آزیترومایسین بهتر است با شکم خالی خورده شود، حداقل ۱ ساعت قبل یا ۲ ساعت بعد از غذا. این دارو به شکل هر 24 ساعت تجویز میشود و در روز اول دو عدد، ولی روزهای بعد یک عدد مصرف می شود. در ضمن در کنار این دارو بایستی از شربتهای خلط آور مثل موکولین یا اکسپکتورانت یا سالبوتامول هر ۸ ساعت یک قاشق و یا قرص های خلط آور، پس از ۲ ساعت مصرف کپسول، استفاده نمود.تا خلطها ی موجود خارج گرددو ایجاد اختلال احتمالی در ریه ننماید .
یک پاسخ حساسیتی نادر به آنتیبیوتیکها آنافیلاکسی است که نیازمند توجه و مراقبت فوری پزشکی میباشد. آنافیلاکسی به سرعت پیشرفت میکند و با علائمی چون تورم لبها و دور چشم، کهیر یا تورمهای پوستی، غش ناگهانی، ضربان قلب تند یا خسخس سینه یا مشکل در تنفس مشخص میشود.
داده های فارماکولژیک[ویرایش]
با مصرف اولین دوز ۵۰۰ میلی گرمی نیمه عمر دارو ۱۱ تا ۱۴ ساعت میباشد. نیمه عمر ۶۸ ساعت بعد از مصرف چند دوز متوالی بدست می آید ( داروشناسی دیویس برای پرستاران ). مدت اثر آزیترومالیسین طولانی است. ۶۸ ساعت طول میکشد تا نیمی از دارو از بدن خارج شود.
پیوند به بیرون[ویرایش]
Azithromycin (Azyth, Zithromax, Azithrocin, Zmax, Azin, Zedd, Azocam, Penalox, Azi-Once, Zeto) is an azalide, a subclass of macrolide antibiotics. It is derived from erythromycin, with a methyl-substituted nitrogen atom incorporated into the lactone ring, thus making the lactone ring 15-membered.
Azithromycin is used to treat or prevent certain bacterial infections, most often those causing middle ear infections, strep throat, pneumonia, typhoid, gastroenteritis, bronchitis and sinusitis. In recent years, it has been used primarily to prevent bacterial infections in infants and those with weaker immune systems. It is also effective against certain sexually transmitted infections, such as nongonococcal urethritis, chlamydia, and cervicitis. Some studies have indicated it also to be effective against late-onset asthma, but these findings are controversial and not widely accepted.
Azithromycin is used to treat many different infections, including acute otitis media, nonstreptococcal bacterial pharyngitis, gastrointestinal infections such as traveler's diarrhea, respiratory tract infections such as pneumonia, cellulitis, babesiosis, Bartonella infection, chancroid, cholera, donovanosis, leptospirosis, Lyme disease, malaria, Mycobacterium avium complex disease, Neisseria meningitis, pelvic inflammatory disease, pertussis, scrub typhus, toxoplasmosis, and salmonellosis. It is used to prevent bacterial endocarditis and some sexually transmitted infections. It is also effective against localized dental infections, uncomplicated skin and skin structure infections, urethritis and cervicitis and also genital ulcer disease. Azithromycin is used as a second line treatment for strep throat and for those allergic to penicillin. It has a similar antimicrobial spectrum to erythromycin, but is more effective against certain Gram-negative bacteria, in particular, Haemophilus influenzae (although it would not be the first choice of treatment in this infection). Azithromycin resistance has been described and is endemic in many areas. Long-term use in treating Staphylococcus aureus infections with azithromycin may increase bacterial resistance to this and other macrolide antibiotics.
Most common side-effects are gastrointestinal: diarrhea (5%), nausea (3%), abdominal pain (3%), and vomiting. Fewer than 1% of patients stop taking the drug due to side-effects. Nervousness, dermatologic reactions, and anaphylaxis have been reported. As with all antimicrobial agents, pseudomembranous colitis can occur during and up to several weeks after Azithromycin therapy. In the past, physicians cautioned women that antibiotics can reduce the effectiveness of oral contraceptives. However, new research shows that antibiotics, with the exception of rifampin and rifabutin, do not affect the effectiveness of hormonal contraceptives, such as the pill, patch or vaginal ring. This change in advice comes because to date there is no evidence that conclusively demonstrates that antibiotics (other than rifampicin or rifabutin) affect these contraceptives.
Azithromycin suspension has an objectionable taste, so it can be difficult to administer to young children, i.e., 2–5 years, who may spit it out.
In 2013, the FDA issued a warning saying that azithromycin "can cause abnormal changes in the electrical activity of the heart that may lead to a potentially fatal irregular heart rhythm." The FDA noted in the warning a 2012 study released by the New England Journal of Medicine that found the drug may increase the risk of death, especially in those with heart problems, compared with those on other antibiotics such as amoxicillin or no antibiotic. The warning indicated that people with preexistent conditions are at particular risk, such as those with QT interval prolongation, low blood levels of potassium or magnesium, a slower than normal heart rate, or those who use of certain drugs used to treat abnormal heart rhythms, or arrhythmias.
Mechanism of action
Azithromycin prevents bacteria from growing by interfering with their protein synthesis. It binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA. Nucleic acid synthesis is not affected.
Spectrum of bacterial susceptibility and resistance
Chlamydia pneumoniae, Chlamydia trachomatis, Eikenella corrodens, Escherichia coli, Haemophilus influenzae, Moraxella catarrhalis, Mycobacterium chelonae, Mycoplasma fermentans, Neisseria gonorrhoeae and Ureaplasma urealyticum are generally susceptible to azithromycin dihydrate, while Pseudomonas aeruginosa, and Staphylococcus aureus are resistant to azithromycin dihydrate. In general, Streptococcus pyogenes is susceptible. Some Brevibacterium spp., Corynebacterium amycolatum, Haemophilus influenzae and Mycobacterium abscessus have developed resistance to azithromycin dihydrate to varying degrees.
The following represents azithromycin susceptibility data on medically significant organisms.
Unlike erythromycin, azithromycin is acid-stable, so it can be taken orally with no need of protection from gastric acids. It is readily absorbed, but its absorption is greater on an empty stomach. Time to peak concentration in adults is 2.1 to 3.2 hours for oral dosage forms and one to two hours after a dose. Due to its high concentration in phagocytes, azithromycin is actively transported to the site of infection. During active phagocytosis, large concentrations are released. The concentration of azithromycin in the tissues can be over 50 times higher than in plasma, due to ion trapping and its high lipid solubility (volume of distribution is too high).
Azithromycin's half-life allows a large single dose to be administered and yet maintain bacteriostatic levels in the infected tissue for several days.
According to Davis' Drug Guide for Nurses, following a single dose of 500 mg, the half-life of azithromycin is 11–14 h. The longer half-life of 68 h is achieved only when multiple doses are consumed. Biliary excretion of azithromycin, predominantly unchanged, is a major route of elimination. Over the course of a week, approximately 6% of the administered dose appears as unchanged drug in urine.
The name Azithromycin is derived from the azane-substituent and erythromycin.
A team of researchers at the Croatian pharmaceutical company Pliva — Gabrijela Kobrehel, Gorjana Radobolja-Lazarevski, and Zrinka Tamburašev, led by Dr. Slobodan Đokić — discovered azithromycin in 1980. It was patented in 1981. In 1986, Pliva and Pfizer signed a licensing agreement, which gave Pfizer exclusive rights for the sale of azithromycin in Western Europe and the United States. Pliva put its azithromycin on the market in Central and Eastern Europe under the brand name of Sumamed in 1988. Pfizer launched azithromycin under Pliva's license in other markets under the brand name Zithromax in 1991. Pfizer's exclusive rights have since lapsed and Pliva-manufactured azithromycin is also marketed in the United States by generic drug maker Teva Pharmaceuticals (which now owns Pliva).
After several years, the U.S. Food and Drug Administration (FDA) approved AzaSite, an ophthalmic formulation of azithromycin, for the treatment of eye infections. AzaSite is marketed in the U.S. and Canada by Inspire Pharmaceuticals, a wholly owned subsidiary of Merck.
Azithromycin is commonly administered in tablet or oral suspension (a one-dose version was made available in 2005). It is also available for intravenous injection and in a 1% ophthalmic solution. Tablets come in doses of 250 mg and 500 mg. Oral suspension comes in strengths of 100 mg/5 ml and 200 mg/5 ml. The 250-mg tablets are often dispensed in packages of six and commonly referred to as a "Z-Pak," whereas the 500-mg tablets are commonly available commercially in a pack of three tablets, or "Tri-Pak," intended as a three-day treatment. A common dose of oral azithromycin therapy consists of a "double dose" of medication on the first day of treatment and subsequent treatment for four or five additional days. With the "Z-Pak", this means two 250-mg tablets (a total of 500 mg) on the first day and one 250-mg tablet once daily for the next four days.
Pfizer brand name, i.e. Zithromax, azithromycin tablets are mottled pink, unscored, film-coated, modified oval-shaped tablets containing azithromycin monohydrate and the following inactive ingredients: butylated hydroxytoluene, calcium phosphate, carmine, colloidal silicon dioxide, FD&C red # 40 lake, FD&C yellow # 6 lake, hypromellose (2910, 15cP), lactose monohydrate, magnesium stearate, pregelatinized starch, sodium lauryl sulfate, talc, titanium dioxide, and triacetin. In Colombia (South America), it is marketed under the name Zaret from Laboratorios Bussié. In Bangladesh, it is marketed under the name Azithin from Chemist Laboratories Ltd. and Penalox from Rephco Pharmaceuticals Limited. In Canada azithromycin is marketed by Sandoz.
Azi-Once™ (6 x 250 mg capsules) is manufactured by Jamjoom Pharmaceuticals in Jeddah, Kingdom of Saudi Arabia