semester 1 Flashcards

1
Q

Pharmacokinetics

A

study of how the body affects the drug

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2
Q

4 phases

A

Absorption
Distribution
Metabolism
Excretion

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3
Q

Law of mass action

A

states that the rate of chemical reactions I proportional to the concentration of reacting substances
D+R=DR RT=R+DR

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4
Q

Emax model

A

Emax{D}/EC50+{D}

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5
Q

Therapeutic index

A

TC50/EC50

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6
Q

Pharmacological effect

A

depends on:
active molecule reaching active site
adequate conc at the active site

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7
Q

Enteral administration

A

drug administration via the GI tract e.g.

oral,rectal,sublingual,buccal,nasogastric,nasojejunal,gastrostomy and jejunostomy

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8
Q

Enteral factors

A

Concentration Lipid solubility
Formulation Molecular size
Gastric contents Blood supply

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9
Q

GI tract

A

consists of mouth, oesophagus, stomach, intestines and anus

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10
Q

First pass metabolism

A

when a drug administered via enteral route travels to the liver and its concetration decreases before it reaches systemic circulation

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11
Q

Parenteral administration

A

administration by any other than via Gi tract e.g.

intramuscular(90),intravenous(20),subcutaneous(45), intradermal(5-10)

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12
Q

Bioavailability(F)

A

Its the fraction of drug which reaches systemic circulation unchanged, Iv has a an F of 1/100%
ER-some lost due to first pass metabolism,
F=AUC oral/AUC Iv

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13
Q

Bioavailability(F) factors

A

1)Drug factors 2)Patient factors
Concentration Blood supply
Formulation Motility
Molecular size Absorption surface
Gastric content
Bile

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14
Q

Formulation

A

the process where different chemical substances including the active drug are combined to give a medicinal product

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15
Q

Active ingredient

A

any component of active drug that intends to furnish pharmacological activity

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16
Q

Drug product

A

finished dosage for e.g. tablet

17
Q

Active transport

A

movement of substances against a concentration gradient from an area of low con to an area of high conc, using ATP

18
Q

Facilitated diffusion

A

movement of substances down a conc gradient using a carrier protein

19
Q

Pinocytosis

A

cells engulf liquid droplets by forming vesicles

20
Q

Diffusion

A

movement of substances down a concentration gradient

21
Q

Weak acids

A

Proton donors

HA–>H++A-

22
Q

Weak bases

A

proton acceptors

B+H+–>BH+

23
Q

Pka

A

50% ionised, 50% unionised (drug)
Ka=[H][Weak base]/[weak acid]
pH=pka+log(A/HA) pr pH=pka+log(B/BH)

24
Q

Topical administration

A

1) Local effect- drug applied to the localised area on body surface to prevent systemic side effects ( creams, ointments, sprays and drops)
2) Systemic effect- drug applied to the body surface to provide an alternative route into blood (nicotine patch)

25
Lipophilic
Utilises intracellular route Can dissolve in oils and fats e.g.ointments
26
Hydrophilic
Utilises intracellular route Attracted and tend to dissolve in water e.g. creams
27
Transdermal application
delivered via the skin for systemic distribution (enter blood) e.g patches
28
Solute carriers
Group of membrane transport proteins: uniporter, symporter and antiporter Organic anion transporter(OAT)- weak acid drugs Organic cation transporter(OCT)-Weak based drugs
29
ATP binding cassettes
They are a transport system superfamily: efflux pump nad p glycoprotein use ATP
30
ACIDIC DRUGS
Highly IONISIED in alkali pH
31
BASIC DRUGS
Highly IONISED in acidic pH
32
Bound drugs
can bind to plasma proteins.lipids and bone. However, they remain in the blood, unable to have an effect and cannot be metabolised or excreted Act as a reservoir when unbound drugs are metablised they can be freed
33
Half-life
the time taken for a drug to reach half its concentration
34
Protein binding factors
the affinity of the drug to binding sites Drug concentration Plasma protein concentration
35
Albumin
most important plasma PROTEIN FOR DRUG BINDING Negatively charged, binds to the acidic drug High affinity for acidic drugs but has low capacity
36
Volume of distribution
Its the apparent volume of drug that disperses in order to produce observed plasma concentration VD=amount of drug in body (g)/ Plasma conc of drug(g/l)
37
VD factors
1)Drug factors 2)Patient factors plasma binding Age tissue binding SEX size Body muscle charge Level of hydration pka Water distribution lipo/hydrophilic