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
Trihexyphenidyl (Artane) Class
Anticholinergics
Trihexyphenidyl (Artane) Therapeutics
Tremor and drooling in Parkinson’s, and really only used if drooling is a major problem (otherwise, very bad mental symptoms)
Trihexyphenidyl (Artane) SE
- Confusion, impaired memory, hallucinations
2. Typical anticholinergic (dry mouth, etc)
Trihexyphenidyl (Artane) Misc.
Contraindicated in demented Parkinson’s; abrupt discontinuation causes exacerbation of symptoms
Amantadine (Symmetrel) Class
Anti-viral
Amantadine (Symmetrel) MOA
Dopaminergic, anticholinergic, anti-NMDA
Amantadine (symmetrel) Therapeutics
Mild early Parkinson’s (2nd-line); best as an adjunct to levodopa/carbidopa for long-term treatment; movement disorders in Huntingtons; only adjunct that reduces dyskinesias
Amantadine (Symmetrel) SE
- DA side effects, edema, psychosis, NMS upon withdrawal
Amantadine (Symmetrel) Misc
Excreted unchanged in urine (renal dysfunction requires lower dose); contraindicated in elderly with dementia (anticholinergic effects)
Deep Brain Stimulation Class
Surgery
Deep Brain Stimulation MOA
Hits subthalamic nucleus
Deep Brain stimulation Therapeutics
Treatment for motor fluctuations or dyskinesias refractory to other medications; reduces ‘off’ time, may reduce levodopa dosage
Deep Brain Stimulation SE
- Fatal intracerebral hemorrhage, cognitive impairment
Deep Brain Stimulation Misc
Patients must still be sensitive to levodopa therapy (or they aren’t a candidate)
Chlorpromazine (Thorazine) Class
First-generation antipsychotics (phenothiazine)
Chlorpromazine (Thorazine) MOA
Catalepsy (trance, muscle rigidity, lack of voluntary movement)
Chlorpromazine (Thorazine) Therapeutics
Schizophrenia (hallucinations, delusions), movement disorder in Huntingtons
Chlorpromazine (Thorazine) SE
- NMS
- Extrapyramidal, tardive dyskinesia; sedation, postural hypotension, weight gain, anticholinergic effects; sexual dysfunction, hyperprolactinemia
Chlorpromazine (Thorazine) Misc.
Little effect on negative symptoms
Fluphenazine (Prolixin) Class
First-generation antipsychotics (phenothiazine)
Trifluoperazine (Stelazine) Class
First-generation antipsychotics (phenothiazine)
Perphenazine (Trilafon) Class
First-generation antipsychotics (phenothiazine)
Thioridazine (Mellaril) Class
First-generation antipsychotics (phenothiazine)
Haloperidol (Haldol) Class
First-generation antipsychotics (phenothiazine)
Fluphenazine (Prolixin) MOA
Catalepsy (trance, muscle rigidity, lack of voluntary movement)
Trifluoperazine (Stelazine) MOA
Catalepsy (trance, muscle rigidity, lack of voluntary movement)
Perphenazine (Trilafon) MOA
Catalepsy (trance, muscle rigidity, lack of voluntary movement)
Thioridazine (Mellaril) MOA
Catalepsy (trance, muscle rigidity, lack of voluntary movement)
Haloperidol (Haldol) MOA
Catalepsy (trance, muscle rigidity, lack of voluntary movement)
Fluphenazine (Prolixin) Therapeutics
Schizophrenia (hallucinations, delusions), movement disorder in Huntingtons
Trifluoperazine (Stelazine) Therapeutics
Schizophrenia (hallucinations, delusions), movement disorder in Huntingtons
Perphenazine (Trilafon) Therapeutics
Schizophrenia (hallucinations, delusions), movement disorder in Huntingtons
Thioridazine (Mellaril) Therapeutics
Schizophrenia (hallucinations, delusions), movement disorder in Huntingtons
Haloperidol (Haldol) Therapeutics
Schizophrenia (hallucinations, delusions), movement disorder in Huntingtons
Fluphenazine (Prolixin) SE
- NMS
- Extrapyramidal (more than chlorpromazine), tardive dyskinesia; sedation (less than chlorpromazine), hypotension, anticholinergic effects; sexual dysfunction, hyperprolactinemia
Fluphenazine (Prolixin) Misc
Little effect on negative symptoms
Trifluoperazine (Stelazine) SE
- NMS
2. Extrapyramidal, tardive dyskinesia; sexual dysfunction, hyperprolactinemia
Trifluoperazine (Stelazine) Misc
Little effect on negative symptoms
Perphenazine (Trilafon) SE
- NMS
- Extrapyramidal (less than chlorpromazine), tardive dyskinesia; sedation (less than chlorpromazine); sexual dysfunction, hyperprolactinemia
Perphenazine (Trilafon) Misc
Little effect on negative symptoms
Thioridazine (Mellaril) SE
- NMS
2. Extrapyramidal, tardive dyskinesia; sexual dysfunction, hyperprolactinemia
Thioridazine (Mellaril) Misc
Little effect on negative symptoms
Haloperidol (Haldol) SE
- NMS
- Extrapyramidal (more than chlorpromazine), tardive dyskinesia; sedation (less than chlorpromazine), hypotension, anticholinergic effects; sexual dysfunction, hyperprolactinemia
Haloperidol (Haldol) Misc
Little effect on negative symptoms
Tetrabenazine (Xenazine) MOA
Dopamine-depleting, VMAT2 inhibitor
Tetrabenazine (Xenazine) Therapeutics
Movement disorder in Huntingtons; tardive dyskinesia
Tetrabenazine (Xenazine) SE
NMS
Dantrolene (Dantrium) Therapeutics
Malignant hyperthermia (associated with NMS)
Dantrolene (Dantrium) MOA
Muscle relaxant
Clozapine (Clozaril) Class
Second-Generation Antipsychotics (tricyclic)
Clozapine (Clozaril) MOA
D2 receptor antagonist, 5HT2 receptor antagonist
Clozapine (Clozaril) Therapeutics
Treatment-resistant psychoses (including schizophrenia); decreases risk of suicide; can be used in pregnancy
Clozapine (Clozaril) SE
- Agranulocytosis; weight gain, type II DM, seizure risk, hyperlipidemia
- Akathesia (rare, at high doses); GI hypomotility; myocarditis
Clozapine (Clozaril) Misc
No catalepsy, no EPS, no TD
Olanzapine (Zyprexa) Class
Second-Generation Antipsychotics (tricyclic)
Olanzaprine (Zyprexa) MOA
D2 receptor antagonist, 5HT2 receptor antagonist
Olanzaprine (Zyprexa) Therapeutics
Schizophrenia (effective against positive symptoms, modest effect on negative); severe bilpolar
Olanzapine (Zyprexa) SE
- Metabolic complications (weight gain, hyperglycemia, type 2 DM, hyperlipidemia)
- Somnolence, dizziness, increased serum hepatic transaminases, postural hypotension, constipation; EPS, hyperprolactinemia, akathesia may occur
Quetiapine (Seroquel) Class
Second-Generation Antipsychotics (tricyclic)
Quetiapine (Seroquel) MOA
D2 receptor antagonist, 5HT2 receptor antagonist
Quetiapine (Seroquel) Therapeutics
Schizophrenia (effective against positive symptoms, modest effect on negative)
Quetiapine (Seroquel) SE
- Weight gain, hyperglycemia, postural hypotension, constipation, somnolence, dizziness
Risperidone (Risperdal) Class
Second-Generation Antipsychotics (non-tricyclic)
Risperidone (Risperdal) MOA
D2 receptor antagonist, 5HT2 receptor antagonist
Risperidone (Risperdal) Therapeutics
Schizophrenia (effective against positive symptoms, modest effect on negative); severe bilpolar
Risperidone (Risperdal) SE
- Weight gain, hyperglycemia, postural hypotension, constipation, insomnia, dizziness, hyperprolactinemia; EPS at greater doses
Risperidone (Risperdal) Misc
Less metabolic complications
Ziprazidone (Geodon) Class
Second-Generation Antipsychotics (non-tricyclic)
Ziprazidone (Geodon) MOA
D2 receptor antagonist, 5HT2 receptor antagonist
Ziprazidone (Geodon) Therapeutics
Schizophrenia (effective against positive symptoms, modest effect on negative)
Ziprazidone (Geodon) SE
- Somnolence, cardiac arrhythmias (QTc prolongation); EPS in 5%Fewer metabolic comlications
Ziprazidone (Geodone) Misc
Fewer metabolic complications
Aripiprazole (Abilify) Class
Second-Generation Antipsychotics (non-tricyclic)
Aripiprazole (Abilify) MOA
Partial D2 and D3 receptor agonist, partial 5HT1a agonist, 5HT2a antagonist
Aripiprazole (Abilify) Therapeutics
Not as effective as other atypicals and typicals at treating schizophrenia; severe bipolar