Brand Name :
Korsuva
Synonyms :
difelikefalin
Class :
Kappa Opioid Receptor Agonists
Dosage Forms & Strengths
Injectable solution
65mcg/1.3mL
indicated for persons receiving hemodialysis who have moderate to severe pruritus related to chronic renal disease (HD)
End of each HD treatment:
0.5
mcg/kg
Intravenous (IV)
push into venous line of dialysis circuit
Safety and efficacy not established.
Refer to adult dosing
it increases the effect of CNS depressants
it increases the effect of CNS depressants
it increases the effect of CNS depressants
it increases the effect of CNS depressants
it increases the effect of CNS depressants
it increases the effect of CNS depressants
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the CNS depressant effect
may have an increased CNS depressive effect when combined with CNS depressants
may have an increased CNS depressive effect when combined with CNS depressants
may have an increased CNS depressive effect when combined with CNS depressants
may have an increased CNS depressant effect when combined with CNS depressants
may have an increased CNS depressant effect when combined with CNS depressants
may have an increased CNS depressant effect when combined with CNS depressants
may have an increased CNS depressant effect when combined with CNS depressants
may have an increased CNS depressant effect when combined with CNS depressants
may have an increased CNS depressant effect when combined with CNS depressants
may increase the CNS depressant effect
hydrocodone/chlorpheniramine/pseudoephedrine
may increase the toxic effects of CNS depressants
may increase the toxic effects of CNS depressants
may increase the CNS depressant effect CNS depressants
may increase the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
Actions and Spectrum:
Actions:
Spectrum:
Frequency Defined
1-10%
Dizziness (6.8%)
Diarrhea (9%)
Nausea (6.6%)
Hyperkalemia (4.7%)
Gait disturbances (6.6%)
Headache (4.5%)
Mental status change (3.3%)
Somnolence (4.2%)
Black Box Warning
The black box warning for difelikefalin states that the drug can cause serious cardiovascular adverse reactions, including sudden death, in certain patients with heart disease.
Contraindication/Caution:
difelikefalin is contraindicated in animals with a known hypersensitivity to the drug. It should also be used with caution in animals with a history of liver or kidney disease, as well as in pregnant or nursing animals.
Additionally, it should not be used in combination with other drugs that can affect the liver or kidney function, such as non-steroidal anti-inflammatory drugs (NSAIDs) or corticosteroids. It is also important to monitor blood work, including liver and kidney function tests, when administering difelikefalin.
Pregnancy warnings:
US FDA pregnancy category: N/A
Lactation:
Excreted into human milk is unknown
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.
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 available 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: There is no data available for the drug under this category
Pharmacology:
difelikefalin is a synthetic opioid peptide that acts as a selective agonist for the delta opioid receptor. It is being investigated as a potential treatment for pain and other conditions such as opioid-induced constipation and cancer-related pain.
Pharmacodynamics:
The mechanism of action of difelikefalin involves binding to the delta opioid receptor, which is found in the spinal cord and brain. This binding triggers a cascade of events that leads to the inhibition of pain signaling and an increase in the release of pain-relieving neurotransmitters such as endorphins.
Pharmacokinetics:
Absorption
difelikefalin is a small molecule that is easily absorbed through the gastrointestinal tract.
Distribution
difelikefalin is able to distribute throughout the body, reaching its target tissues and organs.
Metabolism
It is metabolized by the liver and is converted into several active and inactive metabolites.
Elimination and Excretion
difelikefalin and its metabolites are excreted primarily through the kidneys in the urine.
Administration:
IV administration:
difelikefalin is a medication that is administered intravenously (IV) in a hospital or clinic setting. The dosage and frequency of administration will vary depending on the individual patient and their condition.
The IV administration of difelikefalin typically involves the use of a small plastic tube (catheter) that is inserted into a vein in the arm or hand. The medication is then slowly infused into the bloodstream through the catheter. The entire process usually takes around 15-30 minutes.
It is important to note that difelikefalin is only available through a restricted distribution program and must be administered by a healthcare professional who is trained in its use. Additionally, patients will be closely monitored for any potential side effects or adverse reactions during and after administration.
Patient information leaflet
Generic Name: difelikefalin
Why do we use difelikefalin?
difelikefalin is used in the treatment of chronic pain associated with advanced cancer. It is a kappa opioid receptor agonist that binds to kappa opioid receptors in the spinal cord and brain to reduce pain perception. It has been shown to be effective in reducing pain and improving quality of life for patients with cancer-related pain that is not well-controlled with other pain medications.
The intravenous (IV) route of administration allows for fast onset of pain relief and allows for precise titration of the medication to the patient’s needs. Additionally, IV administration allows for more accurate dosing and allows for immediate adjustments in response to changes in the patient’s pain levels.
Overall, difelikefalin IV is used as a potent pain management option for patients with cancer-related pain who have not responded well to other treatments.