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Intro B Pharmacology > Antipsychotic Drugs > Flashcards

Antipsychotic Drugs Flashcards

1
Q

Antipsychotic drugs are also called

A

Antischizophrenic drugs
Major tranquillisers
Neuroleptics

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2
Q

What are the features of antipsychotic drugs

A

Not curative.
Requires several weeks to control symptoms
90%of patients require a maintenance dose
There’s usually a relapse
70%of patients experience a relapse when the drug is stopped
There’s a level of tolerance and physical dependence

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3
Q

What is psychosis

A

Psychosis is simply a disconnection from reality

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4
Q

What is schizophrenia

A

A mental disorder characterized by psychosis

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5
Q

The prevalence of schizophrenia is equal in males and females T/F

A

True

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6
Q

The prognosis of schizophrenia is poor T/F

A

True

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7
Q

What receptor is mainly responsible for the action of antipsychotic drugs

A

D2 - inhibitory

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8
Q

The dopamine receptor selective for sulpiride is

A

D2 like Receptor

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9
Q

D1B receptor is ……..

A

D5 receptor

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10
Q

D2 receptors inhibit ……..

A

cAMP and
GIRK

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11
Q

GIRK keeps the neurons in the hyperpolarized state, its inhibition by D2-like receptors results in …….

A

It allows the neurons to remain depolarized making them unable to initiate another signal

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12
Q

D1 receptor is selective for ……

A

SCH2339

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13
Q

The dopaminergic Pathways include

A

Mesocortical pathway
Mesolimbic
Nigrostriatal
Tuberoinfudibular pathway

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14
Q

A loss of integrity of the dopaminergic Pathways manifests as …… in the respective pathways

A

Mesolimbic - positive symptoms
Mesocortical- negative symptoms
Nigrostriatal pathway- extrapyramidal symptoms
Tuberoinfudibular - hyperprolactinaemia

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15
Q

The 5 functions of dopamine and the system or Pathways involved

A

Motivation, reward, cognition-mesolimbic
Hyperfunction in schizophrenia

Mesocortical- emotions and cognition hypofunction I schizophrenia

Motor control- nigrostriatal pathway
Extrapyramidal side effects
Endocrine control -Tuberoinfidibular
Hyperprolactinemiain treatment

Emetic effects CTZ in medulla

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16
Q

The major neurotransmitters involved in the pathogenesis of schizophrenia is

A

Dopamine
Glutamate
Serotonin

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17
Q

Briefly describe the effects of drugs on schizophrenia

A

Drugs like amphetamine. Cocaine and levodopa which results in Increased release of dopamine or in the quantity aggravates the positive sympathetic associated with schizophrenia
D2 receptor agonist like Apomorphine and bromocriptine also produce behavioural abnormalities in animals

D2 receptor antagonist are then effective in controlling the positive features of schizophrenia

Some evidence show that there is variation in D4 receptor which might make it a potent receptor for antipsychotic drugs

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18
Q

Role of glutamate in schizophrenia

A

Reduced glutamate conc and densities have been reported in postmortem brains of schizophrenics

Glutamate NMDA receptor antagonists like ketamine and phencyclidine have been reported to produce thought disorders, Hallucinations in humans

19
Q

What is the role of serotonin in schizophrenia

A

Serotonin has a modulator effect on dopamine i.e it sort of counter the effect of dopamine..

Drugs like LSD with mixed agonist and antagonist effects have been found to produce behavioral abnormalities

Some antipsychotic drugs also work on serotonin receptors (antagonists)

20
Q

The MOA of typical antipsychotics include

A

D2 antagonism
Some work on D4 receptor toi

Serotonin blockade ( may improve negative symptom)
Histamine blockade( drowsiness)
Alpha adrenoceptor blockade( postural hypertension)

21
Q

Typical antipsychotics have a limited spectrum of efficacy, explain

A

They target the control of positive symptoms

22
Q

The atypical antipsychotics have

A

Significantly reduced side effect
Improved efficacy profile

23
Q

Group 1 phenothiazenes aka aliphatic anti psychotic are

A

Chlorpromazine
Promazine
Triflupromazine

24
Q

Group 2 phenothiazenes include aka piperidine size chain

A

Thioridazine
Mesoridazine

25
Q

Piperazine derivatives group 3 include

A

Prochlorperazine
Trifluperazine
Thioethylperazine
Butaperazine
Perpenazine
Fluphenazine
Acetophenazine
Carphenazine

26
Q

Substitution on ……. position alters the efficacy ( activity) of phenothiazenes

A

R2
Position 2

27
Q

Substitution at ………. alters potency and adverse effects

A

Nitrogen at position 10

28
Q

Phenothiazenes differ in their potency but not their efficacy T/F

A

True

29
Q

Phenothiazenes are antagonist at ..
……. receptors

A

D1
D2
Adrenergic alpha 1
Muscarinic
Serotonin receptor( less)

30
Q

Allantipsychotics work majorly at …….

A

D2
And sometimes D4 receptor

31
Q

The main side effects of phenothiazenes are

A

Extrapyramidal side effects
Akathisia( hours)
Dystonias( hours to days)
Parkinsonism ( weeks to months)
Rigidity, tremor, and loss of mobility
Tardive dyskinesia (months to years)

32
Q

Acute dystopia side effect in antipsychotic medication

A

MOA: dopamine receptor blockade
Treatment Diphenhydramine and beztropine

33
Q

Akathisia side effects of phenothiazenes

A

MOA: unknown. Extreme motor restlessness
Treatment: reduced dose
Switch to low-potency
Atypical antipsychotics
Propranolol
Benzodiazepine
Amantadine

Sometimes resistant to Anticholinergic antiparkinson agent

34
Q

Muscarinic receptor blockade result in

A

Dry mouth, blurred vision
Urinary retention in males with prostatism aggravation of glaucoma

35
Q

Phenothiazenes cardiac effect os

A

Depressed T Wave and prolonged Q-T interval.
It is reversible after discontinuing the drug

36
Q

The endocrine effect of phenothiazines are

A

Increase prolactin secretion produces lactation in fees and gynecomastia in males.

Menstruation and ovulation disturbances.

Decreased secretion of gonadotropin, growth hormone and ACTH

37
Q

Phenothiazenes causes humans to become poikilothermic by …..

A

Depression of temperature regulating and vasomotor mechanism

38
Q

Why are phenothiazenes used as pre-anesthetic agent

A

To facilitate hypothermia for certain types of surgery

39
Q

Alpha 1 adrenergic antagonism have ……. side effects

A

Orthostatic hypertension
Reflex tachycardia
Sexual dysfunction

40
Q

Antihistaminergic side effevt of phenothiazines are

A

Sedation
Confusion
Disturbed concentration
Weight gain

41
Q

Why can’t clozapine be discontinued abruptly

A

Exacerbation, worsening of pre existing tardiness dyskinesia.
Prominent involuntary lingual movement and somatic symptoms relapse

42
Q

Depot preparations are administered through …….. for an interval of ……

A

Deep IM
1-4 weeks

43
Q

Contraindications of depot preparations

A

Not to be used in children
Confusional state
Parkinsonism
Coma due to CNS depression
Intolerance to antipsychotic

44
Q

Depot preparations are available as

A

Oily injections of decanoate derivatives or incorporation into carbohydrate microspheres
Fluphenazine
Risperidone
Haloperidol
Flupenthixol
Zuclopenthixol

Intro B Pharmacology (38 decks)

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