Cefaclor

J01D - Other beta-lactam antibacterials ATC J01DC04 Small molecule approved 1979 Oral

🧬 Cross-allergy: Cephalosporins

JFDA label: Cloracef MR 375 Tabs

Mechanism of Action

Inhibitor of Bacterial penicillin-binding protein — Bacterial penicillin-binding protein inhibitor

Target	Action	Gene / class
Bacterial penicillin-binding protein efficacy	INHIBITOR

Indications

Approved

Acute bacterial exacerbations of chronic bronchitis (extended-release tablets only)
Lower respiratory tract infections (capsules and oral suspension only)
Otitis media (capsules and oral suspension only)
Pharyngitis and tonsillitis
Secondary bacterial infections of acute bronchitis (extended-release tablets only)
Skin and skin structure infections, uncomplicated
Urinary tract infections (capsules and oral suspension only)

Antimicrobial Spectrum

Expected / intrinsic spectrum (EUCAST breakpoints & labels) — not local resistance. Source: EUCAST v16 · openfda-label.

Bacteria

Organism	Activity	MIC
Acinetobacter calcoaceticus	Active	—
Citrobacter diversus	Active	—
Enterococcus faecalis	Active	—
Escherichia coli	Active	—
Haemophilus influenzae	Active	—
Moraxella catarrhalis	Active	—
Morganella morganii	Active	—
Neisseria gonorrhoeae	Active	—
Proteus mirabilis	Active	—
Proteus morganii	Active	—
Proteus rettgeri	Active	—
Providencia rettgeri	Active	—
Staphylococcus aureus	Active	—
Streptococcus pneumoniae	Susceptible	0.001 mg/L
Streptococcus pyogenes	Active	—

Class profile

gramStatus	Both
spectrumBreadth	Moderate
atypicalCoverage	No
isBactericidal	1
moaCategory	Cell wall synthesis inhibitor (beta-lactam, 2nd generation cephalosporin)
pdIndex	Time-dependent
postAntibioticEffect	None
mrsaCoverage	0
resistanceMechanisms	Beta-lactamase production,PBP mutations

Contraindications

Source: Lexicomp

Hypersensitivity to cefaclor, any component of the formulation, or other cephalosporins Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Hepatobiliary disorders (1)

Common Increased serum transaminases

Renal and urinary disorders (2)

Common Vaginitis · vulvovaginal candidiasis

Blood and lymphatic system disorders (1)

Common Eosinophilia

Immune system disorders (1)

Uncommon Serum-sickness-like reaction (unique to cefaclor)

Gastrointestinal disorders (3)

Common Diarrhea · Diarrhoea · Nausea

Skin and subcutaneous tissue disorders (2)

Common Rash

Uncommon Rash / urticaria

Dosing

Source: Lexicomp

Treatment of susceptible infections: Oral: Immediate-release: 250 to 500 mg every 8 hours Extended-release: 500 mg every 12 hours Indication-specific dosing: Note: An extended-release tablet dose of 500 mg twice daily is clinically equivalent to an immediate-release capsule dose of 250 mg 3 times daily; an extended-release tablet dose of 500 mg twice daily is NOT clinically equivalent to 500 mg 3 times daily of other cefaclor formulations. Acute bacterial exacerbations of chronic bronchitis: Oral: Extended-release: 500 mg every 12 hours for 7 days Secondary bacterial infection of acute bronchitis: Oral: Extended-release: 500 mg every 12 hours for 7 days

(For additional information see "Cefaclor: Pediatric drug information") Treatment of susceptible infections: Usual dosage range: Infants ≥1 month, Children, and Adolescents: Oral: Immediate-release: 20 to 40 mg/kg/day divided every 8 to 12 hours; maximum dose: 1,000 mg/day Adolescents ≥16 years: Oral: Extended-release: 500 mg every 12 hours Indication-specific dosing: Infants >1 month, Children, and Adolescents: Lower respiratory tract infections: Oral: Immediate-release: 20 to 40 mg/kg/day divided every 8 hours (maximum dose: 1,000 mg/day). If beta-hemolytic streptococcus/S. pyogenes suspected, treat for at least 10 days. Otitis media: Oral: Immediate-release: 40 mg/kg/day divided every 12 hours (maximum dose: 1,000 mg/day). If beta-hemolytic streptococcus/S. pyogenes suspected, treat for at least 10 days. Pharyngitis/tonsillitis: Oral: Immediate-release: 20 mg/kg/day divided every 12 hours (maximum dose: 1,000 mg/day). If beta-hemolytic streptococcus/S. pyogenes confirmed, treat for at least 10 days. Note: Not a preferred drug (Shulman 2012). Skin and skin structure infections, uncomplicated: Oral: Immediate-release: 20 to 40 mg/kg/day divided every 8 hours (maximum dose: 1,000 mg/day). If due to beta-hemolytic streptococcus/S. pyogenes, treat for at least 10 days. Urinary tract infections: Oral: Immediate-release: 20 to 40 mg/kg/day divided every 8 hours (maximum dose: 1,000 mg/day). Adolescents ≥16 years: Note: An extended-release tablet dose of 500 mg twice daily is clinically equivalent to an immediate-release capsule dose of 250 mg 3 times daily; an extended-release tablet dose of 500 mg twice daily is NOT clinically equivalent to 500 mg 3 times daily of other cefaclor formulations. Acute bacterial exacerbations of chronic bronchitis: Oral: Extended-release: 500 mg every 12 hours for 7 days Secondary bacterial infection of acute bronchitis: Oral: Extended-release: 500 mg every 12 hours for 7 days

Refer to adult dosing.

Manufacturer’s labeling: Oral, immediate-release: There are no dosage adjustments provided in the manufacturer's labeling; however, half-life is increased in anuric patients; use with caution. Oral, extended-release: There are no dosage adjustments provided in the manufacturer’s labeling. Dialysis: Moderately dialyzable (20% to 50%) Alternative recommendations (off-label dosing) (Aronoff 2007): Adults: Oral, immediate-release: Mild to severe impairment: No dosage adjustment necessary. End-stage renal disease (ESRD) on intermittent hemodialysis (IHD) (administer after hemodialysis on dialysis days): Supplement with 250 to 500 mg after dialysis. Peritoneal dialysis: Administer 250 to 500 mg every 8 hours. Infants, Children and Adolescents: Oral, immediate-release: GFR ≥10 mL/minute: No dosage adjustment necessary. GFR End-stage renal disease (ERD) on intermittent hemodialysis (IHD) (supplemental dose post-hemodialysis needed): Administer 50% of the recommended dose (based on indication). Peritoneal dialysis: Administer 50% of the recommended dose (based on indication).

There are no dosage adjustments provided in the manufacturer’s labeling.

Warnings & Precautions

Source: Lexicomp

Hypersensitivity

Anaphylactic reactions have occurred. If a serious hypersensitivity reaction occurs, discontinue and institute emergency supportive measures, including airway management and treatment (eg, epinephrine, antihistamines, and/or corticosteroids).

Penicillin allergy

Use with caution in patients with a history of penicillin allergy.

Superinfection

Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment. Disease-related concerns:

Gastrointestinal disease

Use with caution in patients with a history of gastrointestinal disease, particularly colitis.

H. influenzae infections

Beta-lactamase-negative, ampicillin-resistant (BLNAR) strains of H. influenzae should be considered resistant to cefaclor.

Renal impairment

Use with caution in patients with renal impairment. Concurrent drug therapy issues:

Drug-drug interactions

Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Dosage form specific issues:

Benzyl alcohol and derivatives

Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer’s labeling.

Extended-release tablet

An extended-release tablet dose of 500 mg twice daily is clinically equivalent to an immediate-release capsule dose of 250 mg 3 times daily; an extended-release tablet dose of 500 mg twice daily is NOT clinically equivalent to 500 mg 3 times daily of other cefaclor formulations.

Pregnancy & Lactation

Pregnancy

FDA category B Teratogenic

Adverse events were not observed in animal reproduction studies. An increased risk of teratogenic effects has not been observed following maternal use of cefaclor.

Lactation

Small amounts of cefaclor are excreted in breast milk. The manufacturer recommends that caution be exercised when administering cefaclor to nursing women. Nondose-related effects could include modification of bowel flora.

Monitoring

Efficacy	Culture and susceptibility testing; clinical resolution (temperature, WBC, CRP, procalcitonin)
Toxicity	Renal function (dose adjustment in renal impairment); hepatic function for hepatically cleared agents; signs of C. difficile infection (diarrhoea)
Clinical pearl	Culture results guide de-escalation to narrower-spectrum therapy. Review antibiotic appropriateness at 48–72 h (antimicrobial stewardship).
Counseling	Complete the full course. Report persistent diarrhoea, rash, or lack of improvement after 48–72 h.

Chemistry & Properties

Formula	C15H16ClN3O5S
Molecular weight	385.83 g/mol
IUPAC name	(6R,7R)-7-[[(2R)-2-amino-2-phenylacetyl]amino]-3-chloro-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
CAS	53994-73-3
PubChem CID	51039
InChIKey	`WKJGTOYAEQDNIA-IOOZKYRYSA-N`
logP	0.62 (XLogP -1.8)
Polar surface area	112.73 Å²
H-bond acceptors / donors	5 / 3
Drug-likeness (QED)	0.67
Lipinski violations	0

SMILES

N[C@@H](C(=O)N[C@@H]1C(=O)N2C(C(=O)O)=C(Cl)CS[C@H]12)c1ccccc1.O

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP3A4	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)NTCP (Inhibitor)OAT1 (Inhibitor)OAT3 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)PEPT1 (Inhibitor)PEPT2 (Inhibitor)OAT1 (Substrate)OAT3 (Substrate)P-gp (Substrate)PEPT1 (Substrate)PEPT2 (Substrate)

Drug–drug interactions (11, DDInter)

Interacting drug	Severity	Management
Aluminum hydroxide	moderate
Balsalazide	moderate
Chloramphenicol	moderate
Dicoumarol	moderate
Ethinylestradiol	moderate
Magnesium hydroxide	moderate
Mycophenolic acid	moderate
Pemetrexed	moderate
Picosulfuric acid	moderate
Teriflunomide	moderate
Warfarin	moderate

Registered Products (52)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Midocef Dry Suspension	Suspension 125 mg/5 ml	60 ml pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	2.310
Cefabac Suspension	Suspension 125 mg/5 ml	60 ml pack varies	The Arab Pharmaceutical Manufactruing Co.	2.600
Forticef-125 suspension	Suspension 125 mg/5 ml	60 ml pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	2.600
Forbatec	Solution 1.57 g	60 ml	United Pharmaceutical	2.830
Midocef Dry Suspension	Suspension 125 mg/5 ml	75 ml pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	2.890
Ceclor	Suspension 125 mg/5 ml	60 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	3.160
Forticef-125 suspension	Suspension 125 mg/5 ml	75 ml pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	3.250
Biocef	Suspension 250 mg/5 ml	75 ml	Noor Drug Store	3.400
Cefabac Suspension	Suspension 125 mg/5 ml	100 ml pack varies	The Arab Pharmaceutical Manufactruing Co.	3.500
Cloracef 125mg/5ml Susp.	Suspension 125 mg/5 ml	75 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	3.500
Pharmaclor suspention	Suspension 125 mg/5 ml	100 ml	Pharma International Company/ Jordan	3.550
Cefabac Suspension	Suspension 250 mg/5 ml	60 ml pack varies	The Arab Pharmaceutical Manufactruing Co.	3.700
Forbatec	Solution 3.15 g	60 ml	United Pharmaceutical	3.700
Forticef-250 suspension	Suspension 250 mg/5 ml	60 ml pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	3.700
Midocef Dry Suspension	Suspension 250 mg/5 ml	60 ml pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	3.700
Midocef Capsules	Capsule (as Monohydrate) 250 mg	12 cap	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	3.870
Ceclor	Suspension 250 mg/5 ml	60 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	3.890
Tibifor	Tablet 750 mg	6 tab	AL Rahma Drug Store	4.290
CLORACEF Forte 250 SUSP.	Suspension 250 mg/5 ml	75 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	4.630
Forticef-250 suspension	Suspension 250 mg/5 ml	75 ml pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	4.630
Midocef Dry Suspension	Suspension 250 mg/5 ml	75 ml pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	4.630
Cloracef MR 375 Tabs	Tablet 375 mg	10 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	5.000
Pharmaclor cap	Capsule 250 mg	16 cap	Pharma International Company/ Jordan	5.140
Midocef Capsules	Capsule (as Monohydrate)250 mg	16 cap pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	5.160
Forticef-250mg capsule	Capsule 250 mg	12 cap pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	5.250
Midocef MR Tablet	Tablet (Monohydrate) 500 mg	10 tab pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	5.540
CLORACEF MR 500 TABS.	Tablet 500 mg	10 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	5.600
Pharmaclor suspension	Suspension 250 mg/5 ml	100 ml	Pharma International Company/ Jordan	5.700
Cefabac Suspension	Suspension 250 mg/5 ml	100 ml pack varies	The Arab Pharmaceutical Manufactruing Co.	5.800
Midocef Capsules	Capsule as Monohydrate 500 mg	12 cap pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	5.950
Forbatec Capsules	Capsule 500 mg	12 cap pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	6.000
Forticef-250mg capsule	Capsule 250 mg	15 cap pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	6.560
CLORACEF 250 CAPS.	Capsule 250 mg	16 cap	Dar Al Dawa Development and Investment Co Ltd/Jordan	7.000
Cloracef MR 375 Tabs	Tablet 375 mg	14 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	7.000
CLORACEF 375 SUSP.	Suspension 375 mg/5 ml	75 ml	Dar Al Dawa Development and Investment Co Ltd/Jordan	7.210
Forbatec Capsules	Capsule 500 mg	15 cap pack varies	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	7.500
CLORACEF MR 750 TABS.	Tablet 750 mg	10 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	7.820
CLORACEF MR 500 TABS.	Tablet 500 mg	14 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	7.840
Midocef Capsules	Capsule as Monohydrate 500 mg	16 cap pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	7.930
Pharmaclor cap	Capsule 500 mg	16 cap	Pharma International Company/ Jordan	8.000
Midocef MR 750	Tablet 750 mg	10 tab	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	8.220
Forticef-500mg capsule	Capsule 500 mg	12 cap pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	8.250
Ceclor 500 MR	Tablet 500 mg	10 tab	Dar Al Dawa Development and Investment Co Ltd/Jordan	8.610
Biocef Cap	Capsule 500 mg	15 cap	IBN CINA DRUG STORE	8.890
Ceclor 750 MR	Tablet 750 mg	10 tab	Dar Al Dawa Development and Investment Co Ltd/Jordan	10.310
Forticef-500mg capsule	Capsule 500 mg	15 cap pack varies	AL-RAM PHARMA.INDUS.CO.LTD/JORDAN	10.310
CLORACEF MR 750 TABS.	Tablet 750 mg	14 tab pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	10.950
CLORACEF F. 500 CAPS.	Capsule 500 mg	16 cap pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	11.000
Midocef Capsules	Capsule (as Monohydrate)250 mg	500 cap pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	124.000
Midocef Capsules	Capsule as Monohydrate 500 mg	500 cap pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	192.500
Midocef MR	Extended-Release Tablet (Monohydrate) 500 mg	500 MR Tab pack varies	MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN	235.450
CLORACEF F. 500 CAPS.	Capsule 500 mg	504 cap pack varies	Dar Al Dawa Development and Investment Co Ltd/Jordan	277.200