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PubMed1999

Sympathetic mediation of salivation induced by intracerebroventricular pilocarpine in rats.

Central cholinergic activation by pilocarpine induces salivation dependent on the integrity of forebrain areas. The present work investigates the autonomic mediation of this salivation. Pilocarpine (500 nmol/rat) was injected into the lateral ventricle (LV) of tribromoethanol-anesthetized adult male rats. Preweighed cotton balls were inserted into the oral cavity and weighed again 7 min later. Alpha-adrenoceptor antagonists (3-50 micromol/kg) prazosin (alpha1), yohimbine (alpha2) or propranolol (beta) injected intraperitoneally (i.p.) produced, 80%, 20% and 0% inhibition respectively of the LV pilocarpine-induced salivation. Intracerebroventricular injections (160 nmol) of the antagonists did not alter the effects of pilocarpine injected into the LV. Bilateral section of chorda tympani nerve or bilateral sympathetic cervical ganglionectomy produced 0% and 40% inhibition of pilocarpine-induced salivation, respectively. Ganglionectomy did not alter salivation induced by i.p. injection of pilocarpine (4 micromol/kg). The results indicate that there is a large sympathetic contribution to the salivation induced by central cholinergic activation.

Adrenergic Antagonists↗
PubMed2002

A randomized, double-blind, placebo-controlled trial of concomitant pilocarpine with head and neck irradiation for prevention of radiation-induced xerostomia.

BACKGROUND: Xerostomia is one of the disturbing side-effects of radiotherapy to the head and neck region. Pilocarpine has been approved for the treatment of this condition in the chronic phase, but its use concurrent with radiation could also be beneficial for prevention or reduction of the subsequent radiation-induced xerostomia. We undertook to test this hypothesis in a clinical trial. METHODS: At the start of radiotherapy, randomization was performed to either pilocarpine 5 mg three times daily or placebo in a double-blind setting. The drug was started with irradiation and continued until 3 months after the end of radiotherapy. Xerostomia was evaluated 6 months after the end of radiation by a subjective visual analog scale questionnaire. Also the objective grade of xerostomia was recorded by two separate observers. RESULTS: A total number of 60 patients were randomized into the trial, but unfortunately only 39 patients were finally evaluated for xerostomia, 18 in the pilocarpine and 21 in the placebo group. Mean age was 42 years, and mean parotid dose was 58 Gy. Mean subjective xerostomia was 40.3 mm in the pilocarpine group and 57 mm in the placebo group (P = 0.02). Also mean objective xerostomia grade was 2.2 in the pilocarpine group and 2.6 in the placebo group (P = 0.01). Subjective and objective xerostomia results were positively correlated (P = 0.01). Age and the parotid dose did not have a significant effect on xerostomia. CONCLUSIONS: Compared to placebo, pilocarpine used with radiotherapy could lead to a significant diminishment of subsequent radiation-induced xerostomia.

Administration, Oral↗
PubMedDate not supplied

[Usefulness of pilocarpine in the prevention of xerostomia in patients with head and neck cancer treated with radiotherapy. Assessment with gammagraphy and salivary flow].

AIM: To assess the utility of salivary gland scintigraphy and salivary flow to quantify salivary function and to evaluate the usefulness of pilocarpine in the treatment of radiation-induced xerestomia in head and neck cancer patients. METHOD: Thirty two patients with head and neck tumor treated with radiotherapy (RDT) were studied. Patients were classified into two groups: pilocarpine group (P), that received prophylactic pilocarpine before RDT and during the first year after treatment. No pilocarpine group (NP) that received RDT without pilocarpine. Salivary gland scintigraphy and salivary flow were performed before RDT and during one year after treatment. Parotid and submaxillary uptake and excretion were calculated. Salivary flow after stimulation during five minutes was also obtained. RESULTS: Uptake and excretion in both salivary glands decreased after RDT. There were no statistical differences comparing P and NP groups (p < 0.001). However, in group P a trend to recovery was observed in parotid uptake values at 12 months after treatment, but it was not statistically significant. In both groups the salivary flow decreased after RDT and a good correlation (r = 0.8) between salivary flow and submaxillary excretion and parotid excretion was found. CONCLUSIONS: Salivary gland scintigraphy and salivary flow could be useful to evaluate salivary gland function in patients with head and neck irradiated tumors. Although better results on the salivary uptake at 12 months were noted, pilocarpine did not significantly improve salivary gland function.

Adult↗
PubMed2002

A Phase III placebo-controlled trial of oral pilocarpine in patients undergoing radiotherapy for head-and-neck cancer.

PURPOSE: To test the hypothesis that the use of oral pilocarpine during and after radiotherapy (RT) for head-and-neck cancer would reduce the symptoms of post-RT xerostomia. METHODS AND MATERIALS: One hundred thirty patients were randomized in a double-blind method to receive either pilocarpine (5-mg tablets) or placebo three times daily starting on Day 1 of RT and continuing for 1 month after treatment. The eligibility criteria included a planned dose of >50 Gy as radical or postoperative RT for head-and-neck cancer, with at least 50% of both parotid glands included in the treatment fields. The primary outcome measure was the severity of xerostomia as assessed by a patient-completed linear analog scale 3 months after RT. Secondary outcome measures included quality of life during therapy (as assessed by the McMaster University Head-and-Neck Questionnaire) and severity of mucositis during RT (as assessed using Radiation Therapy Oncology Group scales). RESULTS: No difference was observed between the pilocarpine-treated patients and the placebo group in the severity of xerostomia score as assessed by linear analog scale at baseline and 1, 3, and 6 months after treatment (repeated measures analysis, p = 0.92). No difference was apparent in the severity of mucositis during RT; 56.3% of patients receiving pilocarpine had Grade III/IV mucositis compared with 50.8% treated with placebo. No difference in quality of life was noted between the treatment groups during or after RT. The questionnaire score at 3 months after RT was 5.0 (SD 1.0). in the pilocarpine group and 4.9 (SD 0.9) in the placebo group. CONCLUSION: We were unable to detect a beneficial effect of pilocarpine on RT-induced xerostomia when administered during RT for head-and-neck cancer.

Administration, Oral↗
PubMed1997

Influence of alpha-cyclodextrin and hydroxyalkylated beta-cyclodextrin derivatives on the in vitro corneal uptake and permeation of aqueous pilocarpine-HCl solutions.

Interactions in aqueous solution between pilocarpine hydrochloride (P-HCl), a rather hydrophilic drug with good water solubility, and various cyclodextrins (CDs) were described recently. To assess the influence of CDs on the diffusion behavior of pilocarpine, in vitro studies were performed using porcine or bovine corneas as diffusion barriers. The affinity of P-HCl for porcine cornea in the presence of alpha-cyclodextrin (alpha-CD) and (hydroxyethyl)-beta-cyclodextrin (HE-beta-CD) was determined by drug uptake experiments. Additionally, in vitro permeation experiments through bovine corneas were conducted with a modified diffusion device optimized for corneal perfusion studies. The results obtained from the corneal uptake studies indicate that the addition of alpha-CD led to increased tissue drug levels. The increase in permeability of pilocarpine in the presence of alpha-CD was approximately 10-fold (log Papp = -4.87 +/- 0.03) in comparison with plain P-HCl solution (log Papp = -5.89 +/- 0.06). Permeation studies with corneas pretreated with alpha-CD solution revealed enhanced corneal permeability of pilocarpine due to alpha-CD induced membrane effects. The hydroxyalkylated beta-CD derivatives HE-beta-CD (log Papp = -6.27 +/- 0.09) and (hydroxypropyl)-beta-cyclodextrin (HP-beta-CD; log Papp = -6.40 +/- 0.03), however, seemed to cause slightly decreased permeation rates, supporting the concept of an interaction between pilocarpine and the hydroxyalkylated-beta-CD derivatives. Considering physiological compatibility, the addition of CDs seems to be an effective tool to modify and optimize the ocular availability of pilocarpine.

Alkylation↗
PubMed1991

Improved corneal pilocarpine permeability with O,O'-(1,4-xylylene) bispilocarpic acid ester double prodrugs.

O,O'-(1,4-Xylylene) bispilocarpic acid esters are pilocarpine prodrugs containing two pilocarpic acid monoesters linked with one pro-moiety. Each mole of prodrug forms two pilocarpine moles in the presence of esterases. Corneal uptake and permeability of various bispilocarpic acid diesters were investigated in vitro using isolated albino rabbit corneas. The permeability coefficient of pilocarpine was 2.8 x 10(-6) cm/sec, whereas for bispilocarpic acid diesters, despite their large molecular weights (between 638 and 722), permeability coefficients were 6.5-20.2 x 10(-6) cm/sec. Only pilocarpine, and no intact prodrug, was observed at the endothelial side. Corneal uptake was increased with increasing lipophilicity, but a parabolic relationship between the logarithm of the apparent partition coefficient (1-octanol-pH 7.4 phosphate buffer) (log PC) and the corneal permeability was noticed. Corneal permeability and the rate of enzymatic hydrolysis of the compounds correlated well. The corneal permeability of pilocarpine given as lipophilic bispilocarpic acid diester (log PC greater than or equal to 3) prodrugs seems to be controlled by the formation of pilocarpine in the corneal epithelium rather than by the absorption of prodrugs into the epithelium or their epithelium-stroma transport rate.

Animals↗
PubMed1992

Pilocarpine disposition and salivary flow responses following intravenous administration to dogs.

Oral doses of pilocarpine increase salivary flow rates in patients afflicted with xerostomia (dry mouth). This study examined the pharmacokinetics of and a pharmacodynamic response (salivation) to intravenous pilocarpine nitrate administration in dogs. Disposition was linear over a dose range of 225-600 micrograms/kg; plasma concentrations were 10-120 micrograms/L. Elimination was rapid and generally biphasic, with a terminal elimination half-life of approximately 1.3 hr. The systemic clearance of pilocarpine was high (2.22 +/- 0.49 L/kg/hr) and its steady-state volume of distribution (2.30 +/- 0.64 L/kg) was comparable to that of many other basic drugs. All doses of pilocarpine induced measurable submaxillary and parotid salivary flow rates which could be maintained constant over time. Cumulative submaxillary saliva flow was linearly related to total pilocarpine dose. Plasma pilocarpine concentration was linearly related to both steady-state and postinfusion submaxillary salivary flow rates.

Animals↗
PubMed2003

Effects of pilocarpine hydrochloride and cevimeline on submandibular/sublingual salivation in rat xerostomia model produced by X-ray irradiation.

The present study was performed to assess the effects of pilocarpine hydrochloride ((3S,4R)-3-ethyl-dihydro-4-[(1-methyl-1H-imidazole-5-yl)methyl]-2(3H)-furanone monohydrochloride, CAS 54-71-7) and cevimeline ((+/-)-cis-2-methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride, hemihydrate, CAS 153504-70-2), muscarinic receptor agonists, on salivary secretion from the submandibular/sublingual (SM/SL) glands in normal rats and in rats with xerostomia induced by X-ray (15 Gy) irradiation. To clarify their pharmacological safety profiles, the two drugs were further compared with regard to subtype selectivity for muscarinic receptors (M1, M2, and M3) and central nervous, respiratory, and cardiovascular effects. Pilocarpine hydrochloride (0.1-0.8 mg/kg i.d.) and cevimeline (3-30 mg/kg i.d.) dose-dependently increased salivary flow rate and total salivary volume in a 120-min period from SM/SL glands in both normal and irradiated rats, the minimum effective doses for their sialagogic effects being 0.2 and 10 mg/kg, respectively. Both drugs also increased protein output from SM/SL glands to a degree that depended on the increase in salivary volume in normal and irradiated rats. In a binding study using radiolabeled antagonists, neither pilocarpine hydrochloride nor cevimeline displayed subtype selectivity for muscarinic receptors, indicating non-selective muscarinic agonism. Effects on the central nervous system (CNS) were assessed by monitoring changes in body temperature in conscious normal rats. Pilocarpine hydrochloride (0.4-4 mg/kg p.o.) had no effect on body temperature, but cevimeline (30 and 100 mg/kg p.o.) caused a significant hypothermia. In terms of respiratory and cardiovascular effects in anesthetized normal rats, there was no clear difference in safety margin between pilocarpine hydrochloride and cevimeline, both drugs inducing significant changes in respiratory rate, heart rate, and blood pressure at doses close to those inducing sialagogic effects. These results suggest that pilocarpine hydrochloride could be used as a sialagogic drug for postirradiation-induced xerostomia with fewer adverse effects on the CNS.

Animals↗
PubMed1984

[Drug therapy of chronic glaucoma with pilocarpine gel].

In an open clinical trial including 19 patients with chronic open-angle glaucoma, the efficacy, duration of action and tolerance of pilocarpine gel were investigated over a treatment period of a 4 weeks on the basis of one application once a day. The vehicle of pilocarpine gel is a highly viscous, cross-linked, hydrophilic polyacrylic acid which renders prolonged release of pilocarpine hydrochloride 4%, and for this reason insures a prolonged duration of action. After single-dose application pilocarpine gel caused a significant lowering of IOP over at least 18 hours, with a relative potency in the range of 23% of 31% on the first day of treatment, and between 13% and 25% on the 29th day of treatment. As the time interval following the preceding pilocarpine-gel application increased, there was a slight but significant rise in the treated pressure level, although therapeutic pressure levels were not exceeded. In the course of the 4 weeks of treatment, there was a small but significant decrease in response, which can be explained by a certain type of subsensitivity caused by the prolonged release of the active drug. The tolerance of pilocarpine gel was good; side-effects were minor and reversible. These results fulfill the expectations of the glaucoma therapists with respect to both efficacy and tolerance.

Acrylic Resins↗
PubMed1993

Oral pilocarpine for post-irradiation xerostomia in patients with head and neck cancer.

BACKGROUND AND METHODS: We evaluated pilocarpine hydrochloride for the treatment of radiation-induced xerostomia, a common complication of irradiation of the head and neck. A prospective, randomized, double-blind, placebo-controlled trial was undertaken to test the safety and efficacy of pilocarpine, particularly in reversing the decrease in the production of saliva and other manifestations of xerostomia. Patients received either placebo or pilocarpine (5 mg or 10 mg orally three times a day) for 12 weeks and were evaluated at base line and every 4 weeks. RESULTS: We studied 207 patients who had each received > or = 4000 cGy of radiation to the head and neck. In the patients receiving the 5-mg dose of pilocarpine, oral dryness improved in 44 percent, as compared with 25 percent of the patients receiving placebo (P = 0.027). There was overall improvement in 54 percent of the 5-mg group as compared with 25 percent of the placebo group (P = 0.003), and 31 percent of the 5-mg group had improved comfort of the mouth and tongue, as compared with 10 percent of the placebo group (P = 0.002). Speaking ability improved in 33 percent of the 5-mg group as compared with 18 percent of the placebo group (P = 0.037). Saliva production was improved, but it did not correlate with symptomatic relief. There were comparable improvements in the group receiving the 10-mg dose. The primary adverse effect was sweating, in addition to other minor cholinergic effects. Six and 29 percent of the patients in the 5-mg and 10-mg groups, respectively, withdrew from the study because of adverse effects. There were no serious adverse effects related to pilocarpine. CONCLUSIONS: Pilocarpine improved saliva production and relieved symptoms of xerostomia after irradiation for cancer of the head and neck, with minor side effects that were predominantly limited to sweating.

Administration, Oral↗
PubMedDate not supplied

In vivo evaluation of submicron emulsions with pilocarpine: the effect of pH and chemical form of the drug.

Submicron emulsions containing 2.0% w/v pilocarpine as pilocarpine HCl, soybean oil (10% w/v) and egg lecithin (1.2% w/v) were formulated. Emulsions at pH 5.0, 6.5 and 8.5 were applied to the rabbit's eye, and the reduction in pupil diameter was measured for 6 h. The miotic effect was compared with that obtained with aqueous solutions at the same pH. A prolonged miotic effect was observed when the submicron emulsion was used as a vehicle. After application of emulsions at pH 5.0, 6.5 or 8.5, the time when 20% reduction of pupil diameter was still observed was 3.9 +/- 1.1 h, 4.3 +/- 1.3 h and 5.3 +/- 0.8 h, respectively, while, after application of a solution, this parameter was shorter by 30-40%. AUC(0-6h) values were larger after application of the submicron emulsions in comparison to aqueous solutions; however, statistically significant differences were only observed for emulsions at pH 6.5. Although the bioavailability of the drug is pH dependent, emulsions at higher pH cannot be considered for clinical use because of pilocarpine degradation which occurs with a similar rate as in aqueous solutions. Introduction of pilocarpine into the oily phase in the form of pilocarpine base or its oleate did not improve either the physicochemical or the pharmacological properties of the formulations. Irrespective of the pH and chemical form of pilocarpine used for emulsion preparation, practically all drug was found in the aqueous phase of the emulsion; thus, partitioning to the oily phase was negligible.

Animals↗
PubMed2002

A prospective, long-term, randomized study of the efficacy and safety of the drug combination pilocarpine 1% with clonidine 0.06% or clonidine 0.125% versus timolol 0.25%.

The purpose of this prospective, randomized study was to evaluate the efficacy and safety of the drug combinations--pilocarpine 1% with clonidine 0.06% and pilocarpine 1% with clonidine 0.125%, in comparison with timolol 0.25%. 54 patients with bilateral primary open angle glaucoma and comparable IOP were assigned to three study groups: group 1 received the drug combination of pilocarpine 1% and clonidine 0.06%, group 2 received the drug combination pilocarpine 1% and clonidine 0.125% and group 3 only timolol 0.25% drops. In all groups twice-daily medication was used. Mean diurnal IOP as well as ocular and systemic side effects were evaluated at week 1, 2, 4, 8 and 12. Changes in blood pressure, pulse rate, pupil size and patient symptoms were also recorded. At three months all patients had completed the study. Diurnal IOP was significantly reduced from baseline in all groups and consistent IOP reduction was achieved in all three groups at all follow up periods. Mean IOP reduction was 18.40%, 28.45% and 24.64% in group 1, group 2 and group 3, respectively. Flattening of the diurnal fluctuation in IOP was also seen in all patients. On comparing the IOP reduction achieved amongst the three groups, there was a statistically significant difference between group 1 and group 2 as well as between group I and group 3 while the difference between group 2 and group 3 was statistically insignificant. The drug combinations of pilocarpine 1% and clonidine did not produce any statistically significant effect on pupil diameter. No statistically significant difference was noted with respect to patient symptoms, blood pressure and pulse rate. In conclusion, the drug combination of pilocarpine 1% and clonidine 0.125% produces IOP reduction comparable to that achieved with timolol 0.25% drops in twice daily dosage and does not result in any significant ocular and systemic adverse effects.

Adrenergic alpha-Agonists↗
PubMed1985

The therapy of Adie's syndrome with dilute pilocarpine hydrochloride solutions.

Impressed by the benefit two patients with Adie's Syndrome derived from topical 0.1% pilocarpine therapy, we performed the present study to examine the measurable effects of 0.1% pilocarpine in several patients with this syndrome. Our study suggests those patients with Adie's Syndrome who lack stereoacuity may benefit from long term therapy with dilute pilocarpine if their stereoacuity may benefit from long term therapy with dilute pilocarpine if their stereoacuity improves following a single drop of 0.1% pilocarpine. Therefore, we recommend measuring stereoacuity during pupil diagnostic testing with 0.1% pilocarpine hydrochloride. Potential problems concerning medical therapy of Adie's Syndrome with parasympathomimetics are discussed.

Adie Syndrome↗
PubMed1997

Effects of pilocarpine and other antiglaucoma drugs on cultured human Tenon's fibroblast cells.

It has been found that long-term therapy with topical antiglaucoma drugs may decrease the success of glaucoma filtering surgery. In this study, various antiglaucoma drugs, including carteolol, betaxolol, levobunolol, pilocarpine, and timolol, were investigated for their proliferative effect on cultured human Tenon's fibroblast cells. It was found that the 3H-thymidine uptake of cultured fibroblast cells was inhibited by commercial antiglaucoma drugs, including carteolol of 0.1% concentration (13%), 0.01% (50%) and 0.001% (53%), betaxolol of 0.05% concentration (14%), 0.005% (42%) and 0.0005% (62%), levobunolol of 0.05% concentration (2%), 0.005% (32%) and 0.0005% (55%), and timolol of 0.025% concentration (4%), 0.0025% (47%) and 0.00025% (55%), whereas the 3H-thymidine uptake was increased by commercial pilocarpine eyedrop from 103% (0.2% of concentration), 170% (0.02% of concentration) to 171% (0.002% of concentration), when cells were treated with commercial drugs for 100 min. Meanwhile, the proliferations of cultured fibroblast cells were stimulated by simultaneously combining 0.2%, 0.02% and 0.002% concentrations of pilocarpine eyedrops with other antiglaucoma drugs, such as carteolol of 0.1% concentration (50%), 0.01% (113%) and 0.001% (138%), betaxolol of 0.05% concentration (24%), 0.005% (128%) and 0.0005% (142%), levobunolol of 0.05% concentration (32%), 0.005% (87%) and 0.0005% (119%), and timolol of 0.025% concentration (15%), 0.0025% (94%) and 0.00025% (118%). Following incubation with pure pilocarpine, the proliferation of Tenon's fibroblast cells was inhibited for 84% (0.2% concentration), 84% (0.02% concentration) and 90% (0.002% concentration). When fibroblast cells were treated with commercial pilocarpine eyedrops for 24 hours, the 3H-thymidine uptake was increased to 160% (0.02% concentration) and 172% (0.002% concentration). This result shows that the commercial pilocarpine may play a crucial role for the proliferation of cultured human Tenon's fibroblast cells.

Adrenergic beta-Antagonists↗
PubMed1996

Determination of the efficacy of topical oral pilocarpine for postirradiation xerostomia in patients with head and neck carcinoma.

Pilocarpine hydrochloride suspended in a candy-like pastille was evaluated as a topical treatment for radiation-induced xerostomia in head and neck cancer patients. This local delivery system, which differs from systemically administered pilocarpine preparations, was developed to hopefully maximize the local response and minimize the systemic side effects. A prospective, randomized, double-blind, placebo-controlled trial was undertaken to determine objective and subjective efficacy in reversing the decrease in salivation. Forty previously irradiated patients received increasingly higher pilocarpine dosages in pastilles for 5 successive weeks. At each successive dose of pilocarpine, no significant increased salivation was noted. However, 25 (74%) of 34 patients reported that pilocarpine alleviated their subjective xerostomia. Topical pilocarpine administration has shown similar results to previous systemic delivery methods for radiation-induced xerostomia, but with improved patient tolerance.

Administration, Oral↗
PubMed2000

Alterations of neuronal connectivity in area CA1 of hippocampal slices from temporal lobe epilepsy patients and from pilocarpine-treated epileptic rats.

PURPOSE: Neuronal network reorganization might be involved in epileptogenesis in human and rat limbic epilepsy. Apart from aberrant mossy fiber sprouting, a more widespread fiber rearrangement in the hippocampal formation might occur. Therefore, we studied sprouting in area CA1 because this region is most affected in human temporal lobe epilepsy. METHODS: In slices from hippocampi of patients operated on for temporal lobe epilepsy (n = 134), from pilocarpine-treated rats (n = 74), and from control rats (n = 15), viable neurons were labeled with fluorescent dextran amines. RESULTS: In human hippocampi as well as in pilocarpine-treated rats, the degree of nerve cell loss varied. In 67 of 134 slices from human specimens with distinct Ammon's horn sclerosis and in 23 of 74 slices from pilocarpine-treated rats, a severe shrunken area CA1 presented with a similar picture: few damaged neurons were labeled, and aberrant fiber connections were not visible. This was in contrast to human resected hippocampi and hippocampi from pilocarpine-treated rats with no or moderate loss of neurons. In these cases, pyramidal cells remote from the injection site were labeled (human tissue, n = 59 of 134; pilocarpine-treated rats, n = 39 of 74). In human resected hippocampi without obvious pathology and in control animals, no pyramidal neurons were labeled apart from the injection site. CONCLUSIONS: Axon collaterals of CA1 pyramidal cells are increased in human temporal lobe epilepsy and in pilocarpine-treated rats. Adjacent CA1 pyramidal cells project via aberrant collaterals to the stratum pyramidale and the stratum radiatum of area CA1. This network reorganization can contribute to hyperexcitability via increased backward excitation.

Animals↗
PubMed1997

Ocular hypotensive effect of pilocarpine before and after argon laser trabeculoplasty.

PURPOSE: The purpose of this study was to compare the hypotensive response of human glaucomatous eyes to 1% pilocarpine solution before and after argon laser trabeculoplasty. METHODS: We designed a prospective, 'repeated measures' study comparing the ocular hypotensive effect of acutely administered 1% pilocarpine solution in 30 medically uncontrolled glaucomatous eyes, before and after argon laser trabeculoplasty. RESULTS: The pilocarpine-induced IOP decrease was 3.6 +/- 0.59 mmHg before argon laser trabeculoplasty, and 1.8 +/- 0.53 mmHg after laser therapy. In both instances, the pilocarpine hypotensive effect was significantly correlated with pretreatment IOP (p = 0.02, r = 0.41 before argon laser trabeculoplasty, and p = 0.003, r = 0.52 after argon laser trabeculoplasty). We built a 'repeated measurements ANCOVA' model, and found no statistically significant difference between the pilocarpine IOP lowering effect before and after argon laser trabeculoplasty (p = 0.4). CONCLUSION: Argon laser trabeculoplasty does not modify the IOP lowering effect of 1% pilocarpine solution.

Aged↗
PubMed1984

Vehicle effects in ophthalmic bioavailability: an evaluation of polymeric inserts containing pilocarpine.

A series of polymeric ophthalmic inserts containing pilocarpine were formulated with four different types of polyvinyl alcohol, PVA, and two types of hydroxypropylcellulose. Pilocarpine was present as the nitrate, or as the salt with polyacrylic acid, PAA. In-vivo miosis vs time experiments on albino rabbits, showed that all inserts increased significantly the bioavailability of pilocarpine, with respect to a standard solution of pilocarpine nitrate. Two PVA inserts, containing the PAA-salt of pilocarpine, were particularly effective. The preparations were also submitted to in-vitro release tests and to differential scanning calorimetry, to ascertain the release mechanism, and to verify, via the thermal behaviour, possible interactions between drug and polymers. The chemical and physiochemical factors, most likely to influence the ophthalmic bioavailability of pilocarpine from the present preparations, are briefly reviewed.

Animals↗