azithromycin, azithromycin dihydrate

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azithromycin, azithromycin dihydrate

Azasite, Zithromax, Zmax

Pharmacologic class: Macrolide

Therapeutic class: Anti-infective

Pregnancy risk category B

Action

Bactericidal and bacteriostatic; inhibits protein synthesis after binding with 50S ribosomal subunit of susceptible organisms. Demonstrates cross-resistance to erythromycin-resistant gram-positive strains and resistance to most strains of Enterococcus faecalis and methicillin-resistant Staphylococcus aureus.

Availability

Oral suspension: 100 mg/5 ml in 15-ml bottles; 200 mg/5 ml in 15-ml, 22.5-ml, and 30-ml bottles

Oral suspension (Zmax extended-release): 2-g bottle

Powder for injection: 500 mg in 10-ml vials

Powder for oral suspension: 100 mg/5 ml, 200 mg/5 ml, 1,000 mg/packet

Solution (ophthalmic): 1% in 5-ml bottle filled with 2.5 ml solution

Tablets: 250 mg, 500 mg, 600 mg

Tablets (Tri-Pak): three 500-mg tablets

Tablets (Z-Pak): six 250-mg tablets

Indications and dosages

Bacterial conjunctivitis caused by CDC coryneform group G, H. influenzae, S. aureus, Streptococcus mitis group, and S. pneumoniae

Adults: Instill 1 drop in affected eye(s) b.i.d., 8 to 12 hours apart for first 2 days; then instill 1 drop in affected eye(s) once daily for next 5 days

Mild community-acquired pneumonia

Adults: 500 mg P.O. on first day, then 250 mg/day for next 4 days. Or, 2 g P.O. as single dose (extended-release oral suspension).

Children ages 6 months and older: 10 mg/kg P.O. (no more than 500 mg/dose) on day 1, then 5 mg/kg (no more than 250 mg/dose) for 4 more days

Community-acquired pneumonia caused by Chlamydia pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae, Streptococcus pneumoniae, Legionella pneumophila, Moraxella catarrhalis, and S. aureus

Adults and adolescents ages 16 and older: 500 mg I.V. daily for at least two doses, then 500 mg P.O. daily for a total of 7 to 10 days

Children ages 6 months to 16 years: 10 mg/kg P.O. as a single dose on day 1, then 5 mg/kg P.O. on days 2 through 5

Pharyngitis and tonsillitis

Adults: 500 mg P.O. on day 1, then 250 mg/day for next 4 days, to a total dosage of 1.5 g

Children ages 2 and older: 12 mg/kg P.O. daily for 5 days. Maximum dosage is 500 mg.

Skin and skin-structure infections

Adults: 500 mg P.O. on first day, then 250 mg/day for next 4 days, to total dosage of 1.5 g

Acute bacterial sinusitis

Adults: 500 mg P.O. daily for 3 days; or, 2 g P.O. as single dose (extended-release oral suspension)

Children ages 6 months and older: 10 mg/kg (maximum, 500 mg) P.O. daily for 3 days

Mild to moderate acute exacerbation of chronic obstructive pulmonary disease

Adults: 500 mg/day for 3 days or 500 mg P.O. on day 1, then 250 mg P.O. daily on days 2 through 5; or, 2 g P.O. (extended-release oral suspension) as single dose

Pelvic inflammatory disease caused by Chlamydia trachomatis, Neisseria gonorrhoeae, or Mycoplasma hominis

Adults: 500 mg I.V. daily on days 1 and 2, then 250 mg P.O. daily for a total of 7 days. If anaerobes are suspected, give continually with appropriate anti-anaerobic antibiotic, as ordered.

Nongonococcal urethritis or cervicitis caused by C. trachomatis; genital ulcers caused by Haemophilus ducreyi (chancroid)

Adults: 1 g P.O. as a single dose

Urethritis and cervicitis caused by N. gonorrhoeae

Adults: 2 g P.O. as a single dose

To prevent disseminated Mycobacterium avium complex disease in patients with advanced human immunodeficiency virus

Adults: 1.2 g P.O. once weekly (given alone or with rifabutin)

Acute otitis media

Children ages 6 months and older: 30 mg/kg as a single dose or 10 mg/kg once daily for 3 days; or 10 mg/kg as a single dose on day 1, followed by 5 mg/kg on days 2 through 5

Off-label uses

• Uncomplicated gonococcal infections of cervix, urethra, rectum, and pharynx

Contraindications

• Hypersensitivity to drug, erythromycin, or other macrolide antiinfectives
• None (ophthalmic solution)

Precautions

Use cautiously in:
• severe hepatic impairment, severe renal insufficiency, prolonged QT interval
• breastfeeding patients.

Administration

• Obtain specimens for culture and sensitivity testing before starting therapy.
• Administer tablets and single-dose packets with or without food.
• Give oral suspension 1 hour before meals or 2 hours afterward. With 1-g packet, or single 2-g bottles, mix entire contents in 2 oz of water.

Don't administer as I.V. bolus or I.M. injection.
• For I.V. use, reconstitute 500-mg vial with 4.8 ml of sterile water for injection.
• As appropriate, dilute solution further using normal or half-normal saline solution, dextrose 5% in water, or lactated Ringer's solution.
• Infuse injection over no less than 60 minutes. Infuse 1 mg/ml over 3 hours or 2 mg/2 ml over 1 hour.
• Know that 1,000-mg packet and extended-release oral suspension aren't for pediatric use.

Adverse reactions

CNS: dizziness, drowsiness, fatigue, headache, vertigo

CV: chest pain, palpitations

EENT: eye irritation (with ophthalmic use)

GI: nausea, diarrhea, abdominal pain, cholestatic jaundice, dyspepsia, flatulence, melena, pseudomembranous colitis

GU: nephritis, vaginitis, candidiasis

Metabolic: hyperglycemia, hyperkalemia

Skin: photosensitivity, rashes, angioedema

Other: overgrowth of nonsusceptible organisms (with prolonged use)

Interactions

Drug-drug.Antacids containing aluminum or magnesium: decreased peak azithromycin blood level

Arrhythmias (such as amiodarone, quinidine): increased risk of life-threatening arrhythmias

Carbamazepine, cyclosporine, digoxin, dihydroergotamine, ergotamine, hexobarbital, phenytoin, theophylline, triazolam: increased blood levels of these drugs

HMG-CoA reductase inhibitors (such as atorvastatin, lovastatin): increased risk of myopathy or rhabdomyolysis

Pimozide: prolonged QT interval, ventricular tachycardia

Warfarin: increased International Normalized Ratio

Drug-food.Any food: decreased absorption of multidose oral suspension

Drug-behaviors.Sun exposure: photosensitivity

Patient monitoring

• Monitor temperature, white blood cell count, and culture and sensitivity results.
• Assess for signs and symptoms of infection.
• Monitor patients at risk for cardiac arrhythmia.

Patient teaching

• Tell patient he may take tablets with or without food.
• Advise patient to take suspension 1 hour before or 2 hours after meals.
• Remind patient to complete entire course of therapy as ordered, even after symptoms improve.
• Advise patient not to wear contact lenses if signs or symptoms of bacterial conjunctivitis exist.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, foods, and behaviors mentioned above.

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References in periodicals archive ?
It was reported yesterday that the contract has been signed for the development and commercialisation of InSite's innovative ophthalmic therapeutic products, AzaSite (one percent azithromycin), AzaSite Xtra (two percent azithromycin) and BromSite (0.
AzaSite contains the drug azithromycin, a broad-spectrum antibiotic formulated with DuraSite(R), InSite Vision's patented drug-delivery vehicle, which offers the benefit of a less frequent, low-dosing regimen, attractive to both the eye-care patient and physician.
InSite Vision is also advancing three novel ophthalmic therapeutics through Phase 3 clinical studies: AzaSite Plus([TM]) and DexaSite([TM]) for the treatment of eye infections, and BromSite[TM] for pain and inflammation associated with ocular surgery.
The contract has been signed to develop and market InSite's azithromycin ophthalmic solution using DuraSite, including AzaSite 1% and AzaSite Xtra 2%, in Japan.
Ophthalmic products company Senju Pharmaceutical Co revealed on Tuesday the launch of a collaboration and license agreement to develop and market InSite Vision's (Other OTC:INSV) azithromycin ophthalmic solution using DuraSite including AzaSite 1% and AzaSite Xtra 2% ocular antibiotics in Japan.
2 million of external costs for the AzaSite Plus([TM]) and DexaSite([TM]) Phase 3 DOUBle and BromSite([TM]) Phase 3 clinical trials in the quarter.
Pharmaceutical company Akorn Inc (NasdaqGS:AKRX) reported on Friday that it has completed the acquisition of three branded ophthalmic products, AzaSite, COSOPT and COSOPT PF, for USD52.
M2 PHARMA-June 25, 2013-Insite Vision reacquires US development rights for AzaSite Xtra(C)2013 M2 COMMUNICATIONS
InSite Vision Incorporated (OTCBB: INSV) today announced that patient enrollment has been completed in the DOUBle Phase 3 clinical trial of AzaSite Plus (ISV-502) and DexaSite (ISV-305) for the treatment of blepharitis.
M2 EQUITYBITES-October 9, 2013-New Jersey District Court sustains InSite Vision's AzaSite patents(C)2013 M2 COMMUNICATIONS http://www.
M2 PHARMA-June 24, 2013-InSite Vision regains development rights to ocular infection drug AzaSite Xtra, with franchise through 2027(C)2013 M2 COMMUNICATIONS
Under the terms of the AzaSite license agreement, the minimum royalties due to InSite in 2012 total $17 million.