Oral Adjunctive therapy for anaphylactic reactions, Allergic conjunctivitis, Allergic reactions to blood or plasma, Angioedema, Perennial allergic rhinitis, Seasonal allergic rhinitis, Urticaria, Vasomotor rhinitis
Adult: As conventional tab or oral solution: 4-8 mg 3-4 times daily. As extended-release susp: 6-16 mg 12 hourly. Dose must be individualised according to the severity of the condition and clinical response. Treatment recommendations may vary among countries and between individual products (refer to specific product guidelines). Child: As conventional forms: 2-5 years As conventional oral solution: 0.2-0.4 mg/kg daily in 3-4 divided doses, or 1-2 mg 3-4 times daily; 6-11 years As conventional tab or oral solution: 2-4 mg 3-4 times daily. As extended-release susp: 2-3 years 3-4 mg 12 hourly; 4-5 years 3-8 mg 12 hourly; 6-11 years 6-12 mg 12 hourly; ≥12 years Same as adult dose. Dose must be individualised according to the severity of the condition and clinical response. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Administration
Carbinoxamine May be taken with or without food. Recommendations on taking w/ or w/o food are product-specific. Consult product literature for specific instructions. Oral susp: Shake well before use.
Contraindications
Neonates and children <2 years. Lactation. Concomitant use with MAOIs. Contraindications may vary between individual products (refer to specific product labelling for detailed information).
Special Precautions
Patient with CV disease (including hypertension and ischaemic heart disease); increased IOP and/or narrow-angle glaucoma; hyperthyroidism; history of asthma; pyloroduodenal obstruction (including stenosing peptic ulcer); prostatic hyperplasia, genitourinary obstruction. Children ≥2 years and elderly. Pregnancy.
Adverse Reactions
Significant: CNS depression (e.g. drowsiness, dizziness); anticholinergic effects (e.g. thickened bronchial secretions, urinary retention, increased IOP). Blood and lymphatic system disorders: Agranulocytosis, haemolytic anaemia, thrombocytopenia. Cardiac disorders: Palpitations, tachycardia, extrasystoles. Ear and labyrinth disorders: Vertigo, tinnitus. Eye disorders: Blurred vision, diplopia. Gastrointestinal disorders: Nausea, vomiting, dry mouth or throat, diarrhoea, constipation, epigastric distress. Immune system disorders: Anaphylactic shock. Metabolism and nutrition disorders: Anorexia. Nervous system disorders: Headache, restlessness, paraesthesia. Renal and urinary disorders: Urinary frequency. Reproductive system and breast disorders: Early menses. Respiratory, thoracic and mediastinal disorders: Wheezing, chest tightness, nasal stuffiness, dry nose. Skin and subcutaneous tissue disorders: Rash, urticaria, photosensitivity, excessive perspiration. Vascular disorders: Hypotension.
This drug may cause drowsiness, dizziness, and impaired mental or physical abilities, if affected, do not drive or operate machinery.
Overdosage
Symptoms: CNS depression or stimulation, convulsions, hallucinations, and atropine-like symptoms (e.g. fixed, dilated pupils, dry mouth, flushing, gastrointestinal symptoms). Management: Symptomatic and supportive treatment. Administer activated charcoal or consider performing gastric lavage in cases of ingestion of potentially fatal amount. May give physostigmine for severe anticholinergic effects. Administer vasopressors for hypotension. Monitor vital signs and ECG.
Drug Interactions
Additive effects with other CNS depressants (e.g. hypnotics, sedatives, tranquillisers). Potentially Fatal: Enhanced and prolonged anticholinergic effects with MAOIs (e.g. phenelzine, tranylcypromine, selegiline).
Food Interaction
Additive CNS depressant effects with alcohol.
Action
Description: Mechanism of Action: Carbinoxamine, a monoethanolamine derivative, is a competitive antagonist of histamine at H1-receptor sites on effector cells in the gastrointestinal tract, respiratory tract, and blood vessels. It is a 1st generation antihistamine with anticholinergic and significant sedative properties. Duration: Approx 4 hours (conventional form). Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1.5-5 hours (conventional form); approx 7 hours (extended-release susp). Metabolism: Extensively metabolised in the liver. Excretion: Via urine (as inactive metabolites). Elimination half-life: 10-20 hours (conventional form); 17 hours (extended-release susp).
Chemical Structure
Carbinoxamine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2564, Carbinoxamine. https://pubchem.ncbi.nlm.nih.gov/compound/Carbinoxamine. Accessed May 28, 2024.
R06AA08 - carbinoxamine ; Belongs to the class of aminoalkyl ethers used as systemic antihistamines.
References
Anon. Carbinoxamine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/03/2024.Anon. Carbinoxamine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/03/2024.Buckingham R (ed). Adverse Effects of Antihistamines. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/04/2024.Buckingham R (ed). Carbinoxamine Maleate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/03/2024.Buckingham R (ed). Precautions for Antihistamines. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/04/2024.Carbimin Tablets 4 mg (Malaysian Pharmaceuticals Industries Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/03/2024.Carbinoxamine Maleate Solution, Tablet (Genus Lifescience Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 23/04/2024.Carbinoxamine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 19/04/2024.Karbinal ER Suspension, Extended Release (Aytu Therapeutics, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 23/04/2024.Ryvent Tablet (Carwin Pharmaceutical Associates, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/03/2024.
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