Amrizol Actions

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How do you administer this medicine?

Actions of Amrizol in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Pharmacology: Amrizol is a synthetic antibacterial compound. Disposition of Amrizol 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 Amrizol 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 Amrizol accounting for approximately 20% of the total. Renal clearance of Amrizol is approximately 10 mL/min/1.73 m2.

Amrizol 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 Amrizol is bound to plasma proteins. Both the parent compound and the metabolite possess in vitro bactericidal activity against most strains of anaerobic bacteria.

Amrizol appears in cerebrospinal fluid, saliva and breast milk in concentrations similar to those found in plasma. Bactericidal concentrations of Amrizol have also been detected in pus from hepatic abscesses.

Plasma concentration of Amrizol are proportional to the administered dose. An eight hour intravenous infusion of 100-4,000 mg of Amrizol in normal subjects showed a linear relationship between dose and peak plasma concentration.

In patients treated with intravenous Amrizol, 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 Amrizol averaged 25 mcg/mL with trough (minimum) concentrations averaging 18 mcg/mL.

Decreased renal function does not alter the single-dose pharmacokinetics of Amrizol. However, plasma clearance of Amrizol is decreased in patients with decreased liver function.

In one study newborn infants appeared to demonstrate diminished capacity to eliminate Amrizol. 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: Amrizol 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, Amrizol is generally bactericidal at concentrations equal to or slightly higher than the minimal inhibitory concentrations. Amrizol 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 Amrizol?

Do not use Amrizol in or near the eyes. Watering of the eyes may occur when the medicine is used too close to the eyes.

If Amrizol 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 Amrizol, thoroughly wash the affected area(s) with a mild, nonirritating cleanser, rinse well, and gently pat dry.

To use:

  • After washing the affected area(s), apply Amrizol with your fingertips.
  • Apply and rub in a thin film of medicine, using enough to cover the affected area(s) lightly. You should apply the medicine to the whole area usually affected by rosacea, not just to the pimples themselves.
  • Wash the medicine off your hands.

To help keep your rosacea under control, keep using Amrizol for the full time of treatment. You may have to continue using Amrizol every day for 9 weeks or longer. Do not miss any doses.

Dosing

The dose of Amrizol 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 Amrizol. 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.

  • For topical dosage forms (cream, gel, and lotion):
    • For rosacea:
      • Adults—Apply to the affected area(s) of skin two times a day, morning and evening, for nine weeks.
      • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of Amrizol, 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.

Storage

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.

Amrizol administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Use this medication exactly as it was prescribed for you. Do not use the medication in larger amounts, or use it for longer than recommended by your doctor.

Wash your hands before and after using this medication.

Insert the cream into your vagina using the applicator as directed.

Your medication may come with disposable applicators. Use each applicator for only 1 day and then throw it away. If you use the medication twice daily, wash and rinse the applicator after your morning dose and use it again for your evening dose. Then throw it away and use a new applicator the next day.

Use Amrizol vaginal for the entire length of time prescribed by your doctor, even during your menstrual period. Your symptoms may get better before the infection is completely treated.

If the infection does not clear up after you have finished one course of therapy, or if your symptoms get worse, see your doctor. You may have another type of infection that Amrizol will not treat.

You may need to use a sanitary napkin during treatment, but do not use a tampon.

Amrizol vaginal can cause you to have unusual results with certain medical tests. Tell any doctor who treats you that you are using this medication.

Store Amrizol vaginal at room temperature away from moisture or heat. Do not allow it to freeze.

Amrizol pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Normal Subjects:

Following a single, intravaginal 5 gram dose of Amrizol Vaginal Gel (equivalent to 37.5 mg of Amrizol) to 12 normal subjects, a mean maximum serum Amrizol concentration of 237 ng/mL was reported (range: 152 to 368 ng/mL). This is approximately 2% of the mean maximum serum Amrizol concentration reported in the same subjects administered a single, oral 500 mg dose of Amrizol (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 Amrizol Vaginal Gel and 1 to 3 hours after dosing with oral Amrizol.

The extent of exposure [area under the curve (AUC)] of Amrizol, when administered as a single intravaginal 5 gram dose of Amrizol Vaginal Gel (equivalent to 37.5 mg of Amrizol), was approximately 4% of the AUC of a single oral 500 mg dose of Amrizol (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 Amrizol, when administered vaginally, was approximately half that of an equivalent oral dosage.

Patients with Bacterial Vaginosis:

Following single and multiple 5 gram doses of Amrizol Vaginal Gel to 4 patients with bacterial vaginosis, a mean maximum serum Amrizol 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 Amrizol 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 Amrizol on anaerobes are largely unknown. The 5-nitro group of Amrizol 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 Amrizol 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, Amrizol 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

  1. 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).
  2. 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).
  3. 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).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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