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Memory test > bases of pharm > Flashcards

bases of pharm Flashcards

1
Q

define affinity

A

effectivness of binding

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2
Q

define intrinsic efficacy

A

response to ligand binding

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3
Q

what is potency

A

affinity+intrinsic efficacy

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4
Q

what is Bmax

A

maximum bining capacity => limited by receptor number

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5
Q

What is Kd

A

concentration of ligand required to occupy 50% of receptors, higher the value the less effective is the drug

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6
Q

define EC50

A

50% of maximum response potency affected by receptor number, potency and ability to mediate a response

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7
Q

define E max

A

maximum response

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8
Q

define IC 50

A

concentration that inhibits 5 0% of response

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9
Q

define oral bivelence

A

Proportion of drug given orally /or any other rout (not IV) that reaches circulation unchanged

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10
Q

What’s LD/TD 50 and ED 50

A

LD50 => maximum total dose (lethal)

ED50 => maximum effective dose (effective)

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11
Q

define volume of distribution

A

Theoretical volume into which drug is distributed if this occurred instantaneously’

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12
Q

why bis pH of urin important in drug elimination

A

weak acids eliminated better with alkaline urine and opposit true, nit reabsorbed

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13
Q

define pharmacokinetics

A

what body does to the drug

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14
Q

define pharmacodynamics

A

what drug does to thebody

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15
Q

what is the difference between eneteral and paraenteral drug delivery

A

enteral =through GI (oral, sublingunal, rectal)

paraenteral=not through GI (IV, IM, transdermarl, subcutenous intrathecal)

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16
Q

what factors affect drug absorption

A

pasive: lipid solubility, pH, size
active: active transport system, splanchnic blood flow, drug distruction

17
Q

what factors affcte biopvelence

A

age, food (less important with hydrophylic), vomiting, malabsorption, first pass metabolism

18
Q

first pass metabolism give examples

A

any metabolism that occurs before drug enters the circulation
GI => acid, proteolytic enzymes, eflux pump
Liver

19
Q

define distribution + examples

A

spread of drug around the body depdnednt on
water/fat solubility
protein binding tissue and blood
density of binding sites and mass of tissue

20
Q

what are the different protein types that bind drugs and what kinds of drugs do they bind

A
  1. Albumin =>Acidic drugs
  2. Globulins =>Hormones
  3. Lipoproteins and Acid Glycoproteins =>Basic drugs
21
Q

When is protein binding of high significance

A

narrow theraputic window, high protein binding, low volume of distribution

22
Q

what can affcet drug protein binding

A

hypoalbuminuria, pregnancy, renal failure, other drugs

23
Q

how is volume of distribution (Vd) calculated

A

total amount of drug in the body/plasma drug concentration at time 0

24
Q

where dose drug distribiut to and what deteremins that distribution

A

intracellular anmd extracellular compartments (apparent volume) and plasma => dependent on lipid solubility and transporters

25
Q

What does Vd indicate

A

Vd =5l => drug in blood
Vd = 15 => drug in extracellular fluid and plasma
Vd > 15l => drug in intracellular

May also have higher Vd if tissue bound i.e. anaesthetics and adipsoe tissue

26
Q

What processes are active in phase 1 metabolism and what is the enzyme involved

A

Cytochrom P450 => hydroxylarion, reduction, oxydation

27
Q

name some incuces of Cytochrom P450

B.S CRAPS

A 
Phenytoin
Carbamazepine
Barbituates
Rifampicin
Alcohol (Chronic)
Sulphonylureas & St. John’s Wort
28
Q

name some inhibitors of Cytochrom P450

I AM SECS GOD

A 
Grapefruit Juice
Omeprazole
Disulfiram
Erythromycin
Valporate
Isoniazid
Cimetidine & Ciprofloxacin
Ethanol (Acutely)
Sulphonamides
Metronidazol
29
Q

what is the purpose of phase 1 and 2 of metabolism

A

1 increase recativity

2 conjugation to water solluble compound

30
Q

What are the 3 molecules used in phase 2 conjugation, what are the cofactors

A

Glucoronic acid, sulphayte ions, glutathion

cofactor, uridine diphosphate glucuronic acid (UDPGA).

31
Q

What factors affect elimination

A

renal blood flow, filtrate pH, plasma protein binding, lipid solubility, organic cations/anions,

32
Q

define clearance

A

The volume of plasma that is completed cleared of drug per unit time (sum of hepatic and renal)

33
Q

what is teh equation for clearnce

A

Clearance=(Amount in urine × Urine flow rate)/(Arterial Plasma Concentration)

34
Q

what factors affct clearnce

A

heart => output
renal=> renal elimination
hepatic=> hepatic elimination

35
Q

what is the equation for half life

A

Half Life= (0.693 × Volume of Distribution)/Clearance

36
Q

what is the link between Kd and kinetics

A

1st order => drug concentration close to Kd

0=> drug concentration much higher than Kd

37
Q

how is loading dose calculated

A

Loading Dose (Dose L)= Vd ×Steady State Concentration in Plasma (CpSS)

38
Q

what drug enhances actions of penicillin by reducting tubular excretion
gibve another genearl example

A

probenecid

NSAIDs

Memory test (11 decks)

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