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Neuro Exam 3 > Neurological Pharmacology > Flashcards

Neurological Pharmacology Flashcards

1
Q

Barbiturate-Containing Compounds

A

● Butalbital/Aspirin/Caffeine (Fiorinal)
● Butalbital/Acetaminophen/Caffeine
(Fioricet)

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2
Q

Barbiturate-Containing Compounds MOA

A

○ Barbiturates are CNS depressants.
○ Another common example
includes Phenobarbital (for
seizures and sedation).
○ Barbiturates, like Butalbital,
increase the effects of GABA, an
inhibitory neurotransmitter. This
causes an influx of Chloride,
hyperpolarizing the cell.

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3
Q

Barbiturate indications

A

○ Tension headaches (FDA indication) - Not first line
○ Sometimes used off-label for migraines

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4
Q

Barbiturate BBW

A

BBW- Fioricet has FDA BBW for possible hepatotoxicity because it
contains Acetaminophen

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5
Q

Contraindications of Barbiturate

A

○ Porphyria- Accumulation of porphyrins can occur with barbiturates.
○ Fiorinal is contraindicated in PUD, gastritis, uncontrolled hypertension,
G6PD deficiency, and bleeding disorders because it contains ASA.

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6
Q

Barbiturate major adverse effects

A

○ Sedation
○ Respiratory Depression

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7
Q

Because these can be abused and dependence can occur, these are
considered Schedule III Narcotics

A

Barbiturate-Containing Compounds

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8
Q

Triptans (Serotonin Agonists)

A

Sumatriptan (Imitrex), Almotriptan (Axert),
Eletriptan (Relpax), Rizatriptan (Maxalt),
Zolmitriptan (Zomig), and
Sumatriptan/Naproxen (Treximet)

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9
Q

Triptans MOA

A

○ Agonistic to Serotonin 5-HT receptors,
which is believed to decrease the release
of substance P and other pain NTs, as
well as causing cerebral vasoconstriction,
working against migraine-type HAs

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10
Q

Triptans indications

A

○ Acute Migraine Headache
○ Sumatriptan (SC) is also
FDA-indicated for Acute
Cluster Headaches

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11
Q

Triptans contraindications

A

○ Uncontrolled hypertension
○ Cerebrovascular Disease
○ Coronary Artery Disease
○ Peripheral Arterial Disease

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12
Q

Triptans adverse effects

A

○ Coronary vasospasm
○ Myocardial ischemia
○ Myocardial infarction
○ Severe hypertension
○ Acute stroke
○ Cerebral hemorrhage
○ Intestinal ischemia
○ Ventricular tachycardia

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13
Q

Ditan (5-HT 1F Agonist)

A

Lasmiditan (Reyvow)

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14
Q

Ditan (5-HT 1F Agonist) MOA

A

○ Similar to the Triptans, Lasmiditan is
believed to work by binding to and
agonizing 5-HT receptors, but this one is
likely specific to the 1F subtype
○ It is thought that this medication may
inhibit peripheral trigeminal nerve firing,
helping to abort migraines

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15
Q

Ditan (5-HT 1F Agonist) indications

A

Acute migraine headache (abortive only!)

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16
Q

_____ is a controlled substance (schedule V)

A

Lasmiditan

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17
Q

Ergotamines

A

● Dihydroergotamine (Migranal)
● Ergotamine/Caffeine (Cafergot)

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18
Q

Ergotamines MOA

A

○ Like Triptans, 5-HT receptor agonists
that are believed to decrease Substance P release and cause vasoconstriction.
○ Additionally, Ergots are partial agonists of Alpha-1 adrenergic receptors, causing vasoconstriction

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19
Q

Ergotamines contraindications

A

○ Like the Triptans, contraindicated in Peripheral Arterial Disease,
Coronary Vasospasm, Coronary Artery Disease, Hypertension.
○ Severe renal impairment
○ Severe hepatic impairment
○ Pregnancy
○ Breastfeeding
○ Sepsis

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20
Q

Ergotamines BBW

A

○ Risk of severe peripheral
ischemia (vasoconstriction)

21
Q

Ergotamines adverse effects

A

○ Valvular Heart Disease
○ Pulmonary Fibrosis

22
Q

Ergotamines and pregnancy

A

○ Contraindicated during pregnancy!
Animal studies have revealed moderate
risk of teratogenicity.
○ Unsafe in lactation.

23
Q

Anti-CGRP Monoclonal Antibodies

A

● Erenumab (Aimovig)
● Fremanezumab (Ajovy)
● Galcanezumab (Emgality)

24
Q

Anti-CGRP Monoclonal Antibodies MOA

A

○ Binds to and blocks calcitonin gene-related peptide (CGRP) receptor, which is thought to be
related to migraine pathophysiology somehow
○ These are subcutaneous injections
that the patient does monthly.
■ Half-life: 27-31 days

25
Q

Anti-CGRP Monoclonal Antibodies indications

A

○ Migraine headache prophylaxis (prevention only!)
○ Emgality is also approved for Episodic Cluster Headaches

26
Q

Anti-CGRP Monoclonal Antibodies adverse effects

A

○ Anaphylaxis has occurred with
Aimovig
○ No serious reactions reported
with the others

27
Q

Dopamine Agonists

A

● Bromocriptine (Parlodel)
● Ropinirole (Requip)
● Pramipexole (Mirapex)

28
Q

Dopamine Agonists MOA

A

○ When dopaminergic neurons are lost
and the D1 and D2 pathways are
unbalanced, movements are not
regulated (tremor, bradykinesia, etc).
Medscape
○ Dopamine Agonists work by activating
D1 and D2 receptors in the striatum,
balancing the pathways as if dopamine
levels from the substantia nigra were
normal, thereby normalizing motor
function (treats tremor, bradykinesia)

29
Q

Dopamine Agonists indications

A

○ All three are indicated in Parkinson’s Disease.
○ Ropinirole and Pramipexole are indicated for Restless Leg Syndrome.
○ Bromocriptine is indicated for Acromegaly and Hyperprolactinemia (as
with Prolactinomas), as it also works to inhibit Prolactin and Growth
Hormone release

30
Q

Dopamine Agonists adverse effects

A

○ Sudden onset sleep - Avoid activities like driving while taking.
○ Others include seizures, stroke, arrhythmias, severe hypotension,
bradycardia, syncope, dyskinesia, Malignant Melanoma.

31
Q

Dopamine Agonists side effects

A

○ Lots and lots, unfortunately. The most common side effects include:
■ Nausea/vomiting
■ Peripheral edema
■ Hypotension
■ Hallucinations or vivid dreams

32
Q

Because of the risk of Melanoma, a regular dermatologic
examination is recommended with _____

A

Dopamine Agonists

33
Q

Dopaminergic Agents

A

Levodopa/Carbidopa (Sinemet, Parcopa), Selegiline (Elderpryl), Rasagiline (Azilect),
Entacapone (Comtan), and Amantadine (Symmetrel).

34
Q

Dopaminergic Agents MOA

A

○ Levodopa (L-Dopa): A precursor of Dopamine that is able to cross BBB. L-Dopa enhances dopamine synthesis in remaining dopaminergic neurons in SN.
○ Carbidopa: Inhibits a decarboxylase enzyme in the peripheral tissues that converts L-Dopa into Dopamine (Dopamine cannot cross BBB).
○ Entacapone: Inhibits peripheral Catechol-O-Methyltransferase (COMT), which normally inhibits L-Dopa in GI tract, so it extends effects of L-Dopa.
■ Adjunct to L-Dopa; no effect when given alone
○ Selegiline and Rasagiline: Irreversible inhibitors of MAO-B in the brain, which
normally metabolizes Dopamine in the brain (increases Dopamine levels)
○ Amantadine: An antiviral drug that was found to increase the release of Dopamine in the brain. (Also blocks cholinergic and NMDA receptors)

35
Q

Dopaminergic Agents Indications

A

○ Levodopa/Carbidopa is considered the first-line drug for Parkinson Dz.
■ There are immediate and extended release forms
○ Entacapone: Adjunct to prevent “wearing off” of Levodopa.
○ Selegiline, Rasagiline, and Amantadine: Theses are all considered
adjunct treatments in Parkinson Disease. Are sometimes used
independently, but more often as adjuncts to Levodopa

36
Q

Anticholinergic Agents

A

Benztropine (Cogentin) and Trihexyphenidyl (Artane)

37
Q

Anticholinergic Agents MOA

A

○ These antagonize the parasympathetic nervous system by binding to
and blocking the Muscarinic Acetylcholine receptors.
■ There is a theory that acetylcholine activity increases as
dopaminergic neurons die in Parkinson Disease, theoretically being
involved in some of the symptoms, including tremor.
■ These anticholinergic drugs theoretically block the effects of
acetylcholine in hopes of treating the symptoms of Parkinson Dz.
● In reality, not extremely effective
Medscape

38
Q

Anticholinergic Agents indications

A

○ Parkinson Disease
○ Extrapyramidal Symptoms (drug-induced movement disorders, such as
dystonia, bradykinesia, and tardive dyskinesia)

39
Q

Anticholinergic Agents adverse reactions

A

○ Anticholinergic
psychosis
○ Tachycardia
○ Severe anhidrosis
○ Heat stroke
○ Acute Angle-Closure
Glaucoma
○ Tardive Dyskinesia
(ironically)

40
Q

Anticholinergic Agents side effects

A

○ Constipation
○ Urinary retention
○ Sedation
○ Nausea/Vomiting
○ Dizziness
○ Headache
○ Tinnitus
○ Blurred vision
○ Flushing
○ Dry mouth

41
Q

Cholinesterase Inhibitors

A

● Donepezil (Aricept), Galantamine (Razadyne),
Rivastigmine (Exelon), Neostigmine
(Bloxiverz), and Pyridostigmine (Mestinon)

42
Q

Cholinesterase Inhibitors MOA

A

○ These drugs inhibit the enzyme
Acetylcholinesterase that normally
breaks Acetylcholine into Acetic Acid
and Choline within the synaptic cleft.
○ By this mechanism, these drugs
enhance acetylcholine transmission

43
Q

Cholinesterase Inhibitors indications

A

○ Donepezil, galantamine, and rivastigmine have stronger effects within the CNS, while neostigmine and pyridostigmine are more peripheral.
○ Donepezil, galantamine, and rivastigmine: Alzheimer’s Dementia
○ Neostigmine and pyridostigmine: Myasthenia Gravis
○ Neostigmine: Reversal of some neuromuscular blocking agents, as well
as urinary retention

44
Q

Cholinesterase Inhibitors contraindications

A

○ Pyridostigmine is contraindicated in GI and GU obstruction.
○ Otherwise, for all, caution is advised in renal and hepatic impairment, as
well as cardiac conduction defects and bradycardia

45
Q

Cholinesterase Inhibitors adverse effects

A

○ AV block
○ Bradycardia
○ Seizures
○ Steven-Johnson Syndrome
○ Urinary obstruction
○ GI bleeding
○ Hemolytic anemia

46
Q

NMDA Receptor Antagonist

A

Memantine (Namenda)

47
Q

NMDA Receptor Antagonist MOA

A

○ Alzheimer’s pathophysiology includes
reduced production of Acetylcholine,
as well as sustained and excessive
stimulation of N-methyl-D-aspartate
(NMDA) receptors, resulting in
neuronal dysfunction and cell death.
Medscape
○ NMDA receptors seem to play a strong
role in learning and memory.
○ Namenda blocks NMDA receptors

48
Q

NMDA Receptor Antagonist indications

A

Alzheimer’s Disease

Neuro Exam 3 (7 decks)

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