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MVST 1B (Fach) / MoDA (Lektion)

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• Gliclazide Use: Diabetes mellitus type II MoA: Sulfonylurea secretagogue, ↑ pancreatic insulin secretion SE: GI upset, weight gain, hypoglycaemia, rash, SIADH → glibenclamide, tolbutamide
• Metformin Use: Type II diabetes mellitus (life style measures failed), polycystic ovarian syndrome MoA: Biguanide; ↑peripheral insulin sensitivity SE: GI upset (→modified release), kidney damage, lactic acidosis Dose: 500 mg PO TDS →sulfonylureas (e.g. gliclazide), glitazones (e.g. pioglitazone), , DPP-4 inhibitors (e.g. gliptins (e.g. sitagliptin)), GLP-1 analogues (e.g. exenatide)
• Pioglitazone Use: Type II diabetes mellitus (on metformin, at rik of hypo's) MoA: PPAR-γ antidiabetic ↓ peripheral insulin resistance SE: GI disturbance, headache. weight gain, water retention, heart failure, fractures →rosiglitazone
• Gliptins Class includes Linagliptin, saxagliptin, sitagliptin, vildagliptin Use: Type 2 diabetes mellitus MoA: Dipeptidylpeptidase-4 inhibitor, ↓ insulin breakdown SE: GI disturbance → GLP-1 analogues (e.g. exenatide)
• Exenatide Use: Type 2 diabetes mellitus MoA: GLP-1 activator, ↑ insulin secretion, ↓ glucagon secretion, gastric emptying SE: GI disturbance, weight loss! →DPP-4 inhibitors (e.g. gliptins) →liraglutide, lixisenatide
• Dapagliflozin Use: Type 2 diabetes mellitus MoA: increase urinary glucose excretion
• Beta-lactam antibiotics Cell wall synthesis: Gram positive   Narrow spectrum benzylpenicillin penicillin G amoxicillin flucloxacillin Broad spectrum (also Gram negative, anaerobes) Co-amoxiclav, pipercillin-tazobactam ("piptaz") cephalosprins: cefuroxime, cefotaxime, ceftriaxone Carbapenems: meropenem, inipenem, ertapenem No atypical or mycobacterial action   Clinical syndromes Respiratory / IE Skin, soft tissue, bone, joints UT/GU Meningities (cross BBB when inflamed) Side effects: Rash Colitis, diarrhoea with broad spectrum Hypersensitivity Safe in pregnancy
• Teicoplanin Use: MRSA, severe peumonia w/ penicillin allergy, C. diff infection MoA: Glycopeptide antibiotic SE: rash pruritis; GI upset; monitor LFT, U&E, FBC, hearing; vancomycin sensitivity → vancomycin
• Macrolide antibiotics → Erythromycin→ Clarythromycin→ Azithromycin Clinical use Respiratory infections, in particular atypical pneumonia & penicillin allergy Skin & soft tissue Enteric infections (e.g. campylobacter jejuni → GBS) Uncomplicated chlamydia   Spectrum of activity: Gram positive: good, but resistance in staph's Gram negative: poor, but respiratory (Legionella, H. influenzae, M. cat) okay Anaerobe: poor Intracellular: good, e.g. chlamydia, azithromycin for enteric fever Mycobacterium: some, e.g. clarithromycin → Amoxicillin, metronidazole, ciprofloxacin
• Amikacin Use: serious Gram-(-) infections resistant to gentamicin MoA: Aminoglycoside antibiotic SE: GI upset, oto-, nephrotixicity → gentamicin, streptomycin
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• Levofloxacin Quinolone antibiotic, not 1st line →ciprofloxacin
• Moxifloxacin Quinolone antibiotic, not 1st line →ciprofloxacin
• Quinolone antibiotics Inhibit DNA syntheis by inhibiting DNA gyrase & supercoiling Spectrum of activity Some Gram positive: levo and moxi good for S. pneumonia Good Gram negative, including pseudomonas (except moxi) Good ntracellular, e.g. legionella, enteric fever, etc. Some mycobacterial, esp moxi Clinical use: Empirical treatment if Gram negative & penicillin allergy Upper UTI, GI infections Respiratory infection without pneumococci Moxi for LRTI, including TB Meningitis contact prophylaxis Side effects Seizures, tendon damage, relative CI in children
• Clindamycin Use: Joint infection, osteomyelitis, intra-abdominal sepsis Spectrum: Gram-(+) bacteria, incl. bacteroides fragilis, and anaerobes MoA: Lincosamide antibiotic; Lipophilic, anti-protein toxin, e.g. Staph. aureus Panton-Valentine Leukocidin toxin SE:  GI upset, oesophagitis, pseudo-membranous colitis → linezolid, lincomycin
• Doxycycline Use: idiosyncratic, e.g. atypical pneumonia MoA: Tetracycline antibiotic SE: Cardiac, photosensitive rash; absolute CI in pregnancy
• Nitrofurantoin Use: Urinary tract infections by Gram negatives MoA: Antibiotic, damages DNA SE: GI upset, pulmonary reactions, peripheral neuropathy; monitor kidney function! → trimethoprim, co-trimaxazole, amoxicillin, cefadroxil; cefuroxime, ciprofloxacin
• Antimicrobial prophylaxis Prevention of secondary cases of Neisseria Meningitidis andHaemophilus Influenzae meningitis →  ciprofloxacin or rifampicin Prevention of pneumococcal infection inpatients with asplenia or hyposplenism → benzylpenicillin + immunisations Prevention of TB in close contacts → rifampicin + isoniazid Prevention of infection in surgical patients: cefuroxime/teicoplanin + gentamicin/ciprofloxacin Prevention of recurrence of rheumatic fever →phenoxymethylpenicillin
• Tuberculosis treatment Standard: Rifampicin → orange tears & urine Isoniazid + pyridoxine (vit B6) → peripheral neuropathy Pyrazinamide → hepatotoxicity Ethambutol → optic neuritis Others D-cycloserine Streptomycin
• Ethambutol Use: tuberculosis MoA: inhibits cell wall synthesis SE: Optic neuritis, nephrotoxicity, red/green colour blindness, peripheral neuropathy → rifampicin, isoniazid + pyridoxine, pyrazinamide
• Pyrazinamide Use: Tuberculosis MoA: pyrazoic acid → accumulation + metabolic disturbance SE: Hepatotoxicity → isoniazid + pyridoxine, ethambutol, rifampicin; D-cycloserine, streptomycin
• Anti-fungal drugs Azoles: inhibit ergosterol synthesis fluconazole itraconazole miconazole Polyenes: bind to ergosterol → leakage amphotericin B nystatin Echinocandins: caspofungin Other: griseofulvin
• Loperamide Use: Acute diarrhoea MoA: μ-opiod receptor agonist, inhibiting the myentieric plexus ↓ peristalsis SE: nausea, flatulence, headache, dizziness; less commonly dyspepsia, vomiting, abdominal pain, dry mouth, drowsiness, rash
• Octreotide Use: carcinoid syndrome, acromegaly, pancreatic tumour MoA: Somatostatin analog SE: GI disturbance, headache, arrythmias   →pegvisomant
• Colchicine Use: Acute gout MoA:inhibits microtubule polymerization SE: nausea, vomiting, profuse diarrhoea → allopurinol, febuxostat
• Benzylpenicillin = Penicillin G Use: endocarditis (S. viridans & empirical → amoxicillin), meningococcal disease, pneumonia (S. pneumoniae), cellulitis;  throat infections, otitis media Spectrum: narrow; Gram positive's: streptococci, gonococci, meningococci MoA: β-lactam antibiotic, β-lactamase sensitive SE: Hypersensitivity reactions, rash with EBV infectious mononucleosis → ampicillin/amoxicillin/co-amoxiclav; flucloxacillin, piptaz; Penicillin V
• Thiamine Use: thiamine deficiency, Wernicke's encephalopathy (=Cofusion, ataxia, nystamgus/external ophthalmoplegia), Korsakoff's psychosis (anterograde amnesia, confabulation) MoA: Vitamin B1; needed for catabolism of glucose, synthesis of ACh and GABA. SE: anaphylaxis Dose: Mild deficiency:25–100 mg PO daily; severe deficiency: 200–300 mg daily in divided doses
• Lorazepam Clinical use: epileptic seizure, status epilepticus, anxiety MoA: Benzodiazepine ↑GABAA SE: as diazepam: respiratory depression, dependence, aggression, confusion amnesia → diazepam, chlordiazepoxide, midazolam, temazepam
• Carbamazepine Use: Epilepsy: focal/partial & 2ary generalized seizures, trigeminal neuralgia MoA: Stabilises inactivated Na+ channels, potentiates GABAA transmission SE: dry mouth, GI upset; auto-inducer of P450 cyt-c → sodium valproate, lamotrigine, phenytoin, levetiracetam, diazepam
• Isotretinoin Use: comedones and inflammatory lesions in acne; mild to moderate→topical; severe→oral MoA: Dry skin, dry moutyh, hair thinning SE: contra-indicated in pregnancy
• Adrenaline* Anaphylaxis, cardiac arrest MoA: β1-radrenoreceptor agonist Dose: Anaphylaxis: 150μg, 300μg, 500μg IM or IV (in <6yrs, 6-12yrs, >12yrs) Cardiac arrest: 1mg = 10ml of 1:10,000 IV   1:10,000 IV = 1mg in 10ml 1:1,000 IM = 1mg in 1 ml
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• Dimercaprol Use: Heavy metal overdoes, injected; superseded by other chelators →desferrioxamine
• Metolazone Use: Oedema, hypertension, heart failure MoA: Potent thiazide-like diuretic SE: ↓K+, ↓Na+, ↓Mg2+, ↑Ca2+, ↑urate (→gout); GI upset, hypotension, chills, chest pain → indapamide, chlortalidone; bendroflumethiazide
• Eplerenone Use: Chronic heart failure MoA: Aldosterone antagonist SE: GI upset, hypotension, rash, hyperkalaemia, no gynacomastia → spironolactone; amiloride/triamteren; ramipril; losartan
• Midazolam Use: conscious sedation for procedures (e.g. endoscopy), status epilepticus (rectal) MoA: Long-acting benzodiazepine, ↑GABAA SE: As diazepam + GI upset, dry mouth hiccups → diazepam, chlordiazepoxide, lorazepam, temazepam
• Fentanyl Use: pre-procedure sedation (e.g. endoscopy), analgesia MoA: Short-acting μ-opiod receptor antagonist SE: nausea & vomiting, constipation, resp depression → codeine, morphine*, diydrocodeine, tramadol, oxycodone; → naloxone  
• Indomethacin Use: Pain & moderate-to-severe inflammation in reumatic disease; gout; dysmennorhoea, premature labour; headache (hemicrania continua) MoA: Non-steroidal SE: bleeding (GI and otherwise), asthma →aspirin; diclofenac, ibuprofen; celecoxib; lansoprozole/omeprazole, ranitidine/cimetidine, misoprostol, pirenzepine, gaviscon
• Denosumab Use: 1ary and 2ary prevention of osteoporotic bone fractures; bone mets from solid tumours (exept prostate) MoA: antibody to RANK ligand, inhibiting osteoclast activity SE: diarrhoea, constipation, dyspnoea, urinary tract infection, upper respiratory tract infection, pain in extremity, sciatica, hypocalcaemia (fatal cases reported), hypophosphataemia, cataracts, rash, sweating; osteonecrosis, atypical femoral fractures → alendronate, calcium, vit D
• Pegvisomant Use: Treatment-resistant acromegaly MoA: Selective growth factor receptor antagonist SE: GI upset, deranged LFT's, headache →octreotide
• Charcoal Acute intoxications, e.g.   MoA: Inhibits absorption from stomach
• N-Acetyl-Cysteine Paracetamol overdose   MoA: Replenish depleted glutathione in the liver
• Docusate sodium Use: Constipation, adjunct in abdominal radiological procedures MoA: Stimulant laxative SE: abdominal cramps, diarrhoea, hypokalaemia, rash →senna*, movicol, glycerol, lactulose*
• Gaviscon Gastro-Oesophageal Reflux Disease, heartburn Over-the-counter MoA: Antacid → omeprazole/lansoprazole; ranitidine, cimetidine; misoprostol; pirenzepine
• Glycerine suppositories Stimulant laxative Over-the-counter.
• Lactulose* Use: Constipation, hepatic encephelopathy MoA: Osmotic laxative, removes urea from gut Dose (constipation): lactulose 3.1–3.7 g/5 mL with other ketoses initially 15 mL twice daily, adjusted according to response →senna*, movicol, glycerol, phosphate enemas, docusata sodium
• Movicol (macrogol) Constipation MoA: Osmotic laxative Dose: Oral powder, macrogol ‘3350’ (polyethylene glycol ‘3350’) 13.125 g, sodium bicarbonate 178.5 mg, sodium chloride 350.7 mg, potassium chloride 46.6 mg/sachet 1–3 sachets daily in divided doses usually for up to 2 weeks →lactulose*; senna*, docuste sodium; loperamide
• Phosphate enema Constipation, bowel evacuation MoA: Osmotic laxative, rectal administration  
• Senna* Use: Constipation MoA: Stimulant laxative; Over-the-counter Dose: Tablets, total sennosides (calculated as sennoside B) 7.5 mg 2–4 tablets, usually at night; initial dose should be low then gradually increased →docusate sodium; lactulose*, gavicol; loperamide
• Ramipril Use: HTN, Heart failure, diabetic nephropathy; post-MI MoA: ACE-Inhibitor, ↓circulating angiotensin II SE: Dry cough, hyperkalaemia, angiooedema; contraindicated in bilateral Renal artery stenosis (→flash pulmonary oedema → stop) → lisinopril, enalapril, captopril
• Lisinopril HTN, Heart failure, post-MI MoA: ACE-Inhibitor, ↓circulating angiotensin II   → ramipril, enalapril, captopril
• Candesartan Use: HTN, heart failure, diabetic nephropathy MoA: Angiotensin-II-receptor (AT-1) antagonist SE:Hyperkalaemia →losartan, irbesartan

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