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PH 110.1 - Pharmaceutical & Medicinal Organic Chemistry (Lab) > MIDTERM 02 - Antiparkinsonian and Antipsychotic Drugs > Flashcards

MIDTERM 02 - Antiparkinsonian and Antipsychotic Drugs Flashcards

1
Q

Hormone that acts as a CNS neurotransmitter, controlling emotion, movement, and reward mechanisms

A

Dopamine

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2
Q

Dopamine is derived from the amino acid __________

A

Tyrosine

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3
Q

Tyrosine is converted to levodopa by the enzyme __________, which is the rate-limiting step in dopamine synthesis

A

Tyrosine hydroxylase (TH)

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3
Q

Dopamine is a precursor of __________ and __________ (NE)

A

Norepinephrine, Epinephrine

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4
Q

__________ is converted to levodopa by the enzyme tyrosine hydroxylase (TH), which is the rate limiting step in dopamine synthesis

A

Tyrosine

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5
Q

Tyrosine is converted into __________ by the enzyme tyrosine hydroxylase (TH), which is the rate-limiting step in dopamine synthesis

A

Levodopa

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6
Q

Tyrosine is converted into levodopa by the enzyme __________, which is the rate-limiting step in dopamine synthesis

A

Tyrosine hydroxylase (TH)

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7
Q

L-aromatic __________ converts levodopa to dopamine

A

Amino acid decarboxylase (AADC)

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8
Q

__________ itself does not cross the BBB

A

Dopamine

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8
Q

L-aromatic __________ converts levodopa to dopamine

A

Amino acid decarboxylase (AADC)

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8
Q

__________ crosses the BBB via the large neutral amino acid carrier

A

L-DOPA

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8
Q

Dopamine metabolism is via __________ or __________ (MC)

A

Monoamine oxidase (MAO), Catechol-O-methyltransferase (COMT)

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9
Q

2 forms of MAO

A

MAO-A, MAO-B (more related to Parkinson’s)

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10
Q

Is a progressive neurodegenerative illness characterized by tremor, muscular rigidity, bradykinesia, and postural imbalane

A

Parkinson’s disease

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11
Q

Parkinson’s disease __________ dopamine and ___________ acetylcholine

A

Decreases, Increases

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12
Q

A prodrug that is metabolized to dopamine after penetrating the BBB

A

Levodopa

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13
Q

Coadministration of levodopa with the AADC inhibitor, __________, prevents decarboxylation of levodopa outside of the CNS

A

Carbidopa

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14
Q

2 irreversible, selective MAO-B inhibitors (SR)

A

Selegiline, Rasagiline

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15
Q

Causes psychomotor and cardiovascular adverse effects due to the metabolites, L-methamphetamine and L-amphetamine (Examples of MAO-B inhibitors)

A

Selegiline

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16
Q

Is more potent that selegiline (Examples of MAO-B inhibitors)

A

Rasagiline

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17
Q

Inhibits COMT in the CNS and periphery (Examples of COMT inhibitors)

A

Tolcapone

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18
Q

Only inhibits peripheral COMT; does not penetrate the BBB (Examples of COMT inhibitors)

A

Entacapone

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19
Q

Dopamine agonists are classified into __________ derivatives and __________ derivatives (EN)

A

Ergot, Non-ergot

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20
Q

Pergolide (Type of dopamine agonist)

A

Ergot derivative

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21
Q

Cabergoline (Type of dopamine agonist)

A

Ergot derivative

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22
Q

Bromocriptine (Type of dopamine agonist)

A

Ergot derivative

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23
Q

Apomorphine (Type of dopamine agonist)

A

Non-ergot derivative

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24
Q

Pramipexole (Type of dopamine agonist)

A

Non-ergot derivative

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25
Q

Ropinirole (Type of dopamine agonist)

A

Non-ergot derivative

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26
Q

Rotigotine (Type of dopamine agonist)

A

Non-ergot derivative

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27
Q

Agents used for treating the tremor aspect of Parkinson’s disease

A

Anticholinergic agents

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28
Q

Benztropine, trihexyphenidyl, orphenadrine, and procyclidine are all examples of __________ agents

A

Anticholinergic

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29
Q

Demonstrated beneficial effects in the treatment of PD; also used in the prevention or treatment of influenza (Examples of anticholinergic agents)

A

Amantadine

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30
Q

Are psychogenic mental disorders involving a loss of contact with reality

A

Psychoses

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31
Q

The most common psychoses in which perception, thinking, communication, social functioning, and attention are altered

A

Schizophrenia

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32
Q

Is a particular kind of psychosis characterized mainly by a clear sensorium but a marked thinking disturbance

A

Schizophrenia

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33
Q

Hallucinations (Types of schizophrenia symptoms)

A

Positive

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34
Q

Delusions (Types of schizophrenia symptoms)

A

Positive

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35
Q

Disorganized speech and behavior (Types of schizophrenia symptoms)

A

Positive

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36
Q

Alogia (Types of schizophrenia symptoms)

A

Negative

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37
Q

Avolition (Types of schizophrenia symptoms)

A

Negative

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38
Q

Affective flattening (Types of schizophrenia symptoms)

A

Negative

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39
Q

Anhedonia (Types of schizophrenia symptoms)

A

Negative

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40
Q

Asociality (Types of schizophrenia symptoms)

A

Negative

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41
Q

Memory (Types of schizophrenia symptoms)

A

Cognitive deficits

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42
Q

Attention (Types of schizophrenia symptoms)

A

Cognitive deficits

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43
Q

Planning (Types of schizophrenia symptoms)

A

Cognitive deficits

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44
Q

Decision making (Types of schizophrenia symptoms)

A

Cognitive deficits

45
Q

3 hypothesis related to schizophrenia pathophysiology (DSG)

A

Dopamine, Serotonin, Glutamate

46
Q

Is the major excitatory neurotransmitter in the brain

47
Q

__________ and __________ are noncompetitive inhibitors of the NMDA receptor that exacerbate both cognitive impairment and psychosis in patients with schizophrenia (PK)

A

Phencyclidine (PCP), Ketamine

48
Q

Previously known as neuroleptic drugs, antischizophrenic drugs, or major tranquilizers; used is the symptomatic treatment of thought disorders, most notably schizophrenia

A

Antipsychotic drugs

49
Q

Antipsychotics are grouped into __________ and __________ categories (TA)

A

Typical (1st generation), Atypical (2nd generation)

50
Q

Both categories of antipsychotics share a common feature, a ____________ that is often hydrophobically substituted

A

Dopamine-like structure

51
Q

Are better for treating positive signs than negative signs (Categories of antipsychotics)

A

Typical (1st generation)

52
Q

Chlorpromazine and haloperidol are examples of __________ antipsychotics (Categories of antipsychotics)

A

Typical (1st generation)

53
Q

Are better for treating negative signs; they target the D2 receptor and other receptors (Categories of antipsychotics)

A

Atypical (2nd generation)

54
Q

Clozapine and risperidone are examples of __________ antipsychotics (Categories of antipsychotics)

A

Atypical (2nd generation)

55
Q

Typical antipsychotics are also associated with a significant degree of __________

A

Extrapyramidal symptoms (EPS)

56
Q

Some EPS associated with typical antipsychotics are defined as __________, which tend to occur within the first few weeks of treatment and decline over time

A

Acute dystonias

57
Q

The EPS that are widely associated with typical antipsychotics is __________, which develops over months to years and is often irreversible

A

Tardive dyskinesia

58
Q

Atypical antipsychotics are ________ to produce extrapyramidal symptoms (EPS)

A

Less prone

59
Q

Atypical antipsychotics are __________ against negative symptoms

A

More active

60
Q

Are also known as first-generation or conventional antipsychotics, classical neuroleptics, or major tranquilizers (Categories of antipsychotics)

A

Typical antipsychotics (1st generation)

61
Q

Phenothiazines, thioxanthenes, butyrophenones, diphenylbutylpiperidines, and dihydroindolones are all examples of __________ antipsychotics

62
Q

Tend to be associated with more EPS and less histaminic, alpha adrenergic, and anticholinergic side effects (Types of typical antipsychotics)

A

High-potency typical antipsychotics

63
Q

Are associated with less EPS but more H1, α1, and muscarinic side effects (Types of typical antipsychotics)

A

Low-potency typical antipsychotics

64
Q

Are marketed primarily for their antiemetic, antihistaminic, and anticholinergic effect (Examples of typical antipsychotics)

A

Phenothiazines

65
Q

Prototype of phenothiazines

A

Chlorpromazine

66
Q

Phenothiazines have a tricyclic structure (6-6-6 system) in which two benzene rings are linked by a __________ and a __________ atom (SAR of phenothiazines) (SN)

A

Sulfur, Nitrogen

67
Q

The best position for substitution is the __________ (SAR of phenothiazines)

A

2-position

68
Q

Activity increases as the electron-withdrawing activity of the 2-substituent __________ (SAR of phenothiazines)

69
Q

The three-carbon chain between position __________ and the aliphatic amino nitrogen is critical for neuroleptic activity (SAR of phenothiazines)

70
Q

Shortening or lengthening the three-carbon chain at position 10 drastically __________ the activity (SAR of phenothiazines)

71
Q

Phenothiazines with __________ carbon atoms separating the two nitrogen atoms lack antipsychotic efficacy (SAR of phenothiazines)

72
Q

Shortening the chain to __________ carbons has the effect of amplifying the antihistaminic and anticholinergic activities (SAR of phenothiazines)

73
Q

The amine in phenothiazines is always __________ (SAR of phenothiazines)

74
Q

The R group in phenothiazines can be a __________ (SAR of phenothiazines)

75
Q

-promazine indicates an __________ side chain (SAR of phenothiazines)

76
Q

-ridazine indicates a __________ side chain (SAR of phenothiazines)

A

Piperidine

77
Q

-phenazine/-perazine indicates a __________ side chain (SAR of phenothiazines)

A

Piperazine

78
Q

Promazine, chlorpromazine, and tiflupromazine has an __________ side chain (SAR of phenothiazines)

79
Q

Thioridazine and mesoridazine have a __________ side chain (SAR of phenothiazines)

A

Piperidine

80
Q

Prochlorperazine, trifluoperazine, perphenazine, and fluphenazine have a __________ side chain (SAR of phenothiazines)

A

Piperazine

81
Q

Several piperazine phenothiazines are __________ at a free hydroxyl with long-chain fatty acids to produce highly lipophilic and long-acting prodrugs (SAR of phenothiazines)

A

Esterified

82
Q

Ranking of phenothiazine side chains according to anti-HAM effects

A

Aliphatic > Piperidine > Piperazine

83
Q

Antihistaminic effect of phenothiazines

84
Q

Anti-adrenergic effect of phenothiazines

A

Orthostatic hypotension

84
Q

2 antimuscarinic and anticholinergic effects of phenothiazines (DC)

A

Dry mouth, Constipation

85
Q

Ranking of phenothiazide side chains according to potency

A

Piperazine > Piperidine > Aliphatic

86
Q

The __________ the potency, the higher the EPS (SAR of phenothiazines)

87
Q

Has a double bond on C10; is less potent that other phenothiazines (Examples of typical antipsychotics)

A

Thioxanthenes

88
Q

Example of thioxanthene

A

Thiothixene

89
Q

Are extremely potent antipsychotic agents; the EPS are extremely marked (Examples of typical antipsychotics)

A

Butyrophenones

90
Q

Attachment of a tertiary amino group to the ___________ carbon of the butyrophenone skeleton is essential for neuroleptic activity (SAR of butyrophenones)

91
Q

Lengthening, shortening, or branching of the three-carbon propyl chain __________ neuroleptic potency (SAR of butyrophenones)

92
Q

Nitrogen is usually incorporated into a six-membered ring that is substituted in the __________ position (SAR of butyrophenones)

93
Q

The most potent butyrophenone compounds have a fluorine substituent in the __________ position of the benzene ring (SAR of butyrophenones)

94
Q

Replacement of the keto moiety __________ neuroleptic potency (SAR of butyrophenones)

95
Q

The keto (C=O) group is important but can be replaced to __________ group (SAR of butyrophenones)

A

p-F-phenyl

96
Q

The __________ group can vary and assist activity (SAR of butyrophenones)

97
Q

__________ is an example of dihydroindolones (Examples of typical antipsychotics)

98
Q

Also known as second-generation antipsychotics; provide a greater reduction in both the positive and negative symptoms of schizophrenia (Categories of antipsychotics)

A

Atypical antipsychotics (2nd generation)

99
Q

Additional tricyclic antipsychotic agents are the ___________, containing a seven-membered central ring (6-7-6 system)

A

Benzazepines

100
Q

The newer __________ antipsychotics include dibenzodiazepines, dibenzoxazepines, thienobenzodiazepines, and dibenzothiazepines

101
Q

__________ antipsychotics provide a low production of EPS and a reduction of negative symptoms

102
Q

A dibenzodiazepine derivative; the first atypical antipsychotic (Examples of atypical antipsychotics - benzazepine and related analogs)

103
Q

A dibenzoxazepine derivative; is actually a typical antipsychotic; is N-demethylated to yield amoxapine (an antidepressant drug) (Examples of atypical antipsychotics - benzazepine and related analogs)

104
Q

Loxapine is N-demethylated to yield __________, an antidepressant drug

105
Q

A thienobenzodiazepine derivative (Examples of atypical antipsychotics - benzazepine and related analogs)

A

Olanzapine

106
Q

A dibenzothiazepine derivative (Examples of atypical antipsychotics - benzazepine and related analogs)

A

Quetiapine

107
Q

Risperidone and paliperidone are both __________ derivatives (Examples of atypical antipsychotics)

A

Benzisoxazole

108
Q

Ziprasidone and lurasidone are both __________ derivatives (Examples of atypical antipsychotics)

A

Benzisothiazole

109
Q

__________ is an example of arylpiperazine quinolinone derivative (Examples of atypical antipsychotics)

A

Aripiprazole

110
Q

From the gastroprokinetic and antiemetic agent, metoclopramide (Examples of atypical antipsychotics - benzamides)

A

Remoxipride

111
Q

Remoxipride is from the gastrokinetic and antiemetic agent, __________

A

Metoclopramide

112
Q

Lithium carbonate, lithium citrate, and lithium chloride are examples of __________ (Examples of atypical antipsychotics - antimanic agents)

A

Lithium salts

112
Q

2 antimanic agents also used as anticonvulsants (Examples of atypical antipsychotics - antimanic agents) (CV)

A

Carbamazepine, Valproic acid

112
Q

Not used because it is hygroscopic and irritating to the GI tract; is an example of lithium salt (Examples of atypical antipsychotics - antimanic agents)

A

Lithium chloride

PH 110.1 - Pharmaceutical & Medicinal Organic Chemistry (Lab) (7 decks)

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