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MVST 1B (Fach) / MoDA (Lektion)

MVST 1B - MoDA

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  • Tirofiban Antiplatlet drug; non-peptide GP-IIa/IIIb-receptor antagonist → aspirin, clopidgrel, dipyridamole, abciximab
  • Tranexamic acid Use: Excessive fibrinolyses (surgery, dental extraction), menorrhagia, epistaxis, trauma, thrombolytic overdose, endometriosis MoA: Anti-fibrinolytic; inhibits plasminogen activation SE: Nausea, vomiting, diarrhoea; VTE → aminocaproic acid; alteplase, desmoteplase; → mefanemic acid
  • Triamterene Use: oedema, K+ conservation with loop and thiazide diuretcs MoA: K+-sparing diuretic; ENaC inhibitor SE: GI upset, hyperkalaemia → amiloride; spironolactone, eplerenone
  • Warfarin* Use: PX of embolisation in rheumatic heart disease and atrial fibrillation; PX after insertion of prosthetic heart valve; PX and TX of VTE; TIA MoA: Oral anticoagulant; VitK peroxide reductase inhibitor; Factors II, VII, IX, X → monitor INR ≅ PT ratio SE: initial hypercoagulability; bleeding, GI upset, diarrhoea, rash; P450 substrate (beware →clarythromycin etc) Dose: aim for INR 2.5, unless: recurrent VTE (→3.5), mechanical mitral valve
  • Ether Obsolete anasthetic
  • Etomidate Use: Induction of anaesthesia MoA: Intravenous anesthetic, IV infusion SE: GI upset, dizziness, apnoea; erroneous muscle movements → pain → propofol, ketamine,thiopental sodium; halothane; suxamethonium; curare derivatives.
  • Halothane Use: Induction/maintenance of anaesthesia MoA: Gaseous anaesthetic SE: halothane hepatitis, arrythmias, malignant hyperthermia (→dantrolene) →isoflurane
  • Nitrous oxide Use: Analgesia (+ O2) in obstretics and emergency; maintenance of anaesthesia MoA: Inhaled gaseous anaesthetic SE: Hypoxia, megaloblastic anaemia →isoflurane; halothane; propofol, ketamine
  • Propofol Use: induction/maintenance of anaesthesia MoA: intravenous anaesthetic SE: rare: muscle activity, convulsions, arrythmia, anaphylaxis, delayed recovery →ketamine, etomidate, thiopental; isoflurane, halothane; suxamethonium; curare derivatives
  • Thiopental Use: induction of anaesthesia, status epilepticus; euthanasia, execution MoA: intravenous anesthetic; fastest-acting barbiturate, not analgesic SE: hypotension, arrhythmias, myocardial depression, laryngeal spasm, cough, headache, sneezing, hypersensitivity reactions, rash → propofol, etomidate, ketamine
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  • Aciclovir Clinical use: Herpes Simplex & Varicella Zoster infections, incl. suspected viral meningitis MoA: Guanosine analogue anti-Herpes; activation by viral thymidine kinase; chain terminator → guanciclovir
  • Amantadine Use: Influenza; Parkinson via unknown mechanism MoA: Blocks M-channel to prevent acidification of endosome and membrane fusion →oseltamivir, zanamivir
  • Amoxicillin* Use: Low to moderate community-aquired pneumonia, otitis media, Listeria meningitis (→ampicillin), strep. viridans infective endocarditis, H. pylori eradication Spectrum: streptococci, β-lactamase sensitive MoA: β-lactam penicillin antibiotic; inhibits cell wall synthesis. SE: GI upset, rash (→discontinue) Dose: 500mg PO TDS +clavulunate → augmentin/co-amoxiclav; →flucoxacillin, penicillin V+G, piptaz
  • Amphotericin B Use: Systemic fungal infections, incl cryptococcal meningitis (India ink stain) MoA: Polyene antifungal; binds ergosterol → membrane leakage; good CNS penetration; systemic administration SE: GI upset, CVS systems incl arrythmias, chest pain, dyspnoea, BP changes → nystatin; -azoles; griseofulvin
  • Ampicillin Use: Listerial meningitis; urinary-tract infections, otitis media, sinusitis, bronchitis, low or moderate-severity community-acquired pneumonia; endocarditis treatment MoA: β-lactam antibiotic, very similar to→ amoxicillin SE: GI upset, rash Dose: Meningitis: IV infusion 2g every 4hours → amoxicillin; ceftriaxone, aciclovir
  • Artemisinin Use: Malaria MoA: no heavy metal; from chinese herb → chloroquine, artesunate, quinine
  • Augmentin / Co-amoxiclav Use: Moderate community aquired pneumonia, bone and joint infections, animal bite Spectrum: Broad, incl Staph. aureus, E. coli, H. influenzae MoA: Amoxicillin (β-lactam antibiotic) + clavulunate (β-lactamase inhibitor) SE: GI upset, hypersensitivity, cholestasis Dose: 250-500mg PO TDS → amoxicillin/ampicillin, flucloxacillin, penicillin G+V, piptaz
  • Bacitracin Antibiotic targetting cell wall biosynthesis; inhibitis dephosphorylation of bactoprenol
  • Bevacizumab Use: Certain cancers, incl Colon-Ca, glioblastoma MoA: α-VEGF antibody → alemtuzumab
  • Bleomycin Use: Anticancer, e.g. squamous cell carcinoma MoA: Anthracycline, Metal chelater; cytostatic in G2- and M-phase; works best with oxygen → ROS SE: Progressive pulmonary fibrosis →mitomycine, daunomycin; doxorubicin/mitoxantrone
  • Cephalosporin Group of β-lactam antibiotics →cefaclor/cefalexin, cefuroxime, ceftazidime, ceftriaxone, cefotaxime, etc.
  • Cetuximab Use: Certain cancers, incl colon Ca MoA: Monoclonal α-EGFR antibody →bevacizumab, trastuzumab
  • Chloramphenicol Use: Life-threatening infections, in particular H. influenzae MoA: Antibiotic targetting protein biosynthesis; binds 26S rRNA in 50S subunit of ribosome.
  • Chloroquine Use: Malaria. MoA: Inhibits haemozoin formation in food vacuole. High resistance  → quinine, Fansidar, artesunate disease-modifying anti-rheumatic drug → hydroxychloroquine (HCX)
  • Cidofovir Use: CMV reitinits in AIDS patients MoA: Acyclic nucleoside analogue; virostatic → ganciclovir, foscarnet; aciclovir
  • Ciprofloxacin Use: LRTI in CF, fistulating Crohn's, prophylaxis of meningococcal meningitis (→rifampicin); gonorrhoea, clamydia; pyelonephritis (→cefuroxime), gastroenteritis (→clarithromycin) Spectrum: Gram-(-) bacteria, including salmonella, shigella, campylobacter, neisseria, and pseudomonas moderate activity against Gram-(+) bacteria such as S.pneumoniae and E.faecalis MoA: Fluoroquinolone antibiotic; inhibits DNA gyrase (topo II) and topo IV SE: GI, headache, dizziness, injection site reactions, tendinopathy, nephrotoxicity → moxifloxacin, → levofloxacin
  • Cisplatin anti-cancer; intra-strand cross links in DNA
  • Clavulanate Lactamase inhibitor, NOT class B +amocillin → augmentin / co-amoxiclav
  • Co-trimoxazole Use: Urinary tract infections, PCP prophylaxis & treatment MoA: Sulfamethoxazole (inhibits DHPS) + trimethoprim (inhibits DHFR): Antifolate antibiotic combination SE: GI upset, Stephen-Johnson syndrom, blood dyscrasias (bone marrow depression, agranulocytosis) → trimthoprim, sulfamethoxazole; nitrofurantoin
  • Cyclophosphamide Use: Certain cancers; rheumatic disease MoA: nitrogen mustard alkylating agent SE: haemorrhagic cystitis (→MESNA); GI upset, anorexia, cardiac toxicity → azathioprine/mycophenolate, ciclosprine/tacrolimus. steroids
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  • Daunomycin Use: Certain cancers MoA: Anthracycline; intercalates in DNA SE: cardiac toxicity →mitomycin, dactinomycin, doxorubicin/mitoxantrone
  • D-cycloserine Use: Second line drug for mycobacterium tuberculosis MoA: Antibiotic targeting cell wall biosynthesis; inhibits alanine racemase and D-alanine ligase in the synthesis of Ala-Ala terminal → isoniazid, pyrazinamide, rifampicin, ethambutol; bacitracin
  • Doxorubicin Use: Certain cancers MoA: Anthracycline anti-cancer; intercalates in DNA cardiotoxic b/c of free oxygen radicals, deliver in liposomes unlike →mitoxantrone (newer) →daunomycin/-rubicin, mitomycin, dactinomycin
  • Erlotinib Use: Certain cancers, e.g. lung MoA: Tyrosine kinase inhibitor acting on EGF-receptor → imatinib
  • Erythromycin Use: Penicillin allergy, syphillis, atypical LRTI Spectrum: similar to pencillins MoA: Macrolide antibiotic targeting protein biosynthesis; blocks exit tunnel of ribosome SE: GI upset, chlestatic jaundice, hepatotoxicity; P450 inhibitor → clarithromycin, azithromycin  
  • Etoposide Use: Certain cancers MoA: Topoisomerase II inhibitor → vinca alkaloids (vincristine, vinblastine), topoisomerase I inhibitors (topotecan, irinotecan)
  • Fansidar Use: Malaria + quinine; not for prophylaxis MoA: Antiprotozoal combination drug: Sulfadoxine (inhibits DHPS) + pyrimethamine (inhibits DHFR) ~ co-trimoxazole; → quinine, chloroquine, artesunate
  • Fluconazole Use: Vaginal, mucosal, invasiv candidiasis; tenia pedis; prevention in immunocompromised, e.g. cryptococcal meningitis MoA: Triazole antifungal; inhibits ergosterol synthesis SE: GI upset, rash, hypersensitivity →itraconazole; amphotericin B, nystatin; griseofulvin
  • 5-Fluorouracil Use: Certain cancers MoA: Pyrimidine analogue; inhibits DNA/RNA synthesis and function through thimidylate synthase ⇒ suicide inhibitor, antimetabolite →folinic acid/leucovorin, methotrexate
  • Flutamide Use: advanced prostate cancer MoA: Androgen receptor antagonist →finasteride, tamoxifen; goserelin
  • Foscarnet Use: CMV disease; refractory herpes simplex in immunocompromised MoA: mimics anion pyrophosphate to inhibit viral DNA polymerase → cidofovir, gaciclovir; aciclovir
  • Fosfomycin Use: uncomplicated urinary tract infection, not 1st line MoA: Antibiotic targeting cell wall biosynthesis; inhibits MurA (ligation of PEP) → trimethoprim, nitrofurantoin, amoxicillin, cefadroxil; cefalexin, cefuroxime, ciprofloxacin
  • Fusidic acid Use: Penicillin-resistant Staph aures osteomyelitis & endocarditis; good skin & soft tissue penetration MoA: bacteriostatic antibiotic; acting on elongation factor G
  • Ganciclovir Use: CMV infection MoA: Guanosine analogue; chain terminator after activation →aciclovir
  • Gentamicin Use: not commonly as monotherapy combined with β-lactam in Gram-(-) sepsis (urinary, biliary, respiratory, GI) combined with β-lactams (→ benzylpenicillin) in Infective Endocarditis Spectrum: Gram-(-)& pseudomonas; Gram-(+) if combined with penicillins MoA: Aminoglycoside antibiotic; inhibits protein biosynthesis at 30S subunit Side effects: Ototoxic, nephrotoxic → amikacin, → streptomycin
  • Goserelin Use: hormone-dependent breast and prostate cancer MoA: GnRH superagonist →flutamide, finasteride, tamoxifen
  • Gramicidin A Use: Not commonly used antibiotic: ear / eye infection with dexamethasone MoA: Bacteriocidal antibiotic targeting the cell membrane; monovalent cation channel (stacked dimer); dissipation of ion gradients.
  • Imatinib Use: Ph+ (t(9,22) brc/abl) CML MoA: Tyrosine kinase inhibitor → erlotinib;
  • Folinic acid Use: Adjuvant to methotrexate chemotherapy, "folinic acid rescue" MoA: provides FH4 to allow DNA synthesis → folic acid
  • Lomustine Anti-cancer; alkylating nitrosourea; readily crosses BBB

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