Term Paper: Moxifloxacin Pharmacology

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Moxifloxacin (Pharmacology)

Composition/formulation & structure/nomenclature a) What is in the drug?

The drug is an antibiotic, and it comes under the classification of fluoroquinolones. It is primarily used to fight bacteria in the body, and to treat bacterial infections, including pneumonia, acute bronchitis, and sinusitis, and at times, for other purposes as well, depending upon the discretion of the attending physician. Its generic name is Moxifloxacin, and the brand names of this drug are Avelox, and Avelox IV.

A b) What form (solid, liquid, salt etc.) and doses of the active ingredient?

Moxifloxacin can be taken in either an oral dose, or can be given intravenously through an IV infusion. One must remember that when the drug Moxifloxacin is to be taken orally, then one must drink plenty of fluids, and even when consuming the drug, one must take care to consume a full glass of water along with it. However, Moxifloxacin can be taken with or also without food, and it is generally to be taken as a single dose, once a day. Every dose must be taken at the same time, every day. One must be very careful to talk to the Doctor first before attempting to take this drug in any form, because of the fact that the drug can be dangerous to those who are suffering from a heart condition of any kind, and are therefore under medication for that ailment, like for example, if they are taking drugs such as quinidine, branded as Cardioquin, Quinidex, and Quinaglute, and others, procainamide, which is branded as Pronestyl, Procan SR, and others, amiodarone, branded under Cordarone, Pacerone, and others, sotalol sold as Betapace, and others. (1)

In addition, if the patient is already suffering from a low level of potassium in his blood, or if he has a slow heart rate, any heart problems, liver diseases, or epilepsy, then he must inform the physician about it, so that extra precautions may be taken. The medicine can be taken about four hours before, or about eight hours after antacids which contain or have as their most important component magnesium, calcium, or aluminum. Even if the patient has had to have ulcer medication, like for example, sucralfate, then vitamin or zinc supplements, or powders which contain didanosyne as one of their ingredients may be given as an additional supplement, and this may well increase the absorption of the drug into the system. (1) The active ingredient in Moxifloxacin is moxifloxacin hydrochloride, and in its IV form, the drug, sold as Avelox, can be administered as an intravenous 0.8% sodium chloride solution which contains 400 mg moxifloxacin. (2)

What are the inactive ingredients (excipients)?

The inactive ingredients of the drug Moxifloxacin are as follows: "microscocrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, hypromellose, titanium dioxide, polyethylene glycol and ferric oxide." (3) This is a list containing the excipients of the drug Moxifloxacin and the solution for that of infusion are "Sodium chloride Ph. Eur., USP, Ph. Jap., hydrochloric acid 1N, sodium hydroxide solution 2N, water for injection Ph. Eur., USP, Ph. Jap." (4) d) What is the chemical name and structure of the active component?

The chemical name of the drug Moxifloxacin is considered as "moxifloxacin, MXFX, IUPAC:1-cyclopropyl-7-(5,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-8-methoxy-4-oxo-quinoline-3-carboxylic acid, MW: 401.431 | MF: C21H24FN3O4." (5) As far as the structure of the active component of Moxifloxacin is concerned, it must be noted that all drugs of this type, that is, quinolones, with antibacterial activity, have a 4-quinolone nucleus having nitrogen at position 1, a carboxyl group which is at position 3, and also a ketone coming at position 4. (6) It must also be noted that Moxifloxacin varies from other quinolones because of the fact that it has a methoxy function at the level of the 8 position, and an 'S-S' configured at the diazabicyclononyl ring moiety is found at the 7 position. (7) This can be understood by the following figure.

Diagram Reference: (38) e) What chemical class does it belong to?

The chemical class that the drug Moxifloxacin belongs to is that of a floroquinolone and the drug also is considered to have pneumococcal activity, which can be proved to be better than that of levofloxacin, and is found to be almost similar to that of trovafloxacin. (8) f) What aspects of its structure are important with respect to its function?

The newly developed moxifloxacin compound can be stated to be superior to the already existing ones in its potency, in its broad spectrum of activity, in its basic pharmacodynamics, and also in its pharmacokinetics. It has been found that its safety profiles are also infinitely superior to others of the same kind. (9) In general, when a person has a bacterial infection in his body, it is characterized by a systemic inflammation demonstrated in the massive activation of both the macrophages in the reticuloendothelial systems, and in the circulating leukocytes, and in the release of cytokines, the development of hypotension, and in the adhesion molecule expression on the epithelial cells. The inevitable consequences of all these events may be sepsis, septic shock, and even multiple organ failure. Also, in general, when such an infection is initially treated with appropriate antibiotics, there will inevitably be a certain type of reaction. Quinolones such as Moxifloxacin served to reduce the in-vitro production of TNF-a, IL-1b, and IL-6 by LPS-stimulated human monocytes. However, in alveolar macrophages, it was found that the TNF production after the introduction of LPS stimulation was not reduced by ciprofloxacin. (10)

2. Absorption, distribution, metabolism & excretion a) How is the drug absorbed and distributed?

When Moxifloxacin is given as an oral tablet, it gets absorbed by the gastrointestinal tract, which is the entire digestive tract, right from the mouth up to the anus. The complete 'bioavailability' of Moxifloxacin can be said to be about 90%, where bioavailability means the rate and also the extent to which an active drug is able to enter the general circulation of an individual, thereby allowing access to the very site of the action. The phenomenon is measured either by the measurement of the concentration of the drug in the system, or by the degree of the pharmacologic response being exhibited by the patient. When the drug is administered with a fatty meal, the absorption is not at all affected, and in the same way, the consumption of yoghurt also does not in a great way affect the absorption of Moxifloxacin. (11) It must be stated that the absorption of the drug happens almost immediately after it has been applied. In the case of an IV infusion, after a single 400 mg intravenous one hour infusion, the peak plasma concentrations were found at the end of the infusion. (12)

Diagram Reference: (38) b) What are the effects of protein binding and lipid/tissue uptake?

When experiments were conducted to evaluate the protein binding action of the drug Moxifloxacin, by a method called the 'ultra filtration method', the process is as described: the test materials in the form of fluids, like for example, human and rabbit serum, beef broth, and sterile water, were all incubated in ambient air for about two hours, and after the pH was adjusted, the drug was added to the various fluids in concentrations of 5, 10, 20, and 40 µg/ml, after which the fluids were incubated again for two more hours. Half the samples were centrifuged at 3000 into g for twenty minutes. The following protein binding was seen as being different for different samples: in human serum it was at "54%, + or - 14%, in rabbit serum it was 24% + or - 5%, in beef broth it was 33%, and in sterile water, it was 0%." (13) In addition, there was found to be no co-relation between the degree of protein binding and concentration of the drug. (13) Most of the time, the lasting equilibrium between blood and tissue cannot be always the same, and what this mean is that although in general all antibiotics manage to achieve equilibrium in blood and tissues, it need not happen all the time. When micro dialysis was used to measure the tissue drug absorption in the case of Moxifloxacin, it was found that concentrations in ISF of this drug corresponded to unbound concentrations in plasma, and was lower in whole tissue specimens. (14)

Describe its pharmacokinetic parameters.

The pharmacokinetics of moxifloxacin was studied in NMRI mice, and in monkeys, beagle dogs, and other animals, and in healthy human beings. The plasma concentration vs. time courses of the compound which was unchanged and the derived pharmacokinetic parameters were used to study the pharmacokinetic parameters. The results reveal a clear dependence on the species. The drug was absorbed quickly, and a major portion reached systemic circulation within two hours after absorption. (15) d) What is the drug's route and extent of metabolism

Moxifloxacin is a drug which attains good penetration into both peripheral tissues as well as into inflammatory fluids. It also shows in vitro activity in cases of staphylococci and… [END OF PREVIEW]

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