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PCOL > MODULE 1 > Flashcards

MODULE 1 Flashcards

1
Q

the body of knowledge concerned with the action of chemicals on biologic systems.

A

PHARMACOLOGY

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1
Q

The study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal body processes.

A

PHARMACOLOGY

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2
Q

The science of substances used to prevent, diagnose, and treat disease.

A

MEDICAL PHARMACOLOGY

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3
Q

The branch of pharmacology that deals with the undesirable effects of chemicals on living systems, from individual cells to humans to complex ecosystem.

A

TOXICOLOGY

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4
Q
  • the science of medical use of drugs
  • was developed as the precursor to pharmacology
A

THE MATERIA MEDICA

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5
Q

developed the methods of experimental physiology and pharmacology

A

FRANCOIS MAGENDIE
CLAUDE BERNARD

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5
Q

the use of drugs in the treatment of disease, which is a development from the ancient practice of “____” and spirits in attending to sick

A

SHAMANS

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6
Q

The latest development was on

A

PHARMACOGENOMICS

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7
Q

It is the relation of the individual’s genetic makeup to his or her response to specific drugs.

A

PHARMACOGENOMICS

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8
Q

Short nucleotide chains called ____, were synthesized to be complementary to natural RNA or DNA

A

ANTISENSE OLIGONUCLEOTIDES (ANOs)

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9
Q

It may be defined as any substance that brings about a change in biologic function through its chemical actions

A

DRUG

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10
Q

DRUG MAY INTERACT AS AN:

activator of a specific molecule

A

AGONIST

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11
Q

DRUG MAY INTERACT AS AN:

inhibitor of a specific molecule

A

ANTAGONIST

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12
Q

DRUG MAY INTERACT AS AN:

“the target molecule” for drug

A

INTERACTS WITH THE RECEPTOR

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13
Q

A drug may be synthesized within the body

A

HORMONES, ENDOGENOUS

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14
Q

A drug may be chemicals not synthesized in the body

A

XENOBIOTICS “ STRANGER”, EXOGENOUS

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15
Q

refers to a drug that have almost exclusively harmful effects.

A

POISON

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16
Q

The ____ of the drug makes the poison (Paracelsus)

A

DOSE

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17
Q

Another similar term for poison which refers to poison of biologic origin and is usually synthesized by plants or animals

A

TOXIN

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18
Q

To achieve selective binding, the drug molecule should be at least ____ units in size.

A

100 MW

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19
Q

Drugs with MW greater than 1000 ____ between compartments, so must be administered directly into the compartment where they have their effect.

A

DO NOT DIFFUSE READILY

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20
Q

MAJOR TYPES OF DRUG-RECEPTOR CHEMICAL FORCES/BONDS

  • very strong; not reversible.
  • Example: Aspirin (acetyl group) and cyclooxygenase
A

COVALENT

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21
Q

MAJOR TYPES OF DRUG-RECEPTOR CHEMICAL FORCES/BONDS

  • weaker than covalent
  • vary from relatively strong linkages between permanently charged ionic molecules to weaker hydrogen bonds and very weak induced dipole forces
A

ELECTROSTATIC

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22
Q

MAJOR TYPES OF DRUG-RECEPTOR CHEMICAL FORCES/BONDS

usually quite weak; it is the interaction of highly lipid-soluble drugs with the lipids of the cell membrane

A

HYDROPHOBIC

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23
Q

MAJOR TYPES OF DRUG-RECEPTOR CHEMICAL FORCES/BONDS

HYDROPHOBIC:
* Certain drugs exhibit chirality (stereoisomerism) such as ____
* Its (S)(-) isomer is a potent beta blocker while the (R)(+) isomer is a hundred-fold weaker at the beta receptor.

A

CARVEDILOL

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24
Q

MAJOR TYPES OF DRUG-RECEPTOR CHEMICAL FORCES/BONDS

HYDROPHOBIC:
Carvedilol (S)(-) isomer

A

POTENT BETA BLOCKER

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25
Q

MAJOR TYPES OF DRUG-RECEPTOR CHEMICAL FORCES/BONDS

HYDROPHOBIC:
Carvedilol (R)(+) isomer

A

hundred-fold weaker at the beta receptor

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26
Q

MAJOR TYPES OF DRUG-RECEPTOR CHEMICAL FORCES/BONDS

The (+) enantiomer of ____ is more potent and is less toxic than the (-) enantiomer

A

KETAMINE

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27
Q

TWON DIVISIONS OF PHARMACOLOGY

  • Is the study of how the body absorbs, distributes, metabolizes, and excretes drugs (ADME)
  • What the body does to the drug
A

PHARMACOKINETICS

K - katawan

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28
Q

TWON DIVISIONS OF PHARMACOLOGY

  • Describes the action of drugs
  • It includes the measurement of responses to drugs and how response relates to drug dose or concentration
  • What the drug does to the body
A

PHARMACODYNAMICS

D - drug

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29
Q

DISCIPLINES RELATED TO PHARMACOLOGY

  • the study of the use of drugs to treat diseases.
  • The use of drug treatment is to:
  • Cure a disease
  • Delay disease progression
  • Alleviate the signs and/or symptoms of the disease
  • Facilitate nonpharmacologic therapeutic intervention
A

PHARMACOTHERAPEUTICS (PHARMACOTHERAPY)

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30
Q

DISCIPLINES RELATED TO PHARMACOLOGY

is the study of the relationship of genetic factors to variations in drug response

A

PHARMACOGENETICS

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31
Q

DISCIPLINES RELATED TO PHARMACOLOGY

is the study of the cost effectiveness of drug treatments

A

PHARMACOECONOMICS

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32
Q

DISCIPLINES RELATED TO PHARMACOLOGY

is the study of the effect of drugs on population

A

PHARMACOEPIDEMIOLOGY

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33
Q

study of drug’s adverse effects

A

TOXICOLOGY

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34
Q

is the study of a poison, usually one produced by or occurring in a plant or microorganism

A

TOXINOLOGY

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35
Q

study of doses

A

POSOLOGY

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36
Q

study of drug’s manufacture, preparation and dispensing of drugs

A

PHARMACY

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37
Q

is the study of preparing and dispensing drugs

A

PHARMACEUTICS

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38
Q

is the study of the identification and preparation of crude drugs from natural sources

A

PHARMACOGNOSY

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39
Q

the science of drug preparation and the medical use of drugs

A

MATERIA MEDICA

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40
Q

is the application of all principles in pharmacy to humankind

A

CLINICAL PHARMACY

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41
Q

refers to what the body does to a drug. Four properties determine the onset, intensity, and the duration of drug action

A

PHARMACOKINETICS

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42
Q

PHARMACOKINETICS

____ from the site of administration permits entry of the drug (either directly or indirectly) into plasma

A

ABSORPTION

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43
Q

PHARMACOKINETICS

the drug may then reversibly leave the blood-stream and distribute into the interstitial and intracellular fluids.

A

DISTRIBUTION

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44
Q

PHARMACOKINETICS

he drug may be biotransformed by ____ by the liver or other tissues.

A

METABOLISM

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45
Q

PHARMACOKINETICS

the drug and its metabolites are eliminated from the body in urine, bile, or feces.

A

ELIMINATION

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46
Q

The pre-requisite to drugs’ access to the biologic system is the

A

ROUTE OF ADMINISTRATION

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47
Q

Drugs administered via ____ route, gets into the system rapidly and more efficiently than those given via extravascular route.

A

INTRAVASCULAR

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48
Q

Drugs given IV need not undergo ____ since it is administered directly into the systemic circulation.

A

ABSORPTION

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49
Q

A hundred percent (100%) bioavailability is expected once the drug is administered ____

A

INTRAVENOUSLY

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50
Q

For drugs given via extravascular route (oral, peroral, rectal, etc.) need to undergo ____ process (depending on the dosage form used) prior to absorption

A

LIBERATION

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51
Q

Drugs that undergo absorption especially via the GI tract need to be in

A

SOLUTION

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52
Q

The ____ characteristics of the drugs influences its absorption

A

PHYSICOCHEMICAL

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53
Q

For rapid and efficient absorption, the drug must be in

A

SOLUTION

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54
Q

____, ____, ____ drug molecules cross the biologic membrane more rapidly and efficiently than the ionized, more polar moiety

A

SMALL, NONIONIC, LIPOPHILIC

LUNA

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55
Q

Once the drug becomes available in the plasma, ____ follows

A

DISPOSITION

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56
Q

is the process by which drug leaves the systemic circulation and enters the various compartments (tissue compartments)

A

DISPOSITION

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57
Q

The term ____ includes distribution to different organs such as the site of action (e.g. CNS, heart, etc.), liver (for metabolism and excretion) and kidneys (for excretion)

A

DISPOSITION

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58
Q

process that terminates the action of the drug by promoting its clearance

A

DRUG ELIMINATION (metabolism & excretion)

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59
Q

Important Pharmacokinetic Principles

____ properties of drugs are partly responsible for their actions.

A

PHARMACOKINETIC

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60
Q

The ____ characteristics of the drug influences the rate and extent of drug input (liberation and absorption) and output (distribution, metabolism and excretion) processes.

A

PHYSICOCHEMICAL

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61
Q

provides the fundamental concept of the PK characteristics of drugs based on the degree of ionization as influenced by pH.

A

HENDERSON-HASSELBALCH

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62
Q
  • At low pH (acid environment) these are in their unionized form.
  • The unionized form is more lipophilic, thus can cross the membrane rapidly and efficiently through passive diffusion.
  • remain unionized in the acid region of the GIT (stomach), thus optimum absorption occurs in this area.
  • At high pH (basic environment) these become ionized, thus more polar in character.
  • Excretion is favorable when the drug is in its ionized form.
A

WEAK ACIDS

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63
Q

environment in which WEAK ACIDS are in their unionized form

A

low ph
acidic environment

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64
Q

environment in which WEAK ACIDS are in their ionized form

A

high pH
basic environment

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65
Q

the unionized form of weak acids are more ____

A

lipophilic

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66
Q

weak acids in their unionized form can cross the membrane rapidly and efficiently through

LIPOPHILIC

A

PASSIVE DIFFUSION

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67
Q

optimum absorption of weak acids occurs in what area

A

STOMACH

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68
Q

Excretion is favorable when the drug is in its ____ form

A

IONIZED

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69
Q
  • are best absorbed in the alkaline region of the GIT (small intestines) because they are in their unionized form.
  • As mentioned earlier, unionized moiety is nonpolar and lipophilic, so can cross the membranes more efficiently.
  • To promote the excretion of ____, an acid environment (low pH) is desired since it could make alkaline drugs to become more ionized.
  • More ionized form of the drug is polar and less lipophilic (hydrophilic), thus are excretable.
A

WEAK BASES

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70
Q

Weak bases are best absorbed in what area

A

SMALL INTESTINES

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71
Q

To promote the excretion of weak bases, an ____ environment (____) is desired since it could make alkaline drugs to become more ionized.

A

acidic, low pH

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72
Q

an important PK principle that determines the ability of the drug to reach the circulation and be distributed to various organs and reach its site of action.

A

PERMEATION across the membrane

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73
Q

MECHANISMS OF DRUG PERMEATION

The most commonly mechanism involved in drug permeation is

(either through intercellular junctions or through the cell membrane)

A

PASSIVE DIFFUSION

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74
Q

MECHANISMS OF DRUG PERMEATION

Drug permeation is governed by ____ which describes the passive flux of molecules down a concentration gradient (from a region of higher concentration to a region of lower concentration)

A

FICK’S LAW / FICK’S FIRST LAW OF DIFFUSION

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75
Q

MECHANISMS OF DRUG PERMEATION

Some permeation mechanism utilized a ____ system

A

CARRIER-MEDIATED

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76
Q

MECHANISMS OF DRUG PERMEATION

CARRIER-MEDIATED SYSTEM:
The transport system may be an ____ (against the concentration gradient) or ____ (along the concentration gradient) process.

A

ACTIVE, PASSIVE

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77
Q

MECHANISMS OF DRUG PERMEATION

Both ____ and ____ (carrier-mediated) utilized a carrier or transporter to cross the membrane.

A

ACTIVE TRANSPORT & FACILITATED DIFFUSION

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78
Q

MECHANISMS OF DRUG PERMEATION

  • a mechanism of drug permeation.
  • This involves the engulfment of impermeant molecules by the vesicles in cell membrane via endocytosis (pinocytosis or phagocytosis), release into the cell, and expulsion of the material via membrane vesicles (exocytosis)
A

VESICULAR TRANSPORT

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79
Q

MECHANISMS OF DRUG PERMEATION

pinocytosis or phagocytosis

A

ENDOCYTOSIS

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80
Q

MECHANISMS OF DRUG PERMEATION

release into the cell, and expulsion of the material

A

EXOCYTOSIS

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81
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

target of cocaine and some tricyclic antidepressants

A

NET

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82
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

target of selective serotonin reuptake inhibitors and some tricyclic antidepressants

A

SERT

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83
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

target of reserpine

A

VMAT

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84
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

  • increased expression confers resistance to certain anticancer drugs
  • inhibition increases blood levels of digoxin
A

MDR1

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85
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

confers resistance to certain anticancer and antifungal drugs

A

MRP1

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86
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

NET physiologic function

A

norepinephrine reuptake from synapse

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87
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

SERT physiologic funtion

A

serotonin reuptake from synapse

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88
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

VMAT physiologic function

A

transport of dopamine and norepinephrine into adrenergic vesicles in nerve endings

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89
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

MDR1 physiologic function

A

transport of many xenobiotics out of cells

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90
Q

TRANSPORT MOLECULES IMPORTANT IN PHARMACOLOGY

MRP1 physiologic function

A

leukotriene secretion

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91
Q

describes the actions of a drug on the body and the influence of drug concentrations on the magnitude of the response.

A

PHARMACODYNAMICS

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92
Q

Most drugs exert their effects, both beneficial and harmful, by ____ (that is, specialized target macromolecules) present on the cell surface or within the cell

A

INTERACTING WITH RECEPTORS

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93
Q

The drug–receptor complex initiates alterations in biochemical and/or molecular activity of a cell by a process called

A

SIGNAL TRANSDUCTION

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94
Q

is the division of Pharmacology that describes the action of drugs. It includes the **measurement of responses **to drugs and how response relates to drug dose or concentration.

A

PHARMACODYNAMICS

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95
Q

TYPE OF ACTION PRODUCED BY THE DRUG

  • drugs may increase or enhance the function of an organ or a system.
  • Example: Caffeine increases the activity of the CNS that makes us awake or stimulated (energized)
A

STIMULATION

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96
Q

TYPE OF ACTION PRODUCED BY THE DRUG

  • Drugs inhibit or decrease the function of an organ or the system.
  • Alcohol is an example, it decreases the activity of the CNS leading to drowsiness, decrease concentration, affect balance and equilibrium and even decrease memory and learning functions.
A

DEPRESSION

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97
Q

TYPE OF ACTION PRODUCED BY THE DRUG

  • This is an action attributed to local effects of the drug to a tissue or cell.
  • An example of drug that gives this type of action are the stimulant cathartics. Some laxatives promote peristaltic movement by irritating the wall of the GIT causing increase motility and evacuation.
A

IRRITATION

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98
Q

TYPE OF ACTION PRODUCED BY THE DRUG

action of vitamins, minerals, or other supplements

A

REPLACING DEFICIENCY OF AN ESSENTIAL CHEMICAL

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99
Q

TYPE OF ACTION PRODUCED BY THE DRUG

action of anti-infectives and antineoplastics

A

Killing/Weakening invading microorganism/rapidly proliferating cells

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100
Q

Based on the action produced by the drug on a particular system

intended; it is usually the desired effect that leads to its therapeutic use

A

PRIMARY

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101
Q

Based on the action produced by the drug on a particular system

unintended; commonly leading to undesired effects (side effects, adverse drug reactions)

A

SECONDARY

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102
Q

MAJOR MECHANISMS OF DRUG ACTION (MOA)

  • Alter the cell environment by physical or chemical processes
  • Example:
    Ø action of antacid - alters the pH of the stomach
    Ø action of antidotes, e.g., activated charcoal - adsorbs the toxins
A

STRUCTURAL NONSPECIFIC

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103
Q

MAJOR MECHANISMS OF DRUG ACTION (MOA)

  • Alter cell function by **drug-receptor interactions **
  • Majority of drugs’ action is through this mechanism
  • To understand this mechanism, it is important to know the different targets into which drugs are capable of interacting with.
A

STRUCTURAL SPECIFIC

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104
Q

targets for drug action are either ____ or ____

A

PROTEIN OR NON-PROTEIN

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105
Q

Majority of drugs interact with ____ targets such as receptors, ion-channel, enzymes and carrier molecules

A

PROTEIN

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106
Q

DIFFERENT LEVELS OF DRUG ACTION

  • Interaction with drug’s molecular target
  • The drug target (receptor, ion channel, enzyme, carrier molecule)
A

MOLECULAR

106
Q

DIFFERENT LEVELS OF DRUG ACTION

  • Transduction
  • The biochemicals linked to drug target (ion channel, enzyme G protein)
A

CELLULAR

107
Q

DIFFERENT LEVELS OF DRUG ACTION

  • An effect on tissue function
  • Electrogenesis, contraction secretion, metabolic activity, proliferation
A

TISSUE

108
Q

DIFFERENT LEVELS OF DRUG ACTION

  • An effect on system function
  • Integrated systems including linked systems (e.g., NS, CVS)
A

SYSTEM

109
Q

For a drug to produce an action, it must first interact with a ____ within the molecule

A

SPECIFIC TARGET

110
Q

For a drug to produce an action, it must first interact with a specific target within the molecule. This interaction will be followed by a ____ wherein a cellular response is produced.

A

TRANSDUCTION MECHANISM

111
Q
  • Any target molecule with which a drug molecule has to combine in order to elicit its specific effect
  • It is the component of a cell or organism that interacts with a drug and initiates the chain of events leading to the drug’s observed effects.
A

DRUG RECEPTOR

112
Q

is the capacity of a drug to form the complex with its receptor (DR complex), e.g., the key entering the hole of the lock has got an affinity to its levers

A

AFFINITY

113
Q

it is the ability of a drug to trigger the pharmacological response after making the drug receptor complex

A

INTRINSIC ACTIVITY / EFFICACY

114
Q

refers to any molecule which attaches selectively to particular receptors or sites

A

LIGAND

115
Q
  • refers to an agent which activates a receptor to produce an effect similar to that of the physiologic signal molecule.
  • It has both high affinity as well as high intrinsic activity, therefore can trigger the maximal biological response
A

AGONIST

116
Q
  • an agent which prevents the action of an agonist on a receptor but doesn’t have any effect of its own.
  • it has only affinity but no intrinsic activity. this drug binds to the receptor and blocks the binding of an endogenous agonist.
A

ANTAGONIST

117
Q
  • an agent which** activates a receptor** to produce a sub maximal effect but antagonizes the actions of full agonist.
  • it has full affinity but with low intrinsic activity and hence are only partly as effective as agonist.
A

PARTIAL AGONIST

118
Q
  • Agent which activates a receptor produce an effect in the opposite direction to that of the agonist
  • Have full affinity but intrinsic activity ranges between 0 to -1
A

INVERSE (NEGATIVE ANTAGONIST)

119
Q

largely determine the quantitative relations between dose or concentration of drug and pharmacologic effects

A

RECEPTORS

120
Q

are responsible for selectivity of drug action

A

RECEPTORS

121
Q

mediate the actions of pharmacologic agonists and antagonists

A

RECEPTORS

122
Q

NATURE OF DRUG RECEPTORS

so-called because their ligands are presently unknown, which may prove to be useful targets for the development of new drugs

A

ORPHAN RECEPTOR

123
Q

NATURE OF DRUG RECEPTORS

  • the best characterized receptors;
  • modify the actions of endogenous chemical signals (neurotransmitters, autacoids, hormones)
A

REGULATORY PROTEINS

124
Q

Other proteins identified as drug receptors

  • may be inhibited (or less commonly activated) by binding a drug.
  • Example: dihydrofolate reductase - receptor for methotrexate
A

ENZYMES

125
Q

receptor for methotrexate

A

DIHYDROFOLATE REDUCTASE

126
Q

Other proteins identified as drug receptors

Example: Na+, K+ ATPase – receptor for digoxin

A

TRASNPORT PROTEINS

127
Q

Other proteins identified as drug receptors

Example is Tubulin – the receptor for colchicine

A

STRUCTURAL PROTEINS

128
Q

recepor for colchicine

A

TUBULIN

129
Q

Aspects of Drug-receptor Functions

Receptors as determinants of the quantitative relation between the ____ of a drug and the ____

A

concentration of a drug & pharmacologic response

130
Q

Aspects of Drug-receptor Functions

Receptors as ____ and ____ that provide targets for important drugs

A

REGULATORY PROTEINS
COMPONENTS OF CHEMICAL SIGNALING MECHANISMS

130
Q

inhibits depolarization = relaxants
1) Class I Anti-arrhythmic
2) Local Anesthetics: Ester: 1 “i” * Amide: 2 “i
3) Some anticonvulsants: Carbamazepine, Phenytoin

A

Na channel blockers

130
Q

Aspects of Drug-receptor Functions

Receptors as key determinants of the ____ and ____ effects of drugs in patients

A

THERAPEUTIC
TOXIC

130
Q

Five basic mechanisms of transmembrane signaling

A ____ that can be induced to open or close by the binding of a ligand

A

LIGAND-GATED TRANSMEMBRANE ION CHANNEL

131
Q

Five basic mechanisms of transmembrane signaling

A ____ whose intracellular enzymatic activity is allosterically regulated by a ligand that binds to a site on the protein’s extracellular domain

A

TRANSMEMBRANE RECEPTOR PROTEIN

131
Q

Five basic mechanisms of transmembrane signaling

A ____ that crosses the membrane and acts on an intracellular receptor;

A

LIPID-SOLUBLE LIGAND

131
Q

Five basic mechanisms of transmembrane signaling

A transmembrane receptor that binds and stimulates a protein ____

A

TYROSINE KINASE

132
Q

TYPES OF RECEPTORS

  1. Receptor-Operated Channel (ROC)
  2. Voltage-Operated Channels (VOC)
A

TYPE 1: ION CHANNEL TYPES

132
Q

Five basic mechanisms of transmembrane signaling

A transmembrane receptor protein that stimulates a ____ (G protein), which in turn modulates production of an intracellular second messenger.

A

GTP-BINDING SIGNAL TRANSDUCER PROTEIN

132
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

  • Also known as ligand gated ion channels, or transmitter operated channels
  • Directly linked to a receptor, and opens only when the receptor is activated
    Ø Na+ ion channel: Nicotinic receptor + acetylcholine -
    Heart (VOC), Muscles (ROC) -
    Sodium inside the cell > depolarization of the membrane or increase of conduction of the impulse of the membrane > Contraction of muscles
    Ø Cl- ion channel: GABAA Receptor
    Ø Glycine receptor, 5HT3 receptor
A

RECEPTOR-OPERATED CHANNEL

132
Q
  • most abundant receptor
  • Are sometimes called metabotropic receptors, 7 transmembrane serpentine receptor
  • Are receptors for many hormones and slow transmitters
  • e.g. muscarinic Ach receptor, adrenergic receptors and neuropeptide receptors
  • Are membrane receptors which are coupled to intracellular effector systems via G-protein
A

TYPE 2: G-PROTEIN COUPLED RECEPTORS

133
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

ROC BEHAVIOR 3 RECOGNIZED STATES:
open

A

ACTIVATED

133
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

Receptor-Operated Channel is also known as

A

ligand gated ion channel
transmitter operated channel

133
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

ROC BEHAVIOR 3 RECOGNIZED STATES:
Closed, but openable in response to an appropriate stimulus

A

RESTED (NON-CONDUCTING)

133
Q

EXCITATORY

VGIC opening

A

Na⁺, Ca⁺²

134
Q

C

ROC BEHAVIOR 3 RECOGNIZED STATES:
Closed, and unable to open in response to an appropriate stimulus for a rested state channel

A

INACTIVATED

134
Q

molecular mechanism of action that involves modulation of the transition of the ROC between states

A

GATING

134
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

VOLTAGE-OPERATED:
5 types of Ca channels

A

L T N P Q

134
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

VOLTAGE-OPERATED (Na channel):
opens and closes slowly (in 10’s of millisecond)

A

SLOW GATE

134
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

  • The behavior is modulated endogenously by membrane potential (voltage)
  • Examples:
    Ø Na channel (cardiac)- contains two voltage operated
    gates
A

VOLTAGE-OPERATED CHANNEL

134
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

VOLTAGE-OPERATED:
* opening of channels result in generation of outgoing currents
* more than 10 types in the heart

A

K channels

135
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

VOLTAGE-OPERATED (Na channel):
opens and closes quickly (in milliseconds)

A

FAST GATE

135
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

VOLTAGE-OPERATED:
* found in heart & smooth muscles
* opens during depolarization and then activates by voltage depending gating

A

Ca channels

135
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

VOLTAGE-OPERATED:
most important type in Ca channel

A

L

136
Q

TYPES OF RECEPTORS | TYPE 1: ION CHANNEL TYPES

VOLTAGE-OPERATED:
* channels in the CNS and in the peripheral

A

Cl channels

136
Q
  • Acts as an on-off switches for cell signaling
  • Stimulation or inhibition results in the modulation of the enzyme system responsible for producing the following transduction components;
  • Cyclic nucleotides – cAMP
  • Diacylglycerol
  • Inositol phosphates (IP3)
A

G-PROTEIN

136
Q

EXCITATORY

cell change

A

+

136
Q

INHIBITORY

cell change

A

-

136
Q

EXCITATORY

state

A

depolarization

136
Q

EXCITATORY

response

A

stimulation
contraction

137
Q

inhibit hyperpolarization = stimulants
1) Insulin secretagogues

A

K channel blocker

137
Q

INHIBITORY

VGIC opening

A

K⁺, Cl⁻

137
Q

INHIBITORY

response

A

depression
relaxation
dilation

137
Q

INHIBITORY

state

A

hyperpolarization

137
Q

cAMP SYSTEM

lungs

A

β2

137
Q

stimulant hyperpolarization = relaxants
* Minoxidil - arteriolar vasodilator
* Diazoxide - arteriolar vasodilator

A

K channel stimulants

137
Q

cAMP SYSTEM

general effect

A

CONTRACTION

137
Q

cAMP SYSTEM

metabolize cAMP
decrease cAMP levels
inhibit contraction

A

PDE3

137
Q

TYPE 2: G-PROTEIN COUPLED RECEPTORS

are also known

A

METABOTROPIC RECEPTORS

137
Q

cAMP SYSTEM

heart

A

β1

137
Q

G-Protein Coupled Effector Systems

A
  1. The adenylate cyclase/cAMP system
  2. The phospholipase C/Inositol phosphate system
  3. The regulation of ion channel
138
Q

cAMP SYSTEM

for stimulation

A

Gs

139
Q

cAMP SYSTEM

decrease cAMP

A

GI

140
Q

cAMP SYSTEM

responsible for production of cAMP

A

AC SYSTEM

141
Q

G-Protein Coupled Effector Systems

involves GQ

A

PHOSPHOLIPASE C / INOSITOL PHOSPHATE SYSTEM

142
Q

PHOSPHOLIPASE C / INOSITOL PHOSPHATE SYSTEM

Phospholipase C produces ____ and ____

secondary messengers produced in phospholipase C

A

DAG & IP₃

143
Q

PHOSPHOLIPASE C / INOSITOL PHOSPHATE SYSTEM

secondary messenger that activates protein kinase

A

DAG

144
Q

PHOSPHOLIPASE C / INOSITOL PHOSPHATE SYSTEM

DAG activates ____

A

protein kinase

145
Q

PHOSPHOLIPASE C / INOSITOL PHOSPHATE SYSTEM

secondary messenger that increases calcium ions

A

IP3

146
Q

PHOSPHOLIPASE C / INOSITOL PHOSPHATE SYSTEM

IP3 increases ____

A

calcium ions

147
Q

PHOSPHOLIPASE C / INOSITOL PHOSPHATE SYSTEM

  • responsible for contraction
  • important for the heart
A

calcium ions

148
Q
  • Activation of hormone-sensitive lipase
  • Inactivation of glycogen synthase
  • Activation of phosphorylase kinase
    • Increased lipolysis
    • Reduced glycogen synthesis and increased glycogen breakdown
  • Activation of L-type calcium channels and sarcoplasmic reticulum in cardiac cells
    • Increased calcium currents and release
A

PHOSPHORYLATION

149
Q
  • Modulation of the release of endocrine hormones and neurotransmitters
  • Smooth muscle contraction
  • Inflammation
  • Ion transport
  • Tumor promotion
A

PROTEIN-KINASE LINKED TRANSDUCTION

150
Q
  • Smooth muscle contraction
  • Increased rate of contraction and relaxation of cardiac myocytes
  • Secretion of transmitter molecules of glandular secretions
  • Hormone release
  • Cytotoxicity
  • Activation of certain enzymes
A

Ca⁺²-linked transduction

151
Q

G-protein couple receptors can control ion channel function by mechanism that do not involve

A

secondary messengers

152
Q

G-protein interacts ____ with the channel

A

directly

153
Q

an opioid receptor that open K+ channel thus enhance K+ permeability

A

MUSCARINIC ACH

154
Q

SECONDARY MESSENGERS

  • mediates hormonal responses:
  • mobilization of stored energy
  • conservation of water by the kidney
  • Ca2+ homeostasis
  • increased rate and contractile force of heart muscle
  • It also regulates the production of adrenal and sex steroids
  • relaxation of smooth muscle
  • other endocrine and neural processes
A

CYLIC ADENOSINE MONOPHOSPHATE (cAMP)

155
Q

SECONDARY MESSENGERS | cAMP

the breakdown of carbohydrates in liver or triglycerides in fat cells stimulated by b-adrenomimetic catecholamines

A

mobilization of stored energy

156
Q

SECONDARY MESSENGERS | cAMP

  • conservation of water by the kidney is mediated by ____
  • it is an anti-diuretic hormone ADH
A

vasopressin

156
Q

SECONDARY MESSENGERS | cAMP

Ca⁺² homeostasis is regulated by ____

A

parathyroid hormone

156
Q

SECONDARY MESSENGERS | cAMP

DAG when phosphorylated yields ____

A

phosphatidic acid

156
Q

SECONDARY MESSENGERS | cAMP

  • Confined to the membrane, where it activates a phospholipid- and calcium sensitive protein kinase called protein kinase C
  • Terminated by either phosphorylation to yield phosphatidic acid, which is then converted back into phospholipids, or it is deacylated to yield arachidonic acid
A

diacylglycerol (DAG)

156
Q

SECONDARY MESSENGERS | cAMP

DAG when deacylated yield ____

A

arachidonic acid

156
Q

SECONDARY MESSENGERS | cGMP

a blood-borne peptide hormone

A

ATRIAL NATRIURETIC PEPTIDE

157
Q

SECONDARY MESSENGERS | cAMP

  • responsible for the increase of Ca
  • Diffuses through the cytoplasm to trigger release of Ca2+
  • Elevated cytoplasmic Ca2+ concentration promotes the binding of Ca2+ to the calcium-binding protein calmodulin
  • Inactivated by dephosphorylation
  • Ca2+ is actively removed from the cytoplasm by Ca2+ pumps
A

INOSITOL TRIPHOSPHATE (IP3)

157
Q

SECONDARY MESSENGERS | cGMP

  • enhance production of IP3, and DAG → increase Ca = Contraction
  • by Gq
A

PHOSPHOLIPASE C (PLC) SSYSTEM

157
Q

SECONDARY MESSENGERS

  • Produced by membrane-bound guanylyl cyclase
  • Acts by stimulating a cGMP-dependent protein kinase
  • Terminated by enzymatic degradation of the cyclic nucleotide and by dephosphorylation of kinase substrates
  • Increased concentration causes relaxation of vascular smooth muscle
A

CYCLIC GUANOSINE MONOPHOSPHATE (cGMP)

157
Q

SECONDARY MESSENGERS | cGMP

  • Activation - by Gs
    → increase concentration of 2°messenger: cAMP
  • Inhibition - by Gi
    → reduce concentration of 2°messenger: cAMP
A

ADENYLYL CYCLASE (AC) SYSTEM

157
Q

SECONDARY MESSENGERS | cGMP

binds to and activates a cytoplasmic guanylyl cyclase

vasodilation

A

NITRIC OXIDE

157
Q

TYPE 3: KINASE-LINKED RECEPTORS

an intracellular protein kinase domain that they incorporate within their structure

A

tyrosine kinase

157
Q

TYPES OF RECEPTORS

  • These are membrane receptors which incorporate an intracellular protein kinase domain (tyrosine kinase) within their structure
  • Examples are insulin receptors and receptors for various cytokines and growth factors
  • Transduction mechanisms are mainly involved in events controlling cell growth and differentiation, and act directly by regulating gene transcription
A

TYPE 3: KINASE-LINKED RECEPTORS

157
Q

TYPE 3: KINASE-LINKED RECEPTORS

mechanisms that are mainly involved in events controlling cell growth and differentiation

A

transduction

158
Q

TYPE OF RECEPTORS

  • Also known as nuclear receptors
  • Intracellular receptors
  • Include receptors for steroid hormones, thyroid hormones, Vitamin D and retinoic acid
  • Effects are produced as a result of altered protein synthesis, and thus slow in onset
A

TYPE 4: RECEPTORS THAT REGULATE GENE TRANSCRIPTION

159
Q

TYPE 4: RECEPTORS THAT REGULATE GENE TRANSCRIPTION

are also known as

A

NUCLEAR RECEPTORS

160
Q

TYPE 4: RECEPTORS THAT REGULATE GENE TRANSCRIPTION

effects are produced as a result of

A

altered protein synthesis

161
Q

TYPE 4: RECEPTORS THAT REGULATE GENE TRANSCRIPTION

onset

A

slow

162
Q
A
163
Q

ion channel in GABA receptor

A

CHLORIDE ION

164
Q

interaction leads to reduced level causing peripheral neuritis

A

ISONIAZID & PYRIDOXAL PHOSPHATE

165
Q

stimulate dopa decarboxylase leading to nullification of L -Dopa’s action

A

PYRIDOXAL PHOSPHATE

166
Q

inhibits xanthine oxidase prevents conversion to uric acid

A

ALLOPURINOL

167
Q

tx for acute gout

A

colchicine

168
Q

tx for chronic gout

A

allopurinol

169
Q
  • Facilitate passage of ions or molecules across cell membranes by altering their conformation from a rested state to an activated state
  • Classes: Uniporters, Symporters, Antiporters
A

ENERGY-INDEPENDENT

170
Q
  • Translocate its passenger through altered conformation where proteins are converted into an enzyme that normally hydrolyzes ATP (energy dependence)
  • e.g. Na+/K+ - ATPase
A

ENERGY-DEPENDENT

171
Q

usual movement of K⁺ when activated

A

exit

172
Q

effect of partial agonist + full agonist

A

antagonism effect

173
Q

1 intrisic activity

A

full agonist

174
Q

more than 0, less than 1 IA

A

partial agonist

175
Q

less than 0 IA

A

inverse agonist

176
Q

The relative concentration required to produce a given magnitude of effect is ____ and depends on affinity and efficacy

A

potency

177
Q

has high efficacy (full activation)

A

full agonist

178
Q

Types of Drug Antagonism

  • also known as physiologic antagonism
  • 2 ligands acting on different targets producing opposite effects
    Example: Norepinephrine and Acetylcholine
  • NE target B1—> tachycardia (increased heart rate)
  • ACh target M2 —> bradycardia (heart rate slower than normal)
A

FUNCTIONAL ANTAGONISM

179
Q

has intermediate efficacy (less activation)

A

partial agonist

180
Q

Types of Drug Antagonism

Functional antagonism is also known as

A

physiologic antagonism

181
Q

Types of Drug Antagonism

  • Pharmacologic antagonism
  • 2 ligands acting on the same target producing opposite effects
    Example: Norepinephrine + Propranolol
  • NE activate B1—> tachycardia
  • Propranolol inhibit B1 —> bradycardia
A

RECEPTOR ANTAGONISM

182
Q

Types of Drug Antagonism

Receptor antagonism is also known as

A

PHARMACOLOGIC ANTAGONISM

183
Q

Types of Drug Antagonism

Neutralization, chelation

A

CHEMICAL ANTAGONISM

184
Q

involves metal

A

chelation

185
Q

antidote for Heparin

A

Protamine sulfate

186
Q

Fe poisoning

A

Deferoxamine

187
Q

Cu poisoning

A

Penicillamine

188
Q

Classification of antagonism based on duration of action

  • fast noncovalent interaction;
  • within 24 hours - safer
A

reversible

189
Q

Classification of antagonism based on duration of action

  • slow covalent interaction;
  • days to weeks - toxic
A

irreversibleq

190
Q

Classification based on surmountability

  • Surmountable
  • Increase the dose of the agonist
  • reversible; safe
A

competitive

191
Q

Classification based on surmountability

  • Non surmountable;
  • no effect even with increasing the dose of agonist
  • irreversible; toxic
A

noncompetitive

192
Q

Types of Drug Interaction

the response elicited by combined drugs is equal to the combined responses of the individual drugs (1 + 1 = 2)

alcohol, sedative

A

addition

193
Q

Types of Drug Interaction

the response elicited by combined drugs is greater than the combined responses of the individual drugs (1 + 1 = 3)

A

SYNERGISM

194
Q

Types of Drug Interaction

a drug which has no effect on the system enhances the effect of the other (0 + 1 = 2)

levodopa & carbidopa, amoxicillin & clavulanic acid

A

POTENTIATION

195
Q

Types of Drug Interaction

Drug inhibits the effect of another due to opposite pharmacological actions (1 + 1 = 0)

A

ANTAGONISM

196
Q

Special pharmacological responses

the effect of the drug gradually diminishes when given continuously or repeatedly

A

DESENSITIZATION & TACHYPHYLAXIS

197
Q

Special pharmacological responses

  • describes a more gradual decrease in responsiveness to a drug
  • administration of low doses in long periods
A

TOLERANCE

198
Q

Special pharmacological responses

used to describe the loss of effectiveness of antimicrobial or antitumor drugs

A

DRUG RESISTANCE

199
Q

Special pharmacological responses

beneficial therapeutic response that arises from psychological factors

A

PLACEBO

200
Q

POTENCY

Lesser dose

A

greater potency

200
Q

maximum response

A

EFFICACY

200
Q

It is characterized by the magnitude of resistance increasing continuously with greater concentration of unbound drug at the receptor site

A

GRADED RESPONSE

200
Q

dose required to achieve 50% of efficacy

A

POTENCY

200
Q

more common type of graph in graded response

A

sigmoidal

200
Q

Smallest dose which produces efficacy

A

ceiling dose

200
Q

POTENCY

Greater dose

A

lesser potency

201
Q
  • Degree of changes in response with a change in the dose of the drug administered
  • Slanting assess safety
A

slope

201
Q

is the concentration of drug yielding 50% occupancy of the receptor and is dependent on the affinity of a drug for its receptor

A

MAXIMAL BINDING Kd

201
Q

Kd

Drugs with high binding affinity

A

LOW Kd

201
Q
  • are the proportion of receptors not needed for the production of the maximal response.
  • It exists if the maximal drug response is obtained at less than maximal occupation of the receptor. Determination is usually made by comparing the concentration for 50% of maximal effect (EC50) with the concentration for 50% of maximal binding (KD)
A

spare receptors

202
Q

Kd

Drugs with low binding affinity

A

HIGH Kd

203
Q
  • Graphically plots the percent of the population that responds to a drug versus the drug dose
A

QUANTAL DOSE RESPONSE RELATIONSHIP

204
Q

the observable response can be described only in terms of an all or none event.

A

QUANTAL RESPONSE

205
Q
  • Indicates potential variability of responsiveness among individuals
  • May be used to generate information regarding margin of safety
A

QUANTAL DOSE RESPONSE CURVE

206
Q

QUANTAL DOSE CURVE

the dose at which 50% of the individual exhibit the specified quantal effect

A

MEDIAN EFFECTIVE DOSE (ED50)

207
Q

QUANTAL DOSE CURVE

the dose required to produce a particular toxic effect in 50% of humans

A

MEDIAN TOXIC DOSE (TD50)

208
Q

QUANTAL DOSE CURVE

the dose with which the toxic effect is death to 50% of the animals

A

MEDIAN LETHAL DOSE (LD50)

209
Q
  • Also called Margin of Safety
  • The ratio of the lethal doses to 50% of the population over the median effective dose
  • The higher the TI, the safer the drug; the lower the TI, the greater the possibility of toxicity
  • Example: TI for barbiturates as a class is 10; for cardiac glycosides 3.0.
A

THERAPEUTIC INDEX

210
Q

Therapeutic index is also called

A

MARGIN OF SAFETY

211
Q

formula for Therapeutic index

A

LD50 or TD50 / ED50

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