Zyprexa Zydis 5mg Tab 28’s Potential Overview:

• Brand Name: Zyprexa Zydis
• Generic Name: Olanzapine
• Quantity: 28 tablets per pack
• Size: 5 mg per tablet

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Zyprexa Zydis 5 mg is an orally disintegrating formulation of olanzapine, an atypical antipsychotic used to treat schizophrenia and bipolar disorder. It works by regulating neurotransmitters in the brain, particularly dopamine and serotonin, to improve mood and reduce psychotic symptoms.

Mechanism of Action (MOA):

• Olanzapine is an atypical antipsychotic that modulates dopamine (D2) and serotonin (5-HT2) receptors, as well as other receptors like histamine and adrenergic receptors. This helps in reducing psychotic symptoms (e.g., delusions, hallucinations) and stabilizing mood in disorders like schizophrenia and bipolar disorder.

Indications:

1. Schizophrenia:
   • For the acute and maintenance treatment of schizophrenia, reducing both positive (e.g., hallucinations, delusions) and negative symptoms (e.g., social withdrawal).
2. Bipolar Disorder:
   • Used in acute manic episodes and for maintenance treatment of bipolar disorder, particularly in stabilizing mood swings.

Dosage:

• Schizophrenia:
  • Initial dose: 5 mg to 10 mg once daily.
  • Maintenance dose: Typically between 10 mg to 20 mg daily, based on response.
• Bipolar Disorder (Acute Mania):
  • Initial dose: 5 mg to 10 mg once daily.
  • Maintenance dose: Can be adjusted to 5 mg to 20 mg depending on clinical response.
• Geriatric Patients:
  • Typically start with lower doses (e.g., 5 mg), especially for elderly patients with lower tolerability or higher risk for side effects.

Side Effects:

• Common side effects:
  • Sedation, weight gain, dry mouth, increased appetite, and dizziness.
• Serious side effects (less common):
  • Neuroleptic Malignant Syndrome (NMS), tardive dyskinesia, severe metabolic changes (e.g., hyperglycemia, dyslipidemia), and orthostatic hypotension.

Precautions:

1. Metabolic monitoring:
   • Regular monitoring of blood glucose, weight, and lipid profiles is important due to potential side effects such as weight gain, hyperglycemia, and dyslipidemia.
2. Elderly patients:
   • Increased sensitivity in older adults, especially those with dementia-related psychosis, which increases the risk of stroke and mortality.
3. CNS Depressants:
   • Caution with other CNS depressants (e.g., alcohol, sedatives), as olanzapine may add to the sedative effects.
4. Hepatic Impairment:
   • Dose adjustments may be necessary in patients with liver disease.

Contraindications (CI):

1. Hypersensitivity:
   • Contraindicated in individuals with a known allergy or hypersensitivity to olanzapine or any of its components.
2. Comatose States:
   • Contraindicated in patients who are in a coma or severe CNS depression.
3. Severe Hepatic Impairment:
   • Olanzapine should be avoided in patients with severe liver impairment due to altered metabolism.

Pharmacist Related Data

Chemical Formula:

Olanzapine

• Chemical Formula: C17H20N4S

Half-Life:

• Half-life of olanzapine is typically between 21 to 54 hours.
• This half-life may vary depending on the individual’s age, liver function, and other factors like smoking or other drug interactions.

Metabolism:

• Olanzapine is primarily metabolized in the liver via the cytochrome P450 (CYP) enzyme system, predominantly CYP1A2 and to a lesser extent CYP2D6.
• After metabolism, olanzapine is converted into inactive metabolites, mainly the 7-hydroxymethyl olanzapine metabolite.
• The drug undergoes extensive hepatic metabolism and has minimal renal excretion as the unchanged drug.

Drug Interactions:

1. With Medications:
   • CNS Depressants (e.g., alcohol, benzodiazepines): Combining olanzapine with other CNS depressants may enhance sedation and respiratory depression. Caution is advised.
   • CYP1A2 Inhibitors (e.g., fluvoxamine, ciprofloxacin): These can increase olanzapine levels by inhibiting its metabolism, leading to a higher risk of side effects.
   • CYP1A2 Inducers (e.g., carbamazepine, rifampin, smoking): These may reduce olanzapine levels, potentially making the drug less effective.
   • Antihypertensive Medications: Olanzapine may have additive effects when taken with antihypertensive drugs, increasing the risk of hypotension (low blood pressure).
2. With Food:
   • Food does not significantly alter the absorption of olanzapine, and it can be taken with or without food.
   • The Zydis formulation (orally disintegrating tablet) allows the medication to dissolve without needing water, making it easier to take for those who have difficulty swallowing tablets.

Pharmacodynamics:

• Mechanism of Action (MOA):
  • Olanzapine is an atypical antipsychotic that works by modulating dopamine (D2) and serotonin (5-HT2) receptors, as well as affecting histamine, adrenergic, and muscarinic receptors in the brain.
  • Olanzapine is thought to help balance the levels of these neurotransmitters, which in turn reduces symptoms such as hallucinations, delusions, and disorganized thinking in schizophrenia and bipolar disorder.
  • Additionally, it helps stabilize mood and reduce manic episodes in bipolar disorder.
• Therapeutic Effects:
  • Reduces positive symptoms of schizophrenia (e.g., hallucinations, delusions).
  • Improves negative symptoms of schizophrenia (e.g., emotional withdrawal, lack of motivation).
  • Mania stabilization in bipolar disorder, reducing symptoms such as irritability, impulsivity, and agitation.

Pharmacokinetics:

1. Absorption:
   • Olanzapine is well absorbed after oral administration, with oral bioavailability of approximately 60% to 80%.
   • The Zydis (orally disintegrating) form allows for fast absorption without the need for water.
   • Peak plasma concentration is reached within 5-8 hours after administration.
2. Distribution:
   • Olanzapine is extensively distributed in the body, including the central nervous system (CNS), and has a large volume of distribution (Vd).
   • It is approximately 93% bound to plasma proteins, mainly to albumin.
3. Metabolism:
   • Olanzapine undergoes extensive metabolism in the liver, mainly by CYP1A2, with a minor contribution from CYP2D6.
   • The major metabolite is 7-hydroxymethyl olanzapine, which is inactive. It has a small contribution to olanzapine’s overall activity.
4. Excretion:
   • Olanzapine and its metabolites are mainly excreted in urine (about 57%), with the remainder being eliminated through the feces (about 30%).
   • The half-life of olanzapine is about 21 to 54 hours and is prolonged in the elderly and those with liver dysfunction.