Drugs Flashcards
Abx Side Effects
Amoxicillin
SE: rash with infectious mononucleosis
Co-amoxiclav
SE: cholestasis
Flucloxacillin
SE: cholestasis (several weeks after use)
Erythromycin
SE: GI upset, ^QT
Ciprofloxacin
SE: v seizure threshold, tendonitis
Trimethoprim
SE: rash, itchy, photosensitivity, suppress haematopoiesis
Abx - mechanisms
Cell wall synthesis
= penicillins, cephalosporins, carbapanems (beta-lactam), vancomycin (glycopeptide)
Nucleic acid synthesis
= sulphonamides, trimethoprim, quinolones, rifampicin
Protein synthesis
30S = tetracyclines, aminoglycosides
50S = macrolide, clindamycin
ACE Inhibitors
U&E prior to treatment, dose increase and annually
SE - ^K, chronic cough, v BP, AKI
Teratogenic = renal dysgenesis, craniofacial abnormalities
Adrenaline
Sympathomimetic amine, stimulates alpha and beta adrenergic receptors
^CO, ^total peripheral resistance, vasoconstriction in the skin and kidneys (narrow pulse pressure)
Used in anaphylaxis, cardiac arrest
Phentolamine for reversal (distal ischaemia)
Allopurinol
Xanthine oxidase inhibitor
Used in gout, Lesch-Nyhan syndrome
SE: stop allopurinol immediately if rash,
severe cutaneous adverse reaction (SCAR), drug reaction with eosinophilia and systemic symptoms (DRESS), Stevens-Johnson syndrome
Chinese, Korean and Thai increased risk
Interacts - Azathioprine (^levels of 6-mercaptopurine, use 25% dose), cyclophosphamide (marrow toxicity), theophylline
Alpha blockers
Doxazosin and tamsulosin
Used for - benign prostatic hyperplasia and hypertension
SE - postural hypotension, drowsiness, SOB, cough
Amiodarone
MOA - class III antiarrhythmic, blocks potassium channels and inhibits repolarisation, prolongs AP, also blocks sodium channels, 20-100d HL
SE - thyrotoxicosis (stop drug), hypothyroidism, corneal deposits, optic neuritis, pulmonary fibrosis, pneumonitis, liver fibrosis, hepatitis, peripheral neuropathy, myopathy, photosensitivity, slate-grey skin, thrombophlebitis, bradycardia, ^QT
Interacts - warfarin (^INR), ^digoxin levels
TFT and LFT 6monthly (+ baseline with U&E and CXR)
Aspirin
COX-1 and 2 inhibitor
Blocks prostaglandin, prostacyclin and thromboxane A2 formation
Used in IHD
SE - Reye’s syndrome (<16yrs), haemorrhage, peptic ulcers, gastritis, tinnitus
Interacts - potentiated by oral hypoglycaemics, warfarin, steroids
Azathioprine
MOA - metabolised to active mercaptopurine, inhibits purine synthesis
SE: bone marrow depression, n+v, pancreatitis, non-melanoma skin cancer
Interacts with allopurinol (lower dose of azathioprine)
SAFE in pregnancy
Monitor
TPMT test
FBC, LFT baseline and 3monthly
FBC weekly for first month
Beta-blockers
SE: bronchospasm (esp. asthma), fatigue, cold peripheries, v BP, v HR, worsens acute HF
Calcium channel blockers
dihydropyridines (nifedipine and amlodipine)
non-dihydropyridines (diltiazem and verapamil)
SE: headache, flushing, ankle oedema
Nifedipine, amlodipine, felodipine
Used for hypertension, angina, Raynaud’s
Affects peripheral vascular smooth muscle more than myocardium
SE - flushing, headache, ankle swelling, reflex tachycardia (nifedipine, shorter acting)
Verapamil, diltiazem
Verapamil
Used for angina, HTN, arrhythmias
SE - HF, constipation, v BP, v HR, flushing
Contra with b-blockers (heart block)
Diltiazem
Used for angina, HTN
SE - v BP, v HR, HF, ankle swelling
Caution with b-blockers (less neg inotropic)
Carbamazepine
Teratogen = NTD, craniofacial abnormalities
Chloramphenicol
Teratogen = grey-baby syndrome
Ciclosporin
Calcineurin inhibitor, decreases clonal proliferation of T cells by reducing IL-2 release
Used for organ transplant, RA, psoriasis, UC, pure red cell aplasia
Trough levels immediately before dose
SE - nephrotoxic, hepatotoxic, fluid retention, hypertension, ^K, hypertrichosis, gingival hyperplasia, tremor, IGT, hyperlipidaemia, immunosuppressed
Cocaine and smoking
Teratogen = IUGR, preterm labour
Diabetes Drugs
Metformin (biguanide)
SE: GI, lactic acidosis, v appetite
Sulfonylurea (insulin secretagogues - Gliclazide, Tolbutamide, Glipizide)
SE: hypoglycaemia, ^appetite, weight gain, SIADH, cholestasis
Glitazones (PPAR agonists)
SE: weight gain, fluid retention, liver dysfunction, fractures
Gliptins (DPP-4 inhibitors)
SE: pancreatitis
Diclofenac
NSAID
SE - increased risk of cardiovascular events
Contra - IHD, PAD, cerebro VD, congestive HF
Digoxin
Cardiac glycoside, positive inotropic properties
Used for rate control in AF, symptoms in heart failure.
MOA - v conduction through AVN, slows ventricular rate, ^ force of cardiac muscle contraction (inhibits Na+/K+ ATPase pump), also stimulates vagus nerve
Narrow therapeutic index, monitor in suspected toxicity (8 to 12 hours of last dose)
Monitor serum electrolytes and renal function
Dopamine receptor agonists
Bromocriptine, ropinirole, cabergoline, apomorphine
Used in Parkinson’s, prolactinoma, galactorrhea, cyclical breast disease, acromegaly
SE - n+v, postural hypotension, hallucinations, daytime somnolence, ergot-derived (b/ c) associated with pulmonary, retroperitoneal and cardiac fibrosis
-> baseline ESR, creatinine and chest x-ray
Doxazosin
SE: postural hypotension
Lithium Monitoring
TFT and U&E baseline and 6monthly
Lithium level weekly until stable and then 3mthly
12hours after last dose
Normal serum-lithium concentration of 0.4-1
Lithium
Use - mood stabiliser in Bipolar
*Narrow therapeutic range and long half-life
SE: n+v, diarrhoea, fine tremor, diabetes insipidus, hypothyroidism (enlarge), flat/ inverted T wave, weight gain, idiopathic IC HTN, leucocytosis, ^PTH (^Ca)
Teratogenic = Ebstein’s anomaly (atrialised RV)
Toxicity with dehydration, renal failure, thiazides, ACEi/ARB, NSAIDs, metronidazole
Methotrexate
MOA - inhibits dihydrofolate reductase and thymidylate synthesis
SE: myelosuppression, mucositis, liver/ lung fibrosis
FBC, U&E, LFT baseline, weekly and then 2-3monthly
Sodium valproate
SE: liver toxicity
LFT and FBC baseline, LFT periodically in first 6mths
Teratogen = NTD, craniofacial abnormalities
Statins
LFT Baseline, 3 month, 12 month
SE: myopathy, rhabdomyolysis
Caution in liver disease
Contra with macrolides
Drugs that cause IGT
thiazides, furosemide (less common)
steroids
tacrolimus, ciclosporin
interferon-alpha
nicotinic acid
antipsychotics
Beta-blockers
Drug-induced thrombocytopenia
quinine
abciximab
NSAIDs
diuretics: furosemide
antibiotics: penicillins, sulphonamides, rifampicin
anticonvulsants: carbamazepine, valproate
heparin
Drug-induced urinary retention
tricyclic antidepressants e.g. amitriptyline
anticholinergics e.g. antipsychotics, antihistamines
opioids
NSAIDs
disopyramide
Drug-induced photosensitivity
thiazides
tetracyclines (doxy), sulphonamides, ciprofloxacin
amiodarone
NSAIDs e.g. piroxicam
psoralens
sulphonylureas
O&G drugs - Syntocinon, Ergometrine, Mifepristone
Syntocinon
= Synthetic oxytocin, stimulates uterine contraction (v PPH)
Used for active management of third stage, induces labour
Ergometrine
= Ergot alkaloid, stimulates a/d/serotonin receptors, constricts vascular smooth muscle
Used for active management of third stage
SE - coronary artery spasm
Mifepristone
= Prostaglandin analogue, competitive progesterone receptor antagonist
Used with misoprostol to terminate pregnancy
SE - menorrhagia
Serotonin agonists
sumatriptan
= 5-HT1D agonist, acute treatment of migraine
ergotamine
= partial agonist of 5-HT1 receptors
Serotonin antagonist
pizotifen
= 5-HT2 receptor antagonist, migraine prophylaxis
cyproheptadine
= 5-HT2 receptor antagonist, control diarrhoea in carcinoid syndrome
ondansetron
= 5-HT3 receptor antagonist, antiemetic
Finasteride
5 alpha-reductase inhibitor (stops testosterone to dihydrotestosterone)
Used for BPH, male-pattern baldness
SE - impotence, v libido, ejaculation disorders, gynaecomastia, breast tenderness, v PSA levels
Flecainide
Vaughan Williams class 1c antiarrhythmic
MOA - slows AP conduction by acting as a potent sodium channel blocker = wide QRS and PR
Used in AF, accessory SVT e.g. WPW
Contra - post-MI, SHD (HF), sinus node dysfunction, second-degree or greater AV block,
atrial flutter
SE - negatively inotropic, v HR, proarrhythmic, oral paraesthesia, visual disturbances
Gentamicin
Aminoglycoside Abx
SE - ototoxic (auditory/ vestibular nerve damage, irreversible), nephrotoxic (via acute tubular necrosis)
Caution - renal failure
Contra - myasthenia gravis
peak (1 hour after administration) and trough levels (just before the next dose) are measured
Teratogenic = ototoxic
Heparin
activate antithrombin 3
SE - bleeding, thrombocytopenia, osteoporosis, ^K (v aldosterone secretion)
UF
Inhibits thrombin, Xa, IXa, XIa and XIIa
IV, short action
APTT to monitor
^risk of thrombocytopenia and osteoporosis
LMWH
Inhibits Xa only
SC, longer action
HRT
Used for menopausal symptoms (+ P if uterus) and in premenopause (until 50yrs)
PO, patch (better if risk of VTE) or gel
SE -
reduced risk of colorectal cancer
Macrolides
E.g., erythromycin, clarithromycin, azithromycin
MOA - inhibit bacterial protein synthesis, block translocation, bacteriostatic
SE - ^QT, GI, cholestatic jaundice, hearing loss/ tinnitus (azithro)
!!P450 inhibitor
Interacts - stop statins (^myopathy/ rhabdo)
Pain ladder
- paracetamol, NSAIDs
- weak opioid (codeine)
- strong opioid (morphine)
Acute/ post-op
1. strong + anaesthetics
2. oral route
3. peripherally acting only
Maternal DM
Teratogen = macrosomia, NTDs, polyhydramnios, preterm labour, caudal regression syndrome
Metformin
Used in T2DM (titrate up slowly)
MOA - biguanide, activates AMP-activated protein kinase, ^insulin sens, v hep gluconeogenesis
SE - nausea, anorexia, diarrhoea, v B12 absorption, lactic acidosis
No weight gain or hypos
Caution - severe liver disease/ renal failure
Contra - CKD (stop if GFR <30, reduce <45), post-MI, AKI, sepsis, severe dehydration, iodine-containing contrast (day of to 48hrs after), alcohol abuse
Oculogyric crisis
Dystonic reaction
Causes - antipsych, metoclopramide, post-encephalopathic Parkinson’s
Management - stop med, IV benztropine/ procyclidine (antimuscanics)
CYP450 System
Inhibitors (SICKFACES.COM)
Sodium valproate, SSRIs
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Alcohol (binge), amiodarone, allopurinol
Chloramphenicol
Erythromycin
Sulphomanides
Ciprofloxacin
Ommeprazole
Metronidazole
Inducers (CRAP GPS)
Carbamazepine
Rifampicin
Alcohol (chronic)
Phenytoin
Griseofulvin
Phenobarbitone
Sulphonylureas, St John’s Wort
Smoking (affects CYP1A2, why smokers need more aminophylline)
Pharmacokinetics - reactions
Phase I reactions: oxidation, reduction, hydrolysis (by P450 enzymes, alcohol dehydrogenase, xanthine oxidase etc.)
= active, toxic products
Phase II reactions: conjugation
= inactive products, excreted in urine or bile
^Mostly occur in liver
Pharmacokinetics - first pass
Concentration greatly reduced before reaching systemic circulation due to hepatic metabolism - need larger doses PO than other routes
aspirin
isosorbide dinitrate
glyceryl trinitrate
lignocaine
propranolol
verapamil
isoprenaline
testosterone
hydrocortisone
Zero order - phenytoin, salicylates (e.g. high-dose aspirin), heparin, ethanol