Midterm Chapter 6 Halogen To Antitubercular Agent Flashcards
What Group was Halogen belong in the Periodic Table?
GROUP VIIA: HALOGENS (Salt-forming group)
Elements belong to Halogen Group or Group VIIA
Flourine
Chlorine
Bromine
Iodine
Astatine
Also know as Oldest Germicide
Iodine
5% iodine in water with KI
Strong Iodine Solution (Lugol’s Solution)
2% iodine in water with Nal
Iodine Solution
2% solution of iodine in 50% alcohol with NaI
Iodine Tincture
PVP (nonionic surfactant)
Povidone-Iodine (Betadine®)
Iodine preparations official in the USP
Iodine Tincture
Lugols’s Solution/ Strong Iodine Solution
Iodine Solution
Inorganic iodide salts are present to solubilize the iodine and reduce its ———-
volatility (Easily Evaporate)
Memorize
Iodine MOA: probably acts to inactivate proteins by iodination of aromatic residues and oxidation
……
Simplify Moa of Iodine
Targeting Bacterial Protein result to cell death
complexes of iodine and non-ionic surfactants
Iodophors
Means its a subtance that will lower down the surface tension
Surfactants
Combination of iodine and non-ionic surfactants
-Iodophors
Additional info:
such complexes retain the germicidal properties of iodine and also reduce its volatility and essentially remove its irritant properties
Example of Iodophors
Povidone-Iodine
Target: Both Bacteria and Fungi
Povidone-Iodine
• 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
Blue - 7.5 %solution Antiseptic (Skin Cleaner)
Yellow - 10% Antiseptic (Wound Solution)
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
Use as For :
-Wounds
-Dental irrigation
-lavage (Panglimpyo sa wound, pwede sad sa ngipon)
Chloroazodin
this solution is used as wound dressing
glyceryltriacetate solution
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
• quaternaryammoniumcompoundsthat ionize in water and exhibit surface-active properties
• MOA:adsorbontosurfaceofthebacterial cell, at which they cause lysis
• inactivatedbysoapsandotheranion detergents
• tissueconstituents,blood,serum,and pus tend to reduce the effectiveness of these substances
Cationic Surfactants
• used as detergent, emulsifying agent and wetting agent
• used with sodium nitrate as a preservative
Benzalkonium Chloride • Merthiolate® - New
• used specifically for the treatment of diaper rash in infants caused by Bacterium ammoniagenes (causes liberation of ammonia in decomposed urine)
Methylbenzethonium Chloride • Diaparene®
diaper rash in infants caused by
Bacterium ammoniagenes
• 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
Positive result
Negative result
P- Violet
N -Pink/Red
Primary Stain
Mordant
Decolorizer
Counterstain
Cristal Violet
Iodine
Alcohol
Safranin
• Crystalviolet,hexamethyl-p-rosaniline chloride, methyl violet, methyl-rosaniline chloride
• primarydyeingram-staining
• availableasvaginalsuppositoriesforthe treatment of yeast infections (pessaries)
• availableastopicalsolutionsforthe treatment of cutaneous Candida albicans infections
• usedorallyasananthelminticfor 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
Methylene Blue
• 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
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
• usedtopreventmicrobialcontamination
• IdealCharacteristics:effectiveatlow concentrations against all possible microorganisms, nontoxic, compatible with other constituents used in the preparation, stable for the shelf-life of the preparation
Preservatives
• useful as preservative for liquid dosage forms
• have ANTIFUNGAL properties
• preservative effect tends to increase with molecular weight
PARABENS
• p-hydroxybenzoic acid
• 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
CHLOROBUTANOL
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
• MOA:inhibitsthesynthesisofmycolic acid, an important component of the cell wall of mycobacteria
• Principaladverseeffect:Peripheral neuritis due to the competition of INH with pyridoxal phosphate for the enzyme apotryptophanase
• co-administrationofpyridoxineprevents peripheral neuritis
ISONIAZID (INH or H)
• Isonicotinic acid hydrazide
• Nydrazid®
• structural analogue of isoniazid
• used in the treatment of isoniazid- resistant tuberculosis
• S/E: GI irritation, hepatotoxicity, peripheral neuropathies, optic neuritis
Ethionamide
• Trecator SC®
• 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)
• Pyrazinecarboxamide
• 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)
• Myambutol®
• 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)
• MOA: unkwown
• basic red-dye used in the treatment of leprosy, including dapsone-resistant forms
• S/E: Colored-maroon urine
Clofazimine
• Lamprene®
