APPENDIX VIII: DRUGS THAT COUNTERACT HISTAMINE
Histamine is one of the mediators released by mast cells when they degranulate. It is also released by various other cells in the body, since it acts as a local messenger substance, conveying instructions to neighbouring cells.
The main effects of histamine are to make smooth muscles (in the bronchi, gut, bladder etc) contract, to make the small blood vessels enlarge, and to make the capillaries (tiny blood vessels) become more leaky. These last two effects cause a drop in blood pressure. Locally, the increased leakiness of the capillaries contributes to inflammation.
Antihistamines (more correctly referred to as ‘histamine H1-receptor antagonists’) block the effects of histamine. They do this by binding to the H1 receptors on cells. Histamine normally binds to these receptors triggering off a reaction by the cell. So by blocking the receptors, antihistamines prevent histamine from affecting those cells.
There are a wide range of antihistamines available today. Most of these are rather unspecific and can also bind to the receptors for other messenger substances, such as adrenaline and serotonin. They tend to cause drowsiness through blocking messengers such as adrenaline, and they can also cause dizziness, nervousness, tremors, stomach upsets, dry mouth, blurred vision and impotence. These side-effects are not damaging in the long term, although they can be inconvenient. Some patients develop a tolerance of these drugs after a while, and the side-effects diminish. So if an antihistamine controls the allergic symptoms well, but causes side-effects, it is worth persisting with it for a while. Sometimes the sedative effects of antihistamines can be advantageous, as in children with urticaria who tend to scratch at night.
More specific drugs, which show a stronger preference for histamine receptors, have now been introduced. Astemizole (Hismanal) and terfenadine (Triludan) are the main ones. These can have some side-effects but should not cause as many problems as the other antihistamines.
Antihistamines, taken by mouth, are useful in hay-fever and perennial rhinitis, where there are symptoms in both the nose and eyes, together with itching in the mouth or ears. Where there are only symptoms in the nose, a sodium cromoglycate or corticosteroid spray may be more appropriate, as these have fewer side-effects. Some medicines contain antihistamines combined with sympathomimetics (see Section 3).
Antihistamines are also effective in some cases of chronic urticaria.
including cold-induced urticaria. They are not effective in asthma, because other mediators, besides histamine, play a major role in producing the symptoms.
2A Antihistamines
acrivastine (Semprex) astemizole (Hismanal) brompheniramine (Dimotane) cetirizine (Zirtek)
chlorpheniramine (Piriton, Haymine) clemastine (Tavegil) dimethindene (Fenostil) diphenylpyraline (Histryl Spansule, Lergoban)
hydroxyzine (Atarax) mebhydrolin (Fabahistin) mequitazine (Primalan) oxatomide (Tinset) phenindamine (Thephorin) pheniramine (Daneral) promethazine (Phenergan) terfenadine (Triludan) trimeprazine (Vallergan) triprolidine (Actidil, Pro-Actidil)
Ketotifen (Zaditen) acts both as an antihistamine and a mast-cell stabilizer (Section 1), and is used to prevent asthma attacks. Its side-effects are similar to those of most antihistamines.
Azatadine (Optimine) and cyproheptadine (Periactin) act both as antihistamines and serotonin antagonists. They are used for allergic rhinitis and urticaria.
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