Pharmacology basics Flashcards

Cover the basic terms and understandings of pharmacology

1
Q

Define: a medicine

A

Any substance administered which may restore, correct or modify physiological function

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2
Q

Define: Pharmcology

A

The science of chemicals (food and medicine) and how they interact with the body

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3
Q

Define: pharmacodynamics

A

What the drug does to the body; the drug affect

Relationship between the concentrationn of drug at the action site and the response produced by the drug in the patient

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4
Q

Define: phwrmcokinetics

A

The way the body affects the drug over time:

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5
Q

Define: therapeutics

A

The branch of medicine concerned with the treatment of disease: translating action of drug into benefit for the patient

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6
Q

What are the 4 main target groups of drug action in pharmacodynamics?

A
  • Receptors (lock and key)
  • enzymes
  • carrier molecules/transporters
  • ion channel
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7
Q

Explain: receptors - lock & key (drug action)

A

Drug is the “key”, aiming to bind to the specific “lock”/receptor. Broken into agonist, partial agonists, or antagonists

They are protein molecules, usually found on the cell membrane, and usually respond to chemicals in the body

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8
Q

Explain: agonists (3 points)

A

Mimic the naturally occuring substrate that would usually respond to receptor site (mostly found on cell membranes)

Produces transduction mechanism on binding that causes a cascade of other effects or activating other enzymes

May also change channel shape (owning in the cell wall) to allow an influx/efflux of ions (e.g. Na, K+, Ca) which have a physiological effect

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9
Q

Define: partial agonists (+ example drug)

A

Activating receptors to produce desired response but not to a maximum level, to create a desired effect with less side effects

E.g. buprenorphine

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10
Q

Define: antagonists (3 points + 2 examples)

A

Bind and block, causing NO effect, or preventing any other drug/naturally occurring substrate to bind to receptor site.

Effect is either, - no effect or dampening down effect

Effects may be reversible or irreversible (depending on how long acting the drug is)

Salbutamol - B2 Agonist
PPI - short half life, but only OD as permanently binds to receptor site for its life

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11
Q

Explain: enzymes (3 points)

A

Proteins that speed up the chemical reaction in the body (catalysts). End in -ase

Drugs enhance or inhibit the enzymes in the physiological process within the body.

Most drugs that work on enzymes are enzyme inhibitors

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12
Q

Explain: enzyme inhibitors (and enzyme inducers)

A

Account for most drugs working on enzymes, blocking the enzyme from being metabolised.

  • enzymes are proteins, and cause a substrate to be made into an “product”
  • . If enzymes are prevented from being metabolised, the amount of “product” being produced is reduced, due to the substrate being reduced

Enzyme inducers do the opposite and speed up the process

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13
Q

Explain: HISTAMINE DIAGRAM

A

H2 is a histamine receptor (responsible for stomach acid production)

H2 receptor agonists have lock and key fit/receptors, reducing dyspepsia symptoms (e.g. ranitidine)

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14
Q

Explain: COX FLOW DIAGRAM

A

Cox = cyclooxygenase

NSAIDs are inhibitors - work on COX2 to reduce inflammation, pyrexia and pain, but as they are non-specific, also target COX1, giving negative effects on gastric mucus production and renal function, leading to s/e of dyspepsia, ulceration, upper GI bleed and renal failure

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15
Q

Explain: RENIN ANGIOTENSIN SYSTEM (RAS)

A

RAS important for maintaining water balance in the body and vasoconstriction, so is beneficial for control of BP.

Two enzymes involved are Renin and Angiotensin Converting Enzymes (ACE)
Angiotensin I leads to Angiotensin II production with ACE, which leads to aldosterone production, causing water and sodium retention, and causing negative feedback to reduce angiotensinogen.

ACE inhibitors - e.g. Ramipril - block after Angiotensin I, preventing ACE being produced, leading to less water and sodium retention, and so BP is lowered.

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16
Q

Explain: Carrier Molecules/Transporter

2 points and example

A

Like the “bouncers/ferry boat men”
Sit on the cell membrane and only allow passage if they have the right “properties” to be let into the cell.

Work on the action in the nerve synapse.
- drugs can affect cell transport mechanism (e.g. carrier proteins, or transporter)

e. g. Antidepressants act by preventing re-uptake of neurotransmitters
- reuptake is facilitated by reuptake transporter

17
Q

Explain: Ion Channels

3 points plus drug

A

Drugs that affect cell transportation

Interfere with the movement of ions across cell membranes.

Ion channels are openings within the cell membrane wall, and channel blockers are the drugs mainly used here

Ion channels can also be modulators, and bind to receptors on ion channels and change the shape of them (e.g. make it wider or narrow)
CCB: (amlodipine) prevent the influx of calcium ions, which lowers BP (as calcium moves through channel following a high to low gradient, which causes contraction of vesses which would increase BO)

18
Q

How do antacids work? (e.g. Aluminium chloride)

A

Neutralises stomach acid, does not need to go to cellular level

19
Q

How do alginates work?

A

works like a “raft” preventing regurgitation, working in the stomach, does not need to go to cell level

20
Q

How do emollients work?

A

Moisturise skin, don’t go to cellular level

21
Q

How does general anaesthesia work?

A

Reduces CNS function

22
Q

How do osmotic laxatives work? (e.g. lactulose, movicol)

A

Increase the amount of water in the large bowel

23
Q

What are the two main mode of action of antimicrobials?

A

Bactericidal & Bacteriostatic

24
Q

Explain: Bactericidal

2 points + example

A

Inhibits bacterial cell wall synthesis (e.g. Penecillins)

break up formation of cell wall leading to death of bacteria

25
Q

Explain: Bacteriostatic

2 points + example

A

Inhibits bacterial protein synthesis (e.g. macrolides - erythromycin)

Affects protein synthesis to prevent bacteria replicating itself properly

26
Q

How do antifungals work?

2 points + example

A

Inhibit ergosterol in fungal cell membrane.

Mammalian cells don’t use ergosterol, they use cholesterol, and drug targets this difference.

e.g. Nystatin

27
Q

What are the 4 broad processes involved in pharmacokinetics

A
  • Drug ABSORPTION
  • Drug DISTRIBUTION
  • Drug METABOLISM
  • Drug EXCRETION
28
Q

Explain: Absorption

A

The process of transfer of the drug from the site of administration into the systemic circulation

29
Q

What can affect absorption?

9 points

A
  • Route
  • Age (younger have different acid pH that changes with age, as do older people, topical also a risk due to thin skin)
  • Diet - interaction with food and medicine
  • Medical conditions - anything affecting blood flow to small intestine also affects absorption, or previous surgery
  • Gut content - full/empty
  • GI motility - how quick can the drug reach where it needs to be
  • Splanchic blood flow - what blood reaches there
  • Particle size and formulation - smaller the particle, the quicker theyre absorbed
  • physiochemical properties - is a drug lipid/water solube? drug formation, is it dispersible, MIR
30
Q

How can oral absorption be improved?

A

phsyiochemical factors, including some drug interactions

Changing strategy on getting drugs into the body

  • alter the physio-chemical properties - is it lipid/fat or water soluble?
  • change formulation? EC?
  • can the molecules be made smaller?
  • administered by various routes
31
Q

Explain: Distribution

A

Once in the systemic circulation, the durg needs to find its way to the site of action, and some will get eliminated before

32
Q

Explain: metabolism

A

Before it reaches the site of action, the drug passes through the liver, which leads to excretion

33
Q

Explain: Excretion

A

Once water soluble, drugs can be excreted by the kidneys

34
Q

Explain: Bioavailability

A

Proportion of a drug or other substance which enters the circulatory system

35
Q

Explain: Drug bioavailability factor (F)

A

Represents the decimal percentage of a drug substance available (e.g. 60% or 0.6, can be either way in the textbook)

36
Q

What affects bioavailability

A
  • Dosage form
  • Dissolution and absorption of drug
  • Route of admin
  • Stability of drug in GI tract (PO)
  • presence of food/drugs in GI tract (PO)
  • extent of drug metabolism before reaching systemic circulation (first pass metabolism)
37
Q

Explain: First Pass Mechanism

A

Once drug has been ingested, it goes through the stomach, into the GI mucosal layer, and is then transferred into the hepatic portal vein.

Blood then travels to the liver

Some drugs are inactivated in the gut or by the liver;

  • first pass gut examples: benpen and insulin
  • first pass liver examples - propranolol, lignocaine, GTN

This affects drug dose needed to be given via different routes.