Monday, 19 September 2016

Amoxicillin and Clavulanate Potassium



Class: Aminopenicillins
VA Class: AM052
Chemical Name: [2R - (2α,3Z,5α)] - 3 - (2 - Hydroxyethylidene) - 7 - oxo - 4 - oxa - 1 - azabicyclo[3.2.0]heptane - 2 - carboxylic acid monopotassium salt mixt. with [2S - [2α,5α,6β(S*)]] - 6 - [[Amino(4 - hydroxyphenylacetyl]amino] - 3,3 - dimethyl - 7 - oxo - 4 - thia - 1 - azabicyclo[3.2.0] heptane-2-carboxylic acid trihydrate
Molecular Formula: C16H19N3O5S•3H2O C8H8KNO5
CAS Number: 74469-00-4
Brands: Augmentin

Introduction

Antibacterial; β-lactam antibiotic; fixed combination containing amoxicillin (an aminopenicillin) and clavulanate potassium (a β-lactamase inhibitor).1


Uses for Amoxicillin and Clavulanate Potassium


Otitis Media


Treatment of acute otitis media (AOM) caused by β-lactamase producing H. influenzae or M. catarrhalis.1 3 67 74 77 78 81 82 88 89 92 93 94 95 96 98 99 101 115 AAP, AAFP, CDC, and others recommend fixed combination of amoxicillin and clavulanate (instead of amoxicillin) for initial treatment of AOM in those with severe illness (moderate to severe otalgia or fever ≥39°C)115 or when the infection is suspected of being caused by β-lactamase-producing Haemophilus influenzae or Moraxella catarrhalis.74 76 77 78 81 89 115


Treatment of persistent or recurrent AOM caused by H. influenzae (including β-lactamase-producing strains), M. catarrhalis (including β-lactamase-producing strains), or Streptococcus pneumoniae (penicillin MIC ≤2 mcg/mL) in pediatric patients.76 79 81 89 90 91 97 115 Drug of choice for retreatment of AOM that has not responded to other anti-infectives81 89 90 100 107 115 (e.g., no response to amoxicillin within 48–72 hours).115 Not indicated for AOM caused by S. pneumoniae with penicillin MIC ≥4 mcg/mL.3


Has been used for management of otitis media with effusion (OME).68 94 102 107 Anti-infectives not usually recommended;102 103 104 105 107 116 they provide only limited benefit in enhancing resolution of effusion and may promote resistance.103 104 105 106 107 AAP, AAFP, and others recommend watchful waiting for 3 months from date of effusion onset or diagnosis in those 2 months to 12 years of age who are not at risk for speech, language, or learning problems; some suggest a short course of anti-infectives may be considered for possible short-term benefits when parent and/or caregiver expresses a strong aversion to impending surgery.116 If anti-infectives are used for treatment, amoxicillin and clavulanate or amoxicillin recommended.102 107


Pharyngitis and Tonsillitis


Treatment of symptomatic patients who have multiple, recurrent episodes of pharyngitis known to be caused by S. pyogenes (group A β-hemolytic streptococci).75 76 80


Not a drug of choice for treatment of streptococcal pharyngitis and tonsillitis,75 76 80 but one of several possible alternatives recommended by AAP, IDSA , and AHA when multiple episodes occur and the patient fails to respond to drugs of choice (oral penicillin V, IM penicillin G benzathine, oral amoxicillin).75 76 80


Consider that multiple, recurrent episodes of symptomatic pharyngitis occurring within several months to years may indicate that the patient is a streptococcal carrier experiencing repeated episodes of nonstreptococcal (e.g., viral) pharyngitis;75 80 treatment not usually recommended for streptococcal pharyngeal carriers.75 76 80


Respiratory Tract Infections


Treatment of acute sinusitis and lower respiratory tract infections caused by susceptible H. influenzae1 2 5 17 53 67 68 69 or M. catarrhalis.1 2 5 17 53 59


Treatment of acute sinusitis or community-acquired pneumonia (CAP) caused by or suspected to be caused by β-lactamase-producing pathogens (i.e., H. influenzae, M. catarrhalis, H. parainfluenzae, Klebsiella pneumoniae, oxacillin-susceptible Staphylococcus aureus).4 9


Treatment of acute sinusitis or CAP caused by or suspected of being caused by S. pneumoniae with reduced penicillin susceptibility (i.e., penicillin MIC 2 mcg/mL).4 9 18 Not indicated for treatment of infections caused by S. pneumoniae with penicillin MIC ≥4 mcg/mL.4


Recommended by IDSA and ATS as an alternative for outpatient empiric treatment of CAP in immunocompetent adults;9 18 ATS recommends use with a macrolide or doxycycline in those with cardiopulmonary disease and/or other factors that increase risk for multidrug-resistant S. pneumoniae or gram-negative bacteria.18


Skin and Skin Structure Infections


Treatment of skin or skin structure infections (e.g., abscesses, cellulitis, impetigo) caused by β-lactamase-producing S. aureus, Escherichia coli, or Klebsiella.1 2 5 33 42


Urinary Tract Infections (UTIs)


Treatment of UTIs caused by β-lactamase-producing E. coli, Klebsiella, or Enterobacter.1 2 5 14 17 27 28 32 41 43 44 45 47 49 51 53 111


Useful for outpatient treatment of recurrent UTIs or UTIs acquired in hospitals or nursing homes likely to be caused by drug-resistant S. aureus, Enterococcus, or gram-negative bacilli.111 In severe gram-negative infections, consider concomitant use of an aminoglycoside (amikacin, gentamicin, tobramycin).111


Active Tuberculosis


Alternative recommended by ATS and others for use in multiple-drug regimens for treatment of active tuberculosis in patients with multidrug-resistant Mycobacterium tuberculosis.20 31 66


Bite Wounds


Empiric treatment of animal or human bites.109 112 Active against most likely bite pathogens, including anaerobes, Staphylococcus, Eikenella corrodens, Pasteurella multocida.108 110 112


Alternative for treatment of infections caused by P. multocida or E. corrodens.111


Pelvic Inflammatory Disease


Treatment of acute pelvic inflammatory disease (PID).36 46 52 64


Not a drug of choice for PID.36 According to CDC, may be effective when used in conjunction with doxycycline, but GI adverse effects may limit compliance.36


Amoxicillin and Clavulanate Potassium Dosage and Administration


Administration


Oral Administration


The various film-coated, scored, and chewable tablets and the oral suspension containing 125, 200, 250, or 400 mg of amoxicillin/5 mL may be administered without regard to meals.1 However, administration with meals results in optimal absorption of clavulanate potassium and may minimize adverse GI effects.1 2 17 37 41 48 53


Extended-release tablets containing 1 g of amoxicillin4 and the oral suspension containing 600 mg of amoxicillin/5 mL3 should be administered at the start of a meal to enhance absorption and minimize adverse GI effects.


Chewable tablets should be thoroughly chewed before swallowing.


In adults who have difficulty swallowing tablets, the oral suspension containing 125 or 250 mg of amoxicillin/5 mL may be substituted for 500-mg film-coated tablets or the oral suspension containing 200 or 400 mg of amoxicillin/5 mL may be substituted for 875-mg scored tablets.1


When 500-mg film-coated tablets are indicated, do not substitute 250-mg film-coated tablets and do not substitute chewable tablets.2


When extended-release tablets containing 1 g of amoxicillin are indicated, do not substitute film-coated, scored, or chewable tablets.4


Reconstitution

Reconstitute oral suspension at the time of dispensing.1 3 Tap bottle to thoroughly loosen powder and then add the amount of water specified on the bottle in 2 portions; agitate vigorously after each addition.1 3


Agitate suspension well prior to administration of each dose.1 3


Dosage


Available as fixed combination containing amoxicillin and clavulanate potassium;1 2 3 4 dosage expressed in terms of amoxicillin.1 2 3 4


Not all preparations of amoxicillin and clavulanate are interchangeable since they contain different amounts of clavulanic acid.1 3


Powders for oral suspension contain a 4:1, 7:1, or 14:1 ratio of amoxicillin to clavulanic acid;1 3 chewable tablets contain a 4:1 or 7:1 ratio of the drugs;1 film-coated tablets contain a 2:1 or 4:1 ratio of the drugs;2 scored tablets contain a 7:1 ratio of the drugs;1 and extended-release tablets contain a 16:1 ratio of the drugs.4


Pediatric Patients


Children weighing <40 kg should not receive film-coated tablets containing 250 mg of amoxicillin since this preparation contains a high dose of clavulanic acid.1


The oral suspension containing 125 mg of amoxicillin/5 mL is the only preparation recommended for use in neonates and infants <12 weeks (3 months) of age.1


Acute Otitis Media (AOM)

AOM in Neonates and Infants <12 Weeks (3 Months) of Age

Oral

Oral suspension: Manufacturer recommends 30 mg/kg daily given in divided doses every 12 hours for 10 days using the oral suspension containing 125 mg/5 mL.1


AOM in Children ≥12 Weeks of Age Weighing <40 kg

Oral

Oral suspension: Manufacturer recommends 45 mg/kg daily given in divided doses every 12 hours for 10 days using the suspension containing 200 or 400 mg/5 mL; alternatively, 40 mg/kg daily given in divided doses every 8 hours using the suspension containing 125 or 250 mg/5 mL.1


Chewable tablets: Manufacturer recommends 45 mg/kg daily given in divided doses every 12 hours for 10 days using the chewable tablets containing 200 or 400 mg; alternatively, 40 mg/kg daily given in divided doses every 8 hours using chewable tablets containing 125 or 250 mg.1


AOM in Children Weighing ≥40 kg

Oral

Film-coated tablets: Manufacturer recommends one 250-mg tablet every 8 hours or one 500-mg tablet every 12 hours for 10 days.1 2


Oral suspension: Manufacturer recommends 500 mg every 12 hours for 10 days using the suspension containing 125 or 250 mg/5 mL.1


AOM with Severe Illness or When β-Lactamase-producing Strains are Suspected

Oral

90 mg/kg daily given in divided doses every 12 hours recommended by AAP and AAFP.115


Usual duration is 10 days; optimal duration is uncertain.115 AAP and AAFP recommend 10 days in those <6 years of age and in those with severe disease and state 5–7 days may be appropriate in those ≥6 years of age with mild to moderate AOM.115


AOM that Failed to Respond to Amoxicillin

Oral

90 mg/kg daily given in divided doses every 12 hours recommended by AAP and AAFP.115


Usual duration is 10 days; optimal duration is uncertain.115 AAP and AAFP recommend 10 days in those <6 years of age and in those with severe disease and state 5–7 days may be appropriate in those ≥6 years of age with mild to moderate AOM.115


Persistent or Recurrent AOM

Infections in Children ≥3 Months of Age Weighing <40 kg

Oral

Oral suspension: Manufacturer recommends 90 mg/kg daily given in divided doses every 12 hours for 10 days using the suspension containing 600 mg/5 mL.3





















Pediatric Dosage of Oral Suspension Containing 600 mg/5 mL (Augmentin ES-600) for Persistent or Recurrent AOM1

Weight (kg)



Volume of Suspension to Provide 90 mg/kg daily



8



3 mL twice daily



12



4.5 mL twice daily



16



6 mL twice daily



20



7.5 mL twice daily



24



9 mL twice daily



28



10.5 mL twice daily



32



12 mL twice daily



36



13.5 mL twice daily


Pharyngitis and Tonsillitis

Oral

40 mg/kg daily (up to 750 mg daily) in 3 divided doses for 10 days for treatment of multiple, recurrent episodes of pharyngitis known to be caused by S. pyogenes.80


Respiratory Tract Infections

Infections in Neonates and Infants <12 weeks (3 months) of Age

Oral

Oral suspension: 30 mg/kg daily given in divided doses every 12 hours using the suspension containing 125 mg/5 mL.1


Infections in Children ≥12 Weeks of Age Weighing <40 kg

Oral

Oral suspension: 45 mg/kg daily given in divided doses every 12 hours using the suspension containing 200 or 400 mg/5 mL; alternatively, 40 mg/kg daily given in divided doses every 8 hours using the suspension containing 125 or 250 mg/5 mL.1


Chewable tablets: 45 mg/kg daily given in divided doses every 12 hours using chewable tablets containing 200 or 400 mg; alternatively, 40 mg/kg daily given in divided doses every 8 hours using chewable tablets containing 125 or 250 mg.1


Infections in Children Weighing ≥40 kg

Oral

Film-coated or scored tablets: One 500-mg tablet every 8 hours or one 875-mg tablet every 12 hours.1


Oral suspension: 500 mg every 8 hours using the suspension containing 125 or 250 mg/5 mL1 2 or 875 mg every 12 hours using the suspension containing 200 or 400 mg/5 mL.1 2


Skin and Skin Structure Infections

Infections in Neonates and Infants <12 Weeks (3 Months) of Age

Oral

Oral suspension: 30 mg/kg daily in divided doses every 12 hours using the suspension containing 125 mg/5 mL.1


Infections in Children ≥12 Weeks of Age Weighing <40 kg

Oral

Oral suspension: 25 mg/kg daily in divided doses every 12 hours using the suspension containing 200 or 400 mg/5 mL; alternatively, 20 mg/kg daily in divided doses every 8 hours using the suspension containing 125 or 250 mg/5 mL.1 For severe infections, 45 mg/kg daily in divided doses every 12 hours using the suspension containing 200 or 400 mg/5 mL; alternatively, 40 mg/kg daily in divided doses every 8 hours using the suspension containing 125 or 250 mg/5 mL.1


Chewable tablets: 25 mg/kg daily in divided doses every 12 hours using chewable tablets containing 200 or 400 mg.1 For severe infections, 45 mg/kg daily given in divided doses every 12 hours using chewable tablets containing 200 or 400 mg.1


Infections in Children Weighing ≥40 kg

Oral

Film-coated or scored tablets: One 250-mg tablet every 8 hours or one 500-mg tablet every 12 hours.1 2 For severe infections, one 500-mg tablet every 8 hours or one 875-mg tablet every 12 hours.1


Oral suspension: 500 mg every 12 hours using the suspension containing 125 or 250 mg/5 mL.1


Urinary Tract Infections (UTIs)

Infections in Neonates and Infants <12 Weeks (3 Months) of Age

Oral

Oral suspension: 30 mg/kg daily in divided doses every 12 hours using the suspension containing 125 mg/5 mL.1


Infections in Children ≥12 Weeks of Age Weighing <40 kg

Oral

Oral suspension: 25 mg/kg daily in divided doses every 12 hours using the suspension containing 200 or 400 mg/5 mL; alternatively, 20 mg/kg daily in divided doses every 8 hours using the suspension containing 125 or 250 mg/5 mL.1 For severe infections, 45 mg/kg daily in divided doses every 12 hours using the suspension containing 200 or 400 mg/5 mL; alternatively, 40 mg/kg daily in divided doses every 8 hours using the suspension containing 125 or 250 mg/5 mL.1


Chewable tablets: 25 mg/kg daily in divided doses every 12 hours using chewable tablets containing 200 or 400 mg.1 For severe infections, 45 mg/kg daily given in divided doses every 12 hours using chewable tablets containing 200 or 400 mg.1


Infections in Children Weighing ≥40 kg

Oral

Film-coated or scored tablets: One 250-mg tablet every 8 hours or one 500-mg tablet every 12 hours.1 2 For severe infections, one 500-mg tablet every 8 hours or one 875-mg tablet every 12 hours.1


Oral suspension: 500 mg every 12 hours using the suspension containing 125 or 250 mg/5 mL.1


Adults


Respiratory Tract Infections

Oral

Scored tablets: one 875-mg-tablet every 12 hours.2


Oral suspension: 875 mg every 12 hours using the suspension containing 200 or 400 mg/5 mL.1


Community-acquired Pneumonia

Oral

Extended-release tablets: Two 1-g tablets every 12 hours for 7–10 days.4


Sinusitis

Oral

Extended-release tablets: Two 1-g tablets every 12 hours for 10 days.4


Acute Otitis Media (AOM)

Oral

Film-coated tablets: One 500-mg tablet every 12 hours or one 250-mg tablet every 8 hours.2 For severe infections, one 875-mg tablet every 12 hours or one 500-mg tablet every 8 hours.2


Oral suspension: 500 mg every 12 hours using the suspension containing 125 or 250 mg/5 mL.1 For severe infections, 875 mg every 12 hours using the suspension containing 200 or 400 mg/5 mL.1


Pharyngitis and Tonsillitis

Oral

500 mg twice daily for 10 days for treatment of multiple, recurrent episodes of pharyngitis known to be caused by S. pyogenes.80 Adult dosage was extrapolated from pediatric dosage and has not been evaluated in clinical studies.80


Skin and Skin Structure Infections

Oral

Film-coated or scored tablets: One 500-mg tablet every 12 hours or one 250-mg tablet every 8 hours.2 For severe infections, one 875 mg-tablet every 12 hours or one 500-mg tablet every 8 hours.2


Oral suspension: 500 mg every 12 hours using the suspension containing 125 or 250 mg/5 mL.1 For severe infections, 875 mg every 12 hours using the suspension containing 200 or 400 mg/5 mL.1


Urinary Tract Infections (UTIs)

Oral

Film-coated or scored tablets: One 500-mg tablet every 12 hours or one 250-mg tablet every 8 hours.2 For severe infections, one 875-mg tablet every 12 hours or one 500-mg tablet every 8 hours.2


Oral suspension: 500 mg every 12 hours using the suspension containing 125 or 250 mg/5 mL.1 For severe infections, 875 mg every 12 hours using the suspension containing 200 or 400 mg/5 mL.1


Special Populations


Hepatic Impairment


Select dosage with caution and monitor hepatic function.1 2 3 4 (See Hepatic Effects under Cautions.)


Renal Impairment


Dosage adjustment necessary in patients with moderate to severe renal impairment.2 5 17 63 65


Do not use scored tablets containing 875 mg of amoxicillin in those with severe renal impairment and GFR <30 mL/minute.2


Do not use extended-release tablets containing 1 g of amoxicillin in those with Clcr <30 mL/minute or in hemodialysis patients.4











Dosage of Film-coated Tablets for Adults with Renal Impairment2

GFR (mL/min)



Daily Dosage



10–30



250 or 500 mg every 12 hours depending on infection severity



<10



250 or 500 mg every 24 hours depending on infection severity



Hemodialysis Patients



250 or 500 mg every 24 hours depending on infection severity; with an additional dose both during and at the end of dialysis


Geriatric Patients


No dosage adjustments except those related to renal impairment.4 (See Renal Impairment under Dosage and Administration.)


Cautions for Amoxicillin and Clavulanate Potassium


Contraindications



  • Known hypersensitivity to any penicillin.1 2 3 4




  • Previous history of amoxicillin and clavulanate-associated cholestatic jaundice or hepatic dysfunction.1 2 3 4




  • Use of extended-release tablets containing 1 g of amoxicillin in those with Clcr <30 mL/minute or in hemodialysis patients.4



Warnings/Precautions


Warnings


Superinfection/Clostridium difficile-associated Colitis

Possible emergence and overgrowth of nonsusceptible bacteria or fungi.1 2 3 4 Discontinue and institute appropriate therapy if superinfection occurs.1 2 3 4


Treatment with anti-infectives may permit overgrowth of clostridia.1 Consider Clostridium difficile-associated diarrhea and colitis (antibiotic-associated pseudomembranous colitis) if diarrhea develops and manage accordingly.1 2 3 4 83 84 85 86 87


Some mild cases of C. difficile-associated diarrhea and colitis may respond to discontinuance alone.1 2 3 4 83 84 85 86 87 Manage moderate to severe cases with fluid, electrolyte, and protein supplementation; appropriate anti-infective therapy (e.g., oral metronidazole or vancomycin) recommended if colitis is severe.1 2 3 4 83 84 85 86 87


Hepatic Effects

Rare reports of hepatic dysfunction (e.g., increases in serum AST, ALT, bilirubin, and/or alkaline phosphatase), especially in geriatric patients, males, or with prolonged therapy.1 2 3 4


Hepatic dysfunction may occur during or several weeks following discontinuance of therapy.1 2 3 4


Hepatic dysfunction may be severe, but usually is reversible.1 2 3 4 Histologic findings indicate predominantly cholestatic, hepatocellular, or mixed cholestatic-hepatocellular changes.1 2 3 4


Fatalities has been reported rarely,1 2 3 4 71 most frequently in those with serious underlying diseases or concomitant drug therapy.1 2 3 4


Assess hepatic function periodically during prolonged therapy.1 2 3 4


Use with caution if there is evidence of hepatic dysfunction.1 2 3 4


Sensitivity Reactions


Hypersensitivity Reactions

Serious and occasionally fatal hypersensitivity reactions reported with penicillins.1 2 3 4


Prior to initiation of therapy, make careful inquiry regarding previous hypersensitivity reactions to penicillins, cephalosporins, or other drugs.1 2 3 4 Partial cross-allergenicity occurs among penicillins and other β-lactam antibiotics including cephalosporins and cephamycins.1 2 3 4


If hypersensitivity reaction occurs, discontinue immediately and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, maintenance of an adequate airway and oxygen).1 2 3 4


General Precautions


Renal Effects

Acute interstitial nephritis and hematuria reported rarely.1 2 3 4


Assess renal function periodically during prolonged therapy.1 2 3 4


Hematologic Effects

Adverse hematologic effects (e.g., anemia, hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia, thrombocytopenic purpura) reported with penicillins.1 2 3 4 Usually reversible when drug discontinued; may be a hypersensitivity reaction.1 2 3 4


Assess hematologic function periodically during prolonged therapy.1 2 3 4


Mononucleosis

Possible increased risk of erythematous rash in patients with mononucleosis; use in these patients not recommended.1 2 3 4 22 23


Phenylketonuria

Chewable tablets containing 200 or 400 mg of amoxicillin contain aspartame (NutraSweet), which is metabolized in the GI tract to provide 2.1 or 4.2 mg of phenylalanine, respectively.1


Oral suspensions containing 200, 400, or 600 mg of amoxicillin/5 mL contain aspartame (NutraSweet), which is metabolized in the GI tract to provide 7 mg of phenylalanine/5 mL.1 3


Other commercially available preparations do not contain aspartame;1 2 4 these other preparations should be used in individuals with phenylketonuria (i.e., homozygous genetic deficiency of phenylalanine hydroxylase) and other individuals who must restrict their intake of phenylalanine.1


Potassium and Sodium Content

Chewable tablets containing 125 or 250 mg of amoxicillin contain 0.16 or 0.32 mEq of potassium, respectively; chewable tablets containing 200 or 400 mg of amoxicillin contain 0.14 or 0.29 mEq of potassium, respectively.1


Each 5 mL of oral suspension containing 125 or 250 mg of amoxicillin contains 0.16 or 0.32 mEq of potassium, respectively.1 Each 5 mL of oral suspension containing 200 or 400 mg of amoxicillin contains 0.14 or 0.29 mEq of potassium, respectively.1 Each 5 mL of oral suspension containing 600 mg of amoxicillin contains 0.23 mEq of potassium.3


Each film-coated or conventional tablet containing 250, 500, or 875 mg of amoxicillin contains 0.63 mEq of potassium.2


Each extended-release tablet containing 1 g of amoxicillin contains 12.6 mg (0.32 mEq) of potassium and 29.3 (1.27 mEq) of sodium.4


Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of amoxicillin and clavulanate and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.1 2 3 4


When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.1 2 3 4 In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.1 2 3 4


Use of Fixed Combination

When used in fixed combination with other agents, consider the cautions, precautions, and contraindications associated with the concomitant agents.


Specific Populations


Pregnancy

Category B.1 2 3 4


Lactation

Distributed into milk; use with caution.1 2 3 4


Pediatric Use

Renal clearance of amoxicillin may be delayed in neonates and young infants because of incompletely developed renal function.1 Dosage adjustments necessary in those <12 weeks (3 months) of age compared with older infants and children.1 (See Pediatric Patients under Dosage and Administration.)


Adverse effects profile similar to adults.1 In children 2 months to 12 years of age receiving oral suspension, diarrhea occurs less frequently with dosing every 12 hours compared with every 8 hours.1


Safety and efficacy of oral suspension containing 600 mg of amoxicillin/5 mL (Augmentin ES-600) not established in children <3 months of age.


Safety and efficacy of extended-release tablets containing 1 g of amoxicillin not established in children <16 years of age.4


Geriatric Use

Possible increased incidence of hepatic dysfunction compared with younger adults.1 2 3 4 (See Hepatic Effects under Cautions.)


Studies using extended-release tablets containing 1 g of amoxicillin indicate no substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.4


Substantially eliminated by kidneys.4 Monitor renal function since geriatric patients more likely to have decreased renal function.17 63 65


Consider that extended-release tablets containing 1 g of amoxicillin contain 29.3 mg (1.27 mEq) of sodium.4


Hepatic Impairment

Use with caution;1 2 3 4 assess hepatic function periodically during prolonged therapy.1 2 3 4


Renal Impairment

Substantially eliminated by kidneys; risk of dose-dependent adverse effects may be greater in those with impaired renal function.17 63 65


Evaluate renal function periodically during prolonged therapy.1 2 3 4


Dosage adjustments necessary in moderate or severe renal impairment.2 5 17 63 65


Tablets containing 875 mg of amoxicillin should not be used in those with severe renal impairment (GFR <30 mL/minute).2


Pharmacokinetics of extended-release tablets not evaluated in renal impairment;4 extended-release tablets contraindicated in those with Clcr <30 mL/minute and in hemodialysis patients.4


Common Adverse Effects


Adverse GI effects (e.g., diarrhea or loose stools,1 2 3 4 17 27 32 33 41 42 44 49 nausea,1 2 3 4 27 32 42 53 vomiting),1 2 3 4 27 32 42 53 hypersensitivity reactions (e.g., rash,1 2 3 4 46 urticaria).1 2 3 4


Adverse GI effects may be more frequent with fixed-combination preparations of amoxicillin and clavulanate potassium than with amoxicillin alone.5 Severe diarrhea may occur less frequently in adults if 875 mg given every 12 hours rather than 500 mg every 8 hours.1


Interactions for Amoxicillin and Clavulanate Potassium


Specific Drugs and Laboratory Tests





















Drug or Test



Interaction



Comments



Allopurinol



Possible increased incidence of rash;1 2 3 4 reported with ampicillin but no data regarding amoxicillin1 2 3 4 113 114



Unclear whether potentiation of rash is caused by allopurinol or hyperuricemia present in these patients1 2 3 4 113 114



Antacids



No effect on pharmacokinetics of amoxicillin or clavulanate when antacids administered simultaneously with or 2 hours after extended-release tablets containing amoxicillin and clavulanate potassium4



Hormonal contraceptives



Possible decreased efficacy of oral contraceptives1 2 3 4



Probenecid



Decreased renal tubular secretion of amoxicillin and increased and prolonged amoxicillin plasma concentrations.1 2 3 4 56


No effect on renal elimination of clavulanic acid.1 2 3 4 5



Concomitant use not recommended1 2 3 4



Tests for glucose



Possible false-positive reactions in urine glucose tests using Clinitest, Benedict’s solution, or Fehling’s solution;1 2 3 4 reported with ampicillin but no data regarding amoxicillin1 2 3 4



Use glucose tests based on enzymatic glucose oxidase reactions (e.g., Clinistix, Tes-Tape)1 2 3 4


Amoxicillin and Clavulanate Potassium Pharmacokinetics


Absorption


Bioavailability


Both amoxicillin and clavulanate potassium well absorbed following oral administration.1 2 3 4 5 30 41 53 62

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