Block 6 Drugs

Front 1

Cholestyramine
Colestipol

Back 1

--bile acid sequestrants
--positively charged anion exchange resins

--dec LDL plasma levels

--act in enterohepatic circulation to bind bile acids and increase bile acid excretion
--causes inc HMG CoA reductase levels
--causes up-regulation of LDL receptors to increase LDL clearance from blood

--may cause bloating, gas, constipation
--impair absorption of warfarin, digoxin, fat soluble vitamins

--contraindicated in patients with high TG's

Front 2

Colesevelam

Back 2

--bile acid sequestrant
--polymeric hydrophilic gel

--dec LDL plasma levels
--adjunct treatment in type 2 diabetics
--act in enterohepatic circulation to bind bile acids and increase bile acid excretion
--causes inc HMG CoA reductase levels
--causes up-regulation of LDL receptors to increase LDL clearance from blood

--cause less side effects vs. cholestyramine and colestipol

-impair absorption of warfarin, digoxin, fat soluble vitamins

--contraindicated in patients with high TG's

Front 3

Lovastatin
Simvastatin
Atorvastatin

Back 3

--HMG CoA reductase inhibitors

--dec LDL plasma levels
--inc HDL levels
--dec TG levels
--dec CRP

--inhibit hepatic HMG CoA reductase
--leads to up regulation of LDL receptors

--may cause myopathy and inc liver enzymes

--metabolized by CYP3A4 (important for drug interactions)

--contraindicated in pts with liver disease, those who are pregnant or breast feeding

Front 4

Fluvastatin

Back 4

--HMG CoA reductase inhibitor

--dec LDL plasma levels
--inc HDL levels
--dec TG levels
--dec CRP

--inhibit hepatic HMG CoA reductase
--leads to up regulation of LDL receptors

--may cause myopathy and inc liver enzymes

--metabolized by CYP2C9(important for drug interactions)

--contraindicated in pts with liver disease, those who are pregnant or breast feeding

Front 5

Pravastatin
Rosuvastatin

Back 5

--HMG CoA reductase inhibitors

--dec LDL plasma levels
--inc HDL levels
--dec TG levels
--dec CRP

--inhibit hepatic HMG CoA reductase
--leads to up regulation of LDL receptors

--may cause myopathy and inc liver enzymes

--not significantly metabolized by CYP's and less affected by other drugs

--contraindicated in pts with liver disease, those who are pregnant or breast feeding

Front 6

Ezetimibe

Back 6

--cholesterol absorption blocker

--acts at small intestine brush border to inhibit NPC1L1
--reduces intestinal absorption of cholesterol and decreased delivery of intestinal cholesterol to liver

--causes upregulation of LDL receptors
--only medicine approved for treatment of sitosterolemia

--may cause diarrhea and depression
--contraindicated in pts with liver disease

Front 7

Niacin

Back 7

--vitamin B3, nicotinic acid

--acts on GPR109A to decrease lipolysis
--causes dec VLDL and dec LDL
--most efficacious in increasing HDL
--most efficacious in decreasing LP(a)

--may cause flushing
--OTC nicotinic acid SR associated with hepatotoxicity
--contraindicated in pts with peptic ulcers, gout, liver disease

Front 8

Fenofibrate

Back 8

--fibric acid derivative

--full PPAR-alpha agonist
--leads to change in gene transcription
--increases fatty acid oxidation in liver, muscle
--dec Apo CIII which causes increased lipoprotein lipase

--dec TG
--inc HDL
--treats atherogenic dyslipidemia

--better at lowering TG and raising HDL vs. statins

--may prolong warfarin INR

Front 9

Gemfibrozil

Back 9

--fibric acid derivative

--selective PPAR-alpha modulator

--dec TG
--inc HDL
--treat atherogenic dyslpidemia

--inhibits CYP2C8 and increases AUC of statins
--more likely than fenofibrate to cause myalgia when combined w/ statin

Front 10

PUFA

Back 10

--omega-3 polyunsaturated fatty acid

--dec TG
--dec VLDL
--increase large, buoyant, less atherogenic LDL particles

--most efficacious in decreasing TG

--dual effect
--high dose decreases TG
--low doese inhibits platelet aggregation

Front 11

Levothyroxine

Back 11

--isomer of T4
--synthetic

--used to treat hypothyroidism
--drug of choice!

--provides large T4 pool for conversion to T3

Front 12

Liothyronine

Back 12

--isomer of T3
--synthetic

Front 13

Liotrix

Back 13

--mixture of levothyroxine and liothyronine

--T4:T3 ratio is 4:1
--mimics thyroid output

Front 14

Thyroid USP

Back 14

--organic TH extract
--dessicated powder of animal thyroid glands

--not bioassayed

--cheaper vs. synthetic preparations but has major variability and safety issues

Front 15

Thyroglobulin USP

Back 15

--organic TH extract
--purified extract of pig thyroid

--is bioassayed

--cheaper vs. synthetic preparations but has major variability and safety issues

Front 16

Propylthiouracil (PTU)
Methimazole

Back 16

--thioamide used to treat hyperthyroidism

--inhibits organification and coupling steps in TH synthesis via inhibition of thyroid peroxidase

--inhibits peripheral T4 to T3 conversion

--short half-life
--accumulate in thyroid

--long onset of effect
--palliative therapy but does decrease excessive hormone synthesis

Front 17

Perchlorate
Pertechnetate
Thiocyanate

Back 17

--monovalent anion inhibitors
--treat hyperthyroidism

--block iodide uptake by follicle cells
--effects of these drugs can be overcome by large doses of iodide

--perchlorate can block iodide-induced or amiodarone-induced hyperthyroidism

Front 18

Potassium Iodide, USP
Sodium Iodide, USP
Potassium Iodide Oral Solution, USP

Back 18

--iodide preparations
--considered pharmacologic doses of iodide
--used to treat hyperthyroidism

--inhibit organificatio of iodide at level of TPO
--dec release of T4, T3 at level of proteolysis
--reduces vascularity of hyperfunctioning thyroid

--used to rapidly relieve thyrotoxicosis effects
--used with thiourea drugs

--beneficial effects are rapid but transient

Front 19

Strong iodine solution, USP
Lugols solution

Back 19

--considered pharmacologic doses of iodide
--iodine must be reduced to iodide in GI tract
--treats hyperthyroidism

--inhibit organification of iodide at level of TPO
--dec release of T4, T3 at level of proteolysis
--reduces vascularity of hyperfunctioning thyroid

--used to rapidly relieve thyrotoxicosis effects
--used with thiourea drugs

--beneficial effects are rapid but transient

Front 20

Iodinated contrast media

Back 20

--inhibits peripheral deiodination
--suppresses T3, T4 production

--used mainly for diagnosis of thyroid disease

Front 21

Iodide-131

Back 21

--used to treat hyperthyroidism

--is a beta emitter that accumulates in thyroid gland and used in TH synthesis
--is stored in colloid and releases beta particles to destroy some of the surrounding follicular tissue

Front 22

Propanolol

Back 22

--beta blocker

--used to prevent symptoms of thyrotoxicosis (palliative)

Front 23

Iodide supplements

Back 23

--used to treat endemic goiter

--often given with T4 to negatively inhibit TSH secretion and prevent acute hyperthyroid event

Front 24

Mitotane

Back 24

--DDT derivative
--drug therapy in Cushing's disease

--inhibits 21, 17alpha, 11beta hydroxylases
--destroys adrenal tissue
--no longer on US market

Front 25

Amphenone B

Back 25

--drug therapy in Cushing's disease
--more potent than mitotane

--inhibits 21, 17alpha, 11beta hydroxylases
--does not destroy adrenal tissue
--no longer on US market

Front 26

Metyrapone

Back 26

--drug therapy in Cushing's disease
--specific inhibitor of 11beta hydroxylase

--blocks 11-deoxycortisol to cortisol conversion

--used to test for pituitary reserve of ACTH
--may be used to treat cortisol excess before cause is known
--rarely used as therapy

Front 27

Aminoglutethimide

Back 27

--drug therapy in Cushing's disease

--inhibits cholesterol to pregnenolone conversion
--reduces secretion of MCC, GCC and androgens

--blunts androgen synthesis in testes

--ACTH release can overcome its effects
--used mainly in Cushings 2ndary to adrenal cancer
--used with dexamethasone to dec androgen secretion

Front 28

Ketoconazole

Back 28

--drug therapy in Cushing's disease

--leads to compensatory increase in ACTH, androgens, aldosterone

--displaces estrogen and testosterone from binding proteins
--increases estrogen:testosterone ratio

--can cause gynecomastia and oligospermia in males
--can alter menstrual cycle in females

Front 29

Mifepristone

Back 29

--GCC receptor antag

Front 30

Spironolactone

Back 30

--MCC receptor antag

--treats excessive aldosterone secretion
--K+ sparing diuretic

Front 31

Captopril
Losartan

Back 31

--both are inhibitors of renin/angiotensin system

--captopril is an ACE-I
--losartan is an angiotensin-1 receptor antag

Front 32

Methyltestosterone

Back 32

--Type B synthetic testosterone
--17alpha substitution

--orally active
--not metabolized to testosterone
--can cause liver cancer

Front 33

Mesterolone

Back 33

--Type C synthetic testosterone
--ring alteration

--orally active
--not metabolized to testosterone
--can cause liver cancer

Front 34

Enanthate
Cypionate

Back 34

--Type A synthetic testosterone
--17beta esterification

--injected with delayed absorption
--metabolized to testosterone

--often used to treat primary testicular failure

--if given in high doses, won't cause decreased plasma testosterone levels

Front 35

Danazol

Back 35

--Type BC synthetic testosterone

--exerts negative feedback on pituitary without estrogenic effects to induce a "pseudomenopause" state
--commonly used for treatment of endometriosis

--drug of choice for hereditary angioneurotic edema
--danazol leads to increase in the hepatic synthesis of the active inhibitor of the first component of complement

Front 36

Leuprolide

Back 36

--GnRH analog

--if given continuously, has inhibitory effects on LH/FSH
--if given in pulsatile manner, will increase LH/FSH production

--continuous administration would be beneficial if the need is to suppress androgens

--often coupled with androgen receptor antagonists for the treatment of excess androgens in women or for the treatment of advanced prostate cancer

Front 37

Sustained release GnRH analogs:
Goserelin
Gonadorelin
Leuprolide
Nafarelin

Back 37

--GnRH analogs

--if given continuously, has inhibitory effects on LH/FSH
--if given in pulsatile manner, will increase LH/FSH production

--continuous administration would be beneficial if the need is to suppress androgens
--continuous administration decreases pituitary gonadotropin secretions
--useful in treatment of endometriosis and prostate cancer

Front 38

Finasteride

Back 38

--5alpha reductase inhibitor
--used to treat BPH
--blocks hirsutism in women

Front 39

Cyproterone
Flutamide

Back 39

--androgen receptor antagonists

--used to treat excess androgens in women
--used to treat advanced prostate cancer

--often coupled with a GnRH agonist like leuprolide

Front 40

Gossypol

Back 40

--means of male contraception

--destroys elements of seminiferous epithelium to impair spermatogenesis

--decreases sperm motility

--does not affect endocrine funciton

Front 41

Sulfonylureas

Back 41

--insulin secretagogues

--make pancreatic beta cells more sensitive to ATP, leading to depolarization and stimulation of more insulin secretion

--contraindicated in liver failure
--can cause hypoglycemia

Front 42

Metformin

Back 42

--increases tissue glucose uptake and reduces liver gluconeogenesis

--can delay or prevent onset of NIDDM

--does NOT depend on insulin secretion
--does NOT produce hypoglycemia

--can cause lactic acidosis, especially if patient drinks alcohol

Front 43

Thiazolidinediones

Back 43

--acts through PPAR-gamma receptor to alter gene expression

--leads to decreased circulating lipids
--causes reduction in TNFalpha
--causes increase in adiponectin and insulin sensitivity
--may delay onset of NIDDM

--can cause weight gain, can promote CHF

Front 44

Alpha-glucosidase inhibitors

Back 44

--inhibits alpha-glucosidase in the gut which slows absorption of glucose

--taken orally with meals

Front 45

Amylin analog

Back 45

--pramlintide is an amylin analog

--reduces postprandial glucose in both IDDM and NIDDM
--may cause hypoglycemia

Front 46

Incretins

Back 46

--leads to increased insulin secretion
--leads to increased beta cell growth
--reduces glucagon secretion
--slows gastric emptying
--reduces appetite

Front 47

DPP IV inhibitors

Back 47

--block incretin degradation

Front 48

Albuterol
Levalbuterol

Back 48

--quick acting beta2 agonist inhaler
--relax airway smooth muscle which increases cAMP and produces functional antagonism to bronchoconstriction

--therapy of choice for relief of acute asthma symptoms and prevention of exercise induced bronchoconstriction

Front 49

Budesonide
Fluticasone
Mometasone

Back 49

--inhaled corticosteroids

--block late reaction to allergen and reduce airway hyperresponsiveness

--indicated for asthma patients who use their short acting inhaler more than 2days/week or more than 2x/month for nighttime awakenings

--local effects (oral thrush, hoarseness)
--systemic effects (impaired growth in kids, osteoporosis, disseminiated varicella, etc)

Front 50

Cromolyn
Nedocromil

Back 50

--inhibit activation and release of mediators from mast cells, eosinophils

--used prophylactically to trevent exercise-induced asthma or asthma caused by unavoidable exposure to known allergens

--nedocromil is better at inhibiting bronchospasm caused by exercise and by cold dry air

--may cause transient cough

Front 51

Ipratropium
Tiotropium

Back 51

--inhaled anticholinergic

--used alone, relieves bronchospasm in chronic bronchitis and COPD

--treatment of choice for bronchospasm due to beta-blocker therapy
--does not prevent exercise-induced asthma

--can cause dry mouth and a bitter taste
--no CNS activity

--ipratropium used 4x/day
--tiotropium used once daily

Front 52

Montelukast

Back 52

--leukotriene receptor antagonist
--can be used concomitantly with inhaled corticosteroids for moderate persistent asthma

--useful in exercise-induced asthma in kids

--used to treat asthma and allergic rhinitis

--may cause neuropsychiatric events

Front 53

Zileuton

Back 53

--inhibits synthesis of all leukotrienes by inhibiting 5-lipoxygenase enzyme

--used concomitantly with inhaled corticosteroids for moderate persistent asthma

--attenuates bronchoconstriction from exercise and from aspirin in aspirin-sensitive people

--can cause liver toxicity
-may inhibit metabolism of warfarin and theophylline due to its metabolism by several CYPs

Front 54

Omalizumab

Back 54

--for adults and teens with severe persistent asthma who have a positive skin test to an aeroallergen and whose symptoms are not well controlled with inhaled corticosteroids or LABA's

--monoclonal antibody that inhibits binding of IgE to IgE receptor on mast cells and basophils
--leads to reduction in number of IgE receptors on basophils in atopic patients

--half-life is about 26 days
--administered subQ

--doses are determined by patient's serum total IgE level

--may cause anaphylactic reactions that can occur between 2h or 4 days after injection

Front 55

Theophylline

Back 55

--used as an adjuvant to inhaled corticosteroids for prevention of nocturnal asthma symptoms

--causes smooth muscle relaxation

--oral drug
--routine serum concentration monitoring is required since high levels can cause insomnia, tremor, anorexia, and even seizures and cardiac arrhythmias

Front 56

Prednisone

Back 56

--systemic corticosteroid

--has 4x as much glucocorticoid/antiinflammatory activity compared to mineralocorticoid activity

--used in the long-term prevention and control of symptoms in severely uncontrolled asthma

--used as "burst" therapy when initiating long-term asthma therapy in a patient

Front 57

Cortisol

Back 57

--corticosteroid produced by fasciculata zone of adrenal cortex
--cortisol release is controlled by ACTH pulses

--stimulates hepatic glucose formation while diminishing glucose use in the periphery to protect glucose dependent tissues like the brain and heart

--potency of antiinflammatory effect to mineralocorticod effect is 1:1

--used as replacement therapy in the case of primary adrenal insufficiency (Addison's disease)

Front 58

Aldosterone

Back 58

--mineralocorticoid produced by the glomerulosa zone of the adrenal cortex
--aldosterone release is also regulated by angiotensin

--acts in kidneys to increase sodium reuptake and to increase K+ and H+ excretion
--leads to increased extracellular fluid and increased blood pressure
--has very little (almost zero) antiinflammatory effect

Front 59

Dexamethasone

Back 59

--synthetic corticosteroid
--has 30x the antiinflammatory effect of cortisol
--no mineralocorticoid effect

-- Dexamethasone Suppression Test: used to dx Cushings; principle of the test - if you give low dose dex to normal person, ACTH will be turned "off"; if 4x that dose is needed to turn off ACTH, the patient has Cushing's disease

Front 60

Fludrocortisone

Back 60

--synthetic corticosteroid
--has 10x the anti-inflammatory effect of cortisol
--has 125x the sodium retention effect of cortisol

--sometimes used as a supplement to cortisol replacement therapy to better regulate blood pressure

Front 61

Triamcinolone

Back 61

--synthetic corticosteroid
--just like dexamethasone, has no sodium retention effect
--has 5x the antiinflammatory effect of cortisol

Front 62

Estradiol

Back 62

--endogenous steroid hormone derived from testosterone via the enzyme aromatase

--controls early to mid- menstrual cycle
--effects: development of 2ndary sex characteristics, proliferation of endometrium, increased uterine and tubal motility, watery cervical secretions

--substantial first pass metabolism, which limits its oral utility

Front 63

Estrone

Back 63

--endogenous steriod hormone derived from androstenedione via the enzyme aromatase

--substantial first pass metabolism, which limits its oral utility

Front 64

Ethinylestradiol
Mestranol

Back 64

--semi-synthetic estrogen agonists derived from estradiol

--have 17-ethinylation modification which blunts the 1st pass metabolism that natural estrogens experience

--clinical uses: post-menopausal hormone replacement and osteoporosis prevention; dysmenorrhea; contraception

Front 65

Diethylsilbestrol

Back 65

--most potent synthetic estrogen
--useful for inoperable prostatic cancer

--its use in the past to maintain pregnancies in habitual aborters led to teratogenic effects

Front 66

Progesterone

Back 66

--endogenous steroid hormone
--dominates in late menstrual cycle to develop secretory endometrium, produce viscous cerival secretions and to decrease uterine motility

--maintains pregnancy
--has thermogenic effect

--well absorbed but experiences high 1st pass metabolism

Front 67

Medroxyprogesterone

Back 67

--semi-synthetic progesterone

--useful as a long-acting injection for the purpose of female contraception

Front 68

Norethindrone
Norethynodrel
Ethynodiol
Norgestrel

Back 68

--19-nortestosterones
--synthetic progesterones

--orally useful
--clinical uses: dysfunctional uterine bleeding, contraception

--used to quiet the uterus in the case of a threatened abortion if patient has luteal dysfunction and inadequate progesterone production

Front 69

Clomiphene

Back 69

--estrogen receptor antagonist
--useful for anovulatory infertility treatment if the cause of the anovulation is related to endocrine feedback problems

Front 70

Tamoxifen

Back 70

--estrogen receptor antagonist
--useful for management of estrogen dependent cancer (i.e. breast cancer)

Front 71

Anastrazole
Exemestane

Back 71

--aromatase inhibitors
--allows decrease in estrogen action without interference of H-P-O axis or use of receptor antagonists

--often used in the treatment of breast cancer

Front 72

Raloxifene

Back 72

--selective estrogen receptor modulator (SERM)

--useful for maintaining bone mass post-menopause without stimulation of breast or uterine tissue

Front 73

Mefipristone [RU-486]

Back 73

--progesterone receptor antagonist
--useful as an abortifacient since it reverses uterine quieting effect of progesterone

Front 74

GnRH analogs
(FSH, hMG, hCG)

Back 74

--used to mimic pituitary function and stimulate the ovary in fertility therapy
--also useful in treatment of endometriosis

Front 75

Bromocryptine

Back 75

--dopamiineric agonist
--decreases prolactin release

--useful in the suppression of postpartum lactation

Front 76

Oxytocin

Back 76

--hormone from posterior pituitary that increases rate and force of uterine contraction
--stimulus for release is stretch sensed at the uterus, vagina, breasts

--uterine sensitivity to oxytocin increases in the 3rd trimester of pregnancy
--only a gravid uterus will respond to oxytocin

--short plasma half-life
--involved in a neuroendocrine reflex

Front 77

Prostaglandin E2, (aka: Dinoprostone)
Misoprostol

Back 77

--prostaglandins and oxytocic agents
--good activity on both gravid adn non-gravid uterus

--dinosprostone useful as an abortifacient and for ripening the cervix and for control of post-partum bleeding

Front 78

Ergonovine
Methylergonovine

Back 78

--ergot alkaloids and oxytocic agents
--NOT used for labor induction
--used to control post-partum bleeding

Front 79

MgSO4

Back 79

--tocolytic agent
--used to prolong pregnancy til the fetus is viable

--if patient experiences hallucinations, can give calcium gluconate to reverse MgSO4 effects

Front 80

MgSO4
Ritodrine
Terbutaline
Indomethacin
Nifedipine

Back 80

--tocolytic agents
--used to prolong pregnancy until the fetus is viable

--ritodrine and terbutaline are beta-2 agonsits

Front 81

Ipecacuanha

Back 81

--rapidly induces emesis
--used to treat non-corrosive poisoning when patient is conscious

--mechanism: irritatnt action that acts locally in the stomach

Front 82

Apomorphine

Back 82

--morphine derivative
--induces emesis

--acts on CTZ to activate DA receptors

Front 83

L-DOPA

Back 83

--induces emesis

--converted in the liver to dopamine

--increased extracerebral dopamine concentration stimulates D2-receptors in CTZ to induce vomiting

Front 84

Cinnarzine
Cyclizine

Back 84

--H1-receptor antagonists
--anti-emetic agents

--act against substances in the stomach but are ineffective agaisnt substances acting in CTZ

--good agents for control of motion sickness

Front 85

Promethazine

Back 85

--H-1 antagonist

--acts against substances in the stomach but ineffective against substances acting in the CTZ
--act at level of vestibular nucleus in the medulla

--used to treat severe morning sickness

Front 86

Hyoscine

Back 86

--muscarinic-receptor antagonist
--acts on vestibular nucleus and vomiting center to block visceral afferents activated by stimuli in the stomach

--most potent drug for prevention of motion sickeness but NOT effective against agents that stimulate the CTZ

Front 87

Metoclopramide

Back 87

--D2 receptor antagonist
--anti-emetic

--acts centrally in CTZ
--acts peripherally by antagonism of 5HT-3 receptors

Front 88

Domperidone

Back 88

--D2 receptor antagonist
--anti-emetic

--acts peripherally but NOT centrally
--preferred in treatment of vomiting caused by L-DOPA

--mainly used to inhibit vomiting associated with chemo and radiation

Front 89

Ondansetron
Granisetron

Back 89

--5HT-3 antagonists
--anti-emetics

--useful for treating emesis due to cytotoxic drugs

--anti-emetic action synergizes with use of steroids

Front 90

Nabilone

Back 90

--synthetic cannabinol derivative
--anti-emetic

--acts on CTZ
--side effects: drowsiness, dry mouth, dizziness

Front 91

Cimetidine

Back 91

--H2 receptor antagonist
--used in treatment of ulcers

--promote healing of gastric and duodenal ulcers
--useful in hypersecretory states since it reduces acid secretion by 70%
--useful in treatment of Zollinger-Ellison Syndrome

--may cause gynecomastia, prolactin release, male impotence
--binds to testosterone receptors
--may increase half-life of many drugs due to inhibition of microsomal enzymes

Front 92

Ranitidine
Nizatidine

Back 92

--H2 receptor antagonits
--used in treatment of ulcers

--5-10x more potent than cimetidine

--no anti-androgenic properties
--do not alter drug metabolism
--do not bind testosterone receptors

Front 93

Famotidine

Back 93

--H2 receptor antagonist

--2x more potent than ranitidine (the latter is 5-10x more potent than cimetidine)

Front 94

Propantheline
Isopropamide
Scopolamine
Atropine

Back 94

--cholinergic antagonists
--used to treat ulcers
--anti-diarrheals

--decrease ACh stimulated acid secretion and GI motility
--useful in patients with ulcers who are resistant to H2 antagonist therapy

--reduce colonic cramping but has little effect on diarrhea

Front 95

Calcium carbonate

Back 95

--antacid
--partially absorbed fom GI
--stimulates gastrin release which may cause rebound acid production

--containdicated in people with renal disease
--may cause hypercalcemia

Front 96

Aluminum hydroxide

Back 96

--antacid
--not absorbed from GI

--binds bile acids
--may cause constipation
--stimulates mucus secretion

Front 97

Magnesium hydroxide

Back 97

--antacid
--not absorbed from GI
--may cause diarrhea
--can cause hypotension

Front 98

Sodium bicarbonate

Back 98

--absorbed systemically
--not for long term therapy

--contraindicated in those iwth HTN

Front 99

Omeprazole

Back 99

--proton pump inhibitor
--heals erosive esophagitis more rapidly than H2 blockers
--provides ulcer symptom relief

--inhibits parietal cell proton pump
--reduces acid secretion

--used in treatment of H.pylori infections

--useful in treatment of ulcers in esophagus, duodenum, stomach
--used in management of Zollinger-Ellison Syndrome

--may cause gastrin cell hypertrophy
--inhibits microsomal enzymes

Front 100

Urogastrone
Enterogastrone

Back 100

--decrease gastric acid secretion (both basal and stimulated)

Front 101

Sulcralfate

Back 101

--protective agent used in treatment of ulcers

--complex polysaccharide complexed with aluminum hydroxide that forms crosslinks as a result of acidic gastric pH

--polymer has affinity for exposed proteins in peptic ulcers
--may cause nausea and constipation

Front 102

Psyllium
Dietary fiber

Back 102

--laxatives
--retain water in the bowel
--increased mass results in stimulated peristalsis

--laxation occurs after 2-4 days

Front 103

Polycarbophil
Calcium polycarbophile

Back 103

--laxative
--retain 60-100x its weight in water

--calcium polycarbophil releases calcium into the intestinal tract and should be avoided in patients who have hypercalcemia or are taking tetracyclines

Front 104

Magnesium sulfate
Magnesium citrate
Magnesium hydroxide
Sodium phosphates
Mineral waters

Back 104

-- salt-containg laxatives
--retain water by osmosis

--used in bowel evacuation
--used in the elimination of parasites afer therapy

Front 105

Glycerine
Lactulose
Polythylene glycol

Back 105

--non-salt containing osmotic agents
--laxatives

Front 106

Diphenylmethane derivatives
Bisacodyl
Anthraquinones

Back 106

--irritant agents
--cause decreased water absorption in gut lumen
--stimulates intestinal secretions and peristalsis

Front 107

Docusates

Back 107

--wetting agent
--laxative

--promotes mixing of water and fatty substances to increase intestinal mass
--short term laxation

Front 108

Mineral oil

Back 108

--coating agent
--laxative

--coats feces and reduces water absorption

Front 109

Kaolin
Pectin
Dietary Fiber

Back 109

--adsorbent agents
--anti-diarrheal agents

--absorb toxic compounds from intestinal waer

Front 110

Bismuth

Back 110

--anti-diarrheal agent
--inhibits prostaglandin production
--reduces intestinal secretion
--may cause tinnitus

Front 111

Loperamide

Back 111

--anti-diarrheal agent
--binds to opiod receptors in GI tract

--little CNS activity

Front 112

Diphenoxylate
Codeine

Back 112

--anti-diarrheal opiod preparations
--act on mu receptors to decrease transit rate
--stimulates segmental contractions of intestines but inhibits longitudinal contractions

--may cause nausea, sedation and vomiting

Front 113

Penicillin G

Back 113

--beta-lactam cell wall synthesis inhibitor

--IV or IM
--99% eliminated by kidney
--distributes widely
--gets into the CFS in the presence of meningeal inflammation
--repository forms include procaine and benzathine

Front 114

Penicillin V

Back 114

--beta-lactam cell wall synthesis inhibitor

--resistant to gastric acid (unlike Pen G)
--oral administration

Front 115

Methicillin
Oxacillin
Cloxacillin
Dicloxacillin
Nafcillin

Back 115

--beta lactam cell wall synthesis inhibitors
--penicillinase-resistant penicillins

--only uesd to treat penicillinase-producing staphylococci

Front 116

Ampicillin

Back 116

--beta lactam cell wall synthesis inhibitor

--given orally, IM or IV
--active against Gm(+) and E.coli, H.influenza, Salmonella and Shigella

--may cause diarrhea
--along with amoxicillin, may cause a non-immune mediated rash

Front 117

Amoxicillin

Back 117

--beta lactam cell wall synthesis inhibitor

--oral administration

--similar spectrum to ampicillin but amoxicililn is not used to treat shigellosis

--along with ampicillin, may cause a non-immune mediated rash

Front 118

Carbenicillin
Ticarcillin
Piperacillin

Back 118

--beta lactam cell wall synthesis inhibitors
--antipseudomonal penicillins

--often combined with aminoglycosides to treat serious Pseudomonas infections

--carbenicillin and ticarcillin may cause impaired platelet aggregation and electrolyte disturbances

Front 119

Piperacillin

Back 119

--beta lactam cell wall synthesis inhibitor
--antipseudomonal penicillin

--"ureide" penicillin
--active vs. Gm(-) and Gm(+) bac

--chief advantage is activity vs Pseudomonas and Klebsiella

Front 120

Clavulanic acid
Sulbactam
Tazobactam

Back 120

--B-lactamase inhibitors
--irreversibly inactivate some B-lactamases and prevent inactivation of penicillins

--amoxicillin + clavulanic acid
--ampicillin + sulbactam
--piperacillin + tazobactam
--ticarcillin + clavulanic acid

Front 121

Cephalexin
Cefazolin

Back 121

--1st gen cephalosporins
--B-lactam cell wall synthesis inhibitors

--active vs. Gm(+) cocci and E.coli, Klebsiella

--cefazolin is eliminated via glomerular filtration with tubular secretion playing a 2ndary role, meaning that it has a longer half-life

Front 122

Cefuroxime
Cefaclor
Cefotetan

Back 122

--2nd gen cephalosporins
--B-lactam cell wall synthesis inhibitors

--less active vs. Gm(+) bac compared to 1st gen but slower to be hydrolyzed by Gm(-) B-lactamases

--active against Gm(+) and E.coli, Klebsiella, Proteus, H.influenza and M.catarrhalis

--cefotetn has added activity vs B.fragilis

Front 123

Cefotaxime
Ceftazidime
Ceftriaxone

Back 123

--3rd gen cephalosporins
--B-lactam cell wall synthesis inhibitors

--expanded Gm(-) spectrum: Enterobacteria, Pseudomonas, N.gonorrhea

--penetrates CNS (unlike 1st and 2nd generation)

Front 124

Cefepime

Back 124

--4th gen cephalosporin
--B lactam cell wall synthesis inhibitor

--most resistant to Gm(-) B-lactamases

Front 125

Imipenem

Back 125

--B lactam cell wall synthesis inhibitor

--formulated with cilistatin
--treats nosocomial UTI's

--has some cross-sensitivity with penicillins and cephalosporins

Front 126

Aztreonam

Back 126

--B lactam cell wall synthesis inhibitor
--only useful vs aerobic Gm(-) bac
--very stable to B-lactamase
--no cross-reactivity with other B-lactams

Front 127

Vancomycin

Back 127

--cell wall synthesis inhibitor
--binds to terminal D-ala-D-ala to inhibit transglycosylase

--narrow Gm(+) spectrum: MRSA, antibiotic-induced enterocolitis, penicillin-resistant Strep
--may cause red neck syndrome

Front 128

Erythromycin

Back 128

--macrolide protein synthesis inhibitor
--binds to 23S rRNA of 50S ribosome to inhibit translocation

--narrow spectrum: Strep, Staph, Mycoplasma pneumonia, Legionella

--concentrated in the liver and excreted in the bile

--not stable in gastric acid
--may cause abdominal cramping
--can cause cholestatic hepatitis
--inhibits P450 enzymes

Front 129

Clarithromycin

Back 129

--macrolide protein synthesis inhibitor
--binds to 23S rRNA of 50S ribosome to inhibit translocation

--excreted by the kidney

--less likely to cause GI upset compared to erythromycin
--may cause mania

Front 130

Azithromycin

Back 130

--macrolide protein synthesis inhibitor
--binds to 23S rRNA of 50S ribosome to inhibit translocation

--tissues act as reservoir for this drug
--excreted in the bile

--spectrum: Staph, Strep, Mycoplasma pneumonia, chlamydia, M.avium, H.influenza

Front 131

Telithromycin

Back 131

--protein synthesis inhibitor
--binds to domains II and V of the 23S rRNA of the 50S ribosome

--treats community acquired pneumonia

--not to be given to patients with hx of hepatitis or myasthenia gravis

Front 132

Clindamycin

Back 132

--protein synthesis inhibitor
--binds the 23S rRNA of the 50S ribosome

--spectrum: Staph, Strep, community-acquired MRSA, B.fragilis
--affinity for osseous tissues

--frequently associated with pseudomembranous colitis

Front 133

Quinupristin/Dalfopristin

Back 133

--protein synthesis inhibitors
--bind to 50S ribosome
--no cross resistance with other agents

--specturm: Gm(+), nosocomial infections; bloodstrem infection with VREF; skin infection with Staph or Strep

Front 134

Linezolid

Back 134

--protein synthesis inhibitors
--bind to 50S ribosome

--oral bioavailability is close to 100%

--spectrum: Gm(+) bac; VRE, MRSA, VISA, GISA; all enterococci; penicillin-susceptible and resistant Strep.

--may cause myelosuppression, peripheral neuropathy and serotonin syndrome

Front 135

Chloramphenicol

Back 135

--protein synthesis inhibitors
--bind to 50S ribosome

--rapidly absorbed from the GI tract
--conjugated in lier by glucuronosyl transferase

--only used to treat infections that cannot be treated with other antibioitics

--can cause aplastic anemia, blood dyscrasias and gray-baby syndrome

Front 136

Tetracycline
Minocycline
Doxycycline

Back 136

--protein synthesis inhibitors
--bind to 30S ribosome

--absorption is impaired by milk and aluminum hydroxide antacid
--tetracycline and minocycline are eliminated via glomerular filtration while doxycycline is excreted in the feces

--doxycycline has a longer hal-life and doesn't accumulate in patients with compromised renal function

--spectrum: rickettsiae, chlamydia, H.pylori, plasmodia and amebas

--may cause photoxic reaction, teeth discoloration, hypersensitivity and GI irritation

Front 137

Doxycycline

Back 137

--protein synthesis inhibitor
--binds to 30S ribosome

--tetracycline and minocycline are eliminated via glomerular filtration while doxycycline is excreted in the feces

--doxycycline has a longer hal-life and doesn't accumulate in patients with compromised renal function

Front 138

Tigecycline

Back 138

--protein synthesis inhibitor
--binds to 30S ribosome
--no cross resistance

--spectrum: MRSA, VRE, penicillin-resistant Strep; Acinetobacter resistant to imipenem

Front 139

Gentamicin
Tobramycin
Amikacin

Back 139

--aminoglycoside protein synthesis inhibitors
--concentration-dependent killing

--poorly absorbed after oral administration
--distributes in all extracellular fluids
--excreted by glomerular filtration (with active reabsorption)

--treat systemic infections due to Gm(-) bacteria

--amikacin may be active against some organisms that are resistant to gentamicin or tobramycin

--may cause ototoxicity and nephrotoxicity
--may cause neuromuscular blockade

Front 140

Ciprofloxacin
Levofloxacin
Gatifloxacin
Moxifloxacin

Back 140

--fluoroquinolones
--inhibit bacterial DNA gyrase in Gm(-) and topoisomerase IV in Gm(+)

--ciprofloxacin is most effective vs. Pseudomonas compared to other fluoroquinolones

--levo-, gati- and moxifloxacin are more active vs. Strep, including MDRSP

Front 141

Rifampin

Back 141

--inhibits DNA-dep RNA polyermase
--2nd most important drug in treatment of TB (after isoniazid)

--alone, given as prophylaxis to people exposed to N.meningitidis or carriers of N.meningitidis

--often used in combo to treat other infections like MRSA, legionella

--potent inducer of CYP3A4

Front 142

Sulfisoxazole
Sulfamethoxazole

Back 142

--antimetabolite antibiotics
--competitive inhibitors of dihydropteroate synthetase, leading to depletion of folic acid in bacteria

--absorbed rapidly after oral administration
--acetylated and excretion in the urine

--treat UTI's

--most toxic effects involve skin
--can cause kernicterus

Front 143

Sulfacetamide

Back 143

--antimetabolite antibiotic
--competitive inhibitor of dihydropteroate synthetase, leading to depletion of folic acid in bacteria

--absorbed rapidly after oral administration
--acetylated and excretion in the urine

--treats ophthalmic infections (conjunctivitis)

--most toxic effects involve skin
--can cause kernicterus

Front 144

Silver Sulfadiazine

Back 144

--antimetabolite antibiotic
--competitive inhibitor of dihydropteroate synthetase, leading to depletion of folic acid in bacteria

--absorbed rapidly after oral administration
--acetylated and excretion in the urine

--prevents colonization of burns by bacteria

--most toxic effects involve skin
--can cause kernicterus

Front 145

Sulfasalazine

Back 145

--antimetabolite antibiotic
--competitive inhibitor of dihydropteroate synthetase, leading to depletion of folic acid in bacteria

--absorbed rapidly after oral administration
--acetylated and excretion in the urine

--ulcerative colitis treatment

--most toxic effects involve skin
--can cause kernicterus

Front 146

Trimethoprim

Back 146

--antimetabolite antibiotic
--inhibits dihydrofolate reductase, which blocks dihydrofolate reduction to tetrahydrofolate

--TMP + SMZ exerts a synergistic and bactericidal effect

Front 147

Trimethoprim

Back 147

--antimetabolite antibiotic
--inhibits dihydrofolate reductase, which blocks dihydrofolate reduction to tetrahydrofolate

--TMP + SMZ exerts a synergistic effect

Front 148

Daptomycin

Back 148

x

Front 149

Sulfisoxazole
Sulfamethoxazole

Back 149

--antimetabolite antibiotics
--competitive inhibitors of dihydropteroate synthetase, leading to depletion of folic acid in bacteria

--absorbed rapidly after oral administration
--acetylated and excretion in the urine

--treat UTI's

--most toxic effects involve skin
--can cause kernicterus

Front 150

Colistin (Polymixin E)
Polymixin B

Back 150

x

Front 151

Sulfacetamide

Back 151

--antimetabolite antibiotic
--competitive inhibitor of dihydropteroate synthetase, leading to depletion of folic acid in bacteria

--absorbed rapidly after oral administration
--acetylated and excretion in the urine

--treats ophthalmic infections (conjunctivitis)

--most toxic effects involve skin
--can cause kernicterus

Front 152

Metronidazole

Back 152

x

Front 153

Silver Sulfadiazine

Back 153

--antimetabolite antibiotic
--competitive inhibitor of dihydropteroate synthetase, leading to depletion of folic acid in bacteria

--absorbed rapidly after oral administration
--acetylated and excretion in the urine

--prevents colonization of burns by bacteria

--most toxic effects involve skin
--can cause kernicterus

Front 154

Sulfasalazine

Back 154

--antimetabolite antibiotic
--competitive inhibitor of dihydropteroate synthetase, leading to depletion of folic acid in bacteria

--absorbed rapidly after oral administration
--acetylated and excretion in the urine

--ulcerative colitis treatment

--most toxic effects involve skin
--can cause kernicterus

Front 155

Spectinomycin

Back 155

x

Front 156

TMP-SMZ

Back 156

--trimethoprim + sulfamethoxazole

--trimethoprim interferes with folate utilization and inhibits dihydrofolate reductase
--sulfamethoxazole intereferes with folate synthesis and inhibits dihydropteroate synthetase

--TMP-SMZ treats conditions where sulfonamides alone are ineffective (bronchitis, otitis media)

--TMP-SMZ is the drug of choice for treatment of Pneumocystis jiroveci

Front 157

Pyrimethamine

Back 157

--used in combination with the sulfonamides to treat toxoplasmosis

Front 158

Nitrofurantoin

Back 158

--urinary tract antiseptic
--no systemic activity and rapidly excreted by kidney

--treats acute cystitis and is a UTI prophylaxis

--serious toxic effect involves lungs (chills, cough, pulmonary infiltrations)

Front 159

Daptomycin

Back 159

--acts at bacterial cytoplasmic membrane
--binds to cell membane of Gm(+) bac and disrupts cell membrane potential by forming pores, allowing K+ ions to leak out

--spectrum overlaps vancomycin

Front 160

Pyrimethamine

Back 160

--used in combination with the sulfonamides to treat toxoplasmosis

Front 161

Pyrimethamine

Back 161

--used in combination with the sulfonamides to treat toxoplasmosis

Front 162

Colistin, Polymyxin E
Polymyxin B

Back 162

--act at bacterial cytoplasmic membrane
--have lipophilic and lipophobic groups and penetrate cell membranes

--fell into disuse by 1980 b/c of nephrotoxicity

--occasionally needed to treat Pseudomonas and other resistant Gm(-) bac

Front 163

Metronidazole

Back 163

--miscellaneous antibiotic
--bacteria reduce its nitro group to generate free radicals

--antiprotozoal agent but effective vs. anaerobic bac like C.difficile

-may cause metallic taste or disulfuram-like reaction

Front 164

Nitrofurantoin

Back 164

--urinary tract antiseptic
--no systemic activity and rapidly excreted by kidney

--treats acute cystitis and is a UTI prophylaxis

--serious toxic effect involves lungs (chills, cough, pulmonary infiltrations)

Front 165

Nitrofurantoin

Back 165

--urinary tract antiseptic
--no systemic activity and rapidly excreted by kidney

--treats acute cystitis and is a UTI prophylaxis

--serious toxic effect involves lungs (chills, cough, pulmonary infiltrations)

Front 166

Daptomycin

Back 166

--acts at bacterial cytoplasmic membrane
--binds to cell membane of Gm(+) bac and disrupts cell membrane potential by forming pores, allowing K+ ions to leak out

--spectrum overlaps vancomycin

Front 167

Daptomycin

Back 167

--acts at bacterial cytoplasmic membrane
--binds to cell membane of Gm(+) bac and disrupts cell membrane potential by forming pores, allowing K+ ions to leak out

--spectrum overlaps vancomycin

Front 168

Colistin, Polymyxin E
Polymyxin B

Back 168

--act at bacterial cytoplasmic membrane
--have lipophilic and lipophobic groups and penetrate cell membranes

--fell into disuse by 1980 b/c of nephrotoxicity

--occasionally needed to treat Pseudomonas and other resistant Gm(-) bac

Front 169

Colistin, Polymyxin E
Polymyxin B

Back 169

--act at bacterial cytoplasmic membrane
--have lipophilic and lipophobic groups and penetrate cell membranes

--fell into disuse by 1980 b/c of nephrotoxicity

--occasionally needed to treat Pseudomonas and other resistant Gm(-) bac

Front 170

Metronidazole

Back 170

--miscellaneous antibiotic
--bacteria reduce its nitro group to generate free radicals

--antiprotozoal agent but effective vs. anaerobic bac like C.difficile

-may cause metallic taste or disulfuram-like reaction

Front 171

Metronidazole

Back 171

--miscellaneous antibiotic
--bacteria reduce its nitro group to generate free radicals

--antiprotozoal agent but effective vs. anaerobic bac like C.difficile

-may cause metallic taste or disulfuram-like reaction

Front 172

Spectinomycin

Back 172

--miscellaneous antibacterial
--treats N.gonorrhea but not T.pallidum

Front 173

Isoniazid

Back 173

--primary agent in treatment of TB
--only drug approved for prophylaxis of TB

--rate limiting step for its elimination is acetylation, making a patient's acetylator status very important

--may cause peripheral neuropathy like that of vitB6 deficiency
--may cause hepatotoxicity

Front 174

Ethambutol

Back 174

--treats mycobacterial infections
--may cuase ocular toxicity and hyperuricemia

Front 175

Pyrazinamide

Back 175

--treats mycobacterial infections

Front 176

Streptomycin

Back 176

--aminoglycoside

--all other anti-tubercular drugs are taken orally but streptomycin must be injected

Front 177

Dapsone
Clofazimine
Rifampin

Back 177

--treat leprosy

--dapsone inhibits folic acid synthesis
--clofazimine intereferes with bac DNA replication

Front 178

Nystatin

Back 178

--polyene anti-fungal agent
--binds to ergosterol and alters membrane permeability

--for LOCALIZED fungal infections

Front 179

Amphotericin B

Back 179

--polyene antifungal agent
--gold standard for treating serious fungal infections

--given IV and has half-life of 15days

--can cause hypersensitivity
--causes decreased renal function

Front 180

Flucytosine

Back 180

--anti-fingal agent
--doesn't bind to ergosterols; instead it is concerted to 5-FU and causes RNA miscoding and DNA syn inhibition

--synergistic with amphotericin B

--can cause BM depression, GI upset, hepatic dysfunction

Front 181

Itraconazole

Back 181

--anti-fungal agent
--most potent of the azoles

--inhibit fungal enzyme that converts lanosterol to ergosterol

--spectrum: common fungi like Blastomyces, Candida, Cryptococcus, Coccidiodes

--good activity vs. Aspergillus
--distributes well into lipohilic tissues but not so well into aqueous tissues

--accumulates in stratum corneum

--its major metabolite is active

Front 182

Itraconazole

Back 182

--anti-fungal agent
--most potent of the azoles

--inhibit fungal enzyme that converts lanosterol to ergosterol

--spectrum: common fungi like Blastomyces, Candida, Cryptococcus, Coccidiodes

--good activity vs. Aspergillus
--distributes well into lipohilic tissues but not so well into aqueous tissues

--accumulates in stratum corneum

--its major metabolite is active

Front 183

Fluconazole

Back 183

--anti-fungal agent
--inhibit fungal enzyme that converts lanosterol to ergosterol

--wide distribution (urine, skin >> saliva, nails, blister, plasma)

--distributes well into CSF
--spectrum: common fungi like Blastomyces, Candida, Cryptococcus, Coccidiodes

--eliminated via kidneys

--of the azoles, least likely to ihibit P450's

Front 184

Fluconazole

Back 184

--anti-fungal agent
--inhibit fungal enzyme that converts lanosterol to ergosterol

--wide distribution (urine, skin >> saliva, nails, blister, plasma)

--distributes well into CSF
--spectrum: common fungi like Blastomyces, Candida, Cryptococcus, Coccidiodes

--eliminated via kidneys

--of the azoles, least likely to ihibit P450's

Front 185

Voriconazole

Back 185

--anti-fungal agent
--inhibit fungal enzyme that converts lanosterol to ergosterol

--spectrum: common fungi like Blastomyces, Candida, Cryptococcus, Coccidiodes

--treats invasive funal infections (including aspergillosis in kids who are refractory to other therapy)

Front 186

Voriconazole

Back 186

--anti-fungal agent
--inhibit fungal enzyme that converts lanosterol to ergosterol

--spectrum: common fungi like Blastomyces, Candida, Cryptococcus, Coccidiodes

--treats invasive funal infections (including aspergillosis in kids who are refractory to other therapy)

Front 187

Terbinafine

Back 187

--anti-funal agent
--inhibits funal enzyme, squalene epoxidase, and prevents epoxidation (early important step in ergosterol synthesis)

--spectrum: dermatophytes, Cryptococcus, some Candida and Aspergillus

--with amphotericin B or itraconazole or voriconazole, has synergistic interactions vs. Aspergillus

Front 188

Terbinafine

Back 188

--anti-funal agent
--inhibits funal enzyme, squalene epoxidase, and prevents epoxidation (early important step in ergosterol synthesis)

--spectrum: dermatophytes, Cryptococcus, some Candida and Aspergillus

--with amphotericin B or itraconazole or voriconazole, has synergistic interactions vs. Aspergillus

Front 189

Caspofungin

Back 189

--anti-fungal agent
--inhibits synthesis of beta-1,3-D-diglucans, a component of fungal cell wall

--treats azole-resistant aspergillosis

Front 190

Caspofungin

Back 190

--anti-fungal agent
--inhibits synthesis of beta-1,3-D-diglucans, a component of fungal cell wall

--treats azole-resistant aspergillosis

Front 191

Emtricitabine
Tenofovir
Abacavir
Lamivudine
Didanosine
Zidovudine

Back 191

--nRTI's
--purine or pyrimidine analogs that require intracellular phophorylation to triphospate forms

--act as competitive inhibitors of normal nucleoside triphosphates for HIV reverse transcriptase
--incroporate into growing proviral DNA chains and act as chain terminators

--cause lactic acidosis, hepatic steatosis, neuropathy, myopathy, lipoatrophy

--inhibit mitochondrial DNA polymerase-gamma

Front 192

Efavirenz
Nevirapine

Back 192

--nnRTI's
--bind to pocket near active site of HIV reverse transcriptase and "lock" enzyme into inactive state

--not active against HIV-1 O subtype or HIV-2

--may cause rash
--involved in drug interactions since metabolized by P450's

Front 193

Atazanavir
Fosamprenavir
Darunavir
Lopinavir
Saquinavir

Back 193

--protease inhibitors
--HIV treatment

--inhibit HIV protease that cleaves gag and gag-pol polyprotein precursors

--may cause bleeding in hemophiliacs, insulin resistance, fat wasting and redistribution, lipodystrophy, hyperlipidemia

--rifampin decreases their effectiveness

Front 194

Enfuvirtide

Back 194

--fusion inhibitor
-- 2ndary HIV treatment
--bind gp41 on HIV to prevent HIV envelope from fusing with cell membrane of host CD4 cells

Front 195

Maraviroc

Back 195

--entry inhibitor
--2ndary HIV treatment

--binds to CCR5 on human CD4+ cells so that HIV can't bind and enter the cell

Front 196

Raltegravir

Back 196

--integrase inhibitor
--2ndary HIV treatment

--prevents insertion of HIV DNA into human genome

Front 197

Amantadine
Rimantadine

Back 197

--anti-virals
--block M2 protein found only in influenza A viruses
--inhibits viral uncoating

--major use is prophylaxis during influenza A epidemics

--CNS adverse effects: confusion, hallucination, seizure, coma

Front 198

Oseltamivir
Zanamivir

Back 198

--anti-virals
--inhibit viral neuraminidase so that sialic acid residues are not removed from virus surface

--sialic acid residues interact with hemagglutinin, causing virus particles to clump, rendering them noninfectious

-active against both influenza A and B

--zanamivir given via inhalation and can cause bronchospasm

--oseltamivir given orally and my cause delirium in kids

Front 199

Ribavirin

Back 199

--anti-viral
--phosphorylated intracellularly to a triphosphate to inhibit guanosine triphosphate-dependent 5'-capping of influenza viral mRNA

--active against influenza, RSV, adenovirus

--with INF-alpha, treats hepatitis C infections

Front 200

Acyclovir
Valacyclovir

Back 200

--anti-virals
--phosphorylated by viral thymidine kinase then converted to triphosphate by mammalian enzymes

--inhibits viral DNA polymerase and incorporates into viral DNA to cause chain termination

--acyclovir activity: HSV-1,2 > VZV > CMV

--valacyclovir is metabolized to acyclovir and has better oral availability

Front 201

Famciclovir
Penciclovir

Back 201

--nucleoside anti-virals

--famciclovir is the prodrug of penciclovir, which is an active moiety and does not require viral enzymes for its activation

--do not cause chain termination (whereas acyclovir does)

--active agaisnt HSV-1,2, VZV, EBV

Front 202

Ganciclovir
Valaganciclovir

Back 202

--nucleoside anti-virals
--nucleoside analog like acyclovir but has better activity vs. CMV and greater toxicity

--same mechanism of activation (viral enzyme phosphorylation) as acyclovir in HSV and VZV infected cells

--in CMV infected cells, ganciclovir is phosphorylated by a UL97 protein kinase, for which acyclovir is a poor substrate

--concentrations of ganciclovir in CMV infected cells is 10x higher than that of acyclovir

--can cause granulocytopenia, thrombocytopenia

--treats CMV retinitis, colitis, esophagitis and to treat CMV in transplant patients

Front 203

Cidofovir

Back 203

--nucleoside anti-viral
--alternate to ganciclovir

--treats CMV infections resistant to ganciclovir

Front 204

Trifluridine

Back 204

--nucleoside anti-viral
--for local application only because so toxic

--treats HSV keratoconjunctivitis

Front 205

Foscarnet

Back 205

--non-nucleoside antiviral

--last resort drug
--treats resistant CMV retinitis and resistant HSV and VZV

--can cause renal dysfunction

Front 206

Mechlorethamine

Back 206

--alkylating agent
--anti-cancer drug

--part of MOPP regimen in treating Hodgkin's

Front 207

Cyclophosphamide

Back 207

--alkyltaing agent
--anti-cancer drug
--effective immunosuppressant

--pro-drug
--may cause hemorrhagic cystitis (risk of this reduced by use of mesna which binds urotoxic metabolites)
--

Front 208

Chlorambucil
Melphalan
Busulfan
Temozolomide
Altretamine
Bendamustine

Back 208

--alkylating agents
--anticancer therapy

--common toxicities include myelosuppression, GI effects, reproductive effects, carcinogenesis

Front 209

Carmustine
Lomustine

Back 209

--nitrosourea alkylating agents
--anti-cancer drugs

--have high lipid solubility
--can cross BBB

--can cause delayed myelosuppression

Front 210

Streptozocin

Back 210

--alkylating agent
--anti-cancer drug

--can cause renal damage

--used to treat pancreatic islet cell carcinoma

Front 211

Procarbazine

Back 211

--alkylating agent
--anti-cancer drug

--may cause myelosuppression, CNS depression

--may cause disulfiram-like effect after drinking EtOH
--is a weak MAOI

Front 212

Dacarbazine

Back 212

--alkylating agent

--treats malignant melanoma

Front 213

Cisplatin

Back 213

--platinum compound
--anti-cancer drug

--similar mechanism to that of alkylating agents

--may cause nephrotoxicity and ototoxicity
--may cuase peripheral neuropathy, electrolyte disturbances, and anaphylactic-like rxns

Front 214

Carboplatin
Oxaliplatin

Back 214

--platinum compounds
--anti-cancer drugs

--carboplatin causes dose-limiting myelosuppression

--oxaliplatin causes dose-limiting peripheral neuropathy

Front 215

Methotrexate

Back 215

--folic acid analog
--anti-cancer drug

--inhibits DHFR to prevent formation of FH4

--other uses other than cancer include rheumatoid arthritis and psoriasis

--leucorvin is the antidote for excessive MTX dose

Front 216

Pemetrexed

Back 216

--folic acid analog
--anti-cancer drug

--inhibits thymidylate synthase

--supplement with folic acid and vitB12 to avoid toxic effects

Front 217

6-Mercaptopurine

Back 217

--purine analog
--anti-cancer drug

--metabolized by TPMT, making a patient's TPMT activity and polymorphisms important clinically

--if given with allopurinol, 6-MP dose must be reduced

--can cause myelosuppression, liver toxicity, immunosuppression

Front 218

6-Thioguanine

Back 218

--purine analog

--metabolized by TPMT just like 6-MP

--do NOT have to lower dose of 6-TG if it is given with allopurinol

Front 219

Fludarabine

Back 219

--purine analog
--anti-cancer drug

--a nucleotide that is dephosphorylated extracellularly and then re-phosphorylated to an active nucleotide in the cell

--myelosuppression, immunosuppression

Front 220

Cladribine

Back 220

--purine analog
--anti-cancer drug