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At least 577 records · Page 32Linked to original sources
PubMed1977

Mechanism of methacholine-induced rise in intraocular pressure in the dog.

The mechanism of the methacholine-induced rise in intraocular pressure in the dog was studied to determine the basis of the relationship, if any, between lens thickness and intraocular pressure. The results rule out a vasodilator component in methacholine intraocular pressure elevation, and the tonometric recording of the elevation makes unlikely the involvement of methacholine stimulation of the rectus muscles of the eye. Thus, indirect evidence points to methacholine stimulation of ciliary muscle contraction with consequent thickening of the lens as responsible for its intraocular pressure-elevating effect and, hence, the ability of the response under investigation to specify the cycloplegic liability of a neurotropic antispasmodic agent.

Animals↗
PubMed1993

Glycopyrronium bromide blocks differentially responses mediated by muscarinic receptor subtypes.

To analyse the potency of glycopyrronium bromide in blocking responses mediated via subtypes of muscarinic receptors in vitro, we tried to determine its equilibrium dissociation constants at prejunctional muscarinic receptors inhibiting the twitch response of rabbit vas deferens (presumed M1 type), at M2 (paced at left atria), M3 (guinea pig ileum) muscarinic receptor subtypes and at the muscarinic receptor of the rabbit iris sphincter (not M1-M4, not m5). Glycopyrronium bromide shifted to the right the curve for inhibition of the twitch response induced by the agonist McN-A-343, and the methacholine-induced curves for inhibition of rat atrial contraction, and for tonic contraction of guinea pig ileum and rabbit iris sphincter. Glycopyrronium bromide blocked with very high potency (> 11, apparent -log KB) the response in rabbit vas deferens. Its affinity was low (9.09) for the M2 subtype, and intermediate (10.31 or 10.13) for the ileal M3 and the atypical iris muscarinic receptor subtype, respectively. Except at the receptors in rabbit vas deferens, the blockade of agonist effect appeared to be of simple competitive type. In conclusion, glycopyrronium bromide is about 10 or 100 fold more potent in preventing a response to activation of the prejunctional receptor in rabbit vas deferens than in blocking an M3 or M2 muscarinic receptor subtype, respectively, in vitro. The low affinity for M2 receptors may, in part, explain the low incidence of unwanted tachycardia in therapy. The drug failed to discriminate between an M3 receptor and the atypical rabbit iris sphincter receptor.

(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethy↗
PubMed1986

Analysis of some antispasmodic drugs: oxyphencyclimine and glycopyrronium bromide.

Oxyphencyclimine hydrochloride (via its tertiary amine group) and glycopyrronium bromide (via its quaternary ammonium group) were analysed by two different colorimetric methods. The first method depends on the dye-salt formation method using tropeolin ooo as the anionic dye and 1,2-dichloroethane as solvent for the extraction of the formed ion pairs. The coloured ion pairs have maximum absorption at 483-486 nm. The second method is based on the use of citric acid-acetic anhydride reagent. The coloured complex has maximum absorption at 562-565 nm.

Chemical Phenomena↗
PubMed1994

Recovery of neuromuscular function after atracurium and pancuronium maintenance of pancuronium block.

The study was undertaken to determine whether a neuromuscular blockade induced with pancuronium but maintained with atracurium was associated with a shorter time to complete recovery after administration of neostigmine than if the blockade was maintained with pancuronium alone. Anaesthesia consisted of thiopentone, N2O/O2/enflurane and fentanyl, and the neuromuscular blockade, induced by pancuronium 0.1 mg.kg-1 was monitored by the force of contraction of adductor pollicis during major abdominal surgery lasting 2-5 hr. In 24 patients--Group 1--atracurium 0.07 mg.kg-1 was repeated when the first twitch of the train-of-four (TOF) returned to 25% of control (T1/TC 25). In 28 patients--Group 2--pancuronium 0.015 mg.kg-1 was given at similar recovery of T1/TC. At the end of surgery, neostigmine 0.07 mg.kg-1 and glycopyrolate 0.015 mg.kg-1 were given to reverse the residual neuromuscular blockade which was indicated by a T1/TC of less than 25% in all patients. The time from injection of the reversal drugs to a TOF ratio of 70% was similar in both groups (Group 1, 11.6 +/- 7.6 min; Group 2, 10.1 +/- 6 min; P = NS), but the recovery index was smaller in Group 2 (Group 1, 4 +/- 2.6 min; Group 2, 2.61 +/- 1.2 min; P < 0.05). Furthermore, there was no difference between groups in the duration of action of each redose. The study showed that when compared with pancuronium, equipotent doses of atracurium were not associated with (a) a shorter time to complete recovery from a neuromuscular blockade induced with pancuronium or (b) a shorter duration of action.

Adult↗