SYNTHETIC ANTIBACTERIALS Flashcards by Karrizze Basto

Synthetic antibacterial agents are antibiotics.

True or False

False

Antibiotics are from natural origin.

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QUINOLONES

Quinolones are patterned after ____, which is a ____ derivative.

Nalidixic acid
Naphthyridine

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QUINOLONES

Prototype quinolone

Nalidixic Acid

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QUINOLONES

Nalidixic Acid

Identify the isosteric heterocyclic grouping.

Napthyridines

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QUINOLONES

Enoxacin

Identify the isosteric heterocyclic grouping.

Napthyridines

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QUINOLONES

Cinoxacin

Identify the isosteric heterocyclic grouping.

Cinnolines

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QUINOLONES

Norfloxacin

Identify the isosteric heterocyclic grouping.

Quinolones/Fluoroquinolones

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QUINOLONES

Ciprofloxacin

Identify the isosteric heterocyclic grouping.

Quinolones/Fluoroquinolones

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QUINOLONES

Ofloxacin

Identify the isosteric heterocyclic grouping.

Quinolones/Fluoroquinolones

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QUINOLONES

Lomefloxacin

Identify the isosteric heterocyclic grouping.

Quinolones/Fluoroquinolones

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QUINOLONES

Sparfloxacin

Identify the isosteric heterocyclic grouping.

Quinolones/Fluoroquinolones

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QUINOLONES

Mechanism of action of quinolones

DNA Topoisomerase IV inhibitor
DNA gyrase inhibitor (TP II) -> Supercoiling -> -Cidal

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QUINOLONES

Nalidixic Acid

Identify the generation.

1st

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QUINOLONES

Cinoxacin

Identify the generation.

1st

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QUINOLONES

Norfloxacin

Identify the generation.

2nd

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QUINOLONES

Ciprofloxacin

Identify the generation.

2nd

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QUINOLONES

Enoxacin

Identify the generation.

2nd

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QUINOLONES

Ofloxacin

Identify the generation.

2nd

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QUINOLONES

Levofloxacin

Identify the generation.

3rd

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QUINOLONES

Sparfloxacin

Identify the generation.

3rd

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QUINOLONES

Moxifloxacin

Identify the generation.

3rd

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QUINOLONES

Gemifloxacin

Identify the generation.

3rd

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QUINOLONES

Trovafloxacin

Identify the generation.

4th

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QUINOLONES

Gram (-)
Not Pseudomonas species

Identify the generation based on the spectrum described.

1st

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# QUINOLONES * Gram (-) + Pseudomonas species * Gram (+) (S. aureus) * Atypical microorganisms | Identify the generation based on the spectrum described.

2nd

# QUINOLONES * Gram (-) + Pseudomonas species * Extended Gram (+) and atypical microorganisms coverage | Identify the generation based on the spectrum described.

3rd

# QUINOLONES * Gram (-) + Pseudomonas species * Extended Gram (+) and atypical microorganisms coverage * Broad anaerobic coverage | Identify the generation based on the spectrum described.

4th

# QUINOLONES Gastroenteritis caused by G. bacilli

Ciprofloxacin

# QUINOLONES This quinolone increases the effect of warfarin due to its enzyme inhibitor nature.

Ciprofloxacin

# QUINOLONES A quinolone that binds divalent cations, which decreases its absorption. Food also delays its absorption.

Ciprofloxacin

# QUINOLONES Ciprofloxacin is contraindicated with milk and ____ due to binding of divalent cations.

1. Antacids 2. Calcium supplements

# QUINOLONES This drug can lead to ruptured tendons in patients under 18 years old.

Moxifloxacin

# QUINOLONES The only quinolone that is taken once daily. It is the most phototoxic.

Lomefloxacin

# NITROFURANS First nitro heterocyclic compounds to be introduced into chemotherapy.

Nitrofurans

# NITROFURANS Nitrofurans are derivatives of ____, formed on reaction with the appropriate hydrazine or amine derivative.

5-nitro-2-furaldehyde

# NITROFURANS One of the earliest prototype nitrofurans

Nifurtimox

# NITROFURANS Tx of trypanosomiasis and leishmaniasis

Nifurtimox | Anti-protozoal

# NITROFURANS Adverse effects of nitrofurans

Mutagenic and Carcinogenic

# NITROFURANS Antimicrobial activity is present only when the nitro group is in the ____-position of Furan ring

# NITROFURANS Amebicide nitrofuran

Metronidazole

# NITROFURANS MOA: Reduction (nitrofuran reductase) of the nitro group -> ____ (reactive intermediates) -> ____ damage -> inhibition of DNA, RNA, protein, and cell wall synthesis

1. Free radicals 2. Ribosomal proteins

# NITROFURANS The overall effect of nitrofurans to bacterial growth

Bactericidal

# NITROFURANS Topical tx of burns and prevention of bacterial infection associated with skin grafts

Nitrofurazone

# NITROFURANS Oral treatment of bacterial or protozoal diarrhea

Furazolidone

# NITROFURANS Nitrofuran that can inhibit aldehyde dehydrogenase | D/I: Alcohol

Furazolidone

# NITROFURANS Oral tx of UTI

Nitrofurantoin

# NITROFURANS Administered in a microcrystalline form to improve GI tolerance without inferring oral absorption

Nitrofurantoin

# METHENAMINE & ITS SALTS Methenamine is prepared by evaporating a solution of ____ and ____ to dryness.

1. Formaldehyde 2. Strong ammonia water

# METHENAMINE & ITS SALTS Methenamine is used for the treatment of ____.

Chronic UTI

# METHENAMINE & ITS SALTS To liberate the formaldehyde, the pH of the solution must be ____ (weakly acidic).

5.5

# METHENAMINE & ITS SALTS MOA: Liberation of ____ and enhanced by ____ with sodium bisphosphate or ammonium chloride

1. Formaldehyde 2. Acidifying

# URINARY ANALGESIC Former use: Urinary antiseptic Current use: Urinary analgesic on the UT

Phenazopyridine HCl | Pyridium

# URINARY ANALGESIC Phenazopyridine HCl may tint the urine ____.

Red-orange

# URINARY ANALGESIC The stain by Phenazopyridine HCl may be removed by ____.

0.25% sodium dithionite

# URINARY ANALGESIC Phenazopyridine HCl is used in combination in ____ and ____.

1. Azo-Gantrisin (+ Sulfisoxazole) 2. Urobiotic (+ Oxytetracycline + Sulfamethizole)

# ANTI-TUBERCULOSIS Causative organism of tuberculosis

Mycobacterium tuberculosis | Koch Bacillus

# ANTI-TUBERCULOSIS Mycobacterium tuberculosis is a gram __ __ bacillus that live inside macrophages and lysosomes.

(+), acid-fast

# ANTI-TUBERCULOSIS Therapy for the management of TB

Shotgun Therapy | Use of multiple drug regimen

# ANTI-TUBERCULOSIS 1st line single agent for TB

Streptomycin

# ANTI-TUBERCULOSIS 1st line combination for TB

1. Rifampicin 2. Isoniazid 3. Pyrazinamide 4. Ethambutol | RIPE

# ANTI-TUBERCULOSIS MOA of rifampicin

RNA polymerase inhibitor

# ANTI-TUBERCULOSIS MOA of isoniazid

Mycolid acid inhibitor

# ANTI-TUBERCULOSIS MOA of pyrazinamide

Production of pyrazinoic acid -> low pH

# ANTI-TUBERCULOSIS MOA of streptomycin

30s ribosome inhibitor

# ANTI-TUBERCULOSIS MOA of ethambutol

Arabinogalactan synthesis and mycolic acid inhibition | Cell wall synthesis inhibition

# ANTI-TUBERCULOSIS Type of TB wherein the bacteria is resistant to 1-2 of the anti-TB drugs | Resistance to Isoniazid and Rifampin

Multidrug-resistant TB (MDR TB)

# ANTI-TUBERCULOSIS DOTS

Directly Observed Treatment Short-course

# ANTI-TUBERCULOSIS Type of TB wherein the bacteria is resistant to first-line and second-line anti-TB drugs

Extensively drug-resistant (XDR) TB

# ANTI-TUBERCULOSIS Recommended regimen for pulmonary TB that is virtually 100% effective but expensive

6-Month Regimen

# ANTI-TUBERCULOSIS Drugs included in the first two of 6-month TB regimen

1. Rifampicin 2. Isoniazid 3. Pyrazinamide 4. Ethambutol | RIPE

# ANTI-TUBERCULOSIS Drugs included in the next 4 months of 6-month TB regimen

1. Rifampicin 2. Isoniazid 3. Pyrazinamide | RIP

# ANTI-TUBERCULOSIS Adverse effect of ethambutol

Retinobulbar Optic Neuritis | (Colorblindness)

# ANTI-TUBERCULOSIS Rifampicin is produced by ____.

Streptomyces mediterranei

# ANTI-TUBERCULOSIS The most active first line agent against TB

Rifampicin

# ANTI-TUBERCULOSIS Rifampicin is an enzyme ____, which ____ the effect of paracetamol when taken concomitantly. This can lead to ____.

1. Inducer 2. Decreases 3. Hepatotoxicity

# ANTI-TUBERCULOSIS Rifampicin can tint the urine, stool, saliva, tears, and skin ____.

Red-orange

# ANTI-TUBERCULOSIS 1st choice for TB prophylaxis

Isoniazid

# ANTI-TUBERCULOSIS 2nd choice for TB prophylaxis

Rifampicin

# ANTI-TUBERCULOSIS Safest, most potent and effective against all forms of M. tuberculosis

Isoniazid

# ANTI-TUBERCULOSIS Adverse effects of isoniazid

1. Hepatotoxicity 2. Insomnia 3. Peripheral Neuropathy | HIP

# ANTI-TUBERCULOSIS Peripheral neuropathy associated with isoniazid can be managed by ____.

Vitamin B6 Pyridoxine

# ANTI-TUBERCULOSIS 1st line agent for short term TB

Pyrazinamide

# ANTI-TUBERCULOSIS Synthetic analogue of Nicotinamide that penetrates inflamed meninges

Pyrazinamide

# ANTI-TUBERCULOSIS Active against dividing mycobacteria

Ethambutol

# ANTI-TUBERCULOSIS Basic red dye that exerts slow bactericidal effects on M. leprae

Clofazimine

# ANTI-TUBERCULOSIS 3 Secondary drugs treatment for TB

1. Ethionamide 2. Aminosalicylic Acid 3. Aminosalicylate sodium

# ANTI-TUBERCULOSIS Prophylaxis of disseminated MAC in AIDS patients

Rifabutin

# ANTI-TUBERCULOSIS Isolated from S. orchidaceus, S. garyphalus, S. lavendulus

Cycloserine

# ANTI-TUBERCULOSIS Strongly basic cyclic peptide (aminoglycoside) isolated from S. capreolus that is used as an alternative to streptomycin

Sterile capreomycin sulfate

# ANTI-TUBERCULOSIS Adverse effect of rifampicin

1. Cholestatic jaundice 2. Renal toxicity 3. Flu-like symptom

# ANTI-TUBERCULOSIS Adverse effect of pyrazinamide

1. Hepatotoxicity 2. Hyperuricemia

# ANTIPROTOZOAL Triad of features for metronidazole

1. Trichomoniasis 2. Amebiasis 3. Giardiasis | TAG

# ANTIPROTOZOAL Alternative for Vancomycin in the treatment of pseudomembranous colitis, anti-biotic induced diarrhea, and Clostridium difficile infection

Metronidazole | Flagyl

# ANTIPROTOZOAL Tx of asymptomatic carriers of E. histolytica

Diloxanide

# ANTIPROTOZOAL Parent compound that is an antibacterial and antifungal

8-Hydroxyquinoline

# ANTIPROTOZOAL Tx of acute and chronic intestinal amebiasis

Iodoquinol

# ANTIPROTOZOAL Adverse effect of iodoquinol

Neuropathy | Management: Vitamin B6 Pyridoxine

# ANTIPROTOZOAL Tx of for balantidial dysentery, fluke infestations, and liver diseases

Emetine | From Ipecac

# ANTIPROTOZOAL Tx for: * P. carinii pneumonia * African trypanosomiasis (Prophylaxis) * Visceral leishmaniasis | PAV

Pentamidine isethionate

# ANTIPROTOZOAL Originally an antimalarial drug, but Plasmodium falciparum developed tolerance

Atovaquone

# ANTIPROTOZOAL Alternative to pentamidine isethionate for the treatment of P. carinii pneumonia (PCP)

Atovaquone

# ANTIPROTOZOAL MOA of eflornithine

Ornithine decarboxylase inhibition

# ANTIPROTOZOAL Tx of West African sleeping sickness, caused by Trypanosoma gambiense

Eflornithine

# ANTIPROTOZOAL Drug of choice for acute and chronic Chaga's disease

Nifurtimox

# ANTIPROTOZOAL Alternative to nifurtimox for Chaga's disease

Benznidazole

# ANTIPROTOZOAL 2 Adverse effects of benznidazole

1. Peripheral neuropathy 2. Bone marrow suppression

# ANTIPROTOZOAL Drug of choice for later stages of African trypanosomiasis

Melarsoprol

# ANTIPROTOZOAL Melarsoprol is known to cause ____ toxicity.

Arsenic

# ANTIPROTOZOAL Drug of choice for various leishmaniasis

Sodium Stibogluconate

# ANTIPROTOZOAL MOA of Dimercaprol | British Anti-Lewisite (BAL)

Chelation

# ANTIPROTOZOAL Drug of choice for long term prophylactic agent for African trypanosomiasis

Suramin Sodium

# ANTHELMINTHICS Platyhelminthes

1. Tapeworms 2. Flukes

# ANTHELMINTHICS Nemathelminthes

Nematodes or true round worms

# ANTHELMINTHICS Alternative treatment for pinworm (Enterobius vermicularis) and roundworm (Ascaris lumbricoides) infestations.

Piperazine

# ANTHELMINTHICS Selective anthemintic activity against filariasis and ascariasis

Diethylcarbamazepine Citrate

# ANTHELMINTHICS Depolarizing neuromuscular blocking agent for the treatment of pinworms and ascaris | spastic paralysis in susceptible helminths

Pyrantel Pamoate

# ANTHELMINTHICS Pyrantel Pamoate has an antagonistic effect against ____.

Piperazine

# ANTHELMINTHICS Broad-spectrum anthelmintic activity in human and livestock

Thiabendazole

# ANTHELMINTHICS Broad-spectrum anthelmintic activity similar with thiabendazole

Mebendazole

# ANTHELMINTHICS Broad-spectrum anthelmintic against intestinal nematodes

Albendazole

# ANTHELMINTHICS Active against blood trematodes

Niridazole

# ANTHELMINTHICS A potent taenicide; Saline purge 1 to 2 hours after ingestion to remove scolex and worm segments

Niclosamide

# ANTHELMINTHICS * Chlorinated bisphenol that is formerly used in soaps and cosmetics due to antimicrobial activity * Fasciolicide and taeniacide

Bithionol

# ANTHELMINTHICS Tx of Schistosoma mansoni (intestinal schistosomiasis)

Oxamniquine

# ANTHELMINTHICS MOA of praziquantel

Tetanic-like contraction of the fluke due alteration in the influx of calcium ions

# ANTHELMINTHICS Drug of choice for blood flukes

Praziquantel

# ANTHELMINTHICS Obtained from Streptomyces avermitilis

Ivermectin

# ANTHELMINTHICS Controls endo and ecto parasites in domestic animals

Ivermectin

# ANTHELMINTHICS Use of ivermectin in humans

Onchocerciasis (river blindness) | Oncocerca vovulus

# SCABICIDE AND PEDICULICIDE Compounds used to control mites (Sarcoptes scabiei)

Scabicide

# SCABICIDE AND PEDICULICIDE Used to eliminate head, body, crab lice, and fleas

Pediculicide

# SCABICIDE AND PEDICULICIDE Benzyl alcohol + Benzoyl chloride

Benzoyl benzoate

# SCABICIDE AND PEDICULICIDE Ester topical scabicide from peru balsam

Benzoyl benzoate

# SCABICIDE AND PEDICULICIDE Halogenated hydrocarbon with insecticidal activity

Lindane

# SCABICIDE AND PEDICULICIDE Direct contact poison: fumigant effect and acts as stomach poison

Lindane

# SCABICIDE AND PEDICULICIDE Topical treatment for scabies that has an antipruritic effect and local anesthetic action

Crotamiton | Eurax

# SCABICIDE AND PEDICULICIDE Lethal action against lice, ticks, mites, and fleas and pediculicide treatment of head lice

Permethrin

# SULFONAMIDES Brilliant azo red dye which was found to protect against and cure Streptococcal infections in mice

Prontosil

# SULFONAMIDES Active metablite of prontosil

Sulfanilamide

# SULFONAMIDES Non-aniline sulfonamide

Mafenide Acetate | for burn therapy

# SULFONAMIDES Sulfonamides are derived from ____.

p-amino-benzenesulfonamide

# SULFONAMIDES MOA of sulfonamides

Dihydropteroate Synthetase inhibition | No DNA synthesis

# SULFONAMIDES Mechanism of resistance of pathogen against sulfonamides

Increase production of PABA

# SULFONAMIDES 5 Adverse effects of sulfonamides

1. Crystalluria 2. Rashes 3. Anemia 4. Nausea 5. Kernicterus | CRANK

# SULFONAMIDES: ORAL ABSORBABLE SINGLE Prodrug of sulfisoxazole

Sulfisoxazole Acetyl

# SULFONAMIDES: ORAL ABSORBABLE SINGLE Diethanolamine + Sulfisoxazole solution

Sulfisoxazole Diolamine

# SULFONAMIDES: ORAL ABSORBABLE SINGLE More soluble in acidic urine

Sulfamethazine

# SULFONAMIDES: ORAL ABSORBABLE MIX 3 Components of trisulfapyrimidines

1. Sulfa**dia**zine 2. Sulfa**mera**zine 3. Sulfa**metha**zine

# SULFONAMIDES: ORAL ABSORBABLE SINGLE First agent for the tx of pneumonia

Sulfapyridine

# SULFONAMIDES: ORAL ABSORBABLE MIX Tx for pateints with malaria (Plasmodium falcifarum) and with chloroquine resistance

Sulfadoxine + Pyrimethamine

# SULFONAMIDES: ORAL ABSORBABLE MIX Used for malaria prophylaxis for traveller's where chloroquine resistant malaria is endemic

Sulfadoxine + Pyrimethamine

# SULFONAMIDES: TOPICAL Used as eye drops in ophthalmic infections and very soluble in water

Sulfacetamide sodium

# SULFONAMIDES: TOPICAL Short to intermediate acting sulfonamide IM, IV

Sulfisoxazole diolamine

# SULFONAMIDES: TOPICAL 3 Components of TriSulfa

1. Sulfa**benz**amide 2. Sul**facet**amide 3. Sulfa**thiozole**

# SULFONAMIDES: TOPICAL Vaginal cream for Haemophilus vaginalis

TriSulfa

# SULFONAMIDES: TOPICAL NON-ABSORBABLE Non-absorbable topical sulfonamides are used for ____.

Burn Therapy

# SULFONAMIDES: TOPICAL NON-ABSORBABLE Homologue of the sulfanilamide molecule that is not inhibited by PABA

Mafenide Acetate | SULFAMYLON

# SULFONAMIDES: TOPICAL NON-ABSORBABLE Adverse effect of mafenide acetate (Sulfamylon)

Systemic Acidosis

# SULFONAMIDES: TOPICAL NON-ABSORBABLE Tx of Pseudomonas spp. infections

Silver sulfadiazine + Zinc Salt

# SULFONAMIDES: TOPICAL NON-ABSORBABLE Very potent antimicrobial for burns, scald, and wound infections with better patient acceptance than mafenide

Silver sulfadiazine + Zinc Salt

# SULFONAMIDES Effective in treating ulcerative colitis

Sulfasalazine | Colon specific

# SULFONAMIDES Sulfasalazine is a prodrug metabolized into ____ and ____.

p/m-aminosalicylic acid and sulfapyridine

# DIHYDROFOLATE REDUCTASE INHIBITORS For uncomplicated UTI

Trimethoprim

# DIHYDROFOLATE REDUCTASE INHIBITORS Potent antibacterial that is closely related to several anti-malarials but does not have good antimalarial activity

Trimethoprim

# DIHYDROFOLATE REDUCTASE INHIBITORS For chronic UTI and the drug of choice for complicated and uncomplicated UTI especially caused by entero-bacteria

Sulfamethoxazole + Trimethoprim | SMX + TMP = CO-TRIMOXAZOLE

# DIHYDROFOLATE REDUCTASE INHIBITORS Co-trimoxazole is a combination of ____ and ____.

Sulfamethoxazole + Trimethoprim | SMX + TMP

# SULFONES Sulfones are mainly used for treating ____ (Leprosy) caused by Mycobacterium leprae

Hansen's Disease

# SULFONES Test animals to culture M. Leprae.

Mice and Armadillo

# SULFONES Parent sulfone and protype

Dapsone, DDS | Avlosulfone

# SULFONES For both lepromatous and tuberculoid leprosy

Dapsone, DDS | Avlosulfone

# SULFONES Dapsone is the drug of choice for ____.

Dermatitis Herpetiformis

# SULFONES Dapsone is sometimes used with ____ for the tx of malaria with TMP for PCP.

Pyrimethamine

# SULFONES Adverse effects of dapsone

1. Hemolytic anemia (G6PCD) 2. Methemoglobinemia 3. Hepatotoxicity

# SULFONES Reported to be effective against malaria and rickettsia infections

Sulfones