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cvs drug lol Flashcards

1
Q

nicotinic acid (niacin)

A

ลด VLDL เป็นหลัก ลดได้ 20-80% in 1-2wks ส่วน LDL ลดได้บ้างๆๆ 10-15% in 3-5wks

action: inh VLDL secretion, decrease LDL production, increase HDL (by decrease fractional clearance of Apo-A1)

ADR: vasodi → cutaneous flushing due to PGD2 formation , hyperpigment , hyperuricemia , hyperglycemia

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2
Q

fibric acid (some are -fibrate) - 1st line

A
  • gemfibrozil, bezafibrate, fenofibrate
  • 1st line for ลด TG
  • action: PPARα agonist → increase FA oxidation /// also increase activity of enz LPL
  • ADR: gallstone, myopathy (esp combine gemfibrozil x higher dose of statin)

DI: gemfibrozil x statin

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3
Q

omega3

A
  • EPA+DHA
  • FDA for treating TG levels of 500 mg/dL or greater (severe hypertriglyceridemia)
  • ใช้คู่ fibrate หรือเมื่อใช้ fibrate ไม่ได้ผล
  • ADR: minor side effects (vomiting, constipation, diarrhea, nausea, heartburn, stomach pain, joint pain) pt tx w anticoagulants should be monitor
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4
Q

cholestyramine

A

action: bile acid sequestrants

ADR: GI distress, steatorrhea, increase TG in plasma //เอา CHO ไปสร้าง bile แล้วขี้หมด

DI w acidic drug ~ กินให้ห่างกัน อย่ากินคู่กัน เป็นพอ

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5
Q

statin - 1st line

A

action: HMG-CoA reductase inh & increase LDL-receptor gene on hepatocyte

1st line for LDL (CHO) lowering

ADR: liver toxicity โดยการเพิ่ม aminotransferase enzyme activity ดังนั้น 3 เดือนแรกควร monitor liver enz (chronic liver disease ห้ามใช้) / muscle จะเพิ่ม creatine kinase activity and can lead to rhabdomyolysis / อย่าให้ใน preg เพราะ CHO สำคัญต่อ fetus development

DI: w gemfibrizil cause myopathy (กก OATP1B1) / CYP3A4 — sim ator lova

มีพูดเรื่อง Pleiotropic effects (beyond cholesterol lowering effect) พวกการ improve endothelial fx, inh plt aggregation, decrease LDL oxidation, reduce vascular inflam, stabilize atherosclerotic plaque !!

ALL STATIN should administered in evening except ator & rosu

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6
Q

ezetimibe

A

action: inh intestinal CHO absorption (inh at Niemann-Pick C1–Like 1 protein aka NPC1L1) → upregulate of LDL receptor → increase LDL uptake into cell and lower LDL in blood level

ให้คู่กับ statin ได้ / เลือกเปน 2nd line ถ้ามี contrain for statin

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7
Q

รวมมิตร non statin

A

evolocumab: Inhibiting PCSK9 → preventing LDL receptor degradation / potency ดี เปนยาฉีด ลด LDL ได้ 50-60%

lomitapide: microsomal triglyceride transfer protein (MTTP) inh

bempedoic acid: adenosine triphosphate-citric lyase (ACL) inh

inclisiran: small interfering RNA (siRNA) against PCSK9

evinacumab: ANGPTL3 inh

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8
Q

thiazide (hydrochlorothiazide - HCTZ)

A
  • inhibit Na/Cl Cotransporter at DCT — secrete at PCT ดังนั้นห้ามใช้ถ้า GFR<60
  • indication: HT HF nephrolithiasis (เฉพาะนิ่วแบบ idiopathic calcinuria)
  • ADR: volume depletion, hyperuricemia เพราะออกช่องเดียวกับ HCTZ เลยกำจัดไม่หมด, hyperlipid, hyponat, hypoka, allergic when take w sulfonamide // hypercal hypoka hypomag hypergly hyperlipid hyperuricemia
  • DI: ลด effect ของ anticoag, sulfonylurea, insulin / เพิ่ม effect ของ anes, digitalis, lithium, loop di / NSAID จะลด effect thiazide / bile acid จะลด thiazide absorption / เพิ่ม risk hypoka เมื่อกินกับ amphotericin B, corticosteroid / เพิ่ม risk torsade de pointes เมื่อกินกับ quinidine !!
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9
Q

loop diuretics (furosemide)

A

**most potent diuretic

  • inhibits Na/K/2Cl cotransporter at thick ascending loop (TAL) → reduces re-absorption of Na Cl Ca Mg K ดังนั้นน อย่าลืม monitor e’lyte ~
  • indication: acute pulmonary edema, CHF, acute RF (จาก oliguria สู่ non oliguria งี้), HF (not 1st line!!)
  • ADR: tinnitus, hearing impair, deaf, vertigo, hyperuricemia, hypoka, hypoka met alkalo, allergic when take w sulfonamide
  • DI: aminoglycoside เพิ่ม risk of ototoxicity / ลด effect ของ anticoag / เพิ่ม risk arrhythmia เมื่อกินกับ digitalis / เพิ่ม lithium blood level / เพิ่ม risk hypogly เมื่อกินกับ sulfonylurea / NSAID จะลด effect loop di
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10
Q

potassium sparing diuretics (spironolactone, amiloride, triamterene)

A

** lowest potency, used in combine w other diuretics เปนแค่ซัพพอร์ตเต้อ

used to correct drug-induced hypokalemia

  • spironolactone: aldosterone receptor anta / slow onset, short t1/2
  • amiloride, triamterene: ENaC blocker / longer action and t1/2
  • indication: HT (ใช้พร้อมกับ HCTZ or loop di), hypoka from mineralocorticoid excess — เจอใน conn HF cirrhosis NS
  • ADR: hyperka, androgenic effect (เพราะโมเลกุลคล้าย steroid) อย่างพวก gynecomastia libido hirsutism
  • contraindication: anuria, acute renal insuff, hyperka
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11
Q

alpha2 ago (methyldopa, clonidine)

A

indication: HT in preg (methyldopa), cancer pain (clonidine), opioid withdrawal (clonidine)

ADR: sedation, impair mental concentrate, nightmare, depress, bradycardia // มันจะง่วง ๆ โง่ ๆ

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12
Q

block nerve terminal (guanethidine, reserpine) ไม่ค่อยใช้ละ

A
  • prevent NE realease from postganglion sympathetic neurons
  • PHARMACOLOGIC SYMPATHECTOMY! ออกฤทธิ์ทั่วร่างกาย กี้ดด
  • ไม่ค่อยใช้ละ **
  • ADR: guanethidine → postural HT, sexual dysfx, diarrhea / reserpine → sedation nightmare depress diarrhea GI irritate
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13
Q

beta blocker

A

non-selective (-ISA): propranolol, sotalol, timolol
non-selective (+ISA): pindolol, oxprenolol
beta-1 selective (-ISA): atenolol, metoprolol, bisoprolol
beta-1 selective (+ISA): celiprolol, acebutolol
with alpha blocking: carvidolol, labetolol

used in: HT, angina, HF, pheo, thyroid storm (esmolol)

ADR: bradycardia or heart block, asthma attack (in non-selective), withdrawal syndrome (on ยาอยู่ละลืมกิน) จะ tachycardia มากๆๆ, diarrhea constipation, nightmare depression insomnia

contraindication: asthma COPD, cardiogenic shock, decompensate HF, heart block

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14
Q

alpha-1 blocker

A
  • at vss and prostate gland
  • non-selective: prazosin, doxazosin, terazosin, alfuzosin
  • selective (ใช้กับ BPH): tamsulosin, silodosin
  • indication: HT (not 1st line), BPH
  • ADR: first dose phenomenon คือ hypotension in upright position จากยาที่ทำให้ vasodi ไวเกิน แต่ถ้าผ่านช่วงแรกไปได้จะโอเคมากๆๆ, dizzy, palpitation, headache
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15
Q

Ca channel blocker - CCB (dihydropyridine, non-dihydropyridine)

A
  • inh Ca2+ influx into smooth muscle cells by blocking ligand-gated calcium channels in vascular and smooth muscle cells
  • dihydropyridine (vasodi, ไม่บล้อก heart): amlodipine, felodipine, nicardipine, nifedipine, lercanidipine, manidipine, nimodipine, isradipine
  • non-dihydropyridine (บล้อก heart หยุดทุกอย่างช้าลงหน่อย): phenyl alkylamine, benzodiazepines
  • indication: HT in low renin patients, angina, svt, hypertrophic cardiomyopathy, migraine, reynaud phenomenon
  • ADR (cardiac): dihydropyridine → MI / non-di → arrhythmia, heart block, HF
  • ADR (vascular): palpitation, peripheral (pretibial) edema บวมเหมือนถุงเท้า, flushing, constipation, dizzy, gingival hyperplasia
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16
Q

older oral vasodilators (hydralazine)

A
  • NO from endothelial cell release → +cGMP → arteriole > vein dilate → afterload ลด // cause HR drop by baroreceptor → must combined w diuretic and beta-blocker
  • used in severe HT
  • ADR: dose-related SLE แต่หยุดยาปุ้บหายยย
17
Q

parenteral vasodilators (sodium nitroprusside)

A
  • vss dilate via NO pathway
  • used in hypertensive emergency (>200/120)
  • ADR: CN toxicity (เพราะมี cyanide เปนสปก) weakness, psych, convulsion, arrhythmia, met acido, excessive hypotension & death — แก้ ADR ด้วย sodium thiosulfate
18
Q

potassium channel openers (minoxidil)

A
  • opens K-ATP channel → hyperpolarises plasma membrane → inh Ca influx → vasodi
  • used in: severe/refractory HT & male pattern alopecia
  • ADR: reflex tachycardia, flushing, hypotension, hirsutism, fluid retention
19
Q

ACEi/ARB
(RAAS anta) 1st line for HT ⁉️⁉️

A

ACEi - pril / ARB - sartan

used in: HT esp pt w high renin, proteinuria in DM, CHF, DN, MI

ADR: severe first dose HT, ARF esp in renal artery stenosis, hyperkalemia, angioedema, only ACEi → dry&nonproductive cough //เพราะไปลด bradykinin เจ๋งมาก มันเกี่ยวด้วยอะ

contraindication: hx of angioedema, bilat renal artery stenosis, renal failure, pregnancy (category X)**

20
Q

beta blocker in anti-ischemic

A
  • decrease HR, contractility, AV conduction → - myocardial O2 demand and time-to-angina onset during exercise
  • beta-1 blocker: metoprolol, bisoprolol, atenolol, nebivolol
  • non-beta selective: carvedilol
  • discontinuation should be progressive and not abrupt
21
Q

CCBs in anti-ischemic

A

เพิ่ม O2 supply: amlodipine, nifedipine, felodipine

ลด O2 demand: diltiazem, verapamil // beta-blocker + verapamil = risk of heart block!

22
Q

nitrate (nitroglycerin)

A
  • T1/2 nitrate: 2-8 mins
  • rapidly de-nitrated in the liver and in smooth muscle, 90% first pass effect, แต่ถ้าเปนฟอร์ม subling and transdermal จะไม่มี first pass effect
23
Q

guideline for acute angina

A

use short-acting nitrate

  • subling & spray nitroglycerin
  • isosorbide dinitrate: slower onset than nitroglycerin due to hepatic conversion to mononitrate
24
Q

guideline for angina prophylaxis

A
  • use long acting nitrate (Nitroglycerin, Isosorbide dinitrate, Isosorbide mononitrate) เป็น 2nd line therapy for angina relief เมื่อ BB or non-DHP CCB ใช้ไม่ได้
  • discontinuation should be progressive, not abrupt to avoid rebound increase in angina
  • contraindication: HOCM, severe aortic valvular stenosis, co-administration of phosphodiesterase inhibitors (sildenafil tadalafil vardenafil)
25
Q

guideline for chronic coronary syndrome

A

1st step BB or CCB
2nd step BB + DHP-CCB
3rd step add 2nd line drug

  • ivabradine: HR lowering by selective inh SA node / metabolize via CYP3A4 / SE → bradycardia AF / contraindication → acute decompensate HF, AV block, resting HR < 60, severe liver impair, pacemaker dependence
  • nicorandil: systemic venous and coronary vasodi + stimulate ATP-sensitive K channel / SE → nv, severe oral intestinal mucosal ulceration
  • ranolazine: selective inh of late inward sodium current / metabolize via CYP3A4 / SE → dizzy, nausea, constipation / ** QT prolong
26
Q

tx of ischemic (NSTEMI STEMI คิดว่าไม่น่าออกปะ)

A

คิดว่าไม่น่าออก ถ้าออกมาเติมละกัน

27
Q

Class I : Sodium Channel Blocker

A

IA: quinidine, procainamide, disopyrimide / เพิ่ม AP, ERP, QT, กก K channel blocking / used in arrhythmia esp reentry and ectopic svt & vt / ADR → cinchonism (quinidine), SLE-like (procainamide), HF (disopyramide), thrombocytopenia, torsade de pointes / caution and contrain → LVH, HF (diso qui), QT prolong (procain)

IB: lidocaine, mexiletine, +/- phenytoin / ลด AP duration, affect ischemic & depolarize purkinje and ventricular tissue / used in acute ventricular arrhythmia (esp post MI), digitalis induce arrhythmia / ADR → CNS stimulate or depress, CVS depress

IC: flecainide, propafenone / prolong ERP in AV node and accessory bypass tracts / used in SVT inc AF, last resort in refractory VT / ADR proarrhythmia esp post-MI (contrain!) / contraindication → structural heart disease, ischemic heart disease

28
Q

Class III : Amiodarone

A

like class I → block sodium channels at rapid pacing frequency / like class II → antisym / like class III → AP ยาว, block K channel / like class IV → negative chronotropic effect

action: negative inotropic effect, vasodi

ADR: amiodarone → torsade, pulmonary toxic, hypothyroid, hepatic toxic, corneal deposit, optic neuropathy, skin discolor / dofetilide → torsade / sotalol → torsade, CHF, bradycardia, hypotension, COPD exacerbate, bronchospasm / dronedarone → exacerbate of advance HF

contraindication: prolong QT (dofe), LVH (dofe sota), advance HF (drone)

29
Q

Class V : Adenosine

A

action: slow AV nodal conduction, interrupt reentry pathway through AV node, restore normal sinus rhythm in patients with Paroxysmal SVT inc one ass w WPW syndrome

30
Q

anticoag (เลือดไหล) - parenteral 3 ตัวแรก

A
  • heparin: bind to antithrombin III ทำให้ thrombin → inactive clotting factor (IIa IXa Xa) / lipidemia clearing effect, direct anticoag, dont cross blood-placenta / ADR: bleeding, thrombocytopenia, hypersen, alopecia, osteoporosis / antidote: protamine sulfate / monitor: aPTT accept at 2-3 times normal value
  • LMW heparin: ทำให้ Xa → inactive factor X by antithrombin / no lab monitor require exp renal insuff, obesity, preg / lower thrombocytopenia & bleed ถ้าเทียบกับ heparin / drug: nadroparin enoxaparin dalteparin
  • fondaparinux: no monitor require / cant using protamine as antidote
31
Q

anticoag (เลือดไหล) - parenteral 3 ตัวหลัง

A
  • hirudin: direct thrombin inh / used in pt w heparin-induced thrombocytopenia (HIT) and ass thromboembolic disease / monitor aPTT: accept 1.5-2.5 times normal range
  • bivalirudin: direct thrombin inh / for pt w or at risk of HIT, undergoing coronary angioplasty
  • argatroban: direct thrombin inh / in pt w or at risk of thrombocytopenia, HIT, undergoing PCI / monitor aPTT: accept 1.5-3 times normal range
32
Q

warfarin — oral anticoag

A
  • vitK anta / act on VKORC1 → inh reduction of vitK epoxide → inh gamma-carboxylation of glu in factor 2 7 9 10 (พูดง่าย ๆ คือ inh clotting factor ในตับ sooo easily bleed โคตร ๆ) แตตตต่ ถ้าในคนที่มี VKORC1 น้อย ก้ลดโดสลงได้ (less VKORC1 inh require for anticoag :))
  • act only in vivo, delayed onset on action until depletion of performed clotting factors
  • antidote: parenteral vitK1 (phytonadione)
  • protein binding 99% → กระทบโปรตีนนิดนึงคือเกินโดสได้เลย ดังนั้น high DI !
  • metabolized by CYP2C9: CYP2C9’1 (normal ppl), CYP2C9’2/3 (poor metaboliser) ยาถูกขับลดลงเลยต้องลดโดสที่ให้
  • cross placenta = in 1st tri is teratogenic (dont give to preg)
  • monitor by PT and adjust to INR (INR should be within 2.5-3.5)
  • DI: เพิ่ม anticoag → ABX (reduce vitK absorption), salicylate (displacement plasma protein), allopurinol metronidazole (inh hepatic biotransform), aspirin clopidogrel (inh plt aggregate), quinidine (reduce clot production) // ลด anticoag → barbiturate rifampicin (induction of metabolic enz), vitK contraceptive (enhance clot production)
  • ADR: bleeding, teratogen (dont use in preg), cutaneous necrosis (ไปลด protein C, S)
  • factor affecting activity of warfarin โดยรวม ๆ: dietary e.g. vitK fat, GI and liver disease, preg, hyperthyroid, NS
33
Q

oral anticoag อีก 2 ตัว มักใช้แทน warfarin เพราะรายนั้น ADR เย้ออ

A
  • dabigatran etexilate: direct thrombin inh / indication: prevent thrombosis after hip or knee replacement, DVT, PE, embolism prophylaxis in non-vulvular AF / antidote: idarucizumab ใช้เมื่อ urgent makk such as uncontrolled bleeding
  • rivaroxaban: direct factor Xa inh (เปน competitive reverse anta of active Xa) / indication: DVT prophylaxis, thromboembolism, reduce risk of stroke and systemic emboli in non-vulvular AF, reduce MI CAD PAD เมื่อใช้คู่กับ aspirin / antidote: andexanet alpha / pros → rapid therapeutic effect, no monitor, fewer DI / cons → short T1/2 แม้จะให้ยาแต้ก้เสี่ยงที่จะเกิด thromboembolism อยู่ดี
34
Q

antiplt overview แบบทั่วไป

A
  • prevent thrombosis → prevent stroke, MI in CAD
  • therapeutic use จำนะะ น่าออก: 2nd prevention in vascular event พวก angina งี้ → ASA clopidogrel / ischemic heart disease → ASA clopidogrel heparin / PCI & stent insertion → abxicimab tirofiban eptifibatide
  • รวมแฟค: aspirin can protect risk of occlusion vascular, clopidogrel มักใช้แทนใน aspirin-contraindicated pt, add 2nd antiplt ต่อจาก aspirin อาจช่วยได้ในบางกรณี e.g. after PCI
35
Q

antiplt 5 กลุ่ม สุ้ ๆ จร้า

A
  1. plt COX inh (aspirin): non-selective COX (TXA2), irreverse inh plt aggregate / ADR: GI irritate, bleed, anemia / low dose
  2. P2Y12 anta (5 ตัว): ticlopidine (prodrug) / clopidogrel (prodrug) → convert to active form by CYP2C19, reduce risk of stroke MI ในคนที่เคยเป็นแล้ว (2nd prevention) / prasugrel (prodrug) → by CYP3A4 CYP2B6, caution in ppl<60kg or renal impair, contrain in hx of cerebrovascular disease / ticagrelor → reduce thrombotic risk in ACS pt, metabolized by CYP3A4, ADR: dyspnea bleeding, contrain in active pathological bleed or hx of intracranial bleeding / cangrelor
  3. phosphodiesterase III enz inh (dipyridamole, cilostazol เน้นตัวนี้): metabolized by CYP3A4>CYP2C19 / indication: increase claudication, stroke / contrain: CHF
  4. plt GPIIb/IIIa anta (3 ตัว): prevent fibrinogen bleeding / abciximab → used in PCI / eptifibatide→ กก heptapeptide, ใช้มาก bleed / tirofiban
  5. PAR-1 anta (vorapaxar): indication → reduction of thrombolytic in MI & arterial disease / ADR: bleed
36
Q

thrombolytic (fibrinolytic drug)

A
  • ให้ทันทีที่ MI แต่ถ้าให้มากไปจน toxic อาจ hemorrhage
  • 1st gen: plasminogen activation / drug: streptokinase ฮิตกว่า, urokinase
  • 2nd gen: activate plasminogen in fibrin domain = clot selective จะช่วยลด bleed ได้ / drug: alteplase, anistreplase
  • 3rd gen ฮิตสุดสุด: longer T1/2, resistance to plasma protease inh, selective binding to fibrin, drug: tenecteplase (reduce AMI mortality), lanoteplase, reteplase, monteplase, pamiteplase
37
Q

antifibrinolytic drug — actually antidote of thrombolytic drug

A
  • compete for lysine binding site on plasminogen and plasmin → inh fibrinolysis
  • used in bleeding from fibrinolytic drug therapy (indication หลักคือใช้เปน antidote)
  • drug: EACA, tranexamic acid (ตัวหลังใช้ได้ใน various bleed e.g. hemorrhage following prostatectomy, dental extraction, menorrhagia
38
Q

normal range of lipid

A
  • TC (total CHO) < 200 mg/dl
  • LDL - C < 130 mg/dl
  • HDL - C > 40 mg/dl
  • TG < 150 mg/dl

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