Dipivefrine

Acylation of ami noketone 8 with the acid chloride from p-toluic acid affords the corresponding ester (10) catalytic hydrogenation leads to the bronchodilator bitolerol (11). An analogous scheme starting from the N-methyl ketone (12) and pivaloyl chloride gives ami noalcohol (14). This compound is then resolved to isolate the levorotatory isomer. There is thus obtained the drug dipivefrin. 

CjHgClO 3282-30-2) see Cefazolin Ceftezole Dexamethasone pivalate Dipivefrine Efavirenz ... 

Dipivefrin Prodrug Propine Solution 0.1 1 drop twice a day Increased aqueous... 

Pilocarpine and dipivefrin, a prodrug of epinephrine, are used as third-line therapies because of adverse events or reduced efficacy as compared with newer agents. 

Pharmacology Dipivefrin is a prodrug of epinephrine. Dipivefrin, converted to epinephrine in the eye by enzymatic hydrolysis, appears to act by decreasing aqueous production and enhancing outflow facility. It has the same therapeutic effects as epinephrine with fewer local and systemic side effects. 

Hypersensitivity to dipivefrin or any formulation component narrow-angle glaucoma. 

Ocupress Ophthalmic) Dipivefrin (Propine) Dorzolamide (Trusopt)... 

Partition coefficient ofun-ionised compound at acidic pH Octanol/water ca 631. Other drugs containing phenolic ester group metipranolol, vitamin E, benorylate, dipivefrin. 

GC provides a useful technique for estimating volatile degradation products. For example the pivalic acid release from the hydrolysis of dipivefrin in an eyedrop preparation (Fig. 11.19) used for treating glaucoma may be estimated by GC. Isovaleric acid, which is an isomer of pivalic acid, provides a suitable internal standard. Breakdown products of esters are more likely to occur in aqueous formulations such as eyedrops or injections. 

Pharmacokinetics Onset of action occurs within 30 min and peak effect in 1 hr. Dipivefrin is more lipophilic than epinephrine. Distributed to cornea. Dipivefrin is converted to epinephrine inside the eye by enzyme hydrolysis. 

Contraindications Narrow-angle glaucoma, hypersensitivi ty to dipivefrin or any component of the formulation... 

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