Drug's List Flashcards
1
Q
Metformin
Primary mechanism of action:
A
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.
2
Q
Metformin
Drug target:
A
5′-AMP-activated protein kinase (AMPK)
(in hepatocyte mitochondria)
3
Q
Metformin
Main side effects:
A
GI side effects (20-30% of patients)
e.g. Abdominal pain, decreased appetite, diarrhoea, vomiting
4
Q
Dipeptidyl-peptidase 4 (DPP-4) inhibitors
Example
A
Sitagliptin
5
Q
Dipeptidyl-peptidase 4 (DPP-4) inhibitors
Primary mechanism of action:
A
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
6
Q
Dipeptidyl-peptidase 4 (DPP-4) inhibitors:
Drug target
A
DPP-4 (vascular endothelium)
7
Q
Dipeptidyl-peptidase 4 (DPP-4) inhibitors
Main side effects:
A
Upper respiratory tract infections
Flu-like symptoms
8
Q
Sulphonylurea
Example:
A
Gliclazide
9
Q
Sulphonylurea
Primary mechanism of action:
A
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
10
Q
Sulphonylurea
Drug target:
A
ATP-sensitive potassium channel
11
Q
Sulphonylurea
Main side effects:
A
Weight gain
Hypoglycaemia
12
Q
Sodium-glucose co-transporter (SGLT2) inhibitors
Example:
A
Dapaglifozin
13
Q
Sodium-glucose co-transporter (SGLT2) inhibitors
Primary mechanism of action:
A
inhibits the SGLT2 co-transporter so that more Na and glucose + water is excreted in the urine
14
Q
Sodium-glucose co-transporter (SGLT2) inhibitors
Drug target:
A
SGLT2 co-transporter in PCT
15
Q
Sodium-glucose co-transporter (SGLT2) inhibitors
Main side effects:
A
UTI
Slight decrease in bone formation
Can worsen diabetic ketoacidosis
16
Q
Lamotrigine
Primary mechanism of action:
A
Blocks voltage gated Na+ channels -> preventing Na+ influx.
Prevents depolarisation of glutamatergic neurones + reduces glutamate excitotoxicity
17
Q
Lamotrigine
Drug target:
A
Voltage gated Na+ channels
18
Q
Lamotrigine:
Main side effects
A
rash
drowsiness
SJS
suicidal thoughts
19
Q
Sodium valproate
Primary mechanism of action:
A
Inhibition of GABA transaminase prevents the breakdown of GABA.
-> increases GABA concentrations directly in the synapse presynaptically
-> indirectly prolongs GABA in the synapse
20
Q
Sodium valproate
Drug target:
A
GABA transaminase
21
Q
Sodium valproate
Main side effects:
A
(MANY):
Common: Stomach pain and diarrhoea, drowsiness, weight gain, hair loss
Serious:
hepatotoxicity, teratogenicity, pancreatitis
22
Q
Diazepam
Primary mechanism of action:
A
Increases choride ion influx in response to GABA binding at the GABA A receptor
-> hyperpolarisation of excitatory neurones.
23
Q
Diazepam
Drug target:
A
Benzodiazepine site on the GABA A receptor
24
Q
Diazepam
Main side effects:
A
Common:
Drowsiness, respiratory depression (if i.v. or at high dose)
Uncommon but serious:
Haemolytic anaemia, jaundice
25
Levetiracetam
Primary mechanism of action:
Inhibition of the synaptic vesicle protein SV2A
-> prevents vesicle exocytosis -> reduction in glutamate secretion
-> reduces glutamate excitotoxicity
26
Levetiracetam
Drug target:
Synaptic vesicle protein SV2A
27
Levetiracetam
Main side effects:
Common:
dizziness, somnolence, fatigue and headache
28
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)
29
Sertraline
Drug target:
Serotonin transporter
30
Sertraline
Main side effects:
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
31
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)
32
Citalopram
Drug target:
Serotonin transporter
33
Citalopram
Main side effects:
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
34
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)
35
Fluoxetine
Drug target:
Serotonin transporter
36
Fluoxetine
Main side effects:
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia
37
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)
38
Venlafaxine
Drug target:
Serotonin transporter
Noradrenaline transporter
39
Venlafaxine
Main side effects:
GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia, hypertension (at higher doses)
40
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)
41
Mirtazapine
Drug target:
Alpha-2 receptor
5-HT2 receptor
42
Mirtazapine
Main side effects:
Weight gain, sedation
43
Angiotensin converting enzyme inhibitors
Examples:
Ramipril
Lisinopril
Perindopril
44
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
45
Angiotensin converting enzyme inhibitors
Drug target:
angiotensin converting enzyme
46
Angiotensin converting enzyme inhibitors
Main side effects:
cough
Hypotension
Hyperkalaemia (care with K+ supplements or K+-sparing diuretics)
Foetal Injury (AVOID IN PREGNANT WOMEN)
Renal failure (in patients with renal artery stenosis)-
Urticaria/Angioedema
47
Calcium channel blockers
Examples:
amlodipine
Felodipine
48
Calcium channel blockers
Primary mechanism of action:
Block L-type calcium channels
-> decrease in calcium influx (with downstream inhibition of myosin light chain kinase and prevention of cross-bridge formation).
-> vasodilation -> reduced peripheral resistance.
49
Calcium channel blockers
Drug target:
L-type calcium channel
(predominantly on vascular smooth muscle)
50
Calcium channel blockers
Main side effects:
Ankle oedema
Constipation
Palpitations
Flushing/Headaches
51
Thiazide or thiazide-like diuretics
Examples:
Bendro-flumethiazide (thiazide)
Indapamide (thiazide-like)
52
Thiazide or thiazide-like diuretics
Primary mechanism of action:
block the Na+, Cl- co-transporter in the early DCT.
-> Na+ and Cl- reabsorption is inhibited.
-> osmolarity of the tubular fluid increases, decreasing the osmotic gradient for water reabsorption in the collecting duct
53
Thiazide or thiazide-like diuretics
Drug target:
Sodium/chloride cotransporter in the PCT
54
Thiazide or thiazide-like diuretics
Main side effects:
Hypokalemia
Hyponatremia.
Metabolic alkalosis (increased hydrogen ion excretion)
Hypercalcemia.
Hyperglycemia (hyperpolarised pancreatic beta cells).
Hyperuricemia
55
Angiotensin receptor blockers
Examples:
Losartan
Irbesartan
Candesartan
56
Angiotensin receptor blockers
Primary mechanism of action:
non-competitive antagonists at AT1 receptor
(found on kidneys and on the vasculature)
57
Angiotensin receptor blockers
Drug target:
Angiotensin receptor
(found on kidneys and on the vasculature)
58
Angiotensin receptor blockers
Main side effects:
Hypotension
Hyperkalaemia (care with K+ supplements or K+-sparing diuretics)
Foetal Injury (AVOID IN PREGNANT WOMEN)
Renal failure (in patients with renal artery stenosis)-
59
Salbutamol
Primary mechanism of action:
β2 receptor agonist on airway smooth muscle cells. -> reduces Ca2+ entry -> prevents smooth muscle contraction
60
Salbutamol
Drug target:
β2 receptor agonist
(airway smooth muscle cells)
61
Salbutamol
Main side effects:
Palpitations/ agitation
Tachycardia/ Arrythmias
Hypokalaemia (at higher doses)
62
Fluticasone
Primary mechanism of action:
Multiple actions on many different cell types.
directly decreases number of inflammatory cells + cytokines they produce.
63
Fluticasone
Drug target:
Glucocorticoid receptor
64
Fluticasone
Main side effects:
Local side effects:
Sore throat, hoarse voice, opportunistic oral infections
Systemic side effects:
Growth retardation in children
Hyperglycaemia
Decreased bone mineral density
Immunosuppression
Effects on mood
(Many others)
65
Mometasone
Primary mechanism of action:
Multiple actions on many different cell types.
directly decreases number of inflammatory cells + cytokines they produce.
66
Mometasone
Drug target:
Glucocorticoid receptor
67
Mometasone
Main side effects:
Local side effects:
Sore throat, hoarse voice, opportunistic oral infections
Systemic side effects:
Growth retardation in children
Hyperglycaemia
Decreased bone mineral density
Immunosuppression
Effects on mood
(Many others)
68
Budesonide
Primary mechanism of action:
Multiple actions on many different cell types.
directly decreases number of inflammatory cells + cytokines they produce.
69
Budesonide
Drug target:
Glucocorticoid receptor
70
Budesonide
Main side effects:
Local side effects:
Sore throat, hoarse voice, opportunistic oral infections
Systemic side effects:
Growth retardation in children
Hyperglycaemia
Decreased bone mineral density
Immunosuppression
Effects on mood
(Many others)
71
Montelukast
Primary mechanism of action:
CysLT1 leukotriene receptor antagonist (on eosinophils, mast cells and airway smooth muscle cells)
-> decreases eosinophil migration, broncho-constriction and inflammation induced oedema
72
Montelukast
Drug target:
CysLT1 leukotriene receptor
(on eosinophils, mast cells and airway smooth muscle cells)
73
Montelukast
Main side effects:
Mild side effects:
Diarrhoea
Fever
Headaches
Nausea or vomiting
Serious side effects:
Mood changes
Anaphylaxis
74
NSAIDS:
Examples
ibuprofen
naproxen
diclofenac
75
NSAIDS:
Primary mechanism of action
blocks COX -> less PGs -> less pain
76
NSAIDS:
Drug target
COX
77
NSAIDS:
Main side effects
gastric irritation, ulceration and bleeding and, in extreme cases, perforation
reduced creatinine clearance and possible nephritis
and bronchoconstriction in susceptible individuals (contraindicated in asthma)
Skin rashes & other allergies, dizziness, tinnitus.
Adverse cardiovascular effects (hypertension, stroke, MI) may occur following prolonged use or in patients with pre-existing CV risk.
Prolonged analgesic abuse over a period of years is associated with chronic renal failure.
Aspirin has been linked with a rare but serious post-viral encephalitis (Reye’s syndrome) in children.
78
Proton pump inhibitors (PPIs)
Examples:
omeprazole
lansoprazole
79
Proton pump inhibitors (PPIs)
Primary mechanism of action:
Irreversible inhibitors of H+/K+ ATPase in gastric parietal cells.
Proton pump inhibitors inhibit basal and stimulated gastric acid secretion by >90%.
80
Proton pump inhibitors (PPIs)
Drug target:
H+/K ATPase (proton pump)
81
Proton pump inhibitors (PPIs)
Main side effects:
Unwanted effects are uncommon but may include headache, diarrhoea, bloating, abdominal pain & rashes.
82
Histamine (H2) receptor antagonists
Examples:
ranitidine
83
Histamine (H2) receptor antagonists
Primary mechanism of action:
competitive antagonists of H2 histamine receptors
inhibit the stimulatory action of histamine released from enterochromaffin-like (ECL) cells on the gastric parietal cells
inhibit gastric acid secretion by approximately 60%.
84
Histamine (H2) receptor antagonists
Drug target:
Histamine H2 receptor
(parietal cell)
85
Histamine (H2) receptor antagonists
Main side effects:
Incidence of side-effects is low.
Diarrhoea, dizziness, muscle pains & transient rashes have been reported.
86
Paracetamol (aka acetaminophen)
Primary mechanism of action:
inhibit a peroxidase enzyme which is involved in the conversion of arachidonic acid to prostaglandins
87
Paracetamol (aka acetaminophen)
Drug target:
Unclear.
5HT3 receptors/Cannabinoid reuptake proteins/Peroxidase
88
Paracetamol (aka acetaminophen)
Main side effects:
Relatively safe drug with few common side effects.
OVERDOSE:
Liver damage and less frequently renal damage.
Nausea and vomiting early features of poisoning (settle in 24h).
Onset of right subcostal pain after 24hindicates hepatic necrosis.
89
Statins
Examples:
atorvostatin
Simvastatin
90
Statins
Primary mechanism of action:
competitively inhibits HMG-CoA reductase
91
Statins
Drug target:
HMG-CoA reductase
92
Statins
Main side effects:
Muscle toxicity
Constipation or diarrhoea + other GI symptoms.
93
Aspirin
Primary mechanism of action:
Irreversible inactivation of COX enzyme.
Prevents oxidation of arachidonic acid to produce prostaglandins.
Reduction of thromboxane A2 in platelets reduces aggregation.
Reduction of PGE2
- (i) at sensory pain neurones reduces pain and sensation
- (ii) in the brain decreases fever.
94
Aspirin
Drug target:
COX
95
Aspirin
Main side effects:
Dyspepsia
Haemorrhage
96
Trimethoprim
Primary mechanism of action:
Direct competitor of the enzyme dihydrofolate reductase.
preventing synthesis of purines required for DNA and protein production.
97
Trimethoprim
Drug target:
Dihydrofolate reductase
98
Trimethoprim
Main side effects:
Diarrhoea
Skin reactions
99
Gentamicin
Primary mechanism of action:
Binds to the bacterial 30s ribosomal subunit disturbing the translation of mRNA leading to the formation of dysfunctional proteins.
100
Gentamicin
Drug target:
30s ribosomal subunit
101
Gentamicin
Main side effects:
Ototoxicity and nephrotoxicity are important side effects to consider.
102
Opioids
Examples (weak):
codeine
tramadol
103
Opioids
Examples (strong):
morphine
fentanyl (heroin)
104
Opioids
Primary mechanism of action:
Over-arching mechanism at a cellular level is a depressant effect on cellular activity.
Multiple sites within pain pathway, where activation of the opioid receptor leads to decreased perception or increased tolerance to pain.
105
Opioids
Drug target:
Opioid receptor
106
Opioids
Main side effects:
Mild – nausea & vomiting and constipation
OVERDOSE - respiratory depression
107
Co-amoxiclav
Primary mechanism of action:
binds to bacterial penicillin binding proteins -> prevents transpeptidation
Clavulanate is an inhibitor of beta lactamase.
Beta lactamase is a bacterial enzyme that can degrade beta lactam antibiotics and thus confer resistance to these antibiotics.
108
Co-amoxiclav
Drug target:
Amoxicillin = penicillin binding proteins
Clavulanate = beta lactamase
109
Co-amoxiclav
Main side effects:
few
nausea and diarrhoea
110
Lactulose
Primary mechanism of action:
non-absorbable disaccharide
reaches the large bowel unchanged
-> water retention via osmosis -> easier to pass stool
111
Lactulose
Drug target:
No drug target
112
Lactulose
Main side effects:
Abdominal pain, diarrhoea, flatulence, nausea
