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Neuro Module > Pharmacology > Flashcards

Pharmacology Flashcards

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
Q

Ropinirole

A

Replace dopamine: DA agonist (D2 receptor)

  • CYP1A2 metabolism: warfarin, caffeine reduce clearance
  • nausea, hypotension, dyskinesia, hallucinations, delusions
  • *Parkinson disease
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26
Q

Pramipexole

A

Replace Dopamine: DA agonist (D3 receptor)

  • nausea, hypotension, dyskinesia, hallucinations, delusions
  • *Parkinson disease
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27
Q

Rotigotine

A

Replace dopamine: transdermal DA agonist

  • nausea, hypotension, dyskinesia, hallucinations, delusions
  • *Parkinson disease
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28
Q

Domperidone

A

DA antagonist in PNS (doesn’t cross BBB)

  • reduces adverse effects of DA agonists
  • Ropinirole, Pamipexole, Rotigotine
  • *Parkinson disease
29
Q

Benzotropine

A

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
Q

Trihexylphenidyl

A

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
Q

Amantadine

A

Block ACh response: anti-muscarinic, ↓ DA transmission

  • works less well than L-dopa
  • livedo reticularis: red-blue skin discoloration
32
Q

Sinemet

A

L-dopa + carbidopa

**Parkinson disease

33
Q

Drugs to Replace DA

A
  • L-dopa
  • Sinemet
  • rasagiline
  • selegiline
  • entacapone
  • tolcapone
  • bromocriptine
  • ropinirole
  • pramipexole
  • rotigotine
  • *Parkinson disease
34
Q

Antipsychotics that can be used to treat side effects of L-dopa w/o worsening Parkinson symptoms

A

Atypical antipsychotics:

  • risperidone
  • olanzapine
  • quetiapine
35
Q

Drug class used to treat Alzheimers

A 
acetylcholinesterase inhibitors
-Donepezil
-Rivastigmine
-Galantamine
NMDA receptor antagonist
-Memantine
36
Q

Donepezil

A

CNS selective ACh-esterase inhibitor

  • nausea, vomiting, diarrhea, abdominal pain, anorexia
  • *Alzheimer disease
37
Q

Rivastigmine

A

CNS selective ACh-esterase inhibitor

  • nausea, vomiting, diarrhea, abdominal pain, anorexia
  • *Alzheimer disease
38
Q

Galantamine

A

CNS selective ACh-esterase inhibitor

  • nausea, vomiting, diarrhea, abdominal pain, anorexia
  • *Alzheimer disease
39
Q

Memantine

A

NMDA receptor antagonist

** Alzheimer disease

40
Q

Mechanism of Parkinson Disease

A

Substantia Nigra, pars compacta: ↓ DA-ergic neurons
↓ inhibition of indirect pathway: more movement
↓ stimulation of direct pathway: difficulty initiating movement

41
Q

Symptoms of Schizophrenia

A 
Positive:
- thought disorders (illogical)
- hallucinations/delusions
Negative:
- flat affect
- withdrawal from others
42
Q

What is neuroleptic syndrome?

A

disinterest in the environment with limited range of affect

  • adverse effect of all antipsychotic medications
  • *Schizophrenia
43
Q

What is the dopamine hypothesis?

A

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
Q

Side effects of antipsychotics

A

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
Q

Mechanism of action of typical/atypical antipsychotics

A

Typical: block Dopamine receptors (D2)
Atypical: block D2 and also 5HT-2A Serotonin receptors

46
Q

chlorpromazine

A

Typical antipsychotic:

  • antagonist to D2, alpha adrenergic, and cholinergic receptors
  • relieve positive sx
  • sedation > haloperidol
  • orthostatic hypotension
  • *Schizophrenia, manic bipolar
47
Q

haloperidol

A 
Typcial antipsychotic
-antagonist at D2 receptor only
-relieves positive sx
Neurological sx, prolactinemia > chlorpromazine
**Schizophrenia
48
Q

Risperidone

A 
Atypical antipsychotic
blocks D2, 5HT-2A receptors
relieves positive and negative sx
↑ prolactinemia
**Schizophrenia, manic bipolar
49
Q

Clozapine

A

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
Q

Olanzapine

A

Atypical antipsychotic
blocks D2=D4, 5HT-2A
relieves positive and negative sx, ↑ cognitive function
↑ prolactinemia
**Schizophrenia, manic bipolar, depressive bipolar (w/fluoxetine)

51
Q

Quetiapine

A

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
Q

Ziprasidone

A 
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
Q

Aripiprazole

A 
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
Q

Diphenhydramine (Benadryl)

A

Antihistamine w/ anticholinergic properties

  • treat dystonias due to typical antipsycotics
  • *Schizophrenia
55
Q

Transmitters and foci of action for addiction

A

1) NE: locus coeruleus –> all over cortex
2) DA: substantia nigra –> striatum
VTA –> nucleus accumbens
3) 5-HT: Raphe nuclei –> all over brain

56
Q

Amphetamine

A

↑ 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
Q

Where does NE act in the brain?

A

Locus coeruleus –> all levels of brain

  • enhances excitatory inputs
  • attention/arousal
58
Q

Where does 5HT act in the brain?

A 
Raphe Nuclei (brainstem) --> many parts of brain
- mood, sleep, appetite, temperature control, pain perception, bp regulation, vomiting
59
Q

Where does dopamine work in the brain?

A

Substantia nigra –> striatum
-movement
VTA –> limbic structures (nucleus accumbens)
-emotion

60
Q

Methamphetamine

A

↑ NE, DA, 5HT in synapse

  • works same as amphetamine (monoamine release + MAOI)
  • high abuse potenial
  • *ADHD, obesity
61
Q

Atomoxitine

A 
↑ NE in synapse:
-blocks reuptake of NE (NET)
-↓ sympathetic outflow
adverse effects: orthostatic tachycardia, drowsiness, sexual dysfunction, SI
**ADHD
**
62
Q

Methylphenidate

Ritalin

A

↑ NE, DA, 5HT in synapse:
Block reuptake of NE (NET), DA (DAT), 5HT (SERT)
-potential for abuse
**ADHD, narcolepsy

63
Q

Modafinil

Provigil

A 
↑ NE, DA, 5HT, glutamate and ↓ GABA
Blocks NET, and DAT, otherwise unknown mechanism
-improve alertness
-adverse effects: ↑BP/HR mildly
**Narcolepsy
64
Q

How does addiction work?

A

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
Q

How does DA affect Nucleus Accumbens

A

DA –> inhibit GABAergic neurons (REWARDING)
meanwhile
PFC (planning, motivation)–> stimulate GABAergic neurons
Amygdala (+/- perceptions)–> (DISAGREEABLE)
Hippocampus (memories)–>

66
Q

What is the mechanism for withdrawal symptoms from amphetamine?

A

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
Q

Sumatriptan

A

Agonist to 5HT-1B/1D

**Migraines

68
Q

Propanolol

A

beta-adrenergic blocker
nonselective for beta-1 & beta-2
**Migraine prophylaxis

Neuro Module (5 decks)

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