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Advanced Pharmacology > Nervous System Rx > Flashcards

Nervous System Rx Flashcards

1
Q

Name the neurotransmitters and whether they are excitory or inhibitory

A

Norepinephrine- primarily excitatory/ inhibitory in some areas
Serotonin- excitatory/inhibitory
Dopamine- primarily inhibitory
Gamma aminobutyric acid (GABA)- major inhibitory
Acetylcholine (ACh)- excitatory
Glutamate- major excitatory

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2
Q

What are the theories behind depression disorders?

A

older theory- decreased activity of monoamines (norepi, serotonin, dopa)
contemporary theory- neuroendocrine dysfunction leads to neuroplasticity, decreasing monoamin concentrations; chronically increased cortisol, dysregulation of brain derived neurotropic factor (BDNF)

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3
Q

What is the goal of antidepressive therapy?

A

complete remission without relapse or recurrence- often not achieved with 1st drug or takes combo Rx

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4
Q

What is the mechanism of action of SSRIs?

A

Selective Serotonin Reuptake Inhibitors

selectively blocks reuptake of serotonin by presynaptic terminal => increased serotonin available for neurotransmission

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5
Q

What are the indications for SSRIs?

A

1st line for Depression
Also OCD, panic disorders, anxiety, bulimia
NOT useful for pain disorders
Takes 2-12 weeks for effective treatment

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6
Q

Name common SSRIs

A 
Cetalopram (Celexa)
Escitalopram (Lexapro)
Fluoxetine (Prozac)
Fluvoxamine (Luvox)
Paroxetine (Paxil)
Sertraline (Zoloft)
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7
Q

What are adverse effects of SSRIs?

A

Akathisia (EPS)- inability to sit still, restlessness
Headache - common complaint early in Rx
Tinnitus
Sexual dysfunction
early wt loss followed by wt gain
serotonin syndrome-greatest risk if on >1 serotonergic drug
withdrawal if abruptly stopped (antidepressant discontinuation syndrome), esp. shorter half-life: HA, malaise, flu-like sx, agitation

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8
Q

What are the symptoms of serotonin syndrome?

A

mild- agitation, jitter, tremor; increased BP/pulse; diarrhea
severe- mydriasis (dilated pupils), diaphoresis, agitation, tachycardia, HTN, diarrhea, clonus/tremor/hyperreflexia (> in LE)

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9
Q

What are notable drug interaction for SSRIs?

A

Heterocyclics- increase levels
Warfarin- potentiates bleeding
Tamoxifen- decreases efficiency
Consider CYP450 with Paroxitine and Fluoxetine

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10
Q

Fluoxetine (Prozac)

A

SSRI- “activating”- good for lethargy
unique 5HT2c antagonist property
complements olanzapine - used together for bipolar
markedly long half-life => weekly dosing available

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11
Q

Sertraline (Zoloft)

A

SSRI
dopamine transport inihibition and sigma-1 receptor binding => produce activation in pts with low energy
frequently combined with bupropion
movre helpful in psychotic depression

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12
Q

Paroxetine (Paxil)

A
  • SSRI - Anxiety (often 1st line)
  • anticholinergic and norepi transmitter inhibition function => calming
  • concern for rebound if withdrawn suddenly
  • short half-life- often prescribed QHS
  • Not good for breastcancer hx or high risk
  • If used with pravastatin- increased serum glucose
  • Do not take if pregnant
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13
Q

Fluvoxamine (Luvox)

A

SSRI

  • potent sigma-1 binding
  • used primarily for OCD, social anxiety, and panic disorder
  • approved for children
  • less sexual dysfunction
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14
Q

Citalopram (Celexa)

A

SSRI- anxiety/depression
mild antihistamine properties - good for anxiety
well tolerated in elderly
inconsistent response in lower doses, but concern for prolonged QT on higher doses (FDA- no >40 mg/day)

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15
Q

Escitalopram (Lexapro)

A

SSRI- anxiety/depression

  • best tolerated SSRI, lower doses are usually effective
  • few drug interactions
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16
Q

What are SPARIs?

A

Serotonin partial agonist/reuptake inhibitors
Vilazodon (Viibryd) and Vortioxetine (Trintellix)
newest class of antidepressants
similar to SSRI, plus serotonin agonist
rapid onset, but worse GI side effects
lesser sexual side effects

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17
Q

What is the mechanism of action of SNRIs?

A

serotonin/norepinephrine reuptake inhibitors => increased serotonin and norepi available => effective against depression and neuropathic pain

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18
Q

Name SNRIs

A

Venlafaxin (Effexor)
Duloxitine (Symbalta)
Desvenlafaxine (Pristiq)
Levomilnacipran (Fetzima)

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19
Q

What are indications for SNRIs

A

Depression (2nd line)
Anxiety
depression with associated pain
*needs to be titrated down over >4 wks

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20
Q

What are adverse effects of SNRIs?

A

similar to SSRIs- nausea, anxiety, drowsiness, insomnia, sexual dysfunction
HTN (venlafaxin in high doses)

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21
Q

Buprion (Wellbutrin)

A

NDRI- norepi/dopamine reuptake inhibitor =>increased dopamine and norepi available
Used for depression and to inhibit cravings (smoking)
helpful for reduced positive affect/ anhedonia
less sexual side effects

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22
Q

Mirtazapine

A

Enhances noradrenergic and sertoninergic release by blocking presynaptic receptors
potent antihistimine effect => sedative
lesser sexual side effects

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23
Q

L-methylfolate (Deplin)

A

monoamine modulator- facilitates amine synthesis to make patients more responsive to antidepressants
available as “medical food”

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24
Q

What is the mechanism of action of Heterocyclics (TCAs)

A

block reuptake of norepi and serotonin
potent muscarinic antagonist (anticholinergic)
weak alpha1 receptor and histimine antagonist

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25
Q

Name heterocyclic drugs

A

Imipramin (Toranil)
Amitriptyline (Elavi)
Doxepin (Sinequin)
Trimipramine (Surmontil)

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26
Q

What are side effects of heterocyclics?

A

anticholinergic effects (dry mouth, constipation, urinary rentention, blurry vision, heart block, slowed gastric emptying
orthostatic hypotension, tachycardia
sedation, drowsiness
CNS hyperactivity- lower seizure threshold

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27
Q

What contraindications are there for heterocyclics?

A

acute MI recovery
conduction blocks
severe hepatic/renal impairment

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28
Q

What is the mechanism of action of MAOIs?

A

Monamine oxidase inhibitors => inhibit oxidation of monamines => decreases degradation of neurotransmitters => increased norepi, serotonin, and dopamine
*Especially helpful in anxiety, but often last line

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29
Q

Name MAOIs

A

Isocarboxazid (Marplan)
Phenelzine (Nardil)
Tranylcypromine (Parnate)
Selegiline patch (EMSAM)

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30
Q

What are side effects for MAOIs?

A

HTN
dysrhythmias
anticholinergic effectsd
many drug-drug and drug-food interactions: Tyramine-containing foods (cheese, beer, chocolate, red wine, aged meats)

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31
Q

How is unipolar depression Rx managed

A

1) SSRI
2) SNRI
3) reconsider diagnosis - bipolar could be worsened on antidepressants
4) expand from antidepressant spectrum
5) consider atypical antipsychotics- Abilify, Symbyax, Seroquel
6) consider alternative antidepressant- Lithium, Liothyronine, Buspiron

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32
Q

What are atypical antipsychotics

A

Ariprazole (Abilify)
Olanzapine/fluoxeitine (Symbyax)
Quetiapine (Seroquel)
Brexpiprazole (Rexulti)
*best for patients with treatment-resistant depression, bipolar, or depression with psychotic features
*may cause more adverse metabolic effects (obesity, hyperglycemia, dyslipidemia)

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33
Q

Lithium

A

atypical antidepressant
often used for bipolar disorder
demonstrates suicidality improvement

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34
Q

Liothyronine

A

Alternative antidepressant
“T3”- can be used for unipolar depression
pts need to have normal thyroid studies and agree to monitoring of TSH levels

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35
Q

Buspirone

A
  • alternative antidepressant
  • serotonin agonist that may also trigger oxytocin release
  • Effective for generalized anxiety disorder - alternative to benzos as not addicting
  • not meant for acute management of anxiety (delayed onset)
36
Q

What is the difference between generalized and partial seizure disorders?

A

Generalized- diffuse, bilateral brain involvement

Partial- localized to one part of brain; manifestations depend on part of brain involved

37
Q

How do antiseizure medications work?

A

decrease the neuronal excitability and raise the seizure threshold by inhibiting glutamate and/or potentiating GABA
Glutamate antagonist, GABA agonists, or SV2A binding

38
Q

Name medications for seizure disorders

A 
Brivaracetam (Briviact)
Levetiracetam (Keppra)
Phenytoin (Dilantin)
Fosphenytoin (Cerebryx)
Lamotrigine (Lamictal)
Gabapentin (Neurontin)
Divalproex (Depakote)
Carbamazepine (Tegretol)
Oxycarbamazepine (Trileptal)
Benzodiazepines (Valium, Ativan) - acute management
39
Q

How is treatment for seizure disorders managed?

A

Often only requires one drug
If first drug does not work at max doses, gradually add another and then taper off the first
*concern for increased risk of suicidal thoughts on AEDs

40
Q

Phenytoin (Dilantin)

A

Antiepileptic
has zero order kinetics- it saturates its routes of elimination, so the higher the concentration of drug, the longer the half-life

41
Q

Carbamazepine (Tegretol)

A

Antiepileptic

  • causes auto-induction of its own metabolism- may need dose increases throughout therapy
  • may cause hypersensitivity reaction in certain patients, esp of Asian descent- test for HLA-B1502 gene
42
Q

Fosphenytoin (Cerebryx)

A

Antiepileptic
prodrug that is rapidly converted to phenytoin
given parenterally

43
Q

Topiramate (Topamax) and Zonisamide (Zonegran)

A

Antiepileptics
Carbonic anhydrase inhibitors
increased risk for metabolic acidosis- early in rx, monitor HCO3 prior to treatment

44
Q

Valproic Acid (Depakote)

A

Antiepileptic

pts may develop pancreatitis

45
Q

What is the pathophysiology of Parkinson disease?

A

Loss of dopamine-containing neurons in substantia nigra => ACh (excitatory) is uninhibited and overactive => loss of control over muscle movements

46
Q

Levodopa/Carbidopa

A

Drugs for Parkinson disease

  • Levodopa- dopamine precursor that crosses blood-brain barrier and breaks down into dopamine
  • Carbidopa- dopamine decarboxylase inhibitor that reduces metabolism of dopamine
  • Adverse effects- anorexia, nausea, tachycardia, hypotension, flushing, hallucinations
  • on-off phenomena- symptoms worsen throughout day
47
Q

Name Dopamine receptor agonists

A 
*Parkinson disease*
Bromocriptine (Parlodel)
Pramipexole (Mirapex)
Ropinirole (Requip)
Cabergoline (Dostinex)
Rotigotine patch (Neupro)
48
Q

What is the mechanism of action of Dopamine receptor agonists?

A

stimulate dopamine receptors in basal ganglia
used to treat parkinson’s disease- most useful early in treatment
1st line in younger patients (<70) to delay symptoms for 5 years

49
Q

What are adverse effects of Dopamine receptor agonists?

A 
anorexia, N/V
postural hypotension
HA
cardiac dysrhythmia
drowsiness
50
Q

What is the use of anticholinergics in managing parkinsons?

A
  • reduces the impact of unihibited ACh release
  • Benztropine and Trihexyphenidyl
  • typical anticholinergic side effects
51
Q

What are COMT inhibitors?

A
  • for parkinson’s disease
  • Catechol-O-methyl transferase inhibitors => blocks breakdown of dopamine
  • Entacapone (Comtan) and tolcapone (Tasmar)
  • tolcapone associated with hepatotoxicity (check LFTs)
  • used if not responding to other treatment- discontinue if not working in 3 weeks
52
Q

What are MAO-B inhibitors?

A
  • for parkinson’s disease
  • inhibits breakdown of dopamine
  • should be given with Levodopa
  • Selegiline (deprenyl)
53
Q

What are side effects of COMT and MAO-B inhibitors?

A 
orthostatic hypotension
HTN
dysrhythmia
psychotic symptoms
*not to be used with heterocyclics
54
Q

What is the patho of Alzheimer’s disease?

A

production of apolipoprotein E => accumulation of amyloid plaques in brain => loss of neurons in limbic pathway that drives memory => decreased ACh activity

55
Q

What is the focus of pharmacologic treatment of Alzheimer’s?

A

prolonging ACh breakdown to allow for greater opportunity for ACh binding at receptor sites

56
Q

What are adverse effects of AChE inhibitors?

A
  • inhibit breakdown of ACh by acetylcholinesterase =>cholinergic stimulation => modest reduction in Alzheimers sx
  • bradycardia, tremors, myalgia, syncope, N/V, diarrhea
57
Q

Donepezil (Aricept)

A

AChE inhibitor- Alzheimers Rx

CYP450 metabolism, but no hepatotoxicity

58
Q

Galantamine (Razadyne)

A

AChE inhibitor- Alzheimers Rx
CYP450 metabolism
available in ER, IR, and liquid forms

59
Q

Rivastigmine (Exelon)

A

AChE inhibitor- Alzheimers Rx
available PO and as patch- take with food
fewer drug interactions (no CYP450)

60
Q

Memantine HCl (Namenda)

A
  • NMDA receptor antagonist - Alzheimers Rx
  • blocks overactive glutamate from binding to NMDA receptors, preventing cognitive damage
  • Minimal side effects and drug interactions
  • For moderate-severe AD
  • often given as in combo with AChE inhibitor
61
Q

How is hypersexuality associated with Alzheimer’s managed?

A
  • discontinue benzodiazepines
  • consider Cimetidine- has antiandrogen effect
  • consider SSRIs
  • consider Seroquel
62
Q

What part of the brain is highly involved in anxiety disorders?

A

The Amygdala - flight, fight, or freeze (fear/anxiety)

The CSTC Loop- apprehension/worry

63
Q

What neurotransmitters are involved in anxiety?

A

GABA
Norepinephrine
dopamine
Serotonin

64
Q

What medication classes are often used for treatment of chronic anxiety?

A
  • SSRIs/SNRIs- often require higher doses than for depression
  • Buspirone
  • Benzodiazepines
  • Alpha2 ligands
65
Q

What are Alpha2-delta Ligands?

A
  • Gabapentin (Neurontin) and Pregabalin (Lyrica)
  • block excitatory neurotransmitters- glutamate
  • effective for social anxiety and panic disorder
66
Q

What are first line therapies for generalized anxiety disorder?

A

SSRI/SNRI
Buspirone
Alpha2-delta ligands
benzodiazepines

67
Q

What are first line therapies for PTSD?

A

SSRI/SNRI

*pharmacotherapy not preferred

68
Q

What are first line therapies for Panic disorder?

A

SSRI/SNRI
Benzodiazepines
Alpha-2-delta ligands

69
Q

What are first line therapies for social anxiety?

A 
SSRI/SNRI
Alpha-2-delta ligands
beta blockers (alternative option)
70
Q

What is the drug of choice for acute anxiety?

A

Benzodiazepines

71
Q

What are Benzodiazepines?

A
  • Very effective for acute anxiety- subject to abuse
  • metabolized by liver
  • Function as GABA agonists => inhibits motor responses triggered by amygdala => CNS depressant
  • used for acute anxiety, panic attacks
  • should be tapered off slowly
72
Q

Name benzodiazepines

A
  • Alprazolam (Xanax) (panic disorders)
    • Diazepam (Valium) (generalized anxiety)
    • Chlordiazepoxide (Librium) (alcohol w/d)
    • Lorazepam (Ativan) (generalized anxiety)
    • Temazepam (Restoril) (sleep disorder)
    • Clonazepam (Klonopin) (maintenance)
    • Oxazepam (Serax) (may be safer in liver dz)
73
Q

What alternatives are there to benzodiazepines for acute anxiety?

A 
First generation antihistamines (hydroxyzine)
Antiadrenergic agonists (clonidine)
Beta blockers (propranolol)
* useful in cases of addictive behaviors
74
Q

What is insomnia?

A

Difficulty falling asleep or staying asleep, waking early morning, non-restorative sleep
often undertreated

75
Q

What is acute vs chronic insomnia?

A

Acute- identifiable trigger, doesn’t last >4 mnths

Chronic- predisposing factors, multifactorial, > 4 mnths

76
Q

What is associated insomnia?

A

related to underlying mood disorder

77
Q

How is insomnia therapy managed?

A
  1. BzRAs or melatonin agonist
  2. Sedating antidepressants
  3. Antiepileptics
  4. 2nd Generation antipsychotics
78
Q

What are Benzodiazepine receptor agonists (BzRAs)?

A
  • used for insomnia, not intended for long-term
  • Triazolam
  • Estazolam
  • Temazepam
  • Flurazepam
79
Q

What are non-benzodiazepine receptor agonists?

A

For insomnia, The “Z” drugs:

  • Zolpidem (Ambien)
  • Zaleplon (Sonata)
  • Eszopiclone (Lunesta)
  • minimize adverse effects and abuse potential
80
Q

Zolpidem (Ambien)

A

Insomnia

  • adverse effects- AM hangover, anterograde amnesia
  • CYP450 considerations
81
Q

Zaleplon (Sonata)

A

Insomnia- esp middle-of-night awakenings
Rapid onset/short half-life
no issue with morning grogginess

82
Q

Eszopiclone (Lunesta)

A

Insomnia

  • longer half-life
  • CYP450 considerations
  • AM hangover
83
Q

Ramelteon (Rozarem)

A

Insomnia- difficulty falling asleep

  • Melatonin agonist
  • no fall risk or cognitive impairment
  • CYP450 considerations
84
Q

Doxepin (Silenor)

A

Tricyclic antidepressant approved for insomnia

- do not take with food

85
Q

Suvorexant (Belsomra)

A

Insomnia
Orexin receptor antagonist- improves total sleep time and sleep onset
need planned >7 hrs of sleep

Advanced Pharmacology (9 decks)

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