Ketotifen

Chemical Name 4-(1 -Methyl-4-piperidylidene)-4H-benzo[4,5]cyclohepta[ 1,2-b] -thiophen-lO(9H)-one 

Trada Nama Manufacturer Country Year Introduced 

10-Methoxy-4H-ben2o[4.5] cyclohepta[1.2-b] thiophen-4-one Hydrogen chloride 

The chloroform solution is concentrated and the residue recry stall i2ed from 270 cc of absolute ethanol. The pure 10-methoxy-4-(1 -methyl-4-piperldyl)-4H-ben2o[4,5] cyclohepta[1,2-b] -thiophen-4-ol base, having a melting point of 194°C to 196°C, is obtained in this manner. Microanalysis corresponds with the formula Q20H23NO2S. 

Amixture of 3.4 gof 10-methoxy-4-(1 -methyl-4-piperidyl)-4H-ben2o[4,5]cyclohepta[1,2-b]-thiophen-4-ol base and 40 cc of 3 N hydrochloric acid is kept in a boiling water bath at 95°C to 100°C for 1 hour. The mixture is subsequently made alkaline with concentrated caustic soda solution at 20°C while cooling, and the free base Is extracted with chloroform. The chloroform solution is concentrated, and the residue is recrystalli2ed from ethanol/water 1 1. The pure 4-(1 -methyl-4-piperldylidene)-4H-ben2o[4,5]cyclohepta[1,2-b] thiophen-10(9H)-one base, having a melting point of 152°C to 153°C, is obtained in this manner. 

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Other Pharmaceuticals. Other pharmaceutical products incorporating the thiophene ring include the antiasthmatic dmg Ketotifen [34580-13-7] (Sandoz) (53), which is particularly marketed in Japan. The antifungal dmg Tioconazole [65899-73-2] (Pfizer) (54) is based on... 

Zactane - Ethoheptazine Zactipar- Ethoheptazine Zactirin - Ethoheptazine Zaditen Ketoprofen Zaditen Ketotifen... 

CI HzoBrNOS 59776-37-3) see Ketotifen 9a-bromo-16p-methylprednlsolone 21-acetate (Cj4H, BrO 4735-65-3) see Betamethasone... 

C 9H,2N0S 34580-09-1) see Ketotifen 4,9-dihydro-4-(l-methyl-4-piperidinylidene)-10/f-benzo [4,5]cyclohepta l,2-l>)thiophen-10-one (C19H19NOS 34580-13-7) see Ketotifen... 

C24H2 N2S 59743-86-1) see Ketotifen l-methyl-4-[9-(l-piperidinyl)-4W-benzo[4,5]cyclohepta-[l,2-Ii]thien-4-ylidene]piperidine (C24H2 N2S 5974i-S5-0) see Ketotifen... 

C21H23NO 3967-32-6) see Cyproheptadine l-methylpiperidin-4-ylmagnesium chloride (CfiH 2ClMgN 63463-36-5) see Azatadine Cyproheptadine Ketotifen Loratadine Pizotifen... 

Ketotifen Hrreceptor antagonist, mast cell stabilizer, eosinophil inhibitor, platelet-activating factor inhibitor May inhibit eosinophil chemotaxis... 

Ketotifen 1 drop in affected eye(s) twice daily Red eyes (conjunctival injection), headache... 

Recently, NGF has been shown to cause a significant proliferation of connective tissue mast cells when injected subcutaneously into newborn (day 1) rats [122]. This effect of NGF is blocked by DSCG, which suggests that products released from NGF-stimulated mast cells are responsible (directly or indirectly) for the proliferation or recruitment of other mast cells. In adult rats, a similar proliferation of mucosal mast cells in the small intestine is known to accompany an infection by intestinal nematode, N. brasilensis [123] and has also been reported to accompany the repeated injections of compound 48/80 [ 124], It may be relevant in this regard that mast cells are frequently prominent in a wide variety of fibrotic conditions such as neurofibromatosis where itching around the growing neurofibroma is a common symptom [125]. Treatment of neurofibromatosis with ketotifen, a mast cell stabilizer similar to DSCG, results... 

Zaditen syrup contains ketotifen, an antihistamine that may cause drowsiness. Patients are therefore advised not to drive or operate machinery. 

Inhibitors of histamine release One of the effects of the so-called mast cell stabilizers cromoglycate (cromolyn) and nedocromil is to decrease the release of histamine from mast cells (p. 72, 326). Both agents are applied topically. Release of mast cell mediators can also be inhibited by some Hi antihistamines, e.g., oxatomide and ketotifen, which are used systemically. 

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