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Anaerobyl Actions |
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Pharmacology: Anaerobyl is a synthetic antibacterial compound. Disposition of Anaerobyl in the body is similar for both oral and intravenous dosage forms, with an average elimination half-life in healthy humans of eight hours.
The major route of elimination of Anaerobyl and its metabolites is via the urine (60-80% of the dose), with fecal excretion accounting for 6-15% of the dose. The metabolites that appear in the urine result primarily from side-chain oxidation [1-(β-hydroxyethyl)-2-hydroxymethyl-5-nitroimidazole and 2-methyl-5-nitroimidazole-1-yl-acetic acid] and glucuronide conjugation, with unchanged Anaerobyl accounting for approximately 20% of the total. Renal clearance of Anaerobyl is approximately 10 mL/min/1.73 m2.
Anaerobyl is the major component appearing in the plasma, with lesser quantities of the 2-hydroxymethyl metabolite also being present. Less than 20% of the circulating Anaerobyl is bound to plasma proteins. Both the parent compound and the metabolite possess in vitro bactericidal activity against most strains of anaerobic bacteria.
Anaerobyl appears in cerebrospinal fluid, saliva and breast milk in concentrations similar to those found in plasma. Bactericidal concentrations of Anaerobyl have also been detected in pus from hepatic abscesses.
Plasma concentration of Anaerobyl are proportional to the administered dose. An eight hour intravenous infusion of 100-4,000 mg of Anaerobyl in normal subjects showed a linear relationship between dose and peak plasma concentration.
In patients treated with intravenous Anaerobyl, using a dosing regimen of 15 mg/kg loading dose followed six hours later by 7.5 mg/kg every six hours, peak steady-state plasma concentrations of Anaerobyl averaged 25 mcg/mL with trough (minimum) concentrations averaging 18 mcg/mL.
Decreased renal function does not alter the single-dose pharmacokinetics of Anaerobyl. However, plasma clearance of Anaerobyl is decreased in patients with decreased liver function.
In one study newborn infants appeared to demonstrate diminished capacity to eliminate Anaerobyl. The elimination half-life, measured during the first three days of life, was inversely related to gestational age. In infants whose gestational ages were between 28 and 40 weeks, the corresponding elimination half-lives ranged from 10.9 to 22.5 hours.
Microbiology: Anaerobyl is active in vitro against most obligate anaerobes, but does not appear to possess any clinically relevant activity against facultative anaerobes or obligate aerobes. Against susceptible organisms, Anaerobyl is generally bactericidal at concentrations equal to or slightly higher than the minimal inhibitory concentrations. Anaerobyl has been shown to have in vitro and clinical activity against the following organisms: Anaerobic Gram-Negative Bacilli, Including: Bacteroides species, including the Bacteroides fragilis group (B. fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, B. vulgatus), Fusobacterium species.
Anaerobic Gram-Positive Bacilli, Including: Clostridium species and susceptible strains of Eubacterium.
Anaerobic Gram-Positive Cocci, Including: Peptococcus species, Peptostreptococcus species.
Do not use Anaerobyl in or near the eyes. Watering of the eyes may occur when the medicine is used too close to the eyes.
If Anaerobyl does get into your eyes, wash them out immediately, but carefully, with large amounts of cool tap water. If your eyes still burn or are painful, check with your doctor.
Before applying Anaerobyl, thoroughly wash the affected area(s) with a mild, nonirritating cleanser, rinse well, and gently pat dry.
To use:
To help keep your rosacea under control, keep using Anaerobyl for the full time of treatment. You may have to continue using Anaerobyl every day for 9 weeks or longer. Do not miss any doses.
The dose of Anaerobyl will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Anaerobyl. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of Anaerobyl, apply it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Take the extended-release Anaerobyl tablet (Anaerobyl) on an empty stomach, at least 1 hour before or 2 hours after eating a meal.
Do not crush, chew, or break an extended-release tablet. Swallow it whole. Breaking the pill may cause too much of the drug to be released at one time.
Take this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Anaerobyl will not treat a viral infection such as the common cold or flu.
To be sure this medication is not causing harmful effects, your blood may need to be tested often. Your liver function may also need to be tested. Visit your doctor regularly.
This medication can cause unusual results with certain medical tests. Tell any doctor who treats you that you are using Anaerobyl.
Store at room temperature away from moisture and heat.
Normal Subjects:
Following a single, intravaginal 5 gram dose of Anaerobyl Vaginal Gel (equivalent to 37.5 mg of Anaerobyl) to 12 normal subjects, a mean maximum serum Anaerobyl concentration of 237 ng/mL was reported (range: 152 to 368 ng/mL). This is approximately 2% of the mean maximum serum Anaerobyl concentration reported in the same subjects administered a single, oral 500 mg dose of Anaerobyl (mean Cmax = 12,785 ng/mL, range: 10,013 to 17,400 ng/mL). These peak concentrations were obtained in 6 to 12 hours after dosing with Anaerobyl Vaginal Gel and 1 to 3 hours after dosing with oral Anaerobyl.
The extent of exposure [area under the curve (AUC)] of Anaerobyl, when administered as a single intravaginal 5 gram dose of Anaerobyl Vaginal Gel (equivalent to 37.5 mg of Anaerobyl), was approximately 4% of the AUC of a single oral 500 mg dose of Anaerobyl (4977 ng-hr/mL and approximately 125,000 ng-hr/mL, respectively).
Dose-adjusted comparisons of AUCs demonstrated that, on a mg to mg comparison basis, the absorption of Anaerobyl, when administered vaginally, was approximately half that of an equivalent oral dosage.
Patients with Bacterial Vaginosis:
Following single and multiple 5 gram doses of Anaerobyl Vaginal Gel to 4 patients with bacterial vaginosis, a mean maximum serum Anaerobyl concentration of 214 ng/mL on day 1 and 294 ng/mL (range: 228 to 349 ng/mL) on day five were reported. Steady state Anaerobyl serum concentrations following oral dosages of 400 to 500 mg BID have been reported to range from 6,000 to 20,000 ng/mL.
Microbiology:
The intracellular targets of action of Anaerobyl on anaerobes are largely unknown. The 5-nitro group of Anaerobyl is reduced by metabolically active anaerobes, and studies have demonstrated that the reduced form of the drug interacts with bacterial DNA. However, it is not clear whether interaction with DNA alone is an important component in the bactericidal action of Anaerobyl on anaerobic organisms.
Culture and sensitivity testing of bacteria are not routinely performed to establish the diagnosis of bacterial vaginosis.
Standard methodology for the susceptibility testing of the potential bacterial vaginosis pathogens, Gardnerella vaginalis, Mobiluncus spp., and Mycoplasma hominis, has not been defined. Nonetheless, Anaerobyl is an antimicrobial agent active in vitro against most strains of the following organisms that have been reported to be associated with bacterial vaginosis:
Bacteroides spp.
Gardnerella vaginalis
Mobiluncus spp.
Peptostreptococcus spp.
Users | % | ||
---|---|---|---|
After food | 15 | 57.7% | |
Empty stomach | 6 | 23.1% | |
Before food | 3 | 11.5% | |
With a meal | 2 | 7.7% |
Taken 4 hours after moderate alcohol consumption caused unsteadiness and loss of balance. (Would have been fatal to have driven) Symptoms still persisting after 24 hours of finishing course. |
Information checked by Dr. Sachin Kumar, MD Pharmacology
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