Double-Blind Comparison of Astemizole, Terfenadine and Placebo in Hay Fever with Special Regard to Onset of Action

Girard, Jean Pierre; Sommacal-Schopf, D; Bigliardi, P; Henauer, S.

doi:10.1177/030006058501300205

Cited by 24 publications

(9 citation statements)

References 7 publications

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“…In this study both the plain terfenadine preparation and the terfenadine-phenylpropanolamine combination relieved nasal symptoms. Girard et al [9] compared astemizole. terfenadine and placebo in hay fever with special attention to the onset of action.…”

Section: Discussionmentioning

confidence: 99%

Terfenadine with or without phenylpropanolamine in the treatment of seasonal allergic rhinitis

Nuutinen

Holopainen

Malmberg

et al. 1989

Clin Experimental Allergy

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The efficacy of terfenadine in combination with phenylpropanolamine was assessed by comparison with terfenadine alone in a double-blind, parallel group study of 66 patients with nasal birch pollen allergy. The patients were allocated randomly into two groups; 34 patients received terfenadine (60 mg) twice daily and 32 patients a combination tablet containing terfenadine (60 mg) and phenylpropanolamine (50 mg) twice daily for 17 days during the birch pollen season. Nasal symptoms (sneezing, discharge, itching and blockage) were relieved significantly by both drugs, but control of symptoms was more rapid and better with the terfenadine-phenylpropanolamine combination. Rhinoscopic evaluation of nasal secretion and mucosal swelling showed no differences between the treatment groups. Compared with pre-season values, nasal peak expiratory flow (PEF)-values worsened significantly during the season in the terfenadine, but not in the terfenadine-phenylpropanolamine, group. The general condition of the patients was significantly better in the terfenadine-phenylpropanolamine group. There were no marked side-effects in either group. At the end of the trial some of the patients in both treatment groups still had symptoms; this is apparently due to the long-lasting and severe pollen season. It is concluded that terfenadine combined with phenylpropanolamine gives better control of seasonal allergic rhinitis than terfenadine alone.

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Section: Discussionmentioning

confidence: 99%

Terfenadine with or without phenylpropanolamine in the treatment of seasonal allergic rhinitis

Nuutinen

Holopainen

Malmberg

et al. 1989

Clin Experimental Allergy

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“…This metabolite is cleared at only 1/10th the rate of astemizole. Clinically, it may take two days following a dose of astemizole for symptom alleviation to occur in the treatment of hay fever (134). However, the effect is very long lasting: after a single 10-mg tablet, significant antihistaminic activity can be demonstrated in volunteers for about 20 days (135).…”

Section: Antihistaminesmentioning

confidence: 99%

“…Oral terfenadine has a relatively rapid onset (134), and a sufficiently long duration of action that it needs to be dosed only once or twice a day. Clinical studies show: it effectively blocks histamine-induced bronchospasm (124); it causes modest bronchodilation (139,140); and it provides limited protection against either exerciseinduced asthma (140,141) or challenge using nebullized water (139).…”

Section: Antihistaminesmentioning

confidence: 99%

Antiasthmatic Agents

Bernstein¹

2000

Kirk-Othmer Encyclopedia of Chemical Technology

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Asthma is an extremely complex condition characterized by variable and reversible airways obstruction combined with nonspecific bronchial hypersensitivity. Asthma affects 3–5% of the population and is one of the most common chronic illnesses. Clinically, there are several ways of classifying asthma, and treatment varies depending upon the classification. In extrinsic asthma, also called allergic asthma, experienced by adults and, most commonly, by children, it is possible to demonstrate specific causal agents, usually antigens, eg, animal danders, foods, drugs, house dust, pollens, or mold spores. Intrinsic asthma, also called idiopathic asthma, usually develops in adulthood; allergic factors are not demonstrable in intrinsic asthma. Episodes may be triggered by a variety of stimuli, eg, emotional state, exposure to cold air, or inert dusts. Both intrinsic and extrinsic asthmatics can be prone to exercise‐induced attacks. Individuals who experience a combination of extrinsic and intrinsic asthmatic reactions have mixed asthma. Current asthma treatments are not curative and historically have relied on pharmacologic intervention with bronchodilators. More recently the focal points of both treatment and research efforts have shifted from bronchodilators to agents which reduce the underlying inflammatory state. Management of extrinsic asthma usually includes manipulation of the patient's environment to minimize or completely eliminate the causal agent. Improvements in asthma treatment include the development of more effective, safer formulations of known drugs. Also, the use of reliable sustained release formulations has revolutionized the use of oral xanthines which have a very narrow therapeutic index. For many individuals, asthma symptoms tend to worsen at night and the inhaled bronchodilators do not usually last through an entire night's sleep. β 2 ‐Agonists are widely used in the symptomatic treatment of asthma. Although both oral and aerosol formulations of these bronchodilators have been available for many years, advances have occurred in delivery technology with the development of dry powder aerosols. Nonselective β‐agonists can produce many undesirable side effects. Some selectivity in action was needed. Isoproterenol is a selective agonist at the β receptor. Aerosol administration of isoproterenol produces a prompt (2–5 min) intense bronchodilatation of relatively short (1‐h) duration, and has been widely used for many years. A significant advance in β‐agonist therapy occurred with the discovery of metaproterenol, C 11 H 17 NO 3 , which has a longer (4‐h) duration of action. Terbutaline, C 12 H 19 NO 3 , is an orally active agent having a duration of action of from 6–7 h. Terbutaline has about six times the selectivity of isoproterenol and is claimed to produce fewer side effects. Albuterol, C 13 H 21 NO 3 , also called salbutamol, is the most widely prescribed β 2 ‐agonist for either aerosol or oral administration both in the United States and worldwide. There are several longer acting agents currently under clinical evaluation, eg, bitolterol, C 28 H 31 NO 5 ; clenbuterol, C 12 H 18 Cl 2 N 2 O; and salmeterol, C 25 H 37 NO 4 . For many years oral xanthines were the preferred first‐line treatment for asthma in the United States. Within this class of compounds theophylene, ie, 1,3‐dimethylxanthine, is one member of a class of naturally occurring alkaloids. Common side effects of theophylline therapy for asthma include headache, dyspepsia, and nausea. More serious side effects can occur if blood levels are too high. Many derivatives of theophylline have been prepared. However, the most universal solution has resulted from the development of reliable sustained‐release formulations. The effectiveness of theophylline in the treatment of asthma seems to result from a combination of biological properties not clearly understood. Its predominant mode of action appears to be bronchodilation. Although the benefit of theophylline treatment is without question, its use is decreasing. Steroids use for the preventative treatment of asthma appears to be increasing, because of the identification of asthma as an inflammatory disease. It is known that steroids bind to cytosolic receptors. The steroid–receptor complex then enters the cell nucleus where the complex acts at specific sites and affects protein synthesis. The effect is to reduce the inflammatory response. While disodium chromoglycate (DSCG), C 23 H 14 Na 2 O 11 , enjoys modest success as a preventative antiasthmatic agent, it has never achieved the same level of popularity in the United States as in other markets, eg, the United Kingdom. Although it is considered one of the safest available antiasthmatic agents, it seems to work best as an adjunct to other therapy. The beneficial effect of atropine, used for centuries, is in preventing exercise‐induced asthma; it and other anticholinergic agents have no effect on bronchial hyperresponsiveness, the release of other mediators, or on the inflammatory process. Ipratropium bromide, C 20 H 30 BrNO 3 , a newer anticholinergic agent, seems to be useful in patient populations that show limited response to β 2 ‐adrenergic agonists.

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“…12. [30][31][32][33] Increased weight usually has been associated with an increase in appetite. Similar effects have also been reported with cyproheptadine, an antihistamine with antiserotonin activity.…”

Section: Adverse Effects and Drug Interactionsmentioning

confidence: 99%

Astemizole: A Long-Acting, Nonsedating Antihistamine

Krstenansky

Cluxton²

1987

Drug Intelligence & Clinical Pharmacy

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Astemizole is a long-acting, highly selective histamine1-receptor antagonist with minimal central and anticholinergic effects. Comparison studies have shown astemizole to be equal or superior to currently available antihistamines, beclomethasone nasal spray, and cromolyn sodium in relieving allergic symptoms of seasonal and perennial allergic rhinitis. Other uses include treatment of allergic conjunctivitis and chronic urticaria. Astemizole is not as effective for treatment of acute allergic symptoms because of its delayed onset of action. Astemizole and its active metabolite, desmethylastemizole, have long elimination half-lives permitting once-daily dosing. The incidence of sedation is lower than with conventional antihistamines, but increased appetite and weight gain do occur. Astemizole should be useful for both maintenance and prophylactic therapy in patients with chronic allergic conditions who cannot tolerate the sedative or anticholinergic effects of conventional antihistamines.

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Double-Blind Comparison of Astemizole, Terfenadine and Placebo in Hay Fever with Special Regard to Onset of Action

Cited by 24 publications

References 7 publications

Terfenadine with or without phenylpropanolamine in the treatment of seasonal allergic rhinitis

Terfenadine with or without phenylpropanolamine in the treatment of seasonal allergic rhinitis

Antiasthmatic Agents

Astemizole: A Long-Acting, Nonsedating Antihistamine

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