5: Pharmacology of Major Drug Classes Flashcards

1
Q

What is Chemotherapy?

A
  • The use of chemicals to destroy pathogens which have invaded the body
  • It includes the use of chemicals to destroy our own cells which have become malignant
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Enemy Bacteria: Cell Wall Synthesis

A

Our cells don’t have cell walls, but they are vital to the survival of bacteria and fungi. Disruption of the ability to make or maintain the cell wall will therefore destroy the bacteria but not affect our cells (penicillin)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Enemy Bacteria: Protein Synthesis

A

Bacteria synthesise proteins like our cells do, but their ribosomes are different. Here again, is a point that could be disrupted without harming our cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Enemy Bacteria: Cell Membrane

A

Our cells have a cell membrane of course, and the bacterial cell membrane is similar to ours (phospholipid bilayer), but in bacteria it is much more readily disrupted by detergents than ours

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Enemy Bacteria: Metabolic Pathways

A

The best example is the synthesis of folic acid. Folic acid is vital for all cells – it is involved in the process of DNA synthesis. However, we have to absorb and use folic acid from our food, as we cannot synthesise it, whereas bacteria and fungi have to make theirs, as they cannot absorb it. Blocking the production of folic acid will therefore prevent the bacteria from synthesising DNA and therefore replicating. Drugs that act in this way are known as bacteriostatic. Successful use of these drugs does depend on an effective immune system in the patient, though

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Enemy Bacteria: RNA or DNA Synthesis

A

All cells have to do this, but in bacteria, different enzymes are used at some stages. Again, this can be exploited to prevent the cells from reproducing

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Enemy Bacteria: Recognising or Attaching Host Cells

A

The ability to recognise or attach to a host cell impact on the ability of the invaders to spread from cell to cell and therefore take over. Reducing this ability can give the immune system time to deal with the pathogens before it is overwhelmed by their rapid proliferation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Enemy Fungi

A
  • Most prominent lipid in fungi cell membranes is ergosterol
  • Different lipid, therefore different enzymes to make it. A point of attack that will disrupt the fungal cell membrane but not harm ours
  • Cell wall enzymes or components can be attacked (we don’t have so it won’t affect us)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Enemy Viruses

A
  • The virus is essentially a bundle of RNA inside a protective coat
  • In order to reproduce and spread successfully, it has to hijack our own cell’s machinery
  • The points of attack for viruses therefore, tend to be in the way they interact with the host cells
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Tumour Cells

A
  • Difficult to differentiate cancer cells from healthy ones
  • No structural or metabolic differences to exploit
  • Cytotoxic effects on both cancer cells and healthy cells
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Cytotoxic Drugs

A
  • Cell death by apoptosis

- Damage the cell’s DNA or disrupt the separation of chromatids during mitosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Treatment of Mania

A
  • Most commonly seen as a component of bipolar disorder
  • Lithium is a mood stabiliser, which “evens out” moods, and limits the occurrence of manic episodes and also of depressive episodes:
    > Narrow therapeutic index (margin of safety) and so blood levels need to be monitored
    > Toxic doses can result in confusion, seizures and coma
    > Side effects include fine muscle tremor, nausea, vomiting, diarrhoea, polydipsia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Lithium: Mechanism of Action

A

Reduces excitatory (dopamine and glutamate) but increases inhibitory (GABA) neurotransmission

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Autonomic Drugs

A
  • Potential to be used for many conditions, since these can manipulate autonomic effects in organs and glands
  • In practice, use is limited, as side effects are often a problem
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Autonomic Neurotransmitters: Sympathetic Division (Fight or Flight)

A
  • Noradrenaline

- Adrenaline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Autonomic Neurotransmitters: Parasympathetic Division

A

Acetylcholine

17
Q

Receptors for Acetylcholine: Cholinergic Receptors

A
  • Nicotinic – found on skeletal muscle, produce contraction

- Muscarinic – found in brain and on organs and glands, produce parasympathetic response

18
Q

Clinical Uses for Autonomic Drugs

A
  • Treatment of hypertension
  • Reduction of risk of cardiac arrhythmia after an M.I.
  • Treatment of asthma
  • Treatment of glaucoma
  • Treatment of nasal congestion
  • Treatment of diarrhoea, motion sickness
  • Emergency resuscitation (cardiac arrest)
  • Treatment of anaphylaxis
19
Q

Analgesics: NSAIDs

A
  • Reduce inflammation
  • The NSAIDs operate by reducing the stimulation of nociceptors by reducing the production of inflammatory mediators in response to tissue damage
20
Q

Analgesics: Opioids

A
  • Act more centrally
  • The opioids act at the site of tissue damage, in the spinal cord and also in the brain, to reduce the pain signals. In doing this, opioid drugs are simply mimicking the effects of our natural endogenous opioids on their own pain modulation system
21
Q

Pain

A
  • Nociceptors signal pain to brain via spinal cord
  • Perceived in the cerebral cortex
  • Activates the limbic structures of the brain, responsible for emotions
22
Q

Inflammation Cardinal Signs

A
  • Heat
  • Redness
  • Swelling
  • Pain
  • Loss of function
23
Q

Inflammation: Prostaglandins and Histamine

A
  • P stimulate pain receptors

- Histamine causes blood vessels to dilate and also increase their permeability

24
Q

How do NSAIDs Have Their Effects?

A
  • Act by inhibiting the enzyme cyclooxygenase (COX)
  • This enzyme is required for the production of prostaglandins
  • NSAIDs are analgesic, anti-inflammatory, and anti-pyretic
25
Q

Narcotic Analgesics Are….

A

Agonists at our endogenous opioid receptors

26
Q

Endogenous Opioids

A
  • Our are: beta endorphin, enkephalins and dynorphin
  • The endogenous opioids and their neurons form a pain modulation system that operates during extreme stress
  • This system “damps down” pain signals when it might be detrimental to be experiencing extreme pain
27
Q

Effects of Opioid Agonists

A
  • Respiratory depression
  • Constriction of pupils
  • Nausea & vomiting
  • Constipation
  • Sedation
  • Cough suppression (codeine, pholcodine)
  • Sphincter of Oddi & ureter spasms (morphine)
  • Tolerance & dependence
28
Q

Tolerance and Physical Dependence

A
  • Develops after about 2-3 weeks of regular dosing. Faster with higher doses and more frequent doses
  • Cross-tolerance with other opioids occurs
  • In a naïve person, 60 mg of morphine - respiratory arrest
  • In a tolerant person, 2000 mg over a 2-hour period may not produce much respiratory depression at all
  • Tolerance to the sedating and respiratory depressant effects is lost after a few days off the drug
29
Q

Opioid Overdose Signs

A
  • Pinpoint pupils
  • Decreased respiratory rate (even apnoea)
  • Coma
  • Hypotension
  • Convulsions
30
Q

Treatment of Opioid Dose

A
  • Opioid antagonist – naloxone or naltrexone
  • In addicts, a large dose may precipitate explosive withdrawal syndrome, and patient will regain consciousness
  • Antagonist may be titrated to reduce respiratory depression but maintain sedation
  • Naloxone has a relatively short duration of action so repeat dosing required to prevent relapse