Top 100 Drugs Flashcards
what are 2 examples of 5 alpha-reductase inhibitors?
finaseteride
dutasteride
what drug class is finasteride?
5 alpha-reductase inhibitor
what are 2 indications for 5 alpha reductase inhibitors?
BPH causing LUTS
Androgenetic alopecia - male patterned baldness
what is the MOA of 5 alpha reductase inhibitors?
inhibits intracellular enzyme 5-alpha-reductase which converts testosterone to the more active dihydrotestosterone, stimulating prostatic growth
how long does it take 5-alpha-reductase inhibitors to work?
up to 6 months
what are 5 adverse effects of 5-alpha-reductase inhibitors?
Impotence
Reduced libido
breast tenderness and gynaecomastia
BREAST CANCER
SUICIDAL THOUGHTS
hair growth
what are the warnings needed with 5-alpha-reductase inhibitors?
NEVER in women - can cause genital birth defects in male foetuses
avoid contact with women of childbearing potential including with SEMEN
what is the starting dose of finasteride given for BPH?
5mg OD PO
review after 3-6 mon for efficacy then every 6-12 mon
what is the dose of dutasteride for BPH?
500 micrograms OD PO
what is the dose of finasteride for male patterned baldness?
10mg OD PO
what is the monitoring for 5-alpha reductase inhibitors?
review after 3-6 mon for efficacy then every 6-12 mon
what are 2 examples of Acetylcholinesterase inhibitors?
donepezil
rivastigimine
what are 2 indications for Acetylcholinesterase inhibitors?
mild to moderate Alzheimers
Mild to moderate dementia in parkinsons - rivastigimine
what is the MOA of Acetylcholinesterase inhibitors?
Ach is needed for memory and learning. Acetylcholinesterase inhibitors inhibit the breakdown of Acetylcholine in the CNS => increasing the availability of acetylcholine allowing for improved cognitive function and slower decline though this is not universal
what drug class is rivastigimine?
Acetylcholinesterase inhibitors
what drug class is donepezil?
Acetylcholinesterase inhibitors
what is the most common adverse effect to Acetylcholinesterase inhibitors?
GI upset
What can Acetylcholinesterase inhibitors cause in asthma and COPD?
Bronchospasm
what are 3 peripheral side effects of Acetylcholinesterase inhibitors?
Peptic ulcers and bleeding
Bradycardia
Heart block
what are 4 central cholinergic side effects of Acetylcholinesterase inhibitors?
hallucinations
altered/aggressive behaviour
extrapyramidal symptoms
neuroleptic malignant syndrome
what are 2 life threatening side effects of Acetylcholinesterase inhibitors?
neuroleptic malignant syndrome
Bronchospasm in asthma/COPD
what are 2 contraindications to Acetylcholinesterase inhibitors?
Sick sinus syndrome
heart block
what are 4 cautions in Acetylcholinesterase inhibitors?
Asthma
COPD
Peptic ulcers
Parkinsons - rivastigimine may worsen tremor
what are 2 medications that interact with Acetylcholinesterase inhibitors to increase risk of peptic ulcers?
NSAIDS
Systemic corticosteroids
what medications should be used with caution alongside Acetylcholinesterase inhibitors due to increased risk of neuroleptic malignant syndrome?
antipsychotics
what medications should be used with caution alongside Acetylcholinesterase inhibitors due to risk of Brady/heart block?
beta blockers
what medications can worsen cognitive decline so should not be used with Acetylcholinesterase inhibitors?
anticholinergics - antimuscarinics, tricyclic antidepressants
what are 5 medications that should be used with caution with Acetylcholinesterase inhibitors?
NSAIDs
Systemic corticosteroids
Antipsychotics
beta blockers
anticholinergics
what is the usual starting dose for donepezil?
5mg OD
what is the usual starting dose for rivastigimine?
1.5mg every 12 hours
when should donepezil be taken?
at night
may cause vivid dreams, in which case take in morning
which Acetylcholinesterase inhibitors is available as a patch?
rivastigimine
what is the monitoring for Acetylcholinesterase inhibitors?
review for adverse effects at 2-4 weeks
review for efficacy at 3 months - only continue if effective
what are 2 examples of aldosterone antagonists?
Spironolactone
Eplerenone - only licensed for CHF
What are 3 indications for aldosterone antagonists?
1 - Ascites and oedema due to liver cirrhosis - Spiro 1’
2 - CHF - Spiro 3’ in addition to Beta blocker and ACEi
3 - primary hyperaldosteronism
what is aldosterone?
Mineralocorticoids produced in glomerulosa of adrenal cortex and acts on mineralocorticoid receptors in distal tubule of kidney to increase activity of luminal epithelial sodium channel causing increased sodium and water retention and increased potassium excretion
what is the MOA of aldosterone antagonists?
Competitively inhibit mineralocorticoid receptors to decrease activity of luminal epithelial sodium channels causing increased sodium and water excretion and increased potassium retention
what are 4 adverse effects of aldosterone antagonists?
Hyperkalaemia
Gynaecomastia - SPIRO
Liver impairment and jaundice
Steven Johnsons syndrome - SPIRO
what are 5 signs of hyperkalaemia on ECG?
peaked T wave - tall tented
flattened P wave
prolonged PR interval
ST depression
prolonged QRS duration (broad QRS complexes)
what are 4 symptoms of hyperkalaemia?
muscle weakness
arrhythmia
cardiac arrest
nausea
what are 3 contraindications to aldosterone antagonists?
Renal impairment
Hyperkalaemia
adrenal insufficiency
what is one caution to aldosterone antagonists?
should be avoided in pregnancy and breast feeding - can cross placenta
what are 2 medications that should be used with caution with aldosterone antagonists?
ACEI and ARBs - also increase risk of hyperkalaemia
what is one medication hat should not be taken with aldosterone antagonists?
potassium
what is a typical starting dose for Spironolactone in CHF and resistant HTN?
25mg OD PO
what is a typical starting dose for spironolactone in ascites or nephrotic syndrome?
100mg OD PO
when should spironolactone be taken?
with food
what are 2 things patients should be told when starting on Spironolactone (or other aldosterone antagonists)?
May cause gynaecomastia/impotence
Need to come back for potassium monitoring
what monitoring is needed for aldosterone antagonists?
For safety - U+E (K+ and Creatinine) - 1 week after initiation and after any dose increase
monthly for first 3 months
then every 3 months for 1 year
then every 6 months
Also monitor for efficacy
what are 3 examples of antacids?
sodium bicarbonate
calcium carbonate
magnesium carbonate
what are 2 indications for antacids/alginates?
GORD
Dyspepsia
what is the MOA of alginates?
increase viscosity of stomach contents and lead to floating ‘raft’ seperating stomach contents from oesophagus
what is the MOA of antacids?
buffer stomach acid
what are 2 adverse effects of antacids?
magnesium salts - diarrhoea
Sodium salts - constipation
most compound alginates have few side effects
when should alginates/antacids be used with caution?
hyperkalaemia/fluid overload - e.g renal impairment
what interactions are there with alginates/antacids? (8)
Can reduce serum conc of:
- ACEI
- Bisphosphonates
- PPIs
- Digoxin
- Levothyroxine
- ABx - Tetracyclines, cephalosporins, ciprofloxacin
Can increase excretion of:
- aspirin
- lithium
Should leave 2 hours between interactive medications
what should alginates not be used with as cause too thick stomach contents?
thickened infant formula
how are alginates/antacids usually available as?
liquid or chewable tablets
what are 4 lifestyle measures to reduce GORD?
eat smaller meals more often
stop smoking
avoid food triggers - fatty, spicy
raise head of bed
what are 4 GORD red flags?
bleeding
vomiting
dysphagia
wt loss
what are 5 medications that may cause dyspepsia?
NSAIDs
antimuscarinics
aspirin
bisphosphonates
corticosteroids
what are 3 indications of allopurinol?
1 - gout prevention
2- prevention of uric acid and calcium oxalate renal stones
3 - prevent hyperuricaemia and tumour lysis syndrome in chemo
when is allopurinol used in gout prevention?
2+ attacks a year
OR joint damage
OR renal impairment
what is the MOA of allopurinol?
xanthine oxidase inhibitor
xanthine oxidase metabolises xanthine (from purines) to uric acid
what is second line to allopurinol?
febuxostat
non-purine xanthase oxidase inhibitor
what are 5 adverse effects of allopurinol?
May trigger gout attack on initiation
Skin rash
- Steven’s johnson syndrome/TEN
Allopurinol hypersensitivity syndrome
what are 3 contraindications to allopurinol?
acute gout attack (can continue but do not start treatment)
Recurrent skin rash
Severe hypersensitivity
what are 2 cautions for use of allopurinol?
renal impairment
hepatic impairment
Co-prescription of allopurinol and what medication increases risk of toxic levels of the drug due to it being metabolised by xanthine oxidase?
azathioprine
Co-prescription of allopurinol and what 2 medications causes increased risk of hypersensitivity reaction?
ACEi
thiazides
Co-prescription of allopurinol and what medication causes increased risk of skin rash?
Amoxicillin
what is the starting dose of allopurinol for gout?
100mg OD PO
titrate up to 200-600mg in 1/2 divided doses
what should be co-prescribed with allopurinol?
NSAIDs or Colchicine to prevent acute attack in first month/till uric acid levels stabalise
how should allopurinol be taken?
After meals
Maintain good hydration - 2-3L/day
what is the monitoring of allopurinol?
Uric acid levels after 4 weeks from starting/dose change
what uric acid level is aimed for in gout?
<300 umol/L
what are 3 medication that can trigger gout?
Increase serum uric acid conc:
-Thiazide diuretics
-Loop diuretics
Decrease uric acid excretion:
-Aspirin
What are 3 examples of alpha blockers?
Tamsulosin
Doxazosin
alfuzosin
what are 2 indications of alpha blockers?
1 - To improve LUTS in BPH
2 - resistant HTN - 4th line after ACEI, CCB and thiazide diuretic
what is the MOA of alpha blockers?
Highly selective inhibitors of alpha1-adrenoreceptors causing smooth muscle relaxation in both blood vessels and urinary vessels
what are 3 adverse effects of alpha blockers?
Dizziness
syncope
Postural hypotension
Due to effect on vascular smooth muscle
who should not be given alpha blockers?
people with postural hypotension
what is an important consideration when starting alpha blockers?
May need to omit dose of antihypertensive or Beta-blocker to prevent 1st dose postural hypotension
Also may need to advise on risk of hypotension in combination with phosphodiesterase-5 inhibitors (sildenafil)
which alpha blocker is licenced for both BPH and HTN?
Doxazocin
which alpha blocker is licenced in BPH only?
Tamsulosin
what is the dose of doxazocin for HTN?
1mg OD and then increase after 1/2 weeks to 2mg then to response up to max of 16mg OD
what is the dose of doxazocin for BPH?
1mg OD and titrate 1/2 weekly to response up to max of 16mg OD
what is the dose of tamsulosin?
400micrograms OD
when should alpha blockers be taken?
At night due to effect on BP
What are 3 examples of aminoglycosides?
gentamicin
amikacin
neomycin
what type of bacteria do aminoglycosides treat?
gram negative aerobes
including pseudomonas aeruginosa
what are 5 indications for aminoglycosides?
1 - Sepsis
2 - Pyelonephritis - NOT 1st line
3 - Intrabdominal infections - diver with metro and co-amox
4 - Endocarditis
5 - Otitis externa - neomycin
what is the spectrum of activity of aminoglycosides?
treat gram negative aerobes, staph and mycobacteria
NO ACTIVITY AGAINST - strep and anaerobes - often used in combo with penicillin and metronidazole
what is the MOA of aminoglycosides?
Bind irreversibly to bacterial ribosomes and inhibit protein synthesis
Enter cells through oxygen-dependent transport systems so only work in aerobes and staph
what are 2 adverse effects of aminoglycosides?
ototoxicity
nephrotoxicity
Accumulate in tubular epithelial cells and cochlear and vestibular hair cells
what are 4 cases where aminoglycosides can be used but with caution?
Neonates
Elderly
Renal impairment
Myasthenia Gravis - can impair neuromuscular transmission
what 2 medications increase risk of ototoxicity in aminoglycosides?
loop diuretics
glycopeptide antibiotics - vancomycin, teicoplanin, etc
what 4 medications increase the risk of nephrotoxicity in aminoglycosides?
loop diuretics
glycopeptide antibiotics - vancomycin, teicoplanin, etc
Cephalosporins - cephalexin, ceftriaxone
NSAIDs
Other nephrotoxic drugs
How are aminoglycosides administered?
Parenterally as NOT absorbed by gut
Usually OD IV over 30 minutes - given every 24 hours but can be up to 48 hourly in renal impairment
can be given locally
what need to be measured before administering aminoglycosides?
renal function
what monitoring is needed for aminoglycosides?
Trough levels taken 18-24 hours after dose or mid interval concentration taken 6-14 hours after dose to determine whether it is safe to give the next dose and when
what is the safe trough level of gentamicin?
<1 mg/mL
How do you calculate adjusted body weight?
[ideal body weight] + 0.4x [actual body weight] - [ideal body weight]
what weight is used to calculate aminoglycosides doses?
adjusted body weight
what are 2 aminosalicylates?
Mesalazine
Sulfasalazine
what are 2 indications for aminosalicylates?
1 - For mild-moderate UC - Mesalazine 1ST LINE - Sulfasalazine can also be used
2 - For RhA - Sulfasalazine - DMARD
What is the MOA of aminosalicyclates?
release 5-aminosalicylic acid - exat MOA unknown but thought to have local anti-inflammatory and immunosuppressive properties
what are 6 side effects of aminosalicyclates?
GI upset - most common - more with sulfasalazine
Headache
Blood abnormalities - leukopenia, thrombocytopenia
renal impairment
oligospermia
hypersensitivity reaction
what medication are aminosalicyclates related to?
ASPIRIN
who cannon take aminosalicyclates?
people with Aspirin allergies as also a salicylate
what are 2 medications that may interact with aminosalicyclates?
PPIs - may cause premature capsule breakdown
Lactulose - may cause delayed capsule breakdown
in tablets with pH sensitive coating
what is the prescription for aminosalicyclates in mild/moderate UC?
1st line - Mesalazine enema/suppository every 12/24 hours for 4-6 weeks to induce remission
can also be taken orally if preferred
what monitoring should be done with aminosalicyclates?
Mesalazine - renal function
Sulfasalazine - FBC and LFTs
what is amiodarone used for?
AF
Atrial flutter
supraventricular tachycardia
ventricular tachycardia
refractory ventricular fibrillation
usually not 1st line
What is the MOA of amiodarone?
effects myocardial cells including blockading sodium, calcium and potassium channels
Also Antagonises alpha and beta adrenergic receptors
Reduces spontaneous depolarisation and increases refractor period
What are 6 long term side effects of amiodarone?
Pneumonitis
Bradycardia
AV block
Hepatitis
Skin - photosensitivity and grey discolouration
Thyroid abnormalities - due to iodine content
What is amiodarone’s half life like?
long - 25 to 100 days
What is a short term side effect of IV amiodarone?
Hypotension
When should amiodarone be avoided? (3)
Severe Hypotension
heart block
active thyroid disease
What are 3 medications that amiodarone increases plasma concentrations of ?
Digoxin
Diltiazem
Verapamil
Dose should be halved if starting amiodarone
What food should be avoided with amiodarone?
Grapefruit juice
Down regulates cytochrome P450 3A4 increasing amiodarone exposure
Long half life so should be avoided after exposure
When is amiodarone given in ALS?
In cardiac arrest with VF OR pulseless VT
Give immediately after 3rd shock
What is the dose of amiodarone given in ALS?
300mg IV
Followed by 20ml 0.9% saline or 5% glucose flush
what is a complication of peripheral administration of amiodarone?
phlebitis
How is amiodarone usually administered?
through central line
What should always be done when administering amiodarone?
continuous cardiac monitoring
what is the monitoring for long term amiodarone?
Renal, liver and thyroid monitoring baseline and 6 monthly
Baseline CXR
What are 3 examples of local anaesthetics?
lidocaine
Bupivacaine
levobupivacaine
what are 3 indications for local anaesthetics?
Surface anaesthesia
SC local anaesthesia
Regional anaesthesia - spinal/epidural
For what non-anaesthetic purpose can lidocaine be used?
2nd line for ventricular tachycardia
what is the MOA of local anaesthetics?
reversibly inhibit voltage gated sodium channels on plasma membranes
Prevents initiation and propagation of action potentials in neurones
What property of lidocaine makes it good for topical anaesthesia?
readily absorbed through epithelia and has rapid onset
what local anaesthetic is good for blocks and epidurals?
bupivacaine
high affinity to binding sites and long duration
what is the most common side effect of local anaesthetics?
stinging at injection site
what are 6 effects of IV administration of local anaesthetics?
drowsiness
restlessness
tremor
seizures
Hypotension
arrhythmia
what are 5 complications of local anaesthetics for blocks/epidruals?
infection
bleeding
higher than intended anaesthetic level
Hypotension and bradycardia - blockage of sympathetic fibres
weakness/paralysis
what are 2 cases in which local anaesthetics should be used with caution?
Hepatic impairment
cardiac failure
metabolised hepatically and reliant on hepatic blood flow
what medication can be given with local anaesthetics to prolong their effect?
Vasoconstrictors - adrenaline
what local anaesthetic is usually used for SC local anaesthesia and what dose?
1% (10mg/ml) solution of lidocaine hydrochloride up to a max dose of 3mg/kg or 200mg (whatever is lower)
If combined with adrenaline can go up to 7mg/kg or 500mg
what is the brand name of topical anaesthetic cream?
Emla 5%
What are 3 examples of angiotensin receptor blockers (ARBs)?
losartan
candesartan
irbesartan
what are 4 indications for ACEI/ARBs?
1 - hypertension - 1st/2nd line
2 - heart failure
3 - secondary prevention of cardiac events
4 - diabetic nephropathy and CKD with proteinuria
what is the MOA of ARBs?
blocks action of angiotensin II on angiotensin type I receptor
angiotensin II causes vasoconstriction so blocking it’s effect leads to vasodilation including of the efferent arteriole in the kidney reducing pressures. Also reduces amount of aldosterone secreted leading to increased sodium and water excretion which is beneficial in heart failure
what are 3 adverse effects of ARBs?
hyperkalaemia
hypotension
renal failure - in renal artery stenosis due to inadequate filtration pressures
what are 2 cases where ACEI/ARBs should be avoided?
Renal artery stenosis
AKI
what are 3 cases where ACEI/ARBs should only be used with caution?
Pregnancy
breast feeding
CKD - use lower doses and monitor closely
what are 4 medications that ARBs shouldn’t be prescribed with?
Potassium supplements
aldosterone antagonists
potassium sparing diuretics
NSAIDs - due to nephrotoxicity risk
what is the usual starting dose for losartan in heart failure?
12.5mg OD
what is the usual starting dose for losartan HTN and as secondary prevention?
50mg OD
what is the max dose of losartan?
100mg
what is the safety monitoring for ARBs?
take baseline U+Es and renal function then take at 1-2 weeks and after dose adjustment
at what GFR or creatinine should ACEI/ARBs be stopped?
If serum creatinin conc rises >30%
If GFR falls >25%
at what serum potassium level should ACEI/ARBs be reduced and at what level should they be stopped?
reduce at 5 mmol/L
STOP at 6 mmol/L
what are 3 examples of Angiotensin converting enzyme inhibitors (ACEI)
ramipril
lisinopril
peridopril
what is the MOA of ACEI?
inhibit action of angiotensin converting enzyme reducing the conversion of angiotensin I to angiotensin II
what are 6 adverse reactions to ACEIs?
hypotension
hyperkalaemia
renal failure
dry cough
angioedema
anaphylaxis
what is a common starting dose for ramipril in heart failure?
1,25mg od
what is a common starting dose for ramipril in HTN?
2.5mg OD
what is the max dose for ramipril?
10mg
What are 4 examples of selective serotonin reuptake inhibitors (SSRIs)?
Sertraline
Fluoxetine
Citalopram
Escitalopram
what are 3 indications for SSRIS?
depression - 1st line in moderate/severe and 2nd after CBT in mild
Panic disorder/PTSD/Social anxiety
OCD
What is the MOA of SSRIs?
inhibit neuronal uptake of 5-hydroxytraptamine (5-HT)from the synaptic cleft
what are 9 side effects of SSRIs?
GI upset
appetite/weight change
hypersensitivity reaction
Hyponatraemia
Suicidal thoughts/behaviour in first few weeks
lowered seizure threshold
Prolonged QT - citalopram
increase bleeding risk
serotonin syndrome
what are 4 side effects of SSRI withdrawal?
GI disturbance
neurological symptoms - zaps
flu-like symptoms
sleep disturbance
which SSRI causes long QT?
citalopram
when are 4 times SSRIs should be used with caution?
Hepatic impairment
young people - children - limited efficacy
epilepsy
peptic ulcer disease
what medications interact with SSRIs?
monoamine oxidase inhibitors
serotonergic drugs - triptans, tramadol
Bleeding risk - aspirin, nsaids, anticoagulants - also gastroprotection
Drugs that prolong QT (antipsychotics) and citalopram
what is the typical starting dose for sertraline?
50mg OD
what is the typical starting dose for citalopram?
20mg OD
does citalopram have higher bioavailability in tablets or drops? what is the dosage difference?
DROPS!
20mg tablets equivalent to 16mg drops
what is the monitoring of SSRIs?
review after 1-2 weeks
maintain dose for 6-8 weeks before changing
continue therapy till at least 6 months after symptoms have gone
what SSRI can be stopped suddenly due to longer half life?
fluoxetine
how should SSRIs be stopped?
slowly over 4 weeks reducing dose or frequency
what 2 SSRIs shouldn’t be prescribed with tamoxifen?
paroxetine
fluoxetine
as they inhibit CYP2D6
what drug class are duloxetine and venlofaxine?
serotonin noradrenaline reuptake inhibitors (SNRIs)
what drug class is mertazipine?
tetracyclic antidepressant
what SNRI can be used for diabetic neuropathy?
duloxetine
what is mirtazapine indicated for?
depression
what are venlefaxine and duloxetine indicated for?
Depression
Generalised anxiety disorder
diabetic neuropathy - duloxetine
what is the MOA of mirtazapine (tetracyclic antidepressant)?
antagonises inhibitory pre-synaptic alpha adrenoreceptors. Increases availability of monoamines for neurotransmission
fewer antimuscarinic side effects than tricyclics
what are side effects of SNRIs and mirtazapine?
GI upset
dry mouth
neurological effects - headache, insomnia, abnormal dreams
hyponatraemia
serotonin syndrome
which SNRI can cause long Q-T?
Venlafaxine
what is a serious side effect of mirtazapine?
bone marrow suppression
what SNRI is associated with greater risk of withdrawal symptoms?
venlafaxine
in what 4 cases should SNRIs/Mirtazapine be used with cation?
Older people
renal impairment
hepatic impairment
arrythmias
what medications shouldn’t be used with SNRIs/Mirtazapine?
other antidepressants
what is the typical starting dose for duloxetine in neuropathic pain?
60mg OD
When should mirtazapine be taken?
at night as can be sedating
what are 3 tricyclic antidepressants?
amitriptyline
nortriptyline
lofepramine
what class of medication is trazodone?
serotonin-antagonist-and-reuptake-inhibitor
what are 4 indications of tricyclic antidepressants?
depression
neuropathic pain
IBS - 2nd line after antispasmodic (antimuscarinic or mebeverine)
Migraine prophylaxis - Amitryptiline - 3rd line
what is the MOA of tricyclic antidepressants?
inhibit neuronal uptake of 5-hydroxytriptamine (serotonin) and noradrenaline
Block muscarininc, adrenergic, dopamine and histamine receptors
what are 12 side effects of tricyclic antidepressants?
Dry mouth
constipation
urinary retention
cognitive impairment
sedation
hypotension
arrhythmias - long QT
breast changed
extrapyramidal symptoms - tremor, dyskinesia
sexual dysfunction
what are 6 patients that tricyclic antidepressants should be used with caution in?
Older people
epilepsy
cardiovascular disease
constipation
glaucoma
prostate enlargement
what medications should tricyclic antidepressants NOT be given with?
monoamine oxidase inhibitors - increase risk of hypertension, hyperthermia and serotonin syndrom
what is the typical starting dose of amitriptyline in neuropathic pain?
10mg OD at night
what formulations are tricyclic antidepressants available as?
tablets and oral solution