exam 5 drugs Flashcards
1
Q
open angle glaucoma tx
A
-PG analogs (-oprost) +
-B-blockers (-olol) -
-a2 (-inidine) +-
-carbonic anhydrqase inhibitors (-zolamide) -
-rho kinase inhibitors (netarsudil) +
-cholinergics (carbachol and pilocarpine) +
2
Q
Apoliproteins
A
-ApoA: HDL, reverse cholesterol transport
-ApoB: 100 VLDL-LDL, 48 chylomicron
-ApoE: reverse choleserol transport w HDL
-ApoCII: TG hydrolysis
3
Q
lipid transport
A
-EXO: chylomicrons + LPL from intestine
-ENDO: VLDL from liver to IDL (ApoE) then LDL (ApoB)
4
Q
Hepatic lipase
A
-IDL to LDL
5
Q
Hyperlipoproteinemia
A
-artheroclerosisi
-CAD
-stroke
6
Q
HyperTG
A
-panreatitis
-xanthomas
-inc CHD risk
7
Q
Artherosclerosis
A
-macrophages
-smooth muscle cells from injury
=foam cells
-oxidized LDL attract more macrophages
-ACAT1 esters cholesterol in macrophage
-CEH: frees cholesterol to ApoA1 or HDL
8
Q
HoFH tx
A
-LDLR reduced
-lomitapide (juxtapid) (apoB)
-mipomersen (apoB)
-Evinacumab-dgnb (ANGPTL3)
9
Q
juxtapid (lomitapide)
A
-inhibits ApoB lipoproteins in liver and intestine
-chylomicrons and VLDL-LDL
-restricted rx (liver)
10
Q
Mipomersen
A
-anti-sense
-ApoB100 in liver inhibited
-SQ qweek
-restricted rx (hepatic steatosis)
11
Q
Evinacumab-dgnd
A
-IV qmonth
-inc LPL and E(lipase_ by inhibiting ANDPTL
-gets rid of IDL before it turns into LDL
12
Q
Hyper TG tx
A
-fibrates
-niacin
-omega-3
13
Q
Fibric acid derivatives
A
-PPARa (transcription factor_
-aromatic ring-o-spacer grp-carbox
14
Q
Niacin
A
-inc LPL to get rid of VLDL
-dec hepatic VLDL production (dec TG transport_
-dec FFA release (DGAT2) and transport to liver (GPR109A)
-dec CE content in macrophages by inc ABCA1 expression = HDL uptake
15
Q
nonHDL-C=
A
TC-HDL
16
Q
LDL=
A
TC-HDL -TG/5
-not valid when TGs >400
17
Q
TC/HDL goal
A
<5:1
18
Q
lifestyle changes dyslipidemia
A
-olestra
-soluble fiber
-plant stenols and sterols
-weight/exercise
-smoking cessation
19
Q
omega-3
A
-reduce TG
-lovaza 2-4g qd or BID
-Vascepa 2g BID wf (IPE)
-caution AFIB
20
Q
Statin high intensity
A
-atorvastatin 40-80mg
-rosuvastatin 20-40mg
21
Q
Lipophillic statins
A
-fluva
-pitava
-lova
-simva
-atorva
-more likely for muscle pain
22
Q
Hydrophillic
A
-pravastatin
-rosuvastatin
-inc liver toxicity
23
Q
A
24
Q
statins and muscle injury
A
-if CYP3A4 watch interactions, try CoQ10 before starting statin again
-switch hydrophillic
-consider alt dosing
25
simvastatin contraindications
-conazoles
-thromycins
-HIV protease inhibitors
-gemfibrozil
-cyclosporin
-danazol
-verapamil and siltiazem at 10mg
-amlodipine at 20mg
26
Bile Acid Resins
-cholestyramine (Questran)
-colestipol (colestid)
-colesevelam (welChol)
-space apart other meds
-may inc TG
-GI effects
-interfere w fat-soluble ADEK
-hypernatremia and CL
-gi obstruction
27
BAR contraindications
-bilary obstruction (cholestyramine)
-hx bowel obstruction
-TG>500
-pancreatitis
28
BAR interactions
-acetaminophen
-TZDs
-warfarin
-digozin
-contraceptives
-steroids
-ezetimibe
-fibrates
29
Niacin flushing tx
-take ASA 325mg 30 min before
-close to meal
-avoid alc and hot drinks
-titrate up
30
Niacin probs
-hyperuricemia
-hyperglycemia
-inc LFTs
-inc levels of statins
31
Niacin contraindications
-hepatic disease
-peptic ulcer
-arterial hemorrhage
32
Ezetimibe
-combo w statin
-inhibit intestinal absorption
-block NPC1L1
-fatigue and GI upset
33
Fibrate probs
-GI, rash, myalgia, dizziness
-gallbladder, ESRD, liver disease
-inc levels of statins, sulfonylureas, warfarin
34
PCSK9 for
-ASCVD on max statin
-high risk and statin intolerant
-LDL>190 on max statin
35
Inclisiran
-similar to PCSK9 but dosed 2x year
36
Bempedoic acid
-works upstream of statin
-may lead to GOUT
-prob not gonna use
-dont use w simva or prava
37
red yeast rice active ingredient
-lovastatin
38
high intensity statin
-when LDL >190
-risk assess in DM and over 75y/o
-secondary prevention
39
nonstatin tx guidelines
1. ezetimibe
2. PCSK9 inhibitors
other: BAS
40
LDL goals
<100 primary
<70 secondary
41
tx HyperTG
-statin
-fibrate*
-omega-3*
-dec pancreatitis risk
42
Cav1.2
-L-type Ca Channel
-PKA phosphorylation inc contractility and force and AV conduction
43
Ca channel in vasc smooth muscle
-vasodilation (dec BP, relieve angina) when blocked
-EC Ca required to release Ca from RYR2
-myosin LC PO4 + actin =contraction
44
Ca channels in SA/AV node
-antiarrhytmic
-Ca binds troponin C
=tropomysin displace
=actin binding
=contraction
45
CCB classes
-dihydropyridines (-odipine)
-phenylalkylyamine (verapamil)
-benzothiazepines (diltiazem)
46
DHPs
-ring w N
-clevidipine short acting give IV when PO not possible
-(+) blocks current, interferes opening
-(-) potentiates current, interferes closing
-not antiarrhytmic
-TONIC BLOCK (FREQ DEPENDENT)
-vasodilation
-dec afterload
-little effect on CO (may inc HR)
-nimodipine used for hemorrhage
-relex tachycardia except amlodipine
-dec o2 need (angina)
-liver metabolism
-amlodipine slow onset long duration
-nifedipine MI
47
Verapamil
-CCB
-phenylalkylamine
-less potent vasodilator
-DEC HR and force (slows conduction)
-little reflec tachycardia
-Freq dependent
-constipation
48
Diltiazem
-vasodilation and slows conduction
-initial reflex tachycardia
-inhibits heart less than verapamil
-some tonic block some freq dependence
-ankle edema
-flushing
-tachycardia
49
Vasodilators
-cyclic GMP modulators
-K agonists
-Endothelin antagonists
-PGI analogs
50
K channel openers
-minoxidil
-diazoxide
-adenosine
-equilibrium makes Ca channels harder to open
51
minoxidil
-K opener
-prodrug 1A1
-use w loop and B-blocker
-resistant HTN
-cAMP PDE inhibition
52
Diazoxide
-K opener
-IV for resistant HTN
-inhibits insulin release
-used orally for hypoglycemia due to hyperinsulinemia
53
Adenosine
-inc conduction of K channel
-A1 receptor GPCR
-IV coronary stress test and arrhytmia
-hyperpolarization when binding GIRK
54
Nitric Oxide synthase
-activated by Ca-CAM
-NO binds guanylate cyclase in smooth muscle = protein kinase G (cGKI activation)
-relax smooth muscle
55
Protein kinase G
-inhibit Cav1.2
-stimulate k channels (BKca)
-myosin phosphatase 1
-enhance Ca uptake in ER (phospholamban)
56
organic nitrates
-nonselective
-prodrugs (breakdown to NO)
-(-nitrate except nitroprusside and hydralazine)
-give sublingually in acute angina attacks
-tolerance
-glycerol trinitrate (GTN) doesnt work well in asians bc Glu504
-activation ALDH-2 independent
-activators: xanthine, glutathione, ALDH
-nitroprusside vasodilator
-give IV for HTN crisis
-metabolized by erythroxytes = limited duration
-hydralazine vasodilator intereferes w Ca release, lupus syndrome
-combo w ISDN in BiDil=dec mortality inn black pt
57
Natriuretic peptide (BNP)
-vasodilator
-activates guanylate cyclase
-cleaved by neprilysin
58
Sacubitril
-inhibts neprilysin
-combo w ARB
-prevent breakdown of BNP = inc action
-not used w ACEi
-tx HF
59
PDE inhibtors
-inhibit breakdown of cGMP and AMP
-PED3 (cAMP) (amrinone and milrinone)
-PDE5 (cGMP) (dipyridamole and -afils)
60
amrinone/milrinone
-give IV
-PDE3
-cAMP
-CHF
61
PDE5
-cGMP
-bluish vision
-not very systemic
-levitra shorter onset
-cialis longer duratoin
-DO NOT USE W ORgANIC NITRATES accumulation of cGMP and maybe cAMP
62
Vasoconstrictor (endothelin) antagonists
-(-entan)
-Bosentan
-Macitentan
-Ambrisentan (ETa only)
-block ETa and ETB
-PAH
-AVOID in preg and hepatotoxicity
63
Prostacyclin analogs
-PGI2
-treprostinil
-iloprost
-selexipag
-PAH
64
Riociguat
-PAH
-activate sGC
-inc cGMP in smooth musc
-substrate for P-gp, CYP1A1, 3A
65
Sotatercept-CSRK
-binds/neutralizes activin
-PAH
-reduce proliferation of smooth muscle cells
-reduces resistance
-erythrocytosis, thrombocytopenia, bleeding, infertility
66
Substances that can inc BP
-illicit drugs
-caffeine, nicotine
-decongestants
-amphetamines
-antidepressants/psychotics
-immunosuppressants
-contraceptices NSAIDs
-steroids
67
Masked HTN
-no HTN in office
-HTN at home
68
white coat HTN
-HTN in office not at home
69
BP classification
normal: <120/80
elevated:120-129/80
stage 1: 130-139/80-89
-stage 2: >140/90
70
elevated BP tx
-non pharma reassess 3-6months
71
Stage 1 HTN tx
-pharma if ASCVD >10%, reassess 1 month
72
stage 2 HTN
-2 meds
-reasses 1 month
73
BP goals
-<130/80. if not old
74
Pharma options for HTN
-ACEi
-ARBs
-CCBs
-diuretics
-a1 blockers
-a2 agonists
-B-blockers
-vasodilators
75
First-line HTN tx
1. thiazides
-ACE/ARB or CCB
-most need more than one anyway
76
HTN tx in stable ischemic HD
-B-blockers
-ACEi/ARBs
-add dihydropyridine CCBs if needed
77
HTN tx HF
-HFrEF: ANRI + B-blocker + MRA + SGLT2 (can add loop but avoid CCBs)
-HFpEF: SGLT2 (can add loop, MRA, ARB)
78
CKD HTN tx
-ACEi/ARBs if stage 1/2 w albuinuria or stage 3+
-CCBs after kidney transplant
79
HTN tx CVD (secondary stroke prevention
-ACEi/ARBs
-TZD
-combo
-dont initiate until 140/90
80
HTN tx diabetes
-tx like normal
-ACEi or ARB if albuminuria
81
HTN tx pregnancy
-methyldpoa
-nifedipine
-labetalol
-AVOID ACEi/ARBs and renin inhibitors
82
HTN tx in race
-TZD or CCB in black pt w/o HF or CKD
83
Diuretics for HTN tx
-TZDS
-loop (furosemide)
-MRA (spirinolactone)
-potassium sparing
84
TZDs
-HCTZ, chlorthalidone, indapamide, metolazone
-first-line for most HTN pt
-better than loop at >30ml/min
85
TZD cautions
-HYPO- K,Mg, Ca
-HYPERuricemia, glycemia, lipidemia, sexual dysfunction
-toxicity w lithium
-sulfa allergy
86
Loop diuretics for HTN
-preferred in HF
-more effective than TZDs at CrCL<30ml/min
-hypoK,Mg,Ca
-hyperuricemia
-ototoxicity
-sulfa allergy
87
MRAs
-spirinolactone for resistant HTN
-watch potassium
-inc risk of hyperkalemia w ACEi/ARBs/renin.NSAIDs
-AVOID eplerenone in T2DM
88
ACEi
-opril
-good for DM, post MI, CKD
-angioedema
-cough
-hyperkalemia
-renal failure
-AVOID in hx of angioedema, aliskiren use in DM pt, preg
89
ARBs
-osartans
-back up if ACEi not tolerated
-less cough (no blocking bradykinin breakdown)
-angioedema, hyperkalemia, renal failure
-ACVOID in hx of angioedema, aliskiren in DM, preg/breastfeeding
90
CCBs for HTN
-DHPs more vasodilation
-good for reynaud and elderly pt
-avoid short aciting
-dipines
-reflex tachycardia, flushing, diziness, HA, edema
-inc risk of angina/MI in pt w obstructive CAD
-avoid CYP3A4
-NON-DHPs (diltiazem and verapamil) good for AFIB and pt w angina that cant take beta blocker
-bradycardia
-avoid CYP3A4 and B-blockers
-contraindications: heart block, left ventricular dysfunction
91
B-blockers for HTN
-not first line unless HF and CAD
-dec CO
-avoid abrupt cessation
-cardioselective: atenolol, metoprolol, beta, biso, nebiv
-nonselective: nadolol and propranolol (avoid in COPD)
-ISA: acebutolol, penbutolol, pindolol
-mixed:carvedilol, labetalol
-bronchospasm, bradycardia, fatigue
-can mask hypoglycemia
-carvedilol for PAH
-AVOID in heart block, post MI, severe bradycardia
92
Direct arterial vasodilators
-hydralazine and minoxidil
-last line for resistant HTN
-gove minoxidil w diuretic AND B-blocker
93
a1 blockers
-azosins
-not using
-reflex tachycardia, renin release
-vasodilator
94
a2 agonists
-clonidine
-methyldopa
-guanfacine
-CNS effects
-avoid abrupt cessation (rebound HTN)
-dec HR, contractility, renin
95
Resistant HTN tx
-max lifestyle and drugs
-substitute optimized TZA (chlorthalidone, indapamide)
-add MRA
-add BB if HR >70, consider a2 (clonidine)
-add hydralazine
-sub hydralazine for minoxidil
96
nonselective BB
-propranolol
-nadolol
-timolol
-dec CO and HR
-reduce renin release
97
ISA activity
-Pindolol
-carteolol
-less likely for bradycardia
98
Selctive B1
-metaprolol
-bisoprolol
-atenolol
-esmolol
-nebivolol 3rd gen NO
99
mixed a1 and B
-carvedilol
-labetolol
100
CYP3A4 statin
101
102
