Kipengele K,
Bpharm
Basic Pharmacology
NTA Level 4 Semester 2
2020
1
Description of Macrolide Drugs
Session 5:
By the end of this session you
are expected to be able to:
• List indications of Macrolide Drugs
• List Contraindications of Macrolide Drugs
• Describe dose, dosage and course of
Macrolidede Drugs
• List side effects and adverse effects of
Macrolide Drugs
• Describe interactions and precautions of
Macrolide Drugs
What are macrolide antibiotics?
Macrolides are a class of antibiotic that
includes
• Erythromycin
• Clarithromycin
• Azithromycin
• Roxithromycin
The indication of the macrolides
• Are effective against gram-positive organisms, especially
pneumococci, streptococci, staphylococci, and corynebacteria
• Also effective to Mycoplasma, legionella, Chlamydia
trachomatis, Chlamydia psittaci, Chlamydia pneumoniae,
helicobacter, listeria, and certain mycobacteria
(Mycobacterium kansasii,
M scrofulaceum)
• Gram-negative organisms such as Neisseria sp, Bordetella
pertussis, Bartonella henselae, and B quintana (etiologic
agents of cat-scratch disease and bacillary angiomatosis)
some rickettsia sp, Treponema pallidum, and campylobacter
sp are susceptible.
Contraindication of Macrolide Drugs
• Erythromycin is contraindicated in:
– In patient with hepatic impairment
– In patient with Renal impairment
• Clarithromycin is contraindicated in:
– Pregnancy
– Hepatic dysfunction
– Renal impairment
• Azithromycin are contraindicated in:
– Breastfeeding
– Pregnancy
– Hepatic dysfunction
– Renal impairment
Dose, Dosage and Course of Macrolide
drugs
• Erythromycin
– The oral dosage of erythromycin base is 250-500mg
every 6 hours (for children, 40 mg/kg/d)
– Over 8 years 250-500mg every six hours Or 4000mg
daily in divided doses in severe infection.
– The dosage of erythromycin ethylsuccinate is 400-
600mg every 6 hours.
– Oral erythromycin base (1 g) is sometimes combined
with oral neomycin or kanamycin for preoperative
preparation of the colon.
– The intravenous dosage of erythromycin gluceptate
or lactobionate is 500-1000 mg every 6 hours for
adults and 20-40 mg/kg/d for children.
Dose, Dosage and Course of Macrolide
drugs
• Azithromycin
– 500mg once daily for 3three days
– 500mg on the firstday then250mg once daily for 4
days
– Child over 6 month 10mg/kg once daily for 3
days
• Clarithromycin
– 250mg every 12 hours for seven days
– In severe infections 500mg 12hourly for 14 days
– Intravenously infusion 500mg twice daily
Side effects/adverse effects of
macrolides drugs
• Anorexia, nausea, vomiting, and Diarrhoea
occasionally accompany oral administration
• Gastrointestinal intolerance, which is due to a
direct stimulation of gut motility,
• Can produce acute cholestatic hepatitis (fever,
jaundice, impaired liver function)
• Other allergic reactions include fever,
eosinophilia, and rashes
Interaction and Precaution of Essential
Macrolide drugs
Interaction
• Erythromycin metabolites can inhibit cytochrome P450
enzymes thus increase the serum concentrations of
theophylline, oral anticoagulants, cyclosporine, and
methylprednisolone
• Erythromycin increases serum concentrations of oral digoxin
by increasing its bioavailability
Precaution
• Should be avoided if
– You have had a previous allergic reaction to them.
– You have an inherited blood disorder, such as porphyria,
or a heart rhythm disorder (or you are at risk of
developing a heart rhythm disorder).
Key Points
• Macrolide drugs includes erythromycin,
Clarithromycin and azithromycin.
• Macrolides are effective against gram-positive
organisms, especially pneumococci, streptococci,
staphylococci, and corynebacteria
• Macrolides are contraindicated in: Pregnancy, Hepatic
dysfunction Renal impairment
• Macrolides can be given orally or by injection
• Common side effects of Macrolides are Anorexia,
nausea, vomiting, and Diarrhoeadiarrhoea
• Macrolides increases effects of many drugs like
digoxin and theophylline
Self Evaluation
• What are the indications of Macrolide drug?
• What are the Contraindications of Macrolide
drugs?
• What are the dose, dosage and course of
Macrolide drugs?
• What are side effects and adverse effects of
Macrolide drugs?
• What are the interactions and precautions of
Macrolide drugs?
