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Pharmacology > Drug's List > Flashcards

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.

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2
Q

Metformin
Drug target:

A

5′-AMP-activated protein kinase (AMPK)

(in hepatocyte mitochondria)

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3
Q

Metformin
Main side effects:

A

GI side effects (20-30% of patients)

e.g. Abdominal pain, decreased appetite, diarrhoea, vomiting

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4
Q

Dipeptidyl-peptidase 4 (DPP-4) inhibitors
Example

A

Sitagliptin

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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

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6
Q

Dipeptidyl-peptidase 4 (DPP-4) inhibitors:
Drug target

A

DPP-4 (vascular endothelium)

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7
Q

Dipeptidyl-peptidase 4 (DPP-4) inhibitors
Main side effects:

A

Upper respiratory tract infections
Flu-like symptoms

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8
Q

Sulphonylurea
Example:

A

Gliclazide

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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

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10
Q

Sulphonylurea
Drug target:

A

ATP-sensitive potassium channel

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11
Q

Sulphonylurea
Main side effects:

A

Weight gain
Hypoglycaemia

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12
Q

Sodium-glucose co-transporter (SGLT2) inhibitors
Example:

A

Dapaglifozin

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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

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14
Q

Sodium-glucose co-transporter (SGLT2) inhibitors
Drug target:

A

SGLT2 co-transporter in PCT

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15
Q

Sodium-glucose co-transporter (SGLT2) inhibitors
Main side effects:

A

UTI
Slight decrease in bone formation
Can worsen diabetic ketoacidosis

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16
Q

Lamotrigine
Primary mechanism of action:

A

Blocks voltage gated Na+ channels -> preventing Na+ influx.

Prevents depolarisation of glutamatergic neurones + reduces glutamate excitotoxicity

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17
Q

Lamotrigine
Drug target:

A

Voltage gated Na+ channels

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18
Q

Lamotrigine:
Main side effects

A

rash
drowsiness
SJS
suicidal thoughts

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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

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20
Q

Sodium valproate
Drug target:

A

GABA transaminase

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21
Q

Sodium valproate
Main side effects:

A

(MANY):
Common: Stomach pain and diarrhoea, drowsiness, weight gain, hair loss
Serious:
hepatotoxicity, teratogenicity, pancreatitis

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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.

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23
Q

Diazepam
Drug target:

A

Benzodiazepine site on the GABA A receptor

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24
Q

Diazepam
Main side effects:

A

Common:
Drowsiness, respiratory depression (if i.v. or at high dose)

Uncommon but serious:
Haemolytic anaemia, jaundice

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25
Q

Levetiracetam
Primary mechanism of action:

A

Inhibition of the synaptic vesicle protein SV2A
-> prevents vesicle exocytosis -> reduction in glutamate secretion
-> reduces glutamate excitotoxicity

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26
Q

Levetiracetam
Drug target:

A

Synaptic vesicle protein SV2A

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27
Q

Levetiracetam
Main side effects:

A

Common:
dizziness, somnolence, fatigue and headache

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28
Q

Sertraline
Primary mechanism of action:

A

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)

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29
Q

Sertraline
Drug target:

A

Serotonin transporter

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30
Q

Sertraline
Main side effects:

A

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

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31
Q

Citalopram:
Primary mechanism of action

A

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)

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32
Q

Citalopram
Drug target:

A

Serotonin transporter

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33
Q

Citalopram
Main side effects:

A

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

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34
Q

Fluoxetine
Primary mechanism of action:

A

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)

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35
Q

Fluoxetine
Drug target:

A

Serotonin transporter

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36
Q

Fluoxetine
Main side effects:

A

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia

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37
Q

Venlafaxine
Primary mechanism of action:

A

more potent inhibitor of serotonin reuptake than norepinephrine reuptake.

(Noradrenaline in the central nervous system is implicated in the regulation of emotions and cognition)

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38
Q

Venlafaxine
Drug target:

A

Serotonin transporter

Noradrenaline transporter

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39
Q

Venlafaxine
Main side effects:

A

GI effects (nausea, diarrhoea), sexual dysfunction, anxiety, insomnia, hypertension (at higher doses)

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40
Q

Mirtazapine
Primary mechanism of action:

A

Antagonises central presynaptic alpha-2-adrenergic receptors -> increased release of serotonin and norepinephrine.

Antagonises central 5HT2 receptors -> leaves 5HT1 receptors unopposed (anti-depressant effects)

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41
Q

Mirtazapine
Drug target:

A

Alpha-2 receptor

5-HT2 receptor

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42
Q

Mirtazapine
Main side effects:

A

Weight gain, sedation

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43
Q

Angiotensin converting enzyme inhibitors
Examples:

A

Ramipril
Lisinopril
Perindopril

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44
Q

Angiotensin converting enzyme inhibitors
Primary mechanism of action:

A

inhibits the angiotensin converting enzyme so that less angiotensin 2 is made and as such there is less vasoconstriction and aldosterone

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45
Q

Angiotensin converting enzyme inhibitors
Drug target:

A

angiotensin converting enzyme

46
Q

Angiotensin converting enzyme inhibitors
Main side effects:

A

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
Q

Calcium channel blockers
Examples:

A

amlodipine
Felodipine

48
Q

Calcium channel blockers
Primary mechanism of action:

A

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
Q

Calcium channel blockers
Drug target:

A

L-type calcium channel
(predominantly on vascular smooth muscle)

50
Q

Calcium channel blockers
Main side effects:

A

Ankle oedema
Constipation
Palpitations
Flushing/Headaches

51
Q

Thiazide or thiazide-like diuretics
Examples:

A

Bendro-flumethiazide (thiazide)
Indapamide (thiazide-like)

52
Q

Thiazide or thiazide-like diuretics
Primary mechanism of action:

A

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
Q

Thiazide or thiazide-like diuretics
Drug target:

A

Sodium/chloride cotransporter in the PCT

54
Q

Thiazide or thiazide-like diuretics
Main side effects:

A

Hypokalemia
Hyponatremia.
Metabolic alkalosis (increased hydrogen ion excretion)
Hypercalcemia.
Hyperglycemia (hyperpolarised pancreatic beta cells).
Hyperuricemia

55
Q

Angiotensin receptor blockers
Examples:

A

Losartan
Irbesartan
Candesartan

56
Q

Angiotensin receptor blockers
Primary mechanism of action:

A

non-competitive antagonists at AT1 receptor
(found on kidneys and on the vasculature)

57
Q

Angiotensin receptor blockers
Drug target:

A

Angiotensin receptor
(found on kidneys and on the vasculature)

58
Q

Angiotensin receptor blockers
Main side effects:

A

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
Q

Salbutamol
Primary mechanism of action:

A

β2 receptor agonist on airway smooth muscle cells. -> reduces Ca2+ entry -> prevents smooth muscle contraction

60
Q

Salbutamol
Drug target:

A

β2 receptor agonist
(airway smooth muscle cells)

61
Q

Salbutamol
Main side effects:

A

Palpitations/ agitation
Tachycardia/ Arrythmias
Hypokalaemia (at higher doses)

62
Q

Fluticasone
Primary mechanism of action:

A

Multiple actions on many different cell types.

directly decreases number of inflammatory cells + cytokines they produce.

63
Q

Fluticasone
Drug target:

A

Glucocorticoid receptor

64
Q

Fluticasone
Main side effects:

A

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
Q

Mometasone
Primary mechanism of action:

A

Multiple actions on many different cell types.

directly decreases number of inflammatory cells + cytokines they produce.

66
Q

Mometasone
Drug target:

A

Glucocorticoid receptor

67
Q

Mometasone
Main side effects:

A

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
Q

Budesonide
Primary mechanism of action:

A

Multiple actions on many different cell types.

directly decreases number of inflammatory cells + cytokines they produce.

69
Q

Budesonide
Drug target:

A

Glucocorticoid receptor

70
Q

Budesonide
Main side effects:

A

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
Q

Montelukast
Primary mechanism of action:

A

CysLT1 leukotriene receptor antagonist (on eosinophils, mast cells and airway smooth muscle cells)

-> decreases eosinophil migration, broncho-constriction and inflammation induced oedema

72
Q

Montelukast
Drug target:

A

CysLT1 leukotriene receptor
(on eosinophils, mast cells and airway smooth muscle cells)

73
Q

Montelukast
Main side effects:

A

Mild side effects:
Diarrhoea
Fever
Headaches
Nausea or vomiting

Serious side effects:
Mood changes
Anaphylaxis

74
Q

NSAIDS:
Examples

A

ibuprofen
naproxen
diclofenac

75
Q

NSAIDS:
Primary mechanism of action

A

blocks COX -> less PGs -> less pain

76
Q

NSAIDS:
Drug target

77
Q

NSAIDS:
Main side effects

A

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
Q

Proton pump inhibitors (PPIs)
Examples:

A

omeprazole
lansoprazole

79
Q

Proton pump inhibitors (PPIs)
Primary mechanism of action:

A

Irreversible inhibitors of H+/K+ ATPase in gastric parietal cells.

Proton pump inhibitors inhibit basal and stimulated gastric acid secretion by >90%.

80
Q

Proton pump inhibitors (PPIs)
Drug target:

A

H+/K ATPase (proton pump)

81
Q

Proton pump inhibitors (PPIs)
Main side effects:

A

Unwanted effects are uncommon but may include headache, diarrhoea, bloating, abdominal pain & rashes.

82
Q

Histamine (H2) receptor antagonists
Examples:

A

ranitidine

83
Q

Histamine (H2) receptor antagonists
Primary mechanism of action:

A

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
Q

Histamine (H2) receptor antagonists
Drug target:

A

Histamine H2 receptor
(parietal cell)

85
Q

Histamine (H2) receptor antagonists
Main side effects:

A

Incidence of side-effects is low.

Diarrhoea, dizziness, muscle pains & transient rashes have been reported.

86
Q

Paracetamol (aka acetaminophen)
Primary mechanism of action:

A

inhibit a peroxidase enzyme which is involved in the conversion of arachidonic acid to prostaglandins

87
Q

Paracetamol (aka acetaminophen)
Drug target:

A

Unclear.
5HT3 receptors/Cannabinoid reuptake proteins/Peroxidase

88
Q

Paracetamol (aka acetaminophen)
Main side effects:

A

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
Q

Statins
Examples:

A

atorvostatin
Simvastatin

90
Q

Statins
Primary mechanism of action:

A

competitively inhibits HMG-CoA reductase

91
Q

Statins
Drug target:

A

HMG-CoA reductase

92
Q

Statins
Main side effects:

A

Muscle toxicity

Constipation or diarrhoea + other GI symptoms.

93
Q

Aspirin
Primary mechanism of action:

A

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
Q

Aspirin
Drug target:

95
Q

Aspirin
Main side effects:

A

Dyspepsia
Haemorrhage

96
Q

Trimethoprim
Primary mechanism of action:

A

Direct competitor of the enzyme dihydrofolate reductase.

preventing synthesis of purines required for DNA and protein production.

97
Q

Trimethoprim
Drug target:

A

Dihydrofolate reductase

98
Q

Trimethoprim
Main side effects:

A

Diarrhoea
Skin reactions

99
Q

Gentamicin
Primary mechanism of action:

A

Binds to the bacterial 30s ribosomal subunit disturbing the translation of mRNA leading to the formation of dysfunctional proteins.

100
Q

Gentamicin
Drug target:

A

30s ribosomal subunit

101
Q

Gentamicin
Main side effects:

A

Ototoxicity and nephrotoxicity are important side effects to consider.

102
Q

Opioids
Examples (weak):

A

codeine
tramadol

103
Q

Opioids
Examples (strong):

A

morphine
fentanyl (heroin)

104
Q

Opioids
Primary mechanism of action:

A

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
Q

Opioids
Drug target:

A

Opioid receptor

106
Q

Opioids
Main side effects:

A

Mild – nausea & vomiting and constipation

OVERDOSE - respiratory depression

107
Q

Co-amoxiclav
Primary mechanism of action:

A

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
Q

Co-amoxiclav
Drug target:

A

Amoxicillin = penicillin binding proteins
Clavulanate = beta lactamase

109
Q

Co-amoxiclav
Main side effects:

A

few

nausea and diarrhoea

110
Q

Lactulose
Primary mechanism of action:

A

non-absorbable disaccharide

reaches the large bowel unchanged

-> water retention via osmosis -> easier to pass stool

111
Q

Lactulose
Drug target:

A

No drug target

112
Q

Lactulose
Main side effects:

A

Abdominal pain, diarrhoea, flatulence, nausea

Pharmacology (10 decks)

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