Drug's List Flashcards
Metformin
Primary mechanism of action:
activates AMPK in hepatocyte mitochondria -> inhibits ATP production
blocks gluconeogenesis + subsequent glucose output
blocks adenylate cyclase which promotes fat oxidation
Both help to restore insulin sensitivity.
Metformin
Drug target:
5′-AMP-activated protein kinase (AMPK)
(in hepatocyte mitochondria)
Metformin
Main side effects:
GI side effects (20-30% of patients)
e.g. Abdominal pain, decreased appetite, diarrhoea, vomiting
Dipeptidyl-peptidase 4 (DPP-4) inhibitors
Example
Sitagliptin
Dipeptidyl-peptidase 4 (DPP-4) inhibitors
Primary mechanism of action:
inhibiting the action of DPP-4 and this increasing the conc of incretins in the plasma
help stimulate the production of insulin, slow down digestion and decrease appetite
Dipeptidyl-peptidase 4 (DPP-4) inhibitors:
Drug target
DPP-4 (vascular endothelium)
Dipeptidyl-peptidase 4 (DPP-4) inhibitors
Main side effects:
Upper respiratory tract infections
Flu-like symptoms
Sulphonylurea
Example:
Gliclazide
Sulphonylurea
Primary mechanism of action:
Inhibit the ATP-sensitive potassium (KATP) channel on the pancreatic beta cell
This channel controls beta cell membrane potential.
Inhibition causes depolarisation which stimulates Ca2+ influx and subsequent insulin vesicle exocytosis
Sulphonylurea
Drug target:
ATP-sensitive potassium channel
Sulphonylurea
Main side effects:
Weight gain
Hypoglycaemia
Sodium-glucose co-transporter (SGLT2) inhibitors
Example:
Dapaglifozin
Sodium-glucose co-transporter (SGLT2) inhibitors
Primary mechanism of action:
inhibits the SGLT2 co-transporter so that more Na and glucose + water is excreted in the urine
Sodium-glucose co-transporter (SGLT2) inhibitors
Drug target:
SGLT2 co-transporter in PCT
Sodium-glucose co-transporter (SGLT2) inhibitors
Main side effects:
UTI
Slight decrease in bone formation
Can worsen diabetic ketoacidosis
Lamotrigine
Primary mechanism of action:
Blocks voltage gated Na+ channels -> preventing Na+ influx.
Prevents depolarisation of glutamatergic neurones + reduces glutamate excitotoxicity
Lamotrigine
Drug target:
Voltage gated Na+ channels
Lamotrigine:
Main side effects
rash
drowsiness
SJS
suicidal thoughts
Sodium valproate
Primary mechanism of action:
Inhibition of GABA transaminase prevents the breakdown of GABA.
-> increases GABA concentrations directly in the synapse presynaptically
-> indirectly prolongs GABA in the synapse
Sodium valproate
Drug target:
GABA transaminase
Sodium valproate
Main side effects:
(MANY):
Common: Stomach pain and diarrhoea, drowsiness, weight gain, hair loss
Serious:
hepatotoxicity, teratogenicity, pancreatitis
Diazepam
Primary mechanism of action:
Increases choride ion influx in response to GABA binding at the GABA A receptor
-> hyperpolarisation of excitatory neurones.
Diazepam
Drug target:
Benzodiazepine site on the GABA A receptor
Diazepam
Main side effects:
Common:
Drowsiness, respiratory depression (if i.v. or at high dose)
Uncommon but serious:
Haemolytic anaemia, jaundice
Levetiracetam
Primary mechanism of action:
Inhibition of the synaptic vesicle protein SV2A
-> prevents vesicle exocytosis -> reduction in glutamate secretion
-> reduces glutamate excitotoxicity
Levetiracetam
Drug target:
Synaptic vesicle protein SV2A
Levetiracetam
Main side effects:
Common:
dizziness, somnolence, fatigue and headache
Sertraline
Primary mechanism of action:
inhibition of serotonin reuptake so that there is a higher conc of serotonin in the synapse
(Serotonin in the central nervous system plays a role in the regulation of mood, personality, and wakefulness)
Sertraline
Drug target:
Serotonin transporter
Sertraline
Main side effects:
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
Citalopram:
Primary mechanism of action
inhibition of serotonin reuptake so that there is a higher conc of serotonin in the synapse
(Serotonin in the central nervous system plays a role in the regulation of mood, personality, and wakefulness)
Citalopram
Drug target:
Serotonin transporter
Citalopram
Main side effects:
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
Fluoxetine
Primary mechanism of action:
inhibition of serotonin reuptake so that there is a higher conc of serotonin in the synapse
(Serotonin in the central nervous system plays a role in the regulation of mood, personality, and wakefulness)
Fluoxetine
Drug target:
Serotonin transporter
Fluoxetine
Main side effects:
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
Venlafaxine
Primary mechanism of action:
more potent inhibitor of serotonin reuptake than norepinephrine reuptake.
(Noradrenaline in the central nervous system is implicated in the regulation of emotions and cognition)
Venlafaxine
Drug target:
Serotonin transporter
Noradrenaline transporter
Venlafaxine
Main side effects:
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia, hypertension (at higher doses)
Mirtazapine
Primary mechanism of action:
Antagonises central presynaptic alpha-2-adrenergic receptors -> increased release of serotonin and norepinephrine.
Antagonises central 5HT2 receptors -> leaves 5HT1 receptors unopposed (anti-depressant effects)
Mirtazapine
Drug target:
Alpha-2 receptor
5-HT2 receptor
Mirtazapine
Main side effects:
Weight gain, sedation
Angiotensin converting enzyme inhibitors
Examples:
Ramipril
Lisinopril
Perindopril
Angiotensin converting enzyme inhibitors
Primary mechanism of action:
inhibits the angiotensin converting enzyme so that less angiotensin 2 is made and as such there is less vasoconstriction and aldosterone