CHEMISTRY OF TRAMADOL

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Product Category: Seminar

Product Code: 00002621

No of Pages: 45

No of Chapters: 3

File Format: Microsoft Word

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TABLE OF CONTENTS

 

CHAPTER ONE

1.0          INTRODUCTION

1.1     HISTORY OF TRAMADOL AND ITS STASTITICS

 

CHAPTER TWO

20      CHEMISTRY OF TRAMADOL AND CLASSIFICATION OF TRAMADOL

2.1.1 STRUCTURE AND CHEMICAL NAME OF TRAMADOL CHEMICAL STRUCTURE OF TRAMADOL (cis-configuration)  

2.1.2             SYNTHESIS OF TRAMADOL MECHALISM OF ACTION

2.1.3  CHEMICAL AND PHYSICAL PROPERTIES OF TRAMADOL

 

CHAPTER 3

3.0     USES OF TRAMADOL

3.0     THERAPEUTIC APPLICATION AND EXTENT OF THERAPEUTIC USES AND EPIDMIOLOGY

3.1.0 EFFECT OF TRAMADOL (POSITIVE)

3.1.1 ADVERSE REACTIONS IN HUMANS

3.12  HARMFULL USE OF TRAMADOL

3.1.3  ABUSE OF TRAMADOL AND DEPENDENSE

3.1.4 TOXICOLOGY OF TRAMADOL

3.1.5 CONTROL OF TRAMADOL AND IMPACT OF SCHEDULING

 

4.0     SUMMARY

REFERENCES  

 

 

 

 

 

 

CHAPTER ONE

1.0 INTRODUCTION

Tramadol hydrochloride [TMH], chemically known as [1R,2R]-vel-2-[dimethlamino]-1-[3-methoxyphecy] cynonexanol [figure]is a synthetic analogue of codine and is a naturally acting analgestic agent.

1.    It is metabolized by the anytochrom P450 enzyme system in the liver to form eleven matabolites of which 0-desmethy tramado [M1] predomilate and has anagestic properties

2.    It has been used since 1977 for the  relief of severe physical pain and has been the most widely sold opioid analgestic drug in the world.

3.    TMH is official in European pharamacopeia [EP]

4.    It describe nonaqueoua titration with perchloric acid as tritrant the end point being located pontentiometically ultraviolet spetrophometry.

High performance liquid chometrography, thin layer chomatrography –detromrtry capillary isotachophysis flow injection chemileum nescence spectrometry, voitametry ion-setective-bised potentionmetry visible spectrometry, and trtrimetry for determining TMH in pharmaceutical dosage forms.

In addition, there have been part of its assay when present in combination with other drugs. TDH and ibuprofen ware assayed simultaneously by the first –order denvative spetrophytometry and HPLC with UV-detected. The TMH along with detetroprofen and haloperidot have been determine by HPLC-deode array detection [DAD] method simultaneous analysis of TMH and acceclofenac  in a commercial tablet was accomplished also by HPLC with UV-detection method. Simultaneous determination of paracetamol, TNH and dompenriodone in combine dosage form using RP-HPLC has been reported by karun akaran etal.

 In recent years, there has been an increased tending towards  development of stability –indication analysis, using the approach to stress testing enshrimed in international  conference harmonization [ICT] guideline Q2A[R2].this approach is being extended to pharmaceutical to enable accurate and prease qualification of drugs in the presence of their degradation products. Though there are many reported methods of the analysis of TMH either alone or in combination with other drugs in pharmaceutical dosage forms, the literate on the stability –indication method is scarce. Mohammed etal have elevated the stability of tramadol enantiomers using a chiral stability – indicating capillary electrophoresis  method and its application to pharmaceutical analysis. Chemical stability of TMH in infection has been reported by Gupta.

Ultra-performance liquid chromatography [UPEC] is a relatively  new technique giving new possibility in liquid  chromatography especially concerning stecrise of time and anal solvent consumption. UPLC system is designed in a special way to withstand high system back pressure special analysis colume UPLC acquity UPLC BEH C18 packed with 1.7 jum partickes are used in the system. The UPLC system allows shortening analysis time up to nine time compared to used convention of HPLC system, but separation efficiency remains the same or even improve as efficiency and speed of analysis are of great importance in many application of liquid chonmatography, especially in pharmaceutical, toxicological and chemical analysis, where cost, UPLC could play significant role in the future of liquid chromatography.

Three report are found in the literature dealing with the application of UPLC with mass spectrometric detection for the determine nations of TMH in different matrices. A sensitive UPLC-MS\MS method for TMH in urine and whole blood in forenoons context has very recently been reported kasprzk-hordarn etal. Determine TMH in surface water by solid-phase extraction and UPLC-positive etectrospray ionization mass spectrometry.

Simultaneous screening and quantification of 29 drugs abuse including TMH in oral third has seen reported by badawi atai sohd phrase extraction and UPLC-MS/MS.

 

TABLE 1: LINEARITY AND REGRESSION PARAMETERS WITH PRESSISION DATA

Parameters

Value

Linear range ng ml-1                      

0.5-300

Limits of quantification [LOG], ng ml-1

0.2

Slope [b]

 

Intercept [a]

19330.0

Correlation coefficient [r]           

0.9999

Standard deviation of b,[sb]             

76.0

 

Standard deviation of a [sa]           

13694.5

 

By liquid chromatography positive etectrospray ionization tender mass spectrunetry has recently been used for the multiresidue analysis  of drugs of abuse in waste water and surface water.

Though a member of  liquid chromate graphing method have earlier propose for TMH no attempt has been made to apply these new type of LC [UPLC] for pharmaceutical except in body fluids oral fluids and surface and waste water despite its many fold advantages.

The aim of this work was to develop a rapid, precise, accurate and validated stability indication UPLC method for  the determination of tramadol HCL in bulk and tablet. This was accomplish with a water acquity UPLC system and acquity UPLC system and acquity BEH column [C18,100mm 21MM,AND 1.7 JUM]. The stability indicating power of the method was established  by comparing the chromatogram obtained under optimize condition before forced degredation with those after degredation via acidic, basic, hydrytitic, oxidative then and photolytic stress condition.


1.1   HISTORY OF TRAMADOL AND ITS STASTITICS

Tramadol [brand name ultra] is an oral, opiod pain relieving drug that is marketed under a veriety of trade names with ultram and ultracent being the most widely prescribe and recognized.

Tramadol is most often prescribe to that moderate level of pain including dental, osteoporosis, and neuropathy in both acute and chronic setting it is also improved for treating cancer pain in period lees than three months.

Tramadol is thought to be safe due to lower risk of tolerance abuse, and dependence, but it has lower clinical value then other opiates. The drugs has only about one-tenth of the pain-reducing qualities of morphine.

Tramadol stand apart from other operates for two reasons;

·      Tramadol is a fully synthetic drug, which means that it is man-made and does not occur in nature. This is in contract to morphine and codine-which are natural operates derived from the opium poppy. It also differs from drugs like hydromorphine, hydro codeine, and oxycodone which, whole also semi synthetic and made in a laboratory, still retain some natural qualities.

·      Tramadol has an uncommon, anal- acting benefit. Tramadol works as an opiate in the expected way to manage the perception of pain, but be young that, it allows increase availability of two other neuro transmitter chemical in the brain called norepinephrine and Serotonin-Norepinephrine is note for its ability to improve concentration, and serotonin manges an array of function including sleep and mood.

 Comepared to others drugs and medications, tramadol is relatively young. The drugs was created by a German drugs and company that specialize in treating pain in 1962. The medication was tested for 15 years in 1977 under the name tramal. The drugs was a success for the company tramadol is widely prescribe around the world for pain relief .however it was not until 1995 that the drugs become available in the US. Now, the medication is quite popular in America.

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