Winter 2 Flashcards
1
Q
Sulfonylureas drugs
A
-Glyburude, glipizide, glimepiride
2
Q
hydralazine
A
- Selective arteriolar vasodialators
- decrease BP by decreasing TPR thru direct dilating arterioles( not arteries or veins)
- PRIMARY AFTERLOAD REDUCTION IN CHF -works by releasing NO from endothelium
- high first pass effect with rapid acetylators
- alone- increase hydrostatic pressure in capillaries leading to edema and retention of H2O and Na in the Kidney, also Symp and renal compensation-> massive catecholamine and renin release
SE: tachycardia, edema, and loss of affect, lupus like reaction
-use - effective as “third drug” to diuretics and B blockers
3
Q
Lidocaine
A
Class 1B anti arrhythmic drugs
- Rapidly interact with Phase 0 Na channels, shortens phase 3( decreasing AP duration and ERP due to inhibition of late Na channels open in the plateau -USE- emergent treatment of Vent arrhythmias during MI/ ischemia
- suppress vent arhtyhm via decrese slope of phase 4 and increase threshold, abolish reentry arrhythmias, stop TdP b/c down APD
- IV only -SE-drowsyness , slurred speech, confusion, arrhythmias in presence of Hyper K
4
Q
fifth generation Cephalosporins
A
Ceftaroline-Parenteral
- increased binding to PBP 2a–> used to treat MRSA
- CAP- s. pneumo, S aureus(metacillin resistant only), h flu, kleb pneumo, e coli
- Acute skin infections- MRSA
5
Q
Exenatide
A
GLP-1 agonist BID sub Q injection b4 meals
- rapidly absorbed after injection and peak action in 2 hours, little metabolism and excrete via kidney Bind to GLP-1 R in pancreatinc B cells and increase insulin synthesis and secretion in glucose dependent manner
- delay gastric emptying and decrease apatite - decrease the release of post prandial glucagon( mech unknown)
- antagonize glucagon and increase affect of insulin
- SE- GI disturbance, nausea at start of therapy, weight loss, hypo glycemic when combined w. sulfonylurea, pancreatitis( rare but serious), delay in gastric empty can alter other drugs
contra- pancreatitis history,
USE- mono or combination therapy for DM2
6
Q
Procainamide
A
Class 1A anti arrhythmic drugs -blocks Na channels to decrease slope of phase 0 and blocks K channels(metabolite) to prolonge Action potential duration and Effective refractory period
- USA IV only, acetylated in the liver to NAPA->K channel effects, NAPA eliminated via kidney
- SE-lupus syndrome, confusion (CNS effect), GI intolerance, less a block/atropine effect, V arrhythmias but less TdP than quinidine
7
Q
Colesevelam
A
Bile acid binding resin -in intestine exchange Cl- for Bile acids and sequester them from reabs -overall effect is decreased LDL by Liver taking up more to have cholesterol to synthesize bile acids -initially increases VLDL( don’t use in high VLDL pts) and may increase HDL -USE: high LDL hyperlipidemia , SE: no systemic toxiciticy, resins can sequester other drugs and nutrients in GI tract and should be taken at separate times, interfere w/ fat soluble vitamins/iron abs NEW- -SE-GI disturbance, increase triglycerides, contra- hypertriglyceridemia, pancreatitis history, esophageal/ GI disorders, - treat DM2, taken BID
8
Q
Amylin Analogues
A
Pramlitide
9
Q
Cefixime
A
third generation Cephalosporins, oral 2nd line N gonorrhea
10
Q
thiazolidinediones drugs
A
pioglitazone rosiglitazone
11
Q
excretion of penicillins
A
10% Glomerular filtration, 90% tubular secretion - dose modification for renal function -exception: Naficillin- biliary excretion, oxacillin and dicoxacillin by both renal and biliary( no dose adjustment for renal function w/ these drugs)
12
Q
carvedilol
A
antioxidant, alpha blocker and B blocker
13
Q
Treatment go Digitalis toxicity
A
-discontine or reduce dose -discontinue or reduce diuretics of K gets too low( many pts have high RAAS-> decreased K and that ^ neg effects of digoxin) -above don’t work then administer KCl - administer Digoxin Abs in life threatening tox or sever HYPER K due to masive inhibition of Na/K ATPase - Lidocaine and propanolol- rapidly counteract dig toxicity arrhythmia
14
Q
MOA of penicillins
A
- inhibition of cell wall synthesis -B lactam ABx inhibit the transpeptidase enzyme and the production of a highly cross linked peptidoglycan cell wall - only effect actively dividing cells that are producing cell walls - binding to penicillin binding proteins -activation of cell wall autolytic enzymes, autolysin - use in combinatinon with aminoglycosides
15
Q
nesiritide
A
vasodialator and diuretic only given IV
decreases arterial and venous smooth muscle tone via increaseing [cGMP]i
-diuretic action from its natural ability to act as a natriuretic peptide
16
Q
Glyburide
A
Sulfonylureas insulin secretagogues -require functioning Beta cells–> only intreating early Type 2 diabetes, T1/2=10 hrs -Bind to K ATP channel on B cells and inhibit their activity causing depolarization-> influx of calcium-> insulin release -highly bound, metabolized in liver and secreted in urine -SE- HYpoglycemia, Weight gain, sulfur allergy -contra- hepatic impairment, renal insufficiency, pregnant and brest feeding -clinical use- type 2DM, BID, lose efficacy as B cell function decreases, and can be combined w/ metformin and thiazolidinediones
17
Q
Antipseudomonal Penicillins
A
Ticarcillin + Clavulanate potassium
Piperacillin + Tazobactam
tilcarcillin- used in pseudoonas and mixed anaerobic aerobic infections caused by bacteroides(metronidazole prefered)
18
Q
Penicillin V
A
more stable under acidic conditions therefore better GI absorption - less active than PenicillinG- only used for moderate infections
19
Q
Nitroglycerin
A
antianginal agent
- PRIAMARY PREOAD REDUCTION IN CHF
- decreases peripheral resistance and thus preload( low doses and Afterload(higher doses)
- decreases O2 demand of cardiac cells by decreasing cell tension
- long term therapy an lead to tolerance
20
Q
AceButolol
A
Class II anti arrhythmia drugs
- B adrenergic blocker
- B1 selective blocker, reduces risk of bronchospasm -Partial Agonist (ISA)
diminish phase 4 depolarization, depressing automaticity, especially in nodal tissues
- treat arrhythms cause by too much symp activity
- careful in use w/ Ca channel blockers b/c together can too much depress normal cardiac function
- Membrane stabilizing
- low lipid solubility ?
21
Q
Ceftriaxone
A
third generation Cephalosporins,
- Parenteral first line N gonnorrhoeae
- neuro complication from lyme disease
22
Q
macrolides
A
Erythromycin, and semisynthetic derivatives clarithromycin, azithromycin
- broken down by acid, poor abs with food, esters of the base made to increase Abs
- wide distribution except to CNS, can cross placenta and in breast milk, avoid use in liver disease
MOA- bacteriostatic by reversible binding to the 50S subunit to inhibit protein synthesis, similar binding site to chloramphenicol-> they have antagonistic effects on eachother
-resistance- breakdown by bacterial esterases, MODIFICATION OF THE 50S BINDING SITE or methylase enzyme that binds to prevent drug from binding
23
Q
DPP-4 inhibitors
A
sitagliptin
- DPP-4 is an enzyme that degrades incretin hormones, taken 1x/day
- increase the circulating levels of GLP-1 and GIP thus increasing post prandial insulin and decreased glucagon level
- other drugs- saxagliptin, linagliptin, alogliptin
- high oral availability, inhibit DPP-4 for 12 hours -saxagliptin is a prodrug
SE- increased rate of infection, headache, hypoglycemia when given with other drugs, pancreatitis, hypersensitivity rxn
use-mono/combination therapy for DM2
24
Q
Piperacillin + Tazobactam
A
Ureidopenicillins, Antipseudomonal Penicillins
- piperacillin is B lactamase sensative and tazobactam is given with it to stop this
- broader spectrum of action than carbenicillin and ticarcillin, esp in G- aerobic bacilli and mixed infections
- Use- CAP, HAP w/ fluoroquinolone, septicemia from G- bac, UTI in hospitilized(w/aminogylcoside), OB infections, intraabdominal infections,
- less sodium than ticarcillin –> better for CHF pts, less prolonging of bleeding time
25
Digoxin use and toxicities
- slow oral route for non emergent cases, fast IV for emergent cases
- can be anti arrhythmic, protect vent rate in Afib and flutter - given w/ loading dose first of just maintenance doses( this way safer) TOX-LOW MARGIN OF SAFTY
GI- anorexia, nausea, vomiting, dhrea
CV-every known type of arrthymia( V fib and Vtach are most serious)
CNS- mental disoreintations( digitalis dilerium)
Vision- blurred , white border/halos on objects
- sudden increase in plasma Ca can induce arrthymia in these patients
- use with k wasting drugs will ^ risk of neg side effects(K is an antidote for dig tox)
26
Bromocriptine
dopamine agonist
MOA- increase insulin sensativity
reset circadian rhythm to help with insulin resistance
met by the liver, wuick release, first pass met
SE-hypoTN, faint, dizzy, hypo glycemia when w/ sulfonureas
-USE- DM2 adjunct/monotherapy
27
Class II anti arrhythmia drugs
Propanolol Acebutolol Esmolol
diminish phase 4 depolarization, depressing automaticity, especially in nodal tissues
- treat arrhythms cause by too much symp activity
- careful in use w/ Ca channel blockers b/c together can too much depress normal cardiac function
28
Class III anti arrhythmia drugs
Amiodarone
Dofetilide
- inhibit the outflowing K channel and prolong the repolarization, causing longer APD and ERP,
- no affect on other AP phases
29
Imipenem + Cilastatin
Carbapenems, B Lactam Abx
- not orally absorbed, broken down in kidney by dehydropeptidase so cilastatin is added to inhibit this
- renal excretion and dose adjustment for renal impairment, resistant to breakdown by most B lactamases
- inhibits \>90% of clinically important bacteria, ^ permeability in G-, resistant to B lactamase, ^ affinity for PBP
- use only in the worst infections in hospitals, ex: Pseudmonas resistant to all others ( combo w/ aminoglycoside)
- causes induction of B Lactamases to decrease effectivity of other B Lactam ABx,
- tox-can cause seizures, NV, allergic rxn -finish this
30
Digoxin Immune Fab
antigen binding fragments that bind digoxin and the resulting Fab-Fragment-Dititalis complex is excreted int the urine -used in Digoxin toxicity
31
Bacterial resistance to penicillins
- structural differences in PBPs -inibality of penicillin to penetrate to site of action, ex G+ have action near surface where G- have to diffuse thru outermembrane thru morons and many penicillins cannot, eflux pumps ex:pseudomonas lacks high permeability porins, p. aeruginosa, e. coli, N. gonorrhea have active eflux pumps
32
Cephalosporin MOA
interfere w/ bacterial cell wall synthesis- B lactam ring - split B lactam ring destroy activity
33
Digoxin
Digitalis glycoside -increase myocardial contraction and decrease heart rate
- MOA- ^ contractility- inhibits surface bound Na/K ATPase -\> increasing intracell Na-\> reversal of Na/Ca symporter-\> increased [Ca]i and increased force of contraction b/c of Ca
- inotropic effects- ^ CO(quickly), diuresis (eventually and not direct effect), some SNS reversal
- MOA- decreased HR-VAGAL and EXTRAVAGAL( at dangerous high doses)
- interactions- phenylbutazone, phenobarbital and phenytoin, Quinidine, antacids, sulfasalazine, bile acid binding resins
- renal diseaseand hypothyroidism ^ t1/2
34
Cefoxitin
second generation Cephalosporins - activity against B. fragilis
35
Dofetilide
Class III anti arrhythmia drugs
- inhibit the outflowing K channel and prolong the repolarization, causing longer APD and ERP, pure class 3
- USE-SV arrhythmias, corrected via suppress reentry phenomena, very good for A FIB
- iv and oral
- TOX- ventriculat TdP especially in high IV doses
36
repaglinide
Meglitinides, insulin secretagogues, REPAGLINIDE, nateglinide MOA-require functioning Beta cells--\> only intreating early Type 2 diabetes, -Bind to K ATP channel on B cells and inhibit their activity causing depolarization-\> influx of calcium-\> insulin release - quickly absorbed, highly bound, met in liver -Hypoglycemia( less frequent w/ nateglinide) -contra- hepatic impairment, renal insufficiency USE- DM type 2, quicker acting so more preprandial dosing, can be used in sulfer allergies, mono therapy or w/ metformin
37
thiazolidinediones
increase insulin sensitivity in target tissues -PPARgamma agonists - increased sensitivity to insulin stimulate uptake of glossy and fatty acids, alters adipokine production - increased sensitivity in liver and muscle too -long term lower Triglyceride and slight increase HDL and LDL -highly bound, long t1/2 and met in liver -SE-weight gain and edema(most important) osteoporosis and fracture in women, increased risk of CHF, contra- preg, hepatic inpairment( freq LFT needed), heart failure
38
third generation Cephalosporins
Ceftriaxone -Parenteral (longest t.5=8hrs) biliary secretion-\> no dose adjust in renal DS
Cefixime- oral
Cefotaxime-Parenteral
Ceftazidime -Parenteral, good 4 pseudomonas
more G- than 2nd gen- B lactamase resistant lessG+ than 1st gen -useful- G- rods resistant to other ceph, pen and aminoglycosides ABx
-DONT USE w/ enterobacter( makes Chromosoaml B lactamase) - CNS for meningitis- empirical for sepsis
39
Class 1 anti arrhythmic drugs
1A- Quinidine and Procainamide 1B- Lidocaine( Xylocaine) 1C- Flecainide -block mainly Na channels - Quinidine and active metabolite of procainamide also blocks K channels - Use dependent- preferentially block channels in tissues that are abnormally firing high rate - inhibit Na channels in phase 4 and 0 to slow rate of rise of phase 0(1C\>1A\>1B) - increase the threshold for excitability
40
Canagliflozin
SLGT2 inhibitors -inhibits glucose reabs in the proximal tubule -\> decrease blood glucose and increase Glucose in urine - High oral availability, peak at 1-2 hours T1/2=10-13 -SE- Genital mycotic infections, UTI, diuretic effect, CANAgliflozin increases serum digoxin, dapagliflozin increased risk of bladder cancer contra- sever renal impairment USE- mono and adjunct therapy for Dm2, 1x/day before first meal
41
penicillinase resistant penicillins
methicillin naficillin(IVprefered) oxacillin
IV usage for serious systemic Staph infections
- relatively resistant to B-lactamases b/c of bulkier side chains -naficillin is most resistant
naficillin-biliary excretion, oxacillin- biliary and renal, no dose adjustment in renal disease
- these are less active than Penicillin G, use dropped sue to MRSA
- USES- G+ cocci B lacatamase producers-S aureus,( skin infecions, osteomyolitis, acute endocarditis
- not effective to G- aerobes(e coli, kleb, enterbacter)
- methicillin- type 4 interstitial nephritis- use vanco to treat MRSA in hospital
42
Esmolol
Class II anti arrhythmia drugs -B 1 adrenergic blocker Not partial Agonist Not Membrane stabilizing Low Lipid Soluble rapid action, rapid broken down by plasma esterase's - acute arrhythmias during surgeries
43
Magnesium
treatment of TdP, unknown MOA
44
GLP-1 agonist
Exenatide( short acting) liraglutide(longer acting abiglutide( longer acting) -incretins are GI hormones secreted after a meal that augment insulin release from B cells -GLP-1 is an incretin, GLP-1 agonists are used to treat DM 2 Bind to GLP-1 R in pancreatinc B cells and increase insulin synthesis and secretion in glucose dependent manner - delay gastric emptying and decrease apatite - decrease the release of post prandial glucagon( mech unknown)
45
ARBs, Angiotensin II receptor blockers
Losartan Valsartan Candesartan-prodrug converted in GI tract provide better treatment of CHF b/c they also block the locally produced AII in the heart and reduce the Hypertrophy from the AII
46
Ceftazidime
third generation Cephalosporins -Parenteral Pseudomonal coverage
47
Diltiazem
Class IV anti arrhythmia drugs, Ca channel blocker - deceases L type Ca channels activity to decrease the slope of phase 0 and 4- slowing conduct velocity and automaticity -mainly in the AV node, increase APD and ERP -USE- better at rhythms that must pass the AV node, SVT\>VT, yet good at stopping DADs, reentry SVT and protecting normal Vent rate during aFIB and flutter -IF GIVEN IV MAY MAKE ARRHYTHMIAS WORSE WHEN WPW W/ A FIB -iv and oral, met in liver( careful w/ liver disfunction) -TOX- decreased normal sinus rate and AV conduction, negative intrepid effect, avoid combo w/ B Blockers
48
Cefuroxime oral Cefuroxime IV
second generation Cephalosporins -sinusitis, otitis media bugs(S. pnumo, Hflu, moraxella, s. pyogenes) -useful in CAP- H Flu, S. pneumo, K pneumo)
49
thiazolidinediones uses
treatment of DM type 2 taken once a day -Nuclear receptor agonist so they take time before you se any affect, 1-3 months -monotherapy or conjunction w/ metformin, sulfonylureas, or insulin
50
Ace inhibitors drugs
"..PRIL"
Captopril
enalapril- prodrug activated to enalaprilat
lisinipril
fosinipril- prodrug, good when used in renal insufficiency pt
quinapril-prodrug
ramipril-prodrug
51
amoxcillin
extended spectrum penicillins better oral absorption\
- food doesn't interfere with abs -suseptible to B-lactamase enzymes produced by G+and G- BUGs so paired with B lactamase inhibitors- clavulanate+ amoxcillin=augmentin
- HELPSS ME spectrum of action
- amox causes less diarrhea than ampicillin, decrease effectiveness w/ real contraceptive
- amox and ampicillin can cause non allergic skin rash-1-28 days later
52
cefazolin
first generation Cephalosporins-parenteral
- drug of choice for pre surgery prophylaxis
- alternate for staph and strep in pts w/penicillin allergy
- sensative to B lactamase
53
bisprolol
B blocker
54
Glucagon
emergency treatment of severe hypoglycemia via sim of breakdown of hepatic glycogen stores
- treatment of overdose of B-adrenoreceptor blocker
- binds G protein coupled Receptors-\> stim adenylate cyclase--\> increased cAMP
- stim gluconeogenesis and ketogenesis
SE- transient NV, intropic effect--\> transient tachycardia and HTN
55
toxic effects of tetracyclines
- GI side effects-NV
- superinfections- via disrupting normal flora from candidia or drug resistant BActeria, ex: C dif
- bones and teeth- binds to calcium and complex deposited in teeth and bone-\> yellow teeth and bone deformity, dont use in preg and children under 8
- renal tubular acidosis and damage
- light sensativity
56
Cefprozi
second generation -sinusitis, otitis media bugs(S. pnumo, Hflu, moraxella, s. pyogenes)
57
NITROPRUSSIDE
antianginal agent only given IV
- PRIAMARY PREOAD and afterload REDUCTION IN CHF
- decreases peripheral resistance and thus preload( low doses and Afterload(higher doses)
- decreases O2 demand of cardiac cells by decreasing cell tension
58
ACE inhibitors actions
inhibits ACE-\> decreased AII in the blood and a reduced vaso constrict effect and reduced aldosterone-\> decreased preload and afterload
- ^CO and decreased pulm and peripheral congestion
- SE- nonproductive cough
- too much reduction in arterial BP may occur when in combination use with other antihypertensives or diuretics
- reduce AII production in the heart that contributes to hypertrophy in CHF
59
dopamine
B1 adrenergic agonist -endogenous catecholamine only given IV for severe, refractory CHF -causes increased cardiac output mainly by increased ventricular B1 R action ( positive intrepid effect, increases HR and O2 demand more than dobutamine -low to intermediate dose can increase renal Blood flow -\> increased Na and H20 excretion -tolerance can develop - out of favor b/c of side effects( tach, ^ O2 demand and arrhythmia)
60
clarithromycin
azithromycin
telithromycin
macrolide antibiotics that bind to and inhibit the 50S subunit in bacterial, different side groups give each different activity
-be sure to look this stuff up dummy
61
Meglitinides
insulin secretagogues, REPAGLINIDE, nateglinide MOA-require functioning Beta cells--\> only intreating early Type 2 diabetes,
- Bind to K ATP channel on B cells and inhibit their activity causing depolarization-\> influx of calcium-\> insulin release
- quickly absorbed, highly bound, met in liver -Hypoglycemia( less frequent w/ nateglinide)
- contra- hepatic impairment, renal insufficiency USE- DM type 2, quicker acting so more preprandial dosing can be used in sulfer allergies, mono therapy or w/ metformin
62
Amiodarone
Class III anti arrhythmia drugs
- inhibit the outflowing K channel and prolong the repolarization, causing longer APD and ERP does show some class 1, 2 and 4 activity, can cause TdP SE
- decrease conduct velocity via decreased cell-cell coupling
- USE-severe and refractory SVT and VT, also decreases amount of time ICD must fire, LIMITED by toxicities
- IV and incomplete oral ABS, concentrated in tissues w/ long half life( weeks), long time to make effect, similar structure to thyroxine
- TOX- interstitial pulm fibrosis, dizzy, hyper or hypothyroid, blue skin discoloration(I in skin), TdP
63
Cefaclor
second generation Cephalosporins
- sinusitis, otitis media bugs(S. pnumo, Hflu, moraxella, s. pyogenes)
- B lactamase sensative
64
rosiglitazone
increase insulin sensitivity in target tissues -PPARgamma agonists - increased sensitivity to insulin stimulate uptake of glossy and fatty acids, alters adipokine production - increased sensitivity in liver and muscle too -long term lower Triglyceride and slight increase HDL and LDL -highly bound, long t1/2 and met in liver -SE-weight gain and edema(most important) osteoporosis and fracture in women, increased risk of CHF, contra- preg, hepatic inpairment( freq LFT needed), heart failure -treatment of DM type 2 -taken once a day -Nuclear receptor agonist so they take time before you se any affect, 1-3 months -monotherapy or conjunction w/ metformin, sulfonylureas, or insulin
65
isosorbide dinitrate
antianginal agent
- PRIAMARY PREOAD REDUCTION IN CHF
- decreases peripheral resistance and thus preload( low doses and Afterload(higher doses)
- decreases O2 demand of cardiac cells by decreasing cell tension
- long term therapy an lead to tolerance
66
Penicillin G Benzathine
- provide slow release from the injection area allowing low persistent concentration of the drugs
- IM in gluteus maximus -1.2 mil units = 26 day activity
- has local anesthetic efffecs
- Strep pharengitis, prophylaxis for Reumatic fever, syphillis -
67
SLGT2 inhibitors
Canagliflozin and other .."gliflozin -inhibits glucose reabs in the proximal tubule -\> decrease blood glucose and increase Glucose in urine - High oral availability, peak at 1-2 hours T1/2=10-13 -SE- Genital mycotic infections, UTI, diuretic effect, CANAgliflozin increases serum digoxin, dapagliflozin increased risk of bladder cancer contra- sever renal impairment USE- mono and adjunct therapy for Dm2, 1x/day before first meal
68
Inamrinone
Phosphodiesterase inhibitor
- non-glycoside , non- catecholamine positive intrepid drug, a bipyrine
- USE- IV only for treatment of severe refractory CHF or after tolerance to other B agonists develops
- MOA-Phosphodiesterase inihibitor-\> increased cAMP-\>increased free Ca availability for contractual proteins in systole
- also improves relaxation via more Ca uptake during diastole - little tolerance develops peripheral vasodilator actions
- tox-THROMBOCYTOPENIA, increased O2 demand( can be fatal in ischemic heart disease
69
cephalexin
first generation Cephalosporins- oral -for UTI, minor staph, minor polymicrob lesion
70
Dobutamine
B1 adrenergic agonist -synthetic catecholamine only given IV for severe, refractory CHF -causes increased cardiac output mainly by increased ventricular B1 R action ( positive intropic effect -SE- can cause some tach and increase cardiac O2 demand and arrhythmia ( not as much as other B agonists) - tolerance can develop to to down reg of B1 Receptors
71
Augmentin
Amoxcillin plus clavulanic acid
USE- Resp tract infections- otitis media and sinusitis, UTI-e coli, klebsiella, enterobacter, skin/skin structures- human and animal bites, gonorrhea
72
Flecainide
Class 1C anti arrhythmic drugs
- interacts more slowly w/ phase 0 Na channels more than other class 1 drugs
- marked depression of phase 0 slope in Na dependent myocardial fibers
- inhibits some K channels and also blocks late opening Na channel-\> no net effect on action potential duration or ERP
- increases threshold for phase 0
- USE- reserved for severe arrthymia resistant to other drugs -well absorbed, minimal biotransformation
- SE-negative intrepid effects aggravate CHF,, dizzy nausea, headache, blurry vision, aggravate arrhythmias/ induce Vtach aggravated by hyper K
73
Penicillin G Procaine
- provide slow release from the injection area allowing low persistent concentration of the drugs
- IM in gluteus maximus -600,000 units = several day activity
- has local anesthetic efffecs S. pyogenes (GAS)
- SE- bad taste, dizzy palpation, auditory/visual disturbance
74
metoprolol
B blocker
75
Tolvaptan
Vasopressin antagonist V-2 receptor antagonist for oral treatment of hyponatremia from increased vasopressin activity
- no reduction in mortality in CHF pt
- useful intreating SIADH
76
tetracycline
broad spectrum bacteriostatic agent to inhibit protein synthesis by binding to the 30S subunit of ribosomes, and blocking amino acyl T-RNA to Bind and add AA
- excreted via renal filter(10-50%), in bile
- resistance- increased efflux pumps, Tet(AE) conver resistance to G- to tetra, doxy and minocycline, production of protein to prevent binding to 30S tet(M) ,enzymatic inactivation
- USE-not 1st choice for G+, G- aerobes, or anaerobes
- drugs of choice for- spirochetes(Lyme Ds), clamidia, Rickettsiae(RMSF)(DOXY), Mycoplasm pneumo, brucella, H pylori, peridontitis
77
Ticarcillin + Clavulanate potassium
carboxypenicillin -Antipseudomonal Penicillins
- ticarcillin is B-lastamase sensative so adm w/ clavulanate K
- better anti pseudomonal than older drugs, extended spectrum for infection by G- aerobic rods, and mixed aerobic/anaerobic infections
- tox-excess Na in dosage forms, can prolong bleeding time
78
first generation Cephalosporins
cefazolin- parenteral
cephalexin-oral
poor entry to CNS- not 4 meningitis
- good for G+ and modest for some G-, -G+ except MRSA and S. epidermis,enterococci, PECK(G- enterics), oral cavity anaerobs( except b fragilis)
- cefazolin drug of choice for pre surgery prophylaxis
- alternate for staph and strep in pts w/penicillin allergy oral form--for UTI, minor staph, minor polymicrob lesion,
- B lactamase sensative
79
sitagliptin
DPP-4 inhibitors, prodrug metabolize by CYP3A4/5 -DPP-4 is an enzyme that degrades incretin hormones, taken 1x/day -increase the circulating levels of GLP-1 and GIP thus increasing post prandial insulin and decreased glucagon level -other drugs- saxagliptin, linagliptin, alogliptin -high oral availability, inhibit DPP-4 for 12 hours -saxagliptin is a prodrug SE- increased rate of infection, headache, hypoglycemia when given with other drugs, pancreatitis, hypersensitivity run - reduce dose with CYP3A4/5 inhibitors use-mono/combination therapy for DM2
80
Adenosine
class IV anti arrhythmia drug
- decreases conduct velocity and decreases abnormal impulse formation in the AV node via inhibit Ca influx by activating ACh sensitive phase 4 K current( cause hyper polarization) prolongues AV node refractory period
- USE\_ drug of choice for PSVT of AV and WPW origin
- low TOX,- apprehension, fear of doom, sob , flushing, and chest pain - 15s duration of action
81
Pramlitide
Amylin Analogue -MOA- acts in hindbrain to suppress glucagon, delay gastric emptying, and promote satiety - SUB Q injection, not high bound and excrete in kidney SE- hypoglycemia, Nausea, weight loss contra- gastroparesis or GI motility disorders -USE- treatment of DM 1 and 2 as an adjunct to insulin, preprandial injection separate from insulin, mealtime glucose can be reduced by 50 %
82
fourth generation Cephalosporins
Cefepime-Parenteral
extend spectrum conpaired to third gen -Plasmid and chromosomal B lactamamse resistant
--UTI, skin/soft tissue, pneumo, complicated intra AB
- treat G- bugs resistant to 3rd gen- pseudomonas/ some enterobacteriaceae
- use-more useful in enterobacter, Penicillin resistant Strep
- penetrates CNS well to treat meningitis
83
Aztreonam
monobactam b/c only has monocyclic bantam ring
- highly resistant to B lactase produced by G- bac, poor orally, parenteral, excrete renally, t.5=1-2hr
- only effective against G- rods,
- use- in G- infections w/ pt w/ history of B lactam sensitivity, if G+ also present another ABX NEEDS TO BE ADDED
- renal excretion and dose adjustment for renal impairment
84
Quinidine
Class 1A anti arrhythmic drugs
- blocks Na channels to decrease slope of phase 0 and blocks K channels to prolonge Action potential duration and Effective refractory period
- USE-limited by side effects, maintain normal rhythm after A fib(Less now in USA), V fib of brugada syndrome, A fib of pts w/short QT
- IV and oral forms
- SE-other arrhythmias TdP due to prolonged QT, nausea vomit, Dhrea, alpha blocking action and atropine like effect -\> decreased BP and ^ sinus rate, ^ digoxin levels
85
milrinone
Phosphodiesterase inhibitor
- non-glycoside , non- catecholamine positive intrepid drug, a bipyrine
- USE- IV only for treatment of severe refractory CHF or after tolerance to other B agonists develops
- MOA-Phosphodiesterase inihibitor-\> increased cAMP-\>increased free Ca availability for contractual proteins in systole - also improves relaxation via more Ca uptake during diastole
- little tolerance develops peripheral vasodilator actions
- tox-increased O2 demand( can be fatal in ischemic heart disease
86
Penicillin G
natural penicillin, oral arm only 33% absorbed gastric acid destroys this and food interferes w/ abs, K and Na salts of Penicillin G given for parenteral use
- adm w/ aminoglycosides to enhance effect, probenecid increases plasma levels
- effective for G+ and G- aerobic cocci, most sprocetes, some G+ aerobic and anaerobic bacilli non resistent Staph and strep
- sensative staph and strep, pneumococal pneumo( use macrolide until sensative test), pneumococal meningitis, strep thraot, spirochete - syphillis, actinomyces israelii
add more drugs from p13
87
Verampamil
Class IV anti arrhythmia drugs, Ca channel blocker - deceases L type Ca channels activity to decrease the slope of phase 0 and 4- slowing conduct velocity and automaticity
- mainly in the AV node, increase APD and ERP
- USE- better at rhythms that must pass the AV node, SVT\>VT, yet good at stopping DADs, reentry SVT and protecting normal Vent rate during aFIB and flutter
- IF GIVEN IV MAY MAKE ARRHYTHMIAS WORSE WHEN WPW W/ A FIB
- iv and oral, met in liver( careful w/ liver disfunction)
- TOX- decreased normal sinus rate and AV conduction, negative intrepid effect, avoid combo w/ B Blockers
88
Liraglutide
GLP-1 agonist once per day sub Q -slowly absorbed after injection and peak action in 8-12 hours after injection, highly bound to plasma proteins -Bind to GLP-1 R in pancreatinc B cells and increase insulin synthesis and secretion in glucose dependent manner - delay gastric emptying and decrease apatite - decrease the release of post prandial glucagon( mech unknown) -antagonize glucagon and increase affect of insulin -SE- GI disturbance, nausea at start of therapy, weight loss, hypo glycemic when combined w. sulfonylurea, pancreatitis( rare but serious), delay in gastric empty can alter other drugs contra- pancreatitis history, black box warning for pts w/ history of medullary cancer, caused thyroid cancer in rodents USE- mono or combination therapy for DM2
89
Conivaptan
Vasopressin antagonist V-1a and V-2 receptor antagonist for IV treatment of hyponatremia from increased vasopressin activity
- no reduction in mortality in CHF pt
- useful intreating SIADH
90
pioglitazone
increase insulin sensitivity in target tissues -PPARgamma agonists - increased sensitivity to insulin stimulate uptake of glossy and fatty acids, alters adipokine production - increased sensitivity in liver and muscle too -long term lower Triglyceride and slight increase HDL and LDL -highly bound, long t1/2 and met in liver -SE-weight gain and edema(most important) osteoporosis and fracture in women, increased risk of CHF, contra- preg, hepatic inpairment( freq LFT needed), heart failure -treatment of DM type 2 -taken once a day -Nuclear receptor agonist so they take time before you se any affect, 1-3 months -monotherapy or conjunction w/ metformin, sulfonylureas, or insulin
91
Sulfonylureas
insulin secretagogues -Glyburude, glipizide, glimepiride -require functioning Beta cells--\> only intreating early Type 2 diabetes -Bind to K ATP channel on B cells and inhibit their activity causing depolarization-\> influx of calcium-\> insulin release -highly bound, metabolized in liver and secreted in urine -SE- HYpoglycemia, Weight gain, sulfur allergy -contra- hepatic impairment, renal insufficiency, pregnant and brest feeding -clinical use- type 2DM, BID, lose efficacy as B cell function decreases, and can be combined w/ metformin and thiazolidinediones
92
propanolol
Class II anti arrhythmia drugs
-B1 and B2 selective blocker good to reduce incidence of adrenergically driven arrhythmic death after MI
diminish phase 4 depolarization, depressing automaticity, especially in nodal tissues
- treat arrhythms cause by too much symp activity
- careful in use w/ Ca channel blockers b/c together can too much depress normal cardiac function
\_membrane stabilizing property can inhibit some arrhythmias but at higher doses therefor risk of side effects
- no partial agonist
- Membrane stabilize
- High Lipid soluble
93
Tigecycline
derative of minocycline
- Parenteral adm, T1/2 of 36 hours, eliminated via non renal mech-\> no dose adjust in renal disease
- binds to 30S subunit to inhibit bacterial protein production, but not pumped out by Tet(AE) or Tet(K)-\> useful in tetracycline resistant bacteria( except proteus and pseudomonas), not inhibited by TET(M) protein( prevents binding to 30s of other tetras
- USE-against MRSA, B lactamase producing G- and Acinetobcater, used in skin/skin structure and abdominal infections
94
Cefotaxime
third generation Cephalosporins-Parenteral
95
extended spectrum penicillins
Ampicillin amoxicillin, great er action on G- than pen G
- suseptible to B-lactamase enzymes produced by G+and G- BUGs so paired with B lactamase inhibitors- clavulanate
- greater activity to non B-lactamase producing G+ and G- bugb/c they better penetrate the membrane
- HELPSS ME spectrum of action
- same tox as Penicillin G
- amox causes less diarrhea than ampicillin, decrease effectiveness w/ oral contraceptives
96
second generation Cephalosporins
Cefaclor oral-more type 3 hypersense- serum sickness, good sinusitis/OM
Cefoxitin -parenteral
Cefuroxime oral
Cefuroxime IV- cvr s. pneumom and sinusitis/otitis media
Cefprozi oral
poor entry to CNS( except cefuroxime),not 4 meningitis, some treat b fragilis
- less G+ activity but more G- than 1st gen-(h flu Moraxella)
- No pseudomonas activity, DONT USE w/ enterobacter( makes Chromosoaml B lactamase)
97
Adverse effects of penicillins
- hypersensitivity rxn, .7-8%, 2nd only to blood products to allergic rxns in hospital patients
- major allergic determinants are breakdown products ex: Benzylpenicilloyl
- minor determinants: penicillinitself and other breakdown products
- Anti Penicillin ABs are present in most persons, adults more suseptible than children
- oral adm is less sensitizing than parenteral, topical is worst - cross sensitizing and cross allergic, direct proportion to the duration of treatment and total doses received
type2-cytotoxin( hemolytic anemia), type 3( IC mediated, type4 CMI- delayed( methicillin most common- allergic interstitial nephritis- T4)
98
type 1 Hypersensitivity to penacillins
- most common, IgE mediated, release of histamine from mast cells, 1 -72 hours post adm, skin testing most useful
- Skin reactions ‐ Rash, Angioedema (swelling of lips, tongue, face), urticaria, pruritis
- GI Manifestations – Nausea, abdominal pain, vomiting, and diarrhea
- Respiratory tract involvement – dyspnea or wheezing
- Cardiovascular manifestations – hypotension, tachycardia, and arrythmias
- Fatality is usually due to laryngeal edema or cardiovascular collapse
99
Acarbose
alpha glucosidase inhibitor -competitive inhibitor of enteric a-glucosidase( enzyme that breaks down complex carbs and oligosaccharides) -delay post prandial abs of gluscose -attenuates plasma glucose increases post prandial-\> insulin sparing effect -SE- GI disturbance(fart, drhea, ab pain) -contra- IBS, any condition worsened by gas - USE- type 2 DM, prior to each meal, mono therapy or with other meddler insulin -in mild to mod hypoglycemia pts should be given dextrose not sucrose
100
Class IV anti arrhythmia drugs
Verapamil
Diltiazem
block Votage sensative L type Ca channels
decrease inward current carried by calcium
