Pilocarpine dosage

The Ocusert Pilo-20 and Pilo-40 Ocular Therapeutic System is an elliptical membrane that is soft and flexible and designed to be placed in the inferior cul-de-sac between the sclera and the eyelid and to release pilocarpine continuously at a steady rate for 7 days. The design of the dosage form is described by Alza in terms of an open-looped therapeutic system, having three major components (a) the drug, (b) a... 

Semisolid Dosage Forms The nature of the base (vehicle) used for the fabrication of semisolid dosage forms affects their hydrolytic stability. Increased degradation of benzylpenicillin sodium in hydrogels of various natural and semisynthetic polymers has been reported [14]. Also at pH 6 in Carbopol hydrogels, the percentage of undecomposed pilocarpine at equilibrium is a function of the apparent viscosity of the medium [15]. 

Loucas, S. P. and H. M. Haddad. 1972. Solid-state ophthalmic dosage systems in effecting prolonged release of pilocarpine in the cul-de-sad. Pharm. Sci61 985-986. 

Pilocarpine is commerciaUy available in a carbomer gel vehicle.The 4% pilocarpine gel is packaged in a 3-5-g tube similar to ophthalmic ointments. A practical advantage of this sustained delivery system is the once-daily dosage regimen, with the drug usuaUy administered at bedtime. Minor side effects include superficial corneal haze, which may occur after long-term use (>8 weeks), and superficial pimctate keratitis, which can affect almost one-half the treated patients but usually resolves spontaneously. 

The usual dosage of pilocarpine gel is a l inch ribbon applied in the lower conjunctival sac of the affected eye or eyes once a day at bedtime. Adverse events associated with the once-daily dosage of the 4% gel are not significantly different from those associated with fiaur-times-daily instillation of the 4% drops. 

Treatment of patients with reduced salivary flow should include the following (1) drug and dosage changes by the patient s physician in consultation with the patient s dentist (2) use of artificial saliva in a spray form (3) use of mouth moisturizers and lip balms (4) use of sugarless hard candy (5) frequent sipping of water (6) use of decaffeinated products (7) use of pilocarpine (Salagen) 3-5 x daily and (8) inclusion of citrus and pineapple flavors in the diet. 

Controlling the release of medication at the site of action is often desirable, especially for compounds that are absorbed rapidly through mucous membranes or are removed rapidly from the site of action. The approach normally reduces the systemic side effects of the agent. The application of this approach can be illustrated with the Progestasert and Pilocarpine Ocusert dosage forms. 

Pilocarpine is a drug commonly used in glaucoma therapy to relieve intraocular pressure (lOP), which is a cause of great discomfort to the patient. Piloplex is a sustained-release product based on an emulsion system of pilocarpine bound to a polymeric carrier [87,88]. Piloplex was shown to prolong a reduction in lOP as compared to standard pilocarpine hydrochloride drops. This is attributed to its bioadhesive properties, which keep the drug in the precorneal area longer than do conventional ocular dosage forms. 

S. P. Loucas and H. M. Haddad, Solid-State Ophthalmic Dosage Systems in Effecting Prolonged Release of Pilocarpine in the Cul-De-Sac, J. Pharm. Sci. 61 985 (1972). 

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