Macrolides: Uses, common brands, and safety info

Antibiotics are commonly used medications for the treatment of various bacterial infections. Unfortunately, there are millions of different types of bacteria pathogens so choosing the correct one is vital for accurately treating these types of infections. Macrolide antibiotics specifically are a type of infectious disease medication used to treat bacteria that usually infect the lungs, skin, or soft tissues. They are also quite effective against combating sexually transmitted infections. The chart below provides some common macrolides available in the United States as well as coupons and their safety information.

Other macrolides

• Biaxin (clarithromycin)

• Biaxin XL (clarithromycin)

• Ketek (telithromycin)

• Ketek Pak (telithromycin)

• Zmax (azithromycin)

What are macrolides?

Macrolides are a type of broad-spectrum antimicrobial used to fight against various bacteria such as mycoplasma, chlamydia, and legionella. They are most effective against gram-positive cocci bacteria and treat infections of the lung, skin, and soft tissues. 

Macrolide antimicrobial activity is usually considered bacteriostatic as they are only inhibitors of the bacteria they are treating. This is related to them only having the capability of preventing the growth of bacteria and not actually killing them. Occasionally if macrolides are used in very high doses or depending on the type of bacteria, they may be able to be bactericidal as well—killing the organism. They are also quite effective against group A streptococcal and pneumococcal infections if the organisms are penicillin-resistant or there is a penicillin allergy. 

Because of the common overuse of antibiotics, macrolide resistance is very common with many pathogens they are intended to treat. A common pathogen with bacterial resistance to macrolide antibiotics is pseudomonas so an alternative is needed when treating this bacteria. 

How do macrolides work?

Macrolide antimicrobial agents are a type of antibiotic that consists of at least one macrocyclic lactone ring, which makes its pharmacology capable of having either antifungal or antibacterial properties. The macrolide antibiotic mechanism of action involves stopping the RNA that is responsible for bacterial protein synthesis and therefore, suppressing the bacteria’s growth. RNA is able to be altered by macrolides reversibly binding to something called the P site on the 50S ribosomal subunit found in microorganisms such as bacteria. This prevents the production of protein in certain bacteria that is required for them to thrive. 

This mode of action found in macrolides is similar to antibiotics such as lincosamides and streptogramins—other types of antibiotics derived from the soil-borne Streptomyces bacteria. Macrolides, however, work differently from other popular antibiotics used more frequently. An example would be the difference from tetracycline antibiotics as tetracyclines bind to the 30S ribosomal subunit (not the 50S subunit found in macrolides). The focus on the bacterial ribosome is important as this structure is found in almost all bacteria. This makes macrolide antibiotics broad-spectrum antibiotics that can fight against a variety of organisms that cause disease. 

Macrolides are known to come in many options such as pills, creams, solutions, and intravenous formulations. These antimicrobial agents are not absorbed well orally, so many preparations are used intravenously. 

Unfortunately, if there is an allergy to one macrolide there will likely be an allergy to all as they display cross-resistance. Bacterial resistance is also quite common with these antibiotics mostly from overutilization of the medication in the past.

What are macrolides used for?

There are a variety of microorganisms and medical conditions that are treated with macrolide antibacterials. Here are the different types of bacteria treated with macrolide antibiotics:

• Aerobic and anaerobic gram-positive cocci, except for most enterococci

• Borrelia burgdorferi

• Campylobacter species

• Chlamydia trachomatis

• Chlamydophila pneumoniae

• Corynebacterium diphtheriae

• Legionella species

• Mycoplasma pneumoniae

• Propionibacterium acnes

• Treponema pallidum

Here are the common medical conditions that macrolide antibiotics can treat:

• Babesiosis

• Bacterial endocarditis prevention

• Bacterial infection

• Bartonellosis

• Bowel preparation

• Bronchitis

• Bullous pemphigoid

• Campylobacter gastroenteritis

• Cervicitis

• Chancroid

• Chlamydia infection

• Clostridioides difficile Infection

• COPD

• Cystic fibrosis

• Dental abscess

• Diphtheria

• Gonococcal infection

• Granuloma inguinale

• Haemophilus influenzae

• Helicobacter pylori infection

• Lyme disease

• Lymphogranuloma venereum

• Mycobacterium avium-intracellulare

• Nongonococcal urethritis

• Ocular rosacea

• Otitis media

• Pelvic inflammatory disease

• Pemphigoid

• Pertussis

• Pharyngitis

• Pneumonia

• Rheumatic fever 

• Sinusitis

• Skin infection

• Staphylococcus aureus infections

• STD prophylaxis

• Strep throat

• Streptococcal infection

• Streptococcus pneumoniae

• Syphilis

• Tonsillitis/pharyngitis

• Toxoplasmosis

• Typhoid fever

• Upper respiratory tract infection

Types of macrolides 

Ketolides

These types of macrolide antibiotics are newer derivatives from erythromycin but are known to be more effective with improved pharmacokinetics. This is in relation to them having two ribosomal binding sites. They were developed to address the issue of bacterial resistance that commonly occurs with the use of traditional macrolides and have a broader ability to address multiple bacteria. Ketolides have been found to be quite effective against respiratory tract infections, particularly for those with gram-positive bacteria. They are bacteriostatic at low doses and bactericidal at higher doses similar to traditional macrolides.

Examples of ketolide antibiotics: Ketek Pak and Ketek

Macrolides

Macrolides are a class of antibiotics from a soil-based bacteria called Saccharopolyspora erythraea previously known as Streptomyces bacteria. They are mostly used for gram-positive cocci organisms and are mainly bacteriostatic due to their inhibition of bacteria growth unless used in high concentrations. There are a few gram-negative bacteria that macrolides can fight against as well such as with Helicobacter pylori infections. 

Macrolides are the first choice of antibiotics to treat pneumonia, chlamydia, and urethritis. These antimicrobials are also known to have immunomodulatory benefits and anti-inflammatory properties, so they can treat other conditions rather than just bacteria infections. Common examples would be their use for cystic fibrosis and chronic obstructive pulmonary disease (COPD) symptoms.

Examples of macrolide antibiotics: Biaxin, Erythrocin, Zmax

Who can take macrolides?

Macrolide antibiotics are relatively safe for men, women, seniors, and children. 

Because of cardiac concerns with their use, people with known heart problems are considered high-risk patients. Due to the potential QT prolongation with the use of macrolides, monitoring of the heart on an ECG can also be done as a precaution for these patients. However, it is highly recommended that alternative treatments be sought out first. 

Seniors may also have lower hepatic functionality, so close monitoring should always be done when prescribing these medications to this demographic.

Can you use macrolides while pregnant or breastfeeding?

Certain macrolides can be used during pregnancy and breastfeeding. However, these medications must be monitored closely. Macrolides are not commonly the first antibiotic drug option during the first trimester and alternatives are highly encouraged. Currently, clarithromycin is not recommended during pregnancy due to the potential risk for spontaneous abortion and cardiovascular abnormalities. 

All macrolides can be used while breastfeeding; however, there are known risks associated with their use. Risks to the infant while breastfeeding includes diarrhea, vomiting, and rash while taking macrolides. More serious side effects include hypertrophic pyloric stenosis in infants.

Are macrolides safe?

Macrolide antibiotics are considered safe to use. There is some concern however with drug interactions with certain medications so a thorough systematic review must be performed by your healthcare provider. They must be made aware of all medications and supplements you may be taking so that there is no potential adverse interaction with macrolide antibiotics. Some medications your healthcare provider may be concerned with for potential drug interactions may include warfarin, colchicine, cholesterol medications, and benzodiazepines. 

Macrolide antibiotic restrictions

 Do not use macrolides if you have:

• Hypersensitivity to medication

• History of cardiac disease particularly arrhythmias and problems with the QT interval

• Liver disease

• End-stage kidney disease

• Irregularities with electrolytes

• Myasthenia gravis

Are macrolide antibiotics controlled substances?

Macrolide antibiotics are not controlled substances since they are not habit-forming and they do not pose any risk of dependency to the medication.

Common macrolides side effects

The majority of side effects associated with the antimicrobial macrolide usually involve gastrointestinal distress. The most common adverse effects include:

• Nausea

• Vomiting

• Abdominal cramps

• Diarrhea

• Tinnitus

• Dizziness

• Reversible hearing loss

• Rash

• Anorexia

• Fever

• Dermatitis

• Elevated liver enzymes

Here are some more serious reactions that can occur with the use of macrolide antibiotics:

• Angioedema

• Severe allergic reaction

• Cholestatic jaundice

• Liver damage

• Infantile hypertrophic pyloric stenosis

• Stevens-Johnson syndrome

• Toxic epidermal necrolysis

• Acute generalized exanthematous pustulosis

• Clostridioides difficile associated diarrhea

• QT heart interval prolongation

• Torsades de pointes

• Myasthenia gravis exacerbation

• Superinfection

• Kidney damage

• Pancreatitis

• Seizures

• Hallucinations

• Reversible hearing loss

• Psychosis

• Hypoglycemia

• Death of muscle fibers

How much do macrolides cost?

Prices for a macrolide antibiotic can vary greatly. There are some generic antibiotics in this category that cost around $30. On the other hand, there are some expensive macrolide preparations that can be as high as more than $5,600. Antimicrobials are important for the treatment of sometimes serious, life-threatening medical conditions. Receiving quality medication should be a priority when faced with infections. Luckily, there can be substantial savings when discounts are used from SingleCare, taking away financial stressors so the focus can be on recovery.