CHAP 6 ORGMRD Flashcards
- one of the oldest known germicides in use today
inorganic iodide salts are present to solubilize the iodine and reduce its volatility
- MOA: probably acts to inactivate
proteins by iodination of
aromatic residues and oxidation
IODINE
the following are iodine preparations official in the USP:
- Iodine Tincture
- Lugol’s Solution/ Strong Iodine Solution
- Iodine Solution
2% solution of iodine in 50% alcohol with NaI
Iodine Tincture
5% iodine in water with KI
Lugol’s Solution/ Strong Iodine Solution
2% iodine in water with Nal
Iodine Solution
complexes of iodine and non-ionic
surfactants
- such complexes retain the germicidal properties of iodine and also reduce its volatility and essentially remove its irritant
properties
Iodophors
Betadine®
- Polyvinylpyrrolidone(PVP)-Iodine
- used as an aqueous solution for presurgical disinfection of the incision site
- used to treat wounds and damage to the skin and effective for local bacterial and fungal infections
Povidone-Iodine
MOA
* release of hypochlorous acid (HClO): chlorination of amide nitrogen atoms and oxidation of sulfhydryl groups in proteins
Chlorine-Containing
Compounds
used to disinfect drinking
water
Halazone
- used to disinfect wounds, as packing for dental caries and for lavage and irrigation
- a glyceryltriacetate solution is
used as wound dressing
Chloroazodin
used to treat localized infections to
remove necrotic tissue from massive
infections or radiation necrosis, to
counteract odorous discharges, to
act as an irritant, and to disinfect
cysts and fistulas
Oxychlorosene Sodium
quaternary ammonium compounds that
ionize in water and exhibit surface-active
properties
Cationic Surfactants
- MOA: adsorb onto surface of the bacterial
cell, at which they cause lysis - inactivated by soaps and other anion
detergents - tissue constituents, blood, serum, and
pus tend to reduce the effectiveness of
these substances
Cationic Surfactants
- Merthiolate® - New
- used as detergent, emulsifying
agent and wetting agent - used with sodium nitrate as a
preservative
Benzalkonium Chloride
Diaparene®
- used specifically for the treatment of diaper rash in infants caused by Bacterium ammoniagenes (causes liberation of ammonia in decomposed urine)
Methylbenzethonium Chloride
used as a general antiseptic
- available form: throat lozenges and mouthwashes
- FDA approved for the treatment
of gingivitis
Cetylpyridinium Chloride
Bactidol®, Chlorhex®, Hibiclens®
- in RP - Bactidol® is Hexetidine
- used as irrigation solution and as mouthwash
- not absorbed through skin or mucous membrane and does not cause systemic toxicity
Chlorhexedine gluconate
cationic dyes are active against gram-positive bacteria and many fungi
- gram-negative bacteria are generally resistant
DYES
Crystal violet, hexamethyl-p-rosaniline
chloride, methyl violet, methyl-rosaniline
chloride
- primary dye in gram-staining
- available as vaginal suppositories for the treatment of yeast infections (pessaries)
- available as topical solutions for the
treatment of cutaneous Candida albicans
infections
Gentian violet
used orally as an anthelmintic for
strongyloides and oxyuriasis
Gentian violet
- ingredient of carbol-fuchsin solution (Castellani’s paint), used topically in the treatment of fungal infections, such as ringworm and athlete’s foot
Basic Fuchsin
- antidote for cyanide poisoning
- in high concentrations, it promotes the conversion of hemoglobin to methemoglobin, which because of its high affinity for cyanide ion diverts it from inactivating cytochrome C oxidase
- in low concentrations, it is used to treat drug-induced methemoglobinemia
Methylene Blue
used for the treatment of cystitis and urethritis
* bacteriostatic
Methylene Blue
- MOA: reacts with SULFHYDRYL (- SH) groups in enzymes and other proteins
- this is reversible by thiol-containing
compounds such as CYSTEINE and
DIMERCAPROL
USES
* Antiseptic, disinfectant and
preservatives
MERCURY COMPOUNDS MERCURIALS
- Corrosive sublimate
- HgCl2
MERCURIC CHLORIDE
- Calomel
- Hg2Cl2
MERCUROUS CHLORIDE
- HgNH2Cl
- White precipitate
- used for skin infections
Ammoniated Mercury
- was once a very popular antiseptic for skin and ocular infections
NITROMERSOL
Merthiolate® - old
* weak bacteriostatic antiseptic that is
applied topically in ointments or
aqueous solutions
THIMEROSAL
- used to prevent microbial contamination
- Ideal Characteristics: effective at low
concentrations against all possible
microorganisms, nontoxic, compatible
with other constituents used in the
preparation, stable for the shelf-life of the
preparation
Preservatives
p-hydroxybenzoic acid
* useful as preservative for liquid dosage
forms
* have ANTIFUNGAL properties
* preservative effect tends to increase with
molecular weight
PARABENS
- more effective against molds
Methylparaben
- more effective against yeasts
- more oil-soluble so it is preferred for
oils and fats
Propylparaben
employed as a bacteriostatic agent in
pharmaceuticals for injection, ophthalmic
use, and intranasal administration
Cholorobutanol
commonly used as preservative in vials of
injectable drugs in concentrations of 1%
to 4% in water or saline solution; has
local anesthetic action
BENZYL ALCOHOL (Phenylcarbinol,
Phenylmethanol)
occurs naturally in rose oil and pine-needle
oil; used primarily in perfumery
PHENYLETHYL ALCOHOL
used externally as an antiseptic for lotions,
ointments and mouthwashes; more
effective as a preservative in foods and
pharmaceutical products at low pH
BENZOIC ACID
used as preservative in acidic liquid
preparations in which benzoic acid is
releases
SODIUM BENZOATE
effective antifungal that is used as preservative
SODIUM PROPIONATE
an effective antifungal preservative; used to
preserve syrups, elixirs, ointments, and lotions
containing components such as sugars that
support mold growth
SORBIC ACID
used as the same way as sorbic acid
POTASSIUM SORBATE
used to preserve injectable drugs but bacteriostatic efficacy is reduced in the presence of serum
PHENYLMERCURIC NITRATE
used as preservative
PHENYLMERCURIC ACETATE
Acid fast bacteria
* Rod shaped, aerobic bacteria that
does not form spores
* facultative intracellular, obligate
aerobe
* causes Koch’s disease
* Lowenstein-Jensen medium
(serpentine growth colonies)
Mycobacterium tuberculosis
- Isonicotinic acid hydrazide
Nydrazid® - MOA: inhibits the synthesis of mycolic
acid, an important component of the cell
wall of mycobacteria - Principal adverse effect: Peripheral
neuritis due to the competition of INH with
pyridoxal phosphate for the enzyme
apotryptophanase - co-administration of pyridoxine prevents
peripheral neuritis
ISONIAZID (INH or H)
Trecator SC®
* structural analogue of isoniazid
* used in the treatment of isoniazidresistant
tuberculosis
* S/E: GI irritation, hepatotoxicity,
peripheral neuropathies, optic
neuritis
Ethionamide
Pyrazinecarboxamide
* MOA: unknown
* used in combination with other
agents because resistance develops
rapidly
* S/E: hepatotoxicity (inc. ALT/AST)
* must be enzymatically hydrolyzed to
pyrazinoic acid (active form)
Pyrazinamide (PZA or Z)
Myambutol®
* S/E: Optic neuritis
* loss of ability to discriminate
between red and green
* MOA: inhibits the incorporation of
mycolic acids in the cell walls of the
bacteria
Ethambutol (EMB or E)
- MOA: acts as a competitive
inhibitor for p-aminobenzoic acid
(PABA) in folate biosynthesis - S/E: severe gastric irritation
- second-line treatment for TB
Para-Aminosalicylic Acid (PASA/PAS)
Lamprene®
* MOA: unkwown
* basic red-dye used in the
treatment of leprosy, including
dapsone-resistant forms
* S/E: Colored-maroon urine
Clofazimine
