Block 31 Pharmacology Flashcards
Thiazide diuretics e.g.s?
- Bendroflumethiazide
- Chlortalidone
- Indapamide
- Metolazone
use of thiazide diuretics?
Hypertension, chronic heart failure, oedema
how do thiazide diuretics work?
inhibiting reabsorption of sodium (Na+) and chloride (Cl−) ions from the distal convoluted tubules in the kidneys by blocking the thiazide-sensitive Na+-Cl− symporter
thiazide like diuretics?
chlorthalidone and metolazone
contraindications of thiazide diuretics?
- Addison’s disease
- hypercalcaemia
- hyponatraemia
- symptomatic hyperuricaemia
side effects of thiazide diuretics?
- dizziness
- electrolyte imbalance
- erectile dysfunction
- hyperglycaemia
- hyperuricaemia
- postural hypotension
diuretics can cause?
gout - hyperuricaemia
drugs used for bacterial endocarditis?
- Benzylpenicillin
- Amoxicillin
- Gentamicin
- Vancomycin
- Flucloxacillin
penicillins mechanism of action?
- binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall
- preventing cross linkage
- causes cell lysis by autolysins
gentamicin mechanism of action?
- aminoglycoside
- inhibits 30S ribosome
vancomycin mechanism?
- glycopeptide
- binds to D-Ala-D-Ala peptide motif of the peptidoglycan precursor
- prevents transglycosylation of the cell wall
side effects of the penicillins?
- hypersensitivity
- nausea
- skin reactions
- thrombocytopenia
- vomiting
cautions for penicillins?
history of allergy
CI of aminoglycosides?
MG - aminoglycosides impair NM transmission
side effects of aminoglycosides
- ototoxicity
- nephrotoxicity
- haemoptysis
- tinnitus
vancomycin CI?
- prev hearing loss w IV use
- abs can be enhanced with inflammatory disorders of intestinal mucosa
side effects of vancomycin?
- nephrotoxicity
- vancomysin infusion reaction
- agranulocytosis
- tinnitus
warfarin mechanism?
- Vit K antanogist
- II, VII, IX, and X have decreased clotting ability
warfarin indications?
- Prevention of venous thromboembolism,
- treatment of DVT and PE,
- myocardial infarction, unstable coronary disease,
- anticoagulation in valvular and nonvalvular AF
warfarin contra-indications?
- haemorrhagic stroke
- sig bleeding
- within 48 hrs post-partum
side effects of warfarin?
- haemorrhage
- Blue Toe syndrome
- skin necrosis
DOACs?
- Apixaban
- Rivaroxaban
- Dabigatran
dabigatran mechanism?
- reversible direct thrombin inhibitor (DTI) that competitively inhibits thrombin - factor IIa
DOAC indications?
- Prevention of venous thromboembolism, treatment of DVT and PE,
- anticoagulation in non-valvular AF
dabigatran CI?
- Antiphospholipid syndrome
- active bleeding
- do not use for prosthetic heart valve
dabigtran side effects?
- haemorrhage
- abn hepatic function
- nausea, diarrhoea, GI discomfort
apixaban CI?
- anti-phospholipid syndrome
- bleeding/ risk of bleeding
- prosthetic HV
SE of apixaban?
- anemia
- haemorrhage
- nausea
- skin reacrions
SE of rivaroxaban?
- hypotension
- menorrhagia
- oedema
- renal impairment
loop diuretics?
- Furosemide
- Bumetanide
indications of loop diuretics?
- Acute pulmonary oedema,
- chronic heart failure,
- diuretic resistant oedema,
- resistant hypertension
Loop diuretics mechanism?
- reduce sodium chloride reabsorption in the thick ascending limb of the loop of Henle.
- This is achieved by inhibiting the Na-K-2Cl carrier
Loop diuretics contra-indications?
- anuria
- severe hypokalaemia
- severe hyponatreamia
hypokalaemiaa and loop diuretics?
- dangerous in severe CV disease and in patients also being treated w cardiac glycosides
side effects of loop diuretics?
- metabolic alkalosis
- dizziness
- muscle spasms
potassoium sparing diuretics examples?
- Amiloride
- Spironolactone
amiloride Mx?
- Amiloride blocks the epithelial sodium channel (ENaC) in the late distal tubule,
- > reduced sodium abs and reduced potassium excretion
amiloride and spironolactone contra-indications?
- addisons
- anuria
- hyperkalaemia
amiloride side effects?
- angina
- arrythmia
- AV block exacerbation
- gout
indications of K+ sparing diuretics?
- Prevention of hypokalaema alongside a loop or thiazide diuretic [e.g. amiloride]
- oedema in cirrhosis of liver,
- severe heart failure,
Conn’s syndrome tx?
aldosterone antagonists
spironolactone mechanism?
- aldosterone antagonist
- promotes sodium and water excretion and potassium retention.
spironolactone side effects?
- AKI
- agranulocytosis
- breast neoplasm benign
- hyperkalaemia - discontinue
BBs examples
“Atenolol Propranolol Bisoprolol”
Beta blockers Indications?
- Angina
- hypertension
- myocardial infarction
- arrhythmias
- heart failure,
-symptomatic relief of thyrotoxicosis, - prophylaxis of migraine
BBs CI ?
- ASTHMA
- hypotension
- bradycardia
- prinzmetal’s angina
- AV block and SSS
- PAD
Side effects of BBs?
- bradycardia
- ED
- heart failure
- PVD
cardioselective BBs?
- atenolol
- bisoprolol
non cardioselective BBs?
- propanolol
- timolol
CCBs?
- Amlodipine
- Felodipine
- Diltiazem
- Verapamil
CCBs mechanism?
- binds to and blocks L type calcium channels
- calcium can’t enter cells -> vasodilation and decreased BP
dihydropyridine CCBs?
- anti-hypertensive properties - potent vasodilaor
- amlodepine
non DHP CCBs?
- verapamil
- diltiazem
CCBs adverse effects?
- Headache
- Flushing
- Dizziness
- Peripheral oedema
- Reduced cardiac contractility
- Constipation
CCB indications?
- Hypertension,
arrhythmias [e.g. verapamil] - angina
CCB CI?
- Cardiogenic shock
- sig AS
- unstable angina
- hypotension
- AV block
ACEi indications?
- Chronic heart failure,
- hypertension,
- diabetic nephropathy,
- prophylaxis of cardiovascular events
ACEi Mx?
- reduced aldosterone secretion - reduced Na+ and water retention
- reduced ADH - reduced water reabs
- reduced vasoconstriction
- reduced sympathetic activity
ACEi side effects - bradykinin?
- dry cough
- due to increase in bradykinin within the lungs (ACE breaks down bradykinin).
side effects of ACEi?
- Headache
- Postural hypotension
- Rashes
- Angio-oedema
- Strongly teratogenic
CI of ACEi?
- angioedema
- AKI
- First dose hypertension
ARBs examples?
Losartan & Candesartan
ARBs mechanism?
- prevention of angiotensin II binding causes vascular smooth muscle relaxation, lowering blood pressure
Ix of ARBs?
- Chronic heart failure,
- hypertension,
- diabetic nephropathy
ARB antagonists CI?
- with aliskiren for AKI and DM
SE of ARBs?
- abd pain
- cough
- hyperkalaemia
- postural hypertension
Alpha blockers?
- Doxazosin
- Tamsulosin (benign prostatic hyperplasia)”
Alpha blockers mechanism?
- blockage of alpha 1 receptors
- Reduced arteriolar tone - lowering peripheral vascular resistance.
- Venous dilation - reducing venous return and cardiac output.
alpha blockers side effects?
- Postural hypotension
- Headaches
- Dizziness
- Nausea
- Rhinitis
- Urinary frequency
CI of Alpha blockers?
- micturition syncope (in patients with benign prostatic hypertrophy);
- postural hypotension
- doxasocin: overflow bladder or anuria
indications of alpha blockers?
- Resistant hypertension,
- prostatic hyperplasia
statins Ix?
reduction of CV risk
statins?
“Simvastatin Atorvastatin Rosuvastatin”
statins mechanism?
- competitively inhibiting HMG-CoA reductase
- reduction of LDL cholestrol
statins cautions?
Risk factors for muscle toxicity, including myopathy or rhabdomyolysis
side effects of statins?
- arthralgia
- GI discomfort
- thrombocytopenia
- muscle complaints
fibrates?
- Bezafibrate
- Fenofibrate
Ix of fibrates?
reduction of CV risk
fibrates mechanism of action?
- Activating PPARs induces the transcription of a number of genes that facilitate lipid metabolism.
- inhibit hepatic synthesis of triglycerides
fibrates CI?
- GB disease
- hypoalbuminaemia
- nephrotic syndrome
fibrate SE?
- decreased appetite
- GI disorder
Ezetemibe Ix?
reduction of CV risk
ezetimibe mechanism?
- blocks NPC1L1 receptor
- cholesterol abs inhibitor
- reduces total cholesterol, LDL, Ao-B
ezetimibe side effects?
- asthenia
- GI discomfort
Parenteral anticoagulants?
- Unfractionated heparin
- Dalteparin
- Fondaparinux
parenteral AC Ix?
- Prevention of venous thromboembolism,
-treatment of DVT and PE, - myocardial infarction,
- unstable coronary disease
UFH mechanism?
- forms a complex wth AT preventing fibrin formation
- inhibition of several activated blood coagulation factors: thrombin (factor IIa), factor IXa, Xa, XIa and XIIa
dalteparin mechanism?
- inc antithombin III activity
- which inhibits factor 2A, and 10A
fondaparinux mechanism?
- selectively INHIBITS FACTOR 10
- Inhibits thrombin formation
fondaparinux CI?
active bleeding and bacterial endocarditis
side effects of fondaparinux?
anemia and haemorrhage
UFH/ dalteparin CI?
- bac endocarditis
- haemophilia/ other haemorrhagic disorders
- recent surgery
- thrombocytopenia
side effects of heparins?
- Haemorrhage
- heparin-induced thrombocytopenia
- skin reactions
BBs Ix?
- Ischaemic heart disease,
- angina,
- hypertension,
- myocardial infarction,
- arrhythmias, heart failure,
- anxiety conditions,
- symptomatic relief of thyrotoxicosis,
-prophylaxis of migraine
tinolol machanism?
- beta 2 blockage -> decreased peripheral resistance
- reduces occular pressure by decreases AH secretion
BBs used in HF?
- Bisoprolol and Carvedilol
Anti-anginals?
- BBs
- CCBs
- nitrates
- nicronadil
- ivabradine
- ransolazine
Nitrates?
- Glyceryl trinitrate (GTN)
- Isosorbide dinitrate
GTN/ Isosorbide dinitrate mechanism?
- relaxation of vascular SM -> vasodilation
- converted to NO
NITRATES CI?
- aortic stenosis
- constrictive pericarditis
- hypertrophic cardiomyopathy
- mitral stenosis
- raised ICP
nitrates are also CI for
toxic pulmonary oedema
side effects of nitrates?
- arrhythmias
- flushing
- cerebral ischaemia
- hypotension
Nicorandil mechanism?
- relaxes vascular SM by increasing CGMP levels
- activates potassium channels causing hyperpolarization -> vasodilation
nicorandil CI?
- acute Pulm oedema
- LV dysfunction
- severe hypotension
- shock and hypovolaemia