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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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Ketamine Hydrochloride and Fentanyl Citrate Injection
From International Journal of Pharmaceutical Compounding, 11/1/04

METHOD OF PREPARATION

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

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

2. Accurately weigh and/or measure each ingredient.

3. Aseptically, obtain the required quantity of ketamine and fentanyl and mix well in a suitable sterile container.

4. Aseptically, add sufficient 0.9% sodium chloride injection to volume and mix well.

5. Package and label.

PACKAGING

Package in tight, light-resistant containers.1

LABELING

Keep out of reach of children. Use only as directed.

STABILITY

If no sterility testing is done, a beyond-use date of 24 hours at room temperature, 3 days at refrigerated temperature or 45 days at

USE

Ketamine and fentanyl in combination are used in the treatment of moderate-to-severe pain.

QUALITY CONTROL

Quality-control assessment can include weight/volume, physical observation, pH, specific gravity, osmolality, assay, color, clarity, particulate matter, sterility and pyrogenicity.3,4

DISCUSSION

Ketamine hydrochloride injection is available in concentrations equivalent to 10, 50 or 100 mg/mL of ketamine base. The pH of the injection is from 3.5 to 5.5. The injection also contains 0.1 mg/mL of benzethonium chloride, and the 10 mg/mL concentration is rendered isotonic with sodium chloride.

Ketamine hydrochloride (C^sub 13^H^sub 16^ClNO.HCl, MW 274.2) is used as an anesthetic and analgesic. It occurs as a white crystalline powder with a slight characteristic odor. Approximately 1.15 mg is equivalent to 1 mg of ketamine base. It is soluble 1 g in 4 mL of water, 14 mL of alcohol and 60 mL of absolute alcohol. Ketamine hydrochloride injection is a sterile solution of ketamine hydrochloride in water for injection. It contains an amount of ketamine hydrochloride equivalent to not less than 95.0% and not more than 105.0% of the labeled amount of ketamine. The injection has a pH of 3.5-5.5, and it contains not more than 0.4 USP endotoxin units per mg of ketamine hydrochloride. It should be stored at controlled room temperature and protected from light.1,5

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 crystalline powder. Fentanyl citrate injection contains fentanyl, as the citrate 50 µg per mL with hydrochloric acid and/or sodium hydroxide to adjust pH to the range of 4 to 7.5. Fentanyl citrate 157 µg is approximately equal to 100 µg of fentanyl. It is soluble 1 g in 40 mL of water and slightly soluble in alcohol. The pH of the fentanyl injection is in the range of pH 4.0 to 7.5. Fentanyl citrate is a synthetic opioid analgesic used as a sedative, analgesic, preoperative medication and an adjunct to general or regional anesthesia and in the management of chronic pain.6

0.9% Sodium chloride injection contains not less than 95.0% and not more than 105.0% of the labeled amount of sodium chloride in water for injection. It has a pH between 4.5 and 7.0 and contains no added antimicrobial agents. They can be sterilized by filtration or autoclaving. Sodium chloride will decrease the solubility of some organic compounds; methylparaben is not as soluble in sodium chloride solutions as it is in water. Sodium chloride is soluble in water to the extent of 1 g in 2.8 mL water, and is slightly soluble in alcohol (1 g in 250 mL of 95% ethanol).1

REFERENCES

1. US Pharmacopeial Convention, Inc. United States Pharmacopeia 27-National Formulary 22. Rockville, MD: US Pharmacopeial Convention, Inc.; 2004: 1054-1056, 1700, 2345-2349, 2768.

2. Ambados F, Brealey J. Compatibility of ketamine hydrochloride and fentanyl citrate in polypropylene syringes. Am J Health Syst Pharm 2004; 61: 1438-1439.

3. Allen LV Jr. Standard operating procedure for particulate testing for sterile products. IJPC 1998; 2: 78.

4. Allen LV Jr. Standard operating procedure: Quality assessment for injectable solutions. IJPC 1999; 3: 406-407.

5. Sweetman SC, ed. MARTINDALE: The Complete Drug Reference. 33rd ed. London: Pharmaceutical Press; 2002: 1262-1263.

6. Reynolds JEF, ed. MARTINDALE: The Extra Pharmacopoeia. 30th ed. London: Pharmaceutical Press; 1993: 1076-1077.

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