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181 Cards in this Set
- Front
- Back
- 3rd side (hint)
Central NS includes?
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Brain, spinal cord and pre-ganglionic neurons.
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Centrally acting drugs affect?
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the brain - makes you drowsy
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PNS includes
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ganglion and post-ganglionic neurons
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Clonidine
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Alpha 1 Agonist
Hypertension (pre-ganglionic)>> centrally acting drug. Makes you drowsy. ADR=Rebound HTN |
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Periphery acting drugs
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don’t make you drowsy.
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Drugs can work at
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1) Axon (only local anesthetics)
2) Or synapse (gap) 3) One nerve to another 4) Direct to muscle (terminal) Somatic). |
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Neurotransmitters are made of
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protein and glucose, metabolized in Krebs cycle
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ACh
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Acetalcholine (comes from AcetylCoA)
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Drugs that compete w/binding site
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Competitive antagonist
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Steps in Nerve transmission
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1.Synthesis of NT
2.Storage of NT (in nerve endings) most of the time 3.Binding receptor (to match) 4.Action happens 5.Termination (all are degraded) |
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PNS subdivisions
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1) Autonomic NS
2) Somatic NS |
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Autonomic subdivisions
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1.Parasympathetic
2.Sympathetic |
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Axonal conduction
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ONly local anesthetics
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Synaptic conduction
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can be selective, influences a specific type of NT
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Receptors
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has abilitity to influence behavior of another cell, ultimately depends on ability of that neuron to alter receptor activity on target cell
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Neoropharmacology
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Study of drugs that alter processes controlled by Nervous System
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Brain Stem
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Midbrain
Pons Medulla |
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Forebrain
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cerebrum. Includes Thalamus
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Somatic NS
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Voluntary activity: Skeletal muscle contraction
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Sympathetic NS
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Adrenergic
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Parasympathetic NS
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Cholinergic
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Automonic NS functions:
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1. regulation of heart
2. Regulation of secretory glands 3. regulation of smooth muscles ex: urogenitcal muscles, git, blood vessels. |
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Innervation of SNS and PNS.
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(generally) opposing action
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Exception to opposing action of dual innervation SNS/PNS
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Heart rate and dec. HR. Except in blood vessels. Only sympathetic effect.
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Complementary innervation SNS/PNS
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SNS-causes ejaculation
PNS-erection in repro. organs |
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Neurotransmitters in PNS
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1. Epinephrine - (Epi) most from adrenal medulla
2. Norepinephrine (NE) released in POSTganglionic neurons of the SNS. 3. ACh 4. Dopamine - most junctions in PNS. |
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Forebrain
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memory learning
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Temporal
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speech, hearing
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Optic nerve
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decussation ends in occipital lobe vision
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Sympathetic NT =
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epinephrine and norepinephrine (Adrenergic)
-adrenergic stimulant = sympathetic stimulant |
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Effects of sympathetic (adrenergic agonist)
similar to "fight or flight" |
Eye=Pupil dilates=Far vision
Heart=Increased contractility=Pumps faster, HR goes up Lungs=Bronchials dilate( Need more air to breath Coronary Arteries=dilate=Increase blood flow to heart. Increased nutrients. GI=Slows motility=No food digestion Glucose=Glycogenolysis=More fuel/sugar Urinary= Detrussor(relax) + Sphincter constricts=No pee pee. Skeletal Muscles=Contract=RUN Peripheral blood vessels=Constrict=BP up Alimentary (poop)=colon GI relax=Sphincter (Constrict)No poop |
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Adrenergic agonists/sympathetic agonists
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Non-selective: direct action: Epinephrine and Norepineprhine, Isoproterenol
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1-Epiniphrine Tx for
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1-anaphylactic shock Subq 0.1 ml of 1:1000 PRN acts in 20 min.
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2-Epiniphrine Tx for
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2-Cardiac resuscitation: 1:1000 IV (1mg/ml) acts 5-10 min) can be diluted in 10 ml saline
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3-Epiniphrine Tx for
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3-Allergic rxn (bee sting etc).
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4-Epiniphrine Tx for
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4-Bronchospasm
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Indirect acting sympathetic NT (adrenergic agonist). Stimulates the RELEASE of NE
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Amphetamines (Tx ADHD - improves motor tasks and Narcolepsy)
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Mixed acting sympathetic NT (adrenergic agonist).Stimulates the receptors AND release
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Ephedrine. Stimulates adrenergic receptors AND stimulates release of NE.
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CAUTIONS for using sympathetic agonists
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HTN: HR goes too high. Prostatic hypertrophy: because constricts sphincter (can't pee pee).
Cardiac arrythmias. |
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More CAUTIONS for using sympathetic agonists
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Check vital signs q3-5 minutes incl. BP and HR. Check IV site can cause tissue necrosis. check blood sugar (since glycogenolysis is increased)
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More CAUTIONS for using sympathetic agonists
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Peudoephedrine (Sudafed, Pedia care, Co-tylenol) are alpha 1 and beta 1 agonists. Tx for nasal congestion. Do not give with cardiac, HTN.
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Alpha2 agonist
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Clonidine (catapres) and Methyldopa (aldomet) Tx HTN
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Caution for Alpha2 agonist
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Rebound HTN (if withdrawn abruptly)
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Beta 2 selective agonist
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Inhalders (relax bronchials) dilaation.
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Examples of Beta 2 SELECTIVE agonist
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Terbutaline (bricanyl)
Levalbuterol (Xopenex) Albuterol (ventolin) Salmetrerol (Serevent) |
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Beta 1 and Beta 2 NON-SELECTIVE agonist
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Metaproterenol (alupent)
Isoproterenol (Isuprel) Ritodrine (Yutopar) |
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Alpha 1 antagonist Tx for HTN
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Prazocin (minipres)
Doxazocin (cardura) Phentolamine (regitine) used for dopamine infiltration, hypertensive emergcency. T 1/2 = 20 min. |
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Tamsulosin-What kind of receptor?
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Selective Alpha 1 (peripheral) Antagonist.
Tx BPH Do not drive or operate machinery after 1st dose (b/c Alpha 1 dilates eyes) blurry vision |
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Tamsulosin- TX for
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Indications
Management of outflow obstruction in male patients with prostatic hyperplasia |
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Tamsulosin-method of action
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Decreases contractions in smooth muscle of the prostatic capsule by preferentially binding to alpha1-adrenergic receptors
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Indirect acting sympathetic NT (adrenergic agonist). Stimulates the RELEASE of NE
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Amphetamines (Tx ADHD - improves motor tasks and Narcolepsy)
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Alpha 1 (action of stimulation)
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Blood vessels=Vaso-constrict
Eyes=Dilates Bladder=contraction (sphincter) Prostrate=contraction |
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Mixed acting sympathetic NT (adrenergic agonist).Stimulates the receptors AND release
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Ephedrine. Stimulates adrenergic receptors AND stimulates release of NE.
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CAUTIONS for using sympathetic agonists
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HTN: HR goes too high. Prostatic hypertrophy: because constricts sphincter (can't pee pee).
Cardiac arrythmias. |
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Alpha 2 (action of stimulation)
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Located on nerve terminals. Presynaptic or prejunctional. Regulate NT release. NE can bind to A-2 (on same neuron that (NE was released)>> suppression of further NE release. REDUCE NE.
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More CAUTIONS for using sympathetic agonists
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Check vital signs q3-5 minutes incl. BP and HR. Check IV site can cause tissue necrosis. check blood sugar (since glycogenolysis is increased)
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More CAUTIONS for using sympathetic agonists
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Peudoephedrine (Sudafed, Pedia care, Co-tylenol) are alpha 1 and beta 1 agonists. Tx for nasal congestion. Do not give with cardiac, HTN.
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Beta 1 (action of stimulation)
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Heart=increase HR; Increase force of contraction; Increase AV velocity
Kidney=increase Renin> vasoconstriction>BP up |
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Alpha2 agonist
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Clonidine (catapres) and Methyldopa (aldomet) Tx HTN
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Caution for Alpha2 agonist
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Rebound HTN (if withdrawn abruptly)
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Beta 2 (action of stimulation)
Affects the... |
Arterioles, Heart, Lung, Skeletal muscles=Dilation
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Beta 2 selective agonist
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Inhalders (relax bronchials) dilaation.
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Examples of Beta 2 SELECTIVE agonist
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Terbutaline (bricanyl)
Levalbuterol (Xopenex) Albuterol (ventolin) Salmetrerol (Serevent) 1st choice for COPD b/c less ADRs assoc. w/Beta 1's & HTN. |
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Beta 2 (action of stimulation)
Affects the... |
Lungs=Bronchodilation (Albuterol)
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Beta 1 and Beta 2 NON-SELECTIVE agonist
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Metaproterenol* (alupent) COPD
Isoproterenol* (Isuprel) COPD Ritodrine (Yutopar) Relax uterus. For premature labor (Bronchospasm treatment) DO NOT GIVE TO PATIENT W/HTN B/C NOT SELECTIVE AND *AFFECTS B1- WHICH BP GOES UP. But is more selective for Beta-2. |
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Beta 2 (action of stimulation)
Affects the... |
GI Tract=increases GI motility
Uterus=Relaxation Liver=Glycogenolysis Skeletal muscle=Enhanced contraction, glycogenolysis |
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Beta 2 is like... (my words)
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Giving birth. uterus relaxes, other muscles contract, more blood sugar, lungs breath better. All blood vessels dilate to lower BP
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Beta 1 is like (my words)
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"you betta renin" faster b/c your HR is up and BP is up from renin in kidneys.
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Alpha 2- is like (my words)
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The great inhibitor. Opposite to the Alpha male type.
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Alpha 1- is like (my words)Like the Alpha male, dominant and aggressive
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dilated pupils, High BP (from constriction), can't pee but can ejaculate
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Peripheral Adrenergic Receptor Subtypes
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Alpha 1
Alpha 2 Beta 1 Beta 2 |
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Non-selective Alpha 1, B1 and B2 blockers ANTAGONISTS
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Carvedilol (Coreg) Tx HTN mild to mod. heart failure
Labetalol (trandate) doing surgery. |
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Non-Selective Beta Blockers CANNOT BE USE FOR...
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asthmatic patients b/c can cause brochoconstriction.
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Nursing checks for Non-selective Alpha 1, B1 and B2 blockers.
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low BP and HR and wheezing.
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Nonselective B1 and B2 ANTAGONIST
Hint >N (in alphabet) |
Propanolol (interal) tx HTN, supraventricular tachycardia
Pindolol (visken) Timolol (opthalmic ointment, tx for IOP. Sotalol (betapace) (Do not use w/Asthma, Rebound HTN). Nadolol (corgard) |
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Contraindication of NON-SELECTIVE B1 and B2 ANTAGONIST
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1) asthmatic patients b/c can cause brochoconstriction.
2) rebound HTN 3) Sedation |
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SELECTIVE B1 ANTAGONIST
Tx HTN |
Metoprolol (lopressor)
Atenolol (Tenormine) Esmolol Betaxolol (decreases BP, and MI/agina, also used for CHF) Acebutolol |
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Glucagon counteracts the effect of sympatholytic effect of...
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beta blockers
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Cholinergic agonists or parasympathomimetics
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Direct acting Cholinergic agonists: Acethylcholine
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Direct acting Cholinergic agonists
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Bethanicol (urecholine)
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Muscarinic agonists
“HESE” mimics ACh |
bethanechol:
1.Heart-down 2.Exocrine glands-gland secretion up 3.Smooth muscles-smooth muscle contract 4.Eye-pupils constrict/lens curves-near vision HESE - PNS |
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Muscarinic ANTagonists
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Atropine=
1.Heart-up 2.Exocrine glands-gland secretion dwn 3.Smooth muscles-relax 4.Eye-pupils dilate far vision |
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Ganglionic stimulating agents
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nicotine-Promotes ganglionic transmission
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Ganglionic blocking agents
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mecamylamin-Blocks ganglionic transmission
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Neuromuscular blocking agents
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d-Tubocurarine, succinylcholine. Blocks Skeletal muscle contraction
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Cholinesterase inhibitors
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increases activation @ ALL cholinergic receptors by inhibiting cholinsterase (which would degrade ACh) so it keeps ACh in the synapse and working.
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Bethanacol is a selective agonist @ muscarinic cholinergic Rxns. Predict it's actions: (Caution w/Asthma b/c bronchoconstriction)
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1.Muscarinic receptors: ocular effects (miosis and ciliary muscle contraction)
2.Slow heart rate 3.Bronchial constriction 4.Urination 5.Glandular secretion 6.Stimulation of GI tract 7.Penile erection 8.vasodilation |
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Muscarinic Agonists
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Cause receptor activation:
1. Heart 2. Exocrine glands 3. Smooth muscles (lung and GI tract) 4. Eye |
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Muscarinic Agonists (also called Cholinergic)
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Heart-Bradycardia
Exocrine glands-increase sweating, glands -secrete>saliva, bronchial secretion and gastric acid Smooth muscles>(lung and GI tract)>contraction Eye>Miosis, ciliary muscle contracts Bladder>Pee pee |
All parasympathetic target organs.
1. Eye-constrict 2.Heart-slows 3.Lung-constriction 4.Bladder-relax sphincter, contstrict trigone=pee pee 5. GI tract-constriction 6. Sweat Glands-more secretion 7. Sex organs-more secretion 8.Blood vessels-dilates BP down |
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Muscarinic (cholinergic) Agonists affects on eye
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Eye-Miosis, ciliary muscle contract>>Pupils constrict, accommodation for near vision.
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Muscarinic (cholinergic) Agonists affects on smooth muscles
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Smooth muscles
(lung and GI tract)>contraction>>tone and motility of GI tract (up), bladder emptying>>Vasodilation - BP down |
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Muscarinic (cholinergic) Agonists
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Resemble stimulation of PS nerve. Also known as PS mimetic agents
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Bethanacol
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-Direct acting muscarinic agonist.
-Bind irreversibly to muscarinic cholinergic receptors causes activation Has little or no effect on nicotinic receptors or ganglia or skeletal muscle. |
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Pharmacological effect-Bethanacol
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Purpose: alleviates urinary retention (stimulates bladder to empty). By relaxing trigone and sphincter muscles.
Also used to treat GI reflux. Increased GI motility and GI paralysis (but NOT w/obstruction) |
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Bethanacol- CONTRAINDICATED
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If blockage b/c muscles contract but pee pee can’t come out. Also for asthma, hypotension, coronary insufficiency and hyperthyroidism.
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Bethanacol- Assessments
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Assess – I&O
Patient teaching: take 1 hour BEFORE or 2 hours AFTER meals to reduce GI upset. |
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Bethanocol-OVERDOSE:
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S&S- bradycardia. Atropine (muscarinic antagonist)
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Toxicology of Muscarinic Agonists- Inocybe and Cilocybe (lots of muscarine)
(Cholinesterase inhibitors) |
Symptoms:
Excessive activation of muscarinic receptors. Profuse salivation, lacrimation (tears), visual disturbances, bronchospams, diarrhea |
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Muscarinic Antagonists
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Anticholinergic Drugs= less ACH. Muscles relax.
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Muscarinic Antagonists-Anticholinergic Drugs
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Produce receptor blockade of ACH at muscarinic receptors. Also known as:
-parasympatholytic drugs -Antimuscarinic, muscarinic blockers -anticholinergic drugs – ONLY @ muscarinic receptors NOT ALL cholinergic receptors. |
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Muscarinic Antagonists-Anticholinergic Drugs Example
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Atropine. Used for pre-op to dec. salv. secretions, dilate pupils, relax smooth muscle. Also to treat bradycardia b/c BP goes up when ACH is blocked.
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Muscarinic Antagonists-Anticholinergic Drugs Effects
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Heart-HR up
Exocrine-salivation (Xerostomia) - down Hyperthermia smooth muscles bronchi (down) tone in bladder (down) eye-mydriasis (dialates pupil) (far vision) mild CNS excitation TOO MUCH hallucinations/delirium, coma, rep. arrest, death |
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Muscarinic Antagonists-Anticholinergic Drugs Effects @low dose
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Can be blocked at some sites w/low dose
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Muscarinic Antagonists-Anticholinergic Drugs Effects
@ high dose |
-more for stomach blockade.
-If give enough for effect, will also cause affects in heart, exocrine glands, smooth muscle and eye. |
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Drug interactions: Some other drugs (not muscarinic antagonists)
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can also produce blockade (have anti-cholinergic actions). They can enhance effects of atropine and related agents. Avoid use w/atropine, makes effect too strong.
1.Antihistamines 2.Phenothiazine antipsychotics 3.Tricyclic antidepressants |
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Anticholinergic drugs for Overactive bladder (Urge incontinence) (OAB).
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Four symptoms:
1. Urinary urgency (have to go). 2. frequency (> 8x/24 hours) 3. Nocturia (waking 2+ times/night to go). 4. Urge incontinence (leakage) Comes from involuntary contraction of bladder detrusor muscle. Detrustor instabilility or overactivity. |
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Drug treatment for Overactive Bladder (OAB)
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block muscarinic receptors in bladder detrusor, inhibit voiding urge.
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Drugs treatment for Overactive Bladder (OAB)
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1. Oxybutynin- (Ditropan, Oxytrol)
a. 2 short acting, 2 long actin, less intense side effects but only 30% effective. b. IR tabs – works but only modest effectiveness. c.Undergoes 1st pass effect. d. Highly lipid soluble, can pass BBB e. Short half life, need multiple dosing 2. Tolterodine 3.Darifenacin – most selective for M3. Low side effects (ER tabs) |
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Side effects of (OAB) drugs that block muscarinic receptors
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CNS: drowsiness, confusion, hyperpyrexia.
EENT: blurred vision, cycloplegia, photophobia, dry eyes, mydriasis. CV: tachycardia, palpitations, arrhythmias. GI: dry mouth, constipation, impaired GI motility. GU: urinary hesitancy, retention, impotency. Resp: tachypnea, pulmonary edema. Misc: flushing, decreased sweating. |
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How to minimize side effects of OAB drugs
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1. Use long acting formulation – steady but low dose.
2. Drugs that don’t cross BBB – can’t cause CNS effects 3. Selective for drugs to bladder muscarinic receptors- M3 receptor specific to bladder detrusor. Will NOT cause tachycardia b/c that is an M2 receptor. But will have other less serious side effects. |
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Cholinesterase inhibitors are:
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drugs that prevent degradation of (ACh) by acetylcholinesterase (ChE). Have broad range of effects. Make ACh work better/longer.
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Cholinesterase (ChE)
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Normally ChE breaks down ACh → choline + acetic acid (hydrolysis reaction)
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Other characterstics of ChE on the break down of ACh
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2. Involves water = hydrolysis
3. Very fast 4.1 molecule of ChE can break down large amounts of ACh. 5. Prevent inactivation of ACh → enhance actions of ACh from cholinergic Neurons) at: a.Muscarinic b.Ganglionic c.Neuromuscular 6.Therefore C. inhibitors are – indirect acting cholinergic agonist. |
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Cholinesterase inhibitors are:
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also called...indirect acting cholinergic agonist. (make ACh work better)
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Purposes Cholinesterase inhibitors:
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1.Treat Myasthenia Gravis
2.Glaucoma – reduce IOP 3.Treat Alzheimers 4.Antidote to Atropine poisoning. |
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Direct acting Cholinergic agonists (acethycholine)
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Bethanocol (urecholine) tx to increase urination and abnormal abdominal distention
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Nursing assessment: Bethanocol
(cholinergic agonist) |
assess urine output > 600 ml/day check for Orthstatic hypotension
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Metoclopramide (regland) Tx
(cholinergic agonist) |
for GERD and gastroperesis (incl. gastric emptying time)
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Carbachol (miostate
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cholinergic agonist
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Pilocarpine(Pilocar) TX
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IOP due to glaucoma
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Indirect acting cholinesterase inhibitors (prevent degradation of Ach Tx
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for alzheimers
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Other Indirect acting cholinesterase inhibitors
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1. Tacrine (cognex)
2. Donezepil (aricept) (enhances cholinergic function). |
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Atropine used for
(Anti-Cholinergic) |
pre-operative. Decrease salivation and dilate pupils. Antispasmotic to relax smooth muscles and decrease peristalysis. Bradycardia
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Atropine (secondary) Tx for
(Anti-Cholinergic) |
anti-muscarinic poinsing like Bethanicol.
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Cautions for Atropine
(Anti-Cholinergic) |
COPD, CHF, Renal and hepatic OD
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Nursing assessment Atropine
(Anti-Cholinergic) |
Urinary retention, GI obstruction, check vital signs.
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Other anti-cholinergic drugs
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Scopalamine, Dimehhydrinate (dramamine) = tx motion sickness.
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Cholinergic agonists or parasympathomimetics
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1. Bethanicol (urecholine) OAB
2. Metoclopramide (reglan) GERD 3. Pilocarpine (IOP) 4. Carbachol (miostat) ADRs - lungs constrict and BP (down) |
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Indirect acting cholinesterase inhibitors
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prevent degradation of ACh (for Tx Alzheimers
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Examples of indirect acting cholinesterase inhibitors (CHE-I)
(prevents degradation of ACH) Tx Alzheimers |
1. Tacrine (cognex)
2. Donezepil (aricept) |
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Drugs to treat Myasthenia gravis and Multiple sclerosis
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1)Pryridostigmine (mestinon)
2) Neostigmine (prostigmine) dur. 2-4 hrs. freq. dosing 3) Edrophonium Cl (Tensilon) (CHE-I) = more ACH. Antagonist. Curare. |
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Myasthenia gravis etiology
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autoimmune disease involves an antibody response agains the receptors of ACH in skeletal muscles. Leads to degradation of Ach receptors resulting in lack of ACH reaching cholindergic receptors
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Myasthenia gravis S&S
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weakness starting in facial muscles, resuling in dysphagia, res. muscle weakness.
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CAUTIONS W/Pryridostigmine (mestinon)
to treat Myasthenia gravis and Multiple sclerosis |
Asthma, bradycardia, dysrimias, pregnancy.
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CAUTIONS W/Edrophonium Cl (Tensilon) to treat Myasthenia gravis and Multiple sclerosis
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ineffective breathing, myasthenic crisis, resp. depression, bronchospasm.
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Antagonist for Drugs to treat Myasthenia gravis and Multiple sclerosis
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Curare (decreases muscle contraction) Too much = total flacid parlysis
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Non-depolarizing Neuromuscular Blockers I:
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Tubocurarine
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MOA Tubocurarine
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1) Muscle relaxation-during surgery (CNS)
2) Facilitation of mechanical ventiation 3) adjunct to electroconvulsive therapy. 4) Endotracheal intubation 5) Diagnonsis of myasthenia gravis. |
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Parkinson's Disease
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neurodegenerative disease of extrapryamidal system (NOT Corticospinal) assoc w/disruption of NT w/i striatum. Too little Dopamina. Too much ACH.
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Parkinson's Disease
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Characterized by dyskinesias and akinesia
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Parkinson's Disease
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proper function of striatum req. balance between NT dopamine and ACh.
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Parkinson's Disease and dopamine
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Dopamine usually maintains control of ACh and INHIBIT it's excitatory response.
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Parkinson's Disease and dopamine
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Degeneration of dopaminergic neurons result in unopposed Ach thereby causing excititation of GABA
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Parkinson's Disease S&S
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Bradykinesia (slow movements) (initiation of movement), and tremors, stooping.
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Parkinson's Disease DRUGS
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1) Levodopa (will convert to dopamine and cross BBB).
2) Carvidopa - permits more levopopa to reach striatum nerve terminals (increase lifetime of dopa) 3) Amantadine (dopamine agonist) MAIO (monamine oxidase inhibitor) Increases synthesis of dopamine-agonist) 4) COMT inhibitors.) NOT USED (used to treat anti-virals, influenza. Now works for anti-parkinson) |
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Dopamine Agents
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1) Levodopa-promotes dopamine synthesis
2) dopamine agonist - stimulate dopamine receptors directly. 3) Selegiline: Inhibits dopamine breakdown. 4) amantadine: promotes dopamine release. 5) COMT inhibitors: Enhance effects of levodopa by blocking it's degradation. |
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Succinnylcholine (CNS drug)
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NEUROMUSCULAR BLOCKER. For intubation of clients. Causes paradoxical muscle relaxation.
Cation channels remain open. Short acting (2 min). Causes persistent depolarization. |
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Succinnylcholine (addtl. uses)
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NEUROMUSCULAR BLOCKER.Muscle relaxation - surgery
Mechanical ventilation Electroconvulsive therapy To diagnose Myasthenia Gravis |
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How Succinnylcholine is used to diagnose Myasthenia Gravis
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NEUROMUSCULAR BLOCKER. Can differentiate between MG and cholinergic crisis. Aggravates MG but no effect on cholinergic crisis.
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Parkinsons is a problem of...
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Too little Dopamine (from the Substania Negra) and too much ACH.
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What are MAOI's
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Monanamine Oxidase Inhibitors
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What do MAOI's do?
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They degrade Epi and NE in the synapse (recycle). Net effect is increase in Dopamine in the synpase.
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What are MAOI's used for
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Depression b/c they lack Seratonin and NE, Epi. This increases the amount in synpase. Also to Parkinson's patients.
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What food(s) are contraindicated for people on MAOI's?
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Anything that is fermened i.e. Alcohol, aged cheeses, pickles. Can cause HTN Rxn.
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What kind of disease is Parkinsons?
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Progressive, degenerative. WE can slow down progression but not cure it.
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What is pre-cursor to Dopamine and where does it come from?
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Phenalanine (an essential amino acid) we must eat it, then it's converted to Tyrosine, then Dopamine.
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What causes lack of Dopamine in Parkinsons Patients?
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Dopaminic neurons degenerate, resulting in unopposed ACH, causing GABA excitation.
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Best drugs for Parkinsons
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Levodopa
Carvidopa (give them what they need) *Dopamine doesn't easily cross BBB. |
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Other drugs for Parkinsons
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Amantadine (promotes Dopamine release)
Selegilne (inhibits dopamine breakdown). |
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Altzheimers-what are contributing factors?
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Degeneration of Cholinergic receptors. Development of neuritic plaques.
SSX: memory loss due to dementia. |
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Drugs for Alzheimers
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Cholinergic agonists - increase ACH to improve memory.
1. Tacrine (cognex) (CHE-I) 2. Donexepil (aricept) 3. Galantamine (razadyne) Rivastigmine (excelon) CHE-I |
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Alzheimers S&S
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Memory loss
Confusion Disoriented Impaired judgement Personality Changes Diff. w/self care Behav. probl. (pacing, watering , agitation, screaming). Inability to remember family. Inability to communicate. |
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Drugs for Alzheimers
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Cholinesterase Inhibitors. (helps slow progress - not a cure).
ADRs Cholinergic side effects. GI, Dizzy, Headache, Bronchoconstriction, Liver injury (tacrine). OPPOSITE OF PS. |
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NEW Drugs for Alzheimers
(better tolerated) |
Memantine (Namenda)
N-methyl D-aspartate. Receptor antagonists. Lowers amt. of Calcium |
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Multiple Sclerosis Disease Process
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Autoimmune disease that attacks myelin sheath of nerve fibers in brain and spinal cord, causing plaques, common 20-40 yr. old white women.
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Multiple Sclerosis Diagnois
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Increase in IgG in the CSF /albumin ratio and multiple lesions in MRI
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Drugs for Multiple Sclerosis
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1. Diazepam (valium) - enhances GABA. Relieve muscle spasm.
2. Muscle relaxants - baclofen (look for depression, dizzy, cloudy consciousness, hypotension) |
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Drugs for Multiple Sclerosis
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1. Since Myelin sheath is made of proteins...give protein
2. Steroid to decrease inflammation. 3. Anti-convulsives |
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NEW DRUGS to treat Multiple Sclerosis
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1. Immuno regulators = Interferon Beta. Glycoprotein. Supresses destruction of sheat. AVONEX, REBIF (flu-like ADRs)
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Other NEW DRUGS to treat Multiple Sclerosis
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Glatiramer Acetate (Copaxone or copylomer) similar to glycoprotein structure of myelin sheath.
Mitoxantrone - inhibits DNA and RNA synthesis. |
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Other S&S Multiple Sclerosis
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1. Photophobia
1. Spastic Gait 3. Tingling. 4. Inability to reg. Temp. |
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CHOLINERGIC (PS) EFFECTS.
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All parasympathetic target organs.
1. Eye-constrict 2. Heart-slows 3. Lung-constriction 4. Bladder-relax sphincter, contstrict trigone=pee pee 5. GI tract-constriction 6.Sweat Glands-more secretion 7. Sex organs-more secretion 8. Blood vessels-dilates BP down |
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BETA 2 RECEPTOR ACTIVATION CAUSES
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1. Arterioles, Heart, Skeletal Muscle (Dilation)
2. Bronchi-Dilation 3. Uterus-Relaxation 4. Liver-Glycogenolysis 5. Skeletal muscle-Enhanced contraction, Glycogenolysis |
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BETA 1 RECEPTOR ACTIVATION CAUSES
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1. Heart-Increases rate & force of contraction & Increases AV conduction velocity
2. Kidney-Renin release |
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ALPHA 2 - RECEPTOR ACTIVATION CAUSES
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Presynaptic nerve terminal-Inhibits transmitter release
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ALPHA 1 - RECEPTOR ACTIVATION CAUSES
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1. Eye-Contracts radial muscle of eye (causes mydriasis)
2. Constricts: Arterioles, Skin Viscera, Mucous membranes 3. Constricts: Prostate capsule, Veins, Sex Organ, male Ejaculation. 4. Relaxes Bladder-Constricts trigone and sphincter =no pee |
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NICOTINIC (N) RECEPTOR ACTIVATION CAUSES
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all automomic ganglia and adrenal medulla- promotes transmission at PS and S POST ganglionic nerve and promotes release of epinephrine
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NICOTINIC (M) RECEPTOR ACTIVATION CAUSES
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Neuromuscular junction-Causes contraction of skeletal muscle.
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Epinephrine is the only NT that works on
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Beta 2 receptors
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Dopamine only works on
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Alpha1 and Beta 1 receptors
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Dopamine only works on
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Dopamine receptors
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