Intranasal Fentanyl for Breakthrough Pain Control

2012 ◽  
Vol 4 ◽  
pp. CMT.S7298 ◽  
Author(s):  
Claudia F. Clavijo ◽  
Rachael Rzasa Lynn ◽  
Uwe Christians ◽  
Jeffrey L. Galinkin
Keyword(s):  
Short Duration ◽  
Breakthrough Pain ◽  
Immediate Release ◽  
Rapid Onset ◽  
Time Profile ◽  
Economic Consequences ◽  
Onset Of Action ◽  
Oral Medications ◽  
Pharmacokinetic Properties ◽  
High Bioavailability

Breakthrough pain (BTP) is experienced by approximately 65% of children and adults with chronic pain. Undiagnosed or untreated BTP produces negative emotional, physical, and economic consequences. BTP episodes have a rapid onset and short duration. Short acting oral opioids are the cornerstone of BTP management. Oral medications available to treat BTP episodes like immediate-release morphine or oxycodone have a delayed onset of action so that there is a mismatch between the episode of BTP and the effect of the oral opioids. Novel fentanyl delivery systems for BTP offer pharmacokinetic properties that match the time profile of BTP. Among the transmucosal routes, intranasal fentanyl has gained popularity due to its high bioavailability, rapid onset of action, high potency, short duration, and ease of administration. Its efficacy and safety have been demonstrated in adults who are opioid tolerant. Although children with chronic cancer pain also experience BTP, there is paucity of data on the use of intranasal fentanyl for BTP in this age group.

A review of rapid-onset opioids for breakthrough pain in patients with cancer

2014 ◽  
Vol 10 (3) ◽  
pp. 207 ◽  
Author(s):  
Steven M. Simon, RPh, MD ◽  
Lee S. Schwartzberg, MD, FACP
Keyword(s):  
Breakthrough Pain ◽  
Immediate Release ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Abrupt Onset ◽  
Onset Of Action ◽  
Duration Of Action ◽  
Patients With Cancer ◽  
Duration Of Effect ◽  
Effective Pain Relief

Pain management in patients with cancer remains suboptimal. Breakthrough pain (BTP) is characterized by abrupt onset of severe pain in a background of otherwise stable managed pain and presents a substantial burden to patients, as it disrupts activities and quality of life. Rapid-onset opioids (ROOs), with an appropriate onset and duration of effect, provide new options for effective and well-tolerated management of BTP. All currently available ROOs are various formulations of transmucosal immediate-release fentanyl (TIRF) and, although they were originally developed and approved for use in children before painful procedures, are only approved for use in opioid-tolerant adult patients with cancer and BTP. The formulation options include oral lozenge, buccal tablet, buccal film, sublingual tablet, nasal spray, and a sublingual spray; each has practical considerations that vary with the product and route of administration. All have the common advantage of rapid entry into the systemic circulation via transmucosal absorption, avoiding hepatic and intestinal first-pass metabolism and allowing a rapid onset of action that rivals intravenous injections. Rapid onset and short duration of action allow good patient control of analgesia. The pharmacokinetic and analgesic properties of ROOs may allow reduction of the total opioid burden and associated adverse effects, while still providing effective pain relief. The shared TIRF risk evaluation and mitigation strategy program implemented in March 2012 has simplified enrollment and administration of these products to help mitigate the risks of abuse and misuse and to help ensure safe use in patients with cancer suffering from BTP.

scholarly journals Non-Traditional Administration of Remifentanil in an Experimental Setting

2019 ◽  
pp. S97-S103
Author(s):  
A. KURZOVÁ ◽  
J. MÁLEK ◽  
L. HESS ◽  
M. JAČEK ◽  
J. SLÍVA
Keyword(s):  
Arterial Oxygen Saturation ◽  
Pharmacokinetic Profile ◽  
Rapid Onset ◽  
Arterial Oxygen ◽  
Onset Of Action ◽  
Routes Of Administration ◽  
Arterial Blood ◽  
Pharmacokinetic Properties ◽  
Righting Reflex ◽  
Cardiovascular Functions

Remifentanil is ultrashort-acting opioid with a unique pharmacokinetic profile. It is used exclusively intravenously. While considering its rapid onset of action and other pharmacokinetic properties, we decided to assess its effects following administration via non-traditional routes. Rabbits (n=10 per each group) were randomized into six groups: remifentanil 1 μg/kg and 3 μg/kg IM, 5.0 and 10.0 μg/kg conjunctivally, and 10 μg/kg and 25.0 μg/kg intranasally. Sedating effects were assessed via a loss of the righting reflex. Secondary, mean arterial blood pressure, arterial oxygen saturation of hemoglobin, and pulse rate was monitored in all rabbits. Non-traditional routes of administration were shown to provide a rapid onset of action as well as fast recovery. Importantly, the administration of remifentanil did not result in any deterioration of cardiovascular functions.

Oral transmucosal fentanyl citrate for the treatment of breakthrough pain in cancer patients: An overview of its pharmacological and clinical characteristics

2005 ◽  
Vol 1 (1) ◽  
pp. 36 ◽  
Author(s):  
Kyriaki Mystakidou, MD, PhD ◽  
Emmanuela Katsouda, MD ◽  
Efi Parpa, BA, MA ◽  
Marinos L. Tsiatas, MD, PhD ◽  
Lambros Vlahos, MD, PhD
Keyword(s):  
Cancer Patients ◽  
Pain Treatment ◽  
Breakthrough Pain ◽  
Rapid Onset ◽  
Review Article ◽  
Brand Name ◽  
Fentanyl Citrate ◽  
Onset Of Action ◽  
Oral Transmucosal Fentanyl Citrate

Breakthrough pain is a transitory flare of pain occurring in most cancer patients against a background of otherwise controlled persistent pain. Treatment of breakthrough pain is a challenging phenomenon. Oral transmucosal fentanyl citrate (OTFC; brand name Actiqm, Cephalon Inc., West Chester, PA), a new opioid formulation with a unique delivery system, reflects the characteristics of breakthrough pain (rapid onset of action and short duration), making it an effective treatment for cancer patients who already receive opioids and experience flares of pain. This review article aims to present the role of oral transmucosal fentanyl citrate in the management of breakthrough pain in cancer patients. In particular, it is going to discuss the synthesis, clinical pharmacology, pharmacokinetic and pharmacodynamic properties, toxicity, and clinical efficacy of this novel agent.

scholarly journals Formulation and Quality Control of Orally Disintegrating Tablets (ODTs): Recent Advances and Perspectives

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Mohammadali Poursharifi Ghourichay ◽  
Seyed Hossein Kiaie ◽  
Ali Nokhodchi ◽  
Yousef Javadzadeh
Keyword(s):  
Quality Control ◽  
Immediate Release ◽  
Rapid Onset ◽  
Review Article ◽  
Oral Dosage ◽  
Onset Of Action ◽  
Current Review ◽  
Orally Disintegrating Tablets ◽  
Release Property ◽  
Preparation Techniques

Orally disintegrating tablets (ODTs) rapidly disintegrate or dissolve in the oral cavity without using water. Demand for ODTs has increased, and the field has overgrown in the pharmaceutical industry and academia. It is reported that ODTs have several advantages over other conventional tablets. Since some of them are absorbed from the mouth, pharynx, and esophagus as the saliva passes down into the stomach, in such cases, the bioavailability of the drug improves meaningfully. Furthermore, the immediate release property of ODTs makes them a popular oral dosage form in patients with swallowing challenges, children, and for cases with a need for rapid onset of action. The current review article explains the features of active ingredients and excipients used in the formulation of ODTs, discusses multiple ODT formulation and preparation techniques with their merits and demerits, and also, offers remedies for problems associated with ODTs. Moreover, quality control steps and required considerations are presented.

scholarly journals Formulation Development of Mouth Dissolving Film of Etoricoxib for Pain Management

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
K. Senthilkumar ◽  
C. Vijaya
Keyword(s):  
Pain Management ◽  
Immediate Release ◽  
Rapid Onset ◽  
Ease Of Use ◽  
Taste Masking ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Onset Of Action

Etoricoxib is a potent, orally active, and highly selective COX-2 inhibitor that exhibits anti-inflammatory, analgesic, and antipyretic activities. The present research was undertaken to develop mouth dissolving films of etoricoxib to have rapid onset of action. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use, and the consequent patient compliance. Solubility enhancement and taste masking of etoricoxib were the two challenges solved by formulating drug-inclusion complex with beta-cyclodextrin (BCD). MDF prepared by solvent casting etoricoxib-BCD complex along with HPMC as film forming polymer was found to possess desirable physicomechanical properties. In vitro release of etoricoxib from MDF in simulated salivary fluid and 0.1 N HCl was more than 95% within 2 minutes. Taste masking and in vivo disintegration were in acceptable range as assessed by human volunteers. Etoricoxib MDF was further characterized by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy. The index of analgesia shown by etoricoxib MDF was comparable to that of immediate release tablets (100% activity within 40 minutes) in animal studies. Conclusively, the present study documents the development of a commercially viable formula for an MDF of etoricoxib with rapidity in pain management.

Pharmacokinetic peculiarities of drugs used in the form of rapidly dispersible tablets (oral delivery system)

2020 ◽  
pp. 7-24
Author(s):  
Zhanna Kozlova ◽  
Ivan Krasnyuk ◽  
Yuliya Lebedeva ◽  
Ekaterina Odintsova
Keyword(s):  
Oral Mucosa ◽  
Oral Delivery ◽  
Chemical Properties ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Systemic Delivery ◽  
Onset Of Action ◽  
Mucosal Drug Delivery ◽  
Physical And Chemical ◽  
Pass Metabolism

Oral mucosal drug delivery is an alternative method of systemic delivery with several advantages over both injectable and enteral methods. Drugs that are absorbed through the oral mucosa directly enter the systemic circulation, passing through the gastrointestinal tract and first-pass metabolism in the liver due to oral mucosa being highly vascularised. This results in rapid onset of action for some drugs because of a more comfortable and convenient way of delivery than the intravenous one. But not all drugs can be administered through the oral mucosa due to characteristics of the oral mucosa and physical and chemical properties of the drug.

A Review on Enteric Coated Pellets Composed of Core Pellets Prepared by Extrusion-Spheronization

2019 ◽  
Vol 13 (2) ◽  
pp. 83-90 ◽  
Author(s):  
Hetal Patel ◽  
Mukesh Gohel
Keyword(s):  
Dosage Form ◽  
Extended Release ◽  
Rapid Onset ◽  
Enteric Coating ◽  
Onset Of Action ◽  
The Core ◽  
Current State ◽  
Enteric Coated ◽  
Extrusion Spheronization ◽  
Acid Labile

Enteric coated dosage form bypasses the stomach and releases the drug into the small intestine. Advantages of enteric coated pellets in comparison with enteric coated tablets are a) Pellets provide rapid onset of action and faster drug release due to the smaller size than tablets and b) Pellets exhibit less residence time of acid-labile drugs in the stomach compared to tablets. Dosage form coat can be damaged by longer resistance time in the stomach. The present review summarizes the current state of enteric coated pellets where core pellets are prepared by extrusion-spheronization technique and the enteric coating is applied in a fluidized bed processor. Two approaches are involved in the preparation of core pellets. In the first approach, a mixture of drug and excipient(s)/co-processed excipient is passed through extruders to prepare core pellets. In the second approach, excipient core pellets are prepared by extrusion technique and the drug is layered onto it before the enteric coating. The excipients present in the core pellets decide immediate or extended release of drug in the intestine. The coprocessed excipient pellets provide less batch variability and provide a platform for layering of many drugs before enteric coating. Some patents included enteric coating pellets [CN105456223 (A), CN105596310 (A), CN105616371 (A), CN105663095 (A), CN101611766B, CN106511862 (A), CN106668018 (A), CN106727381 (A), CN106924222 (A), TW200624127 (A), US 2017/0165248A1, US 2017/0224720A1] are discussed.

scholarly journals Nasal Delivery of Acute Medications for Migraine: The Upper Versus Lower Nasal Space

2021 ◽  
Vol 10 (11) ◽  
pp. 2468
Author(s):  
Vincent Martin ◽  
John Hoekman ◽  
Sheena K. Aurora ◽  
Stephen B. Shrewsbury
Keyword(s):  
Acute Treatment ◽  
Drug Efficacy ◽  
Hepatic Metabolism ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Nasal Delivery ◽  
Attractive Alternative ◽  
Gi Tract ◽  
Onset Of Action ◽  
First Pass

The acute treatment of migraine requires effective drugs that are well tolerated and provide rapid and consistent pain relief. Oral tablets are the most commonly used acute treatment for migraine; however, their effectiveness is limited by the rate of gastrointestinal (GI) tract absorption and first-pass hepatic metabolism, and they may not be ideal for patients experiencing GI motility issues. Nasal delivery is an attractive alternative route as it may circumvent GI tract absorption, avoid first-pass metabolism in the liver, and potentially reduce the frequency of GI adverse events. The large surface area and high vascularity within the nose may permit rapid absorption of therapeutics into the systemic circulation, allowing for rapid onset of action. However, the site of drug deposition (upper versus lower nasal cavity) may influence drug pharmacokinetics. Most approved nasal migraine therapies target the lower nasal space where the epithelium is less permeable, and they may be quickly cleared away due to increased ciliary function or dripping from the nose or swallowing, resulting in variable absorption and limited bioavailability. Together with its abundant vascularization, relative mucosal thickness stability, and low clearance rates, the upper nasal space harnesses the benefits of nasal delivery to potentially maximize drug efficacy.

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