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

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:

Oral: 2 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):
Children:
- 2 to 5 years:
  - 0.5 mg every 4 to 6 hours
- 6 to 11 years:
  - 1 mg every 4 to 6 hours
- 12 years:
  - 2 mg every 4 to 6 hours
Adolescents:
- 2 mg every 4 to 6 hours

Dexchlorpheniramine Pregnancy Category: B

Even though data on its use during pregnancy are limited, there have been no adverse pregnancy outcomes.
Cetirizine, fexofenadine and loratadine of the second-generation antihistamines are preferred to the first-generation.
They may still be used during pregnancy for rhinitis and itching.
Patients suffering from pruritis caused by intrahepatic cholesterol are not advised to take antihistamines.

Use during breastfeeding:

Avoid using it during breastfeeding. If mothers take it before breastfeeding, it can cause a drop in maternal serum prolactin concentrations.
Premature infants and newborns are particularly at risk for developing intolerance to the drug, so it is contraindicated.

Dose in Kidney Disease:

There are no dosage adjustments provided in the manufacturer’s labeling.

Dose in Liver disease:

There are no dosage adjustments provided in the manufacturer’s labeling.

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:

Allergy reactions to dexchlorpheniramine malate, other antihistamines with similar chemical structures, or any component in the formulation
Use in infants and newborns
Mothers who are lactating
Patients with asthma or lower respiratory tract symptoms should not use this medication.
MAOI therapy may be used in conjunction.

Warnings and precautions

CNS depression:
- It can cause depression in the central nervous system, which may lead to sedation or drowsiness.
- It is important to warn patients if they are required to drive or operate heavy machinery.
Cardiovascular disease
- Patients suffering from hypertension or ischemic heart disease should be cautious about taking the drug.
Narrow-angle Glaucoma
- Patients with narrow-angle Glaucoma could experience worsening symptoms. Therefore, it is important to take the drug with caution.
Prostatic hyperplasia/urinary block:
- Patients with genitourinary blockage and patients with prostatic hyperplasia need to be cautious about taking the drug.
Occlusion of the pyloroduodenum:
- Patients with stenotic or peptic ulcers, as well as patients with pyloroduodenal blockage, should be cautious about taking the drug.
Thyroid dysfunction:
- Patients suffering from thyroid dysfunction should be cautious when using it.

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:

It is the active compound of chlorpheniramine.
It is twice as active than the racemic compound.
It binds to the H-1 receptors of histamine in the gastrointestinal, blood vessels and respiratory tracts and inhibits them.

Metabolism: