Category: Psychiatric and Neurological

Alprazolam (Xanax®, Niravam®)

Alprazolam is a short-acting benzodiazepine medication used in the treatment of anxiety disorders.  It acts as a positive allosteric modulator of synaptic GABAA receptors, increasing neuronal hyperpolarization and CNS depressant effects.  Alprazolam is the only benzodiazepine with significant antidepressant efficacy.

Continue reading “Alprazolam (Xanax®, Niravam®)”

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Lidocaine HCl (Xylocaine®, Zingo®, Lidoderm®, RectiCare®, LMX®, Akten®)

Continue reading “Lidocaine HCl (Xylocaine®, Zingo®, Lidoderm®, RectiCare®, LMX®, Akten®)”

Bupropion (Wellbutrin®, Forvivo®, Zyban®, Aplenzin®)

Overview

Bupropion is an aminoketone antidepressant medication indicated for the treatment of major depressive disorder and to reduce withdrawal symptoms during smoking cessation. Continue reading “Bupropion (Wellbutrin®, Forvivo®, Zyban®, Aplenzin®)”

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®)”

Sertraline (Zoloft®)

Overview

Sertraline is a selective serotonin reuptake inhibitor drug used in the treatment of major depressive disorder and anxiety disorders.  It blocks the serotonin transporter (SERT) and increases CNS synaptic concentrations of serotonin, thereby enhancing serotonergic neurotransmission.  Through incompletely understood mechanisms, this contributes to both acute and adaptive neuronal changes that lead to improved mood and decreased anxiety.

Sertraline has approved uses in post-traumatic stress disorder, OCD, social anxiety, panic disorder, premenstrual dysphoric disorder, and major depressive disorder.  The most common adverse effects include dry mouth, drowsiness, and sexual dysfunction but use of the drug may be associated with more serious conditions.  Patients < 24y may experience increased suicidality, and patients with bipolar I/II can trigger a hypomanic/manic episode via sertraline exposure.  Concomitant use with other serotonergic medications (e.g., SNRIs, triptans) can also lead to serotonin syndrome.

In Plain English

Sertraline changes the chemical balance in your brain by increasing the amount of active serotonin, which regulates mood and stress.

Clinical Considerations

sertraline.png

Figure 1. Sertraline clinical considerations at a glance

Evidence Basis

  • For depression: http://www.cochrane.org/CD006117/DEPRESSN_sertraline-versus-other-antidepressive-agents-for-depression

 

Sertraline In the News

https://www.cbsnews.com/news/antidepressants-really-work-study-confirms-some-better-than-others/

 

 

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 9.
  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/.

 

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/.

 

Succinylcholine (Anectine®, Quelicin®)

Succinylcholine is a nicotinic cholinergic receptor agonist used as a paralytic in emergency procedures and surgery.  It binds to and activates postsynaptic nAChR at the neuromuscular junction, which depolarizes muscle end plates.  Since succinylcholine is more resistant than acetylcholine to synaptic acetylcholinesterase degradation, the drug maintains a depolarized neuromuscular block for the duration of its effect.

Succinylcholine manifests a rapid onset and short duration of action.  In patients with previously undiagnosed genetic myopathies (e.g., Duchenne muscular dystrophy), administration of the drug can cause a severe reaction marked by rhabdomyolysis and hyperkalemia.  Other serious adverse reactions include anaphylaxis and malignant hyperthermia.

 

succinylcholine

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/.

 

Venlafaxine (Effexor®)

Venlafaxine is a serotonin-norepinephrine reuptake inhibitor (SNRI)-class antidepressant drug used in the treatment of major depressive disorder (MDD) and several anxiety disorders.  Due to concerns about increased risk of suicide in younger patients, this drug is generally prescribed for selective serotonin reuptake inhibitor (SSRI)-refractory cases.

Venlafaxine works primarily by inhibiting presynaptic serotonin reuptake in the CNS, alongside less potent blockade of the norepinephrine and dopamine transport.  It has several off-label uses including post-traumatic stress disorder and migraine headache prophylaxis.

venlafaxine

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