Pharmacodynamics Flashcards

1
Q

Radioactive Iodine

A

Iodine is actively concentrated in the thyroid and the radiation will destroy all tissue within 2-3mm causing focal, controlled destruction

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2
Q

How does down regulation of receptors occur?

A

Internalizing the receptors in lysosomes, recycling them, sequestering or degrading.

Part of normal cellular metabolism

Tolerance

Tachyphylaxis

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3
Q

Down Regulation of Receptors

A

Number of receptors decreases and therefore a reduction in the effect

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4
Q

Full Agonist

A

Binds to the receptor to elicit a maximal response

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5
Q

Examples of non receptor biological reactions

A

Voltage Gated Channels

Enzymes

Carrier Proteins

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6
Q

Targets for drug reaction are divided into what two categories

A

Physical Interactions

Biological Interactions

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7
Q

Common receptor for secretory and smooth muscle functions whre the changes occur over seconds.

A

Metabotropic Receptors

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8
Q

Nonspecific drug effects occur in (physical/biological) interactions

A

Physical Interactions

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9
Q

Examples of nonspecific drug effects

A

Osmotic Diuretics

Antacids

Radioactive Iodine

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10
Q

Drug effects on Voltage Gated Channels

A

Blocking of ion channels can occur by the drug moleucle physically obstructing the channel to impair ion movment. Drug may also modulate the opening/or closing of the channel

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11
Q

The straight portion of the sigmoidal drug response curve falls between what range? This corresponds to what?

A

20-80%

Therapeutic Range

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12
Q

Ionotropic Receptors

A
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13
Q

Steroids and thyroid hormones are examples of what type of receptor, new protein production starts over the course of hours

A

Nuclear Receptors

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14
Q

Mixed Agonist - Antagonist

A

Acts as an agonist in one type of receptor and as an antagonist on other types of receptors

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15
Q

Side Effects

A

Secondary to the intended effect and may be good or bad

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16
Q

Agonist

A

Mimics the effect of the endogenous ligand

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17
Q

Toxic Effects

A

Responses to a drug that are harmful to the health or life of the animal

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18
Q

Efficacy

A

Maximal effect a drug can have

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19
Q

Types of pharmacodynamic receptors

A

Ionotropic Receptors

Metabolic Receptors

Kinase-Coupled Receptors

Nuclear Receptors

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20
Q

Antacids (Direct Neutralizers)

A

Given orally they direct interact with acid in the GI tract, a form of physiologic antagonism

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21
Q

Drug effects on Enzymes

A

Drugs can be analogs that compete with the real substrate for binding to the enzyme, prodrugs where the drug needs to be metabolized into its active form or can act as false substrates which will lead to the formation of abnormal metabolites instead of active product.

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22
Q

Lethal Dose 50 (LD50)

A

Dose which kills 50% of animals

23
Q

Ceiling effect

A

A partial agonist may never be able to achieve full efficacy

24
Q

Osmotic Diuretics

A

Molecules move through the body dragging water with them by osmosis until they are excreted

25
Q

Partial Agonist

A

Will bind to the receptor but not cause as much effect as a full agonist, it does prevent anything else from binding to the receptor while docked there

26
Q

Effective Concentration 50 (EC50)

A

Concentration at which a drug produces 50% of its maximal effect, only applies to in vitro preparations useful to compare the efficacy of different ligands

27
Q

Onset of Action (Latent Period)

A

Time required after drug administration for a response to be observed

28
Q

T/F: Endogenous neurotransmitters often bind to more than one type of receptor. The same signaling molecule can then cause different effects or have different affinity in different tissues or species.

A

True

29
Q

A low therapeutic index indicates a (safe/dangerous) drug

A

Dangerous

30
Q

Chemical Antagonism

A

Two drugs chemically inactivate each other

31
Q

Therapeutic Effects

A

Effects that clinicians want

32
Q

Quantification of drug response typically gives what type of curve when plotted on semi-log paper

A

Sigmoidal Curve

33
Q

Drugs can bind and activate or prevent from opening, often involved in fast neurotransmission.

A

Ionotropic Receptors

34
Q

Adverse Effects

A

Unintended and unwanted, this includes not producing the clinical effect

35
Q

Insulin receptors and growth promoting hormones and factors are of these type of receptors.

A

Kinase-Coupled Receptors

36
Q

Therapeutic Index

A

Ratio of LD50 and ED50

37
Q

Potency

A

Comparison of the concentratio of two drugs needed to induce the same magnitude effect

38
Q

Up Regulation of Receptors

A

Increase in the number of receptors, resulting in increase in the effect of drug

39
Q

Duration of Action

A

Length of time that a drug is effective - from onset of action until termination of action

40
Q

Nuclear Receptors / Transcription Factor Receptors

A

Located in the cytoplasm but after ligand binds translocate to the nucleus of the cell and bind to a response element within the DNA to initiate specific gene transcription

41
Q

Pharmacodynamics

A

Efects of drugs and their mechanism of action within the body

42
Q

Drug effects on Carrier Proteins

A

Some small, polar molecules cannot cross cell membranes and get carried in and out by carrier proteins. Drugs may alter this movement either preventing re-uptake of a molecule which increases its levles or preventing output of a molecule to decrease its levels

43
Q

Pharmacokinetic antagonsim

A

Drug alters ADME of another drug and reduces its effect

44
Q

Antagonist - Neutral Agonist

A

Binds to the receptor but does nothing on its own, however it sits and prevents anything else from binding and thus blocks the receptor

45
Q

Non-Competitive Antagonism

A

Ligand that interacts somewhere other than the receptor but causes a change in the receptor that blocks its ability to bind to the normal ligand

46
Q

A high therapeutic index indicates (safe/dangerous) drug

A

Safe

47
Q

Kinase-Coupled Receptors

A

Transmembrane proteins have an extracellular receptor portion and an intracellular portion that has enzymatic activity. Phosphorylation and activation of proteins activate effectors

48
Q

Physiologic Antagonism

A

Drugs have opposite effects that cancel each other out

49
Q

Ligand

A

Anything that binds to a recognition site

50
Q

Competitive Antagonism

A

Antagonist ligand binds and releases as long as it is present and so if the antagonist is present as well as an agonist they will compete for the binding, who binds more often will be determined by the concentration and affinity

51
Q

Metabotropic Receptors

A

G protein receptors (7TM) receptors, transduce an extracellular signal to an intracellular one by activating the G-Protein second messanger system

____________________

Allow for signal amplification and specificity

52
Q

Biological interactions include

A

Receptors

Non Receptors

53
Q

Effective Dose 50 (ED50)

A

Dose that produces a result (usually desired) in 50% of the animals

54
Q

Reverse Agonist

A

Will bind to the receptor and cause the opposite effect as the endogenous ligand would