This injection is used to treat bacterial infections in many different parts of the body.
This medicine is also used for the prevention of Mycobacterium avium complex diseases in patients who have HIV (human immunodeficiency virus).
It works by killing the bacteria or preventing their growth. However, it will not work for colds, flu, or other virus infections. Azitrocin injection may be used for other problems as determined by your doctor.
Azitrocin is available only with a prescription from your doctor.
Once a drug has been approved for marketing for a particular use, experience may show that it is useful for other medical problems as well.
Although these uses are not listed on the product labeling, azitrocin is used in certain patients with the following medical condition:
- Trachoma (treatment).
Indications of azitrocin
Azitrocin extended-release granules are indicated for the treatment of patients with mild to moderate infections caused by susceptible strains of designated microorganisms under the specific conditions listed below.
Uncomplicated acute bacterial sinusitis, caused by the following bacteria:
- Moraxella catarrhalis.
- Streptococcus pneumoniae.
- Haemophilus influenzae.
Tonsillitis or pharyngitis, caused by Streptococcus pyogenes bacteria, as an alternative treatment in patients unable to use first-line therapy. Penicillin is generally the usual drug in the treatment of this infection.
There are susceptibility tests that must be carried out in patients treated with this drug since there are some strains that are resistant to it.
Mild to moderate community-acquired pneumonia in pediatric patients 6 months of age and older due to:
- Mycoplasma pneumoniae.
- Haemophilus influenzae
- Streptococcus pneumoniae.
- Chlamydophila pneumoniae.
In patients suitable for oral treatment, pediatric use in this indication is based on extrapolation of efficacy from the adult.
To reduce the development of drug resistant bacteria and maintain the effectiveness of azitrocin and other antibacterial drugs, azitrocin should only be used to treat infections that are known or suspected to be caused by susceptible bacteria.
When culture and susceptibility information are available, they should be considered when selecting or modifying antibacterial therapy.
Prior to treatment to determine the causative organism, appropriate susceptibility and culture tests should be performed.
Azitrocin therapy can be started before the results of these tests are known; once results are available, antimicrobial therapy should be adjusted accordingly.
How should azitrocin be used?
Use azitrocin as directed by your doctor and check the label on the medication package for use.
- An additional booklet is available for the azitrocin patient. Talk to your pharmacist if you have questions about this information.
- Azitrocin is for use in the eye only. Do not swallow it.
- Wash your hands immediately before using Azitrocin.
- To use azitrocin, turn the bottle upside down and shake once before each use. Remove the cap while the bottle is still upside down. Tilt your head back. Pull the lower eyelid away from the eye to form a pocket with your index finger.
- If a drop does not come out of the bottle when you use your dose, repeat these steps.
- To prevent germs from contaminating your medicine, do not touch the applicator tip to any surface, including the eye. Keep the container closed.
- Do not wear contact lenses while using azitrocin. Take care of your contact lenses according to the manufacturer’s directions. Check with your doctor before using them.
- To completely clear up your infection, use azitrocin throughout treatment. Keep using it even if you feel better in a few days.
Description of azitrocin
Each capsule contains Azitrocin dihydrate 262.05 mg equivalent to Azitrocin base 250 mg. As excipients it contains cornstarch, magnesium stearate, anhydrous lactose, and sodium lauryl sulfate. The capsule shell contains gelatin, titanium dioxide (E171), and up to 1,000 ppm sulfur dioxide.
Each tablet contains Azitrocin dihydrate 262.05 mg equivalent to Azitrocin base 250 mg. As excipients it contains anhydrous dibasic calcium phosphate, pregelatinized starch, magnesium stearate, croscarmellose sodium and sodium lauryl sulfate.
The film coating contains hydroxypropyl cellulose, triacetin, and titanium dioxide (E171).
Each 5 ml of powder for oral suspension contains Azitrocin dihydrate 209.64 mg equivalent to Azitrocin base 200 mg.
It also contains sucrose (1.94 g / 100 mg dose), anhydrous tribasic sodium phosphate, hydroxypropylcellulose, xanthan gum, artificial cherry, vanilla cream, and banana flavors as excipients.
Each sachet contains Azitrocin dihydrate 100.16 mg equivalent to Azitrocin base 100 mg.
It also contains sucrose (1.85 g / azithromycin 100 mg dose), anhydrous tribasic sodium phosphate, hydroxypropyl cellulose, xanthan gum, artificial cherry, vanilla cream, and banana flavors as excipients.
It also contains a dry powder that produces, when added to water, a white to off-white, cherry / banana suspension with a slight vanilla odor.
Each vial contains azitrocin dihydrate 524.1 mg equivalent to Azitrocin base 500 mg. It also contains anhydrous citric acid and sodium hydroxide as excipients. It is supplied in lyophilized form under vacuum in a 10 ml vial for intravenous administration.
After reconstitution, the azitrocin powder produces a solution containing the equivalent of 100 mg / ml of azitrocin.
Azitrocin is 9-deoxy-9a-aza-9a-methyl-9a-homoerythromycin A. The molecular weight is 749.
It is recommended to take azitrocin extended-release granules at least 1 hour before or 2 hours after eating.
The recommended dose for adults is a single dose of 2.0 g of azitrocin extended-release granules. In Phase 3 studies, no patient vomited within 5 minutes of dosing the azitrocin extended-release granules.
In case a patient vomits within 5 minutes after administration, additional antibiotic treatment may be considered as there will be minimal absorption of azitrocin. In patients with delayed gastric emptying, alternative therapy should be considered.
For pediatric patients 6 months and older, azitrocin should be taken as a single dose of 60 mg / kg (equivalent to 27 mg / lb) of body weight. The azitrocin dose in mL is equivalent to the child’s weight in lb (1 mL / lb dose, see Table 7), for a body weight of less than 75 lb (34 kg).
Pediatric patients weighing 75 lbs. (34 kg) or more should receive the adult dose (2 g).
How safe and effective the drug is in pediatric patients younger than 6 months has not yet been established.
Additional treatment after vomiting with azitrocin : In case a patient vomits within 5 minutes after administration, the doctor should consider additional antibiotic treatment as there will be minimal absorption of azitrocin.
In patients with delayed gastric emptying, alternative therapy should be considered.
Elderly: no dose adjustment is necessary in elderly patients requiring azitrocin therapy. Elderly patients may be more susceptible to the development of torsades de pointes arrhythmias.
In patients with renal insufficiency: it is not recommended to adjust the dose from mild to moderate (glomerular filtration rate of 10-80 ml / min). Caution should be exercised when administering azitrocin prolonged-release granules to patients with severe renal impairment (GFR <10 ml / min).
In patients with hepatic impairment: The pharmacokinetics of azitrocin in patients with hepatic impairment have not been established for azitrocin prolonged-release granules.
Based on studies with immediate-release formulations, adjusting the dose from mild to moderate is not recommended. Azitrocin should be used with caution in patients with severe hepatic impairment.
In patients receiving azitrocin and antacids, the drugs should not be taken simultaneously.
Azitrocin does not interact significantly with the hepatic cytochrome P450 system.
The frequency of monitoring prothrombin time should be taken into consideration when using azitrocin in people receiving oral anticoagulants (coumarin type), even if a causal relationship has not yet been established.
Great care should be taken before giving a patient a combination of some of these drugs together with azitrocin. Cyclosporine levels should be regulated and the doses of cyclosporine adjusted, if the administration of these drugs is necessary for the patient.
Concomitant administration of a single 1,200 mg dose of azitrocin had no statistically significant effect on the pharmacokinetics of indinavir administered as 800 mg three times daily for 5 days.
Azitrocin side effects
Clinical trial experience
Because clinical trials are conducted under widely varying conditions, the rates of adverse reactions seen in clinical trials of one drug cannot be directly compared to rates in clinical trials of another drug and may not reflect the rates seen in the drug. practice.
All patients received a single 2 g oral dose of azitrocin. The population studied had acute bacterial sinusitis and community-acquired pneumonia.
In controlled clinical trials with azitrocin, the majority of reported treatment-related adverse reactions were gastrointestinal in nature and of mild to moderate intensity.
Overall, the most common treatment-related adverse reactions in adult patients receiving a single 2-g dose of azitrocin were diarrhea / loose stools (12%), nausea (4%), abdominal pain (3%), abdominal pain. head (1%). and vomiting (1%).
The incidence of treatment-related gastrointestinal adverse reactions was 17% for azitrocin and 10% for the combined comparators.
Treatment-related adverse reactions after azitrocin treatment that occurred with a frequency of <1% included the following:
- Cardiovascular: palpitations, chest pain.
- Gastrointestinal: constipation , dyspepsia, flatulence, gastritis, oral moniliasis.
- Genitourinary: vaginitis.
- Nervous system: dizziness, vertigo.
- General: asthenia.
- Allergic: rash, itching, hives .
- Special senses: perversion of taste.
The data described below reflect exposure to azitrocin in 907 pediatric patients. The population was between 3 months and 12 years old. All patients received a single oral dose of 60 mg / kg of azitrocin.
As in adults, the most common treatment-related adverse reactions in pediatric patients were gastrointestinal in nature. All pediatric subjects received a single 60 mg / kg dose (equivalent to 27 mg / lb) of azitrocin.
In a trial of 450 pediatric subjects (ages 3 months to 48 months), vomiting (11%), diarrhea (10%) loose stools (9%), and abdominal pain (2%) were treatment-related gastrointestinal reported with more often.
Many treatment-related gastrointestinal adverse reactions with an incidence greater than 1% began on the day of administration in these subjects [43% (68/160)] and the majority [53% (84/160)] resolved within 48 hours after the start.
Treatment-related adverse events that were not gastrointestinal and that occurred with a frequency of ≥ 1% were: rash (5%), anorexia (2%), fever (2%), and dermatitis (2%).
In a second trial of 337 pediatric subjects, aged 2 years to 12 years, the most frequently reported treatment-related adverse reactions also included vomiting (14%), diarrhea (7%), loose stools (2%), nausea ( 4%) and abdominal pain (4%).
A third trial investigated the tolerability of two different concentrations of azitrocin oral suspension in 120 pediatric subjects (3 months to 48 months), all of whom were treated with azitrocin.
The study tested the hypothesis that a more dilute and less viscous formulation (the recommended concentration of 27 mg / ml azitrocin) is less likely to induce vomiting in young children than a more concentrated suspension used in other pediatric studies.
The vomiting rate in subjects taking the diluted concentration of azitrocin was 3% (2/61). The rate was numerically lower but not statistically different from vomiting for the more concentrated suspension.
In both treatment groups, the only treatment-related adverse events with a frequency of ≥ 1% were vomiting (6%, 7/120) and diarrhea (2%, 2/120).
Treatment-related adverse reactions with a frequency <1% after azitrocin treatment in the 907 pediatric patients in phase 3 studies were:
- Body in general: chills, fever, flu syndrome, headache.
- Lymphatic and hematological: leukopenia.
- Digestive: gas, constipation, abnormal stools, dyspepsia, gastritis, hepatitis. and gastrointestinal disorder.
- Nervous system: agitation, emotional responsibility, hostility, hyperkinesia, insomnia, irritability, paraesthesia, drowsiness.
- Respiratory: rhinitis, cough, asthma, cough, dyspnea, bronchitis, pharyngitis.
- Skin and appendages: dermatitis, fungal dermatitis, maculopapular rash, pruritus, urticaria.
- Special senses: taste changes, otitis media.
- Urogenital: disuria.
Post-marketing experience with other azitrocin products
Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship with drug exposure.
Adverse events reported with azitrocin immediate-release formulations during the post-marketing period for which a causal relationship cannot be established include:
- Allergic: arthralgia, edema, urticaria and angioedema.
- Cardiovascular: arrhythmias and palpitations (including hypotension and ventricular tachycardia).
- There have been reports of QT prolongation and torsades de pointes.
- Gastrointestinal: anorexia, constipation, dyspepsia, flatulence, vomiting / diarrhea, pseudomembranous colitis, pancreatitis, oral candidiasis, pyloric stenosis, and rare reports of tongue discoloration.
- General: asthenia, paraesthesia, fatigue, malaise and anaphylaxis.
- Genitourinary: vaginitis, interstitial nephritis, renal insufficiency.
- Hematopoyético: neutropenia leve, trombocitopenia.
- Liver / Biliary: Adverse reactions related to liver dysfunction have been reported in post-marketing experience with azitrocin.
- Nervous system: seizures, headaches, hyperactivity, drowsiness, hyperactivity, nervousness, syncope, agitation, vertigo and dizziness.
- Psychiatric: anxiety and aggressive reactions.
- Skin / Appendages: Itching, rash, photosensitivity, severe skin reactions including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
- Special Senses: Hearing disorders including hearing loss, deafness and / or tinnitus and reports of perversion / loss of taste / odor.
In subjects with normal baseline values, the following clinically significant laboratory abnormalities (regardless of drug relationship) were reported in clinical trials with azitrocin in adults and pediatric patients:
Laboratory abnormalities with an incidence greater than or equal to 1%: decreased lymphocytes and increased eosinophils; reduced bicarbonate Laboratory abnormalities with an incidence of less than 1%: leukopenia, neutropenia, elevated bilirubin, AST, ALT, BUN, creatinine, potassium disturbances.
Laboratory abnormalities with an incidence greater than or equal to 1%: elevated eosinophils, BUN, and potassium; decreased lymphocytes; and changes in neutrophils; with an incidence of less than 1%: elevation of SGOT, SGPT and creatinine; decreased potassium; and alterations in sodium and glucose.
Contraindications of azitrocin
Azitrocin tablets are contraindicated in patients with known hypersensitivity to the administration of azitrocin, erythromycin, any macrolide or ketolidium.
Azitrocin tablets are contraindicated in patients with a history of cholestatic jaundice / liver dysfunction associated with previous use of azitrocin.