NSG 502 Week 1 Discussion Board Riviera
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Chose a medication discussed in Week 1 or Week 2. Review the medication in Stahl, S.M. (2017). Stahl’s Essential Psychopharmacology Prescriber’s Guide (6th Ed.).
Your initial post should discuss the medication‘s classification, pharmacodynamics, pharmacokinetics, neurotransmitters and receptor sites involved. Be sure to discuss to if your medication is an agonist, antagonist etc and how it will affect the receptors involved. Discuss side effects, be sure to explain why the side effects may be occurring (remember to use neuroscience and your knowledge of receptor sites). In your discussion of pharmacokinetics be sure to include the CYP 450 system. Lastly, include FDA approval and off label use for this medications. You may include any additional information you find interesting. It is expected that you will have sources for this discussion.
You must respond to two other students’ initial post. Your responses are due 48 hours after the initial post’s due date. Please respond to different medications so you will be exposed to three different medications. Your response post should be substantive, adding to the discussion of the initial post you are responding to. This will requires a minimum of 250 words as well as use APA citations and references.
Venlafaxine is a serotonin norepinephrine reuptake inhibitor used mainly for patients struggling with depression. I chose to investigate this medication further because although I see it prescribed very frequently on the adolescent psychiatric unit I work on, I feel that I do not have a vast understanding of its neuroscience in relation to its value. I am particularly interested in learning more about this drug class and medication because of its theoretical increased rate of remission and increased onset of action time when compared to the typical first line SSRI medications used for depression. When patients are experiencing depression and feeling desperate, an onset time of 2-4 weeks compared to the 4+ weeks it can take other antidepressants to improve mood can be lifesaving.
SNRI’s are known as dual acting medications, although they actually work on norepinephrine, serotonin, and partially dopamine. They inhibit both the serotonin and norepinephrine transporters resulting in increased availability of serotonin and norepinephrine at the synapse. Dopamine is inactivated by norepinephrine reuptake in the prefrontal cortex, therefore this medication can increase dopamine in this area additionally leading to an improved mood (Stahl, 2013). Due to this action venlafaxine is considered a potent serotonin and norepinephrine transport antagonist, with additional but reduced dopamine reuptake antagonism.
Venlafaxine is almost completely absorbed after oral administration with food intake being irrelevant. It is weakly protein bound (27%), and is primarily metabolized by the liver. Effexor is metabolized by CYP2D6 and is converted into the active metabolite O-desvenlafaxine. The parent drug has a 3-7 hour half life, while it’s metabolite has a 9-13 hour half life (Stahl, 2017). It is ultimately excreted through the renal system (Schatzberg & Debattista, 2015).
This drug class has improved safety and tolerability when compared to TCAs, and MAOIs. SNRIs are more selective in the receptors that they target resulting in a decreased affinity for histamine, adrenergic, and cholinergic receptors and therefore less side effects such as weight gain, sedation, orthostatic hypotension, and dry mouth (Schatzberg & Debattista, 2015). Most side effects stem from the increases in serotonin or norepinephrine in areas the drug was not prescribed to target. This can include insomnia stemming from the action of serotonin on sleep centers, and norepinephrine’s effect on sweating and blood pressure. Notable side effects include headache, nervousness, insomnia, diarrhea, nausea, sexual dysfunction, sweating, and high blood pressure. Many side effects can be transient and resolve in 2-3 weeks therefore patients are encouraged to wait and see if side effects resolve prior to altering treatment (Stahl, 2017). The most significant side effects associated with the use of Venlafaxine are increased blood pressure and nausea. The increase in blood pressure associated with the use of SNRIs is related to the increase of norepinephrine available at the synapse. This risk is dose dependent and it is important to monitor blood pressure for patients taking this medication and prior to treatment initiation. The second most troublesome side effect, nausea, can be improved by utilizing the extended release formulation of venlafaxine which can be administered once daily for improved compliance and tolerance (Stahl, 2017).
Venlafaxine doses should be lowered for patients with renal or hepatic impairment. It is also important to taper doses slowly when discontinuing to prevent withdrawal reactions. Drug interactions can include an increased risk of bleeding with anticoagulants, interference of analgesic actions of drugs such as codeine, fatal serotonin syndrome with MAOIs, and an increased risk of seizure when combined with tramadol. There is also evidence that Effexor can increase Haldol levels by effecting excretion (Stahl, 2017). As with many antidepressants the SNRIs come with a black box warning for increased suicidality in children, adolescents, and young adults. For this reason it is critical to monitor patients for suicidal thoughts and intent.
Venlafaxine is FDA approved for the treatment of depression, generalized anxiety disorder, social anxiety disorder, and panic disorder. It is also commonly prescribed for posttraumatic stress disorder and premenstrual dysphoric disorder (Stahl, 2017). It has been shown to improve ADHD, and numerous studies have concluded that it may be a safe and effective option for improving neuropathic pain (Aiyer et al., 2016).
Aiyer, R., Barkin, R. L., & Bhatia, A. (2016). Treatment of neuropathic pain with venlafaxine: A systematic review. Pain Medicine. https://doi.org/10.1093/pm/pnw261
Alan F Schatzberg, & D. M. Charles DeBattista, (2015). Manual of Clinical Psychopharmacology; 8th edition. Arlington: American Psychiatric Publishing.
Stahl, S. M. (2017). Stahl’s essential Psychopharmacology, Prescriber’s guide (6th ed.). Cambridge University Press.
Stephen M. Stahl, (2013). Stahl’s Essential Psychopharmacology Neuroscientific Basis and Practical Applications; 4th Edition. New York: Cambridge University Press.
You did a great job on your post, very extensive about Venlafaxine (Effexor, Effexor XR). One of the benefit, it is both serotonin and norepinephrine reuptake inhibitor. It is FDA approved and can be used for patients that have depression, generalized anxiety disorder, social anxiety disorder which goes hand in hand with GAD, and panic disorder. If patients have more than one diagnoses that I mentioned above Venlafaxine would be one of the best choice for them. “Potential advantages are patients with comorbid anxiety. Patients with depression may have higher remission rates on SNRIs than on SSRIs” (Stahl, 2017, P. 789). Patients with depression that SSRIs don’t work for them, might have a better chance of an SNRI like Venlafaxine that will work. It is the preferred SNRI treatment for depression. Venlafaxine XR is another depressant medication that can be given once a day to reduce side effects of nausea and patients compliance. It has no habit forming, so it cannot be addictive. Venlafaxine XR comes in capsules for patients that cannot swallow whole tablets, especially children and elderlies. Capsules of the medication can be open and sprinkle into a spoon of applesauce or ice cream for them. Providers need to be careful in prescribing it for patients that have high blood pressure and heart problem. Again with this medication, providers have to outweigh the benefits and the risks with their patients.
Carline
Reference:
Stahl, S.M. (2017). Stahl’s Essential Psychopharmacology Prescriber’s Guide.
(6th Ed.). Cambridge University Press: New York, NY. ISBN 978-1-316-61813-4
This was such an informative post on Venlafaxine. I was unaware that Venlafaxine may increase dopamine neurotransmission. I guess this is why there is increased research on the positive effects the medication has on patients diagnosed with ADHD. I see this drug prescribed a lot in my family medicine clinic after patients have tried and failed several SSRI treatment, or who are using for it for a different purpose, such as pain management or migraine prevention. I find it interesting that one of the side effects of this drug is headaches, but yet is used to prevent migraines (Stahl, 2017). According to Dr. Stahl, due to GI and insomnia side effects, Venlafaxine can be augmented with Mirtazapine for improvement in symptoms.
While it is recommended to start out at 37.5mg XR daily, the dosage can increase up to 225mg/day, or even up to 375mg/day for non responders. At lower doses, the medication is mostly serotonergic in nature, while the higher doses are dual serotonin and norepinephrine acting (Stahl, 2017). Luckily, nausea is less of an issue with the extended release tablets, and elevated BP is typically only seen with doses > 225mg/day. While it seems patients tolerate these medications much better than TCA/MAOIs, I think the discontinuation/withdrawal of these medications are a challenge. I have witnessed firsthand the difficulty with discontinuing both venlafaxine and desvenlafaxine at my current family medicine practice. I find it helpful that Dr. Stahl provided tips for discontinuing venlafaxine, such as adding in an SSRI with a long-half life (such as Fluoxetine) prior to discontinuing the SNRI and then taper slowly, and also reducing by 1% every 3 days for patients who struggle (Stahl, 2017).
Lastly, I have noticed that desvenlafaxine is being prescribed more in clinical practice than venlafaxine. I wonder if this is due to desvenlafaxine having a greater potency for NET and thus making it more preferable for those with vasomotor symptoms/pain conditions. I am wondering if anyone has thoughts about this or currently is prescribing these medications.
Overall, I think this SNRI is a great drug to keep in mind for certain patients, and I really learned a lot from your post. Thank you for sharing!
Alexandra
Stahl, S.M. (2017). Stahl’s Essential Psychopharmacology Prescriber’s Guide. (6th Ed.). Cambridge University Press: New York, NY. ISBN 978-1-316-61813-4


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