Zertalin 250mg 6 Tab, Azithromycin
ZERTALIN containing azithromycin, an azalide antibiotic, a new group of antibiotics originated from eritromcina. Laazitromicina is indicated in infections caused by susceptible organisms, in lower respiratory tract infections including bronchitis and pneumonia, and infections of skin and soft tissue, otitis media and upper respiratory tract infections, including sinusitis, and pharyngitis . (Penicillin is usually the drug of choice in the treatment of pharyngitis Streptococcuspyogenes and prophylaxis of rheumatic fever.
Azithromycin is generally effective in the eradication of streptococci from the oropharynx, but currently no data are available to establish the efficacy of azithromycin in subsequent prevention of rheumatic fever).
In sexually transmitted infections, azithromycin is indicated in men as in women in the treatment of uncomplicated genital infections due to Chlamydia trachomatis. It is also indicated for the treatment of chancroid because Haemophilusducreyi.
It is also indicated in the treatment of uncomplicated genital infections due to Neisseria gonorrhoeae seamultirresistente not.
You must exclude concomitant infection with Treponema pallidum.
Azithromycin has shown in vitro activity against a broad spectrum of bacteria, including:
Aerobic gram-positive bacteria: Staphylococcus aureus, Streptococcus pyogenes (group A beta-hemolytic streptococcus), Streptococcus pneumoniae, alpha-hemolytic streptococci (viridans group), other streptococci and Corynebacterium diphtheriae.
Azithromycin has shown cross-resistance to erythromycin-resistant gram-positive strains that, including: Streptococcusfaecalis (enterococci) and most of the methicillin-resistant strains of staphylococci.
Aerobic gram-negative bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, deAcinetobacter species, Yersinia species, Legionella pneumophila, Bordetella pertussis, Bordetella parapertussis, Shigella species, Pasteurella species, Vibrio cholerae and parahaemolyticus, Plesiomonas shigelloides. The activity against Escherichia coli, Salmonella enteritidis, Salmonella typhi, Enterobacter species, Aeromonas hydrophila and Klebsiella species is variable and should be tested for susceptibility.
Usually strains resistant Proteus species, Serratia species, and Morganella species Pseudomonas aeruginosa.
Anaerobic bacteria: Bacteroides fragilis and Bacteroides species, Clostridium perfringens, and Peptococcus dePeptoestreptococcus species, Fusobacterium necrophorum and Propionibacterium acnes.
Pathogens of sexually transmitted diseases: ZERTALIN is active against Chlamydia trachomatis and also shows good activity against Treponema pallidum, Neisseria gonorrhoeae and Haemophilus ducreyi.
Other agencies: Borrelia burgdorferi (causative agent of Lyme disease), Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycoplasma hominis, Ureaplasma urealyticum, Campylobacter and Listeria monocytogenes.
Opportunistic pathogens associated with HIV infections: Mycobacterium avium-intracellulare complex, Pneumocystis carinii yToxoplasma gondii.
Human Pharmacokinetics: Azithromycin is the first member of a class of antibiotics designated chemically as azalides. Chemically caused by insertion of a nitrogen atom in the lactone ring of erythromycin A.
The mechanism of action of azithromycin is by inhibiting protein synthesis by bacteria, due to its 50S ribosomal binding lasubunidad avoiding peptide translocation.
After oral administration in humans, azithromycin is widely distributed throughout the body. Its bioavailability is about 37%. Administering azithromycin capsules after a large meal subiodisponibilidad decreases by at least 50%. The time required to reach peak plasma levels is two to three hours. Terminal half-life of plasma elimination half-life closely reflects tissue depletion two to four days.
In elderly volunteers (aged 65 years), after a five-day regimen were observed values â€‹â€‹of area under the curve (AUC) slightly higher than those observed in younger volunteers (under 40 years) but these do not were considered clinically significant, and therefore is not recommended dosage adjustment.
In patients with moderate renal impairment (creatinine clearance less than 40 ml / min), no evidence of significant changes in the pharmacokinetics of azithromycin in serum, compared with patients with normal renal function. There are no pharmacokinetic study results concerning the use of azithromycin in patients with more severe renal insufficiency.
In patients with mild hepatic impairment (Class A) to moderate (class B) there is no evidence of significant changes in the pharmacokinetics of azithromycin in serum, compared with patients with normal liver function. It seems that in these patients increases the urinary recovery of azithromycin, probably to compensate for the decrease in hepatic clearance.
Pharmacokinetic studies have shown levels much higher azithromycin in tissues than in plasma (up to 50 times the maximum concentration observed in the plasma), indicating that the drug binds strongly to tissue. After a dose of 500mg, concentrations in target tissues such as lung, tonsil and prostate exceed the MIC90 for likely pathogens in these tissues.
After intravenous administration of antibiotics, approximately 12% is excreted in the urine within three days as unchanged drug, mostly in the first 24 hours. Found very high concentrations of unchanged drug in human bile, along with ten metabolites formed by N and O demethylation, hydroxylation desoxamina and rings breaking aglycone and cladinose conjugate.
Comparing the levels in tissues by microbiological methods and high-pressure liquid chromatography, suggesting that metabolites play no role in microbiological activity azithromycin.
Studies in animals have been observed at high concentrations of azithromycin phagocytes. In experimental models, it has been observed that there is greater release of azithromycin during phagocytosis active when compared with unstimulated phagocytes. In animal models, this results in the release of high concentrations of azithromycin at the site of infection.
CONTRAINDICATIONS: The use of ZERTALIN is contraindicated in patients with a history of allergic reactions to azitromicinao any of the macrolide antibiotics.
PRECAUTIONS: As with erythromycin and other macrolides, have been rarely reported cases of severe allergic reactions, including angioedema and anaphylaxis (rarely fatal).
Some of these reactions with azithromycin have resulted in recurrent symptoms, requiring longer periods of observation and treatment. No information is available concerning the use of azithromycin in patients with creatinine clearance less than 40 ml / min, from the above, caution should be exercised before prescribing azithromycin in these patients.
Because the liver is the major route of elimination for azithromycin, should be used with caution in patients with significant liver disease. In patients who are administered ergot derivatives, has precipitated ergotismo administered simultaneously with the certain macrolide antibiotics. No information is available concerning the possibility of interactions between azithromycin and ergot. However, because of the theoretical possibility of ergotism, should not be administered simultaneously azithromycin and ergot derivatives. As with any antibiotic, should be monitored for signs of superinfection with non-susceptible organisms including fungi.
Effects on ability to drive motor vehicles or operate machinery: No evidence that azithromycin may affect ability to drive motor vehicles and operate machinery.
PRECAUTIONS OR RESTRICTIONS OF USE DURING PREGNANCY AND LACTATION: Animal reproduction studies have shown that azithromycin crosses the placenta, but revealed no evidence of harm to the fetus. There are no data on secretion in breast milk. No security has been established for use during pregnancy and lactation.
Azithromycin should only be administered to pregnant or lactating when no suitable alternatives available.
ZERTALIN is usually well tolerated, with a low frequency of side effects, which include:
Gastrointestinal: Anorexia, nausea, vomiting, diarrhea (rarely causing dehydration) and loose stools, dyspepsia, abdominal discomfort (pain, cramps), constipation and flatulence, pseudomembranous colitis and rarely discoloration of the tongue.
Senses: It is reported hearing impairment with macrolide antibiotics.
There have been reports of hearing impairment, including hearing loss, deafness and / or tinnitus in many patients recibenazitromicina. Many of these have been associated with prolonged use of large doses in research.
In these cases, when the tracking information was available, the majority of events were reversible. There have been rare reports of altered sense of taste.
Genitourinary: interstitial nephritis have been reported and acute renal failure.
Liver-bile duct: Abnormalities in liver function including hepatitis and cholestatic jaundice, as well as rare cases of necrosis and liver failure, which have rarely resulted in death. However, no causal relationship has been established.
Psychiatric: Aggressive reactions, nervousness, agitation and anxiety.
Central and Peripheral Nervous System: Dizziness, vertigo, seizures (seen with other macrolides), headache, somnolence, paresthesia, and hyperactivity.
Leukocytes: In clinical studies have been occasionally observed transient episodes of mild neutropenia, although no causal relationship has been established with azithromycin.
Skin and appendages: allergic reactions have been reported which include itching, rash, photosensitivity, edema, urticaria and angioedema. Have occurred rarely serious skin reactions including erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis.
Cardiovascular: palpitations and arrhythmias have been reported, including ventricular tachycardia (as with other macrolides), although a causal relationship has not been established azithromycin.
General: asthenia has been reported, although no causal relationship has been established; also been reported moniliasis and anaphylaxis (rarely fatal), although no causal relationship has been demonstrated.
DRUG INTERACTIONS AND OTHER GENDER
Antacids: In a pharmacokinetic study that investigated the effects of simultaneous administration of antacids with azithromycin, there was no effect on the bioavailability as such, although the peak serum concentration was reduced by up to 30%. Patients receiving both azithromycin and antacids should not take these drugs simultaneously.
Carbamazepine: In a pharmacokinetic interaction study in healthy volunteers, there was no significant effect on plasma levels of carbamazepine or its active metabolite in patients receiving concomitant azithromycin.
Cimetidine: A pharmacokinetic study investigated the effects of a single dose of cimetidine, administered 2 hours prior to laazitromicina, showed no alteration in the pharmacokinetics of the latter.
Cyclosporine: In the absence of conclusive data or pharmacokinetic clinical studies relating to the potential interaction between cyclosporine azitromicinay, caution should be exercised before the administration of these drugs. If coadministration is necessary, should be monitored cyclosporine levels and adjust the dose according to the needs.
Digoxin has been reported that some macrolide antibiotics alter microbial metabolism of digoxin in the gut of certain patients. Should be borne in mind the possibility of reaching high levels of digoxin in patients receiving azithromycin (an antibiotic related azalide macrolide) and digoxin.
Ergot: Because of the theoretical possibility of ergotism, no concomitant use of azithromycin with ergot derivatives.
Methylprednisolone: â€‹â€‹In a pharmacokinetic study conducted in healthy volunteers, azithromycin had no significant effect on the pharmacokinetics of methylprednisolone.
Theophylline No evidence pharmacokinetic interaction when administered jointly azithromycin and theophylline in healthy volunteers.
Terfenadine: Pharmacokinetic studies have reported no evidence of interaction between azithromycin and terfenadine. There have been rare cases reported where the possibility of such interaction may not be fully excluded, but no specific evidence that this interaction occurred.
Oral anticoagulants of the coumarin type: In a pharmacokinetic interaction study, azithromycin did not alter the anticoagulant effect of a single dose of 15 mg of warfarin when administered to healthy volunteers. In post-marketing studies have been reports of potentiated anticoagulation as a result of the concomitant administration of azithromycin and oral anticoagulantescumarínicos. Although not a causal relationship, should be considered the frequency of prothrombin time monitoring.
Zidovudine: The administration of single doses of 1000 mg and repeated doses of 1,200 or 600 mg of azithromycin did not affect the plasma pharmacokinetics and urinary excretion of zidovudine or its glucuronide metabolite. However, deazitromicina administration increased the concentration of phosphorylated zidovudine, clinically active metabolite in the peripheral blood mononuclear cells.
It is unclear clinical significance of this finding, but may be beneficial for patients.
Didanosine: Concurrent administration of daily doses of 1,200 mg of azithromycin with didanosine in six patients did not appear to affect the pharmacokinetics of didanosine, compared with placebo.
Rifabutin Simultaneous administration of azithromycin and rifabutin not modify the serum levels of any of the drugs. While neutropenia was observed using rifabutin not established a causal relationship conazitromicina combination.
LABORATORY TESTING CHANGES: To date there are no known interferences in laboratory tests porazitromicina induced.
PRECAUTIONS IN RELATION TO EFFECTS Carcinogenesis, Mutagenesis, Impairment of Fertility: There have been long-term studies in animals to evaluate carcinogenic potential.
Azithromycin has shown no mutagenic potential in standard laboratory tests, as proof of lymphoma in mice pruebaclastogénica test in human lymphocytes and clastogenic in mouse bone marrow.
DOSAGE AND ADMINISTRATION: Oral.
ZERTALIN should be administered as a single daily dose. Dosing period regarding the infection mentioned below. ZERTALIN can be taken with food.
Adults: For the treatment of sexually transmitted diseases caused by Chlamydia trachomatis, Haemophilus ducreyi or susceptible strains of Neisseria gonorrhoeae, ZERTALIN dose is 1,000 mg as a single dose. For all other indications, ZERTALIN total dose is 1,500 mg administered at 500 mg daily for three days.
Elderly: the same dose used in adults.
Patients with renal impairment: In patients with mild renal impairment (creatinine clearance less than 40 ml / min) can be used the same dose in patients with normal renal function. No information is available regarding the use of ZERTALIN in patients with more severe renal impairment.
Patients with hepatic impairment may be given the same dosage to patients with mild to moderate hepatic impairment than patients with normal hepatic function.
Children: Except for the treatment of strep throat, the total dose of azithromycin in children is 30 mg / kg in three days, administered as a single daily dose of 10 mg / kg / day for three days.
ZERTALIN tablets should only be given to children weighing more than 45 kg.
For strep throat, ZERTALIN been shown to be effective in a single dose of 10 mg / kg or 20 mg / kg, for three days, however, it is advisable not to administer doses above 500 mg daily. In clinical studies, in which we compared the two dose regimens, similar clinical efficacy was observed, but it was evident bacterial eradication greater the dose of 20 mg / kg. However, penicillin is the drug of choice for the treatment of Streptococcus pyogenes pharyngitis, including prophylaxis of rheumatic fever.
Overdosage: REPRESENTATIONS AND MANAGEMENT (antidotes): Adverse events reported with administration of higher than recommended doses were similar to those observed with normal doses. If desobredosificación, according to needs, and symptomatic treatment is recommended general supportive measures.
Drug Name: Zertalin
Comparable drug patent: Azitrocin
Active substance: Azithromycin
Concentration: 500 mg
Extended-release tablets: No
Laboratory: Collins, SA de CV
Box with 3 Pills
Made in Mexico