Product Description
Clozapine is an antipsychotic medication that is used to treat severe schizophrenia symptoms in peoplewho have not responded to other medications.
Clozapine belongs to a group of medicines called antipsychotics. These medicines work on the balanceof chemical substances in the brain which may cause mental illness.
Clozapine is prescribed in particular for people with schizophrenia. It is also known as a secondgeneration antipsychotic (SGA) or atypical antipsychotic. Clozapine rebalances dopamine and serotoninto improve thinking, mood, and behavior.
Schizophrenia is a mental health problem that causes disordered ideas, beliefs and experiences. Someonewith schizophrenia may have difficulty distinguishing between what is real and what is imaginary; maybe unresponsive or withdrawn; and may have difficulty expressing normal emotions in social situations.
Symptoms of schizophrenia include:
- Hallucinations - imagined voices or images that seem real
- Delusions - beliefs that are not true (e.g., other people are reading your thoughts)
- Disorganized thinking or trouble organizi
- Trouble speaking clearly
- Lack of motivation
Clozapine may help some or all of these symptoms.
Therapeutic Indication:
- For Schizophrenia
- Psychosis in people with Parkinson's disease
Uses:
- Helps reduce the risk of suicidal behavior in people with schizophreniaor similar disorders
- Sometimes used for people who have behavior problems
- Helps you feel calm and relaxed
- Controls your temper
Pharmacology:Mechanism of Action:Clozapine has been shown to be an antipsychotic agent that is different from classic antipsychotics. Inpharmacological experiments, it does not induce catalepsy or inhibit apomorphine- oramphetamine-induced stereotyped behaviour. It has only weak dopamine receptor-blocking activity atD
1, D
2, D
3 and D
5 receptors, but shows high potency for the D
4 receptor, in addition to potent anti-alpha-adrenergic, anticholinergic, antihistaminic, and arousal reaction-inhibiting effects. It has also beenshown to possess antiserotoninergic properties.
Pharmacodynamic:Clinically Clozapine produces rapid and marked sedation, and exerts antipsychotic effects in patients withschizophrenia resistant to other antipsychotic agents. In such cases, Clozapine has proven effective inrelieving both positive and negative schizophrenic symptoms in short- and long-term trials.
Clozapine is unique in that it produces virtually no major extrapyramidal reactions such as acute dystoniaand tardive dyskinesia. Furthermore, parkinsonian-like side effects and akathisia are rare. In contrast toclassical antipsychotics, clozapine produces little or no prolactin elevation, thus avoiding adverse effectssuch as gynaecomastia, amenorrhoea, galactorrhoea, and impotence.
Pharmacokinetics:Absorption:The absorption of orally administered clozapine is 90% to 95%; neither the rate nor theextent of absorption is influenced by food. Clozapine is subject to moderate first-pass metabolism,resulting in an absolute bioavailability of 50% to 60%.
Distribution: In steady-state conditions, when given twice daily, peak blood levels occur on an average at2.1 hours (range: 0.4 to 4.2 hours), and the volume of distribution is 1.6 L/kg. Clozapine is approximately95% bound to plasma proteins.
Metabolism: Clozapine is almost completely metabolised before excretion. Of the main metabolites onlythe desmethyl metabolite was found to be active. Its pharmacological actions resemble those of clozapine,but are considerably weaker and of short duration.
Excretion:Its elimination is biphasic, with a mean terminal half-life of 12 hours (range: 6 to 26 hours).After single dose of 75 mg the mean terminal half-life was 7.9 hours; it increased to 14.2 hours whensteady-state conditions were reached by administering daily doses of 75 mg for at least 7 days. Only traceamounts of unchanged drug are detected in the urine and faeces, approximately 50% of the administereddose being excreted as metabolites in the urine and 30% in the faeces.
Pregnancy and Lactation:Please consult the doctor before taking this medicine.
Contraindications:Clozapine is contraindicated in patients with a previous hypersensitivity to clozapine or any othercomponent of this drug, in patients with myeloproliferative disorders, uncontrolled epilepsy, paralyticileus, or a history of clozapine-induced agranulocytosis or severe granulocytopenia.
Warning & Precaution: This has been prescribed for the patient's specific condition only.
Side Effects:The most commonly reported side effects when taking Tamsulosin include: dizziness, headache, abnormal ejaculation, asthenia (weakness), and palpitations.
Storage:Store protected from light and moisture.