fentanyl transmucosal

Action and Spectrum

Actions and Spectrum: 

Actions: 

fentanyl transmucosal formulations provide potent analgesic (pain-relieving) effects by binding to opioid receptors of the CNS. They help to alleviate severe pain, including breakthrough pain episodes that occur despite ongoing opioid therapy. 

fentanyl transmucosal medications are designed to provide a rapid onset of pain relief. When used as directed, they can deliver fentanyl directly into the bloodstream via mucous membranes of the mouth or buccal cavity, leading to a relatively quick onset of action. 

Spectrum: 

The spectrum of fentanyl transmucosal refers to its effectiveness and potential uses. fentanyl transmucosal products are indicated explicitly for breakthrough cancer pain in patients tolerant to opioid therapy. Breakthrough pain is a sudden and severe flare-up that occurs despite ongoing opioid treatment for chronic cancer pain. fentanyl transmucosal formulations are intended to provide additional analgesia during these episodes of breakthrough pain. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Asthenia 

Confusion 

Constipation 

Dry mouth 

Nausea 

Somnolence 

Sweating 

Vomiting 

1-10% 

Anorexia 

Abdominal pain 

Diarrhea 

Euphoria 

Anxiety 

Apnea 

Depression 

Fatigue 

Dizziness 

Dyspepsia 

Dyspnea 

Hemoptysis 

Hypoventilation 

Hallucinations 

Headache 

Pruritus 

Urinary retention 

Influenza-like symptoms 

Nervousness 

Pharyngitis 

Upper respiratory tract infection 

Frequency Not Defined 

Amnesia 

Agitation 

Abnormal coordination 

Thinking 

Gait 

Dreams 

Application site reaction 

Flatulence 

Micturition disorder 

Back pain 

Bronchitis 

Fever 

Mucosal inflammation 

Hiccups 

Accidental injury 

Rhinitis, sinusitis 

Speech disorder 

Paranoid reaction 

Paresthesia 

Rash 

Syncope 

ST-segment elevation 

Ventricular tachycardia 

Tremor 

Bradycardia 

QT-interval prolongation 

Severe cardiac arrhythmias 

Cardiac arrest 

MI 

Angina pectoris 

Visual disturbances 

Mental clouding 

Respiratory/circulatory depression 

Respiratory arrest 

Shock 

Black Box Warning

Black Box Warning: 

• Risk of Respiratory Depression: fentanyl transmucosal formulations can cause respiratory depression, characterized by slow or shallow breathing. Respiratory depression can be life-threatening, leading to coma or death, especially in non-opioid-tolerant individuals or those who receive higher-than-recommended doses. 
• Risk of Accidental Ingestion: fentanyl transmucosal products should be kept out of reach of children. Accidental ingestion, especially by young children, can result in a fatal overdose due to the high potency of fentanyl. 
• Addiction, Abuse, and Misuse: fentanyl is a potent opioid with a high risk of addiction, abuse, and misuse. It leads to psychological and physical dependence, and individuals with a history of substance addiction or abuse may be at higher risk. Misuse of fentanyl transmucosal products can lead to overdose and death. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Active pathological bleeding 

Cautions 

• Increased risk of bleeding 
• Renal impairment 
• Hepatic impairment 
• Drug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

Category C 

Breastfeeding warnings:  

The drug is excreted in breast milk.  

Use the during lactation only when no other substitute is available.  

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

fentanyl, the active ingredient in fentanyl transmucosal formulations, is a potent opioid analgesic. It acts primarily by binding to the mu-opioid receptors in the central nervous system, exerting agonist effects. By activating these receptors, fentanyl inhibits the transmission of pain signals, resulting in analgesia. 

Pharmacodynamics: 

• Analgesia: fentanyl transmucosal provides potent analgesia by binding to mu-opioid receptors in the brain, spinal cord, and peripheral tissues.  
• Respiratory Depression: fentanyl is a potent respiratory depressant, and fentanyl transmucosal formulations can cause dose-dependent respiratory depression.  
• Sedation and CNS Effects: fentanyl transmucosal can cause sedation, drowsiness, and CNS depression. It can also induce a euphoric effect and alter mood and cognition. 

Pharmacokinetics: 

Absorption 

The bioavailability of onsolis is 71% 

The duration of action is 1-2 hours 

Distribution 

The peak plasma concentration is achieved at 0.5-4 hours 

Metabolism 

CYP3A4 extensively metabolizes the drug. Inactive nor fentanyl metabolites are formed 

Elimination and Excretion 

The half-life is 1.5-6 hours 

The drug is excreted in feces and urine. 

Adminstartion

Administration: 

fentanyl transmucosal formulations are typically administered using specific delivery systems designed for mucosal absorption. The most common administration forms include fentanyl buccal tablets (also known as fentanyl buccal soluble film) and fentanyl sublingual tablets (also known as fentanyl sublingual spray). 

Patient Information Leaflet

Patient information leaflet 

Generic Name: fentanyl transmucosal 

Pronounced: fen-tah-nyl traans-myuh-cosal 

Why do we use fentanyl transmucosal? 

fentanyl transmucosal formulations are designed to provide rapid relief during cancer breakthrough pain episodes.