Drug Targets Flashcards

1
Q

Corticosteroids

A

Nomenclature: “-son” or “-one”

MOA: bind glucocorticoid receptors and ultimately modulate transcription

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2
Q

Imatinib (Gleevec)

A

MOA: Y kinase inhibitor binds ATP binding site on bcr-abl

Use: CML

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3
Q

Strychnine

A

MOA: competitive inhibitor of glycine at glycine receptors

Effect: excessive spasticity

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4
Q

Methylxantines

A

Ex: caffeine, theophylline

MOA: competitive inhibitors of adenosine receptors

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5
Q

Tetrodotoxin

A

MOA: blocks voltage gated Na+ channels in nerve and muscle

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6
Q

Midazolam metabolism

A

MOA: benzodiazipine - increases frequency of GABAa receptor Cl- channel openings

Metabolism: CYP3A4 + glucuronide conjugation

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7
Q

Benzodiazepines

A

Nomenclature: “-azepam” or “-azolam” drugs

MOA: allosteric activator of GABAa receptors, increasing frequency of GABAa-gated Cl- channel opening and increasing synaptic inhibition.

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8
Q

Tetanus toxin

A

MOA: presynaptic inhibitor of glycine release

Effect: excessive spasticity

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9
Q

Memantine

A

MOA: open channel blocker (uncompetitive inhibitor) of glutamate-NMDA Ca2+ channel

Use: Alzheimer’s

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10
Q

Cimetidine metabolism

A

MOA: H2 histamine receptor blocker

Notes: also inhibits many CYPs

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11
Q

Diazepam (Valium)

A

MOA: Allosteric activator of GABAa gated Cl- channel

Notes: Good TI (~100)

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12
Q

Zolpidem (Ambien)

A

MOA: allosteric activator of GABAa-gated Cl- channel

Use: sleep aid

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13
Q

Local anaesthetics

A

MOA: block voltage gated Na+ channel associated with the action potential; preferentially binds inactivated state of channel

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14
Q

Warfarin

A

MOA: inhibits synthesis of clotting factors via inhibition of VKORC1

Use: Prevent clots after surgery, Afib

Notes: Low TI (~1)

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15
Q

Penicillin

A

MOA: open channel blocker of GABAa receptor

Effect: inhibition of inhibitory signalling => excessive excitation and seizures

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16
Q

Ondansetron

A

Nomenclature: “-setron” drugs

MOA: Competitive inhibitors of serotonin 5HT-3 receptors

Use: Treat nausea and vomiting