Prescribing Flashcards
Describe the mechanism of action of insulin
When binds (beta chains link) = active tyrosine kinase = initiates phosphorylation cascade = GLUT 4 expression = allows uptake of insulin in cells
Name the role of insulin in the body
Liver - Decreases gluconeogenesis
Muscle + liver - increase glucogenesis and decrease glycogenolysis
Liver + adipose tissue - Increase glycolysis
Muscle, liver + adipose tissue - Increase amino acid uptake and protein synthesis
Decrease lipolysis
Fatty acids in liver + adipose tissue - increase lipogenesis + esterification
What type of compound is insulin
Anabolic
Name 2 drugs which have a potential severe interaction with insulin to cause hypoglycaemia
Clarithromycin
Metreleptin
Beta blockers?
What are SGLT-2 inhibitors used to treat
Type 2 diabetes
Describe the mechanism of action of SGLT-2 inhibitors
Expressed in the proximal renal tubules
Prevent reabsorption of filtered glucose from tubular lumen.
Increases urinary glucose excretion
What is the ending of SGLT-2 inhibitors
-liflozin
Name 4 examples of SGLT2 inhibitors
Canagliflozin
Dapagliflozin
Empagliflozin
Ertugliflozin
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When do you not prescribe SGLT-2 inhibitors
People with DKA
Moderate/severe renal impairment
- Avoid initiation < 60
- Avoid continuation < 45
Severe hepatic impairment
Describe the mechanism of action of GLP-1 inhibitors
Increases levels of hormones ‘incretins’ - stimulates secretion of of insulin and lowers blood glucose levels
What do GLP-1 inhibitors end in
- lutide
- atide
Name 2 of the additional benefits of GLP-1 inhibitors
Weight loss
Blood pressure reduction
Name the contradictions of GLP-1 inhibitors
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Ketoacidosis
Pancreatitis
Renal impairment
Severe hepatic impairment
Severe GI disease
Women childbearing age - contraception
Name 3 drug interactions of GLP-1 inhibitors
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Beta-blockers
Paracetamol
Warfarin
Describe the general mechanism of action of metformin
Increases peripheral sensitivity to insulin
Describe the 4 parts of the mechanism of action of metformin
- Inhibition of hepatic gluconeogenesis = decrease production of glucose
- Enhance insulin sensitivity = decrease insulin resistance
- Mitochondrial actions
- Weight loss
What is a main risk of metformin
Lactic acidosis
Name 3 drug interactions of metformin
Alcohol - Increases risk of lactic acidosis
Beta-blockers
Topiramate
Name 2 risk of metformin
Lactic acidosis
Low vitamin B12 levels on increased dose
Why should beta blockers be avoided with antidiabetic medication
Can mask the warning signs of hypoglycaemia
What condition are DPP-4 inhibitors used to treat
Type 2 diabetes
What do DPP-4 inhibitor drug names end in
-liptin
Describe the mechanism of action in DPP-4 inhibitors
Inhibits DPP-4 enzyme = increases beta-cell insulin secretion in the pancreas = reduces the post prandial and fasting hyperglycaemia
What are the contradictions and cautions of DPP-4 inhibitors
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Ketoacidosis
Hepatic impairment
Heart failure
Name 5 interactions of DPP-4 inhibitors
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Beta blockers
ACE inhibitors
Digoxin
Ketoconazole
Rifampicin
Describe the 1st line medical management for type 2 diabetes
High-risk of CVD/chronic heart failure = metformin + SGLT-2 inhibitor
Not above = metformin
What do you do if metformin is not tolerated such as due to GI side effects
Switch to modified-release metformin
What is 2nd line medical treatment for type 2 diabetes
Add one of:
DPP-4 inhibitors
Pioglitazone
Sulfonylurea
SGLT-2 inhibitor
What is 3rd line medical treatment of type 2 diabetes
Add another drug (from the 2nd line drug treatment list)
OR
Start insulin-based treatment
At what % Q-risk would a patient who is on metformin be prescribed as an add on a SGLT-2 inhibitor
QRISK > 10%
Describe the action of thrombolysis with alteplase
Alteplase = tissue plasminogen activator - rapidly breaks down clots
What are the side effects of thrombolysis with alteplase
Risk of intracranial or systemic haemorrhage
When can thrombolysis with alteplase be given and for what condition
4.5 hours after symptom onset
For ischemic stroke (must have ruled out haemorrhagic stroke)
In which type of stroke much blood pressure be sorted
Yes - aggressive haemorrhagic stroke
NO - ischaemic stroke
Describe the role of atorvastatin
Statin
Lower cholesterol and other lipids
Describe the general role of antiplatelets
Inhibit thrombus formation
Name 2 antiplatelet medications
Aspirin
Clopidogrel
Describe antiplatelet used in prevention
Primary prevention - atherothrombotic events for people at high risk
Secondary prevention:
- acute coronary syndrome
- stable angina
- peripheral artery disease
- undergoing cardiac interventions
- had a stroke or TIA
- AF
What combination of antiplatelet can be used in an acute MI ST-elevation
Clopidogrel and low dose aspirin
Describe the mechanism of action of clopidogrel
Antiplatelet
Inhibit the binding of ADP to its platelet P2Y12 receptor + blocks platelet activation and aggregation
When is clopidogrel used
Peripheral artery disease
MI
Ischaemic stroke
When is clopidogrel not prescribed
Active pathological bleeding e.g. peptic ulcer, intracranial haemorrhage
Renal/hepatic impairment
Describe the mechanism of action of aspirin
Antiplatelet
Irreversibility inhibits cyclo-oxygenase and blocks production of thromboxane
What use in aspirin indicated for
NOT indicated in primary prevention
Acute MI/unstable angina
TIA
Stroke
+ secondary prevention
What is aspirin contraindicated for
Asthmatics
What is the dose of aspirin
300mg then 75mg
Describe salbutamol
Short acting beta-2 agonist
Rapid onset (5 minutes)
Lasts up to 4 hours
Describe the mechanism of action of salbutamol
Bronchodilation
Stimulates beta-2 adrenoreceptors in the bronchial muscles = relaxation of bronchial smooth muscle + dilation of airways
What is the 1st line management in hypertension
Lifestyle
What is the 1st medical step of treatment of hypertension in a man with type 2 diabetes OR < 55, not black ethnicity
ACEi or ARB
What is the 2nd medical step of treatment of hypertension in a man with type 2 diabetes OR < 55, not black ethnicity
ACEi or ARB
+
CCB or thiazide diuretic
What is the 1st medical step of the treatment of hypertension in someone without diabetes + > 55 or black ethnicity
CCB
What is the 2nd medical step of the treatment of hypertension in someone without diabetes + > 55 or black ethnicity
CCB
+
ACEi or ARB or thiazide-like diuretic
What is the 3rd medical step in the treatment of hypertension
ACEi or ARB + CCB + thiazide diuretic
What is the 4th medical step in the treatment of hypertension
Confirm resistant hypertension
+
low dose spironolactone or alpha block or beta blocker
What is the role of an ARB
Allows blood vessels to relax + widen
Angiotensin II receptor blocker
Name an example of an ACEi
Ramipril
Name an example of a CCB
Amlodipine
What is the role of a thiazide diuretic
Helps the kidneys pass more fluid
What is the role of spironolactone
Potassium receptor antagonist
Diuretic
Describe the mechanism of action of Ramipril
Look at this is the bottom bit in relation to an ARB
Angiotensin-converting enzyme inhibitor
ACE involved in RAAS - stimulates the conversion of angiotensin I to angiotensin II
Angiotensin II is a vasoconstrictor - when inhibited - blood vessels are dilated and decreased aldosterone secretion
What medication must Ramipril be careful being prescribed with due to decreasing blood pressure
Diuretics
What do ACEi end in
pril
What 3 things are ACEi contraindicated against
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Angio-oedema
Diabetes < 60 eGFR
Pregnant women/breastfeeding
What type of medication is amlodipine
Calcium channel blocker
Describe the mechanism of action of amlodipine
Interferes with the inward displacement of calcium ions through the slow channels of active cell membranes.
Influence myocardial cells = decreased myocardial contractility = decrease blood pressure
Name the contraindications in amlodipine
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Cardiogenic shock
Significant aortic stenosis
Unstable angina
Elderly - STOPP criteria
Name 2 examples of a PPI
Lansoprazole
Omeprazole
Name 2 examples of a H2 receptor antagonist
Ametidine
Ranitidine
In what condition would H2 receptor antagonist be used
GORD
What type of drug is lansoprazole
PPI
Describe the mechanism of action of lansoprazole
Inhibits the membrane enzyme H+/K+ ATPase in gastric parietal cells = reduced stomach acid
What are the two main drugs in the treatment of autoimmune conditions in rheumatology
DMARDs
Biological agents
Describe the role of DMARDS
Disease modifying anti-rheumatic drugs
Dampen the immune system to reduce inflammation - aim to control disease progression
Describe how DMARDs can be taken
More than one can be used in combination
Oral or subcut
Name 4 examples of DMARDs
Methotrexate
Leflunomide
Sulfasalazine
Hydroxychloroquine
Name the side effects of methotrexate
DMARD
Bone marrow suppression
Neutropenia/neutropenic sepsis
Highly teratogenic
Toxic effects
Name the side effects of leflunomide
DMARD
Hypertension
Peripheral neuropathy
Name the side effects of sulfasalazine
Orange urine
Male infertility - reduces sperm count
Name the side effects of hydroxychloroquine
DMARD
Retinal toxicity
Blue-grey skin pigmentation
Hair bleaching
What must methotrexate be co-prescribed with
Folic acid
= reduce toxic effects
Describe the mechanism of action of methotrexate
Inhibits several enzymes responsible for nucleotide synthesis = suppresses inflammation and prevents cell division
When are biological agents given in autoimmune rheumatology
If DMARDs fail
Describe the role of biological agents in autoimmune rheumatology
Target specific signalling pathways/molecules
May be used in monotherapy or in combination with DMARDs
Expensive
Can develop antibodies to the drug overtime
Name 2 examples of biological agents in autoimmune rheumatology
Tumour necrosis factor inhibitors (anti-TNF)
B-cell direct
Name examples of tumour necrosis factor inhibitors (anti-TNF)
Adalimumab
Infliximab
Etanercept
Name an example of B-cell direct biological drug
Rituximab
Name 2 side effects of rituximab
Night sweats
Thrombocytopenia
Name the overall side effects of biological drugs
Immunosuppression
Opportunistic infection
Neutropenic sepsis
Reactivation of latent infections (e.g. TB)
Higher lifetime risk of cancer
What is the mechanism of action of rituximab
Monoclonal antibody that targets CD20, a protein expressed on the surface of B-cells
What is folic acid
Systemic form of B9
Describe the mechanism of action of folic acid
Biosynthesis of nucleotides for incorporation into DNA/RNA
Remyelination of homocysteine to form methionine
Methylation of substrates
Name 2 reasons why folic acid may be prescribed
Prevent neural tube defects
Reduce side effects of methotrexate
Describe the mechanism of action of NSAIDs
Non-selective inhibitor of cyclooxygenase (COX). (1 and 2)
COX is involved in synthesis of prostaglandins (mediators of pain and fever) and thromobane (stimulation of blood clotting) via the arachidonic acid pathway
Name 5 side effects of NSAIDs
Peptic ulcers
Renal dysfunction
Increased risk of cardiovascular events
Risk of hepatoxicity
Antiplatelet activation
NO - in 3rd trimester of pregnancy