Chloropyramine
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Chloropyramine is a first-generation antihistamine drug approved in several Eastern European countries such as Russia for the treatment of allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic (allergic) conditions. Related indications for clinical use include angioedema, allergic reactions to insect bites, food and drug allergies, and anaphylactic shock.Script error: No such module "Unsubst".
Chloropyramine is known as a competitive reversible H1 receptor antagonist (also known as an H1 inverse agonist), meaning that it exerts its pharmacological action by competing with histamine for the H1 subtype histamine receptor. By blocking the effects of histamine, the drug inhibits the vasodilation, increased vascular permeability, and tissue edema associated with histamine release in the tissue. The H1 antagonistic properties of chloropyramine can be used by researchers for the purposes of blocking the effects of histamine on cells and tissues. In addition, chloropyramine has some anticholinergic properties.[1]
Chloropyramine's anticholinergic properties and the fact that it can pass through the blood–brain barrier are linked to its clinical side effects such as drowsiness, weakness, vertigo, fatigue, dry mouth, constipation, and rarely — visual disturbances and increase of intraocular pressure.Script error: No such module "Unsubst".
Contraindications
Contraindications for parenteral or oral administration include benign prostatic hyperplasia, peptic ulcer, pyloric and duodenal stenosis, uncontrolled glaucoma, pregnancy and breast-feeding. It is not intended for the management of acute bronchospasm.[1] It should be used with caution in patients with hyperthyroidism, cardiovascular diseases, and asthma.Script error: No such module "Unsubst".
Adverse effects
In children, it can induce agitation, and in many adult patients, dizziness may be observed. Because of the pronounced sedative effect, the preparation should be prescribed cautiously in drivers and people working with machines.Script error: No such module "Unsubst".
A large study on people 65 years old or older linked the development of Alzheimer's disease and other forms of dementia to the "higher cumulative" use of first-generation antihistamines, due to their anticholinergic properties.[2]
Interactions
Chloropyramine should not be used internally with MAO inhibitors. Because of its anticholinergic activity, concurrent administration with cholinomimetics is not advisable. Chloropyramine should also not be used internally with alcohol, sedatives, and hypnotics because of the potentiation of the effects. General anesthetics, opioids, and other depressants potentiate the sedative effect of chloropyramine.Script error: No such module "Unsubst".
Dosage
In cases of severe allergic reactions, chloropyramine can be injected intramuscularly or intravenously. Oral administration: In adults, 25 mg can be taken 3 to 4 times daily (up to 150 mg); in children over 5 years old, 25 mg can be taken 2 to 3 times daily. For external application, the skin or the eye conjunctiva can be treated up to several times a day by applying a thin layer of cream or ointment containing 1% chloropyramine hydrochloride.Script error: No such module "Unsubst".
Trade names
- Allergopress, Chimpharm AD (KZ)
- Allergosan, Sopharma AD (BG, GE, LV)
- Suprastin, Egis Pharmaceuticals PLC (GE, HU, KZ, LT, LV, UA, RU)
- Supralgon, Biopharm JSC (GE)
- Supranorm-Tsiteli A, Rompharm Co. (GE)
- Synopen, Pliva d.o.o. (BA, HR, RS,MK)
Synthesis
The preparation begins with the condensation of 4-chlorobenzaldehyde with 1,1-dimethyethylenediamine. The resulting Schiff base is reduced. The resulting amine is then further reacts with 2-bromopyridine in the presence of sodamide.
See also
- Mepyramine (4-methoxy analog)
- Methapyrilene
- Chlorothen
References
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- ↑ a b Cite error: Script error: No such module "Namespace detect".Script error: No such module "Namespace detect".
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- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, Kenneth HL, "N, n-dimethyl-n'-(4-halobenzyl)-n'-(2-pyridyl) ethylenediamines and preparation of the same", issued Script error: No such module "auto date formatter"., assigned to American CyanamideScript error: No such module "Check for unknown parameters".
- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, Cates EM, Phillips RF, "Process of preparing n, n-dimethyln'-(p-chlorobenzyl)-n'-(2-pyridyl)-ethylenediamine", issued Script error: No such module "auto date formatter"., assigned to Merck & Co.Script error: No such module "Check for unknown parameters".
- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, "Verfahren zur Herstellung eines Äthylendiaminderivates.", issued Script error: No such module "auto date formatter"., assigned to J. R. Geigy AGScript error: No such module "Check for unknown parameters".
- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, "Verfahren zur Herstellung eines Äthylendiaminderivates.", issued Script error: No such module "auto date formatter"., assigned to J. R. Geigy AGScript error: No such module "Check for unknown parameters".
- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, "Verfahren zur Herstellung eines Äthylendiaminderivates.", issued Script error: No such module "auto date formatter"., assigned to J. R. Geigy AGScript error: No such module "Check for unknown parameters".
- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, "Manufacture of n-(2-pyridyl)-n-(p-chloro-benzyl)-n:n-dimethyl-ethylenediamine", issued Script error: No such module "auto date formatter"., assigned to J. R. Geigy AGScript error: No such module "Check for unknown parameters".
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