MT1 Flashcards

1
Q

Volume of Distribution (Vd)

A

Vd = dose of drug / measured conc.

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2
Q

Half Life

A

t1/2 = (0.693*Vd) / CL (clearance)

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3
Q

Factors affecting Distribution

A
  1. organ blood flow
  2. molecular size ex. heparin
  3. lipid solubility (*brain)
  4. plasma protein binding (10-99%)
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4
Q

Metabolism

A

Liver via 2 processes:
Phase 1: Biotransformation
*oxidative / reductive / hydrolytic rxns –> P450 (CYP) monooxygenase system
Phase 2: conjugation rxns –> liver enzymes

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5
Q

Metabolism Phase II

A

commonly added molecules
- glucuronic acid
- sulfate
- carboxylic acid

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6
Q

Excretion (kidney - renal)

A
  1. passive glomerular filtration
  2. active tubular secretion
  3. passive tubular reabsorption (urine pH is key)
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7
Q

Excretion (bile)

A

Liver –> intestine via common bile duct
- larger drugs
- conjugated metabolites
(carrier mediated process)

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8
Q

Viral Replication

A

APURAR

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9
Q

Covid-19 virus

A
  • ssRNA
  • 125nm diamter
  • genomic proofreading mech.
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10
Q

RDRP inhibitors

A
  • remdesivir
  • ribavirin
  • favipiravir

MOA: RDV-TP resembles ATP and competes w the nucleotide during viral RNA synth. RDV-TP forms phosphodiester bond w next nucleotide

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11
Q

MIC vs MBC

A

MIC: lowest conc. of antibiotic that inhibits visible growth of a microorganism after overnight incubation
MBC: min bacteriocidal conc.
MBC:MIC
- less than or equal to 4 is bacteriocidal
- over 4 is bacteriostatic

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12
Q

b- lactam antibiotics

A

Penicillin
MOA: inhibits synth of bacterial PG cell wall

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13
Q

Macrolides (antibiotic)

A

Azithromycin (product of actinomycetes)
MOA: inhibits bacterial protein synth by binding reversibly to 50S ribosomal subunit

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14
Q

Aminoglycosides (antimicrobial)

A

Gentamicin
MOA:
- interferes w bacterial protein synth by irreversibly binding 30 and 50S subunits
- creates fissures in outer membranes of bacteria

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15
Q

Tetracyclines (antimicrobial)

A

Doxycycline
MOA:
- inhibits bacterial protein synth by binding REVERSIBLY to 30S subunit (and possibly 50S)
- cause changes in cytoplasmic membrane

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16
Q

Sulfonamides (antimicrobial)

A

Sulfamethoxazole
MOA: interferes w folic acid synth by inhibiting dihydropteroate synthetase and prevents addition of para-aminobenzoic acid (PABA) into folic acid

17
Q

Quinolones (antimicrobial)

A

Ciprofloxacin
MOA: inhibits DNA gyrase/ topoisomerase

18
Q

Glycopeptides (antimicrobial)

A

Vancomycin
MOA: inhibits cell wall synth in gram + bacteria by binding to the D-alanyl-D-alanine terminus of cell wall precursor units

19
Q

Oxazolidinone (antimicrobial)

A

Linezolid
MOA: inhibits protein synth by binding at the P site of the 50S ribosomal subunit

20
Q

TNM classification of solid tumours

A

T: extent of primary tumour (size)
N: presence/absence and extent of regional lymph node metastasis
M: presence/absence of distant metastasis

21
Q

Chemotherapy

A

MOA: damage DNA/ interfere with DNA synthesis
- phase specific vs nonspecific agents
- most cytotoxic to cells w high growth fraction

22
Q

Akylating agents (chemotherapy)

A

Cyclophosphamide
MOA: bind DNA by creating covalent bonds that cross-link DNA –> prevents unwinding of DNA –> decreased protein synth.

23
Q

Epipodophyllotoxins (chemotherapy)

A

Etoposide
MOA: inhibits topoisomerase II, inhibits DNA synth.

24
Q

Taxanes (chemotherapy)

A

Docetaxel
MOA:
- promotes assembly and stabilization of microtubules (prevents cell replication)
- may also inhibit angiogenesis (blood vessel formation)

25
Q

Antimetabolites (chemotherapy)

A

5-Fluorouracil (5-FU)
MOA:
- resemble naturally occurring nuclear structural components
- incorporate into DNA or RNA
- may also inhibit enzymes involved in synthesis of DNA or proteins (ex. polymerase)

26
Q

Antitumour antibiotics (chemotherapy)

A

Doxorubicin
MOA:
- insert bw DNA base pairs, uncoil DNA, inhibit synth
- may also inhibit polymerase

27
Q

Alkylating agent + antitumour antibiotic

A

Streptozocin
- naturally occurring methylnitrosurea
- specific for b and exorine cells of pancreas due to an attached sugar moiety
MOA: undergoes spontaneous decomp. –> reactive methylcarbonium ions –> alkylate DNA –> interstrand cross links –> inhibits mitosis

28
Q

Camptothecins (chemotherapy)

A

Irinotecan
MOA: bind topoisomerase I, prevents religation of DNA strand
- results in cell death

29
Q

Vinka Alkaloids (chemotherapy)

A

Vincristine
MOA: prevent polymerization of tubulin to form microtubules
- induce depolymerization of formed tubules
- inhibits mitosis

30
Q

Targeted Therapy

A

Monoclonal antibodies
ex. Trastuzumab (Herceptin): Anti-HER2 (breast cancer cells)

31
Q

Endocrine therapy

A

Aromatase inhibitors
ex. Letrozole

32
Q

Catecholamines

A
  • dopamine
  • NE
  • epinephrine
    (all synth. from tyrosine)