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MBChB 3 Drug Database > Neurology/Psychiatry Drugs > Flashcards

Neurology/Psychiatry Drugs Flashcards

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1
Q

what is a dopamine precursor drug?

A

levodopa

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2
Q

what is the MoA for levodopa?

A

pro drug
crosses BBB and is converted to dopamine
striatal dopaminergic neurotransmission increased

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3
Q

what are the indications for levodopa?

A

PD

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4
Q

list some side effects of levodopa

A 
Dyskinesia
Compulsive disorders
Hallucinations
Nausea
GI upset
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5
Q

what is important regarding pharmaco-kinetics/dynamics for levodopa?

A

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

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6
Q

what info should be given to patient before starting levodopa?

A

Dyskinesia common
Reduced efficacy over time
Avoid abrupt withdrawal

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7
Q

what are some dopamine agonists?

A 
Apomorphine 
Pramipexole 
Bromocriptine 
Pergolide 
Rotigotine
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8
Q

what is the MoA for dopamine agonists?

A

Stimulate post synaptic dopamine receptors
Apomorphine: non selective D1 and D2 dopamine subfamily of receptors
Pramipexole: selective D3 receptor

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9
Q

what are the indications for dopamine agonists?

A

PD

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10
Q

list some side effects of dopamine agonists?

A

Apomorphine: pain at site of injection, nausea, vomiting
Pramipexole: hallucinations, nausea, drowsiness, involuntary movements

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11
Q

what is important regarding pharmaco-kinetics/dynamics for dopamine agonists?

A

Apomorphine: highly emetic, hence limited use. Short half life (40 mins). Needs to be via injection.
Pramipexole: Cimetidine increases its toxicity, long half life (8 hrs)
Dopamine Agonists have reduced efficacy over time

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12
Q

what info should be given to patient before starting a dopamine agonist?

A

Apomorphine can only be injected

Dopamine agonists are weaker then L-DOPA so treatment may be modified in time.

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13
Q

what is an example of a Catechol-o-methyl transferase Inhibitor (COMT)?

A

Entacapone

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14
Q

what are the indications for a COMT inhibitor?

A

Parkinson’s Disease in conjunction with L-DOPA and dopamine decarboxylase inhibitor

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15
Q

list the side effects of a COMT inhibitor?

A 
Dyskinesia
Nausea 
Abdominal pain
Vomiting
Dry mouth
Dizziness
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16
Q

what is important regarding pharmaco-kinetics/dynamics for a COMT inhibitor?

A

Rapidly absorbed

Levodopa dose may need to be reduced by 10-30% when given with Entacapone

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17
Q

what info should be given to patient before starting a COMT inhibitor?

A

Urine may turn brown – normal
Could become lightheaded/dizzy while doing daily activities
Avoid abrupt withdrawal

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18
Q

give examples of an anti-epileptic drug?

A 
Carbamazepine
sodium valproate
phenytoin
Lamotrigrine
Levetiracetam
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19
Q

what is the MoA for Carbamazepine?

A

Voltage gated Na+ channel blocker on pre-synaptic membrane

Blocks the Na+ influx; reduces neuronal excitability and decreases the action potential

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20
Q

what are the indications for Carbamazepine?

A

Epilepsy
Trigeminal Neuralgia
Neuropathic pain

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21
Q

list the side effects of Carbamazepine?

A 
Dizziness
Dry mouth
Ataxia
Fatigue
Headache
Diplopia
Blurred vision
Hyponatraemia
Stevens-Johnson’s syndrome
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22
Q

what is important regarding pharmaco-kinetics/dynamics for 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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23
Q

what info should be given to patient before starting Carbamazepine?

A

Avoid alcohol

Avoid grapefruit juice

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24
Q

what is the MoA of sodium valproate

A

Weak sodium ion channel blocker
Inhibitor of GABA degrading enzymes
Increased GABA stops action potential

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25
what are the indications for sodium valproate
Epilepsy Bipolar disorder Depression
26
list the side effects of sodium valproate
``` Nausea Diarrhoea Gastric irritation Weight gain Hyponatraemia Behavioral disturbances Confusion Stevens-Johnson Syndrome ```
27
what is important regarding pharmaco-kinetics/dynamics for sodium valproate
Enzyme inhibitor of cytochrome P450 Rapid absorption from GI tract – varies with formulation administered when administered Can cause interactions with other anti-epileptic drugs.
28
what info should be given to patient before starting sodium valproate
Avoid alcohol Take with food Do not take with milk Liver function test must be monitored before and during the initial 6 months
29
what is the MoA for phenytoin
Acts as a voltage-gated Na+ channel blocker on the pre-synaptic neuronal membrane Limits action potential transmission Hence limiting spread of seizure activity
30
what are the indications for phenytoin?
Epilepsy (including status epilepticus) | Trigeminal neuralgia
31
list the side effects of phenytoin:
``` nsomnia Headache Rash Constipation Vomiting Gingival hyperplasia Liver damage ``` Rare: Stevens-Johnson Syndrome, Leucopenia, Thrombocytopenia
32
what is important regarding pharmaco-kinetics/dynamics for phenytoin?
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
33
what info should be given to patient before starting phenytoin?
Avoid alcohol Do not take calcium, aluminum, magnesium or iron supplements within 2 hours of ingestion Take with food to reduce irritation
34
What is the MoA for Lamotrigrine?
Varied mechanism of action Inhibits voltage-gated Na+ channels and/or Ca2+ channels Acts on pre-synaptic neuronal membrane Reduces action potential and excitatory signals
35
what are the indications for Lamotrigrine?
Epilepsy (used for both partial and generalized seizures) | Depressive episodes associated with Bipolar disorder
36
list the side effects of Lamotrigrine:
``` Nausea Vomiting Diarrhoea Tremor Insomnia Blurred vision Aggression Skin reactions including Sevens-Johnson syndrome and toxic epidermal necrolysis (rare) ```
37
what is important regarding pharmaco-kinetics/dynamics for Lamotrigrine?
Half-life doubles in chronic renal impairment so dose adjustment is required.
38
what info should be given to patient before starting Lamotrigrine
Take without regard to meals | Seek medical advice if any rash or signs/symptoms of hypersensitivity.
39
What is the MoA for Levetiracetam?
SV2A is a synaptic vesicle protein required for neurotransmitter release Levetiracetam blocks this and reduced neurotransmitter release Induces an anti-epileptic effect
40
what are the indications for Levetiracetam?
Epilepsy
41
list the side effects of Levetiracetam?
``` Headache Fatigue Anxiety Irritability Drowsiness Constipation ```
42
what is important regarding pharmaco-kinetics/dynamics for Levetiracetam?
Rapidly and almost completely absorbed after oral administration (99%) Food does not affect bioavailability Cytochrome P450 is not involved in its metabolism
43
what info should be given to patient before starting Levetiracetam?
It might affect your ability to drive or operate machinery | Not recommended during pregnancy and breastfeeding
44
what are some examples of selective serotonin reuptake inhibitors (SSRIs)?
``` Citalopram Fluoxetine Paroxetine Escitalopram Sertraline ```
45
what is the MoA for SSRIs?
Inhibition of reuptake of serotonin at the serotonin reuptake pump of the synaptic cleft (in the central nervous system) Increases serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors
46
what are the indications for SSRIs?
Depression Bulimia Obsessive Compulsive Disorder
47
list the side effects of SSRIs:
``` Dry mouth Nausea Insomnia Anxiety Decreased libido Seizures (rare) Dyskinesia (rare) ```
48
what is important regarding pharmaco-kinetics/dynamics for SSRIs?
SSRIs bind with less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs. This leads to fewer side effects. Less dangerous in overdose than tricyclic antidepressant drugs.
49
what info should be given to patient before starting a SSRI?
Be wary with alcohol - toxicity possible Improvement in depressive symptoms may take several weeks to occur. Abrupt discontinuation from SSRIs may cause withdrawal symptoms (fatigue, tremor, sweating)
50
what are some examples of tricyclic antidepressants?
Amitriptyline Imipramine Doxepin
51
what is the MoA for tricyclic antidepressants?
Stops the reuptake of monoamines Binds to monoamine pump at pre-synaptic cleft The reduced reuptake of norepinephrine and/or serotonin combats depression
52
what are the indications for tricyclic antidepressants?
Depression Panic disorders Neuropathic pain
53
list the side effects of tricyclic antidepressants
Sedation (anti-histaminergic effects) Postural hypotension, tachycardia (anti-adrenergic effects) Urinary retention, dry mouth, blurred vision / diplopia (anti-cholinergic effects) overdose can be serious - causing seizures and cardiac arrhythmias
54
what is important regarding pharmaco-kinetics/dynamics for tricyclic antidepressants?
Blocks histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects Well absorbed orally First pass effect (liver)
55
what info should be given to patient before starting tricyclic antidepressants?
Reduction in depressive symptoms may take several weeks to appear.
56
what are some examples of anti-psychotic drugs?
1. First generation anti-psychotics. Act non selectively on D1-like and D2-like receptors = Haloperidol; Chlorpromazine 2. Atypical anti-psychotics. Varying effects on dopamine and serotonin receptors = Olanzapine; Clozapine
57
what is the MoA for anti-psychotic drugs?
Block dopamine receptors Action on mesolimbic and nigrostriatal parts of brain Also have anti-histaminergic and anti-cholinergic effects These effects reduce positive symptoms of schizophrenia and can cause sedation and provide anti-emetic activity.
58
what are the indications for anti-psychotic drugs?
``` Schizophrenia Mania Delusions, hallucinations Behavioral problems Anti-emetic (Haloperidol) ```
59
list the side effects of anti-psychotic drugs
Sedation (anti-histaminergic effect) Postural hypotension, tachycardia (anti-adrenergic effect) Urinary retention, dry mouth, blurry vision (anti-cholinergic effect)
60
what is important regarding pharmaco-kinetics/dynamics for anti-psychotic drugs?
Have effects on numerous receptor systems within the CNS
61
what info should be given to patient before starting anti-psychotic drugs?
Symptoms may not always disappear while on medication | Dosage may have to be increased if no improvement after a few weeks
62
what are 3 examples of benzodiazepines?
Diazepam Lorazepam Midazolam
63
what is the MoA for benzodiazepines?
Increases GABA affinity for GABA receptor GABA binding to receptor increases chloride flow through chloride channels Hyperpolarization occurs - reducing activity of limbic, thalamic and hypothalamic areas of the brain.
64
what are the indications or benzodiazepines?
Anxiety Epilepsy Muscle spasm Alcohol withdrawal
65
list the side effects of benzodiazepines
Sedation Ataxia Altered mental status Insomnia
66
what is important regarding pharmaco-kinetics/dynamics for benzodiazepines?
Diazepam is a long acting benzodiazepine with active metabolites. Can accumulate in longer term use and in patients with liver failure. Can be oral, rectal or parenteral. Lorazapam accumulates less with long term use or in patients with liver failure so is preferred in this setting. It cannot be given rectally. Midazolam is a potent and short acting benzodiazepine typically given parenterally, although buccal preparations exist.
67
what info should be given to patient before starting benzodiazepines?
Monitor breathing and report if severe breathlessness or palpitations Only prescribed for short terms – risk of addiction

MBChB 3 Drug Database (10 decks)

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