Amebazole Actions

How times a day do you take this medicine?
sponsored

Actions of Amebazole in details

The 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.
sponsored

Pharmacology: Amebazole is a synthetic antibacterial compound. Disposition of Amebazole 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 Amebazole 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 Amebazole accounting for approximately 20% of the total. Renal clearance of Amebazole is approximately 10 mL/min/1.73 m2.

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

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

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

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

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

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

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

If Amebazole 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 Amebazole, 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 Amebazole for the full time of treatment. You may have to continue using Amebazole every day for 9 weeks or longer. Do not miss any doses.

Dosing

The dose of Amebazole 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 Amebazole. 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.

Missed Dose

If you miss a dose of Amebazole, 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.

Amebazole administration

Administration 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.
sponsored

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 Amebazole tablet (Amebazole) 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. Amebazole 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 Amebazole.

Store at room temperature away from moisture and heat.

Amebazole pharmacology

Pharmacokinetics 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.
sponsored

Normal Subjects:

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

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

Patients with Bacterial Vaginosis:

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

Reviews

The results of a survey conducted on ndrugs.com for Amebazole are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Amebazole. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

User reports

2 consumers reported administration

When best can I take Amebazole, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Amebazole should be taken Empty stomach. In any case, this may not be the right description on how you ought to take this Amebazole. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Amebazole can be taken.
Users%
Empty stomach2
100.0%


Consumer reviews


There are no reviews yet. Be the first to write one!


Your name: 
Email: 
Spam protection:  < Type 28 here

Information checked by Dr. Sachin Kumar, MD Pharmacology

| Privacy Policy
This site does not supply any medicines. It contains prices for information purposes only.
© 2003 - 2022 ndrugs.com All Rights Reserved