Peak plasma concentrations occur 2 to 3 hours after an oral dose and 1 to 2 hours after intravenous dosage. However, azithromycin is extensively distributed into the tissues, and tissue concentrations subsequently remain much higher than those in the blood; in contrast to most other antibacterials, plasma concentrations are therefore of little value as a guide to efficacy. High concentrations are taken up into white blood cells.
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There is little diffusion into the CSF when the meninges are not inflamed. Data from animal studies indicate that azithromycin crosses the placenta. Small amounts of azithromycin are demethylated in the liver, and it is excreted in bile mainly as unchanged drug and a number of inactive metabolites have also been detected. The terminal elimination half-life is about 68 hours. Azithromycin is a nitrogen-containing macrolide azalide with actions and uses similar to those of erythromycin.
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It is given in the treatment of respiratory-tract infections including otitis media , in skin and soft-tissue infections, and in uncomplicated genital infections. Azithromycin may also be used for the prophylaxis, and as a component of regimens in the treatment, of Mycobacterium avium complex MAC infections. It is used in some countries for the prophylaxis of endocarditis in atrisk patients unable to take penicillin.
It is also used in the management of trachoma and typhoid. For details of all these infections and their treatment, see under Choice of Antibacterial.
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Azithromycin has been tried in protozoal infections such as babesiosis below , crytosporidiosis, and toxoplasmosis. It is given orally or by intravenous infusion usually as the dihydrate; doses are expressed in terms of the anhydrous substance. Azithromycin dihydrate mg is equivalent to about mg of anhydrous azithromycin. The capsule formulation should be given at least 1 hour before, or 2 hours after, meals. The usual oral adult dose of azithromycin is mg as a single dose daily for 3 days. Alternatively, an initial dose of mg may be followed by mg daily for a further 4 days.
For uncomplicated genital infections caused by Chlamydia trachomatis and for chancroid, 1 g of azithromycin is given as a single dose. A single dose of 2 g has been given for uncomplicated gonorrhoea. For the treatment of granuloma inguinale, an initial dose of 1 g followed by mg daily may be given, or 1 g may be given once a week for at least 3 weeks, until all lesions have completely healed. In the USA, a modified-release preparation given as an oral suspension is available. The product delivers a single dose of 2 g and should also be taken on an empty stomach.
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It is licensed for the treatment of acute bacterial sinusitis or community-acquired pneumonia in adults. For prophylaxis of disseminated MAC infections, azithromycin 1. For treatment or secondary prophylaxis, mg once daily should be given with other antimycobacterials.
For mild or moderate typhoid caused by mumdrug-resistant strains, mg once daily may be given for 7 days. For details of doses in infants and children, see below. Azithromycin dihydrate may also be given initially by intravenous infusion to adults in doses equivalent to mg of azithromycin as a single daily dose in the treatment of community-acquired pneumonia and pelvic inflammatory disease; treatment should be changed to the oral route after at least 2 days in pneumonia and after 1 or 2 days in pelvic inflammatory disease. In a prospective, randomised study involving 58 patients with babesiosis, azithromycin with atovaquone was found to be as effective as, and associated with fewer adverse effects than, standard therapy with quinine and clindamy-cin.
Azithromycin mg once daily, or to mg on day 1 followed by mg once daily thereafter, with atovaquone mg twice daily, both orally for 7 to 10 days, has been recommended by some experts in the USA for the treatment of Babesia microti infections.
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Immunocompromised patients may be given higher doses of azithromycin to mg daily. Azithromycin with quinine was reported to be effective in 2 patients who had not responded to quinine plus clindamycin. Azithromycin has been tried in the treatment of cholera. Macrolide antibacterials, including azithromycin, clarithromycin, and roxithromycin, have been investigated in the prevention of ischaemic heart disease, based on a suggested link between atherosclerosis and infection with Chlamydophila pneumoniae Chlamydia pneumoniae.
Although preliminary results from some pilot studies were promising, longer-term studies in large numbers of patients were disappointing and none of the three macrolides decreased ischaemic events or provided clinical benefit; indeed, in one study an unexpected increase in cardiovascular mortality was seen in those taking clarithromycin. Azithromycin has been studied in the management of malaria. Studies have shown that an initial loading dose of mg of azithromycin on the first day followed by mg daily thereafter for 20 weeks was effective in the prophylaxis of Plasmodium vivax malaria; the drug was well tolerated and the most frequently reported adverse effects were heartburn, paraes-thesia, and itching.
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Azithromycin in a dose of 0. However, further studies are warranted, especially in children and pregnant women. For reference to the use of azithromycin in the management of respiratory disorders, see under Erythromycin. Side effects are similar to E-Mycin, but usually milder. The big question is, do pills expire?
With a splitting headache, you reach into your medicine cabinet for some aspirin only to find the stamped expiration date on the medicine bottle is more than a year out of date. So, does medicine expire? Do you take it or don't you?
If you decide to take the aspirin, will it be a fatal mistake or will you simply continue to suffer from the headache? This is a dilemma many people face in some way or another. A column published in Psychopharmacology Today offers some advice. It turns out that the expiration date on a drug does stand for something, but probably not what you think it does. Since a law was passed in , drug manufacturers are required to stamp an expiration date on their products. This is the date at which the manufacturer can still guarantee the full potency and safety of the drug.
Most of what is known about drug expiration dates comes from a study conducted by the Food and Drug Administration at the request of the military. With a large and expensive stockpile of drugs, the military faced tossing out and replacing its drugs every few years. So, the expiration date doesn't really indicate a point at which the medication is no longer effective or has become unsafe to use. Medical authorities state if expired medicine is safe to take, even those that expired years ago.
A rare exception to this may be tetracycline, but the report on this is controversial among researchers.
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