References

pulmo

Пульмонология

PULMONOLOGIYA

0869-01892541-9617

Scientific and Practical Journal “PULMONOLOGIYA” LLC

pulmo-2775

Research Article

ОРИГИНАЛЬНЫЕ ИССЛЕДОВАНИЯ

ORIGINAL STUDIES

Форадил и его место в терапии бронхиальной астмы

Foradil and its place in bronchial asthma therapy

Калманова

Е. Н.

Kalmanova

E. N.

Айсаиов

З. Р.

Aisanov

Z. R.

НИИ пульмонологии М3 РФРоссияНИИ пульмонологии М3 РФRussian Federation

2001

30032001

016572

2001

Калманова Е.Н., Айсаиов З.Р.

Kalmanova E.N., Aisanov Z.R.

Данная работа распространяется под лицензией Creative Commons Attribution 4.0.

This work is licensed under a Creative Commons Attribution 4.0 License.

https://journal.pulmonology.ru/pulm/article/view/2775

Формотерола фумарат в форме Форадила является самым распространенным и хорошо изученным пролонгированным ß2-агонистом, представленным сегодня на мировом фармацевтическом рынке. В настоящем обзоре обсуждены особенности как самого активного вещества, так и его сравнение с другими ß2-агонистами, а также сравнительный анализ средств доставки. Для того, чтобы определить место препарата в современном спектре антиастматических и бронходилатационных средств, рассмотрены его специфические характеристики как препарата, являющегося представителем своего класса. Приведены данные исследований, демонстрирующих уникальное сочетание фармакологических свойств формотерола: высокая эффективность в сочетании с высокой ß2-селективностью; высокая внутренняя активность; быстрое начало действия; продолжительность эффекта. Изложена гипотеза промежуточной липофильности, объясняющая уникальность сочетания фармакологических свойств формотерола по сравнению с чисто липофильными агентами, такими как сальметерол.

Имеющиеся на сегодняшний день данные свидетельствуют о том, что формотерол (Форадил) является наиболее оптимальным и универсальным (с точки зрения быстроты и продолжительности действия) бронхорасширяющим препаратом, который может применяться и как симптоматическое средство у больных бронхиальной астмой легкого течения, и как препарат первой линии для контроля течения заболевания и предотвращения ночных приступов бронхиальной астмы, а также в качестве профилактического средства для предотвращения бронхоспазма, вызванного различными триггерами. Сочетанное применение препарата с ингаляционными средствами признано наиболее эффективной комбинацией в большинстве современных руководств по лечению тяжелой бронхиальной астмы.

Today formoterol fumarat (Foradil) is the most well-known long-acting ß2-agnist worldwide. This review discusses characteristic features of the active substance, its comparison with other ß2-agonists and its delivery as well. Specific pharmacologic characteristics of the drug are viewed to determine its place in the modern spectrum of antiasthmatic and bronchodilating medications. Study results demonstrating unique pharmacologic properties of formoterol are given: high effectiveness together with high ß2-selectivity; high intrinsic activity; rapid starting the action; the effect duration. An intermediate lipophylity hypothesis is reported to explain the unique combination of formoterol pharmacologic properties compared with clear lipophylic agents, such as salmeterol.

Recent data evidence that formotero! (Foradil) is the most optimal and universal (in terms of the action rate and duration) bronchodilating drug which can be used as symptomatic means in mild bronchial asthma patients and as the first-line therapy for asthma control and nighttime attacks prevention, and as a preventing drug for bronchospasm development caused by different triggers. A joined application of the formoterol and inhaled medications is proved to be the most effective combination and is recommended by the majority of modern guidelines for severe asthma management.

References1

Anderson G.P., Linden A., Rabe K.F. Why are long-acting betaadronoceptor agonists long-acting? Eur. Respir.J. 1994; 7: 569-578.

Anderson G.P. Formoterol: pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective ß2-adrcnoceptor agonist bronchodilator. Life Sei. 1993; 52: 2145-2160.

Arvidsson P., Larsson S., Lirfdahl C.G. et al. Formoterol, a new long-acting bronchodilator for inhalation. Eur. Respir. J. 1989; 2: 25-30.

Bhagat R., Kaira S., Swystun V.A., Gockroft D.W. Rapid onset of tolerance to the broncho-protective effect of salmeterol. 1995; 108: 1235-1239.

Bhagat R., Swystun V.A., Cockroft D.W. Salbutamol-induced increased airway responsiveness to allergen and reduced protection versus methacholine: dose response. J. Allergy Clin. Immunol. 1996; 97: 47-52.

Booth, H., Bish R., Walters J. et al. Salmeterol tachyphylaxis in steroid treated asthmatic subjects. Thorax 1996; 51: 1100-1104.

Boulet L.P., Cartier A., Thompson N.C. et al. Asthma and increases in non-allergic bronchial responsiveness from seasonal pollen exposure. J. Allergy Clin. Immunol. 1983; 71: 399-406.

Cazzola M., Matera M.G., Santangelo G. et al. Salmeterol and formoterol in partially irreversible sever chronic obstructive pulmonary disease: dose-response study. Respir. Med. 1995; 89: 357-362.

Cockroft D.W., McPharland C.P., Britto S.A., Swystun V.A. Regular inhaled salbutamol and airway responsiveness to allergen. Lancet. 1993; 342: 833-836.

Cockroft D.W., Killian D.N., Mellon J.J.A., Hargreave F.E. Bronchial reactivity to histamine: a method and clinical survey. Clin. Allergy. 1977; 7: 235-243.

Derom E.Y., Pauwels R.A. Time course of bronchodilating effect of inhaled formoterol, a potent and long-acting sympathomimelic. Thorax. 1992; 47: 30-33.

Derom E.Y., Pauwels R.A., Van der Straeten M.E.F. The effect of inhaled salmeterol on methacholine responsiveness in subjects with asthma up to 12 hours. J. Allergy Clin. Immunol. 1992; 89: 811-815.

Di Bartolio C.G, Gonzalez J.G, Ruggieri M.P et al. Evaluation of the effectiveness and acceptability of Foradil® Aerolizer™ and Oxis Turbuhaler® in asthmatics. In: Program and abstracts of the 96th International conference of the American thoracic society. Toronto, Ontario, Canada; 2000. Session A21.

Djukanovic R., Feather I., Gratiziou C. et al. Effect of natural allergen exposure during the grass pollen season on inflammatory cells and asthma symptoms. Thorax 1996; 51: 575-581.

Esmailpour N., Hogger P., Rabe K.F. et al. Distribution of inhaled fluticasone propionate between human lung tissue and serum in vivo. Eur. Respir. J. 1997; 10: 1496-1499.

Fitzgerald J.M., Chapman K.R., Delia Doppa G. et al. Sustained bronchoprotection, bronchodilatation, and symptom control during regular formoterol use in asthma of moderate or greater severity. The Canadian FO/OD1 Study Group. J. Allergy Clin. Immunol. 1999; 103: 427-435.

Grainger J., Woodman K., Pearce N. et al. Prescribed fenoterol and death from asthma in New Zealand, 1981-7: a further casecontrol study. Thorax. 1991; 46: 105-111.

Gronnerod T.A., Hamre H.S., Oepen G., von Berg A. Protective effect of single doses of formoterol Turbuhaler® 4.5 ug and 9 ug in children with exercise-induced broncho-constriction. Am. J. Respir. Crit. Care Med. 1999; 159(S3, pt2): A858.

Hacki M.A., Hinz G.W., Medici T.C. Clinical experience over five years of daily therapy with formoterol in patients with bronchial astlima. Clin. Drug Invest. 1997; 14: 165-174.

Ind P., Boszormeny Nagy G., Pietinalho A. et al. Formoterol, 4.5 ng, used as-needed via Turbuhaler was as safe and well tolerated as terbutaline 0.5 mg. Eur. Respir. J. 1999; 14(suppl.30): 148s.

Inman M.D., Hamilton A.L., Kerstjens H.A.M. et al. The utility of methacholine airway responsiveness measurements in evaluating anti-asthma drugs. J. Allergy Clin. Immunol. 1998; 101: 342-348.

Jadad A.R, Molier M., Browman G.P. et al. Systematic reviews and meta-analyses on treatment of asthma: critical evaluation. Br. Med. J. 2000; 320: 537-540.

Jeppsson A.B., Kdllstrym B.L., B. Waldeck. Studies on the interaction between formoterol and salmeterol in guinea-pig trachea in vitro. Pharmacol. Toxicol. 1992; 71: 272-277.

Kdllstrym B.L., Sji{berg J., Waldeck B. The interaction between salmeterol and p2-adrenoceptor agonists with higher efficacy on guinea-pig trachea and human bronchus in vitro. Br. J. Pharmacol. 1994; 113: 687-692.

Kips K.C., O’Connor B.J., Inman K. et al. A long-term study of the antiinflammatory effect of low-dose budesonide plus formotel versus high-dose budesonide in asthma. Am. J. Respir. Crit. Care Med. 2000; 161: 996-1001.

Linden, A., Bergendal A., Ullman A. et al. Salmeterol, formoterol, and salbutamol in the isolated guinea-pig trachea: differences in maximum relaxant effect and potency but not in functional antagonism. Thorax . 1993; 48: 547-553.

Lipworth B., Tan S., Devlin M. et al. Effects of treatment with formoterol on bronchoprotection against, methacholine. Am. J. Med. 1998; 104: 431-438.

L y fd a h l C.-G., S v edm y r N. Formoterol fumarate, a new p2 adrenocept agonist. Allergy. 1989; 44: 264-271.

Lytvall J, Mellen A, Arvidsson P. et al. Similar bronchodilation with formoterol delivered by Aerolizer or Turbuhaler. Can. Respir. J. 1999; 6: 412-416.

Lotvall J, Persson G, Larsson P., et al. Tolerahility of inhaled high doses of formoterol and salbutamol in asthmatic patients maintained on twice daily formoterol 12 micrograms (9 micrograms delivered). Eur. Respir. J. 1997; 10(suppl.25): 103s.

Lótvall J., Inman M., O’Byrne P.M. Measurement of airway hyperresponsiveness: new considerations. Thorax. 1998; 53: 419-424.

Maconochie J.G., Forster J.K. Dose-response study with highdose inhaled salmeterol in healthy subjects. Br. J. Clin. Pharmacol. 1992; 33: 342-345.

Madolepszy J., Boszormeny Nagy G., BranderR., Larsson P. Formoterol 90 mg via Turbuhaler was safe in patients with acute bronchoconstriction. Eur. Respir. J. 1998; 12(Suppl.28): 323s.

Maesen F.P.V., Smeets J.J., Gubbelmans H.L.L., Zweers P.G.M.A. Bronchodilator effect of inhaled formoterol vs salbutamol over 12 hours. Chest 1990; 97:590-594.

Maesen F.P.V., Costongs R., Smeets J.J. et al. The effect of maximal doses of formoterol and salbutamol from a metered dose inhaler on pulse rates, ECG, and serum potassium concentrations. Ibid. 1991; 99: 1367-1373.

Mak J.C., Grandordy B, Barnes P.J. High affinity [3H] formoterol binding sites in lung:characterization and autoradiographic mapping. Eur. J Pharmacol. 1994; 269: 35-41.

Molimard M., Naline E., Zhang Y. et al. Long- and shortadrenoceptor agonists: interactions in human contracted bronchi. Eur. Respir. J. 1998; 11: 583-588.

Mullen M., Mullen B., Carey M. The association between betaagonist use and death from asthma. A meta-analytical integration of case-control studies. JAMA. 1993; 270: 1842-1845.

Naline E., Zhang Y., Qian Y. et al. Relaxant effects and durations of action of formoterol and salmeterol on the isolated human bronchus. Eur Respir J. 1994; 7: 914-920.

National Heart, Lung, and Blood Institute, National Institutes of Health, World Health Organization. Global initiative for asthma. Pocket guide for asthma management. Bethesda: NIH/NHLBI, 1998. publication number 96-3659B.

Nightingale J.A., Rogers D.F., Barnes P.J. Comparison of the effects of salmeterol and formoterol in patients with severe asthma. Am. J. Respir. Crit. Care Med. 2000; 161: A190.

Nightingale J.A., Rogers D.F., Barnes PJ. Differential effect of formoterol on adenosine monophosphate and histamine reactivity in asthma. Ibid. 1999; 159: 1786-1790.

O’Connor B.J., Alkinan S.L., Barnes P.J. Tolerance to the nonbronchodilator effects of inhaled p2-agonists in asthma. N. Engl. J. Med. 1992; 327: 1204-1208.

Palmqvist М., Ibsen Т., Mellen A., Lotvall J. Comparison of the relative efficacy of formoterol and salmeterol in asthmatic patients. Am. J. Respir. Crit. Care Med. 1999; 160: 244-249.

Palmqvist М., Persson G., Lazer L. et al. Inhaled dry powder formoterol and salmeterol in asthmatic patients: onset of action, duration of effect and potency. Eur. Respir. J. 1997; 10: 2484-2489.

Pearce N., Beasley R., Crane J. et al. End of the New Zealand asthma mortality epidemic. Lancet. 1995.; 345: 41-44.

Pauwels R.A., L y fd a h l C.G., Postma D.S. et al. Effect of inhaled formoterol and budesonide on exacerbations of asthma. N. Engl. J. Med. 1997; 337: 1405-1411.

Politiek M.J., Boorsma М., Aalbers R. Comparison of formoterol, salbutamol and salmeterol in methacholine-induced severe bronchoconstriction. Eur. Respir. J. 1999; 13: 988-992.

Postma D.S., Lyfdahl C.G., Tattersfield A. et al. Formoterol used on demand improves quality of life in patients with asthma. Ibid 14(suppl.30): 4s.

Rabe K.F., Jyrres R., Nowak D. et al. Comparison of the effects of salmeterol and formoterol on airway tone and responsiveness over 24 hours in bronchial asthma. Am. Rev. Respir. Dis. 1993; 147: 1436-1441.

Ramsdale E.H., Otis J., Kline P.A. et al. Prolonged protection against methacholine-induced bronchoconstriction by the inhaled p2-agonist formoterol. Ibid 1991; 143: 998-1001.

Ryan G., Latimer K.M., Dolovich J., Hargreave F.E. Bronchial responsiveness to histamine: relationship to diurnal variation of peak flow rate, improvement after bronchodilator and airway calibre. Thorax. 1982; 37: 423-439.

Smyth E.T., Pavord I.D., Wong C.S. et al. Interaction and dose equivalence of salbutamol and salmeterol in patients with asthma. Br. Med. J. 1993; 306: 543-545.

Sterk P.J., Fabbri L.M., Quanjer P.H. et al. Airway responsiveness: standardized challenge testing with pharmacological, physical and sensitizing stimuli in adults. Eur. Respir. J. 1993; 6(suppl.l6): 53-83.

Tattersfield A., Lyfdahl C.G., Postma D.S. et al. On demand treatment,: comparison of formoterol and terbutaline in moderate asthma. Ibid. 1999; 14(suppl.30): 4s.

The British Guidelines on Asthma Management. Thorax. 1997; 52(suppl.l) 1-20.

Tokuyama K., Lotvall J., Lyfdahl C.G. et al. Inhaled formoterol inhibits histamine-induced airflow obstruction and airway microvascular leakage. Eur. J. Pharmacol. 1991; 193: 35-39.

Torphy T.J., Rinard G.A., Rietow M.G., Mayer G.E. Functional antagonism in canine tracheal smooth muscle: inhibition by methacholine of the mechanical and biochemical responses to isoproterenol. J. Pharmacol. Exp. Ther. 1983; 227: 694-699.

Ullman A., Svedmyr N. Salmeterol, a new long-acting inhaled p2-adrenoceptor agonist: comparison with salbutamol in asthmatic patients. Thorax. 1990; 43: 998-1001.

Ulrik C.S., Kok-Jensen A. Different bronchodilating effect of salmeterol and formoterol in an adult asthmatic. Eur Respir J. 1994; 7: 1003-1005.

Van Noord J.A., Smeets J.J., Raaijmakcrs J.A. et al. Salmeterol versus formoterol in patients with moderately severe asthma: onset, and duration of action. Ibid. 1996; 9: 1684-1688.

Wallin A., Sandstrom Т., Soderberg M. et al. The effects of regular inhaled formoterol, budesonide, and placebo on mucosal inflammation and clinical indices in mild asthma. // Am. J. Respir. Crit. Care Med. 1999; 159: 79-86.

Yates D.H., Sussman H.S., Shaw M. et al. Regular formoterol treatment in mild asthma: effect on bronchial responsiveness during and after treatment. Ibi

The authors declare that there are no conflicts of interest present.