User:Lena08041993/AsenapineExample
Clinical data | |
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Trade names | Saphris, Sycrest |
AHFS/Drugs.com | Monograph |
MedlinePlus | a610015 |
License data | |
Pregnancy category |
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Routes of administration | sublingual |
ATC code | |
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Asenapine, sold under the trade names Saphris and Sycrest, is an atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder.
It was chemically derived via altering the chemical structure of the tetracyclic (atypical) antidepressant, mianserin.[5]
Medical uses
Asenapine has been approved by the FDA for the acute treatment of adults with schizophrenia and acute treatment of manic or mixed episodes associated with bipolar I disorder with or without psychotic features in adults.[6] In Australia asenapine's approved (and also listed on the PBS) indications include the following:[7]
- Schizophrenia
- Treatment, for up to 6 months, of an episode of acute mania or mixed episodes associated with bipolar I disorder
- Maintenance treatment, as monotherapy, of bipolar I disorder
In the European Union and the UK asenapine is only licensed for use as a treatment for acute mania in bipolar I disorder.[3][4]
Absorbed readily if administered
Schizophrenia
In a 2013 study in a comparison of 15 antipsychotic drugs in effectivity in treating schizophrenic symptoms, asenapine demonstrated low-medium effectivity. Less effective than clozapine, slightly less effective than haloperidol, quetiapine, and aripiprazole, approximately as effective as ziprasidone and chlorpromazine, and slightly more effective than lurasidone.[9] It appears to be less efficacious than other antipsychotics in the treatment of schizophrenia,[10] although its all-cause discontinuation rate is moderate.[10]A 2015 systematic review examined the effects of asenapine for people with schizophrenia:
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There is some, albeit preliminary, evidence that asenapine provides an improvement in positive, negative, and depressive symptoms, whilst having few adverse effects. However, due to the low-quality and limited quantity of evidence, it remains difficult to recommend the use of asenapine for people with schizophrenia. There is need for large-scale, longer-term, better-designed and conducted randomized controlled trials investigating the clinical effects and safety of asenapine.[11] | ||||||||||||||||||||||||||||||||||||||||||||
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Acute mania
As for its efficacy in the treatment of acute mania, a recent meta-analysis showed that it produces comparatively small improvements in manic symptoms in patients with acute mania and mixed episodes than most other antipsychotic drugs (with the exception of
Adverse effects
Adverse effect incidence[1][2][3][4]
Note: The discussion below these lists provides some more context into the frequency and severity of these adverse effects.
Very common (>10% incidence) adverse effects include:
Common (1-10% incidence) adverse effects include:
- Weight gain
- Increased appetite
- Extrapyramidal side effects (EPS; such as dystonia, akathisia, dyskinesia, muscle rigidity, parkinsonism)
- Sedation
- Dizziness
- Dysgeusia
- Oral hypoaesthesia
- Increased alanine aminotransferase
- Fatigue
Uncommon (0.1-1% incidence) adverse effects include:
- Hyperglycaemia— elevated blood glucose (sugar)
- Syncope
- Seizure
- Dysarthria
- Sinus bradycardia
- Bundle branch block
- QTc interval prolongation (has a relatively low risk for causing QTc interval prolongation.[14][15])
- Sinus tachycardia
- Orthostatic hypotension
- Hypotension
- Swollen tongue
- Dysphagia (difficulty swallowing)
- Glossodynia
- Oral paraesthesia
Rare (0.01-0.1% incidence) adverse effects include:
- sweating, reduced consciousness, and sudden change in blood pressure and heart rate)
- Tardive dyskinesia
- Speech disturbance
- Rhabdomyolysis
- Angioedema
- Blood dyscrasias such as agranulocytosis, leukopenia and neutropenia
- Accommodation disorder[clarification needed]
- Pulmonary embolism
- Gynaecomastia
- Galactorrhoea
Unknown incidence adverse effects
- Allergic reaction
- Restless legs syndrome
- Nausea
- Oral mucosal lesions (ulcerations, blistering and inflammation)
- Salivary hypersecretion
- Hyperprolactinaemia
Asenapine seems to have a relatively low weight gain liability for an atypical antipsychotic (which are notorious for their metabolic side effects) and according to a recent meta-analysis it produces
Pharmacology
Asenapine shows high
Receptor | Affinity (pKi)[17] |
Affinity (Ki (nM))[6]
|
---|---|---|
5-HT1A | 8.6 (agonist) | 2.5 (agonist) |
5-HT1B | 8.4 | 4.0 |
5-HT2A | 10.2 | 0.06 |
5-HT2B | 9.8 | 0.16 |
5-HT2C | 10.5 | 0.03 |
5-HT5A | 8.8 | 1.6 |
5-HT6 | 9.5 | 0.25 |
5-HT7 | 9.9 | 0.13 |
α1-Adrenergic | 8.9 | 1.2 |
α2A-Adrenergic | 8.9 | 1.2 |
α2B-Adrenergic | 9.5 | 0.32 |
α2C-Adrenergic | 8.9 | 1.2 |
D1 |
8.9 | 1.4 |
D2 |
8.9 | 1.3 |
D3 |
9.4 | 0.42 |
D4 |
9.0 | 1.1 |
H1 |
9.0 | 1.0 |
H2 |
8.2 | 6.2 |
mACh | < 5 | 8,128 |
History
Its developed by
References
- ^ a b c d e f "PRODUCT INFORMATION SAPHRIS® (asenapine maleate)" (PDF). TGA eBusiness Services. Merck Sharp & Dohme (Australia) Pty Limited. 14 January 2013. Retrieved 23 October 2013.
- ^ a b c d e f "SAPHRIS (asenapine maleate) tablet [Organon Pharmaceuticals USA]". DailyMed. Organon Pharmaceuticals USA. March 2013. Retrieved 23 October 2013.
- ^ a b c d e f g "Sycrest 5mg and 10mg sublingual tablets - Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Lundbeck Limited. 18 April 2013. Retrieved 23 October 2013.
- ^ a b c d e f g "Product information 21/02/2013 Sycrest -EMEA/H/C/001177 -II/0012" (PDF). European Medicines Agency. N.V. Organon. 21 February 2013. Retrieved 23 October 2013.
- PMID 20642375.
- ^ a b "Saphris (asenapine) prescribing information" (PDF). Schering Corporation. 2009-08-01. Archived from the original (PDF) on 2009-11-22. Retrieved 2009-09-05.
- ISBN 978-0-9805790-9-3.
- PMID 22494521.
- S2CID 32085212.
- ^ S2CID 32085212.
- ^ PMID 26599405.
- S2CID 25512763.
- PMID 21689438.)
{{cite journal}}
: CS1 maint: unflagged free DOI (link - ^ Washington, Nicole B. (October 2012). "Which psychotropics carry the greatest risk of QTc prolongation?". Current Psychiatry. 11 (10): 36–39. Retrieved 14 April 2017.
- ISBN 978-0-470-97948-8.
- ^ http://cat.inist.fr/?aModele=afficheN&cpsidt=21237275
- ^ S2CID 206489515.
- ^ "Bipolar Disorder". Clinical Trials Update. Genetic Engineering & Biotechnology News. 2007-06-15. pp. 52, 55.
- ^ "Schering-Plough Announces Asenapine NDA Accepted for Filing by the U.S. FDA" (Press release). Schering-Plough. 2007-11-26. Retrieved 2008-12-29.[permanent dead link]