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11. Drugs for parkinson & spasticity
lecture 11
26
Other
Undergraduate 2
10/12/2015

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Term
What is decreased in Parkinson's?
Definition
dopaminergic neurons in the substantia nigra
Term
Describe the disrupted flow of info through the basal ganglia in Parkinson's.
Definition
The direct pathway is inhibited
The indirect pathway is activated
Result - decreased movement
Term
What are the broad types of treatments for Parkinson's?
Definition
1. Drugs that increase dopamine levels
2. Drugs that are dopamine receptor agonists
3. Acetylcholine receptor antagonists
Term
What is L-dopa?
Definition
a biosynthetic precursor to dopamine
Term
L-dopa (can/cannot) cross the BBB.
Definition
CAN
Term
What converts L-dopa into dopamine?
Definition
l-amino acid decarboxylase (LAAD)
Term
What are some adverse effects of L-dopa?
Definition
nausea
orthostatic hypotension
cardiac arrythmias

(due to increased catecholamines in peripheral tissues)
Term
What is Carbidopa?
Definition
- an analog of l-dopa
- it inhibits LAAD from converting l-dopa to dopamine
-
Term
Peripherally administered dopamine (can/cannot) cross the BBB.
Definition
CANNOT
Term
What is Entacapone?
Definition
It is a COMT inhibitor.
It prevents the conversion of L-dopa to 3-OMD, which competes with l-dopa to cross the BBB
Term
What are the longterm effects of L-dopa?
Definition
dyskinesia & involuntary movements
psychotic effects
Term
Why do dopamine receptors cause nausea and vomiting?
Definition
Because they stimulate dopamine receptors in the vomiting centre of the medulla.
Term
What are two types of MOA-B inhibitors?
Definition
Selegiline and rasagiline
Term
MOA-B inhibitors inhibit the oxidation of dopamine into ____
Definition
dihydroxyphenlacetic acid
DOPAC
Term
Who is selegiline best suited for?
Definition
young patients or those with mild parkinson's disease
Term
What does selegiline get metabolized into?
Definition
amphetmine and methamphetamine

which cause anxiety and insomnia
Term
What would happen if you administered a non-selective MOA inhibitor while a patient was taking L-dopa?
Definition
They may have a life-threatening hypertensive crisis
Term
What is neuroleptic malignant syndrome?
Definition
A potentially life-threatening condition characterized by rigidity, confusion and hyperthermia

it is caused if there's abrupt withdrawal of l-dopa or other dopaminergic meds.
Term
What are some peripheral adverse effects of antimuscarinics?
Definition
dry mouth
urinary retention
constipation
blurred vision
Term
Describe spasticity.
Definition
increased tone, DTR & clonus
velocity dependent
asymmetric about the joints
Term
Describe the monosynaptic muscle stretch reflex arc
Definition
1. Muscle spindle is stimulated
2. Ia afferents synapse on motor neurons
3. they synapse on UMN which projects to the muscle causing it to contract
Term
How are spinal reflexes suppressed?
Definition
pyramidal UMN from the cortex suppress spinal reflexes by activating inhibitory interneurons in the spinal cord
Term
How does spasticity occur?
Definition
damage to UMN that inhibit the reflex --> hyperreflexia
Term
Baclofen - type, action, what it treats, effects
Definition
GABAb agonist
Increases spinal inhibition of motor neurone
CP, MS, Stroke
Sedation and weakness
Term
Tizanidine - type, action, what it treats, side effects
Definition
alpha 2 adrenoreceptor agonist
increases inhibition of spinal cord motor neurone
MS, ALS, stroke
sedation, weakness and hypotension
Term
Dantrolene - type, action, what it's used for, side effects
Definition
RyR1 Ca2+ channel antagonists in the sarcoplasmic reticulum of skeletal muscles
Reduces actin-myosin interaction, weakens skeletal msucl contraction
used for drug induced hyperthermia + CP, spinal cord injury and MS
side effect: weakness
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