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drugs Flashcards

1
Q

Buspirone

A

5HT agonist
non-sedative
anxiolytic
takes a while for it to become effective

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2
Q

Phenytoin

A 
Na+ channel blocker
Anti-convulsant 
Non-sedative 
Used to treat grand mal and partial epilepsy  
Episodic ataxia treatment
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3
Q

What breaks down GABA?

A
  • GABA transaminase

- succinate semialdohyde dehydrogenase

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4
Q

Vigabatrin

A

inhibits GABA transaminase
suicide inhibitor
Anti-epileptic

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5
Q

What is a suicide inhibitor?

A

When a drug is bound to a compound (e.g. enzyme) it forms a covalent bond which inactivates the compound immediately

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6
Q

Tiagabine

A

GABA uptake inhibitor

Anti-epileptic

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7
Q

Valproate

A

HDAC inhibitor - increases transcription of GAD to increase GABA production
:( binds to other proteins e.g. can block NMDA receptors

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8
Q

Carbamazepine

A 
Na+ channel blocker 
Most widely used anti-epileptic 
Better side effect profile 
Less toxicity 
Type I episodic ataxia treatment
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9
Q

Lamotrigine

A

Na+ channel blocker
Anti-epileptic
Not used for absence seizures

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10
Q

What class of drugs are used for absence seizures?

A

T type Ca2+ channel blockers

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11
Q

Ethosuximide

A

T type Ca2+ channel blocker

Anti-epileptic

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12
Q

GABApentin

A

Prevents trafficking of T-type Ca2+ channels to the membrane by binding to α2δ subunit
Anti-epileptic
Analgesic

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13
Q

Levetiracetam

A 
targets SV2 (protein found in synaptic vesicles) 
decreases amount of glutamate stored in vesicles or interferes with fusion of vesicles with plasma membrane
Anti-epileptic
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14
Q

What mutations cause epilepsy?

A

Mutations in:
LOF Nav1.1 in inhibitory interneuron
LOF GABAa receptor on post-synaptic excitatory neuron
K+ channels
GOF Nicotinic ACh receptors on excitatory neurons downstream of 1st excitatory neuron
GOF Nav1.2 on excitatory axons

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15
Q

Amiloride

A

ENaC inhibitor

treatment for Liddle’s syndrome

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16
Q

Spironolactone

A

mineralocorticoid (e.g. aldosterone) receptor antagonist

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17
Q

desmopressin

A

antidiuretic
central diabetes insipidus treatment
binds AVPR2 –> response –> urine osmolality increases
effect decays away over time

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18
Q

cell permeable antagonists

A

nephrogenic diabetes insipidus treatment
enters cell and binds misfolded AVPR2 + unfolds AVPR2
AVPR2 shuttled to membrane
AVP binds AVPR2 (replaces antagonist)
AQP2 can shuttle to apical membrane

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19
Q

cell permeable receptor agonists

A

nephrogenic diabetes insipidus treatment
enters cell and stimulates misfolded AVPR2 while it is inside the cell, causing stimulation of downstream signalling pathway

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20
Q

cell permeable agonists

A

nephrogenic diabetes insipidus treatment
enters cell and binds + corrects misfolded AVPR2
corrected AVPR2 trafficked to membrane + bound agonist stimulates signalling

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21
Q

compounds bypassing AVPR2 signalling

A

nephrogenic diabetes insipidus treatment

  1. binds prostaglandin receptor
  2. activates cAMP
  3. AQP2 inserted in apical membrane
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22
Q

prostaglandin receptor agonists

A

nephrogenic diabetes insipidus treatment

induce AQP2 expression + membrane abundance

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23
Q

PDES inhibitor

A

nephrogenic diabetes insipidus treatment
inhibits cGMP breakdown
cGMP regulates AQP2 insertion

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24
Q

PDE4 inhibitor

A

nephrogenic diabetes insipidus treatment
inhibits cAMP breakdown
cAMP activates PKA which phosphorylates vesicles containing AQP2

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25
Statins
nephrogenic diabetes insipidus treatment prevents internalisation of AQP2 more water is reabsorbed
26
heat shock protein 90 inhibitors
nephrogenic diabetes insipidus treatment | helps misfolded AQP2 reach the membrane
27
DEFINE: sedative
drug that causes calming, makes you drowsy and helps you sleep
28
DEFINE: anxiolytic
drug that reduces anxiety
29
DEFINE: hypnotic
treats symptoms of insomnia
30
what drugs are used to treat anxiety?
- benzodiazepines - propranolol - buspirone - anti-depressants
31
how are β blockers used to treat anxiety? what is an example of a β blocker used to treat anxiety?
blocks sympathetic symptoms of anxiety | e.g. propranolol
32
which subunits of the GABAa receptor do benzodiazepines bind to?
α1, α2, α3 or α5
33
Muscimol
GABAa receptor agonist | binds to orthosteric site
34
Bicuculline
GABAa receptor competitive antagonist | binds to orthosteric site
35
Picrotoxin
GABAa receptor non-competitive antagonist blocks channel binds to orthosteric site results in convulsions
36
Diazepam
benzodiazepine GABAa receptor agonist at allosteric site increases frequency of GABAa receptor opening when GABA is bound increases affinity of receptor for GABA anxiolytic sedative anti-convulsant metabolised to produce active intermediate (chlordiazepoxide) with very long half life
37
Flumazenil
GABAa receptor competitive antagonist (competes with benzodiazepines) at allosteric site prevents/reverses action of benzodiazepine useful for treatment of diazepam overdose
38
β-carboline
GABAa receptor inverse agonist | decreases frequency of channel opening
39
GABAb receptor
metabotropic G-protein receptor located on the pre-synapse and post-synapse inhibits voltage gated Ca2+ channels on pre-synapse activates K+ channels (GIRK) on post-synapse mediates slow transmission
40
Baclofen
GABAb agonist
41
Phaclofen
GABAb antagonist
42
Rohypnol
prevents memory of events while under the influence | used as an anaesthetic for surgery
43
Zoipidem
benzodiazepine short half-life insomnia treatment not used as anxiety treatment
44
Triazolam
benzodiazepine short half life insomnia treatment may cause daytime anxiety when used to treat sleep disorders
45
Promethazine
anti-histamine | insomnia treatment
46
Diphenhydramine
anti-histamine | insomnia treatment
47
Reserpine
depletes monoamine transmitters in the brain | causes depression
48
Iproniazid
MAO inhibitor | antidepressant
49
MAO
enzyme breaking down amine transmitters | found inside the neuron and outside the neuron
50
Moclobemide
MAO subtype A inhibitor | Less side effects
51
Phenylzine
MAO inhibitor | less selectivity
52
Imipramine
inhibits post-synaptic NA transporters and 5-HT transporters (which reuptakes NA and 5-HT) NA and 5-HT accumulates at synapse --> more activation of post-synaptic NA and 5-HT receptors tricyclic antidepressant
53
SSRIs e.g. fluoxetine
5-HT transporter (reuptakes 5-HT) inhibitor | anti-depressant
54
Reboxitane
NA transporter (reuptakes NA) inhibitor
55
dopamine β-hydroxylase
enzyme synthesising NA from dopamine
56
Citalopram
5HT uptake inhibitor
57
Propofol
intravenous anaesthetic | rapid metabolism so rapid recovery
58
Etomidate
intravenous anaesthetic | avoids unwanted side effects e.g. respiratory and cardiovascular depression
59
Thiopental
``` intravenous anaesthetic barbiturate high lipid solubility rapid induction short duration of action due to redistribution accumulates in fat = hangover ```
60
Ketamine
analgesic anti-depressant anaesthetic NMDA receptor blocker
61
NO
inhalational anaesthetic | NMDA receptor blocker
62
Dantrolene IV
RyR1 antagonist | counteract malignant hyperthermia triggered by inhalation anaesthetics
63
Acetazolomide
carbonic anhydrase inhibitor changes pH in a way which suppresses electrical activity in cerebellum type I and type II episodic ataxia treatment
64
Amphetamines
increase dopaminergic signalling
65
Chlorpromazine
D2 receptor antagonist | anti-psychotic
66
Haloperidol
D2 receptor antagonist | anti-psychotic
67
COMT
enzyme breaking down amine transmitters, including dopamine
68
Sulpiride
D2 receptor antagonist Atypical anti-psychotic Impacts other amine transmitter systems
69
Clozapine
D2 receptor antagonist Atypical anti-psychotic Impacts other amine transmitter systems
70
Risperidione
D2 receptor antagonist Atypical anti-psychotic Impacts other amine transmitter systems
71
Mexilitene
voltage gated Na+ channel inhibitor use dependent block myotonia congenital treatment
72
what is used to treat malignant hyperthermia?
- dantrolene - iv hydration - sweating decreases ECV (results in decrease in BP) - diuretics - increased muscle breakdown produces myoglobin = toxic to kidney. diuretics increase urine flow rate to remove myoglobin and prevent kidney damage. - NaHCO3 - counters acidosis - mechanical hyperventilation removes CO2
73
Pyridostigmine
acetylcholinesterase inhibitor | treats mild symptoms of myasthenia gravis
74
Prednisolone
corticosteroid treats mild to moderate symptoms of myasthenia gravis immunosuppressant - reduces antibodies (against AChR) levels
75
Cyclosporin
immunosuppressant | myasthenia gravis treatment
76
what is used to treat myasthenia gravis?
- pyridostigmne = acetylcholinesterase inhibitor - prednisolone = corticosteroid - cyclosporin = immunosuppressant - IV immunoglobulins - treats severe symptoms. mops up antibodies by binding to them. - plasmapheresis - acute intervention/treats very severe symptoms. blood is filtered by immunoadsorption. filter contains molecules mimicking AChR which binds to the antibodies. - thymectomy - removal of tumour on thymus OR removal of thymus. removes AChR secreting β cells.
77
TTX
blocks neuronal and muscle voltage gated Na+ channels
78
Saxitoxin
blocks neuronal and muscle voltage gated Na+ channels
79
Conotoxin
blocks: Cav2.2 Nav1.8
80
Tetanus toxin
blocks ACh release into synaptic cleft
81
Botulinum toxin
blocks ACh release into synaptic cleft
82
Tubocurarine
blocks AChR channel
83
Bungarotoxin
blocks AChR channel
84
Eu1.6
conotoxin | inhibits voltage gated Ca2+ channels e.g. Cav2.2
85
Tp1a
tarantula toxin inhibits Nav1.7 in sensory neurons decreases current nM levels required to have an impact
86
OD1
activates Nav1.7 and Nav1.6 on sensory neuron | Na+ channels open for longer so more likely to fire AP
87
GPTx-1
Nav1.7 blocker smaller currents smaller open probability analgesic in mice
88
Barbiturate
Used in euthanasia | increases open time of GABAa receptor
89
Alphaxalone
steroid | intravenous general anaesthetic
90
Isoflurane
intravenous general anaesthetic | halogenated hydrocarbon

phys and pharm (15 decks)

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