Azithromycin Capsule 250 mg

White capsule No. 0 filled with white powder.
Each 1 capsule contains Azithromycin dihydrate equivalent to Azithromycin 250 mg.

Pharmacologic category: Macrolide Antibiotic.
Pharmacology: Pharmacodynamics: Azithromycin usually is bacteriostatic, although the drug may be bactericidal in high concentrations against selected organisms. Bactericidal activity has been observed in vitro against Streptococcus pyogenes, S. pneumoniae, and Haemophilus influenzae.
Azithromycin inhibits protein synthesis in susceptible organisms by penetrating the cell wall and binding to 50S ribosomal subunits, thereby inhibiting translocation of aminoacyl transfer-RNA and inhibiting polypeptide synthesis. The site of action of azithromycin appears to be the same as that of the macrolides, clindamycin, lincomycin, and chloramphenicol. The antimicrobial activity of azithromycin is reduced at low pH. Azithromycin concentrates in phagocytes, including polymorphonuclear leukocytes, monocytes, macrophages, and fibroblasts. Penetration of the drug into phagocytic cells is necessary for activity against intracellular pathogens (e.g. Staphylococcus aureus, Legionella pneumophilia, Chlamydia trachomatis, Salmonella typhi).
Pharmacokinetics: Absorption: Azithromycin is rapidly absorbed from GI tract after oral administration. The absolute oral bioavailability of azithromycin is reported to be approximately 34-52% with single doses of 500 mg to 1.2 g administered as various conventional dosage form. Peak plasma azithromycin concentrations averaged 0.5 mcg/mL at about 2 hours. Food increased peak plasma concentration by 23%, but no effect on AUC.
Distribution: Azithromycin appears to be distributed into most body tissues and fluids after oral administration. Volume of distribution is 31.1-33.3 L/kg. Azithromycin is 51% bound to plasma proteins at drug concentrations of 0.02 mcg/mL and 7% bound at drug concentrations of 2 mcg/mL. Azithromycin crosses the placenta and is distributed into cord blood and amniotic fluid. Azithromycin is distributed into milk.
Metabolism: Azithromycin is metabolized by hepatic.
Elimination: The elimination half-life is 68 hours. The average tissue half-life is estimated to be 1-4 days. The half-life in peripheral leukocytes ranges from 34-57 hours. Azithromycin is excreted in feces principally as unchanged drug. Biliary excretion of azithromycin, predominantly as unchanged drug, is a major route of elimination following oral administration. Only a small portion of each azithromycin dose is excreted in urine (approximately 6%).

Azithromycin is used orally for the treatment of mild to moderate upper and lower respiratory tract infections (pharyngitis and tonsillitis, acute sinusitis, acute exacerbations of chronic bronchitis and mild to moderate community-acquired pneumonia (CAP)), uncomplicated skin and skin structure infections caused by susceptible organisms, urethritis or cervicitis caused by Chlamydia trachomatis or Neisseria gonorrhea, chancroid caused by Haemophilus ducreyi, disseminated infections caused by Mycobacterium avium complex (MAC) in patients with human immunodeficiency virus (HIV) infection.

Recommended Dose: Pharyngitis or Tonsillitis: Usual dosage: 500 mg single dose on first day, followed by 250 mg once daily on days 2-5.
Acute sinusitis: Usual dosage: 500 mg once daily for 3 days.
Acute for exacerbations of chronic bronchitis: Usual dosage: 500 mg once daily for 3 days.
Alternative dosage: 500 mg single dose for first day, followed by 250 mg once daily on days 2-5.
Mild to moderate community-acquired pneumonia (CAP): Usual dosage: 500 mg single dose on first day, followed by 250 mg once daily on days 2-5.
Uncomplicated skin and skin structure infections: Usual dosage: 500 mg single dose on first day, followed by 250 mg once daily on days 2-5.
Urethritis or cervicitis: Uncomplicated chlamydial infection: Usual dosage: 1 g single dose.
Gonorrhea caused by Neisseria gonorrhoeae: Usual dosage: 2 g single dose.
Chancroid: Usual dosage: 1 g single dose.
Disseminated infections caused by Mycobacterium avium complex (MAC) in patients with human immunodeficiency virus (HIV) infection: Usual dosage: 500-600 mg/day once daily in combination with ethambutol (15 mg/kg once daily).
Mode of Administration: For oral administration, can be taken with or without food.

Overdose and Treatments: Limited information is available on the acute toxicity of azithromycin. The acute lethal dose of the drug in humans is not known. The oral LD₅₀ of azithromycin in mice or rats is 3,000 - 4,000 mg/kg.
Adverse events experienced in higher than recommended doses were similar to those seen at normal doses. In the event of overdose, the administration of medicinal charcoal and general symptomatic treatment and supportive measures are indicated as required.

1. Hypersensitivity to azithromycin or any macrolide or ketolide antibiotic.
2. History of cholestatic jaundice/hepatic dysfunction associated with prior azithromycin use.

Because azithromycin is eliminated principally via the liver, the drug should be used with caution in patients with impaired hepatic function. Discontinue immediately if symptoms of hepatitis occur (malaise, nausea, vomiting, abdominal colic, fever). In addition, because of limited data regarding use of azithromycin in patients with renal impairment, the drug should be used with caution in patients with glomerular filtration rates less than 10 mL/minute.
Prolonged cardiac repolarization and QT interval with risk of cardiac arrhythmia and torsades de pointes has been reported with macrolides, including azithromycin. There have been reports of arrhythmias, ventricular tachycardia, hypotension, QT prolongation, and torsades de pointes in patients receiving azithromycin during post marketing surveillance. Use with caution in patients at risk of prolong cardiac repolarization. Consider avoiding use in patient with prolonged QT interval, uncorrected hypokalemia or hypomagnesemia, clinically significant bradycardia, or concurrent use of Class IA (e.g. quinidine, procainamide) or Class III (e.g. amiodarone, dofetilide, sotalol) antiarrhythmic agents.
Prolong use antibiotics may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD). It should be considered in the differential diagnosis of patients who develop diarrhea during or following azithromycin therapy and manage accordingly. If CDAD is suspected or confirmed, azithromycin may need to be discontinued.
Serious allergic reactions, including angioedema, anaphylaxis, and dermatologic reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported rarely in patients on azithromycin therapy. Although rare, fatalities have occurred. If an allergic reaction occurs with azithromycin, discontinue and institute appropriate therapy.
Cautions in patients with myasthenia gravis. There have been reports that azithromycin may aggravate the weakness of patients with myasthenia gravis.

Pregnancy: Pregnancy category: B.
Adverse events were not observed in animal reproduction studies. Azithromycin crosses the placenta. Fetal malformations have not been observed following maternal use of azithromycin. The maternal serum half-life of azithromycin is unchanged in early pregnancy and decreased at term; however, high concentrations of azithromycin are sustained in the myometrium and adipose tissue.
There are no adequate and controlled studies to date using azithromycin in pregnant women, and the drug should be used during pregnancy only when clearly needed.
Lactation: Azithromycin has been detected in human milk. The drug should be used with caution in nursing women.

>10%: Gastrointestinal: Diarrhea, nausea.
2% to 10%: Dermatologic: Pruritus, rash.
Gastrointestinal: Abdominal pain, anorexia, cramping, vomiting.
Genitourinary: Vaginitis.
≤1% (Limited to important or life-threatening): Acute renal failure, aggressive behavior, agitation, allergic reaction, anaphylaxis, anemia, angioedema, anxiety, arrhythmia (including ventricular tachycardia), arthralgia, bronchospasm, candidiasis, chest pain, cholestatic jaundice, conjunctivitis (pediatric patients), constipation, cough increased, deafness, dehydration, dermatitis (fungal), diaphoresis, dizziness, dyspepsia, eczema, edema, enteritis, erythema multiforme (rare), facial edema, fatigue, fever, flatulence, fungal infection, gastritis, headache, hearing disturbance, hearing loss, hepatic failure, hepatic necrosis, hepatitis, hyperactivity, hyperkinesia, hypotension, insomnia, interstitial nephritis, jaundice, leukopenia, LFTs increased, loss of smell, loss of taste, malaise, melena, mucositis, nephritis, nervousness, neutropenia (mild), oral candidiasis, pain, palpitation, pancreatitis, paresthesia, pharyngitis, photosensitivity, pleural effusion, pseudomembranous colitis, pyloric stenosis, QTc prolongation (rare), rhinitis, seizure, smell perversion, somnolence, SJS (rare), syncope, taste perversion, thrombocytopenia, tinnitus, tongue discoloration (rare), torsade de pointes (rare), toxic epidermal necrolysis (rare), urticaria, vertigo, vesiculobullous rash, weakness.

Avoid concomitant use: Avoid concomitant use of azithromycin with any of the following: BCG, highest risk QTc-prolonging agents, ivabradine, mifepristone, pimozide, quinine and terfenadine.
Increased effect/toxicity: Azithromycin may increase the levels/effects of: amiodarone, cardiac glycosides, cyclosporine, highest risk QTc-prolonging agents, moderate risk QTc-prolonging agents, ivermectin, pimozide, quinine, rivaroxaban, tacrolimus, terfenadine and vitamin k antagonists.
The level/effects of azithromycin may be increased by: ivabradine, mifepristone, nelfinavir, QTc-prolonging agent.
Decreased effect: Azithromycin may decrease the levels/effects of: BCG, sodium picosulfate, typhoid vaccine.

Preserve in well-closed containers and store below 30°C.

Macrolides

J01FA10 - azithromycin ; Belongs to the class of macrolides. Used in the systemic treatment of infections.

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