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How does botulinum toxin work?

Botulinum toxin prevents the release of neurotransmitter at all cholinergic terminals.

What are the major effects of 1-receptor activation?


1-Receptor activation increases vascular smooth muscle contraction, as well as pupillary dilator
muscle contraction ,mydriasis.

What are the major functions of 2-receptor activation?


2-Receptor activation decreases sympathetic outflow and insulin release.

What are the major functions of 1-receptor activation?


1-Receptor activation increases the following: heart rate and contractility; release from the kidneys; and lipolysis of adipose tissue.

What is the major effect of 2-receptor activation on the body's vasculature? What is the effect on the respiratory system?
Vasodilation; bronchodilation.

How does 2-receptor activation affect glucagon release?


2-Receptor activation increases glucagon release.

Name five indirect cholinergic agonists


Neostigmine, pyridostigmine, edrophonium, physostigmine, and echothiophate.

What symptoms are likely in patients taking cholinomimetic agents?


Exacerbation of COPD, asthma, and peptic ulcers.

Which pharmacologic agent is used to treat atropine overdose?


Physostigmine. It crosses the blood-brain barrier and is able to reverse effects on the CNS and the peripheral nervous system.

What is a methacholine challenge test?


A test in which methacholine is inhaled to stimulate muscarinic receptors and induce broncho- constriction. The test is used to diagnose asthma.

A farmer presents with diarrhea, abdominal pain, wheezing, pinpoint pupils, copious tears, and
salivation. What medications should be prescribed?
This patient has the classic signs of organophosphate poisoning, which is treated with atropine and pralidoxime.

Why is pyridostigmine used to treat myasthenia gravis?


Pyridostigmine increases the amount of acetylcholine in the neuromuscular synapse, thereby increasing muscle strength.

A patient recently began taking haloperidol to treat schizophrenia, but visits his physician because of new-onset Parkinson's-like motor symptoms.
What drug could be used to treat these symptoms?
Benztropine.

What are the two effects of atropine on the eye?


Pupil dilation and cycloplegia.

True or False: Diarrhea is a sign of atropine toxicity.


False. Constipation is a sign of atropine toxicity.

Low doses of epinephrine are selective for _______ (1, 2, 1, 2) adrenergic receptors.
1.

Isoproterenol is an agonist for which receptors?


1 and 2 (equally).

Dopamine __________ (is/is not) ionotropic and __________ (is/is not) chronotropic, whereas dobutamine __________ (is/is not) ionotropic and
__________ (is/is not) chronotropic.
Dopamine is ionotropic and chronotropic; dobutamine is ionotropic but is not chronotropic.

What are the clinical applications of epinephrine?


Anaphylaxis, open-angle glaucoma, asthma, and hypotension.

What role does dopamine have in treating shock?


Dopamine increases blood pressure while maintaining renal perfusion.

What are the clinical applications of phenylephrine?


Phenylephrine treats nasal decongestion, causes vasoconstriction, and dilates pupils.


What is the clinical application for albuterol?
Acute asthma.

Which sympathomimetics can reduce premature uterine contractions?


Terbutaline and salmeterol.

What effect does isoproterenol have on pulse pressure and heart rate?
Isoproterenol increases pulse pressure and heart rate.

What is the effect of clonidine on central adrenergic outflow? On which receptor does it act?
Clonidine is an 2-agonist that decreases central adrenergic outflow. Remember: the 2-receptor is responsible for negative feedback.

What is the clinical application and mechanism of action of phentolamine?


Phentolamine is a nonselective -blocker used to treat pheochromocytoma.

What is the net effect of epinephrine on blood pressure before and after nonselective -blockade?
Why?
Before -blockade, epinephrine increases blood pressure. After -blockade, it decreases blood pressure. This is because epinephrine also activates 2,
which lowers blood pressure and is not blocked.

A 63-year-old man is referred long-term care after his first myocardial infarction. Is a -blocker suggested or contraindicated for this patient? Why?
Suggested. After myocardial infarction, patients should receive -blockers to decrease risk of mortality.

How do -blockers work in the setting of angina pectoris?


They decrease heart rate and contractility as well as myocardial oxygen consumption.

Which -blockers have partial agonist activity?


Pindolol and acebutolol. Remember: PA = Partial Agonist

Name two nonselective - and -antagonists.


Carvedilol and labetalol.

name the two types of Ach receptors


Nicotinic ACh receptors and Muscarinic ACh receptors

Nicotinic ACh receptors are


ligand-gated Na+/K+ channels

Muscarinic ACh receptors are


G-protein-coupled receptors that act through 2nd messengers;
5 subtypes: M1, M2, M3, M4, and M5.

name Sympathetic receptors


1, 2, 1, 2

name para- Sympathetic receptors


M1 M2 M3

mnemonic for F protein class receptors


"Qiss (kiss) and qiq (kick) till you're siq (sick) of sqs (sex) ."

name the receptor: Increase vascular smooth muscle contraction, Increase pupillary dilator muscle contraction (mydriasis), Increase intestinal and
bladder sphincter muscle contraction
1

name the receptor: decreases sympathetic outflow


a2

name the receptor: decreases insulin release


a2

name the receptor: increases renin release


b1

name the receptor: Vasodilation, bronchodilation

b2

name the receptor: insulin release


b2

name the receptor: decreases uterine tone


b2

name the receptor:CNS, enteric nervous system


m1

name the receptor: decreases heart rate and contractility of atria


m2

name the receptor: increases exocrine gland secretions (e.g., sweat, gastric acid)
M3

name the receptor:bronchoconstriction


m3

name the receptor:I pupillary sphincter muscle contraction (miosis)


m3

name the receptor: Relaxes renal vascular smooth muscle


d1

name the receptor: Modulates transmitter release, especially in brain


d2

name the receptor: increases nasal and bronchial mucus production, contraction ofbronchioles, pruritus, and pain
h1

name the receptor: increases gastric acid secretion


h2

name the receptor: increases H20 permeability and reabsorption in the collecting tubules of the kidney
v2

name the receptors: increases lipolysis


b1 b2

Protein kinase A does what two things


1) increase [Ca2+] (heart)
2) block Myosin light-chain
kinase (smooth muscle)

name the receptor: Phospholipase C


Gq

name the two types of Cholinomimetic agents


Direct agonists and Indirect agonists anticholinesterases

used 4 Postoperative and neurogenic ileus and urinary


retention
Bethanechol

used for Glaucoma, pupillary contraction, and relief of


intraocular pressure
Carbachol

Potent stimulator of sweat, tears, saliva


Pilocarpine

Challenge test for diagnosis of asthma and MOA?


Methacholine:Stimulates muscarinic receptors in airway when inhaled.

drugs for myasthenia gravis


Neostigmine,Pyridostigmine,Edrophonium

DUMBBELSS
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation ofskeletal muscle and CNS, Lacrimation, Sweating, and Salivation.

Muscarinic antagonists drugs for Peptic ulcer treatment name 3 of them


Methscopolamine, pirenzepine, propantheline

Muscarinic antagonists drugs to Reduce urgency in mild cystitis and reduce


bladder spasms treatment name 2 of them
Oxybutynin, glycopyrrolate

Muscarinic antagonists drug for Asthma, COPD


lpratropium

Muscarinic antagonists drug for Motion sickness


Scopolamine

Muscarinic antagonists drug for PARKinson's disease


Benztropine

Muscarinic antagonists drugs used for: Produce mydriasis and cycloplegia name three of them
Atropine, homatropine, tropicamide

tropicamide
Muscarinic antagonists drugs used for: Produce mydriasis and cycloplegia

homatropine
Muscarinic antagonists drugs used for: Produce mydriasis and cycloplegia

Atropine
Muscarinic antagonists drugs used for: Produce mydriasis and cycloplegia

Benztropine
Muscarinic antagonists drug for PARKinson's disease

Scopolamine
Muscarinic antagonists drug for Motion sickness

propantheline
Muscarinic antagonists drugs for Peptic ulcer treatment

pirenzepine
Muscarinic antagonists drugs for Peptic ulcer treatment

Methscopolamine
Muscarinic antagonists drugs for Peptic ulcer treatment

Oxybutynin
Muscarinic antagonists drugs to Reduce urgency in mild cystitis and reduce
bladder spasms

glycopyrrolate
Muscarinic antagonists drugs to Reduce urgency in mild cystitis and reduce
bladder spasms

name the two types of Sympathomimetics


Direct sympathomimetics, Indirect sympathomimetics

used 4 Anaphylaxis, glaucoma (open angle), asthma, hypotension


Epinephrine

Epinephrine used for ?


used 4 Anaphylaxis, glaucoma (open angle), asthma, hypotension

Norepinephrine used for ?


Hypotension (but decreases, renal perfusion)

Isoproterenol used for ?


AV block (rare)

Dopamine used for ?


Shock (renal perfusion), heart failure , inotropic and chronotropic; D1 > b> a

Dobutamine used for


Heart failure, cardiac stress testing; inotropic,
but not chronotropic

Phenylephrine used for


Pupillary dilation, vasoconstriction, nasal decongestion

MOA of Clonidine
Centrally acting a2-agonists, decreases adrenergic outflow

MOA of a-methydopa
Centrally acting a2-agonists, decreases adrenergic outflow

Mirtazapine MOA
a2blocker

which class of drugs are for Hypertension, urinary retention in BPH


a1blockers (-zosin ending)

doxazosin MOA
a1 blocker

Give to patients on MAO inhibitors who eat


tyramine-containing foods
Phentolamine alpha nonselective blocker

Nonselective alpha blockers?


Phenoxybenzamine and Phentolamine

a1 selective blockers are used for


Hypertension, urinary retention in BPH

alpha2 selective blocker used for


Depression Mirtazapine

mnemonic for the list of all the b1-selective antagonists


a-m

mnemonic for the list of all the Nonselective antagonists


n-z

carvedilol, labetalol are?


Nonselective (vasodilatory) a- and b-antagonists

is it better to give a diabetic patient beta 1 blocker /beta2 blocker/ or nonselective beta blocker
nonselective mask the adrenergic system so give beta 1, which is better

mnemonic for the receptors


alpha beta males don't have vaginas
A1A2B1B2M1M2M3D1D2H1H2V1V2

promethazine
1st generation H1 receptor antagonist

dipenhydramine
1st generation H1 receptor antagonist

chlorpheniramine
1st generation H1 receptor antagonist

hydroxyzine
1st generation H1 receptor antagonist

fexofenadine
2nd generation H1 receptor antagonist

loratadine
2nd generation H1 receptor antagonist

desloratadine
2nd generation H1 receptor antagonist

cetirizine
2nd generation H1 receptor antagonist

insulin acts on which receptor


tyrosine kinase > protein phosphates > dephorylates glycogen syntase >glycogen synthesis

Where in the presynapts does Ca+ work


just before the release of Ach or Ne

where does vesmicol which in the presynapts


inhibits making the vesicle Ach

where does reserpine work


inhibits just before making the vesicle in NE

where does Guanethidine work and do


stops NE release

what is the MOA of amphetamines


increase release of NE and blocks the reuptake of NE

why is pralidoxime given with atropine


you want to simulate both the M and N receptors, atropine only reverses the M receptors so pralidoxime also prevents N effects such as Muscle
paralysis "restores/ regenterates cholinererase

what is the tx for jimson weed poisoning "gardeners mydriasis


physostigmine not atropine

what is the tx for medicated induced parkinsonism


benztropine

name one SE of first generation H1 blocker


antimuscarinic

SE of Mirtazapine
sedation, increase serum cholesterol, increase appetite, increase weight gain. good for a sad anorexic

what drug is presently the 1st line medication for the tx of essential HTN in the general population
hydrocholorothiazide

doxazosin is used for


tx of both BPH and HTN

prazosin is used for


tx of both BPH and HTN

terazosin is used for


tx of both BPH and HTN

pt with coronary artery disease and heart failure along with HTN will benefit from ?
beta blockers

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