A-Z Drug Facts > Azithromycin

Azithromycin

Pronouncation: (UHZ-ith-row-MY-sin)
Class: Macrolide

Trade Names:
Zithromax
- Tablets 250 mg (as dihydrate)
- Tablets 500 mg (as dihydrate)
- Tablets 600 mg (as dihydrate)
- Powder for injection, lyophilized 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)

Z-Pak (Canada)

Pharmacology

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Interferes with microbial protein synthesis.

Pharmacokinetics

Absorption

Oral

Rapidly absorbed.

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.

Distribution

Widely distributed into body (skin, lung, sputum, cervix, 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).

Elimination

The t _½ 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).

Indications and Usage

Adults

Treatment of infections of the respiratory tract, acute bacterial sinusitis, acute bacterial exacerbations of COPD, community-acquired pneumonia, Mycobacterium avium complex, pelvic inflammatory disease, pharyngitis/tonsillitis, skin and skin structure infections, and STDs caused by susceptible organisms.

Children

Treatment of acute bacterial sinusitis, acute otitis media caused by susceptible organisms, community-acquired pneumonia, pharyngitis/tonsillitis caused by Streptococcus pyogenes in patients who cannot use first-line therapy.

Contraindications

Hypersensitivity to azithromycin, erythromycin, or to any macrolide antibiotic.

Dosage and Administration

Bacterial Infections
Adults

PO 500 mg as single dose on first day, then 250 mg/day on days 2 through 5.

Acute Bacterial Sinusitis
Adults

PO 500 mg every day for 3 days.

Children 6 mo of age and older

PO 10 mg/kg oral suspension once daily for 3 days.

Acute Otitis Media
Children 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).

Community-Acquired Pneumonia
Adults and children 16 yr of age and older

PO 500 mg as a single dose on the first day followed by 250 mg once daily on days 2 through 5.

Adults

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

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).

Genital Ulcer Disease caused by Haemophilus ducreyi (chancroid), Nongonococcal Urethritis/Cervicitis caused by Chlamydia trachomatis
Adults

PO Single 1 g dose.

Gonorrhea
Adults

PO Single 2 g dose.

Mild to Moderate Acute Bacterial Exacerbations of COPD
Adults and children 16 yr of age and older

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.

M. Avium Complex
Adults

PO Prevention: 1.2 g taken weekly. Treatment: 600 mg/day in combination with ethambutol (15 mg/kg).

Pelvic Inflammatory Disease
Adults

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/Tonsillitis
Adults and children 16 yr of age and older

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 Infections
Adults and children 16 yr of age and older

PO 500 mg as a single dose on the first day followed by 250 mg once daily on days 2 through 5.

General Advice

• Oral suspension/Tablets
• Administer prescribed dose without regard to meals. Administer with food if GI upset occurs.
• Administer tablets with a full glass of water.
• Shake suspension well before measuring dose. Administer prescribed dose of suspension using dosing syringe, dosing spoon, or medicine cup.
• When administering 1,000 mg single dose packet, thoroughly mix entire contents of packet with 60 mL (2 oz) water and have patient drink immediately. Add an additional 60 mL of water, mix, and have patient drink immediately to ensure complete consumption of dosage.
• Administer azithromycin 2 h before or after antacids containing aluminum or magnesium.

• Injection
• For administration by IV infusion only. Not for intradermal, subcutaneous, IM, IV bolus, or intra-arterial administration.
• Reconstitute powder for injection with 4.8 mL sterile water for injection. Shake vial until all of the drug has dissolved. Reconstituted solution contains 100 mg/mL.
• Further dilute reconstituted solution with sodium chloride 0.9% injection, sodium chloride 0.45% injection, D5W, lactated Ringer's solution, dextrose 5% in ½ normal saline, dextrose 5% in lactated Ringer's solution, dextrose 5% in 1/ 3 normal saline. Adding 5 mL of reconstituted solution to 500 mL of diluent provides a final concentration of 1 mg/mL; adding 5 mL of reconstituted solution to 250 mL of diluent provides final concentration of 2 mg/mL.
• Infuse prescribed dose over a period of not less than 60 min.
• Inspect solution visually before administration. Do not administer if solution is cloudy, discolored, or contains particulate matter.
• Discard any unused product. Vials are for single-use only. Do not save medication for future use.

Storage/Stability

Injection

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 (36° to 46°F).

Oral suspension/Tablets

Store tablets and dry powder for oral suspension at 59° to 86°F. Store single dose packets and reconstituted oral suspension in refrigerator or at 41° to 86°F. Use oral suspension within 10 days of reconstitution. Discard oral suspension after full dosing is completed.

Drug Interactions

Aluminum- and magnesium-containing antacids

May reduce the peak serum levels but not the AUC of azithromycin.

Cyclosporine, pimozide, theophyllines

Levels may be elevated by azithromycin, increasing the risk of toxicity.

HMG-CoA reductase inhibitors (eg, lovastatin)

Increased risk of myopathy and rhabdomyolysis.

Nelfinavir

Azithromycin levels may be elevated, increasing the risk of side effects.

Tacrolimus

Increased tacrolimus plasma levels with increased risk of toxicity.

Warfarin

The anticoagulant effect may be increased, increasing the risk of hemorrhage.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations, chest pain; arrhythmias, hypotension, QT prolongation, torsades de pointes (postmarketing).

CNS

Dizziness, headache, vertigo, somnolence, fatigue; agitation, aggressive behavior, anxiety, asthenia, convulsions, hyperactivity, malaise, nervousness, paresthesia, syncope (postmarketing).

Dermatologic

Rash, photosensitivity; erythema multiforme, Stevens-Johnson syndrome, pruritus, toxic epidermal necrolysis, urticaria (postmarketing).

EENT

Deafness, hearing disturbances, hearing loss, tinnitus (postmarketing).

GI

Diarrhea, nausea, vomiting, abdominal pain, dyspepsia, flatulence, melena; anorexia, oral candidiasis, constipation, pseudomembranous colitis, pancreatitis, tongue discoloration (postmarketing).

Genitourinary

Vaginitis, monilia, nephritis; acute renal failure, interstitial nephritis (postmarketing).

Hematologic-Lymphatic

Thrombocytopenia (postmarketing).

Hepatic

Cholestatic jaundice; abnormal LFTs, hepatitis, hepatic failure, hepatic necrosis (postmarketing).

Musculoskeletal

Arthralgia (postmarketing).

Miscellaneous

Angioedema, anaphylaxis; edema (postmarketing).

Precautions

Monitor Sensitivity 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. Notify health care provider if infection does not appear to be improving or is worsening.

Pregnancy

Category B .

Lactation

Undetermined.

Hypersensitivity

Serious reactions, including anaphylaxis, have occurred.

Renal Function

Use cautiously.

Hepatic Function

Use cautiously.

Superinfection

Prolonged use of antibiotics may result in bacterial or fungal overgrowth of nonsusceptible microorganisms.

Cardiac effects

Serious CV events have occurred with other macrolide antibiotics, including prolonged cardiac repolarization and QT interval.

Pneumonia

Only effective for mild community-acquired pneumonia.

Pseudomembranous colitis

May be factor in patients who develop diarrhea.

Patient Information

• Review dosing schedule and prescribed length of therapy with patient. Advise patient that dose, dosing frequency, and duration of therapy are dependent on site and cause of infection.
• Advise patient or caregiver that injection will be prepared by a health care provider and administered in a health care setting.
• Instruct patient using tablets to take prescribed dose with a full glass of water.
• Instruct patient or caregiver using oral suspension to shake suspension well and then measure and administer prescribed dose using dosing spoon, dosing syringe, or medicine cup.
• Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
• Advise patient to take 2 h before or after antacids containing aluminum or magnesium.
• Instruct patient to complete entire course of therapy, even if symptoms of infection have disappeared.
• Advise patient to discontinue therapy and contact health care provider immediately if skin rash, hives, itching, or shortness of breath occur.
• Advise patient to report signs of superinfection to health care provider: black “furry” tongue, white patches in mouth, foul-smelling stools, vaginal itching or discharge.
• Warn patient that diarrhea containing blood or pus may be a sign of a serious disorder and to seek medical care if noted and not treat at home.

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