Fentanyl = A Tutorial Snipet

[Guest guest]

Dear All,

I researched fentanyl patches and injection on the internet. I also

used Fax and Comparison and RxList.com.

I have compiled and organized several main ideas from four main sites

and have paraphrased and re-written some areas into the following

article:

Therapeutic Use: Fentanyl is a potent synthetic (man-made) narcotic

and was first synthesized in Belgium in 1950's. Its chemical name

is N-(1-phenethyl-4-piperidyl)-N-phenyl-propanamide. It has an

analgesic potency of about 80 times that of morphine, Transdermal

systems labeled as delivering 50, 75, or 100 µg/hour (mcg/hr). A 100

µg (mcg ) dose of fentanyl is approximately equal to 10 mg of

morphine. It works to increase the threshold to pain and reduce the

perception of pain.

Sublimaze. is trade name for fentanyl marketed in 1968. Duragesic is

a trade name for the fentanyl patch. Fentanyl patches were

introduced in the mid 1990's with a flavored-lollipop of fentanyl

citrate mixed with inert fillers on a stick was introduced under the

trade name of Actiq, which became the first quick-acting formation of

fentanyl for use with breakthrough chronic pain. Most currently an

effervescent tab for buccal absorption and a buccal spray device for

fast-acting relief have been developed with other delivery methods

currently in development.

Part of the Black Box Warning is:

" DURAGESIC® should ONLY be used in patients who are already receiving

opioid therapy, who have demonstrated opioid tolerance, and who

require a total daily dose at least equivalent to DURAGESIC® 25

mcg/h. Patients who are considered opioid-tolerant are those who have

been taking, for a week or longer, at least 60 mg of morphine daily,

or at least 30 mg of oral oxycodone daily, or at least 8 mg of oral

hydromorphone daily or an equianalgesic dose of another opioid. "

" THE APPLICATION OF HEAT TO A FENTANYL PATCH CAN LEAD

TO SUDDEN DELIVERY OF A LARGE AMOUNT OF FENTANYL.

Human deaths have been reported in patients

with patches sleeping on heated water beds.

If your pet has a fentanyl patch, be sure to avoid situations

where the patch could be excessively heated. "

Some of the therapeutic effects of opiates are:

pain

relief

drowsiness

euphoria

addictiveness

diarrhea control

respiratory depression

hallucinations

Mechanism of Action:

Opiate drugs bind to different types of opiate receptors throughout

the nervous system. The different types of opiate receptors are

responsible for creating different narcotic effects. The " mu "

receptor is responsible for the narcotic effects of euphoria,

addiction, and respiratory depression. (there are also " kappa "

and " sigma " receptors with other effects) The strength of different

opiate drugs are generally compared to those of one of the oldest of

the opiates: morphine sulfate. Fentanyl binds only the mu receptor

and does so approximately 75 to 100 times stronger than morphine.

Veterinarian use:

It reaches its peak blood level in 3 to 6 hours in cats but may

require a full 12 hours in dogs to reach its full effect. After

removal, fentanyl blood levels drop to zero within 24 hours. Patches

last at least 4 days in pets.

Side Effects: The most serious potential side effect is respiratory

depression.

Occasionally, a pet or person may react to the adhesive on the

transdermal patch. Removal of the patch should resolve the situation

and the application of a topical cortisone product may also be

indicated.

Illicit Use: " China White " is the name for the illegally made and

illicit drug. which is the fentanyl analogue alpha -methylfentanyl

(AMF). In 2006 , the lethal combination known as ' the bomb'

or 'magic' surfaced in many urban areas of US which is an ilegal or

illicitly-produced combo of fentanyl Plus cocaine or fentanyl and

heroine. " To date, over 12 different analogues of fentanyl have been

produced clandestinely and identified in the U.S. drug traffic. The

biological effects of the fentanyls are indistinguishable from those

of heroin, with the exception that the fentanyls may be hundreds of

times more potent. Fentanyls are most commonly used by intravenous

administration, but like heroin, they may also be smoked or snorted. "

" Diversion and theft from pharmacies, hospitals and nursing homes of

fentanyl oral transmucosal lozenges (Actiq®) are typically sold at

$20-25 per unit or $450 per carton (contains 24 units) while

transdermal patches (Duragesic®) are sold at prices ranging from $10

to $100 per patch depending upon the dose of the unit and

geographical area. "

If you wish to read all articles in full that I got the information

from you may go to:

http://www.medicinenet.com/fentanyl_transdermal_system/article.htm

http://cdb.ics.uci.edu/CHEMDB/Web/cgibin/ChemicalDetailWeb.py?

chemical_id=3966642

http://www.streetdrugs.org/fentanyl.htm

http://www.marvistavet.com/html/body_fentanyl.html

I hope this proves interesting and serves as a tutorial to the

newbies. Feel free to add any factual information.

Respectfully,

Jeanetta Mastron CPhT BS

Pharm Tech Edudator