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Sports Pharmacology Exam 1
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Terms in this set (72)
Pharmacokinetics
the processes of drug absorption, drug distribution, drug metabolism, and drug excretion.
Neurotransmitter
a chemical released by one neuron that alters activity of another neuron.
EPSP
Excitatory Post Synaptic Potential: speed up action potential.
IPSP
Inhibitory Post Synaptic Potential: slow down or block an action potential.
Ways to alter synapse:
1) Block excretion of neurotransmitter.
2) Block re-uptake of a neurotransmitter.
3) Block post-synaptic receptor site.
4) Destruction of a neurotransmitter by enzymatic activity.
5) Mimic of a neurotransmitter.
6) Mimic an enzyme.
7) Stimulate post-synaptic receptor.
8) Inducing release of a neurotransmitter.
Drug
a substance, chemical (natural or synthetic) that cause appreciable change in homeostasis when ingested.
Ways a drug can be administered:
1) Oral administration: must be stable in stomach fluid and be able to get into bloodstream.
2) Rectal administration: if person is vomiting.
3) Inhalation: very fast absorption rate due to surface area of lungs, proximity to pulmonary veins, popular method of illicit drugs.
4) Mucous membranes: works very quickly.
5) Skin administration: nicotine and estrogen in patch form.
6) Intravenous: easier than oral admin, precise dosage, immediate altering effects, most EFFECTIVE way.
7) Intramuscular: absorbs rapid but slower than IV, rate of absorption depends on blood flow and drug solubility.
8) Subcutaneous: allergy testing, and small amount under skin.
Intravenous
fastest way of absorption and administration.
Homeostasis
normal state of balance among body's internal organs.
Synergism
combination of two drugs exceeds the sum of the two.
Synesthesia
taking something that causes neurotransmitter breakdowns such as hallucinogens, hearing light and seeing sounds.
Addiction
purely psychological and more permanent, it is genetic.
Dependence
withdrawal symptoms with the sensation of the drug, "abstinence symptom".
What do drug dosages depend on?
Male, 150lbs.
ED50
Effective Dose: effective dosage for 50% of population.
LD50
Lethal Dose: dosage that kills 50% of population.
Therapeutic Index
LD50/ED50: LD should be higher than ED50, biggest safety margin.
Safety Margin
Difference between ED50 and LD50, OTC drugs have a pretty large safety margin.
Drug Excretion
Desired effect over, primarily due to hepatic exposure and kidney filtration.
The common ways of drug excretion are:
renal (urine), GI (feces), and respiratory (exhaled gases).
Drug Excretion Mechanisms
Lungs: example alcohol
Skin: 15% of drugs eliminated.
Bile: small amounts.
Kidneys: can eliminate inactive or active metabolites or actual drug.
Liver: in charge of metabolism
Drug Half-Life
time it takes for the drug effect to fall by 1/2 in the blood stream.
pH
dictates ionization and unionization of drugs. Body ph:
1.0 = gastric juice
2.0 = upper int.
6.6 = lower int.
4.5 - 7.0 = urine
7.3 - 7.4 = blood
Buffers
chemicals added to drugs for a purpose such as to make it absorb in different locations.
Binders
chemicals added to drugs for a purpose such as holding a drug together for consumption.
Acid/Base Concept
Most drugs are termed "weak acids" or "weak bases".
Weak acid = Base
Weak base = Acid
Acidic drugs
easily absorbed in stomach, not ionized, exist largely in fat soluble form.
Alkaline drugs
not given orally because they become "ion trapped" in stomach, not readily diffused across cell membrane, injection or suppository.
MAO
Mono-amine Oxidase: enzyme that metabolizes norepinephrine, dopamine, and serotonin.
Six types of Tolerance
1) Cross-tolerance
2) Reverse tolerance
3) Inverse tolerance
4) Neuronal tolerance
5) Enzyme-induction tolerance
6) Behavioral tolerance
Cross-tolerance
tolerant to one depressant you will be tolerant to all depressants.
Reverse tolerance
people will elicit same response at a much lower dosage than previously taken.
Inverse tolerance
first time users may not experience any response at all.
Neuronal tolerance
brain specific nerve tissue tolerance such as alcoholics who appear sober.
Enzyme-induction tolerance
your liver produces enough of the enzyme to take care of the drug, most common type of tolerance.
Behavioral Tolerance
a person learns how to control the way a drug makes them behave.
Drug Abuse
taking a drug for a use other than intended.
Indication
what the drug is prescribed or indicated for.
Contraindication
not a side effect, "don't use if" begins statement.
Ionized state
- drug is "electrically charged" and water soluble.
- does not cross cell membrane.
- quantity of drug is higher where degree of ionization is higher.
Unionized state
- readily cross a cell membrane and will be readily absorbed.
- fat soluble.
Zero-order Kinetic
a set amount of a drug is metabolized or excreted over a given amount of time, nothing can be done to speed up or get rid of the effect.
Agonists
bind to specific receptor and produce drug action.
Antagonists
blocks other drugs.
Hyperpolarized
change in membrane potential that makes inside of cell more negative so it can't respond to stimulation.
Uptake
"first pass metabolism", concentration greatly reduced before reaching systemic circulation.
Reuptake
taken back up into body again and metabolized again.
Metabolite
products of metabolism that may be as active as original substance.
Metabolism
breaking down
Three kinds of drug names/nomenclatures?
Brand or Trade name
Generic name
Chemical name
Drug References
-United States Pharmacopeia/National Formulary
-Physicians' Desk Reference
-Drug Facts and Comparisons
-United States Pharmacopeia Dispensing Information -Drug Informations American Hospital Formulary
Service
Drug Facts and Comparisons
Most recent and current information for drugs, monthly.
Polypharmacy
situation that involves multiple drug prescriptions.
Factors of aging that affect drug absorption
- decrease in blood flow to intestinal tract
- decrease in gastric acid secretion
- decrease in intestinal motility
Factors of aging that affect drug distribution
- decrease in lean body mass and body water
- decrease in plasma proteins like albumin
- increase in body fat
Factors of aging that affect drug metabolism and excretion
- decrease in metabolism rate
- decrease in DMMS
- decrease in renal blood flow
DMMS
drug microsomal metabolizing enzyme that oxidize drugs.
Creatinine
product of muscle metabolism excreted by the kidneys.
Creatinine Clearance
Test to determine kidney function.
Factors of aging that affect drug response
- Nutritional Status
- Presence of chronic diseases
- Alteration of pharmacodynamic response
- Drug compliance
Drug compliance
following drug prescription directions exactly as written.
Nm
Nicotinic-muscle receptor: located on skeletal muscle.
Stimulated by ACH from somatic nerves to contract skeletal muscle.
Nn
Nicotinic-nerve receptor: located on parasympathetic and sympathetic ganglia.
Stimulated by ACH to conduct impulses across autonomic ganglia to the postganglionic fibers if both autonomic divisions.
Organs that regulate visceral nerves
Hypothalamus and Medulla Oblongata
How do we lower blood pressure?
...
Tachycardia
caused by a disruption in the normal electrical impulses that control our heart's pumping action rhythm, the rate at which our heart pumps.
Causes of Tachycardia
coronary artery disease (atherosclerosis)
heart valve disease
heart failure
heart muscle disease (cardiomyopathy)
Hypertension
Smoking
Sympathetic
Adrenergic = Norpinephrine
Parasympathetic
Cholinergic = ACH
Alpha 1 receptors
Vasoconstriction of blood vessels, contraction of smooth muscle.
Beta 1 receptors
Found on heart and mediate cardiac simulation, an increase in heart rate and force contraction.
Beta 2 receptors
Found on smooth muscle and relax smooth muscle, relaxation of respiratory smooth muscle (bronchodilation).
Norepinephrine Synthesis
Used to lower blood pressure.
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