LESSON 2 PHARMACODYNAMICS Flashcards
True or false
drugs, a chemical substance of known structure other than a nutrient produces a biological effect
True
True or false
In pharmacodynamics, it deals with drugs’ effects on the body
True
True or false
In PHARMACODYNAMICS, it study the chemical and pathological effects of drugs and
their mechanisms of actions
False
(biochemical and physiological)
Drugs create effects de novo
False
Drugs do not create effects de novo
In effects de novo, drugs only alter or modify the underlying biochemical and
physiological processes
True
In PHARMACODYNAMICS Drug will not work unless it is bound to sites known as “drug
targets”
True
most drug targets are protein molecules
True
most drug targets are protein molecules except propanol, in treating osteoporosis, will
bind to calcium salts in the bone matrix
False
most drug targets are protein molecules
bisphosphonates, in treating osteoporosis, will
bind to calcium salts in the bone matrix
There are (4) main types of target proteins:
o Receptors
o Enzymes
o Carrier Molecules (Transporter) o Ion Channels
True
Enzymes are the biologic partners of drug action
False
Receptors are biologic partners of drug action
Receptors are cellular macromolecules with which the drug interacts to elicit a
cellular response leading to the drug’s observed effects
True
RECEPTORS are sensing elements in the system of chemical communications that
coordinates the functions of all the different cells in the body, it is also a components of cell or organisms that interact with the drug that initiates a chain of events that leads to the drug’s observed
effects
True
ENZYMES are micromolecules having biological functions and possessing reactive sites for selected substrates
False
ENZYMES are macromolecules having biological functions and possessing reactive sites for selected substrates
a drug acts as competitive inhibitor of an enzyme
True
TRANSPORT PROTEINS act as catalysts; speed up the metabolic functions of the cell
False
ENZYMES act as catalysts; speed up the metabolic functions of the cell
TRANSPORT PROTEINS
transport ions across the cell membrane
True
ION CHANNELS
form water-filled pores that span the membrane
True
CHARACTERISTIC FEATURES OF RECEPTORS are:
- SPECIFICITY
- SELECTIVITY
- RECEPTORS LARGELY DETERMINE THE QUANTITATIVE RELATIONS BETWEEN DOSE/CONCENTRATION OF DRUG & PHARMACOLOGICAL EFFECTS
- RECEPTORS MEDIATE THE ACTIONS OF PHARMACOLOGIC AGONISTS & ANTAGONISTS
- RECEPTORS HAVE THE ABILITY TO AMPLIFY SIGNAL DURATION & INTENSITY
True
No drug acts with complete specificity.
True
In selectivity molecular size, shape, & electrical charge will determine whether it will bind to a particular receptor
True
there is a “fit” for a drug to its receptor that influences its selectivity
True
ENZYMES LARGELY DETERMINE THE QUANTITATIVE RELATIONS BETWEEN DOSE/CONCENTRATION OF DRUG & PHARMACOLOGICAL EFFECTS
False
RECEPTORS LARGELY DETERMINE THE QUANTITATIVE RELATIONS BETWEEN DOSE/CONCENTRATION OF DRUG & PHARMACOLOGICAL EFFECTS
the drug effect will be affected also by the pharmacokinetics
of the drug
True
Potency is the measure of the amount of drug to produce an effect of a given magnitude
True
Infinite refers to the ability of the drug to bind with the receptors.
False
Affinity refers to the ability of the drug to bind with the receptors.
Potency is the concentration or dose of a drug required to produce 60% of the drug’s maximal effect
True
Potency will depend in part on affinity of receptors and efficiency with which drug-receptor interaction is coupled to receptors
True
In potency the less drug required to produce an effect, the more potent the drug is
True
Maximal Efficacy (Intrinsic Activity) is the ability of drug, once bound, to initiate changes that lead to effects
True
Maximal Efficacy (Intrinsic Activity) will depends on number of drug-receptor complexes formed
True
The clinical effectiveness of a drug depends not on its potency but on its maximal efficacy
True
RECEPTORS MEDIATE THE ACTIONS OF PHARMACOLOGIC AGONISTS & ANTAGONISTS
True
Agonists is a biologic response that mimics the response of endogenous ligand
True
Antagonists bind to receptors without causing activation but they block the effect of agonist on receptors
True
Antagonists’ efficacy is zero, no intrinsic activity
True
Competitive Antagonism can be reversible or irreversible
True
Competitive Antagonism, most direct mechanism by which one drug
can increase the effect of another
False
Competitive Antagonism, most direct mechanism by which one drug
can decreased the effect of another
antagonist binds to a site in the receptor other than where the agonist bonds without blocking agonist binding and that’s Non-Competitive Antagonism
True
Non-Competitive Antagonism can be reversible or irreversible
False
Non-Competitive Antagonism are usually irreversible
Non-Competitive Antagonism: no matter how you increase the agonist concentration, it will not dissociate the antagonists
True
Chemical Antagonism is a drug or ligand combines with another drug and renders it inactive
True
In Chemical Antagonism the effect of the active drug is lost
True
Physiological Antagonism acts at a completely separate receptor which produce effects that are functionally opposite to those of agonist
True
antagonist effectively reduces the concentration of the active drug at its site of action
True
In Pharmacokinetic Antagonism
increasing the degradation the drug producing a lower effect, increasing the excretion of a drug reduces its effect as well
True
Block of Receptor–Effector Linkage Antagonism, blocks from the receptor to chain of events leading to production of response by agonist
True
second messengers are the hormones, neurotransmitters (NT), peptides
True
Desensitization of Receptors also known as tachyphylaxis
True
In Desensitization of Receptors there’s a temporary inaccessibility of receptors which the
effect of drug gradually diminishes
True
In Desensitization of Receptors it allows potential damage to the cell
False
In Desensitization of Receptors it prevents potential damage to the cell
Below are the mechanisms of Desensitization of Receptors:
o exhaustion of receptors
o translocation of receptors
o physiological adaptation
o altered drug metabolism
True
IDENTIFY!
occurs when a drug is repeatedly or chronically given to a patient
Desensitization of Receptors
IDENTIFY!
receptors are unresponsive to the ligand
Desensitization of Receptors
IDENTIFY!
cell’s responsiveness to ligand is reduced
Down-Regulation
degradation of receptors occurs slower than de novo synthesis of receptors
False
degradation of receptors occurs faster than de novo synthesis of receptors
In Down-Regulation after activation, the receptors
are either degraded or recycled
True
degradation is more faster than recycling of the receptors
True
degradation of receptors reduces effects
True
hydrophilic ligands cannot enter or penetrate the cell and they interact with extracellular receptors.
True
Hydrophobic or lipophilic ligands can enter the cell and interact with intracellular receptors.
True
The location of Ligand-Gated Ion Channels, G CHON-Coupled Receptors, Enzyme-Linked Receptors are in the membrane
True
Location of Nuclear Receptors is in the membrane
False
Location of Nuclear Receptors is in the INTRACELLULAR
Ligand-Gated Ion Channels are receptors on which fast neurotransmitters act, involving mainly fast (chemical) synaptic transmissions occurring in milliseconds
True
Ligand-Gated Ion Channels is responsible for the regulation of flow of ions across the cell
membrane
True
IDENTIFY!
serpentine receptors
G CHON-Coupled Receptors
G CHON-Coupled Receptors constitutes the largest family, 7 membrane spanning alpha helices
True
G CHON-Coupled Receptors pass on the message to the effector systems that generate a cellular response
True
G CHON-Coupled Receptors needs second messengers in order to have a response
True
second messengers are also known as neuromodulators or neurohormones essential in conducting and amplifying signals
from G-protein coupled receptors
True
Enzyme-Linked Receptors respond mainly to protein mediators
True
Enzyme-Linked Receptors has 2 domain:
enzyme domain, surface receptor domain
True
Enzyme-Linked Receptors takes seconds to produce effects such as insulin
False
take HOURS to produce effects such as insulin
IDENTIFY!
regarded as ligand activated transcription factors that
transduce signals by modifying gene transcription
INTRACELLULAR OR NUCLEAR RECEPTORS
Low Therapeutic Index means
more side effects; not safe
True
High Therapeutic Index means
less side effects; safer to use
True
Toxicity refers to the adverse effects of a drug.
True
The primary goal of drug therapy is to achieve a desired
pharmacologic effect without causing adverse reactions.
True
Hyperreactive means patients who are unexpectedly resistant to the conventional doses of a drug
FALSE
HYPOREACTIVE means patients who are unexpectedly resistant to the conventional doses of a drug
Hyporeactive means patients that are unusually sensitive to a drug
FALSE
HYPERREACTIVE means patients that are unusually sensitive to a drug
Non compliance means patient will not take the drug as prescribed at a given time
True
FACTORS INFLUENCING DRUG EFFECTS
(PATIENT FACTORS)
→ body, weight & composition
→ age
→ sex, pregnancy, lactation
→ environmental factors–diet
→ genetic factor
→ physiologic variables
→ pathologic factor–decrease in organs of absorption, distribution, metabolism,
excretion
True
Normal patients may show unusual resistance for highly lipophilic agents especially when it is given in repeated doses.
False
OBESE patients may show unusual resistance for highly lipophilic agents especially when it is given in repeated doses.
Children have a risk of having tooth discoloration when given tetracycline.
True
men are more vulnerable than women with respect to certain drugs.
False
Women are more vulnerable than men with respect to certain drugs.
In pregnancy, drugs can have teratogenic effects on the fetus resulting in genetic abnormalities.
True
In elderly patients, the dose needs to be adjusted.
True
There are certain drugs not given together with food. An
example of which is tetracycline which is not to be given with
dairy products or antacids which have contraindications.
True
variables in drug administration–time, duration
True
placebo effect means
o any effect attributable to medication or procedure that is
not related to its pharmacodynamic or specific properties
o most often, there is an inert substance
True
placebo effect means a psychological condition where the response arises from
expectations of the patient concerning their effects
True
IDENTIFY!
According to Onset
According to Degree
According to Predictability
According to Onset
- acute
- subacute
- delayed
According to Degree
- mild
- moderate
- severe
According to Predictability
- predictable & dose-related
- unpredictable & not necessarily
dose-related
furosemide, is a diuretic which reduces edema.
True
SIDE EFFECTS can be predictable, dose-dependent reaction related to the goal of therapy
FALSE
SIDE EFFECTS can be predictable, dose-dependent reaction UNRELEATED to the goal of therapy
IDIOSYNCRATIC REACTIONS
is an unexpected response to a drug
True
IDIOSYNCRATIC REACTIONS is a dose-dependent, unpredictable
True
IDENTIFY!
→ adverse reaction of immunologic origin
DRUG ALLERGY
In drug allergy, the nature of unfavorable effect is not a function of the
offending drug but of the immune mechanism involved
True
→ anaphylactic responses
→ within minutes or hours
→ release of histamine & other mediators
Is a type of allergy in type 2
FALSE
TYPE 1
Is a type of allergy in type 1
→ more likely in parenteral injection
→ treatment is epinephrine
True
IDENTIFY
What type of allergy?
→ cytotoxic
→ usually delayed
→ caused by circulating antibodies
TYPE 2
Type of allergy
TYPE 3 is an immune complex reactions
True
In type 4 allergy it is cell- mediated
True
Type 2 & 4 in allergy is usually delayed
True
Drug will work if it is bound to sites known as “drug
targets”
False
(Drug will not work unless it is bound to sites known as “drug
targets”)