Antimicrobial Drugs-Penicillins

Name of the Penicillins Drugs

• 1.Pencillins V
• 2.Penicillin G
• 3.Nafcillin
• 4.Oxacillin
• 5.Dicloxacillin
• 6.Amoxicillin
• 7. Carbenicillin
• 8. Ticarcillin
• 9.Piperacillin
• 10.Mezlocillin
• 11.Cefoxitin
• 12.Aziocillin

1.Pencillins V

Pencillins V

Availability Oral solution: 200,000 units (125 mg)/ 5 ml, 400,000 units (250 mg)/5 ml Tablets: 400,000 units (250 mg), 800,000 units (500 mg)

Indications and dosages Upper respiratory streptococcal infections, including scarlet fever and mild erysipelas Adults and children ages 12 and older: 125 to 250 mg P.O. q 6 to 8 hours for 10 days Children younger than age 12: 25 to 50 mg/kg/day P.O. in divided doses q 6 hours for 10 days Pneumococcal respiratory infections, including otitis media Adults and children ages 12 and older: 250 to 500 mg P.O. q 6 hours until afebrile for at least 2 days Skin and soft-tissue staphylococcal infections; fusospirochetosis (Vincent’s infection) of oropharynx Adults and children ages 12 and older: 250 to 500 mg P.O. q 6 to 8 hours To prevent recurrence of rheumatic fever or chorea  Adults and children ages 12 and older: 125 to 250 mg P.O. b.i.d. on a continuing basis

Mechanism of Action

Inhibits final stage of bacterial cell wall synthesis by competitively binding to penicillin-binding proteins inside the cell wall. Penicillin-binding proteins are responsible for various steps in bacterial cell wall synthesis. By binding to these proteins, penicillin leads to cell wall lysis.

Pharmacokinetics

• Bioavailability: 60-73%
• Peak plasma time: 0.5-1 hr
• Protein bound: 80%
• Crosses placenta; poor blood-brain barrier diffusion
• Metabolism: Hepatic
• Half-life: 0.5-0.6 hr
• Excretion: Urine

Administration

• Before giving, ask patient about allergies to penicillin, beta-lactamase inhibitors, or benzathine. Know that crosssensitivity to imipenem and cephalosporins may occur.
• Keep epinephrine and emergency equipment at hand in case anaphylaxis occurs.
• Give with water 1 hour before or 2 hours after meals. Don’t give with fruit juice or carbonated beverages

Contraindications

 Hypersensitivity to penicillin’s or beta-lactamase inhibitors (piperacillin/ tazobactam)

Precautions:

• severe renal insufficiency
• pregnant or breastfeeding patients.

Adverse reactions

• CNS: lethargy, hallucinations, anxiety, depression, twitching, seizures, coma
• GI: nausea, vomiting, diarrhea, epigastric distress, abdominal pain, colitis, blood in stool, glossitis, pseudomembranous colitis
• GU: interstitial nephritis Hematologic: anemia, hemolytic anemia, increased bleeding, leukopenia, granulocytopenia, bone marrow depression, thrombocytopenia, thrombocytopenic purpura
• Metabolic: hypokalemia, hyperkalemia, metabolic alkalosis
• Skin: rash, urticaria
• Other: fever, superinfection, anaphylaxis, serum sickness

Patient monitoring

• Watch for signs and symptoms of anaphylaxis and serum sickness.
•   In long-term therapy, monitor electrolyte levels and CBC with white cell differential; watch for electrolyte imbalances and blood dyscrasias.
• Assess neurologic status, especially for seizures and decreasing level of consciousness.
• Monitor patient closely for signs and symptoms of superinfection and pseudomembranous colitis.

Patient teaching

• Instruct patient to take with water 1 hour before or 2 hours after meals. Tell him not to take with fruit juice or carbonated beverages
• Teach patient to recognize anaphylaxis symptoms. Tell him to immediately contact emergency medical services if these occur.
•  Instruct patient to report signs and symptoms of superinfection.
•  Advise patient to contact prescriber if infection symptoms get worse.
• Tell patient drug may cause diarrhea. Instruct him to immediately report severe, persistent diarrhea and fever.
•  Instruct patient to complete entire course of therapy as prescribed, even after symptoms improve.
•  Tell female patient drug may make hormonal contraceptives ineffective.
• Advise her to use barrier birth-control method if she wishes to avoid pregnancy.
• 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

• Obtain body tissue and fluid samples for culture and sensitivity tests as ordered before giving first dose. Expect to begin drug therapy before test results are known.
• Reconstitute vials of penicillin for injection with sterile water for injection, D5W, or sodium chloride for injection.
• Administer penicillin at least 1 hour before other antibiotics.
• Inject I.M. form deep into large muscle mass. Apply ice to relieve pain.
• Be aware that I.M. drug is absorbed slowly, which may make allergic reactions difficult to treat.
• Assess patient for signs of secondary infection, such as profuse, watery diarrhea. If such diarrhea develops, contact prescriber and expect to obtain a stool specimen to rule out pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold pencillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.
• Monitor serum sodium level and assess for early signs of heart failure in patients receiving high doses of penicillin G sodium.
• When giving penicillin G potassium to patient at risk for hypertension or fluid overload, be aware that each gram of pencillin G potassium also contains 1.02 mEq of sodium

2.Penicillin G

Penicillin G

Availability Oral solution: 200,000 units (125 mg)/ 5 ml, 400,000 units (250 mg)/5 ml Tablets: 400,000 units (250 mg), 800,000 units (500 mg)

Indications and dosages Upper respiratory streptococcal infections, including scarlet fever and mild erysipelas Adults and children ages 12 and older: 125 to 250 mg P.O. q 6 to 8 hours for 10 days Children younger than age 12: 25 to 50 mg/kg/day P.O. in divided doses q 6 hours for 10 days Pneumococcal respiratory infections, including otitis media Adults and children ages 12 and older: 250 to 500 mg P.O. q 6 hours until afebrile for at least 2 days Skin and soft-tissue staphylococcal infections; fusospirochetosis (Vincent’s infection) of oropharynx Adults and children ages 12 and older: 250 to 500 mg P.O. q 6 to 8 hours To prevent recurrence of rheumatic fever or chorea Adults and children ages 12 and older: 125 to 250 mg P.O. b.i.d. on a continuing basis

Mechanism of Action

Inhibits final stage of bacterial cell wall synthesis by competitively binding to penicillin-binding proteins inside the cell wall. Penicillin-binding proteins are responsible for various steps in bacterial cell wall synthesis. By binding to these proteins, penicillin leads to cell wall lysis.

Pharmacology

• Half-Life: 20-30 minutes
• Absorption: IM, slow absorption for up to 24 hr
• Vd: 0.3-0.47 L/kg
• Peak Plasma Time: 2-4 hr
• Peak Plasma Concentration: 1.5 units/mL
• Protein Bound: 60%
• Metabolism: ~30% in liver
• Excretion: urine (60-90% within 24-36 hr)

Administration

• Before giving, ask patient about allergies to penicillin, beta-lactamase inhibitors, or benzathine. Know that crosssensitivity to imipenem and cephalosporins may occur.
• Keep epinephrine and emergency equipment at hand in case anaphylaxis occurs.
• Give with water 1 hour before or 2 hours after meals. Don’t give with fruit juice or carbonated beverages.

Contraindications

Hypersensitivity to penicillins or beta-lactamase inhibitors (piperacillin/ tazobactam)

Precautions:

• severe renal insufficiency
• pregnant or breastfeeding patients.

Adverse reactions

• CNS: lethargy, hallucinations, anxiety, depression, twitching,seizures, coma
• GI: nausea, vomiting, diarrhea, epigastric distress, abdominal pain, colitis, blood in stool, glossitis, pseudomembranous colitis
• GU: interstitial nephritis
• Hematologic: anemia, hemolytic anemia, increased bleeding, leukopenia, granulocytopenia, bone marrow depression, thrombocytopenia, thrombocytopenic purpura
• Metabolic: hypokalemia, hyperkalemia, metabolic alkalosis
• Skin: rash, urticaria
• Other: fever, superinfection, anaphylaxis, serum sickness

Patient monitoring

•  Watch for signs and symptoms of anaphylaxis and serum sickness.
• In long-term therapy, monitor electrolyte levels and CBC with white cell differential; watch for electrolyte imbalances and blood dyscrasias.
• Assess neurologic status, especially for seizures and decreasing level of consciousness. 2Monitor patient closely for signs and symptoms of superinfection and pseudomembranous colitis.

Patient teaching

•  Instruct patient to take with water 1 hour before or 2 hours after meals. Tell him not to take with fruit juice or carbonated beverages.
• Teach patient to recognize anaphylaxis symptoms. Tell him to immediately contact emergency medical services if these occur.
• Instruct patient to report signs and symptoms of superinfection.
• Advise patient to contact prescriber if infection symptoms get worse.
• Tell patient drug may cause diarrhea. Instruct him to immediately report severe, persistent diarrhea and fever.
• Instruct patient to complete entire course of therapy as prescribed, even after symptoms improve.
• Tell female patient drug may make hormonal contraceptives ineffective.

Nursing Considerations

• Obtain body tissue and fluid samples for culture and sensitivity tests as ordered before giving first dose. Expect to begin drug therapy before test results are known.
• Reconstitute vials of penicillin for injection with sterile water for injection, D5W, or sodium chloride for injection.
• Administer penicillin at least 1 hour before other antibiotics.
• Inject I.M. form deep into large muscle mass. Apply ice to relieve pain.
• WARNING Give penicillin G benzathine and penicillin G procaine only by deep I.M. injection; I.V. injection may be fatal, and intra-arterial injection may cause extensive tissue and organ necrosis.
• Be aware that I.M. drug is absorbed slowly, which may make allergic reactions difficult to treat.
• Assess patient for signs of secondary infection, such as profuse, watery diarrhea. If such diarrhea develops, contact prescriber and expect to obtain a stool specimen to rule out pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold pencillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.
• Monitor serum sodium level and assess for early signs of heart failure in patients receiving high doses of penicillin G sodium.
• When giving penicillin G potassium to patient at risk for hypertension or fluid overload, be aware that each gram of pencillin G potassium also contains 1.02 mEq of sodium.

3.Nafcillin

Nafcillin

Availability injectable solution 20mg/mL, 2g/100mL powder for injection 1g, 2g,10g

Indications and Dosages To treat infections caused by penicillinase-producing Staphylococcus aureus CAPSULES, TABLETS Adults and adolescents. 250 to 1,000 mg every 4 to 6 hr. Maximum: 6,000 mg daily. Children over age 1 month. 6.25 to 12.5 mg/kg every 6 hr. Neonates. 10 mg/kg every 6 to 8 hr. I.V. INFUSION Adults and adolescents. 500 to 1,500 mg every 4 hr. Maximum: 20,000 mg daily. Children from birth to age 12. 10 to 20 mg/ kg every 4 hr, or 20 to 40 mg/kg every 8 hr. I.M. INJECTION Adults and adolescents. 500 mg every 4 to 6 hr. Maximum: 12,000 mg daily. Children over age 1 month. 25 mg/kg every 12 hr. Neonates. 10 mg/kg every 12 hr. To treat streptococcal pharyngitis CAPSULES, TABLETS Children. 250 mg every 8 hr. To treat bone and joint infections, endocarditis, meningitis, and pericarditis caused by susceptible organisms I.V. INFUSION Adults and adolescents. 1,500 to 2,000 mg every 4 to 6 hr. Maximum: 20,000 mg daily.  I.V. INFUSION, I.M. INJECTION Children from birth to age 12. 10 to 20 mg/ kg every 4 hr or 20 to 40 mg/kg every 8 hr. For meningitis in neonates weighing up to 2 kg (4.4 lb), 25 to 50 mg/kg every 12 hr for first week after birth and then 50 mg/kg every 8 hr. For neonates weighing 2 kg or more, 50 mg/kg every 8 hr during first week after birth and then 50 mg/kg every 6 hr.

Mechanism of Action

Binds to certain penicillin-binding proteins in bacterial cell walls, thereby inhibiting the final stage of bacterial cell wall synthesis. The result is cell lysis. Nafcillin’s action is bolstered by its chemical composition; its unique side chain resists destruction by beta-lactamases.

Pharmacokinetics

• Half-Life: 0.5-1.5 hr (adults); 0.75-1.9 hr (children)
• Peak Plasma Time: 0.5-1 hr
• Protein binding: 90%
• Absorption: Poorly absorbed orally
• Distribution: In fluid, bone, bile, crosses placenta
• Vd: 0.5-1.5 L/kg
• Metabolism: Liver
• Excretion: Liver (primarily), renal (10-30%)
• Enzymes induced: Hepatic CYP3A4

Contraindications

Hypersensitivity to nafcillin, other penicillins, or their components

Adverse Reactions

• CNS: Depression, headache, seizures
• EENT: Oral candidiasis
• GI: Abdominal pain, diarrhea, nausea, pseudomembranous colitis, vomiting
• GU: Vaginitis
• HEME: Leukopenia, neutropenia
• SKIN: Exfoliative dermatitis, pruritus, rash, urticaria
• Other: Anaphylaxis; hypokalaemia; injection site pain, redness, and swelling; serum sickness like reaction

Nursing Considerations

• Obtain body fluid or tissue samples for culture and sensitivity testing, as prescribed, and obtain test results, if possible, before giving nafcillin, as ordered.
• Give capsules or tablets at least 1 hour before meals or 2 hours afterward.
• For I.M. injection, use only reconstituted solutions from vials. Inject deep into large muscle, preferably upper outer quadrant of gluteus maximus or lateral thigh.
• For intermittent I.V. infusion, infuse over 30 to 60 minutes.
• Give nafcillin at least 1 hour before or after aminoglycosides, especially if patient has renal disease.
• When giving nafcillin to patient at risk for hypertension or fluid overload, be aware that each gram contains 2.5 mEq sodium.
• Monitor serum nafcillin level closely in children, as ordered, because liver and biliary tract, the main routes of nafcillin elimination, function immaturely in children.
• Watch for evidence of superinfection, such as oral candidiasis and pseudomembranous colitis, especially in elderly, immunocompromised, or debilitated patients who receive large doses of nafcillin. If profuse, watery diarrhea develops, contact prescriber and expect to obtain a stool specimen to rule out pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold nafcillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Patient Teaching

• Instruct patient to take nafcillin capsules or tablets on an empty stomach.
• Urge patient to complete entire prescription, even if she feels better.
• Advise patient to notify prescriber if she experiences chills, fever, GI distress, or rash.
• Urge patient to tell prescriber if diarrhea develops, even 2 or ore months after nafcillin therapy ends.

Administration

• Initial therapy for suspected penicillin G-resistant streptococcal or staphylococcal infections.
• Use parenteral therapy initially in severe infections.
• Change to oral therapy as condition warrants. Due to thrombophlebitis, particularly in the elderly, administer parenterally only for short term (1-2 d); change to oral route as clinically indicated.

4.Oxacillin

Oxacillin

Availability infusion solution ,1g/50mL, 2g/50mL powder for injection,1g, 2g, 10g

Indications and Dosages To treat bacteraemia, bone and joint infections (such as osteomyelitis and infectious arthritis), CNS infections (such as ventriculitis and meningitis), endocarditis, septicaemia, skin and soft tissue infections, upper and lower respiratory tract infections, and UTI caused by penicillinase-producing strains of Staphylococcus or other susceptible organisms CAPSULES, ORAL SOLUTION Adults and children weighing 40 kg (88 lb) or more. 500 to 1,000 mg every 4 to 6 hr. Maximum: 6 g daily. Children weighing less than 40 kg. 50 to 100 mg/kg daily in divided doses every 4 to 6 hr To treat mild to moderate infections caused by penicillinase-producing strains of Staphylococcus or other susceptible organisms I.V. INFUSION, I.M. INJECTION Adults and children weighing 40 kg or more. 250 to 500 mg every 4 to 6 hr. Infants and children weighing less than 40 kg. 50 mg/kg daily in divided doses every 4 to 6 hr. Neonates over age 7 days weighing more than 2,000 g. 25 to 50 mg/kg every 6 hr.  Neonates over age 7 days weighing less than 2,000 g. 25 to 50 mg/kg every 8 hr. Neonates age 7 days and under weighing more than 2,000 g. 25 to 50 mg/kg every 8 hr. Neonates age 7 days and under weighing 2,000 g or less. 25 to 50 mg/kg every 12 hr To treat severe infections caused by penicillinase-producing strains of Staphylococcus or other susceptible organisms I.V. INFUSION, I.M. INJECTION Adults and children weighing 40 kg or more. 1,000 mg every 4 to 6 hr  Infants and children weighing less than 40 kg. 100 to 200 mg/kg daily in divided doses every 4 to 6 hr. Neonates over age 7 days weighing more than 2,000 g. 25 to 50 mg/kg every 6 hr. Neonates over age 7 days weighing less than 2,000 g. 25 to 50 mg/kg every 8 hr. Neonates age 7 days and under weighing more than 2,000 g. 25 to 50 mg/kg every 8 hr. Neonates age 7 days and under weighing 2,000 g or less. 25 to 50 mg/kg every 12 hr. To treat endocarditis caused by methicillin-susceptible Staphylococcus aureus in patients without a prosthetic valve I.V. INFUSION Adults. 2 g every 4 hr for 4 to 6 wk To treat endocarditis caused by methicillin-susceptible S. aureus in patients with a prosthetic valve I.V. INFUSION Adults. 2 g every 4 hr for at least 6 wk

Mechanism of Action

Inhibits bacterial cell wall synthesis. In susceptible bacteria, the rigid, cross-linked cell wall is assembled in several steps. Oxacillin affects final stage of cross-linking process by binding with and inactivating penicillin binding proteins (enzymes responsible for linking the cell wall strands). This action causes bacterial cell lysis and death.

Pharmacokinetics

• Half-Life: 23-60 min (adults; prolonged in renal insufficiency); 0.9-1.8 hr (children)
• Peak Plasma Time: 30-60 min
• Protein binding: 94%
• Distribution: Bile, synovial, pleural, peritoneal, pericardial fluids
• Metabolism: Hepatic to active metabolites
• Excretion: Urine and feces

Contraindications

• Hypersensitivity to oxacillin,
• Penicillins, or their components

Adverse Reactions

• CNS: Anxiety, depression, fatigue, hallucinations, headache, seizures
• EENT: Oral candidiasis
• GI: Diarrhea, nausea, pseudomembranous colitis, vomiting
• GU: Interstitial nephritis, vaginal candidiasis
• HEME: Agranulocytosis, anemia, granulocytopenia, neutropenia
• SKIN: Exfoliative dermatitis, pruritus, rash, urticaria
• Other: Anaphylaxis

Nursing Considerations

• Administer oxacillin at least 1 hour before other antibiotics.
• Give oral forms on an empty stomach, preferably 1 hour before or 2 hours after a meal, to prevent impaired absorption.
• Before reconstitution, tap bottle several times to loosen powder. For I.M. injection, reconstitute with sterile water for injection, half-normal (0.45) saline solution, or normal saline solution. Shake until solution is clear.
• For I.V. infusion, reconstitute only with normal saline solution or D5W.
• When giving drug to patient at risk for hypertension or fluid overload, be aware that each gram of oxacillin contains 4.02 mEq of sodium
• Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold oxacillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.

Patient Teaching

• Advise patient to take oxacillin on an empty stomach.
• Instruct patient to notify prescriber immediately should a rash develop.
• Advise female patient who uses an oral contraceptive to use an additional contraceptive method during oxacillin therapy. Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and can be serious, requiring prompt treatment.

5.Dicloxacillin

Dicloxacillin

Availability Capsule 250mg (generic), 500mg (generic)

Indications and Dosages To treat mild to moderate upper respiratory tract and localized skin and soft tissue infections caused by penicillinase producing staphylococci CAPSULES, ORAL SOLUTION  Adults and children weighing 40 kg (88 lb) or more. 125 mg every 6 hr. Children weighing less than 40 kg. 12.5 mg/kg daily divided into four equal doses and given every 6 hr To treat severe infections, such as lower respiratory tract or disseminated infections, caused by penicillinase-producing staphylococci CAPSULES, ORAL SOLUTION Adults and children weighing 40 kg or more. 250 mg every 6 hr, or higher doses, if needed. Maximum: 6 g daily. Children over age 1 month weighing less than 40 kg. 25 mg/kg daily divided into 4 equal doses and given every 6 hr, or higher doses if needed.

Mechanism of Action

Inhibits cell wall synthesis in susceptible bacteria, which assemble rigid, cross-linked cell walls in several steps. Dicloxacillin affects final cross-linking by inactivating penicillin-binding protein (the enzyme needed to link cell wall strands). This action inhibits cell wall synthesis and causes cell lysis and death.

Pharmacokinetics

• Half-Life: 0.6-0.8 hr
• Peak Plasma Time: 0.5-2 hr
• Protein Bound: 96%
• Absorption: 35-76%, decreased by food
• Distribution: widespread, highest in kidneys & liver, CSF low
• Metabolism: hepatic CYP3A4
• Excretion: Urine (56%), feces

Contraindications

 Hypersensitivity to dicloxacillin, other penicillins, beta-lactamase inhibitors (such as piperacillin/tazobactam), cephalosporins, imipenem, or their components

Adverse Reactions

• CNS: Dizziness, fatigue, fever, insomnia
• EENT: Black “hairy” tongue, dry mouth, glossitis, laryngeal edema, laryngospasm, stomatitis, taste perversion
• GI: Abdominal pain, anorexia, diarrhea, flatulence, nausea, pseudomembranous colitis, transient hepatitis, vomiting
• GU: Nephropathy, vaginitis
• MS: Prolonged muscle relaxation
• SKIN: Dermatitis, erythema multiforme, pruritus, rash, urticaria, vesicular eruptions
• Other: Anaphylaxis, serum sicknesslike reaction, superinfection

Nursing Considerations

•  Before dicloxacillin therapy begins, expect to obtain body fluid and tissue samples for culture and sensitivity tests, as ordered, and review the results, if possible. Also check for history of sensitivity to cephalosporins, penicillins, and other substances.
• If diarrhoea develops, notify prescriber; it could be the development of pseudomembranous colitis.

Patient Teaching

• Instruct patient to take drug 1 hour before or 2 hours after meals.
•  Instruct patient to take drug around the clock, not to miss a dose, and to complete the entire prescription unless directed otherwise by prescriber.
• Advise patient to take oral solution with a cold beverage but not acidic juice, such as orange juice. Explain that solution is effective for 7 days at room temperature and for 14 days if refrigerated.
• Caution patient not to open capsules and mix contents with food or liquids because an unpleasant taste and decreased drug absorption will result.
• Instruct parent to shake oral solution thoroughly and measure doses with a calibrated device for accuracy.
• Advise patient to notify prescriber if she experiences adverse GI reactions or signs of hypersensitivity or superinfection.
• If patient takes an oral contraceptive, advise her to use an additional form of contraception during therapy.
• Instruct patient to store drug away from heat, moisture, and direct light and to refrigerate—but not freeze—oral solution.

Cautions

• Monitor PT if patient is taking warfarin concurrently
• Prolonged use may result in superinfection
• Elimination of drug in neonates is slow; use caution

6.Amoxicillin

Amoxicillin

Availability oral suspension, 125mg/5mL, 200mg/5mL, 250mg/5mL, 400mg/5mL capsule 250mg, 500mg Tablet, 500mg, 875mg tablet, chewable 125mg, 250mg

Indications and Dosages To treat ear, nose, throat, GU tract, skin, and soft-tissue infections caused by susceptible gram-positive and gram-negative organisms CAPSULES, CHEWABLE TABLETS, ORAL SUSPENSION, PEDIATRIC DROPS, POWDER OR TABLETS FOR ORAL SUSPENSION, TABLETS Adults and children weighing 20 kg (44 lb) or more. 250 mg every 8 hr; for severe infections, 500 mg every 8 hr or 875 mg every 12 hr. Children age 12 wk and over weighing less than 20 kg. 20 mg/kg daily in divided doses every 8 hr; for severe infections, 40 to 45 mg/kg/day in divided doses every 8 hr.  Children under age 12 wk. 30 mg/kg/ day in divided doses every 12 hr To treat tonsillitis or pharyngitis caused by Streptococcus pyogenes E.R. TABLETS (MOXATAG) Adults and children age 12 and over. 775 mg once dailyfor 10 days, taken within 1 hr of finishing a meal Ø To treat lower respiratory tract infections caused by susceptible gram-positive and gram-negative organisms CAPSULES, CHEWABLE TABLETS, ORAL SUSPENSION, PEDIATRIC DROPS, POWDER OR TABLETS FOR ORAL SUSPENSION, TABLETS Adults and children weighing 20 kg or more. 875 mg every 12 hr; for severe infections, 500 mg every 8 hr. Children age 12 wk and over weighing less than 20 kg. 40 to 45 mg/kg daily in divided doses every 8 hr. Children under age 12 wk. 30 mg/kg daily in divided doses every 12 hr. To treat gonorrhoea and acute uncomplicated anogenital and urethral infections caused by susceptible strains of gram-positive and gram-negative organisms CAPSULES, CHEWABLE TABLETS, ORAL SUSPENSION, POWDER OR TABLETS FOR ORAL SUSPENSION, TABLETS Adults and post pubertal children. 3 g as a single dose. Prepubertal children age 2 and over. 50 mg/kg of amoxicillin plus 25 mg/kg of pro-benecid as a single dose. As adjunct to eradicate Helicobacter pylori to reduce risk of duodenal ulcer recurrence CAPSULES, CHEWABLE TABLETS, ORAL SUSPENSION, POWDER OR TABLETS FOR ORAL SUSPENSION, TABLETS Adults. 1 g every 12 hr with 500 mg of clarithromycin every 12 hr and 30 mg of lansoprazole every 12 hr for 14 days. Or, 1 g every 8 hr with 30 mg of lansoprazole every 8 hr for 14 days To prevent bacterial endocarditis before dental, oral, or upper respiratory tract procedures CAPSULES, CHEWABLE TABLETS, ORAL SUSPENSION, POWDER OR TABLETS FOR ORAL SUSPENSION, TABLETS Adults and children weighing 20 kg or more. 2 g 1 hr before procedure. Children weighing less than 20 kg. 50 mg/ kg 1 hr before procedure.

Mechanism of Action

Kills bacteria by binding to and inactivating penicillin-binding proteins on the inner bacterial cell wall, weakening the bacterial cell wall and causing lysis.

Pharmacokinetics

• Absorption: Rapidly absorbed
• Bioavailability: 74-92%
• Peak plasma time: 2hr (capsule); 3.1 hr (extended-release tab); 1 hr (suspension)
• Distribution: Most body fluids and bone, CSF <1%
• Protein bound: 17-20%
• Metabolism: Hepatic
• Excretion: Urine
• Half-life: 3.7 hr (full-term neonates); 1-2 hr (infants and children); 0.7-1.4 hr (adults)

Contraindications

 Hypersensitivity to amoxicillin or its components

Adverse Reactions

• CNS: Agitation, anxiety, behavior changes, confusion, dizziness, insomnia, reversible hyperactivity, seizures
• CV: Hypersensitivity vasculitis
• EENT: Black, hairy tongue; mucocutaneous candidiasis; tooth discoloration
• GI: Diarrhoea, diarrhoea related to Clostridium difficile, elevated liver enzymes, hemorrhagic or pseudomembranous colitis, jaundice, hepatic dysfunction, nausea, vomiting
• GU: Crystalluria, vaginal mycosis
• HEME: Agranulocytosis, anemia (including haemolytic anaemia), eosinophilia, granulocytosis, leukopenia, thrombocytopenia, thrombocytopenic purpura
• SKIN: Erythema multiforme, erythematous maculopapular rash, generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
• Other: Allergic reaction, anaphylaxis, serum sickness like reaction (such as arthralgia, arthritis, fever, myalgia, rash, and urticaria)

Nursing Considerations

• Patients with mononucleosis shouldn’t receive amoxicillin because this class of drugs may cause an erythematous rash. Use drug cautiously in patients with hepatic impairment. Monitor hepatic and renal function and CBC, as ordered, in patients on prolonged therapy. Also use cautiously in breast-feeding and elderly patients.
• Expect to start therapy before culture and sensitivity test results are known.
• Be aware that chewable tablets and tablets for oral suspension contain phenylalanine.
• Don’t confuse amoxicillin tablets with amoxicillin tablets for oral suspension (DisperMox). They’re not interchangeable. WARNING If allergic reaction occurs, stop amoxicillin immediately and provide emergency care as indicated and ordered.
• Monitor patient closely for diarrhea, which may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber, expect to withhold amoxicillin, and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.
•  Expect treatment that lasts at least 10 days for hemolytic streptococci infections.
• Monitor patient for superinfection. If it occurs, expect to discontinue drug and provide treatment as ordered.

Patient Teaching

• Tell patient to refrigerate reconstituted suspension and to shake well before each use.
•   When amoxicillin suspension is prescribed for a child, instruct parents to place it directly on child’s tongue to swallow. If this doesn’t work, tell parents to mix dose of suspension with formula or cold drink (milk, fruit juice, ginger ale, water) and have child drink it immediately.
• Instruct patient using DisperMox tablets to place one tablet and about 2 teaspoonfuls of water in a glass, drink entire mixture, add more water to the glass, and drink again to ensure delivery of full dose.
•   Tell patient to chew or crush chewable tablets and not to swallow them whole.
• To prevent infection from recurring, urge patient to take amoxicillin for full length of time prescribed, even if he feels better.
• Teach patient to report adverse reactions and notify prescriber if infection worsens or doesn’t improve after 72 hours.
• Urge patient to tell prescriber about diarrhea that’s severe or lasts longer than 3 days. Remind patient that watery or bloody stools can occur 2 or more months after antibiotic therapy and may be serious, requiring prompt treatment.

7. Carbenicillin

Carbenicillin

Availability Each tablet contains carbenicillin indanyl sodium equivalent to 382-764 mg of carbenicillin

Indications and Dosages URINARY TRACT INFECTIONS Escherichia coli, Proteus species, and Enterobacter 1-2 tablets 4 times daily Pseudomonas and Enterococcus 2 tablets 4 times daily PROSTATITIS Escherichia coli, Proteus mirabilis, Enterobacter and Enterococcus 2 tablets 4 times daily

Side effects

• hives,
• difficulty breathing,
• Swelling of your face, lips, tongue, or throat,
• fever,
• pain or difficulty passing urine,
• swollen, back, or “hairy” tongue,
• Stomach cramps
• seizures,
• unusual bleeding,
• easy bruising,
• weakness,
• tiredness, and
• redness, blistering, peeling or loosing of the skin, including inside the mouth

Contraindications

Penicillin allergy.

Mechanism of action

Carbenicillin exerts its antibacterial activity by interference with final cell wall synthesis of susceptible bacteria. Penicillins acylate the penicillin-sensitive transpeptidase C-terminal domain by opening the lactam ring.

Pharmacokinetics

• Absorption: Rapidly absorbed from the small intestine following oral administration. Oral bioavailability is 30 to 40%
• Protein binding: 30 to 60%
• Metabolism: Minimal
• Half-life:1 hour

Adverse Effects

• Hematologic:  anemia, thrombocytopenia, neutropenia, agranulocytosis
• CNS:  seizures
• Renal:  nephrotoxicity, interstitial nephritis
• Hepatic:  transient increases in transaminases
• Other:  Jarisch-Herxheimer Reaction (fever, chills, sweating, tachycardia, hyperventilation, flushing, and myalgia)

Contraindications

Anaphylaxis to carbenecillin or other penicillins

Precautions

Cephalosporin hypersensitivity

Congestive heart failure or hypertension (the sodium content of high doses of parenteral carbenicillin should be considered in patients who require sodium restriction).

Monitoring Requirements

• Therapeutic:  Culture and sensitivities, signs and symptoms of infection
• Toxic:  Periodic CBC, urinalysis, BUN, SCr, AST and ALT, diarrhea, skin rash

8. Ticarcillin

Ticarcillin

Availability Adult and pediatric dosage Injection, powder for reconstitution (3g/100mg)/vial ,(30g/1g)/bulk vial Ready-to-use IV solution(3g/100mg)/100mL

Indications and Dosages Septicemia Adult dosage 3.1 g IV every 4-6 hours Lower Respiratory Infections Adult dosage 3.1 g IV every 4-6 hours Bone & Joint Infections Adult dosage 3.1 g IV every 4-6 hours Skin & Skin Structure Infections Adult dosage 3.1 g IV every 4-6 hours Urinary Tract Infections Adult dosage 3.1 g IV every 4-6 hours Intra-abdominal Infections Adult dosage 3.1 g IV every 4-6 hours Gynecologic Infections Adult dosage Dose based on ticarcillin component Moderate: 200 mg/kg/day IV divided every 4-6 hours  Severe: 300 mg/kg/day IV divided every 4 hours Infections Pediatric dosage Dose based on ticarcillin component Less than 3 months: Safety and efficacy not established Children weighing below 60 kg and above3 months: 200-300 mg/kg/day IV divided q4-6hr; not to exceed 24 g/day Children above 60 kg: As adults; 3.1 g IV every 4-6 hour Neonates (less than 7 days old, weighing below 2 kg) OR (more than 7 days old, weighing below 1.2 kg): 150 mg/kg/day IV divided every 12 hours (less than 7 days old, weighing above 2 kg) OR (more than 7 days old, 1.2-2 kg): 225 mg/kg/day IV divided every 8 hours More than 7 days old, weighing above 2 kg: 300 mg/kg/day IV divided every 8 hours Cystic Fibrosis Pediatric dosage 300-600 mg/kg/day IV/IM divided every 6 hours; not to exceed 24 g/day

Side effects

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• watery or bloody diarrhea,
• Blood in the urine
• feeling an urgent need to urinate,
• fast heart rate,
• light-headedness
• Fainting
• painful or difficult urination              
• easy bruising,
• unusual bleeding,
• unusual weakness,
• Dry mouth
• increased thirst,
• confusion,
• increased urination,
• muscle pain or weakness,
• fast heart rate,

Contraindications

• Allergy  to penicillins or other beta-lactam antibacterials (eg, cephalosporins, imipenem)

Cautions

• Serious and occasionally fatal hypersensitivity reactions reported  
•  clostridium difficile  associated diarrhea was reported with the use of nearly all  antibacterial agents, including ticarcillin
• Seizures were reported when the dose exceeded, especially in presence of renal impairment
• Risk of a bleeding complication                     
• Potential for microbial overgrowth or bacterial resistance
• Laboratory tests: High urine concentrations of ticarcillin may produce false-positive protein reactions; Clavulanate may cause a nonspecific binding of IgG and   albumin  by RBC leading to a false-positive Coombs test
• Hypokalaemia reported
• Monitor renal, hepatic, and hematologic function

Adverse Reactions/Side Effects

• CNS: SEIZURES (HIGH DOSES), confusion, lethargy. 
• CV: CHF, arrhythmias. 
• GI: PSEUDOMEMBRANOUS COLITIS, diarrhea, nausea. 
• GU: hematuria (children only). 
• Derm: rashes, urticaria. 
• F and E: hypokalemia, hypernatremia. 
• Hemat: bleeding, blood dyscrasias, increased bleeding time.
•  Local: phlebitis. 
• Metab: metabolic alkalosis. 
• Misc: HYPERSENSITIVITY REACTIONS, INCLUDING ANAPHYLAXIS, superinfection.

Mechanism of action

Binds to bacterial cell wall membrane, causing cell death. Addition of clavulanate enhances resistance to beta-lactamase, an enzyme that can inactivate penicillins.

Pharmacokinetics

• Absorption: Ticarcillin is administered parenterally since it is poorly absorbed from the gastrointestinal tract
• Distribution: Systemically administered ticarcillin is widely distributed in bodily fluids and tissues.
• Plasma Protein Binding: 45-65%
• Metabolism: Up to 10-15% of an administered dose of ticarcillin is metabolized by hydrolysis.
• Plasma Half-Life :0.93-1.3 hrs
• Elimination: Ticarcillin is rapidly excreted in urine by tubular secretion and glomerular filtration. A portion is excreted in feces by way of the bile 

Contraindications/Warnings/Precautions:

Contraindications:  Anaphylaxis to ticarcillin or other penicillins

Precautions: 

• Cephalosporin hypersensitivity
• History of asthma, or allergic-type reactions to other medications

Monitoring Requirements:

Therapeutic:  Culture and sensitivities, signs and symptoms of infection

Toxic:  Periodic CBC, urinalysis, BUN, SCr, AST and ALT, diarrhea, skin rash

9.Piperacillin

Piperacillin

Availability Powder for injection: 2 g piperacillin and 0.25 g tazobactam/vial, 3 g piperacillin and 0.375 g tazobactam/vial, 4 g piperacillin and 0.5 g tazobactam/vial

Indications and dosages Community-acquired pneumonia; ruptured appendix; peritonitis; pelvic inflammatory disease; skin and skin structure infections Adults and children older than age 12: 3.375 g (3 g piperacillin and 0.375 g tazobactam) I.V. q 6 hours for 7 to 10 days Nosocomial pneumonia Adults and children ages 12 and older: 3.375 g (3 g piperacillin and 0.375 g tazobactam) I.V. over 30 minutes q 4 hours for 7 to 14 days, given with an aminoglycoside

Mechanism of Action

Binds to specific penicillin-binding proteins and inhibits the third and final stage of bacterial cell wall synthesis by interfering with an autolysin inhibitor. Uninhibited autolytic enzymes destroy the cell wall and result in cell lysis.

Administration

• Ask patient about allergy to penicillins, cephalosporins, imipenems, or beta-lactamase inhibitors before giving.
•   Dilute each gram with 5 ml of diluent, such as sterile or bacteriostatic water for injection, normal saline solution for injection, dextrose 5% in water, dextrose 5% in normal saline solution for injection, or 6% dextran in normal saline solution. Don’t use lactated Ringer’s solution.
• Shake vial until drug dissolves. Dilute again to a final volume of 50 ml; infuse over 30 minutes.
• Don’t mix with other drugs. If possible, stop primary infusion while piperacillin infuses.
• Don’t mix in same container with aminoglycosides, which are chemically incompatible with piperacillin.

Pharmacokinetics

• Half-Life: 0.7-1.2 hr
• Protein binding: ~30%
• Metabolism: Hepatic to desethyl metabolite (piperacillin) and inactive metabolite (tazobactam)
• Excretion:  Piperacillin: Urine (68%); feces (10-20%)
• Tazobactam: Urine (80%)
• Both also excreted in bile

Contraindications

 Hypersensitivity to penicillins, cephalosporins, imipenems, or betalactamase inhibitors

 Neonates

Precautions Use cautiously in:

• heart failure, renal insufficiency (in children), seizures, bleeding disorders, uremia, hypokalemia, cystic fibrosis
•  patients with sodium restrictions
•  pregnant or breastfeeding patient
•  children younger than age 12 (safety and efficacy not established).

Adverse reactions

• CNS: headache, insomnia, agitation, dizziness, anxiety, lethargy, hallucinations, depression, twitching, coma, seizures
• CV: hypertension, chest pain, tachycardia
• EENT: rhinitis, glossitis
• GI: nausea, vomiting, diarrhea, constipation, dyspepsia, abdominal pain, pseudomembranous colitis
• GU: proteinuria, hematuria, vaginal candidiasis, vaginitis, oliguria, interstitial nephritis, glomerulonephritis
• Hematologic: anemia, increased bleeding, bone marrow depression, leukopenia, thrombocytopenia
• Metabolic: hypokalemia, hypernatremia Respiratory: dyspnea Skin: rash, pruritus
• Other: fever; pain, edema, inflammation, or phlebitis at I.V. site; superinfection; hypersensitivity reactions including serum sickness and anaphylaxis

Patient monitoring

• Assess neurologic status, especially for seizures.
• Monitor vital signs and fluid intake and output.
• Evaluate electrolyte levels, CBC with white cell differential, and culture and sensitivity tests. Watch for evidence of hypokalemia and blood dyscrasias.
• In patients receiving high doses or prolonged therapy, monitor for signs and symptoms of bacterial or fungal superinfection and pseudomembranous colitis.
• Monitor patient’s dietary sodium intake (drug has high sodium content).
• Immediately report rash, hives, severe diarrhea, black tongue, sore throat, fever, or unusual bleeding or bruising.

Patient teaching

• Tell patient to monitor urinary output and report significant changes.
• Instruct patient to report unusual pain, redness, swelling, or other changes at infusion site.  As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above

Nursing Considerations

• Expect to obtain blood, sputum, or other samples for culture and sensitivity testing before giving piperacillin and to start therapy before results are available.
• Be aware that sunlight may darken piperacillin powder for dilution but won’t alter drug potency.
• For initial dilution for I.V. infusion, reconstitute each gram of drug with at least 5 ml sterile water for injection, sodium chloride for injection, D5W, dextrose 5% in normal saline solution, or bacteriostatic water that contains parabens or benzyl alcohol. Shake solution vigorously after adding diluent and inspect for particles and discoloration before giving.
• For further dilution, use sodium chloride for injection, D5W, dextrose 5% in normal saline solution, lactated Ringer’s solution, or dextran 6% in normal saline solution. Solutions diluted with lactated Ringer’s solution should be given within 2 hours.
• For intermittent infusion, infuse appropriate dose over 20 to 30 minutes.
• Give aminoglycosides 1 hour before or after piperacillin; use a separate site, I.V. bag, and tubing. 
• For I.M. injection, reconstitute each gram of piperacillin with at least 2 ml of an appropriate diluent listed above.
• Don’t give more than 2 g I.M. in one site. Use deltoid area cautiously and only if well developed to avoid injuring radial nerve.
• Watch for bleeding or excessive bruising because drug can decrease platelet aggregation, especially in patients with renal failure. If bleeding occurs, notify prescriber and expect to stop piperacillin.
• Monitor CBC regularly, as ordered, to detect hematologic abnormalities, such as leukopenia and neutropenia.
•  Monitor serum potassium level to detect hypokalemia from urinary potassium loss.
• Check for diarrhea during and after therapy because it may indicate pseudomembranous colitis caused by Clostridium difficile. If diarrhea occurs, notify prescriber and expect to withhold piperacillin and treat with fluids, electrolytes, protein, and an antibiotic effective against C. difficile.
• Watch for hypersensitivity reactions, especially if patient has cystic fibrosis. Notify prescriber, and expect to stop drug.

10.Mezlocillin

Mezlocillin

Indications and Dosages To treat moderate to severe infections, including bacteremia, bone and joint infections, gynecologic infections (such as endometritis, pelvic cellulitis, and pelvic inflammatory disease), intraabdominal infections (such as cholangitis, cholecystitis, hepatic abscess, intraabdominal abscess, and peritonitis), lower respiratory tract infections (such as pneumonia and lung abscess), meningitis, septicemia caused by susceptible bacteria, or skin and soft-tissue infections (such as cellulitis and diabetic foot ulcer); to manage febrile neutropenia I.V. INFUSION, I.M. INJECTION Adults and adolescents. 3 g every 4 hr or 4 g every 6 hr To treat life-threatening infections of the types listed above  I.V. INFUSION, I.M. INJECTION Adults and adolescents. Up to 350 mg/kg daily. Maximum: 24,000 mg daily. Children and infants. 50 mg/kg every 4 hr (or infused over 30 min every 4 hr). Neonates over age 7 days weighing 2,000 g (4.4 lb) or less. 75 mg/kg I.V. every 8 hr. Neonates age 7 days or less weighing 2,000 g or less. 75 mg/kg I.V. every 12 hr. Neonates age 7 days or less weighing more than 2,000 g. 75 mg/kg  I.V. every 6 hr To treat uncomplicated UTI I.V. INFUSION, I.M. INJECTION Adults. 1.5 to 2 g every 6 hr. To treat complicated UTI I.V. INFUSION Adults. 3 g every 6 hr

Mechanism of Action

Inhibits bacterial cell wall synthesis. In susceptible bacteria, the rigid, cross-linked cell wall is assembled in several stages. Mezlocillin affects final stage of cross-linking process by binding with and inactivating penicillin-binding proteins (enzymes responsible for linking cell wall strands). This causes bacterial cell lysis and death.

Contraindications

• Hypersensitivity to mezlocillin, other penicillins, or their components

Adverse Reactions

• CNS: Depression, headache, seizures
• EENT: Oral candidiasis
• GI: Abdominal pain, diarrhea, pseudomembranous colitis, nausea, vomiting
• GU: Vaginitis
• HEME: Leukopenia, neutropenia
• SKIN: Exfoliative dermatitis, pruritus, rash, urticaria
• Other: Anaphylaxis; hypokalemia; injection site pain, redness, and swelling; serum sickness like reaction

Nursing Considerations

WARNING Before starting mezlocillin, make sure patient has had no previous hypersensitivity reactions to penicillins.

• Anticipate that mezlocillin therapy will last for at least 2 days after signs and symptoms have resolved—typically 7 to 10 days, depending on severity of infection. Complicated infections may need longer treatment. Group A beta-hemolytic streptococcal infections usually are treated for at least 10 days to reduce risk of rheumatic fever or glomerulonephritis.
• For I.M. injection, reconstitute each gram of mezlocillin with 3 to 4 ml sterile water for injection and shake vigorously. Inject no more than 2 g into a large muscle, such as the gluteus maximus, over 12 to 15 seconds to minimize discomfort.
• Although drug may be given I.M., expect to use intermittent I.V. infusion, as directed, for serious infections.
• For I.V. use, reconstitute each gram of mezlocillin with 9 to 10 ml sterile water for injection, D5W, or sodium chloride for injection and shake vigorously. Inject directly into I.V. tubing over 3 to 5 minutes.
• For intermittent infusion, further dilute to desired volume (50 to 100 ml) with an appropriate I.V. solution and administer over 30 minutes. Discontinue other infusions during mezlocillin administration.
• Be aware that mezlocillin powder and reconstituted solution may darken slightly but that potency isn’t affected.
• Periodically monitor serum potassium level during long-term therapy, as ordered.
• During long-term therapy, watch for signs and symptoms of superinfection, such as oral candidiasis and vaginitis.

Patient Teaching

• Instruct patient taking mezlocillin to notify prescriber immediately about increased bruising or other bleeding tendencies.
• Advise patient to report diarrhea and to check with prescriber before taking an antidiarrheal medicine because of the risk of masking pseudomembranous colitis.

Precautions: 

• Cephalosporin hypersensitivity
• Patients with mononucleosis are more likely to develop a skin rash
• Coagulation abnormalities (bleeding time, platelet disorders)
• Electrolyte/fluid status (1.85 mEq sodium per gram or Hypokalemia)
• Prolonged neuromuscular blockade if used with vecuronium-type agents

11.Cefoxitin

Cefoxitin

Availability Powder for injection: 1 g, 2 g Premixed containers: 1 g/50 ml in dextrose 5% in water (D5W), 2 g/50 ml in D5W

Indications and dosages Respiratory tract infections, skin infections, bone and joint infections, urinary tract infections, gynecologic infections, septicemia Adults: For most infections, 1 g I.M. or I.V. q 6 to 8 hours. For severe infections, 1 g I.M. or I.V. q 4 hours or 2 g I.M. or I.V. q 6 to 8 hours. For life threatening infections, 2 g I.V. q 4 hours or 3 g I.V. q 6 hours. Children ages 3 months and older: For most infections, 13.3 to 26.7 mg/kg I.M. or I.V. q 4 hours or 20 to 40 mg/kg q 6 hours. Preoperative prophylaxis Adults: 1 to 2 g I.V. within 60 minutes of incision, then q 6 hours for up to 24 hours

Mechanism of Action

Interferes with bacterial cell-wall synthesis and division by binding to cell wall, causing cell to die. Active against gram-negative and gram-positive bacteria, with expanded activity against gram-negative bacteria. Exhibits minimal immunosuppressant activity

Administration

• Obtain specimens for culture and sensitivity testing as necessary before starting therapy.
• Reconstitute 1-g dose with 10 ml of sterile water; reconstitute 2-g dose with 10 to 20 ml.
• For direct I.V. injection, give 10 ml of sterile water with each gram of cefoxitin over 3 to 5 minutes. Inject into large vein and rotate sites or give through existing I.V. tubing.
• For intermittent or continuous I.V. infusion, add reconstituted drug to compatible solution, such as D5W, normal saline solution, or D5W and normal saline solution.
• For I.M. injection, reconstitute each gram with 2 ml of sterile water or 2 ml of 0.5% lidocaine hydrochloride (without epinephrine)
• Inject I.M. deep into large muscle mass; divide 2-g dose in half and inject into separate large muscle masses.
• Know that dry powder and solution may darken, but this does not alter drug efficacy

Pharmacokinetics

• Half-Life: 45-60 min
• Peak Plasma Time: 20-30 min (IM); within 5 min (IV)
• Protein Bound: 65-79%
• Distribution: Widely distributed to body tissues & fluids, including pleural, synovial, ascitic fluid, bile, poor CSF penetration
• Excretion: Unchanged in urine (85%)

Contraindications

• Hypersensitivity to cephalosporins or penicillins
• Precautions Use cautiously in:
• renal impairment, hepatic disease, or biliary obstruction
• history of GI disease
• elderly patients
• children.

Adverse reactions

• CNS: headache, lethargy, paresthesia, syncope,seizures
• CV: hypotension, palpitations, chest pain, vasodilation, thrombophlebitis
• EENT: hearing loss
• GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis
• GU: vaginal candidiasis, nephrotoxicity
• Hematologic: lymphocytosis, eosinophilia, bleeding tendency, haemolytic anaemia, hypoprothrombinaemia, 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. site, anaphylaxis, serum sickness

Patient monitoring

• Assess CBC and kidney and liver function test results.
• Monitor fluid intake and output. Report significant decrease in output.
• 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 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 and tests mentioned above.

Nursing Considerations

• Use cefoxitin cautiously in patients hypersensitive to penicillin; cross-sensitivity has occurred in about 10% of such patients.
• Also use cautiously in patients with a history of GI disease, particularly colitis, because of an increased risk of pseudomembranous colitis.
• If possible, obtain culture and sensitivity test results, as ordered, before giving drug.
• For I.V. use, reconstitute 1 g with 10 ml sterile water for injection or 2 g with 10 to 20 ml diluent.
• For I.V. injection, give slowly over 3 to 5 minutes through tubing of a flowing compatible I.V. solution.Ø For intermittent infusion, further dilute with 50 to 100 ml D5W or normal saline solution.
• For continuous high-dose infusion, add cefoxitin to I.V. solutions of D5W, normal saline solution, or dextrose 5% in normal saline solution.
• For I.M. use, reconstitute each 1 g with 2 ml sterile water for injection.
• Discard unused drug after 24 hours if stored at room temperature or after 1 week if refrigerated.
• Be aware that powder or solution may darken during storage, which doesn’t reflect altered potency.
• Be aware that an allergic reaction may occur a few days after therapy starts.
• Monitor BUN and serum creatinine for early signs of nephrotoxicity. Also monitor fluid intake and output; decreasing urine output may indicate nephrotoxicity.
• Assess patient’s bowel pattern daily; severe diarrhea may indicate pseudomembranous colitis. Assess for pharyngitis, ecchymosis, bleeding, and arthralgia; they may indicate a blood dyscrasia.

12.Aziocillin

Aziocillin

Dosage Gram-negative infections:  2 to 5 grams every 8 hours IV Serious infections:  225 to 300 mg/kg/day IV in 4 to 6 divided doses (usual IV doses 3g q4h or 4g q6h) (up to 18 g/day)

Mechanism of Action

Exerts bactericidal activity via inhibition of bacterial cell wall synthesis by binding one or more of the penicillin binding proteins (PBPs).  Exerts bacterial autolytic effect by inhibition of certain PBPs related to the activation of a bacterial autolytic process.

Pharmacokinetics

• Distribution:  Total protein binding: 30 to 40%;
• Distribution sites:  aqueous humor, bile, bone, CSF, lungs, urine
• Volume of distribution:  14 L
• Excretion:  Renal excretion: 60 to 75%; elimination half-life: 1.53 hours

Adverse Effects

• Hematologic:  anemia, thrombocytopenia, neutropenia, agranulocytosis
• Endocrine:  hyperthermia
• Renal:  nephrotoxicity, interstitial nephritis
• Hepatic:  transient increases in transaminases
• Other:  Jarisch-Herxheimer Reaction (fever, chills, sweating, tachycardia, hyperventilation, flushing, and myalgia)

Contraindications/Warnings/Precautions

Contraindications:  Anaphylaxis to azlocillin or other penicillins

Precautions: 

• Cephalosporin hypersensitivity
• Patients with mononucleosis are more likely to develop a skin rash
• Patients with restricted salt intake; each gram of azlocillin contains 2.17 mEq of sodium
• Renal insufficiency

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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