N658: Neuro

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Cholinesterase Inhibitors Drugs:

1) donepezil (Aricept) (she loves this drug!!)
2) rivasigmine (Exelon)
3) galantamine (Razadyne or old name Reminyl)

Cholinesterase Inhibitors Indications:

1st Line Management of mild to moderate Alzheimers type dementia

Cholinesterase Inhibitors MOA:

Block enzyme (cholinesterase) that degrades acetylcholine in the brain, resulting in more acetylcholine at the synaptic cleft and enhancing cholinergic transmission (gives more time for the message to transmit)

Cholinsterase Inhibitors, info to know

- Improves cognitive function in 6 weeks, but may take 18-24 weeks for optimal effects
- Diminishes s/s of dementia and improves function and slows progression over 6-9 mos, then gradual decline will begin again
- smoking decreases absorption (enhances liver metabolism of drug)

Cholinesterase Inhibitors. Adverse Reactions

- Insomnia
- Fatigue
- Dizziness
- Confusion
- Ataxia
- Agitation/depression
- GI: anorexia, n/v/d, dyspepsis, abdominal pain

Cholinesterase Inhibitors Contraindications:

1) Pregnancy (God help me if I'm pregnant and senile!)
2) Sick-sinus syndrome
3) GI bleeding
4) seizures
5) asthma/COPD

Cholinesterase Inhibitors Monitoring

1) CBC
2) LFT's

donepezil (Aricept)

Class: cholinesterase inhibitor
Special Info:
1) Start at 5 mg then increase to 10 mg QD
2) Take with dinner
3) Can induce hepatotoxicity - check ALT 1 mos into the drug
4) Decreases effects of anticholinergics
5) P450 - many drug/drug interactions
6) SE: N/V/D

rivastigmine (Exelon)

Class: cholinesterase inhibitor
Special info:
1) 1.5mg to 6mg BID
2) dosing is tapered up over time (may be difficult for patient to follow)
3) SE: N/V/D, weight loss, weakness, dizziness, HA
4) titrate slowly with hepatic or renal disease

galantamine (Razadyne)

Class: cholinesterase inhibitor
Special Info:
1) multiple dosing steps, more complicated than Aricept
2) 4-12 mg BID (max 24mg/day)
3) CI in patients with severe hepatic or renal disease
4) SE: N/V/D, bradycardia, syncope

NMDA Receptor Antagonists Drug

mementine hydrochloride (Namenda)

NMDA Receptor Antagonists Indications

- Moderate to severe dementia of Alzheimers type
- May be given in addition to cholinesterase inhibitors

NMDA Receptor antagonists MOA

-NMDA receptor is linked to learning and memory; associated with storing, processing, and retrieval of information. Excessive stimulation leads to excitotoxicity
- blockade of this receptor blocks excitotoxic effects associated with abnormal transmission of glutamate

NMDA Receptor Antagonist Dosing

1) renal impairment dosing if CrCl 5-29 mL/min...."anyone not on hemodialysis can use"
2) Take with or without food

NMDA Receptor Antagonist Precautions

- seizures
- severe renal impairment
- GU conditions
- concomitant use of other NMDA antagonist
- severe liver disease

NMDA Receptor Antagonist AE

- dizziness
- HA
- HTN
- tachycardia
- back pain
- gait abnormalities
- arthralgia
- confusion
- somnolence
- hallucinations
- Stevens-Johnson

NMDA Receptor Antagonist Labs

Creatinine at baseline

mementine hydrochloride (Namenda)

Class: NMDA Receptor Antagonist

Dopamine

Function: regulates mood and movement; D1 - excitation, D2 - inhibition
Diseases: Parkinson's, depression, ADHD, narcolepsy
AE: Extra pyramidal symptoms,increased prolactin levels, psychosis, insomnia, anorexia, psychomotor activation

5-HT, Serotonin

Function: regulates anxiety, movement, obsessions, compulsions, appetite and eating behaviors, sleep, sexual function, and GI motility
Diseases: depression, ADHD, HA, GI disorders, eating disorders
AE: Anxiety, agitation, anorexia, GI distress, HA, hypotension, sexual dysfunction

Acetylcholine

Function: voluntary movement, regulates ANS, memory
Diseases: dementia
AE: memory dysfunction, tachycardia, blurred vision, dry mouth, urinary retention, constipation

GABA

Function: Brains most widespread neurotransmitters. Involved in most facets of brain function, ranging from memory to sleep. Used for sedating effects, muscle relaxants
Diseases: Anxiety, seizures, muscle spasms

Glutamate

Function: Excitatory, important to learning and memory
Diseases: Alzheimer's, CVA, Huntingtons, seizures, ALS

Norepinephrine (Noradrenergic neurons)

Function: within brain, excitatory: memory, attention and arousal. Outside brain: important in SNS stimulation, "fight or flight"
Diseases: Depression
AE: tachycardia, tremors, sexual dysfunction, augments sympathomimetics

Noradrenergic neurons

Function: main funciton is attention. Have role in memory, psychomotor function, movement, BP, HR, bladder emptying
Disease: Memory, depression, HR, BP, movement

A1-adrenergic

AE: orthostatic hypotension, dizziness, cardiac conduction disturbances

Histamine:

AE: sedation, hypotension, weight gain, allergy

First line treatment for Mild to Moderate Migraines

1) Prevention of triggers (non-pharm)
2) Combo of acetaminophen, ASA, caffeine
3) Excedrin Migraine - OTC
4) NSAIDS - OTC
5) TCA's - Elavil
6) SSRI - Prozac
7) Beta blockers/CCB

Excedrine Migraine

From notes:
- OTC combo of ASA, Tylenol, and Caffeine for mild to moderate migraines
- Dose: 2 tabs q6hrs prn, max of 8 tabs/day
- Preg: ASA - D, Caffeine - C, Tylenol - B (so D)

Ibuprofen

Class: NSAID
From notes:
- OTC use for mild to moderate migraines

ibuprofen (Motrin) - taken from Test 1 cards made by Kelli....thanks!

NSAIDs
AE-heart burn, nausea
***inhibit platelet activation (reversible, last 24hr, do not stop med before surgery)
***decreased renal bl flow r/t prostaglandin-no for kidney problem
***provoke asthma & increase risk CV disease (sm dose shortest time

First LIne treatment for Moderate to Severe Migraines

1) Triptans
2) Dihydroergotamine
3) Ergotamine
4) Opioids

Serotonin 5-HT receptor agonists (Triptans) Drugs

- eletriptan (Relpax) - longer acting: 1/2 life 4 hrs (nearly 5 per notes)
- sumatriptan (Imitrex) - short acting: 1/2 life 1.5 hrs
- frovatriptan (Frova) - Long acting: 1/2 life 25 hrs
- Rizatriptan (Maxalt) - Short acting: 1/2 life 2-3 hrs

Triptans Dosing Routes available

- eletriptan (Relpax) - PO only
- sumatriptan (Imitrex) - PO, Nasal spray, SQ
- frovatriptan (Frova) - PO
- rizatriptan (Maxalt) - PO, Melt

Triptans Indication

- Migraine HA with or without aura

Triptans MOA

- Activates 5HT 1B and 5HT 1D receptors
- Prevents release of Calcitonin Gene related peptide which prevents vasodilation - resulting in cranial vessel constriction, inhibition of neuropeptide release, and reduced transmission in trigeminal pathways

Triptans Contraindications

- hemiplegic or basilar migraines
- Patients with ischemic heart disease
- coadministration of two 5 HT agonists within 24hrs of each other
- peripheral vascular disease
- uncontrolled HTN
- should not be used within 24 hrs of ergot derivative
- NSAIDS, if danger of gastric erosion or renal/hepatic DZ
- MAOI use within 2 weeks, can cause Serotonin Syndrome
- combo with SNRI or SSRI can cause serotonin syndrome

sumatriptan (Imitrex)

Class: 5HT agonist (Triptan)
Indication: Migraine with or without aura, or cluster HA
Dosing: SQ, PO, Nasal spray. Max PO is 200mg/24 hr, Max SC is 2 doses or 12 mg/24 hrs
Pregnancy: C
Lactation: no breastfeeding for 12 hrs post dose

sumatriptan (Imitrex) CI

- HTN, uncontrolled
- ischemic heart disease
- coronary vasospasm
- cerebrovascular DZ
- migraine, basilar or hemiplegic
- PVD
- ischemic bowel DZ

sumatriptan (Imitrex) Cautions

- elderly pts
- cardiac disease risk (HTN, Hypercholesterolemia, obesity, DM, smokers, strong fam hx)
- hepatic impairment is mild-moderate (PO use)
- seizure disorder

sumatriptan (Imitrex) Adverse Reactions

- paresthesias
- hot or cold sensation
- malaise/fatigue
- chest pain/pressure/tightness
- neck pain/pressure/tightness
- jaw pain/pressure/tightness
- dizziness/vertigo
- flushing (SC)
- weakness (SC)
- drowsiness/sedation (SC)
- injection site rxns (SC)

sumatriptin (Imitrex) Precautions

- give 1st dose in health care providers office if pt has a risk of unrecognized coronary disease and HTN crisis
- angina symptoms - ECG for ischemic changes - may cause coronary vasospasm in pts with hx of coronary heart dz. Rare reports of MI, major arrhythmias, angina symptoms, and death

What to monitor after Triptan dosing?

1) HA severity
2) s/s suggestive of angina
3) monitoring of BP, HR, ECG on 1st dose for those with likelihood of unrecognized coronary DZ

frovatriptan (Frova)

Class: 5HT agonist (Triptan)
Dose: PO only. Longest 1/2 life of 25 hrs and a favorable recurrence rate. Some specialists prescribe daily dosing for a limited period for menstrual and prolonged migraines
Indications: freq. used for treatment of menstrual migraine and for attacks longer in duration
AE: small risk for Serotonin Syndrome
Preg: C

eletriptan (Relpax)

Class: 5HT agonist (Triptan)
Dose: PO only. 1/2 life nearly 5 hrs. relatively rapid onset but a longer duration
Preg: C

. rizatriptan (Maxalt)

Class: 5HT agonist (Triptan)
Dose: PO or melt, may repeat dose after 2 hrs
Preg: C

Severe Serotonin Syndrome

- With SSRI DDI: any drug that co-stimulates serotonin.
- Ex. MAOI's, Lithium, buproprion, amphetamine, psychostimulants, dopamine agonists, tryptophan - may result in this syndrome

Severe Serotonin Syndrome symptoms

- autonomic instability
- HA
- dizziness
- agitation
- rigidity
- hyperpyrexia
- widely fluctuating vital signs
- HTN
- confusion
- tremors
- DEATH....possibly

Severe Serotonin Syndrome prevention

1) wean SSRI's over 2 weaks
2) Do not dose Triptans with SNRI or SSRI if preventable

dihydroergotamine mesylate (DHE)

Class: Ergot Alkaloid
Indication: acute moderate to severe migraines with or without aura or cluster HA (injection)

DHE MOA

1) directly stimulates vascular smooth muscle, constricting veins and arteries (constricts peripheral and cranial blood vessels)
2) depresses central vasomotor centers
3) reduces extracranial blood flow
4) agonist and antagonist actions on alpha 1&2, serotonin 5HT, and dopaminergic D2 receptors
5) inhibits reuptake of norepi

DHE Dosing

1) Intranasal
2) IM/IV/SQ

DHE Adverse Reactions

1) CV: pulselessness, precordial distress or pain, transient tachycardia or bradycardia, raised arterial pressure, coronary vasoconstriction
2) GI: N/V, abdominal pain
3) Misc: numbness and tingling of fingers and toes, muscle pain in extremities, weakness in legs, localized edema, ithcing
4) Ergotism

Ergotism

Cause: prolonged use of ergots
S/S: N/V/D, severe thirst, hypoperfusion, chest pain, BP changes, confusion

DHE Drug/Drug

1) uses P450
2) triptans, azole antifungals - increase risk for vasospasm
3) macrolide antibiotics (Biaxin, Emycin), grapefruit juice, Flagyl, SSRI, diltiazem, P450 drugs: increase risk of ergot toxicity, severe vasospasm and ischemia
4) nitrates: decrease effectiveness

DHE monitoring

1) VS: esp. pulse and BP
2) Mental Status: changes (confusion, drowsiness)
3) HA relief effectiveness: pain assessments Q15 min and for minimal effective dose
4) check neurocirculatory status of extremities, esp distally (eg. pulse, warmth, and color)

DHE Preg/Lactation

Preg: X
Lact: excreted in breast milk and may inhibit lactation. Drug can cause ergotism symptoms in infant

DHE patient teaching

1) Take drug at first sign of impending HA
2) do not exceed max dosage
3) Have pt relax in supine position in quiet, darkened room
4) Notify provider if diagnosed with heart or peripheral vasc DZ
5) Report symptoms: pain, itching, weakness, tingling, edema, pallor, coolness, numbness (esp. distal etremities), chest discomfort, pain or any change in mental status
6) avoid ETOH, Smoking, cold exposure - these vasoconstrictors may further impair peripheral circ or cause/aggravate migraine HA

propranolol (Inderal)

Class: Beta-blocker
Indication: besides MI, HTN, etc....for this topic FDA approved for migraine prevention
MOA: in migraine, not understood but thought to involve anxiolytic effects as well as vacular changes and stabilization
Dose: 20 mg PO BID (one dose at night)
Info: may take up to 3 mos to see effects
Preg: C - trimester specific

verapamil (Calan)

Class: CCB
Indication: besides HTN, treatment for migraine prevention ( well tol and can be as effective as B-Blockers)
MOA: regulate vascular smooth muscle contraction, neurotransmission, and hormone secretion enzyme activity. believed to alter serotonin release and inhibit PLT serotonin uptake and release within the brain
Dose: More effective and commonly recommended to pts. Dose varies from 120-480 mg/day
Preg: C

Migraine therapy and pregnancy

Category B: Tylenol and Motrin
Category C: Triptans, may be in breast milk; TCA's (Elavil); SSRI (Prozac)
Category D: topiramate (Topamax), Excedrine (D/T ASA)
Category X: ergotamines (DHE)

*no treatment drug has US FDA approval during pregnancy*
Imitrex is recommended pump and dump

topiramate (Topamax) Indications

1) Migraine prophylaxis
2) Partial seizures

topiramate (Topamax) MOA

Exact mechanism is unknown: May block repetitive firing of CNS neurons by enhancing the ability of GABA to cause influx of Cl into CNS neurons. Blocks Na++ channels, decreases Ca++ channels, inhibits carbonic anhydrase. This reduces HA pain, frequency, and duration.

topiramate (Topamax) PK/PD

1) CP450
2) excreted by urine
3) 1/2 life - 21 hrs

topiramate (Topamax) AE

Common: nervousness, somnolence, fatigue, ataxia, tremors, nystagmus, diplopia, paresthesias, nausea

Occasional: sometimes psychomotor retardation can occur, altered concentration, word finding difficulty and decreased memory

topiramate (Topamax) CI

- Renal dosing: CrCl 10-70 decreased dose 50%. CrCL<10 decrease dose 75%; Hemodialysis....pick a different drug
- Caution: liver DZ, lung DZ, dehydration
- Do not stop abruptly
- do not drink ETOH

topiramate (Topamax) Pregnancy

Preg: D

topiramate (Topamax) Drug/Drug

- Mult due to P450 a path
- combined with valproic acid (Depakote) it will increase ammonia levels -> risk for encephalitis
- oral contraceptives= decreased effectivenss
- metformin = increases risk for hypoglycemia

topiramate (Topamax) Monitoring

1) Cr, bicarb at baseline then periodically
2) S/Sx of depression, behavior changes, suicidality

topiramate (Topamax) Overdose Symptoms

- blurred vision (optho yearly)
- diplopia
- difficulty speaking
- dizziness
- drowsy
- dizzy
- agitated
- altered mentation/coordination
- low BP
- ABD pain
- poss. seizures

phenytoin (Dilantin)

Class: Hydantoin
Indications: generalized seizures: tonic-clonic TX

phenytoin (Dilantin) MOA

- Acts at motor cortex in inhibiting spread of seizure activity.
- possibly works by promoting Na efflux from neurons, thereby stabilizing threshold against hyperexcitability
- also decreases posttetanic potentiation at synapse

phenytoin (Dilantin) Preg/lact

Preg: D; risk of birth defects must be considered along with risk of seizures to fetus in untreated epileptic mothers
Lact: in milk

phenytoin (Dilantin) Dosing

- brands vary in bioavailability....dont change brands
- don't give for seizures due to hypoglycemia, petit mal (absence) epilepsy, or other metabolic causes
- abrupt withdrawal may precipitate status epilepticus. Dose must be reduced or other anticonvulsant substitute gradually added

phenytoin (Dilantin) AE and drug/drug and CI

AE: nystagmus, blurred vision, dizziness, drowsiness, N/V, gingival hyperplasia, folic acid depletion, osteomalacia and hyperglycemia
Drug/Drug: Many.....many....to many to write (she said "I don't expect you to remember these")
CI: heart blocks

What is the most commonly complained about AE of Dilantin?

Drowsiness (from her lecture)

Pts on Dilantin should see a dentist twice per year. True or False.

True....R/T gingival hyperplasia

Dilantin pt teaching:

1) take med with food
2) notify HCP if rask develops
3) No ETOH
4) Don't stop abruptly, don't change dose without HCP
5) Good oral hygiene...tell dentist you are on the med
6) DM - Blood sugars may change, monitor closely
7) Urine may turn pink
8) Get med ID that says you are on the drug
9) Tell surgeon's, HCP's, dentists you are on the drug before any procedures
10) May cause drowsiness, caution with driving or performing other tasks

What is Dilantins spectrum of effect?

Partial

valproic acid (Depakote)

Class: Valproates
Indication: complex partial seizures. can be ordered as monotherapy or adjunct therapy
MOA: GABA agonist
Preg: D

valproic acid (Depakote) BLACK BOX Warning

- Hepatotoxicity
- Teratogen
- Pancreatitis

valproic acid (Depakote) AE/CI

AE: blurred vision, HA, appetite changes, tinnitus, somnolence, dyspepsia, thrombocytopenia, nausea, tremor, hair loss, weight gain
CI: liver or kidney DZ
Caution: bleeding disorders, hypoalbuminemia, and organic brain syndrome

valproic acid (Depakote) Labs

- LDH, AST, ALT, ammonia (all may be elevated)
- TSH
- CBC, PLTS, and bleeding times
- Ca - may be decreased
- she added amylase/lipase for Pancreatits BLACK BOX

What is Depakotes spectrum of effect?

Broad

primidone (Mysoline)

Class: Barbituate
DEA: Schedule IV (secure script)
Indications: partial and generalized tonic-clonic seizures
Preg: D

primidone (Mysoline) MOA

- alters sensory cortex, cerebellar, and motor activities
- produces sedation, hypnosis, and anesthesia (barbituate)

primidone (Mysoline) AE/CI

AE: drowsiness, dizziness, lethargy, constipation, rashes, angioedema, respiratory depression, sedation, psychomotor slowing
CI: renal impairment, avoid abrupt withdrawal

primidone (Mysoline) Monitoring

- Cr at baseline
- drug levels
- folate
- CBC
- LFT's
- BUN/Cr if prolonged tx
- resp status if given IV
- S/Sx of depression, behavior changes, and suicidality

What is Mysolines spectrum of effect?

Partial

How often and the method for collecting serum levels of Anti-epileptic drugs (AED)?

q3mos. should be drawn 8 hours after the dose

When do you draw a blood level if the patient took Dilantin at 0600?

1400

What drugs/disorders may alter drug levels?

Drugs: e-mycin, sulfonamides, warfarin, cimetidine, and ETOH
Disorders: pregnancy (decreases serum concentration)....yes, she listed pregnancy as a disorder in her notes!

AED Pregnancy categories:

- notes - recommend against use of AEDs with cat C or D while pregnant or nursing
Cat C: gabapentin (Neurontin), pregabalin (Lyrica), levetiracetam (Keppra) **none are on the study guide**
Cat D: phenytoin (Dilantin), valproic acid (Depakote), primidone (Mysoline), carbamazepine (Tegretol) *not on guide*

What drugs are used for status epilepticus?

Benzo's - Ativan/Valium

What are the most important teaching pearls for the pt. regarding Dilantin bioavailability?

#1 - same brand
#2 - same time
#3 - level q 3 mos
#4 - take without food

What is the Parkinson Triad?

1) Tremor
2) Bradykinesia
3) Rigidity

carbidopa plus levodopa (Sinemet)

Indications: Tx bradykinesia, tremor, and rigidity for patients over 60 y/o

carbidopa plus levodopa (Sinemet) MOA

-Levodopa is converted to Dopamine by I-AAD
- carbidopa blocks this conversion to Dopamine in the periphery since Dopamin does not cross the blood brain barrier
- This combo allows for increased Dopamine in the brain

carbidopa plus levodopa (Sinemet) PK/PD

- Metabolized: GI tract, kidney, liver
- Excreted: urine
- 1/2 life: 0.75-1.5 hrs

carbidopa plus levodopa (Sinemet) Food and Vitamin Effects

- Vit B6 decreases conversion of Dopamine in the brain
- ETOH antagonizes effects of Levodopa
- High PRO foods block effect of Levodopa (red meat, poultry, fish, milk, cheese, eggs)
- Taken best on an empty stomach....if nauseous, may take a snack

carbidopa plus levodopa (Sinemet) AE

AE: syncope, dry mouth, difficulty swallowing, worsening tremors, numbness, hallucinations, irregular heartbeat, difficulty with urination, dizziness, orthostatic hypotension, depression, mood changes, nausea, vomiting, anxiety, confusion, long term use can result in dyskinesias (r/t no more dopamine)

carbidopa plus levodopa (Sinemet) Monitoring

Labs: Baseline CBC, LFT's, Renal Fx, Uric Acid levels
- Levodopa can increase ALT, AST, LDH, bilirubin, and uric acid

carbidopa plus levodopa (Sinemet) CI

- use with MAOI drugs
- narrow angle glaucoma
- hx MI
- uncontrolled HTN
- psychosis

It is safe to stop Sinemet abruptly. True or Falsee.

False. Must taper the dose. a rapid dose reduction has resulted in a symptom complex resembling neuroleptic malignant syndrome.

So, what is neuroleptic malignant syndrome?

- Potentially lethal hypodopamindergic AE, related to high potency antipsychotic drugs and abrupt withdrawal of PD drugs
- typically occurs within 2 weeks of treatment

Neuroleptic Malignant Syndrome (NMS) Criteria

1) hyperthermia (fever up to 108)
2) muscle rigidity
3) presence of 5 of the following: stupor, tremors, tachycardia, incontinence, unstable BP, metabolic acidosis, tachypnea or hypoxia, elevation of CPK, diaphoresis, leukocytosis, exclusion of other central and systemic causes of hyperthermia

What causes death in NMS?

aspiration, PNA, sepsis, renal failure, DIC, cardiac arrest

What drugs shouldn't your patient take on Sinemet?

- MAOI....must be D/C'd 2 weeks prior to starting Sinemet

Why don't you give Sinemet to patients <60 y/o?

Long term Levodopa can have more motor complications....
- dyskinesias
- end-of-dose wearing off causing shorter duration of benefit from each dose
- unpredictable switching between decreased mobility and times when med is working (on-off periods)
** these effects occur within 5 yrs and on/off can occur >1yr.

pramipexole (Mirapex)

Class: Dopamine Agonist
Indication: treats bradykinesia, tremor, and rigidity associated with Parkinsons (ok for Michael J. Foxx....pt <60 y/o). Also Restless Leg syndrome
Preg: C
Lact: UNK
Drug/drug: Many

pramipexole (Mirapex) MOA

direct stimulation of dopamine receptors to restore Dopamine needed for correct functioning of basal ganglia

pramipexole (Mirapex) PK/PD

Metabolized: no hepatic biotrans (nice to liver)
Excreted: Urine (hard on kidneys)
Dose: adjust for renal impairment

pramipexole (Mirapex) AE

AE: orthostatic hypotension, GI disturbances (nausea, constipation), dizziness, drowsiness, insomnia, Dyskinesias are less frequent (r/t it being synthetic)

pramipexole (Mirapex) Monitoring

Labs: Cr at baseline
Exam: Derm
S/Sx: orthostatic hypotension esp. with dose titration - consider reducing dose if pt becomes hypotension

It is safe to abruptly stop Mirapex. True or False.

False. Neuroleptic Malignant Syndrome rears its ugly head! (remember.....elevated temp, muscle rigidity, altered consciousness, and autonomic instability)

trihexyphenidyl (Artane)

Class: Anticholinergic
Indications: 2nd line tx for Parkinson....treats tremor only (due to excessive unopposed acethylcholine)

trihexyphenidyl (Artane) AE

AE: impaired memory, confusion, constipation, blurred vision, urinary retention, xerostomia, angle-closure glaucoma

*usually avoided due to side effects*

trihexyphenidyl (Artane) Education

- take with food if GI upset occurs
- no driving d/t drowsiness
- avoid ETOH
- dry mouth can occur
- constipations and urinary retention can occur

selegiline (Eldepryl)

Class: MAO-B inhibitor
Indications: 2nd line Parkinson (chosen over Artane)....treats Bradykinesia, tremor, and rigidity

selegiline (Eldepryl) MOA

Selective inhibition which irreversibly blocks the metabolism of dopamine in the brain

- may delay the need for Levodopa or can be used as an adjunct to Sinemet in all stages of PD

selegiline (Eldepryl) AE

AE:insomnia, nausea, anorexia, orthostatic hypotension, hallucinations
Drug/Drug: interactions with SSRI and meperidine

entacapone (Comtan)

Class: COMT inhibitor
Indications: Third line, last resort therapy to reduce motor fluctuations in patients with advanced dz, but increases dyskinesias (use before Dopamine in pts <60 y/o)

entacapone (Comtan) MOA & AE

MOA: Delays the breakdown of levadopa to prolong dopamine effects....central and/or peripheral dopamine blockers of dopamine metabolism

AE: Nausea and orthostatic hypotension

Do you have to monitor drug levels for the PD drugs?

No

How do you judge effectiveness of the PD drugs?

Patient response

What is an off label use of Provigil for PD patients?

given to help increase daytime function. PD drugs tend to be very sedating.

risperidone (Risperdal)

Class: Dibenzepins (Second Gen Anti-psychotic)
Indications: bipolar, mania, psychosis (commonly used in the elderly)

Risperdal BLACK BOX

Increased mortality for elderly pts with demetia related psychosis. Cause of death varied but most appeared to be CV or infectious in nature. Instructor said she has seen stroke. Risperdal is not approved for tx of patients with dementia-related psychosis.

Note

Not sure why Risperdal was on the Neuro list....but it was. If anyone remembers or can invent THE BEST reason for it to be in the neuro section.....I owe you a cupcake!

carbamazepine (Tegretol)

Class: Anti-Epileptic Drug (Narrow Spectrum)
Indications: tonic-clonic and partial seizures; trigeminal neuralgia, bipolar disease, migraine prophylaxis

carbamazepine (Tegretol) AE/BLACK BOX

AE: restlessness, aggression, irritability, agitation
BLACK BOX: Stevens-Johnson syndrome, aplastic anemia, agranulocytosis

carbamazepine (Tegretol) CI

1) Liver or Kidney Disease
2) No MAOI within 14 days
3) No abrupt withdrawal
4) caution if increased IOP

carbamazepine (Tegretol) Safety and Monitoring

Preg: D
Labs:
1) CBC, PLT, Reticulocytes, Iron, BUN, LFT's, UA at baseline
2) lipid panel, serum drug levels (decreases Na, Ca, T3, T4 levels)
Exams:
1) Opthalmic Exam at baseline then periodically
Monitor:
1) S/Sx of depression, behavior changes, suicidality

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