Trade Names:AzaSite- Solution, ophthalmic 1%
Trade Names:Azithromycin- Injection, lyophilized powder for solution 2.5 g
Trade Names:Zithromax- Tablets 250 mg (as dihydrate)- Tablets 500 mg (as dihydrate)- Tablets 600 mg (as dihydrate)- Injection, lyophilized powder for solution 500 mg- Powder for oral suspension 100 mg per 5 mL- Powder for oral suspension 200 mg per 5 mL- Powder for oral suspension 1 g/packet (as dihydrate)
Trade Names:Zmax- Powder for oral suspension, ER 2 gCO Azithromycin (Canada)Z-Pak (Zithromax) (Canada)
Interferes with microbial protein synthesis.
Rapidly absorbed.Oral, immediate-release
Bioavailability is 38%.Oral, ER suspension
Bioavailability is 83% relative to the oral immediate-release suspension.IV
C max is approximately 3.63 mcg/mL; C min is approximately 0.2 mcg/mL (at 24 h); AUC 24 is approximately 9.6 mcg•h/mL.
Widely distributed into body (cervix, lung, skin, sputum, tonsils), but distributes poorly in the CSF. Higher concentrations in tissues than in plasma or serum. Vd is 31.1 L/kg (oral) and 33.3 L/kg (IV). Protein binding is 7% to 50% (concentration dependent).
The half-life is approximately 68 h. Plasma Cl is 630 mL/min (oral) and 10.18 mL/min/kg (IV). Excreted primarily in the bile, predominantly as unchanged drug. Approximately 6% is excreted in urine as unchanged drug (oral); approximately 11% is excreted in the urine after first dose and 14% after fifth dose (IV).
C max and AUC increased 61% and 35%, respectively, in subjects with severe renal impairment; use with caution.Hepatic Function Impairment
Pharmacokinetics have not been established.Elderly
Pharmacokinetic parameters in men 65 to 85 yr of age are similar to younger adults; however, in elderly women, a higher C max was observed but there was no change in drug accumulation.Gender
No differences in drug disposition between men and women. No dosage adjustment is needed based on gender.
Treatment of acute bacterial exacerbation of COPD, acute bacterial sinusitis, community-acquired pneumonia, pharyngitis/tonsillitis caused by Streptococcus pyogenes in patients who cannot use first-line therapy, uncomplicated skin and skin structure infections, urethritis and cervicitis, and genital ulcer disease (in men) caused by susceptible organisms.Oral suspension (ER)
Treatment of acute bacterial sinusitis and community-acquired pneumonia caused by susceptible organisms.Ophthalmic solution
Treatment of bacterial conjunctivitis caused by susceptible organisms.IV infusion
Treatment of community-acquired pneumonia and pelvic inflammatory disease caused by susceptible organisms.Children Oral tablets and oral suspension (immediate-release)
Treatment of acute bacterial sinusitis, acute otitis media caused by susceptible organisms, community-acquired pneumonia, pharyngitis/tonsillitis caused by S. pyogenes in patients who cannot use first-line therapy.Oral suspension (ER)
Treatment of community-acquired pneumonia caused by susceptible organisms.Ophthalmic solution
Bacterial conjunctivitis caused by susceptible organisms.
Acne vulgaris (topical), acute pharyngitis or tonsillitis (group A streptococcal) in children, acute skin and soft tissue infections, babesiosis, chlamydial infections caused by Chlamydia trachomatis , granuloma inguinale caused by Klebsiella granulomatis , early lime disease, lower respiratory tract infections, prevention of coronary events, prophylaxis after a sexual assault, rosacea (topical), rosacea (oral), traveler's diarrhea, and treatment of cholera in adults.
Hypersensitivity to azithromycin, erythromycin, or to any macrolide antibiotic.
PO 500 mg every day for 3 days (immediate-release); single 2 g dose, taken on an empty stomach, at least 1 h before or 2 h after a meal (ER).Children 6 mo of age and older
PO 10 mg/kg oral suspension once daily for 3 days (immediate-release).Acute Otitis MediaChildren 6 mo of age and older
PO 30 mg/kg given as a single dose or 10 mg/kg once daily for 3 days or 10 mg/kg as a single dose on the first day (not to exceed 500 mg/day) followed by 5 mg/kg on days 2 through 5 (not to exceed 250 mg/day).Bacterial ConjunctivitisAdults and Children 1 yr of age and older
Ophthalmic Instill 1 drop in affected eye(s) twice daily, 8 to 12 h apart for the first 2 days, then 1 drop in affected eye(s) once daily for the next 5 days.Community-Acquired PneumoniaAdults
PO 500 mg as a single dose on the first day followed by 250 mg once daily on days 2 through 5 (immediate-release); single 2 g dose (ER).Adults and Children 16 yr of age and older
IV 500 mg as a single daily dose for at least 2 days. Follow IV therapy by the oral route at a single daily dose of 500 mg to complete 7- to 10-day course of therapy.Children 6 mo of age and older Immediate-release
PO 10 mg/kg as a single dose on the first day (not to exceed 500 mg/day), followed by 5 mg/kg on days 2 through 5 (not to exceed 250 mg/day).Children 6 mo of age and older ER
PO single dose of 60 mg/kg (equivalent to 27 mg/lb). The Zmax dose in mL is equivalent to the child's weight in lb (ie, 1 mL/lb dose). Thus, for a child weighing less than 75 lb (34 kg), the dose in mL is equivalent to the child's weight in pounds (ie, a 20 lb child should receive a single 20 mL dose [540 mg]). Children weighing 75 lb (34 kg) or more should receive the adult dose (2 g).Genital Ulcer Disease Caused by Haemophilus ducreyi (chancroid) Nongonococcal Urethritis and Cervicitis Caused by C. trachomatisAdults
PO Single 1 g dose.GonorrheaAdults
PO Single 2 g dose.Mild to Moderate Acute Bacterial Exacerbations of COPDAdults
PO 500 mg/day for 3 days or 500 mg as a single dose on the first day followed by 250 mg once daily on days 2 through 5.Pelvic Inflammatory DiseaseAdults
IV 500 mg as a single daily dose for 1 to 2 days. Follow IV therapy by the oral route at a single daily dose of 250 mg to complete a 7-day course of therapy.Pharyngitis/TonsillitisAdults
PO 500 mg as a single dose on the first day followed by 250 mg once daily on days 2 through 5.Children 2 yr of age and older
PO 12 mg/kg/day for 5 days, not to exceed 500 mg/day.Uncomplicated Skin and Skin Structure InfectionsAdults
PO 500 mg as a single dose on the first day followed by 250 mg once daily on days 2 through 5.
Store powder for injection at 59° to 86°F. Store reconstituted solution below 86°F for up to 24 h. Diluted infusion solution may be stored for up to 24 h at or below 86°F or for 7 days if stored in refrigerator (41°F).Ophthalmic solution
Store refrigerated at 36° to 46°F. Once opened, store at 36° to 77°F for up to 14 days. Discard after 14 days.Oral suspension packets
Store reconstituted suspension at 41° to 86°F and discard when full dosing is completed.Tablets, oral suspension
Store oral tablets at 59° to 86°F. Store dry powder for oral suspension below 86°F.Zmax
Store dry powder at or below 86°F. Store reconstituted suspension at 59° to 86°F. Do not freeze. Administer within 12 h of constitution.
May reduce the peak serum levels but not the AUC of azithromycin.Carbamazepine, hexobarbital, phenytoin
Serum concentrations of these agents have been elevated by azithromycin, increasing the pharmacologic effects and risk of adverse reactions. Monitor serum concentrations of these agents and observe the patient for adverse reactions. Adjust the dose as needed.Cyclosporine, theophyllines
Levels may be elevated by azithromycin, increasing the risk of toxicity. Monitor drug levels and adjust the dose as needed.Digoxin
Digoxin plasma concentrations may be elevated, increasing the risk of toxicity. Monitor digoxin levels and observe the patient for signs of digoxin toxicity. Adjust the digoxin dose as needed.Dronedarone
Dronedarone plasma concentrations and pharmacologic effects may be increased. Avoid coadministration.Ergot derivatives (eg, dihydroergotamine, ergotamine)
Acute ergotism manifested as peripheral ischemia has been reported. Closely monitor for ergotism.Nelfinavir
Azithromycin levels may be elevated, increasing the risk of adverse reactions (eg, abnormal LFTs, hearing impairment). Monitor for azithromycin adverse reactions.Nilotinib
Increased nilotinib plasma concentrations with cardiotoxicity may occur. Avoid coadministration.Pimozide
Pimozide plasma concentrations may be elevated, increasing the risk of cardiotoxicity. Coadministration is contraindicated.QT prolonging drugs (eg, antiarrhythmic agents [class III (eg, dofetilide, sotalol) and class IA (eg, procainamide, quinidine)], arsenic trioxide, chlorpromazine, cisapride, dolasetron, droperidol, gatifloxacin, halofantrine, levomethadyl, lithium, maprotiline, mefloquine, mesoridazine, methadone, paliperidone, pentamidine, perflutren, pimozide, probucol, propafenone, sparfloxacin, tacrolimus, thioridazine, ziprasidone, quinolone antibiotics [eg, levofloxacin, moxifloxacin], tetrabenazine)
Risk of life-threatening cardiac arrhythmias, including torsades de pointes, may be increased. Use with caution. Avoid coadministration with paliperidone or propafenone. Close clinical and ECG monitoring is advised.Rifabutin
Risk of neutropenia may be increased.Triazolam
Plasma concentrations may be elevated by azithromycin, increasing the pharmacologic effect and risk of adverse reactions. Observe the clinical response of the patient and adjust the triazolam dose as needed.Warfarin
The anticoagulant effect may be increased, increasing the risk of hemorrhage. Monitor anticoagulant parameters and adjust the warfarin dose as needed.
None well documented.
Chest pain, palpitations (1% or less); arrhythmias including ventricular tachycardia, hypotension, QT prolongation, syncope, torsades de pointes (postmarketing).
Dizziness, headache (1%); agitation, fatigue, hyperkinesia, insomnia, malaise, nervousness, somnolence, vertigo (1% or less); aggressive reaction, anxiety, asthenia, convulsions, hyperactivity, paresthesia (postmarketing).
Rash (5%); dermatitis, pruritus (2%); eczema, fungal dermatitis, photosensitivity, swelling, urticaria, vesiculobullous rash (1% or less); erythema multiforme, Stevens-Johnson syndrome, TEN (postmarketing).
Eye irritation with ophthalmic solution (1% to 2%); conjunctivitis, pharyngitis, rhinitis (1% or less); deafness, hearing disturbances including hearing loss, smell perversion or loss, taste perversion or loss, tinnitus (postmarketing).Ophthalmic
Blurring vision, eye pain, eyelid swelling, itching eye, reduced visual acuity (postmarketing).
Nausea (18%); diarrhea/loose stools, vomiting (14%); abdominal pain (5%); anorexia (2%); dyspepsia (1%); constipation, enteritis, flatulence, gastritis, melena (1% or less); oral candidiasis, pancreatitis, pseudomembranous colitis, tongue discoloration (postmarketing).
Vaginitis (3%); monilia, nephritis (1% or less); acute renal failure, interstitial nephritis (postmarketing).
Cholestatic jaundice, jaundice (1% or less); abnormal liver function including hepatic failure, hepatic necrosis, hepatitis (postmarketing).
Decreased lymphocytes, decreased neutrophils, increased eosinophils, increased lymphocytes, increased neutrophils, and increased platelet count (at least 1%); anemia, leukopenia (1% or less); thrombocytopenia (postmarketing).
Angioedema (1% or less); anaphylaxis (postmarketing).Ophthalmic
Allergic reactions including facial swelling, hives, periocular swelling, rash, and urticaria (postmarketing).
Elevated ALT, AST, and creatinine (4% to 6%); elevated bilirubin and LDH (1% to 3%); decreased hematocrit, hemoglobin, and blood glucose; increased blood glucose, BUN, GGT, serum creatine, phosphokinase, and potassium (at least 1%).
Pain at injection site (7%); local inflammation (3%).
Cough, pleural effusion (1% or less).
Fever (2%); face edema, fungal infection, pain (1% or less); edema (postmarketing).
Review results of culture and sensitivity testing as appropriate.STD testing
Ensure patient being treated for sexually transmitted urethritis or cervicitis has serologic test for syphilis and cultures for gonorrhea performed at time of diagnosis, and that appropriate antimicrobial therapy and follow-up tests are initiated if infection is confirmed.Therapy response
Monitor patient's response to therapy. For bacterial conjunctivitis, when clinical judgment dictates, examine patient with the aid of magnification and, when appropriate, fluorescein staining.
Category B .
Safety and efficacy not established in children younger than 6 mo of age.Pharyngitis/Tonsillitis
Safety and efficacy not established in children younger than 2 yr of age.Ophthalmic solution
Safety and efficacy not established in children younger than 1 yr of age.IV infusion
Safety and efficacy not established in children younger than 16 yr of age.
Serious, life-threatening reactions, including anaphylaxis, angioedema, and dermatologic reactions (including Stevens-Johnson syndrome and TEN), have occurred.
Prolonged use of antibiotics may result in bacterial or fungal overgrowth of nonsusceptible microorganisms.
Serious CV events, including prolonged cardiac repolarization and QT interval, have occurred with other macrolide antibiotics.
New onset and exacerbation of symptoms of myasthenia gravis have been reported.
May be a factor in patients who develop diarrhea.
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