PCOL M1.3 part 1 Flashcards

1
Q

What is the relationship of Pk, Pd, Physico-chemical properties

A

reversible

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2
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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3
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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4
Q

3 aspects on how a drug works

A

Physico-chemical properties
Pharmacodynamics
Pharmacokinetics

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5
Q

The intensity and quality of effect

A

Pharmacodynamic properties

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6
Q

it is depended to the physical and chemical of the drug
Ex. The drugs become bioavailable when the drugs cross the membrane.

A

Pharmacokinetics properties

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7
Q

The Chracteristic Pharmacokinetics properties is when a drug that capable of crossing the membrane more rapidly and efficiently is when it is

A

lipophilic, unionized, lower size of molecular weight

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8
Q

in the systemic circulation [pagnandoon na sya sa katawan] then it is able to bridge the site of action called DISTRIBUTION

A
  • Bioavailable
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9
Q

—–it is the metabolism and excretion [determine by ——-

A
  • Clearance and physiochemical properties
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10
Q

– is the connection between the brainstem and the spinal cord

A

 medulla oblongata

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11
Q

include cardiovascular receptors, respiratory, and vasomotor centers

A

o depression

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12
Q

What do you called Blood Brain barrier that separation of CNS

A

parenteral system [outside the central nervous system]

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13
Q
  • drugs may increase or enhance the function of an organ or a system. And give Example of drug that can cause stimulation of CNS
A
  • STIMULATION - Caffeine
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14
Q
  • drugs inhibit or decrease the function of an organ or the system
A
  • DEPRESSION - drugs inhibit or decrease the function of an organ or the system
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15
Q

example of CNS depressant, it decreases the activity of the CNS leading to drowsiness, decrease concentration, affect balance and equilibrium and even decrease memory and learning functions.

A

Alcohol

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16
Q

– memory/learning

A

o Cerebral cortex

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17
Q

this is an action attributed to local affects of the drug to a tissue or cell and example and explain

A
  • IRRITATION
    laxatives promote peristaltic movement by irritating the wall of the GIT causing increase motility and evacuation
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18
Q

is a laxative is used treat constipation

A

SENNA

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19
Q

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

A
  • PRIMARY
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20
Q

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

A
  • SECONDARY
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21
Q
  • Alter the cell environment by physical or chemical processes
  • Example and explain
A

Structural nonspecific
the patient has hyperacidity - the action of antacid is a bases that will lead (alters the pH of the stomach); to ‘neutralized’ [pagacidic yung patient need nya ng antacid para magneutralized]
* ‘hyperacidity – mataas ang acid than normal’
* there is hyperacidity = higher stimulation = nagkakaroon ng depress
* action of antidotes, e.g., activated charcoal (adsorbs the toxins by the process of absoption)

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22
Q
  • Alter cell function by drug-receptor interactions
  • Majority of drugs’ action is through this mechanism
  • treat for ulcer is what
A

Structural specific
Omeprazole – proton bound inhibitor [push the acid] – disable the proton bound in the cell

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23
Q

2 target for drug action

A

protein and non protein target

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24
Q

Majority of drugs interact with protein targets such as —- or 4 Regulatory Protein as Primary Target for Drug Action

A

receptors, ion-channel, enzymes and carrier molecules/Transporters

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25
Q

. After interacting with the target, a ——-of event follows

A

cascade

26
Q

 Structural specific mechanism

A

Protein target

27
Q

 Structural nonspecific mechanism

A

Non-protein target

28
Q

Non-protein target can be the target for the drug action

A

o Binding
o Per drug may exhibit neutralizing effect
o It promotes osmosis

29
Q

possible events that will follow the interaction

A

o Agonist/ inverse agonist

30
Q
  • possible events that will NOT follow the interaction / NO EFFECT
A

o Antagonist

31
Q

They promote permeability of the union/they modulate the permeability of union
o Blockers
o Modulators

A

B. Ion channels

32
Q

C. Enzyme - Normal reaction inhibited

A

o Inhibitors

33
Q

C. Enzyme - Abnormal metabolite produced

A

o False substrate

34
Q

C. Enzyme - Active drug produces

A

o Prodrug

35
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. [describes it as a target for drug’s action.]
A

RECEPTOR

36
Q

o Drug bind to the receptor/ positive
o is the capacity of a drug to form the complex with its receptor (DR complex)

A

 AFFINITY

37
Q

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

A

 INTRINSIC ACTIVITY (OR) EFFICACY

38
Q

o refers to any molecule which attaches selectively to particular receptors or sites
o it is a drug, natural or any substrate if it matches to a specific receptor

A

 LIGAND

39
Q

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

A

 AGONIST (Positive)

40
Q

 Agent which activates a receptor to 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) agonists

41
Q

o an agent which prevents the action of an agonist on a receptor but doesn’t have any effect of its own.
o It has only affinity but no intrinsic activity [no response/efficacy].
o This drug binds to the receptor and blocks the binding of an endogenous agonist.

A

 ANTAGONIST

42
Q

o Agent which activates a receptor to produce a sub maximal effect but antagonizes the actions of full agonist
o Have full affinity but with low intrinsic activity and hence are only partly as effective as agonists

A

 PARTIAL AGONIST

43
Q

o so-called because their ligands are presently unknown, which may prove to be useful targets for the development of new drugs
o coded
o No particular receptor of this drug

A

“ORPHAN” RECEPTOR

44
Q

o the best characterized receptors
o modify the actions of endogenous chemical signals
 neurotransmitters [ex. NE]
 autacoids [Histamine, serotonin]
 hormones [estrogen, thyroid hormones]

A
  • REGULATORY PROTEINS
45
Q

Types of protein

A

Enzymes , Transport proteins, receptor, and Structural proteins

46
Q
  • Also known as ligand gated ion channels, or transmitter operated channels
A

. RECEPTOR-OPERATED CHANNEL (ROC)

47
Q
  • Directly linked to a receptor, and opens only when the receptor is activated
A

. RECEPTOR-OPERATED CHANNEL (ROC)

48
Q

receptor for Na+ ion channel

A
  • Nicotinic receptor
49
Q

receptor for Cl- ion channel

A

GABAA receptor

50
Q

o Closed, but openable in response to an appropriate stimulus

A
  • Rested
51
Q

o Closed, and unable to open in response to an appropriate stimulus for a rested state channel

A
  • Inactivated
52
Q

open/ capable of opening the channel

A
  • Activated
53
Q

ROC behavior has 3 recognized states

A
  • Rested, Activated, and Inactivated
54
Q

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

A
  • GATING
55
Q

4 example of VOLTAGE-OPERATED CHANNELS (VOC)

A

o Na channel (cardiac), Ca channels, K channels, and other channels

55
Q
  • The behavior is modulated endogenously by membrane potential
A

VOLTAGE-OPERATED CHANNELS (VOC)

56
Q

o 5 types Ca channels

A

L [heart],
T[Brain],
N, P, Q

57
Q
  • Are sometimes called metabotropic receptors
A

G-PROTEIN COUPLED RECEPTORS

58
Q
  • Are receptors for many hormones and slow transmitters
A

G-PROTEIN COUPLED RECEPTORS
e.g. muscarinic Ach receptor, adrenergic receptors and neuropeptide receptors

59
Q
  • Are membrane receptors which are coupled to intracellular effector systems via —-
A

G-protein