Group —> MoA Flashcards
Antacids
Gastric Acid Neutralisation
Antacid + Alginate
Gastric Acid Neutralisation
H2 Receptor Antagonist
Blockade of gastric H2 histamine receptors
Proton Pump Inhibitor (PPI)
Blockade of Stomach Acid Transporters (H+ Pump)
Pancreatic Enzymes
Restoration of Pancreatic Enzymes
Bulk Laxatives
Polymers that aren’t broken down by normal digestion bulk up stool.
Water retained in the GI lumen, softening and increasing faecal bulk and promote increased motility.
Faecal Softner
Lower surface tension at oil-water interface allows water or fats to enter the stool and soften it.
Osmotic Laxative
Create an osmotic gradient which pulls water into the lumen of the colon leading to distensión of the colon and purgation.
Stimulant Laxatives
Stimulates rectal mucosa (myenteric plexus) resulting in mass movements.
Opioid Anti-Motility Agents
u-opioid receptor agonist in myenteric plexus blocking intestinal muscarinic receptors.
Loop Diuretics
Inhibits Na/K/2Cl transporter in the Loop of Henle which causes less water to be reabsorbed.
Thiazides
Decreases sodium and chloride reabsorption by inhibiting transporters.
Potassium Sparing Diuretics
Mineralocorticoid receptor blockade prevents production of co transporters leading to decreased K secretion and decreased Na reabsorption. (spironolactone, eplerenone)
Blockade of ENaC leads to decreased sodium reabsorption (amiloride)
Osmotic Diuretic
Increased plasma osmolarity causing water to leave cells and enter blood stream.
Carbonic Anhydrase Inhibitor
Inhibiting carbonic anhydrase prevents the reabsoprtion of Bicarbonate and therefore sodium and water,
H2CO3 reaction in PCT.
Reduces aqueous humour volume
ACEi
Inhibits conversion of Angiotensin 1 to angiotensin 2. Therefore blocking vasoconstriction.
ARBs
Blocks angiotensin 2 receptors and so blocks the renin-angiotensin system.
RAAS aim is to increase BP normally.
Neprilysin Inhibitor
Inhibtion of Natriuretic Peptide breakdown means increased concentration and so increased diuresis.
Given with ARBs because they prevent vasoconstriction?
Beta Blockers
Antagonism of beta adrenergic receptors leads to negative inotropy and chronotropy.
Alpha Blockers
Antagonism of Alpha adrenergic receptors leads to Vasodilation and a decrease in TPR.
CCB
Antagonism of calcium channels leads to blockage of vascular smooth muscle contraction (decreased vasoconstriction)
Nitrates
Nitric oxide release leads to smooth muscle relaxation and vasodilation
Sympathomimetics
Adrenergic stimulation leads to increased inotropy
Antiplatelets
Inhibition of Thromboxane synthesis (aspirin)
Inhibition of platelet activation by Adenosine Diphosphate (ADP) (clopidogrel)
Anticoagulant - Coumarin
Inhibition of Vitamin K epoxide reductase leads to decreased clotting.
Anticoagulant - Direct Thrombin Inhibitor
Inhibition of Thrombin
Anticoagulants - Direct Factor Xa inhibitors
Inhibition of Factor Xa in the coagulation cascade
Anticoagulants - Heparins
Inactivation of thrombin and factor Xa via complexing antithrombin III
Thromoblytics/Fibrinolytics
Activation of plasminogen for proteolytic breakdown of thrombus fibrin
HMG-CoA Reductase inhibitors
Inhibition of mavelonate pathway required for cholesterol synthesis
Class 1 Antiarrythmic
Voltage gated sodium channel blockage
Prolongs QT interval leading to increased QRS duration. Decrease chance of arrythmia
Class 2 Antiarrythmic
Beta adrenergic receptor blockage
reduction in adrenergic effects on rate and inotropy
Class 3 Antiarrythmic
Potassium channel blockage.
Evidence of beta blocker and calcium channel blocker properties
Prolongs QT interval
Class 4 Antiarrythmic
Cardiac calcium channel blockade
Reduction of action potential and cardiac output.
Cardiac Glycosides
Reduces conductivity of AV node.
Decreased HR
Adenosine
Activates adenosine receptors
Causes hyperpolarisation
Slows conduction through AV node.
Antimuscarinic (Anticholinergic)
Blockage of vagal muscarinic ACh receptors
Increases HR
Magnesium
Unclear
Possibly alters Na K Ca ion balance via channels and transporters.
Beta-2-Adrenergic Agonist
Dilation of bronchial smooth muscle
Antimuscarinics
Blocks muscarinic receptors to promote bronchial dilation
Methylxanthines
Bronchodilator by increasing cAMP in smooth muscle
Glucocorticoids
Reduction of inflammation and mucus production
Leukotriene Antagonist
Blockage of leukotriene receptors to reduce inflammation.
Mucolytic
Synthetic DNAse 1 - breakdown of extracellular DNA to reduce sputum viscosity. (dornase alfa)
Cleavage of mucous glycoproteins to reduce viscosity (Carbocisteine)
Dopaminergics
Increased dopamine synthesis and dopaminergic function. (Basal Ganglia)
Dopa-decarboxylase inhibitor
Stops breakdown of Levodopa in the periphery by inhibiting dopa-decarboxylase.
Monoamine Oxidase B Inhibitors (MAOI)
Inhibit the breakdown of dopamine
Catechol-O-methyl transferase inhibitor (COMT)
Blockade of dopamine precursor breakdown by inhibition of COMT.
Anticholinergics
Muscarinic cholinergic receptor antagonist.
Dopamine-depleting drugs
Blocks VMAT (vesicular monoamine transporter) preventing uptake of DA into vesicles.
Selective Serotonin reuptake inhibitors (SSRIs)
Inhibition of serotonin (5HT) reuptake pump in synaptic cleft
Reversible inhibitor of monoamine oxidase type A (RIMA)
Inhibits monoamine oxidase A, preferentially decreases breakdown of serotonin and noradrenaline
Tricylic Antidepressants (TCA)
Inhibition of noradrenaline and serotonin reuptake in synaptic cleft.
H1 antagonist
M1 antagonist
Adrenergic Antagonist.
Atypical Antidepressants Venlafaxine and Reboxetine
Noradrenaline reuptake inhibitor
Atypical Antidepressant Buproprion
Noradrenaline and Dopamine reuptake inhibitor
Atypical Antidepressant Agomelatine
Melatonin agonist
Atypical Antidepressant Mirtazepine
Alpha-2-antagonist
Antipsychotic 1st Generation
Selective D2 dopamine receptor blockade
Antipsychotic 2nd Generation
Selective D2 doapmine receptor blockade
5-HT receptor blockade
Mood Stabiliser
Unclear - possible neuronal calcium channel blockade.
Cholinesterase Inhibitor
Inhibition of Acetylcholinesterase (reversible)
NMDA receptor antagonist
VD blocker of NDMA
Anxiolytics
GABA Positive Allosteric Modulator (PAM) (y-subunit) increase GABA receptor acitivity.
5HT partial Agonist (buspirone)
Non-Benzodiazepine Hypnotic
GABA Positive Allosteric Modulator (PAM) (y-subunit) increase GABA receptor acitivity. (y-subunit)
Anti-Epilepsy Drugs (AEDs)
Sodium channel blockers.
Ethosuximide = Calcium channel blocker
Slows down action potentials to make seizures less likely.
Benzodiazepines
GABA positive allosteric modulator (PAM) (y-subunit) causing increased activity of GABA receptors to enhance GABA effects.
Benzodiazepine Antagonist
Antagonises GABA receptors and signalling.
Barbiturates
GABA Positive Allosteric Modulate (B-subunit) –> enhanced effect of GABA.
Weak Analgesic / Antipyretic
Unclear - Possible COX inhibitor in CNS.
NSAID
Non-selective COX inhibitors, blockade of prostaglandin (healing proteins) synthesis
COX2-selective NSAIDs
COX-2 inhibition, localised prostaglandin (healing proteins) blockade
Weak Opioid Analgesics
Stimulation of analgesic opioid receptors
Strong Opioid Analgesics
Stimulation of analgesic opioid receptors
Partial/mixed agonist opioid analgesics
Modulation of analgesic opioid receptors (u and k)
Opioid Antagonist
Opioid Receptor Antagonist
Opioid Addiction Management
Narcotic opioid replacement, opioid receptor agonist/modulator
Drugs for Neuropathic Pain
Voltage dependant calcium channel antagonist (gabapentin, pregabalin)
Tri-cyclic antidepressant (amitryptiline)
Inhaled Analgesics
Unclear Mechanism
General Anaesthetics
Unclear - possible enhancement of GABA function
Ketamine - NMDA receptor blockade.
Local Anaesthetic
Voltage-gated sodium channel blockade
Neuromuscular Blockers
Competitive antagonist at ACh receptor
Initially depolarisations and desensitisation of ACh receptor
Drugs for reversing neuromuscular block
Oligosaccharide that forms a complex with NMBs removing them from Neuromuscular Junction (Sugammadex)
Peripheral Acetylcholinesterase Inhibitor (Neostigmine)
Muscle Relaxants and Sedatives
BDZ - GABA Positive allosteric modulator to increase GABA receptor activity. (Temazepam)
Alpha-2-agonists inhibit sympathetic activity (Dexmedetomidine)
opiod receptors lead to muscle relaxation and sedation (fentanils)
Anti-Emetic Cyclizine
Histamine H1 receptor blockade
Anti-Emetic Domperidone and Metoclopramide
Dopamine D2 receptor blockade in the Chemoreceptor trigger zone
Penicillins (Beta Lactam)
Beta-Lactam: Inhibition of bacterial cell wall synthesis.
Carbapenems (Beta Lactam)
Meropenem
Beta-Lactam: Inhibition of bacterial cell wall synthesis.
Cephalosporins (Beta Lactam)
Ceftriaxone
Beta-Lactam: Inhibition of bacterial cell wall synthesis
Antifolate Antibiotic
Trimethoprim
Inhibition of dihydrofolate reductase
Fluroquinolones
Ciprofloxacin
Inhibition of bacterial DNA gyrase
Marcolide Antibiotic
Erthromycin, Azithromycin
Inhibition of bacterial protein synthesis
Tetracycline Antibiotic
Doxycycline
Inhibition of bacterial protein synthesis
Nitrofuran
Nitrofurantoin
Bacterial DNA interference
Aminoglycoside
Gentamycin
Inhibition of bacterial protein synthesis
Glycopeptide
Vancomycin
Inhibition of cell wall synthesis in Gram-Positive Bacteria
Nitroimidazole (anti-anaerobe)
Metronidazole
Inhibition of bacterial DNA synthesis
Anti-TB Drugs
Isoniazid, Ethambutol
- Inhibition of mycobacterium cell wall synthesis
Rifampicin
- Inhibition of mycobacterial RNA synthesis
Therapeutic Cytokines
Interferon Alpha
- Activation of antiviral intracellular and immune responses
DNA Polymerase Inhibitors
Aciclovir, Ganciclovir
- Virus Replication Blockade
Neuraminidase Inhibitors
Oseltamivir
- Prevention of viral budding and infectivity
Nucleoside Analogues
Ribavarin
- Disrupts viral RNA synthesis
Nucleoside reverse transcriptase inhibitors (NRTI)
Tenofovir
- Blockade of viral reverse transcriptase function for viral genetic replication.
Non-nucleoside reverse transcriptase inhibitors (NNRTI)
Efavirenz
- Blockade of viral reverse transcriptase function for viral genetic replication.
Viral Protease Inhibitor
Lopinavir
- Blockade of viral protease required for virus particle assembly
Integrase Inhibitor
Dolutegravir
- Disrupts integration of HIV genome into host chromosomes.
Viral Fusion Inhibitors
Enfuvirtide
- Blockade of virus fusion to target cell membrane
Chemokine receptor/CCR5 Antagonist
Maraviroc
- Blockade of HIV binding to co-factor for cell entry
Triazole anti-fungal agent
Fluconazole
- Disruption of fungal membrane function.
Blood glucose-reducing hormones
Insulin
- Stimulation of glucose uptake by cells (GLUT-2)
Oral Biguanide
Metformin
- Increases insulin sensitivity
- Inhibits hepatic gluconeogenesis
Sulphonylurea
Gliclazide
- Stimulates pancreatic insulin secretion
Thiazolidinedione
Pioglitazone
- Increases insulin sensitivity in muscle and adipose tissue
Glucagon-like peptide-1 receptor (GLP-1) agonist
Exenatide
- Incretin (decreased blood glucose) analogue - improves glucose control.
- Acts on the glucagon receptors to increase cell uptake of glucose.
Dipeptidyl peptidase-4 (DPP-4) inhibitor
Sitagliptin
- Reduces inactivation of incretins (hormones that reduce blood glucose)
Lipase Inhibitor
Orlistat
- Inhibition of GI uptake of dietary fat
Thyroid Hormones
T4, T3
- Sythetic hormones that act on thyroid hormone receptors.
Antifolate Antiproliferative
Methotrexate
- Inhibition of dihydrofolate reductase and DNA synthesis for lymphocyte proliferation (decreased immune response)
Antimetabolite Immunosuppressant
Azathioprine
- Unclear, possible inhibition of DNA synthesis and lymphocyte proliferation (decreased immune response)
Cytokine Modulators
Adalimumab, Etanercept, Infliximab
- TNF-alpha blockade (decreased immune response)
Aminosalicylates
Sulfasalazine, Mesalazine
- Unclear, possible COX inhibition
- Possible free radical scavenging, T cell suppression.
Oral combination pill contraceptives
Mimics ovulation, reduces LH and FSH
Oral mini-pill contraceptives Progestogen-only
Mimics ovulation, reduces LH and FSH, endometrial changes, thickening of cervical mucous
Implants/Injectable Contraceptives
Mimics ovulation, reduces LH and FSH
Hormone Replacement Therapy (HRT)
Restores decreased hormone level and function via oestrogen to lessen symptoms of the menopause
Progesterone is added to prevent the thickening of the endometrium via oestrogen, and so reduce the cancer risk
Induction of Labour
Prostaglandin E2 - stimulates cervical ripening
Augmentation Agents
Stimulation of uterine contractions
Antiprogestogen/Prostaglandin for medical termination
Steroidal antiprogestogen in combination with synthetic prostaglandin
- Mifepristone blocks progesterone –> thinning of the uterine lining and preventing embryo implantation
- Mesoprostol, synthetic prostaglandin, causes the uterus to contract and expel the embryo through the vagina
Antifibrinolytic for Menorrhagia
Inhibits fibrin clot breakdown by plasmin
NSAID (for dysmenorrhoea)
Inhibition of Prostaglandin Synthesis
Alpha-1-blocker
- Tamsulosin
Smooth muscle relaxant acting on bladder neck
Urinary Antispasmodic (Antimuscarinic)
Blockade of acetylcholine receptors leading to bladder smooth muscle relaxation
Beta-3-Agonist
- Mirabegron
Stimulation of Beta-3 adrenergic receptors, leading to detrusor smooth muscle relaxation.
Anti-Androgen
- Finasteride
Inhibition of synthesis of dihydrotestosterone which leads to prostatic growth.
Anti-Histamine
H1 histamine receptor blockade
Glucocorticoids
Intracellular transcription factor interactions, gene expression
Calcineurin Inhibitors
- Cyclosporin
- Tacrolimus
Inhibition of T cell signalling
Classical Alkylating Agent
- Cyclophosphamide
DNA crosslinking that changes the conformation of DNA strands
Taxanes
Inhibition of microtubule assembly in mitotic spindle
Vinca Alkaloids
Inhibition of microtubule assembly in mitotic spindle
Antifolates
- Methotrexate
Inhibition of dihydrofolate reductase and DNA synthesis
Antipyramidines
Inhibition of RNA and DNA synthesis
Antipurines
Inhibition of RNA and DNA synthesis
Anthracycline Antibiotics
- Doxorubicin
DNA intercalation
Inhibition of RNA and DNA synthesis
Antineoplastic Monoclonal antibodies
- Trastuzumab
Targetting of cells overexpressing Human Epidermal Growth Factor Receptor-2 (HER-2) for tumour reduction and destruction
Antineoplastic Monoclonal Antibodies
- Rituximab
Targeted destruction of CD20+ B cells
Antineoplastic Monoclonal Antibodies
- Nivolumab
Stimulation of anti-tumour responses via blocking PD-1
Immunomodulator
- Lenolidamide
Stimulation of T cell responses
Selective oestrogen receptor modulator (SERM)
- Tamoxifen
Inhibition of oestrogen receptor function and cell proliferation in the breast
Luteinising hormone releasing hormone (LHRH) receptor agonist
- Goserelin
Synthetic analogue of LHRH
Activates LHRH receptor funcction leading to sustained reduction in testosterone.
Therapeutic Hormones for Calcium Homeostasis
- Calcitonin
Inhibits mobilisation of calcium from bones
Bisphosphonates
Inhibits osteoclast function and bone resorption via osteoclast apoptosis
Drugs for Hypocalcaemia
Restoration of calcium levels and metabolism
Vitamin D
Restores Vitamin D levels
Selective oestrogen receptor modulator (SERM) for Osteoporosis
- Raloxifene
Stimulation of oestrogen function in bone
Denosumab
Inhibition of osteoclast function and bone resorption
Ferrous Sulphate
Iron Provision
Folic Acid
Supports nucleic acid synthesis
Vitamin B12 (parenteral)
Enzyme Co-Factor
N-Acetylcysteine Paracetamol Antidote
Restoring and maintaining hepatic intracellular glutathione required for paracetamol detoxification
Chlordiazepoxide BDZ for alcohol withdrawal
Potentiation of GABAa receptor agonist
Clomethiazole Non-BDZ hypnotic for alcohol withdrawal
GABA mimetic - GABAa receptor agonist
Acamprostate for treatment of alcohol abuse
GABA mimetic - GABAa receptor agonist, possible NMDA receptor antagnosit
Aliskiren (direct renin inhibitor)
Direct inhibition of renin enzymatic function and of angiotensin 1 generation
Doxazosin (alpha 1 adrenergic antagonist)
Vasodilator, decreases TPR
Clonidine (alpha 2 adrenergic agonist)
Stimulation of alpha 2 receptors driving vasodilation
Ivabradine
Inhibition of cardiac l(funny) current in the SA node
Antiplatelets Prasugrel and Ticagrelor
Purinergic receptor blockers
Lithium Carbonate
Neuronal Calcium channel blockage
Sumatriptan (Migraine treatment)
Stimulation of 5-HT receptors
Topiramate (Migraine Prophylaxis)
Blockade of voltage-gated sodium and calcium channels
Anti-emetic Ondansetron
Serotonin type 3 (5-HT3) receptor blockade
Lincosamide
Clindamycin
Inhibition of bacterial protein synthesis
Viral Entry inhibitor (Maraviroc)
Blockade of HIV binding to co-factor for cell entry
Anti-helmintic (Mebendazole)
Disruption of microtubule assembly in helminth cells
Pyrethrine anti-infestation (Permethrin)
Inhibits invertebrate neural sodium channels, causing paralysis of pests
GLP-1 Agonist
Incretin analogue - improves glucose control
SGLT-2 inhibitor
Blockade of renal glucose-sodium co-transporter
PPAR-alpha activator (Fenofibrate)
Activation of PPAR-alpha transcription factor.
Vasopressin Analogue (Desmopressin)
Agonist for ADH receptors
Dopamine receptor agonists for endocrinology
Stimulation of D2 receptors in the pituitary gland for prolactin secretion
Anti-thyroid drugs
Inhibition of Thyroid peroxidase (TPO) enzyme
Thiopurine Antiproliferative
Inhibitor of purine synthesis- possible inhibition of DNA synthesis and lymphocyte proliferation
Antimetabolite Antiproliferative Leflunomide
Inhibitor of pyrimidine synthesis, reducing DNA and RNA synthesis and lymphocyte proliferation
Anti Gout agent Colchicine
Possible inhibition of inflammatory cell motility
Xanthase oxidase inhibitor
Inhibition of uric acid synthesis
NSAID for gout Indometacin
COX enzyme inhibition
Progesterone receptor modulator Ulipristal
Stimulation of progesterone-like responses in pituitary and endometrium
Inosine monophosphate dehydrogenase inhibitor (Mycophenolate)
Inhibition of purine synthesis; anti-proliferative
Synthetic G-CSF (Filgrastim)
Stimulation of neutrophil production in bone marrow
Hydroxocobalamin (paraenteral)
Vitamin B12 - Enzyme co-factor