Fluoroquinolones - Revision history

Fiorecastro at 16:50, 6 January 2023

2023-01-06T16:50:29Z

Kitnmre at 02:45, 23 May 2016

2016-05-23T02:45:16Z

Janlino: /* Side Effects and Contraindications */

2013-01-08T12:50:21Z

Side Effects and Contraindications

Karag7: /* Spectrum of Activity */

2009-08-20T16:22:36Z

Spectrum of Activity

Jtulloch at 09:48, 24 October 2008

2008-10-24T09:48:17Z

Jtulloch: /* Side Effects and Contraindications */

2008-10-24T09:47:36Z

Side Effects and Contraindications

Jtulloch: /* Pharmacokinetic Considerations */

2008-10-24T09:43:04Z

Pharmacokinetic Considerations

Jtulloch: /* Pharmacokinetic Considerations */

2008-10-24T09:33:18Z

Pharmacokinetic Considerations

Jtulloch: /* Spectrum of Activity */

2008-10-24T09:31:35Z

Spectrum of Activity

Jtulloch: /* Mechanism of Action */

2008-10-24T09:24:34Z

Mechanism of Action

← Older revision		Revision as of 16:50, 6 January 2023
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	{{Learning		{{Learning
	\|Vetstream = [https://www.vetstream.com/equis/Content/Freeform/fre00358.asp Nitrofurans Nitroimidazoles Quinolones]}}		\|Vetstream = [https://www.vetstream.com/equis/Content/Freeform/fre00358.asp Nitrofurans Nitroimidazoles Quinolones]}}
		+
		+	==Webinars==
		+	<rss max="10" highlight="none">https://www.thewebinarvet.com/pharmacology/webinars/feed</rss>

← Older revision		Revision as of 02:45, 23 May 2016
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	* In young growing dogs there can be '''erosion of the articular cartilages'''. This may be the case in other young growing animals, we however do know that it is safe to use danofloxacin with calves.		* In young growing dogs there can be '''erosion of the articular cartilages'''. This may be the case in other young growing animals, we however do know that it is safe to use danofloxacin with calves.
	* In man small CNS problems have been reported, as yet these haven't been confirmed in animals. They include nausea, vomiting, headaches and a predisposition of seizures if a patient is an epileptic. There is an increased risk of these problems if NSAIDs are given concurrently.		* In man small CNS problems have been reported, as yet these haven't been confirmed in animals. They include nausea, vomiting, headaches and a predisposition of seizures if a patient is an epileptic. There is an increased risk of these problems if NSAIDs are given concurrently.
		+
		+	{{Learning
		+	\|Vetstream = [https://www.vetstream.com/equis/Content/Freeform/fre00358.asp Nitrofurans Nitroimidazoles Quinolones]}}

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 They are on the whole safe drugs with few side effects; those of significance are mentioned below:
 * High doses of enrofloxacin in cats can cause '''retinal blindness'''.
-* In young growing dogs there can be '''erosion of the articular cartilages'''. This may be the case in other young growing animals, we however do know that this it is safe to use danofloxacin with calves.
+* In young growing dogs there can be '''erosion of the articular cartilages'''. This may be the case in other young growing animals, we however do know that it is safe to use danofloxacin with calves.
-* In man small CNS problems have been reported, as yet these haven't been confirmed in animals. They include nausea, vomiting, headaches and a predisposition of seizures if a patient is an epileptic. They is an increased risk of these problems if NSAIDs are given concurrently.
+* In man small CNS problems have been reported, as yet these haven't been confirmed in animals. They include nausea, vomiting, headaches and a predisposition of seizures if a patient is an epileptic. There is an increased risk of these problems if NSAIDs are given concurrently.

@@ Line 26: / Line 26: @@
 * Works well against Mycoplasmas and Rickettsia.
 * Poor activity against obligate anaerobes.
-* Their activity is very pH dependent wit their activity increasing above pH 7.4 and decreasing below pH 7.0.
+* Their activity is very pH dependent with their activity increasing above pH 7.4 and decreasing below pH 7.0.
 It should be noted that they are active at very low concentrations, they don't kill protective enterococci and anaerobes, and they will inhibit aminoglycoside and beta-lactam resistant bacteria.
 ==Pharmacokinetic Considerations==

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+{{review}}
 {{toplink
 |linkpage =WikiDrugs
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 [[Image: Nalidixic Acid.png|thumb|right|250px|Nalidixic Acid - The Parent Drug of the Fluoroquinolones]]
 The parent drug of the quinolone family was '''Nalidixic acid''', this was found to be very narrow spectrum. It worked well only against gram negative enterobacteriaceae and resistance quickly developed. This limited it's use now for just urinary tract infections and for treatment of ''Aeromonas salmonicida'' in fish. Due to the restricted spectrum of the quinolones fluoroquinolones were developed to increase the range. The most commonly used in practice are '''Enrofloxacin, Marbofloxacin, Danofloxacin, Difloxacin, Ibafloxacin and Orbifloxacin.'''
@@ Line 17: / Line 18: @@
 These drugs also have the ability to cross animal's cell membranes through porins. This means that this group of drugs is capable of acting upon intracellular pathogens.
 ==Spectrum of Activity==
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 It should be noted that they are active at very low concentrations, they don't kill protective enterococci and anaerobes, and they will inhibit aminoglycoside and beta-lactam resistant bacteria.
 ==Pharmacokinetic Considerations==
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 * They are excreted in both the bile and urine, 70% in the bile. Urine concentrations do reach high levels and remain high up to a day after a single dose.
 * Some metabolites are active (such as ciprofloxacin of enrofloxacin). The formation of these active metabolites are highly species dependent as it depends upon the liver enzymes present in each species. For example the horse doesn't metabolise enrofloxacin very well.
 ==Side Effects and Contraindications==

← Older revision		Revision as of 09:47, 24 October 2008
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	==Side Effects and Contraindications==		==Side Effects and Contraindications==
		+	They are on the whole safe drugs with few side effects; those of significance are mentioned below:
		+	* High doses of enrofloxacin in cats can cause '''retinal blindness'''.
		+	* In young growing dogs there can be '''erosion of the articular cartilages'''. This may be the case in other young growing animals, we however do know that this it is safe to use danofloxacin with calves.
		+	* In man small CNS problems have been reported, as yet these haven't been confirmed in animals. They include nausea, vomiting, headaches and a predisposition of seizures if a patient is an epileptic. They is an increased risk of these problems if NSAIDs are given concurrently.

@@ Line 32: / Line 32: @@
 * They are highly lipophilic and have a low degree of ionisation.
 * They are well absorbed from the gastrointestinal tract.
-* It isn't very well protein bound and so
+* They aren't very well protein bound and so distribute well into extracellular and all intracellular fluids, including the CSF and prostatic fluid. They on do have a tendency to accumulate in the prostate, kidney and lung.
 ==Side Effects and Contraindications==

← Older revision		Revision as of 09:31, 24 October 2008
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	==Spectrum of Activity==		==Spectrum of Activity==

		+	* Active against gram-negative species including aerobic species such as ''Pseudomonas aeruginosa''.
		+	* Active against gram-positives (doesn't work that well against Streptococcal species and enterococci.)
		+	* Works well against Mycoplasmas and Rickettsia.
		+	* Poor activity against obligate anaerobes.
		+	* Their activity is very pH dependent wit their activity increasing above pH 7.4 and decreasing below pH 7.0.

		+	It should be noted that they are active at very low concentrations, they don't kill protective enterococci and anaerobes, and they will inhibit aminoglycoside and beta-lactam resistant bacteria.

	==Pharmacokinetic Considerations==		==Pharmacokinetic Considerations==

← Older revision		Revision as of 09:24, 24 October 2008
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	==Mechanism of Action==		==Mechanism of Action==

		+	Fluoroquinolones work by inhibiting bacterial DNA gyrase or the topoisomerase enzyme and thus inhibit bacterial DNA replication and transcription. The gyrase enzyme is usually the target in gram-negative bacteria, whilst the topoisomerase enzyme is the target in most gram-positive bacteria. This kills the bacteria and so the drug is a bactericidal and concentration dependent.

		+	These drugs also have the ability to cross animal's cell membranes through porins. This means that this group of drugs is capable of acting upon intracellular pathogens.

	==Spectrum of Activity==		==Spectrum of Activity==