Pilocarpine dosing

The development of two soluble gels for the delivery of pilocarpine has been reported. One of these systems, described as a high viscosity acrylic vehicle, delivers a 24 h pilocarpine dose from a single, night-time placement in the cul-de-sac. ... 

Cardiovascular disease Patients with significant cardiovascular disease may be unable to compensate for transient changes in hemodynamics or rhythm induced by pilocarpine. Pulmonary edema has been reported as a complication of pilocarpine toxicity from high ocular doses given for acute angle-closure glaucoma. Administer... 

The dose-related cardiovascular effects of pilocarpine include hypotension, hypertension, bradycardia, and tachycardia. 

Methacholine, bethanechol, and pilocarpine are selective agonists of muscarinic receptors, whereas carbachol and ACh can activate both muscarinic and nicotinic receptors. However, at usual therapeutic doses, the effects of carbachol and ACh are entirely due to the activation of muscarinic receptors. This apparent preference for muscarinic receptors can be attributed to the greater accessibility and abundance of these cholinoreceptors compared with the nicotinic receptors. 

Radioprotective effect. Rice seeds of cul-tivars Katakutara and Kusabue, kept in the seed hull and irradiated with y-radiation, showed greater germination than those that had been dehulled and irradiated ° . Salivary secretion. Decoction of the grain, administered intraperitoneally to mice at a dose of 100 mg/kg, was inactive vs pilocarpine-induced salivary flow in streptozo-tocin-diabetic mice " . ... 

The dramatic antagonism of limbic seizures by intracerebroventricularly administered inositol is a useful paradigm to study the time-course and dose response of behavioral effects of inositol. We injected rats with Li and 10 mg of inositol intracerebroventricularly at different time intervals before the subcutaneous injection of pilocarpine. Inositol was effective at 1, 4, and 8 hours before pilocarpine administration. When injected immediately before or 24 hours before pilocarpine injection, inositol did not prevent seizures in any rat when injected 12 hours before pilocarpine, 50% of rats had seizures. This time-course suggests that inositol must have time to distribute within the brain and to enter cells and that it is extruded from the brain or metabolized within 8-24 hours after injection. This time-course is long enough that therapeutic use of inositol seemed possible (Bersudsky et al. 1993b). 

Bersudsky Y, Vinnitsky 1, Grisaru N, et al Dose-response and time-curve of inositol prevention of Li-pilocarpine seizures. Eur Neuropsychopharmacol 2 428-429,... 

Pilocarpine when given IV increases the flow from salivary gland and other exocrine glands. Bronchial smooth muscle and intestinal smooth muscle contract. Small doses generally cause fall in BP, but higher doses elicit rise in BP and tachycardia (which is due to ganglionic stimulation). 

Vandamme and Brobeck [97] studied the residence time as well as the miotic and mydriatic effect of different generations of fluorescein, pilocarpine nitrate, and tropicamide-loaded PAMAM, respectively. A single dose of 25 pL of drug-loaded dendrimer solution was applied each time on the conjunctival sac of albino rabbit eye. PAMAM dendrimeric solutions... 

Figure 12.7 The Ocusert pilocarpine system is a thin multilayer membrane device. The central sandwich consists of a core containing the drug pilocarpine. The device is placed in the eye, where it releases the drug at a continuous rate for 7 days. Devices with release rates of 20 or 40 p,g/h are used. Controlled release of the drug eliminates the over- and under-dosing observed with conventional eyedrop formulations, which must be delivered every 4-6 h to maintain therapeutic levels of the drug in the eye tissue [18]...

Drugs (e.g., pilocarpine) that cause rapid lacrimation by stinging or by stimulation of lacrimal glands in normal individuals are formulated at high concentration to offset the dilution and washout that occur from tear flow. Patients with dry eyes that do not tear readily can absorb greatly exaggerated doses of topically applied medications. In children, who cry and lacrimate more easily than do adults, rapid drug washout can prevent adequate absorption of topically applied medications. 

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