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Neuro Drugs Flashcards

1
Q

Drugs used to treat epilepsie (Anti-epileptic drugs/ AED)

A
  1. Reduce pre-synaptic excitability
    a. Voltage-gated Na+ channel antagonist (carbamazepine, lamotrigrine)
    b. Voltage-gated K+ channel agonist (retigabine)
  2. Stops neurotransmitter release
    a. SV2A vesicle antagonist (levetiracetam)
    b. Voltage-gated Ca2+ channel antagonist (pregablin and gabapentin)
  3. GABA-ergic system agonists
    a. GABA metabolism inhibitor (valproate, vigabatrin)
    b. GABA transporter antagonist (tiagabine)
  4. Reduces post-synaptic excitability
    a. GABA receptor agonist (benzodiazepines)
    b. AMPA and NMDA receptor antagonist
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2
Q

Carbamazepine Mechansm of action

A
  • voltage gated Na+ channel blocker on pre-synaptic membrane
  • Na+ influx increases excitability and drives action potentials
  • Drug bloks the Na+ influx, reduces neuronal excitability and decreased the action potential
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3
Q

Carbamazepine

A

Pre-synantic Na+ channel blocker

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4
Q

Carbamazepine indications

A

epilepsy, trigeminal neuralgia, neuropathic pain

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5
Q

Side effects of carbamazepine

A 
Dizziness
Dry mouth
Ataxia
Fatigue
Headache
Diplopia
Blurred vision
Hyponatraemia
Stevens-Johnson’s syndrome (rarely
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6
Q

Important PK/PD of carbamazepine

A

Response to the drug can be variable
Enzyme inducer of cytochrome P450; induces metabolism of itself
Interactions with other anti-convulsants
The transporter that can confer drug resistance is RALBP1
Grapefruit can significantly increase serum levels of this drug
HLA-B*1502 allele raises the risk for SJS; avoid in these patients

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7
Q

Patient information of carbamazepine

A

Avoid alcohol

Avoid grapefruit juice

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8
Q

Retigabine

A

Pre-synaptic K+ channel agonist

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9
Q

Mechanism of action of retigabine

A
  • voltage gated K+ channel agonist on pre-synaptic membrane
  • K+ efflux reduces neuronal excitability
  • Drug increases the channel activity reducing the action potential
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10
Q

Phenytoin

A

Pre-synaptic sodium channel blocker

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11
Q

Phenytoin mechanism of action

A
  • Acts as a voltage-gated Na+ channel blocker on the pre-synaptic neuronal membrane
  • Limits action potential transmission
  • Hence limiting spread of seizure activity
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12
Q

Indications for phenytoin

A

epilepsy (including status epilepticus

trigeminal neuralgia

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13
Q

Side effects of phenytoin

A 
MORE THAN CARBAMAZEPINE 
Insomnia
Headache
Rash
Constipation
Vomiting
Gingival hyperplasia
Liver damage

Stevens-Johnson Syndrome (rare)
Leucopenia (rare)
Thrombocytopenia (rare)

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14
Q

Important PK/PD of phenytoin

A

Enzyme inducer of cytochrome P450
Can cause interactions with other anti-epileptic drugs
Narrow therapeutic index
Relationship between dose and plasma concentration is non-linear

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15
Q

Patient information for phenytoin

A

Avoid alcohol
Do not take calcium, aluminum, magnesium or iron supplements within 2 hours of ingestion
Take with food to reduce irritation

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16
Q

Levetiracetam

A

Reduces neurotransmitter release by blocking SVA2

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17
Q

Levetiracetam mechanism of action

A
  • SV2A is a synaptic vesicle protein required for neurotransmitter release
  • Levetiracetam blocks this and reduced neurotransmitter release
  • Induces an anti-epileptic effect
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18
Q

Levetiracetam indication

A

epilepsy

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19
Q

Side effects of levetiracetam

A 
Headache
Fatigue
Anxiety
Irritability
Drowsiness
Constipation
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20
Q

Important PK/PD of levetiracetam

A
  • Rapidly and almost completely absorbed after oral administration (99%)
  • Food does not affect bioavailability
  • Cytochrome P450 is not involved in its metabolism
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21
Q

Patient information of levetiracetam

A
  • It might affect your ability to drive or operate machinery

- Not recommended during pregnancy and breastfeeding

22
Q

Pregablin and gabapentin

A

Blocks voltage gated Ca2+ channels to decrease neurotransmitter release

23
Q

Mechanism of action of pre-gablin

A
  • ca2+ influx drivers neurotransmitter release

- Channel inhibited by pregablin and gabapentin

24
Q

Tiagabine

A

Gabaergic system - GABA transporter

25
Tiagabine mechanism of action
- removes GABA from the synapse | - inhibited by tiagabine (to elevate GABA levels)
26
Valproate
GABAergic system - GABA metabolism
27
Valproate mechanism of action -
- degrades GABA transaminases | - inhibited by valproate (to elevate GABA levels)
28
Perampanel, felbamate and topiramte mechanism of action
Reduce post-synaptic effects - glutamate receptors are not selectively targeted by an approed AEDs - permapanel has main aactivity blocking AMPA receptors - Felbamate has weak affinity for NMDA receptors - Topirmate binds both AMPA and kainate receptors
29
Benzodiazepines mechanism of action
Reduces neuronal excitability - GABAa receptor activity increased - Increase the frequency of channel openin which leads to increase in chloride ion conduction and inhibitor of the action potential
30
Drugs for localised onset
lamotrigine, carbamazepine
31
Drugs for generalised onset
Valproate, levetiracetam, lamotrigine
32
Drugs used to treat parkinsons
Drugs that increase dopaminergic activity a. dopamine precursors b. dopamine agonists c. drugs that stimulate dopamine release d. MAO-B inhibitors Drugs that inhibit strialtal cholinergic activity a. anticholingeric agents
33
Example of dopamine precursor
- Levodopa
34
Mechanism of action of L-dopa
- Immedaite precursor of dopamine - Able to cross the blood-brain barrier to replenish dopamine content of the corpus striatum - L-dopa is decarboxylated to dopamine to dopamine in the brain by Dopa decarboxylase - beneficial effects on the actions of D2 receptors
35
Indication of levodopa
parkinsons disease
36
Side effects of levodopa
``` dyskinesia compulsive disorders hallucinations nausea GI upset ```
37
Important pharmacokinetics/ pharmacodynamics for l-dopa
- Converted to dopamine in peripheries (which can cause the motor side effects) - Given with a dopamine decarboxylase inhibitor or COMT inhibitor to reduce these effects - Short half life – 50 to 90 mins - Rapidly absorbed from the proximal small intestine via the large neutral amino acid (LNAA) transport carrier system
38
Patient information for l-dopa
- Dyskinesia common - Reduced efficacy over time - Avoid abrupt withdrawal
39
Dopamine Agonists examples
Rotigotine Bromocriptine Apoorphine Pramipexole
40
Mechanism of action of dopamine agonists
Dopamine agoinsts selective for the D2 receptor in the CNS Inhibits the release of prolactin from the anterior pituitary gland Duration longer than L-dopa Stiulates post synaptic dopamine receptors Apomorphine works also at D2 receptor- non selective Pramipexole: selective D3 receptor
41
Indication for dopamine agonists
Parkinsons disease
42
Side effects of dopamine agonists
apopmorphine: pain at site of injection, nausea, vomitting Pramipexole; hllucinations, nausea, drowiness, involuntary movements
43
Important PD/PK of dopamine agonists
Apomorphine: highly emetic, hence limited use. Short half life (40 mins). Needs to be given via injection. Pramipexole: Cimetidine increases its toxicity, long half life (8 hrs) Dopamine Agonists have reduced efficacy over time
44
Patient information for dopamine agonists
Apomorphine can only be injected | Dopamine agonists are weaker then L-DOPA so treatment may be modified in time.
45
Catechola-o-methyl transferase inhibitor
Entacapone
46
Mechanism of action of entacapone
Prevents the peripheral breakdown of levodopa by inhibiting COMT (COMT converts L-DOPA into 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD). 3-OMD doesn’t cross the blood brain barrier). Therefore more levodopa reaches the brain
47
Indication of catechol-o =-methyl transferase inhibitor
Parkinson’s Disease in conjunction with L-DOPA and dopamine decarboxylase inhibitor
48
Side effects of catechol-o-methyl transferase inhibitor
``` Dyskinesia (common, up to 27%) Nausea (11%) Abdominal pain Vomiting Dry mouth Dizziness ```
49
Important PK/PD of catechol-o-methyl transferase inibitor
Rapidly absorbed | Levodopa dose may need to be reduced by 10-30% when given with Entacapone
50
Patient information of catechol-methyl transferase inhibitor
- Urine may turn brown – normal - Could become lightheaded/dizzy while doing daily activities - Avoid abrupt withdrawal
51
Selegiline, rasagiline
MAO-B inhibitor
52
Mechanism of action of selegiline, rasagiline
- prevents dopamine breakdown by binding irreversibly to monoamine oxidase - can be prescribed as monotherapy in early disease or as adjunct in later disease - well tolerated

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