15/22/23 Flashcards
(39 cards)
Variation in the drug concentrations achieved by equivalent doses
inter-individual variation: Pharmacokinetics
What is much more important cause of the inter-individual variation in drug response in clinical practice
Variation in the drug concentrations achieved by equivalent doses
inter-individual variation: Pharmacokinetics
Factors affecting Individual variations in drug response
• Rates of drug absorption
• Rates of drug distribution
• Rates of elimination, either alteration in metabolism or excretion
• variety of drug interactions which may influence pharmacokinetic parameters
• Age
• The degree of plasma-protein binding
The degree of plasma-protein binding influences what?
influences the distribution, action, metabolism and renal excretion of drugs.
Variation in the response to equivalent drug concentrations arises because of various factors, such as:
- differences in receptor number and structure
- receptor-coupling mechanisms
- and physiological changes in target organs resulting from differences in genetics, age and health.
- sensitivity of receptors/enzyme targets to drug changed with age or disease
result in altered responsiveness in drug
targets (e.g. receptor function) or (e.g. enzyme activity).
genetic polymorphisms
Examples of personalized medicine
using targeted therapies to treat specific types of cancer cells, such as Trastuzumab HER2-positive breast cancer cells
Acetylcholine from …… fibers
Cholinergic
Ex of Cholinergic Receptors
Nicotinic (N)
Muscurinic
Ex of Adrenergic Receptors
Alpha/Beta
Alpha-1 receptors
- Vasoconstriction
- Mydriasis
- Contraction of the GIT &urethral sphincters
- Increase B.P
Alpha-2 receptors are mainly ……
presynaptic
Which receptor stimulation decreases nor adrenalin release
Alpha-2
Beta-1 works mainly on?
Heart
(+) inotropic effect (^ force)
(+) chronotropic effect (^rate)
Beta-2
bronchodilatation,
uterus, bladder & GIT wall relaxation
vasodilatation of B.Vs
Steps of adrenergic transmission
Synthesis
Store in vesicles
Release
Binding to receptor
Degradation/metabolism
Reuptake
Adrenaline is
Catecholamine Direct Adrenergic agonists SYMPATHOMIMETICS non-selective
Noradrenaline is
Catecholamine Direct Adrenergic agonists SYMPATHOMIMETICS non-selective
Dopamine
Catecholamine Direct Adrenergic agonists SYMPATHOMIMETICS non-selective
D1 (minimal doses)
ß1 (intermediate dose)
alpha1 (high dose)
Phenylephrine is / act on which receptor?
Non-catecholamines Direct Adrenergic agonists SYMPATHOMIMETICS selective
Alpha1
Albuterol is / act on which receptor?
Non-catecholamines Direct Adrenergic agonists SYMPATHOMIMETICS selective
Beta2
Epinephrine release into the bloodstream brings about several physiological changes, such as:
• increased heart rate
• Broncho dilatation
• raised blood sugar levels
• increased strength and physical performance
Epinephrine acts on the alpha- and beta-adrenoreceptors in the ?
muscles, lungs, heart, and blood vessels.
Norepinephrine promotes what that causes what?
vasoconstriction, which is a narrowing of the blood vessels, and this increases blood pressure.