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Systemic Pharmacology > 2 - Neuromodulators > Flashcards

2 - Neuromodulators Flashcards

1
Q

what are 3 amphetamine-based stimulants (psychomotor stimulants)?

A

amphetamine (Adderall), dextroamphertamine (Dexedrine), methylphenidate (Ritalin, Concerta)

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2
Q

what are the indications for amphetamine?

A

ADHD and narcolepsy

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3
Q

what is the mechanism of action for amphetamine?

A

stimulates CNS through sympathomimetic mechanism - enhanced release and reduced re-uptake of NE and E

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4
Q

what are some common side effects for amphetamine?

A

sympathomimetic = photosensitivity, visual disturbance, elevated BP, infection, headaches

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5
Q

what are some serious side effects for amphetamine?

A

dependency, abuse, psychosis, growth suppression, heart failure, stevens-johnson syndrome

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6
Q

which two types of drugs will have an additive effect with amphetamine?

A

NSAIDs (caffeine based) and decongestants

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7
Q

what three types of drugs when combined with amphetamine create hypertensive crisis?

A

sympathomimetics, ophthalmic beta-blockers and alpha2 agonists

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8
Q

what happens when CAIs are taken with amphetamine?

A

renal excretion decreased in alkaline urine

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9
Q

Ex: you have a patient with ADHD and is taking Visine. If you need to dilate them what drug should you use?

A

tropicamide - not phenylephrine (decongestant)

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10
Q

what is a contraindication for amphetamine?

A

glaucoma (glaucoma is treated with drugs that block sympathetic activity and amphetamine enhances sympathetic activity)

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11
Q

what are the 5 antidepressant drug classes?

A

SSRIs, SNRIs, TCADs, atypical and MAOIs

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12
Q

what are TCADs inhibiting?

A

very non-selective = inhibit re-uptake of NE, serotonin and dopamine

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13
Q

what are the 6 SSRI antidepressants?

A

Excitalopram (Lexapro), Sertraline (zoloft), fluozetine (prozac), paroxetine (paxil), fluvoxamine (luvox), citalopram (celexa)

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14
Q

what is escitalopram indicated for?

A

major depressive disorder and generalized anxiety disorder

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15
Q

what is the mechanism for escitalopram?

A

selective serotonin re-uptake inhibitor (SSRI)

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16
Q

what are the distinguishing side effects for escitalopram (SSRIs)?

A

suicidal risk, serotonin syndrom, neuroleptic malignant syndrome (NMS), seizures

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17
Q

what are the ocular side effects for escitalopram (SSRIs)?

A

dry eye, blur, diplopia, conjunctivitis, ptosis = all due to sympathomimetic effect

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18
Q

what causes 5-HT syndrome in SSRIs?

A

the excessive serotonin overwhelms the effects of dopamine and the body doesn’t recognize dopamine like it normally would

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19
Q

what symptoms can occur with low levels of dopamine (or with 5-HT syndrome, NMS)?

A

parkinson like symptoms = life-threatening, bradykinesia/muscle rigidity (elevated CPK) and leukocytosis

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20
Q

what happens if you take escitalopram with NSAIDs and omega-3?

A

hemorrhage risk = reduced serotonin reduces platelet clotting (patient may have sub-conjunctival hemorrhage)

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21
Q

what happens if you take escitalopram with ophthalmic beta-blockers?

A

reduced metabolism of beta-blockers = side effects will be enhanced, may need to reduce dose/concentration

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22
Q

what are 3 SNRI antidepressants?

A

duloxetine (cymbalta), venlafaxine (effexor), and desyenlafaxine (pristiq)

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23
Q

what is the indication for duloxetine?

A

depression, anxiety, nueropathic pain (DM) and fibromyalgia

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24
Q

what is the pharmacology for duloxetine?

A

antidepressant, analgesic: SNRI

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25
Q

what is the mechanism of action for duloxetine?

A

selective serotonin and norepinephrine re-uptake inhibitor (SNRI)

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26
Q

what are the common side effects for duloxetine?

A

sympathomimetic effects = blurred vision, headache, dizziness, sweating, ED, HTN, orthostatic hypotension, syncope, yawning, constipation

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27
Q

what is the distinguishing side effect for duloxetine?

A

serotonin syndrome

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28
Q

what hypersensitivities may occur with duloxetine?

A

angioedema and stevens-johnson syndrome

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29
Q

what is the ocular side effect for duloxetine?

A

glaucoma

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30
Q

what happens if you take opioids with duloxetine?

A

there is an additive effect = risk of 5-HT syndrome/NMS increases

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31
Q

what happens if you take NSAIDs and omega-3,6 with duloxetine?

A

hemorrhages = there is reduced clotting with reduced serotonin

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32
Q

what happens if you take oral beta-blockers with duloxetine?

A

reduced metabolism of beta-blockers = AV block and hypotension, bradycardia (used for high BP)

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33
Q

what are 2 cautions for duloxetine?

A

bleeding risk and angle closure glaucoma

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34
Q

what are 3 atypical antidepressants?

A

trazodone (desyrel), nefazadone (serzone), bupropion (wellbutrin, zyban)

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35
Q

what are the indications for trazodone?

A

major depressive disorder and insomnia

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36
Q

what is the mechanism of action for trazodone?

A

selective serotonin re-uptake inhibitor (SSRI) and adrenergic alpha1 blocker

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37
Q

what are the common side effects for trazodone?

A

headache, dizziness, blurred vision, ocular irritation (sympathomimetic effects)

38
Q

what are the distinguishing side effects for trazodone?

A

suicidal ideation and 5-HT syndrome

39
Q

what is a CVS side effect for trazodone?

A

hemorrhage (platelets depend on serotonin for clotting)

40
Q

what happens if you take cyclosporine, macrolides, and azoles with trazodone?

A

QT prolongation and imparied hepatic metabolism

41
Q

what happens if you take NSAIDs with trazodone?

A

hemorrhage risk is increased

42
Q

what are 4 anti-psychotic/neuroleptics?

A

Quetiapine (seroquel), Halloperidol (haldol), Chlorpromazine (thorazine), Thioridazine (mellaril)

43
Q

what are the indications for quetiapine?

A

schizophrenia and bipolar disorder

44
Q

what is the pharmacology for quetiapine?

A

2nd generation anti-psychotic and bipolar disorder

45
Q

what is the mechanism of action for quetiapine?

A

antagonizes dopamine receptors and 5-HT receptors (ancillary effects may arise from antagonism of histamine and alpha1 receptors)

46
Q

what are the common side effects for quetiapine?

A

headache and anemia

47
Q

what is an ocular side effect for quetiapine?

A

cataracts

48
Q

what is a hypersensitivity connected to quetiapine?

A

stevens-johnson syndrome

49
Q

what happens if you take macrolides, azoles and cyclosporine with quetiapine?

A

prolonged QT segment

50
Q

what happens if you take classic (sedating) anti-histamines with quetiapine?

A

additive CNS depression

51
Q

Ex: if a patient has an allergic conjunctivitis due to sinusitis and is taking quetiapine, what do you prescribe for an oral/topical anti-histamine?

A

needs to be 2nd generation and non-drowsy (non-CNS depressant)

52
Q

what happens to patients with Alzheimer’s disease?

A

there is a significant loss of cholinergic neurons in temporal lobe and entorhinal cortex

53
Q

what are two classes of drugs used to treat Alzheimer’s disease?

A

acetylcholinesterase inhibitors (AChEI) and NMDA-glutamate receptor antagonists

54
Q

what are 5 drugs used to treat Alzheimer’s disease?

A

Donepezil (aricept), Galantamine (razadyne), Rivastigmine (exelon), Tacrine (cognex), Memantine (namenda)

55
Q

which of the Alzheimer’s drugs is the NMDA receptor agonist (neuro-protective)?

A

Memantine (namenda) - may be used to treat glaucoma

56
Q

what is the mechanism of action for donepezil?

A

indirect (central) acting - reversibly binds to and inactivates acetylcholinesterase (AChE) = produces excessive ACh (rest/digest symptoms)

57
Q

what are the common side effects for donepezil?

A

headache, dizziness, arthritis (relaxes vascular tone)

58
Q

what are some serious side effects of donepezil?

A

CNS (seizures, dream disturbances), hemolytic anemia, CV (AV block, bradycardia, syncope)

59
Q

what happens if you take cholinergic agents with donepezil?

A

additive effect (ex: pilocarpine use punctal occlusion)

60
Q

what happens if you take NSAIDs and donepezil?

A

hemorrhagic risk (hemolytic anemia produced by donepezil)

61
Q

what happens if you take anti-cholinergics with donepezil?

A

antagonism occurs

62
Q

what happens if you take macrolides and azoles with donepezil?

A

reduced metabolism of donepezil

63
Q

what happens if you take dexamethasone with donepezil?

A

enhanced metabolism of donepezil (patients may show Alzheimer’s symptoms even if taking medication)

64
Q

what happens if you take Brimonidine (alpha2 agonist) and timolol (beta-blocker) ophthalmics with donepezil?

A

both ophthalmic drugs reduce sympathetic activity + donepezil reduced sympathetic activity = bradycardia and bronchospasm

65
Q

what happens if you take ester anesthetics with donepezil?

A

reduced metabolism of anesthetics (proparacaine and benzocaine are esters)

66
Q

what causes Parkinson’s disease?

A

imbalance between excitatory cholinergic neurons and diminished inhibitory dopaminergic neurons

67
Q

what is the goal of Parkinson’s disease therapy?

A

restoring dopamine in basal ganglia and antagonizing the excitatory effect of cholinergic neurons (restores D/ACh balance)

68
Q

what are 2 anti-parkinson drugs?

A

Carbidopa + Levodopa (sinemet) and Bromocriptine (Parlodel)

69
Q

what is the mechanism of action for sinemet (carbidopa and levodopa)?

A 
carbidopa = inhibits dopa decarboxylase (which degrades levodopa to dopa)
levodopa = dopamine precursor that can cross BBB to enhance DA synthesis in substantia nigra
70
Q

what are the common side effects for sinemet?

A

headache and confusion

71
Q

what are the serious CNS side effects for sinemet?

A

psychosis, suicidal ideation, hallucinations

72
Q

what are the drug interactions for sinemet?

A

there are no ophthalmic drug interactions

73
Q

where do the majority of anxiolytics and hypnotics act?

A

at the GABAa receptor = CNS’s major inhibitory neurotransmitter

74
Q

what are the 3 long lasting benzodiazepines?

A

diazepam (valium), chlordiazepoxide (librium), Flurazepam (dalmane)

75
Q

what are the 2 short acting benzodiazepines?

A

midazolam (versed), triazolam (halcion)

76
Q

what are the indications for alprazolam?

A

anxiety and panic disorder

77
Q

what is the mechanism of action for alprazolam?

A

selectively binds to GABAa-BZD receptors - enhancing GABA effects = inhibitory effect on CNS (ligand gated ion channel)

78
Q

what are the common adverse effects for alprazolam?

A

diplopia, drowsiness, anterograde amnesia, confusion, dizziness, hypotension

79
Q

what are the 2 hypersensitivities for alprazolam?

A

stevens johnson syndrome and angioedema

80
Q

what happens if you take alprazolam with cyclosporine, Azoles, or erythromycins?

A

reduced alprazolam metabolism

81
Q

what happens if you take alprazolam with chlorpheniramine, diphenhydramine or opioids?

A

there is an additive effect

82
Q

what are the contraindications/cautions for alprazolam?

A

unstable myasthenia gravis

83
Q

what are the 3 non-benzodiazepines?

A

zolpidem (ambien), eszopiclone (lunesta) and zaleplon (sonata)

84
Q

what is the indication for zolpidem?

A

insomnia (only short term)

85
Q

what is the pharmacology for zolpidem?

A

non-BZD sedative hypnotic

86
Q

what is the mechanism of action for zolpidem?

A

selective agonist of GABAa-BZD-1 receptors

87
Q

what are the common side effects for zolpidem?

A

headache, sinusitis, and pharyngitis

88
Q

what are the CNS side effects seen with zolpidem?

A

amnesia, suicidal ideation, agression, and hallucinations

89
Q

what happens if you take zolpidem with cyclosporine or azoles?

A

reduced metabolism of zolpidem

90
Q

what happens if you take zolpidem with classic antihistiminics or opioids?

A

there is an additive effect

Systemic Pharmacology (6 decks)

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