Clozapine - 3 Flashcards by Arteen Ahmed

what class is clozapine classfied in ?

tricyclic benzodiazepine drivatives

How well did you know this?

Not at all

Perfectly

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

How well did you know this?

Not at all

Perfectly

unique thing about clozpane mechanism compared to other antipsychotics?

high affinity at D4
weak at D2
More active at limbic
less active at striatal

How well did you know this?

Not at all

Perfectly

why clozapine is thougt to be more EPSE safe?

weak at D2

How well did you know this?

Not at all

Perfectly

clozapine main metabolizer cyp?

cyp1a2

How well did you know this?

Not at all

Perfectly

what does smoking do to clozapine

reduce in blood (induce cyp1a2)

How well did you know this?

Not at all

Perfectly

what does coffeee do to clozapine?

increase in blood ( inhibit cyp1a2)

How well did you know this?

Not at all

Perfectly

is it absolute necessary to avoid coffee in clozapine therapy?

no, just don’t fluctuate the amount consumed

How well did you know this?

Not at all

Perfectly

drugs that increase clozapine level?

SEC
—-

SSRIs
Erythromycin
Caffeine

How well did you know this?

Not at all

Perfectly

drugs that decrease clozapine level?

PCT

Phenytoin
Carbamazepine
Tobacco

How well did you know this?

Not at all

Perfectly

main active clozapine metabolite

nor clozapine (n-desmethyl clozapine)
Clozapine N-Oxide

How well did you know this?

Not at all

Perfectly

side effects of clozapine (losing)

Nausea
Vomitting
Salivation

How well did you know this?

Not at all

Perfectly

side effects of clozapine (gaining)

constipation
weight gain
dyspepsia

How well did you know this?

Not at all

Perfectly

side effects of clozapine (sleepy)

Dizziness
Sedation
Insomnia

How well did you know this?

Not at all

Perfectly

rate of hypertention in clozapine therapy

1/100

How well did you know this?

Not at all

Perfectly

prevalence of hypersalivation in clozapine therapy?

31%

How well did you know this?

Not at all

Perfectly

risks of hypersalivations?

asphyxiation
pneumonia
embarrasing in society

How well did you know this?

Not at all

Perfectly

when is hypersalivation worse?

at evening

when is usually hypersalivation seen in clozapine therapy/

early in therapy

RCT based medication used in hypersalivation?

-amisulpride
-propantheline

medication used in hypersalivation commonly but no data?

hyoscine hydrobromide

what does sympathetic stimulation do to saliva

increase protein contain

what does parasympathetic stimulation do to saliva

increase the flow

hypothesis for hypersalivation due to clozpaine

reduced swallowing
a 2 adrenoceptor antagonist increases saliva
-M4 agonist

Adverse events associated with clozapine?

pancreatitis agranulocytosis myocarditis seizure severe orthost. hypotension mortality in the elderly and dementia cases colitis thrombocytopenia insulin resistant thromboembolism

prevalence of diabetes in clozapine

33%

which conditions BNF requries caution about in clozapine therapy?

Above 60 Prostatic hypertrophy Susceptible to angle closure glaucoma

is there any therapeutic window established for clozapine

What is generally accepted as the level required to trigger a therapeutic response in clozapine therapy?

0.35 mg/l

what level indicate caution in clozapine therapy?

above 0.5 mg/l

prevalence of clozapine induced myocarditis?

1/500

when do myocarditis happen in the course of clozapine therapy

80% in first 4 week 90% in first 8 weeks

what pathology suggests in post mortum analysis of clozapine-induced myocarditis?

Type 1 Ig E- mediated acute hypersensitivity reaction

findings of pathological analysis of clozapine induced myocarditis(CIM)?

infiltration of eosinophils and myocytes

will recurrent myocarditis happen in a subsequent restart of clozapine?

yes

features of myocarditis(CIM)?

Fever flu like chest pain dyspnoea palpitation tackycardia ECG changes (prolongation) Elevated oesinophils and cardiac enzymes

gold standard to Rx clozapine induced myocariditis (CIM)?

biopsy

biomarkers of CIM

Creatine Kinase Lactate dehydrogenase Aspartate aminotransferase Myoglobin Troponin

what troponin type is specifict to CIM?

Troponin I & T

mortality rate in CIM?

50%

contraindication for clozapine?

paralytic ileus Epilepsy (uncontrolled) Unable to undergo regular blood tests hx of agranulocytosis concomitant use of depot impaired bone marrow renal, cardiac or liver diseases

what are two completely atypical antipsychotics?

clozapine and possibly quetiapine