Pharmacology Flashcards
Aspirin
Action: Irreversibly inhibits COX-2 causing reduced thromboxane production and therefore platelet activation
+ reduced prostaglandin production, reducing inflammation
Indications: Anti-inflammatory- fever/ pain/ headache
Anti-platelet- MI/ stroke
Contras: decrease in gastric mucin production- GI bleed/ ulceration/ H.pylori
Warfarin
Action: Vitamin K antagonist, reduces production of clotting factors, therefore reducing thrombosis
Delayed effect, bleeding risk if high so do INR
Indications: treatment for venous thrombosis and PE
Prophylaxis of embolism in AF, rheumatic HD, prosthetic valve, TIA, post DVT
Contras: bleeding risk, dietary vitamin K (pomegranate)
Heparin
Heparin/ enoxaparin/ daltteparin/ riveparin
Action: glycoaminoglycan, binds to antithrombin and increases it’s activity
Unfractioned- IV Fractioned/ LMW-SC
Indications: treatment of PE/ DVT/ unstable angina/ claudication
Thromboprophylaxis: post DVT/ post surgery/ pregnancy
Contras: bleeding/ thrombocytopoenia + hyperkalaemia
DOACs (direct oral anti-coagulants)
Apixaban
Rivaroxaban
Endoxaban
Inhibits factors 2 and 10
Benefit over warfarin as less monitoring and short dose- response time
Indications: treatment of DVT/ PE
Prophylaxis- post op, post DVT/ PE, second line in prophylaxis with AF
P2Y12 inhibitors
Clopidogrel/ tricagrelor
Inhibits ADP reception on platelets thus reducing activation
Indications: MI gold standard, dual anti-platelet therapy- Aspirin + P2Y12 inhibitor
Contras: bleeding
Beta blockers
Propanolol/ bisoprolol/ atenolol (B1 selective)
B1- vasolation
B2- bronchoconstriction
Negatively ionotropic and chronotropic
Indications: HTN, angina, arrhythmia, post MI/ stable HF (if sinus rhythm)
Contras: severe HF, bronchospasm, asthma, COPD, bradycardia, cold peripheries
Statins
Atorvostatim, simvastatin
Action: reduce cholesterol synthesis
Indications: hypercholesterolaemia, primary/ secondary prevention of CAD
Contras: toxicity to liver/ muscles
ACE inhibitors
Ramipril, enalapril
Action: Inhibit angiotensin converting enzyme at lungs, reducing affect of RAAS, causing systemic vasodilation and a drop in BP
Indications: HTN, HF, secondary to MI
Contras: hypotension, renal as reduces GFR, hyperkalaemia
Causes increased bradykinin- cough, rash, anaphylaxis
Angiotensin receptor blocker
Candesartan/ losartan/ valsartan
Action: antagonise angiotensin II receptors
Indications: when ACE-inhibitors are not tolerated (cough/ rash)
HTN
Contraindications: work poorly in afro-caribbean
Renal artery stenosis as contracts further
Calcium channel blockers
Dihydropyridines: Amlodopine, peripheral vasodilator and coronary artery vasodilator- increases BP and myocardial supply
Indicated: HTN/ angina
Contras: flushing, dizziness, hypotension, oedema
Non-DHPs: verapamil, slows conduction from SAN to AVN
Indicated: angina, HTN, supraventricular tachycardia
Contras: oedema/ bradycardia
Thiazides
Bendroflumethazide
Action: inhibits Na+ absorption at beginning of DCT so less water is absorbed
Downstream epithelial cells try to compensate by reabsorbing Na+ using Na+/K+ antiporters, may lead to hypokalaemia
Indications: oedema/ HTN/ HF
Contras: hypotension/ reduces uric acid secretion so can cause gout/ may worsen diabetes
Loop diuretics
Furosemide
Action: inhibits the N/K/Cl co-transporter in the loop of Henle thus increasing osmolarity of filtrate retaining water
Potential hypokalaemia
Indications: oedema/ secondary for HTN when resistant
Contras: hyponatraemia/ hypokalaemia
K sparing diuretic (aldosterone antagonists)
Spironolactone
Action: alsosterone stimules Na uptake and K excretion, antagonising this reduces water reabsorption and K+ excretion
Indication: oedema/ ascites/ HF/ HTN/ hyperaldosteronism
Contras: addisons (adrenal insufficiency)/ hyperkalaemia/ avoid in kidney damage
Nitrates
GTN spray (glyceryl tri-nitrates)
Action: arterio and venous dilators to reduce BP
Relax CA to increase supply to myocardium
Indications: prophylaxis of angina/ HF and unstable angina
Contras: aortic stenosis/ tamponade/ hypotension
Reslizumab
Monoclonal AB
Interferes with binding of IL-5, reducing eosinophil activity
Indication: severe eosinophilic asthma
Contra: concurrent helminth infection (treat this first)
May cause anaphylaxis
Beta-2 adrenergic agonists
Salbutamol/ salmeterol/ formeterol
Action: B adrenergic receptors relax airway smooth muscle and inhibit histamine release
Indications: asthma/ COPD/ can be SABA or LABA
Contras: tachy/ arrhythmia, hyperkalaemia/ acidosis
Anticholinergics
Atropine, ipratropium, tiotropium
Action: blocking parasympathetic receptors results in bronchodilation
Indication: asthma, COPD,
Cautions: potential glaucoma, paradoxical bronchospasm, prostatic hyperplasia
Inhaled corticosteroids
Beclometasone, budenoside
Action: Reduce oedema, inflammation and immune activation
Increases B2 receptor expression so increase effect of salbutamol
Indication: Asthma, (COPD generally unresponsive)
Cautions: Prolonged high doses can lead to adrenal insufficiency and loss of bone density
Behavioural change
Candidiasis
Leukotriene receptor antagonist
Monteleukast
Action: leukotrienes are inflammatory mediators causing inflammation and WBC activation
Indication: asthmatic prophylaxis, treatment of allergy
Caution: thirst, abdo pain, headache
Proton pump inhibitors
Omeprazole, lanzoprazole
Action: block the H/K ATPase at parietal cells thus less H+ into the lumen
Indication: GORD/ gastric ulcer prophylaxis and treatment/ H. pylori eradication (+ amoxicillin and clarithromycin)
Cautions: Osteoporosis, may trigger SLE rash, abdo pain, headache/ nausea
Histamine 2 receptor antagonists
Ranitidine, cimetidine
Action: Block parietal cell stimulation by histamine thus reducing H+ into lumen
Indication: Gastric ulceration/ GORD
Caution: may mask gastric cancer
SE: Diarrhoea, dizziness, headache
Steroids: prednisolone
Action: mimic effects of adrenal hormones to reduce inflammation and immune response
Indication: reversible obstructive resp disease, allergy, inflammatory conditions: UC, chron’s/ autoimmune: rheymatoid/ joint infections
Cautions: related to hypoadrenalism, HTN, water retention, diabetes, osteoporosis
Try to avoid long-term therapy
Hyoscine butylbromide (buscopan)
Action: antispasmodic agent acting directly on GI tract smooth muscle
Indications: Symptomatic relief for cramps/ spasms in IBS
Used in bowel imaging to reduce spasms
Cautions: may reduce bowel movement too much
Tachycardia/ constipation/ dry mouth/ dry skin
Loperamide
Action: an opioid receptor agonist, acts at peripheral not central receptors thus different to opiate analgaesics, acts at mesenteric plexus on smooth muscle to reduce tone and activity
Indication: acute or chronic diarrhoea
Contras: UC/ Chron’s
SE: Dizziness, headach, flatulance
Movicol/ macrogol
Osmotic laxative (polyethylene glycol)
Action: cannot be absorbed but is osmotically active, thus draws water into lumen relieving diarrhoea
Indication: constipation
Contras: chrons/ UC + arrhythmia
Caution: may cause abdo pain, nausea and flatulence
NSAIDs: apirin, celecoxib, ibuprofen, naproxen, diclofenac
Inhibition of COX enzymes involved in prostaglandin production
GI effects- increased acid production
Less prostaglandins causes pre-glomerular constriction and therefore reduced GFR: nephrotic
Indication: mild-moderate analgesia/ pyrexia/ symptom relief for inflammation
Contras: gastric ulceration/ renal impairment
Paracetamol
Mild analgesic
Indication: pyrexia, analgesic
Caution: high dose is heptotoxic
Give N-acetyl-cysteine in OD
Bisphosphonates
Alendronate, risedronate
Action: reduce bone metabolism thus used in osteoporosis
Have a high affinity for calcium, ingested by and cause death of osteoclasts
Indications: osteoporosis- general/ post-menopausal
Contra: hypocalcaemia
Caution/SE: abdo distention and pain/diarrhoea or constipation/ dyspepsia
Chloramphenicol
Action: abx that inhibits protein synthesis, so is bacteroatatic
Indications: eye and ear infections/ haemophilus influenzae/ typhoid/ meningitis/ cholera
Caution: marrow suppression, diarrhoea, dry mouth, headache, nausea
Ciclosporin
Action: immunosuppressant, acting to suppress T cells and IL2 communication
Indication: rheumatoid arthritis, UC, psoriasis, post transplant
Caution: nephrotoxic, infection risk
SE: abdo pain, fatigue, leukopoenia, HTN
Rifampicin
Action: abx stopping DNA transcription
Indication: TB, serious staph, legionnaires, endocarditis + H. Influenzae
Caution: liver toxic
Orange/ red secretion in urine
Renal damage/ adrenal insufficiency/ flu like symptoms
Opiates
Codeine, morphine, fentanyl, oxycodone
Analgesic acting on central mu receptors
Antagonist = naloxone (in OD and addiction)
Indication: moderate- severe analgesia+ some sedation/ trauma/ MI/ chronic pain
Cautions: addiction and dependance
Respiration depression
Nausea/ constipation/ hypotention/ bradycardia
Atracurium
Neuromuscular blockade by blocking Ach on muscle
Indication: for stillness in surgery/ intubation
SE:anaphylactoid, myopathy, bronchospasm, hypotension
B-lactams
Penicillin/ amoxicillin/ flucloxicillin
Cephalosporins: more resistant to B lactamases
Carbapenems: more resistant
Action: inhibit cell wall production and are therefore bacterocidal
More effective against gram positive
Indication: gram positive infection
Contras: penicillin allergy
Mesalazine
Action: strong anti-inflammatory
Indication: achieving and maintaining remission in UC, often given PR (and given in acute attack)
Less used in Chrons
Caution in elderly
SE: abdo pain, headache, dizziness
Ciclosporin
Action: Immunosuppressant, acting to suppress T cells and IL-2 communication
Indication: RA, UC, psoriasis, post transplant to prevent rejection
Caution: Nephrotoxic and hepatotoxic, immunosuppressant so infection risk
SE: abdo pain, fatigue, leukopenia, HTN
Dobutamine
Beta-1 adrenergic agonist is therefore sympathomimetic
Indication: Acute/ reversible HF i.e. in surgery, septic shock and congestive HF
Contra: IHD, HD (as increases oxygen requirement)
SE: HTN, angina, arrhythmia
Sulfasalazine
Action: 5 amino salicylic acid, strong anti-inflammatory with some immuno-modulatory effects
Indication: RA = DMARD, UC, Chrons
Contra: Renal disease, blood disorder
SE: liver/ kidney toxic, marrow suppression
Oxybutynin
Action: anticholinergic, antagonises muscarinic Ach receptors, reducing tone and spasm at the bladder, reducing ureteric peristalsis
Indication: Urge incontinence, LUTS, kidney stones
Contra: BPH, UC, GI obstruction
Tamulosin/ Doxasozin
Action: Alpha blocker thus relaxes smooth muscle and vasodilates
Indication: BPH
SE: hypotension
Hormone replacement therapy
Oestrogen and progesterone
Action: Relieves symptoms from androgen withdrawal and menopause such as hot flush, night sweats, mood swings, vaginal dryness
Contra: Hx of breast/ ovarian cancer, liver disease, HTN
SE: Increased breast cancer risk, increased clot risk, headache, nausea
Metformin
Action: reduces amount of hepatic gluconeogenesis, lowering blood sugar
Indication: T2DM, polycystic ovary syndrome
Contra: kidney/ liver disease
SE: Diarrhoea, nausea, risk of hypoglycaemia
Sildenafil (viagra)
Action: Inhibits cyclic GMP specific phosphodiesterase 5 (this enzyme degrades cGMP which, when present, relaxes smooth muscle= vasodilation= erection)
Indication: ED, pulmonary artery HTN
SE: Headache, heartburn, flushed skin
Contra: CVD
Lidocaine
Action: Blocks fast Na channels on neurone thus preventing axonal transmission
Indication: SC, local anaesthesia, acute arrhythmia
SE: Sleepiness, twitching, tingling
Cyclophosphamide
Action: Causes apoptosis as it’s metabolite causes DNA cross-linking (only produced in cells with low aldehyde dehydrogenase so less SE)
Indication: Chemo: leukaemia, myeloma, lymphoma, breast, ovarian, immunosuppression
SE: Low WCC, hair loss, pulmonary fibrosis, GU bleed
