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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
Q

Statins

A

nephrogenic diabetes insipidus treatment
prevents internalisation of AQP2
more water is reabsorbed

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26
Q

heat shock protein 90 inhibitors

A

nephrogenic diabetes insipidus treatment

helps misfolded AQP2 reach the membrane

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27
Q

DEFINE: sedative

A

drug that causes calming, makes you drowsy and helps you sleep

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28
Q

DEFINE: anxiolytic

A

drug that reduces anxiety

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29
Q

DEFINE: hypnotic

A

treats symptoms of insomnia

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30
Q

what drugs are used to treat anxiety?

A
  • benzodiazepines
  • propranolol
  • buspirone
  • anti-depressants
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31
Q

how are β blockers used to treat anxiety? what is an example of a β blocker used to treat anxiety?

A

blocks sympathetic symptoms of anxiety

e.g. propranolol

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32
Q

which subunits of the GABAa receptor do benzodiazepines bind to?

A

α1, α2, α3 or α5

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33
Q

Muscimol

A

GABAa receptor agonist

binds to orthosteric site

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34
Q

Bicuculline

A

GABAa receptor competitive antagonist

binds to orthosteric site

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35
Q

Picrotoxin

A

GABAa receptor non-competitive antagonist
blocks channel
binds to orthosteric site
results in convulsions

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36
Q

Diazepam

A

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

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37
Q

Flumazenil

A

GABAa receptor competitive antagonist (competes with benzodiazepines) at allosteric site
prevents/reverses action of benzodiazepine
useful for treatment of diazepam overdose

38
Q

β-carboline

A

GABAa receptor inverse agonist

decreases frequency of channel opening

39
Q

GABAb receptor

A

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
Q

Baclofen

A

GABAb agonist

41
Q

Phaclofen

A

GABAb antagonist

42
Q

Rohypnol

A

prevents memory of events while under the influence

used as an anaesthetic for surgery

43
Q

Zoipidem

A

benzodiazepine
short half-life
insomnia treatment
not used as anxiety treatment

44
Q

Triazolam

A

benzodiazepine
short half life
insomnia treatment
may cause daytime anxiety when used to treat sleep disorders

45
Q

Promethazine

A

anti-histamine

insomnia treatment

46
Q

Diphenhydramine

A

anti-histamine

insomnia treatment

47
Q

Reserpine

A

depletes monoamine transmitters in the brain

causes depression

48
Q

Iproniazid

A

MAO inhibitor

antidepressant

49
Q

MAO

A

enzyme breaking down amine transmitters

found inside the neuron and outside the neuron

50
Q

Moclobemide

A

MAO subtype A inhibitor

Less side effects

51
Q

Phenylzine

A

MAO inhibitor

less selectivity

52
Q

Imipramine

A

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
Q

SSRIs e.g. fluoxetine

A

5-HT transporter (reuptakes 5-HT) inhibitor

anti-depressant

54
Q

Reboxitane

A

NA transporter (reuptakes NA) inhibitor

55
Q

dopamine β-hydroxylase

A

enzyme synthesising NA from dopamine

56
Q

Citalopram

A

5HT uptake inhibitor

57
Q

Propofol

A

intravenous anaesthetic

rapid metabolism so rapid recovery

58
Q

Etomidate

A

intravenous anaesthetic

avoids unwanted side effects e.g. respiratory and cardiovascular depression

59
Q

Thiopental

A 
intravenous anaesthetic 
barbiturate 
high lipid solubility 
rapid induction 
short duration of action due to redistribution
accumulates in fat = hangover
60
Q

Ketamine

A

analgesic
anti-depressant
anaesthetic
NMDA receptor blocker

61
Q

NO

A

inhalational anaesthetic

NMDA receptor blocker

62
Q

Dantrolene IV

A

RyR1 antagonist

counteract malignant hyperthermia triggered by inhalation anaesthetics

63
Q

Acetazolomide

A

carbonic anhydrase inhibitor
changes pH in a way which suppresses electrical activity in cerebellum
type I and type II episodic ataxia treatment

64
Q

Amphetamines

A

increase dopaminergic signalling

65
Q

Chlorpromazine

A

D2 receptor antagonist

anti-psychotic

66
Q

Haloperidol

A

D2 receptor antagonist

anti-psychotic

67
Q

COMT

A

enzyme breaking down amine transmitters, including dopamine

68
Q

Sulpiride

A

D2 receptor antagonist
Atypical anti-psychotic
Impacts other amine transmitter systems

69
Q

Clozapine

A

D2 receptor antagonist
Atypical anti-psychotic
Impacts other amine transmitter systems

70
Q

Risperidione

A

D2 receptor antagonist
Atypical anti-psychotic
Impacts other amine transmitter systems

71
Q

Mexilitene

A

voltage gated Na+ channel inhibitor
use dependent block
myotonia congenital treatment

72
Q

what is used to treat malignant hyperthermia?

A
  • 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
Q

Pyridostigmine

A

acetylcholinesterase inhibitor

treats mild symptoms of myasthenia gravis

74
Q

Prednisolone

A

corticosteroid
treats mild to moderate symptoms of myasthenia gravis
immunosuppressant - reduces antibodies (against AChR) levels

75
Q

Cyclosporin

A

immunosuppressant

myasthenia gravis treatment

76
Q

what is used to treat myasthenia gravis?

A
  • 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
Q

TTX

A

blocks neuronal and muscle voltage gated Na+ channels

78
Q

Saxitoxin

A

blocks neuronal and muscle voltage gated Na+ channels

79
Q

Conotoxin

A

blocks:
Cav2.2
Nav1.8

80
Q

Tetanus toxin

A

blocks ACh release into synaptic cleft

81
Q

Botulinum toxin

A

blocks ACh release into synaptic cleft

82
Q

Tubocurarine

A

blocks AChR channel

83
Q

Bungarotoxin

A

blocks AChR channel

84
Q

Eu1.6

A

conotoxin

inhibits voltage gated Ca2+ channels e.g. Cav2.2

85
Q

Tp1a

A

tarantula toxin
inhibits Nav1.7 in sensory neurons
decreases current
nM levels required to have an impact

86
Q

OD1

A

activates Nav1.7 and Nav1.6 on sensory neuron

Na+ channels open for longer so more likely to fire AP

87
Q

GPTx-1

A

Nav1.7 blocker
smaller currents
smaller open probability
analgesic in mice

88
Q

Barbiturate

A

Used in euthanasia

increases open time of GABAa receptor

89
Q

Alphaxalone

A

steroid

intravenous general anaesthetic

90
Q

Isoflurane

A

intravenous general anaesthetic

halogenated hydrocarbon

phys and pharm (15 decks)

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