Carbinoxamine maleate - Indications, dose, side effects

Carbinoxamine maleate is a first-generation antihistamine like chlorpheniramine that is used to treat:

  • Allergies
  • Allergic reactions including allergic skin reactions like urticaria (hay fever), dermatographism & angioedema,
  • Allergic rhinitis
  • Vasomotor rhinitis
  • Allergic conjunctivitis
  • As an adjunct to epinephrine in severe anaphylactic reactions, and
  • For the treatment & prophylaxis of allergic reactions due to blood or blood products.

Carbinoxamine maleate Dose in Adult:

Use of Carbinoxamine in the treatment of Allergies:

  • Extended-release formulations:
    • 6 - 16 mg twice daily.
  • Immediate-release formulations:
    • 4 - 8 mg 3 or 4 times a day.

Carbinoxamine maleate Dose in children:

 Use of Carbinoxamine in the treatment of Allergic rhinitis, urticaria, and other allergic reactions:

  • Immediate-release formulations:
    • Children 2 - 5 years:
      • 0.2 to 0.4 mg/kg/day of oral solution in 3 or 4 divided doses or
      • 1 - 2 mg/dose 3 or 4 times a day to a maximum daily dose of 0.4 mg/kg/day
    • Children 6 - 11 years:
      • 2 - 4 mg/dose 3 or 4 times a day.
    • Children older than 12 years and Adolescents:
      • 4 - 8 mg/dose 3 or 4 times a day.
  • Extended-release suspension:
    • Children 2 - 3 years:
      • 3 - 4 mg/dose twice daily.
    • Children 4 - 5 years:
      • 3 - 8 mg/dose twice daily
    • Children 6 - 11 years:
      • 6 - 12 mg/dose twice daily
    • Children older than 12 years and Adolescents:
      • 6 - 16 mg/dose twice daily.

Pregnancy Risk Factor C

  • It has not yet been tested in pregnant women. If necessary, you can use other preferred agents.
  • Animal studies have not shown any birth defects.

Carbinoxamine use duringBreastfeeding:

  • It is unknown if carbinoxamine can be found in breastmilk. The manufacturer suggests that you stop breastfeeding while using it.
  • It can also lead to a decrease in prolactin production and impair lactation.

Carbinoxamine maleate Dose in Renal:

The manufacturer does not recommend any dose adjustment in patients with renal disease.

Carbinoxamine maleate Dose in liver disease:

Dose adjustment is not recommended in patients with liver disease. However, patients with advanced liver disease should use it with caution.

Common Side Effects Of Carbinoxamine Include:

  • Cardiovascular:
    • Chest tightness
    • Extrasystoles
    • Hypotension
    • Palpitations
    • Tachycardia
  • Central nervous system:
    • Ataxia
    • Chills
    • Confusion
    • Dizziness
    • Drowsiness
    • Euphoria
    • Excitability
    • Fatigue
    • Headache
    • Hysteria
    • Insomnia
    • Irritability
    • Nervousness
    • Neuritis
    • Paresthesia
    • Restlessness
    • Sedation
    • Seizure
    • Vertigo
  • Dermatologic:
    • Diaphoresis
    • Skin photosensitivity
    • Skin rash
    • Urticaria
  • Endocrine & metabolic:
  • 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
    • Hypersensitivity reaction
  • Neuromuscular & skeletal:
    • Tremor
  • Ophthalmic:
    • Blurred vision
    • Diplopia
  • Otic:
    • Labyrinthitis
    • Tinnitus
  • Respiratory:
    • Dry nose and dry throat
    • Nasal congestion
    • Thickening of bronchial secretions
    • Wheezing

Contraindication to Carbinoxamine include:

  • Allergy reactions to carbinoxamine and any component of this formulation
  • Concomitant monoamine-oxidase (MAOI) inhibitors
  • Children younger than 2 years old
  • Breastfeeding women

Warnings and Precautions

  • CNS depression:
    • It is important to exercise caution when operating heavy machinery or performing skilled work.
  • Asthma
    • It should be used with caution by patients suffering from asthma.
  • Cardiovascular disease
    • Patients with hypertension, cardiovascular disease, or ischemic heart disease are advised to exercise caution.
  • Increased intraocular pressure
    • Patients with narrow-angle glaucoma, high intraocular pressure, or both should exercise caution.
  • Prostatic hyperplasia and urinary obstruction:
    • Anticholinergic properties of the drug should be avoided by patients with genitourinary and prostatic hyperplasia.
  • Occlusion of the pyloroduodenum:
    • Patients suffering from a pyloroduodenal obstruction or stenotic pepticule should not use this drug.
  • Thyroid dysfunction:
    • Thyroid disease patients should be cautious when using the drug.

Carbinoxamine: 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 drugs could not have as much of a therapeutic impact.
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 Acetylcholinesterase inhibitors' therapeutic efficacy can be lessened by anticholinergic drugs.
Anticholinergic Agents May lessen antihistamines' sedative effects.
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 Other anticholinergic agents could be harmful or poisonous.
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 Anticholinergic drugs could be harmful or poisonous. The brain may be more significantly depressed by CNS Depressants. Management: The maker of the pregnancy-safe drug Diclegis (doxylamine/pyridoxine) particularly advises against combining it with other CNS depressants.
Dronabinol CNS Depressants may intensify the effects of CNS Depressants.
Esketamine CNS Depressants may intensify the effects of CNS Depressants.
Gastrointestinal Agents (Prokinetic) The therapeutic effects of gastrointestinal agents can be lessened by anticholinergic 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 Anticholinergic medications may reduce Nitroglycerin's absorption. Anticholinergic drugs may slow down the sublingual nitroglycerin tablet's ability to dissolve, which could hinder or delay nitroglycerin absorption.
Piribedil Piribedil's CNS depressing effects could be amplified by other CNS depressants.
Pitolisant Pitolisant's therapeutic effects can be lessened 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 Benzylpenicilloyl Polylysine's diagnostic potency may be diminished by antihistamines. Management: Delay testing until systemic antihistaminic effects have subsided and discontinue systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing. A histamine skin test can be used to check for lingering antihistaminic effects.
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 who are taking other CNS depressants.
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 Antihistamines may lessen the therapeutic effects of hyaluronidase. Treatment: Patients taking antihistamines, especially at larger doses, may not respond clinically to hyaluronidase at conventional doses. Hyaluronidase dosages may need to be increased.
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, benzodiazepines, or other CNS depression drugs. 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 Anticholinergic drugs may enhance the ulcerogenic potential of potassium chloride. Treatment: Patients should avoid consuming any oral dose form of potassium chloride if they are taking medications with strong anticholinergic effects.
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:

  • Monitor the patient for change in mental status as it may cause drowsiness.
  • Monitor CBC, uric acid, and ECG Monitor thyroid functions during prolonged therapy 

How to take Carbinoxamine?

Shake the suspension before its use. Take the drug orally on an empty stomach with water.

Mechanism of action of Carbinoxamine maleate:

Carbinoxamine maleate, a first-generation antihistamine, competes with histamine to affect the effector cells of the gastrointestinal tract, blood vessels and respiratory tract.

The drug is available immediately and has a DUration of actionAbout 4 hours It works wellabsorbedFrom the gastrointestinal tractMetabolizedBy the liver.

The extended-release tablet is now available.half-life eliminationIt takes approximately 17 hours to get there and 1.5 to 5 hours to return. peak serum concentration. It is primarilyexcretedVia urine

International brands of Carbinoxamine maleate:

  • Arbinoxa
  • Karbinal ER
  • RyVent
  • Allergefon
  • Clistin
  • Histin
  • Prindex
  • Ramallerge
  • Santimin

Carbinoxamine maleate Brands in Pakistan:

Carbinoxamine (Maleate) [Drops 1 Mg/Ml]
Flunec-D Stanley Pharmaceuticals (Pvt) Ltd.
Rondec-D Abbott Laboratories (Pakistan) Limited.

Carbinoxamine (Maleate) [Syrup 2 Mg/5ml]
Asovil Askari Pharmaceuticals.
Davedix Neo Medix
Triocof Wilsons Pharmaceuticals
Triocof-Sf Wilsons Pharmaceuticals

Carbinoxamine (Maleate) [Syrup 1.34 Mg/5ml]
Jumsol Helicon Pharmaceutek Pakistan (Pvt) Ltd.

Carbinoxamine (Maleate) [Tabs 8 Mg]
Rondec-Tr Abbott Laboratories (Pakistan) Limited.
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