Post on 06-Jul-2018
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I Love pharm
A love/hate relationship story
narrated by Monica andMariam
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OTHER CNS DRUGS
Anti-Smoking
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Nicotine Replacements
• Nicorette – Nicotine Gum
– ransdermal !atch
• "-#igarettes
• Nasal Spray
•
Nicotine Inhalers
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Nicotine M$A
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%upropion &'yban(
• M$A) *A and N" reuptake inhibition decreasesre+arding e,ects o nicotine
• S" and #autions) – Sei.ure prone patients
• 0 o sei.ures
• Anore0ia/bulimia
• ead trauma
• #NS tremor
• #irrhosis
– Increased suicidal thinking – #aution in patients +ith &especially when using transdermal
patch))• #1 *isease
• N
• #A*
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1arenicline hanti0(
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#hanti0
• S" and #autions – Increased suicidal thinking
– Increased incidence o stroke and heart attacks
–Aggression/violence
– A,ects vision2 cognition2 and motor control• rouble operating machinery
– N/1
– Strange dreams
– Sei.ures
– Need to ad3ust dose or renal dysunction
– **I +ith alcohol
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OTHER CNS DRUGS
Migraines
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*iagnosis
• 4ive headaches marked by pain and t+o o theollo+ing) – $ne-sided
– !ulsating
– Moderate to severe intensity
– Aggravated by routine physical activity
• !lus one) – N/1 or both
– Abnormal sensitivity to light and sound• $ther criteria
– Last rom 5-67 hours
– No underlying cause +hen evaluated medically
–Not be attributable to any condition other than migraine
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Acute reatment
• $#) aspirin2 ylenol2 NSAI*S
• Midrin – Acetaminophen 8 Isometheptene 8 *ichloralphena.one
• !rescription strength NSAI*s – *icloenac
– Indomethacin
– oradol
• Triptans – Abortive
– 5-HT 1B/1D receptor agonists
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!reventive Medications
• %! Meds – %eta-blockers &propranolol(
– ##%s &1erapamil 9 cluster headaches(
• Anti-sei.ure Meds – *epakote
– opama0
– Gabapentin
• #As – Amitriptyline
– Nortriptyline
– !rotriptyline
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$ther Medications
• %utalbital preparations – #ombine sedative butalbital +ith aspirin
and ca,eine
– #an be addictive and may cause reboundheadaches
• $pioids such as codeine
• #orticosteroids2 especially or migrainesthat last or : days or more
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OTHER CNS DRUGS
Anti-!arkinson;s
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$vervie+
• !rogressive disease that a,ectsnerve cells in the part o the braincontrolling muscle movement
• #ause) damage o nerve cells insubstantia nigra that typicallyrelease *A
– *A transmits signals bet+een substantianigra and corpus striatum allo+ingmuscles to make smooth2 controlledmovements
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reatment
• Medications) – Sinemet &Levodopa and #arbidopa(
• #arbidopa blocks destruction o levodopa by dopa-%
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$ther Medications
• Mirape0
– Synthetic *A receptor agonist
– #an cause compulsive gambling
• Selegiline &"ldepyrl( – MA$-% Inhibitor
– !revents breakdo+n o *A by MA$-%
– #an also be used as an antidepressant
• #ogentin – Anticholinergic
– Reduces Ach to reduce tremoring caused by
e0cessive Ach activity
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Implications or *entistry
• >erostomia
• "namel erosion rom N/1
•*i?culty brushing teeth
• I oral tremor2 dental care di?cult
– Schedule @-B minutes ater levodopadose +hen symptoms are ma0imallyreduced2 ho+ever levodopa can causedyskinesias
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**Is
• Levodopa may sensiti.e heart to epi inducedarrhythmias – #aution +ith epi
• #$M inhibitors) – Increase %! and sensiti.e myocardium to arrhythmias
• #aution +ith epi
– "rythromycin and Ampicillin can reduce biliaryelimination o "ntacapone
• Selegilene – Metaboli.ed to amphetamine and methamphetamine
• Avoid epi
– his is an MA$I 9 avoid Meperidine• #auses buildup o to0ic metabolites o Meperidine
ypertensive crisis2 convulsions2 symptoms o opioid $* suchas respiratory depression
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UEST!ONS
$ther #NS *rugs
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Match the anti-!arkinson drug +ith M$A
CD MA$-% inhibitor
7D #rosses the %%% and converts to *A bynerve cells in the brain
:D Synthetic *A receptor agonist5D #$M inhibitor
ED Anticholinergic2 reducing Ach
AD#ogentin%DMirape0#D"ntacapone*DSinemet
"DSelegiline
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All o the ollo+ing are used ormigraine prevention ">#"!
AD Gabapentin
%D !ropranolol#D *epakote
*D riptans
"D Amitriptyline
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/4) 'yban acts as a nicotine receptor
antagonist2 decreasing re+ardinge,ects o nicotineD #hanti0 inhibits *Aand N" reuptake2 decreasing re+arding
e,ects o nicotineD
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Migraine diagnosis includes Fve headachesmarked by pain and t+o o the ollo+ing ">#"!)
AD !ulsating%D Moderate-severe intensity
#D Aggravated by routine physical
activity*D %ilateral
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#arbidopa is used as a treatment o!arkinson;s because it
AD !otentiates the central action o dopamine
%D !otentiates the central action o N"
#D *ecreases the peripheral metabolism olevodopa
*D Inhibits the peripheral stimulatory Fbersrom the #NS
"D Increases the permeability o the %%% toLevodopa
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#ontrol o %lood !ressure
• 7 systems control %!)
CD Sympathetic NS
7D Renin-Angiotensin-Aldosterone system
Sympathetic
RAAS
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%lood !ressure
%! < otal !eripheral Resistance &!R( 0 #ardiac$utput $(
– *rugs that a,ect !R)• Alpha C blockers
• *iuretics
• A#" Inhibitors
• AR%S
•##% type II
– *rugs that a,ect #$)• %eta %lockers
• ##% type I
• *iuretics
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%eta %lockers
• "nd in -$L$LH• 5 types)
CD SpeciFc %eta blockers)• Atenolol/Metoprolol &%C blockers(
7D Non speciFc %eta blockers)• !ropranolol &%C and %7 blockers(
– #auses bronchoconstriction
– Not good or asthmatics
:D Intrinsic Sympathomimetic Activity &ISA(• !indelol2 Acebutolol
– !artial agonists) Stimulate heart a little2 but not as much as body +ould normallystimulate heart Lo+er #$ than normal
– Good or athletes
5D Alpha/beta %lockers• Labetolol
– AA) vasodilating beta blockers
– Lo+ers !R and #$ Good or #4 patients
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%eta %lockers
• Adverse e,ects) – Mask signs o hypoglycemia JJJJ
– "levate blood lipids
– 4atigue2 sleep disturbance
– Impotence
– Korsens bronchoconstriction in
asthmatics &nonselective %%( – Induces hypoglycemia &nonselective %%(
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AlphaC blockers
• "nd in -osinH – !ra.osin2 era.osin2 *o0a.osin
• Lo+er !R Lo+er %!
• Advantages) – Good or elderly patients +ho have a
lo+ #$ but still have high %! due to
elevated !R – *oesn;t a,ect blood lipids like %%
– Also used or %enign !rostate
ypertrophy
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AlphaC %lockers
• Adverse e,ects) – !ostural hypotension
– *ry mouth2 di..iness2 headache2
dro+siness2 nausea
• **I) – "pi reversal
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#entral Acting Alpha7Agonists
• Methyldopa2 #lonidine – Kork #"NRALL
– Khen alpha7 receptors are activated2 it
tells the neuron to S$! releasing theN &N"(
– Activating alpha7 less N" reduced
sympathetic outo+ in #NS reduced%!
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REN!N-ANG!OTENS!NS$STE%
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A#" Inhibitors
• %lock conversion o Ang I Ang II – %locks breakdo+n o %radykinin
– *ecreases sympathetic activation
– *ecreases aldosterone release&decreases uid retention(
• "nd in -prilH
– Lisinopril2 "nalapril2 #aptopril
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Lisinopril
• A#"-I
• reatment) – N
– #4
– MI
– !revents renal/ retinal complication o
diabetes
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A i i II R
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Angiotensin II Receptor%lockers
• "nd in -SartanH – Losartan2 1alsartan &*iovan(
– y.aar) &Losartan 8 #'(
• !revent Angiotensin II rom binding toreceptor
• Results in)
– *ecreased Aldosterone secretion
– *ecreased vasoconstriction – *ecreased sympathetic activation
*ecreased %! *$ N$ a,ect %radykinin
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#a #hannel %lockers
• ype I) – Kork on #a8 channels in the heart to lo+er cardiac output
– "0) 1erapamil
• ype II) – Kork on #a8 channels in vascular smooth muscle to vasodilate
+hich reduces peripheral resistance• &reduces aterloadH(
– "nd in -!ineH• Niedipine
• Amlodipine
• Advantages) – =seul or N patients that also have)
• Asthma2 diabetes2 angina2 peripheral vascular disease2 blacks2 elderly
• Adverse ",ects) – Gingival yperplasia JJJ &espD Niedipine(
– "dema
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Calcium Channel Blockers
Ca+ Ca+
Reduced
Peripheral
Resistance
Reduced
cardiac
output
Type I:
verapamil
diltiazem
Type II:
Nifedipine
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Amlodipine
• Aka) Norvasc
• #a8 channel blocker- ype II
• =ses)
– ypertension – Angina !ectoris
• Least likely to cause gingival hyperplasia
• Metaboli.ed by :A5 – Macrolides 8 antiungals decrease metabolism
o Amlodipine increase to0icity
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ekalmo
• Aliskiren &ekturna( 8 Amlodipine – eturna) targets RAAS by inhibiting
Renin
• Renin is responsible or the Cst step in RAAS+hich is the conversion o Angiotensin Angiotensin I
– Amlodipine) ##% &type II(
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*iuretics
• #ause person to lose Na8 and 7$ by impairing thereabsorption o Na8 in the renal tubules
• ypes)
CD hia.ides) ydrochlorothia.ide &#'(• Korks in the distal tubule
7D igh-ceiling/ Loop diuretics) 4urosemide &Lasi0(• Korks in the loop o enle
:D !otassium sparing) Spironolacton2 Amiloride
• Cst line drug or NJJ
• =ses) –. #4
–. N
• Adverse e,ect) –. ypokalemia &e0cept the potassium sparing(
• #an be used in combo +ith other N drugs to enhance their
e,ect
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hia.ide *iuretics
• #'
• M$A) – Inhibit Na8 reabsorption in distal tubule
and thereore increase the e0cretion oNa82 #l-2 and 7$
• Adverse e,ects)
– ypokalemia +eakness2 atigue2di..iness2 leg cramps
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Loop *iuretics
• 4urosemide &Lasi0(
• More potent than hia.ide diurectics
• =se) – Khen use o hia.ide diuretics is #/I due
to impaired renal unction because thesediuretics preserve renal blood o+
– Good or elderly2 blacks• Adverse e,ects)
– ypokalemia2 dehydration
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!otassium Sparing *iuretics
• Spironolactone2 riamterene2Amiloride – Spironolactone M$A)
• #ompetitive antagonist at aldosteronereceptor
– riamterene M$A)• %locks apical membrane Na8 channel
• =sually used as a combo +ith otherdiuretics to reduce 8 loss rom theFrst diuretic
•
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Diuretics and N%&ID%
Fluid
volumeFluid
volume
Diuretics act in 'idneys
Na+
H!
"+
Reduced
Peripheral
Resistance
#P
decrease
Reduced C$
N%&ID% act via P(inhi)ition in the
renal
system to reduce
renal perfusion*
causin Na+
and H! retention*
thus reducindiuretic effect
#ombo Antihypertensive
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#ombo AntihypertensiveMeds
• =sually a thia.ide diuretic 8 another Nmed
• "0amples)
– Lotensin #) %ena.epril 8 #' – 'estoretic) Lisinopril 8 #'
– riben.or) $lmesartan medo0omil 8Amlodipine 8 #'
– y.aar) Losartan 8 #'
– eklamo) Amlodipine 8 ekturna &direct renininhibitor(
!h l i l i i h
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!harmacological issues +ith
ypertensive patients
• =se "pi +ith caution – Avoid epi cords
• NSAI*s can reduce antihypertensive
e,ect o drugs
• Katch out or additive sedativee,ects
• Katch out or orthostatichypotension
&ntihypertensive Drus %ummary Ta)le
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Class Agents Mechanism Of Action Adverse SideEects
Drug:Drug nteractions
alpha-Cblockers
pra.osintera.osin
alpha-C block rela0es smoothmuscles in vascular epitheliumcausing vasodilation
orthostatichypotension
epi reversal
beta-blockers
propranolol2nadololatenolol2
metoprololpindolol2acebutolollabetolol2carvediol
beta-C P beta-7 blockspeciFc beta-C blockISA activity
alphaC and %C2 %7 block reduction o cardiac output2reduction in renin output anddecrease in sympathetic outo+rom #NS
all) elevationo blood lipids2masking o
signs ohypoglycemiain diabetics2GI upset2atigueD!ropranolol)bronchoconstriction
•NSAI*S may decreasehypotensive e,ects•potential hypertensive crisis +ith
epi2 especially +ith propranolol•propranolol decreasesmetabolism o lidocaine2dia.epam2 morphine viacompetition or en.ymes#entrally
actingsympatholytics
clonidine methyldopa
direct alpha-7 agonist converted to alphamethylN"2 adirect a-7 agonistQboth reduce sympathetic outo+rom #NS
sedation additive #NS depression) %*'s2alcohol2 narcotic analgesics
A#"Inhibitors
captorpril2enalaprillisinopril
•blocks conversion o angiotensin C toangiotensin-7 &a potentvasoconstrictor(Q•also decreased rate o bradykinininactivation &bradykinin is potentvasodilator( these actions result in
peripheral vasodilation• hese drugs are less e,ective in ArianAmerican patients
coughangioedema&captopril(altered taste
NSAI*S may decreasehypotensive e,ects
Angiotensin Receptor%lockers
Losartan$'AAR(1alsartan&*I$!AN(
competitive anatagonists at theangiotensin-C &A-C( receptorD heseblock the action o angiotensins II andIII2 blocking the vasoconstrictor andaldosterone secreting e,ects oangiotensin II producing a reduction inblood pressure similar to the A#"-inhibitorsD hese drugs are lesse,ective in Arian American patients
heir increasedselectivity oaction vsD theolder A#"inhibitors2ho+ever2 resultsin their lackingthe adverse sidee,ectsassociated +iththese drugs suchas coughing andangioedemaD
same as A#"-Inhibitors
#alcium#hannel%lockers
niedipine2amlodipine&ype I I( verapamil2diltia.em
&ype I(
peripheral arterial vasodilationvia direct action on vascularsmooth muscle
+ork mainly via negative
inotropic e,ect on myocardiumQalso dilates areterioles
gingivalhyperplasia&niedipine( All) edema2 GIupset2
headache
NSAI*S may decreasehypotensive e,ects niedipine can increase digo0inlevels
*iuretics urosemide&loop acting( hydrochlorothia.ide &distaltubules( spironolactone&potassiumsparing(
reduces %! by causing uidreduction via increased sodiume0cretionQ also via vasodilatoryaction
•ypokalemia•Increased risko arrythmias•hypokalemia2alteration oglucose levels •hyperkalemia
may increase the oto0icity oaminoglycosides NSAI*S may decreasehypotensive e,ects Increased chance o hypotension+ith sedatives or opioids
*irect-actingvasodilators
mino0idilhydrala.ine
vasodilation via direct rela0ationo precapillary sphincters
mino0idil)tachycardia2hypertrichosis hydrala.ine)ree0
tachycardia
t ype te s e us %u a y a) e
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UEST!ONS
Antihypertensive drugs
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Su?0
• Remember) – Alpha C blockers -osinH
– %eta blockers -ololH
– A#"-I -prilH
– AR%s -sartanH
– #a8 #% type II -pineH#aliornia a( has a lot o !IN" trees
Sartan sounds like Sultanhe Sultan is an ARa
he A#" takes !ILLS &pril(
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Match the drug +ith its M$A
CD Spironolactone
7D Losartan
:D !ropranolol
5D Lisinopril
ED #lonidine
@D 4urosemide
6D Atenolol
D !ra.osin
BD Labetolol
CD1erapamilCCDAmiloride
C7DNiedipine
C:Dydrochlorothia.ide
AD Alpha-C blocker
%D Alpha-7 agonist
#D Non speciFc beta blocker
*D SpeciFc betaC blocker
"D 1asodilating beta blocker4D A#"-I
GD AR%
D ##% type I
ID ##% type II
TD hia.ide diuretic
D Loop acting diuretic
LD 8 sparing diuretic
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Khich o the ollo+ing drugs is acombination o an A#" inhibitor 8 adiureticU
AD 'estoretic
%D y.aar
#D Lotrel
*D eklamo
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Khich antihypertensive medication+orks in the #NS to reduce bloodpressureU
AD !ra.osin
%D #'
#D 1erapamil
*D #lonidine
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Khich o the ollo+ing diuretics cancause hyperkalemiaU
AD #'
%D 4urosemide
#D Lisinopril
*D Spironolactone
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All o the ollo+ing antihypertensivemedications +ork by lo+ering !Re0cept)
AD !ra.osin
%D Atenolol
#D #'
*D 1erapamil
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Khich o the ollo+ingantihypertensive medications iscontraindicated or asthmatics and
diabeticsUAD Lisinopril
%D Losartan
#D !ropranolol*D !ra.osin
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Khich o the ollo+ingantihypertensive medications is alsoused to treat benign prostate
hypertrophyUAD Atenolol
%D Labetolol
#D #lonidine
*D !ra.osin
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Khich o the ollo+ing is not acomplication o A#"-IU
AD ypokalemia
%D Angioedema
#D yperkalemia
*D *ry cough
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Khich o the ollo+ing drugscommonly causes gingivalhyperplasiaU
AD 4urosemide
%D Niedipine
#D Lisinopril
*D Atenolol
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Khich o the ollo+ing diuretics +orksin the distal tubuleU
AD #'
%D 4urosemide
#D Spironolactone
*D Amiloride
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• Khich o the ollo+ing drugs iscontraindicated +ith "pi because itcauses an epi-reversal reactionU
AD !ra.osin%D !ropranolol
#D #lonidine
*D Losartan
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STAT!NS
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Lipid *isorders
• "levated cholesterolatherosclerosis coronary arterydisease
• #omplications due to atherosclerosis) – $bstructed blood o+2 aneurysms
• reatment or hypercholesteromia)
– Statins
• *iabetics) automatically placed onStatins
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Statins)
• Impair cholesterol synthesis) – Atorvastatin &Lipitor( J
– Simvastatin &'ocor(
– Rosuvastatin restor(
• M$A) – Inhibit MG #oA reductase +hich inhibits
cholesterol synthesis
– Increases V o L*L receptors in liver cell
increased removal o L*L rom blood
• !otency ranking) – #restor W Lipitor W Simvastatin
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Statins
• Advantages) – !revents #1 disease
– reats pts +ith hyperlipidemia
– Anti-inammatory) =seul in treating !eriodontal disease
• Adverse e,ects) – Myopathies
– Rhabdomyelosis
– Memory clouding
–
*iabetesU• **Is)
– :A5 inhibitors ¯olides( increase plasma conc incrisk o rhabdomyelosis
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1ytorin
• 'etia 8 Simvastatin – *ual inhibititon o cholesterol synthesis
8 absorption
1ytorin) 'etia and Simvastatin
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!#SB inhibitors
• Ne+ therapeutic alternative tostatins – !#SB reduce L*L receptors
• Inhibitors block !#SB so you have M$R"L*L receptors more uptake o L*L out oblood and into Liver to be broken do+n
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CARD!O"ASCU#AR DRUGS
Anti-Angina
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ypes o Angina
• ",ort induced2 classic or stable – Most common
– Atherosclerosis coronary artery obstruction reducedblood supply and hence o0ygen delivery to heart
– 0) nitrates2 ##%2 beta-blockers• =nstable
– Increased reXuency and duration and intensityprecipitated by less e,ort
– Symptoms not relieved by rest or nitrates
• !rin.metal2 variant2 vasospastic or rest angina – Least common
– $ccurs at rest due to coronary artery spasm
– 0) nitrates and ##
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reatment - Nitrates
• Nitroglycerin &sublingual2 oral2 patches(
• Isosorbide mononitrate &oral(
• Acute episodes) sublingual
• !rophyla0is) patches2 paste2 oral• M$A)
– Re&'ces pre(oa& reduced o0ygen demand
–*ilates coronary vasculature increaseso0ygenation and perusion to the heart
• **I) 1iagra &potent vasodilator( – hypotension bad
l k
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reatment 9 %eta %lockers
• !ropranolol &non-speciFc(
• Metroprolol2 Atenolol &%C speciFc(
• M$A) Reduces – o0ygen demand o the heart
– cardiac output
– %!
• =sed or prophyla0is taken chronically
•#ontraindications) – Asthma
– *iabetes
– #$!*
–1asospastic angina
##
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reatment 9 ##%s
• 1erapamil – *ecreases R2 contractility2 %!2 and o0ygen demand
• Niedipine2 Amlodipine – Arteriolar vasodilators
• M$A) Decreases a)ter(oa& – %locks calcium entry into cardiac and smooth mm
cells o coronary arteriolar vasodilation reduces myocardial demand P consumption
• Side ",ects – Gingival yperplasia &mainly Niedipine(
– "dema
reatment 9 Ranola0ine
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reatment Ranola0ine&Rane0a(
• #hronic angina
• M$A) Reduces elevated calcium levels reducescardiac output reduces o0ygen demand o theheart
• Sae +ith 1iagra
• **Is – Macrolides and Antiungals
• :A5 substrate) Macrolides and Antiungals +ill inhibit
metabolism o Rane0a to0ic levels and lo+ere,ectiveness
– #odeine• 7*@ inhibitor) Inhibits codeine conversion to morphine
reduces e,ectiveness o #odeine
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%ite of &ction of &nti&ninal Drus
,eins &rteriesHeart -uscle
Before Nitrates(high preload)áBP
After Nitrates (low dose causes
venodilation. reduces preload)âBP
Before Ca++ ChannelBlockers (high afterload) áBP
After Ca++ ChannelBlockers(reduced afterload)âBP
#eta.)loc'ers*HR+ *o'tp't+*B,
Ca++
Ca++
verapamildiltiazem
* contractility*HR+ vaso&i(ation
nifedipine/vasodilation0
Nitrolycerin/Hih dose reducesafterload via dilation
of coronary arteries0
S'..ar/ Tab(e O) Dr'gs Use& To Treat Angina0
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S'..ar/ Tab(e O) Dr'gs Use& To Treat Angina0
Dr'g C(ass %ain Dr'gs %ecanis. o) Action Si&e E))ects
Nitrates
2ac'te terap/-pi((3Cronic terap/ 4 patc3
Nitrog(/cerin Re&'ction o) ./ocar&ia(
o5/gen &e.an&+ pri.ari(/via veno&i(ation 2re&'cing
6pre(oa&738 a(so arteria(
vaso&i(ation
Ortostatic /potension+
ea&aces
Beta-B(oc9ers
2cronic terap/3
,roprano(o(+
Ateno(o(+
%etopro(o(+
,in&o(o(+
Aceb'ta(o(
Re&'ction o) ./ocar&ia(
o5/gen &e.an& via
re&'ction o) eart rate
an& contracti(it/ o)
./ocar&i'. via beta-1
./ocar&ia( receptor b(oc9
Ortostatic /potension+
&i::iness; Ateno(o( acts
peripera((/+ t's &oes
not pro&'ce CNS e))ects
associate&
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UEST!ONS
Anti-Angina
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Khich o the ollo+ing is most useul intreating or preventing angina pectorisU
AD *igo0in
%D Yuinidine#D !ropranolol
*D Lisinopril
"D All the above
"ach o the ollo+ing can be used in
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"ach o the ollo+ing can be used inprevention and treatment o angina ">#"!)
AD *igo0in
%D !ropranolol#D Nitroglycerin
*D 1erapamil
Khich anti-angina medication
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Khich anti angina medicationreduces preloadU
AD Niedipine
%D !ropranolol
#D Nitroglycerin
*D 1erapamil
Khich anti-angina medication
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Khich anti angina medicationdecreases aterloadU
AD Niedipine
%D !ropranolol
#D Nitroglycerin
*D Atenolol
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CARD!O"ASCU#AR DRUGS
eart 4ailure
$ i
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$vervie+
• eart is unable to pump enoughblood to meet the body;s needs blood backs up builds up in lungs
and legs edema heart tries torespond to increased demands constant increased preload volume
and aterload pressure ventricularremodeling
#auses
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#auses
• yperthyroidism – Metabolic demands greatly e0ceed #$
• #ongestive eart 4ailure
– eart is diseased typically rom heartattacks killing cardiac muscle
– eart ine?cient at pumping blood
throughout body ventricles havereduced orce o contraction
t t !h th G l
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reatment 9 !harmacotherapy Goals
• o get rid o the e0cess uid thatbuilds up in the body reducesvolume o uid that +eakened heart
has to pump• Advanced cases) Glycoside therapy
– o increase contractility o the heart
reatment
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reatment
• A#" inhibitors – Reduce L ventricular volume and Flling
pressure +hile decreasing !R
prevents enlargement o the heart• *iuretics &loop acting() reduces
preload –
Increases sodium and +ater e0cretion reduces uid backup/edema
• 1asodilating beta-blockers – Reduce R and vasodilate
reatment 9 Glycosides)
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y*igo0in
• Inhibits Na82 8 A!AS" increased calciuminu0 increases orce o contraction omyocardium &positive inotropic e,ect(
• Korks to reduce compensatory changes associated
+ith #4 such as increased heart si.e2 rate2 edema• 4or advanced stages o heart ailure
• Narro+ therapeutic +indo+
• **I
– Macrolides• *ecrease GI bacteria that metaboli.e digo0in increased
plasma levels
• :A5 substrate) :A5 inhibitors +ill decrease metabolism increased plasma levels
reatment AR%s
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reatment 9 AR%s
• 1alsartan/Sacubitril &"ntresto() Reduce !R – Sacubitril) prodrug converted to sacubitrilat
inhibits neprilysin en.yme preventsbreakdo+n o vasoactive peptides increased
level o these peptides vasodilation andreduction o "#4 volume via sodium e0cretion
– 1alsartan) blocks angiotensin II receptor vasodilation and reduction o "#4 volume
• **Is – NSAI*S and #$>-7 inhibitors 9 potential renal
ailure
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UEST!ONS
eart 4ailure
*igo0in e0erts its positive inotropic
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g p p
e,ect by
AD Activation o adenylcyclase
%D An agonist e,ect o beta-receptors
#D Inhibition o Na82 8 A!ase leadingto increased calcium inu0
*D *ecreasing the amount o calcium
available or e0citation-contractioncoupling
Khich o the ollo+ing is N$ used
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gin treatment o heart ailureU
AD Lisinopril
%D #'#D 1alsartan
*DLasi0
"D Labetolol
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he cardiac glycosides +ill increase the concentrationo +hich ion in an active heart muscleU
AD Sodium
%D !otassium
#D #hloride
*D #alcium
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CARD!O"ASCU#AR DRUGS
Antiarrhythmics
$vervie+
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$vervie+
• Arrhythmias) abnormalities in impulseormation and conduction in themyocardium
• #an result in) – %radycardia &R Z@ bpm(
– achycardia &R W C bpm(
– 4ibrillation &irregular heart beat(
• ypes – 1entricular Arrhythmia
– Supraventricular Arrhythmia
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SA No&e
• 4unctions as thepacemakerH o heart
• Automaticallygenerates impulses2telling heart to beat
• Sets the pace o heart
beat• #onducts impulses
directly into both atia
A" no&e
• 4unctions as pacesetterH o heart
• Located bt+ atriumand ventricles
• Relays and intensiFesimpulse rom SA node
• 4ibers e0tend rom A1node to ventricles&perkin3e Fbers( – elp ventricles contract
Arrhythmias
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Arrhythmias
• Supraventricular arrhythmias) originate abovethe A1 node – Supraventricular tachycardia)
• Rapid2 regular R &CE-7bpm(
• #an be caused by ca,eine2 alcohol2 etc• Less serious than 1entricular arrythmias
• No t0 reXuired
– A 4ib)• Rapid2 irregular heart rhythm
• Main cause o stroke J &blood pools in the heart and clots(
• reatment) – Anticoagulants
– %eta blockers/ #a channel blockers
– "lectrical cardioversion therapy to restore normal sinus rhythm
Arrhythmias
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Arrhythmias
• 1entricular arrhythmias – 1entricular tachycardia)
• SA node not controlling beating o ventricles
– !remature 1entricular #ontractions &!1#()
• 1entricles contract too soon/ out o seXuence +ithnormal heartbeat
• can be caused by ca,eine2 $# cold meds
• %enign
– 1entricular 4ibrillation)• Lie threatening
• =ncontrolled2 irregular heart beat W :bpm
• atal heart attack
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reatment
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reatment
#lassed by Mechanism• ype I 9 Na channel blockers
– Ia) Xuinidine
– Ib) Lidocaine2 phenytoin – Ic) ecainide
• ype II 9 %eta-blockers) propranolol2metoprolol
• ype III 9 channel blockers) amiodarone
• ype I1 9 #a channel blockers) verapamil2diltia.em
*rug Induced Arrhythmias
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*rug Induced Arrhythmias
• Some drugs can prolong Y interval ventricular arrhythmias
• "0 include) –
Some antiarrhythmics2 especially channelblockers• Amiodarone
– Macrolides
– A.ole antiungals – #A antidepressants
– Atypical antipsychotics
ype I *rugs) block Na channels• Ia) Yuinidine
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• Ia) Yuinidine – M$A) Increases the reractory period o cardiac muscle reduces conduction
velocity o heart
–
0)• A-Fb• ventricular tachyarrhythmias
– as some #lass III activity &can cause ventricular arrhythmias(
– **Is• 7*@ Inhibitor) Lo+ers #odeine e,ectiveness
• Additive e,ects +ith muscaranic antisialogogues
• Ib) Lidocaine – M$A) *ecrease cardiac e0citability
– Acute ventricular arrhythmias arising during MI
– Given I1
– JJdrug o choice or pts hospitali.ed due to 1D Arrhythmia
•
Ic) 4lecainide &ambacor( – M$A) !rolongs cardiac action potential – !revent and treat tachyarrhythmias &supraventricular and ventricular(
– #autions• 7*@ substrate) due to genetic variations in 7*@ e0pression2 patient monitoring o drug e,ects
and dose titration reXuired
• #an aggravate pree0isting arrhythmias or induce lie-threatening ventricular tachycardia
• Increases mortality in pts +ho have had an MI
ype II *rugs) %eta-blockers
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ype II *rugs) %eta-blockers
• !ropranolol P Metoprolol – Reduces incidence o arrhythmias ater
MI
– !revents supraventriculartachyarrhythmias
• "smolol –
Short acting – I1
– Acute arrhythmias occurring duringsurgeries
•
#lass III *rugs 9 channel
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blockers• Amiodarone• !rolong A! duration by slo+ing rate o
repolari.ation
• Severe reractory supraventricular and
ventricular tachyarrhythmias• 0)
– A-Fb
• S"/**I – %lue skin discoloration due to iodine accumulation
ound in drug
– 7*@ inhibitor) Lo+ers #odeine e,ectiveness
#lass I1 *rugs) ##%s
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#lass I1 *rugs) ##%s
• 1erapamil and *iltia.em• Slo+s conduction and prolongs
reractory period
• Atrial arrhythmias W 1entriculararrhythmias
Supraventricular *rugs o
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#hoice
• "erapa.i(• Digoin
– *ecreases the rate o A1 conduction
• %eta blockers
• Yuinidine
• ospitali.ed patients) lidocaine is the
Frst line o treatment
*entistry Implications
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*entistry Implications
• $rthostatic hypotension can be anissue since #1 unction depressed
• Stress can provoke arrhythmias
• #aution +ith epi – Avoid +ith propranolol
• 7*@ inhibitors
– Yuinidine – Amiodarone
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UEST!ONS
Anti-Arrhythmics
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Khich o the ollo+ing anti-arrhythmicdrugs are contraindicated +ith#odeineU
AD Yuinidine%D Lidocaine
#D Amiodarone
*D 1erapamil
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Khich antiarrhythmic drug class mostcommonly causes arrhythmiasU
AD ype I
%D ype II
#D ype III
*D ype I1
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Khat is the antiarrhythmic drug ochoice used to treat 1-arrhythmias inthe hospitalU
AD Yuinidine%D Lidocaine
#D 4lecainide
*D 1erapamil
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Antiplatelets
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• Aspirin – Most +idely used anti-platelet
– Inhibits thrombo0ane synthetase irreversibly inhibits !Gsynthesis
– !rophyla0is against stroke and MI
– *aily baby aspirin Cmg dose
• #lopidogrel &!lavi0(2 iclopidine &iclid(2 !rasugrel
– inhibits platelet aggregation mediated by A*!
– Given or patients +ith aspirin allergy
– Atherosclerotic patients to prevent A2 strokes2 coronary arteryclosure in pts underdoing angioplasty
– *o not stop !lavi0 prior to surgery or patients +ith cardiac stents
– **Is/#autions• 7#CB Substrate) people di,er genetically +ith this gene
– !rasugrel is alternative2 as it is not a 7#CB substrate
• Avoid heartburn meds can reduce e,ectiveness o !lavi0 and increaseMI risk
• %oth used or unstable angina
eparin !roducts
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• eparin Sodium2 eparin #alcium
– hrombin Inhibitors
– Acts in bloodstream &I1(
– %lock conversion o prothrombin thrombin
– Measured by !
– S") increased bleeding and thrombocytopenia• "no0aparin &Loveno0(2 *alteparin &4ragmin(
– LMK
– SY
– More selective
– Monitoring not necessary
• *12 pulmonary embolus2 unstable angina2 acuteMI2 prosthetic heart valves
#oumarin !roducts
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#oumarin !roducts
• Kararin Sodium oumadin(• #ompetitively inhibits the synthesis o 1itamin- dependent
coagulation actors in the liver
• Stroke prevention in patients +ith A-Fb2 stroke2 *1
•
Measured by !/INR• Narro+ therapeutic +indo+
• Should not be stopped beore routine dental surgery
• **Is 9 Increased bleeding – 7#B inhibitors &Metronida.ole2 macrolides2 a.oles(
• Inhibit metabolic breakdo+n o Kararin accumulation increasedbleeding
– Antibiotics &etracycline( diminish gut ora responsible or 1it synthesis can increase bleeding
– Acetaminophen2 Aspirin2 NSAI*s) compete or plasma sites on
protein
*irect hrombin Inhibitors
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• *abigatran &!rada0a(
• #ompetitive direct thrombin inhibitor 9 preventsconversion o Fbrinogen to Fbrin
• #linical advantage vs Kararin – No blood monitoring
– Korks Xuicker – 4e+er **Is
– =na,ected by ood
• Advantage) Reversal agent &!ra0bind( 9 binds
directly to drug• Kararin alternative or or *1 prophyla0is ater 3oint
replacement
• Also used as orally administered Loveno0 alternative
4actor >a Inhibitors
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4actor >a Inhibitors
• Rivora0aban &>arelto(• Api0aban &"liXuis(
• "do0aban &Savaysa(
• *1 and non-valvular A-Fb• $ral administration
• Inhibits actor >a preventing Fbrinproduction decreased blood coagulation
• Antidote in development
• **Is – :A5 Substrate) Avoid :A5 inhibitors
increased bleeding
*ental #onsiderations
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*ental #onsiderations
• #onsult +ith physician on +hether ornot to discontinue anticoagulanttherapy
• #onsider prophylactic antibiotics• NSAI*S cause gastric erosion and GI
bleeding increased bleeding +ith
all the above anticoagulants
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UEST!ONS
Anticoagulants
Match the anticoagulantith M$A
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+ith M$ACD Inhibits synthesis o 1it- dependent coagulation
actors
7D 4actor >a inhibitor
:D Inhibits thrombo0ane synthetase
5D !revents conversion o prothrombin thrombin
ED *irect thrombin inhibitor
@D Inhibits platelet aggregation mediated by A*!
AD !lavi0%D Kararin#D !rada0a*Deparin"D Aspirin
4D Rivora0aban
Khich anticoagulant is a 7#CB
substrateU
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substrateU
AD Kararin
%D Aspirin
#D Rivora0aban*D!lavi0
"D !rada0a
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!atients on eparin reXuire !/INR
monitoringD !atients on KararinreXuire ! monitoringD
AD %oth statements true
%D %oth statements alse
#D 4irst statement true2 second
statement alse
*D 4irst statement alse2 secondstatement true
Khich anticoagulant has theadvantage o an antidote availableU
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advantage o an antidote availableU
AD Kararin
%D Aspirin
#D Rivora0aban
*D!lavi0
"D *abigatran
Khich anticoagulant is a :A5 substrate and
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Khich anticoagulant is a :A5 substrate andshould not be combined +ith a :A5 inhibitorU
AD Kararin
%D Aspirin#D Rivora0aban
*D!lavi0
"D *abigatran
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DRUG-DRUG!NTERACT!ONS
Antibiotic **Is
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CD #idal-Static **I – #idal Abs target actively gro+ing bacteria cell +allD Static Abs inhibit
bacterial gro+thD hereore Static Abs decrease e,ectiveness o cidal Abs
7D etracycline)
– Metal cations &e0) ums2 rolaids() orm comple0 +ith etracycline andinhibit absorption rom GI tract
– *igo0in) etracycline +ipes out bacterial ora in GI +hich is responsibleor metaboli.ing *igo0in increase in digo0in to0icity
– Kararin) etracycline +ipes out bacterial ora in GI +hich is involved in1it synthesis additive bleeding
:D Metronida.ole)
– Alcohol) *isulFram- r0nD Metronida.ole inhibits acetaldehyde
dehydrogenase +hich is needed to metaboli.e alcohol build up oalcohol acetalaldehyde N/1
– Kararin) Metronida.ole inhibits 7#B +hich is needed to metaboli.eKararin increase in Kararin increased bleeding and INR
Antibiotic **Is
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• Macrolides- :A5 inhibition **Is)CD %en.os) increases duration o action o ben.os
7D >arelto/ "liXuis) increased bleeding
:D Lipitor) increased risk o rhabdomyelosis
resulting in mm pain2 +eakness2 kidney ailure5D #arbame.epine/ !henytoin) increases plasma
levels increased to0icity o anticonvulsants
ED Anticancer agents) increased to0icity
@D Antianginal drugs &Rane0a() increased to0icity
Jsame **Is +ith A.ole antiungals
Antibiotic **Is
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• Macrolides) non :A5 **I interactions)CD Kararin- "rythromycin)
aD Kararin is metaboli.ed by 7#BD "rythromycininhibits 7#B increased bleeding
7D *igo0in-"rythromycin/#larithromycin)aD "rythromycin +ipes out GI bacteria that
metaboli.es *igo0in increased *igo0into0icity &same **I as tetracyclines-*igo0in(
bD "rythro/#larithro inhibits !-gp drug e[u0 pump increases oral absorption and decreasesclearance o *igo0in *igo0in to0icity
Analgesic **Is
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g
• Aspirin 8 plasma protein bounddrugs) – Aspirin competes +ith protein binding o
Kararin &results in increased bleeding(and !henytoin &results in antisei.ureto0icity( leading to increased blood conco these drugs
• Acetaminophen)CD %arbiturate/ Alcohol **I) IN#R"AS"
metabolism o tylenol to its
hepatoto0ic orm
NSAI* **Is
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• **Is that increase bleeding)CD Anticoagulants) increases INR and GI bleeding
7D !a0il/ !ro.ac &SSRIs() Increased upper GI bleeding
:D erbals) additive bleeding due to altered plateles &anyherbal that starts +ith G(
5D Alcohol) increased GI bleeding2 ulcerations• $ther **Is)
CD Aspirin) ibuproen INI%IS blood thinning action o Aspirin+hen taken beore aspirinD ake aspirin 7 hrs beore NSAI*
7D Lithium) NSAI* reduces renal clearance o lithium lithium
to0icity:D Antihypertensive drugs) NSAI*s increase Na8/7$ retention decreased e,ectiveness o antihypertensive drugs
$pioid **Is
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p
• #NS depressants) cause additive #NS depression – Include %en.os2 %arbs2 anticonvulsants2 antihistamines2 etc
• Respiratory depressants) cause additive respiratorydepression
– Include ben.os2 barbs
• 7*@ inhibitors 8 #odeine) inhibit conversion o codeineto morphine decreases e,ectiveness o #odeine
– 7*@ inhibitors include)• SSRIs &!a0il/ !ro.ac(
• Antiarrhymic drugs &Yuinidine/ Amiodarone(
• Antianginal drugs &Ranola0ine(
– Also e,ects $0ycodone/ hydrocodone but to a lesser degree
• Nalo0one/ Naltere0one) these are opioid antagonists decrease e,ectiveness o $pioids
Local Anesthetic **Is
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• #As/ SNRIs/ #ocaine – %lock reuptake o N"/" hypertensive crisis due
to too much "pi
• Non speciFc % %lockers
– "pi acts on alpha and beta receptorsD Khen betais blocked2 "pi can only +ork on alpha receptorsresulting in too much vasoconstriction Ncrisis ollo+ed by ree0 bradycardia
• Antipsychotic agents/ Alpha C blockers) – "pi reversalD $rthostatic hypotension ollo+ed by