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IASM > Week 11 Drugs > Flashcards

Week 11 Drugs Flashcards

1
Q

4 Common drug targets

A
  1. Enzymes - increase/inhibit activity
  2. Ion channels - enhance/inhibit movement of ions
  3. Receptors - mimic endogenous compounds
  4. Transporters - occupy binding site -> prevent transportation of endogenous compounds
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2
Q

What is true drug receptor?

A
  • only known ligand is drug

- no endogenous ligand has been identified

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3
Q

What are orthosteric agonist and allosteric agonists?

A
  1. Orthosteric agonist: binds to orthosteric site of receptor -> produce ultimate response
  2. Allosteric agonist: binds to allosteric site of receptor -> alters affinity/efficacy of receptor to ligand
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4
Q

3 Parameters affecting magnitude of receptor response

A
  1. Occupancy of receptors
  2. Efficacy of receptor signal
  3. Number of receptors
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5
Q

2 Observable properties of drugs

A
  1. Potency - concentration required to elicit the same magnitude of response
  2. Efficacy - maximal response that can be achieved
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6
Q

2 Properties of antagonist and agonists

A
  1. Affinity - degree of attraction (for both agonist and antagonist)
  2. Efficacy - effect resulted from binding of receptor (for agonist ONLY as antagonist blocks activation of receptor)
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7
Q

4 Phases of pharmacokinetics

A
  1. Absorption
  2. Distribution
  3. Metabolism
  4. Elimination
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8
Q

4 Mechanisms of drug movement from circulation to organ

A
  1. Simple diffusion (passive) - small, non-polar drugs
  2. Ion trapping - for weak electrolytes (weak acid can cross in acidic environment)
  3. Carrier-meditaed transport (facilitated diffusion and active transport) - larger drugs
  4. Pinocytosis - for macromolecules
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9
Q

What is bioavailability

A

Fractional extent to which a dose of drug reaches its site of action

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10
Q

3 steps of absorption of orally administered drugs

A
  1. Disintegration of dosage form - into granules
  2. Dissolution of drugs in fluids in absorption site (gastric fluid)
  3. Transfer of drug molecule across membrane lining the GI tract into systemic circulation
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11
Q

What is first-pass effect?

Main organ in which first-pass effect occurs for orally-administered drugs

A

Drug is metabolized between the site of absorption and site of sampling for measurement of drug concentration

Main organ: Liver

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12
Q

Where do drugs go after absorption into systemic circulation?

A

Distribution:

enter interstitial fluid -> intracellular fluid

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13
Q

What is drug displacement?

The two classes of drugs classified

A

Drug displacement:
competition between drugs for binding with plasma proteins

Class I: dose is less than protein binding capacity
Class II: dose is higher than protein binding capcity

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14
Q

What property does lipophillic drugs have in pharmacokinetics

A

Promote absorption and distribution

Hinder elimination and excretion

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15
Q

2 Types of drug metabolism

A
  1. Phase I: change functional group of parent chemical

2. Phase II: add a conjugate to the parent chemical

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16
Q

What is CYP450? What is its primary reaction?

A

Most well-known drug metabolic enzyme

Phase I reaction: change functional group of parent chemical (drug)

17
Q

Major organ involved in drug excretion

A

Kidney

18
Q

3 Common Phase II reaction of drug metabolism

A
  1. Glucuronidation - increases water solubility of parent drug
  2. Sulfation
  3. Acetylation
19
Q

Routes of drug excretion

A
  1. By kidney as urine
  2. Biliary excretion (as bile)
  3. Fecal excretion
  4. Other routes: saliva, breast milk, tears, sweat
20
Q

How are half-lives of zero-order, first-order and second-order drugs affected?

A

Zero-order: proportional to initial concentration (high conc -> stay in body for longer)
First-order: constant
Second-order: inversely proportional to initial concentration

21
Q

6 Types of Adverse Drug reactions

A
  1. Type A - augmented (dose-related)
  2. Type B - bizarre
  3. Type C - chronic (long term, dose accumulation)
  4. Type D - delayed
  5. Type E - end-of-treatment
  6. Type F - failure of efficacy (no response)
22
Q

4 types of patients due to metabolic phenotype

A
  1. Poor metabolizer
  2. Intermediate metabolizer
  3. Extensive metabolizer
  4. Ultrarapid metabolizer
23
Q

Functions of 4 main types of adrenergic receptors

A

alpha-1: vasoconstriction, contraction of smooth muscles
alpha-2: suppress release of presynaptic noradrenaline
beta-1: increase heart contractility, increase heart rate
beta-2: vasodilation, relaxation of smooth muscle

24
Q

2 broad types of drugs that affect sympathetic nervous sytem

A
  1. Sympathomimetics - direct (bind to adrenergic receptors) /indirect (increase release of noradrenaline)
  2. Sympatholytics - direct (block receptor activation) /indirect (inhibit synthesis of noradrenaline)

IASM (18 decks)

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