Pharm Section 2 Flashcards
components/function of central nervous system
brain + spinal cord; interprets incoming sensory info, dictates motor response (integration, command center)
components/function of peripheral nervous system
spinal nerves (impulses to/from spinal cord); cranial nerves (impulses to/from brain); sensory/afferent (impulses from sensory receptors to CNS); motor/efferent (impulses from CNS to effector organs); somatic afferent (impulses from skin, skeletal muscle, joints); visceral afferent (impulses from visceral organs)
voluntary/somatic nervous system
impulses from CNS to skeletal muscle
involuntary/autonomic nervous system
impulses that regular activity of smooth muscles, cardiac muscles, and glads (“automatic”). consists of sympathetic (fight/flight) and parasympathetic (rest/digest)
ganglion and parasympathetic post-ganglionic fibers release…
acetylcholine
sympathetic post-ganglionic fibers release…
catecholamines (norepinephrine and epinephrine)
the release of catecholamines produces a _________ response
fight or flight
what enzyme inhibits the action of acetylcholine?
acetylcholinesterase
what enzymes inhibit the action of catecholamines?
monoamine oxidase (MAO) and catechol-o-methyl transferase (COMT)
What types of receptors are present in the sympathetic/adrenergic system?
alpha 1, dopaminergic, beta 1, beta 2
alpha 1 receptors (location/stimulation)
located in vascular smooth muscle; stimulation causes vasoconstriction
dopaminergic receptors (location/stimulation)
located in renal and coronary vessels; stimulation causes vasoconstriction
beta 1 receptors (location/stimulation)
located in heart; stimulation causes tremors, tachycardia
beta 2 receptors (location/stimulation)
located in lungs; stimulation causes tremors, bronchodilation
“you have one heart and two lungs” explain.
beta 1 receptors located at heart; beta 2 receptors located at lungs
What type of receptors are present in the parasympathetic/cholinergic system?
muscarinic and nicotinic
muscarinic receptors
end-receptor stimulated by the release of acetylcholine from post-ganglionic fibers in the parasympathetic nervous system. subclasses M1 (CNS), M2 (heart), M3 (smooth muscle), M4 (CNS), and M5 (CNS).
nicotinic receptors
end-receptor stimulated by the release of acetylcholine from post-ganglionic fibers in the parasympathetic nervous system. subclasses N1 (neuromuscular junction) and N2 (autonomic ganglia, CNS, adrenal medulla)
adrenergic refers to…
sympathetic nervous system (adrenaline–adrenergic. Think catecholamines.)
cholinergic refers to…
parasympathetic nervous system (think acetylCHOLINE–cholinergic.)
steps in enzymatic synthesis of catecholamines
tyrosine > dopa > dopamine > norepinephrine > epinephrine
types of sympathomimetic (adrenergic) drugs
alpha stimulants/agonists (aka alphamimetics), beta stimulants/agonists (aka betamimetics), and mixed alpha and beta stimulants/agonists
alpha 1 agonists
phenylephrine (Neo-Synephine) and norepinephrine (Levophed). potent vasoconstrictors.
what are alpha 1 agonists used for?
vasoconstrictors (hypotensive shock), treat priapism, nasal decongestant (constrict vessels @ nasal mucosa, decrease swelling, increase nasal patency)
which route of administration would you NEVER use to administer alpha 1 agonists?
Intramuscular
what do you use to reverse the effects of alpha 1 agonists?
alpha blocker phentolamine (Regitine)
beta agonists + mechanism of action
some are “preferential” or “selective” or beta 1 or 2, but none are 100% selective, so will always get some stimulation @ both. mechanism of action: activate adenyl cyclase and increase intracellular concentrations of cAMP
what are beta agonists used for?
bronchodilation for asthma/COPD, cardiac stimulant, tocolytic effect (uterine relaxation),
dobutamine and dopamine are what type of beta agonists?
beta 1 agonists (heart)
terbutaline, albuterol, levabuterol, salmeterol, formoterol, arformoterol, clenbuterol are what type of agonists?
beta 2 agonists (lungs)
mixed alpha and beta agonists
includes epinephrine (Adrenalin, Epi-pen, AuviQ), ephedrine, pseudoephedrine (Sudafed)
what are mixed alpha and beta agonists used for?
allergic reactions/anaphylaxis, nasal and sinus decongestants, bronchodilation, and cadriogenic shock and bradycardia
side effects of adrenergic/sympathomimetic drugs?
increased BP, vasoconstriction, increased HR, stroke, mydriasis (dilated pupils), cardiac arrhythmias, increased BGC (hyperglycemia), intracellular movement of K+ (hypokalemia), urinary retention (males with enlarged prostate), and uterine relaxation (tocolytic effect–B2)
sympatholytic/antiadrenergic drugs
include alpha and beta blockers
alpha blockers
include phentolamine (Regitine, OraVerse) and phenoxybenzamine (Dibenzyline)
what are alpha blockers used for?
diagnosis and pre-op mgmt of pheochromocytoma (adrenal gland tumor) and to reverse the vasoconstrictive effects of alpha agonists.
how can you reverse severe vasoconstriction?
give alpha blockers
beta blockers
some of the most widely-used drugs. usually end in -olol/-alol/-ilol, esp -olol. Selective and non-selective, but selective only so for beta 1. don’t want to block beta 2 because it would stop breathing.
contraindications or precautions for using beta blockers
diabetes, asthma, COPD, peripheral vascular disease,
why would you want to use a selective beta blocker?
if you have asthma, COPD pts where you want to limit the action of the blocker @ lungs. Will still get some stimulation, but less than if use a non-selective beta blocker
benefit of using beta blockers with ISA (intrinsic sympathomimetic activity) or PAA (partial agonist activity)?
fewer side effects, esp decrease in heart rate at rest. preferred for clients who develop bradycardia with other beta blockers
when should you NOT use beta blockers with ISA?
for patients with angina pectoris, as cardiac protection during surgery, or after MI (b/c low O2 levels)
what are beta blockers used for?
cardiac arrythmias, angina pectoris, hypertension, migraine headache prophylaxis, actue anxiety reactions, prevent recurrent MIs, glaucoma (topical), chronic CHF, pre/post-op (non cardiac surgeries)
side effects of beta blockers
hypoglycemia/masks signs of hypoglycemia, bradycardia, fatigue, prevents bronchiole dilation, don’t stop abruptly or “super reactive” to sympathetic stimulation, caution with peripheral vascular disease
parasympathomimetic (cholinergic) agonists
direct-acting drugs that stimulate cholinergic receptors like acetylcholine. includes pilocarpine, mathacholine, cevimeline, and bethanechol
pilocarpine
cholinergic agonist. direct acting. eye drops for glaucoma and for dry mouth
methacholine (Provocholine)
cholinergic agonist. direct acting. inhaled for tx of bronchial airway hyperactivity
cevimeline (Evoxac)
cholinergic agonist. direct acting. dry mouth tx for pts with Sjogren’s syndrome (dry mouth, eyes, mucosa)
bethanechol (Urecholine, Duvoid)
cholinergic agonist. direct acting. tx for urinary retention.
acetylcholinesterase inhibitors
indirect acting cholinergic drugs. inhibits enzyme acetylcholinesterase, which increases body’s natural ACh activity. Includes drugs to treat alzheimer’s, myasthenia graves, etc.
tacrine (Cognex), donepezil (Aricept), rivastigmine (Exelon), and galantamine (Razadyne) are used to treat what?
Alzheimer’s disease. indirect acting cholinergic drugs (aka acetylcholinesterase inhibitors).
Neostigmine (Prostigmin) and Pyridostigmine (Mestinon) are used to treat what?
myasthenia gravis (muscle weakness, face droop that moves down body). indirect actin cholinergic drugs (aka acetylcholinesterase inhibitors)
organophosphates are used as what?
insecticides. poisonous to humans because they are acetylcholinesterase inhibitors. atropine is antidotal. (Scene from “The rock” where nick cage is exposed and uses atropine injection to heart to save himself)
what are cholinergic agents used for?
neurological diseases (Alzheimer’s, myasthenia gravis), glaucoma, dry mouth, stimulate GIT and GUT (tx urinary prevention)
side effects of cholinergic agents?
abdominal cramping, diarrhea, increased secretions, DUMBBELSS mnemonic (diarrhea, urination, mitosis–pupil constriction, bradycardia, bronchoconstriction, emesis, lacrimation, salivation, sweating)
parasympatholytics (anticholinergic/antimuscarinic)
derived from natural sources like the belladonna plant or manufactured synthetically. tertiary amines absorbed @ CNS
belladonna alkaloids
atropine (classic anticholinergic drug), scopolamine, and hyoscyamine
what are anticholinergic drugs used for?
decrease glandular secretions, pupil dilation (either mydriasis–dilation or cycloplegia–paralysis of focusing mechanism @ eye), treatment of Parkinsonism, stimulate heart for bradyarrythmias (atropine), stimulate bronchodilation (asthma, COPD), illicit central effect @ CNS to produce anti-nausea effect and somnolence (sleepiness) and “twilight sleep”, to decrease GIT/GUT actions (tx for diarrhea, enuresis–involuntary urination, IBS, and OAB), to treat hyperhidrosis (excessive sweating), and to block skeletal muscles for intubation prior to surgery.
side effects of anticholinergic drugs
classic adverse reactions: dry mouth, blurred vision (cycloplegia), urinary retention, constipation, increased temp (flushing), tachycardia (heart palpitations), central effects including confusion, amnesia, hallucinations.
anticholinergic drugs and elderly
strong evidence that they are associated with brain atrophy in elderly patients…increase risk for dementia.
two main types of incontinence
stress and urge incontinence
symptoms of stress incontinence
involuntary loss of urine, associated with sneezing/coughing/laughing/lifting
symptoms of urge incontinence
involuntary urine loss preceded by strong desire to empty bladder
causes of stress vs. urge incontinence
stress: inefficient urethral closure
urge: uncontrolled bladder contractions