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PB&T Vocab: Pharm, ANS, Chemotherapy, etc
Terms in this set (64)
endogenous catecholamine: NOREP, EP, and DOPAMINE
Functions (4): Cardiac rate & force, resistance of blood vessels and bronchioles, release of insulin, breakdown of fat
ANS: Both sympathetic & parasympathetic
Mediated by ACETYLCHOLINE
In neuromuscular junction, ANS, CNS.
-2 different types of receptors:
Muscarinic (G-protein linked at the terminal synapses of all parasympatheric postganglionic fibers and few sympathetic postganglionic fibers, autonomic ganglia, and in the CNS
Nicotinic: ligand gated ion channels that are concentrated postsynaptically at many excitatory synapses
sends messages toward the brain (CNS) or spinal cord; they are SENSORY NEURONS
motor neurons; send message from the CNS or spinal cord to an effector
molecule that binds to a receptor and stabilizes the receptor in a particular conformation (usually the active conformation)
molecule that inhibits the action of an agonist but has no effect in the absence of the agonist
electrophilic molecules attacked by nucelophilic sites of DNA resulting in the covalent linkage of an alkyl group
- affect cell function in all phases and are therefore cell-cycle nonspecific. Alpha- and beta-adrenoreceptors -cyclophosphamide, mechlorethamine, melphalan, chlorambucil, thiotepa
A life-threatening hypersensitivity reaction caused by systemic mast cell degranulation after exposure to an allergen in a previously sensitized individual
CYTOTOXIC AGENT; chemical that inhibits the use of a metabolite, which is another chemical that is part of normal metabolism.
-Such substances are often similar in structure to the metabolite that they interfere with. The presence of antimetabolites can have toxic effects on cells, such as halting cell growth and cell division, so these compounds are used as chemotherapy for cancer.
inhibit clotting cascade
decrease platelet aggregation and inhibit thrombus formation
host system attacks its own tissue mistaking self antigen for foreign; typically results in inflammation
receptors on presynaptic membrane that regulate neurotransmitter release
The amount of the drug available to the target organ; aka fraction absorbed.
functions in sympathetic neuron transmission; all derived from tyrosine
- Includes dopamine, norepinephrine, and epinephrine.
-Most synthesis occurs at the synaptic nerve ending
-removed from the synaptic cleft by re-uptake, enzymatic breakdown into metabolites or by diffusion from the synaptic cleft. These neurotransmitters modulate many vital para/sympathetic functions, and many drugs target the synthesis, storage, release, and reuptake of these neurotransmitters and their post-synaptic receptors.
ligand that forms two or more separate bindings between a polydentate (multiple bonded) ligand and a single central atom
agents that target cell growth and division; cell cycle specific and non cell cycle specific
- Almost all chemotherapeutic drugs also cause apoptosis of cancer cells
combination antineoplastic therapy
use of antineoplastic drugs that both work during particular cell cycle point and that work throughout cell cycle
-Drugs in a multidrug regimen can interact synergistically to enhance the antineoplastic therapy and can decrease likelihood that resistance will emerge.
competitive (reversible) antagonist
binds reversibly to the active site of a receptor
Noncompetitive (irreversible) active site antagonist
can either bind to the active or allosteric site; if it binds to the ACTIVE site it does so with HIGH AFFINITY OR COVALENTLY SO THAT it's in affect IRREVERSIBLE
response to drug is proportional to the concentration of receptors that are bound by the drug
GRADED DOSE-RESPONSE relationships: effect of dose of drug on an individual. Can get potency (EC50) (concentration at which drug elicits 50% of maximal response) and efficacy (Emax)(max response produced by the drug.
QUANTAL DOSE-RESPONSE relationships: effect of dose of drug on a population. observed for presence or absence of a response. can get effectiveness (ED50), toxicity (TD50) and lethality (LD50)
down-regulation of receptor
prolonged receptor stimulation by ligand induces the cell to endocytose and sequester receptors in endocytic vesicles; CELLULAR DESENSITIZATION
-RATE OF ELIMINATION of the drug from the body relative to the concentration of the drug in plasma OR
- RATE AT WHICH the plasma would have to be cleared of the drug to account for the observed kinetics of change of the total amount of drug in the body assuming that all the drug in the body is present at the same concentration as that in the plasma
= metabolism+excretion/ [drug] in the plasma
-metabolism and excretion are expressed as rates (amt/time)
clearance= Crenal + Chepatic + Cother
interactions between drugs that affect their actions
drug metabolism or biotransformation
biochemical changes in drugs
2 types: ox/red AND conjugation/hydrolysis
amount of time over which the drug concentration in the plasma decreases to ½ of its original value
T1/2= 0.693(Vd)/ clearance
-Vd=volume of distribution
enteral administration of drugs
by mouth; first pass metabolism in the liver; liver enzymes may inactivate part of the drugs
parenteral administration of drug
directly across barrier into systemic circulation; parenteral can into vascularized tissue, blood, or Cerebrospinal fluid; NOT FIRST PASS; fast
Increase in the expression of the enzyme through increased transcription, increased translation, or decreased degradation. induction and inhibition can be incidental (a side effect of the drug) or deliberate (the desired effect of therapy).
can occur through competitive inhibition, or mixed, or through irreversible inhibition in which a drug or metabolite binds to the enzyme either at the active site or another site to allow for a conformation change. ** An important consequence of enzyme inhibition is the decreased metabolism of drugs that are metabolized by the inhibited enzyme.
first order kinetics
the amount of drug that is metabolized/excreted in a given unit of time is directly proportional to concentration of drug in systemic circulation
zero order kinetics
clearance rate remains the same despite increasing plasma drug levels; occurs at or near the therapeutic concentration of the drug; once saturation occurs the clearance level stays the same
drugs are carried by the portal system to the liver before entering the systemic circulation; serves to protect by detoxifying but can end up inactivating part of the drug intaken
exaggerated response at high levels of stimuli—upward shift in stimulus-response curve
abnormal response to low levels of stimuli—stimulus-response curve shifts LEFT
Suppression of the body's immune system and its ability to fight infections and other diseases.
- may be deliberately induced with drugs, as in preparation for bone marrow or other organ transplantation, to prevent rejection of the donor tissue. It may also result from certain diseases such as AIDS or lymphoma or from anticancer drugs
are transmembrane ion channels, which facilitate fast signal transduction (ligand-gated ion channels)
membrane-bound receptors, which facilitate slow signal transduction through the activation of second messengers (G protein-coupled receptors)
dose first administered taking into account the tissue volume in addition to the plasma volume to reach a therapeutic level
once the steady state plasma level is achieved and equilibrium between drug concentration in tissues and plasma subsequent doses need to replace only the drug lost through metabolism
median effective dose (ED50)
dose of drug that is therapeutically effective in 50% of the population
median lethal dose (LD50)
dose at which 50% subjects die
multiple drug resistance (MDR) receptors
transporters that transport hydrophobic compounds out of the brain and back into the blood vessel lumen; in many cell types and play impt role in processes such as resistance of tumor cells to chemotherapeutic agents
muscarinic vs. nicotinic receptors
muscarinic vs. nicotinic cholinergic receptors (not adrenergic)
***all receptors on postsynaptic membranes in SYMP and PARASYMP are NICOTINIC
end organs of PARA have muscarinic
**sweat glands of SYMP have muscarinic
molecule that binds to a receptor at its active site but produces only a PARTIAL response, even when all of the receptors are occupied (bound) by the agonist. A partial agonist can reduce the response produced by a full agonist, and in this way acts as a competitive antagonist
phenomenon that occurs due to the acid dissociation constants of drugs and the pH gradient across the membrane; like basic blood and acidic stomach forces aspirin into blood!
most important mechanisms of tolerance; results from change in drug-receptor interaction
-change in the number of receptors or the signal transduction path
develops when the ability to metabolize or excrete the drug increases over time
refers to the adverse physical symptoms and sign that result from the withdrawal of a drug
more complex phenomenon that can occur even with drugs that do not produce tolerance and physical dependence; occurs when a drug affects the reward system of the brain; when the drug is withheld adaptations in the brain reward system manifest as dysphoria and drug craving
concentration at which the drug elicits 50% of the maximal response
the maximal response produced by the drug
an inactive compound that is metabolized by the body into its active form
selective vs. nonselective agonist
selective binds selectively. nonselective binds to whatever it wants.
selective vs. nonselective antagonist
?selective binds selectively. nonselective binds to whatever it wants.
occurs when maximal effect of drug is achieved when not all the receptors are bound by ligand
steady-state drug concentration
= (fraction absorbed x maintenance dose)/ (dosing interval x clearance)
drugs that mimic the effects of the sympathetic nervous system such as catecholamines, epinep, norep, dopamine
drug is a medication, which inhibits the postganglionic functioning of the sympathetic nervous system
-they can all be used as antihypertensives.
rapidly decreasing response to a drug or physiologically active agent after administration of a few doses
TD50/ED50; toxic response in 50% over the effective dose in 50%
used to lyse already formed clots and thereby restore the patency of an obstructed vessel before distal necrosis occurs
foreign substances that are not naturally found in the body
alpha and beta adenoreceptors
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