M2.6 Flashcards
1
Q
- a MOVEMENT disorder
- unknown cause
- a degenerative disease of the brain that often impairs MOTOR SKILLS, speech, and other functions
A
PARKINSON’S DISEASE
2
Q
Parkinson’s disease is also known as
A
Primary Parkinsonism
Idiopathic PD
idopathic - unknown
3
Q
PATHOPHYSIOLOGY OF PARKINSONISM
occurs because of a LOSS of ____ in the nigrostriatal pahtway
A
DOPAMINE
4
Q
PATHOPHYSIOLOGY OF PARKINSONISM
disrupts the balance between ____ and ____ systems within the striatum and basal ganglia
low DA, high Ach
A
dopaminergic and cholinergic systems
5
Q
DRUG-INDUCED PARKINSONISM
deplete BIOGENIC MONOAMINES from their storage vesicles
inhibit DA storage
A
Reserpine and Tetrabenazine
6
Q
DRUG-INDUCED PARKINSONISM
block DOPAMINE receptor
A
Haloperidol
Metoclopramide
Phenothiazines
7
Q
DRUG-INDUCED PARKINSONISM
for TOURETTE’S
A
HALOPERIDOL
8
Q
DRUG-INDUCED PARKINSONISM
a PROKINETIC agent
A
Metoclopramide
9
Q
DRUG-INDUCED PARKINSONISM
inhibit storage of DA in vesicles
A
Reserpine
10
Q
ANTIPARKINSON’S AGENTS
drugs that directly INCREASE dopamine levels
A
Levodopa
Selegiline
Amantadine
11
Q
ANTIPARKINSON’S AGENTS
antiviral - for influenza
A
Amantadine
12
Q
ANTIPARKINSON’S AGENTS
Dopamine receptor antagonist
A
Bromocriptine
Pergolide
Pramipexole
Ropinirole
13
Q
ANTIPARKINSON’S AGENTS
ergot derivatives
from fungi
A
Bromocriptine
Pergolide
14
Q
ANTIPARKINSON’S AGENTS
Acetylcholine receptor antagonist
A
Benztropine
Trihexyphenidyl
Biperiden
also used for EPS
15
Q
ANTIPARKINSON’S AGENTS
Dopa decarboxylase inhibitor
A
Carbidopa
16
Q
ANTIPARKINSON’S AGENTS
COMT ihibitor
A
Tolcapone
Entacapone
17
Q
ANTIPARKINSON’S AGENTS
____ cannot pass through the Blood Brain Barrier
A
DOPAMINE
18
Q
ANTIPARKINSON’S AGENTS
- Pramipexole
- Ropinirole
- Bromocriptine
- Pergolide
are agonist of ____
A
Parkinsonism / Dopamine
19
Q
ANTIPARKINSON’S AGENTS
____ can enter the Blood Brain Barrier
A
L-DOPA
20
Q
ANTIPARKINSON’S AGENTS
L-DOPA when metabolized will turn into
A
DOPAMINE
21
Q
ANTIPARKINSON’S AGENTS
the enzyme that metabolizes L-DOPA before it enters the BBB
A
DOPA decarboxylase
COMT
22
Q
ANTIPARKINSON’S AGENTS
inhibit DOPA decarboxylase
A
Carbidopa
23
Q
ANTIPARKINSON’S AGENTS
converts L-DOPA to dopamine
A
DOPA decarboxylase
24
Q
ANTIPARKINSON’S AGENTS
MAO B inhibitors
A
Selegiline
Rasagiline
25
# **ANTIPARKINSON'S AGENTS**
inhibits **COMT** -- converts dopamine to 3-OMD
Tolcapone
26
# **MANAGEMENT OF PARKINSON'S DISEASE**
**FIRST** line
Amantadine
Benztropine
Selegiline
27
# **ANTIPARKINSON'S AGENTS**
**SECOND** line
L-dopa
Carbidopa
Entacapone
Tolcapone
28
# **ANTIPARKINSON'S AGENTS**
**THIRD** line
Bromocriptine
Pergolide
Pramipexole
Roopinorole
29
# **AGENTS THAT INCREASE DOPAMINE LEVELS**
* is the **metabolic precursor** of **DOPAMINE**
* transported into the brain and subsequently converted to dopamine in the **basal ganglia**
* **can pass through BBB**
* it **restores** the dopamine levels in the **extrapyramidal centers**
* it is **decarboxylated** in the **periphery**
* given in combination with **carbidopa**
* decreases the **rigidity**, **tremors** and other symptoms
LEVODOPA
30
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
**transported** into the **brain** and subsequently **converted** to **dopamine** in the ____
basal ganglia
31
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
it **restores** the dopamine levels in the ____
extrapyramidal centers
32
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
it is **decarboxylated** in the ____
periphery
33
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
given in **combination** with
carbidopa
34
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
L-dopa + Carbidopa
Sinemet 125
35
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
L-dopa + Carbidopa + ENTACAPONE
Stalevo
36
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
how many **%** goes to the **BRAIN**
1-3%
37
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
how many **%** gets **metabolized** in the **GI TRACT**
70%
38
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
how many **%** gets **metabolized** in the **PERIPHERAL TISSUES (toxicity)**
27-29%
39
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
Levodopa + Carbidopa:
what type of action
potentiation
| carbidopa - does not have an effect itself; 1 + 0 = 1
40
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
PERIPHERAL EFFECTS:
involving **eyes**; **DILATION**
MYDRIASIS
41
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
PERIPHERAL EFFECTS:
**LOW** WBC
blood dyscracias
42
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA**
PERIPHERAL EFFECTS:
test for **hemolytic anemia**
+ COOMBS TEST
43
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA | AE/SE**
**off**-periods of **marked akinesia** alternate over the course of a few hours with **on**-periods of **imporved mobility** but often **marked dyskensia**
ON-OFF PHENOMENON
| **OFF** - less akinesia - no mobility
**ON** - dyskenisia - more movemen
44
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA | CONTRAINDICATIONS**
**HYPERTENSIVE crisis** due to **excess dopamine** in the **periphery**
NONSELECTIVE MAOIs
45
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA | CONTRAINDICATIONS**
**diminishes** the effectivness of **levodopa** because it **increases PERIPHERAL BREAKDOWN** of the drug
PYRIDOXINE
46
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA | CONTRAINDICATIONS**
**Pyridoxine** is also known as
vit. b6
47
# **AGENTS THAT INCREASE DOPAMINE LEVELS | LEVODOPA | CONTRAINDICATIONS**
**oppose** levadopa's effect
(**antag**onist)
antipsychotics
48
# **AGENTS THAT INCREASE DOPAMINE LEVELS**
* **selectively** inhibits **MAO B**
* **decrease** the **metabolism** of **dopamine** by preventing **inter-neuronal degradation**
* inhibition of MAO-B **slows** the **breakdown** of **dopamine** in the **striatum**
SELEGILINE
(Deprenyl)
49
# **AGENTS THAT INCREASE DOPAMINE LEVELS | SELEGILINE**
**decrease** the **metabolism** of dopamine by preventing ____
inter-neuronal degradation
50
# **AGENTS THAT INCREASE DOPAMINE LEVELS | SELEGILINE**
**inhibition** of **MAO B** SLOWS the breakdown of dopamine in the ____
striatum
51
# **AGENTS THAT INCREASE DOPAMINE LEVELS**
* an **ANTIVIRAL** agent (for***influenza***) that **enhances** the **release** of dopamine from surviving nigral neurons
* **inhibits** the **reuptake** of **dopamine** at synapses
AMANTADINE
52
# **DOPAMINE RECEPTOR AGONIST**
* an **ergot** derivatice that predominantly **stimulates** the **STRIATAL D2 NON-ADENYL CYCLASE-linked** dopamine receptors
* ADVERSE EFFECTS:
* **hallucination** and **delirium**
* nausea and vomiting
* **cardiac arrythmia**
* **postural hypotension**
* **erythromelalgia**
* worsen **ulcer**
BROMOCRIPTINE
(Parlodel)
53
# **DOPAMINE RECEPTOR AGONIST**
* **stimulates POSTSYNAPTIC DOPAMINE receptors** at both **D1** and **D2** receptor site in the **nigrostriatum**
* ADVERSE EFFECTS:
* **anxiety**
* **confusion**
* **hallucinations**
* **dyskenisia**
PERGOLIDE
54
# **DOPAMINE RECEPTOR AGONIST**
* a **NON-ergot D2-receptor SELECTIVE agonist**
* ADVERSE EFFECTS:
* **drowsiness**
* **hallucination**
* **insomnia**
* **nausea**
* **orthostatic hypotension**
Pramipexole
55
these are used to:
* help **reduce cholinergic output** of the striatum
* **restore** a **normal balance** between dopamine and acetylcholine within nigrostriatal system
ADVERSE EFFECTS:
* **mydriasis** (blurred vision; dilation)
* **constipation**
* **dry mouth and skin**
* **urinary retention**
* **tachycardia**
anticholinergics
56
**ACETYLCHOLINE RECEPTOR AGONIST**
Benztropine
Biperiden
Trihexyphenidyl
| BBT
57
# **ACETYLCHOLINE RECEPTOR AGONIST**
* **blocks** **MUSCARINIC CHOLINERGIC receptor** in the CNS
* **reduces** the **EXCESSIVE cholinergic activity** present in **parkinsonism**
* ADVERSE EFFECTS:
* **agitation**, **nervousness**, and **confusion**
* **blurred vision**
* **memory loss**
* **hallucination**
* **difficulty breathing**
BENZTROPINE
58
# **ACETYLCHOLINE RECEPTOR AGONIST**
* **partially block CENTRAL CHOLINERGIC receptors**
* helps in **restoring** the **BALANCE** of cholinergic and dopaminergic activity in the basal ganglia
TRIHEXYPHENIDYL
59
# **ACETYLCHOLINE RECEPTOR AGONIST**
are **anticholinergics** EQUALLY EFFECTIVE as **levodopa**?
NO, it is much **LESS efficacious** than levodopa
| Levodopa > anticholinergics
they are only used to reduce symptoms
60
# **ACETYLCHOLINE RECEPTOR AGONIST**
clinical effects
reduce **tremor**, **rigidity**, **akinesia**, and **drooling**
61
# **DOPA DECARBOZYLASE INHIBITOR**
* it does **NOT** cross blood brain barrier; **cannot** inhibit **L-dopa conversion** in the **brain**
* **reduces** the **metabolism** of **levadopa** in the **periphery**
* **increases** the **availability** of dopamine to the CNS
* **decrese** the **severity** of the **side effects** of **peripherally formed dopamine**
CARBIDOPA
62
# **COMT INHIBITORS**
* a **SELECTIVE** and **REVERSIBLE** inhibitor of COMT
ENTACAPONE
63
# **DRUGS FOR OTHER MOVEMENT ABNORMALITIES**
* **CHRONIC MULTIPLE TICS**
* pathophysiologic basis is unknown
TOURETTE'S SYNDROME
64
# **DRUGS FOR OTHER MOVEMENT ABNORMALITIES**
**most effective** pharmacologic approach for **TOURETTE'S syndrome**
HALOPERIDOL
65
# **DRUGS FOR OTHER MOVEMENT ABNORMALITIES**
**Tourette's** syndrome is also known as
Gilles de la Tourette's Syndrome
66
# **DRUGS FOR OTHER MOVEMENT ABNORMALITIES**
* characterized by **PROGRESSIVE CHOREA** and **dementia**
| **involuntary movement of HANDS & FEET**
HUNTINGTON'S DISEASE
67
# **DRUGS FOR OTHER MOVEMENT ABNORMALITIES**
* seems to be related to **imnbalance** of dopamine, Ach, and Dopa
* results from **functional overactivity** in **dopaminergic** nigrostriatal pathways
CHOREA
68
# **DRUGS FOR OTHER MOVEMENT ABNORMALITIES**
drugs that alleviate **CHOREA**
(Huntington's Disease):
* **deplete** CENTRAL MONOAMINES
Reserpine
Tetrabenazine
69
# **DRUGS FOR OTHER MOVEMENT ABNORMALITIES**
drugs that alleviate **CHOREA**
(Huntington's Disease):
* **block** DOPAMINE receptors
Phenothiazine
Butyrophenone
70
# **TIC CLASSIFICATIONS**
* **SUDDEN**
* **BRIEF**
* **random**
* **MEANINGLESS**
* isolated to muscle group: **facial** and **neck**, **abdomen**, **extrimities**, others
SIMPLE | MOTOR
71
# **TIC CLASSIFICATIONS**
* **SUDDEN**
* **MEANINGLESS**
* **random**
* often **"allergy"-like** (grunting, sniffing, throat clearing, coughing)
* sometimes **nonvocal** (tounge clicking, sucking, hissing)
* **animal noises** (barking, chirping, whistling)
SIMPLE | PHONIC
72
# **TIC CLASSIFICATIONS**
* **SLOWER** and **LONGER**
* **PURPOSEFUL**
* **dystonic**, **imitative**, **self-abusive**
COMPLEX | MOTOR
73
# **TIC CLASSIFICATIONS**
* often **SUDDEN**
* **MEANINGFUL** linguistic elements
* may be **IMITATIVE (echoic)**
* **speech atypicalities**: palilalia
COMPLEX | PHONIC
74
# **TIC CLASSIFICATIONS**
repeating **own** spech
OWN SPEECH?!
PALILALIA
75
# **DRUG-INDUCED DYSKENISIAS**
* a disorder characterized by a variety of **ABNORMAL MOVEMENTS**
* a **common complication** of **LONG-TERM** **neuroleptic** or **metoclopramide** drug treatement
TARDIVE DYSKINESIA
76
# **DRUG-INDUCED DYSKENISIAS**
* **INVOLUNATRY UNCONTROLLABLE** movement in **LOWER part** of the body
Tardive Dystonia / Akathisia
77
# **DRUG-INDUCED DYSKENISIAS**
* manifested by **rhytmic VERTICAL movements**about the **MOUTH**
RABBIT SYNDROME
78
* characterized by an **unpleasant CREEPING DISCOMFORT** that seem to arise **deep within the LEGS** and occasionally in the **arms**
RESTLESS LEG SYNDROME
79
preferred treatment for **RESTLESS LEG SYNDROME**
DOPAMINE therapy
80
* **inherited** disorder of **COPPER METABOLISM** (copper **deficiency**)
* ***biochemically***, by **reduced serum copper** and **ceruplasmin** concentrations
* ***pathologically***, by marked **increase copper** in the **brain** and **viscera**
* ***clinically***, by signs of **hepatic** and **neurologic dysfunction**
WILSON'S DISEASE
81
# **DRUGS FOR ALZHEIMER'S DISEASE AND OTHER DEGENERATIVE DISORDERS**
a **combination drug** in **extended release capsule** that was approved in **2014** for moderate to severe disease
Donepizil + Memantine
82
# **DRUGS FOR ALZHEIMER'S DISEASE AND OTHER DEGENERATIVE DISORDERS**
* cholinesterase inhibitor for **MODERATE to SEVERE** AD
* prevents the breakdown of **acetylcholine** in the brain
* AE: N&V, diarrhea
DONEPIZIL
83
# **DRUGS FOR ALZHEIMER'S DISEASE AND OTHER DEGENERATIVE DISORDERS**
* cholinesterae inhibitor for **MILD to MODERATE** AD
* prevents the breakdown of **acetylcholine** and stimulates **nictonic** receptors
* AE: N&V, diarrhea, loss of appetite, weight loss
GALANTAMINE
84
# **DRUGS FOR ALZHEIMER'S DISEASE AND OTHER DEGENERATIVE DISORDERS**
* cholinesterase inhibitor for **MILD to MODERATE** AD
* prevents the breakdown of **acetylcholine** and **butyrylcholine** in the brain
* AE: N&V, diarrhea, loss of appetie, weight loss, muscle weakness
RIVASTIGMINE
85
# **DRUGS FOR ALZHEIMER'S DISEASE AND OTHER DEGENERATIVE DISORDERS**
* N-methyl-D-aspartate agonist for **MODERATE to SEVERE** AD
* blocks the **toxic effects** associated with **excess glutamate** and regulates **glutamate activation**
* AE: dizziness, headache, constipation, confusion
MEMANTINE
86
**DRUGS FOR ALZHEIMER'S DISEASE**
Tacrine
Donezipil
Galantamine
Rivastigmine
Memantine
| **MEMANTINE** - NOT a cholinesterase inhibitor
