Term
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Definition
-absorbed from gut (urine excreted), crosses BBB, decarboxylated to DA
-carbidopa prevents peripheral deCO (prevents conversion to E and NE)
-increases life span
-bradykinesia, rigidity, and tremor respond immediately
-flat affect and gait- less responsive
SE
-b-adrenergic effects (tachycardia, cardiac arrythmias, hypertension)
-OH
-GI
-tolerance develops in a few weeks (rare)
Major SE effecting quality of life
1)"wearing-off" or "on-off" effects- receptor supersensitivity--> freezing
2)"peak does" SEs- grimacing, abnormal movements of the face and tongue (dyskinesia)
3) behavioral SE (20-25% of patients)- psychosis, confusion, hallucination, anxiety, delusion, inappropriate sexual behavior
4) dementia |
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Term
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Definition
-DA agonist
*Used in "frozen" cases (Reverses "off" state) |
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Term
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Definition
*D2 agonist/ D1 antagonist (older gen- ergot derivative)
-Short half-life of 4-6 Hs (liver)
• Low GI absorption (28%)
• Only 6% reach to blood (max concentration in blood at ~2 Hs)
**Primary use: adjunctive therapy with L-DOPA (lets us use less L-DOPA at one time)
• Only works in patients responsive to L-DOPA
• Titrate slowly (start with low dose 1.25 mg, and no more than 5 mg/first week)
SE: N/V= medicate with meals, OH and cardiac arrhythmia (b-adrenergic effects on heart conduction system), contraindicated for women who are pregnant or breast feeding, depression, anxiety, hallucinations |
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Term
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Definition
-potent D2&D1 agonist (older drug gen- ergot derivative)
*Withdrawn from market due to heart valve regurgitation |
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Term
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Definition
*D2 receptor agonist: newer drug (non-ergot derivatives)
• Most effective in early mono-therapy
• Good GI absorption with a peak effect ~2 Hs from intake
• Half-life of 8-14 Hs (kidney)
• Also used in adjunctive therapy: its reduces L-DOPA “on-off” effects by ~25%
SE: N/V= medicate with meals, contraindicated for women who are pregnant or breast feeding, depression, anxiety, hallucinations |
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Term
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Definition
*D2 receptor agonist: newer drug (non-ergot derivatives)
• Short half-life of 3-4 Hs (liver)
• Most effective in early mono-therapy with good GI absorption (~to Pramipexole)
• Also used in adjunctive therapy
SE: N/V= medicate with meals, contraindicated for women who are pregnant or breast feeding, depression, anxiety, mostly hallucinations |
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Term
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Definition
*MAO-B inhibitor - prevents catabolism of DA and enhances DA in brain
• Early mono-therapy (e.g., 10 mg/day) or in combination with L-DOPA
• Improves cognitive functions associated with PD (early stages)
*Adjunctive therapy when L-DOPA effects start to decline (DON'T use it alone- helps with not having to increase the level of L-DOPA needing to be given)
• Good GI absorption. It reaches quickly to the CNS
• Peak concentration in blood within 1 hour of administration
• Half-life of 1.5 hour (liver)
• Reduce off-time
• Drug contraindications
a. tricyclic anti-depressants
b. serotonin reuptake inhibitors (Prozac)
SE: insomnia,dyskinesia, nausea, headache, cardiac arrhythmias, hypertension |
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Term
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Definition
MOA: blocks viral penetrating/uncoating (M2 protein) & release of DA from intact nerve terminals
-Prophylaxis and treatment for influenza A; Parkinson's disease
-Toxicities: ataxia, dizziness, slurred speech
"A Man to dine" takes off his coat
(Rimantidine is a derivative with fewer CNS side effects. Does not cross the BBB)
**Primary use: PD exhibiting bradykinesia as its primary symptom & early onset of PD (young population)
1. An anti-viral agent introduced in 1969 to treat PD bradykinesia and ridigity
2. Relatively effective to attenuate dyskinesia and motor fluctuations
- Adjunctive therapy, often to reduce L-DOPA-induced motor side effects
- Not effective to attenuate PD tremor
3. It enhances DA release or blocks DA re-uptake
4. Anticholinergic action: muscarinic receptor antagonist
5. NMDA receptor antagonist
6. Half-life: 9-13 hours
SE: N/V, contraindicated for women who are pregnant or breast feeding |
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Term
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Definition
*inhibits CNS and peripheral COMT
-Primary use in patients whose have received prolonged L-DOPA/Carbidopa treatment for 5-7 years + motor side effects induced by L-DOPA
1)Adjunctive therapy, often late in disease progression
-Effective in patients that develop “freezing”
-Primary use to ameliorate peak dose dyskinesia
2)Reduce L-DOPA-induced motor side effects
3)Attenuates the “wearing-off” time
4)Reduce the clearance of L-DOPA by enhancing its bioavailability
5)Enable lowering the dose of L-DOPA by 25-30% (Tolcapone)
6)Prolongs L-DOPA therapeutic action (I.e., motor symptoms)
*fetal hepatotoxicity |
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Term
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Definition
*inhibits peripheral COMT only
-Primary use in patients whose have received prolonged L-DOPA/Carbidopa treatment for 5-7 years + motor side effects induced by L-DOPA
1)Adjunctive therapy, often late in disease progression
-Effective in patients that develop “freezing”
-Primary use to ameliorate peak dose dyskinesia
2)Reduce L-DOPA-induced motor side effects
3)Attenuates the “wearing-off” time
4)Reduce the clearance of L-DOPA by enhancing its bioavailability
5)Enable lowering the dose of L-DOPA by 25-30% (Tolcapone)
6)Prolongs L-DOPA therapeutic action (I.e., motor symptoms) |
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Definition
*Treats Tourette's Syndrome
**Neuroleptic
-most effective but has large SE profile |
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Term
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Definition
*Treats Tourette's Syndrome
*a-2 agonist
-titrate slowly at low doses- patient must have normal blood pressure |
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Term
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Definition
*GABA-B receptor agonist (used to help with spasticity)
**Used to treat Amyotrophic Lateral Sclerosis (ALS)
-prolongs time before tracheostomy |
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Term
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Definition
*Reduces glutamate release
**Used to treat Amyotrophic Lateral Sclerosis (ALS)
-prolongs time before tracheostomy |
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Term
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Definition
*Anti-convulsant
**Used to treat benign essential tremor (inherited)
-abuse potential |
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Term
| Drugs that cause Parkinson-like syndrome |
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Definition
| Haloperidol, chlorpromazine, reserpine, metoclopramide |
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Term
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Definition
-INC in schizophrenia
-DEC in PD and depression
-Location of synthesis= Ventral tegmentum and SNc |
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Term
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Definition
*PD= DEC DA, INC ACh
*Schizophrenia= INC DA
*Huntington's disease= DEC GABA, DEC ACh
*Alzheimer's disease= DEC ACh
*Depression= DEC NE, DEC Seratonin (5-HT), DEC DA
*Anxiety= INC NE, DEC GABA, DEC Seratonin (5-HT) |
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Term
| Parkinson's disease (nigrostriatal dopamine depletion) |
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Definition
**resting tremor, rigidity, akinesia (loss or impairment of the power of voluntary movements), postural instability
**eosinophilic cytoplasmic inclusion in nerve cell= lewy body (Parkinson's disease) |
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Term
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Definition
*Drug-induced syndrome
-Butyrophenones
-Phenothiazines
-Bromocriptine
**Typical symptoms are oral-facial dyskinesias
-Long-lasting and persists even after withdrawal of the drug.
-Most common treatment: decrease the dose of the neuroleptic drug
--very often associated with D2 receptor antagonists |
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