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
when should tricyclic antidepressants be taken?
at night due to drowsiness
what kind of medication are dopamine D2 receptor antagonists?
Antiemetics
what are 3 examples of dopamine D2 receptor antagonists?
metoclopramide
prochlorperazine
domperidone
what cause of nausea are dopamine D2 receptor antagonists especially good at dealing with?
reduced gut motility
What is the MOA of D2 receptor antagonists?
triggering of vomiting centre in medulla which receives inputs from the chemoreceptor trigger zone (CTZ), the vagus nerve, vestibular system and higher centres. Dopamine D2 receptor is the main receptor in the chemoreceptor trigger zone which senses emetogenic substances. Dopamine also leads to gut relaxation and reduced motility. Therefore antagonism of dopamine receptors leads to increased gut motility and reduced triggering of CTZ.
what are the 2 different types of D2 receptor antagonists?
Benzamides - metoclopramide, domperidone
phenothiazines - prochlorperazine
what is the most common side effect of D2 receptor antagonists?
Diarrhoea
which 2 D2 receptor antagonists can cause extrapyramidal side effects?
metoclopramide
Prochlorperazine
Cross BBB
Which D2 receptor antagonists doesn’t cause extrapyramidal side effects and why?
Domperidone
Doesn’t cross BBB
which D2 receptor antagonists can cause drowsiness?
prochlorperazine
which D2 receptor antagonists can cause long QT and arrhythmias?
domperidone
which D2 receptor antagonists can be used in parkinsons?
Domperidone - doesn’t cross BBB
what conditions are all D2 receptor antagonists contraindicated in due to their prokinetic nature?
Bowel obstruction and perforation
who should metoclopramide be avoided in?
Neonates always!
Children and young adults
what condition should metoclopramide and prochlorperazine be avoided in?
PARKINSONS (and Lewy body dementia)
when is domperidone contraindicated?
severe hepatic impairment
cardiac conduction defects
children <12 years
Weight <35kg
what are 5 medications that inhibit cytochrome P450 enzymes?
amiodarone
Diltiazem
Macrolides - erythromycin, clarithromycin
fluconazole
protease inhibitors
what are 6 examples of medications that increase QT interval?
D2 receptor antagonists
Antipsychotics
SSRIs
Quinine
Amiodarone
Macrolides
what are 4 types of medications that shouldn’t be prescribed with D2 receptor antagonists?
Antipsychotics
Dopaminergic agents for parkinson’s - cancel each other out
Drugs that prolong QT
Drugs than inhibit cytochrome P450
what is the maximum duration of D2 receptor antagonists?
5-7 days
what is the stating dose for metoclopramide and domperidone?
10mg 8 hourly (TDS) PO if >60kg
500 micrograms <60kg
what is the dosing for IM and IV metoclopramide?
same as oral
give IVs slowly over 3 mins
what are 3 examples of Histamine H1 receptor antagonists used as antiemetics?
Cyclizine
Promethazine
Cinnarazine
what are Histamine H1 receptor antagonists used for in antiemesis?
prophylaxis of nausea and vomiting especially motion sickness and vertigo
what is the MOA of Histamine H1 receptor antagonists in antiemesis?
Histamine and muscarinic Ach are used in communication between vomiting centre and vestibular system so antagonism of histamine receptors inhibits nausea
what are 3 side effects of Histamine H1 receptor antagonists as antiemetics?
Drowsiness
Anticholinergic - dry mouth and throat, urinary retention, constipation, confusion
Tachycardia - after IV injection
what are 2 contraindications to Histamine H1 receptor antagonists used as antiemetics?
Prostatic enlargement - due to anticholinergic effect
Hepatic encephalopathy - due to drowsiness
what are 2 medication classes that interact with Histamine H1 receptor antagonists?
sedatives - benzos, opioids - may increase drowsiness
Anticholinergics - ipratropium, tiotropium
what is a typical prescription of cyclizine for nausea?
50mg 8 hourly PRN
what is the dosing for cyclizine IM and IV?
same as oral
How should iv cyclizine be administered?
slowly over 2 minutes
what are 2 examples of 5HT3 (serotonin) receptor antagonists?
Ondansetron
Granisetron
what are 5HT3 (serotonin) receptor antagonists used for?
nausea and vomiting particularly with chemo and general anaesthetics
what is the MOA of 5HT3 (serotonin) receptor antagonists?
There are 5HT3 receptors in chemoreceptor trigger zone which are stimulated by emetogenic substances in bloodstream. 5HT (serotonin) is a key neurotransmitter in gut which stimulates vagus nerve to activate vomiting centre. Blockade of these pathways reduces nausea.
Not effective in motion sickness as no involvement in vestibular system
what are 3 common side effects of 5HT3 (serotonin) receptor antagonists?
Constipation
Headache
Flushing
At what dose may ondansetron prolong QT?
> 16 mg
what can ondasetron cause in pregnancy?
congenital defects - cleft lip and palate, heart defects
what are 2 contraindications to 5HT3 (serotonin) receptor antagonists?
Pregnancy - congenital defects
Long QT
what medications shouldn’t be prescribed with 5HT3 (serotonin) receptor antagonists?
Those than prolong QT
SSRIs
Antipsychotics
Quinine
D2 receptor antagonists (antiemetics - metoclopramide)
what is the typical starting dose of ondansetron?
4-8mg 12 hourly oral or IV
dosage depends on indication - usually higher for chemo induced nausea
what are 3 examples of antifungals?
nystatin
clotrimazole
fluconizole
what is the MOA of antifungals?
target ergosterol on fungal cell membranes either by binding to it and creating a polar pore (nystatin) or by inhibiting ergosterol synthesis (clotrimazole, fluconizole)
what are 6 side effects of fluconazole?
GI upset
headache
increased liver enzymes
hypersensitivity and anaphylaxis
severe hepatotoxicity
prolonged QT and arrythmias
what are 4 contraindications to fluconazole?
Liver disease
QT prolongation
Renal impairment - requires dose reduction
Pregnancy - can cause foetal malformation
what medications does fluconazole interact with?
inhibits cytochrome p450 so increases concentration of anything metabolised through this pathway
- carbamezapine
- phenytoin
- Warfarin
- diazepam
- simvastatin
- sulphonureas
may reduce activity of colpidogrel as prodrug is metabolised through liver
Do not prescribe with medications that prolong QT
what is the dose of nystatin for oral thrush?
100 000 units - 1mL - oral suspension dropped into the mouth QDS for 7 days
what is the dosage for clotrimazole cream?
1% (1g in 100g)
Applied BD/TDS for 1-2 weeks
what is the dose for fluconazole in vaginal thrush?
150mg orally once
what is the dose of fluconazole for other infections?
50mg OD for 1-2 weeks
when should oral nystatin be administered?
After food
what are 4 H1-receptor antagonists used as amtihistamines?
certifizine
fexofenadine
loratadine
chlorphenamine
what are 3 indications for H1-receptor antagonists (antihistamines)?
1st line for tx of allergies particularly hayfever
for pruritus and urticaria
For skin symptoms in anaphylaxis
what is the MOA of H1-receptor antagonists ?
Block H1 receptor and therefore blocking the effects of histamine.
Histamine is release from storage granules in mast cells in response to antigens binding to IgE on the cell surface
which antihistamines causes sedation?
1st generation - chlorphenamine
which antihistamines don’t cross BBB?
fexofenadine
certirizine
loratadine
Do not cause drowsiness
In what condition are chlorphenamine antihistamines contraindicated?
severe liver disease due to risk of hepatic encephalopathy
what is the dose of certirizine?
10mg tablet once daily
what is the dose of chlorphenamine?
4mg tablets
2mg/5ml solution
every 4-6 hours
what is the dose of loratidine?
10mg tablets once daily
what are 4 examples of antimuscarinics used as bronchodilators?
tiotropium
umeclidinium
glycopyrronium
ipraropium
what are 2 respiratory uses of antimuscarinics?
COPD for acute breathlessness
Acute severe asthma and 3rd line in chronic management
what is the MOA of antimuscarinics?
competitively inhibit muscarinic receptors in place of acetylcholine
cause increase HR and conduction, reduced smooth muscle tone (GI, GU, Resp), reduce respiratory secretions, relax pupillary and cilliary muscles preventing accomodation
what are 5 adverse effects of antimuscarinics?
dry mouth, cough and hoarse voice
Tachycardia
constipation
urinary retention
blurred vision
Drowsiness and confusion
Less likely to have adverse effects when inhaled than with systemic use
what are 4 contraindications to antimuscarinics?
angle-closure glaucoma - can cause dangerous rise in orbital pressure
Arrythmias
Urinary retention and BPH
Older age and dementia
what type of antimuscarinic is ipratropium?
short acting
what dose of ipratropium is prescribed in stable COPD?
50micrograms every 6 hours via INH
what dose of ipratropium if prescribed in acute asthma/COPD exacerbations?
500micrograms nebulised every 4-6 hours as require - max dose 2mg
what antimuscarinic is used for muscle spasms in IBS?
hyoscine butylbromide
what medication is second line for muscle spasm in IBS?
meverine - may be better tolerated than hyoscine butylbromide
what antimuscarinics are used for reducing resp secretions in palliative care?
hyoscine butylbromide
Glycopyrronium bromide
what antimuscarinics are used for treatment of bradycardia?
Atropine
Glycopyrronium bromide
what medication can antimuscarinics interact with?
increased side effects when used in combination with medications with antimuscrinic side effects like TRICYCLIC ANTIDEPRESSANTS
what antimuscarinic and at what dose is usually given for bradycardia?
Atropine IV 500 micrograms every 5 mins up to max of 3mg
glycopyronium can also be given but is less readily available
what antimuscarinic is usually given or IBS and at what dose?
hyoscine butylbromide (buscapan) 10mg 8 hourly
what are 3 examples of antimuscarinics used for overactive bladder syndrome?
solifenacin
Oxybutynin
tolterodine
which antimuscarinic used for overactive bladder crossess the BBB and therefore causes confusion?
oxybutynin
what is the 1st line management for overactive bladder?
Bladder retraining
avoid caffeine
weight loss
what would a typical prescription for overactive bladder be?
tolterodine 2mg PO every 12 hours
how long can antimuscarinics used for overactive bladder take to work?
At least 4 weeks
What are 4 examples of anti-platelet medications?
Clopidogrel
Ticagrelor
Parasugrel
Aspirin
what are 3 indications for anti-platelets?
1 - Treatment of ACS
2 - Secondary prevention of major adverse cardiovascular event
3 - Prevention of stent occlusion
what class of medication are clopidogrel, ticagrelor and parasugrel?
ADP-receptor antagonists
what is the MOA of non-aspirin anti-platelets (e.g. clopidogrel)?
prevent platelet aggregation by irreversibly (clopidogrel and parasugrel) or reversibly (ticagrelor) binding to adenosine diphosphate (ADP) receptors on the surface of platelets
what are 3 adverse effects of non-aspirin antiplatelets?
Bleeding
GI upset - dyspepsia, pain, diarrhoea
Thrombocytopenia rarely
what are 4 contraindications to non-aspirin antiplatets?
bleeding - absolute contraindication
Elective surgery in next 7/52
renal impairment
hepatic impairment - especially with impaired clotting
co-prescribing non-aspirin antiplatelets with which 3 medication types increases bleeding risk?
anticoagulants
antiplatelets - aspirin
NSAIDs
what medications interact with clopidogrel?
any cytochrome P450 inhibitors reduce metabolism from prodrug
omeprazole
ciprofloxacin
erythromycin
antifungals
some SSRIs
Grapefruit juice
what PPIs are safe to use with clopidogrel?
lansoprazole
pantoprazole
what preparation is clopidogrel available as?
oral only
what is the loading dose of clopidogrel?
300mg once
what is the maintenance dose of clopidogrel?
75mg OD PO
how long should antiplatelets be given after a drug eluting stent is placed?
12 months - to reduce risk of stent thrombosis
How long are dual antiplatelets given after CV event or stroke?
12 months
then continue aspirin and stop ADP-receptor antagonist in CVD and vice versa in stroke
what is the MOA of Apirin?
irreversibly inhibits cyclooxygenase (COX) to reduce synthesis of the pro-aggregatory factor thrombane from arachidonic acid, reducing platelet aggregation
as irreversibly bound > lasts for lifetime of platelet 7-10 days
what are 4 side effects of aspirin?
GI upset
peptic ulceration and haemorrhage
Hypersensitivity and bronchospasm
Tinnitus - in high doses
what are the symptoms of aspirin (salicylate) overdose?
Hyperventilation
hearing changes
metabolic acidosis
confusion
cardiovascular collapse
respiratory arrest
what are 5 contraindications to aspirin?
Children <16 - Reye’s syndrome
Pregnancy in 3rd trimester - may precipitate premature closing od ductus arteriosus
Aspirin/NSAID hypersensitivity
Peptic ulceration
Gout - can trigger attack
what formulations of aspirin are available?
oral or rectal
what is the loading dose of aspirin?
300mg once
what is the usual dose of aspirin?
75mg OD PO
what is the maximum daily dose of aspirin?
4g
when should gastroprotection be considered in aspirin therapy?
> 65 years
comorbidities - diabetes, CVD
previous gastric ulcer
concurrent therapy with other gastric irritant medications - prednisolone, NSAIDs
How should aspirin be taken?
after food
what are 3 examples of typical (1st gen) antipsychotics?
Haloperidol
chlorpromazine
Flupentixol
what are 4 indications for typical antipsychotics?
Rapid tranquillisation
Schizophrenia - especially when metabolic side effects of atypicals are problematic
Bipolar - particularly acutely
Nausea and vomiting - palliative particularly
what is the MOA of typical antipsychotics?
block post synaptic dopamine (D2) receptors in 3 pathways - mesolimbic, nigrostriatal, tuberohypophyseal
blockade of which neural pathway causes exrapyramidal side effects by antipsychotics?
nigrostriatal pathway - connects substantia nigra to corpus striatum in basal ganglia
what are 4 extrapyramidal side effects?
acute dystonia - involuntary contractions
Akathisia - restlessness
Neuroleptic malignant syndrome
Tardive dyskinesia - automatisms e.g. lip smacking
what are 6 side effects of typical antipsychotics?
Extrapyramidal side effects
Long QT > Arrhythmias
Drowsiness
hypotension
erectile dysfunction
hyperprolactinaemia
what are 3 symptoms of hyperprolactinaemia?
galactorrhoea
menstrual disturbance
breast pain
what are 3 cautions in using typical antipsychotics?
older age
Dementia
parkinsons disease
what medications interact with typical antipsychotics?
MANY!!
Any that prolong QT - amiodarone, macrolides
what is the starting dose for haloperidol in agitation in the elderly?
500 micrograms IM or PO
what is the dose of haloperidol in agitation for adults?
1-10mg IM or PO
what monitoring is needed for typical antipsychotics?
prolactin at baseline, 6 months and yearly
baseline ECG
what medication can be used for intractable hiccups in palliative care?
chlorpromazine 25mg TDS
what are 4 examples of atypical antipsychotics?
quetiapine
olanzapine
risperidone
clozapine
what are 2 indications for atypical antipsychotics?
Schizophrenia - especially if had extrapyramidal side effects on typicals
Bipolar - particularly acutely
what is the difference in the MOA between typical and atypical antipsychotics?
atypicals work on same pathways but also affect 5HT2 receptors and bind more losely to D2 receptors meaning there are fewer side effects and are better at treating treatment resistant schizophrenia
what 3 side effects are less common in atypical antipsychotics?
drowsiness
cognitive impairement
extrapyramidal side effects
what are 4 side effects of atypical antipsychotics?
Extrapyramidal side effects - less common
Metabolic side effects - more common
long QT > Arrhythmias
Breast symptoms
what atypical antipsychotic often causes breast symptoms?
risperidone
what atypical antipsychotic often causes metabolic disturbance?
olanzapine
what are 2 rare side effects of clozapine?
agranulocytosis - low neutrophils
myocarditis
what are 3 metabolic disturbances common with atypical antipsychotics?
diabetes mellitus
weight gain
lipid changes
what are 2 contraindications to clozapine?
neutropenia
severe heart disease
when should atypical antipsychotics be used with caution?
cardiovascular disease
what are 2 medications that atypical antipsychotics should not be prescribed with?
D2 receptor antagonists - antiemetics
drugs that prolong QT
Other sedating drugs
How should atypical antipsychotics be taken?
at same time every day - if make drowsy, take at night
what monitoring should be done for atypical antipsychotics?
prolactin baseline, 6 months, yearly
Weight, lipid profile, fasting blood glucose baseline, 3 monthly, yearly
what extra monitoring is needed for clozapine?
FBC weekly for 18 weeks, then 2/52 for 1 year then monthly
what lifestyle factor can alter clozapine metabolism?
Smoking increases metabolism»_space; stopping smoking can cause rise in clozapine levels
what are 2 indications for aciclovir?
Treatment of herpes virus infections including HSV and VZV
Suppression of recurrent herpes simplex attacks happening more that 6x per year
what kind of viruses are herpes viruses?
DNA
Includes HSV1, HSV2 and VZV
what is the MOA of aciclovir?
enters herpes infected cells and inhibits herpes specific DNA polymerase stopping further replication
what are 6 side effects of aciclovir?
headache
dizziness
GI upset
rash
phlebitis - if IV
AKI - can precipitate in renal tubules, minimise risk by infusing slowly into well hydrated patient
what are 3 cautions for aciclovir?
pregnancy
breast feeding
severe renal impairment - renally excreted
what are 2 interactions for aciclovir?
can increase plasma conc of aminophylline and thenophylline
other nephrotoxic drugs - NSAIDs, methotrexate, antibiotics - aminoglycosides, cephalosporins, trimeth, vacomycin
what is the dose of aciclovir for oral or genital HSV outbreaks?
200mg 5x per day PO
what is the dose of aciclovir for suppression of recurrent disease?
400mg every 12 hours PO
what is the dose of aciclovir in herpes simplex encephalitis?
10mg/kg IV 8 hourly
for 14-21 days
what is the dose of aciclovir for VZV treatment?
800mg 5x per day for 7 days
what blood need to be monitored for safety in IV aciclovir?
renal function
what are 4 bits of self care advice for cold sores and genital herpes?
stay hydrated
topical analgesia
barrier preparations
OTC analgesia
what are 5 examples of antivirals?
Oseltamivir
nirmatrelavir
tenofovir
efaverezn
atanazavir
what are 3 indications for antivirals?
Treatment of viral infections - e.g. COVID
PrEP or PEP
Treatment to suppress load of hep A/B or HIV
what are 4 side effects of all antivirals?
Dizziness
GI upset
Sleep problems
Skin reactions
what is a side effect of inhaled zanamivir?
bronchospasm
what are 4 adverse effects of long term antivirals?
dyslipidaemia
hyperglycaemia
hypertension
weight gain
^^CVD risk factors
what are 4 adverse immune mediated effects of antivirals?
hypersensitivity reaction
hepatitis
blood diseases
severe cutaneous reactions
what is the MOA of oseltamivir and zanamivir?
inhibit neuroamidases - surface enzymes needed for viral entry and exit of host cells
what is the MOA of molnuparvir and remdesivir?
nucleotide analoges that block viral RNA synthesis
what are 2 examples of antiretrovirals?
emtricitibine
tenofovir
efavirenz
what is the MOA of antiretrovirals?
non/nucleoside reverse transcriptase inhibitors => inhbit synthesis of DNA from viral RNA
non-nucleoside reverse transcriptase inhibitors (NNRTIs) and protease inhibitors are contraindicated in what 2 conditions?
acute porphoria
QT prolongation
what is the dose of antiviral for influenza in adults?
oseltamivir 75mg po
zanamivir 10mg IHR
BD for 5 days for treatment
OD for 10 days for prophylaxis
what antigen can be tested for to reduce risk of hypersensitivity reaction to abacavir in those who carry it?
human leukocyte antigen
what ar 4 examples of benzodiazepines?
chlorodiazepoxide
lorazopam
midazolam
diazepam
what are 4 indications for benzodiazepines?
status epilepticus - 1st line
alcohol withdrawal reactions - 1st line
Sedation in palliative care, procedures or rapid tranquilization
Short term treatment of anxiety of insomnia
what is the MOA of benzodiazepines?
change shape of GABA receptors to facilitate binding and increase resistance to depolarisation of cells. Causes widespread depression of synaptic transmission leading to clinical effects of anti-anxiety, seizure cessation, sedation and sleepiness
How does alcohol affect GABA?
alcohol also increases binding of gaba and increased resistance to depolarisation leading to tolerance. When alcohol is abruptly withdrawn there is a decrease in GABA binding and therefore an increase in neuronal excitability leading to symptoms of alcohol withdrawal
what are 4 adverse effects of benzodiazepines?
drowsiness, sedation, coma
overdose - resp depression (less than opioids) and death due to loss of airway reflexes
Dependance
withdrawal effects
what is the best choice of benzo in liver failure?
lorazepam - less dependant on liver for elimination
what are 4 conditions to be cautious with when prescribing benzodiazepines?
the elderly - may need reduced dose
Respiratory impairement
Neuromuscular disease
Liver failure
using benzodiazepines with what medications may increase their effects?
cytochrome P450 inhibitors - amiodarone, macrolides, diltiazem, fluconizole, protease inhibitors
what medication(s) and what dose is usually given for stopping a seizure?
lorazepam 4mg IV
Diazepam 10mg IV
Midazolam 10mg buccally
what are 3 choices of benzodiazepines in alcohol withdrawal?
chlordiazepoxide - usually
Lorazepam
Diazepam
what benzodiazepine is preferred for procedural sedation?
midazolam as short acting
what is the antagonist to benzodiazepines?
Flumazenil
not usually used as can precipitate seizures
what are 4 examples of beta-agonists?
Salbutamol
Salmeterol
Formeterol
Indacaterol
what are 2 indications for beta agonists?
Asthma
COPD
what is the MOA of beta-agonists?
acts on beta receptors in smooth muscle of bronchi, gut, uterus and blood vessels leading to smooth muscle relaxation and bronchodilation
Also cause increased action of ATPase which shifts K+ into intracellular compartment causing hypokalaemia - beneficial in Tx of hyperkalaemia
what are 9 side effects of beta-agonists?
Fine tremor
tachycardia
palpitations
anxiety
headache
Hypokalaemia
Raised lactate
hyperglycaemia
muscle cramps - LABAs
what should always be prescribed with a LABA?
steroids
when should there be caution in prescribing beta-agonists?
in CVD as tachycardias may lead to tachyarrhythmias
what is a usual PRN prescription for salbutamol?
100-200 micrograms IHR PRN
what is the usual nebulised prescription of salbutamol?
2.5 mg nebulised 4 hourly
How long before LABA therapy can be ‘stepped down’?
3 months
what are 2 medications that when used with beta-agonists can increase risk of hypokalaemia?
thenophylline
corticosteroids
what are 5 examples of beta blockers?
Atenolol
Bisoprolol
Propanolol
Metoprolol
Carvedilol
what are 7 indications for beta blockers?
ischaemic heart disease - improves outcomes in angina and ACS
Heart failure - improves prognosis
AF - reduces ventricular rhythm and increases time spent in sinus
SVT - to restore sinus rhythm
Resistant HTN - 4th line
Prophylaxis of migraine
Thyrotoxicosis - for symtoms
what is the MOA of beta blockers?
act on beta1 adrenoreceptors to decrease heart rate and contractility
what are 7 side effects of beta blockers?
cold peripheries
fatigue
headache
GI upset
sleep disturbance
nightmares
impotence
what are 3 contraindications to beta blockers?
asthma
heart block
hypotension
what are 2 conditions to be cautious when prescribing beta blockers in?
Heart failure - start slowly and titrate
hepatic failure - may need dose reduction
what medication should not be used with beta blockers?
non-dihydropyridine calcium channel blockers - verapamil, diltiazem
may cause heart failure, bradycardia, asystole
when may IV beta blockers be needed?
SVT and AF - when quick action is needed
what advice should be given to those with heart failure being prescribed a beta blocker?
symptoms may initially get worse - seek medical advice is this occurs
what HR should be aimed for with beta blockers in IHD?
55-60 BPM
what measurement can be useful in initiation of beta blockers in heart failure?
daily weights for accumulation of fluids
How should beta blockers be stopped?
slowly over 2 weeks
abrupt withdrawal can lead to increased risk of Myocardial ischaemia
what are 4 examples of bisphosphonates?
alendronic acid
risendronate
disodium pamidronate
Zolendronic acid
what are 4 indications for bisphosphonates?
osteoporosis prevention - alendronic acid or risendronate 1st line
Hypercalcaemia due to malignancy - zolendronic acid and pamidronate
Bone mets - myeloma and breast Ca - reduce risk of pathological fracture
Paget’s disease of the bone
what is the MOA of bisphosphonates?
reduce bone turn over by inhibiting osteoclast activity and promoting apoptosis
what are 4 side effects of bisphosphonates?
Osteonecrosis of jaw - more common with IV
oesophagitis
hypophosphataemia
atypical femoral fractures
How are bisphosphonates excreted?
renally
what are 3 contraindications to bisphosphonates?
severe renal impairment
hypocalcaemia - check levels before commencing
upper GI disorders
what are 2 cautions in prescribing bisphosphonates?
smokers - increased risk of osteonecrosis of jaw
dental disease
what are 3 things that bisphosphonates interact with?
calcium salts including in milk
antacids
iron salts
should not be taken with any of these
who can take a weekly dose of bisphosphonate?
women
what is the usual dose of alendronic acid for osteoporosis?
10mg OD PO or 70mg once weekly PO
once weekly only in women
How long may it take for bisphosphonates to lower calcium levels in hypercalcaemia?
up to 1 week/10 days
How should bisphosphonates be taken orally?
Swallowed whole at least 30 minutes before breakfast or any other medications and taken with plenty of water
The patient should remain upright for at least 30 minutes after taking them
what advice needs to be given to people taking bisphosphonates?
Indication
Advice on how to take
symptoms of osophagaetis
Advise to see dentist
Advice on dosing especially in once weekly preparations
what needs to be monitored in bisphosphonates?
DEXA every 3-5 years
side effect monitoring
Blood for calcium levels
what are 2 vitamin D formulations?
colecalciferol
alfacalcidol
what are 2 types of calcium tablets?
calcium carbonate
calcium gluconate
what are 4 indications for calcium and vitamin D?
osteoporosis
CKD - for secondary hyperparathyroidism and renal osteodystrophy
Severe Hyperkalaemia - to prevent life threatening arrythmia
Hypocalcaemia - <1.9, or symptomatic
Vitamin D deficiency prevention and treatment
what are 5 symptoms of hypocalcaemia?
tetany - involuntary muscle contractions
seizure
parasthaesia
confusion
stiff, achy muscles
How does vitamin D help to absorption of calcium?
stimulating intestinal calcium and phosphorus absorption
stimulates bone calcium mobilization, increases renal reabsorption of calcium in the distal tubule
what are 2 side effects of oral calcium?
dyspepsia
constipation
what are 2 side effects of IV calcium gluconate?
tissue damage if accidentally given SC
Hypotension with rapid administration
what are 4 medications that oral calcium decreases absorption of?
Iron
bisphosphonates
levothyroxine
tetracyclines (doxy)
what is one medication that should not be mixed IV with calcium?
sodium bicarb - can cause precipitation
what is a usual dose of calcium in osteoporosis?
1 -1.2 g OD PO
what is the usual dose of vitamin D in osteoporosis?
400-800 units OD PO
what are the 2 different types of vitamin D?
D2 - from plant sources
D3 - from animal fats
what is the dose of calcium in severe hyperkalaemia?
30 ml calcium gluconate 10% for slow IV injection
How far apart should calcium and interacting medications be taken?
4 hours apart
what are 3 foods that could interact with calcium tablets and how far apart should they be eaten?
spinach
whole cereals
bananas
2 hours apart
what is the monitoring required for calcium administration?
ECG monitoring if IV
Serum calcium levels at regular intervals
how much stronger is calcium gluconate compared to calcium carbonate?
3X more calcium
what is the loading dose of vitamin d in deficiency?
50 000 units for 6 weeks
what are 5 examples of calcium channel blockers?
amlodipine
finodipine
nifedipine
diltiazem
verapamil
what are 3 indications of calcium channel blockers?
Tx of HTN
Angina control in IHD
Diltiazem and verapamil only - Rhythm control for supraventricular arrhythmias
what is the MOA of calcium channel blockers?
decrease calcium ion entry into vascular and cardiac cells reducing intracellular calcium concentration which causes relaxation and vasodilation in arterial smooth muscle
reduce cardiac contractility in heart by suppressing cardiac conduction through AV node => reduces myocardial demand => reduces angina
what type of calcium channel blockers are more selective for the heart?
non-dihydropyridines - verapamil (most cardio-selective), diltiazem
what type of calcium channel blockers are more selective for the vessels?
dihydropyridines - amlodipine, felodipine
what are 4 common side effects of amlodipine and nifedipine?
ankle swelling
flushing
headache
palpitations
what are 4 side effects of verapamil?
constipation
bradycardia
heart block
heart failure
what is the side effect profile of diltiazem?
can have all calcium channel blocker side effects
ankle swelling, flushing, headache, palpitations, constipation, bradycardia, heart block and heart failure
what are 2 conditions where verapamil and diltiazem should be used with caution?
impaired L ventricular function
Heart block/Av node delay
what are 2 contraindications to amlodipine and nifedipine?
unstable angina - vasodilation causes reflex increase in HR => increases angina
severe aortic stenosis - can cause collapse
what medication should non-dihydropyridine calcium channel blockers be prescribed with?
Beta blockers - both negatively inotropic
what is the only calcium channel blockers that can be given IV?
verapamil
how should modified release calcium channel blockers be prescribed?
with the brand name as bioequivalence differs
what is a standard dose of amlodipine for HTN?
5-10mg PO OD
what is a standard dose of MR diltiazem for angina?
90mg PO 12 hourly
what is the dose of verapamil for supraventricular arrhythmias?
40-120mg PO 8 hourly
what should be communicated with the patient when prescribing calcium channel blockers?
indication
measures to reduce other CVD risk factors
common side effects - ankle swelling
what are 2 indications for carbamezpine?
Seizures - 2nd line in focal
Trigeminal neuralgia
what is the MOA of carbamezapine?
not fully known
inhibits neuronal sodium channels stabilising resting membrane potentials and inhibiting repeated firing
what are 6 side effects of carbamezpine?
GI upset
neurological effects - dizzy, ataxia
oedema
hyponatraemia
skin rashes
hypersenitivity reactions and SJS/TEN
what genetic component is associated with carbamezpine and Steven johnson syndrome and what population is most affected?
HLA B-1502 allele
Han Chinese and Thai people
what can carbamezapine cause in pregnancy?
neural tube defects
cardiac and urinary tract abnormalities
cleft palate
what are 3 conditions to use carbamezapine with caution in?
hepatic, renal or cardiac disease
increased risk of toxicity
what medications does carbamezapine interact with?
is a cytochrome P450 INDUCER
reduces - warfarin, oestrogen, progesterones - metabolised by CYP450
carbamezpine conc is increased by CYP450 INHIBITORS - as also metabolised by CYP450
efficacy reduced by drugs that lower seizure threshold - antipsychotics, tramadol
interacts with other antiepileptics
how can carbamezapine be administered?
oral or rectal
what is the max dose of carbamezapine?
1.6g per day in divided doses
what is the usual starting dose of carbamezapine?
100-200mg OD PO
increase gradually to tolerance
what symptoms should patients started on carbamezapine be warned of?
signs of hypersensitivity
skin rashes, bruising, bleeding
high temperature, mouth ulcers - blood toxicity
reduced appetitie, abdo pain - liver toxicity
CONTRACEPTION
what is the driving advice for focal seizure epilepsy?
12 months seizure free or 6 months after withdrawal/change of medication
what are 3 cephalosporins?
cefalexin
ceftriaxone
cefuroxime
what are 2 carbopenems?
meropenem
ertapenem
what are oral cephalosporins used for?
2nd/3rd line in UTI and pneumonia/other resp tract infection (epiglotitis)
what are IV cephalosporins and carbopenems used for?
Very severe/complicated infections or antibiotic resistant infections
what is the activity of cephalosporins and carbopenems?
broad spectrum
increasing generations of cephalosporins increase activity against gram negatives
what is the MOA of cephalosporins and carbopenems?
contain BETA LACTAM RING
inhibit enzymes responsible for cross linking of peptidoglycan walls which weakens bacterial cell wall
what are 4 side effects of cephalosporins and carbopenems?
GI upset
C.Diff and antibiotic associated collitis
Hypersensitivity reaction - not concern for mild penicillin allergies
seizures
what are 2 cautions for cephalosporins and carbopenems?
renal impairment - requires dose reduction
at risk of C. DIff - older
what are 2 interactions for cephalosporins and carbopenems?
Enhance effect of warfarin - kill normal gut flora that synthesise vit K
Carbapenems - reduce plasma conc and efficacy of valporate
what is the usual adult dose of cephalosporin for bacterial meningitis?
Ceftriaxone 4mg IV OD
what is ertapenem?
a carbopenem that is administered once daily
what are the formulations of meropenem?
IV
what are the formulations of cephalosporins?
oral - suspension, tablet, capsule
IV/IM injection
what are 2 indications for general anaesthetic agents?
general anaesthesia
sedation
what are 3 IV general anaesthetics?
propofol
thiopental
ketamine
what are 2 inhaled general anaesthetic agents?
sevoflurane
nitrous oxide
what is the general MOA of general anaesthetics?
lipid soluble molecules that disrupt neuronal cell membranes especially potassium channels either directly or indirectly though disrupting crystallin lipids that surround them
Either enhance action of GABA (inhibitory neurotransmitter) or decrease action of NMDA (excitatory neurotransmittter) or nichotinic cholinergic receptors
what is one key side effect of propofol?
pain on injection
what are 3 common side effects of general anaesthetics?
bradycardia
Hypotension
vasodilations
which general anaesthetics does not cause brady, hypotension and vasodilation?
Ketamine - may cause hypertension and tachy
what is a common post operative side effect of general anaesthetics?
nausea and vomiting
what classification system is often used for anaesthetic ris§k?
american society of anaesthesiologists classification
what medications do general anaesthetics enhance the effect of?
other medications that reduce consciousness and cardiorespiratory function - benzos, opioids
what monitoring is needed with general anaesthetics?
BP
HR
RR
sats
Temp
ECG
End tidal CO2 - capnograph
what is the MOA of chloramphenicol?
Binds to ribosomes therefore inhibiting protein synthesis
bacteriostatic and can be bacteriocidal
what are 3 side effects of topical chloramphenicol?
stinging
burning
itching
what are 4 side effects of systemic chloramphenicol?
Dose related bone marrow suppression
Aplastic anaemia
Grey baby syndrome - neonates cannot alway metabolise
optical and peripheral neuritis
what are 5 contraindications to chloramphenicol?
Hypersensitivity
Bone marrow disorder
3rd trimester pregnancy
Breastfeeding
< 2 years
what is 1 caution in systemic chloramphenicol use?
hepatic impairement
what are 2 thing to communicate with patients having chloramphenicol eye drops?
may blur vision and do not drive is vision blurred
Avoid use of contact lenses
ho long should a course of chloramphenicol eye drop be?
48 hours after healing
what is the spectrum of clindamycin?
gram positive aerobes and anaerobes
what is the MOA of clindamycin?
binds to ribosomes and prevents protein synthesis
what are 6 side effects of clindamycin?
diarrhoea
Abdo pain
rashes and SJS
Abnormal liver enzymes
Antibiotic related colitis - C. diff
what is 1 contraindication to clindamycin?
acute porphyria
what is 1 condition to use clindamycin with caution in?
IBD
what is one interaction with clindamycin?
can increase effect of neuromuscular blocking drugs => delays postoperative recovery
what dose of topical clindamycin is used in acne?
1/2% once a day applied thinly
how should clindamycin be administered IV?
diluted in 5% glucose or normal saline and given over 10-60mins
what is the length of clindamycin course in acne?
6 months minimum