MIDTERM 02 - Antiparkinsonian and Antipsychotic Drugs Flashcards
1
Q
Hormone that acts as a CNS neurotransmitter, controlling emotion, movement, and reward mechanisms
A
Dopamine
2
Q
Dopamine is derived from the amino acid __________
A
Tyrosine
3
Q
Tyrosine is converted to levodopa by the enzyme __________, which is the rate-limiting step in dopamine synthesis
A
Tyrosine hydroxylase (TH)
3
Q
Dopamine is a precursor of __________ and __________ (NE)
A
Norepinephrine, Epinephrine
4
Q
__________ is converted to levodopa by the enzyme tyrosine hydroxylase (TH), which is the rate limiting step in dopamine synthesis
A
Tyrosine
5
Q
Tyrosine is converted into __________ by the enzyme tyrosine hydroxylase (TH), which is the rate-limiting step in dopamine synthesis
A
Levodopa
6
Q
Tyrosine is converted into levodopa by the enzyme __________, which is the rate-limiting step in dopamine synthesis
A
Tyrosine hydroxylase (TH)
7
Q
L-aromatic __________ converts levodopa to dopamine
A
Amino acid decarboxylase (AADC)
8
Q
__________ itself does not cross the BBB
A
Dopamine
8
Q
L-aromatic __________ converts levodopa to dopamine
A
Amino acid decarboxylase (AADC)
8
Q
__________ crosses the BBB via the large neutral amino acid carrier
A
L-DOPA
8
Q
Dopamine metabolism is via __________ or __________ (MC)
A
Monoamine oxidase (MAO), Catechol-O-methyltransferase (COMT)
9
Q
2 forms of MAO
A
MAO-A, MAO-B (more related to Parkinson’s)
10
Q
Is a progressive neurodegenerative illness characterized by tremor, muscular rigidity, bradykinesia, and postural imbalane
A
Parkinson’s disease
11
Q
Parkinson’s disease __________ dopamine and ___________ acetylcholine
A
Decreases, Increases
12
Q
A prodrug that is metabolized to dopamine after penetrating the BBB
A
Levodopa
13
Q
Coadministration of levodopa with the AADC inhibitor, __________, prevents decarboxylation of levodopa outside of the CNS
A
Carbidopa
14
Q
2 irreversible, selective MAO-B inhibitors (SR)
A
Selegiline, Rasagiline
15
Q
Causes psychomotor and cardiovascular adverse effects due to the metabolites, L-methamphetamine and L-amphetamine (Examples of MAO-B inhibitors)
A
Selegiline
16
Q
Is more potent that selegiline (Examples of MAO-B inhibitors)
A
Rasagiline
17
Q
Inhibits COMT in the CNS and periphery (Examples of COMT inhibitors)
A
Tolcapone
18
Q
Only inhibits peripheral COMT; does not penetrate the BBB (Examples of COMT inhibitors)
A
Entacapone
19
Q
Dopamine agonists are classified into __________ derivatives and __________ derivatives (EN)
A
Ergot, Non-ergot
20
Q
Pergolide (Type of dopamine agonist)
A
Ergot derivative
21
Cabergoline (Type of dopamine agonist)
Ergot derivative
22
Bromocriptine (Type of dopamine agonist)
Ergot derivative
23
Apomorphine (Type of dopamine agonist)
Non-ergot derivative
24
Pramipexole (Type of dopamine agonist)
Non-ergot derivative
25
Ropinirole (Type of dopamine agonist)
Non-ergot derivative
26
Rotigotine (Type of dopamine agonist)
Non-ergot derivative
27
Agents used for treating the tremor aspect of Parkinson's disease
Anticholinergic agents
28
Benztropine, trihexyphenidyl, orphenadrine, and procyclidine are all examples of __________ agents
Anticholinergic
29
Demonstrated beneficial effects in the treatment of PD; also used in the prevention or treatment of influenza (Examples of anticholinergic agents)
Amantadine
30
Are psychogenic mental disorders involving a loss of contact with reality
Psychoses
31
The most common psychoses in which perception, thinking, communication, social functioning, and attention are altered
Schizophrenia
32
Is a particular kind of psychosis characterized mainly by a clear sensorium but a marked thinking disturbance
Schizophrenia
33
Hallucinations (Types of schizophrenia symptoms)
Positive
34
Delusions (Types of schizophrenia symptoms)
Positive
35
Disorganized speech and behavior (Types of schizophrenia symptoms)
Positive
36
Alogia (Types of schizophrenia symptoms)
Negative
37
Avolition (Types of schizophrenia symptoms)
Negative
38
Affective flattening (Types of schizophrenia symptoms)
Negative
39
Anhedonia (Types of schizophrenia symptoms)
Negative
40
Asociality (Types of schizophrenia symptoms)
Negative
41
Memory (Types of schizophrenia symptoms)
Cognitive deficits
42
Attention (Types of schizophrenia symptoms)
Cognitive deficits
43
Planning (Types of schizophrenia symptoms)
Cognitive deficits
44
Decision making (Types of schizophrenia symptoms)
Cognitive deficits
45
3 hypothesis related to schizophrenia pathophysiology (DSG)
Dopamine, Serotonin, Glutamate
46
Is the major excitatory neurotransmitter in the brain
Glutamate
47
__________ and __________ are noncompetitive inhibitors of the NMDA receptor that exacerbate both cognitive impairment and psychosis in patients with schizophrenia (PK)
Phencyclidine (PCP), Ketamine
48
Previously known as neuroleptic drugs, antischizophrenic drugs, or major tranquilizers; used is the symptomatic treatment of thought disorders, most notably schizophrenia
Antipsychotic drugs
49
Antipsychotics are grouped into __________ and __________ categories (TA)
Typical (1st generation), Atypical (2nd generation)
50
Both categories of antipsychotics share a common feature, a ____________ that is often hydrophobically substituted
Dopamine-like structure
51
Are better for treating positive signs than negative signs (Categories of antipsychotics)
Typical (1st generation)
52
Chlorpromazine and haloperidol are examples of __________ antipsychotics (Categories of antipsychotics)
Typical (1st generation)
53
Are better for treating negative signs; they target the D2 receptor and other receptors (Categories of antipsychotics)
Atypical (2nd generation)
54
Clozapine and risperidone are examples of __________ antipsychotics (Categories of antipsychotics)
Atypical (2nd generation)
55
Typical antipsychotics are also associated with a significant degree of __________
Extrapyramidal symptoms (EPS)
56
Some EPS associated with typical antipsychotics are defined as __________, which tend to occur within the first few weeks of treatment and decline over time
Acute dystonias
57
The EPS that are widely associated with typical antipsychotics is __________, which develops over months to years and is often irreversible
Tardive dyskinesia
58
Atypical antipsychotics are ________ to produce extrapyramidal symptoms (EPS)
Less prone
59
Atypical antipsychotics are __________ against negative symptoms
More active
60
Are also known as first-generation or conventional antipsychotics, classical neuroleptics, or major tranquilizers (Categories of antipsychotics)
Typical antipsychotics (1st generation)
61
Phenothiazines, thioxanthenes, butyrophenones, diphenylbutylpiperidines, and dihydroindolones are all examples of __________ antipsychotics
Typical
62
Tend to be associated with more EPS and less histaminic, alpha adrenergic, and anticholinergic side effects (Types of typical antipsychotics)
High-potency typical antipsychotics
63
Are associated with less EPS but more H1, α1, and muscarinic side effects (Types of typical antipsychotics)
Low-potency typical antipsychotics
64
Are marketed primarily for their antiemetic, antihistaminic, and anticholinergic effect (Examples of typical antipsychotics)
Phenothiazines
65
Prototype of phenothiazines
Chlorpromazine
66
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)
Sulfur, Nitrogen
67
The best position for substitution is the __________ (SAR of phenothiazines)
2-position
68
Activity increases as the electron-withdrawing activity of the 2-substituent __________ (SAR of phenothiazines)
Increases
69
The three-carbon chain between position __________ and the aliphatic amino nitrogen is critical for neuroleptic activity (SAR of phenothiazines)
10
70
Shortening or lengthening the three-carbon chain at position 10 drastically __________ the activity (SAR of phenothiazines)
Decreases
71
Phenothiazines with __________ carbon atoms separating the two nitrogen atoms lack antipsychotic efficacy (SAR of phenothiazines)
2
72
Shortening the chain to __________ carbons has the effect of amplifying the antihistaminic and anticholinergic activities (SAR of phenothiazines)
2
73
The amine in phenothiazines is always __________ (SAR of phenothiazines)
Tertiary
74
The R group in phenothiazines can be a __________ (SAR of phenothiazines)
Ring
75
-promazine indicates an __________ side chain (SAR of phenothiazines)
Aliphatic
76
-ridazine indicates a __________ side chain (SAR of phenothiazines)
Piperidine
77
-phenazine/-perazine indicates a __________ side chain (SAR of phenothiazines)
Piperazine
78
Promazine, chlorpromazine, and tiflupromazine has an __________ side chain (SAR of phenothiazines)
Aliphatic
79
Thioridazine and mesoridazine have a __________ side chain (SAR of phenothiazines)
Piperidine
80
Prochlorperazine, trifluoperazine, perphenazine, and fluphenazine have a __________ side chain (SAR of phenothiazines)
Piperazine
81
Several piperazine phenothiazines are __________ at a free hydroxyl with long-chain fatty acids to produce highly lipophilic and long-acting prodrugs (SAR of phenothiazines)
Esterified
82
Ranking of phenothiazine side chains according to anti-HAM effects
Aliphatic > Piperidine > Piperazine
83
Antihistaminic effect of phenothiazines
Sedation
84
Anti-adrenergic effect of phenothiazines
Orthostatic hypotension
84
2 antimuscarinic and anticholinergic effects of phenothiazines (DC)
Dry mouth, Constipation
85
Ranking of phenothiazide side chains according to potency
Piperazine > Piperidine > Aliphatic
86
The __________ the potency, the higher the EPS (SAR of phenothiazines)
Higher
87
Has a double bond on C10; is less potent that other phenothiazines (Examples of typical antipsychotics)
Thioxanthenes
88
Example of thioxanthene
Thiothixene
89
Are extremely potent antipsychotic agents; the EPS are extremely marked (Examples of typical antipsychotics)
Butyrophenones
90
Attachment of a tertiary amino group to the ___________ carbon of the butyrophenone skeleton is essential for neuroleptic activity (SAR of butyrophenones)
Fourth
91
Lengthening, shortening, or branching of the three-carbon propyl chain __________ neuroleptic potency (SAR of butyrophenones)
Decreases
92
Nitrogen is usually incorporated into a six-membered ring that is substituted in the __________ position (SAR of butyrophenones)
Para
93
The most potent butyrophenone compounds have a fluorine substituent in the __________ position of the benzene ring (SAR of butyrophenones)
Para
94
Replacement of the keto moiety __________ neuroleptic potency (SAR of butyrophenones)
Decreases
95
The keto (C=O) group is important but can be replaced to __________ group (SAR of butyrophenones)
p-F-phenyl
96
The __________ group can vary and assist activity (SAR of butyrophenones)
Y
97
__________ is an example of dihydroindolones (Examples of typical antipsychotics)
Molindone
98
Also known as second-generation antipsychotics; provide a greater reduction in both the positive and negative symptoms of schizophrenia (Categories of antipsychotics)
Atypical antipsychotics (2nd generation)
99
Additional tricyclic antipsychotic agents are the ___________, containing a seven-membered central ring (6-7-6 system)
Benzazepines
100
The newer __________ antipsychotics include dibenzodiazepines, dibenzoxazepines, thienobenzodiazepines, and dibenzothiazepines
Atypical
101
__________ antipsychotics provide a low production of EPS and a reduction of negative symptoms
Atypical
102
A dibenzodiazepine derivative; the first atypical antipsychotic (Examples of atypical antipsychotics - benzazepine and related analogs)
Clozapine
103
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)
Loxapine
104
Loxapine is N-demethylated to yield __________, an antidepressant drug
Amoxapine
105
A thienobenzodiazepine derivative (Examples of atypical antipsychotics - benzazepine and related analogs)
Olanzapine
106
A dibenzothiazepine derivative (Examples of atypical antipsychotics - benzazepine and related analogs)
Quetiapine
107
Risperidone and paliperidone are both __________ derivatives (Examples of atypical antipsychotics)
Benzisoxazole
108
Ziprasidone and lurasidone are both __________ derivatives (Examples of atypical antipsychotics)
Benzisothiazole
109
__________ is an example of arylpiperazine quinolinone derivative (Examples of atypical antipsychotics)
Aripiprazole
110
From the gastroprokinetic and antiemetic agent, metoclopramide (Examples of atypical antipsychotics - benzamides)
Remoxipride
111
Remoxipride is from the gastrokinetic and antiemetic agent, __________
Metoclopramide
112
Lithium carbonate, lithium citrate, and lithium chloride are examples of __________ (Examples of atypical antipsychotics - antimanic agents)
Lithium salts
112
2 antimanic agents also used as anticonvulsants (Examples of atypical antipsychotics - antimanic agents) (CV)
Carbamazepine, Valproic acid
112
Not used because it is hygroscopic and irritating to the GI tract; is an example of lithium salt (Examples of atypical antipsychotics - antimanic agents)
Lithium chloride
