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 g
CO Azithromycin (Canada)Z-Pak (Zithromax) (Canada)Interferes with microbial protein synthesis.
Rapidly absorbed.
Oral, immediate-releaseBioavailability is 38%.
Oral, ER suspensionBioavailability is 83% relative to the oral immediate-release suspension.
IVC 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 ImpairmentPharmacokinetics have not been established.
ElderlyPharmacokinetic 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.
GenderNo 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 solutionTreatment of bacterial conjunctivitis caused by susceptible organisms.
IV infusionTreatment 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 solutionBacterial 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 olderPO 10 mg/kg oral suspension once daily for 3 days (immediate-release).
Acute Otitis MediaChildren 6 mo of age and olderPO 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 olderOphthalmic 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 PneumoniaAdultsPO 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 olderIV 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-releasePO 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 ERPO 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. trachomatisAdultsPO Single 1 g dose.
GonorrheaAdultsPO Single 2 g dose.
Mild to Moderate Acute Bacterial Exacerbations of COPDAdultsPO 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 DiseaseAdultsIV 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/TonsillitisAdultsPO 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 olderPO 12 mg/kg/day for 5 days, not to exceed 500 mg/day.
Uncomplicated Skin and Skin Structure InfectionsAdultsPO 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 solutionStore 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 packetsStore reconstituted suspension at 41° to 86°F and discard when full dosing is completed.
Tablets, oral suspensionStore oral tablets at 59° to 86°F. Store dry powder for oral suspension below 86°F.
ZmaxStore 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, phenytoinSerum 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, theophyllinesLevels may be elevated by azithromycin, increasing the risk of toxicity. Monitor drug levels and adjust the dose as needed.
DigoxinDigoxin 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.
DronedaroneDronedarone 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.
NelfinavirAzithromycin levels may be elevated, increasing the risk of adverse reactions (eg, abnormal LFTs, hearing impairment). Monitor for azithromycin adverse reactions.
NilotinibIncreased nilotinib plasma concentrations with cardiotoxicity may occur. Avoid coadministration.
PimozidePimozide 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.
RifabutinRisk of neutropenia may be increased.
TriazolamPlasma 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.
WarfarinThe 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).
OphthalmicBlurring 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).
OphthalmicAllergic 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%).
Arthralgia (postmarketing).
Cough, pleural effusion (1% or less).
Fever (2%); face edema, fungal infection, pain (1% or less); edema (postmarketing).
Category B .
Undetermined.
Safety and efficacy not established in children younger than 6 mo of age.
Pharyngitis/TonsillitisSafety and efficacy not established in children younger than 2 yr of age.
Ophthalmic solutionSafety and efficacy not established in children younger than 1 yr of age.
IV infusionSafety 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.
Use cautiously.
Use cautiously.
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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