Benadryl (diphenhydramine hydrochloride) is an antihistamine drug having the chemical name 2-(Diphenylmethoxy)-N,N-dimethylethylamine hydrochloride. It occurs as a white, crystalline powder, is freely soluble in water and alcohol and has a molecular weight of 291.82. The molecular formula is C₁₇H₂₁NO • HCl, and structural formula:

Benadryl in the parenteral form is a sterile, pyrogen-free solution available in a concentration of 50 mg of diphenhydramine hydrochloride per mL. The solutions for parenteral use have been adjusted to a pH between 5.0 and 6.0 with either sodium hydroxide or hydrochloric acid. The multidose Steri-Vials^® contain 0.1 mg/mL benzethonium chloride as a germicidal agent.

Benadryl in the injectable form is effective in adults and pediatric patients, other than premature infants and neonates, for the following conditions when Benadryl in the oral form is impractical.

Antihistaminic

For amelioration of allergic reactions to blood or plasma, in anaphylaxis as an adjunct to epinephrine and other standard measures after the acute symptoms have been controlled, and for other uncomplicated allergic conditions of the immediate type when oral therapy is impossible or contraindicated.

Motion sickness

For active treatment of motion sickness.

Antiparkinsonism

For use in parkinsonism, when oral therapy is impossible or contraindicated, as follows: parkinsonism in the elderly who are unable to tolerate more potent agents; mild cases of parkinsonism in other age groups, and in other cases of parkinsonism in combination with centrally acting anticholinergic agents.

THIS PRODUCT IS FOR INTRAVENOUS OR INTRAMUSCULAR ADMINISTRATION ONLY.

Benadryl in the injectable form is indicated when the oral form is impractical.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

DOSAGE SHOULD BE INDIVIDUALIZED ACCORDING TO THE NEEDS AND THE RESPONSE OF THE PATIENT.

Pediatric Patients, other than premature infants and neonates: 5 mg/kg/24 hr or 150 mg/m²/24 hr. Maximum daily dosage is 300 mg. Divide into four doses, administered intravenously at a rate generally not exceeding 25 mg/min, or deep intramuscularly.

Adults: 10 to 50 mg intravenously at a rate generally not exceeding 25 mg/min, or deep intramuscularly, 100 mg if required; maximum daily dosage is 400 mg.

Benadryl in parenteral form is supplied as:

Benadryl Steri-Vials^®

-sterile, pyrogen-free solution containing 50 mg diphenhydramine hydrochloride in each milliliter of solution with 0.1 mg/mL benzethonium chloride as a germicidal agent. Available in 10-mL (NDC 0071-4402-10) Steri-Vials.

-sterile, pyrogen-free solution containing 50 mg diphenhydramine hydrochloride in each milliliter of solution. Available in packages of twenty-five 1 mL (NDC 0071-4259-13) Steri-Vials.

Benadryl Steri-Dose^®

-sterile, pyrogen-free solution containing 50 mg diphenhydramine hydrochloride in a 1-mL disposable syringe (Steri-Dose). Available in packages of ten syringes (NDC 0071-4259-45).

Benadryl Ampoule

-sterile, pyrogen-free solution containing 50 mg diphenhydramine hydrochloride in a 1-mL ampoule. Available in packages of ten (NDC 0071-4259-03).

Store at controlled room temperature 15°-30°C (59°-86°F). Protect from freezing and light.

Rx only

The most frequent adverse reactions are underscored.

General: Urticaria, drug rash, anaphylactic shock, photosensitivity, excessive perspiration, chills, dryness of mouth, nose, and throat

Cardiovascular System: Hypotension, headache, palpitations, tachycardia, extrasystoles

Hematologic System: Hemolytic anemia, thrombocytopenia, agranulocytosis

Nervous System: Sedation, sleepiness, dizziness, disturbed coordination, fatigue, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, euphoria, paresthesia, blurred vision, diplopia, vertigo, tinnitus, acute labyrinthitis, neuritis, convulsions

GI System: Epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation

GU System: Urinary frequency, difficult urination, urinary retention, early menses

Respiratory System: Thickening of bronchial secretions, tightness of chest or throat and wheezing, nasal stuffiness

Diphenhydramine hydrochloride has additive effects with alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, etc).

MAO inhibitors prolong and intensify the anticholinergic (drying) effects of antihistamines.

Antihistamines should be used with considerable caution in patients with narrow-angle glaucoma, stenosing peptic ulcer, pyloroduodenal obstruction, symptomatic prostatic hypertrophy, or bladder-neck obstruction.

Local necrosis has been associated with the use of subcutaneous or intradermal use of intravenous Benadryl.

Use in Pediatric Patients

In pediatric patients, especially, antihistamines in overdosage may cause hallucinations, convulsions, or death.

As in adults, antihistamines may diminish mental alertness in pediatric patients. In the young pediatric patient, particularly, they may produce excitation.

Use in the Elderly (approximately 60 years or older)

Antihistamines are more likely to cause dizziness, sedation, and hypotension in elderly patients.

General

Diphenhydramine hydrochloride has an atropine-like action and therefore, should be used with caution in patients with a history of bronchial asthma, increased intraocular pressure, hyperthyroidism, cardiovascular disease or hypertension. Use with caution in patients with lower respiratory disease including asthma.

Information for Patients

Patients taking diphenhydramine hydrochloride should be advised that this drug may cause drowsiness and has an additive effect with alcohol.

Patients should be warned about engaging in activities requiring mental alertness such as driving a car or operating appliances, machinery, etc..

Drug Interactions

Diphenhydramine hydrochloride has additive effects with alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, etc).

MAO inhibitors prolong and intensify the anticholinergic (drying) effects of antihistamines.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term studies in animals to determine mutagenic and carcinogenic potential have not been performed.

Pregnancy

Pregnancy Category B. Reproduction studies have been performed in rats and rabbits at doses up to 5 times the human dose and have revealed no evidence of impaired fertility or harm to the fetus due to diphenhydramine hydrochloride. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Pediatric Use

Benadryl should not be used in neonates and premature infants (see CONTRAINDICATIONS).

Benadryl may diminish mental alertness, or, in the young pediatric patient, cause excitation. Overdosage may cause hallucinations, convulsions, or death (see WARNINGS, OVERDOSAGE, and DOSAGE AND ADMINISTRATION sections).

Antihistamine overdosage reactions may vary from central nervous system depression to stimulation. Stimulation is particularly likely in pediatric patients. Atropine-like signs and symptoms; dry mouth; fixed, dilated pupils; flushing; and gastrointestinal symptoms may also occur. Stimulants should not be used.

Vasopressors may be used to treat hypotension.

Use in Neonates or Premature Infants

This drug should not be used in neonates or premature infants.

Use in Nursing Mothers

Because of the higher risk of antihistamines for infants generally, and for neonates and prematures in particular, antihistamine therapy is contraindicated in nursing mothers.

Use as a Local Anesthetic

Because of the risk of local necrosis, this drug should not be used as a local anesthetic.

Antihistamines are also contraindicated in the following conditions: Hypersensitivity, to diphenhydramine hydrochloride and other antihistamines of similar chemical structure.

Diphenhydramine hydrochloride is an antihistamine with anticholinergic (drying) and sedative side effects. Antihistamines appear to compete with histamine for cell receptor sites on effector cells.

Benadryl in the injectable form has a rapid onset of action. Diphenhydramine hydrochloride is widely distributed throughout the body, including the CNS. A portion of the drug is excreted unchanged in the urine, while the rest is metabolized via the liver. Detailed information on the pharmacokinetics of Diphenhydramine Hydrochloride Injection is not available.

Patients taking diphenhydramine hydrochloride should be advised that this drug may cause drowsiness and has an additive effect with alcohol.

Patients should be warned about engaging in activities requiring mental alertness such as driving a car or operating appliances, machinery, etc.

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

DIPHENHYDRAMINE - INJECTION

(dye-fen-HI-druh-meen)

COMMON BRAND NAME(S): Benadryl

USES: Diphenhydramine injection is an antihistamine used to treat life-threatening allergic reactions (anaphylaxis) along with epinephrine and other treatments. It is also used to relieve symptoms of household allergies, hay fever and the common cold when medication cannot be given by mouth. Common allergy symptoms relieved by antihistamines include rash, itching, watery eyes, itchy eyes/nose/throat, cough, runny nose and sneezing.

It is also used to treat nausea, vomiting and dizziness caused by motion sickness when medication cannot be given by mouth. Diphenhydramine works by blocking a certain natural substance (histamine) that your body makes during an allergic reaction. Its drying effects on such symptoms as watery eyes and runny nose are caused by blocking another natural substance made by your body (acetylcholine).

Diphenhydramine should not be used in newborns or premature infants because of an increased risk of side effects.

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

Diphenhydramine injection is also used alone or with other medications to treat shaking (tremor) and muscle stiffness caused by Parkinson's disease when medication cannot be given by mouth. It may also be used to treat side effects of certain psychiatric drugs such as involuntary movements and muscle stiffness (e.g., EPS). It works by blocking acetylcholine. (See also Uses section.)

HOW TO USE: This medication is injected into a vein (IV) no faster than 25 milligrams per minute, or deeply into a muscle as directed by your doctor. Be very careful to inject into a vein or muscle and not into the skin or just under the skin. If this medication is injected into or just under the skin, it can destroy the skin and tissues around the injection site (necrosis).

If you are giving this injection to yourself, be sure you learn the proper technique for injecting this drug. Before injecting each dose, clean the injection site with rubbing alcohol. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Follow your doctor's directions carefully. Learn how to store and discard needles and medical supplies safely. Consult your pharmacist.

Do not use this medication more often than prescribed. Your dosage is based on your medical condition and response to therapy. Inform your doctor if your condition does not improve or if it worsens.

SIDE EFFECTS: Drowsiness, dizziness, headache, irritability, stomach upset, vision changes (e.g., blurred vision), decreased coordination, or dry mouth/nose/throat may occur. These effects may decrease as your body adjusts to the medication. If they persist or become bothersome, inform your doctor.

To relieve dry mouth, suck on (sugarless) hard candy or ice chips, chew (sugarless) gum, drink water or use a saliva substitute. Diphenhydramine can dry up and thicken the mucus in your lungs, making it more difficult to breathe and clear your lungs. To help prevent this effect, be sure to drink plenty of fluids unless otherwise directed by your physician.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these rare but serious side effects occur: pounding/irregular heartbeat, ringing in the ears, seizure, difficulty urinating.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using diphenhydramine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: breathing problems (e.g., asthma, emphysema), glaucoma, heart problems, high blood pressure, liver disease, mental/mood disorders, seizures, stomach problems (e.g., ulcers, obstruction), overactive thyroid, difficulty urinating (e.g., enlarged prostate, urinary retention).

This drug may make you dizzy or drowsy or cause blurred vision. Use caution engaging in activities requiring alertness such as driving or using machinery. Limit the use of alcohol and certain other drowsiness-causing medications (for more details, see Drug Interactions). To minimize dizziness and lightheadedness, get up slowly when rising from a seated or lying position.

Caution is advised when using this drug in children because they are more sensitive to the effects of antihistamines. This drug can often cause excitement in young children instead of drowsiness.

Caution is advised when using this drug in the elderly because they may be more sensitive to its effects, especially dizziness, drowsiness and low blood pressure.

This medication should be used only when clearly needed during pregnancy. Tell your doctor if you are pregnant before using this medication.

This drug passes into breast milk and may have undesirable effects on a nursing infant. Therefore, breast-feeding is not recommended while using this medication. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: antispasmodics (e.g., atropine, belladonna alkaloids), drugs for Parkinson's disease (e.g., anticholinergics such as benztropine, trihexyphenidyl), MAO inhibitors (e.g., furazolidone, isocarboxazid, linezolid, moclobemide, phenelzine, procarbazine, rasagiline, selegiline, tranylcypromine), tricyclic antidepressants (e.g., amitriptyline).

Tell your doctor or pharmacist if you also take drugs that cause drowsiness such as: certain antihistamines (e.g., dimenhydrinate), anti-seizure drugs (e.g., carbamazepine), medicine for sleep or anxiety (e.g., alprazolam, diazepam, zolpidem), muscle relaxants, narcotic pain relievers (e.g., codeine), psychiatric medicines (e.g., chlorpromazine, risperidone, amitriptyline, trazodone). Check the labels on all your medicines (e.g., cough-and-cold products) because they may contain drowsiness-causing ingredients. Ask your pharmacist about the safe use of those products.

Check the labels on all your medicines because they may also contain diphenhydramine or other antihistamines (e.g., dimenhydrinate). This includes medications taken by mouth or applied to the skin (e.g., anti-itch cream, ointment, spray). Ask your pharmacist about the safe use of those products.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly. Symptoms of overdose may include large pupils, flushing, fever, hallucinations, weakness, shaking (tremor), muscle twitching, loss of consciousness, and seizures. In children, excitement may occur first, followed by loss of coordination, drowsiness, loss of consciousness, and seizures.

NOTES: Do not take for several days before allergy testing. Test results can be affected.

Do not share this medication with others.

MISSED DOSE: If you miss a dose, use it as soon you remember. If it is near the time of your next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature between 59-86 degrees F (between 15-30 degrees C) away from moisture and light. Do not store in the bathroom. Do not freeze. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.