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Biochem > Pharmacology Final Content > Flashcards

Pharmacology Final Content Flashcards

1
Q

Tetracyclines

Vacuum Her Bedroom

A

Doxycycline, Minocycline, Demclocycline

Tularemia,
Vibrio cholerae, acne, chlamydiae, ureaplasma, urealyticum, Mycoplasma Pneumoniae, H. Pylori, Borrellia Burgdorferi, Brucella, Rickettsiae

also malaria, gonococcals, prophylaxis of chronic bronchitis

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2
Q

Doxycycline

A

Fat soluble, used in infectious prostatitis in the young, fat soluble so broken down in the liver

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3
Q

Minocycline

A

water soluble used by dentists

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4
Q

Demeclocycline

A

not really used as an antibiotic, Blocks the ADH receptors and is therefore used as a treatment for SIADH

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5
Q

Chelation and Tetracylcines

A

tetracyclines chelate divalent cations, go after calcium in teeth, brown teeth, Contraindicated CI in Preggers, children —> due to calcium disruption in bones and teeth

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6
Q

Chloramphenicol

A

50S inhibitor RNA inhibitor, PHEN= lipid soluble, used in sepsis and meningitis b/c it penetrates CSF.

  • Dose dependent Bone marrow Supression
  • inhibitor of CYP450
  • “gray baby syndrome” bilirubin kernicterus and lack of UDPglucouronyl transferase so it remains un-metabolized in the body
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7
Q

AmiNOglycosides

A

GNATS: Gentamycin, Neomycin, Amikacin, Tobramycin, Streptomycin

  • used for gram(-) rods
  • used P.aeruginosa
  • O2 dependent uptake,
  • nephrotoxicity, ototoxicity, NMJ blockade
  • -Bacteriocidal due to misfolded protein and kinking, remember —–Raymond’s drawing
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8
Q

Streptomycin

A

for TB, DOC for bubonic plague and tularemia

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9
Q

Neomycin

A
  • -Only aminoglycoside used topically,

- -can cause contact dermatitis

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10
Q

Resistance to Aminoglycosides

A

Production of conjugating enzymes: acetylases, adenylases

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11
Q

Macrolides

A

Wide Spectrum Bacteriostatic

  • Erythromycin, Azithromycin, clarithromycin
  • -“thromycin” = macrolide
  • -Gram+ cooci (not MRSA)
  • -good for atypicals: chalmydia, mycoplasma, ureaplasma, LEGIONELLA, c.jejuni, Mycobaterium Avium Cellulare (MAC), H.pylori

Toxicity:

  1. QT prolongation –> predisposes to Torsades de Pointes
  2. CYP3A4 inhibition (can cause increase coumadin, theophylline)
  3. hepatotoxicity and upset GI

Azithromycin doesn’t inhibit CYP3A4

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12
Q

Macrolides

-pharmacokinetics

A

inhibit CYP450
-EXCEPT Azithromycin (slightly water soluble no crossing of placenta preggers)
side effects: GI distress, stimulates MOTILIN RECEPTORS–> more peristalsis. (looks like just erythromycin)
–reversible ototoxicity

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13
Q

Telithromycin

A

ketolide, used in macrolide resistant strept. Pneumoniae

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14
Q

Macrolide mode of resistance

A

Methylation of the 50S RNA, methylation of bacteria by methyltransferases hence no inhibition of translocation

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15
Q

Clindamycin

A
  • -not a macrolide, but same MOA and Resistance
  • -Gram + great for S. Aureus therefore great for osteomyelitis
  • -good in mixed pneumonias
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16
Q

Linezolid

A
  • -MOA inhibits the formation of initiation complexes in 50S subunits
  • treats VRSA, VRE, drug resistant pneumoccociae
  • Side effects: bone marrow supression
17
Q

Quinupristin-Dalfopristin

A 
AKA Streptogramins 
MOA: like A site but on 50S site 
spectrum: VRSA and VRE
---resistance to enterococci MO resistance for Vancomycin? 
--replace D-ALA to D-Lactate
18
Q

Lincosamides

A

Clindamycin and Lincomycin

  • -> lincomycin rarely used
  • -like macrolides they bind the 23S rRNA of the 50S subunit, block translocation from the A site to the P site
  • -inhibits formation of initiation complex
  • -Supresses peptidyltransferase activity
  • -Useful against anaerobes B. Fragillis, C. Perfringens
  • -malaria, Gram+ in PCN allergic pt.’s
  • ***Goldstein)) blocks transpeptidation by Reversible binding of the 50 S subunit at site near macrolides
19
Q

Clindamycin

A
  • -Can cause a C DiFF overgrowth
  • -Wide distribution! but can’t go into CSF even when meninges are inflamed
  • t.5= 2-3 hours but can vary based on the route
20
Q

Clindamycin Activity

A

Gram + cocci

  • -pneumococci, S. Pyogenes, viridians streptococci, MSSA, some MRSA and Nocardia
  • -MRSA D TEST for Clindamycin!!
  • –>disc approximation test
  • -Gram + and Gram - bacteria, C. Prefringens (not C.DIFF)
  • actinomyces, Bacteroides fragillis
  • -Pneumocystits Jiroveci is second line: clindamycin +primarquine (anti-malarial)
  • -toxoplasma gondii encephalitis clindamycin + pyramethamine (antimalarial, toxoplasma is a protozoa)
  • -clindamycin is no good against UTI but is used in Pelvic inflammatory disease
21
Q

Clindamycin Resistance

A

Gram (-), aerobic bacteria and enterobacteriaceae poorly penetrate the outer membranes

  • -enterococci and C DIFF
  • -MRSA and coagulase staph
  • -RIBOSOMAL METHYLATION, erm encoding, D test , iMSLB inducible resistance that can occur during therapy
22
Q

Clindamycin drug interactions

A
  • –macrolides, chloramphenicol and clindamycin all attack the same site on the 50S. don’t use together
  • –NMJ blockers and clind. lincoasamides inhibit release of Ach and enhance effects of NMJ for anesthesia
  • –Device Interaction: oleaginous base in clindamycin vaginal cream may weaken condoms and diaphragms
23
Q

Pharm HTN emergencies

A
  • -get a vasodilator on board, IV
  • -Sodium Nitroprusside, Fenaldopam, Diazoxide
  • -Sodium Nitroprusside= MONITOR Thiocyanate levels!
  • -Fenaldopam is only selective D1 dopamine receptor agonist for IV emergencies
24
Q

Sulfonylureas

A

Glyburide, Glipizide,
Tolbutamide

-reduce dose in Renal failure also reduce some in hepatic

25
Q

Alpha Glucosidase Inhibitors

A
  • -Acarbose and Miglitol
  • -Disaccharidases prevent conversion to monosaccharides by brush border enzymes
  • -osmotic diarrhea presents more sugars to flora causing flatulence
26
Q

Biguanides

A
  • –Metformin
  • -activates AMPCK –> increase expression of orphan nuclear receptor (Small Heterodimer Partner) inhibits expression of liver PEPCK and glucose 6 phosphate thus repressing hepatic gluconeogenesis
27
Q

Insulins Rapid Acting

A

Rapid-Acting)

-Humalog or LISPRO
O) 15-30 min P) 30-90 min D) 3-5 hours

-Novolog or ASPART
O) 10-20 min. P) 40-50 min. D) 3-5 hours

-Apidra or GLULISINE
O)20-30 min. P) 30-90 min.
D) 1-2½ hours

28
Q

Short Acting Insulins

A

—-Regular (R) humulin or novolin O) 30 min.-1 hour P) 2-5 hours D) 5-8 hours

–Velosulin (for use in the insulin pump)
O) 30 min.-1 hour P)2-3 hours D)2-3 hours

29
Q

Intermediate Acting Insulin

A

–NPH (isophane)
O) 1-2 hours
P) 4-12 hours
D) 18-24 hours

30
Q

Long Acting Insulin

A

–Lantus (GLARGINE)
O) 1-1.5 hours P) none, steady D) 20-24 hours
–Levemir (DETEMIR)
O) 1-2 hours P) 6-8 D) up to 24 hours

31
Q

Statins

A

Rosuvastatin >Atorvastatin> Simvastatin> Lovastatin ~~ pravastatin > Fluvastatin

MOA) inhibition HMG-COA reductase

Cholesterol Synthesis))) Acetyl COA –> HMG-COA –> Mevalonate –> Farnesyl Pyrophosphate

–HMG COA –> mevalonate = 2NADPH –> NADP+ + HSCOA

HMG COA reductase

  • -> insulin (increases action)
  • -> Glucagon, phosphorylation (decreases action )
32
Q

Fibrates

A

Gemfibrozil, Fenofibrate

—activation of nuclear transcription factor PPAR alpha –> upregulation of LPL –> increased clearance of TG rich lipoproteins

—Fibrates + statins —> ATN, acute tubular necrosis

33
Q

Resins

A

(Bile Acid Sequestrants): Cholestyramine, colestipol, colsevelam

–upregulation of hepatic LDL receptors

34
Q

Cardiac Glycosides

A

oral avail, .5 life, elim.
Digoxin 75% 40 kidneys
Digitoxin >90% 160 liver
Ouabain 0% 20 kidneys

Biochem (5 decks)

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