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standards of non-Merck sources.
Pronunciation
(klor fen IR a meen)
Generic Available (U.S.)
Yes: Syrup, tablet
Index Terms
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria
Use: Dental
Treatment of histamine-induced allergic symptoms
Pregnancy Risk Factor
C
Pregnancy Considerations
Reproduction studies have not been conducted with chlorpheniramine tannate.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Hypersensitivity to chlorpheniramine maleate or any component of the formulation; narrow-angle glaucoma; bladder neck obstruction; symptomatic prostate hypertrophy; during acute asthmatic attacks; stenosing peptic ulcer; pyloroduodenal obstruction. Avoid use in premature and term newborns due to possible association with SIDS.
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease).
• Increased intraocular pressure: Use with caution in patients with increased intraocular pressure.
• Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction.
• Respiratory disease: Use with caution in patients with asthma or other chronic breathing disorders.
• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Elderly: May be inappropriate in this age group due to potent anticholinergic effects; nonanticholinergic antihistamines preferred for treating allergic reactions (Beers Criteria).
• Pediatrics: Antihistamines may cause excitation in young children. Not for OTC use in children <2 years of age.
Adverse Reactions
>10%:
Central nervous system: Slight to moderate drowsiness
Respiratory: Thickening of bronchial secretions
1% to 10%:
Central nervous system: Headache, excitability, fatigue, nervousness, dizziness
Gastrointestinal: Nausea, xerostomia, diarrhea, abdominal pain, appetite increase, weight gain
Genitourinary: Urinary retention
Neuromuscular & skeletal: Arthralgia, weakness
Ocular: Diplopia
Renal: Polyuria
Respiratory: Pharyngitis
Metabolism/Transport Effects
Substrate of CYP2D6 (minor), 3A4 (major); Inhibits CYP2D6 (weak)
Drug Interactions
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Management: Upon completion/discontinuation of conivaptan, allow at least 7 days before initiating therapy with drugs that are CYP3A4 substrates. Risk D: Consider therapy modification
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: For patients being treated with hydroxyzine, a reduction in the dose of any other CNS depressants that are to be used in combination is recommended. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Storage
Protect from light.
Mechanism of Action
Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract
Pharmacodynamics/Kinetics
Half-life elimination, serum: 20-24 hours
Dosage
Oral:
Children: 0.35 mg/kg/day in divided doses every 4-6 hours
2-6 years: 1 mg every 4-6 hours, not to exceed 6 mg in 24 hours
6-12 years: 2 mg every 4-6 hours, not to exceed 12 mg/day or sustained release 8 mg at bedtime
Children >12 years and Adults: 4 mg every 4-6 hours, not to exceed 24 mg/day or sustained release 8-12 mg every 8-12 hours, not to exceed 24 mg/day
Elderly: 4 mg once or twice daily. Note: Duration of action may be 36 hours or more when serum concentrations are low.
Hemodialysis: Supplemental dose is not necessary
Administration: Oral
May be administered with food or water. Timed release oral forms are to be swallowed whole, not crushed or chewed.
Dietary Considerations
May be taken with food or water.
Geriatric Considerations
Anticholinergic action may cause significant confusional symptoms, constipation, or problems voiding urine. If an antihistamine is indicated, a second generation nonsedating antihistamine would be a more appropriate choice.
This medication is considered to be potentially inappropriate in this patient population (Beers Criteria severity: High).
Additional Information
Not effective for nasal stuffiness.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation). Chronic use of antihistamines will inhibit salivary flow, particularly in elderly patients; this may contribute to periodontal disease and oral discomfort.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness is common; may cause excitability, nervousness, fatigue, or depression
Mental Health: Effects on Psychiatric Treatment
Dry mouth and sedation may be exacerbated by concurrent psychotropic use
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Suspension, oral, as tannate:
P-Tann: 8 mg/5 mL (473 mL [DSC]) [sugar free; contains sodium benzoate; bubblegum flavor]
Suspension, oral, as tannate [drops]:
Ed Chlorped: 2 mg/mL (60 mL) [DSC]
Syrup, oral, as maleate:
Aller-Chlor®: 2 mg/5 mL (118 mL) [contains ethanol 5%, propylene glycol]
Diabetic Tussin® for Children Allergy Relief: 2 mg/5 mL (118 mL) [dye free, ethanol free, sugar free; contains phenylalanine 8.4 mg/5 mL]
Tablet, oral, as maleate: 4 mg
Aller-Chlor®: 4 mg [scored]
Chlor Hist: 4 mg
Chlor-Trimeton® Allergy: 4 mg
Chlorphen: 4 mg
Ed-Chlortan: 4 mg [scored]
Teldrin® HBP: 4 mg
Tablet, extended release, oral, as maleate:
Chlor-Trimeton® Allergy: 12 mg
Tablet, extended release, oral, as tannate:
Ed-Chlor-Tan: 8 mg [DSC]
Tablet, long acting, oral, as tannate:
Ahist™: 12 mg [scored]
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
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