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pharmacology 1

Terms

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hemicholinium
choline reuptake
botulism toxine
release
M3 smooth ms of GIT
I contractility ^ motility
M3 lung
bronchospasm ^ secretion
m2 heart
decrease SAN , AVN decrease HR ^ CODUCTION
M3 ON gland
^ secretion
m3 on urinary bladder
^ contractility relaxation to sphinctor
m3 on endothelium
dilatation by NO deriving relation factor
desentisized quickly\nn or muscarinic or adrenergic receptor
nicotinic receptor
m1 receptor work on which G protein
Gq which stimulate phosholipase c which release IP3 Ca DAG
m2 receptor work on which gene?
Gi which inhibit adenyl cyclsae
m3 receptor work on which genes?
Gq which stim phospholipase c which release IP3 Ca DAG
B1 WORK on wich gene?
Gs which stimulate adenyl cyclase
alpha1 receptor work on which gene?
Gq
alpha2 receptor mechanism?
Gi
B2 receptor mech?
Gi
d1 and d2 receptor mech?
Gs
D1 receptor where it work?
renal and mesenteric vascular
pilocarpine
muscarinic agonist for glucoma and xerostomia
methacholine
muscarinic agonist
bethacholine
muscarinic agoinst
edrophonium
short acting reversible acetyl choline inhibitor use for1- dx myasthenia 2-cholinergic crisis
physostigmeine
ach cholinesterase inh use for Rt glucoma 2- in atropine overdose (lipid soluble)
neostigmeine
use in urinary retension myasthenia ileus (no cross BBB)
pyridosigmine
U retension , ileus myasthenia
donepezil
ach cholinesterase inhibitor used in alzehimers
malathion
like parathione is irreversible organophoshates drug act as ach cholinesterase inh
tacrine
ach cholinesterase inh use in alzehimers
echothiophate
like methation and parathion but used in glucoma
Rx of organophoshorous poison
atropine pralidoxime 2 PAM( work on skeletal muscle) as early as possible
manifestation of chronic organophosphate
peripheral neuropathy and demylination
pt leave several hours wiyhout Rx against organophoshorouse what will happen?
desenthesization and lead to Ms paralysis
atropine
muscarinic antagonist
tricyclic antidepression overdose
3c cardiotxicity convulsion coma
atropine overdose Rx
sympthomatic + physostigmine
name 3 other muscarinic antagonist
antihistamine tricyclic antidepression amantidine quinidine
atropine use 4
antispasmodic antidiarhea antisecritory op poisoning
tropicamide
topical eye in ophthalmology exam
ipratropium promide
is muscarinc receptor blocker use in asthma COPD
scoplamine
muscarinic receptor block use in motion sickness
trihexyphenidyl
muscarinic blocker antiparkinson and in acute extraparkinson induced by drug
hexamethonium
ganglion block
mecamylamine
ganglion block use in sever hypertension
phenylephirine
alph1 agoinist used as nasal decongestion and ophthalmology exa(syst side effect)
methoxamine
alpha1 agonists used in Rx of paraxysmal atrial tachycardia
clonidine
alpha2 agonist used in Rx of mild to mod HPT
methyldopa
as clonidine alpha2 agonist used in RX of HPT
salmeterol (family and used)
B2 agonist used in RX of asthma.
isoproterenol (family and used)
non selective B agonist used in asthma heart block bradyarrhythemias
dobutamine
B1>B2 agonist used in Rx of acute congestive heart faliure
ritodrine
B2 agonist used in Rx of premature labor
terbutaline
B2 agonist used in Rx of asthma
who s adrenergic group icrease in pulse pressure
B agonist , epinephrine(low and medium dose )
name 2 releaser of norepinephrine
tyramine amphetamine ephidrene(cold medication)
if pts on MAO inhibitor what things should avoid and why?
red wine ,cheese , sausage ,avocado ,dried fish(tyramine containing) amphetamine cold medication like...................................ephedrine
name drugs work on NE reuptake
cocain , tricyclic antidepresion
phentolamine
compatitive inhibitor non selective alpha antagonist
phenoxybenzamine
non compatitive non selective alpha antagonist
use of phentolamine
Rx of HPN pheochromocytoms BPH
prazosin
like terazosin/doxazosin\alpha 1 antagonist
yohimbine
alpha 2 blocker used in RX of postural HPT, impotence
mirtazapine
alpha 2 blocker used as antidepression
name 3 contraindication for use B blocker
ASTHMA vasospasm DM
why prefer b blocker in Rx of HPN than alph blocker?
1_ no reflex tachycardia with b blocker. 2_no reflex increase in renine secretion.
which B blocker has no hyperlipidemic effeck
acebutolol pindolol
which B blocker has no sedative effect?
atenolol
which B blocker has B1 selectivity?
atenolol acebutalol metoprolol
which B blocker has strongest sedative effect?
propranolol
atenolol, propranolol , timolool ,pindolol which one is safe in asthma , DM ,prinzmetal angina?
atenolol or any B1 blocker
HPN Pts whith BPH what best drug?
alph1 blocker like phentolamine.
HPN with MI which antiHPN prefer?
B blocker
USED OF B blocker?
HPN antiarrhythemia glucoma(timolol) migraine , thyrotoxicosis(propranolol)
sotalol
k channel blocker +b blocker (antiarrhythemia)
quinidine use
antiarrhythemia class 1 (na channel blocker block open or active state channels)
quinidine antiarrhythmic and proarrhythemic effect?
antiarrhythemic block fast na channel and increase action potential duration proarrhythemic cause M receptor blocker--^HR and alpha blocker---reflex tacycardia
quinidine S/E
GIT upset, tinnitius,blurred vision, prolonged QRS and QT interval
procainamide
class 1 antiarrhythemia (Na blocker) has same quinidine effect but less muscarinic receptor blocker
procainamide S/E
1_SLE like syndrome 2_hematotoxicity(thrombocytopenia ) CVS effect
SLE inducer drugs?
procainamide hydralazine INZ
what assesstement need for pts on procainamide?
hematological assesstment like cbc regulary
lidocain
class 1b antarrythemia work on inactivated na channal
lidocain uses?
antiarrhythemia esp post MI ,open heart, digitalies toxicity given iv
name class 1b drug antiarrhythemia given orally ?
mexiletine tocainide
S/E of lidocain ?
CNS TOXICITY seizure
flecainide
class 1 c antiarrhythemic drug block all channel in his purkinje fibers
S/E of flecainide?
suuden death so limitted use
esmolol
cardioselective B blocker class 2 use in Rx of SVT
effect of fecainide on APD IS ? INCREASE DECREASE NO CHANGE
NO CHANGE
amidarone
class 4 ant arrhythemic dx used as K blocker
amidarone S/E
pulmonary fibrosis thyroid dysfunction liver toxicity corneal deposition blue pigmentation of skin( smurf skin)
verapamil
like deltiazem ca channel blocker use in Rx of SVT
S/E OF Deltiazem
hypotension flashing face constipation AV blocker
what things should be avoided with verapamil or any ca channel blocker?
1_add with B blocker becouse it cause AV block 2_ verapamil cause displacement digoxine from binding site
adenosine
work on Gi coupled decrease in cAMP used in SVT
drugs cause torsades?
k channel blocker eg amidarone 2_class 1 c eg quinidine ,procainamide. 3_tricyclic antidepression 4_thioridazine other disease like prolonged QT syndrome
Rx torsades
Rx hypokalemia Rx hypomagnesemia RX magnesium
S/E of methyldopa
coombs test positive -CNS depression -oedema
reserpine
destroys vesicles so decrease NE,seretonine,dopamine used in Rx of HPN
reserpine S/E
depression edema
prazosine(azosin)
DOC in Rx HPT with BPH
Prazosine S/E
first dose syncope orthostatic hypotension urinary incontaince
hydralazine
arteriolar dilatation through NO. use in Rx mod to sever HPN.
S/E hydrlazine
SLE like syndrome edema no cause CNS depreesion or postural Hypotesion reflex tachycardia
nitroprosside
work on arteriolar and venules decrease in TPR (NO)
nitroprosside S/E
cyanide toxicity
nifidipine
Ca channel blocker more selective VD
S/E of Ca channel blocker
gingival hyperplasia reflex tachcardia
DOC in emmergency HPN
nitroprosside but should be less than 12-24hr.
losortan
block AT1 receptors
use of losortan
1_mild to mod HPN 2_protective of diabetic nephropathy 3_CHF
S/E of captpril
dry cough (bradykinine degredation) hyperkalemia acute renal faliure in renal artery stenosis angioedema
HPN + ANGINA
B blocker, CCB
HPN+DM
ACEI,ARBS
HPT+HEART FALIURE
ACEI ,ARBS
HPT + POST MI
B blocker
HPT + BPH
ALPH blocker
HPN + DYSLIPIDEMIA
ALPHA blocker + CCBs ,ACEI
Bosentan
endothelin A receptor antagonest used in Rx of pulmonary HPN highly teratogenic
mannitol?
osmotic diuretic
mannitol uses?
1_decrease IOP 2_decrease intracranial pressure 3_rhabdomyolysis 4_anuric state
acetazolamide
like dorzolamide which is carbonic anhydrase inhibitor
dorzolamide
like acetazolamide used in 1_glucoma 2_metabolic acidosis 3_acute motion sickness
acetazolamide S/E
like dorzolamide can cause 1_m acidosis 2_hypokalemia 3_renal stone 4_hyperchloemia
furasemide
loop diuretic
used of furasemide
acute pulmonary edema heart faliure hypertension acute renal faliure hypercalemia
pts found sensitive to sulf group and you want to give loop diuretic what will select?
ethacrynic acid
S/E of furasemide
hypokalemia hypocalcemia hyperuresemia hypophosphatemia sulf group sensitivity ototoxicity (more with ethacrynic acid)
precusion with furasemide ?
co adminestered with aminoglycoside lithium digoxine
hydrochorothiazide use?
HPN CHF nephrolithiasis nephrogenic DI
S/E OF HYDROCHOROTHIAZIDE
sulfa sensitivity hypokalemia hypercalcemia alkalosis hyperurecemia hyperglycemia hyperlipidemia
spirnolactone used
k sparing diuretic hyperaldosteron add with other diuretic to avoid hypokalemia antiandrogen use (female hirstism) CHF
precusion with use thiazide?
not used in DM not use in hyperlipedemia
eplerenone
selective aldosterone receptor blocker have no antiandrogenic effect
pts with prinzmetal angina DOC is?
Ca channel blocker esp nifidipine
what role of B blocker in prinzmetal angina?
C/I
which antiangina drug is safe in DM pts and use chronic use?
isosorpide di nitrate.
what mechanism nitrate is chare with sildenafil?
both increase cGMP so C/I CO adaminester togather
amiloride
Na channel blocker work as k sparing like aldosteron.
common S/e if given compination of losartan and spironolactone?
hyperkalemia
what is MOA for BZ?
inhibit GABAa receptor which activate Cl- channel--hyperploarization
BZ1 work on ?
sedation
BZ2 work on ?
antianxity
what effect of barbiturates on mitochondria?
inhibit complex 1 of electron transport chain
name drug act as antidot to BZ?
flumazenil(non specific BZ receptor antagonest
pts with liver disease and want to use BZ which drugs are safe?
lorazepam ,oxazepam tamazepam are safe becouse not metabolite in liver
imitriptyline
tricyclic antidepreesor
imipramine
TCAs drugs like imitriptyline
uses of TCAs ?
major depression anuresis obssesive compulsive disorder panic attack neuroleptic pain
tri cyclic antidepression toxicity?
3 c cardiotoxicity convulsion coma
phenalzine
MAO inhibitor
tranylcypromine
MAO inhibitor
paroxitine
SSRIs
fluoxitine
SSRI drug
mirtazepine
like yohimbine alpha 2 antagonist but used as antisuppression associated with wt gain
bupropion
dopamin reuptake blocker ,used in smoke cessation
DOC for bipolar Disorder
lithium
MOA of lithium
prevent recycle of inositol and decrease in cAMP
S/E of lithium
1-tremor 2 life threatening seizure 3-hypothyroidism (inhibit deiodinase ) 4-Neph diabeties insipidus Rx by amiloride teratogenic (truncus artheriosis)
names 2 drug used for bipolar disorder
Lithium valproat
drug used for neuroleptic pain?
1- tricyclic antidepreesion 2-carpamazepine(trigeminal neuralgia) 3-gabapentine
tolcapone
COMT inhibitor which ihnibit conversion L dopa to 3 o methydopa
S/E of tolcapone ?
hepatotoxicity
selegiline
MAOb inhibitor
seritonin syndrom
rigidity,sweating, hyperthermia,myoclonus seizure
cefazolin
first generation cephalosporine
cephalexin
first generation cephalosporine
cefotetan
second generation cephalosporine
cefaclor
second generation cephalosporine
cefuroxime
second generation cephalosporine and cross BBB
cefoperazone
3ed generation cephalosporine and doesnt cross BBB
cefdinir
3ed generation cephalosporine
cefixime
3ed generation cephalosporine
cephepime
4ed generation cephalosporine
organism that not cover with cephalosporine
listeria monocytogenesis atypical eg mycoplasma MRSA enterococci
name drug which commonly given with imipenem that inhibit rapid metabolities in kindney?
cilastatin
aztreonam advantage ?
no cross allerenicity with penicilline or cephalosporine
vancomycine MOA?
inhibit D ala D ala muramyl pentapeptide
ototoxicity drugs?
aminoglycoside vancomycine ethacrynic acid
S/E of vancomycine?
1-red man syndrome 2-ototoxicity nephrotoxicity
piperacilline
like ticarcillin antipseudomonus
azlocillin
antipseudomonus
which penicilline group are lipid soluble
nafcillin oxacillin
which penicilline drug cause interstitial nephrities
methacillin
ticarcilline
antipseudomonus
abcixiumab
antiplatet(monoclonal antibody against gp11b 111a
infliximab
monoclonal AB against TNF used in Rheum arthrities,crhons disease
trastuzumab
used in breast cancer (monoclonal ab against erb b2
dacliximab
kindney tansplant ab block IL2 receptor
muromonab
used in kidney transplant against allograft rejection
palivizumab
used against RSV
rituximab
non hodkin lymphoma
aldeslekin 2
useed in renal cell cancer ,melanoma
filgrastim
increase granulocytes used for bone marrow recovery
sargramostim
inrease both granulocyte and macrophage usd in bone marrow recovery
interferon gamma
used in chronic granulomatouse disease by increase TNF
interferone B
used in multiple myloma
interlukine 11
icrease in platelat formation used in thrombocytopenia
myclophenal add to cyclosporine as adjuvent by work on ?
inhibit purine synthesis
cyclosporine MOA?
bind to cyclophilin which reduce calcineurin (cytoplasm phosphatase)then decrease T cell transcription factor
S/E OF cyclosporine
gingival hypertrophy ,hepatotoxicity ,nephrotoxicity ,hyerglycemia,hyperlipidemia,HPN,peripheral neuropathies,hirstism
azathioprim
prodrug to 5MP
tacrolimus
work as cyclosporine but not bind to cyclophiline(direct inh calcineurin)
alendrolate
IS bisphosphonate used as DOC FOR postmonopousal osteoporosis ,glucocorticoid induced osteoporosis paget disease
MOA of alendronate
enhanced hydroxyapatite bone strucure,and induce oseoblasts and reduce osteoclast activity...decrease progress of osteoporesis
S/E of alendronate
oesophageal ulcer
teriparatide
recombinant DNA PTH analogus
S/E of teriparatide
if given more than 2 year has high risk of osteosarcoma
leuprolide
GnRH analogus used in case of endometriosis and prostate cancer
pergolide
dopamie used in Rx of hyperprolactenemia
cosyntropin
ACTH used in Rx of infantile spasm
octreotide
somatostatine used in Rx of acromegaly
somatrem
GH derivative
somatropine
human recombanant GH
nafreline
as leuprolide is GnRH analogus
glipizide
second generation sulfonylurea need ndecrease dose in hepatic dysfunction
acetohexamide
first generation sulphonylurea
glyburide
second generation oral hypoglycemia
S/E of sulfonylurea
hypoglycemia weight gain hypersensitivity
chloropropamide? S/E
first generation oral hyoglycemia disulfiram
S/E of metformine
lactic acidosis
ACARBOSE?
ORAL hypoglycemic drug
ACARBOSE? MOA?
ORAL Hypoglycemia drug act by inhibit alpha glucosidase in brush border of GIT
S/E of ACARBOSE?
GIT Disturbance diarrhea ,flatulenc hepatotoxicity, no hypoglycemia
pioglitazone
like rosiglitazone bind to PPAR....INCREASE insuline genes ,increase receptor
S/E of rosiglitazone?
hyoglycemia hyperTG(wt gain) oedema
danaparoid
heparine with different structure and safe in nhypersensitivity to heparin
enoxaparin
LMW heparine less heparine induce thrombocytopenia
argatroban
direct thrombin inhibitor \doesnot reguired AT111---used in heparin iduced thrombocytopenia.
argatropan used?
heparine induced thrombocytopenia
warfarin MOA ?
inhibit epoxide reductase
warfarin antidot
vit k in slow onset fresh frozen plasma (fast)
increase platelet aggregation ?
ADP,5TH,TXA2,THROMBINE,ALPHA2 AGONEST
DECREASE plt aggregation by?
PGI2, cAMP,ASA,GP 11b/111a BLOCKER

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