ALL THE DRUGS Flashcards
muscarinic agonist
increase SLUDGE, decrease HR, miosis, dec dopamine. bronchoconstriction
acetylcholine
muscarinic agonist, quat, all synapses
methacholine
muscarinic agonist, B carbon methyl, quat, induces asthma attack
carbachol
muscarinic agonist, quat, carbamate, glaucoma
bethanechol
muscarinic agonist, carbamate and methyl on b carbon, treats urinary retention (non-obstructive) and dec symptoms of depression
muscarine
muscarinic agonist, quat,
pilocarpine
muscarinic agonist,, tert, glaucoma, miosis after eye exam
cevimeline
muscarinic agonist, tert, salivary gland issue
muscarinic antagonist
decreases slud, mydriasis, increases HR, bronchodilation
muscarinic agonist SAR
- N capable of being + , no huge groups dec methyls for H on N terminal = dec potency / increased carbons on N antagonist
- ethylene bridge (2C)
- alcoxyl group (ketone, ester, ether)/ Ing’s rule of 5/
SAR muscarinic antagonist
- N tertiary or quat
- R1 and R2 heterocyclic (can’t be naphthelene)
- R3 -H, -OH part of ring
- X=ester, ether
atropine
muscarinic antagonist, ophthalmic, tert
tropicamide
muscarinic antagonist, opthalmic, tert
cyclopentolate
muscarinic antagonist,, opthalmic, tert
iptratropium
COPD, muscarinic antagonist,, quat
tiotropium
COPD, tert, muscarinic antagonist,
umeclidinium
COPD, tert, muscarinic antagonist,
glycopyrrolate
COPD, tert, muscarinic antagonist,
acidinium
COPD, tert, muscarinic antagonist,
benztopine
parkinsons, tert, muscarinic antagonist,
trihexylphenydil
parkinsons, tert, muscarinic antagonist,
dicycloamine
IBS-D, tert, muscarinic antagonist,
scopolamine
motion sickness, tert, muscarinic antagonist,
oxybutynin
tert, OAB/urinary retention, muscurinic antagonist, cmax related to ADE/lipophillic/P450
tolterodine
tert, OAB/urinary retention, muscurinic antagonist, prodrug 2D6
solifenacin
tert, OAB/urinary retention, muscurinic antagonist, functional selectivity for M3 bladder/ 3A4
darifenacin
tert, OAB/urinary retention, muscurinic antagonist, , pharmacologically selective M3, cause dry mouth, 3A4 and 2D6
trospium
tert, OAB/urinary retention, muscurinic antagonist, P450/esterase/hydroxylation
fesoterodine
tert, OAB/urinary retention, muscurinic antagonist, prodrug 5-HMT
AChE inhibitors
increases the ACh, increase SLUDGE, decreases HR and miosis of the eye
neostigmine
AChE inhibitor, quat, carbamate ester, myasthenia gravis
phyostigmine
AChE inhibitor, tert, carbamate ester
pyridostigmine
AChE inhibitor, quat, carbamate ester, myasthenia gravis
rivastigmine
alzheimers, carbamate ester, tert
carbamate ester
“stigmine” temporary covalent modification, work through being metabolized
edrophenium
reversible inhibitor of AChE, quat
galantamine
reversible inhibitor of AChE, tert, alzheimers
doneprexil
reversible inhibitor of AChE, tert, alzheimers
echothiophate
irreversible inhibitor of AChE, quat, glaucoma
organophosphates
toxic/dephosphroylate = resistant to hydrolysis = too much ACh build up / use 2-PAM if hasn’t aged
neuromusuclar blocking agent MOA
immobilize patients for surgery, procedures = work by causing paralysis
depolarizing agents
opens the cel membrane and becomes refractory and the muscle becomes resistant to further stimulation, fasciculations and then flaccid paralysis
succinylcholine
more ach wouldnt do anything because you are blocking to the binding site to cause muscle activation
mivacurium
benzylisoquinolines, non-depolarizing NMBA, shorter half life, quat
atracurium
shorter half life, benzylisoquinolines, quat, non-depolarizing, degradation/hoffman elimination
cisatrascurium
non-depolarizing NMBA, spontaneous degradation/hoffman elimination
rocuronium
amino steroid, hepatic and renal, intermediate half life, non-depolarizing NMBA, hepatic and renal
vecuronium
amino steroid, hepatic and renal, intermediate half life, non-depolarizing NMBA
pancuronium
amino steroid, hepatic and renal, longest half life, non-depolarizing NMBA
alpha 1 agonist
vasoconstriction, decongestant, red eye, inc BP
phenylephrine
alpha 1 agonist, decongestant
naphazoline
alpha 1 agonist
tetrahydrozoline
alpha 1 agonist
oxymethazoline
alpha 1 agonist
high dose DA
alpha 1 agonist
Epi high dose
alpha 1 agonist = B, vasoconstrict, inc TPR
Epi low dose
B, inc HR, dec insulin, dec digestion, inc lipolysis, dec uterine, dec urgency
NE
alpha, alpha 2, b1 (NO B2), vasoconstrict, cardiac dec (vagal), dec digestion, dec urine
alpha 2 agonist
dec SNS, dec HR, dec BP, dec TPR - upregulation of alpha 1 and b1
SAR alpha 2 agonist
2, 5 ortho substituents (cl)/ bridge / basic nitrogen grouping/ perpendicular
clonidine
alpha 2 agonist, with opioid for pain, causes xerostomia
guanacifine
alpha 2 agonist, ADHD
methyldopa
alpha 2 agonist
dexmedetomidine
sedative
b1 agonist
inc FOC, inc HR, used to preserve CO
dobutamine
B1
isoproterenol
nonselective B agonist
mid dose D1
D1, B1
B2 agonist MOA
bronchodilation
B2 agonist SAR
2 hydroxyl required, 3-hydroxymethyl, 3-formamido, carbostyril ethanolamine side chain (R conformation) / basic substituents
albuterol
B2 agonist, SA
tertbutaline
B2 agonist
salmeterol
B2 agonist, LA
fomoterol
B2 agonist
indacterol
B2 agonist
oldaterol
B2 agonist, LA
vilanterol
B2 agonist, LA
fenoldapam
D1 agonist - expensive
D1 MOA
low dose dopamine, mesenteric dilation, “renal dose”
cardioselective B1 antagonist MOA
dec HR, dec FOC, dec CO
cardioselective B1 antagonist SAR
SAR: adernergic side chain / ether group / para substituents with an H bond acceptor 1 to 2 atoms away
metroprolol
cardioselective B1 antagonist
atenolol
cardioselective B1 antagonist MOA, renal
bisoproprolol
cardioselective B1 antagonist MOA, renal
acebutolol
cardioselective B1 antagonist MOA, hepatic
esmolol
cardioselective B1 antagonist MOA, 10 min t1/2 bc esterase
alpha 1 antagonist
BPH, kidney stone, last option for decrease in HR
parazosin
non-selective alpha 1 antagonist
terazosin
non-selective alpha 1 antagonist
doxazosin
non-selective alpha 1 antagonist
alfuzosin
A alpha 1 antagonist- BPH/kidney stones
tamulosin
A alpha 1 antagonist- BPH/kidney stones
silodosin
A alpha 1 antagonist- BPH/kidney stones
pentoalimine
non-selective alpha, extraversion of vasculature
phenoxybenzamine
nonselective alpha = irrreversible= pneumocytoma
partial agonist
labetol (B2), acebutolol (B1), pinidol (B1)
nonselective B antagonists
pinidolol, propanolol, nadelol
labetalol
bblocker with vasodilation, alpha 1 antagonsit/ B1 antagonist / B2 ISA, glucuronidation, CYP450
nebivolol
bblocker with vasodilation, NO increased production
carvedilol
bblocker with vasodilation, block Ltype CC, antagonist at alpha 1, antioxidation, undergoes o-dealkylation
bblockers with vasodilation good for
asthma and COPD
renally metabolized bblockers are good for
patients with decreased liver function
renally metabolized bblocker
nadelol, atenolol, bisprolol
esmolol
quickly metabolized by plasma esterases
BBlockers elim by which enzyme
CYP2D6
random uses of BBlockers
glaucoma, thyrotoxosis, tremors, migraine
BBlockers adverse effects
lipid cns depression dec libido hypoglycemia mask overdose causes AV block
when do you not want to use a nonselective BBlocker?
pts with asthma/ COPD (constrict airways), diabetes - dec insulin secretion