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190 Cards in this Set
- Front
- Back
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cancer theraputic drugs targer which type of cells
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rapidly repilcating cells
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what are the normal side effects seen with cancer theraputic drugs
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hair loss, GI problems (nausea and vomiting, suscpetability to infection, anrmia, bone marrow suppression, and liver or kidney damage
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what are alkylating agents
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drugs that transfer alkyl groups or cross link DNA to stop it from being copied or read to make RNA and proteins
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are alkylating drugs cell cycle specific or non- specific?
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alkylating agents are cell cycle non-specific
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what are the 3 types of alkylating agents?
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nitrogen mustards, cisplatin, mitomycin
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what are the uses of alkylating agents?
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hodgkins disease, lymphoma, leukemia, ovarian, breast, testicular cancers, head, neck, and lung cancers, neuroblastomas and brain tumors
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cyclophosphamide
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alkylating agent
nitrogen mustard must be activated in liver inhibits DNA systhesis by alkylation |
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mechlorethamide
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alkylating agent
nitrogen mustard shortest duration of action inhibits dna synthesis |
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chlorambucil
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alkylating agent
nitrugen mustard least toxic inhibits dna synthesis |
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carmustine
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alkylating agent
nitrogen mustard alkylates DNA, RNA lipid soluble so it crosses the BBB and exerts effects on brain (ie used to fight brain tumors) |
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cisplatin
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alkylating agent
does not techincally alkylate dna but it cross links dna to give same effect to prevent dna replication and cell replication major side effect is renal toxicity which can be prevented by hydration |
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mitomycin
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alkylating agent
antibiotic used as chemotherapy because it alkylated dna and causes dna breakage to inhibit dna synthesis |
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side effects of alkylating agents
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nausea, hair loss, bone marrow suppression, renal toxicity
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antimetabolites
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subsitute nucloetides into dna to make it non-functional
most active in S phase and are cell cycle specific drugs |
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side effects of anitmetabolites
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hair loss, bone marrow suppression, liver dysfunction, GI pain and upset
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6-mercaptopurine and Thioguanine
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antimetabolites
purine analogs aka purine antagonists sub for guanine in dna to produce abnormal dna |
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5-fluorouracil
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antimetabilote
pyrimidine analog (pyramidine antagonists) sub for uracil which is precourser to thymidine produce abnormal dna |
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cytosine arabinose
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antimetabolite
pyrimidine analog sub for cytosine and produce abnormal dna |
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methotrexate
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antimetabolite
folic acid analog inhibits dihydrofolate reductase to inhibit production of thymidine reduces production of DNA |
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uses of anitmetabolite
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breast, colorectal cancer, osteosarcoma
leukemias, and non-hodgkins lymphoma |
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mitotic inhibitors
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stop mitosis by causing tubulin dysfunction
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vinblastine, vincristine, paclitaxel
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mitotic inhibitors
bind and prevent normal polymerization and depolymerization of tubulin so tubulin cannot move large molecules and organelles in the cell |
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what does tubulin dysfunction in a cell cause
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loss of movement of large molecules and organelles
also chromosome separation is disrupted neurons are particulatly affected because they must move large molecules down the axon |
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vinblastine, vincristine, paclitaxel
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mitotic inhibitors
inhibit tubulin inhibit mitosis uses- hematologic cancers (leukemias)and breast cancers and other solid tumors side effects- bone marrow suppression, hair loss, and neuronal based problems |
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steroid hormone receptors
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estrogens, androgens, glucocorticoids,
affect rate of cell replication these drugs may slow rate of replication but do not casue tumor regression |
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diethylstillbestrol and ethinyl estradiol
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estrogen receptor agonists
estrogens uses- prostatic carcinoma and advanced mammary cancer in post menopausal women side effects- hyper calcemia, uterine bleeding, thrombosis |
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testosterone propionate and fluxymesterone
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androgen receptor agonists
andregens uses- carcinomas of the breast side effects-virilization, edema, hypercalcemia |
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prednisone
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corticosteroid receptor agonist
glucocorticoids uses- leukemias in children side effects- GI ulcers, osteoporosis, mental confusion |
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medroxyprogesterone, hydroprogesterone, megestrol
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progesten receptor agonists
progestins uses- renal carcinoma and endometrial carcinoma |
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tamoxifen
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anti-estrogens
uses- breast cancer side effects- not a steroid (less toxic) |
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flutamide
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anti-androgen
uses- metastatic prostate cancer |
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erlotinib and imatinib
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tyrosine kinase inhibitors
inhibit tyrosine kinase which an important 2nd messenger in signal transduction pathways uses and s/x under study |
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rituximab
trastuzumab bevacizumab |
monocolinal antibodies
target anitgens for cancer types tend to be very specific and restricted still being studied to see if normal cells express cancer antigens |
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rituximab
trastuzumab bevacizumab |
non-hodgkins lymphoma
metastatic breast cancer colon cancer |
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antibiotic
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extract of an organism
effective in low concentrations against infections of other microorganisms |
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anitbacterial
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synthetic agent effective at low concentration against infectious bacteria
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bacteriostatic
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ability of drug to inhibit multiplication of microorganism
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bactericidal
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ability of drug to kill microorganism
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spectrum of action
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range of microorganisms that are sensitive to the actions of the drug
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nosocomial infection
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infection arising from exposure to bacteria in hospital or other clean facility
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drug resistance
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state of insensitivity of decreased sensitivity to drugs
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direct toxic effects
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result from too high blood levels
no prior exposure needed organs most involved- renal, hepatic, nervous, and digestive |
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allergy
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may require prior exposure
does not require full dose may be immediate or delayed |
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immediate allergy
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smooth muscle spasm, vascular damage
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delayed allergy
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edema, fever, dermatitis
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superinfectious
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overgrowth of resistant organisms resulting from elimination of normal flora
common after use of broad term anitbiotics most common in GI, UB, and respiratory may arise in tissues that were not site of original infection |
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folic acid
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precourser for thymidine which is used to make DNA
must be obtained through diet |
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cocci
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spherical shaped
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bacilli
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rod shaped
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spirochetes
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spiral shaped
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4 characteristics (sites of attack) of antibacterials
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1) presence of enzymes needed to metabolize folic acid
2)bacterial cell wall 3)bacterial ribosomes 4)bacterial dna repair enzymes |
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two types of bacteria based on structure of cell wall
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gram positive and gram negative
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Penicillin G
Cephalosporins (1st and 2nd generations) VAncomycin Clindamycin Linezolid Vancomycin |
narrow spectrum antibacterial
attack gram positive bacteria |
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aminoglycosides
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narrow spectrum antibacterial
gram negative aerobes |
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methicillin
erythromycin cephalosporins (3rd and 4th generations) tetracyclines trimethoprim sulfonamides quinolones |
broad spectrum antibacterials
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sulfonamides and trimethoprim
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completely block bacterial intermediary metabolism
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penicillin, cephalosporins, vancomyocin
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cell wall disruption
inhibit cell wall synthesis |
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tetracyclines, erythromycin, clindamycin
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bacteriostatic inhibition of protein systhesis
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aminoglycosides
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bactericidal inhibition of protein synthesis
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quinolones
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inhibit dna/rna synthesis
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sulfonamide mechanism of action and spectrum
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are structural analogs of PABA
reduce bacterial PABA metabolism, folic acid production, and purine synthesis and DNA synthesis broad spectrum and gram positive tend to be more sensitive |
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uses and restrictions of sulfonamides
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restrictions-
toxicity, crystaluria, urinary and renal tract injury, nausea, vomiting, anemia, allergic rxn, resistance uses- UTI, meningococcal infections, chlamydial infections |
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sulfonamide subgroups
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sulfisoxazole
sulfmethoxazole sulfacetamide mafenide |
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sulfisoxazole
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sulfonamide subgroup
rapidly absorbed across the GI tract, rapidly excreted used against systemic infections, respiratory infections, CNS, urinary tract short acting |
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sulfamethoxazole
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sulfonamide subgroup
slowly absorbed across GI long acting Used for GI tract infections |
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sulfacetamide
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sulfonamide subgroup
topically applied, not systematically used for opthalamic infections |
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mafenide
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sulfonamide subgroup
topically applied prevention of infection on burned skin |
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trimethoprim
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suppresses folate reductase
broad spectrum tendancy for gram+ due to diff wall structure used to treat UTI used with sulfonamides |
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penicillins
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includes penicillin g and penicillin derived drugs
destroy cell wall by binging PBPs with failure of crosslinking of peptidoglycan strands and disfunction of cell wall and eventual rupture narrow spectrum (gram + such as streptococci and staphylococci) |
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why are gram- bacteria usually resistant to penicillin?
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because they have more penicillinase in their cell wall
yet penicillin is useful against the bacteria that cause gonorrhea and syphillis (neisseria gonorrhea, and treonema pallidum) |
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absorption of pencillin
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not well absorbed in GI (80% broken down in GI but still can be administered orally)
can also be IV or IM Penicillin G does not easially enter the CNS, eye, or joints, or cross placents BUT INFLAMMATION OF THESE AREAS WILL INCREASE PERMEABILITY |
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rxn to penicillin
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intrinsic toxicity is low
significant incidence of hypersensitivity rxns anaphylactic shock GI upset |
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restrictions of penicillin
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resistant organisms can destroy drug with penicillinase
cell wall- gram- bacteria can be resistant |
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uses of penicillin
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pneumonia, meningitis, endocarditis, gas gangrene, tetanus, anthrax
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penicillin derivatives
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methicillin
oxacillin ampicillin amoxicillin |
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penicillinase inhibitors
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amoxicillin+clavulanate (augmentin)
ticaricillin+clavulanate (timentin) |
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cephalosporins
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mechanism-
bind PBPs with failure of crosslinking causing dysfunction of cell wall bacteriacidal spectrum- gram+ *have been overused at broad spectrum absorption- most poorly absorbed across GI usually IM or IV restrictions- allergic s/sx include rashes and anaphylactic shock toxic rnx include bone marrow suppression |
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cefazolin and cephalexin
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1st generation of cephalosporin
gram+ and minimal gram- sensitive to penicillinase uses- 1st and 2nd generation drugs not used for active infections except in cases of penicillinallergy. most uses are as antibacterial prior to surgery |
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cefoxitin
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2nd generation of cephalosporin
high resistance to penicillinase high gram + effectivness high entry to CNS uses- 1st and 2nd generation drugs not used for active infections except in cases of penicillinallergy. most uses are as antibacterial prior to surgery |
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cefotaxamine
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3rd generation of cephalosporins
high gram + and - activity high resistance to penicillinase high entry into CNS uses- 3rd and 4th generation drugs used for meningitis resulting from gram- bacilli, gonorrhea, hemophilus influenzae, salmonella, and some nosocomial infections |
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cefepime
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high spectrum action high resistance to penicillinase
high entry into cns uses- 3rd and 4th generation drugs used for meningitis resulting from gram- bacilli, gonorrhea, hemophilus influenzae, salmonella, and some nosocomial infections |
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vancomyocin
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new systhetic drug
mechanism- inhibits cell wall synthesis by inhibiting peptidoglycan synthesis bacteriostatic spectrum- gram+ Absorption- poorly for GI, cant cross BBB, used for systemic use, must be used by IV uses- severe infections resistant to methicillin or in patients allergic to penicillin and cephalosporins very useful against staphococcal infections restrictions- side effects include skin rashes, anaphylactic shock, ototoxicity, nephrotoxicity |
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erytromyocin
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isolated from streptococcus
mechanism- binds and inhibits 50s ribosome to inhibit protein systhesis bacteriostatic against gram+ spectrum-broad absorption- oral, iv or im excreted by liver in bile uses- alternative to penicillin when pt is allergic legionaires disease whooping cough diphtheria chlamydial infections mycoplasma induced pneumonia side effects GI liver injury |
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clindamycin
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binds 50s ribosome to inhibit protein synthesis
used against abdominal and pelvic infections restrictions severe colitis-often fatal |
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tetracyclines
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bind and inhibit 30s ribosome
bacterialcidal for gram+ and some gram- broad spectrum given orally (75% crosses GI) |
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types of tetracycline
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tetracycline -shortest duration
demechlorcycline- medium doxycycline- long |
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uses of tetracyclines
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used to be used extensively but not as much now
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restrictions for tetracyclines
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GI upset
liver damage surpainfections, teeth discoloration, renal damage, ototoxicity |
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streptomyocin
neomycin kanamycin gentamicin tobramycin |
aminoglycosides
bind 30s ribosome bacterialcidal for gram+ and - broad spectrum and gram- may be more sensitive not well absorbed in GI IV topical for eye skin and nose only penetrates cns for meningitis uses- gram- such as e coli pseudomonas tubercle bacillus usualy reserved for serious infections because of their potential for toxicity damage to 8th cranial nerve- hearing loss crosses placenta to cause hearing loss causes dysfunctional at NMJ bacteria can become resistant |
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linezolid
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made in response to resistant bacteria
inhibit bacterial protein synthesis by inhibiting 30s bactericidal acts on gram+ new drug so s/sx are unknown |
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quinolone antibiotics
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inhibit topoisomerase to inhibit DNA fcn
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Nalidixic acid
cinoxacin norfloxacin ciprofloxacin |
quinolone antibiotics
inhibit systhesis and maintenance of dna broad spectrum (activity restricted only by ability to enter cytoplasm of gram - bacteria good oral absorption can lead to improper bone development in fetus cns effects nephrotoxicity GI problems uses- UTI, bacterial dirrhea, bone infections and for joints and soft tissue anthrax |
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gram + bacteria
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staph- pneumonia, endocarditis, osteomyelitis
strep- otitis media, meningitis, pneumonia enterococcus- endocraditis clostridium- gangrene,botulism,tetanus anthrax- anthrax |
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gram-
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campylobacter-ulcers
heliobacter- GI ulcers legionella- legionaires disease neisseria- gonorrhea, meningitis bordetella-whooping cough klebsiella- pneumonia escherichia- gi tract shigella-dysentry salmonella- enteritis hemophilus- meningitis, respiratory tract gardnerella- vaginitis bacteriodes- visceral, wounds, repro and respiratory, GI |
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chlamydias and rickettsias
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urinary and reproductive (chlamydia)
typhus (rickettsias) |
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spirochetes
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borrelis-lyme disease
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mycobacteria
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mycobacteria-leprosy, TB
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insomnia
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30% of us complains of poor sleep
causes by stress, drugs, pain, drug withdrawl trx-relaxation, exercise, drugs |
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anxiety
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sx-apprehension,tension, uneasyness
adaptive anxiety- useful to dealing with situation that induces it maladaptive anxiety- anxiety causing the disruption of normal activities panic disorder,social phobia, PTSD trx-behavioral changes drugs best ones are longer duration usually used chronically benzodiazepines mostly used |
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seizures
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cns driven muscle contractions
due to- stress,structural problem, traumatic injury, or fever trx- prophylactic (preventative) benzodiazepines and barbituates used |
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anesthesia
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lack of sensation of all types
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GABA
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major inhibitory neurotransmitter in CNS
all CNS neurons have GABA-a receptors and some have GABA-b activation of GABA-a will decrease neuronal activity |
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benzodiazepines
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enhance GABA
increases affinity of GABA for its binding site on the receptor lipid soluble absorbed orally widely distributed rapid onset |
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triazolam,oxazepam
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short (3-8 hrs) inactive
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midazolam
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short (3-8 hrs) and active
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alprazolam
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medium (10-20 hrs) active
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lorazepam and temazepam
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medium (10-20hrs) inactive
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diazepam and chlordiazepoxide
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long (1-3 days) active
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clonazepam
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long (1-3 days) inactive
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side effects of benzodiazepines
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daytime sedation
bizarre behaviors low abuse potential slow development of cellular tolerance and dependance side effects with ethanol psychotic patients may become aggressive not usually considered fatal. deaths usually come from addition of another sedative such as ethanol |
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triazolam and temazepam
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benzodiazepines
relief of insomnia reduces sleep induction time and decreases number of awakenings and nocturnal awake time |
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diazepam (valium), chlordiazepoxide, lorazepam, alprozalam (xanax)
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benzodiazepines
relief of anxiety may produce euphoria |
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diazepam (valium), clonazepam
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relief of seizures and sleep disorders
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diazepam (valium)
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relief of muscle spasm
acts on SC and not NMJ |
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alprazolam (Xanax)
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relief of panic disorders
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pre-anesthesia
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diazepam (valium)
lorazepam midazolam (versed) |
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anesthesia
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midazolam (versed)
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chlordiazepoxide (librium)
diazepam (valium) |
used for alcohol detox
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overdose of benzodiazepines
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confusion,sedation, sleep, coma
fatal overdose only with other sedatives like alcohol trx- flumazenil |
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barbiturates
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phenobarbital (luminal)
secobarbital thiopental pentobarbital |
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phenobarbital
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medium onset, long duration(12-18 hrs), sedative
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secobarbital
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short onset, medium duration (6-8hrs) sedative
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pentobarbital
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short onset, medium duration, sedative
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thiopental
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immediate onset (by iv), short duration (30sec), anesthetic
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barbituates actions
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paradoxical stimulation
sedation hypnosis anesthesia coma respiratory despression death |
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mechanism of barbituates
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enhance GABA
lipid soluble hepatic degradation and renal elinimation |
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side effects of barbituates
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tolerance and physical dependance
suppression of REM sleep liver dysfunction |
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uses of barbituates
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anticonvulsant
preanesthetic anesthesia |
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overdose of barbituates
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sedation leading to coma
trx- artificial respiration, increased urine production |
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zolpidem (ambien)
zaleplon (sonata) |
not benzodiazepines
activate benzodiazepine receptor short duration less likely to have daytime hangover, tolerance, or dependance |
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eszopicione (lunesta)
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not benzodiazepine
binds to BZ site to mimic BZ |
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ramelteon (rozerem)
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agonist at melatonin receptors
mimics melatonic to induce sleep not antiepileptic, or anesthetic |
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buspirone (buspar)
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does not act through GABA
little drowsiness or euphoria and no withdrawl problems latency of action 7-10 days side effects tachycardia, palpitations, nervousness |
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reactive depression
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not treated with drugs
cause known prevalent in young ppl |
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endogenous depression
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cause unknown
unipolar- about 20% of all deep melancholy, poor appetite, sleep disorders, fatigue, guilt, loss of interest in activites bipolar- periods of overactivity and periods of deep depression |
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drug induced depression
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some antihypertensives
antipsychotics sedatives |
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tricyclic antidespressants
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imipramine
desimipramine amytriptyline nortriptyline clomirpamine *amitriptyline have more potent anticholinergic effects while desipramine has less potent effects |
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mechanism of TCA's
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inhibits reuptake of NE and seratonin
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uses of TCAs
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unipolar depression
prevention of relapse of unipolar despression trx of bipolar eating disorders aid in chronic pain trx of anxiety |
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theraputic effects of TCAs
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short term use- delay 1-3 weeks for theraputic effects
effective for treating major depressions over 4-6 weeks long term use-trx for 6 mo to 1 yr as prophylactic no increased risk of side effects for long term use |
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side effects of TCAs
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dry mouth , blurred vision, constipation, sedation
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MAOIs
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isocarboxazid
phenelzine tranylcypromine |
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mechanism of MAOI
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inhibits monoamine oxidase
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uses and effects of MAOIs
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antidespressants
not often used because of dangerous food or drug interactions orthostatic hypotension hypertensive crisis |
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Fluoxetine (prozac)
sertraline (zoloft) paroxetine (paxil) bupropion (wellbutrin) trazodone (destrel) |
serotonin selective reuptake inhibitor
do nto act through NE delayed action reduced cholinergic effects |
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fluoxetine is marketed under what two names
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Prozac - depression
sarafem- PMDD |
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bupropion is marketed under what two names
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wellbutrin-depression
zyban- nicotine addiction |
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duloxetine (zymbalta)
venlafaxine (effexor) |
inhibit NW and 5HT reuptake
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lithium salts
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treat bipolar disorder
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lithium carbonate
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treatment of mania and bipolar disorder
not effective for unipolar depression may cause depression low theraputic index taken oraly eliminated via urine potential for toxicity when used with K wasting diuretics side effects apathy mescular rigidity tremor coma, death |
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TRX of ADHD
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MAOIs
Amphetamines |
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atomoxetine (strattera)
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inhibits NE reuptake
not used for depression! |
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buproprion (wellbutrin)
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inhibits 5ht reuptake and not NE
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Methyphenidate (ritalin)
amphetamine+dextroamphetamine (adderall) |
substitutes for NE on NE transporter
taken into NE axon terminals induces NE release |
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opiate effects
|
cns-analgesia of sc and brain
drowsiness and sedation in brain euphoria and dysphoria in brain pupillary constriction nausea and vomiting respiratory depression cough depressant blunting of baroreflex induces vasodialation decreased gi motility, absorption, bile secretion feces retention and constipation bladdre wall relaxation blunting of micturation reflex urine retention decreased uterine motility |
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morphine
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opiate receptor agonist
analgesic, sedative, respiratory depressant, antitissive, anti diarrheal, miotic tolerance and dependance highly addictive |
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fentanyl
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opiate receptor agonist
analgesic, sedative, respiratory depressant, antitissive, antidirrheal, tolerance and dependance highly addictive |
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meperidine (demerol, dolantin)
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analgesic, sedative, respiratory depressant
no miosis weak antitissive and antidirrheal weak effect on uterus used as IM injection shorter development of tolerance and dependance withdrawl sx shorter and less severe |
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oxycodone (percolone), hydrocodone (vicodin)
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similar to morphine
well absorbed orally addictive |
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methadone
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analgesic, sedative
similar sedation, respiratory depression and antitissuve less constipation effective orally longer duration used to relieve pain and trx of heroin addiction tolerance and depandance withdrawl less severe than morphine |
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codeine, dextromethorphan (delsym)
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opiate receptor agonist
less effective as analgesic than morphine more effective than asprin well absorbed oraly antitissuve doses that are not analgesic addictive |
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loperamide (imodium), diphenyoxylate (lomotin)
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opiate receptor agonist
effective orally low potential for abuse targets GI trx of diarrhea |
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morphine, meperidine (demerol), oxycodone, fentanyl
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relief of pain (trauma, surgery, MI, cancer
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morphine, fentanyl
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used with general anesthetic
morphine - analgesic fentanyl- amnesiac |
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diphenyoxylate (lomotil), loperamide (imodium)
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antidiarrheal
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codeine, dextromethorphan
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antitussive
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morphine, meperidine
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trx of dyspnea
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methadone
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trx of opiate addiction
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major side effects of opiate receptor agonists
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tolerance
dependance withdrawl (irritability, insomnia, chills, sweating, nausea, vomiting, diarrhea, cramps, pupil dialation) addiction compulsive drug use |
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detection of addiction
|
use of opiate receptor antagonist to initiate withdrawl
if no effect then no addiction naloxone naltrexone |
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overdose of opiate receptor agonists
|
triad (pinpoint pupils, respiratory depression, coma)
hypothermia muscle flacidity convulsions trx- opiate antagonist |
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naloxone
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pure antagonist
IV only |
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naltrexone
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pure antagonist
orally useful |
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uses of opiate receptor antagonists
|
reversal of opiate overdose
test for dependance prevent occurance of addiction trx of alcohol addiction |
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ziconotide
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CNS acting analgesics
injected intraspinally targets neuronal ca channel reduces transmitter release from neurons reduces pain many possible side effects |
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gabapentin, pregabalin
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cns active analgesic
orally related to GABA but do not act on GABA r's targets neuronal ca channel reduces pain many potential side effects |
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duloxentine (zymbalta), imipramine (tofranil), amitriptyline, fluoxetine (prozac)
|
cns acting analgesic
orally target seratonin reuptake enhances activation and release of dynorphin from dynorphinergic nerons to reduce pain many possible side effects |
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positive sx of schizophrenia
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distortion of nml activity
paranoia delusions hallucinations disordered thinking (word salad) |
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negative sx of schizophrenia
|
diminution of nml activity
blunted emotional response social withdrawl lack of speech |
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|
chlorpromazine (thorazine)
thoridazine (mellaril) haloperidol (haldol) |
typical antipsychotic drugs
have good effect on positive signs side effects with include movement disorders |
|
|
olanzepine,resperidone, clozapine
|
atypical antipsychotic drugs
have good effect on positive sx and on negative sx of schizophrenia do not produce or produce much less movement disorders |
|
|
mechansm of action for antipsychotic drugs
|
antagonist at dopamine receptors
effects due to actions at limbic and cortical regions of the brain |
|
|
use of antipsychotic drugs
|
treat
schizophrenia, mania, psychotic disorders |
|
|
effect of antipschotic drugs
|
orthostatic hypotension
reflex tachycardia sedative blurred vision inhibition of prolactin secretion effects on movement parkinsons like sx |
|
|
trx of parkinsons
|
increase Dopamine and decrease ach in brain
no cure relief of sx is best surgical- cell transpants, removal of brain lesions |
|
|
levodopa (dopar)
|
trx of parkinsons
precourser of dopamine incrases dopamine production does not prevent progressive cell death effectiveness decreases with time used with carbidopa |
|
|
carbidopa+levodopa (sinemet)
|
carbidopa increases central effects of ldopa by increasing central availability of ldopa
side effects-nausea, vomiting, psychosis, depression, jerky movements, hypotension (reflex tachycardia) |
|
|
amantadine (symmetrel)
|
slows reuptake of dopamine into neurona
useful in early stages may be used with L dopa |
|
|
bromocriptine, pergolide
|
dopamine receptor agonists
do not alter domamine synthesis or degradation effective in early stages |
|
|
pramipexole, ropinirole
|
newer dopamine receptor agonists
do not alter dopamine synthesis or degradation increase brain dopamine availability only useful in early stages in the disease |
