Drug examples for each lecture Flashcards
Biomarkers and drug targets drug examples (non-specific targets)
Lactulose (osmotic laxative)
Sodium thiosulphate (binds cyanide - reverses toxicity)
Potassium permanganate (antiseptic
Ferrous sulphate for anaemia
calcium/magnesium carbonates: antacids
Drug examples for VGICs
Benzocaine, lidocaine, procaine: Nav blocker: local anaesthetic. Lidocaine also used for arrhythmias.
Phenytoin and pregabalin blocks VGCCs for epilepsy.
Nifedipine blocks L-type VGCC in vascular SM
Verapamil acts on L-type VGCCs in cardiac muscle.
Diazoxide binds to SUR1 KATP channel, opens channel to hyperpolarise. Used for hypoglycaemia.
Nicorandil binds to SUR2 KATP channel, opening channel to hyperpolarise, used for angina.
Glibenclamide and tolbutamide induce insulin release for diabetes by inhibiting the KATP channels.
Aconitine activates while tetrodotoxin inhibits VGSC opening
Drug examples for LGICs
Piracetam PAM at AMPA for myoclonus.
Ketamine antagonist at NMDA for depression/anaesthesia (or memantine for dementia)
Ondansetron: 5-HT3 antagonist for chemo nausea
Atracurium/pancuronium blocks nAChR for neuromuscular blockade in surgery. agonists nicotine and varenicline for smoking cessation
GABAA PAM: benzos, barbiturates, testosterone, progesterone, ethanol, propofol. NAMs: penicillins, picrotoxin, DMCM (BZD site)
Elimination drug examples
Affected by urinary pH: bases and acids, e.g., amphetamine (base)
Prodrugs: codeine -> morphine.
Active metabolites: codeine-6-glucuronide and morphine-6-glucuronide more potent than parent compounds
Catalytic receptors drug examples
Nesiritide agonist at RGC-A for decompensated congestive heart failure
Linacotide (Sta1) and plecanatide (uroguanylin analogue) are agonists at RGC to treat constipation.
Riociguat activates soluble GC for hypertension
Nitric oxide donors (e.g., GTN, ISDN, ISMN) activate soluble RGC
Larotrectinib inhibits the RTK NRTK1 to treat advanced solid tumours. Imatinib inhibits several RTKs to treat cancers
Nuclear hormone receptors drug examples
Estradiol - ER agonist - estragen replacement therapy
Tamoxifen - ER antagonist - breast cancer
Fluvestrant is a SERD, degrades ER: breast cancer
Norethisterone is a progesterone receptor agonist: oral contraceptive. Ulipristal is a progesterone antagonist: plan B. Mifepristone is a progesterone antagonist used for plan B and abortions.
hydrocortisone, dexamethasone agonists at glucocorticoid receptor: asthma, IBD, immunosuppression, etc…
Fludrocortisone (mineralocrticoid receptor agonist) for adrenocortical insufficiency. Eplerenone (antagonist) for oedema
Oxylmetholone, test agonists at androgen receptor for osteoporosis, anemia, etc… flutamide antagonist for prostate cancer
Tretinoin acts at retinoic acid receptor, acitretin acts at retinoid x receptor, both for psoriasis/acne. Retinol is metabolised into retinoic acid which acts at both RXR and RAR.
Pioglitazone (for DM2) agonist at PPARgamma
Transporters drug examples
Digoxin inhibits Na+/K+ ATPase - antiarrhythmic
omeprazole (PPIs) inhibit H+/K+ ATPase - peptic ulcer
SSRIs
Bendroflumathiazide (diuretic) inhibits the Na+/Cl- symporter
Loop diuretic furosemide inhibits Na+/K+/Cl- symporter
Dapagliflozin inhibits SLGT2 to reduce renal glucose reabsorption: DM2
CNS exclusion by Pgp for cetirizine, loperamide
Glibenclamide inhibits KATP channel for DM2
DDI examples
Lopinavir and subtherapeutic dose of ritonavir to increase [lopinavir] for HIV. Zidovudine and lamivudine syngeristically treat HIV.
Grapefruit inhibits CYP3A4. Broccolo induces CYP1A2
Diazepam displaces phenytoin from plasma proteins.
Terfenadine metabolism into fexofenadine inhibited by ketoconazole (CYP3A4) - terfenadine accumulation toxic
Digoxin renal excretion increased by ACEIs and NSAIDs
NSAIDs compete with methotrexate for renal OATs.
Probenecid increases penacillin halflife by inhibition of renal excretion (exploited therapeutically)
Interindividual variability in PK drug examples
CYP2D6 polymorphism -> different codeine metabolism
Theophyline half-life longer in men
Propranolol clearance lower in women
Lipophillic drugs (e.g., benzos/opioids) higher Vd in women -> lower Cp
[Ethanol] higher in women
Smoking induces CYP1A2
DILI examples
Paracetamol - NAPQI build up from GSH depletion
Halothane - binds to proteins - immune response
Isoniazid - toxicity from lower NAT2 enzyme function
Diclofenac metabolites can cause metabolic and immunoligc reactions
Liver structure and function drug examples
Colestyramine to bind to bile acids - pruritis
Lactulose to prevent growth of the ammonia-producing bowel bacteria. Neomycin or rifaximin as antibiotics to target these bacteria. For hepatic encephalopathy.
Atypical drugs examples
Tubulin inhibitors: vinblastine, vincristine - cancer and gout
Thalidomide - cereblon inhibitor for multiple myeloma
unknown mechanism: cannabidiol, valproate, latanoprost
Conestat alfa (biopharmaceutical recombinant endogenous) a proteainase inhibitor for angiooedma
idursulfase (recombinant) removes sulphate build up -hunter syndrome
Trastuzumab emtansine - tubulin inhibitor and monoclonal antobody combination for breast cancer
Nusinersen (ASODN) to produce SMN1 for spinal muscular atrophy
Inotersen slows translation of transthyretin for transthyretin amyloidosis
volanesorsen slows apolipoprotein C-III translation for chylomicronemia syndrome
ataluren to suppress production of transthyretin for duchenne muscular dystrophy
Patisiran is siRNA to treat tranthyretin amyloidosis. interferes with translation
Chronic therapy examples
salbutamol (and other Adrenergic asthma drugs) get desensitisation/tolerance/downregulation
Beta-blockers (e.g., propranolol) lead to upregulation of the beta adrenoceptors
Capsaicin to desensitise the TRPV1 channels - reduction in pain signalling
Degarelix antagonises GnRH1 to reduce test synthesis for prostate cancer
SM drug examples
Vascular SM:
Losartan (AT1 antagonist), captopril (ACEI) and nifedipine (L-type VGCC inhibitor) to inhibit SM contraction.
Glyceryl trinitrate (GTN, a soluble RGC agonist), sildenafil (PDE5 inhibitor) and diazoxide (KATP activation) used to enhance SM relaxation.
Intestinal SM:
Atropine/hyoscine (M3 antagonist), loperamide (mu-opioid agonist) for diarrhoea
Papaverine (PDE inhibitor) and those above used as antispasmodic of the GI
Bladder SM:
Oxybutynin (M3 antagonist) and mirabegron (B2-AR agonist) reduce bladder tone - treat overactive bladder
Bethanechol (M3 agonist) used to treat urinary retention
Bronchial SM:
Aclindium (M3 antagonist) and montelukast (CysLT1 antagonist) to prevent SM constrction
Salbutamol (B2-AR agonist) and roflumilast (PDE4 inhibitor) to increase SM relaxation
Neuronal function drug examples
Thiorphan inhibits neprilysin in the GIT to prevent breakdown of enkephalins - treats diarrhoea
Amitryptaline (TCA) targets NET, DAT, SERT, inhibits mAChR, histamine receptors, 5-HT2, a1-AR, and VGSCs. used in depression, and neuropathic pain
