Histamine Phosphate

(USAN)

💊 Chemical information

Histamiinifosfaatti; Histamin difosfát monohydrát; Histamina, fosfato de; Histamine Acid Phosphate; Histamine Diphosphate; Histamine, phosphate d’; Histaminfosfat; Histamini Diphosphas Monohydricus; Histamini phosphas; Histamino fosfatas; Histaminy fosforan; Hisztamin-foszfát.
Chemical formula: C5H9N3,2H3PO4,H2O = 325.2.
CAS — 51-74-1 (anhydrous histamine phosphate). ATC — V04CG03.
ATC Vet — QV04CG03.

Pharmacopoeias.

In Eur.. Chin. and US specify the anhydrous substance.

Ph. Eur. 6.2

(Histamine Phosphate). Colourless, long prismatic crystals. Freely soluble in water; slightly soluble in alcohol. A 5% solution in water has a pH of 3.75 to 3.95. Protect from light.

USP 31

(Histamine Phosphate). Anhydrous histamine phosphate occurs as colourless, odourless, long prismatic crystals. Is stable in air but is affected by light. Soluble 1 in 4 of water. Its solutions are acid to litmus. Store in airtight containers. Protect from light.

Stability.

A study concluded that solutions of histamine phosphate could be sterilised by heating in an autoclave with little degradation. 1 Autoclaved solutions could be stored for a minimum of 4 months. 1. McDonald C, et al. Stability of solutions of histamine acid phosphate after sterilization by heating in an autoclave. J Clin Pharm Ther 1990; 15: 41–4.

💊 Adverse Effects and Treatment

Injection of histamine salts can produce adverse effects including headache, flushing of the skin, general vasodilatation with a fall in blood pressure, tachycardia, bronchial constriction and dyspnoea, visual disturbances, vomiting, diarrhoea, and other gastrointestinal effects. These reactions can be severe; excessive dosage can produce collapse and shock, and may be fatal. Reactions may occur at the injection site. Some of these effects may be relieved by an antihistamine, but adrenaline may be required and should always be available.

💊 Precautions

Histamine salts should be used with care in patients with asthma or other hypersensitivity disorders, in elderly patients, and in patients with cardiovascular disorders.

💊 Pharmacokinetics

Histamine salts exert a rapid, though transient, effect when given parenterally. Histamine is rapidly metabolised by methylation and oxidation; the metabolites are excreted in the urine.
1. Middleton M, et al. Pharmacokinetics of histamine dihydrochloride in healthy volunteers and cancer patients: implications for combined immunotherapy with interleukin-2. J Clin Pharmacol 2002; 42: 774–81.

💊 Uses and Administration

Histamine causes stimulation of smooth muscle, especially of the bronchioles, and lowers blood pressure by dilating the arterioles and capillaries. It also stimulates exocrine gland secretion, especially the gastric glands. Intradermal injection of histamine produces the characteristic ‘triple response’ of erythema, flare, and wheal. This is utilised as a control response in skin testing for hypersensitivity. Also, since it is mediated in part by axon reflexes, it has been used to test the integrity of sensory nerves, for example in leprosy. Inhalation of histamine causes bronchoconstriction and is used as a test of bronchial reactivity. Histamine has also been given subcutaneously to identify the causes of achlorhydria and intravenously in the diagnosis of phaeochromocytoma, but safer tests are generally preferred. Histamine is included in some combination topical preparations for musculoskeletal disorders. Histamine hydrochloride is under investigation as an adjunct in the management of acute myeloid leukaemia and malignant melanoma. It has also been tried as an adjunct to interferons and other drugs in the management of hepatitis C.

💊 Preparations

USP 31: Histamine Phosphate Injection.

Proprietary Preparations

Mex.: Destamin; Port.: Soluprick; Venez.: Histalgan Balsamo†. Multi-ingredient: Arg.: Histaglobin; Infrarub†; Austria: Histaglobin; Canad.: Midalgan†; Cz.: Histaglobin†; Fr.: Algipan; Ger.: Histadestal; India: Algipan; Histaglobulin; Neth.: Cremor capsici comp; Cremor Capsici compositus; Kruidvat Spierbalsem; Pol.: Histaglobulina; Port.: Midalgan†; S.Afr.: Histaglobin; Infrarub; Switz.: Midalgan; Radalgin.
Published May 08, 2019.