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Azithromycin


Pronunciation

 (az ith roe MYE sin)


U.S. Brand Names

 Zithromax®


Synonyms

 Azithromycin Dihydrate; Zithromax® TRI-PAK™; Zithromax® Z-PAK®


Generic Available

 No


Canadian Brand Names

 Zithromax®


Use

 Treatment of acute otitis media due to H. influenzae , M. catarrhalis , or S. pneumoniae ; pharyngitis/tonsillitis due to S. pyogenes ; treatment of mild-to-moderate upper and lower respiratory tract infections, infections of the skin and skin structure, community-acquired pneumonia, pelvic inflammatory disease (PID), sexually-transmitted diseases (urethritis/cervicitis), pharyngitis/tonsillitis (alternative to first-line therapy), and genital ulcer disease (chancroid) due to susceptible strains of C. trachomatis , M. catarrhalis , H. influenzae , S. aureus , S. pneumoniae , Mycoplasma pneumoniae , and C. psittaci ; acute bacterial exacerbations of chronic obstructive pulmonary disease (COPD) due to H. influenzae, M. catarrhalis, or S. pneumoniae ; acute bacterial sinusitis


Use - Dental

 Alternate antibiotic in the treatment of common orofacial infections caused by aerobic gram-positive cocci and susceptible anaerobes alternate antibiotic for the prevention of bacterial endocarditis in patients undergoing dental procedures


Use - Unlabeled/Investigational

 Prevention of (or to delay onset of) or treatment of MAC in patients with advanced HIV infection; prophylaxis of bacterial endocarditis in patients who are allergic to penicillin and undergoing surgical or dental procedures


Pregnancy Risk Factor

 B


Pregnancy Implications

 Azithromycin has been shown to cross the placenta. It has been used as an alternative treatment of Chlamydia in late-term pregnancy. There are no adequate and well-controlled studies in pregnant women; use during pregnancy only if clearly needed.


Lactation

 Enters breast milk/use caution


Contraindications

 Hypersensitivity to azithromycin, other macrolide antibiotics, or any component of the formulation


Warnings/Precautions

 Use with caution in patients with hepatic dysfunction; hepatic impairment with or without jaundice has occurred chiefly in older children and adults; it may be accompanied by malaise, nausea, vomiting, abdominal colic, and fever; discontinue use if these occur. May mask or delay symptoms of incubating gonorrhea or syphilis, so appropriate culture and susceptibility tests should be performed prior to initiating azithromycin. Pseudomembranous colitis has been reported with use of macrolide antibiotics; use caution with renal dysfunction. Prolongation of the QTc interval has been reported with macrolide antibiotics; use caution in patients at risk of prolonged cardiac repolarization. Safety and efficacy have not been established in children <6 months of age with acute otitis media, acute bacterial sinusitis, or community-acquired pneumonia, or in children <2 years of age with pharyngitis/tonsillitis.


Adverse Reactions

1% to 10%: Gastrointestinal: Diarrhea, nausea, abdominal pain, cramping, vomiting (especially with high single-dose regimens)

<1%: Agitation, allergic reaction, anemia, anorexia, candidiasis, chest pain, conjunctivitis, dermatitis (fungal), dizziness, dyspepsia, eczema, enteritis, facial edema, fatigue, flatulence, gastritis, headache, hyperkinesia, increased cough, insomnia, jaundice, leukopenia, malaise, nervousness, pain, pharyngitis, pleural effusion, pruritus, rash, rhinitis, urticaria

Postmarketing and/or case reports: Acute renal failure, aggressive behavior, anaphylaxis, angioedema, anxiety, arrhythmia (including ventricular tachycardia), arthralgia, cholestatic jaundice, deafness, edema, erythema multiforme (rare), hearing loss, hepatic necrosis (rare), hepatitis, hypertrophic pyloric stenosis, hypotension, interstitial nephritis, pancreatitis, paresthesia, pseudomembranous colitis, QTc prolongation (rare), seizure, somnolence, Stevens-Johnson syndrome (rare), syncope, taste abnormality, thrombocytopenia, tinnitus, tongue discoloration (rare), torsade de pointes (rare), vertigo, weakness


Overdosage/Toxicology

 Symptoms of overdose include nausea, vomiting, diarrhea, and prostration. Treatment is supportive and symptomatic.


Drug Interactions

 Substrate of CYP3A4 (minor); Inhibits CYP3A4 (weak)

Decreased peak serum levels: Aluminum- and magnesium-containing antacids by 24% but not total absorption

Increased effect/toxicity: Azithromycin may increase levels of tacrolimus, phenytoin, ergot alkaloids, alfentanil, bromocriptine, carbamazepine, cyclosporine, digoxin, disopyramide, and triazolam; azithromycin did not affect the response to warfarin or theophylline although caution is advised when administered together; nelfinavir may increase azithromycin serum levels (monitor for adverse effects)

Avoid use with pimozide due to significant risk of cardiotoxicity


Ethanol/Nutrition/Herb Interactions

 Food: Rate and extent of GI absorption may be altered depending upon the formulation. Azithromycin suspension, not tablet form, has significantly increased absorption (46%) with food.


Stability

Injection: Store intact vials of injection at room temperature. Reconstitute the 500 mg vial with 4.8 mL of sterile water for injection and shake until all of the drug is dissolved. Each mL contains 100 mg azithromycin. Reconstituted solution is stable for 24 hours when stored below 30°C/86°F.

The initial solution should be further diluted to a concentration of 1 mg/mL (500 mL) to 2 mg/mL (250 mL) in 0.9% sodium chloride, 5% dextrose in water, or lactated Ringer's. The diluted solution is stable for 24 hours at or below room temperature (30°C or 86°F) and for 7 days if stored under refrigeration (5°C or 41°F).

Other medications should not be infused simultaneously through the same I.V. line.

Suspension: Store dry powder below 30°C (86°F); following reconstitution, store suspension at 5°C to 30°C (41°F to 86°F).

Tablets: Store between 15°C to 30°C (59°F to 86°F).


Compatibility

 Other medications should not be infused simultaneously through the same I.V. line.


Mechanism of Action

 Inhibits RNA-dependent protein synthesis at the chain elongation step; binds to the 50S ribosomal subunit resulting in blockage of transpeptidation


Pharmacodynamics/Kinetics

Absorption: Rapid

Distribution: Extensive tissue; distributes well into skin, lungs, sputum, tonsils, and cervix; penetration into CSF is poor

Protein binding (concentration dependent): 7% to 50%

Metabolism: Hepatic

Bioavailability: 37%; variable effect with food (increased with oral suspension, unchanged with tablet)

Half-life elimination: Terminal: 68 hours

Time to peak, serum: 2.3-4 hours

Excretion: Feces (50% as unchanged drug); urine (~5% to 12%)


Dosage

Oral:

Children 6 months:

Community-acquired pneumonia: 10 mg/kg on day 1 (maximum: 500 mg/day) followed by 5 mg/kg/day once daily on days 2-5 (maximum: 250 mg/day)

Bacterial sinusitis: 10 mg/kg once daily for 3 days (maximum: 500 mg/day)

Otitis media:

1-day regimen: 30 mg/kg as a single dose (maximum dose: 1500 mg)

3-day regimen: 10 mg/kg once daily for 3 days (maximum: 500 mg/day)

5-day regimen: 10 mg/kg on day 1 (maximum: 500 mg/day) followed by 5 mg/kg/day once daily on days 2-5 (maximum: 250 mg/day)

Children 2 years: Pharyngitis, tonsillitis: 12 mg/kg/day once daily for 5 days (maximum: 500 mg/day)

Children:

M. avium -infected patients with acquired immunodeficiency syndrome (unlabeled use): 5 mg/kg/day once daily (maximum dose: 250 mg/day) or 20 mg/kg (maximum dose: 1200 mg) once weekly given alone or in combination with rifabutin

Treatment and secondary prevention of disseminated MAC (unlabeled use): 5 mg/kg/day once daily (maximum dose: 250 mg/day) in combination with ethambutol, with or without rifabutin

Prophylaxis for bacterial endocarditis (unlabeled use): 15 mg/kg 1 hour before procedure

Uncomplicated chlamydial urethritis or cervicitis (unlabeled use): Children 45 kg: 1 g as a single dose

Adolescents 16 years and Adults:

Respiratory tract, skin and soft tissue infections: 500 mg on day 1 followed by 250 mg/day on days 2-5 (maximum: 500 mg/day)

Alternative regimen: Bacterial exacerbation of COPD: 500 mg/day for a total of 3 days

Bacterial sinusitis: 500 mg/day for a total of 3 days

Urethritis/cervicitis:

Due to C. trachomatis : 1 g as a single dose

Due to N. gonorrhoeae : 2 g as a single dose

Chancroid due to H. ducreyi : 1 g as a single dose

Prophylaxis of disseminated M. avium complex disease in patient with advanced HIV infection (unlabeled use): 1200 mg once weekly (may be combined with rifabutin)

Treatment of disseminated M. avium complex disease in patient with advanced HIV infection (unlabeled use): 600 mg daily (in combination with ethambutol 15 mg/kg)

Prophylaxis for bacterial endocarditis (unlabeled use): 500 mg 1 hour prior to the procedure

I.V.: Adults:

Community-acquired pneumonia: 500 mg as a single dose for at least 2 days, follow I.V. therapy by the oral route with a single daily dose of 500 mg to complete a 7-10 day course of therapy

Pelvic inflammatory disease (PID): 500 mg as a single dose for 1-2 days, follow I.V. therapy by the oral route with a single daily dose of 250 mg to complete a 7-day course of therapy

Dosage adjustment in renal impairment: Use caution in patients with Clcr<10 mL/minute

Dosage adjustment in hepatic impairment: Use with caution due to potential for hepatotoxicity (rare). Specific guidelines for dosing in hepatic impairment have not been established.


Administration

I.V.: Infusate concentration and rate of infusion for azithromycin for injection should be either 1 mg/mL over 3 hours or 2 mg/mL over 1 hour. Other medications should not be infused simultaneously through the same I.V. line.

Oral: Suspension and tablet may be taken without regard to food.


Monitoring Parameters

 Liver function tests, CBC with differential


Dietary Considerations

Powder for oral suspension may be administered with or without food.

Tablet may be administered with food to decrease GI effects.

Sodium content:

Injection: 114 mg (4.96 mEq) per vial

Powder: 3.7 mg per 100 mg/5 mL of constituted solution; 7.4 mg per 200 mg/5 mL of constituted solution; 37 mg per 1 g single-dose packet

Tablet: 0.9 mg/250 mg tablet; 1.8 mg/500 mg tablet; 2.1 mg/600 mg tablet


Patient Education

 Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take as directed. Take all of prescribed medication and do not discontinue until prescription is completed. Take capsule form 1 hour before or 2 hours after meals; suspension may be taken with or without food; tablet form may be taken with meals to decrease GI effects. Do not take with antacids that contain aluminum or magnesium. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. If taken to treat a sexually-transmitted disease, follow advice of prescriber related to sexual intercourse and preventing transmission. May cause transient abdominal distress, diarrhea, and headache. Report signs of additional infections (eg, sores in mouth or vagina, vaginal discharge, unresolved fever, severe vomiting, or diarrhea). Breast-feeding precaution: Consult prescriber if breast-feeding.


Additional Information

 Capsules are no longer being produced in the United States.


Cardiovascular Considerations

 The clinical implications of the association between infection ( Chlamydia and cytomegalovirus) and coronary artery disease (CAD) is unknown. A recent trial showed no difference in clinical events in azithromycin-treated patients who had CAD and positive C. pneumoniae antibodies.


Dental Health: Effects on Dental Treatment

 No significant effects or complications reported


Dental Health: Vasoconstrictor/Local Anesthetic Precautions

 No information available to require special precautions


Mental Health: Effects on Mental Status

 Macrolides have been reported to cause nightmares, confusion, anxiety, and mood lability; may rarely cause dizziness, agitation, nervousness, and insomnia


Mental Health: Effects on Psychiatric Treatment

 Contraindicated with pimozide; may increase concentration of bromocriptine, carbamazepine and triazolam


Dosage Forms

Injection, powder for reconstitution, as dihydrate: 500 mg

Powder for oral suspension, as dihydrate: 100 mg/5 mL (15 mL); 200 mg/5 mL (15 mL, 22.5 mL, 30 mL) [cherry creme de vanilla and banana flavor]; 1 g [single-dose packet; cherry creme de vanilla and banana flavor]

Tablet, as dihydrate: 250 mg, 500 mg, 600 mg

Zithromax® TRI-PAK™ [unit-dose pack]: 500 mg (3s)

Zithromax® Z-PAK® [unit-dose pack]: 250 mg (6s)


References

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Amsden GW, "Erythromycin, Clarithromycin, and Azithromycin: Are the Differences Real?" Clin Ther , 1996, 18(1):56-72.

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Dajani AS, Taubert KA, Wilson W, et al, "Prevention of Bacterial Endocarditis Recommendations by the American Heart Association," JAMA , 1997, 277(22):1794-801.

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International Brand Names

 Abacten® (CL); Adefin® (HN); Artricina® (DO); Aruzilina® (CR, DO, GT, HN, PA, SV); Arzomicin® (AR, DO); Asipral® (CL); Atizor® (CL); Azacid® (TR); Azadose® (FR); Azalid® (CL); Azatek® (TR); Azatril® (BG); AZ® (BD); Azenil® (IL); Azi® (BR); Azicin® (BD); Azimax® (BR); Azimin® (CO); Azimix® (BR); Azin® (BD); Azithral® (IN); Azithrocin® (BD); Azitrax® (BR); Azitrix® (PT); Azitrocin® (IT, MX); Azitromax® (NO, SE); Azitrom® (CL, DO); Azitromicina® (CL, EC); Azitromicina Dupomar® (AR); Azitromicina Genfar® (EC); Azitromicina MK ® (CO, CR, DO, GT, HN, PA, SV); Azitromicina Northia® (AR); Azitromicina Richet® (AR); Azitromicina Rigar® (PA); Azitromin® (BR, EC); Azitro® (TR); Azitrox® (CZ); Azitroxil® (BR); Aziwok® (IN, RU, ZA); Azomax® (TR); Azro® (TR); Aztrin® (ID); Azyth® (BD); Biosine® (GT); Clearsing® (AR); Clindal AZ® (BR); Cronopen® (AR); Dinamicina® (CL); Donozyt® (GT, SV); Doyle® (AR); Eritrosima® (BR); Fabramicina® (AR); Farmiz® (PT); Fina-3® (AR); Forcin® (CL); Gigatrom® (PT); Goxil® (ES); Hemomycin® (YU); Kromicin® (CO); Macromax® (AR); Mazitrom® (BR); Misultina® (AR); Mixoterin® (AR); Neblic® (AR); Nifostin® (AR); Nor-Zimax® (SV); Novegam® (CR, DO, GT, PA); Novozitron® (AR); Odazyth® (BD); Orobiotic® (AR); Pediagesic® (DO); Ribotrex® (IT); Selimax® (BR); Sumamed® (CZ, HR, HU, PL, RO, RU, SI); Sumir® (AR); Tanezox® (AR); Tobil (EC); Tobyl® (CO); Toraseptol® (ES); Tremac® (TR); Trex® (CL, EC); Triamid® (AR); Tritab® (AR); Tromic® (DO); Tromix® (CO); Trozocina® (IT); Ultrabac® (EC); Ultreon® (DE); Unizitro® (PT); Vinzam® (ES); Zaret® (CO, GT); Zentavion® (ES); Zeto® (IL); Zibramax® (ID); Zifin® (ID); Zimax® (BD); Zimericina® (CO); Zistic® (ID); Zithrax® (ID); Zithromac® (JP); Zithromax® (AT, AU, CA, CH, CL, CY, DE, DO, EG, FI, FR, GB, ID, IE, IL, JO, KW, LB, NL, NZ, PT, SG, TH, ZA); Zithrox® (BD); Zitrim® (CO); Zitrobifan® (CO); Zitromax® (AR, BE, BR, CO, DK, ES, IT, LU, TR); Zitroneo® (BR); Zitrotek® (TR); Zomax® (EG, JO, KW, LB, SY); Zycin® (ID)


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