Parkinson's, Alzheimer's, ADD/ADHD, Anticonvulsants Flashcards
Parkinson’s PATHO
movement disorder
TRAP: tremor, rigidity, bradykinesia, postural dysfunction, abnormal gait
GOAL: symptom control
Must balance AE of drug therapy
Carbidopa-Levodopa USES
Sinemet or Parcopa
Combo drug to tx Parkinson’s
Levodopa = precursor dopamine; cross BBB
combo cross BBB more effectively
MOA: improves nerve impulses by changing the dopamine/acetylcholine balance
Carbidopa-Levodopa ADMINISTRATION
oral administration starts to take effect in 1-2 months, but may take 6 months for noticeable effects
duration: 6-12 hrs
half life: 1-2 hrs
Carbidopa-Levodopa CONTRA/CAUTIONS
CONTRA: Hx sensitivity, undiagnosed pigmented lesions or Hx melanoma, closed angle glaucoma
CAUTION: cardiac disease, MI, pulmonary, DM, PUD, Hx psychiatric disorder
Carbidopa-Levodopa INTERACTIONS
MAOI, TCA, phenothiazines, pyridoxine
AVOID high protein diet
AVOID food w/ large amounts pyridoxine
manage body weight
Carbidopa-Levodopa AEs
GI, orthostatic hypotension
abnormal movements: bruxism, ballismus
Bradykinetic episodes: on-off
NMS
Hyperventilation, bizarre breathing patterns, hoarseness, INC nasal secretions
Carbidopa-Levodopa DOSAGE
dose for adults
25/100mg tabs BID to QID for maximum dose of 200/2000 mg daily
Lose effectiveness after 2-5 yrs of therapy
Parkinson’s: Non-Ergot Derived Dopamine Agonists
Ropinierole, pramipexole
Monotherapy to control sx and delay use of levodopa
May also be used in pts who experience levodopa “wearing off”
CAUTION: renal, hepatic impairment
extensive first pass; 40% protein bound
Parkinson’s: Non-Ergot Derived
AEs/INTERACTIONS
AE: GI, postural hypotension, dyskinesias, somnolence, dizziness, unsteadiness, hallucinations, confusion
Interactions:
1. pramipexole: cimetidine
2. ropinirole: a lot
AVOID St. John’s wort, Kava, Valerian
Parkinson’s: Anticholinergics
Benztropine (cogentin) and Trihexyphenidyl (Artane)
Alter relative balance of cholinergic and dopaminergic influences in the EPS by inhibiting the cholinergic neurons
MOA: DEC acetylcholine = blocking acetylcholine
DEC EPS symptoms
Parkinson’s: Amantadine
antiviral agent
used to tx: mild PD, drug induced parkinsonism, late stage PD
Effective for resting tremors and in combo w/ levodopa
MOA: block reuptake of dopamine and stimulate dopamine release from nerve storage sites
Do NOT recommend for parkinson’s pt w/ flu = double dosing
Alzheimer’s PATHO
senile dementia
slow progressive decline in cognition
drug therapy is to slow the progression of the disease
confirmed only by autopsy
Alzheimer’s Drug GOAL
Maintain and maximize the patient’s functional ability, quality of life, and independence for as long as possible
Alzheimer’s DRUGS
- Donepezil
- Galantamine
- Memantine
- Rivastigmine
- Tacrine
Cholinesterase inhibitors MOA/USES
Used to inhibit one or both types of cholinesterase enzymes
Reduce apathy, psychosis, anxiety, depression, agitation
MOA: SLOW the progression of cognitive, functional and behavior symptoms
Cholinesterase Inhibitors ADMINISTRATION
effect usually seen in 3-6 wks
peak 1-3
half life 7-70
Cholinesterase Inhibitor CONTRA/AEs/CAUTION
CONTRA: prev sensitivity
CAUTION: liver or kidney dysfunction, PUD
AE: GI, N/V/D- dose dependent; bradycardia, HA, fatigue, weight loss
do NOT smoke, low intake of charcoal broiled foods
Cholinesterase Inhibitors INTERACTIONS
anticholinergic agents, acetylcholinesterase inhibitors, cholinergic agonists
St. John’s wort, Gingko biloba
MONITOR: weight loss, hypotension
Cholinesterase Inhibitor DOSAGE: Tacrine
10mg QID max 160mg
Onset rapid
peak 1-2 hrs
half life 2-4 hrs
Cholinesterase Inhibitor DOSAGE: Rivastigmine
3-6mg BID max 12mg
Onset intermediate
duration 10 hrs
half life 1.5hrs
Cholinesterase Inhibitor DOSAGE: Donepezil
5-10mg daily
Onset and duration unknown
half life 70hrs
Cholinesterase Inhibitor DOSAGE: Galantamine
regular 4mg BID 12-24mg
ER 8mg QID, max 24mg
Peak 1-4.5hrs
half life 7hrs
Memantine MOA/USES
Namenda
MOA: block receptors involved in learning and memory and excessive stimulation of NMDA receptors is believed to be involved in Alzheimer’s
Memantine CONTRA/CAUTION
CONTRA: prev sensitivity
CAUTION: seizure disorders, hepatic dysfunction, severe renal dysfunction
Clearance is significantly reduced by alkaline urine
Memantine AEs/INTERACTIONS
AE: dizziness, confusion, HA, hallucinations, somnolence, constipation, vomiting, weight loss
HTN- monitor BP
Interactions: drugs cause alkaline urine, carbonic anhydrase inhibitors, sodium bicarb
Memantine DOSAGE
Start 5mg per day and target dose of 20mg
Dose oral 2mg/mL or 5-10mg tabs
Peak 3-7hrs
Half life 60-80hrs
Selegiline MOA/USE
selective MAOI
5mg BID
Some evidence shows it may delay progression and possibly improve cognition
Selegiline AEs/INTERACTIONS
AE: orthostatic hypotension, hallucinations, agitation, insomnia
INC BP w/ tyramine containing foods
Interactions: carbamazepine, SSRI, TCA, SNRI, meperidine
Alzheimer’s Other Agents
- ergoloid mesylates
- NSAIDs and estrogen replacement: lack well-designed efficacy studies
- statins: theory DEC cholesterol in brain will reduce plaque formation
Alzheimer’s Noncognitive Sx Management
used to manage sx of AD:
1. antipsychotics
2. benzos
3. antidepressants
FIRST line: cholinesterase inhibitor, DONEPEZIL
SECOND line: Add vit E or Selegiline
THIRD line: switch cholinesterase inhibitor
Alzheimer’s MONITORING
- follow-up every 3-6 months to monitor cognitive and behavioral sx. Switch if no improvement
- add memantine if MMSE score <10
- Assess ADL’s
ADHD Drug Therapy
- Stimulants
- Non-Stimulants
- Antidepressants
- Clonidine
Stimulant: Dextroamphetamine USES/MOA
Schedule II
PREG C
Adults: narcolepsy, exogenous obesity
Peds: narcolepsy, ADHD
ASSESS: psychopathology, homicidal, suicidal, or addiction
Stimulant: Dextroamphetamine AEs/CONTRA
AVOID ETOH, caffeine, OTC meds
Can cause physical dependency
Taper dose when d/c
AE: dry mouth, N/V/D, altered libido
DM: monitor BG
REPORT: CNS changes, abd distress, changes in sexual behavior, blurred vision
Stimulant: Methylphenidate USES/MOA
Schedule II
PREG C
Adults: narcolepsy, ADHD
Peds (>6yo): ADHD
Stimulant: Methylphenidate CONTRA/CAUTION
AVOID ETOH, CNS drugs, take on empty stomach
CAUTION: seizure disorders
MONITOR BP, CBC, growth
Stimulant: Methylphenidate AE/INTERACTIONS
AE: cardiovascular events, HA, insomnia, anorexia, N/V, tics, weight loss, EPS, NMS
Interactions: Alpha2-agonists, anticonvulsants, anticoagulants, TCA, SSRI, ETOH
Stimulant: Dexmethylphenidate HCl USES/MOA
Schedule II
PREG C
Adults/peds (>6yo): ADHD
Stimulant: Dexmethylphenidate HCl CONTRA/CAUTION
CONTRA: marked anxiety, tension, agitation, glaucoma, Hx of tics or Tourette’s in patient/family, use of MAOI
CAUTION: seizure disorders, paradoxical symptoms, HTN, heart disease, hyperthyroidism
Stimulant: Dexmethylphenidate HCl AEs/MONITOR
AE: HA, anorexia, abd pain, insomnia, weight loss, nausea, dizziness, dyskinesia, HTN, tics, psychosis, seizures, blood dyscrasias
MONITOR: Ht/Wt, emotional instability, behavior disturbance, thought disorders, BP, CBC
Stimulant: Lisdexamfetamine BLACK BOX
Schedule II
PREG C
Black box: serious cardiovascular events including SUDDEN DEATH in patients w/ pre-existing cardiac abnormalities or other serious heart problems
Black box: potential for drug dependency w/ prolonged use
Stimulant: Lisdexamfetamine CONTRA/CAUTION
CONTRA: Hx drug abuse, use of MAOI, glaucoma, agitation, hypersensitivity or use of sympathomimetics
CAUTION: bipolar disorder, psychosis, tics, tourette’s, seizure, impaired renal, hepatic, thyroid
Stimulant: Lisdexamfetamine AEs/INTERACTIONS
AE: DEC appetite, weight loss, dry mouth, irritability, jitteriness, dizziness, HA, anxiety, fatigue, insomnia, upper abd pain, GI upset, HTN, blurred vision, psychosis, tics, rash
Interactions:
1. risk serotonin syndrome w/ SSRI
2. TCA may cause hypertensive crisis
3. NO ETOH or other CNS stimulants
May take w/ or w/o food
Non-Stimulant: Atomoxetine USES/MOA
Non-stimulant
PREG C
Black Box: may INC risk of suicide ideation in peds patients
cardiac risk
dose adjustment w/ hepatic impairment
Adults: ADHD
Peds (>6yo): ADHD based on weight
Non-Stimulant: Atomoxetine CONTRA/CAUTION
CONTRA: MAOI, glaucoma
CAUTION: HTN, cardiac disease, hepatic dysfunction, psychosis, bipolar, depression
Non-Stimulant: Atomoxetine AEs/MONITOR/INTERACTIONS
AE: HA, insomnia, xerostomia, abd pain, N/V, anorexia, cough
MONITOR: growth, BP, pulse, suicidal ideation, aggressive behavior or hostility, depression
NO ETOH
Guanfacine USE/MOA
Newest drug
TX: ADHD in children and adolescents 6-17 yo
Selective alpha-2 adrenergic receptor agonist
Same drug as HTN med Tenex
Guanfacine AE/INTERACTIONS
AE: somnolence, sedation, abd pain, dizziness, constipation, hypotension
CAUTION: hypotension, bradycardia, syncope
Dose adjustment w/ hepatic or renal impairment
Do NOT stop abruptly
ADHD Other Treatment
TCA is SECOND-LINE tx
Bupropion efficacy not different from methylphenidate
Clonidine used for mood, activity level, cooperation and frustration
Anticonvulsants GOALS of THERAPY
- DEC # of seizures
- Completely control seizures IDEAL
- Improved QOL
- Return to normal ADLs
Phenytoin MOA/USES
Dilantin
oldest and most effective
FIRST LINE MONOTHERAPY
Use: generalized tonic-clonic (grand mal), any seizure type
Prevents seizure post head trauma, neurosurgery, hemorrhagic stroke
MOA: DEC influx Na ions across cell membrane, inhibit Ca conduction
Phenytoin CONTRA/AEs
Dosage: loading dose followed by normal maintenance dose based on weight in adults, age in children
MONITOR: serum levels
PROTEIN BOUND
CONTRA: allergies
AE: hypotension, bradycardia, arrhythmias, CV collapse, thrombophlebitis, GINGIVAL HYPERPLASIA, SJS
Fosphenytoin (Cerebyx) MOA/USES
Prodrug of phenytoin
parenteral
short-term use when phenytoin unavailable, inappropriate, or less advantageous
WARNING: do NOT confuse w/ celebrex
Carbamazepine (Tegretol) MOA/USES
FIRST LINE MONOTHERAPY: simple/complex partial sz
MOA: limit influx of Na ions
Start LOW and INC weekly
Drug monitoring
Carbamazepine CONTRA/AEs
CONTRA: allergy to drug or TCA, bone marrow suppression, recent MAOI
AE: hematologic abnormalities, drowsiness, fatigue, SIADH, rash, GI upset, confusion
May exacerbate myoclonic sz
INC risk SJS in Asians
AE (concentration related): dizziness, drowsiness, N/V, tremors, agitation, arrhythmias, coma, resp depression
Oxcarbazepine (Trileptal) MOA/USES
Monotherapy or adjunctive: partial szs
MOA: block Na channels to stabilize hyper neural membranes
Also used: bipolar disorder, trigeminal neuralgia
Oxcarbazepine CONTRA/AEs
CONTRA: allergy
AE: dizziness, somnolence, diplopia, N/V, ataxia, abd pain
Valproic Acid (Depakote) MOA/USES
FIRST LINE: generalized tonic clonic, simple partial, complex partial, absence
Monotherapy or adjunctive: complex partial & complex absence sz
MOA: work on GABA
Also used: bipolar disorder-manic, migraine prophylaxis
Valproic Acid CONTRA/AE
CONTRA: hepatic disease, urea cycle disorders
AE: fatigue, tremor, GI upset, behavioral changes, weight gain
Severe AE: thrombocytopenia, pancreatitis, encephalopathy, hepatotoxicity
Ethosuximide (Zarontin) MOA/USES
DOC: absence szs
Always in combo w/ another drug
MOA: unknown
CONTRA: allergy
AE: GI upset, fatigue
Barbiturates (Phenobarbital) MOA/USES
broad spectrum activity
Alternative monotherapy: generalized tonic-clonic
Sedating
long-term cognitive, memory, and behavioral effects
dependency issues
phenobarb most commonly used
MOA: binds to GABA
CHEAP
Loading dose, followed by maintenance dose
frequent drug monitoring
Barbiturates CONTRA/AE
CONTRA: severe liver disease, resp disease, Hx of sedative or hypnotic addiction
AE: drowsiness, fatigue, ataxia, N/V, blurred vision, constipation, cognitive impairment, arrhythmias, dizziness
Barbiturates OVER DOSAGE/INTERACTIONS
Over dosage: unsteady gait, slurred speech, confusion, jaundice, hypothermia, hypotension, resp depression, coma
Interactions: INC toxicity w/ benzos, CNS depressants, methylphenidate
Gabapentin (Neurontin) MOA/USES
Adjunct therapy: complex partial sz, generalized tonic-clonic
MOA: DEC presynaptic GABA release
mainly used in neuropathic pain control
Gabapentin CONTRA/AE/ INTERACTIONS
CONTRA: hypersensitivity
AE: fatigue, dizziness, blurred vision. May resolve over time. Some reports of weight gain
Interactions: Antacids may block absorption
Pregabalin (Lyrica) MOA/USES
one of newest
adjunctive therapy: partial onset sz
MOA: binds to Ca channels to inhibit excitatory neurotrans release
Other uses: fibromyalgias, post-herpetic neuralgia, neuropathic pain
Pregabalin CONTRA/AE/ INTERACTIONS
CONTRA: hypersensitivity
AE: peripheral edema, weight gain
Interactions: enhance sedative effect of CNS depressants
Lamotrigine (Lamictal) MOA/USES
Generalized tonic-clonic, absence, complex partial
MOA: stabilizes neuronal membranes by acting on amino acid release and Na channels
Also used: bipolar maintenance
Lamotrigine CONTRA/AE
CONTRA: hypersensitivity
AE: N/V, fatigue, dizziness
Levetiracetam (Keppra) MOA/USES
adjunctive partial onset or primary generalized tonic-clonic
MOA: facilitate GABA transmission, reduce K+ currents
Levetiracetam CONTRA/AE
CONTRA: hypersensitivity
AE: somnolence, HA, infection, usually within first 4 wks, behavioral changes
Topiramate (Topamax) MOA/USES
Monotherapy or adjunctive: partial onset sz, generalized tonic-clonic
MOA: block Na channels by enhancing GABA activity
Do NOT stop abruptly
Also used: migraine prophylaxis
Topiramate CONTRA/AE
CONTRA: hepatic or renal impairment, pregnancy, breast-feeding
AE: fatigue, dizziness, somnolence, psychomotor slowing (stupidimate), memory difficulty, nausea, weight loss, change in taste
Weight loss: Who Qualifies
- 20% of more over ideal body weight
- BMI >27 w/ 1 comorbid condition
- BMI >30
Weight loss: Amphetamines
Not widely used
HIGH risk abuse and cardiovascular SEs
Schedule II
Dextroamphetamine and methamphetamine
MOA: INC release Norepi
Use at lowest effective dose
Appetite Suppressants: Nonamphetamine Derivatives
diethylpropion (tenuate), phendimetrazine (bontril), phentermine (adipex)
tolerance may develop after a few weeks
MOA: DEC appetite by stimulating hypothalamus to release catecholamines norepi and dopamine
Schedule II
potential for abuse
CONTRA: MAOIs
AE: CNS stimulation, dry mouth, nausea, INC BP, tachycardia
CAUTION in DM
Lipase Inhibitor (Orlistat)
work locally in GI
blocks absorption of fats
take during or 1 hr after fat containing meal, meal should contain less than 30% fat
CONTRA: malabsorption syndrome, cholestasis
AE: diarrhea, fatty stools, flatulence, leakage, nausea, abd pain, DEC absorption fat soluble vitamins
TAKE multivitamin
CAUTION w/ coumadin b/c changes in Vit K
Weight loss: Other Agents
- Antidepressants: bupropion
- Diabetes: metformin, byetta, januvia
- Antiseizure meds: topirimate, aonisamide
Weight loss: Qsymia (phentermine and topiramate)
Newest
Combo appetite suppressant and antiseizure med
PREG X
Warning/Precaution: tachycardia, suicidal behavior/ideation, glaucoma, mood and sleep disorder, cognitive impairment, metabolic acidosis
Potential seizure w/ abrupt withdrawal of med
AE: tachycardia, suicidal ideation, acute angle glaucoma, mood and sleep disorder, cognitive impairment, metabolic acidosis
