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Fentanyl

Fentanyl is an opioid analgesic, first synthesized in Belgium in the late 1950s, with an analgesic potency of about 80 times that of morphine. It was introduced into medical practice in the 1960s as an intravenous anesthetic under the trade name of Sublimaze. Fentanyl has an LD₅₀ of 3.1 milligrams per kilogram in rats. The LD₅₀ in humans is not known. Fentanyl is a Schedule II drug. more...

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Analogues

The pharmaceutical industry has developed several analogues of fentanyl:

Alfentanil (Alfenta), an ultra-short acting (5–10 minutes) analgesic,
Sufentanil (Sufenta), a potent analgesic (15 to 10 times more potent than fentanyl) for use in heart surgery.
Remifentanil, currently the shortest acting opioid, has the benefit of rapid offset, even after prolonged infusions.
Carfentanil (Wildnil) is an analogue of fentanyl with an analgesic potency 10,000 times that of morphine and is used in veterinary practice to immobilize certain large animals.

Therapeutic use

Today, fentanyls are extensively used for anesthesia and analgesia. Duragesic, by Janssen Pharmaceutica, is a fentanyl transdermal patch used in chronic pain management. In the past few years, this compound has gone generic and is available for lower cost. Duragesic is manufactured in five patch sizes. They are 12.5 mcg/hr, 25 µg/h, 50 µg/h, 75 µg/h, and 100 µg/h. Dosage is based on the size of the patch, since the transdermal absorption rate is generally constant at skin temperature.

Actiq, by Cephalon, is a recently-developed solid formulation of fentanyl citrate on a stick that dissolves slowly in the mouth for transmucosal absorption. Actiq is intended for opiate-tolerant individuals and is effective in treating breakthrough cancer pain. It is also useful for breakthrough pain for those suffering bone injuries, severe back pain, neuropathy, arthritis, and some other examples of chronic nonmalignant pain. The unit is a berry-flavored lozenge on a stick which is swabbed on the mucosal surfaces inside the mouth - under and on the tongue and gums—to release the fentanyl quickly into the system. It is most effective when the lozenge is consumed in 15 minutes. The drug is practically ineffective if swallowed, absorption from the alimentary tract being negligible. Actiq is available in 6 dosages, from 200 µg to 1,600 µg (There are no 1,000 µg or 1,400 µg doses)in 200 µg increments.

Fentanyl is frequently given intrathecally as part of spinal anesthesia or epidurally for epidural anesthesia and analgesia.

Illicit use

Illicit use of pharmaceutical fentanyls first appeared in the mid-1970s in the medical community and continues to be a problem in the United States. United States authorities classify fentanyl as a narcotic. 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. Also, fentanyl has a shorter duration than heroin does. Fentanyls are most commonly used by intravenous administration, but like heroin, they may also be smoked or snorted. One common street name for fentanyl is china white. This is not always accurate, as it was originally given to alpha-methyl-fentanyl, although in recent years this terminology has faded somewhat. AMF has longer metabolism than fentanyl because the methyl group retards metabolism.

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Fentanyl 15-mg/mL Injection, Preservative Free
From International Journal of Pharmaceutical Compounding, 1/1/05

METHOD OF PREPARATION

Note: This preparation should he prepared in a laminar airflow hood in a cleanroom or via isolation barrier technology by a validated aseptic compounding pharmacist using strict aseptic technique. This is a high-risk preparation.

1. Calculate the required quantity of each ingredient for the total amount to be prepared.

2. Accurately weigh and/or measure each ingredient.

3. Dissolve the fentanyl citrate and sodium chloride in about 95 mL of sterile water for injection.

4. Adjust the pH, if necessary, to the pIT range 4.0 to 7.5.

5. Add sufficient sterile water for injection to volume and mix well.

6. Filter through a sterile 0.220 -µm lilter into a pump cassette or other appropriate container.

7. Package and label.

PACKAGING

Package in tight, light-resistant containers.1

LABELING

Keep out of reach of children. Use only as directed. Store in a refrigerator.

STABILITY

If sterility tested: A beyond-use date of up to 24 hours at room temperature, up to 3 days at refrigerated temperature (2 to 8°C), or up to 45 days if frozen can be used for this preparation.'

If not sterility tested: A bcyond-use date of up to 14 days stored in a refrigerator can be used for this preparation.1

USE

Fentanyl citrate injection is used in the treatment of chronic, severe pain.

QUALITY CONTROL

Quality-control assessment can include weight/volume, physical observation, pH, specific gravity, osmolaliry, assay, color, clarity, paniculate matter, sterility and pyrogcnicity.2,3

DISCUSSION

Fentanyl is a synthetic phenylpiperidine-derivative opiate agonist used as a sedative, analgesic, preoperative medication, and adjunct to general or regional anesthesia and in the management of chronic pain. Fentanyl is commercially available in a number of dosage forms, including a 50-µg/mL injection. Higher concentrations are required, however, in pumps for chronic administration.

Fentanyl citrate (C^sub 22^H^sub 28^N^sub 2^O.C^sub 6^H^sub 8^O^sub 7^, MW 528.6) occurs as white granules or as a white, glistening, crystalline powder. It melts at about 150°C, with decomposition. Fcntanyl citrate 157 µg is approximately equal to 100 µg of fentanyl. Tt is soluble l g in 40 mL of water and slightly soluble in alcohol. Fentanyl Citrate Injection USP contains not less than 90.0% and not more than 110.0% of the labeled amount of fentanyl, present as the citrate. It should be protected from light. The pH of the injection is between 4.0 and 7.S.1,4

Sodium chloride (NaCl, MW 58.44) is available as a white crystalline powder or as colorless crystals. It has a saline taste and is used in a variety of parenteral and nonparenteral pharmaceutical formulations.5

Sodium hydroxide (NaOH, MW 40.00, caustic soda, soda lye) occurs as dry, very deliquescent, white or almost white sticks, pellets or fused masses that are hard and brittle. It is strongly alkaline and corrosive and rapidly absorbs moisture and carbon dioxide when it is exposed to air. It is soluble l g in 1 mL of water and is freely soluble in alcohol. A 0.01% solution in water has a pH of not less than 11.0. It should be stored in airtight, nonmetallic containers.4

Citric acid (C^sub 6^H^sub 8^O^sub 7^,H^sub 2^O, MW210.24, citric acid monohydrate) occurs as colorless or translucent crystals, or as a white crystalline, efflorescent powder that is odorless and has a strong, tart, acidic taste. Its melting point is about 100°C, but it softens at about 75°C. One gram is soluble in less than 1 mL of water and 1.5 mL of cthanol.6

Sterile water for injection is water for injection that has been sterilized and suitably packaged; it contains no added substance.'

REFERENCES

1. United States Pharmacopeial Convention, Inc. United States Pharmacopeia 27-NationalFormulary22. Rockville, MD: US Pharmacopeial Convention, Inc.; 2004: 785-786,1950,2345-2349,2762.

2. Alien LV Jr. Standard operating procedure for paniculate testing for sterile products. /JPC1998;2(1):78.

3. Alien LVJr. Standard operating procedure: Quality assessment for injectable solutions. /JPC1999; 3(5): 406-407.

4. Reynolds JE, ed. MARTINDALE: The Extra Pharmacopeia. 30th ed. London: The Pharmaceutical Press; 1993:1076-1077,1415.

5. Owen SC. Sodium chloride. In: Rowe RC, Sheskey PJ1 Weller PJ, eds. Handbook of Pharmaceutical Excipients. 4th ed. Washington, DC: American Pharmaceutical Association; 2003: 556-559.

6. Amidon GE. Citric acid monohydrate. In: Rowe RC, Sheskey PJ, Weller PJ, eds. Handbook of Pharmaceutical Excipients. 4th ed. Washington, DC: American Pharmaceutical Association; 2003: 158-160.

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