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Pharm
Exam 4
125
Pharmacology
Professional
01/02/2013
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Term
Amphotericin B
 Definition
Antifungal. Polyene Macrolide. Antibiotic produced by Streptomyces. MOA: Binds to sterols in fungi; Can also bind to kidney and erythrocytes. TOX: Fever and chills; Renal (azotemia); anemia (decreased EPO). USE Systemic; superficial (candidiasis); protozal infections. DENTAL: No significant effects or complications except liposomal (Ambisome): facial swelling, postural hypotension, mucositis, stomatitis.
Term
Ketoconazole
 Definition
Antifungal. Imidazole. MOA: Inhibition of 14-α-demethylase affects ergosterol biosynthesis and membrane function. Half life 7-8 hours. TOX: GI nausea and vomiting; Endocrinologic abnormalities; inhibits P450 3A4 USE: Systemic; superficial (candidiasis and ringworm). DENTAL: none.
Term
Micronazole
 Definition
Antifungal. Imidazole. MOA: Inhibition of 14-α-demethylase affects ergosterol biosynthesis and membrane function. Half life 12 hours. TOX: low. USE systemic; superficial(candidiasis). DENTAL: none. Emperic anitfungal therapy
Term
Fluconazole
 Definition
Antifungal. Tridazole. MOA: Inhibition of 14-α-demethylase affects ergosterol biosynthesis and membrane function. Half life 25-30 hours. TOX: low. USE systemic; superficial (candidiasis; interacts with members of cytochrome P-450 family DENTAL: abnormal taste. Alternative to Ketoconazone since less toxic.
Term
Itraconazole
 Definition
Antifungal. Tridazole. MOA: Inhibition of 14-α-demethylase affects ergosterol biosynthesis and membrane function. Half life 30 hours. TOX: low, increases plasma concentration of drugs metabolized by cytochrome P450 family. USE: systemic; superficial (candidiasis). DENTAL: none.
Term
Griseofulvin
 Definition
Antifungal. MOA: Disrupts cell mitotic apparatus, arrests cells in metaphase; Depositied in keratic precursor cells. TOX: CNS (headache) GI (nausea, vomiting) Hypersentivity rare. USE: Dermatophytoses. DENTAL: Soreness or irritation of mouth or tongue. May cause oral thrush.
Term
Nystatin
 Definition
Antifungal. Polyene antibiotic produced by Streptomyces noursei. MOA: binds to sterols of fungal cell membrane, cells leak. TOX: low, hypersensitivity rare. USE candidiasis. Dental: none.
Term
Terbinafine Hydrochloride
 Definition
Antifungal. Sythetic allylamine. MOA: inhibition of squalene monooxygenase affects ergosterol biosynthesis and membrane function. TOX: low. USE dermatophytoses, candidiasis. DENTAL: taste disturbance.
Term
Caspofungin
 Definition
Antifungal. Semisynthetic lipopeptide. MOA: blocks synthesis of β (1,3)-d-glucan, a polysaccharide of the fungal cell wall. TOX: fever, rash, nausea, vomiting. USE: systemic (aspergillosis), esophageal candidiasis. DENTAL: none.
Term
Immune Globulin
 Definition
Antiviral. Human Immune Globulin (IgG; IgM). MOA: prevention of attachment and penetration fo viral particles into host cell; passive immunity increased; prevention of infectious diseases in susceptible individuals. USE: prevention of measles and hepatitis A; Prophylactically for hepatitis B and measles. TOX: mild; susceptible individuals to immune globulin or ingredients of formulations. DENTAL: none
Term
Palivizumab
 Definition
Antiviral. Humanized monoclonal antibody (IgG1) MOA: Antibody neutralizes respiratory syncitial virus (RSV) inhibiting pathogenesis in infants and children. USE: prevention of serious lower respiratory tract disease caused by RSV. TOX: fever, otitis, rhinitis, upper respiratory tract infections, acute anaphylaxis/hypersensitivity. DENTAL: none.
Term
Amantadine
 Definition
Antiviral. Synthetic trycyclic amine. MOA: blocks penetration and uncoating of virus by buffering the pH of endosomes. Blocks M2 viral protein channel required for nucleocapsid release USE influenza A virus (RNA virus). TOX: CNS effects. DENTAL: xerostomia (normal salivary flow resumes upon discontinuation); orthostatic hypotension.
Term
Ribavirin
 Definition
Antiviral. Purine nucleoside. MOA: DNA and RNA synthesis inhibition, inhibits RNA polymerases and thus messenger RNA synthesis. USE: NOT indicated for use in adults; Respiratory syncytial virus (RNA virus); Hep C virus (RNA virus) in combination with interfreon alpha TOX teratogenesis. DENTAL: xerostomia (normal salivary flow resumes upon discontinuation); taste perversion
Term
Zanamivir
 Definition
Antiviral. Dihydro-oxane derivative. MOA: nuraminidase inhibitor USE influenza A and B. TOX: nasal and throat discomfort but uncommon. DENTAL: none
Term
Oseltamivir
 Definition
Antiviral. Cyclohexane derivative. MOA: nuraminidase inhibitor. USE: influenza A and B. TOX nausea and vomiting and headache. DENTAL: none
Term
Trifluridine
 Definition
Antiviral. Pyrimidine nucleoside. MOA: DNA synthesis inhibition (viral and cellular), TK phosphorylates to triphosphate derivative, which inhibits viral and cellular DNA polymerases by causing chain termination USE: Herpes simplex keratitis (DNA virus). TOX: teratogenic; visual haze (burning or stinging and palpable edema.) DENTAL: none.
Term
IFN-α-2b
 Definition
Antiviral. Glycoprotein. MOA: viral protein and replication inhibition, inhibits translation USE: genital and anal warts; hep B; hep C and ribavirin. TOX: flu-like syndrome; myalgia; transient hematologic. DENTAL: xerostomia (normal salivary flow resumes upon discontinuation); metallic taste, taste alteration, gingivitis.
Term
Acyclovir
 Definition
Antiviral. Purine Nucleoside. MOA: DNA synthesis inhibition, inhibits herpes viral DNA polymerase and thereby inhibits viral DNA synthesis and viral replication USE: mucosal, cutaneous, systemic herpes simplex; genital herpes; varicella zoster. TOX: virtually nil. DENTAL: systemic - none. topical - dry, cracked lips and dry, flaky skin in fewer than 1 in 100
Term
Ganciclovir
 Definition
Antiviral. Purine Nucleoside. MOA: DNA synthesis inhibition. USE: cytomegalovirus (DNA virus) retinitis. TOX: teratogenic; myelosuppression; neutropenia. DENTAL: none.
Term
Foscarnet
 Definition
Antiviral. Phoponoformic acid. MOA DNA synthesis inhibition. USE cytomegalovirus retinitis in AIDS pts. TOX: renal. DENTAL xerostomia (normal salivary flow resumes upon discontinuation); taste perversion; ulcerative stomatitis.
Term
Natural Penicillins
 Definition
Pen G & Pen VK. G = parenteral. V = oral. ~90% of Staph aureus resistant. Pneumococcal pneumonia ~25% resistance. Pneumococcal meningitis usually sensitive. Steptococcal pharyngitis resistance not a problem. Given with aminoglycoside for synergistic effect. activity against neisseria meningitidis, clostridium perfringens, clostridium tetani, treponema pallidum, actinomycetes israelii. Probenicid increases plasma levels of penicillin. Pen G highly effects to tx of syphilis at all stages
Term
Penicillin V
 Definition
Natural penicillin. Modified side chain therefore is more stable then Pen G under acidic conditions. Less active than Pen G for most microorganisms = used for tx of minor infections.
Term
Penicillin G Procaine and Penicillin G Benzathine
 Definition
Natural penicillin. Repository form that provide a slow release from injected area (Glute / thigh). Pen G procaine - strep pyogenes. Pen G benzathine - strep pharyngitis; prophy for rheumativ fever by reinfection with group a strep; syphilis at all stages
Term
Penicillinase Resistant Penicillins
 Definition
Nafcillin, Oxacillin. Bulky side group makes them resistant to breakdown by staph beta-lactamases. Nafcillin one of the most resistant to break down. Do not need to adjust for renal failure (eliminated in bile). Because of increase in MRSA the empirical use of these drugs dropped. IV admin preferred for Nafcillin. For serious systemic staphylococcal infections, Naf and Oxa are administered IV. Drug of choice for penicillinase producting (gm+ cocci) Staph aureus --> skin infections, soft tissue infections, osteomyelitis, acute endocarditis.
Term
Extended Spectrum Penicillins.
 Definition
Ampicillin, Amoxicillin. Greater activity against gram (-) bacteria than Pen G b/c they better penetrate the outer membrane. Susceptible to breakdown by beta-lactamase. Can be combined with beta-lactamase inhibitors. "HELPSS- ME." Amoxicillin causes less diarrhea than Ampicillin. Decreased effectiveness of comboination oral contraceptives (kill off the normal microbial flora that hydrolyze the ethinyl estradiol conjugates.)
Term
Augmentin
 Definition
Amoxicillin & Clavulanic Acid.
Term
Unasyn
 Definition
Ampicillin & Sulbactam
Term
Antipsuedomonal
 Definition
Carboxypenicillins and Ureidopenicillins. Active against Pseudomonas; penicilin-resistant anerobes; major use is for peudomonal infections such as septicemia and UTIs; mixed aerobic-anerobic infections.
Term
Ticarcillin & Clavulanate potassium
 Definition
Antipseudomonal penicillin. Carboxypenicillin. Dose must be adjusted for impaired renal function. Ticarcillin inactivated by beta-lactamase. Useful for treating seriuos infections cause by gm (-) aerobic bacilli and mixed aerobic-anaerobic. Excessive Na can be problematic for pts with CHF or renal failure. Can prolong bleeding time.
Term
Piperacillin & Tazobactam
 Definition
Antipseudomonal penicillin. Ureidopenicillin. Broader spectrum of activity than ticarcillin. Often used in combo with aminoglycoside for synergistic kiling (avoid in vitro mixing) Tx of serious infections cause by gm (-) aerobic bacilli and mixed aerobic-anerobic infections; CAP by H influenzae or Ps aeruginosa; Nosocomial peuemonia by H influenzae, Klebsiella pneumoniae or Ps. aeruginosa; septicemia, burns, pneumonia, UTIs, intra-abdominal. Less Na and bleeding than Ticarcillin.
Term
Aztreonam
 Definition
Monobactam. highly resistant to breakdown by beta-lactamase produced by gm (-) bacilli. Similar spectrum of activity as aminoglycoside. Activity against MDR pseudomonas. UTIs, intra-abdominal infections, gynecological infections, lower-respiratory infections. Pts allergic to penicillins appear not to reat to actreonam (b/c of unique chemical structure.)
Term
Imipenem & Cilastatin
 Definition
Carbapenms. "Big Gun" active >90% clinically important bacteria. Broadest spectrum. Imperical therapy for life threatening illness. Imipenem is rapidly broken down by dehydropeptidases in renal tubule. Cilastatin inhibits this enzyme and increases concentrations of Imipenem in the kidney. Increased permeability through porin channels in gm (-) bacteria, resistance to beta-lactamase, and high affinity to PBP. NOT uses for CAP, reserved for serious hospital acquired infections; Mixed aerobic/anerobic; infections resistant to penicillin family members. Seizures in pts with renal failure; serious Ps. aeurginos infections resistant to other beta-lactamases. Should be used in combo with aminoglycoside.
Term
Clavulanic Acid
 Definition
Beta-lactamase inhibitor. Resemble beta-lactam antiB in structure but have only weak antibacterial activity. More active against plasmid encoded beta-lactamases v. inducible chromosomal beta-lactamases
Term
Tazobactam
 Definition
Beta-lactamase inhibitor. Resemble beta-lactam antiB in structure but have only weak antibacterial activity.
Term
Augmentin
 Definition
Amoxicillin & Calvulanic acid. UTIs, respiratory (ear and Sinus), Human animal bite wounds (S. aureus).
Term
Timentin
 Definition
Ticarcillin & Clavulanic acid
Term
Zosyn
 Definition
Piperacillin and Tazbactam
Term
Cefazolin
 Definition
Cephalosporin. 1st generation. Does not have good penetration into CNS even when meninges are inflamed. Susceptible to breakdown by beta-lactamase. Good against gm(+) modest against gm(-). Alternate agent for penicillin for Strep and Staphylococcal infections in pts with mild penicillin allergy. Activity against oral cavity anerobes. "PECK" not active against pseudomonas aeruginosa. Not used for serious systemic infections. Drug of choice for surgical prophy. Intolerence of alcohol. Bleeding disorders
Term
Cephalexin
 Definition
Cephalosporin. 1st generation. Does not have good penetration into CNS even when meninges are inflamed. Susceptible to breakdown by beta-lactamase. Alternate agent for penicillin for Strep and and Staphylococcal infections in pts with mild penicillin allergy."PECK" not active against pseudomonas aeruginosa. Not used for serious systemic infections.
Term
Cefaclor
 Definition
Cephalosporin. 2nd generation. Does not have good penetration into CNS even when meninges are inflamed. Susceptible to breakdown by beta-lactamase. Less gm+ activty than 1st generation, more gm-. NOT active against pseudomonas aeruginosa. Sinusitis; otitis media. More commonly implicated in causing serum-sickness like reactions like erythema multiforme
Term
Loracarbef
 Definition
Cephalosporin. 2nd generation. Does not have good penetration into CNS even when meninges are inflamed. Less gm+ activty than 1st generation, more gm-. NOT active against pseudomonas aeruginosa.Sinusitis; otitis media.
Term
Cefoxitin
 Definition
Cephalosporin. 2nd generation. Does not have good penetration into CNS even when meninges are inflamed. Less gm+ activty than 1st generation, more gm-. activity against. NOT active against pseudomonas aeruginosa. B. fragilis
Term
Cefuroxime
 Definition
Cephalosporin. 2nd generation. Does not have good penetration into CNS even when meninges are inflamed. Less gm+ activty than 1st generation, more gm-. NOT active against pseudomonas aeruginosa. Sinusitis; otitis media. Strep pneumoniae
Term
Cefprozil
 Definition
Cephalosporin. 2nd generation. Does not have good penetration into CNS even when meninges are inflamed. Less gm+ activty than 1st generation, more gm-. NOT active against pseudomonas aeruginosa. Sinusitis; otitis media.
Term
Ceftriaxone
 Definition
Cephalosporin. 3rd generation. Tx of Meningitis. Much more active against gm- than second generation. Less active than first generation against gm+. Longest half-life of cephalosporins. active against strep pneumoniae, lyme disease. First line drug of choice for tx of gonorrhea by n. gonorrhoeae. Mainly extected via bile so dosage adjustments with renal failure not required.
Term
Cefixime
 Definition
Cephalosporin. 3rd generation. Much more active against gm- than second generation. Less active than first generation against gm+. First line drug of choice for tx of gonorrhea by n. gonorrheae.
Term
Ceftizoxime
 Definition
Cephalosporin. 3rd generation. Tx of Meningitis.Much more active against gm- than second generation. Less active than first generation against gm+
Term
Ceftazidime
 Definition
Cephalosporin. 3rd generation. Tx of Meningitis.Much more active against gm- than second generation. Less active than first generation against gm+. pseudomonas aeruginosa.
Term
Cefepime
 Definition
Cephalosporin. 4th generation. Tx of meningitis. Penetrates CSF in animal models. Pseudomonas aeurginosa, some enterobacteriaceae. , penicillin-resistant streptococci.
Term
Chloramphenicol
 Definition
Broad spectrum antiB. Not a first line agent b/c of tox. Mostly used for life threatening bacterial meningitis (H. influenzae, N. Meningitidid, Strept pneumoniae); brain abscess; rickettsial infections. Binds to 50S. Widely distributed in body and reaches therapeutic levels in CSF. Adjust dose for premi/infants, hepatic failure but not renal failure (glucuronide conjugate does not cause toxicity.) Mostly bacteriostatic, cidal for H. influenzae, N. Meningitidid, Strept pneumoniae, Bacteroides. RESISTANCE: bacteria produces acetyltransferase which acetylates chloramphenicol and prevents binding to ribosome. TOX: can also inhibit mitochondrial protein synthesis in mammalian cells;Reversible bone marrow supression, aplastic anemia. Gray baby syndrome.
Term
Tetracycline
 Definition
Tetracycline. Short acting. Broad spectrum. Bacteriostatic. Bind to 30S to block binding of amino acid containing amnioacyl-tRNA = new amino acids cant be added to growing chain. Widely distributed throughout body with exception of CSF; but cross placenta and found in breast milk. RESISTANCE increased efflux by an active transport pump. ACTIVITY not drug of choice for many gm+ aerobic inections. Mycoplasma pneumoniae. TOX GI, superinfection C. diff and vaginal or oral candidiasis. Can bind to calcium and the complex can be deposited into teeth. Renal damage, Phototosensitivity.
Term
Doxycycline
 Definition
Tetracycline. Long acting. Broad spectrum. Bacteriostatic. Bind to 30S to block binding of amino acid containing amnioacyl-tRNA = new amino acids cant be added to growing chain Widely distributed throughout body with exception of CSF; but cross placenta and found in breast milk. Preferred for IV admin.(serious infections and if oral admin causes GI problems). Excreted by non-renal mechanisms and does not accumulate with renal failure. RESISTANCE increased efflux by an active transport pump. Drug of choice to tx lyme disease (borrelia burgdorferi (spirochetes)). Drug of choice for RMSF. TOX GI, superinfection C. diff and vaginal or oral candidiasis. Can bind to calcium and the complex can be deposited into teeth. Renal damage, Phototosensitivity.
Term
Minocycline
 Definition
Tetracycline. Long acting. Broad spectrum. Bacteriostatic. Bind to 30S to block binding of amino acid containing amnioacyl-tRNA = new amino acids cant be added to growing chain Widely distributed throughout body with exception of CSF; but cross placenta and found in breast milk. Lipid soluble secreted in tears and saliva. RESISTANCE increased efflux by an active transport pump. TOX GI, superinfection C. diff and vaginal or oral candidiasis. Can bind to calcium and the complex can be deposited into teeth. Renal damage, Phototosensitivity.
Term
Tigecycline
 Definition
Newer antibiotic. Eliminated by non-renal mechanisms (no dosage adjustment for renal failure). Same MOA as tetracycline. Not effectively pumped out of bacteria by Tet(AE) or Tet(K) efflux pumps. Tet(M) ribosomal protection protein does not block binding to 30S ribosome. Proteus sp. and Pseudomonas resistant. Some activity against MRSA. TX skin an skin structure infections and intra-abdominal infections.
Term
Erythromycin
 Definition
Macrolide. Bacteriostatic, at high concentrations may have some cidal actions. Bind to 50S ribosomal subunit and prevent movement of polypeptide chain from the acceptor to donor site. Widely distributed but does not enter brain or CSF. Poor oral absorption as broken down by acid, enteric coating improves. Esters have been produced to increase oral absorption and increase acid stability. Metabolized by hepatic p450 system. Do not need to adjust dose for renal function, avoid with liver disease. RESISTANCE by modification of the 50S by the bacterial enzyme methylase. NOT a good anerobic agent. Mycoplasma pneumonia, Leginella pneumophila, nonstreptococcal pharyngitis, chlamydial infections. TOX GI, liver. Can inhibit cytochrome p450
Term
Clarithromycin
 Definition
Macrolide. Bacteriostatic, at high concentrations may have some cidal actions. Bind to 50S ribosomal subunit and prevent movement of polypeptide chain from the acceptor to donor site. Widely distributed but does not enter brain or CSF. Semi-synthetic derivative which increases stability in acid, tissue permeability, and increase the antiB spectrum of activity. Do not need to adjust dose for renal function, avoid with liver disease. RESISTANCE by modification of the 50S by the bacterial enzyme methylase. NOT a good anerobic agent. More active agains mycobacterium avum, H. influenzae. Pharyngitis/tonsillitis, Sinusitis, bronchitis, CAP, uncomplicated skin infections TOX GI(Less than erythromycin), liver. Inhibits cytochrome p450
Term
Azithromycin
 Definition
Macrolide. Bacteriostatic, at high concentrations may have some cidal actions. Bind to 50S ribosomal subunit and prevent movement of polypeptide chain from the acceptor to donor site. Widely distributed but does not enter brain or CSF. Semi-synthetic derivative which increases stability in acid, tissue permeability, and increase the antiB spectrum of activity. Do not need to adjust dose for renal function, avoid with liver disease. RESISTANCE by modification of the 50S by the bacterial enzyme methylase. NOT a good anerobic agent. TOX GI, liver
Term
Streptomycin
 Definition
Aminoglycoside. Less activity against gm- bacteria than other aminoglycosides. Used in combo with Pen G to treat bacterial endocarditis. Gentamicin ususally preferred over this drug for treating endocarditis. But some gentamicin resistant strains are susceptible to this drug. Commonly associated with vestibular toxicity
Term
Gentamicin
 Definition
Aminoglycoside. Hospital acquired UTI - good coverage against gm- bacteria. Use in combo with a beta-lactam antibiotic to get good initial coverage. Hospital acquired pneumonia cause by gm- bacilli. Aminoglycoside and beta-lactam antibiotic. Not recommended for CAP. Once Antibiotic susceptibility tests are performed if there is a less toxic antibiotic you can switch to another drug.Gm+ infections - entercococcal endocarditis, use in combo with PenG. Sepsis by gm- bacilli, use in combo with antipseudomonal penicillin. Auditory, vestibular, and nephrotoxcity.
Term
Tobamycin
 Definition
Aminoglycoside. Hospital acquired UTI - good coverage against gm- bacteria. Use in combo with a beta-lactam antibiotic to get good initial coverage. Hospital acquired pneumonia cause by gm- bacilli. Aminoglycoside and beta-lactam antibiotic. Not recommended for CAP. Once Antibiotic susceptibility tests are performed if there is a less toxic antibiotic you can switch to another drug. Slightly better activity agains pseudomonas aeruginosa. Tx sepsis, osteomyelitis and pneumonia by pseudomonas sp. vestibular and nephrotoxicity
Term
Amikacin
 Definition
Aminoglycoside. Hospital acquired UTI - good coverage against gm- bacteria. Use in combo with a beta-lactam antibiotic to get good initial coverage. Hospital acquired pneumonia cause by gm- bacilli. Aminoglycoside and beta-lactam antibiotic. Not recommended for CAP. Once Antibiotic susceptibility tests are performed if there is a less toxic antibiotic you can switch to another drug. Broades spectrum of activity of all aminoglycosides. Resistant to bacterial aminoglyucoside inactivation enzymes. Use is reserved for serious hospital acquired gm- bacilli infections. auditory toxicity.
Term
Ciprofloxacin
 Definition
Fluoroquinolone. Bactericidal. Inhibit DNA gyrase and Toppisomerase IV. Oral absorption impaired by divalent cations found in antacid. Also zinc, Fe and Ca. Excreted by kidney. UTIs by MDR bacteria, Prostatitis, Bacterial diarrhea, LRT infections like CAP. NO against gonorrhea. TOX: Nausea, headache, dizziness most common. CNS stim (inhibits GABA, use caustion with epileptics. Photosensitivity, dame cartalige (not <18y)
Term
Levofloxacin
 Definition
Fluoroquinolone. Bactericidal. Inhibit DNA gyrase and Toppisomerase IV. Oral absorption impaired by divalent cations found in antacid. Also zinc, Fe and Ca. Excreted by kidney. active against gm+ bacteria like strep pneumoniae. TOX: Nausea, headache, dizziness most common. CNS stim (inhibits GABA, use caustion with epileptics. Photosensitivity, dame cartalige (not <18y)
Term
Moxifloxacin
 Definition
Fluoroquinolone. Bactericidal. Inhibit DNA gyrase and Toppisomerase IV. Oral absorption impaired by divalent cations found in antacid. Also zinc, Fe and Ca. Excreted by non-renal mechanisms. Most active against gm+ bacteria like strep pneumoniae.TOX: Nausea, headache, dizziness most common. CNS stim (inhibits GABA, use caustion with epileptics. Photosensitivity, dame cartalige (not <18y). Non renal excretion, dosage does NOT need to be adjusted for pts with renal failure.
Term
Vancomycin.
 Definition
bactericidal antibiotic. Inhibits bacterial cell wall syn. Resistance from alterations in cell wall precursors so it can't bind IV admin. Can penetrate CSF when meninges inflammed. 1. Serious staph infections by MRSA; 2 gm+ infections in pts allergic to Pen and Cephalo; 3 Diarrhea/pseudomembranous colitis by c diff; 4 memingitis by staph in pts allergic to beta-lactam antiB (inculde with 3rd generation cephalo for meningitis with pen-resistant strep pneumoniae). TOX: otottoxicity and nephrotoxicity (rare), "red neck."
Term
Clindamycin
 Definition
Bacteriostatic. MOA: binds to 50S ribosomal subunit and inhibits protein synthesis. RESISTANCE: mutations in 50S prevent drug from binding. Bacteria produce methylase that modifies 50S. Resistance to erythromycin usually means resistance to clindamycin. DOES NOT penetrate the CNS well for bacterial meningitis, but does penetrate well into abscess. Metabolized by liver and excreted into bile. good activity against gm- and gm+ anerobes (B. fragilis) --> penetrates well into abscesses; prophy for endocarditis in high risk pt for dental procedure with pen allergy. TOX pseudomembranous colitis from c. diff.
Term
Nitrofurantoin
 Definition
Bactericidal and static. good oral absorption. Intact drug and metabolites rapidly excreted into urine, so rapid systemic effects not seen. NOT for use in pts with renal failure. MOA Reduced form of the drug may damage bacterial DNA. Pseudomonas aeruginosa and many proteus strains resistant. ***USE tx of chronic UTI (urinary tract antiseptic)*** TOX GI (anorexia, nausea, vomiting); rare hemolytic anemia.
Term
Polymyxins B & E
 Definition
Small peptides produced by Bacillus polymyxa and Bacillus colistinus. B- opthalmic, otic, and topical; can be combined with neomycin (used to irrigate urinary bladder with indewelling catheters) and bacitracin for topical. E- parenterally; associated with nephro and neurotoxicity MOA cationic detergent and interacts with cell membrase phospholipids to disrupt the cell membranse = leakage of intracellular components. Better activity against gm-.
Term
Metronidazole
 Definition
Drug of choice for anerobes (B. fragilis and C. diff). Bactericidal. good oral absorption. Widely distributed through the body (CNS and brain). Metabolized in liver and excreted in urine. MOA reduced form of the drug can bind to intracellular macromolecules and inhibit DNA synthesis. USE NOT really effectve agains gm+ or gm- aroves. Anerobic infections like brain abscesses and pseudomembranous colitis; tx of peptic ulcer cause by H. pylori. TOX carcinogenic potential in animals - avoid with breast feeding and pregnancy. Dilsulfiram like interaction with alchool. Nausea, diarrhea, peripheral neuropathy with prolonged use.
Term
Bacitracin
 Definition
Group of polypeptide antibiotics produced by Bacilus subtilis. Opthalmic and dermatological uses. Not used parenterally b/c of nephrotoxicity. MOA inhibits bacterial cell wall synthesis by interacity with lipids that transport the peptidoglycan subunits. Active against many gm+ and some gm- lik Neisseria and H. influenzae. Used topically for open wounds; eye infections. TOX nephrotoxicity due to tubular and glomerular necrosis.
Term
Zidovudine
 Definition
Nucleoside reverse transcriptase inhibitor. MOA: prevents phosphodiester linkage from being formed. TOX: neutropenia / anemia; CNS, GI, HEMA. USE: alone, started at 14-34 weeks of gestation, and continued in infant for first 6 w of life may decrease HIV transmission. DENTAL: taste perversion, oral mucosa pigmentation, dysphagia, mouth ulcer
Term
Didanosine
 Definition
Nucleoside reverse transcriptase inhibitor. MOA: competes with dATP for active site of enzyme, leads to chain termination. TOX peripheral neuropathy, potentially fatal pancreatitis and GI disturbances. DENTAL: xerostomia
Term
Lamivudine
 Definition
Nucleoside reverse transcriptase inhibitor. TOX: low cellular toxicity, does not cause peripheral neuropathy. nasal congestion, nausea, malasise, fatigue, flare of HEP B USE also active against Hep B. DENTAL: none
Term
Abacavir
 Definition
Nucleoside reverse transcriptase inhibitor. TOX: severe hypersensitivity with rash, fever and malaise and sometimes respiratory and GI symptoms. DENTAL: none
Term
Emtricitabine
 Definition
Nucleoside reverse transcriptase inhibitor. TOX: among the best tolerated; hyperpigmentation of palms and soles. Flare of Hep B DENTAL: none.
Term
Tenofavir
 Definition
Nucleotide reverse transcriptase inhibitor. effective to HIV strands that are resistant to other reverse transcriptase inhibitor. TOX: nausea, vomiting and diarrhea; RENAL TOXICITY; flare of Hep B. USE HIV and Hep B. DENTAL: none
Term
Nevirapine
 Definition
Non-nucleoside reverse transcriptase inhibitor. Binds directly to reverse transcriptase. Metabolized by cytochrome p450 = interaction with -azole antifungals. TOX severe hepatotoxicity; fever, nausea, headache; rash is common in early tx. DENTAL: ulcerative stomatitis and oral lesions.
Term
Efavirenz
 Definition
Non-nucleoside reverse transcriptase inhibitor. TOX: dizziness, headache, insomnia, inability to concentrate and rash; nueral tube defects. DENTAL: abnormal taste
Term
Ritonavir
 Definition
HIV Protease inhibitor. TOX: nausea vomiting, weakness and diarrhea; circumoral and peripheral paresthesias, elevated aminotransferases; extensively metabolized by hepatic p450. DENTAL: xerostomia and taste perversion.
Term
Indinavir
 Definition
HIV Protease inhibitor. TOX: nephrolithiasis, dermatologic changes including alopecia, dry skin and mucous membranes; hyperbilirubinemia; GI extensively metabolized by hepatic p450. DENTAL: abnormal taste.
Term
Nelfinavir
 Definition
HIV Protease inhibitor. most commonly used protease inhibitor. TOX: diarrhea, nausea. DENTAL: mouth ulcers.
Term
Regular insulin
 Definition
Rapid acting insulin preparation. Clear solution, human sequence. Relatively short acting. Only insulin available for IV use.
Term
Insulin Aspart
 Definition
Rapid acting insulin preparation. More readily forms monomer in solution than regular insulin.
Term
Insulin glulisine
 Definition
Rapid acting insulin preparation. More readily forms monomer in solution than regular insulin.
Term
Insulin lispro
 Definition
Rapid acting insulin preparation. More readily forms monomer in solution than regular insulin.
Term
NPH insulin
 Definition
Intermediate acting insulin preparation. Cloudy, colloidal suspension, human sequence. Aggregates and time involved in breaking down.
Term
Insulin glargine
 Definition
Long acting insulin preparation. Soluble at pH 4, poorly soluble at pH7. When injected SQ, form microprecipitant in interstitial fluids.
Term
Insulin detemir
 Definition
Long acting insulin preparation. Long acting due to self association at SQ injections site and binding to albumin.
Term
Metformin
 Definition
Biguanide. MOA: reduces hepatic gluconeogenesis "euglycemic agent." Prevents hyperglycemica, but does not induce hypoglycemia. TOX: GI and lactic acidosis (rare). CONTRAINDICATION: alcoholism, renal insufficiency, hepatic disease, hypoxic pulmonary. USE: Firt-line therapy for T2DM; weight loss, decrease LDL and VLDL
Term
Glyburide
 Definition
Sulfonylurea. Second generation. MOA: increases endogenous insulin secretion by inhibiting K_ATP channels of pancreatic B cells. TOX: hypoglycemia, weight gain, sulfa allergy. CONTRAINDICATIONS: hepatic/renal insufficiency, pregnant and breastfeeding women, pts susceptible to hypoglycemia.
Term
glipizide
 Definition
Sulfonylurea. Second generation. MOA: increases endogenous insulin secretion by inhibiting K_ATP channels of pancreatic B cells. TOX: hypoglycemia, weight gain, sulfa allergy. CONTRAINDICATIONS: hepatic/renal insufficiency, pregnant and breastfeeding women, pts susceptible to hypoglycemia.
Term
Glimepiride
 Definition
Sulfonylurea. Second generation. MOA: increases endogenous insulin secretion by inhibiting K_ATP channels of pancreatic B cells. TOX: hypoglycemia, weight gain, sulfa allergy. CONTRAINDICATIONS: hepatic/renal insufficiency, pregnant and breastfeeding women, pts susceptible to hypoglycemia.
Term
Repaglinide
 Definition
Meglitinides. MOA: "Insulin secretagogues" inhibits the activity of K_ATP channels. TOX: hypoglycemia and weight gain (taken before a skipped meal). TOX: hepatic/renal insufficiency. USE: may be suitable for pts with sulf allergy, more frequent pre-prandial dosing possible.
Term
Nateglinide
 Definition
Meglitinides. MOA: "Insulin secretagogues" inhibits the activity of K_ATP channels. TOX: hypoglycemia, adjust dosage for pt with decreased renal function. USE: may be suitable for pts with sulf allergy, more frequent pre-prandial dosing possible.
Term
Pioglitazone
 Definition
Thiazolidinediones. MOA: Peroxisome proliferator-activated receptor gamma agonist = increases insulin sentivity in target tissues, particularly adipocytes. TOX: weight gain and edema; congestive heart failure, bladder cancer. Contraindications: pregnancy, hepatic impairment, heart failure. Liver Function Tests periodically. USE T2DM
Term
Rosiglitazone
 Definition
Thiazolidinediones. MOA: Peroxisome proliferator-activated receptor gamma agonist = increases insulin sentivity in target tissues, particularly adipocytes. TOX: weight gain and edema; congestive heart failure; MI or stroke. Contraindications: pregnancy, hepatic impairment, heart failure. Liver Function Tests periodically. USE T2DM
Term
Activated Charcoal
 Definition
Non-specific antidote to ingested toxin. Non-specific chelator, limits drug absorption, not as efficacious if drug is rapidly absorbed.
Term
Polyethylene Glycol, PEG 3350
 Definition
Non-specific antidote to ingested toxin. Whole-bowel irrigation. Non-absorbale. In balanced electrolyte solution. Useful when the ingestion of a drug occurs that is poorly absorbed by activated charcol. i.e., Fr, Li.
Term
Calcium EDTA
 Definition
Given IV or IM for severe lead poisioning. Toxic to kidney at high dose. Chills, fever, nausea, vomiting.
Term
Succimer
 Definition
First orally effective metal metal chelator. More rapidly effective than EDTA for lead, also used for mercury or arsenic
Term
Organophosphatea
 Definition
Insecticide. All act as acetylcholine esterase inhibitors . S&S: headache. MOA: respiratory failure to diaphragm muscle paralysis. TX: atropine for both organophosphates and carbamates. For the non-carbamate organophosphates, pralidoxime (2-PAM) is given.
Term
Ethylene Glycol
 Definition
S&S: high affinity for Ca causing hypocalcemic tetany. When Ca is bound to oxalic acid the result is crystal formation. Renal injury occurs as these crystals pass through the renal tubules and eventually end up in the urine. TX: Fomepizole.
Term
Arsenic
 Definition
Metal toxin. SOURCE: rural/municipal water supplies. S&S: acute - hemorrhagic gastroenteritis (rice water diarrhea), chronic - hyperkeratosis, exfoliative dermatitis on palms and soles. MOA: high affinity for -SH groups = oxidative stress. TX: metal chelator Dimercaprol
Term
Lead
 Definition
Metal toxin. SOURCE: ingestion of paint chips and inhalation of dust, consuming contaminated food. S&S: hypochromic microcytic anemia, weak wrist or ankle extensor muscles, encephalopathy, colic. MOA: inhibits hemoglobin synthesis = anemia. TX: control source until levels are high, then metal chelator with succimer (1st line) or EDTA (2nd line). Dexamethasone can be given for cerebral edema.
Term
Methylmercury
 Definition
Metal toxin. Highly absorbed and readily passes blood brain barrier. SOURCE: consumption of contaminated fish and grain fungicide. S&S: cerebellar ataxia and movement disorders associated with cerebellar dysfunction, loss of balance, sensory deficits, loss of visual field, deafness, dysarthria. Women who are nursing or pregnant should avid predatory fish due to teratogenic effects. TX: metal chelators (EDTA) only used in pts with highly elevated metal levels or severe toxicity. Chelation therapy only reduced the readily accessible pool of metal. After chelator therapy ends, blood metal levels can rebound.
Term
Carbon Monoxide
 Definition
SOURCE: any burning or combustion process. S&S: headache. MOA: out competes oxygen binding to Hb, forms carboxyhemoglobin = reduction of oxygens ability to dissociate from Hb
Term
Cyanide
 Definition
SOURCE: smoke, industrial, warfare. S&S: headache, "bitter-almond breath." MOA: binds to cytochrome oxidase = inhibition of ETC and cell's ability to use oxygen in producing ATP. TX: 1-step
Term
Asbestos
 Definition
filamentous silica. SOURCE: old building materials. S&S: Mesothelioma lung cancer 15-20 yrs after exposure. Plural effustions 5-10 yrs after exposure. TX: no antidote.
Term
PCBs
 Definition
SOURCE: flame retardants, farm raised salmon. S&S: dermal acne-like eruptions called chloracne, nausea, headache, vomiting. Tx - none.
Term
Dioxin
 Definition
contaminant of agent orange. not intentionally produced. Tx - none
Term
Bisphenol A
 Definition
SOURCE: leaching from water bottles, plastic-lined canned food, polycarbonate plastic. S&S - unknown. MOA: unknown. TX - none.
Term
Fomepizole
 Definition
for Tx of ethylene glycol poisoning. Reduces toxic metabolite production because it out compete ethylene glycol at ADH enzyme.
Term
Etyinyl estradiol + levonorgestrel
 Definition
Monophasic Combination oral contraceptive
Term
Ethinyl estradiol +desogestrel
 Definition
Monophasic Combination oral contraceptive
Term
Plan B Kit
 Definition
one tablet of levonorgestrel 1.5mg emergency contraception. May delay ovulation and decrease endometrial recptivity. TOX: nausea and vomiting.
Term
Ethinyl estradiol
 Definition
estrogen component of combination oral contraceptive
Term
Levonorgestrel
 Definition
progestin component of combination oral contraceptive
Term
Norgestimate
 Definition
progestin component of combination oral contraceptive
Term
Norethindrone
 Definition
progestin component of combination oral contraceptive
Term
Menotropins
 Definition
GnRH. LH and FSH insolated from urine of post menopausal women; igiven IM to prevent hypersentivity. Women - used with hCG to tx infertile anovulatory. Men - used with hCH to stimulate spermatogenesis.
Term
Chorionic gonadotropin.
 Definition
used for prepubertal cryptochidism, ovulation induction and spermatogenesis. gonadotropin given IM
Term
Androgel
 Definition
USE: male - hypogonadism/ testosterone deficiency, male senescence / ANDRO-pause, athletics enhancement
Term
Finasteride
 Definition
anti-androgen.5aplha-reductase inhibitor USE: decrease porstate size in benign prostatic hyperplasia. act to inhibit conversion of testosterone to more active metabolite dihydrotestosterone. can also be used to tx male pattern baldness
Term
Oxytoxin
 Definition
Uterine acting Drug. USE: increase uterine contratctility - induce or augment labor, control postpartum uterine hemorrhage after delivery of the fetus
Term
PGE2- Dinoprostone
 Definition
Uterine acting Drug. cause cervical ripening by increasing the secretion of collagenase. Bind to receptorsin the myometrium and cause contraction of the uterus.
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