Fentanyl (CAS Number: 437-38-7)

Clinical Use of Fentanyl

               Fentanyl (Sublimaze) and its related phenylpiperidine derivatives are extremely potent drugs.They are used as adjuncts to anesthesia, and fentanyl may be given transdermally as an analgesic and as an oral lozenge for the induction of anesthesia, especially in children who may become anxious if given IV anesthesia.
Fentanyl is 80 to 100 times as potent as morphine. Sufentanil (Sufenta) is 500- to 1,000-fold more potent than morphine, while alfentanil (Alfenta) is approximately 20 times more potent than morphine. Their onset of action is usually less than 20 minutes after administration. Dosage is determined by the lean body mass of the patient, since the drugs are lipophilic and tend to get trapped in body fat, which acts as a reservoir, prolonging their half-life. In addition, redistribution of the drugs from the brain to fat stores leads to a rapid offset of action. Droperidol, a neuroleptic agent, is generally administered in combination with fentanyl for IV anesthesia.
             Fentanyl transdermal patches are available for analgesia in chronic pain and for postsurgical patients. The use of the patch is contraindicated, however, for patients immediately after surgery because of the profound respiratory depression associated with its use. The patches must be removed and replaced every 3 days. The onset of action of transdermal fentanyl is slower than that of oral morphine. Thus, patients may require the use of oral analgesics until therapeutic levels of fentanyl are achieved. Fentanyl lozenges have been used to induce anesthesia in children and to reduce pain associated with diagnostic tests or cancer in adult patients. However, all of the adverse side effects associated with morphine are produced with far greater intensity, but shorter duration, by fentanyl in the patch, the lozenge, or IV administration. Given the abuse liability of fentanyl, controversy exists as to the ethics of marketing a lollipop lozenge form.
Sufentanil is much more potent than fentanyl and is indicated specifically for long neurosurgical procedures. In such patients, sufentanil maintains anesthesia over a long period when myocardial and cerebral oxygen balance are critical.


Side effects

         In addition to all of the adverse effects and contraindications previously described for morphine, the following contraindications apply specifically to these drugs. They are contraindicated in pregnant women because of their potential teratogenic effects. They also can cause respiratory depression in the mother, which reduces oxygenation of fetal blood, and in the newborn; the incidence of sudden infant death syndrome (SIDS) in the newborn is also increased.
Cardiac patients need to be monitored closely when receiving these drugs because of their bradycardiac effects (which can lead to ectopic arrhythmias), and hypotensive effects resulting from prolonged vasodilation. In addition, the drugs stiffen the chest wall musculature, an effect reversed by naloxone.

Manufacturing Process

       To the stirred solution of 5 parts of N-(4-piperidyl)propionanilide, 6.85 parts sodium carbonate, 0.05 part potassium iodide in 120 parts hexone is added portionwise a solution of 3.8 parts β-phenylethyl chloride in 24 parts 4- methyl-2-pentanone. The mixture is stirred and refluxed for 27 hours. The reaction mixture is filtered while hot, and the filtrate is evaporated. The oily residue is dissolved in 160 parts diisopropyl ether and the solution is filtered several times until clear, then concentrated to a volume of about 70 parts. The residue is then cooled for about 2 hours at temperatures near 0°C to yield N- [1-(β-phenylethyl)-4-piperidyl]propionanilide, melting at about 83° to 84°C as described in US Patent 3,141,823.
The starting material is prepared by reacting 1-benzyl-4-piperidone with aniline, reducing the condensation product with lithium aluminum hydride, reacting the product thus obtained with propionic anhydride, then hydrogen.


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What is FENTANYL (CAS NUMBER: 437-38-7)

Fentanyl binds to the body’s opioid receptors, increasing dopamine levels in the central nervous system.

The increase in dopamine produces a state of relaxation, relieves pain, decreases the perception of suffering, and promotes a feeling of well-being (euphoria).

A schedule 2 prescription narcotic analgesic, fentanyl is roughly 100 times more potentTrusted Source than morphine.

It is used to manage pain during surgery; it is also used to treat moderate-to-severe chronic pain syndromes in people who are already physically tolerant to opiates.

Fentanyl depresses the respiratory centers and the cough reflex and constricts the pupils. It can work within minutes to relieve pain and produce sedation. Fentanyl has a short duration of effect – just 30-90 minutes.

Fentanyl affects everyone differently. The effects are dependent on an individual’s size, weight, overall state of health, the amount that is taken, whether fentanyl is taken in combination with other drugs, and whether the person is used to taking opioids.

Medically prescribed fentanyl is available in a variety of formulations, including lozenges, lollipops, oral and nasal sprays, and injections.

Fentanyl patch

For continuous delivery, fentanyl can be administered through a transdermal patch that adheres to the skin. The patch works by slowly releasing fentanyl through the skin into the bloodstream over 48-72 hours.

A fentanyl patch is only used in patients who are already tolerant to opioid therapy of a similar strength. Because it has already been absorbed through the skin, fentanyl can continue to be effective for 13-24 hours after the patch is removed.

fentanyl has many other name people called it on the street some of this names are 



important things you need to know about  fentanyl

1 The difference between a therapeutic dose and a deadly dose of fentanyl is very small.

2 Here are some key points about fentanyl. More detail and supporting information is in the main article.

3 Oral formulations of fentanyl contain an amount of the drug that can be fatal to a child.

4 Fentanyl is a potent synthetic opioid that is very effective at relieving moderate-to-severe chronic pain.

5 There are many illegal analogs and derivatives of fentanyl that are much stronger than the prescription version.