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Pharmacology - Unit 4 - 10 > Unit 6 - Rx of the CNS > Flashcards

Unit 6 - Rx of the CNS Flashcards

1
Q

Continuum Chart

A
  • death
  • convulsion or seizures
  • tremors and hallucinations
  • anxiety
  • euphoria
  • NORMAL– neutral
  • sedation (drowsy)
  • hypnosis (sleep)
  • general anesthesia
  • coma
  • death
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2
Q

stimulation increases:

A
  • sensory acuity

- motor activity

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3
Q

depression inhibits:

A
  • sensory acuity

- motor activity

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4
Q

CNS stimulants

A

MOA: increase excitability of CNS increases lvls of nor-epi in brain.

Agents:

  • Amphetamines
  • Xanthines
  • Cocaine / cocaine derivatives
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5
Q

Amphetamines:

therapeutic uses for CNS stimulants

A

Amphetamines: narcolepsy, weight control (?), ADHD

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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
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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

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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.
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9
Q

Sedative

A

drugs administered at a dose level to cause mild drowsiness or sedation or to reduce restlessness & anxiety.

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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)

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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.

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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

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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
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14
Q

Benzos: _____ dependent

A

gabba

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15
Q

Therapeutic Uses: Sedative Hypnotics

A
  • relieves anxiety
  • sleep disorders
  • epilepsy (barbiturates)
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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)
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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+
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18
Q

General anesthetics

A

Goals:

  1. Analgesia (narcotics, Ketamine)
  2. Loss of consciousness (gases, nitrous oxide)
  3. Muscle relaxation (maybe curare)
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19
Q

Types

General anesthetics

A
  • inhalation

- IV

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20
Q

Antiepileptic Agents

A

MOA: 2 ways

  1. Decreasing movement of ions into nerve cells (block Na) and therefore, reduce repetitive firing of neurons.
    - Phenytoin, oxycarbazine
  2. Alters activity of neurotransmitter
    (increasing GABA or decrease glutamate)
  • Benzos (clonazepam), Barbiturates (phenobarbital), newer AED’s
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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
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22
Q

Parkinson’s Disease

A

loss of dopaminergic neurons resulting in an imbalance of dopamine and acetylcholine in the basal ganglia (substancia nigra)

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23
Q

Parkinson’s Disease - treatment

A
  • increase dopamine

- decrease acetylcholine

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24
Q

Antiparkinsonian Agents

A
  • Leva-dopa
  • Bromocriptine
  • Selegiline
  • Anticholinergic drugs
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25
Q

Leva-dopa

A

replaces dopamine 

Carbidopa

26
Q

Bromocriptine

A

stimulates postsynaptic dopamine receptors

27
Q

Selegiline

A

decreases MAO-B, which leads to a decrease in the degradation of dopamine

28
Q

Anticholinergic drugs

A

blocks Ach receptors and helps to restore a “false” balance

Artane, Cognetin, Kemadrin

29
Q

Treating Pain

A

Analgesics: agents that relieve pain w/o loss of consciousness.

  • Narcotics (opioids)
  • non-narcotics (salicylate, acetaminophen, NSAIDs)
30
Q

Narcotics

A
  • acts on CNS
  • severe pain
  • assoc w/ tolerance, abuse, physical dependence
31
Q

Non-narcotics

A
  • 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
Q

Salicylates

Therapeutic effects

A
  • 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
Q

Aniline type (acetaminophen)

Therapeutic effects

A
  • relief of pain (same except not OA)
  • antipyretic (decrease fever)
  • NO anti-inflammatory
  • NO anticoagulant
34
Q

Salicylates

Acute Side effects

A

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
Q

Aniline type (acetaminophen)

Acute Side effects

A

GI - NO

CNS stimulation - NO

36
Q

Salicylates

Toxicities w/ Chronic Use

A

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
Q

Aniline type (acetaminophen)

Toxicities w/ Chronic Use

A

No hearing loss

Kidney or liver damage
- irreversible liver damage w/ one overdose of acetaminophen

Blood diseases - anemia

Poss. link to bladder cancer

38
Q

Psychotrophic Agents

A
  • antidepressants
  • antianxiety agents
  • antipsychotic agents
  • drugs to tear Manic Depressive episodes
39
Q

Catecholamine Theory of Mood

A 
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
Q

Depression

A
  • 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
Q

depression characterized by:

A
  • depressive mood
  • loss of interest in activities
  • loss of pleasure in previously satisfying activities
42
Q

Antidepressant agents

A

MOA: increase nor-epi and often serotonin levels in the synapse (mostly re-uptake inhibitors)

43
Q

Antidepressants agents - Drugs

A

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
Q

Antianxiety agents

A

Prescribed more frequently than any other CNS class.
- Designed for short term use. 

Drugs:

  • Sedative Hypnotics (benzodiazepenes) 
  • Beta Blockers
  • Buspirone
45
Q

Psychosis

A

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
Q

Schizophrenia

A

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
Q

Psychosis and Schizophrenia

Treatment goals

A
  • 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
Q

Psychosis and Schizophrenia

side effects

A

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
Q

Drugs to treat Manic Depressive Episodes

A

Lithium is the only drug to specifically treat bipolar disorder

50
Q

Lithium - How does it work?

A

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
Q

Cations w/ Lithium

A

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
Q

All antipsychotic agents block the effects of ________.

A

dopamine

53
Q

A drug that induces a loss of consciousness is a:

A

general anesthetic

54
Q

A common therapeutic use for benzodiazepines is:

A

The treatment for of anxiety disorders

55
Q

Which of the non-narcotic analgesic agents has the potential to cause irreversible liver damage with even a single overdose?

A

aniline derivatives

56
Q

___________ refers to the state where a patient must continue to increase the dose of the drug in order to achieve the desired effect.

A

Tolerance

57
Q

Of the antiepileptic or anticonvulsant drugs:

A

some are general depressants

58
Q

According to the continuum chart, anxiety is a sign of:

A

CNS stimulation

59
Q

What class of antidepressant agents are indicated for severe depression?

A

tricyclics

60
Q

A child taking methylphenidate may experience:

A

all the choices are possibles

  • weight loss
  • malnutrition
  • increased heart rate and/or cardiac arrhythmias
  • supression of growth
61
Q

Parkinsonism may be treated with:

A

anticholinergic drugs

Pharmacology - Unit 4 - 10 (7 decks)

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