Pharmacology

Pharmacology

Immuno-modulating drugs
1. Cyclosporine
  1. Inhibs IL-2 production
    1. Binds cyclophilin
2. Tacrolimus
  1. Inhibits IL-2
    1. Binds FK12-BP
3. Sirolimus
  1. Inhibs mTOR (mammalian target of rapamycin
4. Azathioprine
  1. Inhibs DNA synth required for lymphocyte proliferation
5. Mycophenolate mofetil
  1. Inhibs DNA synth for lymphocyte proliferation
    1. Inhibs IMP dehydrogenase
6. Prednisone
  1. Inhibs cytokine gene expression
7. Basilixmab, Daclizumab
  1. Bind IL-2 receptor--> inhibits IL-2 binding
8. Belatacept
  1. Directed against CD80 glycoprotein on APC
    1. Inhibs costume of T cell lymphocytes
Anti-fungals
1. Amphotericin B
  1. Mech Axn: Binds ergosterol in membrane-->forms pores--> electrolytes and cell content leak
    1. Adverse Affects--> fevers, chills, & flu like rxn, renal toxicity: hydrate and give electrolytes, anemia, Shake n Bake
      1. Indications: Systemic mycoses--> Cryptococcus, Blastomyces, Coccidioides, Coccidioides, Histoplasma, Candida, & Mucor
2. Polyenes
  1. Nystatin
    1. Binds ergosterol: fungistatic or fungicidal
      1. Topical only-->adverse effects are too toxic for systemic use
        Indications: oral candidiasis, topical yeast infections--> vaginal candidiasis & intertrigo
  2. Flucytosine
    1. Converted by fungal enzyme cytosine deaminase to 5-fluorouracil-->inhibit NA synth
      1. Effects: Bone marrow suppression
        Indications: Systemic mycoses--> Cryptococcus
3. Azoles
  1. Mech: inhibs 14-alpha demethylase--> key in ergosterol synth in fungi. Fungistatic
    1. Effects: Anti-androgen effects via inhibiting testosterone synthesis, gynecomastia (ketoconazole), inhibs CYP450
      1. Indication: Mild Systemic mycoses
        Fluconazole: Chronic suppression of Cryptococcus in immunosuppressed pts
        Itraconazole: Blastomyces, Coccidioides, Histoplasma
        Voriconazole: Aspergillus & Candida
        Isavuconazole: Aspergillus & Mucor
4. Allylamine: Terbinafine
  1. Inhibs squalene epoxidate-->lanosterol synthesis & Fungicidal
    1. Effects: GIT upset, Hepatotoxicity, taste disturbance
      1. Indications: widespread dermatophyte infections & Onychomycosis
5. Griseofulvin
  1. Mech: inhibits mitosis--> microtubule dysfunction, especially targets keratin containing tissues; nails, & Fungistatic
    1. Effects: Teratogenic, Disulfiram-like rxn, Neuro: confusion and HA, & induces CYP450
      1. Indication: Superficial infections & dermatophytes
6. Echinocandins
  1. Mech: inhibs cell wall synth-->inhibs beta gluten synth, fungistatic or fungicidal
    1. Effects: Flushing-->histamine
      1. Indications: Aspergillosis and Candida
Antivirals
1. Acyclovir, Famciclovir, Valacyclovir
  1. Mech: Guanosine analogs-->inhibs viral DNA poly
    1. Indication in HSV/VZV
      1. Effects: Obstructive crystalline nephropathy-->acute renal failure, hydrate pt can prevent
2. Ganciclovir and Valganciclovir
  1. Mech: Guanosine analog-->inhibits viral DNA poly
    1. Indication: CMV
      1. Effects: Bone Marrow Suppression
3. Foscarnet
  1. Mech: Inhibs viral DNA & RNA poly
    1. Indication: Ganciclovir resistant CMV
      1. Effects: Renal toxicity & electrolyte abnormalities
4. Cidofovir
  1. Mech: Inhibs DNA poly inhibits; uses host enzymes
    1. Indications: CMV retinitis, Acyclovir resistant HSV
      1. Effects: Renal toxicity. Coadmin with probenecid and hydrate
Antibiotics
1. Beta lactams
  1. Penicillins
    1. Penicillin G
      1. Mech: Inhibits bacterial cell wall synth-->bind and inhibits transpeptidases
        Indication: Strep, meningococcal, neurosyphili
        Effects: Immediate hypersensitivity, rash, and seizures
  2. Aminopenicillins
    1. Ampicillin and Amoxicillin
      1. G - coverage
  3. Penicillinase-resistant penicillins
    1. Methicillin, Nafcillin, Oxacillin, Cloxaccillin, Dicloxacillin
      1. Stability to staphylococcal beta lactamase
  4. Anti-pseudomonal penicillins
    1. Carbenicillin, Ticarcillin, piperacillin
      1. G- bacteria: P. aeruginosa, anaerobic bacteria
  5. Cephalosporins
    1. 1st gen: Cefazolin, Cephalexin (Keflex)
      1. G+
    2. 2nd gen: Cefoxitin, cefaclor, cefuroxime
      1. G+ some G-, anaerobes
    3. 3rd gen: Cefixime, Ceftriaxone, Cefotaxime, Ceftazidime
      1. Serious G- infections, Meningitis, Pseudomonas
    4. 4th gen: Cefepime
      1. Expanded coverage G+ and G- (Pseudomonas)
    5. 5th gen: Ceftaroline
      1. Broad spectrum against G+ & MRSA
        Effects: Hypersensitivity reactions, nephritis, granulocytopenia, and hemolytic anemia
        Local-->pain after IM & thrombophlebitis after IV
        Hypoprothrominemia (give K+) and bleeding (cefoperazone & cefotetan
        Disulfiram like reaction: Cefoperazone, cefotetan
  6. Beta-lactamase inhibitors: Clavulanic acid, Sulbactam, Tazobactam and Avibactam
  7. Monobactams
    1. Aztreoname
      1. Indication: pts with immediate hypersensitivity to penicillins
        Effects: No cross allergic reaction with penicillins
    2. Carbapenems
      1. Imipenem-cilastatin, Meropenem, Doripenem, Ertapenem
        Indication: G- rods, P. aeruginosa, G+ organisms, and anaerobes
        Toxicity: Seizures especially in renal failure or with high doses
    3. Glycopeptide
      1. Vancomycin
        Inhibs cell wall synthesis-->bind D-Ala D-Ala of peptidoglycan
        Resistance turns into D-Ala D-Lac
        Indication: Sepsis, endocarditis, meningitis and C. diff
        Toxcity: Red man Syndrome
    4. Daptomycin
      1. Mech: Binds cell membrane-->depolarize and rapid cell death, increase K+
        Indication G+ bacteria; sepsis and endocarditis
        Effects: Myopathy, increase CK
2. Aminoglycosides
  1. Gentamicin, Amikacin, Neomycin, Streptomycin, Tobramycin
    1. Mech: Inhibits 30S-->initiation, misreading mRNA, breakup polysomes into nonfunctional monosomes
      1. Indication: bactericidal, synergistic against G+ w/ beta lactam or vanco, [dependent] killing, post-antibio effect
        Effects: Nephrotoxicity (revers), ototoxicity (irrevers), neuromuscular blockade
3. Tetracyclines
  1. Tetracycline, Doxy (safe CKD), Mino, Erava, Sare, Omada, methe, tige(safe CKD)
    1. Mech: Bacteriostatic, passive diffusion, blocks 30S, block aminoacyl-tRNA to acceptor site on mRNA; no add of aa to growing peptide
      1. Indication: G+, G-, mycoplasma, Chlamydiae, Rickettsiae
        Effects: divalent cations inhibits oral absorption, GIT upset, hepatotoxicity, photosensitivity, deposition in bone and teeth
4. Macrolides
  1. Erythromycin, azithromycin, clarithromycin
    1. Mech: binds 50S by peptidyltransferase center-->inhibs elongation-->blocks E site
      1. Indication: Bacteriostatic, Mycoplasma pneumonia, pertussis, Corynebacterium, Chlamydia
        Effect: CYP 450 inhibitor, GIT upset, QT prolongation
5. Protein Synthesis Inhibitors
  1. Clindamycin
    1. Mech: inhibits 50S
      1. Indication: Bacteriostatic against susceptible bacteria, anaerobe infections
        Effects: C. difficile colitis
  2. Quinupristin-dalfopristin
    1. Mech: inhibits 50S
      1. Indication: Bactericidal, Staph, and Vance resistant strains of E. faecium
        Effects: Infusion related myalgias and arthralgia
  3. Chloramphenicol
    1. Mech: Inhibs 50S
      1. Effect: Dose related anemia, idiosyncratic aplastic anemia, gray baby syndrome
  4. Linezolid
    1. Mech: Inhibs 23S from binding to 50S
      1. Indication: MRSA, VRE
        Effect: Duration dependent bone marrow suppression, neuropathy, and optic neuritis, 5-HT syndrome when admin w/ other serotonergic drugs (SSRIs)
6. Sulfonamides
  1. Sulfamethoxazole, Cotrimoxazole (TMZ-SMP), sulfadiazine, sulfadoxine, sulfacetamide
    1. TMZ-SMZ (Bactrim)
      1. Mech: inhibits folate synthesis and DHFR
        Indication: P. jiroveci, Toxoplasma gondii
        Effects: rash, fever, bone marrow suppression, hemolytic anemia in G6PD deficiency, Stevens Johnson Syndorme, toxic epidermic necrolysis (TEN), kernicterus in newborns-->increased bilirubin leads to encephalopathy
        Like to be basic
7. 1. Fluoroquinolones
    1. Norfloxacin (G-), G+ & G- : Cipro, Oslo, Levi, Gemi, and G+: Moxi
      1. Mech: Inhibs DNA replication-->binds DNA gyros (topo II) and topoisomerase IV
        Indication: G= and G+
        Effects: neurotoxicity, tendonitis
        Not advised in <18 y/o d/t damage growing cartilage and cause arthropathy, be careful of giving to patients with use of corticosteroids, and do NOT give with antacids

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	Criado por Samantha Bailey mais de 2 anos atrás