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chlorpheniramine (ChlorTrimeton, Diabetic Tussin)

 

Classes: Antihistamines, 1st Generation

Dosing and uses of ChlorTrimeton, Diabetic Tussin (chlorpheniramine)

 

Adult dosage forms and strengths

tablet

  • 4mg
  • 8mg
  • 12mg

syrup

  • 2mg/5mL

 

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

 

Pediatric dosage forms and strengths

tablet

  • 4mg
  • 8mg
  • 12mg

suspension

  • 2mg/mL

syrup

  • 2mg/5mL

 

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

 

Geriatric dosage forms and strengths

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

 

ChlorTrimeton, Diabetic Tussin (chlorpheniramine) adverse (side) 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

 

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

 

Pregnancy and lactation

Pregnancy category: C

Lactation: excretion in milk unknown/not recommended

 

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.

 

Pharmacology of ChlorTrimeton, Diabetic Tussin (chlorpheniramine)

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

Onset: 6 hr

Peak Plasma Time: 2-3 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

 

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