1. Name of the medicinal product
Azithromycin 500 mg film-coated tablets
2. Qualitative and quantitative composition
Each film-coated tablet contains 500 mg of azithromycin (as dihydrate).
Excipient with known effect: Each film-coated tablet contains 10.80 mg lactose monohydrate.
For the full list of excipients, see section 6.1.
3. Pharmaceutical form
Azithromycin Ritisca 500 mg film-coated tablets:
White to off-white, oval shaped, film coated biconvex tablets debossed with “6” and “7” on either side of the score-line on one side and “D” on other side. The tablet can be divided into equal doses. The size is 17.1 mm x 8.5 mm.
4. Clinical particulars
4.1 Therapeutic indications
Azithromycin is indicated for the following bacterial infections induced by microorganisms susceptible to azithromycin (see sections 4.4 and 5.1):
• Acute bacterial sinusitis (adequately diagnosed)
• Acute bacterial otitis media (adequately diagnosed)
• Pharyngitis, tonsillitis
• Acute exacerbation of chronic bronchitis (adequately diagnosed)
• Mild to moderately severe community acquired pneumonia
• Infections of the skin and soft tissues of mild to moderate severity e.g. folliculitis, cellulitis, erysipelas
• Uncomplicated Chlamydia trachomatis urethritis and cervicitis
Consideration should be given to official guidance on the appropriate use of antibacterial agents.
4.2 Posology and method of administration
Azithromycin should be given as a single daily dose. Duration of the treatment for the different infection diseases is given below.
Children and adolescents with a body weight above 45 kg, adults and the elderly
The total dose is 1500 mg, administered as 500 mg once daily for 3 days. Alternatively, the same total dose (1500 mg) can be administered in a period of 5 days, 500 mg on the first day and 250 mg on day 2 to 5.
In the case of uncomplicated Chlamydia trachomatis urethritis and cervicitis, the dose is 1000 mg as a single oral dose.
Children and adolescents with a body weight below 45 kg
Azithromycin tablets are not suitable for patients under 45 kg body weight. Other dosage forms are available for this group of patients.
For elderly patients the same dose as for adults can be applied. Since elderly patients can be patients with ongoing proarrhythmic conditions a particular caution is recommended due to the risk of developing cardiac arrhythmia and torsades de pointes. (see section 4.4).
Patients with renal impairment
Dose adjustment is not required in patients with mild to moderate renal impairment (GFR 10-80 ml/min) Caution should be exercised when azithromycin is administered to patients with severe renal impairment (GFR < 10 ml/min) (see section 4.4 and section 5.2).
Patients with hepatic impairment
Dose adjustment is not required for patients with mild to moderate hepatic dysfunction (see section 4.4).
Method of administration
Azithromycin Aurovitas should be given as a single daily dose. The tablets can be taken with or without food. The tablets should be taken with ½ glass of water.
Hypersensitivity to the active substance, erythromycin, any macrolide, ketolide antibiotic, or to any of the excipient listed in section 6.1.
4.4 Special warnings and precautions for use
As with erythromycin and other macrolides, rare serious allergic reactions, including angioneurotic oedema and anaphylaxis (rarely fatal), dermatologic reactions including acute generalized exanthematous pustulosis (AGEP), Stevens Johnson syndrome (SJS), toxic epidermal necrolysis (TEN) (rarely fatal) and drug reaction with eosinophilia and systemic symptoms (DRESS) have been reported. Some of these reactions with <product name> have resulted in recurrent symptoms and required a longer period of observation and treatment.
If an allergic reaction occurs, the medicinal product should be discontinued and appropriate therapy should be instituted. Physicians should be aware that reappearance of the allergic symptoms may occur when symptomatic therapy is discontinued.
Since the liver is the principal route of elimination for azithromycin, the use of azithromycin should be undertaken with caution in patients with significant hepatic disease. Cases of fulminant hepatitis potentially leading to life-threatening liver failure have been reported with azithromycin (see section 4.8). Some patients may have had pre-existing hepatic disease or may have been taking other hepatotoxic medicinal products.
In case of signs and symptoms of liver dysfunction, such as rapid developing asthenia associated with jaundice, dark urine, bleeding tendency or hepatic encephalopathy, liver function tests/ investigations should be performed immediately. Azithromycin administration should be stopped if liver dysfunction has emerged.
Ergot alkaloids and azithromycin
In patients receiving ergot derivatives, ergotism has been precipitated by coadministration of some macrolide antibiotics. There are no data concerning the possibility of an interaction between ergotamine derivatives and azithromycin. However, because of the theoretical possibility of ergotism, azithromycin and ergot derivatives should not be co-administered (see section 4.5).
As with any antibiotic preparation, it is recommended to pay attention to signs of superinfection with nonsusceptible microorganisms like fungi. A superinfection may require an interruption of the azithromycin treatment and initiation of adequate measures.
Clostridium difficile associated diarrhoea (CDAD) has been reported with use of nearly all antibacterial agents, including azithromycin, and may range in severity from mild diarrhoea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.
C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C.difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhoea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents. In case of CDAD anti-peristaltics are contraindicated.
In patients with severe renal impairment (GFR < 10 ml/min) a 33% increase in systemic exposure to azithromycin was observed (see section 5.2).
Prolonged cardiac repolarisation and QT interval, imparting a risk of developing cardiac arrhythmia and torsades de pointes, have been seen in treatment with other macrolides, including azithromycin (see section 4.8). Therefore as the following situations may lead to an increased risk for ventricular arrhythmias (including torsade de pointes) which can lead to cardiac arrest, azithromycin should be used with caution in patients with ongoing proarrhythmic conditions (especially women and elderly patients) such as patients:
- With congenital or documented acquired QT prolongation.
- Currently receiving treatment with other active substances known to prolong QT interval such as antiarrhythmics of class IA (quinidine and procainamide) and class III (dofetilide, amiodarone and sotalol), cisapride and terfenadine; antipsychotic agents such as pimozide; antidepressants such as citalopram; and fluoroquinolones such as moxifloxacin and levofloxacin.
- With electrolyte disturbance, particularly in cases of hypokalaemia and hypomagnesaemia
- With clinically relevant bradycardia, cardiac arrhythmia or severe cardiac insufficiency.
Epidemiological studies investigating the risk of adverse cardiovascular outcomes with macrolides have shown variable results. Some observational studies have identified a rare short term risk of arrhythmia, myocardial infarction and cardiovascular mortality associated with macrolides including azithromycin. Consideration of these findings should be balanced with treatment benefits when prescribing azithromycin.
Exacerbations of the symptoms of myasthenia gravis and new onset of myasthenia syndrome have been reported in patients receiving azithromycin therapy (see section 4.8).
Safety and efficacy for the prevention or treatment of Mycobacterium avium complex in children have not been established.
The following should be considered before prescribing azithromycin:
Azithromycin Aurovitas is not suitable for treatment of severe infections where a high concentration of the antibiotic in the blood is rapidly needed.
The selection of azithromycin to treat an individual patient should take into account the appropriateness of using a macrolide antibacterial agent based on adequate diagnosis to ascertain the bacterial etiology of the infection in the approved indications and the prevalence of resistance to azithromycin or other macrolides.
In areas with a high incidence of erythromycin A resistance, it is especially important to take into consideration the evolution of the pattern of susceptibility to azithromycin and other antibiotics.
As for other macrolides, high resistance rates of Streptococcus pneumoniae (> 30 %) have been reported for azithromycin in some European countries (see section 5.1). This should be taken into account when treating infections caused by Streptococcus pneumoniae.
Azithromycin is not the substance of first choice for the treatment of pharyngitis and tonsillitis caused by Streptococcus pyogenes. For this and for the prophylaxis of acute rheumatic fever penicillin is the treatment of first choice.
Often, azithromycin is not the substance of first choice for the treatment of sinusitis.
Acute otitis media
Often, azithromycin is not the substance of first choice for the treatment of acute otitis media.
Skin and soft tissue infections
The main causative agent of soft tissue infections, Staphylococcus aureus, is frequently resistant to azithromycin. Therefore, susceptibility testing is considered a precondition for treatment of soft tissue infections with azithromycin.
Infected burn wounds:
Azithromycin is not indicated for the treatment of infected burn wounds.
Sexually transmitted disease:
In case of sexually transmitted diseases a concomitant infection by T. pallidium should be excluded.
Neurological or psychiatric diseases:
Azithromycin should be used with caution in patients with neurological or psychiatric disorders.
Patients with rare hereditary problems of galactose intolerance, the total lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Azithromycin contains less than 1 mmol (23 mg) of sodium per tablet, that is to say it is essentially 'sodium-free.'
4.5 Interaction with other medicinal products and other forms of interaction
In a pharmacokinetic study investigating the effects of simultaneous administration of antacids with azithromycin, no effect on overall bioavailability was seen, although peak serum levels were reduced by approximately 25%. In patients receiving both azithromycin and antacids, the medicinal products should not be taken simultaneously. Azithromycin must be taken at least 1 hour before or 2 hours after antacids.
Co-administration of azithromycin prolonged-release granules for oral suspension with a single 20 ml dose of co-magaldrox (aluminium hydroxide and magnesium hydroxide) did not affect the rate and extent of azithromycin absorption.
Co-administration of a 600 mg single dose of azithromycin and 400 mg efavirenz daily for 7 days did not result in any clinically significant pharmacokinetic interactions.
In healthy volunteers, coadministration of a 5-day regimen of azithromycin with cetirizine 20 mg at steady-state resulted in no pharmacokinetic interaction and no significant changes in the QT interval.
Didanosins (Dideoxyinosine): Coadministration of 1200 mg/day azithromycin with 400 mg/day didanosine in 6 HIV- positive subjects did not appear to affect the steady-state pharmacokinetics of didanosine as compared with placebo.
Digoxin (P-gp substrates) and colchicine:
Concomitant administration of macrolide antibiotics, including azithromycin, with P-glycoprotein substrates such as digoxin, has been reported to result in increased serum levels of the P-glycoprotein substrate. Therefore, if azithromycin and P-gp substrates such as digoxin are administered concomitantly, the possibility of elevated serum concentrations of the substrate should be considered.
Single 1000 mg doses and multiple doses of 600 mg or 1200 mg azithromycin had little effect on the plasma pharmacokinetics or urinary excretion of zidovudine or its glucuronide metabolite. However, administration of azithromycin increased the concentrations of phosphorylated zidovudine, the clinically active metabolite, in peripheral blood mononuclear cells. The clinical significance of this finding is unclear, but it may be of benefit to patients.
Azithromycin does not interact significantly with the hepatic cytochrome P450 system. It is not believed to undergo the pharmacokinetic drug interactions as seen with erythromycin and other macrolides. Hepatic cytochrome P450 induction or inactivation via cytochrome metabolite complex does not occur with azithromycin.
Due to the theoretical possibility of ergotism, the concurrent use of azithromycin with ergot derivatives is not recommended (see section 4.4).
Pharmacokinetic studies have been conducted between azithromycin and the following drugs known to undergo significant cytochrome P450 mediated metabolism.
There are no known data on interactions with astemizole or alfentanil. Caution is advised in the coadministration of these medicines with Azithromycin because of the known enhancing effect of these medicines when used concurrently with the macrolide antibiotic erythromycin.
Coadministration of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not alter the plasma concentrations of atorvastatin (based on a HMG CoA-reductase inhibition assay). However, postmarketing cases of rhabdomyolysis in patients receiving azithromycin with statins have been reported.
In a pharmacokinetic interaction study in healthy volunteers, no significant effect was observed on the plasma levels of carbamazepine or its active metabolite in patients receiving concomitant azithromycin.
Cisapride is metabolized in the liver by the enzyme CYP 3A4. Because macrolides inhibit this enzyme, concomitant administration of cisapride may cause the increase of QT interval prolongation, ventricular arrhythmias and torsades de pointes.
Cimetidine: In a pharmacokinetic study investigating the effects of a single dose of cimetidine, given 2 hours before azithromycin, on the pharmacokinetics of azithromycin, no alteration of azithromycin pharmacokinetics was seen.
Coumarin Type Oral Anticoagulants:
In a pharmacokinetic interaction study, azithromycin did not alter the anticoagulant effect of a single 15-mg dose of warfarin administered to healthy volunteers. There have been reports received in the postmarketing period of potentiated anticoagulation subsequent to coadministration of azithromycin and coumarin type oral anticoagulants. Although a causal relationship has not been established, consideration should be given to thefrequency of monitoring prothrombin time when azithromycin is used in patients receiving coumarintypeoral anticoagulants.
In a pharmacokinetic study with healthy volunteers that were administered a 500 mg/day oral dose of azithromycin for 3 days and were then administered a single 10 mg/kg oral dose of cyclosporin, the resulting cyclosporin Cmax and AUC0-5 were found to be significantly elevated. Consequently, caution should be exercised before considering concurrent administration of these drugs. If coadministration of these drugs is necessary, cyclosporin levels should be monitored and the dose adjusted accordingly.
Coadministration of a 600 mg single dose of azithromycin and 400 mg efavirenz daily for 7 days did not result in any clinically significant pharmacokinetic interactions.
Coadministration of a single dose of 1200 mg azithromycin did not alter the pharmacokinetics of a single dose of 800 mg fluconazole. Total exposure and halflife of azithromycin were unchanged by the coadministration of fluconazole, however, a clinically insignificant decrease in Cmax (18%) of azithromycin was observed.
Coadministration of a single dose of 1200 mg azithromycin had no statistically significant effect on the pharmacokinetics of indinavir administered as 800 mg three times daily for 5 days.
In a pharmacokinetic interaction study in healthy volunteers, azithromycin had no significant effect on the pharmacokinetics of methylprednisolone.
In healthy volunteers, coadministration of azithromycin 500 mg/day for 3 days did not cause clinically significant changes in the pharmacokinetics and pharmacodynamics of a single 15 mg dose of midazolam.
Coadministration of azithromycin (1200 mg) and nelfinavir at steady state (750 mg three times daily) resulted in increased azithromycin concentrations. No clinically significant adverse effects were observed and no dose adjustment is required.
Coadministration of azithromycin and rifabutin did not affect the serum concentrations of either medicinal product. Neutropenia was observed in subjects receiving concomitant treatment of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship to combination with azithromycin has not been established (see section 4.8).
In normal healthy male volunteers, there was no evidence of an effect of azithromycin (500 mg daily for 3days) on the AUC and Cmax of sildenafil or its major circulating metabolite.
Pharmacokinetic studies have reported no evidence of an interaction between azithromycin and terfenadine. There have been rare cases reported where the possibility of such an interaction could not be entirely excluded; however there was no specific evidence that such an interaction had occurred.
Theophylline: There is no evidence of a clinically significant pharmacokinetic interaction when azithromycin and theophylline are co-administered to healthy volunteers. As interactions of other macrolides with theophylline have been reported, alertness to signs that indicate a rise in theophylline levels is advised.
In 14 healthy volunteers, coadministration of azithromycin 500 mg on Day 1 and 250 mg on Day 2 with 0.125 mg triazolam on Day 2 had no significant effect on any of the pharmacokinetic variables for triazolam compared to triazolam and placebo.
Coadministration of trimethoprim/sulfamethoxazole DS (160 mg/800 mg) for 7 days with azithromycin 1200 mg on Day 7 had no significant effect on peak concentrations, total exposure or urinary excretion of either trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were similar to those seen in other studies.
4.6 Fertility, pregnancy and lactation
There are no adequate data from the use of azithromycin in pregnant women. In reproduction toxicity studies in animals azithromycin was shown to pass the placenta, but no teratogenic effects were observed (see section 5.3). The safety of azithromycin has not been confirmed with regard to the use of the active substance during pregnancy. Therefore azithromycin should only be used during pregnancy if the benefit outweighs the risk.
Azithromycin has been reported to be secreted into human breast milk, but there are no adequate and well controlled clinical studies in nursing women that have characterized the pharmacokinetics of azithromycin excretion into human breast milk.
Because it is not known whether azithromycin may have adverse effects on the breast-fed infant, nursing should be discontinued during treatment with azithromycin. Among other things diarrhoea, fungus infection of the mucous membrane as well as sensitisation is possible in the nursed infant. It is recommended to discard the milk during treatment and up until 2 days after discontinuation of treatment. Nursing may be resumed thereafter.
In fertility studies conducted in rat, reduced pregnancy rates were noted following administration of azithromycin. The relevance of this finding to humans is unknown.
4.7 Effects on ability to drive and use machines
No data are available regarding the influence of azithromycin on a patient's ability to drive or operate machinery. However, the possibility of undesirable effects like dizziness and convulsions should be taken into account when performing these activities. Visual impairment and vision blurred may have an effect on a patient's ability to drive or operate machinery (section 4.8).
4.8 Undesirable effects
The table below lists the adverse reactions identified through clinical trial experience and post-marketing surveillance by system organ class and frequency. Adverse reactions identified from post-marketing experience are included in italics.
The frequency grouping is defined using the following convention: Very common (≥1/10); Common (≥ 1/100 to <1/10);Uncommon (≥1/1,000 to <1/100); Rare (≥ 1/10,000 to <1/1,000); Very Rare (< 1/10,000);and Not known (cannot be estimated from the available data). Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.
Adverse reactions possibly or probably related to azithromycin based on clinical trial experience and post-marketing surveillance:
≥ 1/100 to < 1/10
≥ 1/1,000 to < 1/100
≥ 1/10,000 to <1/1,000
frequency cannot be estimated from available data
Infections and infestations
Pseudo-membranous colitis (see section 4.4)
Blood and lymphatic system disorders
Immune system disorders
Anaphylactic reaction (see section 4.4.)
Metabolism and nutrition disorders
Nervous system disorders
Myasthenia gravis (see section 4.4)
Ear and labyrinth disorders
Torsades de pointes (see section 4.4)
Arrhythmia (see section 4.4) including ventricular tachycardia
Electro-cardiogram QT prolonged (see section 4.4)
Respiratory, thoracic and mediastinal disorders
Tongue and teeth discoloration
Hepatic function abnormal
Hepatic failure (which has rarely resulted in death) (see section 4.4)
Skin and subcutaneous tissue disorders
Allergic reactions including
Acute generalised exanthematous pustulosis (AGEP)
Toxic epidermal necrolysis
Multiforme DRESS (Drug reaction with eosinophilia and systemic symptoms)
Musculoskeletal and connective tissue disorders
Renal and urinary disorders
Renal failure acute
Reproductive system and breast disorders
General disorders and administration site conditions
Lymphocyte count decreased
Eosinophil count increased
Blood bicarbonate decreased
Aspartate aminotransferase increased
Blood bilirubin increased
Blood urea increased
Blood creatinine increased
Blood potassium abnormal
Blood alkaline phosphatase increased
Electrocardiogram QT prolonged (see section 4.4)
Injury and poisoning
Post procedural complications
Adverse reactions possibly or probably related to Mycobacterium Avium Complex prophylaxis and treatment based on clinical trial experience and post-marketing surveillance. These adverse reactions differ from those reported with immediate release or the prolonged release formulations, either in kind or in frequency:
System Organ Class
Metabolism and Nutrition Disorders
Nervous System Disorders
Ear and Labyrinth Disorders
Skin and Subcutaneous Tissue
Musculoskeletal and Connective
General Disorders and Administration
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.
Adverse events experienced in higher than recommended doses were similar to those seen at normal doses.
The typical symptoms of an overdose with macrolide antibiotics include reversible loss of hearing, severe nausea, vomiting and diarrhoea.
In the event of overdose, general symptomatic and supportive measures are indicated as required.
5. Pharmacological properties
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Antibacterials for systemic use, macrolides. ATC code: J01FA10.
Azithromycin is a macrolide antibiotic belonging to the azalide group.
The molecule is constructed by adding a nitrogen atom to the lactone ring of erythromycin A. The chemical name of azithromycin is 9-deoxy-9a-aza-9a-methyl-9a-homoerythromycin A. The molecular weight is 749.0.
Mechanism of action
Azithromycin is an azalide, a sub-class of the macrolide antibiotics. By binding to the 50S ribosomal sub-unit, azithromycin avoids the translocation of peptide chains from one side of the ribosome to the other. As a consequence of this, RNA-dependent protein synthesis in sensitive organisms is prevented.
For azithromycin the AUC/MIC is the major PK/PD parameter correlating best with the efficacy of azithromycin.
Mechanism of resistance:
Resistance to azithromycin may be inherent or acquired. There are three main mechanisms of resistance in bacteria: target site alteration, alteration in antibiotic transport and modification of the antibiotic.
Following the assessment of studies conducted in children, the use of azithromycin is not recommended for the treatment of malaria, neither as monotherapy nor combined with chloroquine or artemisinin based drugs, as non-inferiority to anti-malarial drugs recommended in the treatment of uncomplicated malaria was not established.
Complete cross resistance exists among Streptococcus pneumoniae, betahaemolytic streptococcus of group A, Enterococcus faecalis and Staphylococcus aureus, including methicillin resistant S. aureus (MRSA) to erythromycin, azithromycin, other macrolides and lincosamides.
EUCAST (European Committee on Antimicrobial Susceptibility Testing)
MIC breakpoint (mg/L)
Streptococcus spp. (Group A, B, C, G)
Note1: Clinical evidence for the efficacy of macrolides in H. influenzae respiratory infections is conflicting due to high spontaneous cure rates. Should there be a need to test any macrolide against this species, the epidemiological cut-offs (ECOFFs) should be used to detect strains with acquired
The prevalence of acquired resistance may vary geographically and with time for selected species and local information on resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local prevalence of resistance is such that the utility of the agent in at least some types of infections is questionable.
Pathogens for which resistance may be a problem: prevalence of resistance is equal to or greater than 10% in at least one country in the European Union.
Table of susceptibility
Commonly susceptible species.
Aerobic Gram-negative microorganisms
Species for which acquired resistance may be a problem
Aerobic Gram-positive microorganisms
Inherently resistant organisms
Aerobic Gram-positive microorganisms
Staphylococcus aureus – methicillin resistant and erythromycin resistant strains
Streptococcus pneumoniae – penicillin resistant strains
Aerobic Gram-negative microorganisms
Anaerobic Gram-negative microorganisms
* Clinical effectiveness is demonstrated by sensitive isolated organisms for approved clinical indications.
5.2 Pharmacokinetic properties
Bioavailability of azithromycin after oral administration is approximately 37%. Peak plasma concentrations are attained after 2-3 hours. The mean maximum concentration observed (Cmax) after a single dose of 500 mg is approximately 0.4 μg/ml.
Orally administered azithromycin is widely distributed throughout the body.
Pharmacokinetic studies have demonstrated that the concentrations of azithromycin measured in tissues are noticeably higher (up to 50 times the maximum observed concentration in plasma) than those measured in plasma. This indicates that the agent strongly binds to tissues (steady-state distribution volume approx. 31 l/kg).
At the recommended dose no accumulation appears in the serum. Accumulation appears in tissues where levels are much higher than in serum. Three days after administration of 500 mg as a single dose or in partial doses concentrations of 1,3-4,8 μg/g, 0,6-2,3 μg/g, 2,0-2,8 μg/g and 0-0,3 μg/ml have been measured in resp. lung, prostate, tonsil and serum.
In experimental in vitro and in vivo studies azithromycin accumulates in phagocytes. Release is stimulated by active phagocytosis. In animal models this process contributes to the accumulation of azithromycin in tissue.
Binding of azithromycin to serum proteins is variable and varies from 50% at 0,05 mg/l to 18% at 0,5 mg/l, depending on the serum concentration.
The terminal plasma elimination half-life closely reflects the elimination half-life from tissues of 2-4 days.
Approximately 12% of an intravenously administered dose is excreted in unchanged form with the urine over a period of 3 days; the major proportion in the first 24 hours. Concentrations of up to 237 μg/ml azithromycin, 2 days after a 5-day course of treatment, have been found in human bile. Ten metabolites have been identified (formed by N and O demethylation, by hydroxylation of the desosamine and aglycone rings, and by splitting of the cladinose conjugate). Investigations suggest that the metabolites do not play a role in the microbiological activity of azithromycin.
Pharmacokinetics in Special populations:
Following a single oral dose of azithromycin 1 g, mean Cmax and AUC0-120 increased by 5.1% and 4.2% respectively, in subjects with mild to moderate renal impairment (glomerular filtration rate of 10-80 ml/min) compared with normal renal function (GFR > 80ml/min). In subjects with severe renal impairment, the mean Cmax and AUC0-120 increased 61% and 33% respectively compared to normal.
In patients with mild to moderate hepatic impairment, there is no evidence of a marked change in serum pharmacokinetics of azithromycin compared to normal hepatic function. In these patients, urinary recovery of azithromycin appears to increase perhaps to compensate for reduced hepatic clearance.
The pharmacokinetics of azithromycin in elderly men was similar to that of young adults; however, in elderly women, although higher peak concentrations (increased by 30-50%) were observed, no significant accumulation occurred.
In elderly volunteers (> 65 years) higher (29%) AUC values have been measured after a 5 day treatment than in younger volunteers (< 45 years). These differences are not regarded as clinically relevant; dose adjustment is therefore not recommended.
Infants, toddlers, children and adolescents:
Pharmacokinetics has been studied in children aged 4 months – 15 years taking capsules, granules or suspension. At 10 mg/kg on day 1 followed by 5 mg/kg on days 25, the Cmax achieved is slightly lower than in adults, with 224 μg/l in children aged 0.6-5 years and after 3 days dosing, and 383 μg/l in those aged 6-15 years. The half-life of 36 h in the older children was within the expected range for adults.
5.3 Preclinical safety data
In animal studies using exposures 40 times those achieved at the clinical therapeutic dosages, azithromycin was found to have caused reversible phospholipidosis, but as a rule there were no associated toxicological consequences. The relevance of this finding to humans receiving azithromycin in accordance with the recommendations is unknown.
Electrophysiological investigations have shown that azithromycin prolongs the QT interval.
Long-term studies in animals have not been performed to evaluate carcinogenic potential.
There was no evidence of a potential for genetic and chromosome mutations in in-vivoand in-vitro test models.
Teratogenic effects were not observed in rat reproductive toxicity studies. In rats, azithromycin doses of 100 and 200 mg/kg body weight/ day led to mild retardation in foetal ossification and in maternal weight gain. In peri- and postnatal studies in rats mild retardations in physical and reflex development were noted following treatment with 50 mg/kg/day azithromycin and above.
6. Pharmaceutical particulars
6.1 List of excipients
Calcium hydrogen phosphate, anhydrous
Starch, pregelatinized (maize starch)
Sodium lauryl sulfate
Titanium dioxide (E 171)
6.3 Shelf life
6.4 Special precautions for storage
This medicinal product does not require any special storage conditions.
6.5 Nature and contents of container
Azithromycin film-coated tablets are available in clear PVC- Aluminium blister packs.
Blister packs: 2, 3, 4, 6 and 12 film-coated tablets
Not all pack sizes may be marketed.
6.6 Special precautions for disposal and other handling
Any unused medicinal product or waste material should be disposed of in accordance with local requirements
7. Marketing authorisation holder
Odyssey Business Park, West End Road
8. Marketing authorisation number
9. Date of first authorisation/renewal of the authorisation
10. Date of revision of the text
Azithromycin is used to treat certain bacterial infections, such as bronchitis; pneumonia; sexually transmitted diseases (STD); and infections of the ears, lungs, sinuses, skin, throat, and reproductive organs.Is azithromycin 500 mg safe? ›
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Azithromycin is marketed under the brand names Zithromax and Zmax. FDA-approved indications for azithromycin include: Acute bacterial exacerbations of chronic obstructive pulmonary disease. Acute bacterial sinusitis.What is the side effects of azithromycin 500mg? ›
- Feeling sick (nausea) Stick to simple meals and do not eat rich or spicy food while you're taking this medicine.
- Diarrhoea. ...
- Being sick (vomiting) ...
- Losing your appetite. ...
- Headaches. ...
- Feeling dizzy or tired. ...
- Changes to your sense of taste.
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Pre-clinical studies have shown immunomodulatory and in vitro activity of azithromycin against SARS CoV-2, which has led to its widespread usage in COVID-19.Is azithromycin good against Covid? ›
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If you are taking aluminum or magnesium-containing antacids, do not take them at the same time that you take Zithromax®. These medicines may keep azithromycin from working properly. However, you can take antacids with Zmax®.
Azithromycin oral tablet doesn't cause drowsiness, but it can cause other side effects.Is azithromycin a good antibiotic? ›
Azithromycin is a popular antibiotic medication that treats a variety of health conditions. It works by stopping the growth of certain types of bacteria. It does not work against viruses. Z-Paks are easy to use, generally affordable, and highly effective.Should I be worried about azithromycin? ›
For the vast majority of people, it is perfectly safe to take azithromycin.How long does it take to recover from azithromycin? ›
Generally it takes 5.5 x half-life for a drug to be removed from the body, when it is deemed to no longer have an effect. Therefore for Zithromax it would take about 374 hours (5.5 x 68 hours) which is 15.5 days to be removed from the body.
It takes 7 days for the medicine to work in your body and cure Chlamydia infection. If you have sex without a condom during the 7 days after taking the medicine, you could still pass the infection to your sex partners, even if you have no symptoms.Can azithromycin cause permanent heart damage? ›
Azithromycin can cause what's known as a prolonged QT interval, when the electrical system in the heart takes longer than it should to recharge between beats. This delay is visible on an EKG, and can lead to a potentially fatal abnormal heart rhythm, says Dr. Virani.What does azithromycin do to the brain? ›
Impact: AZ treatment decreases sensorimotor impairment and severity of brain injury, and improves survival, after inflammation-amplified HI brain injury, and this can be achieved even with a 2 h delay in initiation.Can azithromycin raise blood pressure? ›
Treatment with erythromycin was found to increase the risk of low blood pressure almost 6-fold, while clarithromycin increased the risk almost 4-fold. In contrast, azithromycin did not increase the risk of hypotension.How do you know if azithromycin is working? ›
Azithromycin starts working soon after you take your first dose. Oral azithromycin usually needs about 2 to 3 hours to reach its full concentration in your body, but the effects might not be noticeable right away. You should start to feel better after a few days of taking azithromycin.Does azithromycin make your heart race? ›
Also sold under the names Zithromax and Zmax, and often called a Z-pack, the antibiotic can cause changes in the electrical system of the heart, leading to arrhythmia. The medication can also trigger a form of rapid heartbeat called torsades de pointes.
The hepatocellular forms of liver injury from azithromycin can be severe and lead to acute liver failure and death or need for emergency liver transplantation. However, in most cases, recovery occurs within 4 to 8 weeks.Can antibiotics damage your heart? ›
Certain antibiotics can cause painful and sometimes fatal damage to the body's main artery, the Food and Drug Administration said Thursday. Fluoroquinolone antibiotics might raise the risk of an aortic dissection, and people who are already at risk should be cautious about taking those antibiotics, the FDA said.Why do doctors prescribe azithromycin for Covid? ›
Azithromycin (Zithromax) is the most consistently studied antibiotic for use in treating patients infected with the SARS-CoV-2 virus; it does not improve mortality after 28 days or affect the clinical course for hospitalized adults with COVID-19.
Will I need antibiotics for COVID-19? No, because antibiotics are not effective against viruses. Antibiotics are designed to treat bacterial infections.How long should I take azithromycin for Covid? ›
We recommend formal clinical trials of azithromycin in its prepackaged form at the first sign of COVID‐19 infection in adults and children, using an initial adult dose of 500 mg followed by 250 mg per day for 4 days, a total cumulative dose of 1.5 g, and for children 5 to 18 years of age, 10 mg/kg on the first day ...What to do to make Covid go away faster? ›
- Keep a daily routine, such as taking a shower and getting dressed.
- Take breaks from COVID-19 news and social media.
- Eat healthy meals and drink plenty of fluids.
- Stay physically active.
- Get plenty of sleep.
- Avoid use of drugs, tobacco and alcohol.
Take this medication by mouth as directed by your doctor, usually once daily with or without food. You may take this medication with food if stomach upset occurs. The dosage is based on your medical condition and response to treatment. For the best effect, take this antibiotic at evenly spaced times.Is azithromycin a steroid? ›
Is azithromycin a steroid? No. Azithromycin is a macrolide antibiotic that works by inhibiting the growth of bacteria.Is azithromycin a high risk medication? ›
Azithromycin was associated with a significantly increased hazard of cardiovascular death (hazard ratio [HR], 1.82; 95% CI, 1.23-2.67) but not sudden cardiac death (HR, 1.59; 95% CI, 0.90-2.81) within 5 days of exposure.Why is azithromycin given for 3 days? ›
Azithromycin is sometimes prescribed long-term to prevent chest infections if you keep getting them. In this case you will usually need to take it 3 times a week, often on a Monday, Wednesday and Friday.
Tiredness or fatigue is not a common side effect of antibiotic use, but it can happen. The antibiotics most likely to cause tiredness as a side effect are amoxicillin, azithromycin, and ciprofloxacin.Can azithromycin cause eye problems? ›
Common side effects of azithromycin ophthalmic may include:
eye irritation; dry or itchy eyes; blurred vision; stuffy nose; or.
Antibiotic resistance is not a distant threat, but is in fact one of the most dangerous global crises facing the modern world today. Taking antibiotics when you don't need them puts you and your family at risk of developing infections which in turn cannot be easily treated with antibiotics.What kind of bacteria does azithromycin treat? ›
Azithromycin is a broad-spectrum macrolide antibiotic with bacteriostatic activity against many Gram-positive and Gram-negative bacteria including Bordetella pertussis and Legionella species. It also has activity against Mycoplasma pneumoniae, Treponema pallidum, Chlamydia species and Mycobacterium avium complex.Why is azithromycin taken on an empty stomach? ›
May be taken with or without food; however, azithromycin may be better tolerated if taken with food. Do not take aluminum or magnesium-containing antacids two hours before or two hours after you take azithromycin because antacids can make azithromycin less effective.How long do side effects last after azithromycin? ›
How long do azithromycin side effects last? Most azithromycin side effects go away after the drug has been stopped, but it may take a while. It takes the body 68 hours—three days—to clear out half a dose of azithromycin from the body, so some side effects may linger for a week or more.How long does it take for azithromycin to work for throat infection? ›
A Z-Pack typically takes at least five days to fully work, but it can start to relieve your sore throat and other symptoms on the first day you take it. If your doctor prescribes a generic version of azithromycin, your treatment may only last three days.How many azithromycin 500mg do I take a day? ›
Dosage and strength
The usual dose is 500mg a day for 3 to 10 days depending on the infection being treated. For some infections, you'll be given a one-off higher dose of 1g or 2g. The dose may be lower for children or if you have liver or kidney problems.
1. How long does it take azithromycin to work? Azithromycin starts working soon after you take your first dose. Oral azithromycin usually needs about 2 to 3 hours to reach its full concentration in your body, but the effects might not be noticeable right away.What is the best time to take azithromycin tablets? ›
You or your child must take this medicine within 12 hours after it has been mixed with water. It is best to take the Zmax® extended-release oral suspension on an empty stomach or at least 1 hour before or 2 hours after a meal.
Official answer. Azithromycin will be in your system for around 15.5 days, after the last dose. Azithromycin has an elimination half-life of 68 hours. The prolonged terminal half-life is thought to be due to extensive uptake and subsequent release of drug from tissues.What should not be taken with azithromycin? ›
If you are taking aluminum or magnesium-containing antacids, do not take them at the same time that you take Zithromax®. These medicines may keep azithromycin from working properly. However, you can take antacids with Zmax®.Does azithromycin affect the heart? ›
The U.S. Food and Drug Administration (FDA) is warning the public that azithromycin (Zithromax or Zmax) can cause abnormal changes in the electrical activity of the heart that may lead to a potentially fatal irregular heart rhythm.Does azithromycin make you tired? ›
Tiredness or fatigue is not a common side effect of antibiotic use, but it can happen. The antibiotics most likely to cause tiredness as a side effect are amoxicillin, azithromycin, and ciprofloxacin.Does azithromycin make you feel better? ›
Take all the azithromycin doses
Take this medicine for as many days as instructed. It's common to feel a lot better after a few days of antibiotics, but the infection isn't completely gone. Even if the medicine makes you feel bad, take it faithfully until the very end to make sure the bacteria are gone for good.
Furthermore, some patients with viral respiratory illness might develop a secondary bacterial infection or present with a bacterial co-infection, which azithromycin could effectively treat. Azithromycin use in primary care has increased during the COVID-19 pandemic,7 which could contribute to antimicrobial resistance.What happens if you take azithromycin on an empty stomach? ›
May be taken with or without food; however, azithromycin may be better tolerated if taken with food. Do not take aluminum or magnesium-containing antacids two hours before or two hours after you take azithromycin because antacids can make azithromycin less effective.Should azithromycin be taken for 3 days or 5 days? ›
The overall clinical cure rate was 95.7% and 96.1%, and bacteriological eradication rate 90.1% and 94.2% in the 3-day and 5-day groups, respectively. Side effects, mostly mild gastrointestinal disturbances, were observed in 5.3% of children from the 3-day, and 6.7% from the 5-day group.Why is azithromycin taken for 3 days? ›
It is concluded that a 3-day regimen of azithromycin prescribed as tablets is as clinically and microbiologically effective as a 10-day regimen of co-amoxiclav in the treatment of acute lower respiratory tract infections.