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Intro to Pharmacology > Basics 1 > Flashcards

Basics 1 Flashcards

1
Q

What is Pharmacology?

A

The science concerned with the understanding of interactions b/w chemical substances and living systems

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2
Q

What is medical pharmacology?

A

relates this understanding to human beings and the practice of medicine

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3
Q

Pharmacy

A

deals with the chemical and physical properties of drugs, their formulations and packaging.

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4
Q

What is a drug?

A

any substance that when administered to a living organism, brings about fxnl changes as a consequence of interactions at the molecular level.

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5
Q

What can drugs be?

A

Inorganic
Small/Large organic molecules
Bio-macromolecules
Recombinant proteins, antibodies, polysaccharides, nucleic acids . etc

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6
Q

Drugs can exist as diff types of stereoisomers ?

A

many drugs are administered as a RACEMIC mixture of the drug molecules’s stereoisomer. Typically, only 1 stereoisomer of a drug molecule will be significantly pharmacologically active. INTERACTIONS B/W BIOMOLECULES IS STEREOSPECIFIC

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7
Q

Drug size and molecular weight

A

7(lithium) to over 50K.

100 usually poorlu absorbed and distributed

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8
Q

Drug shape

A

Structural Isomer-same mol. formula, but bonded together in a different order.
May be chain, position, or functional group isomers.
Stereoisomers-same formula and sequece of bonded atoms, but diff 3D shape.
Chiral enantiomers-non-superimposable mirror images. Many receptors/drugs prefer some enantiomers over others. . . most chiral drugs are still provided as RACEMIC MIXTURES b/c it’s expensive to separate.

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9
Q

What is pharmacokinetics?

A 
"what the body does to the drug" Study of fate of drugs once ingested and the variability of drug response in varying patient populations. "ADME"
Absorption
Distribution
Metabolism/biotransformation
Elimination
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10
Q

Routes of administration: What is the local effect?

A

at or near the site of administration

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11
Q

Routes of administration: What is the systemic effect?

A

At site or sites near and distant to site of administration.

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12
Q

What are the 2 broad categories of routes of administration?

A

Enteral and parenteral

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13
Q

What is enteral administration?

A

delivery of drugs via the GI route:
Oral
Sublingual
Rectal

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14
Q

What is parenteral administration?

A 
Delivery of drugs NOT via the GI tact!
Injections
Subcutaneous
Intradermal
Intramuscular
Intravenous
Cutaneous-topical/transdermal
Mucous membrane admin-eyes, nose, ear, vaginally, urethral .etc .anything not taken orally or rectally.
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15
Q

What is Drug absorption?

A

process by which unchanged drug proceeds from the site of admin to the site of measurement w/in the body (systemic circ.)

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16
Q

What is the quantitative measurement of Drug Absorption?

A

Bioavailability

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17
Q

What is bioavailability?

A

the fraction of a drug dose reaching the systemic circulation unchanged when administered by any route. (differs depending on route of admin.

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18
Q

Why is the IV bioavailability of ALL DRUGS 100%?

A

b/c they are injected directly into the blood stream/systemic circulation.

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19
Q

What are the 3 major areas that drugs are distributed to the body?

A

Therapeutic sites of action
Tissue réservoirs
Unwanted sites of action

20
Q

What are therapeutic sites of action?

A

Tissues/organs of the body where you want the drug to go so that it can function as a proper prophylactic, therapeutic, diagnostic agent.

21
Q

What is a tissue reservoir?

A

other tissues/organs of the body where the drug can be stored “DRUG DEPOT”

22
Q

What are unwanted sites of action?

A

tissues/organs where the drug is able to elicit effects that you do not necessarily desire->responsible for adverse effects and toxicities…

23
Q

What is volume of distribution (VD)?

A

Quatitative measurement of drug distribution

24
Q

How does conversion of a drug into different chemical substance effect it?

A

may inactivate the drug, maintain drug activity, or activate the activate the drug

25
Q

What is the major organ and enzyme involved in drug metabolism?

A

Liver! Cytochrome P450 (CYP) enzymes- located in SER of hepatocytes

26
Q

Drug Excretion

A

passing the drug out of the body. Renal excretion is the most important-via urine.
Others include: intestines, lungs,skin, body secretions, etc, gaseous

27
Q

How do you measure drug excretion?

A

Clearance of a drug (CL)

28
Q

Pharmacodynamics?

A 
"what the drug does to the body"
study of effects, actions, and mechanisms of action of drugs:
Receptors
Mediators
Targets
Toxicity
29
Q

Mechanism of action

A

Drugs interact with MOLECULES within tissues and organs, (which causes changes in the tissues/organs) . . not whole tissues/organs.
how the drug works at the molecular level

30
Q

Drug receptor

A

any cell component to which a drug binds to initiate the chain of biochemical events leading to the drug’s observed effects.
Usually cellular bio-macromolecules/proteins:
regulatory proteins,ion channels,cell surface/cytoplamic receptors, enzymes, carrier proteins, and structural proteins.
Note: a single drug may posses more than receptor and may affect them in different ways/diff degrees ie, may be determined by selectivity

31
Q

Via what type of bonds do drugs bind to their receptors

A

NON-covalent bonds:
hydrogen bonds
van der Waals attractions
Ionic bonds
Weaker non-covalent bonds require a better fit, and are reversible.
Covalent bonds/very strong involve less selectivity and an irreversible interaction

32
Q

What are bound drugs? (know these well)

A

Agonist->full and partial
Antagonist
Inverse Agonist

33
Q

What is a full agonist?

A

a drug when bound to its receptor, activates the receptor to produce a maximal response.

34
Q

What is a partial agonist?

A

drug when bound to its receptor, activates the receptor to produce a response below the maximal level

35
Q

What is an antagonist?

A

drug when bound to the receptor, fails completely to produce any activation of that receptor-inibits/blocks/decreases agonist mediated responses of the receptor/ action.

36
Q

What is an inverse agonist?

A

drug that when bound to a constitutively active receptor (display biological activity in absence of any ligand), decreases the basal activity of that receptor.

37
Q

How do bound drugs exert their functions on their receptors?

A

through interaction with ACTIVE SITE/LIGAND BINDING site of a molecule or through direct interaction with an ALLOSTERIC site.

38
Q

In terms of inhibition drug receptors, how do antagonist and inverse agonists function?

A

Irreversible (suicide) inhibition
Competetive inhibition
Non-competetive inhibition
Uncompetetive inhibition

39
Q

What is pharmacological action?

A

the functional or physiological modifications caused by the drug’s interaction with its receptor(s)->leads to pharmacological effect

40
Q

What is pharmacological effect?

A

the observed effect which has been produced by the drug

41
Q

What is an example of a mechanism of action?

A

Drug X functions as a full agonist of cardiac beta-receptors

42
Q

What is an example of pharmacological action?

A

Drug X increases the freq of spontaneous depolarizations of the SA node of the heart.

43
Q

What is an example of pharmacological effect?

A

Drug X induces tachycardia.

44
Q

What is toxicology?

A

studies the adverse effects of drugs, the mechanisms of these effects , and the conditions that surround these effects.

45
Q

What are contraindications and precautions?

A

A condition which makes the use of a particular inadvisable.
Absolute contraindication:absolutely inadvisable
Relative contraindication: somewhat inadvisable, but does not rule it out (PRECAUTION)
Often seen in anti-psychotics or seizure medicine that can harm the fetus.

46
Q

What are congeners & “me too” drugs?

A

Drugs that are similar to a drug that already exist. ie, just has an extra hydroxyl group.

Intro to Pharmacology (4 decks)

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