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