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MINE Pharm Semester 1 BASICS > Final PPT > Flashcards

Final PPT Flashcards

1
Q

4 types of permeation

A

1) aqueous diffusion
2) lipid diffusion
3) special carriers
4) endocytosis and exocytosis

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2
Q

pH<pKa

A
  • favors protonated form
  • base = charged
  • acid = uncharged
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3
Q

pH>pKa

A
  • favors unprotonated form
  • base = uncharged
  • acid = charged
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4
Q

therapeutic ratio

A

TD50 / ED50

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5
Q

rational dosing

A

achieve desired beneficial effect with minimal adverse effects

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6
Q

bond strength is ___ proportional to specificity

A

indirectly

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7
Q

flux is ___ proportional to concentration

A

directly

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8
Q

Kd is ___ proportional to drug binding

A

indirectly

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9
Q

drug safety is ___ proportional to the therapeutic index (TI)

A

directly

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10
Q

volume of distribution (Vd) is ___ proportional to the concentration of drug outside of the systemic circulation

A

directly

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11
Q

volume of distribution (Vd)

A

amount of drug/concentration

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12
Q

clearance

A

body’s ability to remove drug

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13
Q

1st order elimination

A

clearance is constant

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14
Q

zero order elimination

A

rate of elimination is constant (think you want a 0 mortgage RATE) and transporters are full

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15
Q

half life

A

time to change the drug concentration to half of that

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16
Q

time to full effective dose

A

about 4 doses

17
Q

what 4 things affect passive diffusion?

A

1) molecular weight
2) pKa
3) lipid solubility
4) plasma protein binding

18
Q

4 basic mechanisms of transmembrane signaling

A

1) direct crossing to intercellular receptor (lipid soluble)
2) enzymatic action mediated by ligand binding (tyrosine kinase activated)
3) ligand gated ion channel (inotropic, nACh-R)
4) G protein receptor (metabotropic)

19
Q

describe desensitization

A

how the cell fixes a covalent bond

beta arrestin phosphorylates –> clattering coated pit –> endocytosis –> either breaks apart and recycled, OR lysosome breaks it all down

20
Q

major drug efflux transporters

A
  • ATP binding cassette or ABC transporters

most common = B, C, G

21
Q

P450 induction

A
  • some drugs enhance synthesis and inhibit degradation
  • decreased drug effect is metabolism deactivates
    increased drug effect if metabolism activates
22
Q

P450 inhibition

A
  • decrease/irreversibly inhibit P450
  • competitive inhibition –> co-administer drugs metabolized by P450
23
Q

6 neuotransmitter classes and drugs in them

A

1) esters (cholinergic, ACh)
2) monoamines (adrenergic, NE/Dopa/5HT; GPCRs)
3) Amino Acids (glutamine - E, GABA - I; ion channels)
4) Purines (adenosine, ATP)
5) Peptides (substance P - pain, endorphins - exogenous opioid)
6) inorganic gases (NO, not stored)

24
Q

sympathetic NS (anatomy)

A
  • needs constant activation
  • thoracolumbar
  • short preganglionic
  • close to spinal cord
25
Q

parasympathetic NS (anatomy)

A
  • activated once
  • brain and sacral spinal cord
  • long preganglionic
  • visceral effector organs
26
Q

adrenergic receptors

A
  • a1 (Gq - phospholipase C), a2 (Gi - AC decreases)
  • b1, b2, b3 (Gs - AC increases)
27
Q

cholinergic receptors

A
  • nicotinic (ion channels)
  • muscarinic (2)
    1) M1, M2, M3 - activates phospholipase
    2) M2, M4 - inhibits AC
28
Q

direct acting adrenergic agonists (7)

A
  • albuterol
  • clonidine
  • dobutamine
  • dopamine
  • epinephrine
  • isoproterenol
  • norepinephrine
29
Q

indirect adrenergic agonist (1)

A

amphetamine

30
Q

both direct and indirect adrenergic agonist (1)

A

ephedrine

31
Q

B agonism in relation to the heart

A
  • direct effects
  • increased CO
  • decreased peripheral resistance
32
Q

CO equation

A

CO = SV x HR

33
Q

5 catecholamines and what receptors they work on

A

1) epinephrine (a 1, a2, b1, b2)
2) norepinephrine (a1, a2, b1)
3) isoproterenol (b1, b2)
4) dopamine (D1-5, high dose = a1, b1)
5) dobutamine (b1)

34
Q

reversible adrenoreceptor antagonists (4)

A

1) phentolamine
2) tolazoline
3) prazosin
4) labetalol

35
Q

1 irreversible adrenoreceptor antagonist

A

1) phenoxybenzamine (formed covalent bond, recovery requires new receptor)

36
Q

B antagonism in relation to the heart and blood vessels

A
  • heart –> negative inotrope and chronotrope
  • BV –> oppose B2 mediated vasodilation (acute = increase PVR; chronic = decrease PVR)
37
Q
A

MINE Pharm Semester 1 BASICS (5 decks)

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