Ofloxacin Actions

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Actions of Ofloxacin 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.
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Pharmacokinetics: Drug concentrations in serum (in subjects with tympanostomy tubes and perforated tympanic membranes), in otorrhea and in mucosa of the middle ear (in subjects with perforated tympanic membranes) were determined following otic administration of Ofloxacin solution. In two single-dose studies, mean Ofloxacin serum concentrations were low in adult patients with tympanostomy tubes, with and without otorrhea, after otic administration of 0.3% solution [4.1 ng/mL (n=3) and 5.4 ng/mL (n=5), respectively]. In adults with perforated tympanic membranes, the maximum serum drug level of Ofloxacin detected was 10 ng/mL after administration of a 0.3% solution. Ofloxacin was detectable in the middle ear mucosa of some adult subjects with perforated tympanic membranes (11 out of 15 subjects). The variability of Ofloxacin concentration in the middle ear mucosa was high. The concentrations ranged from 1.2-602 mcg/g after otic administration of a 0.3% solution. Ofloxacin was present in high concentrations in otorrhea (389-2850 mcg/g, n=13) 30 min after otic administration of a 0.3% solution in subjects with chronic suppurative otitis media and perforated tympanic membranes. However, the measurement of Ofloxacin in the otorrhea does not necessarily reflect the exposure of the middle ear to Ofloxacin.

Microbiology: Ofloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Ofloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation and transcription. Cross-resistance has been observed between Ofloxacin and other fluoroquinolones. There is generally no cross-resistance between Ofloxacin and other classes of antibacterial agents eg, β-lactams or aminoglycosides.

Ofloxacin has been shown to be active against most strains of the following microorganisms, both in vitro and clinically in otic infections :

Gram-Positive Aerobes: Staphylococcus aureus and Streptococcus pneumoniae.

Gram-Negative Aerobes: Haemophilus influenzae, Proteus mirabilis, Moraxella catarrhalis and Pseudomonas aeruginosa.

How should I take Ofloxacin?

Take Ofloxacin only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

Ofloxacin comes with a Medication Guide. Read and follow the instructions carefully. Ask your doctor if you have any questions.

You may take Ofloxacin with or without food.

Drink plenty of fluids while you are being treated with Ofloxacin. Drinking extra water will help to prevent some unwanted effects of Ofloxacin.

If you are also using antacids containing aluminum or magnesium (such as Maalox®, Mylanta®), multivitamins (with calcium, iron, or zinc), didanosine (Videx®), or sucralfate (Carafate®), take these medicines at least 2 hours before or 2 hours after you take Ofloxacin. These medicines may keep Ofloxacin from working properly.

Keep using Ofloxacin for the full treatment time, even if you feel better after the first few doses. Your infection may not clear up if you stop using the medicine too soon.

Dosing

The dose of Ofloxacin 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 Ofloxacin. 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 Ofloxacin, take 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. Do not double doses.

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.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Ofloxacin 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.
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Use Ofloxacin otic exactly as directed by your doctor. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you.

Do not use this medication in the eyes or take it by mouth. Ofloxacin otic is intended for use in the ears only.

In general, Ofloxacin otic should be used as follows:

Ofloxacin ear drops are usually used twice a day, about 12 hours apart. Follow your doctor's instructions.

Use all of the medication that has been prescribed. Symptoms may begin to improve before the condition is completely treated. If you do not use all of the medication prescribed, the condition could return or worsen.

It is important to use Ofloxacin otic regularly to get the most benefit.

Notify your doctor if the condition does not improve or appears to worsen.

Avoid getting water inside of the affected ear(s) during treatment with Ofloxacin. Care should be used while bathing, and swimming may not be recommended. Talk to your healthcare provider.

Store Ofloxacin otic at room temperature, away from moisture, heat, and direct light. Keep the bottle properly capped.

Ofloxacin 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.
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Pharmacokinetics:

Serum, urine and tear concentrations of Ofloxacin were measured in 30 healthy women at various time points during a ten-day course of treatment with Ofloxacin Ophthalmic Solution. The mean serum Ofloxacin concentration ranged from 0.4 ng/mL to 1.9 ng/mL. Maximum Ofloxacin concentration increased from 1.1 ng/mL on day one to 1.9 ng/mL on day 11 after QID dosing for 10 1/2 days. Maximum serum Ofloxacin concentrations after ten days of topical ophthalmic dosing were more than 1000 times lower than those reported after standard oral doses of Ofloxacin.

Tear Ofloxacin concentrations ranged from 5.7 to 31 mcg/g during the 40 minute period following the last dose on day 11. Mean tear concentration measured four hours after topical ophthalmic dosing was 9.2 mcg/g.

Corneal tissue concentrations of 4.4 mcg/mL were observed four hours after beginning topical ocular application of two drops of Ofloxacin Ophthalmic Solution every 30 minutes. Ofloxacin was excreted in the urine primarily unmodified.

Microbiology:

Ofloxacin has in vitro activity against a broad range of gram-positive and gram-negative aerobic and anaerobic bacteria. Ofloxacin is bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Ofloxacin is thought to exert a bactericidal effect on susceptible bacterial cells by inhibiting DNA gyrase, an essential bacterial enzyme which is a critical catalyst in the duplication, transcription, and repair of bacterial DNA.

Cross-resistance has been observed between Ofloxacin and other fluoroquinolones. There is generally no cross-resistance between Ofloxacin and other classes of antibacterial agents such as beta-lactams or aminoglycosides.

Ofloxacin has been shown to be active against most strains of the following organisms both in vitro and clinically, in conjunctival and/or corneal ulcer infections as described in the section.

*Efficasy for this organism was studied in fewer than 10 infection

The safety and effectiveness of Ofloxacin Ophthalmic Solution in treating ophthalmologic infections due to the following organisms have not been established in adequate and well-controlled clinical trials. Ofloxacin Ophthalmic Solution has been shown to be active in vitro against most strains of these organisms but the clinical significance in ophthalmologic infections is unknown.

Clinical Studies:

Conjunctivitis: In a randomized, double-masked, multicenter clinical trial, Ofloxacin Ophthalmic Solution was superior to its vehicle after 2 days of treatment in patients with conjunctivitis and positive conjunctival cultures. Clinical outcomes for the trial demonstrated a clinical improvement rate of 86% (54/63) for the Ofloxacin treated group versus 72% (48/67) for the placebo treated group after 2 days of therapy. Microbiological outcomes for the same clinical trial demonstrated an eradication rate for causative pathogens of 65% (41/63) for the Ofloxacin treated group versus 25% (17/67) for the vehicle treated group after 2 days of therapy. Please note that microbiologic eradication does not always correlate with clinical outcome in anti-infective trials.

Corneal Ulcers: In a randomized, double-masked, multi-center clinical trial of 140 subjects with positive cultures, Ofloxacin Ophthalmic Solution treated subjects had an overall clinical success rate (complete reepithelialization and no progression of the infiltrate for two consecutive visits) of 82% (61/74) compared to 80% (53/66) for the fortified antibiotic group, consisting of 1.5% tobramycin and 10% cefazolin solutions. The median time to clinical success was 11 days for the Ofloxacin treated group and 10 days for the fortified treatment group.



References

  1. DailyMed. "OFLOXACIN: 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. EPA DSStox. "Ofloxacin: 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 Ofloxacin 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 Ofloxacin. 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

1 consumer reported administration

When best can I take Ofloxacin, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Ofloxacin should be taken After food. In any case, this may not be the right description on how you ought to take this Ofloxacin. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Ofloxacin can be taken.
Users%
After food1
100.0%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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