PCOL Reviewer

November 20, 2017 | Author: Paul Michael Joules Salise | Category: Enzyme Inhibitor, Virus, Chemotherapy, Biosynthesis, Immune System
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AIDS Influenza A Herpes -Antimetabolite DOC for respiratory syncytial virus in young children -SARS -Lassa fever, Hantavirus, Hepa C( chronic cases) Cytomegalovirus(retinitis) Acyclovir-resistant VZ & HS Cytomegalovirus Hepa A&C herpes 8, papilloma v, Kaposi sarcoma, hairy cell leukemia chronic myclogenous anemia Hepa B (chronic cases) HIV T1 Herpes 1 and 2, VZ, ImmCmp w/ HSV keratitis Systemic amebiasis Luminal and systemic amebiasis Luminal amebiasis Trematodes(flukes) & Cestodes(flat and tape) Clonorchiasis(liver fluke), Paragonimiasis(lung fluke), Schistosomiasis Roundworms(ascariasis) Lymphatic filariasis Cutaneous filariasis River blindness & strongyloidiasis Trichuriasis( whipworm) Enterobiasis(pinworm) Hookworm Strongyloidiasis Systemic Mycoses Candida albicans Dermatophytoses & onychomycoses(nail) Subcutaneous and systemic mycoses Aspergillus and candida species Topical mycoses Topical & Systemic mycoses Systemic mycoses Alkylating a(Cancer)

2 transciptase inhibitors + 1 protease Amantadine, Oseltamivir, Rimantidine Acyclovir, penciclovir, valacyclovir, Zanamivir Ribavirin

Foscarnet Ganiclovir Interferon-a Lamivudine Vidarabin Chloroquine, dehdroxyemetine & emetine Metronidazole, tinidazole Paronomycin, iodoquinol Praziquantel (DOC)

Mebendazole (DOC), Pyrantel Diethylcarbamazine + Albendazole Ivermectin Mebendazole Mebendazole or Pyrantel pamoate Mebendazole or Pyrantel pamoate Ivermectin or Thiabendazole Amphotericin B (DOC) Nystatin, Micafungin & Anidulafungin (both IV) Terbinafine (DOC) Echinomandins Caspofungin (IV) Imidazoles(cotrimazole, econazole) Imidazoles(ketoconazole, miconazole) Triazoles( fluconazole, itraconazole;dec ADR) Cyclophosphamide (most commonly used)

Slow growing tumors Tumor therapy Acute leukemia Hodgkin’s and non-Hodgkin’s lymphoma Breast Cancer Metastatic breast cancer Breast Cancer in postmenopausal women

Metastatic hormone responsive breast and endometrial neoplasms Competitive antagonist for prostate cancer Granulocyte colony-stimulating factor (to recover neutrophils Granulocyte-stimulating factor(bone marrow repopulation after chemo, radiation, and bone marrow transplantation) Lymphatic & solid cancer For infertility Postmenopausal osteoporosis For testicular deficiency Stimulate linear bone growth & Rx anemia For erectile dysfunction Stimulate hair growth; BPH For allergic rhinitis, motion sickness, sleep COPD Oral & chronic asthma Prophylactic treatment for asthma Duodenal & Gastric ulcers cause by H. Pylori Histamine induced acid release NSAID-induced ulceration Severe Chron’s disease (refractory to other meds) X transplant rejection, specifically T cells DOC

Adverse Effects

Fluorouracil(5-FU) Dactinomycin (first antibiotic) Daunorubicin & idarubicin Prednisone (potent synthetic antiinflammatory corticosteroid) Tamoxifen and toremifene; Aminoglutethimide Anastrozole and letrozole (nonsteroidal imidazoles) Firstline(other countries) Tamoxifen (first-line in US) Megestrol acetate (progestins) Flutamide, nilutamide, bicalutamide Filgrastim Salgramostin

Cisplatin (first member) Clomiphene Raloxifene Testosterone Danazol Sildenafil Finasteride H1 antagonist Cholinergic antagonist Leukotriene modifiers Cromolyn sodium Pepto-Bismol & H2 blockers H2 blockers(-TIDINE) Misoprostol Infliximab Cyclosporine

Metronidazole Amphotericin B Caspofungin Mica & Anidulafungin Streptozocin Alkylating agents Anthracyclines Bleomycin Cisplatin Estradiol, estrone & estriol Diethylstilbestrol Mifepristone Progestins Sucralfate Orlistat Cyclosporine

N,v,d; dark urine or red-brown, metallic taste, disulfiram-like reaction if taken w/ alcohol Nephrotoxicity Flushing AE due to release of histamine(X cylcosporine) Diabetogenic; toxic to Beta cells of Is of Langerhans(insulinomas) Cytotoxic, mutagenic, carcinogenic lead to secondary malignancies Cardiac toxicity Fatal pulmonary fibrosis Severe toxicity(renal) N&V Cervical and vaginal cancer in daughters Abortifacient Weight gain, edema, depression Constipation Causes flatulence, oily spotting & fecal urgency Nephrotoxicity

Other information Mechanism of Action Reverse Transcriptase Inhibitor

Protease Inhibitor Acyclovir Metronidazole Mebendazole Pyrantel

Diethylcarbamazine Ivermectin Praziquantel Thiabendazole Niclosamide


Inhibit formation of viral DNA from RNA Interfere w/ processing of viral protein Inhibits DNA polymerase Reduced drug inhibits DNA replica Inhibits protein function & by interfering w/ the assembly of the parasites’ microtubules & also decrease glucose uptake Causes paralysis the parasite by acting as depolarizing, NMblocking agent, causing persistent nicotinic receptor activation Alters surface of the worm & immobilize them for phagocytosis Paralyzes worm muscle by inc. Cl-influx(targets glutamategated CL-channel) –hyperpolarization Increases membrane permeability to Ca2+ causing contracture and paralysis of worm Affects microtubular aggregation Inhibits the parasite’s mitochondrial phosphorylation of ADP w/c produces usable ATP; inhibits anaerobic metabolism Inhibits microtubule synthesis & glucose uptake

Azoles (Broad sp)

Polyenes Caspofungin Alkylating agents

-Inhibits synthesis of ergosterol -inhibits C-14 alpha-demethylase( a CP450 enzyme) blocking the demethylation of lanosterol to ergosterol Bind to ergosterol, principal fungal membrane sterol Interfere w/ synthesis of fungi cell wall by inhibiting the synthesis of Beta(1,3)-d-glucan that cause lysis and death Adding an alkyl group to DNA; not cell specific; most widely used ; Alter structure and function of DNA by cross-linking and/or fragmenting of DNA strands, also cisplatin)



structurally related to normal cell compounds that interfere w/ the availability of normal purine or pyrimidine nucleotide precursors by inhibiting their synthesis or competing w/ them in DNA & RNA syntheis Structurally related to folic acid; inhibits dihydrofolate; leucovorin “rescues” normal cells from methotrexate effect; Inhibition of dihydrofolate reductase leads to an inhibition of purine ring and dTMP biosynthesis.

Etoposide & Teniposide Vinca alkaloids(microtubular inhibitors) Steroid hormones Cellular growth factors Propylthiouracil & methimazole

Glucocorticoid Sulfonlyureas alpha-Glucodase inhibitors Meglitinides Methyxanthines Leukotriene Modifiers


Inhibits topoisomerase Bind to tubulin & disrupt spindle apparatus during cell division Induce remission in acute lymphocytic leukemia(2T Hodgkin’s) Stimulate cells in the bone marrow to accelerate recovery from cytotoxic drugs Inhibit thyroid synthesis (thyroid cubical epithelium extracts from the blood stream and concentrates iodide (iodide trapping)-iodine links w/ tyrosine to form moniodotyrosine (MIT). 2 MITCC produce dioiodotyrosin (DIT). 2 DIT & 1 MIT produce triidothyronine (T3) and 2 DIT produce tetraidiothyronine (T4 or thyroxine). The hormones are stored as thyroglobulin (fig 23.6 & 23.7) Increase glucose; inhibit inflammation & immunological response; osteoporosis Stimulate release of insulin Delay absorption of glucose Stimulates insulin secretion Increase cAMP levels Block binding of LTD4( predominant leukotriene in airways) to this receptor; zileuton inhibits leukotriene synthesis by blocking 5 lipoxygenase Prostaglandin analogue that increase bicarbonate and mucin release and reduces acid secretion; treat NSAIDinduced ulceration

Bulk-forming agents Stimulants and cathartics Saline salts of Mg & Na(MOM) Docusate Sulfasalazine Infliximab Orlistat Immunosuppressive Cyclosporine Cylcophosphamide & azathioprine Basiliximab & daclizumab Muromonab Flucytosine and amphotericin B Tamoxifen and toremifene Trastuzumab, rituximab, bevacizumab & cetuximab Cellular growth hormones Platinum coordination complexes Bleomycin

Dactinomycin Cytarabine

6-Mercaptopurine and 6Thioguanine MICROTUBULE INHIBITORS 5-Fluorouracil

Contain plant matter that absorbs water and soften the stool Increase water and electrolytes in feces w/c increase motility Draw water into the colon Improves penetration of water and fat in feces Metabolized in colon by bacteria into active form 5-ASA & sulfapyridine w/c is absorbed Monoclonal Ab that binds and inhibits TNF-alpha, a proinflammatory protein Pancreatic and gastric lipase inhibitor thus reducing the absorption of dietary fat by 30% Modulate immune response Inhibits Ab and cell-mediated immune responses Kill immunologically competent cells Block the interleukin-2 (II-2)-mediated activation of T lymphocytes Binds to CD3 protein complex in T lymphocytes, blocking Ag recognition Synergism increase membrane permeability Competitive estrogen antagonist, binding to E receptors Enhance T-cell function and natural killer cells Stimulate stem cells in the bone marrow to accelerate recover from cytotoxic drugs Similar to alkylating agents Including daunorubicin and doxorubicin cause scission of DNA by an oxidative process Intercalate with DNA, disrupting DNA function, daunorubicin and doxorubicin have this MOA too ; First antibiotic in tumor therapy Terminates DNA chain elongation. Incorporated into DNA and RNA results in altered functioning of nucleic acids. Inhibit the de novo synthesis of purine ring; Inhibit nucleotide Interconversions. Bind to tubulin and disrupt spindle apparatus Inhibits dTMP synthesis


Acyclovir & Valacyclovir

Metabolized to acyclovir triphosphate, which inhibits viral DNA polymerase Blockage of the M2 protein ion channel and its ability to modulate intracellular pH

Herpes simplex, varicella-zoster, cytomegalovirus


Inhibition of viral DNA polymerase ; indicated only for virus-induced retinitis



Same as penciclovir

Herpes simplex, varicella-zoster


Inhibition of viral DNA polymerase and reverse transcriptase at the pyrophosphate-binding site

Cytomegalovirus, acyclovirresistant herpes simplex, acyclovir-resistant varicella zoster

Ganciclovir Interferon-α

Inhibits viral DNA polymerase Induction of cellular enzymes Hepatitis B and C, human herpes virus 8, papilloma virus, that interfere Kaposi sarcoma, hairy cell with viral protein synthesis


Influenza A

leukemia, chronic myelogenous leukemia


Inhibition of viral DNA polymerase reverse transcriptase

Hepatitis B (chronic cases), human immunodeficiency virus type 1

Oseltamivir & Zanamivir

Inhibition of viral neuramidase Metabolized to penciclovir triphosphate, which inhibits viral DNA polymerase Interference with viral messenger RNA

Influenza A





Blockage of the M2 protein ion channel and its ability to modulate intracellular pH Inhibits viral DNA synthesis

Herpes simplex

Lassa fever, hantavirus (hemorrhagic fever renal syndrome), hepatitis C (in chronic cases in combination with interferonα) RSV in children and infants Influenza A

HSV-1, HSV-2, and VZV; its

use is limited to treatment of immunocompromised patients with HSV keratitis GH-Liver-insulin-like growth factors ACTH-Adrenal cortex glucocorticoids, mineralcorticoids and androgens TSH- thyroid-thyroxine; FSH-Estrogen; LH-ovary (estrogen and progesterone) LH-Testis-Testosterone; Prolactin-breast

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