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Parkisons drugs
2nd to last drugs pharm exam 3
16
Medical
Professional
02/16/2013

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Cards

Term
amantadine
Definition
Adjunct with Sinemet
unknown mechanism; anti-viral

May cause livodo reticularis (skin looks like when its cold)

avoid patients SEIZURE and HF
Term
apomorphine
Definition
Potent non-selective DA agonist

delivered subcutaneously, rapidly distributed through blood to CNS, benefit in 10 minutes, lasts 2 hours

horrible nausea and very poorly tolerated treat with anti-emetic trimethybenzamide
Term
benztropine
Definition
Muscarinic receptor antagonsit: balances ach/DA ratio

may reduce tremor
SE: dry mouth,tachycardia, SOME POTENTIAL FOR ABUSE
Term
bromocriptine
Definition
Ergot - Based DA Agonists (D2)
excreted in bile and feces

Do not require metabolic conversion and can be used as monotherpy BUT
HAS OFF TARGET EFFECTS INCLUDING NAUSEA, INSOMNIA, DAYTIME SLEEPYNESS
Term
carbidopa
Definition
Dopa decarboxylase inhibitors
Does not cross BBB
inhibits nausea and cardia effects LDOPA

LDOPA never given without
Term
entacapone
Definition
Catechol-O-Methyl Transferase (COMT)
Inhibitors: upregulated with use of dopa decarboxylase inhibitors

nausea, orange-colored urine, orthostatic
hypotension, dyskinesia, hallucination, sleep disordersmainly
Term
levodopa
Definition
L-Dopa; Prodrug dopamine
DA does not cross B3 Even if it did,
peripheral side effects likely intolerable

gold standard works well 1/3, ok 1/3

Clinical efficacy decreases with
time

competes with amino acids for uptake therfore must give 50X needd
2/3 excreted as homovanilla acid urine

GI DISTURBANCES PROFOUND AVOID PROMETHAZINE ANTIEMETIC (abdominal involentary movements)

psycomimetic

DRUG HOLIDAY NOT RECOMMENDED
NO MAOI --> HYPERTENSIVE CRISIS
Term
pramipexole
Definition
partial D3 agonist
Anti-oxidant free radical scavanger
RENAL SECRETION


relief on/off in l-dopa therapy
Term
ropinirole
Definition
Greatest affinity D2
CYP450 metabolism!

relief on/off in l-dopa therapy
Term
selegeline
Definition
selective (at therapeutic doses), irreversible MAOB (targets dopamine) inhibitor

Side effects: mood elevating, nausea, dry mouth, confusion,
adverse reactions with meperidine, TCAs, and SSRIs

MAY REDUCE LIFE SPAN
Term
Subtype 1 Parkinsons
Definition
Tremor predominant
occurs approximately 40
more marked impairment first DX
slower cognitive progression
Term
subtype 2
Definition
Postural imbalance and gait disorder
>70 years old at diagnosis
Akinesia, rigidity, gait/ balance impairment
Rapid decline, cognitive complications more prevalent
Term
Circuit parkinsons D1/D2
Definition
D1 = excitory
D2 = inhibitory

D2>D1 PD

oldschool ACH>D1
Term
Sinemet
Definition
L-Dopa/Carbadopa
Term
Stalevo
Definition
carbidopa/l-dopa/entacapon
Term
DA Agonist Adverse Effects
Definition
GI: Anorexia, Nausea, Vomiting, Constipation, Reflux
Esophagitis, Peptic Ulcer Bleeding

Cardiovascular: Postural hypotension, Vasospasm (ergot
agents), Cardiac arrhythmia

Dyskinesia: probably associated with increased L-Dopa
delivery to CNS and/or off-target (non-striatal) effects

Mental disturbance: reports of amplified impulsive behavior
(shopping, gambling, cross-dressing), psychotomimetic at
higher doses

AVOID PERIPHERAL VASCULAR DISEASE
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