Pharmacology Flashcards
mechanism of action on benzodiazepines
GABA A receptor agonist which potentiates effects of GABA nad increased frequency of Cl channel opening (activates Cl channels)
mechanism of action of melatonin
binds to MT1 receptors in suprachiasmic nucleus of anterior hypothalamus and regulates circadian rhythm
mechanism of action of methyphenidate
inhibits reuptake of dopamine and noradrenaline so increases level of dopamine and noradrenaline in basal ganglia
sodium dependent dopamine transporter inhibitor
side effects of methylphenidate
- reduced appetite
- sleep disturbance
- hypertension
mechanism of action of atomextine
noradrenergic effect via alpha and beta receptors
side effects of atomextine
hypertension
tachycardia
stroke, heart attacks
sudden death
mechanism of action of rituximab
targets CD20 surface molecule on B cells
mechanism of action of tociluzumab
acts by inhibiting IL-6 and prevents inflammation
mechanism of action of adalidumab
binds to TNF-alpha and neutralises its bioactivity and causes apoptosis of TNF expressing mononuclear cells
mechanism of action of IV immunoglobulin
blocks fragment crystallisable receptors and reduces haemolysis
mechanism of action of vigabatrin
inactivates GABA transaminase so inhibits GABA breakdown
side effects of vigabatrin
diplopia
reduced peripheral vision
optic neuritis
retinal atrophy
aggression
alopecia
mechanism of action of phenobarbital
binds to GABA -A receptors and prolongs chloride channel opening time and increases threshold for action potential and depressing central nervous system
mechanism of action of phenytoin
blocks voltage gated Na channels and reduces synpatic transmission
side effects of phenytoin
hair changes - excessive hair growth
nystagmus
teratogenic
gingivial hypertrophy
vit D deficiency
mechanism of action of sodium valproate
reduction of catabolism of GABA to increase availability of GABA.
blocks voltage gated Na channels and suppresses neuronal hyperexcaitability
side effects of sodium valproate
- teratogenic
- increased appetite and weight gain
- insulin resistance and metabolic syndrome
- easy bruising
- hair loss
- tremor
mechanism of action of retinoids
vitamin A derivative
features of fetal retinoid syndrome
small low set ears
stenosis of ear canals +/- deafness
microcephaly
celft lip and palate
transposition of great arteries, hypoplastic l heart syndrome
mechanism of action of lidocaine
prolongs inactivation of voltage gated sodium channels which prevents action potentials firing
mechanism of action of bisphosphonates
inhibits osteoclast actvity
mechanism of action of oxybutynin
muscarinic receptor antagonist for acetylcholine which causes relaxtion of bladder smooth muscle to increase capacity
mechanism of action of desmopressin
synthetic analogue of ADH - increases cellular permeability of collecting ducts and increases reabsorption of water
mechanism of action of adenosine
A1 adenosine receptor agonist which reduces conduction time in AV node by inhibiting calcium influx and promoting K efflux
1/2 life of adenosine
10 secs -> give large vein close to heart
mechanism of action of amiodarone
potassium channel blocker which prolongs action potential
side effects of amiodarone
pulmonary fibrosis
hypothyroidism
corneal deposits
photo sensitivity rash
mechanism of action of milrinone (phosphodiesterase 3 inhibitor)
+ve inotrope and vasodilator
competitive phosphodiesterase 3 inhibitor that inhibits degradation of camp and increase cAMP to increase myocardial contractility, promotes myocardial relaxation and reduced vascular tone in circulation
mechanism of action of atropine
blocks vagal impulses
mechanism of action of statins
inhibits HMG Co-a and reduces LDL cholesterol levels
mechanism of action of ezetimibe
inhibits dietary cholesterol absorption in intestine by blocking NPC1L1 at brush border
mechanism of action of trimethoprim
dihydrofolate reductase inhibitor so blocks DNA synthesis
/ inhibition of tetrahydrofolic acid synthesis
side effect: rise of creatinine
side effects of rifampicin
orange bodily fluids
liver dysfunction
potent enzyme inducer (effects INR)
side effects of isoniazid
peripheral neuropathy (vit B6 deficiency)
deranged liver function
agranulocytosis
cutaneous adverse reactions
seizures (if in newborn)
side effects of ethambutol
visual disturbances
ocular toxicty
treatment of TB meningitis
12 months rifampicin and isoniazid
2 months pyrazinamide and ethambutol
initial steroids
mechanism of action of fusidic acid
inhibit protein synthesis (bacteriostatic effect)
mechanism of action of aminoglycoside
eg. gentamicin, amikacin
inhibit protein/ bacterial synthesis (binds to 30S ribosome)
side effects of gentamicin
vestibulo toxicity -> hearing loss
nephrotoxicity
how is heparin monitored
anti Xa levels
antidote of unfractioned heparin
protamine
mechanism of action of ibuprofen
reduces prostaglandin synthesis through non selective inhibition of COX 1 and 2
mechanism of action of osmotic diuretic e.g. mannitol
osmosis in the proximal renal tubule.
does not cross blood brain barrier - increases intravascular volume and promotes fluid shift from brain to blood to prevent cerebral oedema
mechanism of action of potassium sparing diuretics e.g. spironolactone
block action of aldosterone at collecting duct leading to loss of Na and water excretion (retain K and H ions)
mechanism of action of loop diuretics e.g. furosemide, bumetanide
inhibit Na-K-Cl co transporter in thick ascending limp of loop of henle causing loss of Na, K, Cl and water in the urine
side effect of furosemide
metabolic alkalosis
dizziness
headache
hypokalaemia
hyponatraemia
hypocalcaemia
mechanism of action of thiazide diuretics e.g. bendroflumethiazide
acts at proximal part of distal convulated tubule
mechanism of action of prostaglandin E1
acts on E4 receptors on smooth muscle of ductus coupled to Gs GPCR and causes smooth muscle relaxation and patent ductus arteriosus
side effects of prostaglandin E1
apnoea
resp depression
tissue oedema
fever
seizures
side effects of calcium channel blockers
gym hypertrophy (nifedipine)
constipation
bradycardia
hypotension
AV blocker
vertigo
side effects of corticosteroids
1st week - insomnia *, psychosis
prolonged - diabetes, immunosuppression, pathological fractures (osteoporosis)
striae
acne
hypertension
glaucoa
reduction in growth velocity
mechanism of action of low dose of adrenaline
acts at beta 1 adrenoreceptors in myocardium (in the heart) to increase contractility and reduced systemic vascular resistance
mechanism of action of high doses of adrenaline
acts at alpha 1 ** and 2 adrenoreceptors on peripheral vasculature (in veins + arterioles) to cause vasoconstriction to increase systemic vascular resistance (IN ANAPHYLAXIS)
mechanism of action of ipratropium
anti muscarinic bronchodilator and cholingeric receptor blocker
side effects of ipratropium
myodriasis
flushing of skin
hyperthermia
dry skin
agitation
mechanism of action of salbutamol
beta 2 adrenergic receptor agonist
activates adenyl cyclase to form cAMP and relaxes smooth muscle
mechanism of action of montelukast
leukotriene receptor antagonist which reduces bronchoconstriction and inflammation in asthma
indicated , 5 y/o when unable to use iCS
mechanism of action of aminophylline
phosphodiesterase inhibitor (type 3) to relax smooth muscle
mechanism of action of penicillin
inhibit bacterial cell wall synthesis
mechanism of action of quinolones e.g. ciprofloxacin
inhibit DNA gyrase
side effects of vancomycin
red man syndrome (GIVE SLOWLY IV)
ototoxicity - auditoray portion of VIII cranial nerve
nephrotoxicity - interstitial nephritis short term
mechanism of action of dornase alpha
endonucleatic cleavage of extracellular DNA and reduces sputum viscosity (used in CF)
mechanism of action of WARFARIN
vitamin K antagonist and reduces factors 2, 7, 9 , 10 and protein C and S
mechanism of action of ondansetron
selective 5-HT3 (serotonin) receptor antagonist
mechanism of action of ursodeoxycolic acid
reduces hepatocellular apoptosis
mechanism of flecainide
block Na channel so reduces rate of depolarisation of phase 0 without changing length of duration of action potential
mechanism of action of indomethacin
inhibit prostaglandin E2 synthesis
prostaglandin E2 relaxes smooth muscle and inhibits closure of patent ductus arteriosus
NSAID
mechanism of clindamycin
inhibit protein synthesis (at 50S subunit)
side effects of atypical anti psychotics e.g. risperidone, olazapine
hyperprolactinaemai e.g. enlarged breast, secondary amenorrhoea, reduced libido (risperidone ***)
extrapyramidal symptoms - tremor, parkinson like symptoms, tradive dyskinsea
mechanism of action of risperidone
inhibit dopamine D2 receptors in mesolimbic pathway
D2, 5-HT, alpha 1 and histamine antagonist
mechanism of action of serotonin
5HT-1D (serotonin) receptor agonist resulting in vasoconstriction of cranial blood vessels
mechanism of action of isoniazid
inhibit mycolic acid synthesis
selective for mycobacteria
Severe side effect of metoclopramide
dystonic reaction!
can occur in 25% in first 24 hours
torsion of neck, fixed glaze
treat with IV procyclidine
treatment of malignant hyperthermia
IV dantrolene
presentation of malignant hyperthermia
rigidity, fever, tachycardia
mechanism of action of LMWH
acclerates anti thrombin dependent inactivation of factor Xa
CAUSES REDUCED THROMBIN PRODUCTION AND LESS FIBRINOGEN CONVERTED TO FIBRIN AND FEWER CLOTS
mechanism of action of acetazalomide
carbonic anyhydrase inhibitor
Increases secretion of bicarbonate, Na, K, water from kidneys - therefore at risk of metabolic acidosis
potency of steroids
mild = hydrocortisone
moderate = eumovate, trimovate
potent = betnovate
very potent = dermovate
side effects of tetracyclines e.g. doxycycline
yellow discolouration of teeth
not licensed <12 y/o and during breatsfeeding
dental hypoplasia
side effect of vincristine
inhibits microtubule activity
motor and sensory neuropathies
ataxia
LOSS OF ANKLE JERKS
side effects of SSRIs
GI bleeding
GI upset
headache
dry mouth, excessive sweating
loss of libido
insomnia
mechanism of action of topiramate
modulates voltage gated sodium channels
potentiates GABA inhibition
blocks glutamate neurotransmision
side effect of topriamate (epilepsy)
nephrolithiasis
side effects of ciclosporin
chronic interstitial nephritis
excessive growth and thickness of hair
gum hypertrophy
mechanism of action of infliximab
inactivates TNF alpha with high affinity
IgG monoclonal antibody
mechanism of action of sulfasalazine
inhibit leukotrienes
presentation of paracetamol overdose
nausea and vomiting, anorexia, liver enlarged and tender -> acute liver failure, lactic acidosis, hypoglycaemia
management of paracetamol overdose
N-acetylcysteine - replaces gluthione stores , 21 hour regime
(activated charcoal if within 1 hour of ingestion)
presentation of benzodiazepine overdose
ataxia, slurred speech, nystagmus, blurred vision, sedation, hallucinations
treatment of benzodiazepine overdose
flumzenil - benzodiazepine receptor site antagonist
presentation of opiate overdose
hypoventilation, hypotension, mioism, sedation, bradycardia
treatment of opiate overdose
naloxone - competitive antagonist of opioid receptor
presentation of lead poisoning
abdo pain, vomiting, constipation, headache, irritable, encephalopathy, hypertension, fanconi syndorme, nephritis
investigations for lead poisoning
- blood lead levels
- FBC
- peripheral smear - basophilic stripping of RBC
management of lead poisoning
chelation, DMSA, penicillamine
presentation of salicylate (aspirin) overdose
- nausea and vomiting
- tinnitus
- deafness
- dehydration, sweating
- restless
- pulmonary oedema
- confusion, seizures
blood gas of salicylate overdose
initially = resp alkalosis
progresses = metabolic acidosis
investigations for salicylate overdose
plasma salicylate levels:
2 hours if symptomatic
4 hours if asymptomatic
management of salicylate overdose
activated charcoal if < 1 hour
gastric lavage
dialysis
presentation of CO poisoning
headache, dyspnoea, coma, convulsions, death
management of CO poisoning
100% oxygen
management of anti freeze poisoning
fomepizole - inhibitor of alcohol dehydrogenase
management of beta blocker overdose
- atropine
- IV glucagon (stimulate cAMP)
mechanism of cylizine
H1 histamine antagonist whichg acts at H1 receptors in chemoreceptor trigger zone in vestibular nucleus - acts at medulla oblongata
side effect of cyclizine
urinary retention, sedation
conversion of oral/ s/c morphine
3mg oral morphine = 1.5 mg s/c or iV morphine morphine = 1mg diamorphine
mechanism of action of carbamazepine
binds to voltage gated Na channels and extends inactivated phase to prevent rapid action potentials
mechanism of action of lamotrigine
acts at voltage gated N channels to inactivate them
side effects of lamotrigine
rash -> stevens johnson syndrome
ATAXIA
mechanism of action of ethosuximide
calcium channel blocker -> reduces calcium channel (T type) currents in thalamic neurones
side effect of ethosuximide
nausea, vomiting
sleep disturance
drowsiness
hyperactivity
distinctive taste - poor compliance
presentation of myasthenia gravis
fatiguable weakness - proximal , upper limb, worse throughout the day
eye lid weakness (ptosis)
reduced facial expression
speech and swallowing problems
diagnosis of myasthenia gravis
- EMG conduction studies
- antibody testing
- improvement with anticholineresterase edriohonism
mechanism of action of ACE-I
prevent conversion of angiotensin 1 to angiotensin 2 so they reduce aldosterone secretion
reduces preload and afterload in HF by decreasing vascular resistance
mechanism of action of beta blockers
increase stroke volume and decrease contractility of heart
mechanism of action of digoxin
cardiac glycoside inhibits Na/K ATPase that increases intracellular Na and secondary increase in intracellular Ca increasing force of contraction
mechansim of action of dopamine
catecholaemine that stimulates beta 1, alpha 1 and dopaminergic receptors
mechanism of action of dobutamine
sympathomimetic :
1. beta 1 stimulation (stronger than alpha) - increases contractility
2. beta 2 stimulation - systemic vasodilation
mechanism of action of metformin
decreases gluconeogenesis and increases peripheral utilisation of glucose
Side effects of cyclophosphamide
causes cell apoptosis
haemorrhagic cystitis
side effects of doxorubicin
inhibits topiosomerase §
dilated cardiomyopathy
5 drugs used in hodgkins lymphoma
rituximab
cyclophosphamide
doxorubicin
vincristine
prednisolon
medications prolonging QT interval
clarithromycin
fluoeoquinolones
anti malarials
ketonazole
mechanism of action of blinatumomab
used in B cell leukaemia
targets CD19 antigens on B lymphocytes
dose of adrenaline in anaphylaxis
1 IN 1000 IM adrenaline
< 6 MONTHS - 0.15ml
6m-6 y/o - 0.3ml
> 6 y/o - 0.5ml
which drugs cause steven johnsons rash
carbamazepine
phenytoin
lamotrigine
phenobarbital
mechansim of clarithromycin (macrolide)
bind to 50s subunit to inhibit bacterial synthesis
mechanism of action of cyclopentolate
muscarinic acetylcholine M1 receptor antagonist
causes dilatation of the eye and prevents accommodation for eye exams e.g. ROP exams
mechanism of action of pilocarpine
binds to M1, M2 and M3 muscarinic acetylcholine receptors
constricts pupils and used in management of raised intra-ocular pressure and to induce myosis
mechanism of action of allopurinol
xanthine oxidase inhibior directly and through its active metabolite
mechanism of topical atropine
binds and inhibits muscarinic (M1-M5) acetylcholine receptors to block the action of pupillary sphincter muscle and cause pupil dilatation
side effects of topical atropine
flushing
dilated pupils
blurred vision
dry mouth
tachycardia
(autonomic symptoms)
mechanism of prednisolone
inhibits migration of neutrophils (polymorphonuclear leukocytes)
mechanism of action of hyoscine butylbromide
blocks muscarinic receptors in smooth muscle GI tract (anticholinergic)
mechanism of fexofenadine
H1 antagonist
mechanism of action of amlodipine
inhibition of calcium ion influx at L type calcium channels causing peripheral vascular resistance to decrease
mechanism of action of ranitidine
H2 receptor blocker
mechanism of action of propanolol
beta 1 (cardiac myocytes) and 2 (peripheral blood vessels) receptor antagonist
mechanism of rocuronium
competitive acetylcholine receptor antagonist
used to cause muscle paralysis
mechanism of action of vancomycin
inhibit synthesis of bacterial cell wall (treats MRSA)
Mechanism of action of mycophenolate
inhibit synthesis and proliferation of DNA
mechanism of action of chloramphenicol
inhibit 50s subunit of ribosome
treat typhoid, otitis externa and bacterial conjunctivitus
mechanism of action of levetiracetam
modulates synaptic vesicle protein 2a
mechanism of action of domperidone
dopamine receptor antagonist
SE= dry mouth, constipation
mechanism of action fo sildenafil
phospodiesterase V inhibitor to cause vasodilation
mechanism of caffeine in neonates
blocks adenosine receptors and causing increase sensisitivity to CO2
side effect of gangliciclovir
leukopenia, anaemia, thromboctypenia
monitor FBC
topical atropine side effects
flushing
dilated pupils
blurred vision
tachycardia
dry mouth
TCA overdose
dilated pupils
tachycardia
dry skin
hot
confusion
opiate toxicity symptoms
constricted pupils
bradycardia
drowsy
coma
seizures
resp depression
urinary retention
indomethacin side effects
agranulocytosis
arrhythmias
fludi retention
hypotension
amphotericin side effects
anaemia
diarrhoea
hepatic and electrolyte abnormalities
sildenafil side effects
haemorrhage
vasodilation
arrhythmias
GORD
mechanism of action of azathioprine
inhibition of purine nucleotide synthesis
management of iron overload
desferroxamine iV
describe serotonin syndrome
sweaty
dilated pupils
increased tone
increased reflexes
agitated
mechanism of oseltamivir
neurominadase inhibitor
hydrolyses sialic acid residues on host cells to release newly formed virions
mechanism of botulinum toxin
acts at presynaptic cholinergic nerve terminals and inhibits release of acetylcholine
examples of gram -ve rods
e.coli
pseudomonas
burkholderia
examples of gram +ve rods
c.diff
listeria
mechanism of sulphorylureas e.g. gliclazide
act at ATP sensitive K channel in beta cells -> increases channel closing so insulin is released