Antimicrobial Drugs – Cephalosporins 3rd Generation

Name of the Cephalosporins 3rd Generation Drugs

• Ceftazidime (Avycaz)
• Cefixime (Suprax)
• Cefditoren (Spectracef)
• Cefdinir
• Cefotaxime (Claforan)
• Cefoperazone
• Cefpodoxime (Vantin)
• Ceftibuten (Cedax )
• Ceftriaxone

1.Ceftazidime (Avycaz)

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the cross-linking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Pharmacokinetics

• Peak plasma concentration: 88.1 mg/L (single 2.5 g-dose); 90.4 mg/L (multiple 2.5 g-dose)
• AUC: 289 mg·h/L (single 2.5 g-dose); 291 mg·h/L (multiple 2.5 g-dose)
• Protein bound: <10% (ceftazidime); 5.7-8.2% (avibactam)
• 80-90% of ceftazidime IV dose is eliminated unchanged via the urine
• Nearly 100% of avibactam IV dose is eliminated unchanged via the urine
• Half-life: 3.27 hr (single 2.5 g-dose); 2.76 hr (multiple 2.5 g-dose)
• Clearance (L/h): 6.93 L/h (single 2.5 g-dose); 6.86 L/h (multiple 2.5 g-dose)
• Excretion: Urine (~80- 90% as unchanged drug)

Administration

• Obtain specimens for culture and sensitivity testing as necessary before starting therapy.
• Reconstitute powder for injection with sterile water, following manufacturer’s directions for amount of diluent to use.
• For I.V. injection, dilute in sterile water as directed, and give single dose over 3 to 5 minutes. Inject into large vein; rotate injection sites.
• For intermittent I.V. infusion, dilute further with 100 ml of sterile water or another compatible fluid, such as normal saline solution or dextrose 5% in water. Infuse over 30 minutes.
• Don’t dilute with sodium bicarbonate.
• For I.M. injection, reconstitute with sterile water, bacteriostatic water, or 0.5% or 1% lidocaine hydrochloride.
• When giving I.M., inject deep into large muscle mass.

Contraindications

Hypersensitivity to cephalosporins or penicillins

Precautions:

• Renal impairment, hepatic disease, biliary obstruction, phenylketonuria
• History of GI disease
• Elderly patients 
• Pregnant or breastfeeding patients
• Children.

Adverse reactions

• CNS: headache, confusion, hemiparesis, lethargy, paresthesia, syncope, asterixis, neuromuscular excitability (with increased drug blood levels in renally impaired patients),seizures, encephalopathy
• CV: hypotension, palpitations, chest pain, vasodilation
• EENT: hearing loss
• GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis
• GU: vaginal candidiasis, nephrotoxicity
• Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression Hepatic: hepatic failure, hepatomegaly
• Musculoskeletal: arthralgia
• Respiratory: dyspnea
• Skin: urticaria, maculopapular or erythematous rash
• Other: chills, fever, superinfection, I.M. site pain, anaphylaxis, serum sickness

Patient monitoring

• Monitor for extreme confusion, tonic-clonic seizures, and mild hemiparesis when giving high doses.
• Assess CBC and kidney and liver function test results.
• Monitor for signs and symptoms of superinfection and other serious adverse reactions.
• Be aware that cross-sensitivity to penicillins may occur.

Patient teaching

• Instruct patient to report reduced urine output, persistent diarrhea, bruising, and bleeding.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

Nursing Considerations

• Use ceftazidime cautiously in patients hypersensitive to penicillin because cross sensitivity occurs in about 10% of such patients. Watch for allergic reactions a few days after therapy starts.
• Use cautiously in patients with a history of GI disease, particularly colitis, because risk of pseudomembranous colitis is increased.
• Ceftazidime l-arginine (Ceptaz) is not recommended for children under age 12.
• If possible, obtain culture and sensitivity test results, as ordered, before giving drug.
• Protect ceftazidime powder and reconstituted drug from heat and light; both tend to darken during storage.
• If pharmacy delivers frozen solution, thaw it at room temperature, not in water bath or microwave. Store thawed solution for up to 12 hours at room temperature or 7 days in refrigerator; don’t refreeze.
• For I.V. bolus, reconstitute 1 to 2 g with 10 ml sterile water for injection, D5W, or sodium chloride for injection. Shake to dissolve. Administer I.V. injection slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. fluid.
• For intermittent infusion, further dilute in 50 to 100 ml D5W or normal saline solution. Avoid using sodium bicarbonate injection as a diluent because drug is least stable in it. During ceftazidime administration, temporarily stop other solutions being given at the same I.V. site.
• For I.M. use, reconstitute each gram with 3 ml sterile water for injection or bacteriostatic water for injection.
• Give I.M. injection deep into large muscle mass, such as gluteus maximus.
• Rotate I.V. sites every 72 hours. Assess for phlebitis and extravasation.
• Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.
• Monitor CBC, hematocrit, and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels during long-term therapy
• Monitor PT, as ordered, in at-risk patients,such as those with renal or hepatic impairment or poor nutritional state and those receiving anticoagulant or prolonged antibiotic therapy. Notify prescriber if PT decreases, and expect to give vitamin K.
• Assess patient for perineal itching, fever, malaise, redness, swelling, rash, and change in cough or sputum; they may indicate a superinfection.
• Watch for pharyngitis, ecchymosis, bleeding, and arthralgia (possible blood dyscrasia). Monitor PT and bleeding time.

2.Ceftibuten (Cedax )

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the cross-linking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Pharmacokinetics

• Half-Life: 2.4 hr
• Peak Plasma Time: 2-3 hr
• Absorption: rapid; food decreases peak concentrations, delays Tmax, & lowers AUC
• Vd: children: 0.5 L/kg; adults: 0.21 L/kg
• Excretion: urine (56%); feces (39%)

Administration

Obtain specimens for culture and sensitivity testing as necessary before starting therapy.

Give oral suspension at least 1 hour before or 2 hours after a meal.

Contraindications

Hypersensitivity to cephalosporins and penicillins

Precautions:

• Renal impairment, hepatic disease, biliary obstruction, phenylketonuria
• History of GI disease
• Elderly patients
• Pregnant or breastfeeding patients
• Children.

Adverse reactions

• CNS: headache, lethargy, paresthesia, syncope,seizures
•  CV: hypotension, palpitations, chest pain, vasodilation
• EENT: hearing loss
• GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis
• GU: vaginal candidiasis, nephrotoxicity
• Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression
• Hepatic: hepatic failure, hepatomegaly Musculoskeletal: arthralgia
• Respiratory: dyspnea
• Skin: urticaria, easy bruising, maculopapular or erythematous rash
• Other: chills, fever, superinfection, anaphylaxis, serum sickness

Patient monitoring

• Assess CBC and kidney and liver function test results.
• Monitor for signs and symptoms of superinfection and other serious adverse reactions.
• Be aware that cross-sensitivity to penicillins may occur.

Patient teaching

• Instruct patient to take oral suspension at least 1 hour before or 2 hours after a meal.
• Inform diabetic patient that oral suspension contains 1 g sucrose per teaspoon.
• Advise patient to continue to take full amount prescribed even when he feels better.
• Tell patient to report signs and symptoms of allergic response and other adverse reactions, such as rash, easy bruising, bleeding, severe GI problems, or difficulty breathing.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

Nursing Considerations

• Use ceftibuten cautiously in patients hypersensitive to penicillins because cross sensitivity occurs in up to 10% of such patients.
• If possible, obtain culture and sensitivity test results, as ordered, before giving drug.
• Refrigerate oral suspension; shake well before using. Discard after 14 days.
• Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.
• Be aware that an allergic reaction may occur a few days after therapy starts.
• Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.
• Assess patient for perineal itching, fever, malaise, redness, swelling, rash, and change in cough or sputum; they may indicate a superinfection.
• Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

3.Cefixime (Suprax)

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Pharmacokinetics

• Bioavailability: 40-50%
• Average peak plasma concentration: ~2 mcg/mL (single 200 mg-tablet); ~3.7 mcg/mL (single 400 mg-tablet)
• Peak plasma time: 2-6 hr (single 200mg, 400 mg–tablet or 400mg suspension); 2-5 hr (single 200 mg-suspension); 3-8 hr (single 400 mg-capsule)
• Food reduces absorption following administration of the capsule by ~15% based on AUC and 25% based on peak plasma concentrations
• Distribution: Distributed widely throughout body and reaches therapeutic concentration in most tissues and body fluids, including synovial, pericardial, pleural, and peritoneal; bile, sputum, and urine; bone, myocardium, gallbladder, skin, and soft tissue
• Protein bound: 65%
• Half-life: 3-4 hr
• Excretion: Urine (50% as unchanged drug), feces (10%)

Administration

• Obtain specimens for culture and sensitivity testing as necessary before starting therapy.
• Know that drug may be taken with food.
• Be aware that suspension should be given for otitis media because it provides higher serum concentration.

Contraindications

Hypersensitivity to cephalosporins or penicillins

Precautions:

• Renal impairment, phenylketonuria
• History of GI disease
• Elderly patients
• Pregnant or breastfeeding patients
• Children.

Adverse reactions

• CNS: headache, lethargy, paresthesia, syncope,seizures
• CV: hypotension, palpitations, chest pain, vasodilation
• EENT: hearing loss
• GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis
• GU: vaginal candidiasis, nephrotoxicity
• Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression
• Hepatic: hepatic failure, hepatomegaly
• Musculoskeletal: arthralgia
• Respiratory: dyspnea Skin: urticaria, maculopapular or erythematous rash
• Other: chills, fever, superinfection, anaphylaxis, serum sickness

Patient monitoring

• Monitor baseline CBC and kidney and liver function test results.
• Monitor for signs and symptoms of superinfection and other serious adverse reactions.
• Be aware that cross-sensitivity to penicillins may occur.

Patient teaching

• Tell patient to take once-daily doses at same time each day.
• Advise patient to take drug exactly as prescribed and to continue to take full amount prescribed even when he feels better.
• Instruct patient to report signs and symptoms of allergic response and other adverse reactions, such as rash, easy bruising, bleeding, severe GI problems, or difficulty breathing.
• Caution patient not to take herbs without consulting prescriber.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

Nursing Considerations

• Use cefixime cautiously in patients with impaired renal function or a history of GI disease, especially colitis. Also use cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.
• If possible, obtain culture and sensitivity test results, as ordered, before giving drug.
• Tablets shouldn’t be substituted for oral suspension to treat otitis media because cefixime suspension produces a higher peak blood level than do tablets when administered at the same dose.
• Monitor BUN and serum creatinine for early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.
• Be aware that an allergic reaction may occur a few days after therapy starts.
• Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.
• Assess for signs of superinfection, such as perineal itching, fever, malaise, redness, pain, swelling, drainage, rash, diarrhea, and cough or sputum changes.
• Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

4.Cefotaxime (Claforan)

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting cross-linking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Pharmacokinetics

• Peak plasma time: IM, 30 min
• Partially metabolized in liver
• Metabolite: Desacetylcefotaxime (active)
• Half-life: Parent drug, 1-1.5 hr; active metabolite, 1-1.9 hr
• Excretion: Urine

Administration

• Obtain specimens for culture and sensitivity testing as necessary before starting therapy.
• Reconstitute powder for I.V. injection with at least 10 ml of sterile water and give over 3 to 5 minutes. For intermittent infusion, drug may be diluted further with 50 or 100 ml of normal saline solution or dextrose 5% in water (D5W) and given over 30 minutes.
• Reconstituted drug may be diluted further for a continuous I.V. infusion of up to 1,000 ml with a compatible solution, such as normal saline solution, dextrose 5% or 10% in water, or D5W and normal saline solution. Give over 6 to 24 hours, depending on concentration.
• Don’t use diluents with pH above 7.5 (such as sodium bicarbonate).
• Rotate infusion sites.
• Inject I.M. deep into large muscle mass. Divide 2-g dose in half and inject into separate large muscle masses

Contraindications

Hypersensitivity to cephalosporins or penicillins

Precautions:

• Renal impairment, phenylketonuria
• History of GI disease
• Elderly patients
• Pregnant or breastfeeding patients
• Children

Adverse reactions

• CNS: headache, lethargy, paresthesia, syncope,seizures
• CV: hypotension, palpitations, chest pain, vasodilation
• EENT: hearing loss
• GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis
• GU: vaginal candidiasis, nephrotoxicity
• Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression
• Hepatic: hepatic failure, hepatomegaly
• Musculoskeletal: arthralgia
• Respiratory: dyspnea
• Skin: urticaria, maculopapular or erythematous rash
• Other: chills, fever, superinfection, pain at I.M. injection site, anaphylaxis, serum sickness

Patient monitoring

• Monitor CBC and kidney and liver function test results.
• Monitor for signs and symptoms of superinfection and other serious adverse reactions.
• Be aware that cross-sensitivity to penicillin’s may occur.

Patient teaching

• Advise patient to report reduced urinary output, persistent diarrhea, bruising, and bleeding.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

Nursing Considerations

• Use cefotaxime cautiously in patients with impaired renal function, a history of GI disease (especially colitis), or hypersensitivity to penicillin because cross-sensitivity has occurred in about 10% of such patients.
• If possible, obtain culture and sensitivity test results, as ordered, before giving drug.
• For I.V. use, reconstitute each 0.5-, 1-, or 2-g vial with 10 ml of sterile water for injection. Shake to dissolve.
• For intermittent I.V. infusion, further dilute in 50 to 100 ml of D5W or normal saline solution.
• For I.M. use, reconstitute each 500-mg vial with 2 ml sterile water for injection or bacteriostatic water for injection; each 1-g vial with 3 ml diluent; and each 2-g vial with 5 ml diluent. Shake to dissolve.
• Give cefotaxime by I.V. injection over 3 to 5 minutes through tubing of a free-flowing compatible I.V. solution. Temporarily stop other solutions being given through same I.V. site.
• Discard unused drug after 24 hours if stored at room temperature, 5 days if refrigerated.
• Protect cefotaxime powder and solution from light and heat.
• Monitor I.V. sites for signs of phlebitis or extravasation. Rotate I.V. sites every 72 hours.
• Monitor BUN and serum creatinine levels and fluid intake and output for signs of nephrotoxicity.
• Be aware that allergic reaction may occur a few days after cefotaxime therapy starts.
• Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold cefotaxime and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.
• Assess patient for pharyngitis, ecchymosis, bleeding, and arthralgia, which may indicate a blood dyscrasia. Monitor CBC, PT, and bleeding time, as ordered.
• Monitor patient closely for superinfection. If evidence appears, notify prescriber and expect to stop drug and provide care.

5.Cefoperazone

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die.

Contraindications

 Hypersensitivity to cephalosporins or their components

Adverse Reactions

• CNS: Chills, fever, headache, seizures
• CV: Edema
• EENT: Hearing loss
• GI: Abdominal cramps, diarrhea, elevated liver function test results, hepatic failure, hepatomegaly, nausea, oral candidiasis, pseudomembranous colitis, vomiting
• GU: Elevated BUN level, nephrotoxicity, renal failure, vaginal candidiasis
• HEME: Eosinophilia, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, unusual bleeding
• MS: Arthralgia
• RESP: Dyspnea
• SKIN: Ecchymosis, erythema, erythema multiforme, pruritus, rash, Stevens-Johnson syndrome
• Other: Anaphylaxis; injection site pain, redness, and swelling; superinfection

Nursing Considerations

• Use cefoperazone cautiously in patients with a history of bleeding problems, GI disease (especially colitis), or severely impaired hepatic or renal function. Also use cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.
• If possible, obtain culture and sensitivity test results, as ordered, before giving drug.
• For I.V. use, reconstitute with required amount of diluent. Then further dilute in compatible solution, such as D5W, D10W, dextrose 5% in lactated Ringer’s solution, dextrose 5% in quarter-normal (0.2) saline solution, dextrose 5% in normal saline solution, lactated Ringer’s injection, normal saline solution, Normosol M and D5W, or Normosol R. (See manufacturer’s guidelines for details.)
• Give I.V. drug as intermittent infusion over 15 to 30 minutes or as continuous infusion. Direct bolus injection isn’t recommended.
• For I.M. injection, reconstitute drug with bacteriostatic water for injection (that contains benzyl alcohol or parabens) or sterile water for injection.
• After reconstitution, let foam dissipate, and inspect the solution to ensure complete dissolution.
• Store reconstituted solution at room temperature for 24 hours.
• Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.
• Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.
• Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.
• Assess for evidence of superinfection, such as perineal itching, fever, malaise, redness, pain, swelling, drainage, rash, diarrhea, and cough or sputum changes.

Patient Teaching

• Advise patient to avoid alcohol during therapy and for at least 3 days after last dose.
• Explain that I.M. injection may hurt.
• Tell patient to immediately report severe diarrhea to prescriber.

Adverse Effects:

• Hypersensitivity: Maculopapular rash, Urticaria, Pruritis, Anaphylaxis/angioedema, eosinophilia
• Hematologic: Hypoprothrombinaemia, Neutropenia, Leukopenia, Thrombocytopenia
• GI: Diarrhea, C. difficile disease
• Renal: Interstitial nephritis

Precautions:

• Hypersensitivity to penicillins,
• History of gastrointestinal disease,
• Particularly colitis,
• Renal impairment,
• Dosage reduction may be necessary in patients with liver dysfunction,
• Concomitant alcohol use (disulfiram-like reaction),
• Patients with a poor nutritional status, malabsorption states

6.Cefpodoxime (Vantin)

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die

Pharmacokinetics

• Bioavailability: 50%; acid stable
• Peak plasma time: ≤1 hr
• Distribution: Distributed well into tissues, including lungs and tonsils; penetrates into pleural fluid
• Protein bound: 18-23%
• Metabolism: Metabolized in liver to active metabolite
• Half-life: 2-3 hr; prolonged with renal impairment
• Excretion: Urine (80% as unchanged drug) in 24 hr

Administration

• Obtain specimens for culture and sensitivity testing as necessary before starting therapy.
• Give tablets with food to enhance absorption. Oral suspension may be given with or without food.
• Don’t give antacids within 2 hours of cefpodoxime

Contraindications

 Hypersensitivity to cephalosporins or penicillins

Precautions:

• Renal impairment, phenylketonuria
• History of GI disease
• Elderly patients
• Pregnant or breastfeeding patients
• Children.

Adverse reactions

• CNS: headache, lethargy, paresthesia, syncope,seizures
• CV: hypotension, palpitations, chest pain, vasodilation
• EENT: hearing loss
• GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis
• GU: vaginal candidiasis, nephrotoxicity
• Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression
• Hepatic: hepatic failure, hepatomegaly
• Musculoskeletal: arthralgia Respiratory: dyspnea
• Skin: urticaria, maculopapular or erythematous rash
• Other: chills, fever, superinfection, anaphylaxis, serum sickness

Patient monitoring

• Assess CBC and kidney and liver function test results.
• Monitor for signs and symptoms of superinfection and other serious adverse reactions.
• Be aware that cross-sensitivity to penicillins may occur.

Patient teaching

• Instruct patient to take drug with food or milk to reduce GI distress and enhance absorption.
• Advise patient not to take antacids within 2 hours of drug.
• Tell patient to continue to take full amount prescribed even when he feels better.
• Instruct patient to report signs and symptoms of allergic response and other adverse reactions, such as rash, easy bruising, bleeding, severe GI problems, or difficulty breathing.
• If patient is being treated for gonorrhea, instruct him to have partner tested and treated (as needed) and to use barrier contraception to prevent reinfection.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

Nursing Considerations

• Use cefpodoxime cautiously in patients who have impaired renal function or are receiving potent diuretics. Also use drug cautiously in patients hypersensitive to penicillin because cross-sensitivity has occurred in about 10% of such patients.
• If possible, obtain culture and sensitivity test results, as ordered, before giving cefpodoxime.
• Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis.
• Be aware that an allergic reaction may occur a few days after therapy starts

7.Ceftriaxone

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting cross-linking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die.

Pharmacokinetics

• Absorption: IM preparation well absorbed
• Peak plasma time: 2-3 hr (IM)
• Distribution: Distributed throughout body, including gallbladder, lungs, bone, bile, and CSF (higher concentrations achieved when meninges are inflamed); crosses placenta; enters amniotic fluid and breast milk
• Protein bound: 85-95%
• Vd: 6-14 L
• Metabolism: Metabolized in liver
• Half-life: 5-9 hr (normal hepatic and renal function); 12-16 hr (mild-to-severe renal impairment)
• Excretion: Urine (33-67% as unchanged drug), feces

Administration

• Obtain specimens for culture and sensitivity testing as necessary before starting therapy.
• Be aware that drug mustn’t be given with or within 48 hours of calcium-containing I.V. solutions, including calcium-containing continuous infusions such as parenteral nutrition, because of risk of precipitation of ceftriaxone calcium salt (particularly in neonates).
• Know that drug for I.V. injection is compatible with sterile water, normal saline solution, dextrose 5% in water (D5W), half-normal saline solution, and D5W and normal saline solution.
• After reconstituting, dilute further to desired concentration for intermittent I.V. infusion. Infuse over 30 minutes.
• For I.M. use, reconstitute powder for injection with compatible solution by adding 0.9 ml of diluent to 250-mg vial, 1.8 ml to 500-mg vial, 3.6 ml to 1-g vial, or 7.2 ml to 2-g vial, to yield a concentration averaging 250 mg/ml.
• Divide high I.M. doses equally and administer in two separate sites. Inject deep into large muscle mass.

Contraindications

 Neonates (28 days or younger)

Precautions:

 Hypersensitivity to cephalosporins or penicillins, allergies

 Renal impairment, hepatic disease, gallbladder disease, phenylketonuria

Adverse reactions

• CNS: headache, confusion, hemiparesis, lethargy, paresthesia, syncope, seizures
• CV: hypotension, palpitations, chest pain, vasodilation
• EENT: hearing loss
• GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis, pancreatitis,Clostridium difficile–associated diarrhea
• GU: vaginal candidiasis
• Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinaemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression
• Hepatic: jaundice, hepatomegaly
• Musculoskeletal: arthralgia
• Respiratory: dyspnea
• Skin: urticaria, maculopapular or erythematous rash
• Other: chills, fever, superinfection, pain at I.M. injection site, anaphylaxis, serum sickness

Patient monitoring

• Monitor for extreme confusion, tonic-clonic seizures, and mild hemiparesis when giving high doses.
• Monitor coagulation studies.
• Assess CBC and kidney and liver function test results.
• Monitor for signs and symptoms of superinfection and other serious adverse reactions.
• Be aware that cross-sensitivity to penicillins and cephalosporins may occur.

Patient teaching

• Instruct patient to report persistent diarrhea, bruising, or bleeding.
• Caution patient not to use herbs unless prescriber approves.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

Nursing Considerations

• Use ceftriaxone cautiously in patients who are hypersensitive to penicillins because cross-sensitivity has occurred in about 10% of such patients.
• If possible, obtain culture and sensitivity results, as ordered, before giving drug.
• Protect powder from light.
• For I.V. use, reconstitute with an appropriate diluent, such as sterile water for injection or sodium chloride for injection, as follows: for 250-mg vial, add 2.4 ml; for 500-mg vial, add 4.8 ml; for 1-g vial, add 9.6 ml; and for 2-g vial, add 19.2 ml to yield 100 mg/ml. For piggyback bottles, reconstitute with 10 ml of diluent indicated above for 1-g bottle and 20 ml for 2-g bottle. After reconstitution, further dilute to 50 to 100 ml with diluent indicated above and infuse over 30 minutes.
• For I.M. administration, reconstitute with an appropriate diluent, such as sterile water for injection or sodium chloride for injection, as follows: for 250-mg vial, add 0.9 ml; for 500-mg vial, add 1.8 ml; for 1-g vial, add 3.6 ml; and for 2-g vial, add 7.2 ml to make a 250-mg/ml concentration. Shake well. Inject deep into large muscle mass, such as the gluteus maximus.
• Monitor BUN and serum creatinine levels to detect early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.
•  Monitor patient for allergic reactions a few days after therapy starts.
• Assess CBC, hematocrit, and serum AST, ALT, bilirubin, LD, and alkaline phosphatase levels during long-term therapy. If abnormalities occur, notify prescriber. Drug may need to be discontinued.
• Assess bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold cefotaxime and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.
• Monitor patient for evidence of gallbladder disease (abdominal pain, nausea, vomiting) because drug may cause ceftriaxonecalcium salt to deposit in the gallbladder, which may mimic gallstones. Expect drug to be discontinued if gallbladder disorders arise.
• Assess for perineal itching, fever, malaise, redness, swelling, rash, and change in cough or sputum; they may indicate a superinfection.
• Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

8.Cefditoren (Spectracef)

Mechanism of Action

 Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes the cell membrane rigid and protective. Without it, bacterial cells rupture and die. This mechanism of action is most effective against bacteria that divide rapidly, including many gram-positive and gram-negative bacteria. Cefditoren isn’t inactivated by beta lactamase produced by some bacteria.

Pharmacokinetics

• Half-Life: 1.2-2 hr
• Peak Plasma Time: 1.5-3 hr
• Excretion: urine

Contraindications

Carnitine deficiency or inborn metabolic disorder that causes it; hypersensitivity to cephalosporins or their components

Adverse Reactions

• CNS: Headache, hyperactivity, hypertonia, seizures
• GI: Abdominal pain, diarrhea, dyspepsia, hepatic dysfunction, nausea, pseudomembranous colitis, vomiting
• GU: Acute renal failure, renal dysfunction, toxic nephropathy
• HEME: Aplastic anemia, hemolytic anemia, hemorrhage, thrombocytopenia
• MS: Arthralgia
• RESP: Pneumonia
• SKIN: Erythema multiforme, StevensJohnson syndrome, toxic epidermal necrolysis
• Other: Allergic reaction, anaphylaxis, carnitine deficiency, drug fever, serum sicknesslike reaction, superinfection

Nursing Considerations

• Cefditoren shouldn’t be used for prolonged treatment because of the risk of carnitine deficiency.
• If possible, obtain culture and sensitivity test results before giving cefditoren.
• Assess patient for evidence of Clostridium difficile infection and pseudomembranous colitis, such as profuse, watery diarrhea. For mild cases, expect to discontinue cefditoren. For moderate to severe cases, expect to also give fluids and electrolytes, protein supplementation, and an antibacterial drug effective against C. difficile.
• If an allergic reaction occurs, expect to discontinue drug, as prescribed. For serious acute hypersensitivity reactions, expect to also give epinephrine, oxygen, and I.V. fluids, antihistamines, corticosteroids, and vasopressors, as prescribed.
• Monitor BUN and serum creatinine levels to detect early signs of renal dysfunction. Also monitor fluid intake and output.
• Watch for a decreased PT, as ordered, in at-risk patients, such as those with renal or hepatic impairment, those with a poor nutritional state, and those receiving anticoagulant or prolonged antibiotic therapy. Notify prescriber if a decrease occurs, and give vitamin K as ordered.

Patient Teaching

•  Urge patient to complete prescribed course of therapy.
•  Instruct patient to take cefditoren with meals to enhance drug absorption.
• Advise patient not to take cefditoren with aluminum- or magnesium-containing antacids or other drugs used to reduce stomach acids because these drugs may interfere with cefditoren absorption.
• Explain that yogurt and buttermilk help maintain normal intestinal flora and can decrease diarrhea during therapy.
• Instruct patient to immediately report severe diarrhea to prescriber.

Cautions

May cause diarrhea, nausea, and vaginal moniliasis (yeast infection); pseudomembranous colitis may occur; clinical manifestations of carnitine deficiency may occur with prolonged use; prolonged use may result in the emergence and overgrowth of resistant organisms; caution in breastfeeding

9.Cefdinir

Mechanism of Action

Interferes with bacterial cell wall synthesis by inhibiting the final step in the crosslinking of peptidoglycan strands. Peptidoglycan makes cell membranes rigid and protective. Without it, bacterial cells rupture and die. Because cefdinir is not degraded by some bacterial beta-lactamase enzymes, it’s effective against many organisms that are resistant to both penicillins and some cephalosporins.

Pharmacokinetics

• Bioavailability: 16-21% (capsule); 25% (suspension)
• Peak plasma time: 2-4 hr
• Plasma protein: 60-70%
• Distribution: Distributed into blister fluid, middle-ear fluid, tonsils, sinus tissue, bronchial mucosa, epithelial lining fluid
• Vd: 0.29-1.05 L/kg (6 months-12 years); 0.06-0.64 L/kg (adults)
• Metabolism: Not appreciably metabolized
• Half-life: 100 min
• Excretion: Urine (7-25% as unchanged drug)

Administration

• Obtain specimens for culture and sensitivity tests as necessary before starting therapy.
• Give with or without food.
• Administer 2 hours before or after iron supplements or antacids containing aluminum or magnesium.
• Give capsules, if possible, to diabetic patients (oral suspension contains 2.86 g of sucrose per teaspoon).

Contraindications

• Hypersensitivity to cephalosporins or penicillins

Precautions:

• Renal impairment, phenylketonuria
• History of GI disease (especially colitis)
• Elderly patients
• Pregnant or breastfeeding patients
• Children.

Adverse reactions

• CNS: headache, lethargy, paresthesia, syncope,seizures
• CV: hypotension, palpitations, chest pain, vasodilation
• EENT: hearing loss
• GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis
• GU: vaginal candidiasis, nephrotoxicity
• Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression Hepatic: hepatomegaly, hepatic failure
• Musculoskeletal: arthralgia
• Respiratory: dyspnea
• Skin: chills, fever, urticaria, maculopapular or erythematous rash
• Other: superinfection, anaphylaxis, serum sickness

Patient monitoring

• Monitor CBC and kidney and liver function test results.
• Monitor for signs and symptoms of superinfection and other serious adverse reactions.

Patient teaching

• Tell patient he may take drug with or without food.
• Instruct patient to report persistent diarrhea (more than four episodes daily) and other adverse effects.
• If patient uses antacids or iron containing preparations (such as iron supplements), tell him to take these 2 hours before or after cefdinir.
• Inform patient that drug may temporarily discolor stools.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

Nursing Considerations

• To reconstitute cefdinir powder for oral suspension, tap bottle to loosen powder, and then dilute with water to 125 mg/ 5 ml. Shake well before each use. Discard any unused portion after 10 days. Keep suspension bottle tightly closed, and store it at room temperature.
• Give antacids that contain aluminum or magnesium and iron salts at least 2 hours before or after cefdinir because they may interfere with cefdinir absorption.
• Monitor patient allergic to penicillin for evidence of hypersensitivity reaction, from a mild rash to fatal anaphylaxis, because cross-sensitivity can occur.
• Monitor patient with a chronic GI condition, such as colitis, for signs and symptoms of a drug-related exacerbation.
• Because all cephalosporins have the potential to cause bleeding, monitor elderly patients and patients with a preexisting coagulopathy, including vitamin K deficiency, for elevated PT or APTT.
• Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold cefdinir and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.
• Assess for other evidence of superinfection, including perineal itching; loose, foul-smelling stools; and vaginal drainage.

REFERENCES

1. Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
2. McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
3. April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
4. Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
5. Nursebro.com, Search – Nursebro

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