CNS 1 and 2 Flashcards
Levodopa (L-DOPA) (Dopar) Class
Dopamine precursor
Levadopa (L-DOPA) MOA
Oral, absorbed in small bowel
Levadopa (L-DOPA) Therapeutics
Given with carbidopa; first-line treatment for Parkinson’s unless patient is young (want to delay as long as possible)
Levadopa (L-DOPA) Important SE
Hallucinations, dyskinesias; on-off phenomenon, neuroleptic malignant syndrome (NMS)*, psychosis possible with chronic use
Levadopa other SE
Nausea/GI distress, hypotension, dizziness
Levadopa Misc
Given with carbidopa; may accelerate PD progression; relatively short half-life (3 hours)
Carbidopa (Lodosyn) Class
Aromatic amino acid decarboxylase inhibitor
Carbidopa (Lodosyn) MOA
Inhibits peripheral conversion of L-DOPA to dopamine; does not cross BBB
Bromocriptine (Parlodel) Class
Ergot Derivative
Rasagiline (Azilect) Class
MAO-b inhibitor
Deep Brain Stimulation Misc
Patients must still be sensitive to levodopa therapy (or they aren’t a candidate)
Haloperidol (Haldol) Class
First-generation antipsychotics (phenothiazine)
Haloperidol (Haldol) Therapeutics
Schizophrenia (hallucinations, delusions), movement disorder in Huntingtons
Haloperidol (Haldol) Misc
Little effect on negative symptoms
Carbidopa (Lodosyn) Therapeutics
Parkinson’s (given with Levadopa)
Carbidopa (Lodosyn) Important SE
Dyskinesias, on-off phenomenon, neuroleptic malignant syndrome (NMS), psychosis possible with chronic use
Carbidopa (Lodosyn) Misc
MAO-A inhibitors are contraindicated (except MAO-B, which only hits DA)
Bromocriptine (Parlodel) MOA
D2 agonist, D1 antagonist
Bromocriptine (Parlodel) Therapeutics
Mild Parkinson’s; DA agonism in NMS; hyperprolactinemia
Bromocriptine (Parlodel) SE
- Pleural effusions, cough, shortness of breath, pulmonary fibrosis
- Peripheral DA-like effects
Bromocriptine (Parlodel) Misc
Must be titrated slowly due to hypotension
Pramipexole (Mirapex) Class
Non-ergot DA
Pramipexole (Mirapex) MOA
Selective D2 agonist
Pramipexole (Mirapex) Therapeutics
Mild Parkinson’s (first-line); to delay L-dopa treatment, usually in combination with ropinorole
Pramipexole (Mirapex) SE
- More acute: psychosis, nausea/GI, edema, compulsive behavior (nucleus accumbens, D3)
Pramipexole (Mirapex) Misc.
Less effective with motor symptoms of PD
Apomorphine (Apokyn) Class
Non-ergot DA
Apomorphine (Apokyn) Therapeutics
Rescue therapy for ‘off’ periods (immobility)
Apomorphine (Apokyn) SE
- Psychosis, drowsiness, hypersexuality (increase in erections); emesis (pre-administer trimethobenzamide or domiperidone); hypotension with serotonin receptor antagonists
- Peripheral DA effects
Apomorphine Misc
Injectable only; serotonin receptor antagonists contraindicated (e.g., ondansetron)
Entacapone (Comtan) Class
COMT Inhibitor
Entacapone (Comtan) MOA
Prevents breakdown of DA
Entacapone (Comtan) Therapeutics
Prolong half-life of levodopa, reduce ‘off’ time; primarily works peripherally
Entacapone (Comtan) SE
- Increase in dyskinesias, diarrhea, urine discoloration
2. DA SE
Entacapone Misc
Short-acting (2 hours)
Selegiline (Eldepryl) CLass
MAO-B inhibitor
Selegiline (Eldepryl) MOA
Prevents breakdown of DA
Selegiline (Eldepryl) Therapeutics
Mild early Parkinson’s (monotherapy); may delay onset of levodopa therapy
Selegiline (Eldepryl) SE
- Hypotension, GI distress, dyskinesia, psychosis
2. N/V
Selegiline (Eldepryl) Misc
Antidote to environmental toxins; contraindications: decongestants, dextromethorphan, St. John’s wort, analgesics, methadone, tramadol, propoxyphene; caution with SSRIs, MAO-A inhibitors
Rasagiline (Azilect) Class
MAO-b inhibitor
Rasagiline (Azilect) MOA
Prevents breakdown of DA
Rasagiline (Azilect) Therapeutics
Mild early Parkinson’s (monotherapy); may delay onset of levodopa therapy; also, as an adjunct with levodopa (reduces ‘off’ time)
Rasagiline (Azilect) SE
- Hypotension, GI distress, dyskinesia, psychosis
2. N/V
Rasagiline (Azilect) Misc.
Contraindications: decongestants, dextromethorphan, St. John’s wort, analgesics, methadone, tramadol, propoxyphene; caution with SSRIs, MAO-A inhibitors
Benztropine (Cogentin) Class
Anticholinergics
Benztropine (Cogentin) Therapeutics
Tremor and drooling in Parkinson’s, and really only used if drooling is a major problem (otherwise, very bad mental symptoms)
Benztropine (Cogentin) SE
- Confusion, impaired memory, hallucinations
2. Typical anticholinergic (dry mouth, etc)
Benztropine (Cogentin) Misc
Contraindicated in demented Parkinson’s; abrupt discontinuation exacerbates symptoms