Pharmacology Flashcards
Drug Targets
- Receptors
- Enzymes
- Transporters
- Ion channels
Affinity and efficacy
Affinity = how well ligand binds to receptor
(antagonists + agonists)
Efficacy = how well a ligand activates receptor
(agonists)
Tolerance
Reduction in drug effect over time
Desensitisation of receptors
- Uncoupled - can’t interact with G protein
- Internalised - in vesicle
- Degradation
B blockers - contraindication
Asthma
Bronchoconstriction
Compartments of water
- Intracellular 2/3
- Extracellular 1/3
- Plasma (20% of ECF)
Movement between compartments
- Simple Diffusion
- Facilitated Diffusion
- Non-ionic diffusion
- Active transport
Stages of Pharmacokinetics
- Absorption
- Distribution
- Metabolism
- Excretion
Bioavailability
Amount of drug taken up as proportion of amount administered
Reporting ADRs
- MHRA Yellow Card scheme
- All suspected for new medicines
- All in children
- All serious reactions
Naloxone
- Competitive receptor antagonist of morphine
2. Correct morphine overdose - resp depression
Therapeutic index
Dosage difference between therapeutic effect and toxic affect
Simvistatin
Types of ADRs
ABCDE A - Augmented (extension of clinical effect) B - Bizarre (unexpected C - Chronic (LT therapy) D - Delayed (many years) E - End of use (withdrawal)
Adherence
Extent to which patient’s actions match agreed recommendations
Anaphylaxis
- Type 1 hypersensitivity
- IgE mediated
- Prior exposure to drug
- Mast cell degranulation
- Histamine
- Thromboxane / prostaglandins
- TNF - Rash
Half life
Time taken for plasma drug concentration to fall to half of its original value
Adreno-receptors
A1 = vasconstricion, pupil dilation + bladder contraction A2 = presynaptic inhibition of neuroadrenaline --> reduce insulin release B1 = increase HR + force + electrical conduction, more renin + increased BP B2 = bronchodilation, vasodilation + less GI motility B3 = more lipolysis, relax bladder
Type 2 diabetes - Treatment
- Lifestyle + dietary changes
- Biguanide - Oral Metformin
- Sulfonylurea - Oral gliclazide (HbA1c >53mmol/L 16wks)
- HbA1c >57mmol/L 6mths
- Isophane insulin
Hyperkalaemia - Treatment
Calcium gluconate
Hepatic extraction ratio
Proportion of drug removed by one passage through liver
EC50
EC50 = conc that gives half the maximal response