Histamine: initiates the inflammatory response, stimulates pain receptors

H-1 Receptors: vascular smooth muscle, digestive tract, bronchi

H-2 Receptors: stomach (this is why H-2 blockers are used to treat ulcers)

Leukotrienes: similar effects to histamine

Bradykinin: vasodilator that causes pain
Complement: proteins that neutralize or destroy antigen
Prostaglandins: stored and released by mast cells, cause pain (this is why NSAIDs
work to lower painit inhibits prostaglandin
NSAIDs
-

Primary drugs for tx of simple inflammation

Inhibits cyclooxygenase (enxymes in the pathway of prostaglandin synthesis)
SE: increased gastic acid secretion, irritating to the stomach lining, increased
risk for bleeding
Cox-2 only inhibitors: Celebrexwithout GI SE but there are cardiac side
effects

Glucocorticoids
-

Effective for acute/severe inflammation

Natural hormones released by the adrenal cortex
Suppress the actions of histamine and prostaglandin
Prednisone (synthetic glucocorticoid)
o Acute asthma, skin allergies, cancer
o Long term effects: Cushings, poor glycemic control, gastric ulcers

Humoral immunity: production of antibodies

B-cells: produces antibodies
Memory b-cells: remembers the antigens
T-cells: produce cytokines
Vaccines cause active immunity by making the body produce antibodies (memory B
cells)
Passive immunity occurs when antibodies themselves are administered; used when
pt has been exposed to a pathogen or is at high risk for exposure
Interferons (IFNs): cytokines; work to slow the spread of viral infection
-

Alpha IFNs: cancer, chronic hepatitis B

C Beta IFNs: MS

Interleukins: boost natural defense mechanisms

-

Interleukin-2: metastatic renal cell carcinoma

Interleukin-11: derived from bone marrow cells (Neumega) stimulates platelet

production

Immunosuppressants: used to avoid tissue rejection

-

Cyclosporine (Sandimmune, Neoral)

o Psoriasis, RA (May be used along with prednisone)
o Can be toxic to the kidneys or liver (monitor kidney/liver function)
o Can affect the bone marrow (monitor blood counts)
o No grapefruit juice!

_____________________________________________________________________________________
Nearly all strains of staph aureus in the U.S. are resistant to PCN
Bacteriocidal antibiotics: able to kill bacteria
Bacteriostatic antibiotics: slow bacterial growth
Acquired resistance: occurs when bacteria has mutated, making it resistant to the
antibiotic
Superinfections: normal host flora of body are destroyed by antibiotics
PCN: kill bacteria by disrupting their cell walls
-

SE/Adverse Reactions
o Mildrash, pruritus, fever, and hivesRx w/antihistamines
o Severeanaphylactic shock-occurs within 20 minRx w/epi
Amoxicillin (Amoxil) IV or PO
o Broad spectrum
o Beta-lactamase sensitive
o Streptococci, pneumococci infections
Amoxicillin clavulanate (Augmentin)
o Beta-lactamase resistant
o Major SE: diarrhea

Drugs which inhibit beta-lactamase and therefore are effective:

-

Oxacillin and nafcillin

Amoxicillin combined with clavulanate=Augmentin
Piperacillin combined with tazobactam=Zosyn
Ampicillin + sulbactam=Unasyn

Cephalosporin Antibiotics: one of the most widely prescribed; beta-lactam ring like
PCNs
-

Bacteriocidal: inhibit bacterial cell wall synthesis

1st Generation
o Cefadroxil (Duricef) PO
o Cephalexian (Keflex) PO
o Cefazolin (Ancef) IM or IV
2nd Generation: broader gram (-) coverage

o Cefaclor (Ceclor) PO
o Cefoxitin (Mefoxin) IV
o Cefuroxime (Ceftin, Xinacef) PO, IM, IV
3rd Generation: borad spectrum; more effective against gram (-) orgamisms
o Cefotaxime (Claforan) IM or IV
o Ceftazidime (Fortaz) IM or IV
o Ceftriaxone (Rocephin) IM or IV
o SE: D/N/V
4th Generation
o Cefepime (Maxipime) IV or IM
o Resistant to most beta-lactamase bacteria

Tetracyclines Antibiotics: extracted from soil

-

Bacteriostatic
Limited usefulness
Binds to calcium and iron: should not be taken with milk or iron
Should be taken with food
SE: N/D/V
Can cause photosensitivity
Can cause permanent yellow-brown tooth discoloration in young children
Tetracycline (Sumycin) PO, IM, topical
o Broad spectrum
o Short acting/short half-life
o Ance
o Decrease the efficacy of oral contraceptives

Macrolides Antibiotics
-

Often prescribed for infections resistant to PCN

Bacteriocidal or bacteriostatic
Whooping cough, Legionnaires Disease, Haemophilus influenza, Mycoplasma
pneumonia, strep
Erythromycin (E-Mycin)
Axithromycin (Zithromax aka Z-pack) PO or IV
o Long half-life
o Less GI SE
o Bacteriostatic
o Bronchitis
Clarithromycin
SE: GI disturbances
Take with food
Do not take with statin drugs!!!

Aminoglycosides Antibiotics
-

More toxic than most antibiotic classes

Bacteriocidal: inhibit bacterial protein synthesis
Not given PO!!!
SE: ototoxicity, nephrotoxicity
Gentamicin

FLuoroquinolones
-

Ciprofloxacin (Cipro) IV or PO
Levofloxacin (LEvaquin) IV or PO
Bacteriocidal: inhibit bacterial DNA synthesis
UTIs, lover resp. infections, bone and joint infections, GI, skin infections,
Anthrax
Dont take with multivitamin!!!
Contraindicated in children under 18 yrsmay affect cartilage development

Sulfonamides
-

Bacteriostatic: inhibit folic acid synthesis

UTIs!!!!!
Sulfasalazine (Azulfidine)for UC and RA
Topical forms for skin infections, burns
SE: skin rash, N/V

Misc. Antibiotics
-

Clindamycin (Cleocin) PO, IM, IV, topical

Vancomycin (Vancocin) IV
o Bacteriocidal for gram (+) bacteria
o MRSA, C. diff
o SE: ototoxicity and nephrotoxicity
Linezolid (Zyvox)
o New antibiotic for MRSA and VRE

TB Tx
-

First oral drug: isoniazid (INH)

1960s to present: Rifampin, pyrazinamide, and ethambutol used in
combination with INH; daily for 2 months
INH and rifampin 2-3x/week for next 4 months
For prophylaxis: 2 months INH + pyrazinamide

Fungi: systemic Mycoses

-

Amphotericin B (Fungizone) IV
o SE: flushing, fever/chills, N/V, decreased BP
o Highly toxic
o Nephrotoxicity and electrolyte imbalance possible

Antifungals
-

Fluconazole (Diflucan)
o Systemic and superficial mycoses
o PO, IV, topical
o Oral thrush!!!
Ketoconazole (Nizoral)
o Ststemic candidiasis
o PO or topical
Nystatin (Mycostatin)

o
o

Superficial candidiasis
Oral thrush, vaginosis

Antiretroviral: block a component of the virus replication cycle

-

Nucleoside & Nucleotide Reverse Transcriptase Inhibitors (NRTIs & NtRTIs)

o Zidovudine (Retrovir, AZT)
Can prevent infection from being passed to baby
SE: low blood counts, A/N/V/D
Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Protease Inhibitors

Herpes Simplex Virus (HSV)

-

Type-1 & type-2

CMV
Varicella: shingles & chicken pox
Epstein-Barr virus
Acyclovir (Zovirax)

Antivirals for Flu

-

Amantadine (Symmetrel)
Oseltamivir (Tamiflu)
Zanamivir (Relenza)

Antiprotozoan Drug
-

Metronidazole (Flagyl)
o Antiparasitic and antibiotic

Antineoplastics (aka chemo drugs)

-

Alkylating drugs
o Act by binding with CA cells DNA, changing its structurekilling or
slowing tumor cell replication
o Nitrogen mustardsfirst type developed
Cyclophosphamide (Cytoxin, Cytoxan) PO, IV
Hodgkins, lymphoma, multiple myeloma, breast, ovarian,
lung cancers
SE: immunosuppressant, low blood counts peak at 9-14
days, N/V/D, weight loss, alopecia, impotenece, sterility,
stomatitis
Patients should be well hydrated to prevent hemorrhagic
cystitis
o Nitrosoureas
o Miscellaneous
Cisplatin, carboplatin
Antimetabolites Drugs
o Interferes with nutrient or nucleic acid metabolism of rapidly growing
tumor cells

Folic acid antagonists: prototype: methotrexate

Methotrexate (Trexall)
Immunosuppressant therapy
RA, SLE, psoriasis
Fluorouracil (5-FU)
Blocks enzyme necessary for DNA/RNA synthesis
Breast, colon, rectum, stomach, pancreas
o Pyrimidine analogues: prototype: fluorouracil
o Purine analogues: prototype: mercaptopurine
Antitumor Antibiotics
o Prevent CA cell replication
o IV
o SE: bone marrow suppression, tissue blistering if IV infiltrates
o Bleomycin
Squamous cell carcinoma, testicular tumors, lymphoma
Long duration
SE: pylmonary toxicity
o Adriamycin (doxorubicin)
Lymphomas, leukemias, breast, lung, testes, thyroid, ovaries
(solid tumors)
Often used with other drugs
SE: Cardiac toxicitymay result in HF, and usual N/V/D, bone
marrow suppression and alopecia
Plant Alkaloids/Natural Products
o Mitotic Inhibitors: kill by preventing cell division
Vinca Alkaloids (vin-)
Vincristine (Oncovin) IV
Lymphoma, leukemia, bladder, and breast CA
Taxanes
Excellent anti-tumor activity
Paclitaxel (Taxol), Taxotere
Advanced ovarian and breast CA
SE: low blood counts, alopecia, stomatitis, N/V
Hormones/Hormone Antagonists
o To slow growth of hormone-dependent tumors (prostate &breast)
Estrogen (Premarin)
Use in men to decrease progression of prostate cancer
Anti-estrogen drug tamoxifen
Blocks estrogen receptors in cancer cells
Breast CA tx and prevention of breast CA in high risk
patients
SE: N/V, increased risk of uterine CA, hot flashes, fluid
retention, DVTs, and abnormal vaginal bleeding
Other hormones: Corticosteroids
o Prednisone can suppress inflammatory response
o Gives patient a sense of well-being/euphoria
o

SE: fluid rentention, K+ loss, incrased infection risk/blood sugar,

Cushing-like effect, bleeding tendencies, and increased appetite
Biologic Response Modifiers (BRMs)
o Enhance the bodys immune system to help fight the CA
o Interferons
Proteins produced by the immune system in response to a viral
infection
Alpha-2 (just know as interferon)
Used to treat hairy cell leukemia, CML, Kaposis sarcoma, &
chronic hepatitis B or C
Suppresses growth of cancer cells
SQ, IM, IV
SE: flue-like syndrome in 50%
May produce GI, neurologic, and hepatic toxicity
o Colony stimulating factors
Proteins used to stimulate bone marrow
Stimulate growth and maturation fo WBCs, RBCs, and platelets
Erythropoietin or Epoetin alfa (Procrit, Epogen)
o Use to treat anemia which occurs because of:
Chronic renal failure
CA/AIDS tx
Filgrastim (Neupogen)
o Stimulates WBC production
o Useful in patients on chemotherapy agents
Oprelvekin (Neumega)
o Stimulates platelet production
o Interleukins (metastatic renal cell CA)
o Monoclonal antibodies
Human or genetically engineered antibodies
To target specific antigens on CA cells
Trastuzumab (Herceptin)
Rituximab (RItuxin)
o Non-Hodgkins lymphoma
o SE: can cause rigors
o