pharmacologypharmacology - centegra health system · nervous system drugs that affect the: nervous...
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PharmacologyPharmacologyPharmacology
Drugs That Affect The:Nervous System
Drugs That Affect The:Nervous System
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TopicsTopicsTopics
• Analgesics and antagonists• Anesthetics• Anti-anxiety and sedative-hypnotics• Anti-seizure / anti-convulsants• CNS stimulators• Psychotherapeutics• ANS/PNS/SNS agents
• Analgesics and antagonists• Anesthetics• Anti-anxiety and sedative-hypnotics• Anti-seizure / anti-convulsants• CNS stimulators• Psychotherapeutics• ANS/PNS/SNS agents
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A colorful review of neurophysiology!
A colorful review of neurophysiology!
But first...But first...But first...
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Nervous SystemNervous SystemNervous System
CNSCNS PNSPNS
SomaticSomaticAutonomicAutonomic
ParasympatheticParasympatheticSympatheticSympathetic
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AnalgesicsAnalgesicsAnalgesics
• Decrease in sensation of pain.• Classes:
– Opioid.• Agonist.• Antagonist.• Agonist-antagonist.
– Non-opioids.• Salicylates.• NSAIDs.• Adjuncts.
• Decrease in sensation of pain.• Classes:
– Opioid.• Agonist.• Antagonist.• Agonist-antagonist.
– Non-opioids.• Salicylates.• NSAIDs.• Adjuncts.
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OpioidsOpioidsOpioids
• Generic reference to morphine-like drugs/actions– Opiate: derivative of opium
• Prototype: morphine– Morpheus: god of dreams
• Act on endorphin receptors:– Mu (most important)– Kappa
• Generic reference to morphine-like drugs/actions– Opiate: derivative of opium
• Prototype: morphine– Morpheus: god of dreams
• Act on endorphin receptors:– Mu (most important)– Kappa
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Actions of Opioid ReceptorsActions of Opioid ReceptorsActions of Opioid Receptors
Response Mu Kappa
Analgesia
Respiratory DepressionSedation
Euphoria
Physical Dependence
⇓ GI motility
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Actions at Opioid ReceptorsActions at Opioid ReceptorsActions at Opioid Receptors
Drugs Mu Kappa
Pure Agonists-morphine, codeine, meperidine (Demerol®), fentanyl (Sublimaze®), remifentanil (Ultiva®), propoxyphene (Darvon®), hydrocodone (Vicodin®), oxycodone (Percocet®)
Agonist Agonist
Agonist-Antagonist-nalbuphine (Nubaine®), butorphanol (Stadol®)
Antagonist Agonist
Pure Antagonist-naloxone (Narcan®)
Antagonist Antagonist
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General Actions of OpioidsGeneral Actions of OpioidsGeneral Actions of Opioids
• Analgesia• Respiratory depression• Constipation• Urinary retention• Cough suppression• Emesis• Increased ICP
– Indirect through CO2retention
• Analgesia• Respiratory depression• Constipation• Urinary retention• Cough suppression• Emesis• Increased ICP
– Indirect through CO2retention
• Euphoria/Dysphoria• Sedation• Miosis
– Pupil constriction
• ⇓ Preload & afterload– Watch for
hypotension!
• Euphoria/Dysphoria• Sedation• Miosis
– Pupil constriction
• ⇓ Preload & afterload– Watch for
hypotension!
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Non-opioid AnalgesicsNonNon--opioidopioid AnalgesicsAnalgesics
• Salicylates– Aspirin (Bayer® ) * (prototype for class)
• Non-Steroidal Anti-Inflammatory Drugs• Ibuprofen (Motrin®, Advil®)
– Propionic Acid derivative
• Naproxen (Naprosyn®)• Naproxen sodium (Aleve®)• All compete with aspirin for protein binding sites
– Ketorolac (Toradol®)
• Salicylates– Aspirin (Bayer® ) * (prototype for class)
• Non-Steroidal Anti-Inflammatory Drugs• Ibuprofen (Motrin®, Advil®)
– Propionic Acid derivative
• Naproxen (Naprosyn®)• Naproxen sodium (Aleve®)• All compete with aspirin for protein binding sites
– Ketorolac (Toradol®)
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NSAID PropertiesNSAID PropertiesNSAID Properties
Drug Fever Inflammation Pain
Aspirin
Ibuprofen
Acetaminophen
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Aspirin Mechanism of ActionAspirin Mechanism of ActionAspirin Mechanism of Action
• Inhibit synthesis of cyclooxygenase (COX)– Enzyme responsible for synthesis of:
• Inhibit synthesis of cyclooxygenase (COX)– Enzyme responsible for synthesis of:
Prostaglandins–Pain response –Suppression of gastric acid secretion–Promote secretion of gastric mucus and bicarbonate–Mediation of inflammatory response–Production of fever–Promote renal vasodilation (⇑ blood flow)–Promote uterine contraction
Prostaglandins–Pain response –Suppression of gastric acid secretion–Promote secretion of gastric mucus and bicarbonate–Mediation of inflammatory response–Production of fever–Promote renal vasodilation (⇑ blood flow)–Promote uterine contraction
Thromboxane A2–Involved in platelet –aggregation
Thromboxane A2–Involved in platelet –aggregation
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Aspirin EffectsAspirin EffectsAspirin Effects
Good• Pain relief• ⇓ Fever• ⇓ Inflammation
Good• Pain relief• ⇓ Fever• ⇓ Inflammation
Bad• GI ulceration:
– ⇑ Gastric acidity– ⇓ GI protection
• ⇑ Bleeding• ⇓ Renal elimination• ⇓ Uterine contractions
during labor
Bad• GI ulceration:
– ⇑ Gastric acidity– ⇓ GI protection
• ⇑ Bleeding• ⇓ Renal elimination• ⇓ Uterine contractions
during labor
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Acetaminophen (Tylenol®)Acetaminophen (TylenolAcetaminophen (Tylenol®®))
• NSAID similar to aspirin• Only inhibits synthesis of CNS
prostaglandins– Does not have peripheral side effects of ASA:
• Gastric ulceration• ⇓ Platelet aggregation• ⇓ Renal flow• ⇓ Uterine contractions
• NSAID similar to aspirin• Only inhibits synthesis of CNS
prostaglandins– Does not have peripheral side effects of ASA:
• Gastric ulceration• ⇓ Platelet aggregation• ⇓ Renal flow• ⇓ Uterine contractions
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Acetaminophen MetabolismAcetaminophen MetabolismAcetaminophen Metabolism
AcetaminophenAcetaminophen Non-toxicmetabolitesNon-toxic
metabolites
Major Pathway
Minor Pathway
P-450
Toxicmetabolites
Toxicmetabolites
Non-toxicmetabolitesNon-toxic
metabolites
Induced by ETOH
Induced by ETOH
Glutathione
Depleted by ETOH &APAP overdose
Depleted by ETOH &APAP overdose
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AnestheticsAnestheticsAnesthetics
• Loss of all sensation– Usually with loss of consciousness– ⇓ propagation of neural impulses
• General anesthetics– Gases
• Nitrous oxide (Nitronox®), halothane, ether– IV
• Thiopental (Pentothal®), methohexital (Brevitol®), diazepam (valium®), remifentanil (Ultiva®)
• Loss of all sensation– Usually with loss of consciousness– ⇓ propagation of neural impulses
• General anesthetics– Gases
• Nitrous oxide (Nitronox®), halothane, ether– IV
• Thiopental (Pentothal®), methohexital (Brevitol®), diazepam (valium®), remifentanil (Ultiva®)
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AnestheticsAnestheticsAnesthetics
• Local– Affect on area around injection– Usually accompanied by epinephrine
• Lidocaine (Xylocaine ®), topical cocaine
• Local– Affect on area around injection– Usually accompanied by epinephrine
• Lidocaine (Xylocaine ®), topical cocaine
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Anti-anxiety & Sedative-hypnotic DrugsAntiAnti--anxiety & Sedativeanxiety & Sedative--hypnotic Drugshypnotic Drugs• Sedation: ⇓ anxiety & inhibitions• Hypnosis: instigation of sleep• Insomnia
– ⇑ Latent period– ⇑ Wakenings
• Classes:– Barbiturates– Benzodiazepines– Alcohol
• Sedation: ⇓ anxiety & inhibitions• Hypnosis: instigation of sleep• Insomnia
– ⇑ Latent period– ⇑ Wakenings
• Classes:– Barbiturates– Benzodiazepines– Alcohol
Chemically different, Functionally similar
Chemically different, Functionally similar
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Mechanism of actionMechanism of actionMechanism of action
• Both promote the effectiveness of GABA receptors in the CNS– Benzodiazepines promote only– Barbiturates promote and (at high doses)
stimulate GABA receptors• GABA = chief CNS inhibitory
neurotransmitter– Promotes hyperpolarization via ⇑ Cl- influx
• Both promote the effectiveness of GABA receptors in the CNS– Benzodiazepines promote only– Barbiturates promote and (at high doses)
stimulate GABA receptors• GABA = chief CNS inhibitory
neurotransmitter– Promotes hyperpolarization via ⇑ Cl- influx
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Benzodiazepines vs. BarbituratesBenzodiazepines vs. Benzodiazepines vs. BarbituratesBarbituratesCriteria BZ Barb.
Relative Safety High Low
Maximal CNS depression Low High
Respiratory Depression Low High
Suicide Potential Low High
Abuse Potential Low High
Antagonist Available? Yes No
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BenzodiazepinesBenzodiazepinesBenzodiazepines
Benzodiazepines• diazepam (Valium®)• midazolam (Versed®)• alprazolam (Xanax®)• lorazepam (Atiavan®)• triazolam (Halcion®)
Benzodiazepines• diazepam (Valium®)• midazolam (Versed®)• alprazolam (Xanax®)• lorazepam (Atiavan®)• triazolam (Halcion®)
“Non-benzo benzo”• zolpidem (Ambien®)• buspirone (BusPar®)
“Non-benzo benzo”• zolpidem (Ambien®)• buspirone (BusPar®)
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BarbituratesBarbituratesBarbiturates
Subgroup Prototype Typical Indication
Ultra-short acting
thiopental (Pentothol®)
Anesthesia
Short acting secobarbital(Seconal®)
Insomnia
Long acting phenobarbital(Luminal®)
Seizures
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BarbituratesBarbituratesBarbiturates
• amobarbital (Amytal®)• pentobarbital (Nembutal®)• thiopental (Pentothal®)• phenobarbital (Luminal ®)• secobarbital (Seconal ®)
• amobarbital (Amytal®)• pentobarbital (Nembutal®)• thiopental (Pentothal®)• phenobarbital (Luminal ®)• secobarbital (Seconal ®)
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Anti-seizure MedicationsAntiAnti--seizure Medicationsseizure Medications
• Seizures caused by hyperactive brain areas• Multiple chemical classes of drugs
– All have same approach– Decrease propagation of action potentials
• ⇓ Na+, Ca++ influx (delay depolarization/prolong repolarization)
• ⇑ Cl- influx (hyperpolarize membrane)
• Seizures caused by hyperactive brain areas• Multiple chemical classes of drugs
– All have same approach– Decrease propagation of action potentials
• ⇓ Na+, Ca++ influx (delay depolarization/prolong repolarization)
• ⇑ Cl- influx (hyperpolarize membrane)
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Anti-Seizure MedicationsAntiAnti--Seizure MedicationsSeizure Medications
Benzodiazepines• diazepam (Valium®)• lorazepam (Ativan®)Barbiturates• phenobarbital
(Luminal®)
Benzodiazepines• diazepam (Valium®)• lorazepam (Ativan®)Barbiturates• phenobarbital
(Luminal®)
Ion Channel Inhibitors• carbamazepine
(Tegretol®)• phenytoin (Dilantin®)Misc. Agents• valproic acid
(Depakote®)
Ion Channel Inhibitors• carbamazepine
(Tegretol®)• phenytoin (Dilantin®)Misc. Agents• valproic acid
(Depakote®)
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Ion DiffusionIon DiffusionIon Diffusion
• Key to neurophysiology• Dependent upon:
– Concentration gradient– Electrical gradient
• Modified by:– ‘Gated ion channels’
• Key to neurophysiology• Dependent upon:
– Concentration gradient– Electrical gradient
• Modified by:– ‘Gated ion channels’
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Where Does Diffusion Take the Ion?Where Does Diffusion Take the Where Does Diffusion Take the Ion?Ion?
Exterior
Interior
K+
5 mMK+
5 mM
Cl-
LowCl-
Low
Cl-
HighCl-
High
K+
150 mMK+
150 mMNa+
15 mMNa+
15 mM
Na+
150 mMNa+
150 mM
OUT
OUT
ININ
ININ
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Action Potential ComponentsAction Potential ComponentsAction Potential ComponentsM
embr
ane
P ote
ntia
l (m
V)
-50
+30
ThresholdPotential
-70
0
Time (msec)
ThresholdPotential
Resting MembranePotential
Resting MembranePotential
Na+ equilibriumNa+ equilibrium
ActionPotentialAction
Potential
Depolarization!Depolarization!
HyperpolarizedHyperpolarized
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Membrane PermeabilityMembrane PermeabilityMembrane Permeability
Mem
bran
e P o
tent
ial (
mV
)
-50
+30
ThresholdPotential
-70
0
Time (msec)
ThresholdPotential
Resting MembranePotential
Resting MembranePotential
Na+
Influ
x K+
Efflux
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Mem
bran
e P o
tent
ial (
mV
)
-50
+30
ThresholdPotential
-70
0
Time (msec)
ThresholdPotential
Resting MembranePotential
Resting MembranePotential
Na+
Influ
x K+
Efflux
It getshyperpolarized!
It getshyperpolarized!
What Happens to the Membrane If Cl-
Rushes Into the Cell During Repolarization?What Happens to the Membrane If Cl-
Rushes Into the Cell During Repolarization?
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Mem
bran
e P o
tent
ial (
mV
)
-50
+30
-70
0
Time (msec)
It decreases!
It decreases!
What Happens to the Frequency of Action Potentials If the Membrane Gets Hyperpolarized?
What Happens to the Frequency of Action Potentials If the Membrane Gets Hyperpolarized?
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Clinical CorrelationClinical Correlation
• Remember that it is the rate of action potential propagation that determines neurologic function.– Determined by frequency of action potentials.
• Remember that it is the rate of action potential propagation that determines neurologic function.– Determined by frequency of action potentials.
What is a seizure?What is a seizure?What would be the effect on the membrane
of ⇑ Cl- influxduring a seizure?
What would be the effect on the membrane
of ⇑ Cl- influxduring a seizure? Hyperpolarization &
⇓ seizure activity!
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Gamma Amino Butyric Acid ReceptorsGamma Amino Butyric Acid Gamma Amino Butyric Acid ReceptorsReceptors
GABA ReceptorGABA
Receptor
Exterior
Interior
Cl -Cl -
Hyperpolarized!Hyperpolarized!
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GABA+Bz ComplexGABA+BzGABA+Bz ComplexComplexBz
ReceptorBz
ReceptorGABA
ReceptorGABA
Receptor
Exterior
Interior
Cl -Cl -
ProfoundlyHyperpolarized!
ProfoundlyHyperpolarized!
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Are You Ready for a Big Surprise?Are You Ready for a Big Are You Ready for a Big Surprise?Surprise?
Many CNS drugs act on GABA Many CNS drugs act on GABA receptors to effect the frequency receptors to effect the frequency and duration of action potentials!and duration of action potentials!
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SNS StimulantsSNS StimulantsSNS Stimulants
• Two general mechanisms:– Increase excitatory neurotransmitter release– Decrease inhibitory neurotransmitter release
• Two general mechanisms:– Increase excitatory neurotransmitter release– Decrease inhibitory neurotransmitter release
• Three classes:• Amphetamines• Methylphendidate• Methylxanthines
• Three classes:• Amphetamines• Methylphendidate• Methylxanthines
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AmphetaminesAmphetaminesAmphetaminesamphetaminemethamphetaminedextroamphetamine
(Dexedrine®)
amphetaminemethamphetaminedextroamphetamine
(Dexedrine®)
Side Effects•Tachycardia•Hypertension•Convulsion•Insomnia•Psychosis
Side Effects•Tachycardia•Hypertension•Convulsion•Insomnia•Psychosis
Indications•Diet suppression•⇓ Fatigue•⇑ Concentration
Indications•Diet suppression•⇓ Fatigue•⇑ Concentration
MOA:promote release of norepinephrine, dopamine
MOA:promote release of norepinephrine, dopamine
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Methylphenidate (Ritalin®)Methylphenidate (RitalinMethylphenidate (Ritalin®®))
• Different structure than other stimulants– Similar mechanism– Similar side effects
• Indication: ADHD– Increase ability to focus & concentrate
• Different structure than other stimulants– Similar mechanism– Similar side effects
• Indication: ADHD– Increase ability to focus & concentrate
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MethylxanthinesMethylxanthinesMethylxanthines
• Caffeine• Theophylline (Theo-Dur®)• AminophyllineMechanism of action• Reversible blockade of adenosine receptors
• Caffeine• Theophylline (Theo-Dur®)• AminophyllineMechanism of action• Reversible blockade of adenosine receptors
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A patient is taking theophylline and becomes tachycardic (SVT). You want to give her adenosine. Is there an interaction you should be aware of? How should you alter your therapy?
A patient is taking theophylline and A patient is taking theophylline and becomes tachycardic (SVT). You want to becomes tachycardic (SVT). You want to give her adenosine. Is there an interaction give her adenosine. Is there an interaction you should be aware of? How should you you should be aware of? How should you alter your therapy?alter your therapy?
Methylxanthines blocks adenosine receptors. A typical dose of adenosine may not be sufficient to achieve the desired result.
Methylxanthines blocks adenosine receptors. A typical dose of adenosine may not be sufficient to achieve the desired result.
Double the dose!
Double the dose!
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News You Can Use…News You Can UseNews You Can Use……
Source Amount of Caffeine
Coffee•Brewed•Instant
40 – 180 mg/cup30 – 120 mg/cup
Decaffeinated Coffee 2 - 5 mg/cup
Tea 20 – 110 mg/cup
Coke 40 – 60 mg/12 oz
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Psychotherapeutic MedicationsPsychotherapeutic Psychotherapeutic MedicationsMedications• Dysfunction related to neurotransmitter
imbalance.– Norepinephrine.– Dopamine.– Seratonin.
• Goal is to regulate excitory/inhibitory neurotransmitters.
• Dysfunction related to neurotransmitter imbalance.– Norepinephrine.– Dopamine.– Seratonin.
• Goal is to regulate excitory/inhibitory neurotransmitters.
Monoamines
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Anti-Psychotic Drugs (Neuroleptics)AntiAnti--Psychotic Drugs Psychotic Drugs (Neuroleptics)(Neuroleptics)• Schizophrenia
– Loss of contact with reality & disorganized thoughts
– Probable cause: increased dopamine release– Tx. Aimed at decreasing dopamine activity
• Schizophrenia– Loss of contact with reality & disorganized
thoughts– Probable cause: increased dopamine release– Tx. Aimed at decreasing dopamine activity
Two ChemicalClasses:
Two ChemicalClasses:
• Phenothiazines• chlorpromazine (Thorazine ®)
• Butyrophenones• haloperidol (Haldol®)
• Phenothiazines• chlorpromazine (Thorazine ®)
• Butyrophenones• haloperidol (Haldol®)
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Other Uses for AntipsychoticsOther Uses for Other Uses for AntipsychoticsAntipsychotics
• Bipolar depression• Tourette’s Syndrome• Prevention of emesis• Dementia (OBS)• Temporary psychoses from other illness
• Bipolar depression• Tourette’s Syndrome• Prevention of emesis• Dementia (OBS)• Temporary psychoses from other illness
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Antipsychotic MOAAntipsychotic MOAAntipsychotic MOA
• Mechanism is similar• Strength ([]) vs. Potency (‘oomph’)
– Phenothiazines – low potency– Butyrophenones – high potency
• Receptor Antagonism– Dopamine2 in brain – Muscarinic cholinergic– Histamine– Norepi at alpha1
• Mechanism is similar• Strength ([]) vs. Potency (‘oomph’)
– Phenothiazines – low potency– Butyrophenones – high potency
• Receptor Antagonism– Dopamine2 in brain – Muscarinic cholinergic– Histamine– Norepi at alpha1
Therapeutic effects
Uninteded effects
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Antipsychotic Side EffectsAntipsychotic Side EffectsAntipsychotic Side Effects
• Generally short term• Extrapyramidal symptoms (EPS)• Anticholinergic effects (atropine-like)
– Dry mouth, blurred vision, photophobia, tachycardia, constipation)
• Orthostatic hypotension• Sedation• Decreased seizure threshold• Sexual dysfunction
• Generally short term• Extrapyramidal symptoms (EPS)• Anticholinergic effects (atropine-like)
– Dry mouth, blurred vision, photophobia, tachycardia, constipation)
• Orthostatic hypotension• Sedation• Decreased seizure threshold• Sexual dysfunction
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Extrapyramidal SymptomsExtrapyramidal SymptomsExtrapyramidal Symptoms
Reaction Onset Features
Acute dystonia Hours to 5 days Spasm of tongue, neck, face & back
Parkinsonism 5 – 30 days Tremor, shuffling gait, drooling, stooped posture, instability
Akathesia 5 – 60 days Compulsive, repetitive motions; agitation
Tarditivedyskinesia
Months to years Lip-smacking, worm-like tongue movement, ‘fly-catching’
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Treatment of EPSTreatment of EPSTreatment of EPS
• Likely caused by blocking central dopamine2 receptors responsible for movement
• Anticholinergic therapy rapidly effective– diphenhydramine (Benadryl®)
• Likely caused by blocking central dopamine2 receptors responsible for movement
• Anticholinergic therapy rapidly effective– diphenhydramine (Benadryl®)
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Antipsychotic AgentsAntipsychotic AgentsAntipsychotic Agents
• chlorpromazine (Thorazine®)• thioridazine (Mellaril®)• trifluoperazine (Stelazine®)• haloperidol (Haldol®)
• chlorpromazine (Thorazine®)• thioridazine (Mellaril®)• trifluoperazine (Stelazine®)• haloperidol (Haldol®)
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AntidepressantsAntidepressantsAntidepressants
• Likely cause: inadequate monoamine levels• Treatment options:
– Increasing NT synthesis in presynaptic end bulb
– Increasing NT release from end bulb– Blocking NT ‘reuptake’ by presynaptic end
bulb
• Likely cause: inadequate monoamine levels• Treatment options:
– Increasing NT synthesis in presynaptic end bulb
– Increasing NT release from end bulb– Blocking NT ‘reuptake’ by presynaptic end
bulb
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Tricyclic Antidepressants (TCAs)TricyclicTricyclic Antidepressants Antidepressants (TCAs)(TCAs)• Block reuptake of both NE & serotonin
– Enhance effects• Similar side effects to phenothiazines
• Block reuptake of both NE & serotonin– Enhance effects
• Similar side effects to phenothiazines
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TCA Side EffectsTCA Side EffectsTCA Side Effects
• Orthostatic hypotension• Sedation• Anticholinergic effects• Cardiac toxicity
– Ventricular dysrythmias
• Orthostatic hypotension• Sedation• Anticholinergic effects• Cardiac toxicity
– Ventricular dysrythmias
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Selective Serotonin Reuptake Inhibitors (SSRIs)Selective Serotonin Reuptake Selective Serotonin Reuptake Inhibitors (SSRIs)Inhibitors (SSRIs)• Block only serotonin (not NE) reuptake
– Elevate serotonin levels• Fewer side effects than TCS
– No hypotension– No anticholinergic effects– No cardiotoxicity
• Most common side effect– Nausea, insomnia, sexual dysfunction
• Block only serotonin (not NE) reuptake– Elevate serotonin levels
• Fewer side effects than TCS– No hypotension– No anticholinergic effects– No cardiotoxicity
• Most common side effect– Nausea, insomnia, sexual dysfunction
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Monoamine Oxidase Inhibitors (MAOIs)Monoamine Monoamine OxidaseOxidase Inhibitors Inhibitors ((MAOIsMAOIs))• Monoamine oxidase
– Present in liver, intestines & MA releasing neurons
– Inactivates monoamines– Inactivates dietary tyramine in liver
• Foods rich in tyramine: cheese & red wine
• Monoamine oxidase– Present in liver, intestines & MA releasing
neurons– Inactivates monoamines– Inactivates dietary tyramine in liver
• Foods rich in tyramine: cheese & red wine
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MAOI Side EffectsMAOI Side EffectsMAOI Side Effects
• CNS Stimulation– Anxiety, agitation
• Orthostatic hypotension• Hypertensive Crisis
– From increased tyramine consumption• Excessive arteriole constriction, stimulation of heart
• CNS Stimulation– Anxiety, agitation
• Orthostatic hypotension• Hypertensive Crisis
– From increased tyramine consumption• Excessive arteriole constriction, stimulation of heart
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MAOI & Dietary TyramineMAOI & Dietary TyramineMAOI & Dietary Tyramine
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Antidepressant MechanismAntidepressant MechanismAntidepressant Mechanism
TCAs & SSRIs
Block Here
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Antidepressants AgentsAntidepressants AgentsAntidepressants Agents
TCAs• imiprimine (Tofranil®)• amitriptyline (Elavil®)• nortriptyline (Pamelor ®)
SSRIs• fluoxetine (Prozac®)• paroxetine (Paxil®)• sertraline (Zoloft®)
TCAs• imiprimine (Tofranil®)• amitriptyline (Elavil®)• nortriptyline (Pamelor ®)
SSRIs• fluoxetine (Prozac®)• paroxetine (Paxil®)• sertraline (Zoloft®)
MAOIs• phenelzine (Nardil®)
Atypical Antidepressants• bupropion (Wellbutrin®)
MAOIs• phenelzine (Nardil®)
Atypical Antidepressants• bupropion (Wellbutrin®)
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Parkinson’s DiseaseParkinsonParkinson’’s Diseases Disease
• Fine motor control dependent upon balance between excitatory and inhibitory NT– Acetylcholine = excitatory– Dopamine =inhibitoryGABA= inhibitory
• Fine motor control dependent upon balance between excitatory and inhibitory NT– Acetylcholine = excitatory– Dopamine =inhibitoryGABA= inhibitory
Control GABArelease
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Parkinson’s DiseaseParkinsonParkinson’’s Diseases Disease
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Parkinson’s Symptoms:ParkinsonParkinson’’s Symptoms:s Symptoms:
• Similar to EPS• Dyskinesias
– Tremors, unsteady gait, instability• Bradykinesia• Akinesia in severe cases
• Similar to EPS• Dyskinesias
– Tremors, unsteady gait, instability• Bradykinesia• Akinesia in severe cases
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Parkinson’s TreatmentParkinsonParkinson’’s Treatments Treatment
• Dopaminergic approach– ⇑ Release of dopamine– ⇑ [Dopamine]– ⇓ Dopamine breakdown
• Cholinergic approach– ⇓ Amount of ACh released– Directly block ACh receptors
• All treatment is symptomatic and temporary
• Dopaminergic approach– ⇑ Release of dopamine– ⇑ [Dopamine]– ⇓ Dopamine breakdown
• Cholinergic approach– ⇓ Amount of ACh released– Directly block ACh receptors
• All treatment is symptomatic and temporary
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LevodopaLevodopaLevodopa
• Sinemet ® = levodopa + carbidopa• Increase central dopamine levels• Side effects:
– Nausea and vomiting– Dyskinesia (~80% of population)– Cardiovascular (dysrythmias)
• Sinemet ® = levodopa + carbidopa• Increase central dopamine levels• Side effects:
– Nausea and vomiting– Dyskinesia (~80% of population)– Cardiovascular (dysrythmias)
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Levodopa MechanismLevodopaLevodopa MechanismMechanism
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Other AgentsOther AgentsOther Agents
• amantadine (Symmetrel®)– ⇑ release of dopamine from unaffected neurons
• bromocriptine (Parlodel®)– Directly stimulated dopamine receptors
• selegiline (Carbex®, Eldepryl®)– MAOI selective for dopamine (MAO-B)
• benztropine (Cogentin®)– Centrally acting anticholinergic
• amantadine (Symmetrel®)– ⇑ release of dopamine from unaffected neurons
• bromocriptine (Parlodel®)– Directly stimulated dopamine receptors
• selegiline (Carbex®, Eldepryl®)– MAOI selective for dopamine (MAO-B)
• benztropine (Cogentin®)– Centrally acting anticholinergic
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Drugs That Affect the Autonomic Nervous SystemDrugs That Affect the Drugs That Affect the Autonomic Nervous SystemAutonomic Nervous System
Word of WarningCarefully review the A&P material &
tables on pages 309 – 314 and 317 – 321!
Word of WarningCarefully review the A&P material &
tables on pages 309 – 314 and 317 – 321!
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PNS DrugsPNS DrugsPNS Drugs
• Cholinergic– Agonists & Antagonistis (Anticholinergics)– Based on response at nicotinic(N&M) &
muscarinic receptors
• Cholinergic– Agonists & Antagonistis (Anticholinergics)– Based on response at nicotinic(N&M) &
muscarinic receptors
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Acetylcholine ReceptorsAcetylcholine ReceptorsAcetylcholine Receptors
Figure 9-8, page 313, Paramedic Care, V1
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Cholinergic AgonistsCholinergic AgonistsCholinergic Agonists
SalivationLacrimationUrinationDefecationGastric motilityEmesis
SalivationLacrimationUrinationDefecationGastric motilityEmesis
Cholinergic agentscause SLUDGE!
HINT!These effects arepredictable by knowingPNS physiology (table 9-4)
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Direct Acting CholinergicsDirect Acting Direct Acting CholinergicsCholinergics
• bethanechol (Urecholine) prototype– Direct stimulation of ACh receptors– Used for urinary hesitancy and constipation
• bethanechol (Urecholine) prototype– Direct stimulation of ACh receptors– Used for urinary hesitancy and constipation
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Indirect Acting CholinergicsIndirect Acting Indirect Acting CholinergicsCholinergics
• Inhibit ChE (cholinesterase) to prolong the duration of ACh stimulation in synapse
• Reversible• Irreversible
• Inhibit ChE (cholinesterase) to prolong the duration of ACh stimulation in synapse
• Reversible• Irreversible
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Reversible ChE InhibitorsReversible ChE InhibitorsReversible ChE Inhibitors
• neostigmine (Prostigmine®)– Myasthenia Gravis at nicotinicM receptors– Can reverse nondepolarizing neuromuscular
blockade
• physostigmine (Antilirium®)– Shorter onset of action– Used for iatrogenic atropine overdoses @
muscarinic receptors
• neostigmine (Prostigmine®)– Myasthenia Gravis at nicotinicM receptors– Can reverse nondepolarizing neuromuscular
blockade
• physostigmine (Antilirium®)– Shorter onset of action– Used for iatrogenic atropine overdoses @
muscarinic receptors
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Irreversible ChE InhibitorsIrreversible ChE InhibitorsIrreversible ChE Inhibitors
• Very rarely used clinically• Very common in insecticides & chemical
weapons– VX and Sarin gas– Cause SLUDGE dammit and paralysis
• Tx: atropine and pralidoxime (2-PAM®)– Anticholinergics
• Very rarely used clinically• Very common in insecticides & chemical
weapons– VX and Sarin gas– Cause SLUDGE dammit and paralysis
• Tx: atropine and pralidoxime (2-PAM®)– Anticholinergics
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AnticholinergicsAnticholinergicsAnticholinergics
• Muscarinic antagonists– Atropine
• Ganglionic antagonists– block nicotinicN
receptors– Turns off the ANS!– trimethaphan
(Arfonad®)• Hypertensive crisis
• Muscarinic antagonists– Atropine
• Ganglionic antagonists– block nicotinicN
receptors– Turns off the ANS!– trimethaphan
(Arfonad®)• Hypertensive crisis
• Atropine Overdose– Dry mouth, blurred
vision, anhidrosis
• Atropine Overdose– Dry mouth, blurred
vision, anhidrosis
Hot as HellBlind as a BatDry as a BoneRed as a BeetMad as a Hatter
Hot as HellBlind as a BatDry as a BoneRed as a BeetMad as a Hatter
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Neuromuscular BlockersNeuromuscular BlockersNeuromuscular Blockers
• Nicotinic Cholinergic Antagonists– Given to induce paralysis
• Depolarizing– succinylcholine (Anectin®)
• Nondepolarizing– tubocurarine from curare– rocuronium (Zemuron®)– vecuronium (Norcuron®)
• Nicotinic Cholinergic Antagonists– Given to induce paralysis
• Depolarizing– succinylcholine (Anectin®)
• Nondepolarizing– tubocurarine from curare– rocuronium (Zemuron®)– vecuronium (Norcuron®)
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Warning!Warning!Warning!
• Paralysis without loss of consciousness!– MUST also give sedative-hypnotic– Common agents:
• fentanyl (Sublimaze®)• midazolam (Versed®)
• Paralysis without loss of consciousness!– MUST also give sedative-hypnotic– Common agents:
• fentanyl (Sublimaze®)• midazolam (Versed®)
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SNS DrugsSNS DrugsSNS Drugs
• Predictable response based on knowledge of affects of adrenergic receptor stimulation
• HINT: Know table 9-5, page 321• Each receptor may be:
– Stimulated (sympathomimetic)– Inhibitied (sympatholytic)
• Predictable response based on knowledge of affects of adrenergic receptor stimulation
• HINT: Know table 9-5, page 321• Each receptor may be:
– Stimulated (sympathomimetic)– Inhibitied (sympatholytic)
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Alpha1 AgonistsAlphaAlpha11 AgonistsAgonists
• Profound vasoconstriction– Increases afterload & blood pressure when
given systemically– Decreases drug absorption & bleeding when
given topically
• Profound vasoconstriction– Increases afterload & blood pressure when
given systemically– Decreases drug absorption & bleeding when
given topically
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Alpha1 AntagonismAlphaAlpha11 AntagonismAntagonism
• Inhibits peripheral vasoconstriction– Used for hypertension– prazosin (Minipress®)– doxazosin (Cardura®)– phentolamine (Regitine®)
• Blocks alpha1&2 receptors
• Inhibits peripheral vasoconstriction– Used for hypertension– prazosin (Minipress®)– doxazosin (Cardura®)– phentolamine (Regitine®)
• Blocks alpha1&2 receptors
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Beta1 AgonistsBetaBeta11 AgonistsAgonists
• Increases heart rate, contractility, and conductivity
• Increases heart rate, contractility, and conductivity
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Beta Antagonists (β Blockers)Beta Antagonists (Beta Antagonists (ββ Blockers)Blockers)
• Frequently used• Lower Blood Pressure• Negative chronotropes & inotropes
• Frequently used• Lower Blood Pressure• Negative chronotropes & inotropes
Beta1 Selective Blockade• atenolol (Tenormin®)• esmolol (Brevibloc®)• metoprolol (Lopressor®)
Beta1 Selective Blockade• atenolol (Tenormin®)• esmolol (Brevibloc®)• metoprolol (Lopressor®)
Nonselective• propranolol (Inderal®)• labetalol (Normodyne®,
Trandate®)• sotalol (Betapace®)
Nonselective• propranolol (Inderal®)• labetalol (Normodyne®,
Trandate®)• sotalol (Betapace®)
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Adrenergic Receptor SpecificityAdrenergic Receptor SpecificityAdrenergic Receptor Specificity
Drug α1 α2 β1 β2 Dopaminergic
EpinephrineEphedrineNorepinephrinePhenylephrineIsoproterenolDopamineDobutamineterbutaline
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Web ResourcesWeb ResourcesWeb Resources
• Web based synaptic transmission project– http://www.williams.edu/imput/index.html
• Web based synaptic transmission project– http://www.williams.edu/imput/index.html
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Thank You!Thank You!Thank You!
• To Temple College EMS Professions for permission to use their materials
• To Temple College EMS Professions for permission to use their materials