stuff Flashcards

Question

``` Class II propranolol bisoprolol metoprolol esmolol ```

Answer 1

^APD anf refactory period in AV node to slow AV conduction velocity decrease phase 4 depolarisation (catecholamine dependent) ECG: ^PR lower HR uses: treating sinus and catecholamine dependent tachycardia converting re-entrant arrhythmias at AV node protecting the ventricles from high atrial rates *bronchospasm hypotension X partial AV block or acute heart failure (are used in stable heart failure)

Answer 2

``` Amiodarone: increase refractory period and ^APD (K+) decrease phase 0 and conduction (Na+) increase threshold decrease phase 4 (beta block and Ca2+ block) decrease speed of AV conduction ``` ECG: ^PR ^QRS ^QT decrease HR Uses: very wide spectrum: effective for most arrhythmias ``` *Pulmonary fibrosis hepatic injury increase LDL thyroid disease photosensitivty optic neuritis (transient blindness) ``` ! may need to reduce dose of digoxin and monitor warfarin more closely Sotalol: ^APD and refractory period in atrial and ventricular tissue slow phase 4 (beta blocker) slow AV conduction ECG: ^QT lower HR uses: wide spectrum: supraventricular and ventricular tachycardia *Proarrhythmia fatigue insomnia

Answer 3

slow conduction through AV (Ca2+) increase refractory period in AV node increase slope of phase 4 in SA to slow HR ECG: ^PR increase/decrease HR depending on BP and baroreflex uses: control ventricles during supraventricular tachycardia convert supraventricular tachycardia (re-entry around AV) *GI (constipation) caution when partial AV block is present - can get asystole if Beta blocker is on board caution with hypotension, decreased cardiac output or sick sinus- slow sinus node

Answer 4

rapid iv bolus natural nucleoside binding to A1 and blocks adenylyl cyclase - reducing cAMP which activates K+ currents in AV and SA causing hyperpolarisation- stopping HR leads to decreased Ca currents- increase refractory period in AV node slows AV conduction uses: convert re-entrant supraventricular arrhythmias diagnosis of coronary artery disease (scans)

Answer 5

Blocks If (funny currents) highly expressed in SA slows SA node but doesn't effect BP uses: reduce inappropriate sinus tachycardia, reduce HR in heart failure and angina (avoiding BP drops) *flashing lights teratogenicity not known

Answer 6

enhances vagal activity (increases k+ currents, decreases Ca currents ^refractory period slows AV conduction and slows HR uses: treatment to reduse ventricular rates in atrial fib and flutter

Answer 7

selective muscarinic antagonist block vagal activity to speed AV conduction and increase HR Uses: treat vagal bradycardia

Answer 8

potent platelet aggregating agent thromboxane A2 (TXA2) formed from arachidonic acid by COX-1 aspirin inhibits COX-1 mediated production of TXA2 and reduces platelet aggregation- irreversible higher doses inhibit endothelial prostacyclin (PGl2) absorbed by passive diffusion- hepatic hydrolysis to salicylic acid *GI irritation, GI bleeding, haemorrhage (stroke), hypersensitivity X reye's syndrome <16, hypersensitivity, 3rd trimester -closure of ductus arteriosus ! other antiplatelet and anticoagulants (additive/synergistic action)

Answer 9

inhibit binding of ADP and P2Y12 receptor -- inhibit activation of GPIIb/IIIa receptors -independent of COX clopidogrel (slower onset) and prasugrel are irreversible - prodrugs with hepatic active metabolites *Bleeding GI upset - dyspepsia and diarrhoea rarely thrombocytopenia X caution in high bleed risk patients with renal and hepatic impairment ! clopidogrel requires CYPs for activation CYP inhibitors - omeprazole, ciprofloxacin, some SSRIs need to concider use of other PPIs with clopidigrel ticagrelor can interact with CYP inhibitors and inducers caution when prescribed with other antiplatelet or anticoagulant

Answer 10

inhibit cellular reuptake of adenosine = increased adenosine = inhibit platelet aggregation via adenosine A2 receptors also acts as phosphodiesterase inhibitor preventing cAMP deg = inhibit expression of GPIIB/IIIa *V+ dizziness ! antiplatelet and anticoags, adenosine

Answer 11

blocks binding of fibrinogen and vWF target final common pathway - more complete platelet aggregation *Bleeding - dose adjust for weight ! caution with other antiplatelet and anticoags

Answer 12

convert plasminogen to plasmin *Bleeding ! antiplatelets and anticoags

Answer 13

anti-metabolite DNA and RNA synthesis *bone marrow suppression malignancy risk risk of infection hepatitis

Answer 14

inhibition of COX decrease prostaglandin, prostacyclin and thromboxane synthesis compete with arachidonic acid for hydrophobic site of COX enzymes Analgesic: Decrease PGE2 synthesis in dorsal horn - decrease neurotransmitter release - decrease excitability of neurones in pain relay pathway Anti-inflammatory: decrease in COX activity = less prostaglandin mediated increase in vasodilation so vasoconstriction and less oedema Antipyretic: inhibition of hypothalamic COX-2 where cytokine induced prostaglandin synthesis is elevated results in a reduction in temperature ``` *Dyspepsia nausea peptic ulcer -less mucus and bicarb ^acid, less blood flow bleeding perforation exacerbation of IBD Renal impairment hypernatremia ``` X elderly, prolonged use, smoking, alcohol, peptic ulcer Hx, h. pylori, CKD, heart failure ! Aspirin, glucocorticoid steroid, anticoag (PPI considered) ACEi, ARBs, diuretics

Answer 15

inhibits COX-2 more than COX-1 less GI ADR does not share antiplatelet action but inhibits PGl2 - potentially leading to unopposed aggregatory effects X increased risk of MI

Answer 16

COX-2 selective inhibition in CNS (spinal cord) NAPQI highly reactive metabolite- some analgesic effect suggested harmless at therapeutic doses- conjugation with glutathione -hepatic glutathione is limited NAPQI highly neucleophilic - oxidising key metabolic enzymes - causing cell death- neurosis and apoptosis

Answer 17

glutathione thiol replacement - gets in hepatocyte

Answer 18

activate cytoplasmic receptors, activated receptor then passes in to nucleus to modify transcription reduces mucosal inflammation, widens airways, reduces mucus reduces symptoms, exacerbations and prevents death *can cause a local immunosuppressive action - candidiasis, hoarse voice X Pneumonia risk in COPD at high doses ! Few if taken correctly

Answer 19

relaxes smooth muscle prevention of bronchoconstriction prior to exercise ``` *Adrenergic- fight or flight effects Tachycardia palpitations anxiety and tremor ^glycogenolysis (liver) ^renin (kidney) SVT ``` X LABA should only be prescribed along ICS, CVD ! beta blockers may reduse effects of B2 agonists

Answer 20

Block CysLT1 at CYSLTR1 that are released by mast cells/eosinophils *headache GI upset dry mouth hyperactivity X used as add on in specific circumstances ! nothing major

Answer 21

block vagally mediated contraction of airway smooth muscle *Infrequent- anticholinergic effects- dry mouth, urinary retension, dry eyes X generally ok

Answer 22

decrease bronchoconstriction X narrow theraputic index - arrhythmia ! CYP450 inhibitors - increase conc

Answer 23

opioid receptor agonist Morphine: metabolism = morphine + glucuronic acid = M6G+M3G ``` *resp depression emesis decreased GI motility ^sphincter tone cardiovascular miosis histamine release -asthma caution ``` Fentanyl: metabolism = CYP3A4 less histamine release *resp depression constipation vomiting Codine: codine -> morphine via CYP2D6 CYP2D6 inhibited by fluoxetine mild analgesia, cough depressant *constipation resp depression - worse in children

Answer 24

buffering in stomach increase stomach content viscosity and reduce reflux *Magnesium salts can cause diarrhoea and aluminium salts cause constipation X Na and K containing preparations caution in renal failure hyperglycaemia in DM ! can reduce absorbtion of many drugs - separate doses increases aspirin excretion

Answer 25

irreversibly inhibit H/K ATPase in gastric parietal cells final stage in pathway- very significant reduction in acid secretion *GI disturbance - abdo pain, constipation diarrhoea Headache, dizziness Drowsiness/confusion X mask symptoms of gastro-oesophageal cancer osteoporosis ! omeprazole CYP inhibitor - reduced clopidogrel action PPIs can increase effects of warfarin and phenytoin - monitor

Answer 26

inhibition of H2 receptors only partial reduction because of other pathways * generally ok, diarrhoea, headache X mask symptoms of gastro-oesophageal cancer, renal impairment ! few ranitidine - possible carcinogen

Answer 27

used for ulcerative colitis release of 5-aminosalsylic acid - reduce inflamation *GI disturbance - nausia, dyspepsia leukopenia X aspirin sensitivity ! enteric coated tablets may break down quicker in presence of PPI

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