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Journal articles on the topic 'CNS drugs'

Author: Grafiati

Published: 4 June 2021

Last updated: 5 February 2022

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1

Generali, Joyce A. "CNS and Psychiatric Drugs." Hospital Pharmacy 37, no. 8 (August 2002): 888–94. http://dx.doi.org/10.1177/001857870203700802.

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“Black-box” warnings report valuable postmarketing safety data about prescription drugs, keeping practitioners informed about potential adverse events, drug interactions, key dosing information, monitoring and administration requirements, and at-risk patient populations. They are especially crucial for newly approved agents. A list of agents with black-box warnings does not currently exist; however Hospital Pharmacy will be publishing comprehensive lists by drug category in this column until November 2002. At that time, a complete list in wall chart form will be released. Hospital Pharmacy will update the data as salient information becomes available.

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2

Marsden, Charles A., and S. Clare Stanford. "CNS Drugs III: Psychotherapeutics." Expert Opinion on Investigational Drugs 9, no. 8 (August 2000): 1923–29. http://dx.doi.org/10.1517/13543784.9.8.1923.

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3

Vastag, B. "More Children on CNS Drugs." JAMA: The Journal of the American Medical Association 287, no. 15 (April 17, 2002): 1930—a—1930. http://dx.doi.org/10.1001/jama.287.15.1930-a.

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4

Vastag, Brian. "More Children on CNS Drugs." JAMA 287, no. 15 (April 17, 2002): 1930. http://dx.doi.org/10.1001/jama.287.15.1930-jha20004-2-1.

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5

Schou, Magnus, and Katarina Varnäs. "PET microdosing of CNS drugs." Clinical and Translational Imaging 5, no. 3 (March 23, 2017): 291–98. http://dx.doi.org/10.1007/s40336-017-0226-y.

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6

Tobinick, Edward Lewis. "Perispinal Delivery of CNS Drugs." CNS Drugs 30, no. 6 (April 27, 2016): 469–80. http://dx.doi.org/10.1007/s40263-016-0339-2.

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7

&NA;. "Elderly less tolerant of CNS drugs." Reactions Weekly &NA;, no. 501 (May 1994): 3. http://dx.doi.org/10.2165/00128415-199405010-00005.

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8

Ghose, Karabi. "Prescribing CNS Drugs for Elderly Patients." Drugs & Aging 4, no. 4 (April 1994): 275–84. http://dx.doi.org/10.2165/00002512-199404040-00001.

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9

BOSCHERT, SHERRY. "CNS Drugs And Cognitive Decline Tied." Family Practice News 38, no. 4 (February 2008): 34. http://dx.doi.org/10.1016/s0300-7073(08)70241-x.

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10

Preskorn, Sheldon H. "CNS Drug Development: Part I: The Early Period of CNS Drugs." Journal of Psychiatric Practice 16, no. 5 (September 2010): 334–39. http://dx.doi.org/10.1097/01.pra.0000388628.44405.c0.

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11

Fregni, Felipe. "CNS or Classic Drugs for the Treatment of Pain in Functional Dyspepsia? A Systematic Review and Meta-Analysis of the Literature." October 2008 5;11, no. 10;5 (October 14, 2008): 597–609. http://dx.doi.org/10.36076/ppj.2008/11/597.

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Background: Recent evidence has suggested that pain in functional dyspepsia (FD) is associated with nervous system dysfunction; indicating that therapies aimed at nervous system modulation might be associated with pain relief in FD Objective: To conduct a systematic review and meta-analysis to quantify the efficacy of drugs targeting the central nervous system (antidepressants and antianxiety agents — referred as “CNS drugs”) and drugs targeting gastric modulation (antisecretory and prokinetic — referred as “classic drugs”) for the treatment of pain in FD and, in an exploratory way, compare these 2 modalities of treatment. Methods: MEDLINE and reference lists were examined for relevant articles. We included prospective studies that evaluated the effects of either CNS drugs or classic drugs (subdivided in prokinetic and antisecretory drugs) on the symptoms of FD. Results: Seven studies for CNS drugs and 11 studies for gastric drugs met our inclusion criteria. The analyses of these drugs showed that the 2 groups of drugs are associated with a significant reduction in dyspeptic symptoms. The pooled effect size (standardized mean difference between pre-treatment versus post-treatment means) from the random effects model was 1.25 (95% C.I., 0.83, 1.67) for CNS; 1.63 (95% C.I., 1.28, 1.97) for prokinetic, and 0.93 (95% C.I., 0.57, 1.29) for antisecretory drugs. The exploratory comparison between classes of drugs revealed no significant difference in dyspeptic symptoms reduction between CNS and prokinetic drugs; however CNS drugs were associated with a larger reduction in symptoms as compared with antisecretory drugs. Conclusions: The results show that both CNS and classic drugs are associated with a significant pain reduction in functional dyspepsia. Key words: antidepressants, antianxiety, prokinetics, antisecretory agents, brain activity, functional dyspepsia, epigastric pain

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12

Kharkar, Prashant S. "Drugs acting on central nervous system (CNS) targets as leads for non-CNS targets." F1000Research 3 (March 21, 2014): 40. http://dx.doi.org/10.12688/f1000research.3-40.v2.

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Innovative drug discovery approaches are currently needed to rejuvenate the shrinking product pipelines of the pharmaceutical companies across the globe. Here a theme is presented – the use of central nervous system (CNS) drugs as leads for non-CNS targets. The approach is related to the use of existing drugs for new indications. Suitable chemical modifications of the CNS drugs abolish their CNS penetration. These novel analogs may then be screened for activity against non-CNS targets. Careful selection of the appropriate structural modifications remains the key to success.

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13

Saganuwan, Saganuwan Alhaji. "Chirality of Central Nervous System (CNS) Acting Drugs: A Formidable Therapeutic Hurdle Against CNS Diseases." Central Nervous System Agents in Medicinal Chemistry 19, no. 3 (October 31, 2019): 171–79. http://dx.doi.org/10.2174/1871524919666190624150214.

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Background: Over fifty percent of drugs being used clinically are chiral and 90% of them are racemates. Unfortunately, they have both adverse and beneficial effects on body systems. Methods: Because of the erratic effects of chiral compounds on body functional systems, literature search was carried out with a view to identify CNS chiral drugs, their clinical advantages and disadvantages, unique physicochemical properties and structural modifications into safer drugs. Results: Findings have shown that majority of CNS and non-CNS acting drugs have chiral functional groups that may occur as either dextrorotatory (clockwise) or levorotatory (anticlockwise) or racemates which are inert. Sometimes, the enantiomers (optical isomers) could undergo keto-enol tautomerism, appearing in either acidic or basic or inert form. Chiral CNS acting drugs have agonistic and antagonistic effects, clinical advantages, disadvantages, and special clinical applications, possible modifications for better therapeutic effects and possible synthesis of more potent drugs from racemates. Clockwise chirality may be more effective and safer than the drugs with anticlockwise chirality. When chiral drugs are in racemate state they become inert and may be safer than when they are single. Also, diastereoisomers may be more dangerous than stereoisomers. Conclusion: Therefore, chiral compounds should be adequately studied in lab rodents and primates, and their mechanisms of actions should be comprehensively understood before being used in clinical setting. Since many of them are toxic, their use should be based on principle of individualized medicine. Their molecular weights, functional groups, metabolites, polymers and stereoisomers could be valuable tools for their modifications.

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14

&NA;. "CNS adverse events induced by antimalarial drugs." Reactions Weekly &NA;, no. 556 (June 1995): 3. http://dx.doi.org/10.2165/00128415-199505560-00007.

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15

Kennedy, Gina M., and Samden D. Lhatoo. "CNS Adverse Events Associated with Antiepileptic Drugs." CNS Drugs 22, no. 9 (2008): 739–60. http://dx.doi.org/10.2165/00023210-200822090-00003.

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16

Mart??nez-Cano, H. "Seizures following withdrawal of CNS depressor drugs." Behavioural Pharmacology 6, SUPPLEMENT 1 (May 1995): 85. http://dx.doi.org/10.1097/00008877-199505001-00098.

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17

Lam, Y. W. Francis. "CNS‐active drugs and risk of fall." Brown University Psychopharmacology Update 30, no. 7 (June 8, 2019): 2–3. http://dx.doi.org/10.1002/pu.30445.

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18

Cacabelos, Ramón. "Pharmacogenomics of Central Nervous System (CNS) Drugs." Drug Development Research 73, no. 8 (October 18, 2012): 461–76. http://dx.doi.org/10.1002/ddr.21039.

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19

Rao, Kavitha S., Anuja Ghorpade, and Vinod Labhasetwar. "Targeting anti-HIV drugs to the CNS." Expert Opinion on Drug Delivery 6, no. 8 (June 30, 2009): 771–84. http://dx.doi.org/10.1517/17425240903081705.

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20

Sourkes, Theodore L. "Early clinical neurochemistry of CNS-active drugs." Molecular and Chemical Neuropathology 17, no. 1 (August 1992): 21–30. http://dx.doi.org/10.1007/bf03159978.

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21

Möhler, H., and U. Rudolph. "Selective GABAA circuits for novel CNS drugs." Drug Discovery Today: Therapeutic Strategies 1, no. 1 (September 2004): 117–23. http://dx.doi.org/10.1016/j.ddstr.2004.08.019.

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22

Polianchik, D. E., V. Yu Grigor’ev, G. I. Sandakov, A. V. Yarkov, S. O. Bachurin, and O. A. Raevskii. "Binary Classification of CNS and PNS Drugs." Pharmaceutical Chemistry Journal 50, no. 12 (March 2017): 800–804. http://dx.doi.org/10.1007/s11094-017-1535-1.

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23

Govoni, S., F. Battaini, M. Trabucchi, and R. Paoletti. "CNS effects of calcium channel blocking drugs." International Journal of Developmental Neuroscience 3, no. 4 (1985): 440. http://dx.doi.org/10.1016/0736-5748(85)90135-2.

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24

Sturman, Gillian. "Histaminergic drugs as modulators of CNS function." Pflügers Archiv European Journal of Physiology 431, S6 (November 1996): R223—R224. http://dx.doi.org/10.1007/bf02346349.

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25

Ashley, Elizabeth Dodds. "Antifungal Drugs: Special Problems Treating Central Nervous System Infections." Journal of Fungi 5, no. 4 (October 11, 2019): 97. http://dx.doi.org/10.3390/jof5040097.

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Treating fungal infections in the central nervous system (CNS) remains a challenge despite the availability of new antifungal agents. Therapy is limited by poor understanding of the kinetic properties of antifungal drugs in the CNS compounded by lack of data for many agents. In some cases, clinical response rates do not correspond to data on drug concentrations in the cerebral spinal fluid and/or brain parenchyma. In order to better characterize the use of antifungal agents in treating CNS infections, a review of the essential principles of neuroPK are reviewed. Specific data regarding antifungal drug concentrations in the cerebral spinal fluid and brain tissue are described from human data where available. Alternative dosing regimens and the role of antifungal drug concentration monitoring in treating fungal infections in the CNS are also discussed. Having a better understanding of these key concepts will help guide clinicians in determining the best treatment courses for patients with these devastating infections.

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26

Saganuwan, Saganuwan Alhaji. "Chemistry and Effects of Brainstem Acting Drugs." Central Nervous System Agents in Medicinal Chemistry 19, no. 3 (October 31, 2019): 180–86. http://dx.doi.org/10.2174/1871524919666190620164355.

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Background: Brain is the most sensitive organ, whereas brainstem is the most important part of Central Nervous System (CNS). It connects the brain and the spinal cord. However, a myriad of drugs and chemicals affects CNS with severe resultant effects on the brainstem. Methods: In view of this, a number of literature were assessed for information on the most sensitive part of brain, drugs and chemicals that act on the brainstem and clinical benefit and risk assessment of such drugs and chemicals. Results: Findings have shown that brainstem regulates heartbeat, respiration and because it connects the brain and spinal cord, all the drugs that act on the spinal cord may overall affect the systems controlled by the spinal cord and brain. The message is sent and received by temporal lobe, occipital lobe, frontal lobe, parietal lobe and cerebellum. Conclusion: Hence, the chemical functional groups of the brainstem and drugs acting on brainstem are complementary, and may produce either stimulation or depression of CNS.

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27

&NA;. "Prescribing CNS-active drugs during pregnancy and lactation." Reactions Weekly &NA;, no. 782 (December 1999): 2. http://dx.doi.org/10.2165/00128415-199907820-00001.

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28

Morgan, Althea, and David Clark. "CNS Adverse Effects of Nonsteroidal Anti-Inflammatory Drugs." CNS Drugs 9, no. 4 (1998): 281–90. http://dx.doi.org/10.2165/00023210-199809040-00004.

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29

Wynn, Heather E., Richard C. Brundage, and Courtney V. Fletcher. "Clinical Implications of CNS Penetration of Antiretroviral Drugs." CNS Drugs 16, no. 9 (2002): 595–609. http://dx.doi.org/10.2165/00023210-200216090-00002.

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30

Hroch, Lukas, Laura Aitken, Ondrej Benek, Martin Dolezal, Kamil Kuca, Frank Gunn-Moore, and Kamil Musilek. "Benzothiazoles - Scaffold of Interest for CNS Targeted Drugs." Current Medicinal Chemistry 22, no. 6 (January 20, 2015): 730–47. http://dx.doi.org/10.2174/0929867322666141212120631.

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31

&NA;. "Recommendations for using CNS-active drugs in breastfeeding." Reactions Weekly &NA;, no. 666 (August 1997): 2. http://dx.doi.org/10.2165/00128415-199706660-00001.

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32

Santini, Stefano Angelo, Francesco Panza, Madia Lozupone, Antonello Bellomo, Antonio Greco, and Davide Seripa. "Genetics of tailored medicine: Focus on CNS drugs." Microchemical Journal 136 (January 2018): 164–69. http://dx.doi.org/10.1016/j.microc.2017.02.018.

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33

Schuster, Charles R., and Jack Henningfield. "Conference on abuse liability assessment of CNS drugs." Drug and Alcohol Dependence 70, no. 3 (June 2003): S1—S4. http://dx.doi.org/10.1016/s0376-8716(03)00095-4.

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34

Romach, Myroslava K., Kerri A. Schoedel, and Edward M. Sellers. "Human abuse liability evaluation of CNS stimulant drugs." Neuropharmacology 87 (December 2014): 81–90. http://dx.doi.org/10.1016/j.neuropharm.2014.04.014.

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35

Sourkes, Theodore L. "Early clinical neurochemistry of CNS-active drugs. Bromides." Molecular and Chemical Neuropathology 14, no. 2 (April 1991): 131–42. http://dx.doi.org/10.1007/bf03159932.

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36

Gray, John A., and Bryan L. Roth. "Developing selectively nonselective drugs for treating CNS disorders." Drug Discovery Today: Therapeutic Strategies 3, no. 4 (December 2006): 413–19. http://dx.doi.org/10.1016/j.ddstr.2006.11.009.

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37

Richardson, Peter J., Silvia Ottaviani, Alessandro Prelle, Justin Stebbing, Giacomo Casalini, and Mario Corbellino. "CNS penetration of potential anti-COVID-19 drugs." Journal of Neurology 267, no. 7 (May 2, 2020): 1880–82. http://dx.doi.org/10.1007/s00415-020-09866-5.

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38

Reddy, D. Samba. "Novel Drugs and Biologics of 2016: A Boom for Neurodrugs in the Pipelin." International Journal of Pharmaceutical Sciences and Nanotechnology 10, no. 5 (September 30, 2017): 3809–14. http://dx.doi.org/10.37285/ijpsn.2017.10.5.1.

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This article provides a brief overview of novel drugs approved by the U.S. FDA in 2016. It also focuses on the emerging boom in the development of neurodrugs for central nervous system (CNS) disorders. These new drugs are innovative products that often help advance clinical care worldwide, and in 2016, twenty-two such drugs were approved by the FDA. The list includes the first new drug for disorders such as spinal muscular atrophy, Duchenne muscular dystrophy or hallucinations and delusions of Parkinson’s disease, among several others. Notably, nine of twenty-two (40%) were novel CNS drugs, indicating the industry shifting to neurodrugs. Neurodrugs are the top selling pharmaceuticals worldwide, especially in America and Europe. Therapeutic neurodrugs have proven their significance many times in the past few decades, and the CNS drug portfolio represents some of the most valuable agents in the current pipeline. Many neuroproducts are vital or essential medicines in the current therapeutic armamentarium, including dozens of “blockbuster drugs” (drugs with $1 billion sales potential). These drugs include antidepressants, antimigraine medications, and anti-epilepsy medications. The rise in neurodrugs’ sales is predominantly due to increased diagnoses of CNS conditions. The boom for neuromedicines is evident from the recent rise in investment, production, and introduction of new CNS drugs. There are many promising neurodrugs still in the pipeline, which are developed based on the validated “mechanism-based” strategy. Overall, disease-modifying neurodrugs that can prevent or cure serious diseases, such as multiple sclerosis, epilepsy, and Alzheimer’s disease, are in high demand.

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Yamamoto, Marumi, Yoshinori Ohta, Mio Sakuma, Chisa Matsumoto, and Takeshi Morimoto. "Adverse Drug Events due to Central Nervous System Depressant Drugs in Pediatric Patients With or Without Surgery." Journal of Pediatric Pharmacology and Therapeutics 25, no. 4 (May 1, 2020): 295–302. http://dx.doi.org/10.5863/1551-6776-25.4.295.

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OBJECTIVES To identify differences in the incidence and severity of adverse drug events (ADEs) due to CNS depressant drugs among pediatric patients with and without surgery. METHODS The Japan Adverse Drug Events Study was a cohort study enrolling pediatric inpatients. Potential ADEs were identified by onsite review of medical charts, incident reports, and prescription queries. Two independent physicians classified ADEs and severity. We compared the incidence and characteristics of ADEs between pediatric patients with surgery (surgery group) and without surgery (non-surgery group). We evaluated severity of ADEs due to CNS depressant drugs among both groups. RESULTS We enrolled 944 patients, 234 in surgery group and 710 in non-surgery group. A total of 480 ADEs due to any drugs occurred in 225 patients. Among 81 ADEs due to CNS depressant drugs, 42 ADEs were in surgery group, whereas 39 were in non-surgery group. The risk of fatal or life-threatening ADEs due to CNS depressant drugs was significantly higher than other drugs (12% vs. 2%, p < 0.001). In the surgery group, anesthetics led to 2 fatal or life-threatening, 8 serious, and 30 significant ADEs, whereas in the non-surgery group anesthetics led to 2 fatal or life-threatening, 5 serious, and 4 significant ADEs. Anesthetics were higher risk in the non-surgery group (p = 0.049). CONCLUSIONS The risks of fatal and life-threatening ADEs were significantly higher with CNS depressant drugs than other drugs. Pediatric patients without surgery have higher risks of fatal or life-threatening ADEs due to anesthetics than those with surgery.

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Manallack, David T. "The pKa Distribution of Drugs: Application to Drug Discovery." Perspectives in Medicinal Chemistry 1 (January 2007): 1177391X0700100. http://dx.doi.org/10.1177/1177391x0700100003.

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The acid-base dissociation constant (p Ka) of a drug is a key physicochemical parameter influencing many biopharmaceutical characteristics. While this has been well established, the overall proportion of non-ionizable and ionizable compounds for drug-like substances is not well known. Even less well known is the overall distribution of acid and base p Ka values. The current study has reviewed the literature with regard to both the proportion of ionizable substances and p Ka distributions. Further to this a set of 582 drugs with associated p Ka data was thoroughly examined to provide a representative set of observations. This was further enhanced by delineating the compounds into CNS and non-CNS drugs to investigate where differences exist. Interestingly, the distribution of p Ka values for single acids differed remarkably between CNS and non-CNS substances with only one CNS compound having an acid p Ka below 6.1. The distribution of basic substances in the CNS set also showed a marked cut off with no compounds having a p Ka above 10.5. The p Ka distributions of drugs are influenced by two main drivers. The first is related to the nature and frequency of occurrence of the functional groups that are commonly observed in pharmaceuticals and the typical range of p Ka values they span. The other factor concerns the biological targets these compounds are designed to hit. For example, many CNS targets are based on seven transmembrane G protein-coupled receptors (7TM GPCR) which have a key aspartic acid residue known to interact with most ligands. As a consequence, amines are mostly present in the ligands that target 7TM GPCR's and this influences the p Ka profile of drugs containing basic groups. For larger screening collections of compounds, synthetic chemistry and the working practices of the chemists themselves can influence the proportion of ionizable compounds and consequent p Ka distributions. The findings from this study expand on current wisdom in p Ka research and have implications for discovery research with regard to the composition of corporate databases and collections of screening compounds. Rough guidelines have been suggested for the profile of compound collections and will evolve as this research area is expanded.

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Saleh, Mohammed A. A., Chi Fong Loo, Jeroen Elassaiss-Schaap, and Elizabeth C. M. De Lange. "Lumbar cerebrospinal fluid-to-brain extracellular fluid surrogacy is context-specific: insights from LeiCNS-PK3.0 simulations." Journal of Pharmacokinetics and Pharmacodynamics 48, no. 5 (June 17, 2021): 725–41. http://dx.doi.org/10.1007/s10928-021-09768-7.

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AbstractPredicting brain pharmacokinetics is critical for central nervous system (CNS) drug development yet difficult due to ethical restrictions of human brain sampling. CNS pharmacokinetic (PK) profiles are often altered in CNS diseases due to disease-specific pathophysiology. We previously published a comprehensive CNS physiologically-based PK (PBPK) model that predicted the PK profiles of small drugs at brain and cerebrospinal fluid compartments. Here, we improved this model with brain non-specific binding and pH effect on drug ionization and passive transport. We refer to this improved model as Leiden CNS PBPK predictor V3.0 (LeiCNS-PK3.0). LeiCNS-PK3.0 predicted the unbound drug concentrations of brain ECF and CSF compartments in rats and humans with less than two-fold error. We then applied LeiCNS-PK3.0 to study the effect of altered cerebrospinal fluid (CSF) dynamics, CSF volume and flow, on brain extracellular fluid (ECF) pharmacokinetics. The effect of altered CSF dynamics was simulated using LeiCNS-PK3.0 for six drugs and the resulting drug exposure at brain ECF and lumbar CSF were compared. Simulation results showed that altered CSF dynamics changed the CSF PK profiles, but not the brain ECF profiles, irrespective of the drug’s physicochemical properties. Our analysis supports the notion that lumbar CSF drug concentration is not an accurate surrogate of brain ECF, particularly in CNS diseases. Systems approaches account for multiple levels of CNS complexity and are better suited to predict brain PK.

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Gardner, Shea N. "Scheduling Chemotherapy: Catch 22 between Cell Kill and Resistance Evolution." Journal of Theoretical Medicine 2, no. 3 (2000): 215–32. http://dx.doi.org/10.1080/10273660008833047.

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Dose response curves show that prolonged drug exposure at a low concentration may kill more cells than short exposures at higher drug concentrations, particularly for cell cycle phase specific drugs. Applying drugs at low concentrations for prolonged periods, however, allows cells with partial resistance to evolve higher levels of resistance through stepwise processes such as gene amplification. Models are developed for cell cycle specific (CS) and cell cycle nonspecific (CNS) drugs to identify the schedule of drug application that balances this tradeoff.The models predict that a CS drug may be applied most effectively by splitting the cumulative dose into many (>40) fractions applied by long-term chemotherapy, while CNS drugs may be better applied in fewer than 10 fractions applied over a shorter term. The model suggests that administering each fraction by continuous infusion may be more effective than giving the drug as a bolus, whether the drug is CS or CNS. In addition, tumors with a low growth fraction or slow rate of cell division are predicted to be controlled more easily with CNS drugs, while those with a high proliferative fraction or fast cell division rate may respond better to CS drugs.

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43

Hasan, Zaidi, Nirwan, Ghori, Javid, Ahmadi, and Babar. "Use of Central Nervous System (CNS) Medicines in Aged Care Homes: A Systematic Review and Meta-Analysis." Journal of Clinical Medicine 8, no. 9 (August 23, 2019): 1292. http://dx.doi.org/10.3390/jcm8091292.

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Background: Both old age and institutionalization in aged care homes come with a significant risk of developing several long-term mental and neurological disorders, but there has been no definitive meta-analysis of data from studies to determine the pooled estimate of central nervous system (CNS) medicines use in aged care homes. We conducted this systematic review to summarize the use of CNS drugs among aged care homes residents. Methods: MEDLINE, EMBASE, CINAHL, Scopus, and International Pharmaceutical Abstracts (IPA) databases were searched (between 1 January 2000 and 31 December 2018) to identify population-based studies that reported the use of CNS medicines in aged care homes. Pooled proportions (with 95% confidence interval), according to study location were calculated. Results: A total of 89 studies reported the use of CNS medicines use in aged care. The pooled estimate of CNS drugs use varied according to country (from 20.3% in Ireland to 49.0% in Belgium) and region (from 31.7% in North America to 42.5% in Scandinavia). The overall pooled estimate of psychotropic medicines use was highest in Europe (72.2%, 95% CI, 67.1–77.1%) and lowest in ANZ region (56.9%, 95% CI, 52.2–61.4%). The pooled estimate of benzodiazepines use varied widely from 18.9% in North America to 44.8% in Europe. The pooled estimate of antidepressants use from 47 studies was 38.3% (95% CI 35.1% to 41.6%) with highest proportion in North America (44.9%, 95% CI, 35.3–54.5%). Conclusion: The overall use of CNS drugs varied among countries, with studies from Australia-New Zealand reported the lowest use of CNS drugs. The criteria for prescribing CNS drugs in clinical practice should be evidence-based. The criteria should be used not to prohibit the use of the listed medications but to support the clinical judgement as well as patient safety.

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44

Nwogu, Jacinta Nwamaka, Qing Ma, Chinedum Peace Babalola, Waheed Adeola Adedeji, Gene D. Morse, and Babafemi Taiwo. "Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals." AIDS Research and Treatment 2016 (2016): 1–13. http://dx.doi.org/10.1155/2016/2587094.

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Neurological complications associated with the human immunodeficiency virus (HIV) are a matter of great concern. While antiretroviral (ARV) drugs are the cornerstone of HIV treatment and typically produce neurological benefit, some ARV drugs have limited CNS penetration while others have been associated with neurotoxicity. CNS penetration is a function of several factors including sieving role of blood-brain and blood-CSF barriers and activity of innate drug transporters. Other factors are related to pharmacokinetics and pharmacogenetics of the specific ARV agent or mediated by drug interactions, local inflammation, and blood flow. In this review, we provide an overview of the various factors influencing CNS penetration of ARV drugs with an emphasis on those commonly used in sub-Saharan Africa. We also summarize some key associations between ARV drug penetration, CNS efficacy, and neurotoxicity.

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45

Alelyunas, Yun W., James R. Empfield, Dennis McCarthy, Russell C. Spreen, Khanh Bui, Luciana Pelosi-Kilby, and Cindy Shen. "Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate." Bioorganic & Medicinal Chemistry Letters 20, no. 24 (December 2010): 7312–16. http://dx.doi.org/10.1016/j.bmcl.2010.10.068.

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Paul, Steven. "CNS drug discovery in the 21st century." British Journal of Psychiatry 174, S37 (February 1999): 23–25. http://dx.doi.org/10.1192/s0007125000293628.

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The discovery of new drugs for psychiatric and neurological disorders has been greatly facilitated by advances in molecular biology, genetics and chemistry. Several examples are given of how these revolutionary advances have been applied to the discovery of new drugs that selectively modify serotonergic neurotransmission, including compounds which may prove to be more effective antidepressants.

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Saganuwan, Saganuwan A. "Conversion of Benzimidazoles, Imidazothiazoles and Imidazoles into more Potent Central Nervous System Acting Drugs." Central Nervous System Agents in Medicinal Chemistry 20, no. 1 (March 3, 2020): 3–12. http://dx.doi.org/10.2174/1871524919666190621160323.

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Background: Benzimidazole (albendazole), imidazothiazole (levamisole) and imidazole (euconazole) are used in chemotherapy of helminthosis and mycosis respectively, with central nervous system (CNS) side effects. But only a limited number of azole groups are used clinically in the treatment of CNS diseases, which are on increase and could not be cured permanently. Due to increased incidence of more challenging new CNS diseases, there is a need for the synthesis of more potent CNS drugs. Methods: Hence, literature studies were carried out for the identification of common pathways for the synthesis of the three groups of compounds, their CNS properties and the possibility of modifying them to potent CNS drugs. Results: Findings have shown that gloxal with formaldehyde in the presence of ammonia can be converted into imidazole, imidazothiazole and benzimidazole via distillation, condensation, alkylation, acylation, oxidation, cyclization, sulphation and amidation. However, agents such as phosphorus pentoxide, ethanolic potassium hydroxide, sodium hypochlorite, sodium hexafluroaluminate, aniline, calcium acetate, calcium benzoate, sodium hydroxide, aromatic aldehydes, bromoketones, alpha dicarbonyl compounds among others are used as reagents. The furan ring(s) may have a strong capability of penetrating CNS for the treatment of neurological disorders. The products from the three groups have agonistic, antagonistic, mixed agonistic and mixed antagonistic depressant and stimulant activities due to the presence of heteroatoms such as nitrogen, oxygen and sulphur. Imidazole may be the most potent with best characteristics of CNS penetrability and activity followed by imidazothiazole and benzimidazole. Conclusion: Azole group is common to all the three classes and may be responsible for some of their CNS effects. The resultant compounds could act via all neurotransmitters, voltage and ligand-gated ion channels and may be chiral.

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Duarte, Diana, Armando Cardoso, and Nuno Vale. "Synergistic Growth Inhibition of HT-29 Colon and MCF-7 Breast Cancer Cells with Simultaneous and Sequential Combinations of Antineoplastics and CNS Drugs." International Journal of Molecular Sciences 22, no. 14 (July 10, 2021): 7408. http://dx.doi.org/10.3390/ijms22147408.

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Several central nervous system (CNS) drugs exhibit potent anti-cancer activities. This study aimed to design a novel model of combination that combines different CNS agents and antineoplastic drugs (5-fluorouracil (5-FU) and paclitaxel (PTX)) for colorectal and breast cancer therapy, respectively. Cytotoxic effects of 5-FU and PTX alone and in combination with different CNS agents were evaluated on HT-29 colon and MCF-7 breast cancer cells, respectively. Three antimalarials alone and in combination with 5-FU were also evaluated in HT-29 cells. Different schedules and concentrations in a fixed ratio were added to the cultured cells and incubated for 48 h. Cell viability was evaluated using MTT and SRB assays. Synergism was evaluated using the Chou-Talalay, Bliss Independence and HSA methods. Our results demonstrate that fluphenazine, fluoxetine and benztropine have enhanced anticancer activity when used alone as compared to being used in combination, making them ideal candidates for drug repurposing in colorectal cancer (CRC). Regarding MCF-7 cells, sertraline was the most promising candidate alone for drug repurposing, with the lowest IC50 value. For HT-29 cells, the CNS drugs sertraline and thioridazine in simultaneous combination with 5-FU demonstrated the strongest synergism among all combinations. In MCF-7 breast cancer cells, the combination of fluoxetine, fluphenazine and benztropine with PTX resulted in synergism for all concentrations below IC50. We also found that the antimalarial artesunate administration prior to 5-FU produces better results in reducing HT-29 cell viability than the inverse drug schedule or the simultaneous combination. These results demonstrate that CNS drugs activity differs between the two selected cell lines, both alone and in combination, and support that some CNS agents may be promising candidates for drug repurposing in these types of cancers. Additionally, these results demonstrate that 5-FU or a combination of PTX with CNS drugs should be further evaluated. These results also demonstrate that antimalarial drugs may also be used as antitumor agents in colorectal cancer, besides breast cancer.

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AHMED, SAIMA, MUHAMMAD ASADULLAH, and ATA-UR REHMAN. "EFFECT OF DRUGS;." Professional Medical Journal 20, no. 01 (December 10, 2012): 103–13. http://dx.doi.org/10.29309/tpmj/2013.20.01.586.

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ABSTRACT... Objective: The aim of this study was to determine head-dipping exploratory test parameter as a measure of strongmodulating effect on brain and behavior. Design: It was an observational animal study. Setting: University of Karachi. Period: Jan 2004 toJuly 2006. Material & methods: In this present study, drugs used reserpine, nux- vomica; anacardium and chlorpromazine were widerange of pharmacological actions. We evaluate the effectiveness of these drugs as agents with modulating effect on brain and behavioraccessed by head dipping parameter. In this study, 25 mice were included belonging to both sexes. The study animals were divided intofive groups of five animals each. Four groups were given drugs and one group was kept as control. Mice (20-35g) of either sex were usedin this study. One group was kept as control for drugs. Mice were kept under room temperature. Tap-water was allowed ad-Libitum.30minutes after giving drugs, animals were observed for 10 minutes with two minutes of interval. Tablet crushed in 10ml of water, 1cc wasgiven. Screening method used was head dipping. Results: Strychnos Nux-Vomica when used in a dose of 0.07mg has strong action oncholinergic system, CNS activity and frequent head dipping (39.8±28.8) was observed. Rauwolfia serpentine is an active alkaloidparticularly present in reserpine (62.2±43.4) no significant head dipping effect was observed. Anacardium (37.2±28.6) &Chlorpromazine (39.4±32.4), show decrease effects. Keeping in view, the medicinal importance of these herbs, our present study wasdesigned to screen these drugs for CNS activity on albino mice.

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Lochhead, Jeffrey J., and Thomas P. Davis. "Perivascular and Perineural Pathways Involved in Brain Delivery and Distribution of Drugs after Intranasal Administration." Pharmaceutics 11, no. 11 (November 12, 2019): 598. http://dx.doi.org/10.3390/pharmaceutics11110598.

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One of the most challenging aspects of treating disorders of the central nervous system (CNS) is the efficient delivery of drugs to their targets within the brain. Only a small fraction of drugs is able to cross the blood–brain barrier (BBB) under physiological conditions, and this observation has prompted investigation into the routes of administration that may potentially bypass the BBB and deliver drugs directly to the CNS. One such route is the intranasal (IN) route. Increasing evidence has suggested that intranasally-administered drugs are able to bypass the BBB and access the brain through anatomical pathways connecting the nasal cavity to the CNS. Though the exact mechanisms regulating the delivery of therapeutics following IN administration are not fully understood, current evidence suggests that the perineural and perivascular spaces of the olfactory and trigeminal nerves are involved in brain delivery and cerebral perivascular spaces are involved in widespread brain distribution. Here, we review evidence for these delivery and distribution pathways, and we address questions that should be resolved in order to optimize the IN route of administration as a viable strategy to treat CNS disease states.

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