All Drugs

Front 1

Dorzolamide/acetazolamide

Back 1

CA inhibitor --> topical to reduce intraocular pressure

sometimes brain edema

Front 2

Mannitol

Back 2

osmotic diuretic (IV) to relieve brain edema

oral: osmotic diarrhea to rid toxins

Front 3

Amiloride/triamterene

Back 3

ENaC inhibitors: blunt hypokalemia/alkalosis from other diuretics

Li induced nephrogenic diabetes insipidus

Front 4

Spironolactone

Back 4

Competitive inhibitor of aldosterone: blunt hypokalemia/alkalosis from other diuretics

severe CHF (less myocardial remodeling)

edema due to hepatic cirrhosis

Front 5

Furosemide

Back 5

edema (liver, renal or CHF)

relieve pulmonary congestion in CHF

acute hypercalcemia, hyperkalemia, toxic OD of halogens

acute renal failure

Front 6

Thiazides (hydrochlorothiazide and chlorthalidone)

Back 6

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

Front 7

Enalapril/lisinopril

Back 7

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)

Front 8

Aliskiren

Back 8

Renin inhibitor: HTN (use with thiazide)

Front 9

Losartan/valsartan

Back 9

AT-1 antagonists: HTN in patients with ACEI-mediated cough

CHF (block cardiac remodeling and reduce cardiac work)

Acute MI

Front 10

Valsartan + sacubitril

Back 10

CHF

block Ang II, enhance ANP

Front 11

B-blockers

Back 11

HTN (second line-use for complicated HTN)

Cardiac arrhythmia

Angina

Acute MI ** (first line)

HF

Thyrotoxicosis

Front 12

Propranolol

Back 12

non-selective, extensive first pass metabolism

CHF, acute MI, angina, arrhythmia

Front 13

Metoprolol

Back 13

beta-1

SR formula for CHF

Front 14

Atenolol

Back 14

beta-1 (no first pass)

CHF, acute MI, arrhythmia, angina

Front 15

Pindolol

Back 15

beta-1,2,ISA: initially increase HR (less ADEs)

*NOT for use in MI

Front 16

Labetolol

Back 16

alpha,beta,ISA: HTN in pregnant women

less cardiac uses

Front 17

Carvedilol

Back 17

alpha-1,beta: CHF (reduces lipid peroxidation by radicals and reduces SM mitogenesis)

Front 18

Esmolol

Back 18

ultra short beta-1: IV

supraventricular arrhythmia

acute HTN

acute MI

Front 19

Sotalol

Back 19

beta + K: anti-arrhythmia

Front 20

Nebivolol

Back 20

beta-2 agonist: HTN

Front 21

Ivabradine

Back 21

If inhibitor: CHF pts that can't use b-blockers (HR > 70) --> reduce pacemaker activity by blocking phase 0 of SA node

Front 22

Methyldopa

Back 22

central sympatholytic (a-2 agonist): HTN during pregnancy

Front 23

Clonidine

Back 23

central sympatholytic (a-2 agonist): HTN

blunt SS reflex due to VDs

*NOT for depressed patients

Front 24

Prazosin

Back 24

a-1 antagonist: HTN

*NOT for use as monotherapy due to hypotensive response (add b-blocker or diuretic)

BPH urinary issues (tamulosin)

Front 25

Nifedipine

Back 25

DHP CCB: HTN

*May cause baroreceptor reflex mediated hypotension

Front 26

Amlodipine

Back 26

DHP CCB: HTN and CHF (LVD)

Front 27

Nicardipine/clevidipine

Back 27

short acting DHPs: IV for emergency HTN

Front 28

Nimodipine

Back 28

DHP CCB: subarachnoid hemorrhagic stroke

Front 29

Verapamil

Back 29

non-DHP CCB: angina (decrease FOC by blocking Ca influx)

anti-arrhythmia: SVT and prevent spread with A-fib

suppress EADs and DADs

Front 30

Diltiazem

Back 30

non-DHP CCB: angina

anti-arrhythmia: SVT and prevent spread of A-fib

suppress EADs and DADs

Front 31

Nitroglycerin/isosorbide dinitrate

Back 31

ISCHEMIA ISSUES:

classic angina (ATH obstruction)

variant angina (transient spasm)

unstable angina (increased tone or clots)

CHF

recovery from MI

Front 32

Sildenafil

Back 32

PDE5 inhibitor: erectile dysfunction

pulmonary hypertension** (leads to RVF)

Front 33

Ranolazine

Back 33

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)

Front 34

Bosantan

Back 34

endothelin receptor blocker (ET-1): arterial pulmonary HTN

Front 35

Hydralazine

Back 35

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)

Front 36

Minoxidil

Back 36

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)

Front 37

Sodium nitroprusside

Back 37

VD (generates NO) - continuous IV

EMERGENCIES (that need reduced pre/afterload)
HTN emergencies

Acute aortic dissection

Cardiogenic shock

Induce controlled hypotension for anesthesia

Front 38

Digoxin

Back 38

cardiac glycoside (increase contractility): blocks Na/K ATPase (accumulate Na and Ca)

CHF

Front 39

Dobutamine

Back 39

sympathomimetic amine = beta agonist (significant increase in contractility and CO)

short-term for acute cardiac decompensation

acute HF or MI

diagnose coronary obstructions

Front 40

Dopamine

Back 40

severe CHF with compromised renal function

high dose: cardiogenic/septic shock (acts on a-adr to increase TPR)

Front 41

Procainamide

Back 41

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

Front 42

Esmolol/sotalol

Back 42

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

Front 43

Amiodarone

Back 43

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

Front 44

Verapamil/diltiazem

Back 44

suppress EADs and DADs

reentrant SVT

reduce risk of vent tachycardia with A-fib

**avoid with Wolf-White

Front 45

Adenosine

Back 45

SVT (IV only)

inhibits SA, atrial and AV conduction

Front 46

Magnesium sulfate (IV only)

Back 46

digoxin related arrhythmia

drug induced torsades de pointes

arrhythmia due to hypomagnesia

Front 47

Statins

Back 47

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)

Front 48

Alirocumab/evolucumab

Back 48

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

Front 49

Lovastatin/simvastatin

Back 49

lactone ring side group must be cleaved in liver to activate - prodrugs

Front 50

Statins + bile acid resins

Back 50

reduced liver cholesterol and increased LDL-R uptake

20-30% more LDL-C lowering

Front 51

Statins + ezetimide

Back 51

decrease LDL-C by up to 60% and better mortality and morbidity

Front 52

Statin combos

Back 52

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

Front 53

Statins + fibrates

Back 53

patients with high TGs and LDL-C

avoid gemfibrizol, or half dose of statins

Front 54

Statins + niacin

Back 54

patients with high LDL-C and low HDL-C (niacin improves HDL levels)

Front 55

Ezetimibe

Back 55

blocks absorption of cholesterol from diet (inhibits intestinal transporter NPC1L1)

Vytorin = statin + ezetimibe --> enhance LDL reduction

Front 56

Cholestyramine/colestipol

Back 56

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

Front 57

Niacin

Back 57

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

Front 58

Gemfibrozil/fenofibrate

Back 58

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

Front 59

Fomepizole

Back 59

blocks ADH metabolism in case of methanol overdose (stop formation of formaldehyde)

Front 60

Disulfiram

Back 60

blocks aldehyde dehydrogenase (ALDH) from metabolizing acetaldehyde to acetate

Adversive: causes unpleasant ADEs associated with alcohol use so that patients will decrease drinking

Front 61

Flunitrazepam (rohypnol), GHB, GBL

Back 61

"roofies" and other date rape drugs

Front 62

Alcohol

Back 62

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

Front 63

Abstinence syndrome

Back 63

~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)

Front 64

Delirium tremens

Back 64

~2-3 days after last use

confusion, disorientation, agitation, hyperpyresis, dehydration

Front 65

Naltrexone

Back 65

anti-craving opioid antagonist ("depo")

used to decrease use and desire of alcohol

Front 66

Acamprosate

Back 66

anti-craving NMDA antagonist/GABA agonist

used to decrease use and desire for alcohol

Front 67

Cocaine HCl

Back 67

powder (diluents)

can be used to cause vasoconstriction/local anesthesia, or to snort (inhale) or inject

Front 68

Cocaine free base

Back 68

crack --> use to smoke

Front 69

Norcocaine

Back 69

active cocaine metabolite formed by N-demethylation

toxic

Front 70

Cocaethylene

Back 70

active metabolite formed from use of EtOH + cocaine

toxic: seizures, immune system depression, hepatotoxicity

Front 71

Cocaine

Back 71

euphoria, dysphoria, hallucinosis, psychosis

profound CNS excitation, leading to desynchronization (with OD)

increase HR, BP, RR, temp, SM tone, eye dilation, seizures, decrease appetite

Front 72

5-FU

Back 72

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

Front 73

Leucovorin

Back 73

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

Front 74

Uridine triacetate

Back 74

"antidote" to decrease toxicity of 5-FU

overcome 5-FU block of pathway to make T, compete for RNA incorporation

Front 75

Dipyramidole

Back 75

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

Front 76

Ethynyluracil

Back 76

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

Front 77

Capecitabine

Back 77

5-FU prodrug that is activated in liver and then at tumor site to make 5-FU orally active

refractory breast cancer

Front 78

Tegafur

Back 78

5-FU prodrug activated in liver (make 5-FU orally active)

Front 79

TAS-114

Back 79

inhibits DPD and dUTPase (enzyme that cleaves 5-FU UDP)

given with capecitabine/5-FU to increase its activity by decreasing metabolism

Front 80

TAS-102

Back 80

cytotoxic trifluridine + tipiracil --> inhibit thymidine phosphorylase and kill cells when incorporated into DNA

use for patients that have failed all other drugs

Front 81

S-1

Back 81

tegafur + DPD inhibitor + 5-FU phos inhibitor

Front 82

Irinotecan

Back 82

inhibits TS activity to increase efficacy of 5-FU in chemotherapy (even in patients with high TS levels)

Front 83

FOLFOX

Back 83

cycles of 5-FU/leucovorin/oxaliplatin infusion to determine target range of 5-FU and to individualize dosage (and minimize toxicity)

Front 84

Opiates (heroin, oxycodone, meperidine, methadone)

Back 84

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

Front 85

Naloxone

Back 85

opioid antagonist for use in toxicity/OD

atomizer

Front 86

Methadone

Back 86

used for 'detox' during opioid withdrawal -> cross dependence allows lessening of abstinence syndrome symptoms

Front 87

Clonidine + acetaminophen

Back 87

used for opioid withdrawal to 'detox'

must decrease dose of 'detox' by 25% each day until withdrawal is over

Front 88

Buprenorphine + naloxone (suboxone)

Back 88

long-term management for opioid withdrawal

Front 89

Methylnaltrexone and Naloxegol

Back 89

opioid constipation

Front 90

Cannabinoids

Back 90

anticonvulsant, sedative, antimicrobial, decrease neuropathic and inflammatory pain

Front 91

Dronabinol

Back 91

oral cannabinoid used in wasting disease to increase appetite

Front 92

THC

Back 92

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)

Front 93

Glucagon

Back 93

reversal of diabetic coma due to insulin OD when oral glucose cannot be administered

Front 94

Soluble/regular insulin

Back 94

monomeric form for rapid absorption (at meals)

Front 95

NPH insulin

Back 95

intermediate acting, mixed with protamine

Front 96

Lente/ultralente insulin

Back 96

slow absorption (bound to zinc) for basal levels or nighttime

Front 97

Lispro/aspart insulin

Back 97

most soluble, rapid-acting forms (no self-association due to mutations)

Front 98

Glargine insulin (LANTUS)

Back 98

peakless insulin, ultra long acting

hexamer form to precipitate and leach away from site of injection for steady baseline all day

Front 99

Metformin (biguanide)

Back 99

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

Front 100

Sulfonylureas: glimepiride, glipizide, glyburide

Back 100

bind ATP sensitive K channel to block its conductance and allow depol of b-cell to increase insulin secretion (insulin secretagogue)

Front 101

Glitinides: repaglinide + nateglinide

Back 101

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)

Front 102

TZDs/glitazones: rosiglitazone + pioglitazone

Back 102

second line only (ADEs) to reduce insulin R by binding PPARy on adipose cells to suppress resistin release

Front 103

Exenatide

Back 103

GLP-1 homolog (Gila monster) -2x/day injection causes increase in insulin release and blunt post-prandial surge-> insulin secretagogue

Front 104

Liraglutide

Back 104

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

Front 105

Sitagliptin

Back 105

DPP-4 inhibitor to increase half-life and action of endogenous GLP-1 (use when diet/exercise and metformin fail)

oral, once daily

Front 106

Acarbose/miglitol (a-glucosidase inhibitors)

Back 106

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

Front 107

SGLT2 inhibitors: dapagliflozin + canagliflozin

Back 107

inhibit renal glucose reuptake transporter SGLT2 to increase glucose excretion in urine and lower blood glucose

combo with metformin

Front 108

Orlistat

Back 108

long-term weight loss (modest 4-7lbs) pill (take with meals)

inhibits intestinal lipases that hydrolyzes TGs so fats are not absorbed

Front 109

Lorcaserin

Back 109

appetite suppressing weight loss drug (selective 5-HT2c agonist) for obese patients with co-morbidities

promotes POMC production to promote satiety

oral - ~10 lbs

Front 110

Phentermine/topiramate

Back 110

weight loss drug for obese pts with co-morbidities (stimulant + anticonvulsant)

appetite suppression

Front 111

Bupropion/naltrexone

Back 111

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

Front 112

Levothyroxine

Back 112

synthetic T4 for hypothyroidism (due to Hashimoto's auto-immune thyroid impairment or destruction of thyroid)

once daily pill

congenital thyroid deficiency - prevent cretinism

Front 113

Liothyronine sodium

Back 113

synthetic T3 (multiple doses per day) for hypothyroidic coma

Front 114

Thioureylenes

Back 114

methimazole and propylthiouracil = anti-thyroid drugs to block the production of thyroid hormone (inhibit tyrosyl iodination on thyroglobulin)

competitive inhibitor of thyroperoxidase

Front 115

Methimazole

Back 115

once daily dosing for hyperthyroidism (oral) --> first line

Front 116

Propylthiouracil

Back 116

inhibits peripheral de-iodination of T4 -->

use for acute thyroid storm

hyperthyroidism (long-term stabilization)

Front 117

High dose iodide

Back 117

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

Front 118

Propranolol for thyrotoxicosis

Back 118

symptomatic relief to decrease tachycardia, arrhythmia, tremor and agitation caused by hyperthyroid state (thyroid storm)

use during lag for thioureylenes to be effective (2-4 months)

Front 119

Tamoxifen

Back 119

anti-estrogen used for estrogen receptor-positive breast cancer patients requiring adjuvant therapy after surgical removal of the tumor

pre or post-menopausal women

Front 120

Diethylstilbestrol (in males)

Back 120

synthetic estrogen used in males for palliative treatment of prostate cancer

acts on hypothalamus (negative feedback) to depress GnRH and subsequent androgen release

Front 121

Leuprolide (in males)

Back 121

GnRH agonist that is used with an antiandrogen (for initial upregulation period) to downregulate GnRH and androgen release to treat prostate cancer

Front 122

Postmenopausal HRT estrogen therapy

Back 122

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

Front 123

Progestin alone

Back 123

"minipill" for contraception

less efficacy and more irregular cycle, so less used

Front 124

Diethylstilbestrol (in females)

Back 124

"morning after pill" - use within 72 hours of coitus

synthetic estrogen that changes cervical mucus and endometrium to decrease implantation

Front 125

Norgestrel/ethinyl estradiol (preven)

Back 125

emergency contraception within 72 hours of coitus

Front 126

Mifepristone (RU-486)

Back 126

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)

Front 127

Lipopristone/ZK98734

Back 127

mifepristone analog that may be used for progesterone sensitive tumors

Front 128

Progestins

Back 128

medroxyprogesterone, norethindrone, norgestrel, ethynodiol

oral contraception/HRT (with estrogen) to decrease cancer risk

dysfunctional uterine bleeing

dysmenorrhea

premenstrual syndrome

endometriosis

metastatic endometrial carcinoma

Front 129

Norgestrel

Back 129

'plan B'

progestin used for emergency contraception within 72 hours of coitus

subcutaneous implant capsules that slowly release progestin for contraception

Front 130

Oral contraceptives

Back 130

progestin + estrogen is best

inhibit ovulation (suppress both FSH and LH)

99-100% effective in preventing pregnancy

Front 131

Tamoxifen

Back 131

estrogen receptor competitive antagonist (anti-estrogen) + partial agonist

breast cancer PRE-MENOPAUSAL

Front 132

Clomiphene

Back 132

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

Front 133

Aromatase inhibitors

Back 133

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)

Front 134

Leuprolide (in females)

Back 134

GnRH agonist

Pulsatile treatment: increase GnRH for infertility

Chronic treatment: antiestrogen/androgen by desensitizing GnRH receptors to suppress hormone release --> endometriosis, fibroids, precocious puberty

Front 135

Tamoxifen + aromatase inhibitors

Back 135

treat breast cancer in men

Front 136

Anastrozole/letrozole

Back 136

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)

Front 137

Exemestane

Back 137

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

Front 138

Androgens (testosterone-IM, oxandrolone, methyltestosterone, fluoxymesterone)

Back 138

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

Front 139

Danazol

Back 139

17a-ethinyl testosterone deriv with weak progestin and androgen activity

suppresses ovarian function (inhibit midcycle LH surge) --> treat endometriosis

Front 140

Antiandrogens

Back 140

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)

Front 141

Finasteride

Back 141

anti-androgen that inhibits 5a-reductase (blocks testosterone to DHT conversion)

BPH and male pattern baldness

Front 142

Cyproterone acetate

Back 142

anti-androgen that competitively antagonizes DHT at the androgen receptor

acne, baldness, virilization in women, BPH/prostate cancer, precocious puberty

Front 143

Flutamide/Bicalutamide

Back 143

non-steroidal anti-androgens that competitively antagonize DHT at the androgen receptor

prostate cancer (in conjunction with leuprolide)

Front 144

Abiraterone acetate

Back 144

prodrug that inhibits CYP17A1 enzyme that creates testosterone

castration-resistant prostate cancer

(enzyme found in prostate tumors)

Front 145

Spironolactones

Back 145

competitive antagonist for androgen receptor

female hirsutism

Front 146

Nafarelin

Back 146

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

Front 147

Cetrorelix acetate

Back 147

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)

Front 148

Oxytocin

Back 148

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

Front 149

Atosiban

Back 149

oxytocin antagonist (competitive antagonist at receptor)

suppress pre-term labor

Front 150

Bosentan/ambrisentin

Back 150

blocks the ETa and ETb endothelin receptors (ET-1 receptor antagonists)

atrial pulmonary HTN, HTN, cardiac remodeling (but disappointing for HF and CAD)

Front 151

ANPs/BNPs

Back 151

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

Front 152

Nesiritide and ularitide

Back 152

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

Front 153

Sacubitril (+ valsartan)

Back 153

neprilysin inhibitor used for heart failure (must be de-ethylated to be active)

Front 154

Neprilysin inhibitors

Back 154

analgesics

antihypertensives

treatment for sexual arousal disorder in females

Front 155

Somatotropin

Back 155

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

Front 156

Mecasermin

Back 156

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

Front 157

Octreotide/lanreotide

Back 157

somatostatin analogs (stable, long lasting)

injected once every 2-4 weeks

inhibit secretion of GH and thyroid hormone for use in gigantism or acromegaly

Front 158

Pegvisomant

Back 158

GH antagonist (mutant GH)

blocks GH receptor to use in acromegaly/gigantism when somatostatin agonists are not effective

Front 159

Desmopressin

Back 159

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

Front 160

Demeclocycline

Back 160

tetracycline ABX used to interfere with renal actions of ADH in SIADH to prevent hyponatremia induced death

Front 161

Methotrexate

Back 161

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

Front 162

MTX + 5-FU

Back 162

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)

Front 163

Cytosine arabinose (ara-C)

Back 163

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

Front 164

Gemcitabine

Back 164

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

Front 165

6-mercaptopurine

Back 165

phosphorylated to become adenine analog (antimetabolite) that impairs purine synthesis and DNA formation

leukemia, lymphoma, immunosuppression

Front 166

Allopurinol

Back 166

inhibits formation of uric acid that builds up when chemotherapy is destroying significant amounts of tumor --> prevent gout

inhibits metabolism of 6-MP

Front 167

Nitrogen mustard

Back 167

alkylating agent (all other compounds contain this structure) used for emergency reduction in tumor size (such as spinal cord tumor)

requires constant infusion

Front 168

Cyclophosphamide (CTX)

Back 168

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

Front 169

MESNA

Back 169

protects bladder from cyclophosphamide metabolite damage by detoxifying the cytotoxic acrolein product

Front 170

Temolozolomide

Back 170

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

Front 171

Cis-platinum

Back 171

alkylating agent - DNA crosslinker (binds DNA, prevents it from dividing, so it warps and gets damaged)

testicular tumors

Front 172

Bleomycin/actinomycin B

Back 172

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

Front 173

Daunorubicin/doxorubicin

Back 173

complex structures with OH groups that form O radicals that intercalate into DNA and cause damage/distortion

Front 174

Anthracyclines

Back 174

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)

Front 175

Vinca alkaloids (vincristine + vinblastine)

Back 175

(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

Front 176

Taxol

Back 176

binds tubulin to prevent cell division and proliferation (can't form microtubules) to cause apoptosis of tumor cells

ovarian tumors

Front 177

Camptothecin

Back 177

tree bark pdt --> topoisomerase 1 antagonist (prevents DNA unwinding leading to cell death)

Front 178

Irinotecan

Back 178

topoisomerase 1 antagonist

commonly used with 5-FU

colorectal cancer

Front 179

Etoposide

Back 179

topoisomerase II inhibitor

solid tumors

Front 180

Gleevec (imatinib)

Back 180

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)

Front 181

Iressa (gefitinib)

Back 181

Bind EGFR (intracellularly) to block downstream signaling in non-SS lung tumors

Front 182

Tykerb (lapatinib)

Back 182

Bind erbB2 (Her2)

breast cancer

Front 183

Monoclonal antibodies for tumors

Back 183

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)

Front 184

Bevacizumab (avastin)

Back 184

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

Front 185

Tyrosine Kinase Inhibitors

Back 185

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)

Front 186

Sunitinib

Back 186

TKI that blocks intracellular signaling of VEGF + tumors (and other pathways)

kidney cancer (advanced)

Front 187

Cetuximab

Back 187

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+)

Front 188

Erlotinib

Back 188

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

Front 189

Trastuzumab (herceptin)

Back 189

anti-Her2 Ab that binds receptor to block downstream signaling

early stage or metastatic breast cancer

Front 190

Lapatinib (Tykerb)

Back 190

Her2 TKI (block MAPK and m-TOR pathways)

breast cancer and brain metastasis

may be used in combo with capecitabine

Front 191

Pertuzumab

Back 191

anti-Her2 Ab that binds receptor to block dimerization

breast cancer

Front 192

t-DM1

Back 192

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

Front 193

Ipilimumab

Back 193

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

Front 194

Nivolumab

Back 194

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