Macrolides

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Questions and Answers

Which of the following are within the subfamily macrolides?

  • Erythromycin (correct)
  • Tulathromycin (correct)
  • Tylosin
  • Clarithromycin (correct)

Can you list all of the drugs within the subfamily macrolides?

Erythromycin, clarithromycin, tylosin, tilmicosin and tildipirosin

What drugs are in the subfamily azalides?

Azithromycin and gamithromycin

Which of the following macrolides is classified as a triamilide?

<p>Tulathromycin (C)</p> Signup and view all the answers

What is the ranking of macrolides in the World Health Organization's list of medically important antimicrobials?

<p>Critically important</p> Signup and view all the answers

What is a key characteristic of macrolide molecules?

<p>Large lactones with 13 to 16 carbons (B)</p> Signup and view all the answers

Choose the correct description of Macrolides regarding their chemistry and formulation

<p>Liposoluble (A), Weak base (D)</p> Signup and view all the answers

Why are azalides and triamilides less liposoluble in acidic environments?

<p>They become ionized, reducing their ability to pass through bacterial membranes (B)</p> Signup and view all the answers

Which macrolide is known for being extremely sensitive to pH, leading to inactivation?

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

Which macrolide is coated for oral administration in order to prevent degradation in the stomach?

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

The oral bioavailability of macrolides is variable between the molecule and their formulations.

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

Which erythromycin formulation is best absorbed intact from the intestine?

<p>Erythromycin estolate (C)</p> Signup and view all the answers

Injectable macrolides have better bioavailability

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

Why do injectable macrolides have better bioavailability than oral formulations?

<p>They avoid first-pass metabolism (A)</p> Signup and view all the answers

What is a key distribution characteristic of macrolides?

<p>Large volume of distribution (Vd) (A)</p> Signup and view all the answers

Pharmacokinetics: Distribution of macrolides

<p>Well distributed in most tissues (A), Highly liposoluble (C)</p> Signup and view all the answers

Which statement is true about macrolide distribution in leukocytes?

<p>They concentrate in leukocytes, making them effective against intracellular pathogens (B)</p> Signup and view all the answers

What effect does the weak base nature of macrolides have on their distribution?

<p>It leads to ion trapping in acidic environments like milk, CSF, and purulent material (B)</p> Signup and view all the answers

What macrolide is noted to have lung concentrations higher than concentration in the liver and kidneys in food animals?

<p>Tulathromycin (C)</p> Signup and view all the answers

Which macrolide has the highest lung concentration compared to liver and kidney concentrations in food animals?

<p>Tulathromycin (C)</p> Signup and view all the answers

Which group of macrolides is known to concentrate more than other macrolides in acidic environments such as milk, cerebrospinal fluid (CSF), gastric fluids, purulent material, and prostatic fluid?

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

How are most macrolides metabolized?

<p>Primarily by the liver (B)</p> Signup and view all the answers

Which macrolide is highly metabolized and undergoes enterohepatic circulation?

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

Which macrolide has a short half-life due to extensive metabolism?

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

Which group of macrolides has a longer half-life due to reduced metabolism?

<p>Azalides (Azithromycin, Gamithromycin) (B)</p> Signup and view all the answers

Which macrolides interfere with cytochrome P450 enzymes, leading to drug interactions?

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

How are most macrolides eliminated from the body?

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

Which macrolide has the longest half-life and is excreted mainly unchanged in bile?

<p>Tilmicosin (C)</p> Signup and view all the answers

Why is the use of extra-label long-acting macrolides discouraged in dairy cattle?

<p>Long-lasting residues may occur (C)</p> Signup and view all the answers

What effect does enterohepatic circulation have on macrolides like erythromycin?

<p>It increases their half-life (A)</p> Signup and view all the answers

Which macrolide requires dosage adjustment in renal disease due to partial renal excretion?

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

The use of ELDU in long-acting macrolide formulations in dairy cattle is strongly encouraged

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

Which of the following drugs should not be combined with erythromycin due to its interference with cytochrome P450 enzymes?

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

Why are erythromycin and other macrolides commonly administered with rifampin?

<p>To enhance antimicrobial synergism and reduce resistance development (A)</p> Signup and view all the answers

What effect does the co-administration of rifampin have on clarithromycin in foals?

<p>It significantly decreases the oral bioavailability of clarithromycin (B)</p> Signup and view all the answers

What is the primary mechanism of action of macrolides?

<p>Binding to the 50S ribosomal subunit to prevent protein synthesis (C)</p> Signup and view all the answers

How do macrolides interfere with bacterial protein synthesis?

<p>They prevent the enzyme peptidyltransferase from adding amino acids to the growing peptide chain (B)</p> Signup and view all the answers

What pharmacodynamic property determines whether macrolides act as bacteriostatic or bactericidal agents?

<p>AUC/MIC ratio (B)</p> Signup and view all the answers

Macrolides are most active in which type of environment?

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

Aside from their antimicrobial properties, macrolides also have what non-antimicrobial effects?

<p>Modulation of inflammatory mediators and gastrointestinal motility (B)</p> Signup and view all the answers

Why should extreme care be taken when administering macrolides to foals with respiratory disease during hot weather?

<p>Macrolides induce hyperthermia and anhidrosis (inability to sweat) (A)</p> Signup and view all the answers

Which macrolide has the highest potential for cardiotoxicity, especially if administered intravenously in cattle or other species?

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

Why is the routine use of epinephrine NOT recommended in cases of tilmicosin toxicity in swine?

<p>Epinephrine potentiates the lethality of tilmicosin by exacerbating tachycardia and myocardial depression. (B)</p> Signup and view all the answers

Which treatment options may be effective in reversing the cardiovascular effects of intravenous tilmicosin toxicity?

<p>Calcium chloride and intravenous lipid emulsion infusion (C)</p> Signup and view all the answers

Why should tilmicosin only be administered subcutaneously (SC) in ruminants?

<p>To avoid severe tissue necrosis and carcass damage (B)</p> Signup and view all the answers

Why are most macrolides administered intravenously (IV), subcutaneously (SC), or orally (PO) rather than intramuscularly (IM)?

<p>IM injection causes severe irritation and pain at the injection site. (B)</p> Signup and view all the answers

Which macrolide is an exception to injection site reactions and is given subcutaneously (SC) in cattle and intramuscularly (IM) in swine?

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

What are macrolides spectrum of activity?

<p>Broad spectrum</p> Signup and view all the answers

The macrolide, _____________, is more active against staphylococci, streptococci, Chlamydia and R. equi

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

Which macrolide is more active against Gram-negative bacteria and anaerobes compared to erythromycin?

<p>Azithromycin (C)</p> Signup and view all the answers

Which two macrolides are active against Helicobacter spp?

<p>Clarithromycin and azithromycin</p> Signup and view all the answers

Which macrolide has high activity against Gram-negative respiratory pathogens and Mycoplasma bovis in vitro?

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

Bacterial resistance to macrolides develops quickly from _________________.

<p>repeated exposure</p> Signup and view all the answers

Which of the following is NOT a common mechanism of bacterial resistance to macrolides?

<p>Increased bacterial cell wall synthesis (D)</p> Signup and view all the answers

What is a major concern with the widespread use of macrolides in both human and veterinary medicine?

<p>Extensive cross-resistance between macrolides</p> Signup and view all the answers

Which formulation of erythromycin is labeled for use in both food animals and small animals?

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

What is the labeled formulation of erythromycin for dairy cattle?

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

There are multiple injectable and oral formulations of macrolides approved in food animals

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

Which macrolide is available as an injectable formulation for subcutaneous (SC) use in cattle and sheep and as an oral premix for swine and cattle?

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

Tulathromycin is labeled for administration via which routes in cattle and swine?

<p>SC in cattle, IM in swine (B)</p> Signup and view all the answers

The macrolide __________, is also labeled for SC administration in beef cattle

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

Erythromycin has multiple clinical uses in small animals. What has erythromycin been used to treat?

<p>Pyodermas, bacterial enteritis, osteomyelitis, and soft tissue infections</p> Signup and view all the answers

Which macrolide is commonly used in cats for treating Chlamydophila and Mycoplasma respiratory infections?

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

Why is azithromycin often preferred over erythromycin in small animals?

<p>It requires less frequent dosing and has fewer gastrointestinal side effects (B)</p> Signup and view all the answers

What is erythromycin recommended for in small animals?

<p>Treatment of Campylobacter enteritis (A)</p> Signup and view all the answers

Why is erythromycin usually limited to foals for the treatment of Rhodococcus equi infections?

<p>It is associated with potentially fatal colitis in adult horses (B)</p> Signup and view all the answers

Which two macrolides are considered the newest “one-shot” treatments for bovine respiratory disease (BRD) in beef cattle?

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

What is a key reason tulathromycin is effective as a one-shot treatment for bovine respiratory disease (BRD)?

<p>It has prolonged lung concentrations above the MIC for 9 days (A)</p> Signup and view all the answers

What is tilmicosin used to treat in rabbits?

<p>Pasteurella (&quot;snuffles&quot;) (A)</p> Signup and view all the answers

Flashcards

Macrolides

A subfamily of antimicrobials including erythromycin.

Drugs within Macrolides

Erythromycin, clarithromycin, tylosin, tilmicosin, and tildipirosin.

Drugs within Azalides

Azithromycin and gamithromycin.

Triamilide Macrolide

Tulathromycin

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Macrolides Ranking (WHO)

Critically important

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Macrolide Molecules

Large lactones with 13 to 16 carbons

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Macrolides: Chemistry

Liposoluble

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Azalides/Triamilides in Acid

They become ionized, reducing their ability to pass through bacterial membranes

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pH-Sensitive Macrolide

Tulathromycin

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Coated Macrolide

Erythromycin

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Oral Bioavailability

True

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Best Absorbed Erythromycin

Erythromycin estolate

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Injectable Macrolides

True

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Injection vs Oral

They avoid first-pass metabolism

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Macrolide Distribution

Large volume of distribution (Vd)

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Tissue Distribution

Well distributed in most tissues

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Macrolides in Leukocytes

They concentrate in leukocytes, making them effective against intracellular pathogens

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Macrolide Concentration

Lung tissue (pulmonary epithelial lining and alveolar macrophages)

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Weak Base Effect

It leads to ion trapping in acidic environments like milk, CSF, and purulent material

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High Lung Concentration Macrolide

Tulathromycin

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Highest Lung Concentration

Tulathromycin

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Acidic Environment Concentration

Azalides and triamilides

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Macrolide Metabolism

Primarily by the liver

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Enterohepatic Circulation Macrolide

Erythromycin

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Short Half-Life Macrolide

Tylosin

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Long Half-Life Macrolides

Azalides (Azithromycin, Gamithromycin)

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Cytochrome P450 Interference

Erythromycin and clarithromycin

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Macrolide Elimination

Biliary excretion

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Longest Half-Life Macrolide

Tilmicosin

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Dairy Cattle & Macrolides

Long-lasting residues may occur

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