Introduction - histamine
Introduction
Uses
Conventional antihistamines
Antihistamine creams
Non-sedating antihistamines
H2-receptor antagonists
Histamine is a vasoactive chemical. This means it has an effect on small blood vessels, resulting in dilated capillaries (redness), and leakage of protein-rich fluid into surrounding skin (swelling). Histamine affects nearby nerves resulting in itching. Histamine is stored in granules within mast cells together with other vasoactive chemicals.
Histamine release occurs in the following skin conditions:
Antihistamines are medications that counteract the effect of the natural chemical histamine.
Antihistamines are used to reduce symptoms due to type 1 allergic diseases (such as anaphylaxis) and other conditions mediated by histamine, such as urticaria. They do not always result in complete control because they do not counteract the other chemicals that may be responsible for the symptoms.
There are at least two kinds of histamine receptors, hence antihistamines are classified as H1 and H2 antagonists. Antihistamines used in dermatology are mainly H1 antagonists.
As well as tablets, antihistamines are available as injections, elixirs, and creams.
As the older type of antihistamines result in relaxation and help to induce sleep, they may be prescribed in other itchy skin diseases such as eczema. They are not thought to be addictive but cause sedation, respiratory depression and cognitive impairment.
Antihistamines are also used for:
Conventional or 'sedating' H1 antihistamines include:
Short-acting alkylamines
Longer-acting phenothiazines (these can help reduce nausea but can be quite sedating)
Ethanolamine
Propylamine derivatives
Piperazine
Others
In some countries, label statements indicate that sedating antihistamines should not be used in children under the age of 2 years for any reason; they should not be used in children under 6 years for a cough and cold symptoms, and they should not be used for insomnia in children under the age of 12 years. Side effects might be greater in older patients. At any age, the manufacturer's recommended dose should not be exceeded without medical advice.
Side effects are anticholinergic (antimuscarinic) and include:
Alcohol in combination with antihistamines could result in excessive and potentially dangerous drowsiness. Care should be taken when combining with other sedative or anticholinergic drugs and when driving, flying or diving underwater.
Because they are broken down by the liver, those with liver disease are best to take a reduced dose as there will be excessive levels circulating in the bloodstream.
In general, all drugs are best avoided in pregnancy, but there is no data to suggest that antihistamines are harmful to the mother or fetus so they are sometimes prescribed for severe urticaria in pregnant women. If a mother is breastfeeding, antihistamines may reduce milk production and could result in drowsiness of the infant, so are best avoided.
Unfortunately, antihistamine creams can occasionally cause contact allergic dermatitis so they should not be applied to large areas, and should be discontinued if they result in a rash. They should be avoided on broken skin.
Non-sedating antihistamines are much less likely to cause drowsiness and anticholinergic effects but can do so in susceptible individuals. The dose should be reduced in renal impairment and in older people.
These include:
Terfenadine (Teldane™) and astemizole (Hismanal™) have been withdrawn from some countries. These drugs may result in electrical disturbances in the heart resulting in palpitations and rarely sudden death when taken at the same time as the following medicines:
The second type of histamine receptor (H2) is found in the stomach and skin. H2 blockers were developed to reduce stomach acid secretion and proved useful for patients with peptic ulcers. H2 blockers have been used for some patients with urticaria but are no longer recommended for this indication.
H2 blockers include:
Side effects of H2 blockers are uncommon but include:
Approved datasheets are the official source of information for medicines, including approved uses, doses, and safety information. Check the individual datasheet in your country for information about medicines.
We suggest you refer to your national drug approval agency such as the Australian Therapeutic Goods Administration (TGA), US Food and Drug Administration (FDA), UK Medicines and Healthcare products regulatory agency (MHRA) / emc, and NZ Medsafe, or a national or state-approved formulary eg, the New Zealand Formulary (NZF) and New Zealand Formulary for Children (NZFC) and the British National Formulary (BNF) and British National Formulary for Children (BNFC).
