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Inflammation
Histamine, 5-HT, pain killers, corticosteroids, asthma, COPD, autoimmune disease
| Term | Definition |
|---|---|
| Abatacept MoDA | Biological DMARD for RA -> synthetic fusion protein of costimulatory CTLA4 (cytotoxic T-lymphocyte protein 4) and human IgG1 Fc fragment -> binds to APC CD80/86 -> interferes w/ interaction w/ T cell CD28 |
| Abatacept effect | Prevent T cell co-stimulation -> dampen immune response against RA |
| Acarbose MoDA | Alpha-glucosidase inhibitor for T2DM -> slows GI tract breakdown of starch/disccharides into glucose -> reduce amount of glucose entering bloodstream |
| Acarbose effects and side effects | T2DM treatment -> alpha glucosidase inhibitor in GI tract -> aids weight loss (less calories), side effects -> flatulence/diarrhoea |
| Acetylcysteine MoDA | Treat paracetamol overdose -> increase hepatic glutathione production -> conjugates to NAPQI and prevent oxidisation of cellular protein thiol groups -> prevent liver damage |
| Adalimumab MoDA | Biological DMARD for RA -> human monoclonal anti-TNF alpha Ab -> sequester high levels of TNF alpha -> reduce inflammation |
| Anti-TNF alpha therapy side effects | Biological DMARD for RA -> allergic reactions, bone marrow suppression, increased infection susceptibility (high risk for TB/HBV reactivation), risk of MS |
| Adrenaline MoDA in inflammation and effects | Treat anaphylaxis -> administered intramuscularly ->non-selective AR agonist -> counteract systemic vasodilation/reduction in tissue perfusion (alpha 1), relieve bronchospasm (beta 2) |
| Alemtuzumab MoDA and effects | Immunosuppressant -> treat chronic lymphocytic leukaemia, T cell lymphoma, MS -> humanised mAb -> binds to CD52 Ag on mature lymphocytes -> target for destruction |
| Anakinra MoDA and effects | Recombinant IL-1 receptor antagonist for RA -> binds to IL-1R w/ higher affinity than IL-1 -> doesn't initiate receptor signalling -> dampen immune response |
| Arthrotec MoDA | Treat NSAID-induced ulceration -> combination of diclofenac (NSAID) and misoprostol (PGE1 analogue), also used as RA treatment |
| Aspirin binding | NSAID -> acetylates Ser530 -> irreversibly inactivates COX (long-lasting) |
| Aspirin MoDA on platelets | Express COX-1/TX synthase -> TXA2 source (usually induces platelet aggregation/vasoconstriction) -> switches off TXA2 production for platelet lifetime (10 days) -> anti-thrombotic |
| Aspirin MoDA on endothelial cells | Endothelium produces PGI2 (normally inhibits platelet aggregation/vasodilation) -> aspirin-acetylated COX-1 replaced by newly synthesised protein (no side effects) in endothelial cells -> overall anti-thrombotic |
| Aspirin side effects | Reye's syndrome -> exclusively in children -> fatal hepatic encephalopathy -> aspirin treatment for viral symptoms, salicylism -> aspirin overdose |
| What happens with small aspirin doses in the context of salicylism? | Kreb's cycle inhibition -> uncouple skeletal muscle O2 phosphorylation -> increased O2 consumption/CO2 production -> stimulates peripheral/central chemoreceptors -> increased ventilatory rate -> respiratory alkalosis -> renal HCO3 excretion compensation |
| What happens with large aspirin doses in the context of salicylism? | Depressed respiratory centres -> accumulated CO2 -> reduced plasma HCO3 due to previous compensation -> combined w/ metabolic acidosis (accumulated acidic metabolites from disrupted CHO metabolism) -> fever/emesis -> coma/death |
| What is the treatment for salicylism? | Aspirin overdose -> administer fluids, HCO3 (enhance aspirin elimination), activated charcoal (adsorbs aspirin in GI tract), haemodialysis for severe cases |
| Azathioprine MoDA | Immunosuppressant -> prodrug for 6-mercaptopurine -> 6-methyl-TIMP (inhibits de novo purine synthesis) and 6-TGN (incorporated into cellular nucleic acids) -> inhibit nt/protein synthesis |
| Azathioprine effects | Treat autoimmune diseases (IBD/RA) -> inhibit cellular proliferation of rapidly proliferating active T/B cells -> prevent transplant rejection |
| Azathioprine side effects | 6-mercaptopurine prodrug -> GI disturbance, bone marrow depression, hepatotoxicity, common TPMT genetic polymorphism in Caucasian/African-Americans (low activity levels) -> increased generation of 6-thioguanine nt analogues |
| Basiliximab MoDA and effect | Immunosuppressant -> chimeric mAb against IL-2 CD25 alpha subunit (receptor antagonist) -> IL-2 receptors upregulated on activated T/B cells -> decreases incidence/severity of acute rejection following transplant |
| Belatacept MoDA and effect | Same as abatacept -> immunosuppressant -> synthetic fusion protein of costimulatory CTLA4 and human IgG1 Fc fragment -> binds to APC CD80/86 -> interferes w/ T cell CD28 interaction -> prevent T cell costimulation -> prevent graft transplant rejection |
| Belimumab MoDA and effect | Treat SLE -> sequesters B-lymphocyte stimulator (BLyS) -> prevents B cell survival/differentiation/Ab production |
| Beclomethasone MoDA and effect | Regular inhaled corticosteroid -> binds to glucocorticoid receptor -> upregulates anti-inflammatory genes -> treat asthma |
| Beclomethasone disadvantages | Treat asthma -> corticosteroid -> inhaled (risk of oral candidiasis infection), slow onset (genomic MoDA) -> not useful for acute bronchoconstriction |
| Betamethasone MoDA and effect | Corticosteroid -> IV administration -> unknown mechanism -> onset of 10 minutes not explainable by genomic effects -> reduce nasal irritation from allergic rhinitis patient pollen suspension |
| Botulinum toxin A pathology MoDA and effect | Cleaves peripheral neuron synaptobrevin -> impaired exocytosis of excitatory ACh -> flaccid paralysis |
| Botulinum toxin A clinical MoDA and effect | Only advised in chronic migraine patients (headaches for >15 days / month) -> intramuscular injection to head/neck -> cleave synaptobrevin -> decreased nociceptor neurotransmitter release |
| Capsaicin MoDA and effect | Treat OA -> topical cream applied 3-4 times a day -> activate nociceptor TRPV1 -> constant agonist presence -> depolarising nociceptor block -> nociceptor degeneration -> pain relief |
| Catumaxomab MoDA and effect | Treat ascites in cancer patients -> rat/mouse hybrid mAb (bi-specific) -> Fab1 binds tumour epithelial cell adhesion molecule, Fab2 binds T cell CD3, Fc binds macrophage/NK cell/DC -> reduces tumour burden -> withdrawn in 2017 |
| Ciclosporin A (CsA) MoDA and effect | Immunosuppressant -> cyclic 11 aa peptide ->binds to cytoplasmic cyclophilin (CpN) -> complex binds/inhibits CaN -> prevent NF-AT dephosphorylation -> prevent translocation to nucleus -> inhibit IL-2 transcription -> suppress transplant organ rejection |
| Clarithromycin uses | Macrolide Abx that eradicates H pylori -> treat peptic ulcers |
| Cyclophosphamide MoDA and effect | Immunosuppressant -> prodrug converted by CYP450 -> 2 alkylating groups to crosslink DNA G via N7 groups -> substitutes A-T for G-C -> defective DNA replication -> guanine excision/chain breakage -> kill proliferating B/T cells |
| Cyclophosphamide side effects | Bone marrow depression, potential infertility, bladder irritation, cancer -> lymphoma (acrolein metabolite activates TRPA1 in bladder innervating nociceptors) |
| Dapagliflozin MoDA and effects | Treat T2DM -> inhibit SGLT2 in kidney PCT -> increase urinary glucose loss -> calorie loss -> weight loss |
| Dapagliflozin side effects and contraindications | Inhibit PCT SGLT2 -> increased UTI/genital infections, increased urinary frequency (polyuria), increased liver ketone production (ketoacidosis), contraindicated in patients w/ reduced renal function -> lower efficacy |
| Diclofenac MoDA and effect | NSAID for chronic RA -> inhibit COX enzymes by H-bonding to hydrophobic channel Arg120 -> prevent FA AA entrance -> pain relief |
| Domperidone MoDA and effect | Treat emesis -> D2 receptor anagonists in CTZ (some in GI tract) more peripherally selective than metoclopramide (less acute dystonia) -> inhibits chemoreceptor trigger zone (CTZ) in brain medulla -> no signals to vomiting centre |
| Erenumab MoDA and effect | Treat migraine -> mAb against CGRP receptor -> CGRP levels elevated in EJV during migraine attack and can induce headaches/migrain-like attacks in migraineurs |
| Etanercept MoDA and effect | Biological DMARD against RA -> fusion protein of soluble TNF-alpha receptor and IgG1 Fc -> sequester high levels of TNF-alpha -> inhibit immune response activation |
| Etoricoxib MoDA and effect | COX-2 selective NSAID -> treat OA/RA -> inhibit COX enzymes by H-bonding to hydrophobic channel Arg120 -> prevent FA AA entrance -> pain relief w/ lower risk of GI bleeding |
| Etoricoxib side effects and contraindications | Some COX-2 constitutively expressed in endothelial/vascular smooth muscle cells -> inhibition decreases PGI2 (vasoconstriction/platelet aggregation) and increases endogenous eNOS inhibitors (vasoconstriction) -> increased myocardial risk |
| Exenatide MoDA and effect | Treat T2DM -> synthetic version of exendin-4 -> mimic effect of GLP-1 but longer acting -> subQ injection twice daily (more stable than GLP-1) -> simulate insulin release/inhibit glucagon release -> acts in amygdala to reduce appetite/body weight |
| Fremanezumab MoDA and effect | Treat migraine -> mAb against CGRP -> CGRP levels elevated in EJV during migraine attack and can induce headaches/migraine-like attacks in migraineurs |
| Fexofenadine MoDA and effect | 3rd generation antihistamine -> activated form of 2nd gen terfenadine (metabolised by CYP450 3A4) -> H1-receptor antagonist -> non-drowsy (can't cross BBB), lack cardiac side effects -> treat hay fever, allergy, urticaria (hives) |
| Formoterol MoDA and effect | Treat histamine pathophysiology -> long acting beta2-AR agonists -> long lipophilic tail incorporated into PM (drug reservoir) -> binds to extra binding site on beta2-AR -> raise cAMP -> inhibit mast cell degranulation -> bronchodilation -> treat asthma |
| Glargine MoDA and effect | Long-acting insulin analogue -> treat T1DM -> w/ aa changes to A/B chains (isolectric point is more neutral pH) -> forms microprecipitate of stable hexamers/higher aggregation -> retard/prolong absorption -> onset 2-4 hrs, duration 20-24 hrs |
| Glibenclamide/glipizide MoDA and effect | Treat T2DM -> sulfonylureas -> bind to pancreatic beta cell K-ATP channel SUR1 subunit -> close channel -> trigger depolarisation -> Ca2+ influx -> insulin release |
| Glibenclamide/glipizide advantages/disadvantages | SU drugs -> well absorbed, peak plasma [ ] w/in few hours, duration 24 hrs, specificity for pancreatic SUR1 (cardiac SUR2A), only beneficial w/ intact beta cells, can evoke hypoglycaemia, can increase appetite (weight gain) |
| What are the different metabolism pathways of sulfonylurea compounds? | Glipizide -> metabolised in liver to inactive products and excreted in urine, glibenclamide -> converted to active products in liver before urinary excretion -> potentiated effects in patients w/ renal insufficiency |
| What are contraindications of sulfonylurea compounds? | Treat T2DM -> can cross placenta/enter breast milk -> contraindicated in pregnant/breastfeeding mothers |
| Hydrocortisone MoDA and effect | Corticosteroid -> immunosuppressant -> inhibit neutrophil degranulation -> anti-inflammatory -> decrease circulating leucocytes |
| Hydroxychloroquine MoDA and effect | Biological DMARD against RA -> lipophilic weak base -> accumulates in cytoplasmic acidic vesicles -> reduce macrophage Ag presentation/neutrophil ROS generation |
| Ibuprofen MoDA and effect | Non-selective COX inhibitor -> small -> can enter both hydrophobic channels |
| Imatinib MoDA and effect | Antihistamine -> histamine receptor antagonists -> Tyr K inhibitor -> inhibit mast cell degranulation -> only efficacious in patients w/out D816V c-Kit mutation (can't bind to mutated constitutive Tyr K) |
| Icatibant MoDA and effect | Treat hereditary angiooedema from mutation in C1-INH gene leading to xcs bradykinin (severe swelling) -> B2 (bradykinin) antagonist -> prevent bradykinin downstream signalling effects |
| Indacaterol MoDA and effect | Long-acting beta 2 antagonists -> treat COPD -> stimulate bronchodilation |
| Infliximab MoDA and effect | Biological DMARD against RA -> chimeric monoclonal anti-TNF alpha Ab -> sequester high levels of TNF alpha -> reduce removal of tight junctions btwn vascular epithelium and increasing vascular permeability |
| Insulin actrapid MoDA and effect | Short-acting insulin analogue -> treat T1DM -> 30-60 min onset, 8-10 hr duration |
| Insulin lispro MoDA and effect | Fast-acting insulin analogue -> treat T1DM -> swapping Lys residue for Pro towards insulin B chain C-terminus -> reduce dimer/hexamer formation -> larger amount of active monomeric insulin after injection -> 15 min onset, 4-6 hr duration |
| Ipratropium MoDA and effect | Non-selective muscarinic antagonist -> inhibit M3 on bronchial smooth muscle -> bronchodilation -> short-acting -> treat COPD |
| Lasmiditan MoDA and effect | Non-triptan 5-HT 1F agonist -> more potent at 1F receptors than 1B/D receptors (no vasoconstriction) -> highly lipophilic (readiliy crosses BBB) -> inhibit nociceptor activity/CGRP release -> treat migraine |
| Leflunomide MoDA and effect | Treat RA -> prodrug converted to active teriflunomide -> inhibit dihydroorotate deHase (pyrimidine synthesis) -> inhibits DNA/RNA synthesis in rapidly dividing B/T cells -> dampen immune response |
| Loratadine MoDA and effect | 3rd generation anti-histamine -> non-drowsy (doesn't cross BBB), no cardiac side effects (doesn't inhibit cardiac Kv11.1 for repolarisation) -> treat hay fever, allergy, urticaria |
| Montelukast MoDA and effect | Treat asthma -> CysLt1 receptor antagonist -> induce bronchodilation |
| Mepyramine MoDA and effect | 1st generation anti-histamine -> H1 receptor antagonist -> causes drowsiness (permeates BBB) -> topical cream for inset bites, reduce cold/flu symptoms while sleeping |
| Metformin MoDA and effect and contraindications | Treat T2DM -> activates AMPK -> decrease hepatic gluconeogenesis genes -> increase glucose uptake, decrease intestinal CHO absorption, decreased appetite -> inhibit hepatic lactate uptake (contraindicated in patients w/ renal dysfunction -> acidosis) |
| Methotrexate MoDA and effect and side effects | DMARD against RA -> inhibits DHFR, competes w/ folic acid transport into cells -> lower tetrahydrofolate production for purine/thymidylate synthesis -> antiproliferative -> reduce immune response -> bone marrow suppression, GI disturbance |
| Metoclopramide MoDA and effect and side effects | Treat emesis -> D2 receptor antagonists -> primarily in CTZ but also some in GI tract -> inhibit signals to vomiting centre -> can affect DA signalling in brain and cause acute dystonia |
| Misoprostol MoDA and effect | Treat peptic ulcers -> PGE1 analogue that overrides inhibition of PGE synthesis from NSAIDs and prevents xcs gastric acid secretion from causing peptic ulcer formation -> coadministered w/ NSAIDs |
| Muromonab-CD3 MoDA and effect | Anti-inflammatory -> murine mAb that targets CD3 (component of TCR) -> clears TCR and invokes T cell apoptosis -> reduce acute transplant rejection |
| Mycophenolic acid MoDA and effect | Immunosuppressant -> inhibit IMPDH (de novo guanosine synthesis) -> antiproliferative for activated B/T cells -> diminish transplant rejection/treat autoimmune diseases (myasthenia gravis) |
| Naproxen MoDA and effect | NSAID treat RA -> nonselective COX inhibitor -> reduce FA AA entrance for PGE synthesis -> lower cardiovascular risk than diclofenac |
| Naratriptan MoDA and effect | Treat migraine -> 5-HT 1B/D/F agonist -> 1B vasoconstriction, 1D/F inhibit nociceptors -> crosses BBB, long duration of action, fewer cardiac side effects |
| NPH insulin MoDA and effect | IM-acting insulin analogue -> treat T1DM -> suspension of protamine polypeptide/insulin -> forms relatively insoluble crystals (slow absorption) -> 2-4 hr onset, 12-18 hr duration |
| Omalizumab MoDA and effect | Treat severe asthma -> binds to IgE C eta3 region -> prevent heavy chain binding to Fc etaRI -> reduce mast cell Fc eta RI expression -> inhibit allergen-induced mast cell degranulation |
| Omeprazole MoDA and effect | Treat peptic ulcers -> proton pump inhibitor -> covalent/irreversible bonds w/ H+/K+ pump -> override inhibition of PGE synthesis from NSAIDs and prevents xcs gastric acid secretion from causing peptic ulcer formation -> coadministered w/ NSAIDs |
| Ondansetron MoDA and effect | Treat emesis -> 5-HT3 antagonist -> treat chemotherapy-induced emesis (CTZ 5-HT3), treat post-surgery emesis (anaesthesia) |
| Paracetamol MoDA and effect | Non-NSAID -> COX-1/2 inhibitor but poor anti-inflammatory -> good antipyretic/analgesic properties |
| What can cause paracetamol toxicity? | Saturated hepatic conjugation enzymes -> toxic NAPQI metabolite not conjugated to GSH -> oxidise thiol groups of cellular proteins -> hepato/renal toxicity -> liver failure -> death |
| How to treat paracetamol toxicity? | Xcs NAPQI -> acetylcysteine -> increase hepatic GSH production -> conjugate to NAPQI and prevent liver damage |
| Pioglitazone MoDA and effect and side effects | Treat T2DM -> activates PPAR gamma in adipose tissue/liver/muscle -> increase lipogenesis, increase tissue glucose/FA uptake, increase GLUT 4 transcription -> enhances amiloride-sensitive Na+ reabsorption (K+ sparing diuretic) -> fluid retention |
| Prednisolone MoDA and effect | Artificial steroid treat RA -> decrease IL-2 transcription (inhibit Th cell proliferation), decrease IL-1/TNF-alpha transcription (inhibit pro-inflammatory response) -> locally injected into inflamed joint |
| Proglumide MoDA and effect | Treat gastric acid secretion -> CCK2 receptor antagonist -> reduce ECL histamine secretion -> reduce parietal cell H+ pump activity |
| Propranolol MoDA and effect and contraindications | Non-selective beta receptor antagonist -> treat migraine -> prevent extracerebral vasodilation -> also act on central ACh system -> contraindicated in asthmatics (bronchospasm) |
| Ranitidine MoDA and effect | Treat peptic ulcers -> 1st gen H2 antagonist -> reduce parietal cell H+ pump activity -> can inhibit CYP450 -> 3A4 isoform important for many prodrugs |
| Repaglinide MoDA and effect | Treat T2DM -> bind to SUR1 and inhibit K-ATP -> no K+ efflux -> depolarisation -> Ca2+ influx -> insulin vesicle exocytosis -> taken before meal to reduce hypoglycaemia |
| Rituximab MoDA and effect and side effect | Treat RA -> binds B cell CD20 -> prevents B cell differentiation into plasma cell, provides binding site for NK cell ADCC -> increased risk of progressive multifocal leucoencephalopathy (reactivation of John Cunningham virus) |
| Roflumilast MoDA and effect | Treat COPD -> PDE IV specific inhibitor -> expressed in neutrophils, T cells, macrophages -> reduce immune response and prevent chronic inflammation |
| Salbutamol MoDA and effect | Treat asthma -> short-acting beta2 agonist -> induce bronchodilation, inhibit mast cell degranulation -> 20 min onset, 3-5 hr duration |
| Sirolimus MoDA and effect | Rapamycin -> immunosuppressant -> binds to FKBP -> binds/inhibits mammalian mTOR1 -> Ser/ThrK for cell cycle progression/protein synthesis -> decreased T cell activation/proliferation -> prevent transplant rejection |
| Sitagliptin MoDA and effect | Treat T2DM -> inhibit DDP4 (metabolises incretins that decrease BGC) -> prevent GLP-1/GIP degradation |
| Sodium cromoglycate MoDA and effect | Treat histamine pathophysiology -> inhibit mast cell degranulation, inhibit inward Cl- conductance -> not -ve enough to sustain Ca2+ influx -> reduce mast cell histamine release -> treat hay fever (eye drops), treat asthma |
| Sulfasalazine MoDA and effect | Treat RA -> broken down by colonic bacteria -> 5-aminosalicylic acid scavenges neutrophil ROS -> inhibits ROS oxidative burst -> prevent oxidative damage |
| Sumatriptan MoDA and effect and contraindications | Treat migraines -> 5-HT 1B agonist -> vasoconstriction, 1D/F agonist -> inhibit nociceptor -> can cause peripheral vasoconstriction -> contraindicated in coronary disease |
| Tacrolimus MoDA and effect | Immunosuppressant -> binds to FKBP -> inhibits CaN -> NF-AT (nuclear factor of activated T cells) still phosphorylated -> retained in cytoplasm -> inhibit IL-2 synthesis -> suppress transplant organ rejection |
| Terfenadine MoDA and effect | 2nd gen antihistamine -> H1 receptor antagnoist -> pro-drug converted to fexofenadine -> cannot cross BBB (non-drowsy) but inhibits cardiac Kv11.1 for K+ efflux repolarisation -> long QT syndrome |
| Theophylline MoDA and effect | Treat asthma/COPD -> inhibits PDE -> raise cAMP -> inhibit mast cell degranulation -> prevent inflammation |
| Tiotropium MoDA and effect | Treat COPD -> long acting muscarinic antagonist -> inhibit M3 -> prevent PLC activation -> inhibit IP3 generation -> inhibit smooth muscle contraction |
| Tocilizumab MoDA and effect | Treat RA -> anti-IL-6 mAb -> reduce production of pro-inflammatory cytokine and inhibit production of CRP |
| Topiramate MoDA and effect | Treat migraine -> inhibit VGNaC and activate GABA-A receptors -> decrease attack frequency |
| Trastuzumab MoDA and effect | Herceptin -> humanised mAb -> treat HER2 breast cancer -> binds to truncated HER2 receptor and switches constitutive HER2 receptor off -> inhibit xcs mTOR/MAPK signalling -> decrease p27 -> cell cycle inhibition |
| Trastuzumab emtansine MoDA and effect | T-DM1 -> trastuzumab combined w/ maytansine (DM1) -> binds to HER2 -> internalised -> lysosomal degradation -> DM1 release -> binds to tubulin -> prevent polymerisation -> cytotoxicity, disrupt HER2 signallin , target tumour cells for ADCC |
| Vonoprazan MoDA and effect | Treat peptic ulcers -> proton pump inhibitor -> P-CAB potassium competitive acid blocker -> competes w/ K+ binding site on H+/K+ pump -> greater stability than omeprazole |
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