Macrolides in Antibiotics

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Questions and Answers

What is the mechanism of action of macrolides?

Macrolides inhibit protein synthesis by binding with the 50s ribosome.

What are three common mechanisms of bacterial resistance to macrolides?

The three common mechanisms of bacterial resistance to macrolides are modification of the ribosomal binding site, production of esterases, and reduced permeability.

What is the antimicrobial spectrum of Erythromycin?

  • Limited to Gram-positive bacteria
  • Similar to Penicillin G (correct)
  • Specific for fungal infections
  • Effective against all bacteria

Which routes of administration are available for Erythromycin?

<p>Oral, intravenous, and topical (B)</p> Signup and view all the answers

What is a common use of Erythromycin?

<p>Erythromycin is often used as an alternative to penicillin for patients who are allergic to penicillin.</p> Signup and view all the answers

What is a major adverse drug reaction associated with macrolides?

<p>Gastrointestinal disturbances, such as epigastric pain, anorexia, nausea, vomiting, and diarrhea, are common adverse drug reactions associated with macrolides.</p> Signup and view all the answers

What are three common adverse drug reactions associated with Erythromycin?

<p>Three common adverse drug reactions associated with Erythromycin are allergic reactions, reversible sensory neural deafness, and thrombophlebitis.</p> Signup and view all the answers

What type of drug interaction is characteristic of Erythromycin?

<p>Erythromycin is a hepatic microsomal enzyme inhibitor, which can lead to QT prolongation, torsades de pointes, and potentially serious ventricular arrhythmias and death.</p> Signup and view all the answers

What is Roxithromycin known for?

<p>Roxithromycin is a long-acting macrolide that is acid-stable and can be administered twice daily.</p> Signup and view all the answers

What is the usual route of administration for Roxithromycin?

<p>Roxithromycin is usually administered orally.</p> Signup and view all the answers

What is the common dose of Roxithromycin?

<p>The common dose of Roxithromycin is 150 mg twice daily, taken before meals.</p> Signup and view all the answers

What is the mode of action of Clarithromycin?

<p>Clarithromycin acts by inhibiting protein synthesis in bacteria, similar to other macrolides.</p> Signup and view all the answers

What are the routes of administration for Clarithromycin?

<p>Clarithromycin can be administered orally or intravenously.</p> Signup and view all the answers

What is the typical dosage of Clarithromycin?

<p>The average dose of Clarithromycin is 250 mg twice daily for 7 days, or 500 mg twice daily for 14 days in severe cases.</p> Signup and view all the answers

What is a noteworthy use for Clarithromycin?

<p>Treating <em>H. pylori</em> infections linked to peptic ulcer disease (C)</p> Signup and view all the answers

How is Azithromycin typically administered?

<p>Azithromycin is typically administered orally, but it can also be given intravenously or as eyedrops.</p> Signup and view all the answers

What is the standard dose of Azithromycin?

<p>The standard dose of Azithromycin is 500 mg once daily.</p> Signup and view all the answers

What are some uses for Azithromycin?

<p>Azithromycin is used for a variety of infections, including Legionnaires' disease, chlamydial infections, chancroid, pertussis, MAC infections in HIV-positive patients, subacute bacterial endocarditis, meningococcal meningitis, and malaria.</p> Signup and view all the answers

What is a notable use for Spiromycin?

<p>Treating toxoplasmosis and cryptosporidiosis (D)</p> Signup and view all the answers

What are some common adverse drug reactions associated with Spiromycin?

<p>The most common adverse drug reactions associated with Spiromycin are nausea, vomiting, diarrhea, and abdominal pain.</p> Signup and view all the answers

What is the main use for Telithromycin?

<p>Telithromycin is commonly used for the treatment of respiratory tract infections.</p> Signup and view all the answers

Which of the following statements about macrolides is true?

<p>Macrolides are a class of antibiotics that inhibit protein synthesis in bacteria. (A)</p> Signup and view all the answers

Macrolides can cause cross-resistance with other antibiotics.

<p>True (A)</p> Signup and view all the answers

Erythromycin is the only macrolide that can be administered topically.

<p>False (B)</p> Signup and view all the answers

Which macrolide is known for its use in treating H. pylori associated peptic ulcer disease?

<p>Clarithromycin (D)</p> Signup and view all the answers

Macrolides are generally contraindicated in pregnancy.

<p>True (A)</p> Signup and view all the answers

The most common adverse drug reaction associated with macrolides is allergic reactions.

<p>False (B)</p> Signup and view all the answers

Macrolides are a newer class of antibiotics developed in the 21st century.

<p>False (B)</p> Signup and view all the answers

The mode of action of macrolides is the same as that of penicillins.

<p>False (B)</p> Signup and view all the answers

All macrolides are effective against Mycobacterium tuberculosis.

<p>False (B)</p> Signup and view all the answers

Macrolides are the only class of antibiotics that can cause QT prolongation.

<p>False (B)</p> Signup and view all the answers

Macrolides are generally considered safe and well-tolerated drugs.

<p>True (A)</p> Signup and view all the answers

Flashcards

Macrolide Antibiotics

A class of antibiotics that inhibit bacterial protein synthesis by binding to the 50S ribosomal subunit, preventing the formation of peptide bonds.

Bacteriostatic

The action of a drug that inhibits bacterial growth but does not kill the bacteria.

Resistance to Macrolides

The ability of bacteria to resist the effects of an antibiotic, often due to mutations in their ribosomes or the production of enzymes that degrade the antibiotic.

Cross-resistance

When a bacterium becomes resistant to one antibiotic, it also often becomes resistant to similar antibiotics in the same drug class.

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Erythromycin

The first macrolide discovered, used for infections like those caused by Streptococcus, Staphylococcus, Mycoplasma, Chlamydia, and some Rickettsia.

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Antimicrobial Spectrum

The spectrum of bacterial species that an antibiotic is effective against.

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Oral Route of Administration

The process of administering medication via the gastrointestinal (GI) tract, either orally (swallowing) or rectally.

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Intravenous Infusion (IV)

The process of administering medication directly into a vein (IV) using a needle.

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Thrombophlebitis

Inflammation or irritation of a vein, often a side effect of IV medications.

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Torsades de Pointes

A condition where the electrical activity of the heart is disrupted, leading to an abnormal, potentially life-threatening heart rhythm.

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Hepatic Microsomal Enzyme

An enzyme in the liver that plays an important role in drug metabolism.

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Hepatic Microsomal Enzyme Inhibitor

The ability of certain drugs to inhibit the activity of hepatic microsomal enzymes, affecting the metabolism of other drugs.

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Roxithromycin

A macrolide with an extended duration of action, allowing for twice-daily dosing.

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Clarithromycin

A macrolide effective against H. pylori, Mycobacterium avium intracellulare, Mycobacterium leprae, and some protozoans.

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Azithromycin

A long-acting macrolide with once-daily dosing, used for a variety of infections, including Legionella, Chlamydia, Pertussis, and Mycobacterium avium complex (MAC).

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Spiramycin

A macrolide used in combination with metronidazole against anaerobic bacteria, particularly effective for infections like Toxoplasmosis and Cryptosporidiosis.

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Telithromycin

A macrolide with once-daily dosing, used for respiratory tract infections.

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Pertussis

A serious infectious disease caused by the bacterium Bordetella pertussis, characterized by violent coughing fits.

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Diphtheria

A serious infection caused by the bacterium Corynebacterium diphtheriae, characterized by a thick, gray membrane in the throat.

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Chancroid

A sexually transmitted infection caused by the bacterium Haemophilus ducreyi, characterized by painful sores on the genitals.

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Chlamydial Infections

A group of infections caused by the bacterium Chlamydia trachomatis, including pneumonia, conjunctivitis, and sexually transmitted infections such as pelvic inflammatory disease.

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Epididymitis

Inflammation of the epididymis, a coiled tube in the testicles, often caused by a sexually transmitted infection.

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Urethritis

Infection or inflammation of the urethra, the tube that carries urine from the bladder to outside the body.

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Pneumonia

Bacterial infection of the lungs, characterized by coughing, fever, and difficulty breathing.

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Pelvic Inflammatory Disease (PID)

A serious infection of the uterine tubes, ovaries, and surrounding pelvic organs, often caused by sexually transmitted infections.

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Conjunctivitis

An inflammation of the conjunctiva, the clear membrane lining the inside of the eyelids and covering the white part of the eye.

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Trachoma

A severe form of conjunctivitis, often caused by Chlamydia trachomatis, that can lead to blindness if left untreated.

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Legionnaire's Disease

A life-threatening infection caused by the bacterium Legionella pneumophila, often spread through contaminated water systems.

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Campylobacter Enteritis

A bacterial infection of the stomach, characterized by nausea, vomiting, diarrhea, and abdominal pain.

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Toxoplasmosis

A parasitic infection caused by Toxoplasma gondii, affecting the brain, eyes, and other organs, often in immunocompromised individuals.

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Cryptosporidiosis

Gastrointestinal infection caused by Cryptosporidium parasites, often transmitted through contaminated water.

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Meningococcal Meningitis

A serious bacterial infection of the meninges, the membranes surrounding the brain and spinal cord, often caused by the bacteria Neisseria meningitidis.

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Syphilis

A bacterial infection caused by Treponema pallidum, a sexually transmitted infection that can have serious consequences if left untreated.

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Gonorrhea

A bacterial infection often caused by Neisseria gonorrhoeae, a sexually transmitted infection that can cause infertility and other complications.

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Typhoid

A bacterial infection caused by Salmonella typhi, a serious illness that can be fatal.

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Study Notes

Macrolides

  • Macrolides are a class of antibiotics.
  • Examples include erythromycin, clarithromycin, roxithromycin, azithromycin, and spiramycin.
  • These antibiotics are bacteriostatic, inhibiting protein synthesis by binding to 50S ribosomes.
  • Resistance mechanisms include modification of ribosomal binding sites, production of esterases, and reduced permeability.
  • Cross-resistance exists between macrolides, clindamycin, and chloramphenicol.
  • Erythromycin has a similar antimicrobial spectrum to penicillin G, active against Gram-positive and Gram-negative bacteria, Mycoplasma, Chlamydia, Rickettsiae, and Spirochetes.
  • Routes of administration for erythromycin include oral (base, estolate, stearate, ethyl succinate), and intravenous (lactobionate and gluceptate).
  • Erythromycin dosage is typically 250-500mg four times a day (q.i.d).
  • Uses of erythromycin include dental infections, periodontal and periapical abscesses, ANUG (acute necrotizing ulcerative gingivitis), post-extraction infections, pertussis, diphtheria, treatment of Corynebacterium diphtheriae, chancroid, and chlamydial infections (e.g., pneumonia, psittaci).
  • Roxithromycin is a long-acting, acid-stable macrolide, dosed twice daily. It is similar to erythromycin in its spectrum.
  • Administration of roxithromycin is oral, with a dose of 150mg twice daily before meals.
  • Oral, intravenous, and eyedrop administrations are options for azithromycin. Its dosage is 500mg once daily.
  • Azithromycin has a wide spectrum of use including chlamydial and legionnaire's pneumonia, epididymitis, NGU (Nongonococcal urethritis), lymphogranuloma venerium, pelvic inflammatory disease, trachoma, infections and chancroid.
  • Clarithromycin usage is similar to erythromycin with additional activities against H. pylori, Mycobacterium avium, intracellular, Mycobacterium leprae, and various protozoa and has broad usage.
  • Its dosage is 250mg twice a day for 7 days, and 500mg twice a day for 14 days in severe cases.
  • Uses of clarithromycin include odontologic infections, atypical pneumonia, H. pylori infections, legionnaire's disease, and MAC infections in HIV patients.
  • Spiramycin is used against anaerobic organisms and is synergistic with metronidazole. It is given orally. Uses include toxoplasmosis, cryptosporidiosis, and chlamydial/gonococcal infections.
  • Telithromycin is a ketolide. It is used orally on a daily basis for various respiratory infections.
  • Adverse reactions may include gastrointestinal problems (nausea, vomiting, diarrhea, abdominal pain, anorexia), hepatotoxicity (jaundice), allergic reactions and hypersensitivity including rashes, pruritis and urticaria), headache and vertigo, and potentially reversible sensory neural deafness.
  • Drug interactions with macrolides can occur, notably with QT prolongation (Torsades de pointes).
  • Some contraindications exist, including pregnancy.

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