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Therapeutics II > exam 5 drugs > Flashcards

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) +

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2
Q

Apoliproteins

A

-ApoA: HDL, reverse cholesterol transport
-ApoB: 100 VLDL-LDL, 48 chylomicron
-ApoE: reverse choleserol transport w HDL
-ApoCII: TG hydrolysis

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3
Q

lipid transport

A

-EXO: chylomicrons + LPL from intestine
-ENDO: VLDL from liver to IDL (ApoE) then LDL (ApoB)

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4
Q

Hepatic lipase

A

-IDL to LDL

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5
Q

Hyperlipoproteinemia

A

-artheroclerosisi
-CAD
-stroke

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6
Q

HyperTG

A

-panreatitis
-xanthomas
-inc CHD risk

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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

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8
Q

HoFH tx

A

-LDLR reduced
-lomitapide (juxtapid) (apoB)
-mipomersen (apoB)
-Evinacumab-dgnb (ANGPTL3)

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9
Q

juxtapid (lomitapide)

A

-inhibits ApoB lipoproteins in liver and intestine
-chylomicrons and VLDL-LDL
-restricted rx (liver)

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10
Q

Mipomersen

A

-anti-sense
-ApoB100 in liver inhibited
-SQ qweek
-restricted rx (hepatic steatosis)

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11
Q

Evinacumab-dgnd

A

-IV qmonth
-inc LPL and E(lipase_ by inhibiting ANDPTL
-gets rid of IDL before it turns into LDL

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12
Q

Hyper TG tx

A

-fibrates
-niacin
-omega-3

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13
Q

Fibric acid derivatives

A

-PPARa (transcription factor_
-aromatic ring-o-spacer grp-carbox

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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

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15
Q

nonHDL-C=

A

TC-HDL

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16
Q

LDL=

A

TC-HDL -TG/5

-not valid when TGs >400

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17
Q

TC/HDL goal

A

<5:1

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18
Q

lifestyle changes dyslipidemia

A

-olestra
-soluble fiber
-plant stenols and sterols
-weight/exercise
-smoking cessation

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19
Q

omega-3

A

-reduce TG
-lovaza 2-4g qd or BID
-Vascepa 2g BID wf (IPE)
-caution AFIB

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20
Q

Statin high intensity

A

-atorvastatin 40-80mg
-rosuvastatin 20-40mg

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21
Q

Lipophillic statins

A

-fluva
-pitava
-lova
-simva
-atorva

-more likely for muscle pain

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22
Q

Hydrophillic

A

-pravastatin
-rosuvastatin

-inc liver toxicity

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23
Q
A
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24
Q

statins and muscle injury

A

-if CYP3A4 watch interactions, try CoQ10 before starting statin again
-switch hydrophillic
-consider alt dosing

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25
Q

simvastatin contraindications

A

-conazoles
-thromycins
-HIV protease inhibitors
-gemfibrozil
-cyclosporin
-danazol

-verapamil and siltiazem at 10mg
-amlodipine at 20mg

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26
Q

Bile Acid Resins

A

-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

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27
Q

BAR contraindications

A

-bilary obstruction (cholestyramine)
-hx bowel obstruction
-TG>500
-pancreatitis

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28
Q

BAR interactions

A

-acetaminophen
-TZDs
-warfarin
-digozin
-contraceptives
-steroids
-ezetimibe
-fibrates

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29
Q

Niacin flushing tx

A

-take ASA 325mg 30 min before
-close to meal
-avoid alc and hot drinks
-titrate up

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30
Q

Niacin probs

A

-hyperuricemia
-hyperglycemia
-inc LFTs
-inc levels of statins

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31
Q

Niacin contraindications

A

-hepatic disease
-peptic ulcer
-arterial hemorrhage

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32
Q

Ezetimibe

A

-combo w statin
-inhibit intestinal absorption
-block NPC1L1

-fatigue and GI upset

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33
Q

Fibrate probs

A

-GI, rash, myalgia, dizziness
-gallbladder, ESRD, liver disease
-inc levels of statins, sulfonylureas, warfarin

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34
Q

PCSK9 for

A

-ASCVD on max statin
-high risk and statin intolerant
-LDL>190 on max statin

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35
Q

Inclisiran

A

-similar to PCSK9 but dosed 2x year

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36
Q

Bempedoic acid

A

-works upstream of statin
-may lead to GOUT
-prob not gonna use
-dont use w simva or prava

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37
Q

red yeast rice active ingredient

A

-lovastatin

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38
Q

high intensity statin

A

-when LDL >190
-risk assess in DM and over 75y/o
-secondary prevention

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39
Q

nonstatin tx guidelines

A
  1. ezetimibe
  2. PCSK9 inhibitors
    other: BAS
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40
Q

LDL goals

A

<100 primary
<70 secondary

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41
Q

tx HyperTG

A

-statin
-fibrate*
-omega-3*

-dec pancreatitis risk

42
Q

Cav1.2

A

-L-type Ca Channel
-PKA phosphorylation inc contractility and force and AV conduction

43
Q

Ca channel in vasc smooth muscle

A

-vasodilation (dec BP, relieve angina) when blocked
-EC Ca required to release Ca from RYR2
-myosin LC PO4 + actin =contraction

44
Q

Ca channels in SA/AV node

A

-antiarrhytmic
-Ca binds troponin C
=tropomysin displace
=actin binding
=contraction

45
Q

CCB classes

A

-dihydropyridines (-odipine)
-phenylalkylyamine (verapamil)
-benzothiazepines (diltiazem)

46
Q

DHPs

A

-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
Q

Verapamil

A

-CCB
-phenylalkylamine
-less potent vasodilator
-DEC HR and force (slows conduction)
-little reflec tachycardia
-Freq dependent

-constipation

48
Q

Diltiazem

A

-vasodilation and slows conduction
-initial reflex tachycardia
-inhibits heart less than verapamil
-some tonic block some freq dependence

-ankle edema
-flushing
-tachycardia

49
Q

Vasodilators

A

-cyclic GMP modulators
-K agonists
-Endothelin antagonists
-PGI analogs

50
Q

K channel openers

A

-minoxidil
-diazoxide
-adenosine

-equilibrium makes Ca channels harder to open

51
Q

minoxidil

A

-K opener
-prodrug 1A1
-use w loop and B-blocker
-resistant HTN
-cAMP PDE inhibition

52
Q

Diazoxide

A

-K opener
-IV for resistant HTN
-inhibits insulin release
-used orally for hypoglycemia due to hyperinsulinemia

53
Q

Adenosine

A

-inc conduction of K channel
-A1 receptor GPCR
-IV coronary stress test and arrhytmia
-hyperpolarization when binding GIRK

54
Q

Nitric Oxide synthase

A

-activated by Ca-CAM
-NO binds guanylate cyclase in smooth muscle = protein kinase G (cGKI activation)
-relax smooth muscle

55
Q

Protein kinase G

A

-inhibit Cav1.2
-stimulate k channels (BKca)
-myosin phosphatase 1
-enhance Ca uptake in ER (phospholamban)

56
Q

organic nitrates

A

-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
Q

Natriuretic peptide (BNP)

A

-vasodilator
-activates guanylate cyclase
-cleaved by neprilysin

58
Q

Sacubitril

A

-inhibts neprilysin
-combo w ARB
-prevent breakdown of BNP = inc action
-not used w ACEi
-tx HF

59
Q

PDE inhibtors

A

-inhibit breakdown of cGMP and AMP
-PED3 (cAMP) (amrinone and milrinone)
-PDE5 (cGMP) (dipyridamole and -afils)

60
Q

amrinone/milrinone

A

-give IV
-PDE3
-cAMP
-CHF

61
Q

PDE5

A

-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
Q

Vasoconstrictor (endothelin) antagonists

A

-(-entan)
-Bosentan
-Macitentan
-Ambrisentan (ETa only)

-block ETa and ETB
-PAH
-AVOID in preg and hepatotoxicity

63
Q

Prostacyclin analogs

A

-PGI2
-treprostinil
-iloprost
-selexipag
-PAH

64
Q

Riociguat

A

-PAH
-activate sGC
-inc cGMP in smooth musc
-substrate for P-gp, CYP1A1, 3A

65
Q

Sotatercept-CSRK

A

-binds/neutralizes activin
-PAH
-reduce proliferation of smooth muscle cells
-reduces resistance
-erythrocytosis, thrombocytopenia, bleeding, infertility

66
Q

Substances that can inc BP

A

-illicit drugs
-caffeine, nicotine
-decongestants
-amphetamines
-antidepressants/psychotics
-immunosuppressants
-contraceptices NSAIDs
-steroids

67
Q

Masked HTN

A

-no HTN in office
-HTN at home

68
Q

white coat HTN

A

-HTN in office not at home

69
Q

BP classification

A

normal: <120/80
elevated:120-129/80
stage 1: 130-139/80-89
-stage 2: >140/90

70
Q

elevated BP tx

A

-non pharma reassess 3-6months

71
Q

Stage 1 HTN tx

A

-pharma if ASCVD >10%, reassess 1 month

72
Q

stage 2 HTN

A

-2 meds
-reasses 1 month

73
Q

BP goals

A

-<130/80. if not old

74
Q

Pharma options for HTN

A

-ACEi
-ARBs
-CCBs
-diuretics
-a1 blockers
-a2 agonists
-B-blockers
-vasodilators

75
Q

First-line HTN tx

A
  1. thiazides
    -ACE/ARB or CCB
    -most need more than one anyway
76
Q

HTN tx in stable ischemic HD

A

-B-blockers
-ACEi/ARBs
-add dihydropyridine CCBs if needed

77
Q

HTN tx HF

A

-HFrEF: ANRI + B-blocker + MRA + SGLT2 (can add loop but avoid CCBs)
-HFpEF: SGLT2 (can add loop, MRA, ARB)

78
Q

CKD HTN tx

A

-ACEi/ARBs if stage 1/2 w albuinuria or stage 3+

-CCBs after kidney transplant

79
Q

HTN tx CVD (secondary stroke prevention

A

-ACEi/ARBs
-TZD
-combo

-dont initiate until 140/90

80
Q

HTN tx diabetes

A

-tx like normal
-ACEi or ARB if albuminuria

81
Q

HTN tx pregnancy

A

-methyldpoa
-nifedipine
-labetalol

-AVOID ACEi/ARBs and renin inhibitors

82
Q

HTN tx in race

A

-TZD or CCB in black pt w/o HF or CKD

83
Q

Diuretics for HTN tx

A

-TZDS
-loop (furosemide)
-MRA (spirinolactone)
-potassium sparing

84
Q

TZDs

A

-HCTZ, chlorthalidone, indapamide, metolazone
-first-line for most HTN pt
-better than loop at >30ml/min

85
Q

TZD cautions

A

-HYPO- K,Mg, Ca
-HYPERuricemia, glycemia, lipidemia, sexual dysfunction

-toxicity w lithium
-sulfa allergy

86
Q

Loop diuretics for HTN

A

-preferred in HF
-more effective than TZDs at CrCL<30ml/min

-hypoK,Mg,Ca
-hyperuricemia
-ototoxicity

-sulfa allergy

87
Q

MRAs

A

-spirinolactone for resistant HTN
-watch potassium
-inc risk of hyperkalemia w ACEi/ARBs/renin.NSAIDs

-AVOID eplerenone in T2DM

88
Q

ACEi

A

-opril
-good for DM, post MI, CKD

-angioedema
-cough
-hyperkalemia
-renal failure

-AVOID in hx of angioedema, aliskiren use in DM pt, preg

89
Q

ARBs

A

-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
Q

CCBs for HTN

A

-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
Q

B-blockers for HTN

A

-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
Q

Direct arterial vasodilators

A

-hydralazine and minoxidil
-last line for resistant HTN

-gove minoxidil w diuretic AND B-blocker

93
Q

a1 blockers

A

-azosins
-not using
-reflex tachycardia, renin release
-vasodilator

94
Q

a2 agonists

A

-clonidine
-methyldopa
-guanfacine

-CNS effects
-avoid abrupt cessation (rebound HTN)

-dec HR, contractility, renin

95
Q

Resistant HTN tx

A

-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
Q

nonselective BB

A

-propranolol
-nadolol
-timolol

-dec CO and HR
-reduce renin release

97
Q

ISA activity

A

-Pindolol
-carteolol
-less likely for bradycardia

98
Q

Selctive B1

A

-metaprolol
-bisoprolol
-atenolol
-esmolol

-nebivolol 3rd gen NO

99
Q

mixed a1 and B

A

-carvedilol
-labetolol

100
Q

CYP3A4 statin

Therapeutics II (55 decks)

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