Evigrade

Chloropyramine

First-generation H1 antihistamine, ethylenediamine derivative

ATC code: R06AC03

Updated · Methodology

Indications

C

Severe allergic reactions

Adjunct

Chloropyramine is a first-generation antihistamine, registered in Russia in an injectable form among others. The injection is used in acute allergic reactions when the person cannot swallow a tablet. An important correction: in anaphylaxis an antihistamine neither replaces nor delays adrenaline. Intramuscular adrenaline into the anterolateral thigh is the only agent that changes outcome; an antihistamine relieves skin manifestations, itch and urticaria only, and works more slowly. Delaying adrenaline for the sake of an antihistamine injection is a known error with severe consequences. In Spain AEMPS has not registered chloropyramine, and the data here come from the Russian state register.

ICD-10: T78.2 · ICD-11: 4A84

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

D

Allergic rhinitis

Not recommended

In allergic rhinitis chloropyramine reduces sneezing, itch and watery discharge, but barely touches nasal blockage: that comes from mucosal swelling rather than histamine directly. The modern approach to persistent rhinitis is built around intranasal corticosteroids, with second-generation antihistamines for episodic and mild symptoms. Chloropyramine loses in that line-up not on efficacy but on profile: it dries the mucosa, causes sleepiness, lasts 4–6 hours and needs repeat dosing, and in older people it adds confusion and urinary retention. The 2023 American Geriatrics Society Beers Criteria list first-generation antihistamines among potentially inappropriate medications at 65 and older. If chloropyramine was prescribed for long-term treatment of allergic rhinitis, consider seeking a second opinion.

ICD-10: J30.9 · ICD-11: CA08.0

D

Urticaria

Not recommended

In urticaria chloropyramine relieves itch and weals – H1 blockade does its job. The question is what the effect costs. The international /GA2LEN/EuroGuiDerm 2021 urticaria guideline keeps non-sedating second-generation antihistamines at standard dose as first line, with escalation to fourfold dosing when the response falls short, and speaks directly against routine use of first-generation agents. The reason lies in the profile: sedation, disrupted REM sleep, reduced attention and reaction speed the next morning, anticholinergic effects, short action and several doses a day. Cetirizine, levocetirizine, bilastine, fexofenadine and rupatadine deliver the same symptom control without that cost. If chloropyramine was prescribed as the main treatment for urticaria, consider seeking a second opinion.

ICD-10: L50 · ICD-11: EB05

F

Common cold

Not recommended

Chloropyramine often gets added to cold treatment, on the expectation that it dries a runny nose and relieves nasal swelling. The 2015 Cochrane review pooled 18 trials and 4342 participants and found this: in adults antihistamines give a small short-lived effect on overall symptom severity on day one or two, by day three the difference disappears, and there is no effect on nasal congestion, sneezing or rhinorrhoea taken separately. In children even that did not appear. Adverse effects, meanwhile, were markedly more frequent than on placebo, sedation first among them. Colds are caused by viruses rather than histamine, and a dried mucosa performs its barrier job worse. If chloropyramine was prescribed as treatment for a viral respiratory infection, consider seeking a second opinion.

ICD-10: J00 · ICD-11: CA00

F

Insomnia and sleep disorders

Not recommended

The sleepiness chloropyramine produces gave it a second reputation: the drug gets taken as a sleeping aid, including being given to children so they sleep better. Sedation here is an adverse effect rather than a therapeutic action, and it treats sleep architecture badly: H1 blockade suppresses REM sleep, the person wakes unrested, and tolerance to the effect builds within days. Sluggishness and slowed reactions persist into the morning, driving included. In children first-generation agents produce paradoxical agitation instead of sleep, and overdose in a child unfolds as seizures. The 2023 Beers Criteria list first-generation antihistamines among potentially inappropriate medications at 65 and older, pointing separately to confusion and falls. If chloropyramine was suggested for sleep, consider seeking a second opinion.

ICD-10: G47.0 · ICD-11: 7A00

F

Pre-vaccination premedication for reaction prevention

Not recommended

An antihistamine before vaccination to head off a reaction is a persistent habit, especially in paediatric practice. It makes no sense for two reasons. Ordinary post-vaccination reactions – redness, induration, fever, lethargy – are not histamine-mediated; they are the work of the innate immune response, and an H1 blocker does not touch it. True anaphylaxis cannot be prevented by premedication: it unfolds within minutes and calls for adrenaline, not a prophylactic tablet. The harm meanwhile is concrete: sedation and dry mouth mask early signs of a reaction, and the first symptoms can be written off as drug effect. The exception is a child with confirmed allergy to a vaccine component, and such cases are handled separately with an allergist. If an antihistamine was prescribed routinely before vaccination, consider seeking a second opinion.

ICD-10: Z29.8

How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

Chloropyramine is an inverse agonist at H1 receptors: it shifts the receptor towards its inactive state and removes the effects of histamine – vasodilatation, swelling, itch, smooth muscle contraction. The molecule is small and lipophilic, so it crosses the blood-brain barrier easily and occupies H1 receptors in the brain, where histamine maintains wakefulness. Sleepiness and slowed reactions follow. It has no selectivity for H1: muscarinic receptors are blocked alongside, bringing dry mouth, urinary retention, constipation, blurred vision and, in older people, confusion. The action is short, 4–6 hours, so the drug is taken several times a day.

Safety

Contraindications

  • Hypersensitivity to chloropyramine or to other ethylenediamine derivatives
  • Acute asthma attack
  • Newborn and preterm infants
  • Angle-closure glaucoma
  • Prostatic hyperplasia with urinary retention
  • Pregnancy and breastfeeding

Serious adverse effects

  • Confusion and falls in older people
  • Paradoxical agitation and seizures in children, especially in overdose
  • Acute urinary retention
  • Angle-closure glaucoma attack
  • Respiratory depression when combined with other sedating drugs

Common adverse effects

  • Sleepiness and sluggishness, including the following morning
  • Dry mouth
  • Dizziness
  • Blurred vision
  • Constipation and difficulty passing urine

Pregnancy: can you take Chloropyramine?

There are no controlled studies of chloropyramine in pregnancy, and the Russian label lists pregnancy among the contraindications. When an antihistamine is needed during pregnancy, molecules with accumulated safety data are chosen: loratadine or cetirizine.

Breastfeeding: can you take Chloropyramine?

First-generation antihistamines pass into breast milk and make the infant sleepy and lethargic at the breast, while in the mother they can reduce milk production. The Russian label lists lactation among the contraindications. When treatment is needed during this period, loratadine or cetirizine are used.

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Check interaction with another drug

Opens the checker prefilled with this drug. Pick the second one from your regimen.

Open checker

Summary of a multi-drug list →

Medicine list: everything you take in one place →

Frequently asked

What is Chloropyramine used for?

Chloropyramine is evaluated for the following indications with varying evidence strength: Severe allergic reactions (evidence tier C), Urticaria (evidence tier D), Allergic rhinitis (evidence tier D). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Chloropyramine?

Common side effects of Chloropyramine (≥ 1 in 100): Sleepiness and sluggishness, including the following morning, Dry mouth, Dizziness, Blurred vision, Constipation and difficulty passing urine. See the Safety section for uncommon and serious reactions.

Is Chloropyramine safe during pregnancy?

There are no controlled studies of chloropyramine in pregnancy, and the Russian label lists pregnancy among the contraindications. When an antihistamine is needed during pregnancy, molecules with accumulated safety data are chosen: loratadine or cetirizine.

Is Chloropyramine compatible with breastfeeding?

First-generation antihistamines pass into breast milk and make the infant sleepy and lethargic at the breast, while in the mother they can reduce milk production. The Russian label lists lactation among the contraindications. When treatment is needed during this period, loratadine or cetirizine are used.

Who should not take Chloropyramine?

Chloropyramine is contraindicated in: Hypersensitivity to chloropyramine or to other ethylenediamine derivatives; Acute asthma attack; Newborn and preterm infants; Angle-closure glaucoma; Prostatic hyperplasia with urinary retention. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

Other drugs in this group

Chlorpheniramine, Desloratadine, Dexchlorpheniramine, Dimenhydrinate, Doxylamine/pyridoxine, Ketotifen, Promethazine, Diphenhydramine