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Pharm atbx

Pharm 3

-Generalized tonic-clonic seizures and partial seizures. -low toxicity and low cost -metabolized by the hepatic microsomal system, MOA: (sedation) GABAA receptors. (Anticonvulsant): Ca++ channel inhibition /decreases excitatory transmitter release. Phenobarbital
- Generalized Tonic-clonic and partial seizures. -efficacy is due both to drug and active metabolites (Phenobarbital). -two active metabolites, phenobarbital and phenylethylmalonamide (PEMA) Primidone (Mysoline)
- Generalized tonic-clonic, simple, and complex-partial seizures. - trigeminal (tic douloureux) , glossopharyngeal neuralgias and manic-depressive affective disorder( resistant to lithium) pain associated with multiple sclerosis -Hepatic metabolism Carbamazepine (Tegretol)
-epilepsy, mood disorders, anxiety -analog of carbamazepine - active metabolite (10-hydroxycarbazepine) that is equipotent to carbamazepine - fewer SE’s that carbamazepine - hyponatremia -anticholinergic activity - synergistically with nmb Oxcarbazepine (Trileptal)
-central agent in treating absence seizures. - More effective in managing absence seizures than trimethadione SE : euphoria, anemia Bone marrow depression, Stevens-Johnson syndrome -Tegretol decreases levels. - Isoniazid increases levels. Ethosuximide (Zarontin)
-alone or in combination to treat partial and generalized seizures, bipolar disorder and depression - sodium channel antagonist and high voltage dependent Ca++ channels -decrease the release of aspartate and glutamate -met. by liver -hep enzyme induc Lamotrigine (Lamictal)
-used to treat partial sz in adults and neuropathic pain -mono- or adjunctive therapy -bind to synaptic vesicles decreasing release of NT -SE h/a, anxiety, CNS depression ,initial sedation, depression , hallucinations -no liver met or protein binding Levetiracetam (Keppra)
DOC for status epilepticus also used for status epilepticus, other sz - interaction with GABAA ionophore to increase the duration of GABA binding and -increase chloride flux leading to hyperpolarization - low toxicity - used as anesthesia adjuvant Benzodiazepines Diazepam (Valium) Lorazepam (Ativan)
-May also be used in combination with other drugs to tx: akinetic sz, absence sz refractory to succinimides or valproic acid (Depakene), infantile spasms -MOA: benzo-mediated enhancement of GABA-induced ^ in Cl- conductance (hyperpolarization). Clonazepam (Klonopin)
- Partial and tonic-clonic sz but NOT absence sz - widely used - Hep microsomal system. SE: status epilepticus the most apparent toxic sign is cardiac arrhythmia cerebellar and vestibular disturbances, hirsuitism -Etoh decreases efficacy. Phenytoin (Dilantin)
-a Phenytoin prodrug used by injection for status epilepticus (5 day max use, only if Phenytoin not usable) -more water soluble and metabolized to formic acid Fosphenytoin (Generic)
- Partial, generalized seizures and absence seizures -extensively protein bound and conjugated - MOA d/t ^^ recovery time of voltage activated Na+ channels. -Can cause serum phenobarbital to increase by 40%. Valproic Acid (Depakene)
-adjunct for partial and generalized seizures, obesity, migraines and Parkinson’s disease -acts at GABAA receptor to enhance GABA binding - blocks voltage-gated T-type calcium channels -metabolism can be inhibited by ketoconazole, carbamazepine(Tegreto Zonisamide (Zonegran)
-adjunct for partial sz, anxiety disorders (panic attacks), and neuropathic pain - inhibits GABA neuronal reuptake -^^ duration of GABA interaction at receptor zone - ^^ neuronal inhibition -use may actually trigger sz in non-epileptics Tiagabine (Gabitril)
-tx partial, generalized, absence sz, bulimia, migraine h/a, tremors -structurally a monosaccharide r/t fructose - inhibit voltage gated Na and Ca channels - enhances GABA Cl ion flux -inhibits glutamate induced neuronal excitation - SE kidney ston Topamax
-no longer the clinical agent of choice for absence seizure due to toxicity. MOA: Similar to ethosuximide (Zarontin) -inhibits T-type Ca++ currents. -metabolite Dimethadione. Trimethadione (Tridione)
-Structural analog of GABA -chronic pain therapy -MOA: increase GABA synthesis, -increase interaction with GABA receptors -decrease GABA reuptake rate -1/2 life 6 hours No plasma protein binding Gabapentin (Neurontin)
• Cross links DNA (cant divide). • DLT is bone marrow dep • Uses: Hodgkin’s lymphomas, leukemias, lung breas, ovarian ca, burkitt’s lymphoma • agent for kids w/ neuroplastomas/ Retinoblastomas • used in combo w/ methorexate + 5-fluorouracil for breast Alkylating Agent: Cyclosphoshamide (cytoxan)
• MOA: DNA crosslink • Uses: CML and polycythemi vera • DLT; Bone marrow dep. • SE: alopecia, lung fibrosis, impotence • causes myelosupression (granulocytes > plts, erythrocytes >pancytopenia • no cytotoxicity to lymphoid tissue or GI epilthelium Alkylating agent: Busulfan (myleran)
• Inhibit topisomerase II • Bind to DNA to inhibit DNA/RNA synthesis • O2 radical production • DLT for doxorubin and saunorubicin is CM (d/t O2 radicals) • Bone marrow dep in 2 weeks, recovery in 4 weeks. More severe w/ dexrazoxane Antibiotic anticancer agents: Anthracyclines Doxorubicin, Daunorubicin, and others)
• Uses: soft tissue osteogenic an other sarcomas; lungs, bladder, ovarian, thyroid cancers; Hodgkin, lymphoma, acute leukemia • If given to rapidly IV, erythematous streaking along proximal veins • Chelates iron and other metals Doxorubicin (adriamycin)
• uses: acute leukemias, some solid tumors in children. • Daunoxome approven 1st line therapy for advance Karposi sarcoma Daunorubicin (Daunomycin)
Cu-chelating glycopeptides, isolated from streptomyces • MOA: breaks DNA strands >Free radicals • DLT: Pulmonary fibrosis • Uses: testicular tumors, skin cancers, lung, Kaposi’s sarc. lymphoma, Hodgkins • SE: N/V fever, skin toxicity, anaphylactic rx *Bleomycin Antibiotic anti cancer agent
anaolog of folic acid. • Uses ALL in kids, carc. of breast, head, neck, gastric, bladders. used in high doses for osteogenic sarcomas along w/ "rescue” of host toxicity by leucovorin (folinic acid, citrovorum fx). • DLT is mucositis. • TERATOGENIC Anti metabolic anti cancer agent: *Methotrexate;
Analog of uraciil w/ flourine @ 5-position • cells can be “rescue from high doses by giving uridine • Methotrexate ^^ activity • Use stomach, colon, bladder, prostate, breast, and ovarian ca, • Warning of ^ dose= anorexia, nausea, > stomatitis & diar *5-Fluorouracil
• Isolated from the periwinkle plant. • MOA; spindle poisons, causes mitotic arrest at metaphase. • May need allopurinol to prevent hyperuricemia • Fatal if given intrathecally Natural product anticancer Agents: *Vincristine (oncovin)t1/2=85hr Vinblastine (Velban)t1/2=25hr
from the Pacific and European Yew Tree (Bark fungus) • MOA mitotic spindle poison. • Uses; breast head, lung ca, Kaposi sarcoma & restinosis (taxus). • Docetaxel & Carbazitaxel for prostate ca • SE: N/V alopecia, neutropenia, anemia, thrombocytopenia Natural product anticancer Agents: Paclitaxel, Docetaxel (Taxotere), CArbazitaxel (Jevtana)
MOA: after hydrolysis, loses Cl & forms platinum species that reacts w/ DNA & protein to from cross link. Use testicular tumors, ca. of bladder, neck, cervical, lung, esophagus, neuro & retinoblastomas SE: n/V, ototox neurotox, anaphylaxis DLT-nephrot Natural product anticancer Agents: Cisplatin (Platinol)
• Less nephrotoxic than cisplatin • 2nd generation compound • Uses: ovarian, head, neck and lung ca • DLT: bone marrow depression • Longer half life than cisplatin Carboplatin.
• Ethyl or Isopropyl • Iso more effective than Ethyl • Antiseptic and disinfectant • Bactericidal • Repeated wiping increases efficacy • Ineffective against fungal or viral organisms . Alcohol
• Benzalkonium and Cetylpyridinium • Effective against most bacteria, fungal and viruses. NOT mycobacterium tuberculosis • Mixed with alcohol to increase efficacy • Alters cell permeability • Also used as preservatives and to sterilize surgical equip. Quatenery ammonia compounds
Effective against bacterial, viral, and fungus • Toxicity fairly low, but caution in allergic pts. • Use as a skin antiseptic, but must be applied for 1-2 mins to assure good action • Causes skin staining, beneficial notification of application . Iodine
• Combination of an organic molecule carrier with iodine • Povidine-iodine most common agent • Free iodine concentration is low enough that little staining is observed • Not as effective as iodine • Used in handsoaps and surgical swabs Iodophors
• No longer used d/t easy absorption and severe dermatological, neurological, and possible teratogenic effects • Neonates especially susceptible • Handwash effective against gram+ bugs • Sticks to skin providing continued action • Presscript only for Hexachlorophene (pHisoHex)
• Used as a caustic astringent and antiseptic • Bactericidal, and often used in eyes of newborns of mothers with gonococcal infections • Used on burns and other wounds Silver Nitrate
• Mercurochrome & Merthiolate (Thiomersal) • Not used much now. Thiomersal used as preservative in a few vaccines • Poor efficacy • Allergic reactions and poisoning (oral) Mercurous compounds
1. Alcohol 2. Quatenery ammonia compounds 3. Iodine 4. Iodophors 5. Chlorahexidine (Hibiclens) 6. Hexachlorophene 7. Silver Nitrate 8. Mercurous compounds Antiseptic
• Effective against bacterial, viral, and fungal organisms • Glutaraldehyde more effective than formaldehyde • Requires several hours exposure for maximum effectiveness • Acts by precipitating proteins in the organism • Reacts with any proteins, Aldehydes
• Bactericidal against most organisms including Mycobacterium tuberculosis • A phenol derivative, it causes burns to skin, therefore is only used as a disinfective Cresol
• Used in Gas sterilization • Requires a treatment chamber to hold instruments for the several hour contact period required • Air-out plastic components sterilized by this method to allow ethylene oxide to out-gas from materila Ethylene Oxide
Alcohol Aldehydes Cresol Chlorine Ethylene oxide Heat Disinfectants
Bind to 30S subunit of bacterial ribosome & inhibit PRO synthesis by blocking the binding of aminoacyl tRNA to acceptor site (A) on the mRNA-ribosome complexà AA can’t be added to the growing peptide Tetracyclines
Irreversible inhibitors of PRO synthesis that bind to receptor PRO on 30S subunit à misreading of mRNA message -Gentamicin, Tobramycin, Amikacin, Streptomycin, Neomycin (Combined with polymixin as Neosporin), Kanamycin Aminoglycosides
Inhibits PRO synthesis & binds to the 30S subunit (doesn’t à misreading like AG’s do) Spectinomycin (Trobicin)
PRO synthesis inhibitor that reversibly binds to site on 50S subunit & inhibits translocation step where peptidyl tRNA moves from A site on the ribosome to P site & reversibly blocks PRO synthesis. Macrolides - erythromycin (E-mycin), clarithromycin (Biaxin), azithromycin Zithromax)
binds reversibly to 50S subunit of bacterial ribosomes & inhibits PRO synthesis (like macrolides) -lincomycin (Lincocin),clindamycin (Cleocin) Lincosamides: -lincomycin (Lincocin),clindamycin (Cleocin)
PRO synthesis inhibitor by reversibly binding to 50S subunit of bacterial ribosomes & inhibits transpeptidation by inhibiting peptidyl transferase. It prevents binding of AA end of aminoacyl tRNA to the acceptor site on 50S subunit. Chloramphenicol
Inhibits PRO synthesis by binding to bacterial 23S ribosomal RNA of the 50S subunit thus px formation of a functional 70S initiation complex, an essential step (unique MOA & doesn’t show cross resistance to other antibx) Oxazolidione (Linezolid)
Bind to 23S RNA of the 50S subunit (like macrolides); do not induce the methylase enzyme (so not subject to MLS resistance?) Streptogramins
Same as other B-lactam antibx: Disrupts synthesis of peptidoglycan layer of bacterial cell wall. Inhibits final stage of cell wall synthesis that involves peptide crosslinking by transpeptidases; structural analog of d-ala d-ala Penicillins
Parenterals: methicillin and Nafcillin, Oral: Isoxazolyls Penicillinase-Resistant Penicillins
Carboxypenicillins (ticarcillin disodium(Timentin – with clavulanic acid) , Ureidopenicillins (piperacillin) Antipseudomonal
Same as other B-lactam antibx: Disrupts synthesis of peptidoglycan layer of bacterial cell wall. Includes 1st, 2nd, 3rd, and 4th generations Cephalosporins
Oral:Cephalexin (Keflex),Cefadroxil Parenteral: Cefazolin (Ancef, Kefzol) 1st gen. Cephalosporins
Oral:Cefaclor (Ceclor, Raniclor),Cefuroxime axetil (Ceftin),Cefprozil Parenteral:Cefoxitin (Mefoxin) Cefuroxime sodium (Zinacef) Cefotetan (contains N-methylthiotetrazole group) 2nd gen. Cephalosporins
Oral: Cefixime (Suprax) Cefpodoxime proxetil Ceftibuten (Cedax) Parenteral: Cefotaxime (Claforan) Ceftriaxone (Rocephin) Ceftazidime (Fortaz) 3rd gen. Cephalosporins
Cefepime (Maxipime) 4th. Gen. Cephalosporins
Inhibition of cell wall synthesis -Imipenem (available with cilastatin as Primaxin), Meropenem (Merrem), Doripenem (Doribax), Ertapenem (Invanz) Carbapenems
Same as other B-lactam antibx: Disrupts synthesis of peptidoglycan layer of bacterial cell wall. Begins with Mono. Monobactam
Inhibits cell wall synthesis (peptidoglycan synthesis) by irreversibly binding to the pair of d-ala molecules of cell wall precursor units Vancomycin
Inhbits cell wall synthesis by binding to a precursor of cell wall& forming unusable complex; acts 1 step before the one inhibited by vancomycin Bacitracin
Inhibits early stage of cell wall synthesis; inhibits enolpyruvyl transferase & irreversibly blocks condensation of UDP-N-actely glucosamine w/p-enolpyruvate; inhibits bacterial adherence to uroepithelial cells Fosfomycin Tromethamine (Monurol)
PABA analog that competitively inhibits DHPS which is required for folic acid synthesis; it only affects bacteria that synthesize own folic acid Sulfonamides (Sulfamethoxazole, Sulfisoxazole, Sulfadiazine,Sulfacetamide, Sulfamylon, Silvadene Trimethoprim-Sulfamethoxazole (Bactrim, Septra)
Nitro group activated by intracellular electron transport PRO in anaerobic organism to chemically reactivate intermediates that react with DNA & can> ↑ degradation of existing DNA, altered DNA helical structure, ↑ strand breaks, & inhibition of DNA syn. Metronidazole (Flagyl)
anoxic or hypoxic condition is required for formation of cytotoxic metabolites) Metronidazole (Flagyl)
Surface active agents that disrupt osmotic properties and transport mechanisms of cell membranes in gram – bacteria only; also binds & inactivates endotoxins Polymixins
Reversibly binds to bacterial isoleucyl-tRNA synthase & blocks PRO synthesis Mupirocin (Bactroban)
Inhibits DNA gyrase which is a topoisomerase responsible for breaking & rejoining DNA strands necessary for DNA replication -ciprofloxacin ophthalmic (CILOXAN), ofloxacin , etc Fluoroquinolones ciprofloxacin (CIPRO) ophthalmic (CILOXAN), ofloxacin ophthalmic (OCUFLOX), norfloxacin (NOROXIN),lomefloxacin, Levofloxacin (LEVAQUIN), Gatifloxacin (Zymar - ophthalmic), Moxifloxacin (Avelox)
Similar to the Macrolides, keto group a 3 position instead of a hydroxyl group and removal of a sugar group, binds to the 50s bacterial ribosomal subunit -Telithromycin (Ketek) (oral tablets) Ketolides
Hydrolyzed in acidic urine to formaldehyde and ammonia, Formaldehyde is bactericidal in urine ph < 5.5, Used for chronic lower UTIs. Activity is higher in acid urine, Primarily used to px UTIs and to px bacteriuria after prostatectomy, urinary analgesic Urinary tract Antiseptics: Methenamine (Hiprex), Nitrofurantoin (Furadantin), Hemolytic anemia (if G6PD-deficient)
Not DOC for anything (alone) Sulfa
DOC for prevention of burn infections Silver Sulfadiazine
DOC for empiric treatment of acute UTI, Nocardia, moraxella catarrhalis, H. flu, Yersinia enterocolitica Trimethoprim + sulfamethoxazole (Bactrim, Septra) 5:1 SMZ:TMPà [blood] ratio of 20:1
Listeria monocytogenes Ampicillin
Proteus mirabilis, Eikenella corrodens AminoPCN (ampicillin, amoxicillin)
1 of DOC for pseudomonas aeruginosa Ticarcillin + aminoglycoside
DOC for syphilis PCN
Antbx for Rheumatic recurrence Use Pen V or benzathine Pen G
DOC Endocarditis prevention if valvular disease undergoing dental/surgical procedures PO DOC= amoxicillin 1 hour before procedure Parenteral DOC= ampicillin 30 min before procedure
Typhoid fever DOC ceftriaxone
Gonorrhea DOC Ceftriaxone or cefixime
DOC for enterobacteriaceae (E. coli, Klebsiella, Proteus, Providencia stuartii, Serratia 3rd gen. Cephalosporins
Drug used for H. flu meningitis Ceftriaxone or cefotaxime
Drugs used for Surgical Prophylaxis Cefazolin- ‘clean’ surgery Cefoxitin or cefotetan- colorectal surgery, appendectomy, hysterectomy, or ‘dirty’ surgery
DOC for Enterobacter, Citrobacter freundi, Acinetobacter, C. fetus Imipenem
Reserved for very serious gram- infections resistant to less expensive drugs Azactam
DOC for mycoplasma pneumo (or a TCN), legionella pneumophila (+ rifampin), bordetella pertussis, corynebacterium diptheriae, campylobacter jejuni (if fluoroquino are c/i) DOC valvular heart disease undergoing dental/surgical procedures & allergic to PCN Macrolides
DOC for helicobacter pylori (TCN+ flagyl+ bismuth subsalicylate). Also useful for rickettsial, mycoplasmal, spirochetal, chlamydial. tetracyclines
DOC for UTI due to pseudomonas aeruginosa ciprofloxacin (fluoroquinolone)
DOC for campylobacter jejuni, shigella, salmonella, Fluoroquinolones
DOC for rickettsial disease (Rocky Mountain spotted fever) if unable to take TCN (↓ renal fxn, pregnant, peds), glanders (w/streptomycin), N. Meningitis & H. influenzae meningitis if PCN allergic Chloramphenicol
DOC w/TCN for glanders (pseudomonas mallei) Streptomycin
Used to tx vancomycin resistant enterococcus faecium, community acquired pneumonia d/t staph aureus, streptococcus penumoniae, & skin infections (even those d/t MRSA) Zyvox
DOC for MRSA Vancomycin
DOC for giardiasis (anaerobic protozoa); DOC for C. difficile & H. pylori (PO form only); DOC for gardnerella vaginalis Flagyl
Bacteriocidal antibiotics PCN, cephalosporins, carbapenems, fluoroquinolones, flagyl, monobactam, aminoglycosides, fosfomycin
Bacteriostatic sulfamides, macrolides, lincosamides, tetracyclines, chloramphenicol, Zyvox, Vancomycin, spectinomycin
SE: -metallic taste & neurotoxicity (neuropathies, dizziness, convulsions, vertigo)à c/I in active CNS disease -disulfram like rxn with ETOH -Reddish brown urine, reversible neutropenia -may potentiate warfarin; may potentiate lithium toxicity Flagyl
SE: -rapid infusion à ‘red neck’ syndrome = flushing over upper chest, urticarial rash, tachycardia, hypotension d/t histamine release -ototoxicity & nephrotoxicity- especially if renal impairment Vancomycin
-it’s a weak MAOI (avoid tyramine rich foodsà HTN crisis) Zyvox
-all s/e are dose-dependent except hypersensitivity (which is rare) -ototoxicity (its irreversible b/c sensory hair cells do not regenerate) ​*auditory toxicity: can lead to deafness ​*vestibular toxicity: h/a, n/v, vertigo, ataxia aminoglycosides
SE: -nephrotoxicity: ↑BUN & Crt; its reversible since proximal tubular cells can regenerate ​Drug: dose or duration (streptomycin least nephrotoxic, gentamicin most nephrotoxic) ​Patient: age extremes, & critically ill pts Aminoglycosides
-Neuromuscular blockade: inhibits presynaptic Ach release @ NMJ & ↓ postsynaptic receptor sensitivity; characterized as respiratory depression; patients with myasthenia gravis or hypocalcemia > susceptible; potentiation w/NMBD Aminoglycosides
SE: -Most adverse effects d/t inhibitory effect on PRO synthesis in mitochondria -Bone marrow disturbances ​*toxic erythroid bone marrow depression- (dose related) usually have complete recovery after d/c’d Chloramphenicol
SE: ​aplastic anemia- (not dose related) irreversible & fatal -Gray Baby Syn.- 40% fatality; turns skin ash gray - use w/caution in babies & limit dose -irreversible inhibition of liver microsomal P450 enzymes > ↑t1/2 warafin, phenytoin, etc. Chloramphenicol ​
-rare & infrequent s/e -cartilage deterioration (arthropathy) in young animals so c/I in kids < 18y/o or during pregnancy or nursing -Ofloxacin (Floxin) may potentiate anticoagulant activity of warfarin fluoroquinolones
-GI effects (take with food and a full glass of H2O) -superinfections much more common d/t broad spectrum -Hepatotoxicity (especially if pregnant- so c/I during pregnancy) -Renal toxicity (r/t TCN used, dose, duration, & extent of renal damage before u tetracyclines
-binds to Ca2+ deposits in new forming bone & teeth à permanent brown discoloration of teeth in kids <8y/o & depression of bone growth (so c/i in pregnancy and peds) -Vestibular toxicity with minocycline (abates after d/c’d) tetracyclines
-Benign intracranial HTN in adults (pseudotumore cerebri) manifested as H/A, blurred vision, bulging fontanels -Can ↓ prothrombin activity (so may need to decrease dose of anticoagulants) -↓ effectiveness of oral contraceptives tetraclyclines
-High incidence of diarrhea & pseudomembranous colitis not r/t dose or route (caused by necrotizing endotoxin) lincosamides
-Inhibits cytochrome P450 enzymes>↑ effects of drugs such as anticoagulants, carbamazepine, cyclosporine, ergotamine, triazolam, lovastatin, theophylline -Cholestatic jaundice in adults may be d/t hypersensitivity to estolate ester (dont use if pregnant macrolides
-high doses> transient reversible hearing impairment -rare reports of ventricular arrhythmias in patients w/ prolonged QT interval macrolides
T or F. The Monobactam, Azactam is ok to use if PCN allergic; can >gram+ superinfections True
T or F. -If PCN allergic, consider also allergic to imipenem Can cause seizures: especially if elderly, predisposed to seizures, or high doses with renal impairment (meropenem least likely) True
-Cefotetan & Cefoperazone: contain N-methylthiotetrazole group that can be cleaved & inhibit Vit K metabolism & aldehyde dehydrogenase > hypoprothrombinemia, bleeding disorders, & disulfiram-like rxn Cephalosporins
-Pseudomembranous colitis & superinfections (especially with 3rd generation); candidiasis is common Cephalosporins
-CarboxyPCN: high Na+ content > CHF -Carbenicillin: abnormal platelet aggregation & bleeding -Intrathecal PCN: epileptogenic (never give IT) PCN
-Toxic concentrations of all PCN possible if patient renally impaired > seizures -Ampicillin rash: not a hypersensitivity rxn -Jarisch-Herxheimer rxn: if used in patients with secondary syphilis PCN
-may be antagonized by LA with are esters of PABA (procaine) -toxic epidermal necrolysis & Stevens-Johnson syndrome if hypersensitivity rxn occurs Sulfa
SE: -hepatic necrosis -blood dyscrasias (agranulocytosis, aplastic anemia, hemolytic anemia) -Mafenide: metabolic acidosis d/t inhibition of carbonic anhydrase -Bactrim or Septra: CNS toxicity in AIDS patients sulfa
Created by: Bvaleris