Beta Lactamase Inhibitors and Cephalosporins
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Questions and Answers

What is the primary mechanism of action for B-lactamase inhibitors?

  • Inhibit protein synthesis
  • Block the B-lactamase enzyme (correct)
  • Increase penicillin resistance
  • Enhance drug absorption

    • Which class of antibiotics would you expect to treat Klebsiella infections?

  • Cephalosporins (correct)
  • Macrolides
  • Aminoglycosides
  • Tetracyclines

    • What is a known side effect of Ceftriaxone?

  • Dry mouth
  • Hepatotoxicity
  • Hypotension
  • Nephrotoxicity (correct)

    • Which medication combination helps to mitigate the nephrotoxic effects of imipenem?

    <p>Cilastatin</p> Signup and view all the answers

    For which patient scenario is Ceftriaxone particularly indicated?

    <p>Treatment of gonorrhea</p> Signup and view all the answers

    What is the primary mechanism of action of Isoniazid?

    <p>Inhibiting mycobacterial biosynthesis of mycolic acid</p> Signup and view all the answers

    What dose is recommended for oral adult patients taking amoxicillin combined with a B-lactamase inhibitor?

    <p>375 mg three times daily</p> Signup and view all the answers

    Which of the following is NOT a side effect of Rifampicin?

    <p>Peripheral neuritis</p> Signup and view all the answers

    Which of the following cephalosporins belongs to the first generation?

    <p>Cefalexin</p> Signup and view all the answers

    What is the recommended dose of Isoniazid for adults?

    <p>5 mg/kg/day</p> Signup and view all the answers

    What route of administration is common for carbapenems?

    <p>Intravenous or intramuscular</p> Signup and view all the answers

    Which condition is a contraindication for using Isoniazid?

    <p>Liver disease</p> Signup and view all the answers

    What is a key nursing responsibility for patients taking Rifampicin?

    <p>Informing them about the potential orange-red discoloration of bodily secretions</p> Signup and view all the answers

    What is the classification of Rifampicin?

    <p>Anti tuberculosis</p> Signup and view all the answers

    What is the primary reason for combining Isoniazid and Rifampicin in tuberculosis treatment?

    <p>To increase treatment efficacy</p> Signup and view all the answers

    Which of the following is a true statement regarding Leprosy?

    <p>It is caused by Mycobacterium leprae and transmitted by prolonged contact</p> Signup and view all the answers

    What is the mechanism of action of diloxanide furoate?

    <p>Inhibition of protein synthesis</p> Signup and view all the answers

    Which of the following conditions is a contraindication for using certain medications mentioned?

    <p>CNS disease</p> Signup and view all the answers

    What should be monitored in patients taking lithium during treatment?

    <p>Elevated lithium levels</p> Signup and view all the answers

    Which is a common side effect of diloxanide furoate?

    <p>Skin rash</p> Signup and view all the answers

    What is the primary mechanism through which chloroquine acts against malaria?

    <p>Increasing pH in the acidic food vacuole</p> Signup and view all the answers

    In the treatment of malaria, which drug is the mainstay for erythrocytic P. falciparum malaria?

    <p>Chloroquine</p> Signup and view all the answers

    What is the effect of chloroquine on heme within the malaria parasite?

    <p>It prevents heme polymerization to hemazoin.</p> Signup and view all the answers

    Which type of malaria is chloroquine less effective against?

    <p>P. vivax</p> Signup and view all the answers

    What is the mechanism of action of allylamines such as terbinafine?

    <p>Inhibits ergosterol synthesis by inhibiting squalene epoxidase</p> Signup and view all the answers

    Which of the following conditions is a contraindication for the use of micafungin?

    <p>Chronic hepatic disease</p> Signup and view all the answers

    For which infection is terbinafine primarily indicated?

    <p>Onychomycosis of toe</p> Signup and view all the answers

    What nursing responsibility is essential when administering allylamines?

    <p>Do not administer to breastfeeding mothers</p> Signup and view all the answers

    What side effect is common with both allylamines and beta-glucan synthesis inhibitors?

    <p>Neutropenia</p> Signup and view all the answers

    What is the main clinical indication for micafungin?

    <p>Candidiasis in patients intolerant to azoles</p> Signup and view all the answers

    Which of the following is a recommended nursing action prior to administration of micafungin?

    <p>Assess for signs of hepatic disease</p> Signup and view all the answers

    What is the recommended dosage of terbinafine for treating onychomycosis?

    <p>250mg four times daily for 6 weeks</p> Signup and view all the answers

    What is the primary action of Methenamine in treating urinary tract infections?

    <p>It hydrolyzes into formaldehyde which is toxic to bacteria.</p> Signup and view all the answers

    Which of the following best describes a contraindication for Methenamine use?

    <p>Renal insufficiency</p> Signup and view all the answers

    Which statement about Ciprofloxacin is accurate?

    <p>It is recommended to be taken without food to accelerate absorption.</p> Signup and view all the answers

    In addition to Escherichia coli, which other pathogen is most commonly associated with urinary tract infections?

    <p>Staphylococcus saprophyticus</p> Signup and view all the answers

    How does Methenamine achieve its bacteriostatic effect in the urinary tract?

    <p>By releasing formaldehyde in an acidic environment.</p> Signup and view all the answers

    What should be monitored to ensure optimal action of Methenamine?

    <p>Urine pH level</p> Signup and view all the answers

    What is a common adverse effect of Methenamine?

    <p>Gastritis</p> Signup and view all the answers

    What is the recommended patient hydration strategy when administering Ciprofloxacin?

    <p>Consume copious fluids to prevent crystal urea formation.</p> Signup and view all the answers

    Study Notes

    Beta Lactamase Inhibitors

    • Beta lactamase inhibitors are agents that prevent beta-lactam enzymes from destroying beta-lactam molecules.
    • Examples include clavulanic acid and amoxicillin.
    • They act by blocking the beta-lactamase enzyme, rendering the organism susceptible to amoxicillin.
    • They have a rapid bacterial effect at concentrations obtainable in the body.
    • Indications, side effects, contraindications, and routes of administration are similar to penicillin.
    • Oral dose for adults is 375mg three times a day or 625mg twice a day.
    • Oral dose for children aged 2-6 years is 5ml of a 225mg/5ml solution.

    Cephalosporines

    • There are five generations of cephalosporines.
      • First generation: Cephalexin, Ceohalothin, Cephadrine
      • Second generation: Cefaclor, Cefuroxime, Cefdroxil
      • Third generation: Ceftriaxone, Cefixime, Cefpodoxime
      • Fourth generation: Cefepime, Cefpirome
      • Fifth generation: Ceftaroline

    Ceftriaxone

    • Class: Cephalosporines
    • Mechanism of action: Similar to penicillin
    • Indications: Klepsiella, enterobacter, H-influenza, proteus
    • It's a drug of choice in the treatment of gonorrhea, as well as meningitis in adults and children under 3 months.
    • Side effects: Abdominal pain, nephrotoxicity, rashes
    • Contraindications: Hypersensitivity reaction
    • Route of administration: Intravenous, intramuscular
    • Dose: 1-2 grams daily

    Cephalexin

    • Class: Cephalosporines
    • Dose: 250-500mg every 6 hours

    Cefixime

    • Dose: Adults and children over 10 years should receive 200-400mg daily.
    • Children 6 months to 10 years should receive 8mg/kg in divided doses.
    • Dose for gonorrhea is 100mg in divided doses.
    • Dose for children 5-10 years is 20mg daily.

    Carbapenems

    • Examples include Doripenem, Imipenem, Ertapenem, Meropenem.
    • Imipenem is susceptible to degradation by the enzyme called dehydro-peptidase 1, found in the border of the renal tubules.
    • This enzyme forms an inactive metabolite that is potentially nephrotoxic.
    • Cilastin blocks the metabolism of imipenem in the kidney, preventing toxicity.
    • Cilastin has no antimicrobial activity.
    • Side effects: Nausea, vomiting, diarrhea, skin rashes, seizures, liver and renal failure.
    • Dose: 0.25-0.5g in divided doses.
    • Doripenem dose: 0.5g every 4 hours.
    • Meropenem dose: 0.5g-1g every 8 hours.
    • Indications: Similar to cephalosporines.
    • Contraindications: Hypersensitivity reaction.
    • Mechanism of action: Similar to cephalosporines.
    • Nursing responsibilities Similar to cephalosporines.

    Ciprofloxacin

    • Ciprofloxacin is used to treat a disease after 7-10 days.

    Urinary Tract Antiseptics/Antimicrobials

    • Urinary tract infections (UTIs) in women of childbearing age and the elderly are common problems.
    • Escherichia coli is the most common pathogen.
    • Staphylococeus saprophyticus is the second most common bacterial pathogen causing UTIs.
    • Other pathogens include Klebsiella pneumonia and proteus mirabilis.

    Drug Treatment

    • Drugs include Methenamine, Nitrofurantoin, Quinolones, and Nalidixic acid.
    • These drugs inhibit bacterial growth in urine because they are concentrated in the renal tubules.

    Methenamine (Hexamethylene Tetramine)

    • Group: Hexamethylene tetramine
    • Mechanism of action: The drug hydrolyzes to formaldehyde, which is toxic to most bacteria.
    • It is active in an acidic environment (pH ≤ 6).
    • It acts by denaturing proteins and nucleic acids of bacteria.
    • Indications: Urinary tract infection prophylaxis. It has no antibacterial activity in tissue or blood.
    • Route of administration: Oral
    • Dose: Children 6-12 years: 1g every 12 hours. Adults: 1g twice to four times daily.
    • Various agents are used to acidify urine, including ascorbic acid (vitamin C).
    • Low pH alone is bacteriostatic.
    • Adverse effects: Gastritis, chemical cystitis, hematuria, dysuria, nausea, decreased appetite, skin rash.
    • Contraindications: Renal insufficiency, liver disease, severe dehydration. Do not combine with sulphonamide as it reacts with formaldehyde.

    Nursing Responsibilities for Methenamine

    • Monitor urine pH (optimum drug action requires a pH of ≤5.1).
    • Monitor input and output ratio and pattern (the drug is ineffective when fluid intake is maintained at 1500-1200ml).
    • Copious amounts of fluids can increase diuresis, elevate urine pH, and dilute formaldehyde concentration.

    Anti TB Drugs

    • Regimen means combining drugs for a certain duration.
    • Anti-TB drugs undergo resistance more than any other drugs.

    Isoniazid/Isonicotinic Hydrazide (INH)

    • Class: Anti-TB
    • Mechanism of action: It inhibits the biosynthesis of mycotic acid in mycobacteria.
    • It is a prodrug activated by an enzyme called mycobacterium catalase peroxidase (kat-G).
    • The active form forms acyl carrier protein (acp-m) and keto beta acyl carrier protein, which inhibit the synthesis of mycolic acid.
    • Indications: Management of all forms of TB
    • Side effects: Isoniazid can induce hepatitis, anemia, fever, chills, peripheral neuritis, and rashes.
    • Contraindications: Pregnancy, liver disease, and renal disease.
    • Dose: 5mg/kg/day.
    • Route of administration: Oral and intravenous.

    Rifampicin

    • Class: Anti-TB
    • Mechanism of action: It inhibits the DNA-dependent, RNA polymerase of sensitive bacteria, thereby inhibiting RNA synthesis.
    • Indications: Co-administered with isoniazid in the management of tuberculosis
    • Side effects: Nausea and vomiting, fever, myalgia, hemolytic anemia, shock, orange-red color discoloration, jaundice.
    • Route of administration: Oral
    • Dose: Available alone or as a fixed-dose combination with isoniazid (150mg isoniazid and 300mg rifampicin).
    • This combination is the most effective method for managing tuberculosis.
    • It can be administered 1 hour before a meal or 2 hours after a meal.
    • For children over 12 years, the dose is 10-15mg/kg body weight.
    • Contraindications: Jaundice due to reduced bilirubin, the first trimester of pregnancy, liver disease.

    Nursing Responsibilities for Rifampicin

    • Inform the patient that the drug causes a brownish-yellow discoloration in secretions like saliva and urine and that they should not discontinue the drug.

    Anti-Leprosy

    • Leprosy is a chronic disease prevalent in tropical countries, especially India, the Philippines, and Brazil.
    • It is a public health problem.
    • The disease was first identified by a Norwegian physician, G.A. Hansen, in 1873 and is also known as "Hansen's disease."
    • Transmission occurs through close and prolonged contact via inhalation of bacilli present in nasal secretions or through skin erosions.
    • Nursing interventions: Do not administer with antacids, H2 blockers, proton pump inhibitors, or ketoconazole as they require an acidic environment for absorption. If antacids are needed, administer at least 2 hours apart. Continue long-term therapy until the infection is eradicated. Monitor hepatic function more frequently throughout treatment.

    Allylamines

    • Examples: Amorolfin, Terbinafin, Naftifine.
    • Group: Antifungal, antimycotic agent.
    • Class: Allylamine
    • Mechanism of action: Inhibits ergosterol synthesis by inhibiting the enzyme called squalene epoxidase.
    • Clinical indications: Onychomycosis of the toe and ringworm infection, dermatophyte infection
    • Side effects: Abdominal pain, anorexia, diarrhea, dyspepsia, rash, vomiting, headache, neutropenia
    • Contraindications: Chronic or active hepatic disease, hypersensitivity, lactating mothers.
    • Route of administration: Topical, oral.
    • Dosage: 250mg four times a day for six weeks.

    Nursing Responsibilities for Allylamines

    • Do not give to breastfeeding mothers.
    • Notify the physician if the drug causes increased skin irritation or sensitivity.
    • Learn the correct technique for application.

    Inhibitors of Beta Glucan Synthesis

    • They are made up of three groups: Echinocandins, Aculeacins, Papilafungins.
    • Echinocandins are also made up of three drugs: Micafungins, Anidulufungin, Caspofungin.

    Micafungins

    • Group: Antimycotic agent
    • Class: Inhibitors of beta glucan synthesis
    • Mechanism of action: Inhibits beta (1-3) glucan synthesis. This enzyme, glucan synthase, is essential for the integrity of the fungal cell wall. This inhibits the production of the pathogen.
    • Clinical indications: Candida. Its spectrum of activity is limited. It's a second-line drug for patients who cannot tolerate azoles or amphotericin B.
    • Side effects: Rash, gastrointestinal disturbances, fever, headache, flushing, plebitis.
    • Route of administration: Intravenous
    • Dosage: 150mg per day.
    • Contraindications: Hepatic insufficiency, intravascular hemolytic, hypersensitivity

    Nursing Responsibilities for Micafungins

    • Monitor for signs of anaphylaxis (rash, pruritus, wheezing, laryngeal edema, abdominal pain)
    • Check for hepatic disease before administration
    • Assess for injection site reaction (phlebitis, thrombophlebitis)

    Inhibitors of Nucleic Acid, Antimetabolite

    • Group: Antifungal
    • Dosage: Metronidazole 750mg three times daily or 500mg intravenously every 6 hours for 10 days, or Tinidazole 2g daily for 3 days, plus a luminal agent 650mg three times daily.
    • Contraindications: Central nervous system disease, blood dyscrasias, pregnancy, Phenytoin and Phenobarbital, lithium.

    Diloxanide Furoate

    • Dosage: 500mg three times daily for ten days.
    • Mechanism of action: Inhibits protein synthesis
    • Side effects: Flatulence, nausea, abdominal cramps, and rashes.
    • Contraindication: Pregnancy

    Nursing Responsibilities for Diloxanide Furoate

    • Discontinue the drug if symptoms of CNS toxicity develop.
    • Monitor patients on lithium for elevated lithium levels.
    • Repeat fecal examinations up to three times to ensure elimination.
    • Refrain from intercourse during drug therapy unless using condoms to prevent reinfection.
    • Do not drink alcohol during drug therapy.
    • Do not breastfeed while taking the drug.

    Malaria

    • Malaria is an acute infectious disease caused by four species of the protozoa genus Plasmodium.
    • It is transmitted to humans through the bites of female Anopheles mosquitoes.
    • Anopheles mosquitoes thrive in humid, swampy areas.
    • Plasmodium falciparum is the most dangerous species, causing an acute, rapidly fulminating disease.
    • P. falciparum infection is characterized by persistent high fever, orthostatic hypotension, and massive erythrocytosis.
    • Classification of anti-malaria agents:
      • Aryl amino compounds: Quinine, Quinidine, Chloroquine, Amodauine, Mefloamine, Halofantrin, Lumefantrin, Pipequine, Tafenaquine.
      • Antifolates compounds: Pyrimethamine, Proguanil, Chloroproguanil, Trimetropim.
      • Artemisinin compounds: Artemisinin, Dehydroartemisinin, Artemeter, Artesunate.
      • Others: Atovaquone.
      • Antibacteria: Clindamycin, Tetracycline.

    Chloroquine

    • Chloroquine is a synthetic blood schizonticide, a 4-aminoquinolone that has been the mainstay of antimalaria therapy.
    • It is a drug of choice in the treatment of erythrocytic P. falciparum malaria, except in resistant strains.
    • It is less effective against P. vivax malaria.
    • It is highly specific for the sexual form of plasmodia.
    • Mechanism of action: After transferring into the erythrocyte and plasmodium membrane, chloroquine (a diprotic weak base) is concentrated in the organism's acidic food vacuole primarily by ion trapping.
    • The parasite digests host hemoglobin in the acidic food vacuole to obtain essential amino acids.
    • Chloroquine specifically binds to heme, preventing its polymerization into hemozoin.
    • The increased pH and accumulation of heme leads to oxidative damage to the membrane, resulting in the lysis of both the parasite and red blood cells.

    Therapeutic Use/Indication

    • Chloroquine's therapeutic use is for the management of malaria.
    • It is indicated for the treatment of uncomplicated malaria and is used as chemoprophylaxis.

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