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clemastine

 

Classes: Antihistamines, 1st Generation

Dosing and uses of Clemastine

 

Adult dosage forms and strengths

tablet

  • 1.34mg
  • 2.68mg

syrup

  • 0.67mg/5mL

 

Allergic Rhinitis

1.34 mg PO q12hr; not to exceed 8.04 mg/day for syrup or 2.68 mg/24 hours for tablets

 

Urticaria

2.68 mg PO qDay-q8hr; not to exceed 8.04 mg/day

 

Angioedema

2.68 mg PO qDay-q8hr; not to exceed 8.04 mg/day

 

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

  • 1.34mg
  • 2.68mg

syrup

  • 0.67mg/5mL

 

Allergic Rhinitis

<6 years old: 0.05 mg/kg/day as clemastine base or 0.335-0.67 mg/day clemastine fumarate (0.25-0.5 mg base/day) divided q8-12hr; not to exceed 1.34 mg (1 mg base)

6-12 years old: 0.67-1.34 mg clemastine fumarate (0.5-1 mg base) q12hr; not to exceed 4.02 mg/day (3 mg/day base)

>12 years old: As in adults

 

Urticaria

<6 years old: 0.05 mg/kg/day as clemastine base or 0.335-0.67 mg/day clemastine fumarate (0.25-0.5 mg base/day) divided q8-12hr; not to exceed 1.34 mg (1 mg base)

6-12 years old: 0.67-1.34 mg clemastine fumarate (0.5-1 mg base) q12hr; not to exceed 4.02 mg/day (3 mg/day base)

>12 years old: As in adults

 

Geriatric dosage forms and strengths

Administer lower doses to patients >60 years

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

 

Allergic Rhinitis

1.34 mg PO q12hr; not to exceed 8.04 mg/day for syrup or 2.68 mg/24 hours for tablets

 

Urticaria

2.68 mg PO qDay-q8hr; not to exceed 8.04 mg/day

 

Angioedema

2.68 mg PO qDay-q8hr; not to exceed 8.04 mg/day

 

Clemastine 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

Eczema, pruritus, inflammation, papular rash, erythema on exposed skin may occur with topical formulation

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

 

Caution

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

 

Pregnancy and lactation

Pregnancy category: B

Lactation: enters breast milk/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 Clemastine

Mechanism of action

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

 

Pharmacokinetics

Onset: 5-7 hr

Duration: 8-12 hr

Peak Plasma Time: 2-5 hr

Vd: 800 L

Metabolism: Hepatic

Bioavailability: ~40%

Half-life elimination: 21 hr

Excretion: Urine

Sedation: Low to moderate

Antihistamine activity: Low to moderate

Anticholinergic activity: High

Antiemetic effects: Low to moderate