Pharmacology Flashcards

Terms Definitions
What is Pharmacology
The study of the interaction of foreign chemicals with living systems
What is Therapeutics and it's goal with drugs?
Treatment of disease
Goal - deliver right amount of drugs for right amount of time with minimum adverse side effects
Drug Receptor Formula?
Drug + Receptor -> Drug Receptor Complex -> Biological Effect
What is Pharmacokinetics based on?
How the body reacts/what it does to the drug
For the Drug and Receptor, what pharmacokinetic properties can occur?
Absorption, distribution, Biotransformation, and Excretion
What is Pharmacodynamics based on?
What the drug does to the body
For the Drug Receptor complex what are pharmacodynamic properties?
Drug effects, mechanism of action
What is a receptor?
Any macromolecule that the drug interacts with to initiate a series of events leading to a pharmacological effect
3 Main receptor/Interaction types?
Classical, Non classical, and Non receptor mediated
Classical Receptors have what specificity?
Steric and Structural
Classical Receptors have a limited what, making them?
Limited number of binding sites making them Saturable
At physiological concentrations classical receptors have what?
A high affinity for endogenous ligands
What is an endogenous ligand?
a biological signalling molecule used for cellular communication
4 types of Classical receptor?
Ion channel
G Protein Coupled receptor
Transmembrane enzymes
Intracellular receptor
Example of Ion Channel receptor?
Nicotinic Ligand gated Ion channel
For nicotinic ligand gated ion channels what is the endogenous ligand?
Acetylcholine is the endogenous ligand substituted by Nicotine
which classical receptor is the targeted most?
G protein coupled
Example of a G protein coupled receptor?
Muscarinic GPCR
The muscarinic receptor usually does?
Decreases heart rate by acetylcholine release from vagus nerve and binding to the GPCR receptor at heart.
Also increases salivary gland secretion.
Transmembrane enzymes typically respond to what and act on what
Respond to growth factors or peptides hormones and usually act on gene expression
Example of a transmembrane enzyme receptor?
Insulin receptor, promoting glucose to glycogen reaction
Example of an intracellular receptor?
Estrogen
NOn classical receptors may be difficult to what?
May be difficult to saturate due to high concentrations of receptor
Non classical receptors often have what effects
Complex, non-specific physiological effects
Major classes of Non classical receptors?
Enzymes and Transporters
Example of Nonclassical Receptor?
COX enzyme clyclo-oxygenase, acted on by NSAIDS and Aspirin which normally helps catalyze reaction to produce prostaglandins
Antibiotics do what?
Interfere with bacteria by inhibiting cell wall synthesis, or protein synthesis, or nucleic acid synthesis
Example of a Non receptor mediated reaction?
Stomach acid neutralization with bicarbonate
HCl + NaHCO3 -> NaCl + H2CO3
H2CO3 -> H2O + CO2
Metal Chelators are what? Example/
non receptor mediated reactions, EDTA example used for heavy metal poisoning
What is the basic tenet of pharmacology?
For most drugs their effects are directly proportional to the concentration of their active forms at receptors
How is the concentration of drug in active form at receptor determined?
Dose and pharmacokinetics
The Time response curve involves?
Time to onset
Time to peak
Duration
Small charged molecules are what and diffuse best in what
Hydrophilic (lipophobic), diffuse best in aqueous
Small uncharged molecules are what and diffuse best in what
Hydrophobic (lipophilic), diffuse best in lipid biological membranes
Passive diffusion at lipid membrane involves?
Small uncharged diffusing through membrane, charged not
Examples of Lipophilic/Hydrophobic
Steroids, Diazepam, Estradiol
Hydrophilic drugs/molecules may be transported how?
Active transport (i dopa for parkinsons), facilitated diffusion (glucose transporters)
Hydrophilic/Small charged drugs are usually what
Weak acids or bases
At biological pH what do weak acids and bases do?
resonate between charged and uncharged forms
(RCOOH vs RCOO-) and (RNH2 vs RNH3+)
When can small charged molecules cross membranes?
WHen they are in their uncharged/non-ionized states
What is henderson hasselbach equation?
pKa = pH + Log(protonated concentration/unprotonated concentration)
pKa is?
pH at which 50% of the hydrogens have dissociated
What is absorption?
movement of drug from site of application to the bloodstream
What is Distribution
Movement of drug between blood and tissues
What is Biotransformation/Metabolism
the conversion of a drug to metabolites
what is excretion
removal of drug from the body to the external environment
What is the enteral route?
through GI tract - Oral, Sublingual, stomach/intestine absorption, Rectal
what is parenteral route?
bypass GI tract - IV, IM, SubQ, Inhalation, Transdermal/Topical
What factors control distribution? (4)
Rate of delivery to tissues due to blood flow
Ability of drug to pass through capillaries due to capillary permeability
Binding of drugs to protein and tissue components
Hepatic first pass effect metabolism before active site (oral admin gets this)
what in plasma may bind free drugs?
albumin
fluid compartments specialized?
blood/brain barrier, fetal placental
specialized tissue compartment
fat
most common sites of biotransformation? What can it involve?
Blood plasma and Liver, may involve deletion or addition of chemical group, and detoxification or activation of a drug
what biotransformation occurs in liver?
glucuronidation - conjugation with glucuronic acid making compounds less lipid soluble and better excreted
types of elimination
renal through kidneys
non-renal through lungs, sweat, saliva, feces, breast milk
What does Probenecid do?
Blocks or slows drug transport in kidney slows excretion of penicillin and tamiflu as examples
what is dosing
the quantity and interval at which a drug is administered to reach a steady state concentration
what was added to the salycylic acid to make aspirin less severe on stomach
an acetyl group
where is aspirin absorbed
stomach and intestine rapid in blood within 2 minutes
what is rate limiting step of aspirin
disintegration and dissolution of tablet
what deacetylates aspirin in blood
plasma esterases
elimination half life of aspirin
2-3 hours after single dose
aspirin side effects
dyspepsia, nausea, gastric bleedings, peptic ulcer
prostaglandins do what normally in stomach
mediate cytoprotective mechanisms in gastric mucosal cells to resist acid penetration
Mild salicylism
Tinnitus
reversible loss of hearing
headache
confusion
severe salicylism
respiratory stimulation and depression
acid base imbalance
coma, death
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