Pilocarpine HCl Research Articles

Pilocarpine HCl for treatment of salivary gland hypofunction in primary Sjogren's syndrome: [formula omitted], Jane C. Atkinson, Alice A. Macynski, and Bruce J. Baum. CIPCB, NIDR, NIH, Bethesda, MD USA

Pilocarpine HCl for treatment of salivary gland hypofunction in primary Sjogren's syndrome: [formula omitted], Jane C. Atkinson, Alice A. Macynski, and Bruce J. Baum. CIPCB, NIDR, NIH, Bethesda, MD USA

Influence of some preservatives on the corneal permeability of pilocarpine and dexamethasone, in vitro

The influence of some commonly used preservatives on the corneal permeability and uptake of pilocarpine and dexamethasone were investigated in vitro. Isolated corneas were exposed to benzalkonium chloride (0.01%), chlorobutanol (0.5%), metagin (0.04%) + propagin (0.02%), and chlorhexidine digluconate (0.01%), all in clinically used concentrations, for 4 h at 35 °C. Benzalkonium chloride and chlorobutanol significantly increased the uptake and permeability of the two drugs. The influence of the parabens was of lower magnitude and the effect of chlorhexidine digluconate resulted in small or insignificant changes of the studied parameters. The barrier function of the corneal epithelium was strong. Both drugs showed a significant increase in permeability and uptake when de-epithelized corneas were used. Abrasion of the epithelium or preservatives showed a more pronounced influence on the corneal permeability and uptake for dexamethasone than pilocarpine HCl.

Permeability of phenylephrine hydrochloride. Its related compounds, and pilocarpine hydrochloride across bovine eye-lens capsule (author's transl)

Membrane potentials and membrane permeability coefficients of bovine eye-lens capsule and cellulose membrane were measured for L-phenylephrine HCl (mydriatic), its related compounds [DL-phenylpropanolamine HCl, and phenethylamine HCl] as well as pilocarpine HCl (myotic) and sodium chloride. It has been found that there is fairly strong interaction between phenylephrine cation and capsule, and also that pilocarpine HCl makes capsule more porous, so that its permeability coefficient across the capsule becomes large compared to other substances.

Mydriasis from Topically Administered Phenylephrine HCl Powder

Microgram amounts of finely powdered phenylephrine HCl were administered to the conjunctiva of volunteers. A dose-response curve for white subjects showed a threshold mydriasis of less than 5 micrograms and a clinically useful mydriasis was obtained with one application of 50 micrograms. The time-response curve for the one time use of 50 micrograms of the powder was equivalent to giving three applications of 10% phenylephrine HCl drops. Twenty-five micrograms of pilocarpine HCl powder produced marked miosis. We investigated methods to deliver nonirritating microgram amounts of powdered phenylephrine HCl, pilocarpine HCl, and fluorescein.

Reduced cell proliferation in fetal lung after maternal administration of pilocarpine: a scintillation autoradiographic study.

Fetuses were obtained on the 28th gestational day from pregnant New Zealand white rabbits treated daily, on the 24th through the 27th gestational day, with pilocarpine HCl, 5 mg/kg in saline, or saline alone. Lung fragments from these fetuses were incubated for two hours in medium containing 3H-thymidine. Scintillation autoradiography of 1-micrometer-thick sections of these fetal lungs revealed that the lung tissue from pilocarpine-treated fetuses had significantly lower labelled cell indices for both alveolar epithelial cells and interstitial cells. These results indicate that pilocarpine treatment promotes differentiation of immature cells in the fetal lung at the expense of cell proliferation.

Transcorneal Flux of Topical Pilocarpine to the Human Aqueous

Aqueous fluid was withdrawn from eyes of patients undergoing cataract extraction at various intervals after administration of two drops of 2% pilocarpine HCl in a standard manner. Determination of aqueous pilocarpine concentration was made both by spectroscopy of a ferric hydroxylamine complex and by gas-liquid chromatography. Results of both methods were consistent in indicating that concentration does not rise at any time following such topical instillation beyond 5 microgram/ml, with an average of 1.67 microgram/ml, representing a flux efficiency of 0.03%. These findings correlate well with previous investigations of transcorneal flux of pilocarpine for the rabbit in a transport chamber system, in which comparable low flux efficiency was found after simulated drop administration. This serves in some measure to validate an extrapolation of other findings in chamber experiments to the living human eye.

A modified ion-selective electrode method for measurement of chloride in sweat.

A modified method of analysis of sweat chloride concentration with an ion-selective electrode is presented. The original method of sweat chloride analysis proposed by the Orion Research Corporation (Cambridge, Massachusetts 02139) is inadequate because it produces erratic and misleading results. The modified method was compared with the reference quantitative method of Gibson and Cooke. In the modified method, individual electrode pads are cut and placed in the electrodes rather than using the pads supplied by the company; pilocarpine nitrate (2,000 mg/l) is used in place of pilocarpine HCl (640 mg/l); sodium bicarbonate as the weak electrolyte is used instead of K2SO4. A 10-minute period for sweat accumulation is employed rather than a zero-time collection as in the original Orion method. The modification has been studied for reproducibility in individuals, reproducibility between right and left arm in individuals; it has been compared extensively with the quantitative method of Gibson and Cooke, both in normal individuals and in patients with cystic fibrosis. There is excellent agreement between the modified method and the quantitative reference method. There appears to be a slight bias toward higher concentrations of chloride from the right arm compared with the left arm, but this difference is not medically significant.

Neural regulation of product discharge from the hedonic glands of the red‐spotted newt, Notopthalmus viridescens

AbstractThe mechanism whereby secretory product is extruded from the lumina of hedonic glands in the red‐spotted newt has been investigated and the chemical nature of that product has been examined. The ultrastructure of the myoepithelium has been studied. Endings of unmyelinated axons, containing both clear and dense‐cored synaptic vesicles, were seen to lie between the myoepithelium and the secretory epithelium, occasionally touching on the myoepithelial cells. Mean luminal diameters of hedonic glands in explants incubated in solutions of acetyl choline decreased by 58% of control values while those of explants incubated in solutions of epinephrine remained the same. Preincubation in the muscarinic blocking agent atropine sulfate, but not in nicotinic blocking agent d‐tubocurarine chloride, prevented the cholinergic response. Two PAS (+) bands were present in polyacrylamide gels prepared from secretions discharged by hedonic glands after treatment of male newts in breeding conformation with pilocarpine HCL and also in gels from skin samples containing mucous glands, but were absent from hedonic secretions of laboratory conditioned males. A smaller but similar band from hedonic glands of breeding females correlated with one of the two. Since hedonic glands, but not mucous glands, from breeding newts of both sexes incorporated 35SO4 into their product, bands from hedonic glands could be distinguished from those of mucous glands in gels. It is concluded that the product of hedonic glands is a sulfated mucin that is discharged in response to cholinergic stimulation of muscarinic receptors in myoepithelial cells.

Further evidence for cholinergic control of gonadotropin and prolactin secretion.

SummaryOvariectomized adult rats were injected with 10 μg of estradiol benzoate sc and 48 hr later with cholinergic drugs sc between 8:30 and 9:30 AM. Either pilocarpine HCl (5 or 50 mg/kg body wei...

Effect of hypercalcemia on salivary secretion in the dog.

An attempt was made to ascertain the effects of an elevated serum calcium level on the rate of secretion and on the movement of sodium, potassium, chloride, bicarbonate, and calcium ions across gland cell membranes in the parotid and mixed glands of three chronic fistulous dogs. Pilocarpine HCl (.36 mg/kg) was injected intravenously to prime secretion and 45 min after the injection of pilocarpine, in the experimental studies, 5–10 ml of calcium gluconate was injected intravenously. Saliva was collected at 15-min intervals for 45 min after the calcium gluconate injection. An increase in the volume secreted, outputs, and concentrations of the ions were noted for the mixed glands during the first 15-min postcalcium injection. During the second 15-min postcalcium, the volumes secreted were significantly below control levels for both the parotid and the mixed gland preparations. Calcium output during the second 15-min postcalcium was decreased in comparison to control values for the parotid glands.