ANTIMICROBIAL THERAPY

DEFINITION ANTIMICROBIAL ± Chemical substance which is capable in low concentration of inhibiting the growth or killing micro-organisms MOLD ± Is capable of producing penicillins that kill other micro-organisms NARROW SPECTRUM BROAD SPECTRUM y Kills or inhibits the growth of many y Inhibits the growth or kills a limited different organisms including number of different organisms infecting and non-infecting organisms y Less potential for Super-Infections y Alters Natural flora and can lead to super-infection & pseudomembranous colitis y Uses: y Unidentified organism y Mixed infections y No other alternatives BACTERIOSTATIC BACTERIOCIDAL y At safe serum levels, inhibits the y At safe serum levels ± kills sensitive growth of sensitive microorganisms organisms y Allows the body¶s immune system to y Effective in immuno-compromised kill the micro-organisms individuals y Ineffective in Immuno-compromised individuals MECHANISM OF ACTION RESISTANCE y Only effective in replicating INHERENT: Organism has never been organisms sensitive to a particular antimicrobial y Interrupts cell wall synthesis, protein agent synthesis, vitamin utilization ACQUIRED: Organism had previously been sensitive but has acquired an insensitivity y Associated with over use of antimicrobial agents CAUSES OF ANTIMICROBIAL FAILURE ANTIMICROBIAL SELECTION y Fever not due to infection y Identify organism and its sensitivity y Improper dose y Identify source of infection y Improper selection of antimicrobial y Select the most narrow spectrum y Improper duration of therapy agent possible ± To Avoid Super y Failure to utilize ancillary measures Infections y Avoid Hypersensitivity -> Allergic to y Incision & Drainage of WBC¶s Cephalosporin -> possibly to PCN y Cost y Use SYNERGISTIC combination in immuno-compromised patients PATIENT VARIABLES y Age y Gentic ± Metabolism of antimicrobial agents y Quinolones ± Affects tendons in children y Allergies ± Cross Allergies y Tetracyclines ± No use in children due to adv rxns of teeth mottling and effect on bone growth.

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PENICILLINS
y y BACTERIOCIDAL ± can¶t use static in immune compromised. Allergic to one ± Allergic to all PCN y y Narrow to Broad Spectrum Crosses Blood Brain Barrier

PENICILLINASE RESISTANT PENICILLINS
Dicloxacillin (Dynapen) - p.o. AB - Penicillinase Resistant y Resistant to Penicillinase Enzyme produced by Staph Aureas y MRSA strains can still destroy this antimicrobial agent. y MRSA has another ase ± Enzyme y Narrow Spectrumo Staph Aureas -> Produces Penicillinase  Infections of the: y Skin y Otitis y Respiratory Tract

Methicillin (Staphcillin) ± inj

Nafcillin (Unipen) - p.o., inj

Oxacillin (Bactocil, Prostaphlin) p.o., inj

PENICILLIN G¶s
Penicillin G Potassium (Pentids) - p.o. Penicillin V Potassium (Pen VK) - p.o. AB - Penicillin G y Spectrum: o Strept Pneumonia  Respiratory, Skin, Otitis o Anaerobic Strept  Respiratory o Trepenema Pallidum (Syphilis)  STD

Procaine Penicillin G (Wycillin) - inj

Wider Spectrum Penicillins
y y
Examples: Ampicillin, amoxicillin Spectrum ± Same as penicillin G¶s ± E. Coli ‡ GI, UTI ± Hemophilus influenza ‡ Respiratory, otitis ± Enterococcus ‡ GI, UTI

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EXTENDED SPECTRUM PENICILLINS
Amoxicillin (Amoxil) - p.o. Amoxicillin/Clavulanate(Augmentin)PO Ampicillin (Omnipen) - p.o., inj Ampicillin/Sulbactam (Unasyn) - inj. *Piperacillin (Pipracil) - inj. *Piperacillin/Tazobactam (Zosyn) - inj. *Ticarcillin (Ticar) - inj. *Ticarcillin/Clavulanate (Timentin) inj AB y y y y - Penicillin - Extended Spectrum Other Example: Mezlocillin Synergistic with Aminoglycosides Spectrum: Same as wider spectrum o Pseudomonas Aerginosa  UTI  Respiratory

PENICILLIN POTENTIATORS
y y y EXAMPLES: Clavulanate, Tazobactam, Sulbactam Overcomes resistant organisms Overcomes enzymes that would destroy the penicillin antimicrobial agent

CEPHALOSPORINS
y y y y y Bacteriocidal 10% Cross Allergenicity with Penicillins 1st Generation does not cross Blood Brain Barrier (BBB) Only Cefuroxime of 2nd generation cross BBB All 3rd generation cross BBB

FIRST GENERATION CEPHALOSPORINS
Cephalexin (Keflex) PO Cefazolin (Kefzol, Ancef) IV Cephalothin (Keflin) IV Cephapirin (Cefadyl) IV AB - Cephalosporins - 1st Generation PO Spectrum y E. Coli, Staph, Hemophilus Influenza y Klebsiella - Respiratory Doesn¶t Cross BBB

2ND GENERATION CEPHALOSPORINS
Cefotetan (Cefotan) IV Cefoxitin (Mefoxin) IV Cefuroxime (Zinacef) IV Crosses BBB Cefaclor (Ceclor) PO Cefadroxil (Duricef) PO Cefuroxime (Ceftin) PO AB - Cephalosporins - 2nd Generation - IV y May be effective in 1st generation resistance y Spectrum o Bacteroids (Anaerobe) ±> Broader Spectrum = Increased Risk for Super Infections  GI, RESP, SKIN

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3rd GENERATION CEPHALOSPORINS
Cefoperazone (Cefobid) Crosses BBB IV Cefotaxime (Claforan) Crosses BBB IV Ceftazidime (Fortaz, Tazicef, Tazidime)
BBB

Ceftriaxone (Rocephin) Crosses BBB IV

Cefdinir (Omnicef) Crosses BBB PO

AB - Cephalosporins - 3rd Generation - inj y May be effective against organisms resistant to 1st & 2nd generation y Synergistic with Aminoglycosides y Spectrum o Broader -> Increased Risk for Super Infection o Similar to second generation o Pseudomonas

ERYTHROMYCIN
Bacteriostatic Erythromycin Estolate y y y y y y y y y y y y y y y y Well absorbed No GI upset Assoc with cholestatic Hepatitis Rarely used But causes Liver Damage IV Use Cannot give IM Well absorbed Causes GI upset Systemically Absorbed Kills normal flora Irritate GI lining Oral Poorly absorbed Useful for Bowel Sterilization prior to surgery Use only when not needed systemically

Erythromycin Lactobionate - inj Erythromycin Stearate

Erythromycin Base

Use: y Penicillin Allergy to Gram Positive Cocci ± For tx respiratory, otitis & syphilis y Topical use for acne ± bacteria that clogs pores y Legionnaire¶s Disease ± Legionella ± Terrible Respiratory infection Side Effect: y Significant GI Upset

MACROLIDES
Azithromycin (Zithromax) Clarithromycin (Biaxin) Respiratory Infection Mycobacterium Avium Respiratory Infection Mycobacterium Avium Helicobacter pylori (Assoc with Many ulcers)

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CLINDAMYCIN
CLINDAMYCIN (Cleocin) - p.o., inj Bacteriostatic y Bacteriocidal with Increase Dose & IV use y Use: Anaerobic infections (Staph): Gi, Resp Adv Reactions: y Diarrhea ± killing nat flora y Pseudomembranous colitis-limit therapy no more than 7 days y Topically for acne

METRONIDAZOLE
METRONIDAZOLE (Flagyl) - p.o., inj Antibiotic - Own Class Bacteriostatic / Bacteriocidal Use: y Trichomonas ± Sexually trans disease y Anaerobic infections y Helicobacter pylori ± GI ulcers Adv Reactions: y Disulfiram like reaction with alcohol ± life threatening reaction. Will be violently sick!!!

VANCOMYCIN
VANCOMYCIN (Vancocin) - inj. Antibiotic - Own Class Bacteriocidal No PO absorption-but given PO to tx pseudomembranous colitis. Use: y PCN allergy for gram positive cocci y MRSA y Pseudomembranous colitis Monitor: y Peak & Trough Blood levels Adv Reactions: y Ototoxic ± Hearing y Nephrotoxic ± Kidney fxn(30-90min)

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TETRACYCLINES
AB ± TETRACYCLINES Bacteriostatic y **Extremely Broad Spectrum - risk of super-infection Food / Drug Interaction: y Minerals: Mg, Ca, Fe, Al (Antacids), Dairy, Various foods. Avoid in Children: y Affects Teeth & Long bone. Deformed & stained. Side Effects: y Photosensitivity (exaggerated sunburn) y GI Upset Fanconi Syndrome: y Expired medication can turn into something toxic, abdominal inflammation. Use for the following infections: y Chlamydia y Acne y COPD Chloera

Doxycycline (Vibramycin) - p.o., inj.

Minocycline (Minocin) ± p.o.

Tetracycline (Sumycin, Tetracyn) ± PO, IV

CHLORAMPHENICOL
CHLORAMPHENICOL (Chloromycetin) - IV Antibiotic - Own Class y Hepatic elimination, not used for Kidney infection y Poor elimination in infants y Crosses Blood Brain Barrier Adverse Reactions y Aplastic Anemia y No WBC & RBC y Need bone marrow transplant Use: y Meningitis y Anaerobic Infections

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AMINOGLYCOSIDES (Are Like Vancomycin ± as far as blood levels)
Amikacin (Amikin)-Reserved for resistance to Gentamicin Gentamicin (Garamycin) Neomycin Tobramycin (Nebcin) -Reserved for resistance to Gentamicin AB - AMINOGLYCOSIDES ± inj y No PO absorption ± Neomycin used PO as bowel Tx. y Nephrotoxic & Ototoxic y Monitor therapy with peak/trough levels y Good Gram negative coverage y Synergistic with penicillins Use: y IV for systemic Gram Negatives y Topical ± Neosporin, Opth & Otic

QUINOLONES
AB ± QUINOLONES Ciprofloxacin (Cipro) - p.o., inj. Levofloxacin (Levaquin) - p.o., inj. Moxifloxacin (Avelox) ± p.o., inj Norfloxacin (Noroxin) - p.o. Ofloxacin (Oflox) - p.o. y y y y Use: y y Broad Spectrum ± For Anthrax Minerals Block absorption Affects tendon growth in children Increasing rate of resistance

UTI Respiratory Infection

URINARY TRACT INFECTION
Co-Trimoxazole (Bactrim, Septra) (Trimethoprim/Sulfamethoxazole) Methenamine (Mandelamine) - p.o. Nitrofurantoin (Macrodantin) - p.o. Sulfamethoxazole (Gantanol) - p.o. Sulfisoxazole (Gantrisin) - p.o. AB - URINARY TRACT ANTI-INFECTIVES y Increasing resistance in hospital & community acquired infections y Sulfonamides (Sulfa) not very usefull anymore

SULFONAMIDES
y y y y High Acquired Resistance Folic Acid - > Tetra Hydro Folate When host gets high dose, will be affected. High usually with HIV, & Pneumocystic Carini Use in combination with trimethoprim to overcome resistance

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CO-TRIMOXAZOLE
Co-Trimoxazole (Bactrim, Septra) (Trimethoprim/Sulfamethoxazole) AB - URINARY TRACT ANTI-INFECTIVES y Trimethoprim/sulfamethoxazole (cotrimoxazole) inhibits bacteria ability to activate folic acid to tetrahydrofolate USE: y UTI y Respiratory Infection y Pneumocystis Carinii (high does therapy) ADVERSE REACTIONS: y Anemia assoc with high dose therapy y Serious Skin Rashes y Diarrhea

METHENAMINE
Methenamine (Mandelamine) - p.o. AB - URINARY TRACT ANTI-INFECTIVES y Breaks down to formaldehyde in acidic environment y Enteric coated to avoid breakdown in the stomach, breaks down in the intestines. y Forms formeldahyde in urine y Cranberry juice and Vitamin C help to acidify urine y Not useful with indwelling Foley catheters, doesn¶t help because urine doesn¶t stay in bladder. y For Chronic UTI¶s

FUNGAL INFECTIONS
y y y SYSTEMIC RESPIRATORY (COCCIDIOIDOMYCOSIS) URINARY MENINGITIS y DERMATOLOGIC ATHLETE¶S FOOT

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AMPHOTERICIN B
Amphotericin B (Fungizone) ± IV ANTIFUNGAL y IV and Bladder Irrigation y Precipitates in Saline, therefore intravenous admixtures in Dextrose and bladder irrigation in H2O. y Do Not Mix with Saline!!! y Protect from Light y Test Dose is administered. y Dose is gradually increased y Adverse Reactions y Headache, chills, fever  Premedicate, with antipyretic, steroids, antihistamines y Hypokalemia y Nephrotoxicity - reversible

Amphotericin B Liposomal (AmBisome) IV

FLUCONAZOLE
Fluconazole (Diflucan) - p.o., inj. ANTIFUNGAL y PO and IV Therapy y Less effective than Amphotericin y Less Side Effects y Advantage: Oral agent for Systemic Infections

NYSTATIN
y y Oral Use for Candida (Thrush) ± Abx or Overuse of steroid inhalers Topical use for Skin & Vaginal Infections (1 Use)

FLUCYTOSINE
Flucytosine (Ancoban) - p.o. ANTIFUNGAL y Oral Use y Adjunct therapy for meningitis

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MISCELLANEOUS
Griseofulvin (Fulvicin) - p.o. ANTIFUNGAL y Oral for dermatologic and nail infections y Duration of therapy can be 6 months to a year (Risk liver damage) ANTIFUNGAL y Dermatologic and Oral infections ANTIFUNGAL y Topical and vaginal use ANTIFUNGAL y Oral use for Candida (thrush). Abx or overuse of steroid inhalers! y Topical use for skin and vaginal infections. (1 Use) ANTIFUNGAL y Nail infections ± Topical and oral. Risk of Liver Damage >1 Month

Ketoconazole (Nizoral) - p.o. Miconazole (Monistat) - topical Nystatin (Mycostatin) - p.o., supp

Terbinafine (Lamisil) - p.o., topical

MYCOBACTERIUM y y y
Slow growing organism Difficult to Eradicate Mycobacterium Tuberculi can be cured

TUBERCULOSIS THERAPY
Ethambutol (Myambutol) - p.o. Isoniazid (INH) - p.o. Rifampin (Rifadin) - p.o. Streptomycin - inj TUBERCULOSIS THERAPY y y Non-Compliance leads to Resistance!!!!! Most Medications are Hepatotoxic ± Monitor LFT¶s

Severity of Disease
Prophylactic Therapy for healthy positive converters Minimal - Moderate Advanced (Disseminated)

# of Drugs 1?? 2 Drugs 3 Drugs

Length of Tx 9-12 months 2 Years 3 Years

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VIRAL THERAPY
Acyclovir (Zovirax) - p.o., inj., topical Valcyclovir (Valtrex) ± p.o. ANTIVIRAL Stop Flare Ups Oral / Genital Herpes ANTIVIRAL Stop Flare Ups Oral / Genital Herpes ANTIVIRAL May hasten recovery Influenza type A ANTIVIRAL ANTIVIRAL ANTIVIRAL

Amantadine (Symmetrel) - p.o.

Lamivudine (Epivir) - p.o. Oseltamivir (Tamiflu) ± p.o. Zidovudine (Retrovir) (AZT) - p.o.

y Some viral infections cannot be cured ± **HIV, Herpes ± Shingles and cold sores

CHEMOTHERAPY GENERAL PRINCIPLES
y DNA ± ± ± ± ± ± Review Double helix structure Chromosomes that direct cellular life Directs formation of RNA Protein synthesis dependent on mRNA and tRNA Each 3 codones make up an amino acid Chemotherapy can block synthesis

GENERAL PRINCIPLES
y Cancer Cell Cycle ± S Phase is replicating phase y Most drugs work on this phase ± G° Phase is non-replicating phase (Sleeping Phase) y No drugs can work on this phase y Drug Resistance ± Innate ± Acquired

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GENERAL PRINCIPLES
Daunomycin (Cerubidine) Plicamycin (Mithracin) 5-Fluorouracil (Fluorouracil) 6-Mercaptopurine (Purinethol) Azathioprine (Imuran) Cytosine Arabinoside (Cytosar) Vinblastine (Velban) ONC ONC ONC ONC ONC ONC ONC AGENTS AGENTS AGENTS AGENTS AGENTS AGENTS AGENTS - ANTITUMOR ANTIBIOTICS - ANTITUMOR ANTIBIOTICS - ANTIMETABOLITES - ANTIMETABOLITES ± ANTIMETABOLITES - ANTIMETABOLITES - PLANT ALKALOIDS

y Drugs kill by first order kinetics ± Effective therapy kills 99.9% of tumor cells ± But 99.9% is not good enough. Because there are always some Cancer cells in G-Phase. y Importance of scheduling regimens & Adv of combo therapy ± Use Neupogen ± For Increase WBC

ALKYLATING AGENTS
(Toxicity ± Rapid growing tissues)
Chlorambucil (Leukeran) Cyclophosphamide (Cytoxan) Mechlorethamine (Mustargen) ONC AGENTS - ALKYLATING AGENTS ONC AGENTS - ALKYLATING AGENTS ONC AGENTS - ALKYLATING AGENTS

y y y

Causes Abnormal pairing of DNA strands Toxicities - Rapid growing normal tissues - hematopoetic (blood cells), GI, hair, gonads Bone marrow depression occurs slowly and recovers in 4 to 6 wks

NITROSOUREAS
(Crosses BBB ± CNS Tumors)
Carmustine (BCNU) Lomustine (CCUN) ONC AGENTS - NITROSOUREAS ONC AGENTS - NITROSOUREAS

y Crosses Blood Brain Barrier y Effective against **CNS tumors**

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CISPLATIN
(Toxicity ± Nephro/Kidney)
Cisplatin (Platinol) ONC AGENTS ± MISCELLANEOUS Extremely Toxic: y Nephrotoxicity ± Must use a lot of fluids and diuretics(Lasix) to protect kidneys, by decreasing contact time of medication with kidneys. y Extensive Nausea & Vomiting Prevention Includes: y Marijuana derivitive ± dronabionol/marinol y Metoclopramide/Reglan ± Increases GI motility y 5HT-3 Antagonist ± Ondansetron (Zofran) or Granisetron (Kytril)

DOXORUBICIN
(Toxicity ± Bone Marrow & Cardio)
Doxorubicin (Adriamycin) ONC AGENTS - ANTITUMOR ANTIBIOTICS Toxicities: y ***Bone Marrow Aplasia*** y Delayed cardiotoxicity leading to CHF ± builds up in the heart. o There is a maximum cumulative lifetime dose that cannot be exceeded

BLEOMYCIN
(Toxicity mainly to lungs)
Bleomycin (Blenoxane) ONC AGENTS - ANTITUMOR ANTIBIOTICS y Used in Combination y Toxicities: Mainly on the Lungs y Pneumonitis y Minimal effect on bone marrow

METHOTREXATE
Methotrexate (Mexate) ONC AGENTS ± ANTIMETABOLITES y Interferes with activation of folic acid to tetrahydrofolate. y May require Leucovorin rescue ± Active form of Folic Acid y Active form of Folate

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HORMONAL THERAPY
Diethylstilbestrol (DES) Medroxyprogesterone (Provera) ONC AGENTS ± HORMONAL y Estrogenens ± Tx of testosterone sensitive tumors ONC AGENTS ± HORMONAL y Progesterone - Tx of uterine cancers

y Palliative therapy - not curative y First line therapy - less toxic y Sex Hormone Therapy ± Testosterone - Tx of estrogen sensitive tumors

ANTI-ESTROGENS
ANTIHORMONAL
Anastrozole (Arimidex) Bicalutamide (Casodex) Flutamide (Eulexin) Goserelin (Zoladex) Leuprolide (Lupron) Mitotane (Lysodren) Tamoxifen (Nolvadex) Palliative ONC ONC ONC ONC ONC ONC ONC AGENTS AGENTS AGENTS AGENTS AGENTS AGENTS AGENTS - ANTIHORMONAL - ANTIHORMONAL - ANTIHORMONAL - ANTIHORMONAL - ANTIHORMONAL - ANTIHORMONAL ± ANTIHORMONAL

y Palliative therapy of breast cancer y Prevention of breast cancer y Possible adverse reaction of uterine cancer

CORTICOSTEROIDS
Dexamethasone (Decadron) ONC AGENTS - CORTICOSTEROIDS Adjunct Therapy for Lymphocytic Cancers y Lymphomas y Leukemias

Prednisone (Orasone)

VINCRISTINE
(Toxicity ± Neurological numbness/weakness)
Vincristine (Oncovin) ONC AGENTS - PLANT ALKALOIDS y Used in Combination Toxicities: y Neurologic numbness & weakness y Minimal effects on bone marrow

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IMMUNOADJUVANT
y y Attempting to assist Body¶s Immune System Everyone will have a cancer cell in their body ± whether or not it continues to grow ± if the person¶s body recognizes it as cancer and whether or not there is cancer proliferation. Levamisole: GI Cancers BCG Vaccine: (TB Vaccine) For bladder Cancer Interferons: to fight viruses. There is a lot of association with viruses & cancer. o Hepatitis ± A hepatic tumor o HIV ± Karposi¶s Sarcoma Laetrile-Cyanide: This therapy will kill you. Apricot pits ± outside is cyanide.

y y y

y

TOXICITY REVIEW
y y y y Nausea/vomiting ± Pretreat prior to therapy: Zofran, Reglan, Marinol Alopecia ± No treatment Bone Marrow Depression ± Treat with filgrastim (Neupogen®) Extravasation of vesicant drugs ± Prevented with careful administration ± only through a central line.

MISCELLANEOUS
y y COMBINATION THERAPY REGIMENS to get 99.9% DOSE BY SURFACE AREA (mg/M²) o Nomogram o Height/Weight = BSA 1.7m/sq (normal)

RESPIRATORY HISTAMINES
Naturally occurring in human tissue ± Skin ± Intestinal Mucosa ± Respiratory tract y Stored in mast cells

y

y H1 ± Cardiovascular y H2 ± Gastrointestinal

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HISTAMINE PHARMACOLOGY
CARDIOVASCULAR (H1 effect)
y y Cerebral vessel dilation - causes histamine headache Capillary dilation  Increased vascular volume  Decreased BP  Histamine Shock Increased capillary permeability  Allows free passage of plasma and proteinrhinorrhea  Leads to edema Bronchoconstriction Sensory Nerve Ending - itch y y

GASTROINTESTINAL (H2 Effect)
Secretagogue Increases gastric acid section ± Direct effect on parietal cells

y

y y

HISTAMINE MECHANISM OF ACTION Stimulate Histamine Receptors
y H1 RECEPTOR Blocked by Antihistamines y y H2 RECEPTOR Blocked by Anti-Ulcer H2 Antagonists H2 Antagonists o Tagamet o Pepcid o Zantac

FUNCTIONS OF HISTAMINES
y Hypersensitivity Reaction ± Allergy ± Anaphylactic Shock Normal Physiology ± Histamines are good for: ± Regulate microcirculation ± Tissue Growth and Repair ± Gastric acid secretion

y

CLINICAL USE OF HISTAMINE
y Diagnostic Agent for Gastritis or Cancer Achlorhydria ± without Hydrogen Chloride ± Hydrochloric Acid. Increased Acid Production with Increased Histamine.

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INHIBITION OF HISTAMINE RELEASE
Cromolyn (Intal, Nasalcrom) ± inh. COPD - Mast Cell Stabilizer y Prophylactic Agent that inhibits histamine release from mast cells. Needs to be given 72hrs before exposure to have maximum effect. y Oral Inhaler, Nasal Inhaler, & Opth use

ANTIHISTAMINE PHARMACOLOGY
VASCULAR Blocks permeability & vasodilation NERVOUS SYSTEM Blocks Itch SMOOTH MUSCLE Antagonizes Bronchoconstriction Not Acute Therapy ± For Acute Therapy -> Need Epinephrine SIDE EFFECTS Sedation Anticholinergic: y Dry Eyes & Mouth y Urinary Retention y Constipation THERAPEUTIC USE y Symptomatic Relief of Allergies ± Need 3 days to be fully effective o Exudative Allergies o Allergic Dermatoses  Hives  Urticaria o Pruritis

INEFFECTIVE FOR y y y Anaphylactic Shock Acute Bronchial Asthma Common Cold o Utilizes Anticholinergic properties ± no antihistaminic HOW IT WORKS y y y y Blocks H1 receptors so that histamines cannot bind and stimulate. Blocks Muscarinic Receptor. Onset of H1 blockade can be delayed 3 days if histamines have already been released Can¶t give an agent to block a receptor that is already occupied. Other properties ± Anticholinergic ± Drying Property

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ANTIHISTAMINES
Brompheniramine Maleate (Dimetane) Chlorpheniramine Maleate (ChlorTrimeton) Cetirizine (Zyrtec) Diphenhydramine (Benadryl) Fexofenadine (Allegra) Loratadine (Claritin) Cyproheptadine (Periactin) Hydroxyzine (Atarax, Vistaril) Desloratadine (Clarinex)
ANTIHISTAMINES LESS SEDATING ANTIHISTAMINES LESS SEDATING ANTIHISTAMINES HIGHLY SEDATING ANTIHISTAMINES HIGHLY SEDATING ANTIHISTAMINES LONG ACTING ANTIHISTAMINES LONG ACTING ANTIHISTAMINES ANTIHISTAMINES ANTIHISTAMINES

THEOPHYLLINES
Aminophylline - inj., p.o. COPD - Theophylline Type Pharmacology y Bronchodilation (smooth muscle effect) o Dilate Bronchioles ± Asthmatics y Diuretic Effect (Chem related to caffeine) y At High Doses ± Increased Heart Rate y At Toxic Doses ± Induces Seizures

Theophylline (Theodur) - inj., p.o.

LEUKOTRIENE RECEPTOR ANTAGONISTS
Montelukast (Singulair) ± p.o. Zafirlukast (Accolate) ± p.o. COPD - Leukotriene Receptor Antag y Relaxes Bronchiole Smooth Muscle y Problem ± Children Started having behavioral changes

ADRENERGICS
Albuterol (Ventolin, Proventil) ± p.o., inhal Epinephrine (Adrenalin) ± inj, inhal Isoproterenol (Isuprel) ± inj, inhal Metaproterenol (Alupent) ± p.o., inhal Terbutaline (Brethine, Bricanyl) ± p.o., inhal., inj.
COPD - BRONCHODILATOR ± ADRENERGIC y Beta 2 Property ± y Increased HR y Shaking y Sweating y Bronchodilation y Beware of Beta 1 Spillover y Utilize Inhalation in order to decrease S/E

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CORTICOSTEROIDS
Beclomethasone Inhaler (Qvar) Budesonide (Pulmicort) y Flunisolide (Aerobid) Fluticasone (Flovent) y Can¶t be on more than 7 days systemically Avoid Adrenal Suppression o By using non-systemic inhalers COPD - CORTICOSTEROIDS (Inhaler) y Inhaler is preferred route

EXPECTORANT
Guaifenesin (Robutussin) COPD - EXPECTORANTS y Stimulates increased production of mucous y Decreases viscosity of mucous o Decreases Thickness y Facilitates removal of mucous through ciliary action and cough y Controversial Effectiveness Not enough expectorant in production to be effective.

Potassium Iodide (SSKI)

MUCOLYTIC
Acetylcysteine (Mucomyst) COPD - MUCOLYTIC AGENTS y Acetylcysteine via Nebulizer o Administered via Respiratory Therapy o Breaks up Mucous in Respiratory Tract o Also utilized as an antidote to acetaminophen toxicity. y Robitussin ± Need 4oz. / day in order to be effective y Mucinex ± 2 Tabs / 2 X Day

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GASTROINTESTINAL CONSTIPATION
DEFINITION y Passage of unduly hard feces, usually occurs when intestinal transit time is prolonged & excessive. Caused by lack of motility and/or moisture DIET CORRECTION OF CONSTIPATION LAXATIVE USE y y y y Acute constipation Chronic Constipation Preparation for Radiologic or GI Exam Preparation for GI Surgery o Cleaning out intestine before Antibiotics given ± to decrease chance of peritonitis To avoid straining o Postop ± Cardiac Patients o CHF y y y y y y y SYMPTOMS Abdominal discomfort Loss of Appetite

y

y y y

Increase Fluids Increase Fibers Increase Excercise CLASSIFICATION OF LAXATIVES Hydrophillic Colloids ± Bulk Forming Saline Cathartics Surface Wetting (Stool Softner) Lubricant Oils Stimulant Cathartics

y

HYDROPHILLIC COLLOIDS
Psyllium Seed (Metamucil) LAXATIVES - Hydrophillic Colloid y Indigestible Fibers y Doesn¶t go to any receptors y Stays in intestinal tract y Increases bulk which increases water in intestinal lumen y Leads to increased motility y Must consume with water

USE: CHRONIC CONSTIPATION ONSET OF ACTION: 24-72 Hrs (Not for Acute Use)

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SALINE CATHARTICS
Epsom Salt LAXATIVES - Saline Cathartics Golytely y Magnesium Citrate Milk of Magnesia Polyethylene glycol 3350 (MiraLax) Inorganic, poorly absorbed salts y Increases Osmotic Pressure which increases H2O in intestinal lumen y Increases bulk which increases motility

USE: ACUTE CONSTIPATION OR PREP FOR AN EXAM ONSET OF ACTION: 30 MINUTES ± 3 HOURS SIDE EFFECT: DIARRHEA, HABIT FORMING

SURFACE WETTING AGENT
Dioctyl Calcium Sulfosuccinate (Surfak) Dioctyl Sodium Sulfosuccinate (Doss, Colace)
LAXATIVES - Surface Wetting (S-Softeners) y Reduces stool surface tension promoting water and fat mixture

USE: PREVENT CONSTIPATION, PREVENT STRAINING ONSET OF ACTION: 1- 3 Days HABIT FORMING: CHRONIC CONST, THOSE WHO CAN¶T STRAIN

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LUBRICANTS
Mineral Oil
LAXATIVES ± Lubricant y Lubricates Intestinal Lumen

USE: ACUTE AND CHRONIC CONSTIPATION ONSET OF ACTION: 6 ± 8 Hrs SIDE EFFECTS: y HABIT FORMING, DECREASES ABSORPTION OF FATS AND FAT SOLUBLE MEDICATIONS (VIT A, D, E, K) y ASPIRATION PNEUMONITIS IF TAKEN AT BEDTIME ± PT LAY DOWN AND IT CAN COME BACK UP & INTO LUNGS

STIMULANT CATHARTICS
Bisacodyl (Dulcolax) Cascara Castor Oil Senna (Senokot) LAXATIVES - Stimulant Cathartics y Irritates intestinal mucosa and stimulates peristalsis

USE: ACUTE CONSTIPTION & PREPARATION FOR EXAM ONSET OF ACTION: 2 ± 8 Hrs SIDE EFFECTS: CRAMPING & HABIT FORMING

DIARRHEA
ETIOLOGY
y y y y y Increase amount of Osmotically active substances in GI Lumen Increased Rate of Intestinal Secretions - Diseases Alteration of Permeability of Intestinal Lumen - Infections Increased Rate of Peristalsis ANS Infection y

DRUG THERAPY
Narcotic Derivatives o Contraindicated in Infestious Diarrhea Adsorbants Hydrophillic Colloids ± Psyllium Fiber o Absorbs Water Restore Intestinal Flora Electrolyte Replacement

y y y y

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ADSORBANTS
Bismuth Salt (Peptobismol, Kaopectate) ANTIDIARRHEAL ± Adsorbants y Absorbs toxins and bacteria causing diarrhea. y Also absorbs medications and vitamins (Bismuth/Salts) o Administer at different time y Useful to prevent infectious diarrhea especially when traveling

RESTORE INTESTINAL FLORA
Lactobacillus Acidophillus (Bacid, Lactinex) ANTIDIARRHEAL- Restore Intestinal Flora y Replaces natural flora bacteria in intestinal tract (Lactobacillus Acidophillus)

USE: Useful following broad spectrum Abx therapy ONSET: 1-2 Days ALTERNATIVES: Dairy Products

ELECTROLYTE REPLACEMENT
Pedialyte ANTIDIARRHEAL - Electrolyte Rep y Especially useful in children that have had diarrhea y Replaces Fluid and Electrolytes

ULCERS ETIOLOGY
y y y y y Stress (Physiologic not psychologic) ± Body releases corticosteroids Alcoholism Idiopathic ± Unknown reason Drug Induced ± ASA, NSAIDS Bacteria Induced (Helicobacter pylori) ± 14 Day course of Abx y y y y y

THERAPY
Antibiotics Antacids Histamine 2 Antagonists Proton Pump Inhibitors Sucralfate

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ANTACIDS
Neutralizes excess acid that causes ulcerations Provides symptomatic relief-Immediate Promotes healing of Ulcers Goal: o Buffer stomach pH between 4 ± 5 o Exceeding pH of 5 leads to rebound acidity y Administration Time: o 1 ± 3 hours post meal ULCER THERAPY - ANTACIDS y y y y Aluminum Hydroxide (Alternagel, Amphojel) Magnesium Hydroxide / Aluminum Hydroxide (Maalox, Mylanta) Sodium Bicarbonate (Rolaids) y Weak antacid, constipating

y y y y

Mag ± Good antacid + causes diarrhea Alum ± Weak antacid + constipating Best Neutralizing Antacid, High Na Content May Neutralize too well and exceed pH5

HISTAMINE 2 BLOCKERS
Cimetidine (Tagamet) - p.o., inj ULCER THERAPY - Histamine H-2 Blockers y NOT FOR GERD!!! y Blocks H-2 receptor in stomach y Blocks secretion of acid y Promotes healing of ulcers (6-8 Weeks) y Utilized to prevent recurrence of ulcers (Life long therapy) y Prevents nocturnal acid

Famotidine (Pepcid) - p.o.

Ranitidine (Zantac) - p.o., inj.

PROTON PUMP INHIBITORS
Dexlansoprazole (Dexilant) ± p.o. Esomeprazole (Nexium) ± p.o. Lansoprazole (Prevacid) - p.o. Omeprazole (Prilosec) - p.o. Pantaprozole (Protonix) ± p.o., inj Rabeprazole (Aciphex) ± p.o. ULCER THERAPY - Proton Pump Inhibitors y FOR GERD!!! y Prevents acid secretion ± Take 30 min before a meal in order to get absorbed. y Gets into the Proton Pump and it doesn¶t work for 24hrs y Prevents gastro esophageal reflux (GERD) y Promotes healing of Ulcers y Not to be used more than 14 days (OTC)

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SUCRALFATE
Sucralfate (Carafate) ULCER THERAPY ± Miscellaneous y Non-Absorbed y Disaccharide y Acts as a barrier on the ulcer y Allows ulcer to heal by preventing acid contact y Sucralfate is attracted to the GI Ulcer & Covers ulcer. y Not Prophylactic

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