T2: ANS, Histamine Flashcards
(205 cards)
1
Q
bactericidal drugs
A
penicillinscephalosporinsaminoglycosidesvancomycinaztreonamimipenemfluroroquinolonesmetronidazolepolymyxinsquinupristin-dalfopristinbacitracin
2
Q
bacteriostatic drugs
A
erythromycin (macrolides)clindamycintetracyclinechloramphenicolsulfonamidestrimethoprimnitrofurantoin
3
Q
narrow spectrum
A
only G+ or G-: isoniazid against mycobacterium
4
Q
extended spectrum
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G+, some G- i.e. ampicillin
5
Q
broad spec
A
wide variety of G+ and G-: tetracycline, chloramphenicol, imipenem
6
Q
expense of drug administration
A
IV>IM>oral (cheapest)
7
Q
drugs that inhibit synthesis of bacterial cell walls: PCN (B-lactam): natural penicillins
A
G, V Potassium, G Procaine, G Benzathine, G Benzathine + Penicillin G Procaine
8
Q
drugs that inhibit synthesis of bacterial cell walls: PCN (B-lactam): Penicillinase resistant Penicillins (anti-staph)
A
methicillinnafcillinoxacillin
9
Q
drugs that inhibit synthesis of bacterial cell walls: PCN (B-lactam): ext. spec PNC
A
ampicillinamoxicillin
10
Q
drugs that inhibit synthesis of bacterial cell walls: PCN (B-lactam): antipseudomonal
A
Ticarcillin + clavulanate potassium (Timentin)Piperacillin + Tazobactam (Zosyn)
11
Q
drugs that inhibit synthesis of bacterial cell walls: PCN (B-lactam): monobactams
A
aztreonam
12
Q
drugs that inhibit synthesis of bacterial cell walls: PCN (B-lactam): carbapenems
A
Imipenem + Cilastatin
13
Q
drugs that inhibit synthesis of bacterial cell walls: PCN (B-lactam): B-lactamase inhibitors
A
Clavulanic acid, Tazobactam
14
Q
drugs that inhibit synthesis of bacterial cell walls: cephalosporin (B-lactam): 1st gen
A
CefazolinCephalexin
15
Q
drugs that inhibit synthesis of bacterial cell walls: cephalosporin (B-lactam): 2nd gen
A
CefaclorCefoxitinCefuroximeCefprozil
16
Q
drugs that inhibit synthesis of bacterial cell walls: cephalosporin (B-lactam): 3rd gen
A
CeftriaxoneCefiximeCefotaximeCeftazidime
17
Q
drugs that inhibit synthesis of bacterial cell walls: cephalosporin (B-lactam): 4th gen
A
Cefepime
18
Q
drugs that inhibit synthesis of bacterial cell walls: cephalosporin (B-lactam): 5th gen
A
Ceftaroline
19
Q
other drugs that inhibit bacterial cell wall synthesis
A
vancomycinbacitracin
20
Q
drugs that alter cell membrane permeability
A
Polymyxin BDaptomycin
21
Q
drugs that inhibit bacterial protein synthesis: Tetracyclines
A
short-acting: Tetracycline long-acting: Doxycycline, Minocyclinenew: Tigecycline
22
Q
drugs that inhibit bacterial protein synthesis: Macrolides
A
Erythromycin base” Estolate, “ Stearate, “ Ethylsuccinate, “ LactobionateClarithromycinAzithromycinTelithromycin
23
Q
drugs that inhibit bacterial protein synthesis: Aminoglycosides
A
Gentamicin; generic: Garamycin, JenamicinTobramycin; generic: NebcinAmikacin; generic: AmikinStreptomycinNeomycin
24
Q
drugs that inhibit bacterial protein synthesis: Misc.
A
ClindamycinQuinupristin/DalfopristinLinezolid
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act on 50S ribosomal subunit
Cloramphenicol, macrolides, clindamycin, quinupristin/dalfopristin, linezolid
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act on 30S ribosomal subunit
Aminoglycosides, Tetracyclines
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drugs that act as anti-metabolites: Sulfonamindes
Silver Sulfadiazine (SILVADINE): topicalTrimethoprim-sulfamethoxazole
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drugs that inhibit nucleic acid synthesis: Fluoroquinolones
Ciprofloxacin (CIPRO)Levofloxacin (LEVAQUIN)Moxifloxacin (AVELOX)
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Misc. drugs that act via nucleic acids
MetronidazoleNitrofurantoinRifampin
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empirical therapy
"best guess" therapy, br. spec/combo abxguided by Gs, site of inf, clinical experience, local hospital antibiogram susc. reports-should be changed to rational therapy (narrow spec) when susc. tests performed and org. ID'd
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epsilometer (E) test:
also determines MIC, plastic strip containing gradient of known conc. abc placed on agar plate containing pt's bac. isolate
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how to monitor antimicrobial activity in vivo
serum inhibitory titer: greatest dilution of pt's serum that inhibits visible growth of pt's infecting pathogenbactericidal titer: plate out above no-growth samples onto abx-free plates
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min. drug conc. at infected site should be..
>= MIC, ideally 2-4x MIC(abscesses must be drained)
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BBB may prevent..
penetration of drug into CSF-but during infection BBB is diminished (opened up tight junctions of cerebral capillaries)-->inc. penetration
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this may prevent abx penetration to site of action (and dec. levels of free drug)
abx binding to plasma proteins
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med doses may need to be adjusted for..
renal/hepatic failurenewbornsoral vs. parenteral admin
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bactericidal or bacteriostatic?
cidal is better, esp. if immunecomp
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strains of these are resistant to all known drugs
EnterococciPseudomonasEnterobacter
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bacterial resistance factors
indiscrim. use (misuse)delay in optimal txadmin of subopt. dosetx during dormant stageinability to reach inf. site (CNS, eye, prostate, abscess) defective funct. status of host defense mech agricult. used of abx in livestock
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how microorganisms produce resistance
mutation and selection i.e. resistance to:-strep (ribosomal mut.)-quinolone (DNA gyrase)-linezolid (rRNA)-rifampin (RNA polymerase)-M. tuberculosis
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resistance mediated by genetic exchange
HGT: transformation (PCN res. in pneumo.)transduction (Staph, penicillinase)conjugation
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conjugation
2 sets of genes transferred: R-determinant (resistance) and resistance transfer factor (RTF)-->ind or combine to for R-factor*can have >1 abx resis. gene!**>50% ppl have int. bac containing R-factors
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transposon
DNA sequences that can "jump from place to place", can carry drug resis. genesplasmid-->plasmidplasmid-->chromosome (and vis versa)
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biochem mechs of drug resistance
1. dec. perm. of org to drug: porins do not allow in anymore (G-) OR active efflux (tetras)2. inactivation of abx by enzymes: (PCN, Chloramphenicol, Aminoglycosides): B-lactamases (+ and -) acetyl/phosphoryl/adenylate drug (amino glycosides, G-)3. altered drug target site: PBP w/ altered affinity for drug, mut. in FQ target (DNA gyrase)
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forms of synergism seen with combo abx tx
-block of seq. steps in metabolic pathway (Trimethoprim + Sulfamethosazole-->folic acid)-inhib. enz. inact. of abx (B-lactamase inhibitor)-enhanced abx uptake by bac (aminoglycoside + B-lactam)
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synergism
4x or greater reduction in MIC or MBC when drug combined
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antagonism
>50% MIC of each drug needed to produce inhibition of growth
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antagonism exs.
bacteriostatic antags. bactericidal (need actively growing org) (PCN + chlortetracycline)induction of enz. inact.: imipenem (induces B-lactamase) + piperacillin (susc. to B-lactamase)
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combo abx tx uses
mixed bac infunknown specific cause-empirical tx (i.e. pneumonia: macrolides for M. pneumo + ceftriaxone for G-)synergism may be nec. to kill org. (PCN + AMGS better tx for enterococcal endocarditis)may prevent resistances (bismuth salts + amos/tetra/or clarithro + metronidazole for H. pylori)
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disadv. of combo abx tx
inc. toxic side effectsselection of orgs resis. to >1 abxpossible antag. effect if wrong combo
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abx ppx
-post-exposure to certain microorgs: gon, syph, anthrax-prevent recurrent dis. in susc. pt: artific. heart valve undergoing dental proc. to prevent bac endocarditis, emphysema pts to prevent chron. bronchitis, frequent UTIs-surgical procedures: 0-2 hrs before, during, 3-4 hrs after-trauma contam wounds
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abx ppx approved surgical procedures
contam, clean-contam operations, dirty wounds, prosthetic placement, immune comp host (any proc)
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superinfections
new infection appears during chemotx for other infection
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why do superinfections occur?
doses of abx can inhibit NF growth-->other orgs uninhibited
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superinfection orgs
enterobacteriaceae, pseudomonas, candida, fungi
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inc. risk of superinfection w/
brd spec abx, longer course, oral admin over IM/IV
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abx misuse
-for viral infection (fever 2 wks which could be tb, intra-abd. abscess, inf. endocarditis, Ca-undetermined cause (NOT antipyretics)-improp. dosage -abx has to reach inf. site (get rid of pus and kidney stones)-lack of adeq. bac info: more testing!-improp. duration of tx (finish your abxs!)
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receptors at parasympathetic end organs (and symp. sweat glands)
muscarinic: M1-5, 2,3*most common
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B1 adrenergic receptor
heart (inc. force, rate)kidney (mediate renin secr) brain
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B2 adrenergic receptor
airway, BVs of skel music, pregnant uterus-smooth musc relaxation
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B3 adrenergic receptor
bladder smooth musc: relaxation
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a1 adrenergic receptor
most BVs, urinary sphincters, eye-mediate contraction of smooth musc
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a2 adrenergic receptor
some end organs, @ adrenergic nerve endings and in CNS
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organs that received both parasym and symp innervation
heart, GI, bladder, eye, etc
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organs w/ only symp innervation
adrenal medulla, spleen capsule, pilomotor musc, BVs of skin and skeletal muscd
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reserpine blocks adrenergic system..
produces exaggerated cholinergic response: inc. GI motility, secretions
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atropine blocks cardiac vagal influence..
cardiac acceleration, reduction of GI motility, secretion
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eye sympathetics
a1: mydriasis (dilator musc. of iris) B2: inc. aqueous humor
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gland sympathetics
a, BB2: respiratory secretions
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heart sympathetics
B1, B2:inc. rate (SA node), contractility (ventricles), automaticity, conduction velocity (SA, AV nodes)
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BVs sympathetics (mucosa, saliva, skin, splanchnic)
a1, a2: constriction
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BVs sympathetics (skeletal musc)
a1: constrictionB2: dilation
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BVs parasyms
no PS inn to most vasc beds, but muscarinic rec are present on endo cells: activation of these receptors: NO-med. vasodilation
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airway symps
relaxation: B2
75
GI symps
relaxation: a1, a2, B1, B2 dec. motility
76
Urinary bladder wall, sphincter, prostate sympathetics
relaxation: B2, B3 (widens out)contraction: a1 (sphinter)
77
kidney JG cell symp
inc. renin secretion: B1
78
uterus symp
contraction: a1relaxation: B2 (later on)
79
male sex organs symp
ejaculation: a1
80
male sex organs PS
erection
81
liver, fat cells symp
inc. glucose output: B2inc. FA output: B1
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skin pilomotor music and sweat glands symps
contraction: a1secretion: muscarinic
83
eye PS
miosis (pupillary sphincter musc) accommodation- near vision (ciliary musc.)
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PS ciliary musc contraction also...
inc. pressure on trabecular meshwork-->inc. outflow of AH in canal of Schlemm and dec. intraocular pressure
85
PS action on lacrimal gland
inc. tear production
86
acetylcholine is formed by action of
choline acetyl transferse (choline + acetate)
87
ACh pathway
stored in vesicles-->AP-->inc. IC [CA2+]-->storage vesicle fuses with plasma mem-->ACh rel. into synapse-->acts on postmen. rec-->activates transduction pathway-->response
88
nicotinic rec. usually coupled to
Na+ channels
89
muscarinic rec may be coupled to
phospholipase C, K+ channelsor act thru G-protein mechanism to inhibit adenylate cyclase
90
actions of ACh terminated by
acetycholinesterase (rapid hydrolysis) choline and acetate recycle to ACh by presyn. nerve ending
91
specific sites where drugs can modify cholinergic system
#NAME?
92
tyrosine-->DOPA-->DA-->NE
1. tyrosine hydroxylase* 2. DOPA decarboxylase 3. Dopamine B-hydroxylase
93
NE acts on postsyn. rec
a1 or B1-->signal transduction pathway-->response
94
Noradrenergic signal transduction pathway
typ. involve G-prot. coupled rec. B-rec: coupled to adenylate cyclasea-rec: coupled to pholspholipases or ion channels
95
NE can also act on
a2 rec on presynaptic nerve ending: feedback inhibition on NE release
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action of NE terminated mostly by
rapid reuptake into presyn. nerve ending, med. by high affinity transport pump-->broken down by MAO or requestered in storage vesicles
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sites of pharm intervention on Noradrenergic system
#NAME?
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direct acting muscarinic agonists
acetycholine (Miochol-E)carbachol (Isopto Carbachol)methacholine (Provocholine)bethanechol (Urecholine)pilocarpine (Salagen/Ocusert Pilo)cevimeline (Evoxac)
99
indirect acting drugs: cholinesterase inhibitors -reversible
edrophonium (Tensilon)physostigmine/eserineneostigmine (Prostigmin)pyridostigmine (Mestinon)rivastigmine (Exelon)donepezil (Aricept)carbamate insecticides (Carbaryl)
100
indirect acting drugs: cholinesterase inhibitors-irreversible
DFP/diisopropylfurophosphate/isoflurophate and echothiophateorganophasphate insecticides (Parathion, Malathion)nerve gases in chem warfare (Sarin, soman, Tabun, Vx)
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indirect acting drugs: cGMP phosphodiesterase (PDE-5) inhibitors
sildenafil (Viagra)vardenafil (Levitra)tadalafil (Cialis)
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Cholinesterase Reactivator
pralidoxime/2-PAM (Protopam)
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Toxins
botulinum toxin (BOTOX)
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Muscarinic ANTAGONISTS (anticholinergics)
atropine (hyoscyamine) and homatropinescopolamine and methscopolaminedicyclomine (Bentyl)propanthelineglycopyrrolate (Robinul)ipratropium (Atrovent)tiatropium (Spiriva)benztropine (Cogentin)trihexyphenidyl (Artane)tolterodine (Detrol)oxybutynin (Ditropan)solifenacin (VESIcare)tropicamide (Mydriacyl)
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Botulinum toxin (BOTOX) acts by
inhib. syn/rel of ACh
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M1 rec
in symp. gang and myenteric plexus, unclear functionpossibly stomach: med gastric acid sec
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M2 rec
located in heart, some smooth musc
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M3 rec
glands, smooth musc, BVs
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ACh stimulated muscarinic rec in what kind of manner
dose/conc. dependent, relatively nonselective
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Nm vs Nn rec.
Nm rec. located on sk. music at NM junc, Nn rec. located in autonom ganglia and adrenal medulla
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at low/mod doses ACh...at high doses...
-stim both types nicotinic receptor-desensitizes rec at high conc.-->gang. blockade, muscle paralysis(in contrast to muscarinic: no desensitization, just plateau)
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PS heart
atria, SA node, AV node, minor to ventricles-dec. HR by slowing firing of SA nodal pacemaker cells and slowing AV conduction-only min. effects on ventricular contractility and automaticity
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PS BVs
not inn. by PS, but endothelial cells in most BVs do contain muscarinic rec., stim. by ACh or muscarinic agonists-->NO (cGMP) med vasodilation-->dec. in BP-enhanced by cholinesterase inhibs like edrophonium, blocked by muscarinic antagonists such as atropine
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BVs that receive more PS inn.
corpus cavernosum, some cerebral, coronary, skeletal musc. BVs
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PS eye
pupillary constrictor muscles: miosisciliary muscle: accommodation-lowered IOP (outflow of AH)
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PS smooth muscle
bladder, stomach, sm. intestine, bowel, etc.-typ. stim. contraction of sm. musc to increase motility
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PS glands
salivary, lacrimal, mucosa of GI, airway, etc.-stimulate secretions (muscarinic ANTAGONISTS have drying effect)
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PS airways
bronchoconstriction and inc. respiratory secretions-
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Muscarinic ANTAGONISTS useful in asthma tx
ipratropium (Atrovent) tiatropium (Spiriva)(muscarinic agonist or cholinesterase inhibs. can aggravate asthma)
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PS GI
stimulate GI motility and secretionalso reg by "enteric NS"
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PS NM junction
ACh released by motor neurons can act on nicotinic rec. at motor end plate to cause musc. contraction *receptors are DESENSITIZED if excess ACh (i.e. high dose cholinesterase inhib.)-->musc. paralysis*exogenously admin. ACh has little effect on skel. musc. -nicotinic effects can be inhib by ganglionic and NM blockers
122
direct acting muscarinic agonist activity
inc. GI motility, secretiondec. HRdec. BP due to dec. CO and direct vasodilationcontraction of bladder, relax. of ur. sphinctersmiosis and dec. IOPstim of secretions
123
adverse effects of muscarinic stimulation
hypotension, bradycardia, chronchoconstriction, diarrhea, cramping, urinary incontinence, excessive sweating, salivation
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major tx uses of muscarinic agonists
promote GI motility (bethanechol)tx urinary retention (bethanechol)tx of glaucoma (pilocarpine, acetylcholine, carbachol)tx of sal. gland dysfunc (pilocarpine, cevimeline)pulmonary function testing in asthma (methacholine)- dangerous dx test
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when muscarinic agonists are contraindicated/used w/ caution
asthma, bradycardia, hypotension, vasomotor instability, CAD, peptic ulcer disease, hyperthyroidism, weakened smooth musc of bladder/GI, urinary/intestinal obstruction
126
DO NOT give choinesters..
IV or IM, but rather subQ, orally, topically(eye)
127
acetylcholine
limited, tx for glaucoma-->rapidly hydrolyzed by pseudocholinesterase in plasma
128
carbachol
analog of ACh, resistant to hydrolysis-stim both muscarinic and nicotinic-topically for glaucoma
129
methacholine
ACh analog, stim muscarinic (little nicotinic effect)used in asthma pulmonary function testing
130
bethanechol (Urecholine)
ACh analog, resis to hydrolysis, direct muscarinic agonist (little nicotinic effect)stim. GI motility and tx for urinary retention
131
pilocarpine (Salagen, Ocusert Pilo)
muscarinic agonist, tx for glaucoma and xerostomia (dry mouth) due to poor salivary secretion
132
cevimeline (Evoxac)
muscarinic agonist, tx for salivary gland dysfunction
133
ascarine
natural in mushrooms (Inocybe and Clitocybe)-salivation, lacrimation, nausea, extreme GI hypermotility, bronchospasm, bradycardia, hypotension, shock-can be tx with high dose atropine (1-2 mg IM every 30 min)
134
cholinesterase inhibitors have similar effects as muscarinic agonists, plus
stimulation of skeletal muscle-->paralysis of skeletal muscles @ toxic doses
135
toxic effects of cholinesterase inhibitors (cholinergic crisis)
i.e. organophosphate insecticide/nerve gase poisoning-SLUDGE (salivation, lacrimation, urination, defection, GI distress, emesis)-skel musc fasciculations-->paralysis-bradycardia, hypotension, shock-severe miosis-CNS stimulation and seizures-->coma-chronic exposure to some-->demyelination of axons and various neuropathies
136
tx of acute cholinesterase inhibitor poisoning
-administer high doses atropine (2-4 mg IV initially) followed by 2 mg IM every 10 min until symptoms disappear to block muscarinic receptors -admin pralidoxime to reactivate enzyme (effective w/ organophosphates only)-provide additional symptomatic tx as needed (i.e. diazepam for seizures)
137
major tx uses of cholinesterase inhibitors: myasthenia gravis
dx: endrophonium testtx: pyridostigmine, neostigmineMG is AI against nicotinic rec. at motor end plate
138
Tensilon Test
admin 2-8 mmg edrophonium; improvement in musc. strength suppors myasthenia gravis dxif musc. wkns worsens: indicative of musc. wkns from exc. doses other cholinesterase inhibitors (cholinergic crisis)- 5 min duration of action
139
other (more commonly used) myasthenia gravis dx tests
electromyography (EMG)serology
140
cholinesterase inhibitors: tx of glaucoma
cholinergic agonists (acetylcholine, carbachol, pilocarpine)cholinesterase inhibitors (echothiophate)again..these contract ciliary musc-->put tension on trabecular meshwork-->inc. outflow of AH through canal of Schlemm
141
cholinesterase inhibitors: tx of Alzheimer's
loss of cholinergic neurons (Nucleus basal is of Meynert)-->raise ACh levels and reverse deficittetrahydroaminoacridine (Tacrine)* original, but causes liver damagerivastigmine (Exelon)donepezil (Aricept)galantamine (Reminyl)
142
other uses of cholinesterase inhibitors
-tx of poisoning by atropine/other antimuscarinic drugs: physostigmine-reversal of NM blockade by nondepol. NM blockers: neostigmine, pyridostigmine-tx of atony of bladder or GI tract (i.e.: urine retention, paralytic ileus, etc)-pyridostigmine used by military to protect against nerve gas: ""pre-exposure antidotal enhancement"
143
CI's and precautions in cholinesterase inhibitor use
asthmabradycardia, hypotension, CADpeptic ulcer diseaseurinary or intestinal obstruction
144
reversible cholinesterase inhibitors, quaternary ammonium compounds- cannot enter CNS
edrophonium (Tensilon), neostigmine (Prostigmin) pyridostigmine (Mestinon)
145
reversible cholinesterase inhibitor, nonquaternary-so able to enter CNS
physostigmine/eserine (Antilirium)tx for atropine/other antimuscarinic agent poisoning(fallen into disfavor, esp. with tricyclic antidep. OD)
146
Organophosphate insecticides
parathion, malathion-->need to be oxidized to active metabolites (paroxone and malaoxone) happens faster in insects, cannot detoxify(but can still cause toxicity in humans)-can be absorbed thru skin-S&S typical of cholinesterase inhibs.-tx poisoning w. atropine, pralidoxime (& other sympt. support)
147
Carbamate insecticides
carbaryl-absorbed less thru skin-tx poisoning w/ atropine, pralidoxime is NOT useful in tx of carbamate insecticides!
148
DFP/Isoflurophate and Nerve Gases
Sarinpotent, toxic, irreversible cholinesterase inhibitors-S&S typ. for cholinesterase inhibs.-tx poisoning w/ atropine and pralidoxime-DFP/Isoflurophate: glaucoma tx
149
Pralidoxime/2-PAM (Protopam)
cholinesterase reactivator! binds phosphate grp that inhib. enzyme thereby regenerating enzyme-antidote for orgphos poisoning w/in 2 hours of exposure-does not work with carbamate insecticides
150
ED drugs
Sildenafil (Viagra)Vardenafil (Levitra)Tadalafil (Cialis)-NO activates guanylcyclase in vasc. sm musc to produce cGMP-->vasodilation-->erection-drug inhibits cGMP phosphodiesterase type 5 (PDE-5) which breaks down cGMP
151
ED drug side effects/toxicities
-general vasodilation-->hypotension-->reflex inc. in HR (problem for men w/ CV disease)-visual distrubances: blue/green discrim. probs-auditory disturbances
152
ED pharmacokinetics
oral admin, sildenafil and vardenafil onset: 30 min, pk plasma levels about 1 hr, duration 4 hrs tadalafil longer 1/2 life, onset 45 min, and duration about 36 hrs-metabolized by CYP3A4: potential for drug interactions-dosage adj. for renal/hepatic disease pts
153
ED drug interactions
erythromycin, ketaconazole, cimetidine, others metabolized by CYP3A4vasodilators (nitrates, Ca2+ channel blockers, a1 blockers)sympathomimetics
154
botulinium toxin
produced by Clostridium botulinium-rel. of ACh from nerve endings-->affects both autonomic nerve endings (antichol. effects) and NM junction (paralysis)-death from diaphragmatic paralysis, 0.5-1.0 ug dose may be fataltx: sympt. support (resp) + abx to toxin-med uses: optham. disorders, wrinkles (BOTOX), dystonia, exc. sweating, over-active bladder
155
anticholinergic pharm effects
competitive antagonists at muscarinic receptors-drying of secretions-dec. tone and motil. of GI tract-relax. of bladder and urine retention-bronchodilation-mydriasis w/ cycloplegia (loss of accomm.) and inc. in IOP-inc. HR (*atropine may cause initial slight bradycardia)-CNS: sedation and amnesia at low doses; excitation and seizures at toxic doses*quaternary salts do NOT produce CNS effects
156
therapeutic uses of anticholinergics part 1
-GI disorders-urine incontinence-opth: mydriatic agents (*do NOT use in pts w/ glaucoma!)-anesthesiology to reduce vagal tone on heart and dry secretions; also to prevent muscarinic side effects when cholinesterase inhibs used to reverse effects of NM blockers-antidote for poisoning with cholinesterase inhibs. or muscarinic agonists (some mushroom poisoning)
157
therapeutic uses of anticholinergics part 2
-prevent motion sickness (Scopolamine)-Parkinson's (benztropine, trihexyphenidyle, diphenhydramine)-dental proc. to inhib salivation (atropine, glycopyrrolate)-cardiac stim in emergencies (atropine)-asthma and COPD (ipratropium, tiatropium)-pulmonary med to dry resp secretions
158
anticholinergic side effects/toxicities
dry mouthdry, hot skinconstipation, urine ret.visual disturbances, blurred vision, photophobiaCNS effects: sedation, confusion, amnesia (elderly)
159
anticholinergics/muscarinic antagonist CIs/precautions
glaucoma (esp. narrow angle)prostatic hypertrophyCV instabilitysevere ulcerative colitis
160
acute antichol. poisoning
dry, hot skin/ hyperthermiasevere mydriasis, blurring, photophobiaCNS stim: agitation, halluc, seizure-->coma-->deathcessation of GI motility (no bowel sounds)weak rapid pusle, tachy, arrhyths.
161
tx of acute antichol. poisoning
admin of physostigmine or other cholinesterase inhibitorsbenzos for seizure txice baths to cool down, keep pt in dark, quiet area
162
other drugs with anticholinergic side effects
antihistamines, antipsychotics, antidepressants, etc.
163
atropine (Hyoscyamine) and Homatropine
#NAME?
164
atropine effects: heart
tachycardia w/ slight inc. CO (may have transient bradycardia)tx for MI w/ inc. vagal tone: low CO and dec. BP
165
atropine effects: BVs
can reverse hypotensive actions of acetylcholine/other muscarinic agonistscutaneous vasodil and flushing of skin
166
atropine effects: eye
#NAME?
167
atropine effects: GI tract
inhib. motility and tone (antispasmodic action for IBS)need high dose to dec. acid sec, so H2-histamine blockers (cimetidine, ranitidine, nizatidine, famotidine, or PPIs) used for peptic ulcers instead
168
atropine effects: urinary tract
relaxes bladder body and contracts sphincter-->retentiontx incontinence, CI in prostatic hypertrophy
169
atropine effects: sweat glands
blocks muscarinic rec.-->inhib sweating-->rise in body temp *children extra sensitive
170
atropine effects: salivary glands
inhib. saliva sec. "dry mouth"
171
atropine effects: respiratory tract
dries secretions, bronchodilation
172
atropine effects: CNS
depressant (low doses) and stimulation (hight doses): agitation and seizuresmod-high: hallucinogenic
173
atropine tx uses
#NAME?
174
at 0.5 mg atropine
some cardiac slowing, mouth dryness, sweating inhib
175
1.0 mg atropine
def dry mouth, thirst, heart accel. (slowing 1st), mild pupil dilation
176
2.0 mg atropine
rapid HR, marked dry mouth, dil. pupils, blurred near vision
177
5.0 mg atropine
all above + diff speaking/swallowing, restless, fatigue, HA, dry, hot skin, diff mictur., red intestinal peristalsis
178
10.0+ mg atropine
all above + more marked, pulse rapid/wk, iris almost obliterated, vision v. blurred, skin flushed, hot dry, scarlet, ataxia, restless, excitement, hallucinations, delirium, coma
179
Scopolamine (hyoscine) and Methscopolamine
-plant Hyoscyamus niger (henbane), chem sim to atropinequarternary analog, does NOT cross BBB-sim to atropine but more of CNS depressant (sed/amn) than atropine-oral and patch form (Transderm Scop) for pref of motion-sickness, vertigo
180
Dicyclomine (Bentyl)
nonquart. antimuscarinic-used as intestinal antispasmodic for IBS tx
181
Propantheline (Pro-Banthine)
antimuscarinic-antispasmodid, IBS txquaternary comp. w/ few CNS effects
182
Glycopyrrolate (Robinul)
quart. antimuscarinic (no CNS effects)-used in anesthesiology as prep med to dry resp. sec and inhib vagal reflexes-also used as gen purpose antimuscarinic
183
Ipratropium (Atrovent)Tiatropium (Spiriva)aclidinium (Tudorza)
antimuscarinicsquat. salts admin. by inhalation for asthma and COPD txfew systemic effectstiatropium longer duration than ipratropiumaclidium: new drug approved for COPD (long acting in lungs, broken down by esterases in plasma: few systemic effects)
184
Benztropine (Cogentin)Trihexyphenidyl (Artane)
centrally acting antimuscarinics used in Parkinson's/drug-ind. Parkinsonism tx
185
Tolterodine (Detrol)Oxbutynin (Ditropan)Solifenacin (VESIcare)
antimuscarinics, tx of urinary incontinence due to overactive bladder
186
Tropicamide (Midriacyl)
antimuscarinic used to dilate pupil for examination
187
first gen H1 antagonists: v. sedating antihistamines
Promethazine hydrochloride (Phenergan)Hydroxyzine (Vistaril)
188
first gen H1 antagonists: sedating antihistamines
Diphenhydramine (Benadryl)Dimenhydrinate (Dramamine)Doxylamine (Unisom)Chorpheniramine maleate (Chlor-Trimeton)Meclizine (Bonine, Antivert)
189
second gen H1 antagonists: non-sedating antihistamines
Loratadine (Claritin, Alavert)/Desloratidine (Clarinex)Certirizine (Zyrtec) and Levocetirizine (Xyzal)Fexofenadine (Allegra)
190
H2 antagonists
Cimetidine (Tagamet)Ranitidine (Zantac)Famotidine (Pepcid)Nizatidine (Axid)
191
histamine functions
mediates phys. resp to tissue/cell injurymediates inflamm. resp/allergic reactionsreg. cell growth/repairreg. gastric acid secNT in CNSpos. reg. of cardiac functions
192
histamine syn
syn from histidine by histidine decarboxylase
193
histamine metab
involved N-methylation-->oxidation to N-methylimidazole acetic acid
194
histamine storage
mast cells and basophilsskin and mucosa of GI and resp tractsIC histamine stored in granules, loosely bound to proteoglycans like heparin sulfate or chondroitin sulfate
195
histamine release: drug/chem induced
-displaced by amine drugs (morphine, tubocurarine, B-blockers)-compound 48/80-toxins and venoms
196
histamine release may released in response to
cell/tissue damage
197
histamine release: immunologic stimulation
mast cells sensitized w/ IgE Abs-->rel. histamine when exposed to approp. allergen-other autocoids syn or del: PGs, LKTs, kinins (bradykinin)
198
histamine release: neuronal and endocrine stimulation
gastric mucosa: rel in resp to neuronal (vagal)/endocrine stim (gastrin)-neuronal med. by ACh -the histamine binds to H2 rec on parietal cells-->HCl sec-->permissive effect, allows gastrin and acetyl choline to directly stim. acid secretion(H2 rec ANTAGONISTS are effective in red. sec of gastric acid in response to histamine, vagal stim, ACh, or gastrin)
199
physio effects of histamine
- dilation of sm. BVs-->flushing, lowered peri. resis., dec. BP
- inc. cap perm-->leakage of fluid and protein into extravascular space
- stim of peripheral nerve ending: pain, burning, itching
200
physio effects of histamine: triple respons
- red spot, local (dilation of minute BVs)
- flare (dil. or neighboring arterioles)
- wheal (inc. cap perm)
201
physio effects of histamine: histamine shock
vasodilation and fluid leakage into EV space-->sig. drop in BP (resembles traumatic, septic, or hemorrhagic shock)
202
physio effects of histamine: bronchial constriction
asthmatic and anaphylactic bronchospasm
-not completely dep on histamine, so not effec. antag by antihistamines alone (use sympathomimetic drugs, methylaxanthines)
203
physio effects of histamine: stimulation of gastric acid secretion
in response to stress, vagal stim, gastrin and cholinergic agonists
-mediated by H2 receptors (blocking these red. stomach acid sec.)
204
physio effects of histamine: cerebral vessels and histamine
-v. sens. to histamine!-->intense dilation-->pulsatory HA (stretching of sensory nerve endings-histamine cephalalgia)
(attempt to antag H1 and H2 rec, little success)
205
physio effects of histamine: direct effects on heart
inc. force of contraction
| slowing of AV conduction
