CLOZAPINE
Brand name: Clozaril, Fazaclo, Versacloz Mechanism of Action: Clozapine is a dibenzodiazepine
Generic name: Clozapine derivative. It has a weak dopamine receptor-blocking
activity at D1, D2, D3 and D5 but has high affinity to
D4. It also possesses α-adrenergic blocking,
antimuscarinic, antihistaminic, antiserotonergic and
sedative properties.
General action: Second generation antipsychotic Side effects:
(SGA) or atypical antipsychotic Low blood pressure (hypotension)
Fast heart rate
Fever, sedation, seizures (with high doses)
Appetite increased
Constipation
Heartburn
Nausea
Increased hunger
Excess salivation/drooling (especially at night)
Vomiting
Weight gain
Sleep problems
Increased sweating
Dry mouth
Blurred vision
Drowsiness
Spinning sensation
Headache
Drug to Drug Interactions: Enhances the CNS Time best given: Clozapine is usually taken 2 times a
effects of narcotics, antihistamines and day. However, if your total daily dose is 200 mg or less,
benzodiazepines. May reduce therapeutic effect of you may be able to take the whole amount in a single
norepinephrine. Increased plasma level with CYP1A2 dose, usually in the evening. Try to take your clozapine
inhibitors (e.g. ciprofloxacin, fluvoxamine, enoxacin, dose at the same times each day. You can take clozapine
oral contraceptives, caffeine). Decreased plasma level with or without food
with CYP1A2 inducers. Increased risk of neuroleptic
malignant syndrome with lithium. Risk of seizures
with valproic acid.
RISPERIDONE
Brand name: Risperdal Consta, Risperdal, Perseris, Mechanism of Action:
Rykindo Risperidone is a benzisoxazole atypical antipsychotic
Generic name: Risperidone and a selective monoaminergic antagonist that has high
affinity for serotoninergic 5-HT2, dopaminergic D2,
adrenergic (α1 and α2), and histaminergic H1 receptors.
It has no affinity for cholinergic receptors.
General action: Second generation antipsychotics Side effects:
Drowsiness
Insomnia
Agitation
Anxiety
Headache
Runny or stuffy nose
Fatigue
Parkinsonism
Restlessness
Increased appetite
Vomiting
Drooling
Urinary incontinence
Tremor
Bedwetting
Constipation
Indigestion
Nausea
Abdominal pain
Aggressive reaction
Facial swelling
QT prolongation
Dizziness
Extrapyramidal symptoms (EPS) (muscle
spasms, restlessness, muscle rigidity, slowness
of movement, tremor, and jerky movements)
Male breast enlargement in children
Rash
Fast heart rate
Lightheadedness or fainting
Slow heart rate
Palpitation
Chest pain
Agitation
Dizziness upon standing
Itching
Acne
Hyperprolactinemia
Sexual dysfunction
Dry mouth
Drug to Drug Interactions: Time best given:
May enhance effects of antihypertensives and CNS Once a day: this is usually in the evening. Twice a day:
depressants. Increased risk of QT prolongation with this should be once in the morning and once in the
antiarrhythmics (e.g. quinidine, disopyramide, evening. Ideally these times are 10–12 hours apart
procainamide, propafenone, amiodarone, sotalol),
TCAs (e.g. amitriptyline), tetracyclic antidepressants
(e.g. maprotiline), certain antihistamines, certain
antimalarials (e.g. quinine, mefloquine), other
antipsychotics, and with medicines causing electrolyte
imbalance (hypokalaemia, hypomagnesaemia) or
bradycardia. May antagonise the actions of levodopa
and other dopamine agonists. Plasma concentrations of
the active antipsychotic fraction (risperidone plus 9-
hydroxyrisperidone) may be decreased with
carbamazepine and other CYP3A4 enzyme inducers
(e.g. rifampicin, phenytoin, phenobarbital). Increased
bioavailability with cimetidine, ranitidine. Increased
plasma concentration with strong CYP2D6 inhibitors
(e.g. fluoxetine, paroxetine), phenothiazines,
verapamil; increased plasma concentrations of active
antipsychotic fraction with strong CYP3A4 inhibitors
(e.g. itraconazole). Concomitant use with
psychostimulants (e.g. methylphenidate) may lead to
extrapyramidal symptoms when adjusting one or both
drugs.
