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194 Cards in this Set
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Dorzolamide/acetazolamide |
CA inhibitor --> topical to reduce intraocular pressure sometimes brain edema |
|
Mannitol |
osmotic diuretic (IV) to relieve brain edema oral: osmotic diarrhea to rid toxins |
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Amiloride/triamterene |
ENaC inhibitors: blunt hypokalemia/alkalosis from other diuretics Li induced nephrogenic diabetes insipidus |
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Spironolactone |
Competitive inhibitor of aldosterone: blunt hypokalemia/alkalosis from other diuretics severe CHF (less myocardial remodeling) edema due to hepatic cirrhosis |
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Furosemide |
edema (liver, renal or CHF) relieve pulmonary congestion in CHF acute hypercalcemia, hyperkalemia, toxic OD of halogens acute renal failure |
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Thiazides (hydrochlorothiazide and chlorthalidone) |
HTN (decrease TPR) --> prescribe for early HTN add to other anti-HTN drugs (lisinopril) for moderate HTN idiopathic hypercalcuria with kidney stones Li-induced nephrogenic diabetes insipidus |
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Enalapril/lisinopril |
ACE inhibitor prodrugs: decrease TPR w/o increasing HR HTN CHF (slow ventricular dilation and remodeling) LVD after MI (acute MI) Diabetic nephropathy (increase RBF+natriuresis) |
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Aliskiren |
Renin inhibitor: HTN (use with thiazide) |
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Losartan/valsartan |
AT-1 antagonists: HTN in patients with ACEI-mediated cough CHF (block cardiac remodeling and reduce cardiac work) Acute MI |
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Valsartan + sacubitril |
CHF block Ang II, enhance ANP |
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B-blockers |
HTN (second line-use for complicated HTN) Cardiac arrhythmia Angina Acute MI ** (first line) HF Thyrotoxicosis |
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Propranolol |
non-selective, extensive first pass metabolism CHF, acute MI, angina, arrhythmia |
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Metoprolol |
beta-1 SR formula for CHF |
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Atenolol |
beta-1 (no first pass) CHF, acute MI, arrhythmia, angina |
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Pindolol |
beta-1,2,ISA: initially increase HR (less ADEs) *NOT for use in MI |
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Labetolol |
alpha,beta,ISA: HTN in pregnant women less cardiac uses |
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Carvedilol |
alpha-1,beta: CHF (reduces lipid peroxidation by radicals and reduces SM mitogenesis) |
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Esmolol |
ultra short beta-1: IV supraventricular arrhythmia acute HTN acute MI |
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Sotalol |
beta + K: anti-arrhythmia |
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Nebivolol |
beta-2 agonist: HTN |
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Ivabradine |
If inhibitor: CHF pts that can't use b-blockers (HR > 70) --> reduce pacemaker activity by blocking phase 0 of SA node |
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Methyldopa |
central sympatholytic (a-2 agonist): HTN during pregnancy |
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Clonidine |
central sympatholytic (a-2 agonist): HTN blunt SS reflex due to VDs *NOT for depressed patients |
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Prazosin |
a-1 antagonist: HTN *NOT for use as monotherapy due to hypotensive response (add b-blocker or diuretic) BPH urinary issues (tamulosin) |
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Nifedipine |
DHP CCB: HTN *May cause baroreceptor reflex mediated hypotension |
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Amlodipine |
DHP CCB: HTN and CHF (LVD) |
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Nicardipine/clevidipine |
short acting DHPs: IV for emergency HTN |
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Nimodipine |
DHP CCB: subarachnoid hemorrhagic stroke |
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Verapamil |
non-DHP CCB: angina (decrease FOC by blocking Ca influx) anti-arrhythmia: SVT and prevent spread with A-fib suppress EADs and DADs |
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Diltiazem |
non-DHP CCB: angina anti-arrhythmia: SVT and prevent spread of A-fib suppress EADs and DADs |
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Nitroglycerin/isosorbide dinitrate |
ISCHEMIA ISSUES: classic angina (ATH obstruction) variant angina (transient spasm) unstable angina (increased tone or clots) CHF recovery from MI |
|
Sildenafil |
PDE5 inhibitor: erectile dysfunction pulmonary hypertension** (leads to RVF) |
|
Ranolazine |
Late Na current blocker (INaL): classic angina for patients still symptomatic after other treatments (reduce Ca, so reduce EDV to improve coronary flow) Use with nitrates/b-blockers/CCBs to increase exercise duration (not lifespan) |
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Bosantan |
endothelin receptor blocker (ET-1): arterial pulmonary HTN |
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Hydralazine |
VD Triple combo w/b-blocker and diuretic: complicated HTN (rare to use) With nitrate: CHF in pts that can't use standard therapy (ACEI, b-blocker, loop diuretic) |
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Minoxidil |
VD (activate K channel on SM to relax) Triple combo w/b-blocker and diuretic: complicated HTN unresponsive to other agents **Rogaine - use for male baldness (topical) |
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Sodium nitroprusside |
VD (generates NO) - continuous IV EMERGENCIES (that need reduced pre/afterload) Acute aortic dissection Cardiogenic shock Induce controlled hypotension for anesthesia |
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Digoxin |
cardiac glycoside (increase contractility): blocks Na/K ATPase (accumulate Na and Ca) CHF |
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Dobutamine |
sympathomimetic amine = beta agonist (significant increase in contractility and CO) short-term for acute cardiac decompensation acute HF or MI diagnose coronary obstructions |
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Dopamine |
severe CHF with compromised renal function high dose: cardiogenic/septic shock (acts on a-adr to increase TPR) |
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Procainamide |
Na channel blocker (state-dep): anti-arrhythmia due to decrease in diastolic depol - slow SA conduction and increase threshold atrial and ventricular arrhythmia sustained ventricular arrhythmia after MI |
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Esmolol/sotalol |
most effective anti-arrhythmics to increase lifespan suppress EADs and DADs prevent vent tachycardia in A-fib prevent recurrence of SVT **avoid in Wolf-White |
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Amiodarone |
K channel blocker (inhibit repole of myocardium): anti-arrhythmic --> increase refractory period and decrease re-entry restore sinus rhythm in atrial tachycardia recurrent vent tachycardia and fibrillation |
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Verapamil/diltiazem |
suppress EADs and DADs reentrant SVT reduce risk of vent tachycardia with A-fib **avoid with Wolf-White |
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Adenosine |
SVT (IV only) inhibits SA, atrial and AV conduction |
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Magnesium sulfate (IV only) |
digoxin related arrhythmia drug induced torsades de pointes arrhythmia due to hypomagnesia |
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Statins |
inhibit HMG-COA reductase to block cholesterol biosynthesis in liver (accounts for most chol) induce up-regulation of LDL-R (main action to reduce cholesterol) directly lower risk of MI/stroke (plaque stability, improved vascular tone, reduced inflammation and coagulation) |
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Alirocumab/evolucumab |
PCSK9 inhibitors (bind and remove from circulation to prevent LDL-R degradation) to use in heart patients who LDL-C levels are not sufficiently lowered by statins raise LDL-R levels |
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Lovastatin/simvastatin |
lactone ring side group must be cleaved in liver to activate - prodrugs |
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Statins + bile acid resins |
reduced liver cholesterol and increased LDL-R uptake 20-30% more LDL-C lowering |
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Statins + ezetimide |
decrease LDL-C by up to 60% and better mortality and morbidity |
|
Statin combos |
used when insufficient LDL-C lowering with statins alone, or for patients with statin side effects (myopathy) that require lower doses use statin to enhance other drugs because on their own they will be compensated by up-regulation of cholesterol pdtion |
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Statins + fibrates |
patients with high TGs and LDL-C avoid gemfibrizol, or half dose of statins |
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Statins + niacin |
patients with high LDL-C and low HDL-C (niacin improves HDL levels) |
|
Ezetimibe |
blocks absorption of cholesterol from diet (inhibits intestinal transporter NPC1L1) Vytorin = statin + ezetimibe --> enhance LDL reduction |
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Cholestyramine/colestipol |
form insoluble gels in intestine to bind and rid bile acids in feces, forcing more cholesterol to be used for bile acid synthesis must give statin before BAS or the resin will sequester statin as well as cholesterol |
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Niacin |
improve all aspects of lipid profile bind GPCR in adipose tissue to decrease release of FFAs from stored TGs (reduces VLDLs and thus LDLs). stabilizes apoA1 on HDLs combo with statins when HDL low |
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Gemfibrozil/fenofibrate |
Fibrates: lower triglycerides, may raise HDL activate PPARa to lower liver release of VLDL use with statin for high TG levels patients with high TGs and risk of pancreatitis |
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Fomepizole |
blocks ADH metabolism in case of methanol overdose (stop formation of formaldehyde) |
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Disulfiram |
blocks aldehyde dehydrogenase (ALDH) from metabolizing acetaldehyde to acetate Adversive: causes unpleasant ADEs associated with alcohol use so that patients will decrease drinking |
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Flunitrazepam (rohypnol), GHB, GBL |
"roofies" and other date rape drugs |
|
Alcohol |
CNS excitation, followed by depression with state dependent learning (differentiated cognitive state) and labile affect. Anterograde amnesia, nystagmus. myocardial depression, cutaneous VD, HDL elevation, diuresis, increased ACTH/cortisol/oxytocin, decreased FSH/LH |
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Abstinence syndrome |
~6-8 hours after last use, withdrawal due to dependence craving, hyperirritability, anxiety, tremor, insomnia, nausea, sweating, hallucinations, seizure can manage by substitution therapy (BZs that cross-react), symptomatic therapy (treat seizures), or supportive (NSAIDs and thiamine) |
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Delirium tremens |
~2-3 days after last use confusion, disorientation, agitation, hyperpyresis, dehydration |
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Naltrexone |
anti-craving opioid antagonist ("depo") used to decrease use and desire of alcohol |
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Acamprosate |
anti-craving NMDA antagonist/GABA agonist used to decrease use and desire for alcohol |
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Cocaine HCl |
powder (diluents) can be used to cause vasoconstriction/local anesthesia, or to snort (inhale) or inject |
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Cocaine free base |
crack --> use to smoke |
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Norcocaine |
active cocaine metabolite formed by N-demethylation toxic |
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Cocaethylene |
active metabolite formed from use of EtOH + cocaine toxic: seizures, immune system depression, hepatotoxicity |
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Cocaine |
euphoria, dysphoria, hallucinosis, psychosis profound CNS excitation, leading to desynchronization (with OD) increase HR, BP, RR, temp, SM tone, eye dilation, seizures, decrease appetite |
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5-FU |
adjuvant chemotherapy treatment for cancer, or used for advanced cancer (colon, breast, head/neck,stomach,pancreas) (post-surgery) --> increases long-term survival interferes with TS, incorporates into RNA/DNA |
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Leucovorin |
activated folic acid used with 5-FU to increase binding of 5-FU to TS, therefore increasing efficacy (tertiary complex forms to block U-->T) also increases toxicity |
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Uridine triacetate |
"antidote" to decrease toxicity of 5-FU overcome 5-FU block of pathway to make T, compete for RNA incorporation |
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Dipyramidole |
increase efficacy of 5-FU if given before treatment by blocking thymidine into cell, or decreases efficacy if given after by increasing 5-FU clearance |
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Ethynyluracil |
inhibits DPD activity to allow increased half-life of 5-FU (make it oral and eliminated totally by urinary excretion- check kidney function!) useful in rats/mice, not humans |
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Capecitabine |
5-FU prodrug that is activated in liver and then at tumor site to make 5-FU orally active refractory breast cancer |
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Tegafur |
5-FU prodrug activated in liver (make 5-FU orally active) |
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TAS-114 |
inhibits DPD and dUTPase (enzyme that cleaves 5-FU UDP) given with capecitabine/5-FU to increase its activity by decreasing metabolism |
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TAS-102 |
cytotoxic trifluridine + tipiracil --> inhibit thymidine phosphorylase and kill cells when incorporated into DNA use for patients that have failed all other drugs |
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S-1 |
tegafur + DPD inhibitor + 5-FU phos inhibitor |
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Irinotecan |
inhibits TS activity to increase efficacy of 5-FU in chemotherapy (even in patients with high TS levels) |
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FOLFOX |
cycles of 5-FU/leucovorin/oxaliplatin infusion to determine target range of 5-FU and to individualize dosage (and minimize toxicity) |
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Opiates (heroin, oxycodone, meperidine, methadone) |
Euphoria -> sedation -> analgesia depressed respiration (less CO2 response) constipation (increased resting tone of GI) miosis nausea and emesis (CTZ stimulation) reduced BP -> orthostatic hypotension cerebral vasodilation |
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Naloxone |
opioid antagonist for use in toxicity/OD atomizer |
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Methadone |
used for 'detox' during opioid withdrawal -> cross dependence allows lessening of abstinence syndrome symptoms |
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Clonidine + acetaminophen |
used for opioid withdrawal to 'detox' must decrease dose of 'detox' by 25% each day until withdrawal is over |
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Buprenorphine + naloxone (suboxone) |
long-term management for opioid withdrawal |
|
Methylnaltrexone and Naloxegol |
opioid constipation |
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Cannabinoids |
anticonvulsant, sedative, antimicrobial, decrease neuropathic and inflammatory pain |
|
Dronabinol |
oral cannabinoid used in wasting disease to increase appetite |
|
THC |
intoxication syndrome: well being, euphoria, relaxation, intensified sensory perception, lapse of attention, poor concentration, anterograde amnesia - amotivational high dose = anxiety, dysphorai, panic, delusions state dependent learning (like EtOH) hypothermia, stimulated appetite, tachycardia, postural hypotension, decreased sex hormones, impaired immunity, suppress nausea, suppress REM sleep, decrease intraocular pressure (good for glaucoma) |
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Glucagon |
reversal of diabetic coma due to insulin OD when oral glucose cannot be administered |
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Soluble/regular insulin |
monomeric form for rapid absorption (at meals) |
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NPH insulin |
intermediate acting, mixed with protamine |
|
Lente/ultralente insulin |
slow absorption (bound to zinc) for basal levels or nighttime |
|
Lispro/aspart insulin |
most soluble, rapid-acting forms (no self-association due to mutations) |
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Glargine insulin (LANTUS) |
peakless insulin, ultra long acting hexamer form to precipitate and leach away from site of injection for steady baseline all day |
|
Metformin (biguanide) |
first-line anti-diabetic for T2DM oral, to act on liver, mm, gut to reduce GNG and insulin resistance (activate AMPK) no hypoglycemia or weight gain risk |
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Sulfonylureas: glimepiride, glipizide, glyburide |
bind ATP sensitive K channel to block its conductance and allow depol of b-cell to increase insulin secretion (insulin secretagogue) |
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Glitinides: repaglinide + nateglinide |
insulin secretagogues - close ATP sensitive K channel to increase insulin secretion rapid acting and short duration (oral at mealtime - decreases hypoglycemia risk compared to sulfonylureas) |
|
TZDs/glitazones: rosiglitazone + pioglitazone |
second line only (ADEs) to reduce insulin R by binding PPARy on adipose cells to suppress resistin release |
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Exenatide |
GLP-1 homolog (Gila monster) -2x/day injection causes increase in insulin release and blunt post-prandial surge-> insulin secretagogue |
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Liraglutide |
DPP-4 resistant GLP-1 (1x/day injection) to increase insulin release and blunt post-prandial surge -> insulin secretagogue significant weight loss (blunts appetite by delayed gastric emptying) --> approved for obesity |
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Sitagliptin |
DPP-4 inhibitor to increase half-life and action of endogenous GLP-1 (use when diet/exercise and metformin fail) oral, once daily |
|
Acarbose/miglitol (a-glucosidase inhibitors) |
reduce intestinal absorption of glucose by slowing degradation of starches and sucrose --> not very effective, use in combo with other anti-diabetics for controlling post-prandial spikes |
|
SGLT2 inhibitors: dapagliflozin + canagliflozin |
inhibit renal glucose reuptake transporter SGLT2 to increase glucose excretion in urine and lower blood glucose combo with metformin |
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Orlistat |
long-term weight loss (modest 4-7lbs) pill (take with meals) inhibits intestinal lipases that hydrolyzes TGs so fats are not absorbed |
|
Lorcaserin |
appetite suppressing weight loss drug (selective 5-HT2c agonist) for obese patients with co-morbidities promotes POMC production to promote satiety oral - ~10 lbs |
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Phentermine/topiramate |
weight loss drug for obese pts with co-morbidities (stimulant + anticonvulsant) appetite suppression |
|
Bupropion/naltrexone |
weight loss drug for obese pts with co-morbidities to cause appetite suppression --> patients with BMI > 30 or BMI > 27 w/CHD/stroke risk (high LDL, high BP, diabetes) bupropion also for smoking cessation and antidepressant (weak NDRI) naltrexone also for opioid/alcohol dependence |
|
Levothyroxine |
synthetic T4 for hypothyroidism (due to Hashimoto's auto-immune thyroid impairment or destruction of thyroid) once daily pill congenital thyroid deficiency - prevent cretinism |
|
Liothyronine sodium |
synthetic T3 (multiple doses per day) for hypothyroidic coma |
|
Thioureylenes |
methimazole and propylthiouracil = anti-thyroid drugs to block the production of thyroid hormone (inhibit tyrosyl iodination on thyroglobulin) competitive inhibitor of thyroperoxidase |
|
Methimazole |
once daily dosing for hyperthyroidism (oral) --> first line |
|
Propylthiouracil |
inhibits peripheral de-iodination of T4 --> use for acute thyroid storm hyperthyroidism (long-term stabilization) |
|
High dose iodide |
relatively rapid inhibition of thyroid hormone release to treat hyperthyroidism --> not effective long term thyroid storm management pre-op for thyroidectomies to reduce size and vascularity of gland |
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Propranolol for thyrotoxicosis |
use during lag for thioureylenes to be effective (2-4 months) |
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Tamoxifen |
anti-estrogen used for estrogen receptor-positive breast cancer patients requiring adjuvant therapy after surgical removal of the tumor pre or post-menopausal women |
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Diethylstilbestrol (in males) |
synthetic estrogen used in males for palliative treatment of prostate cancer acts on hypothalamus (negative feedback) to depress GnRH and subsequent androgen release |
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Leuprolide (in males) |
GnRH agonist that is used with an antiandrogen (for initial upregulation period) to downregulate GnRH and androgen release to treat prostate cancer |
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Postmenopausal HRT estrogen therapy |
estradiol, estradiol salts (IM), ethinylestradiol (oral), diethylstilbestrol osteoporosis, hot flashes, atrophic vaginitis give with progesterone to decrease endometrial hyperplasia and cancer risk dose cyclically so that bleeding will occur during withdrawal (if occurs) to differentiate from endometrial cancer |
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Progestin alone |
"minipill" for contraception less efficacy and more irregular cycle, so less used |
|
Diethylstilbestrol (in females) |
"morning after pill" - use within 72 hours of coitus synthetic estrogen that changes cervical mucus and endometrium to decrease implantation |
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Norgestrel/ethinyl estradiol (preven) |
emergency contraception within 72 hours of coitus |
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Mifepristone (RU-486) |
single 600mg dose = postcoital contraceptive antiprogestin that competitively inhibits progesterone and glucocorticoid receptors and can cause early termination of pregnancy (with PGs) --> abortifacent admin in follicular phase --> prevent ovulation admin in luteal phase --> menstrual bleeding (block progesterone action on uterus) |
|
Lipopristone/ZK98734 |
mifepristone analog that may be used for progesterone sensitive tumors |
|
Progestins |
medroxyprogesterone, norethindrone, norgestrel, ethynodiol oral contraception/HRT (with estrogen) to decrease cancer risk dysfunctional uterine bleeing dysmenorrhea premenstrual syndrome endometriosis metastatic endometrial carcinoma |
|
Norgestrel |
'plan B' progestin used for emergency contraception within 72 hours of coitus subcutaneous implant capsules that slowly release progestin for contraception |
|
Oral contraceptives |
progestin + estrogen is best inhibit ovulation (suppress both FSH and LH) 99-100% effective in preventing pregnancy |
|
Tamoxifen |
estrogen receptor competitive antagonist (anti-estrogen) + partial agonist breast cancer PRE-MENOPAUSAL |
|
Clomiphene |
partial agonist/competitive antagonist of estrogen receptor (anti-estrogen) infertility: enlarges ovaries and blocks the estrogen receptor in the hypothalamus to stop estrogen negative feedback, allowing GnRH release and increased ovulation/steroidogenesis |
|
Aromatase inhibitors |
targets intratumor aromatase in POST-MENOPAUSAL women with estrogen-positive breast cancer (more E2 in tumor than in circulation for these women; pre-menopausal women have more in circulation) |
|
Leuprolide (in females) |
GnRH agonist Pulsatile treatment: increase GnRH for infertility Chronic treatment: antiestrogen/androgen by desensitizing GnRH receptors to suppress hormone release --> endometriosis, fibroids, precocious puberty |
|
Tamoxifen + aromatase inhibitors |
treat breast cancer in men |
|
Anastrozole/letrozole |
aromatase inhibitors (nonsteroidal) that interact irreversibly with heme on CYPs (aromatase = CYP) breast cancer in POST menopausal women induce ovulation in PRE menopausal women with infertility (letrozole) (decrease neg feedback) |
|
Exemestane |
aromatase inhibitor (steroidal) 'suicide inhibitor' that acts as a substrate analog to irreversibly inactivate aromatase breast cancer in POST menopausal women infertility/increase ovulation in PRE menopausal |
|
Androgens (testosterone-IM, oxandrolone, methyltestosterone, fluoxymesterone) |
Hypogonadism/testicular failure in boys with delayed puberty (not for age-related decrease in androgens) --> must have balanced growth hormone levels catabolic states - improve nitrogen balance following injury/surgery abused for sport performance (not effective in building muscle unless immature boy/woman) stimulate EPO - refractory anemia, BMS, renal failure (replaced often by recombinant EPO) palliative breast cancer tx in PRE-menopause |
|
Danazol |
17a-ethinyl testosterone deriv with weak progestin and androgen activity suppresses ovarian function (inhibit midcycle LH surge) --> treat endometriosis |
|
Antiandrogens |
hyperplasia and carcinoma of the prostate gland also for acne, baldness, virilization of females, precocious puberty, inhibit libido block synthesis or action of androgens: finasteride, cyproterone, flutamide, abiraterone, spironolactones, **leuprolide (most effective) |
|
Finasteride |
anti-androgen that inhibits 5a-reductase (blocks testosterone to DHT conversion) BPH and male pattern baldness |
|
Cyproterone acetate |
anti-androgen that competitively antagonizes DHT at the androgen receptor acne, baldness, virilization in women, BPH/prostate cancer, precocious puberty |
|
Flutamide/Bicalutamide |
non-steroidal anti-androgens that competitively antagonize DHT at the androgen receptor prostate cancer (in conjunction with leuprolide) |
|
Abiraterone acetate |
prodrug that inhibits CYP17A1 enzyme that creates testosterone castration-resistant prostate cancer (enzyme found in prostate tumors) |
|
Spironolactones |
competitive antagonist for androgen receptor female hirsutism |
|
Nafarelin |
GnRH agonist (nasal prep) to treat menorrhea, endometriosis and fibroids (shrink fibroid to allow surgery) acts like leuprolide to desensitize GnRH receptors and cause decreased estrogen production |
|
Cetrorelix acetate |
GnRH antagonist that reversibly binds GnRH receptors to block them endometriosis and fibroids more rapid decrease in estrogen levels (don't need to desensitize first) |
|
Oxytocin |
use with PGs to induce labor (stimulate uterine contractions) -> augment abnormal labor that is protracted or arrested IV is pre-mature labor, increase hydration to lower oxytocin conc in plasma |
|
Atosiban |
oxytocin antagonist (competitive antagonist at receptor) suppress pre-term labor |
|
Bosentan/ambrisentin |
blocks the ETa and ETb endothelin receptors (ET-1 receptor antagonists) atrial pulmonary HTN, HTN, cardiac remodeling (but disappointing for HF and CAD) |
|
ANPs/BNPs |
natriuretic, diuretic, vasorelaxant (released due to atrial stretch, SS, endothelins, adrenal steroids, vasopressin) increased levels in CHF, renal failure, primary aldosteronism (level correlates with severity) increase GFR (to increase sodium and water loss), suppress renin/aldosterone/vasopressin, decrease arterial BP |
|
Nesiritide and ularitide |
recombinant BNP and urodilatin - IV for hospitalized patients with decompensated heart failure improve CO, decrease BP and SS activity and renin, reduce dyspnea and fatigue |
|
Sacubitril (+ valsartan) |
neprilysin inhibitor used for heart failure (must be de-ethylated to be active) |
|
Neprilysin inhibitors |
analgesics antihypertensives treatment for sexual arousal disorder in females |
|
Somatotropin |
human recombinant GH used for GH deficiency Pituitary dwarfism Noonan syndrome, Prader-Willi, Turner syndrome (congenital disorders w/stunted growth) Idiopathic short stature Adult GH deficiency (pituitary adenoma/head trauma) Muscle wasting in AIDS |
|
Mecasermin |
recombinant IGF-1 correct growth deficiencies due to decreased IGF-1 --> Laron-type dwarfism GH deficiency where anti-GH Abs exist or unresponsive to GH treatment |
|
Octreotide/lanreotide |
somatostatin analogs (stable, long lasting) injected once every 2-4 weeks inhibit secretion of GH and thyroid hormone for use in gigantism or acromegaly |
|
Pegvisomant |
GH antagonist (mutant GH) blocks GH receptor to use in acromegaly/gigantism when somatostatin agonists are not effective |
|
Desmopressin |
Synthetic ADH analog (intranasal or oral, 2x/day) CENTRAL diabetes insipidus (not nephrogenic!) Nocturnal enuresis (oral only) in kids/elderly Coagulation disorders (vW disease, mild hemophilia A - factor VIII def, thrombocytopenia) Less V1 affinity than ADH, so less VC |
|
Demeclocycline |
tetracycline ABX used to interfere with renal actions of ADH in SIADH to prevent hyponatremia induced death |
|
Methotrexate |
Inhibits dihydrofolate reductase from producing THFA to act as a 1-C donor for converting dUMP to dTMP to make DNA blocks DNA synthesis (folate anti-metabolite) of rapidly growing tumors to cause apoptosis of cells rate of uptake into leukemic cells determines efficacy |
|
MTX + 5-FU |
MTX will antagonize the action of 5-FU if given first (block folate from binding in the tertiary complex that 5-FU forms to strongly block DNA synthesis/TS) |
|
Cytosine arabinose (ara-C) |
phosphorylated to Cys analog to incorporate into DNA and terminate elongation (anti-metabolite) to block DNA synthesis (and DNA pol) or rapidly growing leukemias/lymphomas S-phase specific |
|
Gemcitabine |
Cys analog (anti-metabolite) with F attached targets G0/G1 cells to accumulate S phase cells by incorporating into DNA and inhibiting ribonucleotide reductase **pancreatic cancer and small cell lung cancer |
|
6-mercaptopurine |
phosphorylated to become adenine analog (antimetabolite) that impairs purine synthesis and DNA formation leukemia, lymphoma, immunosuppression |
|
Allopurinol |
inhibits formation of uric acid that builds up when chemotherapy is destroying significant amounts of tumor --> prevent gout inhibits metabolism of 6-MP |
|
Nitrogen mustard |
alkylating agent (all other compounds contain this structure) used for emergency reduction in tumor size (such as spinal cord tumor) requires constant infusion |
|
Cyclophosphamide (CTX) |
alkylating agent (powder-oral) that is activated by CYP450 in liver (add OH) and then further opened up into active metabolites no cycle specificity- can be used for slow growing tumors unresponsive to anti-metabolites eradicate marrow before transplants |
|
MESNA |
protects bladder from cyclophosphamide metabolite damage by detoxifying the cytotoxic acrolein product |
|
Temolozolomide |
alkylating agent converted to active form at physiological pH (ring opened up to release alkylating product that binds DNA and causes damage) can cross BBB --> useful for some brain tumors |
|
Cis-platinum |
alkylating agent - DNA crosslinker (binds DNA, prevents it from dividing, so it warps and gets damaged) testicular tumors |
|
Bleomycin/actinomycin B |
intercalate into DNA structure to cause warping that inhibits DNA synthesis (natural pdt) no marrow toxicity, so used to decrease dose of other drugs that are causing BMS |
|
Daunorubicin/doxorubicin |
complex structures with OH groups that form O radicals that intercalate into DNA and cause damage/distortion |
|
Anthracyclines |
intercalate into DNA to warp/break it broad spectrum efficacy against slower growing cancers --> scheduling is critical and must be injected (unstable at low pH) |
|
Vinca alkaloids (vincristine + vinblastine) |
(periwinkle plant pdts) bind tubulin dimers to prevent dimers from forming microtubules --> to arrest cells in mitosis and causes apoptosis excellent for leukemia and solid tumors |
|
Taxol |
binds tubulin to prevent cell division and proliferation (can't form microtubules) to cause apoptosis of tumor cells ovarian tumors |
|
Camptothecin |
tree bark pdt --> topoisomerase 1 antagonist (prevents DNA unwinding leading to cell death) |
|
Irinotecan |
topoisomerase 1 antagonist commonly used with 5-FU colorectal cancer |
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Etoposide |
topoisomerase II inhibitor solid tumors |
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Gleevec (imatinib) |
TKI that turns off the tyrosine kinase that is permanently on in CML, activating growth factors --> blocks GFs designer drug, made to fit into Bcr-Abl tyr kinase enzyme ATP binding site to block GF phos CML (leukemia) |
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Iressa (gefitinib) |
Bind EGFR (intracellularly) to block downstream signaling in non-SS lung tumors |
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Tykerb (lapatinib) |
Bind erbB2 (Her2) breast cancer |
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Monoclonal antibodies for tumors |
used to target specific/unique cancer pathways and structures to kill solid/slow-growing tumors that are refractory to current treatments target EGRF, VEGF, Her2 (receptors that activate to cause growth and angiogenesis of tumor) USE IN COMBO (IV only) |
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Bevacizumab (avastin) |
anti-VEGF antibodies (bind VEGF receptor to prevent dimerization and activation of angiogenesis) --> decrease BF to tumor IV colon, lung, kidney, glioblastoma increase progression free and overall survival, shrink tumor size to allow operation |
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Tyrosine Kinase Inhibitors |
used to target unique cancer pathways and inhibit intracellular downstream phosphorylation of slow-growing/solid cancer cells insert into ATP binding pockets of signaling enzymes/tyrosine kinases (increase degradation) USE ALONE (oral) |
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Sunitinib |
TKI that blocks intracellular signaling of VEGF + tumors (and other pathways) kidney cancer (advanced) |
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Cetuximab |
EGRF MoAb that binds receptor + ligand to promote complement-mediated lysis of cells and block downstream signaling to induce apoptosis combo with chemo/radiation metastatic colorectal cancer (EGRF +/KRAS wild type) --> shrink tumor, so operable and increase lifespan (6 mths to 24+) |
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Erlotinib |
EGRF TKI that blocks signaling to arrest cell in G1 and induce apoptosis (oral, better option than other lung cancer txs, so screen for mutation) EGRF+ lung cancer/adenocarcinoma common in female, Asian, non-smokers |
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Trastuzumab (herceptin) |
anti-Her2 Ab that binds receptor to block downstream signaling early stage or metastatic breast cancer |
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Lapatinib (Tykerb) |
Her2 TKI (block MAPK and m-TOR pathways) breast cancer and brain metastasis may be used in combo with capecitabine |
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Pertuzumab |
anti-Her2 Ab that binds receptor to block dimerization breast cancer |
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t-DM1 |
antibody (trastuzumab) - drug (roche) conjugate Ab acts as vehicle to deliver toxic drug to tumor to be effective at site of cancer and less toxic --> deliver to Her2+ breast cancer cells breast cancer |
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Ipilimumab |
IV anti-CTLA-4 Ab that binds and blocks CTLA-4 so it can't bind an APC and cause decreased activation of T-cells --> release the brakes from T-cells to increase their activity on cancer cells |
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Nivolumab |
anti-PD-1 Ab that binds and blocks PD-1 on T-cells to prevent its apoptosis/down-regulation of T-cell activation checkpoint inhibitor (allows more active T cells) lung cancer and melanoma |