asenapine transdermal

Action and Spectrum

Actions and spectrum: 

asenapine is an atypical antipsychotic medication that exerts its actions through multiple mechanisms. It acts as an antagonist at various receptor sites in the brain, including dopamine D2 and D3 receptors, serotonin 5-HT1A and 5-HT2A receptors, and histamine H1 receptors. 

The spectrum of asenapine’s actions includes the treatment of schizophrenia and bipolar disorder. It reduces the symptoms associated with conditions, such as hallucinations, delusions, disorganized thinking, and mood disturbances. 

asenapine is thought to have a broad spectrum of action due to its ability to modulate multiple neurotransmitter systems in the brain. This allows it to target both positive and negative symptoms of schizophrenia, as well as stabilize mood in bipolar disorder. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Increased weight (4-6%) 

Akathisia (4%) 

Increased transaminases (1.6-3.1%) 

Diarrhea (1-3%) 

Dystonia (1-3%) 

URTI (1-3%) 

Hypertension (2%) 

Dry mouth (<2%) 

Myalgia (<2%) 

Headache (9%) 

Constipation (4-5%) 

Somnolence (3-4%) 

Dyspepsia (1-3%) 

increased Blood glucose (1-3%) 

Nasopharyngitis (1-3%) 

increased Creatine kinase (1.6-2.1%) 

Vomiting (<2%) 

Asthenia (<2%) 

Increased prolactin (1.3%)  

>10% 

Extrapyramidal symptoms (8-13%) 

Reactions at Application site (14-15%)  

<1% 

Temporary block of bundle-branch 

Swollen tongue 

Dysarthria 

Anemia 

Accommodation disorder 

Hyponatremia 

Thrombocytopenia 

Post marketing Reports 

Choking 

Black Box Warning

Black Box Warning:  

asenapine transdermal does not have any black box warning 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Known hypersensitivity: asenapine should not be used in patients with known hypersensitivity to the drug. 
• QT interval prolongation: asenapine should not be used in patients with known QT interval prolongation or in combination with other medications known to prolong the QT interval. 
• Recent myocardial infarction or unstable cardiovascular disease: asenapine is contraindicated in patients who have recently experienced a myocardial infarction or have unstable cardiovascular disease. 
• Concurrent use with strong CYP1A2 inhibitors: asenapine should not be used concurrently with strong CYP1A2 inhibitors (e.g., fluvoxamine) due to the potential for increased asenapine concentrations.

Caution: 

• Cardiovascular effects: asenapine may cause orthostatic hypotension (low blood pressure upon standing), tachycardia (rapid heartbeat), and bradycardia (slow heartbeat).  
• CNS depression: asenapine may cause sedation and impairment of cognitive and motor function.  
• Anticholinergic effects: asenapine may have anticholinergic effects such as dry mouth, constipation, urinary retention, and blurred vision.  
• Hyperglycemia and diabetes: asenapine may cause hyperglycemia (high blood sugar) and exacerbate pre-existing diabetes. 
• Dyslipidemia: asenapine may cause changes in lipid profile, including increases in triglycerides and total cholesterol. Lipid monitoring is advised, especially in patients with pre-existing dyslipidemia. 
• Neuroleptic malignant syndrome (NMS): As with other antipsychotic medications, asenapine carries a risk of NMS, a potentially life-threatening condition characterized by hyperthermia, muscle rigidity, autonomic instability, and altered mental status. Prompt medical attention should be sought if NMS symptoms occur.

Comorbidities: 

• Diabetes: asenapine may increase blood glucose levels and worsen glycemic control. Patients with pre-existing diabetes or those at risk for developing diabetes should be closely monitored while taking asenapine. 
• Seizure disorders: asenapine can lower the seizure threshold, potentially increasing the risk of seizures.  
• Neurological disorders: asenapine should be used under caution in patients with conditions that may have an increased risk of adverse neurological effects, such as Parkinson’s disease, dementia, or conditions predisposing to seizures. 
• Hepatic impairment: asenapine is metabolized in the liver, so patients with hepatic impairment may experience altered drug metabolism. Dose adjustments or careful monitoring may be necessary in these individuals. 
• Renal impairment: asenapine is eliminated via the kidneys, so patients with renal impairment may require dosage adjustments to ensure appropriate drug levels and minimize the risk of adverse effects. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

asenapine is an atypical antipsychotic medication that exerts its pharmacological effects through its interaction with various neurotransmitter receptors in the brain. It acts as an antagonist or partial agonist at different receptor sites, leading to its therapeutic effects. 

• Dopamine receptor antagonism: asenapine blocks dopamine receptors, particularly D2 and D3 receptors, in the brain. By antagonizing these receptors, asenapine helps to reduce the excessive dopamine activity associated with certain mental health conditions like schizophrenia and bipolar disorder. 
• Serotonin receptor antagonism: asenapine also blocks several serotonin receptors, including 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors. This antagonism contributes to the antipsychotic and mood-stabilizing effects of the medication. 

Pharmacodynamics: 

• Histamine receptor antagonism: Asenapine acts as an antagonist at histamine H1 receptors. This action may contribute to its sedative and antihistaminic effects, which can help alleviate symptoms such as agitation and insomnia. 
• Adrenergic receptor antagonism: asenapine has antagonistic effects on alpha-1 adrenergic receptors. This may lead to the side effects such as orthostatic hypotension and sedation. 
• Muscarinic receptor antagonism: asenapine also exhibits antagonistic effects on muscarinic acetylcholine receptors. This action may contribute to side effects such as dry mouth, constipation, and cognitive impairment. 

Pharmacokinetics: 

Absorption 

As a transdermal medication, asenapine is often applied topically. It can penetrate the skin and absorb into the deeper tissues. 

Distribution 

The tissues close to the application site contain asenapine transdermal in various concentrations. It has a moderate volume of distribution, indicating that it is distributed throughout the body tissues. 

Metabolism 

asenapine undergoes hepatic metabolism primarily by the enzymes cytochrome P450 (CYP) 1A2 and CYP2D6. The major metabolite of asenapine is an inactive compound called N-desmethyl asenapine. Other minor metabolites may also be formed. 

Elimination and excretion 

The renal pathway accounts for most asenapine transdermal and its metabolite elimination. The byproducts of metabolism are eliminated in the urine. 

Adminstartion

Administration: 

Before administering the asenapine transdermal, make sure the application area is tidy and dry. Avoid applying any creams, oils, or lotions to the region prior because these might prevent absorption. 

Apply the patch to the targeted area of skin after removing it from the packaging if you’re using a asenapine transdermal patch. Use the appropriate dosage of asenapine transdermal cream or gel on your fingertips. Apply the gel or cream to affected region evenly and gently, rubbing it in until it is absorbed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: asenapine transdermal 

Pronounced: (Uh-SEN-uh-peen)  

Why do we use asenapine transdermal? 

asenapine is an antipsychotic medication that is primarily used to treat schizophrenia and bipolar disorder. It is prescribed to manage symptoms such as hallucinations, delusions, disorganized thinking, and mood disturbances associated with these conditions. asenapine may also be used as an adjunctive treatment in major depressive disorder. 

• Schizophrenia: asenapine is used to treat schizophrenia in adolescents aged 13-17 years and adults. 
• Bipolar I Disorder: asenapine is used to treat acute manic or mixed episodes with bipolar I disorder in adults. 
• Adjunctive Treatment in Major Depressive Disorder: asenapine may be prescribed in combination with an antidepressant for major depressive disorder in adults.