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211 Cards in this Set

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Furosemide
Sulfonamide LOOP diuretic. Inhibits Na+/K+/2Cl- pump (thick ascending loop) (this normally will remove all 3 form the urine, making it less concentrated). By Inhibiting it, the urine contains more solute and the Renal Medulla will become less hypertonic. LOOPs LOSE Ca2+ (Ca2+ and Mg2+ paracellular reabsorption is induced by the NKCC pump) USES: Edema, HTN, Hypercalcemia SIDE EFFECTS: OH DANG! Ototoxic, Hypokalemia, Dehydration, Allergy (sulfa), Nephritis, Gout
Spironolactone
K+ Sparing Diuretic. Blocks Aldosterone receptors (in Cortical collecting Ducts, which would lead to increased Na+ reabsorption). USES: Hyperaldosteronism (Conn's), hypokalemia, CHF SIDE effects: Hyperkalemia (arrhythmia), can cause gynecomastia via antiandrogen effects. (other K+ sparing diuretics: Triamterene and Amiloride)
Digoxin (aka Digitalis)
Blocks Na+/K+ Pumps on myocytes, --> increases intercellular Na+ levels ---> decreases Na+/Ca2+ exchange ---> Increases Ca2+ inside the cell ---> which will decrease the HR (prolong phase 4 and 0 of the nodal action potential) and increase the force of contraction (increase Ca2+ release from sarcoplasmic reticulum) USES: CHF, Atrial Fib Side Effects: Cholinergic: Nausea, Vomiting, Diarrhea, blurry yellow vision, hyperkalemia
Verapamil
Anti-arrhythmic, Class 4, Ca2+ channel blocker. primary effect at AV node, decrease conduction velocity, increase PR interval and ERP(effective refractory period). USES: to prevent Nodal Arrhythmias, ex: SVT-supravetricular tach. SIDE effects: Constipation, flushing, edema, -- CHF, AV Block, sinus node depression.
Amlodipine
Ca2+ channel blocker, relaxes smooth muscle in arterioles, Decreases BP, and increases blow flow to heart (coronaries). USES: Angina, and HTN
Valsartan
ARB, angiotensin II receptor Blocker, USES: CHF, HTN, and Post-MI
Amiodarone
Anti-arrhythmic, K+ channel blocker - Class 3, (but really all 4 classes), increase AP duration, increase ERP (eff. refract. period), increase QT interval, SIDE EFFECTS: Must check LFTs, PFTs, TFTs - Liver toxic, pulmonary fibrosis, hypo/hyper thyroidism
Digoxin (aka Digitalis)
Blocks Na+/K+ Pumps on myocytes, --> increases intercellular Na+ levels ---> decreases Na+/Ca2+ exchange ---> Increases Ca2+ inside the cell ---> which will decrease the HR (prolong phase 4 and 0 of the nodal action potential) and increase the force of contraction (increase Ca2+ release from sarcoplasmic reticulum) Side Effects: Cholinergic: Nausea, Vomiting, Diarrhea, blurry yellow vision, hyperkalemia
Dopamine
Activates D1=D2 receptors > Beta > Alpha (inotropic and chronotropic) -- USES: treat shock (increases renal perfusion), and Heart failure
Dobutamine
Activates B1 > B2 , only inotropic, USES: treat shock, heart failure, and used in cardiac Stress Testing
Inamrinone
PDEIII (phosphodiesterase) inhibitor, increases cAMP, increases Ca2+, also has vasodilation activity. USES: Severe CHF SIDE effects: thrombocytopenia ---- Milrinone used instead
Milrinone
PDEIII (phosphodiesterase) inhibitor, increases cAMP, increases Ca2+, also has vasodilation activity. USES: Severe CHF
Prazosin
Blocks a1 receptors - USES: HTN, urinary retention from BPH SIDE effects:1st dose orthostatic hypotension, dizziness, headache.
Phentolamine
reversible Non-selective Alpha-adrenergic blocker - used to diagnose pheochromocytoma,
Atenolol
Block B1 selective > B2 receptors - USES: HTN, Anigina, MI, CHF SIDE effects: bradycardia, AV block, CHF
Propranolol
Non-selective blocker of Beta - adrenergic receptors B1=B2 - USES: HTN, CAD, tachycardia from hyperthyroidism, chronic migrains SIDE effects: bronchoconstriction (B2 blockade), Fasting hypoglycemia (B2 blockade), hypotension
Sotalol
non-selective blocker of Beta - adrenergic receptors B1=B2 - ALSO has K+ channel blocking activity (Class 3 anti-arrhythmic) (prolongs PR and OT intervals) - USES: HTN, atrial fibrillation. - SIDE effects:
Labetalol
Block both Alpha and Beta - adrenergic receptors - USES: refractory HTN
Carvedilol
Block both Alpha and Beta - adrenergic receptors - USES: CHF
Clonidine
Agonist at A2 receptors in the medulla - lowers NE release peripherally, - does NOT decrease renal blood flow so .. USES: HTN (especially in patients with renal disease). SIDE Effects: Rebound HTN if withdrawn quickly, bradycardia
Fenoldopam
Agonist at D1 receptors - splanchnic and renal vasodilation - USES: Severe HTN
Captopril
ACE Inhib. decreases Angiotensin II levels, prevents bradykinin breakdown (vasodilator), USES: CHF, HTN, diabetic renal disease SIDE effects: COUGH, Hyperkalemia, angioedema, proteinuria, taste problems, HypOtension, Rash, increased renin,
Losartan
ARB, angiotensin II receptor Blocker, (does not effect bradykinin degradation like ACE Inhibs) USES: CHF, HTN, and Post-MI, Diabetic nephropathy - SIDE effects: hyperkalemia and renal failure with patients who have renal insufficiency
Spironolactone
Blocks Aldosterone receptors - causes salt and water loss (since Na+ is normally exchanged for K+, it also lowers K+ excretion) -- USES: Hyperaldosteronism, CHF, hypertension -- SIDE effects: Hyperkalemia, gynecomastia, impotence, mentruation irregularites
Eplerenone
Blocks Aldosterone receptors - causes salt and water loss (since Na+ is normally exchanged for K+, it also lowers K+ excretion) -- USES: Hyperaldosteronism, CHF, hypertension -- SIDE effects: Hyperkalemia,
Aliskiren
Renin Inhibitor - USES: HTN SIDE effects: Angioedema, Hyperkalemia, hypotension, increased uric acid - Gout, renal stones
Hydralazine
directly relaxes arteriolar (only) smooth muscle - USES: HTN, CHF - SIDE effects: reflex tachycardia (contraindicated in patients with CAD), durg-induced lupus
Minoxidil
Dilates arterial (only) smooth muscle - opens potassium channels --> hyperpolarizes the muscle (relaxation) - USES: HTN, Hair growth (rogaine) --- SIDE effects: reflex tachycardia (contraindicated in patients with CAD or ventricle Hypertrophy,
Sodium Nitroprusside
Metabolized to NO in the blood --> NO activates guanyl cyclase --> increased cGMP ---> relaxes smooth muscles in BOTH veins and arteries - USES: acute Hypertensive crisis - SIDE effects: CYANIDE poisoning, thiocyanate is the metabolite, MUST be taken IV, if oral ---> becomes cyanide in GI tract (treat with thiosulfate)
Nifedipine
Ca2+ channel blocker, relaxes smooth muscle in arterioles, Decreases BP, and increases blow flow to heart (coronaries). Smaller effect on cardiac tissue in comparison to Verapamil. USES: Angina, and HTN --- SIDE effects: hypotension, peripheral edema
Amlodipine
Ca2+ channel blocker, relaxes smooth muscle in arterioles, Decreases BP, and increases blow flow to heart (coronaries). Smaller effect on cardiac tissue in comparison to Verapamil. USES: Angina, and HTN --- SIDE effects: hypotension, peripheral edema
Nicardipine
Ca2+ channel blocker, relaxes smooth muscle in arterioles, Decreases BP, and increases blow flow to heart (coronaries). Smaller effect on cardiac tissue in comparison to Verapamil. USES: Angina, and HTN --- SIDE effects: hypotension, peripheral edema
Clevidipine
Ca2+ channel blocker, relaxes smooth muscle in arterioles, Decreases BP, and increases blow flow to heart (coronaries). Smaller effect on cardiac tissue in comparison to Verapamil. USES: Angina, and HTN --- SIDE effects: hypotension, peripheral edema
Verapamil / diltiazem
Anti-arrhythmic, Class 4, Ca2+ channel blocker. primary effect at AV node, decrease conduction velocity, increase PR interval and ERP(effective refractory period). USES: to prevent Nodal Arrhythmias, ex: SVT-supravetricular tach. SIDE effects: Constipation, flushing, edema, -- CHF, AV Block, sinus node depression.
Guanadrel
false neurotransmitter, taken up and stored as NE but has no effect, replaces NE -- USES: HTN -- SIDE effects: if given IV it will initially release NE and increase BP
Reserpine
Binds to vesicles in neurons, inhibits transport of NE and Dopamine into vesicles -- leads to sympathetic dysfunction, and takes days-weeks to resynthesize vesicles after discontinuing treatment -
Guanabenz / clonidine / guanfacine
Alpha 2 -adrenergic agonist - low dose only A2a (CNS) agonist - but high dose A2b agonist (smooth muscle, peripheral) and can cause intial vasoconstriction (increase BP)
Nitroglycerin
dilates venous (more) and arteries, USES: treat hypertensive crisis in patients with cardiac ischemia or after bypass surgery
Esmolol
short acting B1 blocker, USES: aortic dissection, post-op HTN,
Aliskiren
Renin inhibitor, USES: HTN
Captopril
ACE Inhibitor, shorter half life, less effective in blacks, USES: HTN, CHF, MI, diabetic neuropathy, SIDE effects: COUGH, Hyperkalemia, hypotension, altered taste, decreased renal function (dec GFR), --- Contraindication: Renal impairment (artery stenosis), hypotension, pregnant, hyperkalemia, ---- DRUG interactions: NSAIDs, Digoxin, K+ sparing diuretics, Thiazide(loop) diuretics.
Enalapril
ACE Inhibitor, Longer half life, less effective in blacks, USES: HTN, CHF, MI, diabetic neuropathy, SIDE effects: COUGH, Hyperkalemia, hypotension, altered taste, decreased renal function (dec GFR), --- Contraindication: Renal impairment (artery stenosis), hypotension, pregnant, hyperkalemia, ---- DRUG interactions: NSAIDs, Digoxin, K+ sparing diuretics, Thiazide(loop) diuretics.
Losartan
ARB, angiotensin II receptor Blocker, (does not effect bradykinin degradation like ACE Inhibs) USES: CHF, HTN, and Post-MI, Diabetic nephropathy - SIDE effects: hyperkalemia and renal failure with patients who have renal insufficiency
Spironolactone
K+ Sparing Diuretic. Blocks Aldosterone receptors (in Cortical collecting Ducts, which would lead to increased Na+ reabsorption). USES: Hyperaldosteronism (Conn's), hypokalemia, CHF SIDE effects: Hyperkalemia (arrhythmia), can cause gynecomastia, impotence via antiandrogen effects. weak androgen antagonist, weak progesterone agonist. (other K+ sparing diuretics: Triamterene and Amiloride)
Eplerenone
K+ Sparing Diuretic. Blocks Aldosterone receptors (in Cortical collecting Ducts, which would lead to increased Na+ reabsorption). USES: Hyperaldosteronism (Conn's), hypokalemia, CHF SIDE effects: Hyperkalemia (arrhythmia), less antiandrogen effect. (other K+ sparing diuretics: Triamterene and Amiloride)
Nitroglycerin
Releases NO which will activate guanyl cyclase ---> increase cGMP ---> dilation of venules, dilation of coronary arteries. USES: Stable, unstable, variant (prinzmetal) angina, CHF, and MI ---- SIDE effects: hypotension, headaches, dizzy, weak, reflex tachycardia ---- Contraindications: Patients on Sildenafil, hypotensive, Hypertrophic cardiomyopathy, diastolic heart failure
Isosorbide Dinitrate
Chewable, longer duration (2-3hrs) -- Releases NO which will activate guanyl cyclase ---> increase cGMP ---> dilation of venules, dilation of coronary arteries. USES: Stable, unstable, variant (prinzmetal) angina, CHF, and MI ---- SIDE effects: hypotension, headaches, dizzy, weak, reflex tachycardia ---- Contraindications: Patients on Sildenafil, hypotensive, Hypertrophic cardiomyopathy, diastolic heart failure
Isosorbide -5-mononitrate
Releases NO which will activate guanyl cyclase ---> increase cGMP ---> dilation of venules, dilation of coronary arteries. USES: Stable, unstable, variant (prinzmetal) angina, CHF, and MI and ---- SIDE effects: hypotension, headaches, dizzy, weak, reflex tachycardia ---- Contraindications: Patients on Sildenafil, hypotensive, Hypertrophic cardiomyopathy, diastolic heart failure
Verapamil
Ca2+ channel blocker (L-type) --- more cardiac effect, will decrease HR, contractility, and conduction through the AV node (increases PR interval), --- USES: Variant Angina, stable, and unstable angina, and MI. and SVT's like artial fib --- SIDE effects: cardiac arrest, bradycardia, AV block, CHF (contraindicated in patient with heart failure)
Nifedipine
Ca2+ channel blocker (L-type) --- more effects on Vasculature, it decreases BP (and has a relfex tachycardia and increase in CO) --- USES: Variant Angina, stable, and unstable angina, and MI. --- SIDE effects: hypotension, and at high conc. bradycardia, AV block
Nimodipine
Ca2+ channel blocker (L-type) --- more effects on Vasculature (specifically Cerebral vessels), it decreases BP (and has a relfex tachycardia and increase in CO) --- USES: may reduce vasospasm and mortality after subarachnoid hemorrhage, Variant Angina, stable, and unstable angina, and MI. --- SIDE effects: hypotension, and at high conc. bradycardia, AV block
Dilitazem
Ca2+ channel blocker (L-type) --- more effect on the heart, decreases HR, contractility, and conduction through the AV node, (but unlike Verapamil - also has inhibitory effect on the sympathetic nervous system) --- USES: Variant , stable, unstable angina. MI, and SVT's like Atrial Fib --- SIDE effects: cardiac arrest, bradycardia, AV block, CHF (contratindicated in patients with heart failure)
Sotalol
Non-selective Beta-Blocker --- USES: angina, arrhythmia, post MI --- SIDE effects: erectile dysfunction, depression, insomnia, --- Contraindication: Not for patients with asthma (B2 blockade = bronchoconstriction) Not to be used in Prinzmetal (variant) angina (B2 blockade = vasoconstiction, increased pre-load, and afterload - decreases coronary flow)
No new drugs - Good lecture to put it all together
Quinidine
Class 1a - Na+ channel blocker - antiarrythmic - binds active state - decreases Phase 0 upstroke velocity, also blocks K+ channels which prolongs repolarization (increases QT interval)
Procainamide
Class 1a - Na+ channel blocker - antiarrythmic - binds active state - decreases Phase 0 upstroke velocity, also blocks K+ channels which prolongs repolarization (increases QT interval)
Lidocaine
Class 1b - Na+ channel blocker - antiarrythmis - binds BOTH inactive and active - MILD Na+ blockade, little K+ block so NO increase in QT interval
Flecainide
Class 1 C - Na+ channel blocker - antiarrythmic - STRONG Na+ channel blockade NO effect on repol. - NO increase in QT
Amiodarone
Class 3 (but also 1,2,4) K+ channel blocker - antiarrhythmic, alters lipid membrane - USES: V Tach or V Fib, atrial fib --- SIDE effects: long QT, hyper/hypothyroidism, liver enzyme inc, neuropathy, corneal deposits. INHIBITS CYP3A4, 2C9, (interactions with digoxin, warfarin, etc.)
Sotalol
Class 3 K+ channel blocker, but also Class 2 non-selective B blocker - USES: severe V tach --
Carvedilol
(and labetalol) 3rd gen Beta blocker - Class 2 antiarrhythmic - B1 selective with alpha blockade (vasodilation)
Ibutilide
Class 3 antiarrhythmic - K+ channel blocker - but also enhances slow Na+ inward current and therefore prolongs QT even more --- SIDE effects: long QT leading to serious torsades de pointes
Bretylium
Class 3 antiarrhythmic - K+ channel blocker - but also is an antihypertensive drug - acts like guanethidine and will replace NE in storage vesicles (initial release of NE) which lowers the amount of NE released --- Acts mainly on purkinje fibers ---USES: only in recurrent V tach or Fib
Adenosine
activates K+ current in atria SA and AV nodes - shortens the Action Potential and slows automaticity, increases AV refractory period --- USES: PSVT
digoxin
Inhibits the Na+/K+ ATPase - USES: CHF with reentry V tach --- positive inotrope, but also acts at the vagus nerve as a negative chronotrope
K+ ion
K+ levels must be carefully monitored as Hyper or Hypo K+ can cause arrhythmia, --- HYPO can cause EADs DADs and ectopic beats in myocytes --- HYPER can depolarize membranes and slow the conduction velocity
Acetazolamide
Carbonic anhydrase inhibitor (proximal tubule) --- Diuretic --- less Cl-/H+ excreted and more HCO- excreted --- leads to hyperchloremic acidosis after a few days of use --- USES: edematous patients with metabolic alkalosis, alkalinates the urine --- SIDE effects: renal stones, potassium loss
Mannitol
Osmotic diruetic --- lowers water reabsorption in prox tubule --- increased urine volume --- USES: acute renal failure --- TOxicity: dehydration, HYPERnatremia (due to excess water loss compared to Na+) this leads to Extracellular volume expansion
Furosemide (aka Lasix)
Loop diuretic (Na/K/2Cl transporter inhibitor) - Thick ascending loop (most potent type of diuretic) --- USES: Acute Pulmonary edema, nephrotic edema, hypercalcemia, --- SIDE effects: HYPO, K+,Na+, Mg+, HYPER, uricemia, glycemia (but HCTZ, more common), hypersensitivity Rxn with interstitial nephritis
Bumetanide
Loop diuretic (Na/K/2Cl transporter inhibitor) - Thick ascending loop (most potent type of diuretic) --- USES: Acute Pulmonary edema, nephrotic edema, hypercalcemia, --- SIDE effects: HYPO, K+,Na+, Mg+, HYPER, uricemia, glycemia (but HCTZ, more common), hypersensitivity Rxn with interstitial nephritis
Torsemide
Loop diuretic (Na/K/2Cl transporter inhibitor) - Thick ascending loop (most potent type of diuretic) --- USES: Acute Pulmonary edema, nephrotic edema, hypercalcemia, --- SIDE effects: HYPO, K+,Na+, Mg+, HYPER, uricemia, glycemia (but HCTZ, more common), hypersensitivity Rxn with interstitial nephritis
Ethacrynic Acid
Loop diuretic (Na/K/2Cl transporter inhibitor) - Thick ascending loop (most potent type of diuretic) --- USES: Acute Pulmonary edema, nephrotic edema, hypercalcemia, --- SIDE effects: HYPO, K+,Na+, Mg+, HYPER, uricemia, glycemia (but HCTZ, more common), hypersensitivity Rxn with interstitial nephritis, ALSO ototoxicity and GI bleeding
Chlorothiazide
Diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Polythiazide
Diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Methyclothiazide
Diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Hydrochlorothiazide (HCTZ)
diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Bendroflumethazide
diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Chlorthalidone
diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Quinethazone
diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Indapamide
diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Metolazone
diurectic, inhibits Na/Cl symport in distal tubule - increases Na+,Cl+ and K+ excretion, but leads to reabsorption of Ca+ --- USES: essential HTN, CHF, nephrogenic DI --- SIDE effects: HYPO K+, HYPER, glycemia, uricemia, lipidemia, calcemia
Spironolactone
inhibits aldosterone (in collecting tubule) --- postassium sparing diurectic -- used WITH other diuretics in order to reduce K+ loss, and have slight additive diueretic effect, --- USES: CHF --- SIDE effects: endocrine = gynecomastia, menstrual irregularities, impotence, decreased libido, hyperkalemia
Eplerenone
competitively inhibits aldosterone (collectiing tubule) --- postassium sparing diurectic -- used WITH other diuretics in order to reduce K+ loss, and have slight additive diueretic effect, --- USES: CHF --- SIDE effects: less endocrine effects compared to spironolactone, but Hyperlipidemia, hyperkalemia
Triamterene
Potassium sparing diuretic - aldosterone INDEPendent --- blocks Na+ channel in collecting tubule, SIDE effects: Hyper K, azotemia, crystalluria, triamterene stones, acute renal failure
Amiloride
potassium sparing diuretic - aldosterone INDEPendent --- blocks Na+ channel in collecting tubule, SIDE effects: Hyper K
Aspirin
Irreversibly blocks COX enzyme --- prevents formation of TXA2 --- USES: CAD and unstable angina --- SIDE effects: GI bleeding and peptic ulcer dz
Clopidogrel
Irreversibly blocks ADP receptors (thienopyridine - a pro drug) --- prevents acitivation which would stimuilate expression on GP2b/3a --- USES: CAD and unstable angina --- SIDE effects: bleeding, peptic ulcer
Ticlopidine
Irreversibly blocks ADP receptors (thienopyridine - a pro drug) --- prevents acitivation which would stimuilate expression on GP2b/3a --- USES: CAD and unstable angina --- SIDE effects: bleeding, peptic ulcer
Dipyramidole
Inhibits cAMP phosphodiesterase -- increases cAMP levels, and acts like Thienopyridines, but also is a vasoDilator, USES: prophylaxis of heart valve thrombi, prevention of stroke recurrence.
Prasugrel
Irreversibly blocks ADP receptors (thienopyridine- a pro drug) --- prevents acitivation which would stimuilate expression on GP2b/3a --- USES: CAD and unstable angina --- SIDE effects: bleeding and even hemorrhagic stroke, peptic ulcer ---- NEW drug, faster onset, more potent, and less variation due to p450 polymorphs -
Abciximab
Antibody against GP2b/3a - IV during angioplasty -- Expensive, excessive bleeding or major hemorrhage may occur
Eptifibatide
peptide that Inhibits GP2b/3a - shorter duration of action compared to abciximab - less expensive
Tirofiban
reversible, non-peptide inhibitor of GP2b/3a, similar to eptifibatide
Heparin (Unfractioned)
Binds and activates Antithrombin III --- antithrombin III will inhibit Thrombin, and factors 9,10,11,12 --- half life increases with dose --- Monitor aPTT, target 1.5-2.5 times normal --- Unfrac. Heparin is not cleared by the kidney so it is used for patients with compromised renal function (in comparison to LMWH) --- SIDE effects: bleeding (reversed by protamine sulfate when severe), HIT - heparin induced thrombocytopenia (immune reaction)
LMW Heparin
Bind and activates Antithrombin III - However, will not help inhibit thrombin, Mainly acts by inhibiting Factor 10. --- aPTT is not used to monitor therapy --- USES: 1st line to treat thromoboembolism, prevent PE, angina and MI --- SIDE effects: bleeding, NEVER give heparin to patients undergoing brain, spinal cord or eye surgery.
Enoxaparin, et al
Is a Low molcular wieght heparin --- binds and activates Antithrombin III --- which inhibits Factor 10
Protamine Sulfate
Used to treat heparin induced severe bleeding, is a basic protein (binds to and neutrolizes the acidic heparin molecule) ---DOES NOT reverse LMWH overdose
Fondaparinux
selective inhibitor of Factor 10a. smaller than LMWH but also cleared by the kidneys (like LMWH) --- USES: prophylaxis for DVT
Lepirudin
irudin = inhibitor, reversible, of thrombin --- both clot bound and circulating thrombin, cleared by the kidneys (like LMWH), so caution with those with renal impairment
Bivalirudin
irudin = inhibitor, reversible, of thrombin --- both clot bound and circulating thrombin, cleared by the kidneys (like LMWH), so caution with those with renal impairment
Argatroban
inhibits thrombin --- but cleared by the liver p450 enzyme, use with caution with liver problem patients
Warfarin
Inhibits vitamin K epoxide reductase --- this stops activation of factors 2,7,9,10 - monitor PT and INR --- USES: Post MI to prevent stroke or PE, Atrial fib, prosthetic heart valve
Dabigatran
direct thrombin inhibitor, prodrug, superiority over warfarin in stroke prevention from atrial fib
Rivaroxaban
direct factor 10a inhibitor - prevents Venous thromboembolism following knee or hip replacement
Urokinase
normally produced in the kidney --- directly converts plasminogen to plasmin ---
Streptokinase
facilitates the conversion of plasminogen to plasmin --- 5% of patients have allergic response
Anistreplase
mix of streptokinase and human plasminogen
t-PA
activates plasminogen, but ONLY in the presence of Fibrin, so no systemic activation of plasmin, which is good
Fish Oil
omega - 3 FAs can be made into TXA3 - which is a vasodilator that blocks platelet aggregation --- however, aspirin would negate the positive effects by inhibiting COX and therefore the produciton of TXA3
Niacin
Decreases VLDL synthesis --- Increases HDL (more than any other drug) --- USES: hetero fam hypercholesterolemia, mixed lipemia, combined hyperlipoprotenemia, DYSBETAlypoproteinemia, Lipoprotein A hyperlipoproteinemia ----- SIDE effects: flushing (treat with aspirin or laropiprant), pruritis, rash, hyperuricemia
Fenofibrate
Fibric acid derivative -- activates PPARa = increases lipoprotein lipase activity, decreases VLDL synth, increases HDL --- reduces risk of MI or CHD --- USES: severe hypertriglyceridemia, DYSBETAlipropeinemia SIDE EFFECTS: --- myopathy and rhabdomyolysis = when COMBINED WITH STATIN !!! --- anemia and gallstones also reported
Colestipol
Binds bile acids --> prevents reabsorption --> leads to liver creating more bile acids via cholesterol --> leads to more uptake of LDL, IDL VLDL by the liver... via increase in ApoB100 and ApoE receptor expression. USES: heterozygous Fam hypercholesterolemia, hyperlipidemia --- SIDE effects: constipation, bloating, rarely steatorrhea or gallstones
Cholestyramine
Binds bile acids --> prevents reabsorption --> leads to liver creating more bile acids via cholesterol --> leads to more uptake of LDL, IDL VLDL by the liver... via increase in ApoB100 and ApoE receptor expression. USES: heterozygous Fam hypercholesterolemia, hyperlipidemia --- SIDE effects: constipation, bloating, rarely steatorrhea or gallstones
Colesevelam
Binds bile acids --> prevents reabsorption --> leads to liver creating more bile acids via cholesterol --> leads to more uptake of LDL, IDL VLDL by the liver... via increase in ApoB100 and ApoE receptor expression. USES: heterozygous Fam hypercholesterolemia, hyperlipidemia --- SIDE effects: LESS SIDE EFFECTS, and LESS DRUG INTERACTIONS constipation, bloating, rarely steatorrhea or gallstones
Lovastatin
HMG CoA reductase inhibitor (indirectly upregulates ApoE and ApoB100 receptors (lowers LDL) --- activated in GI tract --- 30% absorbed -- big first pass metabolism -- and large first pass metabolism in liver (%5 bioavail) --- USES: fam hypercholesterolemia, or combined hyperlipidemia --- SIDE effects: mild hepatotoxic , myopathy (reversible), rhabdomyolysis at high dose.
Simvastatin
HMG CoA reductase inhibitor (indirectly upregulates ApoE and ApoB100 receptors (lowers LDL) --- activated in GI tract --- BETTER absorbed than lovastatin, 2x potency --- USES: fam hypercholesterolemia, or combined hyperlipidemia --- SIDE effects: mild hepatotoxic , myopathy (reversible), rhabdomyolysis at high dose.
Atorvastatin
HMG CoA reductase inhibitor --- ACTIVE drug given --- reduces LDL cholesterol by 50-60%
Rosuvastatin
HMG CoA reductase inhibitor --- similar to atrovastatin --- but HIGHer incidence of SIDE effects like rhabdomyolysis and renal failure
Ezetimibe
inhibits the absorption of cholesterol at the brush border of intestinal villi --- when combined with a statin LDL is lowered by another 25% --- Does not prevent or reduce plaque build-up , NO evidence that it reduces Coronary events or stroke
Laropiprant
D2 prostaglandin inhibitor --- Used to treat flushing from Niacin use)
Neomycin
Exerts a complimentary effect with NIACIN --- helps lower cholesterol levels --- USED in: fam hypercholest, fam combined hyperlipid
Gemfibrozil
Like Fenofibrate --- Fibric acid derivative --- activates PPARa but not as good as fenofibrate
Somatotropin
recombinant hGH --- USED: to treat hypopituitary dwarfism (subcutaneous or IM) --- glucocorticoids can retard growth rate (fyi) ---
Sermorelin
recombinant GHRH --- USED: to treat hypopituitary dwarfism (alternative)
Somatomedin C
aka IGF-1
Mecasermin
recombinant IGF-1 ( with IGF-BP3, which binds IGF-1 and increases half life) --- USED: to treat HYPERpituitary dwarfism (Laron syndrome), due to defective GH receptors
Pegvisomant
GH blocker --- binds to GH receptor and blocks binding of endogenous GH --- decreases IGF-1 production --- USES: Acromegaly --- SIDE effects: nausea diarrhea, chest pain, flu symptoms
Bromocriptine
Dopamine agonist (D2) --- USED: to treat acromegaly (50% respond, possibly because these tumors are both prolactin and GH secreting), aslo used for hyperprolactinemia (prolactinoma), Parkinson's Dz, Neuroleptic malignant syndrome ---- Bromocriptine will stop the symptoms of hyperprolactinemia (galactorrhea and amenorrhea) as well as shrink the tumor (adenoma, if present)
Octreotide
Somatostatin analog (with increased half life compared to endogenous SST) --- supresses GH, and ACTH, TSH, insulin, glucagon, VIP --- USES: Acromegaly, pancreatic cholera (due to VIPoma, MEN1 assn)
Thyroid USP
used to treat HYPOthyroidism, potency varies with each preperation
Thyroglobulin
used to treat HYPOthyroidism, potency varies with each preperation
Levothyroxine
Used to treat HYPOthyroidism, Specifically MYXedema
Sodium Liothyronine (T3)
Used to treat HYPOthyroidism, SHORT-acting
Liotrix Euthyroid
Used to treat HYPOthyroidism, 4:1 mix of T4 and T3
Methimazole
Used to treat HYPERthyroidism or Thyrotoxicosis, Inhibits thyroid Peroxidase, --- which blocks activation of Iodine --- this drug gets into mother's breast milk so breast feeding is not advised
Propylthiouracil
Used to treat HYPERthyroidism or Thyrotoxicosis, Inhibits thyroid Peroxidase, --- which blocks activation of Iodine --- this drug gets into mother's breast milk so breast feeding is not advised --- ALSO use with caution in Pregnant patients becuase PTU crosses the placenta
Lugol's Solution
Used to treat HYPERthyroidism or thyrotoxicosis --- KI and I2, this type of iodine will interfere with thyroid function, --- used in combination with methimazole or PTU
I131 (Radioactive Iodine)
Used to treat HYPERthyroidism, especially for destroying TOXIC adenoma, --- NEVER use in Pregnant patient
Calcitriol
1,25 D3 --- upregulates calcium binding transport protein in the gut --- increases Ca2+ absorption, also increases Ca2+ release from bone
Ergocalciferol (Vitamin D)
D2 made by fungi and yeast --- can also be hydroxylated to 1,25 D2 which has similar effects as D3
Raloxifene
SERM (selective estrogen receptor modulator) --- stimulates estrogen receptor on bone, but inhibits estrogen on breast --- USES: ERP Breast cancer, postmenopausal osteoporosis ---
Alendronate
Bisphosphonate, which inhibits osteoclast breakdown and demineralization of bone. It deposits in newly formed bone and protects it. ---USES: Osteoporosis, Paget's disease --- SIDE effects: heartburn and esophageal irritation, also after 5 years of treatment increased risk of non-traumatic femur fracture
Risedronate
Bisphosphonate, which inhibits osteoclast breakdown and demineralization of bone. It deposits in newly formed bone and protects it. ---USES: Osteoporosis, Paget's disease --- SIDE effects: heartburn and esophageal irritation, also after 5 years of treatment increased risk of non-traumatic femur fracture
Ibandronate (aka Boniva)
Bisphosphonate, which inhibits osteoclast breakdown and demineralization of bone. It deposits in newly formed bone and protects it. ---USES: Osteoporosis, Paget's disease --- ONLY need to take it once per MONTH --- SIDE effects: heartburn and esophageal irritation, also after 5 years of treatment increased risk of non-traumatic femur fracture
Zoledronic Acid
Bisphosphonate, which inhibits osteoclast breakdown and demineralization of bone. It deposits in newly formed bone and protects it. ---USES: Osteoporosis, Paget's disease --- ONLY need IV Infusion once per YEAR --- SIDE effects: fever, flu-like symptoms, myalgia (rare, but osteonecrosis of jaw)
Prednisone
Used to treat vitamin D intoxication --- blocks intestinal absorption of Ca2+ and lowers the hypercalcemia seen with D3 intox
Teriparatide
human PTH1-34 --- Stimulates osteoBlasts, stimulates new bone growth, decreases incidence of vertebral fracture --- Used to treat osteoporosis
Adrenocorticotropin
ACTH is released by the pituitary and activates MC2R Melanocortin receptor, Stimulates the production of Glucocorticoids
Corticotropin Releasing Factor
Released by the hypothalamus, stimulates the release of ACTH... increased levels of cortisol will ihibit the release of both CRF and ACTH. Negative feedback
Cortisol
Corisol is released by the zona fasiculata (adrenal cortex), --- involved in carbohydrate, protein, and lipid metabolism --- binds GRalpha receptor intracellularly, then together they binds the cis-acting elements to effect mRNA transcription.
Prednisolone
4x the glucocorticoid action of corisol, and less mineralocorticoid action
Dexamethasone
Very potent glucocorticoid and NO mineralocorticoid effect, also feedback inhibits ACTH production and therefore lowers endogenous corticosteroid production
Cortisone
INACTIVE until metabolized, similar effects to cortisol but less glucocorticoid effect
Prednisone
INACTIVE until metabolized, 4x the glucocorticoid activity, lowered mineralocorticoid activity
Fluticasone
First Pass metabolism is extensive, which results in fewer side effects
Mometasone
First Pass metabolism is extensive, which results in fewer side effects
Beclomethasone
More rapidly metabolized in the lungs, so fewer systemic side effects, administered via Inhalation
Aldosterone
VERY VERY potent Mineralocorticoid effect ---
Mifepristone
very potent ANTI-glucocorticoid effect --- Used to induce early-term ABORTION via antiprogestational effect
Spironolactone
Inhibits Aldosterone --- Treats HTN and CHF --- SIDE effects: hyperkalemia (potassium sparing), gynecomastia and impotence (anti-androgen), menstural issues (anti progestin)
Eplerenone
Selective mineralocorticoid receptor inhibitor --- like spironolactone but with less anti-anderogen, anti-progestin side effects ---
Androstenedione
Weak androgen produced in the zona reticularis --- main sources of androgens in females, metabolized to estrogens in males, --- this increases estrogens, and also lowers HDL
Dehydroepiandrsterone
Weak androgen produced in the zona reticularis --- main sources of androgens in females, metabolized to estrogens in males, --- this increases estrogens, and also lowers HDL
Estradiol
Produced from testosterone via Aromatase
Testosterone
made from androstenedione via 17B hyrdoxysteroid DH
Metyrapone
Blocks 11b-hydroxylase --- this causes a decrease in coritisol and aldosterone, however, there is less effect on mineralocortioid suppression becuase the precursor 11-deoxycorticosterone has mineralocorticoid effects.
Aminoglutethimide
Inhibts P450 scc (side chain cleavage) which normally makes pregnenalone from cholesterol... this leads to DECREASE in ALL ADRENAL steroid biosynthesis --- also inhibits aromatase (whic normally converts testosterone to estradiol...
Testosterone Enanthate
Transdermal treatment for HYPOgonadism
Testoderm
testosterone film taped onto scrotum (testes) --- used to treat Andropause or the decrease in testosterone with age
Androderm
Skin patch with testosterone AND permeation enhancers
AndroGel
GEL with permeation enhancers and testosterone, rubbed on shoulders
Danazol
orally active androgen (targets liver) --- stimulates compliment esterase inhibitors ---- Used to treat Hereditary Angioedema, which is due to defective C1-esterase inhibitor, therefore there is overactive compliment which caused vascular permeability --> angioedema
Stanozolol
orally active androgen (targets liver) --- stimulates compliment esterase inhibitors ---- Used to treat Hereditary Angioedema, which is due to defective C1-esterase inhibitor, therefore there is overactive compliment which caused vascular permeability --> angioedema
Leuprolide
GnRH agonist --- indirectly downregulates LH and FSH and therefore testosterone and estradiol
Flutamide
Inhibits Androgen receptors --- reactively increases LH, therefore Leuprolide (GnRH agonist) is added to limit this effect --- USED to treat METASTATIC PROSTATE cancer
Bicalutamide
Inhibits Androgen receptors --- reactively increases LH, therefore Leuprolide (GnRH agonist) is added to limit this effect --- USED to treat METASTATIC PROSTATE cancer
Cyproterone acetate
Weak inhibitor of androgen receptor --- used to treat HIRSUTISM in women
Finasteride
5a redcutase inhibitor Type II (which would make DHT from testosterone) --- Used to treat BPH and also Male pattern baldness (propecia)
Dutasteride
Blocks both Type I and II 5a reductase ---- therefore it works in all tissues
Equilin
equine estrogen, avoids 1st pass metabolism by addition of SO4 --- Used to treat: hypogonadism, Post-menopause HRT,
17a-ethinyl estradiol
17a modifcation makes it Orally active,
Norethindrone
Progesterone derivative added to ethinyl estradiol for HRT --- decreased risk of bone fracture and colon cancer --- BUT, INCreased risk of: MI, stroke, blood clots, breast cancer
Tamoxifen
SERM (selective estrogen receptor modulator) --- For treating estrogen receptor positive BREAST cancer --- it is an inhibitor of estrogen at breast tissue but and AGONIST at bone and endometirum, this decreases osteoporosis, but increases risk of endometrial cancer and thrombosis
Raloxifene
SERM (selective estrogen receptor modulator) --- For treating estrogen receptor positive BREAST cancer --- it is an inhibitor of estrogen at breast tissue and endometrium but and AGONIST at BONE --- Therefore it is used to TREAT Osteoporosis
Letrozole
Aromatase inhibitor, Used to treat BREAST cancer, (no risk of thrombosis, endometrial cancer or hot flashes)
Insulin
Normal Human hormone produced by B-cells in the islets of the pancreas --- realeased in response to elevated Glucose or GLP-1 (glucagon-like peptide) --- Normally stored as a hexamer with Zinc --- stimulates gylcogen sythesis in the Liver --- glucose/amino acid uptake in the muscle --- lipogenesis in the adipose tissue
Insulin Lispro (aka Humalog)
Absorbed very rapidly compared to other insulins, it can be injected just prior to eating (compared to regular insulin which must be injected 30 minutes beforehand)
NPH Insulin (aka Isophane)
Long duration insulin, but has a peak concentration at 8-12 hours
Zinc extended Insulin
Long duration insulin, but has a peak concentration at 8-12 hours, also lasts 36 hours
Insulin glargine
ULTRA LONG acting synthetic insulin prep, does not produce a peak concentration like other insulins
Insulin determir
LONG acting synthetic insulin, does not produce a peak concentration, injected twice a day subcut. and gives a smooth background insulin all day.
Tolbutamide
First generation sulfonylurea --- Inhibits K+ efflux from B-cells in the pancreas --- causes depolarization and Ca2+ influx and release of Insulin
Glyburide
Second generation sulfonylurea --- 200x more potent that tolbutamide ---- also inhibits K+ efflux, depol B-cell, Ca2+ influx, release of insulin
Glipizide
Second generation sulfonylurea --- 200x more potent that tolbutamide ---- also inhibits K+ efflux, depol B-cell, Ca2+ influx, release of insulin
Metformin
Used to treat Type II diabetes, Inhibits Gluconeogenesis in the liver, thereby reducing fasting and post-prandial hyperglycemia, almost never causes hypoglycemia --- However, rarely it may cause Lactic Acidosis (can be fatal)
Acarbose
Alpha-glucosidase inhibitor --- inhibits breakdown of sucrose in the gut which reduces hyperglycemia following a meal (used to treat Type II diabetes) --- SIDE effects: Gas, bloating, and diarrhea
Pioglitazone
A "glitizone" --- decreases insulin resistance --- activates the PPARgamma nuclear receptor --- this increases insulin sensitivity by increasing glucose transporters on cell membranes of skeletal muscle and adipose cells --- may also reduce gluconeogenesis in the liver --- May reduce risk of MI and stroke
Repaglinide
Not a sulfonylurea, But mechanism of action is the same, K+ efflux inhibition, depol cell, Ca2+ influx, release of insulin
Sitagliptin phosphate
Causes and increase in GLP-1 --- mech: inhibits DPP-4 (dipeptidyl peptidase) which breaks down GLP-1 ---> therefore GLP-1 levels increase which stimulate insulin release and inhibits glucagon release
Levonorgestrel IUD
IUD containing a progestin (Levonorgestrel) --- lasts 5 years --- prevents fertilization via: sterile inflammation, destruction of sperm, and inhibition of ovulation --- Benefits: lowers menstural bleeding, no system exposure to hormones, can be used during lactation period (post-partum), --- SIDE effects: Acne, need to check for string (make sure its still there), risk of uterine perf, pelvic infection (1st 20 days) --- increased likelihood of PIC if patient has gonorrhea, or chlamydia
Norplant
6 rods implanted that release levonorgestrel --- 5 years protection, suppressed ovulation, thickens cervical mucus, thins endometrium --- benfits: ease, can be used during lactation, decreases anemia, PID, endometrial cancer, ectopic preg --- SIDE effects: irregular bleeding (66%), weight gain, headaches, acne, mood changes, mastalgia (breast pain) , requires minor surgery
Depo-Provera
subcutaneous injection (every 3 months) --- depot-medroxy progesterone --- inhibits ovulation, thickens cervical mucus, thins edometrium --- Benefits: ease, can be used during lactation, decreases anemia, PID, ectopic preg, endometrial cancer --- SIDE effects: Irregular mesturation, Amenorrhea (50% by 1 year, 80% by 3 years) , weight gain, acne, mood changes, headaches, bone loss
Estrogen/Progesterone Ocs
inhibits LH surge (ovulation), thickens cervical mucus, increases fibrinogen, factor V, VII, and X, increases risk of thromboembolism ---- Benefits: lowers risk of: PID, dysmenorrhea, Acne, RA, osteoporosis, endometrial cancer and ovarian cancer --- RISKS: increased risk of thromboembolism (stop smoking, do not use if patient has Hx or HTN, PE, DVT, CAD or diabetes), increased risk of cervical cancer (need pap smear), breast tenderness, nausea, fluid retention
Progestin-only OC
do not consistently inhibit ovulation
NuvaRing
Placed in vagina for 3 weeks, then removed for a week... - Benefits likely similar to OCPs --- SIDE effects: vaginal discharge, vaginitis, spotting, nausea, breast tenderness
PlanB
89% reduction in pregnancy risk --- contains ONLY levonorgestrel --- 1 pill
Preven
2 pills, each has Levonorgestrel and estradiol --- less total levonorgestrel than PlanB
LoOrvral
4 pills, estradiol and Norgestrel (only .3mg) --- note that this is not levonorgestrel
Clomiphene
SERM (selective estrogen receptor modulator) used to increase frequency of ovulation during each period (with infertility) --- binds to HYPOTHALAMIC estrogen receptors, which slows receptor replenishment, and decreases estrogens negative feedback effect on the release of GnRH ----> INCREASES GnRH , this favors release of FSH ---- It is CONTRAindicated after conception has occurred --- SIDE effects: Flushing, blurred vision, headache
Gonadotropins
LH and FSH --- LH activates the theca cell to make androgens and FSH activates the granulosa cell to make aromatase to convert androgens to estrogen --- Used to induce ovulation if Clomiphene fails or for hypothalamic anovulatory issues --- Drug of choice to Harvest eggs during IVF ---