Azithromycin


Description

Azithromycin is a broad-spectrum macrolide antibiotic with a long half-life and a high degree of tissue penetration [

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Pharmacology

Indication

Azithromycin should be used only to treat or prevent infections that are proven or strongly suspecte... Read more

Pharmacodynamic

Macrolides stop bacterial growth by inhibiting protein synthesis and translation, treating bacterial... Read more

Mechanism of action

In order to replicate, bacteria require a specific process of protein synthesis, enabled by ribosoma... Read more

Absorption

Bioavailability of azithromycin is 37% following oral administration. Absorption is not affected by... Read more

Protein binding

The serum protein binding of azithromycin varies in humans, decreasing from 51% at 0.02 g/mL to 7% a... Read more

Volume of distribution

After oral administration, azithromycin is widely distributed in tissues with an apparent steady-sta... Read more

Clearance

Mean apparent plasma cl=630 mL/min (following single 500 mg oral and i.v. dose) [FDA label]

Half life

Terminal elimination half-life: 68 hours [FDA label]

Route of elimination

Biliary excretion of azithromycin, primarily as unchanged drug, is a major route of elimination. Ove... Read more

Toxicity

**Rat Oral LD50**: >2000 mk/kg [MSDS]

Possible major adverse effects include cardiovascular arrhy...
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Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Pain at injection site US
  • Kind: experimental
    • Percent: 7%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 4-6%
  • Clinical Trial
    Loose stools US
  • Kind: experimental
    • Percent: 4-6%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 1-6%
  • Clinical Trial
    Local inflammation at injection site US
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: <3%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 2-3%
  • Clinical Trial
    Increase in serum phosphate US
  • Kind: experimental
    • Percent: <1
  • Clinical Trial
    Increased bilirubin US
  • Kind: experimental
    • Percent: <1
  • Clinical Trial
    Increased serum alkaline phosphatase US
  • Kind: experimental
    • Percent: <1
  • Clinical Trial
    Increased bicarbonate US
  • Kind: experimental
    • Percent: <1
  • Clinical Trial
    Increased basophils US
  • Kind: experimental
    • Percent: <1
  • Clinical Trial
    Allergic Reactions US
  • Kind: experimental
    • Percent: <1
  • Hyperkinesia US
  • Kind: experimental
    • Percent: <1
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: <1
  • Pruritis US
  • Kind: experimental
    • Percent: <1
  • Heart palpitations US
  • Kind: experimental
    • Percent: <1
  • Clinical Trial
    Conjunctivitis US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Vesiculobullous rash US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Urticaria US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Sweating US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Fungal dermatitis US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Eczema US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Rhinitis US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Pleural Effusion US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Cough US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Pharyngitis US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Pain US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Malaise US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Face edema US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Fungal Infection US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Fever US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Nervousness US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Anemia US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Oral moniliasis US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Leukopenia US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Headache US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Agitation US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Hyperkinesia US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Taste perversion US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Anorexia US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Chest Pain US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Enteritis US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Jaundice US
    • pediatric
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Photosensitivity US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Angioedema US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Bronchospasm US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial
    Gastritis US
  • Kind: experimental
    • Percent: ≤1%
  • Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Cholestatic jaundice
        • Drugbank Id: DBCOND0094562
    • Patient Conditions Associated With:
        • Name: Prior azithromycin use
        • Drugbank Id: DBCOND0117160
    • Regions: US
    • Patient Conditions:
        • Name: Hepatic dysfunction
        • Drugbank Id: DBCOND0094733
    • Patient Conditions Associated With:
        • Name: Prior azithromycin use
        • Drugbank Id: DBCOND0117160
    • Regions: US
    • Patient Conditions:
        • Name: Known hypersensitivity to any ketolide
        • Drugbank Id: DBCOND0117159
    • Regions: US
    • Patient Conditions:
        • Name: Known hypersensitivity to any macrolide
        • Drugbank Id: DBCOND0117158
    • Regions: US
    • Patient Conditions:
        • Name: Known hypersensitivity to erythromycin
        • Drugbank Id: DBCOND0117157
    • Regions: US
    • Patient Conditions:
        • Name: Known hypersensitivity to azithromycin
        • Drugbank Id: DBCOND0117156

    Food Interactions

    • Do not take Aluminum or magnesium antacids or supplements while on this medication.
    • Take on empty stomach: 1 hour before or 2 hours after meals.

    Interactions

    Type in a drug name to check for interaction with Azithromycin

    The risk or severity of adverse effects can be increased when Azithromycin is combined with (R)-warfarin.
    The risk or severity of adverse effects can be increased when Azithromycin is combined with (S)-Warfarin.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Azithromycin.
    The risk or severity of adverse effects can be increased when Azithromycin is combined with 4-hydroxycoumarin.
    The metabolism of 5-androstenedione can be decreased when combined with Azithromycin.
    The metabolism of Azithromycin can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Azithromycin.
    The metabolism of Azithromycin can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Azithromycin.
    The metabolism of Azithromycin can be increased when combined with Abatacept.
    The risk or severity of adverse effects can be increased when Azithromycin is combined with Abciximab.
    The serum concentration of Abemaciclib can be increased when it is combined with Azithromycin.
    The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Abexinostat.
    The metabolism of Abiraterone can be decreased when combined with Azithromycin.
    The metabolism of Azithromycin can be decreased when combined with Acalabrutinib.
    The serum concentration of Acebutolol can be increased when it is combined with Azithromycin.
    The risk or severity of adverse effects can be increased when Azithromycin is combined with Acenocoumarol.
    The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Aceprometazine.
    The serum concentration of Acetaminophen can be increased when it is combined with Azithromycin.
    The metabolism of Azithromycin can be decreased when combined with Acetazolamide.

    References

    • 1 . Noedl H, Krudsood S, Chalermratana K, Silachamroon U, Leowattana W, Tangpukdee N, Looareesuwan S, Miller RS, Fukuda M, Jongsakul K, Sriwichai S, Rowan J, Bhattacharyya H, Ohrt C, Knirsch C: Azithromycin combination therapy with artesunate or quinine for the treatment of uncomplicated Plasmodium falciparum malaria in adults: a randomized, phase 2 clinical trial in Thailand. Clin Infect Dis. 2006 Nov 15;43(10):1264-71. Epub 2006 Oct 12. [PubMed: 17051490]
    • 2 . Peters DH, Friedel HA, McTavish D: Azithromycin. A review of its antimicrobial activity, pharmacokinetic properties and clinical efficacy. Drugs. 1992 Nov;44(5):750-99. doi: 10.2165/00003495-199244050-00007. [PubMed: 1280567]
    • 3 . McMullan BJ, Mostaghim M: Prescribing azithromycin. Aust Prescr. 2015 Jun;38(3):87-9. Epub 2015 Jun 1. [PubMed: 26648627]
    • 4 . Fohner AE, Sparreboom A, Altman RB, Klein TE: PharmGKB summary: Macrolide antibiotic pathway, pharmacokinetics/pharmacodynamics. Pharmacogenet Genomics. 2017 Apr;27(4):164-167. doi: 10.1097/FPC.0000000000000270. [PubMed: 28146011]
    • 5 . Champney WS, Miller M: Inhibition of 50S ribosomal subunit assembly in Haemophilus influenzae cells by azithromycin and erythromycin. Curr Microbiol. 2002 Jun;44(6):418-24. [PubMed: 12000992]
    • 6 . Champney WS, Burdine R: Macrolide antibiotics inhibit 50S ribosomal subunit assembly in Bacillus subtilis and Staphylococcus aureus. Antimicrob Agents Chemother. 1995 Sep;39(9):2141-4. [PubMed: 8540733]
    • 7 . Dinos GP: The macrolide antibiotic renaissance. Br J Pharmacol. 2017 Sep;174(18):2967-2983. doi: 10.1111/bph.13936. Epub 2017 Aug 10. [PubMed: 28664582]
    • 8 . Singlas E: [Clinical pharmacokinetics of azithromycin]. Pathol Biol (Paris). 1995 Jun;43(6):505-11. [PubMed: 8539072]
    • 9 . Zithromax FDA label [File]
    • 10 . Azithromycin, Ophthalmic FDA label [File]
    • 11 . Sandoz Azithromycin Canadian Monograph [File]

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