Paliperidone

2. PALIRIS XR
1.5mg, 3mg, 6mg(Paliperidone)
RPh Yousra Ashraf

3. Anti-psychotic Drug
FDAApproved
XR Medication
Formulated using osmotically released oral (OROS)
delivery system
Treat Schizophrenia & Schizoaffective Disorder
Good Safety Profile
Cost Effective

4. Schizophrenia
 Schizophrenia is a brain disorder that affects the
way a person behaves, thinks, and sees the world.
 People with schizophrenia often have an altered
perception of reality. They may see or hear things
that don’t exist, speak in strange or confusing
ways, believe that others are trying to harm them,
or feel like they’re being constantly watched.
 This can make it difficult to negotiate the activities
of daily life, and people with schizophrenia may
withdraw from the outside world or act out in
confusion and fear.

6. Schizoaffective Disorders
A condition in which a mood episode and the active phase symptoms of
schizophrenia occurs together and were proceed or are followed by 2
weeks of delusions & hallucinations without prominent mood
symptoms.

8. Although schizophrenia & schizoaffective
disorder are chronic conditions, but there
is help available. With support,
medication, and therapy, many people
with schizophrenia & schizoaffective
disorder are able to function independently
and fulfilling life goals.
Anatomic, neurotransmitter, and immune
system abnormalities have been founded
the causes of Schizophrenia &
Schizoaffective disorder.

9. PALIRIS XR
Paliperidone belongs to a class of drugs called atypical antipsychotics. It
works by helping to restore the balance of certain natural substances in the
brain. It is a dopamine antagonist and 5-HT2A antagonist.
Formulated using osmotically released oral (OROS) delivery system.
It is Resperidone’s active metabolite(9-hydroxy Resperidone).
Approved as quarterly therapy for patients with schizophrenia.
Don’t be afraid
of the world

10. Mode of action
Specific mechanism of action is unknown, but it has been proposed that the
drug's therapeutic activity in schizophrenia is mediated through a combination
of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor
antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2
adrenergic receptors and H1 histaminergic receptors, which may explain some
of the other effects of the drug.
Pelip

11. Comparison of side effects with other antipsychotics

12. Comparison of pharmacokinetic parameters of atypical
antipsychotics

13. Less side effects than resperidone like:

14. Dosage
Usual Adult Dose for Schizophrenia Usual Adult Dose for Schizoaffective Disorder
6 mg orally once a day
-Dose range: 3 to 12 mg per day; dose increases may
be made in increments of 3 mg per day and should
occur at intervals of more than 5 days.
-Maximum dose: 12 mg/day
6 mg orally once a day
-Dose range: 3 to 12 mg per day; dose increases may
be made in increments of 3 mg per day and should
occur at intervals of more than 4 days.
-Maximum dose: 12 mg/day
Usual Pediatric Dose for Schizophrenia Renal dose adjustments
12 to 17 years old:
-Initial dose: 3 mg orally once a day
-Dose range: 3 to 12 mg per day; dose increases may
be made in increments of 3 mg per day and should
occur at intervals of more than 5 days.
-Maximum dose: 12 mg/day
initial dose: 3 mg orally once a day; may increase to a
maximum of 6 mg orally once a day based on
efficacy and tolerability.
Pregnancy: class C

15. • Black box warning for the use with dementia
• Contraindicated in case of hypersensitivity with any of
ingredient present in formulation.
• QTc interval monitoring necessary.
• Not recommended for lactating women.

16. Advantages than Resperidone
• Due to favorable pharmacodynamics profile i.e. antagonism of 5HT2A,
α1and D2; it has improved positive and negative symptoms (reduction
in PANSS score), as compared with resperidone.
• Reduced extra pyramidal side effects.
• Paliperidone does not require oral supplementation during treatment
initiation, as its pharmacokinetic (PK) profile allows both a rapid
achievement of therapeutic plasma levels as well as a gradual and
continuous release of the drug over the dosing interval.