Term
| what type of receptor stimulation is usually Activation (vasoconstriction, increased heart rate, etc) except in the GI tract |
|
Definition
|
|
Term
| What receptor stimulation is usually inhibitory (vasodilation, bronchiodilation) except in the heart. |
|
Definition
|
|
Term
| The sympathetic nervous system directly influences four major variables: |
|
Definition
| peripheral vascular resistance, heart rate, contractile force, and venous tone. |
|
|
Term
| The parasympathetic nervous system directly influences what variable |
|
Definition
|
|
Term
| these receptors are located on the smooth muscle of the vasculature where when activated cause relaxation of the vessal walls and result in vasodilation. They can also cause decreased activity of the heart and cause glandular secretion. |
|
Definition
|
|
Term
| A direct-acting cholinomimetic drug |
|
Definition
| produces its pharmacological effect by receptor activation. |
|
|
Term
| An indirect-acting choliomimetic drug inhibits |
|
Definition
| acetylcholinesterase, thereby increasing endogenous acetylcholine levels, resulting in increased cholinergic response |
|
|
Term
|
Definition
direct acting agonist
Bethanecol is used mainly to increase the smooth muscle tone of the bladder.
more resistant to cholinesterases than Ach |
|
|
Term
| Carbachol and Pilocarpine |
|
Definition
Direct Agonist
Carbachol and Pilocarpine are used in the treatment of glaucoma. Causes Miosis and a drop in intraocular pressure
resistant to cholinesterase deactivation
Pilocarpin is also used to increase salavation |
|
|
Term
|
Definition
| These effects include CNS stimulation (uncommon with direct-acting agonists). miosis. spasm of accommodation. bronchoconstriction, increased gastro-intestinal and genitourinary smooth muscle activity, increased secretory activity (sweat glands, airway, gastrointestinal tract), and vasodilation. Transient bradycardia occurs, followed by reflex tachycardia if the drug is administered as an intravenous bolus—reflex tachycardia otherwise. |
|
|
Term
| contraindications for cholinergic drugs |
|
Definition
Asthma- increased bronchial constriction
Coronary insufficiency- stimuli of M receptors in Coronary arteries causes vasoconstriction
peptic ulcer disease |
|
|
Term
|
Definition
| Toxic effects include CNS stimulation (including convulsions), ganglionic stimulation, and neuromuscular end plate depolarization leading to fasciculations and paralysis. |
|
|
Term
| An indirect-acting choliomimetic drug MOA |
|
Definition
| These drugs block acetylcholinesterase the enzymatic breakdown of acetylcholine. Increases the amount of acetlycholin in the synaptic spaces |
|
|
Term
Edrophonium
Donepezil
Tacring |
|
Definition
reversible indirect acting cholinergic agonists drugs
Short Acting |
|
|
Term
|
Definition
reversible indirect acting cholinergic agonists drugs
intermediate acting |
|
|
Term
|
Definition
reversible indirect acting cholinergic agonists drugs
Long Acting (Malathion)
Irreversible:
Isoflurophate
Echthiophate |
|
|
Term
|
Definition
| Donepezil was the first of the “new generation” acetylcholinesterase inhibitors (reversible) used for alzheimer’s dementia. It’s major advantage is its once daily dosing schedule. Much better tolerated than Tacrine with no liver toxicities and no liver enzyme monitoring. |
|
|
Term
| Physostigmine Therapeutic uses |
|
Definition
reversible AChE inhibitors
include: 1- treatment of post surgical bladder and GI tract atony. 2-topically in the eye for glaucoma because it allows the aqueous humor to flow out through the canal of Schlemn thus reducing the intraocular pressure . 3- Given by injection to counteract the toxicities associated with overdoses of anticholinergic drugs (atropine, phenothiazines, and tricyclics) |
|
|
Term
|
Definition
| Myasthenia Gravis can be diagnosed using the Tensilon Test, which can also assess the adequacy of treatment with AChE inhibitors. Small doses of edrophonium improve muscle strength in untreated myasthenics or in treated patients in whom AchE inhibition is inadequate. |
|
|
Term
|
Definition
| effects of the anticholinesterases are to inhibit the breakdown of Ach and therefore allow for a higher concentration at the neuromuscular junction for maximal binding and competition with these antibodies for the binding sites. Bladder an GI stimulant |
|
|
Term
|
Definition
used in Myasthenia Gravis reversible AntiAchesterase.
NM blocking agent antidote |
|
|
Term
| Toxicities of AChE inhibiors |
|
Definition
| DUMBELS: Diarrhea, Urination, Miosis, Bronghocnstriction, Excitation(skeletal muscle and CNS), Lacrimation, Salivation, Sweating |
|
|
Term
| Antidote for Covalently bound Organophosphates |
|
Definition
| Administer Atropine parenterally to inhibit muscarinic effects |
|
|
Term
| classes of Cholinergic Antagonists (muscarinic) |
|
Definition
1- Antimuscarinic drugs (Anticholinergic) drugs used mainly in treating GI problems
2- The neuromuscular blocking drugs used to paralyze patients during induction of anesthesia, intubation, and ECT
3. The Ganglionic blocker drugs are not used therapeutically due to the non- specificity and unpredictability of effect. |
|
|
Term
| Atropine and Scopalamine are what type of agents |
|
Definition
| Cholinergic Antagonists- Antimuscarinic agents |
|
|
Term
| Antimuscarinic Agents are used for? |
|
Definition
| Parkinson's diseases, Overactive bladder, Neuroleptic induced drug SEs, COPD, Motion sickness/ nausea, glaucoma |
|
|
Term
|
Definition
| pupil dilation(careful open angle glaucoma) GI antispasmodic, detrusor antispasmotic, bracycardia, antidote for organophosphate poisoning |
|
|
Term
| Anticholinergic Toxicities |
|
Definition
Avoid in the elderly-
Mad as a Hatter (delirious)
Blind as a bat (dilate pupils)
Red as a beet (flushing)
Dry as a bone (Dry Skin)
Hot as a hare (Overheating or hyperthermia) |
|
|
Term
|
Definition
Anticholinergic
Scopolamine (used orally, intravenously, or transdermally) prevents motion sickness by blocking muscarinic receptors in the vestibular system and in the CNS. Scopolamine or atropine is also administered intravenously during spinal anesthesia to prevent bradycardia during surgery, or to prevent the muscarinic effects of AChE inhibitors used to reverse muscle paralysis at the end of surgery. Scopolamine also has amnestic and sedative properties. |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Anticholinergic Bronchodialator Aerosol form |
|
|
Term
|
Definition
| anti spasmodic (overactive bladder) Anticholinergic. |
|
|
Term
|
Definition
| Overactive bladder anticholinergic |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Smooth Muscle, glands, endothelium |
|
|
Term
|
Definition
| Ganglia and Skeletal Muscle |
|
|
Term
|
Definition
| Arteries, eye, nose, uterus |
|
|
Term
|
Definition
| Vasoconstriction, increase peripheral resistance, increase in BP, Mydriasis |
|
|
Term
|
Definition
| presynaptic neurons, veins |
|
|
Term
|
Definition
|
|
Term
|
Definition
inhibition of NE release, inhibition of Ach release
inhibits lipolysis
inhibits insulin release |
|
|
Term
|
Definition
|
|
Term
|
Definition
Bronchodilation, vasodilation (NO release), relax uterine smooth muscle
Stimulate gycogenolysis in liver
stimulate insulin release from pancreas |
|
|
Term
|
Definition
| slow down HR and decrease contractility |
|
|
Term
|
Definition
| vasodilation, increased bowel activity |
|
|
Term
|
Definition
| depolarizes, evokes action potential |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Relax renal vascular smooth muscle |
|
|
Term
|
Definition
| dihydroxyphenylethylamine derivative |
|
|
Term
|
Definition
| Drug that causese vasoconstriction (nasal, ophthalmic, mucosal |
|
|
Term
|
Definition
|
|
Term
| Sympathomimetics: list some catecholamines |
|
Definition
Dopamine, Epinephrine, Isoproterenol, Norepinephrine
Isoproterenol is a synthetic catecholamines. |
|
|
Term
| Sympathomimetics: list some noncatecholamines |
|
Definition
Salmeterol, Terbutaline, Albuterol, Metaproterenol, Isoetharine
These are not metabolized by COMT and some are not by MAO |
|
|
Term
| The endogenous adrenoceptor agonists (Epi, Norepi, Dopamine) are catecholamines and are rapidly metabolized by: |
|
Definition
| COMT (catechol-o-methy-transferase) and MAO (monoamine oxidase) they are inactive when given orally. Catecholamines have a short duration of action bc they are taken up and metabolized quickly |
|
|
Term
| Epinephrin/norepi have a ______ affinity for alpha receptors than does isoproterenol. And Isoproterenol has a ________ for beta receptors than epi and norepi |
|
Definition
|
|
Term
| Alpha 1 receptors are located on _______ membrane sites and when activated cause what? |
|
Definition
| located on effector membranes sites and cause realease of calcium in to the cytosol of the target organ...causing the vasculature of the smooth muscle to contract. vasocostriction |
|
|
Term
| Alpha 2 receptors are located on the _______ membrane and when activated causes? |
|
Definition
| negative feedback regulating the amount of neurotransmitter that is synthesized and released. Initially the norepi binds to the Alpha 1 sites but then when there is a surplus is starts to bind to Alpha 2 |
|
|
Term
| Beta Adrenoceptors have the highest affinity for what catacholamine? |
|
Definition
Isoproterenol then Epi and then Norepi
Both B1 and B2 have equal affinites for Isoproterenol |
|
|
Term
| B1 receptors have ________ affinity for Epi and Norepi |
|
Definition
|
|
Term
| Beta 2 receptors have greater affinity for ________ than _______ |
|
Definition
|
|
Term
| List some Noncatecholamines |
|
Definition
Phenylephrine, ephedrine, amphetamine
longer half-life and greater CNS penetration than catecholamines |
|
|
Term
| Direct acting adrenergic agonists |
|
Definition
| actually replace and/or mimic the ntural catecholamine |
|
|
Term
| Indirect Acting adrenergic agonists |
|
Definition
| stimulate release of NE from the terminal (ex: amphetamines)They are taken up into the terminal and stimulate the release of NE |
|
|
Term
| Mixed Acting adrenergic agonists |
|
Definition
| Can do some of both direct and indirect acting |
|
|
Term
| The prototype Alpha 2 agonist |
|
Definition
Clonidine: has both alpha 2 and 1 agonists properties. The alpha 2 affinity is greatest. At the alpha 2 receptor they prevent the release of NE
Classic treatment for alcholic and drug withdrawal |
|
|
Term
| How does an indirect acting Alpha 2 adrenergic agonist work? |
|
Definition
increases the release of NE causing the Alpha 2 receptor to cause neg feedback.
ex: Amphetamine and Tyramine |
|
|
Term
| Examples of a mixed acting Alpha and Beta adrenergic agonists (direct and indirect) |
|
Definition
| Ephedrine and Metaraminol (aramine) |
|
|
Term
|
Definition
acts on alpha and beta receptors
actions are on beta receptors mostly in heart, vascular and other smooth muscle
Cardiac stimulant
low dose mainly beta:
high dose will start to hit alpha |
|
|
Term
| Norepinephrine is synthesized from? |
|
Definition
DOPA: dihydroxyphenylalanine
stored in vesicles
COMT metabolized
restored or MAO metabolized |
|
|
Term
What is converted to DOPA?
What is DOPA converted into? |
|
Definition
Tyrosine
Dopamine
Dopamine is then acted on to make norepinephrine |
|
|
Term
| NE is converted to what in the adrenal medulla? |
|
Definition
|
|
Term
| When the adrenal Medulla is stimulated what is released at what precentage? |
|
Definition
|
|
Term
| Norephinephrine stimulates what receptors and causes what to happen |
|
Definition
beta 1 and alpha receptors
causes increased total peripheral resistance, increased diastolic pressure at a greater extent than EPI
increases Systolic Bp and Mean arterial pressure |
|
|
Term
| If a large dose of Atropine was given to a patient, and then a moderate dose of NE was injected, would the HR go up or down? consider the effects atropine and baroreceptor and NE on the heart. |
|
Definition
| increase in HR caused by direct cardiac action. |
|
|
Term
Dopamine activates what receptors and causes what?
What happens at high doses? |
|
Definition
beta 1 receptors to increase heart rate and contractility.
activates dopamine receptors in the renal, coronary, splanchnic vessels to reduce arterial resistance and increase blood flow.
High doses it activates Alpha receptors causes vasoconstrict and reflex decreasin HR |
|
|
Term
|
Definition
related to dopamine
Beta 1 selective with no effect on dopamine receptors
increases CO lowers TPR
high dose increases HR and BP
Used for shock and HF |
|
|
Term
| Metaproterenol, Albuterol, Bitolterol, Terbutaline |
|
Definition
more selective Beta 2 agonists that relaxes bronchial smooth muscle with fewr cardiac effects than epinephrine and lasts longer.
Terbutaline used to suppress premature labor |
|
|
Term
|
Definition
| stimulates beta 2 inhibit uterine contractions like terbulaline |
|
|
Term
|
Definition
| symptomatic orthostatic hypotension |
|
|
Term
|
Definition
| beta 1 and alpha agonists to increase HR and BP. Used for acute hypotensive state associated with spinal anesthesia |
|
|
Term
|
Definition
stimulate HR and force of contractility
stimulate renin release |
|
|
Term
|
Definition
| Conversion of the pressor response (typical of large doses of epi) to a blood pressure lowering effect; caused by alpha blockers |
|
|
Term
| intrinsic sympathomimetic |
|
Definition
| Partial agonist action by adrenoceptor blockers; typical of several beta blockers |
|
|
Term
| Mebrane stabilizing activity (MSA): |
|
Definition
| local anestetic action typical of several beta blockers |
|
|
Term
|
Definition
| Hypotesion that is most marked in the upright position; caused by venous polling or inadequate blood volume typical of alpha blockade |
|
|
Term
|
Definition
| tumor that resembles the adrenal medulla consisting of cells that release varying amounts of norepinephrine, epinephrinem or both into the circulation |
|
|
Term
|
Definition
| receptor located on the presynaptic nerve terminal; the receptor modulates transmitter release from the terminal |
|
|
Term
|
Definition
Lowered Peripheral vascular resistance. Lowered blood pressure.
they convert the pressor response of agonists with combined alpha and beta receptor agonist activity to a depressor response. Referred to as epinephrine reversal |
|
|
Term
| Alpha 1-selective (give example) |
|
Definition
|
|
Term
| Prazosin, terazosin, and doxazosin are |
|
Definition
alpha 1 adrenergic blockers. they dilate both arterioles and veins. supine and standing pressure are lowered.
relaxation of bladder neck sphincter muscles
Have little CV activity
used for treatment of benign prostatic hyperplasia |
|
|
Term
|
Definition
| Alpha-1 blocker (flomax) BPH treatment relaxes smooth muschle imporving urine flow. |
|
|
Term
|
Definition
Vasomax- nonselective alpha antagonist
decreases total periferal resistance and BP
clinically used therapy for Pheochromocytosis HTN emergencies(1st line)
increases peripheral vasodilation in Raynaud's,
prevention of dermal necrosis after extravasation of damaging
treatment of erectile dysfunction
blocks vasoconstriction to incerase tissue perfusion in patients with shock |
|
|
Term
|
Definition
binds covalently to the alpha receptor irreversable blockade
Used to treat pheochromocytoma and Hypertensive crisis |
|
|
Term
|
Definition
| Epinephrine has both alpha and beta agonist properties. In the presence of an alpha blocker the pressor effect of epi is bocked |
|
|
Term
Beta Adrenergic Blockers
(antagonist) |
|
Definition
selective High beta 1 affinity
Non selective beta 1 and 2 affinities
do not effect alpha receptors |
|
|
Term
| Adverse effects of beta blockers |
|
Definition
| Brochoconstriction, Arrhythmias, sexual impairment, Metabolic disturbances |
|
|
Term
| Cardioselective Beta Blockers |
|
Definition
Beta 1 cardioselective: used in angina to increase exercise tolerance and in HTN
Acebutalol, Atenolol, betaxolol, metoprolol (lopressor) |
|
|
Term
| Non-cardioselective Beta antagonist |
|
Definition
| Timolol: treates elevated IOP, HTN angina |
|
|
Term
|
Definition
block beta 1 and beta 2 adrenoceptors
Sotalol, propranolol, carteolol, penbutolol, nadalol |
|
|
Term
|
Definition
Coreg
alpha-beta adrenergic blocker
side effects: orthostasis and bradycardia
used for HTN |
|
|
Term
| Skeletal muscles are innervated by somatic motor nerves that originate in the spinal cord, terminate at muscle cells, and release what neurotransmitter at this synapse |
|
Definition
|
|
Term
| What type of receptor is located on muscle cell membrane |
|
Definition
|
|
Term
| When a drug is an agonist what does this mean? |
|
Definition
| The drug facilitates or mimics the action of the endogenous neurotransmitter |
|
|
Term
| When a drug is an antagonist what does that mean |
|
Definition
| The drug blocks or reduces the action of the endogenous neurotransmitter |
|
|
Term
| What is the only clinically used depolarizing agent? |
|
Definition
|
|
Term
| What is Succinylchline used for |
|
Definition
| Produce muscle paralysis for surgical procedures |
|
|
Term
| How can the blockade of non depolarizing agents be reversed. |
|
Definition
| administer AchE inhibitors in order to increase the concentration of Ach in the synaptic cleft |
|
|
Term
| What are the side effects of anticholinergic drugs? |
|
Definition
| Tachycardia, xerostomia, decreased persperation, mydriasis, urinary retention, decreased gatric secretions |
|
|
Term
| GABA is what type of neurotransmitter |
|
Definition
|
|
Term
Centrally Acting Skeletal muscle relaxants:
name a few |
|
Definition
Dantrolene, Baclofen, Diazepen (Vaium), Tizanidine
treat neurological disorders |
|
|
Term
| What effects will an alpha blocker have on the hemodynamic responses to epinephrine? |
|
Definition
| lower blood pressure by arteriol dilation mediated by antagonism of post-synaptic alpha-1 adrenergic receptors. epinephrine also has vasodilator properties allowing beta activity to manifest with an alpha blocker |
|
|
Term
| Compare pk of propranolol, atenolol, esmolol, and nadolol |
|
Definition
atenolol beta1 selective, renal elim
esmolol- red blood cell
nadolol-renal
propranolol- hepatic |
|
|
Term
| Dialation of vessels in muscle, constriction of cutaneous vessels, and positive inotropic (hr) and chronotropic (contractility) effects on the heart are all actions of? |
|
Definition
|
|
Term
| A long acting indirect sympathomimetic agent which has sometimes been used by the oral route for significant bed wetting in young children |
|
Definition
|
|
Term
| When pupillary dilation but not cycloplegia (paralysis of ciliary muscles) is desired a good choice would be? |
|
Definition
phenylephrine
mainly alpha-1 agonist |
|
|
Term
| When a moderate pressor dose of Norepi is given after pretreatment with a large dose of atropine, which of the folowing is the most probable response to the norepi |
|
Definition
| An increase in HR caused by direct cardiac action: Atropine will prevent the normal reflex bradycardia since that requires integrity of the vagal pathway. The direct action of Norepi on the SA node will be masked |
|
|
Term
Which of the following may stimulate the CNS
antimucarinic drugs , sympathomimetic drugs |
|
Definition
both
amphetamines stimulate CNS
and antimuscarinic agents are capable of inducing hallucinations and convulsions |
|
|
Term
| Beta2 selective stimulants are often effective in treating? |
|
Definition
|
|
Term
| Beta 2 stimulants frequently cause? |
|
Definition
|
|
Term
| Stimulation of Renin is primarily a Beta what response |
|
Definition
|
|
Term
| sympathomimetic at low doses increases renal blood flow |
|
Definition
|
|
Term
| pure alpha adrenergic agonist |
|
Definition
|
|
Term
| Contraindicated in patients using MAO inhibitors |
|
Definition
| tyramine containing foods |
|
|
Term
| centrally acting, reduces sympathetic outflow |
|
Definition
|
|
Term
| what drug causes constriction of vessels in the nasal mucosa |
|
Definition
|
|
Term
| If you give Isoproternol to normal subjects what happens to the systolic and diastolic pressures |
|
Definition
systolic remains constant and diastolic decreases
the decrease in diastolic is from the decreased in vascular resistance and it increases pulse pressure |
|
|
Term
| If you give Norepi to a normal subject what happens to the systolic and diastolic pressure |
|
Definition
|
|
Term
| marked increases in diastolic pressure can suggest what type of receptor activation |
|
Definition
|
|
Term
| an increase in pulse pressure is a sign of what type of receptor activation |
|
Definition
| Beta receptor _ contractility |
|
|
Term
| with phenylephrine use in patients what type of response will you see with BP, Cardiac output and Heart Rate |
|
Definition
increase in systolic and diastolic BP, decrease in CO and HR
Strong alpha very little to no beta effect |
|
|
Term
Both phentolamine and phenoxybenzamine: cause hypertension or hypotenstion?
what else can result from this effect |
|
Definition
| hypotenstion that then leads to reflex tachycardia |
|
|
Term
| Beta blockers can exacerbate what disease? |
|
Definition
|
|
Term
| Name a adrenergic antagonist that will decrease blood pressure and cardiac output |
|
Definition
| Labetalol or Carvedilol because they block Beta and alpha receptors Mixed action |
|
|
Term
| Beta blockers like Atenolol are used to treat HTN but a common side effect is? |
|
Definition
| fatigue and exercise intolerance |
|
|
Term
if your patient is in acute heart failure and you want to improve is cardiac function but not significantly increase his Heart rate what adrenergic drug would be best:
Epi, Norepi, phenylephrine, dobutamine |
|
Definition
| Dobutamine: increases cardiac output Beta-1 and does not significantly increase Heart rate |
|
|
Term
Which of the following drugs when administered IV can decrease blood flow to the skin, increase blood flow to skeletal muscle, and increase the force and rate of cardiac output?
epinephrine, isoproterenol, norepi, phenylephrine, terbutaline. |
|
Definition
| Epinephrine- stimulates alpha and beta equally |
|
|
Term
| Mydriasis is in response to what type of receptor activation |
|
Definition
|
|
Term
Which of the following may precipitate an attack of Open angle glaucoma if instilled in the eyes?
physostigmine, Atropine, pilocarpine, echothiophate |
|
Definition
| Atropine: mydriatic effect that can result in narrowing of the canal of schlemm increase IOP |
|
|
Term
patient is confused, HR 45, blood pressure low, sweating, salivating: which treatment would you give him?
Physostigmine, Norepi, atropine |
|
Definition
| atropine (anticholinergic) |
|
|
