Zukaria 5 Sublingual Tablet
Asenapine
5 mg
Incepta Pharmaceuticals Ltd.
| Pack size | 30's pack |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 30.00 AED |
Indications
Zukaria 5 Sublingual Tablet is used for:
Schizophrenia, Bipolar Disorder
Adult Dose
Sublingual
Schizophrenia
Adult: Initially, 5 mg bid, may increase to 10 mg bid after 1 week if tolerated.
Acute manic episodes of bipolar disorder, Acute mixed episodes of bipolar disorder
Adult:
As monotherapy: 10 mg PO bid initially; may be decreased to 5 mg PO bid on day 2 and subsequent days if warranted by adverse effects or individual tolerance (90% of patients typically remain on higher dose)
As adjunct to lithium or valproate: Initially, 5 mg bid, may increase to 10 mg bid depending on clinical response and tolerability.
Child Dose
Bipolar Disorder
Indicated as monotherapy for acute treatment of manic or mixed episodes associated with bipolar I disorder
<10 years: Safety and efficacy not established
10-17 years: 2.5 mg SL 12 hourly initially; may increase to 5 mg SL 12 hourly after 3 days and to 10 mg SL 12 hourly after 3 additional days
Renal Dose
Renal impairment
Dose adjustment is not necessary on the basis of a patient’s renal function (mild to severe renal impairment, glomerular filtration rate between 15 and 90 mL/minute).
Administration
Sublingual tablet; to allow optimal absorption, place under tongue and allow to dissolve completely (dissolves within seconds)
Do not chew, split, crush, or swallow sublingual tablet
Do not eat or drink for at least 10 minutes after administration
Contra Indications
Hypersensitivity to asenapine. Dementia-related psychosis. Severe (Child-Pugh Class C) hepatic impairment.
Precautions
Not indicated for dementia-related psychosis; increased risk of death in elderly patients with dementia-related psychosis; placebo-controlled trials with other atypical antipsychotics (ie, risperidone, aripiprazole, olanzapine) showed a higher incidence of cerebrovascular adverse reactions (eg, cerebrovascular accidents [CVAs], transient ischemic attacks [TIAs]), including fatalities, in comparison with placebo.
Cerebrovascular Adverse Reactions in Elderly Patients with Dementia-Related Psychosis: Increased incidence of cerebrovascular adverse reactions (e.g., stroke, transient ischemic attack).
Neuroleptic Malignant Syndrome: Manage with immediate discontinuation and close monitoring.
Tardive Dyskinesia: Discontinue if clinically appropriate.
Metabolic Changes: Monitor for hyperglycemia/diabetes mellitus, dyslipidemia, and weight gain.
Orthostatic Hypotension: Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope.
Leukopenia, Neutropenia, and Agranulocytosis: Perform complete blood counts (CBC) in patients with pre-existing low white blood cell count (WBC) or history of leukopenia or neutropenia. Consider discontinuing Asenapine if a clinically significant decline in WBC occurs in absence of other causative factors.
QT Prolongation: Increases in QT interval; avoid use with drugs that also increase the QT interval and in patients with risk factors for prolonged QT interval.
Seizures: Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold.
Potential for Cognitive and Motor Impairment: Use caution when operating machinery.
Monitoring Parameters
Monitor weight gain in pediatric patients and assess against that expected for normal growth.
Monitor blood pressure and adjust the dosage of the antihypertensive drug accordingly.
Orthostatic vital signs should be monitored in patients who are vulnerable to hypotension (elderly patients, patients with dehydration, hypovolemia, concomitant treatment with antihypertensive medications
Pregnancy-Lactation
Pregnancy category: C
Neonates exposed to antipsychotic drugs during 3rd trimester of pregnancy are at risk for EPS or withdrawal symptoms after delivery; these complications vary in severity, with some being self-limited and others requiring ICU unit support and prolonged hospitalization
Lactation: Excretion in milk unknown; use with caution
Interactions
Increased plasma concentration w/ fluvoxamine.
May increase exposure of paroxetine.
May antagonize the effects of levodopa and dopaminergic.
Antihypertensive Drugs: Asenapine may cause hypotension. May enhance the effects of certain antihypertensive agents (due to its α1-adrenergic antagonism) and CNS depressants.
Paroxetine (CYP2D6 substrate and inhibitor): Reduce paroxetine by half when used in combination with Asenapine.
Contraindicated (6)
amisulpride
dronedarone
fluconazole
posaconazole
thalidomide
thioridazine
Adverse Effects
Side effects of Asenapine :
>10%
Somnolence (24%)
Headache (12%)
Dizziness (11%)
Pediatric patients
Oral paraesthesia (27%)
Somnolence (49%)
1-10%
Extrapyramidal symptoms (EPS) other than akathisia (7%)
Insomnia (6%)
Weight gain (5%)
Akathisia (4%)
Anxiety (4%)
Fatigue (4%)
Oral hypoesthesia (4%)
Dyspepsia (4%)
Dry mouth (3%)
Dysgeusia (3%)
Arthralgia (3%)
Toothache (3%)
Depression (2%)
Extremity pain (2%)
Pediatric patients
Nausea (6%)
Abdominal pain (6%)
Fatigue (9%)
Increased weight (3%)
Hyperinsulinemia (2%)
Increased appetite (8%)
Headache (9%)
Dizziness (7%)
Dysgeusia (6%)
Akathisia (2%)
Insomnia (3%)
Suicidal ideation (3%)
Tachycardia (1%), Glossodynia (1%), Irritability (1%), Muscle pain (1%), Increased ALT (1%), Increased AST (1%), Dehydration (1%), Myalgia (1%), Parkinsonism (1%), Anger (1%), Dysmenorrhea (1%), Rash (1%), Nasal congestion (1%), Dyspnea (1%), Oropharyngeal pain (1%)
Potentially Fatal: Neuroleptic malignant syndrome (manifesting as hyperthermia, muscle rigidity, altered mental status, autonomic instability, elevated serum creatine phosphokinase levels, myoglobinuria, acute renal failure), agranulocytosis, hyperglycaemia (associated w/ ketoacidosis or hyperosmolar coma).
Mechanism of Action
Asenapine, a dibenzo-oxepino pyrrole derivative, is a 2nd generation or atypical antipsychotic w/ mixed antagonistic activity. It has a atyhigh affinity for serotonin (5-HT1A-B, 2A-C, 5-7), dopamine (D1-4), adrenergic (α1-2), and histamine (H1) receptors; and moderate affinity for H2 receptor.
Note
Zukaria 5 5 mg Sublingual Tablet manufactured by Incepta Pharmaceuticals Ltd.. Its generic name is Asenapine. Zukaria 5 is availble in Bangladesh.
Farmaco BD drug index information on Zukaria 5 Sublingual Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.