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  1. desferrioxamine
    Indications: iron overload

    SC infusion

    Notes: expensive, iron excreted in urine and stool
  2. deferiprone
    Indications: iron overload

    • Contraindications: hepatotoxicity, extreme overload
    • Route: PO TDS

    • Notes:
    • - cardio-protective 
    • - less effective than desferrioxamine?
    • - iron excreted in urine
  3. deferasirox
    Route: PO OD

    Notes: iron excreted in stool
  4. prednisolone
    • Class: corticosteroid (no mineralocorticoid activity)
    • Dose: 5 - 7.5mg is equivalent to endogenous secretion

    • MoA:
    • - decrease prostaglandin synthesis
    • - decrease phagocyte trafficking and proteolytic enzyme release
    • - sequestration of lymphocytes in lyphoid tissue
    • - induction of lymphocyte apoptosis
    • - inhibition of cytokine gene expression
    • - decreased antibody production

    Adverse Effects: diabetes, obesity, lipid abnormalities, osteoporosis

    USA give prednisone, which is metabolised to prednisolone by the liver.
  5. Eicosanoid Synthesis
    Image Upload
  6. Adverse Effects of Steroids
    metabolic: diabetes, central obesity, lipid abnormalities, osteoporosis, adrenal suppression

    visible: bruising, striae, moon face, buffalo hump, hirsuitism

    glaucoma, peptic ulcers, immunosuppression, cataracts,  pancreatitis, avascular necrosis, psychosis

    • Notes:
    • - patients taking steroids for more than 3 weeks need to be tapered off gradually 
    • - patients are at risk if exposed to VZV
  7. cyclophosphamide
    • Indications: severe connective tissue disease with end-organ damage (SLE, Wegener's) or Cancer

    Class: anti-proliferative

    Mechanism: alkylates guanine Image Upload DNA damage therefore blokcs cell division

    Adverse Effects: bone marrow suppression, hair loss, sterility (M > F), haemorrhagic cystitis, immunosuppression,  infection, teratogenesis 
  8. azathioprine
    • Indications: transplantation, auto-immune and auto-inflammatory diseases (Crohn’s, UC)

    Class: anti-proliferatives

    • ˜Mechanism: liver metabolises to 6-mercaptopurine which blocks de novo purine (G & A) synthesis.
    • (Suppresses Tc activation and proliferation in particular)

    Adverse Effects: bone marrow suppression (esp Tc and plt), hepatotoxicity (idiosyncratic), immunosppression,  infection, teratogenesis

    • 1:300 people have a Thiopurine methyltransferase
    • (TPMT) polymorphism meaning they cannot metabolise azathioprine and get severe bone marrow suppression
  9. mycophenolate mofetil
    Indications: transplantation, auto-immune disease with end-organ damage

    Class: anti-proliferatives˜

    Mechanism: blocks de novo nucleotide synthesis

    Adverse Effects: bone marrow suppression (espTc and plt), immunosppression, infection, teratogenesis, reactivation of viruses including herpes and JC (no test available for JC virus)

    JC reactivation Image Upload progressive multifocal  leukoencephalopathy (PML)
  10. ciclosporin
    • Indications: transplantation, severe auto-immune disease

    Class: calcineurin inhibitors, immunosuppressants

    Mechanism: blocks intracellular signalling in Tc, therefore inhibiting IL-2 mediated proliferation and activation

    Adverse effects: nephrotoxicity, neurotoxicity, hypertension, dysmorphism (gingival hypertrophy, hirsuitism)
  11. tacrolimus
    Indications: transplantation, topical for skin disease

    Class: calcineurin inhibitors, immunosuppressants

    Mechanism: blocks intracellular signalling in Tc, therefore inhibiting IL-2 mediated proliferation and activation

    Adverse effects: nephrotoxicity, neurotoxicity, hypertension, diabetes mellitus
  12. alendronate
    Class: bisphosphonate

    Mechanism: Inhibit osteoclasts to reduce bone resorption

    Indications: osteoporosis, hypercalcaemia
  13. etidronate
    • Class: bisphosphonate

    Mechanism: Inhibit osteoclasts to reduce bone resorption

    Indications: osteoporosis, hypercalcaemia
  14. raloxifene
    • Class: SERM

    Mechanism: Agonist of oestrogen ?at bone decreases rate of bone resorption

    Indications: osteoporosis
  15. demeclocycline
    • Mechanism: Makes collecting duct less responsive to ADH therefore decrease water retention

    Indications: SIADH, euvolaemic hyponatraemia
  16. tolvaptan
    Class: V2 receptor blocker

    Mechanism: Blocks ADH therefore collecting duct less permeable, more water excreted

    Indications: SIADH, euvolaemic hyponatraemia

  17. calcium gluconate
    • Indications: high potassium

    Mechanism: protects the myocardium

    Route: IV 10ml 10% asap
  18. salbutamol
    Class: Beta 2 agonist

    Mechanism: Bronchodilation, movement of potassium into cells

    Indications: acute asthma, hyperkalaemia
  19. colchine
    • Class: Anti inflammatory

    Indications: acute gout
  20. allopurinol
    Class: Xathine oxidase inhibitor

    Mechanism: decreases synthesis of uric acid, halts pathway at xanthine which is excreted in urine? 

    Indications: after an acute episode of gout, before starting chemo for haematological malignancies (avoiding tumour lysis syndrome)

    Notes: extends the mercaptopurine from azathioprine metabolism, so increases bone marrow toxicity
  21. Phase I Metabolism of lipid soluble drugs
    Oxidation byt cytochrome P450
  22. Digoxin Toxicity - Symptoms
    • * arrhythmia - particularly ventricular extrasystoles, bigeminy/trigeminy, atrial tachy + complete heart block
    • * anorexia, nausea and vomiting
    • * xanthopsia, blurred vision, photophobia

    Symptoms of under-treatment and toxicity may be similar... 
  23. gentamycin
    Adverse effects: ototoxicity, nephrotoxicity

    monitor peak and trough levels
  24. lithium
    if given with thiazides Image Upload decreased excretion, raised plasma level, increased risk of toxicity
  25. Enzyme Inducers
    4 for BUGS: Griseofulvin (antifungal), Rifampicin, Rifabutin, Rifapentine

    4 for BAD DAYS: Barbituates (phenobarbitone, phenobarbitol, meprobamate, primidone), Alcohol (chronic use - CYP 2E1), Smoking, St John's Wort (Hypericum perforatum)

    4 for FITS: Phenytoin, Carbamazepine > Oxcarbazepine, Topiramate (induces OCP)

    3 for HIV: Nevirapine (substrate and inducer), Efavirenz (substrate, inducer, inhibitor = the 'triple'), Ritonavir (substrate, inducer, inhibitor = the 'triple')

    and a handful for SUGAR: Sulfonylureas (tolbutamide, glipizide, gliclazide, glibenclamide)
  26. Enzyme Inhibitors

    SICK COP with MAD FACE VS A SAD GP --> 6 Antidepressants
    • Sodium valproate
    • Isoniazid (especially in slow acetylators)
    • Cimetidine (not ranitidine)
    • Ketoconazole (> itraconazole > fluconazole)

    • Ciprofloxacin (esp. w. Warfarin and theophylline),
    • Omperazole (not lansoprazole)
    • Phenylbutazone

    • Metronidazole
    • Allopurinol
    • Disulfiram

    • Fluconazole
    • Alcohol (binge drinking)
    • Chloramphenicol
    • Erythromycin, clarithromycin, telithromycin (not Azithromycin)

    • Verapamil
    • Sulfinpyrazone

    • Synerdic (Quinuprustin-Dalfopristin)
    • Amiodarone
    • Diltiazem

    • Grapefruit juice
    • Protease inhibitors (Ritonavir is "triple")

    Anti-depressants: MAOI, duoloxetine, fluoxetine, fluvoxamine, sertraline, paroxetine (not citalopram)
Card Set:
2012-07-16 21:39:12
pharmacology medicine

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