P31 Flashcards
Ramipril
Lisinopril
Captopril
Perindopril
ACE inhibitors
Antihypertensive!
SE:
- Dry cough 10-20% secondary to increased bradykinin which is usually inactivated by ACE,
- Hypotension,
- Hyperkalaemia (lower aldosterone promotes K+ retention),
- Worsen renal failure,
- Angioedema,
- Other anaphylactoid reactions
Simvastatin
Atorvastatin
Rosuvastatin
Statins
HMG-CoA reductase inhibitor [rate-limiting enzyme in cholesterol synthesis]
- Inhibition reduces hepatic cholesterol synthesis
- This leads to upregulation of LDL-receptors and increased hepatic removal of LDL from circulation
SE:
- Headache,
- Gastrointestinal disturbances,
- Muscle aches,
- Myopathy,
- Rhabdomyolysis (rare),
- Risk in liver enzymes (ALT) leading to drug induced hepatitis (rare)
Antianginal drug classes
Beta blockers / Ca antagonist Nicorandil if above not tolerated Short acting nitrate Aspirin Lipid lowering drug
Antihypertensive drug classes
- ACE Inhibitors
- Angiotensin receptor blockers
- Beta blockers
- Calcium channel blockers
- Thiazide-like/thiazide diuretics
- Spironolactone (aldosterone antagonist)
- Alpha-receptor blockers
- Loop diuretics
Atenolol
Bisoprolol
Propranolol
Metoprolol
Beta-blockers
Anti-anginal
SE:
- Dizziness, fatigue, cold hands, impotence
- Hypotension (falls in elderly)
- Bronchoconstriction (care in asthma)
- Bradycardia / heart block
- Masking hypoglycaemia
- Raynaud’s phenomenon
Diltiazem
Verapamil
Fendiline
Non-dihydropyridine calcium channel blockers
SE:
- Headache
- Flushing
- Tachycardia
- Peripheral oedema
- Constipation
Glyceryl trinitrate (spray) Isosorbide dinitrate (tablet)
Nitrates
- Gives rise to NO which activates PKG and reduces contraction.
- They work on peripheral vessels mainly.
- Dilates venous vessels to decrease preload.
- Dilates arterial vessels to decrease afterload.
- Increases perfusion and oxygenation of cardiac muscle.
SE:
- Headache,
- Postural hypotension,
- Syncope,
- Flushing,
- Reflex tachycardia
- Tolerance with prolonged use,
Aspirin
COX inhibitor
Analgesic, antiplatelet
Irreversibly binds to COX and inhibits prostaglandin + thromboxane formation
SE:
- GI irritation
- Ulceration + haemorrhage
- Bronchospasm
AF drugs
Beta blocker
Non-dihydropyrrhidine calcium channel blocker
Digoxin
Amiodarone
Amiodarone
Anti-dysarrythmic (class III)
Non-selective action sodium and calcium receptors and alpha receptors.
Amiodarone is also used in the management of tachycardias.
IV infusion in stable wide complex tachycardia. After failed cardioversion in unstable wide complex tachycardias.
Anticoagulation drug classes
LMWH
Directly acting oral anticoagulants – only apixaban and rivaroxaban licenced for use without bridging therapy with LMWH currently
Fondaparinux
Unfractionated heparin (less common now)
Warfarin
Anticoagulant
- Inhibits vitamin K epoxide reductase
- Prevents recycling of Vit K → functional Vit K deficiency
- Inhibits synthesis of factors 2, 7, 9, 10, C and S
- Initially procoagulant: protein S is depleted first
Co-trimoxazole
Trimethoprim and sulfamethoxazole
These are used in combination (as co-trimoxazole) because of their synergistic activity (the importance of the sulfonamide group of antibiotics has decreased as a result of increasing bacterial resistance and their replacement by antibacterials which are generally more active and less toxic).
LRTI
Bendroflumethiazide
Chlorthalidone
Indapamide
Metolazone
Thiazide diuretics
Inhibits the Na/Cl co-transporter in the luminal membrane of the distal convoluted tubule
- Increases NaCl excretion
Indication: Hypertension,
Chronic heart failure
SE:
- Hypokalaemia,
- Hyponatremia
- Metabolic alkalosis,
- Hyperuricemia,
- Increased glucose in DM,
- Erectile dysfunction!
Compliance
Compliance – patient expected to stick to regimen prescribed by doctor, without question
Concordance
Concordance – a mutually agreed contract between doctor and patient, to take medicines in a way which suits both parties.
Adherence
Adherence – why a patient may not take medicines in the way agreed between doctor and patient:
Unintentional non-adherence – lack of understanding.
Intentional non-adherence – doesn’t actually agree with what was decided.
Ipratropium Tiotropium Glycopyrronium Aclidinium Umeclidinium
Muscarinic antagonists (bronchodilators - used in asthma)
Ipratropium (SAMA) Tiotropium (LAMA) Glycopyrronium Aclidinium Umeclidinium
Salbutamol
Short-acting beta2 agonist (SABA)
Bronchodilator
Asthma
SE:
- Tachycardia
- Fine tremor (particularly in the hands);
- Angioedema;
- Arrhythmias;
- Behavioural disturbances;
- Collapse;
- Headache;
- Hyperglycaemia (especially when given intravenously)
Acute asthma medications
Salbutamol Ipratropium Bromide Hydrocortisone Magnesium sulfate Aminophylline
IV fluids
Magnesium sulphate + aminophylline - should only be given after senior consultation
Magneusium sulphate
Bronchodilator (unlicensed use)
Severe acute asthma
Aminophylline
Aminophylline is a methylxanthine bronchodilator composed of theophylline and ethylenediamine.
MoA not completely understood.
Theophylline relaxes smooth muscle in the respiratory tract and suppresses airway stimuli.
SE:
- Tachycardia,
- Arrhythmia
- Nausea/vomiting
Tiotropium
LAMA
Salmeterol
LABA
Roflumilast
A selective, long-acting inhibitor of the enzyme phosphodiesterase-4.
It has anti-inflammatory properties.
Adjunct to bronchodilators for the maintenance treatment of patients with severe chronic obstructive pulmonary disease associated with chronic bronchitis and a history of frequent exacerbations.
Anti-anginal drug classes
- Beta blockers / Ca antagonist
- Nicorandil (short acting nitrate) if above not tolerated
- Aspirin
- Lipid lowering drug (statins)
AF medications
- Beta blockers
- Non-DHP calcium channel blocker (Diltiazem, Verapamil, Fendiline)
- Digoxin
- Amiodarone
Adrenaline
To protect heart and brain by peripheral vasoconstriction
Indicated in cardiac arrest
If you suspect a pulmonary embolism what treatment should be initiated before the result of the investigation is available?
Low molecular weight heparin
Also could use Direct Factor Xa inhibitor (DOAC) such as apixaban or rivaroxaban.
List some anticoagulants
LMWH
Directly acting oral anticoagulants (apixaban and rivaroxaban)
Fondaparinux
Unfractionated heparin (less common now)
Dalteparin (LMWH)
Enoxaparin (LMWH)
Action: Anticoagulant
MOA: accelerates action of antithrombin III by increasing its inactivation of factor Xa
Use: VTE prevention. Treat DVT, PE, MI and unstable angina
Dose calculated via body weight
ADE: given subcut, renally excreted
SE: bleeding. less likely than heparin to cause thrombocytopaenia. Hypersensitivity reactions. Osteoporosis
- Blood tests prior to starting: APTT, PT, U&Es, platelets
- No routine monitoring
- Takes up to 5 days to reach therapeutic range
Do COAG and FBC prior to treatment to ascertain baseline coagulation status and to ensure platelet count is normal before starting a heparin (risk of heparin induced thrombocytopenia).
When is it safe to stop LMWH when switching to warfarin?
After 5 days provided the INR has been therapeutic above 2 for a minimum of 48 hours.
High INR managment
Major bleeding—stopwarfarin sodium; givephytomenadione(vitamin K1) by slow intravenous injection; givedried prothrombin complex(factors II, VII, IX, and X); if dried prothrombin complex unavailable, fresh frozen plasma can be given but is less effective; recombinant factor VIIa is not recommended for emergency anticoagulation reversal
INR >8.0, minor bleeding—stopwarfarin sodium; givephytomenadione(vitamin K1) by slow intravenous injection; repeat dose ofphytomenadioneif INR still too high after 24 hours; restartwarfarin sodiumwhen INR <5.0
INR >8.0, no bleeding—stopwarfarin sodium; givephytomenadione(vitamin K1) by mouth using the intravenous preparation orally [unlicensed use]; repeat dose ofphytomenadioneif INR still too high after 24 hours; restart warfarin when INR <5.0
INR 5.0–8.0, minor bleeding—stopwarfarin sodium; givephytomenadione(vitamin K1) by slow intravenous injection; restartwarfarin sodiumwhen INR <5.0
INR 5.0–8.0, no bleeding—withhold 1 or 2 doses ofwarfarin sodiumand reduce subsequent maintenance dose
Ezetimibe
Actions: inhibits absorption of cholesterol from intestine. Decreases LDL
MOA: Blocks sterol carrier protein in brush border of enterocytes. Decrease biliary and dietary cholesterol delivered to liver
Use: hypercholesterolaemia, usually adjunct to statin
SE: few. GI upsets. Headaches. Rashes. Myalgia
Fenofibrate
Bezafibrate
Actions: marked decrease in plasma VLDL and triglyceride. Modest decrease in LDL and small increase in HDL
MOA: increase transcription for genes for lipoprotein lipase and apoproteins apoA1 and apoA5. Increased LDL uptake by receptors.
Use: mixed dyslipidemia.
SE: GI upset. Rash. Moderate increase in gallstones. myositis
Do not give with a statin
Co-trimoxazole
Combination of:
- Trimethoprim and
- Sulfamethoxazole
These are used in combination (as co-trimoxazole) because of their synergistic activity (the importance of the sulfonamide group of antibiotics has decreased as a result of increasing bacterial resistance and their replacement by antibacterials which are generally more active and less toxic).
Use: pneumonia, bronchitis, infections of the urinary tract, ears, and intestines
Causes of hyponatraemia?
Urinary sodium >20 mmol/L:
- Addison’s disease
- Thiazide + loop diuretics
- SIADH
- Hypothyroidism
Urinary sodium <20mmol/L:
- Vomiting, diarrhoea
- Burns
- Psychogenic polydipsia
- Renal failure
- Secondary hyperaldosteronism: liver cirrhosis. heart failure
Causes of hypernatraemia
- Diabetes insipidus
- Primary aldosteronism
- Dehydration
- Excess IV saline
- Osmotic diuretics
Causes of hyperkalemia
- Acute renal injury
- Metabolic acidosis
- Addison’s disease
- Rhabdomyolysis
- Massive blood transfusion
- Type 4 renal tubular acidosis
- Drugs (ACEi, ARBs, spironolactone, amiloride, ciclosporin, heparin)
Causes of hypokalemia
Haemolysis!
Hypokalemia with hypertension:
- Cushing’s syndrome
- Conn’s syndrome (primary hyperaldosteronism)
- Liddle’s syndrome
- 11-beta hydroxylase deficiency
Hypokalaemia without hypertension:
- Thiazide diuretics
- GI loss (diarrhoea, vomiting)
- Renal tubular acidosis (type 1 and 2)
- Bartter’s syndrome
- Gitelman syndrome
Causes of hypocalcemia
- Primary hyperparathyroidism
- Malignancy induced: bone metastases, myeloma, PTHrP from SqCC
- Sarcoidosis
- Vitamin D intoxication
- Acromegaly
- Thyrotoxicosis
- Milk-alkali syndrome
- Drugs: thiazides, calcium containing antacids
- Dehydration
- Addison’s disease
- Paget’s disease of the bone
- Multiple endocrine neoplasia type I
Causes of hypocalcemia
- Bisphosphonates toxicity
- Vitamin D deficiency
- Magnesium deficiency
- Hypoparathyroidism
- Pseudohypoparathyroidism
- Rhabdomyolysis
- Chronic kidney disease
Hyponatremia treatment?
Give IV fluids to correct any hypovolaemia (0.9% NaCl or Hartmann’s)
Beta-blocker + verapamil?
Can interact to cause serious bradycardia
Antibiotics most frequently implicated in predisposition to C. difficile associated diarrhea (CDAD)?
Fluoroquinolones,
Clindamycin,
Broad-spectrum penicillins (amoxicillin) and cephalosporins.
List 3 types of healthcare acquired infections that use of broad spectrum antibiotics predispose one to?
C difficile
MRSA
ESBL - Extended-spectrum beta-lactamases (ESBL) are enzymes that confer resistance to most beta-lactam antibiotics, including penicillins, cephalosporins, and the monobactam aztreonam.
Carbapenem resistant enterococci
Compliance vs concordance vs adherence?
Compliance – patient expected to stick to regimen prescribed by doctor, without question!
Concordance – a mutually agreed contract between doctor and patient, to take medicines in a way which suits both parties.
Adherence – why a patient may not take medicines in the way agreed between doctor and patient:
Unintentional non-adherence – lack of understanding.
Intentional non-adherence – doesn’t actually agree with what was decided.
What factors could improve medication adherence and concordance?
Simplification / rationalise therapy
Assessment
- Fuller’s Self-medication screening risk assessment
- Self medication schemes
- Medication review service
Aids
- Reminder charts
- Nomad / Dosette boxes
- Medication Record Charts
Terbutaline
Short-acting beta-2 agonist
Actions: bronchodilation. Relaxes uterine smooth muscle.
MOA: decreased calcium mediated contraction in bronchioles. Increased cAMP which activates PKA. PKA inhibits myosin light chain kinase - mediator of contraction
Use: asthma. Acute attacks. COPD
Side effects: tremors, tachycardia, dysrhythmias, peripheral dilation.
Note: hypertensive crisis if used with MAO inhibitor.
When should a low dose of ICS be started in asthma treatment?
A low dose of inhaled corticosteroid should be started if
- Inhaled short-acting beta2 agonist used 3+ times a week
- Waking at night due to asthma symptoms at least once a week.
- BTS/SIGN (2016) also recommend initiation in patients who have had an asthma attack in the last 2 years, and starting inhaled corticosteroids at a dose appropriate to the severity of asthma.
5 steps in asthma management
Step 1:
- SABA
Step 2:
- SABA
- ICS
Step 3:
- SABA
- ICS/LABA combo
Step 4:
- SABA
- ICS/LABA combo
- High dose ICS
Step 5:
- Everything in step 4 plus additional treatments (montelukast)
Montelukast
Class: leukotriene receptor antagonist (LTRA)
Indication: maintenance treatment of asthma and to relieve symptoms of seasonal allergies.
It is usually administered orally.
MoA: Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes. This reduces bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation.
Because of its method of operation, it is not useful for the treatment of acute asthma attacks.
Formoterol vs salmeterol?
Formoterol and salmeterol are both long-acting bronchodilators that are effective in the treatment of asthma.
Formoterol has a rapid onset of action, whereas salmeterol causes bronchodilation in a somewhat slower manner.
Formoterol has higher intrinsic activity than salmeterol, which means that it is a full agonist, whereas salmeterol is a partial agonist on the beta2-receptor.
SE of beta-2 agonists? (e.g. Salbutamol)
Tremor and tachycardia are the most frequent side effects seen in clinical practice.
- Angioedema;
- Arrhythmias;
- Behavioural disturbances;
- Collapse;
- Fine tremor (particularly in the hands);
- Headache;
- Hyperglycaemia (especially when given intravenously);
- Hypersensitivity reactions;
- Hypokalaemia (with high doses);
- Hypotension; ketoacidosis (especially when given intravenously);
- Muscle cramps;
- Myocardial ischaemia;
- Nervous tension;
- Palpitation;
- Paradoxical bronchospasm (occasionally severe);
- Peripheral vasodilation;
- Rash;
- Sleep disturbances;
- Tachycardia;
- Urticaria
Acute asthma medications
- Short-acting beta2 agonist (salbutamol)
- Ipratropium bromide: antimuscarinic bronchodilator (LAMA)
- Hydrocortisone
- Magnesium sulfate: bronchodilator effect
- Aminophylline
- IV fluids to correct dehydration and perhaps reduce tenacity of mucous airway secretions
Acute asthma treatment.
Acute asthma management is based on:
- Assessing severity (mild/moderate, severe or life-threatening) while starting bronchodilator treatment immediately
administering oxygen therapy, if required, and titratingoxygen saturation to target of92–95% (adults) or at least 95% (children)
completing observations and assessments (when appropriate, based on clinical priorities determined by baseline severity). - Administering systemic corticosteroids within the first hour of treatment.
- Repeatedly reassessing response to treatment and either continuing treatment or adding on treatments, until acute asthma has resolved, or patient is transferred to an intensive care unit or admitted to hospital.
- Observing the patient for at least 1 hour after dyspnoea/respiratory distress has resolved, providing post-acute care and arranging follow-up.
Roflumilast
MoA: Selective, long-acting inhibitor of the enzyme phosphodiesterase-4.
It has anti-inflammatory properties.
Indication: Adjunct to bronchodilators for the maintenance treatment of patients with severe chronic obstructive pulmonary disease associated with chronic bronchitis and a history of frequent exacerbations
List SABAs
- Bitolterol
- Carbuterol
- Fenoterol
- Pirbuterol
- Procaterol
- Reproterol
- Rimiterol
- Salbutamol (albuterol)
- Levosalbutamol
- Terbutaline
- Tulobuterol
List LABAs
- Bambuterol
- Clenbuterol
- Formoterol/Arformoterol
- Salmeterol
- Salmefamol
List is LAMAs
- Aclidinium bromide
- Glycopyrronium bromide
- Ipratropium bromide
- Oxitropium bromide
- Tiotropium bromide
- Umeclidinium bromide
List leukotriene antagonists
- Montelukast
- Pranlukast
- Zafirlukast
List corticosteroids used in asthma
- Beclometasone
- Betamethasone
- Budesonide
- Ciclesonide
- Flunisolide
- Fluticasone propionate
- Mometasone
- Triamcinolone
