Drugs Flashcards
Acetylecholine
Nicotinic and muscarinic receptors
“Chief parasympathetic NS NT –> contracts smooth muscle, dilates blood vessels, increases secretions, slows heart rate
Additionally involved in muscle contraction (ex. Myasthenia gravis “
Donepezil (Acetylcholinesterase inhibitor)
Increased ACh. Used in alzheimers
improves memory function, attention, ability to ineract with others in CNS diseases “
Neostigmine (Acetylcholinesterase inhibitor)
Neo CNS = No CNS penetration (quaternary
amine).
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative).
Physostigmine (Acetylcholinesterase inhibitor)
Increases ACh. Phreely (freely) crosses blood-brain
barrier = CNS (tertiary amine).
“Can reduce pressure in the eye by decreasing fluid (treatment for glaucoma)
Antidote for anticholinergic toxicity; physostigmine “phyxes” atropine overdose.
Edrophonium (Acetylcholinesterase inhibitor)
increase in the ACh
Historically used to diagnose myasthenia gravis
Pyridostigmine (Acetylcholinesterase inhibitor)
Increased ACh. Increased muscle strength. Preferred use for MG (long acting). does not penetrate CNS (quaternary amine).
Pilocarpine (Cholinomemetic)
Potent stimulator of sweat, tears, and saliva Open-angle and closed-angle glaucoma,
xerostomia (Sjögren syndrome)
resistant to AChE, can cross blood- brain barrier (tertiary amine). “You cry, drool, and sweat on your ‘pilow.’ ”
Bethanechol
Cholinomemetic
muscarinic and nictonic receptors
Activates bowel and bladder smooth muscle; resistant to AChE. No nicotinic activity. “Bethany, call (bethanechol) me to activate your bowels and bladder.”
Nicotine (stimulant of nicotinic acetylcholine receptors in autonomic ganglia)
nicotinic receptors
increase HR, heightened mood, elevated BP, increased alertnes, better memory
Atropine (anti-muscarinic)
Used to dilate the pupil.
Blocks DUMBBeLSS in cholinesterase inhibitor poisoning. Does not block excitation of skeletal muscle and CNS (mediated by nicotinic receptors).
Side effects:
Hot as a hare Dry as a bone Red as a beet Blind as a bat Mad as a hatter Full as a flask
Darifenacin (Anti-muscarinic)
inhibiton of muscarinic receptors
typically used to treat overactive bladder or urgency incontinance (by relaxing bladder muscles)
Botulinum toxin (Anti-cholinomemtic )
SNARE proteins in motor neurons causing inhibition of release of ACh
“Causes decending flaccid paralysis
Affects PNS only (can’t break BBB)”
Glycopyrrolate (muscarinic antagonist)
M1 and M3 specific antagonist both are Gq
typically used preoperatively to reduce drooling and to reduce airway secretions
Ipratropium (Inhaled M3 antagonist)
M3 in the lungs
COPD, asthma (“I pray I can breathe soon!”).
Oxybutynin (Oral M3 antagonist)
Reduce bladder spasms and urge urinary
incontinence (overactive bladder).
Scopolamine (M1 antagonist)
CNS M1 antagonist
can be used in a transdermal patch to treat motion sickenss
Pralidoxime (Cholinesterase reactivator)
AChE
“antidote to organophosphate
adminstered after atropine in organophosphate poisoning “
Hexamethonium (non-depolarizing nicotinic receptor blocker)
especially blood vessel nAChR
used for chronic hypertension
A compound that activates the M3 receptor would do what?
PNS: Rest and digest: M1-M5
Bronchoconstriction, vasodilation, urination, defecation, pupil constriction, bradycardia
ACH injection would cause what symptoms?
Bradycardia, miosis, bronchoconstriction, urination, defecation, vasodilation
Pilocarpine would increase saliva secretion and what else? What receptor is activated?
It would induce miosis (pupil constriction) and would act on the M2
Blocking nicotinic receptors at PNS and SNS ganglia would cause what symptom?
Urinary retention
Loss of basal autonomic tone (mainly PNS)
Vasculature + sweat glands are under SNS control
An overdose of pyridostigmine would cause what symptoms?
Bradycardia
pyridostigmine= ACHE inhibitor, increase ASH = increase PNS
DUMBELLS
What medication is used for COPD and is a muscarinic receptor inhibitor?
Ipratropium (induces bronchodilation)
What medication is used to test for MGr?
Edrophonium
Nicotine overdose may cause convulsions and tachycardia. Why?
Nicotine activates the autonomic ganglia of the CNS
A medication given to treat urinary retention would stimulate what receptor and cause what 2nd messenger?
M3(q) which would increased IP3 + DAG
Hexamethonium does what to pupil, blood pressure, and HR?
Decreases blood pressure (hypotension), dilate eyes (SNS), and cause tachycardia (SNS)
Hexamethonium is a ganglionic blocker, basal autonomic tone will be reversed
Eye dilation can be caused by what cholinergic antagonist?
Scopolamine (motion -sickness, dilation)
What side effect would be brought on by atropine?
Atropine is a muscarinic antagonist so you get bronchodilation
Darifenacin does what? What receptor does it inhibit?
Darifenacin treats urinary incontinence. It works on the M3 receptor
How does scopolamine transdermal patch work?
it produces a steady blood level that inhibits M1, M4, and M5 receptors
transdermal = steady
Where does Botulinum toxin work in neurons to treat urinary incontinence?
works on the SNARES to prevent release of ACH and PNS stimulation
What drug inhibits M3 receptors but has minimal CNS?
glycopyrrolate (inhibits M2 + M3 in periphery)
why would prolonged treatment w/Donepezil cause bradycardia?
Donepezil = ACHE inhibitor, Increased activation of M2 receptor
If someone has an extremely low blood pressure (80/40 HG), what reflex response would occur in the ANS?
baroreceptor reflex would increase vasoconstriction
Doxazocin, used for BPH, works by what mechanism?
acts as an alpha 1 (vasoconstriction) blocker
“decrease blood pressure
indicated for BPH”
How does Atenolol work on cardiac calls (Gx)?
Atenolol = B1 blocker so it will have opposite Gs function. It will decrease cAMP
A man has increased Tyramine content food + drink. On MAO inhibitor. Why are he having headaches and CP?
Tyramine displaces norepinephrine from synaptic vesicles
Tyramine is a dietary arnine that is an agonist that induces release of norepinephrine (indirect agonist by reversal of NET)
“causes hypertension
metabolized by MAO - hypertensive crisis results from eating aged food while on MAO drugs”
A medication to cause bronchodilation, vasodilation, relaxation of smooth muscle of bladder wall, increase glycogenolysis and gluconeogenesis. What drug is it?
Albuterol: Beta receptors in the lungs (Beta 2 more than Beta 1)
“Treatment for acute asthma / COPD
Bronchodilator for increased air intake “
What would be the side-effect of using phenylephrine long-term in addition to nasal congestion?
phenylephrine (Alpha 1 agonist) will also lead to urinary retention
causes mydriasis, bradycardia, thickening of mucous secretion and significant vasoconstriction
What cardioselective B-blocker also enhances NO productivity?
Nebivolol (decrease Heart rate, increase vasodilation)
Beta 1 blocker, Beta 3 stimulator
“decreases HR and contractility
activation of Beta 3 leads to vasodilation and decreased BP”
Labetalol (Antiarrythmics (class II))
Non-selective Beta blocker and alpha 1 blocker
Similar effects as carvedilol - specifically indicated for hypertension during pregnancy
“slows HR / contractility (Beta block)
decreases vasoconstriction thru blocking alpha 1 (decreases BP)”
Proprnaolo (beta blocker)
general beta blocker
“decreases HR and contractility
helps decrease BP”
If compound Q (B1 drug) is given by itself and has 60% activity/max response. When dobutamine is given, compound Q decreases dobutamine’s affect. What compound is Q?
Acebutolol is a partial agonist. When a full agonist is given, a partial agonist acts as an antagonist
Carvedilol
Non-selective Beta blocker and alpha 1 blocker
a1 antagonist
“slows HR / contractility (Beta block)
decreases vasoconstriction thru blocking alpha 1 (decreases BP)”
Metoprolol
Cardioselective beta blocker
Beta 1 recptors
slows HR and contractility
A man with enlarged prostate is given a med that decreases IP3 + DAG. What is it?
Tamsulosin
Selective alpha 1 antagonist
mostly used to treat BPH (benign prostatic hyperplasia) when the patient is normtensive
cocaine use would result in what physiological effects?
- vasoconstriction
- cocaine is indirect agonist, prevents reuptake of norepinephrine activating SIVS
- Agitaiton, hypertension, tachycardia, pupillary dilation (kind of mimics a sympathetic response)
-Inhibitor of DAT and NET
Med 1 causes vasoconstriction, med 2 causes vasodilation. What are the drugs?
drug 1: phenylephrine
drug 2: doxazocin
A medication (v) increases HR, decreases pupil dilation, decreases blood pressure. What is the drug?
Phentolamine
Non-selective alpha blocker
“Can be used to reverse tyramine toxicity
Decreases BP due to blocking Alpha 1”
A med decreases HR, decreases BP, constricts bronchioles, no change in pupil size. What is the drug?
Propranolol :”decreases HR and contractility
helps decrease BP”
need a dilatory eye agent w/ short lasting effects (so pt can drive home). What drug?
Phenylephrine
a1 agonist
Medication Z increase HR and decreases BP. Acts the same w/Phentolamine and atropine. Propanolol gives opposite effects
propanolol is a non-selective B blocker so the med z must be an B1 and B2 agonist
treatment of HTN w/methydopa would cause what signal transduction to occur?
methyldopa is an a2 agonist so it has Gi effects (decrease cAMP)
Mostly used to treat gestational hypertension
increased HR + increased BP after consuming foods high in tyramine is caused by what pathway?
increase of norepinephrine release
Drug Y has low BP, Drug Y + hexamethonium lowers bo even more. Drug y + atropine raises BP. What is Drug y?
Drug Y = Ach (reversed by atropine) works on M3 to lower BP
Albuterol
β2 > β1
acute asthma or COPD
Amphetamine
Indirect general agonist, reuptake inhibitor, also releases stored catecholamines
ADHD, narcolepsy, obesity
Clonidine (α2-agonists)
Hypertensive urgency (limited situations), ADHD, Tourette syndrome, symptom control in opioid withdrawal
Adverse effects: CNS depression, bradycardia, hypotension, respiratory depression, miosis, rebound hypertension with abrupt cessation
Cocaine
Indirect general agonist, reuptake inhibitor
Norepinephrine and Dopamine transporter inhibitor
Causes vasoconstriction and local anesthesia. Caution when giving β-blockers if cocaine
intoxication is suspected (can lead to unopposed α1 activation, activation = extreme hypertension, coronary vasospasm).
Dobutamine
β1 > β2, α
Heart failure (HF), cardiogenic shock (inotropic > chronotropic), cardiac stress testing.
Epinephrine
β>α
Anaphylaxis, asthma, open-angle glaucoma; α effects predominate at high doses. Significantly stronger effect at β2-receptor than norepinephrine.
Isoproterenol
β1 = β2
Formerly for asthma and bradycardia
Electrophysiologic evaluation of tachyarrhythmias. Can worsen ischemia.
Has negligible α effect.
α-methyldopa (α2-agonists)
Hypertension in pregnancy
Midodrine
α1
Autonomic insufficiency and postural hypotension. May exacerbate supine hypertension.
Mirabegron
β3
Urinary urge incontinence or overactive bladder.
Norepinephrine
α1 >α2 >β1
Hypotension, septic shock.
Methylphenidate
Displaces stored catecholamines and inhibits NET and DAT
ADHD, narcolepsy, obesity
Phenylephrine
α1 > α2
Hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant), ischemic priapism.
Pseudoephrine
Non-selective α and ß agonist
Decongestent in cold or rhinitis (vasoconstriction in nasal mucosa, bronchodilation), Sinus or head pressure
Tyramine
Displaces stored catecholamines
Carvedilol
Alpha/Beta non-selective
CV: HTN, Ischemic heart disease, Chronic heart failure, Arrhythmias Non-CV: Glaucoma, Tremor, Thyrotoxicosis, Cirrhosis, Migrain prophylaxis, Performance anxiety
*Beta-blockers not necessarily interchangeable
doxazosin α1 selective (-osin ending)
Urinary symptoms of BPH; PTSD (prazosin);
Adverse effects: 1st-dose orthostatic hypotension, dizziness, headache
Labetalol
β-blockers
Alpha/Beta non-selective
CV: HTN, Ischemic heart disease, Chronic heart failure, Arrhythmias Non-CV: Glaucoma, Tremor, Thyrotoxicosis, Cirrhosis, Migrain prophylaxis, Performance anxiety
*Beta-blockers not necessarily interchangeable
Metoprolol
β-blockers
Beta 1 selectve (A-BEAM)
CV: HTN, Ischemic heart disease, Chronic heart failure, Arrhythmias Non-CV: Glaucoma, Tremor, Thyrotoxicosis, Cirrhosis, Migrain prophylaxis, Performance anxiety
*Beta-blockers not necessarily interchangeable
Phenyloxbenzamine (α-blockers)
Irreversible. Pheochromocytoma (used preoperatively) to prevent catecholamine (hypertensive) crisis
nebivolol
β-blockers
Phentolamine (α-blockers:nonselective)
Reversible. Give to patients on MAO inhibitors who eat tyramine-containing foods and for severe cocaine-induced hypertension (2nd line)
propranolol
β-blockers
Tamsulosin (α1 selective)
Urinary symptoms of BPH
1st-dose orthostatic hypotension, dizziness, headache
