Pharm 3 Cardio Flashcards

1
Q

Numodipine

A

Calcium Blocker

  • Most lipid soluble
  • Cerebral Vasodilator
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2
Q

Diltiazem

Benzothiazipine

A

Calcium Blocker

  • Less tachycardia
  • Depress SA & AV
  • ↓ contractility
  • Bradycardia
  • C/I SA &AV node abnormalities/CHF
  • Aterioles>Veins
  • INHIBIT INSULIN; Interfere plate agg
  • ↑ plasma Digoxin
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3
Q

Captopril

A
  • ACE inhibitor (peptidyl dipeptidase)
  • Increases Angioten I & Bradykinin
  • Bradykinin → ↑ PG syn → vasodilation
  • No reflex sympathetic
  • Young Caucausians (mono therapy ok)
  • DOC: DM, chronic renal, LV hypertropy
  • Synergistic with diuretics
  • Cough, hyperkalemia, angioedema, acute renal failure w/ B/L stenosis, hypotension
  • C/I Pregnancy, K+ diuretics, NSAIDS (block bradykinin
  • active drug (all other ACEI are prodrugs)

**ACEI don’t compromise HEART, KIDNEY, or BRAIN

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4
Q

Verapamil

Papaverine

A

Calcium Blocker

  • strongest Cardiac Effect
  • Less tachycardia
  • Depress SA & AV
  • Constipation
  • Bradycardia
  • Aterioles>Veins
  • INHIBIT INSULIN; Interfere Plate Agg
  • ↑ plasma Digoxin
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5
Q

Nifedipine

Dihydropyridines

A
  • Calcium Blocker
  • Strongest Vaodilator
  • ↓ afterload ↑o2 supply
  • Reflex tachycardia
  • Vascular Side Effects
  • Gingival hyperplasia
  • Less SA AV effect
  • INHIBIT INSULIN; Interfere -Plate Agg
  • ↑ plasma Digoxin
  • Slow release HPT
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6
Q

Losartan

A
  • Inhibit AT1 (ATII receptor) → ↑ ATII
  • No bradykinin effect
  • SE: hyperkalemia, acute renal failure w/ B/L stenosis (?), hypotension
  • Fetal Toxicity
  • Does not cause cough/angioedema
  • More effective lowering mortality Atenolol
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7
Q

Ranolazine

A
  • Partial fatty-acid oxidation inhibitor
  • ↓ left ventricular wall stiffness
  • Oral
  • Inhibits late sodium
  • Metabolized by CYP3A= drug interactions
  • C/I: hypokalemia, Heart rhythym abnormalities
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8
Q

Nitroglycerin

A
  • ↑ cGMP
  • ↓ preload ↓afterload
  • Can ↑ workload by reflex tachycard
  • ↓ O2 requirement & redistribute bf to ischemic
  • ↓ platelet aggregation
  • Acute hypotension, THROBBING headaches
  • Tolerance, “Monday Disease”
  • High first pass effect
  • Sublingual avoids hepatic
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9
Q

Aliskiren

A

-Renin Antagonist block ang I
-Hypertension
Hepatobiliary clearance
Headache
Dizziness
GI events
C/I Pregnancy 2nd 3rd Trimesters Categ D

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10
Q

Sildenafil

A

-Selective inhibior of cGMP phosphodiesterase
-PDE5
-Helps with Impotence
-Treats pulm hypertension
-PDE6 less potent EYE
-Metabol CYP 3A4
Adv Effect
-Nasal congestion, UTI,
-Visual Impairment
-C/I: pregnant/children, NITRATES, alpha blockers

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11
Q

Verdenafil

A
  • Like sildenafil
  • More selective for PDE5>6
  • Faster onset
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12
Q

Dorzolamide

Brinzolamide

A
  • Inhibit Carbonic Anhydrase

- Topically for Glaucoma

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13
Q

Furosemide

A
  • Loop Diuretic/ Inhibit NaK2Cl thick asc
  • ↑ excr Mg & Ca
  • TREAT: CHF, Edema, HyperCalc, excess K
  • HYPOKALEMIA & ALKALOSIS
  • ↑ PG synthesis, Relieve PULM Congestion
  • Hyperuricemia
  • OTOTOXICITY w/ aminioglycosides
  • Thrombocytopenia, Allergies
  • DI: Aminoglyc, Lithium, Digoxin
  • C/I Sulfonamide, hep cirrhosis, renal fail, dangerous in CHF
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14
Q

Ethacrynic Acid

A
  • Loop Diuretic
  • Same Adverse Effects
  • Not a sulfonamide
  • Higher risk of OTOTOXICITY
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15
Q

Hydrochlorothiazide

A

-Inhibit Na/Cl resorption distal tubule
-Depends on PG synthesis (inhib by NSAID)
Uses
-HPTN, CHF, Nephrolithiasis, **Nephrogemoc DI
Effects
-↑ K opening, Lower BP, enhance antihyperten drugs
-Hypokalemia, Hyperuricemia, ↓ Ca excre, ↑Mg. Br, Iodine loss, Hyperglycemia ↓insulin
-↑ Lipids Blood, Dyscrasia, Necrotizing vasculitis, aggravate jaundice infants, Lithium Toxicity

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16
Q

Metolazone

A
  • Similar to Thiazide,

- Produce diuresis in patients with reduced GFR

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17
Q

Indapamide

A
  • Direct vasodilators
  • Thiazide Like
  • Hepatic metabolism
  • No increase in Lipids
  • PRONOUNCED Vasodilation
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18
Q

Spironolactone

A

-Competitive inhibitor of aldosterone
-Binds to glucocorticoid and sex hor receptors @ high doses
Toxicities
-GI, Impotence, GYNECOMASTIA,
-Hyperkalemia, Acidosis
-CAREFUL: w/ ACE inhib and ARB’s
-Most Effective in Hyperaldosteronism

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19
Q

Eplerenone

A

Selective Aldosterone Receptor Antagonist

  • Simular to spironolactone, NO ENDOCRINE EFFECTS ↓ affinits gluco, androgen receptors
  • REDUCE all cause mortality with M.I.
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20
Q

Triamterene

A

-Independent of aldosterone,
-Inhibits Dihydrofolate reductase
-Inhibit sodium potassium exchange distal tube
-NO CAUSE OF HYPERURICEMIA
Toxicity
-Hyperkalemia
-Nausea vomiting
Use
-Combo with K losing diuretics
-Edema w/ CHF,Cirrhosis, Nephrotic synd
-Hirutism.

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21
Q

Amiloride

A

-Independent of aldosterone,
-Inhibit sodium potassium exchange distal tube
-NO CAUSE OF HYPERURICEMIA
Toxicity
-Hyperkalemia
-Nausea vomiting
Use
-Combo with K losing diuretics
-Edema w/ CHF,Cirrhosis, Nephrotic synd
-Hirutism.
DOC: lithium induce Diab Inipidus

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22
Q

Mannitol

A

Osmotic Diuretic
-Freely Filtered @ glomerulus
-Pharmacologically inactive
-Inhibits water resorption at prox and loh
-DOC: less irritable, less likely thrombophlebitis
USES:
-↓ intraocular, ↓ intercranial, ↓ CSF, protect kidney form toxic agents, prophylaxis renal
Toxic - ↑ cerebral bf, dehydration, ECF expansion,
pulm edema CHF, headache

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23
Q

Vasopressin

A
  • Exogenous form of ADH
  • Parenteral
  • Prevent or control poly-uria/dipsia & dehydration
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24
Q

Desmopressin

A

-Synthetic analog of ADH
-Long acting
-↑ coag VIII & vWF
USES:
-Ruptured esophagus varix bleeding

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25
Conivaptan
- Non peptide v1 & v2 adh rec antagonists | - ↑ urine output ↓ resorption water
25
Cilostazol
Anti-platelt - PDE3 inhib → ↑ cAMP - TX intermittent claudication
26
Demeclocycline
- Tetracycline antibiotic - Used to produce Diabetes Insipidus - Uncouple v2 receptor - Lower toxicity than lithium
27
Lithium
Uncouples v2 from adenylyl cyclase
29
Digitalis | Digoxin
-CardOut ↑ in CHF; Not in normal pt: ↓HR -Use for atrial arrhythmias -Inhibits Na/K ATPase -↑ contractility, ↑ free Ca ↑intra Na -K counters Digitalis;Digitalis counters K -Mg and K ↓ toxicity -Hockey Stick Config -Narrow Marg of Saftey: L ADV EFF: arrhythmias, CNS, and skin irrit DO NOT USE CARDIOVERISON C/I: WPW syndrome
30
Digoxin | Drug Interactions
Enhance toxicity: - ↓ Renal Clearance & ↓ VD: - -(quinidine, amiodarone, verapamil, diltiazem, captopril) - ↑ GI Absorption Reduce Toxicity: -↓ GI absorption: Cholestyramine ↓ absorption QUINIDINE: ↑ plasma levels displaces from protein DIURETICS: cause hypokalemia= ↑toxicity ELDERLY: ↑ levels b/c hypochloridia/↓ Clearance INFANTS: ↑ Dose Hypothyroid: ↓renal CL  ↑ plasma levels Use: Lidocaine, Phenytoin or Propranolol for intox
30
Milrinone
-Inodilator or bipyridine -Inhibit PDE, ↑ cAMP -↑ Ca influx -Vasodilatory -ACUTE: ↑ CardOut CHRONIC: ↓ survival Toxicites -Arrhythmias, thrombocytopenia, nausea USE FOR ACUTE HEART FAILURE
31
Inamrinone stop here
-Inodilator or bipyridine -Inhibit PDE, ↑ cAMP -↑ Ca influx -Vasodilatory ACUTE: ↑ CardOut CHRONIC: ↓ survival Toxicites -Arrhythmias, thrombocytopenia, nausea USE FOR ACUTE HEART FAILURE
33
Dopamine
``` -Sympathomimetic USE: Severe refractory CHF & Post op heart -↑ Cardiac Output ↑ RBF -↓ p. resistance -↑ Na excretion -Can treat shock -IV Admin ```
33
Levosimendan | Pimobendan
- Calcium Sensitizers - ↑ calcium sensitivity w/out ↑ tissue calcium - Inhibit PDE III - Sensitizes troponin-C
34
Dobutamine
- Sympathomimetic - Selective B1 - Less Tachycardia - ↑ O2 consumption - Reduced filling pressure - IV admin
36
Nesiritide
- Analog of BNP - Acute Tx of decompensated CHF - Causes ↓ Pulm Wedge Press - Improves Dyspnea and Fatigue - Lack of tolerance (unlike Nitroglycerin) MONITOR BP, hypotension
37
Beta Blockers CHF | Bisoprolol, Carvedilol Metoprolol
-Dangerous in severe CHF -↓ mortality rates class II and III CHF USED in Diastolic Dysfunction & cardiomyopathy Benefits - Attenuation catecholamines - ↑ beta receptors - ↓ HR ↓ Remodeling - Antiarrhythmic effect (UNIQUE)
38
Sodium Nitroprusside
- Used in CHF helps with preload after load - IV for HTN emergencies (↑ infusion = ↓ BP & visa versa) - Vasodilator Art and Veins (veins > arteries) - ADVERSE: Excessive Hypotension - Metabolized to thiocyanate: CYANIDE POISONING - Can cause metabolic acidosis - Sodium Nitrite → methemeglobin → Tx CN poisoning
39
Hydralazine
``` -ORAL: chronic HPT Tx-Vasodilator- peripheral (via NO) -Relax ARTERIOLE smooth muscle (NO VEINS) -↑ HR, Card Output, Left Vent Eject Fraction -SAL: chronic HPT Tx -given in combo w/ diuretics and BB -Use for short term -esp. effective w/ AFRICAN AMERICAN ``` -SLE in slow acetylators **May induce ANGINA and MI in pts w/ CAD
39
Procainamide
-Class IA antiarrythmic/ Like Quinidine -Shorter Duration of Action & IV use -Affected by slow/fast acetylators -Same Adv Effect Quin: Torsdae de Pointes ADV EFFECT: SLE & ↑ ANA -DO NOT USE in complete AV block -USE in ventricular and supraventric TACHY
40
Quinidine
Class IA antiarrythmic--open & inactive Na chan - Myocardial Depress: ↓automaticity&response - ↑ Diastolic Threshold: slow Ca rise rate - ↑ APD & ERD: PREVENTS REENTRY - Block K+: ORAL; First pass - Block M Rec, ekg changes, ↑SA/AV block - LOW Ther INDEX: C/I- Av block,thrbocyto - Cardiac TOXIC;paradox tachy, SYNCOPE, Torsade de Pointes, Diarrhea Cinchonism - ↑ pt time, Phenytoin ↑ metab, ↑K=↑Toxicity - ↑ effect of paralyzing agents
41
Disopyramide
-Class IA inhibitor, Different Structure than Quinidine -Reduces Cardiac Index -Use for premature ventricular & vent tach -Increases ERP, elect threshold, decrease velocity -Toxicity -Torsdade de Pointes, Neg Inotropic effect -Anticholinergic effect DO NOT USE IN SICK SINUS SYNDROM USE FOR VENTRICULAR TACHYCARDIA
42
Lidocaine
- Class Ib- antiarrhythmic & anesthetic - Binds inactivated channels - Decreases APD, Shortens ERP - Block slow Na Window Currents - NO depressant on contractility - NO VAGAL blocking - IV only, NO use for Supravent arrythmia - Toxicity - CNS Depression, Hypotension Convulsion - Bradycardia * *Least negative inotropic
43
Mexiletine
- Class Ib - Similar to lidocain - Also relieves pain in diabetic neuropathy - Toxicity - CNS - Tremor - Blurred - Lethargy CAN BE USED ORALLY
44
Phenytoin
-Class Ib -Binds active and inactive NA channels -Antiepileptic drug -Used with digitalis toxicity -Shortens ERP: depression myocar automaticity Toxicity -Nystagmus, ataxia, slurred speech, confusion -Elevated glucose levels -Fever Rash Blood dyscrasia -Drug Interaction -Warfarin, Disulfiram inhibit the metabolism -Induces P450, inhibits folate dihydro reduct
45
Flecainide
-Class IC- binds to ALL Na channels -No effect APD, ANS -QRS widening, shorten AP perkinje -No first pass Toxicity -BLURRED VISION, Proarrythmic effect C/I -Pre ex AV block -CHF or cardio genic SHOCK *use for life threat ventric arrhythmias, prevent PSVT
46
Propafenone
-Class IC similar to Flecainide -Structurally similar to beta blockers -Use in hospital with monitoring RESERVED FOR LIFE THREATENING
47
``` Beta Blockers (What type of Arrhythmic Drug) ```
Class II
48
Amiodarone
- Class III anti-arrhythmic - Life threat vent arrhythmia & atrial flutt/fib - Blocks K, Binds to inactivated Na, Calcium blocking, - Causes peripheral vasodilation (alpha block) - LARGE half life - Causes bradycardia, heart block, pulm fibrosis - Deposits in tissues cornea, Thyroid dysfunc - Ventricular Arrhythmias * ** NO TORSADES DE POINTES***
49
Sotalol
- Nonselective beta blocker Class II l-isomer - Prolongs action potent Class III d-isomer - USED in ventricular and supraventricular - CAUSES torsades de pointes
50
Ibutilide
- Class III - USED: Rapid Conversion atrial fib/flutter - Promotes Na influx through hslow channels - Increases Length of action potential - DOES NOT alter bp, hr or QRS
51
Dofetilide
- Class III - USED: Conversion and Maintenance atrial fib - Effective supraventricular arrhythmia - Blocks Potassium channels - NO NEGATIVE INOTROPIC ACTIVITY - ORAL - Toxicity - Arrhythmias,TORSADE DE POINTES - Influenza Syndrome, Resp Tract Infect
52
Calcium Channel Blocker | Anti-arrhythmic
-Class IV Verapamil- --Blocks slow cardia Ca, slows AV node, --Supraventricular Tachycardia (Rentry Type) --Minimal tox after ORAL --Constipation **avoid w/ beta blockers** Diltiazem - -Inhibits influx extracell Ca, reduces HR - -Increases exercise capacitance, improve perfus - -Treat paroxysmal supraventricular tach, atrial fib/flutter, Prinzmetal, follow ANGIOPLASTY -affect arteries more than veins
53
Adenosine
-DOC for PSVT and for WPW syndrome -Slows conduction AV node, interrupts Rentry -Atropine doesn’t affect but *Caffeine does -Enhace K conductance, inhib of cAMP Ca -SHORT ACTING: IV ONLY -Flushing, loss of breath, burn chest, hypotension C/I: -Sick sinus syndrome -AV Block
54
Magnesium Sulfate
-Mechanism UNKOWN -Effective even with normal Mg levels USES: -Digitalis induces arrhythmia -TORSADE DE POINTES -Management of Seizures
55
Potassium
- Careful b/c insufficient and excess are both PRO ARRHYTHMIC - Use to normalize K pool - Effects: Resting potential depolarization & membrane stabilization. * Hypokalemia=Increased risk of afterdepolarization
57
Clonidine
-Central acting sympathomimetic -↑medullary α2 stim -> ↓peripheral sympathetic -Presynaptic ↓ transmitter release -Postsynaptic ↓ inhibit neurons -Lowers BP by ↓ vasoconst & ↓ renal renin -Higher effect on HR & C. Outp > Methyldopa Adverse -CNS effects, Xerostomia, -fast withdrawal = Hypertensive crisis Drug Inter: TCA’s and Yohimbine
57
Dexmedetomidine
- Central acting sympathomimetic - Selective α2 - Sedative and analgesic - ADMIN: IV - Anesthesiology and Post-op
58
Methyldopa
-Central acting sympathomimetic -Pro-drug -↑medullary α2 stim -> ↓peripheral sympathetic -Presynaptic ↓ transmitter release -Postsynaptic ↓ inhibit neurons -Lowers BP by ↓ vconst & ↓ renal renin -can be used during pregnancy Adverse: -CNS effects (sedation, dizziness), Xerostomia -**Hemolytic Anemia w/ + coombs test -↑ prolactin: gynecomastia Drug Interaction w/ TCA’s & Yohimbine
59
Mecamylamine
- Ganglionic Blocker - Tertiary amine: Goes to CNS - Promising in Tourettes syndrome NOT typically used TONS side effects
60
Reserpine
-Adrenergic Nerve Blocker -Binds to vesicles: inhibits NE into vesicle (VMAT) -Released NE metab by MAO enzyme Adverse -Sedation -Psychic depression -Stuffy nose -GI
61
Guanethidine
-Adrenergic Nerve Blocker -Replaces NE in vesicles -Inhibits exocytosis Adverse -Interaction w/ TCAs cocaine, indirect sympath
63
Prazosin Terazosin Doxazosin
``` α1 selective BLOCKER -↓ NE vasoconstriction in arteries & veins (equally) -Less tachycardia no block of alpha 2 Adverse effects -Postural Hypotension/ 1st dose effect -↑ renin= sodium water retention -Does not affect plasma lipids ``` *veins have denser alpha 1 concentrations*
63
Drugs that can cause SLE in slow acetylators
Hydralazine Isoniazid Procainamide
64
Betablocker | *Nebivolol
-Reduce CO, ↓ Renin, ↓ SNS vasomotor tone -Preferred: angina, migraines, after M.I. -Least preferred: high physical activity, black, DM, ↑ cholesterol, peripheral vascular disease -Most effective in Young, and Caucasians (thiazide: elderly and blacks) -**Combine w/ other Rx to prevent tachycardia and ↑ renin from other drugs **Nebivolol ↑ endogenous NO production= ↑vasodilation ADVERSE: Heart, Lung, GI, CNS -↑ exercise tolerance, -predispose atherogenesis ↑ VLDL ↓ HDL -Mask symptoms of hypoglycemia ****C/I: Diabetes, sever CHF, heart block, asthma
66
Carvedilol
-Alpha1 and beta blocker - ↓ BP w/o causing tachy -Lower BP in hypertensive emergency Adverse: -Orthostatic hypertension -Bronchospasm -HEPATOTOXIC Lipid Neutral
66
Fenoldopam
-IV for HTN emergencies -Specific D1 receptors agonist (no tachy from B1) -Postsynaptic relax arteriolar smooth muscle Toxicity -Reflex tachycardia -Headache -Flushing
67
Diazoxide
-IV for HTN emergencies -Vasodilator and hyperglycemic (ARTERIES only) -Is a thiazide but not diuretic effect -Activates ATP/K+ channels (inhibit insulin release) -Used with INSULINOMA patients Adverse -Hyperglycemia -Sodium retention -Hyperuricemia (b/c its a Thiazide) -Excessive Hair growth
69
Minoxidil
- ORAL for chronic HTN tx - dilates ARTERIES (via open K+ channel) - given in combo w/ diuretics and BB * *May induce ANGINA and MI in pts w/ CAD - inhibit insulin release
70
drugs that inhibit insulin release
- Diazoxide (K channel → hyper polarize) - Minoxidil (K channel → hyper polarize) - CCB (Ca channel → no Ca induced exocytosis)
71
Least preferred HTN drugs for: 1) 65+ yrs 2) African american 3) Pregnant 4) Angina 5) Asthma 6) Diabetic (?)
1) centrally acting alpha2 agonist (clonidine, methyldopa) 2) BB 3) ACEI, ARB 4) Hydralazine, Minoxidil 5) BB 6) Propanolol can mask symptoms of hypoglycemia, inhibit insulin release, and increase blood lipids
72
1) Classic or Atherosclerotic angina (angina of effort) Tx | 2) Variant or angiospastic angina (Prinzmetal's)
1) ANGINA OF EFFORT - Beta Blockers - CCB - Ranolazine (partial Beta-ox inhib) - do NOT use Hydrazine or Minoxidil w/ CAD 2) VARIANT ANGINA - DOC: Nifedipine - nitrates relieve spasm - CCB (Diltiazam) - do NOT use BB → ↓ HR → ↑ ejection time → ↑ LVEDV → ↑ o2 req.
73
Niacin
Class: Hyperlipidemia MoA: Inhibits VLDL secretion, hepatic chol-genesis - ↓ VLDL & LDL - ↑ HDL USE: heterozygous familial hypercholesterolemia, combined hyperlipopreteinemia, when STATINS INEFFECTIVE ``` ADV/EFF: Vasodilation (from PG → aspirin prevents it) Nausea Elevate aminotransferases Impairs glucose tolerance Hepatotoxicity ```
74
Gemfibrozil
Class: Hyperlipidemia: Fibric Acid Derivative MoA: Ligand TF for ppar-α ↑LPL activity - ↓ VLDL → ↓ TAG (may ↑ LDL) - ↓Cholesterol USE: Fam Dysbetalipoproteinemia & Hypertriglycemia Do NOT USE prim chylomicronemia & Fam Hypercholesterolemia ``` ADV/EFF Skin Rashes, Gi, Hypokalemia ↑ aminotransferases & ALP ↑ cholelithiasis/gallstones **Inhibits metabolism of statins, ↑LDL Potentiate anticoagulay ```
75
Fenofibrate
Class: Hyperlipidemia: Fibric Acid Derivative MoA: Ligand TF for ppar-α ↑LPL activity - ↓ VLDL → ↓ TAG (may ↑ LDL) - ↓Cholesterol USE: Fam Dysbetalipoproteinemia & Hypertriglycemia Do NOT USE prim chylomicronemia & Fam Hypercholesterolemia ``` ADV/EFF Skin Rashes, Gi, Hypokalemia ↑ aminotransferases & ALP ↑ cholelithiasis/gallstones **Inhibits metabolism of statins, ↑LDL Potentiate anticoagulay ```
76
Colestipol
Class: Hyperlipidemia: Bile Acid Resin MoA: Diver Chol from VLDL to synth of Bile Aci ↑ expression of LDL receptor, ↑ LDL uptake ↓ LDL *Take with Meals* USE: LDL elevated HETEROzygous hyperlipidemia DO NOT USE: homozygous hyperlipidemia (no LDL receptors) & hypertriglyceridemia ADV/EFF: Constipation & gallstone (less than fibric acid) Hypoprthrombinemia poor vit K absorption Impair absorption: Digitalis, thiazides, tetracycline, thyroxine, aspirin
77
Cholestyramine
Class: Hyperlipidemia: Bile Acid Resin MoA: Diver Chol from VLDL to synth of Bile Aci ↑ expression of LDL receptor, ↑ LDL uptake ↓ LDL *Take with Meals* USE: LDL elevated HETEROzygous hyperlipidemia DO NOT USE: homozygous hyperlipidemia (no LDL receptors) & hypertriglyceridemia ADV/EFF: Constipation & gallstone (less than fibric acid) Hypoprthrombinemia poor vit K absorption Impair absorption: Digitalis, thiazides, tetracycline, thyroxine, aspirin
78
Colesevelam
Class: Hyperlipidemia: Bile Acid Resin MoA: Diver Chol from VLDL to synth of Bile Aci ↑ expression of LDL receptor, ↑ LDL uptake ↓ LDL *Take with Meals* USE: LDL elevated HETEROzygous hyperlipidemia DO NOT USE: homozygous hyperlipidemia (no LDL receptors) & hypertriglyceridemia ADV/EFF: Constipation & gallstone (less than fibric acid) Hypoprthrombinemia poor vit K absorption Impair absorption: Digitalis, thiazides, tetracycline, thyroxine, aspirin
79
Lovastatin
Class: Hyperlipidemia, Comp inhibitor HMG CoA reduc MoA: Analogs metabolites inhibit HMG CoA, ↓ LDL, ↑ LDL receptors, ↓TAGs ↑ HDL USE: When LDL is elevated *GIVE IN EVENING* BENEFITS: ↓CRP, ↑NO, ↑plaque stability, ↓ LDL oxid ↓ platelet aggregation ``` ADV/EFF: Liver damage &↑ aminotransferase ↑ creatine kinase activity Rhabdomyolysis Myoglobinuria plugs kidney C/I in PREGNANCY Grapefut juice ↑ bioavailability, ```
80
Orlistat
Inhibits pancreatic lipase → ↓ TAG breakdown | used for weight loss
81
``` Lab findings: ↑ Cholesterol → ↑ TAG → ↑ Cholesterol and TAG → ↓ HDL → ```
Cholesytamine, colestipol, ezetimibe Gemfibrozil Statins and niacin, ezetimibe Niacin
82
Heparin sodium
- Anticoagulant, prophylaxis against thrombosis - Binds ATIII → mainly inactivates Xa & thrombin (XII, XI, IX ) - IV ONLY (onset immediate) - can cause HIT - CI: renal or hypatic dysfunction - inactivated by protamine sulfate - monitored by PTT
83
Ezetimibe
Class: Hyperlipidemia: Inhibits cholesterol absorption MoA: Blocks absorption of cholesterol & phytosterols USE: to lower LDL & Cholesterol Synergistic with STATIN to lower Cholesterol Enterohepatic circulated Metabolized by glucoronidation No significant adverse effects
84
Enoxaprin - -Dalteparin - -Danaparoid
- Anticoagulant (LMW heparin) - Binds ATIII → mainly inactivates X - Sub-Q injection - ↓ chance of HIT - not completely reversed by protamine sulfate - monitored by PTT - used during PREGNANCY instead of warfarin
85
Fondaparinux
- Synthetic pentasaccharie - Anticoagulant (LMW heparin) - Binds ATIII → mainly inactivates X - Sub-Q injection - ↓ chance of HIT - not effected by protamine sulfate - monitored by PTT
86
Lepirudin Bivalrudin --Argatroban
DIRECT THROMBIN INHIBITOR - doenst require ATIII - given as alternative in HIT - IV ONLY - Lepirudin → kidney - Bivalrudin → liver - monitored by PTT - -Argatroban → liver
87
Dabigatran
ORAL direct inhibitor of Thrombin
88
Rivaroxaban | --Apixaban
ORAL inhibitor of Xa | Tx: DVT, PE, and FUTURE CLOTS
89
Warfarin
- ORALLY, chronically - ↓ reduction of vit K → - → ↓ synthesis of VII, IX, X, II, protein C** - rapid ↓ protein C → transient hypercoag - -give w/ heparin @ initiation - delayed onset - delayed disappearance of effect - PREVENT emboli - reverse w/ - -VIT. K → slow - -FROZEN PLASMA → immediate - cant use during pregnancy (use Enoxaprin)
90
Warfarin drug interactions
Drugs that affect: - vitamin K - clotting factors (estrogen pregnancy) - platelet aggregation/function - Inhibit microsomal liver enzymes - Induce microsomal liver enzymes
90
Aminocaproic acid | --Tranexamic acid
ANTIFIBRINOLYTIC - Inhibits plasminogen activation - Treatment of bleeding disorder - reversal of fibrinolytic therapy - oral or IV - ADVERSE: can cause intravascular thrombosis
91
Alteplase - -Reteplase - -Tenecteplase
FIBRINOLYTIC - IV or intra-arterially - convert plasminogen → plasmin - lysis of already formed clots → re-establish perfusion - -Higher affinity for FIBRIN-BOUND plasminogen → clot selective -Tenecteplase more fibrin specific and resistant to PAI-1
92
Aspirin
ANTIPLATELET Inhibitor of thrombogenesis -irreversible inhibition of COX → ↓ TXA2 -USED secondary prevention of cardiovascular events in patients with ESTABLISHED CV disease
94
Clopidogrel - Ticlopidine - Prasugrel
Inhibitor of ADP-induced platelet aggregation -Irreversibly block ADP receptor on platelets -Given ORALLY DOC: prevent thrombosis in pt getting CORONARY STENT
95
Abciximab
Inhibitor of GPIIb/IIIa receptor - ↓ platelet aggregation by inhibiting GPIIb/IIIa receptor from binding FIBRINOGEN - given IV** →↑↓