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