DIPHENHYDRAMINE
THERAPEUTICS
Class
- Antihistamine; anticholinergic agent
DIPHENHYDRAMINE commonly prescribed for
(Bold for FDA approved)
How DIPHENHYDRAMINE works
• For drug-induced parkinsonism: diminishes the excess acetylcholine activity caused by removal of dopamine inhibition when dopamine receptors are blocked</br>
• Also has potent histamine 1 antagonist properties
How long until DIPHENHYDRAMINE works
• For drug-induced parkinsonism, onset of action can be within minutes or hours
SIDE EFFECTS
Notable Side Effects
• Sedation, dizziness
• Constipation, nausea
• Dry mouth, blurred vision
Life Threatening Side Effects
• Rare convulsions (at high doses)
• Urinary retention
• Tachycardia, cardiac arrhythmias
• Confusion
• Paralytic ileus/bowel obstruction
weight gain

problematic
sedation

common
What to do about DIPHENHYDRAMINE side effects
• For confusion or hallucinations, discontinue use
• For sedation, lower the dose and/or take the entire dose at night
• For dry mouth, chew gum or drink water
• For urinary retention, obtain a urological evaluation; may need to discontinue use
DOSING AND USE
usual dosage range
• Oral: 50 mg/day
• Injection: 10–50 mg
Dosage Forms
• Injection 50 mg/mL
• Capsule 50 mg
• Elixir 12.5 mg/5 mL
• Also available in formulations in combination with other medications
long term use
• Safe
• Effectiveness may decrease over time, even after a few doses, but side effects such as cognitive impairment and sedation may persist
habit forming
• No
SPECIAL POPULATIONS
Renal Impairment
• No dose adjustment necessary
Hepatic Impairment
• No dose adjustment necessary
Cardiac Impairment
• Not systematically evaluated in patients with cardiac impairment
Elderly
• Some patients may tolerate lower doses better
• Diphenhydramine injection is preferred for parkinsonism in the elderly who are unable to tolerate more potent agents
Children and Adolescents
• Not recommended for children under age 12
• Injection: 5 mg/kg/24 hours or 150 mg/ m2 /24 hours; maximum daily dose 300 mg; divide into 4 doses; can be given intravenously at a rate not exceeding 25 mg/minute, or deep intramuscularly
• Contraindicated in neonates and premature infants
Pregnancy
• Controlled studies have not been conducted in pregnant women
• Animal studies have not shown adverse effects
Breast Feeding
• Contraindicated
Based on data Published online by Cambridge University Press
Compiled by Dr. Jash Ajmera