Abstract
Among the different classes of drugs used in the treatment of asthma, the bronchodilators (β2-adrenoceptor agonists, muscarinic receptor antagonists, methylxanthines) bring symptomatic relief but contribute little to ameliorating the underlying bronchial inflammation. Glucocorticoids (see Chap. 8) exert a potent antiinflammatory effect and, particularly when inhaled, have both therapeutic and prophylactic value. The drug that is now accepted clinically as having a prophylactic effect in asthma, whilst only rarely bringing symptomatic relief, is cromoglycate; the recently introduced nedocromil is another example of the same class of compound. Ketotifen has a different pharmacological profile and has gained some acceptance as a prophylactic agent in asthma. This chapter will only review the pharmacology of drugs in clinical use (cromoglycate, nedocromil, ketotifen), although there is much current research directed towards finding other new types of antiinflammatory agents to be used as first-line durgs in mild asthma, leaving glucocorticoids for treatment of severe asthma.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
Abraham WM Stevenson JS, Chapman GA, Tallent MW, Jackowski J (1987) The effect of nedocromil sodium and cromolyn sodium on antigen-induced responses in allergic sheep in vivo and in vitro. Chest 92: 913–917
Adachi M, Kobayashi H, Aoki N, lijima M, Kokubu F, Furuya A, Takahashi T (1984) A comparison of the inhibitory effects of ketotifen and disodium cromoglycate on bronchial responses to house dust, with special reference to the late asthmatic response. Pharmatherapeutica 4: 36–42
Altounyan REC (1970) Changes in histamine and atropine responsiveness as a guide to diagnosis and evaluation of therapy in obstructive airways disease. In: Pepys J, Frankland AW (eds) Disodium cromoglycate in allergic airways disease. Butterworths, London
Altounyan REC (1980) Review of clinical activity and mode of action of sodium cromoglycate. Clin Allergy 10: 481–489
Altounyan REC, Cole M, Lee TB (1986a) Effect of nedocromil sodium on changes in bronchial hyperreactivity in non-asthmatic, atopic rhinitic subjects during the grass pollen season. Eur J Respir Dis 69 [Suppl 147]: 271–273
Altounyan RCE, Lee TB, Rocchiccioli KMS, Shaw CL (1986b) A comparison of the inhibitory effects of nedocromil sodium and sodium cromoglycate on adenosine monophosphate-induced bronchoconstriction in atopic subjects. Eur J Respir Dis 69: 277–279
Archer CB, Page CP, Paul W, Morley J, MacDonald DM (1985) Actions of disodium cromoglycate ( DSCG) on human skin responses to histamine, codeine and PAF-acether. Agents Actions 16: 6–8
Armour C, Temple DM (1982) The modification by ketotifen of respiratory responses to histamine and antigen in guinea-pigs. Agents Actions 12: 285–288
Arnoux B, Denjean A, Page CP, Morley J, Benveniste J (1985) Pulmonary effects of platelet activating factor in a primate are inhibited by ketotifen. Am Rev Respir Dis 131 [Suppl]: A2
Arnoux B, Denjean A, Page CP, Nolibe D, Morley J, Benveniste J (1988) Accumulation of platelets and eosinophils in baboon lung after pafacether challenge. Am Rev Respir Dis 137: 855–860
Arruzazabala ML, Gonzalez R (1984) Protective effects of ketotifen on guinea pig trachea. Respiration 45: 50–55
Arruzazabala ML, Gonzalez R (1985) Pharmalogical characterization of ketotifen effects on guinea pig ileum. Arch Immunol Ther Exp (Warsz) 33: 353–359
Assem ESK, Monger JL (1970) Inhibition of allergic reactions in man and other species by cromoglycate. Int Arch Allergy Appl Immunol 38: 68–77
Barbato A, Pisetta F, Mesirca P, Ragusa A, Zacchello F (1987) Sodium cromoglycate and carbachol-induced bronchoprovocation in asthmatic children. Pediatr Pulmonol 3: 161–165
Basran GS Page CP, Paul W, Morley J (1983) Cromoglycate (DSCG) inhibits responses to platelet-activating factor (PAF-acether) in man: an alternative mode of action for DSCG in asthma. Eur J Pharmacol 86: 143–144
Bauer CP (1986) The protective effect of nedocromil sodium in exercise-induced asthma. Eur J Respir Dis 69: [Suppl 147] 252–254
Ben-Dov I, Bar-Yishay E, Godfrey S (1983) Heterogeneity in the response of asthmatic patients to pre-exercise treatment with cromolyn sodium. Am Rev Respir Dis 127: 113–116
Benovic JL, Mayor F, Staniszewski C, Lefkowitz RJ Caron MG (1982) Purification and characterization of the ß-adrenergic receptor kinase. J Biol Chem 262: 9026–9032
Bergren DR, Myers DL, Mohrman M (1985) Activity of rapidly-adapting receptors to histamine and antigen challenge before and after sodium cromoglycate. Arch Int Pharmacodyn 273: 88–89
Biggs DF, Goel V (1985) Mechanisms of action of sodium cromoglycate. Can J Physiol Pharmacol 63: 760–765
Bleehen T, Keele CA (1977) Observations on the algogenic actions of adenosine compounds on the human blister base preparation. Pain 3: 367–377
Boner AL, Vallone G, Andreiol A, Biancotto R, Warner JO (1987) Nebulised sodium cromoglycate and verapamil in methacholine induced asthma. Arch Dis Child 62: 264–268
Boner AL, Niero E, Grigolini C, Valletta EA, Biancotto R, Gaburro D (1985) Inhibition of exercise-induced asthma by three forms of sodium cromoglycate. Eur J Respir Dis 66: 21–24
Boner AL, Richelli C, Antolini I, Vibelli C, Andri L (1986) The efficacy of ketotifen in a controlled double-blind food challenge study in patients with food allergy. Ann Allergy 57: 61–64
Bonser RW, Thompson NT, Hodson HF, Beams RM, Garland LG (1988) Evidence that a second stereochemical centre in diacylglycerols defines interaction at the recognition site on protein kinase C. FEBS Lett 234: 341–344
Bradford PG, Rubin RP (1986) The differential effects of nedrocromil sodium and sodium cromoglycate on the secretory response of rabbit peritoneal neutrophils. Eur J Respir Dis 69 [Suppl 147]: 238–240
Breslin FJ, McFadden ER, Ingram RH (1980) The effects of cromolyn sodium on the airway response to hyperpnea and cold air in asthma. Am Rev Respir Dis 122: 11–16
Bretz U, Martin U, Mazzoni L, Ney UM (1983) P-adrenergic tachyphylaxis in the rat and its reversal and prevention by ketotifen. Eur J Pharmacol 86: 321–328
Broberger U, Graff-Lonneving V, Lilja G, Rylander E (1986) Ketotifen in pollen- induced asthma: a double-blind placebo-controlled study. Clin Allergy 16: 119–127
Brodde O-E, Brinkmann M, Schemuth R, O’Hara N, Daul A (1985) Terbutaline- induced desensitization of human lymphocyte -adrenoceptors. J Clin Invest 76: 1096–1101
Brodde O-E, Howe U, Egerszegi S, Konietzko N, Michel MC (1988) Effect of prenisolone and ketotifen on p2-adrenoceptors in ashmatic patients receiving (32-bronchodilators. Eur J Clin Pharmacol 34: 145–150
Brooks CD, Nelson AL, Metzler C (1986) Attentuation of protection with repeated cromolyn dosing before exercise challenge in subjects with asthma. J Clin Pharmacol 26: 91–96
Butchers PR, Fullarton JR, Skidmore IF, Thompson LE, Vardey CJ, Wheeldon A (1979) A comparison of the anti-anaphylactic activities of salbutamol and disodium cromoglycate in the rat, the rat mast cell and in human lung tissue. Br J Pharmacol 67: 23–32
Chiavarelli M, Moncada S, Mullane K (1981) Prostacyclin-induced bradycardia is dependent on the basal heart rate and is antagonised by sodium cromoglycate. Br J Pharmacol 74: 252
Chung KF, Minette P, McCusker M, Barnes PJ (1988) Ketotifen inhibits the cutaneous but not the airway responses to platelet-activating factor in man. J Allergy Clin Immuol 81: 1192–1198
Church MK (1986) Is inhibition of mast cell mediator release relevant to the clinical activity of anti-allergic drugs? Agents Actions 18: 288–293
Church MK, Gradidge CF (1978) Potentiation of histamine release by sodium cromoglycate. Life Sci 23: 1899–1904
Church MK, Young KD (1983) The characteristics of inhibition of histamine release from human lung fragments by sodium cromoglycate, salbutamol and chlorpromazine. Br J Pharmacol 78: 671–679
Church MK, Holgate ST, Hughes PJ (1983a) Adenosine inhibits and potentiates IgE-dependent histamine release from human basophils by an A2-receptor mediated mechanism. Br J Pharmacol 80: 719–726
Church MK, Holgate ST, Pao G J-K (1983b) Histamine release from mechanically and enzymatically dispersed human lung mast cell: Inhibition by salbutamol and cromoglycate. Br J Pharmacol 79: 374p
Church MK, Hughes PJ, Holgate ST (1983c) Adenosine modulation of histamine release from human basophils and mast cells. Fed Proc 42: 1342
Clarke CW, May CS (1980) A comparison of the efficacy of ketotifen (HC 20-511) with sodium cromoglycate ( SCG) in skin test positive asthma. Br J Clin Pharmacol 10: 473–476
Coleridge JC, Coleridge HM, Roberts AM, Kaufman MP, Baker DG (1982) Tracheal contraction and relaxation initiated by lung and somatic afferents in dogs. J Appl Physiol 52: 984–990
Collier JG, Fuller RW (1983) Evidence for an effect of sodium cromoglycate on sensory nerves in man. Br J Clin Pharmacol 16: 639–643
Collier JG, Fuller RW (1984) Capsaicin inhalation in man and the effects of sodium cromoglycate. Br J Pharmacol 81: 113–117
Corcia A, Schweitzer-Stenner R, Pecht I, Rivany B (1986) Characterisation of the ion channel activity in planar bilayers containing IgE-Fc receptor and the cromolyn-binding protein. EMBO J 5: 849–854
Cox JSG, Beach JE, Blair AMJN, Clarke AJ, King J, Lee TB, Loveday DEE, Moss GF, Orr TSC, Ritchie JT, Sheard P (1970) Diodium cromoglycate ( Intal ). Adv Drug Res 5: 115–196
Craps LP, Ney UM (1984) Keototifen: current views on its mechanism of action and their therapeutic implications. Respiration 45: 411–421
Crimi N, Palermo F, Oliveri R, Cacopardo B, Vanchieri C, Mistretta A (1986) Adenosine-induced bronchoconstriction: Comparison between nedocromil sodium and sodium cromoglycate. Eur J Respir Dis 69 [Suppl 147]: 258–262
Crimi N, Palermo F, Vancheri C, Oliveri R, Distefano SM, Polosa R, Mistretta A (1988a) Effect of sodium cromoglycate and nifedipine on adenosine-induced bronchoconstriction. Respiration 53: 74–78
Crimi N, Palermo F, Oliveri R, Vancheri C, Polosa R, Palermo B, Maccarrone C, Mistretta A (1988b) Comparative study of the effects of nedocromil sodium (4 mg) and sodium cromoglycate (10 mg) on adenosine-induced bronchoconstriction in asthmatic subjects. Clin Allergy 18: 367–374
Curtain C, Looney FD, Smelstorius J A (1981) Glycosphingolipid clustering and mast cell degranulation. Int Arch Allergy Appl Immunol 65: 34–41
Cushley MJ, Holgate ST (1985) Adenosine-induced bronchoconstriction in asthma: role of mast cell-mediator release. J Allergy Clin Immunol 75 (2): 272–27S
Cushley MF, Tattersfield AE, Holgate ST (1983) Inhaled adenosine and guanosine on airway resistance in normal and asthmatic subjects. Br J Clin Pharmacol 15, 161–165
Dahlen-S-E, Hansson G, Hedqvist P, Bjorck T, Granstrom E, Dahlen B (1983) Allergen challenge of lung tissue from asthmatics elicits bronchial contraction that correlates with the release of leukotrienes C4, D4, and E4. Proc Natl Acad Sci USA 80: 1712–1716
Davies SE (1968) Effect of disodium cromoglycate on exercise-induced asthma. Br Med J 3: 593–594
Davis B, Roberts AM, Coleridge HM, Coleridge JC (1982) Reflex tracheal gland secretion evoked by stimulation of bronchial C-fibers in dogs. J Appl Physiol 53: 985–991
Deal EC, Wasserman SI, Soter NA, Ingram RH, McFadden ER (1980) Evaluation of the role played by the mediators of immediate hypersensitivity in exercise-induced asthma. J Clin Invest 65: 659–665
Debelic M (1986) Nedocromil sodium and exercise-induced asthma in adolescents. Eur J Respir Dis 69 [Suppl 147]: 266–267
Del Bono L, Dente FL, Patalano F, Del Bono N (1986) Protective effect of nedocromil sodium and sodium cromoglycate on bronchospasm induced by cold air. Eur J Respir Dis 69 [Suppl 147]: 268–270
Del Bufalo D, Fasano L, Patalano F, Ruggieri F, Gunella G (1988) Prevention of non-specific bronchial hyperreactivity. Dose-dependent effect of sodium cromoglycate metered dose aerosol. Allergol Immunopathol (Madr) 16: 77–80
Delaney JC (1983) The effect of ketotifen on aspirin-induced asthmatic reactions. Clin Allergy 13: 247–251
Denjean A, Arnoux B, Lockhart A (1984) Modification of alveolar cell population after PAF-acether induced bronchoconstriction in baboons. Am Rev Respir Dis 129 [Suppl]: A3
Dewar A, Archer CB, Paul W, Page CP, MacDonald DM, Morley J (1984) Cutaneous and pulmonary histopathological responses to platelet activating factor ( Paf acether) in the guinea pig. J Pathol 144: 25–34
Diaz P, Galleguillos FR, Gonzalez MC, Pantin CF, Kay AB (1984) Bronchoalveloar lavage in asthma: the effect of disodium cromoglycate (cromolyn) on leukocyte counts, immunoglobulins, and complement. J Allergy Clin Immuol 74: 41–48
Dickson W (1970) A one year’s trial of Intal compound in 24 children with severe asthma. In: Pepys J, Frankland AW (eds) Disodium cromoglycate in allergic airways disease. Butterworths, London, p 105
Dixon M, Jackson DM, Richards IM (1979) The effects of sodium cromoglycate on lung irritant receptors and left ventricular cardiac receptors in the anaesthetized dog. Br J Pharmacol 67: 569–574
Dixon M, Jackson DM, Richards IM (1980) The action of sodium cromoglycate on ‘C’ fibre endings in the dog lung. Br J Pharmacol 70: 11–13
Dorward AJ, Roberts J A, Thomposn NC (1986) A preliminary report on the effect of riedocromil sodium on histamine airway responsiveness in patients allergic to grass pollen. Eur J Respir Dis 69 [Suppl 147]: 299–301
Durham SR, Carroll M, Walsh GM, Kay AB (1984) Leukocyte activation in allergen-induced late-phase asthmatic reactions. N Engl J Med 311: 1398–1402
Eady RP (1986) The pharmacology of nedocromil sodium. Eur J Respir Dis 61 [Suppl 147]: 112–119
Eady RP, Greenwood B, Jackson DM, Orr TSC, Wells E (1985) The effect of nedrocromil sodium and sodium cromoglycate on antigen-induced broncho-constriction in the Ascaris-sensitive monkey. Br J Pharmacol 85: 323–325
Easu S, del Carpio J, Martin JG (1984) A comparison of the effects of ketotifen and clemastine on cutaneous and airway reactivity to histamine and allergen in atopic asthmatic subjects. J Allergy Clin Immunol 74: 270 - 274
Fabbri LM, Mapp CE, Hendrick DJ (1983) Effect of cromolyn on carbachol-induced bronchoconstriction. Ann Allergy 50: 195–198
Fabbri LM, Aizawa H, Alpert SE, Walters EH, O’Bryne PM, Gold BD, Nadel JA, Holtzman MJ (1984) Airway hyperresponsiveness and changes in cell counts in bronchoalveolar lavage after ozone exposure in dogs. Am Rev Respir Dis 129: 288–291
Fink A, Bibi H, Eliraz A, Schlesinger M, Bentwich Z (1986) Ketotifen, disodium cromoglycate, and verapamil inhibit leukotriene activity: determination by tube leukocyte adherence inhibition assay. Ann Allergy 57: 103–106
Flint KC, Leung KBP, Pearce FL, Hudspith BN, Brostoff J, Johnson N Mcl (1985) Human mast cells recovered by bronchoalveolar lavage: their morphology, histamine release and the effects of sodium cromoglycate. Clin Sci 68: 427–432
Foreman JC, Garland LG (1976) Cromoglycate and other antiallergic drugs: a possilbe mechanism of action. Br Med J 1:820-821 Fuller RW, Collier JG (1984) Sodium cromoglycate and atropine block the fall in FEVi but not the cough induced by hypotonic mist. Thorax 39: 766–770
Fuller RW, MacDermot J (1986) Stimulation of IgE-sensitized human alveolar macrophages by anti-IgE is unaffected by sodium cromoglycate. Clin Allergy 16: 523–526
Garland LG (1973) Effect of cromoglycate on anaphylactic histamine release from rat peritoneal mast cells. Br J Pharmacol 49: 128–130
Garland LG, Hodson HF (1984) Antiallergic drugs. In: Dale MM Foreman JC (eds) Textbook of immuno-pharmacology. Blackwell, London, pp 265–28.
Garland LG, Mongar JL (1974) Inhibition by cromoglycate of histamine release from rat peritoneal mast cells indued by mixtures of dextran, phosphatidyl serine and calcium ions. Br J Pharmacol 50: 137–143
Garland LG, Mongar JL (1976) Differential histamine release by dextran and the ionophore A23187: the actions of inhibitors. Int Arch Allergy Appl Immunol 50: 27–42
Garland LG Green AF, Hodson HF (1979) Inhibitors of the release of anaphylactic mediators. In: Vane JR Ferreira SH (eds) Anti-inflammatory drugs. Springer, Berlin Heidelberg New York, pp 467–530
Godfrey S, Silverman M, Anderson SD (1973) Problems of interpreting exercise-induced asthma. J Allergy Clin Immunol 52: 199–209
Golden HW, Jacuzio DA, Otterness IG (1987) Inhibition of C5a-induced basophil degranulation by disodium cromoglycate. Agents Actions 21: 3–4
Graff-Lonnevig V, Hedlin G (1985) The effect of ketotifen on bronchial hyperreactivity in childhood asthma. J Allergy Clin Immunol 79: 59–63
Greenwood C (1982) The pharmacology of ketotifen. Chest 82:45S-48S Griffin MP, MacDonald N, McFadden ER (1983) Short-and long-term effects of cromolyn sodium on the airways reactivity of asthmatics. J Allergy Clin Immunol 71: 331–338
Gushchin IS, Zebrev AI (1986) Ketotifen-induced histamine release, inhibition of histamine secretion and modulation of immune response. Agents Actions 18: 92–95
Hachisuka H, Nomura H, Sakamoto F, Mori O, Okbo K, Sasai Y (1988) Effect of antianaphylactic agents on substance P-induced histamine release from rat peritoneal mast cells. Arch Dermatol Res 280: 158–162
Holroyde MC, Altounyan REC, Cole M, Dixon M, Elliot EV (1981) Bronchocon-striction produced in man by leukotriene C and D. Lancet ii: 17–18
Holtzman MJ, Fabbri LM, O’Bryne BD, Gold H, Aizawa EH, Walters SE, Aplert SE, Nadel JA (1983) Importance of airway inflammation for hyperresponsiveness induced by ozone. Am Rev Respir Dis 127: 686–690
Huston DP, Bressler RB, Kaliner M, Sowell LK, Baylor MW (1986) Prevention of mast-cell degranulation by ketotifen in patients with physical urticarias. Ann Intern Med 104: 507–510
Hutson PA, Holgate ST, Church MK (1988) The effect of cromolyn sodium and albuterol on early and late phase bronchoconstriction and airway leukocyte infiltration after allergen challenge of nonanesthetized guinea pigs. Am Rev Respir Dis 138: 1157–1163
Jackson DM (1988) The effect of nedocromil sodium, sodium cromoglycate and codeine phosphate on citric acid-induced cough in dogs. Br J Pharmacol 93: 609–612
Jackson DM, Eady RP (1986) Monkeys infected with Ascaris suum (a new in vivo model of airway disease): protective effect of nedocromil sodium and sodium cromoglycate against brochial antigen challenge. Eur J Respir Dis 69: [Suppl 147]: 202–205
Jackson DM, Eady RP (1988) Acute transient S02-induced airway hyperreactivity: effects of nedocromil sodium. J Appl Physiol 65: 1119–1124
Jackson DM, Richards IM (1977) The effects of sodium cromoglycate on histamine aerosol-induced reflex bronchoconstriction in the anaesthetized dog. Br J Pharmacol 61: 257–262
Jackson DM, Eady RP, Farmer JB (1986a) The effect of nedocromil sodium on non-specific bronchial hyperreactivity in the dog. Eur J Respir Dis 69 [Suppl 147]: 217–219
Joseph M, Tonnel, AB, Capron A, Dessaint JP (1981) The interaction of IgE antibody with human alveolar macrophages and its participation in the inflammatory processes of lung allergy. Agents Actions 11: 619–622
Joseph M, Capron A, Thorel T, Tonnel AB (1986) Nedocromil sodium inhibits JgE-dependent activation of rat macrophages and platelets as measured by schistosome killing, chemiluminscence and enzyme release. Eur J Respir Dis 69 [Suppl 147]: 220–222
Joseph M, Marquette CH, Lassalle P, Vorng H, Tonnel AB, Capron A (1988) Inhalation of nedrocromil sodium, but not of sodium cromoglycate, inhibits the abnormal in vitro responses to aspirin of platelets from aspirin-sensitive asthmatics. Am Rev Respir Dis 137: 29
Juniper EF, Latimer KM, Morris MM, Roberts RS, Hargreave FE (1986) Airway responses to hyperventilation of cold dry air: duration of protection by cromolyn sodium. J Allergy Clin Immunol 78: 387–391
Juniper EF, Kline PA, Morris MM, Hargreave FE (1987) Airway constriction by isocapic hyperventilation of cold, dry air: comparison of magnitude and duration of protection by nedocromil sodium and sodium cromoglycate. Clin Allergy 17: 523–528
Kakuta Y, Kato T, Sasaki H, Takishima T (1988) Effect of ketotifen on human alveolar macrophages. J Allergy Clin Immunol 81: 469–474
Karlsson G, Pipkorn U (1984) Effect of disodium cromoglycate on changes in nasal airway resistance induced by platelet activating factor. Eur J Clin Pharmacol 27: 371–373
Kato T, Tenii T, Tagami H (1985) Effects of HC 20-511 (ketotifen) on chemiluminesc-ence of human neutrophils. Inflammation 9: 45–51
Kay AB, Walsh GM, Moqbel R, MacDonal AJ, Nagakura T, Carroll MP, Richerson HB (1987) Disodium cromoglycate inhibits activation of human inflammatory cells in vitro. J Allergy Clin Immunol 80: 1–8
Kenakin TP (1987) Pharmacologic analysis of drug-receptor interaction. Raven, New York Kennedy JD, Hasham F, Clay MJD, Jones RS (1980) Comparison of actions of disodium cromoglycate and ketotifen on exercise-induced brochoconstriction in childhood asthma. Br Med J 281: 1458
Koenig JQ, Marshall SG, van Belle G, McManus MS, Bierman CW, Shapiro GG, Furukawa CT, Pierson WE (1988) Therapeutic range cromolyn dose-response inhibition and complete obliteration of S02-induced bronchoconstriction in atopic adolescents. J Allergy Clin Immunol 81: 897–901
Konig P, Hordvik NL, Kreutz C (1987) The preventive effect and duration of action of nedocromil sodium and cromolyn sodium on exercise-induced asthma ( EIA) in adults. J Allergy Clin Immunol 79: 64–68
Kraemer R, Sennhauser F, Reinhardt M (1987) Effects of regular inhalation of belcomethasone dipropionate and sodium cromoglycate on bronchial hyper-reativity in asthmatic children. Acta Paediatr Scand 76: 119–123
Laitinen LA, Venho K, Poppius H (1986) A controlled study on the effect of treatment with cromolyn sodium pressurized aerosol on bronchial reactivity in patients with asthma. Ann Allergy 56: 270–273
Latimer KM, O’Bryne PM, Morris MM, Roberts R, Hargreave FE (1983) Bronchoconstriction stimulated by airway cooling. Am Rev Respir Dis 128: 440–443
Leitch AG, Lumb EM, Kay AB (1984) Disodium cromoglycate relieves symptoms in symptomatic young smokers. Allergy 39: 211–215
Leung KBP, Flint KC, Brostoff J, Hudspith BN, Johnson NMcl, Pearce FL (1986) A comparison of nedocromil sodium and sodium cromoglycate on human lung mast cells obtained by bronchoalveolar lavage and by dispersion of lung fragments. Eur J Respir Dis 69 [Suppl 147]: 223–226
Lisboa C, Moreno R, Cruz E, Barja S, Sanchez I, Moran J, Ferretti R (1985) Acute effect of ketotifen on the dose-response curve of histamine and methacholine in asthma. Br J Dis Chest 79: 235–243
Loftus BG, Price JF (1987) Long-term, placebo-controlled trial of ketotifen in the management of preschool children with asthma. J Allergy Clin Immunol 79: 350–355
Loftus BG, Price JF, Heaton R, Costello JF (1985) Effects of ketotifen on in vitro bronchoconstricton. Clin Allergy 15: 465–471
Lowhagen O, Rak S (1985a) Modification of bronchial hyperreactivity after treatment with sodium cromoglycate during pollen season. J Allergy Clin Immunol 75: 460–467
Lowhagen O, Rak S (1985b) Bronchial hyperreactivity after treatment with sodium cromoglycate in atopic asthmatic patients not exposed to relevant allergens. J Allergy Clin Immunol 75 (3): 343–347
Lucas AM, Shuster S (1987) Cromolyn inhibition of protein kinase C activity. Biochem Pharmacol 36: 562–565
Martelli NA, Usandivaras G (1977) Inhibition of aspirin-induced bronchoconstriction by sodium cromoglycate inhalation. Thorax 32: 684–690
Martin U, Romer D (1978) The pharmacological properties of a new, orally active antianaphylactic compound: ketotifen, a benzocycloheptathiophene. Arzneimit-telforschung 28: 1–12
Mattoli S, Foresi A, Corbo GM, Polidori G, Ciappi G (1986) Protective effect of disodium cromoglycate on allergen-induced bronchoconstriction and increased hyperresponsiveness: a double-blind placebo-controlled study. Ann Allergy 57: 295–300
Mazurek N, Berger G, Pecht I (1980a) A binding site on mast cells and basophils for the anti-allergic drug cromolyn. Nature 286: 722–723
Mazurek N, Geller-Bernstein C, Pecht I (1980b) Affinity of calcium ions to the anti-allergic drug, dicromoglycate. FEBS Lett 111: 194–196
Mazurek N, Bashkin P, Pecht I (1982) Isolation of a basophilic membrance protein binding the anti-allergic drug cromolyn. EMBO J 1: 585–590
Mazurek N, Bashkin P, Loyter A, Pecht I (1983a) Restoration of Ca2+ influx and degranulation capacity of variant RBL-2H3 cells upon implantation of isolated cromolyn binding protein. Proc Natl Acad Sci USA 80: 6014–6018
Mazurek N, Bashkin P, Petrank A, Pecht I (1983b) Basophil variants with impaired cromoglycate binding do not respond to an immunological degranulation stimulus Nature 303: 528–530
Mazurek N, Schindler H, Schurolz T, Pecht I (1984) The cromolyn binding protein constitutes the Ca2+ channel of basophils opening upon immunological stimulus. Proc Natl Acad Sci USA 81: 6841–6845
Mazzoni L, Morley J, Page CP, Sanjar S (1985) Induction of airway hyperreactivity by platelet activating factor in the guinea pig. J Physiol (Lond) 365: 107 P
Medici TC, Radielovic P, Morley J (1989) Prophylactic treatment of extrinsic bronchial asthma: a multicentre controlled double-blind study. Eur Respir J 2 [Suppl 5]: 400s
Miller PD, Ainsworth D, Lam HF, Amdur MO (1988) Indomethacin and cromolyn sodium alter ozone-induced changes in lung function and plasma eiconsanoid concentrations in guinea pigs. Toxicol Appl Pharmacol 93: 175–186
Mitchell I (1985) Sodium cromoglycate-induced changes in the dose-response curve of inhaled methacholine in cystic fibrosis. Ann Allergy 54: 233–235
Moqbel R, Walsh GM, MacDonald AJ, Kay B (1986a) Effect of disodium cromoglycate on activation of human eosinophils and neutrophils following reversed (anti-IgE) anaphylaxis. Clin Allergy 16: 73–83
Moqbel R, Walsh GM, Kay AB (1986b) Inhibition of human granulocyte activation by nedocromil sodium. Eur J Respir Dis 69 [Suppl 147]: 227–229
Morley J, Sanjar S (1987) Isoprenaline induces increased airway reactivity in the guinea pig. J Phyiol (Lond) 390:180 Morley J Page CP, Mazzoni L, Sanjar S (1986) Effects of ketotifen upon responses to platelet activating factor: a basis for asthma prophylaxis. Ann Allery 56: 335–339
Morley J, Chapman ID, Sanjar S, Schaeublin E (1989) Actions of ketotifen on PAF-induced airway hyperreactivity in the anaesthetised guinea-pig. Br J Pharmacol 96: 76 P
Morley J, Sanjar S, Boubekeur K, Aoki S, Kristersson A (1981) Pharmacological evaluation of prophylactic anti-asthma drugs by reference to the pathological sequelae of exposure to allergen or platelet activating factor. Agents Actions 23 [Suppl]: 187–194
Morton AR, Fitch KD (1974) Sodium cromoglycate BP in the prevention of exercise-induced asthma. Med J Aust 2: 158–162
Myers DJ, Bigby BG, Boushey HA (1986a) The inhibition of sulfur dioxide-induced bronchoconstriction in asthamtic subjects by cromolyn is dose dependent. Am Rev Respir Dis 133: 1150–1153
Myers DJ Bigby BG, Calvayrac P, Sheppard D, Boushey HA (1986b) Interaction of cromolyn and a muscarinic antagonist in inhibiting bronchial reactivity to sulfur dioxide and to eucapnic hyperpnea alone. Am Rev Respir Dis 133: 1154–1158
Nadel JA, Salem H, Tamplin B, Tokiwa Y (1965) Mechanism of bronchoconstriction during inhalation of sulfur dioxide. J Appl Physiol 20: 164–167
Nemeth A, Magyar P, Herceg R, Huszti Z (1987) Potassium-induced histamine release from mast cells and its inhibition by ketotifen. Agents Actions 20: 149–152
Ottenhof M, Ufkes JGR Van Rooij HV. (1985) The effect of prednisolone and ketotifen on the antigen-induced bronchoconstriction and mediator release in rat isolated lungs. Br J Pharmacol 86: 627–636
Page CP, Guerreiro D, Sanjar S, Morley J (1985a) Platelet activating factor ( Paf-acether) may account for late-onset reactions to allergen inhalation. Agents Actions 16: 30–32
Page CP, Tomiak RHH Sanjar S, Morley J (1985b) Suppression of Paf-acether response: an anti-inflammatory effect of anti-asthma drugs. Agents Actions 16: 33–35
Page CP Mazzoni L, Sanjar S (1985c) Induction of non-specific hyperreactivity by platelet activating factor ( PAF) and its inhibition by anti-asthma drugs. Am Rev Respir Dis 131: A44
Papageorgiou N, Carrol M, Durham SR, Lee TH, Walsh GM, Kay AB (1983) Complement receptor enhancement as evidence of neutrophil activation after exercise-induced asthma. Lancet 2: 1220–1223
Patel KR, Wall T (1986) Dose-duration effect of sodium cromoglycate aerosol in exercise-induced asthma. Eur J Respir Dis 69: 256–260
Paterson JW, Yellin RH, Tarala RA (1983) Evaluation of ketotifen (HC20-511) in bronchial asthma. Eur J Clin Pharmacol 25: 187–193
Pauwels R, Van der Straeten M (1986) The effects of nedocromil sodium on adenosine-induced bronchoconstriction in rats. Eur J Respir Dis 69 [Suppl 147]: 235–237
Pauwels R Van Der Straeten M (1988) The effect of ketotifen on bronchial beta-adrenergic tachyphylaxis in normal human volunteers. J Allergy Clin Immunol 81: 674–680
Pearce FL (1983) Mast cell heterogeneity. TIPS 4: 165–167
Pearce FL, Truneh A (1981) Inhibition of histamine release from rat peritoneal mast cells treated with the ionophore A23187. Implications for the mode of action of anti-allergic compounds. Agents Actions 11: 44–50
Pearce FL, Rafii-Tabor E (1983) Inhibition by disodium cromoglygate of anaphylactic histamine secretion from rat peritoneal mast cells in the presence of phosphatidyl-serine. Agents Actions 13: 212–215
Pearce FL, Ali H, Barett KE, Befus AD, Bienenstock J, Brostoff J, Ennis M, Flint KC, Hudspith B, Johnson NM, Leung KBP, Peachell PT (1985) Functional characteristics of mucosal and connective tissue mast cells of man, the rat and other animals. Int Arch Allergy Appl Immunol 77: 274–276
Pepys J, Hargreave FE, Char M, McCarthy DS (1968) Inhibitory effects of disodium cromoglycate on allergen-inhalation tests. Lancet ii: 134
Phillips GD, Richards R, Scott VL, Holgate ST (1988) Sodium cromoglycate and nedrocromil sodium inhibit broncho-constriction provoked by adenosine 5’-monophosphate in atopic and non-atopic asthma. Am Rev Respir Dis 137:29 Phillips MJ, Meyrick Thomas RH, Moodley I, Davies RJ (1983) A comparison of the in vivo effects of ketotifen, clemastine, chlorpheniramine and sodium cromoglycate on histamine and allergen induced weals in human skin. Br J Clin Pharmacol 15: 277–286
Pichurko BM, McFadden ER, Frederick Bowman H, Solway J, Burns S, Dowling N (1984) Influence of cromolyn sodium on airway temperature in normal subjects. Am Rev Respir Dis 130: 1002–1005
Podleski WK, Panaszek BA, Schmidt JL, Burns RB (1984) Inhibition of eosinophil degranulation by ketotifen in a patient with milk allergy manifested as bronchial asthma-an electron microscopic study. Agents Actions 15: 177–181
Polson JB, Krzanowski JJ, Anderson WH, Szentivanyi A (1982) Effects of ketotifen, a benzocycloheptathiophene, on methacholine-and acetylcholine-induced contractions of canine respiratory smooth muscle. Immunopharmacology 4: 69–72
Rackham A, Brown CA, Chandra K, Ho P, Hoogerwerf PE, Kennedy RJ, Knight A, Langer H, Milne J, Moote DW, Nickerson GN, Rosen L, Stephenson H, Broadhead M, Lalonde Y, St Pierre JP (1989.) A Canadian multicenter study with Zaditen (ketotifen) in the treatment of bronchial asthma in children age 5–17 years. J Allergy Clin Immunol 84(3):286–296
Rafferty P, Fergusson RJ, Tweedale PM, Biggs BA, Grant IWB (1985) Effects of verapamil and sodium cromoglycate on bronchoconstriction induced by isocapnic hyperventilation. Clin Allergy 15: 531–534
Rafferty P, Tweedale PM, Ferguson RJ, Biggs BA,Grant IWB (1987) Does regular treatment with ketotifen inhibit broncho-constriction induced by isocapnic hyperventilation? Br J Clin Pharmacol 24: 100–102
Read GW, Knoohuizen M, Goth A (1977) Relationship between phosphatidylserine and cromolyn in histamine release. Eur J Pharmacol 42: 171–177
Rengo F, Trimarco B, Ricciardelli B, Volpe M, Violini R, Sacca L, Chiariello M (1979) Effects of disodium cromoglycate on hypoxic pulmonary hypertension in dogs. J Pharmacol Exp Ther 211: 686–689
Reinhardt D, Ludwig J, Braun D, Kusenbach G, Griese M (1988) Effects of the antiallergic drug ketotifen on bronchial resistance and beta-adrenoceptor density of lymphocytes in children with exercise-induced asthma. Dev Pharmacol Ther 11: 180–188
Richards IM, Dixon M, Jackson DM, Vendy K (1986) Alternative modes of action of sodium cromoglycate. Agents Actions 18: 3–4
Roberts J A, Rodger IW, Thompson NC (1986) Effect of verapamil and sodium cromoglycate on leukotriene D4 induced bronchoconstriction in patients with asthma. Throax 41: 753–758
Robertson DN, Page CP (1987) The effect of platelet agonists on intrathoracic platelet accumulation and airways hyperresponsiveness. Br J Pharmacol 92: 105–112
Ryo UY, Bann K, Townely RG (1976) Cromolyn therapy in patients with bronchial asthma. JAMA 236: 927–931
Sagi-Eisenberg R (1985) Possible role for a calcium-activated, phospholipid-dependent protein kinase in mode of action of DSCG. TIPS 6: 198–200
Sanjar S, Smith D, Kristersson A (1989) Incubation of platelets with PAF produces a factor which causes airway hyperreactivity in guinea-pigs. Br J Pharmacol 96: 75 P
Shaw RJ, Kay AB (1986) Nedocromil sodium, a mucosal and connective tissue mast cell stabilizer, inhibits exercise-induced asthma. Eur J Respir Dis 69 [Suppl 147]: 294–296
Sheppard D, Scott Wong W, Uehara CF, Nadel JA, Boushey HA (1980) Lower threshold and greater bronchomotor responsiveness of asthmatic subjects to sulfur dioxide. Am Rev Respir Dis 122: 873–878
Sheppard D, Nadel JA, Boushey HA (1981) Inhibition of sulfur dioxide-induced bronchoconstriction by disodium cromoglycate in asthmatic subjects. Am Rev Respir Dis 124: 257–259
Skedinger MC, Augustine NH, Morris EZ, Nielson DW, Zimmerman GA, Hill HR (1987) Effect of disodium cromoglycate on neutrophil movement and intracellular calcium mobilization. J Allergy Clin Immunol 80: 573–577
Smith D, Sanjar S, Morley J (1989) Platelet activation and PAF-induced airway hyperreactivity in the anaesthetised guinea-pig. Br J Pharmacol 96:74P Spry CJF, Kumaraswami V, Tai P-C (1986) The effect of nedocromil sodium on secretion from human eosinophils. Eur J Respir Dis 69 [Suppl 147]: 241–243
St Pierre JP, Kobric M, Rackham A (1985) Effect of ketotifen treatment on cold-induced urticaria. Ann Allergy 55: 840–843
Stafford WP, Mansfield LE, Yarbrough J (1984) Cromolyn modifies histamine bronchial reactivity in symptomatic seasonal asthma. Ann Allergy 52: 401–405
Suschitzky JL, Sheard P (1984) The search for antiallergic drugs for the treatment of asthma-problems in finding a successor to sodium cromoglycate. Prog Med Chem 21: 1–61
Szczeklik A, Serwonska M (1979) Inhibition of idiosyncratic reactions to aspirin in asthmatic patients by clemastine. Thoiax 34: 654–657
Tamura G, Mue S, Takishima T (1986) Protective effect of ketotifen on allergen-induced bronchoconstriction and skin weal. Clin Allergy 16: 535–541
Tan WC, Crip E, Douglas N, Sudlow MF, (1982) Protective effect of drugs on bronchoconstriction induced by sulphur dioxide. Thorax 37: 671–676
Tan WC, Lim TK (1987) Double-blind comparison of the protective effect of sodium cromoglycate and ketotifen on exercise-induced asthma in adults. Allergy 42: 315–317
Theoharides TC, Sieghart W, Greengard P, Douglas WW (1980) Antiallergic drug cromolyn may inhibit histamine secretion by regulating phosphorylation of a mast cell protein. Science 207: 80–82
Thompson NC, Roberts J A (1986) Nedocromil sodium attenuates exercise-induced asthma. Eur J Respir Dis 69 [Suppl 147]: 297–298
Tinkleman DG, Moss BA, Bukantz SC, Sheffer AL, Dobken JH, Chodosh S, Cohen BM, Rosenthal RR, Rappaport I, Buckley CE, Chusid EL, Deutsch AJ, Settipane GA, Burns RBP (1985) A multicentre trial of the prophylactic effect of ketotifen, theophylline, and placebo in atopic asthma. J Allergy Clin Immunol 76: 487–497
Tjwa MKT, Smeets J, Maesen F (1986) Ketotifen and methacholine-induced bronchospasm. Allergy 41: 551–555
Truneh A, Pearce FL (1984) Effect of cyclic AMP, disodium cromoglycate and other antiallergic drugs on histamine secretion from rat mast cells stimulated with the calcium ionophore ionomycin. Agents Actions 14: 179–184
Truneh A, White JR, Pearce FL (1982) Effect of ketotifen and oxatomide on histamne secretion from mast cells. Agents Actions 12: 206–209
Tsicopoulos A, Lassale P, Joseph M, Tonnel AB, Thorel T, Dessaint JP, Capron A (1988) Effect of disodium cromoglycate on inflammatory cells bearing the Fc epsilon receptor type II ( Fc epsilon RII ). Int J Immunopharmacol 10: 227–236
Van den Brink FG (1973a) The model of functional interaction. 1. Development and first check of a new model of functional synergism and antagonism. Eur J Pharmacol 22: 270–278
Van den Brink FG (1973b) The model of functional interaction. II. Experimental verification of a new model: the antagonism of P-adrenoceptor stimulants and other agonists. Eur J Pharmacol 22: 279–286
Vargaftig BB, Lefort J, Chignard ML (1980) Platelet activating factor induces a platelet-dependent bronchoconstriction unrelated to the formation of prostaglandin derivatives. Eur J Pharmacol 65: 185–192
Vargaftig BB, Lefort J, Wal F, Chignard M, Medeiros MC (1982) Nonsteroidal anti-inflammatory drugs if combined with anti-histamine and anti-serotonin agents interfere with the bronchial and platelet effects of platelet activating factor ( Paf-acether ). Eur J Pharmacol 80: 212–230
Wells A Taylor B (1979) A placebo-controlled trial of ketotifen (HC 20-511, Sandoz) in allergen induced asthma and comparison with disodium cromoglycte. Clin Allergy 9: 237–240
Wells E, Jackson CG, Harper ST, Mann J, Eady RP (1986) Characterization of primate bronchoalveolar mast cells. J Immunol 137: 3941–3945
Wells E, Mann J (1983) Phosphorylation of a mast cell protein in response to 290 treatment with anti-allergic compounds. Biochem Pharmacol 32: 837–842
White JR, Pearce FL (1983) Effects of anti-allergic and cyclic AMP-active drugs on histamine secretion from rat mast cells treated with the novel calcium ionophore chlortetracycline. Int Arch Allergy Appl Immunol 71: 352–356
White JR, Ishizaka T, Ishizaka K, Sha’Afi RI (1984) Direct demonstration of increased intracellular concentration of free calcium as measured by quin-2 in stimulated rat peritoneal mast cell. Proc Natl Acad Sci USA 81: 3978–3982
Woenne R, Kattan M, Levison H (1979) Sodium cromoglycate-induced changes in the dose-response curve of inhaled methacholine and histamine in asthmatic children. Am Rev Respir Dis 119: 927–932
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1991 Springer-Verlag Berlin Heidelberg
About this chapter
Cite this chapter
Garland, L.G. (1991). Pharmacology of Prophylactic Anti-Asthma Drugs. In: Page, C.P., Barnes, P.J. (eds) Pharmacology of Asthma. Handbook of Experimental Pharmacology, vol 98. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-75855-3_9
Download citation
DOI: https://doi.org/10.1007/978-3-642-75855-3_9
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-642-75857-7
Online ISBN: 978-3-642-75855-3
eBook Packages: Springer Book Archive