ExusAzithromycin (Azithromycin, USP) Capsules 250mg are hard gelatin capsule shells filled with Azithromycin (as azithromycin dihydrate), White or almost white powder 250mg, an antibiotic used to treat a wide variety of bacterial infections derived from erythromycin; however, it differs chemically from erythromycln in that a methyl-substituted nitrogen atom is incorporated into the lactone ring. Its molecular formula is C38H72N2012, and its molecular weight Is 749.00.
ExusAzithromycin is indicated for the treatment with mild to moderate infections caused by susceptible isolates of the designated microorganisms in the specific conditions listed below.
Acute bacterial sinusitis in adults due to Haemophilus influenzae. Moraxella catarrhalis or Streptococcus pneumoniae.
Community-acquired pneumonia in adults and pediatric patients six months of age or older due to Chlamydophila pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniaeor Streptococcus pneumoniae, in patients appropriate for oral therapy.
Pediatric use in this indication is based on extrapolation of adult efficacy.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of ExusAzithromycin and other antibacterial drugs, ExusAzithromycin should be used only to treat infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
Appropriate culture and susceptibility tests should be performed before treatment to determine the causative organism and its susceptibility to ExusAzithromycin. Therapy with ExusAzithromycin may be initiated before results of these tests are known; once the results become available, antimicrobial therapy should be adjusted accordingly.
Dosage and Administration
Capsules for oral administration
Take your capsules 1 hour before a meal or 2 hours after a meal with a drink of water.
Should you require to take an antacid for indigestion, take your capsule one hour before or two hours after the antacid. The usual dose for ExusAzithromycin is 500mg (2 capsules) taken together, once a day, for 3 days.
For Chlamydia or Gonorrhoea the dose is 1g (4 capsules) taken all together on one day only.
ExusAzithromycin Capsules should not be taken by children weighing less than 7 stones (45kg). For children weighing more than 7 stones the doses mentioned above are usually prescribed.
Stomach upset, loose stools, loss of appetite, nausea, vomiting, stomach cramps or vaginal irritation.
Antacids (Aluminium hydrocide; Magnesium hydroxide): Reduced absorption of azithromycin.
The drug is contraindicated in patients with known hypersensitivity to azithromycin, erythromycin or any macrolide or ketolide antibiotic.
Serious allergic reactions, including angioedema, anaphylaxis, and dermatologic reactions including Stevens Johnson Syndrome and toxic epidermal necrolysis have been reported rarely in patients on azithromycin therapy. Although rare, fatalities have been reported. Despite initially successful symptomatic treatment of the allergic symptoms, when symptomatic therapy was discontinued, the allergic symptoms recurred soon thereafter in some patients without further azithromycin exposure.
Phospholipidosis (intracellular phospholipid accumulation) has been observed in some tissues of mice, rats, and dogs given multiple doses of azithromycin. It has been demonstrated in numerous organ systems (e.g. eye, dorsal root ganglia, liver, gallbladder, kidney, spleen, and pancreas) in dogs treated with azithromycin at doses which, expressed on the basis of mg/m2, are approximately equal to the recommended adult human dose, and in rats treated at doses approximately one-sixth of the recommended adult human dose. This effect has been shown to be reversible after cessation of azithromycin treatment. Phospholipidiosis has been observed to a similar extent in the tissues of neonatal rats and dogs given daily doses of azithromycin ranging from 10 days to 30 days. Based on the pharmacokinetic data, phospholipidosis has been seen in the rat (30 mg/kg dose) at observed Cmax value of 1.3 µg/mL (six times greater than the observed Cmax of 0.216 µg/mL at the pediatric dose of 10 mg/kg). Similarly, it has been shown in the dog (10 mg/kg dose) at observed Cmax value of 1.5 µg/mL (seven times greater than the observed same Cmax and drug dose in the studied pediatric population). On a mg/m2 basis, 30mg/kg dose in the neonatal rat (135 mg/m2) and 10mg/kg dose in the neonatal dog (79 mg/m2) are approximately 0.5 and 0.3 times, respectively, the recommended dose in the pediatric patients with an average body weight of 25 kg. Phospholipidosis, similar to that seen in the adult animals, is reversible after cessation of azithromycin treatment. The significance of these findings for animals and for humans is unknown.
Following oral administration of a single 500 mg dose (two 250 mg capsules) to 36 fasted healthy male volunteers, the mean (SD) pharmacokinetic parameters were AUCO-72 = 4.3 (1.2) µg.h/mL; Cmax = 0.5(0.2) µg/mL; Tmax = 2.2 (0.9) hours.
With a regimen of 500 mg (two 250 mg capsules) on day 1, followed by 250 mg daily (one 250 mg capsule) on days 2 through 5, the pharmacokinetic parameters of azithromycin in plasma in healthy young adults (18-40 years of age) are portrayed in the chart below. Cmin and Cmax remained essentially unchanged from day 2 through day 5 of therapy.
In a two-way crossover study, 12 adult healthy volunteers (6 males. 6 females) received 1,500mg of azithromycin administered in single daily doses over either 5 days (two 250 mg capsules on day 1, followed by one 250 mg tablet on days 2-5) or 3 days (500 mg per day for days 1-3). Due to limited serum samples on day 2 (3-day regimen) and days 2-4 (5-day regimen), the serum concentration-time profile of each subject was fit to a 3-compartment model and the AUCO-∞ for the fitted concentration profile was comparable between the 5-day and 3-day regimens.
Median azithromycin exposure (AUCO-288) in mononuclear (MN) and polymorphonuclear (PMN) leukocytes following either the 5-day or 3-day regimen was more than a 1000-fold and 800-fold greater than in serum, respectively. Administration of the same total dose with either the 5-day or 3- day regimen may be expected to provide comparable concentrations of azithromycin within MN and PUN leukocytes.
Two azithromycin 250mg capsules are bioequivalent to a single 500 mg tablet.
The absolute bioavailability of azithromycin 250mg capsules is 38%.
In a two-way crossover study in which 12 healthy subjects received a single 500 mg dose of azithromycin (two 250 mg capsules) with or without a high fat meal, food was shown to increase Cmax by 23% but had no effect on AUC.
When azithromycin suspension was administered with food to 28 adult healthy male subjects, Cmax increased by 56% and AUC was unchanged.
The AUC of azithromycin was unaffected by co-administration of an antacid containing aluminum and magnesium hydroxide with azithromycin capsules; however, the Cmax was reduced by 24%. Administration of cimetidine (800 mg) two hours prior to azithromycin had no effect on azithromycin absorption.
The serum protein binding of azithromycin is variable in the concentration range approximating human exposure, decreasing from 51% at 0.02 µg/mL to 7% at 2 µg/mL.
Following oral administration, azithromycin is widely distributed throughout the body with an apparent steady-state volume of distribution of 31.1 L/kg. Greater azithromycin concentrations in tissues than in plasma or serum were observed. High tissue concentrations should not be interpreted to be quantitatively related to clinical efficacy. The antimicrobial activity of azithromycin is pH related and appears to be reduced with decreasing pH. However, the extensive distribution of drug to tissues may be relevant to clinical activity.
The extensive tissue distribution was confirmed by examination of additional tissues and fluids (bone, ejaculum. prostate, ovary, uterus, salpinx, stomach, liver, and gallbladder). As there are no data from adequate and well-controlled studies of azithromycin treatment of infections in these additional body sites, the clinical importance of these tissue concentration data is unknown.
Following a regimen of 500 mg on the first day and 250 mg daily for 4 days, only very low concentrations were noted in cerebrospinal fluid (less than 0.01 µg/mL) in the presence of non-inflamed meninges.
Store at room temperature between 59-86 degrees F (15-30 degrees C); keep away from light and moisture. Do not Store in the bathroom. Keep all medicines away from children and pets.
ExusAzithromycin Capsules should not be used after the date marked EXP on the box.
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EXUS PHARMACEUTICAL (NIG) LTD
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