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CNS and endocrine
Analgesics
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Niamh M
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Cards (157)
What is the purpose of drug metabolism?
To process and
eliminate
drugs from the body
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Why is paracetamol limited to 4g per day?
To prevent potential
toxic
side effects
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What defines the bioavailability of a drug?
The fraction reaching blood circulation after
metabolism
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What is the therapeutic window?
The range where a drug is
effective
without
toxicity
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How does the body process drugs?
Through
metabolism
in the
liver
and
excretion
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What are xenobiotics?
Chemical
entities in the blood from outside the body
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What is the overall aim of drug metabolism?
To break down drugs into easily excreted
metabolites
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What are the phases of drug metabolism?
Phase I
: Activation by oxidation, reduction, hydrolysis
Phase II
: Conjugation to form more polar molecules
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What is the role of CYP450 enzymes?
They are important for
Phase-I
drug metabolism
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What does polymorphism refer to in CYP450 enzymes?
Different forms of enzymes affecting drug
metabolism
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Why is it important to understand CYP450 interactions?
They affect
metabolic
rates and drug concentrations
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What can inhibit CYP450 activity?
Different drugs can inhibit CYP450
enzymes
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What happens when drugs are given together?
Check how each drug is
metabolized
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Why are older patients at risk with medications?
They
metabolize
drugs less
efficiently
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How can drugs be safely given together?
If they have different
metabolic
routes
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What are the learning outcomes of analgesic metabolism?
Understand analgesic drug metabolism concepts
Learn about
CYP450
enzymes and their interactions
Recognize the importance of
polymorphism
in drug metabolism
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What are the factors affecting CYP450 metabolism?
Genetic
variation in the population
Age differences affecting enzyme
efficiency
Drug-drug
interactions
influencing metabolic rates
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What is the toxic metabolite of paracetamol?
NAPBQI
(
N-acetyl-p-benzoquinone imine
)
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What is the role of glucuronidation in drug metabolism?
It helps convert drugs into inactive
metabolites
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How does codeine metabolize?
It converts to
morphine
and
norcodeine
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What is the significance of CYP450 2D6 and 3A4 in codeine metabolism?
They are involved in
glucuronidation
processes
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How do different drugs affect CYP450 activity?
They can
induce
or
inhibit
enzyme activity
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What is the impact of genetic variation on drug metabolism?
It leads to differences in
enzyme efficiency
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Why is care needed when prescribing to older patients?
They may have reduced
drug elimination efficiency
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What is the main goal of analgesic metabolism?
To increase water solubility for
excretion
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What are the key points in the metabolism of analgesics?
Metabolism involves
Phase-I
and
Phase-II
processes
Aim is to increase water solubility for elimination
Each drug has its own metabolic pathway
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What should you understand regarding analgesic dosage forms?
How they improve
drug delivery
and efficacy
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What type of pain is treated with lidocaine?
Acute lower back pain
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What is an ideal analgesic formulation supposed to be effective against?
A broad
range
of pain types
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What are the steps in the World Health Organization analgesic ladder?
Mild pain: Non-opioids (
Aspirin
,
Paracetamol
, NSAIDs)
Moderate to strong pain: Mild opioids with/without non-opioids
Strong to severe pain: Strong opioids with/without non-opioids
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What types of pain are mentioned in the study material?
Nociceptive
,
neuropathic
, and
psychogenic
pain
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What are the characteristics of an ideal analgesic formulation?
Rapid
onset
, controllable
duration
, and easy administration
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Why is patient’s culture important in choosing a dosage form?
It influences
acceptance
of certain forms
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What factors influence the choice of analgesic dosage form?
Patient characteristics
, culture, and
medical condition
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What is a disadvantage of solid dosage forms like tablets?
Poor
bioavailability
due to unfavorable
properties
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What are the advantages of solid dosage forms?
Convenient,
stable
, and accurate dosing
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What are the disadvantages of capsules as a dosage form?
Susceptible to
moisture
and difficult to fill
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What is a unique feature of modified release capsules?
They release the
drug
slowly over hours
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What is the main advantage of granules as a dosage form?
Faster
dissolution rate
than
tablets
or
capsules
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What is a disadvantage of liquid dosage forms like syrups?
Risk of deterioration and loss of
potency
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