Drug Metabolism - Revision history

Raiyani: /* Introduction */

2010-05-04T05:08:09Z

‎Introduction

Raiyani: /* Introduction */

2010-05-04T05:07:57Z

‎Introduction

Raiyani at 05:07, 4 May 2010

2010-05-04T05:07:39Z

Lakshmikantg: /* Test Results */

2009-11-22T20:59:50Z

‎Test Results

Lakshmikantg: /* Test Results */

2009-11-22T20:58:53Z

‎Test Results

Lakshmikantg: /* Preclinical drug metabolism and pharmacokinetic evaluation of GW844520 */

2009-11-22T20:57:31Z

‎Preclinical drug metabolism and pharmacokinetic evaluation of GW844520

Lakshmikantg: /* Preclinical drug metabolism and pharmacokinetic evaluation of GW844520 */

2009-11-22T20:41:11Z

‎Preclinical drug metabolism and pharmacokinetic evaluation of GW844520

Lakshmikantg: /* Sample Report */

2009-11-22T20:30:53Z

‎Sample Report

Tony.kurian@dolcera.com at 12:08, 18 November 2009

2009-11-18T12:08:44Z

Tony.kurian@dolcera.com at 08:23, 18 November 2009

2009-11-18T08:23:07Z

@@ Line 1: / Line 1: @@
 ==Introduction==
-[[Image:Drug metabolism1.jpg|right|300 px|Drug metabolism]]
+[[Image:Drug metabolism1.jpg|right|250 px|Drug metabolism]]
 Drug metabolism is a detoxification function the human body possesses to defend itself from environment hostility.
 Ideally, a drug should reach the site of action intact, cure the disease, and leave the body after it completes its mission.

@@ Line 1: / Line 1: @@
 ==Introduction==
 Drug metabolism is a detoxification function the human body possesses to defend itself from environment hostility.
 Ideally, a drug should reach the site of action intact, cure the disease, and leave the body after it completes its mission.
@@ Line 6: / Line 6: @@
 *To elucidate the function and fate of the drug
 *To manipulate the metabolic process of a potential drug.
 ==Metabolism Sites==

@@ Line 1: / Line 1: @@
-[[Image:Drug metabolism1.jpg|right|370 px|Drug metabolism]]
 ==Introduction==
 Drug metabolism is a detoxification function the human body possesses to defend itself from environment hostility.
@@ Line 6: / Line 6: @@
 *To elucidate the function and fate of the drug
 *To manipulate the metabolic process of a potential drug.
 ==Metabolism Sites==

@@ Line 73: / Line 73: @@
 '''Models/Species:'''Male CD1 mouse, male Sprague-Dawley rat, male beagle dog, male cynomolgus monkey and mixed gender human liver microsomes.
-==Test Results==
+===Test Results===
 {|border="2" cellspacing="0" cellpadding="4" width="72%"

@@ Line 179: / Line 179: @@
 |align = "center"|5
 |align = "center"|0.60 ± 0.03
 |}

← Older revision		Revision as of 20:57, 22 November 2009
Line 72:		Line 72:

	'''Models/Species:'''Male CD1 mouse, male Sprague-Dawley rat, male beagle dog, male cynomolgus monkey and mixed gender human liver microsomes.		'''Models/Species:'''Male CD1 mouse, male Sprague-Dawley rat, male beagle dog, male cynomolgus monkey and mixed gender human liver microsomes.
		+
		+	==Test Results==
		+
		+	{\|border="2" cellspacing="0" cellpadding="4" width="72%"
		+	\|align = "center" bgcolor = "#C2D69A" colspan = "7"\|'''Pharmacokinetics of GW844520 After Oral Administration to Mouse, Rat, Dog, and Monkey'''
		+
		+	\|-
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''Species'''
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''Dose (mg/kg)'''
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''Cmax (µg/mL)'''
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''Tmax (h)'''
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''AUC0- (µg h/mL)'''
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''T1/2 h'''
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''F (%)'''
		+
		+	\|-
		+	\|align = "center"\|'''Mouse'''
		+	\|align = "center"\|0.5
		+	\|align = "center"\|0.28
		+	\|align = "center"\|4
		+	\|align = "center"\|8.54
		+	\|align = "center"\|23.6
		+	\|align = "center"\|72
		+
		+	\|-
		+	\|align = "center"\|'''Rat'''
		+	\|align = "center"\|0.5
		+	\|align = "center"\|0.25 ± 0.02
		+	\|align = "center"\|2 (1-2)
		+	\|align = "center"\|4.14 ± 0.96
		+	\|align = "center"\|7.1 ± 1.7a
		+	\|align = "center"\|118
		+
		+	\|-
		+	\|align = "center"\|'''Dog'''
		+	\|align = "center"\|0.4
		+	\|align = "center"\|0.14 ± 0.02
		+	\|align = "center"\|24 (4-24)
		+	\|align = "center"\|22.8 ± 7.9
		+	\|align = "center"\|214 ± 30
		+	\|align = "center"\|51 ± 11
		+
		+	\|-
		+	\|align = "center"\|'''Monkey'''
		+	\|align = "center"\|0.4
		+	\|align = "center"\|0.12 ± 0.01
		+	\|align = "center"\|4 (4-8)
		+	\|align = "center"\|13.5 ± 0.6
		+	\|align = "center"\|88.4 ± 4.4
		+	\|align = "center"\|69 ± 6
		+
		+	\|}
		+
		+
		+
		+	{\|border="2" cellspacing="0" cellpadding="4" width="36%"
		+	\|align = "center" bgcolor = "#C2D69A" colspan = "3"\|'''In Vitro Cell Partitioning of GW844520 in Animal and Human Blood'''
		+
		+	\|-
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''Species'''
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''Concentration (µg/mL)'''
		+	\|align = "center" bgcolor = "#8DB4E3"\|'''Blood to plasma ratio'''
		+
		+	\|-
		+	\|align = "center" rowspan = "2"\|'''Mouse'''
		+	\|align = "center"\|0.25
		+	\|align = "center"\|0.56 ± 0.01
		+
		+	\|-
		+	\|align = "center"\|2.5
		+	\|align = "center"\|0.48 ± 0.02
		+
		+	\|-
		+	\|align = "center" rowspan = "2"\|'''Rat'''
		+	\|align = "center"\|0.25
		+	\|align = "center"\|0.50 ± 0.02
		+
		+	\|-
		+	\|align = "center"\|2.5
		+	\|align = "center"\|0.56 ± 0.03
		+
		+	\|-
		+	\|align = "center" rowspan = "2"\|'''Dog'''
		+	\|align = "center"\|0.25
		+	\|align = "center"\|0.52 ± 0.01
		+
		+	\|-
		+	\|align = "center"\|2.5
		+	\|align = "center"\|0.52 ± 0.01
		+
		+	\|-
		+	\|align = "center" rowspan = "2"\|'''Monkey'''
		+	\|align = "center"\|0.25
		+	\|align = "center"\|0.69 ± 0.06
		+
		+	\|-
		+	\|align = "center"\|2.5
		+	\|align = "center"\|0.62 ± 0.01
		+
		+	\|-
		+	\|align = "center" rowspan = "2"\|'''Human'''
		+	\|align = "center"\|0.5
		+	\|align = "center"\|0.54 ± 0.06
		+
		+	\|-
		+	\|align = "center"\|5
		+	\|align = "center"\|0.60 ± 0.03
		+
		+	\|}

← Older revision		Revision as of 20:41, 22 November 2009
Line 68:		Line 68:

	[[Image:struc.jpg\|center\|thumb\|300px\|'''Chemical Structure of GW844520''']]		[[Image:struc.jpg\|center\|thumb\|300px\|'''Chemical Structure of GW844520''']]
		+
		+	Plasmodium falciparum is the species of malaria parasite that predominates in Africa and is the cause of most of the mortality from malaria worldwide. Effective treatment options are often restricted due to drug resistance, particularly for P. falciparum. There is an immediate need to develop novel anti-malarial agents that provide rapid and effective treatment.GW844520 is fully active against isolates carrying resistance determinants to marketed agents and shows no cross-resistance with agents in current use, including atovaquone.
		+
		+	'''Models/Species:'''Male CD1 mouse, male Sprague-Dawley rat, male beagle dog, male cynomolgus monkey and mixed gender human liver microsomes.

@@ Line 61: / Line 61: @@
 [http://books.google.co.in/books?id=eYJXj59Cg_UC&pg=PT51&lpg=PT51&dq=preclinical+drug+metabolism+database&source=bl&ots=75HigyNNky&sig=VDNW182OYEleEr0iLQKgtOrww4I&hl=en&ei=yAEAS4P7KIyGkQWl9fiDDA&sa=X&oi=book_result&ct=result&resnum=3&ved=0CBsQ6AEwAg#v=onepage&q=preclinical%20drug%20metabolism%20database&f=false Source]
-==Sample Report==
+==Sample Example==
-{|border="2" cellspacing="0" cellpadding="4" width="100%"
+===Preclinical drug metabolism and pharmacokinetic evaluation of GW844520===
-|align = "center" bgcolor = "#FCD5B4"|'''S.No.'''
-|align = "center" bgcolor = "#FCD5B4"|'''Database'''
+GW844520, a non-chiral 4(1H)-pyridone derivative, is a potent, selective inhibitor of Plasmodium mitochondrial function blocking the electron transport chain machinery. The site of action of this class of compounds is cytochrome b, a critical element of the respiratory complex III or bc1 complex.
-|align = "center" bgcolor = "#FCD5B4"|'''Search by'''
-|align = "center" bgcolor = "#FCD5B4"|'''Phase'''
+[[Image:struc.jpg|center|thumb|300px|'''Chemical Structure of GW844520''']]
-|align = "center" bgcolor = "#FCD5B4"|'''Type of reaction'''
-|align = "center" bgcolor = "#FCD5B4"|'''Sub Type'''
-|align = "center" bgcolor = "#FCD5B4"|'''Sub sub Type'''
-|align = "center" bgcolor = "#FCD5B4"|'''Product'''
-|-
-|align = "center" bgcolor = "#FCD5B4"|'''1'''
-|align = "center" rowspan = "3"|<font color="#0000FF"><u>[http://www.drugmetabolism.co.uk/ReactionSelector2.aspx Drug Metabolism]</u></font>
-|align = "center"|Reaction Type
-|align = "center"|Phase I(Functionalisation reactions)
-|align = "center"|Oxidation
-|align = "center"|Carbon Oxidation
-|align = "center"|Aromatics
-|align = "center"|Diclofenac  to 3<nowiki>’</nowiki>-hydroxy diclofenac
-|-
-|align = "center" bgcolor = "#FCD5B4"|'''2'''
-|align = "center"|Functional Group - Alcohol
-|align = "center"|Phase I(Functionalisation reactions)
-|align = "center"|
-|align = "center"|
-|align = "center"|
-|align = "center"|Ethanol to Acetaldehyde
-|-
-|align = "center" bgcolor = "#FCD5B4"|'''3'''
-|align = "center"|Substrate - Phenytoin
-|align = "center"|Phase I(Functionalisation reactions)
-|align = "center"|
-|align = "center"|
-|align = "center"|
-|align = "center"|Phenytoin to (S)-hydroxy-phenytoin
-|-
-|align = "center" bgcolor = "#FCD5B4"|'''4'''
-|align = "center" rowspan = "2"|<font color="#0000FF"><u>[http://umbbd.msi.umn.edu/ University of Minnesota Biocatalysis/Biodegradation database]</u></font>
-|align = "center" rowspan = "2"|Pathway- Benzonitrile
-−
-−
-−
-−
-|align = "center"|<font color="#0000FF">[http://umbbd.msi.umn.edu/bzn/bzn_map.html Click here for Pathway]</font>
-|-
-|align = "center" bgcolor = "#FCD5B4"|'''5'''
-−
-−
-−
-−
-|align = "center"|<font color="#0000FF">[http://umbbd.msi.umn.edu/bzn/bzn_image_map.html Click here for Pathway (Graphic 5K format)]</font>
-|-
-|}