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Abacavir With The Trade Name Of Ziagen Biology

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one of the drugs availibe to command HIV is Abacavir ( ABC ) , this drug is a man-made carbocyclic nucleosideanalog that has antiretroviral activity which can suppress both HIV-1 and HIV-2, more of all time it is one type of guanosine nucleoside contrary RNA polymerase inhibitor ( NRTI ) it means that it inhabits the rearward written text of HIV, in this manner it decreases the HIV virus ( Kohler et al. , 2010 ) in other words abacavir dose non bring around the HIV patients but merely holds and decreasses the harm of immune system further more it is besides applicable in bar of HIV when it is combined with other untiviral medicines for those who have been exposed to it.

( application ) this drug applicable in patients how can non take non-nucleoside contrary RNA polymerase inhibitors or peptidase inhibitors intervention of kids particularly those how have developed toxicity to stavudine ( d4T ) .

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Structure and belongingss:

Abacavir with the trade name of Ziagen. it is an enantiomorph with 1S, 4R absolute constellation on the cyclopentene ring.

it can be found in tow froms tablet ( xanthous ) or solution. ( environment ) it has a solubility of 77A mg/mL in distilled H2O at 25A°C. The tablets are coated with a movie that is made of hypromellose, polysorbate 80, man-made yellow Fe oxide, Ti dioxide, and triacetin ( daily med ) . this merchandise is stable. ( environment )

IUPAC Name

{ ( 1S,4R ) -4- [ 2-amino-6- ( cyclopropylamino ) -9H-purin-9-l ] cyclopent-2-en-1-yl } methyl alcohol

( De Clercq, 2009 )

Formula

C14H18N6OA

Molecular Weight

286.33232 [ g/mol ]

H-bond giver:

3

H-bond Acceptor

6

CAS figure

136470-78-5

( pub chem )

Pharmacodynamic belongingss:

Abacavir has a interacellular activation tract that was foremost described at 1994 ( synthesis ) in this tract Abacavir will transform to carbovir triphosphate in the cell abacavir will be hosphorylated by adenosine phosphotransfrase and abacavir monophosphate will be produced, cytosolic deminase will impact this and will bring forth abavir monophosphate wich has 2 parallel in cell triphosphate cabovir and diphosphate cabavir ( Francis, 2002 )

Abacavir active anabolite in cell is, carbovir triphosphate ( CBV-TP ) ) wich competes with an endogenous nucleotid RNA polymerase enzyme and inhibits written text of HIV viral RNA to DNA and will be produced in cell by phosphorylation, acts as concatenation eradicator for viral DNA, because it dose n’t hold the the 3’hydroxyl it prevents the formation of the 5 ‘ to 3 ‘ phosphodiester linkage that is indispensable for DNA olymerization in this manner it blocks HIV reproduction ( Achenbach et al. , 2010 )

Figure: Abacavir, interacellular activation tract

Pharmacokinetic belongingss:

Abacavir has a bioavability of 83 % and is extremely absorbed in unwritten disposal. distribution takes topographic point largely in vescular system and partially in CSF. It binds to about 50 % in plasma proteins ( Daily Med ) and concentration of Abacavir has no consequence in binding of drug to plasma proteins. ( Daily Med ) the half clip of abacavir in organic structure is about 1.5 hours ( European egency 1 ) . the chief metabolization topographic point for it is in liver, it is metabolized into two inactive metabolites via uridine diphosphate glucuronyl transferase and intoxicant dehydrogenase, which will be so eliminated through the hepatic metamorphosis ( kidneys ) ( moheme 7 ) about 83 % of abacavir dosage that have been used can be found in urine as metabolist and unchanged abacavir ( European egency 1 ) which merely 1 % of it is unchanged Abacavir due to this dose prescribed dose non need nephritic accommodation ( Achenbach et al. , 2010 ) .

Side consequence and toxicity information:

Pharmacological Effectss:

abacavir is a cardinal constituent in Ziagen ( R ) , Trizivir ( R ) and Epzicom ( R ) , surveies show that abacavir has more consequence when it is combined with other anti viral drugs ( Mounir Ait-Khaled ) .having a TNF genotype increases the hazard of hypersensitivity ( patent nunber WO 03018745A ( A2 ) ) . The hypersensitivity reaction ( AHSR ) is associated with HLA-B*5701allel that is immune system familial discrepancy ( Hughes et al. , 2004 ) which is a dangerous occurring in 5-8 % of those utilizing the drug, this factor has limited its usage. the hyper sensitiveness symptoms are: febrility, roseola, GI ( sickness, purging, diarrhoea, or abdominal hurting ) , constitutional ( generalised unease, weariness, or achiness ) , and respiratory ( dyspnoea, cough, or sore throat ) ( Hughes et al. , 2004 ) , there for the hazard of abacavir HSR must be considered when utilizing abacavir for HIV intervention ( Clay, 2002 ) , an allel trial is now recommended before utilizing this merchandise, which this will diminish its cost efficiency unless intervention with abacavir is as effectual and economically efficient as alternate drugs which can be used against AIDS ( Hughes et al. , 2004 ) . In some instances addition of destiny in the organic structure had been absorbed, this destiny largely accumulates in upper dorsum and cervix ( “ buffalo bulge ” ) , chest, and around the dorsum, thorax, and stomach country. ( day-to-day med )

Paths of Exposure ( environment )

Target Organ Effectss

No particular

Oral Toxicity

Not expected to be toxic

Skin Effectss

In a direct contact, is non expected

Eye Effectss

In direct contact, sever annoyance might happen

Sensitization

In cuticular exposure, allergic reaction might happen

Familial Toxicity

Mutagenicity occurs in research lab trials.

Carcinogenicity

Limited grounds for this may happen In high concentrations and besides depends to the period of taking the dose

Generative Effectss

Not expected

Interaction with other medicative merchandises and other signifiers of interaction:

abacavir has shown no clinically interaction to nutrient or other drugs because it dose non populate the metamorphosis mediate with CYP 3A4, CYP2C9 or CYP2D6 enzymes, how of all time the plasma concentration of Abacavir diminutions in presence of Potent enzymatic inducers.

Ethanol affects the metamorphosis of Abacavir by raising the AUC of abacavir to about 41 % .

How of all time Abacavir dosage non hold an impact on metamorphosis ethyl alcohol in organic structure. ( European egency 1 )

Posology and method of disposal:

Abacavir is used as a tablet or unwritten solution in HIV patient, the unwritten solution is used more in kids how over 3 months are and have a organic structure weight less than 14 kilogram ( European egency 1 ) . The dose is 600-mg one time a twenty-four hours or 300 milligram twice a twenty-four hours regimen for grownups how of all time in kids the dose used depends on organic structure weight ( jadide 1 pH ) . in kids the disposal alterations, in those who weight more than 30 kg the dose taken is the same as grownups, kids that weight between & gt ; 21 & lt ; 30 should take half of the drug in twenty-four hours and a whole tablet at flushing how of all time in kids which weight 14 to 21 kilogram this sum decreases to half a tablet, twice a twenty-four hours ( European egency 1 ) . the disposal mob is unwritten and are 83 % bio available, the soaking up is speedy and reaches peak concentration of 0.6 3to 2.5 one hr after utilizing.due to its good solubility in H2O and lipotropic dissolvers, it has a good distribution in organic structure with a volume distribution of 0.86A±0.15 L/kg ( Achenbach et al. , 2010 ) abacavir can be taken with or with out nutrient and this has no consequence on its exposure although it changes Tmax and Cmax ( Achenbach et al. , 2010 ) .for patients enduring of nephritic disfunction no accommodation of drug is needed how of all time in patients with mild hepatic jobs, this drug is non recommended because the metabolisation of this drug occurs in liver. abacvir is besides non recommended in gestation and in chest eating of the baby although the consequence of abacavir in this consumers is non yet been confirmed. ( European egency 1 )

No inauspicious reaction was absorbed, in a individual dosage up to 1200 milligram and day-to-day doses up to 1800 milligram with Abacavir. ( European egency 1 )

Synthesis routs Procedure:

Ziagen, ( 1S, Commonwealth of Independent States ) -4- [ 2-amino-6- ( cyclopropylamino ) -9H-pu~-9-y1 ] -2-cyclopentene- 1-methanol, was synthesized from ( IS,4R ) -azabicyclo [ 2.2.l ] hept-5-en-3. The most of import intermediate which makes it possible to acquire an efficient building of the purine is 2-Amino-4, 6-dichloro-5-formamidopyrhidi.

Man-made options:

There are two general attacks to doing 2’3′-didehydro ( i.e. , cyclopentenyl ) carbocyclic nucleosides are matching of the integral purine to a carbocycle and to utilize cyclopentenylamine to build the purine.

Figure: Retrosynthetic analysis of paths to Ziagen.

Different have been experimented:

it is non executable to utilize the path which converts the heterocyclic base to an activated allyalically cyclopntene since, in this mob, 2-aminopurine precursor in 2 amino-6-cyclopropylaminopurne, has a low solubility in the suited dissolver which is one of the grounds that makes the synthesis of 2 amino-6-cyclopropylaminopurne which is comparatively toxic, non fiddling in big graduated table, here the major job is the deficiency of N9/N7 regioselectivity in purine yoke. During the deblocking of intermediates, 7-substitute isomer decays and produces glycone which is a contamination more of all time to sublimate the concluding drug separation of N7 and N9 isomers are besides required and besides the production of intermediates had non been developed in big graduated table.

cyclopentenylamine synthesis:

reaction between sulfonyl nitrile and cyclopentadiene green goodss rademic lactam 3b which is an intermediate used to bring forth carbocyclic nucleoside and is executable in industrial production how of all time its unstable particularly in additive production building of purine from amine 5a.

Figure: Amino intoxicant intermediates to cyclopentenyl nucleosides.

Several jobs occur when transition of 3b to amide 7, isomeric and saturated by merchandises will be generate in the decrease measure, during deprotonation of any I± to the ester group which consequence the pureness of the drug.

Figure: effects of drosss generated in ester decreases.

In big graduated tables, the decrease of 6 with Ca borohydride frequently has a slow reaction another job is that it is hard to divide drosss like 11which is yield in Ca bromide decrease and has non activity against HIV-1 and non toxic and 12 which is synthesized by hydrogenation of 1.

To salvage stairss, they introduced lactam to amino acid and so reduced the amino acid with Li aluminium hydride. Lactam will hydrolyse and generates extremely crystalline salt in nowadays of H2O and strong acid ( 4a-4d ) . The pureness of crystalline depends on pureness of lactam ; if the dross is high it will be washed with THF.

The aluminium salt produced because high chelating of amino intoxicant, which is indissoluble in a hydrated dissolver, and unstable in visible radiation and air when concentrated from solution. To over come this job they add thermodynamically strong ligand for aluminium.for decrease they introduce it to H2O followed by Na fluoride this generates sodium aluminium fluoride which is indissoluble and can be extract by polar dissolver.

This procedure has besides done get downing with racemic lactam 3b, with enzymatic distinction of the monophosphate ; it will bring forth little enantiopure samples of 1 and 1b enantiomorph which is used for antiviral testing.

To sublimate the amino intoxicant 5a the most direct manner is the usage of hydrolysis / LAH decrease of 3a. how of all time an alternate manner is the more efficient, to add THF solutions of BOC lacyam 8 which was generated by derivitization of lactam 3a with di-ter-butyl dicarbonate in presence of catalyc DMAP and is stable at 25 C in aqueous THF, to sodium borohydride will bring forth extremely pure 9 on a 100 – gm graduated table although in larger graduated tables result in slow, uncomplete reactions. More of all time Na borohydride has a inclination to precipitate from THF/water mixture. For multi kg graduated tables, adding of three equivalents of methyl alcohol with catalytic acetic acid is needed.

Chloropyrimidine intermediate:

Rout reference below may supply enantiopure amino intoxicant. the original synthesis of carbocyclic 2-aminopurine nucleosides is to match 2-amino-4, 6-dichloropyrimidine with cyclopentylamines, by phenyldiazo interpolation adding Nitrogen at the 5-position of the ensuing pyrimidine intermediates.

Problems of this mob:

hazard of diazotizations in big graduated table

Properties of triaminopyrimidine intermediate which is generated with zinc decrease of the 5- diazopyrimidine ( 19 )

Chlorination of 13 might give to 14 in presence of with phosphoryl chloride or to 15 if refluxed in methylene chloride or trichloromethane with 6-8 equivalents of “ vilsmeier reagent ” .

To give 2,5-diamino-4,6-dichloropyrimidin ( e1 4 ) , chlorination of 2,5-diamino-4,6-dihydroxypyrimidine ( 13 ) with phosphoryl chloride in presence of quaternate ammonium chloride is required. here the draw dorsums are:

1. High debasement of get downing pyrimidine chlorination.

2.To isolate 14, chromatography is required.

To give 15 refluxing in chloride or trichloromethane with 6-8 equivalents of “ vilsmeier reagent is required ; in mild status this reagent allows efficient chlorination by protecting and stabilising 13. 15 can be stored as stable solid or be converted to 16 by acidic hydrolysis. PH plays an of import function when taking methylene groups from 15 or 16. in PH 1 in aqueous acid converts it to oxopyrimidines, how of all time lifting the PH to 3, will change over 16 to 17 in an ionic strength aqueous phosphate buffer, this buffer bound tats the solubility of reactant and merchandise.by diminishing PH in stairss, an over all of about 70 % output from 17 which can be isolate in a simple manner.due to this in big graduated tables they convert 13 to 17 which dose non required the isolation of 15or 16.

If the PH decreases to 1-2 by adding sulphuric acid, 17 will hydrolysis to 14. At PH 1, 17 will hydrolysis efficaciously to 14 in contrast at the same PH,15 and 16 will change over to oxopyrimdines. By refluxing 17 with catalytic hydrochloric acid in equeous ethyl alcohol, because both 14 and 17 are non sensitive to hydrolysis, a output of 14 ( 77 % ) will happen.

Figure: Chloropyrimidine intermediates to 2-aminopurines.

Matching and purin formation:

Vilsmeier chlorination chemical science and subsequent hydrolysis to supply 17, is scalable due to, demand of simple reagents and work up, simple the purification is and the stableness and pureness of solid intermediates generated in this procedure.17 is the most attractive intermediate in the synthesis of 1 and related 9-subsitituted 2-aminopurines and is utile reagent for synthesis of 2- aminopurins.it supplies 18 in & gt ; 85 % after crystallisation when condensation with amino intoxicant 5a ( which is generated from 9 un refluxing ethanolic HCl ) .

Activation provided with formylation T of the 5 – amino group makes the conditions for formation of 18 is more easier than formation of trimopyrimidines ( e.g 19 ) from 14, more of all time solid crystalline 18 ( which is a 5-formamdiointermediate ) is more stable to light and air compared with trimopyrimidines.with 4 equivalents of concentrated aqueous hydrochloric acid the cyclization of 18 to 20 occurs swimmingly in triethylorthoformate, by fade outing formamide 18 after adding acid the hydrochloride of 20 began to precipitate which will be used to fix 1 ( among a assortment of other fresh parallels ) .

The rapid formation of 20 suggested that the conformation of the formamide of 18 may be unfavourable for cyclization and that the add-on of H2O could interrupt internal H-bonds and facilitate cyclization. In order to better the cyclization mechanism by set uping the beginning of the C-8 C of 18, they synthesized 17 from Vilsmeier reagent, and converted it to [ 13c ] cyclized this in triethylorthoformate / aqueous hydrochloric acid. after crystallisation they have used they have add cyclopropylamin which is a suited salt in refluxing ethyl alcohol to supply them an high output of 1, they have used dissolvers because the free base of 1 is glass or solid froth and in this manner they can pin down them in dissolvers. This path was besides used to fix the HIV-inactive enantiomorph pound from 5d.

Figure: Synthesis of Ziagen

Analysis of procedure for prepration of abacavir:

In prepration of abacavir there are 3 stairss that still need betterment. here the chief stairss advantages and disadvantages of different methods have been compared.

A major and of import measure in readying of abacavir is to fix the intermediate which will transform to abacavir. The synthesis mentioned in EP 434 450 for this intent is clip devouring and needs a protection and reprotection sequence, get downing with di-halo aminopyrimidine and outputs to abacavire as free base.

another attack has been introduced in pateant figure US 6448 403 which uses diamino-dihydroxy as get downing stuff and when it is treated with POCl3 to bring forth the cardinal intermediate nevertheless the toxicity of POCl 3 and the complex salt generated by this reaction which is hard to stair makes the isolation and purification hard. An alternate manner is to handle the dichloro diamino pyrimidine with mixture of formic and acetic anhydride in this manner it becom formylated and to the full protected, the job of this sort of synthesizes is that it needs an extra measure to take the protecting group.

In abacavir synthesis one of the most of import portion is the cyclisation procedure of abacavir intermediates there are still jobs with sum giving up and purification of this procedure, particularly those which have an acyl group that is protecting the amino group at 2- and 5- place of the pyrimidine, due to that looking for a sufficient procedure is still an active field.For cyclisation of the { pyrmidine -5-yl } , In the synthesis of abacavir that is discussed above from ( cf.S.M.Daluge et al 2000 ) they used tritheyl orthoformate and concentrated aqueous hydrochloric acid. they have implied that cyclisation had been eased by add-on of H2O and this had distrupt internal H-bonds.in EP 434450-A which is published before this, cyclisation of the N-2-acylate abacavir intermediates which have protecting amino group at 2 and 5 place of pyrimidine by taking the amino group of the pyrimidine in the intermediate occurs in presence of a co dissolver and strong anhydrous acid they have used formic acid or reactive formic acid derived functions which may take 2 yearss in room temperature, the usage of caustic mineral acids to take the amino protective groups may harm the machines and bring forthing several by merchandises which have consequence on pureness and the concluding output of the merchandise and the sum of agent used is besides high 1-25 mole of solution of agent, high dilution rate and complicate, the long clip that is needed to take the amino protective group, need for isolation after vaporizing of dissolver by usage of chromatography and triturating to sublimate the free Abacavir base indicates the demand of more efficient manner.an alternate manner was introduced in patent figure US2010/0041883 A1 the cyclisation here has high output and pureness, low byproducts and the sum of agent used is besides decreased ( 2-5 mole of cycisating agent per mole ) compare the patents above and this reaction dosage takes topographic point without presence of H2O, here the formyle group of 5-amino group will be removed when it is introduced to anhydrous hydrochloride acid [ ( C1-C4 ) -alcohol ] / isopropoanol in the room temperature which the presence of intoxicant prevents the draw dorsums of known methods, followed by refluxing and presenting to ( C1-C4 ) alkyl orthoformate in temperature between 0 CIS and 30CIS , the compound ensuing from here can be convert to abacavir in presence of a base and a suited dissolver by reaction with cyclopropylamine, followed by hydrolysis in acidic status.

another attack has been introduced in patent figure US2010/0004446 A1 which uses a an inorganic base like alkaline metal hydrated oxide ( as Li, Na, K hydrated oxide ) comprised between 1 and 5 mole of base per mole of get downing stuff in a mixture of H2O and intoxicant to hydrolyse the expression ( ) and take the amino protective group, for this reaction they increased the temperature to 50 C which, reduces the clip of reaction which makes an advantage compared to methods known.

After cyclisation the intermediate abacavir can be isolate, as a salt or as free base, harmonizing to patent figure WO9852949 utilizing free bases to bring forth abacavir generates formless solids that can non be usage in big graduated table and needs purification this has implied the demand of a salt of abacavir. To bring forth the pharmaceutically salt from free base, the free base can be introduced to matching acid. Different sort of salts can be produced for this intent nevertheless abacavir hemi sulphate is the most preferable one. for illustration patent figure PCT/GB95/02014, uses succinate salt of compound, holding some advantages like easy formation of salt, and cristalization how of all time disadvantages like holding the inclination to agglomerates make it unwanted for tableting machines and holding multiple crystallisation signifiers with different belongingss, which indicate the demand of supervising when bring forthing so that unsought signifier is non produced. These have made it non executable in usage in pharmaceutical industry. in contrast abacavir hemi sulphate is preferred to utilize in industry due to characteristic like easy readying and purification, holding merely one signifier of crystallisation, has no inclination in hydration or solvation, this charachtesitic makes it suited for storage, good solubility which makes suited for readying of liquid preparation, no inclination to collection which prevents coevals of formless solids and eases the purification. ( AU7660 ( B2 )

another major measure which is of import in readying of abacavir, is the isolation of abacavir and had been investigated in different ways.in patent figure EP 434450-A isolation of abacavir had been done by usage of chromatography which produces solid exhausts and triturating with acetonitrile that generates gluey solids, these methods are clip devouring and expensive method and generates by merchandises. an alternate ways was introduced in patent figure US2010/0004446 A1 have used dissolvers like ( C2-C8 ) aliphatic quintessences or ( C6-C8 ) -aromatic hydrocarbons before separation of the aqueous stage followed by rinsing with aqueous to take the organic stage before the add-on of acceptable acid, here they have removed the H2O to acquire higher output in anhydrous dissolver, or instead to insulate the abcavir they have introduced crystallisation the abacavir which is the most sufficient manner, for this purpose inorganic stage can be washed before the crystallisation, the advantage of this method is that purification and isolation is much easier, and the concluding output is besides high.

Fabrication and technology:

Natural stuffs:

2,5-Diamino-4,6-dihydroxypyrimidine

( Chloromethylene ) dimethylammonium chloride

( 1S,4R ) -4-Amino-2-cyclopentene-1-methanol

Triethylamine

Tartaric acid, dibenzoate,

( – ) -Orthoformate or diethoxymethyl ethanoate

Cyclopropylamine

Abafungin

Manufacturing Procedure:

The reaction between 2,5-diamino-4,6-dihydroxypyrimidine ( I ) and ( chloromethylene )

dimethylammonium chloride consequences to dichloropyrimidine, in which the both aminic groups will derivate to amidines, with HCl in hot ethyl alcohol it will partly hydrolyze this outputs to N- ( 2-amino-4,6-dichloro-pyrimidin-5-yl ) -N, Ndimethylformamidene ( II ) following that they hydrolysis it with buffer at PH 3.2 that will ensue to ( 2-amino-4,6-dichloro-pyrimididin-5-ylamino ) ethanal ( III ) . Condensation of chloropyrimidine ( III ) in the presence of triethylamine and NaOH Condensation with ( 1S,4R ) -4-amino-2-cyclopentene-1-methanol ( IV ) consequences to [ 2-amino-4-chloro-6- ( 4-hydroxymethyl-cyclopent-2-enylamino ) pyrimidin-5-ylamino ] -acetaldehyde ( V ) .to collect the right enantiomorph ( IV ) of racemic aminocyclopentene they resolut of diastereomeric salts with D-dibenzoyltartaric acid. refluxing triethyl orthoformate or diethoxymethyl ethanoate has done to supply Cyclization of ( V ) to the corresponding purine, which has resulted to nucleoside linear [ 4- ( 2-amino-6-chloro-purin-9-yl ) -cyclopent-2-enyl ] methanol ( VI ) .Abacavir will be produced by replacing of chloride with cyclopropyl aminoalkane in this purine karyon with refluxing butyl alcohol. to corroborate the construction of the Abacavir 1H NMR method and elemental analysis can be used. ( manufactur )

Environmental impact:

The stuff contains a pharmaceutical active ingredient that that is soluble in the H2O and chemically stable in H2O. more of all time, if it is straight into environment it is non likely to be absorbed in dirt or deposit and sludge or biomass farther more it is besides improbable to undergo the exposure debasement in Visible Spectrum 285 nanometer at pH 7due to this grounds it may consequence the Aquatic life, in the trial they made for toxicity it shows that it is toxic for Alga how of all time it did non demo toxicity in Daphnides and Fishes, when released in the environment.

The stuff is inherently biodegradable and is non expected to be prevailing in environment and the per centum of debasement is 96 % in 2 yearss. Further more this stuff dosage non enters the nutrient concatenation. ( environment )

The direct release of the stuffs might be harm full due to the pharmaceutical active ingredients that it has. To restrict the release of the stuffs to environment appropriate safeguards must be taken into history. ( environment ) unluckily no detoxification processs had been identified for this merchandise. .

Transportation system of the drug:

Harmonizing to UN Classification and Labeling, there is no restriction in Transportation and transportation of this drug. In transit it dose non necessitate any particular packaging or labeling for air. ( environment )

Selling and blessing of the drug:

Abacavir was foremost developed by GlaxoSmithKline ( GSK ) which is the largest maker of HIV medicines ( manbah GSK ) and has been approved for selling by FDA on 1988 in America ( Hughes et al. , 2004 ) and in Europe it received the full blessing in 1999. To understand the ABC HSR, ( GSK ) had agreed to carry on a post-approval research. In this cost decrease Ziagen unwritten solution ( abacavir ) had the most important decrease in monetary value. Factors that made it possible for GSK to cut down its monetary values are:

industry betterment and supply

decrease in cost of natural stuffs to bring forth these medical specialties

Drug name

Date of blessing

FDA Application No

Company

Selling position

ZIAGEN ( Brand Name Drug )

December 17, 1998

( NDA ) 020977

VIIV HLTHCARE

Prescription

ZIAGEN ( Brand Name Drug )

December 17, 1998

( NDA ) 020978

VIIV HLTHCARE

Prescription

Cost:

Since 1997 GSK company had reduced it monetary values for HIV medical specialties 5 times as portion of open uping discriminatory, in the last decrease which was in February 2008 GSK had decreased the monetary value of the HIV drugs. ( Price )

Drug name

GSK current $ per battalion

New monetary value

Percentage alteration

New Price per twenty-four hours $ *

Ziagen 300mg tablet

52.29

35.91

– 31.3 %

1.20

Ziagen Syrup 20mg/ml

25.00

15.08

– 39.7 %

0.50

GSK is the lone manufacturer of Abacavir and has non given any licences to generic

Manufacturers to bring forth it. ( TAC ) in 2002 a jurisprudence suit was held against the company by AIDS Healthcare Foundation ( AHF ) , they claimed that the company had monopolisation the fabrication of Abacvir in this manner it exclude competition in the market and the high rate of the monetary values of the drug. ( jurisprudence suit )

Patent:

Abacavir with the trade name name of Ziagen, the discoverer of the drug are research workers from University of Minnesota with the fiscal support from the US authorities. Burroughs Wellcome holds the cardinal usage patent, the company selling it is GSK. The blessing of this drug from US FDA was at 17-Dec-98, the Exclusivity of it expired in Dec 17, 2003 to Jun 17, 2004. The patent figure was EP 0434450A ( A2 ) discoverer DALUGE SUSAN MARY [ US ] and had expired at Jun 26, 2009 to Dec 26, 2009. ( Patent ) .

Decision:

ACHENBACH, C. , SCARSI, K. & A ; MURPHY, R. 2010. Abacavir/lamivudine fixed-dose combination antiretroviral therapy for the intervention of HIV. Progresss in Therapy, 27, 1-16.

CLAY, P. G. 2002. The abacavir hypersensitivity reaction: A reappraisal. Clinical Therapeuticss, 24, 1502-1514.

DE CLERCQ, E. 2009. The history of antiretrovirals: cardinal finds over the past 25 old ages. Review in Medical Virology, 19, 287-299.

FRANCIS, T. 2002. drug design and find In: POVL KROGSGAARD-LARSEN, T. L. , ULF MADSEN ( ed. ) 3rd ed erectile dysfunction. London.

HUGHES, D. A. , VILAR, F. J. , WARD, C. C. , ALFIREVIC, A. , PARK, B. K. & A ; PIRMOHAMED, M. 2004. Cost-effectiveness analysis of HLA B*5701 genotyping in forestalling abacavir hypersensitivity. Pharmacogeneticss and Genomics, 14, 335-342.

KOHLER, J. , HOSSEINI, S. , GREEN, E. , FIELDS, E. , ABUIN, A. , LUDAWAY, T. , RUSS, R. & A ; LEWIS, W. 2010. Absence of Mitochondrial Toxicity in Hearts of Transgenic Mice Treated with Abacavir. Cardiovascular Toxicology, 10, 146-151.

Cite this Abacavir With The Trade Name Of Ziagen Biology

Abacavir With The Trade Name Of Ziagen Biology. (2017, Jul 09). Retrieved from https://graduateway.com/abacavir-with-the-trade-name-of-ziagen-biology-essay/

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