Parkinson Disease Flashcards
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Sinemet
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carbidopa + levodopa
Class: dopamine replacement drug
Levodopa (prodrug) - is a precursor of dopamine.
Carbidopa - inhibits the enzyme dopa decarboxylase, preventing peripheral metabolism of Levodopa.
Indications: Parkinson Disease
MOA:
Dosage forms: IR tablet, ER tablet, ODT
Dosing:
Titrate cautiously.
-* IR (starting dose): 25/100mg PO TID
“What happens with advanced Parkinson’s, is that patients start to freeze up. So, what really would be the best, is to give a little bit of drug more often”.
Max dose:
Contraindications:
** Non-selective MAO inhibitors within 14 days, Narrow angle Glaucoma**
Warnings:
Side Effects:
Nausea, dizziness, orthostasis, dyskinesis, hallucinations, psychosis, xerostomia (dry mouth),
-** can cause brown, black or dark discoloring of urine, saliva or sweat and can discolor clothing**
-** Coombs test: if positive (+), discontinue drug (hemolysis risk).
- unusual sexual urges, priapism; also increases uric acid**
Monitoring:
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-** 70-100mg/day of Carbidopa is required to inhibit Dopa Decarboxylase.
-Long-term use can lead to fluctuations in response and dyskinesias
- DO NOT DISCONTINUE ABRUPTLY; must be tapered**
- GOLD Standard for treating Parkinson disease.
Drug-Drug/Food interactions:
-* separate from oral iron and high protein foods*
-** DO NOT USE with dopamine blockers (antagonists), which will worsen Parkinson symptoms (e.g. phenothiazines, metoclopramide)
- ** Contraindicated with Non-selective MAO inhibitors within 14 days ( a 2-week separation is required)
Dhivy
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carbidopa-levodopa
Class: dopamine replacement drug
Levodopa (prodrug) - is a precursor of dopamine.
Carbidopa - inhibits the enzyme dopa decarboxylase, preventing peripheral metabolism of Levodopa.
Indications: Parkinson Disease
MOA:
Dosage forms: ER tablet
Dosing:
Titrate cautiously.
- ER (starting dose): 50/200mg PO BID
ER tablet is scored and can be cut in half. DO NOT CRUSH or CHEW
Max dose:
Contraindications:
** Non-selective MAO inhibitors within 14 days, Narrow angle Glaucoma**
Warnings:
Side Effects:
Nausea, dizziness, orthostasis, dyskinesis, hallucinations, psychosis, xerostomia (dry mouth),
-** can cause brown, black or dark discoloring of urine, saliva or sweat and can discolor clothing**
-** Coombs test: if positive (+), discontinue drug (hemolysis risk).
- unusual sexual urges, priapism; also increases uric acid**
Monitoring:
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-** 70-100mg/day of Carbidopa is required to inhibit Dopa Decarboxylase.
-Long-term use can lead to fluctuations in response and dyskinesias
- DO NOT DISCONTINUE ABRUPTLY; must be tapered**
- GOLD Standard for treating Parkinson disease.
Drug-Drug/Food interactions:
-* separate from oral iron and high protein foods*
Duopa
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carbidopa-levodopa
Class: dopamine replacement drug
Levodopa (prodrug) - is a precursor of dopamine.
Carbidopa - inhibits the enzyme dopa decarboxylase, preventing peripheral metabolism of Levodopa.
Indications: Parkinson Disease
MOA:
Dosage forms: enteral suspension given via J-tube
*- Duopa cassettes: store in freezer, thaw in refrigerator prior to dispensing (good for 12 weeks upon refrigeration)
Dosing:
Titrate cautiously
- Is administered by a portal pump into the jejunum
Max dose:
Contraindications:
** Non-selective MAO inhibitors within 14 days, Narrow angle Glaucoma**
Warnings:
Side Effects:
Nausea, dizziness, orthostasis, dyskinesis, hallucinations, psychosis, xerostomia (dry mouth),
-** can cause brown, black or dark discoloring of urine, saliva or sweat and can discolor clothing**
-** Coombs test: if positive (+), discontinue drug (hemolysis risk).
- unusual sexual urges, priapism; also increases uric acid**
Monitoring:
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-** 70-100mg/day of Carbidopa is required to inhibit Dopa Decarboxylase.
-Long-term use can lead to fluctuations in response and dyskinesias
- DO NOT DISCONTINUE ABRUPTLY; must be tapered**
- GOLD Standard for treating Parkinson disease.
Drug-Drug/Food interactions:
-* separate from oral iron and high protein foods*
Rytary
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carbidopa-levodopa
Class: dopamine replacement drug
Levodopa (prodrug) - is a precursor of dopamine.
Carbidopa - inhibits the enzyme dopa decarboxylase, preventing peripheral metabolism of Levodopa.
Indications: Parkinson Disease
MOA:
Dosage forms: ER capsule
Dosing:
Titrate cautiously.
ER (starting dose): 50/200mg PO BID
Sustained Release capsules CAN be opened and sprinkled on a small amount of applesauce.
Max dose:
Contraindications:
** Non-selective MAO inhibitors within 14 days, Narrow angle Glaucoma**
Warnings:
Side Effects:
Nausea, dizziness, orthostasis, dyskinesis, hallucinations, psychosis, xerostomia (dry mouth),
-** can cause brown, black or dark discoloring of urine, saliva or sweat and can discolor clothing**
-** Coombs test: if positive (+), discontinue drug (hemolysis risk).
- unusual sexual urges, priapism; also increases uric acid**
Monitoring:
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-** 70-100mg/day of Carbidopa is required to inhibit Dopa Decarboxylase.
-Long-term use can lead to fluctuations in response and dyskinesias
- DO NOT DISCONTINUE ABRUPTLY; must be tapered**
- GOLD Standard for treating Parkinson disease.
Drug-Drug/Food interactions:
-* separate from oral iron and high protein foods*
Inbrija
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Levodopa
Class: dopamine replacement drug
Levodopa (prodrug) - is a precursor of dopamine.
Carbidopa - inhibits the enzyme dopa decarboxylase, preventing peripheral metabolism of Levodopa.
Indications: Parkinson Disease
MOA:
Dosage forms: capsule for oral inhaler
Used for as needed symptoms during off periods.
Dosing:
Titrate cautiously
Max dose:
Contraindications:
** Non-selective MAO inhibitors within 14 days, Narrow angle Glaucoma**
Warnings:
Side Effects:
Nausea, dizziness, orthostasis, dyskinesis, hallucinations, psychosis, xerostomia (dry mouth),
-** can cause brown, black or dark discoloring of urine, saliva or sweat and can discolor clothing**
-** Coombs test: if positive (+), discontinue drug (hemolysis risk).
- unusual sexual urges, priapism; also increases uric acid**
Monitoring:
Pearls/Notes:
-** 70-100mg/day of Carbidopa is required to inhibit Dopa Decarboxylase.
-Long-term use can lead to fluctuations in response and dyskinesias
- DO NOT DISCONTINUE ABRUPTLY; must be tapered**
- GOLD Standard for treating Parkinson disease.
Drug-Drug/Food interactions:
-* separate from oral iron and high protein foods*
Comtan
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entacapone
Class: COMT inhibitors
Indications: Parkinson Disease adjunctive therapy taken with Levodopa*
MOA: drug binds catechol-o-methyltransferase enzyme and inhibits it, preventing it from breaking down dopamine.
- this increases the duration of action of Levodopa
- drug binds to COMT to prevent peripheral conversion of Levodopa
** a decrease in Levodopa dose of 10-30% is usually necessary when adding a COMT inhibitor**
Dosage forms:
Dosing:
**200mg PO with EACH DOSE of carbidopa/levodopa
Max dose: 1600mg/day
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** decrease in Levodopa dose of 10-30% is usually necessary when adding on a COMT inhibitor**
- dyskinesias can occur earlier with COMT inhibitors
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Stalevo
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entacapone + carbidopa + levodopa
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carbidopa/levodopa in a ratio of 1:4 with 200mg of entacapone in each tablet. (ex. 12.5/50/200mg)
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Ongentys
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opicapone
Class: COMT inhibitor
Indications: Parkinson Disease adjunctive therapy taken with Levodopa
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50mg PO QDHS
- dose decrease needed in liver disease
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Tasmar
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tolcapone
Class: COMT inhibitor
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Rarely used due to Hepatotoxicity risk
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Mirapex
Mirapex ER
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pramipexole
Class: Dopamine Agonists
Indications: Parkinson Disease
IR formulation- also approved for (RLS) Restless Leg Syndrome.
MOA: drug acts similar to dopamine at the dopamine receptor
Dosage forms: IR/ER
Dosing:
*IR: start with 0.125mg PO TID, titrate weekly to MAX of 1.5mg TID
*ER: start with 0.375mg PO once daily, titrate weekly to MAX of 4.5mg daily
“If CrCl is less than < 50mL/min, then decrease dose” (90% renally excreted)
MAX dose: 4.5mg daily
Contraindications:
Warnings:
-* Somnolence (including sudden daytime sleep attacks), orthostasis, hallucinations, dyskinesias*, impulse control disorders
- postural deformity (e.g. bent spine, dropped head), rhabdomyolysis
Side Effects:
dizziness, nausea, vomiting, dry mouth, peripheral edema, constipation
Pearls/Notes:
-* A slow titration (no more than weekly) is required due to orthostasis, dizziness, sleepiness; DO NOT DISCONTINUE ABRUPTLY*
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Requip
Requip XL
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ropinirole
Class: Dopamine Agonists
Indications: Parkinson Disease
IR formulation- also approved for (RLS) Restless Leg Syndrome
MOA: drug acts similar to dopamine at the dopamine receptor
Dosage forms:
Dosing:
*IR- start with 0.25mg PO TID, titrate weekly to MAX of 8mg TID
*XL- start with 2mg PO once daily, titrate weekly to MAX of 24mg daily
MAX dose: 24mg daily
Contraindications:
Warnings:
-* Somnolence (including sudden daytime sleep attacks), orthostasis, hallucinations, dyskinesias*, impulse control disorders
Side Effects:
dizziness, nausea, vomiting, dry mouth, peripheral edema, constipation
Monitoring:
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-* A slow titration (no more than weekly) is required due to orthostasis, dizziness, sleepiness; DO NOT DISCONTINUE ABRUPTLY*
-* ropinirole is a substrate of CYP1A2; Caution with CYP1A2 inhibitors*
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Neupro
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rotigotine
Class: Dopamine Agonists
Indications: Parkinson Disease
- also approved for RLS
MOA: drug acts similar to dopamine at the dopamine receptor
Dosage forms: transdermal patch
Dosing: start with 2mg/24hours (early PD)
Max dose: 8mg/24 hours
Contraindications:
Warnings:
-* Somnolence (including sudden daytime sleep attacks), orthostasis, hallucinations, dyskinesias*, impulse control disorders
Side Effects:
dizziness, nausea, vomiting, dry mouth, peripheral edema, constipation,
hyperhidrosis
Pearls/Notes:
-* A slow titration (no more than weekly) is required due to orthostasis, dizziness, sleepiness; DO NOT DISCONTINUE ABRUPTLY*
- apply once daily at the same time each day to the stomach, thigh, hip, side of body or upper arm; DO NOT USE same site for at least 14 days
- Remove the patch before an MRI; do not apply a heat source over the patch; avoid if sensitivity/allergy to sulfites*
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Bromocriptine
dopamine agonist, but NO LONGER RECOMMENDED
Apokyn
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apomorphine
Class: dopamine agonist
Indications:
–* Used as a “rescue” movement drug for “off” periods*
MOA:
Dosage forms: injection
Dosing: [Must be started with a test dose in a medical office]— blood pressure drops very low very quickly.
Start with 0.2mL (2mg) SC as needed (up to 5x/day); titrate by 1mg every few days.
Max single dose: 0.6mL (6mg)
Lasts 45-90 minutes
Max dose:
Contraindications:
** DO NOT USE with 5-HT3 antagonists (e.g. ondansetron) due to severe hypotension and loss of consciousness**
Side Effects:
severe nausea/vomiting, hypotension, yawning, dyskinesias, somnolence, dizziness, QT prolongation
Monitoring:
Pearls/Notes:
- professor said is a SAD drug
- monitor supine and standing blood pressure
** For emesis prevention: Give (Tigan) trimethobenzamide 300mg PO TID, or similar antiemetic, started 3 days prior to the initial dose.
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Kynmobi
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apomorphine
Class: dopamine agonist
Indications:
- Used as a “rescue” movement drug for “off” periods
MOA:
Dosage forms: sublingual film
Dosing:
10-30mg as needed.
Max: 5 doses/day
Contraindications:
** DO NOT USE with 5-HT3 antagonists (e.g. ondansetron) due to severe hypotension and loss of consciousness**
Warnings:
Side Effects:
severe nausea/vomiting, hypotension, yawning, dyskinesias, somnolence, dizziness, QT prolongation
Monitoring:
Pearls/Notes:
- professor said is a SAD drug
- monitor supine and standing blood pressure
** For emesis prevention: Give (Tigan) trimethobenzamide 300mg PO TID, or similar antiemetic, started 3 days prior to the initial dose. NOT a 5-HT receptor blocker (antagonist)**.
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Gocovri
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amantadine
Class: dopamine reuptake inhibitor
Indications: Parkinson Disease
- is indicated for the treatment of dyskinesia in patients receiving levodopa-based therapy
MOA: drug blocks dopamine reuptake into presynaptic neurons and increases dopamine release from presynaptic fibers. Primarily used to treat dyskinesias associated with peak-dose of carbidopa/levodopa.
Dosage forms: ER capsules
Dosing:
- 137mg (one capsule) once daily at bedtime for one week, then may increase to 2 capsules (274mg) once daily at bedtime thereafter. (Not interchangeable with other IR or ER amantadine products).
- Decrease dose in renal impairment; If eGFR < 15mL/min/1.73^m2, ER products are Contraindicated.
Max dose:
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Warnings:
* Somnolence (including falling asleep without warning during activities of daily living), compulsive behaviors, psychosis* (hallucinations, delusions, paranoia)
Side Effects:
*dizziness, orthostatic hypotension, syncope (fainting), insomnia, abnormal dreams, dry mouth, constipation
Cutaneous reaction called *livedo reticularis (reddish skin mottling - can require drug discontinuation)
Monitoring:
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Gocovri— is indicated for the treatment of dyskinesia in patients receiving Levodopa based therapy.
Drug-Drug/Food interactions:
Osmolex ER
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amantadine ER
Class: dopamine reuptake inhibitor
Indications: Parkinson Disease
MOA: drug blocks dopamine reuptake into the presynaptic neurons and increases dopamine release from presynaptic fibers. Primarily used to treat dyskinesias associated with peak-dose of carbidopa/levodopa.
Dosage forms: ER tablets
Dosing:
- take one tablet (129mg) by mouth once daily in the morning for 1 week, then make increase weekly to max dose of 322mg daily.
Max dose: 322mg
Contraindications:
Warnings:
- **Somnolence (including falling asleep without warning during activities of daily living), compulsive behaviors, psychosis (hallucinations, delusions, paranoia).
Side Effects:
- **Dizziness, orthostatic hypotension, syncope, insomnia, abnormal dreams, dry mouth, constipation
- cutaneous reaction called livedo reticularis (reddish skin mottling- can require drug discontinuation)
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Eldepryl
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selegiline
Class: Selective MAO-B inhibitor, anti-Parkinson agent
Indications: Parkinson Disease
MOA: drug binds to the MAO-B enzyme and blocks the breakdown of dopamine which increases dopaminergic activity.
– primarily used as adjunctive treatment to carbidopa/levodopa
Dosage forms:
Dosing:
capsule/tablet: 5mg by mouth BID with breakfast and lunch.
** Selegiline can be activating; DO NOT take dose at bedtime; if does twice daily, take 2nd dose at midday**
ODT: 1.25-2.5mg daily (not recommended if CrCl < 30mL/min)
Max dose:
Contraindications:
** Use in combination with other MAO inhibitors (including linezolid), opioids, SNRIs, TCAs, SSRIs, **
Warnings:
** Serotonin Syndrome, hypertension, nausea, CNS depression, dyskinesias, impulse control disorders, caution in patients with psychotic disorders (may exacerbate) **.
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- selegiline is activating; DO NOT take dose at bedtime, if dosed BID take the 2nd dose midday.
Drug-Drug/Food interactions:
- **foods high in tyramine (pickled, aged cheese, wine, fermented, smoked meats, beer, organ meats). **
- anything that contains dopamine, tyrosine, phenylalanine (sweetener), tryptophan or caffeine, 5HT syndrome
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Emsam
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selegiline patch
only indicated for depression
Zelapar
selegiline
ODT tablet