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Azithromycin

Overview

The antimicrobial agents or antibiotics develops during the last 60 years are among the most dramatic examples of the advances of science. The remarkably powerful and specific activity of antimicrobial drug is due to their selectivity for highly specific targets that are either unique to micro-organism or much more important in them than in humans. Azithromycin belongs to a macrolide antibiotic. Azthromycin is a 15-atom lactone macrolide ring compound. Azithromycin is a semisynthetic derivative of Erythromycin obtained by the addition of methylated nitorgen into the lactone ring of Erythromycin. Azithromycin is effective against gram positive bacterias. Antibiotics require constant drug level in body for therapeutic effect. This is achieved by taking the medication at regular interval of time throughout the day and night as prescribed. Azithromycin is important to take the drug for the full time period as prescribed. If you discontinue the therapy, it may result in ineffective treatment.

Category:

  • 6 Anti-infective drugs
  • 6.2 Antibiotics, systemic
  • 6.2.2 Other anti-bacterial drugs
  • 6.2.2.4 Macrolides

Primary Characterstics

Molecular Structure of Azithromycin
. It is of Semi Synthetic origin and belongs to Azalide. It belongs to Antibacterial (Proetin synthesis inhibitor) pharmacological group on the basis of mechanism of action and also classified in Antibiotics pharmacological group.The Molecular Weight of Azithromycin is 785.00.

Pharmacokinetics

Oral absorption of Azithromycin is found to be 34% ±19. Volume of distribution is found to be 31.1 l/kg and plasma protien binding is 51%. Renal Excretion accounts for < 10% unchanged. Also excreted in bile and plasma half life is 68%.

Indications

Contraindications

Azithromycin is contraindicated in conditions like Hepatic impairment,Hypersensitivity.

Drug Interactions

Azithromycin is known to interact with other drugs, the details of drug interactions is as follows:

DrugDetailsSeverityOnsetManagement
Aluminium Hydroxide and OxidePeak serum drug concentration of azithromycin is decreased.Azithromycin should be given 1 hour before or after 2 hour of antacid.
AstemizoleConcomitant use of both drugs may cause QT-interval prolongation; increased risk of cardiac arrhythmias including ventricular tachycardia and Torsade de pointes. The risk of individual agent or combination of these agents causing ventricular arhythmia in association with QT-prolongation is largely unpredictable but may be increased by some underlying risk factors such as congenital long QT syndrome, cardiac disease and electrolyte disturbances (hypokalemia, hypomagnesemia). In addtion, the extent of drug-induced QT-prolongation is dependent on the perticular drug(s) involved and dosage(s) of the drug(s).ModerateCaution and clinical monitoring recommended
Cyclosporin AMacrolides (e.g Azithromycin) possibly inhibit metabolism of Ciclosporin (increased plasma concentration).
DigoxinAzithromycin may increase the serum concentration of Digoxin.ModerateMonitor increased serum concentrations/altered response of Digoxin if Azithromycin is initiated or discontinued, or dosage is modified.
Ergotamine (Tartrate)
Ibrutinibmay increase the AUC of ibrutinib by a factor of < 2-foldmonitor closely
TerfenadineConcomitant use of both drugs may cause QT-interval prolongation; increased risk of cardiac arrhythmias including ventricular tachycardia and Torsade de pointes. The risk of individual agent or combination of these agents causing ventricular arhythmia in association with QT-prolongation is largely unpredictable but may be increased by some underlying risk factors such as congenital long QT syndrome, cardiac disease and electrolyte disturbances (hypokalemia, hypomagnesemia). In addtion, the extent of drug-induced QT-prolongation is dependent on the perticular drug(s) involved and dosage(s) of the drug(s).Caution and clinical monitoring recommended.
TheophyllineAzithromycin possibly increases plasma concentration of Theophylline.
Triazolam

These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Interference in Pathology

  • False elevated serum aspartate

Side Effects

The severe or irreversible adverse effects of Azithromycin, which give rise to further complications include Pseudomembranous colitis, Jaundice, Maculopapular rash, Cholestasis.

Azithromycin produces potentially life-threatening effects which include Anaphylaxis, Angioneurotic edema. which are responsible for the discontinuation of Azithromycin therapy.

The signs and symptoms that are produced after the acute overdosage of Azithromycin include Severe vomiting, Severe diarrhea, severe nausea, Hearing loss.

The symptomatic adverse reactions produced by Azithromycin are more or less tolerable and if they become severe, they can be treated symptomatically, these include Flatulence, Dizziness, Vertigo, Headache, Fatigue, Nausea, Vomiting, Diarrhea, Palpitation, Abdominal pain, Rashes, Photosensitivity, Deafness, GI disturbance.

Available Brands

Click on the appropriate strength of the dosage form to view its available brands.

Single Ingredient

Inj: 500 mg,
Inf: 500 mg,
Susp: 50 mg/5ml, 100 mg/5ml, 125 mg/5ml, 200 mg/5ml, 250 mg/5ml,
Tabs: 250 mg, 500 mg,
Caps: 250 mg, 500 mg,

Multi ingredient

Tabs: 250 mg,

Dosage

Azithromycin's dosage details are as follows:
Dose Single Dose Frequency Route Instructions

Adult Dosage

250 to 2000 mg1100 (1125)24 hourlyPODose and duration may vary according to indication.

Paedriatic Dosage ( 20 Kg. )

20 mg/kg20 (20)As recommended.OralAs Required

Neonatal Dosage ( 3 Kg. )

6.25 to 12.5 mg/kg9.4 (9.375)As recommended.oralAs required

High Risk Groups

Drug should not be given to Pregnant Mothers, patients suffering from Kidney dysfunction, patients suffering from Liver Malfunction, and Neonates.

If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.

Warning / Precautions

Azithromycin should be used with caution in patients with illness or any allergy, especially allergies to drugs, liver disease, jaundice, history of colitis or stomach problems or kidney disease.This drug should be used only if clearly needed during pregnancy or lactation.

Storage Conditions

Tab, Caps, Oral Susp

Store Below 40°C. Protect from Sunlight and Moisture.

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