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Beta Lactamase Inhibitors and Cephalosporins
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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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    Explore the mechanisms, examples, and classifications of beta lactamase inhibitors and cephalosporins in this comprehensive quiz. Understand the dosage, indications, and similarities with penicillin. Test your knowledge on the different generations of cephalosporins and their respective examples.

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