Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
117 Cards in this Set
- Front
- Back
|
Antacids
|
Drugs used to neutralize gastric acid (HCl secreted by the parietal cells in the stomach); they are buffers
Like all inhibitors of gastric acid secretion, may interfere with the gastric absorption of some drugs that are acidic or weak bases |
|
|
Sodium bicarbonate
|
Alkaseltzer; antacid; obsolete; short-acting, not very effective; can lead to belching and flatulence because they are rapidly converted to CO2 in the gastric contents of the stomach
Can be used in an acute situation |
|
|
Calcium carbonate
|
TUMS; antacid; obsolete; short-acting, not very effective; can lead to belching and flatulence because they are rapidly converted to CO2 in the gastric contents of the stomach
Calcium, once it is absorbed, can enhance gastric acid secretion and can lead to a rebound of the stomach acidity; aren't used for long term benefits of controlling heart burn Can be used in an acute situation |
|
|
Magnesium hydroxide and aluminum hydroxide combinations
|
Mylanta, Maalox
Antacid, neutralizing gastric acid, act as a buffer Little longer duration, do not produce belching or flatulence Minimal risk of any type of toxicity except in patents with renal insufficiency Magnesium hydroxide alone causes diarrhea, aluminum hydroxide alone can cause constipation; balance each other out Often times given along with simethicone (an anti-foaming agent) to help reduce some of the gastroesophageal reflux Main use is for occasional dyspepsia or heart burn, indigestion, etc; not useful for chronic therapy or ulcers or chronic GERD |
|
|
PPIs
|
Proton pump inhibitors; Omeprazole, esomeprazole, lansoprazole; 1x/day dosing
Prodrugs that produce an irreversible blockade of gastric proton pump; new H/K ATPase must be synthesized to resume gastric acid secretion; Long lasting inhibition Must undergo systemic absorption; give on empty stomach Circulating drug concentrates in canaliculi of actively secreting parietal cells via "acid trapping" - eat one hour after dosing to initiate gastric acid secretion; conversion to active form occurs in acidic canalicili and produces irreversible block Rapid hepatic elimination (half life <2 hours); 3-4 days to max effect with daily dosing Preferred treatment of GERD, peptic/duodenal ulcers, prevention of NSAID induced ulcers; prevent stomach bleeding in critical-ill (stress-related gastritis) Do not give at the same time with Clopidogrel or plavix Adverse: slight increase risk of GI infections Minimal risk of major drug interactions |
|
|
"Triple therapy"
|
14 days PPI plus 2 antibiotics (clarithromycin plus amoxicillin or metronidazole) given bid preferred to eradicate H. Pylori; PPI is continued 4-6 weeks to ensure ulcer healing
|
|
|
H2 blockers
|
Cimetidine, ranitidine, famotidine, etc; same uses as PPIs, faster onset but less effective in reducing acid secretion; longer duration of action
Cimetidine is obsolete due to drug interactions (CYP450 inhibition) and weak inhibition of androgen receptors Preferred treatment for reducing stress-related gastritis in critically ill (IV admin) Widely used OTC for treatment/prevention of dyspepsia/heartburn (can take right before meal) Very safe, well tolerated |
|
|
Sucralfate
|
Mucosal protective agent; slurry designed to coat the surface and provde some barrier to have prevention benefits in stress-related gastritis
Given qid via n.g. tube |
|
|
Misoprostol
|
PGE1 analog, mucosal protective agent; can be given orally aid to prevent NSAID-induced ulcers
Adverse effects: diarrhea, abdominal cramps/pain Other potential uses: stimulate uterine contractions to expel an aborted fetus) |
|
|
Pepto bismol (Bismuth)
|
Mucosal protective agent; OTC treatment for dyspepsia and diarrhea
Bismuth has antimicrobial effect and also binds enterotoxins which are compounds produced by pathogenic bacteria in the GI tract that can enhance nausea, vomiting Could be included in a "quadruple treatment" for h. pylori (second line treatment) Anti-secretory, antimicrobial effects of bismuth plus anti-inflammatory effects of salicylic acid lead to OTC antidiarrheal use |
|
|
Metoclopramide
|
Prokinetic agent (stimulates GI motility); produces D2 blockade, weak D4 antagonism and weak H3 antagonism; suppresses inhibitory dopaminergic effects on ACh release from the myenteric plexus leading to propulsive contractions and release of secretions
Increases stomach emptying, increases motility in upper GI tract (little effect on lower GI/colon) Decreases nausea and committing due to chemoreceptor trigger zone stimulation Used to increase stomach emptying in diabetic or post-surgical gastric stasis, also used to treat GERD resistant to PPI/H2 blocker therapy Can be used as anti-emetic although other safer drugs preferred first Adverse CNS effect sin 10-20% (sedation, restlessness, anxiety, agitation in elderly, EPS) Black box warning for risk of tardive dyskinesia |
|
|
Erythromycin
|
Prokinetic agent; Macrolide antibiotic that stimulates receptor for moil in (GI peptide); sometimes used off label to treat gastric stasis
Tolerance rapidly develops |
|
|
Mehylnaltrexone, alvimopan
|
Opioid antagonists that do not cross the BBB; do not block analgesia but prevent opioid-induced constipation
|
|
|
Laxatives
|
Used to prevent/treat constipation; widely used OTC, few accepted indications: prevent or treat constipation post-surgery or due to opioid analgesics; management of diverse GI disorders associated with constipation; evacuation of bowel for examination or surgery
Contraindications: obstructive GI pathoogy Mechanisms diverse but all increase fluid content and decrease transit time |
|
|
Stimulant laxatives (mechanism)
|
Act on enteric nerves to increase colon contractions and secretions
Only one that is really considered safe and effective |
|
|
Bisacodyl
|
Stimulant laxative; 6-10 hour onset after oral dosing, 30-60 min onset with rectal dosing
Safe for acute and chronic use ay be used in combination with stool softeners to treat/prevent opioid-induced constipation, or in combination with an osmotic laxative before bowel surgery/exams |
|
|
Castor oil
|
Obsolete stimulant laxative - toxic and seldom used
|
|
|
Senna, cascara, aloes
|
Antraquinones; stimulant laxatives; 6-12 hr onset orally, 2 hours rectally
Available OTC but not recognized as safe or effective by the FDA |
|
|
Osmotic laxatives (mechanism)
|
solutions of poorly absorbed solutes that retain water in the GI tract via osmotic activate and possible other effects
|
|
|
Balanced (isotonic) polyethylene glycol-electrolyte solutions
|
Osmotic laxative
Safest regiment for bowel cleansing before exams Take 240 ml every 10 min until rectal effluent is clear No fluid shifts, safe in all patients Smaller doses safe to prevent and treat constipation |
|
|
Saline laxatives
|
Osmotic laxative
Magnesium or phosphate salts; fast acting (1-3 hours) Sodium phosphate - two-dose regiment for bowel cleansing before exams (evening dose, second dose 3-5 hours before exam); doses must be accompanied with intake of 1-3 L water to avoid potentially dangerous fluid and electrolyte shifts. Avoid in patients with renal and cardiac disease, electrolyte abnormalities. Tablets by prescription only Magnesium hydroxide (milk of magnesium), magnesium citrate - used to treat acute constipation; risk of hypermagnesemia with chronic use in patients with renal insufficiency |
|
|
Laculose, sorbitol, mannitol
|
Osmotic laxatives, indigestible sugars and alcohols
Slow acting (24-48 hours) Bacterial hydrolysis in lower GI tract can evoke flatulence, cramps Lactulose conversion to fatty acids by colonic bacteria produces acid trap, reduces blood ammonia in hepatic encephalopathy** |
|
|
Bulk forming laxatives
|
Bran, psyllium, methylcellulose, polycarbophil
Slow acting (1-3 days), indigestible colloids absorb water, distend colon, promote peristalsis Safe, physiological; can be used effectively and safely on daily basis Used mostly for prevention of constipation rather than acute management |
|
|
Stool softeners
|
Docusate, glycerin, mineral oil
Slow acting agents; surfactants that increase water and lipid content of stool Oral or rectal dosing Make bowel movements less irritating and painful Not useful for acute relief of constipation Doscusate is commonly given to hospitalized patients to prevent formation of hard, irritating feces |
|
|
Lubiprostone
|
Chloride channel activator; prescription prostanoic acid analog labeled for use in chronic constipation or IBS with constipation
Increases intestinal secretions by activating chloride channel |
|
|
Loperamide
|
Opiate antidiarrheal; widely used OTC
Meperidine analog with negligible CNS penetration Opiates bind to mu opioid receptor and decrease ACh release to inhibit peristalsis; increase non-propulsive GI muscle tone. Prolonged GI transite time allows greater water removal from intestinal contents and relieves diarrhea |
|
|
Diphyoxylate
|
Meperidine analog (prescription agent) with some CNS effects at high doses
Opiate antidiarrheal |
|
|
Octreotide
|
Antidiarrheal; Somatostatin analog that inhibits secretion of GI/pancreatic hormones and 5-HT; intestinal, pancreatic and bile secretions; gastrointestinal motility
Used for: dumping syndrome (diarrhea following gastric surgery); watery diarrhea, flushing, etc of carcinoid tumors and VIPomas; decreased portal pressure and vatical bleeding associated with chronic liver disease |
|
|
Amitryptyline
|
TCA antidepressant which can be used to reduce abdominal pain with chronic use in IBS
|
|
|
Alosetran
|
Potent, long acting 5-HT3 antagonist - approved for women with severe IBS with predominant diarrhea
10% of patients develop constipation and discontinue Black bock warning/restricted use: risk of serious, potentially fatal ischemic colitis; risk of serious constipation requiring hospitalization or surgery |
|
|
5-HT3 antagonists
|
Odansetron, granisetron, dolasetron, palosetron
Antiemetics Excellent saftey, no major drug interactions Oral or IV dosing except for palosetron (IV only) Can be used alone for mild nausea to moderate nausea and vomiting Combination with dexamethasone recommended to manage regiments with high risk of severe acute chemotherapy-induced nausea and vomiting Add NK1 as triple therapy to manage regiments with high risk of severe delated chemotherapy-induced nausea and vomiting |
|
|
Dexamethasone
|
Oral or IV corticosteroid can be used as anti-emetic
Effective alone and chances effects of 5-HT3 antagonists and other classes Routinely used in combo therapy to prevent/treat chemotherapy induced nausea and vomiting |
|
|
Neurokinin 1 receptor antagonists
|
Aprepitant - oral; fosaprepitant - IV
Antagonizes substance P (a neuropeptide) in CNS and periphery Mainly used in combination with other agents to manage delayed chemotherapy induced nausea vomiting Enhances effects of 5-HT3 antagonists and other class of agents Safe, may inhibit metabolism of drugs metabolized by CYP3A4 |
|
|
Phenothiazines
|
Prochlorperazine, chlorpromazine
Weak D2 blocking effects Not that useful for chemotherapy induced nausea and vomiting but may be okay fro mild nausea and vomiting Numerous CNS adverse effects; not first line |
|
|
Metoclopramide
|
Stronger D2 blocking effects useful for chemotherapy induced nausea and vomiting but many adverse effects
Not first line Black box warning: tardive dyskinesia |
|
|
Droperidol
|
Stronger D2 blocking effects useful for chemotherapy induced nausea and vomiting but many adverse effects
Not first line Black box warning: QT prolongation/sudden death |
|
|
Drobaninol
|
THC cannabinoid; 2nd line therapy when other agents are ineffective or poorly tolerated
Actual evidence poor Patient selective |
|
|
Cyclizine
|
H1 antagonist used for motion sickness
Ineffective for chemotherapy induced nausea and vomiting |
|
|
Scopolamine
|
muscarinic antagonist; patch used 24 hours in advance for motion sickness
Ineffective for chemotherapy induced nausea and vomiting |
|
|
Pancrelipase
|
Pancreatic extract containing lipase, amylase and proteolytic activity
Taken orally before meals to treat pancreatic enzyme insufficiency due to cystic fibrosis, pancreatitis, etc |
|
|
Ursodiol
|
Naturally occurring bile acid taken orally to dissolve small cholesterol gallstones, to prevent gallstone formation during rapid weight loss in obese patients, or to treat cholesterol gallstones when other therapies inadvisable
Very safe |
|
|
5-Aminosalicylic acid
|
Evokes topical anti-inflammatory effects on disease GI mucosa; mechanism unclear
Can induce and maintain remissions in mild-moderate ulcerative colitis; efficacy is lower in Crohn's disease Various formulation prevent absorption from upper GI tract, deliver drug to lower bowel Well tolerated except sufasalzine |
|
|
Basalazide, olsalazine, sulfasalazine
|
5-ASA analogs containing azo linkage (N=N) that is converted to 5-ASA by bacterial enzymes in colon
Sulfazalazine is obsolete |
|
|
Mesalamine (pentasa, asacol, lialda)
|
5-ASA delayed release tablets and capsules
|
|
|
Mesalamine (Rowasa, canasa)
|
5-ASA enema and suppository
|
|
|
Antimetabolites used in IBD
|
Azathioprine, 6-mercaptopurine, and methotrexate
Anti-cancer drugs that can interfere with nucleotide synthesis, inhibit cell proliferation, and exert immunosuppressive effects Lower doses in IBD than cancer Azathiprine and 6-mercaptopurine are important for inducing and maintaining remission of both UC and CD. Allows reduction in steroid dose in patents dependent on steroids for symptom control Metotrexate is useful in UC |
|
|
TNF-a antibodies used in IBD
|
infliximab, adalimumab, certrolizumab
Immunosuppressive agents used in patients with moderate to severe IBD that does not respond to other therapies |
|
|
Natalizumab
|
An antibody against the alpha4-subuint of integrins
Interferes with leukocyte adherence and migration through vascular endothelium to target cells in GI mucosa Approved for severe Chron's that is resistant to other therapies Black box warning: can induce fatal leukoencephalopathy by reactivating latent JC virus |
|
|
Chlorpheniramine
|
First generation H1 antagonist
Uses: sedation, motion sickness, antiparkinsonism effect, antiadrenoceptor action, anticholinoceptor actions, antiserotoninergic effect, inhibition of voltage-gated sodium channels |
|
|
Diphenhydramine
|
First generation H1 antagonist
Uses: sedation, motion sickness, antiparkinsonism effect, antiadrenoceptor action, anticholinoceptor actions, antiserotoninergic effect, inhibition of voltage-gated sodium channels |
|
|
Pyrilamine
|
First generation H1 antagonist
Uses: sedation, motion sickness, antiparkinsonism effect, antiadrenoceptor action, anticholinoceptor actions, antiserotoninergic effect, inhibition of voltage-gated sodium channels |
|
|
Cyclizine
|
First generation H1 antagonist
Uses: sedation, motion sickness, antiparkinsonism effect, antiadrenoceptor action, anticholinoceptor actions, antiserotoninergic effect, inhibition of voltage-gated sodium channels |
|
|
Promethazine
|
First generation H1 antagonist; especially heave antiadrenoreceptor action (orthostatic hypotension)
Prescription required Uses: sedation, motion sickness, antiparkinsonism effect, antiadrenoceptor action, anticholinoceptor actions, antiserotoninergic effect, inhibition of voltage-gated sodium channels |
|
|
Cyproheptadine
|
First generation H1 antagonist; heavy on antiserotoninergic effects
Uses: sedation, motion sickness, antiparkinsonism effect, antiadrenoceptor action, anticholinoceptor actions, antiserotoninergic effect, inhibition of voltage-gated sodium channels |
|
|
Fexofenadine
|
Second generation H1 antagonist
|
|
|
Loratadine
|
Second generation H1 antagonist
|
|
|
Cetirizine
|
Second generation H1 antagonist
Prescription required |
|
|
Acrivastine
|
Second generation H1 antagonist
|
|
|
Reserpine
|
Indole alkaloid that is an antipsychotic and antihypertensive; can cause depression due to depletion of serotonin
|
|
|
Buspirone
|
5HT1 agonist for anxiety
|
|
|
Sumtriptan
|
Triptan; acts on 5HT1d/1b receptors; used for migraines
Loss of effectiveness over time |
|
|
Almotriptan
|
Triptan; acts on 5HT1d/1b receptors; used for migraines
Loss of effectiveness over time |
|
|
Rizatriptan
|
Triptan; acts on 5HT1d/1b receptors; used for migraines
Loss of effectiveness over time |
|
|
Cisapride
|
Acts on 5HT4 receptors and is used to treat GERD
Toxic and only used in compassionate use |
|
|
Cyproheptadine
|
Inhibits 5HT2 receptors
Used to treat vomiting and post-surgery GI tract effects such as diarrhea; can help with sleep |
|
|
Ritaserine
|
5HT2 receptor antagonist used to reduce thromboxane formation; locks dopamine reuptake and enhances mood in schizophrenics
|
|
|
Ondansetron
|
Antagonist of 5HT3R in trigger zone and helps with nausea due to cancer chemotherapy
|
|
|
Ketaserin
|
inhibitor of 5HT2 receptors and alpha-1 adrenergic receptors to treat hypertension in europe (Not FDA approved)
|
|
|
n-acetyl-l-cysteine
|
Acetaminphen antidote; inactivates the toxic metabolite
|
|
|
ethanol and fomepizole
|
Antidote for toxic alcohol (methanol, ethylene glycol) overdose; blocks the formation of toxic metabolites
|
|
|
Oxygen (in hyperbaric chamber if available)
|
Antidote to CO poisoning
|
|
|
Hydroxocobalamin (or nitrite and thiosulfate)
|
Antidote for cyanide overdose; converts cyanide to nontoxic metabolite
|
|
|
Naloxone
|
Antidote for heroine (or opioid) overdose
|
|
|
Deferoxamine
|
Antidote for iron overdose; chelator
|
|
|
Dimercaptorol, succimer, EDTA
|
Antidote for inorganic lead overdose; chelators
|
|
|
Dimercaptrol, succimer
|
Antidote for elemental or inorganic mercury, arsenic (MTO) overdose
|
|
|
Atropine, pralidoxime
|
Antidote for anticholinesterase overdose
|
|
|
Bicarbonate
|
Antidote given for salicylates overdose to correct the metabolic acidosis; also used as antidote for membrane-depressant cardiotoxic drugs by increasing pH to reduce cardiotoxicity
|
|
|
17B-estradiol
|
Most important physiological estrogen; rapidly eliminated by liver, poor oral bioavailability
Transdermal patches yield systemic effects and avoid hepatic first-pass Topical creams/vaginal pessaries and Silastic rings (slow release of low doses) primarily are used for local effects but systemic effects can also occur Estradiol tablets composed of "micronized" particles yield stemic effects after p.o. doses, and may be used for post-menopasual therapy |
|
|
Estrone sulfate, equiline sulfate
|
Given p.o.
Absorbed in the lower GI tract in the form of estrone and equiline after enzymatic hydrolysis removes the charged sulfate group Predominant form of oral hormone replacement therapy in post-menopausal women Low potency estrogen |
|
|
Estradiol valerate, estradiol cypionate
|
Esterified estrogens; given by parenteral injections in oil
Much more slowly released from oil vehicle that 17B-estradiol; ester group hydrolyzed after drug enters circulation Provide prolonged systemic delivery of 17B-estradiol to circulation (2 to 4 weeks) in a manner the reduces hepatic effects of estrogens Used in the treatment of hypogonadism, to produce pubertal changes in adolescents needing exogenous hormone |
|
|
Ethinyl estradiol
|
Synthetic steroidal estrogen with a 17-ethyinyl substitution which decreases hepatic first-pass metabolism.
Long-elimination half-life (13-27 hours); partly due to enterohepatic cycling Potent estrogen used in combination oral contraceptives |
|
|
Mestranol
|
Prodrug which gets converted to ethinyl estradiol
|
|
|
Diethylstilbesterol (DES)
|
Synthetic non-steroidal estrogen. Given p.o.
Potent estrogen with prolonged effects Mainly used in large "pharmaceutical doses" (non-physiological) for palliative treatment of advanced prostate or breast cancer after other therapies have failed No longer used due to tetratogenic effects |
|
|
Tamoxifen
|
Selective estrogen receptor modulator/antiestrogen
Potent estrong antagonist on the breast; 1st line agent useful for treatment of ER-positive breast cancer. Also used for the prevention of breast cancer in high risk patients Acts as an estrogen agonist on bone - may be useful for the treatment or prevention of osteoporosis, but not approved or used for this Acts as partial estrogen agonist on uterus; chronic use increases uterine cancer risk |
|
|
Raloxifene
|
Selective estrogen receptor modulator/antiestrogen
Acts as an estrogen antagonist on breast and estrogen agonist on bone Only approved for treatment and prevention of post-menopausal osteoporosis Weaker estrogen antagonist effects on breast than tamoxifen Minimal estrogen agonist effects on uterus - may post less risk of uterine cancer |
|
|
medroxyprogesterone acetate
|
21-carbon analog similar to progesterone; agent in DepoProvera (3 month contraceptive injection); often given p.o. in hormone replacement regimens for post-menopausal women
|
|
|
Megestrol acetate
|
21-carbon analog similar to progesterone; palliative drug used to stimulate appetite and weight gain in patients with AIDs
|
|
|
norethindrone, levonorgestrel
|
19-nortestosterone derivatives; 17-ethinyl group, good p.o. bioavailability; produce decimal change in endometrium but do not support pregnancy in animal models. Stronger inhibitors of LH and FSH release. Used in combination oral contraceptive pills, progestin alone "mini-pills", contraceptive patches, and emergency post-coital contraceptives
Have weak androgen and antiestrogen effects |
|
|
Norethynodrel
|
19-nortestosterone derivatives; 17-ethinyl group, good p.o. bioavailability; produce decimal change in endometrium but do not support pregnancy in animal models. Stronger inhibitors of LH and FSH release. Used in combination oral contraceptive pills, progestin alone "mini-pills", contraceptive patches, and emergency post-coital contraceptives
Has some estrogenic effects |
|
|
Desogestrel, norgestimate
|
19-nortestosterone derivatives; 17-ethinyl group, good p.o. bioavailability; produce decimal change in endometrium but do not support pregnancy in animal models. Stronger inhibitors of LH and FSH release. Used in combination oral contraceptive pills, progestin alone "mini-pills", contraceptive patches, and emergency post-coital contraceptives
Minimal androgenic or estrogenic effects |
|
|
Dienogest
|
19-nortestosterone derivatives; 17-ethinyl group, good p.o. bioavailability; produce decimal change in endometrium but do not support pregnancy in animal models. Stronger inhibitors of LH and FSH release. Used in combination oral contraceptive pills, progestin alone "mini-pills", contraceptive patches, and emergency post-coital contraceptives
Antiandrogenic |
|
|
Drospirenone
|
Spironolactone-related progestin; has anti-mineralcorticoid similar to progesterone; no androgenic activity
May cause less water retention (bloating) and breast tenderness than 19-nortestosterone related progestins |
|
|
Ulipristal acetate
|
A selective progesterone receptor modulator with agonist and antagonist effects. Used for emergency contraception
|
|
|
Testosterone
|
Poor systemic bioavailability after oral dosing or s.c. or i.m. injections in oil due to rapid hepatic metabolism.
T gels and skin patches available for slow transdermal delivery, but absorption can be erratic |
|
|
Testoserone ethanate, testosterone cypionate
|
Parenteral esterified testosterone; preferred for inducing pubertal changes in hypogonadal boys
Converted to T after release from oil vehicle; no hepatotoxicity Injected IM every 2-4 weeks |
|
|
Methyl testosterone, Fluoxymesterone, Oxandrolone
|
Orally active androgens; anabolic steroids
Dose-related hepatotoxicity |
|
|
Danazol
|
Synthetic steroid derivative with 17-ethinyl group (p.o. use) and mix of weak androgen, anti estrogen, progestin and glucocorticoid activity
Widely used to treat endometriosis (mainly in pre-menopausal women). Inhibits ovarian function by decreasing LH and FSH and by direct action on endometrium Used to prevent episodes of hereditary angioneurotic edema in patients with complement C1 inhibitor deficiency. Mechanism unrelated to androgenic activity. |
|
|
Levonorgestrel, levonorgestrel + EE
|
Plan B, Preven; post-coital contraception
80% effective when begun within 72 hours of intercourse Available without prescription |
|
|
Ulpristal acetate
|
Ella; a selective progesterone receptor modulator used for post-coital contraception
Prescription medication; 5-day course of treatment 60% effective when started within 120 hours of intercourse Prevents ovulation and impairs implantation Headache, nausea, dysmennorhea |
|
|
Flutamide
|
Potent non-steroidal antagonist of AR
Mainly used for prostate cancer therapy in combination with GnRH super-agonist Prevents "tumor flare" due to brief rise in testosterone that occurs prior to the desensitization and down regulation of the GnRH receptor |
|
|
Bicalutamide
|
More potent non-steroidal antagonist of AR; longer acting, less hepatotoxic than flutamide
Mainly used for prostate cancer therapy in combination with GnRH super-agonist Prevents "tumor flare" due to brief rise in testosterone that occurs prior to the desensitization and down regulation of the GnRH receptor |
|
|
Spironolactone
|
Weaker AR antagonist that also reduces testis levels of steroid 17alpha-hydroxylase (involved in androgen synthesis)
Often used for hirsutism in women |
|
|
Cyproterone, cimetidine
|
Weak AR antagonists used for hirsutism
|
|
|
Ketoconazole
|
Systemic anti fungal that can inhibit multiple steroidigenic enzymes to decrease androgen as well as corticosteroid synthesis. Sometimes used for cancer therapy
|
|
|
Finasteride
|
5alpha-reductase inhibitor (prevents DHT synthesis). Moderately useful for treatment of benign prostatic hypertrophy; useful in some cases of male-pattern baldness
2% incidence of sexual dysfunction |
|
|
Abiraterone
|
Specific inhibitor of 17alpha-hydroxylase and 17,20-desmolase (CYP17A1) that are involved in the synthesis of glucocorticoids and androgens.
Indicated for the treatment of prostate cancer that has progressed after acstration and docetaxal therapy Given in combination with prednisone |
|
|
Clomiphene
|
Selective estrogen receptor modulator
Pharmacology similar to tamoxifen but exclusively used for the treatment of infertility Estrogen receptor block leads to loss of estrogen feedback inhibition on hypothalamic pituitary axis and causes increases in LH and FSH release Helpful in treatment of infertility in women with adequate pituitary reserves of gonadotropins but impaired release of LH and FSH |
|
|
Anastrzole, letrozole, exemestane
|
Anastrzole, letrozole are non-steroidal; exemestane is steroidal
Inhibitors of aromatase (CYP19) which is involved in converting androgens to estrogens No estrogen agonist effects. Used for breast cancer resistant to tamoxifen; may be used first line; as effective as tamoxifen Increased risk of osteoporosis |
|
|
Fluvestrant
|
Steroidal anti-estrogen (pure estrogen receptor antagonist)
No partial agonist effects. Can decrease estrogen receptor levels in some tissues by impairing receptor dimerization and retention in the nucleus; this may promote receptor degradation Given parenterally for advanced breast cancer resistant to other therapies. Would be expected to increase risk of osteoporosis |
|
|
Mifepristone (RU486)
|
A progesterone receptor antagonist used to induce first trimester abortions
Also has significant effects to block glucocorticoid receptors (used off label for Cushing's) Approved for use in US only during first 7 weeks of conception Adverse effects include nausea, vomiting, diarrhea and vaginal bleeding Misprostol given 2 days later to expel fetus (or dinoprostone) |
|
|
Disulfram therapy
|
For alcoholics - adversive conditioning - evokes acute physical distress due to acetaldehyde poisoning in patients taking drug who drink alcohol
Inhibits acetalaldehyde dehydrogenase |
|
|
Naltrexone therapy
|
For opioid addicts or alcoholics; opioid receptor antagonist reduces rewarding effects of drug use
Requires 7 day prior opiate abstinence Contraindicated in acute hepatitis, liver failure, breastfeeding, opiate use Pregnancy category C Orally active opioid antagonist that reduces reinforcing effete of ethanol by blocking effects of endogenous opioid peptides released in response to ethanol actions. Small effect to reduce relapse. |
|
|
Acamprostate therapy
|
For alcoholics; mild NMDA receptor antagonism reduces reinforcing effects of drug abuse
It inhibits calcium influx linked to NMDA receptor activation |
|
|
Methadone maintenance
|
Reduces craving for heroin and induces tolerance that impairs rewarding effect of heroin. Reslts in less criminal activity and incarceration, improves health, employment, education and family/social outcomes.
Do not need to detox before starting Must be picked up at clinic daily Contraindicated in asthma, respiratory despression, paralytic ileus Pregnancy category C |
|
|
Rimonobant
|
CB1 antagonist developed to treat obesity (Reduce appetite). Withdrawn from market due to concern about psychiatric effects (depression)
|
|
|
Fomepizole
|
cytosolic alcohol dehydrogenase inhibitor; used in methanol or ethylene glycol poisoning
Blocks formation of toxic metabolites (methanol converstion to formaldeyde and formic acid; ethylene glycol conversion to glycolic and oxalic acids) |
