Active Pharmaceutical Ingredients 1

Product Details:

Erythromycin Stearate is a macrolide, acid labile compound derived from Erythromcyin. Erythromycin is a potent macrolide inhibitor of CYP3A4 with anti-inflammatory and prokinetic properties. Macrolides belong to a group of antibiotics that bind to the 50S ribosomal subunit and inhibit protein synthesis. Mouse studies show Erythromycin Stearate increases IL-1 and IL-2 levels.

Synonyms:

• oe7; Wemid; ethril; erypar; Ethryn; eratrex; meberyt; Eryprim; pfizer-e; qidmycin

 

IUPAC Name:

• 11-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-5-ethyl-3,4,12-trihydroxy-9-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-2,4,8,10,12,14-hexamethyl-6-oxacyclotetradecane-1,7-dione; octadecanoic acid

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Domperidone is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.

Synonyms:

• Evoxin; kw-5338; Euciton; Peridon; Peridys; R-33812; MOTILIUM; Nauzelin; Gastronorm; Moperidone

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A white or almost white powder

Synonyms:

• Domperidone Maleate; 5-Chloro-1-[1-[3-(2-Oxo-1,3-Dihydrobenzoimidazol-1-Yl)Propyl]-4-Piperidyl]-1, 3-Dihydrobenzoimidazol-2-One Maleate; 5-Chloro-1-[1-[3-(2-Oxo-1, 3-Dihydrobenzoimidazol-1-Yl)Propyl]-4-Piperidyl]-1, 3-Dihydrobenzoimidazol-2-One Maleate;2H-Benzimidazol-2-One, 5-Chloro-1-(1-(3-(2,3-Dihydro-2-Oxo-1H-Benzimidazol-1-Yl)Propyl)-4-Piperidinyl)-1, 3-Dihydro-, (Z)-2-Butenedioate

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White crystalline powder

Synonyms:

• 2,3-Dihydro-5, 6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]-1H-inden-1-one; 2-(1-Benzyl-4-piperidylmethyl)-5, 6-dimethoxy-1-indanone Hydrochloride

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Off white crystalline powder, can occur in mild hydrochloric acid smell, melts at about 240˚C, with decomposition

Synonyms:

• 2-(3,4-Dihydroxyphenyl)Ethyl-1-13C-Amine Hcl; 3,4-Dihydroxyphenyl-Ethylamine Hydrochloride; 3,4-Dihydroxyphenethylamine, Hcl; 4-(2-Aminoethyl)-1-2-Benzenedial Hydrochloride; 4-(2-Aminoethyl)Pyrocatechol Hydrochloride; 3-Hydroxytyraminium Chloride; Hydroxytyramine Hcl; Labotest-Bb Lt00233111

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White to off white odourless crystalline powder, Melts at about 220˚C

Synonyms:

• 3,3-Diphenyl-1-Ethyl-4-(2-Morpholinoethyl)-2-Pyrrolidinone Hydrochloride

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White, odorless powder. Very soluble in water and in alcohol, freely soluble in . Very slightly soluble in ether and in Benzene

Synonyms:

• Unisom; Hoggarn; Decapryn; Alsadorm; Gittalun; Sedaplus; Mereprine; Decapryn Succinate; Doxylaminesuccinat; Doxylamine Succinate

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Drotaverine Hydrochloride is an antispasmodic, and an analogue of Papaverine.

Synonyms:

• 1,2,3,4-Tetrahydro-6,7-diethoxy-1-((3,4-diethoxyphenyl) methylene)-isoquinoline hydrochloride

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Duloxetine HCl is used to treat major depression—a disorder marked by continuing, serious, and overwhelming feelings of depression that interfere with daily functioning. Symptoms may include major changes in appetite or sleep habits; lack of interest in social or work life; feelings of sadness, guilt, or worthlessness; fatigue; difficulty concentrating or making decisions; and suicidal thoughts or attempted suicide. Duloxetine HCl is also used to treat diabetic peripheral neuropathy, a painful nerve disorder associated with diabetes that affects the hands, legs, and feet. Duloxetine HCl is thought to work by correcting an imbalance of two brain chemicals known to influence mood—serotonin and norepinephrine. It belongs to a class of antidepressants called selective serotonin and norepinephrine reuptake inhibitors.

Synonyms:

• N-Methyl-gama-(1-naphthalenyloxy)-2-thiophenepropanamine

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Efavirenz (brand names and Stocrin®) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1.For HIV infection that has not previously been treated, efavirenz and lamivudine in combination with zidovudine or tenofovir is the preferred NNRTI-based regimen.Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to prevent HIV transmission for those exposed to materials associated with a high risk for HIV transmission.

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Entacapone is a selective, reversible catechol-O-methyl transferase (COMT) inhibitor for the treatment of Parkinson’s disease. It is a member of the class of nitrocatechols. When administered concomittantly with levodopa and a decarboxylase inhibitor (e.g., carbidopa), increased and more sustained plasma levodopa concentrations are reached as compared to the administration of levodopa and a decarboxylase inhibitor.

Synonyms:

• ENTACAPONE; 2-cyano-3-(5-dihydroxyamino-3, 4-dioxo-1-cyclohexa-1, 5-dienyl)-n,n-diethyl-prop-2-enamide; ENTACAPONE FS; OR-611;(2E)-2-Cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide; Comtan; Comtes; Comtess

 

Application:

• This compound belongs to the cinnamic acid amides. These are amides of cinnamic acids. Used as an adjunct to levodopa / carbidopa in the symptomatic treatment of patients with idiopathic Parkinson's Disease who experience the signs and symptoms of end-of-dose "wearing-off.

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Brownish Red Powder.

Synonyms:

• 2na; bromob; eosina; RED 22; Red A; bromo4d; bromofl; bromots; bromoxx; dawnred

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Erythromycin is a macrolide antibiotic produced by Streptomyces erythreus. It inhibits bacterial protein synthesis by binding to bacterial 50S ribosomal subunits; binding inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins. Erythromycin may be bacteriostatic or bactericidal depending on the organism and drug concentration.

Synonyms:

• (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-{[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy}-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione

Application:

• For use in the treatment of infections caused by susceptible strains of microorganisms in the following diseases: respiratory tract infections (upper and lower) of mild to moderate degree, pertussis (whooping cough), as adjunct to antitoxin in infections due to Corynebacterium diphtheriae, in the treatment of infections due to Corynebacterium minutissimum, intestinal amebiasis caused by Entamoeba histolytica, acute pelvic inflammatory disease caused by Neisseria gonorrhoeae, skin and soft tissue infections of mild to moderate severity caused by Streptococcus pyogenes and Staphylococcus aureus, primary syphilis caused by Treponema pallidum, infections caused by Chlamydia trachomatis, nongonococcal urethritis caused by Ureaplasma urealyticum, and Legionnaires' disease caused by Legionella pneumophila.

 

IUPAC Name:

• {[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy}- 14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)- 5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy}- 3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecane-2,10-dione

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Product Details:

Erythromycin Ethylsuccinate exhibits antibiotic properties.

Synonyms:

• Aids007905; Aids-007905;Erythromycin 2'-(Ethyl Succinate); 2'-(Ethyl Butanedioate)Erythromycin; Erythromycin 2'-(Ethyl Butanedioate); Erythromycin Ethyl Succinate - Bp/Ep/Usp 1264-62-6

 

IUPAC Name:

• [[(1R,2R,4R,6R,7R,8S,9R,12R,13S)-9-ethyl-2,7,8-trihydroxy-13-(5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl)oxy-2,4,6,8,12,14-hexamethyl-5,11-dioxo-10-oxacyclotetradec-1-yl]oxy]-6-methyloxan-3-yl] 4-O-ethyl butanedioate

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White or almost white, crystalline powder

Synonyms:

• (S)-1-[3-(Dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile oxalate

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White to off-white spherical pellets

Synonyms:

• Magnesium 5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]benzimidazol-1-ide, Esomeprazole Magnesium Pellets 7.5%, 8.5%, 10%, 15%, 20%, 22%, 22.5%

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Off white to pale yellow powder

Synonyms:

• 5-Methoxy-2-((S)-((4-methoxy-3,5-dimethyl-2-pyridyl)methyl)sulfinyl-1H-benzimidazole sodium sal

 

Application:

• For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastroinetestinal bleeds with NSAID use.

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An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect.

Synonyms:

• (2S,2'S)-2,2'-(Ethylenediimino)dibutan-1-ol dihydrochloride

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Ethamsylate (dicynene) is a haemostatic drug.It is believed to work by increasing capillary endothelial resistance and promoting platelet adhesion.It also inhibits biosynthesis and action of those prostaglandins which cause platelet disaggregation, vasodilation and increased capillary permeability.Indications: Prevention and treatment of capillary haemorrhages associated with (i) Haematemesis, melena, haemoptysis, haematuria, epitaxis (ii) menorrhagia, metrorrhagia, post-abortion and post-partum haemorrhages

Synonyms:

• Ethamsylate;diethylammonium 2,5-dihydroxybenzenesulphonate;2,5-dihydroxybenzenesulfonic acid - N-ethylethanamine (1:1)

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Etodolac is a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic properties. Its therapeutic effects are due to its ability to inhibit prostaglandin synthesis. It is indicated for relief of signs and symptoms of rheumatoid arthritis and osteoarthritis.

Synonyms:

• 1,8-Diethyl-1,3,4,9-Tetrahydropyrano[3,4-B]Indole-1-Acetic Acid

Application:

• For acute and long-term management of signs and symptoms of osteoarthritis and rheumatoid arthritis, as well as for the management of pain.

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Ezetimibe is an anti-hyperlipidemic medication which is used to lower cholesterol levels. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes.

Synonyms:

• ZETIA; Ezitimibe??? EzetimibeC24H21F2N03; (3R,4S)-1-(4-Fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-2-azetidinone, Sch-58235; 1-(4-Flurophenyl)-(3R)-3-(4-flurophenyl)-(3S)-hydroxypropyl-(4S)-(4-hydroxyphenyl)-2-azetidinone; Ezetimide; (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one

 

Application:

• For use as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia.

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Etoricoxib is a new COX-2 selective inhibitor. Current therapeutic indications are: treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout. Like any other COX-2 selective inhibitor, Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces the generation of prostaglandins (PGs) from arachidonic acid.

Synonyms:

• Algix; Etoxib; Etocox; MK 663; Tauxib; Etobrix; Arcoxia; Kingcox; MK 0663; Etropain

 

Application:

• For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.

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A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion. This compound belongs to the 2,4-disubstituted thiazoles. These are compounds containing a thiazole ring substituted at positions 2 and 4 only.

Synonyms:

• ganor; mk208; Ifada; gaster; motiax; muclox; pepcid; pepdul; peptan; fibonel

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Febuxostat belongs to a group of drugs known as xanthine oxidase (XO) inhibitors. It is used to reduce blood uric acid levels in patients with gout, a painful arthritic condition that mainly affects the big toe, but can also affect the ankles, heels, knees, elbows, wrists or fingers.Febuxostat is used in the treatment of gout patients with hyperuricemia, or high uric acid levels.The most common side effects of Uloric are liver problems,nausea,joint pain.

Synonyms:

• Fbx; Uloric; Tmx 67; Tei-6720; Febuxosta; Febuxostat; Febuxostat Api; Febuxostat Tablets; Febuxostat (Uloric); Febuxostat (Tei-6720)

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An antilipemic agent which reduces both cholesterol and triglycerides in the blood.

Synonyms:

• lf-178; lipsin; lipifen; lipidax; sedufen; LIPYDIL; Lipirex; Liposit; Nolipax; Secalip

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Fenticonazole Nitrate is an azole antifungal drug that inhibits CYP51A1 (14 α-demethylase) and ergosterol production. It shows active effects against Malassezia furfur and Candida albicans in vivo.

Synonyms:

• 1-[2-(2,4-dichlorophenyl)-2-[[4-(phenylthio)phenyl]methoxy]ethyl]-1H-imidazolium nitrate; Fenticonazol Nitrate; 1-[2-(2,4-Dichlorophenyl)-2-[(4-phenylsulfanylphenyl)methoxy]ethyl]imidazole nitrate; 1-[2-(2，4-Dichlorophenyl)-2-[[4-(phenylthio)phenyl]methoxy]ethyl]-1H- imidazole mononitrate; Falvin; Fentiderm; Fentigyn; Lomexin; Rec-15―1476; 1-[2-(2,4-dichlorophenyl)-2-{[4-(phenylsulfanyl)benzyl]oxy}ethyl]-1H-imidazole nitrate (1:1); 1-[2-(2,4-dichlorophenyl)-2-{[4-(phenylsulfanyl)benzyl]oxy}ethyl]-1H-imidazole

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Reddish Orange or Reddish Brown Powder

Synonyms:

• Fumaric acid ferrous salt, iron (II) fumarate

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Triazole antifungal agent that is used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS

Synonyms:

• Fluconazole Impurity C;Fluconazole Related Compound C;fluconazole related substance EP C; fluconazole related substance USP C;1,1'-(1,3-phenylene)di-1H-1,2,4-triazole;1,1'-(1,3-Phenylene)bis-1H-1,2,4-triazole

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Fluorescein sodium salt is a disodium salt of fluorescein and a noted pH sensitive fluorophore. Fluorescein sodium salt has been utilized in studies as a drug model, as a penetrating dye and also as a fluorescein tracer. Fluorescein sodium salt has also been used in vitro to quantify root dentin demineralization. Additional reported uses include microscopy, as a gain medium in dye laser use and to detect latent blood stains. Common derivatives of Fluorescein include fluorescein isothiocyanate (FITC), eosin and Rose Bengal (sc-296278) and Rose Bengal sodium salt (sc-203757)

Synonyms:

• Uranine; c.i.766;ful-glo; Uranine Fluorin; furanium; uranineo; F luorone; Yellow 8;S NO 880

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Fluoxetine is an ST (5-hydroxytryptamine/serotonin/5-HT reuptake) inhibitor. This is a racemic mixture and both R and S enantiomers which are reported to inhibit 5-HT uptake in synaptosomal preparations of rat cerebral cortex. Additionally, Fluoxetine is also noted to increase extracellular levels of 5-HT in several areas of the rat brain as a result of reuptake inhibition. This increase in availability of 5-HT is reported to lead to a decrease in synthesis and turnover of 5-HT.

Synonyms:

• Zepax; LY-110; PROZAC; SARAFEM; Alzac 20; Deproxin; DigassiM; PROZAC(R); LY-110140; Affectine

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Pale yellow, viscous liquid or yellow solid

Synonyms:

• 2-[4-[3-[2-(Trifluoromethyl)-10H-phenothiazin-10-yl]propyl]piperazin-1-yl]ethyl decanoate

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Fluticasone propionate, a medium-potency synthetic corticosteroid, is used topically to relieve inflammatory and pruritic symptoms of dermatoses and psoriasis, intranasally to manage symptoms of allergic and non-allergic rhinitis, and orally for the treatment of asthma. Fluticasone proprionate is marketed under several different brand names such as Flonase®. Fluticasone propionate is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista. Dymista is indicated in patients over 12 years old for symptomatic relief of seasonal allergic rhinitis.

Synonyms:

• S-Fluoromethyl-6Alpha,9Alpha-Difluoro-11Beta-Hydroxy-16Alpha-Methyl-3-Oxo-17Alpha-Propionyloxyandrosta-1,4-Diene-17Beta-Carbothioate;-17-(1-Oxopropoxy)-,S-(Fluoromethyl)Ester,(6-Alpha,11-Beta,16-Alpha,17-Alph;Androsta-1,4-Diene-17-Carbothioicacid,6,9-Difluoro-11-Hydroxy-16-Methyl-3-Oxo;Cci18781;Fluticasone17-Propionate;Flutide; (6A,11B,16A,17A)-6,9-Difluoro-11-Hydroxy-16-Methyl-3-Oxo-17-(1-Oxopropoxy)Androsta-1,4-Diene-17-Carbothioic Acid Fluoromethyl Ester; (6 Alpha,11 Beta,16 Alpha,17 Alpha)-6,9-Difluoro-11-Hydroxy-16-Methyl-3-Oxo-17-(1-Oxopropoxy)Androsta-1,4-Diene-17-Carbothioic Acid Fluoromethyl Ester

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Fluvoxamine maleate is a selective SR (serotonin reputake) inhibitor. Fluvoxamine is described to bind the human 5-HT transporter protein with high affinity (Ki = 1.6 nM) while demonstrating very low affinity at the norepinephrine transporter (Ki = 2,950 nM). Fluvoxamine maleate is a Sigma Receptor agonist.

Synonyms:

• Fluvoxamine Maleate; (E)-5-Methoxy-1-[4-(Trifluoromethyl)Phenyl]-1-Pentanone-O-(2-Aminoethyl)Oxime Maleate; 1-Pentanone,5-Methoxy-1-(4-(Trifluoromethyl)Phenyl)-,O-(2-Aminoethyl)Oxime,(;5-Methoxy-4-Trifluoromethylvalerophenone(E)-O-2-Aminoethyloximemonomaleate;Du23000;Faverin50; (E)-5-Methoxy-1-[4-(Trifluoromethyl)Phenyl]-O-(2-Aminoethyl)Oxime-1-Pentanone; Mk-264, Di-23000, Dumirox, Flaverrin, Fevarin, Floxyfral, Luvox, Maveral, (E)-5-Methoxy-1-[4-(Triflurormethyl)Phenyl]-1-Pentanone, Maleate

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Formoterol Fumarate is shown to be a potent β-AR adrenoceptor agonist, with a fast onset of effect on the isolated human bronchus model. This compound demonstrates a 330-fold selectivity for β2 over β1 receptors. Formoterol Fumarate has been reported to be 150-200 times more potent than isoprenaline. This agent has also been noted to reduce the loss of muscle mass in murine models.

Synonyms:

• Ym 08316; Cgp 25827A; Nsc 299587; Farmeterol; Aformoterol; Cgp-25827A-E; Formoterol Fumarate; Formaterol Fumatate; Formaterol Fumarate; Eformoterol Fumarate

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Prodrug of phenytoin that converts to the anticonvulsant, phenytoin, after parenteral administration. Thought to modulate the sodium channels of neurons, calcium flux across neuronal membranes, and enhance the sodium–potassium ATPase activity of neurons and glial cells. The cellular mechanism of phenytoin is thought to be responsible for the anticonvulsant activity of fosphenytoin. Control of generalized convulsive status epilepticus and the prevention and treatment of seizures during neurosurgery, or as a parenteral short-term substitute for oral phenytoin.

Synonyms:

• Ci 982; Cetebyx; Acc-9653; Fospenytoin; Acc 9653-010; Pro-Epanutin; Fosphenytion Sodium; Fosphenytoin Sodium; Fosphenytoin Sodium Usp; Fosphenytoin Disodium Salt

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A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for edema and chronic renal insufficiency. For the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome. Also for the treatment of hypertension alone or in combination with other antihypertensive agents.

Synonyms:

• 5-(aminosulfonyl)-4-chloro-2-((2-furanylmethyl)amino)benzoic acid; 4-chloro-n-furfuryl-5-sulfamoylanthranilic acid; 2-furfurylamino-4-chloro-5-sulfamoylbenzoic acid; Frusemide

 

Application:

• This compound belongs to the aminobenzenesulfonamides. These are organic compounds containing a benzenesulfonamide moiety with an amine group attached to the benzene ring.

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Sumatriptan succinate is a selective 5-HT1 receptor agonist with specificity towards 5-HT1D, 5-HT1B and 5-HT1A. In addition, the physicochemical properties of Sumatriptan succinate can be characterized using FT-IR, HPLC, SEM and XRD. It has been reported that Sumatriptan succinate can be produced via reactive precipitation without the presence of surfactants. Further studies show that molecules of Sumatriptan succinate are carried through cells using liposomes, with positively charged liposomes exhibiting the highest loading efficiency.

Synonyms:

• Gr43175C; Sumitrex; Sumatriptan Succinate; Methanesulfonamide(1:1); Sumatriptan Succinate, Ep;Sumatriptansuccinate(1:1); Sumatriptan Succinate (200 Mg); 3-[2-(Dimethylamino) Ethyl]-N-Methyl-1H-Indole-5-Methane Sulfonamide; Compd.With3-(2-(Dimethylamino)Ethyl)-N-Methyl-1H-Indole-5-Butanedioicaci; 3-[2-(Dimethylamino)Ethyl]-1H-Indol-5-Yl-N-Methylmethanesulfonamide Succinate

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Tamsuolosin Hydrochloride is an α1A-AR (α1-adrenoceptor) antagonist commonly used to treat benign prostatic hypertrophy. Tamsulosin hydrochloride has shown possible usefulness in suppressing central sympathetic hyperactivity in amyotrhophic lateral sclerosis Tamsulosin Hydrochloride is an inhibitor of α1B-AR.

Synonyms:

• Omic; Omnic; Pradif; Ym-617; Flomax; Harnal; Yutana; Yutanal; LY-253351; Ym-12617-1

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This drug is an eye medication that is used in dogs and cats to decrease the pressure in the eye. It is available in the form of drops.

Synonyms:

• Rac-trans Dorzolamide; 4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5, 6-dihydro-6-methyl-, 7,7-dioxide, monohydrochloride, trans-; 4H-Thieno[2,3-b]thiopyran-2-sulfonaMide,4-(ethylaMino)-5, 6-dihydro-6-Methyl-, 7, 7-dioxide, hydrochloride (1:1), (4R,6R)-rel

 

Application:

• Dorzolamide HCl Ophthalmic Solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

 

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acrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after organ transplant to reduce the activity of the patient’s immune system and so the risk of organ rejection. It is also used in a topical preparation in the treatment of severe atopic dermatitis, severe refractory uveitis after bone marrow transplants, and the skin condition vitiligo. It was discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus is chemically known as a macrolide. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription.

Synonyms:

• FK-506; prograf; fr900506; L 679934; Protopic; Advagraf; Fujimycin; TacroBell; TACROLIMUS; FK-506, 99+%

Application:

• For use after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.

IUPAC Name:

• (1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(1E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-(prop-2-en-1-yl)-11,28-dioxa-4-azatricyclo[22.3.1.0^{4,9}]octacos-18-ene-2,3,10,16-tetrone

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