chlorpheniramine (OTC)

Brand and Other Names:ChlorTrimeton, Diabetic Tussin
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 4mg
  • 8mg
  • 12mg

syrup

  • 2mg/5mL
more...

Allergic Rhinitis

Tablets or syrup: 4 mg PO q4-6hr; not to exceed 24 mg/day

Extended-release tablets: 8 mg PO q8-12hr or 12 mg q12hr; not to exceed 24 mg/day

Extended-release capsules: 12 mg PO qDay; not to exceed 24 mg/day

Sustained-release capsules: 8-12 mg PO q8-12hr, up to 16-24 mg/day

Additional Information

See also combo with hydrocodone (Tussionex)

Other Indications & Uses

Perennial & seasonal allergic & vasomotor rhinitis, relief of symptoms from colds, urticaria, angioedema, anaphylactic reactions, pruritus, allergic conjunctivitis

Dosage Forms & Strengths

tablet

  • 4mg
  • 8mg
  • 12mg

suspension

  • 2mg/mL

syrup

  • 2mg/5mL
more...

Allergic Rhinitis

<2 years: Safety & efficacy not established

2-6 years: 1 mg PO q4-6hr; not to exceed 6 mg/day

6-12 years: 2 mg PO q4-6hr; not to exceed 12 mg/day or sustained release HS

>12 years

  • Tablets or syrup: 4 mg PO q4-6hr; not to exceed 24 mg/day
  • Extended-release tablets: 8 mg PO q8-12hr or 12 mg q12hr; not to exceed 24 mg/day
  • Extended-release capsules: 12 mg PO qDay; not to exceed 24 mg/day
  • Sustained-release capsules: 8-12 mg PO q8-12hr, up to 16-24 mg/day

4 mg PO qDay or q12hr

Sustained-release: 8 mg PO qHS

Nonanticholinergic antihistamines should be considered first when treating allergic reactions (Beers Criteria)

Avoid use in elderly because of high incidence of anticholinergic effects

Clearance reduced with advanced age, greater risk of confusion, dry mouth, constipation, and other anticholinergic effects and toxicity

May exacerbate existing lower urinary conditions or benign prostatic hyperplasia

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Interactions

Interaction Checker

and chlorpheniramine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Varies in incidence & severity with the individual drug; also individual patients vary in susceptibility

            Frequency Not Defined

            CNS depression

            Drowsiness

            Sedation ranging from mild drowsiness to deep sleep (most frequent)

            Dizziness

            Lassitude

            Disturbed coordination

            Muscular weakness

            Restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures is less common

            Epigastric distress

            Anorexia

            Nausea

            Vomiting

            Diarrhea

            Constipation

            Cholestasis, hepatitis, hepatic failure, hepatic function abnormality, jaundice is rare

            Tachycardia, palpitation ECG changes (eg, widened QRS)

            Arrhythmias (eg, extrasystole, heart block)

            Hypotension

            Hypertension

            Dizziness, sedation, and hypotension may occur in geriatric patients

            Dryness of mouth, nose, and throat

            Dysuria

            Urinary retention

            Impotence

            Vertigo

            Visual disturbances

            Blurred vision

            Diplopia; tinnitus

            Acute labyrinthitis

            Insomnia

            Tremors

            Nervousness

            Irritability

            Facial dyskinesia

            Tightness of the chest

            Thickening of bronchial secretions

            Wheezing

            Nasal stuffiness

            Sweating

            Chills

            Early menses

            Toxic psychosis

            Headache

            Faintness

            Paresthesia

            Agranulocytosis

            Hemolytic anemia

            Leukopenia

            Thrombocytopenia

            Pancytopenia

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            Warnings

            Contraindications

            Documented hypersensitivity

            Lower respiratory disease, eg, asthma (controversial)

            Preemies & neonates

            Nursing women

            Acute asthma, sleep apnea

            Cautions

            Caution in narrow angle glaucoma, prostatic hypertrophy, stenosing peptic ulcer, pyloroduodenal obstruction, or bladder neck obstruction

            Chlor Trimeton non-drowsy contains no chlorpheniramine, only pseudoephedrine

            All injections discontinued

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            Pregnancy & Lactation

            Pregnancy

            Antihistamine exposure in first trimester not reported to be associated with increased risk of malformations; animal studies not reported; there are no controlled data in human pregnancy; only recommended for use during pregnancy when benefit outweighs risk

            Lactation

            Excretion into human milk; the manufacturer recommends that caution be used when administering chlorpheniramine to nursing women; infants should be monitored for irritability or drowsiness; antihistamines may temporarily decrease maternal serum prolactin concentrations when administered prior to nursing infant for the first time

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Histamine H1-receptor antagonist in blood vessels, respiratory tract, and gastrointestinal tract

            Pharmacokinetics

            Half-Life elimination: 10-13 hr (children); 14-24hr (adult)

            Duration: 24 hr

            Peak Plasma Time: 2-3 hr (range 1-6 hr)

            Protein Bound: 29-37%

            Vd: 4-7 L/kg (children); 6-12 L/kg (adults)

            Metabolism: Liver (CYP2D6)

            Metabolites: Monodesmethylchlorpheniramine, didesmethylchlorpheniramine

            Excretion: Urine

            Sedative effect: Low

            Antihistamine activity: Moderate

            Anticholinergic acitivity: Moderate

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            Administration

            Parenteral forms discontinued

            IV Compatibilities

            Additive: amikacin, calcium chloride, kanamycin, norepinephrine, pentobarbital

            Syringe: diatrizoate meglumine, diatrizoate sodium, iodipamide meglumine, iothalamate meglumine, iothalamate sodium

            IV/IM Administration

            Administer SC/IM/IV injection over 1 min

            100 mg/mL injection should not be given IV

            Storage

            Store at 25C

            Protect from light

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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.