Tag: Pain

Elagolix (Orilissa™)

Continue reading “Elagolix (Orilissa™)”

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Pharmacology News Round-Up: June 21st, 2018

This week’s clinical pharmacology highlights include advances in cancer therapy, long-term followup of the landmark PROACT trial comparing anticoagulation strategies after aortic replacement, and the finding that hydrocortisone may not reduce mortality in septic shock.

Continue reading “Pharmacology News Round-Up: June 21st, 2018”

Ibuprofen (Motrin®, Caldolor®, Advil®)

Overview

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) and non-selective cyclooxygenase inhibitor indicated for the treatment of mild-moderate pain, fever, and arthritis.  Its analgesic, antipyretic, and anti-inflammatory properties are thought to be mediated through inhibition of the cyclooxygenase-2 (COX-2) enzyme.  COX-2 is upregulated by cells during the inflammatory response, resulting in increased production of PGE2 and leading to tissue inflammation, fluid extravasation, pyrexia, pain, and vasodilation.  Inhibition of prostaglandin synthesis by ibuprofen blocks inflammatory signaling pathways and decreases pain and body temperature. Continue reading “Ibuprofen (Motrin®, Caldolor®, Advil®)”

Hydrocodone-Acetaminophen (Vicoden, Norco, Lortab, Maxidone, Xodol, Hycet®)

Overview

Combination hydrocodone/acetaminophen is an analgesic medication prescribed for the treatment of acute and chronic pain.  Hydrocodone activates pre- and post-synaptic μ-opioid receptors in the central nervous system (CNS) and mediates suppression of nociceptive signaling through both ascending and descending neuronal pain tracts.  Hydrocodone is metabolized to hydromorphone, a metabolite with strong agonist properties at the μ-opioid receptor.

Acetaminophen is a non-selective cyclooxygenase (COX) inhibitor that acts primarily in the central nervous system and in endothelial cells, mitigating pain sensation through incompletely understood mechanisms.  Unlike non-steroidal anti-inflammatory drugs (NSAIDS), which also inhibit arachidonate metabolism via inhibition of COX, acetaminophen does not appear to be active in platelets and lymphocytes and thus demonstrates minimal anti-inflammatory or anti-platelet activity.

Opioid combination medications are one of the most frequently prescribed medications in the United States, often given as post-procedural analgesic agents.  They carry a high risk of abuse, dependency, and lethal overdose.

In Plain English

Hydrocodone-acetaminophen medications combine two different painkillers in one pill to decrease pain sensations.  Hydrocodone is an opioid drug, affecting your nerves and brain through the same mechanism as morphine and heroin.  Acetaminophen works by blocking a key enzyme responsible for producing pain sensation and fever.

Clinical Considerations

hydrocodone_acetaminophen

Figure 1. Hydrocodone-Acetaminophen combination clinical considerations at a glance

 

Evidence Basis

 

Hydrocodone-Acetaminophen Combination In the News

 

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 May 14.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRxhttp://www.goodrx.com
  4. “DailyMed.” U.S. National Library of Medicine, National Institutes of Health, dailymed.nlm.nih.gov/dailymed/.

 

Gabapentin (Neurontin®, Gralise®)

Overview

Gabapentin is a neuronal calcium channel blocker and GABA synthesis/degradation modulator used in the treatment of epilepsy involving non-generalizing partial seizures, as well as post-herpetic neuralgia (PHN).  Continue reading “Gabapentin (Neurontin®, Gralise®)”

Codeine Sulfate (Generic)

Codeine is an opioid drug indicated for mild-to-moderate pain.  It functions as a selective μ-opioid receptor agonist and provides milder analgesia and fewer euphoric effects than morphine and several of the synthetic opioids (e.g., fentanyl).  Patients in whom non-opioid pain control (e.g., NSAIDS, acetaminophen, combination medications) has failed should be considered for weak opioids like codeine or tramadol before escalation to strong opioids like hydrocodone or morphine.

Codeine is sometimes prescribed off-label for cough (it is FDA-approved for this use only in combination with chlorpheniramine/guaifenesin/etc) and for acute diarrhea unresponsive to other anti-motility agents.   The drug is contraindicated in fast CYP2D6 metabolizers due to accelerated conversion to morphine and increased risk of respiratory depression and death.  Codeine carries a significant risk of abuse and dependency.

 

codeine

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 April 29.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRxhttp://www.goodrx.com
  4. “DailyMed.” U.S. National Library of Medicine, National Institutes of Health, dailymed.nlm.nih.gov/dailymed/.

 

Celecoxib (Celebrex®) – Non-Steroidal Anti-Flammatory

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) used to treat pain and certain inflammatory conditions.  It is a selective inhibitor of cyclooxygenase-2 (COX2), blocking PGH-2 and downstream PGE-2 synthesis.  Decreased prostaglandin production impairs pro-inflammatory pathways and leads to decreased pain sensation.

Other COX-2-specific inhibitors have been withdrawn from the market due to concerns about thromboembolic risk.  The United States FDA recently determined that the available evidence does not conclusively demonstrate an elevated thromboembolic risk with celecoxib use relative to other NSAIDS.

celecoxib

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 April 26.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRx, www.goodrx.com
  4. Stein, Rob. “FDA Panel Affirms Safety Of Painkiller Celebrex.” NPR, NPR, 25 Apr. 2018, www.npr.org/sections/health-shots/2018/04/25/605226604/fda-panel-affirms-safety-of-painkiller-celebrex.

Methadone (Methadose®, Dolophine®) – Synthetic Opioid

Methadone is a synthetic μ-opioid receptor agonist prescribed for the treatment of opioid dependence and withdrawal.  It is also used in severe pain conditions at lower doses.

Methadone has a longer half-life and fewer euphoric effects than morphine and other opioids, but still carries a dose-dependent risk of the toxicities associated with this class of drugs.  Sedation, dizziness, and headache are common side effects and incorrect dosing or abuse can result in profound sedation, respiratory depression, and death.

methadone

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 April 24.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRx, www.goodrx.com