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Pharmacology ID > ID Beta-Lactams > Flashcards

ID Beta-Lactams Flashcards

1
Q

Penicillins MOA

A

Bind to PCN-binding proteins on bacterial cell wall/membrane; destroy cell wall by inhibiting transpeptidase (enzymes that cross-link peptidoglycan molecules to add strength) causing lysis (bacteriocidal)

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2
Q

Penicillins AE

A

Allergic reaction, n/v/d

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3
Q

Cephalosporins MOA

A

Bind to PCN-binding proteins on bacterial cell wall/membrane; destroy cell wall by inhibiting transpeptidase (enzymes that cross-link peptidoglycan molecules to add strength) causing lysis (bacteriocidal)

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4
Q

Cephalosporin AE

A

Cross-reactivity to penicillin; pseudomembranous colitits; bone marrow suppression; nephrotoxicity

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5
Q

Penicillins Prototype Drug

A

Penicillin G, Penicillin V

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6
Q

Cephalosporins Prototype Drug

A

First-generation: cephalexin; second-generation: cefaclor, cefuroxime; third-generation: ceftazidime; fourth-generation: cefepime

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7
Q

Carbapendems Prototype Drug

A

Imipenem (always combined with cilastatin to inhibit hydrolyzation by renal tubular dipeptidase)

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8
Q

Carbapendems MOA

A

Bind to PCN-binding proteins on bacterial cell wall/membrane; destroy cell wall by inhibiting transpeptidase (enzymes that cross-link peptidoglycan molecules to add strength) causing lysis (bacteriocidal)

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9
Q

Carbapendems AE

A

n/v, fever, imipenem may cause seizures

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10
Q

Glycopeptides Prototype Drug

A

Vancomycin

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11
Q

Glycopeptides MOA

A

Inhibit cell wall synthesis by attaching to the end of the peptidoglycan precursor units (D-alanyl-D-alanine terminus), thereby stopping peptidoglycan synthesis; bacteriocidal

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12
Q

Glycopeptides AE

A

Flushing (red man syndrome), neutropenia; in rare cases: ototoxicity when combined with another ototoxic agent & nephrotoxicity

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13
Q

Fluoroquinolones Prototype Drug

A

Ciprofloxacin

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14
Q

Fluoroquinolones MOA

A

Inhibit DNA gyrase (aka topoisomerase II) in gram-neg organisms and topoisomerase IV in gram-pos organims; bacteriocidal

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15
Q

Fluoroquinolones AE

A

Generally well-tolerated; n/v/d; tendon ruptures

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16
Q

Aminoglycosides Prototype Drug

A

Gentamicin

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17
Q

Aminoglycosides MOA

A
  1. Inhibit protein synthesis by irreversibly binding the 30S ribosomal subunit; at low concentrations, they cause misreading of the mRNA by ribosomes; at high concentrations, they halt protein synthesis, trapping ribosomes at the AUG start codon 2. create fissures and pores in the outer cell membrane, resulting in leakage of intracellular contents and increased antibiotic uptake
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18
Q

Aminoglycosides AE

A

Ototoxicity, nephrotoxicity (indicated by an increase in serum creatinine)

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19
Q

Lincosamides Prototype Drug

A

Clindamycin

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20
Q

Lincosamides MOA

A

Bind the 23S rRNA molecule of the 50S ribosome and inhibit peptidyl transferase, blocking the transfer of the new amino acid onto the growing chain; bacteriostatic; beneficial in toxin-producing infections

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21
Q

Lincosamides AE

A

Pseudomembranous colitis (extremely high incidence of C. diff)

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22
Q

Tetracyclines Prototype Drug

A

Tetracycline

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23
Q

Tetracycline MOA

A

First enter microorganism, then bind reversibly to 16S sununit of the 30S ribosome and inhibits translation; bacteriostatic; Demecloclycline inhibits the binding of ADH to its receptor

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24
Q

Tetracyclines AE

A

Significant n/v/d; mottling of teeth d/t Ca binding; photosensitivity; superinfection; diabetes insipidus; liver damage; kidney damage

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25
Q

Macrolides Prototype Drug

A

Erythromycin

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26
Q

Macrolides MOA

A

Bind to bacterial 50s ribosome and inhibit peptidyl transferase, blocking the transfer of the new amino acid onto the growing chain. Inhibition of protein synthesis does not typically kill bacteria cells, so these agents are generally bacteriostatic , but in high concentrations they can be bactericidal.

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27
Q

Macrolides AE

A

Significant GI upset due to increased gut motility; Acute cholestatic hepatitis . Are better tolerated but can also cause liver impairment

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28
Q

Oxazolidinones Prototype Drug

A

Linezolid

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29
Q

Oxazolidinones MOA

A

blocks the translocation step of protein synthesis by binding the 23S rRNA of the 50S RSU. Therefore bacteriostatic. Can also result in human mitochondrial suppression (mitochondrial inhibitor) causing rare but serous side effects.

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30
Q

Oxazolidinones AE

A

Rare but serious. Serotonin Syndrome, Hyperlactatemia and Metabolic Acidosis, Nerve Damage (neuropathies), and Hematologic (bone marrow suppression and low blood count)

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31
Q

Sulfonamides Prototype Drug

A

Sulfamethoxazole

32
Q

Sulfonamides MOA

A

inhibitors of folate sythesis (bacteriostatic)

33
Q

Sulfonamides AE

A

Crystalluria, hematuria, nausea, vomiting, diarrhea, photosensitivity, hypersensitivity. Rare and Serious: Stevens-Johnson Syndrone (SJS), Blood Cell Problems (hemolytic Anemia, Aplastic Anemia, Thrombocytopenia), Kernicterus (jaundice in newborns)

34
Q

Metronidazole Prototype Drug

A

Metronidazole

35
Q

Metronidazole MOA

A

Prodrug: ferredoxin reduces nitrogen side chain from drug which results in production of toxic products that damage DNA. Effective for anaerobic bacteria

36
Q

Metronidazole AE

A

Nausea, Metallic Taste, CNS toxicity (ataxia, encephalopathy, siezure), RARE: neutropenia, pacreatitis, peripheral neuropathy, hepatitis

37
Q

Ethambutol Prototype Drug

A

Ethambutol (EMB or E)

38
Q

Ethambutol MOA

A

Disrupts formation of the tuberculous cell wall by blocking arabinosyl transferases. bacteriostatic , suppress the growth of TB but does not kill it

39
Q

Ethambutol AE

A

Neurologic, ( Optic neuritis, perminant blindness, red-green color blindness, peripheral neuropathy)Rash, and Fever

40
Q

Isoniazid Prototype Drug

A

Isoniazid (INH or H)

41
Q

Isoniazid MOA

A

Inhibits mycobacterial cell wall synthesis

42
Q

Isoniazid AE

A

Hepatitis, Peripheral Neuropathy, mild CNS effects, and Rash

43
Q

Pyrazinamide Prototype Drug

A

Pyrazinamide (PZA or Z)

44
Q

Pyrazinamide MOA

A

Prodrug: first needs to be converted to pyrazinoic acid by a mycobacterial enzyme called pyrazinamidase. This inhibits cell wall synthesis by inhibiting enzyme called fatty acid sythase I .Drug is active only if the bacterium is in an acidic environment

45
Q

Pyrazinamide AE

A

Serous: Hepatic Injury (drug induced hepatitis) More Common: Arthalgia (joint pain), Increased uric acid, Anorexia, Nausea and Vomiting

46
Q

Rifamycins Prototype Drug

A

Rifampin (rifampicin)

47
Q

Rifamycins MOA

A

Inhibit bacterial RNA sythesis by binding prokaryotic (bacterial) RNA polymerase. bactericidal for extracellular and intracellular bacteria. is highly lipophilic

48
Q

Rifamycins AE

A

Common: Discoloration of secretions (tears, urine, sweat, stool, saliva), Cholestatic Jaundice and Hepatitis, Rash Rare but Serous: Acute interstitial nephritis (AIN) and Thrombocytopenia

49
Q

CCR5 Antagonists Prototype Drug

A

Maraviroc

50
Q

CCR5 Antagonists MOA

A

Block interaction of gp120 (HIV envelope glycoprotein on cell surface-eventually binds w/ CCR5 to initiate conformational change) w/ CCR5 (chemokine coreceptor), preventing viral entry into human cells; Patients w/ HIV may express CXCR4 or CCR5 or a combo of both (“dual-mixed”); CCR% antagonists typically used for those w/ CCR5; use of CCR5 antagonists in patients who are dual-mixed leads to selection of CCRX4 & resistance

51
Q

CCR5 Antagonists AE

A

Antiretrovirals typically administered in combo regimens therefore tough to decipher side effects; However, postural hypotension & syncope is common; Hepatotoxicity (rare); Cardiovascular events such as MI

52
Q

Fusion Inhibitors Prototype Drug

A

Enfuvirtide

53
Q

Fusion Inhibitors MOA

A

Mimics the HIV machinery required to fuse to the CD4 cell; Competes with the HIV proteins & prevents entry of the virus into the CD4 cell; gp120 binds HIV & activates gp41–>gp41 changes conformation & creates pore into cell–>enfuvirtide binds gp41 & prevents conformational change

54
Q

Fusion Inhibitors AE

A

Injection site irritation; Peripheral neuropathy

55
Q

Integrase Inhibitors Prototype Drug

A

Raltegravir

56
Q

Integrase Inhibitors MOA

A

Responsible for incorporating viral DNA into the host genome; Prevent the formation of covalent bonds w/ host DNA therefore preventing incorporation of HIV into host genome

57
Q

Integrase Inhibitors AE

A

Well-tolerated

58
Q

Nucleoside Reverse Transcriptase Inhibitors Prototype Drug

A

Zidovudine

59
Q

Nucleoside Reverse Transcriptase Inhibitors MOA

A

An enzyme that transcribes viral RNA into viral DNA; Upon entry into the cell are converted to nucleotides by host cell kinases; The nucleotides then compete w/ endogenous nucleosides for incorporation into viral DNA; act as competitive inhibitors of reverse transcriptase; Once incorporated into DNA, cause termination of DNA chain (halts viral replication); also inhibit host cell DNA polymerase; not specific for HIV-1 however nonnucleoside may act directly against HIV-1

60
Q

Nucleoside Reverse Transcriptase Inhibitors AE

A

Myalgia; Headache; Diarrhea; Lactic acidosis; Lipodystrophy; Peripheral neuropathy; Pancreatitis; Hepatotoxicity; Bone marrow suppression; Hypersensitivity; Acute renal failure; Stomatitis & oral ulcers

61
Q

Nonnucleoside Reverse Transcriptase Inhibitors Prototype Drug

A

Nevirapine

62
Q

Nonnucleoside Reverse Transcriptase Inhibitors MOA

A

bind to a site distant from the active site of the reverse transcriptase and induce a conformational change in the enzyme; NO ACTIVITY against DNA polymerase; Binding is very specific to reverse transcriptase

63
Q

Nonnucleoside Reverse Transcriptase Inhibitor AE

A

Rash (macular or papular- pruritic); Rash may progress to Stevens-Johnson syndrome; Hepaptitis (more common in females during pregnancy, result of hypersensitivy reaction);

64
Q

Protease Inhibitors Prototype Drug

A

Saquinavir

65
Q

Protease Inhibitors MOA

A

Disrupts viral maturation; Bind to proteases and prevent viral maturation which produces immature, noninfectious virus particles

66
Q

Protease Inhibitors AE

A

GI (n/v/d); Hyperlipidemia; Lipodystrophy (fat redistribution); Hyperglycemia/insulin resistance (inhibit activity of glucose transporter GLUT-4); Crystalluria/nephrolithiasis; Hyperbilirubinemia

67
Q

Uncoating Inhibitors Prototype Drug

A

Amantadine

68
Q

Uncoating Inhibitors MOA

A

Prevents the virus from uncoating not allowing the viral DNA to be translated into mRNA; Uncoating is mediated by a M2 protein which serves as a proton channel facilitating the dissociation of the RNA-protein complex; This dissociation is pH-dependent so when drug prevents the influx of protons through M2, prevent dissociation from occuring; may also inhibit a late step of viral assembly

69
Q

Uncoating Inhibitors AE

A

CNS-Amantadine (nervousness, lightheadedness, difficulty concentrating, insomnia); Loss of appetite, Nausea

70
Q

Neuroaminidase Inhibitors Prototype Drug

A

Zanamivir

71
Q

Neuraminidase Inhibitors MOA

A

Influenza viruses possess 2 surface glycoproteins. Changes in these result in new diseases year after year; cleave the sialic acid residues that are bound to viral hemagglutinin & result in the release of new virus from cells; block the cleavage of sialic acid residues & prevent the release of new virus from early infected cells (earlier administration of drug is more successful)

72
Q

Neuraminidase Inhibitors AE

A

Bronchospasms may occur/worsening of respiratory symptoms; GI symptoms (n/v/abd cramping)

73
Q

Nucleoside Analogues Prototype Drug

A

Acyclovir

74
Q

Nucleoside Analogues MOA

A

Act as DNA polymerase inhibitors; Reduces DNA synthesis & viral replication; Serve as guanosine analogs; Important step in viral life cycle = synthesis of viral DNA; Viral & host cell kinases convert the nucleoside analogues to active nucleoside triphosphates; Nucleoside triphosphates compete w/ viral DNA polymerase for part of the primer strand of viral DNA; Some nucleoside analogues (acyclovir & valacyclovir) cause chain termination when incorporated into DNA strand; Penciclovir inhibits DNA elongation; Selective toxicity based upon (1) affinity for HSV thymidine kinase 200x greater for viral enzyme than human enzyme & (2) greater affinity for viral vs. human DNA polymerase

75
Q

Nucleoside Analogues AE

A

Nausea & diarrhea, Rash, Headache, CNS (confusion, hallucinations, tremor) - Acyclovir & valacyclovir - Esp. renal patients; Nephrotoxicity - Acyclovir & valacyclovir; UNIQUE Hematologic (leukopenia, thrombocytopenia); Reproductive (aspermatogenesis)

Pharmacology ID (2 decks)

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