Antiscabies & Antipedicular - Sulfones Flashcards by Cherie Rosemarie Balorio

are compounds used to control the mite Sarcoptes scabei, an organism that thrives under conditions of poor personal hygiene

Scabicides

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are used to eliminate head, body and crab lice

Pediculicides

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obtained from Peru balsam and other resins
immediate relief from itching
complete cure is achieved with a single application of a 25% emulsion
applied topically as lotion over the entire dampened body, except the face

Benzyl Benzoate

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Eurax®
available in 10% concentration in a lotion and cream intended for topical treatment of scabies

Crotamiton

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derived from Crysanthemum plants
MOA: nerve poisoning

Pyrethrin

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enhances the pediculocide effects of pyrethrin

Piperonyl Butoxide

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for head lice only
10% shampoo

Permethrin

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Kwell
Gamma-benzene hexachloride
ADR: neurotoxicity

Lindane

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Comprise a series of synthetic
antibacterial agents patterned after nalidixic acid (introduced for the treatment of UTI)
1,4-dihydro-4-oxo-3 pyridinecarboxylic acid moiety (essential for antibacterial property)

Quinolones

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the introduction of fluorine atom forming ______ enhances antibacterial activity

Fluoroquinolones

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_______ with sucralfate, antacids aluminum or magnesium, or dietary supplements containing iron or zinc can interfere with the absorption of these antibacterial
agents

Ingestion of the Fluoroquinolones

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Pregnant women with UTI
(inhibits cartilage formation due
to chelating property of quinolones)
Penicillin & Cephalosporins -
DOC for pregnant women with
UTI

Contraindications of Quinolones

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• Diarrhea
• N & V
• Headache
• Dizziness
• Nephrotoxicity
• Phototoxicity
• Crystalluria

Adverse Effects of Quinolones

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• inhibits DNA synthesis due to the inhibition of DNA gyrase (topoisomerase II), an enzyme responsible for introducing supercoils into circular duplex DNA

MOA of Quinolones

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• NegGram®
• useful in the treatment of UTI in which Gram-negative bacteria predominate
• first generation quinolone

Nalidixic Acid

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• Cinobac®
• same action and use with nalidixic acid but with greater oral bioavailability

Cinoxacin

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• Noroxin
• has broad-spectrum of activity against Gram negative & Gram-positive bacteria
• I: UTI caused by E. coli, K. pneumoniae, Enterobacter cloacae, P. mirabilis, indole-positive Morganella morganii, P. aeruginosa, S. aureus, S. epidermidis and group D streptococci; single 800 mg oral dose for uncomplicated gonorrhea

Norfloxacin

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• Penetrex®
• I: UTI and sexually transmitted diseases; approved for treatment of uncomplicated gonococcal urethritis and chancroid caused by Haemophilus ducreyi (single 400 mg/dose)
• Short-elimination half-life dictates twice a day dosing for UTI
• STD - single dose ; UTI - twice a day

Enoxacin

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• Cipro®, Cipro IV®
• the most potent fluoroquinolone
• DOC for bacterial gastroenteritis caused by Gram-negative bacilli
• used for respiratory tract infections such as bronchitis and pneumonia caused by Gram-negative bacteria
• used for combating infections of the skin, soft tissues, bones and joints
• Ciprofloxacin + Ceftriaxone = DOC for disseminated gonorrhea
• single dose Ciprofloxacin + Doxycycline = eradicates gonococcal urethritis
• approved for postexposure treatment of inhalational anthrax

NOTE : used in lower reapiratory tract infections

Ciprofloxacin

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• Floxin®, Floxin IV®
• resembles ciprofloxacin in its antibacterial
spectrum and potency
• approved for the treatment of LRTI inc.
bronchitis and pneumonia caused by Gram-negative bacilli; pelvic inflammatory disease and highly active against gonococci and chlamydia
• single 400 mg dose + doxycycline = recommended for the outpatient treatment of acute gonococcal
urethritis
• infections of the skin and tissues caused by staphylococcus, streptococci and Gram-negative
bacilli may also be treated

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Ofloxacin

Maxaquin®
only quinolone for which once daily oral
dosing suffices
causes the highest incidence of
phototoxicity
I: for acute bacterial exacerbation of
chronic bronchitis causes by H.
influenzae, Moraxella catarrhalis,
Streptococcus pneumoniae; prophylaxis
of infection following transurethral
surgery; acute cystitis and chronic UTI

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Lomefloxacin

newer fluoroquinolone
exhibits higher potency against
Gram-positive bacteria
Has a long elimination half-life that
permits once-a-day dosing for most
indications
Has impressive Gram-negative
bactericidal property
Lowest phototoxicity incidence

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Sparfloxacin

newer fluoroquinolone
L = Lungs (used for pneumonia)

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Levofloxacin

MOA: NONE

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NITROFURAN &
NITROHETEROCYCLIC
COMPOUNDS

* Furazone® * employed topically in the treatment of burns

Nitrofurazone

* Furoxone® * oral treatment of bacterial or protozoal diarrhea caused by susceptible organisms (S. aureus, E.coli, Salmonella, Shigella, Proteus, Enterobacter, V. cholerae) * CI: alcohol (inh. aldehyde dehydrogenase)

Furazolidone

* Furadantin®, Macrodantin® * used as urinary antiseptic * safe for pregnant

Nitrofurantoin

* Antiminth® * Depolarizing neuromuscular blocking agent that causes spastic paralysis in susceptible helminths * Used in the treatment of infestations caused by pinworms and roundworms * DI: should not be given concomitantly with piperazine

Pyrantel Pamoate

* Mintezol® * MOA: inhibits the helminthspecific enzyme fumarate reductase; arrest nematode cell division in metaphase by interfering with microtubule assembly * I: Nematodes infestation

Thiabendazole

* Vermox® * MOA: Irreversibly blocks glucose uptake in susceptible helminths, thereby depleting glycogen stored in parasite; also inhibits cell division in nematodes * I: Nematodes infestation * CI: Pregnancy

Mebendazole

*Eskazole®, Zentel® * Single-dose treatment for ascariasis, Old and New Hookworm infections and trichuriasis * Multiple-dose treatment for pinworm, threadworm, capillariasis, chlonorchiasis and hydatid disease

Albendazole

* Cestocide, Mansonil, Yomesan * a potent taeniacide that causes rapid disintegration of worm segments and the scolex * Note: administer a saline purge 1 to 2 hours after niclosamide therapy to prevent possible cysticercosis resulting from the release of live ova from worm segments damaged by the drug

Niclosamide

* Lorothidol®, Bithin® * DOC for liver fluke (Fasciola hepatica) and lung fluke (Paragonimus westermani) infection

Bithionol

* Vansil® * Indicated for the treatment of Schistosoma mansoni (intestinal schistosomiasis) * MOA: inhibits DNA, RNA and protein synthesis

Oxamniquine

* Bitricide® * DOC for infections caused by schistosomes (blood flukes) * also used for other trematodes infections * MOA: Increases cell membrane permeability of susceptibe worms, resulting in the loss of extracellular calcium -- massive contractions and ultimate paralysis of fluke musculature occurs, followed by phagocystosis of the parasite

Praziquantel

* Cardomec, Eqvalan, Ivomec * produced from Streptomyces avermitilis * Effective for the treatment of Onchoceriasis (River Blindness) * MOA: blocks interneuron-motor neuron transmission in nematodes by stimulating the release of the inhibitory neurotransmitter GABA

Ivermectin

* the first effective chemotherapeutic agents that could be used systematically for the cure of bacterial infections in humans * bacteriostatic

Sulfonamides

Paul's Ehrlich's discovery of the antisyphylitic drug Salvarsan in the year

1908

Gerard Domagk studied a bright red dye

Protonsil

further studies showed that Protonsil was metabolized in vivo to ______ (the active drug)

Sulfunamide

* Antibacterials that are anilinesubstituted sulfonamides (the SULFANILAMIDES) * Prodrugs that react to generate active sulfanilamides (Sulfasalazine) * Nonaniline sulfonamides (Mafenide)

Nomenclature of the Sulfonamides

* because of their structural similarity to PABA, the sulfonamides compete with this substrate for the enzyme dihydropteroate synthetase, thus preventing the synthesis of bacterial folic acid (arrest bacterial growth and cell division)

MOA of Sulfonamide

* crystalluria * Steven-Johnson Syndrome * Kernicterus

Adverse Effects of Sulfonamide

* As a rule, if a microbe is resistant to one sulfonamide, it is resistant to all. * Sulfonamides are usually used with folate reductase inhibitors (inhibit the enzyme dihydrofolate reductase) * Ex: Sulfamethoxazole + Trimethoprim (antibacterial therapy)

Microbial Resistance of Sulfonamides

* Treatment of the first attack of UTI (SMX-TMP = Bactrim) * In burn therapy to prevent and treat bacterial infection (Silver sulfadiazine and mafenide) * Treatment of conjunctivitis and related superficial ocular infections (Na sulfacetamide) * Treatment of Chloroquine-resistant malaria (a combination of quinine, pyrimethamine and sulfadoxime - FANSIDAR) * DOC for Pneumocystis carinii (Bactrim; alternative =pentamidine)

Uses of Sulfonamides

* broken down in the body to maminosalicylic acid and sulfapyridine * used in the treatment of intestinal infections, ulcerative colitis and reduction of bowel flora

Sulfasalazine

* as a single agent - used only for uncomplicated UTI * combined with sulfamethoxazole for a synergistic action and to prevent bacterial resistance

Trimethoprim

* Mechanism of action is similar to that of sulfonamides but are considered less effective * Most were proven useful in the treatment of leprosy

Sulfones

* Avlosulfon® * Used in the treatment of both lepromatous and tuberculoid types of leprosy * Used in combination with clofazimine and rifampin * DOC for dermatitis herpeteformis and sometimes used with pyrimethamine for malaria and trimethoprim for PCP * S/E: Hemolytic anemia, methemoglobinemia, toxic hepatic effects * CI: G6PD-deficient patients

Dapsone

Antiscabies & Antipedicular - Sulfones Flashcards

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