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Promethazine

 
Drug Info: Promethazine
 

Brand names: Anergan™Antinaus®Pentazine®Phenadoz™Phenergan®Phenergan® FortisProgan™Prometh®Promethegan®

Chemical formula:



Promethazine Hydrochloride Rectal suppository

What is this medicine?

PROMETHAZINE is an antihistamine. It is used to treat allergic reactions and to treat or prevent nausea and vomiting from illness or motion sickness. It is also used to make you sleep before surgery, and to help treat pain or nausea after surgery.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•glaucoma
•high blood pressure or heart disease
•kidney disease
•liver disease
•lung or breathing disease, like asthma
•prostate trouble
•pain or difficulty passing urine
•seizures
•an unusual or allergic reaction to promethazine or phenothiazines, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

This medicine is for rectal use only. Do not take by mouth. Wash your hands before and after use. Take off the foil wrapping. Wet the tip of the suppository with cold tap water to make it easier to use. Lie on your side with your lower leg straightened out and your upper leg bent forward toward your stomach. Lift upper buttock to expose the rectal area. Apply gentle pressure to insert the suppository completely into the rectum, pointed end first. Hold buttocks together for a few seconds. Remain lying down for about 15 minutes to avoid having the suppository come out. Do not use more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed. This medicine should not be given to infants and children younger than 2 years old.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•medicines called MAO Inhibitors like Nardil, Parnate, Marplan, Eldepryl
•other phenothiazines like trimethobenzamide

This medicine may also interact with the following medications:
•barbiturates such as phenobarbital
•bromocriptine
•certain antidepressants
•certain antihistamines used in allergy or cold medicines
•epinephrine
•levodopa
•medicines for sleep
•medicines for mental problems and psychotic disturbances
•medicines for movement abnormalities as in Parkinson's disease, or for gastrointestinal problems
•muscle relaxants
•prescription pain medicines

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Tell your doctor or health care professional if your symptoms do not start to get better in 1 to 2 days.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. To reduce the risk of dizzy or fainting spells, do not stand or sit up quickly, especially if you are an older patient. Alcohol may increase dizziness and drowsiness. Avoid alcoholic drinks.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.

This medicine may cause dry eyes and blurred vision. If you wear contact lenses you may feel some discomfort. Lubricating drops may help. See your eye doctor if the problem does not go away or is severe.

This medicine can make you more sensitive to the sun. Keep out of the sun. If you cannot avoid being in the sun, wear protective clothing and use sunscreen. Do not use sun lamps or tanning beds/booths.

If you are diabetic, check your blood-sugar levels regularly.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•blurred vision
•irregular heartbeat, palpitations or chest pain
•muscle or facial twitches
•pain or difficulty passing urine
•seizures
•skin rash
•slowed or shallow breathing
•unusual bleeding or bruising
•yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•headache
•nightmares, agitation, nervousness, excitability, not able to sleep (these are more likely in children)
•stuffy nose

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store in a refrigerator between 2 and 8 degrees C (36 and 46 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Veterinary Dictionary: promethazine
 

A phenothiazine derivative used as an antihistaminic, antiemetic and tranquilizer in the form of the hydrochloride salt.

 
WordNet: promethazine
Top
Note: click on a word meaning below to see its connections and related words.

The noun has one meaning:

Meaning #1: antihistamine (trade name Phenergan) used to treat allergies; also an antiemetic used to treat motion sickness
  Synonym: Phenergan


 
Wikipedia: Promethazine
Top
Promethazine
Systematic (IUPAC) name
(RS)-N,N-dimethyl-1-(10H-phenothiazin-10-yl)propan-2-amine
Identifiers
CAS number 60-87-7
58-33-3 (hydrochloride)
ATC code D04AA10 R06AD02, R06AD05
PubChem 4927
DrugBank APRD00601
ChemSpider 4758
Chemical data
Formula C17H20N2S 
Mol. mass 284.42 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 88% absorbed but after first-pass metabolism reduced to 25% absolute bioavailability
Protein binding 93%
Metabolism Hepatic glucuronidation and sulfoxidation
Half life 16-19 hours
Excretion Renal and biliary
Therapeutic considerations
Pregnancy cat.

C(AU) C(US)

Legal status

P(UK) -only(US)
(injection POM(UK))

Routes Oral, rectal, IV, IM, topical

Promethazine is a first-generation H1 receptor antagonist, antihistamine and antiemetic medication. It can also have strong sedative effects and in some countries is prescribed for insomnia when benzodiazepines are contraindicated. It is a prescription drug in the United States but is available over the counter in the United Kingdom, Canada, Switzerland, Australia, and many other countries (brand names Phenergan, Promethegan, Romergan, Fargan, Farganesse, Prothiazine, Avomine, Atosil, Receptozine, Lergigan).[1]

Chemically, promethazine hydrochloride (HCl) appears as a white to faint yellow crystaline 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]

Contents

Indications

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 (blocker).[6]
  • It has sedative, anti-motion-sickness, anti-emetic, and anti-cholinergic effects

Side effects

Some common side effects include:

  • Confusion in the elderly
  • Drowsiness, dizziness, fatigue, more rarely vertigo
  • Dry mouth
  • Seizures (extremely rare)
  • Neuroleptic malignant syndrome (extremely rare)
  • Respiratory depression in patients under age of 2 and in those with severely compromised pulmonal function
  • Constipation
  • Euphoria (very rare with high IV doses and/or coadministration with opioids/CNS depressants)
  • Restless legs [7]
  • Paresthesia

It is recommended that promethazine only be given through an existing intravenous set in a large vein and diluted to concentration no greater than 25mg per mL, not to exceed a rate of administration of 25mg a min. Serious complications including those listed above have resulted from improper parenteral administration, including those requiring surgical intervention and amputation.[8]

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.

Case law

The U.S. Supreme Court accepted a case involving promethazine that influences product liability. 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 arm 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 pre-emption 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 meant that drug manufacturers could be held liable for injuries, even if they had already warned the patients of potential adverse affects.

References

  1. ^ RxList: Promethazine
  2. ^ http://www.rxlist.com/cgi/generic/phenergan.htm RxList: Promethazine Description
  3. ^ a b c d e RxList Indications for Promethazine
  4. ^ British National Formulary (March 2003). "4.6 Drugs used in nausea and Vertigo - Vomiting of pregnancy". "BNF" (45 ed.). 
  5. ^ [1]
  6. ^ David J. McCann and Brett Roth, Toxicity, Antihistamine, eMedicine Toxicology, updated June 21, 2007
  7. ^ Cordingley Neurology
  8. ^ Baxter: Promethazine HCl Injection, USP Information
  9. ^ Liptak, Adam (2008-09-18). "Drug Label, Maimed Patient and Crucial Test for Justices". The New York Times. http://www.nytimes.com/2008/09/19/us/19scotus.html?n=Top/Reference/Times%20Topics/Organizations/S/Supreme%20Court&_r=1&adxnnl=1&oref=slogin&adxnnlx=1225505895-T2aivHeTdvJTT7b+uEsK1Q. Retrieved on 2008-10-31. 
  10. ^ Stout, David (2009-03-04). "Drug Approval Is Not a Shield From Lawsuits, Justices Rule". The New York Times. http://www.nytimes.com/2009/03/05/washington/05scotus.html. Retrieved on 2009-03-04. 

External links


 
 

 

Copyrights:

Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
WordNet. WordNet 1.7.1 Copyright © 2001 by Princeton University. All rights reserved.  Read more
Wikipedia. This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Promethazine" Read more