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Pharmacology > Exam :0 > Flashcards

Exam :0 Flashcards

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1
Q

What is Pharmacokinetics?

A

What the body does to the drug.
It is the fate of a drug over time through the body

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2
Q

What are the four main pharmacokinetic processes (ADME)?

A

Absorption, Distribution, Metabolism, and Elimination/Excretion.

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3
Q

What is Absorption?

A

How a drug gets from the site of administration into the bloodstream

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4
Q

What is Distribution?

A

How a drug gets around the body to target tissues (site of action) or the reversible transfer of a drug from the systemic circulation to other body tissues and fluids

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5
Q

What is Metabolism?

A

How a drug is changed by the body or the biochemical modification of pharmaceutical substances in the body

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6
Q

What is Elimination/Excretion?

A

How a drug gets out of the body or the irreversible loss of drug from the body.

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7
Q

What are the two main routes of drug elimination?

A

Kidneys and Hepatobiliary system. The Kidneys are the most important

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8
Q

What do drugs need to achieve at target tissues to give therapeutic levels?

A

Adequate concentrations

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9
Q

Name a key barrier drugs must cross to reach their target tissue.

A

Cell membranes

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10
Q

How many cell membranes must a drug cross to get from the GIT to the blood?

A

Two (epithelial layer and vascular endothelium).

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11
Q

What is the main way for a drug to cross a membrane?

A

Diffuse directly through lipid (Transcellular)

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12
Q

Can small molecules pass between cells?

A

yes, this is called paracellular movement

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13
Q

What type of molecule crosses membranes more easily?

A

Lipid-soluble molecules or Unionised molecules

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14
Q

Are charged molecules pass into the cell more easily than uncharged molecules?

A

False. Charged molecules pass less easily than uncharged ones

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15
Q

What are continuous capillaries?

A

The most common type of capillary, found in muscle, liver, and heart. They are “a bit leaky” but block large drugs

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16
Q

What are fenestrated capillaries?

A

Capillaries with large pores, found in the kidney, pituitary, and endocrine glands. They are “very leaky”

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17
Q

What is the Blood-Brain Barrier (BBB)

A

A barrier in the CNS that protects it from toxic substances. It has tight junctions and is “Not leaky

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18
Q

Which types of drugs can cross the Blood-Brain Barrier (BBB)?

A

Only lipophilic or actively transported drugs can cross. Drugs cannot get between the cells due to tight junctions

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19
Q

In the stomach (highly acidic, pH 2), which type of weak drug is primarily absorbed?

A

Weak acid drugs

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20
Q

Why are weak acid drugs absorbed in the stomach?

A

Because in the acidic environment, they are largely protonated (unionised) and can diffuse across the gastric mucosal barrier

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21
Q

Why do weak acid drugs become “trapped” in blood plasma (pH 7.4)?

A

In the alkaline plasma, they become largely deprotonated (ionised/charged), making them unable to diffuse back across the membrane

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22
Q

Where are bases trapped in the body?

A

In acidic compartments (like the stomach or acidic urine).

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23
Q

What relationship is described by the Henderson-Hasselbalch equation?

A

The relationship between pH, pKa, and the degree of ionisation of a weak acid or base drug.

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24
Q

Name the four main ways drugs cross membranes.

A

Diffuse directly through lipid (main); 2. Combine with a carrier protein; 3. Diffuse through aqueous pores; 4. Pinocytosis

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25
Describe Passive Diffusion.
Molecules move from high concentration to low concentration. It is not saturable and has low structural specificity. It depends on drug concentration, lipophilicity, charge, and surface area.
26
Describe Facilitated Diffusion.
A carrier-mediated process that moves molecules down the concentration/electrochemical gradient. It does not require ATP
27
Describe Active Transport.
A process involving carrier proteins that requires ATP (energy). It can move molecules against a concentration/electrochemical gradient. It is saturable and structurally selective.
28
Which type of movement across membranes is important in the Blood-Brain Barrier and placenta?
Active Transport
29
Define Volume of Distribution (Vd).
The theoretical volume into which the drug is distributed. It is the parameter that relates the concentration of a drug in the plasma to the total amount of drug in the body
30
What is the formula for Volume of Distribution (Vd)?
Vd = (Amount of drug in the body) / (Plasma drug concentration) or Vd = Q (amount of drug injected) / Concentration
31
What does a low Vd indicate about a drug?
The drug remains mostly in the plasma (e.g., highly protein-bound drugs or large molecules like Heparin that cannot cross capillaries).
32
What does a high Vd indicate about a drug?
the drug extensively distributes into tissues (e.g., highly lipophilic drugs)
33
What is the relationship between Vd and plasma drug concentration for a given dose?
As Vd increases, plasma concentration decreases
34
Do drugs bind to plasma proteins?
Yes, many drugs bind to plasma proteins (e.g., albumin)
35
Which form of the drug is pharmacologically active?
Only free (unbound) drug is pharmacologically active.
36
Does binding to plasma proteins affect drug movement?
Yes, high protein binding can prolong drug action and alter drug clearance. Free concentration governs the movement of drug between plasma and tissues.
37
What is the primary site of drug metabolism?
The Liver
38
What are the two main phases of drug metabolism?
Phase I Reactions (Modification, e.g., oxidation) and Phase II Reactions (Conjugation).
38
What is the primary goal of drug metabolism?
Drug inactivation and to transform drugs into more water-soluble compounds for easier excretion.
39
What is the role of Cytochrome P450 (CYP) enzymes?
They are the main enzymes in Phase I metabolism and their main job is detoxifying foreign chemicals including drugs
39
What is the First-Pass Effect?
Metabolism of a drug that occurs after absorption from the GIT but before it reaches systemic circulation, primarily in the liver via the portal vein
40
What is a prodrug?
A compound with little or no pharmacological activity that is converted into an active drug compound in the body, often by enzymatic metabolism.
41
What is a Receptor?
Sensing elements in a chemical communication system. They bind endogenous molecules like hormones and transmitters
41
Give an example of a prodrug mentioned
Codeine is a prodrug converted to morphine by CYP2D6. Heroin is mentioned as a prodrug that converts to morphine in the brain
42
What is a Drug Target?
A molecule in the body, usually a protein, that is intrinsically associated with a particular disease process and that could be addressed by a drug to produce a desired therapeutic effect
42
How can the First-Pass Effect be avoided?
By using routes of administration that bypass the portal circulation, such as sublingual or IV
43
What is Pharmacodynamics (PD)?
The branch of pharmacology concerned with the effects of drugs and the mechanism of their action. It describes how drugs act on the body
43
Give examples of common drug targets (macromolecules)
Receptors, Ion Channels, Enzymes, and Carrier Molecules (Transporters). Proteins are commonly targeted because they are involved in disease processes.
44
What is Efficacy?
The maximum effect a drug is capable of producing. The capacity to produce an effect.
44
What is the Therapeutic Index?
The ratio TD50/ED50, reflecting the selectivity of a drug to elicit the desired effect rather than toxicity. A larger value indicates a safer drug
44
What is an Antagonist?
A substance which interferes with or inhibits the physiological action of another by binding to the receptor without causing activation
44
What is an Agonist?
A substance which initiates a physiological response when combined with a receptor.
45
How can genetic polymorphisms affect metabolising enzymes?
They can increase or decrease the speed of drug breakdown.
45
What is Pharmacokinetic variability?
Differences in PK from patient to patient, making standard dosage regimens challenging.
45
What is Affinity
The tendency of a drug to bind to receptors. High potency drugs have high affinity.
46
What is the Therapeutic Window?
The range between the minimum toxic dose and the minimum therapeutic dose. It is the dose range where a drug is effective and relatively non-toxic.
46
What factors can contribute to pharmacokinetic variability?
Genetic polymorphisms, Age, Weight, Organ function (Renal, Hepatic), Sex, Diet, Disease state, and Drug interactions
46
What is an Adverse Drug Reaction (ADR)?
An unintended harmful effect of a drug. They can be dose-related, allergic, or idiosyncratic.
47
What does a narrow therapeutic index mean in terms of ADRs?
If the therapeutic index is narrow, factors like food-drug interactions or small dosing errors can have harmful clinical effects
48
What are Drug Delivery Systems
Technologies that carry drugs into or throughout the body. They include the method of delivery and how drugs are 'packaged'
49
What does targeting drug delivery aim to reduce?
It aims to enhance the concentration of a drug in particular parts of the body relative to others
50
Give examples of drug delivery carrier systems mentioned
Liposomes, Microspheres, and Nanoparticles.
51
What are Liposomes?
Spherical vesicles consisting of one (or more) phospholipid bilayers. They can encase lipophilic and hydrophilic compounds
52
Name the four main types of receptor families
Ligand-Gated Ion Channels. G-Protein-Coupled Receptors (GPCRs). Kinase-Linked Receptors. Nuclear Receptors
53
What is another name for G-Protein-Coupled Receptors (GPCRs) and why are they called this?
They are also called Heptahelical receptors because they span the membrane 7 times.
54
How do GPCRs transmit signals inside the cell?
They are coupled to intracellular effector systems via a G-protein.
55
What types of endogenous molecules do GPCRs typically respond to?
They respond to hormones and 'slow' transmitters
56
Give some examples of GPCRs
Dopamine receptors, Prostaglandin receptors, Histamine receptors
57
What are Ligand-Gated Ion Channels, and what kind of endogenous molecules act here?
They are membrane proteins with an extracellular ligand-binding domain. 'Fast' neurotransmitters act here
58
How quickly do the responses mediated by Ligand-Gated Ion Channels typically occur, and why?
It peaks and decays in a few milliseconds. This is due to the direct coupling between the receptor and the ion channel.
59
Describe Buccal drug delivery
The administration of a drug through the cheek, it avoids first pass metabolism
60
Why can Nasal drug delivery allow for rapid onset of systemic effects?.
The nose is highly vascularised which allows for the diffusion into blood rapidly.
61
How does Pulmonary drug delivery work, and why is the lung good for drug absorption?.
It involves administering a drug via inhalation through the mouth and into the airways. The lung is good for absorption due to the vast absorptive surface area
62
What are two advantages of Pulmonary drug delivery (for systemic effects) mentioned in the source?.
Its unaffected by dietary complications and interpatient metabolic variation.
63
What are Microspheres primarily used for in drug delivery and what are some advantages
They are often used for sustained release of drugs. They're biodegradable, biocompatible, easily administered

Pharmacology (5 decks)

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