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Azithromycin


Dosing

Adult dose

:

Acute infective exacerbation of chronic obstructive pulmonary disease (Mild to Moderate):

500 mg orally once daily

for 3 days

500 mg orally

on day 1 followed by 250 mg/day orally on days 2 to 5.

Babesiosis:

500 mg

to 1000 mg orally on day 1 followed by 250 mg/day thereafter plus atovaquone 750 mg orally every 12 hours for 7 to 10 days; 600 to 1000 mg/day of azithromycin may be

used in

immunocompromised patients.

Bacterial conjunctivitis:
1 drop of 1% solution instilled into the affected eye(s) twice daily (8 to 12 hours apart) for 2 days; followed by 1 drop once daily for an additional 5 days.

Bacterial endocarditis; Prophylaxis:
(High-risk patients; dental; respiratory; or infected skin/skin structure or musculoskeletal tissue procedures) 500 mg orally 30 to 60 minutes prior to procedure

Bacterial sinusitis; acute (Mild to Moderate):
(

Tablets

)

500 mg orally daily

for 3 days

(Extended-release oral suspension)
A single 2g

oral dose



Bartonellosis HIV infection:
(Bacillary angiomatosis; peliosis hepatis; bacteremia; osteomyelitis) 500 mg orally daily for at least 3 months

Chancroid:
1 g orally as a

single dose



Chlamydial infection:
1 g orally as a single dose

Community acquired pneumonia (Mild to Moderate):
(Tablet)
500 mg orally on day 1 followed by 250 mg/day orally on days 2 to 5

(Extended-release suspension)
A single 2 g oral dose

(IV)

500 mg IV

every day for at least 2 days followed by 500 mg orally every day to complete a 7 to 10 day course of therapy.

Cystic fibrosis:
(Less than 40 kg)
250 mg orally 3 times per week was the

dosage

used in 2 clinical studies

(40 kg or greater)
500 mg orally 3 times per week was the dosage used in 2 clinical studies

Disseminated infection due to Mycobacterium avium-intracellulare group; Prophylaxis HIV infection:
Primary prevention:
1200 mg orally once weekly OR 600 mg orally twice weekly

Secondary prevention:
500 to 600 mg orally daily in combination with ethambutol 15 mg/kg orally daily; with or without rifabutin 300 mg orally daily

Disseminated infection due to Mycobacterium avium-intracellulare group HIV infection:
500 to 600 mg orally daily in combination with ethambutol 15 mg/kg orally daily; with or without rifabutin 300 mg orally daily

Gonorrhea; Urethritis or cervicitis:
Preferred regimen:
1 g orally as a single dose in combination with ceftriaxone 250 mg IM as a single dose (

Guideline dosage

)

Alternative regimen:
1 g orally as a single dose in combination with cefixime 400 mg orally as a single dose (Guideline dosage)

Granuloma inguinale:
1 g orally once weekly OR 500 mg orally daily; treat for at least 3 weeks and until all lesions have completely healed (guideline dosage).

HIV infection Toxoplasma encephalitis:
(Alternative therapy) 900 to 1200 mg orally daily; in combination with pyrimethamine 200 mg orally for 1 dose; then 50 mg (less than 60 kg) or 75 mg (60 kg or greater) orally daily plus leucovorin 10 to 25 mg (can increase to 50 mg) orally daily for at least 6 weeks

Infection of skin AND/OR subcutaneous tissue; Uncomplicated:
500 mg orally on day 1 followed by 250 mg/day orally on days 2 to 5

Lyme disease:
(Alternative to first-line therapy) 500 mg orally once daily for 7 to 10 days for early localized or early disseminated Lyme disease associated with erythema migrans or borrelial lymphocytoma.

Mycobacterium avium complex infection; Lung disease:
Nodular/bronchiectatic disease:
Initial; 500 to 600 mg orally 3 times weekly in combination with ethambutol 25 mg/kg 3 times weekly and rifampin 600 mg 3 times weekly

Cavitary disease:
Initial; 250 mg orally daily in combination with ethambutol 15 mg/kg daily and rifampin 10 mg/kg daily (Maximum 600 mg daily); consider addition of streptomycin OR amikacin

Severe or previously treated disease:
Initial; 250 to 300 mg orally daily in combination with ethambutol 15 mg/kg daily and rifabutin 150 to 300 mg daily OR rifampin 10 mg/kg daily (Maximum 600 mg daily); plus streptomycin OR amikacin.

Nongonococcal cervicitis:
1 g orally as a single dose

Nongonococcal urethritis:
1 g orally as a single dose

Pelvic inflammatory disease:
500 mg IV every day for 1 or 2 days followed by 250 mg orally every day to complete a 7 day course of therapy

Pertussis:
500 mg single dose orally on day 1; then 250 mg daily on days 2 through 5 (Guideline dosing)

Sexually transmitted infectious disease; Prophylaxis Victim of sexual aggression:
1 g orally as a single dose; in combination with ceftriaxone 250 mg IM and either metronidazole 2 g orally as a single dose OR tinidazole 2 g orally as a single dose (guideline dosage).

Streptococcal pharyngitis; alternative to first-line therapy:
12 mg/kg orally once daily for 5 days; MAX 500 mg/dose (guideline dosing)
(Tablets and immediate-release suspension) 500 mg single-dose orally on day 1; then 250 mg orally once daily on days 2 through 5 (manufacturer dosing)

Streptococcal tonsillitis; alternative to first-line therapy:
12 mg/kg orally once daily for 5 days; MAX 500 mg/dose (Guideline dosing)
(Tablets and immediate-release suspension)
500 mg single-dose orally on day 1; then 250 mg orally once daily on days 2 through 5 (Manufacturer dosing)

Typhoid fever:
1 g orally on day 1 followed by 500 mg orally once daily for the next 6 days (Study dose)

Pediatric dose

:

Acute otitis media:
(6 months or older)
30 mg/kg as

single oral dose

OR 10 mg/kg orally every day for 3 days OR 10 mg/kg orally on day 1 followed by 5 mg/kg orally every day for days 2 to 5 (manufacturer dosing).

Babesiosis:
10 mg/kg orally on day 1 (

Maximum 500 mg

/dose) followed by 5 mg/kg/day (Maximum 250 mg/dose) thereafter plus atovaquone 20 mg/kg orally (Maximum 750 mg/dose) every 12 hours for 7 to 10 days.

Bacterial conjunctivitis:
(1 year or older)
1 drop of 1% solution instilled into the affected eye(s) twice daily (8 to 12 hours apart) for 2 days; followed by 1 drop once daily for an additional 5 days.

Bacterial endocarditis; Prophylaxis:
(High-risk patients; dental; respiratory; or infected skin/skin structure or musculoskeletal tissue procedures) 15 mg/kg orally 30 to 60 minutes prior to procedure

Bacterial sinusitis; acute (Mild to Moderate):
(6 months or older)
10 mg/kg (Maximum 500 mg/dose) orally once daily for 3 days

Bartonellosis HIV infection:
(Cutaneous bacillary angiomatosis) 5 to 12 mg/kg (Maximum 600 mg/day) orally once daily for 3 months
Chlamydial infection:
(At least 45 kg or at least 8 years of age)
1 g orally as a single dose

Community acquired pneumonia (Mild to Moderate):
(Tablet and immediate-release suspension; 6 months or older)
10 mg/kg (Maximum 500 mg/dose) orally on day 1 followed by 5 mg/kg (Maximum 250 mg/dose) orally on days 2 to 5 (manufacturer dosing) this dosage is also recommended for outpatient treatment in children older than 3 months (guideline dosing)

(Extended-release suspension; 6 months or older; less than 34kg):
A single 60mg/kg ORAL dose; 34 kg and greater; a single 2g ORAL dose (Manufacturer dosing)

(Inpatient treatment; older than 3 months)
10 mg/kg IV daily for at least 2 days; then 5 mg/kg orally once daily to complete treatment course

Cystic fibrosis:
(6 years or older; less than 40 kg)
250 mg orally 3 times per week was the dosage used in 2 clinical studies

(6 years or older; 40 kg or greater)
500 mg orally 3 times per week was the dosage used in 2 clinical studies.

Disseminated infection due to Mycobacterium avium-intracellulare group; Prophylaxis HIV infection:
Primary prevention:
Preferred regimen; 20 mg/kg orally once weekly (Maximum 1200 mg/week); alternative regimen; 5 mg/kg orally once daily (Maximum 250 mg/day)

Secondary prevention:
5 mg/kg orally daily (Maximum 250 mg/day) in combination with ethambutol 15 to 25 mg/kg orally daily (Maximum 2.5 g/day); with or without rifabutin 5 mg/kg orally daily (Maximum 300 mg/day)

Disseminated infection due to Mycobacterium avium-intracellulare group HIV infection:
10 to 12 mg/kg orally once daily (Maximum 500 mg/day) in combination with ethambutol
15 to 25 mg/kg orally once daily (Maximum 2.5 g/day); for severe disease; add rifabutin
10 to 20 mg/kg orally once daily (Maximum 300 mg/day)

Lyme disease:
(Alternative to first-line therapy) 10 mg/kg/day orally for 7 to 10 days for early localized or early disseminated Lyme disease associated with erythema migrans or borrelial lymphocytoma; Maximum 500 mg/day.

Pertussis:
(Younger than 6 months)
10 mg/kg/day single dose orally for 5 days

(6 months or older)
10 mg/kg

single dose orally

on day 1 (Maximum 500 mg); then 5 mg/kg/day on days 2 through 5 (Maximum 250 mg) (Guideline dosing)

Streptococcal pharyngitis; alternative to first-line therapy:
12 mg/kg orally once daily for 5 days; Maximum 500 mg/dose (Guideline dosing)

(Tablets and immediate-release suspension; 2 years or older)
12 mg/kg orally daily for 5 days (Manufacturer dosing)

Streptococcal tonsillitis; alternative to first-line therapy:
12 mg/kg orally once daily for 5 days; Maximum 500 mg/dose(Guideline dosing)
(Tablets and immediate-release suspension; 2 years or older)
12 mg/kg orally daily for 5 days (Manufacturer dosing)

Typhoid fever:
20 mg/kg/day (Maximum 1000 mg/day) orally for 5 days

Azithromycin

10 mg/kg/day (Maximum 500 mg/day) orally for 7 days

Indications
FDA-LABELED INDICATIONS:
Acute infective exacerbation of chronic obstructive pulmonary disease (Mild to Moderate)
Acute otitis media
Bacterial conjunctivitis
Bacterial sinusitis; acute (Mild to Moderate)
Chancroid
Community acquired pneumonia (Mild to Moderate)
Gonorrhea; Urethritis or cervicitis
Infection of skin AND/OR subcutaneous tissue; Uncomplicated
Nongonococcal cervicitis
Nongonococcal urethritis
Pelvic inflammatory disease
Streptococcal pharyngitis; alternative to first-line therapy
Streptococcal tonsillitis; alternative to first-line therapy

NON-FDA LABELED INDICATIONS:
Babesiosis
Bacterial endocarditis; Prophylaxis
Bartonellosis HIV infection
Chlamydial infection
Cholera
Cystic fibrosis
Disseminated infection due to Mycobacterium avium-intracellulare group; Prophylaxis HIV infection
Disseminated infection due to Mycobacterium avium-intracellulare group HIV infection
Druginduced gingival hyperplasia
Granuloma inguinale
Helicobacter pylori gastrointestinal tract infection
HIV infection Toxoplasma encephalitis
Legionella infection
Lyme disease
Mycobacterium avium complex infection, Lung disease
Pertussis
Sexually transmitted infectious disease; Prophylaxis Victim of sexual aggression
Shigellosis
Trachoma
Traveler diarrhea
Typhoid fever

Mechanism of Action




Azithromycin acts by binding to the 23S rRNA of the 50S ribosomal subunit of susceptible microorganisms inhibiting bacterial protein synthesis and impeding the assembly of the 50S ribosomal subunit.

Adverse Effect
Common:
Dermatologic:
Injection site reaction (3.1% to 6.5%)

Gastrointestinal:
Abdominal pain (adult; 1.9% to 14%; pediatric; 2% to 4%)
Diarrhea (adult; 4.3% to 12%; pediatric; 7% to 10%)
Flatulence (5%)
Nausea (adult; 3% to 14%; pediatric; 4%)
Vomiting (adult; up to 13%; pediatric; 11% to 14%)

Hepatic:
Increased liver enzymes (less than 1% to 6%)

Neurologic:
Headache (up to 5%)

Ophthalmic:
Abnormal vision (5%)

Serious:
Cardiovascular:
Prolonged QT interval
Torsades de pointes

Dermatologic:
Generalized exanthematous pustulosis
StevensJohnson syndrome
Toxic epidermal necrolysis

Gastrointestinal:
Congenital hypertrophic pyloric stenosis
Hepatic:
Hepatic necrosis; Hepatitis (less than 1%)
Liver failure
Immunologic:
Drug reaction with eosinophilia and systemic symptoms
Hypersensitivity reaction

Musculoskeletal:
Eaton-Lambert syndrome
Myasthenia gravis
Exacerbation of; Myasthenic crisis

Ophthalmic:
Corneal erosion (less than 1%)

Contraindication
Cholestatic jaundice with prior

azithromycin therapy


Hepatic dysfunction with prior azithromycin therapy

Hypersensitivity to azithromycin

or to any product component; erythromycin; or any macrolide or ketolide antibiotic

Interaction
Nelfinavir:
Co-administration of nelfinavir at steady-state with a single oral

dose of azithromycin

resulted in increased azithromycin serum concentrations. Although a dose adjustment of azithromycin is not recommended when administered in combination with nelfinavir; close monitoring for known adverse

reactions of azithromycin

; such as liver enzyme abnormalities and hearing impairment; is warranted

Warfarin:
Spontaneous post-marketing reports suggest that concomitant

administration of azithromycin

may potentiate the effects of oral anticoagulants such as warfarin; although the prothrombin time was not affected in the dedicated drug interaction study with azithromycin and warfarin. Prothrombin times should be carefully monitored while patients are receiving azithromycin and oral anticoagulants concomitantly

Potential:
Drug-Drug Interaction with Macrolides Interactions with the following drugs listed below has not been reported in clinical trials with azithromycin; however; no specific drug interaction studies have been performed to evaluate potential Drug-Drug interaction. However; drug interactions have been observed with other macrolide products. Until further data are developed regarding drug interactions when digoxin or phenytoin are

used with azithromycin

careful monitoring of patients is advised

Phamacokinetics
Absorption:
Time for Maximum Plasma Concentration (Tmax):

Oral Tablets

: 2.2 to 3.2 hours

Parenteral dosage

forms: 1 to 2 hours
IV in pregnancy: 1 hour
Elderly subjects: 3.8 to 4.4 hours

Bioavailability:
38%

Effects of food:
Minimal
No effect on AUC

Distribution:
Volume of Distribution (Vd):
(Intravenous): 33.3 L/kg
(Oral): 31.1 L/kg

Plasma Protein binding:
7% to 51% (concentration dependent)

Metabolism:
Hepatic: 35%

Excretion:
Biliary:
Major route for unchanged drug

Renal:
(Oral): 6% unchanged
(Intravenous): 11% to 14% unchanged

Elimination:
Adults: 68 hours
Pregnancy: 6.7 hours

Precaution
Cardiovascular:
QT interval prolongation has been reported; including cases of torsade de pointes; especially in patients with known or congenital QT prolongation; history of torsade de pointes; bradyarrhythmias; uncompensated heart failure; proarrhythmic conditions; or patients on concomitant drugs known to prolong the QT interval.

Concomitant use:
Avoid class IA (quinidine; procainamide) or class III (dofetilide; amiodarone; sotalol) antiarrhythmics due to increased risk of QT prolongation and torsade de pointes

Dermatologic:
Localized IV site reactions have been reported; avoid higher concentrations; especially above 2 mg/mL.

Hepatic:
Hepatotoxicity; including abnormal liver function; hepatitis; cholestatic jaundice; hepatic necrosis; and hepatic failure; with some fatalities; has been reported; discontinue immediately if signs and symptoms of hepatitis occur.

Hepatic:
Use caution in patients with hepatic impairment since azithromycin mainly eliminated via liver.

Immunologic:
Serious and sometimes fatal allergic reactions; including angioedema; anaphylaxis; and dermatologic reactions such as acute generalized exanthematous pustulosis (AGEP); drug reaction with eosinophilia and systemic symptoms (DRESS); Stevens Johnson syndrome; and toxic epidermal necrolysis; have been reported. Immediate discontinuation recommended; however; recurrence of allergic symptoms without further azithromycin exposure may occur

Immunologic:
Overgrowth of nonsusceptible microorganisms; including fungi; may occur with

prolonged use

; discontinue if superinfection develops
Musculoskeletal: New onset or exacerbation of myasthenia gravis has been reported
Ophthalmic:
Avoid contact lenses if signs/symptoms of bacterial conjunctivitis present

Renal:
Severe renal function impairment (GFR less than 10 mL/min); higher incidence of gastrointestinal adverse events reported)
Special populations: Elderly patients are at possible increased risk of QTinterval prolongation and torsade de pointes
Special populations: Infantile hypertrophic pyloric stenosis has been reported in neonates (treatment up to 42 days of life

Pregnancy Category
B (FDA)
B1 (AUS)

Breast Feeding
Infant Risk is minimal

Monitoring
Symptomatic improvement
Fever
CBC
Hepatic function (history of hepatic impairment)

How to Take or Administration
Intravenous:
Infusion only; does not give IV bolus or IM
Reconstitute with sterile water for injection; dilute in NS, D5W, or LR to final concentration of 1 to 2 mg/mL
Infuse at 1 mg/mL over 3 hours or 2 mg/mL over 1 hour; do not infuse over less than 60 minutes (

500mg dose

)

Ophthalmic:
For topical ophthalmic Use only; do not administer systemically or directly into the anterior chamber of the eye; do not inject subconjunctivally
Avoid touching the tip of applicator to eye or fingers
Shake once prior to each

Use

while bottle is inverted; remove cap while bottle is still inverted
If vomiting occurs within 60 minutes of ingestion, additional antibiotic therapy may be considered, as there would be minimal

azithromycin absorption

within this time period

Oral:
(Extended-release suspension)
Take on an empty stomach (at least 1 hour before or 2 hours following a meal)
If vomiting occurs 60 minutes or greater following a dose, a

second dose

or alternative therapy is not required in patients with normal gastric emptying

(Tablets and immediate-release suspension)
Take with or without food
Do not give simultaneously with aluminum or magnesium containing antacids

(Suspension)
Shake well before measuring dose

Dosage Form
Intravenous Powder for Solution:
500 MG

Oral Powder for Suspension:
1 GM/1 Packet
100 MG/5 ML
200 MG/5 ML

Oral Tablet:
250 MG
500 MG
600 MG

Ophthalmic Solution:
1 %

Oral Powder for Suspension; Extended Release:
2 GM/60 ML

Treatment
MANAGEMENT OF MILD TO MODERATE TOXICITY:
Toxicity following an acute

overdose

is uncommon. Treatment is symptomatic and supportive. Treat significant vomiting and diarrhea with IV fluids; administer antiemetics, as needed. Manage mild hypotension with IV fluids.

MANAGEMENT OF SEVERE TOXICITY:
Treatment is symptomatic and supportive. Treat severe hypotension with IV 0.9% NaCl at 10 to 20 mL/kg. Add dopamine or norepinephrine if unresponsive to fluids. Dysrhythmias should be treated with standard antiarrhythmic drugs, if necessary.

SEIZURES:
Administer IV benzodiazepines; barbiturates or propofol may be needed if seizures persist or recur.

HYPERSENSITIVITY REACTION:
Administer antihistamines, with or without inhaled beta agonists, corticosteroids or epinephrine.

Toxicology
TOXICITY: In general; the macrolide antibiotics are of low order toxicity. However; side effects can be occur even within the therapeutic range of dosing.

Patient Counselling or Clinical Teaching
Advise patient to immediately report signs/symptoms of hepatotoxicity or Clostridium difficile associated diarrhea (severe; watery; or bloody diarrhea)
Counsel patient using ophthalmic solution to avoid using contact lenses with signs/symptoms of bacterial conjunctivitis and to prevent contamination of solution
Ophthalmic solution may cause blurred vision; eye pain; eye irritation; eye pruritus; and facial swelling
Drug may cause headache; dizziness; rash; abdominal pain; dyspepsia; flatulence; nausea; vomiting; or injection site pain (IV)
Instruct patient taking Extended-release suspension to take solution within 12 hours of reconstitution and immediately discard any unused portion
Tell patient taking Extended-release suspension to take dose on an empty stomach and call physician if patient vomits within 1 hour after administration
Advise patient on proper instillation technique for ophthalmic preparation
Instruct patient using oral tablets and regular suspension to avoid concomitant

Use of

aluminum or magnesium containing antacids. The Extended-release suspension may be taken with antacids

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