Pilocarpine test

The three-point pharmacophore models are shown in Fig. 7. The structures of the y0-alanine analogues and their antiepileptic activities against pilocarpine test are tabulated in Table 3. 

Cholinergic hypersensitivity can be tested by using pilocarpine in 0.0625%, 0.1%, 0.125%, or 0.25% solution (Table 22-5).The usefulness of the pilocarpine test in eliciting cholinergic hypersensitivity depends on the presence of a standardized concentration of dmg at the iris. Thus any clinical procedure that compromises the corneal epithelium, the use of wetting agents, or other factors that enhance corneal penetration may result in false-positive findings. 

Figure 22-6 Pilocarpine test in a 57-year-old woman with right Adie s pupil. (A) Before dmg instillation. (B) After instillation of 0.125% pilocarpine into each eye, the normal left pupil constricts slightly, whereas the right Adie s pupil constricts significantly.

If, however, the patient exhibits only a unilateral fixed and dilated pupil without evidence of ptosis or extraocular muscle involvement, the clinician should perform the pilocarpine test, first using a 0.125% solution to reveal any cholinergic hypersensitivity as evidence for Adie s pupil. If there is no local iris damage by slit-lamp examination, no sector palsy of the iris sphincter, and no cholinergic hypersensitivity demonstrated by the 0.125% pilocarpine test, then the condition might be associated with interruption of the preganglionic innervation to the iris sphincter (i.e., third-nerve palsy). If the patient has third-nerve palsy, topically instilled pilocarpine in moderate concentrations activates the muscarinic receptor sites on the iris sphincter. Therefore if 0.125% pilocarpine reveals no cholinergic hypersensitivity, the practitioner... 

Janssen, P.A.J., Niemegeers, C.J.E. 1967 The Perljdieral and Central Anticholinergic Properties of Benzetimlde (R-4929) and Other Atropine-Like Drugs as Measured In a Ifev Anti-Pilocarpine Test In Rats. Psychoi armacol. 11 231-254. 

The extraction of alkaloids from jaborandi has been dealt with by Wurtzen, and the estimation of pilocarpine in the drug and its preparations by Jowett and by Bourcet and more recently by Taran and by Shupe.ii Elvidge has devised a colorimetric method based on Ekkert s test, < and a polarographic study has been made by Kirkpatrick. Tlie two first-pamed authors depend on the isolation of pilocarpine nitrate, which is also the basis of the process of manufacture described by Cheninitius.12... 

Diagnosis of CF is based on two separate elevated sweat chloride concentrations of greater than or equal to 60 mEq/L (or mmol/L) obtained through pilocarpine iontophoresis (referred to as the sweat test ). Genetic testing (CFTR mutation analysis) may be performed to confirm the diagnosis, screen in utero, or detect carrier status. More than 70% of diagnoses are made by 12 months of age and almost all are made by age 12. 

Muscarinic Agonists. Another approach is to use a medication that directly activates subtypes of the acetylcholine receptors, namely, muscarinic receptor agonists. The muscarinic agonists used in the past have not been effective. This includes bethanecol, pilocarpine, and oxotremorine. This line of treatment, however, has not been entirely abandoned, and several medications are currently in testing. 

Gibson, L.E., and R.E. Cooke. 1959. A test for concentration of electrolytes in sweat in cystic fibrosis of the pancreas utilizing pilocarpine by iontophoresis. Pediatrics Evanston) 23 545. 

The ease of application, the minimization of systemic side effects, and the increased drug penetration directly into the target region resulted in extensive clinical use of iontophoresis mainly in the transdermal field. This technique has been utilized for administration of local anesthetics [2-5], sweat chloride testing in cystic fibrosis patients by transcutaneous delivery of pilocarpine [6,7], administration of vidarabine to patients with herpes orolabialis [8], fluoride administration to patients with hypersensitive dentin [9,10], and gentamicin delivery for the management of burned ears [11],... 

Various lecithin-based MEs were also characterized by Hasse and Keipert [131]. The formulations were tested in terms of their physicochemical parameters (pH, refractive index, osmolality, viscosity, and surface tension) and physiological compatibility (HET-CAM and Draize test). In addition, in vitro and in vivo evaluations were performed. The tested MEs showed favorable physicochemical parameters and no ocular irritation as well as a prolonged pilocarpine release in vitro and in vivo. 

Diepold, R., Kreuter, I, Himber, J., Gurny, R., Lee, V. H., Robinson, J. R., et al. (1989), Comparison of different models for the testing of pilocarpine eyedrops using conventional eyedrops and a novel depot formulation (nanoparticles), Graefes Arch. Clin. Exp. Ophthalmol., 227(2), 188-193. 

Q2 In the sweat test, sweating is induced by passing a weak electric current across an area of skin treated with the secretory stimulant pilocarpine. The current enhances the ability of pilocarpine to penetrate skin and so local secretion of sweat is induced. When this test was performed on Carmen, the diagnosis was confirmed her sweat was found to contain 100 mmol l-1 chloride, normally this is expected to be <60 mmoll-1. 

Pilocarpine 208 Cation Sweat test (cystic fibrosis) 166... 

Janssen and Nlemegeers (280), on the basis of tests with prophylactic administration of benzetlmlde to rats given pilocarpine hydrochloride Intravenously at 80 mg/kg, concluded chat benzetlmlde had sufficient action on the central nervous system to Justify its consideration as a theraupeutlc agent In parkinsonism. They considered also that It was one of only three compounds. In a total of 23 anticholinergic substances examined, that were able at submydrlatlc doses to prevent lacrlmatlon and salivation Induced by pilocarpine. 

The sweat test occurs in three phases sweat stimulation by pilocarpine iontophoresis collection of the sweat onto gauze, filter paper, coil, patch, or capillary tube and qualitative or quantitative analysis of sweat chloride, sodium, conductivity, or osmolality. A survey of 753 laboratories (Table 27-3) performing sweat testing revealed that 47% analyze chloride, 46% analyze conductivity, and less than 7% analyze sodium or osmolality. ... 

LeGrys VA, Retsch-Bogart G. Urticaria associated with the pilocarpine iontophoresis sweat test. Pediatr Pulmol 1977 24 296-7. 

A confusing picture emerges when cannabinoids are evaluated in animal models of epilepsy (Karler and Turkanis 1981 Consroe and Snider 1986). CBD has anticonvulsant properties with a spectrum distinct from standard anticonvulsants, apparently not hampered by the development of tolerance but with a varying profile according to the species tested. THC can produce seizures in some circumstances but is anticonvulsant in others. In a recent study, THC (10 mg/kg) completely abolished spontaneous seizures in the rat pilocarpine model of epilepsy (Wallace et al. 2003). The results also indicated that endogenous cannabinoid tone may modulate seizure termination and duration via the CBi receptor. 

EVAc has been used in the fabrication of a variety of devices for drug delivery. For example, EVAc was used by Alza in devices to deliver pilocarpine to the surface of the eye for glaucoma treatment (Ocusert). Currently, EVAc is used in the Progestasert intra-uterine device for the delivery of contraceptive hormones to the female reproductive tract and as a rate-controlling membrane in a number of transdermal devices. Since EVAc is one of the most biocompatible of the polymers that have been tested as implant materials [30], it has been widely studied as a matrix for controlled drug delivery (see [31, 32] for reviews). 

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