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Dan NPM > NPM > Flashcards

NPM Flashcards

1
Q

Enzyme inducers

A

Example:
Phenytoin,
phenobarbital

  • enhance the (production of) liver enzymes which
    break down drugs
  • faster rate of drug breakdown
  • larger dose of affected drug needed to get the same
    clinical effect
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2
Q

Enzyme Inhibitors

A

Example :
Clarithromycin
omeprazole
* inhibit the enzymes which break down drugs
* decreased rate of drug breakdown
* smaller dose of affected drug needed to produce the
same clinical effect

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3
Q

CYP3A4

A

Simvastatin (substrate)
Inhibitor (Clarithromycin)
EQUALS:
Rhabdomylysis

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4
Q

CYP3A4

A

Birthcontrol (Substrate)
Inducer (Carbamazepine)
EQUALS:
Undesired Pregnancy

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5
Q

Factors affecting drug excretion

A
  • Age
  • Disease (CKD, atherosclerosis)
  • Physicochemical properties of drug
  • pH of urine
  • Protein binding
  • Drug interactions (NSAIDs, Ciclosporin)
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6
Q

Drugs excreted largely unchanged

A

Percentage 100-75%

Furosemide (frusemide), gentamicin,
methotrexate, atenolol, digoxin
75-50% Benzylpenicillin, oxytetracycline,
trimethoprim

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7
Q

drug examples Receptors

A

Morphine Agionist Mu
Naloxone Antagionist

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8
Q

Ion channels
drug example

A

Amlodipine Antagionist
Blocks CCB

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9
Q

Enzyme
drug examples

A

Ramipril/ibuprofen

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10
Q

Transporter
drug examples

A

sertraline SSRI
Blocks the reuptake of seritonin

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11
Q

Affinity

A

measure of the tightness with which a drug binds to
the receptor

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12
Q

Selectivity

A

specific affinity for certain receptors (vs. others)

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13
Q

Drug efficacy

A

the maximum effect the drug will produce on its target
site, e.g. blocking pathway; this is not always related to the
disease treatment efficacy or therapeutic value

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14
Q

Potency

A

the amount/concentration of drug needed to produce a
given effect; the less concentration required to achieve an
effect the more potent the drug is.

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15
Q

what beta-adrenergic receptors
sub-types are known and where
they are located in the body

A

B1B2B3

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16
Q

what is drug tolerance

A

Reduction in body’s response to medication
PD - Changes the ability of a drug to exert its effect
PK - Most common the body breaks the drug down more quickly

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17
Q

What is drug interaction?

A

An interaction occurs when the effect of one drug is
affected by the presence of another drug(s), food,
drink, herbal remedies or some environmental
substances

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18
Q

ADR PK: Distribution

A

After absorption drugs are then moved and distributed
to its site of action(s). During this process presence of
other drugs may interfere with its distribution and
mainly affect its binding to plasma proteins e.g. albumin.
This type of interaction is more significant with drugs that
highly protein bound and have a narrow therapeutic
index.
* Phenytoin and valproic acid
* Warfarin and aspirin

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19
Q

ADR PK: Absorption

A

Absorptions of one drug may be reduced or enhanced by
presence of another drug/food/drinks/herbal.
* Paracetamol and caffeine
* Doxycycline and Iron supplements
* Food and flucloxacillin
* Fentanyl patches and heat

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20
Q

ADR PK: Metabolism

A
  • One of the most important mechanism where clinically
    relevant interactions occur.
  • Drug metabolism is via liver enzymes, cytochrome P450,
    CYP.
  • The metabolism of one drug is enhanced or reduced by
    another drug if the production or action of the enzymes
    involved are affected.
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21
Q

Enzyme inhibition

A

Inhibition:
* Inhibit the enzymes which break down drugs
* Decreased rate of drug breakdown
* Smaller dose of affected drug needed to produce the same
clinical effect

22
Q

Enzyme Induction

A

Induction
* Enhance the (production of) liver enzymes which break
down drugs (usually delayed reaction)
* Faster rate of drug breakdown
* Larger dose of affected drug needed to get the same clinical
effect

23
Q

Examples of CYP3A inhibitors include

A

*Ketoconazole
*Itraconazole
*Fluconazole
*Cimetidine
*Erythromycin
*Grapefruit juice

24
Q

Examples of CYP3A inducers include:

A

*Carbamazepine
*Rifampicin
*Rifabutin
*Barbiturates
*St John’s wort

25
ADR PK: Excretion
Important mechanism of interaction. The excretion of one drug is affected by another, it can increase/decrease its excretion resulting in less therapeutic effect or TOXICITY. * Sodium and lithium * NSAID and methotrexate
26
Pharmacodynamic interactions
**Antagonism**– two (or more) drugs can have opposite effect * Propranolol and salbutamol **Synergism**- two (or more) drugs can have additive effector potentiate each others actions, which could be useful or harmful. * Ramipril and Amlodipine
27
what is Pharmacogenomics
Genetic explanation of individual variability in PK or PD E.G **CYP2D6 and codeine metabolism:** ultra-rapid metabolisers vs poor metabolisers
28
Factors which can increase the fraction of unbound drug
rise in blood urea due to renal impairment * low plasma protein albumin levels (age, liver disease, renal disease, malnutrition) * late pregnancy * displacement from binding site by other drugs – binding for some drugs may be as high as 99%
29
Metabolism
* Primary site: liver * Set of processes aiming at deactivating chemicals and enabling their elimination. * prodrugs (e.g. codeine, enalapril, loratadine) require activation. * metabolites can be active (morphine, benzodiazepines) or even toxic (paracetamol metabolite NAPQI). * Liver enzymes vary depending on genetics. * Metabolic rate can be affected by disease conditions (liver failure) or medication (enzyme inducers); it also differs individually and generally reduces with age
30
Biosimilar medicines
biologics that are highly similar and clinically equivalent (in terms of quality, safety, and efficacy) to an originator medicine (existing biological medicine) * the difference? - active substance of a biosimilar medicine is similar, but not identical, to the originator biological medicine * biosimilar medicine is not the same as a generic medicine (which contains a simpler molecular structure that is identical to the originator medicine)
31
Bioequivalence
Bioequivalent drugs are expected to have the same systemic bioavailability and are predicted to elicit comparable response.
32
Bioavailability
The rate and extent to which the active ingredient is absorbed from the drug product and becomes available in systemic circulation.
33
Factors affecting absorption Drug factors
* Dosage form (e.g. tablet disintegration/dissolution) * Lipid solubility * Particle size * Concentration (dosage) * Susceptibility to 1st pass metabolism
34
Factors affecting absorption Patient/environment factors
* Blood flow (different organs have different blood supply) * GI pH (e.g. benzylpenicillin cannot be given orally as it degrades in stomach pH) * Surface area (disease states e.g. inflammation in Crohn’s or surgeries e.g. gastric bypass) * Interactions with food, other drugs (reduced gut motility with opioids or metoclopramide; pH changes with antacids, PPIs) * Compliance
35
Drugs with high extraction rate
GTN salbutamol
36
Hepatic ‘first-pass’ metabolism
* Affects orally administered drugs * Metabolism of drug by liver before it reaches systemic circulation * Usually reduces bioavailability of drug * Cases where initial metabolism of drug is beneficial: pro- drugs (ramipril, codeine, L-dopa)
37
Routes of administration avoiding first-pass effects:
IV, IM, SC, sublingual, rectal, inhaled, buccal, inhaled, transdermal
38
Transport across biological membranes
Passive Diffusion Facilitated Endocytosis ACTIVE TRANSPORT (needs ATP)
39
Biotransformation
a metabolic process that takes place mainly in the liver and helps to facilitate the excretion of both exogenous and endogenous substances
40
Define the term biosimilar medicine
A biological medicine that is highly similar and clinically equivalent (in terms of quality, safety and efficacy) to an existing biological medicine (reference biological medicine or originator medicine). However differs from the reference/originator medicine in that the active substance is similar but not identical.
41
Drug Y is highly protein bound (99%). Explain why highly protein bound drugs might be subject to significant drug-drug interactions
Means most drug is protein bound with only a small amount of free drug. Anything that disrupts this e.g. displacement by another drug will significantly increase the proportion of free drug leading to toxicity or ADRs. Any similar wording.
42
Define the term bioavailability:
The proportion of drug administered that reaches systemic circulation usually expressed as a percentage - or equivalent types of wording.
43
Explain the difference between pharmacokinetics (1 mark) and pharmacodynamics (1 mark).
Any suitable wording around the theme pharmacokinetics is what the body does to a drug. Pharmacodynamics is what the drug does to the body. Illustrations featuring ADME for kinetics and targets of action for dynamics.
44
Name two issues encountered in renal impairment?
May cause toxicity. Sensitivity to some drugs. Many side effects tolerated poorly by patients Drugs not effective.
45
Give two reasons why using a prodrug may be a useful way to design a drug for oral administration.
To increase bioavailability To decrease adverse effects To increase safety before administration To decrease costs
46
Drugs and/or their metabolites are mainly excreted by the kidneys. Name one other possible routes of excretion for drugs.
breast milk
47
Define both the terms agonist and antagonist
Agonist – a drug that causes a response Antagonist – a drug that prevents a response
48
Give one example of an antagonist drug and one example of an agonist drug.
Agonist drug: Any correct example e.g. adrenaline, salbutamol Antagonist drug: Any suitable example e.g. propranolol, naloxone NOT enzyme inhibitors
49
A prodrug is..
An inactive form of the drug that is metabolised into an active drug by the body
50

Dan NPM (1 decks)

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