-
desferrioxamine
Indications: iron overload
Route: SC infusion
Notes: expensive, iron excreted in urine and stool
-
deferiprone
Indications: iron overload
- Contraindications: hepatotoxicity, extreme overload
- Route: PO TDS
- Notes:
- - cardio-protective
- - less effective than desferrioxamine?
- - iron excreted in urine
-
deferasirox
Route: PO OD
Notes: iron excreted in stool
-
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.
-
-
Adverse Effects of Steroids
(17)
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
-
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
-
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
-
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)
-
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)
-
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
-
alendronate
Class: bisphosphonate
Mechanism: Inhibit osteoclasts to reduce bone resorption
Indications: osteoporosis, hypercalcaemia
-
etidronate
Mechanism: Inhibit osteoclasts to reduce bone resorption
Indications: osteoporosis, hypercalcaemia
-
raloxifene
Mechanism: Agonist of oestrogen ?at bone decreases rate of bone resorption
Indications: osteoporosis
-
demeclocycline
- Mechanism:
Makes collecting duct less responsive to ADH therefore decrease water retention
Indications: SIADH, euvolaemic hyponatraemia
-
tolvaptan
Class: V2 receptor blocker
Mechanism: Blocks ADH therefore collecting duct less permeable, more water excreted
Indications: SIADH, euvolaemic hyponatraemia
Expensive
-
calcium gluconate
- Indications: high potassium
Mechanism: protects the myocardium
Route: IV 10ml 10% asap
-
salbutamol
Class: Beta 2 agonist
Mechanism: Bronchodilation, movement of potassium into cells
Indications: acute asthma, hyperkalaemia
-
-
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
-
Phase I Metabolism of lipid soluble drugs
Oxidation byt cytochrome P450
-
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...
-
gentamycin
Adverse effects: ototoxicity, nephrotoxicity
monitor peak and trough levels
-
lithium
if given with thiazides  decreased excretion, raised plasma level, increased risk of toxicity
-
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)
-
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)
- Synerdic (Quinuprustin-Dalfopristin)
- Amiodarone
- Diltiazem
- Grapefruit juice
- Protease inhibitors (Ritonavir is "triple")
Anti-depressants: MAOI, duoloxetine, fluoxetine, fluvoxamine, sertraline, paroxetine (not citalopram)
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