Drugs! Flashcards
Varenicline
Nicotinic receptor partial agonist
Binds selectively to alpha4 beta 2 nicotinic acetylcholine receptors of the brain - reducing pleasure and satisfaction associated with smoking. Helps decrease nicotinic cravings and withdrawal symptoms.
Use in caution for patients with depression or self harm. Contraindicated in pregnancy and breastfeeding.
Side effect: abnormal dreams! nausea. Other problems: headache, insomnia, abnormal dreams
Roflumilast
Oral phospodiesterase-4 inhibitors (PDE-4)
Reduce risk of COPD in patients with severe COPD (FEV1 <50% after bronchodilator & has 2 or more exacerbations per year despite triple therapy) and history of frequent exacerbations.
Terbutaline
SABA
(like salbutamol)
Tiotropium
LAMA
Beclomethasone (&budesonide) VS fluticasone
Both are inhaled steroids
Fluticasone is more potent
Bupropion
Norepinephrine and dopamine reuptake inhibitor & nicotinic antagonist
Used as smoking cessation.
Small risk of seizures
Contraindicated in epilepsy, pregnancy and breastfeeding. Having eating disorder is a relative contraindication.
Pirfenidone
Anti-fibrotic
Nintedanib
Cancer drug
Memantine
NMDA antagonist
Serotonin antagonist
Dopamine agonist
Donepezil
Contraindication for using donepezil
Acetylcholinesterase and butyrylcholinesterase inhibitor
(Another example is rivastigmine)
Donepezil should not be used for patients with bradycardia/sick sinus syndrome/AVN block. Adverse effect include insomnia
Phenytoin - mechanism of action
Binds to sodium channels and increase their refractory period
Side effect of phenytoin
Induced CYP450
Teratogenic- cleft palate, congenital heart problems
Acute- dizziness, diplopia, nystagmus, slurred speech, ataxia -> confusion, seizures
Chronic - gingival hyperplasia (due to increased PDGF), hirsutism, course facial features, drowsiness, peripheral neuropathy
Idiosyncratic- fevers, rashes, hepatitis, Dupuytren’s contracture, aplastic anaemia
Methylphenidate
CNS stimulant
Dopamine/norepinephrine reuptake inhibitor
Side-effects include abdominal pain, nausea and dyspepsia
Example of xanthine oxidase inhibitor
allopurinol
febuxostat
Colchicine
inhibits microtubule polymerization by binding to tubulin, interfering with mitosis. Also inhibits neutrophil motility and activity
has a slower onset of action
may be used with caution in renal impairment: the BNF advises to reduce the dose if eGFR is 10-50 ml/min and to avoid if eGFR < 10 ml/min
the main side-effect is diarrhoea
Dont use when taking p-glycoprotein inhibitors ( as it can increase colchicine concentration) - eg clarithromycin, erythromycin, ritonavir, verapamil.
Dont use when taking strong CYP3A4 inhibitors - clarithromycin, telithromycin, nefazodone, itraconazole, ketoconazole, atazanivir, darunavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, tipranavir.
Hydroxychloroquine
Used for RA and SLE/discoid SLE
Pharmacologically similar to chloroquine
Can be used in pregnancy
Adverse effect: bull’s eye retinopathy - may result in severe and permanent visual loss. RCOphth guidelines (March 2018) suggest colour retinal photography and spectral domain optical coherence tomography scanning of the macula
baseline ophthalmological examination and annual screening is generally recommened
Methotrexate
Not to be used for pregnancy
Don’t use with trimethoprim or co-trimoxazole (increases risk of marrow aplasia).
Aspirin increases risk of methotrexate toxicity due to reduced secretion.
Tx of toxicity: folinic acid.
Common side effects of: methotrexate
Myelosuppression
Liver cirrhosis
Pneumonitis
Common side effects of: sulfasalazine
Rashes
Oligospermia
Heinz body anaemia
Interstitial lung disease
Common side effects of: leflunomide
Liver impairment
Interstitial lung disease
Hypertension
Common side effects of: hydroxychloroquine
Retinopathy
Corneal deposits
Common side effects of: prednisolone
Cushingoid features
Osteoporosis
Impaired glucose tolerance
Hypertension
Cataracts
Common side effect of gold
Proteinuria
Common side effect of penicillamine
Proteinuria
Exacerbation of myasthenia gravis
Common side effect of etanercept
Demyelination
Reactivation of tuberculosis
Common side effect of:
- infliximab
- rituximab
- adalimumab
infliximab & adalimumab: reactivation of TB
rituximab: infusion reactions
Common side effect of NSAIDs
Bronchospasm in asthmatics
Dyspepsia/peptic ulceration
Mechanism of action of alendronic acid
Reduce bone turnover - reduced amount of calcium in blood from bone stores.
Finasteride
5-alpha reductase inhibitor
Stops conversion of testosterone to DHT therefore, reducing the size of prostate.
Tamsulosin
alpha 1 receptor blocker
works at the bladder neck and prostate that causes relaxation of smooth muscles
first line treatment for BPH
metformin ?contraindicated in chronic kidney disease
if eGFR<45, dose review
if eGFR <30, stop tx
drugs causing thrombocytopaenia
quinine
abciximab
NSAIDs
diuretics: furosemide
antibiotics: penicillins, sulphonamides, rifampicin
anticonvulsants: carbamazepine, valproate
heparin
(probably immune related)
signs of salicylate poisoning
tinnitus is first sign
hyperventilation (centrally stimulates respiration)
lethargy
sweating, pyrexia*
nausea/vomiting
hyperglycaemia and hypoglycaemia
seizures
coma
indications for haemodialysis for salicylate poisoning
serum concentration > 700mg/L
metabolic acidosis resistant to treatment
acute renal failure
pulmonary oedema
seizures
coma
Drugs causing ototoxicity
loop diuretics
aminoglycoside (gentamicin)
Contraindication to viagra (ie phosphodiesterase inhibitor) for erectile dysfunction
Recent MI/stroke
Unstable angina
Patients in whom vasodilation or sexual activity is not advisable
Patients receiving nitrates
Previous history of non-arteritic anterior ischaemic optic neuropathy
Hypotension (esp if SBP<90)
warning when using monoamine oxidase inhibitors!
when patient eats cheese (strong or aged) or smoked/aged meats, alcohol beverages, some fermented food, yeast extract spreads and various sources -they are HIGH in tyramine.
Tyramine has direct and indirect sympathomimetic actions.
MAOi inhibit breakdown of tyramine.
causes hypertensive reaction & can lead to death.
Eg MAOi: Isocarboxazid (Marplan), Phenelzine (Nardil), Selegiline (Emsam), Tranylcypromine (Parnate)
amiodarone
AKA - photosensitiser (ie sunburn)
causes:
grey discolouration of skin
pulmonary fibrosis
hypo/hyperthyroidism
corneal deposits
liver hepatitis/fibrosis
peripheral neuropathy
bradycardia
prolonged QT syndrome
side effect of beta-blockers
(hint: i want sexual side effect)
impotence/erectile dysfunction
Nicorandil
used for angina
activate ATP-dependent potassium channels -> relaxation of vascular smooth muscles (esp venous) -> reduced ventricular filling pressure and myocardial workload.
side effect: headache (most common), oral ulcer, stomatitis
Should NOT use sildenafil as it can worsen the hypotension effect of nicorandil .
what drugs causes gum hypertrophy?
phenytoin
nifedipine
Cannabis - what are the effects?
euphoria
drowsiness
heightened images
altered tactile sensations
tachycardia
hypertension
ataxia
visual and auditory hallucinations
what causes gout (or hyperuricaemia):
bendroflumethiazide
loop diuretic
alcohol
salicylates
pyrazinamide
ethambutol
nicotinic acid
cytotoxic drugs
what abx causes tendon rupture
ciprofloxacin
which ulcerative colitis drug cannot be used for patients who has anaphylaxis to aspirin?
sulfasalazine
(has structural similarities to salicylic acid)
side effect of benzodiazepine
drowsiness
reduced muscle tone and reflexes
hypoventilation
hypotension
coma
confusion
toxic psychosis
convulsions
Side effect of these epileptic drugs:
- levetiracetam
- sodium valproate
- phenytoin
- carbamazepine
- lamotrigine
- Levetiracetam: abdominal pains, nausea, diarrhoea, anxiety, weight changes, aggression, tremor, anorexia,
- SV: hair loss, aggression, tremor, abdo pain, pancreatitis, jaundice, anorexia? weight gain? thrombocytopenia
- P: tremor, gingival hypertrophy, acne, hirsuitism, coarse facial features, peripheral neuropathy, stevens-johnson syndrome, aplastic anaemia, megaloblastic anaemia
- C: aggression, dry mouth, hyponatraemia, aplastic anaemia, thrombocytopenia, leukopenia, haemolytic anaemia, eosinophilia, gynaecomastia, male infertility, hepatitis, restlessness
- Lamotrigine: aggression, tremor, skin rash, hypersensitivity, blurred vision, dizzyness, sleep disturbance, joint pains
which CYP450 system is involved with the metabolism of:
- atorvastatin, simvastatin
- clopidogrel activation
- tamoxifen activation
CYP3A4 (don’t take with grapefruit, amlodipine - inhibitors)
CYPC19 (therefore, by taking omeprazole, this inhibit this process and reduces efficacy of clopidogrel)
CYP2D6 (therefore, taking SSRI - inhibitors - cause reduce plasma concentration and efficacy of tamoxifen)
these drugs affect the CYP450 system—how?
- sodium valproate
sodium valproate is an inhibitor of CYPC29.
blindness, pulmonary oedema, metabolic acidosis, shock, hypoglycaemia
? toxicity of what
& how to treat this
methanol
Tx: fomepizole or ethanol. haemodialysis.
side effect of digoxin
hyperkalaemia
mechanism of action of sumatriptan
used for migraine and cluster headache
structurally similar to 5-HT
it is a 5-HT agonist
activated at the cranial and basilar arteries - causes vasoconstriction
for cluster headache: reduce activity of trigeminal nerve
treatment of anticholinergic toxicity
physostigmine salicylate
DPP IV inhibitors
GLP-1 analogues
SGLT2 inhibitors
thiazolidinediones
give names of drugs
WHICH drug causes these side-effect?
- limb amputation
- vit b12 deficiency
- bladder cancer
DPP IV : -gliptins
GLP-1 analogues: - tides
SGLT2: -flozins (canglifozin cause lower limb amputation)
thiazolidinediones: pioglitazone (cause bladder cancer)
metformin cause b12 deficiency
Acute dystonia reactions - ?causes
metoclopramide
treatment of oculogyric crisis
procyclidine
what respiratory problem can you not use zanamivir for?
asthma as it can cause bronchospasm
which abx can cause photosensitivity?
doxycycline (ie risk of sunburn -> therefore particularly mentioned for those taking this for malarial prophylaxis)
what drug causes Reye disease in children?
aspirin
what drug causes gynaecomastia?
inhibit testosterone: spironolactone, finasteride/dutasteride, metronidazole, alkylating agents
anabolic steroids abuse
flutamine - blocks androgen receptors
others:
digoxin
amiodarone
isoniazid
cimetidine
methyldopa
TCA
diazepam
heroin
heroin
ketoconazole
goserelin
oestrogen in gender reassignment surgery or treatment of prostate cancer
CKD stages and stopping some drugs
Stage 3b: nitrofurantoin
Stage 4 : NSAIDs
examples of benzodiazepine and duration of action
diazepam - long half-life (up to 3 days in elderly)
temazepam, oxazepam - short half-life
drugs causing thrombocytopenia
quinine
abciximab
NSAIDs
diuretics: furosemide
antibiotics: penicillins, sulphonamides, rifampicin
anticonvulsants: carbamazepine, valproate
heparin
disulfiram causes nausea and vomiting when patient drinks alcohol.
what other drug will also cause the same effect?
metronidazole
which drug causes?
- glomerulonephritis
- interstitial nephritis
- acute tubular necrosis
GN: penicillamine, gold, captopril, phenytoin, penicillin, sulfonamides, rifampicin
IN: penicillin, cephalosporin, sulfonamides, thiazide, furosemide, NSAIDs, rifampicin
ATN: aminoglycosides, amphotericin, ciclosporin
which drug causes:
- optic neuritis
- corneal opacities
- cataracts
- retinopathy
ON: metronidazole, ethambutol, amiodarone
CO: indomethacin, amiodarone, hydroxychloroquine
Cataract: steroids
Retinopathy: chloroquine, quinine, hydrocychloroquine (causing bulls eye macula)
what drug causes gingival hyperplasia?
phenytoin
ciclosporin
nifedipine
why can we not give a patient monoamine oxidase inhibitor and SSRI together?
increase risk of serotonin syndrome
- triad of neuromuscular excitation, autonomic effects, altered mental status
what drug - when given with azathioprine causes myelosuppression (ie anaemia and leukipenia)?
ACEi
treatment of fungal nail
5% amorolfine nail lacquer 6 months (fingernail), 12 months (toenails)
terbinafine for 12 weeks (fingernails), 6 months (toenails)
treatment of head lice
dimeticone 4% lotion
wet combing with the BugBuster comb
Permethrin is NO longer recommended due to not effective tx and resistance
drugs causing erectile dysfunction
thiazide
beta-blockers
spironolactone
digoxin
finasteride (5 alpha reductase inhibitors)
bicalutamide (anti-androgens)
TCA
SSRI
Benzodiazepine
Phenytoin
Famotidine (H2 antagonist)
Opiates
ursodeoxycholic acid - mechanism of action
naturally occurring bile acid that is used dissolve cholesterol gall stones
drugs that causes oral ulcers
NSAIDs
azathiopine
methotrexate
penicillamine
gold
captopril, enalapril
losartan
nicorandil
fluoxetine
lithium
protease inhibitors
what does 1% of anaesthetic drug mean?
1ml in 10mg (ie 10mg/ml)
So if it is 2%, this means 1ml for 20mg.
which drug should NOT be used for primary open angle glaucoma?
beta-blocker
sympathomimetic
anti-muscarinic
carbonic anhydrase inhibitor
miotics
anti-muscarinic
which anti-HTN drugs worsen glycaemic control?
thiazide diuretic
(also beta-blockers)
which drugs can cause lichenoid eruptions?
ACEi
NSAIDs
methyldopa
chloroquine
oral anti-diabetic drugs
thiazide
gold
how to treat scalp ringworm?
PO griseofulvin
or TOP ketoconazole shampoo
what are the side effects of statins?
myositis/rhabdomyolysis
deranged liver function
interstitial lung disease
pancreatitis
NOT gallstones (but this is a side effect of fibrate)
causes of Horner syndrome?
central lesions: stroke/demyelinating disease
preganglionic lesions: pancoast tumour, mediastinal/thyroid mass, cervical ribs, neck trauma or surgery
postganglionic lesions: carotid artery dissection, cavernous sinus lesion, otitis media, head & neck trauma
Amantadine
NMDA antagonist - increase dopamine release and blocks dopamine reuptake
treat parkinson’s disease, post herpetic neuralgia and infleunza A
