AIDS 2 transciptase inhibitors + 1 protease
Influenza A Amantadine, Oseltamivir, Rimantidine
Herpes Acyclovir, penciclovir, valacyclovir,
Zanamivir -Antimetabolite DOC for respiratory syncytial virus
in young children -SARS
-Lassa fever, Hantavirus, Hepa C( chronic cases)
Ribavirin
Cytomegalovirus(retinitis)
Acyclovir-resistant VZ & HS Foscarnet
Cytomegalovirus Ganiclovir
Hepa A&C herpes 8, papilloma v, Kaposi sarcoma, hairy cell leukemia chronic myclogenous anemia
Interferon-a Hepa B (chronic cases)
HIV T1
Lamivudine Herpes 1 and 2, VZ, ImmCmp w/ HSV keratitis Vidarabin
Systemic amebiasis Chloroquine, dehdroxyemetine &
emetine
Luminal and systemic amebiasis Metronidazole, tinidazole
Luminal amebiasis Paronomycin, iodoquinol
Trematodes(flukes) & Cestodes(flat and tape) Clonorchiasis(liver fluke), Paragonimiasis(lung fluke), Schistosomiasis
Praziquantel (DOC)
Roundworms(ascariasis) Mebendazole (DOC), Pyrantel
Lymphatic filariasis Diethylcarbamazine + Albendazole
Cutaneous filariasis
River blindness & strongyloidiasis
Ivermectin
Trichuriasis( whipworm) Mebendazole
Enterobiasis(pinworm) Mebendazole or Pyrantel pamoate
Hookworm Mebendazole or Pyrantel pamoate
Strongyloidiasis Ivermectin or Thiabendazole
Systemic Mycoses Amphotericin B (DOC)
Candida albicans Nystatin, Micafungin & Anidulafungin
(both IV)
Dermatophytoses & onychomycoses(nail) Terbinafine (DOC) Subcutaneous and systemic mycoses Echinomandins Aspergillus and candida species Caspofungin (IV)
Topical mycoses Imidazoles(cotrimazole, econazole)
Topical & Systemic mycoses Imidazoles(ketoconazole, miconazole)
Systemic mycoses Triazoles( fluconazole,
itraconazole;dec ADR)
Alkylating a(Cancer) Cyclophosphamide (most commonly
DOC
Adverse Effects
Slow growing tumors Fluorouracil(5-FU)
Tumor therapy Dactinomycin (first antibiotic)
Acute leukemia Daunorubicin & idarubicin
Hodgkin’s and non-Hodgkin’s lymphoma Prednisone (potent synthetic anti-inflammatory corticosteroid)
Breast Cancer Tamoxifen and toremifene;
Metastatic breast cancer Aminoglutethimide
Breast Cancer in postmenopausal women Anastrozole and letrozole (nonsteroidal imidazoles) First-line(other countries)
Tamoxifen (first-line in US) Metastatic hormone responsive breast and
endometrial neoplasms
Megestrol acetate (progestins) Competitive antagonist for prostate cancer Flutamide, nilutamide, bicalutamide Granulocyte colony-stimulating factor (to recover
neutrophils
Filgrastim Granulocyte-stimulating factor(bone marrow
repopulation after chemo, radiation, and bone marrow transplantation)
Salgramostin
Lymphatic & solid cancer Cisplatin (first member)
For infertility Clomiphene
Postmenopausal osteoporosis Raloxifene
For testicular deficiency Testosterone
Stimulate linear bone growth & Rx anemia Danazol
For erectile dysfunction Sildenafil
Stimulate hair growth; BPH Finasteride
For allergic rhinitis, motion sickness, sleep H1 antagonist
COPD Cholinergic antagonist
Oral & chronic asthma Leukotriene modifiers
Prophylactic treatment for asthma Cromolyn sodium
Duodenal & Gastric ulcers cause by H. Pylori Pepto-Bismol & H2 blockers Histamine induced acid release H2 blockers(-TIDINE)
NSAID-induced ulceration Misoprostol
Severe Chron’s disease (refractory to other meds) Infliximab X transplant rejection, specifically T cells Cyclosporine
Metronidazole N,v,d; dark urine or red-brown, metallic taste, disulfiram-like reaction if taken w/ alcohol
Amphotericin B Nephrotoxicity
Caspofungin Flushing AE due to release of histamine(X cylcosporine) Mica & Anidulafungin
Streptozocin Diabetogenic; toxic to Beta cells of Is of Langerhans(insulinomas) Alkylating agents Cytotoxic, mutagenic, carcinogenic lead to secondary malignancies Anthracyclines Cardiac toxicity
Bleomycin Fatal pulmonary fibrosis Cisplatin Severe toxicity(renal) Estradiol, estrone &
estriol
N&V
Diethylstilbestrol Cervical and vaginal cancer in daughters Mifepristone Abortifacient
Progestins Weight gain, edema, depression Sucralfate Constipation
Orlistat Causes flatulence, oily spotting & fecal urgency Cyclosporine Nephrotoxicity
Other information Mechanism of Action
Reverse Transcriptase Inhibitor Inhibit formation of viral DNA from RNA Protease Inhibitor Interfere w/ processing of viral protein
Acyclovir Inhibits DNA polymerase
Metronidazole Reduced drug inhibits DNA replica
Mebendazole Inhibits protein function & by interfering w/ the assembly of the parasites’ microtubules & also decrease glucose uptake Pyrantel Causes paralysis the parasite by acting as depolarizing,
NM-blocking agent, causing persistent nicotinic receptor activation
Diethylcarbamazine Alters surface of the worm & immobilize them for phagocytosis
Ivermectin Paralyzes worm muscle by inc. Cl-influx(targets glutamate-gated CL-channel) –hyperpolarization
Praziquantel Increases membrane permeability to Ca2+ causing contracture and paralysis of worm
Thiabendazole Affects microtubular aggregation
Niclosamide Inhibits the parasite’s mitochondrial phosphorylation of ADP w/c produces usable ATP; inhibits anaerobic metabolism
Azoles (Broad sp) -Inhibits synthesis of ergosterol
-inhibits C-14 alpha-demethylase( a CP450 enzyme) blocking the demethylation of lanosterol to ergosterol Polyenes Bind to ergosterol, principal fungal membrane sterol Caspofungin Interfere w/ synthesis of fungi cell wall by inhibiting the
synthesis of Beta(1,3)-d-glucan that cause lysis and death Alkylating agents 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)
Antimetabolites 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
Methotrexate 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 Inhibits topoisomerase Vinca alkaloids(microtubular
inhibitors)
Bind to tubulin & disrupt spindle apparatus during cell division
Steroid hormones Induce remission in acute lymphocytic leukemia(2T Hodgkin’s)
Cellular growth factors Stimulate cells in the bone marrow to accelerate recovery from cytotoxic drugs
Propylthiouracil & methimazole
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)
Glucocorticoid Increase glucose; inhibit inflammation & immunological response; osteoporosis
Sulfonlyureas Stimulate release of insulin alpha-Glucodase inhibitors Delay absorption of glucose Meglitinides Stimulates insulin secretion Methyxanthines Increase cAMP levels
Leukotriene Modifiers Block binding of LTD4( predominant leukotriene in airways) to this receptor; zileuton inhibits leukotriene synthesis by blocking 5 lipoxygenase
Misoprostol Prostaglandin analogue that increase bicarbonate and mucin release and reduces acid secretion; treat NSAID-induced ulceration
Bulk-forming agents Contain plant matter that absorbs water and soften the stool
Stimulants and cathartics Increase water and electrolytes in feces w/c increase motility
Saline salts of Mg & Na(MOM) Draw water into the colon
Docusate Improves penetration of water and fat in feces
Sulfasalazine Metabolized in colon by bacteria into active form 5-ASA & sulfapyridine w/c is absorbed
Infliximab Monoclonal Ab that binds and inhibits TNF-alpha, a proinflammatory protein
Orlistat Pancreatic and gastric lipase inhibitor thus reducing the absorption of dietary fat by 30%
Immunosuppressive Modulate immune response
Cyclosporine Inhibits Ab and cell-mediated immune responses Cylcophosphamide &
azathioprine
Kill immunologically competent cells
Basiliximab & daclizumab Block the interleukin-2 (II-2)-mediated activation of T lymphocytes
Muromonab Binds to CD3 protein complex in T lymphocytes, blocking Ag recognition
Flucytosine and amphotericin B
Synergism increase membrane permeability
Tamoxifen and toremifene Competitive estrogen antagonist, binding to E receptors Trastuzumab, rituximab,
bevacizumab & cetuximab
Enhance T-cell function and natural killer cells
Cellular growth hormones Stimulate stem cells in the bone marrow to accelerate recover from cytotoxic drugs
Platinum coordination complexes
Similar to alkylating agents
Bleomycin
Including daunorubicin and doxorubicin cause scission of DNA by an oxidative process
Dactinomycin Intercalate with DNA, disrupting DNA function, daunorubicin and doxorubicin have this MOA too ; First antibiotic in tumor therapy Cytarabine Terminates DNA chain elongation.
Incorporated into DNA and RNA results in altered functioning of nucleic acids.
Mercaptopurine and 6-Thioguanine
Inhibit the de novo synthesis of purine ring; Inhibit nucleotide Interconversions.
MICROTUBULE INHIBITORS Bind to tubulin and disrupt spindle apparatus 5-Fluorouracil Inhibits dTMP synthesis
Acyclovir & Valacyclovir Metabolized to acyclovir triphosphate, which inhibits viral DNA polymerase
Herpes simplex, varicella-zoster, cytomegalovirus
Amantadine Blockage of the M2 protein ion channel and its ability to modulate intracellular pH
Influenza A
Cidofovir Inhibition of viral DNA
polymerase ; indicated only for virus-induced retinitis
Cytomegalovirus
Famciclovir Same as penciclovir Herpes simplex, varicella-zoster Foscarnet Inhibition of viral DNA
polymerase and reverse transcriptase at the
pyrophosphate-binding site
Cytomegalovirus, acyclovir-resistant herpes simplex, acyclovir-resistant varicella zoster
Ganciclovir Inhibits viral DNA polymerase Interferon-α Induction of cellular enzymes
that interfere
with viral protein synthesis
Hepatitis B and C, human herpes virus 8, papilloma virus, Kaposi sarcoma, hairy cell leukemia, chronic myelogenous leukemia
Lamivudine Inhibition of viral DNA polymerase
reverse transcriptase
Hepatitis B (chronic cases), human immunodeficiency virus type 1
Oseltamivir & Zanamivir Inhibition of viral neuramidase
Influenza A Penciclovir Metabolized to penciclovir
triphosphate, which inhibits viral DNA polymerase
Herpes simplex
Ribavirin Interference with viral messenger RNA
Lassa fever, hantavirus (hemorrhagic fever renal syndrome), hepatitis C (in chronic cases in
combination with interferon-α)
RSV in children and infants Rimantadine Blockage of the M2 protein
ion channel and its ability to modulate intracellular pH
Influenza A
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
