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157 Cards in this Set
- Front
- Back
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Produced in seawater by the action of bacteria and algae, synthesized for use as a fungicide
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Methyl mercury
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Used in the treatment of Wilson's disease and in copper, arsenic, and lead poisoning
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Penicillamine
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Causes severe diarrhea, abdominal pain, and bone marrow depression
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Arsenic
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An oily chelator with high lipid solubility that readily enters cells
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dimercaptoproponol
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A 46 year old man suffering from insomnia memory loss, irritability, depression, shyness, and tremor visits his PCP. Additional findings include symptoms of gingivitis, stomatitis, and excess salivation. Chronic eposure of which of the following is most likely responsible for these findings?
a. arsenic b. cadmium c. lead d mercury e. thallium |
d. mercury
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Chelating agents and route of administration for lead poisoning:
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CaNa2-EDTA - IV
2,3-dimercaptosuccinate - oral 2,3-dimercaptoproponol (dimercaprol) - IM Penicillamine - oral |
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Chelating agents and route of administration for cadmium poisoning
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CaNa2-EDTA - IV
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Chelating agents and route of administration for mercury poisoning
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2,3-dimercaptosuccinic acid - oral
2,3-dimercaptoproponol - IM Penicillamine - oral N-acety-penicillamine - oral |
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Chelating agents and route of administration for arsenic poisoning
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N-acetyl penicillamine - oral
penicillamine - oral |
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Treatment for arsine gas (AsH3) poisoning
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support and transfusion
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Chelating agents and route of administration for iron poisoning
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deferoxamine - IM, slow IV, rarely oral
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Blood test for lead poisoning shows:
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increased delta-aminolevulonic acid and protoporphyrin IX.
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Toxicity of cadmium
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Inhibits alpha1antitrypsin
extremely nephrotoxic, limits the number of drugs used for tx. Only use CaNa2-EDTA. |
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Mercury toxicity:
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Precipitates proteins, necrosis, inhibits -SH group containing proteins.
Remember Minimata disease |
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Arsenic toxicity
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Increases vascular permeability, inhibits anaerobic and oxidative phosphorylation - no ATP
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Treatment of Wilson's disease
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penicillamine, N-acetyl-penicillamine
or Trientine - less toxic, fewer allergies, teratogenic long term |
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Organophosphates
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parathion, malathion
CNS toxicity acts on ACh-esterase |
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Treatment of organophosphate poisoning
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atropine
pralidoxime |
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Carbamates
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Carbaryl, baygon
pesticide that is anti AChE |
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DDT poisoning
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acute: ataxia, abnormal gait
Chronic: mild anemia |
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Lindane is
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a chlorinated hydrocarbon pesticide.
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toxicity of clorophenoxyherbicides
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Interferes with lipid metabolism, induces myotonia
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Paraquat
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herbicide
targets lung, causes free radical peroxidation |
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pyrethrum
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household insecticide
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rotenone
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household insececticide, pesticide
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glucocorticoids produced in
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zona fasciculata of the adrenal cortex
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Mechanism of action of corticosteroids
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enters cell by diffusion
binds to cytosolic receptors translocates into the nucleus regulates synthesis of proteins |
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Physiological effects of glucocorticoids
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Increase blood glucose
Decreases absorption of Ca, increases excretion of Ca Redistributes fat to trunk and face. Favors protein breakdown Anti-inflammatory, immunosuppresant End result - decreased prostaglandin, thromboxane, and leukotriene production |
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Prednisone, prednisolone
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synthetic glucocorticoids
4x as potent as cortisol at antiinflammation, 8 at sodium retention. Much lower dose, longer half life (18-36 hours) |
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corticosteroid
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refers to both glucocorticoids and mineralcorticoids
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triamcinolone
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synthetic glucocorticoid
5x as effective as cortisol at antiinflammation, no sodium retaining potency. smaller dose, longer half life, duration of action 12-36 hours |
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dexamethasone, betamethasone
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synthetic glucocorticoids
25x as potent as cortisol for anti-inflammatory Long duration of action - 36-54 hours |
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Negative effects of glucocorticoids
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osteoporosis
skin thinning connective tissue breakdown Increased neutrophils, thrombocytes, RBCs Decreased lymphocytes, eosinophils, basophils psychoses, mood instability water retention |
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Glucocorticoids mechanism of anti-inflammatory effect
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Suppress t cell activation and cytokine production
suppress mast cell degranulation decrease capillary permeability Reduce expression of COX2 |
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Diseases in which glucocorticoids are useful
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arthritis
allergic rxns asthma autoimmune Collagen disease Nephrotic syndrome Prevention of graft rejection |
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fludrocortisone
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a mineralocorticoid
useful in addison's disease Treats adrenal insufficiency, cerebral salt wasting, replaces aldosterone, |
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clomiphene
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anti estrogen, induces ovulation in women with intact HPOvarian axis. Blocks normal feeback inh on GnRH, FSH, LH. Induces LH surge
Also increases spermatogenesis in men. bind to estrogen receptor and prevents estrogen from binding |
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tamoxiphen
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estrogen receptor modulator, can be anti, estrogenic, or mixed. Inhibits breast cancer cells, but stimulates endometrial cells
binds to estrogen receptor and prevents estrogen from binding |
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hCG
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activity similar to LH
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mifepriston
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progesterone receptor antgonist
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2 possible estrogenic components of OC pills
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ethinyl estradiol
Mestranol |
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Progesterone only pills
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inhibit about 50% of ovulation
thicken cervical mucus decreases expression of E receptors. Facilitates metabolism of E My act as a partial agonist at the ER |
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Polycyclic aromatic hydrocarbons
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come from burning of carbon based material, found in smoke, grilled foods, exhaust.
Increases risk of lung, skin, and urinary cancers |
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benzopyrene
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Mutagen
Intercalates into DNA found in burnt foods, coffee, smoke |
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nitrosamines
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carcinogen found in meat, fish, beer, pickled foods, tobacco smoke
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ipecac
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irritates gastric mucosa and stimulates emetic center in the medulla to stimulate emesis
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acetylaminofluorine
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compound that is metabolized to be more carcinogenic
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halogenated compounds e.g. vinyl chloride
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Used in plastics industry.
Associated with lung cancer and angiosarcomas of the liver and brain. |
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mycotoxins e.g. aflatoxin B1
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produced by funci that grow on certain grains and peanuts. People can be exposed by eating meat or dairy from animals who ate contaminated feed.
Increases risk for liver cancer |
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apomorphine
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dopamine agonist
emetic agent more potent and rapidly acting than ipecac |
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anti-emetic drugs that don't work against CT/radiatio nausea
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Antihistamines - H1 blockers
Dramamine (diphenhydramine) Meclazine - these act on vestibular afferents and brain stem |
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anti-emetic drug not effective against CT nausea
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Scopalamine - dermal patch, slow release
this is an anticholinergic drug |
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Drug types that work as anti emetics
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antihistamines (not against CT)
anticholinergic (not against CT) D2 dopamine antagonists 5HT3 antagonists Cannabinoids |
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Metoclopramide
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Primary effect 5HT4 agonist - helps gastroparesis
D2 dopamine antagonist - antiemetic against CT nausea |
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Promethazine
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D2 dopamine antagonist
antiemetic against CT nausea |
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Ondansetron
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5HT3 serotonin antagonist
works against CT nausea |
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Dronabinol
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a cannabinoid
works against CT nausea anti emetic |
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Tegaserod
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5HT4 agonist
treats gastroparesis |
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Bethanachol, neostigmine
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Cholinergic drugs
work for gastroparesis but not widely used because of lack of specificity |
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Domperidone
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D2 antagonism - not available in US
Treats gastroparesis |
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erythromycin
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antibiotic that has effects against diabetic gastroparesis
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Metamucil
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acts on diarrhea intraluminally - bulks up stool
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Bismuth salycilate
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pepto!
increases stool viscosity and absorbs water, some antibacterial properties |
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Loperamide
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imodium
an opioid antidiarrheal, little CNS penetration |
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Diphenoxylate
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lomotil - greater CNS effects, Rx only.
opioid antidiarrheal |
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defenoxin
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motofen
greater CNS effects than loperamide, Rx only opioid antidiarrheal |
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octreotide
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antisecretory effects, decreases colonic tone
antidiarrheal in severe AIDS or CT induced cases |
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Cholestyramine
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binds bile salts
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Osmotic laxatives
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magnesium salts, phosphates, glycerine, lactulose, polyethylene glycol
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Bisacodyl
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stimulant laxative
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castor oil
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stimulant laxative - can induce violent catharsis
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Stool softeners
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mineral oil, colace, docusate
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H2 histamine antagonists
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Block stimulation of parietal cells by histamine.
Cimetidine - inhibits CYP3A4 Ranitidine Famotidine Nizatidine |
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Proton pump inhibitors
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Bind covalently to proton pump. More potent than H2 antagonists
Omeprazole Lansoprazole Rabeprazole Pantoprazole |
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Misoprostol
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prostaglandin that inhibits acid secretion and promotes mucus and bicarbonate secretion
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Sucralafate
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sulfated polysacharide that forms a protective layer and buffers acidity in the stomach.
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Sulfasalazine
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NSAID used against Inflammatory bowel disease
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Mesalamine
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NSAID used against inflammatory bowel disease
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Hydrocortisone, prednisone
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corticosteroids used against IBD
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Azathiaprine
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immunosuppressant
used in IBD |
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6-mercaptopurine
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Immunosuppresant
used against IBD |
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Methotrexate
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immunosupressant
used against IBD |
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Cyclosporine
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immunosupressant
used against ibd |
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Inflixomab
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TNF alpha antibody used for treatment of IBD
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5HT in the gut
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mediates vasoconstriction and hemostasis, GI motility
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Insulin lispro
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rapid acting, injected just prior to meals
Humalog |
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Insulin aspart
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Novolog
rapid acting insulin |
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Insulin glulisine
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Apidra, aventis
rapid acting insulin |
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Short acting insulin
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identical to endogenous insulin
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NPH insulin
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NPH delays insulin absorption by making it unavailable
Intermediate acting 4-12 hr duration |
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Insulin glargine
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Lantus
Long acting Provides background insulin replacement, steady state Can't be mixed with others, pH 4.0 |
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Insulin detemir
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Levemir
binds to albumin 1-2 hr onset, 24 hr duration long acting |
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Ultralente
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long acting
Crystalline suspension, must redissolve at site of injection |
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hypoglycemic drugs
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primarily increase insulin secretion
Includes: sulfonureas and meglitinides |
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Antihyperglycemic drugs
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prevent or reduce hyperglycemia
do not induce hypoglycemia Includes: a-glucosidase inhibitors, thiazolidinediones, and biguanides |
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sulfonylureas
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1. stimulates insulin secretion, binds a co-receptor of beta cell K channel.
2. decreases serum glucagon |
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Tolazamide
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a sulfonurea - oral hypoglycemic agent
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glyburide
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sulfonylurea
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glipizide
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sulfonylurea
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acarbose
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prevents larger carbohydrates from being broken down into glucose in the gut by inhibiting alpha glucosidase
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Meglitinides
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similar mechanism to sulfonylurea
rapaglinide nateglinide |
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Repaglinide, nateglinide
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a meglitinide - hypogycemic agent
no sulfur, so can be used with allergies to sulfur drugs |
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Biguanides - Metformin
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No functional beta cells necessary
Increases glycolysis and glucose removal from cells decreases gluconeogenesis decreses glucose absorption decreases plasma glucagon |
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Rosiglitazone
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Lowers triclyceride levels
a thiazolidinedione antihyperglycemic, reduces insulin resistance. PPAR-gamma agonist decreases bioavailability of other drugs like OCs |
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Pioglitazone
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a thiazolidinedione
antihyperglycemic, reduces insulin resistance. PPAR-gamma agonist decreases bioavailability of other drugs like OCs |
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Exantide
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glucagon-like peptide
increases insulin secretion may also increase Beta cell mass |
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Propylthiouracil
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Treatment for hyperthyroid:
Inhibits thyroperoxidase which changes iodide to iodine. It also inhibits t4 conversion to t3. |
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Methimazole
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Inhibits thyroperoxidase in the thyroid, preventing iodide to iodine conversion. No peripheral effect like propylthiouracil
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Thyroid storm
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acute exacerbation of hyperthyroidism, emergency
throw the kitchen sink at these people 1. PTU - propylthiouracil 2. Iodide loading 3. Beta blockers 4. Corticosteroids |
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synthetic t4
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half life 5-7 days
treats |
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synthetic t3
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half life 1-2 days, not as good as synthetic t4
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levothyroxine
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synthetic t4
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Liothyronine
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synthetic t3
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liotrix
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4:1 mixture of t4:t3
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Prostacyclin
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produced by vascular endotheial cells
potent inhibitor of platelet function and vasodilator |
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alprostadil (PGE1)
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used to dilate ductus arteriosus in infants with congenital heart defects until surgery
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aspirin
acetylsalicylic acid |
Prototype NSAID
Inhibits COX1&2 Irreversible inhibitor of COX enzymes Antipyretic/analgesic dose smaller than anti-inflammatory dose |
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diflunisal
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derivative of salicylic acid
more potent anti-inflammatory and analgesic than aspirin, but no antipyretic effect. fewer GI and platelet side effects |
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ibuprofen
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lower incidence of side effects vs aspirin
Half life 2 hrs duration of action 4-8 hrs |
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naproxen
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More irritating to GI tract than ibuprofen
related drugs 20x more potent than aspirin |
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acetaminophin
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Not technically an NSAID
COX3 inhibitor?? analgesic and antipyretic, not anti-inflammatory liver toxicity |
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diclofenac
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acetic acid derivative
Inhibits COX and decreases substrate availability for COX Weakly COX-2 selective |
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ketorolac
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Highly selective for COX-1
Acetic acid derivative. Inhibits COX and decreases availability of AA. |
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celecoxib
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celebrex
COX 2 selective inhibitor Decreases inflammation without GI side effects Used for arthritis, menstrual cramps, post surgery Half life is 11 hrs |
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rofecoxib
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vioxx
COX2 selective inhibitor withdrawn from the market because of increased risk of stroke and mi |
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Histamine is formed from
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histidine by histidine decarboxylase
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Histamine found in:
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basophil and mast cell granules
also in histaminocytes in the stomach and in neurons |
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Histamine release stimulated by
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C3a, C5a, antigen-cell fixed IgE
morphine, tubocurarine |
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Histamine release inhibited by
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beta adrenergic receptor antagonists
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Allopurinol
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inhibits uric acid synthesis by inhibiting xanthine oxidase
Usually administered with NSAIDs treats gout |
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Uricosuric agents
-probenecid -sulfinpyrazone |
increases uric acid excretion by affecting the renal tubule.
good prophylactically |
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colchicine
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gout treatment
disrupts microtubules to prevent neutrophil migration to the joint. |
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to treat acute gout attack:
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NSAID, colchicine
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for gout prophylaxis
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allopurinol inhibits uric acid synthesis
probenecid increases its excretion Don't start these drugs until acute attack has resolved! |
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methotrexate
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folic acid analog
immunosuppressive first choice of DMARD |
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hydroxychloroquine
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used mainly in prevention and treatment of malaria
also causes remission of rheumatoid arthritis |
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sulfasalazine
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DMARD used in RA and IBD
Scavenges toxic O2 metabolites produced by neutrophils Combination of sulfonamide and salicylate |
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gold
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DMARD
mechanism unknown max effect in 3-4 months Concentrates in joints, liver, kidney tubules, adrenal cortex Inhibits PG synthesis and suppresses cellular immune response. Side effects: rashes, mouth ulcers, flu like, proteinuria, thrombocytopenia |
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Penicillamine as a DMARD
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decreases immune response, IL-1 generation
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ciclosporin
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immunosuppressant drug
Inhibits calcineurin phosphatase, preventing Th cell activation Not cytotoxic. Half life 24 hours |
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tacrolimus
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immunosuppressant drug
prevents Th cell activation. worse side effects than cyclosporin |
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azothioprine
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immunosuppressant drug
Inhibits purine synthesis - cytotoxic. decreases clonal expansion during induction phase of immune response |
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Etanercept
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Anticytokine drug
TNFalpha receptor fused with Fc portion of IgG. Binds TNFalpha . Increased risk of fatal fungal infection |
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Anikinra
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anticytokine drug
IL-1 antagonist |
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Immediate hypersensitivity rxn:
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mast cell histamine, cytokines, prostaglandins, leukotrienes, heparin and proteases
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diphenhydramine
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first generation antihistamine (H1 blocker)
crosses CNS also antiemetic and sedative |
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Chlorpheniramine
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first generation H1 antagonist
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Promethazine
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first generation H1 antagonist
also D2 antagonist active vs CT radiation nausea antiemetic, anti allergic |
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meclozine
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anti emetic
anti histamine H1 antagonist |
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Loratidine
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OTC 2nd generation H1 antagonist
doesn't cross CNS |
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Cromolyn sodium
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Inhaled asthma treatment
mast cell stabilizer suppresses release of chemoattractants no bronchodilator or antihistamine activity |
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Asthma defined:
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the presence of intermittent syptoms such as chest tightness, wheeze, and cough, together with demonstrable BHR
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effects of beta 2 agonists in asthma
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1. relax bronchial SM
2. prevent bronchial SM contraction 3 increase mucous clerance 4. prevent mast cell mediator release 5. prevent edema induced by histamine |
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metaproterenol
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beta agonist, inhaled
asthma |
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albuterol, terbutline, salmeterol
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inhaled or oral beta 2 agonists for asthma
albuterol - inhaled terbutaline - oral Salmeterol - inhaled, only prophylaxis because of long half life |
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beclomethasone
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nasal spray inhaler corticosteroid for asthma
reduces number and activity of inflammatory cells in the airway, inhibits release of AA metabolites, increases beta adrenergic responsiveness. |
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theophylline
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caffeine analog for asthma
relaxes smooth muscle decreases mast cell mediator release, increases mucocilliary clearance Inhibits PDE - increasing cAMP Adenosine receptor antagonism - bronchodilation Increased epinephrine from medulla Slow release oral tablets |
