- Drug class - angiotensin receptor blocker - Acts on chymases (act on ATII independently of the RAAS pathway) - Common indications - Diabetic nephropathy I type 2 diabetes - Chronic heart failure (when side effects with ACEi) - Hypertension - reduces risk of stroke inputs w hypertension and left ventricular hypertrophy - Hypertension with intravascular volume depletion - Mechanisms of action - reversible and competitively prevents angiotensin 2 binding to the AT1 receptor - Important adverse drug reactions we discussed - abdo pain - Hypotension - Postural hypotension - Nasuea - Dizziess - Headache - Hyperkalaemia - Retail impairment - Vertigo - Vomitting - - Important drug-drug interactions - combination of ATII receptor antagonist with aliskiren (renin inhibitor) is contra indication inpatients with DM - when together it increases the risk of renal impairment - NSAIDs - Alcohol - Drugs that increase potassium

- Drug class - thiazide like diuretic - Common indication - hypertension - At lower doses its more prominent in diuretics. The diuresis effect becomes are apparent with higher doses/ - Mechanism of action - Inhibits the sodium chloride co transporter therefore less is reabsorbed and more water is excreted into the urine. - Important adverse drug reactions - hyperglycaemia, erectile dysfunction, increased LDL and TG, hypercalcaemia, hypokalemia, hyperuricaemia, electrolyte imbalance, fatigue, headache, constipation/diarrhoea, vomitting, postural hypotension, nausea - Important drug-drug interactions - alcohol - can both increase the risk of hypotension - Amplodipin - can increase the risk of hypotension - Aceclofenac - increase the risk of acute renal failure - Allopurinol - increase the risk of hypersensitivity reactions when given with idapamide - Amfampridine, amiodarone, amisulpride - cause hypokalaemia - Contraindicated if history of hypersensitivity to sulfonamides - Why is the drug taken as a single dose in the morning? - if taken too late in the day, you might have to get up during the night to go to the toilet

- drug class - calcium channel blocker - dihydropyridine - Common indications - hypertension, angina, - Mechanism of action - Blocks L type calcium channels, prevents Ca2+ entering cells and therefore stops smooth cell contraction → relaxation and vasodilation. - It’s selective for peripheral vascular use uses therefore on,y targets BVs - Important adverse drug reactions - abdo pain, dizziness, drowsiness, flushing, headache, nausea, palpitations, peripheral oedema, skin reactions, tachycardia, vomitting - Important drug-drug interactions - alcohol - increase risk of hypotension - Simvastatin - amlodipine increases the effect of the stating - Contraindicated in - unstable angine - Severe aortic stenosis (bc CO is already low) - Tissue region and selectivity of the drug and why it’s important when it comes to its therapeutic use? - Because it's peripheral

- drug class - aldosterone receptor antagonist - potassium sparing diuretic - common indications - resistant hypertension - moderate to severe heart failure - oedema in congestive heart failure - nephrotic syndrome - malignant ascites - oedema - ascites in cirrhosis of the lier - mechanism of action - antagonist of aldosterone, therefore stops the production of aldosterone at the CD so sodium isn’t reabsorbed via EnaC and is excreted with water. - Potassium isn’t pumped via ROMK therefore this drug is potassium sparing - important adverse drug reactions - hyperkalaemia - gynaecomastia - acute kidney injury - electrolyte imbalance - GI disorder - malaise - nausea - confusion/dizziness - important drug-drug interactions - other drugs that are potassium sparing/potassium increasing drugs - alcohol - can increase the risk of hypotension - amiloride - they can both increase the risk of hyponatraemia and hyperkalaemia - amlodipine - increase risk of hypotension - ACEi and ARBS - contraindications - pregnancy - renal and hepatic disease - hyperkalaemia - addisons disease - because they already have an adrenal hormone shortage including aldosterone

- drug class - Class IV anti-arrhythmic - Calcium channel blocker - common indications - angina - Supraventricular Arrhythmia - Hypertension - Mechanism of action - stops calcium entry therefore affects the plateau phase of ventricular AP- less steep slope so slower heart rate - Separates/depresses SA node and slow AV conduction therefore negative inotropy - Important adverse drug reactions - constipation - Bradycardia - Heart block - Cardiac failure - Palpitations - Important drug-drug interactions - beta blockers - Other anti hypertensive and anti arrhythmic drugs - Contraindications - Poor liver function - AV nodal conduction delay - atrial flutter or fibrillation associated with accessory conducting pathways (e.g. Wolff-Parkinson-White-syndrome

- drug class - class III antiarrhythmic - common indications - arrhythmias, esp when other drugs are ineffective or contraindicated - arrhythmias associated with wolf parkinson white syndrome - ventricular fibrillation or pulseless ventricular tachycardia refractor to defibrillation - mechanism of action - block potassium channels - increases action potential duration - prolongs phase 3 and refractory period - prevents early after depolarisations - slows down heart - important adverse drug reactions Restrictive pathology - pulmonary fibrosis, hepatic injury, increase LDL, thyroid disease, photosensitivity, optic neuritis - arrhythmias, hepatic disorders, hyperthyroidism, nausea, respiratory disorders, skin reactions - important drug-drug interactions - amiodarone has a long half life so there is potential for drug interactions to occur for several weeks (or even months) after treatment has been stopped - digoxin - warfarin - atenolol - biaoprolol - contraindications - avoid in severe conduction disturbances (unless pacemaker is fitted) - severe resp failure - severe arterial hypotension - unusual pharmacokinetics and why it is contraindicated in thyroid disease - can lead to the inhibition of T4 and T3 entry into the peripheral tissues - It contains iodine - therefore can causes hyper/hypothyroidism

- drug class - cholesterol absorption inhibitor - common indications - primary hypercholesterolaemia - if statin inappropriate or not tolerated - Hyperlipidaemia - mechanism of action - inhibits NPC1L1 transporter at brush border in small intestines - reduces absorption of cholesterol by the gut - Hepatic LDL receptor expression increases → decrease total cholesterol and LDL - it’s a pro drug - relies on hepatic metabolism to be converted to active form - it undergoes enterohepatic circulation → limits systemic exposure so it stays locally - secreted by bile - important adverse drug reactions - abdominal pain, GI upset, angioedema, headache, asthenia - important drug-drug interactions - mindful if prescribed with statin - theoretical increased risk of rhabdomyolysis - contraindications - hepatic failure - pregnancy - only give if benefits>risks - administration of drug !!! given in single dose

- Drug class - SGLT-2 inhibitors - gliflozins (urine flows out) - Common indications - T2DM - as mono therapy if metformin inappropriate - T2DM - in combination with insulin or other antidiabetic drug - Mechanism of action - decrease glucose absorption from tubular filtrate in PCT, increases urinary glucose excretion - Important adverse drug reactions - UTI (because glucose retention), genital infection, polydipsia and polyuria, pancreatitis? - Important drug-drug interactions - Antihypertensive and other hypoglycaemic agents - Contraindications/warnings - - hypovolaemia - possible hypotension - Avoid initiation if eGFR < 15mL/min - Consider additional antidiabetic drug with dapagliflozin if eGFR < 45mL/min

- drug class - ADP receptor antagonist - Common indications - Prevention of atherothrombotic regents in percutaneous coronary intervention (adjunct w/aspirin) in patients not already on clopidogrel - Transient/acute ischaemic attack for patients with aspirin hypersensitivity, or those intolerant fo aspirin despite the addition of a proton pump inhibitor - Mechanism of action - inhibits binding of ADP to P2Y12 receptor → inhibits the activation of GPIIb/IIIa receptors (independent of COX pathway) - Important adverse drug reactions - bleeding, GI upset - dyspepsia and diarrhoea, haemorrhage, skin reactions - Rarely - thrombocytopenia - Important drug-drug interactions - clopidogrel requires CYPs for activation so - bc it’s a pro drug - Any CYP inhibitors - omeprazole, cirpofloxacin, erthromycin, some SSRIs - Need to consider the use of other PPIs with clopidogrel - Caution when co prescribes with other antiplatelet and anticoagulants or NSAIDs - increased bleeding risk - Contraindications - Caution in high bleed risk patients with renal/hepatic impairment - Avoid in pregnancy - Discontinue 7 days before elective surgery - Careful in elderly - who have significant bleeding risk, such as uncontrolled severe hypertension, bleeding diathesis or recent non-trivial spontaneous bleeding - How if differs to other drugs with the same mechanism of action? - compared to ticagrelor and prasugrel, clopidogrel has a slow onset of action without a loading dose - there’s some inter-individual variability in antiplatelet action

- drug class - Glucagon like peptide 1 receptor agonist (incretin mimetics) - common indications - Type 2 DM as mono therapy (if metformin inappropriate) or in combo with other antidiabetic drug incl insulin if existing treatment fails to achieve adequate glycaemic control - Mechanism of action and route of administration - subcutaneous injection - It binds to and activates the GLP-1 receptor to increase insulin secretion, suppress glucagon secretion and slow gastric emptying - Resistant to degradation but DPP-4 because they’re modified components - Important adverse drug reactions - GI upset, decreased appetite with weight loss - Warnings - renal impairment - Important drug-drug interactions - other hypoglycaemic drugs

- drug class - Sodium channel blocker - class 1c - Anti arrhythmic - Common indications - supraventricular arrhythmia (fibrillation and flute) - Ventricular arrhythmia - Wolff Parkinson white syndrome - Mechanism of action - acts to increase the refractory period, slower depolarisation of cardiac cells and slow heart rate - Increase APD (k+) - Decrease automaticity (increase threshold) - AP shifts to right and doing this multiple times to try and reestablish sinus rhythm - common adverse effects - Arrhythmia, asthenia, dizziness, dyspnoea, fever, oedema, vision disorders - ‘flecainide flutter’ - increase ventricular response to supraventricular arrhythmias - Common drug-drug interactions amiodarone increases the concentration of flecainide

- drug class - Cyclo-oxygenase inhibitor (COX1) - Common indications - some AF patients post stroke - Secondary prevention of stroke and TIA - Secondary prevention of stroke and TIA - Post primary percutaneous coronary intervention and stent to reduce ischaemic complications - Often co prescribed with other antiplatelet agents - NSTEMI/STEMI - chewable is best - GI protection requires for long term use in at risk patients (proton pump inhibitor) - Mechanism of action - it inhibits COX-1 mediated production of TXA2 and reduced platelet aggregation - irreversible - common adverse drug reactions - GI irritation, GI bleeding (peptic ulcer), haemorrhage (stroke), hypersensitivity, dyspepsia - common drug-drug interactions - Other antiplatelet and anticoagulants (additive/synergistic action) - Reye’s syndrome - avoid <16 years, avoid if breastfeeding: regular uses of high doses could impair platelet function and produce hypothrombinaemia in infant if neonatal vitamin K stores are low - Reyes = Permanent brain and over damage - can cause seizures and fits - But can give to kids who have Kawasaki disease - Hypersensitivity - 3rd trimester - premature closure of ductus arteriosus

- drug class - Selective COX 2 inhibitor - Selective - to avoid GI side effects (but there still are risks of GI side effects) - Common indications - pain and inflammation in OA, rheumatoid arthritis, ankylosing spondylitis - Mechanism of action - blocks COX2 therefore inhibits PGI2 - Avoids inhibition of homeostatic actions mediated by COX 1 - Common adverse side effects (come back pls) - Increased risk of MI (bc stops platelet aggregation) - GI (less ? to COX 1 inhibitor?) and renal effects - Common drug-drug interactions - Aciclovir - increase risk of nephrotoxicity - Aspirin - increase risk of bleeding (decrease platelet aggregation)

- drug class - immunosuppressant (non-biologic) - common drug indications? - SLE and vasculitis - as maintenance therapy - RA (weak evidence) - IBD - autoimmune conditions - severe Crohn’s - other uses as a ‘steroid sparing’ drug - mechanism of action? - it’s cleaved into 6-mercaptopurine by TPMT - a metabolite that blocks purine and therefore DNA synthesis so inflammatory cells get inhibited. - TPMT has a variable expression in different people so have to test TPMT activity before prescribing - if high levels, then the drug will have a high effect - common adverse reactions? - bone marrow suppression - monitor FBC - increased risk of malignancy - esp in transplant patients - increased risk of infections - hepatitis - monitor LFTs - leucopenia - pancreatitis - thrombocytopenia - risk of myelosuppression is increased in patients with reduced activity of the TPMT enzyme - common drug-drug interactions? - HPV vaccine, live and influenza vaccine (live) and MMR vaccine (live) - predicted to increase the risk of generalised infection when any of these are given with this drug - ramipril - increase risk of anaemia/leucopenia - contraindications? when used for severe refractory eczema - absent TPMT activity

drugs Flashcards by Iyman Janjua

ARDs of Losartan?

Drug class
- angiotensin receptor blocker
- Acts on chymases (act on ATII independently of the RAAS pathway)
Common indications
- Diabetic nephropathy I type 2 diabetes
- Chronic heart failure (when side effects with ACEi)
- Hypertension - reduces risk of stroke inputs w hypertension and left ventricular hypertrophy
- Hypertension with intravascular volume depletion
Mechanisms of action
- reversible and competitively prevents angiotensin 2 binding to the AT1 receptor
Important adverse drug reactions we discussed
- abdo pain
- Hypotension
- Postural hypotension
- Nasuea
- Dizziess
- Headache
- Hyperkalaemia
- Retail impairment
- Vertigo
- Vomitting
Important drug-drug interactions
- combination of ATII receptor antagonist with aliskiren (renin inhibitor) is contra indication inpatients with DM - when together it increases the risk of renal impairment
- NSAIDs
- Alcohol
- Drugs that increase potassium

How well did you know this?

Not at all

Perfectly

ARDs of Indapamide?

Drug class
- thiazide like diuretic
Common indication
- hypertension
- At lower doses its more prominent in diuretics. The diuresis effect becomes are apparent with higher doses/
Mechanism of action
- Inhibits the sodium chloride co transporter therefore less is reabsorbed and more water is excreted into the urine.
Important adverse drug reactions
- hyperglycaemia, erectile dysfunction, increased LDL and TG, hypercalcaemia, hypokalemia, hyperuricaemia, electrolyte imbalance, fatigue, headache, constipation/diarrhoea, vomitting, postural hypotension, nausea
Important drug-drug interactions
- alcohol - can both increase the risk of hypotension
- Amplodipin - can increase the risk of hypotension
- Aceclofenac - increase the risk of acute renal failure
- Allopurinol - increase the risk of hypersensitivity reactions when given with idapamide
- Amfampridine, amiodarone, amisulpride - cause hypokalaemia
- Contraindicated if history of hypersensitivity to sulfonamides
Why is the drug taken as a single dose in the morning?
- if taken too late in the day, you might have to get up during the night to go to the toilet

How well did you know this?

Not at all

Perfectly

ARDs of amlodipine?

drug class
- calcium channel blocker - dihydropyridine
Common indications
- hypertension, angina,
Mechanism of action
- Blocks L type calcium channels, prevents Ca2+ entering cells and therefore stops smooth cell contraction → relaxation and vasodilation.
- It’s selective for peripheral vascular use uses therefore on,y targets BVs
Important adverse drug reactions
- abdo pain, dizziness, drowsiness, flushing, headache, nausea, palpitations, peripheral oedema, skin reactions, tachycardia, vomitting
Important drug-drug interactions
- alcohol - increase risk of hypotension
- Simvastatin - amlodipine increases the effect of the stating
Contraindicated in
- unstable angine
- Severe aortic stenosis (bc CO is already low)
Tissue region and selectivity of the drug and why it’s important when it comes to its therapeutic use?
- Because it’s peripheral

How well did you know this?

Not at all

Perfectly

ARDs of Atorvastatin?

drug class
- statins
common indications
- Primary hypercholesterolaemia in patients who haven’t responded adequately to diet and other measures
- heterozygous and homozygous familial hypercholesterolaemia in patients who haven’t responded adequately to diet and other measures
- primary prevention of cardiovascular events in pts at high risk of a first cardiovascular event
- secondary prevention of cardiovascular events
mechanism of action
- they competitively inhibit HMG CoA reductase which is an enzyme involved in cholesterol synthesis esp in the liver
- therefore can’t make cholesterol.
- as cholesterol is then low, LDLs will be taken up to distribute cholesterol to cells - decreasing the cholesterol levels, decreases the chances of a CV event
important adverse drug reactions
- arthralgia (joint stiffness), asthenia (weakness, lack of energy and strength), memory loss, pancreatitis, paraesthesia, sexual dysfunction, skin reactions, vomiting
important drug-drug interactions
- Acipimox - increases the risk of rhabdomyolosis when given with this drug
- alcohol - increase the risk of hepatotoxicity
- aprepitant - increase the exposure of atorvastatin (monitor and adjust dose)
- amlodipine - effect of atorvastatin increased
- macrolides, amiodarone - ABs increase the effect of statins
contraindicated
- pregnancy, hepatic or renal failure, breastfeeding

How well did you know this?

Not at all

Perfectly

Spironolactone

drug class
- aldosterone receptor antagonist
- potassium sparing diuretic
common indications
- resistant hypertension
- moderate to severe heart failure
- oedema in congestive heart failure
- nephrotic syndrome
- malignant ascites
- oedema
- ascites in cirrhosis of the lier
mechanism of action
- antagonist of aldosterone, therefore stops the production of aldosterone at the CD so sodium isn’t reabsorbed via EnaC and is excreted with water.
- Potassium isn’t pumped via ROMK therefore this drug is potassium sparing
important adverse drug reactions
- hyperkalaemia
- gynaecomastia
- acute kidney injury
- electrolyte imbalance
- GI disorder
- malaise
- nausea
- confusion/dizziness
important drug-drug interactions
- other drugs that are potassium sparing/potassium increasing drugs
- alcohol - can increase the risk of hypotension
- amiloride - they can both increase the risk of hyponatraemia and hyperkalaemia
- amlodipine - increase risk of hypotension
- ACEi and ARBS
contraindications
- pregnancy
renal and hepatic disease
hyperkalaemia
addisons disease - because they already have an adrenal hormone shortage including aldosterone

How well did you know this?

Not at all

Perfectly

Verapamil

drug class
- Class IV anti-arrhythmic
- Calcium channel blocker
common indications
- angina
- Supraventricular Arrhythmia
- Hypertension
Mechanism of action
- stops calcium entry therefore affects the plateau phase of ventricular AP- less steep slope so slower heart rate
- Separates/depresses SA node and slow AV conduction therefore negative inotropy
Important adverse drug reactions
- constipation
- Bradycardia
- Heart block
- Cardiac failure
- Palpitations
Important drug-drug interactions
- beta blockers
- Other anti hypertensive and anti arrhythmic drugs
Contraindications
- Poor liver function
AV nodal conduction delay
atrial flutter or fibrillation associated with accessory conducting pathways (e.g. Wolff-Parkinson-White-syndrome

How well did you know this?

Not at all

Perfectly

Amiodarone

drug class
- class III antiarrhythmic
common indications
- arrhythmias, esp when other drugs are ineffective or contraindicated
- arrhythmias associated with wolf parkinson white syndrome
- ventricular fibrillation or pulseless ventricular tachycardia refractor to defibrillation
mechanism of action
- block potassium channels
- increases action potential duration
- prolongs phase 3 and refractory period
- prevents early after depolarisations
- slows down heart
important adverse drug reactions
Restrictive pathology
- pulmonary fibrosis, hepatic injury, increase LDL, thyroid disease, photosensitivity, optic neuritis
- arrhythmias, hepatic disorders, hyperthyroidism, nausea, respiratory disorders, skin reactions
important drug-drug interactions
- amiodarone has a long half life so there is potential for drug interactions to occur for several weeks (or even months) after treatment has been stopped
- digoxin
- warfarin
- atenolol
- biaoprolol
contraindications
- avoid in severe conduction disturbances (unless pacemaker is fitted)
- severe resp failure
- severe arterial hypotension
unusual pharmacokinetics and why it is contraindicated in thyroid disease
- can lead to the inhibition of T4 and T3 entry into the peripheral tissues
It contains iodine - therefore can causes hyper/hypothyroidism

How well did you know this?

Not at all

Perfectly

Ezetimibe

drug class
- cholesterol absorption inhibitor
common indications
- primary hypercholesterolaemia - if statin inappropriate or not tolerated
- Hyperlipidaemia
mechanism of action
- inhibits NPC1L1 transporter at brush border in small intestines
- reduces absorption of cholesterol by the gut
- Hepatic LDL receptor expression increases → decrease total cholesterol and LDL
- it’s a pro drug - relies on hepatic metabolism to be converted to active form - it undergoes enterohepatic circulation → limits systemic exposure so it stays locally
- secreted by bile
important adverse drug reactions
- abdominal pain, GI upset, angioedema, headache, asthenia
important drug-drug interactions
- mindful if prescribed with statin - theoretical increased risk of rhabdomyolysis
contraindications
- hepatic failure
- pregnancy - only give if benefits>risks
administration of drug !!!
given in single dose

How well did you know this?

Not at all

Perfectly

Dapagliflozin

Drug class
- SGLT-2 inhibitors - gliflozins (urine flows out)
Common indications
- T2DM - as mono therapy if metformin inappropriate
- T2DM - in combination with insulin or other antidiabetic drug
Mechanism of action
- decrease glucose absorption from tubular filtrate in PCT, increases urinary glucose excretion
Important adverse drug reactions
- UTI (because glucose retention), genital infection, polydipsia and polyuria, pancreatitis?
Important drug-drug interactions
- Antihypertensive and other hypoglycaemic agents
Contraindications/warnings
- - hypovolaemia - possible hypotension
Avoid initiation if eGFR < 15mL/min
Consider additional antidiabetic drug with dapagliflozin if eGFR < 45mL/min

How well did you know this?

Not at all

Perfectly

Clopidogrel

drug class
- ADP receptor antagonist
Common indications
- Prevention of atherothrombotic regents in percutaneous coronary intervention (adjunct w/aspirin) in patients not already on clopidogrel
- Transient/acute ischaemic attack for patients with aspirin hypersensitivity, or those intolerant fo aspirin despite the addition of a proton pump inhibitor
Mechanism of action
- inhibits binding of ADP to P2Y12 receptor → inhibits the activation of GPIIb/IIIa receptors (independent of COX pathway)
Important adverse drug reactions
- bleeding, GI upset - dyspepsia and diarrhoea, haemorrhage, skin reactions
- Rarely - thrombocytopenia
Important drug-drug interactions
- clopidogrel requires CYPs for activation so - bc it’s a pro drug
- Any CYP inhibitors - omeprazole, cirpofloxacin, erthromycin, some SSRIs
- Need to consider the use of other PPIs with clopidogrel
- Caution when co prescribes with other antiplatelet and anticoagulants or NSAIDs - increased bleeding risk
Contraindications
- Caution in high bleed risk patients with renal/hepatic impairment
- Avoid in pregnancy
- Discontinue 7 days before elective surgery
- Careful in elderly - who have significant bleeding risk, such as uncontrolled severe hypertension, bleeding diathesis or recent non-trivial spontaneous bleeding
How if differs to other drugs with the same mechanism of action?
- compared to ticagrelor and prasugrel, clopidogrel has a slow onset of action without a loading dose - there’s some inter-individual variability in antiplatelet action

How well did you know this?

Not at all

Perfectly

Semaglutide

drug class
- Glucagon like peptide 1 receptor agonist (incretin mimetics)
common indications
- Type 2 DM as mono therapy (if metformin inappropriate) or in combo with other antidiabetic drug incl insulin if existing treatment fails to achieve adequate glycaemic control
Mechanism of action and route of administration
- subcutaneous injection
- It binds to and activates the GLP-1 receptor to increase insulin secretion, suppress glucagon secretion and slow gastric emptying
- Resistant to degradation but DPP-4 because they’re modified components
Important adverse drug reactions
- GI upset, decreased appetite with weight loss
- Warnings - renal impairment
Important drug-drug interactions
- other hypoglycaemic drugs

How well did you know this?

Not at all

Perfectly

Flecainide

drug class
- Sodium channel blocker - class 1c
- Anti arrhythmic
Common indications
- supraventricular arrhythmia (fibrillation and flute)
- Ventricular arrhythmia
- Wolff Parkinson white syndrome
Mechanism of action
- acts to increase the refractory period, slower depolarisation of cardiac cells and slow heart rate
- Increase APD (k+)
- Decrease automaticity (increase threshold)
- AP shifts to right and doing this multiple times to try and reestablish sinus rhythm
common adverse effects
- Arrhythmia, asthenia, dizziness, dyspnoea, fever, oedema, vision disorders
- ‘flecainide flutter’ - increase ventricular response to supraventricular arrhythmias
Common drug-drug interactions
amiodarone increases the concentration of flecainide

How well did you know this?

Not at all

Perfectly

Aspirin

drug class
- Cyclo-oxygenase inhibitor (COX1)
Common indications
- some AF patients post stroke
- Secondary prevention of stroke and TIA
- Secondary prevention of stroke and TIA
- Post primary percutaneous coronary intervention and stent to reduce ischaemic complications
- Often co prescribed with other antiplatelet agents
- NSTEMI/STEMI - chewable is best
- GI protection requires for long term use in at risk patients (proton pump inhibitor)
Mechanism of action
- it inhibits COX-1 mediated production of TXA2 and reduced platelet aggregation - irreversible
common adverse drug reactions
- GI irritation, GI bleeding (peptic ulcer), haemorrhage (stroke), hypersensitivity, dyspepsia
common drug-drug interactions
- Other antiplatelet and anticoagulants (additive/synergistic action)
Reye’s syndrome - avoid <16 years, avoid if breastfeeding: regular uses of high doses could impair platelet function and produce hypothrombinaemia in infant if neonatal vitamin K stores are low
Reyes = Permanent brain and over damage - can cause seizures and fits
But can give to kids who have Kawasaki disease
Hypersensitivity
3rd trimester - premature closure of ductus arteriosus

How well did you know this?

Not at all

Perfectly

Celecoxib

drug class
- Selective COX 2 inhibitor
- Selective - to avoid GI side effects (but there still are risks of GI side effects)
Common indications
- pain and inflammation in OA, rheumatoid arthritis, ankylosing spondylitis
Mechanism of action
- blocks COX2 therefore inhibits PGI2
- Avoids inhibition of homeostatic actions mediated by COX 1
Common adverse side effects (come back pls)
- Increased risk of MI (bc stops platelet aggregation)
- GI (less ? to COX 1 inhibitor?) and renal effects
Common drug-drug interactions
- Aciclovir - increase risk of nephrotoxicity
Aspirin - increase risk of bleeding (decrease platelet aggregation)

How well did you know this?

Not at all

Perfectly

Azathioprine

drug class
- immunosuppressant (non-biologic)
common drug indications?
- SLE and vasculitis - as maintenance therapy
- RA (weak evidence)
- IBD
- autoimmune conditions
- severe Crohn’s
- other uses as a ‘steroid sparing’ drug
mechanism of action?
- it’s cleaved into 6-mercaptopurine by TPMT - a metabolite that blocks purine and therefore DNA synthesis so inflammatory cells get inhibited.
- TPMT has a variable expression in different people so have to test TPMT activity before prescribing - if high levels, then the drug will have a high effect
common adverse reactions?
- bone marrow suppression - monitor FBC
- increased risk of malignancy - esp in transplant patients
- increased risk of infections
- hepatitis - monitor LFTs
- leucopenia
- pancreatitis
- thrombocytopenia
- risk of myelosuppression is increased in patients with reduced activity of the TPMT enzyme
common drug-drug interactions?
- HPV vaccine, live and influenza vaccine (live) and MMR vaccine (live) - predicted to increase the risk of generalised infection when any of these are given with this drug
- ramipril - increase risk of anaemia/leucopenia
contraindications?
when used for severe refractory eczema - absent TPMT activity

How well did you know this?

Not at all

Perfectly

Salbutamol

Study These Flashcards

drug class
- B2 agonist
common indications
- asthma
- prophylaxis of allergen - or exercise induced bronchospasm
- uncomplicated premature labour (between 22 and 37 weeks of gestation - specialist supervision under hospital)
mechanism of action !
- binds to b2 adrenoreceptor, which is a G alphaS GPCR, cAMP → AMP, increase in calcium release
- bronchodilator
important adverse drug reactions
- arrhythmias, headache, palpitations, tremor, muscle cramps,
important drug-drug interaction
- clarithromycin - predicted to cause hypokalaemia when given with salbutamol
- beta blockers - because they antagonise each other and there for decrease the effects
what distinguishes this drug pharmacodynamically from others in the broader drug class?

Fentanyl

Study These Flashcards

drug class
- Opioid
Common indications
- Analgesia
- Antitussive
- Dyspnoea caused by pulmonary oedema
- Pallitation
Mechanism of action
- U receptor against
- Highly lipid soluble
Common adverse effects
- constipation, drowsiness, dysphoria, euphoria, flushing, headache, hyperhydrosis, mitosis, nausea, respiratory depression, itching, urinary retention
Warnings and common drug to drug interactions
- warnings: comatose patients, head injury or raised ICP, respiratory depression, paralytic lieu’s, aromatics
- Caution in pregnancy
- Contraindications: CNS depressants, inc anti epileptic drugs, benzodiazepines, other options containing drugs, drugs that cause reduced drug mortality, clarithtomycin, optioid receptor antagonist?
How it differs to other drugs in this class?
given transdermally - provides analgesic effect for a couple of B days

Theophylline

Study These Flashcards

drug class?
- Methylxanthine
common indications?
- chronic poorly controlled asthma
- reversible airway obstruction
- severe acute asthma
- taken orally
mechanism of action?
- adenosine receptor antagonist
- decrease bronchoconstriction
- PDE inhibitor
common adverse drug reactions?
- narrow therapeutic index therefore difficult to use
- potentially life threatening complications including arrhythmia - must measure plasma concentration
- anxiety, diarrhoea, dizziness, GI discomfort, GORD, headaches, nausea, tremor
common drug to drug interactions?
- CYP450 inhibitors - increase concentrations of theophylline
- smoking - can increase theophylline clearance and increased doses of theophylline are therefore required

Metoclopramide

Study These Flashcards

drug class
- D2 receptor antagonist
common indications
- symptomatic treatment of nausea and vomiting including that associated with acute migraine
- hiccup & N+V in palliative care
- acute migraine
- GORG, ileus (where there’s no inflammation bc bowel is inflamed
- Post op/op chemo N+V
mechanism of action
- blocks D2 receptor, increases ACh at muscarinic receptors in the gut to promote gastric emptying and increase peristalsis
common adverse drug reactions/warnings
- depression, diarrhoea, drowsiness, hypotension, galactorrhea, extra-pyramidal effects - dystonia, Parkinsonism (due to lack of dopamine)
- post surgery, GI obstruction, GI perforation, GI haemorrhage
common drug-drug interactions
other dopamine antagonists, levodopa (Parkinson’s medicine)

Omeprazole

Study These Flashcards

drug class
- proton pump inhibitor
mechanism of action
- irreversibly inhibits the H+/K+ATPase in gastric parietal cells.
- targets the final stage in the pathway therefore produces a very significant reduction in acid secretion
common indications
- GORD, peptic ulcerations (prescribed with NSAIDs because of risk of ulceration
common adverse drug effects/warnings
- GI disturbances - abdo pain, constiaption, diarrhoea
- headache, dizziness
- drowsiness/confusion - esp in elderly patients
- masks symptoms of. gastro-oesophageal cancers
- osteoporosis - fracture risk
- Hyponatraemia
- Increase risk of C.diff
common drug to drug interactions
- omeprazole CYP inhibitor - reduced clopidogrel (blood thinner) action
- PPIs can increase effects of warfarin and phenytoin - monitor (can give unwanted side effects)

Ondansetron

Study These Flashcards

drug class
- 5HT3 receptor antagonist
- Antiemetic
Mechanism of action
- blocks 5HT3 receptors in the GI tract and CNS
- Acts centrally to inhibit CTZ
- acts peripherally to reduce gut motility and secretions
Common indications
- Post op and chemo induced nausea and vomiting
Common adverse drug reactions
- headache, GI upset, elevated liver enzymes, long QT syndrome
Common drug to drug interactions
- other drugs with risk of long QT syndrome

Apixaban

Study These Flashcards

Drug class
- direct acting oral anticoagulants
- direct inhibitor of activated factor X (Xa).
Common indications
- treatment of DVT
- treatments of pulmonary embolism
- VTE
- AF
mechanism of action
- direct Xa (anything distal to Xa is cut off) - inhibits both free Xa and that bound with ATIII, doesn’t directly effect thrombin (IIa)
- hepatic metabolism and excreted partly by kidneys
common adverse drug effects/warnings
- bleeding, skin reactions
- caution and dose adjustments esp in GI bleed risk groups
contraindications
- (dabigatran contraindicated in low creatine clearance)
- others are at very low creatinine clearance
- avoid in pregnancy and breastfeeding
- avoid in conditions with significant risk factors for major bleeding, incl current/recent GI ulceration, recent brain or spinal surgery etc
common drug to drug interactions
- less frequent interactions than warfarin but affected by CYP inhibitors and inducers
- reduced by carbamazepine, phenytoin, barbituates
- Plasma concentration increased by macrolides (eg clarythromycin)

pro - Don’t have to monitor doacs

Dalteparin

Study These Flashcards

Drug class
- low molecular weight heparin ( how long the chain is)
Common indications
- Treatment of DVT, pulmonary embolism, unstable coronary artery disease
- Subcutaneous
- Thromboprophylaxis, VTE, ACS
Mechanism of action
- inhibition of Xa specifically by enhancing ATIII activity but doesn’t inactivate thrombin (IIa) because it’s not long enough (unfractioned heparin is longer)
Common adverse drug effects
- Haemorrhage, heparin induced thrombocytopenia, skin reactions, bruising, hyperkalaemia
Common drug to drug interactions
- amiloride - increase risk of hyperkalaemia
- Aspirin - both can cause bleeding
- Other antithrombotic drugs
- ACE inhibitors
- K sparing drugs

Warfarin

Study These Flashcards

drug class
- Vitamin K antagonist
common indications
- venous thromboembolism
- PE
  DVT and secondary prevention
- superficial vein thrombosis
- AF patients where DOAC not suitable or already taking warfarin
- heart valve replacement - bio prosthetic and some mechanical
- generally used in long term anticoagulation compared to heparins
mechanism of action
- inhibits activation of vitamin K dependant clotting factors
- inhibits conversion of vitamin K to active reduced form - competitive inhibitor of VKOR
- (hepatic synthesis of clotting factors II, VII, IX and X required vitamin K as cofactor for activation)
- Less clotting factors means you can’t make the end product fibrin
Important adverse drug reactions
- crosses the placenta - avoided if possible, esp in 1st trimester (teratogenic)
- haemorrhage
- epistaxis and spontaneous retroperitoneal bleeding
reversal of warfarin?
- first option - vitamin k1
- prothrombin complex concentrate - IV
- stop warfarin
- have to consider stopping warfarin when patient having surgery
- use bridging therapy with LMWH when temporarily stopping warfarin as can control heparin better during intraoperative period and then you start up warfarin again later
important drug-drug interactions
- CYP2C9
vitamin K intake
alcohol
NSAIDS and drugs that decrease GI absorption vitamin K → displace warfarin from plasma albumin and likely increase INR therefore more at risk of bleeding
cephalosporin antibiotic - interrupts gut microbiome which disrupts the way that vitamin K is broken down/produced from dietary foods
barbiturates, phenytoin, rifampicin, st johns wort → acceleration of warfarin metabolism so likely to decrease INR and therefore not anticoagulated enough

Co-carelodpa

- drug class - dopamine agonist - peripheral dopa decarboxylase inhibitor. - common indications? - Parkinson’s disease with levodopa - reduces the dosage of levodopa needed reduces side effects - mechanism of action? - blocks peripheral dopa decarboxylase which therefore inhibits levodopa metabolism in the gut and peripheries - more levodopa then crosses blood brain barrier and reaches the brain - important adverse drug reactions? - drowsiness, seizure, sleep disorder, hallucinations, slow loss of efficacy over time, NMS (neuroleptic malignant syndrome) if stopped suddenly - nausea and vomiting - tachycardia - impulse control disorders - pathological gambling, binge eating, hyperrsexuality - important drug-drug interactions? - **pyridoxine (vit B6)** - increases peripheral breakdown. of levodopa - **Monoamine oxidase inhibitors (MAOIs)** - risk hypertensive crisis - **antipsychotic** drugs can block dopamine receptors → Parkinsonism as a side effect

Levetriacem

- drug class - anti epileptic - common indications? - **focal seizures** including secondary generalisation - off label for **status epilepticus** - 2nd line. - one of the safer options in pregnancy (as not teratogenic) and generally well tolerated - mechanism of action? - **inhibition of synaptic vesicle protein 2A (SV2A)** - (control the release of glutamate) - decreased synchronised burst firing without effecting neuronal excitability - important adverse drug reactions? - **anxiety**, appetite decreased, asthenia, behaviour abnormal, cough, depression - **drowsiness**, **dizziness** - QT interval prolonging risk factors - increased risk of somnolence (state of drowsiness) - important drug-drug reactions? - alcohol - CNS depressant effects, can affect the ability to perform skilled tasks - CNS depressants

Lorazepam

- drug class - Benzodiazepine - common indications - anxiety - short term insomnia associated with anxiety - acute panic attack - **status epilepticus - IV** - mechanism of action - potentiate GABA activity at GABAa receptors - positive allosteric modualtors - hyperpolarisation of cell via increased Cl- efflux - phase 2 metabolism scone be better in hepatic dysfunction - important adverse drug reactions - ataxia - depression - drowsienss - hypotension - muscle weakness - sleep disorders - respiratory depression at high doses (warning) - important drug-drug interactions other CNS depressants

drugs Flashcards

(27 cards)