NCMA 216: PRELIM Flashcards by Jannah Michellaine C. Cristobal

In PHARMACOKINETIC PHASE, when drug is taken by mouth, it undergoes 3 phases. What are these phases?

Pharmaceutical/dissolution
Pharmacokinetics
Pharmacodynamics

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In PHARMACEUTIC PHASE, _________ is the breakdown into smaller parts

Disintegration

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In PHARMACEUTIC PHASE, ________ is the further breakdown into smaller parts in GIT-absorption; dissolve into liquid

Dissolution

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PHARMACEUTIC PHASE

TABLET → DISINTEGRATION →
DISSOLUTION

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the 1st phase of drug action.

DISSOLUTION

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___________ is the time it takes the drug to disintegrate and dissolve to become available for the body to absorb it

Rate of dissolution

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are not 100% drug.

Tablets

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excipients

Eillers and inert substances

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Allow drugs to take on particular size and shape and to enhance drug dissolution.

EXCIPIENTS

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Tablet Excipients Formula

Tablet Excipients = Tablets - Drug substance(s)

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are the acidity of the stomach

Gastric ph

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Normal gastric pH

1.5-3.5

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Young/elderly acidity ph

above 3.5

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liquids more absorbed than solid, already in solution, rapidly available for GI absorption

Form of drug ( LIQUID VS. SOLID) -

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resist disintegration in gastric acid

Enteric coated drugs

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Disintegration occurs only in

alkaline environment (intestine)

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interfere with dissolution & absorption, enhance absorption of other drugs, may be protectants of gastric mucosa

Presence of food

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Process of drug movement throughout the body that is necessary to achieve drug
action.

PHARMACOKINETICS

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A drug taken orally is dissolved in the _________ and absorbed in the _________

STOMACH, SMALL INTESTINE

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Passive diffusion across cell membrane
By ____________ through
the spaces between cells
By ___________ of small drug
containing membrane vesicles
through cells, or by the action of drug transporter proteins

Paracellular Transport
Endocytosis

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4 Process

● Absorption
● Distribution
● Metabolism: biotransformation
● Excretion: elimination

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Physiological factors controlling the rate and reliability of drug absorption:

Blood flow to absorbing
site

Total surface area for
absorption

Time of arrival and
contact time at
absorption site

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Physico-chemical factors controlling the rate and reliability of drug absorption:

solubility

Chemical stability

Lipid to water partition
coefficient

Degree of ionization

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Movement of drug particles from GIT to body fluids involve 3 processes:

Passive transport
Pinocytosis
Active Transport

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drugs move across the cell membrane from an area of higher concentration to one of lower concentration.

Diffusion

passive transport - requires a carrier such as enzyme or protein to move the drug against a concentration gradient. This does not require energy.

Facilitated diffusion

is the process by which cells carry a drug across their membrane by engulfing the drug particles in a vesicle.

Pinocytosis

requires energy to facilitate the transport of drug molecules against a concentration gradient, which usually occurs at specific sites in the small intestine

Active Transport

process by which drug becomes available to body fluids and tissues. and is the movement of the drug from the circulation to body tissues.

DISTRIBUTION

Factors affecting drug distribution

● Size of the organ ● Blood flow ● Solubility

or biotransformation is the process by which the body chemically changes drugs into a form that can be excreted

DRUG METABOLISM

Drug given orally may be metabolized by the liver before they reach the systemic circulation

FIRST PASS METABOLISM

Often abbreviated as CYP. Abundant in the liver and different types metabolizes different drugs

CYTOCHROME P450 ENZYMES

Metabolize drugs through a variety of processes:

○ Oxidation ○ Hydrolysis ○ Hydroxylation

is the time it takes for the amount of drug in the body to be reduced by half.

Drug half-life

time it takes for one half of drug concentration to be eliminated

Half-life/ Elimination half-life (t ½)

given several times a day (ex.Penicillin G)

Short t1/2= 4-8 hrs

given 2x or 1x/day (Ex. Digoxin)

Long t ½ = >12 hours

removal of the drug from the body. Drug is changed into an inactive form and excreted by the body.

DRUG EXCRETION

Almost all drugs are filtered by the ______________.

glomerulus

The protonated form of a weak acid is the neutral, more ____________ form

lipid-soluble

are well absorbed in the stomach because they are uncharged at stomach pH.

Weak organic acids

are better absorbed in the intestines where the pH is higher.

Weak bases

● study of the effect of drugs on the body ● Drugs act within the body to mimic the actions of the body's own chemical messengers.

PHARMACODYNAMICS

● how avidly a drug binds its receptor or how the chemical forces that cause a substance to bind its receptor. ● drug's desire to connect to an open receptor ● It refers to how much attraction there is between a drug and a receptor, like a magnet to metal.

DRUG AFFINITY

refers to the drug's ability to activate the receptor once it has bound to it

DRUG EFFICACY

the point at which increasing a drugs dosage no longer increases the desired therapeutic response.

Maximal efficacy

refers to the amount of drug needed to elicit a specific physiologic response to a drug.

POTENCY

describes the relationship between the therapeutic dose of a drug (ED50) and the toxic dose of a drug (TD50)

THERAPEUTIC INDEX (TI)

The higher the therapeutic index – the drug is more ___________ to give.

safe

Therapeutic Index Formula

Therapeutic Index = TD50 / ED50

is the time it takes for a drug to reach the minimum effective concentration (MEC) after administration.

ONSET

occurs when it reaches its highest concentration in the blood/plasma concentration. T0- T2

PEAK

● is the length of time the drug exerts a therapeutic effect. ● period from onset until the drug effect is no longer seen. T1-T3 (trough level)

DURATION OF ACTION

Certain portion of drug molecule (active site) selectively combines with some molecular structure (reactive site) on the cell to produce a biologic effect

DRUG-RECEPTOR INTERACTION

drugs act at specific areas on cell membranes; react with certain chemicals to cause an effect within the cell

RECEPTOR SITE

● a specific chemical (key) approaches a cell membrane and finds fit (the lock) at the receptor site- affects enzyme systems within cells producing certain effects. ● Drug+Receptor=Effect

“LOCK AND KEY THEORY”

Drug Response may be: __________ always desirable/ physiologic effects

Primary

Drug Response may be: __________ desirable or undesirable

Secondary

increased the rate of cell activity/ secretion from the gland.

Stimulation

decreased rate of cell activity / secretion from the gland.

Depression

Interfere with bacterial cell growth

inhibition/Killing of Organism

Laxativeirritate the inner wall of colon---increased peristalsis---increased defecation

Irritation

2 drugs with similar actions are taken for a doubled effect

ADDITIVE EFFECT: 1+1=2

combined effect of 2 drugs is greater than the sum of the effect of each drug given alone;

SYNERGISTIC: 1+1=3

when one drug does not elicit a response on its own but enhances the response to another drug.

POTENTIATION: 0+1=2

means we can often predict these reactions from our knowledge of the pharmacodynamic properties of a drug.

TYPE A: AUGMENTED

sometimes called an adverse drug event–ADE

ADVERSE DRUG REACTIONS (ADR)

one drug inhibits the effect of another drug

ANTAGONISTIC: 1+1=0

study of ADRs is called _________. It is a response to a drug which is noxious and unintended.

PHARMACOVIGILANCE

where the reaction is wholly unexpected and could not be predicted from the pharmacodynamic properties of the drug

TYPE B: BIZARRE

● Response to patient’s immunological system to the presence of the drug ● Do not occur unless the patient has been previously exposed to the agent/ chemical related compound ● Occurs when the patient is first exposed to the drug

ALLERGIC REACTION

The degree to which a drug can be poisonous and thus harmful to the human body.

TOXICITY

Unintentional responses as a result of medical treatment

IATROGENIC RESPONSES

Ototoxic Drugs

● Aminoglycosides ● Diuretics ● Antimalarials ● Anticancer drugs ● Analgesics ● Miscellaneous

nerves that branch off from the spinal cord and extend to all parts of the body.

PERIPHERAL NERVOUS SYSTEM

brain and spinal cord.

CENTRAL NERVOUS SYSTEM

○ Voluntary ○ Skeletal muscles and sensory information. ○ Carry messages from the outer areas of the body

SOMATIC NERVOUS SYSTEM

sensory neuron

Afferent

motor neurons

Efferent

○ Involuntary physiologic processes ○ cardiac and smooth muscles ○ glandular secretions

AUTONOMIC NERVOUS SYSTEM

NCMA 216: PRELIM Flashcards

(81 cards)