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Pharmacology > Antimicrobial Agents > Flashcards

Antimicrobial Agents Flashcards

1
Q

__azole

A

Antifungal Agent

Reduces ergosterol synthesis by inhibiting fungal cytochrome p-450 enzymes. Also inhibits mammalian p-450. Rx for Blasto, Coccidio, Histo. SE: GI upset, abnormal LFTs.

Ex: Ketoconazole: broad-spectrum for Asper, Mucor, Candida. Disrupted gonadal/adrenal steroid synthesis = Rx for Cushings and prostate CA, can cause gynecomastia, decreased libido, menstrual irregularities. Miconazole and Clotrimazole: toxic, only topical use.

Ex: Fluconazole, Itracon-, Voricon-: Systemic Cryptococal meningitis and Candida sepsis. NO disruption of steroid synthesis.

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2
Q

Flucytosine

A

Antifungal Agent

Nucleotide analog that inhibits thymidylate synthetase, which inhibits DNA/RNA synthesis.

Used in combo with others (Amph. B) for systemic Cryptococcus and Candida. SE: bone marrow suppression, hepatotoxicity.

Capsofungin: inhibits glucan synthetase to disrupt cell wall, used for systemic Candida and Aspergillosis.

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3
Q

Amphotericin B, Nystatin

A

Antifungal

Binds ergosterol, punches hole in membrane via change in permeability.

Rx: SYSTEMIC mycosis, give intrathecally w/fungal meningitis. SE: nephrotox, infusion-related rxn (fever, chills, muscle spasm, HA), abnormal LFTs.

Nystatin: oral and cutaneous candidiasis (toxic).

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4
Q

Griseofulvin, Terbinafine

A

Antifungal

Interferes with microtubule function in keratin-rich tissue to inhibit replication.

Rx for topical dermophytic infections, take orally. SE: HA, confusion, GI upset, allergic rxn, hepatitis.

Terbinafine: inhibits qualene epoxidase to inhibit ergosterol synthesis. Same indications.

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5
Q

__cillin

A

Penicillins: Beta-Lactam Antibiotic

Inhibits cell wall synthesis by binding PBP to block peptidoglycan cross-linking.

SE: Allergic rxn, Coombs + hemolytic anemia (Pen), nonallergic skin rash and diarrhea (Amp, Amox), interstitial nephritis (Me), neutropenia (Naf), Hepatitis (Ox).

Ex: Penicillin, Methicillin, Piperacillin, Amoxicillin, Ampicillin.

Others: Aztreonam (no allergy, rash, elevated LFTs, GI upset), Imi/Meropenem (GI upset, rash, seizures) - Imi needs Cilastatin.

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6
Q

Ceph__, Cef__

A

Cephalosporins, Beta-Lactam Antibiotic

Inhibit cell wall synthesis by binding PBP to block peptidoglycan cross-linking.

SE: hypersensitivty rxn (10% with penicillin allergy), disulfiram-like rxn, nephrotoxicity.

Ex: Cephalexin, Cefuroxime, Ceftriaxone.

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7
Q

__mycin

A

Aminoglycosides, Protein Synthesis Inhibitor Antibiotic

30S, inhibits initiation complex and causing mRNA misreading. Severe gram negative rod infections.

SE: nephrotoxicity (ATN with cephalosporins), ototoxicity (with loop diuretics), teratogen.

Ex: Gentamicin, Neomycin, Mikacin, Tobramycin, Streptomycin.

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8
Q

__cycline

A

Tetracyclines. Protein Synthesis Inhibitor Antibiotic

30S tRNA, prevents attachment of tRNA to ribosome.

SE: Teeth discoloration and bone deformity in children, teratogen, GI upset, photosensitivity, dizziness, Fanconi syndrome (aminoaciduria, phosphaturia, acidosis, glycosuria). Avoid taking with divalent cations (milk, iron, antacids), inhibit absorption.

Ex: Tetracycline, Doxycycline, Minocycline, Demeclocycline (SIADH Rx, antagonist at V2 receptors).

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9
Q

__thromycin

A

Macrolides: Protein Synthesis Inhibitor Antibiotic

50S tRNA, blocks translocation and inhibits formation of initiation complex. SE: GI upset, acute cholestatic hepatitis, skin rash, eosinophilia.

Ex: Erythromycin (inhibits P-450), Clarithromycin, Azithromycin.

Others: Chloramphenicol (peptidyl transferase inhibitor - causes aplastic anemia, gray baby syndrome), Clindamycin (pseudomembranous colitis, nausea, diarrhea, skin rash, impaired liver fxn), Linezolid (ribosome complex formation inhibitor).

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10
Q

Sulfa__

A

Sulfonamide Antibiotics

Inhibit folic acid synthesis by inhibiting dihydrofolate reductase, leading to disrupted DNA synthesis.

SE: allergic rxn (Steven-Johnson syndrome), hemolytic anemia, kernicterus in newborns, granulocytopenia (give folinic acid), nephrotoxicity.

Ex: Trimethoprim/Sulfamethoxazole (PABA analog) (TMP/SMX), Sulfisoxazole, Sulfamethizole, Sulfadoxine, Sulfadiazine.

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11
Q

__floxacin

A

Fluroquinolone Antibiotics

Inhibit DNA gyrase topoisomerase2, inducing DNA strand breakage and death.

SE: tendonitis, tendon rupture, GI upset, skin rash, HA, dizziness. Contraindicated in pregnancy and children (damage cartilage).

Ex: Moxifloxacin, Ciprofloxacin, Levofloxacin.

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12
Q

Vancomycin

A

Antibiotic

Binds D-ala D-ala terminus of cell wall precursors, inhibiting transglycosylase, leading to weakened proteins in cell wall and cell lysis.

Rx for serious gram positive infections (sepsis, MRSA, C. diff, endocarditis). SE: oto/nephrotoxicity, Red Man Syndrome (flushing, prevent with slow infusion and antihistamines).

Polymyxins: increase permeability of cell membranes, but very toxic. Only topical use for skin lesions infected with gram negative rods.

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13
Q

Metronidazole

A

Antibacterial and Antiprotozoan agent

Reduces to reactive compounds, overall damage/death.

Rx for anaerobic infections below the diaphragm, protozoans (Giardia, Entamoeba, Trichomonas, Gardenerella), and H. pylori with Bismuth and Amoxicillin or Tetracycline. SE: HA, metalic taste, disulfiram-like effect.

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14
Q

Rifampin

A

Antimycobacterial Agent

Inhibits DNA dependent RNA pol/synthesis. Prophylaxis for N. meningitis and H. flu B, used in combination for Leprosy and TB Rx. SE: Orange secretions/urine, hepatitis, nephritis, rash, thrombocytopenia. Induces P-450.

Rx for TB for 6 months.

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15
Q

Isoniazid

A

Antimycobacterial Agent

Inhibits mycolic acid synthesis. Prophylaxis for contacts of active TB patients. SE: neurotoxicity (give Vitamin B6), induces lupus, hepatitis, G6PD hemolytic anemia. Some pts are fast metabolizers, so watch drug levels.

Rx for TB for 6 months.

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16
Q

Pyrazinamide

A

Antimycobacterial Agent

MOA unknown. Sx: hepatotoxicity, GI intolerance, fever, hyperuricemia (gout).

Rx for TB for 2 months.

17
Q

Ethambutol

A

Antimycobacterial Agent

Inhibits arabinosyl transferase, disrupting cell wall synthesis. SE: retrobulbar neuritis leading to visual disturbances and red/green blindness.

Rx for TB for 2 months (6 if Isoniazid resistant).

18
Q

Dapsone

A

Antimycobacterial Agent

PABA antagonist that inhibits folate/DNA synthesis. SE: hemolytic anemia in G6PD, GI intolerance, rash.

Prophylaxis for PCP, use with Rifampin and Clofazimine for Rx of Leprosy.

19
Q

__quin__

A

Antimalarial Agent

Chloro concentrates in vacuoles and prevents heme metabolism, causing toxicity and death. Others MOA unknown.

SE: C - Gi upset, pruritis, visual disturbances, EKG changes. Q - cinchonism (tinitus, HA, dizziness, nausea), Coombs + hemolytic anemia, contraindicated in pregnancy b/c toxic to fetus. M - mental status changes, GI upset, cardiac abnormalities. P - hemolytic anemia in G6PD, abdominal pain, contraindicated in pregnancy b/c fetal hemolytic anemia.

Ex: Chloroquine (prophylaxis), Mefloquine and Quinine (resistant forms), Primaquine (latent hepatic vivax/ovale).

20
Q

Pentamidine, Nifurtimox, Suramin, Melarsoprol, Sodium Stibogluconate

A

Antiprotozoan Agents

Pentamidine: inhibits RNA synthesis. Alt Rx for T. brucei (African Sleeping Sickness), PCP pro.

Nifurtimox: generates free radicals. Rx for Chagas.

Suramin: inhibits energy metabolism enzymes. Rx for early T. brucei.

Melarsoprol: inhibits enzymes. Rx for late/CNS T. brucei.

Sodium Stibogluconate: inhibits glycolysis. Rx of Leishmaniasis.

21
Q

Mebendazole

A

Antihelminthic Agent

Inhibits microtubule synthesis/fxn. Rx for Whipworm, Hookworm, Pinworm, Roundworm (Trichinella, Ascaris 2nd).

Whipworm (Trichuris): asymptomatic, bloody diarrhea. Get from dried goods. White bodies hanging from inflamed mucosa, barrel-shaped eggs in stool. Treat with Mebendazole.

Hookworm (Necator/Ancylostoma): pneumonia, gastroenteritis, anemia. Get from barefoot and invade blood, eggs in stool. Give iron and folic acid for anemia. Cat and dog hookwarm cause cutaneous larva migrans due to inability to invade blood. Rx with Mebendazole, Pyrantel Pamoate.

22
Q

Thiabendazole

A

Antihelminthic Agent

Inhibits microtubule synthesis/fxn. Rx for Roundworm (Strongyloidiasis, Trichinella), cutaneous larva migrans.

Roundworm (Strongyloidiasis): Diarrhea and eosinophilia, pneumonia, diffuse superinfection in immunodeficient, peritonitis. Get from barefoot and invade blood, larve in stool, string test for duodenal larvae. Rx with Thiabendazole, Ivermectin.

Roundworm (Trichinella spiralis): in pig meat, form cysts with larvae in muscle (myocarditis, no Rx), gastroenteritis, myalgia (give steroids), encephalitis if severe. Rx with Me/Thiabendazole.

23
Q

Albendazole

A

Antihelminthic Agent

Inhibits microtubule synthesis/fxn. Rx for Tapeworm (Dog, Pork [tissue] 2nd), Pinworm, Roundworm (Ascaris 2nd), cutaneous larva migrans.

Echinococcus granulosus (Dog Tapeworm): hyatid cysts in lung, liver, brain. Expansion causes organ displacement, daughter cysts with eggshell calcifications, inject with ethanol to prevent anaphylaxis and resect. Rx with Albendazole.

Pinworm (Enterobius): most common in kids, perianal itching, Scotch tape test for eggs. Fecal-oral from contaminated surfaces. Rx with Me/Albendazole, Pyrantel Pamoate.

24
Q

Pyrantel Pamoate

A

Antihelminthic Agent

Activates nicotinic receptors, paralysis. Rx for Roundworm, Hookworm, Pinworm 2nd.

Roundworm (Ascaris): most common helminth overall, rough eggs, obstruction/pneumonia, malnutrition, asymptomatic. Fecal-oral transmission from soil, hatch in small gut, invade lungs via blood, coughed up and swallowed, mature in GI. Rx with Pyrantel Pamoate, Me/Albendazole.

25
Q

Niclosamide

A

Antihemlinthic Agent

Inhibits ATP production. Rx for Tapeworm (Beef, Pork [intestinal]). Give with a cathartic to accelerate defecation.

Taenia saginata (Beef Tapeworm): proglottids, eggs, no hooks. Asymptomatic, malnutrition, GI discomfort. Treat with Niclosamide, Praziquantel.

26
Q

Praziquantel

A

Antihelminthic agent

Increases Ca++ uptake, contracton/paralysis. Rx for Schistosomiasis, Tapeworm (Pork [both], Beef 2nd).

Schistosomiasis: in fresh water from snails, penetrate flesh and get to blood. Mature in portal vein and invade venous plexuses, eggs in feces and urine. Portal hypertension, esophageal varices, splenomegaly, Katayama Fever, hematuria, bladder carcinoma. Rx with Praziquantel.

T. solium (Pork Tapeworm): proglottids, eggs, hooks. INTESTINAL: Asymptomatic, malnutrition, GI discomfort, Rx with Niclosamide or Praziquantel. TISSUE: cysticercosis and nodules from calcifying cyst dissemination to brain, muscle, eye. Neuro deficits, seizures, blindness. Rx with Praziquantel or Albendazole, plus steroids due to inflammation from dying cysts.

27
Q

Ivermectin

A

Antihelminthic Agent

Activates GABA receptors, leads to worm paralysis/death. Rx for River Blindness, Roundworm (Strongyloidiasis 2nd). SE: Mazotti rxn (fever, rash, hypotension, arthralgias, vertigo).

River Blindness (Onchocera volvulus): skin nodules, thick hyperpigmented rashes, blindness. From black fly bite, microfilariae stay in skin, mature and cause fibrosis/nodules (need surgery), inflammation causes rash, may move to eyes, mosquito picks up larvae from bite, only Rx larvae. Rx with Ivermectin.

28
Q

Diethylcarbamazine

A

Antihelminthic agent. Effective against:

Wuchereria bancrofti (Elephantitiasis, Filariasis): fever, edema and scaly skin on legs and genitalia. Mosquito bite, larvae travel in blood to lymph nodes in genitals and lower extremities, cause fibrosis and interrupt drainage. Worms trigger inflammation and fever, microfilariae detected in blood at night, no Rx for adults. Rx with Diethylcarbamazine.

29
Q

__cyclovir

A

Antiviral Agent

Once phosphorylated by thymidine kinase, inhibits DNA synthesis by incorporating into growing DNA strand and terminating it.

Rx for HSV, VZV, EBV, and CMV (gan only). Other: Foscarnet (inhibits DNA pol, no TK needed). SE: neurotoxicity (tremor, delirium), GI upset, nephrotoxicity.

Ex: Acyclovir, Valacyclovir, Penciclovir, Famciclovir. Ganciclovir needs no thymidine kinase (pancyopenia, nephrotox, seizure, HA).

30
Q

__vudine

A

NRTIs, Nucleoside reverse transcriptase inhibitors. Antiretroviral Agent.

Inhibit HIV reverse transcriptase to block DNA synthesis and compete with nucleoside triphosphates to be added to DNA to make a defective particle.

SE: Neutropenia, hypersensitivity rash, GI upset.

Ex: Zidovudine (AZT) (use in pregnancy, megaloblastic anemia), Lamivudine (3TC) (chronic Hep B Rx), Stavudine (d4T), Didanosine (ddI) (pancreatitis), Zalacitabine (ddC), Emtricitabine (FTC), Abacavir.

31
Q

__vir__

A

NNRTIs, Non-nucleoside reverse transcriptase inhibitors. Antiretroviral Agent.

Bind HIV reverse transcriptase to block DNA synthesis.

Ex: Nevirapine (induces P-450, S-J syndrome, fulminant hepatitis), Efavirenz (causes nightmares/CNS disturbances, rash, insomnia, dizziness), Delavirdine (HA, fatigue, nausea, rash, elevated LFTs, teratogen).

32
Q

__navir

A

Protease Inhibitor. Antiretroviral Agent.

Inhibits HIV protease enzyme to prevent mature protein clevage, prevents viral replication. SE: altered distribution of body fat (buffalo hump, central obesity), insulin resistance, hyperlipidemia, GI discomfort, parasthesia, elevated bilirubin and kidney stones (I).

Ex: Saquinavir, Rito- (inhibits P-450), Indi-, Nelfi-, Ataza-, Fosampre-, Tipra-, Daru-, Ampre-.

33
Q

__mantadine

A

Anti-Influenza Virus Agent

Binds M2 proton channel on influenza A, blocks uncoating of viral RNA which inhibits intracellular viral replication. Stimulates DA release from nigra striatum, so Parkinsons Rx.

SE: CNS symptoms (ataxia, slurred speech, dizziness), GI upset.

Ex: Amantadine, Rimantadine, Zanamivir (inhibits neuraminidase, flu Rx and prophylaxis).

34
Q

Ribavirin

A

Antiviral Agent

Guanosine analog that inhibits G synthesis, inhibiting DNA pol and viral replication.

Rx for RSV, influenza, Hep C. SE: hemolytic anemia, elevated bilirubin, teratogen.

Other: Entecavir (Hep B Rx).

Pharmacology (9 decks)

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