Systems drugs

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Harry Robertson
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Harry Robertson
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lovastatin/atorvastatin used in angina prevention.inhibits HMG CoA reductase. causes decreased liver cholesterol synthesis and increase VLDL and LDL receptor synthesis = less LDL in blood
fibrates angina prevention. PPAR agonist. causes -increased beta oxidation by liver, -decreased hepatic trigyceride secretion, -increased LPL activity -increased HDL
bile acid binding agents (cholestipol, cholestyramine) angina prevention. bind bile acid in the gut. causes - decreased enterohepatic recirculation - increased hepatic production of bile salt - decreased liver cholesterol (cholesterol is needed for bile salts) -increased LDL receptor expression= decreased LDL in blood
beta blockers angina treatment first line therapy for chronic stable angina.
differences between phenylalkylamines, benzothiazepines, dihydropyridines in treating angina aim is to reduce myocardial oxygen demand and increase coronary perfusion in angina. phenylalkylamines (verapamil) are very myocardial selective therefore very little peripheral effect seen Dihydropyridines have lots of peripheral vasodilator action (not wanted for angina treatment because of sympathetic reflex)(also not used for antiarrythmia treatment)(however, useful for treatment of hypertension) Benzothiazepines are a bridge between the two (both cardiac depressant and vasodilator action- able to reduce arterial pressure without having too much of a sympathetic reflex)
why give low dose aspirin in angina treatment inactivates cox in platelets but not in endothelial cells. cox have no nucleus and cannot resynthesise TXA2
thiazides give alternative names hydrochlorothaizide, bendroflumethazide, chlorthalidone, metolazone. mild diuretic effect. direct vasodilator action. Act at the DCT. Blocks the sodium/chloride transporter at collecting duct. Causes increased potassium loss and reduced uric acid. used to treat hypertension
2 phases of effect in ACE inhibitors -rapid due to anti ANG 2 effect -Slower due to blood volume effect and control of thirst
Quinidine class 1a antiarrythmia. causes an increase in APD and ERP. Moderate reduction in phase 0 slope. binds to inactive sodium channel in a use dependent manner. slow unbinding and binding from receptor - shlows phase 4 depolarisation and automaticity suppression. Uses - ventricular tachyarrythmias, prevention ofparoxysmal reuccrent atrial fib
lidocaine class 1b antiarrythmia. Decrease in APD and ERP. Small reduction in phase 0 upslope. Uses: -During and immediately after MI -Ventricular tachycardias
flecainide class 1c antiarrythmia. Large reduction in phase 0 upstroke and no change in ERP and APD. Suppresses automaticity. Uses: -WPW syndrome -CPVT -Recurrent tachyarrythmias arising in abnormal conduction system. CONTRAINDICATED POST MI BECAUSE CAN DECREASE CONTRACTILITY
Atenolol (antiarrythmia) Class II antiarrythmia. Suppress automaticity (mostly through reduction of sympathetic drive). Reduces rate, conduction and exciteability. Uses: Mainly used in supraventricular tachyarrythmias
Amiodarone Class III antiarrythmia, potassium channel blocker. Delays repolarisation and lengthens AP and ERP. Uses: -WPW -Ventricular tachycardias and atrial fibrilation
Diltiazem antiarrythmia class IV antiarrythmia calcium channel blocker. most effective in nodal tissue. Reduced rate and conduction. Blocks AV node therefore useful for supraventricular tachyarrythmia. Uses: - Prevent recurrence of paroxysmal supraventricular tachycardia - reduce ventricular rate in patients with atrial fib
warfarrin inhibits vit k reductase and stops carboxylation of coagulation factors in the liver. taken orally and rapidly digested by the GI tract. metabolised in the liver T1/2 = 40 hours
heparin anticoagulant. binds antithrombin III. binds both factor IIa and Xa but more potent at factor IIa.
LMW heparin anticoagulant. binds antithrombin III. only binds factor Xa. better because can be given subcutatenously
hirudin, hirugen, bivaldurin AT3 independent anticoagulants. Have fewer bleeding problems than heparin.
ticagrelor reversible P2Y12 receptor antagonist
clopidogrel irreversible p2y12 antagonist. prodrug. given orally. effective in reducing ischaemic strokem MI and vascular death
prasugrel irreversible p2y12 antagonist. faster onset than clopidogrel and greater efficacy
ticlopidine irreversible p2y12 antagonist. slow onset
abciximab/tirfiban IIb/IIa receptor antagonist. used in high risk angioplasty patients with heparin and aspirin
tirofiban/eptifibatide IIb/IIa receptor antagonist. cyclic peptides which resemble IIb/IIa ligands. IV admin
epoprostenol IIb/IIa receptor antagonist. drug version of prostacyclin
dipyridamole IIb/IIa receptor antagonist. cAMP phosphodiesterase inhibitor. increseases camp levels in platelets
streptokinase fibrinolytic. promotes conversion of plasminogen.
alteplase/duteplase fibrinolytic. promotes conversion of plasminogen. short half life so can give IV infusion
reteplase fibrinolytic. promotes conversion of plasminogen. longer half live so given as IV bolus
tranexamic acid antifibrinolytic. Oral or IV admin. used when risk of eg dental extraction
aprotinin anti fibrinolytic. proteolytic enzyme inhibitor of plasmin/kallikrein. used after open heart surgery
compactin hmg coa reducatase inhibitor. lowers cholesterol
mevinolin hmg coa reducatase inhibitor. lowers cholesterol
digoxin heart failure treatment. fast onset and short half life, hypdrophilic - low affinity for serum proteins. inhibitor of the sodium potassium ATPase. causes an increase in CICR. Increased force and exciteability, decreased AV conduction and rate. can also be used as an antiarrythmia to convert atrial flutter to atrial fib
dobutamine beta 1 agonist. MUST BE GIVEN IV. used for reversible HF
Milrinone amrinone sympathomimetic used to treat heart failure. phosphodiesterase inhibitor causes increase in cAMP and increased pka activity.
spironolactone potassium sparing diuretic. weak diuretics. used to treat HF.acts at CT. antagonises aldosterone
furesomide loop diuretic used to treat HF. strong. acts at thick ascending loop of henle.
amiloride potassium sparing diuretic. used to treat heart failure. weak action.
triamterene potassium sparing diuretic used to treat heart failure. blocks a sodium channel
denosumab treatment of osteoporosis. RANKL antibody that inhibits that maturation of osteoclasts
dronates bisphosphonates that inhibit resorption of bone. treatment of osteoporosis
sulphasalazine cheap and commonly first choice of DMARD used to treat RA. sulphapyridine mixed with salicylate. hydrolysed by gut to form sulphapyridine and 5 aminosalicylate. -reduces absorption of antigens from the colon that may promote joint inflammation. -reduces the synthesis of inflammatory mediators
gold used as a dmard to treat RA
methotrexate DMARD used in the treatment of RA. accumulation of adenosine. inhibits activation of t cells. supression of adhesion molecule on surface
glucocorticoids intraarticular injections used to treat RA. inhibit transcription of pro inflammatory cytokines. supresses phospholipase a2 and hence inhibits production of eicosanoids
probenecid treatment of gout. increases uric acid secretion
sulphinpyrazone treatment of gout. increases uric acid secretion
colchicine used to treat gout. inhibits leukocyte migration into joints
tenecteplase (TNK-tPA) fibrinolytic useful in STEMI but may be dangerous in unstable angina or NSTEMI. causes activation of plasminogen to break down fibrin
metaclopramide used after an MI - relieves nausea
what is the characteristic x ray appearance of aortic dissection widening of the mediastinum
fluspiriline calcium channel blocker that may be useful in treating angina
ranolazine used to treat angina. blocks late sodium entry. increases QT interval
losartan AT1 blocker used to treat hypertension. Angiotensin II receptor antagonist. Side effects include hyperkalaemia, diarrhoea, dizziness, tiredness
minoxidil/pinacidil K+ channel activators that cause hyperpolarisation. treatment of hypertension
alpha methyl dopa treatment of hypertension. converted in vesicles to alpha methyl NA. false transmitter at the alpha 1 receptors and binds with more affinity to alpha 2 receptors. reduces renin secretion. not metabolised by MAO
guanendrel treatment of hypertension. normally reserved for uncontrolled hypertension. competes with NA for uptake into vesicles. ganglion blocker
magnesium anti-arrythmia. prevents calcium entry through the sarcolemma.
adenosine anti arrythmia. used for SVT, enhances k+ current in atrial tissue
Ca2+ channel blockers Nifedipine, amlodipine. Hypetension treatments. Side effects include peripheral oedema and dizziness.
Ace inhbiitors prils.
a1 adreno receptor blockers Prazosin and doxasozin, treatment of hypertension. alpha 1 receptors constrict vascular smooth muscle.
K+ channel activators. Minoxidil and pinacidil. K+ channel activators leads to hyperpolarisation of the cardiac smooth muscle cells, leads to less exciteability.
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