Neurology and Psychiatric Drugs Flashcards

1
Q

Name the centrally acting skeletal muscle relaxants

A

Diazepam (Benzodiazepene)
Tizanidine (α2 agonist)
Baclofen

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2
Q

Diazepam

A

-Benzodiazepine (“long tapering flag”)

  • increase frequency of oppening of the chloride ion channel
  • binds at allosteric site on GABA-A receptor which is a chloride channel and potentiates GABA effects →Cl- influx →hyperpolarization→less neuronal excitation
  • indicated for spasticity induced by neurological disorders (e.g. MS)
  • produces sedation at required dose for reduction of muscle tone
  • can induce withdrawl affects
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3
Q

Tizanidine

A

-α2 agonist

  • inhibits release of excitatory Amino acids thus re-inforcing both pre/postsynaptic inhibition in the spinal cord
  • indicated for spasticity induced by neurological disorders (e.g. MS)
  • produces sedation at required dose for reduction of muscle tone
  • can induce withdrawl affects
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5
Q

Dantrolene

A
  • block RYR1 receptor → decreasing free intracellular calcium concentration.
  • treats malignant hyperthermia which is a condition resulting from defective RYR receptors in the Sarcoplasmic reticulum
  • useful for spinal injuries ,spasm after stroke
  • may cause severe liver toxicity
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6
Q

Botulinum toxin

A
  • exotoxin of clostridium botulinium
  • controls release of Ach from vesicles by binding to synaptobrevin
  • treats ophthalmic / local muscle spasms
  • local facial injection are used for treatment of wrinkles
  • present on honey - shouldn’t be given to children < 1 y.o.
  • may cause flaccid paralysis
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8
Q

Baclofen

A
  • GABA-B agonist
  • GABA-B receptor is a K+ channel →increase K+ influx →hyperpolarization →Ca+2 ion influx decrease → decrease release of excitatory NTs
  • rapid ,complete absorbtion after oral adminstration
  • used for spasticity induced by neurological disorder (e.g. MS)
  • less sedative but also less effective than Diazepam
  • enhances sedative/resp dep. effects of opiates
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9
Q

Non depolarizing muscular relaxant

A
  • competitive antagonists preventing Ach to depolarize the muscle cells
  • at higher doses they produce more intense motor blockade

1st -muscles of face,eyes
2nd -finger,limbs neck trunk
3rd-intercoastals , diaphragm

  • useful for anesthesia and facilitation of intubation
  • can be reversed by **Neostigmine

Isoquinolone dervatives -**

  • Tubocurarine
  • Atra-curium
  • Cistra-curium

Steroid dervatives -can be reversed by Neostigmine
-Pan-curonium

-Ro-curonium

*have vagolytic effect +enhance NE release

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10
Q

Depolarizing muscle relaxant

A
  • depolarize muscle cells similarly to Ach however they are more resistant to degradation by AChE therefore n-AChR is incapable of transmitting further impulses because of the resistance to depolarization
  • can lead to flaccid paralysis
  • During phase I the reaction is irreversible
  • useful for rapid endotracheal intubation or during electroconvulsive shock
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11
Q

how are benzodiazepens classified ?
name Benzodiazepens for each category
(“Ben’s Diner”)

A

-have “PAM-suffix
(“Pam-cakes in Ben’s diner”)

-have “OLAM-suffix”
(“pamcakes offered ALL A.M.”)
——————————————————————————–
Short acting Benzodiazepens -“ATOM”

Triaz-olam
Oxaze-pam (“fast ox”)
Midaz-olam
——————————————————————————–
Intermediate acting Benzodiazpenes “lora the clown”
Loraze-pam
Alpraz-olam
Clonaze-pam
——————————————————————————–
Long acting Benzodiazpenes
Diaze-pam
Fluraze-pam

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12
Q

Benzodiazpenes MOA

(“Ben’s Diner”)

A

-bind to an allosteric site on GABA-A Receptor
(“Ben’s diner coworker handing the Cab-A driver Pamcakes”)

-GABA-A receptor is a chloride channel, chloride influx hyperpolarizes nerve cells
(“chlo-rider” sign on Cab-A)

-Benzodiazpenes increase the Frequency of opening of the chloride channel
(ben’s diner is :”now open more frequently”)

-potentiates (enhance) transmission of GABA in CNS
(“Red CNS light on Cab-A”)

-GABA is the major inhibitory neurotransmitter in the CNS (the sign on Cab-A says “take it easy” )

-metabolized by the liver and produce long acting active metabolites
(“fast ox has liver spot on him”)

-have addictive potential
(“Ben’s Diner pamcakes have addictive flavour”)

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13
Q

what are Benzodiazepens used for ?

(“Ben’s Diner”)

A

-IV adminstration of Benzodizapenes are useful in managment of alcohol withdrawl , seizures , anesthesia (“Ivy on pole”)

-IV adminstration of Benzos can be used for general anesthesia
(“green shirt sedated customer with straw in mouth”)

-IV adminstration of Benzos is useful to induce
conscious sedation for minor procedures ,e.g.-colonoscopy
(cup saying “lite” infront of sedated customer)
——————————————————————————–
-useful for treatment of status epilepticus
(“coworker unplugging jackhammer”)

  • can treat insomnia (“customer sleeping on table”)
  • **not 1st line due to physical dependence**

-can treat Parasomnias in children
(“crying kid in pajamas”)

-benzos are muscle relaxants used to treat Spasticity cause by upper motor neuron disorders
(“red shirt blacky relaxed on diner’s bench”)

  • useful in treatment of General Anxiety Disorder {G.A.D}
  • *SSRIs/SNRIs are 1st line

(“Anxious cutsomer not sure if he can pay for the date lool”)

  • Benzos are useful for treating Panic disorder
  • *SSRIs/SNRIs are 1st line
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14
Q

Benzodiazepens side effects

A

-can potentially cause addiction
(pam-cakes have “addictive flavour”)

-can cause tolerance (“all are welcome” sign in Ben’s Diner)

-Benzodiazepens can cause Anterograde Amnesia and learning impairment
(“question mark hat on sedated customers head”)

  • useful for conscious sedation so patient will follow orders but will forget unpleasant procedure afterwards
  • Benzos can cause Central Ataxia causing elderly patient to fall

(“unbalanced stack of pamcakes infront of old fart”)

-elderly patients are more sensitive for Benzos side effects (“disoriented man sitting infront of stack of unbalanced pamcakes”)

  • adminstration of Benzos should be avoided with other CNS depressants such as 1st generation antihistamines
    (“coworker with bee swatter smacks old fart customer”)
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16
Q

what are the alcohol withdrawal symptoms

? what role do Benzos have in treating alcohol withdrawal

A

-alcohol also binds GABA-A receptor but on a different allosteric site
(“alcoholic guy is on back of Cab-A”)

-Benzos are useful in treatment of alcohol withrdawl symptoms (“hangover special pamcakes”)

  • especially long acting Benzos such as Diazepam and Chlordiazepoxide
    (“Long tapering flag on hangover special pamcakes”)
  • ​for patients with hepatic insufficiency use short-acting Benzos

Alcohol Withdrawal symptoms -“3 alcohol specialists”

1st specialist (8-12 hours) - insomnia ,tremulousness , anxiety , autonomic instability

2nd specialist (12-48 hours) - Seizures

_3rd specialist (_48-96 hours)-**delirium tremens** 
(fever ,disorientation , severe agitation )
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17
Q

what is the key difference between Benzodiazepens and Barbiturates

A

-the difference between them is that Barbiturates bind different allosteric site on GABA-A receptors

(“barber shop located on other side of Cab-A”)

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18
Q

How can you reverse Benzodiazepens-induced sedation

A

-Flumazenil is a competitive antagonist at the BZD receptor and can reverse Benzos-induced sedation

(“violent-antagonizing fluffy muzzled dog”)

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19
Q

Name the non-Benzodiazepine hypnotics

(“catching some Z’s”)

A

the 3 Z’s

Zolpidem
Zaleplon
esZopiclone

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20
Q

non-Benzodiazepine hypnotics MOA

A

-bind same allosteric site as Benzodiazepines at GABA-A receptor
(“ben’s diner coworker and zzz mattresses coworker are grabbing the same Cab-A handle”)

-GABA-A receptor is a chloride channel,chloride influx hyperpolarizesnerve cells
(“chlo-rider” sign on Cab-A)

-potentiates (enhance) transmission of GABA in CNS
(“Red CNS light on Cab-A”)

-GABA is the major inhibitory neurotransmitter in the CNS (the sign on Cab-A says “take it easy” )

-Barbiturates bind different allosteric site on GABA-A receptors
(“barber shop located on other side of Cab-A”)

-alcohol also binds GABA-A receptor but on a different allosteric site
(“alcoholic guy is on back of Cab-A”)

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21
Q

Pharmakokinetics of Zolpidem Zaleplon es-Zopiclone

A

-Zolpidem and Zaleplon are fast acting non-Benzos with rapid onset (sheeps sign says :”fall asleep FAST”)

-Non-benzos hypnotics have short duration of action
(“sheeps quick jump and fall on sign”)

-Zolpidem and Zaleplon are metabolised by the liver
(“sheeps on sign have liver spot on them”)

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23
Q

Side effects on non-Benzos

A

-elderly are more sensitive to the side effects

-can cause Central Ataxia
(“unbalanced stack of pillows”)

-avoid use with other CNS depressants
(“cannot combine with other CoupoNS”)

  • e.g.- 1st Gen. Antihistamines
    (“bee swatter coworker hitting old fart”)
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24
Q

what are non-Benzodiazepene hypnotics used for ?

A

-useful in treatment of insomnia

  • Zolpidem and Zaleplon are short-acting and therefore useful in treating Sleeep onset insomnia and not for maintaining sleep
  • esZopiclone has longest half life and is therefore effective for both falling asleep and maintaining sleep

​-less likely to cause withdrawal symptoms
(“sale sign says break those bad sleeping habits”)

-non-benzos are less likely to cause tolerance
(sale sign says “returns not tolerated”)

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26
Q

how can you reverse non-benzos sedation ?

A

Flumazenil - BZD Competitive antagonist
(“fluffy muzzled dog biting on zzz matresses red arrow sign”)

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27
Q

what other drugs can be used to treat insomnia ? MOA?

(“let your sleepless nights melt away”)

A
  • *Melatonin**
  • *Ramelteon/Agomelatin** (melatonin receptor agonists)

-MT1 and MT2 melatonin receptors are found in the suprachiasmatic nucleus of the hypothalamus and are activated by Ramelteon
(“nucleus above x shaped ceiling fan”)

  • **-Ramelteon has no direct effects on GABA-ergic transmission in the CNS **
  • melatonin receptors maintain the Circadian rythm (“light and dark spotlights”)

-Ramelteon/Melatonin have fewer side effects and are safer in Geriatric patients
(peacefully sleeping old fart below “melt-away sign”)

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28
Q

Name Barbiturates

A

Thiopental
(“The Ol’ quick shave”)
Primidone
(“Perm is done!” primadona)
Phenobarbital

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29
Q

Barbiturates MOA

A

-GABA-A receptor is a chloride channel,chloride influx hyperpolarizes nerve cells
(“chlo-rider” sign on Cab-A)

-potentiates (enhance) transmission of GABA in CNS
(“Red CNS light on Cab-A”)

-GABA is the major inhibitory neurotransmitter in the CNS (the sign on Cab-A says “take it easy” )

-binds to a separate allosteric site on GABA-A Receptor
(“barber opening dooe on other side of Cab-A driver Pamcakes”)

-Barbiturates increase the duration of opening of the GABA-A receptor chloride channel
(sign at entrance of shop saying :”long hair? now open longer”)

-Barbiturates have long duration of action and therefore “hangover” effects are more common
(“long tapering flag outside barber shop”)

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30
Q

Barbiturates Pharmacokinetics

(mainly Thiopental here?)

A

-Barbiturates have long duration of action and therefore “hangover” effects are more common
(“long tapering flag outside barber shop”)

  • Thiopental has rapid onset and short duration of action because it’s highly lipid soluble
  • plasma levels of Thiopental decrease rapidly due to redistribution to skeletal muscle and adipose

(“barber cuts hair and redistributes it to arms and belly of customer”)

Redistribution graphof Thiopental (on customer’s chest)

Decay line - rapid decay of plasma Thiopental

Brief peak - rapid accumulation of thiopental in brain and rapid redistribution

Growth line-rapid accumulation of Thiopental in skeletal muscle and adipose(recovery from anesthesia)

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32
Q

Barbiturates side effects

A

-chronic use of barbiturates leads to tolerance
(“all are welcome” sign in entrance of barbershop)

-chronic barbiturates use leads to physical dependence
(“addicted to curls” sign)

-can cause hypotension
(“fainted old fart sitting on hair dryer chair”)

-can cause profound cardiac and respiratory depression
(“old fart has collapsed heart and lungs t-shirt”)

-can cause severe CNS depression (coma) ,should be avoided in elderly
(“brain shaped hair dryer”)

-barbiturates are potent inducers of the CYP450 which may increase metabolism of drugs such as warfarin
(activated chrome bumper plate saying “CYP450”)

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33
Q

what are Barbiturates used for ?

A

IV-adminstration of Barbiturates (“Ivy on pole”)

-IV adminstration of Thiopental can be used for induction of anestehsia since its highly lipid soluble and enters the CNS quickly.
(intubated customer getting “The Ol’ quick shave”)

-IV adminstration of Phenobarbital can be used to treat Seizures
(“coworker outside unplugging jackhammer”)

-Primidone (“perm is done!”) can be used to treat seizures and essential tremors - 1st line with propanolol
(“prima dona’s barber has tremulous hand”)

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35
Q

name the IV Anesthetics

(“Ivy on all damn poles”)

A

Propofol
(Introducing Prospero “fall asleep” the hypnotist)

Etomidate
(Introducing the beast from the east “THE INTIMIDATOR”)

Ketamine
(Introducing “snaKE TAMINg” nomad )

Benzodiazepines
(“Ben’s Diner”)

Thiopental
(“The ol’ quick shave”)

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36
Q

Propofol

(prospero “fall asleep” the hypnotist)

A

-potentiate chloride current through the GABA-A receptor complex
(“old Cab-A behind prospero’s stand”)

-can be used for induction of anesthesia
(introducing prospero “fall asleep” the hypnotist)

-can be used for maintenance of anesthesia
(sign next to prospero says :”try to MAINTAIN your sanity!”)

-propofol cause profound vasodilation (arterial+venous)

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37
Q

Etomidate

(“introducing the beast from the east the INTIMIDATOR”)

A

-potentiates chloride current through the GABA-A receptor complex
(“old Cab-A behind the INTIMIDATOR stand”)

-is an IV anesthetic for induction
(“introducing the intimidator”)

-Etomidate preserves cardiovascular stability
(“the buffy intimidator stabilizes the patient “)

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38
Q

Ketamine

(“snaKE TAMINg)

A

-inhibits the NMDA receptor complex which is a glutamate receptor and ion channel
(“hitched nomadic camel”)

-can be used for induction of anesthesia
(“introducing the snaKE TAMINg nomad”)

-causes “dissociative anesthesia”
(“man looking in snakes eye causing dissociative trance”)

-can cause unpleasant emergence reactions

  • vivid colorful dreams
    (“colorful steam from snakes bucket”)
  • ​hallucinations
  • ​out of body experiences

​-can cause cardiovascular stimulation{Incr.BP HR CO}
(“stimulated cobra’s head shaped like heart”)

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42
Q

Benzodiazepines

(“Ben’s Diner”)

A

Midaz-olam ,
Loraze-pam

-IV anestheic used preoperatively

-used for conscious sedation for minor procedures such as colonoscopy
(“bowel water pump outside Ben’s Diner”)

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43
Q

Barbiturates

(“Barber’s shop)

A

-Thiopental has rapid onset and short duration of action since it is highly lipid soluble
(“The Ol’ quick shave”)

-IV Anesthetic used for induction of anesthesia
(“Introducing the BARBER SWEENY PENTAL”)

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44
Q

Neurolept Analgesia

A

Neuroleptanalgesia

  • a state of analgesia ,sedation, muscle relaxation BUT no loss of consciousness
  • Fentanyl + Droperidol
  • contraindicated in parkinsonism
  • useful during diagnositc procedures requiring cooperation of the patient

Neuroleptanesthesia

  • Fentanyl+Dorperidol, Nitrous oxide
  • addition of NO improves amnesia
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45
Q

Peri-operative medications

A

Before surgery

-IV. Barbiturates - Thiopental (“the ol’ quick shave”)
-Sedative/Anxiolytic Benzodiazepine -Diazepam (“long tapering flag”)
-Antimuscarinic - parasympatholytic agent -Atropine(“alice”)
-Analgetics - Opiods (fentanyl) non opioids
—————————————————————————————————
During surgery
-NMB- Succinylcholine (depolarizing) / Curare derivatives ( non-depolarizing)
-Pressors in case of shock - Norepinephrine
—————————————————————————————————
After surgery
-If opioids were used before surgery - non-opioids should be used
-antagonism of NMB -Neostigmine
-antagonism for opioids if respiration is too slow - Naloxone

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46
Q

Gaseous anesthetic

A

Nitrous Oxide (N2O)

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47
Q

Volatile anesthetics

A

Enflurane
Isoflurane
Halothane

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48
Q

Volatile anesthetics pharmacodynamics

A

-volatile anesthetics are liquid at room temperature
(e.g. enflurane, isoflurane, halothane)
(“Air tank in water”)

-volatile anesthetics are fluorinated
(e.g. enflurane, isoflurane,halothane)
(“Balloon flower”)

-highly soluble inhaled anesthetic (e.g. halothane)
(“Moving freely in ball pit”)

more soluble inhaled anesthetics (e.g. halothane) have a slower onset of action
(“Passed out later”)

-more soluble inhaled anesthetics (e.g. halothane) have a longer duration of action (“Long tapering flag”)

  • Partition>>>: higher blood:gas partition coefficient
    (e. g. halothane) → higher solubility → **slower onset of action
  • ———————————————————————————**

Less steep arterial tension curve (e.g. halothane) → higher blood:gas partition coefficient→higher solubility → slower onset of action

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49
Q

Nitrous Oxide Pharmacodynamics

A

less soluble inhaled anesthetic
(“Impeded by ball pit”)
(e.g. N2O)

less soluble inhaled anesthetics (e.g. N2O) have a faster onset of action
(“Passed out earlier”)

less soluble inhaled anesthetics (e.g. N2O) have a faster recovery
(“Immediate rescue” )

Steeper arterial tension curve (e.g. N2O)→ lower blood:gas partition coefficient→ lower solubility → faster onset of action

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50
Q

Volatile Anesthetics side effects

A

-inhaled anesthetics can cause respiratory depression (leading to decreased minute ventilation and hypercapni a)
(“Deflating lung balloons”)

-myocardial depression →hypotension
(“deflating heart balloon”)

-fluorinated anesthetics increase cerebral blood flow (decrease cerebral vascular resistance)(“Red brain wig”)

halothane can be hepatotoxic
(e.g. massive hepatic necrosis) (“Cracked liver”)

enflurance can be nephrotoxic (“Smacked in the flank”)

enflurance can induce seizures (“Shaking”)

-malignant hyperthermia
(skeletal muscle hypersensitivity to volatile anesthetics) (“Magnificent birthday”)

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51
Q

MAC

A

minimum alveolar concentration (MAC)

MAC corresponds to the dose of anesthetic that causes 50% of patients to become unresponsive to painful stimuli
(“1 out of 2 unresponsive”)

1/MAC corresponds to the potency of an inhaled anesthetic ​(“Inverted bowl of potent mac and cheese”)

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53
Q

what is the treatment of malignant hyperthermia

A

Dantrolene
———————————————————————————–

Blocking Ryan: dantrolene blocks ryanodine receptors

-treats malignant hyperthermia

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57
Q

malignant hyperthermia

A

-succinylcholine (depolarizing muscle relaxant) can also causes malignant hyperthermia

malignant hyperthermia is related to a defect in ryanodine receptors (RyR) in the sarcoplasmic reticulum

-excess heat production and consumption of ATP induces rhabdomyolysis

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58
Q

what is the mechanism of action of SSRIs ?

A

-inhibit presynaptic reuptake of Serotonin

(“worker in sitcom keeps post-it stick notes out of the drawer”)

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59
Q

name the SSRIs

(“travel posters behind expreSS tRIps”)

A

Selective Serotonin Re-uptake Inhibitors

Paroxetine
(“Parrot air” poster)

Fluoxetine
(“Fly out”poster)

Sertraline
(“Desert Airline” poster)

Citalopram
(“the City” poster)

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60
Q

MOA of SNRIs

A

-inhibit presynaptic re-uptake of Norepinephrine and Serotonin

(“North and South compass poster above dual copy machine “)

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61
Q

Name the SNRIs

A

SNRIs

-Venlafaxine
(“fax machine infront of compass poster”)

-Duloxetine
(“Dual copy machine below compass poster”)

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62
Q

what can SSRIs AND SNRIs be used for ?

A
  • 1st line treatment for depression {M.D.D}
  • *slower onset than Benzos so not useful for treatment of acute symptoms *

-1st line treatment of G.A.D
(Anxious coworker holding “preformance repot”)

-useful for treatment of panic disorder
(“the scream saver”)

-useful for treatment of PTSD
(coworker holding dog tags saying “PT” and SD”)

(“happy/sad masks logo on right edge of sitcom”)

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63
Q

what can SSRIs specifically be used for?

A

-useful in managment of OCD
(“obsessively neat coworker re-arranging his table”)

-
useful in treatment of Bulimia
(blonde coworker opening “binge snack drawer”)

-useful in treatment of Social Anxiety Disorder
(“shy coworker hiding behind desk “)

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64
Q

what can SNRIs specifically be used for?

A

-useful for treatment of Diabetic Neuropathy
(“coworker feeling pain from Diasweeties machine”)

-useful in treatment of chronic pain (neuropathic)
(“chronically frayed wires from diasweeties machine”)

-useful in treatment of fibromyalgia
(“fiber bars at top shelf in diasweeties machine” )

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65
Q

how long should you wait before considering an alternative treatment for SSRIs/SNRIs ?

A

-SSRIs and SNRIs take 1-2 months to achieve maximum effect

(“2 months calendar behind shy guy”)

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66
Q

what are the Side effects of SSRIs ?

A

-hyponatremia as a result of SIADH {incr. ADH}
(“inappropriately wet head of blacky coworker”)

-SSRIs can cause Sexual Dysfunction
(“patty rejects and throws paper clips in ugly guy’s face”)

-SSRIs can cause weight gain
(“fat guy next to expreSS tRIps counter”)

-SSRIs can cause Drowsiness
(“purple shirt coworker sleeping on the job”)

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67
Q

what condition may percipitate as a result of SSRIs and SNRIs abuse ? what are the characterisitc findings of this condition ?

A

-SSRIs and SNRIs may cause Serotonin Syndrome
(“excessive smiley post-it sticky notes in back office”)

-combination of SSRIs/SNRIs with other drugs may also cause serotonin syndrome {e.g. TCAs,MAOis}
(“Tricycle and mouse traps in smiley backoffice”)

-serotonin syndrome is characterized by hyperthermia and hypertension
(“michelle boss of the office is hot and has steam coming out of his ears”)

-characterized by neuromuscular hyperactivity , hyperreflexia , clonus
(“boss of office hyperactive foot tap”)

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68
Q

what is the treatment for Serotonin Syndrome ?

A

Cyproheptadine (5-HT2 blocker)

(boss of the office holding sign saying “silly pranks prohibited”)

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69
Q

what are the side effects of SNRIs?

A

-SNRIs can cause hypertension

(“hypertensive coworker has steam coming out of his ears because of the fax machine”)

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70
Q

what are the withdrawl symptoms observed after stopping adminstration of SSRIs/SNRIs ?

A
  • withdrawl symptoms from SSRIs/SNRIs include Flu-like symptoms

(office phone has sticky note saying “out with the flu”)

71
Q

Name the tertiary Tricyclic Antidepressants

A

Imipramine
(“Imprint on green shirt boy’s face”)

Amitriptyline
(“green shirt boy tripping from tricycle”)

secondary amines

**Nortriptyline

Desipramine**

72
Q

Name the Secondary amine TCAs

A

NORth siDE prep secondary school”

Nortriptyline

**Desipramine

-**
secondary amines have less anticholinergic effects (woman protected by “Northside prep” sign

*most appropiate for the elderly**

73
Q

what is the MOA of TCAs ?

A

TCAs inhibit presynatpic uptake of serotonin and norepinephrine NET/SERT

(“green shirt boy prevented from picking up smiley and compass balls”)

74
Q

what can TCAs be used for ?

A

-useful in treatment of resistant depression
(“happy/sad mask next to resistant door that kid can’t open”)

-useful in diabetic neuropathy
(“kid having pain from diasweeties machine”)

-useful in treatment of chronic pain (neuropathic)
(“chronically frayed wire next to diasweeties machine”)

-may be used for migraine prophylaxis
(“pounding headbell” )

  • **Amitriptyline is the only TCA with proven efficacy**

-Clomipramine(secondary amine) can treat OCD
(“obessively neat kid re-arranging his marbles”)

  • **not as 1st line treatment - SSRIs are.**
75
Q

what are the side effects of TCAs?

A

-TCAs can cause Sexual dysfunction
(“gym teacher rejected by Mrs. Pearson”)

-can cause Seizures
(“ball hits yellow shirt kid and he becomes shakey”)
——————————————————————————–
-TCAs (mostly tertiary) have severe antimuscarinic effects including:

  • dry mouth (“dry as a cracker”)
  • ​constipation
  • ​blurred vision (“blind as a bat”)
  • urinary retention (“full bladder shaped tea kettle”)
  • ​CNS effects (“mad as a hatter”)

**the antimuscarinic effects are the most common side effects among all TCAs side effects **

***the most potent antimuscarinic effects are exerted by Amitriptyline***

****TCAs are contraindicated in elderly because of these severe antimuscarinic/antihistamine effects****

  • TCAs block H1 receptors (“blacky with bee swatter”)
  • leads to sedation
    (“blue shirt kid sleeping on table”)

​leads to increased appetite weight gain
(“red shit fat kid next to sleeping kid”)
​——————————————————————————–
-TCAs block α1 receptors
(“pink shirt girl holding single extinguished candle”)

  • may cause orthostatic hypotension
    (“pink shirt girl next to tea party is passed out”)

​​——————————————————————————–
-TCAs can cause Serotonin syndrome
(“stack of smiley balls behind blue shirt dodger”)

76
Q

what are cardiac side effects cause by TCAs ? what is the treatment for these undesired effects ?

A

-TCAs block cardiac fast Na+ channels that may cause fatal cardiac arrhythmias
(“inactivated peaNa+ butter jar”)

-can cause wide QRS complex on ECG
(“Wide QRS-shaped crack in heart sign”)

-can induce Torsades de pointes ventricular tachycardia
(“twisted Torsades streamer”)

**the most common cause of death of patients treated with TCAs is TCA overdose causing fatal cardiac arrhythmias

(“dodge ball hitting peaNa+ butter cookie stand and breaking <3 cookies”

  • Sodium Bicarbonate can be used to treat widened QRS and ventricular arrhythmia caused by TCAs overdose (white
77
Q

name the MAO enzymes and their actions !

A

-MAO-A (“albino mouse”) breaks down Serotonin , Norepinephrine , Dopamine
(“white mouse eating smiley cheese , compass cheese and dopa rope”)

-MAO B (“ black mouse”) breaks down dopamine exclusively (“black mouse eating rope”)

78
Q

name non-selective MAOis

A

Tranylcypromine
(“Try a sip of wine !” sign on table)

Phenelzine
(“Funnel in wine bottle on table”)

Isocarboxazid
(“Boxed wine on table”)

79
Q

what are MAOis used for?

A

-MAOis are irreversible
(“mouse skeleton trapped in mouse trap)

-useful in treatment of Atypical depression
(“Chateu Tyramine …not your typical winery”)

-useful in treatment of depression (not 1st line)
(“happy/sad mask on chateu tyramine sign”)

-useful in treatment of resistant depression
(“guy trying to open resistant wine bottle with happy/sad mask label”)

80
Q

-name selective MAOis inhibitor

A

Selegiline - selective MAO B inhibitor
(“guy on ladder with sledge hammer trying to hit black mouse”)

Moclobemide - selective MAO A inhibitor

81
Q

what are selective MAOis used for ?

A

-useful for treatment of Cogwheel rigidity seen in Parkinson’s disease since they increase Dopamine levels in the CNS

(“watch runing by cogwheels above sledge hammer”)

82
Q

what are the side effects of MAOis ?

A

-since non selective MAOis inhibit serotonin breakdown they have similar side effects to SSRIs including:

  • highest rate of sexual dysfunction among anti depressant
  • orthostatic hypotension
  • weight gain

-should be avoided with tyramine containing foods such as aged meats , wine and cheese
(“wine and cheese on table”)

-tyramine is usually broken down in the GI by MAO enzymes
(“albino mouse eating GI meat”)

-when MAOis are adminestered tyramine is not broken down and act as sympathomimetic
(“albino trapped in mouse trap and NE compass cheese released”)

-Tyramine Toxicity can percipitate a hypertensive
crisis

(“blonde lady is hypertensive and sweaty having steam come out of her ears “)

-may cause Serotonin Syndrome
(“pile of smiley cheese next to tricycle”)

-should be avoided with other drugs such as TCAs and SSRIs
(“yellow tricycle in front”)

83
Q

what drug could be adminesterd for management of hypertensive crisis resulting from Tyramine toxicity ?

A

Phentolamine-reversible α1 and α2 antagonist (“phantom of the alpha behind blonde lady”)

84
Q

Name Atypical Antidepressants

A

Bupropion (Unicyclic)
(“blacky pro ball player”)

Mirtazapine (Tetracyclic)
(“mirth and misery” happy/sad mask)

Trazodone
(“cheerleader with Trombone”)

85
Q

Bupropion MOA

A

Inhibits reuptake of Norepinephrine and Dopamine via NET/DAT (“NET DAT ball pro”)

**no effects on serotonin !- no smiley symbols**

86
Q

what can Bupropion be used for ?

A

-atypical antidepressant that used for treatment of depression associated with hypersomnolance (daytime sleepness) since it has CNS activating effects via NE
(“depressed blue shirt boy aroused from sleep”) \

-can be used for treatment of tobbaco dependence
(“pros don’t smoke” sign)

-
Bupropion is less likely to cause weight gain
(“stay fit lose weight” sign )

-Bupropion doesn’t cause sexual dysfunction
(“kissing couple below the basket”)

88
Q

what are the adverse effects of Bupropion ?

A
  • can induce Seizures
  • Bupropion is contraindicated in Bulimia since it can lead to seizures (“shaking popcorn binge snacker”)
  • Bupropion is contraindicated in anorexia nervosa since it can lead to seizures
    (“shaking skinny blacky player”)

(“shaking proball player dunking”)

89
Q

Mirtazapine MOA

(“Mirth and Misery”)

A

-Blocks 5HT-2/5HT-3 receptors
(“retired shirts number 52 and 53 hanging “)
——————————————————————————–
-Mirtazapine blocks H1 receptors leading to

  • weight gain - good for depressed *anorexic
  • ​sedation - good for depressed with *insomnia

​——————————————————————————–
-blocks α2 receptors leading to increased 5HT/NE
(“extinguished double candle above cam screen and released smiley/compass balloons”)

90
Q

Trazodone MOA

A

-Trazodone is a Serotonin Modulator
(“marching drum player modulates serotonin smiley drum”)
-minimal effects on NE/Dopamine therefore Trombone far from “NET DAT BALL”
——————————————————————————–
-blocks 5HT-2 Receptors as well as inhibits reuptake
(“marching drum player wearing retired shirt 52”)
——————————————————————————–
-Trazodone is α1 antagonist receptors
(“lady tromboner holding single extinguished candle “)
——————————————————————————–
-inhibits H1 histamine receptors
(“Bee swatter player”)

91
Q

Trazodone adverse effects

A

-Trazodone can cause Priapism
(“TrazaBONER” male tromboner holding trombone in erected position)

-can cause orthostatic hypotension {via α1 antag.}
(“coach fainting on floor”)

-can cause Sedation {via H1 antagonism}
(“sleeping players on bench”)

-can cause sexual dysfunction
(“trombone player rejected by female player because he is out of her league yo’”)

-can cause Serotonin Syndrome
(“pile of smiley balls on floor”)

92
Q

what can Mirtazapine be used for ?

(“Mirth and misery”)

A
  • Atypical Antidepressants can be used as 1st line treatment of depression (“happy/sad mask” on cam screen):
  • some patients with depression are adminstered with Mirtazapine as 1st line of treatment when the adverse effects are actually desirable e.g.- elderly/anorexic {usually SSRIs}

​-Mirtazapine doesn’t cause sexual dysfunction
(“kiss-cam next to mirth/misery cam”)

93
Q

Name the mood stabilizers

(“stabilizing ski poles”)

A

Lithium (“lifthium lift”)

Valproate (“winter festiVAL”)

Carbamazepine (“classic car carved in ice”)

Lamotrigine (“kid on dads head wearing Llama outfit”)

Antipsychotics (“psychotic painting on high peak”)

94
Q

what is lithium useful for ?

(“lifthium lift”)

A
  • lithium can treat bipolar disorder ​
  • acute mania and maintenance

(“stabilizing chair lift” on “lifthium lift”)

95
Q

what are the side effects of lithium

A

-has very narrow therapeutic index
(“narrow window of opportunity to get off chair LIFTHIUM”)

-lithium therapy can cause hypothyroidism
(“pinguine on snowboard has undone bowtie”) which presents with :

  • weight gain (“fat ass snowboarder”)
  • ​dry skin
  • ​hair loss
  • ​constipation

-lithium can cause nephrogenic diabetes insipidus (“insipidus peeing kid fountain”)

-diuretics like thiazide and NSAIDs→ decrease GFR and clearance of lithium therefore increase lithium levels
(“kid thighs on high dive” and pole saying “low clearance”)

-lithium is teratogenic and can cause Ebsitein’s anomaly (“tarantula hat on yellow shirt girl”)

  • atrialization of the right ventricle occurs as well as ASD and tricuspid valve defects
    (“large right snow head looks defected”)

acute lithium toxicity

  • causes GI symptoms [nausea , vomiting ,diarrhea]
    (“early nauseated green shirt kid” )

chronic lithium toxicity

  • neurologic symptoms-tremor
    (“late trembling blacky girl”)
  • neurologic symptoms-ataxia
    (“late falling black kid”)
96
Q

what other drugs can be used to treat bipolar disorder?

A

Valproate (“winter festiVAL” sign)

  • acute mania and maintenance

Carbamazepine (“classic car carved in ice”)

  • acute mania and maintenance

1st [Haloperidol] and 2nd [Quetiapine] antipsychotics
(“psychotic paintings on high peak”)

  • acute mania

Lamotrigine (“child and dad wearing Llama outfit”)

  • maintenance only
97
Q

name the broad spectrum Antiepileptics

(“Seize the Land”)

A

Valproate
(“festiVAL reception)

Topiramate
(“Toupee”)

Lamotrigine
(“Llama”)

Levetiracetam
(“Elevator”)

98
Q

broad spectrum antiepiletpics MOA

A

-Increase Na+ channel inactivation

(“inactivated baskets of salty peanuts”)

-metabolized by the hepatic cytochrome CYP450 system

(“Chrome CYP450 canon on ship”)

99
Q

what are broad spectrum antiepileptic drugs used for ?

A
  • Focal Seizures
  • Generalized Seizures
  • Juvenile Myoclonic Epilepsy (J.M.E)
100
Q

Valproate

(“welcome festiVAL”)

A

-Increases Na+ channel inactivation
(“inactivated baskes of salty peanuts”)

-increases GABA levels in CNS
(“elevated Cab of king of incas”)

-can cause GI distress (nausea,vomiting)
(“incas king is nauseated “)

-can cause increased appetite and weight gain
(“king of incas is fat”)

-can cause Tremors
(“trembelling weapon baseball bat”)

-can cause Fatal hepatotoxicity
(“liver spot on inca cow”)

-can cause Pancreatitis
(“lady inca squeezing sponge”)

-valproate can be Teratogenic
(“Tarantula on inca shields”)

-valproate therapy during pregnancy can cause neural tube defects
(“inca has baby on her back playing the tubes”)

101
Q

Topiramate

(“admiral’s Toupee”)

A

-increase Na+ channel inactivation
(“inactivated baskes of salty peanuts”)

-allosterically binds to GABA-A receptor
(“admiral shaking hand of Cab-A’s inca driver”)

-can cause somnolence and fatigue
(“fatigued soldier behinnd admiral”)

-can cause confusion and cognitive slowing
(“soldier scratching his head behind admiral”)

-can cause weight loss
(“thin arm of canon operator”)

-topiramate can cause acute angle closure glaucoma
(“admirals helper holding high pressure eye kettle”)

-topiramate may increase the risk for Urolithiasis
(“canon balls next to admiral”)

102
Q

Lamotrigine

(“Llama”)

A

-increase Na+ channels inactivation
(“inactivated basket of salted peanuts”)

-can cause Stevens Johnson Syndrome /Toxic epidermal Necrolysis {SJS/TEN}
(“sloughed off mask of Llama rider”)

-Llamotrigine may cause diplopia
(“crossed eye camel”)

103
Q

Levetiracetam

(“elevator”)

A

-MOA not entirely known

-may cause somnolence
(“sleeping elevator operator”)

104
Q

name the narrow spectrum antiepileptics

(“Seize the night”)

A

Carbamazepine
(“classic car”)

Phenytoin
(“classic tow car”)

Gabapentin
(“Grab a pint! “ on ice-cream parlor)

Vigabatrin
(“raised V-Cab transmission”)

Tiagabine
(“tied up cab driver”)

105
Q

what can narrow spectrum antiepileptics be used for ?

A
  • useful in treatment of focal seizures
  • 2nd line agents used for maintainance during status epilepticus
106
Q

Carbamazepine

(“classic car”)

A

-1st line therapy for Trigeminal Neuralgia
(“three glowing gems”)
——————————————————————————–
-increases Na+ channel inactivation
(“inactivated salty chip bags”)

-induces CYP450
(“classic car Activated chrome plate CYP450”)

-can cause ataxia
(“unbalanced stack”)

-can cause diplopia
(“misaligned headlights of classic car”)

-can cause Drug Reaction with Eosinophilia and Systemic Symptoms Syndrome {DRESS}
(“eosinophilic dress of waiter 1”)

-carbamazepine is teratogenic
(“driver has tarantula shirt”)

-may cause Stevens Johnson Syndrome (SJS) (“sloughed off mask of passenger next to driver of classic car “)
——————————————————————————–
-Carbamazepine can cause SIADH
(“Inappropriate wet head of classic car driver”)

-can cause agranulocytosis
(“sand timer”)

-carbamazepine therapy during pregnancy can cause neural tube defects
(“neural tube exauhst”)

107
Q

Phenytoin

(“classic tow car”)

A

-increases Na+ channel inactivation
(“inactivated salty chip bags”)

-induces CYP450
(“classic car Activated chrome plate CYP450”)

-can cause ataxia
(“unbalanced stack with waiter 2 “)

-can cause diplopia
(“misaligned headlights of tow car”)

-can cause Drug Reaction with Eosinophilia and Systemic Symptoms syndrome {DRESS}
(“eosinophilic dress of waiter 2”)

-carbamazepine is teratogenic
(“towed car driver has tarantula shirt”)

-phenytoin may cause folate deficiency leading to megaloblstic anemia
(“spilled salad above tow car”)

-may cause gingival hyperplasia
(“expanding gum”)

-may cause hirsutism
(“trucker with big bushy beard”)

-phenytoin therapy during pregnancy may cause cleft palate
(“trucker’s cleft hat”)

-can decrease bone density
(“fractured osteoporotic towed car axle”)

108
Q

Carbamazepine and Phenytoin can both cause …

(“classic car and tow car”)

A

drug-induced Lupus

(“wolf between classic cars”)

109
Q

how should you treat Status Epilepticus

(“order status” sign)

A

-treat acutely with IV Benzodiazepines Diazepam, Lorazepam and Phenytoin (2nd line) for maintenance
(“Ben’s diner in the background behind cars”)

-if this treatment didn’t work IV Phenobarbital can be used to treat refractory seizures
(“barbershop in the background”)

110
Q

Gabapentin

(“Grab a pint! “ on ice-cream parlor)

A

-blocks voltage gated Ca+2 channels
(“closed Calci-YUM Ice cream cooler door”)

-useful for treatment of chronic pain
(“chronically frayed wire next to diasweeties machine”)

-can treat diabetic neuropathy
(“diasweeties machine “)

-useful for treatment of Fibromyalgia
(“fiber bars in 1st row of diasweeties machine”)

-useful in treatment of post-herpetic neuralgia
(“Zeus poppin from top of ice cream car”)

-can cause ataxia
(“unbalanced stack of ice cream balls”)

111
Q

Vigabatrin

(“raised V-Cab transmission”)

A

-irreversible inhibition of GABA-Transaminasedecrease GABA degradation

(“V-Cab _trans_mission”)

112
Q

Tiagabine

(“tied up cab driver”)

A

-inhibits GABA-Reuptake

(“tied up driver can’t be re-uptaken into cab”)

113
Q

Absence Seizures are characterized by …

(“Seize the day”)

A

-type of generalized seizure

-sudden momentary lapse in awareness accompanied by staring , blinking , clonic jerks
(“inattentive students”)

-absence seizures manifest as 3 Hz spike wave complexes on EEG
(“3 spikes” sign on wall”)

114
Q

what are the drugs used for treatment of Absence Seizures

A

Ethosuximide
(modes of persuation:”ETHOS”)

Valproate
(“farm festiVAL”)

Lamotrigine
(“Llama outside the class”)

115
Q

Ethosuximide

(“ETHOS”)

A

-useful in treatment of Absence seizures
(teacher holding “absences” clip board)

-Blocks voltage gated T-type Ca+2 channels in the thalamus
(closed Calci-YUM chocolate milk drink next to T thermos”)

-can cause GI distress ( nausea , vomiting)
(“kid gets punched in stomach by bitch-ass bully”)

-ethosuximide may cause lethargy and fatigue

116
Q

Valproate

(“farm fesiVAL”)

A

-valproate is effective against absence seizures

117
Q

Lamotrigine

(“Llama” outside of class)

A

-Lamotrigine is effective against absence seizures

118
Q

name the high potency 1st generation antipsychotics
(“kid high on roof”)

A

“van gogh’s starry gAZINg” - “azine” suffix

  • Haloperidol (“halo of gazing star”)
  • Trifluoperazine (“kid trying to fly”)

-Fluphenazine (“kid trying to fly”)

119
Q

1st Generation antipsychotics MOA

A

-block dopamine D2 receptors in the CNS espeicalliy in mesolimbic and striatofrontal system
(“Van Gogh holding double rope “)

-FGA’s have long half life and thus long duration of action since they’re highly lipophilic
(“kid on crazy peak holding long tapered flag”)

120
Q

name the low potency 1st Generation antipsychotics

(“van gogh’s coloring tools on floor”)

A

-Thioridazine
(“color THEORYdazine”)

-Chloropromazine
(“color-pro” paint on floor)

121
Q

what can 1st Generation Antipsychotics be used for?

A

-can treat positive symptoms of Schizophrenia-hallucinations , delusions , disorganised thoughts
(“Van Goch’s right ear is cut off thus blocking positive voices”)

-useful in treatment of acute psychosis in many condition {e.g. bipolar disorder}
(“kid on crazy peak holding flag”)

-may be used to treat aggitation , aggression
(“kid on agitated peak with marionette”)

-can be used for management of Tourette syndrome
(“tourette’s marionette with agitated aggressive blacky kid”)

122
Q

what are the characteristic features and side effects seen in low potency FGAs

(low potency > high potency)

A

-they have antimuscarininc effects including

  • dry mouth (“dry as a cracker”)
  • constipation
  • blurred vision (“blind as a bat”)
  • urinary retention

-blocks α1 receptors
(“nurse holding single extinguished candle”)

  • leads to orthostatic hypotension
    (“passed out couple in picture”)

​-blocks H1 histamine receptor
(“nurse holding bee swatter”)

  • leads to sedation
    (“picture with Van Gogh’s bed”)

(“alice in wonderland tea party picture”)

123
Q

what are the characteristic features and side effects seen in High potency FGAs

(low potency< high potency)

A

-high potency FGAs cause Extra Pyramidal Symptoms

  • Acute dystonia (“Cocked head”)/ in minutes
  • ​Akathisia (“falling chair”) /in days
  • ​Parkinsonism (“cogwheels of carriage”) /in weeks

-Can cause Tardive dyskinesia
(“kid in carriage sticking out his tongue”)
——————————————————————————–
-any drug blocking dopamine → hyperprolactinemia →galactorrhea, amenorrhea, impotence
(“kfc kid has white mustache”)
——————————————————————————-
-can cause Neuroleptic Malignant Syndrome
(kfc bucket says “now more spicy”)

  • generalized “lead pipe” rigidity
  • altered mental status, fever, autonomic instability
  • ​characterized by Rhabdomyolysis

(“kid on roof wearing extra pyramid hat”)

124
Q
  • *Side effects** seen after adminstration of First Generation Antipsychotics
  • *(low/high)**
A

-FGAs can cause Torsades de Pointes fatal cardiac arrhythmia (“twisted streamer”)

-can lower seizure threshold
(“shaking kid hanging on streamer”)

125
Q

Chlorpromazine

(“color-pro paint”)

A

-can cause corneal deposits

(“corn yellow color-pro paint”)

126
Q

Thioridazine

(“color THEORYdazine”)

A

-can cause retinal deposits
(“deposits on retinal color palette”)

127
Q

name the 2nd generation (atypical) antipsychotics

(“Dali the atypical surrealist”)

A

“quite please only whispering is appropriate “

Quetiapine
(“Quite”)

Olanzapine
(“Only”)

Risperidone
(“whispering”)

Aripiprazole
(“appropriate”)

Clozapine
(“clozapine closet”)

Ziprasidone
(“black dress zipper”)

128
Q

2nd generation (atypical) antipsychotics MOA

A

-block dopamine D2 receptors in the CNS
(“Dali holding double rope”)

-Block serotonin 5HT-2A receptor
(“cut smiley cheese”)

129
Q

what can 2nd generation (atypical) antipsychotics be used for ?

A

-SGAs are useful in treatment of both positive and negative symptoms of Schizophrenia
(“Dali hearing both positive and negative voices”)

-can treat resistant depression
(“resisting bottle” from chateu tyramine)

-useful in managment of OCD adjunctive with SSRIs
(“obssesively neat museum coworker aligning the pictures”)

-can help manage tourette syndrome
( Dali holding “tourett’s marionette”)

130
Q

what are the side effects associated with 2nd generation (atypical) antipsychotics

A

-block H1 histamine receptors

  • causes sedation
    (“passed out brown piece of shit in painting”)

-blocks α1 receptors
(“extinguished single candle on wall”)

  • ​causes orthostatic hypotension
    (“passed out brown piece of shit in painting”)

-SGAs block muscarinic receptors and have Antimuscarinic effects especially Clozapine but in general less antimuscarinic effects than FGAs

  • dry mouth
  • ​constipation
  • ​blurred vision
  • ​urinary retention

(“antimuscarinic tea party painting hanging behind clozapine closet and partialy covered”)

-SGAs , especially Olanzapine and Clozapine can cause

  • Weight gain
    (“fat face of brown piece of shit in painting”)
  • ​ Hyperglycemia
    (“bunch of candy on floor of painting”)
  • ​Dyslipidemia
    (“elevated butter” in painting)

​-SGAs can cause torsade de pointes
(“twisted torsades streamer all over the damn place”)

(coworker with “bee swatter” hitting bee paintings)

135
Q

Clozapine

(“Clozapine Closet”)

A

-can cause Agranulocytosis
(“melting sand timers”)

-can cause myocarditis and cardiomyopathy
(“surreal heart in melting painting”)

-clozapine reduces seizures threshold
(“shaking clock in melting painting”)

136
Q

what is the defining difference between 1st and 2nd generation antipsychotics ?

A
  • the defining difference is that in 2nd generation drug therapy the incidence of Extra Pyramidal Symptoms is reduced [EPS via blocking D2 Receptors]
    (“kid with EXTRA pyramid hat is causing disturbance and is asked to leave the exhibition”)

EPS include (FGA>SGA)

  • acute dystonia
  • ​akathisia
  • ​Parkinsonism

**Risperidone has the highest risk of causing EPS among SGAs**
(“whispering kid whisperes to EXTRA pyramid hat kid”)

-blocking D2 receptors leads to hyperprolactinemia [FGA>SGA]
(“disturbing kid has milk mustache”)
——————————————————————————-another difference is that the incidence of Neuroleptic Malignant Syndrome is also reduced but is still possible [FGA>SGA]

  • NMS Includes mental status changes , rigidity , autonomic instability , fever
  • ​NMS is associated with rhabdomyolysis
137
Q

Name the Drugs used for parkinson’s disease

A

Levodopa

DOPA decarboxylase inhibitor
Carbidopa

COMT inhibitor
Entacapone
Tolcapone

MAOi B
Selegiline

D receptor agonists
Ropinirole
Pramipexole

Endogenous Dopamine enhancement
Amantadine

Antimuscarinic Drugs
Trihexyphenidyl
​Benztropine

139
Q

side effects of Levodopa

A

-levodopa can cause GI distress
(due to peripheral conversion into dopamine)

  • levodopa can cause cardiac arrhythmias
    (due to peripheral conversion into dopamine)

-levodopa can cause orthostatic hypotension
(due to peripheral conversion into dopamine)

  • levodopa can cause neuropsychiatric symptoms e.g. anxiety, agitation, insomnia, confusion, hallucination (due to excess dopamine in the CNS)
  • chronic levodopa therapy can cause response fluctuations (wearing-off reaction, on-off phenomenon) and dyskinesias

-chronic levodopa therapy can cause a wearing-off reaction
(akinesia and dyskinesia re-emerge at the end of each dose)

-chronic levodopa therapy can cause an on-off phenomenon
(periods of akinesia alternate with periods of improved mobility, not related to dose)

-the therapeutic window of levodopa therapy narrows as Parkinson’s progresses

(unpredictable response to therapy) (“watch”)

  • chronic levodopa therapy can cause dyskinesias (choreoathetosis of the face and distal extremities)
  • levodopa is contraindicated in psychotic patients
140
Q

Carbidopa

A
  • carbidopa (peripheral DOPA decarboxylase inhibitor)
  • carbidopa increases the bioavailability of levodopa (prevents peripheral conversion into dopamine)
  • carbidopa decreases peripheral side effects of levodopa therapy

(but exacerbates neuropsychiatric side effects)

141
Q

Entacapone
Tolcapone

A
  • (COMT) converts dopamine to (3-MT) in the CNS
  • tolcapone (a peripheral and central COMT inhibitor) increases the bioavailability of levodopa
  • entacapone (a peripheral COMT inhibitor) increases the bioavailability of levodopa
  • tolcapone (a peripheral and _central C_OMT inhibitor) increases dopamine levels in CNS
  • tolcapone can cause hepatic failure
142
Q

Selegiline

A
  • monoamine oxidase B (MAO-B) selectively metabolizes dopamine
  • selegiline -a selective MAO-B inhibitor increases dopamine levels in the CNS
143
Q

Ropinirole
(“rope in a role”)

Pramipexole
(“big pex”)

A

Ropinirole (D2 dopamine receptor agonists)

is an important initial treatment of Parkinson’s
(“Rope in a roll”):

Pramipexole (D3 dopamine receptor agonist)

is an important initial treatment of Parkinson’s
———————————————————————————-

  • dopamine receptor agonists
    (e. g. ropinirole, pramipexole) treat restless leg syndrome (RLS)
  • dopamine receptor agonists (e.g. ropinirole) may enhance impulse control disorders
    (e. g. gambling, shopping, hypersexuality)
144
Q

Amantadine

A
  • amantadine enhances the effect of endogenous dopamine
    (by increasing its synthesis/release and inhibiting its uptake)
  • amantadine can treat some motor symptoms of Parkinson’s
145
Q

Trihexyphenidyl
Benztropine

A

-Trihexyphenidyl and Benztropine
(antimuscarinic agents used to treat parkinsonism)

-trihexyphenidyl and benztropine (antimuscarinic agents) improve tremor and rigidity of Parkinson’s with no effect on bradykinesia

146
Q

Levodopa metabolism

A

L-DOPA → Dopamine in periphery + CNS

Levodopa can cross BBB
Dopamine can’t cross BBB

147
Q

what is the mechanism of action by which opiates exert their effects ?

A
  • opiates are μ-opioid receptor agonists
    (“μssage parlor”)

-activation of opiate receptors leads to opening of K+ ion channel causing hyperpolarization
(“open banana barrels in the back”)

-activation of opiate receptors closes Voltage Dependent Ca+2 channel
(“closed Calci-YUM ice cream cooler next to bananas”)

-closure of Voltage Dependent Ca+2 channel prevents release of neurotransmitters basically stopping the pain signaling in the brain

(“worker disconnecting presynaptic wire from icecream cooler”)

149
Q

Name the Semi Synthetic opiates and classify them according to their strength

A

Strong
Heroin
Oxycodone

Weak/Intermediate
Dihydrocodeine

Mixed Agonist/Antagonist

Buprenorphine
Nalbuphine

150
Q

Tramadol properties

(“synthetic weak/intermediate”)

A

a weak μ-opioid receptor agonist used to manage chronic pain

  • inhibits reuptake of norepinephrine and serotonin
    (“North-South”)

(“Distant tram”)

151
Q

Names of opiates agonists

A

Fentanyl (opioid analgesic)
(“Fantasy”)

Morphine (opioid analgesic)
(“More fun”)

Tramadol
(“Distant tram”)

(a weak μ-opioid receptor agonist used to manage chronic pain)

152
Q

Codeine
(“Barcode”)

Orphan
(“dextromethorphan”)

Properties

A

Opioid antitussives

  • dextromethorphan antagonizes NMDA receptors
    (“Tethered nomadic camel”)
153
Q

Opiates Side Effects

A

cause CNS depression (e.g.sedation)
(“Cerebral towel”)

-opiates can cause respiratory depression
(“Deflated lung vest”)

-opiates cause miosis (constricted pupils)
(“Constricted hood”)

-can cause constipation
(“Plunger”)

-can cause biliary colic (contract biliary smooth muscle)
(“Biliary tree”)

-patients may develop tolerance to opiates

(“All are welcome”)

  • tolerance does not develop for miosis or constipation
    (“Out of order””)

​-opiate induced hyperalgesia can occur with chronic use
(“Causing pain”)

-opioid withdrawal
(“Anxious, hot, and moist”)

  • rhinorrhea
  • lacrimation
  • yawning
  • hyperventilation
  • hyperthermia
  • muscle aches
  • vomiting
  • diarrhea
  • anxiety
154
Q

Methadone
(“DONE timer”)

Properties

A

long acting opioid used to attenuate withdrawal symptoms

  • methadone and buprenorphine have a long half lives used in opioid detoxification
    (“Long tapering flag”)
156
Q

Loperamide
(“Lop-eared rabbit”)

Diphenoxylate
(“Dolphins”)

properties

A

μ-opioid receptors are located in the GI tract delay stool transit

  • can be used as antidiarrheals
    (“Removed muddy slippers”)
  • Loperamid increases colonic phasic segmentation → increase stool transit time
    (“Loping back and forth”)
160
Q

Buprenorphine

Properties

A

long acting partial μ-opioid agonist used to attenuate withdrawal symptoms

161
Q

partial μ-opioid agonists

Buprenorphine
Nalbuphine
​Butorphanol

Properties

A

partial μ-opioid agonists can induce withdrawals

162
Q

Naloxone use

(“No lax zone”)

A

μ-opioid antagonist used to reverse acute opioid toxicity

  • can precipitate withdrawals
163
Q

Naltrexone use

(“No tricks zone”)

A

μ-opioid antagonist

helps maintain abstinence in heroin addicts
(“no tricks zone just results”)

helps reduce cravings for alcohol and nicotine
(“Tempting alcohol”)

naltrexone can help with weight loss
(“Getting fit”)

164
Q

Name the Synthetic Opiates

A

Strong

Meperidine
Fentanyl
Methadone

Weak/ Intermediate

Diphenoxylate
Loperamide
Tramadol