PHARMACOLOGY Flashcards
what medications can increase methadone effect
fluconazole, voriconazole, ketoconazole
ciprofloxacin
clarithromycin
cimetidine
fluvoxamine
mu-opioid receptor agonist. Metabolised by CYP450 (CYP3A4)
what drug used to treat alcohol withdrawal
chlordiazepoxide, lorazapam, diazapam (benzodiazapine)
what drugs are CI in alcohol withdrawal treatment (due to lowering seizure threshold)
antipsychotics (chlorpromazine, haloperidol)
methadone has a ________ half life
long
supress withdrawal and cravings
first line medications to treat alcohol abstinence
naltrexone - blocks mu-opioid receptor -> inhibits reward and reduce cravings
acamprosate - moderates glutamate neurotransmission at NMDA receptor
disulfram - aldehyde dehydrogenase inhibitor (second line)
rebound tremor, anxiety, insomnia, SNS hyperactivity (diaphoresis, palpitations) is seen in wthdrawal of ….
benzodiazapines i.e. lorazapam
can also result in psychosis, seizures, death
increased risk with shorter acting agents - alprazolam
hyperphagia, hypersomnia, intense psychomotor retardation, severe depression (crash), vivid dreams - is seen in withdrawal of …..
(stimulants) amphetamines, cocaine
manage suicidal ideation
phencyclidine is a
NMDA receptor antagonist
exact MOA unknown -
predicted NMDA hypofunction causes dopamine dysregulation -> psychosis
what to prescribe patients with acute pain and worreid about opioid addiction
short course of opioid based pain meds fo rbreakthrough pain only (most will see improvement 3-5 days)
IFN is used to treat
RNA and DNA viruses
i.e. kaposi sarcoma, HBV
(interferon = ‘interferes’ with replication in host cell)
Downregulates protein synthesis. upregulates MHC.
anticholinesterases
‘stigmine’
physostigmine
neostigmine
pyridostigmine
donepezil, rivastigmine, galantamine
(indirect agonists of Ach)
prevent (anti) breakdown (ases) of Ach (choline)
antidote to anticholinergic toxicity
physostigmine
‘phyxes’ atropine overdose
anticholinergic (anti Ach) -> physostigmine (increases Ach) by inhibiting anticholinesterases (prevents Ach breakdown)
anticholinesterase poisoning antidote
atropine - competitive inhibitor (muscarinic anatgonist)
pralidoxime - regenerates AchE
alpha-2 agonists
clonidine, guanfacine
a-methyldopa
tizanidine
hypertensive emergency, ADHD
mypertension in pregnancy
spasticity
drugs affecting microtubules
mebendazole (helminth)
griseofulvin (fungal)
colchicine (gout)
vinca alkaloids (cancer)
taxanes (cancer)
kinesin and dynein transport cellular cargo along icrotubules
what effect does vitamin K have on clotting factors
y-carboxylation of glutamic residues
post-translational modification
y-carboxylation essential for clotting factor maturation 1972, S, C
epoxide reducase in liver regenerates active vit K for ‘gamma carboxylation’
meningitis in elderly is treated with
vancomycin (G+)
cephtriazone (G-)
ampicillin (coveres listeria)
listeria monocytogenes treated with
ampicillin
penicillinase sensitive penacillin
Treatment of brucellosis
tetracyclines
rifampin
treatment AML
all-trans retinoic acid (vit A)
treatment CML
Imatinib
tyrosine kinase inhibitor -> (stops t9;22) translocation
treatment ALL
cytarabine
pyrimidine analog - nucleoside analog (mimics cytasine) - inhibits DNA s
treatment CLL
comfort,
rituximab (CD20)
fludarabine, clyclophosphamide, chlorambucil, alemtuzamab
rituximab - monoclonal Ab, associated with an increased risk of PML, a demyelinating disease of the CNS caused by the destruction of oligodendrocytes secondary to reactivation of JC virus.
increased risk of PML
JC virus reactivation
rituximab
natalizumab
treatment of DLBCL
R-CHOP
Riuximab (CD20+) -
Cyclophosphamide
Hydroxydaunorubicin (adriamycin)
Oncovin® (vincristine)
Prednisone
rituximab added for B cell
treats non-Hodgkin lymphomas
what is a concerning feature of neoplastic process in lymph nodes
lymphocytes with a single immunoglobulin variable domain allele - (monoclonal)
single cell dividing uncontrollably, produces identical copies of itself
polyclonal - normal response to infection, many B cells mlutify, producing slightly different antibodies
purine analog that mimics adenosine
cladribine
unable to be processed by ADA
treats hairy cell leukaemia
inhibits nucleotide metabolism.
inferes with DNA synthesis
cell cycle non-specific*
‘I’m ‘clad’ you’re ‘hairy’
what drug is resistant to breakdown by adenosine deaminase
cladribine
hairy cell leukaemia
hydroxyurea is used to treat
sickle cell anaemia
polycythemia vera
causes aplastic anaemia
still used to treat bacterial meningitis in resource-poor countries
chloramphenicol
H. influenzae
N. meningiditis
S. pneumoniae
also causes ‘grey baby syndrome’
blood in urine, but no RBC in urinalysis
haemoglobinuria
myoglobinuria
i.e. PNH
true hematuria - blood and RBC in urine
monobactams used to treat
aerobic gram negative rods
enterobacter …
NRTI’s lack a ? group
3’ hydroxyl
terminates chain
HIV reverse transcriptase normally adds nucleotides to the growing DNA strand via a 3’-5’ phosphodiester bond
Since NRTIs resemble natural nucleosides but lack the 3’-OH, they act as chain terminators,
name two first line cephalosporins
cefazolin
cefalexin
‘azolin’ ‘lexin’
‘a stolen lexus’
β-lactam drugs, bactericidal
inhibit cell wall synthesis
less susceptible to penicillinases
Tx gram (+) PEcK
Proteus mirabilis
E coli
Klebsiella pneumoniae
**MOA: **
reversible binding 50S
interrupt peptidyl transferase
**Tx: **
gram (+) and (-)
rocky spotted mountain fever
meningitis
chloramphenicol
aplastic anaemia
gray baby syndrome
treats gram (+) skin infections
can cause myopathy
can treat MRSA
daptomycin
dapt-myo-skin
CONTRAINDICATED in pneumonia (deactivated by surfactant)
tamoxifen can cause
endometrial polyps
endometrial cancer
partial agonists: pro-oestrogen effects on endometrium, bone
anti-oestrogen effects on breast
DES - diethylsetilbestrol can cause
adenosis
persistance of columnar epithelium in vaginal canal
can lead to clear cell adenocarcinoma
what drug decreases vaso-occlusive crises by increasing HbF
hydroxyurea
sickle cell
adverse and serious adverse effects of carbamazepine
CARBAMAZEPINE
C - CNS - vomiting, D’s (dizziness, diplopia, diarrhoea)
A - aplastic anaemia, agranulocytosis
R - rash (face to trunk) - SJS, DRESS
B - blood - pancytopenias
A - ADH - SIADH
M - megaloblastic (rare)
A - autoinduction (induces own CYP450)
Z - sedative zzzz
E - enzyme inducer - CYP450
P - pregnancy (teratogenic), periheral neuropathy
I - increased liver enzymes (hepatotoxicity)
N - nutrition -* folate depletion*, nytagmus
E - oedema
MOA of flutamide
impairs androgen-receptor interaction
non-steroid agent
competitive testosterone receptor inhibitor
used in combo with GnRH agonists to treat prostate cancer
first line pharmacotherapy for primary hyperaldosteronism
spironolactone
eplerenone
mineralocorticoid receptor antagonist
eplerenone (less gynacomastica, decreased libido)
BPH (leading to bladder outlet obstruction) can cause increased pressure presenting as
histology
hydronephrosis
renal parenchymal atrophy
scarring
can progress to CKD
(RCC)
what are the risk factors
smoking, obesity, HTN
round polygonal clear cells
toxin exposure - heavy metals
seen in
hematuria
renal mass
LBP weight loss
lytic bone lesion vertebrae
smokes drinks
renal cell carcinoma
(rounded polygonal clear cells)
bilateral pitting oedema
no abdomen distension
tortuous veins lower abdomen
left flank mass
smoker
renal cell carcinoma
invasion of IVC
RCC tends to invade renal vein -> by extension will invade IVC
key features :
bilateral oedema LL
abdominal walls collaterals
Drug reaction with eosinophilia and
systemic symptoms
DRESS
what can occur if chronic glucocorticoid use is stopped abruptly
adrenal insufficiency
ivermectin
Tx parasites
disrupt microtubles and cellular motility
what is used to prevent vasospasm in subarachnoid haemorrhage
nimodepine
short acting CCB t1/2 <2hrs
adverse effects of bisphosphonates
oesophagitis
osteonecrosis jaw
atypical femoral stress fractures
Use of leucovorin (with methotrexate)
rescues normal cells from methotrexate toxicity bypasses dihydrofolate reductase (methotrexate acts on)
replenishes reduced folate levels
works like folate to reduce myelosuppression
essential if pt has **renal dysfunction **ie.e high creatinine - toxicity, reduced clearace
giving folate wont suffice - methotrexate will complete with it
must give to pts taking 5FU - increases binding of 5FU wth its target - thymidylate synthase
proteasome inhibitors treat
anticancer
**multiple myeloma
mantle cells lymphoma
accumulation of proteins -
**apoptosi
arrest cell cyle at G2-M phase via
degrade unfolded and misfoded proteins
bortezomib
ixazomib
carfilzomib
‘zom’
proteasome needed to clear misfolded/unfolded proteins
not cleared i.e. multiple myeloma (plasma cells produce alot of proteins - Igs)
if proteasome inhibitor inhibits this clearance of proteins
-> apoptosis results
(from response of unfolded protein)
treatment of multiple myeloma
bortezomib
(proteasome inhibitor)
arrests G2-M
protein accumulation
apoptosis
proteasome needed to clear misfolded/unfolded proteins
not cleared i.e. multiple myeloma (plasma cells produce alot of proteins - Igs)
if proteasome inhibitor inhibits this clearance of proteins
-> apoptosis results
(from response of unfolded protein)
treatment of babesiosis (borrelia microti)
atovaquone +
azithromycin
ring forms or tetrad on giemsa stain
atovaquone - inhibits mitochondrial electron transport
azithromycin - binds 50S, inhibits protein synthesis
drug treating muscle cramps
stimulates
Y-aminobutyric acid B receptor
Baclofen
(stimulates _GABA _ receptor)
agonist at GABA-B receptor
Tx muscle spasticity i.e. paraplegic
also cause sedation
increase K+ efflux
hyperpolarise sk ms
decrease action potential frequency
hypertonic saline must be given slowly and carefully due to risk of
central pontine myelinosis
MOA of neomycin in hepatic encephalopathy
kills bacteria in the gut tht generate ammonia
treats hepatic encephalopathy
NO LONGER USED - AKI, ototoxicity
aminoglycoside AB (inhibits 30S) - prevent translation
killing gram negative flora reduces ammonia
cannot kill anaerobes (as require O2 for uptake)
**Rifaximin now drug of choice
what antibiotic is used to treat hyperammonia
rifamixin
neomycin no longer used
atherosclerosis
abdominal pain after eating
weight loss
PAD
CAD
diminished pedal pulses
celiac or mesentierc ischaemia
reduced blood flow to small intestine
acute or chronic
acute = embolic or thrombotic arterial obstruction
chronic = atherosclerotic stenosis (SMA common)
common asssoc findings:
atherosclerotic sequalae - PAD, CAD, pedal pulses
Samters triad caused by aspirin
aspirin sensitivity
nasal polypopsis
asthma
urticara (hives)
NSAIDS –> inhibit co1 –> decrease PGE2 –> promote 5-lipoxygenase –> increase leukotriene 4 –> increased inflammation
in asthma leukotrienes key mediator of inflammation
protease inhibitors function
block formation of mature viral core
in HIV replication
prevents maturation
treatment of Kawasaki disease
high dose aspirin
IV immunoglobulins
normally aspirin CI in children - Reyes syndrome
acute treatment of gout (3)
NSAIDS (indomethacin)
glucocortoids
colchicine
MOA of colchicine
inhibit **microtubule polymerisation **–>
decrease **leukocyte motility **and infiltration into joint
tx gout
stabilises tubulin - inhibits microtuble polymerisation
treatment of chronic gout (2)
allopurinol
febuxostat
xanthine oxidase inhibitors
type of crystals in gout
needle shaped
negative bifringent
yellow under parallel
blue under perpendicular
polarised light:
calcium pyrphosphate deposition disease (pseudogout)
pseudogout
rhomboid crystals
weakly positive bifringent
blue under parallel light
rhomboid crystals
weakly positive bifringent
seen in
calcium pyrphosphate deposition disease
(pseudogout)
blue under parallel light
MOA of probenecid
inhibits PCT reabsorbing uric acid
gout Tx
MOA of pegloticase
increased uric acid solubility in serum/synovial fluid
recombinant form of urate-oxidase enzyme –> converts uric acid to water soluble metabolite (allantoin)
inhibits alcohol dehydrogenase
fomepizole
Tx of methanol poisoning
**first step **of metabolism
prevents conversion methanol to toxic metabolites
inhibits aldehyde dehydrogenase
disulfiram
not used acute management methanol toxicity
name anti-folate medications (4)
phenytoin
methotrexate
trimethoprim
dapsone
mifepristone MOA & use
competitive inhibitor progesterone
dilation of cervix
elective abortion
primes for misoprostol
misoprostol MOA & use
synthetic prostaglandin
uterine contractions
follows mifepristone
main resistance of E coli to B-lactam AB
(i.e. ampicillin)
B-lactamase production
penicillinases
main resistance to B-lactam ABs:
**gram negative **= B-lactamase production
**gram positive **= altered structure transpeptidases PBPs
(B-lactam AB can’d bind)
main resistance of S pneumoniae to B-lactamase AB
(i.e. ampicillin)
altered structure transpeptidases PBPs
main resistance to B-lactam ABs:
**gram negative **= B-lactamase production
**gram positive **= altered structure transpeptidases PBPs
(B-lactam AB can’d bind)
klebsiella, pseudomonas, serratia demonstrate B-lactam resistance by mutations in
genes coding for porins
___ are used by bacteria to decrease intracellular concentrations of AB
(i.e. tetracycline - intracellular working AB)
Efflux pumps
used by E coli
cyanide inhibits enzyme
cytochrome C oxidase
leads to lacrtic acidosis
Inhibits ETC)
tachypnoea
hypotension
confusion, lethagy
bradycardia
metabolic acidosis
toxin
cyanide poisoning
metabolic acidosis from lactic acidosis caused by cytochrom c inhibition - uncoupling electron tranport chain (ETC)
byproduct of sodium pitroprusside
cyanide
tx of malignant HTN
drugs causing radiation pneumonitis
doxorubicin
bleomycin
treatment for anorexia nervosa
olanzapine
treatment for bulimia nervosa
fluoxetine
bupeopion CI - increased seizure risk
treatment of angina
nitroglycerin
vasodilation veins > arteries
decrease Preload
CCB in prinzmetal angina - decrease coronary vasospasm
treatments of myocardial infarction
aspirin / heparin
nitrates
BB
ACEi
supplemental O2
fibrinolysis / angioplasty (opens blocked vessel)
2 adverse risks of fibrinolysis or angioplasty in MI
contraction band necrosis
reperfusion injury
CBN: calcium influx –> hypercontraction myofibrils
RI: oxygen –> free radicals –> myocyte damage
cabergoline and bromocriptine are
dopamine agonists
Tx prolactinomas (reduce tumour size)
omeprazole MOA
direct & irreversible inhibition of luminal H+/K+ ATPase on gastric parietal cells
= proton pump inhibitors ‘prazole’ drugs
treatment GERD
increased risk C diff infection
cimetidine is a potent inhibitor of
CYP450
also has:
antiandrogenic effects
cross BBB, placenta
H2 blocker -> decresed recretion parietal cells
what family impairs DNA synthesis by direct inhibition of DNA gyrase
fluroquinolones
(topioisomerase II in prokaryotes)
Tx legionella pneumophillia - atypical pneumonia
long acting opioid known for
prolonging QT interval
methadone
aripiprazole MOA
**partial agonist **D2
atypical antipsychotic (second gen)
less attenuation dopamine in BG
less likely to lead to drug induced parkinsonian symptoms
(locking limbic system - decreases psychotic symptoms)
what is the function of cilostazol
tx claudication
(peripheral arterial disease)
PDE3 inhibitor (phosphodiesterase III)
decreases CAMP degradation -in platelets / vascular smooth muscle –> increased intracellular CAMP –> increased PKA –> inhibition platelet aggregation
vascular sm - **increased vasodiltion **(inhibition MLCK)
