Single- and multiple-dose pharmacokinetics of biphasic immediate-release/extended-release hydrocodone bitartrate/acetaminophen (MNK-155) compared with immediate-release hydrocodone bitartrate/ibuprofen and immediate-release tramadol HCl/acetaminophen

Devarakonda, Krishna; Kostenbader, Kenneth; Giuliani, Michael J.; Young, Jack

doi:10.2147/jpr.s83416

Cited by 5 publications

(2 citation statements)

References 19 publications

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“…51 Advantages of combination analgesic therapy include increased clinical efficacy due to additivity or synergy between the individual mechanisms of action, 50 reduced adverse effects due to decreased amounts of the individual components, decreased pill burden, decreased potential for abuse and the overlapping of treatment leading to a decrease in pain. 52,53 However, combinations lead to exposure to more than one type of drug, which may produce unintended adverse effects. 52 Likewise, although lessened, the potential for abuse still remains for products that contain opioids.…”

Section: Inadequacy Of Current Mechanistic Optionsmentioning

confidence: 99%

Cebranopadol: novel dual opioid/NOP receptor agonist analgesic

et al. 2016

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SUMMARYWhat is known and objective: Chronic pain presents a difficult clinical challenge because of the limited efficacy, the limiting adverse-effect profile or the abuse potential of current analgesic options. Cebranopadol is a novel new agent in clinical trials that combines dual agonist action at opioid and nociceptin/orphanin FQ peptide (NOP) receptors. It is the first truly unique, centrally acting analgesic in several years. We here review the basic and clinical pharmacology of cebranopadol. Methods: Published literature and Internet sources were searched to identify information related to the basic science (pharmacology and medicinal chemistry) and development (clinical trial) information on the mechanism of dual opioid and NOP receptor pharmacologic action in general, and for cebranopadol in particular. The identified sources were reviewed and the information synthesized. Results: The preclinical testing of cebranopadol has characterized it as a dual opioid and NOP receptor agonist that displays antinociceptive and antihyperalgesic action in a variety of acute and chronic pain models in animals. Unlike most current traditional opioids, it is generally more potent against neuropathic than nociceptive pain. Several phase 2 clinical trials have been completed. What is new and conclusion: Despite the medical need, a truly novel centrally acting analgesic has not been developed in many years. Cebranopadol represents a truly novel mechanistic approach. Its actual place in pain pharmacotherapy awaits the results of phase 3 clinical trials.

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Section: Inadequacy Of Current Mechanistic Optionsmentioning

confidence: 99%

Cebranopadol: novel dual opioid/NOP receptor agonist analgesic

et al. 2016

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“…The active metabolites of opioids have varying pharmacodynamics or pharmacokinetic action. Single-and multiple-dose pharmacokinetics of biphasic immediate-release/ extended-release hydrocodone bitartrate/acetaminophen (MNK-155) compared with immediate-release hydrocodone bitartrate/ibuprofen and immediate-release tramadol HCl/acetaminophen showed similar peak concentration, steady state concentration and adverse effects [40]. In neonates it has been noted that there is decreased clearance of opioids [22].…”

Section: Metabolismmentioning

confidence: 99%

Opioid Analgesic Choices Based On Pharmacokinetics

2016

JAPM

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Introduction: This study looks the multiple factors- specifically the pharmacokinetics that are involved while selecting an opioid to ensure its optimum efficacy. Combinations of analgesics are an enticing option, for achieving maximal analgesia with minimal adverse reactions. The choice of analgesic depends on the sub-population it caters to, and the etiology of pain involved. Methodology: 112 articles involving an inclusion criteria of “pharmacokinetic aspects in combination of opioid” from a Pubmed search were assessed. Associations among the opioids and suggested guidelines were drawn after thoughtful analysis. Discussion: Single-injection neuraxial; fentanyl and sufentanil are preferred over parenteral opioids. Remifentanil and Dexmedetomidine are preferred for ICU patients. Tramadol can be used for mild to moderate pain, and morphine is the choice for severe and intractable pain. The parenteral routes is commonly used but it is beset with pain and other adverse drug reactions. Conclusion: Combination of analgesics having varied mechanisms of action is advocated for optimizing analgesic therapy. Opioid analgesics are widely used but ferreting out the appropriate dose, route and agent is the crux in effect analgesic. A holistic approach that considers all aspects of an opioid need to be considered before selection, and the pharmacokinetics aspect plays a pivotal role.

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