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Neuro Module > Pharmacology > Flashcards

Pharmacology Flashcards

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1
Q

levetiracetam

Keppra

A

↓ glutamate transmission

  • binds SV2A (↓ presynaptic glutamine release)
  • excreted in urine, negligible drug interactions
  • *generalized tonic clonic seizures
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2
Q

lamotrigine

Lamictal

A 
↓ Glutamate release
block Na+ channel
↓ Ca++ channel: HVA
- not recommended for <16yrs, Stevens Johnson syndrome
**variety of seizure types, bipolar
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3
Q

felbamate

Felbatol

A

↓ glutamate transmission: inhibit NMDA post synaptic receptor
↑ GABA transmission: GABA-A receptor
-only in refractory cases
-liver f/x testing required
- liver failure, anaplastic anemia
**partial and generalized tonic-clonic seizures

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4
Q

topiramate

Topamax

A

↓ Glutamate transmission: AMPA/KA receptor antagonist
block Na+ channel
↓ Ca++ channel transmission
↑GABA transmission: GABA-A receptor
↑ K+ channel
– may cause myopia, glaucoma, metabolic acidosis
**variety of seizure types, migraine prophylaxis

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5
Q

phenobarbital

A

↑ GABA transmission: GABA-A receptor
↓ Glutamate transmission: AMPA receptor at HIGH CONCENTRATION
- used in infants, not others due to sedation
**partial and generalized tonic-clonic seizures, sedation

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6
Q

valproate

A

block Na+ channel
↓ Ca++ channel: t-type
↑ GABA transmission: blocks GABA transaminase (block degradation)/stimulates GAD (produces more GABA)
- liver f/x testing required, teratogenic
**variety of seizures, bipolar, migraine prophylaxis

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7
Q

vigabatrin

A

↑ GABA transmission: irreversible inhibitor of GABA transaminase (degradation of GABA)

  • contraindicated: previous mental illness (psychosis)
  • long term progressive, permanent vision loss
  • *refractory complex partial seizures/infantile seizures
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8
Q

tiagabine

Gabitril

A

↑ GABA transmission: inhibit GABA reuptake at GAT-1

  • hepatic metabolism, binds plasma proteins
  • causes seizures/status epilepticus in non-seizure pts
  • *partial and generalized tonic-clonic seizures
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9
Q

carbamazepine

Tegretol

A

block Na+ channel

  • water retention/hyponatremia
  • SJS (esp. Asians), TENS
  • screen HLA-B1502
  • monitor: renal f/x, serum Na+, drug levels
  • *partial and generalized tonic-clonic seizures, bipolar, CNV neuralgia
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10
Q

oxcarbazepine

Trileptal

A 
block Na+ channel
↑ K+ channel
↓ Ca++ channel: HVA
- related to carbamazepine (same end product), less toxic??
- water retention/hyponatremia
- SJS, TENS
monitor: Na+, thyroid levels
**partial and generalized tonic-clonic seizures
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11
Q

phenytoin

Dilantin

A

inhibits Na+ channel

  • hepatic metabolism (unique to each person)
  • monitor drug levels, may interfere w/ thyroid testing
  • nystagmus, gingival hyperplasia, teratogenic
  • *partial and generalized tonic-clonic seizures
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12
Q

zonisamide

Zonegran

A 
inhibits Na+ channel
↓ Ca++ channel: t-type
- inhibits carbonic anhydrase weakly
- drowsiness, kidney stones, metabolic acidosis, teratogenic
**variety of seizures
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13
Q

ethosuximide

Zarontin

A

↓ Ca++ channel: t-type

  • gastric distress, behavioral changes, Parkinson-like sx, photophobia
  • *Absence seizures
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14
Q

gabapentin

Neurontin

A

↓ Ca++ channel: alpha-2-delta subunit

  • excreted in urine, negligible drug interactions
  • can cause behavioral/thought disorders in children 3-12yrs
  • related to Lyrica (pregabalin)
  • *partial and generalized tonic-clonic seizures, neuralgia
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15
Q

Stevens-Johnson Syndrome

A 
SJS- epidermis separates from dermis
possible adverse reaction from:
- lamotrigine
- carbamazepine
- oxcarbazepine
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16
Q

Toxic epidermal necrolysis

A

TENS- more severe form of SJS
possible adverse reaction from:
- carbamazepine
- oxcarbazepine

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17
Q

Drug treatments for partial and generalized tonic-clonic seizures

A
  • levetiracetam (Glu)
  • phenobarbital (GABA, Glu)
  • felbamate (Glu, GABA)- refractory onlyL-
  • tiagabine (GABA)
  • carbamazepine (Na)
  • oxcarbazepine (Na, K, Ca)
  • phenytoin (Na)
  • gabapentin (Ca)
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18
Q

Drugs for a Variety of Seizure types

A
  • lamotrigine (Glu, Na, Ca)
  • topiramate (Glu, GABA, Na, K)
  • valproate (GABA, Na, Ca)
  • zonisamide (Na, Ca)
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19
Q

Drugs for Absence seizures

A

-ethosuximide (Ca)

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20
Q

L-dopa

A

Replace dopamine: precursor to DA

  • *Parkinsons disease
  • early adverse: nausea, orthostatic hypotension, arrhyhmias, psychosis
  • late adverse: dyskinesia, on-off phenomenon, behavioral effects
  • *hypertensive crisis if given with MAOIs
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21
Q

carbidopa

A

inhibitor to decarboxylase in PNS (cannot cross BBB),
use with L-dopa to ↓ peripheral side effects
**Parkinsons disease

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22
Q

rasagiline (selegiline)

A

Replace dopamine:
MAO-B inhibitor: ↓ DA breakdown in CNS only
**Parkinsons disease

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23
Q

entacapone (tolcapone)

A

Replace dopamine: COMT inhibitor- ↓ L-dopa metabolism in PNS
prolongs L-dopa effectiveness
tolcapone only: liver damage
**Parkinson disease

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24
Q

bromocriptine

A

Replace dopamine: DA agonist (ergot)
use with L-dopa/carbidopa to ↓ on/off phenomenon
-adverse effects: swollen hands/feet, pulmonary infiltrate
**Parkinson disease

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25
Ropinirole
Replace dopamine: DA agonist (D2 receptor) - CYP1A2 metabolism: warfarin, caffeine reduce clearance - nausea, hypotension, dyskinesia, hallucinations, delusions * *Parkinson disease
26
Pramipexole
Replace Dopamine: DA agonist (D3 receptor) - nausea, hypotension, dyskinesia, hallucinations, delusions * *Parkinson disease
27
Rotigotine
Replace dopamine: transdermal DA agonist - nausea, hypotension, dyskinesia, hallucinations, delusions * *Parkinson disease
28
Domperidone
DA antagonist in PNS (doesn't cross BBB) - reduces adverse effects of DA agonists - Ropinirole, Pamipexole, Rotigotine * *Parkinson disease
29
Benzotropine
Antimuscarinic in striatum: Block ACh response ↓ tremor - dry mouth, blurred vision, urinary retention (anticholinergic: exaggerated sympathetic response) **Parkinson disease, **Schizophrenia: Parkinsonism/dystonias/akathasias caused by typical antipsychotics
30
Trihexylphenidyl
Antimuscarinic in striatum: Block ACh response ↓ tremor - dry mouth, blurred vision, urinary retention (anticholinergic: exaggerated sympathetic response) **Parkinson disease, **Schizophrenia: Parkinsonism caused by typical antipsychotics
31
Amantadine
Block ACh response: anti-muscarinic, ↓ DA transmission - works less well than L-dopa - livedo reticularis: red-blue skin discoloration
32
Sinemet
L-dopa + carbidopa | **Parkinson disease
33
Drugs to Replace DA
- L-dopa - Sinemet - rasagiline - selegiline - entacapone - tolcapone - bromocriptine - ropinirole - pramipexole - rotigotine * *Parkinson disease
34
Antipsychotics that can be used to treat side effects of L-dopa w/o worsening Parkinson symptoms
Atypical antipsychotics: - risperidone - olanzapine - quetiapine
35
Drug class used to treat Alzheimers
``` acetylcholinesterase inhibitors -Donepezil -Rivastigmine -Galantamine NMDA receptor antagonist -Memantine ```
36
Donepezil
CNS selective ACh-esterase inhibitor - nausea, vomiting, diarrhea, abdominal pain, anorexia * *Alzheimer disease
37
Rivastigmine
CNS selective ACh-esterase inhibitor - nausea, vomiting, diarrhea, abdominal pain, anorexia * *Alzheimer disease
38
Galantamine
CNS selective ACh-esterase inhibitor - nausea, vomiting, diarrhea, abdominal pain, anorexia * *Alzheimer disease
39
Memantine
NMDA receptor antagonist | ** Alzheimer disease
40
Mechanism of Parkinson Disease
Substantia Nigra, pars compacta: ↓ DA-ergic neurons ↓ inhibition of indirect pathway: more movement ↓ stimulation of direct pathway: difficulty initiating movement
41
Symptoms of Schizophrenia
``` Positive: - thought disorders (illogical) - hallucinations/delusions Negative: - flat affect - withdrawal from others ```
42
What is neuroleptic syndrome?
disinterest in the environment with limited range of affect - adverse effect of all antipsychotic medications * *Schizophrenia
43
What is the dopamine hypothesis?
Symptoms of schizophrenia are alleviated with dopamine antagonists, worsen with dopamine agonists (D2) Particularly in mesolimbic areas: Nucleus accumbens, olfactory bult, prefrontal cortex, amygdala, cortical region
44
Side effects of antipsychotics
1) Non-neurological/anticholinergic - orthostatic hypotension (alpha-1 block) - ↓ sex drive (alpha block) - ↑ prolactin (↓ normal DA inhibition) - weight gain (esp. atypicals) - sedation - seizures - anticholinergic - phototoxicity - blood dyscrasias/leukopenia 2) Neurological/extra-pyramidal - Parkinsonism syndrome (typicals) --> benztopine/trihexphenidyl - dystonias --> benztropine/ diphenhydramine - akathasias: restlessness --> benztropine - tardive dyskinesia
45
Mechanism of action of typical/atypical antipsychotics
Typical: block Dopamine receptors (D2) Atypical: block D2 and also 5HT-2A Serotonin receptors
46
chlorpromazine
Typical antipsychotic: - antagonist to D2, alpha adrenergic, and cholinergic receptors - relieve positive sx - sedation > haloperidol - orthostatic hypotension * *Schizophrenia, manic bipolar
47
haloperidol
``` Typcial antipsychotic -antagonist at D2 receptor only -relieves positive sx Neurological sx, prolactinemia > chlorpromazine **Schizophrenia ```
48
Risperidone
``` Atypical antipsychotic blocks D2, 5HT-2A receptors relieves positive and negative sx ↑ prolactinemia **Schizophrenia, manic bipolar ```
49
Clozapine
Atypical antipsychotic blocks D4>D2, inverse agonist to 5HT-2A, 5HT-2C best at relieving sx, ↑ cognitive function no tardive dyskinesia agranulocytosis (↓WBCs) **Schizophrenia
50
Olanzapine
Atypical antipsychotic blocks D2=D4, 5HT-2A relieves positive and negative sx, ↑ cognitive function ↑ prolactinemia **Schizophrenia, manic bipolar, depressive bipolar (w/fluoxetine)
51
Quetiapine
Atypical antipsychotic inverse agonist 5HT-2A > block D2, block H1 (sedation), alpha-1 (hypotension) relieve positive and negative sx ↑ prolactinemia **Schizophrenia, manic bipolar, depressive bipolar
52
Ziprasidone
``` Atypical antipsychotic inverse agonist 5HT-2A > block D2, block H1 (sedation), alpha-1 (hypotension) relieve positive and negative sx ↑ prolactinemia ↓ weight gain **Schizophrenia, manic bipolar ```
53
Aripiprazole
``` Dopamine stabilizer partial agonist D2, 5HT-1A; antagonist 5HT-2A as good as atypical antipsychotics ↓ side effects, wt gain than atypicals **Schizophrenia, manic bipolar ```
54
Diphenhydramine (Benadryl)
Antihistamine w/ anticholinergic properties - treat dystonias due to typical antipsycotics * *Schizophrenia
55
Transmitters and foci of action for addiction
1) NE: locus coeruleus --> all over cortex 2) DA: substantia nigra --> striatum VTA --> nucleus accumbens 3) 5-HT: Raphe nuclei --> all over brain
56
Amphetamine
↑ levels of NE, DA, 5HT in synapse: - enters presynaptic neuron through NET, SERT, or DAT - ↑ release of NE, DA, & 5HT - inhibits MAO - risk of heart attack,stroke, sudden death; withdrawal sx * *ADHD, Narcolepsy
57
Where does NE act in the brain?
Locus coeruleus --> all levels of brain - enhances excitatory inputs - attention/arousal
58
Where does 5HT act in the brain?
``` Raphe Nuclei (brainstem) --> many parts of brain - mood, sleep, appetite, temperature control, pain perception, bp regulation, vomiting ```
59
Where does dopamine work in the brain?
Substantia nigra --> striatum -movement VTA --> limbic structures (nucleus accumbens) -emotion
60
Methamphetamine
↑ NE, DA, 5HT in synapse - works same as amphetamine (monoamine release + MAOI) - high abuse potenial * *ADHD, obesity
61
Atomoxitine
``` ↑ NE in synapse: -blocks reuptake of NE (NET) -↓ sympathetic outflow adverse effects: orthostatic tachycardia, drowsiness, sexual dysfunction, SI **ADHD ** ```
62
Methylphenidate | Ritalin
↑ NE, DA, 5HT in synapse: Block reuptake of NE (NET), DA (DAT), 5HT (SERT) -potential for abuse **ADHD, narcolepsy
63
Modafinil | Provigil
``` ↑ NE, DA, 5HT, glutamate and ↓ GABA Blocks NET, and DAT, otherwise unknown mechanism -improve alertness -adverse effects: ↑BP/HR mildly **Narcolepsy ```
64
How does addiction work?
DA stimulates D2 receptors in Nucleus Accumbens -hyperpolarize GABAergic neurons: open K+ channels/ close Ca++ channels -inhibits adenylyl cyclase: ↓cAMP levels PLEASURE SENSATION **cocaine, opiates, benzos, nicotine, alcohol, stimulants
65
How does DA affect Nucleus Accumbens
DA --> inhibit GABAergic neurons (REWARDING) meanwhile PFC (planning, motivation)--> stimulate GABAergic neurons Amygdala (+/- perceptions)--> (DISAGREEABLE) Hippocampus (memories)-->
66
What is the mechanism for withdrawal symptoms from amphetamine?
1) Exogenous DA for extended time --> less endogenous DA produced - when too little DA: Nucleus accumbens is stimulated --> : ( 2) Extended inhibition of adenylyl cyclase --> more produced - when too much cAMP: activates GABAergic neurons * *anhedonia, depression, hunger, exhaustion
67
Sumatriptan
Agonist to 5HT-1B/1D | **Migraines
68
Propanolol
beta-adrenergic blocker nonselective for beta-1 & beta-2 **Migraine prophylaxis

Neuro Module (5 decks)

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