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315 Cards in this Set
- Front
- Back
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Classes of Antiarrthymic Drugs
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I=Na blockers
II=beta blockers III=K blockers IV=Ca blockers Others |
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Classes of Antihypertensive Drugs
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Sympatholytics
Vasodilators Diuretics ACE Inhibitors Ang II Rec Blockers Others |
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Classes of Antianginal Drugs
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Nitrates/ites
B-blockers Ca-blockers Others |
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Classes of Antihyperlipdemic Drugs
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Nicotinic Acid
HMG CoA Reductase Inhibitors Bile Acid Sequenstrants Cholesterol Absorbtion Inhibitors Fibric Acid Derivatives Omega-3 Fatty Acids |
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Class IA Antiarrthymic Drugs
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Procainamide
Disopyramide Quinidine block Ina, Ik, If |
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Class IB ADs
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Lidocaine
Mexiletine Tocainid Block Ina, If |
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Class IC ADs
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Encainide
Flecainide Propafenone Block Ina, If |
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Class II ADs
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the "olols"
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Class III ADs
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Amiodarone
Dofetilide Ibutilide Sotalol "SAID" |
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Class IV ADs
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Verapamil
Diltiazem Nifedipine |
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Atropine
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muscarinic blocker
used for sinus bradycardia and block |
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Adrenaline
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adrenergic (aka Epi)
nonselective alpha and beta agonist used for cardiac arrest and anaphylaxis |
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Isopraline
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B-agonist
used for heart block |
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Digoxin
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Blocks Na/K Pump resulting in inhibition of Na/Ca exchanger and intracelluar Ca buildup, resulting in increased contractility
Parasympathetic Also sensitizes baroreceptors (causes drop in BP) Used for A-fib and CHF |
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Adenosine
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increases K efflux
used to slow the heart (supraventricular tach) |
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K+ (use in cardiovasuclar pharm)
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used to treat ectopic pacemakers seen in hypokalemia (ie digoxin toxicity)
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Mg2+(use in cardiovasuclar pharm)
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used to treat torsades des pointes (v-fib) and digoxin toxicity
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What causes increased risk of torsades des pointes?
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Long QT
Class IA, III |
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HMG CoA Reducatase Inhibitors
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"statins"
Inhibits mevalonate (rate limiting step in cholesterol syn) Drop LDL, TGs, rise HDL |
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Niacin
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aka Nicotinic acid
Inhibits lipolysis in adipose tissue, reduces hepatic VLDL secretion drops LDL, TGs, rise HDL |
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Bile Acid Sequesterants
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Cholestyramine, Colestipol, Colesereton
prevent intestinal reabsorbtion of bile acids so the live must use cholesterol to make more Drops LDL, slight rise in TG and HDL |
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Cholesterol Absorbtion Blockers
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Ezetimibe
prevents chol absorb at the intestinal brush border Drops LDL |
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Fibric Acid Derivatives
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Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate
upregulate lipoprotein lipase causing increase TG clearance Drops LDL, esp TG. rise in HDL |
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Diuretics
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Loop
Thiazide K sparring Carbonic Anhydrase Inhibitors |
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a2 agonists
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methyldopa
clonidine also inhibit insulin release |
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a1 blockers
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prazosin
terazosin doxazosin "zosins" |
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non-selective B-blockers
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propanolol
pindolol timolol nadolol "NST PP" like Nasty sotaolol |
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B1-blockers
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acetbutolol (partial agonist)
atenolol esmolol metoprolol |
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Mixed a1/B blockers
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carvedilol
labetalol |
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B2 blocker
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Butoxamine
mostly used for experiments |
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Hexamethonium
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nicotinic ach blockers (preganginolic site of both para and sym)
sympatholytic used as antihypertensive also used to block baroreceptor reflex |
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Reserpine
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blocks VMAT (which transports NE, 5HT, Dopamine into presynaptic vesicle)
used as antihypertensive |
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Guanethidine
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inhibits Mg ATPase dept pump, which limits catecholamine release
antihypertensive |
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ACE Inhibitors
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"-Prils"
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Angiotensin II Receptor Blockers
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"sartans"
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Treatment of Malignant HTN
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Nitroprusside
Fenoldopam Diazoxide |
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Fenoldopam
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D1 agonist, which relaxes smooth muscle
used for malignant HTN |
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Hydralazine
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interferes with IP3
vasodilator |
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Minoxidil
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K+ channel agonist or NO agonist
vasodilator aka Rogaine |
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Diazoxide
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K+ channel activator
vasodilator |
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Ca Channel Blockers
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Verapamil
Dilitiazem Nifedipine Nicardipine Amlodopine Antianginal, Antiarrhythmics, Vasodilators |
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Ranolazine
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Alters late Na current, thus indirectly limiting intracellular Ca
Antianginal |
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Finasteride
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aka Propecia
5a reductase inhibitor, used to stop conversion of testosterone into DHT used for male pattern baldness and BPH |
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Gardasil
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quatravalent HPV vaccine 16, 11, 16, 18
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Clomiphene
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SERM used for anovulation and PCOS
body percieves lower estrogen that there really is and therefore increase GnRH which increases FSH and therefore ovulation/preganny |
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SERMs
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Clomiphene
Tamoxifene Raloxifene "ph/fhenes" |
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Tamoxifen
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SERM used to treat breast cancer
risk of endometrial cancer (because partial estrogen) |
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Sildenafil
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aka Viagra
inhibits phosphodiesterase causing increase in cGMP resulting in vasodilation of corpus cavernosum and erection |
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Vardenafil
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like sildenafil/viagra
inhibits phosphodiesterase causing increase in cGMP resulting in vasodilation of corpus cavernosum and erection |
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Flutamide
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competive inhibitor of androgen at testosterone/DHT receptor
used to treat prostate cancer. can also be used to treat excess testosterone in women. |
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Ketoconazole
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inhibits steroid hormone synthesis (inhibits desmolase)
used for PCOS |
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Spironolactone
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K sparring diuretic
inhibits steroid binding used for PCOS, diuresis, hypokalemia |
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Leuprolide
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if given pulsatile, GnRH analog (used for infertility)
if given continuously, GnRH antagonist (used for prostate cancer, uterine fibroids) |
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Mifepristone (RU-486)
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competitive inhibitor of progestin at progesterone recetptor
abortifacient |
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Dinoprostone
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PGE2 analog, used to dilate cervix and cause uterine contractions
induces labor |
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Ritodrine
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B2 agonist that relaxes the uterus
tocolytic |
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Anastrozole
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aromatase inhibitor used in postmenopausal women with breast cancer
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Raloxifene
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SERM, which is an agonist on bone, causing reduction in bone resorbtion
used to treat osteoporosis (esp in breast cancer) |
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Herceptin/Trastuzumab
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monoclonal Ab to Her2/NEU positive breast cancer causing cell arrest
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Betamethasone
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glucocoricoid which accelerates lung maturity and surfactant production in fetus (when parturition imminent)
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Tocolytics
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stop premature labor (for few days)
Ritodrine Terbutaline Nifedipine (off label) think 'TRN' as in terminate labor |
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Terbutaline
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B2 agonist that relaxes the uterus
tocolytic |
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Yohimbine
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a2 antagonist
5HT block can be used in ED b/c of 5HT block |
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Acebutolol
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B1 partial agonist
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Thiazide diuretics
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Hydrocholothiazide
Indapamide Metolazone Block Na/Cl symporter on distal convoluted tubule Cause Hypercalcemia, Hypokalemia, Hyperuricemia Used for HTN, edema, osteoporosis (prevents Ca elimination) |
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Ouabain
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endogenous steroid secreted with high Na intake that block Na/K ATPase (binds to K site)
results in buildup of intracellular Ca (like digitalis) and causes vasc constriction and HTN |
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Cyclosporine
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binds cyclophilin which inhibits calcineuriin, therefore inhibiting NFAT, therefore inhibiting IL2 production (which blocks T cells)
immunosuppressant |
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Tacrolimus
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binds FK binding protein which inhibits calcineuriin, therefore inhibiting NFAT, therefore inhibiting IL2 production (which blocks T cells)
immunosuppressant |
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Azathioprine
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antimetabolite precursor of 6 mercaptopurine which interferes with synthesis of nucleic acids. stops lymphocyte production.
immunosuppressant |
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OKT3
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"muromonab-CD3"
anti CD3 antibody which blocks T cell activation |
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Sirolimus
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mTOR inhibitor, which inhibits IL2 and T cell response
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Rapamycin
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mTOR inhibitor, which inhibits IL2 and T cell response
immunosuppressant |
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Mycophenolate Mofetil
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inhibits de novo guanine synthesis which blocks lymphocyte production
immunosuppressant |
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Daclizumab
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monoclonal Ab which binds IL-2 receptor on T cells
immunosuppressant |
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Use of B-interferon
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MS
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Use of a-interferon
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Hep B&C, Kaposi's, Leukemias, Melanoma
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Alprostadil
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PGE1, vasodilator used to treat ED
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Diabetes Med Classifications
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Insulin Analogs
Sulfonylureas Biguanides Glitizianoes alpha-glucosidase inhibitors |
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Insulin Analogs
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Lispro, Aspart, NPH, Lente, Ultra-lente
only useful for DM I bind insulin receptor (tyrosine kinase activity) risk of hypoglycemia |
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Sulfonylureas
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1st gen= tolbutamide, chlorpropamide
2nd gen= "Gl....ides" close the K channel of B cell causing depolarization, Ca influx and insulin release only for DM 2 1st gen have disulfiram effects 2nd gen have risk of hypoglycemia |
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Biguanides
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metformin
unknown mechanism but possibly increase glycolysis or decrease gluconeogenesis useful for both Type I and 2 DM can cause lactic acidosis |
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Glitazones
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increase target cell response to insulin
only for DM 2 can cause wt gain, edema, hepatotoxic, and CV toxic |
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alpha-glucosidase inhibitors
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acarbose, miglitol
inhibit intestinal brush border enzyme alpha-glucosidase lowering glucose absorbtion, especially good for post prandial gyperglycemia used for type 2 dm can cause GI disturbance |
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Dextrose
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can rapidly convert hyoglycemia
D-glucose, which cannot undergo glycolysis |
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Orlistat
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alters fat metabolism by inhibiting pancreating lipases
used in obesity mang |
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Sibutramine
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5HT and NE reuptake inhibitor
used in obesity mang |
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PTU
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propylthiouracil
inhibits peroxide thus inhibiting Th synthesis. also inhibits 5' monoiodinase preventing conversion of T4-T3 |
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Methimazole
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like PTU, but doesnt block T3 conversion
inhibits peroxide thus inhibiting Th synthesis |
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Ocreotide
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aka somatostatin
used for GH excess, 5HT excess, Gastrinoma, glucagonoma, etc. |
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Desmopressin
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ADH analog used to treat central DI
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Bromocriptine
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dopamine analog
used to for prolactinomas and Parkinson's |
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Carbergoline
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dopamine analog
used to for prolactinomas and Parkinson's |
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Levothyroxine
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thyroxine analog
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Triiodothyronine
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thyroxine analog
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Clonidine, Methyldopa use in DM
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inhibits insulin release
a2 agonists |
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Acetazolamide
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carbonic acid inhibitor used to treat glaucoma, intracranial HTN, etc
causes increased HCO3 excretion, therefore acidosis and hypokalemia |
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Synthetic Minerlaocoricoids
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Aldosternone
Deoxycoricosterone (DOC) 9a-flurocortisol |
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Antiglucocorticoids
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ketoconazole (blocks all steroid syn)
metyrapone (cortisol selective) mitotane - toxic to cortex mifepristone - cortisol and progesterone receptor antagonist |
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Antimineralocorticoids
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spironolactone (aldosterone receptor anatgonist)
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Biophosphonates
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"dronates"
suppress osteoclasts and therefore treat hypercalcemia |
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Ways to Ripen Cervix?
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Prostoglandins (PGE1 (misoprostol), E2 (dinoprostone)
Oxytocin Mechanically |
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Ways to Induce Labor?
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Prostoglandins
Oxytocin |
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Ways to Inhibit Labor?
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Tocolytics (Ritodrine/Terbutaline, Indomethacin (PG inhibitor))
Corticosteriods? |
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Which antihypertensives cause dyslipidemia?
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thiazide diuretics
metoprolol |
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H1 blockers: , uses, AEs?
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1st gen=diphenhydramine, dimenhydrinate, chlorpheniramine
uses: allergy, motion sickness, sleep aid ae: sedation, antimuscarnic, anti-alpha adrenergic 2nd gen=loratadine, fexofentadine, desloratadine, cetirizine use: allergy ae; much less sedation b/c less cns penetration |
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Asthma drugs
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non-specific B-agonist: isoproterenol
B2-agonist: albuterol, salmeterol Methylxanthine: theophylline Muscarnic antagonist: ipratropium cromolyn corticosteroids antileukotrienes: zileuton, zafirlukast, montelukast |
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Isoproterenol
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non specific B agonist
B1 effect = increased heart rate B2 effect = bronchial smooth muscle relaxation (asthma rx) and skeletal muscle vasodilation) |
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Albuterol
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short acting B2 agonist, used for acute asthma
AE some B1 effect |
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Salmeterol
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lng acting B2 agonist, used for prophylaxis for asthma
AE; some B1 effect |
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Theophylline: MOA, use, AE
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"methylxanthine"
bronchodilator inhibits phosphodiesterase, increases cAMP AE: small Therapeutic Index |
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Ipratropium: MOA, use
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competitive muscarinic block
prevents bronchoconstriction used for asthma and copd |
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Cromolyn: MOA, use
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stabilizes mast cells preventing release of mediators
prophylaxis of asthma (not acute asthma attacks) |
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How do corticosteroids help with asthma?
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inhibit virtually all cytokines
inactiate NF-KB (which is needed to induce TNFa and other inflammatory mediators) use: chronic asthma (1st line) |
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Zileuton
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5-lipoxygenase pathway inhibitor which blocks conversion of AA->leukotrienes
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Theophylline: MOA, use, AE
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"methylxanthine"
bronchodilator inhibits phosphodiesterase, increases cAMP AE: small Therapeutic Index |
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Ipratropium: MOA, use
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competitive muscarinic block
prevents bronchoconstriction used for asthma and copd |
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Cromolyn: MOA, use
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stabilizes mast cells preventing release of mediators
prophylaxis of asthma (not acute asthma attacks) |
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How do corticosteroids help with asthma?
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inhibit virtually all cytokines
inactiate NF-KB (which is needed to induce TNFa and other inflammatory mediators) use: chronic asthma (1st line) |
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Zileuton: MOA, Use
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5-lipoxygenase pathway inhibitor which blocks conversion of AA->leukotrienes
used for asthma |
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Zafirlukast: MOA, Use
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block leukotriene receptor
used for asthma, especially aspirin induced asthma |
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Montelukast: MOA, Use
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block leukotriene receptor
used for asthma, especially aspirin induced asthma |
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Expectorants
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Guaifenesin (Robitussin)
N-acetylcysteine |
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Guaifenesin
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aka robotussin
removes excess sputim but large doses needed done not suppress cough |
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N-acetylcysteine
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mucolytic
used to loosen mucous plugs n CF patients also antidote for acetaminophen OD |
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Acetazolamide: MOA, uses, AEs
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carbonic anhydrase inhibitor causes HCO3 secretion/diuresis
used for glaucoma, urinary alkalinzation, metabolic alkalosis, altitude sickness can cause neuropathy, acidosis, Nh3 toxicity, sulfa allergy |
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Mannitol: MOA, uses, AEs
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osmotic diuresis
used in shock, drug OD, and decreases intracranial/intraocular pressure can cause pulmonary edema, dehydration. not for use with anuria, CHF |
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Furosemide: MOA, uses, AEs
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sulfonamide loop diuretic, inhibits cotransport of Na, K, 2Cl of TALH
used for edema (chf, cirrhosis, nephrotic, pulmonary) htn, hypercalcemia, hypokalemia OH DANG ototoxicity hypokalemia dehydration allergy - sulfa nephritis - intersitial Gout also alkalosis |
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Ethacrynic Acid: MOA, uses, AEs
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phenoxacetic acid derivative (not sulfa) which has essentially same function as furosemide
used for diuresis for patients allergic to sulfa drugs toxicity similar to furosemide |
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Hydrocholothiazide: MOA, uses, AEs
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thiazide diuretic, inhibits NaCl reabsorbtion ni early distal tubule
used for HTN, CHF, hypercaliuria, nephrogenic Diabetes Insipidus can cause hypercalemia, hypokalemia, alkalosis, hyperglycemia, hyperlipidemia, hyperuricemia. also sulfa allergy |
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K+ sparring diuretics
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Spironolactone-competitive aldosterone receptor antagonists at collecting duct
Triamterene/Amiloride- Block Na channel in collecting duct used to treat hyperaldosteronism, K depletion, CHF Hyperkalemia Spironolactone causes gynecomastia, has antiandrogen effects acidosis |
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Toxicity of ACE inhibitors?
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CAPTOPRIL
Cough Angioedema Proteinuria Taste change O=hypotension P=pregnancy problems (fetal renal damage) R=rash I=increased renin L=lower ang II also hyperkalemia avoid with bilateral artery stenosis |
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Uses of ACEI's?
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Hypertension
CHF Diabetic renal disease |
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Naloxone, Naltrexone: MOA, use
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competitive opioid inhibitors
used for opioid overdoses |
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Methadone: MOA, use
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long acting oral opoid
heroin detox or long term maintenance |
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Typical Antipsychotics: ex, MOA, AEs
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haloperidol + "azines" (thioidazine, fluphenazine, chloprazine)
block D2 receptor used for schizophrenia, psychosis, acute mania, Tourette's AE: EPS Dopamine blocking effects (hyperprolactinemia, galactorrhea) Muscarinic blocking effects (dry mouth, constipation, etc) alpha blocking (hypotension) Histamine effects (sedation) Neuroleptic Malignant Syndrome Tarditive Dysenesia thioridazine, chlorporamazine are low potency and have non-neurologic side effects |
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Neuroleptic Malignant Syndrome: symptoms, cause, treatment
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rigidity, myoglobinuria, autonomic instability, hyperpyrexia
toxicity of antipsychotic meds (blocking D2) treat with dantrolene and dopamine agonist |
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Tarditive Dyskinesia
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sterotypic oral facial movements probably due to dopamine receptor sensitization
due to long term antipsychotic use |
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Atypical Antipsychotics: ex, MOA, AEs
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Clozapine, Olanzapine, Risperidone, Quetiapine, Aripiprazole, Ziprasidone
"its not atypical for OLd CLosets to RISPER" block 5HT2 and D receptors used for schizophrenia (both positive and negative symptoms) Olanzapine also good for OCD, anxiety, depression, mania, Tourette's less toxic than typicals, fewer EPS and anticholingergic side effects clozapine can cause agranulocytosis |
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Clozapine: classification, AE
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atypical antipsychotic
agranulocytosis (monitor WBC weekly) |
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Lithium: MOA, use, AE
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mech unclear, possibly inhibition of phosphoinsoitol cascade
mood stabilizer for bipolar Lithium Toxicity's Movement (tremor) Nephrogenic DI HypOthroidism Pregnancy Problems (teratogenic) "LMNOP" |
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Busiprone: MOA, use
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5HT1A agonist
anxiolytic (does not cause sedation, addiction, or interact with alcohol) |
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Type of Antidepressants
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SSRI
Heterocyclic Antidepressants (includes tricyclics) MAOIs |
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SSRIs: ex, MOA, use, AEs
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fluoxetine, sertraline, paroxetine, citalopram
ssri, takes 2-3 weeks to work depression and OCD fewer ae's than TCAs. GI distress Sexual dsyfunction (anorgasmia) "Serotonin Syndrome" (with MAOI) |
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Serotonin Syndrome
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use SSRI together with MAOI or meperidine
hyperthermia muscle rigidity cv collapse |
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TCA's: ex, MOA, uses, AEs
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Imipramine, Amitrptyline, Deipramine, Nortriptyline, Clomipramine, Doxepin, Amoxapine
block NE and 5HT reuptake depression bedwetting (imipramine) OCD (clomipramine) sedation, alpha block effects, anticholingergic effects, "Convulsions, Coma, Cardiotoxicity (arrythmias) resp depression, hyperpyrexia |
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Bupropion: use, ae
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aka Wellbutrin
smoking cessation antidepressant stimulant effects, headache, seizure in bulimics |
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Venlafaxine: use, MOA, AE
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antidepressant and for generalized anxiety disorder
inhibit 5HT, NE, Dopamine reuptake stimulant effects, sedation, nausea, constipation, HTN |
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Mirtazapine: MOA, use
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alpha2 antagonist (increases release of NE and 5HT) and potent 5HT2 and 5HT3 antagonist
antidepressant sedation, increased apetite, wt gain, dry mouch |
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Maprotiline: MOA, use
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Blocks NE reuptake
antidepressant |
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Trazodone: moa, use
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5HT reuptake inhibitor
antidepressant |
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MAOIs: ex, moa, use, ae
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phenelzine, tranylcypromine
nonselective MAOI, causes increased levelos of amine NTs used for atypical depression (mood reactivity, rejection, hypersommnia, anxiety, hypocondriasis, etc) Hypertensive crisis with tyramine ingestion (in many foods, esp cheese wine) and B-agonists. CNS stimulation Serotonin Syndrome (dont use with SSRI or mepridine) |
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Methyphenidate: MOA, Use
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aka ritaline
inceases presynaptic NE vesicular release (like amphetamines) used for adhd |
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AE of methyldopa
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hemolytic anemia
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Heparin: moa,
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catalyzes activity of ATIII, short half life
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What do you monitor with Heparin?
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aPTT (intrinsic pathway)
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What do you monitor with warfarin?
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aPTT (extrinsic pathway)
"the EXpat went to WAR" |
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How can you reverse heparin?
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protamine sulfate (positively charged which binds up neg charged heparin)
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Difference between unfractionated and LMW heparin?
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unfractionated must be given freq or continuously
LMW can be given 1-2x/day, don't need monitoring but are its not easily reversible! (ex=enoxaparin) |
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Lepirudin, Bivalirudin: MOA, uses
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hirudin derivatives
directly inhibit thrombin used for alternative to heparin for patients with HIT |
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Warfarin: moa
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interferes with synthesis and gamma-carboxylation of VitK dept clotting factors: 2, 7, 9, 10, S, C
longer half life, so for chronic anticoagulation follow PT/INR |
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Which anticoagulant do you give for pregnant women?
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heparin!
warfarin crosses placenta and is a teratogen!!! |
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How can you treat warfarin OD?
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IV vitK and fresh frozen plasma
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Thrombolytics: ex, moa, use,
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tPA, streptokinase, urokinase, APSAC
convert plasminogen->plasmin used for early MI or early ischemia stroke |
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How do you treat thrombolytic OD?
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aminocarproic acid!
(inhibitor of fibrinolysis) |
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ASA: moa, use, ae's
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irreversibly inhibits COX-1,2 to prevent conversion of AA to TXA2
no effect on PT or PTT also antipyretic, analgesic, anti-inflammatory, antiplatelet drug can cause gastric ulcers, bleeding, hyperventilation, reye's syndrome, tinnitus |
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Clopidogrel, Ticlopidine: moa, use, ae's
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inhibit platelet aggregation by irreversibly blocking ADP receptors which prevents gpIIb/IIIa expression inhibiting fibrinogen cross-bridging
used for acute coronary syndrome, coronary stenting, and to decrease incidence/recurrence of thrombotic stroke ticlopidine can cause neutropenia |
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Abciximab: moa, use, ae's
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monoclonal antibodies that binds gpIIb/IIIa on activated platelets, preventing aggregation
acute coronary syndrome, percutaneous transluminal coronary angioplasty bleeding, thrombocytopenia |
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Methotrexate: moa, ae's
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S-phase specific antimetabolite. folic acid analog that inhibits DHFR resulting in decreased dTMP and therefore decreases DNA/protein synthesis
ae=myelosuppresion (reversible with leucovorin rescue) macrovesicular fatty change in liver antineoplastic |
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5FU
|
S-phase specific antimetabolite. pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid. this complex inhibits thymidylate synthase, resulting in decreased dTMP and same effects as MTX
used for colon cancer, and other solid tumors, basal cell carcinoma, synergy with MTX myelosuppression, which is NOT reversible with leucovorin, photosensitivity. can rescue with "thymidine" |
|
|
6-MP
|
blocks de novo purine synthesis, activated by HGPRTase
used for leukemias and lyphomas (not CLL or Hodgkin's) bad for bone marrow, GI, liver. metabolized by xanthine oxidase thus increases toxicity with allopurinol |
|
|
Leucovorin
|
folininc acid
given to rescue normal tissue from methotrexate damage |
|
|
Cytarabine
|
inhibits DNA polymerase
AML (antineoplastic) causes leukemia, thrombocytopenia, megaloblastic anemia |
|
|
Cyclophosphamide: Ifosfamide: moa, uses, ae's
|
alkylating agent (requires bioactivation in liver)
NHL, breast, ovarian cancer and immunusuppresion causes myelosuppression, hemorrhagic cystitis (can be partially prevented with mesna) |
|
|
Nitrosureas: ex, moa, use, ae's
|
carmustine, lomustine, semustine, streptozocin
alkyating DNA. requires bioactivation. brain tumors (crosses the BBB) CNS toxicity |
|
|
Cisplatin, Carboplatin: moa, use, ae's
|
act like alkylating agent
testicular, bladder, ovary, lung cancer causes nephrotoxicity and acoustic nerve damage |
|
|
Busulfan: moa, use, ae's
|
alkylates DNA
CML causes pulmonary fibrosis, hyperpigmentation |
|
|
Doxorubicin (Adriamycin), Daunoribicin
|
generates free radicals and noncovalently intercalate in DNA
used for ABVD used for hodgkins and for myelomas, sarcomas, and solid tumors cardiotoxicity, myelosuppresion, alopecia |
|
|
Dactinomycin: moa, use, ae
|
intercalates in DNA
used for wilm's tumor, ewing's sarcoma, rhabdomyomas causes myelosuppresion |
|
|
Bleomycin: moa, use
|
forms free radicals, which cause DNA stand breaks
used for testicular ca, lymphomas, aBvd for hodgkins |
|
|
Hydroxyurea: moa, use,
|
inhibits ribonucleotide reductase, causes decreased DNA synthesis (S-phase specific)
also causes increase in synthesis of HbF used for melanoma, CML, and sickle cell disease! |
|
|
Etoposide: moa, use
|
G2-phase specific inhibition of topo II, and increased DNA degradation
small cell carcinoma of lung, prostate, testicicular cancer |
|
|
Prednisone
|
may cause apoptosis (may even work on nondividing cells)
cancers and immunosuppresion cushing-like effects, immunosuppresion, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis |
|
|
Imatinib (Gleevec): moa, use, ae's
|
bcr-abl tyrosine kinase inhibitor
CML causes fluid retention |
|
|
Vincristine, VInblastine; moa, use, ae's
|
M-phase-specific alkaloids that bind to tubulin and block polymerization of microtubulesso that mitotic spindle cannot form.
lymphomas, wilm's, choriocarcinoma vincristine=neurotoxicity (areflexia, peripheral neuritis, paralytic ileus) vinblastine=bone marrow suppression (Blasts your Bone Marrow) |
|
|
Paclitaxel, other Taxols: moa, use, ae's
|
M-phase-specific agents that bind tubulin and prevent anaphase
used for ovarian and breast cancer causes myelosuppresion and hypersensitivity. |
|
|
H2 Blockers: ex, mech, use, ae
|
reversible block H2 receptors causing decreased H+ secretion by parietal cells in stomach. block BAO
cimididine is potent P450 inhibitor, antiandrogenergic effect, crosses BBB and placenta, decreases GFR the others are safe generally cimitidine, ranitidine, ramotidine, nazatidine....."dine" used for peptic ulcers, gastritis, mild GERD |
|
|
Cimitidine: mech, use, ae
|
reversible block H2 receptors causing decreased H+ secretion by parietal cells in stomach
used for peptic ulcers, gastritis, mild GERD potent P450 inhibitor antiandrogenergic effect crosses BBB and placenta decreases GFR the other H2 blockers are generally safe |
|
|
PPI's: ex, mech, use
|
omeprazole, lansoprazole
irreversibly block H/K/ATPase in stomach parietal cells, blocks both BAO and MAO used for peptic ulcers, gastritis, GERD, Zollinger Ellison Syndrome |
|
|
Bismuth
|
form a polymer coat over ulcer providing physical protection, and allowing HCO3 secretion to reestablish pH gradient in mucous layer
used for traveler's diarrhea and ulcer healing |
|
|
Sucralfate
|
form a polymer coat over ulcer providing physical protection, and allowing HCO3 secretion to reestablish pH gradient in mucous layer
used for traveler's diarrhea and ulcer healin |
|
|
Triple Therapy for H. pylori
|
Metroniazole
Amoxiciliin of Tetracycline Bismuth MAB or MTB |
|
|
Misoprostol: mech, uses, aes
|
PGE1 analog
increases productio/secrtion of gastric mucous barrier decreases gastric acid secretion prevention of NSAID-induced ulcers maintanence of patent ductus arteriosus induce labor can cause diarrhea, abortions |
|
|
Muscarinic antagonists GI effects: ex, mech, use, ae's
|
pirenzepine, propantheline, atropine, etc
block M1 receptors on ECL cells (decrease histamine secretion) and M3 receptors on parietal cells (decreases H+ secretions) used for peptic ulcers can cause tachycardia, dry mouth, difficulty focusing eyes |
|
|
Aluminum hydroxide
|
antacid
can affect absorption, bioavailability, urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying specifically this antacid can cause: constipation hypophosphatemia proximal muscle weakness osteodystrophy seizures "aluminimim of amout of poop" |
|
|
Magnesium hydroxide
|
antacid
can affect absorption, bioavailability, urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying specifically this antacid can cause: diarrhea hypooreflexia hypotension cardiac arrest "Mg=Must Go to the bathroom" |
|
|
Calcium Carbonate: mech, ae
|
antacid
can affect absorption, bioavailability, urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying specifically this antacid can cause: hypercalcemia rebound acid chelate and decrease effectiveness of other drugs |
|
|
Infliximab; mech, use, ae
|
monoclonal Ab to TNF
used for Crohn's Rheumatoid arthritis infectoins, esp resp (TB) |
|
|
Sulfasalazine: mech, use
|
combo of sulfapyridine (antibacterial) and mesalamine (anti-inflammatory)
activated by colonic bacteria used for UC and CD |
|
|
Ondansetron: mech, use, ae
|
5HT3 antagoinsit powerful central acting antiemetic
postop and chemo vomiting can cause headache and constipation |
|
|
Cisapride: mech, use, ae
|
acts on 5HT receptors to increase ACh release at myenteric plexus causing increased esophageal gastic, duodenal tone causing improved transit time , including through colon. (prokinetic)
serious side effects and no longer used torsades with erythromycine, ketoconazole, nefazodone, fluconazole |
|
|
Metoclopramide: mech, use, ae
|
D2 receptor antagonist
causes increased resting tone, contractility, LES tone motility does not increase colon transit time used for diabetic and post-surgery gastroparesis can cause parkinsonism, restlessness, drowsiness, fatigue, depression, nausea, diarrhea drug interactions with digoxin and diabetic agents! contraindicated with small bowel obstruction |
|
|
ex of opioid analgesics
|
morphine
fentanyl codeine heroine methadone meperidine dextromethorphan |
|
|
uses of opoids
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphyonxylate) acute pulmonary edema maintance for addicts (methadone) |
|
|
ae's of opioids
|
addiction
respiratory depression constipation miosis (pinpoint pupils) cns depression |
|
|
how can you treat opiod toxicity>
|
naloxone, naltrexone
opioid receptor antagonists |
|
|
phenytoin: moa, uses
|
Na channel inactivation
used for partial (simple and complex) and tonic clonic and propylaxis for status epipeticus 1st line for prophylaxis 1st line for tonic clonic (along with valproic acid and carbamazepine) |
|
|
carbamazepine; moa, uses
|
Na channel inactivation
same uses as phenytoid except not used for prophylaxis for status epilepticus so its good for all types of partial and 1st line for tonic clonic also used for trigeminal neuralgia |
|
|
Lamotrigine: moa, uses
|
blocks voltage gated Na channels
same uses as carbamazepine except its not a 1st choice for tonic clonic so works for all partial and tonic clonic |
|
|
Gabapentin: moa, uses
|
increases GABA release
same as lamotrigine but also can be used for peripheral neuropathy all partial tonic-clonics |
|
|
Topiramate: moa, uses
|
blocks Na channels and increases GABA action
all partial tonic clonic |
|
|
Phenobarbital: moa uses
|
increase GABA actions
all partial tonic clonic first line for pregnant women and children! |
|
|
Valproic Acid: moa, uses, aes
|
Na channel inactivation and increases GABA concentration
used for: all partial tonic clonic (1st choice, along with phenytoin and carbamazepine) absence myoclonic can cause GI distress, rare but fatal hepatotoxicity (measure LFTs), neural tube defects, tremor, wt gain, dont use with pregnancy |
|
|
Ethosuximide: moa, uses, ae
|
blocks thalamic T-type Ca channels
used for absence seizures (1st line) fatigue, GI distress, headaches, steven-johnson's syndrome |
|
|
Benzodiazepines for epilepsy: moa, uses, aes
|
increase GABA action by increasing freq of Cl- channel opening
1st line for acute status epilepticcus eclampsia seizures (although MgSo4 is 1st choice) can cause sedation, tolerance, dependence |
|
|
Treatment of Absence seizures
|
1st choice= ethosuximide
also valproic acid |
|
|
Treatment of epilepsy in preg women?
|
1st choice = phenobarbital
|
|
|
Treatment of epilepsy in children?
|
1st choice = phenobarbital
|
|
|
Treatment of Trigeminal neuralagia?
|
carbamezepine
|
|
|
Treatment of Tonic Clonic seizures?
|
1st choice = valproic acid, carbamazepine, phenytoin
|
|
|
Treatment of acute status epilepticcus?
|
1st line = benzos
|
|
|
Prophylaxs for status epilepticcus?
|
phenytoin
|
|
|
Treatment of eclampsia seizures?
|
1st choice = MgS04
also benzos work |
|
|
Ae's of phenytoin
|
gingival hyperplasia
nystagmus diplopia ataxia sedation hirutism megaloblastic anemia teratogenesis SLE-like syndrome induces CYP450 |
|
|
Barbiturates: ex, moa, uses, aes
|
phenobarbital, pentobarbital, thiopental, secobarbital
increase duration of Cl channel opening therefore increasing action of GABA used for anxiety, seizures, insomnia, inductinon of anesthesia (thiopental) can cause dependnce, cns depression, resp depresison, cv depression, induces cyp450 |
|
|
Benzodiazepines: ex, moa, uses, aes
|
diazepam, lorazepam, traizolam, temazepam, oxazepam, midazolam, chlordiazepoxide, alprazolam
increase frequency of Cl channel opening thus facilitating GABA action used for anxiety, spasticity, status epilepticus, detox of alochol, night terrors, sleepwalking can cause dependence, cns depression (additive with alcohol). less risk of resp depression/coma than barbiturates |
|
|
How can you treat benzo OD?
|
flumazenil (comp antagonist at GABA receptor)
|
|
|
How can you treat barbiturate OD?
|
symptom mang (assist resp, increase BP)
|
|
|
General Principles of anesthetics
|
for drugs to work on cns they must either be lipid soluble or transported
drugs with low blood solubility have rapid induction/recovery times drugs with high lipid solubiliy have increased potency potency = 1/MAC (min alv concentration) |
|
|
Inhaled Anesthetics
|
halothane, Nitrous Oxide, "fluranes"
work by unknown mech cause myocardial depression, resp depression, nausea/emesis, increased cerebral blood flow (lower cerebral metabolic demand) halothane is hepatotoxic methyoxyflurane and enflurane is nephrotoxic can rarely cause malignany hyperthermia proconvu |
|
|
IV Anesthetics
|
Barbiturates
Benzos Ketamine Opiates Propofol B B King on Opiates Proposes Foolishly |
|
|
Thiopental use
|
induction of anesthesia and short procedues
its a barbiturate with high potency and rapid entry into brain |
|
|
Midazolam use
|
endoscopy or adjuct with inhaled anesthetics
benzo |
|
|
Ketamine
|
"arylcyclohexylamine"
pcp analog that acts as a dissociative anesthetic (IV) cv stimulant can cause disorientation, bad dreams, increased cerebral blood flow |
|
|
Propofol
|
IV anesthetic used for rapid induction and short procedures
but with less post-op nausea than thiopental |
|
|
Local anesthetics
|
esters=procaine, cociane, tetracain
amides=iidocaine, mepivacaine, bupivicapine (amides have 2 I's) block Na channels by binding to the inner portion of the channel (preferentially bind to activated channels so most effective in rapidly firing neurons) used for minor surgical procedures, spinal anesthesia can cause cns excitation! cv toxicity (bupivicaine), htn, hypotention, arrhythmias (cocaine) |
|
|
Order of sensation loss in local anesthetic use
|
pain->temp->touch->pressure
|
|
|
Characteristics of local anesthetics on different nerve types
|
works better on small diameter and myelinated fibers
but small outweighs myelination |
|
|
What's different about using local anesthetics in infected tissue?
|
alkaline anesthetics are charged and cant pentrate membrane well when tissue is infected (acidic) so use MORE
|
|
|
Succinylcholine: mech, use, ae
|
depolarizing neuromuscular blocking drug
used for muscle paralysis for surgery can cause hypercalcemia and hyperkalemia |
|
|
Cholinesterase Inhibitors
|
neostigmine, pyridostigmine, physostigmine, echotihophate, edrophonium
|
|
|
Nondepolarizing Neuromuscular blocking drugs: ex, mech
|
all the curoniums, curarines, etc
competitive block of nicotinic ACh receptors |
|
|
Dantrolene: mech, use
|
treatment of malignant hyperthermia
treatment of neuoleptic malignant syndrome prevents release of Ca from SR of skeletal muscle |
|
|
Malignant Hyperthermia: cause, treatment
|
caused by concomitant use of inhalation anesthetics (except nitrous oxide) and succinylcholine
treat with dantrolene |
|
|
Treatment of Parkinson's
|
Bromocriptine, Pramipexole, Ropinirole
Amadtadine L-Dopa, Carbidopa Selegiline, Entacapine, Tolcapone Benztropine |
|
|
Amantadine: mech, use
|
antiviral used for influenza A and rubella
also used for PD b/c increased dopamine release |
|
|
Selegiline: mech, use
|
selective MAO Type B inhibitor, prevent dopamine breakdown
used for PD |
|
|
Entacapone, Tolcapone
|
COMT inhibitors prevent dopamine breakdown
used for PD |
|
|
Benztropine, mech, use
|
antimuscarnic
used to prevent tremor and rigidity but with little effect on bradykinesia in parkinsons |
|
|
L-Dopa: mech, use
|
increase levels of dopamine in brain, by crossing BBB and then being converterd into dopamine by dopa-debarboxylase in cns
used for parkinsons |
|
|
Carbidopa; mech, use
|
peripheral decarboxylase inhibitor which is given with L-Dopa to prevent peripheral side-effects and increase its bioavailabiltity
|
|
|
Sumatripan: mech, use, ae
|
5HT1D agonist which causes vasoconstriction
used for migraines, cluster headaches can caused coronary spasms, tingling, hypertensive emergencies |
|
|
difference between competitive and noncompetitive inhibitors
|
competitive don't change Vmax but they do increase Km
noncompetitive decrease Vmax but dont change Km |
|
|
Vol of Distribution (Vd)
|
drug amt in body/plasma concentration
|
|
|
Drug Clearance (CL)
|
rate of elimination/plasma concentration
=Vd*Ke (elimination constant) |
|
|
t1/2
|
=(0.7*Vd)/CL
reaches ss after 4 half lives (about 94% of ss) |
|
|
Loading Dose
Maintenance Dose |
Loading Dose=(Cp*Vd) /F
Maintenance Dose=Cp*CL/F in patients with renal/hepatic problems, loading dose remains unchanged but maintenance dose is decreased |
|
|
Drugs with zero order elimination
|
PEA
phenytoin ethanol ASA (at high doses) |
|
|
Phase I vs Phase II
|
phase I is reduction, oxidation, hydrolysis, done by CY 450
phase II is acetylation, glucornidation, sulfation |
|
|
Therapeutic Index
|
median toxic dose/median effective dose
LD50/ED50 "TILE" |
|
|
nicotinic vs muscarinic ACh receptor mechanisms
|
nicotinic is ligand gated Na/K channel
muscarinic is G-coupled |
|
|
Metyrosine
|
blocks Tyrosine conversion to Dopamine
|
|
|
Bethanechol: moa, use
|
cholinergic
used for postop/neurogenic bladder and bowel B for Bladder and Bowels "call Beth Ann for to activate bowel/bladder" |
|
|
Carbachol: moa, use
|
cholinergic
used for glaucoma, pupillary contraction |
|
|
Pilocarpine: moa, use
|
cholinergic
stimulates sweat, tears, saliva |
|
|
Methacholine
|
cholinergic
used for challenge test to diagnose asthma |
|
|
Anticholinesterases
|
"-stigmines" plus echothiophate
|
|
|
Neostigmine: moa, uses
|
postop/neurogenic bladder, bowel, myasthenia gravis, reversal of NMJ block (post op)
anticholinesterase with no CNS penetration! NeO = NO cns |
|
|
Pyridostigmine: moa, uses
|
used for myasthenia gravis
anticholinesterase, long acting no cns penetration |
|
|
Edrophonium: moa, use
|
anticholinesterase
very short acting, used for myasthenia gravis diagnosis |
|
|
Physostigmine: moa, use
|
anticholinesterase
does cross bbb used for glaucoma and atropine OD "phys for eyes" |
|
|
Echotiophate: moa, use
|
anticholinesterase used for glaucoma
|
|
|
Choline poisoning
|
Dumbbless
D=diarrhea/abdominal cramping U=urination M=miosis B=bronchospasm B=bradycardia E=excitation of skeletal muscle and CNS L=lacrimation S=sweating S=salivation |
|
|
antidote to anticholinesterase poisoning
|
atropine plus pralidoxime (regnerates active cholinesterase)
|
|
|
Atropine
|
muscarinic antagonist
|
|
|
Benztropine
|
muscarninc antagnoist used for parkinson's disease
"park my benz" |
|
|
Scopolamine
|
muscarinic antagonist use for motion sickness
|
|
|
Ipratropium
|
muscarinic antagonist used for as asthma, copd
|
|
|
methscopolamine
|
muscarinic antagnoist used to reduce bladder spasms in cystitis
|
|
|
oxybutynin
|
muscarinic antagnoist used to reduce bladder spasms in cystitis
methscopalamine oxybutynin glycopyrrolate |
|
|
glycopyrrolate
|
muscarinic antagnoist used to reduce bladder spasms in cystitis
|
|
|
Pirenzepine
|
muscarinic antagonist used to treat peptic ulcers
|
|
|
Propantheline
|
muscarinic antagonist used to treat peptic ulcers
|
|
|
Glaucoma Drugs
|
a-agonists: epi, brimonidine
B-blockers: timolol, betaxolol, carteolol diuretics: acetazolamide Cholinomimetics: pilocarpine, carachol, physostigmine, echotiophate Porstaglandin: Latanoprost (PGF2a) |
|
|
Atropine toxicity
|
Hot as a Hare
Dry as a Bone Red as a Beet Blind as a Bat (mydriasis) Mad as a Hatter |
|
|
Hexamethonium
|
nicotinic antagonist used to prevent vagal reflex responses to changes in bp. (ex: prevents refelx bradycardia caused by NE)
|
|
|
Epi
|
non-specific adrenergic, although low doses are selective for B1
|
|
|
NE
|
a1, a2>B1 agonist
|
|
|
Isoproterenol
|
B-agonst, nonselective
|
|
|
Dobutamine
|
B1>B2 agonist, inotropic not chronotropic
|
|
|
Phenylephrine
|
a1>a2 agonist
|
|
|
Albuterol
|
B2>B1 agonist
|
|
|
Terbutaline
|
B2>B1 agonist used to reduce premature uterine contractions
|
|
|
Amphetamine
|
releases stored catecholamines
|
|
|
Ephedrine
|
releases stored catecholamines
|
|
|
Cocaine
|
cathecholamine uptake inhibitor
also blocks Na channels |
|
|
Selective B2 agonists
|
Metaproterenol
Albuterol Salmeterol Terbutaline Ritodrine "mastr" |
|
|
non selective a blockers
|
phenoxybenzamine
phentolamine |
|
|
a1 selective blockers
|
prazosin
terzosin doxazosin |
|
|
a2 selective blockers
|
mirtazapine used for depression
|
|
|
Gout treatment
|
Uricosuric (probenicid, sulfinpyrazone)
xanthine oxidase inhib (allopurinol) |
|
|
Drugs that can cause SLE-like syndrome
|
Hydralazine
INH Procainamide Phenytoid HIPP |
|
|
Drugs with photosensitivity
|
Sulfonamide
Amiodarone Tetracycline SAT for photo |
|
|
Drugs that can cause tendonitis, tendon rupture
|
fluoroqunilones
|
|
|
Drugs that can cause gout
|
furosemide
thaizide |
|
|
drugs that can cause osteoporosis
|
corticosteroids
heparin |
|
|
Drugs that can cause acute cholestatic hepatitis
|
macrolides
|
|
|
drugs that can cause hepatic necrosis
|
Halothane
Valproic Acid Acetaminophen |
|
|
Drugs that cause Hepatitis
|
INH
|
|
|
Drugs that cause hemolysis in G6PD def?
|
INH
Sulfoamides Primaquine ASA Ibuprofen Nitrofuratoin "IS PAIN" |
|
|
Drugs with atropine-like side effects (anti-muscarinic)
|
TCAs
|
|
|
Drugs that aplastic anemia
|
chloramphenicol
benzene nsaids PTU Methimazole |
|
|
Drugs that cause agranulocytosis
|
clozapine
carbamezepine colchicine PTU methimazole |
|
|
Drugs with nephrotoxicity
|
aminoglycosides, loops, cisplatinin, polymixins
|
|
|
P450 inducers
|
Quinidine
Barbiturates Phenytoin Rifampin Griseofulvin Carbamazepine St. John's Wart Queen Barb takes Phenphen and Refuses Greasy Carb Shakes |
|
|
P450 inhibitors
|
Isoniazin
Sulfonamide Cimeidine Ketoconazole Erythromycin Grapefruit Juice "Inhibitors Stop Cyber Kids from Eating Grapfruit |
