| Common Brands | Saphris |
|---|---|
|
Drug Class |
Atypical antipsychotic |
|
Controlled Substance Classification |
Not a controlled medication |
|
Generic Status |
Lower-cost generic available |
|
Availability |
Prescription only |
The transdermal delivery system of asenapine has been developed with the aim of skin based controlled release of the drug in the region.
The transdermal patch administers asenapine transdermally into the circulation gradually over a period allowing it to avoid the digestive tract and possible adverse effects thanks to the gastrointestinal system.
Even though this mode of delivery is still not incorporated in the practice of administration of asenapine, it could serve as an appropriate alternative for patients who needs a steady drug concentration or can’t use other routes of administration.
Although a transdermal patch version of asenapine is not currently approved by the FDA (as of my knowledge cutoff in 2023), the following guidelines can apply to how a transdermal patch would typically be used, based on other transdermal antipsychotic medications:
Duration of Wear:
A typical transdermal patch may be worn for 24 hours or up to several days, depending on the specific formulation. This allows for continuous release of the medication over time.
• Forgotten Dose: If you forget to replace (or put on) the patch and it is time for the next dose, you should consult your doctor and do as they say. Do not place additional patches on the skin to compensate for a dose that has been missed.
Asenapine (transdermal), like all its other forms, works by modulating dopaminergic and serotonergic activities in the brain. These neurotransmitters relate to emotional, perceptual, and cognitive processes, and their dysfunction is believed to be involved in disorders such as schizophrenia and bipolar disorder.
Asenapine, be it in the form of an oral dosage or applied as a transdermal patch, poses some risks of potential side effects which many are familiar with antipsychotic drugs. Some of these may include:
Drowsiness or sedation o Dizziness o Excessive weight gain o Dry mouth or unpleasant taste
Insomnia or Hypersomnia
Serious side effects:
Neuroleptic Malignant Syndrome (NMS) is a rare neurological disorder characterized by hyperthermia, rigidity, altered consciousness and autonomic instability (e.g. changes in blood pressure and heart rate).
Tardive dyskinesia is a disorder characterized by abnormal and involuntary movements, often stereotyped and affect the tongue or facial area; chronic administration of antipsychotic drugs may induce this condition.
For allergic responses, some patients may have rare but extreme reactions such as swelling, rash, or difficulty in breathing.
Despite the fact that the transdermal form of asenapine has much to offer, there are significant warnings and precautions worth consideration:
Skin Sensitivity – In the case of sensitive skin or adhesive allergies, the transdermal patch may not be appropriate. Transdermal patches are known to cause skin irritations as one of their side effects.
CYP1A2 Inhibitors (such as Ketoconazole, Clarithromycin):
Highly potent CYP1A2 inhibitors like ketoconazole (an antifungal agent) or clarithromycin (an antibiotic) can significantly increase the plasma levels of asenapine, potentially leading to excessive sedation or dizziness.
CYP1A2 Inducers (such as Rifampin, Carbamazepine):
Antibiotics like rifampin or anticonvulsants like carbamazepine may lead to decreased asenapine efficacy by elevating its rate of metabolism and, consequently, lowering its therapeutic effects.
CNS Depressants (such as Benzodiazepines, Opioids):
Asenapine increases the sedative effects when given with other CNS depressants such as benzodiazepines and opioids which may enhance the risk of excessive sedation, dizziness, and respiratory depression.
Antihypertensives
Asenapine causes orthostatic hypotension. In patients receiving antihypertensive medications (including ACE inhibitors, beta-blockers), the risk of blood pressure being too low may be increased.
Consult a health care provider regarding using asenapine with other drugs.
Currently, the transdermal patch formulation of asenapine is neither FDA-cleared nor present in commerce, hence the dosages of this formulation are still being researched. However, it is possible to extrapolate the future trends for transdermal forms by looking at the human administered oral asenapine dosages.
Initial Dosing: 5 mg b.i.d.
Maintenance Dosing: 5-10 mg b.i.d.
Initial Dosing: 10 mg b.i.d.
Maintenance Dosing: 5-10 mg b.i.d.
Asenapine in both oral and transdermal formulations is a controlled medication. It can be acquired only through a valid prescription written by an authorized physician. Considering asenapine for schizophrenia or bipolar disorder, the doctor shall assess the patient’s medical condition, history, and compatibility of other medicines before commencing the medication.
Asenapine is an atypical antipsychotic medication used to treat schizophrenia and bipolar disorder. The transdermal formulation allows it to be absorbed through the skin, providing an alternative to oral administration.
Asenapine works by modulating neurotransmitters in the brain, particularly dopamine and serotonin receptors. This helps in stabilizing mood and reducing psychotic symptoms.
The transdermal system allows for a steady release of medication over time, potentially improving compliance and minimizing fluctuations in drug levels compared to oral forms.
Asenapine transdermal patches are applied to clean, dry, and intact skin on the upper body or arm. They should be changed every 24 hours as prescribed.
Common side effects may include sedation, dizziness, weight gain, dry mouth, and gastrointestinal disturbances.
Asenapine is approved for use in children and adolescents aged 10 and older for bipolar disorder and schizophrenia, but the decision should be made by a healthcare professional.
The safety of Asenapine during pregnancy and breastfeeding is not well established, so it’s crucial to consult a healthcare provider for personalized guidance.
Yes, Asenapine can interact with other drugs, potentially affecting their absorption or efficacy, particularly those that influence the central nervous system.
Asenapine transdermal patches bypass gastrointestinal absorption, so food does not significantly impact its delivery; however, follow your doctor’s advice.
Patients may notice improvements in symptoms within days, but it can take several weeks to experience the full benefits of the medication.
If you miss a dose, apply the patch as soon as you remember. If it is almost time for your next dose, skip the missed dose and resume your regular schedule.
Signs of an allergic reaction may include rash, itching, swelling, dizziness, or trouble breathing. Seek medical attention immediately if these symptoms occur.
Discontinuing Asenapine suddenly can lead to withdrawal symptoms, including insomnia, agitation, or rebound psychosis. It’s important to taper off under medical supervision.
Store Asenapine patches at room temperature, away from moisture and heat, and keep them out of reach of children and pets.
Patients with liver problems should use Asenapine with caution, as liver impairment can affect the medication’s metabolism. Always consult a healthcare provider.
Asenapine may cause sedation and dizziness, impacting your ability to drive. It’s advisable to see how the medication affects you before operating vehicles.
If the Asenapine patch falls off, replace it with a new one immediately to maintain therapeutic levels, unless it’s close to the time for your next dose.
Yes, adopting healthy lifestyle changes, such as regular exercise, a balanced diet, and stress management, can support your treatment and overall well-being.
Regular follow-up appointments are important for monitoring the effectiveness and side effects of the medication. Usually, every few weeks for the first few months is recommended.
For more information, consult your healthcare provider, pharmacist, or reliable sources such as the FDA or medical literature.
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