3011-Cat 1 drugs Flashcards
Digoxin - Class and indication
Antiarrhythmic
cardiac glycoside antiarrhythmic
Indication: atrial fibillation, atrial flutter and hypertension
Digoxin - Dose
Dose:
Initial: 250-500 micrograms every 4-6hr (onset 0.5-2hr, max effect at 2-6hr)
Maintenance: 125-250 micrograms/day
Maximum: 1.5mg/day, 500 micrograms in elderly (initial), 500 micrograms/day and 125 micrograms/day in elderly
Situation where adjustment required: Elderly = 62.5-250 micrograms every 4-6hr (halved) max 500 micrograms
Digoxin - MOA
slows heart rate and reduces AV nodal conduction by an increase in vagal tone (PSNS) and reduction in sympathetic activity
reversibly inhibits Na/K ATPase alpha subunit
positively inotropic and negative chronotropic activity
Digoxin - Common AEs
Anorexia, nausea, vomiting, diarrhoea, visual disturbance, may worsen arrhythmia, seizure, confusion (uncommon if <0.8 microgram/L)
Digoxin - Counselling
monitoring
- Regularly assess the pt for digoxin toxicity including resting heart rate
- When use to control ventricular rate in AF, aim for a ventricular rate <110beats/min
- Tell your dr or pharmacist that you are taking digoxin before using any other medicines including over-the-counter and herbal products
Amiodarone - class and indication
cardiac glycoside antiarrhythmic
treatment and prophylaxis of serious tachyarrythmis (ventricular, arial fibrillation and SV tachycardia
Amiodarone - Dose
Initial: 200mg tid for 1 week, then 200mg bd for 1 week
Maintenance: 100-400mg/day (max effect 1-3 months)
Maximum: 400mg/day
Situation where adjustment required: Dose doubled in significant obesity or ventricular arrhythmia, halved in underweight
Amiodarone - MOA
- decrease SA node automaticity
- slows AV node conduction
- prolongs refractory period
Amiodarone - Common AEs
Nausea and vomiting (especially upon loading dose), constipation, anorexia, taste disturbance, thyroid function alteration, fever, potential to worsen arrhythmias (slow to resolve), hepatotoxicity, optic neuropathy, SIADH
Amiodarone - Counselling
monitoring
-if you develop problems with vision, difficulty breathing, a dry cough, weight loss, muscle weakness, a severe rash or worsening of your heart symptoms, tell your dr
Atenolol - class and indication
cardioselective betablocker antihypertensive
indication: hypertension, angina, tachyarrythmias, MI
Atenolol - Dose
Initial: Adult: 25-50mg/day, increase if required to 100mg/day in 1 or 2 doses Child: 0.5-2mg/kg/day in 1 or 2 doses Maintenance: Patient specific Maximum: Hypertension: 50mg/day Tachyarrhythmia: 100mg/day
Atenolol - MOA
Competitively block beta-receptors in heart, peripheral vasculature, bronchi, pancreas, uterus, kidney, brain and liver. Reduce heart rate, blood pressure, cardiac contractility, decrease sinoatrial node and atrioventricular node rates and prolong atrial refractory period.
Atenolol - Common AEs
Bradycardia, hypotension, nausea, diarrhoea, cold extremities, fatigue, abnormal vision, hallucinations, insomnia, nightmares, depression, heart block, rash, alopecia
Atenolol - Counselling
counselling
- you may feel tired or lacking in energy for a few days after starting this medication or when the dose is increased
- this medicine can cause fatigue, nausea, diarrhoea, constipation and headaches. These may decrease or disappear with continued use
Bisoprolol - Class and Indication
cardioselective betablocker antihypertensive
indication: chronic heart failure with reduced ejection fraction
Bisoprolol - dose
Initial: 1.25mg/day for 1 week, if well tolerated increase dose to 2.5mg/day for 1 week, then 3.75mg/day for 1 week then 5mg/day for 4 weeks, then 7.5mg/day for 4 weeks then 10mg/day
Maintenance: 10mg/day
Maximum: 10mg/day
Bisoprolol - MOA
Competitively block beta receptors in heart, peripheral vasculature, bronchi, pancreas, uterus, kidney, brain and liver. Reduce heart rate, blood pressure, cardiac contractility, decrease sinoatrial node and atrioventricular node rates and prolong atrial refractory period.
Bisoprolol - Common AEs
Hyperthyroidism, hypotension, nausea, diarrhoea, cold extremities, vision disturbances, hallucinations, insomnia, nightmares, heart block, rash, alopecia
Bisoprolol - Counselling
- you may feel tired or lacking in energy for a few days after starting this medication or when the dose is increased
- take your dose of medicine in the morning
- this medicine can cause fatigue, nausea, diarrhoea, constipation and headaches. These may decrease or disappear with continued use
Carvedilol - class and indication
alpha 1 receptor and non-selective betablocker antihypertensive
indication: Hypertension, chronic heart failure with reduced ejection fraction
- Avoid in severe asthma
Carvedilol - Dose
Initial:
Hypertension: 12.5mg/day for 2 days
Heart failure: 3.125 mg bd for 2 weeks then increase at at least 2 week intervals to 6.25mg bd, then 12.5mg bd, then 25mg bd
Maintenance:
Hypertension: 25mg/day, increased if required at intervals of at least 2 weeks
Maximum:
Hypertension: 50mg/day in 1 or 2 doses
Heart failure: 25mg bd if <85kg or severe heart failure, 50mg bd if >85kg
Situation where adjustment required: Weight difference/degree heart failure in heart failure, not tolerating treatment
Carvedilol - MOA
Competitively block beta receptors in heart, peripheral vasculature, bronchi, pancreas, uterus, kidney, brain and liver. Reduce heart rate, blood pressure, cardiac contractility, decrease sinoatrial node and atrioventricular node rates and prolong atrial refractory period
Carvedilol - Common AEs
Bradycardia, orthostatic hypotension, nausea, diarrhoea, cold extremities, vision disturbance, hallucinations, insomnia, nightmares, depression, heart block, rash, alopecia
Carvedilol - counselling
monitoring
Metoprolol - class and indication
selective beta-1 blocker antihypertensive
indication: Hypertension, angina, tachyarrhythmias, MI, chronic heart failure with reduced ejection fraction
Metoprolol - Dose
Initial: Hypertension: 50-100mg/day in 1 or 2 doses Angina: 25-50mg bd Tachyarrhythmias: 25-100mg bd Heart failure (CONTROLLED RELEASE): 23.75mg/day for a minimum of 2 weeks, if well tolerated increase dose remaining at each new dose for at least 2 weeks: 47.5mg, 95mg, 190mg Maintenance: Hypertension: 50-100mg/day or bd Angina: 50-100mg bd or tid MI: 25-50mg bd
Metoprolol - MOA
Competitively block beta receptors in heart, peripheral vasculature, bronchi, pancreas, uterus, kidney, brain and liver. Reduce heart rate, blood pressure, cardiac contractility, depress sinoatrial node and atrioventricular node rate and prolong atrial refractory period.
Metoprolol - Common AEs
Bradycardia, hypotension, nausea, diarrhoea, cold extremities, vision disturbances, hallucinations, insomnia, nightmares, depression, heart block, rash, alopecia
Metoprolol - counselling
- you may feel tired or lacking in energy for a few days after starting this medication or when the dose is increased
- this medicine can cause fatigue, nausea, diarrhoea, constipation and headaches. These may decrease or disappear with continued use
Aspirin - class and indication
antiplatelet
indication: Analgesic, anti-inflammatory, antiplatelet, antipyretic
Aspirin - dose
Initial:
300mg
maintenance 75-150mg
Aspirin - MOA
Inhibits platelet aggregation by irreversible inhibition of COX, reducing the synthesis of thromboxane A2 for the life of the platelet
Aspirin - common AEs
Association with Reye’s syndrome (<16yr), abdominal pain, dose-related tinnitus, GI bleeding (concomitant use with other NSAIDs will increase), concomitant use of anticoagulants increases risk of bleeding
Aspirin - counselling
monitoring
Clopirogrel - class and indication
thienoyridine antiplatelet agent ‘
indication: History of symptomatic atherosclerosis, acute coronary syndrome
- Contraindicated in active bleeding disorders, severe hepatic impairment
Clopidogrel - dose
Initial:
APF: 75mg/day(300-600mg loading dose may be given for some indications)
AMH:
o Prevention of vascular ischaemic events: 75mg/day
o Acute coronary syndrome: 300mg, then 75mg/day with Aspirin for 1-12 months
o Placement of coronary stent: 300-600mg for 6 hours before procedure, then 75mg/day with Aspirin for 1-12 months
Maintenance: As above
Clopidogrel - MOA
Active metabolite of the thienopyridines irreversibly binds to the platelet P2Y12 receptor and inhibits platelet aggregation for the life of the platelet.
Clopidogrel - common AEs
Skin reactions, diarrhoea, GI ulcer, SJS, neutropenia, SIADH
Clopidogrel - counselling
monitoring
Ticagrelor - class and indication
thienopyridine antiplatelet
indication: acute coronary syndrome (with aspirin)
Contraindications: active bleeding disorder, history of intracranial haemorrhage, mod-severe hepatic impairment
Ticagrelor - dose
Initial: 180mg, then 90mg bd for at least 12 months in combination with low dose Aspirin (75-100mg/day)
Maintenance: 180mg/day
ticagrelor - MOA
Reversibly binds to platelet PDY12 receptor and inhibits platelet aggregation for the life of the platelet.
Ticagrelor - common AEs
Dyspnoea, nausea, vomiting, diarrhoea, constipation, dizziness, shortness of breath, non-cardiac chest pain, headache, raised uric acid/creatinine concentration
Ticagrelor - drug interactions
CYP3A4 and Pgp substrate and inhibitor, NSAIDs/SSRIs possible increased risk of bleeding, grapefruit increases risk of bleeding
Ticagrelor - counselling
monitoring - renal function test 1 month after initiation
Heparin - class and indication
anticoagulant
indication: Prevention and treatment of VTE, treatment of acute coronary syndrome, peripheral arterial occlusion
- Contraindicate: severe thrombocytopenia, active bleeding or risk of, severe heaptic impairment/disease
Heparin - Dose
Initial:
Prevention VTE: SC 5000 units 2hr prior, then 5000 units bd or qid for 7-10 days until mobilised
Treatment VTE: IV bolus 5000 units, then IV infusion 1300 units/hr
Maintenance: As above
Maximum: IV bolus: 30000 units/24hrs
Situation where adjustment required: Renal impairment, surgery, elderly
Heparin - MOA
Inactivate clotting factors IIa (thrombin) and Xa by binding to antithrombin III
Heparin - common AEs
Bleeding, bruising, pain at injection site, hyperkalaemia, mild reversible thrombocytopenia, transient ALT elevation, skin necrosis, osteoporosis, alopecia
Heparin - counselling
monitoring
Tell your dr if you have any signs of bleeding eg. nosebleed, black or tarry bowel motions or unexplained bruising) during and after treatment
Warfarin - class and indication
anticoagulant
indication: prevention and treatment of VTW, prevention fo stoke with previous MI
Warfarin -dose
Initial: 5-10mg/day for 2 days then adjust according to INR
Maintenance: 1-10mg/day (dose at same time every day, immediately notify doctor if missed dose, do not swap brands of warfarin, maintain a normal, balanced diet and limit alcohol intake)
Maximum: 10mg/day
Situation where adjustment required: Elderly, hepatic or renal impairment
Warfarin - MOA
Inhibits synthesis of vitamin K-dependent clotting factors and the antithrombotic factors protein C and protein S
Warfarin - common AES
Bleeding, skin necrosis, purple discolouration, alopecia, fever, rash, nausea, vomiting, diarrhoea
Warfarin - DI
CYP1A2, 2C9, 2C19 and 3A4 substrate, vitamin K containing foods/drinks, medicines that affect blood blotting, paracetamol (regular use may increase INR)
Warfarin - counselling
INR (target 2-3)
- Take the tablets at about the same time each day. Use a calendar or anticoagulant book to keep a record of your dose and mark off the date immediately after taking a dose
- if you forget to take a dose, notify the dr immediately. Take the dose as soon as possible on the same day. Don’t take a double dose the next day to make up for the missed dose.
Dabigatran - class and indication
anticoagulant/NOACS
indication: Prevention VTE after elective total hip or knee replacement, treatment of acute VTE, prevention of subsequent VTEs, non-valvular, AF and high-risk stroke or systemic embolism
Dabigatran - dose
Initial:
Hip/knee replacement: treatment for 10 day and 28-35 days after knee and hip surgery respectively: 110mg within 1-4hr of surgery, then 220mg/day
AF/acute VTE/prevention: treatment for over 3 months: 150mg bd
>75yrs = 110mg bd
Maintenance: As above
Dabigatran - MOA
Reversibly inhibit both free and fibrin-bound thrombin, preventing conversion of fibrinogen to fibrin, preventing thrombus formation. Thrombin-induced platelet aggregation is also inhibited.
Dabigatran - common AEs
Gastritis, dyspepsia, GI bleeding, oesophageal ulcers, increased liver enzymes and bilirubin
Dabigatran - DIs
Anticoagulants, NSAIDs, antiplatelets, SSRIs increase risk of bleeding, Pgp inducers and inhibitors may affect concentration (especially verapamil)
Dabigatran - counselling
monitoring of renal function
- this medicine may cause nausea and diarrhoea
- if you develop signs of bleeding or bleeding that will not stop or if you suddenly feel weak, dizzy and short or breath, seek immediate medical attention
- tell your dentist you are taking this
- NSAIDs and SSRIs increase risk of bleeding
Rivaroxaban - class and indication
anticoagulant: factor Xa inhibitor/NOACs
indication: Prevention VTE following elective hip/knee replacement, treatment acute VTE, prevention subsequent VTE, non-valvular AF and high-risk stroke
Rivaroxaban - dose
Initial:
Hip/knee replacement: Oral: 10mg/day starting 6-10hr after surgery, continue 2 wk after knee, 5 wk after hip
VTE: Oral: 15mg bd for 3 wk, then 20mg/day
Prevention emboli in AF: Oral: 20mg/day
Take dose at the same time every day, exactly as prescribed, with good
Maintenance:
Maximum: 30mg/day
Rivaroxaban - MOA
Selectively inhibit factor Xa, blocking thrombin production, conversion of fibrinogen to fibrin and thrombus development
Rivaroxaban - DI
Azoles, HIV-PIs, antiplatelets/NSAODs
Rivaroxaban - common AEs
Peripheral oedema, itch, skin blisters, muscle spasm, hepatotoxicity
Rivaroxaban - counselling
Renal function
Target test results: >50mL/min
-it is important to take this medicine exactly as prescribed. Take the tablets at about the same time each day. It may help to mark off on a calendar each time you take a dose.
-Once daily dose: if you forget to take a dose, take a tablet immediately and continue on the following day with one tablet at the normal time do not double dose
-Twice daily dose: if you forget to take a dose, take a tablet immediately to ensure that you take a total dose of 30mg on that day. If necessary you can take your morning dose at same time as your evening dose.
Enoxaparin - class and indication
anticoagulant (low MW heparin)
indication: Prevention and treatment of VTE, treatment of acute STEMI and non-STEMI, and unstable angina
Enoxaparin - dose
Initial:
Prevention VTE: SC: 20mg/day 7-10day
Tx VTE: SC: 1mg/kg bd or 1.5mg/kg/day
Unstable angina/non-STEMI: SC: 1mg/kg bd for 2-8 day w/ Aspirin
Maintenance:
Maximum: Varies according to indication, risk factors and weight
Situation where adjustment required: Low/high weight, renal impairment, hypertension, risk factors, indication
Enoxaparin - MOA
Inactivate clotting factors IIa (thrombin) and Xa by binding to antithrombin III; high efficacy.
Enoxaparin - DIs
Anticoagulants, antiplatelet agents, NSAIDs (increased risk of bleeding)
Enoxaparin - Common AEs
Bleeding, bruising/pain at injection site, hyperkalaemia, mild reversible thrombocytopenia, transient elevation of liver aminotransferases, severe thrombocytopenia, skin necrosis, osteoporosis, alopecia
Enoxaparin - counselling
bleeding risk if DIs
-inject into a fold of skin on the stomach. Do not rub the area after injecting a dose, rotate injection site.
NSAIDs increase risk of bleeding
Perindopril - class and indication
ACEI
indication: Hypertension, chronic heart failure, reduction MI risk
Perindopril - dose
Hypertension o PA- 5mg/day, max 10mg/day o PE- 4mg/day, max 8mg/day HF: o PA: 2.5mg/day à 5mg/day o PE: 2mg/day à 4mg/day Reduction CV events o PA: 5mg/day 2wks à 10mg/day o PE: 4mg/day 2wks à 8mg/day May take 2-4 weeks to optimal effect
Perindopril - MOA
Prodrug metabolized to perindoprilat = potent, competitive ACEI. Blocks conversion of angiotensin I to angiotensin II and the breakdown of bradykinin. Reduced effects of vasoconstriction, Na retention and aldosterone release, and effect on SNS activity/GF’s
Perindopril - DIs
NSAIDS, sacubitril with valsartan, medicines that increase K+ concentration, Li, digoxin, DPP-4 inhibitors, Angiotensin II receptor antagonists
Perindopril - Common AEs
Hypertension, headache, dizziness, cough (improves within 1-4 wks of stopping), fatigue, nausea, renal impairment, angioedema, rash, diarrhoea
Perindopril - counselling
monitoring of electrolytes and renal function pre-treatment and then review after 1-2 weeks
Ramipril - class and indication
ACEI
indication: Hypertension, post MI with heart failure, prevention MI and cardiovascular death, revascularisation over 55 years
Ramipril - Dose
Initial:
APF: 2.5-10mg/day in 1 or 2 doses
AMH:
Hypertension: 2.5mg/day increase after 2-3wks to 5mg prn.
HF: 2.5mg bd beginning 2-10 post-MI, increase at intervals of 1-3 days to 10mg/day in 2 doses
CV risk: 2.5mg/day increase after 1 wk to 5mg/day, after 3 wk 10mg/day
Maintenance: As above
Maximum:
Hypertension: Max 10mg/day in 1 or 2 doses
HF: 10mg/day in 2 doses
CV risk: 10mg/day
Situation where adjustment required: Volume/Na depletion, primary hyperaldosteronism, black African/Caribbean descent, aortic stenosis, PVD/atherosclerosis, renal impairment, surgery, elderly, women planning to conceive
Ramipril - MOA
Metabolised to ramiprilat- potent, competitive ACEI. Blocks conversion of angiotensin I to angiotensin II and the breakdown of bradykinin. Reduced effects of vasoconstriction, Na retention and aldosterone release, and effect on SNS activity/GF’s
Ramipril - DIs
NSAIDs (increased risk of renal impairment- esp. avoid in those taking diuretics to avoid triple whammy), sacubitril with valsartan (increased risk of angioedema), medicines that increase K+ concentration (increased risk of hyperkalaemia), Li, digoxin, DPP-4 inhibitors, Angiotensin II receptor antagonists
Ramipril - Common AEs
Hypertension, headache, dizziness, cough (improves within 1-4 wks of stopping), fatigue, nausea, renal impairment, angioedema, rash, diarrhoea
Ramipril - Counselling
Electrolytes and renal function pre-treatment and then review after 1-2 weeks
Fursemide - class and indication
loop diuretic
indication: Oedema associated with heart failure and hepatic cirrhosis, renal impairment and nephrotic syndrome
Fursemide - dose
Initial:
Take dose in morning or if bd then morning and lunch time
- Oedema:
o Adult
§ Oral: 20-40mg/day or bd adjust according to clinical response to maintenance dose
§ IV/IM: 20-40mg, repeat at intervals of over 2 hours until desired diuretic effect
o Child
§ Oral: 1-2mg/kg, if required increase dose by 1-2mg/kg every 6-8hr once satisfactory diuresis adjust to lowest effective dose
§ IV/IM: 0.5-1mg/kg, if required increase dose by 1mg/kg at intervals of over 2 hours until desired diuresis
Hypercalcaemia:
o IV: 80-100mg q 1-2hr
Maximum:
Oedema
o Adult
§ Oral: 1g/day
o Child
§ Oral: 6mg/kg every 6 hours
Situation where adjustment required: Renal impairment and hepatic impairment
Frusemide - MOA
Fast onset and short duration (4-6hr). Inhibit reabsorption of Na and Cl in the ascending limb of the loop of Henle à potent.
Frusemide - DIs
ACEI/Angiotensin II receptor antagonist + NSAIDs (risk of nephrotoxicity), Li, ototoxic medicines, medicines that reduce K+ concentration, digoxin
Frusemide - Common AEs
Electrolyte disturbances, dehydration, metabolic alkalosis, gout, orthostatic hypotension, dyslipidemia, rash, tinnitus, vertigo, SJS, agranulocytosis, polyuria
Frusemide - Counselling
serum electrolytes and body weight
Hydrochlorothiazide - class and indication
thiazide diuretic
indication: Hypertension, oedema associated with heart failure, hepatic cirrhosis/nephrotic syndrome
Hydrochlorothiazide - dose
Initial: Single or 2 doses, can take u to 4 weeks to reduce blood pressure effectively Hypertension: o Oral:12.5mg-50mg/day Oedema: o Oral: 25-100mg/day, or intermittently on 3-5 days/wk Kidney stones: o Oral: 25-50mg 1 or 2 x /day Maintenance: Maximum: Adult o Hypertension: 100mg/day o Oedema: 200mg/day Child o 1mnth-12yrs: 3mg/kg (not to exceed 50mg)/day o >12yrs: 50mg/day Situation where adjustment required: Elderly, hepatic impairment, renal impairment
Hydrochlorothiazide - MOA
Moderately potent diuretic. Inhibit reabsorption of Na and Cl in the proximal segment of the distal convoluted tubule, increasing delivery of Na to the collecting tubules and producing a corresponding increase in K+ excretion. Lower BP by a vasodilator effect.
Hydrochlorothiazide - DIs
ACEI + NSAID (risk of nephrotoxicity), Li, antihyperglycaemics
Hydrochlorothiazide - Common AEs
Dizziness, dyslipidaemia, blurred vision, impotence, renal impairment, weakness, muscle cramps, polyuria, orthostatic hypotension, electrolyte disturbances
Hydrochlorothaizide - counselling
hepatic and renal testing
Sprionolactone - class and indication
diuretic
indication: Primary hyperaldosteronism, refractory oedema associated with secondary hyperaldosteronism, resistant hypertension, hirsutism in female
Spironolactone - dose
Initial: Primary hyperaldosteronism o Oral: 50-200mg in 1 or 2 doses Oedema: o Oral: 100mg/day, maintenance 25-200mg/day (max 200mg) in 1 or 2 doses Resistant hypertension: o Oral: 12.5-50mg/day Hirsutism o Oral: 50-100mg/day in 1 or 2 doses Maintenance: Maximum: 200mg/day Situation where adjustment required: Renal impairment
Spironolactone - MOA
Inhibit Na absorption in the distal tubule by antagonizing aldosterone, increasing Na and water excretion and reducing K+ excretion (weak diuretic). May contribute to reducing aldosterone role in heart failure.
Spironolactone - DIs
NSAID + ACEI (increased risk of hyperkalaemia), digoxin
Spironolactone - Common AEs
Nausea, vomiting, diarrhoea, drowsiness, headaches, hyperkalaemia, hyponatraemia, gastric bleeding or ulceration, confusion, mastalgia, reversible gynaecomastia, impotence, menstrual irregularities, alopecia
Spironolactone - counselling
Serum K+ (dietary potassium- dried bananas/fruit, salt substitutes) and renal function
Varenicline - class and indication
Anti-smoking agent
indication: smoking cessation
Varenicline - dose
Initial: 0.5mg/day for 3 days, then 0.5mg bd for 4 days, then maintenance
Maintenance: 1mg bd for 11-23 weeks
Maximum: 2mg/day
Varenicline - MOA
Neuronal NAChR partial agonist = decrease withdrawal effects and decrease pleasure of smoking.
Varenicline - DIs
NRT (increase risk of AEs), CYP1A2 Inhibitor
Varenicline - Common AEs
Nausea, constipation, dyspepsia, flatulence, headaches, dizziness, taste disturbances, insomnia, abnormal dreams, mood disturbances
Varenicline - counselling
neuropsychiatric symptoms
Irbesartan - class and indication
Angiotensin II receptor antagonist
indication: Hypertension, reduction of renal disease progress in patients with Type II diabetes, hypertension, microalbuminuria, proteinuria
Irbesartan - dose
Initial: Hypertension- max effect 4-6 weeks after initiation o Oral: 150mg/day Prevention of renal disease progression o Oral: Maintenance dose 300mg/day Maintenance: 300mg/day Maximum: 300mg/day Situation where adjustment required: Elderly, renal impairment
Irbesartan - MOA
Competitively block binding of angiotensin II to type 1 angiotensin (AT1) receptors. They reduce angiotensin II-induced vasoconstriction, Na reabsorption and aldosterone release. They also reduce the effect of angiotensin II on SNS and growth factors.
Irbesartan - DIs
NSAIDs (increased risk of renal impairment), medicines that increase K+ concentration, Li, Digoxin, ACEI
Irbesartan - Common AEs
Dizziness, headache, hyperkalaemia, rash, diarrhoea, dyspepsia, muscle cramp, myalgia, insomnia, nasal congestion, cough, urticaria
Irbesartan - counselling
Renal function and electrolytes before initiation and after 1-2 weeks,
Atorvastatin - class and indication
statin dyslipidaemic
indication: Hypercholesterolemia, hypertensive patient with additional risk for heart disease
Atorvastatin - Dose
Initial: Increase after 4wk if required Adult: 10-80mg/day Child (>8yr): 10mg/day Maintenance: Maximum: 80mg/day Situation where adjustment required: Hepatic impairment
Atorvastatin - MOA
Competitively inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Increase hepatic cholesterol uptake from blood, reduce conc. of total cholesterol, LDL and triglyceride, and produce a small increase in HDL concentrations.
Atorvastatin - DIs
CYP3A4 substrate, fibrate, colchicine (increased risk of myopathy), sodium fusidate (oral) (CI), grapefruit juice
Atorvastatin - Common AEs
Myalgia (dose-related), mild transient GI sx, headache, sleep disturbance, dizziness
Atorvastatin - counselling
Monitor aminotransferase and creatine kinase at baseline, repeat if indicated
Target test results: Stop if aminotransferase concentration persistently elevated to >4 x ULN, CK concentration is >10 x ULN, persistent unexplained muscle pain or weakness
Simvastatin - class and indication
statin dyslipidaemic
indication: Hypercholesterolemia, high risk coronary heart disease
Simvastatin - Dose
Initial: Increase if required after 4 weeks, take at same time every day
Adult/>8yr: 10-40mg/day
CHD/risk
o 40mg/day
Maintenance:
Maximum: 80mg/day
Situation where adjustment required: Hepatic impairment
Simvastatin - MOA
Competitively inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Increase hepatic cholesterol uptake from blood, reduce conc. of total cholesterol, LDL and triglyceride, and produce a small increase in HDL concentrations.
Simvastatin - DIs
CYP3A4 substrate, fibrate, colchicine (increased risk of myopathy), sodium fusidate (oral) (CI), grapefruit juice, warfarin (possible INR increase)
Simvastatin - Common AEs
Myalgia (dose-related), mild transient GI sx, headache, sleep disturbance, dizziness
Simvastatin - counselling
Monitor aminotransferase and creatine kinase at baseline, repeat if indicated, INR monitoring if tx with warfarin
Target test results: Stop if aminotransferase concentration persistently elevated to >4 x ULN, CK concentration is >10 x ULN, persistent unexplained muscle pain or weakness
Rosuvastatin - class and indication
statin dyslipidaemic
indication: Hypercholesterolemia, high risk CV disease
Rosuvastatin - dose
Initial: Increase if required after 4 weeks Hypercholesterolemia o Oral: 5-10mg/day High CV risk: o Oral: 20mg/day Maintenance: Hypercholesterolemia o Oral: 5-20mg/day Maximum: Hypercholesterolemia o Oral: 40mg/day Situation where adjustment required: Concomitant ciclosporin or gemfibrozil or lopinavir with ritonavir, Asian ancestry (different max)
Rosuvastatin - MOA
Competitively inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Increase hepatic cholesterol uptake from blood, reduce conc. of total cholesterol, LDL and triglyceride, and produce a small increase in HDL concentrations.
Rosuvastatin - DIs
Fibrate, colchicine (increased risk of myopathy), sodium fusidate (oral) (CI), grapefruit juice, warfarin (possible INR increase)
Rosuvastatin - Common AEs
Headache, nausea, insomnia, myopathy, rhabdomyolysis, elevated serum transaminases, hepatitis, interstitial lung disease, hypersensitivity reactions
Rosuvastatin - counselling
Monitor aminotransferase and creatine kinase at baseline, repeat if indicated, INR monitoring if tx with warfarin
Target test results: Stop if aminotransferase concentration persistently elevated to >4 x ULN, CK concentration is >10 x ULN, persistent unexplained muscle pain or weakness
Predsnisolone - class and indication
corticosteriods
indication:
Predsnisolone - dose
Initial: Morning dose to avoid night time insomnia, in prolonged therapy calcium, vitamin D supplements and bisphosphonates may be required.
Adult: Dose determined by severity, prognosis, duration
o Range: 2.5-80mg/day in 1-4 doses or alternate days
o Acute asthma: 40-50mg/day for 3-10 days
o RA: 2.5-10mg/day
Child: Acute asthma: 0.5-2mg/kg/day for at least 3 days
o Croup: 1mg/kg, may be repeated after 12-24hrs
Autoimmune/inflammatory disease: 1-2mg/kg/day, when stabilised reduced to minimum effective dose
Maintenance:
Maximum: 80mg/day
Predsnisolone - MOA
nhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. Involves PPLA2 inhibitory proteins, lipocortin’s and thus prostaglandins. Limits capillary dilation and permeability of vascular structures.
Predsnisolone - DIs
Antihyperglycaemics, NSAIDs, diuretics, digoxin
Predsnisolone - Common AEs
Nausea, changed appetite, diarrhoea/constipation, headaches, mood change, diabetes, hypertension, heart failure, glaucoma, peptic ulcer disease, psychiatric disorders, etc.
Prednisolone - counselling
Blood glucose, electrolytes, weight, BP and BMD may be necessary
Amlodipine - class and indication
antihypertensive
indication: hypertension, angina
Amlodipine - dose
Initial:
Can take up to 2 weeks to decrease blood pressure
Adult: 2.5-5mg/day, increase when required after 1-2wk
<6yr: 0.05-0.2mg/kg/day, increase if required at intervals of 1-2 weeks to 0.6mg/kg, (in 2 doses may be more appropriate to control BP)
Elderly: 2.5mg/day
Maintenance: As above
Maximum: Adult: 10mg/day
Situation where adjustment required: Hepatic impairment, elderly
Amlodipine - MOA
Block inward current of Ca2+ into cells in vascular smooth muscle, myocardium and cardiac conducting system via L-type Ca channels. Acts on coronary arteriolar smooth muscle to reduce vascular resistance and myocardial oxygen requirements, relieving angina sx. Act mainly on arteriolar smooth muscle to reduce peripheral vascular resistance and BP.
Amlodipine - DIs
Simvastatin, CYP3A4 substrate, natural liquorice, grapefruit juice
Amlodipine - Common AEs
Nausea, vasodilatory effects (headache, flushing, dizziness, hypotension, peripheral oedema)
Amlodipine - counselling
monitoring
Diltiazem - class and indication
antihypertensive
indication: angina, hypertensive
Diltiazem - Dose
Initial:
Angina/AF/Atrial flutter
o Oral: 30mg tid/qid increase when required
o CR: 180mg/day, increase when required to 360mg/day
Hypertension (may take up to 2 weeks to lower BP)
o CR: 180-240mg/day increase prn to 360mg/day
Maintenance:
Maximum:
- Angina/AF/Atrial flutter: max 360mg/day in 3 or 4 dose
Situation where adjustment required: Hepatic impairment, elderly
Diltiazem - MOA
Block inward current of Ca2+ into cells in vascular smooth muscle, myocardium and cardiac conducting system via L-type Ca channels. Acts on coronary arteriolar smooth muscle to reduce vascular resistance and myocardial oxygen requirements, relieving angina sx. Act mainly on arteriolar smooth muscle to reduce peripheral vascular resistance and BP
Diltiazem - DIs
Medicines that slow cardiac conduction, CYP3A4 substrate, digoxin
Diltiazem - Common AEs
Nausea, vasodilatory effects (headache, flushing, dizziness, hypotension, peripheral oedema), rash,
Diltiazem - counselling
monitoring
HT: this medicine can take up to 2 weeks to reduce your blood pressure effectively
Verapamil - class and indication
antihypertensive
indication: SVT, AF/Atrial flutter, hypertension, angina
Verapamil -Dose
Initial:
Conventional tablet: 80-160mg bd or tid
Sustained released: 120-240mg bd or tid
Maintenance:
Angina: maintenance 160mg bd or tid
SVT/AF/Atrial flutter: maintenance 160mg bd or tid
Hypertension: maintenance 160mg bd or tid
Maximum: 480mg/day
Situation where adjustment required: Elderly and hepatic impairment
Verapamil - MOA
Block inward current of Ca2+ into cells in vascular smooth muscle, myocardium and cardiac conducting system via L-type Ca channels. Acts on coronary arteriolar smooth muscle to reduce vascular resistance and myocardial oxygen requirements, relieving angina sx. Act mainly on arteriolar smooth muscle to reduce peripheral vascular resistance and BP.
Verapamil - DIs
CYP3A4 substrate and inhibitor, beta-blockers (increased risk of hypotension, heart block), antiarrhythmics, digoxin
Verapamil - Common AEs
Constipation, bradycardia, AV block, development/worsening heart failure, ileus
Verapamil - counselling
monitoring
-this medicine can increase and prolong the effects of alcohol. Limit your alcohol intake until you know how it is going to affect you
Lercanidipine - class and indication
antihypertensive
indication: hypertension
Lercanidipine - dose
Initial: 10mg/day, increase if required after at least 2 weeks
Maintenance:
Maximum: 20mg/day
Situation where adjustment required: Hepatic impairment, renal impairment, elderly
Lercanidipine - MOA
Block inward current of Ca2+ into cells in vascular smooth muscle, myocardium and cardiac conducting system via L-type Ca channels. Acts on coronary arteriolar smooth muscle to reduce vascular resistance and myocardial oxygen requirements, relieving angina sx. Act mainly on arteriolar smooth muscle to reduce peripheral vascular resistance and BP
Lercanidipine - DIs
CYP3A4 substrate
Lercanidipine - Common AEs
Nausea, vasodilatory effects (headache, flushing, dizziness, hypotension, peripheral oedema)
Lercanidipine - counselling
monitoring
Glyceryl Trinitrate - class and indication
nitrate
indication: Prevention and tx of stable angina, heart failureassociated with acute MI
Glyceryl Trinitrate - dose
Initial:
Angina
o SL tab: 300-600 micrograms every 3-4min until pain resolved, max 1800 microgram
o SL spray: 400-800 micrograms (1-2 spray), repeat after 5 min prn to max 3 spray
Prevention chronic angina
o Patch: apply 1 x 5mg/24hr patch/day for 12-14hr each day, if required increase strength to 15mg/24hr
Maintenance:
Maximum: 1800microgram/day
Glyceryl Trinitrate - MOA
Provide exogenous source of NO (mediates vasodilator effects). Predominantly vasodilators, reduce venous return and preload to the heart = reducing myocardial oxygen requirement
Glyceryl Trinitrate - DIs
PDE-5 Inhibitors, vasodilators, antihypertensives
Glyceryl Trinitrate - Common AEs
Headache, flushing, palpitations, orthostatic hypotension, peripheral oedema, contact dermatitis, rebound angina
Glyceryl trinitrate - Counselling
monitoring
Isosorbide Mononitrate - class and indication
nitrate
indication:
Isosorbide Mononitrate - dose
Once daily dosing allows nitrate-free interval, minimising risk of tolerance with prolonged use
Initial: 30-120mg/day
Maintenance:
Maximum: 120mg/day
Situation where adjustment required: Renal impairment
Isosorbide Mononitrate - MOA
?
Isosorbide Mononitrate - DIs
PDE-5 inhibitors, vasodilators, antihypertensives
Isosorbide Mononitrate - Common AEs
Headaches (initially), hypotension, fainting tachycardia, loss of appetite, nausea, diarrhoea, rash
Isosorbide Mononitrate - counselling
monitoring
