Oral Transmucosal Fentanyl Citrate OTFC Stick for Treatment of Breakthrough Pain

The problem of breakthrough pain, lasting for 30 min to 2 h is often observed in patients with cancer pain (Fig. IV-16), which may present a major problem in chronic pain therapy. Breakthrough pain may appear at different instances such as

• Weight bearing/movement

• Walking/sitting

Over Medication

Anouud-liie-Clock Thcrapcutic

(ATC) Medication Window

Ftfa

Relief

Threshold

Ftfa

Relief

Threshold lime

Nociceptive Afferents
Figure IV-16. Schematic representation of breakthrough pain during around-the-clock medication where in spite of a stable and constant plasma blood level, peak nociceptive afferents break through the opioid barrier

• Defecation/urination

• Coughing/breathing

• Spontaneously, or

Breakthrough pain is characterised by the following features. They present a

• Moderate to severe intensity

• Relatively short duration, and have a

• Frequency of 1-4 episodes per day

With a prevalence of 50%-89% the pathology usually is identical to persistent pain (Table IV-9):

Until recently it was advocated to alleviate breakthrough pain by the simultaneous oral intake of a fast acting morphine preparation. Presently, the oral transmucosal fentanyl citrate (OTFC) stick is available, where the active compound, due to its high lipophylicity is rapidly absorbed via the mucous membranes of the oral cavity.

The new galenic preparation of the potent opioid fentanyl is available as oral transmucosal fentanyl citrate (OTFC), also termed "the fentanyl lollypop". It enables rapid and sufficient high absorption through the mucous membrane with sufficient plasma levels within 5 min. Because of the high lipophilicity of fentanyl the opioid is rapidly absorbed through mucous membranes of the oral cavity thus bypassing reabsorption in the intestinal gut, avoiding the degradation through the first liver passage. The fentanyl lollypop (Actiq™, Cephalon company, Pennsylvania/USA) is available in six different concentrations (200, 400, 600, 800, 1200 and 1600 ^g), which enables the patients to use the appropriate dose for treatment individual breakthrough pain intensity (Fig. IV-17). Because of the fast onset of action with a maximum of 5 min and a duration of 30 min to 2 h [31] (depending on the concentration being used), the patients starts with the lowest concentration and then increases the dose if breakthrough pain is not sufficiently relieved (Fig. IV-18). Compared to oral morphine sulfate instant release (MSIR), oral transmucosal fentanyl citrate results in a faster relief of pain, similar side effects

Table IV-9. Pathophysiology of breakthrough pain

Classification

Tissue damaged

Descriptors

Typical treatment

Somatic, nociceptive

General body tissues

Aching Throbbing

Opioids

pain

Stabbing

Visceral, nociceptive

Organs

Deep Dull Aching

Opioids

pain

Neuropathic pain

Nervous system

Burning Tingling

Adjuvant analgesics

Lancinating

Adapted from [29, 30]

Properties of mucuous membranes

Sublingual/transmucosal technology

Large surface area

Uniform temperature

High permeability

Very well vascularized

Rapid absorption

Sufficient high amounts

No resistance to highly lipophilic compounds

Very well vascularized

Sufficient high amounts

No resistance to highly lipophilic compounds

Organs Absorption Opioid

Figure IV-17. Summary of the potential advantages of the mucosal application of opioids, the oral transmucosal fentanyl citrate (OTFC) or sublingual buprenorphine for rapid relief of breakthrough pain

(sedation, nausea, constipation, disorientation) but a longer lasting and significantly better relief of breakthrough pain. Overall acceptance by patients is highly significant when compared to the usual oral morphine sulfate immediate release (MSIR) preparation [32].

While for the sake of practical use oral transmucosal fentanyl citrate is the appropriate compound when the transdermal fentanyl patch is used as this results in a 50% total bioavailability (Fig. IV-19). Also there is an equivalent when the buprenorphine patch is the preferred preparation for the long-term use of chronic

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