GP Pharmacology Flashcards
B2-agonists (SABA, LABA) MOA
Smooth muscle relaxation
Improves airflow in constricted airways, reducing breathlessness
SABA (e.g. salbutamol) indications and dose
First-line relief of breathlessness in COPD and asthma
100-200 micrograms up to 4 times/day
1 puff = 100 micrograms
B2-agonist side effects
Tachycardia Palpitations Anxiety Tremor Muscle cramps (LABA)
LABA (e.g. salmeterol) indications
Chronic asthma, when ICS alone insufficient (must be given with ICS)
Second-line to reduce symptoms/exacerbations in COPD
B-2 agonists interactions
Beta blockers can reduce efficacy of SABA/LABA
SAMA (ipratropium bromide) indications
COPD = first line to reduce exacerbations
Asthma = in acute exacerbations to relieve breathlessness
LAMA (tiotropium bromide) indications
COPD = to prevent exacerbations if no features of asthma/steroid reversibility
Asthma = add to ICS and LABA therapy if 1+ exacerbation per year
Theophylline
Oral bronchodilator
For chronic, uncontrolled by other therapies asthma/COPD
Criteria for LTOT in COPD
O2 <92% on RA Pulmonary oedema Non-smoker Polycythaemia (secondary) Hypoxia/hypercapnia
ACEi MOA
Prevents conversion of angiotensin I to angiotensin II (vasoconstrictor)
Reduces PVR
Reduces aldosterone = Na+ and H20 excretion, lowering BP (can be beneficial to kidneys).
Contraindications of ACEi/ARBs
Renal artery stenosis
AKI
Pregnancy/breastfeeding
Side effects of ACEi
Hypotension = sit/lie down for first dose
Dry cough
Hyperkalaemia
RARE: angioedema/anaphylactoid reaction
Dose of ACEi (ramipril)
1.25-2.5mg OD
Increased up to 10mg (max daily dose)
ACEi/ARBs fist line for which HTN patients
ALL with T2DM
<55 and NOT black/caribbean
Calcium channel blocker indications
HTN
Angina
Calcium channel blocker MOA
Relax/dilate arterial smooth muscle by decreasing Ca2+ entry into vascular/cardiac cells (lowers BP)
Reduce myocardial contractility, reducing rate and myocardial oxygen demand (prevents angina)
Side effects of calcium channel blockers (e.g. amlodipine)
Ankle swelling, flushing, headaches, palpitations (vasodilation and compensatory tachycardia).
Calcium channel blockers for vasculature
Dihydropyridines (amlodipine/nifedipine)
HTN
Calcium channel blockers for the heart
Non-dihydropyridines (verapamil/diltiazem)
Rate limiting = Angina
Amlodipine contra-indications
Unstable angina (tachycardia induced by vasodilation can increase myocardial oxygen demand)
Aortic stenosis (can cause collapse
CCB first line for which HTN patients?
> 55
Black/Caribbean
Thiazide diuretics for HTN in which patients?
Add on when HTN not controlled by CCB + ACEi/ARB
When CCB unsuitable for HTN due to oedema/other features of HF
Examples of thiazide diuretics
Bendroflumethiazide
Indapamide
Side effects of thiazide diuretics
Hyponatraemia (prevention of Na+ reabsorption)
Hypokalemia causing cardiac arrythmias
Male impotence
Increase plasma glucose, LDL and triglycerides
Stage 4 Tx for HTN if K+ >4.5
alpha blocker/beta-blocker
Stage 4 Tx for HTN if K+ <4.5
Spironalactone (k+ sparing diuretic)
Beta-blocker indications
Coronary heart disease (angina)
Chronic heart failure (improves prognosis)
AF (reduce ventricular rate)
HTN (if other medications fail)
Beta-blocker MOA
Reduce force of heart contraction, reducing cardiac work and oxygen demand, relieving cardiac ischaemia (treat angina)
Prolong refractory period of AV node and terminate SVT (treat AF)
Reduce renal renin secretion (lowers BP)
Side effects of beta-blockers
Cold extremeties
Fatigue
Headache
Impotence in men
Contra-indications of beta-blockers
Asthma (can cause bronchospasm)
Heart block
Haemodynamic instability
First line treatment for AF
Beta-blockers (e.g. bisprolol, atenolol)
Rate control and some rhythm control
Spironolactone MOA
Aldosterone antagonist = increase Na+ and H20 excretion (K+ retention)
Spironolactone indications
CIrrhosis
Chronic heart failure (add-on therapy)
Side effects of spironolactone
Hyperkalameia
Gynecomastia
DO NOT GIVE IN RENAL IMPAIRMENT
Nitrates indication and MOA
Angina/MI chest pain
Relax venous capacitance muscles, reducing pre-load and LV filling, reducing cardiac work and O2 demand.
Relieve coronary vasospasm
Relax systemic arteries
Contraindication for nitrates
Aortic stenosis (heart unable to increase CO through narrowed area to maintain pressure)
Hypotension
Nitrate side effects
Flushing, light-headed, hypotension, headaches (vasodilators)
Isosorbide mononitrate indications
Third line angina tx if CCB and beta-blockers not-tolerated
Furosemide indications
Chronic heart failure (tx symptomatic fluid overload, does not improve mortality)
Acute pulmonary oedema to relieve breathlessness
Furosemide MOA
Loop diuretic = inhibit Na+/K+/2Cl- co-transporter in the ascending limb of the loop of Henle, preventing their (and H20) reabsorption
Dilate capacitance veins = reduces pre-load in HF and increases contractility of the heart
Furosemide side effects
Dehydration and hypotension
Low electrolyte states
Hearing loss/tinnitus
CI in AKI/CKD
Ivabradine indications
Rate lowering
Given in HF or angina on failure of other Tx
Digoxin indications
AF (add on to CCB/beta-blocker)
Heart failure (add on Tx)
Digoxin MOA
Negatively chronotropic (reduces HR)
Positively iontropic (increases force of contraction)
Digoxin side effects
Bradycardia, dizziness, rash, GI disturbance
Toxicity = range of arrhythmias (digoxin has narrow therapeutic index)
DO NOT GIVE IN HEART BLOCK
DOSE REDUCTION IN RENAL IMPAIRMENT
Digoxin interactions
Loop/thiazide diuretics increase toxicity risk by causing hypokalaemia
CCB/spironalactone = increase plasma concentrations of digoxin, so increase toxicity risk.
NOAC (e.g. rivaroxaban, dabigatran) indications
AF = to reduce stroke risk with 1+ CHA2DVASc score (20mg daily)
VTE prophylaxis
NOAC side effects
Bleeding (e.g. epistaxis, GI bleeding)
Anameia, GI upset, elevated liver enzymes
CI IF BLEEDING
LOWER DOSE IN HEPATIC/RENAL IMPAIRMENT
NOAC elimination
Hepatic, by CYP enzyme
CYP inhibitors (macrolides) = increase effects CYP inducers (e.g. phenytoin) = decrease effects
Warfarin indications
Arterial embolism prevention (AF/prosthetic valves)
VTE prevention
Needs careful monitoring, takes a few days to reach therapeutic dose.
Warfarin CI
Liver disease (CYP metabolism) Pregnancy
Indications for rate-limiting CCB (+ examples)
AF
E.g. verapamil/diliazem
Amiodarone indications
Rhythm control in AF patients with structural heart defects.
Reduces ventricular rate and helps restore sinus rhythm
Amiodarone adverse effects
dose-dependent hepato/pulmonary fibrosis
thyroid problems (avoid if active disease)
AVOID IN HEART BLOCK
Amiodarone interactions
Increases plasma levels of digoxin, diltiazem and verapamil (half their doses if starting amiodarone)
Atorvostatin indications
20mg OD for primary prevention of CVD if QRISK2 >10%
80mg OD for secondary prevention in established disease
Statin side effects
Mild = headaches/GI disturbances
Muscle effects = aches, myopathy, rhabdomyolysis
Rise in liver enzymes
USE WITH CAUTION/REDUCE DOSE IN LIVER/RENAL IMPAIRMENT
Statin interactions
CYP inhibitors (macrolides, amiodarone, diliatzem) increase risk of adverse effects
Aspirin indications and doses
ACS/Acute stroke (300mg OD for 2 weeks )
Secondary prevention of thrombotic events (75mg OD)
ANTI-PLATELET
Aspirin adverse effects
GI irritation/peptic ulcer (take PPI alongside)
Tinnitus
Bronchospasm (in hypersensitivity)
CAUTION IN GOUT = CAN TRIGGER ATTACK
Clopidogrel indications
Secondary prevention of thrombotic events
300mg loading dose then 75mg OD, or after 2 weeks of 300mg of aspirin
Clopidogrel adverse effects
Bleeding
GI upset
Thrombocytopenia
Increased risk with CYP inhibitors
Metformin indication and MOA
First line for T2DM (500mg/day starting dose)
Lowers blood glucose
Reduces gluconeogenesis and glycogen lysis
Increases skeletal muscle glucose uptake
Metformin contraindications
Renal/hepatic impairment (reduce dose if eGFR <45)
Chronic alcohol abuse (risk of hypo)
WITHHOLD IF:
- AKI
- severe tissue hypoxia (e.g. sepsis/MI)
- IV contrast media
- acute alcohol intoxication
Metformin side effects
GI upset (usually transient)
Lactic acidosis (rare)
Gliclazide indications
Monotherapy for T2DM if metformin not tolerated (40-80mg OD starting dose)
Dual therapy (combination with metformin)if single agent not giving adequate glucose control
Gliclazide MOA
Stimulates pancreatic insulin secretion, so can cause weight gain
Gliclazide side effects
GI upset (mild/infrequent)
Hypoglycaemia
Hypersensitivity (rare)
weight gain
USE WITH CAUTION IN RENAL/HEPATIC IMPAIRMENT
Pioglitazone indication and MOA
T2DM (monotherapy or with metformin/glicllazide)
Lowers blood glucose by decreasing peripheral insulin resistance
Pioglitazone side effects
Bone fractures
Increased weight
Fluid retention (CI in HF)
Risk of liver toxicity
Tests before starting a statin
Hba1c LFT Lipid profile Creatinine kinase (CK) TFTs U&Es
Monitoring tests for statins
LFTs at 3 and 12 months after commencing Tx
CK if unexplained muscular Sx
Hba1c if risk of diabetes