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Pharmacology. > 4. Drug effects and interactions > Flashcards

4. Drug effects and interactions Flashcards

1
Q

What is an unwanted drug effect?

A

Any noxious or unintended reaction when a drug has been given correctly (dose, route, person etc).

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2
Q

What are the three categories we can divide ADR’s into?

A
  1. Can happen to anyone: OD (excess dose or impaired secretion), side effects, interactions.
  2. Susceptible people: intolerance and idiosyncrasy e.g. genetically determined such as sux apnoea.
  3. Allergies.
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3
Q

What is a pseudo allergy?

A

One that manifest similarly clinically due to histamine release, but not immune mediated e.g. morphine.

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4
Q

What are the A to F classifications of ADR’s,with examples?

A

Augmented: dose related e.g. propofol hypotension = dose related
Bizarre: not dose related e.g. Anaphylaxis = dose unrelated
Chronic: dose and time e.g. propofol infusion syndrome = dose and time
Delayed: time related e.g. fluoride nephrotoxicity = time related
End of use: withdrawal e.g. clonidine rebound hypertension = withdrawal
Failure: unexpected failure e.g. the pill = unexpected failure.

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5
Q

What is the DOTS classification of ADR’s?

A

Dose related: sub therapeutic doses, therapeutic doses and sub in susceptible

Time related: rapid (administered too quickly), first dose (e.g. hypotension with ACEi- may not recur), early (gets better e.g. nitrate headache), intermediate (Coombs 2 to 4), late (e.g. withdrawal) and delayed (e.g. post exposure)

Susceptibility

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6
Q

What are the three different broad categories of drug interactions?

A

Pharmacodynamic
Pharmacokinetic
Pharmaceutical incompatibility

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7
Q

What are the different types of pharmaceutical incompatibility with examples?

A

Neutralisation e.g. heparin and protamine

Precipitation: thio and sux

Chelation: sugammadex and roc

Absorption: halothane into rubber. Paraldehyde and plastic (needs glass syringe)

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8
Q

What are the different pharmacokinetic interactions with examples?

A

Absorption: charcoal and poisoning or prokinetics

Distribution: anything that alters cardiac function e.g. beta blockers make it longer for sux to work

Metabolism: e.g. enzyme inducers

Elimination: e.g. doxapram makes volatiles be eliminated more quickly

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9
Q

What are pharmacodynamic interactions?

What are the different categories with examples?

A

When drugs have an agonist or antagonist effect on other drugs. Can be direct or indirect.

Summation: additive e.g. nitrous and volatiles

Synergism: paracetamol and opiates

Potentiation: non depolarising NMB and Mg

Antagonism: flumazenil and benzo’s (direct)

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10
Q

What can hyponatraemia do to a commonly used anaesthetic drug?

A

Potentiate LA’s

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11
Q

What does echinacea do and what interactions does it have?

A

Modulates cytokines, and stimulates macrophages and NK’s

Avoid with hepatotoxic

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12
Q

What does ephedra do and what interactions does it have?

A

CNS stimulant, weight loss and asthma treatment as is a sympathomimetic

Caution with others. Log term use can deplete catecholamine stores causing tachyphylaxis. Arrhythmia with halothane

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13
Q

What does garlic do and what interactions does it have?

A

HTN, hyperlipidaemia and atherosclerosis

Increased bleeding risk

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14
Q

What does ginger do and what interactions does it have?

A

Anti inflammatory and anti emetic through inhibiting serotonergic pathways and stimulating the GI tract

Risk of bleeding

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15
Q

What does ginko biloba do and what interactions does it have?

A

Neuroprotective and increased blood flow as is a free radical scavenger with antiplatelet effects

Increased risk of bleeding

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16
Q

What does ginseng do and what interactions does it have?

A

Mood enhancer / aphrodisiac - sympathomimetic

Risk of bleeding, hypoglycaemia and interactions with other sympathomimetics

17
Q

What does St John’s wart do and what interactions does it have?

A

Antidepressant - inhibits MAO and induces CYP3A4 and 2C9

Serotonergic crisis, sedative, reduces effect of: midazolam, alfi, lidocaine, warfarin and NSAIDs

18
Q

What does valerian do and what interactions does it have?

A

Anxiolysis by potentiating GABA

Reduced anaesthetic requirement

19
Q

What is a drug?

A

An exogenous substance that alters a physiological system.

20
Q

What are the 6 kinds of non-specific Physiochemical reactions of a drug?

Examples of each

A

Adsorption = charcoal and paracetamol
Bonding = covalent etc.
Chelation = O, N or S make coordinate bonds with heavy metals
Neutralisation = sodium citrate or protamine and heparin
Osmotic = mannitol
Radio opacity = contrast

21
Q

What is a ligand?

A

Chemical messenger with the ability to bind to a receptor

22
Q

What is a receptor?

A

An area of a tissue, molecule or membrane which responds specifically to the binding of a ligand

23
Q

What are the two main categories of drug receptors?

A

Membrane and nuclear

24
Q

What are the three main types of membrane drug receptors?

A

GCPR’s
Enzyme linked
Channels

25
Q

What is a g coupled protein receptor?

How are they activated?

How many drugs use these? Examples?

A

Membrane receptor with an intracellular and extracellular binding domain, with 7 transmembrane proteins.
G protein = alpha, beta and gamma subunits

Activated via association of alpha subunit triggering a secondary messenger.

50% of drugs use them e.g. atropine, or phone and salbutamol.

26
Q

What is the basic make up of enzyme linked membrane receptors?

A

Extracellular ligand binding domain
Transmembrane amino acids
Intracellular active enzyme domain - usually kinases.

27
Q

What type of receptors do anaesthetic agents predominantly target?

A

Channels

28
Q

What are the the main types of membrane channels and examples of some others?

A

Voltage gated or ligand gated e.g. nicotinic.

Aquaporin and CFTR etc.

29
Q

What are the two different types of nuclear receptor?

A

Type 1 =ligand binds to cytosol receptor

Type 2 = ligand binds directly to DNA

30
Q

What is drug tolerance?

A

Reduced response to a drug after repeated or prolonged exposure (reduced potency)
- reversed with a holiday
- toxic dose can stay the same

31
Q

What are the different types of drug tolerance?

A

Innate e.g. in high BMI or genetics

Acquired:
- pharmacodynamic = e.g. receptor down regulation
- kinetic e.g. alcohol enzyme induction
- behavioural e.g. opiates

Cross tolerance: resistance to one drug, reduces effect of another e.g. heroin and methadone.

32
Q

What is tachyphylaxis?

A

Hyper acute drug tolerance e.g. hydralazine or ephedrine.
- can happen after first dose.

33
Q

What happens in nitrate tolerance?

A

Lack of vasodilation due to tolerance to NO.

34
Q

What is inversely drug tolerance?

A

Sensitisation, where taking the drug heightens the effect over time

Pharmacology. (22 decks)

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