What is diphenhydramine, and how does it work (mechanism of action)?

Diphenhydramine is an antihistamine used for treating allergic reactions. Histamine is released by the body during several types of allergic reactions and--to a lesser extent--during some viral infections, such as the common cold. When histamine binds to receptors on cells, it stimulates changes within the cells that lead to the release of chemicals that cause sneezing, itching, and increased mucus production. Antihistamines compete with histamine for cell receptors and bind to the receptors without stimulating the cells. In addition, they prevent histamine from binding and stimulating the cells. Diphenhydramine also blocks the action of acetylcholine (anticholinergic effect) and is used as a sedative because it causes drowsiness. The FDA originally approved diphenhydramine in 1946.

BRAND NAME:

Benadryl, Sominex, Unisom, Nytol, and several others

GENERIC AVAILABLE:

Yes

PRESCRIPTION AVAILABLE:

No. Yes (Injection)

What are the side effects of diphenhydramine?

Diphenhydramine commonly can cause:

• sedation,
• tiredness,
• sleepiness,
• dizziness,
• constipation,
• disturbed coordination,
• drying and thickening of oral and other respiratory secretions, and
• urinary retention.

Diphenhydramine also may cause

• low blood pressure,
• palpitations (abnormal heartbeats),
• increased heart rate,
• confusion,
• nervousness,
• irritability,
• blurred vision,
• double vision,
• painful urination or difficulty urinating,
• tremor,
• sweating,
• loss of appetite,
• erectile dysfunction, and
• nausea.

Diphenhydramine should be used with caution (if at all) in persons with narrow-angle glaucoma, prostatic hypertrophy (enlarged prostate gland), hyperthyroidism, cardiovascular disease, high blood pressure (hypertension), and asthma.

What is the dosage for diphenhydramine?

Diphenhydramine doses vary depending on formulation, and has its maximal effect about one hour after it is taken.

• When used to treat insomnia, it is prescribed at bedtime. Indivduals over the age of 60 years are especially sensitive to the sedating and anticholinergic effects of diphenhydramine, and the dose should be reduced.
• A common regimen for treating adult allergic reaction is 25-50 mg every 4-6 hours not to exceed 300 mg daily.
• Insomnia is treated with 50 mg taken 30 minutes before bedtime.

Which drugs or supplements interact with diphenhydramine?

:

Diphenhydramine adds to (exaggerates) the sedating effects of alcohol and other drugs than can cause sedation such as the benzodiazepine class of anti-anxiety (for example, diazepam [Valium], lorazepam [Ativan], clonazepam [Klonopin], alprazolam [Xanax]), the narcotic class of pain medications and its derivatives (for example, oxycodone and acetaminophen [Percocet], and hydrocodone and acetaminophen [Vicodin], guaifenesin with hydromorphone [Dilaudid], codeine, propoxyphene [Darvon]), the tricyclic class of antidepressants (for example, amitriptyline [Elavil, Endep], imipramine [Tofranil], desipramine [Norpramin]), and certain antihypertensive medications (for example, clonidine [Catapres], propranolol [Inderal]). Diphenhydramine also can intensify the drying effects of other medications with anticholinergic properties (for example, dicyclomine [Bentyl] and bethanechol [Urecholine], probanthine).

Is diphenhydramine safe to take if I'm pregnant or breastfeeding?

Diphenhydramine has not been adequately evaluated in pregnant women. It should be used only if the benefit outweighs the potential but unknown risks.

NURSING MOTHERS: Diphenhydramine is secreted in breast milk. Because of the risk of stimulation and seizures in infants, especially newborns and premature infants, antihistamines should not be used by nursing mothers.

What else should I know about diphenhydramine?

What preparations of diphenhydramine are available?

• Capsules: 25 and 50 mg. Tablets: 12.5, 25 and 50 mg.
• Tablet (Chewable or dispersible)): 12.5 mg.
• Strips: 12.5 and 25 mg.
• Elixir, oral solution, liquid: 12.5 mg per teaspoon (5 mL).
• Strip: 25 mg. Injection: 50 mg per ml.

How should I keep diphenhydramine stored?

Diphenhydramine should be stored at room temperature, 15 C to 30 C (59 F to 86 F), and the injection should be protected from freezing and light.