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BNPH700 > Pharmacodynamics, Pharmacokinetics, pharmacogenetics, Adverse drug reactions & Dosing regimens > Flashcards

Pharmacodynamics, Pharmacokinetics, pharmacogenetics, Adverse drug reactions & Dosing regimens Flashcards

1
Q

Define Agonist

A

Medication/drug that causes something to happen (salbutamol, mimics adrenaline)

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2
Q

Define Antagonist

A

Something that opposes/blocks an action

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3
Q

What is CYP450?

A

An enzyme that the liver produces, enabling the liver to break down medications

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4
Q

Define Pharmacodynamics

A

What the drug does to the body. The Interaction between a drug & its molecular target and the resulting pharmacological responses

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5
Q

Define Pharmacokinetics

A

Movement through the body (absorption, metabolism, secretion, excretion) (What the body does to the drug)

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6
Q

Define Bio-Availability

A

The amount of medication the body uses at the end. Depends on how the medication has been administrated (For example, IV, which can go straight into the bloodstream or oral, which absorb through the digestive system, then into the systemic circulation system

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7
Q

What is Prodrug?

A

Some people may not have enough of CYP450 to convert codeine (for example) into morphine in the liver, which means patients may not be getting the full therapeutic dose of codeine to alleviate pain.
- A medication which is converted in the liver to the active drug

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8
Q

What is the Hepatic First Pass and how does it work?

A

Medication travels down through the stomach, absorbed in the small intestine, absorbed in the liver before moving to the systemic circulation

An oral medication, most of the drug is absorbed in the small intestine, drug goes via the portal vein to the liver, the liver may ‘ditch’ some. Then the liver activates it using enzymes and sends it through to the systemic circulation system, and it is sitting in the plasma, these then bind to the albumin in the plasma. Only a certain amount of the drug is ended through to the systemic circulation system.

(refers to the amount of drug removed by the liver following its oral absorption in GI system)

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9
Q

What percent of IV medications are available to the bloodstream and why is this?

A

100% of IV medications are available to the bloodstream, as the medications are administrated via IV goes directly into the systemic circulation, meaning they bypass the digestive system

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10
Q

Define Generic Name

A

Actual name of the drug (e.g. amlodipine), the official name listed in publications and used for prescribing

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11
Q

Define Trade Name

A

Marketed name - the name that the drug is marketed under; several different ways to name the generic drug (e.g. Norvasc)

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12
Q

Define Chemical Name

A

Describes the chemical composition.

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13
Q

List the four main types of proteins that drugs act on

A
  • carrier (transporter)
  • enzyme
  • ion channel
  • receptor
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14
Q

Define Drug Absorption

A

the process by which the unchanged drug proceeds from the site of administration into the blood

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15
Q

What VARIABLES effect drug absorption?

A
  • drug solubility
  • drug ionisation
  • drug formulation (SR, CR, ER)
  • physiological factors (blood flow, rapid intestine transit time, food in stomach, stomach pH)
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16
Q

Define drug distribution

A

the process of reversible transfer of the drug from the blood into other body compartment

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17
Q

What are 4 factors that impact drug distribution

A
  • Capillary permeability
  • plasma protein binding
  • cardiac function
  • tissue binding
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18
Q

Define drug clearance

A

refers to the time taken for the drug to be eliminated from the body

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19
Q

Using reference to pharmacokinetic and pharmacodynamic principles explain why therapeutic drug monitoring is required for some drugs

A

Monitoring is required in some drugs due to the risk of toxicity.

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20
Q

Define Half-Life

A

is the main time taken for blood drug plasma concentration to fall by 50% of its original value

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21
Q

What is the significance of a Half-Life?

A

is that it is determined of the action duration of a drug after a single dose, the time taken to reach steady state with chronic dosing and the dosing frequency required to avoid massive fluctuation in plasma drug.

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22
Q

What factors can influence a half-life?

A
  • volume of distribution
  • clearance
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23
Q

Define Metabolism

A

the process by which the drugs are made less lipophilic (more hydrophilic) for more efficient elimination by the kidneys. The liver is the main site of metabolism of the drugs. Main enzyme—CYP450

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24
Q

What factors influence drug metabolism?

A
  • Age (↓hepatocytes, ↓enzyme)
  • genetic (deficiency of enzymes i.e. codeine)
  • disease state (HF, shock, hepatitis, cirrhosis)
  • diet & environmental factors (grapefruit)
  • drug interactions
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25
Q

Define Drug excretion

A
  • Excretion is a process whereby drugs or metabolites are irreversibly transferred from the internal environment to the external environment through a renal or non-renal route.
26
Q

What factors influence drug excretion?

A

The primary organs involved in excretion include, kidney (renal excretion), bile (biliary excretion), lungs – expired air (pulmonary excretion), sweat (skin excretion), saliva (salivary excretion), milk (mammary excretion).

27
Q

Define elimination

A

the irreversible loss of the drug from the body by the process of metabolism & excretion. Occur mainly in kidney, also in bile, through sweat, saliva, faeces, breast milk, exhaled air.

28
Q

Define Down regulation

A

(desensitisation): a decrease in receptor numbers can lead to desensitisation & loss of response. i.e. salbutamol, opioids

29
Q

What is an Enzyme Induction?

A

when a drug is present in the body for a prolonged period, the amount of metabolising enzymes can increase & thus speed up metabolism of that drug. This can decrease the concentration of active drug, meaning patient may require an increase in drug dose. i.e. morphine; alcohol, tobacco smoking

30
Q

What is an Enzyme Inhibition?

A

if a drug or food inhibits a metabolising enzyme. It is known as an enzyme inhibitor. Substances that cause enzyme inhibition may lead to the accumulation of drugs in the body leading to toxicity. i.e. grapefruit, Erythromycin

31
Q

What is Therapeutic Range?

A

is the range of the drug concentration having a high probability of producing desired therapeutic effect & a low probability of producing adverse effects

32
Q

What does therapeutic range help to ensure?

A
  • High probability of drug producing desired effects
  • Low probability of drug producing adverse effects
33
Q

What is Steady State?

A

dosing schedule is maintained after 3-5 half-life. The rate of administration will equal to the rate of elimination—steady state is the aim of drug therapy

34
Q

What is Loading Dose?

A

allow rapid achievement of therapeutic serum levels.

35
Q

What type of drug are usually loading doses?

A

Antibiotics

36
Q

Why is a higher dose of a loading dose administered at first?

A

To reach the therapeutic range quickly

37
Q

What are Zero-Order Kinetics?

A

is the constant amount of drug per unit time is metabolised (metabolic rate does not increase as drug concentration increase, i.e. alcohol, in drug overdose situation when it’s saturated). Medications that DON’T HAVE a half-life, the body can only metabolise so much, once it reaches past this thresh-hold, it will continue to metabolise at the same rate, which could lead to an overdose due to a build up of the drug. The body doesn’t have the ability to increase the enzymes to break down the drug

38
Q

What are First-Order Kinetics?

A

the amount of drug eliminated from the body is proportional to the drug plasma concentration (increased plasma concentration →increased rate of drug metabolism)—most drugs go through first order kinetics. Medications that HAVE a half-life

39
Q

What drugs can easily cross the cell membrane?

A

lipophilic (lipid-like), small molecules, unionised (more lipid soluble)

40
Q

What should you consider when assessing a person’s ability to excrete drugs?

A

renal function, urinary pH

41
Q

Where is the drug first distributed?

A

To the area of high blood supply –brain, heart, liver, kidney

42
Q

Where do tissue binding and drug storage occur?

A

In muscle, adipose tissue, bone, teeth

43
Q

Define drug competition

A

drug may compete for binding with the plasma protein. i.e. aspirin displaces warfarin, therefore increases warfarin plasma concentration

44
Q

How does renal excretion occur?

A
  • glomerular filtration
  • tubular secretion
  • tubular reabsorption
45
Q

Define Pharmacogenetics

A

the effect of genetics on the drug action & elimination i.e. 6-10% Caucasian lack enzyme that metabolise codeine

46
Q

What food can interact with Tetracyline?

A

Milk Products

47
Q

What food can interact with warfrin?

A

Vitamin K Rich foods

48
Q

What food can interact with Monoamine oxidase inhibitor (MAOi)?

A

Foods high in tyramine

49
Q

What food can interact with Statins?

A

grapefruit juice (grapefruit juice inhibits metabolising enzyme ↑toxicity of statins)

50
Q

What two types of classifications are there for adverse drug reactions?

A

Type A, Type B

51
Q

Explain the difference between Type A and Type B adverse drug reactions

A

TYPE A:
- predictable
- dose-related
- often is an exaggeration of therapeutic effect
- high incidence
- Low morality

TYPE B:
- Unpredictable
- May not be dose-related
- Incidence low
- High mortality

52
Q

List the risk factors for developing an adverse reaction.

A
  • Age (elderly)
  • Gender- women
  • Concurrent disease
  • Genetics
  • History of past reactions
  • Pharmaceutics (chemical characteristics)
  • Route of administration
  • Dose duration and frequency
53
Q

What three medications require blood tests and why?

A
  • Clozapine—risk of agranulocytosis, weekly blood test for first 18 weeks, then monthly
  • Heparin—aPTT, therapeutic range 60-90 seconds
  • Warfarin—PT & INR, therapeutic range 2.0-4.0
54
Q

Which drugs may cause bronchospasm?

A

Aspirin, beta-blocker (Non-selective), NSAIDs, Morphine

55
Q

What drugs could cause ototoxicity?

A

loop diuretics, Aspirin, Aminoglycosides

56
Q

What drugs can increase potassium levels?

A

ACEi, ARBs, K+ sparing diuretics (Spironolactine)

57
Q

What drugs can decrease potassium levels?

A

Loop /Thiazide diuretics, corticosteroids

58
Q

What drugs that decrease therapeutic effect when used excessively or prolonged?

A
  • beta2 agonist (i.e. Salbutamol)
  • Nitrate tolerance
  • loop diuretics resistance
  • opioids
59
Q

What drugs cause withdrawal if stopped suddenly?

A
  • beta blockers—rebound Tachycardia, dysrhythmia, ↑BP, chest pain, sweating, tremors, ↑risk of MI
  • Benzodiazepines withdrawal–Insomnia, agitation/irritability, fearfulness, muscle spasm/tremors, gastric problems, sweating
  • Opioids - Cravings, Insomnia, Agitation, mood swings, tremors
60
Q

What does gastric juice in the stomach contain?

A
  • Hydrochloric Acid (HCI)
    • Mucus
    • Gastric Enzymes
61
Q

What is the function of Hydrochloric Acid (HCI)?

A
  • Kills microbes in food
  • H+ ions are actively pumped into lumen by proton pumps
62
Q

What is the function of the mucus?

A
  • Protects stomach wall from being damaged by the HCL

BNPH700 (8 decks)

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