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PubMedDate not supplied

Determination of drugs used as anti-Parkinson's disease drugs in urine and serum by capillary electrophoresis.

A new capillary electrophoresis method to determine simultaneously eight of the most important anti-Parkinson's disease compounds has been developed. The generic names of the drugs studied are benactyzine (BA), trihexyphenidyl (TP), fenpiverin (FP), diphemin (DF), scopolamine (BL), adiphenine (TS), diethylaminoethylester 1-phenylcyclopentane-1-carboxylate (EKK), and diethylaminoethylester tetramethoxydiphenylacetate (EKO). An untreated fused-silica capillary tube (75 microns i.d., 57 cm total length, 49.5 cm length to the detector) was used with detection at 190 nm. The optimal separation conditions were 50 mM phosphate buffer (pH 2.7) with 7 mM-beta-cyclodextrin, electrokinetic injection for 15 sec at 5 kV, temperature 25 degrees C, and 15-20 kV separation voltage. Complete separation of all compounds was achieved in less than 16 min. The procedure was applied for the determination in urine and serum. The limits of detection (LOD, S/N = 3) for serum were 209 (FP), 234 (EKO), 168 (DF), 182 (BA), 168 (TP), 220 (BL), 174 (TS), and 163 (EKK) ppb. The method can be used for the therapeutic drug monitoring of these central active cholinolytics in clinical laboratories.

Antiparkinson Agents↗
PubMed2001

Local anesthetics noncompetitively inhibit function of four distinct nicotinic acetylcholine receptor subtypes.

Local anesthetics (LAs) are considered to act primarily by inhibiting voltage-gated Na(+) channels. However, LAs also are pharmacologically active at other ion channels including nicotinic acetylcholine receptors (nAChR). nAChR exist as a family of diverse subtypes, each of which has a unique pharmacological profile. The current studies established effects of LAs on function of four human nAChR subtypes: naturally expressed muscle-type (alpha1*-nAChR) or autonomic (alpha3beta4*-nAChR) nAChR, or heterologously expressed nAChR containing alpha4 with either beta2- or beta4-subunits (alpha4beta2- or alpha4beta4-nAChR). Of the LAs tested, those with structures containing two separated aromatic rings (e.g., proadifen and adiphenine) had the greatest inhibition potency (IC(50) values between 0.34 and 6.3 microM) but lowest selectivity (approximately 4-fold) across the four nAChR subtypes examined. From the fused, two-ring (isoquinoline backbone) class of LAs, dimethisoquin had comparatively moderate inhibition potency (IC(50) values between 2.4 and 61 microM) and approximately 30-fold selectivity across nAChR subtypes. Lidocaine, a commonly used LA from the single ring category of LAs, blocked nAChR function with IC(50) values of between 52 and 250 microM and had only approximately 5-fold selectivity across nAChR subtypes. Its quaternary triethyl ammonium analog, QX-314, had greater inhibition potency, but the trimethyl ammonium derivative, QX-222, was the least potent LA at all but the alpha4beta2-nAChR subtype. With only a few exceptions, LA effects were consistent with noncompetitive inhibition of nAChR function and occurred at therapeutic doses. These studies suggest structural determinants for LA action at diverse nAChR subtypes and that nAChR likely are clinically relevant targets of LAs.

Anesthetics, Local↗
PubMed1990

[Electric stimulation of the dental pulp in the evaluation of the central effect of analgesics].

We conducted a double-blind cross-over study in ten volunteers aged from 19 to 30 years, to compare the pain control effects of a single oral dose of two analgesic compounds (drug A: propyphenazone mg 250, ethylmorphine mg 5, caffeine mg 5; drug B: dipyrone mg 500, diphenhydramine mg 12.5, adiphenine mg 5, ethyl aminobenzoate mg 2.5) in an experimental pain model using stimulation of dental pulp. Constant voltage stimuli were delivered through silver chloride electrodes placed in contact with the vestibular surface of the upper medial incisor. At the beginning of the session, the pain input was graded by asking the subject to identify the weakest stimulus perceived (threshold level) and the strongest stimulus endurable (tolerance level). The range between threshold and tolerance level was divided in nine steps plus a subliminal step. The ten steps were delivered randomly, and each series of steps was repeated eight times. The subjects were instructed to rate the pain sensation in an arbitrary scale of 5 degrees. The procedure was repeated at 60 min and 180 min after drug administration. Each subject received two tablets of drug A or drug B in two different sessions at weekly intervals. Statistical analysis of the procedures showed that neither drug A nor drug B significantly affected the pain threshold. Drug A significantly reduced the total pain score (P less than 0.01) and its action peaked 60 min after administration.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMedDate not supplied

[Effect of amisyl and spasmolytin on the blood supply and oxygen metabolism of the brain].

The effect of benactyzine and spasmolytin adiphenine on the blood circulation in the oxygen consumption by the brain were investigated in experiments on dogs. The resulting data point to a biphasic action of benacyzine and spasmolytin on the blood supply of the brain (after a short-lived increase of the blood flow a clearcut decline of it is noted). The oxygen intake from the blood varies irregularly. In chlorophos-poisoned dogs the oxygen absorption by the brain changes under the effect of benactyzine and rises after administration of spasmolytin. The cerebral circulation then changes non-uniformly under the effect of benactyzine, while following spasmolytin injections it dicreases in the majority of experiments.

Absorption↗
PubMed1988

Reversal of inhibition of prolactin secretion in cultured pituitary cells by muscarinic antagonists.

We investigated whether the inhibition of prolactin secretion from pituitary cells by carbachol, a cholinergic agonist resistant to hydrolysis by cholinesterases, would be a useful bioassay to explore an important nonneuronal action of antimuscarinic agents. Carbachol inhibited prolactin secretion from cultured rat anterior pituitary cells in a dose-dependent manner with a mean IC50 of 1.5 +/- 0.6 (S.E.) microM and maximal inhibition at 10(-5) M. Prolactin levels in media were significantly reduced by 30 min of incubation with carbachol. This inhibition persisted for 24 hr and was reversed by 2 microM atropine. The stimulation of prolactin secretion by 10(-6) M thyrotropin releasing hormone (to 1.5 times control) was inhibited by the addition of carbachol (10(-5) M). Addition of atropine (2 microM) to these agents restored maximal stimulation by thyrotropin releasing hormone. The inhibition of carbachol by atropine was competitive, whereas the inhibition of thyrotropin releasing hormone by carbachol was noncompetitive. The apparent affinities (Ki) of several antimuscarinic agents in pituitary cells were determined by their ability to reverse the carbachol inhibition of prolactin secretion: atropine 0.14 nM, scopolamine 0.26 nM, azaprophen 0.3 nM, aprophen 3.0 nM, pirenzepine 42 nM, benactyzine 80 nM and adiphenine 198 nM. These potencies correlated positively with those previously determined for inhibition of alpha amylase secretion from pancreatic acinar cells as well as with those for behavioral depressant actions of the antimuscarinics. Cultured anterior pituitary cells thus provide an effective system for testing the relative potencies of muscarinic antagonists in pituitary cells.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1980

[The dynamics of drug release from suppositories. Part 6: The effects of lipophil and hydrophilic suppository bases on the release of adeiphenin (author's transl)].

On studying the release of adiphenin from suppositories, the authors found that it is most rapid from hydrophilic bases. The release rate decreased in the following order: PEG 1500 leads to PEG 2000 leads to PEG 4000 (70%) + Glycerol (30%) leads to PEG 1000 (70%) + Peg 4000 (30%) leads to PEG 4000 leads to PEG 6000. The release is considerably slower from the bases Witepsol W35, Witepsol H15 and cacao butter.

Chemical Phenomena↗