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General pharmacology

There are so-called tissue hormones in the body, which include mediators such as histamine. These mediator substances are substances that are released from cells or cell clusters and act on neighboring cells. If there is histamine, e.g. B. after an insect bite, in the skin, there is a painful reddening or an itchy wheal. The reaction is caused by antigens that react with antibodies on the mast cells. The histamine is released from these cells. Serious, possibly life-threatening allergic reactions (e.g. anaphylactic shock) are also caused by this release of histamine. In this case, a cortisone-containing agent must be injected as rescue medication.

Effects and indications

For the treatment of allergic reactions, antihistamines are used, which displace histamine from its receptors and thus can neutralize the effects of histamine. The main site of action for the so-called H1 antihistamines is the skin. Older substances also block centrally present H1 receptors and thus have a sedating effect. This "side effect" is the reason why antihistamines are also offered as non-prescription sleeping pills. With newer antihistamines (e.g. cetirizine or loratadine) this sedating undesirable effect is largely absent. Antihistamines are indicated for all diseases in which the release of histamine plays a role, such as E.g. hay fever, urticaria or insect bites. The means are particularly effective as tablets, coated tablets or drops. As creams, gels or ointments, the usefulness of these agents is doubtful.

Antihistamines are not typical addictive substances, but they can increase the effects of other addictive substances such as alcohol or benzodiazepines. In the case of a few antihistamines (e.g. diphenhydramine or doxylamine), however, a development of tolerance is suspected for high dosages. In the case of overdoses, severe sedation and delirium can also occur. Most antihistamines can be bought directly from pharmacies without a prescription; only a few new ones require a prescription.

Consequences of using antihistamines

With regard to possible side effects, the various antihistamines do not differ significantly, regardless of whether they have been approved as hypnotic, antiemetic, antitusive or antiallergic.

As a rule, improper use is accompanied by increased doses, as a result of which the risk of epileptic seizures and delirium increases. If the development of physical and psychological dependence is indicated as a side effect in the Red List 2011, Poser and Poser (1996), based on their own clinical history of addiction and the data from the early warning system, doubt that antihistamines are an addictive substance. According to Poser and Poser, if these preparations were misused, this always occurred in conjunction with other addictive substances.

Antihistamines can weaken the muscles, dizziness, headache, prolong the QT interval and change the blood count. Paradoxical reactions with restlessness, nervousness, anxiety states, tremors and insomnia rarely occur.

Withdrawal or discontinuation of antihistamines

If antihistamines are suddenly discontinued after prolonged use, restlessness and sleep disorders are to be expected as a discontinuation effect. Especially with higher dosages, it should therefore be tapered off gradually. This tapering off can usually take place over a few days; longer intervals are only recommended for extreme doses. Special accompanying measures in withdrawal do not have to be taken.

Prognosis of abuse of antihistamines

Since pure antihistamine dependencies are hardly described, the prognosis stands or falls with the actual addictive substance to which the antihistamine was also taken.

International non-proprietary name

Commercial preparation

Astemizole

Hismanal®

Azelastine

Allergodil tabs®

Bilastine

Bitoses®

Cetirizine

Cetalerg®
Ceterifug®
Ceti Lich®
Ceti TAD®
ceti-blue®
Cetiderm®
Cetidura®
Ceti-pures®
Cetirigamma®
Cetirizine-1 A Pharma®
Cetirizine AbZ®
Cetirizine Actavis®
Cetirizine ADGC®
Cetirizine AL®
Cetirizine Aristo®
Cetirizine AZU®
Cetirizine BASICS®
Cetirizine beta®
Cetirizine CT®
Cetirizine Elac®
Cetirizine Hemopharm®
Cetirizine Heumann®
Cetirizine HEXAL®
Cetirizine ratiopharm®
Cetirizine Sandoz®
Cetirizine STADA®
Cetirizine TEVA®
Cetirlane®
DocMorris Cetirizine®
Reactine®
Zanlan®
Zetir®
Zyrtec®

Cetirizine combinations

Reactine duo retard®

Chlorphenamine

Balkis Snuff Capsules New®

Clemastine

Tavegil®

Cyproheptadine

Peritol®

Desloratadine

Aerius®
Dasselta®
Desloraderm®
Desloratadine AL®
Desloratadine ratiopharm®
Desloratadine STADA®

Dexchlorpheniramine

Polaronil®

Dimetinden

Fenistyle®

Diphenhydramine

Benadryl N®
Benadryl Infant N®

Diphenylpyraline

Arbid N®

Doxylamine

Mereprine®

Ebastine

Ebastel®
Ebastin Aristo®
Ebastine Lindopharm®

Fexofenadine

Fexofenaderm®
Fexofenadine HEXAL®
Fexofenadine Winthrop®
Telfast®

Hydroxyzine

AH3 N®

Ketotifen

Ketof®
Ketofex®
Ketotifen beta®
Ketotifen Heumann®
Ketotifen Lichtenstein®
Ketot ifen-rat iopha m®
Ketotifen STADA®
Ketotifen Trom®
Ketotifen TT Temmler®
Pediatricians®
Zadites®
Zatofug®

Levocetirizine

Levocetirizine AbZ 5 mg®
Levocetirizine AL®
Levocetirizine CT®
Levocetirizine HEXAL®
Levocetirizine ratiopharm®
Levocetirizine STADA®
Sopras®
Xusa l / -acute®

Loratadine

Give loratadine®
Lisino®
Livotab directly®
Lobeta®
Lora ADGC®
Lora BASICS®
Lora Lich®
Loraclar®
Loraderm®
Loragalen®
Loralerg®
Lorano®
Lora-Puren®
Loratadine / acute-1 A Pharma®
Loratadine acis®
Loratadine AL®
Loratadine axcount®
Loratadine AZU®
Loratadine CT®
Loratadin Heumann®
Loratadin KSK®
Loratadine ratiopharm®
Loratadin Sandoz®
Loratadin STADA®
LORATADIN-TEVA®
Loratadura®
Loratagamma®
Loravis®
Vividrin Loratadine®

Mequitazine

Metaplexane®

Mizolastine

Mitzolls®
Zolim®

Oxatomide

TIN SET®

Rupatadin

Rupafin®
Urtimed®

Terfenadine

Hisfedin®
Terfedura®
Terfemundin®
Terfenadine AL®
Terfenadin Heumann®
Terfenadine ratiopharm®
Terfenadin STADA®
terfenadine from ct®

Table last updated: May 2013 (Source: Deutsche Hauptstelle für Suchtfragen, 2013: Drug dependence. Addiction medicine series, Volume 5)

Text: Prof. Dr. Gerd Glaeske, Dr. med. Rüdiger Holzbach, Daniela Boeschen

Mutschler, Ernst et al. (1997): Drug Effects. Textbook of pharmacology and toxicology. Stuttgart: Scientific publishing company.

AKB - drug course book 2010/2011 (2010). Facts and Comparisons for 17,000 Drugs. Berlin: Arzneimittel-Verlags-GmbH.

Poser, Wolfgang; Poser, Sigrid (1996): Medicines - Abuse and Dependence. Origin - course - treatment. Stuttgart: Thieme.

Keup, Wolfram (1993): Abuse Patterns in Addiction to Alcohol, Medicines and Drugs: Early Warning System Data for the Federal Republic of Germany 1976-1990. Freiburg: Lambertus.