Promethazine 

is a first-generation H1 receptor antagonist of the phenothiazine chemical classused

medically as an antihistamine antiemetic. It has a strong sedative effect and in some countries is
prescribed for insomnia when benzodiazepines are contraindicated. It is availableover the counter in
the United Kingdom, Australia, Canada, Switzerland, and many other countries, but by prescription in
the United States (brand
names Phenergan, Promethegan,Romergan, Fargan, Farganesse, Prothiazine, Avomine, Atosil, Re
ceptozine,Lergigan)

Chemically, promethazine hydrochloride appears as a white to faint yellow crystlline powder that is

practically odorless. Slow oxidation may occur upon prolonged exposure to air usually causing blue
discoloration. Promethazine as the hydrochloride salt is freely soluble in water and somewhat soluble in
alcohol. Promethazine is a chiral compound, occurring as a mixture of enantiomers (pictured).[2]

[edit]Indications

 As a sedative.[3]
 For preoperative sedation and to counteract postnarcotic nausea.[3]
 As antiallergic medication to combat hay fever (allergic rhinitis), etc. To treat allergic reactions it
can be given alone or in combination with oral decongestants likepseudoephedrine.[3]
 As an adjunct treatment for anaphylactoid conditions (IM/IV route preferred).[3]
 Together with codeine or dextromethorphan against cough.
 As a motion sickness or seasickness remedy when used with Ephedrine or Pseudoephedrine.[3]
 To combat moderate to severe morning sickness and hyperemesis gravidarum. In
the UK promethazine is drug of first choice, being preferred as an older drug with which there is a
greater experience of use in pregnancy (second line being metoclopramide orprochlorperazine).[4]
 Previously it was used as an antipsychotic,[5] although it is generally not administered for this
purpose now; promethazine has only approximately 1/10 of the antipsychotic strength
of chlorpromazine.
 Also used to potentiate any opiates. Commonly combined with pethidine (AKA, meperidine, or
Demerol) in a brand called Mepergan, a meperidine/promethazine combination. Also frequently used
in conjunction with codeine, in a syrup form. The combination leads to more powerful euphoric effects
than with codeine alone.
[edit]Mechanism of action

 Promethazine is a phenothiazine derivative that competitively blocks histamine H1 receptors

without blocking the secretion of histamine. It also is a very weak dopamine antagonist.[6]
 It has sedative, anti-motion-sickness, anti-emetic, and anti-cholinergic effects.[citation needed]
[edit]Side effects
Some common side effects include:

 Confusion in the elderly

 Drowsiness, dizziness, fatigue, more rarely vertigo
 Dry mouth
 Respiratory depression in patients under age of 2 and in those with severely compromised
pulmonal function
 Constipation
 Chest Discomfort/Pressure. (typically in cases when patient is already taking medication for high
blood pressure)
 Euphoria (very rare, except with high IV doses and/or coadministration with opioids/CNS
depressants)
 Restless legs [7]
 Paresthesia
 Short temper/Irritability

Extremely rare side effects include:

 Seizures
 Neuroleptic malignant syndrome

IV administration: Dilute with 0.9% NaCl or D5W. CONCENTRATION: Doses should not exceed a
concentration of 25 mg/ml. Administer through a large-bore vein through a running IV line into the most
distal port. Slight yellow color does not alter potency. Do not administer if precipitate is present. RATE:
Administer each 25 mg slowly, over at least 10-15min. Rapid administration may produce a transient fall
in blood pressure. [8] Serious complications including those listed above have resulted from improper
parenteral administration, including those requiring surgical intervention and amputation.

Because of potential for more severe side effects, this drug is on the list to avoid in the elderly. (See
NCQA’s HEDIS Measure: Use of High Risk Medications in the Elderly).

[edit]Laboratory examinations
All patients should have their blood pressure measured frequently. During long-term therapy, blood cell
counts, liver function studies, EKG, and EEG are recommended. The intervals should be determined
according to the risk profile of the patient. In high doses, promethazine can create auditory and visual
hallucinations causing panic and intense fear.[citation needed]
[edit]Product liability lawsuit
Main article:  Wyeth v. Levine

In 2009, the U.S. Supreme Court ruled on a product liability case involving promethazine. Diana Levine, a
woman suffering from a migraine, was administered Wyeth's Phenergan via IV push. The drug was
injected improperly resulting in gangrene and subsequent amputation of her right forearm below the
elbow. A state jury awarded her $6 million in punitive damages.

The case was appealed to the Supreme Court on grounds of federal preemption and substantive due
process.[9] The Supreme Court upheld the lower courts' rulings stating that "Wyeth could have unilaterally
added a stronger warning about IV-push administration" without acting in opposition to federal law.[10] In
effect, this means that drug manufacturers can be held liable for injuries if warnings of potential adverse
effects (approved by the U.S. Food and Drug Administration, "FDA") are deemed insufficient by state
courts.

On September 9, 2009, the FDA made the decision that a black box warning for injection be put on
promethazine stating the contraindication for subcutaneous administration. The preferred administrative
route is intramuscular (IM) which reduces risk of surrounding muscle and tissue damage [11]
 Promethazine may cause breathing to slow or stop, and may cause death in children. Promethazine
should not be given to babies or children who are younger than 2 years old and should be given with
caution to children who are 2 years of age or older. Combination products containing promethazine and
codeine should not be given to children younger than 16 years old. Promethazine should not routinely be
used to treat vomiting in children; it should only be used in specific cases when a doctor decides that it is
needed. Tell your child's doctor if your child has any condition that affects his/her breathing such as lung
disease, asthma, or sleep apnea (stops breathing for short periods of time during sleep). Tell your doctor
or pharmacist about all the medications your child is taking, especially barbiturates such as phenobarbital
(Luminal), medications for anxiety, narcotic medications for pain, sedatives, sleeping pills, and
tranquilizers. Call your child's doctor immediately and get emergency medical treatment if your child has
difficulty breathing, wheezes, slows or pauses in breathing, or stops breathing.

Talk to your doctor about the risks of giving promethazine to your child.

Why is this medication prescribed?

Promethazine is used to relieve the symptoms of allergic reactions such as allergic rhinitis (runny nose
and watery eyes caused by allergy to pollen, mold or dust), allergic conjunctivitis (red, watery eyes
caused by allergies), allergic skin reactions, and allergic reactions to blood or plasma products.
Promethazine is used with other medications to treat anaphylaxis (sudden, severe allergic reactions) and
the symptoms of the common cold such as sneezing, cough, and runny nose. Promethazine is also used
to relax and sedate patients before and after surgery, during labor, and at other times. Promethazine is
also used to prevent and control nausea and vomiting that may occur after surgery, and with other
medications to help relieve pain after surgery. Promethazine is also used to prevent and treat motion
sickness. Promethazine helps control symptoms, but will not treat the cause of the symptoms or speed
recovery. Promethazine is in a class of medications called phenothiazines. It works by blocking the action
of a certain natural substance in the body.

How should this medicine be used?

Promethazine comes as a tablet, capsule, and syrup (liquid) to take by mouth and as a suppository to use
rectally. When promethazine is used to treat allergies, it is usually taken one to four times daily, before
meals and/or at bedtime. When promethazine is used to relieve cold symptoms, it is usually taken every 4
to 6 hours as needed. When promethazine is used to treat motion sickness, it is taken 30 to 60 minutes
before travel and again after 8 to 12 hours if needed. On longer trips, promethazine is usually taken in the
morning and before the evening meal on each day of travel. When promethazine is used to treat or
prevent nausea and vomiting it is usually taken every 4 to 6 hours as needed. Promethazine may also be
taken at bedtime the night before surgery to relieve anxiety and produce quiet sleep. Follow the directions
on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not
understand. Take promethazine exactly as directed. Do not take more or less of it or take it more often
than prescribed by your doctor.

Promethazine suppositories are for rectal use only. Do not try to swallow the suppositories or insert in any
other part of your body.
If you are taking promethazine liquid, do not use a household spoon to measure your dose. Use the
measuring spoon or cup that came with the medication or use a spoon made especially for measuring
medication.

To insert a promethazine suppository, follow these steps:

1. If the suppository feels soft, hold it under cold, running water for 1 minute. Remove the wrapper.
2. Dip the tip of the suppository in water.
3. Lie down on your left side and raise your right knee to your chest. (A left-handed person should
lie on the right side and raise the left knee.)
4. Using your finger, insert the suppository into the rectum, about 1/2 to 1 inch (1.25 to 2.5
centimeters) in children who are 2 years of age older and 1 inch (2.5 centimeters) in adults. Hold
it in place for a few moments.
5. Stand up after about 15 minutes. Wash your hands thoroughly and resume your normal activities.

Other uses for this medicine

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This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

What special precautions should I follow?

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Before taking promethazine,

 tell your doctor and pharmacist if you are allergic to promethazine, other phenothiazines (certain
medications used to treat mental illness, nausea, vomiting, severe hiccups, and other conditions)
or any other medications. Also tell your doctor and pharmacist if you have ever had an unusual or
unexpected reaction when you took promethazine, another phenothiazine, or any other
medication. Ask your doctor or pharmacist if you do not know if a medication you are allergic to is
a phenothiazine.
 tell your doctor and pharmacist what prescription and nonprescription medications, vitamins,
nutritional supplements and herbal products you are taking or plan to take. Be sure to mention
any of the following: antidepressants ('mood elevators') such as amitriptyline (Elavil), amoxapine
(Asendin), clomipramine (Anafranil), desipramine (Norpramin), doxepin (Adapin, Sinequan),
imipramine (Tofranil), nortriptyline (Aventyl, Pamelor), protriptyline (Vivactil), and trimipramine
(Surmontil); antihistamines; azathioprine (Imuran);barbiturates such as phenobarbital (Luminal);
cancer chemotherapy; epinephrine (Epipen); ipratropium (Atrovent)medications for anxiety,
irritable bowel disease, mental illness, motion sickness, Parkinson's disease, seizures, ulcers, or
urinary problems; monoamine oxidase (MAO) inhibitors such as isocarboxazid (Marplan),
phenelzine (Nardil), tranylcypromine (Parnate), and selegiline (Eldepryl, Emsam, Zelapar);
narcotics and other pain medication; sedatives; sleeping pills;and tranquilizers. Your doctor may
need to change the doses of your medications or monitor you carefully for side effects.
 tell your doctor if you have or have ever had an enlarged prostate (a male reproductive gland);
glaucoma (a condition in which increased pressure in the eye can lead to gradual loss of vision);
seizures; ulcers; blockage in the passage between the stomach and intestine; blockage in the
 bladder; asthma or other lung disease; sleep apnea; cancer;any condition that affects the
production of blood cells in your bone marrow; or heart or liver disease. If you will be giving
promethazine to a child, also tell the child's doctor if the child has any of the following symptoms
before he or she receives the medication: vomiting, listlessness, drowsiness, confusion,
aggression, seizures, yellowing of the skin or eyes, weakness, or flu-like symptoms. Also tell the
child's doctor if the child has not been drinking normally, has had excessive vomiting or diarrhea,
or appears dehydrated.
 tell your doctor if you are pregnant or plan to become pregnant. If you become pregnant while
taking promethazine, call your doctor. Do not breast-feed while you are taking promethazine.
 if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking
promethazine.
 you should know that this medication may make you drowsy. Do not drive a car or operate
machinery until you know how this medication affects you. If you are giving promethazine to a
child, watch the child to be sure he or she does not get hurt while riding a bike or participating in
other activities that could be dangerous.
 remember that alcohol can add to the drowsiness caused by this medication.
 plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing,
sunglasses, and sunscreen. Promethazine may make your skin sensitive to sunlight.

What special dietary instructions should I follow?

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Unless your doctor tells you otherwise, continue your normal diet.

What should I do if I forget a dose?

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Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip
the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a
missed one.

What side effects can this medication cause?

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Promethazine can cause side effects. Tell your doctor if any of these symptoms are severe or do not go
away:

 dry mouth
 drowsiness
 listlessness
 difficulty falling asleep or staying asleep
 nightmares
 dizziness
 ringing in ears
 blurred or double vision
 loss of coordination
  nausea
 vomiting
 nervousness
 restlessness
 hyperactivity
 abnormally happy mood
 stuffy nose
 itching

Some side effects can be serious. If you experience any of the following symptoms, call your doctor
immediately:

 wheezing
 slowed breathing
 breathing stops for a short time
 fever
 sweating
 stiff muscles
 decreased alertness
 fast or irregular pulse or heartbeat
 faintness
 abnormal or uncontrollable movements
 hallucinations (seeing things or hearing voices that do not exist)
 confusion
 overwhelming or unmanageable fear or emotion
 seizures
 uncontrollable shaking of a part of the body
 unusual bruising or bleeding
 sore throat, fever, chills, and other signs of infection
 uncontrolled eye movements
 tongue sticking out
 abnormal neck position
 inability to respond to people around you
 yellowing of the skin or eyes
 rash
 hives
 swelling of the face, eyes, lips, tongue, throat, arms, hands, feet, ankles, or lower legs
 hoarseness
 difficulty breathing or swallowing

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug
Administration's (FDA) MedWatch Adverse Event Reporting program online
[at http://www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088].
Promethazine may cause other side effects. Call your doctor if you experience any unusual problems
while you are taking this medication.

What storage conditions are needed for this medicine?

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Keep this medication in the carton or container it came in, tightly closed, and out of reach of children.
Store promethazine tablets and liquid at room temperature and away from excess heat and moisture (not
in the bathroom). Store promethazine suppositories in the refrigerator. Protect the medication from light.
Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the
proper disposal of your medication.

In case of emergency/overdose
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In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or
is not breathing, call local emergency services at 911.

Symptoms of overdose may include:

 difficulty breathing
 slowed or stopped breathing
 dizziness
 lightheadedness
 fainting
 loss of consciousness
 fast heartbeat
 tight muscles that are difficult to move
 loss of coordination
 continuous twisting movements of the hands and feet
 dry mouth
 wide pupils (black circles in the middle of the eyes)
 flushing
 nausea
 constipation
 abnormal excitement or agitation
 nightmares

What other information should I know?

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Keep all appointments with your doctor.

Promethazine can interfere with the results of home pregnancy tests. Talk to your doctor if you think you
might be pregnant while you are taking promethazine. Do not try to test for pregnancy at home.
Before having any laboratory test, tell your doctor and the laboratory personnel that you are taking
promethazine.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling
your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter)
medicines you are taking, as well as any products such as vitamins, minerals, or other dietary
supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a
hospital. It is also important information to carry with you in case of emergencies.

Brand names
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 Pentazine®
 Phenadoz®

 Phenergan®
 Promacot®

 Promethegan®

Brand names of combination products

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 Mepergan® Fortis (containing Meperidine, Promethazine)

 Meprozine® (containing Meperidine, Promethazine)
 Pentazine® VC (containing Codeine, Phenylephrine, Promethazine)
 Pentazine® with Codeine (containing Codeine, Promethazine)
 Phen-Tuss® AD (containing Phenylephrine, Promethazine)
 Phen-Tuss® DM (containing Dextromethorphan, Promethazine)
 Phenameth® VC (containing Phenylephrine, Promethazine)

 Phenergan® VC (containing Phenylephrine, Promethazine)

 Phenergan® VC with Codeine (containing Codeine, Phenylephrine, Promethazine)
 Phenergan® with Codeine (containing Codeine, Promethazine)
 Phenergan® with Dextromethorphan (containing Dextromethorphan, Promethazine)
 Prometh VC (containing Phenylephrine, Promethazine)
 Prometh with Codeine (containing Codeine, Guaifenesin, Promethazine)
 Promethazine VC (containing Phenylephrine, Promethazine)

Last Revised - 10/01/2010