Introduction
Asenapine also called Saphris is a medical drug used in treating psychotic conditions such as bipolar disorder, schizophrenia, and maniac depression. It works by mainly altering the chemical actions in the brain. This second-generation antipsychotic medication acts as an antagonist at D2 receptors and 5HT2A. The drug was also approved by the Food and Drug Administration in 2009 as a medication for post-traumatic stress disorder among soldiers. Nonetheless, the full range of efficacy of Asenapine in bipolar disorder and schizophrenia is yet to be identified (Stoner, 2012). There is indication that Asenapine’s efficacy is reinforced by combining the antagonistic activities of 5-HT2A, and D2 receptors.
Background & History
Asenapine was developed in 2007 by Schering-Plough in collaboration with Organon International. The drug which is chemical in nature was generated by altering the chemical structure of the mianserin, which is an atypical antidepressant. Prior to its approval by the FDA as a treatment for psychotic conditions in 2009, the drug went through various stages of clinical trials which involved over 3000 people (Stoner, 2012). Nonetheless, the Food and Drug Administration has not approved the use of asenapine in treating behavioral problems among patients with dementia.
The approval of Asenapine was based on four crucial clinical trials to confirm its efficacy. In the first trial, a 5 mg of asenapine was compared with a placebo of 3mg risperidone sublingually twice daily in a randomized trial that took six weeks to be completed. The trial which was double-blind in nature involved 174 participants who were all suffering from schizophrenia. The basic measure for efficacy was the total score for both the negative and positive syndrome scale (NPASS). In this specific trial, Asenapine indicated a statistically higher level of efficacy from the second week consistently when compared with its placebo. Later, there were also short-term clinical trials where participants were mainly patients with bipolar disorder. The trial went on to affirm that asenapine was statistically more effective when compared to the placebo. However, currently, trials meant for head-to-head comparison of the asenapine medication with other atypical antipsychotics, and schizophrenia is yet to be completed (Ghandhi, and Balaraman, 2010). These could help in determining the efficacy level of other available antipsychotics medications.
Asenapine assignment help
Chemistry
Typically, Asenapine is an antagonist at different adrenergic receptors (α1A and α2), serotonergic (5HT2A to 7), and dopaminergic (D2, D3and D4).The antagonism present in α2adrenoceptors is perceived to improve the cognitive functioning, and negative symptoms associated with schizophrenia and bipolar disorder. It also needs to be considered that asenapine has the capability of blocking α2 receptors, thus raising its potential in providing the stated benefits to psychotic conditions. On the other hand, the antagonistic activity associated with α1 adrenoceptor is responsible for the orthostatic hypotension released by the drug (Salanti, Davis, 2013).
Asenapine has no effect at muscarinic receptors within the range of the standard therapeutic dosage. This means that the drug does not harbor a metabolic syndrome or any level of anticholinergic adverse impact as manifested in other atypical antipsychotics including clozapine and olanzapine. Asenapine is also antagonist at histamine H1 receptors which is responsible for causing sedation. Through its activity and effect on H1 receptors, and through various clinical trials, it has been adduced that the administration of the drug causes weight gain.
The drug’s chemical description is (-2-butenedioate (1:1), (3aRS,12bRS) 12b-tetrahydro-1Hdibenzo , -5Chloro-2-methyl-2,3,3a, [2,3:6,7], pyrrole (2Z)-2-butenedioate (1:1), oxepino[4,5-c]. On the other hand, the standard molecular formula for Asenapine is 17H16ClNO•C4H4O4 while its basic molecular weight is 401.84 (it has a free base of: 285.8) (McIntyre, 2010). Asenapines chemical structure is in figure 1: 1. Inactive ingredients include cherry flavor, mannitol, gelatin and suncralose
Figure 1:1 Asenapine’s chemical structure
Pharmacology
The Asenapine drug has an exceptionally high affinity for the 5-HT7, 5-HT6, 5-HT2C and 5-HT2A receptors as compared to other antipsychotics. Moreover, it also poses an exceedingly higher affinity for the H1 and α2 receptors. This gives asenapine the capability of causing a significant higher-level of improvements in regard to addressing the symptoms associated with psychotic conditions being addressed as compared to other current antipyschotics. Among such effects include stabilization of moods, and cognitive functioning, improvement of cognitive behavior, and positive mood maintenance among others (McIntyre, 2010).
Side Effects and Toxology
The use of asenapine is associated with various side effects. Among these include dry mouth, constipation, dizziness, drowsiness, insomnia, weight gain, and mouth tingling. Other problems include upset stomach, and restlessness. Furthermore, Saphris may also cause problems in the nervous/muscle system including but not limited to stiff muscles, tremor/shaking, uneasiness, problems in swallowing, feelings of anxiety and shuffling walk. What is more, this medication has also been attributed to causing cramping, severe muscle spasms, twisting of the neck, stiff muscles and crinkled face. Other toxicity information associated with the use of asenapine includes the possible occurrence of Neuroleptic malignant syndrome (NMS). This syndrome is potentially risk and requires the drug to be immediately discontinued in case it is identified. Furthermore, the patients being treated with antipsychotic agents such as asenapine have been reported to undergo an intensive symptomatic treatment (American Society of Health-System Pharmacists, 2012).
If the following side effects are manifested, the drug should be stopped and the services of a doctor sought immediately. These side effects include sudden weakness, problems in swallowing, uncontrolled shaking, and uncontrolled movements of the tongue, eyes or legs, and stiffness of the muscles. Patient and caregivers should also check on the reactions of their bodies to the drug and dosage administered. It is possible to identify the negative reactions at an early stage and take appropriate measures as required (Rossi, 2013). However, if no measure is taken in the case of the negative effects, then the consequences may be adverse.
Therapeutic Application
Asenapine is mostly administered in form of tablets which may be in 10 mg, 5mg or 2.5 mg packs. Since this is a sublingual tablet, the patients are normally advised to place it under their tongues and wait for it to dissolve on a gradual basis. In normal cases, the tablet dissolves in the saliva within a few minutes. Patients or caregivers are advised not to chew, crush, swallow or split the Asenapine tablets. In addition, it is advised that patients taking the drug should not drink or eat anything for 10 minutes after taking the drug. The commencement dose for Asenapine is 2.5 mg for two times a day. This should however be increased to 5mg after three days for a more effective results (Ghandhi, H., and Balaraman, 2010).
For patients suffering from Schizophrenia, the Asenapine dose is supposed to be the 5 mg tablet which is supposed to be administered twice per day. As evidenced from clinical trials, there are no added benefits if a 10 mg dose is administered instead of the 5mg. This means that the same dose has similar effects. However, there is a clear increase in specific adverse reactions. It is advised that if the patient is able to tolerate the 10mg tablet instead of the 5mg one, then the former dose need to be used after one week. There is no significant impact on safety which has been reported for doses that are beyond 10mg daily (Rossi, 2013).
Patients with Manic, bipolar or mixed episodes should also take the 5 mg or 10 mg two times a day as the starting dose. For pediatric patients within the age group of 10-17, the 5mg to 10mg dose need to be slightly adjusted according to individual tolerability and response to the medication. These groups of patients are known to be sensitive to dystonia if the recommended dose and the escalation schedule are not adhered to appropriately (Hay, Byers, and Sereno, 2015).
Conclusion
The efficacy of Asenapine in treating psychotic conditions has been proved not only by its extensive clinical trials but also the assessment by the United States, Food and Drug Administration Department. This department is responsible for evaluating the efficacy of new medical drugs on the market and ascertaining their safety. However, caregivers, health practitioners and patients need to be very careful on adhering to the required dosage, as well as in ensuring that patients who develop the negative reactions to the drug are managed accordingly.
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