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2012-07-16 17:39:12
pharmacology medicine

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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
  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  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  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  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)