Unit 6 - Rx of the CNS Flashcards
(61 cards)
1
Q
Continuum Chart
A
- death
- convulsion or seizures
- tremors and hallucinations
- anxiety
- euphoria
- NORMAL– neutral
- sedation (drowsy)
- hypnosis (sleep)
- general anesthesia
- coma
- death
2
Q
stimulation increases:
A
- sensory acuity
- motor activity
3
Q
depression inhibits:
A
- sensory acuity
- motor activity
4
Q
CNS stimulants
A
MOA: increase excitability of CNS increases lvls of nor-epi in brain.
Agents:
- Amphetamines
- Xanthines
- Cocaine / cocaine derivatives
5
Q
Amphetamines:
therapeutic uses for CNS stimulants
A
Amphetamines: narcolepsy, weight control (?), ADHD
6
Q
Amphetamines:
side effects of CNS stimulants
A
- CNS: to much stimulation…nervousness, anxiety,
sleeplessness - Cardiovascular: too much nor-epi..increase adrenergic response. Increase HR, BP, potential arrhythmias.
- Weight loss, malnutrition
- Kids: suppression of growth
- Possible bone marrow suppression
7
Q
therapeutic uses for CNS stimulants
A
Xanthines: pain from headache (vasoconstriction in brain), asthma, bronchitis, emphysema (bronchorelaxation), counter drowsiness
Cocaine derivates: local anesthetics
8
Q
CNS depressants
A
Agent which decreases excitability of tissue in CNS
- Produces sedation, hypnosis, general anesthesia, coma, death
- All drugs in this category can be used as sedatives, hypnotics or general anesthetics…it is dose dependent.
- Higher the dose the greater the depression.
9
Q
Sedative
A
drugs administered at a dose level to cause mild drowsiness or sedation or to reduce restlessness & anxiety.
10
Q
Hypnotic
A
drugs which are administered at a dose lvl to induce sleep or allow an individual to stay asleep. (they can be awoken from this sleep)
11
Q
General Anesthetic
A
a drug given at a dose to depress the CNS to a degree that causes a loss of consciousness (unarousable), as well as analgesia.
12
Q
Sedative Hypnotic
A
- Oldest, largest and most studied class of CNS drugs
- Produce varying degrees of CNS depression depending on the dose administered
- Produce generalized depression of the cellular activity of many organ systems as well as the tissue w/in CNS
- Synapse is the site of action.
Drug classes: barbiturates
13
Q
Barbiturates and Benzodiazepines
A
MOA: act at gabba receptor / chloride ion channel complex
- Both barbiturates and benzos act on these complexes.
- bind diff allosteric sites
- Gabba is an inhibitory neurotransmitter and will produce inhibitory postsynaptic potentials
- Chloride flows through the channel and decreases resting membrane potential.
- Neuron, therefore, is less likely to be stimulated
14
Q
Benzos: _____ dependent
A
gabba
15
Q
Therapeutic Uses: Sedative Hypnotics
A
- relieves anxiety
- sleep disorders
- epilepsy (barbiturates)
16
Q
Side effects: Sedative Hypnotics
A
- Drowsiness
- Impaired performance or decreased perception
and judgment
- Hangover effect
- Hyperalgesia (barbiturates only)
- Overdose - resp. depression (barbiturates, but can be true of any depressants in combination)
17
Q
Cautions: Sedative Hypnotics
A
- Additive w/ other sedative-hypnotics
- Drug abuse and habituation
- W/drawal state: most severe possible
- Sx can last up to 6 wks+
18
Q
General anesthetics
A
Goals:
- Analgesia (narcotics, Ketamine)
- Loss of consciousness (gases, nitrous oxide)
- Muscle relaxation (maybe curare)
19
Q
Types
General anesthetics
A
- inhalation
- IV
20
Q
Antiepileptic Agents
A
MOA: 2 ways
- Decreasing movement of ions into nerve cells (block Na) and therefore, reduce repetitive firing of neurons.
- Phenytoin, oxycarbazine - Alters activity of neurotransmitter
(increasing GABA or decrease glutamate)
- Benzos (clonazepam), Barbiturates (phenobarbital), newer AED’s
21
Q
Antiepileptic Agents:
Goal of treatment
A
- Control the seizures w/o significant CNS impairment.
Frequent adverse effects:
- Sedation - locomotor and CNS
- Kidney, liver damage
- Blood diseases
- Each agent has it’s own adverse effects
22
Q
Parkinson’s Disease
A
loss of dopaminergic neurons resulting in an imbalance of dopamine and acetylcholine in the basal ganglia (substancia nigra)
23
Q
Parkinson’s Disease - treatment
A
- increase dopamine
- decrease acetylcholine
24
Q
Antiparkinsonian Agents
A
- Leva-dopa
- Bromocriptine
- Selegiline
- Anticholinergic drugs
25
Leva-dopa
replaces dopamine
Carbidopa
26
Bromocriptine
stimulates postsynaptic dopamine receptors
27
Selegiline
decreases MAO-B, which leads to a decrease in the degradation of dopamine
28
Anticholinergic drugs
blocks Ach receptors and helps to restore a “false” balance
Artane, Cognetin, Kemadrin
29
Treating Pain
Analgesics: agents that relieve pain w/o loss of consciousness.
- Narcotics (opioids)
- non-narcotics (salicylate, acetaminophen, NSAIDs)
30
Narcotics
- acts on CNS
- severe pain
- assoc w/ tolerance, abuse, physical dependence
31
Non-narcotics
- acts on PNS and CNS (decrease release of prostaglandins)
- for low to moderate pain (HA, OA, peripheral pain)
- not generally abused, does not cause addiction
32
Salicylates
Therapeutic effects
- relief of pain (HA, dysmenorrhea, OA)
- antipyretic (decrease fever)
- anti-inflammatory (RA, Rheumatic fever - decreases scarring of heart valve)
- anticoagulant effect (Venous or coronary thrombosis, after MI and to help prevent stroke)
33
Aniline type (acetaminophen)
Therapeutic effects
- relief of pain (same except not OA)
- antipyretic (decrease fever)
- NO anti-inflammatory
- NO anticoagulant
34
Salicylates
Acute Side effects
GI irritation and decreased coagulation (bleeding) w/ continued use
- gastric mucosa usually heals in 3 days
- Caution: black stools.
CNS stimulation
- respiratory stimulation to point of respiratory alkalosis
35
Aniline type (acetaminophen)
Acute Side effects
GI - NO
| CNS stimulation - NO
36
Salicylates
Toxicities w/ Chronic Use
Hearing
- ringing in ears
- hearing loss (reversible)
- dizziness (inhibits enzyme in the cochlea)
Possible slight decr. GFR
- negligible compared to phenacetin or even acetaminophen toxicity
- No significant liver damage
- Caution: if patient already has liver or kidney damage
No blood disease
No link to bladder cancer
37
Aniline type (acetaminophen)
Toxicities w/ Chronic Use
No hearing loss
Kidney or liver damage
- irreversible liver damage w/ one overdose of acetaminophen
Blood diseases - anemia
Poss. link to bladder cancer
38
Psychotrophic Agents
- antidepressants
- antianxiety agents
- antipsychotic agents
- drugs to tear Manic Depressive episodes
39
Catecholamine Theory of Mood
```
Norepinephrine imbalances implicated
- Low levels --> depression
- High levels --> anxiety
Has been expanded to include Serotonin ...still probably OVER SIMPLIFIED
```
Yet 2/3 of patients are helped by increases in these neurotransmitters.
40
Depression
- Can occur as a natural component of psychological processes and as a result of pathological processes
- Can occur as a primary affective disorder, a reaction to drug(s), as well as with a wide variety of diseases.
- Twice as common in women
- Suicide is 30x more likely in a depressed individual
- Total cost (5yrs ago) of depression in the US = 50 billion $/yr
41
depression characterized by:
- depressive mood
- loss of interest in activities
- loss of pleasure in previously satisfying activities
42
Antidepressant agents
MOA: increase nor-epi and often serotonin levels in the synapse (mostly re-uptake inhibitors)
43
Antidepressants agents - Drugs
Tricyclics (DOC for severe depression)
- Amitriptyline (Tryptizol, Domical, Lentizol, Limbitrol, Triptafen)・Clomipramine (Anafranil)・ Imipramine (Tofranil)・Lofepramine (Gamanil)
Monoamine Oxidase Inhibitors (efficacious but drug/drug and drug/food interactions are common)
Newer agents:
- Serotonin reuptake inhibitors
- Tetracyclics
44
Antianxiety agents
Prescribed more frequently than any other CNS class.
- Designed for short term use.
Drugs:
- Sedative Hypnotics (benzodiazepenes)
- Beta Blockers
- Buspirone
45
Psychosis
Severe mental disorder characterized by:
- disordered thought processes
- Blunted or inappropriate emotional responses
- Bizarre behavior (hypo or hyperactivity, agitation,
aggressiveness, hostility, combativeness, social withdrawal)
- Hallucinations
- delusions
46
Schizophrenia
etiology unclear.
- Most likely results from abnormal neurotransmission in the brain
- Dopamine implicated (high lvls)
- Drug therapy is aimed at block dopamine transmission (also some serotonin)
47
Psychosis and Schizophrenia
Treatment goals
- reduce the bizarreness of behavior
- do not expect a cure
THERAPEUTIC USES:
- Schizophrenia
- Manic phase of bipolar disorder
- Antiemetic & hiccups (?!!)
MOA: blocks dopamine receptors in the chemoreceptor trigger zone
48
Psychosis and Schizophrenia
side effects
Sedation - big problem
Fatigue, indifference, apathy, drastic changes in
personality
Anticholinergic: dryness
Antiadrenergic effects: orthostatic hypotension
Extrapyramidal effects: repetitive, involuntary, purposeless movements of lips, face and torso (looks like movement disorders of Parkinson’s Disease)
Endocrine imbalances (depression of the hypothalamus)
49
Drugs to treat Manic Depressive Episodes
Lithium is the only drug to specifically treat bipolar disorder
50
Lithium - How does it work?
Lithium competes with calcium, magnesium, potassium and
sodium in body tissues and at binding sites.
It alters sodium transmission in nerve and muscle cells.
It effects a shift toward intraneural catecholamine metabolism.
The specific MOA in mania is unknown, but it does affect the synthesis, storage, release and reuptake of the central monoamine neurotransmitters (NE, 5-HT, DA, Ach and GABA).
Its antimanic effects may be the result of increases in NE uptake and increases in serotonin receptor sensitivity.
51
Cations w/ Lithium
Abnormal sodium loss
Lithium competes w/ sodium for reabsorption at the proximal tubule. If sodium levels are low, more lithium will be reabsorbed.
Possible pathological renal damage
Endocrine Abnormalities
- Hypothyroidism
- Diabetes insipidus
Dangers in Pregnancy
- Cardiovascular malformations, kidney damage, euthyroid goiter, hypoglycemia
52
All antipsychotic agents block the effects of ________.
dopamine
53
A drug that induces a loss of consciousness is a:
general anesthetic
54
A common therapeutic use for benzodiazepines is:
The treatment for of anxiety disorders
55
Which of the non-narcotic analgesic agents has the potential to cause irreversible liver damage with even a single overdose?
aniline derivatives
56
___________ refers to the state where a patient must continue to increase the dose of the drug in order to achieve the desired effect.
Tolerance
57
Of the antiepileptic or anticonvulsant drugs:
some are general depressants
58
According to the continuum chart, anxiety is a sign of:
CNS stimulation
59
What class of antidepressant agents are indicated for severe depression?
tricyclics
60
A child taking methylphenidate may experience:
all the choices are possibles
- weight loss
- malnutrition
- increased heart rate and/or cardiac arrhythmias
- supression of growth
61
Parkinsonism may be treated with:
anticholinergic drugs
