Lack of subsensitivitvy to mizolastine over 8‐week treatment

Bousquet, Jean; Chanal, I.; Murrieta, M.; Stalla-Bourdillon, A.

doi:10.1111/j.1398-9995.1996.tb04601.x

Cited by 7 publications

(1 citation statement)

References 14 publications

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“…There is no evidence of 'tachyphylaxis' following regular daily dosage for 8 weeks as judged by suppression of histamine wheals [33,34] . There is also evidence to suggest that the anti-infl ammatory actions of H 1 antihistamines (vide supra) may be enhanced by prolonged regular dosage [35] .…”

Section: Frequency Of Dosage and Tolerance (Subsensitivity)mentioning

confidence: 99%

Antihistamines in Dermatology

Greaves¹

2005

Skin Pharmacol Physiol

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Along with antibiotics, antihistamines are the most widely used systemic drugs in dermatology. This is attributable to the major role played by histamine in common diseases such as urticaria and atopic eczema. Of the currently recognised four subtypes of G protein-coupled histamine receptors, only the H₁ and H₂ subtypes have been positively identified in human skin. Traditionally believed to be competitive antagonists of histamine, H₁ and H₂ antihistamines are now considered to behave as inverse agonists. By consensus, H₁ antihistamines are classified as ‘first generation’ (associated with troublesome side-effects including somnolence, anti-adrenergic and atropine-like actions) and ‘second-generation’ compounds (in which these side-effects are reduced or absent). The main indications for H₁ antihistamines in skin are suppression of pruritus in urticaria and atopic eczema, both of which are associated with increased mast cell numbers and tissue histamine levels. However the evidence basis for use in atopic eczema is ambiguous and controversial, even though these drugs are widely used in practice. Currently, significant side-effects are mainly confined to the first-generation compounds and are especially troublesome in the elderly. Psychomotor impairment may persist throughout the day following administration. Anti-cholinergic and anti-α-adrenergic blockade and cardiotoxicity (torsade de pointes) may also occur with first-generation antihistamines. Two early low-sedation second-generation antihistamines caused arrhythmias in a small number of patients but these compounds have now been withdrawn. Generally, the second-generation H₁ antihistamines are well tolerated.

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Section: Frequency Of Dosage and Tolerance (Subsensitivity)mentioning

confidence: 99%

Antihistamines in Dermatology

Greaves¹

2005

Skin Pharmacol Physiol

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Variations among non-sedating antihistamines: are there real differences?

Mattila

Paakkari²

1999

European Journal of Clinical Pharmacology

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Most of the modern non-sedating H1 receptor antagonists (antihistamines) penetrate the brain poorly, allowing the use of doses large enough to counteract allergic processes in peripheral tissues without important central effects. The antihistamines reviewed here are acrivastine, astemizole, cetirizine, ebastine, fexofenadine, loratadine, mizolastine, and terfenadine. However, these drugs are not entirely free from central effects, and there are at least quantitative differences between them. Although psychomotor and sleep studies in healthy subjects in the laboratory may predict that an antihistamine does not cause drowsiness, the safety margin can be narrow enough to cause a central sedating effect during actual treatment. This might result from a patient's individual sensitivity, disease-induced sedation, or drug dosages that are for various reasons relatively or absolutely larger (patient's weight, poor response, reduced drug clearance, interactions). Mild to even moderate sedation is not necessarily a major nuisance, particularly if stimulants need be added to the regimen (e.g. in perennial rhinitis). Furthermore, patients can adjust doses themselves if needed. Sedating antihistamines are not needed for long-term itching, because glucocorticoids are indicated and more effective. It is wise to restrict or avoid using antihistamines (astemizole, terfenadine) that can cause cardiac dysrhythmias, because even severe cardiotoxicity can occur in certain pharmacokinetic drug-drug interactions. Histamine H1 receptor antagonists (antihistamines) are used in the treatment of allergic disorders. The therapeutic effects of most of the older antihistamines were associated with sedating effects on the central nervous system (CNS) and antimuscarinic effects causing dry mouth and blurred vision. Non-specific "quinidine-like" or local anaesthetic actions often led to cardiotoxicity in animals and man. Although such adverse effects varied from drug to drug, there was some degree of sedation with all old antihistamines. Non-sedating antihistamines have become available during the past 15 years. Some of them also have antiserotonin or other actions that oppose allergic inflammation, and they are not entirely free from sedative effects either. In small to moderate "clinical" concentrations they are competitive H1 receptor antagonists, although large concentrations of some of them exert non-competitive blockade. Daytime drowsiness and weakness are seldom really important, and they restrict patients' activities less than the old antihistamines. Some new antihistamines share with old antihistamines quinidine-like effects on the cardiac conducting tissues, and clinically significant interactions have raised the question of drug safety. This prodysrhythmic effect has also been briefly mentioned in comparisons of non-sedative H1 antihistamines.

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Clinical pharmacology of new H1-receptor antagonists, and why it matters

Simons¹,

Estelle²

1998

Revue Française d'Allergologie et d'Immunologie Clinique

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Lack of subsensitivitvy to mizolastine over 8‐week treatment

Cited by 7 publications

References 14 publications

Antihistamines in Dermatology

Antihistamines in Dermatology

Variations among non-sedating antihistamines: are there real differences?

Clinical pharmacology of new H1-receptor antagonists, and why it matters

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