Physiologic-pharmacologic interpretation of the constants in the hill equation for neuromuscular block: A hypothesis

Journal of Pharmacokinetics and Pharmacodynamics

Volumn 29, Issue 2, 2002, Pages 189-206

  Nigrovic, V ^a   Amann, A ^b,c  

^a MEDICAL COLLEGE OF OHIO   (United States)

^b UNIVERSITY OF INNSBRUCK   (Austria)

^c ETH ZURICH   (Switzerland)

Author keywords

Neuromuscular blocking drugs; Neuromuscular transmission; Postsynaptic receptors; Simulation of neuromuscular block; Skeletal muscle

Indexed keywords

ATRACURIUM; CHOLINERGIC RECEPTOR; DIMETHYLTUBOCURARINE CHLORIDE; FENTANYL; GALLAMINE; HALOTHANE; MUSCLE RELAXANT AGENT; NEUROMUSCULAR BLOCKING AGENT; NITROUS OXIDE; PANCURONIUM; POSTSYNAPTIC RECEPTOR; TUBOCURARINE CHLORIDE;

ARTICLE; CALCULATION; COMPARTMENT MODEL; DISSOCIATION CONSTANT; DRUG BINDING SITE; DRUG DISTRIBUTION; DRUG RECEPTOR BINDING; EQUILIBRIUM CONSTANT; HILL REACTION; HYPOTHESIS; IC 50; MAXIMUM ALLOWABLE CONCENTRATION; MUSCLE CELL; MUSCLE CONTRACTION; NERVE ENDING; NEUROMUSCULAR BLOCKING; NEUROMUSCULAR TRANSMISSION; PHANTOM; PRIORITY JOURNAL; RECEPTOR OCCUPANCY; SIMULATION; SKELETAL MUSCLE; STEADY STATE;

BINDING SITES; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, BIOLOGICAL; MUSCLE, SKELETAL; NEUROMUSCULAR AGENTS; NEUROMUSCULAR BLOCKADE;

EID: 0036553520     PISSN: 1567567X     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1019759725394     Document Type: Article

References (27)

1. G. Fletcher and J. Steinbach. Ability of nondepolarizing neuromuscular blocking drugs to act as partial agonists at fetal and adult mouse muscle nicotinic receptors. Mol. Pharmacol. 49:938-947 (1996).
2. S. Pedersen and J. Cohen. D-tubocurarine binding sites are located at alpha-gamma and alpha-delta subunit interfaces of the nicotinic acetylcholine receptor. Proc. Natl. Acad. Sci. U.S.A. 87:2785-2789 (1990).
3. A. Le Dain, B. Madsen, and R. Edeson. Kinetics of (+)-tubocurarine blockade at the neuromuscular junction. Br. J. Pharmacol. 103:1607-1613 (1991).
4. D. Armstrong and H. Lester. The kinetics of tubocurarine action and restricted diffusion within the synaptic cleft. J. Physiol. 294:365-386 (1979).
5. J. Min, I. Bekavac, M. Glavinovic, F. Donati, and D. Bevan. Iontophoretic study of speed of action of various muscle relaxants. Anesthesiology 77:351-356 (1992).
6. A. Kopman, M. Klewicka, and G. Neuman. An alternate method for estimating the dose-response relationships of neuromuscular blocking drugs. Anesth. Analg. 90:1191-1197 (2000).
7. A. Kopman, M. Klewicka, K. Ghori, F. Flores, and G. Neuman. Dose-response and onset/offset characteristics of rapacuronium. Anesthesiology 93:1017-1021 (2000).
8. L. Sheiner, D. Stanski, S. Vozeh, R. Miller, and J. Ham. Simultaneous modeling of pharmacokinetics and pharmacodynamics: Application to d-tubocurarine. Clin. Pharmacol. Ther. (St. Louis) 25:358-371 (1979).
9. P. Wright, R. Brown, M. Lau, and D. Fisher. A pharmacodynamic explanation for the rapid onset/offset of rapacuronium bromide. Anesthesiology 90:16-23 (1999).
10. B. Plaud, J. Proost, J. Wierda, J. Barre, B. Debaene, and C. Meistelman. Pharmacokinetics and pharmacodynamics of rocuronium at the vocal cords and the adductor pollicis in humans. Clin. Pharmacol. Ther. (St Louis) 58:185-191 (1995).
11. D. Fisher, J. Szenohradszky, P. Wright, M. Lau, R. Brown, and M. Sharma. Pharmacodynamic modeling of vecuronium-induced twitch depression. Rapid plasma-effect site equilibration explains faster onset at resistant laryngeal muscles than at the adductor pollicis. Anesthesiology 86:558-566 (1997).
12. J. Kuipers, F. Boer, E. Olofsen, J. Bovill, and A. Burm. Recirculatory pharmacokinetics and pharmacodynamics of rocuronium in patients. Anesthesiology 94:47-55 (2001).
13. E. Vizi and B. Lendvai. Side effects of nondepolarizing muscle relaxants: Relationship to their antinicotinic and antimuscarinic actions. Pharmacol. Ther. 73:75-89 (1997).
14. E. Bradshaw, N. Harper, B. Pleuvry, and C. Modla. Differing potencies of muscle relaxants on rat and guinea-pig phrenic nerve diaphragm preparations. J. Pharm. Pharmacol. 38:623-624 (1986).
15. G. Bikhazi, I. Leung, C. Flores, H. Mikati, and F. Foldes. Potentiation of neuromuscular blocking agents by calcium channel blockers in rats. Anesth. Analog. 67:1-8 (1988).
16. S. Matsuo, D. Rao, I. Chaudry, and F. Foldes. Interaction of muscle relaxants and local anesthetics at the neuromuscular junction. Anesth. Analog. 57:580-587 (1978).
17. L. Aziz, Y. Ohta, T. Yamada, K. Morita, and M. Hirakawa. The effect of isoflurane and temperature on the actions of muscle relaxants in rat in vitro. Anesth. Analog. 80:1181-1186 (1995).
18. R. Treffers, A. Frankhuyzen, and L. Booij. Effects of neostigmine, edrophonium, 4-aminopyridine and their combinations. Acta Anaesth. Belg. 39:55-58 (1988).
19. D. Stanski, J. Ham, R. Miller, and L. Sheiner. Pharmacokinetics and pharmacodynamics of d-tubocurarine during nitrous oxide-narcotic and halothane anesthesia in man. Anesthesiology 51:235-241 (1979).
20. D. Fisher, O. K. C. D. Stanski, R. Cronnelly, R. Miller, and G. Gregory. Pharmacokinetics and pharmacodynamics of d-tubocurarine in infants, children, and adults. Anesthesiology 57:203-208 (1982).
21. S. Rupp, K. Castagnoli, D. Fisher, and R. Miller. Pancuronium and vecuronium pharmacokinetics and pharmacodynamics in younger and elderly adults. Anesthesiology 67:45-49 (1987).
22. C. Hull, B. H. Van, K. McLeod, A. Sibbald, and M. Watson. A pharmacodynamic model for pancuronium. Br. J. Anaesth. 50:1113-1123 (1978).
23. F. Donati, F. Varin, J. Ducharme, S. Gill, Y. Theoret, and D. Bevan. Pharmacokinetics and pharmacodynamics of atracurium obtained with arterial and venous blood samples. Clin. Pharmacol. Ther. (St. Louis) 49:515-522 (1991).
24. B. Weatherley, S, Williams, and E. Neill. Pharmacokinetics, pharmacodynamics and dose-response relationships of atracurium administered i.v. Br. J. Anaesth. 55 Suppl 1:39S-45S (1983).
25. J. Kitts, D. Fisher, P. Canfell, M. Spellman, J. Caldwell, T. Heier, M. Fahey, and R. Miller. Pharmacokinetics and pharmacodynamics of atracurium in the elderly. Anesthesiology 72:272-275 (1990).
26. D. Fisher, P. Canfell, M. Spellman, and R. Miller. Pharmacokinetics and pharmacodynamics of atracurium in infants and children. Anesthesiology 73:33-37 (1990).
27. R. Matteo, W. Brotherton, K. Nishitateno, H. Khambatta, and J. Dias. Pharmacodynamics and pharmacokinetics of metocurine in humans: Comparison to d-tubocurarine. Anesthesiology 57:183-190 (1982).