Antiepileptics/CNS stimulants/Antiparkisonian Flashcards
(99 cards)
1
Q
Term used to designate a group of chronic central nervous system (CNS) disordered characterized by the onset of sudden disturbances of sensory, motor, autonomic, or psychic origin
A
Epilepsy
2
Q
Goal of epilepsy treatment
A
control seizures with minimal medication related adverse effects
3
Q
Antiepileptics are dosed based on _____ function
A
renal
4
Q
Antiepileptics that rely on renal excretion:
A
Gabapentin Pregabalin Levitiracetam Vigabatrin Zonisamide
5
Q
Principle binding protein for anti epileptic drugs
A
Albumin
6
Q
Highly protein bound antiepileptics
A
Phenylbutazone
Thyroxine
Salicylates
7
Q
Antiepileptics that compete for protein binding sites of highly bound antiepileptic drugs, can displace the bound drug and lead to increase in the plasma concentration:
A
Phenytoin
Valproate
Carbamazepine
8
Q
Enzyme-inducing anti epileptic drugs (7)
A
PPPCLOT Phenobarbital Phenytoin Primidone Carbamazepine Lamotrigine Oxycarbazepine Topiramate
9
Q
Enzyme-inducing anti epileptics affect which cytochrome?
A
p450
10
Q
Enzyme-inducing anti epileptics and oral contraceptives
A
anti epileptics render oral contraceptives ineffective, higher dose required
11
Q
Enzyme-inducing anti-epileptics and induction drugs
A
Increased dose requirements of: thiopental propofol midazolam ipioids non-depolarizing neuromuscular blocking drug
12
Q
Phenytoin is ___% protein bound
A
90%
13
Q
Phenytoin goal plasma concentration and its metabolism is unique:
A
Control of seizures is usually obtained when plasma concentrations are 10-20 ug/ml
When plasma concentration <10, first order kinetics
When plasma concentrations >10, zero order kinetics (saturated and dose dependent)
PLASMA CONCENTRATION MONITORING
14
Q
Only agent for which plasma concentration monitoring is recommended due to nonlinear saturation dose kinetics
A
Phenytoin
15
Q
Na, Ca, Na+Ca, or GABA?
Phenytoin
A
Na+ Ca
16
Q
Na, Ca, Na+Ca, or GABA?
Carbamazepine
A
Na+ Ca
17
Q
Na, Ca, Na+Ca, or GABA?
Phenobarbital
A
Ca and GABA
18
Q
Na, Ca, Na+Ca, or GABA?
Benzodiazepines
A
GABA
19
Q
Na, Ca, Na+Ca, or GABA?
Ethosuximide
A
Ca Channel
20
Q
Na, Ca, Na+Ca, or GABA?
Primidone
A
Na
21
Q
Na, Ca, Na+Ca, or GABA?
Valproate
A
Na + Ca
22
Q
Na, Ca, Na+Ca, or GABA?
Lamotrigine
A
Na + Ca
23
Q
Na, Ca, Na+Ca, or GABA?
Zonisamide
A
Na + Ca
24
Q
Gabapentin acts on what?
A
GABA
25
Phenobarbital class
barbiturates
26
Phenobarbital is a second line anti epileptic due to _____
cognitive and behavioral SE
27
Phenobarbital SE in adult
sedation
28
Phenobarbital SE in peds
hyperactivity
29
Phenobarbital drug interaction:
accelerates interactions with lipid soluble drugs
30
Phenobarbital prolongs ___ channel opening and limits the spread of seizure activity and increases seizure threshold
Cl
31
Drug of choice for Digitalis arrhythmias
Phenytoin
32
Goal plasma concentration of phenytoin
10 to 20 ug/ml
33
Adverse side effects phenytoin
nystagmus, diplopia, vertigo, ataxia, neurotoxic effects
34
Phenytoin induces lipid soluble drugs...
carbamazepine, valproid acid, ethosuximide, anticoagulants, corticosteroids
35
Phenytoin and NMB
need higher doses of non-depolarizers
36
Valproic acid (inhibits/induces) metabolism
inhibits
37
valproic acid and phenytoin
Valproic acid slows metabolism of phenytoin
38
valproic acid and phenobarbital
valproic acid causes phenobarbital plasma concentration to increase by 50%
39
first line treatment for status epilepticus
Diazepam
40
first line treatment for local anesthetic induced seizures
diazepam
41
Status epilepticus:
patient experiences prolonged or rapidly recurring convulsions for 5 minutes or more
42
____ seizure control is associated with improved clinical outcome
rapid
43
Diazepam route in status epilepticus
IV or rectal
44
Other status epilepticus drugs:
fosphenytoin, phenytoin, phenobarbital, valproic acid, levetiracetam, propofol
45
fosphenytoin SE
hypotension and prolongation of QT interval
46
Parkinsons Disease (definition)
chronically progressive neurodegenerative disease results from the loss of dopaminergic neurons in the substantia migration pars compact region of the basal ganglia
47
Principle inhibitory neurotransmitter in Parkisons
Dopamine
48
Goal of Parkinsons treatment
treat debilitating symptoms
49
Does dopamine cross BBB?
No
50
T/F: Parkinsons medications can slow progression of the disease
False, all medications are palliative
51
Parkinsons treatment:
administration of levodopa (dopamine precursor) or drugs that mimic dopamines action
52
When pharmacological options fail for parkinsons, next step is
DBS
53
Does levodopa cross BBB?
yes
54
Where is levodopa metabolized to dopamine?
liver (95%)
55
Levodopa SE:
NV, dyskinesia, psychosis, cardiac dysrhythmias, flushing of skin, orthostatic hypotension, RED/BLACK URINE
56
How to minimize levodopa SE:
administer with peripheral decarboxylase inhibitor
57
Drugs to avoid in Parkinsons:
antipsychotics (butyphenones, phenothiazines)
droperidol
Metoclopramide
58
What vitamins increases metabolism of levodopa
Pyridoxine (B6)
59
What drug class improves symptoms of Parkinsons disease?
anticholinergics
60
MAO-inhibitors in Parkinsons:
increase intra-synaptic time of dopamine
61
Peripheral Carboxylase inhibitors to give with levodopa
Carbidopa and Benserazide
62
Monoamine Oxidase Type B enzyme inhibitors (tx of Parkinson's)
Selegiline
63
Catechol-O-Methyltransferase Inhibitors and SE
| parkinsons pharmacotherapy
Tolcapone: Hepatotoxicity and Rhabdomyolysis
Entacapone: orange urine
64
synthetic dopamine agonists allow you to
reduce the dose of levodopa
65
synthetic dopamine agonists SE:
Visual & auditory hallucinations, hypotension, dyskinesia
Erythromelalgia- red, edematous, tender extremities
Pulmonary fibrosis and effusions
66
synthetic dopamine agonists (drug names)
Bromocriptine & Pergolide (tetracyclic ergot alkaloids)
| Pramipexole, Ropinirole & Rotigotine (nonergot alkaloids)
67
Amantadine
antiviral (prophylaxis influenza A)
MOA unknown
SE: anticholinergic, ankle edema, lived reticularis
68
Doxapram use
temporary measure to maintain ventilation during administration of O2 to patients with COPD who are dependent on the hypoxic drive
69
Doxapram function:
centrally active analeptic that selectively increases MV (by increasing TV) by activating the carotid bodies
70
Doxapram and volatile anesthetics:
Arousal from the residual effects of inhaled anesthetics follows the administration of doxapram but the effects are transient, nonselective, & not recommended.
71
SE of Doxapram/CNS stimulation:
```
Hypertension
Tachycardia,
Cardiac dysrhythmias
Vomiting
Increased body temperature
```
72
Stimulation produced by Doxapram is similar to that produced by a PaO2 of ___ mm/Hg acting on the carotid bodies
38
73
Methylxanthines (list of drugs)
Caffeine
Theophylline
Theobromine
74
Methylxanthines clinical uses:
Primary apnea of prematurity by stimulating medullary respiratory centers by increasing the sensitivity of these centers to carbon dioxide
75
Methylxanthines MOA:
Stimulate the CNS
Produce diuresis
Increase myocardial contractility
Relax smooth muscle, especially those in the airways
76
Caffeine clinical uses
Neonates apnea of prematurity
Post-dural headache
Common cold
77
Methylphenidate:
mild CNS stimulant related to amphetamine
| used for tx of ADHD and narcolepsy
78
Methylphenidate SE:
Hypertension, tachycardia, priapism, seizures, & serious cardiovascular events such as sudden cardiac death, stroke, & myocardial infarction have been described in patients treated with methylphenidate
79
Baclofen is an agonist at the
GABA-B receptor
80
How does Baclofen work?
centrally acting muscle relaxant
suppresses neuronal transmission in cerebral cortex
inhibits excitatory impulses at the spinal cord level
81
What is baclofen used for?
to treat spastic movements in patients with cerebral palsy and spinal cord injuries
to treat central neuropathic pain
82
How is baclofen excreted?
kidneys (80%)
83
Baclofen SE:
sedation, confusion, skeletal muscle weakness
84
Baclofen and General Anesthesia:
Brady, hypotension, delayed awakening
85
Sudden withdraw from Baclofen:
multi-organ system failure, tachycardia, hallucinations
86
Do you modify dose of baclofen in renal failure?
yes
87
Does baclofen work at neuromuscular junction?
NO
88
Cocaine as a CNS stimulant
inhibits NE and dopamine reuptake
89
Cocaine has high abuse potential due to
euphoric effects caused by inhibition of catecholamine uptake, especially dopamine
90
Chronic cocaine use leads to:
cardiomyopathy, HTN, MIs, aortic dissection, psychosis
91
Chronic cocaine use and dopamine:
dopaminergic dysfunction due to dopamine depkletion
92
How is cocaine metabolized?
plasma esterases
93
cocaine and GA:
exaggerated cardiac stimulating effects
94
How does cocaine affect O2 demand?
increases O2 demand
95
Dantrolene MOA
binds to ryanodine calcium channel and reduces Ca efflux from the sarcoplasmic reticulum, counteracting the abnormal intracellular Ca levels accompanying MH
direct action on excitation-contraction coupling
decreases the amount of calcium released by sarcoplasmic reticulum
96
Does dantrolene work at NMJ?
No
97
T/F: Dantrolene produces skeletal muscle relaxation
True
98
Dantrolene SE
liver dysfunction/hepatotoxicity
99
Dantrolene Dose
2.5 mg/kg IV until symptoms subside
| or cumulative dose of 10 mg/kg IV reached
