Mechanism of action of phase 1 drugs

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Hint	Answer
beta-1 adrenergic receptor antagonists	bisoprolol, atenolol
beta-1 adrenergic receptor antagonists MoA	antagonist binds to beta-1 adrenergic receptor on cardiomyocytes reducing inotropy and chronotropy
ACE inhibitors	ramipril, lisinopril
ACE inhibitors MoA	antagonist inhibits conversion of angiotensin 1 to angiotensin 2, lowering angiotensin 2 levels and reducing cardiac afterload and vasoconstriction
ARBs	losartan, valsartan
ARBs MoA	antagonist inhibits angiotensin 2 receptor reducing cardiac afterload and vasoconstriction
HMG-CoA reductase blockers	atorvastatin, simvastatin
HMG-CoA reductase blockers MoA	inhibits mevalonate metabolism in cholesterol synthesis pathway and enhances low-density lipoprotein uptake which lowers plasma cholesterol
Calcium channel antagonists	nifedipine, amlodipine
Calcium channel antagonists MoA	blockades L-type calcium channels on vascular smooth muscle cells which promotes vasodilation
Nitrate vasodilators	glycerol trinitrate, isosorbide mononitrate
Nitrate vasodilators MoA	releases nitric oxide which promotes dilation of smooth muscle in coronary arteries and veins
Neprilysin inhibitors	sacubitril
Neprilysin inhibitors MoA	inhibits neprilysin enzyme which increases natriuretic peptide hormone levels. promotes natriuresis, reduces cardiac preload, improves renal function, decreases fluid retention and increases vasodilation
Antiplatelet drugs	aspirin, clopidogrel
Antiplatelet drugs MoA	antagonists that reduce platelet activation preventing thrombosis. aspirin binds to COX enzyme and inhibits thromboxane A2 production, clopidogrel binds to and inhibits ADP receptors
Anticoagulants	unfractionated heparin, low molecular weight heparin, dalteparin, tinzaparin
Anticoagulants MoA	enhances action of antithrombin 3 to inhibit thrombin and factor Xa, reduces coagulation cascade activity
NSAIDs	ibuprofen, naproxen, diclofenac
NSAIDs MoA	antagonist, inhibit COX activity, block production of prostaglandins from arachidonic acid, reduced na channel opening, reduced depolarisation
Weak analgesics	paracetamol
Weak analgesics MoA	antagonist, inhibits COX activity in CNS not PNS, acts on heat-regulating centres in brain with antipyretic use
Weak opioids	codeine, dihydrocodeine
Strong opioids	morphine, diamorphine
Synthetic opioid	tramadol
Mixed agonist-antagonist opioid	buprenorphine
Opioid receptor antagonist	naloxone
Opioid MoA	agonist, binds to mu-opioid receptors and activates G0 G-protein which switches off cAMP production, inhibits opening of voltage-dependent Ca2+ channels causing reduced Ca2+ influx into the neuron, opens K+ channels in neuron which stimulates K+ outflow from neuron, this promotes hyperpolarisation of neurons reducing their activity
MAOI-b inhibitors	selegiline
MAOI-b inhibitors MoA	antagonist, selectively inhibits the MAO enzyme to sustain neuronal dopamine levels
COMT inhibitors	entacapone
COMT inhibitors MoA	antagonist, inhibits COMT enzymes which themselves inactivate peripheral levodopa, this increases bioavailability of CNS levodopa which increases bioavailability of dopamine
Dopaminergic drugs	levodopa
Dopaminergic drugs MoA	levodopa is a metabolic precursor to dopamine, it is naturally converted into dopamine within neurons to enable dopaminergic neurotransmission
Dopamine receptor agonists	pramipexole, ropinirole
Dopamine receptor agonists MoA	agonist, interacts directly with dopamine receptors in the post-synaptic neuron
Dopa-decarboxylase inhibitors	carbidopa
Dopa-decarboxylase inhibitors MoA	inhibits DDC enzyme activity within periphery increasing levodopa levels within periphery which increases bioavailability of levodopa in CNS
Glucocorticosteroid for CNS inflammation	dexamethasone
Glucocorticosteroid for CNS inflammation MoA	corticosteroid enters cell, binds and forms a complex with glucocorticoid receptor, then acts as a transcription factor enhancing expression of anti-inflammatory products and suppressing pro-inflammatory mediators
Anticholinesterases	donepezil, galantamine
Anticholinesterases MoA	antagonist, inhibits acetylcholinesterase
SSRIs MoA	antagonist, inhibits serotonin 5HT reuptake transporters which increases availability of 5HT in synaptic cleft
SSRIs	sertraline, citalopram
SNRIs	venlafaxine
SNRIs MoA	antagonist, inhibits serotonin-noradrenaline reuptake transporters which increases availability of these neurotransmitters in the synaptic cleft
MAOIs	moclobemide
MAOIs MoA	antagonist, inhibits activity of monoamine A oxidase enzyme which breaks down neurotransmitters, therefore MAOIs increase availability of selective neurotransmitters in the CNS. inhibition is reversible.
Anti-epileptics	valproate, carbamazepine, diazepam
Anti-epileptics MoA	antagonist, inhibits of voltage gated Na channels 2. increases GABA availability
Benzodiazepines	diazepam
Benzodiazepines MoA	agonist, binds to specific sites on GABA-A receptors causing opening of Cl- channels enhancing the inhibitory effect of GABA, which then inhibits neurotransmitter activity
Bisphosphonates	alendronate, pamidronate
Bisphosphonate MoA	antagonist, binds to hydroxyapatite, inhibits osteoclast activity reducing bone breakdown
Selective oestrogen receptor modulator	raloxifene
Selective oestrogen receptor modulator MoA	agonist, activates oestrogen receptor which stimulates osteoblast production and inhibits osteoclast activity maintaining bone density
Bone biologic	denosumab
Bone biologic MoA	antagonist inhibits osteoclast activity
Bone hormones	parathyroid hormone, calcitonin
Bone hormones MoA	modulation of calcium metabolism and bone resorption
Bone vitamins	vitamin D, calcitriol, IV calcium gluconate
Bone vitamins MoA	restores calcium/vitamin D levels
Anti-proliferative agents	methotrexate, azathioprine
Anti-proliferative agents MoA	inhibits enzymatic activity which reduces lymphocyte proliferation
Immunosuppressive agents	sulphasalazine, penicillamine
Disease-modifying biologics	infliximab, rituximab
Disease-modifying biologics MoA	infliximab - antagonist that binds to and inhibits TNF-alpha. rituximab - binds to CD20 and depletes B cells
Anticholinesterase for myasthenia gravis	pyridostigmine
Anticholinesterase for myasthenia gravis MoA	antagonist, inhibits acetylcholinesterase
Antibiotics: Beta-lactams: penicillins	flucloxacillin, benzylpenicillin, amoxicillin
Antibiotics: Beta lactams: carbapenems	meropenem
Antibiotics: Cephalosporins	ceftriaxone
Antibiotics: Lincosamides	clindamycin
Antibiotics: Macrolides	erythromycin
Antibiotics: Tetracyclines	tetracycline, doxycycline

Hint	Answer
Antibiotics: Fluoroquinolones	ciprofloxacin
Antibiotics: Anti-folate antibiotics	trimethoprim
Antibiotics: Beta-lactams: penicillins MoA	bacteriocidal, binds to penicillin binding proteins disrupting cell wall synthesis causing cell lysis
Antibiotics: Beta lactams: carbapenems MoA	bacteriocidal, binds to penicillin binding proteins disrupting cell wall synthesis causing cell lysis
Antibiotics: Cephalosporins MoA	bacteriocidal, binds to penicillin binding proteins disrupting cell wall synthesis causing cell lysis
Antibiotics: Lincosamides MoA	bacteriostatic, binds to 50S subunit of bacterial ribosome inhibiting bacterial protein synthesis causing reduced growth
Antibiotics: Macrolides MoA	bacteriostatic, binds to 50S subunit of bacterial ribosome inhibiting bacterial protein synthesis causing reduced growth
Antibiotics: Tetracyclines MoA	bacteriostatic, binds to 30S subunit of bacterial ribosome inhibiting bacterial protein synthesis causing reduced growth
Antibiotics: Fluoroquinolones MoA	bacteriostatic, inhibits DNA coiling causing reduced bacterial growth
Antibiotics: Anti-folate antibiotics MoA	bacteriostatic, inhibits bacterial folic acid synthesis which inhibits bacterial DNA synthesis reducing growth
Glucocorticosteroid for airway inflammation	beclometasone, prednisolone, hydrocortisone
Glucocorticosteroid for airway inflammation MoA	corticosteroid enters cell, binds and forms a complex with glucocorticoid receptor, then acts as a transcription factor enhancing expression of anti-inflammatory products and suppressing pro-inflammatory mediators
Antimuscarinics	ipratropium, tiotropium, glycopyrronium
Antimuscarinics MoA	antagonist binds to m2-muscarinic receptors, inhibits cholinergic activity of smooth muscle of airway leading to muscle relaxation
Beta-2 adrenergic agonists	salbutamol (short), salmeterol (long)
Beta-2 adrenergic agonists MoA	agonist, binds directly to beta-2 receptors activating adenylyl cyclase which converts ATP to cAMP which activates protein kinase A which acts on the myosin light chain driving Ca2+ from smooth muscle cells leading to dilation and airway muscle relaxation
Methylxanthines	theophylline, aminophylline
Methylxanthines MoA	antagonist, inhibits phosphodiesterase-4 which increases cAMP levels in cells which activates protein kinase A which acts on myosin light chain driving Ca2+ from smooth muscle cells leading to dilation and airway muscle relaxation
Leukotriene receptor antagonists	montelukast, zafirlukast
Leukotriene receptor antagonists MoA	antagonist binds to and inhibits CysLT1 receptors of eosinophils preventing binding of pro-inflammatory leukotrienes
Antacids	aluminium hydroxide and magnesium hydroxide, calcium carbonate and magnesium carbonate
Antacids MoA	gastric acid neutralisation
Alginates	sodium alginate with sodium bicarbonate and calcium carbonate
Alginates MoA	gastric acid neutralisation and formation of a viscous layer when in contact with water which sits on the surface of gastric contents and reduces reflux
Histamine antagonist	famotidine
Histamine antagonist MoA	antagonist inhibits h2-receptors
Proton pump inhibitors	omeprazole, lansoprazole
Proton pump inhibitors MoA	antagonist irreversibly binds to and inhibits H+/K+/ATPase enzyme in gastric parietal cells
Osmotic laxatives	macrogol, lactulose
Osmotic laxatives MoA	increases fluid uptake within GI lumen softening and increasing stool bulk which drives colonic distention and motility
Bulk laxatives	methylcellulose, ispaghula husk
Bulk laxatives MoA	increases water retention within intestinal lumen softening and increasing stool bulk which drives colonic distention and motility
Faecal softeners	docusate, arachis oil
Faecal softeners MoA	increases fat and water uptake into stool softening and increasing stool bulk which stimulates purgation and transit
Stimulant purgatives	bisacodyl, senna
Stimulant purgatives MoA	stimulates intestinal motility and purgation
Opioid anti-motility agents	codeine, loperamide
Opioid anti motility agents MoA	agonist binds to mu-opioid receptor in myenteric plexus reducing intestinal motility
Thyroid medications	levothyroxine, liothyronine
Thyroid medications MoA	activation of thyroid hormone receptors
Loop diuretics	furosemide
Loop diuretics MoA	antagonist inhibits Na+/K+/2A-� transporters in loop of henle
Thiazides	bendroflumethiazide, hydrochlorothiazide, indapamide, chlortalidone
Thiazides MoA	antagonist inhibits Na+/Ck- transporter in early distal tubule
Potassium sparing diuretics	spironolactone, eplerenone, amiloride
Potassium sparing diuretics MoA	antagonist inhibits mineralocorticoid receptors/sodium transport via ENaC channels
Alpha-1a adrenergic receptors (retention)	tamsulosin
Alpha-1a adrenergic receptors MoA	antagonist binds to and inhibits alpha-a1 adrenergic receptors which act on smooth muscle in the bladder and promotes urine passage
Antimuscarinic class (incontinence)	oxybutynin
Antimuscarinic class MoA	antagonist inhibits muscarinic acetylcholine receptors which relax bladder detrusor muscle
Combined oral contraceptives	desogestrel with ethinylestradiol
Combined oral contraceptives MoA	suppresses ovulation and reduces LH and FSH secretion
Progesterone only contraceptives	desogestrel, levonorgestrel
Progesterone only contraceptives MoA	suppresses ovulation and reduces LH and FSH secretion and alters endometrium
Emergency contraceptives	levonorgestrel, ulipristal
Emergency contraceptives MoA	suppresses ovulation and reduces LH and FSH secretion
Device/implants contraceptives	etonogestrel, levonorgestrel
Device/implants contraceptives MoA	suppresses ovulation and alters endometrium
HRT	estradiol, estradiol with noresthisterone, estradiol with medroxyprogesterone
HRT MoA	restores hormone levels and function
Menopausal osteoporosis	raloxifene
Menopausal osteoporosis MoA	binds to oestrogen receptors in bone preventing osteoporosis
Labour augmentation	oxytocin
Labour augmentation MoA	drives myometrial contractions
Essential nutrient for preterm labour	magnesium
Essential nutrient for preterm labour MoA	provides neuroprotection for preterm foetuses reducing risk of cerebral palsy
Labour induction	dinoprostone
Labour induction MoA	stimulates myometrial uterine contractions and cervical ripening
Labour analgesics	remifentanil, pethidine
Labour analgesics MoA	agonist binds to mu-opioid receptor suppressing pain transmission
Essential nutrient for pregnancy (neural tube development)	folic acid
Essential nutrient for pregnancy (neural tube development) MoA	foetal spinal and neural development, reduces risk of spina bifida
Essential nutrient for pregnancy	vitamin D
Essential nutrient for pregnancy MoA	foetal bone, kidney, neural and heart development

First submitted	May 16, 2023
Times taken	11
Average score	45.0%
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