cns side effects
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2021 ◽  
Vol 3 (1) ◽  
pp. 120-124
Author(s):  
Ahmad Ramadhanu

Nausea and vomiting in pregnancy (NVP) is one of the common main complaint in pregnancy. NVP can be a significant burden to the patient, make a decrease in quality of life, pregnancy threatening or even worse can lead to nutritional loss and death. NVP diagnosed when in first trimester of pregnancy and the other possible cause of NVP is excluded. Management of NVP is included maintaining hydration, nutrition, and lifestyle modification. Also avoiding the smells, food, or activity that can cause nause are necessary. There are some methods to treat NVP including pharmalogical or non-pharmalogical. The non-pharmalogical approach is change nutritional habits, lifestyle and medications. Several pharmalogical agents that can be used to relief the symptoms of NVP are pyridoxine, anti- histamines, metoclopramide, pyridoxine/doxylamine, promethazine and metoclopramide. Some patients also want to try more “natural” medications for NVP like ginger. The pharmacological activity is thought to stand in the pungent principles (gingerols and shogaols) and volatile oils (sesquiterpenes and monoterpenes). The true mechanism of action of ginger is probable to be a gastric effect, to increase tone and peristaltic due to anticholinergic and antiserotonin act. Ginger acts straight to the digestive tract and avoids the CNS side effects common to centrally acting antiemetics. Ginger is available in capsule or syrup form or in candy, cookies, beer, tinctures, teas, sodas, and jam. Nowadays, true dosing is available only if one uses standardized extracts; however, women may choose to use another form of ginger.


2020 ◽  
pp. 512-517
Author(s):  
Said Al Jaadi ◽  
Yahya Al Kindi ◽  
Tariq Al-Saadi

Background: One in every three related-injury deaths in United State are linked directly to traumatic brain injury (TBI), for which it is considered as a leading cause of death. Traumatic brain injury took place due to severe head assault to a hard object, with headache and vomiting being amongst the most common presenting symptoms. Metoclopramide is an old antiemetic agent that has been used widely for nausea and vomiting in TBI patients. Aim: A systematic review of the literature to investigate the safety of metoclopramide in treating traumatic brain injury patients. Methods: A literature review was conducted in 6 databases, we determine the pertinence of a study to the inclusion criteria by assessing the title, keywords, and abstracts. Five studies were found to be relevant. Data were extracted using multiple variables that were formulated incongruent with the study aim and then further analyzed. Results: The collective sample size was 93 patients with an average of age 38.5 years. 51.6 % were male and 48.6% were females. Most patients received 10 mg metoclopramide IV with a percentage of 77.4%. While only 22.5% received 20 mg IV metoclopramide. Seventy-one patients received metoclopramide alone and 22 received combination therapy.  Headache was the most common reported side effect (46.2 %), followed by anxiety and drowsiness with (39.7%) and (27.9 %); respectively. Fatigue reported in (24.7%), while dystonia was the least common and developed only in 5.3%. Conclusion: Metoclopramide is a common medication used to treat TBI patients in the emergency department. However, the review demonstrated that the central nervous system (CNS) side effect is excepted. Alternative options with lower CNS side effects may be better tried.


Author(s):  
Said Al Jaadi ◽  
Yahya Al-Kindi ◽  
Tariq Al-Saadi

Abstract Introduction Traumatic brain injuries (TBIs) occur due to severe head assault to a hard object, with headache and vomiting being amongst the most common presenting symptoms. Metoclopramide is an old antiemetic agent that has been used widely for nausea and vomiting in TBI patients. Aim A systematic review of the literature to investigate the safety of metoclopramide in treating TBI patients. Methods A literature review was conducted in six databases, where we determined the pertinence of a study to the inclusion criteria by assessing the title, keywords, and abstracts. Five studies were found to be relevant. Data were extracted using multiple variables that were formulated incongruent with the study aim and then further analyzed. Results The collective sample size was 93 patients with an average of age 38.5 years. As much as 51.6% were male and 48.6% were females. Most patients received 10 mg metoclopramide IV with a percentage of 77.4%, while only 22.5% received 20 mg IV metoclopramide. Seventy-one patients received metoclopramide alone and 22 received combination therapy. Headache was the most common reported side effect (46.2%), followed by anxiety and drowsiness with (39.7%) and (27.9%), respectively. Fatigue was reported in 24.7%, while dystonia was the least common and developed in only 5.3% of patients. Conclusion Metoclopramide is a common medication used to treat TBI patients in the emergency department. However, the review demonstrated that the central nervous system (CNS) side effect is excepted. Treatments with lower CNS side effects may be better options.


Biomolecules ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 1134 ◽  
Author(s):  
Tetsuro Kikuchi

Memantine, an N-methyl-d-aspartate (NMDA) receptor antagonist approved for treating Alzheimer’s disease, has a good safety profile and is increasingly being studied for possible use in a variety of non-dementia psychiatric disorders. There is an abundance of basic and clinical data that support the hypothesis that NMDA receptor hypofunction contributes to the pathophysiology of schizophrenia. However, there are numerous randomized, double-blind, placebo-controlled clinical trials showing that add-on treatment with memantine improves negative and cognitive symptoms, particularly the negative symptoms of schizophrenia, indicating that memantine as adjunctive therapy in schizophrenia helps to ameliorate negative symptoms and cognitive deficits. It remains unclear why memantine does not show undesirable central nervous system (CNS) side effects in humans unlike other NMDA receptor antagonists, such as phencyclidine and ketamine. However, the answer could lie in the fact that it would appear that memantine works as a low-affinity, fast off-rate, voltage-dependent, and uncompetitive antagonist with preferential inhibition of extrasynaptic receptors. It is reasonable to assume that the effects of memantine as adjunctive therapy on negative symptoms and cognitive deficits in schizophrenia may derive primarily, if not totally, from its NMDA receptor antagonist activity at NMDA receptors including extrasynaptic receptors in the CNS.


Author(s):  
Saganuwan A. Saganuwan

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.


Author(s):  
Andrea G. Hohmann

The landmark paper discussed in this chapter, published by Calignano et al. in 1998, focuses on the control of pain initiation by endogenous cannabinoids. In the paper, analgesic lipid mediators are shown to be present in peripheral paw tissue where they control the ability of pain signals to ascend to the central nervous system (CNS). Anandamide acts through a peripheral mechanism to suppress inflammatory pain via cannabinoid type 1 receptors. Palmitoylethanolamine, subsequently identified as an endogenous ligand for peroxisome proliferator-activated receptor-α‎, produces peripheral antinociceptive effects via a mechanism similar to that for the cannabinoid type 2 receptor. These lipids do not serve redundant functions and, in combination, produce synergistic antinociceptive effects. These observations suggested that drug-development efforts targeting peripheral control of pain may elucidate improved pharmacotherapies that lack the unwanted CNS side effects of current treatments.


2018 ◽  
Vol 9 (1) ◽  
pp. 10-17 ◽  
Author(s):  
Thomas W. Hale ◽  
Kathleen Kendall-Tackett ◽  
Zhen Cong

Introduction: Metoclopramide and domperidone are medications that block dopamine receptors on the lactotrophs, allowing prolactin levels to rise. Both medications are prescribed to boost milk production in mothers with low milk production due to hypoprolactinemia. The Food and Drug Administration has not approved the use of domperidone in the U.S. because of concerns about increased risk of cardiac arrhythmias. Metoclopramide is often recommended instead. Unfortunately, metoclopramide affects the central nervous system (CNS) and increases the risk of both depression and tardive dyskinesia (TD).Method: The present study is an online survey of self-reported side effects of 1,990 mothers, representing 25 countries, who took metoclopramide, domperidone, or both medications to enhance milk production. Data were collected in 2010.Results: The results indicated that side effects, in general, affected only a small percentage of women who took either medication. Women were 3.6 times more likely to report no side effects when taking domperidone vs. metoclopramide. There were no significant differences in cardiac arrhythmias for women who took metoclopramide versus domperidone. Racing heart was more common with metoclopramide. Less than 1% reported these symptoms in both groups. However, CNS effects were significantly more common in women who took metoclopramide. Risk of depression increased by seven times, and symptoms of TD (tremors, involuntary grimaces, and jerking) increased by 4 to 19 times when women took metoclopramide.Discussion: The results of the present study are preliminary, but suggest that cardiac arrhythmias are a rare side effect with both medications. The CNS side effects with metoclopramide are more concerning, particularly depression and TD. It is hoped that the recommendations regarding the relative safety of these medications will be re-examined in light of these findings.


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