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what the body does to the drug
pharmacokinetics (absorption, distribution,elimination)
what the drug does to the body
pharmacodynamics (local, systemic, cellular effects and mechanims)
what is the name of the federal agency that governs the safety and efficacy of drugs in the US?
what is the name of the federal agency that enforces the Controlled Substances Act and what does this act say?
Drug Enforcement Agency (DEA) divides drugs into schedules depending on their abuse potential
What does maximal efficacy lead to?
does a potent drug have a higher or lower dose response curve?
lower- and is usually more left on a dose response curve
what does the median effective dose mean?
ED50- the dose at which 50% of the population responds in a desired manner
what does median toxic dose mean?
TD50- the dose at which 50% of the population responds in an undesired manner
what does the therapeutic index mean? and with regards to a higher/lower number?
TI- is the ratio of MD50 to TD50
a higher TI means drug is safer
what does enteral mean?
oral, sublingual, buccal, rectal
what does parental mean?
non-ailmentary administration, no first pass effect
inhalation, injection, IV, intra-arterial, subcutaneous, IM, intrathecal, topical, transdermal
what are the primary sites for metabolism, storage and excretion
how many half lives does it take for the concentration of a medication in in the system to leave the body or reach the steady state
5 half life units
if a drug has a half life of 24 hours how many days does it take to be removed from the body?
how about a half life of 12 hours?
24 hours....takes 5 days
12 hours...takes 2.5 days
a component of the cell where a drug binds and initiates a chain of biochemical events
a drug that can bind to a receptor and initiate change in the fxn of the cell (has both affinity and efficacy)
(has only affinity) meaning the drug will bind to a receptor but it will not cause any direct change in the fxn of the receptor or cell
used to describe the amount of attraction between a drug and receptor
what are the 3 things that can affect affinity
1-acts as an ion channel and directly altering membrane permeability
2-by acting enzymatically to directly influence fxn w/in the cell
3-being linked to regulatory proteins that control other chemical and enzymatic processes w/in the cell
they hunt for the same receptor as the agonist-both agonist and antagonist have an equal opport to occupy the receptor
these form strong, essentially permanent, bonds to the receptor
what are the 3 cell surface receptors and their relative speed or response after activation
1-ion channel (linked directly to surface receptors-fastest)
2-kinase linked-2nd fastest
3-G proteins-takes a substance outside of the cell to couple with the G protein inside to bind to the receptor
G proteins are activated by?
what are the 2 possible locations of intracellular receptor and examples of each
1-cytoplasm (steriods bind here than to nucleus)
2-nucleus (thryoid receptors bind directly)
functions of basal ganglia, reticular formation, and limbic system.
basal ganglia-motor functions
limbic system-mood and emotions
drugs that affect basal ganglia, reticular formation, limbic system
basal ganglia- Ach, dopamine, GABA
reticular formation- NE
limbic system-Ach, dopamine
what is the blood brain barrier?
selective filter and protects CNS by limiting harmful substances that enter into the brain and spinal cord
what type of drug is allowed across the BBB? and how is it passed through? what is more likely to pass thru...1st or 2nd generation antihistamines?
nonpolar-lipid soluble drugs
passed thru passive diffusion
1st generation more likely since 2nd generation is more lipidy
what CNS receptor is affected most by anti-anxiety and sedative hypnotic agents?
used to both relax the pt and to promote sleep (higher doses-hypnosis or even general anesthetic
what are the general classes of sedative hypnotic drugs?
benzos, barbituates, other nonbenzos, alcohol
are benzos or barbituates used more for treating sedative hypnotic conditions?
tricyclic antidepressant agents (block/unblock) the reuptake of amine NTs (what are these NT's) in the brain
dopamine, NE, serotonin
MAOIs (block/unblock) enzymes that break down amine NTs
(1st/2nd) generation antidepressants are more selective for blocking serotonin or NE reuptake and have less SEs
if dietary restriction of MAOIs are not followed what happens?
lead to excessive catecholamine levels and hypertensive crisis
what are anticholinergic symptoms?
dry mouth, constipation, urinary retention, tachycardia
"can't see, can't pee, can't sh*t, can't spit"
what other condition can tricyclic antidepressants help with?
condition characterized by disturbed thought processes (delusions/hallucinations) and that the positive or agitative symptoms of psychosis are thought to be primarily due to an overactivity of dopamine in the limbic system-negative symptoms may be attibutable to decrease dopamine in higher areas of the brain
what do antipsychotic medications block?
dopamine receptors especially D2
do antipsychotic meds have motor and nonmotor side effects?
tardive dyskinesia symptoms are hardest to alleviate and last to show up. T/F
antiseizure meds: generally ______(inhibit/excite) the firing of cerebral neurons usually by _____(increasing/decreasing) inhibitory effects of GABA by ______(increasing/decreasing) the effects of excitatory amino acids
SEs of antiseizure meds
sedation, ataxia, nystagmus, GI distress, dizziness
______% of people can remain seizure fress after their medication is withdrawn
3 main criteria for patients who would be good candidates for slow withdrawal
1-free of seizures for 2 years
2-normal neuro exam
3-young when seizures started
best way to treat a pt who is seizing?
treat emergency, stabilize, restart chronic maintenence therapy
what type of environment would be ideal for a pt prone to seizures?
calm, stress-free environment without much sensory stim
know general NT of PD, area affected and general symptoms
substantia nigra in basal ganglia
how does levidopa work? what enzyme does it metabolize? why is it used with carbidopa?
resolves dopamine deficiency by being converted to dopamine after crossing BBB
converted to dopamine by dopa decarboxylase
carbidopa and levidopa in combo decreases peripheral decarboxylation which decreases amount for levidopa
facial grimicing, lip twitching, tongue protrusion, strange leg movements describe what?
peripheral SE of levidopa
- -GI problems
- -cardiac arrhythmias
central SE of levidopa
effectiveness may suddenly decrease resulting in the abrupt worsening of parkinsonian symptoms =?
remission of symptoms may then generally occur spontaneously or after taking a dose of levidopa
ideal characteristics of general anesthetic (6)
- 1-loss of consciousness/sensation
- 3-skeletal mm relaxation
- 4-inhib of sensory and autonomic reflexes
- 5-minimum of toxic SE
- 6-rapid onset of anesthesia
general anesthetic is given by inhalation or injection. T/F
where are inhalation effects generally stored?
fat and excreted thru the lungs
can a neuromuscular blocker cause anesthesia on its own?
applied directly to the surface of the skin, mucous membranes, cornea or other regions of the body. used for minor abrasions, inflammation, and minor burns, reduces pain prior to minor surgical procedures and used to improve motor function in patients with hypertonicity
used to anesthetize a region of skin before treating painful subcutaneous structures w/o breaking the skin. used in dermatological procedures and to treat localized pain in musculoskeletal conditions and neuropathic pain
injected into a nerve trunk so that transmission along the peripheral nerve is interrupted. used for dental procedures to block other peripheral nerve to allow certain surgical procedures of the hand, foot, shoulder, etc it can be continued after the completion of surgery to provide pain management
peripheral nerve block
injected w/in the spaces surrounding the spinal cord. used when analgesia is needed in a large region, and epidural and spinal routes are used frequently to administer local anesthetics during obstretic procedures
central nerve block
useful in cases of complex regional pain syndrome, RSD and causalgia
(bier block) used to anesthetize the forearm, hand or distal leg, ankle or foot for short periods to allow certain surgeries or to treat conditions such as CRPS
intravenous regional anesthesia
how do local anesthetics work?
block AP propagation along axons, occurs from anesthetic molecule inhibiting the opening of membrane Na channels
ability of a given local anesthetic dose to block specific nerve fiber groups depending on the size of the fibers
differential nerve block
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