Clozapine - 3 Flashcards
what class is clozapine classfied in ?
tricyclic benzodiazepine drivatives
mechanism of clozpaine
—-antagonists at D1, D2, D3 and D4
—-antagonists at alpha adrenoceptors 1 and 2
—-antagonists at 5-HT2A
—-antagonists at muscarinic-receptor (M1, M2, M3, M5)
—agonist at M4
unique thing about clozpane mechanism compared to other antipsychotics?
high affinity at D4
weak at D2
More active at limbic
less active at striatal
why clozapine is thougt to be more EPSE safe?
weak at D2
clozapine main metabolizer cyp?
cyp1a2
what does smoking do to clozapine
reduce in blood (induce cyp1a2)
what does coffeee do to clozapine?
increase in blood ( inhibit cyp1a2)
is it absolute necessary to avoid coffee in clozapine therapy?
no, just don’t fluctuate the amount consumed
drugs that increase clozapine level?
SEC
SSRIs
Erythromycin
Caffeine
drugs that decrease clozapine level?
PCT
Phenytoin
Carbamazepine
Tobacco
main active clozapine metabolite
- nor clozapine (n-desmethyl clozapine)
- Clozapine N-Oxide
side effects of clozapine (loosing)
Nausea
Vomitting
Salivation
side effects of clozapine (gaining)
constipation
weight gain
dyspepsia
side effects of clozapine (sleepy)
Dizziness
Sedation
Insomnia
rate of hypertention in clozapine therapy
1/100
prevalence of hypersalivation in clozapine therapy?
31%
risks of hypersalivations?
asphyxiation
pneumonia
embarrasing in society