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Pharmacology and Medical Chemistry I > Exam 2 ( Antipsychotics) > Flashcards

Exam 2 ( Antipsychotics) Flashcards

1
Q

A9 nigrostriatal DA neurons

A

originate in substantia nigra pars compacta dendrites extend into pars reticulata.

axons innervate corpus striatum

DA release in striatum essential for normal extrapyramidal motor function

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2
Q

A10 mesolimbic DA neurons

A

originate in midbrain ventral tegmental area (VTA)

axons innervate limbic portions of striatum (nucleus accumbens) and cortex

DA release from these neurons important for normal affect, orderly thinking, “drive” states, pleasure and reward

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3
Q

D1 vs D2 receptor

A

D1 = short 3rd intracellular loop, long carboxyl tail

D2 = long 3rd intracellular loop, short carboxyl tail

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4
Q

Epidemiology of schizophrenia

A

1st presents between ages 16 - 20 yr old

1-3% pop overall

genetic predisposition, genetic component probably affected by multiple genes

both neurochemical (nature) and environmental factors (nurture) likely to contribute to development of disease

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5
Q

Organic psychoses

A

cause is known, due to impaired cerebral tissue function; cognitive and intellectual decline

can be secondary to drug abuse, metabolic or toxic insult, trauma, infections, or structural disease of the nervous system

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6
Q

Dopamine theory of schizophrenia

A

cause is postulated to be excessive DA transmission, especially within the limbic striatum and limbic cortical areas innervated by A10 DA neurons (mesolimbic and mesocortical DA pathways)

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7
Q

Idiopathic psychoses

A

cause not known, may have a genetic component.

schizophrenia denotes a form of idiopathic psychosis

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8
Q

Positive symptoms

A

hallucinations, usually auditory (voices talking to patient) delusions (false beliefs), grandiosity, paranoia
disorganized thinking, speech; tangential thinking, “word salad” bizarre behavior, catatonia

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9
Q

Negative symptoms

A

affective (emotional) flattening withdrawal, depersonalization, asociality poverty of speech and thought anhedonia, loss of motivation

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10
Q

Cognitive symptoms

A

impaired attention, deficits in learning and memory

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11
Q

D2 like family

A

D2, D3, D4

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12
Q

D1 like family

A

D1 and D5

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13
Q

D1 receptors

A

lead to stimulation of adenylate cyclase and increase cAMP

Affinity for phenothiazines > butyrophenones

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14
Q

D2 receptor

A

not associated with stimulation of adenylate cyclase and may inhibit it.

Affinity for butyrophenones > phenothiazines

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15
Q

Typical

A

blockade at D2 receptors > 5-HT2A receptors; antipsychotic potency correlates strongly with D2 receptor blockade

Phenothiazine derivatives
Thioxanthene derivatives
Butyrophenone derivatives
Miscellaneous “typical” antipsychotic drugs

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16
Q

Atypical

A

blockade at 5-HT2A receptors > D2 receptors

Loxapine
Clozapine
Risperidone
Quetiapine
Olanzapine
Ziprasidone 
Aripiprazole
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17
Q

Manifestation:
Loss of accommodation, dry mouth, difficulty urinating,
constipation

A

Mechanism:
Muscarinic cholinoreceptor blockade

ANS

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18
Q

Manifestation:

Parkinson’s syndrome, akathisia, dystonias

A

Mechanism:
Dopamine-receptor blockade

CNS

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19
Q

Manifestation:

Tardive dyskinesia

A

Mechanism:
Supersensitivity of dopamine receptors

CNS

20
Q

Manifestation:

Orthostatic hypotension, impotence, failure to ejaculate

A

Mechanism:
α-Adrenoceptor blockade

ANS

21
Q

Manifestation:

Toxic-confusional state

A

Mechanism:
Muscarinic blockade

CNS

22
Q

Manifestation:

Amenorrhea-galactorrhea, infertility, impotence

A

Mechanism:
Dopamine-receptor blockade resilient in hyperprolactinemia

Endocrine System

23
Q

Manifestation:

Weight Gain

A

Mechanism:

Possibly combined H1 and 5-HT2 blockade

24
Q

Clozapine (dibenzodiazepine)

A

1st effective antipsychotic without extrapyramidal side-effects

may suppress tardive dyskinesia due to other agents

reduces positive and negative symptoms

blocks many receptors

most serious side effect: agranulocytosis

other side effects:
hypercholesterolemia, weight gain, diabetes

25
Q

Risperidone (Benzisoxazole)

A

D2 and 5-HT2 receptor blocking properties

no blood toxicity of clozapine

lower incidence of extrapyramidal side effects and tar dive dyskinesia than classical antipsychotics

not as effective in drug resistance cases as clozapine

26
Q

Olanzapine (Thienobenzodiazepine)

A

effective treating both positive and negative symptoms

low incidence of extrapyramidal effects

main side-effects = weight gain and associated with metabolic disorders…diabetes, hypertension, hyperlipidemia

27
Q

Quetiapine (Dibenzothiazepine)

A

one of most widely used

D2> 5-HT2a
low incidence of extrapyramidal side effects

lesser chance of weight gain

effective positive and negative symptoms

28
Q

Ziprasidone (dihydroindolone)

A

injectable form for acute treatment of very agitated or violent patients

may cause QTc segment prolongation and serious cardiac arrhythmias (ventricular tachycardia and sudden death)

29
Q

Aripiprazole (Dihydrocarbostyril)

A

most widely prescribed

1st antipsychotic with partial agonist activity at D2

termed DA stabilizer due to blocking D2 receptor but also stimulating D2

considered 3rd gen antipsychotic

lower weight gain, little effect on prolactin levels, no extrapyramidal side effects

30
Q

Asenapine

A

used for schizophrenia and acute manic episode associated with bipolar disorder

sublingual admin

limited weight gain, no hyperlipidemia, no change in prolactin

minor extrapyramidal effects

31
Q

Lurasidone

A

schizophrenia, depressive episodes associated with bipolar

minimal weight gain

extrapyramidal effects may occur; especially akathisia

32
Q

CNS effects and side effects of antipsychotic

A

sedation
mild anti anxiety
neuroleptic syndrome

33
Q

Neuroleptic syndrome

A

common with typical antipsychotics

cause loss of pleasure and reward

34
Q

Endocrine effects and side effects

A

increased prolactin secretion
increased female, decreased male libido
increase appetite

35
Q

increased prolactin secretion

A

“typical” cause prominent prolactin elevating effects

“atypical” have minimal effects on prolactin release

36
Q

Antiemetic effect

A

due to blockade of DA receptors at chemoreceptor trigger zone (CRTZ) in medulla

37
Q

Other clinical uses of DA receptor antagonists

A

Treating Huntington’s Disease
Treatment of Gilles de la Tourette’s syndrome
As an antiemetic
In anesthesiology to produce neurolepanalgesia
treatment of intractable hiccoughs

38
Q

Parkinson syndrome (EPS)

A

onset 5-30 days, bradykinesia, rigidity, tremor.

Treatable with anticholinergic drugs and amantidine

39
Q

Acute dystonic reactions (EPS)

A

onset 1-5 days, spasm of tongue, neck, face, back muscles.

Treatable with anticholinergic drugs

40
Q

Akathisia

A

Onset 5-6 days, motor restlessness and desire to be in constant motion

Treatable by reducing antipsychotic drug dose.

41
Q

Neuroleptic malignant syndorme

A

Onset weeks, can persist for days after stopping, characterized by fever, unstable blood pressure, stupor, can be fatal

Treat by stop antipsychotic immediately

42
Q

Tardive dyskinesia

A

late occurring movement disorder (Months to years)

characterized by repeated involuntary movements of mouth, tongue, lips, jaws

No effective therapy, crucial to use lowest effective dose to prevent development

Mechanism: chronic blockade of Da receptors causes increase in D2 like receptors in striatum….supersensitivity?

43
Q

Skin Reactions

A

Especially with phenothiazines

hypersensitivity reactions - urticaria, itching
Contact dermatitis - those who handle drug
photosensitivity - resembles sunburn, use sun screen
Abnormal skin pigmentation - grey/blue patches

44
Q

Problem with Dopamine Theory

A
  1. no evidence for increased DA cell activity or DA release, no increase in DA levels or metabolites in brain or CSF of schizophrenics
  2. Poor temporal correlation between DA receptor block and antipsychotic effect
  3. correlation may not imply causation: DA receptor blocking property of anti-psychotic drugs does not necessarily indicate a causative role of DA in psychosis
  4. other transmitter systems and brain areas are also likely involved in etiology of schizophrenia
45
Q

Psychosis

A

Characterized by impaired behavior with inability to think coherently and comprehend reality

46
Q

Support for DA theory

A

Drugs that block DA receptors reduce psychotic symptoms

Drugs that increase synaptic DA levels can cause psychotic symptoms

PET scans show increase D2 like receptors in caudate nucleus of untreated schizophrenics, suggest D@ up regulator is feature of disease

Strong correlation between D2-like receptor blockade and antipsychotic drug potency

Pharmacology and Medical Chemistry I (30 decks)

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