Actions of Rozacrème 0.75% in details
Pharmacology: Rozacrème 0.75% is a synthetic antibacterial compound. Disposition of Rozacrème 0.75% 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 Rozacrème 0.75% 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 Rozacrème 0.75% accounting for approximately 20% of the total. Renal clearance of Rozacrème 0.75% is approximately 10 mL/min/1.73 m2.
Rozacrème 0.75% 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 Rozacrème 0.75% is bound to plasma proteins. Both the parent compound and the metabolite possess in vitro bactericidal activity against most strains of anaerobic bacteria.
Rozacrème 0.75% appears in cerebrospinal fluid, saliva and breast milk in concentrations similar to those found in plasma. Bactericidal concentrations of Rozacrème 0.75% have also been detected in pus from hepatic abscesses.
Plasma concentration of Rozacrème 0.75% are proportional to the administered dose. An eight hour intravenous infusion of 100-4,000 mg of Rozacrème 0.75% in normal subjects showed a linear relationship between dose and peak plasma concentration.
In patients treated with intravenous Rozacrème 0.75%, 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 Rozacrème 0.75% averaged 25 mcg/mL with trough (minimum) concentrations averaging 18 mcg/mL.
Decreased renal function does not alter the single-dose pharmacokinetics of Rozacrème 0.75%. However, plasma clearance of Rozacrème 0.75% is decreased in patients with decreased liver function.
In one study newborn infants appeared to demonstrate diminished capacity to eliminate Rozacrème 0.75%. 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: Rozacrème 0.75% 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, Rozacrème 0.75% is generally bactericidal at concentrations equal to or slightly higher than the minimal inhibitory concentrations. Rozacrème 0.75% 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.
How should I take Rozacrème 0.75%?
Take Rozacrème 0.75% 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 Rozacrème 0.75% tablet (Rozacrème 0.75%) 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 Rozacrème 0.75% 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. Rozacrème 0.75% will not treat a viral infection such as the common cold or flu.
To be sure Rozacrème 0.75% 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 Rozacrème 0.75%.
Store Rozacrème 0.75% at room temperature away from moisture and heat.
Rozacrème 0.75% administration
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 Rozacrème 0.75% tablet (Rozacrème 0.75%) 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. Rozacrème 0.75% 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 Rozacrème 0.75%.
Store at room temperature away from moisture and heat.
Rozacrème 0.75% pharmacology
Normal Subjects:
Following a single, intravaginal 5 gram dose of Rozacrème 0.75% Vaginal Gel (equivalent to 37.5 mg of Rozacrème 0.75%) to 12 normal subjects, a mean maximum serum Rozacrème 0.75% concentration of 237 ng/mL was reported (range: 152 to 368 ng/mL). This is approximately 2% of the mean maximum serum Rozacrème 0.75% concentration reported in the same subjects administered a single, oral 500 mg dose of Rozacrème 0.75% (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 Rozacrème 0.75% Vaginal Gel and 1 to 3 hours after dosing with oral Rozacrème 0.75%.
The extent of exposure [area under the curve (AUC)] of Rozacrème 0.75%, when administered as a single intravaginal 5 gram dose of Rozacrème 0.75% Vaginal Gel (equivalent to 37.5 mg of Rozacrème 0.75%), was approximately 4% of the AUC of a single oral 500 mg dose of Rozacrème 0.75% (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 Rozacrème 0.75%, when administered vaginally, was approximately half that of an equivalent oral dosage.
Patients with Bacterial Vaginosis:
Following single and multiple 5 gram doses of Rozacrème 0.75% Vaginal Gel to 4 patients with bacterial vaginosis, a mean maximum serum Rozacrème 0.75% 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 Rozacrème 0.75% 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 Rozacrème 0.75% on anaerobes are largely unknown. The 5-nitro group of Rozacrème 0.75% 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 Rozacrème 0.75% 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, Rozacrème 0.75% 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.
References
- DailyMed. "BISMUTH SUBCITRATE POTASSIUM; METRONIDAZOLE; TETRACYCLINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Metronidazole: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Metronidazole: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
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Information checked by Dr. Sachin Kumar, MD Pharmacology
