Comprehensive Exam - Pharmacology Flashcards

0
Q

Cephalosporins

A

mechanism same as penicillins, more resistant to B-lactamase
Adverse effects: cross sensitivity with penicillin
Renal excretion generally

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1
Q

penicillins

A

Bind to PBPs and inhibit transpeptidase reaction and cross linking of peptidoglycans.
CSF: enter inflamed meninges.
Excretion: renal (exceptions: ampicillin, naficillin = biliary)
Adverse effects: hypersensitivity reaction (mild-severe), diarrhea, superinfections

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2
Q

Aminoglycosides

A

Bind to 30S subunit & interfere with initiation of protein synthesis. Cause incorporation of wrong amino acids.
Renally excreted
Adverse effects: Renal toxicity (reversible), Cochlear toxicity (irreversible), Vestibular toxicity (reversible)
examples: gentamicin, neomycin

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3
Q

Tetracyclines

A

block tRNA from binding to 30S subunit, preventing addition of new amino acid.
Renal excretion
Adverse effects: bind to calcifying teeth and bone, hepatotoxicity for pregnant women, nephotoxicity, phototoxicity

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4
Q

Macrolides

A

Examples: erythromycin
Bind 50S subunit, block peptidyl transferase.
Adverse effects: ototoxicity (high doses), cholestatic jaundice

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5
Q

Clindamycin

A

Binds 50S subunit.

Adverse effects: superinfection by C. difficile

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6
Q

Sulfonamides

A

Examples: sulfamethoxazole
inhibit dihydropteroate synthase, decrease folic acid
Renal excretion, cause crystaluria, displace other drugs from albumin
Adverse effect: skin rashes/ Stevens-Johnson syndrome, kernicterus in neonates

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7
Q

Trimethoprim

A

Inhibits bacterial dihydrofolate reductase

Adverse effects: cause folate deficiency in pregnant women

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8
Q

Floroquinolones

A

Examples: Ciprofloxacin
Inhibits DNA gyrase
Chelates metals, post antibiotic effect
Toxicity: CNS problems if taken with coffee, phototoxicity, arthropathy in children

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9
Q

Isoniazid

A

Inhibits synthesis of mycolic acid.
High concentration in CSF
Toxicity: hepatitis (risk is high > 50 years), peripheral neuropathy (prevented by B6)
Used for TB prophylaxis

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10
Q

Rifampin

A

Binds to DNA dependent RNA polymerase and inhibits transcription.
Toxicity: hepatitis, hypersensitivity reaction, discoloration of body fluids
Tuberculosis

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11
Q

Ethambutol

A

Blocks arabinosyl transferase (cell wall synthesis)
Enters CSF
Toxicity: optic neuritis, acute gout

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12
Q

Pyrazinamide

A

Pyrasinoic acid inhibits growth
Enters CSF
Toxicity: Acute gout

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13
Q

Chloramphenicol

A

toxicity: gray baby syndrome

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14
Q

Vancomycin

A

Red man syndrome (infusion related toxicity due to histamine release)

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15
Q

Otitis media

A

S. pnumonia, H. influenzae
Drug of choice: amoxicillin
Resistance by beta-lactamase: amoxicillin + clavulanate
If diarrhea, switch to Cefprozil (2nd gen cephalosporin)

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16
Q

Surgical prophylaxis

A

IV administation 2 hrs before surgery.
S. aureus, S. epidermis
Cephazolin (1st generation cephalosporin). Severe penicillin allergy or MRSA: Vancomycin
Colorectal & appendectomy: Add oral antibiotics as well due to increased risk of infection

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17
Q

Community Acquired Pneumonia

A

S. pneumoniae
Erythromycin
Requiring hospitalization: Erythromycin + Cefotaxime (3rd generation cephalosporin)
For neuropenic patients: levofloxacin

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18
Q

Gonorrhea

A

Ceftriaxone (3rd gen cephalosporin)

Severe penicillin allergy: Ciprofloxacin

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19
Q

Traveller’s diarrhea

A

Ciprofloxacin

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20
Q

Pseudomembranous colitis

A

Antibiotic induced diarrhea.
Cause is C. difficile.
Treat with metronidazole

21
Q

Urinary tract infections

A

Trimethoprim-Sulfamethoxazole (TMP-SMX)

Pregnant patients: Cephalexin

22
Q

Ampicillin with gentamicin

A

good synergistic effect. Ampicillin makes pores in bacterial cell wall through which aminoglycoside can enter

23
Q

Erythromycin, fungal azoles, metronidizole with Cyclosporin, or Warfarin

A

inhibit cytochrome P-450 and increase toxicity of warfarin/ cyclosporin
Excess immunosuppression, renal toxicity of CSA
Increase prothrombin time and bleeding (warfarin)

24
Rifampin and isoniazid on fungal azoles, warfarin, cyclosporin
induce P-450 to increase the metabolism of azoles, cyclosporin, warfarin
25
Sulfonamides on methotrexate, warfarin
sulfonamides displace drugs from albumin, increasing their toxicity
26
Floroquinolones on caffeine and theophylline
floroquinolones inhibit microsomal enzymes (CYP1A) involved in caffeine metabolism, increasing its effects. Risk of seizures
27
Floroquinolones with milk products and antiacids
tetracyclines & floroquinolones chelate metals (Calcium) and dairy products interfere with there absorption
28
teratogenic antibiotics
Aminoglycosides Tetracyclines TMP-SMX Fluoroquinolones
29
Bactericidal antibiotics
Cell wall synthesis inhibitors (penicillins, cephalosporins, vancomycin) Aminoglycosides Fluoroquinolones TMP-SMX
30
Bacteriostatic antibiotics
``` Tetracyclines Macrolides Clindamycin Sulfonamide Trimethoprim ```
31
Carbon Monoxide
Hypoxia to brain, hypoxia to heart. High affinity binding to hemoglobin, forms carboxyhemoglobin. Competes with O2 and prevents it from binding to Hb. Antidote: 100% O2, Hyperbaric O2 for serious cases or pregnant women
32
Cyanide
Hypoxic symptoms; no cyanosis. Bitter almond smell, metabolic acidosis Binds to ferric iron of cytochrome oxidase, stops electron transport. Death due to respiratory failure Antidote: 1. Amyl nitrate (Hb to MetHb) 2. Sodium thiosulfate (increase renal excretion) 3. methylene blue (metHb back to Hb)
33
Methanol
(Denatured alcohol, antifreeze) Feeling of being in a snow field, blurred vision, papilledema, abdominal pain. Metabolized by alcohol dehydrogenase to form formic acid -> retinal damage, profound metabolic acidosis. Antidote: ethanol, hemodialysis, bicarbonate
34
Lead
Hypochromic microcytic anemia, encephalopathy, seizures (children), peripheral neuropathy + kidney damage (adults), abdominal pain. Accumulates in bone, decreased heme synthesis, RBC stippling, inhibits ALA dehyratase & ferrochelatase. Antidote: Calcium disodium EDTA, Dimercaprol, Succimer (Children), penicillamine (mild toxicity)
35
Iron overdose
Acidosis, liver failure, GI bleeding, occurs in children. Lipid peroxidation in mitochondria, inhibits electron transport, metabolic acidosis Antidote: deferoxamine
36
Chlorinated aromatic hydrocarbons (Dioxin)
chloracne, porphyria, liver damage, CNS dysfunction & impaired reproduction induces enzymes via arylhydrocarbon receptor. Mimics estrogens. No specific antidote: give Cholestyramine (removes bile acid needed for toxin reabsorption)
37
Paraquat
herbicide. Dyspnea, nonproductive cough, hypoxic symptoms, pulmonary infiltrates & lung fibrosis. Redox cycle: converts O2 into toxic radicals which cause lipid peroxidation, cell death, inflammation. 100% oxygen is contraindicated. Treatment: serial activated charcoal, hemoperfusion
38
Warfarin & superwarfarin toxicity
Rat poison GI bleeding, hematuria, epistaxis, ecchymoses, increased PT, decreased Hb Blocks Vitamin K epoxide reductase by competing with vitamin K Antidote: Vitamin K.
39
Cyclophosphamide & allopurinol
Allopurinol decreases CYP-450 activity and increases the toxicity of cyclophosphamide. therapeutic adjustment: decrease dose of cyclophosphamide
40
Procarbazine and sympathomimetics or tyramine-containing foods
procarbazine inhibits monoamine oxidase (MAO) which results in elevation of tyramine & norepinephrine. This causes hypertension. The patient should not eat tyramine containing foods while taking procarbazine
41
procarbazine & antidepressents
procarbazine inhibits P-450 and potentiates sedative effects of phenothiazine, barbituates, and narcotics.
42
Methotrexate & salicylate (aspirin) or sulfonamide
salicylate or sulfonamide displaces methotrexate from albumin and inhibits its tubular secretion, increasing toxicity. Leucovorin is used as an antidote.
43
6-mercaptopurine & allopurinol
allopurinol inhibits xanthine oxidase and prolongs half life of 6MP, increasing its toxicity. Decrease the dose of 6-MP to 25%.
44
Alpha 1 receptor
Vasoconstictor, dilates pupils
45
Beta 1 receptor
Increases heart rate
46
Beta 2 receptor
vasodilator/ bronchodilator | smooth muscle relaxant
47
alpha 2 receptor
autoregulator: inhibits NT release (decrease norepinephrine) | decrease heart rate
48
Norepinephrine
alpha-1, beta-1
49
Epinephrine
alpha-1, beta-1, beta-2