Autonomic Drugs Flashcards
What is carbachol?
It is a direct agonist of cholinergic receptors (cholinomimetic).
It is a carbon copy of acetylcholine
What is bethanecol?
It is a direct agonist of cholinergic receptors (cholinomimetic)
What is pilocarpine?
It is a direct agonist of cholinergic receptors (cholinomimetic)
What is methacoline?
It is a direct agonist of cholinergic receptors (cholinomimetic)
What does bethanecol do?
Activates bowel and bladder smooth muscle; resistant to AChE
What is bethanecol used for?
Post op ileus
Neurogenic ileus
Atonic bladder
Urinary retention
What is carbachol used for?
Glaucoma
Pupillary contraction
Relief of intraocular pressure
Action: iris moves further from the cornea increasing the angle –> more flow of aqueous humor
What is pilocarpine used for?
Open angle and closed angle glaucoma
How does pilocarpine work?
Contracts ciliary muscle and pupillary sphincter
What is methacoline used for?
Challenge test for the diagnosis of asthma since it stimulates the muscarinic receptors in the airway when they are inhaled
What are the acetylcholinesterases?
Neostigmine Pyridostigmine Edrophonium Physostigmine Donezepil
What is neostigmine used for?
Postoperative and neurogenic ileus
Urinary retention
Myasthenia gravis
Reversal of NMJ blockade postop
What is pyridostigmine used for?
Myasthenia gravis
Longer acting than neostigmine
What is edrophonium used for?
Diagnosis of myasthenia gravis
What is physostigmine used for?
Crosses the bb barrier so used in anticholinergic toxicity (atropine OD)
Also- control hyperthermia if atropine OD
What are the side effects of cholinomimetics?
Lacrimaton, sweating, salivation, incontinence, decrease contractility of the heart, miosis, vasodilation, increase GI motility and secretion.
What can cholinomimetics exacerbate?
COPD
Asthma
Peptic ulcer disease
What do organophosphates do?
Penetrate the bb barrier and Irreversibly inhibit AchE So get DUMBBELSS: Diarrhea Urination Miosis Bradycardia Bronchospasm Excitation of skeletal muscle and CNS Lacrimaton Salivation Sweating
(Ex: parathion)
What is the tx for organophosphate poisoning?
Atropine and pralidoxime
If you treat with only physostigmine the patient will still have muscle paralysis because atropine only works on muscarinic receptors
What are the antimuscarinics?
Atropine Homatropine Tropicamide Benztropine Scopolamine Ipratropium, tiotropium Oxybutynin Glycopyrrolate
What are the toxicities of anti-muscarinics?
Increased body temp due to decreased sweating Rapid pulse Dry mouth Dry, flushed skin Cycloplegia Constipation Disorientation Urinary retention
What is atropine, homatropine, tropicamide used for?
Bradycardia
Eye stuff
What is benztropine used for?
Parkinson’s -decreases muscle tremor
What is scopolamine used for?
Motion sickness
What is ipratropium used for?
COPD, asthma
What is oxybutynin used for?
To reduce urgency in mild cystitis and reduce bladder spasms
What is glycopyrrate used for?
IV pre-op to reduce airway secretions
Oral: to tx peptic ulcer, drooling
What are the sympathomimetics?
Epi, norepinephrine Isoproterenol DA, dobutamine Phenylephrine Albuterol, salmeterol, terbutaline Ritodrine
What is epi used for?
Anaphylaxis
Hypotension
Asthma
Open angle glaucoma
What is norepinephrine used for?
Hypotension
What is isoproterenol used for?
Torsades de pointes
Brandy arrhythmias
Which receptors does dopamine act on?
All of them
What receptors does norepinephrine act on?
Alpha 1
Alpha 2
Beta 1
Acts more on the alphas! Even more than epi - used in hypotension
What receptors does epi act on?
All except D1
Has more effects on betas than alphas - used in anaphylaxis
What receptors does isoproterenol act on?
Betas - used in Bradyarrythmias and torsades
What is dopamine used for?
Increase renal perfusion in shock
Heart failure
What receptor is dobutamine most active on?
Beta 1 - used for heart failure and cardiac stress testing
What is unique about dopamine and dobutamine?
They are inotropic and chronotropic
Inc both contractility and HR
What receptors does phenylephrine act on?
Alphas
Alpha 1 more than alpha 2 - used for hypotension, ocular procedures and rhinitis
What receptors does albuterol, salmeterol, terbutaline act on?
Betas
Beta 2 more than beta 1 - used in asthmatics and COPD
What’s terbutaline used for?
To reduce premature contractions
What receptor does ritodrine act in?
Beta 2 - used for tocolysis
What are the indirect sympathomimetics?
Amphetamine
Cocaine
Ephedrine
How does amphetamine work?
Indirect agonist - releases stored catecholamines
Reverses the DAT
What are amphetamines used in?
Narcolepsy
Obesity
ADD
What is MOA of ephedrine?
Same as amphetamines
What is ephedrine used for?
Nasal decon
Urinary incontinence
Hypotension
What should never be given during a cocaine intoxication?
Beta blockers - causes unopposed alpha 1
Severe hypotension
What are the sympathoplegics?
Centrally acting alpha 2 agonist –> central SNS out flow
Clonidine
Alpha-methyl dopa
What are sympathoplegics used for?
HTN especially with renal disease
No dec in blood flow to kidneys
What is phenoxybenzamine?
Irreversible alpha blocker (non-selective)
What is phenoxybenzamine used for?
Pheochromocytoma before removing the tumor
What are the side effects of phenoxybenzamine?
Orthostatic hypotension
Reflex tachycardia
What is phentolamine?
A reversible alpha blocker (non-selective)
What is phentolamine used for?
People on MAOIs who eat tyramine containing foods
What are the alpha 1 antagonists?
- osin
- ozins
What are prazosin, terazosin, doxazosin, and tamsulosin used for?
HTN
Urinary retention due to BPH
What are the side effects of the -osins?
1st dose orthostatic hypotension*
Dizziness
Headache
What is mirtazapine?
An alpha 2 antagonist
What is mirtazapine used for?
Depression
Inc NE and 5-HT3
What are the side effects of mirtazapine?
Sedation
Increases in serum cholesterol
Increased appetite
What are the beta blockers?
-olol
What is timolol used for?
Glaucoma - decreases the secretion of aqueous humor
What are metoprolol and esmolol used for?
SVT - decreases AV conduction velocity
What are the beta 1 selective antagonists?
A BEAM Acebutalol Betaxolol Esmolol Atenolol Metoprolol
What are the Nonselective beta antagonists?
Propranolol
Timolol
Nadolol
Pindolol
(Please Try Not being (Beta) Picky)
What are the partial beta agonists?
Pindolol
Acebutolol
What is the antidote/tx for beta blocker toxicity?
Glucagon
What is the tx for digitalis toxicity?
Normalize potassium Lidocaine Anti-dig Fab Magnesium = KLAM
What is the tx for iron toxicity?
Deferoxamine
Deferasirox
What is the tx for methemoglobin?
Methylene blue and vitamin C
What is the tx for carbon monoxide poisoning?
100% oxygen
What is the tx for methanol or antifreeze poisoning?
Fomepizole, dialysis
What is the tx for lead poisoning?
CaEDTA, dimercaprol, succimer, penicillamine
What is the tx for mercury, arsenic, gold?
Dimercaprol, succimer
What is the tx for copper, arsenic, gold?
Penicillamine
What is the tx for Cyanide poisoning?
Nitrite+thiosulfate, hydro cobalamin
What is the tx for opioid tox?
Naloxone/naltrexone
What is the tx for TCA poisoning?
NaHCO3
Same as Tx for salicylate tox
What’s the tx for heparin tox?
Protamine
What is the tx for theophylline tox?
Beta-blocker
What are the P450 inducers?
Momma Barb Steals Phen-Phen and Refuses Greasy Carbs Chronically: Modafinil Barbiturates St. John's wort Phenytoin Rifampin Griseofulvin Carbamazepine Chronic alcohol use
What are the P450 inhibitors?
MAGIC RACKS GQ Macrolides Amiodarone Grapefruit juice Isoniazid Cimetidine Ritonavir Acute alcohol abuse Cipro Ketoconazole Gemfibrozil Quinidine
What is the MOA of pralidoxime?
Reactivates cholinesterase by removing the phosphate group that had been added by organophosphates
What are all the effects of phenylephrine?
Increases peripheral vascular resistance
Decreases pulse pressure (due to reflex decrease in stroke volume and increased afterload)
Increases systolic pressure
Decreases heart rate
What does epi do?
Increase pulse and pulse pressure
Decreases peripheral vascular resistance (beta 2)
What are the 2 sympathetic innervations that are cholinergic?
The sweat glands and the adrenal medulla
What are the autonomic receptors that use Gq?
Alpha 1 M1 M3 (increase exocrine glands, lacrimal, gastric acid, gut peristalsis, bladder contraction, bronchoconstriction, miosis, accommodation) H1 V1
What are the autonomic receptors that use Gi?
Alpha 2
M2 (decreases heart rate and contractility of the atria)
D2
What are the autonomic receptors that use Gs?
B1 B2 D1 H2 V2
What is th MOA of pralidoxime?
Reactivates cholinesterase by removing a phosphate group
What is labetolol?
An alpha 1, beta 1, and beta 2 reversible competitive antagonist
What is donepazil?
Indirect cholinergic agonist (inc endogenous ACh)
Treat- Alzheimer’s
Norepinephrine vs isoproterenol
Norepinephrine = a > b activity
- inc both systolic (b1)
- inc diastolic BP (a1)
- reflex bradycardia
Isoproterenol = b > a
- dec systolic (b1)
- dec diastolic (b2)
- reflex tachycardia (b1)
Epi vs phenylephrine responses to alpha-blockade
Before alpha block = both net inc BP (pressor effect)
After alpha block =
- Epi has net depressor effect (hypotension) - bc alpha & b2 action
- phenylephrine levels out BP (no hypotension) - bc pure alpha action
What are the non selective alpha and beta antagonists?
Carvedilol
Labetolol
What is the tx for tPA, streptokinase or urokinase tox?
Aminocaproic acid
What is the tx for warfarin tox?
Vit K
Fresh frozen plasma
What is the tx for amphetamine tox?
NH4Cl
Acidifies the urine
What is the tx for salicylate tox?
NaHCO3
Alkalinizes the urine
Dialysis
What is the tx for actaminophen tox?
N-acetylcysteine
Replenishes glutathione