| Asenapine Pharmacology |
| Asenapine |
| About Asenapine |
| Atypical antipsychotic |
| Mechanism of Action of Asenapine |
| The mechanism of action of asenapine, as with other drugs having efficacy in schizophrenia and bipolar disorder, is unknown. It has been suggested that the efficacy of asenapine in schizophrenia is mediated through a combination of antagonist activity at D2 and 5-HT2A receptors. |
| Pharmacokinets of Asenapine |
| Absorption: Rapidly absorbed, Food or water may decrease asenapine exposure. Distribution:Widely distributed, 95% bound to plasma proteins. Metabolism:Hepatic Elimination:Elimination is 50% in urine and 40% in feces |
| Onset of Action for Asenapine |
| N/A |
| Duration of Action for Asenapine |
| N/A |
| Half Life of Asenapine |
| N/A |
| Side Effects of Asenapine |
| 1.Brain disorder 2.Movement disorder 3.Weight increased 4.Drowsiness 5.Constipation 6.Dry mouth 7.Increased saliva 8.Stomach discomfort 9.Vomiting 10.Fatigue 11.Irritability 12.Increased appetite 13.Weakness 14.Dizziness 15.Sleeplessness 16.High blood pressure |
| Contra-indications of Asenapine |
| 1.Hypersensitivity 2.Severe liver problems 3.Heart diseases 4.Who are taking antiarrhythmic, antipsychotic, phenothiazine, quinolone drugs |
| Special Precautions while taking Asenapine |
| 1.Caution should be exercised in patients with history of high blood pressure, cancer, Alzheimer disease, dementia, Parkinson disease, or esophagus problems, low blood volume, alcoholism, heart, liver, and kidney diseases 2.Do not drive a car or operate machinery and get up slowly from bed while taking this medication. 3.Avoid alcohol consumption. 4.Avoid abrupt withdrawal; withdraw gradually. 5.Patient may develop with increased risk of neuroleptic malignant syndrome (NMS) with the following symptoms: fever; stiff muscles; confusion; abnormal thinking; fast or irregular heartbeat; and sweating. 6.Avoid contact with people who have infections. 7.Drink adequate fluid; otherwise it may lead to dehydration. |
| Pregnancy Related Information |
| Contraindicated |
| Old Age Related Information |
| Use with caution;Dose may be reduced |
| Breast Feeding Related Information |
| Contraindicated |
| Children Related Information |
| Not recommended |
| Indications for Asenapine |
| 1.Bipolar Mania Adjunctive Therapy 2.Schizophrenia |
| Interactions for Asenapine |
| 1.Alcohol, CNS agents :Coadministration may enhance CNS depression. Avoid concurrent use with alcohol. 2.QT interval prolonging medications:Antiarrhythmics-class IA,class III,antibiotics (eg, gatifloxacin, moxifloxacin); antipsychotics (eg, chlorpromazine, thioridazine, ziprasidone):Additive effects on QT interval prolongation may increase the risk of life-threatening arrhythmias, including torsades de pointes. Avoid this combination. 3.Antihypertensive agents:Because of alpha-1 adrenergic antagonism by asenapine, the effect of certain antihypertensive agents may be enhanced. Monitor BP and adjust the dose of the antihypertensive agent as needed. 4.Dextromethorphan :Plasma concentrations of dextromethorphan may be decreased. Use with caution. 5.Fluvoxamine, imipramine :Asenapine plasma concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions. Use with caution. 6.Paroxetine :Asenapine plasma concentrations may be decreased, while paroxetine plasma concentrations may be increased. Use with caution. |
| Typical Dosage for Asenapine |
| Bipolar Mania Adjunctive Therapy Adults:5 mg twice daily initially in combination with lithium or valproate. Increase to 10 mg twice daily depending on the clinical response and tolerability. Bipolar Mania Monotherapy: Adults:10 mg twice daily initially. Dosage may be decreased to 5 mg twice daily if there are adverse effects. Schizophrenia: Adults:5 mg twice daily. Increase up to 10 mg twice daily after 1 wk based on tolerability. |
| Schedule of Asenapine |
| N/A |
| Storage Requirements for Asenapine |
| Store between 59? and 86?F. Do not remove the tablet from packaging until ready to administer. |
| Effects of Missed Dosage of Asenapine |
| Take it as soon as remember. If it is near the time of the next dose, skip the missed dose and resume usual dosing schedule. Do not double the dose to catch up. |
| Effects of Overdose of Asenapine |
| Symptoms: severe drowsiness/deep sleep, agitation, confusion, fainting. Treatment: No specific antidote,give supportive care to the patient. |