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:
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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*
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*
Drug-Drug/Food interactions:
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:
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 (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
-
Emsam
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selegiline patch
only indicated for depression
Zelapar
selegiline
ODT tablet
Azilect
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rasagiline
Class: Selective MAO-B inhibitor
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- rasagiline is a substrate for CYP1A2. Limit dose to 0.5mg daily with ciprofloxacin and other CYP1A2 inhibitors.
Drug-Drug/Food interactions:
** Do NOT eat food high in tyramine, including aged or matured cheese, air-dried or cured meats (e.g. sausages, salamis), sauerkraut, fava or broad bean pods, tap/draft beers. soy sauce or other soybean condiments.
**- Do NOT use with products containing dopamine, tyrosine, phenylalanine, tryptophan or caffeine.
Xadago
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safinamide
Class: Selective MAO-B inhibitor
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** severe hepatic impairment**
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visual changes
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Cogentin
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benztropine
Class: centrally-acting anticholinergic
Indications: primarily used for tremor in early PD.
MOA: drug gas anticholinergic and antihistamine effects
Dosage forms:
Dosing:
0.5 - 2mg TID (start everyday at bedtime)
Max dose:
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Side Effects:
**High incidence of peripheral and central anticholinergic effects: dry mouth, constipation, urinary retention, blurred vision, mydriasis, somnolence, confusion,
Monitoring:
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*- DO NOT USE in elderly**.
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trihexyphenidyl
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Class: centrally-acting anticholinergic
Class: centrally-acting anticholinergic
Indications: primarily used for tremor in early PD.
MOA: drug gas anticholinergic and antihistamine effects
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**High incidence of peripheral and central anticholinergic effects: dry mouth, constipation, urinary retention, blurred vision, mydriasis, somnolence, confusion,
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*- DO NOT USE in elderly**.
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Nourianz
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istradefylline
Northera
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droxidopa
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-used for neurogenic orthostatic hypotension in PD
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Parkinson Disease:
- is a neurological disorder.
- usually develops after age 65, although 15% of cases are diagnosed under age 50.
- it occurs when neurons in a part of the brain called the substantia nigra die or become impaired
- The cause of neuronal death is not well understood but is multi-factorial
- Normally these cells produce the neurotransmitter (DA) dopamine
Dopamine allows for ____
When dopamine producing neuron cells in the substantia nigra are damaged, the ____________
smooth coordinated function and movement of body muscles.
motor symptoms of the disease appear.
Parkinson Disease Symptoms:
remember —– TRAP: “The 4 Primary Motor Symptoms”
T
R
A
P
T- Tremor: when resting
R- Rigidity: in legs, arms, trunk, and face (mask-like face)
A- Akinesia/bradykinesia: lack of/ slow start in movement
P- Postural instability: imbalance, fails
Parkinson Disease: additional symptoms patients experience
- small cramped handwriting (micrographia)
- Shuffling walk, stooped posture
- muffled speech, drooling dysphagia
- depression, anxiety (psychosis in advanced disease)
- constipation, incontinence
Parkinson’s Disease Non-motor disorders it can cause, include:
-depression
-sleep disorders
- weight loss
- orthostatic hypotension
- difficulty speaking
- excessive salivation
- difficulty in swallowing
- respiratory problems
- increased sweating
- constipation
- micronutrition disorders
- sexual problems
- forced closure of the eyelids (blepharospasm)
There are medications that can cause similar symptoms and can mimic PD or make PD worse:
Key Drugs:
“Dopamine blocking drugs CAN WORSEN PD”
- ## phenothiazines (e.g. prochlorperazine), used for psychosis, nausea and agitation
- ## butyrophenones (e.g. haloperidol, droperidol) used for psychosis and behavior disorders or nausea
- ## 1st and 2nd generation antipsychotics (risperidone at higher doses, paliperidone), lowest risk with quetiapine
- metoclopramide, a renally-cleared drug that can accumulate in elderly patients. (DO NOT USE DRUG in elderly population)
(AIMS) Abnormal Involuntary Movement Scale:
can be used to measure involuntary movements (e.g. tardive dyskinesias)
Even with high doses of PD drugs and various combinations, the disease will _______, including extended periods of “off time”. This is when symptoms of the disease worsen before the next dose of medication is due.
An “off” episode, _____
progress
with muscle stiffness, slow movements and difficulty starting movement, is one of the most frustrating aspects of living with the disease.
Mutations in the ________ gene put individuals at higher risk of PD
LRRK2
Patients with Parkinsons Disease have a higher incidence of _________.
_______ or _______ are commonly used for treatment
depression
SSRI’s or SNRIs
Agonists-
drugs that occupy the receptors and activate them
Antagonists-
Drugs that occupy the receptor but DO NOT activate them, antagonists block the receptor activation by agonists.
Dopamine Antagonists, can cause movement disorders.
dystonia is characterized by __________
painful, prolonged muscle contractions that result in abnormal movements and postures.
Related Psychiatric conditions in patients with Parkinsons Disease:
Depression
Anxiety
Psychosis
SSRIs or SNRIs
TCA (preferably the secondary amines) [nortriptyline and desipramine] and the dopamine agonist pramipexole is another option.
Psychosis can occur with advanced disease or can be due to side effects of drug treatment. (Quetiapine is the preferred antipsychotic due to LOW risk of movement disorders, however, be aware it can cause metabolic complications including increased cholesterol and increased blood glucose)
Clozapine has a LOW risk of worsening movement disorders but has a HIGH risk of seizures, agranulocytosis (requires frequent monitoring and reporting of white blood cells).
_________ is a 5HT-2A/5HT-2C receptor inverse agonist, it is FDA approved to treat hallucinations and delusions in Parkinson’s Disease.
(Nuplazid) pimavanserin
Rapid withdrawal of ____________ can lead to a condition similar to (NMS) neuroleptic malignant syndrome, which is a life-threatening condition sometimes seen with antipsychotics.
levodopa or dopamine agonists
Drug Treatment for Parkinson Disease:
- medications are used to improve movement, which also helps related issues, such as psychosis and constipation.
Levodopa is a __________of dopamine
prodrug
__________ is given with levodopa to prevent the peripheral metabolism of levodopa, which would destroy most of the drug before it crosses the blood brain barrier.
carbidopa
Dopamine
- too polar “very hydrophilic” to cross cell membranes and the blood brain barrier
- useful in treating Parkinson disease
- need a way to get across bbb
Levodopa
- also polar but is an amino acid
-carried across cell membranes by carrier proteins for amino acids
- decarboxylated in cell to DA
There are 2 primary ways that dopamine is broken down:
1)
2)
1) Monoamine Oxidase enzyme
2) (COMT) Catechol-o-methyltransferase enzyme
You cannot take levodopa with a non-selective MAO inhibitor because the dopamine levels ____________
will get too high.
metabolically dopamine is then converted to epinephrine. Epinephrine is adrenaline, and this will cause elevations in blood pressure. Leading to Hypertensive Crisis.
In order, to use a COMT inhibitor like COMTAN. The patient must also be on ___________
(Sinemet) levodopa/carbidopa
COMT inhibitors should ONLY be used with levodopa.
Dopamine agonists - mimic dopamine at the dopamine receptor
-
-
Patient Counseling
- melanoma
- dyskinesias
-drug interactions - unusual urges (sometimes sexual)
- mood changes
- Do not stop suddenly
- avoid alcohol
for specific drugs:
- Levodopa/carbidopa: urine can darken, separate from iron
- Dopamine agonists: sudden sleepiness, dose titration, nausea (can take with food)
- Entacapone: same as with levodopa
- MOA-B inhibitors:
