3. Summary
• FDA (1998) approved first line SGA medication.
• From a class of Dibanzothiazepine antipsychotic
medication.
• Basically treat psychosis, schizophrenia, & manic
disorders.
• 100% bioavailability.
• Well-tolerated , less side effects.
• Only medication for bipolar depression as mono-
therapy.
• Have spectrum both on depression and psychotic
features, as like one stop solution.
4. SGA Medications are second generation antipsychotic drugs.
Used as remedies for behavioral disorders, make patient feel
calm & relax. Psychotic disease cause abnormal thinking and
perceptions. Like,
• People with psychoses lose touch with reality.
• People with schizophrenia illness have changes in behavior
and other symptoms, such as delusions and hallucinations.
That last longer than 6 months.
• Manic depression, causes periods of depression and periods
of abnormally elevated mood. During mania, an individual
behaves or feels abnormally energetic, happy, or irritable.
5. Neoquel (Quetiapine)
• Atypical antipsychotic drug.
• Serotonin –Dopamine Antagonists.
• Greater ability to alter 5-HT2A receptor
activity than interference with D2
receptor.
• Nor-quetiapine is the active metabolite
that give therapeutic actions, by acting
on Mesolimbic & Mesocortical areas of
brain.
• No life threatening adverse effects.
6. Mesolimbic & Mesocortical tracts with Mental
illness pathophysiology
• Mesolimbic tract, which is a set of cells involved with
regulating emotions, responsible for positive symptoms
• Mesocortical tract, which is a set of cells involved with
regulating thought, responsible for negative symptoms
7. Mode of Action
• Quetiapine highly antagonize the serotonin activity, mediated by two
serotonin receptors i.e. 5-HT1A and 5-HT2A receptors.
• It reversibly bind with dopamine D2 receptors with low affinity leading to
decreased psychotic symptoms, such as hallucinations and delusions.
• In addition, quetiapine also has an affinity for adrenergic and histamine
receptors and binds to alpha-1, adrenergic and histamine H1 receptors.
8. • Schizophrenia
• Bipolar manic 1 Disorder
• Bipolar depressive Disorder
Condition Immediate release Extended release
Schizophrenia
Day 1: 50 mg/day PO divided q12hr
Days 2-3: Dose increased daily in increments of
25-50 mg q8-12hr to 300-400 mg by day 4;
Dosage range: 150-750 mg/day
Day 1: 300 mg/day PO; subsequently, may be
increased by up to 300 mg/day at intervals ≥1 day
Maintenance (monotherapy): 400-800 mg/day
Patients who have discontinued therapy for >1
week should have their dose reinitiated
Bipolar Manic
Disorder I
Day 1: 100 mg/day PO divided q12hr
Day 2: 200 mg/day PO divided q12hr
Day 3: 300 mg/day PO divided q12hr
Day 4: 400 mg/day PO divided q12hr
Dosage range: 400-800 mg/day; not to exceed 800
mg/day
Day 1: 300 mg PO once daily
Day 2: 600 mg PO once daily
Maintenance (day 3 onward): 400-800
mg/day PO
Bipolar depressive
Disorder
Either immediate-release or extended-release tablets may be given; dosage titrated upward over 4
days. Day 1: 50 mg PO at bedtime. Day 2: 100 mg PO at bedtime. Day 3: 200 mg PO at bedtime
Maintenance (day 4 onward): 300 mg PO at bedtime
9. • Rapidly absorbed by oral route.
• 100% bioavailability.
• Hepatically metabolized by Cyp3A4.
• Half life: 6 hours (IR), 7hours (XR).
• Execrated mainly through urine, some
extant to feces also.
• Sedation
• Weight gain
• Hypotension
• Somnolence
Dose adjustment
required in
special case
12. CYP3A4 Inhibitors
Quetiapine is a CYP3A4
substrate, and CYP3A4 inhibitors
increase quetiapine plasma
concentrations
Enzyme Inducers
Enzyme inducers can produce
marked reductions in quetiapine
plasma concentrations that may
result in loss of quetiapine
efficacy.
Clozapine
Methadone
Drug interactions
Precautions & warnings
High Risk Populations:
1. Pediatrics (Dose adjustment required at
initial levels)
2. Adults (Dose adjustment required in
cardiac dysfunction case also monitor QTc
interval)
3. Pregnancy (fall in class C)
4. Lactating mothers (Not recommended as
excreted in milk)
• Not approved for the use in children less than
12 years
• Increase mortality rate in patients with
dementia.
• Increase risk of suicidal thoughts.
Positive symptoms: Feelings or behaviors that are usually not present,such as:
Believing that what other people are saying is not true (delusions)
Hearing, seeing, tasting, feeling, or smelling things that others do not experience (hallucinations)
Disorganized speech and behavior
Negative symptoms: A lack of feelings or behaviors that are usually present,such as:
Losing interest in everyday activities, like bathing, grooming, or getting dressed
Feeling out of touch with other people, family, or friends
Lack of feeling or emotion (apathy)
Having little emotion or inappropriate feelings in certain situations
Having less ability to experience pleasure
Mesolimbic tract, which is a set of axons involved with regulating emotions
Mesocortical tract, which is a set of axons involved with regulating thought
Inhibitors: aminodrone, deltazim, fluconazole, cyclosporine etc.
Inducers: carbamazepine & phenytoin.