Dexchlorpheniramine (Polaramine) - Uses, Dose, Side effects, MOA, Brands

Dexchlorpheniramine, also known as dexchlorpheniramine maleate, is an antihistamine drug used to relieve symptoms of allergic conditions such as hay fever, allergic rhinitis, and allergic conjunctivitis. It belongs to the class of medications called first-generation antihistamines.

Antihistamines like dexchlorpheniramine work by blocking the action of histamine, a substance in the body that causes allergy symptoms such as sneezing, itching, watery eyes, and runny nose. By blocking histamine, dexchlorpheniramine helps to alleviate these symptoms.

It's worth noting that dexchlorpheniramine may cause drowsiness, which can affect your ability to perform tasks requiring alertness such as driving or operating machinery. Therefore, it's essential to use caution when taking this medication, especially until you know how it affects you.

Dexchlorpheniramine (Polaramine) is the active form of chlorpheniramine (twice as active as chlorpheniramine). It inhibits the release of histamine in the target tissues (primarily the upper respiratory tract) and is used for the treatment of patients with allergic symptoms.

Dexchlorpheniramine Uses:

  • Hypersensitivity reactions:
    • It is indicated for the symptomatic treatment of allergic conditions such as:
      • Seasonal and perennial allergic rhinitis;
      • vasomotor rhinitis;
      • allergic conjunctivitis;
      • mild or uncomplicated allergic skin manifestations of urticaria and angioedema;
      • allergic reactions to blood or plasma;
      • dermatographism;
      • and as adjunctive treatment for the management of anaphylactic reactions.

Dexchlorpheniramine Dose in Adults

Dexchlorpheniramine Dose in the treatment of Allergy symptoms:

  • In treating allergy symptoms, the usual dose of dexchlorpheniramine taken by mouth is 2 milligrams (mg) every 4 to 6 hours.

Dexchlorpheniramine Dose in Children:

For the Treatment of:

  • seasonal and perennial allergic rhinitis;
  • vasomotor rhinitis;
  • dermographism;
  • mild, uncomplicated allergic skin manifestations of urticaria and angioedema;
  • allergic conjunctivitis due to certain foods and inhalant allergens;
  • allergic reactions to blood or plasma;
  • anaphylactic reactions as adjunctive to epinephrine and other standard measures (after initial resuscitation): 

For Children:

  • Ages 2 to 5 years: 0.5 milligrams (mg) every 4 to 6 hours
  • Ages 6 to 11 years: 1 mg every 4 to 6 hours
  • Ages 12 years and older: 2 mg every 4 to 6 hours

For Adolescents (ages 12 and older):

  • 2 mg every 4 to 6 hours

Dexchlorpheniramine Pregnancy Category: B

  • Using antihistamines during pregnancy typically doesn't increase the risk of birth defects, but there's limited information specifically about dexchlorpheniramine.
  • Dexchlorpheniramine is a type of antihistamine used for conditions like rhinitis, urticaria, and rash-related itching during pregnancy, although newer antihistamines might be preferred.
  • However, they're not advised for itching linked with liver issues during pregnancy.

Use during breastfeeding:

  • Premature babies and newborns are more likely to have problems tolerating antihistamines.
  • The manufacturer advises against using them while breastfeeding.
  • Antihistamines might lower the mother's prolactin levels temporarily if taken before breastfeeding is established.

Dose in Kidney Disease:

The manufacturer's labeling doesn't include any adjustments to the dosage for people with kidney problems.

Dose in Liver disease:

The manufacturer's labeling does not specify any adjustments to the dosage for individuals with liver impairment.


Side effects of Dexchlorpheniramine:

  • Cardiovascular:
    • Chest Tightness
  • Central Nervous System:
    • Ataxia
    • Chills
    • Confusion
    • Convulsions
    • Dizziness
    • Drowsiness (Slight To Moderate)
    • Euphoria
    • Excitement
    • Fatigue
    • Hysteria
    • Insomnia
    • Irritability
    • Nervousness
    • Neuritis
    • Paresthesia
    • Restlessness
    • Sedation
    • Vertigo
  • Dermatologic:
    • Diaphoresis
    • Skin Photosensitivity
    • Skin Rash (Due To Drug)
    • Urticaria
  • Gastrointestinal:
    • Anorexia
    • Constipation
    • Diarrhea
    • Epigastric Distress
    • Nausea
    • Vomiting
    • Xerostomia
  • Genitourinary:
    • Difficulty In Micturition
    • Early Menses
    • Urinary Frequency
    • Urinary Retention
  • Hematologic & Oncologic:
    • Agranulocytosis
    • Hemolytic Anemia
    • Thrombocytopenia
  • Hypersensitivity:
    • Anaphylactic Shock
  • Neuromuscular & Skeletal:
    • Tremor
  • Ophthalmic:
    • Blurred Vision
    • Diplopia
  • Otic:
    • Acute Labyrinthitis
    • Tinnitus
  • Respiratory:
    • Dry Nose
    • Dry Throat
    • Nasal Congestion
    • Thickening Of Bronchial Secretions
    • Wheezing

Contraindications to Dexchlorpheniramine:

  • Dexchlorpheniramine maleate should not be used in individuals who have a known hypersensitivity to it, to other antihistamines with similar chemical structures, or to any ingredient in the formulation.
  • It's also not recommended for use in newborns or premature infants, breastfeeding mothers, or for treating lower respiratory tract symptoms like asthma.
  • Additionally, it should not be used in combination with MAOI (Monoamine Oxidase Inhibitor) therapy.

Warnings and precautions

CNS depression:

  • Dexchlorpheniramine may lead to CNS (Central Nervous System) depression, which can affect mental or physical abilities.
  • Patients should be warned about activities requiring mental alertness, such as operating machinery or driving, as they may be impaired while taking this medication.

Cardiovascular disease

  • Dexchlorpheniramine should be used cautiously in patients with cardiovascular disease, including conditions like hypertension (high blood pressure) and ischemic heart disease.

Narrow-angle Glaucoma

  • Dexchlorpheniramine should be used with caution in patients with narrow-angle glaucoma.

Prostatic hyperplasia/urinary block:

  • Dexchlorpheniramine should be used cautiously in patients with prostatic hyperplasia (enlargement of the prostate gland) or urinary obstruction.

Occlusion of the pyloroduodenum:

  • Dexchlorpheniramine should be used cautiously in patients with pyloroduodenal obstruction, including stenotic peptic ulcer.

Thyroid dysfunction:

  • Dexchlorpheniramine should be used cautiously in patients with thyroid dysfunction.

Dexchlorpheniramine: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

Acetylcholinesterase inhibitors

Anticholinergic Agents may have a decreased therapeutic effect. Anticholinergic Agents can decrease the therapeutic effects of Acetylcholinesterase inhibitors.

Alcohol (Ethyl)

CNS Depressants can increase the CNS depressant effects of Alcohol (Ethyl).

Alizapride

CNS Depressants may increase the CNS depressant effects.

Amantadine

Anticholinergic Agents may have an enhanced anticholinergic effect.

Amezinium

Amezinium may have a stronger stimulatory effect if it is combined with antihistamines.

Amphetamines

May decrease the sedative effects of Antihistamines.

Anticholinergic Agents

Other Anticholinergic Agents may have an adverse/toxic effect.

Betahistine

Betahistine's therapeutic effects may be diminished by antihistamines.

Botulinum Toxin-Containing Products

Anticholinergic Agents may have an enhanced anticholinergic effect.

Brexanolone

CNS Depressants can increase the CNS depressant effects of Brexanolone.

Brimonidine (Topical)

CNS Depressants may increase the CNS depressant effects.

Bromopride

CNS Depressants may increase the CNS depressant effects.

Cannabidiol

CNS Depressants may increase the CNS depressant effects.

Cannabis

CNS Depressants may increase the CNS depressant effects.

Chloral Betaine

Anticholinergic Agents may have an adverse/toxic effect.

Chlorphenesin Carbamate

CNS Depressants may have an adverse/toxic effect that can be exacerbated by them.

CNS Depressants

Can increase the toxic/adverse effects of CNS Depressants.

Dimethindene (Topical).

CNS Depressants may increase the CNS depressant effects.

Doxylamine

CNS Depressants may have a greater CNS depressant effect if taken with other CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended.

Dronabinol

CNS Depressants may increase the CNS depressant effects.

Esketamine

CNS Depressants may increase the CNS depressant effects.

Gastrointestinal Agents (Prokinetic)

Anticholinergic Agents can reduce the therapeutic effects of Gastrointestinal Agents (Prokinetic).

Glucagon

Anticholinergic agents may increase the toxic/adverse effects of Glucagon. Particularly, there may be an increase in the likelihood of gastrointestinal adverse reactions.

HydrOXYzine

CNS Depressants may increase the CNS depressant effects.

Itopride

Itopride's therapeutic effects may be diminished by anticholinergic agents.

Kava Kava

CNS Depressants may have an adverse/toxic effect that can be exacerbated by them.

Lofexidine

CNS Depressants may have a greater depressant effect on the brain. Management: Separate drug interaction monographs are available for drugs listed as an exception to this monograph.

Magnesium Sulfate

CNS Depressants may increase the CNS depressant effects.

MetyroSINE

MetyroSINE may have a sedative effect that can be enhanced by CNS depressants.

Mianserin

Anticholinergic Agents may have an enhanced anticholinergic effect.

Minocycline

CNS Depressants may increase the CNS depressant effects.

Mirabegron

Anticholinergic agents may increase the toxic/adverse effects of Mirabegron.

Mirtazapine

CNS Depressants can increase the CNS depressant effects of Mirtazapine.

Nabilone

CNS Depressants may increase the CNS depressant effects.

Nitroglycerin

The absorption of Nitroglycerin may be decreased by anticholinergic agents. Anticholinergic Agents may reduce the dissolution sublingual nitroglycerin tablet, which could impair or slow down nitroglycerin absorbtion.

Piribedil

CNS Depressants could increase the CNS depressant effects of Piribedil.

Pitolisant

Pitolisant's therapeutic effects may be diminished by antihistamines.

Pramipexole

Pramipexole may have a greater sedative effect if it is combined with CNS depressants.

Ramosetron

Ramosetron's constipating effects may be enhanced by anticholinergic agents.

ROPINIRole

CNS Depressants can increase the sedative effects of ROPINIRole.

Rotigotine

CNS Depressants can increase the sedative effects of Rotigotine.

Rufinamide

CNS Depressants may have an adverse/toxic effect that can be exacerbated by this. Particularly, dizziness and sleepiness may be increased.

Selective Serotonin Reuptake inhibitors

CNS Depressants can increase the toxic/adverse effects of Selective Serotonin Resuptake Inhibitors. Particularly, psychomotor impairment could be increased.

Tetrahydrocannabinol

CNS Depressants may increase the CNS depressant effects.

Tetrahydrocannabinol, and Cannabidiol

CNS Depressants may increase the CNS depressant effects.

Thiazide and Thiazide -Like Diuretics

Anticholinergic Agents can increase serum Thiazide or Thiazide-Like Diuretics.

Topiramate

Topiramate's toxic/adverse effects may be exacerbated by anticholinergic agents.

Trimeprazine

CNS Depressants may increase the CNS depressant effects.

Risk Factor D (Consider therapy modifications)

Benzylpenicilloyl polylysine

Antihistamines can reduce the diagnostic effectiveness of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. To assess for persistent antihistaminic effects, a histamine skin test can be performed.

Blonanserin

CNS Depressants can increase the CNS depressant effects of Blonanserin.

Buprenorphine

CNS Depressants can increase the CNS depressant effects of buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Buprenorphine patches (Butrans) should be initiated at 5 mg/hr for adults, when taken with other CNS depression drugs.

Chlormethiazole

CNS Depressants may increase the CNS depressant effects. Monitoring: Look out for signs of CNS depression. If a combination of chlormethiazole and other drugs is required, a reduced dose should be used.

Droperidol

CNS Depressants may increase the CNS depressant effects. Management: Droperidol and other CNS agents, such as opioids, may be reduced or used in combination with droperidol. Separate drug interaction monographs provide more detail on exceptions to this monograph.

Flunitrazepam

CNS Depressants can increase the CNS depressant effects of Flunitrazepam.

Hyaluronidase

Hyaluronidase's therapeutic effects may be diminished by antihistamines. Management: Patients who are taking antihistamines, especially at higher doses, may not have the desired clinical response to standard doses hyaluronidase. Higher doses of hyaluronidase might be necessary.

HYDROcodone

CNS Depressants can increase the CNS depressant effects of HYDROcodone. When possible, avoid concomitant use with hydrocodone, benzodiazepines, or other CNS depressionants. Combining these agents is not recommended unless there are other options. Limit the amount and duration of each drug when combined.

Methotrimeprazine

Methotrimeprazine may have a higher CNS depressant activity than CNS Depressants. Methotrimeprazine can increase the CNS depressant effects of CNS Depressants. Management: Lower the adult dose of CNS Depressants by 50% and start concomitant methotrimeprazine treatment. After clinically proven efficacy of methotrimeprazine, further CNS depressant dose adjustments should only be made.

Opioid Agonists

CNS Depressants can increase the CNS depressant effects of Opioid Aggonists. Management: When possible, avoid concomitant use opioid agonists and other CNS depressants. Combining these agents is not recommended unless there are other options. Limit the amount and duration of each drug when combined.

OxyCODONE

CNS Depressants can increase OxyCODONE's CNS depressant effects. When possible, avoid the simultaneous use of oxycodone and other CNS depressants. Combining these agents is not recommended unless there are other options. Limit the amount and duration of each drug when combined.

Perampanel

CNS Depressants may have a greater CNS depressant effect. Perampanel and any other CNS depressant drug should be used in combination. Patients who take perampanel together with any other drug should not engage in complex or high-risk activities until they have had experience with the combination.

Pramlintide

Anticholinergic Agents may have an enhanced anticholinergic effect. These effects are only for the GI tract.

Secretin

Secretin's therapeutic effects may be diminished by anticholinergic agents. Concomitant use: Secretin and anticholinergic agents should be avoided. Stop using anticholinergic drugs for at least five half-lives before administering secretin.

Sodium Oxybate

CNS Depressants may have a greater depressant effect if taken in combination. Management: Look for alternatives to the combination use. If you must combine use, reduce the doses of any one or more drugs. It is not recommended to combine sodium oxybate and alcohol, or any sedative hypnotics.

Suvorexant

CNS Depressants can increase the CNS depressant effects of Suvorexant. Management: Suvorexant or any other CNS depressionant can be reduced in doses. Suvorexant should not be taken with alcohol. It is also not recommended to take suvorexant along with any other drugs for insomnia.

Tapentadol

CNS Depressants may increase the CNS depressant effects. Tapentadol, benzodiazepines and other CNS depressants should be avoided when possible. Combining these agents is not recommended unless there are other options. Limit the amount and duration of each drug when combined.

Zolpidem

CNS Depressants can increase the CNS depressant effects of Zolpidem. Management: For men who also take CNS depressants, reduce the adult Intermezzo brand sublingual Zolpidem dose to 1.75mg. For women, no dose adjustment is advised. Avoid using CNS depressants at night; do not use alcohol.

Risk Factor X (Avoid Combination)

Aclidinium

Anticholinergic Agents may have an enhanced anticholinergic effect.

Azelastine (Nasal)

CNS Depressants could increase the CNS depressant effects of Azelastine.

Bromperidol

CNS Depressants may increase the CNS depressant effects.

Cimetropium

Cimetropium may have an anticholinergic effect that can be enhanced by the use of anticholinergic agents.

Eluxadoline

Eluxadoline may cause constipation by using anticholinergic agents.

Glycopyrrolate (Oral Inhalation)

Anticholinergic agents may increase the anticholinergic effects of Glycopyrrolate (Oral inhalation).

Glycopyrronium (Topical)

Anticholinergic Agents may have an enhanced anticholinergic effect.

Oral Inhalation with Ipratropium

Anticholinergic Agents may have an enhanced anticholinergic effect.

Levosulpiride

Anticholinergic Agents can reduce the therapeutic effects of Levosulpiride.

Orphenadrine

Orphenadrine may be more effective against CNS depression than other drugs.

Oxatomide

Anticholinergic Agents may have an enhanced anticholinergic effect.

Oxomemazine

CNS Depressants may increase the CNS depressant effects.

Paraldehyde

Paraldehyde may be enhanced by CNS depressants.

Potassium Chloride

Potassium Chloride may have an ulcerogenic effect that can be exacerbated by anticholinergic agents. Treatment: Patients taking drugs that have significant anticholinergic effects should not consume any oral dose form of potassium chloride.

Potassium Citrate

Potassium Citrate may be more ulcerogenic if it is given to anticholinergic agents.

Revefenacin

Revefenacin may be enhanced by anticholinergic agents.

Thalidomide

CNS Depressants can increase Thalidomide's CNS depressant effects.

Tiotropium

Anticholinergic agents may increase the anticholinergic effects of Tiotropium.

Umeclidinium

Anticholinergic Agents may have an enhanced anticholinergic effect.

Monitoring Parameters:

None mentioned. Monitor the response to treatment.   


How to administer Dexchlorpheniramine?

It may be taken with or without food as directed by the physician.

For mild symptoms, it should be taken at night to avoid sedation during the day time.   


Mechanism of action of Dexchlorpheniramine:

  • Dexchlorpheniramine works by competing with histamine for H-receptor sites on cells in the gastrointestinal tract, blood vessels, and respiratory tract.
  • It's the main active part of chlorpheniramine and is about twice as effective as the combined form.

Metabolism:

  • Dexchlorpheniramine is metabolized in the liver.

Half-life elimination:

  • It takes approximately 20 to 30 hours for half of the dexchlorpheniramine to be eliminated from the body.

Time to peak:

  • The peak concentration of dexchlorpheniramine in the blood is typically reached around 3 hours after ingestion.

Excretion:

  • The drug is primarily excreted through urine.

International Brand Names of Dexchlorpheniramine:

  • RyClora
  • Afeme
  • Alergyo
  • Cortiflam-D
  • Dapriton
  • Delamin
  • Destramin
  • Dex Antihist
  • Dexatamin
  • Dexferin
  • Histaklor
  • Histamed
  • Isomerine
  • Liramin
  • Polaramin
  • Polaramin Prolongatum
  • Polaramine
  • Polaramine
  • Polaramine Repetabs
  • Polarax
  • Rhiniramine SR
  • Somin
  • Trenelone

Dexchlorpheniramine Brand Names in Pakistan:

No Brands Available in Pakistan.