just the drugs Flashcards
What are the direct acting cholinomimetics
Ach bethanechol carbachol cevimeline methacholine pilocarpine varenicline(chantix)
What are the main cholinesterase inhibitors
donepezil, neostigmine, physostigmine, pyridostigmine
What is the cholinesterase regenerator
pralidoxime
What are the major anti-muscarbinic drugs
scopolamine, atropine, ipratropium, tiotropium, oxybutynin, trospium,
What is the ganglion blocker
mecamylamine
what is used to Tx motion sickness
anti mAchR- scopolamine
what anti muscarinc drug is used to treat asthma or COPD
ipratropium and tiotropium
what antimAchR is used for urinary disorders
oxybutynin
in cholinergic overdoes what drug is used for reversal
atropine and pralidoxime
Which cholinergic agonists cannot distribute to brain
Ach, carbachol and bethanechol because they are quarternary ammonium groups
what cholinergic mimetic is used orally to treat xerostomia
cevimeline
what drug is given for smoking cessation
mAchR agonist- varenicline
how does alcohol work on mAch transmission
binda AchE and blocks its actions
What are examples of organophosphates
echthiophate, parathion, malathion, sarin, soman, tabun
Which cholinesterase inhibitor is most potent/dangerous
the organophosphates because are covalent and irreversible
why is there no CNS distribution with cholinesterase inhibitors: neostigmine
because they are quaternary and charged
why does physostigmine have CNS distribution
tertiary uncharged AchE inhibitor
do organophosphates cross BBB
yes because lipid soluble
which sites of action do AchE inhibitors work on
nAchRs and mAchRs on effector organs
what drug do you use to Tx and overdoes of anticholinergics when patient is displaying neuro Sx?
physostigmine because crosses BBB
what will occur if use AchE inhibitor with cholinergic agonist
enhanced effect
what happens if use AchE inhibitor with beta blocker
bradycardic
What is a cholinesterase regenerator that we use
pralidoxime
what do you give if suspected nerve gas poisoning
atropine and pralidoxime
to pretreat for nerve agen poisoning what is given
pyridostigmine
is atropine a selectice mAchR antagonist?
no
describe effects of atropine on heart in low doses? high doses?
low causes initial bradycardia
high causes tachycardia
how does atropine suppress thermoregulatory sweating
works on the sympathetic cholinergic nerve fibers
what happens with ganglion blocks
enhanced sympathetic tone
what are the catecholamine adrenergic agonists
epinephrine norepinephrine isoproterenol dopamine dobutamine
what are alpha agonists
phenylephrine, methoxamine, mildodrine
what are the beta 2 specific agonists
albuterol, salmeterol, formoterol, terbutaline, ritodrine, metaproterenol
what are the adrenergic agonists that have mixed actions
ephedrine and pseudoephedrine because release NE and have direct agonist activity
what are the systemic effects of alpha1 adrenergic agonists
constriction blood vessels mydriasis contraction of spleen and uterus constrict sphincter of bladder glycogenolysis ejaculation
what are the systemic effects of alpha 2 agonist
inhibit release of insulin, relaxation smooth m
which adrenergic R is responsible for glycogenolysis in liver
B2
what are the systemic effects of B1 agonist
positive inotropic and chronotropic effects of heart
stimulates renin release
what are the systemic effects of B2 agonists
relaxation of bronchioles and uterul
relaxation of vasc smooth m in blood vessels
glycogenolysis
stimulates release of insulin
relaxation of detrusor muscle and intestinal smooth m
what blood vessels in skel muscle does epi work on
alpha 1 and beta 2, higher affinity for beta2 (low doses then target beta 2 more)
what blood vessels can epi activate beta 2
coronoaries and skel m vasculature
which catecholamine increases HR (chronotropic)
isoproterenol
epinephrine
what catecholamine increases total peripheral R so increases BP
norepi
which catecholamines increase CO
epi and isoproterenol
what are the net effects of epi on BP
diastolic dec
systolic increase
mean unchanged
What is a contraindication for epi
HTN, shock, hyperthyroidism, angina pectoris, asthmatics with degenerative heart disease
norepi does not work on what adrenergic R
beta2
what are the effects of norepi on heart
increase in inotropic and chronotropic
reflex bradycardia from vasoconstriction
so net is inc inotropic and dec chronotropic
What is the net effect of norepi on BP
increased
What R does isoproterenol work on
all of betas
what is the change in BP from isoproterenol
increased systolic and decreased diastolic
decreased MAP
what are the effects of dopamine on the heart
mild positive inotropic and chronotropic effects compared to isoproterenol
what are the effects of dopamine on blood vessels
vasodilation of mesenteric and renal vascular beds (dopamine R)
what is dopamine used clinically for
shock, CHF because increase CO but no change in TPR
what does fenoldopam do and used to Tx?
synthetic dopamine D1 agonist
Tx HTN
what does bromocriptine do and used to Tx?
synthetic dopamine D2
parkinsons or prolactinemia
what is dobutamine
selective B1 agonist (partial
what is dobutamine used for
AMI
increases CO with less change arrhythmias
what is an absolute contraindication for dobutamine
idiopathic hypertrophic subaortic stenosis
What R does phenlephrine work on
alpha 1 agonist
used as nasal decongestant and for glaucoma and mydriasis
What is Midodrine
an alpha 1 agonist used for orthostatic hypotension
what is the mechanism of amphetamines
release NE from terminats and withh inhibit the reuptake by competition
What are the effects of amphetamines
CNS stimulation, vasoconstriction and positive inotropic effect, neg chronotropic
What are the clinical uses of amphetamines
Narcolepsy
ADHD
Obesity
What are the side effects of amphetamines
insomnia, delierium, anxiety
arrhythmias, anginal pain, nausea and vomiting
what are signs of acute and chronic toxication of amphetamines
acute are convulsions, coma and death
chronic are abnormal mental state, weight loss and psychotic reaction
How do we treat amphetamines
ammonium chloride to prevent reabsorption
what is ephedrine/pseudoephredrine and what are they used for?
Beta R effects and releases NE
used for pressor agen in spinal anesthesia
nasal decongestant
severe/acute bronchospasm
what are the sideeffects of ephedrine
anxiety, insomnia, palpitations
