome P450 enzymes (except for weak CYP1A2 inhibition). The primary interaction mechanism is pH-dependent absorption changes for co-administered drugs.

MajorDasatinib
MechanismIncreased gastric pH reduces dasatinib absorption
EffectSignificantly reduced dasatinib exposure; loss of efficacy
ManagementConcomitant use not recommended
FDA PI
MajorDelavirdine
MechanismIncreased gastric pH reduces delavirdine absorption
EffectReduced delavirdine concentrations; risk of HIV treatment failure
ManagementConcomitant use not recommended
FDA PI
MajorCefditoren / Fosamprenavir
MechanismIncreased gastric pH reduces absorption
EffectReduced drug exposure; loss of efficacy
ManagementConcomitant use not recommended
FDA PI
ModerateTizanidine
MechanismFamotidine is a weak CYP1A2 inhibitor; tizanidine is a CYP1A2 substrate
EffectPotentially substantial increases in tizanidine concentrations
ManagementAvoid concomitant use; if necessary, monitor for hypotension, bradycardia, or excessive drowsiness
FDA PI
ModerateOther pH-dependent drugs (atazanavir, ketoconazole, itraconazole, erlotinib, nilotinib, ledipasvir/sofosbuvir, rilpivirine)
MechanismIncreased gastric pH reduces absorption
EffectReduced systemic exposure of the co-administered drug
ManagementSee individual drug prescribing information for staggered dosing or avoidance instructions
FDA PI
Clinical Pearl: Minimal CYP Interaction Profile

Unlike cimetidine, which is a potent inhibitor of multiple CYP enzymes (1A2, 2C9, 2D6, 3A4), famotidine has a much cleaner interaction profile. Its only CYP effect is weak CYP1A2 inhibition, which is clinically relevant primarily for tizanidine. This makes famotidine the preferred H2-receptor antagonist when drug interactions are a concern.

Mon

Monitoring

  • Renal FunctionBaseline and periodically
    Routine
    Assess CrCl at baseline to determine dosing. Monitor periodically in elderly and in patients with known or suspected renal impairment. Half-life can exceed 20 hours when CrCl <10 mL/min.
  • CNS StatusOngoing in at-risk patients
    Trigger-based
    Monitor elderly patients and those with renal impairment for confusion, delirium, hallucinations, disorientation, agitation, seizures, or lethargy. Consider dose reduction if CNS effects develop.
  • Symptom Response4–8 weeks
    Routine
    Assess healing at end of treatment course. Symptomatic response does not preclude gastric malignancy — consider endoscopy or further evaluation if suboptimal response or early relapse, especially in adults.
  • CBCIf symptoms develop
    Trigger-based
    Post-marketing reports of agranulocytosis, pancytopenia, and leukopenia. Monitor if unexplained fever, infection, or bleeding occur.
  • QT IntervalIf renal impairment present
    Trigger-based
    Prolonged QT interval reported in patients with renal impairment whose dose or dosing interval was not adjusted appropriately. ECG monitoring may be warranted.
CI

Contraindications & Cautions

Absolute Contraindications

  • History of serious hypersensitivity reactions (e.g., anaphylaxis) to famotidine or other H2-receptor antagonists

Use with Caution

  • Moderate-severe renal impairment (CrCl <60 mL/min) — dose reduction required; increased risk of CNS adverse reactions and QT prolongation due to drug accumulation
  • Elderly patients — use lowest effective dose; monitor renal function; higher risk of CNS adverse reactions
  • Pathological hypersecretory conditions with renal impairment — avoid use in patients with CrCl <60 mL/min; doses required may exceed those evaluated in renally impaired patients
  • Pregnancy — insufficient human data; use only if clearly needed. Animal studies showed no adverse effects at up to 243× the MRHD in rats and 122× in rabbits
  • Lactation — limited data on presence in human milk; no effects on breastfed infant reported; weigh benefits of breastfeeding against clinical need
  • Paediatric patients <40 kg — use alternate formulation (e.g., oral suspension); 20 mg and 40 mg tablets exceed recommended doses in these patients
FDA Warning CNS Adverse Reactions in Elderly and Renally Impaired Patients

Confusion, delirium, hallucinations, disorientation, agitation, seizures, and lethargy have been reported in elderly patients and patients with moderate and severe renal impairment treated with famotidine. Since famotidine blood levels are higher in patients with renal impairment, dosage adjustments are recommended.

Pt

Patient Counselling

Purpose of Therapy

Famotidine is an acid-reducing medication that blocks histamine receptors in the stomach. It is used to treat and prevent ulcers in the stomach and duodenum, relieve heartburn and GERD symptoms, and help heal damage to the oesophagus caused by acid reflux.

How to Take

Take famotidine once daily at bedtime or twice daily in the morning and at bedtime. It can be taken with or without food and may be given alongside antacids. Shake the liquid suspension vigorously for 5–10 seconds before each dose. Most ulcers heal within 4 weeks but may take up to 8 weeks. Complete the full prescribed course even if symptoms improve.

Mental Status Changes
Tell patientIn rare cases, famotidine may cause confusion, hallucinations, or unusual drowsiness, particularly in elderly patients or those with kidney problems.
Call prescriberImmediately if confusion, hallucinations, agitation, or seizures develop.
Kidney Function
Tell patientPatients with kidney disease may require a lower dose. Always inform healthcare providers about kidney problems before starting famotidine.
Call prescriberIf urine output decreases or ankle swelling develops.
OTC Use Limits
Tell patientOTC famotidine should not be used for more than 14 consecutive days for heartburn unless directed by a doctor. Do not exceed 2 tablets (40 mg) per day for OTC use.
Call prescriberIf heartburn symptoms persist beyond 2 weeks of OTC use, or if difficulty swallowing, bloody vomit, or black stools occur.
Allergic Reactions
Tell patientSerious allergic reactions are rare but can occur.
Call prescriberSeek immediate emergency care for hives, difficulty breathing, or swelling of face, lips, tongue, or throat.
Ref

Sources

Regulatory (PI / SmPC)
  1. Famotidine tablets prescribing information. Aurobindo Pharma Limited. Revised 4/2022. dailymed.nlm.nih.govCurrent FDA-approved PI — primary source for indications, dosing Tables 1 and 2, adverse reactions, drug interactions, and renal impairment recommendations.
  2. PEPCID (famotidine) tablets prescribing information. Merck Sharp & Dohme. 2018. accessdata.fda.govBrand-name PEPCID PI including clinical trial data, paediatric dosing guidance, and pharmacodynamics.
  3. Famotidine injection prescribing information. Sagent Pharmaceuticals. Revised 2025. accessdata.fda.govInjectable formulation PI with IV-specific dosing, benzyl alcohol neonatal warning, and CNS adverse reaction warnings.
Key Clinical Trials
  1. Gitlin N, McCullough AJ, Smith JL, et al. A multicenter, double-blind, randomized, placebo-controlled comparison of nocturnal and twice-a-day famotidine in the treatment of active duodenal ulcer disease. Gastroenterology. 1987;92(1):48–53.Pivotal DU healing trial: 70% healed at week 4, 83% at week 8 with famotidine 40 mg QHS vs 45% placebo.
  2. McCullough AJ, Graham DY, Knuff TE, et al. Suppression of nocturnal acid secretion with famotidine accelerates gastric ulcer healing. Gastroenterology. 1989;97(4):860–866.GU healing trial demonstrating famotidine 40 mg QHS efficacy for gastric ulcer.
Guidelines
  1. Katz PO, Dunbar KB, Schnoll-Sussman FH, et al. ACG Clinical Guideline for the Diagnosis and Management of Gastroesophageal Reflux Disease. Am J Gastroenterol. 2022;117(1):27–56. doi:10.14309/ajg.0000000000001538Current GERD guideline positioning H2RAs as step-down therapy or for nocturnal acid breakthrough when combined with PPIs.
  2. Lanza FL, Chan FK, Quigley EM, et al. Guidelines for prevention of NSAID-related ulcer complications. Am J Gastroenterol. 2009;104(3):728–738. doi:10.1038/ajg.2009.115ACG guideline noting famotidine reduces NSAID-related duodenal but not gastric ulcers; PPIs preferred for gastroprotection.
Mechanistic / Basic Science
  1. Feldman M, Burton ME. Histamine2-receptor antagonists: standard therapy for acid-peptic diseases (first of two parts). N Engl J Med. 1990;323(24):1672–1680. doi:10.1056/NEJM199012133232405Comprehensive NEJM review of H2RA pharmacology including famotidine’s relative potency vs cimetidine and ranitidine.
  2. Langtry HD, Grant SM, Goa KL. Famotidine: an updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in peptic ulcer disease and other allied diseases. Drugs. 1989;38(4):551–590. doi:10.2165/00003495-198938040-00004Major therapeutic review of famotidine covering clinical pharmacology, efficacy, and tolerability.
Pharmacokinetics / Special Populations
  1. Echizen H, Ishizaki T. Clinical pharmacokinetics of famotidine. Clin Pharmacokinet. 1991;21(3):178–194. doi:10.2165/00003088-199121030-00003Key PK review: t½ 2–4 h, bioavailability 40–50%, protein binding 15–22%, Vd 1.0–1.3 L/kg, renal clearance 15 L/h, 70% eliminated unchanged; reduced clearance in renal impairment and elderly.
  2. Lin JH, Chremos AN, Yeh KC, et al. Effects of age, gender, and race on the pharmacokinetics of famotidine. Br J Clin Pharmacol. 1989;27(S1):55S–59S.Population PK study showing famotidine clearance correlates with CrCl; age-related pharmacokinetic changes driven by renal function decline.
  3. Famotidine. In: StatPearls [Internet]. Treasure Island, FL: StatPearls Publishing; Updated September 2025. ncbi.nlm.nih.govComprehensive evidence-based review of famotidine pharmacology, indications, dosing, and monitoring recommendations.