Term
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Definition
Dopamine Analogue
Used to treat Parkinson's. Can cross the blood brain barrier, but is actively converted into Dopamine in the periphery by AADC - Aromatic Aminoacid Decarboxylase (dopamine decarboxylase) in the GI.
Toxicity:
1. "On and Off phenomenon" due to both tolerance and sensitization to the drug.
2. Dyskinesia: Uncontrollable rhythmic movements of head, trunks, and limbs. Linked to drug dosing. Likely at maximal doses.
used with Carbidopa |
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Term
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Definition
Dopamine analogue that inhibits AADC/dopamine decarboxylase.
Prevents the conversion of levodopa in the periphery.
Used with Levodopa |
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Term
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Definition
D2 Agonist
Found to cause fibrosis of cardiac valves |
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Term
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Definition
D1 and D2 agonist
Used for parkinson's disease. Do not require enzymatic conversion by Dopa Decarboxylase. They are non-peptide and can cross the BBB.
Major Limitations: Nausea, peripheral edema, hypotension, and ADVERSE cognitive effects
Dopamine Dysregulation Syndrome - impaired impulse control -- compulsive behavior.
Tox: Found to cause fibrosis of cardiac valves |
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Term
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Definition
D3>D2 Agonists.
Used for parkinsons. Do not require enzymatic conversion by Dopa Decarboxylase. They are non-peptide and can cross the BBB.
Major Limitations: Nausea, peripheral edema, hypotension, and ADVERSE cognitive effects
Dopamine Dysregulation Syndrome - impaired impulse control -- compulsive behavior. |
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Term
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Definition
MAO-B inhibitor - prevents dopamine degredation and formation of free radicals
Used: Parkinson's Disease
Tox: forms toxic metabolite Amphetamine -- sleeplessness and confusion |
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Term
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Definition
MAO-B inhibitor - prevents degredation of Dopamine and formation of free radicals
DOES NOT form amphetamine |
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Term
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Definition
COMT inhibitor
decreases peripheral metabolism of levodopa and make more levodopa available in the CNS
***Can cross the BBB
Tox: FATAL hepatic toxicity |
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Term
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Definition
COMT inhibitor
prevents degredation of dopamine
decreases peripheral metabolism of levodopa and make more levodopa available in the CNS
***Distributes only in the periphery |
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Term
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Definition
1. M2 inhibitor in influenze to prevent viral uncoating.
2. NMDA receptor antagonist
Use: to treat Levodopa induced Dyskinesias that develop late in the course of the disease |
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Term
Trihexyphenidyl
Benztropine |
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Definition
MOA: Muscarinic Antagonists that reduce cholinergic tone in the CNS
Use: Reduce TREMORS in parkinsons MORE than bradykinesia.
Tox: Dry mouth, urinary retention, IMPAIRMENT OF MEMORY AND COGNITION |
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Term
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Definition
MOA: Phenothiazine Antipsychotic that blocks D2 receptors in the Mesolimbics
Lipophillic and can cross BBB
Use: schizophrenia (positive symptoms)
1. Extrapyramidal effects - parkinsonian symptoms (can be treated with amantadine).
2. Neuroleptic Malignant Syndrome - life threatening Catatonia, stupor, fever, and autonomic instability; myoglobinemia and death - CAN ALSO BE SEEN IN PATIENTS WHO ABRUPTLY DISCONTINUE DOPAMINE MEDS
3. TARDIVE DYSKINESIA - abnormal movements with repetitive involuntary stereotyped movements of the face, arms and trunk--due to prolonged treatment due to drugs with high affinity for D2.
---exacerbated by antiparkinson drug
---ameliorated by removing drug
4. PROLACTINEMIA
5. antagonism of muscarinic receptors
6. Antagonism of alpha-adrenergic receptors (depends on potency, higher potency, less effects)
7. Can worsen Parkinson symptoms if administered to patients with parkinson's disease -- inhibits levodopa and dopa agonists. |
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Term
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Definition
MOA: Butyrophenone antipsychotic blocking D2 receptors in the Mesolimbics.
Lipophillic and can cross BBB
Use: Schizophrenia (positive symptoms)
Tox:
1. Extrapyramidal effects - parkinsonian symptoms (can be treated with amantadine).
2. Neuroleptic Malignant Syndrome - life threatening Catatonia, stupor, fever, and autonomic instability; myoglobinemia and death - CAN ALSO BE SEEN IN PATIENTS WHO ABRUPTLY DISCONTINUE DOPAMINE MEDS
3. TARDIVE DYSKINESIA - abnormal movements with repetitive involuntary stereotyped movements of the face, arms and trunk--due to prolonged treatment due to drugs with high affinity for D2.
---exacerbated by antiparkinson drugs
---ameliorated by removing drug
4. PROLACTINEMIA
5. Antagonism of muscarinic receptors
6. Antagonism of alpha adrenergic receptors (depends on potency, higher potency, less effects)
7. Can worsen Parkinson symptoms if administered to patients with parkinson's disease -- inhibits levodopa and dopa agonists. |
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Term
Risperidone
Clozapine
Olanzapine
Quetiapine
Ziprasidone
Aripiprazone |
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Definition
MOA: Atypical antipsychotics - low affinity for D2, antagonist action at both 5-HT2 and D2 receptors.
Use: to treat NEGATIVE symptoms of Schizophrenia. |
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Term
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Definition
Atypical Antipsychotic with distinc pharmacology.
Binds D1-D5, 5-HT2, and Alpha 1, H1, and muscarinic receptors.
Used: patients who have failed all other antipsychotic drugs.
Tox: Agranulocytos!!! Seizures. |
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Term
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Definition
Antipsychotic used in Parkinson's because it does not exacerbate the motor features of the disease.
Can also manage dementia |
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