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Prescriber's Guide_ Stahl's Ess - Stephen M. Stahl.docx
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Monitoring after starting an atypical antipsychotic

✽ BMI monthly for 3 months, than quarterly

✽ Consider monitoring fasting triglycerides monthly for several months in patients at high risk for metabolic complications and when initiating or switching antipsychotics

✽ Blood pressure, fasting plasma glucose, fasting lipids within 3 months and then annually, but earlier and more frequently for patients with diabetes or who have gained >5% of initial weight

• Treat or refer for treatment and consider switching to another atypical antipsychotic for patients who become overweight, obese, pre-diabetic, diabetic, hypertensive, or dyslipidemic while receiving an atypical antipsychotic

✽ Even in patients without known diabetes, be vigilant for the rare but life-threatening onset of diabetic ketoacidosis, which always requires immediate treatment, by monitoring for the rapid onset of polyuria, polydipsia, weight loss, nausea, vomiting, dehydration, rapid respiration, weakness and clouding of sensorium, even coma

• Patients with low white blood cell count (WBC) or history of drug-induced leucopenia/neutropenia should have complete blood count (CBC) monitored frequently during the first few months and asenapine should be discontinued at the first sign of decline in WBC in the absence of other causative factors

Asenapine: side effects How Drug Causes Side Effects

• By blocking alpha 1 adrenergic receptors, it can cause dizziness, sedation, and hypotension

• By blocking dopamine 2 receptors in the striatum, it can cause motor side effects

• By blocking dopamine 2 receptors in the pituitary, it can theoretically cause elevations in prolactin

• Mechanism of weight gain and increased incidence of diabetes and dyslipidemia with atypical antipsychotics is unknown

Notable Side Effects

✽ Sedation, dizziness

• Oral hypoesthesia

• Application site reactions: oral ulcers, blisters, peeling/sloughing, inflammation

✽ Extrapyramidal symptoms, akathisia

✽ May increase risk for diabetes and dyslipidemia

• Rare tardive dyskinesia (much reduced risk compared to conventional antipsychotics)

• Orthostatic hypotension

Life-Threatening or Dangerous Side Effects

• Type 1 hypersensitivity reactions (anaphylaxis, angioedema, low blood pressure, rapid heart rate, swollen tongue, difficulty breathing, wheezing, rash)

• Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, has been reported in patients taking atypical antipsychotics

• Increased risk of death and cerebrovascular events in elderly patients with dementia-related psychosis

• Rare neuroleptic malignant syndrome (much reduced risk compared to conventional antipsychotics)

• Rare seizures

Weight Gain

• Occurs in a significant minority

• May be less than for some antipsychotics, more than for others

Sedation

• Many experience and/or can be significant in amount

What to Do About Side Effects

• Wait

• Wait

• Wait

• Anticholinergics may reduce motor side effects when present

• Weight loss, exercise programs, and medical management for high BMIs, diabetes, dyslipidemia

• Switch to another atypical antipsychotic

Best Augmenting Agents for Side Effects

• Benztropine or trihexyphenidyl for motor side effects

• Many side effects cannot be improved with an augmenting agent

ASENAPINE: DOSING AND USE

Usual Dosage Range

• 10–20 mg/day in 2 divided doses for schizophrenia

• 10–20 mg/day in 2 divided doses for bipolar mania

Dosage Forms

• Sublingual tablet 5 mg, 10 mg

How to Dose

• Must be administered sublingually; patients may not eat or drink for 10 minutes following administration

• Schizophrenia: initial 10 mg/day in 2 divided doses; maximum dose generally 20 mg/day in 2 divided doses; limited experience with once daily administration

• Bipolar mania (monotherapy): initial 20 mg/day in 2 divided doses; can reduce dose to 10 mg/day in 2 divided doses if there are adverse effects

• Bipolar mania (adjunct): initial 10 mg/day in 2 divided doses; can increase to 20 mg/day in 2 divided doses

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