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NAPLEX > Pharmacokinetics And Drug Formulations > Flashcards

Pharmacokinetics And Drug Formulations Flashcards

0
Q

What’s Pharmacodynamics (PD)?

A

Refers to effects of drugs on patients body (MOA)

Also used to explain effect of drug on organism eg bacterioSTATIC or bactericidal

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1
Q

What’s pharmacokinetics?PK

A

Study of time course of drug absorption, distribution, metabolism and excretion

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2
Q

Types of drug admin sites?

A

Intravascular admin

Extravascular admin

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3
Q

What’s Intravascular admin?

A

Where drug is placed directly into the blood either intravenously or intra-arterially

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4
Q

What’s extravascular admin?

A

Oral, sublingual, buccal, IM, SC, dermal, pulmonary, topical ocular, intraocular and rectal

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5
Q

Is there drug absorption when drug is admin intravascular admin?

A

No! (Drug is placed directly into systemic circulation)

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6
Q

What’s dissolution?

A

Oral dosage form dissolving in GI tract and drug is released from the dosage form

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7
Q

Why’s protective coating used in some drugs?

A

To limit drug degradation, which occurs primarily by hydrolysis

By preventing drug dissolution in acidic gut medium, but permits dissolution in basic medium of intestine

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8
Q

How is dissolution rate increased in drug with poor absorption?

A

To reduce particle diameter, which increases the surface area

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9
Q

What describes rate of dissolution?

A

Noyes-Whitney eqn

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10
Q

What determines rate and extent to which drug dissolves in GI fluid?

A

Solubility of drug

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11
Q

T/F? Only dissolved drug is absorbed into the body?

A

T

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12
Q

How does systemic absorption occur?

A

Passive diffusion - across gut wall

Active transport - via transport proteins

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13
Q

When does passive diffusion occur?

A

When there’s a high conc of drug in gut lumen and it moves to equalize drug conc (reach equilibrium) across the gut wall

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14
Q

Whats bioavailability?

A

Extent to which a drug is absorbed into systemic circulation

% of drug absorbed from extravascular admin RELATIVE TO intravascular admin

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15
Q

Howz bioavailability calculated?

A

Using Area under the plasma conc time curve (AUC)

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16
Q

How do u calculate absolute bioavailability (F)?

A

F (%) = 100 x (AUCextravascular/AUCiv) x (DOSEiv/DOSEextravascu)

17
Q

What properties determine how drugs distribute evenly throughout the body?

A

Lipophilicity

Molecular weight

Solubility

Ionization status

Extent of protein binding

18
Q

What’s the primary protein in the body?

A

Albumin

19
Q

What’s the vol of distribution (V or Vd)?

A

How large an area in the pts body the drug has distributed into & is based on properties of that drug

Amt of drug in the body to conc of drug measured in plasma or serum

20
Q

Formula of Vd?

A

Vd = amt of drug in body/ conc of drug in plasma

Conc of drug in body = amt of drug remaining in body x vol parameter

21
Q

Vd formula in bolus IV injection?

A

Vd = dose/Co

22
Q

Vd formula following oral dose?

A

Vd = (F x Dose)/(Kel x AUC)

F = bioavailability
Kel = terminal elimination rate constant
AUC = area under plasma conc-time curve
23
Q

What’s clearance?

A

PK parameter that converts a conc of drug in the body to an amount eliminated per unit time

Rate of elimination = Cl x Conc

24
Q

What’s half-life?

A

Time req for drug conc (and drug amt) to decrease by 50%

25
Q

Half-life formula?

A

t1/2 = 0.693/Kel

Kel = Cl/Vd

26
Q

What’s steady state?

A

When drug accumulates until it reaches steady state where the rate of drug up intake equals the rate of drug elimination

27
Q

Apparent clearance formula?

A

CL/F = dose/AUC

28
Q

What’s first-order kinetics?

A

Amt of drug given is proportional to the increase seen in plasma conc

29
Q

What’s Michaelis-Menten kinetics?

A

Begins as first-order, but when metabolism becomes saturated, the conc increases rapidly.

Drugs with this type of kinetics begin as first-order kinetics, but can change to zero order once a certain dose is reached and metabolizing enzymes are saturated

30
Q

What’s zero order elimination?

A

The elimination rate is independent of the drugs conc

Toxicity can occur here e.g. PHT, theophylline and Voriconazole

31
Q

In saturable kinetics, whats the effect of a small dose on drug conc?

A

A small increase in dose may result in a large increase in drug conc

32
Q

Should long-acting formulations be ground up, if pt has difficulty swallowing?

A

No!

33
Q

Whats a way to mitigate nausea from meds?

A

It may be easier to tolerate if it comes as dissolving form

Many drugs that cause stomach come in long-acting formulations

34
Q

Do patches bypass oral route?

A

Yes

35
Q

Sublingual (SL) formulations bypass the oral route?

A

T

Works faster

36
Q

Advantages of long-action formulations?

A

SE occur less readily as less drug is available to interact with wrong receptor

37
Q

What name or -ending indicated controlled release (other than abbreviations XR, ER, LA, SR, CR, CRT, SA, TR, TD)?

A

-cont

E.g. For controlled release opioids - ms CONTin or oxyCONTin

38
Q

Do u usually cut patches? Exceptions?

A

No!

Lidoderm is only patch that can be cut

39
Q

Should patch be exposed to heat (from fever or electric blanket or heating pad)?

A

No!

This causes more drugs to be released and could result in toxicity

40
Q

What can be done about patch irritating skin?

A

Is pt alternating application site

No shaving immediately b4 application

Topical steroid eg Hydrocortisone (OTC) can be applied to skin AFTERWARDS

41
Q

Which patches need to be removed b4 MRI?

A

Testosterone (Androderm)

Clonidine (Catapress-TTS)

Fentanyl (Duragesic, generics)

Rotigotine (Neurpro)

Scopolamine (Transderm Scop)

Salon Pas Power (OTC)

Nicotine (NicoDerm CQ)

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